Category «Preclinical»

GFH-018

It’s only fair to share… GFH-018 CAS 2169299-67-4 C21 H19 N7 O, 385.42 (E)-3-[6-[2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-[1,2,4]triazolo[1,5-a]pyridin-5-yl]prop-2-enamide 2-Propenamide, 3-[6-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl][1,2,4]triazolo[1,5-a]pyridin-5-yl]-, (2E)- GenFleet Therapeutics Advanced solid tumor; Cancer TGF-beta Receptor Type-1 (TGFBR1; ALK5; SKR4; TbetaR-I) Inhibitors Signal Transduction Modulators GFH-018 , a TGFBR1 inhibitor, being investigated by GenFleet as an oral tablet formulation, for the treatment of cancer, including advanced solid tumors and hepatocellular carcinoma,  …

BI-882370

It’s only fair to share…   BI-882370 XP-102 N-(3-(5-((1-ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide CAS 1392429-79-6 Chemical Formula: C28H33F2N7O2S Molecular Weight: 569.68 Elemental Analysis: C, 59.03; H, 5.84; F, 6.67; N, 17.21; O, 5.62; S, 5.63 N-(3-(5-((1-ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide N-(3-{5-[(1-Ethylpiperidin-4-Yl)(Methyl)amino]-3-(Pyrimidin-5-Yl)-1h-Pyrrolo[3,2-B]pyridin-1-Yl}-2,4-Difluorophenyl)propane-1-Sulfonamide N-[3-[5-[(1-ethylpiperidin-4-yl)-methylamino]-3-pyrimidin-5-ylpyrrolo[3,2-b]pyridin-1-yl]-2,4-difluorophenyl]propane-1-sulfonamide BI 882370 is a highly potent and selective RAF inhibitor that binds to the DFG-out (inactive) conformation of the BRAF kinase. BI …

SRT-1720

It’s only fair to share… SRT-1720 diHCl CAY10559 CAS: 1001645-58-4 (di HCl) , 925434-55-5 (free base)   1001645-58-4 (HCl) Chemical Formula: C25H25Cl2N7OS Molecular Weight: 542.483 Elemental Analysis: C, 55.35; H, 4.65; Cl, 13.07; N, 18.07; O, 2.95; S, 5.91 SRT-1720 HCl, SRT-1720 hudrochloride; SRT1720; SRT-1720; SRT 1720; CAY10559; CAY-10559; CAY 10559; SIRT-1933; SIRT 1933; SIRT1933.  N-(2-(3-(piperazin-1-ylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)quinoxaline-2-carboxamide dihydrochloride Molecular …

K-8986

It’s only fair to share… K-8986 (Z)-but-2-enedioic acid;7-[3-[4-[[1-(2-ethoxyethyl)benzimidazol-2-yl]methyl]piperazin-1-yl]propoxy]-4H-1,4-benzothiazin-3-one cas 1335112-55-4 mono maleate cas 1335112-57-6  di maleate cas 219741-69-2 free form C27 H35 N5 O3 S . C4 H4 O4 2H-1,4-Benzothiazin-3(4H)-one, 7-[3-[4-[[1-(2-ethoxyethyl)-1H-benzimidazol-2-yl]methyl]-1-piperazinyl]propoxy]-, (2Z)-2-butenedioate (1:1) 7-[3-[4-[[1-(2-Ethoxyethyl)benzimidazol-2-yl]methyl]-1-piperazinyl]propoxy]-3,4-dihydro-2H-1,4-benzothiazin-3-one monomaleate KOWA CO., LTD. 福田 友昭 FUKUDA, Tomoaki; JP 纐纈 章泰 KOKETSU, Akiyasu; JP 金児 佳生 KANEKO, Yoshio; JP 芦川 由香 ASHIKAWA, Yuka; JP Mono maleate 1H NMR (396 MHz, DMSO-d6) δ 1.03 (t, J = …

BMS-986169

It’s only fair to share… BMS-986169 CAS 1801151-08-5 Related CAS : 1801151-09-6   1801151-08-5 Chemical Formula: C23H27FN2O2 Molecular Weight: 382.4794 Elemental Analysis: C, 72.23; H, 7.12; F, 4.97; N, 7.32; O, 8.37 (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (3R)-3-[(3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl]-1-[(4-methylphenyl)methyl]pyrrolidin-2-one Preclinical BMS-986169 is a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder. BMS-986169 showed high binding affinity for …

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

It’s only fair to share… 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), …

Takeda’s Peripherally selective noradrenaline reuptake inhibitor

It’s only fair to share… 1-{[(6S,7R)-7-(4-Chloro-3-fluorophenyl)-1,4-oxazepan-6-yl]methyl}-2-oxo-1,2-dihydro-3-pyridinecarboxylic acid Molecular Formula C18H18ClFN2O4 Average mass 380.798 Da CAS 1372185-97-1 CAS 1372180-09-0 hydrochloride Peripherally selective noradrenaline reuptake inhibitor 1-([(6S,7R)-7-(4-Chloro-3-fluorophenyl)-1,4-oxazepan-6-yl]methyl]-2-oxo-1,2-dihydropyridine-3-carboxylic acid monohydrochloride 3-Pyridinecarboxylic acid, 1-[[(6S,7R)-7-(4-chloro-3-fluorophenyl)hexahydro-1,4-oxazepin-6-yl]methyl]-1,2-dihydro-2-oxo-, hydrochloride (1:1) 1-{[(6S,7R)-7-(4-Chloro-3-fluorophenyl)-1,4-oxazepan-6-yl]methyl}-2-oxo-1,2-dihydropyridine-3-carboxylic Acid Hydrochloride (1:1) (1·HCl) TAKEDA PHARMACEUTICAL COMPANY LIMITED [JP/JP]; 1-1, Doshomachi 4-chome, Chuo-ku, Osaka-shi, Osaka 5410045 (JP) ISHICHI, Yuji; (JP). YAMADA, Masami; (US). KAMEI, Taku; …

NVP-LXS196

It’s only fair to share… NVP-LXS196 CAS 1874276-76-2 3-amino-N-[3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl]-6-[3-(trifluoromethyl)pyridin-2-yl]pyrazine-2-carboxamide 3-Amino-N-[3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl]-6-[3-(trifluoromethyl)pyridin-2-yl]pyrazine-2-carboxamide Molecular Formula: C22H23F3N8O Molecular Weight: 472.476 g/mol   Inventors Michael Joseph Luzzio, Julien Papillon,Michael Scott Visser Applicant Novartis Ag   Michael Joseph Luzzio Julien Papillon, Michael Scott Visser SYNTHESIS Uveal melanoma (UM) is the most common cancer of the eye in adults (Singh AD. et al., …

PF 06821497

It’s only fair to share…   PF 06821497 Cas 1844849-11-1 Designed to treat lymphoma 1(2H)-Isoquinolinone, 5,8-dichloro-2-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-3,4-dihydro-7-[(S)-methoxy-3-oxetanylmethyl]- MF C22 H24 Cl2 N2 O5,  MW 467.34 PF 06821497 5,8-Dichloro-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-7-[methoxy(3-oxetanyl)methyl]-3,4-dihydro-1(2H)-isoquinolinone 1(2H)-Isoquinolinone, 5,8-dichloro-2-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-3,4-dihydro-7-(methoxy-3-oxetanylmethyl)- Molecular Formula C22H24Cl2N2O5 Average mass 467.342 Da PF 06821497 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(S)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one US2015361067 Inventors Michael Raymond Collins, Robert Steven Kania, Robert Arnold Kumpf, Pei-Pei Kung, Daniel Tyler Richter, Scott Channing Sutton, …

Debio-1452

It’s only fair to share… Debio-1452, AFN 1252 AFN-1252; UNII-T3O718IKKM; API-1252; CAS 620175-39-5; CHEMBL1652621; (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide MFC22 H21 N3 O3 2-Propenamide, N-methyl-N-[(3-methyl-2-benzofuranyl)methyl]-3-(5,6,7,8-tetrahydro-7-oxo-1,8-naphthyridin-3-yl)-, (2E)-  MW375.42 Phase 2, clinical trials for the oral treatment of staphylococcal infections, including hospital and community-acquired MRSA and acute bacterial skin and skin structure infections Qualified Infectious Disease Product designation GlaxoSmithKline plc INNOVATOR Debiopharm …