US4826868A
Expired / Lapsed
US
⏱️ 0.0 years remaining
1,5-Diaryl-3-substituted pyrazoles pharmaceutical compositions and use
Assignee: Ortho Pharmaceutical Corp
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Filing: 1987-04-29
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Granted: 1989-05-02
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Expires: 2007-04-29
Abstract
Abstract 1,5-Diaryl-3-substituted pyrazoles, a method of their preparation, compositions containing the same and methods of their use are disclosed. The pyrazoles are useful in alleviating inflammatory and cardiovascular disorders in mammals.
Inventors
- 👤 Michael P. Wachter
- 👤 Michael P. Ferro
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 20:23
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/10; C07D231/12; A; A61; A61P; A61P11/00; A61P11/14; A61P17/00; A61P29/00; A61P37/00; A61P37/08; A61P9/00; A61P9/04; A61P9/10; C07C; C07C59/00; C07C59/40; C07C59/76; C07C59/84; C07C59/88; C07D403/00; C07D403/02; C07D403/12; C07D417/00; C07D417/02; C07D417/12
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
78 words
A compound having a structure that corresponds to the formula: ##STR44## wherein R 1 and R 3 are selected from the group consisting of halo, trifluoromethyl and methyl and X is selected from the group consisting of --C(O)--R 5 wherein R 5 is selected from the group consisting of --N(CH 3 )OH, --N(t-butyl)OH, --N(i-propyl)OH, --N(cyclohexyl)OH, --N(ethyl)OH and --N(phenyl)OH or R 5 is --NHCH 2 CO 2 H, or X is --CH 2 NH 2 , --C(O)H or --C(═NOH)H.
Claim 2
Dependent Claim
78 words
A compound having a structure that corresponds to the formula: ##STR44## wherein R 1 and R 3 are selected from the group consisting of halo, trifluoromethyl and methyl and X is selected from the group consisting of --C(O)--R 5 wherein R 5 is selected from the group consisting of --N(CH 3 )OH, --N(t-butyl)OH, --N(i-propyl)OH, --N(cyclohexyl)OH, --N(ethyl)OH and --N(phenyl)OH or R 5 is --NHCH 2 CO 2 H, or X is --CH 2 NH 2 , --C(O)H or --C(═NOH)H.
Claim 3
Dependent Claim
5 words
A compound which is 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-hydroxy-N-methylpropanamide.
Claim 4
Dependent Claim
5 words
A compound which is 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-hydroxy-N-methylpropanamide.
Claim 5
Dependent Claim
5 words
A compound which is 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-tert-butyl-N-hydroxypropanamide.
Claim 6
Dependent Claim
5 words
A compound which is 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-tert-butyl-N-hydroxypropanamide.
Claim 7
Dependent Claim
5 words
A compound which is N-carboxymethyl-3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-propanamide.
Claim 8
Dependent Claim
5 words
A compound which is N-carboxymethyl-3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-propanamide.
Claim 9
Dependent Claim
12 words
A compound selected from the group consisting of 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-hydroxy-N-isopropylpropanamide, 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-cyclohexyl-N-hydroxypropanamide, and 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-ethyl-N-hydroxypropanamide.
Claim 10
Dependent Claim
12 words
A compound selected from the group consisting of 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-hydroxy-N-isopropylpropanamide, 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-cyclohexyl-N-hydroxypropanamide, and 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-ethyl-N-hydroxypropanamide.
Claim 11
Dependent Claim
14 words
A compound selected from the group consisting of 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-hydroxy-N-phenylpropanamide, 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]propylamine, 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]propanal, 5-(4-chlorophenyl)-3-(3-oximino-propyl)-1-(4-methoxyphenyl)pyrazole and 3-(3-hydroxypropyl)-1-(4-methoxyphenyl)-5-(4-tolyl)pyrazole.
Claim 12
Dependent Claim
14 words
A compound selected from the group consisting of 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]-N-hydroxy-N-phenylpropanamide, 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]propylamine, 3-[5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-pyrazolyl]propanal, 5-(4-chlorophenyl)-3-(3-oximino-propyl)-1-(4-methoxyphenyl)pyrazole and 3-(3-hydroxypropyl)-1-(4-methoxyphenyl)-5-(4-tolyl)pyrazole.
Claim 13
Dependent Claim
6 words
A compound which is 3-[1-(4-methoxyphenyl)-5-(4-methylphenyl)-3-pyrazolyl]-N-hydroxy-N-methyl propanamide.
Claim 14
Dependent Claim
6 words
A compound which is 3-[1-(4-methoxyphenyl)-5-(4-methylphenyl)-3-pyrazolyl]-N-hydroxy-N-methyl propanamide.
Claim 15
Dependent Claim
29 words
A compound having a structure that corresponds to the formula: ##STR45## wherein R 1 and R 3 are selected from the group consisting of halo, trifluoromethyl, methyl and methoxy.
Claim 16
Dependent Claim
29 words
A compound having a structure that corresponds to the formula: ##STR45## wherein R 1 and R 3 are selected from the group consisting of halo, trifluoromethyl, methyl and methoxy.
Claim 17
Dependent Claim
8 words
A compound of claim 8 which is 5-(4-chlorophenyl)-3-(3-hydroxypropyl)-1-(4-methoxyphenyl)pyrazole.
Claim 18
Dependent Claim
9 words
A compound of claim 8 which is 5-(4-trifluoromethylphenyl)-3-(3-hydroxypropyl)-1-(4-methoxyphenyl) pyrazole.
Claim 19
Dependent Claim
9 words
A compound of claim 8 which is 1-(4-bromophenyl)-5-(4-chlorophenyl)-3-(3-hydroxypropyl) pyrazole.
Claim 20
Dependent Claim
42 words
A pharmaceutical composition for the alleviation of inflammatory and cardiovascular disorders in mammals for topical, oral, parental and aerosol administration, comprising an effective amount of a substituted pyrazole compound of claim 1 as the active ingredient dispersed in a pharmaceutically acceptable carrier.
Claim 21
Dependent Claim
24 words
A method for alleviating inflammation in a mammal exhibiting an inflammatory response comprising administering to said mammal a pharamaceutical composition according to claim 1.
Claim 22
Dependent Claim
25 words
A method for treating inflammatory conditions of skin, including psoriasis or other dermatitis, comprising administering to said mammal a pharmaceutical composition according to claim 1.
References Cited (Backward Citations)
US4095025A
Cited
US3974176A
Cited
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1992-05-01 | 1992-10-31 | 1993-05-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-05-01 | 1996-10-31 | 1997-05-02 | $3760.00 | Window Closed / Lapsed |
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