3-dimensional Pharmaceuticals, Inc.

Ortho-mcneil Pharmaceutical Corp.

Joan Gushue

Kristi A Leonard

Maxwell David Cummings

Jeremy Mark Travins

Mark James Wall

Sanath K Meegalla

Jinsheng Chen

Shelley K Ballentine

Hui Huang

Nalin L Subasinghe

Heather Rae Hufnagel

Ehab Khalil

Wenxi Pan

Farah Ali

Tianbao Lu

Daniel J Parks

Karen L Milkiewicz

Kenneth J Wilson

M Jonathan Rudolph

Raul R Calvo

Louis V LaFrance

Juan J Marugan Sanchez

Jonathan Rudolph

Pierre Raboisson

Kenneth T Wilson

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

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

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.

Growing community of inventors

Collegeville, PA, United States of America

Joan Gushue