Dihydro-dibenzo[B,E]oxepine based selective estrogen...

Details Dihydro-dibenzo[B,E]oxepine based selective estrogen... Dihydro-dibenzo[B,E]oxepine based selective estrogen...

2008-05-20

2008-05-20

Seaman, D. Margaret (Department: 1625)

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C546S206000

Reexamination Certificate

active

11276203

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; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 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:
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patent: 6471979 (2002-10-01), New et al.
patent: 0 761669 (1996-09-01), None
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Grese, et al., “Synthesis and Pharmacology of Conformationally Restricted Raloxifene Analogues: Highly Potent Selective Estrogen Receptor Modulators,” J. Med. Chem., vol. 41, pp. 1272-1283 (1998).

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