Dihydro-dibenzo[b,e]oxepine based selective estrogren...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Details

C514S215000, C514S431000, C514S443000, C540S576000, C549S001000, C549S354000

Reexamination Certificate

active

07067510

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:
patent: 0761669 (1996-02-01), None
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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