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1. (WO2018107332) CLASS OF CHIRAL AROMATIC HETEROAMINE DERIVATIVE, SYNTHESIS METHOD AND APPLICATION THEREOF
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Pub. No.: WO/2018/107332 International Application No.: PCT/CN2016/109522
Publication Date: 21.06.2018 International Filing Date: 12.12.2016
IPC:
C07D 277/46 (2006.01) ,A61K 31/426 (2006.01) ,A61P 31/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
277
Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
02
not condensed with other rings
20
having two or three double bonds between ring members or between ring members and non-ring members
32
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
38
Nitrogen atoms
44
Acylated amino or imino radicals
46
by carboxylic acids, or sulfur or nitrogen analogues thereof
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
425
Thiazoles
426
1,3-Thiazoles
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: SUN YAT-SEN UNIVERSITY[CN/CN]; SHAN Xiangjie NO. 135 Xingangxi Road, Haizhu District Guangzhou, Guangdong 510275, CN
Inventors: ZHANG, Hui; CN
BO, Chuan; CN
PAN, Ting; CN
WU, Liyang; CN
Agent: YOGO PATENT & TRADEMARK AGENCY LIMITED COMPANY; Room 4416, Tower B, SINOPEC Building, No. 191 Tiyu West Road, Tianhe District Guangzhou, Guangdong 510642, CN
Priority Data:
Title (EN) CLASS OF CHIRAL AROMATIC HETEROAMINE DERIVATIVE, SYNTHESIS METHOD AND APPLICATION THEREOF
(FR) CLASSE DE DÉRIVÉ CHIRAL D'HÉTÉROAMINE AROMATIQUE, PROCÉDÉ DE SYNTHÈSE ET APPLICATION ASSOCIÉS
(ZH) 一类手性芳杂胺类衍生物及其合成方法和应用
Abstract:
(EN) The invention belongs to the technical field of compound synthesis, and specifically discloses a class of chiral aromatic heteroamine derivative and a synthesis method and application thereof. The chiral aromatic heteroamine derivative has a structure represented by formula (I), wherein R1 and R2 are independently selected from hydrogen or halogen; R3 is an alkoxyl, phenyl, methoxyl, alkynyl, cyano or dihalogen-substituted phenyl ring, a 5- or 6-membered heterocyclic, methoxyl, alkynyl, cyano, mono- or dihalogen-substituted 5- or 6-membered heterocyclic ring, or a fused heterocyclic ring; X is oxygen or nitrogen; and Y is carbonyl or sulfonyl. The chiral aromatic heteroamine derivative synthesized by the invention has a function of inhibiting assembly of a Hepatitis B virus core protein, and thus can fundamentally inhibit replication of the Hepatitis B virus, and has wide application prospects in the treatment of Hepatitis B virus-caused diseases.
(FR) L'invention relève du domaine technique de la synthèse de composés, et concerne spécifiquement une classe de dérivés chiraux d'hétéroamine aromatique et un procédé de synthèse et une application associés. Le dérivé chiral d'hétéroamine aromatique a une structure représentée par la formule (I), dans laquelle R1 and R2 sont indépendamment sélectionnés parmi un atome d'hydrogène ou d'halogène ; R3 est un cycle alcoxyle, phényle, méthoxyle, alcynyle, cyano, ou phényle à substitution dihalogéno, un cycle hétérocyclique à 5 ou 6 chaînons, méthoxyle, alcynyle, cyano, hétérocyclique à 5 ou 6 chaînons à substitution mono- ou dihalogéno, ou un cycle hétérocyclique fusionné ; X représente un atome d'oxygène ou d'azote ; et Y représente un groupe carbonyle ou sulfonyle. Le dérivé chiral d'hétéroamine aromatique synthétisé par l'invention a une fonction d'inhibition de l'assemblage d'une protéine capsidique du virus de l'hépatite B, et peut ainsi inhiber fondamentalement la réplication du virus de l'hépatite B, et présente de vastes perspectives d'application dans le traitement de maladies provoquées par le virus de l'hépatite B.
(ZH) 本发明属于化合物合成技术领域,具体公开了一类手性芳杂胺类衍生物及其合成方法和应用。手性芳杂胺类衍生物具有式(I)所示结构,其中,R1、R2独立选自氢或卤素;R3为烷氧基,苯环,甲氧基、炔基、氰基或双卤素取代的苯环,五元或六元杂环,甲氧基、炔基、氰基,单卤素或双卤素取代的五元或六元杂环,稠杂环;X为氧或氮;Y为羰基或磺酰基。本发明合成的手性芳杂胺类衍生物具有抑制乙肝病毒核心蛋白组装的作用,能从根本上抑制乙肝病毒的复制,在乙肝病毒病治疗方面具有广泛的应用前景。
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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)