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1. (WO2017157332) AROMATIC AMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL APPLICATIONS THEREOF
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Pub. No.: WO/2017/157332 International Application No.: PCT/CN2017/077114
Publication Date: 21.09.2017 International Filing Date: 17.03.2017
IPC:
C07D 401/14 (2006.01) ,C07D 401/06 (2006.01) ,C07D 401/12 (2006.01) ,C07D 235/10 (2006.01) ,C07D 235/12 (2006.01) ,A61P 37/00 (2006.01) ,A61P 35/00 (2006.01) ,A61P 29/00 (2006.01) ,C07D 209/12 (2006.01) ,A61K 31/4184 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
10
Radicals substituted by halogen atoms or nitro radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
12
Radicals substituted by oxygen atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
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)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
10
with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
12
Radicals substituted by oxygen atoms
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
4184
condensed with carbocyclic rings, e.g. benzimidazoles
Applicants:
江苏恒瑞医药股份有限公司 JIANGSU HENGRUI MEDICINE CO., LTD. [CN/CN]; 中国江苏省连云港市 经济技术开发区昆仑山路7号 No.7 Kunlunshan Road, Economic and Technological Development Zone Lianyungang, Jiangsu 222047, CN
上海恒瑞医药有限公司 SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD. [CN/CN]; 中国上海市 闵行区文井路279号 NO.279 Wenjing Road, Minhang District Shanghai 200245, CN
Inventors:
陆标 LU, Biao; CN
苟俊 GOU, Jun; CN
张民生 ZHANG, Minsheng; CN
贺峰 HE, Feng; CN
陶维康 TAO, Weikang; CN
Agent:
北京戈程知识产权代理有限公司 GE CHENG & CO.,LTD.; 中国北京市 东城区东长安街1号东方广场东三办公楼19层程伟 David W. Cheng Level 19,Tower E3, The Towers, Oriental Plaza No. 1, East Chang An Avenue, Dongcheng District Beijing 100738, CN
Priority Data:
201610158675.818.03.2016CN
Title (EN) AROMATIC AMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL APPLICATIONS THEREOF
(FR) DÉRIVÉ AMIDE AROMATIQUE, PROCÉDÉ DE PRÉPARATION DE CE DERNIER, ET APPLICATIONS PHARMACEUTIQUES DE CE DERNIER
(ZH) 芳香酰胺类衍生物、其制备方法及其在医药上的应用
Abstract:
(EN) An aromatic amide derivative represented by formula (I), a preparation method therefor, a pharmaceutical composition comprising the derivative, uses thereof as an ROR regulator, and users thereof in preventing or treating inflammatory disease, autoimmune diseases, cancers and other diseases. The aromatic amide derivative has an agitation or anti-agitation activity on ROR. The combined medication of the aromatic amide derivative and a PD-1 antibody can be used in treatment of tumors or cancers.
(FR) L'invention concerne un dérivé amide aromatique représenté par la formule (I), un procédé de préparation de ce dernier, une composition pharmaceutique comprenant le dérivé, des utilisations de ce dernier comme régulateur de ROR, et des utilisations de ce dernier dans la prévention ou le traitement de maladies inflammatoires, de maladies auto-immunes, de cancers et d'autres maladies. Le dérivé amide aromatique a une activité de stimulation ou d'inhibition de ROR. Le médicament combinant le dérivé amide aromatique et un anticorps contre PD-1 peut être utilisé dans le traitement de tumeurs ou de cancers.
(ZH) 一种通式(I)所示的芳香酰胺类衍生物、其制备方法、含有该衍生物的药物组合物,其作为ROR调节剂的用途以及其预防和/或治疗炎症、自身免疫性疾病和癌症等疾病的用途。所述芳香酰胺类衍生物对ROR具有激动或反激动活性。所述芳香酰胺类衍生物与PD-1抗体联合用药可以用于肿瘤或癌症的治疗。
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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, 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)