Bristol-myers Squibb Compnay

Dupont Pharmaceuticals Company

The Dupont Merck Pharmaceutical Company

Bristol-myers Squibb Pharma Company

Dupont Pharmaceuticals, Inc.

Donald J Pinto

Richard Eric Olson

Yun-Long Li

William R Ewing

Mimi Lifen Quan

Jennifer X Qiao

James Russell Pruitt

Douglas G Batt

Michael J Orwat

John Matthew Fevig

John Wityak

Joanne M Smallheer

Wei Han

Joseph J Petraitis

Shaker Ahmed Mousa

Chu-Biao Xue

William John Pitts

Gary Avonn Cain

Patrick Y Lam

William Frank Degrado

Shuaige Wang

Thais Motria Sielecki-Dzurdz

James R Corte

Wu Yang

Paul Joseph Gilligan

Robert A Galemmo, Jr

Zilun Hu

Qi Han

Celia Dominguez

Munir A Hussain

Petrus Fredericus Stouten

Carl P Decicco

Yufeng Wang

Karen Anita Rossi

Ruth Richmond Wexler

Yoon T Jeon

Tianan Fang

Charles G Clark

Amy Han

Patrick Y S Lam

Timur Gungor

Joseph Cacciola

Renhua Li

Sarah R Friedrich

Stephanie Koch

Patrick Lam

Leon M Smith Ii

The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors

The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Substituted biaryl compounds as factor XIa inhibitors

The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.

1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors

The present application describes 1,1-disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, &#x3b2;-aminoacids, &#x3b1;-aminoacids and derivatives thereof of Formula I:P-M-MIor a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein M is a linear core. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

1,1-Disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, &#x3b2;-aminoacids, &#x3b1;-aminoacids and derivatives thereof as factor Xa inhibitors

The present application describes linear chain substituted monocyclic and bicyclic compounds and derivatives thereof of Formula I:P-P-M-MIor pharmaceutically acceptable salt forms thereof, P-M are rings substituted by a linear group. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Linear chain substituted monocyclic and bicyclic derivatives as factor Xa inhibitors

The present application describes sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds and derivatives thereof of Formula I:P-P-M-MIor pharmaceutically acceptable salt forms thereof, wherein M is a ring, P is an optional ring, and Pand Mare as defined below. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors

The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I:or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.

Guanidine mimics factor Xa inhibitors

This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Isoxazoline and isoxazole fibrogen receptor antagonists

The present application describes 6-membered aromatics of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein D may be CH.sub.2 NH.sub.2 or C(.dbd.NH)NH.sub.2, which are useful as inhibitors of factor Xa.

6-membered aromatics as factor Xa inhibitors

The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.

Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and

The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(.dbd.NH)NH.sub.2, which are useful as inhibitors of factor Xa.

Nitrogen containing heteroaromatics as factor Xa inhibitors

The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.

Inhibitors of factor Xa with a neutral P1 specificity group

Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders. The compounds can be represented by the formula: ##STR1## where X is O, S or NR.sup.15.

Isoxazoline, isothiazoline and pyrazoline factor Xa inhibitors

This invention relates to ortho substituted phenyl compounds as inhibitors of prostaglandin synthase, to pharmaceutical compositions comprising such compounds and to methods of using such compounds as antiinflammatory and antipyretic agents. The class of compounds useful in this method of treatment is represented by Formula I below: ##STR1##

Prostaglandin synthase inhibitors

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Donald J Pinto