JP6223452B2 - インドールカルボキサミド誘導体およびその使用 - Google Patents

インドールカルボキサミド誘導体およびその使用 Download PDF

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Publication number
JP6223452B2
JP6223452B2 JP2015530536A JP2015530536A JP6223452B2 JP 6223452 B2 JP6223452 B2 JP 6223452B2 JP 2015530536 A JP2015530536 A JP 2015530536A JP 2015530536 A JP2015530536 A JP 2015530536A JP 6223452 B2 JP6223452 B2 JP 6223452B2
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JP
Japan
Prior art keywords
indole
carboxamide
methylcyclohexyl
dichloro
tuberculosis
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Expired - Fee Related
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JP2015530536A
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Japanese (ja)
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JP2015527388A (ja
Inventor
イリチェク，ヤン
レディ コンドレディ，ラヴィンダー
レディ コンドレディ，ラヴィンダー
ウィリアム スミス，ポール
ウィリアム スミス，ポール
Original Assignee
ノバルティス アーゲー
ノバルティス アーゲー
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015530536A 2012-09-07 2013-09-05 インドールカルボキサミド誘導体およびその使用 Expired - Fee Related JP6223452B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261698033P 2012-09-07 2012-09-07
US61/698,033 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
JP2015527388A JP2015527388A (ja) 2015-09-17
JP6223452B2 true JP6223452B2 (ja) 2017-11-01

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JP2015530536A Expired - Fee Related JP6223452B2 (ja) 2012-09-07 2013-09-05 インドールカルボキサミド誘導体およびその使用

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Country Link
US (3) US9447039B2 (cg-RX-API-DMAC7.html)
EP (1) EP2892880B1 (cg-RX-API-DMAC7.html)
JP (1) JP6223452B2 (cg-RX-API-DMAC7.html)
KR (1) KR20150048759A (cg-RX-API-DMAC7.html)
CN (1) CN104603106B (cg-RX-API-DMAC7.html)
BR (1) BR112015004666B1 (cg-RX-API-DMAC7.html)
CA (1) CA2881351A1 (cg-RX-API-DMAC7.html)
EA (1) EA028093B1 (cg-RX-API-DMAC7.html)
ES (1) ES2660210T3 (cg-RX-API-DMAC7.html)
IN (1) IN2015DN01163A (cg-RX-API-DMAC7.html)
WO (1) WO2014037900A1 (cg-RX-API-DMAC7.html)

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WO2015164482A1 (en) * 2014-04-22 2015-10-29 The Johns Hopkins University Inhibitors of drug-resistant mycobacterium tuberculosis
HUE050706T2 (hu) * 2014-10-24 2020-12-28 Bristol Myers Squibb Co Indol karboxamid vegyületek, amelyek hasznosak kináz inhibitorokként
JP6878460B2 (ja) * 2016-04-15 2021-05-26 浙江中科▲創▼越▲薬▼▲業▼有限公司 複素環カルボン酸アミド配位子および銅触媒によるハロゲン化アリールのカップリング反応におけるその使用
CN106085868B (zh) * 2016-06-15 2019-07-12 中国医学科学院医药生物技术研究所 一株曲霉菌及其应用
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
AU2018231120B2 (en) 2017-03-10 2022-06-23 Rutgers, The State University Of New Jersey Indole derivatives as efflux pump inhibitors
US11180459B2 (en) 2017-03-10 2021-11-23 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
US11938114B2 (en) 2017-03-10 2024-03-26 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
WO2018218192A1 (en) 2017-05-26 2018-11-29 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
US11458121B2 (en) 2017-06-26 2022-10-04 Rutgers, The State University Of New Jersey Therapeutic compounds and methods to treat infection
US11718633B2 (en) 2018-05-17 2023-08-08 Council Of Scientific And Industrial Research Indole compounds, process for the preparation and use thereof
KR102219563B1 (ko) * 2019-02-15 2021-02-24 에스티팜 주식회사 페나진 유도체 제조를 위한 중간체 및 그의 제조방법
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
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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
KR20220069969A (ko) * 2019-09-26 2022-05-27 더 글로벌 얼라이언스 포 티비 드러그 디벨롭먼트, 잉크. 인돌 카복사미드 화합물 및 마이코박테리아 감염 치료를 위한 이의 용도
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
CN115583908B (zh) * 2021-07-05 2024-08-06 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
EA201590504A1 (ru) 2015-07-30
IN2015DN01163A (cg-RX-API-DMAC7.html) 2015-06-26
US9447039B2 (en) 2016-09-20
WO2014037900A1 (en) 2014-03-13
CN104603106B (zh) 2017-05-10
BR112015004666A2 (pt) 2017-07-04
KR20150048759A (ko) 2015-05-07
ES2660210T3 (es) 2018-03-21
EP2892880B1 (en) 2017-11-22
EA028093B1 (ru) 2017-10-31
US20150175539A1 (en) 2015-06-25
CA2881351A1 (en) 2014-03-13
AU2013311235A1 (en) 2015-02-26
CN104603106A (zh) 2015-05-06
EP2892880A1 (en) 2015-07-15
JP2015527388A (ja) 2015-09-17
BR112015004666B1 (pt) 2022-04-26
US20210032202A1 (en) 2021-02-04
AU2013311235B2 (en) 2016-03-24
US20160355477A1 (en) 2016-12-08

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