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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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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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    • 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
    • C07D403/14—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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    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (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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ID=48799685

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

Country Status (12)

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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
PT3060562T (pt) * 2013-10-21 2021-09-02 Genosco Compostos de pirimidina substituídos e sua utilização como inibidores da 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
RS66529B1 (sr) 2014-10-13 2025-03-31 Yuhan Corp Jedinjenja i kompozicije za modulaciju aktivnosti egfr mutant kinaze
ES3042832T3 (en) 2014-12-29 2025-11-24 Us Health 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
RS64545B1 (sr) * 2017-07-28 2023-09-29 Yuhan Corp Postupak za pripremu n-(5-(4-(4-formil-3-fenil-1h-pirazol-1-il)pirimidin-2-ilamino)-4-metoksi-2-morfolinofenil)akrilamida
PL3943491T3 (pl) 2019-03-19 2025-11-17 Voronoi Inc. Pochodna heteroarylowa, sposób jej wytwarzania i kompozycja farmaceutyczna zawierająca ją jako skuteczny składnik
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
US20220401436A1 (en) 2019-11-08 2022-12-22 INSERM (Institute National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
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
JP2023543740A (ja) * 2020-09-23 2023-10-18 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤としてのピラゾリル－ピリミジン誘導体

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000516231A (ja) * 1996-08-09 2000-12-05 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 免疫調節物質としての４―置換β―カルボリン
AU2004225965A1 (en) * 2003-03-25 2004-10-14 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
WO2012101013A1 (en) * 2011-01-28 2012-08-02 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
WO2013109882A1 (en) 2013-07-25
CA2863517C (en) 2019-11-05
KR101944914B1 (ko) 2019-02-07
ES2668479T3 (es) 2018-05-18
CN104203943B (zh) 2017-12-29
EP2804861A1 (en) 2014-11-26
JP2015504093A (ja) 2015-02-05
EP2804861B1 (en) 2018-02-28
KR20140135954A (ko) 2014-11-27
HK1205106A1 (en) 2015-12-11
PL2804861T3 (pl) 2018-08-31
AU2013209586A1 (en) 2014-07-24
CA2863517A1 (en) 2013-07-25
US20130274242A1 (en) 2013-10-17
ZA201406038B (en) 2015-12-23
NZ627113A (en) 2016-07-29
JP6062962B2 (ja) 2017-01-18
US8871778B2 (en) 2014-10-28
CN104203943A (zh) 2014-12-10
EP2804861A4 (en) 2015-07-22

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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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