GELIN, CHRISTINE,FLYER, ALEC,ADAMS, CHRISTOPHER MICHAEL,DARSIGNY, VERONIQUE,HURLEY, TIMOTHY BRIAN,KARKI, RAJESHRI GANESH,JIANG, NAN,KAWANAMI, TOSHIO,MEREDITH, ERIK,SERRANO-WU, MICHAEL H.,RAO, CHANG,SO
申请号:
PE0001142014
公开号:
PE12812014A1
申请日:
2012.07.20
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Refers to compounds derived from tetrahidropirido - tetrahidropirido - pyridine and pyrimidine of formula (i) where X is n or CH Z1 is n or CR1C r1c, where is H, alkyl or Halogen (C1 - C6) or cr1d Z2 is n, where R1D is H, alkyl (C1 - C6) alkoxyl, (C1 - C6), among others, A1A is H, alkyl (C1 - C6), Lac Oxilo (C1 - C6), CN, among others, r1b is H, amino, alquilamino (c1-c4), among others, R1e is H, halogen,CN, alkyl (C1 - C6), among others R2 is H, alkyl, cycloalkyl (C1 - C6) (C3 - C7), among others R3 is phenyl or heteroaryl fenilalquilo (C1 - C3) R4 is H or alkyl (c1-c4) R4 and R5 is H, or R5 in combination are oxo R6 H R6 form a carbonyl or both.Preferred compounds are: 1 - (2 - (2,6-dimethylphenyl) - 6 - (isopropyl - 3 - 1 - methyl - 5 - 1H pyrazole - yl) - minutebug - tetrahidropirido [4,3-d] pyrimidin-4-yl) - 2 - 4 - ol - metilpiperidin Racemic 2 - (2,6 - dimetilfenil) - 4 - (3,3 - dimetilpiperidin - 1 - il) - 6 - (isopropyl - 3 - 1 - methyl - 5 - 1H pyrazole - yl) - minutebug - tetrahidropirido [4,3-d] pyrimid Ina (S) - 2 - (2,6-dimethylphenyl) - 6 - (isopropyl - 3 - 1 - methyl - 5 - 1H pyrazole - yl) - 4 - (2 - methylpiperidin-1-yl) - 5.67.8 - tetrahidropirido [4,3-d] pyrimidine among others. It also relates to a Pharmaceutical composition. These compounds are modulators of Mammalian complement C5A receptors being useful in the treatment of Diabetic Retinopathy, retinitis pigmentosa, ocular pemphigusSE REFIERE A COMPUESTOS DERIVADOS DE TETRAHIDROPIRIDO-PIRIDINA Y TETRAHIDROPIRIDO-PIRIMIDINA DE FORMULA (I) DONDE X ES N O CH Z1 ES N O CR1c, EN DONDE R1c ES H, HALOGENO O ALQUILO(C1-C6) Z2 ES N O CR1d, EN DONDE R1d ES H, ALQUILO(C1-C6), ALCOXILO(C1-C6), ENTRE OTROS R1a ES H, ALQUILO(C1-C6), ALCOXILO(C1-C6), CN, ENTRE OTROS R1b ES H, AMINO, ALQUILAMINO(C1-C4), ENTRE OTROS R1e ES H, HALOGENO, CN, ALQUILO(C1-C6), ENTRE OTROS R2 ES H, ALQUILO(C1-C6) CICLOALQUILO(C3-C7), ENTRE OTROS R3 ES FENILO, HETEROARILO O FENILALQUILO(C1-C3) R4 ES H O ALQUILO(C1-C4) R5 ES H, O R4