Pentacyclic oxepines and derivatives thereof, compositions...

Details Pentacyclic oxepines and derivatives thereof, compositions... Pentacyclic oxepines and derivatives thereof, compositions...

2007-09-18

2007-09-18

Dentz, Bernard (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C540S576000, C544S147000, C544S174000, C546S196000, C546S200000, C546S202000, C546S195000, C548S528000, C549S009000, C549S042000, C549S051000, C549S057000

Reexamination Certificate

active

10521998

ABSTRACT:
The present invention provides a compound of the formula (I) wherein R1is —H, —OH, —O(C1-C4alkyl), —OCOC6H5, —OCO(C1-C6alkyl), or —OSO2(C2-C6alkyl); R0, R2and R3are each independently —H, —OH, —O(C1-C4alkyl), —OCOC6H5, —OCO(C1-C6alkyl), —OSO2(C2-C6alkyl) or halo; R4is 1-piperidinyl, 1-pyrrolidinyl, methyl- 1-pyrrolidinyl, dimethyl-1-pyrrolidiny, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC═CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5is —H or C1-C4alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.

REFERENCES:
patent: 0 761669 (1996-09-01), None
patent: 0 943329 (1999-03-01), None
Grese, et al., Synthesis and Pharmacology of Conformationally Restricted Raloxifene Analogues: Highly Potent Selective Estrogen Receptor Modulators,J. Med. Chem, 1998,vol. 41, pp. 1272-1283.

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