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US4304914A Expired / Lapsed US ⏱️ 0.0 years remaining

Naphthyridone derivatives

Assignee: PHARMACEUTICAL Corp
•
Filing: 1980-07-07
•
Granted: 1981-12-08
•
Expires: 2000-07-07
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Abstract

Abstract Compounds of the formula ##STR1## wherein each of R, R 1 and R 2 is independently H, alkyl, alkenyl, alkoxy, halo, hydroxy, trifluoromethyl, amino, alkylamino, cyano and nitro; R 3 is carbalkoxy, carboxamide alkanoyl, trifluoromethyl and cyano; and Ar is heteroaryl or ##STR2## wherein R 4 and R 5 have the same meaning as each of R, R 1 and R 2 ; and acid addition salts thereof have cardiotonic and hypertensive activity.

Inventors

  • 👤 James R. Shroff
  • 👤 Bernard Loev

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 15:45
CPC Classifications
C; C07; C07D; C07D471/00; C07D471/02; C07D471/04

Claims Analysis

Total Claims: 19
Claim 1
Independent Claim 122 words
A therapeutically active compound of the formula ##STR7## wherein R and R 1 are independently H, alkyl, alkenyl, alkoxy, halo, hydroxy, trifluoromethyl, amino, alkylamino, cyano or nitro, R 2 is an alkyl or alkenyl containing 1 to 5 carbon atoms, R 3 is H, carbalkoxy, carboxamido, alkanoyl, trifluoromethyl or cyano, and Ar is heteroaryl selected from the group consisting of thiophene, furan, pyridine, thiazole, pyrimidine, pyrrole, benzofuran, quinoline, benzothiophene or a radical of the formula ##STR8## wherein R 4 and R 5 have the same meaning as R and R 1 ; wherein the alkenyl groups, the alkyl groups per se and the alkyl groups in alkoxy, alkylamino, carbalkoxy and alkanoyl contain up to 10 carbon atoms; and acid addition salts thereof.
Claim 2
Dependent Claim 122 words
A therapeutically active compound of the formula ##STR7## wherein R and R 1 are independently H, alkyl, alkenyl, alkoxy, halo, hydroxy, trifluoromethyl, amino, alkylamino, cyano or nitro, R 2 is an alkyl or alkenyl containing 1 to 5 carbon atoms, R 3 is H, carbalkoxy, carboxamido, alkanoyl, trifluoromethyl or cyano, and Ar is heteroaryl selected from the group consisting of thiophene, furan, pyridine, thiazole, pyrimidine, pyrrole, benzofuran, quinoline, benzothiophene or a radical of the formula ##STR8## wherein R 4 and R 5 have the same meaning as R and R 1 ; wherein the alkenyl groups, the alkyl groups per se and the alkyl groups in alkoxy, alkylamino, carbalkoxy and alkanoyl contain up to 10 carbon atoms; and acid addition salts thereof.
Claim 3
Dependent Claim 32 words
A compound according to claim 1 wherein the alkenyl groups and the alkyl groups per se and the alkyl groups in alkoxy, alkylamino, carbalkoxy and alkanoyl contain up to 7 carbon atoms.
Claim 4
Dependent Claim 36 words
The compound according to claim 2 wherein R is trifluoromethyl, R 3 is carbalkoxy, R 1 is H, R 2 is alkyl and Ar is phenyl or substituted phenyl wherein the substituent is alkoxy or trifluoromethyl.
Claim 5
Dependent Claim 22 words
A compound according to claim 1 of the formula ##STR9## wherein R, R 1 and Ar are as defined in claim 1.
Claim 6
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is hydrogen, and Ar is 2-methoxyphenyl.
Claim 7
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-methoxy, R 1 is hydrogen, and Ar is phenyl.
Claim 8
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is hydrogen, and Ar is phenyl.
Claim 9
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is hydrogen, and Ar is 4-fluorophenyl.
Claim 10
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is hydrogen, and Ar is 2-pyridyl.
Claim 11
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is hydrogen, and Ar is 3,4-dimethoxyphenyl.
Claim 12
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is 2-methoxy, and Ar is phenyl.
Claim 13
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is hydrogen, and Ar is 4-methoxyphenyl.
Claim 14
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is hydrogen, and Ar is 2-trifluoromethylphenyl.
Claim 15
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is hydrogen, and Ar is 4-trifluoromethylphenyl.
Claim 16
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is hydrogen, and Ar is 3-methoxyphenyl.
Claim 17
Dependent Claim 18 words
A compound according to claim 4 wherein R is 2-trifluoromethyl, R 1 is 2-methoxy, and Ar is 2-methoxyphenyl.
Claim 18
Dependent Claim 18 words
A compound according to claim 4 wherein R is hydrogen, R 1 is hydrogen, and Ar is 2-methoxyphenyl.
Claim 19
Dependent Claim 10 words
A hydrochloride salt of the compound according to claim 3.

References Cited (Backward Citations)

US3555034A Cited
US3590036A Cited
US3963736A Cited
DE2607012A1 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-12-07 1985-06-08 1985-12-08 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-12-07 1989-06-08 1989-12-08 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-12-07 1993-06-08 1993-12-08 $7700.00 Window Closed / Lapsed

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