09-01-2020 дата публикации
Номер: US20200010492A1
Принадлежит:
The present invention relates to a GPR84 receptor antagonist and use thereof. The GPR84 receptor antagonist of the present invention has a structure as represented by formula (I), the definitions of R1, R2, R3, R4, L, L, L, L, L, L, Y, Z, and rings A, B, C, and D are as described in the description and claims. The GPR84 receptor antagonist of the present invention can competitively inhibit the activation of the receptor caused by an agonist of GPR84, and can be used in the preparation of a medicament for treating related diseases caused by high expression or high excitability of GPR84 receptor, the diseases including multiple sclerosis, inflammatory bowel disease, arthritis and the like. 2. The compound according to claim 1 , wherein each of rings A claim 1 , B claim 1 , C and D is independently a benzene ring claim 1 , a C-Ccycloalkane ring claim 1 , a C-Cheterocycloalkane ring or a C-Cheteroaryl ring.3. The compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rare each independently one claim 1 , two or three substituents on rings A claim 1 , B claim 1 , C and D claim 1 , and each substituent is independently absent claim 1 , substituted or unsubstituted C-Calkyl claim 1 , —CH-L-CH claim 1 , —CH—N(CH)—CH claim 1 , hydroxyl claim 1 , mercapto claim 1 , amino claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I; the above substitution means there is one or more substituents selected from the group consisting of halogen claim 1 , hydroxyl claim 1 , amino claim 1 , —COOC-Calkyl claim 1 , —COOH; Lis each independently O claim 1 , S claim 1 , NH claim 1 , each r is independently an integer of 0-4 claim 1 , each s is independently an integer of 0-4 claim 1 , and each t is independently an integer of 1-4.4. The compound according to claim 1 , wherein Land Lare each independently absent claim 1 , CH claim 1 , O claim 1 , S claim 1 , SO claim 1 , SO claim 1 , —CH═CH— claim 1 , CO claim 1 , —C(═CH)— claim 1 , substituted or unsubstituted C-Calkylidene claim 1 , ...
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