Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Jiafang He

Scott D Edmondson

Weiguo Liu

Zhuyan Guo

Santhosh Francis Neelamkavil

Eric Mertz

Lihu Yang

Amjad Ali

Sung-Sau So

Ying-Duo Gao

Alan W Hruza

Anthony K Ogawa

Gui-Bai Liang

Yi Zang

Rudrajit Mal

Mark D Erion

Ashok Arasappan

Jason M Cox

Songnian Lin

John S Debenham

Shawn P Walsh

Derun Li

Rongze Kuang

Subharekha Raghavan

Dongfang Meng

Wanying Sun

Heping Wu

Sriram Tyagarajan

Zhong Lai

Ning Shao

Zahid Hussain

Ellen K Vande Bunte

Min Ge

Fiona Wai Yu Lau

John Bawiec

Andrew F Nolting

Santosh Neelamkavil

The present invention is directed to pyrazolopyrimidine compounds of the general structural formula I: which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Substituted pyrazolo[3,4-d]pyrimidines as PDE9 inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Factor XIa inhibitors

The present invention provides a compound of Formula (I); and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 

The present invention provides a compound of Formula (I) (Formula (I)) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes.

Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.

Substituted bicyclic amines for the treatment of diabetes

Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Antidiabetic bicyclic compounds

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Dayton, NJ, United States of America

Jiafang He