OMEGA-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS
a technology of aryl ureas and octyl aryl ureas, which is applied in the direction of heterocyclic compound active ingredients, biocide, drug compositions, etc., can solve the problems of compound structure-related toxicity, no marketed pharmaceutical agent is able to prevent or slow cartilage loss, etc., and achieves the effect of increasing the viscosity of the matrix
Inactive Publication Date: 2009-05-07
RIEDL BERND +10
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No marketed pharmaceutical agent is able to prevent or slow this cartilage loss, although nonsteroidal antiinflammatory drugs (NSAIDs) have been given to control pain and swelling.
The end result of these diseases is total loss of joint function which is only treatable by joint replacement surgery.
Mol. Eng. 1995, 5, 143, and references therein), causing concern that these compounds may display structure-related toxicity (Howard-Martin et al.
Method used
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[0064]All reactions were performed in flame-dried or oven-dried glassware under a positive pressure of dry argon or dry nitrogen, and were stirred magnetically unless otherwise indicated. Sensitive liquids and solutions were transferred via syringe or cannula, and introduced into reaction vessels through rubber septa. Unless otherwise stated, the term ‘concentration under reduced pressure’ refers to use of a Buchi rotary evaporator at approximately 15 mmHg. Unless otherwise stated, the term ‘under high vacuum’ refers to a vacuum of 0.4-1.0 mmHg.
[0065]All temperatures are reported uncorrected in degrees Celsius (° C.). Unless otherwise indicated, all parts and percentages are by weight.
[0066]Commercial grade reagents and solvents were used without further purification. N-cyclohexyl-N′-(methylpolystyrene)carbodiimide was purchased from Calbiochem-Novabiochem Corp. 3-tert-Butylaniline, 5-tert-butyl-2-methoxyaniline, 4-bromo-3-(trifluoromethyl)aniline, 4-chloro-3-(trifluoromethyl)anilin...
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Abstract
This invention relates to the use of a group of aryl ureas in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This is a continuation-in-part of Ser. No. 09 / 257,265 filed Feb. 25, 1999 and a continuation-in-part of Ser. No. 60 / 115,878 filed Jan. 13, 1999.FIELD OF THE INVENTION[0002]This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.BACKGROUND OF THE INVENTION[0003]Two classes of effector molecules which are critical for the progression of rheumatoid arthritis are pro-inflammatory cytokines and tissue degrading proteases. Recently, a family of kinases was described which is instrumental in controlling the transcription and translation of the structural genes coding for these effector molecules.[0004]The mitogen-activated protein (MAP) kinase family is made up of a series of structurally related proline-directed serine / threonine kinases which are activated either by growth factors (such as EGF) and phorbol ...
Claims
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IPC IPC(8): A61K31/17A61K31/4035A61K31/4412A61K31/5375A61K31/495A61K31/496A61K31/4453A61K31/341A61K31/40A61P35/00A61P19/00A61K31/18C07D295/12A61K31/24A61K31/44A61K31/4439A61K31/535A61K31/5377C07C275/36C07D207/09C07D209/46C07D209/48C07D213/64C07D213/75C07D213/81C07D295/18C07D307/14C07D401/12
CPCA61K31/17A61K31/18A61K31/24A61K31/341A61K31/40A61K31/4035A61K31/5377A61K31/4439A61K31/4453A61K31/495A61K31/496A61K31/535A61K31/5375A61K31/44A61P19/00A61P19/02A61P35/00Y02A50/30
Inventor RIEDL, BERNDDUMAS, JACQUESKHIRE, UDAYLOWINGER, TIMOTHY B.SCOTT, WILLIAM J.SMITH, ROGER A.WOOD, JILL E.MONAHAN, MARY-KATHERINENATERO, REINARENICK, JOELSIBLEY, ROBERT N.
Owner RIEDL BERND