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4. Tetrahydropyridine [3,4-b] estrogen receptor modulator and its application
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:
PE2017001069
公开号:
PE20171330A1
申请日:
2015.12.17
申请国别(地区):
PE
年份:
2017
代理人:
摘要:
It refers to a compound of formula I, wherein: R1, R2, R3 and R4 are h, F, Cl, etc.; R5 is h, c1-c9 tar; R6 is f, Cl, Br, etc.; m is 0, 1, 2, 3, 4; Z1 is link, C (or),Among other things, Z2 is O, s, etc.; Y1 is n or CRB; Y2 is - (CH2)-(CH2CH2)-,Among others, Y3 is NRA or C (RB) 2; RA is h, C1-C6 asphalt, etc.; Rb is h, or (C1-C3 asphalt) -,Among other things, RC is h, C1-C6 asphalt; CY is arildilo c6-c20, c3-c12 carbocyclodilo, etc. (2) - phenyl (2) - phenyl - Fluoro (2) - phenyl (2) fluoro (2) - 1 - (2) - phenyl - Fluoro (23. Methylpropyl-3-methyl-2,3,4,9-tetrahydro-1h-pirido [3,4-b] Indo, etc. He also mentioned a pharmaceutical composer and a production method. These compounds are derivatives of Indian tetrahydropyridine [3,4-b], which regulate estrogen receptors and are useful in cancer treatment.Se 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 produccion. Dichos compuestos son derivados de tetrahidro-pirido[3,4-b]indoles que modulan los receptores de estrogeno, siendo utiles en el tratamiento del cancer
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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