AU2014340249B2 - 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
AU2014340249B2
AU2014340249B2 AU2014340249A AU2014340249A AU2014340249B2 AU 2014340249 B2 AU2014340249 B2 AU 2014340249B2 AU 2014340249 A AU2014340249 A AU 2014340249A AU 2014340249 A AU2014340249 A AU 2014340249A AU 2014340249 B2 AU2014340249 B2 AU 2014340249B2
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methyl
compound
indol
ylamino
formula
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AU2014340249A1 (en
Inventor
Jang-Sik Choi
Yung-geun CHOI
Hae-Jun HWANG
Dong-Sik Jung
Jung-Ho Kim
Se-Won Kim
Jong Sung Koh
In Yong Lee
Jaekyoo Lee
Jaesang Lee
Tae-im LEE
Sung-Ho Park
Paresh Devidas Salgaonkar
Ho-Juhn Song
Byung-Chul Suh
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Oscotec Inc
Genosco
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Oscotec Inc
Genosco
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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
    • 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
    • A61K31/535—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 or 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Otolaryngology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2014340249A 2013-10-21 2014-10-21 Substituted pyrimidine compounds and their use as SYK inhibitors Active AU2014340249B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361893866P 2013-10-21 2013-10-21
US61/893,866 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)

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AU2014340249A1 AU2014340249A1 (en) 2016-04-28
AU2014340249B2 true AU2014340249B2 (en) 2017-05-25

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AU2014340249A Active AU2014340249B2 (en) 2013-10-21 2014-10-21 Substituted pyrimidine compounds and their use as SYK inhibitors

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US (1) US9212178B2 (enExample)
EP (1) EP3060562B1 (enExample)
JP (1) JP6434506B2 (enExample)
KR (1) KR102228034B1 (enExample)
CN (1) CN105940000B (enExample)
AU (1) AU2014340249B2 (enExample)
CL (1) CL2016000939A1 (enExample)
EA (1) EA030962B1 (enExample)
ES (1) ES2890552T3 (enExample)
HU (1) HUE056048T2 (enExample)
IL (1) IL244817B (enExample)
MX (1) MX376059B (enExample)
MY (1) MY184561A (enExample)
NZ (1) NZ718576A (enExample)
PH (1) PH12016500735B1 (enExample)
PL (1) PL3060562T3 (enExample)
PT (1) PT3060562T (enExample)
SA (1) SA516370989B1 (enExample)
SG (1) SG11201602566XA (enExample)
WO (1) WO2015061369A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
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
US20240285621A1 (en) * 2020-09-23 2024-08-29 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
CN121443596A (zh) * 2023-04-24 2026-01-30 深圳市原力生命科学有限公司 Cdk2抑制剂及其使用方法
WO2026148272A1 (en) 2025-01-06 2026-07-09 Oscotec Inc. Crystalline forms of spleen tyrosine kinase inhibitor ski-o-703

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011060295A1 (en) * 2009-11-13 2011-05-19 Genosco Kinase inhibitors
WO2013109882A1 (en) * 2012-01-20 2013-07-25 Genosco Substituted pyrimidine compounds and their use as syk inhibitors

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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
SE0300120D0 (sv) * 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
US7393854B2 (en) * 2003-01-17 2008-07-01 Astrazeneca Ab Thienopyrimidinedinones and their use in modulation of autoimmune disease
SE0300119D0 (sv) * 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
JP2009511527A (ja) 2005-10-13 2009-03-19 グラクソ グループ リミテッド Syk阻害物質としてのピロロピリミジン誘導体
WO2009032703A1 (en) * 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors
JP2011529932A (ja) 2008-08-05 2011-12-15 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 置換ナフチリジン及び医薬としてのその使用
US8604049B2 (en) 2008-08-05 2013-12-10 Boehringer Ingelheim International Gmbh 4-dimethylamino-phenyl-substituted naphthyridines, and use thereof as medicaments
CA2786245A1 (en) 2010-01-29 2011-08-04 Boehringer Ingelheim International Gmbh Substituted naphthyridines and their use as syk kinase inhibitors
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
EP2571880A1 (en) 2010-05-20 2013-03-27 F.Hoffmann-La Roche Ag Pyrrolo [2, 3 - b]pyrazine - 7 - carboxamide derivatives and their use as jak and syk inhibitors
WO2011156698A2 (en) * 2010-06-11 2011-12-15 Abbott Laboratories NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS
UY34484A (es) * 2011-12-15 2013-07-31 Bayer Ip Gmbh Benzotienilo-pirrolotriazinas disustituidas y sus usos
WO2013142382A1 (en) * 2012-03-22 2013-09-26 Genosco Substituted pyridopyrimidine compounds and their use as flt3 inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011060295A1 (en) * 2009-11-13 2011-05-19 Genosco Kinase inhibitors
WO2013109882A1 (en) * 2012-01-20 2013-07-25 Genosco Substituted pyrimidine compounds and their use as syk inhibitors

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SG11201602566XA (en) 2016-05-30
EP3060562B1 (en) 2021-07-28
IL244817A0 (en) 2016-05-31
IL244817B (en) 2019-07-31
SA516370989B1 (ar) 2018-04-05
MX2016004841A (es) 2016-07-26
US20150111883A1 (en) 2015-04-23
US9212178B2 (en) 2015-12-15
WO2015061369A1 (en) 2015-04-30
EP3060562A1 (en) 2016-08-31
NZ718576A (en) 2019-11-29
MX376059B (es) 2025-03-07
MY184561A (en) 2021-04-03
JP6434506B2 (ja) 2018-12-05
CL2016000939A1 (es) 2016-11-11
PL3060562T3 (pl) 2022-01-10
JP2016534054A (ja) 2016-11-04
HUE056048T2 (hu) 2022-01-28
CN105940000A (zh) 2016-09-14
EA201690818A1 (ru) 2016-08-31
KR102228034B1 (ko) 2021-03-16
PH12016500735A1 (en) 2016-05-30
EA030962B1 (ru) 2018-10-31
AU2014340249A1 (en) 2016-04-28
HK1226395A1 (zh) 2017-09-29
PT3060562T (pt) 2021-09-02
KR20160068967A (ko) 2016-06-15
CN105940000B (zh) 2019-12-24
PH12016500735B1 (en) 2022-04-29
BR112016008060A8 (pt) 2020-03-17
EP3060562A4 (en) 2017-06-14
ES2890552T3 (es) 2022-01-20

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