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Last Updated: December 22, 2024

Claims for Patent: 8,227,462


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Summary for Patent: 8,227,462
Title:Pyrrolidine-1,2-dicarboxamide derivatives
Abstract: The present invention relates to a compound of formula (I) ##STR00001## 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.
Inventor(s): Fairhurst; Robin Alec (Basel, CH), Guagnano; Vito (Basel, CH), Imbach; Patricia (Kalseraugst, CH), Caravatti; Giorgio (Bottmingen, CH), Furet; Pascal (Thann, FR)
Assignee: Novartis AG (Basel, CH)
Application Number:12/556,964
Patent Claims: 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]-thia- zol-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}-amid- e).

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}-amid- e), 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}-amid- e), 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]-thia- zol-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}-amid- e) 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.

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