Drug Approvals International – Page 118 – All about Drugs Live by Dr Anthony Melvin Crasto

PH 46A

PH 46A cas 1421332-97-9 C27 H24 O3, 396.48 Benzoic acid, 4-[[(1S,2S)-2,3-dihydro-1-hydroxy[2,2′-bi-1H-inden]-2-yl]methyl]-, methyl ester Methyl 4-(((1S,2S)-1-hydroxy-2,3-dihydro-1H,1’H-[2,2′-biinden]-2-yl)methyl)benzoate FREE ACID CAS 1380445-03-3, Benzoic acid, 4-[[(1S,2S)-2,3-dihydro-1-hydroxy[2,2′-bi-1H-inden]-2-yl]methyl]- N-Methyl-(D)-Glucamine salt (NMDG) 1380445-04-4 C26 H22 O3 . C7 H17 N O5 D-Glucitol, 1-deoxy-1-(methylamino)-, 4-[[(1S,2S)-2,3-dihydro-1-hydroxy[2,2′-bi-1H-inden]-2-yl]methyl]benzoate (1:1) PH46A, belonging to a class of 1,2-Indane dimers, has been developed by Trino Therapeutics Ltd research group as a potential therapeutic agent for the treatment of inflammatory …

Normal Operating Range (NOR) and Proven Acceptable Range (PAR)

In June of this year, the EMA issued a revision of their earlier Q&A document focused on NORs, PARs, and DSp.(2) First issued in draft form in 2015, this has been revised based on feedback and consultation with industry. The document focuses on five questions, which are summarized below along with a reflection on the answer …

Ruthenium-Catalyzed Tandem C–H Fluoromethylation/Cyclization of N-Alkylhydrazones with CBr3F: Access to 4-Fluoropyrazoles

4-Fluoropyrazoles are accessible in a single step from readily available aldehyde-derived N-alkylhydrazones through double C–H fluoroalkylation with tribromofluoromethane (CBr3F). RuCl2(PPh3)3 has been proven to be the most efficient catalyst for this transformation when compared to a range of other Cu-, Pd-, or Fe-based catalyst systems. Alexis Prieto Alexis Prieto, Didier Bouyssi*, and Nuno Monteiro* Univ Lyon, Université Claude Bernard …

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

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 inhibitor potentially for the treatment …

LL 3858, SUDOTERB From LUPIN For TB

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 for Tuberculosis in India (unspecified …

Continuous-Flow Preparation of γ-Butyrolactone Scaffolds, 2-(5,5-dimethyl-2-oxotetrahydrofuran-3- yl)acetic acid

(5,5-dimethyl-2-oxotetrahydrofuran-3-yl)acetic acid 2-(5,5-Dimethyl-2-oxotetrahydrofuran-3-yl)acetic acid 2-carboxymethyl-4-methyl-4-pentanolide, Cas 412298-86-3 2-(5,5-Dimethyl-2-oxotetrahydrofuran-3-yl)acetic acid (4a). 1H NMR (DMSO-d6, 400 MHz): δ = 3.20 – 3.10 (m, 1H), 2.62 (dd, J = 17.1, 4.4 Hz, 1H), 2.54 – 2.45 (m, 1H), 2.31 – 2.21 (m, 1H), 1.84 (t, J = 12.0 Hz, 1H), 1.39 (s, 3H), 1.33 (s, 3H) …

FDA approves first biosimilar Herceptin (trastuzumab) for the treatment of certain breast and stomach cancers

FDA approves first biosimilar for the treatment of certain breast and stomach cancers Ogivri, a biosimilar to the cancer drug Herceptin, is approved for HER2+ breast cancer and metastatic stomach cancers The U.S. Food and Drug Administration today approved Ogivri (trastuzumab-dkst) as a biosimilar to Herceptin (trastuzumab) for the treatment of patients with breast or …

Palladium-catalyzed direct C-H ethoxycarbonylation of 2-aryl-1,2,3-triazoles and efficient synthesis of suvorexant

Palladium-catalyzed direct C-H ethoxycarbonylation of 2-aryl-1,2,3-triazoles and efficient synthesis of suvorexant Org. Chem. Front., 2018, Advance Article DOI: 10.1039/C7QO00945C, Research Article Rui Sang, Yang Zheng, Hailong Zhang, Xiaohua Wu, Qiantao Wang, Li Hai, Yong Wu Palladium-catalyzed direct ethoxycarbonylation with diethyl azodicarboxylate was developed and its reaction mechanism was explored by using DFT calculations. Palladium-catalyzed …

VOXELOTOR

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 Phase I Hypoxia; Liver disorders Discontinued Idiopathic …

The synthesis, biological evaluation and structure–activity relationship of 2-phenylaminomethylene-cyclohexane-1,3-diones as specific anti-tuberculosis agents

CAS 74102-02-6 Molecular Formula: C15H17NO3 Molecular Weight: 259.305 g/mol 2-(((2-hydroxyphenyl)amino)methylene)-5,5-dimethylcyclohexane-1,3-dione (39): White solid; m.p. 249 o C; TLC Rf value, 0.48 (in EtOAc:Hexane,60:40); IR (neat) 2980, 2950, 1678, 1040 cm-1; 1 H NMR (400 MHz, CD3OD) δ 9.86 (1H, bs), 8.66 (1H, d, J = 16.0 Hz), 7.46- 7.34 (1H, m), 7.07-6.84 (3H, m), 2.46 (2H, …