C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 413/14 (2006.01) A61K 31/454 (2006.01) A61K 31/4545 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01)
Patent
CA 2238816
This invention concerns the compounds of formula (I), (see formula I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; X is a covalent bond or a bivalent radical of formula -O-, -S-, -NR3-; =Q is =O or =NR3; R1 is Ar1, Ar1C1-6alkyl or di(Ar1)C1-6alkyl wherein the C1-6alkyl group is optionally substituted; R2 is Ar2, Ar2C1-6alkyl, Het or HetC1-6alkyl; L is a benzimidazole or imidazopyridine derivative of formula (A) or (B); (see formula II) wherein p is 0, 1 or 2; (see formula III)Y~ is a bivalent radical of formula -CH2-, -CH(OH)-, -C(=O)-, -O-, -S-, - S(=O)-, -S(=O)2-, -NR3-, -CH2-NR3- or -C(=O)-NR3-; or a trivalent radical of formula =CH-; -A=B- is a bivalent radical of formula -CH=CH-, -N=CH- or -CH=N-; R3 independently is hydrogen or C1-6alkyl; R4 is hydrogen, C1-6alkyl, C3-7cycloalkyl or a radical of formula -Alk-R7 ~(c-1) or -Alk Z-R8 ~(c-2); wherein Alk is C1-6alkanediyl; Z is a bivalent radical of formula -O-, -S- or -NR3-; R7 is phenyl; phenyl substituted with 1 or 2 substituents selected from halo, C1-6alkyl and . C1-6alkyloxy; furanyl; furanyl substituted with 1 or 2~~ substituents selected from C1-6alkyl, and hydroxyC1-6alkyl; thienyl; thienyl substituted with 1 or 2 substituents selected from halo and C1-6alkyl; oxazolyl; oxazolyl substituted with 1 or 2 C1-6alkyl substituents; thiazolyl; thiazolyl substituted with 1 or 2 C1-6alkyl substituents; pyridinyl or pyridinyl substituted with 1 or 2 C1-6alkyl substituents; R8 is C1-6alkyl or C1-6alkyl substituted with hydroxy, carboxyl or C1-6alkyloxycarbonyl; R5 is hydrogen, halo, hydroxy or C1-6alkyloxy; R6 is hydrogen, C1-6alkyl or Ar1C1-6alkyl; Ar1 is optionally substituted phenyl; Ar2 is naphtalenyl or optionally substituted phenyl; and Het is an optionally substituted monocyclic or bycyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.
L'invention concerne des composés de la formule (I), les dérivés oxyde d'azote de ces composés et leurs sels d'addition acceptables sur le plan pharmaceutique, ainsi que leurs formes isomères stéréochimiques. Dans cette formule, n est 0, 1 ou 2; m est 1 ou 2, à condition que, si m est 2, alors n est 1; X est une liaison covalente ou un radical bivalent de la formule -O-, -S-, -NR<3>-; =Q est =O ou=NR<3>; R<1> est Ar<1>, Ar<1>alkyleC1-6 ou di(Ar<1>)alkyleC1-6, où le groupe alkyleC1-6 est éventuellement substitué; R<2> est Ar<2>, Ar<2>alkyleC1-6, Het ou Hetalkylec1-6; L est un dérivé benzimidazole ou imidazopyridine de la formule (A) ou (B); Ar<1> est un phényle éventuellement substitué; Ar<2> est un naphtalènyle ou un phényle éventuellement substitué; et Het est un hétéromonocycle ou hétérobicycle, éventuellement substitué. Les composés de l'invention sont utiles comme antagonistes de la substance P. L'invention concerne également la préparation de ces composés, des formulations les contenant et leur utilisation en médecine.
Janssens Frans Eduard
Leenaerts Joseph Elisabeth
Sommen Francois Maria
Surleraux Dominique Louis Nestor Ghislaine
Gowling Lafleur Henderson Llp
Janssen Pharmaceutica N.v.
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