Publication number: 20070249691
Abstract: The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine, a polymorphic form or a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, optionally substituted C1-6alkyl, C(?O)—O—R5, C(?O)—NR6aR6b, C(?S)—NR6aR6b, S(?O)2—NR6aR6b or C(?O)—R7; R4 represents hydrogen or C1-6alkyl; n is 1, 2, 3, 4 or 5; Z represents a cyclic ring system. The invention also relates to processes for preparing the compounds of formula (I), their use as CCR2 antagonists and pharmaceutical compositions comprising them.
Type:
Application
Filed:
May 24, 2005
Publication date:
October 25, 2007
Inventors:
Gustaaf Boeckx, Guy Rosalia Eugeen Van Lommen, Julien Georges Pierre-Olivier Doyon, Erwin Coesemans
Publication number: 20070244138
Abstract: The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl) amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, optionally substituted C1-6alkyl, C(?O)—O—R5, C(?O)—NR6aR6b, C(?S)—NR6aR6b, S(?O)2—NR6aR6b or C(?O)—R7; R4 represents hydrogen or C1-6alkyl; n is 1, 2, 3, 4 or 5; Z represents a cyclic ring system. The invention also relates to processes for preparing the compounds of formula (I), their use as CCR2 antagonists and pharmaceutical compositions comprising them.
Type:
Application
Filed:
May 24, 2005
Publication date:
October 18, 2007
Applicant:
JANSSEN PHARMACEUTICA N.V.
Inventors:
Gustaaf Boeckx, Guy Van Lommen, Julien Georges Doyon, Erwin Coesemans
Publication number: 20070203189
Abstract: This invention concerns the use of a compound of formula (I?) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(?O)2—; mono- or di(C1-6alkyl)aminoS(?O)2; —C(?N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula L is optionally substituted phenyl or a
Type:
Application
Filed:
May 1, 2007
Publication date:
August 30, 2007
Inventors:
Christopher Love, Guy Van Lommen, Julien Georges Doyon, Jean-Pierre Bongartz, Marcel Van der Aa, Robert Hendrickx, Peter Jacobus Antonius Buijnsters, Ludwig Cooymans, Nele Vandermaesen, Erwin Coesemans, Gustaaf Boeckx
Publication number: 20070167456
Abstract: The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents cyano, C(?O)—O—R5, C(?O)—NR6aR6b or C(?O)—R7; or a cyclic ring system; R4 represents hydrogen or C1-6alkyl; n is 1, 2, 3, 4 or 5; R10 represents hydrogen, C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, arylcarbonyl, heteroarylcarbonyl, —C(?O)—NH—R5, —C(?S)—NH—R5 or —S(?O)2—R5. The invention also relates to processes for preparing the compounds of formula (I), their use as CCR2 antagonists and pharmaceutical compositions comprising them.
Type:
Application
Filed:
August 10, 2005
Publication date:
July 19, 2007
Inventors:
Guy Lommen, Gustaaf Boeckx
Publication number: 20050090495
Abstract: The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R2 is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4allyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8; R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R9 and R10 are each independently selected from hydrogen, optionally substituted C1-4al
Type:
Application
Filed:
September 25, 2003
Publication date:
April 28, 2005
Inventors:
Jean Lacrampe, Eddy Freyne, Marc Venet, Gustaaf Boeckx