AU2013209586B2 - Substituted pyrimidine compounds and their use as SYK inhibitors - Google Patents

Substituted pyrimidine compounds and their use as SYK inhibitors Download PDF

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Publication number
AU2013209586B2
AU2013209586B2 AU2013209586A AU2013209586A AU2013209586B2 AU 2013209586 B2 AU2013209586 B2 AU 2013209586B2 AU 2013209586 A AU2013209586 A AU 2013209586A AU 2013209586 A AU2013209586 A AU 2013209586A AU 2013209586 B2 AU2013209586 B2 AU 2013209586B2
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Prior art keywords
methyl
pyrazol
indol
pyrimidin
ylamino
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AU2013209586A1 (en
Inventor
Jang-Sik Choi
Yung-geun CHOI
Ik-hwan HAN
Hae-Jun HWANG
Dong Sik Jung
Jung-Ho Kim
Se Won Kim
Jong Sung Koh
Eunho Lee
In Yong Lee
Jaekyoo Lee
Jaesang Lee
Tae-im LEE
Ho-Juhn Song
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Oscotec Inc
Genosco
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Oscotec Inc
Genosco
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    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • 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

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  • Chemical & Material Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2013209586A 2012-01-20 2013-01-18 Substituted pyrimidine compounds and their use as SYK inhibitors Active AU2013209586B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261588793P 2012-01-20 2012-01-20
US61/588,793 2012-01-20
PCT/US2013/022135 WO2013109882A1 (en) 2012-01-20 2013-01-18 Substituted pyrimidine compounds and their use as syk inhibitors

Publications (2)

Publication Number Publication Date
AU2013209586A1 AU2013209586A1 (en) 2014-07-24
AU2013209586B2 true AU2013209586B2 (en) 2017-08-17

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AU2013209586A Active AU2013209586B2 (en) 2012-01-20 2013-01-18 Substituted pyrimidine compounds and their use as SYK inhibitors

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US (1) US8871778B2 (enExample)
EP (1) EP2804861B1 (enExample)
JP (1) JP6062962B2 (enExample)
KR (1) KR101944914B1 (enExample)
CN (1) CN104203943B (enExample)
AU (1) AU2013209586B2 (enExample)
CA (1) CA2863517C (enExample)
ES (1) ES2668479T3 (enExample)
NZ (1) NZ627113A (enExample)
PL (1) PL2804861T3 (enExample)
WO (1) WO2013109882A1 (enExample)
ZA (1) ZA201406038B (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2890552T3 (es) * 2013-10-21 2022-01-20 Genosco Compuestos de pirimidina sustituidos y su uso como inhibidores de SYK
CN103969445B (zh) * 2014-05-08 2015-09-30 中南大学 亚铁血红素—二氧化锰复合物的制备及其用于检测人IgG的方法
HRP20250213T1 (hr) 2014-10-13 2025-04-25 Yuhan Corporation Spojevi i pripravci za modulaciju aktivnosti egfr mutantne kinaze
US10351532B2 (en) 2014-12-29 2019-07-16 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Small molecule inhibitors of lactate dehydrogenase and methods of use thereof
CA3065114A1 (en) 2017-06-14 2018-12-20 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Syk inhibitor and use method therefor
PT3658547T (pt) * 2017-07-28 2023-10-20 Yuhan Corp Processo de preparação de n -(5 -(4 -(4 -formil -3- fenil- 1h -pirazol- 1 -il)pirimidin -2- ilamino) -4 -metoxi 2- morfolinofenil) acrilamida
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
PL3943491T3 (pl) 2019-03-19 2025-11-17 Voronoi Inc. Pochodna heteroarylowa, sposób jej wytwarzania i kompozycja farmaceutyczna zawierająca ją jako skuteczny składnik
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
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
CN116323595B (zh) * 2020-09-23 2025-08-19 内尔维亚诺医疗科学公司 作为激酶抑制剂的吡唑基-嘧啶衍生物

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010038081A2 (en) * 2008-10-03 2010-04-08 Astrazeneca Ab Heterocyclic derivatives and methods of use thereof
WO2011060295A1 (en) * 2009-11-13 2011-05-19 Genosco Kinase inhibitors

Family Cites Families (3)

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PT923581E (pt) * 1996-08-09 2003-10-31 Boehringer Ingelheim Pharma Beta-carbolina 4-substituidas como imunomoduladores.
AU2004225965A1 (en) * 2003-03-25 2004-10-14 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
EP2668177B1 (en) * 2011-01-28 2014-10-22 Boehringer Ingelheim International GmbH Substituted pyridinyl-pyrimidines and their use as medicaments

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010038081A2 (en) * 2008-10-03 2010-04-08 Astrazeneca Ab Heterocyclic derivatives and methods of use thereof
WO2011060295A1 (en) * 2009-11-13 2011-05-19 Genosco Kinase inhibitors
US20110281841A1 (en) * 2009-11-13 2011-11-17 Oscotec, Inc. Kinase Inhibitors

Also Published As

Publication number Publication date
EP2804861A4 (en) 2015-07-22
ZA201406038B (en) 2015-12-23
ES2668479T3 (es) 2018-05-18
KR101944914B1 (ko) 2019-02-07
EP2804861B1 (en) 2018-02-28
CA2863517A1 (en) 2013-07-25
HK1205106A1 (en) 2015-12-11
CN104203943A (zh) 2014-12-10
NZ627113A (en) 2016-07-29
JP2015504093A (ja) 2015-02-05
US20130274242A1 (en) 2013-10-17
CN104203943B (zh) 2017-12-29
PL2804861T3 (pl) 2018-08-31
JP6062962B2 (ja) 2017-01-18
CA2863517C (en) 2019-11-05
KR20140135954A (ko) 2014-11-27
WO2013109882A1 (en) 2013-07-25
AU2013209586A1 (en) 2014-07-24
US8871778B2 (en) 2014-10-28
EP2804861A1 (en) 2014-11-26

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DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ CHOI, JANG-SIK; HWANG, HAE-JUN; LEE, EUNHO; LEE, JAEKYOO; SONG, HO-JUHN; KIM, SE WON; KIM, JUNG-HO; KOH, JONG SUNG; LEE, TAE-IM; CHOI, YUNG-GEUN; HAN, IK-HWAN; LEE, JAESANG; LEE, IN YONG; LEE, JAESANG AND JUNG, DONG SIK

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ CHOI, JANG-SIK; HWANG, HAE-JUN; LEE, EUNHO; LEE, JAEKYOO; SONG, HO-JUHN; KIM, SE WON; KIM, JUNG-HO; KOH, JONG SUNG; LEE, TAE-IM; CHOI, YUNG-GEUN; HAN, IK-HWAN; LEE, JAESANG; LEE, IN YONG AND JUNG, DONG SIK

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