CN105102456B - 非典型蛋白激酶c的氮杂喹唑啉抑制剂 - Google Patents

非典型蛋白激酶c的氮杂喹唑啉抑制剂 Download PDF

Info

Publication number
CN105102456B
CN105102456B CN201380062263.9A CN201380062263A CN105102456B CN 105102456 B CN105102456 B CN 105102456B CN 201380062263 A CN201380062263 A CN 201380062263A CN 105102456 B CN105102456 B CN 105102456B
Authority
CN
China
Prior art keywords
bases
pyrimidine
pyrido
base
pyridine
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201380062263.9A
Other languages
English (en)
Chinese (zh)
Other versions
CN105102456A (zh
Inventor
亨利·J·布雷斯林
布鲁斯·D·多赛
本杰明·J·杜甘
凯瑟琳·M·福勒
罗伯特·L·赫德金斯
尤根·F·米萨罗斯
纳撒尼尔·Jt·蒙克
艾玛·L·莫里斯
艾科奥卢瓦·奥洛沃耶
格雷戈里·R·奥特
格雷瓜尔·A·帕韦
乔纳森·R·A·罗菲
克里斯泰勒·N·苏迪
陶明
克雷格·A·齐费可萨克
阿莉森·L·祖利
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cancer Research Technology Ltd
Original Assignee
Cancer Research Technology Ltd
Cephalon LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Cancer Research Technology Ltd, Cephalon LLC filed Critical Cancer Research Technology Ltd
Publication of CN105102456A publication Critical patent/CN105102456A/zh
Application granted granted Critical
Publication of CN105102456B publication Critical patent/CN105102456B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-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
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic 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
    • C07F9/6581Heterocyclic 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
    • C07F9/6584Heterocyclic 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

Landscapes

  • 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)
CN201380062263.9A 2012-09-28 2013-09-27 非典型蛋白激酶c的氮杂喹唑啉抑制剂 Active CN105102456B (zh)

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 (2)

Publication Number Publication Date
CN105102456A CN105102456A (zh) 2015-11-25
CN105102456B true CN105102456B (zh) 2017-11-14

Family

ID=49326872

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380062263.9A Active CN105102456B (zh) 2012-09-28 2013-09-27 非典型蛋白激酶c的氮杂喹唑啉抑制剂

Country Status (18)

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

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102215272B1 (ko) * 2012-09-28 2021-02-15 이그니타, 인코포레이티드 비정형 단백질 키나제 c의 아자퀴나졸린 억제제
CA2895129C (en) 2012-12-20 2022-07-05 Sanford-Burnham Medical Research Institute Quinazoline neurotensin receptor 1 agonists and uses thereof
ES2845473T3 (es) 2013-03-14 2021-07-26 Boehringer Ingelheim Int (Bencil-ciano-metil)-amidas sustituidas de ácido 2-aza-biciclo[2.2.1]heptano-3-carboxílico inhibidores de la catepsina- C
BR112016005199B1 (pt) 2013-08-23 2022-02-22 Neupharma, Inc Certos compostos químicos, composições, e métodos
WO2015143376A1 (en) * 2014-03-21 2015-09-24 Nivalis Therapeutics, Inc. Novel compounds for the treatment of cystic fibrosis
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
JP6599908B2 (ja) 2014-06-25 2019-10-30 サンフォード−バーンハム メディカル リサーチ インスティテュート ニューロテンシン受容体1の小分子アゴニスト
TW201613919A (en) 2014-07-02 2016-04-16 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
CN107074856A (zh) * 2014-09-05 2017-08-18 阿略斯泰罗斯医疗公司 CaMKII抑制剂及其用途
EP3511331A1 (en) 2014-09-12 2019-07-17 Boehringer Ingelheim International GmbH Spirocyclic inhibitors of cathepsin c
RU2684396C2 (ru) * 2014-10-29 2019-04-09 Донг-А Ст Ко., Лтд. Новые соединения пиридопиримидинона для модулирования каталитической активности гистонлизиндеметилаз (KDMS)
CN105288512A (zh) * 2015-12-08 2016-02-03 李野林 一种治疗肥胖症的中药组合物
WO2017216726A1 (en) 2016-06-13 2017-12-21 Glaxosmithkline Intellectual Property Development Limited Substituted pyridines as inhibitors of dnmt1
WO2018035061A1 (en) 2016-08-15 2018-02-22 Neupharma, Inc. Certain chemical entities, compositions, and methods
CN109641892B (zh) * 2016-08-16 2021-07-02 默克专利有限公司 用作可逆btk抑制剂的2-氧代-咪唑并吡啶及其用途
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
JOP20190257A1 (ar) 2017-04-28 2019-10-28 Novartis Ag مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats
CA3057969A1 (en) 2017-05-02 2018-11-08 Novartis Ag Combination therapy
JP7311228B2 (ja) 2017-06-30 2023-07-19 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 Rho-関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用
KR102563325B1 (ko) 2017-06-30 2023-08-03 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 Rho-관련 단백질 키나아제 억제제, Rho-관련 단백질 키나아제 억제제를 함유하는 약학 조성물, 제조 방법 및 약학 조성물의 용도
CN110582491B (zh) 2017-06-30 2023-09-29 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
RS63661B1 (sr) * 2018-07-25 2022-11-30 Faes Farma Sa Piridopirimidini kao inhibitori histaminskog h4-receptora
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
CA3135196A1 (en) * 2019-03-28 2020-10-01 Cancer Research Technology Ltd Inhibitors of atypical protein kinase c and their use in treating hedgehog pathway-dependent cancers
EP3969449B1 (en) 2019-05-13 2025-02-12 Novartis AG New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
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
CN117088898B (zh) * 2022-05-13 2026-02-06 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
CN120882714A (zh) * 2022-12-13 2025-10-31 风树疗法公司 {5-环丙基-2-[2-(3,6-二氟-吡啶-2-基氨基)-吡啶-4-基]-吡啶并[3,4-d]嘧啶-4-基}-((s)-3,3-二甲基-哌啶-4-基)-胺的固体形式
CN117343005A (zh) * 2023-10-08 2024-01-05 上海泰坦科技股份有限公司 一种异烟酸衍生物的制备方法

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS4936700A (enExample) 1972-08-16 1974-04-05
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
JP2002080423A (ja) * 2000-09-06 2002-03-19 Daikin Ind Ltd トリフルオロ酢酸エチルの合成方法
WO2002022605A1 (en) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
FR2846657B1 (fr) 2002-11-05 2004-12-24 Servier Lab Nouveaux composes pyridopyrimidinone, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JP4895806B2 (ja) * 2003-04-09 2012-03-14 エクセリクシス, インク. Tie−2モジュレータと使用方法
US20050038047A1 (en) * 2003-08-14 2005-02-17 Edwards Paul John Azaquinazoline derivatives
US7582631B2 (en) * 2004-01-14 2009-09-01 Amgen Inc. Substituted heterocyclic compounds and methods of use
JP2008531538A (ja) * 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド 2,4−ジアミノ−ピリドピリミジン誘導体とmTOR阻害剤としてのその使用
CA2659851C (en) * 2006-08-23 2014-02-25 Kudos Pharmaceuticals Limited 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors
BRPI0716880A2 (pt) * 2006-09-08 2013-10-15 Pfizer Prod Inc Síntese de 2-(piridin-2-ilamino)-pirido[2,3-d]pirimidin-7-onas
CN102984941B (zh) * 2009-09-04 2016-08-17 密执安大学评议会 用于治疗白血病的组合物和方法
KR102215272B1 (ko) * 2012-09-28 2021-02-15 이그니타, 인코포레이티드 비정형 단백질 키나제 c의 아자퀴나졸린 억제제
WO2014164543A1 (en) * 2013-03-13 2014-10-09 The Regents Of The University Of Michigan Compositions comprising thienopyrimidine and thienopyridine compounds and methods of use thereof
USRE49687E1 (en) * 2014-09-09 2023-10-10 The Regents Of The University Of Michigan Thienopyrimidine and thienopyridine compounds and methods of use thereof
AU2016378579A1 (en) * 2015-12-22 2018-06-14 Vitae Pharmaceuticals, Inc. Inhibitors of the menin-MLL interaction

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
《2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes》;Maurice J. van Eis et al.;《Bioorganic & Medicinal Chemistry Letters》;20111021;第21卷(第24期);第7367–7372页 *
《Structure-Activity Relationships of the Diuretic Activity if Triaza- and Tetraaza-naphthalene compounds》;Kohei nishikawa et al.;《CHEMICAL AND PHARMACEUTICAL BULLETIN 》;19760101;第24卷(第9期);第2057-2077页 *

Also Published As

Publication number Publication date
KR20150086248A (ko) 2015-07-27
PH12015500689A1 (en) 2015-05-25
US20160102094A1 (en) 2016-04-14
EA201590661A1 (ru) 2015-09-30
IL237918A0 (en) 2015-05-31
EP2900666B1 (en) 2020-11-04
BR112015007061B1 (pt) 2022-10-04
HK1211928A1 (en) 2016-06-03
MX2015004016A (es) 2016-02-18
EP2900666A1 (en) 2015-08-05
US9914730B2 (en) 2018-03-13
US9896446B2 (en) 2018-02-20
CN105102456A (zh) 2015-11-25
NZ706857A (en) 2018-05-25
AU2013323360A1 (en) 2015-04-30
JP6535430B2 (ja) 2019-06-26
WO2014052699A1 (en) 2014-04-03
BR112015007061A8 (pt) 2019-08-20
AU2013323360B2 (en) 2017-09-07
IL237918B (en) 2021-05-31
WO2014052699A9 (en) 2015-07-16
US20140113882A1 (en) 2014-04-24
HK1212336A1 (en) 2016-06-10
BR112015007061A2 (pt) 2017-07-04
PH12015500689B1 (en) 2015-05-25
CA2886495C (en) 2023-09-19
KR102215272B1 (ko) 2021-02-15
SG11201502301YA (en) 2015-04-29
EA030253B1 (ru) 2018-07-31
TW201427978A (zh) 2014-07-16
CL2015000781A1 (es) 2016-04-01
JP2015533822A (ja) 2015-11-26
TWI663165B (zh) 2019-06-21
MX372736B (es) 2020-06-19
CA2886495A1 (en) 2014-04-03
ZA201502783B (en) 2016-01-27

Similar Documents

Publication Publication Date Title
CN105102456B (zh) 非典型蛋白激酶c的氮杂喹唑啉抑制剂
CN114585628B (zh) 囊性纤维化跨膜传导调节因子的调节剂
EP3152210B1 (en) Tank-binding kinase inhibitor compounds
CN115996929B (zh) 腺苷A2a受体的拮抗剂
RS65419B1 (sr) Derivati pirazolila korisni kao sredstva protiv kancera
JP2022552324A (ja) Fgfr阻害剤としての二環式複素環
US10414763B2 (en) Azaquinazoline inhibitors of atypical protein kinase C
CN119546604A (zh) 作为hpk1抑制剂的吡啶并[3,2-d]嘧啶
HK1212336B (en) Azaquinazoline inhibitors of atypical protein kinase c
HK1211928B (en) Azaquinazoline inhibitors of atypical protein kinase c
HK1236197A1 (en) Tank-binding kinase inhibitor compounds
HK1236197B (en) Tank-binding kinase inhibitor compounds

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1212336

Country of ref document: HK

C41 Transfer of patent application or patent right or utility model
TA01 Transfer of patent application right

Effective date of registration: 20170124

Address after: London, England

Applicant after: Cancer Rec Tech Ltd.

Address before: American California

Applicant before: CEPHALON INC.

Applicant before: Cancer Rec Tech Ltd.

GR01 Patent grant
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1212336

Country of ref document: HK