3-dimensional Pharmaceuticals, Inc.

Nalin L Subasinghe

Carl R Illig

M Jonathan Rudolph

Roger Francis Bone

James B Hoffman

Kenneth Jerome Wilson

Tianbao Lu

Jeremy Mark Travins

Richard M Soll

Kristi A Leonard

Shelley K Ballentine

Heather Rae Hufnagel

Ehab Khalil

Farah Ali

Juan Jos&eacute; Marug&aacute;n

Mark James Wall

Bruce Edward Tomczuk

Joseph M Salvino

Sanath K Meegalla

Jinsheng Chen

Maxwell David Cummings

Hui Huang

Kenneth J Wilson

Wenxi Pan

Joan Gushue

Troy L Randle

Scott L Klein

Cynthia L Fedde

Todd L Graybill

Carl L Illig

Jonathan Rudolph

Kenneth T Wilson

Zhengdong Wu

The present invention is directed to conjugated complement cascade inhibitors, and a method of treating a patient using a conjugated complement cascade inhibitor.

Conjugated complement cascade inhibitors

Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula (I) or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R, R, R, Rand Rare defined in the specification, Z is SO or SO, and Ar is an aromatic or heteroaromatic group as defined herein. 

Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions

Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R, R, R, Rand Rare defined in the specification, Z is SO or SO, and Ar is an aromatic or heteroaromatic group as defined herein.

Heteroaryl amidines, methylamidines and guanidines, and the use thereof as protease inhibitors

Compounds and compositions for treating C1s-mediated diseases and conditions

Methods of treating C1s-mediated diseases and conditions and compositions thereof

Heteroaryl amidines, methylamidines and guanidines, and use thereof as protease inhibitors

The present invention is directed to compounds of Formula I:

Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors

The present invention provides a library of compounds, each comprised of a common aminobenzenedicarboxylic acid core structure (scaffold) that serves as a template for synthesizing approximately 10.sup.1 -10.sup.6 compounds which are analogs of the scaffold. The library is employed to study ligand binding by biological receptors, such as enzymes, G-protein coupled receptors and membrane channels. For example, certain individual compounds within the library selectively bind and inhibit the action of trypsin-like serine proteases. The present invention also relates to combinatorial synthetic methods for making such libraries of compounds. Additionally, the present invention relates to novel scaffold-modified solid supports, particularly scaffold-modified polymer resins and methods for preparing said resins. Further, the present invention is directed to methods for screening a compound or plurality of compounds made according to the synthetic methods disclosed herein, which comprise using the compounds in suitable assays developed for detecting the compounds' utility as pharmaceutical agents.

Aminobenzenedicarboxylic acid-based combinatorial libraries

Compounds of the formula: ##STR1## wherein R.sup.1 --R.sup.4, R.sup.7 --R.sup.8, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

Guanidino protease inhibitors

The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: ##STR1## or pharmaceutically acceptable salts thereof; wherein

Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa

The present invention is directed to novel compounds that are thrombin inhibitors and are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The compounds have the general Formula I: ##STR1## and pharmaceutically acceptable salts thereof; wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, n and m are defined herein.

Thrombin inhibitors

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West Chester, PA, United States of America

Nalin L Subasinghe