HYPEREROYL PYRIDYL AND PHENYL FENIL COMPOUNDS Fused BENZENOSULPHONAMIDS, COMPOSITION, METHOD OF MODULATING CCR2 FUNCTION, USES OF COMPOUNDS AND CRYSTALLINE FORM
Antoni Krasinski,Qiang Wang,Solomon Ungashe,Sreenivas Punna,Yibin Zeng
申请号:
BRPI0813695
公开号:
BRPI0813695B1
申请日:
2008.07.11
申请国别(地区):
BR
年份:
2019
代理人:
摘要:
fused heteroaryl pyridyl and phenyl benzenesulfonamide compounds, composition, method of modulating ccr2 function, uses of said compounds and crystalline form. "Compounds which act as potent ccr2 receptor antagonists are provided. The compounds are generally derived from aryl sulfonamide and are Useful in pharmaceutical compositions, methods for treating ccr2-mediated diseases and as controls in assays for the identification of ccr2 antagonists: a compound of formula (i) or a salt thereof: wherein r1 and r2 are each independently hydrogen C 1 -a alkyl, -C 1, or C 1 -a haloalkyl, provided that at least one of R 1 or R 2 is different from hydrogen each R 3 is independently R 4 is hydrogen; R 5 is halogen or C 1 -A alkyl R 6 is hydrogen; x1 is cr7, n or no; x2 and x4 are 15 n or no; x3 is cr7; x6 and x7 are each independently selected from cr7, n and n; each r7 is independently selected from the group. po consisting of hydrogen, halogen, substituted or unsubstituted alkylphenyl, substituted or unsubstituted alkylphenyl cra, substituted or unsubstituted cra alkynyl, -cn = 0, -n02, -or6, -oc (o) r8, -c02r8, -c (o) r8, -c (o) nr0r8.20 -oc (o) nr9r8, -nr1 ° c (o) r8, -nr1 ° c (o) nr9r8, -nr9r8, -nr1 ° c02r8 , -sr8, -s (o) r8, -s (o) zr8, -s (0) 2nr9r8, -nr10s (o) zr8, substituted or unsubstituted aryl, substituted or unsubstituted 5-1 membered heteroaryl -substituted and substituted or unsubstituted 3 to 1 membered heterocyclyl.compostos de heteroaril piridil e fenil benzenossulfonamidas fundidas, composição, método de modular a função de ccr2, usos dos referidos compostos e forma cristalina". são fornecidos compostos que agem como potentes antagonistas do receptor ccr2. os compostos são geralmente derivados de aril sulfonamida e são úteis em composições farmacêuticas, métodos para o tratamento de doenças mediadas por ccr2 e como controles em ensaios para a identificação de antagonistas de ccr2. um composto da fórmula (i) ou um sal do mesmo: em que r1 e r2 são cada um inde