KR102228034B1 - 치환된 피리미딘 화합물 및 syk 억제제로서의 이의 용도 - Google Patents

치환된 피리미딘 화합물 및 syk 억제제로서의 이의 용도 Download PDF

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KR102228034B1
KR102228034B1 KR1020167013308A KR20167013308A KR102228034B1 KR 102228034 B1 KR102228034 B1 KR 102228034B1 KR 1020167013308 A KR1020167013308 A KR 1020167013308A KR 20167013308 A KR20167013308 A KR 20167013308A KR 102228034 B1 KR102228034 B1 KR 102228034B1
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methyl
compound
ylamino
indol
cyclopropyl
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KR20160068967A (ko
Inventor
이재규
최장식
황해준
송호준
김중호
김세원
고종성
이재상
이태임
최영근
박성호
이인용
서병철
파레쉬 데비다스 살가온칼
정동식
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제노스코
주식회사 오스코텍
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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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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)
KR1020167013308A 2013-10-21 2014-10-21 치환된 피리미딘 화합물 및 syk 억제제로서의 이의 용도 Active KR102228034B1 (ko)

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)

Publication Number Publication Date
KR20160068967A KR20160068967A (ko) 2016-06-15
KR102228034B1 true KR102228034B1 (ko) 2021-03-16

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US (1) US9212178B2 (cg-RX-API-DMAC10.html)
EP (1) EP3060562B1 (cg-RX-API-DMAC10.html)
JP (1) JP6434506B2 (cg-RX-API-DMAC10.html)
KR (1) KR102228034B1 (cg-RX-API-DMAC10.html)
CN (1) CN105940000B (cg-RX-API-DMAC10.html)
AU (1) AU2014340249B2 (cg-RX-API-DMAC10.html)
CL (1) CL2016000939A1 (cg-RX-API-DMAC10.html)
EA (1) EA030962B1 (cg-RX-API-DMAC10.html)
ES (1) ES2890552T3 (cg-RX-API-DMAC10.html)
HU (1) HUE056048T2 (cg-RX-API-DMAC10.html)
IL (1) IL244817B (cg-RX-API-DMAC10.html)
MX (1) MX376059B (cg-RX-API-DMAC10.html)
MY (1) MY184561A (cg-RX-API-DMAC10.html)
NZ (1) NZ718576A (cg-RX-API-DMAC10.html)
PH (1) PH12016500735B1 (cg-RX-API-DMAC10.html)
PL (1) PL3060562T3 (cg-RX-API-DMAC10.html)
PT (1) PT3060562T (cg-RX-API-DMAC10.html)
SA (1) SA516370989B1 (cg-RX-API-DMAC10.html)
SG (1) SG11201602566XA (cg-RX-API-DMAC10.html)
WO (1) WO2015061369A1 (cg-RX-API-DMAC10.html)

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)

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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
PH12016500735A1 (en) 2016-05-30
EA030962B1 (ru) 2018-10-31
AU2014340249A1 (en) 2016-04-28
AU2014340249B2 (en) 2017-05-25
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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