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US4110452A Expired / Lapsed US ⏱️ 0.0 years remaining

Pyrazolo (1,5-c) quinazoline derivatives and related compounds

Assignee: ER Squibb and Sons LLC
•
Filing: 1977-10-17
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Granted: 1978-08-29
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Expires: 1997-10-17
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Abstract

Abstract Compounds are provided having the structure ##STR1## wherein R 1 is alkylamino, dialkylamino, or ##STR2## wherein alkyl in the above groups contains 1 to 4 carbons; R 2 is alkylamino, dialkylamino or ##STR3## wherein alkyl in the above groups contains 1 to 4 carbons; at least one of R 1 and R 2 being alkylamino or dialkylamino; R 3 is hydrogen, lower alkyl, benzyl or phenyl (optionally substituted with R 8 ), or ##STR4## (wherein R 6 is amino, alkylamino or dialkylamino, and R 7 is alkyl); and R 4 , R 5 and R 8 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl.

Inventors

  • 👤 George C. Rovnyak
  • 👤 B. Richard Vogt

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 06:22
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/02; C07D487/04

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 171 words
Compounds of the structure ##STR35## wherein R 1 is alkylamino, dialkylamino, or ##STR36## R 2 is alkylamino, dialkylamino, or ##STR37## the alkyl moiety in the above R 1 and R 2 groups having from 1 to 8 carbons; R 3 is hydrogen, lower alkyl, benzyl, phenyl or phenyl substituted by a single R 8 radical, ##STR38## (wherein R 6 is amino, alkylamino having 1 to 4 carbons, or dialkylamino having 1 to 4 carbons in each alkyl, and R 7 is alkyl of 1 to 4 carbons), with the proviso that at least one of R 1 or R 2 is alkylamino or dialkylamino; p1 R 4 , R 5 and R 8 may be the same or different and are hydrogen, lower alkyl of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, hydroxy, alkanoyloxy of 2 to 5 carbons, ##STR39## (wherein X 1 is hydrogen, lower alkoxy of 1 to 4 carbons), hydroxy, Cl, F, Br, CF 3 or NO 2 , and physiologically acceptable salts thereof.
Claim 2
Dependent Claim 171 words
Compounds of the structure ##STR35## wherein R 1 is alkylamino, dialkylamino, or ##STR36## R 2 is alkylamino, dialkylamino, or ##STR37## the alkyl moiety in the above R 1 and R 2 groups having from 1 to 8 carbons; R 3 is hydrogen, lower alkyl, benzyl, phenyl or phenyl substituted by a single R 8 radical, ##STR38## (wherein R 6 is amino, alkylamino having 1 to 4 carbons, or dialkylamino having 1 to 4 carbons in each alkyl, and R 7 is alkyl of 1 to 4 carbons), with the proviso that at least one of R 1 or R 2 is alkylamino or dialkylamino; p1 R 4 , R 5 and R 8 may be the same or different and are hydrogen, lower alkyl of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, hydroxy, alkanoyloxy of 2 to 5 carbons, ##STR39## (wherein X 1 is hydrogen, lower alkoxy of 1 to 4 carbons), hydroxy, Cl, F, Br, CF 3 or NO 2 , and physiologically acceptable salts thereof.
Claim 3
Dependent Claim 13 words
The compound of claim 1 wherein R 1 or R 2 is alkylamino.
Claim 4
Dependent Claim 13 words
The compound of claim 1 wherein R 1 or R 2 is dialkylamino.
Claim 5
Dependent Claim 10 words
The compound of claim 1 wherein R 1 is alkylamino.
Claim 6
Dependent Claim 10 words
The compound of claim 1 wherein R 1 is dialkylamino.
Claim 7
Dependent Claim 13 words
The compound of claim 1 wherein R 1 or R 2 is ##STR40##
Claim 8
Dependent Claim 10 words
The compound of claim 1 wherein R 2 is ##STR41##
Claim 9
Dependent Claim 25 words
The compound of claim 1 wherein R 3 is hydrogen, lower alkyl, benzyl or phenyl and R 1 or R 2 is alkylamino or dialkylamino.
Claim 10
Dependent Claim 23 words
The compound of claim 1 wherein R 3 is ##STR42## wherein R 6 is amino, alkylamino or dialkylamino and R 7 is alkyl.
Claim 11
Dependent Claim 16 words
The compound of claim 1 wherein R 3 , R 4 and R 5 are hydrogen.
Claim 12
Dependent Claim 12 words
The compound of claim 1 having the name 1-(diethylamino)-6-[1-(diethylamino)-3-methoxy-3-oxo-1-propenyl]-5,6-dihydro-5-oxo-pyrazolo[1,5-c]quinazoline-2-carboxylic acid, methyl ester.
Claim 13
Dependent Claim 27 words
A pharmaceutical composition for use in treating allergic conditions comprising a therapeutic amount of a compound as defined in claim 1 and a pharmaceutically acceptable carrier therefor.
Claim 14
Dependent Claim 26 words
A method for treating allergic conditions in mammals, which comprises administering to the mammalian host a therapeutic amount of a compound as defined in claim 1.

References Cited (Backward Citations)

US3171740A Cited
US3313815A Cited
US3531482A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-08-28 1982-02-27 1982-08-29 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-08-28 1986-02-27 1986-08-29 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-08-28 1990-02-27 1990-08-29 $7700.00 Window Closed / Lapsed

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