Tag «PRECLINICAL»

Astellas Pharma Inc. new Glucokinase Activator, ASP ? for Type 2 Diabetes

It’s only fair to share…   ASP ? (2R)-2-(4-cyclopropanesulfonyl-3-cyclopropylphenyl)-N-[5-(hydroxymethyl)pyrazin-2-yl]-3-[(R)-3-oxocyclopentyl]propanamide CAS 1174229-89-0 MW C25 H29 N3 O5 S Benzeneacetamide, 3-cyclopropyl-4-(cyclopropylsulfonyl)-N-[5-(hydroxymethyl)-2-pyrazinyl]-α-[[(1R)-3-oxocyclopentyl]methyl]-, (αR)- Molecular Weight, 483.58 [α]D20 −128.7 (c 1.00, MeOH); 1H NMR (DMSO-d6, 400 MHz) δ 11.07 (s, 1H), 9.20 (d, J = 1.4 Hz, 1H), 8.41 (d, J = 1.4 Hz, 1H), 7.79 (d, J = 8.2 …

AMG-3969

It’s only fair to share… AMG-3969 M.Wt: 522.46 Cas : 1361224-53-4 , MF: C21H20F6N4O3S WO 2012027261 PRODUCT PATENT Inventors Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, Jean …

BMS-960

It’s only fair to share… BMS-960 PRECLINICAL (S)-1-((S)-2-Hydroxy-2-(4-(5-(3-phenyl-4-(trifluoromethyl)isoxazol-5-yl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)piperidine-3-carboxylic Acid 3-Piperidinecarboxylic acid, 1-[(2S)-2-hydroxy-2-[4-[5-[3-phenyl-4-(trifluoromethyl)-5-isoxazolyl]-1,2,4-oxadiazol-3-yl]phenyl]ethyl]-, (3S)- (S)-1-((S)-2-Hydroxy-2-(4-(5-(3-phenyl-4-(trifluoromethyl)isoxazol-5-yl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)piperidine-3-carboxylic Acid CAS 1265321-86-5 FREE FORM FREE FORM 528.48, C26 H23 F3 N4 O5 CAS 1265323-40-7 HCL SALT BASIC PATENT WO201117578, 2011, (US Patent 8399451) Inventors John L. Gilmore, James E. Sheppeck Applicant Bristol-Myers Squibb Company   Sphingosine-1-phosphate (S1P) is the endogenous ligand for the …

DNDI-VL-2098

It’s only fair to share… DNDI-VL-2098 CAS 681492-17-1 (R)-2-Methyl-6-nitro-2-(4-trifluoromethoxyphenoxymethyl)-2,3-dihydroimidazo[2,1-b]oxazole Watch this post, will be updated……….. MF C14 H12 F3 N3 O5, MW 359.26 Imidazo[2,1-b]oxazole, 2,3-dihydro-2-methyl-6-nitro-2-[[4-(trifluoromethoxy)phenoxy]methyl]-, (2R)- Hidetsugu Tsubouchi, Hirofumi Sasaki, Hideaki Kuroda, Motohiro Itotani, Takeshi Hasegawa, Yoshikazu Haraguchi, Takeshi Kuroda, Takayuki Matsuzaki, Kuninori Tai, Makoto Komatsu, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Yuji Seike, Masanori Kawasaki, …

CEP 33779

It’s only fair to share… CEP-33779, CEP33779 CAS 1257704-57-6 Chemical Formula: C24H26N6O2S Molecular Weight: 462.57 Elemental Analysis: C, 62.32; H, 5.67; N, 18.17; O, 6.92; S, 6.93 N-(3-(4-methylpiperazin-1-yl)phenyl)-8-(4-(methylsulfonyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine PRECLINICAL Treatment of Rheumatoid Arthritis, Agents for Colorectal Cancer Therapy Systemic Lupus Erythematosus, Jak2 Inhibitors Matthew A. Curry, Bruce D. Dorsey, Benjamin J. Dugan, Diane E. Gingrich, Eugen F. Mesaros, Karen L. …

Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain from Lilly Research Laboratories

It’s only fair to share… 2-(2-(1H-1,2,3-triazol-5-yl)ethoxy)-1-(2-((2,3-dihydro-1H-inden-2-yl)amino)-5,7-dihydro-6Hpyrrolo[3,4-d]pyrimidin-6-yl)ethan-1-one l-[2-(2,3-dihydro- lH-inden-2-ylamino)-5,7-dihydro-6H-pyrrolo[3,4- d]pyrimidin-6-yl]-2-[2-(lH- l ,2,3-triazol-4-yl)ethoxy]ethanone. CAS 1619971-30-0 1-[2-(2,3-dihydro-1H-inden-2-ylamino)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidin-6-yl]-2-[2-(1H-1,2,3-triazol-4-yl)ethoxy]ethanone; Molecular Formula: C21H23N7O2 Molecular Weight: 405.45302 g/mol US2014200231 Scheme A     Scheme B   Scheme C VI   Scheme E Autotaxin is an enzyme reported to be the source of lysophosphatidic acid (LPA) which up-regulates pain-related proteins through one if its …

JNJ 54166060

It’s only fair to share… JNJ 54166060 JNJ-54166060; JNJ 54166060; JNJ54166060. (R)-(2-chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl)methanone [2-chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanone Methanone, [2-chloro-3-(trifluoromethyl)phenyl][(4R)-1-(5-fluoro-2-pyridinyl)-1,4,6,7-tetrahydro-4-methyl-5H-imidazo[4,5-c]pyridin-5-yl]- CAS 1627900-41-7 OF R ISOMER  DESIRED CAS 1627900-42-8 OF S ISOMER Chemical Formula: C20H15ClF4N4O Exact Mass: 438.0871 JNJ-54166060 is a potent P2X7 antagonist. Bioactivity data of JNJ-54166060: rP2X7 IC50=4 nM; rP2X7 IC50=115nM; HLM/RLM = 0.35/0.64, ED50 = 2.3 mg/kg in rats. JNJ-54166060 …

(3S)-3-[(2-amino-5-methoxypyrimidin-4-yl)amino]heptan-1-ol for the treatment of viral infections

It’s only fair to share… (3S)-3-[(2-amino-5-methoxypyrimidin-4-yl)amino]heptan-1-ol cas  1402802-45-2 JNJ ? WO 2012136834, WO 2014053595 for the treatment of viral infections Molecular Formula: C12H22N4O2 Molecular Weight: 254.32868 g/mol Inventors Gowan David Mc, Pierre Jean-Marie Bernard Raboisson, Werner Embrechts, Tim Hugo Maria Jonckers, Stefaan Julien Last, Serge Maria Aloysius Pieters, Jaromir Vlach,  Applicant Janssen R&D Ireland   (3S)-3-[(2-amino-5-methoxypyrimidin-4-yl)amino]heptan-1-ol Mark Hicken, …

DDD 107498

It’s only fair to share… DDD 107498, DDD 498 PATENT WO 2013153357,  US2015045354 6-Fluoro-2-[4-(morpholinomethyl)phenyl]-N-(2-pyrrolidin-1-ylethyl)quinoline-4-carboxamide 6-Fluoro-2-[4-(4-morpholinylmethyl)phenyl]-N-[2-(1-pyrrolidinyl)ethyl]-4-quinolinecarboxamide 4-Quinolinecarboxamide, 6-fluoro-2-[4-(4-morpholinylmethyl)phenyl]-N-[2-(1-pyrrolidinyl)ethyl]- CAS 1469439-69-7 CAS 1469439-71-1 SUCCINATE MF C27H31FN4O2 MW 462.559043 g/mol 6-fluoro-2-[4-(morpholin-4-ylmethyl)phenyl]-N-(2-pyrrolidin-1-ylethyl)quinoline-4-carboxamide Originator Medicines for Malaria Venture; University of Dundee Class Small molecules Mechanism of Action Protein synthesis inhibitors Highest Development Phases No development reported Malaria Most Recent Events 16 Jul 2016 No recent reports of development identified for …

PF-04745637

It’s only fair to share…   PF-04745637 cas 1917294-46-2 MW 509.00, MF C27 H32 Cl F3 N2 O2 Cyclopentanecarboxamide, 1-(4-chlorophenyl)-N-[2-[4-hydroxy-4-(trifluoromethyl)-1-piperidinyl]-3-phenylpropyl]- rac-1-(4-Chlorophenyl)-N-f2-r4-hvdroxy-4-(trifluoromethyl)piperidin-1-vn-3-phenylpropyDcyclopentanecarboxamide PRODUCT PATENT WO-2016067143-A1 Applicants: PFIZER INC. [US/US]; 235 East 42nd Street New York, New York 10017 (US) Inventors: SWAIN, Nigel Alan; (GB). PRYDE, David Cameron; (GB). RAWSON, David James; (GB). RYCKMANS, Thomas; (GB). SKERRATT, Sarah Elizabeth; (GB). …