US4139638A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Methods for the treatment of hirsutism
Assignee: Merck Sharp & Dohme LLC
•
Filing: 1977-10-03
•
Granted: 1979-02-13
•
Expires: 1997-10-03
Abstract
Abstract This application relates to certain 4'-substituted and to 3', 4'-disubstituted anilides, to methods for their preparation and to methods for their use as antiandrogens. These substituted anilides are useful in the treatment of androgen dependent disease states, such as benign prostatic hypertrophy, hirsutism, acne and the like.
Inventors
- 👤 Rudolph O. Neri
- 👤 John G. Topliss
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 05:28
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/16; A61K31/165
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
129 words
A method useful for the treatment of hirsutism which comprises administering to mammals suffering from hirsutism a therapeutically effective quantity for treating hirsutism of a substituted anilide having the structural formula: ##STR27## or the non-toxic pharmaceutically acceptable salts thereof, wherein X is a member selected from the group consisting of nitro, trifluoromethyl, chloro, bromo and iodo; Y is a member selected from the group consisting of hydrogen, halogen, nitro, lower alkyl, lower alkoxy, lower alkanoyl, polyfluoroloweralkoxy, polyfluoroloweralkyl and trifluoromethylthio, with the proviso that when Y and R' are both hydrogen, X is other than iodo; R' is a member selected from the group consisting of hydrogen and alkyl having less than 5 carbon atoms, and R is cyclopropyl; cyclobutyl or branched chain alkyl having up to 8 carbon atoms.
Claim 2
Independent Claim
129 words
A method useful for the treatment of hirsutism which comprises administering to mammals suffering from hirsutism a therapeutically effective quantity for treating hirsutism of a substituted anilide having the structural formula: ##STR27## or the non-toxic pharmaceutically acceptable salts thereof, wherein X is a member selected from the group consisting of nitro, trifluoromethyl, chloro, bromo and iodo; Y is a member selected from the group consisting of hydrogen, halogen, nitro, lower alkyl, lower alkoxy, lower alkanoyl, polyfluoroloweralkoxy, polyfluoroloweralkyl and trifluoromethylthio, with the proviso that when Y and R' are both hydrogen, X is other than iodo; R' is a member selected from the group consisting of hydrogen and alkyl having less than 5 carbon atoms, and R is cyclopropyl; cyclobutyl or branched chain alkyl having up to 8 carbon atoms.
Claim 3
Dependent Claim
10 words
A method according to claim 1 wherein R is isopropyl.
Claim 4
Dependent Claim
10 words
A method according to claim 1 wherein R is cyclopropyl.
Claim 5
Dependent Claim
10 words
A method according to claim 2 wherein X is nitro.
Claim 6
Dependent Claim
10 words
A method according to claim 3 wherein X is nitro.
Claim 7
Dependent Claim
10 words
A method according to claim 2 wherein Y is trifluoromethyl.
Claim 8
Dependent Claim
10 words
A method according to claim 3 wherein Y is trifluoromethyl.
Claim 9
Dependent Claim
21 words
A method according to claim 2 wherein R' is hydrogen, Y is trifluoromethyl and X is nitro, said compound being 4'-nitro-3'-trifluoromethylisobutyranilide.
Claim 10
Dependent Claim
21 words
A method according to claim 2 wherein R' is hydrogen, Y is trifluoromethyl and X is iodo, said compound being 4'-iodo-3'-trifluoromethylisobutyranilide.
Claim 11
Dependent Claim
21 words
A method according to claim 3 wherein R' is hydrogen, Y is trifluoromethyl, and X is nitro, said compound being 4'-nitro-3'-trifluoromethylcyclopropylcarbanilide.
Claim 12
Dependent Claim
24 words
A method according to claim 1 wherein R' is hydrogen, X is nitro, Y is trifluoromethyl and R is 3'-methyl-2-butyl, said compound being 4'-nitro-3'-trifluoromethyl-2,3-dimethylbutyranilide.
Claim 13
Dependent Claim
25 words
A method according to claim 1 wherein R' is hydrogen, X is nitro, Y is trifluoromethyl and R is 2'-methyl propyl, said compound being 4'-nitro-3'-trifluoromethylisovaleranilide.
Claim 14
Dependent Claim
24 words
A method according to claim 1 wherein R' is hydrogen, X is bromo, Y is trifluoromethyl and R is isopropyl, said compound being 4'-bromo-3'-trifluoromethylisobutyranilide.
Claim 15
Dependent Claim
24 words
A method according to claim 1 wherein R' is hydrogen, X is chloro, Y is trifluoro and R is isopropyl, said compound being 4'-chloro-3'-trifluoromethylisobutyranilide.
Claim 16
Dependent Claim
24 words
A method according to claim 1 wherein R' is hydrogen, X is nitro, Y is bromo and R is isopropyl, said compound being 3'-bromo-4'-nitroisobutyranilide.
Claim 17
Dependent Claim
24 words
A method according to claim 1 wherein R' is hydrogen, X is nitro, Y is chloro and R is isopropyl, said compound being 3'-chloro-4'-nitroisobutyranilide.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-02-12 | 1982-08-14 | 1983-02-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-02-12 | 1986-08-14 | 1987-02-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-02-12 | 1990-08-14 | 1991-02-13 | $7700.00 | Window Closed / Lapsed |