Benzothiophenes, and formulations and methods using same

The invention provides novel benzothiophenes of the formula:wherein R1 is -H, -OH, -O(C1-C4 alkyl), -O-CO(C1-C6 alkyl), -OSO2(C4-C6 alkyl, or -OCOAr where Ar is optionally substituted phenyl; R2 is -H, -OH, -Cl, -Br, -O(C1-C4 alkyl), -OCO(C1-C6 alkyl), -OSO2(C4-C6 alkyl, or -OCOAr where Ar is option...

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Hauptverfasser: CULLINAN GEORGE JOSEPH, FAHEY KENNAN JOSEPH
Format: Patent
Sprache:eng
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Zusammenfassung:The invention provides novel benzothiophenes of the formula:wherein R1 is -H, -OH, -O(C1-C4 alkyl), -O-CO(C1-C6 alkyl), -OSO2(C4-C6 alkyl, or -OCOAr where Ar is optionally substituted phenyl; R2 is -H, -OH, -Cl, -Br, -O(C1-C4 alkyl), -OCO(C1-C6 alkyl), -OSO2(C4-C6 alkyl, or -OCOAr where Ar is optionally substituted phenyl; R3 is -H, -F, -Cl, -(C1-C4 alkyl), -CN, or -O(C1-C3 alkyl); R4 is -H, -F, -Cl, -(C1-C4 alkyl), -CN or -O(C1-C3 alkyl); R5 is -H, -F, -Cl, -(C1-C4 alkyl), or -O(C1-C3 alkyl); and R6 is -H, -F, -Cl, -(C1-C4 alkyl), or -O(C1-C3 alkyl); with the provisos that R3, R4, R5 and R6 can not all be hydrogen, and that when one of R3, R4, R5 or R6 is C1-C4 alkyl, no more than two of R3, R4, R5 and R6 can be hydrogen; Y is -CO-, -CHOH-, or -CH2-; R7 and R8 are independently C1-C4 alkyl or combine to form, with the nitrogen to which they are attached, 1-piperidinyl, 1-pyrrolidinyl, 1-hexamethyleneimino, or morpholino; or a pharmaceutically acceptable salt thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, optionally containing estrogen opr progestin, and the use of such compounds alone, or in combination with estrogen or progestin or alleviating the symptoms of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, and estroge