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
Application filed by Merck Patent GmbH filed Critical Merck Patent GmbH
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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (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 (https=)
EP (1) EP2755965B1 (https=)
JP (1) JP5964974B2 (https=)
KR (1) KR101995605B1 (https=)
CN (1) CN104080782B (https=)
AU (1) AU2012308696B2 (https=)
BR (1) BR112014005554A2 (https=)
CA (1) CA2844830C (https=)
DK (1) DK2755965T3 (https=)
EA (1) EA025098B1 (https=)
ES (1) ES2644536T3 (https=)
HR (1) HRP20171554T1 (https=)
HU (1) HUE035019T2 (https=)
IL (1) IL231383A (https=)
LT (1) LT2755965T (https=)
MX (1) MX346095B (https=)
NO (1) NO2791461T3 (https=)
PL (1) PL2755965T3 (https=)
PT (1) PT2755965T (https=)
RS (1) RS56534B1 (https=)
SG (2) SG10201606301YA (https=)
SI (1) SI2755965T1 (https=)
WO (1) WO2013040059A1 (https=)
ZA (1) ZA201401013B (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103930407B (zh) * 2011-09-12 2019-02-26 默克专利有限公司 用作激酶活性调节剂的氨基嘧啶衍生物
AU2013333938A1 (en) 2012-10-16 2015-04-09 Almirall, S.A. Pyrrolotriazinone derivatives as PI3K inhibitors
AR093511A1 (es) 2012-11-16 2015-06-10 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de cinasas
SG11201505999VA (en) * 2013-03-11 2015-08-28 Merck Patent Gmbh 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity
US9434714B2 (en) 2014-02-11 2016-09-06 Merck Patent Gmbh Pyrimidine imidazole amines as modulators of kinase activity
EP3205645B1 (en) 2014-04-18 2019-10-23 Takeda Pharmaceutical Company Limited Heterocyclic compound
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
CA3164134A1 (en) 2019-12-06 2021-06-10 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofurans as modulators of sodium channels
US11866421B2 (en) 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment
SI4347031T1 (sl) 2021-06-04 2026-01-30 Vertex Pharmaceuticals Incorporated N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov
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
WO2004092154A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
AU2004278413B2 (en) 2003-09-30 2008-07-31 Irm Llc Compounds and compositions as protein kinase inhibitors
JP4800216B2 (ja) 2003-10-24 2011-10-26 エグゼリクシス， インコーポレイテッド ｐ７０Ｓ６キナーゼモジュレーターおよび使用方法
DE602004014969D1 (de) 2003-11-21 2008-08-21 Novartis Ag 1h-imidazochinolinderivate als proteinkinaseinhibitoren
CN1889958A (zh) 2003-12-09 2007-01-03 美国政府健康及人类服务部 抑制免疫应答或治疗增生性疾病的方法
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
CA2590961C (en) 2004-12-28 2013-11-26 Exelixis, Inc. [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases
JP2008528506A (ja) * 2005-01-19 2008-07-31 ニューロジェン・コーポレーション ヘテロアリール置換ピペラジニル−ピリジン類縁体
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
EP1902032A1 (en) 2005-06-22 2008-03-26 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
NZ595087A (en) 2009-02-11 2013-03-28 Merck Patent Gmbh Novel amino azaheterocyclic carboxamides
US9586938B2 (en) 2010-07-29 2017-03-07 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
UA110113C2 (xx) 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
PT2643313T (pt) 2010-11-24 2016-10-11 Merck Patent Gmbh Quinazolina carboxamida azetidinas

Also Published As

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

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EEER Examination request

Effective date: 20170818

MKLA Lapsed

Effective date: 20220912