EA201690818A1 - Замещенные пиримидиновые соединения и их применение в качестве syk ингибиторов - Google Patents

Замещенные пиримидиновые соединения и их применение в качестве syk ингибиторов

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Publication number
EA201690818A1
EA201690818A1 EA201690818A EA201690818A EA201690818A1 EA 201690818 A1 EA201690818 A1 EA 201690818A1 EA 201690818 A EA201690818 A EA 201690818A EA 201690818 A EA201690818 A EA 201690818A EA 201690818 A1 EA201690818 A1 EA 201690818A1
Authority
EA
Eurasian Patent Office
Prior art keywords
application
pyrimidine compounds
substituted pyrimidine
syk inhibitors
formula
Prior art date
Application number
EA201690818A
Other languages
English (en)
Other versions
EA030962B1 (ru
Inventor
Джекиу Ли
Джанг-сик Чой
Хае-Джун Хванг
Хо-Джун Сонг
Джунг-хо Ким
Се-Вон Ким
Джонг Сунг Кох
Джаесанг Ли
Тае-Им Ли
Юнг-геун Чой
Сунг-Хо Парк
Ин Йонг Ли
Бьюнг-Чул Сух
Пареш Девидас Салгаонкар
Донг-Сик Джунг
Original Assignee
Джиноско
Оскотек, Инк.
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.)
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Publication date
Application filed by Джиноско, Оскотек, Инк. filed Critical Джиноско
Publication of EA201690818A1 publication Critical patent/EA201690818A1/ru
Publication of EA030962B1 publication Critical patent/EA030962B1/ru

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    • 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
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/535—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
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0021—Intradermal administration, e.g. through microneedle arrays, needleless injectors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
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    • A61P7/06—Antianaemics
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Abstract

Раскрываются соединения формулы (I) и способы ингибирования киназ, включая тирозинкиназы селезенки. Также раскрываются способы лечения опосредованного киназами заболевания или состояния посредством введения субъекту терапевтически эффективного количества соединения формулы (I).
EA201690818A 2013-10-21 2014-10-21 Замещенные пиримидиновые соединения и их применение в качестве syk ингибиторов EA030962B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361893866P 2013-10-21 2013-10-21
PCT/US2014/061649 WO2015061369A1 (en) 2013-10-21 2014-10-21 Substituted pyrimidine compounds and their use as syk inhibitors

Publications (2)

Publication Number Publication Date
EA201690818A1 true EA201690818A1 (ru) 2016-08-31
EA030962B1 EA030962B1 (ru) 2018-10-31

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201690818A EA030962B1 (ru) 2013-10-21 2014-10-21 Замещенные пиримидиновые соединения и их применение в качестве syk ингибиторов

Country Status (22)

Country Link
US (1) US9212178B2 (ru)
EP (1) EP3060562B1 (ru)
JP (1) JP6434506B2 (ru)
KR (1) KR102228034B1 (ru)
CN (1) CN105940000B (ru)
AU (1) AU2014340249B2 (ru)
BR (1) BR112016008060A8 (ru)
CL (1) CL2016000939A1 (ru)
EA (1) EA030962B1 (ru)
ES (1) ES2890552T3 (ru)
HK (1) HK1226395A1 (ru)
HU (1) HUE056048T2 (ru)
IL (1) IL244817B (ru)
MX (1) MX2016004841A (ru)
MY (1) MY184561A (ru)
NZ (1) NZ718576A (ru)
PH (1) PH12016500735A1 (ru)
PL (1) PL3060562T3 (ru)
PT (1) PT3060562T (ru)
SA (1) SA516370989B1 (ru)
SG (1) SG11201602566XA (ru)
WO (1) WO2015061369A1 (ru)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
JP2023500906A (ja) 2019-11-08 2023-01-11 インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN113248472B (zh) * 2020-02-12 2022-06-28 中国药科大学 抗骨质疏松化合物及其衍生物，药物组合物、制备方法和应用
KR20210152312A (ko) * 2020-06-08 2021-12-15 주식회사 종근당 카나비노이드 수용체 (cb1 수용체) 길항제로서의 4-(4,5-디하이드로-1h-피라졸-1-닐)피리미딘 화합물 및 이를 포함하는 약제학적 조성물

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030158195A1 (en) 2001-12-21 2003-08-21 Cywin Charles L. 1,6 naphthyridines useful as inhibitors of SYK kinase
US20070020253A1 (en) 2002-10-16 2007-01-25 David Williams Spleen tyrosine kinase catalytic domain:crystal structure and binding pockets thereof
SE0300119D0 (sv) * 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
WO2004065395A1 (en) * 2003-01-17 2004-08-05 Astrazeneca Ab Thienopyridazinones and their use in modulation of autoimmune disease
SE0300120D0 (sv) * 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
TW200800215A (en) 2005-10-13 2008-01-01 Glaxo Group Ltd Novel compounds
AU2008296479A1 (en) * 2007-08-28 2009-03-12 Dana Farber Cancer Institute Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis
EP2324022A1 (de) 2008-08-05 2011-05-25 Boehringer Ingelheim International GmbH Substituierte naphthyridine und ihre verwendung als arzneimittel
JP5754568B2 (ja) 2008-08-05 2015-07-29 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ４−ジメチルアミノ−フェニルで置換されているナフチリジン、及び医薬としてのその使用
US8629132B2 (en) 2009-11-13 2014-01-14 Genosco Kinase inhibitors
NZ600857A (en) 2010-01-29 2014-06-27 Boehringer Ingelheim Int Substituted naphthyridines and their use as syk kinase inhibitors
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
KR20130083386A (ko) 2010-05-20 2013-07-22 에프. 호프만-라 로슈 아게 피롤로[2,3-ｂ]피라진-7-카복스아마이드 유도체 및 ＪＡＫ 및 ＳＹＫ 억제제로서의 그의 용도
US8637529B2 (en) * 2010-06-11 2014-01-28 AbbYie Inc. Pyrazolo[3,4-d]pyrimidine compounds
UY34484A (es) * 2011-12-15 2013-07-31 Bayer Ip Gmbh Benzotienilo-pirrolotriazinas disustituidas y sus usos
PL2804861T3 (pl) * 2012-01-20 2018-08-31 Genosco Podstawione związki pirymidyny i ich zastosowanie jako inhibitory SYK
ES2694223T3 (es) * 2012-03-22 2018-12-19 Oscotec, Inc. Compuestos de piridopirimidina y su uso como inhibidores de FLT3

Also Published As

Publication number Publication date
EP3060562B1 (en) 2021-07-28
EP3060562A1 (en) 2016-08-31
IL244817B (en) 2019-07-31
CN105940000B (zh) 2019-12-24
ES2890552T3 (es) 2022-01-20
NZ718576A (en) 2019-11-29
BR112016008060A8 (pt) 2020-03-17
AU2014340249A1 (en) 2016-04-28
WO2015061369A1 (en) 2015-04-30
KR20160068967A (ko) 2016-06-15
PT3060562T (pt) 2021-09-02
IL244817A0 (en) 2016-05-31
SA516370989B1 (ar) 2018-04-05
JP2016534054A (ja) 2016-11-04
MX2016004841A (es) 2016-07-26
MY184561A (en) 2021-04-03
US20150111883A1 (en) 2015-04-23
PH12016500735A1 (en) 2016-05-30
HK1226395A1 (zh) 2017-09-29
JP6434506B2 (ja) 2018-12-05
US9212178B2 (en) 2015-12-15
KR102228034B1 (ko) 2021-03-16
EA030962B1 (ru) 2018-10-31
AU2014340249B2 (en) 2017-05-25
EP3060562A4 (en) 2017-06-14
CN105940000A (zh) 2016-09-14
SG11201602566XA (en) 2016-05-30
HUE056048T2 (hu) 2022-01-28
PL3060562T3 (pl) 2022-01-10
CL2016000939A1 (es) 2016-11-11

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