C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 211/27 (2006.01) A61K 31/135 (2006.01) A61K 31/137 (2006.01) A61P 3/04 (2006.01) C07C 211/08 (2006.01) C07C 215/28 (2006.01) C07C 225/08 (2006.01)
Patent
CA 2460348
The invention is directed, in part, to racemic and stereomerically pure 2- hydroxy derivatives of sibutramine and its metabolites, and 2-hydroxy derivatives of desmethylsibutramine and didesmethylsibutramine in particular. The invention is further directed to novel methods of preparing these derivatives are also disclosed. The invention is also directed to pharmaceutical compositions and dosage forms that comprise therapeutically or prophylactically effective amounts of the compounds, optionally in combination with an additional pharmacologically active compound. These pharmaceutical compositions and dosage forms can be used in the methods of the invention, which provide for the treatment or prevention of a variety of diseases and disorders.
La présente invention concerne notamment des dérivés 2-hydroxy racémiques et stéréomériquement purs de la sibutramine et de ses métabolites, ainsi que des dérivés 2-hydroxy de desméthylsibutramine et de didesméthylsibutramine en particulier. Cette invention concerne également de nouvelles méthodes de préparation de ces dérivés. En outre, cette invention porte sur des compositions pharmaceutiques et des formes dosifiées qui renferment des quantités thérapeutiquement ou prophylactiquement efficaces de ces composés, éventuellement associés à un composé pharmacologiquement actif supplémentaire. Ces compositions pharmaceutiques et ces formes dosifiées peuvent être utilisées dans les méthodes de la présente invention, qui visent à traiter ou à prévenir un certain nombre de maladies et de troubles.
Currie Mark G.
Fang Qun K.
Hsu Bob
Jerussi Thomas P.
Senanayake Chris H.
Osler Hoskin & Harcourt Llp
Sepracor Inc.
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