Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO2018130124) TRICYCLIC COMPOUND AS SELECTIVE ESTROGEN RECEPTOR DOWN-REGULATOR AND USE THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/130124 International Application No.: PCT/CN2018/071700
Publication Date: 19.07.2018 International Filing Date: 08.01.2018
IPC:
C07D 471/04 (2006.01) ,A61K 31/437 (2006.01) ,A61K 31/4545 (2006.01) ,A61P 35/00 (2006.01) ,A61P 25/28 (2006.01) ,A61P 25/32 (2006.01) ,A61P 25/06 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
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
4353
ortho- or peri-condensed with heterocyclic ring systems
437
the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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
44
Non-condensed pyridines; Hydrogenated derivatives thereof
445
Non-condensed piperidines, e.g. piperocaine
4523
containing further heterocyclic ring systems
4545
containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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
25
Drugs for disorders of the nervous system
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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
30
for treating abuse or dependence
32
Alcohol-abuse
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
06
Antimigraine agents
Applicants:
南京圣和药业股份有限公司 NANJING SANHOME PHARMACEUTICAL CO., LTD. [CN/CN]; 中国江苏省南京市 经济技术开发区惠中路9号 No.9, Huizhong Road, Economic and Technological Development Zone Nanjing, Jiangsu 210038, CN
Inventors:
王勇 WANG, Yong; CN
赵立文 ZHAO, Liwen; CN
王小伟 WANG, Xiaowei; CN
张小猛 ZHANG, Xiaomeng; CN
张雁 ZHANG, Yan; CN
庞司林 PANG, Silin; CN
Agent:
南京众联专利代理有限公司 NANJING ZHONGLIAN PATENT AGENCY CO., LTD; 中国江苏省南京市 建邺区福园街129号万达商务楼7层 7 Floor, Wanda Business Building, No.129 Fuyuan Street, Jianye District Nanjing City, Jiangsu 210017, CN
Priority Data:
201710019392.X11.01.2017CN
Title (EN) TRICYCLIC COMPOUND AS SELECTIVE ESTROGEN RECEPTOR DOWN-REGULATOR AND USE THEREOF
(FR) COMPOSÉ TRICYCLIQUE UTILISÉ EN TANT QUE RÉGULATEUR SÉLECTIF DU RÉCEPTEUR DES ŒSTROGÈNES ET SON UTILISATION
(ZH) 作为选择性雌激素受体下调剂的三环类化合物及其应用
Abstract:
(EN) The present invention falls within the field of medical chemistry, and relates to a tricyclic compound as a selective estrogen receptor down-regulator and the use thereof. In particular, provided in the present invention are a compound as shown in formula I or an isomer, a pharmaceutically acceptable salt, a solvate, a crystal or a prodrug thereof, the preparation method therefor and pharmaceutical compositions containing the compounds and the use of the compounds or compositions for treating and/or preventing estrogen receptor-associated diseases. The compound of the present invention has an even better anti-tumour activity, a longer dosing interval and fewer side effects, and seems to be very promising as a therapeutic agent against breast cancer.
(FR) La présente invention se rapporte au domaine de la chimie médicale et concerne un composé tricyclique utilisé en tant que régulateur sélectif du récepteur des œstrogènes et son utilisation. La présente invention concerne particulièrement, un composé tel que représenté par la formule I ou un isomère, un sel pharmaceutiquement acceptable, un solvate, un cristal ou un promédicament de celui-ci. L'invention concerne également, des procédés de préparation dudit composé et des compositions pharmaceutiques contenant ces composés ainsi qu'une utilisation desdits composés ou compositions pour le traitement et/ou la prévention de maladies associées au récepteur des œstrogènes. Le composé de la présente invention présente une meilleure activité antitumorale, un intervalle de dosage plus long et moins d'effets secondaires et semble être très prometteur en tant qu'agent thérapeutique contre le cancer du sein.
(ZH) 本发明属于医药化学领域,涉及一类作为选择性雌激素受体下调节剂的三环类化合物及其应用,具体地,本发明提供式I所示的化合物或其异构体、药学上可接受的盐、溶剂化物、结晶或前药,它们的制备方法以及含有这些化合物的药物组合物和这些化合物或组合物用于治疗和/或预防雌激素受体相关的疾病的用途。本发明的化合物具有更加优异的抗肿瘤活性,给药间隔更长,副作用更小,非常有希望成为乳腺癌治疗剂。
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)