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TETRAHIDRO-PIRIDO[3,4-B]INDOLES MODULADORES DE RECEPTORES DE ESTROGENOS Y USOS DE LOS MISMOS
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
GOODACRE, Simon Charles,LABADIE, Sharada,LIANG, Jun,ORTWINE, Daniel Fred,RAY, Nicholas Charles,WANG, Xiaojing,ZBIEG, Jason,ZHANG, Birong
申请号:
PE0010692017
公开号:
PE13302017A1
申请日:
2015.12.17
申请国别(地区):
PE
年份:
2017
代理人:
摘要:
Refers to a compound of formula I, where R1, R2, R3 and R4 are h, F, CL, among others R5 is H, alkyl C1 C9 R6 F, CL, BR, among others M is 0, 1, 2, 3, 4 Z1 is a Link C (OR), among others Z2 is o, S, among others y1 or Y2 is CRB is N - (CH2) - - - (ch2ch2), among others Y3 is NRA or C (RB) 2 Ra is H, alkyl of C1 - C6, among others RB is H, alkyl - or - C1 - C3), RC is H, among othersC1 - C6 alkyl, among others CY is arildiilo C20 carbociclildiilo C3 C6, C12, among others.Preferred compounds are (1R, 3R) - 1 - (2,6 di Fluorine - 4 - ((1 - (3 - fluor - propyl) - 3 - azetidin il Oxy) - phenyl) - 2 - (2 - fluor - 2-methylpropyl) - 3 - methyl - 2,3,4,9 - tetrahydro - 1H - pirido [3,4-b] indole (1R, 3R) - 1 - (2,6 di Fluorine - 4 - (2 - (3 - azetidin Fluorine methyl) - 1 - il) - ethoxy) - 2 - (phenyl Fluorine - 2-methylpropyl) - 3 - methyl - 2,3,4,9 - tetrahydro Pirido - 1H - [3,4-b] Indo, among others.It also relates to a Pharmaceutical Composition and a method of production. These compounds are Derivatives of tetrahydro - pirido [3,4-b] indoles that modulate estrogen Receptors, being useful in the treatment of cancerSe refiere a un compuesto de formula I, donde: R1, R2, R3 y R4 son H, F, Cl, entre otros R5 es H, alquilo C1-C9 R6 es F, Cl, Br, entre otros m es 0, 1, 2, 3, 4 Z1 es un enlace, C(O), entre otros Z2 es O, S, entre otros Y1 es N o CRb Y2 es -(CH2)-, -(CH2CH2)-, entre otros Y3 es NRa o C(Rb)2 Ra es H, alquilo C1-C6, entre otros Rb es H, -O(alquilo C1-C3)-, entre otros Rc es H, alquilo C1-C6, entre otros Cy es arildiilo C6-C20, carbociclildiilo C3-C12, entre otros. Son compuestos preferidos: (1R, 3R)-1-(2,6-di-fluor-4-((1-(3-fluor-propil)azetidin-3-il)-oxi)fenil-2-(2-fluor-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indol (1R, 3R)-1-(2,6-di-fluor-4-(2-(3-fluor-metil)azetidin-1-il)-etoxi)fenil-2-(2-fluor-2-metilpropil)-3-metil-2,3,4,9-tetrahidro-1H-pirido[3,4-b]indo, entre otros. Tambien se refiere a una composicion farmaceutica y a un metodo de prod
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