Category «Phase 2»

BMS 262084

It’s only fair to share… BMS-262084 CAS 253174-92-4 Molecular FormulaC18H31N7O5 Average mass425.483 Da NII-I0IR71971G I0IR71971G (2S,3R)-1-[4-(tert-butylcarbamoyl)piperazine-1-carbonyl]-3-[3-(diaminomethylideneamino)propyl]-4-oxoazetidine-2-carboxylic acid (2S,3R)-1-{[4-(tert-butylcarbamoyl)piperazin-1-yl]carbonyl}-3-{3-[(diaminomethylidene)amino]propyl}-4-oxoazetidine-2-carboxylic acid (2S,3R)-3-{3-[(Diaminomethylene)amino]propyl}-1-({4-[(2-methyl-2-propanyl)carbamoyl]-1-piperazinyl}carbonyl)-4-oxo-2-azetidinecarboxylic acid 253174-92-4 [RN] 2-Azetidinecarboxylic acid, 3-[3-[(diaminomethylene)amino]propyl]-1-[[4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperazinyl]carbonyl]-4-oxo-, (2S,3R)- Factor XIa inhibitors (thrombosis), BMS; Factor XIa inhibitors (thrombosis), Bristol-Myers Squibb; BMS-654457; Factor XIa inhibitors (cardiovascular diseases), BMS; BMS-724296 Novel crystalline forms of BMS-262084  as Factor XIa antagonist useful for …

Catequentinib, Anlotinib

It’s only fair to share… Catequentinib C23H22FN3O3  407.4 g/mol 1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxyquinolin-7-yl]oxymethyl]cyclopropan-1-amine 1058156-90-3 CAS No. 1360460-82-7 DI HCL Molecular Weight 480.36 Formula C23H22FN3O3 • 2HCl Anlotinib AL3818 UNII-GKF8S4C432 Chia Tai Tianqing Pharmaceutical Group Co Ltd Launched (Metastatic non small cell lung cancer – China – May-2018) Orphan Drug; Priority Review MOA:VEGFR inhibitor Indication:advanced gastric adenocarcinoma; Advanced renal cell carcinoma (RCC); Medullary thyroid …

ETRUMADENANT

It’s only fair to share… ETRUMADENANT CAS 2239273-34-6 C23 H22 N8 O, 426.47 Benzonitrile, 3-[2-amino-6-[1-[[6-(1-hydroxy-1-methylethyl)-2-pyridinyl]methyl]-1H-1,2,3-triazol-4-yl]-4-pyrimidinyl]-2-methyl- 3-[2-Amino-6-[1-[[6-(1-hydroxy-1-methylethyl)-2-pyridinyl]methyl]-1H-1,2,3-triazol-4-yl]-4-pyrimidinyl]-2-methylbenzonitrile AB 928 Arcus Biosciences is developing etrumadenant, the lead from the small molecule adenosine (A2a/A2b) dual receptor antagonist program, for treating cancer. In November 2020, preliminary data from ARC-7 in metastatic NSCLC were expected to report in the first half of 2021. OriginatorArcus Biosciences …

TILDACERFONT

It’s only fair to share… TILDACERFONT Synonyms: Tildacerfont 1014983-00-6 3-(4-Chloro-2-morpholin-4-yl-thiazol-5-yl)-7-(1-ethyl-propyl)-2,5-dimethyl-pyrazolo[1,5-a]pyrimidine 7-(1-ethyl-propyl)-3-(4-chloro-2-morpholin-4-yl-thiazol-5-yl)-2,5-dimethyl-pyrazolo[1,5-a]pyrimidine MW/ MF 420 g/mol/ C20H26ClN5OS Originator Spruce Biosciences Class2 ring heterocyclic compounds; Morpholines; Pyrazoles; Pyrimidines; Small molecules; Thiazoles Mechanism of Action Corticotropin receptor antagonists Orphan Drug Status Yes – Congenital adrenal hyperplasia New Molecular Entity Yes Phase II Congenital adrenal hyperplasia 09 Jul 2020 Spruce Biosciences initiates a phase II trial …

SULCARDINE SULPHATE

It’s only fair to share… sulcardine, HBI-3000 B 87823 Molecular FormulaC24H33N3O4S Average mass459.602 Da N-[[4-hydroxy-3,5-bis(pyrrolidin-1-ylmethyl)phenyl]methyl]-4-methoxybenzenesulfonamide Benzenesulfonamide, N-[[4-hydroxy-3,5-bis(1-pyrrolidinylmethyl)phenyl]methyl]-4-methoxy- N-[4-Hydroxy-3,5-bis(1-pyrrolidinylmethyl)benzyl]-4-methoxybenzenesulfonamide 343935-60-4 [RN] heart arrhythmia CAS No. : 343935-61-5 (Sulcardine sulfate) Synonyms: B-87823; HBI-3000; B87823; HBI3000; B 87823; HBI 3000;N-(4-hydroxy-3,5-bis(pyrrolidin-1-ylmethyl)benzyl)-4-methoxybenzenesulfonamide sulfate Molecular Formula: C24H35N3O8S2 Molecular Weight: 557.67 Originator Jiangsu Furui Pharmaceuticals; Shanghai Institute of Materia Medica Developer HUYA Bioscience International; Jiangsu Furui Pharmaceuticals Class Antiarrhythmics; …

LANRAPLENIB

It’s only fair to share… LANRAPLENIB GS-9876 Phase II, GILEAD Phase II Gilead Cutaneous lupus erythematosus Rheumatoid arthritis Sjogren syndrome GS-9876  LANRAPLENIB Imidazo(1,2-a)pyrazin-8-amine, 6-(6-amino-2-pyrazinyl)-N-(4-(4-(3-oxetanyl)-1-piperazinyl)phenyl)- 6-(6-Aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo|1,2-a]pyrazin-8-amine 6-(6-Amino-2-pyrazinyl)-N-(4-(4-(3-oxetanyl)-1-piperazinyl)phenyl)imidazo(1,2-a)pyrazin-8-amine Molecular Weight 443.50 Formula C₂₃H₂₅N₉O CAS No. 1800046-95-0 Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) …

NIDUFEXOR

It’s only fair to share… NIDUFEXOR LMB763 4-[[benzyl-(8-chloro-1-methyl-4H-chromeno[4,3-c]pyrazole-3-carbonyl)amino]methyl]benzoic acid Nidufexor is a farnesoid X receptor (FXR) agonist. Molecular Weight 487.93 Formula C₂₇H₂₂ClN₃O₄ CAS No. 1773489-72-7 PHASE 2 Treatment of Liver and Biliary Tract Disorders, Agents for Diabetic Nephropathy, NOVARTIS Nidufexor 1773489-72-7, LMB-763, UNII-CJ1PL0TE6J, CJ1PL0TE6J, BCP28929, EX-A1854 Nidufexor pound LMB-763 pound(c) ZINC584641402 4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoic acid HY-109096 CS-0039398   https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.9b01621 1 (7.6 g, 89% yield) as …

LNP 023

It’s only fair to share… LNP 023 CAS 1644670-37-0 ROTATION + 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic acid M.Wt 422.525 Formula C25H30N2O4 4-[(2S,4S)-4-ethoxy-1-[(5-methoxy-7-methyl-1H-indol-4-yl)methyl]piperidin-2-yl]benzoic acid LNP023 RENRQMCACQEWFC-UGKGYDQZSA-N PATENT US9682968, Example-26a BDBM160475 ZINC223246892 HY-127105 CS-0093107 4-((2S,4S)-(4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl))benzoic acid 4-[(2~{S},4~{S})-4-ethoxy-1-[(5-methoxy-7-methyl-1~{H}-indol-4-yl)methyl]piperidin-2-yl]benzoic acid LNP023 (LNP-023) is a highly potent, reversible, selective inhibitor of factor B (IC50=10 nM), the proteolytically active component of the C3 and C5 convertases. …

LYS 228

It’s only fair to share…   LYS228 BOS-228 LYS-228 Molecular Formula, C16-H18-N6-O10-S2 Molecular Weight, 518.4783 (3S,4R)-3-((Z)-2-(2-Ammoniothiazol-4-yl)-2-((1-carboxycyclopropoxy)imino)acetamido)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)azetidine-1-sulfonate RN: 1810051-96-7 UNII: 29H7N9XI1B   UNII-005B24W9YP 005B24W9YP Lys-228 trihydrate 2091840-43-4 Yclopropanecarboxylic acid, 1-(((Z)-(1-(2-amino-4-thiazolyl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxo-3-oxazolidinyl)methyl)-1-sulfo-3-azetidinyl)amino)ethylidene)amino)oxy)-, hydrate (1:3) 1-[(Z)-[1-(2-amino-1,3-thiazol-4-yl)-2-oxo-2-[[(3S,4R)-2-oxo-4-[(2-oxo-1,3-oxazolidin-3-yl)methyl]-1-sulfoazetidin-3-yl]amino]ethylidene]amino]oxycyclopropane-1-carboxylic acid;trihydrate BOS-228 (LYS-228) is a monobactam discovered at Novartis and currently in phase II clinical development at Boston Pharmaceuticals for the treatment of complicated urinary …

Islatravir (MK-8591, EFdA)

It’s only fair to share… Islatravir (MK-8591, EFdA) 2′-Deoxy-4′-ethynyl-2-fluoroadenosine Molecular FormulaC12H12FN5O3 Average mass293.254 Da 865363-93-5 2′-Deoxy-4′-ethynyl-2-fluoroadenosine 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine Adenosine, 2′-deoxy-4′-C-ethynyl-2-fluoro- (2R,3S,5R)-5-(6-amino-2-fluoro-9H-purin-9-yl)-2-ethynyl-2-(hydroxymethyl)tetrahydrofuran-3-ol 2′-deoxy-4′-c-ethynyl-2-fluoroadenosine 865363-93-5 [RN] 9H-Purin-6-amine, 9-(2-deoxy-4-C-ethynyl-β-D-erythro-pentofuranosyl)-2-fluoro- E2FDA (2R,3S,5R)-5-(6-amino-2-fluoropurin-9-yl)-2-ethynyl-2-(hydroxymethyl)oxolan-3-ol MK-8591 UNII:QPQ082R25D Islatravir is known to be a nucleoside reverse transcriptase inhibitor, useful for treating HIV-1 and -2 infection and AIDS. Islatravir (MK-8591, EFdA), useful for the treatment of …