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FGF receptor agonist dimeric compounds (FGFR), procedure for their preparation and therapeutic use thereof
专利权人:
SANOFI
发明人:
BENAZET, Alexandre,GUILLO, Nathalie
申请号:
ES12824733
公开号:
ES2598083T3
申请日:
2012.12.26
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
Agonist compounds of FGF receptors corresponding to the general formula: M1-L-M2 in which M1 and M2, which may be identical or different, each represent, independently of one another, a monomer unit M and L represents a linker group linking M1 and M2 covalently, characterized in that said monomer unit corresponds to the general formula M that follows: in which, * indicates the site of linkage between monomer unit M and linker L, - R1 represents. a group -NHCOPh, said phenyl being substituted with an oxygen atom, so that the oxygen atom is the site of linkage between the monomer unit and the linker L; This group can be designated -NHCOPhO *, or. an aryl group, in particular phenyl, or a heteroaryl group, said group being substituted with a group selected from a divalent oxygen atom so that the oxygen atom is the site of linkage between the monomer unit and the linker L, or an amide group -CONH * -, so that the nitrogen atom is the binding site between the monomer unit and the linker L, - R2 represents an alkyl group, - R3 represents a hydrogen atom or a linear alkyl group, branched, cyclic or partially cyclic, - R4 represents a hydrogen atom or an alkyl or -alkyl-COOR5 group, R5 representing a hydrogen atom or an alkyl group, - L is chosen from the radicals having the following formulas: ** Formulas ** in which - * indicates the connection atom of L with the monomer unit M in the substituent R1, - n represents an integer from 0 to 5, - m represents an integer from 1 to 5, - r represents an integer from 1 to 6, - R2 'and R2 ", which they may be identical or different, they represent a linear alkyl radical having 1 to 5 carbon atoms, and which may be optionally bonded to form a ring, - R6 represents a (C1-C4) alkyl group, optionally substituted with one or more substituents selected from: - an aryl or heteroaryl group, optionally substituted with a group selected from a hydroxyl, amine or NR6'R6 "group, R6 'and R6" being chosen, which may be identical or different, fro
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