3-dimensional Pharmaceuticals, Inc.

Janssen Pharmaceutica Nv

Ortho-mcneil Pharmaceutical Corp.

Dimensional Pharmaceuticals, Inc.

3-dimensional Pharmaceutical, Inc.

Thomas P Markotan

Tianbao Lu

Bruce Edward Tomczuk

Colleen Siedem

Richard M Soll

Carl R Illig

Kristi A Leonard

Cynthia L Fedde

Zhihua Sui

James C Lanter

Thomas P Stagnaro

Maxwell David Cummings

Dana L Johnson

Robert W Tuman

Heather Rae Hufnagel

Nalin L Subasinghe

Richard Scott Alexander

Wenxi Pan

Richard William Connors

Jan L Sechler

Robert A Galemmo

Anna C Maroney

Jeremy Mark Travins

Xuqing Zhang

Ehab Khalil

Zihong Guo

Louis V LaFrance

Juan J Marugan Sanchez

Victor J Marder

David C U'Prichard

Beth M Anaclerio

Wenzi Pan

Tianbo Lu

Mark R Player

Daniel J Parks

Chaozhong Cai

Karen L Milkiewicz

Tho V Thieu

Yu-Kai Lee

Nalin Subasinghe

Louis Vincent Lafrance

Juan Jose Marugan

The present invention comprises compounds of Formula I. wherein: R, R, R, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

Cyclohexyl-azetidinyl antagonists of CCR2

The present invention comprises compounds of Formula (I). wherein: R, R, R, R, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

4-substituted-cyclohexylamino-4-piperidinyl-acetamide antagonists of CCR2

The present invention comprises compounds of Formula (I). wherein: X, R, R, R, and Rare as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

4-azetidinyl-1-heteroaryl-cyclohexane antagonists of CCR2

The invention is directed to triazolopyridazine compounds of Formula I: where R, R, R, R, R, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

Triazolopyridazine compounds

Triazolopyridazines as kinase modulators

The invention is directed to acylhydrazones compounds of Formula I: where R, Rand A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

Acylhydrazones as kinase modulators

The present invention is directed to novel compounds of Formula I: and forms and pharmaceutical compositions thereof, and the use thereof as inhibitors of Factor Xa.

Factor Xa compounds

Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NRand Het, R, R, R, R&#x2014;RR, R, R, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors

The present invention relates to novel substituted indole compounds that are antagonists of alpha V (&#x3b1;v) integrins, for example &#x3b1;&#x3b2;and &#x3b1;&#x3b2;integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by &#x3b1;&#x3b2;and &#x3b1;&#x3b2;integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R, R, R, R, R, R, R, R, R, R, R, R, R, R, D, X, W, a, m, n, i, j, k and v are defined herein.

Substituted indoles and their use as integrin antagonists

Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII:wherein X is O or NRand Het, R, R, R, R&#x2014;R, R, R, R, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

Phenyl acetamide compounds are described, including compounds ofor a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R-R, R, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

Aminopyridyl-substituted phenyl acetamides as protease inhibitors

The present invention relates to novel substituted indole compounds that are antagonists of alpha V (&#x3b1;v) integrins, for example &#x3b1;&#x3b2;and &#x3b1;&#x3b2;integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by &#x3b1;&#x3b2;and &#x3b1;&#x3b2;integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula:where R, R, R, R, R, R, R, R, R, R, R, R, R, R, D, X, W, a, m, n, i, j, k and v are defined herein.

Process for preparing aminoguanidines and alkoxyguanidines as protease inhibitors

Aminoguanidines and alkoxyguanidines as protease inhibitors

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Morgantown, PA, United States of America

Thomas P Markotan