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US4083980A Expired / Lapsed US ⏱️ 0.0 years remaining

Derivatives of quinazolone

Assignee: Boehringer Ingelheim GmbH
•
Filing: 1976-12-15
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Granted: 1978-04-11
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Expires: 1996-12-15
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Abstract

Abstract Compounds of the formula <IMAGE> wherein A is -CH=CH-, -CH=N- or -S-, R1 is hydrogen, lower alkyl, lower alkoxy, amino, acetylamino, cyano, tetrazol-5-yl, -COR3 or a fused benzene ring, WHERE R3 is lower alkoxy, amino, hydroxyamino, tetrazol-5-yl-amino or, when R2 is other than hydrogen, also hydroxyl, and R2 is cyano, tetrazol-5-yl, -COR4 or, when R1 is cyano, tetrazol-5-yl or -COR3, also hydrogen, lower alkyl, lower alkoxy, amino, acetylamino or a fused benzene ring, WHERE R4 is lower alkoxy, amino, hydroxyl, hydroxyamino or tetrazol-5-yl-amino; NON-TOXIC, PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF; AND, WHEN R3 and/or R4 are hydroxyl, non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful primarily as antiallergics.

Inventors

  • 👤 Kurt Schromm
  • 👤 Anton Mentrup
  • 👤 Ernst-Otto Renth
  • 👤 Armin Fugner

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 02:51
CPC Classifications
C; C07; C07D; C07D471/00; C07D471/02; C07D471/04; A; A61; A61P; A61P11/00; A61P11/08; A61P37/00; A61P37/08; A61P9/00; A61P9/08; C07D513/00; C07D513/02; C07D513/04

Claims Analysis

Total Claims: 8
Claim 1
Independent Claim 118 words
A compound of the formula ##STR28## wherein R 1 is hydrogen, lower alkyl, lower alkoxy, amino, acetylamino, cyano, tetrazol-5-yl, --COR 3 or a fused benzene ring, where R 3 is lower alkoxy, amino, hydroxyamino, tetrazol-5-yl-amino or, when R 2 is other than hydrogen, also hydroxyl; and R 2 is cyano, tetrazol-5-yl, --COR 4 or, when R 1 is cyano, tetrazol-5-yl or --COR 3 , also hydrogen, lower alkyl, lower alkoxy, amino, acetylamino or a fused benzene ring, where R 4 is lower alkoxy, amino, hydroxyl, hydroxy-amino or tetrazol-5-yl-amino; a non-toxic, pharmacologically acceptable acid addition salt thereof; or, when R 3 and/or R 4 are hydroxyl, a non-toxic, pharmacologically acceptable salt thereof formed with an inorganic or organic base.
Claim 2
Dependent Claim 118 words
A compound of the formula ##STR28## wherein R 1 is hydrogen, lower alkyl, lower alkoxy, amino, acetylamino, cyano, tetrazol-5-yl, --COR 3 or a fused benzene ring, where R 3 is lower alkoxy, amino, hydroxyamino, tetrazol-5-yl-amino or, when R 2 is other than hydrogen, also hydroxyl; and R 2 is cyano, tetrazol-5-yl, --COR 4 or, when R 1 is cyano, tetrazol-5-yl or --COR 3 , also hydrogen, lower alkyl, lower alkoxy, amino, acetylamino or a fused benzene ring, where R 4 is lower alkoxy, amino, hydroxyl, hydroxy-amino or tetrazol-5-yl-amino; a non-toxic, pharmacologically acceptable acid addition salt thereof; or, when R 3 and/or R 4 are hydroxyl, a non-toxic, pharmacologically acceptable salt thereof formed with an inorganic or organic base.
Claim 3
Dependent Claim 33 words
A compound of claim 1, which is 6-oxo-6H-pyrimido [2,1-b] quinaoline-8-carboxylic acid; a non-toxic, pharmacologically acceptable acid addition acid thereof; or a non-toxic, pharmacologically acceptable salt thereof formed with an inorganic or organic base.
Claim 4
Dependent Claim 10 words
The compound of claim 2, which is 6-oxo-6H-pyrimido [2,1-b]quinazoline-8-carboxylic acid.
Claim 5
Dependent Claim 12 words
The compound of claim 2, which is 6-oxo-6H-pyrimido [2,1-b] quinazoline-8-carboxylic acid hydrochloride.
Claim 6
Dependent Claim 16 words
The compound of claim 2 which, which is the sodium salt of 6-oxo-6H-pyrimido [2,1-b] quinazoline-8-carboxylic acid.
Claim 7
Dependent Claim 22 words
An antiallergic pharmaceutical composition consisting essentially of an inert pharmaceutical carrier and an effective antiallergic amount of a compound of claim 1.
Claim 8
Dependent Claim 33 words
The method of suppressing allergic reactions in warm-blooded animals, which comprises topically, perorally, parenterally or by the respiratory route administering to said animal an effective antiallergic amount of a compound of claim 1.

References Cited (Backward Citations)

US3598823A Cited
US3833588A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-04-10 1981-10-10 1982-04-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-04-10 1985-10-10 1986-04-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-04-10 1989-10-10 1990-04-11 $7700.00 Window Closed / Lapsed

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