US5134142A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pyrazole derivatives, and pharmaceutical composition comprising the same
Assignee: Astellas Pharma Inc
•
Filing: 1990-09-14
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Granted: 1992-07-28
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Expires: 2010-09-14
Abstract
Abstract The present invention concerns pyrazole derivatives of formula: ##STR1## used for the treatment of inflammation, pain, thrombosis and rheumatism.
Inventors
- 👤 Masaaki Matsuo
- 👤 Kiyoshi Tsuji
- 👤 Nobukiyo Konishi
- 👤 Katsuya Nakamura
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 03:03
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/10; C07D231/12; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/415; A61P; A61P1/00; A61P1/02; A61P25/00; A61P25/04; A61P29/00; C07D231/14; C07D401/00; C07D401/02; C07D401/04; C07D403/00; C07D403/02; C07D403/04; C07D409/00; C07D409/02; C07D409/04
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
198 words
A compound of the formula: ##STR5## wherein R 1 is aryl which may be substituted with substituent(s) selected from the group consisting of lower alkyl, halogen, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, hydroxy, lower alkylsulfonyloxy, nitro, amino, lower alkylamino, acylamino and lower alkyl(acyl)amino; or a pyridyl group; R 2 is methyl substituted with amino, lower alkylamino, halogen or acyloxy; acyl; cyano; halogen; lower alkylthio; lower alkylsulfinyl; or a tetrazolyl group; and R 3 is aryl substituted with lower alkyl, lower alkylthio, lower alkylsulfinyl, halogen, amino, lower alkylamino, acylamino, lower alkyl(acyl)amino, lower alkoxy, cyano, hydroxy or acyl; or a thienyl group which may be substituted with lower alkylthio, lower alkysulfinyl or lower alkylsulfonyl; provided that when R 2 is carboxy, esterified carboxy or tri(halo)methyl, then R 3 is aryl substituted with lower alkylthio, lower alkylsulfinyl, amino, lower alkylamino, acylamino, lower alkyl(acyl)amino, hydroxy or acyl; or a thienyl group substituted with lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl, or R 1 is aryl substituted with substituent(s) selected from the group consisting of lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, hydroxy, lower alkylsulfonyloxy, nitro, amino, lower alkylamino, acylamino and lower alkyl(acyl)amino; or a pyridyl group or pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
198 words
A compound of the formula: ##STR5## wherein R 1 is aryl which may be substituted with substituent(s) selected from the group consisting of lower alkyl, halogen, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, hydroxy, lower alkylsulfonyloxy, nitro, amino, lower alkylamino, acylamino and lower alkyl(acyl)amino; or a pyridyl group; R 2 is methyl substituted with amino, lower alkylamino, halogen or acyloxy; acyl; cyano; halogen; lower alkylthio; lower alkylsulfinyl; or a tetrazolyl group; and R 3 is aryl substituted with lower alkyl, lower alkylthio, lower alkylsulfinyl, halogen, amino, lower alkylamino, acylamino, lower alkyl(acyl)amino, lower alkoxy, cyano, hydroxy or acyl; or a thienyl group which may be substituted with lower alkylthio, lower alkysulfinyl or lower alkylsulfonyl; provided that when R 2 is carboxy, esterified carboxy or tri(halo)methyl, then R 3 is aryl substituted with lower alkylthio, lower alkylsulfinyl, amino, lower alkylamino, acylamino, lower alkyl(acyl)amino, hydroxy or acyl; or a thienyl group substituted with lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl, or R 1 is aryl substituted with substituent(s) selected from the group consisting of lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, hydroxy, lower alkylsulfonyloxy, nitro, amino, lower alkylamino, acylamino and lower alkyl(acyl)amino; or a pyridyl group or pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
54 words
A compound according to claim 1, wherein R 2 is methyl substituted with amino, lower alkylamino or acyloxy; carbamoyl optionally substituted with substituent(s) selected from the group consisting of lower alkyl, cyclo(lower)alkyl, aryl and hydroxy; lower alkanoyl optionally substituted with lower alkoxy; pyrrolidinylcarbonyl; n-methylpiperazinylcarbonyl; cyano; halogen; lower alkylthio; lower alkylsulfinyl; lower alkylsulfonyl; or tetrazolyl.
Claim 4
Dependent Claim
26 words
A compound according to claim 2, wherein R 3 is aryl or thienyl, each of which is substituted with lower alkylthio, lower alkylsulfinyl, or lower alkylsulfonyl.
Claim 5
Dependent Claim
20 words
A compound according to claim 3, wherein R 3 is aryl substituted with lower alkylthio, lower alkylsulfinyl, or lower alkylsulfonyl.
Claim 6
Dependent Claim
32 words
A compound according to claim 4, wherein R 1 is phenyl substituted with halogen, R 2 is cyano and R 3 is phenyl substituted with lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl.
Claim 7
Dependent Claim
8 words
A compound of claim 5, which is 1-(4-fluorophenyl)-5-[4-(methylsulfonyl)phenyl]pyrazole-3-carbonitrile.
Claim 8
Dependent Claim
8 words
A compound of claim 5, which is 1-(4-fluorophenyl)-5-[4-methylsulfinyl)phenyl]pyrazole-3-carbonitrile.
Claim 9
Dependent Claim
24 words
A pharmaceutical composition comprising a compound of claim 1, as an active ingredient, in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient.
Claim 10
Dependent Claim
23 words
A method for therapeutic treatment of inflammation pain thrombois and rheumatism which comprises administering an effective amount of a compound of claim 1.
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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) | 1995-07-28 | 1996-01-27 | 1996-07-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-07-28 | 2000-01-27 | 2000-07-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-07-28 | 2004-01-27 | 2004-07-28 | $7700.00 | Window Closed / Lapsed |