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1. WO1996003385 - 3,4-SUBSTITUTED PYRAZOLES FOR THE TREATMENT OF INFLAMMATION

Publication Number WO/1996/003385
Publication Date 08.02.1996
International Application No. PCT/US1995/008788
International Filing Date 20.07.1995
Chapter 2 Demand Filed 06.02.1996
IPC
C07D 231/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
12with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
CPC
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
C07D 231/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
12with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
Applicants
  • G.D. SEARLE & CO. [US/US]; Corporate Patent Dept. P.O. Box 5110 Chicago, IL 60680-5110, US (AllExceptUS)
  • LEE, Len, F. [US/US]; US (UsOnly)
  • PENNING, Thomas, D. [US/US]; US (UsOnly)
  • KRAMER, Steven, W. [US/US]; US (UsOnly)
  • TALLEY, John, J. [US/US]; US (UsOnly)
Inventors
  • LEE, Len, F.; US
  • PENNING, Thomas, D.; US
  • KRAMER, Steven, W.; US
  • TALLEY, John, J.; US
Agents
  • BULOCK, Joseph, W. ; G.D. Searle & Co. Corporate Patent Dept. P.O. Box 5110 Chicago, IL 60680-5110, US
  • BEIL, Hans, Christian; Postfach 80 01 40 Adelonstrasse 58 D-65901 Frankfurt am Main, DE
Priority Data
08/278,29721.07.1994US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 3,4-SUBSTITUTED PYRAZOLES FOR THE TREATMENT OF INFLAMMATION
(FR) PYRAZOLES 3,4-SUBSTITUEES DESTINEES AU TRAITEMENT DES INFLAMMATIONS
Abstract
(EN)
A class of pyrazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), wherein R1 is selected from alkyl, aralkyl, alkynyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl, arylaminocarbonylalkyl, heterocyclicalkyl, and alkoxycarbonylalkyl; wherein R3 is aryl optionally substituted at a substitutable position with one or more radicals independently selected from halo, alkylthio, alkylsulfinyl, alkyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino, heterocyclo and nitro; wherein R4 is haloalkyl; and wherein R5 is selected from alkyl and amino; or a pharmaceutically acceptable salt thereof.
(FR)
On décrit une classe de composés ou leurs sels pharmacologiquement acceptables, à base de pyrazolyle, utiles pour traiter des inflammations et des troubles en découlant. Les composés présentant un intérêt particulier sont définis par la formule (II), où R1 est choisi parmi alkyle, arakyle, alkynyle, cyanoalkyle, carboxyalkyle, aminocarbonylalkyle, arylaminocarbonylalkyle, alkyle hétérocyclique et alcoxycarbonylalkyle; R3 représente aryle éventuellement substitué en une position substituable avec un ou plusieurs radicaux choisis indépendemment parmi halo, alkylthio, alkylsulfinyle, alkyle, cyano, carboxyle, alcoxycarbonyle, aminocarbonyle, alkylaminocarbonyle, arylaminocarbonyle, N-alkyle-N-arylamonicarbonyle, haloalkyle, hydroxyle, alcoxy, hydroxyalkyle, alcoxyalkyle, haloalcoxy, amino, alkylamino, arylamino, hétérocyclo et nitro; R4 représente haloalkyle, et R5 est choisi entre alkyle et amino.
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