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1. (WO2018219309) VINYLARENE DERIVATIVE AND USE THEREOF
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Pub. No.: WO/2018/219309 International Application No.: PCT/CN2018/089152
Publication Date: 06.12.2018 International Filing Date: 31.05.2018
IPC:
C07C 275/42 (2006.01) ,C07C 273/18 (2006.01) ,C07C 335/22 (2006.01) ,C07D 207/16 (2006.01) ,C07C 275/40 (2006.01) ,A61K 31/196 (2006.01) ,A61K 31/216 (2006.01) ,A61K 31/401 (2006.01) ,A61P 35/00 (2006.01) ,A61P 35/02 (2006.01) ,A61P 31/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28
having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
42
being further substituted by carboxyl groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
273
Preparation of urea or its derivatives, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
18
of substituted ureas
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
335
Thioureas, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
04
Derivatives of thiourea
16
having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
22
being further substituted by carboxyl groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04
having no double bonds between ring members or between ring members and non-ring members
10
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
16
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
275
Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28
having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
40
being further substituted by nitrogen atoms not being part of nitro or nitroso groups
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
185
Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19
Carboxylic acids, e.g. valproic acid
195
having an amino group
196
the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
21
Esters, e.g. nitroglycerine, selenocyanates
215
of carboxylic acids
216
of acids having aromatic rings, e.g. benactizyne, clofibrate
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
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
401
Proline; Derivatives thereof, e.g. captopril
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
35
Antineoplastic agents
02
specific for leukemia
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12
Antivirals
Applicants:
沈阳化工研究院有限公司 SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY [CN/CN]; 中国辽宁省沈阳市 铁西区沈辽东路8号 No.8 Shenliao Dong Road, Tiexi District Shenyang, Liaoning 110021, CN
Inventors:
冉兆晋 RAN, Zhaojin; CN
柴宝山 CHAI, Baoshan; CN
王婉秋 WANG, Wanqiu; CN
光海红 GUANG, Haihong; CN
焦佳媛 JIAO, Jiayuan; CN
Agent:
沈阳科苑专利商标代理有限公司 SHENYANG PATENT & TRADEMARK AGENCY ACADEMIA SINICA; 中国辽宁省沈阳市 和平区三好街24号 24 Sanhao Street, Heping District Shenyang, Liaoning 110014, CN
Priority Data:
201710407896.902.06.2017CN
Title (EN) VINYLARENE DERIVATIVE AND USE THEREOF
(FR) DÉRIVÉ DE VINYLARÈNE ET SON UTILISATION
(ZH) 一种芳乙烯衍生物及其应用
Abstract:
(EN) The present invention relates to a vinylarene derivative which modulates or inhibits the enzymatic activity of indoleamine 2,3-dioxygenase 1 (IDO-1), and the use thereof, and further relates to a vinylarene derivative and the use thereof. The vinylarene derivative is a compound as shown in formula I, a stereoisomer, a cis- or trans-isomer, or a tautomer thereof and a pharmaceutically acceptable salt thereof, has an IDO-1 enzyme inhibitory activity, and is expected to provide brand new therapeutic methods and schemes for related diseases caused by IDO enzymes.
(FR) La présente invention concerne un dérivé de vinylarène qui module ou inhibe l'activité enzymatique de l'indoléamine 2,3-dioxygénase 1 (IDO-1), et son utilisation. L'invention concerne également un dérivé de vinylarène et son utilisation. Le dérivé de vinylarène est un composé tel que représenté par la formule I, un stéréoisomère, un cis- ou trans-isomère, ou un tautomère de celui-ci ainsi qu'un sel pharmaceutiquement acceptable dudit composé, le dérivé de vinylarène a une activité inhibitrice de l'enzyme IDO-1, et devrait fournir de nouveaux procédés et schémas thérapeutiques pour des maladies apparentées provoquées par des enzymes IDO.
(ZH) 本发明涉及调节或抑制吲哚胺 2,3 -双加氧酶 1(IDO-1) 的酶活性的芳乙烯衍生物及其应用,进一步的说一种芳乙烯衍生物及其应用。芳乙烯衍生物为式I所示化合物、其立体异构体、顺反异构体、互变异构体以及其药学上可接受的盐,具有 IDO-1 酶抑制活性,可望提供全新的针对 IDO 酶导致的相关疾病的治疗方法与方案。
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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, 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)