Cyanopyrroles for binding the progesterone receptor

Details Cyanopyrroles for binding the progesterone receptor Cyanopyrroles for binding the progesterone receptor

C - Chemistry, Metallurgy

07

D

C07D 413/04 (2006.01) A61K 31/40 (2006.01) A61P 15/16 (2006.01) C07D 403/04 (2006.01)

Patent

CA 2372560

This invention provides compounds that bind the progesterone receptor of formula (1) having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together to form a ring and together contain -CH2(CH2)n CH2-, -CH2CH2CMe2CH2CH2-, -O(CH2)p CH2-, -O(CH2)q O-, -CH2CH2OCH2CH2-, or -CH2CH2NR7CH2CH2-; n=1-5; p=14; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or COR A; R A is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or COR B; R B is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof. (see formula 1)

La présente invention concerne un antagoniste de récepteur de progestérone représenté par la formule (1) dans laquelle T représente O, S, ou aucun élément; R1, and R2 représentent individuellement hydrogène, alkyle, alkyle substitué; ou R1 and R2 sont pris ensemble pour former un cycle et contiennent ensemble -CH2(CH2)nCH2-, -CH2CH2CMe2CH2CH2-, -O(CH2)pCH2-, -O(CH2)qO-, CH2CH2OCH2CH2-, ou -CH2CH2NR7CH2CH2-; n=1-5; p=1-4; q=1-4; R3 représente hydrogène, OH, NH2, alkyle, alkyle substitué, alcényle, alcényle substitué, alcynyle, alcynyle substitué, ou COR<A>; R<A> représente hydrogène, alkyle, alkyle substitué, alcoxy, alcoxy substitué, aminoalkyle, ou aminoalkyle substitué; R4 représente hydrogène, halogène, CN, NH2, alkyle, alkyle substitué, alcoxy, alcoxy substitué, aminoalkyle, ou aminoalkyle substitué; R5 représente hydrogène, alkyle, ou alkyle substitué; R6 représente hydrogène, alkyle, alkyle substitué, ou COR<B>; R<B> représente hydrogène, alkyle, alkyle substitué, alcoxy, alcoxy substitué, aminoalkyle, ou aminoalkyle substitué; R7 représente hydrogène ou alkyle; ou un sel de ceux-ci acceptable sur le plan pharmaceutique.

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