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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.:

US 7947713 B1

PDFFull Text
Date of Patent:
May. 24, 2011

Filed:

Oct. 30, 2007

Tripeptidyl peptidase inhibitors

Applicants:

Henry Joseph Breslin, Lansdale, NJ (US);

Hans Louis Jos DE Winter, Schilde, BE;

Michael Joseph Kukla, Maple Glen, PA (US);

Inventors:

Henry Joseph Breslin, Lansdale, NJ (US);

Hans Louis Jos De Winter, Schilde, BE;

Michael Joseph Kukla, Maple Glen, PA (US);

Assignee:

Janssen Pharmaceutica N.V., , BE;

Attorney:
Primary Examiner:

Yong Chu

Assistant Examiner:

Michael Barker

Int. Cl.
CPC ...
A61K 31/4025 (2006.01); A61K 31/403 (2006.01); A61K 31/4196 (2006.01); A61K 31/4245 (2006.01); A61K 31/427 (2006.01); A61K 31/422 (2006.01); C07D 403/04 (2006.01); C07D 401/04 (2006.01); C07D 413/04 (2006.01); C07D 417/04 (2006.01);
U.S. Cl.
CPC ...
Abstract

The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. wherein n is an integer 0 or 1; X represents O; S; or —(CRR)— wherein m is an integer 1 or 2; Rand Rare each independently from each other hydrogen or Calkyl; Ris Calkylcarbonyl optionally substituted with hydroxy; Calkyloxycarbonyl; aminoCalkylcarbonyl wherein the Calkyl group is optionally substituted with Ccycloalkyl; mono- and di(Calkyl)aminoCalkylcarbonyl; aminocarbonyl substituted with aryl; CalkylcarbonyloxyCalkylcarbonyl; CalkyloxycarbonylaminoCalkylcarbonyl wherein the amino group is optionally substituted with Calkyl; an amino acid; Calkyl substituted with amino; or arylcarbonyl; Ris an optionally substituted 5-membered heterocycle, or Ris optionally substituted benzimidazole; Ris a bivalent radical —CHCH— optionally substituted with halo or phenylmethyl; or Ris a bivalent radical of formula.

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