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1. (WO2019042442) COMPOUND HAVING TYROSINE PROTEIN KINASE JAK1- OR JAK2-INHIBITTION AND DEGRADATION ACTIVITY
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Pub. No.: WO/2019/042442 International Application No.: PCT/CN2018/103707
Publication Date: 07.03.2019 International Filing Date: 02.09.2018
IPC:
C07D 487/04 (2006.01) ,A61K 31/519 (2006.01) ,A61P 35/00 (2006.01) ,A61P 37/06 (2006.01) ,A61P 19/02 (2006.01) ,A61P 17/06 (2006.01) ,A61P 17/00 (2006.01) ,A61P 11/06 (2006.01) ,A61P 3/10 (2006.01) ,A61P 1/04 (2006.01) ,A61P 1/00 (2006.01) ,A61P 25/28 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
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
37
Drugs for immunological or allergic disorders
02
Immunomodulators
06
Immunosuppressants, e.g. drugs for graft rejection
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
02
for joint disorders, e.g. arthritis, arthrosis
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
06
Antipsoriatics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17
Drugs for dermatological disorders
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
06
Antiasthmatics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
08
for glucose homeostasis
10
for hyperglycaemia, e.g. antidiabetics
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
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
Applicants:
上海美志医药科技有限公司 SHANGHAI MEIZER PHARMACEUTICALS CO., LTD. [CN/CN]; 中国上海市 浦东新区万祥镇宏祥北路83弄1-42号20幢118室 Room 118 Building 20, No. 1-42, Lane 83, Hongxiang North Road, Wanxiang Town, Pudong New Area Shanghai 201313, CN
Inventors:
舒永志 SHU, Yongzhi; CN
Agent:
上海德禾翰通律师事务所 DEHEHANTONG LAW FIRM; 中国上海市 徐汇区宜山路425号光启城2102室 Room 2102 21st Floor, Pole Tower, No. 425 Yishan Rd., Xuhui District Shanghai 200233, CN
Priority Data:
201710783082.503.09.2017CN
Title (EN) COMPOUND HAVING TYROSINE PROTEIN KINASE JAK1- OR JAK2-INHIBITTION AND DEGRADATION ACTIVITY
(FR) COMPOSÉ AYANT UNE ACTIVITÉ D'INHIBITION ET DE DÉGRADATION DE PROTÉINE TYROSINE KINASE JAK1 OU JAK2
(ZH) 一类具有抑制并降解酪氨酸蛋白激酶JAK1或JAK2活性的化合物
Abstract:
(EN) The present invention provides a compound having tyrosine protein kinase JAK1- or JAK2-inhibittion and degradation activity. Specifically, the present invention provides a compound as represented by the following formula I, wherein the definition of each group is as stated in the description. The compound provided by the present invention has excellent JAK1- or JAK2-inhibittion and degradation activity, and can be used for preparing drugs for treatment of JAK1- or JAK2-related diseases.
(FR) La présente invention concerne un composé ayant une activité d'inhibition et de dégradation de protéine tyrosine kinase JAK1 ou JAK2. La présente invention concerne particulièrement, un composé tel que représenté par la formule suivante I, dans laquelle la définition de chaque groupe est telle que décrite dans la description. Le composé selon la présente invention présente d'excellentes activités d'inhibition et de dégradation de JAK1 ou JAK2, et peut être utilisé pour préparer des médicaments pour le traitement de maladies liées à JAK1 ou à JAK2.
(ZH) 本发明提供了一类具有抑制并降解酪氨酸蛋白激酶JAK1或JAK2活性的化合物,具体地,本发明提供了一种如下式I所示的化合物;其中,各基团的定义如说明书中所述。本发明的化合物具有很好的JAK1或JAK2抑制及降解活性,可以用于制备治疗间JAK1或JAK2相关的疾病的药物。
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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)