US4910199A
Expired / Lapsed
US
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Imidazo[1,2-]pyridazines for cortical cholinergic deficiencies
Assignee: Sanofi SA
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Filing: 1988-08-31
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Granted: 1990-03-20
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Expires: 2008-08-31
Abstract
Abstract The present invention relates to imidazo[1,2-b]-pyridazines having the formula: ##STR1## in which: R 1 represents hydrogen, a halogen atom, a C 1 -C 4 alkoxy group or a C 1 -C 4 alkyl group occupying one of the free positions of the benzene ring; R 2 represents hydrogen, a C 1 -C 4 alkyl group or a phenyl group; R 3 denotes hydrogen, a C 1 -C 4 alkyl group or a phenyl group; and R 4 R 5 represent hydrogen or a C 1 -C 4 alkyl group, or R 4 and R 5 form, together with the nitrogen atom to which they are bonded, a 5-membered or 6-membered heterocycle optionally containing a second heteroatom. Application: drugs, especially for the treatment of cortical cholinergic deficiencies.
Inventors
- 👤 Jean-Jacques Bourguignon
- 👤 Camille G. Wermuth
- 👤 Paul Worms
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 18:57
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/02; C07D487/04; A; A61; A61P; A61P25/00; A61P25/02; A61P25/28
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
147 words
Imidazo[1,2-b]pyridazines of the formula: ##STR25## in which: R 1 represents hydrogen, a halogen atom, a C 1 -C 4 alkoxy group or a C 1 -C 4 alkyl group occupying one of the free positions of the benzene ring; R 2 represents hydrogen, a C 1 -C 4 alkyl group or a phenyl group; R 3 represents hydrogen, a C 1 -C 4 alkyl group or a phenyl group; and the group ##STR26## occupies the 2-position or 3-position of the ring and, in this group, R 4 and R 5 , taken independently, represent hydrogen or a C 1 -C 4 alkyl group, or R 4 and R 5 , taken with the nitrogen atom to which they are bonded, form a 5-membered or 6-membered heterocycle, optionally having a second heteroatom, selected from pyrrolidine, piperidine or morpholine, and their salts with pharmaceutically acceptable mineral or organic acids.
Claim 2
Dependent Claim
147 words
Imidazo[1,2-b]pyridazines of the formula: ##STR25## in which: R 1 represents hydrogen, a halogen atom, a C 1 -C 4 alkoxy group or a C 1 -C 4 alkyl group occupying one of the free positions of the benzene ring; R 2 represents hydrogen, a C 1 -C 4 alkyl group or a phenyl group; R 3 represents hydrogen, a C 1 -C 4 alkyl group or a phenyl group; and the group ##STR26## occupies the 2-position or 3-position of the ring and, in this group, R 4 and R 5 , taken independently, represent hydrogen or a C 1 -C 4 alkyl group, or R 4 and R 5 , taken with the nitrogen atom to which they are bonded, form a 5-membered or 6-membered heterocycle, optionally having a second heteroatom, selected from pyrrolidine, piperidine or morpholine, and their salts with pharmaceutically acceptable mineral or organic acids.
Claim 3
Dependent Claim
40 words
Compounds according to claim 1 in which the group ##STR27## occupies the 2-position of the imidazole ring and in which R 1 , R 2 , R 3 , R 4 and R 5 are as defined in claim 1.
Claim 4
Dependent Claim
40 words
Compounds according to claim 1 in which the group ##STR28## occupies the 3-position of the imidazole ring and in which R 1 , R 2 , R 3 , R 4 and R 5 are as defined in claim 1.
Claim 5
Dependent Claim
37 words
A pharmaceutical composition for use in the treatment of cortical cholinergic deficiencies in humans comprising a pharmaceutically effective amount of a compound of formula (I) as active principle in combination with a pharmaceutically acceptable carrier or excipient.
Claim 6
Dependent Claim
37 words
A pharmaceutical composition for use in the treatment of cortical cholinergic deficiencies in humans comprising a pharmaceutically effective amount of a compound of formula (I) as active principle in combination with a pharmaceutically acceptable carrier or excipient.
Claim 7
Dependent Claim
18 words
A pharmaceutical composition as claimed in claim 4, wherein the active principle is present in dosage unit form.
Claim 8
Dependent Claim
22 words
A pharmaceutical composition as claimed in claim 5, wherein the unit dosage is between 10 mg and 500 mg of active ingredient.
Claim 9
Dependent Claim
21 words
A pharmaceutical composition as claimed in claim 6, wherein the unit dose can be administered 1 to 4 times per day.
Claim 10
Dependent Claim
16 words
A pharmaceutical composition as claimed in claim 4, 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) | 1993-03-19 | 1993-09-18 | 1994-03-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-03-19 | 1997-09-18 | 1998-03-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-03-19 | 2001-09-18 | 2002-03-20 | $7700.00 | Window Closed / Lapsed |