Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1998-05-29
2000-12-12
Kumar, Shailendra
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514524, 514616, 514628, A61K 31275
Patent
active
061600113
ABSTRACT:
The present invention relates to a nonsteroidal agonist compound having the formula: ##STR1## where R.sub.1, R.sub.2, and R.sub.3 are the same or different and are a hydrogen, a nitro, a cyano, a carbamoyl, a halogen, a perfluoroalkyl, a haloalkylamido, an isothiocyanate, an azide, a diazocarbonyl, a substituted oxirane, or a .beta.-chloroethylamine; R.sub.4 is a hydrogen, an alkyl, or is joined to R.sub.5 ; R.sub.5 is a hydrogen, a hydroxy, an alkoxy, an acyloxy, an amino, an alkylamino, a halogen, an alkyl, a haloalkyl, or is joined to R.sub.4 ; R.sub.6 is a hydrogen, an alkyl, or a haloalkyl; A.sub.1 and A.sub.2 is the same or different, each is direct link or an alkylene; X.sub.1 is an oxygen, a sulfur, a sulphinyl, a sulphonyl, an amino, an alkylimino, or an alkylene; R.sub.7 is a hydrogen, a halogen, an alkoxy, a haloalkoxy, an acyloxy, a haloacyloxy, an aryloxy, a thioalkyl, a thioraryl, an amino, an alkylimino, an alkylamido group, a haloalkylamido group, or a phenyl optionally substituted with a halogen, a nitro group, an alkyl, a haloalkyl, a cyano, a hydroxyl, a carboxylic group, an amino, an alkylamino group, a dialkylamino group, a bisalkylamino group, a haloalkylamino group, a dihaloalkylamino group, a bishaloalkylamino group, an acylamido group, a diacylamido group, an alkylacylamido group, a haloacylamido group, a bis(haloacyl)imido group, or an alkylhaloacylamido group. The present invention further relates to a method of producing the non-steroidal agonist compound, a composition containing the non-steroidal agonist compound, and methods of binding an androgen receptor, suppressing spermatogenesis, and providing hormonal therapy for androgen-dependent conditions.
REFERENCES:
patent: 3875229 (1975-04-01), Gold
patent: 4139638 (1979-02-01), Neri et al.
patent: 4191775 (1980-03-01), Glen
patent: 4239776 (1980-12-01), Glen et al.
patent: 4282218 (1981-08-01), Glen et al.
patent: 4386080 (1983-05-01), Crossley et al.
patent: 4636505 (1987-01-01), Tucker
patent: 4880839 (1989-11-01), Tucker
McKillop et al., "Enantioselective Metabolism and Pharmacokinetics of Casodex in the Male Rat," Xenobiotica, 25(6):623-634 (1995).
Tucker et al., "Resolution of the Nonsteriodal Antiandrogen 4'-Cyano-3-[4-fluorophenyl) sulfonyl]-2-hydroxy-2-mehtyl-3'-(trifluoromethyl)-propionanilide and the Determination of the Absolute Configuration of the Active Enantiomer," J. Med. Chem., 31(4):885-887 (1988).
Kirkovsky et al., "Approaches to Irreversible Non-Steroidal Chiral Antiandrogens," 47th Southeast/51st Southwest Joint Regional Meeting of the American Chemical Society, Memphis, TN (Nov. 29-Dec. 1, 1995).
Dalton James T.
Kirkovsky Leonid I.
Miller Duane D.
Mukherjee Arnab
Cohen Mark S.
Kumar Shailendra
The University of Tennessee Research Corporation
LandOfFree
Non-steroidal agonist compounds and their use in male hormone th does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Non-steroidal agonist compounds and their use in male hormone th, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Non-steroidal agonist compounds and their use in male hormone th will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-218264