3-Dimensional Pharmaceuticals, Inc.

Ortho-Mcneil Pharmaceutical Corp.

Dimensional Pharmaceuticals, Inc.

Juan J Marugan Sanchez

Bruce Edward Tomczuk

Kristi A Leonard

Louis V LaFrance

Victor J Marder

David C U'Prichard

Beth M Anaclerio

Thomas P Markotan

Zihong Guo

Tianbo Lu

Wenzi Pan

Tianbao Lu

Maxwell David Cummings

Daniel J Parks

Karen L Milkiewicz

Raul R Calvo

Joan Gushue

Pierre Raboisson

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

The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R, R, R, R, R, Rand M are defined herein; X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; and Ris &#x2014;COR, &#x2014;COM, &#x2014;OH, &#x2014;NHR, &#x2014;SOR, &#x2014;NHCONHR, optionally-substituted amidino or optionally-substituted guanidino; or R&#x2014;X&#x2014; is hydrogen or an electron pair; Ris oxygen or &#x2014;NRR; Ris cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; and R, Rand Rare independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or Rand R, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with R.

Substituted 1,4-diazepines and uses thereof

The present invention relates to novel substituted benzofurans and benzothiophenes 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 I:where R, R, R, R, R, R, R, R, R, R, R, R, R, R, m, n, i, j and k are defined herein.

Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists

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.

Growing community of inventors

Downingtown, PA, United States of America

Juan J Marugan Sanchez