Merck + Co., Inc.

Bristol-myers Squibb Compnay

Solvias Ag

Thorsten Rosner

Yi Xiao

Yongkui Sun

Nelo R Rivera

Joseph D Armstrong, Iii

Shane W Krska

Lopa V Desai

Benjamin Cohen

Felix Spindler

Guanglin Luo

Ronald L Hanson

Martin D Eastgate

Qi Gao

Gregory L Beutner

Michael Shawn Lawler

Bin Zheng

David Kenneth Leahy

Nicolas Cuniere

Christopher S Regens

Yu Fan

Neil A Strotman

Paul C Lobben

Carolyn S Wei

Keming Zhu

Michael Bryan Hay

Andrew M Clausen

Christophe Malan

Eugenia Njolito

Monica Fitzgerald

The invention relates to an improved process for synthesizing N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide of the formula: (I) Compound (I) is currently in clinical trials for the treatment of myeloproliferative disorders, such as polycythaemia vera, thrombocythaemia and primary myelofibrosis. 

Process for the preparation of N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide

The disclosure generally relates to the novel compounds of formula I, including their 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). 

CGRP receptor antagonists

The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.

Process for the preparation of enantiomerically enriched beta amino acid derivatives

The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.

Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation

Iodohydroxylated olefins can be prepared by treating an olefin with an aqueous solution of an iodine monohalide selected from iodine monochloride and iodine monobromide.

Iodohydroxylation of olefins

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Berkeley Heights, NJ, United States of America

Thorsten Rosner