DI GIORGIO, Patrick,HERT, Jerôme,RUDOLPH, Markus,KUEHNE, Holger,MATTEI, Patrizio,HUNZIKER, Daniel
申请号：
PE0015502016
公开号：
PE11342016A1
申请日:
2015.03.23
申请国别(地区):
PE
年份:
2016
代理人:
摘要：
Bicyclic relates to compounds of formula (i), or pharmaceutically acceptable salts thereof, in which R1 is phenyl or substituted pyridinyl, each of them by R3, R4 and R5, is \u2013n\u2013 or \u2013ch\u2013 W - C (o) -, - C (o) (OR) 2 - or -, - S, \u2013conh\u2013 or \u2013ch2\u2013, among others R2 is 2\u2013oxo \u2013dihidrobenzoxazol\u20136\u2013ilo, indazol\u20135\u2013ilo, bencimidazol\u20135\u2013ilo, indol\u20135\u2013ilo, R3 is heterocicloalcoxi, among othersHeterocicloalquilamino, among others and R4 and R5 are independently h, NH2, alkyl, cycloalkyl, haloalquilo, halogen, CN, among others. It also relates to processes for the production of said Compounds, and to pharmaceutical compositions comprising these compounds.Bicyclic compounds of formula (i) are inhibitors of the production of i.e., Autotaxin (ATX), and therefore also for the production of lysophosphatidic acid (LPA), which are useful in the treatment of Kidney Disease (Acute Kidney Injury, Chronic Kidney Disease), Liver (Cirrus SIS, among others), inflammation (Osteoarthritis, arthritis, multiple sclerosis,Systemic lupus erythematosus, among others), vascular (atherosclerosis, among others), Metabolic, among othersSe refiere a compuestos biciclicos de formula (I) o sus sales farmaceuticamente aceptables, en los cuales R1 es fenilo o piridinilo, cada uno de ellos sustituidos por R3, R4 y R5 A es –N– o –CH– W es –C(O)–, –C(O)O–, –S(O)2–, –CONH– o –CH2–, entre otros R2 es 2–oxo–dihidrobenzoxazol–6–ilo, indazol–5–ilo, bencimidazol–5–ilo, indol–5–ilo, entre otros R3 es heterocicloalcoxi, heterocicloalquilamino, entre otros y R4 y R5 son independientemente H, NH2, alquilo, haloalquilo, cicloalquilo, halogeno, CN, entre otros. Tambien se refiere a procesos para la obtencion de dichos compuestos, y a composiciones farmaceuticas que comprenden dichos compuestos. Los compuestos biciclicos de formula (I) son inhibidores de la produccion de autotaxina (ATX), y por ende tambien de la produccion de acido lisofos
