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1. (WO2017133655) BENZOTHIAZINE AND BENZOTHIADIAZINE COMPOUNDS AND PREPARATION AND USE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/133655 International Application No.: PCT/CN2017/072803
Publication Date: 10.08.2017 International Filing Date: 02.02.2017
IPC:
C07D 473/34 (2006.01) ,C07D 473/40 (2006.01) ,C07D 417/12 (2006.01) ,C07D 487/04 (2006.01) ,C07D 519/00 (2006.01) ,C07D 513/04 (2006.01) ,A61K 31/5415 (2006.01) ,A61K 31/542 (2006.01) ,A61K 31/549 (2006.01) ,A61P 35/00 (2006.01) ,A61P 29/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
26
with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
32
Nitrogen atom
34
attached in position 6, e.g. adenine
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
40
with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
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
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
519
Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
513
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
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
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
5415
ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
542
ortho- or peri-condensed with heterocyclic ring 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
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
549
having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
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
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
Applicants:
浙江大学 ZHEJIANG UNIVERSITY [CN/CN]; 中国浙江省杭州市 西湖区浙大路38号 NO.38, Zheda Road, Xihu District Hangzhou, Zhejiang 310027, CN
Inventors:
盛荣 SHENG, Rong; CN
胡永洲 HU, Yongzhou; CN
危俊 WEI, Jun; CN
马晓东 MA, Xiaodong; CN
Agent:
杭州求是专利事务所有限公司 HANGZHOU QIUSHI PATENT OFFICE CO.,LTD.; 中国浙江省杭州市 西湖区玉古路147号黄鸿年科技综合大楼215室/赵杭丽 ZHAO, Hangli Room 215, Huanghongnian Science and Technology Complex Building, No.147, Yugu Road, Xihu District Hangzhou, Zhejiang 310013, CN
Priority Data:
201610080323.504.02.2016CN
Title (EN) BENZOTHIAZINE AND BENZOTHIADIAZINE COMPOUNDS AND PREPARATION AND USE
(FR) BENZOTHIAZINE ET COMPOSÉS BENZOTHIADIAZINE ET PRÉPARATION ET UTILISATION
(ZH) 苯并噻嗪和苯并噻二嗪类化合物及制备和应用
Abstract:
(EN) Provided are benzothiazine and benzothiadiazine and a structural analogue thereof, as well as a pharmaceutically acceptable salt, a stereoisomer and a solvate thereof, having the structure of general formula a. It has been confirmed by multiple experiments that all of the compounds have PI3Kδ inhibiting effects, wherein most of the compounds selectively have significant inhibiting effects on PI3Kδ and can be used in preparing anti-inflammatory drugs and anti-tumour drugs against a wide range of tumours and inflammatory diseases. In particular, the inhibiting effects on recurrent follicular B-cell non-Hodgkin's lymphoma, recurrent chronic lymphocytic leukaemia, and recurrent small lymphocytic lymphoma during the treatment period are better. The drugs prepared by the present invention can be used in combination with other anti-tumour drugs to produce significant effects, thus providing new drugs for clinically treating tumours and inflammatory diseases. General formula (a) of the present invention is as shown in the figure.
(FR) La présente invention concerne une benzothiazine et benzothiadiazine et un analogue structurel de ces dernières, ainsi qu’un sel, un stéréoisomère et un solvate pharmaceutiquement acceptables de ces derniers, ayant la structure de formule générale a. Il a été confirmé par de multiples expérimentations que tous les composés présentent des effets d’inhibition de PI3Kδ, dans lesquels la plupart des composés présentent sélectivement des effets d’inhibition significatifs sur PI3Kδ et peuvent être utilisés dans la préparation de médicaments anti-inflammatoires et de médicaments anti-tumoraux vis-à-vis d’une large plage de tumeurs et de maladies inflammatoires. En particulier, les effets d’inhibition sur le lymphome récurrent folliculaire des cellules B non hodgkinien, les leucémies lymphocytaires chroniques récurrentes, et le lymphome lymphocytaire à petits lymphocytes récurrent durant la période de traitement sont meilleurs. Les médicaments préparés grâce à la présente invention peuvent être utilisés en combinaison avec d’autres médicaments anti-tumoraux pour produire des effets significatifs, fournissant ainsi de nouveaux médicaments destinés au traitement de manière clinique des tumeurs et des maladies inflammatoires. La formule générale (a) de la présente invention est telle que présentée dans la figure.
(ZH) 本发明提供一种苯并噻嗪和苯并噻二嗪及其结构类似物,以及其药学上可接受的盐、立体异构体、溶剂合物,具有通式a的结构。经多次实验证实,所述化合物均具有PI3Kδ抑制作用,其中大部分化合物选择性的对PI3Kδ有显著的抑制作用,可在制备抗炎和抗肿瘤药物中的应用,涉及的肿瘤及炎性疾病范围广,尤其是对在治疗期复发的滤泡B-细胞非霍奇金淋巴瘤、复发的慢性淋巴细胞性白血病、复发的小淋巴细胞淋巴瘤的抑制效果更佳。本发明制备的药物能和其他抗肿瘤药联合使用,效果显著,为临床抗肿瘤和抗炎性疾病提供新的治疗药物。本发明的通式(a)如图所示。
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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 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)