EA201590504A1 - Индолкарбоксамидные производные и их применение - Google Patents

Индолкарбоксамидные производные и их применение

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Publication number
EA201590504A1
EA201590504A1 EA201590504A EA201590504A EA201590504A1 EA 201590504 A1 EA201590504 A1 EA 201590504A1 EA 201590504 A EA201590504 A EA 201590504A EA 201590504 A EA201590504 A EA 201590504A EA 201590504 A1 EA201590504 A1 EA 201590504A1
Authority
EA
Eurasian Patent Office
Prior art keywords
indolkarboxamid
derivatives
application
present
irreplaceable
Prior art date
Application number
EA201590504A
Other languages
English (en)
Other versions
EA028093B1 (ru
Inventor
Ян Йирицек
Равиндер Редди Кондредди
Пол Уилльям Смит
Original Assignee
Новартис Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201590504A1 publication Critical patent/EA201590504A1/ru
Publication of EA028093B1 publication Critical patent/EA028093B1/ru

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Abstract

Настоящее изобретение относится к соединениям формулы (I), для которых показано, что они являются пригодными в лечении заболевания, расстройства или синдрома, которые опосредованы транспортировкой незаменимых молекул в mmpL3 пути: (I) где R, R, R, R, Rи Rопределены в настоящем изобретении.
EA201590504A 2012-09-07 2013-09-05 Индолкарбоксамидные производные и их применение EA028093B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261698033P 2012-09-07 2012-09-07
PCT/IB2013/058318 WO2014037900A1 (en) 2012-09-07 2013-09-05 Indole carboxamide derivatives and uses thereof

Publications (2)

Publication Number Publication Date
EA201590504A1 true EA201590504A1 (ru) 2015-07-30
EA028093B1 EA028093B1 (ru) 2017-10-31

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201590504A EA028093B1 (ru) 2012-09-07 2013-09-05 Индолкарбоксамидные производные и их применение

Country Status (11)

Country Link
US (3) US9447039B2 (ru)
EP (1) EP2892880B1 (ru)
JP (1) JP6223452B2 (ru)
KR (1) KR20150048759A (ru)
CN (1) CN104603106B (ru)
BR (1) BR112015004666B1 (ru)
CA (1) CA2881351A1 (ru)
EA (1) EA028093B1 (ru)
ES (1) ES2660210T3 (ru)
IN (1) IN2015DN01163A (ru)
WO (1) WO2014037900A1 (ru)

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WO2015164482A1 (en) * 2014-04-22 2015-10-29 The Johns Hopkins University Inhibitors of drug-resistant mycobacterium tuberculosis
AR102426A1 (es) * 2014-10-24 2017-03-01 Bristol Myers Squibb Co Compuestos de indolcarboxamida como inhibidores de btk
CN107298650B (zh) * 2016-04-15 2022-11-15 浙江中科创越药业有限公司 杂环羧酸酰胺配体及其在铜催化芳基卤代物偶联反应中的用途
CN110305798B (zh) * 2016-06-15 2021-11-19 中国医学科学院医药生物技术研究所 一株曲霉菌的用途及由该曲霉菌制备的化合物及其用途
US10383848B2 (en) * 2016-08-04 2019-08-20 Creighton University Indole-based therapeutics
US10858319B2 (en) 2016-10-03 2020-12-08 Iomet Pharma Ltd. Indole derivatives for use in medicine
US11938114B2 (en) 2017-03-10 2024-03-26 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
WO2018165612A1 (en) 2017-03-10 2018-09-13 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
US11826357B2 (en) 2017-05-26 2023-11-28 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
WO2019005841A1 (en) * 2017-06-26 2019-01-03 Rutgers, The State University Of New Jersey THERAPEUTIC COMPOUNDS AND METHODS FOR TREATING INFECTION
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KR102219563B1 (ko) * 2019-02-15 2021-02-24 에스티팜 주식회사 페나진 유도체 제조를 위한 중간체 및 그의 제조방법
CN110577483B (zh) * 2019-09-26 2020-05-12 海南医学院 一种3,3-二取代-2-吲哚酮的绿色合成方法
WO2021062318A1 (en) * 2019-09-26 2021-04-01 The Global Alliance For Tb Drug Development, Inc. Thiazole carboxamide compounds and use thereof for the treatment of mycobacterial infections
CN114746090A (zh) * 2019-09-26 2022-07-12 结核病药物开发全球联盟公司 用于治疗分枝杆菌感染的氮杂吲哚甲酰胺化合物
BR112022005723A2 (pt) * 2019-09-26 2022-08-23 The Global Alliance For Tb Drug Dev Inc Compostos de indol carboxamida e seu uso para o tratamento de infecções micobacterianas
RU2767542C1 (ru) * 2021-05-24 2022-03-17 Федеральное государственное автономное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" (ПГНИУ) Противотуберкулезное средство на основе 4-((гет)ароил)-3- гидрокси-1-(2-гидроксифенил)-5-(фенилтио)-1,5-дигидро-2Н-пиррол-2-онов
CN115583908A (zh) * 2021-07-05 2023-01-10 西北农林科技大学 一种吲哚甲酰胺类化合物及其制备方法和用途
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Also Published As

Publication number Publication date
BR112015004666A2 (pt) 2017-07-04
JP6223452B2 (ja) 2017-11-01
EP2892880A1 (en) 2015-07-15
EA028093B1 (ru) 2017-10-31
WO2014037900A1 (en) 2014-03-13
EP2892880B1 (en) 2017-11-22
ES2660210T3 (es) 2018-03-21
IN2015DN01163A (ru) 2015-06-26
BR112015004666B1 (pt) 2022-04-26
AU2013311235B2 (en) 2016-03-24
AU2013311235A1 (en) 2015-02-26
KR20150048759A (ko) 2015-05-07
CN104603106A (zh) 2015-05-06
US20150175539A1 (en) 2015-06-25
US20210032202A1 (en) 2021-02-04
CN104603106B (zh) 2017-05-10
CA2881351A1 (en) 2014-03-13
JP2015527388A (ja) 2015-09-17
US9447039B2 (en) 2016-09-20
US20160355477A1 (en) 2016-12-08

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