The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Oct. 03, 2006
Filed:
Apr. 21, 2004
Tianbao LU, Churchville, PA (US);
Karen L. Milkiewicz, Exton, PA (US);
Pierre Raboisson, Mechelen, BE;
Maxwell David Cummings, Wayne, PA (US);
Raul R. Calvo, Royersford, PA (US);
Daniel J. Parks, Downingtown, PA (US);
Louis V. Lafrance, Iii, West Chester, PA (US);
Juan Jose Marugan Sanchez, Downingtown, PA (US);
Joan Gushue, Conshohocken, PA (US);
Kristi Leonard, West Chester, PA (US);
Tianbao Lu, Churchville, PA (US);
Karen L. Milkiewicz, Exton, PA (US);
Pierre Raboisson, Mechelen, BE;
Maxwell David Cummings, Wayne, PA (US);
Raul R. Calvo, Royersford, PA (US);
Daniel J. Parks, Downingtown, PA (US);
Louis V. Lafrance, III, West Chester, PA (US);
Juan Jose Marugan Sanchez, Downingtown, PA (US);
Joan Gushue, Conshohocken, PA (US);
Kristi Leonard, West Chester, PA (US);
Ortho-McNeil Pharmaceutical, Inc., Raritan, NJ (US);
Abstract
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 —COR, —COM, —OH, —NHR, —SOR, —NHCONHR, optionally-substituted amidino or optionally-substituted guanidino; or R—X— is hydrogen or an electron pair; Ris oxygen or —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.