EA201400339A1 - Новые имидазоламины в качестве модуляторов киназной активности - Google Patents

Новые имидазоламины в качестве модуляторов киназной активности

Info

Publication number
EA201400339A1
EA201400339A1 EA201400339A EA201400339A EA201400339A1 EA 201400339 A1 EA201400339 A1 EA 201400339A1 EA 201400339 A EA201400339 A EA 201400339A EA 201400339 A EA201400339 A EA 201400339A EA 201400339 A1 EA201400339 A1 EA 201400339A1
Authority
EA
Eurasian Patent Office
Prior art keywords
new
imidazolamines
kynase
modulators
activity
Prior art date
Application number
EA201400339A
Other languages
English (en)
Other versions
EA025098B1 (ru
Inventor
Бейард Р. Хак
Сяолин Чэнь
Юфан Сяо
Руокси Лань
Лизбет Селест Диселм
Сюй Цю
Константин Неагу
Доналд Банкстон
Кристофер Чарлз Виктор Джонс
Original Assignee
Мерк Патент Гмбх
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 Мерк Патент Гмбх filed Critical Мерк Патент Гмбх
Publication of EA201400339A1 publication Critical patent/EA201400339A1/ru
Publication of EA025098B1 publication Critical patent/EA025098B1/ru

Links

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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Изобретение обеспечивает новые соединения имидазоламина в соответствии с формулой (I) и формулой (II), их изготовление и применение для лечения гиперпролиферативных заболеваний, таких как злокачественное новообразование.
EA201400339A 2011-09-12 2012-09-12 Имидазоламины в качестве модуляторов киназной активности EA025098B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161533601P 2011-09-12 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
EA201400339A1 true EA201400339A1 (ru) 2014-08-29
EA025098B1 EA025098B1 (ru) 2016-11-30

Family

ID=46881179

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201400339A EA025098B1 (ru) 2011-09-12 2012-09-12 Имидазоламины в качестве модуляторов киназной активности

Country Status (25)

Country Link
US (2) US9145392B2 (ru)
EP (1) EP2755965B1 (ru)
JP (1) JP5964974B2 (ru)
KR (1) KR101995605B1 (ru)
CN (1) CN104080782B (ru)
AU (1) AU2012308696B2 (ru)
BR (1) BR112014005554A2 (ru)
CA (1) CA2844830C (ru)
DK (1) DK2755965T3 (ru)
EA (1) EA025098B1 (ru)
ES (1) ES2644536T3 (ru)
HK (1) HK1201825A1 (ru)
HR (1) HRP20171554T1 (ru)
HU (1) HUE035019T2 (ru)
IL (1) IL231383A (ru)
LT (1) LT2755965T (ru)
MX (1) MX346095B (ru)
NO (1) NO2791461T3 (ru)
PL (1) PL2755965T3 (ru)
PT (1) PT2755965T (ru)
RS (1) RS56534B1 (ru)
SG (2) SG10201606301YA (ru)
SI (1) SI2755965T1 (ru)
WO (1) WO2013040059A1 (ru)
ZA (1) ZA201401013B (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
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RU2690679C2 (ru) * 2014-02-11 2019-06-05 Мерк Патент Гмбх Новые пиримидинимидазоламины в качестве модуляторов активности киназы

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AU2012308681B2 (en) * 2011-09-12 2017-07-13 Merck Patent Gmbh Aminopyrimidine derivatives for use as modulators of kinase activity
PE20150637A1 (es) 2012-10-16 2015-05-08 Almirall Sa Derivados de pirrolotriazinona como inhibidores de pi3k
CA2890345A1 (en) 2012-11-16 2014-05-22 Merck Patent Gmbh Imidazol-piperidinyl derivatives as modulators of kinase activity
BR112015021324A2 (pt) 2013-03-11 2017-07-18 Merck Patent Gmbh derivados de 6-[4-(1h-imidazol-2-il)piperidin-1-il]pirimidin-4-amina como moduladores de atividade de quinase
US9957251B2 (en) 2014-04-18 2018-05-01 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
CR20220316A (es) 2019-12-06 2022-10-07 Vertex Pharma Tetrahidrofuranos sustituidos como moduladores de canales de sodio
US11866421B2 (en) 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment
CN117794920A (zh) 2021-06-04 2024-03-29 沃泰克斯药物股份有限公司 N-(羟烷基(杂)芳基)四氢呋喃甲酰胺作为钠通道调节剂

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CA2541989C (en) 2003-10-24 2013-10-01 Exelixis, Inc. P70s6 kinase modulators and method of use
RU2006121646A (ru) 2003-11-21 2008-01-10 Новартис АГ (CH) Производные 1h-имидазохинолина в качестве ингибиторов протеинкиназы
BRPI0417498A (pt) 2003-12-09 2007-05-29 Us Gov Health & Human Serv método para suprimir uma resposta imune em um indivìduo; método de inibição da proliferação de um célula; método de tratamento de um distúrbio proliferativo em um indivìduo; método para selecionar um agente imunossupressor ou anti-proliferativo; composição farmacêutica e estente vascular
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WO2006071819A1 (en) 2004-12-28 2006-07-06 Exelixis, Inc. [1h-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2690679C2 (ru) * 2014-02-11 2019-06-05 Мерк Патент Гмбх Новые пиримидинимидазоламины в качестве модуляторов активности киназы

Also Published As

Publication number Publication date
KR20140063694A (ko) 2014-05-27
AU2012308696B2 (en) 2017-04-27
US9145392B2 (en) 2015-09-29
IL231383A (en) 2017-11-30
ZA201401013B (en) 2018-07-25
ES2644536T3 (es) 2017-11-29
US20140343029A1 (en) 2014-11-20
DK2755965T3 (en) 2017-09-25
HUE035019T2 (en) 2018-03-28
SI2755965T1 (sl) 2017-12-29
SG2014009278A (en) 2014-07-30
MX346095B (es) 2017-03-07
EP2755965A1 (en) 2014-07-23
HK1201825A1 (zh) 2015-09-11
CA2844830C (en) 2019-09-10
PL2755965T3 (pl) 2018-01-31
BR112014005554A2 (pt) 2017-03-21
CN104080782A (zh) 2014-10-01
JP2014531436A (ja) 2014-11-27
CA2844830A1 (en) 2013-03-21
KR101995605B1 (ko) 2019-07-02
HRP20171554T1 (hr) 2017-11-17
US20160000785A1 (en) 2016-01-07
WO2013040059A1 (en) 2013-03-21
CN104080782B (zh) 2016-06-01
NO2791461T3 (ru) 2018-07-21
AU2012308696A1 (en) 2014-02-27
IL231383A0 (en) 2014-04-30
RS56534B1 (sr) 2018-02-28
MX2014002832A (es) 2014-05-27
SG10201606301YA (en) 2016-09-29
LT2755965T (lt) 2017-11-10
PT2755965T (pt) 2017-11-02
EA025098B1 (ru) 2016-11-30
EP2755965B1 (en) 2017-07-26
JP5964974B2 (ja) 2016-08-03

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU