CN105924437B - 作为iii型受体酪氨酸激酶抑制剂的化合物 - Google Patents

作为iii型受体酪氨酸激酶抑制剂的化合物 Download PDF

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Publication number
CN105924437B
CN105924437B CN201610248287.9A CN201610248287A CN105924437B CN 105924437 B CN105924437 B CN 105924437B CN 201610248287 A CN201610248287 A CN 201610248287A CN 105924437 B CN105924437 B CN 105924437B
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methyl
base
pyridine
indazole
alkyl
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Expired - Fee Related
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Chinese (zh)
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CN105924437A (zh
Inventor
M.L.博伊斯
R.K.德莱尔
E.J.希肯
A.L.肯尼迪
D.A.马里斯卡
F.P.玛姆萨特
M.C.芒森
B.纽豪斯
B.拉斯特
J.P.里齐
M.E.罗德里格兹
G.T.托帕洛夫
赵千
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Array Biopharma Inc
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Array Biopharma Inc
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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
    • 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201610248287.9A 2010-12-13 2011-12-13 作为iii型受体酪氨酸激酶抑制剂的化合物 Expired - Fee Related CN105924437B (zh)

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US42254710P 2010-12-13 2010-12-13
US61/422,547 2010-12-13
CN201180067342.XA CN103347882B (zh) 2010-12-13 2011-12-13 作为III型受体酪氨酸激酶抑制剂的取代的N-(1H-吲唑-4-基)咪唑并[1,2-a]吡啶-3-甲酰胺化合物

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CN105924437A CN105924437A (zh) 2016-09-07
CN105924437B true CN105924437B (zh) 2018-11-30

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CN201610248287.9A Expired - Fee Related CN105924437B (zh) 2010-12-13 2011-12-13 作为iii型受体酪氨酸激酶抑制剂的化合物
CN201180067342.XA Expired - Fee Related CN103347882B (zh) 2010-12-13 2011-12-13 作为III型受体酪氨酸激酶抑制剂的取代的N-(1H-吲唑-4-基)咪唑并[1,2-a]吡啶-3-甲酰胺化合物
CN201811311712.XA Pending CN109608449A (zh) 2010-12-13 2011-12-13 作为iii型受体酪氨酸激酶抑制剂的化合物

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CN201180067342.XA Expired - Fee Related CN103347882B (zh) 2010-12-13 2011-12-13 作为III型受体酪氨酸激酶抑制剂的取代的N-(1H-吲唑-4-基)咪唑并[1,2-a]吡啶-3-甲酰胺化合物
CN201811311712.XA Pending CN109608449A (zh) 2010-12-13 2011-12-13 作为iii型受体酪氨酸激酶抑制剂的化合物

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EP (1) EP2651939B1 (enExample)
JP (3) JP5868996B2 (enExample)
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CN104496891A (zh) * 2014-12-06 2015-04-08 哈尔滨工业大学 吡啶衍生物2-叔丁氧基-6-亚甲基氯吡啶的合成方法
CN104974078A (zh) * 2015-06-25 2015-10-14 黄荣辉 一种2-甲基-6-氯甲基吡啶盐酸盐的制备方法
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CN114605387A (zh) 2015-08-12 2022-06-10 埃皮吉纳提克斯股份有限公司 取代的苯并咪唑、它们的制备和它们作为药物的用途
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CN109790079B (zh) * 2016-07-29 2022-06-03 香港科技大学 有机锌试剂与杂环(拟)卤化物的C(sp3)-C(sp2)交叉偶联反应
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CN109790141B (zh) * 2016-11-28 2021-06-11 卫材 R&D 管理有限公司 吲唑衍生物的盐及其晶体
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CN112135825A (zh) 2018-03-13 2020-12-25 夏尔人类遗传性治疗公司 血浆激肽释放酶抑制剂及其用途
CN111410654B (zh) * 2019-01-19 2022-05-17 江苏新元素医药科技有限公司 3-溴-5-(2-乙基咪唑并[1,2-a]吡啶-3-羰基)-2-羟基苯甲腈的合成
TWI841671B (zh) 2019-01-24 2024-05-11 日商第一三共股份有限公司 具有取代基之脲化合物
TWI759829B (zh) 2019-08-23 2022-04-01 財團法人生物技術開發中心 作為第iii型受體酪胺酸激酶抑制劑之雜環吡唑衍生物
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JP2013545808A (ja) 2013-12-26
RU2013132758A (ru) 2015-01-20
WO2012082689A1 (en) 2012-06-21
CN103347882B (zh) 2016-05-11
SG191129A1 (en) 2013-07-31
SMT201500165B (it) 2015-09-07
CA2821712C (en) 2019-02-12
US9174981B2 (en) 2015-11-03
MX2013006763A (es) 2014-01-08
RU2591195C2 (ru) 2016-07-10
NZ613235A (en) 2015-04-24
BR112013014854B1 (pt) 2020-12-08
US20180086758A1 (en) 2018-03-29
TW201305156A (zh) 2013-02-01
JP2016040303A (ja) 2016-03-24
US20130274244A1 (en) 2013-10-17
HK1190709A1 (en) 2014-07-11
JP2018065835A (ja) 2018-04-26
MY172110A (en) 2019-11-14
HRP20150571T1 (xx) 2015-07-03
EP2651939A1 (en) 2013-10-23
CA3027814A1 (en) 2012-06-21
CA2821712A1 (en) 2012-06-21
KR101974665B1 (ko) 2019-05-02
CL2013001712A1 (es) 2013-12-06
ME02172B (me) 2015-10-20
JP5868996B2 (ja) 2016-02-24
KR20140014109A (ko) 2014-02-05
US20160002232A1 (en) 2016-01-07
PH12013501221A1 (en) 2022-03-30
EP2651939B1 (en) 2015-04-08
AU2016222468B2 (en) 2017-12-21
TWI527813B (zh) 2016-04-01
CN105924437A (zh) 2016-09-07
CO6751248A2 (es) 2013-09-16
AU2011344001B2 (en) 2016-06-30
SI2651939T1 (sl) 2015-07-31
BR112013014854A2 (pt) 2016-10-18
AU2018201903A1 (en) 2018-04-12
HUE025416T2 (en) 2016-02-29
IL226911A (en) 2016-09-29
DK2651939T3 (en) 2015-06-01
AU2016222468A1 (en) 2016-09-22
US10669269B2 (en) 2020-06-02
CR20130349A (es) 2013-08-09
PL2651939T3 (pl) 2015-10-30
PT2651939E (pt) 2015-08-04
RS54070B1 (sr) 2015-10-30
CN103347882A (zh) 2013-10-09
UY33801A (es) 2013-06-28
AU2018201903B2 (en) 2019-09-19
UA112425C2 (uk) 2016-09-12
US9809590B2 (en) 2017-11-07
ES2540996T3 (es) 2015-07-15
CN109608449A (zh) 2019-04-12
BR112013014854A8 (pt) 2018-03-27

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