Novel tetrahydrobenzindolone derivatives

Details Novel tetrahydrobenzindolone derivatives Novel tetrahydrobenzindolone derivatives

C - Chemistry, Metallurgy

07

D

C07D 209/60 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/44 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2275306

Compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof and a process for producing the same are disclosed. The compounds have progesterone receptor bindinq inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for hysteromyoma, endometriosis, meningioma, and myeloma, abortifacients, oral contraceptive pills, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance. Image wherein R1 represents alkyl or aralkyl; R2 represents a hydrogen atom, alkylcarbonyl, cycloalkylcarbonyl, aromatic acyl, heteroaromatic acyl, saturated heterocyclic acyl, alkyl, alkenyl, aralkyl, carbamoyl, alkylcarbamoyl, aromatic carbamoyl, aralkylcarbamoyl, alkylaminocarbonyl, cycloalkylcarbamoyl, alkoxycarbonyl, aryloxycarbonyl, heteroaromatic thiocarbonyl, saturated heterocyclic thiocarbonyl, or alkyl-thiocarbamoyl: and R3 represents a hydrogen atom, a hydroxyl group, alkyloxy, alkylcarbonyloxy, alkylthio, or arylthio.

L'invention porte sur des composés représentés par la formule générale (I) ou leurs sels pharmacocompatibles et sur leur procédé de production. En raison de leur capacité inhibitrice de la fixation de la progestérone à son récepteur, ces composés peuvent servir à traiter ou prévenir des maladies où la progestérone joue une rôle. Ils sont en particulier utiles comme agents anticancéreux agissant dans le cancer du sein ou des ovaires, comme remèdes contre le myome de l'utérus, l'endométriose, le méningiome et le myélome, comme abortifs, contraceptifs oraux et remèdes ou médicaments préventifs de l'ostéoporose et des symptômes de la ménopause. Dans la formule (I) R<1> représente alkyle ou aralkyle; R<2> représente hydrogène, alkylcarbonyle, cycloalkyl-carbonyle, acyle aromatique, acyle hétérocyclique saturé, alkyle, alcényle, aralkyle, carbamoyle alkylcabamoyle, carbamoyle aromatique, aralkylcabamoyle, alkylamino-carbonyle, cycloalkylcarbamoyle, alcoxycarbonyle, aryloxycarbonyle, thiocarbonyle hétéroaromatic, thiocarbonyle hétérocyclique saturé ou alkylthiocarbamoyle; et R<3> représente hydrogène, hydroxy, alkyloxy, alkylcarbonyloxy, alkylthio ou arylthio.

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