US4004009A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Antihypertensive aryl pyrazolo[4,3-c]pyridazinones
Assignee: Sandoz Inc
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Filing: 1975-07-31
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Granted: 1977-01-18
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Expires: 1995-07-31
Abstract
Abstract The compounds are aryl-pyridazinone derivatives, e.g., 1-methyl-5-(2'-fluoro-5'-trifluoromethylphenyl)-1H-pyrazolo [4,3-c]pyridazin-6(5H)-one. They are useful as antihypertensives and are prepared by treating a hydrazinopyridazinone with a dialkylamino dialkyl-acetal.
Inventors
- 👤 Paul L. Anderson
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 00:09
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/02; C07D487/04; C07D237/00; C07D237/02; C07D237/06; C07D237/10; C07D237/20
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
119 words
A compound which is a pyridazinone of the formula: ##STR16##wherein X is a hydrogen atom, fluoro or chloro; Y 1 and Y 2 are the same or different and are selected from the group consisting of a hydrogen atom, alkyl having from 1 to 4 carbon atoms, fluoro, chloro, bromo, trifluoromethyl, and alkoxy having from 1 to 4 carbon atoms, provided that when both Y 1 and Y 2 are trifluoromethyl or branched alkyl, they are not on adjacent carbon atoms; R is a hydrogen atom or alkyl having from 1 to 3 carbon atoms; and R 3 is a hydrogen atom or alkyl having from 1 to 4 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
119 words
A compound which is a pyridazinone of the formula: ##STR16##wherein X is a hydrogen atom, fluoro or chloro; Y 1 and Y 2 are the same or different and are selected from the group consisting of a hydrogen atom, alkyl having from 1 to 4 carbon atoms, fluoro, chloro, bromo, trifluoromethyl, and alkoxy having from 1 to 4 carbon atoms, provided that when both Y 1 and Y 2 are trifluoromethyl or branched alkyl, they are not on adjacent carbon atoms; R is a hydrogen atom or alkyl having from 1 to 3 carbon atoms; and R 3 is a hydrogen atom or alkyl having from 1 to 4 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
12 words
A compound of claim 1 in which R is a hydrogen atom.
Claim 4
Dependent Claim
10 words
A compound of claim 1 in which R is alkyl.
Claim 5
Dependent Claim
10 words
A compound of claim 3 in which R is methyl.
Claim 6
Dependent Claim
11 words
A compound of claim 4 in which Y 1 is meta-trifluoromethyl.
Claim 7
Dependent Claim
10 words
The compound of claim 5 which is 1-methyl-5-(2'-fluoro-5'-trifluoromethylphenyl)-1H-pyrazolo[4,3-c] pyridazin-6-(5H) -one.
Claim 8
Dependent Claim
8 words
The compound of claim 5 which is 7-chloro-1-methyl-5-(3'-trifluoromethylphenyl)-1H-pyrazolo[4,3-c]pyridazin-6-(5H)-one.
Claim 9
Dependent Claim
10 words
The compound of claim 5 which is 7-chloro-1-methyl-5-(2'-fluoro-5'-trifluoromethylphenyl) -1H-pyrazolo [4,3-c]pyridazin-6-(5H)-one.
Claim 10
Dependent Claim
8 words
The compound of claim 5 which is 1-methyl-5-(3'-trifluoromethylphenyl)-1H-pyrazolo[4,3-c]pyridazin-6-(5H)-one.
Claim 11
Dependent Claim
27 words
A pharmaceutical composition useful for treating hypertension in a mammal comprising a compound of claim 1 in hypertension-reducing effective amount and a non-toxic pharmaceutically acceptable carrier therefor.
Claim 12
Dependent Claim
21 words
A composition of claim 10 in which the compound is present in an amount of from about 20 to 750 milligrams.
Claim 13
Dependent Claim
10 words
A composition of claim 10 which is a solid composition.
Claim 14
Dependent Claim
31 words
A method of treating hypertension in a mammal in need of such treatment comprising internally administering a compound of claim 1, in an amount effective in reducing hypertension, to said mammal.
Claim 15
Dependent Claim
22 words
A method of claim 13 in which the compound is administered in an amount of from about 75 to 1500 milligrams daily.
Claim 16
Dependent Claim
14 words
A method of claim 13 in which the mode of administration is oral administration.
References Cited (Backward Citations)
US3940248A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-01-18 | 1980-07-19 | 1981-01-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-01-18 | 1984-07-19 | 1985-01-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-01-18 | 1988-07-19 | 1989-01-18 | $7700.00 | Window Closed / Lapsed |