Mazisotine

CAS 1638588-92-7

MF C16H23N3O2 MW 289.37 g/mol

(1S,5R)-N-[2-methyl-1-[(3-methyl-2-pyridinyl)oxy]propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide

rac-(1R,5S,6R)-N-{2-methyl-1-[(3-methylpyridin-2-yl)oxy]propan-2-yl}-3-azabicyclo[3.1.0]hexane-6-carboxamide

(1R,5S,6r)-N-{2-methyl-1-[(3-methylpyridin-2-yl)oxy]propan-2-yl}-3-azabicyclo[3.1.0]hexane-6-carboxamide
somatostatin receptor receptor agonist, LY3556050, CNTX-0290, LY 3556050, CNTX 0290, D3M32WP3MH

Mazisotine (also known as LY3556050 or CNTX-0290) is an experimental, non-opioid chemical compound designed to treat chronic and neuropathic pain. It functions as a selective somatostatin receptor 4 (SSTR4) agonist, meaning it activates specific peripheral nerve pathways to block pain signals without activating the central nervous system’s opioid receptors.

While it showed early promise in animal models, Eli Lilly and Company removed mazisotine from its clinical development pipeline after disappointing results in Phase II clinical trials. It currently remains in use strictly as a chemical tool for laboratory pain research.

Key Facts and Clinical History

• Mechanism of Action: It binds to and activates SSTR4. This triggers a cellular response that suppresses pain and inflammation in peripheral sensory neurons.
• Intended Indications: It was being evaluated to treat diabetic peripheral neuropathic pain, osteoarthritis pain, and chronic low back pain.
• Development Partners: The compound was originally licensed by Eli Lilly from Centrexion Therapeutics in 2019 for an upfront fee of $47.5 million.
• Discontinuation: In mid-2025, Eli Lilly officially dropped the drug. Phase II clinical trials revealed that its efficacy did not meet the high success thresholds required to continue human testing.
• Side Effects: In clinical studies, reported treatment-emergent adverse effects were generally mild to moderate. They included constipation, nausea, dizziness, fatigue, and headaches.

Mazisotine (LY3556050, CNTX-0290) is a chemical compound which acts as an agonist at somatostatin receptor 4. It has analgesic effects and has been researched for the treatment of pain associated with arthritis and neuropathic pain. It was not pursued for human medical use following disappointing results in Phase II clinical trials, but continues to be used in research into the role of SST4 receptors in pain perception.^[1][2]

• A Study of LY3556050 in Adult Participants With Diabetic Peripheral Neuropathic PainCTID: NCT06074562Phase: Phase 2Status: CompletedDate: 2025-07-03
• Chronic Pain Master Protocol (CPMP): A Study of LY3556050 in Participants With OsteoarthritisCTID: NCT04627038Phase: Phase 2Status: CompletedDate: 2023-11-02
• Chronic Pain Master Protocol (CPMP): A Study of LY3556050 in Participants With Diabetic Peripheral Neuropathic PainCTID: NCT04707157Phase: Phase 2Status: TerminatedDate: 2023-11-02
• Chronic Pain Master Protocol (CPMP): A Study of LY3556050 in Participants With Chronic Low Back PainCTID: NCT04874636Phase: Phase 2Status: CompletedDate: 2023-11-02
• A Study of Effect of LY3556050 on Metformin in Healthy ParticipantsCTID: NCT05615467Phase: Phase 1Status: CompletedDate: 2023-01-18
• A Study of Single and Repeated Doses of LY3556050 in Healthy ParticipantsCTID: NCT05341102Phase: Phase 1Status: CompletedDate: 2022-04-22
• A Study of LY3556050 in Healthy ParticipantsCTID: NCT04156750Phase: Phase 1Status: CompletedDate: 2020-08-19

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2025096300&_cid=P12-MQYLW5-94119-1

SYN

US10166214,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US214328185&_cid=P12-MQYLW3-94084-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=8B7A9DF85E102CA12206BC0A30612B65.wapp1nC?docId=WO2025193591&_cid=P12-MQYLNG-90472-1

reparation 1

[0081] Methyl (E)-4-((4-methylphenyl)sulfonamido)but-2-enoate

[0082] Methyl 4-bromobut-2-enoate (36.29g, 202.7mmol) was dissolved in MeCN (500 mL) at 15-25 ºC. tert-Butyl tosylcarbamate (50.00 g, 184.3 mmol) was added at 15-25 ºC. K₂CO₃ (30.57 g, 221.2mmol) and KI (3.06 g, 202.7 mmol) were added to the solution at 15-25 ºC, and warmed under nitrogen at 30 ºC for 20 hrs. The solution was cooled to 20 ºC and the mixture filtered. The filtered residue was washed with MeCN (100 mL) to give methyl (E)-4-((N-(tert-butoxycarbonyl)-4-methylphenyl)sulfonamido)but-2-enoate. TFA (101.03 g, 886.06 mmol) was added to the methyl (E)-4-((N-(tert-butoxycarbonyl)-4-methylphenyl)sulfonamido)but-2-enoate in MeCN solution (483.72 g, 143 mmol) and heated to 55-60 ºC for 16 hrs. The reaction solution was concentrated in vacuo to ~50 mL and solvent exchanged with toluene (2 x 250 mL). Toluene (500 mL) was added followed by EtOAc (50 mL) at 15-25 ^°C, and heated to 60 ºC for 1 hr., then cooled to 0 ºC for 12 hrs. The solution was filtered, and the wet cake was rinsed with n-heptane (50 mL). The cake was dried in vacuum at 50 ºC to give the title compound (37.85 g, 74.4%) as a white solid.¹H NMR (CDCl₃) δ 7.68 (d, J = 8.0Hz, 2H) 7.25 (d, J = 8.0Hz, 2H) 6.71 (dt, J = 15.6, 5.2Hz, 1H) 5.88 (dt, J = 15.6, 1.6Hz, 1H) 4.55 (t, J = 6.4Hz, 1H) 3.71 – 3.67 (m, 2H) 3.65 (s, 3H) 2.37 (s, 3H); HRMS (ESI⁺) Calculated for [C12H15NO4S+H] ⁺: 270.0795, Found: 270.0788 (M+H).

Preparation 2

[0083] (1R,5S,6r)-3-Tosyl-3-azabicyclo[3.1.0]hexane-6-carboxylic acid

0084] Methyl (E)-4-((4- 2-enoate (51.90 g) was dissolved in 2-MeTHF (600mL) at 0 ºC . Added (2-bromoethyl)diphenylsulfonium triflate (36.50 g), KF (6.47 g), KOH (18.75 g) to the solution at 0 ºC. Warmed the solution to 15 ºC for 22 hrs. then 30 ºC for 3 hrs. Added water (100 mL) and MeOH (100 mL) into the solution. Added LiOH^.H₂O (4.77 g) and stirred at 30 ºC for 16 hrs. Cooled to 15-25^oC and added n-heptane (100 mL). Stirred at 15-25^oC for 10 min. Separated and collected the aqueous phase and washed the aqueous phase with n-heptane/2-MeTHF (50 mL/200 mL × 2). Concentrated the aqueous phase in vacuo to ~50 mL and added 3M aq. HCl

dropwise to adjust pH to 1~2. Stirred the mixture at 20-30 ºC for 2 hrs. Filtered the solution and rinsed through with EtOH/H2O (15 mL1:4). Dried the wet cake at 45 ºC for 8-10 hrs. to give the title compound as white solid (20.37 g, 65%) ¹H NMR (CDCl₃) δ 7.67 (d, J = 8.2 Hz, 2 H) 7.34 (d, J = 8.2 Hz, 2 H) 3.63 (d, J = 9.4 Hz, 2 H) 3.12 (d, J = 9.4 Hz, 2 H) 2.46 – 2.40 (m, 4 H) 2.07 – 2.01 (m, 2 H); HRMS (ESI⁺) Calcd. for [C13H15NO4S+H] ⁺: 282.0795, Found: 282.0795 (M+H).

Preparation 3

[0085] 2-Methyl-1-((3-methylpyridin-2-yl)oxy)propan-2-amine

0086] 2-Amino-2-methylpropan- mmol) was dissolved in toluene (250 mL) at 15-25 ºC. Added potassium tert-butoxide (60.59 g, 534.6 mmol) to the solution and warmed to 30-40 ºC. Added 2-fluoro-3-methylpyridine (50.00 g, 450.0 mmol) to the solution and warmed to 80 ºC. Stirred the mixture for 18 hrs. at 80 ºC. Cooled the mixture to 15-25 ºC, added water (100 mL) and stirred for 30 min. Separated the aqueous layer and washed the organics with 10% aq. NaCl (300 mL x 3). Added toluene (250 mL) to the organics and concentrated in vacuo to give the title compound as a liquid (107.50 g, 98%). ¹H NMR (CDCl3) δ 7.92 – 7.82 (m, 1H) 7.32 – 7.22 (m, 1H) 6.74 – 6.66 (m, 1H) 3.97 (s, 3H) 2.14 (s, 3H) 1.15 (s, 6H).

Preparation 4

[0087] (1R,5S,6r)-N-(2-Methyl-1-((3-methylpyridin-2-yl)oxy)propan-2-yl)-3-tosyl-3-azabicyclo[3.1.0]hexane-6-carboxamide

[0088] Dissolved 
6-carboxylic acid (32.33 g, 88.2% purity) in toluene (320 mL) at 15~25 ºC. Added DMF (741.0 mg) and (COCl)₂ (19.20 g) to the solution and heated to 45-55 ºC for 3~4 hrs. Concentrated the mixture in vacuo and exchanged with THF (100 mL × 2). Added THF (320 mL) and cooled to 0-10 ºC. Added 2-methyl-1-((3-methylpyridin-2-yl)oxy)propan-2-amine (23.60 g), TEA (30.80 g), DMAP (620.0 mg) at 0-10 ºC then warmed to 15-25 ºC for 2~4 hrs.

Concentrated the mixture in vacuo and solvent exchanged with EtOH (140 mL × 2). Concentrated in vacuo to 140 mL and heated to 50 ºC until the solid was dissolved. Added water (210 mL) dropwise into the solution at 40 ºC. Cooled the solution to 10 ºC for 14 hrs. Filtered and rinsed with EtOH/H2O (75 mL, 1:1.5). Dried the wet cake at 45 ºC for 20 hrs. to give the title compound as a solid (41.87 g, 87.4%).¹H NMR (CDCl3) δ 7.94 – 7.87 (m, 1 H) 7.60 (d, J=8.0 Hz, 2 H) 7.37 (d, J=6.6 Hz, 1 H) 7.26 (d, J=8.0 Hz, 2 H) 6.78 (dd, J=6.6, 5.0 Hz, 1 H) 6.48 (s, 1 H) 4.25 (s, 2 H) 3.52 (d, J=9.4 Hz, 2 H) 2.95 (d, J=9.4 Hz, 2 H) 2.39 – 2.33 (m, 3 H) 2.17 (s, 3 H) 1.84 (s, 2 H) 1.39 (s, 6 H); HRMS (ESI⁺) Calcd. for [C₂₃H₂₉N₃O₄S+H] ⁺: 444.1952, Found: 444.2089 (M+H).

Preparation 5

[0089] (1R,5S,6r)-N-(2-Methyl-1-((3-methylpyridin-2-yl)oxy)propan-2-yl)-3-azabicyclo[3.1.0]hexane-6-carboxamide

[0090] Dissolved 2-yl)oxy)propan-2-yl)-3-tosyl-3-azabicyclo[3.1.0]hexane-6-carboxamide (5.00 g) in MTBE (50 mL) under nitrogen. Cooled to -70-60 ºC and added dropwise 1M Ph2PK in THF (56 mL, 56 mmol) into the solution. Stirred the mixture for 6-8 hrs. at -70-60 ºC. Added 2M aq. HCl (50 mL) to the solution allowing the temperature to rise to 15-25 ºC. Separated and collected the aqueous phase and washed with 2-MeTHF (50 mL × 3). Added 2-MeTHF (50 mL) and adjusted the pH to 8~9 with K2CO3 powder. Separated and extracted the aqueous phase with 2-MeTHF (50 mL). Combined the organics and concentrated in vacuo to give the title compound as a yellow-brown solid (3.05 g, 89.4%) ¹H NMR (CDCl₃) δ 8.01 – 7.92 (m, 1 H) 7.45 – 7.36 (m, 1 H) 6.81 (dd, J=7.0, 5.0 Hz, 1 H) 6.39 (s, 1 H) 4.31 (s, 2 H) 3.09 – 2.89 (m, 4 H) 2.21 (s, 3 H) 1.94 – 1.86 (m, 2 H) 1.69 (s, 1 H) 1.47 (s, 6 H) 1.12 (t, J=2.8 Hz, 1 H); HRMS (ESI⁺) Calcd. for [C16H23N3O2+H] ⁺: 290.1863, Found:

290.1917 (M+H).

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References

References

1.  Stevens R, Corradini L, Doods H (April 2019). “Preclinical Evaluation of Human Somatostatin Receptor 4 (hSSTR4) Agonist CNTX-0290 for Mixed Pain Conditions”. The Journal of Pain. 20 (4): S73. doi:10.1016/j.jpain.2019.02.092.
2.  Nguyen TH, Saito T, Chang W, Navarro A, Davies HM (March 2026). “Diastereoselective Cyclopropanation with Secondary Diazoacetamides to Access endo-Azabicyclo[3.1.0]hexane-6-carboxamides”. Organic Letters. 28 (9): 3063–3067. doi:10.1021/acs.orglett.6c00392. PMC 12973298. PMID 41729728.

Clinical data
Other names	LY3556050, CNTX-0290
Identifiers
IUPAC name
CAS Number	1638588-92-7
PubChem CID	86294067
ChemSpider	77005706
UNII	D3M32WP3MH
ChEMBL	ChEMBL5874446
Chemical and physical data
Formula	C16H23N3O2
Molar mass	289.379 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

PAT

• Novel methods for the preparation of 3-azabicylco[3.1,0]hexane-6-carboxamide derivativesPublication Number: WO-2025096300-A1Priority Date: 2023-10-30
• Methods for the preparation and dose regimens for use of sstr4 agonists and salts thereofPublication Number: WO-2024191686-A1Priority Date: 2023-03-10
• Methods for the preparation and dose regimens for use of sstr4 agonists and salts thereofPublication Number: US-2024307349-A1Priority Date: 2023-03-10
• Methods for preparation and dose regimens for use of sstr4 agonists and salts thereofPublication Number: JP-2024170613-APriority Date: 2023-03-10
• Methods for the preparation of SSTR4 agonists and their salts and dosage regimens for usePublication Number: JP-7569953-B2Priority Date: 2023-03-10Grant Date: 2024-10-18
• Sstr4 agonist saltsPublication Number: US-2024067628-A1Priority Date: 2021-09-14
• SSTR4 agonist saltsPublication Number: US-11834435-B2Priority Date: 2021-09-14Grant Date: 2023-12-05
• New somatostatin receptor subtype 4 (sstr4) agonistsPublication Number: EP-2997021-B1Priority Date: 2013-05-17Grant Date: 2017-12-20
• Somatostatin receptor subtype 4 (SSTR4) agonistsPublication Number: US-9371282-B2Priority Date: 2013-05-17Grant Date: 2016-06-21
• Somatostatin receptor subtype 4 (SSTR4) agonistsPublication Number: US-10166214-B2Priority Date: 2013-05-17Grant Date: 2019-01-01
• New somatostatin receptor subtype 4 (sstr4) agonistsPublication Number: US-2019269650-A1Priority Date: 2013-05-17
• New somatostatin receptor subtype 4 (sstr4) agonistsPublication Number: WO-2014184275-A1Priority Date: 2013-05-17
• Somatostatin receptor subtype 4 (SSTR4) agonistsPublication Number: US-10675268-B2Priority Date: 2013-05-17Grant Date: 2020-06-09
• New Somatostatin receptor subtype 4 (SSTR4) agonistsPublication Number: US-2014343065-A1Priority Date: 2013-05-17
• Somatostatin receptor subtype 4 (SSTR4) agonistsPublication Number: US-9789082-B2Priority Date: 2013-05-17Grant Date: 2017-10-17
• New somatostatin receptor subtype 4 (sstr4) agonistsPublication Number: US-2017014381-A1Priority Date: 2013-05-17
• Somatostatin receptor subtype 4 (sstr4) agonistsPublication Number: US-2018092880-A1Priority Date: 2013-05-17

////////mazisotine, ANAX LABS, somatostatin receptor receptor agonist, LY3556050, CNTX-0290, LY 3556050, CNTX 0290, D3M32WP3MH, PAIN, NEUROPATHIC PAIN

Lonitoclax

CAS 2952589-57-8

MF C43H45ClN4O5 MW733.3 g/mol

5-[5-chloro-2-[(3S)-3-(morpholin-4-ylmethyl)-3,4-dihydro-1H-isoquinoline-2-carbonyl]phenyl]-N-(4-hydroxyphenyl)-N-[(3-methoxy-2-methylphenyl)methyl]-1,2-dimethylpyrrole-3-carboxamide

• 1H-Pyrrole-3-carboxamide, 5-[5-chloro-2-[[(3S)-3,4-dihydro-3-(4-morpholinylmethyl)-2(1H)-isoquinolinyl]carbonyl]phenyl]-N-(4-hydroxyphenyl)-N-[(3-methoxy-2-methylphenyl)methyl]-1,2-dimethyl-
• 5-(5-Chloro-2-(((3S)-3-(morpholin-4-ylmethyl)-3,4-dihydroisoquinolin-2-(1-H)-yl)carbonyl)phenyl)-N-4-hydroxyphenyl)-N-(3-methoxy-2-methylbenzyl)-1,2-dimethyl-1H-pyrrole-3-carboxamide
• 5-[5-chloro-2-[(3S)-3-(morpholinomethyl)- 3,4-dihydro-1H-isoquinoline-2- carbonyl]phenyl]-N-(4-hydroxyphenyl)-N- [(3-methoxy-2-methyl-phenyl)methyl]-1,2- dimethyl-pyrrole-3-carboxamide
• 5-{5-Chloro-2-[(3S)-3-[(morpholin-4-yl)methyl]-3,4-dihydroisoquinoline-2(1H)-carbonyl]phenyl}-N-(4-hydroxyphenyl)-N-[(3-methoxy-2-methylphenyl)methyl]-1,2-dimethyl-1H-pyrrole-3-carboxamide

5-(5-chloro-2-{(3S)-3-[(morpholin-4-yl)methyl]-3,4-dihydroisoquinoline-2(1H)-carbonyl}phenyl)-N-(4-
hydroxyphenyl)-N-[(3-methoxy-2-methylphenyl)methyl]-1,2-dimethyl-1H-pyrrole-3-carboxamide
B-cell lymphoma 2 (Bcl-2) inhibitor, antineoplastic, ZE50-0134, ZE50 0134, Lomond Therapeutics, CANCER, 76NBC3X6A3

Lonitoclax (also known as ZE50-0134) is an investigational, next-generation, orally administered B-cell lymphoma 2 (Bcl-2) inhibitor being developed for the treatment of hematologic malignancies like Acute Myeloid Leukemia (AML) and Chronic Lymphocytic Leukemia (CLL). Developed by Lomond Therapeutics, the drug is engineered as a highly selective option to improve upon existing first-generation Bcl-2 inhibitors like venetoclax.

Mechanism and Advantages Over Venetoclax

Unlike earlier therapies, lonitoclax features a unique binding mode and a structurally distinct chemotype. Its design yields several pharmacology advantages:

• Higher Selectivity: It binds tightly to Bcl-2 while demonstrating exceptional selectivity over Bcl-xL, which helps lower hematologic toxicities.
• Limited Immune Suppression: In preclinical data, lonitoclax spared healthy non-malignant immune cells (B cells, CD8 T cells, and NK cells), a major shift from the immunosuppressive profile of venetoclax.
• Reduced Drug Interaction & Accumulation: It features a shorter half-life (~9–10 hours) and minimal CYP3A4 (P4503A4) inhibition. This prevents the drug from building up dangerously and mitigates the risk of Tumor Lysis Syndrome (TLS), potentially enabling safer outpatient treatments.

Clinical Development Status

Lonitoclax is currently advancing through early-phase clinical trials:

• IND Clearances: The U.S. FDA cleared Investigational New Drug (IND) applications evaluating lonitoclax for CLL/SLL and as a combination treatment for relapsed or refractory AML.
• Healthy Volunteer Studies: Phase 1 single ascending dose (SAD) studies in healthy adults confirmed that the drug is well tolerated with linear pharmacokinetics and no significant safety issues. Target engagement was confirmed through plasma apoptosis assays.
• Combination Trials: Active Phase 1b multicenter trials are underway evaluating the safety, efficacy, and synergy of lonitoclax when combined with hypomethylating agents like azacitidine in AML patients.

SYN

US20250115577, Compound 7

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2023129553&_cid=P11-MQVQMH-93381-1

ADVERISEMENT

ANAX LABORATORIES

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Development Solutions, Developing from Lab scale to PR&D, Kilo Scale-ups and Commercial Scales

SEE MORE………Integrated Solutions, Manufacturing Solutions, Products,
Can’t Find? Let’s Connect

Phone : +91 897704 2010 /  +91 9177075735, Email : info@anaxlab.com

#MedicinalChemistry, #DrugDiscovery, #OrganicSynthesis, #ChemicalLibrary, #BuildingBlocks, #SARStudies, #ChemistryInnovation, #medchem, #Drugdevelopment, #Biotech, #Biotechnology, #AnaxLaboratories, #Pharma

AS ON FEB2026 4.574 LAKHS VIEWS ON BLOG WORLDREACH AVAILABLEFOR YOUR ADVERTISEMENT

join me on Linkedin

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join me on twitter

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References

• Bcl-2 inhibitorsPublication Number: WO-2023129553-A1Priority Date: 2021-12-29
• BCL-2 InhibitorsPublication Number: US-2025115577-A1Priority Date: 2021-12-29
• Bcl-2 inhibitorsPublication Number: EP-4457223-A1Priority Date: 2021-12-29

///////Lonitoclax, ANAX LABS, B-cell lymphoma 2 (Bcl-2) inhibitor, antineoplastic, ZE50-0134, ZE50 0134, Lomond Therapeutics, CANCER, 76NBC3X6A3

Lomonitinib

CAS 2923221-56-9

MF C27H24N4O2 MW436.5 g/mol

3-(3,4-dimethoxyphenyl)-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrazolo[4,5-c]quinoline

• 3-(3,4-dimethoxyphenyl)-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)pyrazolo[4,3-c]quinoline
• 1H-Pyrazolo[4,3-c]quinoline, 3-(3,4-dimethoxyphenyl)-1-(1,2,3,4-tetrahydro-7-isoquinolinyl)-
• 3-(3,4-dimethoxyphenyl)-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)-1H-pyrazolo[4,3-c]quinoline
• 7-[3-(3,4-dimethoxyphenyl)-1H- pyrazolo[4,3-c]quinolin-1-yl]-1,2,3,4- tetrahydroisoquinoline
• 7-[3-(3,4-Dimethoxyphenyl)-1H-pyrazolo[4,3-c]quinolin-1-yl]-1,2,3,4-tetrahydroisoquinoline

3-(3,4-dimethoxyphenyl)-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)-1H-pyrazolo[4,3-c]quinoline
tyrosine kinase inhibitor, antineoplastic, ZE46-0134, Eilean Therapeutics, U4DPU7W7QU

Lomonitinib (also known as ZE46-0134) is a highly potent, selective, orally bioavailable pan-FLT3 and IRAK4 small molecule inhibitor being developed for the treatment of Acute Myeloid Leukemia (AML). Developed by Eilean Therapeutics in collaboration with Expert Systems, it uniquely targets both primary mutations and the major drug-resistance pathways that cause other AML therapies to fail.

Mechanism of Action

Lomonitinib utilizes a dual-targeting framework to bypass conventional drug resistance:

• Pan-FLT3 Inhibition: It binds to and blocks FMS-like tyrosine kinase 3 (FLT3) mutations. This includes the challenging FLT3-ITD-F691L “gatekeeper” mutation, which typically confers resistance to all currently approved standard FLT3 inhibitors like gilteritinib.
• IRAK4 Inhibition: It simultaneously targets interleukin-1 receptor-associated kinase 4 (IRAK4). IRAK4 activation acts as a key “escape pathway” that cancer cells use to survive and build adaptive resistance to standalone FLT3 therapy.

Key Clinical Advantages

According to preclinical models and clinical data presented at the American Society of Hematology (ASH), lomonitinib offers unique benefits:

• Superior Efficacy: In vivo models demonstrate stronger anti-tumor activity and deeper responses in gatekeeper mutation-dependent disease compared to gilteritinib.
• Favorable Loading Strategy: Because of its wide therapeutic index and low toxicity, clinicians can administer a high loading dose on Day 1 followed by a smaller maintenance dose. This achieves effective therapeutic drug levels by Day 4, a rapid target engagement not possible with older long-half-life FLT3 inhibitors.
• Low Drug Interactions: Clinical profiles show minimal pharmacokinetic interference from proton pump inhibitors (PPIs) or CYP3A4 inhibitors like itraconazole.

Development Status

Lomonitinib is currently classified as an investigational new drug:

1. Clinical Trials: It is undergoing open-label, dose-escalation Phase 1/1b trials in both Australia and the United States (such as trial NCT06366789) evaluating adults with FLT3-mutated relapsed or refractory AML.
2. Partnerships: The drug is being studied in the US in collaboration with The Leukemia & Lymphoma Society as part of their Beat AML master clinical trial portfolio

Lomonitinib is an orally bioavailable inhibitor of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2) mutations and interleukin-1 receptor-associated kinase 4 (IRAK4), with potential antineoplastic activity. Upon oral administration, lomonitinib targets, binds to and inhibits the activity of FLT3 mutations, including the FLT3-ITD-F691L gatekeeper mutation, while sparing the wild-type form of FLT3. This inhibits the proliferation of FLT3 mutant-expressing cancer cells. In addition, lomonitinib targets, binds to, and inhibits the kinase activity of IRAK4. This inhibits IRAK4-mediated signaling and may reduce adaptive resistance to FLT3 inhibition as toll-like receptor (TLR) activation plays an important role in resistance to FLT3 inhibition. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B-lineage neoplasms and in acute myeloid leukemias. IRAK4, a serine/threonine-protein kinase, plays a key role in both the TLR and IL-1R signaling pathways.

• Dose Escalation and Expansion Study to Evaluate the Safety, PK, PD and Efficacy of ZE46-0134 in Adults With FLT3 Mutated or Spliceosome Mutated Relapsed or Refractory Acute Myeloid LeukemiaCTID: NCT06366789Phase: Phase 1Status: RecruitingDate: 2025-12-31
• Study of Biomarker-Based Treatment of Acute Myeloid LeukemiaCTID: NCT03013998Phase: Phase 1/Phase 2Status: RecruitingDate: 2025-12-17
• Study of Single and Multiple Ascending Doses of ZE46-0134 in Healthy VolunteersCTID: NCT06399315Phase: Phase 1Status: CompletedDate: 2025-12-09

SYN

US20250011319, Compound 1.31

PAT

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=A1EAFE0DBAFF71D8E655E689964CEA0E.wapp1nC?docId=WO2026080917&_cid=P12-MQUBN3-08111-1

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=US445571045&_cid=P12-MQUBPX-10324-1

Example 34: 3-(3,4-dimethoxyphenyl)-1-(1,2,3,4-tetrahydroisoquinolin-7-yl)-1H-pyrazolo[4,3-c]quinoline dihydrochloride (1.31)

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References

• Substituted 1H-pyrazolo [4,3-c ] quinolines, methods of preparation and uses thereofPublication Number: CN-118076605-APriority Date: 2021-10-15
• SUBSTITUTED 1H-PYRAZOLO [4,3-c] QUINOLINES, METHODS OF PREPARATION, AND USE THEREOFPublication Number: US-2025011319-A1Priority Date: 2021-10-15

////////lomonitinib, anax labs, tyrosine kinase inhibitor, antineoplastic, ZE46-0134, Eilean Therapeutics, U4DPU7W7QU

Lixosicone

CAS 1610878-71-1

MF C29H40O3 MW 436.6 g/mol

1-[(3S,8S,9S,10R,13S,14S,17S)-3-[(4-methoxyphenyl)methoxy]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]ethanone

• 3beta-[(4-methoxyphenyl)methoxy]pregn-5-en-20-one
• (3beta)-3-[(4-Methoxyphenyl)methoxy]pregn-5-en-20-one
• Pregn-5-en-20-one, 3-[(4-methoxyphenyl)methoxy]-, (3beta)-
• 1-[(3S,8S,9S,10R,13S,14S,17S)-3-[(4-methoxyphenyl)methoxy]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]ethanone
• 3?-(4-Methoxybenzyloxy)pregn-5-en-20-one; 1-((3S,8S,9S,10R,13S,14S,17S)-3-((4-Methoxybenzyl)oxy)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)ethan-1-one

3β-[(4-methoxyphenyl)methoxy]pregn-5-en-20-one
cannabinoid CB1 receptor signalling inhibitor, AEF0117, AEF 0117, 9LG9CT78SV

AEF0117 is a small molecule drug. AEF0117 is under investigation in clinical trial NCT05554926 (Study of [4-14C] AEF0117 Following a Single Oral Dose in Healthy Male Subjects).

Lixosicone (AEF0117, 3β-(4-methoxybenzyloxy)pregn-5-en-20-one) is a compound derived from pregnenolone by Aelis Farma, which acts as a biased negative allosteric modulator of the cannabinoid CB₁ receptor, representing a new class of compounds referred to as CB₁-selective signalling-specific inhibitors (CB₁-SSi). It binds to an allosteric site on the CB₁ receptor and modifies the downstream signalling produced as a result of CB₁ activation, preventing CB₁ mediated changes to mitogen-activated protein kinase (MAPK) phosphorylation but without affecting the signalling mediated by cyclic AMP. Unlike pregnenolone, AEF0117 is specific for the CB₁-SSi activity and lacks the neurosteroid action typical of many structurally related compounds.^[1]

In Phase II human clinical trials in patients diagnosed with cannabis use disorder, AEF0117 was found to partly but not completely block the effects of THC, and reduced cannabis self-administration but without producing an acute withdrawal syndrome and with relatively mild side effects. It is hoped that compounds of this type may be useful either as medications for the treatment of cannabinoid dependence, or could be used alongside medicinal cannabis to reduce unwanted side effects while retaining therapeutic efficacy.^[2]

As of March 2026, lixosicone is in phase 2 clinical trials for treatment of substance-related disorders.^[3] It is being developed by Aelis Farma.^[3]

Clinical Development

The compound has shown promising results in clinical settings:

• Phase 2a results: In clinical trials evaluated by the National Institute on Drug Abuse, lixosicone significantly reduced the positive subjective effects (“the high”) of cannabis by 19% at lower doses and up to 38% at higher doses compared to a placebo.
• Reduced consumption: Testing demonstrated that the drug successfully reduced cannabis self-administration.
• Safety profile: Across early-stage evaluations, the drug was found to be safe, well-tolerated, and did not precipitate adverse behavioral withdrawal symptoms

SYN

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=98A554C6AEFBBFD20722462022415D6C.wapp1nA?docId=US402829323&_cid=P10-MQRGET-66134-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=CN309682512&_cid=P10-MQRGHV-67541-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2019162328&_cid=P10-MQRGHV-67541-1

PAT

• 3β-(4-Methoxybenzyloxy)pregnant-5-en-20-one for the treatment of cannabinoid-related disordersPublication Number: CN-111757740-BPriority Date: 2018-02-20Grant Date: 2023-12-15
• 3beta-(4-methoxybenzyloxy)paragan-5-en-20-one for use in the treatment of cannabinoid-related disordersPublication Number: IL-276697-B2Priority Date: 2018-02-20
• 3-BETA-(4-METHOXYBENZYLOXY)PREGN-5-EN-20-ONE FOR USE IN THE TREATMENT OF CANNABINOID-RELATED DISORDERSPublication Number: PT-3755339-TPriority Date: 2018-02-20
• 3beta-(4-methoxybenzyloxy)pregn-5-en-20-one for use in the treatment of Cannabinoids-Related DisordersPublication Number: US-2023226076-A1Priority Date: 2018-02-20
• 3beta-(4-methoxybenzyloxy)pregn-5-en-20-one for use in the treatment of cannabinoids-related disordersPublication Number: EP-3755339-A1Priority Date: 2018-02-20
• 3beta-(4-methoxybenzyloxy)pregn-5-en-20-one for use in the treatment of Cannabinoids-Related DisordersPublication Number: US-2021030768-A1Priority Date: 2018-02-20
• 3-beta-(4-methoxybenzyloxy)pregn-5-en-20-one for use in the treatment of cannabinoids-related disordersPublication Number: EP-3755339-B1Priority Date: 2018-02-20Grant Date: 2024-01-03
• 3BETA-(4-METHOXYBENZYLOXY)PREGN-5-EN-20-ONE FOR USE IN THE TREATMENT OF CANNABINOIDS RELATED DISORDERSPublication Number: MA-51891-B1Priority Date: 2018-02-20
• 3Beta-(4-Methoxybenzyloxy)pregn-5-en-20-one for use in the treatment of cannabinoid-related disordersPublication Number: MD-3755339-T2Priority Date: 2018-02-20
• 3-BETA-(4-METHOXYBENZYLLOXY)PREGN-5-EN-20-ONE FOR USE IN THE TREATMENT OF CANNABINOID-RELATED DISORDERSPublication Number: HR-P20240276-T1Priority Date: 2018-02-20
• 3beta-(4-methoxybenzyloxy)pregn-5-en-20-one for use in the treatment of cannabinoids-related disordersPublication Number: WO-2019162328-A1Priority Date: 2018-02-20
• 3BETA-(4-METHOXYBENCYLOXY)PREGN-5-EN-20-ONE FOR USE IN THE TREATMENT OF CANNABINOID-RELATED DISORDERS.Publication Number: MX-2020008687-APriority Date: 2018-02-20
• 3β-(4-methoxybenzyloxy)pregn-5-en-20-one for use in the treatment of cannabinoids-related disordersPublication Number: US-11484537-B2Priority Date: 2018-02-20Grant Date: 2022-11-01
• 3beta-(4-methoxybenzyloxy)pregn-5-en-20-one for use in the treatment of cannabinoids-related disordersPublication Number: AU-2019223049-A1Priority Date: 2018-02-20
• 3beta-(4-methoxybenzyloxy)pregn-5-en-20-one for use in the treatment of cannabinoids-related disordersPublication Number: CA-3090975-A1Priority Date: 2018-02-20

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References

 “AEF 0117”. AdisInsight. 13 March 2026. Retrieved 17 April 2026.

 US 11484537, Piazza PV, Fabre S, Metna M, Monlezun S, Busquet-Garcia A, Cota D, Marsicano G, Revest JM, Vallée M, “3β-(4-methoxybenzyloxy)pregn-5-en-20-one for use in the treatment of cannabinoids-related disorders.”, issued 1 November 2022, assigned to Universite de Bordeaux.

 Haney M, Vallée M, Fabre S, Collins Reed S, Zanese M, Campistron G, et al. (June 2023). “Signaling-specific inhibition of the CB₁ receptor for cannabis use disorder: phase 1 and phase 2a randomized trials”. Nature Medicine. 29 (6): 1487–1499. doi:10.1038/s41591-023-02381-w. PMC 10287566. PMID 37291212.

Clinical data
Other names	AEF0117; AEF-0117; 3β-(4-Methoxybenzyloxy)pregn-5-en-20-one
Drug class	Cannabinoid CB1 receptor negative allosteric modulator
Identifiers
IUPAC name
CAS Number	1610878-71-1
PubChem CID	139433957
ChemSpider	129421614
Chemical and physical data
Formula	C29H40O3
Molar mass	436.636 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

//////////lixosicone, anax labs, cannabinoid CB1 receptor signalling inhibitor, AEF0117, AEF 0117, 9LG9CT78SV

Lirucitinib

CAS 2458115-78-9

MF C16H25N5OS MW335.5 g/mol

N-[4-[(ethylsulfonimidoyl)methyl]cyclohexyl]-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine

(R)-ethyl(imino)({trans-4-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexyl}methyl)-λ6
-sulfanone
Janus tyrosine kinase inhibitor, anti-inflammatory, GGW101, GGW 101

Lirucitinib is a Janus kinase (JAK) inhibitor primarily known as a novel, Class I veterinary drug. It specifically targets the JAK1 enzyme to block itch-inducing (pruritic) and inflammation-causing cytokines in the body.

Core Information

• Primary Use: The drug is developed for veterinary medicine to treat acute and chronic pruritic (severe itch) skin diseases in dogs, which are commonly caused by allergies, parasites, or infections.
• Approval Status: It received a Class I New Veterinary Drug Certificate from the Ministry of Agriculture and Rural Affairs (MARA) in China.
• Human Medicine: As of 2026, there are no clinical indications or indications that Lirucitinib is being tested for use in humans.
• Chemical Profile: It is an orally active small molecule with the chemical formula C₁₆H₂₅N₅OS and acts specifically as the (R)-enantiomer of the compound.

SYN

[US20220106319A1]

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=4CA57DF508E7B72B516CEB2A97283182.wapp2nC?docId=US356967355&_cid=P22-MQQ0KW-29134-1

  11 (1.0 g, 2.04 mmol) (prepared in step 9), tetrahydrofuran/methanol (10 mL), and cesium carbonate (1.33 g, 4.08 mmol) were added into a 25 mL single-necked flask, refluxed for 12 h, concentrated, and poured into dichloromethane and saturated salt solution, the organic phase was dried with anhydrous sodium sulfate, concentrated, and subjected to a conventional preparation method and a chiral preparation method to obtain product A as a white solid (20 mg, yield: 2.9%), LC-MS: 336 [M+H]+, H ¹-NMR: ¹H NMR (400 MHz, DMSO) δ 11.61 (s, 1H), 8.09 (s, 1H), 7.13 (s, 1H), 6.54 (s, 1H), 4.67 (s, 1H), 3.90-3.83 (m, 1H), 3.17 (s, 3H), 3.06-2.93 (m, 4H), 2.12-2.01 (m, 3H), 1.73-1.70 (m, 4H), 1.31-1.22 (m, 5H) and product B as a white solid (25 mg, yield: 3.7%), LC-MS: 336 [M+H]+, H ¹—NMR: ¹H NMR (400 MHz, DMSO) δ 11.59 (s, 1H), 8.09 (s, 1H), 7.12 (dd, J=3.3, 2.6 Hz, 1H), 6.54 (s, 1H), 4.67 (s, 1H), 3.58 (s, 1H), 3.17 (s, 3H), 3.06-2.89 (m, 4H), 2.16-1.93 (m, 3H), 1.74-1.69 (m, 4H), 1.25-1.23 (m, 5H).

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PAT

• Jak inhibitor and preparation method thereforPublication Number: EP-3915989-B1Priority Date: 2019-01-30Grant Date: 2023-06-28
• Jak inhibitor and preparation method thereforPublication Number: US-2022106319-A1Priority Date: 2019-01-30
• Jak inhibitor and preparation method thereforPublication Number: WO-2020155931-A1Priority Date: 2019-01-30
• Jak inhibitor and preparation method thereforPublication Number: EP-3915989-A1Priority Date: 2019-01-30

/////////lirucitinib, anax labs, Janus tyrosine kinase inhibitor, anti-inflammatory, GGW101, GGW 101

Linvemastat

CAS 2389060-50-6

MF C20H17N3O4S MW395.43

5-[3-[4-[(2-methyl-4-pyridinyl)methoxy]phenyl]sulfanylfuran-2-yl]imidazolidine-2,4-dione

• 2,4-Imidazolidinedione, 5-[3-[[4-[(2-methyl-4-pyridinyl)methoxy]phenyl]thio]-2-furanyl]-
• 5-[3-[[4-[(2-Methyl-4-pyridinyl)methoxy]phenyl]thio]-2-furanyl]-2,4-imidazolidinedione
• rac-(14R)-72-methyl-5-oxa-3-thia-7(4)-pyridina-1(4)-imidazolidina-2(2,3)-furana-4(1,4)-benzenaheptaphane-12,15-dione

matrix metalloproteinase-12 inhibitor, lung diseases, FP 020, FP2AMM4SVF

Linvemastat (also known by its developmental code FP-020) is an investigational, orally active small-molecule drug designed to selectively inhibit matrix metalloproteinase-12 (MMP-12). It is being developed as a potential disease-modifying therapy for chronic inflammatory and fibrotic diseases, primarily targeting respiratory conditions and gastrointestinal disorders.

How Linvemastat Works

• Targeting MMP-12: MMP-12 is an enzyme secreted by macrophages that breaks down extracellular matrix proteins like elastin.
• Controlling Damage: Overexpression of MMP-12 is strongly linked to tissue destruction, chronic inflammation, and fibrosis in the lungs and gut.
• High Selectivity: Unlike older matrix metalloproteinase inhibitors, linvemastat targets MMP-12 with high specificity, avoiding off-target interactions with other vital MMP enzymes.

Primary Therapeutic Indications under Research

• Severe, Uncontrolled Asthma: Evaluated to reduce airway inflammation and improve overall lung function.
• Chronic Obstructive Pulmonary Disease (COPD): Investigated for preventing structural lung damage and progressive emphysema.
• Inflammatory Bowel Disease (IBD): Researched to minimize continuous gut wall inflammation and intestinal fibrosis.
• Other Fibrotic Conditions: Explored in preclinical models for conditions like idiopathic pulmonary fibrosis (IPF) and kidney damage.

Current Clinical Status

Initially developed by Foresee Pharmaceuticals, global development rights for the program were transitioned to Primevera Therapeutics LLC.

• Phase 1 Trial: Completed trials in healthy volunteers demonstrated a favorable safety and pharmacokinetic profile, with only minor, recoverable side effects like mild nausea or headache.
• Phase 2 Trial: Undergoing mid-stage clinical evaluation, such as the global, randomized syMMPonia study. This trial is measuring changes in forced expiratory volume (FEV₁) to assess the drug’s impact on adults with partially controlled, moderate-to-severe asthma.

Effect of Linvemastat in Patients With Partially Controlled Asthma (syMMPonia)

CTID: NCT07191535

Phase: Phase 2

Status: Not yet recruiting

Date: 2025-10-20

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2019222157&_cid=P10-MQOLFP-71317-1

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=US276884719&_cid=P10-MQOLBE-66887-1

SYN

US10851089, Compound FC-4

PAT

• US10851089, Compound FC-30
• US10851089, Compound FC-31

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PAT

[1]. YANG, W J, et al. Matrix metalloproteinase (mmp) inhibitors and methods of use thereof. WO2019222157A1. 2019-11-21.

• Matrix metalloproteinase (MMP) inhibitors and methods of use thereofPublication Number: US-10851089-B2Priority Date: 2018-05-15Grant Date: 2020-12-01
• Matrix metalloproteinase (mmp) inhibitors and methods of use thereofPublication Number: US-2019352287-A1Priority Date: 2018-05-15

//////////////linvemastat, anax labs, matrix metalloproteinase-12 inhibitor, lung diseases, FP 020, FP2AMM4SVF

Gadoquatrane

CAS2048221-65-2MW2579.0 g/mol

FDA 2026, APPROVALS 2026, Ambelvist, OZG7J613HK, BAY-1747846, BAY 1747846

2-[4,10-bis(carboxylatomethyl)-7-[1-oxo-1-[[2-oxo-2-[[3-[[2-[2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetrazacyclododec-1-yl]propanoylamino]acetyl]amino]-2,2-bis[[[2-[2-[4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetrazacyclododec-1-yl]propanoylamino]acetyl]amino]methyl]propyl]amino]ethyl]amino]propan-2-yl]-1,4,7,10-tetrazacyclododec-1-yl]acetate;tetrakis(gadolinium(3+))

TETRAGADOLINIUM (4,10-BIS(CARBOXYLATOMETHYL)-7-(3,6,12,15-TETRAOXO-16-(4,7,10-TRIS-(CARBOXYLATOMETHYL)-1,4,7,10-TETRAAZACYCLODODECAN-1-YL)-9,9-BIS(((((2-(4,7,10-TRIS-(CARBOXYLATOMETHYL)-1,4,7,10-TETRAAZACYCLODODECAN-1-YL)PROPANOYL)AMINO)ACETYL)-AMINO)METHYL)-4,7,11,14-TETRAAZAHEPTADECAN-2-YL)-1,4,7,10-TETRAAZACYCLODODECAN-1-YL)ACETATE

To detect and visualize lesions with abnormal vascularity, in conjunction with MRI

Gadoquatrane (marketed as AMBELVIST®) is a low-dose, macrocyclic gadolinium-based contrast agent (GBCA) developed by Bayer for use in magnetic resonance imaging (MRI). It is designed to enhance the visualization of lesions in the central nervous system (CNS) and other body regions in adult and pediatric patients.

Core Highlights:

• Lower Gadolinium Exposure: It requires a dose of 0.04 mmol/kg, which results in 60% less gadolinium exposure compared to standard macrocyclic GBCAs.
• Regulatory Approval: The FDA approved it in June 2026 for use in adults and pediatric patients, including term neonates. It was also approved in Japan in March 2026.
• Efficacy & Safety: Phase III clinical trials (the QUANTI studies) showed it effectively detects lesions with abnormal vascularity while maintaining an efficacy and safety profile comparable to other standard macrocyclic agents.
• Structure: Gadoquatrane features a tetrameric, macrocyclic structure that gives it high relaxivity and stability in the body

SYN

https://patents.google.com/patent/US20250114485A1

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PAT

• Gadolinium chelate compounds for use in magnetic resonance imagingPublication Number: US-11491245-B2Priority Date: 2015-06-04Grant Date: 2022-11-08
• Gadolinium chelate compounds for use in magnetic resonance imagingPublication Number: US-2025114485-A1Priority Date: 2015-06-04
• Formulation of contrast media and process of preparation thereofPublication Number: US-2024252690-A1Priority Date: 2018-11-23
• Formulation of contrast media and process of preparation thereofPublication Number: US-12303573-B2Priority Date: 2018-11-23Grant Date: 2025-05-20
• New gadolinium chelate compounds for use in magnetic resonance imagingPublication Number: EP-3611169-A1Priority Date: 2015-06-04
• New gadolinium chelate compounds for use in magnetic resonance imagingPublication Number: US-2023113481-A1Priority Date: 2015-06-04
• New gadolinium chelate compounds for use in magnetic resonance imagingPublication Number: EP-3303307-B1Priority Date: 2015-06-04Grant Date: 2019-09-04
• Generation of artificial contrast-enhanced computed tomography imagesPublication Number: US-2024346718-A1Priority Date: 2023-04-13
• Generation of artificial contrast-enhanced radiological imagesPublication Number: WO-2024100233-A1Priority Date: 2022-11-12
• Generation of artificial contrast-enhanced radiological imagesPublication Number: EP-4616420-A1Priority Date: 2022-11-12
• Automated analysis of radiological imagesPublication Number: WO-2024083466-A1Priority Date: 2022-10-17
• Formulation of contrast media and process of preparation thereofPublication Number: US-11944690-B2Priority Date: 2018-11-23Grant Date: 2024-04-02

/////////gadoquatrane, anax labs, FDA 2026, APPROVALS 2026, Ambelvist, OZG7J613HK, BAY-1747846, BAY 1747846

Lasmotinib

CAS 2127107-15-5

MF C19H19FN4O2S MW386.4 g/mol

3-(carbamoylamino)-5-[2-(3-fluorophenyl)ethynyl]-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide

• N-(2-(N-((3S)(3-Piperidyl))carbamoyl)-5-(2-(3-fluorophenyl)ethynyl)(3-thienyl))aminamide
• 2-Thiophenecarboxamide, 3-((aminocarbonyl)amino)-5-(2-(3-fluorophenyl)ethynyl)-N-(3S)-3-piperidinyl-
• 3-(carbamoylamino)-5-[2-(3-fluorophenyl)ethynyl]-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide
• 2-Thiophenecarboxamide, 3-[(aminocarbonyl)amino]-5-[2-(3-fluorophenyl)ethynyl]-N-(3S)-3-piperidinyl-
• 3-(carbamoylamino)-5-(2-(3-fluorophenyl)ethynyl)-N-((3S)-piperidin-3-yl)thiophene-2-carboxamide

3-(carbamoylamino)-5-[(3-fluorophenyl)ethynyl]-N-[(3S)-piperidin-3-yl]thiophene-2-carboxamide
tyrosine kinase inhibitor, antineoplastic, PHI-101, PHI 101, U2UY9TBQ8Z

Lasmotinib (also known by its research code PHI-101) is a next-generation, orally bioavailable targeted cancer therapy. It functions as a dual FLT3 and CHK2 inhibitor. It is primarily being investigated to treat Acute Myeloid Leukemia (AML) and ovarian cancer.

How It Works

• FLT3 Inhibition: It targets FMS-like tyrosine kinase 3 (FLT3), an enzyme that is often mutated in AML. Lasmotinib is designed to attack not just single activating mutations (ITD or TKD), but also difficult-to-treat double and triple-resistant mutations.
• CHK2 Inhibition: It also inhibits Checkpoint Kinase 2 (CHK2), preventing cancer cells from repairing DNA damage. This causes the cancer cells to undergo apoptosis (programmed cell death).

Key Clinical Advantages

• High Efficacy: In relapsed or refractory AML patients who have previously failed other FLT3 inhibitors, lasmotinib has demonstrated high rates of composite complete remission.
• Safety Profile: Preclinical and early-stage trials indicate a promising safety profile with a very low or 0% occurrence rate of cardiotoxicity (heart damage), which is a common hurdle for some other FLT3-targeting drugs.

Current Development & Combinations

• Developer: Discovered by Seoul National University Hospital and being developed by Pharos iBio.
• Synergistic Therapies: Lasmotinib is currently moving into global clinical trials as a powerful combination therapy. Research shows it synergizes strongly with existing treatments like Venetoclax or Azacytidine, as well as with emerging Menin inhibitors (such as bleximenib) to achieve deep tumor growth inhibition

Lasmotinib is an orally bioavailable inhibitor of checkpoint kinase 2 (chk2), with potential antineoplastic and chemopotentiating activities. Upon oral administration, lasmotinib binds to and inhibits the activity of chk2, which may prevent the repair of DNA damage caused by DNA-damaging agents. This may result in tumor cell apoptosis and potentiate the antitumor efficacies of various chemotherapeutic agents. Chk2, an ATP-dependent serine–threonine kinase, is a key component in the DNA replication-monitoring checkpoint system and is activated by double-stranded breaks (DSBs); activated chk2 is overexpressed by a variety of cancer cell types.

• Chk2 Inhibitor for Recurrent EpitheliAl periToneal, fallopIan or oVarian cancEr (CREATIVE Phase IA Trial)CTID: NCT04678102Phase: Phase 1Status: Unknown statusDate: 2023-06-26
• Evaluation of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of PHI 101 for the Treatment of AMLCTID: NCT04842370Phase: Phase 1Status: Unknown statusDate: 2021-04-20

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=JP405710409&_cid=P21-MQIVJB-43702-2

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=US465154324&_cid=P21-MQIVJB-43702-2

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2024015484&_cid=P21-MQIVJB-43702-2

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2025210599&_cid=P21-MQIVJB-43702-2

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PAT

• Inhibitors of brutons tyrosine kinasePublication Number: US-2021070748-A1Priority Date: 2015-06-02
• New, substituted quinoline compounds as inhibitors of S-nitrosoglutathion reductasePublication Number: HU-E025653-T2Priority Date: 2010-10-08
• New hybrid oligomers. Their preparation process and pharmaceutical compositions containing themPublication Number: AU-2006256439-A1Priority Date: 2005-03-18
• NEW THIOPHENE COMPOUND SUBSTITUTED IN POSITIONS 2,3,5, USED AS A PROTEIN KINASE INHIBITORPublication Number: BR-112018016729-B1Priority Date: 2016-02-16
• 2, 3, 5-substituted thiophene compounds as protein kinase inhibitorsPublication Number: CN-108884066-BPriority Date: 2016-02-16Grant Date: 2021-08-24
• 2,3,5-substituted thiophene compound as protein kinase inhibitorPublication Number: US-10442796-B2Priority Date: 2016-02-16Grant Date: 2019-10-15
• Novel compound of 2,3,5-substituted thiophene as a protein kinase inhibitorPublication Number: RU-2724957-C2Priority Date: 2016-02-16Grant Date: 2020-06-29
• Novel 2,3,5-substituted thiophene compounds as protein kinase inhibitorsPublication Number: KR-101965326-B1Priority Date: 2016-02-16Grant Date: 2019-04-03
• Novel 2,3,5-substituted thiophene compound as protein kinase inhibitorPublication Number: WO-2017142325-A1Priority Date: 2016-02-16
• Novel 2,3,5-substituted thiophene compound as protein kinase inhibitorPublication Number: US-2019047993-A1Priority Date: 2016-02-16
• Novel 2,3,5-substituted thiophene compounds as protein kinase inhibitorsPublication Number: KR-20180136425-APriority Date: 2016-02-16
• Novel 2,3,5-substituted thiophene compound as protein kinase inhibitorPublication Number: EP-3418275-B1Priority Date: 2016-02-16Grant Date: 2021-03-17
• Novel 2,3,5-substituted thiophene compounds that are protein kinase inhibitorsPublication Number: JP-2019504900-APriority Date: 2016-02-16
• Use of 2,3,5-substituted thiophene compound for enhancement of radiotherapyPublication Number: EP-3804719-A1Priority Date: 2018-05-30
• Use of 2,3,5-substituted thiophene compound to prevent, ameliorate, or treat breast cancersPublication Number: EP-3804718-A1Priority Date: 2018-05-30
• Novel 2,3,5-substituted thiophene compound as protein kinase inhibitorPublication Number: EP-3418275-A1Priority Date: 2016-02-16
• New 2,3,5-substituted thiophene compound as a protein kinase inhibitorPublication Number: RU-2018130703-APriority Date: 2016-02-16
• Novel 2,3,5-substituted thiophene compounds as protein kinase inhibitorsPublication Number: KR-20190035671-APriority Date: 2016-02-16
• Radiotherapy-enhancing applications of 2,3,5-substituted thiophene compoundsPublication Number: JP-2021525285-APriority Date: 2018-05-30
• Use of 2,3,5-substituted thiophene compound for enhancement of radiotherapyPublication Number: US-2021205289-A1Priority Date: 2018-05-30
• Use of 2,3,5-Substituted Thiophene Compound for Prevention, Improvement or Treatment of Breast CancerPublication Number: KR-102227117-B1Priority Date: 2018-05-30Grant Date: 2021-03-15
• Use of 2,3,5-Substituted Thiophene Compound for Prevention, Improvement or Treatment of Breast CancerPublication Number: KR-20190136976-APriority Date: 2018-05-30
• Use of 2,3,5-substituted thiophene compound to prevent, ameliorate, or treat breast cancersPublication Number: US-2021205290-A1Priority Date: 2018-05-30

////////lasmotinib, anax labs, tyrosine kinase inhibitor, antineoplastic, PHI-101, PHI 101, U2UY9TBQ8Z

Larubrilstat

CAS 2765226-31-9

MF C21H25N5O2 MW379.5 g/mol

[2-[[(5R)-6,7-dihydro-5H-cyclopenta[b]pyridin-5-yl]amino]pyrimidin-5-yl]-(8-oxa-2-azaspiro[4.5]decan-2-yl)methanone

• [2-[[(5R)-6,7-dihydro-5H-cyclopenta[b]pyridin-5-yl]amino]pyrimidin-5-yl]-(8-oxa-2-azaspiro[4.5]decan-2-yl)methanone
• Methanone, [2-[[(5R)-6,7-dihydro-5H-cyclopenta[b]pyridin-5-yl]amino]-5-pyrimidinyl]-8-oxa-2-azaspiro[4.5]dec-2-yl-

(2-{[(5R)-6,7-dihydro-5H-cyclopenta[b]pyridin-5-yl]amino}pyrimidin-5-yl)(8-oxa-2-azaspiro[4.5]decan-2-
yl)methanone
vascular non-inflammatory molecule-1 (VNN1) inhibitor, AG6K4Y29B4

Larubrilstat is the International Nonproprietary Name (INN) for an experimental, small-molecule vascular non-inflammatory molecule-1 (VNN1) inhibitor. VNN1, also commonly known as Vanin-1 or pantetheinase, is an enzyme involved in tissue response to oxidative stress and inflammation.

Current Status

• Development Context: Larubrilstat is a designated compound linked to therapeutic exploration in inflammatory pathways. Research and patent filings, such as those cataloged by the IUPHAR/BPS Guide to PHARMACOLOGY, track its evaluation alongside similar Vanin-1 inhibitors

SYN

US20240083873,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US425298584&_cid=P20-MQHGA8-93141-1

COMP 2-1 IS PRODUCT

Example 2: Synthesis of Compound 2, Compound 2-1 and Compound 2-2

Step 2

Step 3

Step 4: Preparation of Compound 2-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=28F257EBC3EA6EE7D447E4442C7CC489.wapp2nA?docId=US458059800&_cid=P20-MQHG5H-85832-1

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PAT

• Pyrimidine carboxamide compound and application thereofPublication Number: US-2024083873-A1Priority Date: 2020-09-25
• Pyrimidine carboxamide compound and application thereofPublication Number: WO-2022063197-A1Priority Date: 2020-09-25
• Pyrimidine carboxamide compound and application thereofPublication Number: WO-2022063333-A1Priority Date: 2020-09-25

////////larubrilstat, ANAX LABS, vascular non-inflammatory molecule-1 (VNN1) inhibitor, AG6K4Y29B4

Laporolimus

Rapamycin, 42-cyclohexanecarboxylate

CAS 1504576-27-5

MF C58H89NO14 MW 1024.3 g/mol

[(1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.0^4,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]-2-methoxycyclohexyl] cyclohexanecarboxylate

(1R,2R,4S)-4-{(2R)-2-[(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-10,21-dimethoxy6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,3
1,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1,4]oxazacyclohentriacontin-3-yl]propyl}-2-methoxycyclohexyl
cyclohexanecarboxylate
immunosuppressant, CRC-015, CRC 015, F5041W3RVA, Rapamycin, 42-cyclohexanecarboxylate

Laporolimus is an experimental immunosuppressant compound that acts as an mTOR (mechanistic target of rapamycin) pathway inhibitor. It is chemically classified as a macrolide derivative and is also known by its chemical synonym, rapamycin 42-cyclohexanecarboxylate.

Currently, Laporolimus is designated for research use only and has not been approved for clinical medical applications in humans or animals.

Key Technical Details

• Mechanism of Action: It blocks the mTOR signaling pathway, which is responsible for regulating cell growth, proliferation, and immune cell activation.

Distinguishing Laporolimus from Clinical Alternatives

Because it ends with the suffix -limus, it shares structural and nomenclature similarities with widely used clinical immunosuppressants. However, its legal status and development stage differ significantly:

If you are researching this compound for a laboratory study, you can review its structural data and biochemical properties via the PubChem Laporolimus Compound Page

Laporolimus (CAS 1504576-27-5) is an immunosuppressive agent and mTOR inhibitor structurally derived from rapamycin as a cyclohexanecarboxylate derivative. Its total chemical synthesis is highly complex, typically achieved via semisynthesis starting from natural macrolides produced by Streptomyces fermentation.

Semisynthetic Pathway

Because the core macrocyclic lactone (a 36-membered polyketide ring) is incredibly challenging to build from scratch, researchers and pharmaceutical manufacturers rely on a derivatization approach:

1. Fermentation: The baseline macrolide is produced via large-scale fermentation of Streptomyces hygroscopicus (similar to the base rapamycin process).
2. Purification: The naturally produced macrocyclic core is isolated and purified from the fermentation broth using column chromatography.
3. Esterification: The C-42 hydroxyl group of the macrolide core is selectively protected and subjected to acylation with a cyclohexanecarboxylic acid derivative (or reactive cyclohexanecarbonyl chloride).
4. Deprotection & Purification: The C-42 cyclohexanecarboxylate is then deprotected and purified via preparative chromatography to yield pure laporolimus.

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PAT

/////////laporolimus, immunosuppressant, CRC-015, CRC 015, F5041W3RVA, Rapamycin, 42-cyclohexanecarboxylate