Derivative of dihydro-dibenzo (a) anthracenes and their use...

Details Derivative of dihydro-dibenzo (a) anthracenes and their use... Derivative of dihydro-dibenzo (a) anthracenes and their use...

2006-10-10

2006-10-10

Saeed, Kamal A. (Department: 1626)

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C514S319000, C544S154000, C548S528000, C549S042000, C558S048000, C564S426000

Reexamination Certificate

active

07119206

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-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is S— or —HC═CH—; 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: 0 759 434 (1997-02-01), None
patent: 0 761 669 (1997-03-01), None
patent: WO 02 16316 (2002-02-01), None
Grese, T.A. et al., “Structure-Activity Relationships of Selective Estrogen Receptor Modulators: Modifications to the 2-Arylbenzothiophene Core of Raloxifene”Journal of Medicinal Chemistry, American Chemical Society, Washington, US. 1997. vol. 40, No. 2, pp. 146-167.

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