CN102066340B - 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物 - Google Patents

作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物 Download PDF

Info

Publication number
CN102066340B
CN102066340B CN200980122631.8A CN200980122631A CN102066340B CN 102066340 B CN102066340 B CN 102066340B CN 200980122631 A CN200980122631 A CN 200980122631A CN 102066340 B CN102066340 B CN 102066340B
Authority
CN
China
Prior art keywords
carboxamide
pyrimidine
phenylamino
cyclopropylamino
compound
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN200980122631.8A
Other languages
English (en)
Chinese (zh)
Other versions
CN102066340A (zh
Inventor
S·M·鲍尔
Z·J·贾
宋永红
徐亲
M·梅赫罗特拉
J·W·罗斯
黄沃林
C·文卡塔拉曼尼
A·潘迪
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Portola Pharmaceuticals LLC
Original Assignee
Portola Pharmaceuticals LLC
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.)
Filing date
Publication date
Application filed by Portola Pharmaceuticals LLC filed Critical Portola Pharmaceuticals LLC
Publication of CN102066340A publication Critical patent/CN102066340A/zh
Application granted granted Critical
Publication of CN102066340B publication Critical patent/CN102066340B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • 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
    • A61P11/06—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
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN200980122631.8A 2008-04-16 2009-04-16 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物 Active CN102066340B (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US4540608P 2008-04-16 2008-04-16
US4541708P 2008-04-16 2008-04-16
US61/045,417 2008-04-16
US61/045,406 2008-04-16
US12034808P 2008-12-05 2008-12-05
US12034408P 2008-12-05 2008-12-05
US61/120,344 2008-12-05
US61/120,348 2008-12-05
PCT/US2009/002420 WO2009145856A1 (en) 2008-04-16 2009-04-16 2, 6-diamino-pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors

Publications (2)

Publication Number Publication Date
CN102066340A CN102066340A (zh) 2011-05-18
CN102066340B true CN102066340B (zh) 2014-05-14

Family

ID=40750850

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980122631.8A Active CN102066340B (zh) 2008-04-16 2009-04-16 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物

Country Status (13)

Country Link
EP (1) EP2321283B1 (enExample)
JP (2) JP5705720B2 (enExample)
KR (1) KR101623997B1 (enExample)
CN (1) CN102066340B (enExample)
CA (2) CA2723205C (enExample)
DO (1) DOP2010000310A (enExample)
EA (1) EA024109B1 (enExample)
HN (1) HN2010002119A (enExample)
HR (1) HRP20161310T1 (enExample)
MA (1) MA32280B1 (enExample)
MY (1) MY155639A (enExample)
SV (1) SV2010003706A (enExample)
WO (1) WO2009145856A1 (enExample)

Families Citing this family (105)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20100132550A (ko) * 2008-04-16 2010-12-17 포톨라 파마슈티컬스, 인코포레이티드 ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
EP2361242B1 (en) 2008-10-17 2018-08-01 Oryzon Genomics, S.A. Oxidase inhibitors and their use
WO2010084160A1 (en) 2009-01-21 2010-07-29 Oryzon Genomics S.A. Phenylcyclopropylamine derivatives and their medical use
US8367689B2 (en) 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK
EP2428508B9 (en) 2009-05-08 2016-04-20 Astellas Pharma Inc. Diamino heterocyclic carboxamide compound
CA2812683C (en) 2009-09-25 2017-10-10 Oryzon Genomics S.A. Lysine specific demethylase-1 inhibitors and their use
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
EP2513098B1 (en) 2009-12-17 2016-11-09 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
WO2011075560A1 (en) 2009-12-17 2011-06-23 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
US8440689B2 (en) 2009-12-23 2013-05-14 Takeda Pharmaceutical Company Limited Fused heteroaromatic pyrrolidinones
WO2011106105A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
WO2011106573A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
JP2011182847A (ja) 2010-03-05 2011-09-22 Three M Innovative Properties Co 医療用粘着剤組成物
HUE030938T2 (en) 2010-04-19 2017-06-28 Oryzon Genomics Sa Lysine-specific demethylase-1 inhibitors and their use
PL2589592T3 (pl) 2010-06-30 2019-03-29 Fujifilm Corporation Nowe pochodne nikotynamidu lub ich sole
JP6035238B2 (ja) * 2010-07-21 2016-11-30 ライジェル ファーマシューティカルズ， インコーポレイテッド プロテインキナーゼｃ阻害剤およびその使用
WO2012013727A1 (en) 2010-07-29 2012-02-02 Oryzon Genomics S.A. Cyclopropylamine derivatives useful as lsd1 inhibitors
MX341732B (es) 2010-07-29 2016-08-30 Oryzon Genomics S A * Inhibidores de la demetilasa lsd1 basados en arilciclopropilamina y sus usos médicos.
WO2012045020A1 (en) * 2010-09-30 2012-04-05 Portola Pharmaceuticals, Inc. Combinations of 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide and fludarabine
US9061966B2 (en) 2010-10-08 2015-06-23 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
EP2712316A1 (en) * 2011-02-08 2014-04-02 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
EP3981395A1 (en) * 2011-02-08 2022-04-13 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
EP2489663A1 (en) 2011-02-16 2012-08-22 Almirall, S.A. Compounds as syk kinase inhibitors
UA120740C2 (uk) 2011-04-22 2020-02-10 Сігнал Фармасьютікалз, Елелсі Заміщені діамінокарбоксамідні і діамінокарбонітрильні похідні піримідинів, їх композиції і способи лікування з їх допомогою
EP2706852B1 (en) 2011-05-10 2018-08-22 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
JP2014513687A (ja) 2011-05-10 2014-06-05 メルク・シャープ・アンド・ドーム・コーポレーション Ｓｙｋ阻害薬としてのピリジルアミノピリジン
MX2013013090A (es) 2011-05-10 2013-12-16 Merck Sharp & Dohme Aminopirimidinas como inhibidores de tirosina cinaza del bazo.
EP2750671A2 (en) * 2011-05-19 2014-07-09 Oryzon Genomics, S.A. Lysine demethylase inhibitors for thrombosis and cardiovascular diseases
EP2741741A2 (en) * 2011-05-19 2014-06-18 Oryzon Genomics, S.A. Lysine demethylase inhibitors for inflammatory diseases or conditions
KR101255939B1 (ko) * 2011-05-31 2013-04-23 동화약품주식회사 4-(1ｈ-인다졸-6-일아미노)-ｎ-아이소프로필-2-(메틸티오)피리미딘-5-카르복스아미드 화합물 또는 이의 약학적으로 허용가능한 염을 포함하는 당뇨병 예방 또는 치료용 조성물
EP2723739B1 (en) 2011-06-22 2016-08-24 Takeda Pharmaceutical Company Limited Substituted 6-aza-isoindolin-1-one derivatives
WO2013054351A1 (en) * 2011-08-08 2013-04-18 Cadila Healthcare Limited Heterocyclic compounds
WO2013052393A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2763974B1 (en) 2011-10-05 2016-09-14 Merck Sharp & Dohme Corp. Phenyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
EP2763976B1 (en) 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
WO2013057322A1 (en) 2011-10-20 2013-04-25 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
BR112014009306B1 (pt) 2011-10-20 2021-07-20 Oryzon Genomics S.A. Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1
CA2856301C (en) 2011-11-23 2020-10-06 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
CA2856306A1 (en) * 2011-11-23 2013-05-30 Portola Pharmaceuticals, Inc. Selective kinase inhibitors
CN104169272A (zh) 2011-12-23 2014-11-26 赛尔佐姆有限公司 作为激酶抑制剂的嘧啶-2,4-二胺衍生物
ES2661444T3 (es) 2011-12-28 2018-04-02 Fujifilm Corporation Nuevo derivado de nicotinamida o sal del mismo
CN104159891B (zh) * 2012-01-10 2016-09-07 霍夫曼-拉罗奇有限公司 哒嗪酰胺化合物和它们作为syk 抑制剂的用途
US9085540B2 (en) * 2012-01-17 2015-07-21 Astellas Pharma Inc. Pyrazinecarboxamide compound
AU2013250378B2 (en) * 2012-04-17 2016-01-14 Fujifilm Corporation Nitrogen-containing heterocyclic compound or salt thereof
CN102731412A (zh) * 2012-06-13 2012-10-17 盛世泰科生物医药技术(苏州)有限公司 一种2,4-二氯-5-嘧啶甲醛的合成方法
WO2013192125A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
WO2013192128A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
CN102731375A (zh) * 2012-06-20 2012-10-17 盛世泰科生物医药技术(苏州)有限公司 4,6-二氯-5-嘧啶甲醛的合成
EP2863916B1 (en) 2012-06-22 2018-07-18 Merck Sharp & Dohme Corp. Substituted pyridine spleen tyrosine kinase (syk) inhibitors
US9416111B2 (en) 2012-06-22 2016-08-16 Merck Sharp & Dohme Corp. Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors
KR101446742B1 (ko) 2012-08-10 2014-10-01 한국화학연구원 Ｎ2,ｎ4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
WO2014031438A2 (en) 2012-08-20 2014-02-27 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
CN104640863B (zh) * 2012-09-20 2016-06-08 山东亨利医药科技有限责任公司 嘧啶胺衍生物及其制备方法和应用
EP2900665B1 (en) 2012-09-28 2018-01-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
CA2883534A1 (en) 2012-10-19 2014-04-24 F. Hoffmann-La Roche Ag Inhibitors of syk
US9540333B2 (en) * 2012-11-08 2017-01-10 Bristol-Myers Squibb Company Alkyl amide-substituted pyrimidine compounds useful in the modulation of IL-12, IL-23 and/or IFNα
WO2014093191A1 (en) 2012-12-12 2014-06-19 Merck Sharp & Dohme Corp. AMINO-PYRIMIDINE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2934525B1 (en) 2012-12-21 2019-05-08 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
EP2988749B1 (en) 2013-04-26 2019-08-14 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
WO2014176210A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
IN2013MU02611A (enExample) 2013-08-07 2015-06-12 Cadila Healthcare Ltd
SG10201901902WA (en) * 2013-10-21 2019-04-29 Merck Patent Gmbh Heteroaryl compounds as btk inhibitors and uses thereof
JP6345786B2 (ja) 2013-12-05 2018-06-20 ファーマサイクリックス エルエルシー ブルトン型チロシンキナーゼの阻害剤
US9783531B2 (en) 2013-12-20 2017-10-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
EP3083559B1 (en) 2013-12-20 2021-03-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
EP3083560B1 (en) 2013-12-20 2021-10-27 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
NZ715903A (en) * 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
EP3116506B1 (en) 2014-03-13 2019-04-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
MX2016012574A (es) * 2014-03-28 2017-09-26 Calitor Sciences Llc Compuestos heteroarilo sustituidos y metodos de uso.
JP6684780B2 (ja) 2014-08-25 2020-04-22 ソーク インスティテュート フォー バイオロジカル スタディーズ 新規ｕｌｋ１阻害剤およびそれを使用する方法
JP6649540B2 (ja) * 2014-10-14 2020-02-19 ノース・アンド・サウス・ブラザー・ファーマシー・インベストメント・カンパニー・リミテッド 置換されたヘテロアリール化合物および使用方法
JP6903577B2 (ja) * 2014-12-16 2021-07-14 シグナル ファーマシューティカルズ，エルエルシー 皮膚におけるｃ−Ｊｕｎ Ｎ末端キナーゼの阻害の測定方法
CA3210612A1 (en) 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
WO2016123291A1 (en) 2015-01-29 2016-08-04 Signal Pharmaceuticals, Llc Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
CN107683139A (zh) 2015-05-29 2018-02-09 博尔托拉制药公司 用于治疗b细胞恶性肿瘤的赛度替尼
CA2993173C (en) 2015-07-24 2023-10-03 Celgene Corporation Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein
EP3328496A4 (en) * 2015-08-02 2018-12-19 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibitors of ack1/tnk2 tyrosine kinase
ES2913119T3 (es) 2015-08-12 2022-05-31 Portola Pharm Inc Cerdulatinib para tratar mieloma
AR106830A1 (es) * 2015-12-04 2018-02-21 Asana Biosciences Llc Usos de piridazinonas para tratar el cáncer
WO2017096303A2 (en) 2015-12-04 2017-06-08 Portola Pharmaceuticals, Inc. Cerdulatinib for treating hematological cancers
KR101936054B1 (ko) 2017-06-23 2019-01-11 한국과학기술연구원 항염증 활성을 가지는 6-페녹시피리미딘 유도체, 이의 제조방법 및 이를 활성성분으로 하는 약학 조성물
US20200172529A1 (en) * 2017-08-18 2020-06-04 Beijing Hanmi Pharm. Co., Ltd. Chemical Compound, Pharmaceutical Composition Thereof, and Use and Application Thereof
AU2018337138B2 (en) 2017-09-21 2021-04-01 Beijing Scitech-Mq Pharmaceuticals Limited 2-substituted pyrazole amino-4-substituted amino-5-pyrimidine formamide compound, composition, and application thereof
JP2020537678A (ja) 2017-10-19 2020-12-24 バイエル・アニマル・ヘルス・ゲーエムベーハー 動物における疾患の治療および予防のための縮合ヘテロ芳香族ピロリドンの使用
JP7167146B2 (ja) 2017-11-06 2022-11-08 ブリストル－マイヤーズ スクイブ カンパニー Ｈｐｋ１阻害剤として有用なイソフラノン化合物
JP7254076B2 (ja) * 2017-11-19 2023-04-07 サンシャイン・レイク・ファーマ・カンパニー・リミテッド 置換ヘテロアリール化合物及び使用方法
CN108299312B (zh) * 2018-03-29 2020-10-30 郑州大学第一附属医院 一组嘧啶类衍生物及其在制备抗肿瘤药物中的应用
JP7324778B2 (ja) * 2018-05-04 2023-08-10 ポートラ ファーマシューティカルズ， エルエルシー セルデュラチニブ（ｃｅｒｄｕｌａｔｉｎｉｂ）の固体形態
JP7343526B2 (ja) * 2018-05-04 2023-09-12 ポートラ ファーマシューティカルズ， エルエルシー セルデュラチニブの合成
WO2020187292A1 (zh) * 2019-03-19 2020-09-24 北京赛特明强医药科技有限公司 2-取代吡唑氨基-4-取代氨基-5-嘧啶甲酰胺类化合物、组合物及其应用
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
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
TW202227418A (zh) * 2020-10-12 2022-07-16 大陸商四川海思科製藥有限公司 一種雜環衍生物及其在醫藥上的應用
US20240165123A1 (en) * 2021-03-09 2024-05-23 Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. Use of a compound containing a tricyclic heteroaryl group
WO2023043630A1 (en) * 2021-09-16 2023-03-23 Lomond Therapeutics, Inc. Compounds having n-arylpyrimidin-2-amine derivatives as therapeutic agents
WO2023109954A1 (en) 2021-12-16 2023-06-22 Lynk Pharmaceuticals Co. Ltd. Tyk2 inhibitors and compositions and methods thereof
WO2023108536A1 (en) * 2021-12-16 2023-06-22 Lynk Pharmaceuticals Co. Ltd. Tyk2 inhibitors and compositions and methods thereof
CN114621206B (zh) * 2022-03-24 2023-11-24 安徽医科大学 一种5-取代的嘧啶二胺类衍生物及其制备方法与应用
CN115304550A (zh) * 2022-07-25 2022-11-08 南通大学 哌嗪苯基氨基取代的嘧啶氨基酸衍生物及制备方法与应用
CN115141150B (zh) * 2022-07-25 2024-04-26 南通大学 2,4,5-三取代嘧啶羟胺酰衍生物及其制备方法与应用
WO2024107017A1 (ko) * 2022-11-18 2024-05-23 가톨릭대학교 산학협력단 Stat6 억제제를 이용한 전신경화증 비멘틴 변이 단백질 활성 억제 치료 조성물

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1665789A (zh) * 2002-06-28 2005-09-07 山之内制药株式会社 二氨基嘧啶酰胺衍生物
WO2008009458A1 (en) * 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE401312T1 (de) * 1997-12-15 2008-08-15 Astellas Pharma Inc Pyrimidin-5-carboxamid-derivate
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US8367689B2 (en) * 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1665789A (zh) * 2002-06-28 2005-09-07 山之内制药株式会社 二氨基嘧啶酰胺衍生物
WO2008009458A1 (en) * 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors

Also Published As

Publication number Publication date
WO2009145856A1 (en) 2009-12-03
CN102066340A (zh) 2011-05-18
EP2321283A1 (en) 2011-05-18
MA32280B1 (fr) 2011-05-02
EA201001619A1 (ru) 2011-06-30
CA2960692A1 (en) 2009-12-03
SV2010003706A (es) 2011-03-23
KR20100126863A (ko) 2010-12-02
JP5705720B2 (ja) 2015-04-22
HN2010002119A (es) 2013-06-17
HRP20161310T1 (hr) 2016-12-02
JP2011518158A (ja) 2011-06-23
DOP2010000310A (es) 2011-03-15
EA024109B1 (ru) 2016-08-31
CA2723205A1 (en) 2009-12-03
CA2960692C (en) 2019-09-24
KR101623997B1 (ko) 2016-05-24
EP2321283B1 (en) 2016-07-13
MY155639A (en) 2015-11-13
CA2723205C (en) 2017-03-14
JP2015078194A (ja) 2015-04-23

Similar Documents

Publication Publication Date Title
CN102066340B (zh) 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物
US11414410B2 (en) Inhibitors of protein kinases
KR101773313B1 (ko) ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드
US9139581B2 (en) Inhibitors of protein kinases
US8318755B2 (en) Inhibitors of SYK and JAK protein kinases
AU2009251863B2 (en) 2, 6-diamino-pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors
HK1158179B (en) 2, 6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors
HK1153192A (en) Inhibitors of protein kinases
HK1153192B (en) Inhibitors of protein kinases

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant