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US4788205A Expired / Lapsed US ⏱️ 0.0 years remaining

Dihydropyridine anti-allergic and antiinflammatory agents

Assignee: Pfizer Inc
•
Filing: 1987-07-20
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Granted: 1988-11-29
•
Expires: 2007-07-20
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Abstract

Abstract Certain 4-aryl-5-carbamoyl-1,4-dihydropyridines useful in the treatment of allergic and inflammatory conditions in mammals.

Inventors

  • 👤 Kelvin Cooper
  • 👤 Michael J. Parry
  • 👤 Peter E. Cross
  • 👤 Kenneth Richardson

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 14:51
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/80; C07D211/82; C07D231/00; C07D231/02; C07D231/10; C07D231/12; A; A61; A61P; A61P37/00; A61P37/08; C07D211/84; C07D211/90; C07D233/00; C07D233/54; C07D233/56; C07D249/00; C07D249/02; C07D249/08; C07D417/00; C07D417/14

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 212 words
A compound of the formula ##STR61## or a pharmaceutically acceptable salt thereof, wherein R is phenyl, fluorophenyl, chlorophenyl, trifluoromethylphenyl, difluorophenyl, methylphenyl or methoxyphenyl; R 1 is hydrogen, alkyl having one to six carbon atoms, cycloalkyl having from three to seven carbon atoms, cycloalkylmethyl having four to eight carbon atoms, phenyl, phenylalkyl having seven to nine carbon atoms, indanyl, thenyl, pyridyl, methylpyridyl, picolyl, chloropyridyl, 2-thiazolyl, methyl-2-thiazolyl, dimethyl-2-thiazolyl, 2-benzothiazolyl, 6-alkoxy-2-benzothiazolyl said alkoxy having one to three carbon atoms, 1,3,4-thiadiazol-2-yl, 5-methyl-1,3,4-thiadiazol-2-yl, quinolyl, 3-isoxazolyl, 5-methyl-3-isoxazolyl, methylpyrazol-1-ylmethyl, or alpha-carboalkoxybenzyl said alkoxy having from one to three carbon atoms; R 2 is hydrogen or alkyl having one to six carbon atoms; R 1 and R 2 taken together with the nitrogen to which they are attached form a heterocyclic ring selected from piperidine, morpholine, thiomorpholine, piperazine or N-substituted piperazine where said substituent is alkyl having one to five carbon atoms, phenyl or alkanoyl having one to four carbon atoms; R 3 is alkyl having one to six carbon atoms or ethoxyalkyl having four to six carbon atoms; Y is alkylene having two to eight carbon atoms, having at least two carbon atoms in the chain linking X to the oxygen atom; and X is imidazol-1-yl optionally substituted with from one to three substituents selected from methyl and chloro.
Claim 2
Dependent Claim 212 words
A compound of the formula ##STR61## or a pharmaceutically acceptable salt thereof, wherein R is phenyl, fluorophenyl, chlorophenyl, trifluoromethylphenyl, difluorophenyl, methylphenyl or methoxyphenyl; R 1 is hydrogen, alkyl having one to six carbon atoms, cycloalkyl having from three to seven carbon atoms, cycloalkylmethyl having four to eight carbon atoms, phenyl, phenylalkyl having seven to nine carbon atoms, indanyl, thenyl, pyridyl, methylpyridyl, picolyl, chloropyridyl, 2-thiazolyl, methyl-2-thiazolyl, dimethyl-2-thiazolyl, 2-benzothiazolyl, 6-alkoxy-2-benzothiazolyl said alkoxy having one to three carbon atoms, 1,3,4-thiadiazol-2-yl, 5-methyl-1,3,4-thiadiazol-2-yl, quinolyl, 3-isoxazolyl, 5-methyl-3-isoxazolyl, methylpyrazol-1-ylmethyl, or alpha-carboalkoxybenzyl said alkoxy having from one to three carbon atoms; R 2 is hydrogen or alkyl having one to six carbon atoms; R 1 and R 2 taken together with the nitrogen to which they are attached form a heterocyclic ring selected from piperidine, morpholine, thiomorpholine, piperazine or N-substituted piperazine where said substituent is alkyl having one to five carbon atoms, phenyl or alkanoyl having one to four carbon atoms; R 3 is alkyl having one to six carbon atoms or ethoxyalkyl having four to six carbon atoms; Y is alkylene having two to eight carbon atoms, having at least two carbon atoms in the chain linking X to the oxygen atom; and X is imidazol-1-yl optionally substituted with from one to three substituents selected from methyl and chloro.
Claim 3
Dependent Claim 25 words
A compound of claim 1, wherein R is 2-chlorophenyl, Y is --(CH 2 ) 2 , R 3 is ethyl and R 2 is hydrogen.
Claim 4
Dependent Claim 14 words
The compound of claim 2, wherein X is 2,4,5,-trimethylimidazol-1-yl and R 1 is t-butyl.
Claim 5
Dependent Claim 14 words
The compound of claim 2, wherein X is 2,4,5,-timethylimidazol-1-yl and R 1 is 2-pyridyl.
Claim 6
Dependent Claim 14 words
The compound of claim 2, wherein X is 2,4,5,-trimethylimidazol-1-yl and R 1 is 6-methyl-2-pyridyl.
Claim 7
Dependent Claim 14 words
The compound of claim 2, wherein X is 2,4,5-trimethylimidazol-1-yl and R 1 is 2-thiazolyl.
Claim 8
Dependent Claim 14 words
The compound of claim 2, wherein X is 2,4,5-trimethylimidazol-1-yl and R 1 is 2-benzothiazolyl.
Claim 9
Dependent Claim 27 words
A method of treating an allergic condition in a mammal which comprises administering to said mammal an anti-allergic effective amount of a compound according to claim 1.
Claim 10
Dependent Claim 27 words
A method of treating an inflammatory condition in a mammal which comprises administering to said mammal an antiinflammatory effective amount of a compound according to claim 1.
Claim 11
Dependent Claim 22 words
A pharmaceutical composition comprising an anti-allergic effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier or diluent.
Claim 12
Dependent Claim 22 words
A pharmaceutical composition comprising an antiinflammatory effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier or diluent.

References Cited (Backward Citations)

US3867393A Cited
DE2228377A1 Cited
US4515799A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1991-11-29 1992-05-30 1992-11-29 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-11-29 1996-05-30 1996-11-29 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-11-29 2000-05-30 2000-11-29 $7700.00 Window Closed / Lapsed

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