Opko Health, Inc.

Merck Sharp + Dohme Corp.

Schering Corporation

Scherig Corporation

Ahmed Samatar

Alan Cooper

Sunil Paliwal

Jagdish Desai

Hugh Zhu

Joseph Kelly

Hon-chung Tsui

Yiji Wu

M. Arshad Siddiqui

Alan Hruza

Azim A. Celebi

Hon-Chung Tsui

Neng-Yang Shih

Dong Xiao

Cheng Wang

Anandan Palani

Michelle Laci Wrobleski

Gregory A Reichard

Xianhai Huang

Ashwin Umesh Rao

Sapna S Shah

Ingrid Mergelsberg

Ronald J Doll

Alan B Cooper

Gerald Wayne Shipps, Jr

Yongqi Deng

Xiaolei Gao

Jagdish A Desai

Sobhana Babu Boga

Ahmed Abdi Samatar

James J-s Wang

Hugh Y Zhu

Liang Zhu

Brian Alexander McKittrick

M Arshad Siddiqui

Vincent Stewart Madison

Joseph Michael Kelly

Alan W Hruza

Li Xiao

Thierry Olivier Fischmann

Xiao Chen

Angela Dawn Kerekes

Robert Sun

Mehul F Patel

Gerald W Shipps

Juan D Arredondo

Dominik Hermann Scherer

Monika Erika Huttenloch

Yang Nan

Abdul-Basit Alhassan

Tong Wang

Mary Ann Caplen

Hyunjin M Kim

Youhao Dong

Azim Alan Celebi

Matthew Rainka

Sara Esposite

Xin Yao

Ang Li

Subrahmanyam Gudipati

Sapna Majmundar Shah

Azim A Celebi

Ronald Doll

Jr Shipps Gerald W

Vincent S Madison

James Wang

James J-S Wang

This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1,7-diazaspiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid.

Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds

A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NKreceptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.

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A NKantagonist having the formula (I), wherein Arand Arare optionally substituted phenyl or heteroaryl, Xis an ether, thio or imino linkage, Rand Rare not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.

This application discloses a process to synthesize 8-({1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy)-methyl]-8-pheny-1.7-diaza-spiro[4.5]decan-2-one comprising reacting a compound of the Formula 27a-sulfonate with zinc in the presence of acetic acid. 

NK1 antagonists

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydropyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0. 

Compounds that are ERK inhibitors

The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R, R, R, and Rare as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway. 

N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1

This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations.

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

A compound having the general structure shown in Formula I: or pharmaceutically acceptable salt and/or solvates thereof are useful in treating diseases or conditions mediated by NKreceptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.

Growing community of inventors

East Brunswick, NJ, United States of America

Hon-Chung Tsui