US4472408A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Substituted trifluoromethylphenyltetrahydropyridines having an anorectic activity
Assignee: Elf Sanofi SA
•
Filing: 1982-03-03
•
Granted: 1984-09-18
•
Expires: 2002-03-03
Abstract
Abstract The invention relates to 4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridines of formula ##STR1## in which R represents a cyano, acetyl or cycloalkyl group of from 3 to 7 carbon atoms and Alk represents a straight or branched alkylene of from 1 to 4 carbon atoms, as well as to the salts thereof, having an anorectic activity, to a process for preparing same and to pharmaceutical compositions containing said compounds, useful in the treatment of obesity.
Inventors
- 👤 Dino Nisato
- 👤 Emilio Crisafulli
- 👤 Alberto Bianchetti
- 👤 Paolo Carminati
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 23:55
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/68; C07D211/70; A; A61; A61P; A61P3/00; A61P3/04
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
52 words
A compound selected from the group consisting of substituted trifluoromethylphenyl-1,2,3,6-tetrahydropyridines of formula ##STR7## wherein R is, acetyl or a cycloalkyl group of from 3 to 7 carbon atoms and Alk represents a straight or branched alkylene group of from 1 to 4 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
52 words
A compound selected from the group consisting of substituted trifluoromethylphenyl-1,2,3,6-tetrahydropyridines of formula ##STR7## wherein R is, acetyl or a cycloalkyl group of from 3 to 7 carbon atoms and Alk represents a straight or branched alkylene group of from 1 to 4 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
9 words
4-(3-trifluoromethylphenyl)-1-(3-oxobutyl)-1,2,3,6-tetrahydropyridine, or a pharmaceutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
9 words
4-(3-trifluoromethylphenyl)-1-(3-oxobutyl)-1,2,3,6-tetrahydropyridine, or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
9 words
4-(3-trifluoromethylphenyl)-1-(2-cyclohexylethyl)-1,2,3,6-tetrahydropyridine, or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim
9 words
4-(3-trifluoromethylphenyl)-1-(2-cyclohexylethyl)-1,2,3,6-tetrahydropyridine, or a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
9 words
4-(3-trifluoromethylphenyl)-1-(3-cyclohexylpropyl)-1,2,3,6-tetrahydropyridine, or a pharmaceutically acceptable acid addition salt thereof.
Claim 8
Dependent Claim
9 words
4-(3-trifluoromethylphenyl)-1-(3-cyclohexylpropyl)-1,2,3,6-tetrahydropyridine, or a pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim
9 words
4-(3-trifluoromethylphenyl)-1-acetonyl-1,2,3,6-tetrahydropyridine, or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Dependent Claim
9 words
4-(3-trifluoromethylphenyl)-1-acetonyl-1,2,3,6-tetrahydropyridine, or a pharmaceutically acceptable acid addition salt thereof.
Claim 11
Dependent Claim
75 words
A pharmaceutical composition in dosage unit form with anorectic activity comprising from 1 to 500 mg of an active ingredient selected from the group consisting of trifluoromethylphenyl-1,2,3,6-tetrahydropyridines of formula ##STR8## wherein R is, acetyl or a cycloalkyl group of from 3 to 7 carbon atoms and Alk represents a straight or branched alkylene group having from 1 to 4 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof; in admixture with a pharmaceutical carrier.
Claim 12
Dependent Claim
75 words
A pharmaceutical composition in dosage unit form with anorectic activity comprising from 1 to 500 mg of an active ingredient selected from the group consisting of trifluoromethylphenyl-1,2,3,6-tetrahydropyridines of formula ##STR8## wherein R is, acetyl or a cycloalkyl group of from 3 to 7 carbon atoms and Alk represents a straight or branched alkylene group having from 1 to 4 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof; in admixture with a pharmaceutical carrier.
Claim 13
Dependent Claim
17 words
A pharmaceutical composition as claimed in claim 6 in which the active ingredient is the 4-(3-trifluoromethylphenyl)-1-(2-cyclohexylethyl)-1,2,3,6-tetrahydropyridine hydrochloride.
Claim 14
Dependent Claim
17 words
A pharmaceutical composition as claimed in claim 6 in which the active ingredient is the 4-(3-trifluoromethylphenyl)-1-(3-cyclohexylpropyl)-1,2,3,6-tetrahydropyridine hydrochloride.
Claim 15
Independent Claim
62 words
A method for suppressing appetite comprising the step of administering therapeutically-effective doses of a pharmaceutically-active compound possessing anorectic activity and having the formula ##STR9## wherein R is acetyl, or a cycloalkyl group of from 3 to 7 carbon atoms, and Alk is a straight or branched alkylene group of from 1 to 4 carbon atoms, or a pharmaceutically-acceptable acid addition salt thereof.
Claim 16
Independent Claim
62 words
A method for suppressing appetite comprising the step of administering therapeutically-effective doses of a pharmaceutically-active compound possessing anorectic activity and having the formula ##STR9## wherein R is acetyl, or a cycloalkyl group of from 3 to 7 carbon atoms, and Alk is a straight or branched alkylene group of from 1 to 4 carbon atoms, or a pharmaceutically-acceptable acid addition salt thereof.
Claim 17
Dependent Claim
12 words
The method of claim 9 wherein the pharmaceutically-active compound is 4-(3-trifluoromethylphenyl)-1-(3-oxobutyl)-1,2,3,6-tetrahydropyridine hydrochloride.
Claim 18
Dependent Claim
12 words
The method of claim 9 wherein the pharmaceutically-active compound is 4-(3-trifluoromethylphenyl)-1-(2-cyclohexylethyl)-1,2,3,6-tetrahyropyridine hydrochloride.
Claim 19
Dependent Claim
12 words
The method of claim 9 wherein the pharamaceutically-active compound is 4-(3-trifluoromethylphenyl)-1-(3-cyclohexylpropyl)-1,2,3,6-tetrahydropyridine hydrochloride.
Claim 20
Dependent Claim
12 words
The method of claim 9 wherein the pharamaceutically-active compound is 4-(3-trifluoromethylphenyl)-1-acetonyl-1,2,3,6-tetrahydropyridine hydrochloride.
Claim 21
Independent Claim
52 words
A method for suppressing appetite comprising the step of administering therapeutically-effective doses of a pharmaceutically active compound possessing anorectic activity and having the formula ##STR10## wherein R is cyano and Alk is a straight or branched alkylene group of from 1 to 4 carbon atoms, or a pharmaceutically-acceptable acid addition salt thereof.
Claim 22
Independent Claim
52 words
A method for suppressing appetite comprising the step of administering therapeutically-effective doses of a pharmaceutically active compound possessing anorectic activity and having the formula ##STR10## wherein R is cyano and Alk is a straight or branched alkylene group of from 1 to 4 carbon atoms, or a pharmaceutically-acceptable acid addition salt thereof.
Claim 23
Dependent Claim
12 words
The method of claim 14 wherein the pharamaceutically-active compound is 4-(3-trifluoromethylphenyl)-1-(2-cyanoethyl)-1,2,3,6-tetrahydropyridine hydrochloride.
Claim 24
Dependent Claim
12 words
The method of claim 14 wherein the pharamaceutically-active compound is 4-(3-trifluoromethylphenyl)-1-(2-cyano-1-methyl)ethyl-1,2,3,6-tetrahydropyridine hydrochloride.
Claim 25
Dependent Claim
12 words
The method for claim 14 wherein the pharmaceutically-active compound is 4-(3-trifluoromethylphenyl)-1-(3-cyanopropyl)-1,2,3,6-tetrahydropyridine hydrochloride.
References Cited (Backward Citations)
US3072648A
Cited
US3125488A
Cited
GB881894A
Cited
GB948071A
Cited
GB984364A
Cited
US3284457A
Cited
US3626066A
Cited
US3627775A
Cited
DE2101997A1
Cited
US4012374A
Cited
US4024151A
Cited
US4213989A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-09-18 | 1988-03-19 | 1988-09-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-09-18 | 1992-03-19 | 1992-09-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-09-18 | 1996-03-19 | 1996-09-18 | $7700.00 | Window Closed / Lapsed |