UY25856A1 - 4 AND 5 ALKYNYLXOXYDOLS AND 4 AND 5 ALKYNYLXOXYDOLES WHICH ARE USEFUL AS ANTI-INFLAMMATORY AGENTS - Google Patents

4 AND 5 ALKYNYLXOXYDOLS AND 4 AND 5 ALKYNYLXOXYDOLES WHICH ARE USEFUL AS ANTI-INFLAMMATORY AGENTS

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Publication number
UY25856A1
UY25856A1 UY25856A UY25856A UY25856A1 UY 25856 A1 UY25856 A1 UY 25856A1 UY 25856 A UY25856 A UY 25856A UY 25856 A UY25856 A UY 25856A UY 25856 A1 UY25856 A1 UY 25856A1
Authority
UY
Uruguay
Prior art keywords
conr6r7
cor4
coor4
halogen
useful
Prior art date
Application number
UY25856A
Other languages
Spanish (es)
Inventor
Kin-Chun Luk
Steven Gregory Mischke
Paige E Mahaney
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of UY25856A1 publication Critical patent/UY25856A1/en

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los 4- y 5-alquiniloxindoles así como 4- y 5-alqueniloxindoles que tienen la fórmula I (como: rac-(Z)-1,3-dihidro-4-[3-hidroxi-3-(4-metoxifenil)-1-propinil]-3-[(3-metoxi-1H-pirrol-2-il)metilen]-2H-indol-2-ona (H)) y II (como por ejemplo: (Z)-1,3-dihidro-5-etinil-3-[(1H-pirrol-2-il)metilen]-2H-indol-2-ona (SSS)) en donde R1 es alquilo inferior que esta sustituido por arilo, ariloxi, heteroarilo, heteroarilo R2 es H, OR4, OCOR4, COR4, COOR4, CONR6R7, NR6R7, halogeno NO2, CN, SO2R4, etc; R3 se selecciona entre H, OR4, COR4, COOR4, CONR6R7, halogeno, CN, perfluororalquilo, etc; X es =n o CH; y el enlace en lines de puntos representado por Z es opcional; R11 es H, COR4, COOR4, CONR6R7, alquilo inferior, cicloalquilo, heterociclo, arilo, etc; R12 es H, OR4, OCOR4, COR4, COOR4, CONR6R7, NR6R7, halogeno, NO2, CN, SO2R4, etc. Una composición farmacéutica que comprende como ingrediente activo un compuesto de fórmula l o ll y un vehiculo o excipiente farmacéuticamente aceptable. Uso de dichos compuestos para la preparación de un medicamento que inhiben y modulan proteína quinasas, en particular proteína quinasas JNK y son útiles como agentes antiinflamatorios, en particular en el tratamiento de la artritis reumatoide.The 4- and 5-alkynyloxyindoles as well as 4- and 5-alkenyloxyindoles having the formula I (such as: rac- (Z) -1,3-dihydro-4- [3-hydroxy-3- (4-methoxyphenyl) - 1-propynyl] -3 - [(3-methoxy-1H-pyrrol-2-yl) methylene] -2H-indole-2-one (H)) and II (such as: (Z) -1,3- dihydro-5-ethynyl-3 - [(1H-pyrrol-2-yl) methylene] -2H-indole-2-one (SSS)) where R1 is lower alkyl which is substituted by aryl, aryloxy, heteroaryl, heteroaryl R2 it is H, OR4, OCOR4, COR4, COOR4, CONR6R7, NR6R7, halogen NO2, CN, SO2R4, etc; R3 is selected from H, OR4, COR4, COOR4, CONR6R7, halogen, CN, perfluororalkyl, etc; X is = n or CH; and the link in dotted lines represented by Z is optional; R11 is H, COR4, COOR4, CONR6R7, lower alkyl, cycloalkyl, heterocycle, aryl, etc; R12 is H, OR4, OCOR4, COR4, COOR4, CONR6R7, NR6R7, halogen, NO2, CN, SO2R4, etc. A pharmaceutical composition comprising as an active ingredient a compound of formula I or II and a pharmaceutically acceptable carrier or excipient. Use of said compounds for the preparation of a medicine that inhibit and modulate protein kinases, in particular JNK protein kinases and are useful as anti-inflammatory agents, in particular in the treatment of rheumatoid arthritis.

UY25856A 1998-12-17 1999-12-16 4 AND 5 ALKYNYLXOXYDOLS AND 4 AND 5 ALKYNYLXOXYDOLES WHICH ARE USEFUL AS ANTI-INFLAMMATORY AGENTS UY25856A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US11258998P 1998-12-17 1998-12-17

Publications (1)

Publication Number Publication Date
UY25856A1 true UY25856A1 (en) 2001-07-31

Family

ID=27733543

Family Applications (1)

Application Number Title Priority Date Filing Date
UY25856A UY25856A1 (en) 1998-12-17 1999-12-16 4 AND 5 ALKYNYLXOXYDOLS AND 4 AND 5 ALKYNYLXOXYDOLES WHICH ARE USEFUL AS ANTI-INFLAMMATORY AGENTS

Country Status (5)

Country Link
AR (1) AR035156A1 (en)
CO (1) CO5261520A1 (en)
PE (1) PE20001354A1 (en)
UY (1) UY25856A1 (en)
ZA (1) ZA200104281B (en)

Also Published As

Publication number Publication date
CO5261520A1 (en) 2003-03-31
AR035156A1 (en) 2004-05-05
PE20001354A1 (en) 2000-11-29
ZA200104281B (en) 2002-08-26

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Legal Events

Date Code Title Description
109 Application deemed to be withdrawn

Effective date: 20091215