ZHUANG, Linghang,ZHENG, Yajun,ZHAO, Wei,YUAN, Jing,TICE, Colin M.,SINGH, Suresh B.,CLAREMON, David A.,LOTESTA, Stephen D.,LIU, Zhijie,JIA, Lanqi,FAN, Yi,DONG, Chengguo,DILLARD, Lawrence Wayne,MARCUS,
申请号：
PE0013022016
公开号：
PE13722016A1
申请日:
2015.01.30
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Refers to dihidropirrolopiridina derived compounds of formula I or a pharmaceutically acceptable salts of the same, where R2 and R3 is Hydrogen, Hydroxy, among others r4es Hydrogen, C1 or C3 alkyl - C = o X is - C (o) NH - or \u2013nhc (- OR) M is 0, 1 or 2 n is 0, 1, 2 or 3 L1 is asuente or s O2 or cr7r8 CY1 is absent or alkyl haloalquilo C1 - C3, C1 - C3Among others, Cy2 is absent or alcoxicarbonilo C1 - C6, aryl, heteroaryl, among others R7 and R8 is Hydrogen, Hydroxy, or among others, R7 and R8 along with the carbon Atom to which together form a cycloalkyl or heterociclilo 3 to 6 members.Preferred compounds are: (S) - N - (4 - (ethylsulfonyl) benzyl) - 7 - isopropyl - 6 - (4 - (trifluoromethyl) benzyl) - 6.7 - dihydro - 5h pyrrolo [3,4-b] pyridin - 3 - carboxamide (S) - N - (5 - (ethylsulfonyl) pyridin-2-yl) methyl) - 7 - (isopropyl - 6 - (trans-4 - (trifluoromethyl) cyclohexyl) methyl) - 6.7 - dihydro - 5h pyrrolo [3,4-b] pyridin - 3 - carboxa Measure among others. It also relates to a Pharmaceutical Composition and a method of treatment.These compounds are inhibitors of receptor ROR gamma, being useful in the treatment of inflammatory diseases, Metabolic, autoimmune, among othersSe refiere a compuestos derivados de dihidropirrolopiridina de formula I o sales farmaceuticamente aceptables de los mismos, donde: R2 y R3 son hidrogeno, hidroxi, entre otros R4es hidrogeno, alquilo C1-C3 o C=O X es –C(O)NH- o –NHC(O)- m es 0, 1 o 2 n es 0, 1, 2 o 3 L1 esta asuente o es SO2 o CR7R8 Cy1 esta ausente o es alquilo C1-C3, haloalquilo C1-C3, entre otros Cy2 esta ausente o es alcoxicarbonilo C1-C6, arilo, heteroarilo, entre otros R7 y R8 son hidrogeno, hidroxi, entre otros, o R7 y R8 junto con el atomo de carbono al cual se unen forman un cicloalquilo o heterociclilo de 3 a 6 miembros. Son compuestos preferidos: (S)-N-(4-(etilsulfonil)bencil)-7-isopropil-6-(4-(trifluorometil)bencil)-6,7-dihidro-5H-pirrolo[3,4-b]piridin-3-carboxamida (S)-N-((5-(etilsulfonil)piridin-2-il)meti
