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1. (WO2019042267) PYRROLE-2-FORMAMIDE COMPOUND, AND PREPARATION METHOD THEREFOR AND APPLICATIONS THEREOF
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Pub. No.: WO/2019/042267 International Application No.: PCT/CN2018/102618
Publication Date: 07.03.2019 International Filing Date: 28.08.2018
IPC:
C07D 207/30 (2006.01) ,C07D 401/02 (2006.01) ,C07D 403/02 (2006.01) ,C07D 471/02 (2006.01) ,A61K 31/402 (2006.01) ,A61K 31/4025 (2006.01) ,A61P 31/04 (2006.01) ,A61P 31/06 (2006.01)
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
30
having two double bonds between ring members or between ring members and non-ring members
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
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
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
402
1-aryl-substituted, e.g. piretanide
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
4025
not condensed and containing further heterocyclic rings, e.g. cromakalim
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
04
Antibacterial agents
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
04
Antibacterial agents
06
for tuberculosis
Applicants:
中国医学科学院药物研究所 INSTITUTE OF MATERIA MEDICA ,CHINESE ACADEMY OF MEDICAL SCIENCES [CN/CN]; 中国北京市 西城区南纬路甲2号张徐斌 ZHANG, Xubin NO.A2, Nan Wei Road,Xicheng District Beijing 100050, CN
Inventors:
黄海洪 HUANG, Haihong; CN
张东峰 ZHANG, Dongfeng; CN
高永鑫 GAO, Yongxin; CN
林紫云 LIN, Ziyun; CN
赵红义 ZHAO, Hongyi; CN
高猛 GAO, Meng; CN
马辰 MA, Chen; CN
李燕 LI, Yan; CN
盛莉 SHENG, Li; CN
Priority Data:
201710749746.628.08.2017CN
Title (EN) PYRROLE-2-FORMAMIDE COMPOUND, AND PREPARATION METHOD THEREFOR AND APPLICATIONS THEREOF
(FR) COMPOSÉ PYRROLE-2-FORMAMIDE, SON PROCÉDÉ DE PRÉPARATION ET SES APPLICATIONS
(ZH) 吡咯-2-甲酰胺类化合物及其制备方法和用途
Abstract:
(EN) Disclosed in the present invention are a pyrrole-2-formamide compound, a preparation method therefor, a pharmaceutical composition thereof, and application thereof in the preparation of drugs for treating or preventing infective diseases caused by mycobacterium tuberculosis. Specifically, the present invention relates to a compound represented in formula (I), a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the component in the present invention, R1 and R2 being shown in the specifications. The present invention aims at preparing a new compound for resisting against the activity of mycobacterium tuberculosis; and as a new potential drug, the compound can be used for overcoming the problems related to drug resistance of mycobacterium tuberculosis.
(FR) La présente invention concerne un composé pyrrole-2-formamide, son procédé de préparation, une composition pharmaceutique de celui-ci, et son application dans la préparation de médicaments pour le traitement ou la prévention de maladies infectieuses provoquées par mycobacterium tuberculosis. La présente invention concerne particulièrement, un composé représenté par la formule (I), un sel pharmaceutiquement acceptable de celui-ci et une composition pharmaceutique comprenant le composant selon la présente invention, R1 et R2 étant représentés dans les spécifications. La présente invention concerne la préparation d'un nouveau composé résistant à l'activité de mycobacterium tuberculosis ; et, en tant que nouveau médicament potentiel, le composé peut être utilisé pour résoudre des problèmes liés à la résistance aux médicaments de mycobacterium tuberculosis.
(ZH) 本发明公开了吡咯-2-甲酰胺类化合物、其制备方法、药物组合物及在制备治疗或预防结核分枝杆菌引起的感染性疾病药物中的应用。具体地说,本发明涉及式(I)所示化合物,其药学可接受的盐以及包含本发明化合物的药物组合物,其中R 1和R 2如说明书所述。本发明旨在制备具有抗结核分枝杆菌活性的新化合物,其作为潜在的新药物,同时可用于克服与结核分枝杆菌耐药相关的问题。
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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)