CN104053661B - 非典型性蛋白激酶c的噻吩并嘧啶类抑制剂 - Google Patents

非典型性蛋白激酶c的噻吩并嘧啶类抑制剂 Download PDF

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CN104053661B
CN104053661B CN201280057805.9A CN201280057805A CN104053661B CN 104053661 B CN104053661 B CN 104053661B CN 201280057805 A CN201280057805 A CN 201280057805A CN 104053661 B CN104053661 B CN 104053661B
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CN104053661A (zh
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布鲁斯·D·多尔西
基思·S·勒恩
艾玛·L·莫里斯
格雷戈里·R·奥特
乔纳森·R·罗菲
克里斯泰勒·N·苏迪
贾森·C·瓦格纳
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Cancer Research Technology Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/081Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201280057805.9A 2011-11-23 2012-11-19 非典型性蛋白激酶c的噻吩并嘧啶类抑制剂 Active CN104053661B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161563310P 2011-11-23 2011-11-23
US61/563,310 2011-11-23
PCT/US2012/065831 WO2013078126A1 (en) 2011-11-23 2012-11-19 Thienopyrimidine inhibitors of atypical protein kinase c

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CN104053661A CN104053661A (zh) 2014-09-17
CN104053661B true CN104053661B (zh) 2018-06-19

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US (3) US9604994B2 (https=)
EP (2) EP2782917B1 (https=)
JP (1) JP6206926B2 (https=)
CN (1) CN104053661B (https=)
AU (2) AU2012340869B2 (https=)
CA (1) CA2855446C (https=)
ES (1) ES2575143T3 (https=)
IL (1) IL232559B (https=)
IN (1) IN2014CN04558A (https=)
MX (1) MX355088B (https=)
WO (1) WO2013078126A1 (https=)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8703941B2 (en) 2011-01-10 2014-04-22 Nimbus Iris, Inc. IRAK inhibitors and uses thereof
CN104582705A (zh) * 2012-01-10 2015-04-29 林伯士艾瑞斯公司 白介素-1受体相关激酶(irak)抑制剂和其用途
HK1210696A1 (en) 2012-07-11 2016-05-06 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2014011906A2 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
JP2016505012A (ja) 2013-01-10 2016-02-18 ニンバス アイリス, インコーポレイテッド Irak阻害剤およびその使用
BR112016006319A2 (pt) 2013-09-27 2017-08-01 Nimbus Iris Inc inibidores de irak e usos dos mesmos
TWI675836B (zh) * 2014-03-25 2019-11-01 美商伊格尼塔公司 非典型蛋白質激酶c之氮雜喹唑啉抑制劑
JP7114076B2 (ja) * 2015-12-22 2022-08-08 シャイ・セラピューティクス・エルエルシー がん及び炎症性疾患の処置のための化合物
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
KR20180075228A (ko) * 2016-12-26 2018-07-04 한미약품 주식회사 싸이에노피리미딘 화합물의 신규 제조방법 및 중간체
JP7514005B2 (ja) 2017-06-21 2024-07-10 シャイ・セラピューティクス・エルエルシー がん、炎症性疾患、ラソパシー、及び線維性疾患の治療のためのrasスーパーファミリーと相互作用する化合物
WO2019119206A1 (en) * 2017-12-18 2019-06-27 Merck Sharp & Dohme Corp. Purine inhibitors of human phosphatidylinositol 3-kinase delta
CN108658999B (zh) * 2018-04-24 2021-02-05 温州大学 2-苯基杂环并[2,3-d]嘧啶-4(3H)-酮类化合物的合成方法
EP3632908A1 (en) 2018-10-02 2020-04-08 Inventiva Inhibitors of the yap/taz-tead interaction and their use in the treatment of cancer
JP7629200B2 (ja) * 2018-11-20 2025-02-13 ジョージタウン ユニバーシティ 神経変性、筋変性及びリソソーム蓄積障害を治療するための組成物及び方法
JP7407461B2 (ja) 2018-12-19 2024-01-04 シャイ・セラピューティクス・エルエルシー がん、炎症性疾患、ras病、及び線維性疾患の処置のためのrasスーパーファミリーと相互作用する化合物
EP3725788A1 (en) 2019-04-15 2020-10-21 Bayer AG Novel heteroaryl-substituted aminoalkyl azole compounds as pesticides
CN116410205B (zh) * 2021-12-29 2024-07-05 上海皓元生物医药科技有限公司 一种3-取代-9-甲基-噻吩并三唑并噁嗪类化合物的制备方法
CN116925098B (zh) * 2022-04-09 2026-02-17 深圳湾实验室 靶向泛素特异性蛋白酶1(usp1)的小分子抑制剂及其应用
WO2025085725A1 (en) * 2023-10-20 2025-04-24 Scorpion Therapeutics, Inc. Methods for treating a p53-associated cancer

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008073785A2 (en) * 2006-12-07 2008-06-19 Genentech, Inc. Phosphoinositide 3-kinase inhibitor compounds and methods of use
WO2010080996A1 (en) * 2009-01-08 2010-07-15 Curis, Inc. Phosphoinositide 3-kinase inhibitors with a zinc binding moiety
WO2011130628A1 (en) * 2010-04-16 2011-10-20 Curis, Inc. Treatment of cancers having k-ras mutations

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA782648B (en) 1977-05-23 1979-06-27 Ici Australia Ltd The prevention,control or eradication of infestations of ixodid ticks
US6187777B1 (en) 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
JP2000038350A (ja) 1998-05-18 2000-02-08 Yoshitomi Pharmaceut Ind Ltd 糖尿病治療薬
TW564247B (en) 1999-04-08 2003-12-01 Akzo Nobel Nv Bicyclic heteraromatic compound
IL148903A0 (en) 1999-09-30 2002-09-12 Neurogen Corp Certain alkylene diamine-substituted heterocycles
CN1186324C (zh) 2000-04-27 2005-01-26 山之内制药株式会社 稠合杂芳基衍生物
US6608053B2 (en) 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
KR20030034232A (ko) 2000-09-29 2003-05-01 닛뽕소다 가부시키가이샤 티에노피리미딘 화합물 및 그 염 및 제조방법
AU2002336462A1 (en) 2001-09-06 2003-03-24 Millennium Pharmaceuticals, Inc. Piperazine and homopiperazine compounds
DE60236322D1 (de) 2001-12-07 2010-06-17 Vertex Pharma Verbindungen auf pyrimidin-basis als gsk-3-hemmer
WO2004017950A2 (en) 2002-08-22 2004-03-04 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
TW200410975A (en) 2002-09-26 2004-07-01 Nihon Nohyaku Co Ltd New pesticide and method for using it, new substituted thienopyrimidine derivative, its intermediate, and method for producing it
ES2217956B1 (es) 2003-01-23 2006-04-01 Almirall Prodesfarma, S.A. Nuevos derivados de 4-aminotieno(2,3-d)pirimidin-6-carbonitrilo.
PL1641803T6 (pl) 2003-06-11 2011-04-29 Xention Ltd Pochodne tienopirymidyny jako inhibitory kanału potasowego
WO2005067546A2 (en) 2004-01-13 2005-07-28 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
AU2005254057B2 (en) 2004-06-15 2011-02-17 Isis Pharmaceuticals, Inc. C-purine nucleoside analogs as inhibitors of RNA-dependent RNA viral polymerase
WO2006093518A2 (en) 2004-06-25 2006-09-08 Apath, Llc Thienyl compounds for treating virus-related conditions
WO2006010568A2 (de) 2004-07-23 2006-02-02 Curacyte Discovery Gmbh Substituierte pyrido [3',2':4,5]thieno[3,2-d]pyrimidin-2,4(1 h,3h)-diones und -4(3h)-one sowie pyrido [3',2' :4,5] furo[3,2-d]pyrimidin -2,4(1 h,3h)-dione und -4(3h)-one zur verwendung als inhibitoren der tnf-allpha freisetzung
DE102005013621A1 (de) 2005-03-24 2006-09-28 Curacyte Discovery Gmbh Substituierte 2-Aryl(Hetaryl)-5-aminothieno[2,3-d]pyrimidin-6-carbonsäureamide, Verfahren zu ihrer Herstellung und Verwendung als Pharmazeutika
TWI498332B (zh) 2006-04-26 2015-09-01 Hoffmann La Roche 作為pi3k抑制劑之嘧啶衍生物及相關製備方法、醫藥組合物、用途、套組及產物
WO2008037607A1 (de) 2006-09-25 2008-04-03 Basf Se Carbonylgruppen-enthaltende heterocyclische verbindungen und deren verwendung zur bekämpfung von phytopathogenen pilzen
EP2334380B1 (en) 2008-05-30 2021-09-01 Mitologics Ant-ligands molecules and biological applications
UA109775C2 (xx) 2009-10-29 2015-10-12 N-вмісні гетероарильні похідні як інгібітори jak3-кінази

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008073785A2 (en) * 2006-12-07 2008-06-19 Genentech, Inc. Phosphoinositide 3-kinase inhibitor compounds and methods of use
WO2010080996A1 (en) * 2009-01-08 2010-07-15 Curis, Inc. Phosphoinositide 3-kinase inhibitors with a zinc binding moiety
WO2011130628A1 (en) * 2010-04-16 2011-10-20 Curis, Inc. Treatment of cancers having k-ras mutations

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
A 3-Phosphoinositide-dependent Protein Kinase-1 (PDK1) Docking Site Is Required for the Phosphorylation of Protein Kinase Cz(PKC z) and PKC-related Kinase 2 by PDK1;Anudharan Balendran et al.;《THE JOURNAL OF BIOLOGICAL CHEMISTRY》;20000410;第275卷(第27期);第20806-20813页 *

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EP2782917B1 (en) 2016-03-02
IN2014CN04558A (https=) 2015-09-18
US20140323435A1 (en) 2014-10-30
EP2782917A1 (en) 2014-10-01
AU2017203725B2 (en) 2019-02-28
IL232559B (en) 2018-04-30
AU2017203725A1 (en) 2017-06-22
ES2575143T3 (es) 2016-06-24
NZ625447A (en) 2015-09-25
US9604994B2 (en) 2017-03-28
JP6206926B2 (ja) 2017-10-04
HK1202529A1 (zh) 2015-10-02
US10183950B2 (en) 2019-01-22
CA2855446A1 (en) 2013-05-30
US20170158706A1 (en) 2017-06-08
EP3048106A1 (en) 2016-07-27
JP2014533728A (ja) 2014-12-15
MX2014006233A (es) 2014-10-17
CA2855446C (en) 2021-04-20
WO2013078126A1 (en) 2013-05-30
US20190106433A1 (en) 2019-04-11
CN104053661A (zh) 2014-09-17
AU2012340869B2 (en) 2017-03-02
IL232559A0 (en) 2014-06-30
MX355088B (es) 2018-04-04
AU2012340869A1 (en) 2014-06-19
EP3048106B1 (en) 2019-11-06
US10954251B2 (en) 2021-03-23

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