US4479955A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Heterocycle-fused pyrazolo[3,4-d]pyridin-3-ones as benzodiazepine receptor modulators
Assignee: Novartis Corp
•
Filing: 1983-01-10
•
Granted: 1984-10-30
•
Expires: 2003-01-10
Abstract
Abstract Disclosed are e.g. 2-aryl-pyrazolo[4,3-c][1,6]naphthyridin-3(5H)-ones, 2-aryl-thieno[2,3-b]pyrazolo[4,3-d]pyridin-3(5H)-ones, 2-aryl-pyrazolo[4,3-c][1,7]naphthyridin-3(5H)-ones, useful as benzodiazepine receptor modulators.
Inventors
- 👤 Naokata Yokoyama
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 10:23
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/72; C07D213/74; A; A61; A61P; A61P25/00; A61P25/08; A61P25/20; C07D213/75; C07D213/78; C07D213/79; C07D213/80; C07D231/00; C07D231/02; C07D231/10; C07D231/14; C07D231/28; C07D231/30; C07D231/32; C07D231/34; C07D401/00; C07D401/02; C07D401/04; C07D401/12; C07D471/00; C07D471/02; C07D471/04; C07D471/12; C07D471/14; C07D495/00; C07D495/12; C07D495/14
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
122 words
A compound of formula IA or IB ##STR10## wherein A together with the two carbon atoms to which it is attached represents fused 2,3-, 3,4- or 4,3-pyrido wherein the carbon atoms forming said rings are unsubstituted or one or two are substituted by lower alkyl, lower alkoxy or halogen; R 1 represents phenyl, or phenyl mono- or disubstituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R 1 represents an aromatic heterocyclic radical selected from pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl, or any said heterocyclic radical mono- or di-substituted by lower alkyl, lower alkoxy or halogen; R 2 , R 3 and R 3 ' independently represent hydrogen or lower alkyl; or a tautomer thereof; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
122 words
A compound of formula IA or IB ##STR10## wherein A together with the two carbon atoms to which it is attached represents fused 2,3-, 3,4- or 4,3-pyrido wherein the carbon atoms forming said rings are unsubstituted or one or two are substituted by lower alkyl, lower alkoxy or halogen; R 1 represents phenyl, or phenyl mono- or disubstituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R 1 represents an aromatic heterocyclic radical selected from pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl, or any said heterocyclic radical mono- or di-substituted by lower alkyl, lower alkoxy or halogen; R 2 , R 3 and R 3 ' independently represent hydrogen or lower alkyl; or a tautomer thereof; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
71 words
A compound according to claim 1 of formula IA or IB wherein A together with the two carbon atoms to which it is attached represents fused 2,3-, 3,4- or 4,3-pyrido, or any of said pyrido rings mono- or di-substituted by lower alkyl, lower alkoxy or halogen; R 1 , R 2 , R 3 and R 3 ' have meaning as given in claim 1; or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim
70 words
A compound according to claim 2 of formula IA or IB wherein A together with the two carbon atoms to which it is attached represents fused 3,4- or 4,3-pyrido, or said 3,4- or 4,3-pyrido ring mono- or di-substituted by lower alkyl, lower alkoxy or halogen; R 1 , R 2 , R 3 and R 3 ' have meaning as given in claim 1; or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim
83 words
A compound according to claim 3 of the formula II ##STR11## wherein R 1 represents phenyl or phenyl mono- or di-substituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R 1 represents an aromatic heterocyclic radical selected from pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl, or any said radical mono- or disubstituted by lower alkyl, lower alkoxy or halogen; R 4 and R 5 represent independently hydrogen, lower alkyl, lower alkoxy or halogen; or a tautomer thereof; or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim
83 words
A compound according to claim 3 of the formula III ##STR12## wherein R 1 represents phenyl or phenyl mono- or di-substituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R 1 represents an aromatic heterocyclic radical selected from pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl, or any said radical mono- or disubstituted by lower alkyl, lower alkoxy or halogen; R 6 and R 7 represent independently hydrogen, lower alkyl, lower alkoxy or halogen; or a tautomer thereof; or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
13 words
A compound of claim 4 being 2-phenyl-pyrazolo[4,3-c][1,6]naphthyridin-3(5H)-one or a pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim
13 words
A compound of claim 4 being 2-(3-pyridyl)-pyrazolo[4,3-c][1,6]naphthyridin-3(5H)-one or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim
13 words
A compound of claim 4 being 2-(2-thiazolyl)-pyrazolo[4,3-c][1,6]naphthyridin-3(5H)-one or a pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
13 words
A compound of claim 5 being 2-p-chlorophenyl-pyrazolo[4,3-c][1,7]naphthyridin-3(5H)-one or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
13 words
A compound of claim 4 being 2-(2-pyrimidyl)-pyrazolo[4,3-c][1,6]naphthyridin-3(5H)-one or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
13 words
A compound of claim 3 being 7-methyl-2-phenylpyrazolo[4,3-c][1,8]naphthyridin-3(5H)-one or a pharmaceutically acceptable salt thereof.
Claim 13
Dependent Claim
13 words
A compound of claim 4 being 2-p-chlorophenylpyrazolo[4,3-c][1,6]naphthyridin-3(5H)-one or a pharmaceutically acceptable salt thereof.
Claim 14
Dependent Claim
46 words
A pharmaceutical composition suitable for oral or parenteral administration to mammals for the treatment of nervous system conditions responsive to the action of a benzodiazepine receptor modulator, comprising an effective amount of a compound of claim 1 in combination with one or more pharmaceutically acceptable carriers.
Claim 15
Dependent Claim
52 words
A method for treating nervous system diseases responsive to benzodiazepine receptor modulation in mammals which comprises administering to a mammal in need thereof an effective amount of a compound of claim 1 or a pharmaceutical composition comprising an effective amount of said compound in combination with one or more pharmaceutically acceptable carriers.
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) | 1987-10-30 | 1988-04-30 | 1988-10-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-10-30 | 1992-04-30 | 1992-10-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-10-30 | 1996-04-30 | 1996-10-30 | $7700.00 | Window Closed / Lapsed |