Tag «PRECLINICAL»

BMS-986169

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 GluN2B subunit allosteric modulatory …

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Debio-1452

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 SA, Melioidosis, Enoyl ACP reductase Fabl …

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

  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 Hz, 1H), 7.41 (dd, J …

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AMG-3969

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 David Joseph St., Jr., Nuria …

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BMS-960

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 sphingosine-1-phophate receptors (S1P1–5) and triggers …

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DNDI-VL-2098

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, Takumi Sumida, Shin Miyamura,  Applicant …

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CEP 33779

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. Milkiewicz, Applicant Cephalon, Inc. Worldwide …

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

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 cognate receptors, LPAi. LPA is …

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JNJ 54166060

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 shows high oral bioavailability and …

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