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US4211786A Expired / Lapsed US ⏱️ 0.0 years remaining

Mercaptoacyldihydropyrazole carboxylic acid derivatives

Assignee: ER Squibb and Sons LLC
•
Filing: 1979-03-08
•
Granted: 1980-07-08
•
Expires: 1999-03-08
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Abstract

Abstract Hypertension can be treated using compounds having the formula or a basic salt thereof, wherein R 1 is hydrogen, alkyl, aryl, arylalkyl or ##STR1## wherein R 5 is alkyl or aryl; R 2 is hydrogen or alkyl; R 3 is aryl; R 4 is hydrogen, alkyl or arylalkyl and n is 0, 1 or 2.

Inventors

  • 👤 George C. Rovnyak

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-27 10:38
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/06; A; A61; A61P; A61P43/00; A61P9/00; A61P9/12

Claims Analysis

Total Claims: 21
Claim 1
Independent Claim 88 words
A compound having the formula ##STR14## or a basic salt thereof, wherein R 1 is hydrogen, alkyl, aryl or arylalkyl; R 2 is hydrogen or alkyl; R 3 is aryl; R 4 is hydrogen, alkyl or arylalkyl; and n is 0, 1 or 2; wherein the term "aryl" refers to phenyl or phenyl substituted with one, two or three halogen, alkyl, alkoxy, hydroxy, ##STR15## nitro, amino, alkylamino, dialkylamino, trifluoromethyl, cyano or carboxyl groups, and the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms.
Claim 2
Dependent Claim 88 words
A compound having the formula ##STR14## or a basic salt thereof, wherein R 1 is hydrogen, alkyl, aryl or arylalkyl; R 2 is hydrogen or alkyl; R 3 is aryl; R 4 is hydrogen, alkyl or arylalkyl; and n is 0, 1 or 2; wherein the term "aryl" refers to phenyl or phenyl substituted with one, two or three halogen, alkyl, alkoxy, hydroxy, ##STR15## nitro, amino, alkylamino, dialkylamino, trifluoromethyl, cyano or carboxyl groups, and the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms.
Claim 3
Dependent Claim 12 words
A compound in accordance with claim 1 wherein R 1 is hydrogen.
Claim 4
Dependent Claim 12 words
A compound in accordance with claim 1 wherein R 1 is alkyl.
Claim 5
Dependent Claim 12 words
A compound in accordance with claim 1 wherein R 1 is aryl.
Claim 6
Dependent Claim 12 words
A compound in accordance with claim 1 wherein R 1 is arylalkyl.
Claim 7
Dependent Claim 12 words
A compound in accordance with claim 1 wherein R 2 is hydrogen.
Claim 8
Dependent Claim 12 words
A compound in accordance with claim 1 wherein R 2 is methyl.
Claim 9
Dependent Claim 12 words
A compound in accordance with claim 1 wherein R 4 is hydrogen.
Claim 10
Dependent Claim 12 words
A compound in accordance with claim 1 wherein R 4 is alkyl.
Claim 11
Dependent Claim 12 words
A compound in accordance with claim 1 wherein R 4 is arylalkyl.
Claim 12
Dependent Claim 11 words
A compound in accordance with claim 1 wherein n is 0.
Claim 13
Dependent Claim 11 words
A compound in accordance with claim 1 wherein n is 1.
Claim 14
Dependent Claim 11 words
A compound in accordance with claim 1 wherein n is 2.
Claim 15
Dependent Claim 23 words
A compound in accordance with claim 1 wherein R 1 , R 2 and R 4 each is hydrogen and n is 1.
Claim 16
Dependent Claim 9 words
The compound in accordance with claim 1, DL-4,5-dihydro-1-(3-mercapto-1-oxopropyl)-3-phenyl-1H-pyrazole-5-carboxylic acid.
Claim 17
Dependent Claim 9 words
The compound in accordance with claim 1, D,L-3-(4-chlorophenyl)-4,5-dihydro-1-(3-mercapto-1-oxopropyl)-1H-pyrazole-5-carboxylic acid.
Claim 18
Dependent Claim 9 words
The compound in accordance with claim 1, D,L-3-(4-methoxyphenyl)-4,5-dihydro-1-(3-mercapto-1-oxopropyl)-1H-pyrazole-5-carboxylic acid.
Claim 19
Dependent Claim 9 words
The compound in accordance with claim 1, D,L-3-(4-fluorophenyl)-4,5-dihydro-1-(3-mercapto-1-oxopropyl)-1H-pyrazole-5-carboxylic acid.
Claim 20
Independent Claim 108 words
A method for reducing blood pressure in mammals which comprises administering to a mammal in need thereof, an effective amount of a compound having the formula ##STR16## or a basic salt thereof, wherein R 1 is hydrogen, aryl, or arylalkyl; R 2 is hydrogen or alkyl; R 3 is aryl; R 4 is hydrogen, alkyl or arylalkyl; and n is 0, 1 or 2; wherein the term "aryl" refers to phenyl or phenyl substituted with one, two or three halogen, alkyl, alkoxy, hydroxy, ##STR17## nitro, amino, alkylamino, dialkylamino, trifluoromethyl, cyano or carboxyl groups, and the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms.
Claim 21
Independent Claim 108 words
A method for reducing blood pressure in mammals which comprises administering to a mammal in need thereof, an effective amount of a compound having the formula ##STR16## or a basic salt thereof, wherein R 1 is hydrogen, aryl, or arylalkyl; R 2 is hydrogen or alkyl; R 3 is aryl; R 4 is hydrogen, alkyl or arylalkyl; and n is 0, 1 or 2; wherein the term "aryl" refers to phenyl or phenyl substituted with one, two or three halogen, alkyl, alkoxy, hydroxy, ##STR17## nitro, amino, alkylamino, dialkylamino, trifluoromethyl, cyano or carboxyl groups, and the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms.

References Cited (Backward Citations)

US4105776A Cited
BE861454A Cited
US4129566A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1983-07-08 1984-01-07 1984-07-08 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1987-07-08 1988-01-07 1988-07-08 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1991-07-08 1992-01-07 1992-07-08 $7700.00 Window Closed / Lapsed

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