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.

Date of Patent:
Nov. 05, 2013

Filed:

Aug. 25, 2006
Applicants:

Ralf Plate, Oss, NL;

Christiaan Gerardus Johannes Maria Jans, Oss, NL;

Assignee:

Merck Sharp & Dohme B.V., BN Haarlem, NL;

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61P 5/44 (2006.01); A61P 29/00 (2006.01); A61K 31/55 (2006.01); C07D 471/04 (2006.01);
U.S. Cl.
CPC ...
Abstract

This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: —Ris —H or —(1-4C)alkyl; —Ris —C(O)Ror —S(O)R; —Ris —H, —(1-4C)alkyl or —OR; —Ris —H, —(1-4C)alkyl or —OR; —Ris —H or —C(R)NOR; —Ris —H, -halogen, -cyano; —(1-6C)alkyl, —(2-6C)alkenyl or —(2-6C)alkynyl, all optionally substituted with -amino, -hydroxyl or -halogen; —Ris —H, -cyano, -halogen, -nitro; —(1-6C)alkyl, —(2-6C)alkenyl, —(2-6C)alkynyl or —O(1-6C)alkyl, all optionally substituted with -amino, -hydroxyl or -halogen; -(hetero)aryl, optionally substituted with -cyano, -halogen, —(1-4C)alkyl, —(1-4C)alkoxy, —(1-4C)alkoxy(1-4C)alkyl or -(hetero)aryl; —C(R)NOR; —C(O)N(R); —C(O)R18, —C(O)OR, —NHC(O)R, or —NHS(O)R; —Ris —H, -halogen, -cyano, or —(1-4C)alkyl, optionally substituted with -halogen; —Ris —H or —(1-4C)alkyl; —Ris —H; —Ris —H, -cyano or —(1-4C)alkyl; —Ris —H, —(1-4C)alkyl, -halogen or -formyl; —Ris —H, -halogen, -cyano, —(1-4C)alkyl or -(hetero)aryl; or a pharmaceutically acceptable salt thereof. The compounds of this invention are highly specific for the glucocorticoid receptor and may be used for treating inflammatory diseases.


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