CN104603106B - 吲哚甲酰胺衍生物及其用途 - Google Patents

吲哚甲酰胺衍生物及其用途 Download PDF

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Publication number
CN104603106B
CN104603106B CN201380046508.9A CN201380046508A CN104603106B CN 104603106 B CN104603106 B CN 104603106B CN 201380046508 A CN201380046508 A CN 201380046508A CN 104603106 B CN104603106 B CN 104603106B
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China
Prior art keywords
indole
carboxamides
methylcyclohexyls
chloro
bis
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Expired - Fee Related
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CN201380046508.9A
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English (en)
Chinese (zh)
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CN104603106A (zh
Inventor
J·基里塞克
R·R·孔德雷蒂
P·W·史密斯
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Novartis AG
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Novartis AG
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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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201380046508.9A 2012-09-07 2013-09-05 吲哚甲酰胺衍生物及其用途 Expired - Fee Related CN104603106B (zh)

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
CN104603106A CN104603106A (zh) 2015-05-06
CN104603106B true CN104603106B (zh) 2017-05-10

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

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EP3444031B1 (en) * 2016-04-15 2022-11-30 CE Pharm Co.,Ltd Heterocyclic carboxylic acid amide ligand and applications thereof in copper catalyzed coupling reaction of aryl halogeno substitute
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
WO2018165612A1 (en) 2017-03-10 2018-09-13 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
CN110770224B (zh) 2017-03-10 2022-11-18 罗格斯新泽西州立大学 作为外排泵抑制剂的吲哚衍生物
EP3630109A4 (en) * 2017-05-26 2021-03-17 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
WO2019220461A1 (en) * 2018-05-17 2019-11-21 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
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
CA3151288A1 (en) * 2019-09-26 2021-04-01 Takushi Kaneko Thiazole carboxamide compounds and use thereof for the treatment of mycobacterial infections
CA3151407A1 (en) * 2019-09-26 2021-04-01 Takushi Kaneko Indole carboxamide compounds and use thereof for the treatment of mycobacterial infections
WO2021062316A1 (en) 2019-09-26 2021-04-01 The Global Alliance For Tb Drug Development, Inc. Azaindole carboxamide compounds for the treatment of mycobacterial infections
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
EP4370207B1 (en) * 2021-07-12 2025-12-17 Nido Biosciences, Inc. Bicyclic compounds as androgen receptor modulators
AR131250A1 (es) * 2022-12-02 2025-02-26 Merck Sharp & Dohme Llc Preparación de derivados condensados de azol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2
CN118724763B (zh) * 2024-09-02 2024-12-06 辽宁龙田化工科技有限公司 一种4-甲基苯磺酰氯合成方法

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Publication number Publication date
BR112015004666B1 (pt) 2022-04-26
ES2660210T3 (es) 2018-03-21
EA028093B1 (ru) 2017-10-31
JP6223452B2 (ja) 2017-11-01
CN104603106A (zh) 2015-05-06
CA2881351A1 (en) 2014-03-13
EA201590504A1 (ru) 2015-07-30
US20150175539A1 (en) 2015-06-25
BR112015004666A2 (pt) 2017-07-04
EP2892880A1 (en) 2015-07-15
JP2015527388A (ja) 2015-09-17
US9447039B2 (en) 2016-09-20
US20160355477A1 (en) 2016-12-08
IN2015DN01163A (https=) 2015-06-26
EP2892880B1 (en) 2017-11-22
AU2013311235A1 (en) 2015-02-26
WO2014037900A1 (en) 2014-03-13
AU2013311235B2 (en) 2016-03-24
US20210032202A1 (en) 2021-02-04
KR20150048759A (ko) 2015-05-07

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