99197-79-2

Upstream product

• 99197-78-1 (S)-2-((tert-butoxycarbonyl)amino)-3-(2-nitrophenoxy)propanoic acid 
• 3262-72-4 (S)-N-(tert-butoxycarbonyl)serine 
• 1493-27-2 ortho-nitrofluorobenzene 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 1562199-65-8 (S)-tert-butyl 5-((6-bromo-1-(2-cyanophenyl)-1H-indazol-3-yl)methyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-ylcarbamate 
• 1562199-11-4 (S)-N-((S)-5-((2-cyano-1-(2-cyanophenyl)-1H-indol-3-yl)methyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-2-(methylamino)propanamide trifluoroacetate 
• 1562199-15-8 tert-butyl (S)-1-((S)-5-((2-cyano-1-(2-cyanophenyl)-1H-indol-3-yl)methyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-ylamino)-1-oxopropan-2-yl(methyl)carbamate 
• 1562198-75-7 tert-butyl (S)-1-((S)-5-((2-chloro-1-(phenylsulfonyl)-1H-indol-3-yl)methyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-ylamino)-1-oxopropan-2-yl(methyl)carbamate 
• 1562198-63-3 (S)-N-((S)-5-((2-chloro-1-(2-cyanophenyl)-1H-indol-3-yl)methyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-2-(methylamino)propanamide 
• 1562198-66-6 tert-butyl (S)-1-((S)-5-((2-chloro-1-(2-cyanophenyl)-1H-indol-3-yl)methyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-ylamino)-1-oxopropan-2-yl(methyl)carbamate 
• 1562197-79-8 (S)-N-((S)-5-(2-chlorobenzyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-2-(methylamino)propanamide 
• 1562197-81-2 tert-butyl (S)-1-((S)-5-(2-chlorobenzyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-ylamino)-1-oxopropan-2-yl(methyl)carbamate 
• 99198-11-5 tert-butyl 3(S)-[1(S)-ethoxycarbonyl-3-cyclohexylpropyl]amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-5-acetate 
• 99228-14-5 tert-butyl 3(S)-[1(R)-ethoxycarbonyl-3-cyclohexylpropyl]amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-5-acetate 
• 99198-15-9 (S)-2-((S)-9-Carboxymethyl-8-oxo-6,7,8,9-tetrahydro-5-oxa-9-aza-benzocyclohepten-7-ylamino)-4-cyclohexyl-butyric acid benzyl ester; hydrochloride 
• 99198-16-0 (S)-2-((S)-9-Carboxymethyl-8-oxo-6,7,8,9-tetrahydro-5-oxa-9-aza-benzocyclohepten-7-ylamino)-4-cyclohexyl-butyric acid ethoxycarbonylmethyl ester; hydrochloride 
• 99198-17-1 (S)-2-((S)-9-Carboxymethyl-8-oxo-6,7,8,9-tetrahydro-5-oxa-9-aza-benzocyclohepten-7-ylamino)-4-cyclohexyl-butyric acid butyl ester; hydrochloride 
• 97871-02-8 benzyl 2-[(3S)-3-amino-4-oxo-2,3,4,5-tetrahydro-5H-1,5-benzoxazepin-5-yl]-ethanoate hydrochloride 

Relevant academic research and scientific papers

Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer

RIP1 regulates cell death and inflammation and is believed to play an important role in contributing to a variety of human pathologies, including immune-mediated inflammatory diseases and cancer. While small-molecule inhibitors of RIP1 kinase have been ad

Structure-based bioisosterism design of thio-benzoxazepinones as novel necroptosis inhibitors

Necroptosis is reported to play a critical role in contributing to a variety of human pathologies. The benzoxazepinone GSK′772 is a potent necroptosis inhibitor optimized using a hit from a DNA-encoded library, which is currently in phase II clinical tria

Thio-seven-membered ring derivative and application thereof

The invention discloses a thio-seven-membered ring derivative or a pharmaceutical salt, a solvate, a stereoisomer and a racemate thereof. The structure of the thio-seven-membered ring derivative is shown as a general formula I, wherein the definition of e

FUSED RING HETEROARYL COMPOUNDS AS RIPK1 INHIBITORS

The invention provides novel substituted heterocyclic compounds represented by Formula I, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided c

benzo[b][1,4]oxazepin derivatives and pharmaceutical composition for use in preventing or treating kinase-related disease

The present invention relates to a benzo[b][1,4]oxazepine derivative represented by the following chemical formula 1, and a pharmaceutical composition for treating kinase-related diseases including the same as an active ingredient. The benzo[b][1,4]oxazep

3-substituted-1,5-benzodiazepine compound and pharmaceutical application thereof

The invention belongs to the technical field of medicine, and relates to a 3-substituted-1,5-benzodiazepine compound with a general molecular formula of a formula I and application of the 3-substituted-1,5-benzodiazepine compound to medicine. The 3-substituted-1,5-benzodiazepine compound can selectively inhibit the activity of glycogen synthase kinase-3beta (GSK 3beta) and can be used for the preparation of the medicine for preventing and/or treating diseases with abnormal pathological characteristics of the GSK 3beta, wherein the diseases includes cancer, neurological diseases, metabolic syndromes and the like. (Please see the specification for the formula.)

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases

RIP1 regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including immune-mediated inflammatory diseases. Small-molecule inhibitors of RIP1 kinase that are suitable for advancement into

SUBSTITUTED HETERO-AZEPINONES

There are provided compounds of the formula (1) wherein W, X, Y, Z, R1, R2, R3, R4, R5 and R6 are described herein. These compounds are useful for the treatment of proliferative diseases, including cancer.

HETEROCYCLIC AMIDES AS KINASE INHIBITORS

Disclosed are compounds having the formula (I) wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.

Benzazepinones and benzoxazepinones as antagonists of inhibitor of apoptosis proteins (IAPs) selective for the second baculovirus iap repeat (BIR2) domain

XIAP is a key regulator of apoptosis, and its overexpression in cancer cells may contribute to their survival. The antiapoptotic function of XIAP derives from its BIR domains, which bind to and inhibit pro-apoptotic caspases. Most known IAP inhibitors are selective for the BIR3 domain and bind to cIAP1 and cIAP2 as well as XIAP. Pathways activated upon cIAP binding contribute to the function of these compounds. Inhibitors selective for XIAP should exert pro-apoptotic effects through competition with the terminal caspases. This paper details our synthetic explorations of a novel XIAP BIR2-selective benzazepinone screening hit with a focus on increasing BIR2 potency and overcoming high in vivo clearance. These efforts led to the discovery of benzoxazepinone 40, a potent BIR2-selective inhibitor with good in vivo pharmacokinetic properties which potentiates apoptotic signaling in a manner mechanistically distinct from that of known pan-IAP inhibitors.