BEIGHT, Douglas W.,COATES, David A.,JOSEPH, Sajan,MCMILLEN, William T.,PARTHASARATHY, Saravanan,PEI, Huaxing,SAWYER, Jason Scott,WOLFANGEL, Craig D.,ZHAO, Gaiying
申请号：
PE0005362017
公开号：
PE06622017A1
申请日:
2015.09.30
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Refers to a compound of formula I, where R1 is Hydrogen, Methyl, among others R2 is Ethyl Tert Butyl, among others R3 is carbamoilfenilo, pyridin thiocyanatoacetate, among others.Preferred compounds are: {2 - [4 - (4 - [3 - (1 - 2-cyclopropyl-1 - tetrahydro - 2H - piran - 4-yl) - 1h-pyrazol-4-yl] oxy] pyridin-2-yl) amino] pyridin-2-yl) propan-2-ol 4 - metilbencesulfonato {2 - [4 - (4 - [3 - (1 - 2-cyclopropyl-1 - tetrahydro - 2H - piran - 4-yl) - 1h-pyrazol-4-yl] oxy] pyridin-2-yl) amino] pyridin-2-yl) propan-2-ol among others. You. It also relates to a Pharmaceutical composition.These compounds are derived from aminopiridiloxipirazol that inhibit the activity of the Receptor of Transforming Growth Factor Beta 1 (tgfbetar1), being useful in the treatment of cancer, preferably colon cancer, melanoma, Carcinoma, among othersSe refiere a un compuesto de formula I, donde: R1 es hidrogeno, isopropilo, entre otros R2 es etilo, terc-butilo, entre otros R3 es carbamoilfenilo, piridin-2-ilo, entre otros. Son compuestos preferidos: 2-{4-[(4-{[1-ciclopropil-3-(tetrahidro-2H-piran-4-il)-1H-pirazol-4-il]oxi}piridin-2-il)amino]piridin-2-il}propan-2-ol 4-metilbencesulfonato de 2-{4-[(4-{[1-ciclopropil-3-(tetrahidro-2H-piran-4-il)-1H-pirazol-4-il]oxi}piridin-2-il)amino]piridin-2-il}propan-2-ol entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son derivados de aminopiridiloxipirazol que inhiben la actividad del receptor 1 del factor del crecimiento transformante beta (TGFBETAR1), siendo utiles en el tratamiento del cancer, preferentemente cancer de colon, melanoma, carcinoma, entre otros
