KEMP Mark Ien (GB),КЕМП Марк Иэн (GB),STOKLI Martin Li (GB),СТОКЛИ Мартин Ли (GB),VUDROU Majkl Devid (GB),ВУДРОУ Майкл Дэвид (GB),DZHONS Elison (GB),ДЖОНС Элисон (GB)
申请号：
RU2018133279
公开号：
RU0002730552C2
申请日:
2017.03.02
申请国别(地区):
RU
年份:
2020
代理人:
摘要：
FIELD: organic chemistry.SUBSTANCE: invention relates to a compound of formula I:a tautomer thereof or a pharmaceutically acceptable salt thereof. In formula (I), each of R1a, R1b, R1c and R1d is hydrogen； each of R1e and R1f is hydrogen； ring A is 5–11 member monocyclic or bicyclic heterocyclyl ring which in addition to amide nitrogen can contain 1, 2 or 3 heteroatoms, each of which is independently selected from N, O and S, and which can optionally be substituted with one or two -Q1-(R2)n, which can be identical or different, where n is 0 or 1, Q1 is halogen, oxo, -CONR3R4, -C1-C6alkyl, -C1-C6alkoxy, covalent bond, -CO-, -CONR3- or C1-C6alkylene； wherein said alkyl is optionally substituted with 1–4 halogen substituents, R2 represents 3–10 membered heterocyclyl, heteroaryl or aryl ring, which is optionally substituted with one or two substitutes independently selected from halogen, cyano, oxo, -CONR6R7, -NR6COR7, -C1-C6alkyl, -C1-C6alkoxy, -Q2a-R8, -Q2b-CONR6-Q2c-R8 and -Q2-NR6SO2-Q2c-R8； wherein said heterocyclyl and heteroaryl rings contain 1, 2 or 3 heteroatoms, each of which is independently selected from N, O and S； wherein said aryl ring is selected from phenyl and naphthyl； wherein said alkyl is optionally substituted with hydroxyl； and wherein said alkoxy is optionally substituted with one or more halogen； Q2a is a covalent bond, an oxygen atom, -SO2-, -CO- or C1-C6alkylene； each of Q2b and Q2c is a covalent bond； each of R3 and R4 independently represents hydrogen or C1-C6alkyl； each of R6 and R7 independently represents hydrogen or C1-C6alkyl； R8 denotes 6-member heterocyclyl which is optionally substituted with methyl； phenyl, which is optionally substituted with chlorine； or cyclopropyl； where said heterocyclyl ring contains 1 or 2 heteroatoms, each of which is independently selected from N and O. Also disclosed is a pharmaceutical composition.EFFECT: disclosed are novel compounds for use as Cezanne 1 inhibitors.16 cl, 7 tbl, 39 exИзобретение относится
