CN106488919B - 3-取代的2-氨基吲哚衍生物 - Google Patents

3-取代的2-氨基吲哚衍生物 Download PDF

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Publication number
CN106488919B
CN106488919B CN201580034535.3A CN201580034535A CN106488919B CN 106488919 B CN106488919 B CN 106488919B CN 201580034535 A CN201580034535 A CN 201580034535A CN 106488919 B CN106488919 B CN 106488919B
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pyrrolo
amine
pyrimidin
benzenesulfonyl
methyl
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Expired - Fee Related
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CN201580034535.3A
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Chinese (zh)
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CN106488919A (zh
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格雷戈里·巴克
理查德·达文波特
罗伯特·唐纳姆
威廉·法纳比
安妮·戈德比
邓肯·汉娜
大卫·哈里森
亨瑞特·威廉斯
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Takeda Pharmaceutical Co Ltd
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Takeda Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201580034535.3A 2014-06-25 2015-06-24 3-取代的2-氨基吲哚衍生物 Expired - Fee Related CN106488919B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1411236.1A GB201411236D0 (en) 2014-06-25 2014-06-25 Novel compounds
GB1411236.1 2014-06-25
PCT/GB2015/051840 WO2015198045A1 (en) 2014-06-25 2015-06-24 3-substituted 2-amino-indole derivatives

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CN106488919A CN106488919A (zh) 2017-03-08
CN106488919B true CN106488919B (zh) 2018-10-23

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US (1) US10059713B2 (https=)
EP (1) EP3160965A1 (https=)
JP (1) JP6574450B2 (https=)
CN (1) CN106488919B (https=)
CA (1) CA2952339A1 (https=)
GB (1) GB201411236D0 (https=)
WO (1) WO2015198045A1 (https=)

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CA3005766A1 (en) 2015-12-17 2017-06-22 Merck Patent Gmbh Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders
JP7125385B2 (ja) 2016-08-08 2022-08-24 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｔｌｒ７／８アンタゴニストおよびそれらの使用
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
TWI707849B (zh) 2018-02-13 2020-10-21 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
CN108440496B (zh) * 2018-03-01 2019-09-10 苏州大学 一种制备2-氨基吲哚衍生物的方法
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
KR102591947B1 (ko) 2018-04-19 2023-10-25 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
EP3820572B1 (en) 2018-07-13 2023-08-16 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
US11236085B2 (en) 2018-10-24 2022-02-01 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
CN114829362A (zh) * 2019-12-10 2022-07-29 成都倍特药业股份有限公司 一种可用作shp2抑制剂的含氮杂原子的六元并五元芳环衍生物

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WO2004060893A1 (en) * 2002-12-20 2004-07-22 Abbott Laboratories Pyrrolopyridine potassium channel openers
WO2005023818A2 (en) * 2003-09-10 2005-03-17 Gpc Biotech Ag Heterobicyclic compounds as pharmaceutically active agents
CN102917707A (zh) * 2010-05-06 2013-02-06 默沙东公司 可用作faah调节剂的氮杂吲哚衍生物
US20130137708A1 (en) * 2010-06-04 2013-05-30 The Regents Of The University Of California Methods and compositions for kinase inhibition
US20130245032A1 (en) * 2010-11-09 2013-09-19 Sanford-Burnham Medical Research Institute at Lake Nona Bicyclic and tricyclic inhibitors of sumoylation enzymes and methods of their use
US20140018361A1 (en) * 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof

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US6187777B1 (en) * 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
TW200306191A (en) * 2002-02-22 2003-11-16 Teijin Ltd Pyrrolopyrimidine derivatives

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Publication number Priority date Publication date Assignee Title
WO2004060893A1 (en) * 2002-12-20 2004-07-22 Abbott Laboratories Pyrrolopyridine potassium channel openers
WO2005023818A2 (en) * 2003-09-10 2005-03-17 Gpc Biotech Ag Heterobicyclic compounds as pharmaceutically active agents
CN102917707A (zh) * 2010-05-06 2013-02-06 默沙东公司 可用作faah调节剂的氮杂吲哚衍生物
US20130137708A1 (en) * 2010-06-04 2013-05-30 The Regents Of The University Of California Methods and compositions for kinase inhibition
US20130245032A1 (en) * 2010-11-09 2013-09-19 Sanford-Burnham Medical Research Institute at Lake Nona Bicyclic and tricyclic inhibitors of sumoylation enzymes and methods of their use
US20140018361A1 (en) * 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof

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CA2952339A1 (en) 2015-12-30
EP3160965A1 (en) 2017-05-03
US10059713B2 (en) 2018-08-28
JP6574450B2 (ja) 2019-09-11
CN106488919A (zh) 2017-03-08
US20170158700A1 (en) 2017-06-08
GB201411236D0 (en) 2014-08-06
JP2017519023A (ja) 2017-07-13
WO2015198045A1 (en) 2015-12-30

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