CA2844830C - Novel imidazole amines as modulators of kinase activity - Google Patents

Novel imidazole amines as modulators of kinase activity Download PDF

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Publication number
CA2844830C
CA2844830C CA2844830A CA2844830A CA2844830C CA 2844830 C CA2844830 C CA 2844830C CA 2844830 A CA2844830 A CA 2844830A CA 2844830 A CA2844830 A CA 2844830A CA 2844830 C CA2844830 C CA 2844830C
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CA
Canada
Prior art keywords
imidazol
fluoro
piperidin
trifluoromethyl
ethyl
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.)
Expired - Fee Related
Application number
CA2844830A
Other languages
English (en)
French (fr)
Other versions
CA2844830A1 (en
Inventor
Bayard R. Huck
Xiaoling Chen
Yufang Xiao
Ruoxi Lan
Lizbeth Celeste DESELM
Hui QIU
Constantin Neagu
Donald Bankston
Christopher Charles Victor Jones
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.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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
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Publication of CA2844830A1 publication Critical patent/CA2844830A1/en
Application granted granted Critical
Publication of CA2844830C publication Critical patent/CA2844830C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Peptides Or Proteins (AREA)
CA2844830A 2011-09-12 2012-09-12 Novel imidazole amines as modulators of kinase activity Expired - Fee Related CA2844830C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161533601P 2011-09-12 2011-09-12
US61/533,601 2011-09-12
PCT/US2012/054900 WO2013040059A1 (en) 2011-09-12 2012-09-12 Novel imidazole amines as modulators of kinase activity

Publications (2)

Publication Number Publication Date
CA2844830A1 CA2844830A1 (en) 2013-03-21
CA2844830C true CA2844830C (en) 2019-09-10

Family

ID=46881179

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2844830A Expired - Fee Related CA2844830C (en) 2011-09-12 2012-09-12 Novel imidazole amines as modulators of kinase activity

Country Status (24)

Country Link
US (2) US9145392B2 (cg-RX-API-DMAC7.html)
EP (1) EP2755965B1 (cg-RX-API-DMAC7.html)
JP (1) JP5964974B2 (cg-RX-API-DMAC7.html)
KR (1) KR101995605B1 (cg-RX-API-DMAC7.html)
CN (1) CN104080782B (cg-RX-API-DMAC7.html)
AU (1) AU2012308696B2 (cg-RX-API-DMAC7.html)
BR (1) BR112014005554A2 (cg-RX-API-DMAC7.html)
CA (1) CA2844830C (cg-RX-API-DMAC7.html)
DK (1) DK2755965T3 (cg-RX-API-DMAC7.html)
EA (1) EA025098B1 (cg-RX-API-DMAC7.html)
ES (1) ES2644536T3 (cg-RX-API-DMAC7.html)
HR (1) HRP20171554T1 (cg-RX-API-DMAC7.html)
HU (1) HUE035019T2 (cg-RX-API-DMAC7.html)
IL (1) IL231383A (cg-RX-API-DMAC7.html)
LT (1) LT2755965T (cg-RX-API-DMAC7.html)
MX (1) MX346095B (cg-RX-API-DMAC7.html)
NO (1) NO2791461T3 (cg-RX-API-DMAC7.html)
PL (1) PL2755965T3 (cg-RX-API-DMAC7.html)
PT (1) PT2755965T (cg-RX-API-DMAC7.html)
RS (1) RS56534B1 (cg-RX-API-DMAC7.html)
SG (2) SG2014009278A (cg-RX-API-DMAC7.html)
SI (1) SI2755965T1 (cg-RX-API-DMAC7.html)
WO (1) WO2013040059A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201401013B (cg-RX-API-DMAC7.html)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2755958T3 (en) * 2011-09-12 2017-09-25 Merck Patent Gmbh AMINOPYRIMIDINE DERIVATIVES USED AS MODULATORS OF KINASE ACTIVITY
JP2015533181A (ja) 2012-10-16 2015-11-19 アルミラル・ソシエダッド・アノニマＡｌｍｉｒａｌｌ， Ｓ．Ａ． Ｐｉ３ｋ阻害剤としてのピロロトリアジノン誘導体
ES2807539T3 (es) 2012-11-16 2021-02-23 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de quinasa
HK1218756A1 (zh) * 2013-03-11 2017-03-10 默克专利有限公司 用作激酶活性调节剂的6-[4-(1h-咪唑-2-基)哌啶-1-基]嘧啶-4-胺衍生物
KR20160110953A (ko) * 2014-02-11 2016-09-23 메르크 파텐트 게엠베하 키나아제 활성의 조절자로서의 피리미딘 이미다졸 아민
WO2015159938A1 (ja) 2014-04-18 2015-10-22 武田薬品工業株式会社 複素環化合物
CN109467538A (zh) 2017-09-07 2019-03-15 和记黄埔医药（上海）有限公司 环烯烃取代的杂芳环类化合物及其用途
KR20200093159A (ko) 2019-01-28 2020-08-05 주식회사 링크모션 스마트 팜 모듈 구조물
SI4069691T1 (sl) 2019-12-06 2025-02-28 Vertex Pharmaceuticals Incorporated Substituirani tetrahidrofurani kot modulatorji natrijevih kanalčkov
US11866421B2 (en) 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment
EP4347031B1 (en) 2021-06-04 2025-10-29 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels
CN117567435A (zh) * 2022-01-30 2024-02-20 上海市第十人民医院 谷氨酰胺环化酶抑制剂及其应用

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
JP2006522124A (ja) 2003-04-03 2006-09-28 バーテックス　ファーマシューティカルズ　インコーポレイテッド プロテインキナーゼのインヒビターとして有用な組成物
US7189729B2 (en) 2003-09-30 2007-03-13 Irm Llc Methods and compositions as protein kinase inhibitors
US7816353B2 (en) 2003-10-24 2010-10-19 Exelixis, Inc. P70S6 kinase modulators and method of use
ATE400573T1 (de) 2003-11-21 2008-07-15 Novartis Pharma Gmbh 1h-imidazochinolinderivate als proteinkinaseinhibitoren
JP2007513962A (ja) 2003-12-09 2007-05-31 アメリカ合衆国 免疫応答を抑制するため、または増殖性障害を治療するための方法
JP5213229B2 (ja) 2004-04-23 2013-06-19 エグゼリクシス， インコーポレイテッド キナーゼ調節因子および使用方法
JP5274842B2 (ja) 2004-12-28 2013-08-28 エグゼリクシス， インコーポレイテッド 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター（ｐ７０Ｓ６Ｋ、Ａｋｔ−１およびＡｋｔ−２）としての［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジンまたは［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジン化合物
CN101107245A (zh) 2005-01-19 2008-01-16 神经能质公司 经杂芳基取代的哌嗪-吡啶类似物
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
WO2006136821A1 (en) 2005-06-22 2006-12-28 Astex Therapeutics Limited Pharmaceutical compounds
AR064416A1 (es) * 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas.
UA99284C2 (ru) * 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
AR074072A1 (es) 2008-11-11 2010-12-22 Lilly Co Eli Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme
UA107188C2 (uk) 2009-02-11 2014-12-10 Карбоксамідні похідні хіназолінів або хінолінів та фармацевтична композиція на їх основі
CN103140484B (zh) 2010-07-29 2015-04-22 默克专利有限公司 环状胺氮杂杂环甲酰胺
UA110113C2 (xx) 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
AU2011334173B2 (en) 2010-11-24 2015-07-16 Merck Patent Gmbh Quinazoline carboxamide azetidines

Also Published As

Publication number Publication date
JP2014531436A (ja) 2014-11-27
NO2791461T3 (cg-RX-API-DMAC7.html) 2018-07-21
AU2012308696B2 (en) 2017-04-27
SG10201606301YA (en) 2016-09-29
MX346095B (es) 2017-03-07
PL2755965T3 (pl) 2018-01-31
IL231383A (en) 2017-11-30
KR20140063694A (ko) 2014-05-27
IL231383A0 (en) 2014-04-30
SI2755965T1 (sl) 2017-12-29
US9145392B2 (en) 2015-09-29
EA025098B1 (ru) 2016-11-30
LT2755965T (lt) 2017-11-10
HK1201825A1 (zh) 2015-09-11
PT2755965T (pt) 2017-11-02
HRP20171554T1 (hr) 2017-11-17
BR112014005554A2 (pt) 2017-03-21
SG2014009278A (en) 2014-07-30
HUE035019T2 (en) 2018-03-28
JP5964974B2 (ja) 2016-08-03
EP2755965A1 (en) 2014-07-23
ES2644536T3 (es) 2017-11-29
US20140343029A1 (en) 2014-11-20
MX2014002832A (es) 2014-05-27
RS56534B1 (sr) 2018-02-28
CN104080782A (zh) 2014-10-01
EA201400339A1 (ru) 2014-08-29
AU2012308696A1 (en) 2014-02-27
CA2844830A1 (en) 2013-03-21
CN104080782B (zh) 2016-06-01
KR101995605B1 (ko) 2019-07-02
DK2755965T3 (en) 2017-09-25
WO2013040059A1 (en) 2013-03-21
ZA201401013B (en) 2018-07-25
EP2755965B1 (en) 2017-07-26
US20160000785A1 (en) 2016-01-07

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Effective date: 20170818

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Effective date: 20220912