HUANG, TAISHENG,XUE, CHU-BIAO,WANG, ANLAI,KONG, LING,YE, HAI FEN,YAO, WENQING,RODGERS, JAMES D.,SHEPARD, STACEY,WANG, HAISHENG,SHAO, LIXIN,LI, HUI-YIN,LI, QUN
申请号：
PE0014672012
公开号：
PE00382013A1
申请日:
2011.03.09
申请国别(地区):
PE
年份:
2013
代理人:
摘要：
Refers to compounds derived from piperidin-4-yl il azetidine of formula (i) where X is n or CR2, where R2 is H, Halo, CN, alkyl (c1-c4), among others and is n or Cr3, where R3 is H, CN, Nitro,Alquenilo (C2 - C6), among others) Z is H, alkyl, Halo, (C1 - C3), among others l is C (= o), S (= o) 2, C (= o) or, among others it is (C1 - C6 alkyl, cycloalkyl () C3 C14), aryl (C6, C14)Among others r1 is alkyl (c1-c4), Hydroxy, alkoxy (c1-c4), F, among others n is 0 to 4.Preferred compounds are: {1 - {[1 - 3 - fluoro - 2 - (trifluoromethyl) isonicotinoil piperidin-4-yl il}] - 3 - [4 - (7H pyrrolo [2,3 - d] pyrimidin-4-yl) - 1H pyrazol-1-yl] - 3 - azetidin acetonitrile {il} 1 - [1 - (3 - 4 - 5 - fluoro - ilbenzoil quinolin-1) piperidin-4-yl il] - 3 - [4 - (7H pyrrolo [2,3 - d] pyrimidin-4-yl) - 1H pyrazol-1-yl] - 3 - azetidin {il} acetonitrile 3 - [4 - (7H pyrrolo [2,3-d] pyrimidin-4-yl) - 1H pyrazol-1-yl] - [1 - (1 - 3.4,5 - trifluorobenzoil) piperidin-4-yl] - 3 - azetidin Il Il} acetonitrile among others. It also relates to a Pharmaceutical composition.These compounds are modulators of the activity of Janus kinase JAK1) being useful in the treatment of rheumatoid arthritis, lupus, atopic dermatitisSE REFIERE A COMPUESTOS DERIVADOS DE PIPERIDIN-4-IL AZETIDINA DE FORMULA (I) DONDE X ES N O CR2, EN DONDE R2 ES H, HALO, CN, ALQUILO(C1-C4), ENTRE OTROS Y ES N O CR3, EN DONDE R3 ES H, CN, NITRO, ALQUENILO(C2-C6), ENTRE OTROS Z ES H, CN, HALO, ALQUILO(C1-C3), ENTRE OTROS L ES C(=O), S(=O)2, C(=O)O, ENTRE OTROS A ES ALQUILO(C1-C6), CICLOALQUILO(C3-C14), ARILO(C6-C14), ENTRE OTROS R1 ES ALQUILO(C1-C4), HIDROXILO, ALCOXI(C1-C4), F, ENTRE OTROS n ES DE 0 A 4. SON COMPUESTOS PREFERIDOS: {1-{1-[3-FLUORO-2-(TRIFLUOROMETIL)ISONICOTINOIL]PIPERIDIN-4-IL}-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]AZETIDIN-3-IL}ACETONITRILO {1-[1-(3-FLUORO-4-QUINOLIN-6-ILBENZOIL)PIPERIDIN-4-IL]-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]AZETIDIN-3-IL}ACETONITRILO {3-[4-(7H-PIRROLO[2,
