CN101910127B - 在5位上被取代的(氮杂)吲哚衍生物、包含它的药物组合物、中间体化合物及其制备方法 - Google Patents

在5位上被取代的(氮杂)吲哚衍生物、包含它的药物组合物、中间体化合物及其制备方法 Download PDF

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Publication number
CN101910127B
CN101910127B CN2008801227655A CN200880122765A CN101910127B CN 101910127 B CN101910127 B CN 101910127B CN 2008801227655 A CN2008801227655 A CN 2008801227655A CN 200880122765 A CN200880122765 A CN 200880122765A CN 101910127 B CN101910127 B CN 101910127B
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Chinese (zh)
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CN101910127A (zh
Inventor
M·A·艾里斯
G·富洛蒂
N·卡佐拉
C·毛杰里
P·德拉高内
B·加洛法罗
I·科莱塔
G·曼加诺
B·加罗内
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Angelini Acraf SpA
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Aziende Chimiche Riunite Angelini Francesco ACRAF SpA
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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 C07D451/00 - C07D463/00
    • C07D471/02—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 C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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 containing two hetero rings
    • C07D401/04—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 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN2008801227655A 2007-12-28 2008-12-16 在5位上被取代的(氮杂)吲哚衍生物、包含它的药物组合物、中间体化合物及其制备方法 Expired - Fee Related CN101910127B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP07425830A EP2078711A1 (en) 2007-12-28 2007-12-28 (Aza)indole derivative substituted in position 5, pharmaceutical composition comprising it, intermediate compounds and preparation process therefor
EP07425830.2 2007-12-28
PCT/EP2008/067622 WO2009083436A1 (en) 2007-12-28 2008-12-16 (aza)indole derivative substituted in position 5, pharmaceutical composition comprising it, intermediate compounds and preparation process therefor

Publications (2)

Publication Number Publication Date
CN101910127A CN101910127A (zh) 2010-12-08
CN101910127B true CN101910127B (zh) 2013-01-23

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CN2008801227655A Expired - Fee Related CN101910127B (zh) 2007-12-28 2008-12-16 在5位上被取代的(氮杂)吲哚衍生物、包含它的药物组合物、中间体化合物及其制备方法

Country Status (20)

Country Link
US (2) US8399477B2 (enExample)
EP (3) EP2078711A1 (enExample)
JP (1) JP5698985B2 (enExample)
KR (2) KR20160029861A (enExample)
CN (1) CN101910127B (enExample)
AR (1) AR069961A1 (enExample)
AU (1) AU2008342705B2 (enExample)
BR (1) BRPI0821450A2 (enExample)
CA (1) CA2707339C (enExample)
DK (2) DK2234968T3 (enExample)
EA (1) EA020373B1 (enExample)
ES (2) ES2523167T3 (enExample)
GE (1) GEP20125547B (enExample)
IL (1) IL206062A (enExample)
PL (2) PL2234968T3 (enExample)
PT (2) PT2444392E (enExample)
SG (1) SG187400A1 (enExample)
SI (2) SI2234968T1 (enExample)
UA (1) UA100867C2 (enExample)
WO (1) WO2009083436A1 (enExample)

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KR101365824B1 (ko) 2010-10-22 2014-02-20 엘지디스플레이 주식회사 유기전계발광소자
UA121309C2 (uk) 2014-02-03 2020-05-12 Вітае Фармасьютікалс, Ллс Дигідропіролопіридинові інгібітори ror-гамма
ES2838625T3 (es) * 2014-04-14 2021-07-02 Shanghai hengrui pharmaceutical co ltd Derivados de amida y sales farmacéuticamente aceptables de los mismos, su método de preparación y aplicación médica de los mismos
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
ES2856931T3 (es) 2015-08-05 2021-09-28 Vitae Pharmaceuticals Llc Moduladores de ROR-gamma
MX385332B (es) 2015-11-20 2025-03-18 Vitae Pharmaceuticals Llc Moduladores de ror-gamma.
TW202220968A (zh) 2016-01-29 2022-06-01 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
CN107033026A (zh) * 2017-06-07 2017-08-11 李博强 一种对硝基苯肼盐酸盐的制备方法
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
CN111225914B (zh) 2017-07-24 2022-10-11 生命医药有限责任公司 RORγ的抑制剂
WO2021040393A1 (ko) 2019-08-26 2021-03-04 국제약품 주식회사 인돌 카복사미드 유도체 및 그를 포함하는 약제학적 조성물
CN114605303A (zh) * 2022-03-14 2022-06-10 武汉工程大学 一种地拉韦啶及其中间体的合成方法
CN119019389A (zh) * 2024-06-05 2024-11-26 四川大学 7-氮杂吲哚类化合物及其合成方法和用途
CN119101040B (zh) * 2024-11-08 2025-03-21 杭州澳赛诺医药技术有限公司 一种通过去对称化合成芳基取代的手性四氢吡喃环的方法

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FR2354766A1 (fr) * 1976-06-17 1978-01-13 Labaz Derives n-aminoalkyles d'indole et procedes pour les preparer
EP1060166A1 (de) * 1998-02-03 2000-12-20 Boehringer Ingelheim Pharma KG 5-gliedrige benzokondensierte heterocyclen als antithrombotika
US6114532A (en) * 1998-02-03 2000-09-05 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, the preparation thereof, and their use as pharmaceuticals
DE19834751A1 (de) * 1998-08-01 2000-02-03 Boehringer Ingelheim Pharma Disubstituierte bicyclische Heterocyclen, ihre Herstellung und ihre Verwendung als Arzneimittel
CA2402516A1 (en) * 2000-03-20 2001-09-27 Roopa Rai Non-amidine containing protease inhibitors
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IL140096A0 (en) * 2000-12-05 2002-02-10 Internat Specialty Products Is Process for preparation of zafirlukast
DE10147672A1 (de) * 2001-09-27 2003-04-10 Bayer Ag Substituierte 2,5-Diamidoindole und ihre Verwendung
JP2006511562A (ja) * 2002-12-20 2006-04-06 バイエル・ヘルスケア・アクチェンゲゼルシャフト 泌尿器系疾患の処置のための置換２，５−ジアミドインドール類の使用
SE0300908D0 (sv) * 2003-03-31 2003-03-31 Astrazeneca Ab Azaindole derivatives, preparations thereof, uses thereof and compositions containing them
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Publication number Publication date
JP5698985B2 (ja) 2015-04-08
AU2008342705A1 (en) 2009-07-09
SI2234968T1 (sl) 2013-06-28
PL2444392T3 (pl) 2015-03-31
US8399477B2 (en) 2013-03-19
IL206062A (en) 2015-08-31
US20130158269A1 (en) 2013-06-20
EP2234968B1 (en) 2013-03-27
UA100867C2 (uk) 2013-02-11
KR20160029861A (ko) 2016-03-15
HK1165410A1 (en) 2012-10-05
EA201070804A1 (ru) 2010-12-30
GEP20125547B (en) 2012-05-25
EP2078711A1 (en) 2009-07-15
EP2234968A1 (en) 2010-10-06
ES2408955T3 (es) 2013-06-24
AU2008342705B2 (en) 2013-11-14
KR101671874B1 (ko) 2016-11-03
HK1145172A1 (en) 2011-04-08
ES2523167T3 (es) 2014-11-21
WO2009083436A1 (en) 2009-07-09
PT2444392E (pt) 2014-11-19
PT2234968E (pt) 2013-06-03
US8871948B2 (en) 2014-10-28
CN101910127A (zh) 2010-12-08
EA020373B1 (ru) 2014-10-30
DK2234968T3 (da) 2013-06-17
CA2707339C (en) 2018-05-01
PL2234968T3 (pl) 2013-08-30
BRPI0821450A2 (pt) 2015-06-16
EP2444392A1 (en) 2012-04-25
IL206062A0 (en) 2010-11-30
AR069961A1 (es) 2010-03-03
CA2707339A1 (en) 2009-07-09
EP2444392B1 (en) 2014-09-24
SG187400A1 (en) 2013-02-28
KR20100103569A (ko) 2010-09-27
DK2444392T3 (en) 2014-12-08
SI2444392T1 (sl) 2014-12-31
JP2011507929A (ja) 2011-03-10
US20100286189A1 (en) 2010-11-11

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