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)
  • 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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (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) ES2408955T3 (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)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101365824B1 (ko) 2010-10-22 2014-02-20 엘지디스플레이 주식회사 유기전계발광소자
DK3102576T3 (da) 2014-02-03 2019-07-22 Vitae Pharmaceuticals Llc Dihydropyrrolopyridininhibitorer af ror-gamma
KR20160134865A (ko) * 2014-04-14 2016-11-23 샹하이 헨그루이 파마수티컬 컴퍼니 리미티드 아미드 유도체 및 이의 약제학적으로 허용되는 염, 이의 제조방법 및 이의 의학적 적용
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
EP3331876B1 (en) 2015-08-05 2020-10-07 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
EP3868750A1 (en) 2015-11-20 2021-08-25 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
TWI757266B (zh) 2016-01-29 2022-03-11 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
CN115716826A (zh) 2017-07-24 2023-02-28 生命医药有限责任公司 RORγ的抑制剂
CN114302874B (zh) * 2019-08-26 2025-02-25 国际药品株式会社 吲哚甲酰胺衍生物和包含吲哚甲酰胺衍生物的药物组合物
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
CN119019389B (zh) * 2024-06-05 2026-05-26 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
WO1999040072A1 (de) * 1998-02-03 1999-08-12 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
US20030225036A1 (en) * 2000-03-20 2003-12-04 Aleksandr Kolesnikov Non-amidine containing protease inhibitors
US20020052373A1 (en) * 2000-10-26 2002-05-02 Zorn Stevin H. Combination treatment for dementia or cognitive deficits associated with alzheimer's disease and parkinson's disease
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
EP1833829A2 (en) * 2004-12-23 2007-09-19 F. Hoffmann-Roche AG Benzamide substituted imidazo- and pyrrolo-pyridines as protein kinase inhibitors
EP1933834A1 (en) * 2005-10-12 2008-06-25 Biolipox AB Benzoxazoles useful in the treatment of inflammation
JP5420395B2 (ja) * 2006-04-07 2014-02-19 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｐ結合カセット輸送体の調節剤
JP2008006663A (ja) * 2006-06-28 2008-01-17 Pilot Ink Co Ltd 出没式筆記具
ITMI20061368A1 (it) * 2006-07-14 2008-01-15 Acraf Composto 2-arilindolico sostituito in posizione 5, composizione farmaceutica che lo comprende nonche' composti intermedi e procedimento per prepararlo

Also Published As

Publication number Publication date
US8399477B2 (en) 2013-03-19
US20130158269A1 (en) 2013-06-20
UA100867C2 (uk) 2013-02-11
BRPI0821450A2 (pt) 2015-06-16
IL206062A0 (en) 2010-11-30
PL2444392T3 (pl) 2015-03-31
ES2408955T3 (es) 2013-06-24
AU2008342705B2 (en) 2013-11-14
US8871948B2 (en) 2014-10-28
JP2011507929A (ja) 2011-03-10
IL206062A (en) 2015-08-31
DK2444392T3 (en) 2014-12-08
SI2234968T1 (sl) 2013-06-28
PT2234968E (pt) 2013-06-03
PT2444392E (pt) 2014-11-19
EP2444392B1 (en) 2014-09-24
HK1165410A1 (en) 2012-10-05
US20100286189A1 (en) 2010-11-11
SI2444392T1 (sl) 2014-12-31
EP2444392A1 (en) 2012-04-25
SG187400A1 (en) 2013-02-28
CN101910127A (zh) 2010-12-08
EP2234968B1 (en) 2013-03-27
EA020373B1 (ru) 2014-10-30
EP2234968A1 (en) 2010-10-06
CA2707339A1 (en) 2009-07-09
EA201070804A1 (ru) 2010-12-30
PL2234968T3 (pl) 2013-08-30
DK2234968T3 (da) 2013-06-17
KR20100103569A (ko) 2010-09-27
WO2009083436A1 (en) 2009-07-09
AU2008342705A1 (en) 2009-07-09
AR069961A1 (es) 2010-03-03
KR20160029861A (ko) 2016-03-15
EP2078711A1 (en) 2009-07-15
CA2707339C (en) 2018-05-01
GEP20125547B (en) 2012-05-25
HK1145172A1 (en) 2011-04-08
JP5698985B2 (ja) 2015-04-08
KR101671874B1 (ko) 2016-11-03
ES2523167T3 (es) 2014-11-21

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