DEVIS Stiven Dzhon (GB),ДЭВИС Стивен Джон (GB),PINTET Stefan (GB),ПИНТЭТ Стефан (GB),NORT Karl Lesli (GB),НОРТ Карл Лесли (GB),MOFFAT Devid Festus Charlz (GB),МОФФАТ Дэвид Фестус Чарльз (GB),DEVIS Stiven Dzhon,ДЭВИС Стивен Джон,PINTET Stefan,ПИНТЭТ Стефан,NORT Karl Lesli,НОРТ Карл Лесли,MOFFAT Devid Festus Charlz,МОФФАТ Дэвид Фестус Чарльз
申请号：
RU2014153423
公开号：
RU0002642777C2
申请日:
2013.06.26
申请国别(地区):
RU
年份:
2018
代理人:
摘要：
FIELD: pharmacology.SUBSTANCE: invention relates to a compound that is an amino acid or ester of an amino acid of formula , or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against CSF-1R kinase. In formula (I), ring A is a phenyl group； R1 and R2 independently represent a hydrogen atom, a halogen atom or an unsubstituted C1-4 alkyl； n is 1； X is NH； V is -N=, W is -C(Z)=； Z represents a hydrogen atom, a fluorine atom, a chlorine atom or unsubstituted C1-3 alkyl； ring B is a 1,4-phenylene, 1,3-phenylene or pyridinyl group； [Linker] is a -(CH2)m-X1-(Alk1)x-Y1 group, where m is 0, 1, 2 or 3； x is 0 or 1； Alk1 is an unsubstituted C1-3 alkylene group； X1 and Y1 independently represent a bond, -O-, -S-, -NR7th-, -C(=O) - or -C(=O)NR5-, where R5 is a hydrogen atom or C1-4 alkyl and R7 is a hydrogen atom, unsubstituted C1-4 alkyl or -C(=O)CH3； R is a group of formula or , in which R8 is a -COOH group or an ester group of the formula -(C=O)OR14, where R14 is R15R16R17C-, where any R15 represents a hydrogen atom or C1-3alkyl-(Z1)a-[(C1-C3)alkyl]b-, where a and b are independently 0 or 1, Z1 is -O-, -S- or -NH-, R16 and R17 independently represent a hydrogen atom or C1-3 alkyl- or R15 and R16, taken together with the carbon atom to which they are attached, form a 3-7-membered cycloalkyl ring； and R17 represents a hydrogen atom； where (i) R9 and R10 are side chains of natural amino acids, (ii) one of R9 and R10 represents a hydrogen atom or unsubstituted C1-4 alkyl, and the other is an unsubstituted C1-6 alkyl group or C1-6 alkyl group substituted by a C1-4 alkoxy group, or (iii) R9 and R10, taken together with the carbon atom to which they are attached, form a saturated spiro-cyclobutyl ring； R11 represents a hydrogen atom or an unsubstituted C1-2alkyl group； ring D is a 5- to 7-membered saturated heterocyclyl group with at least one nitrogen atom in the ring. The invention also relates to a pharmaceutical composition, a method of treatment or
