IP Library Granted Patent US 8,227,462
Granted Patent B2
US 8,227,462 · App. 12/556,964 · Granted Jul 24, 2012

Pyrrolidine-1,2-dicarboxamide derivatives

Assignee: Novartis AG
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Quick Facts
Patent No.
US 8,227,462
App. No.
12/556,964
Granted
Jul 24, 2012
Kind
B2
Abstract

The present invention relates to a compound of formula (I) or a salt thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.

Claims (5)

1. A compound, in free form or in pharmaceutically acceptable salt form, that is (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide).

2. A compound, in free form or in pharmaceutically acceptable salt form, that is (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(1-methyl-cyclopropyl)-pyridin-4-yl]-thiazol-2-yl}-amide).

3. A method of treatment of a disease selected from melanoma, colorectal adenoma and cancers of the breast and pancreas, comprising the step of administering to a subject in need thereof a therapeutically effective amount of a compound selected from (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide) and (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(1-methyl-cyclopropyl)-pyridin-4-yl]-thiazol-2-yl}-amide), in free form or in pharmaceutically acceptable salt form.

4. A pharmaceutical composition comprising a therapeutically effective amount of a compound selected from (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide) and (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(1-methyl-cyclopropyl)-pyridin-4-yl]-thiazol-2-yl}-amide), in free form or in pharmaceutically acceptable salt form and one or more pharmaceutically acceptable carrier.

5. A combined pharmaceutical composition, adapted for simultaneous or sequential administration, comprising a therapeutically effective amount of a compound selected from (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide) and (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(1-methyl-cyclopropyl)-pyridin-4-yl]-thiazol-2-yl}-amide) in free form or in pharmaceutically acceptable salt form and a therapeutically effective amount of one or more combination partners; and one or more pharmaceutically acceptable excipients.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 8, 2011
From: FAIRHURST, ROBIN ALEC; GUAGNANO, VITO; IMBACH, PATRICIA; CARAVATTI, GIORGIO; FURET, PASCAL
To: NOVARTIS AG
Reel/Frame 026563/0668 →
Priority Claims (1)
EP 08164104 · Sep 10, 2008 · regional
Continuity (2)
Provisional Application 61096674 · Sep 12, 2008
Related Publication 20100105711A1 · Apr 29, 2010