Category «Preclinical»

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 …

SEN 826

It’s only fair to share… SEN 826 CAS 1160833-51-1 C25 H31 N5 O, 417.55 Methanone, [1-[3-(1-methyl-1H-benzimidazol-2-yl)phenyl]-4-piperidinyl](4-methyl-1-piperazinyl)- CAS HBr SALT 1612250-71-1 WO2009074300 product patent Russell John Thomas, Mohr Gal.La Pericot, Giacomo Minetto, Annette Cornelia Bekker, Pietro Ferruzzi,  Applicant Siena Biotech S.P.A. Siena Biotech S.p.A. operates as a drug discovery and development company which develops a portfolio of …

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 …

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. …