JP6535430B2 - 非定型プロテインキナーゼｃのアザキナゾリン阻害薬 - Google Patents

非定型プロテインキナーゼｃのアザキナゾリン阻害薬 Download PDF

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Publication number
JP6535430B2
JP6535430B2 JP2015534689A JP2015534689A JP6535430B2 JP 6535430 B2 JP6535430 B2 JP 6535430B2 JP 2015534689 A JP2015534689 A JP 2015534689A JP 2015534689 A JP2015534689 A JP 2015534689A JP 6535430 B2 JP6535430 B2 JP 6535430B2
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Japan
Prior art keywords
pyridin
pyrido
cyclopropyl
pyrimidin
piperazin
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JP2015534689A
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English (en)
Japanese (ja)
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JP2015533822A (ja
JP2015533822A5 (OSRAM
Inventor
ブレスリン、ヘンリー、ジェイ．
ドーシー、ブルース、ディー．
デュガン、ベンジャミン、ジェイ．
ファウラー、キャサリン、エム．
ハドキンズ、ロバート、エル．
メサロス、オイゲン、エフ．
モンク、ナサニエル、ジェイティー
モリス、エマ、エル．
オロウォーイ、イケオルワ
オット、グレゴリー、アール．
ペイヴ、グレゴアール、エー．
ルーフェイ、ジョナサン、アール．エー．
サウディ、クリステル、エヌ．
タオ、ミン
ズィフィクサック、クレイグ、エー．
ズッリ、アリソン、エル．
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Cancer Research Technology Ltd
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Cancer Research Technology Ltd
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Publication of JP2015533822A5 publication Critical patent/JP2015533822A5/ja
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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
    • A61K31/495—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (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)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015534689A 2012-09-28 2013-09-27 非定型プロテインキナーゼｃのアザキナゾリン阻害薬 Active JP6535430B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261707340P 2012-09-28 2012-09-28
US61/707,340 2012-09-28
US201361781364P 2013-03-14 2013-03-14
US61/781,364 2013-03-14
PCT/US2013/062085 WO2014052699A1 (en) 2012-09-28 2013-09-27 Azaquinazoline inhibitors of atypical protein kinase c

Publications (3)

Publication Number Publication Date
JP2015533822A JP2015533822A (ja) 2015-11-26
JP2015533822A5 JP2015533822A5 (OSRAM) 2017-06-22
JP6535430B2 true JP6535430B2 (ja) 2019-06-26

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JP2015534689A Active JP6535430B2 (ja) 2012-09-28 2013-09-27 非定型プロテインキナーゼｃのアザキナゾリン阻害薬

Country Status (18)

Country Link
US (2) US9914730B2 (OSRAM)
EP (1) EP2900666B1 (OSRAM)
JP (1) JP6535430B2 (OSRAM)
KR (1) KR102215272B1 (OSRAM)
CN (1) CN105102456B (OSRAM)
AU (1) AU2013323360B2 (OSRAM)
BR (1) BR112015007061B1 (OSRAM)
CA (1) CA2886495C (OSRAM)
CL (1) CL2015000781A1 (OSRAM)
EA (1) EA030253B1 (OSRAM)
IL (1) IL237918B (OSRAM)
MX (1) MX372736B (OSRAM)
NZ (1) NZ706857A (OSRAM)
PH (1) PH12015500689B1 (OSRAM)
SG (1) SG11201502301YA (OSRAM)
TW (1) TWI663165B (OSRAM)
WO (1) WO2014052699A1 (OSRAM)
ZA (1) ZA201502783B (OSRAM)

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US10118902B2 (en) 2014-06-25 2018-11-06 Sanford Burnham Prebys Medical Discovery Institute Small molecule agonists of neurotensin receptor 1
WO2016004305A2 (en) 2014-07-02 2016-01-07 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
WO2016037106A1 (en) * 2014-09-05 2016-03-10 Allosteros Therapeutics, Inc CaMKII INHIBITORS AND USES THEREOF
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JP2020525525A (ja) 2017-06-30 2020-08-27 ベイジン タイド ファーマシューティカル カンパニー リミテッドＢｅｉｊｉｎｇ Ｔｉｄｅ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｃｏ．， Ｌｔｄ． Ｒｈｏ−関連プロテインキナーゼ阻害剤、ｒｈｏ−関連プロテインキナーゼ阻害剤を含む医薬組成物、当該医薬組成物の調製方法及び使用
WO2019000683A1 (zh) 2017-06-30 2019-01-03 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
BR112021001270A2 (pt) * 2018-07-25 2021-04-20 Faes Farma, S.A. piridopirimidinas como inibidores do receptor h4 da histamina
US20210347785A1 (en) * 2018-08-01 2021-11-11 Shanghai Ennovabio Pharmaceuticals Co., Ltd. Preparation and application of aromatic compound having immunoregulatory function
CN111100063B (zh) * 2018-10-25 2022-05-17 南京药石科技股份有限公司 一种合成2-氟甲基取代的吡咯烷、哌啶以及哌嗪衍生物的制备方法
KR20220002930A (ko) * 2019-03-28 2022-01-07 캔써 리서치 테크놀로지 리미티드 비정형 단백질 키나제 c의 억제제 및 헷지호그 경로 의존성 암의 치료에서 이의 용도
BR112021022335A2 (pt) 2019-05-13 2021-12-28 Novartis Ag Formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinopiridin-4-il)-4-metilfenil)-2 (trifluorome-til)isonicotinamida como inibidores raf para o tratamento de câncer
CN116120243B (zh) * 2021-11-15 2025-07-29 都创(上海)医药科技股份有限公司 aPKC抑制剂化合物中间体片段及其制备方法和应用
CN114349711B (zh) * 2022-02-28 2023-08-15 四川依维欣医药科技有限公司 一种（R）-1-Boc-3-羟甲基哌嗪的合成方法
CN117088898A (zh) * 2022-05-13 2023-11-21 中国药科大学 稠环嘧啶类化合物及其制备方法、药物组合物和应用
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Also Published As

Publication number Publication date
EA201590661A1 (ru) 2015-09-30
PH12015500689A1 (en) 2015-05-25
AU2013323360B2 (en) 2017-09-07
US20140113882A1 (en) 2014-04-24
BR112015007061A8 (pt) 2019-08-20
JP2015533822A (ja) 2015-11-26
CA2886495C (en) 2023-09-19
SG11201502301YA (en) 2015-04-29
HK1211928A1 (en) 2016-06-03
CN105102456B (zh) 2017-11-14
HK1212336A1 (en) 2016-06-10
CL2015000781A1 (es) 2016-04-01
TWI663165B (zh) 2019-06-21
AU2013323360A1 (en) 2015-04-30
US9896446B2 (en) 2018-02-20
EP2900666B1 (en) 2020-11-04
IL237918B (en) 2021-05-31
MX2015004016A (es) 2016-02-18
IL237918A0 (en) 2015-05-31
KR102215272B1 (ko) 2021-02-15
WO2014052699A1 (en) 2014-04-03
NZ706857A (en) 2018-05-25
BR112015007061A2 (pt) 2017-07-04
PH12015500689B1 (en) 2015-05-25
ZA201502783B (en) 2016-01-27
MX372736B (es) 2020-06-19
TW201427978A (zh) 2014-07-16
BR112015007061B1 (pt) 2022-10-04
CA2886495A1 (en) 2014-04-03
EP2900666A1 (en) 2015-08-05
EA030253B1 (ru) 2018-07-31
KR20150086248A (ko) 2015-07-27
US9914730B2 (en) 2018-03-13
US20160102094A1 (en) 2016-04-14
WO2014052699A9 (en) 2015-07-16
CN105102456A (zh) 2015-11-25

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