Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO2018161831) GPR84 RECEPTOR ANTAGONIST AND USE THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/161831 International Application No.: PCT/CN2018/077584
Publication Date: 13.09.2018 International Filing Date: 28.02.2018
IPC:
C07F 9/547 (2006.01) ,C07F 9/6561 (2006.01) ,C07F 9/6553 (2006.01) ,C07F 9/655 (2006.01) ,C07F 9/553 (2006.01) ,C07F 9/09 (2006.01) ,A61K 31/675 (2006.01) ,A61K 31/67 (2006.01) ,A61K 31/665 (2006.01) ,A61K 31/661 (2006.01) ,A61P 29/00 (2006.01) ,A61P 19/02 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
547
Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
547
Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6561
containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
547
Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6553
having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
547
Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
655
having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
547
Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
553
having one nitrogen atom as the only ring hetero atom
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
06
without P-C bonds
08
Esters of oxyacids of phosphorus
09
Esters of phosphoric acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
66
Phosphorus compounds
675
having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
66
Phosphorus compounds
67
having sulfur as a ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
66
Phosphorus compounds
665
having oxygen as a ring hetero atom, e.g. fosfomycin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
66
Phosphorus compounds
661
Phosphorus acids or esters thereof not having P-C bonds, e.g. fosfosal, dichlorvos, malathion
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
02
for joint disorders, e.g. arthritis, arthrosis
Applicants:
中国科学院上海药物研究所 SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES [CN/CN]; 中国上海市 浦东张江祖冲之路555号 555 Zu Chong Zhi Road Zhang Jiang, Pudong Shanghai 201203, CN
Inventors:
南发俊 NAN, Fajun; CN
谢欣 XIE, Xin; CN
陈林海 CHEN, Linhai; CN
张庆 ZHANG, Qing; CN
肖瑜峰 XIAO, Yufeng; CN
杨慧 YANG, Hui; CN
Agent:
上海一平知识产权代理有限公司 XU AND PARTNERS, LLC.; 中国上海市 普陀区真北路958号天地科技广场1号楼106室 Room 106, Building No. 1 Universal High-Tech Plaza 958 Zhen Bei Road, Putuo District Shanghai 200333, CN
Priority Data:
201710128201.306.03.2017CN
Title (EN) GPR84 RECEPTOR ANTAGONIST AND USE THEREOF
(FR) ANTAGONISTE DU RÉCEPTEUR GPR84 ET SON UTILISATION
(ZH) GPR84受体拮抗剂及其应用
Abstract:
(EN) 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, L1, L2, L3, L4, L5, L6, 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.
(FR) La présente invention concerne un antagoniste du récepteur GPR84 et son utilisation. L'antagoniste du récepteur GPR84 de la présente invention possède une structure telle que représentée par la formule (I), les définitions de R1, R2, R3, R4, L1, L2, L3, L4, L5, L6, Y, Z, et les cycles A, B, C et D sont tels que décrits dans la description et les revendications. L'antagoniste du récepteur GPR84 de la présente invention peut inhiber de manière compétitive l'activation du récepteur provoquée par un agoniste de GPR84, et peut être utilisé dans la préparation d'un médicament pour le traitement de maladies apparentées provoquées par une expression élevée ou une haute excitabilité du récepteur GPR84, les maladies comprenant la sclérose en plaques, la maladie intestinale inflammatoire, l'arthrite et analogues.
(ZH) 本发明涉及一种GPR84受体拮抗剂及其应用。本发明的GPR84受体拮抗剂,结构如式(I)所示,其中R1、R2、R3、R4、L1、L2、L3、L4、L5、L6、Y、Z、环A、B、C、D的定义如说明书和权利要求书所述。本发明的GPR84受体拮抗剂,可以竞争性的抑制GPR84的激动剂引起的该受体的激活,可用于制备治疗因GPR84受体高表达或兴奋性过高所导致的相关疾病的药物,所述疾病包括多发性硬化症、炎症性肠病、关节炎等。
front page image
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)