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US4946855A Expired / Lapsed US ⏱️ 0.0 years remaining

Carboxamide derivatives having tetrazole and thiazole rings and their use

Assignee: Sawai Pharmaceutical Co Ltd
•
Filing: 1988-11-28
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Granted: 1990-08-07
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Expires: 2008-11-28
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Abstract

Abstract A compound of the formula: ##STR1## wherein the free valency of the groups A-, R- and --X--Y-- is attached to any of 2-, 4- and 5- positions of the thiazol ring, A is a C 1-6 alkyl group, an aryl group which is unsubstituted or substituted with at least one substituent selected from the group consisting of hydroxy C 1-6 alkoxy, aryl-(C 1-6 )alkoxy, halo-(C 1-6 )alkyl, halogen, and nitro, or 5- or 6-membered heterocyclic group containing at least one hetero atom selected from oxygen, nitrogen and sulfur, or a condensed heterocyclic group consisting of a heterocycle as defined above and a benzene nucleus, these two heterocyclic groups being unsubstituted or substituted with at least one substituent selected from halogen, R is hydrogen or a C 1-6 alkyl group, X is --CO--or --NH--, and Y is --NH--or --CO--, with the proviso that (a) X and Y cannot be the same group, and (b) when X is --CO--and Y is --NH--, the group --X--Y--is attached to 2- or 5-position, or a pharmaceutically acceptable salt thereof are nobel and useful as antiallergic.

Inventors

  • 👤 Junji Yoshinaga
  • 👤 Takeshi Shogaki
  • 👤 Takao Kakita
  • 👤 Hiromi Ozeki
  • 👤 Yoshiko Kato

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 20:07
CPC Classifications
C; C07; C07D; C07D417/00; C07D417/02; C07D417/12; C07D417/14

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 163 words
The compound which is represented by the formula: ##STR63## wherein A is a C 1-6 alkyl group, an aryl group having 6 to 10 ring carbon atoms which is unsubstituted or substituted with at least one substituent selected from the group consisting of hydroxy, C 1-6 alkoxy, aryl-(C 1-6 ) alkoxy, halo-(C 1-6 ) alkyl, halogen and nitro, or 5-membered heterocyclic group having from 1 to 4 ring carbon atoms containing at least one hetero atom selected from oxygen, nitrogen and sulfur, or a condensed heterocyclic group consisting of a heterocycle as defined above and benzene nucleus, or a 6-membered heterocyclic group having from 1 to 5 ring carbon atoms containing at least one hetero atom selected from oxygen, nitrogen, and sulfur, or a condensed heterocyclic group consisting of a heterocycle as defined above and a benzene nucleus, these two heterocyclic groups being unsubstituted or substituted with at least one substituent selected from halogen, R is hydrogen or a C 1-6 alkyl group.
Claim 2
Dependent Claim 163 words
The compound which is represented by the formula: ##STR63## wherein A is a C 1-6 alkyl group, an aryl group having 6 to 10 ring carbon atoms which is unsubstituted or substituted with at least one substituent selected from the group consisting of hydroxy, C 1-6 alkoxy, aryl-(C 1-6 ) alkoxy, halo-(C 1-6 ) alkyl, halogen and nitro, or 5-membered heterocyclic group having from 1 to 4 ring carbon atoms containing at least one hetero atom selected from oxygen, nitrogen and sulfur, or a condensed heterocyclic group consisting of a heterocycle as defined above and benzene nucleus, or a 6-membered heterocyclic group having from 1 to 5 ring carbon atoms containing at least one hetero atom selected from oxygen, nitrogen, and sulfur, or a condensed heterocyclic group consisting of a heterocycle as defined above and a benzene nucleus, these two heterocyclic groups being unsubstituted or substituted with at least one substituent selected from halogen, R is hydrogen or a C 1-6 alkyl group.
Claim 3
Dependent Claim 35 words
The compound of claim 1, in which A is methyl, phenyl, methylphenyl, (1-methylethyl)phenyl, (1,1-dimethylethyl)phenyl, naphtyl, hydroxyphenyl, methoxyphenyl, dimethoxyphenyl, trimethoxyphenyl, benzyloxyphenyl, trifluoromethylphenyl, chlorophenyl, nitrophenyl, pyridyl, furyl, thienyl, or quinolyl, and R is hydrogen, methyl or 1-methylethyl.
Claim 4
Dependent Claim 132 words
The compound which is represented by the formula: ##STR64## wherein A is an aryl group having from 6 to 12 ring carbon atoms which is unsubstituted or substituted with at least one substituent selected from the group consisting of C 1-6 alkoxy, aryl-(C 1-6 ) alkoxy, halo-(C 1-6 ) alkyl, halogen, and nitro, or 5-membered heterocyclic group having from 1 to 4 ring carbon atoms containing at least one hetero atom selected from oxygen, nitrogen and sulfur, or 6-membered heterocyclic groups having 1 to 5 ring carbon atoms containing at least one hetero atom selected from oxygen, nitrogen and sulfur, these two heterocyclic groups being unsubstituted or substituted with at least one substituent selected from halogen, R is hydrogen or a C 1-6 alkyl group, X is --NH--, and Y is --CO--.
Claim 5
Dependent Claim 132 words
The compound which is represented by the formula: ##STR64## wherein A is an aryl group having from 6 to 12 ring carbon atoms which is unsubstituted or substituted with at least one substituent selected from the group consisting of C 1-6 alkoxy, aryl-(C 1-6 ) alkoxy, halo-(C 1-6 ) alkyl, halogen, and nitro, or 5-membered heterocyclic group having from 1 to 4 ring carbon atoms containing at least one hetero atom selected from oxygen, nitrogen and sulfur, or 6-membered heterocyclic groups having 1 to 5 ring carbon atoms containing at least one hetero atom selected from oxygen, nitrogen and sulfur, these two heterocyclic groups being unsubstituted or substituted with at least one substituent selected from halogen, R is hydrogen or a C 1-6 alkyl group, X is --NH--, and Y is --CO--.
Claim 6
Dependent Claim 33 words
The compound of claim 3, in which A is phenyl, methylphenyl, ethylphenyl, dimethylphenyl, biphenylyl, naphthyl, methoxyphenyl, dimethoxyphenyl, benzyloxyphenyl, chlorophenyl, trichlorophenyl, trifluoromethylphenyl, nitrophenyl, pyridyl, furyl, thienyl, or chlorothienyl, and R is hydrogen or methyl.
Claim 7
Dependent Claim 58 words
The compound which is represented by the formula: ##STR65## wherein A is an aryl group having from 6 to 10 ring carbon atoms which is unsubstituted or substituted with at least one substituent selected from the group consisting of C 1-6 alkoxy, halogen and nitro, R is C 1-6 alkyl group, X is --NH--, and Y is --CO--.
Claim 8
Dependent Claim 58 words
The compound which is represented by the formula: ##STR65## wherein A is an aryl group having from 6 to 10 ring carbon atoms which is unsubstituted or substituted with at least one substituent selected from the group consisting of C 1-6 alkoxy, halogen and nitro, R is C 1-6 alkyl group, X is --NH--, and Y is --CO--.
Claim 9
Dependent Claim 21 words
The compound of claim 5, in which A is phenyl, methylphenyl, methoxyphenyl, dimethoxyphenyl, trimethoxyphenyl, chlorophenyl, or nitrophenyl, and R is methyl.
Claim 10
Dependent Claim 39 words
A Pharmaceutical composition comprising a therapeutically or prophylactically effective amount for the treatment of allergic diseases of at least one compound of claim 1 or a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier or diluent.
Claim 11
Dependent Claim 39 words
A Pharmaceutical composition comprising a therapeutically or prophylactically effective amount for the treatment of allergic diseases of at least one compound of claim 3 or a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier or diluent.
Claim 12
Dependent Claim 39 words
A Pharmaceutical composition comprising a therapeutically or prophylactically effective amount for the treatment of allergic diseases of at least one compound of claim 5 or a pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable carrier or diluent.
Claim 13
Dependent Claim 37 words
A method of treating allergic diseases which comprises administering a therapeutically or prophylactically effective amount of at least one compound of claim 1 or a pharmaceutically acceptable salt thereof to a subject in need of such treatment.
Claim 14
Dependent Claim 37 words
A method of treating allergic diseases which comprises administering a therapeutically or prophylactically effective amount of at least one compound of claim 3 or a pharmaceutically acceptable salt thereof to a subject in need of such treatment.
Claim 15
Dependent Claim 37 words
A method of treating allergic diseases which comprises administering a therapeutically or prophylactically effective amount of at least one compound of claim 5 or a pharmaceutically acceptable salt thereof to a subject in need of such treatment.

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USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1993-08-06 1994-02-05 1994-08-07 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1997-08-06 1998-02-05 1998-08-07 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2001-08-06 2002-02-05 2002-08-07 $7700.00 Window Closed / Lapsed

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