New Drug Approvals

Opakalim

DR ANTHONY MELVIN CRASTO Ph.D — Mon, 20 Jul 2026 02:33:22 +0000

Opakalim

CAS 2376397-93-0

MF C18H22F2N4O MW 348.4 g/mol

N-(1-tert-butyl-6-cyano-4,7-difluorobenzimidazol-2-yl)-3,3-dimethylbutanamide

N-(1-tert-butyl-6-cyano-4,7-difluoro-1H-1,3-benzimidazol-2-yl)-3,3-dimethylbutanamide
potassium channel activator, antiepileptic, BHV-7000; BHV7 000, BPN-25203, BPN 25203, KB-3061, KB 3061, 73H9J7RBA2

BHV-7000 is under investigation in clinical trial NCT06419608 (Efficacy and Safety Study of BHV-7000 Monotherapy in Major Depression).

Opakalim (also known as BHV-7000) is an investigational, small-molecule medication that acts as a selective activator of Kv7.2 and Kv7.3 potassium channels. Developed by Biohaven Pharmaceuticals, it targets a clinically validated pathway to regulate neuronal hyperexcitability, primarily for the treatment of epilepsy and focal seizures.

Key Characteristics

Mechanism of Action: It opens Kv7.2/7.3 potassium channels. This stabilizes electrical activity in the brain. Unlike older class drugs, it has minimal to no (GABA_A) receptor activity.
Safety Benefit: Its precision prevents typical central nervous system side effects. Patients experience much lower rates of somnolence, fatigue, and severe dizziness compared to other anti-seizure medications.
Administration: It is taken orally once a day. It requires no titration period before reaching therapeutic dosing.

Current Clinical Status

Refractory Focal Epilepsy: The drug is undergoing phase 2/3 clinical evaluation. The pivotal RISE 3 study completed patient enrollment, with high-profile top-line efficacy data anticipated in the second half of 2026.
Idiopathic Generalized Epilepsy (IGE): Recent clinical data highlights a three-fold prolongation in the time to a second generalized tonic-clonic seizure compared to a placebo.
Other Explored Indications: While it is actively tested for conditions like bipolar disorder and erythromelalgia (pain), an exploratory phase 2 trial for major depressive disorder failed to meet its primary goals.

Opakalim (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code names BHV-7000, BPN-25203, and KB-3061) is a highly selective K_v7.2 and K_v7.3 potassium channel opener which is under development for the treatment of bipolar disorders, epilepsy, partial epilepsies, major depressive disorder, erythromelalgia, pain, infantile spasms, and mood disorders.^[1][2][3][4] It is taken orally.^[1] The drug was originated by Channel Biosciences and was under development by Biohaven Pharmaceuticals or Biohaven Therapeutics.^[1][2] As of April 2026, it is in phase 2/3 clinical trials for bipolar disorders, epilepsy, and partial epilepsies, phase 2 trials for major depressive disorder, and phase 1 trials for erythromelalgia and pain, whereas no recent development has been reported for infantile spasms and mood disorders.^[1][2] A phase 2 trial for major depressive disorder failed to meet its primary efficacy endpoint, resulting in focus more on epilepsy instead.^[3]

Study to Determine if BHV-7000 is Effective and Safe in Adults With Refractory Focal Onset EpilepsyCTID: NCT06309966Phase: Phase 2/Phase 3Status: Active, not recruitingDate: 2026-07-01
A Study to Determine if BHV-7000 is Effective and Safe in Adults With Refractory Focal Onset EpilepsyCTID: NCT06132893Phase: Phase 2/Phase 3Status: RecruitingDate: 2026-05-01
Long-term Safety and Tolerability of BHV-7000CTID: NCT06443463Phase: Phase 2Status: Enrolling by invitationDate: 2026-05-01
A Phase 1b Study of BHV-7000 in Participants With Inherited ErythromelalgiaCTID: NCT07262268Phase: Phase 1Status: Enrolling by invitationDate: 2026-04-08
Long-term Safety Study of BHV-7000 in Participants With Major Depressive Disorder (MDD)CTID: NCT06423781Phase: Phase 2Status: CompletedDate: 2026-04-01
A Study to Determine if BHV-7000 is Effective and Safe in Adults With Idiopathic Generalized Epilepsy With Generalized Tonic-clonic SeizuresCTID: NCT06425159Phase: Phase 2/Phase 3Status: TerminatedDate: 2026-03-24
Efficacy and Safety Study of BHV-7000 Monotherapy in Major DepressionCTID: NCT06419608Phase: Phase 2Status: CompletedDate: 2026-01-07
BHV-7000 Acute Treatment of Bipolar ManiaCTID: NCT06419582Phase: Phase 2/Phase 3Status: CompletedDate: 2025-12-16
BHV-7000 Open-Label Extension Bipolar Mania StudyCTID: NCT06423794Phase: Phase 2Status: TerminatedDate: 2025-12-16

PAT

[US20230000831]

https://patentscope.wipo.int/search/en/detail.jsf?docId=US383826737&_cid=P20-MRSLRP-32698-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2025035066&_cid=P20-MRSLVM-39325-2

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References

Kv7 channel activators compositions and methods of usePublication Number: US-11724990-B2Priority Date: 2018-03-19Grant Date: 2023-08-15
KV7 channel activators compositions and methods of usePublication Number: US-12286408-B2Priority Date: 2018-03-19Grant Date: 2025-04-29
KV7 channel activators compositions and methods of usePublication Number: US-11261162-B2Priority Date: 2018-03-19Grant Date: 2022-03-01
Kv7 channel activators compositions and methods of usePublication Number: US-2019284142-A1Priority Date: 2018-03-19
Kv7 channel activators compositions and methods of usePublication Number: US-10851067-B2Priority Date: 2018-03-19Grant Date: 2020-12-01
KV7 channel activator composition and method of use thereofPublication Number: KR-20200133259-APriority Date: 2018-03-19
Kv7 channel activators compositions and methods of usePublication Number: US-2021130299-A1Priority Date: 2018-03-19
KV7 channel activator composition and method of use thereofPublication Number: KR-102731128-B1Priority Date: 2018-03-19Grant Date: 2024-11-18
Methods of use for kv7 channel activatorsPublication Number: US-2025312316-A1Priority Date: 2019-09-17
Methods of use for KV7 channel activatorsPublication Number: US-12370176-B2Priority Date: 2019-09-17Grant Date: 2025-07-29
How to use KV7 channel activatorPublication Number: CN-118986972-APriority Date: 2019-09-17
Kv7 channel activators compositions and methods of usePublication Number: US-2024002349-A1Priority Date: 2018-03-19
Kv7 channel activators compositions and methods of usePublication Number: US-2023000831-A1Priority Date: 2018-03-19

References

“Biohaven Pharmaceuticals”. AdisInsight. 15 April 2026. Retrieved 31 May 2026.
“Delving into the Latest Updates on Opakalim with Synapse”. Synapse. 2 April 2026. Retrieved 31 May 2026.
Pelorosso C, Balestrini S, Guerrini R (May 2026). “Potassium channel agonists emerging as treatment options for focal epilepsy: are we breaking new ground?”. Expert Opinion on Emerging Drugs: 1–8. doi:10.1080/14728214.2026.2675274. hdl:2158/1473832. PMID 42153277.
Pong AW (December 2025). “Expanding the toolkit: An update on the evolution of new therapies for Lennox-Gastaut Syndrome”. Seminars in Pediatric Neurology. 56 101242. doi:10.1016/j.spen.2025.101242. PMID 41371876.

Clinical data

Other names	BHV-7000; BHV7000; BPN-25203; BPN25203; KB-3061; KB3061
Routes of administration	Oral^[1]
Drug class	K_v7.2 and K_v7.3 potassium channel opener
Identifiers
IUPAC name
CAS Number	2376397-93-0
PubChem CID	139487180
DrugBank	DB22041
ChemSpider	129910012
UNII	73H9J7RBA2
KEGG	D13061
Chemical and physical data
Formula	C₁₈H₂₂F₂N₄O
Molar mass	348.398 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

////////opakalim, anax labs, potassium channel activator, antiepileptic, BHV-7000; BHV7 000, BPN-25203, BPN 25203, KB-3061, KB 3061, 73H9J7RBA2

Ontunisertib

DR ANTHONY MELVIN CRASTO Ph.D — Sat, 18 Jul 2026 02:34:47 +0000

Ontunisertib

CAS 2647949-48-0

MFC27H21F2N5O MW469.5 g/mol

N-[(2,6-difluorophenyl)methyl]-2-[3-(6-methyl-2-pyridinyl)-4-quinolin-4-ylpyrazol-1-yl]acetamide

N-(2,6-difluorobenzyl)-2-(3-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazol-1-yl)acetamide

N-[(2,6-difluorophenyl)methyl]-2-[3-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazol-1-yl]acetamide
serine/threonine kinase inhibitor, AGMB 129, SF6HGC94LK

Ontunisertib (AGMB-129) is an experimental, orally active small-molecule drug developed by Agomab Therapeutics to treat Fibrostenosing Crohn’s Disease (FSCD). It acts as a highly selective inhibitor of ALK5 (also known as Transforming Growth Factor-beta type I receptor or TGF-β RI).

Mechanism of Action

Local Targeting: Designed to act specifically within the gastrointestinal (GI) tract.
High Tissue Exposure: Provides high local exposure in inflamed and scarred intestinal tissues.
Liver Inactivation: Undergoes rapid first-pass metabolism in the liver immediately after GI absorption.
Safety Feature: Converts into an inactive metabolite to prevent systemic exposure and avoid cardiac toxicity.

Clinical Development Status

FDA Status: Granted Fast Track Designation by the U.S. FDA.
Phase 2a Results: Successfully completed the STENOVA clinical trial. Results demonstrated excellent safety, high local tissue penetration, and positive structural improvements in bowel strictures.
Phase 2b Trial: Enrolling patients for the global, 52-week NOV-ERA trial to test multiple doses against a placebo. The primary goal is assessing the endoscopically confirmed widening of narrowed intestinal strictures

NOV-ERA – A Clinical Trial to Assess the Efficacy and Safety of Ontunisertib Compared to Placebo in Patients With Fibrostenosing Crohn’s DiseaseCTID: NCT07683325Phase: Phase 2Status: Not yet recruitingDate: 2026-07-06
Human Mass Balance Study of [14C] Ontunisertib in Healthy VolunteersCTID: NCT07672574Phase: Phase 1Status: Not yet recruitingDate: 2026-06-29
A Multiple Ascending Dose Study With AGMB-129 in Healthy ParticipantsCTID: NCT07118878Phase: Phase 1Status: CompletedDate: 2025-11-21
STENOVA – A Study to Evaluate Safety, Tolerability, PK and PD of AGMB-129 in Patients With Fibrostenotic Crohn’s DiseaseCTID: NCT05843578Phase: Phase 2Status: Active, not recruitingDate: 2025-11-21
Drug-Drug Interaction Study With AGMB-129 and Midazolam in Healthy ParticipantsCTID: NCT05937386Phase: Phase 1Status: CompletedDate: 2024-06-18

SYN

US12297186, Example 24

SYN

[WO2021105317A1]

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2021105317&_cid=P20-MRPQUQ-14721-1

Example 24: N-(2,6-difluorobenzyl)-2-(3-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazol-1 -yl)acetamide

¹H-NMR (300 MHz, DMSO-d₆): δ = 8.84 (d, J = 4.4 Hz, 1H), 8.76 (t, J = 5.3 Hz, 1H), 8.11-7.97 (m, 2H), 7.75-7.28 (m, 7H), 7.13 (t, J = 7.8 Hz, 2H), 6.97 (d, J = 7.5 Hz, 1 H), 4.99 (s, 2H), 4.43 (d, J = 5.3 Hz, 2H), 1.83 (s, 3H).

HPLC-MS: Rt 17.513 m/z 470.0 [M+H]⁺.

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2025176835&_cid=P20-MRPR39-19345-1

Potent inhibitors of TGFpRII-TGFpRI (ALK5) have been described in W02021/105317 including the compound (/V-(2,6-difluorobenzyl)-2-(3-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)-1/7-pyrazol-1-yl)acetamide) which is the compound of formula (I) as shown below (see Example 24):

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References

///////////ontunisertib, anax labs, serine/threonine kinase inhibitor, AGMB 129, SF6HGC94LK

Olisutrigine bromide

DR ANTHONY MELVIN CRASTO Ph.D — Mon, 13 Jul 2026 02:33:00 +0000

Olisutrigine bromide

Cas 1393836-45-7

MF C25H35BrN2 MW443.5 g/mol

N-[2-[(2R)-1,1-dimethylpiperidin-1-ium-2-yl]ethyl]-N-(2-methylphenyl)-2,3-dihydro-1H-inden-2-amine bromide

(2R)-2-{2-[N-(2,3-dihydro-1H-inden-2-yl)-2-methylanilino]ethyl}-1,1-dimethylpiperidin-1-ium bromide
sodium channel blocker, analgesic, ASN008, ASN 008, EN 3427, 0M9Q318030

Olisutrigine bromide (also known as ASN-008 or EN3427) is an investigational, permanently charged sodium channel blocker being studied for its potent, long-lasting analgesic (pain-relieving) properties.

Key Characteristics

Mechanism of Action: It acts as a membrane-impermeant sodium channel blocker. Because it carries a permanent cationic charge, it cannot easily cross healthy cell membranes on its own.
Targeted Delivery: It often requires a “vehicle” or a combination drug (like lidocaine) to activate specific channels (such as TRP channels), allowing olisutrigine entry into pain-sensing neurons where it becomes entrapped and blocks pain signaling.
Efficacy: Rodent pain models demonstrate that its analgesic effects are significantly longer-lasting than lidocaine alone.
Chemical Profile: Its molecular formula is C₂₅H₃₅BrN₂ with a molecular weight of 443.5 g/mol, and its CAS registry number is 1393836-45-7.

Current Status

Investigational Drug: It is not approved for human or veterinary medical use and remains in the research and development phase.
Availability: It is strictly available as a reference standard compound for laboratory and preclinical research through chemical suppliers like MedChemExpress and BenchChem.

A Study to Evaluate the Anti-pruritic Effectiveness of ASN008 in Adults With Mild to Moderate Atopic Dermatitis

CTID: NCT05870865

Phase: Phase 2

Status: Completed

Date: 2025-05-16

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2012112969&_cid=P11-MRILQZ-81481-1

Example 43: General Procedure M – Preparation of (R)-1,1 -dimethyl-2-[2-((indan-2-yl)(2-methylphenyl)amino)ethyl]piperidinium bromide

Alcohol 37b was synthesized as previouslydescribed (Tetrahedron 2007, 63, 3000-3005)

To a 250 mL round bottom flask was charged 2-(2-hydroxyethyl)piperidine-1-carboxylic acid tert-butyl ester 37b (5.0 g, 21.80 mmol), dichloromethane (7.50 mL), a solution of KBr (0.52 g, 4.36 mmol) in 2.0 mL of water and TEMPO (0.1 g, 0.64 mmol). The mixture was cooled to about -5 °C. A solution of NaOCl (31.1 mL, 5.25%, 24.1 mmol) was added slowly over 20 minutes while maintaining the temperature at 0 °C. The mixture was further stirred at 0°C for 20 minutes. The organic layer was separated, and the aqueous layer was extracted with

dichloromethane. The combined dichloromethane extract was washed with water (50 mL), followed by brine. After drying over MgSO₄, the mixture was filtered and concentrated. The crude was purified with silica gel column chromatography to give product 38b (4.1 g, 83%) as colorless oil.

To a clean and dry 250 mL round bottom flask was charged sodium triacetoxyborohydride (5.59 g, 26.40 mmol), 4 A molecular sieves (10.0 g), amine 7e (7.37 g, 33.00 mmol) and dichloromethane (20.0 mL). The mixture was stirred and cooled to about 0 °C, and a solution of aldehyde 38b (5.0 g, 22.00 mmol) in 40 mL of dichloromethane was added. The mixture was then stirred further at 0 °C for about 1 hour and at ambient temperature for an additional 40 minutes. The reaction mixture was quenched with aqueous saturated NaHCO₃ (100 mL). After separation of organic layer, the mixture was extracted with dichloromethane. After drying over MgSO₄, the organic layer was concentrated. The crude product was purified by silica gel column chromatography to give product 40f (7.2 g, 75.3%) as colorless oil.

To a clean and dry 250 mL round bottom flask was charged lithium aluminum hydride (1.53 g, 40.27 mmol) and THF (30.0 mL). The mixture was heated to reflux. A solution of carbamate 40f (7.0 g, 16.11 mmol) in THF (40.0 mL) was added dropwise over 5 minutes. After refluxing for 15 h, the reaction mixture was cooled to 0 °C, and water (1.55 mL) was added slowly and carefully, followed by THF (100 mL) and 15% NaOH (1.55 mL). After stirring the mixture at room temperature for 1.0 h, MgSO₄ was added, and the mixture was stirred further for 15 minutes. The mixture was filtered and concentrated to obtain the crude product, which was purified by silica gel column chromatography to afford product 11e (4.7 g, 84%) as pale yellow oil. Optical purity by chiral HPLC: 99.3% ee.

To a clean and dry 250 mL round bottom flask was charged diamine 11e (4.70 g, 13.49 mmol) and 1.07 M bromomethane in MTBE (126.0 mL, 134.8 mmol). After stirring at room temperature for 20 h, the reaction mixture was filtered. The solid cake was washed with MTBE to give the product (4.40 g, 73%) as white powder. Optical purity by chiral HPLC: 99.3% ee.

PAT

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=53D672FEEE9931FFC5F125D61A00D7FA.wapp1nB?docId=WO2026050699&_cid=P11-MRILJW-76628-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2025250498&_cid=P11-MRILME-78328-1

Compound 1 is described in WO2012/112969, wherein Compound 1 is reported at Example 43, and certain formulations of Compound 1 are described in WO2020/113050,

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References

AMINOINDANE COMPOUNDS AND THEIR APPLICATION FOR THE TREATMENT OF PAIN

Publication Number: RU-2013142433-A

Priority Date: 2011-02-18

Aminoindane compounds and use thereof in treating painPublication Number: US-8865741-B2Priority Date: 2011-02-18Grant Date: 2014-10-21
Aminoindan compound and its use in treating painPublication Number: CN-107540599-BPriority Date: 2011-02-18Grant Date: 2021-06-04
Aminoindane compounds and their use in the treatment of painPublication Number: ES-2675510-T3Priority Date: 2011-02-18Grant Date: 2018-07-11
Aminoindane compounds and use thereof in treating painPublication Number: EP-2675787-B1Priority Date: 2011-02-18Grant Date: 2018-03-28
AMINOINDANE COMPOUNDS AND THEIR APPLICATION FOR THE TREATMENT OF PAINPublication Number: RU-2016151688-APriority Date: 2011-02-18
Aminoindane compounds and use thereof in treating painPublication Number: RU-2612959-C2Priority Date: 2011-02-18Grant Date: 2017-03-14
AMINOINDAN COMPOUNDS AND USE THEREOF IN THE TREATMENT OF PAINPublication Number: DK-2675787-T3Priority Date: 2011-02-18Grant Date: 2018-07-16
Load Aminoinden Compounds and Therapeutic Compounds Containing Them and Uses in the Treatment of Itching and PainPublication Number: IL-227967-APriority Date: 2011-02-18
Aminoindane compounds and use thereof in treating painPublication Number: EP-3363437-B1Priority Date: 2011-02-18Grant Date: 2021-07-28
Aminoindane compounds and use thereof in treating painPublication Number: KR-20200125765-APriority Date: 2011-02-18
Aminoindane compounds and use thereof in treating painPublication Number: WO-2012112969-A1Priority Date: 2011-02-18
Aminoindane compounds and use thereof in treating painPublication Number: CA-2826648-CPriority Date: 2011-02-18Grant Date: 2019-06-04
Aminoindane compounds for use in treating urological painPublication Number: EP-3970723-A1Priority Date: 2011-02-18
Aminoindane compounds and use thereof in treating painPublication Number: CA-2826648-A1Priority Date: 2011-02-18
Aminoindane Compounds and Use Thereof in Treating PainPublication Number: US-2012214809-A1Priority Date: 2011-02-18
Use of aminoindane compounds in treating overactive bladder and interstitial cystitisPublication Number: US-9044482-B2Priority Date: 2012-08-15Grant Date: 2015-06-02
Aminoindane compounds and their use in the treatment of painPublication Number: ES-2898910-T3Priority Date: 2011-02-18Grant Date: 2022-03-09
Aminoindane compounds and use thereof in treating painPublication Number: AU-2012219254-A1Priority Date: 2011-02-18
Aminoindane compounds and use thereof in treating painPublication Number: EP-2675787-A1Priority Date: 2011-02-18
Aminoindane compounds and use thereof in treating painPublication Number: EP-3363437-A1Priority Date: 2011-02-18
6-(4-Nitro-phenoxy)-2H-pyridazin-3-one and 6-(4-amino-phenoxy)-2H-pyridazin-3-one as intermediates of thyroid hormone analogs The preparation method of ketone derivativePublication Number: CN-116406356-APriority Date: 2020-10-23
Use of Aminoindane Compounds in Treating Overactive Bladder and Interstitial CystitisPublication Number: US-2014051702-A1Priority Date: 2012-08-15
Use of aminoindane compounds in treating overactive bladder and interstitial cystitisPublication Number: US-2015290182-A1Priority Date: 2012-08-15
Use of aminoindane compounds in treating overactive bladder and interstitial cystitisPublication Number: US-9375423-B2Priority Date: 2012-08-15Grant Date: 2016-06-28
Use of aminoindane compounds in treating overactive bladder and interstitial cystitisPublication Number: WO-2014028675-A1Priority Date: 2012-08-15

///////////olisutrigine bromide, anax labs, sodium channel blocker, analgesic, ASN008, ASN 008, EN 3427, 0M9Q318030

Netanasvir

DR ANTHONY MELVIN CRASTO Ph.D — Sun, 12 Jul 2026 02:30:51 +0000

Netanasvir

CAS 2007900-70-9

MF C51H58N8O7 MW895.1 g/mol

methyl N-[(1R)-2-[(2S,4S)-2-[5-[7-[2-[(2S,5S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]-5-methylpyrrolidin-2-yl]-3H-benzo[e]benzimidazol-7-yl]-2,3-dihydro-1H-inden-4-yl]-1H-imidazol-2-yl]-4-(methoxymethyl)pyrrolidin-1-yl]-2-oxo-1-phenylethyl]carbamate

antiviral, Dongweizhuo, HCV, Antaitavir Hasophate, HEC 74647 PA, 4Y7YD32BYY

Netanasvir (commonly prescribed as netanasvir phosphate) is a direct-acting antiviral medication primarily used to treat chronic hepatitis C virus (HCV) infection. It was approved by the China National Medical Products Administration (NMPA) under the trade name Dongweizhuo.

Key Clinical Information

Mechanism of Action: It acts as a potent and selective NS5A inhibitor. By targeting the HCV NS5A protein, it successfully blocks viral RNA replication, virion assembly, and viral clearance mechanisms.
Combination Therapy: It is exclusively indicated for use in combination with encofosbuvir (an NS5B polymerase inhibitor).
Target Genotypes: The combination regimen effectively treats adult patients with chronic HCV genotypes 1, 2, 3, or 6.
Patient Profiles: It is suitable for patients who are either treatment-naïve or have been previously treated with interferon, with or without compensated liver cirrhosis.
Administration & Elimination: Taken orally, the drug demonstrates high metabolic stability, with feces serving as its primary elimination pathway

OriginatorSunshine Lake Pharma
ClassAntivirals
Mechanism of ActionHepatitis C virus NS 5 protein inhibitors
RegisteredHepatitis C
08 Feb 2025Registered for Hepatitis C (Combination therapy, Treatment-experienced) in China (PO)
08 Feb 2025Registered for Hepatitis C (Combination therapy, Treatment-naive) in China (PO)
31 Dec 2023NMPA, China accepts NDA for netanasvir for Hepatitis C for review

Netanasvir is an antiviral drug used to treat hepatitis C virus (HCV).^[1] In China, netansavir is approved for use in combination with encofosbuvir for the treatment of adult patients with chronic HCV genotypes 1, 2, 3, or 6, who are either treatment-naive or have been previously treated with interferon.^[2]

PAT

Compounds as hepatitis c virus inhibitors and pharmaceutical uses thereof

Publication Number: WO-2016141890-A1

Priority Date: 2015-03-12

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2016141890&_cid=P22-MRH62L-18160-1

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References

“Netanasvir phosphate – Sunshine Lake Pharma”. Adis Insight. Springer Nature Switzerland AG.
“Netanasvir Phosphate Capsules Approved for Marketing by China NMPA”. National Medical Products Administration. 2025-06-11.

Clinical data

Trade names	东卫卓; Dongweizhuo
Legal status
Legal status	Rx in China
Identifiers
IUPAC name
CAS Number	2007900-70-9
PubChem CID	122535557
UNII	4Y7YD32BYY
Chemical and physical data
Formula	C₅₁H₅₈N₈O₇
Molar mass	895.074 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

//////////netanasvir, anax labs, APPROVALS 2025, CHINA 2025, antiviral, Dongweizhuo, HCV, Antaitavir Hasophate, HEC 74647 PA, 4Y7YD32BYY

Nelremagpran

DR ANTHONY MELVIN CRASTO Ph.D — Fri, 10 Jul 2026 02:25:01 +0000

Nelremagpran

CAS 2492595-24-9

MFC15H9ClF4O3 MW 348.67 g/mol

3-[[2-Chloro-4-(trifluoromethyl)phenoxy]methyl]-2-fluorobenzoic acid

3-{[2-chloro-4-(trifluoromethyl)phenoxy]methyl}-2-fluorobenzoic acid
Mas-related G protein-coupled receptor inverse agonist, anti-inflammatory, MRGPRX4 modulator-2, BL83FAK6DZ,

Nelremagpran is an experimental drug that acts as a potent and selective antagonist (or possibly inverse agonist) of the MAS-related Gq protein-coupled receptor X4 (MRGPRX4). It has antiinflammatory effects in animal studies. This receptor is poorly characterised but is thought to be involved in immune system function, and development of selective ligands is essential for researching its role in the body.^[1][2]

Nelremagpran is an experimental drug that acts as a potent and selective antagonist or inverse agonist of the Mas-related G-protein-coupled receptor X4 (MRGPRX4). It was initially developed by Escient Pharmaceuticals, Inc. for its anti-inflammatory and anti-itch properties.

Core Mechanism

The drug targets MRGPRX4, a poorly characterized receptor found in the immune and nervous systems. It functions with high potency, exhibiting an half-maximal inhibitory concentration (IC50) of less than 100 nM.

Potential Research Applications

Because the receptor plays a significant role in mediating severe itch and pain pathways, Nelremagpran is actively used as a chemical probe to study:

Chronic Pruritus: Conditions involving persistent, debilitating itch sensations, such as cholestatic pruritus.
Autoimmune Diseases: Underlying mechanisms in conditions like psoriasis, multiple sclerosis, and Stevens-Johnson Syndrome.
Inflammatory Sensation: How the body signals pain and immune hypersensitivity

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020198537&_cid=P12-MREAZN-03524-1

Synthesis of Compound 1-55

Step 4-4. Synthesis of methyl 3-(bromomethyl)-2-fluorc>benzoate (INT 4-C)

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References

Identifiers

IUPAC name
CAS Number	2492595-24-9
PubChem CID	155145968
ChemSpider	115008493
UNII	BL83FAK6DZ
ChEMBL	ChEMBL4855031
Chemical and physical data
Formula	C₁₅H₉ClF₄O₃
Molar mass	348.68 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

References

WO 2020/198537, Yeager A, Selfridge B, Sainz M, Martinborough E, Boehm M, Huang, “Modulators of mas-related G-protein receptor x4 and related products and methods.”, published 1 October 2020, assigned to Escient Pharmaceuticals, Inc.
“International Nonproprietary Names for Pharmaceutical Substances (INN)” (PDF). WHO Drug Information. 38 (4). 2024.

Modulators of Mas-related G-protein receptor X4 and related products and methodsPublication Number: US-11840521-B2Priority Date: 2019-03-28Grant Date: 2023-12-12
Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: EP-3946304-A1Priority Date: 2019-03-28
Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: US-2023159474-A1Priority Date: 2019-03-28
Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: US-2023053860-A1Priority Date: 2019-03-28
Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: US-2021032213-A1Priority Date: 2019-03-28
Modulators of mas-related G-protein receptor X4 and related products and methodsPublication Number: US-11643399-B2Priority Date: 2019-03-28Grant Date: 2023-05-09
Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: US-2024300907-A1Priority Date: 2019-03-28
Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: WO-2020198537-A1Priority Date: 2019-03-28
Modulators of MAS-related G protein receptor X4 and related products and methodsPublication Number: CN-113939288-BPriority Date: 2019-03-28Grant Date: 2025-04-25

//////////nelremagpran, anax labs, Mas-related G protein-coupled receptor inverse agonist, anti-inflammatory, MRGPRX4 modulator-2, BL83FAK6DZ,

Nedizantrep

DR ANTHONY MELVIN CRASTO Ph.D — Wed, 08 Jul 2026 02:26:30 +0000

Nedizantrep

CAS 2376824-99-4

MF C20H19ClN6O3 MW 426.9 g/mol

1-[[3-[(3R,5R)-5-(4-chlorophenyl)oxolan-3-yl]-1,2,4-oxadiazol-5-yl]methyl]-2,7-dimethylpurin-6-one

1-({3-[(3R,5R)-5-(4-chlorophenyl)oxolan-3-yl]-1,2,4-oxadiazol-5-yl}methyl)-2,7-dimethyl-1,7-dihydro-6Hpurin-6-one
transient receptor potential (TRP) ion channel antagonist, GDC-6599, GDC 6599, RG 6341, RG-6341, ENQ95FVE4X

Nedizantrep (also known by its developmental code GDC-6599) is a potent, selective, and orally active chemical compound developed as a transient receptor potential ankyrin 1 (TRPA1) cation channel antagonist. It was originally designed by Roche Holding AG/Genentech to manage respiratory conditions, particularly chronic cough associated with asthma and Chronic Obstructive Pulmonary Disease (COPD).

Key Characteristics & Mechanism

Target Engagement: It acts as a TRPA1 inhibitor with high potency, exhibiting an IC50 value of 5.3 nM in humans. [1, 2]
Therapeutic Purpose: It blocks TRPA1 cation channels, which are thermoTRP channels known to function as sensor transducers for temperature, pain, and environmental irritants. Inhibiting this pathway prevents the sensory nerve hypersensitivity that triggers chronic coughing fits.
Research Status: As per data recorded by platforms like the IUPHAR/BPS Guide to PHARMACOLOGY, its chemical structure was publically disclosed in late 2023, and it has been evaluated through Phase 2 clinical trials
A Study To Evaluate The Efficacy, Safety, Pharmacokinetics, And Pharmacodynamic Effects Of GDC-6599 In Patients With Chronic Cough
CTID: NCT05660850
Phase: Phase 2
Status: Completed
Date: 2025-12-16

PAT

US10710994,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US251637879&_cid=P12-MRBG82-53830-1

Example 8: 1-((3-((3R,5R)-5-(4-chlorophenyl)tetrahydrofuran-3-yl)-1,2,4-oxadiazol-5-yl)methyl)-2,7-dimethyl-1H-purin-6(7H)-one

The overall Example 8 reaction scheme is as follows:

Step 4: Preparation of 1-((3-((3R,5R)-5-(4-chlorophenyl)tetrahydrofuran-3-yl)-1,2,4-oxadiazol-5-yl)methyl)-2,7-dimethyl-1H-purin-6(7H)-one

5-(chloromethyl)-3-[(3R,5R)-5-(4-chlorophenyl)tetrahydrofuran-3-yl]-1,2,4-oxadiazole (8.40 g, 28.1 mmol, prepared according to a similar procedure as example 1), 2,7-dimethyl-1H-purin-6(7H)-one (5.07 g, 30.9 mmol) and potassium carbonate (11.6 g, 84.2 mmol) were charged in a 200 mL RBF. DMF (56 mL) was added and the mixture was stirred in a 40° C. oil bath for 2 hours. Heat was removed and the reaction mixture was transferred to a separatory funnel containing EtOAc (100 mL) and water (500 mL). The mixture was extracted with EtOAc (3×100 mL). The combined organic layers were washed with a mixture of water (40 mL) and brine (40 mL), dried over anhydrous Na ₂SO ₄, filtered and concentrated under reduced pressure to give the crude product (77% purity by LCMS). The crude brown oil was dissolved in EtOAc (100 mL) and Heptane (60 mL) was added dropwise which led to the slow formation of a solid. The mixture was stirred at 0° C. for 30 min. and the solid was collected on a Büchner funnel, rinsed with heptane and air dried for 15 min. to give a first lot of 1-((3-((3R,5R)-5-(4-chlorophenyl)tetrahydrofuran-3-yl)-1,2,4-oxadiazol-5-yl)methyl)-2,7-dimethyl-1H-purin-6(7H)-one (8.0 g, 18.7 mmol, 67% yield, 92% purity by LCMS) as a yellow solid. The filtrate was concentrated and it was purified by reverse phase chromatography (C18, MeCN/10 mM NH ₄HCO ₂in H ₂O, pH 3.8, 0 to 60% gradient) to afford a second lot of 1-((3-((3R,5R)-5-(4-chlorophenyl)tetrahydrofuran-3-yl)-1,2,4-oxadiazol-5-yl)methyl)-2,7-dimethyl-1H-purin-6(7H)-one (950 mg, 2.23 mmol, 8% yield, >99% purity by LCMS) as a white solid.

The first lot of desired product (8.0 g, 92% purity by LCMS) was combined with a third lot obtained from a previous batch (1.3 g, 96% purity by LCMS). The material was dissolved in EtOAc (250 mL) and the solvent was displaced with iPrOH on the rotavap (3 cycles of iPrOH addition (50 mL)/evaporation of 50 mL of solvent). During the process, a solid crashed out and the solvent was reduced to ˜100 mL on the rotavap. The suspension was cooled to 0° C. and the solid was collected on a Büchner funnel, rinsed with cold iPrOH and air dried for 15 min. to give a fourth lot of 1-((3-((3R,5R)-5-(4-chlorophenyl)tetrahydrofuran-3-yl)-1,2,4-oxadiazol-5-yl)methyl)-2,7-dimethyl-1H-purin-6(7H)-one (8.50 g, 99% purity by LCMS) as a light beige solid. Still not satisfied with the color of the purified material, it was dissolved in EtOAc (500 mL) and the brown solution was treated with 8 g of activated charcoal. The mixture was allowed to stir for 15 min. The suspension was filtered on celite and the cake was rinsed with EtOAc. The colorless filtrate was evaporated under reduced pressure to give a fifth lot of 1-((3-((3R,5R)-5-(4-chlorophenyl)tetrahydrofuran-3-yl)-1,2,4-oxadiazol-5-yl)methyl)-2,7-dimethyl-1H-purin-6(7H)-one (7.50 g, 99% purity by LCMS) as a white solid. Finally, the second lot (950 mg, >99% purity by LCMS) and the fifth lot (7.50 g, 99% purity by LCMS) were combined in a 200 mL RBF and iPrOH (100 mL) was added. The suspension was stirred in a 100° C. oil bath until full dissolution and water was added (3 mL). The flask was removed from oil bath and the light yellow clear solution was allowed to cool down at room temperature. The suspension was cooled in an ice bath and the solid was collected on a Buchner funnel, rinsed with cold iPrOH (20 mL) and air dried for 24 hours to give the title compound 1-((3-((3R,5R)-5-(4-chlorophenyl)tetrahydrofuran-3-yl)-1,2,4-oxadiazol-5-yl)methyl)-2,7-dimethyl-1H-purin-6(7H)-one (7.3 g) as a white solid. LCMS: purity=99.4%, MH ⁺=427.2/429.2. ¹H NMR (400 MHz, DMSO-d6) δ 8.18 (s, 1H), 7.46-7.33 (m, 4H), 5.63 (s, 2H), 5.00 (t, J=7.4 Hz, 1H), 4.35 (dd, J=8.4, 7.5 Hz, 1H), 3.93 (s, 3H), 3.95-3.88 (m, 1H), 3.79-3.70 (m, 1H), 2.60 (s, 3H), 2.63-2.53 (m, 1H), 2.13 (ddd, J=12.7, 8.9, 7.8 Hz, 1H).

PAT

[WO2019182925A1]

EG 8

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References

Oxadiazole compounds as transient receptor potential channel inhibitors

Publication Number: EP-3768260-B1

Priority Date: 2018-03-19

Grant Date: 2025-10-08

Oxadiazole transient receptor potential channel inhibitorsPublication Number: TW-202003510-APriority Date: 2018-03-19
Oxadiazole transient receptor potential channel inhibitorsPublication Number: US-10710994-B2Priority Date: 2018-03-19Grant Date: 2020-07-14
Oxadiazole transient receptor potential channel inhibitorsPublication Number: TW-I829676-BPriority Date: 2018-03-19Grant Date: 2024-01-21
Oxadiazole transient receptor potential channel inhibitorsPublication Number: US-2025122184-A1Priority Date: 2018-03-19
Oxadiazole transient receptor potential channel inhibitorsPublication Number: EP-3768260-A1Priority Date: 2018-03-19
Oxadiazole transient receptor potential channel inhibitorsPublication Number: US-2019284179-A1Priority Date: 2018-03-19
Oxadiazole transient receptor potential channel inhibitorsPublication Number: KR-20230070333-APriority Date: 2018-03-19
Oxadiazole transient receptor potential channel inhibitorsPublication Number: US-12202824-B2Priority Date: 2018-03-19Grant Date: 2025-01-21
Oxadiazole transient receptor potential channel inhibitorPublication Number: KR-102533094-B1Priority Date: 2018-03-19Grant Date: 2023-05-16
Oxadiazole transient receptor potential channel inhibitorsPublication Number: TW-202438496-APriority Date: 2018-03-19
Oxadiazole transient receptor potential channel inhibitorsPublication Number: US-2020308161-A1Priority Date: 2018-03-19
Oxadiazole transient receptor potential channel inhibitorsPublication Number: US-2023121700-A1Priority Date: 2018-03-19
Oxadiazole transient receptor potential channel inhibitorsPublication Number: WO-2019182925-A1Priority Date: 2018-03-19
Oxadiazole transient receptor potential channel inhibitorsPublication Number: US-11655245-B2Priority Date: 2018-03-19Grant Date: 2023-05-23
Oxadiazole transient receptor potential channel inhibitorsPublication Number: CN-111867585-APriority Date: 2018-03-19

////////////nedizantrep, anax labs, transient receptor potential (TRP) ion channel antagonist, GDC-6599, GDC 6599, RG 6341, RG-6341, ENQ95FVE4X

Navlimetostat

DR ANTHONY MELVIN CRASTO Ph.D — Sun, 05 Jul 2026 02:44:22 +0000

Navlimetostat

CAS 2630904-45-7

ALSO 2630904-44-6

MF C23H18ClFN6O2 MW464.9 g/mol

(2M)-2-{4-[4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl] -1-methyl-1H-pyrazol-5-yl}-4-chloro-6-(cyclopropyloxy)-3-fluorobenzonitrile
antineoplastic, MRTX-1719, BMS-986504, MRTX 1719, BMS 986504

Navlimetostat (also known as MRTX-1719 or BMS-986504) is an investigational, first-in-class oral targeted cancer therapy being developed by Bristol-Myers Squibb. It works by selectively binding to the PRMT5-MTA complex, exploiting synthetic lethality to kill cancer cells with MTAP gene deletions while sparing healthy cells.

Navlimetostat is currently in Phase 1/2 clinical trials for advanced solid tumors, including MTAP-deficient non-small cell lung cancer (NSCLC), pancreatic cancer, and glioblastoma.

Key highlights and ongoing research:

Mechanism: In MTAP-deleted cancer cells, a metabolite called MTA accumulates and binds to PRMT5. Navlimetostat targets and inhibits this specific PRMT5-MTA complex, leading to tumor cell death.
Clinical Trials: It is currently being investigated as a monotherapy (e.g., in MTAP-deleted advanced solid tumors) and in combination with other agents like pumitamig

OriginatorMirati Therapeutics
DeveloperBristol-Myers Squibb; Mirati Therapeutics
ClassAntineoplastics; Small molecules
Mechanism of ActionPRMT5 protein inhibitors
Phase II/IIIAdenocarcinoma; Non-small cell lung cancer
Phase I/IIMesothelioma; Neurilemmoma; Pancreatic cancer; Solid tumours
22 May 2026University of Southampton in collaboration with Bristol-Myers Squibb plans a phase II SELECTmeso1 trial for Malignant mesothelioma (Second-line therapy or greater) in United Kingdom in May 2026 (PO, Tablet) (NCT07602946)
13 May 2026Northwestern University plans a phase Ib/II trial for Solid tumours (Metastatic disease, Second-line therapy or greater, Combination therapy) in USA(PO) in December 2027 (NCT07594626)
12 May 2026M.D. Anderson Cancer Center plans a phase I/II trial for Non-small cell lung cancer (Combination therapy, Late-stage disease, Metastatic disease, Second-line therapy or greater) in USA (PO), in November 2026 (NCT07579221)

PRMT5 Inhibitor BMS-986504 is an orally bioavailable methylthioadenosine (MTA)-selective inhibitor of the protein arginine methyltransferase 5 (PRMT5), with potential antineoplastic activity. Upon oral administration, PRMT5 inhibitor BMS-986504 targets, binds to and inhibits PRMT5 that is bound to MTA, a complex that is elevated in methylthioadenosine phosphorylase (MTAP)-deleted cancer cells, thereby specifically inhibiting the function of PRMT5 solely within MTAP-deleted cancer cells and not in normal, healthy cells. By inhibiting the methyltransferase activity of PRMT5, levels of both monomethylated and dimethylated arginine residues in histones H2A, H3 and H4 are decreased. This modulates the expression of genes involved in several cellular processes, including cellular proliferation. This may increase the expression of antiproliferative genes and/or decrease the expression of genes that promote cell proliferation, which may lead to decreased growth of rapidly proliferating cancer cells. BMS-986504 also causes dysregulated RNA splicing and decreased retinoblastoma protein (pRb). Together, this decreases proliferation and increases apoptosis specifically in MTAP-deleted cancer cells. PRMT5, a type II methyltransferase that catalyzes the formation of both omega-N monomethylarginine (MMA) and symmetric dimethylarginine (sDMA) on histones and a variety of other protein substrates involved in signal transduction and cellular transcription, is essential for the viability of cancer and normal cells. It is overexpressed in several neoplasms. Elevated levels are associated with decreased patient survival. MTAP is deleted in certain cancer cells leading to an accumulation of the metabolite MTA; MTA binds to and partially inhibits the activity of PRMT5.

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2021050915&_cid=P12-MR76CL-04796-1

[0186] Step 6: To a solution of 6-bromo-4-(chloromethyl)-2H-phthalazin-1-one 13c (148 g, crude) in DMF (1.5 L) was added (1,3-dioxoisoindolin-2-yl)potassium (121 g, 653 mmol). The reaction mixture was stirred at 90 °C for 2 hours and then cooled to 25 °C. The formed precipitate was filtered and washed with DMF (200 mL x 2) and the filter cake triturated with water (1.00 L), filtered and dried to give Intermediate F, 2-[(7-bromo-4-oxo-3H-phthalazin-1-yl)methyl]isoindoline-1,3-dione (162 g, 413 mmol, 76% yield) as a white solid.¹H NMR (400 MHz, DMSO-d₆) d = 12.59 (s, 1H), 8.43 (d, J = 1.2 Hz, 1H), 8.18 (d, J = 8.4 Hz, 1H), 8.07 (dd, J = 1.6, 8.4 Hz, 1H), 7.97 – 7.93 (m, 2H), 7.92 – 7.86 (m, 2H), 5.19 (s, 2H). LCMS [M+1]: 383.9.

[0327] Step 4: A mixture of 4-chloro-6-(cyclopropoxy)-3-fluoro-2-(2-methylpyrazol-3-yl)benzonitrile (180 mg, 0.617 mmol, 1.00 eq) and N-bromosuccinimide (220 mg, 1.23 mmol, 2.00 eq.) in acetonitrile (10 mL) was stirred at 40 °C for 2 hours under a nitrogen atmosphere. After such time the mixture was concentrated and the residue was purified by prep-TLC (SiO₂, petroleum ether: ethyl acetate 20%) to give 2-(4-bromo-2-methyl-pyrazol-3-yl)-4-chloro-6-(cyclopropoxy)-3-fluoro-benzonitrile (170 mg, 0.455 mmol, 74% yield) as a white solid. LCMS [M+1] ⁺ = 371.8; ¹H NMR (400 MHz, CDCl₃) d = 7.61 (s, 1H), 7.55 (d, J = 6.0 Hz, 1H), 3.93 – 3.85 (m, 1H), 3.80 (s, 4H), 0.97 – 0.94 (m, 4H).

EXAMPLE 16-7 and 16-8

[0590] Example 4-230, 2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1H-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile (30 mg, 0.065 mmol) separated by SFC (DAICEL CHIRALPAK IC (250 mm × 30 mm x 10 mm); mobile phase:

[0.1% NH₃H₂O isopropanol]; B%: 40% isocratic, 4.1 min cycle; 120 min total ) to give example 16-7 (ee > 99%, 13 mg, 0.026 mmol, 25% yield) as a yellow solid and example 16-8 (8 mg, ee = 84% ). Example 16-8 was then then further separated by SFC (DAICEL CHIRALPAK IC (250 mm × 30 mm,10 mm); mobile phase: [0.1% NH₃H₂O EtOH]; B%: 60% isocratic, 3.1 min cycle; total 50 min) to give Example 16-8 (ee > 99%, 4 mg, 0.007 mmol, 7% yield) as a yellow gum. Spectra data for Example 16-7: LCMS [M+1] ⁺ = 465.1; ¹H NMR (400 MHz, DMSO-d₆) d = 12.59 – 12.44 (s, 1H), 8.29 (s, 1H), 8.15 (d, J = 8.4 Hz, 1H), 8.01 (d, J = 6.0 Hz, 1H), 7.75 (s, 1H), 7.67 (br d, J = 7.6 Hz, 1H), 4.23 – 4.17 (m, 1H), 3.86 (br s, 2H), 3.78 (s, 3H), 0.94 – 0.88 (m, 2H), 0.84 – 0.79 (m, 2H). Spectra data for Example 16-8: LCMS [M+1] ⁺ = 465.1; ¹H NMR (400 MHz, DMSO-d₆) d = 12.49 – 12.37 (s, 1H), 8.26 (s, 1H), 8.15 (d, J = 8.4 Hz, 1H), 8.00 (d, J = 6.0 Hz, 1H), 7.73 (d, J = 1.6 Hz, 1H), 7.72 – 7.68 (m, 1H), 4.19 (m, 1H), 3.80 (s, 2H), 3.77 (s, 3H), 0.93 – 0.87 (m, 2H), 0.83 – 0.78 (m, 2H).

PAT

MTA-synergistic PRMT5 inhibitorsPublication Number: CN-114728912-APriority Date: 2019-09-12
Mta-cooperative prmt5 inhibitorsPublication Number: WO-2021050915-A1Priority Date: 2019-09-12
MTA-Cooperative PRMT5 InhibitorsPublication Number: US-2021078994-A1Priority Date: 2019-09-12
MTA-Cooperative PRMT5 InhibitorsPublication Number: US-2021079003-A1Priority Date: 2019-09-12

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References

Dynamic Kinetic Resolution of Axially Chiral MRTX1719Publication Name: SynfactsPublication Date: 2022-10-18DOI: 10.1055/s-0041-1738738
Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2H)-one derivatives as novel PRMT5/MTA inhibitorsPublication Name: Bioorganic & Medicinal ChemistryPublication Date: 2022-10-01PMID: 35926325DOI: 10.1016/j.bmc.2022.116947
Synthesis of MRTX1719Publication Name: SynfactsPublication Date: 2022-03-18DOI: 10.1055/s-0041-1737934
Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted CancersPublication Name: Journal of Medicinal ChemistryPublication Date: 2022-01-18PMID: 35041419DOI: 10.1021/acs.jmedchem.1c01900
Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to dependence on PRMT5Publication Name: Science (New York, N.Y.)Publication Date: 2016-03-11PMID: 26912361DOI: 10.1126/science.aad5944
Synthesis of MRTX1719DOI: 10.1055/s-0041-1737934Publication Date: 2022Publication Name: Synfacts
Dynamic Kinetic Resolution of Axially Chiral MRTX1719DOI: 10.1055/s-0041-1738738Publication Date: 2022Publication Name: Synfacts

////////navlimetostat, anax labs, antineoplastic, MRTX-1719, BMS-986504, MRTX 1719, BMS 986504

Moxetomidate

DR ANTHONY MELVIN CRASTO Ph.D — Sat, 04 Jul 2026 02:32:02 +0000

Moxetomidate

CAS 1567838-90-7

MF C15H18N2O3 MW 274.31 g/mol

2-methoxyethyl 3-[(1R)-1-phenylethyl]imidazole-4-carboxylate

2-methoxyethyl 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylate
GABAA receptor agonist, hypnotic, ET-26, ET 26, LPQ2K767W2

Moxetomidate (also known as methoxyetomidate or ET-26) is a novel, investigational short-acting intravenous anesthetic and sedative-hypnotic agent. It functions as a{GABA}_A} receptor agonist and is designed as a “soft drug” analogue of the traditional anesthetic etomidate.

The Purpose of Its Development

Traditional etomidate is highly valued in clinical settings for its exceptional cardiovascular stability, making it the agent of choice for inducing anesthesia in patients with low blood pressure, trauma, or severe heart conditions. However, its primary drawback is that it causes prolonged adrenocortical suppression by inhibiting the enzyme 11β-hydroxylase. This limits its safety for continuous infusions or repeated uses.

Moxetomidate was synthesized to overcome this exact limitation. It retains the favorable, heart-safe properties of etomidate while undergoing rapid metabolic breakdown into an inactive compound. This prevents prolonged suppression of the adrenal gland.

Key Scientific Properties

Mechanism of Action: It acts as a positive allosteric modulator and agonist at the \(GABA}_A}) receptor site, depressing the central nervous system to induce hypnosis and sedation.
Chemical Profile: Its chemical formula is C₁₅H₁₈N₂O₃ with a molecular weight of 274.31 g/mol. Its IUPAC name is 2-methoxyethyl (R)-1-(1-phenylethyl)-1H-imidazole-5-carboxylate.
Clinical Trial Status: Developed by entities including Jinzhou Ahon Pharmaceutical Co., Ltd., moxetomidate hydrochloride (ET-26 HCl) has progressed into Phase 3 clinical trials as an induction anesthetic.

Methoxyetomidate is an investigational anesthetic agent being developed by Jinzhou Ahon Pharmaceutical Co., Ltd. It is a short-acting intravenous anesthetic that acts as a positive allosteric modulator of GABAA receptors.^[1][2] As of 2024, methoxyetomidate is undergoing Phase 3 clinical trials for use in anesthesia.^[3][1]

PAT

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=D2B4BB918D25AFB75D4682C639A62719.wapp2nB?docId=US189917922&_cid=P21-MR5QSJ-95402-1

EG 1

Preparation of the Formula (I) Compound Guided by the Present Invention

The compound of Formula (II) (CAS: 56649-48-0) (216 mg, 1 mmol), the compound of Formula (III) (CAS: 6482-24-2) (278 mg, 2 mmol), and anhydrous potassium carbonate (564 mg, 3 mmol) were mixed and added in 15 mL of N,N-dimethylformamide, and the mixture was stirred at 50° C. and reacted overnight. Next day, the reaction solution was poured into 100 mL of cold water to obtain a clear solution, and was then extracted with ethyl acetate for three times (50 mL for each time). The combined organic layer was dried with anhydrous sodium sulfate and filtered to give the filtrate. Evaporation of the solvent under the reduced pressure provided oily crude products. After purification by silica gel column (eluent: cyclohexane/ethyl acetate=3/2), colorless oily product (150 mg) was obtained, with a yield of 54%.

1) NMR: apparatus: Bruker, internal standard substance: TMS

¹H-NMR (400 MHz CDCl ₃) δ: 1.862 (3H, d, J=7.2 Hz), 3.393 (3H, s), 3.645 (3H, t, J=4.8 Hz), 4.31˜4.405 (2H, m), 6.348 (1H, q, J=7.2 Hz), 7.17˜7.359 (m, 5H), 7.742 (s, 1H), 7.827 (s, 1H).

¹³C-NMR (100 MHz CDCl ₃) δ: 22.30, 55.48, 59.15, 63.53, 70.48, 122.39, 126.36, 128.08, 128.93, 138.63, 140.02, 141.20, 160.26.

2) MS: mass spectrometer: API3000 LC-Ms/Ms from American ABI company; ionization mode: ESI.

(M+H).HRMS: for C ₁₅H ₁₈N ₂O ₃+H, calcd 275.1396, found 275.1396.

3) Optical rotation value: The ethanol solution of the compound of Formula (I) was prepared at a concentration of 1 g/100 mL, and [α]D ²⁰value was measured using Polarimeter 341 polarimeter, with [α] _D ²⁰=+71.9°.

4) The ee value: The compound of Formula (I) was dissolved in methanol at a concentration of 1 mg/mL and then diluted 100 times before injection. The detection was performed by HPLC using chiral AD column, wavelength of UV detector: 254 nm, mobile phase: 20% isopropanol-n-hexane, flow rate: 1 mL/min. The optical purity of the compound of Formula (I) was determined to be 100% ( FIG. 1).

PAT

N-substituted imidazole carboxylic ester chiral compound containing an ether side chain, its preparation and applicationPublication Number: US-9969695-B2Priority Date: 2013-12-23Grant Date: 2018-05-15
N-substituted imidazole carboxylic ester chiral compound containing ether side chain, preparation method and applicationPublication Number: EP-3088394-A1Priority Date: 2013-12-23
N-Substituted Imidazole Carboxylic Ester Chiral Compound Containing an Ether Side Chain, Its Preparation and ApplicationPublication Number: US-2017001963-A1Priority Date: 2013-12-23
N-substituted imidazole carboxylic ester chiral compound containing ether side chain, preparation method and applicationPublication Number: WO-2015096551-A1Priority Date: 2013-12-23

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References

“ET-26 Methoxyetomidate Hydrochloride Development Information”. Synapse by Patsnap. Retrieved 2024-11-23.
Wang B, Chen S, Yang J, Yang L, Liu J, Zhang W (2017). “ET-26 hydrochloride (ET-26 HCl) has similar hemodynamic stability to that of etomidate in normal and uncontrolled hemorrhagic shock (UHS) rats”. PLOS ONE. 12 (8) e0183439. Bibcode:2017PLoSO..1283439W. doi:10.1371/journal.pone.0183439. PMC 5557577. PMID 28813523.
“ET-26 Clinical Trials Overview”. Synapse by Patsnap. Retrieved 2024-11-23.

Clinical data

Other names	ET-26; Moxetomidate
Identifiers
IUPAC name
CAS Number	1567838-90-7
PubChem CID	74766803
ChemSpider	133326476
UNII	LPQ2K767W2
Chemical and physical data
Formula	C₁₅H₁₈N₂O₃
Molar mass	274.320 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES
InChI

//////////moxetomidate, anax labs, GABAA receptor agonist, hypnotic, ET-26, ET 26, LPQ2K767W2

Mirivadelgat

DR ANTHONY MELVIN CRASTO Ph.D — Thu, 02 Jul 2026 02:46:52 +0000

Mirivadelgat

CAS 1804941-96-5

MF C30H34FN3O5 MW535.6 g/mol

L-Valine, [2-[4-(cyclopropylmethoxy)-3-[[[(3-fluoro-4-methoxyphenyl)methyl]amino]carbonyl]phenyl]-3-pyridinyl]methyl ester

[2-[4-(cyclopropylmethoxy)-3-[(3-fluoro-4-methoxyphenyl)methylcarbamoyl]phenyl]-3-pyridinyl]methyl (2S)-2-amino-3-methylbutanoate

L-Valine, [2-[4-(cyclopropylmethoxy)-3-[[[(3-fluoro-4-methoxyphenyl)methyl]amino]carbonyl]phenyl]-3-pyridinyl]methyl ester

{2-[4-(cyclopropylmethoxy)-3-{[(3-fluoro-4-methoxyphenyl)methyl]carbamoyl}phenyl]pyridin-3-yl}methyl
L-valinate
aldehyde dehydrogenase 2 activator, antianaemic, FP 045, 22TB7Q431D

Mirivadelgat (also known as FP-045) is a first-in-class, orally bioavailable small molecule that acts as a selective activator of mitochondrial aldehyde dehydrogenase 2 (ALDH2). Developed by Foresee Pharmaceuticals, this novel therapy helps cells clear toxic reactive aldehydes, reducing mitochondrial stress, cellular inflammation, and fibrosis. It is currently being evaluated in clinical trials for its disease-modifying potential across several serious conditions.

Current Clinical Development

The drug is undergoing clinical evaluation for multiple indications:

Pulmonary Hypertension with Interstitial Lung Disease (PH-ILD): Mirivadelgat is currently in a multinational, Phase 2 trial known as the WINDWARD Study. The double-blind trial is assessing whether the drug can safely improve pulmonary vascular resistance and overall lung and cardiac function.
Parkinson’s Disease: The drug was selected for the SLEIPNIR multi-drug Phase 2a platform trial funded by Cure Parkinson’s. It will evaluate mirivadelgat’s safety, brain penetration, and ability to clear the toxic waste products that drive Parkinson’s progression.
Fanconi’s Anaemia: It has also reached Phase I/II testing for this rare genetic condition.
Other Conditions: Early-stage Phase I research has explored its utility for metabolic and kidney disorders.

Mechanism of Action

When administered once daily, mirivadelgat targets deep cellular mechanics:

ALDH2 Activation: It binds selectively to the ALDH2 enzyme in the mitochondria.
Waste Clearance: It accelerates the metabolism of toxic reactive aldehydes produced by oxidative stress.
Mitochondrial Protection: Lowering toxic aldehyde levels protects cellular structures and shields tissues from fibrosis and dysfunction.

Mirivadelgat is an orally bioavailable selective activator of the mitochondrial isoform of aldehyde dehydrogenase (ALDH2), with potential protective activity. Upon oral administration, mirivadelgat increases ALDH2 activity. This increases the metabolism of toxic reactive aldehydes and lowers the level of the toxic aldehydes. This may protect cells from the toxic aldehydes and prevent mitochondria diseases and disorders. ALDH2, a mitochondrial regulator of toxic aldehyde metabolism, plays an important role in the metabolism of toxic aldehydes. Toxic aldehydes are produced by oxidative stress.

Study to Evaluate Safety and Efficacy of Mirivadelgat in PH-ILD

CTID: NCT06475781, Phase: Phase 2, Status: Recruiting, Date: 2025-10-06

OriginatorForesee Pharmaceuticals
ClassAntianaemics; Antihypertensives; Cardiovascular therapies; Hepatoprotectants; Small molecules
Mechanism of ActionAldehyde dehydrogenase 2 stimulants
Phase IIPulmonary hypertension
Phase I/IIFanconi’s anaemia
Phase IKidney disorders; Metabolic disorders
No development reportedCardiovascular disorders; Non-alcoholic fatty liver disease; Non-alcoholic steatohepatitis
08 Jun 2026Foresee Pharmaceuticals in collaboration with Haukeland University Hospital plans a phase IIa SLEIPNIR Platform trial for Parkinson’s disease (PO)
02 Jun 2026Helse Bergen HF, Cure Parkinson’s, Norwegian Parkinson’s Association plan the phase IIa SLEIPNIR-2 trial for Parkinson’s disease in Norway (PO, Capsule), in September 2026 , (CTIS2025-523570-17-00)
28 Oct 2025No recent reports of development identified for phase-I development in Cardiovascular-disorders in USA (PO)

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2015127137&_cid=P20-MR2WCE-70172-1

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References

Mitochondrial aldehyde dehydrogenase-2 binding compounds and methods of use thereofPublication Number: US-9879036-B2Priority Date: 2014-02-19Grant Date: 2018-01-30
Mitochondrial aldehyde dehydrogenase-2 binding compounds and methods of use thereofPublication Number: US-2017057982-A1Priority Date: 2014-02-19
Mitochondrial aldehyde dehydrogenase 2 (aldh2) binding polycyclic amides and their use for the treatment of cancerPublication Number: EP-3107899-B1Priority Date: 2014-02-19Grant Date: 2020-08-12

//////////mirivadelgat, anax labs, aldehyde dehydrogenase 2 activator, antianaemic, FP 045, 22TB7Q431D

Milpecitinib

DR ANTHONY MELVIN CRASTO Ph.D — Wed, 01 Jul 2026 02:43:44 +0000

Milpecitinib

CAS 1415819-54-3

MF C20H20N4O2S MW380.5 g/mol

N-[3-[4-[5-(pyrrolidine-1-carbonyl)-1H-pyrrol-3-yl]-1,3-thiazol-2-yl]phenyl]acetamide

N-(3-{4-[5-(pyrrolidine-1-carbonyl)-1H-pyrrol-3-yl]-1,3-thiazol-2-yl}phenyl)acetamide
Janus tyrosine kinase inhibitor, anti-inflammatory, veterinary, PF-06263276, PF 06263276, Ph 1012, DNX 04013, CPh 1012, Ph-1012, CVXL 0074-02, 4Q8TT4B4GN

Milpecitinib is a small molecule drug. Milpecitinib has a monoisotopic molecular weight of 380.13 Da.

Milpecitinib (also known by its developmental codes PF-06263276, Ph-1012, and DNX-04013) is a potent, small-molecule Janus kinase (JAK) inhibitor used primarily in veterinary medicine and laboratory research. It functions as an ATP-competitive, broad-spectrum (pan-JAK) inhibitor that targets all four members of the JAK family: JAK1, JAK2, JAK3, and Tyrosine Kinase 2 (TYK2).

Primary Indication and Target

Veterinary Use: Milpecitinib is designated for the control of pruritus (itching) associated with canine allergic dermatitis and the management of canine atopic dermatitis (CAD).
Sponsorship: The United States Adopted Name (USAN) for this drug was officially adopted following sponsorship by Phibro Animal Health.
Research Use: In laboratory settings, it is utilized to study complex inflammatory pathways, immune disorders, and certain cancers.

Mechanism of Action

Milpecitinib works by blocking the ATP-binding site of JAK enzymes. This inhibition halts the JAK-STAT signaling pathway, which plays a critical role in cellular responses to inflammatory cytokines. By blocking this cascade, the drug prevents the production and signaling of pro-inflammatory cytokines that cause severe itching and skin inflammation in dogs.

SYN

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=5D288DBBA230B78048641EFCD848FF01.wapp1nA?docId=US76372787&_cid=P10-MR1GR5-42689-1

A solution of acetyl chloride in DCM was added dropwise to a mixture of aniline and triethylamine in DCM under cooling on ice bath. Partial dissolution was observed followed by white precipitation. The solid was collected by filtration, washed with water and dried over vacuum yielding white powder (0.128 g 22%). HPLC—100% purity. LCMS—(ES ⁺) Calcd. 380.13. Found 381.1 (MH ⁺).

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References

Compositions and methods for modulating kinasesPublication Number: JP-6054379-B2Priority Date: 2011-06-07Grant Date: 2016-12-27
Compositions and methods for modulating a kinasePublication Number: EP-2718290-B1Priority Date: 2011-06-07Grant Date: 2016-05-04
Compositions and methods for modulating a kinasePublication Number: CA-2837268-CPriority Date: 2011-06-07Grant Date: 2020-05-12
Compositions and Methods for Modulating a KinasePublication Number: US-2012316148-A1Priority Date: 2011-06-07
Compositions and methods for modulating a kinasePublication Number: EP-2718290-A2Priority Date: 2011-06-07
Compositions and methods for modulating a kinasePublication Number: WO-2012172438-A9Priority Date: 2011-06-07
Compositions and methods for modulating a kinasePublication Number: US-8937065-B2Priority Date: 2011-06-07Grant Date: 2015-01-20
Compositions and methods for modulating kinasesPublication Number: JP-2014520108-APriority Date: 2011-06-07
Compositions and methods for modulating a kinasePublication Number: WO-2012172438-A2Priority Date: 2011-06-07
Compositions and methods to modulate a kinasePublication Number: ES-2585244-T3Priority Date: 2011-06-07Grant Date: 2016-10-04
Compound for modulating a kinase
Publication Number: BR-112013031121-B1
Priority Date: 2011-06-07

//////////milpecitinib, anax labs, Janus tyrosine kinase inhibitor, anti-inflammatory, veterinary, PF-06263276, PF 06263276, Ph 1012, DNX 04013, CPh 1012, Ph-1012, CVXL 0074-02, 4Q8TT4B4GN