C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 495/04 (2006.01) A61K 31/4365 (2006.01) A61P 7/02 (2006.01)
Patent
CA 2536052
The present invention relates to novel crystalline forms of the platelet aggregation inhibitor (+)-(S)-methyl-2-(2-chlorophenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetate, clopidogrel (1), in the form of hydrogen bromide salts, identified as polymorph forms 1, 2 and 3. The present invention further relates to processes for preparing such forms, pharmaceutical compositions comprising such forms, and uses for such forms and compositions. The pharmaceutical compositions may be used, in particular, for inhibiting platelet aggregation or for treating, preventing or managing thrombosis, atherothrombosis, an atherothrombotic event, ischaemic stroke, myocardial infarction, non-Q-wave myocardial infarction, atherosclerosis, peripheral arterial disease, or unstable angina. The present invention also relates to methods of treating said disorders. Formula (1).
L'invention concerne des formes cristallines de l'inhibiteur de l'agrégation des plaquettes (+)-(S)-méthyl-2-(2-chlorophényl)-(6,7-dihydro-4H-thiéno[3,2-c]pyrid-5-yl)acétate, le clopidogrel (1), sous la forme de sels de bromure d'hydrogène, soit les formes de polymorphes 1, 2 et 3. L'invention concerne également des procédés de préparation de telles formes, des compostions pharmaceutiques renfermant de telles formes et des utilisations de telles formes et compositions. Les compositions pharmaceutiques peuvent être utilisées, notamment, pour inhiber l'agrégation des plaquettes ou pour traiter, empêcher ou gérer une thrombose, une athérothrombose, un événement athérothrombotique, un accident vasculaire cérébral ischémique, un infarctus du myocarde, un infarctus du myocarde sans onde Q, une athérosclérose, une maladie artérielle périphérique ou une angine instable. L'invention concerne également des méthodes de traitement de ces troubles.
Arul Ramakrishnan
Gadakar Maheshkumar
Gray Jason
Pise Abhinay
Rao Rajesh
Generics (uk) Limited
Osler Hoskin & Harcourt Llp
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