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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (enExample)
EP (1) EP2892880B1 (enExample)
JP (1) JP6223452B2 (enExample)
KR (1) KR20150048759A (enExample)
CN (1) CN104603106B (enExample)
BR (1) BR112015004666B1 (enExample)
CA (1) CA2881351A1 (enExample)
EA (1) EA028093B1 (enExample)
ES (1) ES2660210T3 (enExample)
IN (1) IN2015DN01163A (enExample)
WO (1) WO2014037900A1 (enExample)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015150097A1 (en) 2014-04-04 2015-10-08 Iomet Pharma Ltd Indole derivatives for use in medicine
US20170044100A1 (en) * 2014-04-22 2017-02-16 The Johns Hopkins University Inhibitors of drug-resistant mycobacterium tuberculosis
DK3461821T3 (da) * 2014-10-24 2020-08-17 Bristol Myers Squibb Co Indolcarboxamidforbindelser, der er brugbar som kinasehæmmere
WO2017177979A1 (zh) * 2016-04-15 2017-10-19 中国科学院上海有机化学研究所 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
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
KR102697360B1 (ko) 2017-03-10 2024-08-20 루트거스, 더 스테이트 유니버시티 오브 뉴 저지 유출 펌프 억제제로서의 인돌 유도체
US11938114B2 (en) 2017-03-10 2024-03-26 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
US11180459B2 (en) 2017-03-10 2021-11-23 Rutgers, The State University Of New Jersey Bacterial efflux pump inhibitors
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
US20220396586A1 (en) * 2019-09-26 2022-12-15 The Global Alliance For Tb Drug Development, Inc. Thiazole carboxamide compounds and use thereof for the treatment of mycobacterial infections
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
EP4034108A4 (en) * 2019-09-26 2023-09-13 The Global Alliance for TB Drug Development, Inc. AZAINDOLE CARBOXAMIDE COMPOUNDS FOR THE TREATMENT OF MYCOBACTERIAL INFECTIONS
EP4034103A4 (en) * 2019-09-26 2023-10-25 The Global Alliance for TB Drug Development, Inc. Indole carboxamide compounds and use thereof 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
US12012398B2 (en) * 2021-07-12 2024-06-18 Nido Biosciences, Inc. Bicyclic compounds as androgen receptor modulators
GEAP202516792A (en) * 2022-12-02 2025-10-10 Merck Sharp & Dohme Llc Preparation of fused azole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101087781A (zh) * 2004-12-23 2007-12-12 阿斯利康(瑞典)有限公司 用于治疗肺结核的吲哚衍生物
JP2012107001A (ja) * 2010-10-22 2012-06-07 Shionogi & Co Ltd インドールアミド化合物を含有する医薬

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US883049A (en) * 1907-09-12 1908-03-24 John W Piver Tongue-and-groove joint for flooring.
FR2705095B1 (fr) * 1993-05-12 1995-06-23 Adir Nouveaux indoles substitués, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
HU227197B1 (en) * 2000-10-24 2010-10-28 Richter Gedeon Nyrt Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them
WO2003000657A1 (en) 2001-06-20 2003-01-03 Daiichi Pharmaceutical Co., Ltd. Diamine derivatives
US7129225B2 (en) 2001-10-22 2006-10-31 The Research Foundation Of State University Of New York Protection against and treatment of hearing loss
US6759428B2 (en) 2001-12-04 2004-07-06 Roche Palo Alto Llc Indole nitriles
MXPA04005263A (es) 2001-12-04 2004-10-11 Hoffmann La Roche 2-amino-cicloalcanocarboxamidas substituidas y su uso como inhibidores de cisteina proteasa.
JPWO2003091213A1 (ja) * 2002-04-25 2005-09-02 アステラス製薬株式会社 新規なアミド誘導体又はその塩
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
CA2617123C (en) * 2005-08-12 2015-05-26 United States Government As Represented By The Secretary Of The United States Army And The U.S. Army Medical Research & Materiel Command Broad spectrum antibacterial compounds
BRPI0710527B8 (pt) 2006-04-04 2021-05-25 Fibrogen Inc compostos de pirrolo- e tiazolo-piridina e composição farmacêutica que os compreende
WO2009063495A2 (en) 2007-09-20 2009-05-22 Cadila Healthcare Limited Substituted indole and its derivatives as cannabinoid modulators
CN102325753B (zh) * 2008-12-19 2014-09-10 百时美施贵宝公司 用作激酶抑制剂的咔唑甲酰胺化合物
AP3069A (en) 2009-02-27 2014-12-31 Siga Technologies Inc Thienopyridine derivatives for the treatment and prvention of dengue virus infection
AU2010278730A1 (en) 2009-07-31 2012-03-01 Biocryst Pharmaceuticals, Inc. Pyrrolo [1, 2-b] pyridazine derivatives as janus kinase inhibitors
AU2010327936B2 (en) 2009-12-11 2015-08-20 Nono Inc. Agents and methods for treating ischemic and other diseases
US9200046B2 (en) * 2011-06-29 2015-12-01 Cornell University Reporter system for high throughput screening of compounds and uses thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101087781A (zh) * 2004-12-23 2007-12-12 阿斯利康(瑞典)有限公司 用于治疗肺结核的吲哚衍生物
JP2012107001A (ja) * 2010-10-22 2012-06-07 Shionogi & Co Ltd インドールアミド化合物を含有する医薬

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Bis(1H-2-indolyl)methanones as a Novel Class of Inhibitors of the Platelet-Derived Growth Factor Receptor Kinase;Siavosh Mahboobi et al;《Journal of Medicinal Chemistry》;20020130;第45卷(第5期);1002-1018 *
Identification and Biochemical Characterization of Small-Molecule Inhibitors of West Nile Virus Serine Protease by a High-Throughput Screen;Niklaus H. Mueller et al;《Antimicrobial Agents and Chemotherapy》;20090131;第53卷(第1期);第341页 *

Also Published As

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

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