Compound having hydroxycarbonyl-halogenoalkyl side chains

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 59/56 (2006.01) A61K 31/20 (2006.01) A61K 31/381 (2006.01) A61K 31/538 (2006.01) A61K 31/565 (2006.01) C07C 51/38 (2006.01) C07C 59/54 (2006.01) C07C 59/64 (2006.01) C07C 401/00 (2006.01) C07D 209/12 (2006.01) C07D 265/36 (2006.01) C07D 303/18 (2006.01) C07D 311/60 (2006.01) C07D 333/56 (2006.01) C07J 1/00 (2006.01)

Patent

CA 2394636

A compound in which either a compound having reduced oral activity or a group having a framework thereof is chemically bonded to a group represented by the general formula (1) (wherein R1 represents hydrogen, etc. ; R2 represents C1-7 halogenoalkyl, etc. ; m is an integer of 2 to 14; and n is an integer of 2 to 7); an optical isomer of the compound; or a hydrate or pharmacologically acceptable salt of these compounds. When imparted to a framework of, e. g. , a compound having anti-estrogen activity, those compounds can have significantly improved oral activity. The compounds are hence useful as a medicine.

L'invention concerne un composé dans lequel, un composé à activité orale réduite ou un groupe de structure apparentée est chimiquement lié à un groupe représenté par la formule générale (1) (dans laquelle R¿1? représente un atome d'hydrogène, etc., R¿2? représente un halogénoalkyle en C¿1?-C¿7?, etc., m est un entier prenant une valeur de 2 à 14, et n est un entier prenant une valeur de 2 à 7). L'invention concerne aussi un isomère optique du composé, ainsi qu'un hydrate ou un sel de ces composés, acceptables sur le plan pharmaceutique. Leur apport à une structure d'un composé, présentant une activité anti-estrogène, par exemple, confère à ces composés une amélioration significative de l'activité orale. Ils peuvent donc être utilisés comme un médicament.

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