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US4983603A
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Tricyclic cholinergic receptor agonists
Assignee: Elf Sanofi SA
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Filing: 1988-12-23
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Granted: 1991-01-08
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Expires: 2008-12-23
Abstract
Abstract The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors. These derivatives have the formula ##STR1## in which X=O, S, --OCH 2 -- or --SCH 2 --; R 1 =H or halogen; and R 2 = ##STR2## in which Alk is an alkylene group and R 3 , an R 4 , which are identical or different, are hydrogen or a lower alkyl group, or R 3 and R 4 , with the nitrogen atom to which they are bonded, form a 5- or 6-membered cyclic amino group optionally containing a second heteroatom; or R 2 is a group ##STR3## where R 5 =C 1 -C 4 -alkyl. Application: agonists of cholinergic receptors.
Inventors
- 👤 Camille G. Wermuth
- 👤 Paul Worms
- 👤 Jean-Jacques Bourguignon
- 👤 Roger Brodin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 11:23
CPC Classifications
C; C07; C07D; C07D491/00; C07D491/02; C07D491/04; A; A61; A61P; A61P25/00; A61P25/02; C07D495/00; C07D495/02; C07D495/04
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
130 words
A tricyclic compound having the formula ##STR17## in which: X represents an oxygen or sulfur atom or X represents --OCH 2 -- or --SCH 2 --; R 1 represents hydrogen or a halogen atom; and R 2 represents: ##STR18## in which: Alk represents a linear or branched alkylene group having from 2 to 5 carbon atoms, and R 3 and R 4 each independently represent hydrogen or a lower alkyl group having 1 to 4 carbon atoms; or R 3 and R 4 , with the nitrogen atom to which they are bonded, form a pyrrolidin-1-yl, piperidino, morpholino or piperazin-1-yl group; or ##STR19## in which R 5 represents a lower alkyl group having 1 to 4 carbon atoms, or a salt thereof with a pharmaceutically acceptable mineral or organic acid.
Claim 2
Dependent Claim
130 words
A tricyclic compound having the formula ##STR17## in which: X represents an oxygen or sulfur atom or X represents --OCH 2 -- or --SCH 2 --; R 1 represents hydrogen or a halogen atom; and R 2 represents: ##STR18## in which: Alk represents a linear or branched alkylene group having from 2 to 5 carbon atoms, and R 3 and R 4 each independently represent hydrogen or a lower alkyl group having 1 to 4 carbon atoms; or R 3 and R 4 , with the nitrogen atom to which they are bonded, form a pyrrolidin-1-yl, piperidino, morpholino or piperazin-1-yl group; or ##STR19## in which R 5 represents a lower alkyl group having 1 to 4 carbon atoms, or a salt thereof with a pharmaceutically acceptable mineral or organic acid.
Claim 3
Dependent Claim
13 words
A compound according to claim 1, wherein R 1 is a chlorine atom.
Claim 4
Dependent Claim
27 words
A pharmaceutical composition comprising an amount effective to treat cortical cholinergic deficiencies of at least one compound of formula (I), in combination with a pharmaceutically acceptable vehicle.
Claim 5
Dependent Claim
27 words
A pharmaceutical composition comprising an amount effective to treat cortical cholinergic deficiencies of at least one compound of formula (I), in combination with a pharmaceutically acceptable vehicle.
Claim 6
Dependent Claim
16 words
A pharmaceutical composition as claimed in claim 3, wherein the cortical cholingeric deficiency is Alzheimer-type dementia.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-01-07 | 1994-07-09 | 1995-01-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-01-07 | 1998-07-09 | 1999-01-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-01-07 | 2002-07-09 | 2003-01-08 | $7700.00 | Window Closed / Lapsed |