Amine compound and use thereof for medical purposes

Details Amine compound and use thereof for medical purposes Amine compound and use thereof for medical purposes

C - Chemistry, Metallurgy

07

C

C07C 217/64 (2006.01) A61K 31/137 (2006.01) A61K 31/165 (2006.01) A61K 31/222 (2006.01) A61K 31/277 (2006.01) A61K 31/325 (2006.01) A61K 31/351 (2006.01) A61K 31/357 (2006.01) A61K 31/661 (2006.01) A61K 31/675 (2006.01) A61K 31/695 (2006.01) A61P 3/10 (2006.01) A61P 11/06 (2006.01) A61P 13/12 (2006.01) A61P 17/00 (2006.01) A61P 17/06 (2006.01) A61P 19/00 (2006.01) A61P 19/02 (2006.01) A61P 25/00 (2006.01) A61P 27/16 (2006.01) A61P 29/00 (2006.01) A61P 37/02 (2006.01) A61P 37/06 (2006.01) C07C 255/59 (2006.0

Patent

CA 2633374

A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. (see formula I) wherein R is a hydrogen atom or P(=O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH=CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5 - 8.

La présente invention concerne un nouveau composé aminé représenté par la formule générale (I) ci-dessous, un sel d'addition d'acide pharmaceutiquement acceptable du composé, ou un hydrate ou solvate du composé ou du sel, qui est excellent en terme d'effet immunosuppresseur, d'effet de suppression de réponse de rejet et similaire et a des effets secondaires indésirables tels que la brachycardie réduits. La présente invention concerne en outre une composition pharmaceutique comprenant le composé et un véhicule pharmaceutiquement acceptable. (I) où R représente un atome d'hydrogène ou P(=O)(OH)<SUB>2</SUB> ; X représente un atome d'oxygène ou de soufre ; Y représente CH<SUB>2</SUB>CH<SUB>2</SUB> ou CH=CH ; R<SUB>1</SUB> représente un alkyle ayant de 1 à 4 atomes de carbone qui est substitué par un atome d'halogène ou un cyano ; R<SUB>2</SUB> représente un alkyle ayant de 1 à 4 atomes de carbone qui peut être substitué par un groupe hydroxyle ou un atome d'halogène ; R<SUB>3</SUB> et R<SUB>4</SUB> représentent indépendamment un atome d'hydrogène ou un alkyle ayant de 1 à 4 atomes de carbone ; et n représente 5 à 8.

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