Category «PHASE 3»

Fedratinib

It’s only fair to share… FEDRATINIB SAR-302503; TG-101348, 6L1XP550I6, 936091-26-8 [RN], WHO 9707 Molecular Formula: C27H36N6O3S Molecular Weight: 524.684 g/mol FLT3, JAK2 http://www.ama-assn.org//resources/doc/usan/fedratinib.pdf Fedratinib had been in phase III clincial trials by Sanofi for the treatment of myelofibrosis. However, Sanofi had discontinued this research because of the safety issues. Orphan drug designation was assigned in the U.S. and in …

Larotrectinib, ларотректиниб , 拉罗替尼 ,

It’s only fair to share…   Larotrectinib ARRY-470, LOXO-101, PF9462I9HX Molecular Formula: C21H22F2N6O2 Molecular Weight: 428.444 g/mol (3S)-N-{5-[(2R)-2-(2,5-Difluorphenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl}-3-hydroxy-1-pyrrolidincarboxamid (S)-N-{5-[(R)-2-(2,5-Difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl}-3-hydroxypyrrolidine-1-carboxamide 10360 1223403-58-4 [RN] UNII:PF9462I9HX ларотректиниб [Russian] [INN] 拉罗替尼 [Chinese] [INN] (3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxypyrrolidine-1-carboxamide NTRK-fusion solid tumours TRK inhibitor orphan drug designation in the U.S In 2013, Array Biopharma licensed the product to Loxo Oncology for development and commercialization in the U.S. In 2016, breakthrough therapy …

ELECLAZINE, элеклазин , إيليكلازين , 依来克秦 , REVISITED

It’s only fair to share… ELECLAZINE GS-6615 Molecular Formula: C21H16F3N3O3 Molecular Weight: 415.372 g/mol 1443211-72-0 4-(pyrimidin-2-ylmethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1,4-benzoxazepin-5-one 4-(pyrimidin-2-ylmethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3,4,5- tetrahydro-1,4- benzoxazepin-5-one 7-(4-(Trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one 1,4-Benzoxazepin-5(2H)-one, 3,4-dihydro-4-(2-pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]- Eleclazine; UNII-PUY08529FK; 1443211-72-0; GS-6615; PUY08529FK; 4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-on элеклазин [Russian] [INN] إيليكلازين [Arabic] [INN] 依来克秦 [Chinese] [INN] Phase III Long QT syndrome INGREDIENT UNII CAS Eleclazine Hydrochloride 4R1JP3Q4HI 1448754-43-5 Eleclazine has been used in trials studying the treatment of LQT2 Syndrome, Long …

LASMIDITAN

It’s only fair to share…   LASMIDITAN, COL-144 , LY-573144 613677-28-4 HYDROCHLORIDE 439239-90-4 (free base) 2,4,6-Trifluoro-N-[6-(1-methylpiperidin-4-ylcarbonyl)pyridin-2-yl]benzamide 2,4,6-trifluoro-N-{6-[(1-methylpiperidin-4-yl)carbonyl]pyridin-2-yl}benzamide CoLucid Pharmaceuticals, PHASE 3, MIGRAINE UNII:760I9WM792 Lasmiditan succinate; UNII-W64YBJ346B; Lasmiditan succinate [USAN]; W64YBJ346B; 439239-92-6; Lasmiditan succinate (USAN) Molecular Formula: C42H42F6N6O8 Molecular Weight: 872.822 g/mol Lasmiditan (COL-144) is an investigational drug for the treatment of acute migraine. It is being developed by Eli Lilly and …

ELAGOLIX

It’s only fair to share… ELAGOLIX Molecular FormulaC32H30F5N3O5 Average mass631.590 Da NBI56418, ABT 620 UNII:5B2546MB5Z 4-({(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-3,6-dihydro-1(2H)-pyrimidinyl]-1-phenylethyl}amino)butanoic acid 834153-87-6 FREE ACID SODIUM SALT  832720-36-2 Acide 4-({(1R)-2-[5-(2-fluoro-3-méthoxyphényl)-3-[2-fluoro-6-(trifluorométhyl)benzyl]-4-méthyl-2,6-dioxo-3,6-dihydro-1(2H)-pyrimidinyl]-1-phényléthyl}amino)butanoïque Butanoic acid, 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]- GNRH antagonist, Endometriosis Endometriosis PREREGISTERED Phase III Uterine leiomyoma WO2001055119A2, Inventors Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers, Applicant Neurocrine Biosciences, Inc. WO 2005007165 PDT PATENT …

Gedatolisib, гедатолисиб , غيداتوليسيب , 吉达利塞 ,

It’s only fair to share… Gedatolisib Pfizer PF-05212384; PF-5212384; PKI-587 CAS 1197160-78-3 Chemical Formula: C32H41N9O4 Molecular Weight: 615.72 1-(4-{[4-(Dimethylamino)-1-piperidinyl]carbonyl}phenyl)-3-{4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl}urea 3-{4-[bis(morpholin-4-yl)-1,3,5-triazin-2-yl]phenyl}-1-{4-[4-(dimethylamino)piperidine-1-carbonyl]phenyl}urea N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N‘-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea гедатолисиб [Russian] [INN] غيداتوليسيب [Arabic] [INN] 吉达利塞 [Chinese] [INN] Phase III Acute myeloid leukaemia Phase II Colorectal cancer; Non-small cell lung cancer Phase I Breast cancer; Solid tumours Discontinued Endometrial cancer Most Recent Events 22 Nov 2017Pfizer suspends patient enrolment in a phase I/II …

FEVIPIPRANT

It’s only fair to share…   FEVIPIPRANT Molecular Formula: C19H17F3N2O4S Molecular Weight: 426.41 g/mol UNII-2PEX5N7DQ4; 2PEX5N7DQ4; NVP-QAW039; QAW039; CAS 872365-14-5 Product patent WO2005123731A2, NOVARTIS Inventors Kamlesh Bala, Catherine Leblanc, David Andrew Sandham, Katharine Louise Turner, Simon James Watson, Lyndon Nigel Brown, Brian Cox, Less « Applicant Novartis Ag, Novartis Pharma Gmbh Jun 17, 2004 priority   expiry 2014 SYN 2-[2-methyl-1-[[4-methylsulfonyl-2-(trifluoromethyl)phenyl]methyl]pyrrolo[2,3-b]pyridin-3-yl]acetic acid 2-Methyl-1-[[4-(methylsulfonyl)-2-(trifluoromethyl)phenyl]methyl]-1H-pyrrolo[2,3-b]pyridine-3-acetic acid [1-(4-((Methane)sulfonyl)-2-trifluoromethylbenzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]acetic acid Fevipiprant (INN; …

Upadacitinib, ABT-494, упадацитиниб , أوباداسيتينيب , 乌帕替尼 ,

It’s only fair to share… ABT 494 (-)-(3S,4R)  cis form CAS 1310726-60-3 FREE FORM    MF C17H19F3N6O MW 380.36757 g/mol Tartrate form  C17 H19 F3 N6 O . C4 H6 O6 . 4 H2 O ………….CAS 1607431-21-9 1-Pyrrolidinecarboxamide, 3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-, (3S,4R)-, (2R,3R)-2,3-dihydroxybutanedioate, hydrate (1:1:4) FREE FORM (3s,,4R)-3-ethyl-4-(3H-imidazo[l,2-fl]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine- l-carboxamide. (35,,4R)-3-ethyl-4-(3H- imidazo[l,2-fl]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine- l-carboxamide, (cis,)-3-ethyl-4-(3H-imidazo[l,2-fl]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-l-carboxamide 1-Pyrrolidinecarboxamide, 3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-, (3S,4R)- rel-(-)-(3S,4R)-3-Ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide A Jak1 …

LL 3858, SUDOTERB From LUPIN For TB

It’s only fair to share… LL 3858, SUDOTERB UNII-SK2537665A; CAS 676266-31-2; N-[2-methyl-5-phenyl-3-[[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]methyl]pyrrol-1-yl]pyridine-4-carboxamide; N-[2-Methyl-5-phenyl-3-[[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]methyl]-1H-pyrrol-1-yl]-4-pyridinecarboxamide Sudoterb(TM) Molecular Formula: C29H28F3N5O Molecular Weight: 519.572 g/mol Originator Lupin Class Antituberculars; Isonicotinic acids; Pyrroles Mechanism of Action Undefined mechanism Orphan Drug Status No New Molecular Entity Yes Highest Development Phases No development reported Tuberculosis Most Recent Events 23 Jul 2015 No recent reports on development identified – Phase-II …

VOXELOTOR

It’s only fair to share… VOXELOTOR GBT 440; GTx-011, Treatment of Sickle Cell Disease RN: 1446321-46-5 UNII: 3ZO554A4Q8 Molecular Formula, C19-H19-N3-O3, Molecular Weight, 337.3771 Benzaldehyde, 2-hydroxy-6-((2-(1-(1-methylethyl)-1H-pyrazol-5-yl)-3-pyridinyl)methoxy)- 2-hydroxy-6-((2-(1-(propan-2-yl)-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde NMR http://file.selleckchem.com/downloads/nmr/S854001-GBT440-CDCl3-hnmr-selleck.pdf Originator Global Blood Therapeutics Class Antianaemics; Small molecules Mechanism of Action Abnormal haemoglobin modulators; Sickle haemoglobin modulators Orphan Drug Status Yes – Sickle cell anaemia New Molecular Entity Yes Highest Development Phases Phase III Sickle cell anaemia …