Category «Preclinical»

SK1-I , BML 258

It’s only fair to share…   SK1-I , BML 258 Sphingosine kinase 1 (SphK1) inhibitor; antiproliferative (1E)-1,2,4-Trideoxy-4-(methylamino)-1-(4-pentylphenyl)-D-erythro-pent-1-enitol (E,2R,3S)-2-(Methylamino)-5-(4-pentylphenyl)pent-4-ene-1,3-diol D-erythro-Pent-1-enitol, 1,2,4-trideoxy-4-(methylamino)-1-(4-pentylphenyl)-, (1E)- Name: (2R,3S,4E)-N-methyl-5-(4′-pentylphenyl)-2-aminopent-4-ene-1,3-diol . HCl Formula: C17H27NO2 . HCl MW: 313.9 CAS: 1072443-89-0   Originator Enzo Biochem; Virginia Commonwealth University Developer Enzo Biochem Class Antineoplastics; Small molecules Mechanism of Action Sphingosine kinase inhibitors Preclinical Autoimmune hepatitis; Haematological malignancies; Liver cancer; Solid tumours …

SYN-01

It’s only fair to share…     SYN-01, SYN-510 Synthena AG Preclinical Synthena , presumed to be under license from  University of Bern , is investigating (presumably SYN-01 ), a lead from the tricyclo(tc)-DNA based antisense oligonucleotides (AON) developed using its proprietary tricyclo-DNA technology platform, for the treatment of Duchenne muscular dystrophy. In January 2017, …

HS-10340

It’s only fair to share…   HS-10340 CAS 2156639-66-4 MF C26 H31 N7 O5 MW 521.57 1,8-Naphthyridine-1(2H)-carboxamide, N-[5-cyano-4-[[(1R)-2-methoxy-1-methylethyl]amino]-2-pyridinyl]-7-formyl-3,4-dihydro-6-[(tetrahydro-2-oxo-1,3-oxazepin-3(2H)-yl)methyl]- (R)-N-(5-cyano-4-((1-methoxypropan-2-yl)amino)pyridin-2-yl)-7-formyl-6-((2-carbonyl)-1,3-oxazepine-3-yl)methyl)-3,4-dihydro-1,8-naphthyridin-1(2H)-carboxamide CAS 2307670-65-9 Jiangsu Hansoh Pharmaceutical Group Co Ltd Being investigated by Jiangsu Hansoh, Shanghai Hansoh Biomedical and Changzhou Hengbang Pharmaceutical ; in June 2018, the product was being developed as a class 1 chemical drug in China. Useful for treating liver cancer, gastric …

CS-3001

It’s only fair to share…   CS-3001 BB 7, VX 033 CAS 2159116-56-8 Propanoic acid, 2-[[5-bromo-4-(3-cyclopropyl-5,5-difluoro-4,5,6,7-tetrahydrobenzo[c]thien-1-yl)-4H-1,2,4-triazol-3-yl]thio]-2-methyl- Molecular Weight, 478.37 C17 H18 Br F2 N3 O2 S2 CStone Pharmaceuticals Co Ltd, JUNE 2018 IND FILED CHINA URAT1 inhibitor – useful for treating hyperuricemia and gout. The compound was originally claimed in WO2017202291 , covering thiophene derivative URAT1 inhibitors, useful for treating hyperuricemia …

TL-487

It’s only fair to share… TL-487 CAS  1469746-55-1 2-Butenamide, N-[3-cyano-7-ethoxy-4-[(4-phenoxyphenyl)amino]-6-quinolinyl]-4-(dimethylamino)-, (2E)- Molecular Weight, 507.58, MF C30 H29 N5 O3 Teligene Inc(2E)-N-[3-Cyano-7-ethoxy-4-[(4-phenoxyphenyl)amino]-6-quinolinyl]-4-(dimethylamino)-2-butenamide (E)-N-(3-cyano-7-ethoxy-4-((4-phenoxyphenyl)amino)quinolin-6-yl)-4-(dimethylamino)but-2-enamide Maleate in anhydrous or monohydrate CAS, 2326561-36-6, AND 2326561-38-8 form are BTK and HER-2 kinase inhibitor useful for treating cancer Useful for treating breast cancer, ovary cancer and colon cancer. are BTK and HER-2 kinase inhibitor useful for treating cancer. Anticancer …

HM04 or H0900

It’s only fair to share…   HM04 or H0900 Cas 1808913-24-7 MF C20 H22 Cl2 F3 N5 O MW 476.32 Urea, N‘-[(1R)-1-[2,3-dichloro-4-(2-pyrazinyl)phenyl]-2,2,2-trifluoroethyl]-N-methyl-N-(1-methyl-4-piperidinyl)- (R)-3-(1-(2,3-dichloro-4-(pyrazin-2-yl)phenyl)-2,2,2-trifluoroethyl)-1-methyl-1-(1-methylpiperidin-4-yl) urea The compound was disclosed in WO2015134839 . Helsinn under license from Novo Nordisk , is investigating ghrelin antagonists for treating obesity, Prader-Willi syndrome and other metabolic disorders; in May 2015, the program was listed as being in 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 = …