CA2886495C - Azaquinazoline inhibitors of atypical protein kinase c - Google Patents

Azaquinazoline inhibitors of atypical protein kinase c Download PDF

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Publication number
CA2886495C
CA2886495C CA2886495A CA2886495A CA2886495C CA 2886495 C CA2886495 C CA 2886495C CA 2886495 A CA2886495 A CA 2886495A CA 2886495 A CA2886495 A CA 2886495A CA 2886495 C CA2886495 C CA 2886495C
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Prior art keywords
pyridin
pyrido
pyrimidin
optionally substituted
piperazin
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CA2886495A
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English (en)
French (fr)
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CA2886495A1 (en
Inventor
Henry J. Breslin
Bruce D. Dorsey
Benjamin J. Dugan
Katherine M. Fowler
Robert L. Hudkins
Eugen F. Mesaros
Nathaniel Jt Monck
Emma L. MORRIS
Ikeoluwa OLOWOYE
Gregory R. Ott
Gregoire A. Pave
Jonathan R. A. Roffey
Christelle N. SOUDY
Ming Tao
Craig A. Zificsak
Allison L. Zulli
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Cancer Research Technology Ltd
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Cancer Research Technology Ltd
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Publication of CA2886495A1 publication Critical patent/CA2886495A1/en
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
CA2886495A 2012-09-28 2013-09-27 Azaquinazoline inhibitors of atypical protein kinase c Active CA2886495C (en)

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
CA2886495A1 CA2886495A1 (en) 2014-04-03
CA2886495C true CA2886495C (en) 2023-09-19

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CA2886495A Active CA2886495C (en) 2012-09-28 2013-09-27 Azaquinazoline inhibitors of atypical protein kinase c

Country Status (18)

Country Link
US (2) US9914730B2 (https=)
EP (1) EP2900666B1 (https=)
JP (1) JP6535430B2 (https=)
KR (1) KR102215272B1 (https=)
CN (1) CN105102456B (https=)
AU (1) AU2013323360B2 (https=)
BR (1) BR112015007061B1 (https=)
CA (1) CA2886495C (https=)
CL (1) CL2015000781A1 (https=)
EA (1) EA030253B1 (https=)
IL (1) IL237918B (https=)
MX (1) MX372736B (https=)
NZ (1) NZ706857A (https=)
PH (1) PH12015500689A1 (https=)
SG (1) SG11201502301YA (https=)
TW (1) TWI663165B (https=)
WO (1) WO2014052699A1 (https=)
ZA (1) ZA201502783B (https=)

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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
WO2016037106A1 (en) * 2014-09-05 2016-03-10 Allosteros Therapeutics, Inc CaMKII INHIBITORS AND USES THEREOF
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CN109843858B (zh) * 2016-08-15 2023-05-05 润新生物公司 某些化学实体、组合物及方法
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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
ES2952265T3 (es) 2017-05-02 2023-10-30 Novartis Ag Terapia combinada que comprende un inhibidor de Raf y trametinib
WO2019000682A1 (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
CN110582489B (zh) 2017-06-30 2023-10-27 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
US10323023B2 (en) 2017-06-30 2019-06-18 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
MX2021000966A (es) * 2018-07-25 2021-07-06 Faes Farma Sa Piridopirimidinas como inhibidores del receptor de histamina h4.
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
US20220143028A1 (en) * 2019-03-28 2022-05-12 Cancer Research Technology Ltd Inhibitors of atypical protein kinase c and their use in treating hedgehog pathway-dependent cancers
ES3025633T3 (en) 2019-05-13 2025-06-09 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

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Also Published As

Publication number Publication date
JP6535430B2 (ja) 2019-06-26
IL237918B (en) 2021-05-31
PH12015500689B1 (en) 2015-05-25
EP2900666B1 (en) 2020-11-04
KR20150086248A (ko) 2015-07-27
TW201427978A (zh) 2014-07-16
US20140113882A1 (en) 2014-04-24
BR112015007061B1 (pt) 2022-10-04
SG11201502301YA (en) 2015-04-29
TWI663165B (zh) 2019-06-21
KR102215272B1 (ko) 2021-02-15
BR112015007061A2 (pt) 2017-07-04
US9896446B2 (en) 2018-02-20
MX372736B (es) 2020-06-19
CL2015000781A1 (es) 2016-04-01
AU2013323360B2 (en) 2017-09-07
US9914730B2 (en) 2018-03-13
IL237918A0 (en) 2015-05-31
US20160102094A1 (en) 2016-04-14
JP2015533822A (ja) 2015-11-26
CN105102456B (zh) 2017-11-14
ZA201502783B (en) 2016-01-27
NZ706857A (en) 2018-05-25
BR112015007061A8 (pt) 2019-08-20
AU2013323360A1 (en) 2015-04-30
EA030253B1 (ru) 2018-07-31
WO2014052699A9 (en) 2015-07-16
CN105102456A (zh) 2015-11-25
HK1212336A1 (en) 2016-06-10
EP2900666A1 (en) 2015-08-05
WO2014052699A1 (en) 2014-04-03
MX2015004016A (es) 2016-02-18
HK1211928A1 (en) 2016-06-03
PH12015500689A1 (en) 2015-05-25
CA2886495A1 (en) 2014-04-03
EA201590661A1 (ru) 2015-09-30

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