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1. (WO2017092638) OPIOID RECEPTOR ANTAGONIST DERIVATIVE, PREPARATION METHOD THEREOF AND USE THEREOF IN MEDICINE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/092638 International Application No.: PCT/CN2016/107513
Publication Date: 08.06.2017 International Filing Date: 28.11.2016
IPC:
C07D 489/00 (2006.01) ,A61K 31/439 (2006.01) ,A61P 25/02 (2006.01) ,A61P 1/04 (2006.01) ,A61P 1/14 (2006.01) ,A61P 11/00 (2006.01) ,A61P 39/02 (2006.01) ,A61P 1/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
489
Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
439
the ring forming part of a bridged ring system, e.g. quinuclidine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
02
for peripheral neuropathies
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
04
for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
14
Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
39
General protective or antinoxious agents
02
Antidotes
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
10
Laxatives
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
成都盛迪医药有限公司 SUNCADIA PHARMACEUTICALS CO., LTD. [CN/CN]; 中国四川省成都市 高新区科园南路88号天府生命科技园B4-903 B4-903 Tianfu Life Sciences Park, No.88 Keyuan South Road, High-tech Zone Chengdu, Sichuan 610000, CN
Inventors:
黄金昆 HUANG, Jinkun; CN
张连山 ZHANG, Lianshan; CN
薛州洋 XUE, Zhouyang; CN
李磊 LI, Lei; CN
杨昌永 YANG, Changyong; CN
南文汇 NAN, Wenhui; CN
孙星 SUN, Xing; CN
王亚里 WANG, Yali; 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:
201510863385.901.12.2015CN
Title (EN) OPIOID RECEPTOR ANTAGONIST DERIVATIVE, PREPARATION METHOD THEREOF AND USE THEREOF IN MEDICINE
(FR) DÉRIVÉ D'ANTAGONISTE DE RÉCEPTEUR OPIOÏDE, PROCÉDÉ DE PRÉPARATION DE CELUI-CI ET UTILISATION DE CELUI-CI EN MÉDECINE
(ZH) 阿片样受体拮抗剂类衍生物、其制备方法及其在医药上的应用
Abstract:
(EN) The present invention relates to an opioid receptor antagonist derivative, a preparation method thereof and a use thereof in medicine. In particular, the present invention relates to a naloxone derivative as shown by general formula (I) and a pharmaceutically acceptable salt thereof, a preparation method thereof, and a use of thereof as a therapeutic agent for treating diseases such as constipation caused by long-term use of opioid receptor agonists such as morphine. The drug acts on peripheral nerves, wherein the definitions of the substituents in general formula (I) are the same as those defined in the description.
(FR) La présente invention concerne un dérivé d'antagoniste de récepteur opioïde, un procédé de préparation de celui-ci et une utilisation de celui-ci en médecine. En particulier, la présente invention concerne un dérivé de naloxone tel que décrit par la formule générale (I) et un sel pharmaceutiquement acceptable de celui-ci, un procédé de préparation de celui-ci, et une utilisation de celui-ci en tant qu’agent thérapeutique pour le traitement de maladies telles que la constipation causée par l'utilisation à long terme d'agonistes de récepteur opioïde tels que la morphine. Le médicament agit sur les nerfs périphériques, les définitions des substituants dans la formule générale (I) étant les mêmes que celles indiquées dans la description.
(ZH) 本发明涉及阿片样受体拮抗剂类衍生物、其制备方法及其在医药上的应用。具体而言,本发明涉及一种通式(I)所示的纳洛酮类衍生物、其可药用盐,及其制备方法,以及它们作为治疗剂治疗因长期使用吗啡等阿片样受体激动剂而引起的便秘等疾病的用途,该药物作用于外周神经。其中通式(I)中的各取代基的定义与说明书中的定义相同。
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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, 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 Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)
Also published as:
CN107406456