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Isoxazole O-linked carbamoyl cyclohexyl acid as LPA antagonist
专利权人:
브리스톨-마이어스 스큅 컴퍼니
发明人:
쳉, 피터 타이 와,칼텐바흐, 로버트 에프., 3세,장, 하오,시, 얀,리, 준
申请号:
KR1020207020878
公开号:
KR1020200101957A
申请日:
2018.12.18
申请国别(地区):
KR
年份:
2020
代理人:
摘要:
The present invention provides a compound of formula (Ia) or (Ib), or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate thereof, Wherein X 1 , X 2 , X 3 , and X 4 are each independently CR 6 or N; Provided that two or less of X 1 , X 2 , X 3 , or X 4 are N; L is C 1-4 alkylene substituted with 0 to 4 R 7 ; R 1 is (-CH 2 ) a R 9 ; a is an integer of 0 or 1; Each R 2 is independently halo, cyano, hydroxyl, amino, C 1-6 alkyl, C 3-6 cycloalkyl, C 4-6 heterocyclyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, Alkoxy, alkoxyalkyl, haloalkoxyalkyl, or haloalkoxy; n is an integer of 0, 1, or 2; R 3 is hydrogen, C 1-6 alkyl, C 1-6 deuterated alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; Alkyl is optionally substituted with deuterium on its own or as part of another moiety, partially or completely; R 4 is C 1-10 alkyl, C 1-10 deuterated alkyl, C 1-10 haloalkyl, C 1-10 alkenyl, C 3-8 cycloalkyl, 6 to 10-membered aryl, 3 to 8-membered Heterocyclyl, -(C 1-6 alkylene)-(C 3-8 cycloalkyl), -(C 1-6 alkylene)-(6 to 10-membered aryl), -(C 1-6 alkylene )-(3 to 8-membered heterocyclyl), or -(C 1-6 alkylene)-(5 to 6-membered heteroaryl); Wherein each alkyl, alkylene, alkenyl, cycloalkyl, aryl, heterocyclyl, and heteroaryl is independently substituted with 0 to 3 R 8 by itself or as part of another moiety; Or alternatively, R 3 and R 4 together with the N atom to which they are attached form a 4 to 9-membered heterocyclic ring moiety, which is substituted with 0 to 3 R 8 ; R 5 and R 6 are each independently hydrogen, halo, cyano, hydroxyl, amino, C 1-6 alkyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or Haloalkoxy; R 7 is halo, oxo, cyano, hydroxyl, amino, C 1-6 alkyl, C 3-6 cycloalkyl, C 4-6 heterocyclyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy Alkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; R 8 is each independently deuterium, halo, hydroxyl, amino, cya
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