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Benzopyrone derivatives exhibiting anti-allergic activity

Assignee: Roche Diagnostics GmbH
•
Filing: 1976-12-01
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Granted: 1978-05-30
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Expires: 1996-12-01
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Abstract

Abstract Benzopyrones of the formula <IMAGE> wherein R1 is a hydrogen or halogen atom or a hydroxyl, lower alkyl, alkoxy, alkylthio or trifluoromethyl radical, R2, R3, R4 and R5 each independently is hydrogen, a halogen atom, a hydroxyl radical, a lower alkyl or lower alkoxy radical, or a lower alkyl or lower alkoxy radical substituted by at least one of hydroxyl, halogen, mesyloxy or tosyloxy or by an oxirane, dioxane or dioxolane ring, A is a lower alkylene radical, and N IS 0, 1 OR 2, AND SALTS THEREOF EXHIBIT ANTI-ALLERGIC ACTIVITY.

Inventors

  • 👤 Werner Winter
  • 👤 Max Thiel
  • 👤 Kurt Stach, deceased
  • 👤 Androniki Roesch
  • 👤 administrator by Werner Plattner
  • 👤 Wolfgang Schaumann

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 11:59
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/10; C07D295/104; C07D295/108; A; A61; A61P; A61P37/00; A61P37/08; C07C; C07C45/00; C07C45/61; C07C45/67; C07C45/68; C07C45/70; C07C45/71; C07D295/14; C07D295/145; C07D295/15; C07D309/00; C07D309/02; C07D309/08; C07D309/10; C07D309/12; C07D311/00; C07D311/02; C07D311/04; C07D311/22; C07D317/00; C07D317/08; C07D317/10; C07D317/14; C07D317/18; C07D317/22

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 92 words
A benzopyrone of the formula ##STR8## wherein R 1 is a hydrogen or halogen atom or hydroxyl, lower alkyl, alkoxy, alkylthio or trifluoromethyl, R 2 , r 3 , r 4 and R 5 each independently is hydrogen, a halogen atom, hydroxyl, lower alkyl or lower alkoxy, or lower alkyl or lower alkoxy substituted by at least one of hydroxyl, halogen, mesyloxy or tosyloxy or by an oxirane, dioxane or dioxolane ring, A is lower alkylene, and n is 0, 1 or 2, or a salt thereof with a pharmacologically compatible acid.
Claim 2
Dependent Claim 92 words
A benzopyrone of the formula ##STR8## wherein R 1 is a hydrogen or halogen atom or hydroxyl, lower alkyl, alkoxy, alkylthio or trifluoromethyl, R 2 , r 3 , r 4 and R 5 each independently is hydrogen, a halogen atom, hydroxyl, lower alkyl or lower alkoxy, or lower alkyl or lower alkoxy substituted by at least one of hydroxyl, halogen, mesyloxy or tosyloxy or by an oxirane, dioxane or dioxolane ring, A is lower alkylene, and n is 0, 1 or 2, or a salt thereof with a pharmacologically compatible acid.
Claim 3
Dependent Claim 106 words
A benzopyrone according to claim 1, wherein R 1 is a hydrogen, fluorine, chlorine or bromine atom, or hydroxyl, trifluoromethyl, or alkyl, alkoxy or alkylthio containing up to 3 carbon atoms, R 2 , r 3 , r 4 and R 5 each independently is a hydrogen, fluorine, chlorine or bromine atom, or hydroxyl, alkyl or alkoxy containing up to 3 carbon atoms, or alkyl or alkoxy radical containing up to 3 carbon atoms and substituted by at least one of hydroxyl, fluorine, chlorine, bromine, mesyloxy, tosyloxy, oxiranyl, dioxanyl and dioxolanyl, A is alkylene of up to 4 carbon atoms, and n is 0 or 1.
Claim 4
Dependent Claim 19 words
A benzopyrone or a salt thereof according to claim 1 wherein said benzopyrone is 2-{2-[4-(2-methoxyphenyl)-piperazinyl-1]-ethyl}-5-methoxy-4-oxo-4H-1-benzopyran of the formula ##STR9##
Claim 5
Dependent Claim 19 words
A benzopyrone or a salt thereof according to claim 1 wherein said benzopyrone is 2-{2-[4-(3-methoxyphenyl)-piperazinyl-1]-ethyl}-5-methoxy-4-oxo-4H-1-benzopyran of the formula ##STR10##
Claim 6
Dependent Claim 19 words
A benzopyrone or a salt thereof according to claim 1 wherein said benzopyrone is 2-{2-[4-(2-methylphenyl)-piperazinyl-1]-ethyl}-5-methoxy-4-oxo-4H-1-benzopyran of the formula ##STR11##
Claim 7
Dependent Claim 19 words
A benzopyrone or a salt thereof according to claim 1 wherein said benzopyrone is 2-{2-[4-(2-methoxyphenyl)-piperazinyl-1]-ethyl}-5-(2,3-dihydroxypropoxy)-4-oxo-4H-1-benzopyran of the formula ##STR12##
Claim 8
Dependent Claim 19 words
A benzopyrone or a salt thereof according to claim 1 wherein said benzopyrone is 2-{2-[4-(2-methoxyphenyl)-piperazinyl-1]-ethyl}-5-(2-hydroxypropoxy)-4-oxo-4H-1-benzopyran of the formula ##STR13##
Claim 9
Dependent Claim 22 words
An anti-allergic composition comprising an anti-allergically effective amount of at least one benzopyrone according to claim 1, in admixture with a diluent.
Claim 10
Dependent Claim 26 words
A method of combating allergy in a patient comprising administering to said patient an anti-allergically effective amount of at least one benzopyrone according to claim 1.
Claim 11
Dependent Claim 24 words
The method according to claim 9, wherein such benzopyrone is 2-{2-[4-(2-methoxyphenyl)-piperazinyl-1]-ethyl}-5-methoxy-4-oxo-4H-1-benzopyran, 2-{2-[4-(3-methoxyphenyl)-piperazinyl-1-ethyl}-5-methoxy-4-oxo-4H-1-benzopyran, 2-{2-[4-(2-methylphenyl)-piperazinyl-1]-ethyl}-5-methoxy-4-oxo-4H-1-benzopyran, 2-{2-[4-(2-methoxyphenyl)-piperazinyl-1]-ethyl}-5-(2,3-dihydroxypropoxy)-4-oxo-4H-1-benzopyran, 2-{2-[4-(2-methoxyphenyl)-piperazinyl-1]-ethyl}-5-(2-hydroxypropoxy)-4-oxo-4H-1-benzopyran or a salt thereof with a pharmacologically compatible acid.

References Cited (Backward Citations)

US3410851A Cited
US4001280A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-05-29 1981-11-28 1982-05-30 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-05-29 1985-11-28 1986-05-30 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-05-29 1989-11-28 1990-05-30 $7700.00 Window Closed / Lapsed

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