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US4232024A Expired / Lapsed US ⏱️ 0.0 years remaining

1-Oxo-1H-pyrimido[6,1-b]benzthiazole derivatives

Assignee: Roche Diagnostics GmbH
•
Filing: 1979-02-26
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Granted: 1980-11-04
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Expires: 1999-02-26
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Abstract

Abstract Anti-allergy novel 1-oxo-1H-pyrimido[6,1-b]benzthiazole derivatives of the formula <IMAGE> wherein R1, R2, R3 and R4 each independently is hydrogen, halogen, hydroxy, nitro, trifluoromethyl, or lower alkyl, alkoxy or alkylthio, or R2 and R3 together are alkylenedioxy, and X is hydroxy, alkoxy or tetrazolyl-5-amino, or salts thereof, as well as their production by saponification of <IMAGE> to form <IMAGE> or tautomers thereof, followed by acidification.

Inventors

  • 👤 Werner Winter
  • 👤 Herman Hindermayr
  • 👤 Egon Roesch
  • 👤 Androniki Roesch
  • 👤 Otto-Henning Wilhelms

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-01 21:07
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/52; C07D239/54; C07D239/545; C07D239/557; A; A61; A61P; A61P37/00; A61P37/08; C07D513/00; C07D513/02; C07D513/04; C07D513/12; C07D513/14

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 72 words
A 1-oxo-1H-pyrimido[6,1-b]benzthiazole of the formula ##STR8## wherein R 1 , R 2 , R 3 and R 4 each independently is hydrogen, halogen, hydroxy, nitro, trifluoromethyl, or alkyl, alkoxy or alkylthio containing up to 6 carbon atoms, or R 2 and R 3 together are alkylenedioxy containing up up to 3 carbon atoms, and X is hydroxy, alkoxy containing up to 6 carbon atoms or tetrazolyl-5-amino, or a pharmacologically acceptable salt thereof.
Claim 2
Dependent Claim 72 words
A 1-oxo-1H-pyrimido[6,1-b]benzthiazole of the formula ##STR8## wherein R 1 , R 2 , R 3 and R 4 each independently is hydrogen, halogen, hydroxy, nitro, trifluoromethyl, or alkyl, alkoxy or alkylthio containing up to 6 carbon atoms, or R 2 and R 3 together are alkylenedioxy containing up up to 3 carbon atoms, and X is hydroxy, alkoxy containing up to 6 carbon atoms or tetrazolyl-5-amino, or a pharmacologically acceptable salt thereof.
Claim 3
Dependent Claim 59 words
A compound according to claim 1, wherein R 1 , R 2 , R 3 and R 4 each independently is hydrogen, halogen, hydroxy, nitro, trifluoromethyl, or alkyl, alkoxy or alkylthio of up to 4 carbon atoms, or R 2 and R 3 together are methylenedioxy, and X is hydroxy, alkoxy of up to 4 carbon atoms or tetrazolyl-5-amino.
Claim 4
Dependent Claim 16 words
A compound according to claim 1, wherein such compound is 7-methoxy-1-oxo-1H-pyrimido[6,1-b]benzthiazole-4-carboxylic acid of the formula ##STR9##
Claim 5
Dependent Claim 16 words
A compound according to claim 1, wherein such compound is 7,8-dimethyl-1-oxo-1H-pyrimido[6,1-b]benzthiazole-4-carboxylic acid of the formula ##STR10##
Claim 6
Dependent Claim 16 words
A compound according to claim 1, wherein such compound is 7-methyl-1-oxo-1H-pyrimido[6,1-b]benzthiazole-4-carboxylic acid of the formula ##STR11##
Claim 7
Dependent Claim 16 words
A compound according to claim 1, wherein such compound is 6,8-dimethyl-7-methoxy-1-oxo-1H-pyrimido[6,1-b]benzthiazole-4-carboxylic acid of the formula ##STR12##
Claim 8
Dependent Claim 10 words
A compound according to claim 1, wherein X is hydroxy.
Claim 9
Dependent Claim 21 words
An anti-allergy pharmaceutical composition comprising a physiologically acceptable diluent and an anti-allergically effective amount of a compound according to claim 1.
Claim 10
Dependent Claim 26 words
A method of inhibiting an allergic rection in a patient comprising administering to such patient an anti-allergically effective amount of a compound according to claim 1.
Claim 11
Dependent Claim 19 words
The method according to claim 9, wherein such compound is 7-methoxy-1-oxo-1H-pyrimido[6,1-b]benzthiazole-4-carboxylic acid, 7,8-dimethyl-1-oxo-1H-pyrimido[6,1-b]benzthiazole-4-carboxylic acid, 7-methyl-1-oxo-1H-pyrimido[6,1-b]benzthiazole-4-carboxylic acid, or 6,8-dimethyl-7-methoxy-1-oxo-1H-pyrimido[6,1-b]benzthiazole-4-carboxylic acid.

References Cited (Backward Citations)

US3538086A Cited
DE2126148A1 Cited
US4041163A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1983-11-04 1984-05-05 1984-11-04 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1987-11-04 1988-05-05 1988-11-04 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1991-11-04 1992-05-05 1992-11-04 $7700.00 Window Closed / Lapsed

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