1289023-67-1

Basic information

• Product Name: BMS 927711
• Synonyms: BMS 927711;BMS-927711;4-(2,3-Dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-1-yl)-1-piperidinecarboxylic acid (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl ester;Rimegepant;(5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate;1-Piperidinecarboxylic acid, 4-(2,3-dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-1-yl)-, (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl ester
• CAS NO: 1289023-67-1
• Molecular Formula: C₂₈H₂₈F₂N₆O₃
• Molecular Weight: 534.5571264
• Mol File: 1289023-67-1.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• Density: 1.45±0.1 g/cm3(Predicted)
• Solubility: Soluble in DMSO
• PKA: 12.03±0.20(Predicted)
• CAS DataBase Reference: BMS 927711(CAS DataBase Reference)
• NIST Chemistry Reference: BMS 927711(1289023-67-1)
• EPA Substance Registry System: BMS 927711(1289023-67-1)

Safety Data

• Hazardous Substances Data: 1289023-67-1(Hazardous Substances Data)

Usage

Description

BMS 927711 is a drug compound that is currently in development for the treatment of various medical conditions. It is a selective antagonist of the human 5-HT1F receptor, which plays a role in the modulation of migraine headaches. BMS 927711 has demonstrated efficacy in clinical trials for the acute treatment of migraine with or without aura in adults.

Uses

Used in Pharmaceutical Industry:
BMS 927711 is used as a drug compound for the acute treatment of migraine with or without aura in adults. It works by selectively blocking the human 5-HT1F receptor, which helps to alleviate migraine symptoms.
Used in Migraine Treatment:
BMS 927711 is used as a migraine treatment for providing relief from pain and the most bothersome symptoms associated with migraine attacks. In clinical trials, a single dose of BMS 927711 has shown superiority over placebo in achieving freedom from pain and freedom from the most bothersome symptom at 2 hours post-dose.

Upstream product

• 1190363-50-8 (5S,6S,9R)-6-(2,3-difluorophenyl)-9-(triisopropylsilyloxy)-6,7,8,9-tetrahydro-5H-cyclohepta[b]-pyridin-5-ol 
• 1289024-04-9 (5R,6S,9R)-5-chloro-6-(2,3-difluorophenyl)-9-(triisopropylsilyloxy)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridine 
• 1289024-05-0 (5S,6S,9R)-5-azido-6-(2,3-difluorophenyl)-9-(triisopropylsilyloxy)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridine 
• 1289024-06-1 (5S,6S,9R)-5-azido-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-ol 
• 1289023-63-7 (5S,6S,9R)-5-azido-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo-[4,5-b]pyridin-1-yl)piperidine-1-carboxylate 
• 1190363-46-2 (6S,9R)-6-(2,3-difluorophenyl)-9-((triisopropylsilyl)oxy)-6,7,8,9-tetrahydro-5Hcyclohepta[b]pyridin-5-one 

Downstream Products

• 1289023-77-3 (5S,6S,9R)-6-(2,3-difluorophenyl)-5-(dimethylamino)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate 
• 1289023-74-0 (5S,6S,9R)-6-(2,3-difluorophenyl)-5-(methylamino)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate 

Relevant articles and documents

Solid form of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione having specified X-ray diffraction pattern

The invention relates to a packaging comprising one or more administration units comprising a solid form of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione.

Discovery of (5S,6S,9R)-5-aqmino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro- 5H-cyclohepta[b]pyridin-9-yl4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl) piperidine-1-carboxylate (BMS-927711): An oral Calcitonin Gene-Related Peptide (CGRP) antagonist in cinical trials for treating migraine

Calcitonin gene-related peptide (CGRP) receptor antagonists have demonstrated clinical efficacy in the treatment of acute migraine. Herein, we describe the design, synthesis, and preclinical characterization of a highly potent, oral CGRP receptor antagonist BMS-927711 (8). Compound 8 has good oral bioavailability in rat and cynomolgus monkey, attractive overall preclinical properties, and shows dose-dependent activity in a primate model of CGRP-induced facial blood flow. Compound 8 is presently in phase II clinical trials.

CGRP RECEPTOR ANTAGONISTS

The disclosure generally relates to the novel compounds of formula (I), including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).