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FENILUREAS Y FENILAMIDAS COMO LIGANDOS DEL RECEPTOR DE VANILLOIDES
专利权人:
GRUNENTHAL GMBH
发明人:
FRANK, ROBERT,BAHRENBERG, GREGOR,CHRISTOPH, THOMAS,SCHIENE, KLAUS,DE VRY, JEAN,DAMANN, NILS,FRORMANN, SVEN,LESCH, BERNHARD,LEE, JEEWOO,KIM, YONG-SOO,KIM, MYEON-SEOP
申请号:
PE0019162011
公开号:
PE03742012A1
申请日:
2010.05.06
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Referring to a fenilamida phenylurea compound and Derivative of formula (i), where X is Cr3 or N R3 is H, alkyl C1 - C10 is or cr5b n n is an integer from 1 to 4 r1 is alkyl C1 - C10, ciclalquilo C3 - C10, C (= o) - Oh, among others R2 is H, NO2, NS, F, sh, among others R4 is H, FL, CL, Oh, alkyl C1 - C10 Among others, r5a is H, alkyl Oh, C1 - C10, among others r5b is H or alkyl R0, R0 is C1 - C10Cycloalkyl C3 - C10, among others, R6, R7, R9 and R10 are h, F, NO2, CN, CF3, among others R8 is H, F, CN, CF3, cf2h, among others.Preferred compounds are: N - (3 - (tert - butyl - 1 - methyl - 5 - 1H pyrazole - yl) methyl 2 - (3 - (4 - Fluorine - metilsulfonamido) phenyl) propanamide, N - (3 - (tert - butyl - 1 - Hexyl - 1H pyrazole - 5 - yl) methyl 2 - (3 - (4 - Fluorine - metilsulfonamido) phenyl) propanamide, N - (3 - (tert - butyl - 1 - Cyclohexyl - 1H pyrazole - 5 - yl) methyl 2 - (3 - (4 - metilsulfona Fluorine Mido) phenyl) propanamide, among others.It also relates to a Pharmaceutical Composition and a method for obtaining. These compounds have activity on the vanilloides receptor subtype 1 (TRPV1 receptor VR1 \/) and are useful in the treatment of Pain and inflammationREFERIDA A UN COMPUESTO DERIVADO DE FENILUREA Y FENILAMIDA DE FORMULA (I), DONDE X ES CR3 O N R3 ES H, ALQUILO C1-C10 A ES N O CR5b n ES UN ENTERO DE 1 A 4 R1 ES ALQUILO C1-C10, CICLALQUILO C3-C10, C(=O)-OH, ENTRE OTROS R2 ES H, CN, F, NO2, SH, ENTRE OTROS R4 ES H, Fl,Cl, OH, ALQUILO C1-C10, ENTRE OTROS R5a ES H, OH, ALQUILO C1-C10, ENTRE OTROS R5b ES H O r0 R0 ES ALQUILO C1-C10, CICLOALQUILO C3-C10, ENTRE OTROS R6, R7, R9 Y R10 SON H, F, NO2, CN, CF3, ENTRE OTROS R8 ES H, F, CN, CF3, CF2H, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-((3-TERT-BUTIL-1-METIL-1H-PIRAZOL-5-IL)METIL-2-(3-FLUOR-4-(METILSULFONAMIDO)FENIL)PROPANAMIDA, N-((3-TERT-BUTIL-1-HEXIL-1H-PIRAZOL-5-IL)METIL-2-(3-FLUOR-4-(METILSULFONAMIDO)FENIL)PROPANAMIDA, N-((3-TERT-BUTIL-1-CICLOHEXIL-1H-PIRAZOL-5-IL)METIL-2-(3-FLUOR-4-(METILSULFONAMIDO
来源网站:
中国工程科技知识中心
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