4-fluoroalkyl-2h-benzopyrans with anti-estogenic activity

Details 4-fluoroalkyl-2h-benzopyrans with anti-estogenic activity 4-fluoroalkyl-2h-benzopyrans with anti-estogenic activity

2005-01-18

2005-01-18

Dentz, Bernard (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S228200, C514S233500, C514S320000, C514S422000, C514S456000, C540S596000, C544S062000, C544S151000, C546S196000, C548S525000, C549S406000

Reexamination Certificate

active

06844336

ABSTRACT:
This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I,in whichZ is a straight-chain or branched-chain alkyl group with up to 5 carbon atoms that is fluorinated in at least one place, preferably a trifluoromethyl group, and R1, R2, X, Y and n have the meanings that are indicated in the description.The new compounds have at their disposal strong antiestrogenic action. In addition, they can have at their disposal estrogenic action that occurs in a tissue-selective manner. They can be used for the production of pharmaceutical agents, especially for the treatment of estrogen-dependent diseases and tumors and pharmaceutical agents for hormone replacement therapy (HRT) as well as for the prevention and treatment of osteoporosis.

REFERENCES:
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patent: 6060503 (2000-05-01), Labrie et al.
patent: 0470310 (1992-02-01), None
patent: WO 9626201 (1996-08-01), None
patent: WO 9902512 (1999-01-01), None
A. P. Sharma et al., “Structure-Activity-Relationship of Antiestrogens. Effect of the Side Chain and Its Position on the Activity of 2,3-Diaryl-2H-1-benzopyrans,” J. Med. Chem., 1990, pp. 3216-3222 and pp. 3219-3220, vol. 33, XP002170868.

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