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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (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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US (3) US9174981B2 (OSRAM)
EP (1) EP2651939B1 (OSRAM)
JP (3) JP5868996B2 (OSRAM)
KR (1) KR101974665B1 (OSRAM)
CN (3) CN105924437B (OSRAM)
AU (3) AU2011344001B2 (OSRAM)
BR (1) BR112013014854B1 (OSRAM)
CA (2) CA3027814A1 (OSRAM)
CL (1) CL2013001712A1 (OSRAM)
CO (1) CO6751248A2 (OSRAM)
CR (1) CR20130349A (OSRAM)
DK (1) DK2651939T3 (OSRAM)
ES (1) ES2540996T3 (OSRAM)
HR (1) HRP20150571T1 (OSRAM)
HU (1) HUE025416T2 (OSRAM)
IL (1) IL226911A (OSRAM)
ME (1) ME02172B (OSRAM)
MX (1) MX2013006763A (OSRAM)
MY (1) MY172110A (OSRAM)
NZ (1) NZ613235A (OSRAM)
PH (1) PH12013501221A1 (OSRAM)
PL (1) PL2651939T3 (OSRAM)
PT (1) PT2651939E (OSRAM)
RS (1) RS54070B1 (OSRAM)
RU (1) RU2591195C2 (OSRAM)
SG (1) SG191129A1 (OSRAM)
SI (1) SI2651939T1 (OSRAM)
SM (1) SMT201500165B (OSRAM)
TW (1) TWI527813B (OSRAM)
UA (1) UA112425C2 (OSRAM)
UY (1) UY33801A (OSRAM)
WO (1) WO2012082689A1 (OSRAM)

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UA108222C2 (xx) * 2009-12-21 2015-04-10 СПОЛУКИ ЗАМІЩЕНОГО N-(1H-ІНДАЗОЛ-4-ІЛ)ІМІДАЗОЛ$1,2-а]ПІРИДИН-3-КАРБОКСАМІДУ ЯК ІНГІБІТОРИ cFMS
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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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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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MD3658552T2 (ro) 2017-07-28 2024-02-29 Yuhan Corp Procedeu de obținere a N-(5-((4-(4-((dimetilamino)metil)-3-fenil-1H-pirazol-1-il)pirimidin-2-il)amino)-4-metoxi-2-morfolinofenil)acrilamidei prin prin reacţia aminei corespunzătoare cu clorură de 3-halo-propionil
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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US9174981B2 (en) 2015-11-03
CA2821712A1 (en) 2012-06-21
IL226911A (en) 2016-09-29
TW201305156A (zh) 2013-02-01
US20180086758A1 (en) 2018-03-29
CN109608449A (zh) 2019-04-12
AU2018201903A1 (en) 2018-04-12
BR112013014854B1 (pt) 2020-12-08
JP2016040303A (ja) 2016-03-24
AU2016222468B2 (en) 2017-12-21
CA3027814A1 (en) 2012-06-21
US10669269B2 (en) 2020-06-02
CN103347882B (zh) 2016-05-11
TWI527813B (zh) 2016-04-01
CA2821712C (en) 2019-02-12
AU2016222468A1 (en) 2016-09-22
NZ613235A (en) 2015-04-24
RU2013132758A (ru) 2015-01-20
UA112425C2 (uk) 2016-09-12
JP5868996B2 (ja) 2016-02-24
EP2651939B1 (en) 2015-04-08
CO6751248A2 (es) 2013-09-16
ME02172B (me) 2015-10-20
KR101974665B1 (ko) 2019-05-02
WO2012082689A1 (en) 2012-06-21
PL2651939T3 (pl) 2015-10-30
CL2013001712A1 (es) 2013-12-06
JP2013545808A (ja) 2013-12-26
SI2651939T1 (sl) 2015-07-31
JP2018065835A (ja) 2018-04-26
HUE025416T2 (en) 2016-02-29
SG191129A1 (en) 2013-07-31
HK1190709A1 (en) 2014-07-11
DK2651939T3 (en) 2015-06-01
BR112013014854A2 (pt) 2016-10-18
CN103347882A (zh) 2013-10-09
SMT201500165B (it) 2015-09-07
BR112013014854A8 (pt) 2018-03-27
RU2591195C2 (ru) 2016-07-10
PT2651939E (pt) 2015-08-04
RS54070B1 (sr) 2015-10-30
KR20140014109A (ko) 2014-02-05
MY172110A (en) 2019-11-14
ES2540996T3 (es) 2015-07-15
AU2011344001B2 (en) 2016-06-30
UY33801A (es) 2013-06-28
EP2651939A1 (en) 2013-10-23
CR20130349A (es) 2013-08-09
PH12013501221A1 (en) 2022-03-30
US20130274244A1 (en) 2013-10-17
CN105924437A (zh) 2016-09-07
US9809590B2 (en) 2017-11-07
AU2018201903B2 (en) 2019-09-19
HRP20150571T1 (xx) 2015-07-03
US20160002232A1 (en) 2016-01-07
MX2013006763A (es) 2014-01-08

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