1403902-55-5

Upstream product

• 1403898-64-5 (2R,5R)-5-(hydroxymethyl)-2-methylpiperazine-1-carboxylic acid tert-butyl ester 
• 1403901-32-5 (2R,5R)-4-benzyl-5-hydroxymethyl-2-methyl-piperazine-1-carboxylic acid tert-butyl ester 
• 1403898-63-4 ((2R,5R)-5-methyl-piperazin-2-yl)-methanol hydrochloride 
• 124-63-0 methanesulfonyl chloride 
• 100-52-7 benzaldehyde 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1403898-62-3 (3S,6R)-3-(hydroxymethyl)-6-methylpiperazine-2,5-dione 

Downstream Products

• 1605312-01-3 (2R,5S)-5-(4,4-dimethyl-2-oxo-pyrrolidin-1-ylmethyl)-4-{2-[6-(4-fluorobenzyl)-3,3-dimethyl-2,3-dihydro-pyrrol[3,2-b]pyridin-1-yl]-2-oxo-ethyl}-2-methyl-piperazine-1-carboxylic acid tert-butyl ester 
• 1605311-65-6 (2R,5S)-4-benzyl-2-methyl-5-(4-methyl-2-oxo-pyrrolidin-1-ylmethyl)piperazine-1-carboxylic acid tert-butyl ester 
• 1605312-12-6 (2R,5S)-4-{2-[6-(4-fluoro-benzyl)-3,3-dimethyl-2,3-dihydro-pyrrolo[3,2-b]pyridin-1-yl]-2-oxo-ethyl}-2-methyl-5-((R)-2-methyl-5-oxo-morpholin-4-ylmethyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 1605312-09-1 (2R,5S)-4-{2-[6-(4-fluoro-benzyl)-3,3-dimethyl-2,3-dihydro-pyrrolo[3,2-b]pyridin-1-yl]-2-oxo-ethyl}-2-methyl-5-(1-oxo-1,3-dihydro-isoindol-2-ylmethyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 1605312-38-6 (2R,5S)-4-{2-[3-(4-fluoro-benzyl)-7,7-dimethyl-6,7-dihydro-pyrrolo[3,2-c]pyridazin-5-yl]-2-oxo-ethyl}-2-methyl-5-(1-oxo-1,3-dihydro-isoindol-2-ylmethyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 1605312-50-2 (2R,5S)-4-{2-[3-(2,4-difluoro-benzyl)-7,7-dimethyl-6,7-dihydro-pyrrolo[3,2-c]pyridazin-5-yl]-2-oxo-ethyl}-2-methyl-5-(1-oxo-1,3-dihydro-isoindol-2-ylmethyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 1605312-67-1 (2R,5S)-4-{2-[3-(2,4-difluoro-benzyl)-7,7-dimethyl-6,7-dihydro-pyrrolo[3,2-c]pyridazin-5-yl]-2-oxo-ethyl}-5-(4-fluoro-1-oxo-1,3-dihydro-isoindol-2-ylmethyl)-2-methyl-piperazine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

PYRIDO[2,3-B] [1,4] OXAZINES OR TETRAHYDROPYRIDO[2,3-B][1,4] OXAZEPINES AS IAP ANTAGONISTS

Disclosed herein are novel 2,3-dihydro-1H-pyrido[2,3-b][1,4] oxazine or 1,2,3,4-tetrahydropyrido[2,3-b][1,4]oxazepine derivatives used as antagonists of IAPs (Inhibitors Apoptosis Proteins), also known as Smac mimetics. Disclosed herein is the use of these antagonists for inducing or sensitizing cells to the induction of apoptotic cell death, and the use of such compounds for treating proliferative disease such as cancer.

IAP ANTAGONIST COMPOUNDS AND INTERMEDIATES AND METHODS FOR SYNTHESIZING THE SAME

A compound of formula (XXIII) and methods for preparation thereof are provided (XXIII).

Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP)

XIAP and cIAP1 are members of the inhibitor of apoptosis protein (IAP) family and are key regulators of anti-apoptotic and pro-survival signaling pathways. Overexpression of IAPs occurs in various cancers and has been associated with tumor progression and resistance to treatment. Structure-based drug design (SBDD) guided by structural information from X-ray crystallography, computational studies, and NMR solution conformational analysis was successfully applied to a fragment-derived lead resulting in AT-IAP, a potent, orally bioavailable, dual antagonist of XIAP and cIAP1 and a structurally novel chemical probe for IAP biology.

BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY

The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY

The invention relates to new bicyclic heterocycle compounds of formula (I): wherein R1 is seected from specific pyrazolyl, imidazolyl, pridinyl and triazolyl groups. The invention also realtes to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY

The invention relates to new bicyclic heterocycle compounds of formula (I): (Formula (I)), pharmaceutical compositions comprising said compounds and to use of said compounds in the treatment of diseases, e.g. cancer.

BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY

The invention relates to new bicyclic heterocycle compounds of formula (I):,to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.