Novartis Ag

Rhone-Poulenc Rorer Pharmaceuticals Inc.

Lexicon Pharmaceuticals, Inc.

Ciba-Geigy Corporation

Bristol-Myers Squibb Compnay

Novartis Corporation

Cynthia Anne Fink

Alfred P Spada

Michael R Myers

Fariborz Firooznia

John E Macor

Joanne J Bronson

Yulian Zhang

Carolyn Diane Dzierba

Yingzhi Bi

Michael Alan Green

Joseph Barbosa

Li Dong

St&eacute;phane De Lombaert

Jiancheng Wang

Arco Yingcheu Jeng

David Kimball

Soojin Kwon

Greg Zipp

Denton Wade Hoyer

Kenneth Gordon Carson

Gary Michael Ksander

Spencer David Kimball

Mahavir Prashad

Zhi-Cai Shi

Giovanni Cianchetta

Hartmuth C Kolb

Ashok R Tunoori

Benoit J Vanasse

Paivi Jaana Kukkola

Laurence W Reilly

Faribroz Firooznia

G Gregory Zipp

Eli M Wallace

Michael Green

This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.

Multicyclic compounds and methods of their use

The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.

Modulators of G protein-coupled receptor 88

This invention concerns novel thiazolopyrazole compounds and compositions comprising them. Methods of using these compounds for the treatment, prevention and management of various diseases and disorders are also encompassed by the invention.

Thiazolopyrazoles and methods of their use

Compounds of the formula (I), wherein R, R&#x2013;Rand alk have meaning as defined, pharmaceutical compositions thereof, and use thereof for the treatment and/or prevention of cardiovascular disorders responsive to ACE and NEP inhibition and/or ECE inhibition. 

Pyrane derivatives as both ACE-and NEP-inhibitors

Compounds of the formulawherein R, R, COOR, R&#x2013;R, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.

Dipeptide derivatives

Certain heteroaryl substituted thiol inhibitors of endothelin-converting enzyme

Certain thiol inhibitors of endothelin-converting enzyme

Certain cyclic thio substituted acylaminoacid amide derivatives

Amino-benzocycloalkane derivatives

Disclosed are compound of formula I wherein

Compounds of the Formula ##STR1## wherein: K is N or N.fwdarw.O; Q is CH.sub.2 or O; T is ##STR2## or R.sub.3 O--CH.sub.2 ; X is a straight or branched chain alkylene, cycloalkylene or cycloalkenylene group, each of which is optionally substituted by at least one CH.sub.3, CH.sub.3 CH.sub.2, Cl, F, CF.sub.3 or CH.sub.3 O; Y is NR.sub.4, O or S; a=0 or 1; Z is of the formula ##STR3## Z.sub.1 is N, CR.sub.5, (CH).sub.m --CR.sub.5 or (CH).sub.m --N, m being 1 or 2; Z.sub.2 is N, NR.sub.6, O or S, n being 0 or 1; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H, alkyl, aryl or heterocyclyl; R.sub.a and R.sub.b are independently H, OH, alkyl, hydroxyalkyl, alkyl mercaptyl, thioalkyl, alkoxy, alkyoxyalkyl, amino, alkyl amino, carboxyl, acyl, halogen, carbamoyl, alkyl carbamoyl, aryl or heterocyclyl; and R' and R' are independently hydrogen, alkyl, aralkyl, carbamoyl, alkyl carbamoyl, dialkylcarbamoyl, acyl, alkoxycarbonyl, aralkoxycarbonyl, aryloxycarbonyl, or R' and R' together may form ##STR4## where R.sub.c is hydrogen or alkyl, ##STR5## where R.sub.d and R.sub.e are independently hydrogen, alkyl, or together with the carbon atom to which they are attached may form a 1,1-cycloalkyl group; provided that when X is straight chain alkylene and Q is oxygen, then Z represents a heterocyclyl including at least two heteroatoms, which are adenosine agonists useful as antihypertensive, cardioprotective, antiischemic, and antilipolytic agents, pharmaceutical compositions including such compounds, and their use in treating hypertension, myocardial ischemia, ameliorating ischemic injury and myocardial infarct size consequent to myocardial ischemia, hyperlipidemia and hypercholesterolemia are claimed.

Compounds having antihypertensive, cardioprotective, anti-ischemic and

Growing community of inventors

Lebanon, NJ, United States of America

Cynthia Anne Fink