Amgen Inc.

Eisai R&d Management Co., Ltd.

Biovitrum Ab

George Moniz

Matthew J Frizzle

Christopher Michael Tegley

Qingyian Liu

Christopher Harold Fotsch

Guolin Cai

Chester Chenguang Yuan

Qi Huang

Michael D Bartberger

Nianhe Han

Randall W Hungate

Aiwen Li

David Joseph St Jean, Jr

Lars Johansson

Evert Homan

Meredith Williams

Martin Henriksson

Eric A Bercot

Toshiaki Tanaka

Michael J Martinelli

Arani Chanda

Kristen Sanders

Charles Bernard

Jay Larrow

Farid Benayoud

Kenshi Yoshida

Keiichi Sorimachi

Margaret M Faul

Annie Zhu Wilcoxen

John JianShi Wang

Ming-Hong Hao

Dominic J Reynolds

Sudeep Prajapati

Takashi Satoh

Taro Terauchi

Huiming Zhang

Jaemoon Lee

Yu Yoshida

Anand Selvaraj

Yoshimitsu Naoe

Yuji Kazuta

Karl Bennett Hansen

Teresa L Marshall

Ayumi Takemura

Roger Nani

Liane Klingensmith

A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-y1)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.

Crystalline FGFR4 inhibitor compound and uses thereof

A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.

The present disclosure provides compounds and methods that are useful for the preparation of compounds useful as orexin-2 receptor antagonists.

Methods and compounds useful in the synthesis of orexin-2 receptor antagonists

The present invention relates to compounds with the formula (I), (II), (III) or (IV): 

Inhibitors of 11-&#x3b2;-hydroxy steroid dehydrogenase type 1

The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-&#x3b2;-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-&#x3b2;-hydroxysteroid dehydrogenase type 1 enzyme.

Inhibitors of 11-beta-hydroxysteroid dehydrogenase type 1

The present invention relates to methods of making compounds that inhibit 11-hydroxysteroid dehydrogenase type 1 enzyme (11-HSD1). One method comprises (a) contacting a compound of formula (II) sequentially with a chiral base in the presence of an amine, and an alkylating agent R3-LG, (b) contacting the product of (a) with an acid to form a salt, and (c) reacting the salt with a base to form the compound of formula (I), wherein Z, R1, R2, and R3 are defined herein.

Process for making substituted 2-amino-thiazolones

The present invention relates to methods of making compounds that inhibit 11-&#x3b2;-hydroxysteroid dehydrogenase type 1 enzyme (11-&#x3b2; HSD1). One method comprises (a) contacting a compound of formula (II) with a chiral base, deprotonating agent, and an alkylating agent R-LG, (b) contacting the product of (a) with an acid to form a salt, and (c) reacting the salt with a base to form the compound of formula (I); wherein Z, R, R, and Rare defined herein. 

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Cambridge, MA, United States of America

George Moniz