US5338735A
Expired / Lapsed
US
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Pharmaceutical compounds
Assignee: Lilly Industries Ltd
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Filing: 1993-08-12
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Granted: 1994-08-16
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Expires: 2013-08-12
Abstract
Abstract Compounds of the formula: ##STR1## in which each R 1 is hydrogen, C 1-4 alkyl, C 1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R 2 is hydrogen, C 1-4 alkyl or C 2-4 alkenyl, R 3 and R 4 are each hydrogen, C 1-4 alkyl, optionally substituted phenyl or C 6-9 cycloalkyl optionally substituted by 1 to 4 C 1-4 alkyl groups, R 5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C 6-10 cycloalkyl optionally substituted with 1 to 4 C 1-4 alkyl groups or a phenyl group, or C 4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof. The compounds are indicated for use in the treatment of disorders of the central nervous system.
Inventors
- 👤 John Fairhurst
- 👤 David E. Tupper
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 09:05
CPC Classifications
C; C07; C07D; C07D409/00; C07D409/02; C07D409/12; A; A61; A61P; A61P25/00; A61P43/00; C07D333/00; C07D333/50; C07D333/52; C07D333/62; C07D333/68; C07D333/70; C07D417/00; C07D417/02; C07D417/12
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
131 words
A compound of the formula: ##STR8## in which each R 1 is hydrogen, C 1-4 alkyl, C 1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R 2 is hydrogen, C 1-4 alkyl or C 2-4 alkenyl, R 3 and R 4 are each hydrogen, C 1-4 alkyl, optionally substituted phenyl or C 6-9 cycloalkyl optionally substituted by 1 to 4 C 1-4 alkyl groups, R 5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C 6-10 cycloalkyl optionally substituted with 1 to 4 C 1-4 alkyl groups or a phenyl group, or C 4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.
Claim 2
Dependent Claim
131 words
A compound of the formula: ##STR8## in which each R 1 is hydrogen, C 1-4 alkyl, C 1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R 2 is hydrogen, C 1-4 alkyl or C 2-4 alkenyl, R 3 and R 4 are each hydrogen, C 1-4 alkyl, optionally substituted phenyl or C 6-9 cycloalkyl optionally substituted by 1 to 4 C 1-4 alkyl groups, R 5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C 6-10 cycloalkyl optionally substituted with 1 to 4 C 1-4 alkyl groups or a phenyl group, or C 4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.
Claim 3
Dependent Claim
24 words
A compound according to claim 1 in which y is 0, z is 0, 1 or 2 and R 5 is C 6-9 cycloalkyl.
Claim 4
Dependent Claim
28 words
A compound according to claim 1 in which y is 1, R 3 is hydrogen, R 4 is C 6-9 cycloalkyl and R 5 is C 6-9 cycloalkyl.
Claim 5
Dependent Claim
59 words
A compound according to claim 1 in which R 1 is hydrogen, R 2 is C 1-4 alkyl, R 5 is C 6-9 cycloalkyl, x is 2, and either (1) y is 0 and z is 0, 1 or 2, or (2) R 3 is hydrogen, R 4 is C 6-9 cycloalkyl, y is 1 and z is 0.
Claim 6
Dependent Claim
24 words
A pharmaceutical formulation which comprises a compound according to claim 1, or a pharmaceutically-acceptable salt thereof, together with a pharmaceutically-acceptable diluent or carrier therefor.
Claim 7
Dependent Claim
56 words
A method of treating a mammal including a human, suffering from or susceptible to a 5-HT 1A related condition selected from the group consisting of obesity, bulimia, depression, hypertension, sexual dysfunction, anxiety, gastrointestinal disorders, headaches, and cardiovascular disorders, which comprises administering an effective amount of a compound according to claim 1, or a pharmaceutically-acceptable salt thereof.
References Cited (Backward Citations)
US3662070A
Cited
GB1234699A
Cited
US3838169A
Cited
EP0160408A1
Cited
US4782080A
Cited
GB2193961A
Cited
US5118680A
Cited
US5096908A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-08-15 | 1998-02-14 | 1998-08-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-08-15 | 2002-02-14 | 2002-08-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-08-15 | 2006-02-14 | 2006-08-16 | $7700.00 | Window Closed / Lapsed |