DOWDELL, Sarah E.,EIDAM, Hilary Schenck,ELBAN, Mark,FOX, Ryan Michael,HAMMOND, Marlys,HILFIKER, Mark A.,YE, Guosen,KALLANDER, Lara S.,LAWHORN, Brian Griffin,MANNS, Sharada,PHILP, Joanne,WASHBURN, Davi
申请号：
PE0011132016
公开号：
PE09982016A1
申请日:
2015.01.09
申请国别(地区):
PE
年份:
2016
代理人:
摘要：
Relates to compounds of formula (i), or salts thereof, wherein R1 is H, alkyl or c1\u2013c4 hidroxialquilo c1\u2013c4 c1\u2013c11 R2 is H, alkyl, alkyl (c1\u2013c3) \u2013cicloalquilo (c3\u2013c6) alkyl (c1\u2013c3) \u2013fenilo, among others and R3 is: (a) phenyl optionally substituted with 1 to selected 3 groups Regardless c1\u2013c6 Swims between alkyl, ciclopropilo, CONH2, COOH, NH2, sh,Among others or (b) optionally substituted heteroaryl groups selected independently with 1 or 2 c1\u2013c4 between alkyl, alkoxy c1\u2013c4, Oxo, COOH, among others. It also relates to pharmaceutical compositions and combinations comprising such compounds of formula (i).These compounds are inhibitors of formula (i) or TLL2 tll1 bmp1,, which are useful in the treatment of diseases associated with fibrosis, Cardiac arrhythmias, myocardial infarction, chronic renal insufficiency, idiopathic pulmonary fibrosis, cirrhosis, among others), muscular dystrophy Among otherSe refiere a compuestos de Formula (I) o sales de los mismos, donde R1 es H, alquilo C1–C4 o hidroxialquilo C1–C4 R2 es H, alquilo C1–C11, alquil (C1–C3)–cicloalquilo (C3–C6), alquil (C1–C3)–fenilo, entre otros y R3 es: (a) fenilo opcionalmente sustituido con 1 a 3 grupos seleccionados independientemente entre alquilo C1–C6, ciclopropilo, CONH2, NH2, SH, COOH, entre otros o (b) heteroarilo opcionalmente sustituido con 1 o 2 grupos seleccionados independientemente entre alquilo C1–C4, alcoxi C1–C4, oxo, COOH, entre otros. Tambien se refiere a composiciones y combinaciones farmaceuticas comprendiendo dichos compuestos de Formula (I). Dichos compuestos de Formula (I) son inhibidores de BMP1, TLL1 o TLL2, por lo cual son utiles en el tratamiento de enfermedades asociadas con fibrosis (infarto de miocardio, arritmias cardiacas, insuficiencia renal cronica, fibrosis pulmonar idiopatica, cirrosis, entre otros), distrofias musculares, entre otras
