KR101700454B1 - 피리미딘-2-아민 화합물 및 ｊａｋ 키나제 억제제로서의 그의 용도 - Google Patents

피리미딘-2-아민 화합물 및 ｊａｋ 키나제 억제제로서의 그의 용도 Download PDF

Info

Publication number
KR101700454B1
KR101700454B1 KR1020107020561A KR20107020561A KR101700454B1 KR 101700454 B1 KR101700454 B1 KR 101700454B1 KR 1020107020561 A KR1020107020561 A KR 1020107020561A KR 20107020561 A KR20107020561 A KR 20107020561A KR 101700454 B1 KR101700454 B1 KR 101700454B1
Authority
KR
South Korea
Prior art keywords
methyl
pyrimidin
amine
phenyl
heptan
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.)
Expired - Fee Related
Application number
KR1020107020561A
Other languages
English (en)
Korean (ko)
Other versions
KR20100124292A (ko
Inventor
소마세카르 바미디파티
제프리 클러프
앙쿠쉬 아게이드
라진더 싱
바딤 마르코프트소프
핑유 딩
지아신 유
앤디 아투에그부
후이 홍
이하브 다르위쉬
삼비아 토타
Original Assignee
리겔 파마슈티칼스, 인크.
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 리겔 파마슈티칼스, 인크. filed Critical 리겔 파마슈티칼스, 인크.
Publication of KR20100124292A publication Critical patent/KR20100124292A/ko
Application granted granted Critical
Publication of KR101700454B1 publication Critical patent/KR101700454B1/ko
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020107020561A 2008-02-15 2009-02-13 피리미딘-2-아민 화합물 및 ｊａｋ 키나제 억제제로서의 그의 용도 Expired - Fee Related KR101700454B1 (ko)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US2926508P 2008-02-15 2008-02-15
US61/029,265 2008-02-15
US3867208P 2008-03-21 2008-03-21
US61/038,672 2008-03-21
US11204608P 2008-11-06 2008-11-06
US61/112,046 2008-11-06
PCT/US2009/034159 WO2009103032A1 (en) 2008-02-15 2009-02-13 Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases

Publications (2)

Publication Number Publication Date
KR20100124292A KR20100124292A (ko) 2010-11-26
KR101700454B1 true KR101700454B1 (ko) 2017-01-26

Family

ID=40591956

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020107020561A Expired - Fee Related KR101700454B1 (ko) 2008-02-15 2009-02-13 피리미딘-2-아민 화합물 및 ｊａｋ 키나제 억제제로서의 그의 용도

Country Status (20)

Country Link
US (3) US8309566B2 (https=)
EP (1) EP2265607B1 (https=)
JP (2) JP5711537B2 (https=)
KR (1) KR101700454B1 (https=)
CN (1) CN102007124B (https=)
AU (1) AU2009214440B2 (https=)
CA (1) CA2715658C (https=)
CY (1) CY1118969T1 (https=)
DK (1) DK2265607T3 (https=)
ES (1) ES2617622T3 (https=)
HR (1) HRP20170317T1 (https=)
HU (1) HUE030912T2 (https=)
IL (1) IL207609A (https=)
LT (1) LT2265607T (https=)
MX (1) MX2010008926A (https=)
NZ (1) NZ587589A (https=)
PL (1) PL2265607T3 (https=)
PT (1) PT2265607T (https=)
SI (1) SI2265607T1 (https=)
WO (1) WO2009103032A1 (https=)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2078010B1 (en) 2006-12-29 2014-01-29 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
WO2008083353A1 (en) 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
JP2010514810A (ja) 2006-12-29 2010-05-06 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 Ａｘｌインヒビターとして有用な置換トリアゾール
CA2710046C (en) * 2006-12-29 2016-02-09 Rigel Pharmaceuticals, Inc. N3-heteroaryl substituted triazoles and n5-heteroaryl substituted triazoles useful as axl inhibitors
US8012965B2 (en) 2006-12-29 2011-09-06 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
JP5611826B2 (ja) * 2007-09-04 2014-10-22 ザ スクリプス リサーチ インスティテュート タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン
EP2205592B1 (en) * 2007-10-26 2013-05-08 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
HUE030912T2 (en) 2008-02-15 2017-06-28 Rigel Pharmaceuticals Inc Pyrimidine-2-amine compounds and their use as inhibitors of yak kinases
ES2537480T3 (es) 2008-07-09 2015-06-08 Rigel Pharmaceuticals, Inc. Triazoles sustituidos con heteroarilo policíclicos útiles como inhibidores de Axl
JP5613156B2 (ja) 2008-07-09 2014-10-22 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 Ａｘｌ阻害剤として有用な架橋二環ヘテロアリール置換トリアゾール
PL2387395T3 (pl) 2009-01-16 2015-03-31 Rigel Pharmaceuticals Inc Inhibitory Axl do zastosowania w terapii skojarzonej do zapobiegania, leczenia lub postępowania z nowotworem przerzutowym
EP2512246B1 (en) 2009-12-17 2015-09-30 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
KR101445012B1 (ko) 2009-12-17 2014-09-26 머크 샤프 앤드 돔 코포레이션 Ｓｙｋ 억제제로서의 아미노피리미딘
ES2577829T3 (es) 2010-06-04 2016-07-19 F. Hoffmann-La Roche Ag Derivados de aminopirimidina como moduladores de la LRRK2
JP2013531687A (ja) 2010-07-16 2013-08-08 パーデュー、ファーマ、リミテッド、パートナーシップ ナトリウムチャネル遮断剤としてのピリジン化合物
NO2638031T3 (https=) 2010-11-10 2018-03-10
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
EP2706853B1 (en) 2011-05-10 2017-06-14 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
CA2834062A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
WO2013136170A1 (en) 2012-03-16 2013-09-19 Purdue Pharma L.P. Substituted pyridines as sodium channel blockers
WO2013173506A2 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
US8809359B2 (en) * 2012-06-29 2014-08-19 Ym Biosciences Australia Pty Ltd Phenyl amino pyrimidine bicyclic compounds and uses thereof
CN103709172B (zh) * 2012-09-28 2018-02-13 江苏先声药业有限公司 取代呋喃并哌啶衍生物及其应用
EP2935257B1 (en) 2012-12-20 2018-02-07 Purdue Pharma LP Cyclic sulfonamides as sodium channel blockers
GB201303109D0 (en) 2013-02-21 2013-04-10 Domainex Ltd Novel pyrimidine compounds
WO2015019365A1 (en) 2013-08-07 2015-02-12 Cadila Healthcare Limited N-cyanomethylamides as inhibitors of janus kinase
CN104414427A (zh) * 2013-08-26 2015-03-18 皇家飞利浦有限公司 用于准备食物的具有带滑动机构的抽屉的装置
CN104860941B (zh) * 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
US10730866B2 (en) 2014-04-07 2020-08-04 Purdue Pharma L.P. Indole derivatives and use thereof
CN111333627B (zh) * 2015-03-11 2024-09-13 正大天晴药业集团股份有限公司 作为抗癌药物的取代的2-氢-吡唑衍生物
WO2017007658A1 (en) * 2015-07-07 2017-01-12 Rigel Pharmaceuticals, Inc. A combination for immune mediated cancer treatment
CN106810536A (zh) * 2015-11-30 2017-06-09 甘李药业股份有限公司 一种蛋白激酶抑制剂及其制备方法和医药用途
GB201702947D0 (en) 2017-02-23 2017-04-12 Domainex Ltd Novel compounds
WO2019246273A1 (en) 2018-06-20 2019-12-26 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with a jak or other kinase inhibitor
MA55909A (fr) 2019-05-05 2022-03-16 Qilu Regor Therapeutics Inc Inhibiteurs de cdk
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
CN113880813B (zh) * 2020-07-01 2024-05-28 杭州百诚医药科技股份有限公司 一种2-氨基嘧啶类杂环化合物及应用
WO2022042738A1 (zh) * 2020-08-31 2022-03-03 甘李药业股份有限公司 一种含cdk4/6抑制剂的药物组合物
WO2022147622A1 (en) * 2021-01-07 2022-07-14 Ontario Institute For Cancer Research (Oicr) Isoindolinone aminopyrimidine compounds as inhibitors of nuak kinases, compositions and uses thereof
CN115073425B (zh) * 2021-03-16 2023-11-14 中国科学院上海药物研究所 一类作为tbk1抑制剂的化合物、包含其的药物组合物及其用途
CN115160341B (zh) * 2022-07-18 2023-07-18 中国医学科学院医学实验动物研究所 苯并噁嗪类化合物及其药物用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007089768A2 (en) * 2006-01-30 2007-08-09 Exelixis, Inc. 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and pharmaceutical compositions containing them
WO2008003766A2 (en) * 2006-07-06 2008-01-10 Boehringer Ingelheim International Gmbh 4-heter0cycl0alkylpyri(mi)dines, process for the preparation thereof and their use as medicaments

Family Cites Families (114)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4788195A (en) 1986-01-13 1988-11-29 American Cyanamid Company 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines
US4876252A (en) 1986-01-13 1989-10-24 American Cyanamid Company 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines
US5728536A (en) 1993-07-29 1998-03-17 St. Jude Children's Research Hospital Jak kinases and regulation of Cytokine signal transduction
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
WO1995010506A1 (en) 1993-10-12 1995-04-20 The Du Pont Merck Pharmaceutical Company 1n-alkyl-n-arylpyrimidinamines and derivatives thereof
US6316635B1 (en) 1995-06-07 2001-11-13 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
US6696448B2 (en) 1996-06-05 2004-02-24 Sugen, Inc. 3-(piperazinylbenzylidenyl)-2-indolinone compounds and derivatives as protein tyrosine kinase inhibitors
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
GB9622363D0 (en) 1996-10-28 1997-01-08 Celltech Therapeutics Ltd Chemical compounds
US6316429B1 (en) 1997-05-07 2001-11-13 Sugen, Inc. Bicyclic protein kinase inhibitors
US6486185B1 (en) 1997-05-07 2002-11-26 Sugen, Inc. 3-heteroarylidene-2-indolinone protein kinase inhibitors
AU8181098A (en) 1997-07-03 1999-01-25 Du Pont Pharmaceuticals Company Aryl-and arylamino-substituted heterocycles as corticotropin releasing hormone antagonists
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US6133305A (en) 1997-09-26 2000-10-17 Sugen, Inc. 3-(substituted)-2-indolinones compounds and use thereof as inhibitors of protein kinase activity
WO2000000202A1 (en) 1998-06-30 2000-01-06 Parker Hughes Institute Method for inhibiting c-jun expression using jak-3 inhibitors
KR20010089171A (ko) 1998-08-21 2001-09-29 추후제출 퀴나졸린 유도체
US6841567B1 (en) 1999-02-12 2005-01-11 Cephalon, Inc. Cyclic substituted fused pyrrolocarbazoles and isoindolones
US6624171B1 (en) 1999-03-04 2003-09-23 Smithkline Beecham Corporation Substituted aza-oxindole derivatives
GB9904995D0 (en) 1999-03-04 1999-04-28 Glaxo Group Ltd Substituted aza-oxindole derivatives
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
BR0013551A (pt) 1999-08-13 2003-06-17 Vertex Pharma Inibidores de cinases n-terminal cjun (jnk) e outras cinases de proteìnas
GB9924862D0 (en) 1999-10-20 1999-12-22 Celltech Therapeutics Ltd Chemical compounds
CA2392554A1 (en) 1999-11-30 2001-06-28 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
DE60037345T2 (de) 1999-12-10 2008-11-13 Pfizer Products Inc., Groton Pyrrolo(2,3-d)pyrimidin-Verbindungen
CO5271715A1 (es) 1999-12-21 2003-04-30 Sugen Inc 7-aza-indolin-2-onas sustituidas en 4 y su uso como inhibidores de proteiuna quinasa
EP1250137B1 (en) 2000-01-24 2007-08-15 Genzyme Corporation Jak/stat pathway inhibitors and the use thereof for the treatment of primary generalized osteoarthritis
KR20010111298A (ko) 2000-02-05 2001-12-17 버텍스 파마슈티칼스 인코포레이티드 Ｅｒｋ의 억제제로서 유용한 피라졸 조성물
JP4739632B2 (ja) 2000-02-05 2011-08-03 バーテックス ファーマシューティカルズ インコーポレイテッド Ｅｒｋのインヒビターとして有用なピラゾール組成物
US6608048B2 (en) 2000-03-28 2003-08-19 Wyeth Holdings Tricyclic protein kinase inhibitors
AR028261A1 (es) 2000-03-28 2003-04-30 Wyeth Corp Inhibidores triciclicos de la proteina quinasa
ATE423120T1 (de) 2000-06-26 2009-03-15 Pfizer Prod Inc Pyrroloä2,3-düpyrimidin verbindungen als immunosuppressive wirkstoffe
GB0022438D0 (en) 2000-09-13 2000-11-01 Novartis Ag Organic Compounds
AU2001229722A1 (en) 2000-11-29 2002-06-11 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
ATE407132T1 (de) 2000-12-05 2008-09-15 Vertex Pharma Inhibitoren von c-jun n-terminalen kinasen (jnk) und anderen proteinkinasen
US20020115173A1 (en) 2000-12-11 2002-08-22 Children's Medical Center Corporation Short peptides from the 'A-region' of protein kinases which selectively modulate protein kinase activity
WO2002055517A2 (en) 2000-12-20 2002-07-18 Jingrong Cui 4-(hetero)aryl substituted indolinones
US20040102455A1 (en) 2001-01-30 2004-05-27 Burns Christopher John Method of inhibiting kinases
AUPR279101A0 (en) 2001-01-30 2001-02-22 Cytopia Pty Ltd Protein kinase signalling
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
ES2316546T3 (es) 2001-02-20 2009-04-16 Astrazeneca Ab 2-arilamino-pirimidinas para el tratamiento de trastornos asociados a gsk3.
CA2441733A1 (en) 2001-03-29 2002-10-10 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
AU2002338642A1 (en) 2001-04-13 2002-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
ES2274035T3 (es) 2001-06-01 2007-05-16 Vertex Pharmaceuticals Incorporated Compuestos de tiazol utiles como inhibidores de proteina quinasas.
CA2450769A1 (en) 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
ATE337312T1 (de) 2001-07-03 2006-09-15 Vertex Pharma Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen
US7109204B2 (en) 2001-08-01 2006-09-19 Merck & Co., Inc. Tyrosine kinase inhibitors
US6433018B1 (en) 2001-08-31 2002-08-13 The Research Foundation Of State University Of New York Method for reducing hypertrophy and ischemia
WO2003020698A2 (en) 2001-09-06 2003-03-13 Prochon Biotech Ltd. Protein tyrosine kinase inhibitors
US6777417B2 (en) 2001-09-10 2004-08-17 Sugen, Inc. 3-(4,5,6,7-tetrahydroindol-2-ylmethylidiene-2-indolinone derivatives as kinase inhibitors
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
PY0228255A (es) 2001-12-06 2004-06-01 Pfizer Prod Inc Compuestos cristalinos novedosos
WO2003051886A1 (en) 2001-12-17 2003-06-26 Smithkline Beecham Corporation Pyrazolopyridazine derivatives
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US6998391B2 (en) 2002-02-07 2006-02-14 Supergen.Inc. Method for treating diseases associated with abnormal kinase activity
RU2004135386A (ru) 2002-05-06 2005-07-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Тиадиазолы или оксадиазолы и их применение в качестве ингибиторов протеинкиназы jak
JP2005528443A (ja) 2002-05-30 2005-09-22 バーテックス　ファーマシューティカルズ　インコーポレイテッド Ｊａｋキナーゼおよびｃｄｋ２プロテインキナーゼのインヒビター
GB0215844D0 (en) * 2002-07-09 2002-08-14 Novartis Ag Organic compounds
US7361665B2 (en) 2002-07-09 2008-04-22 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
AU2003262642B2 (en) 2002-08-14 2010-06-17 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
AU2003286876A1 (en) 2002-11-01 2004-06-07 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
US7259161B2 (en) 2002-11-04 2007-08-21 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
EP1560824A1 (en) 2002-11-05 2005-08-10 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
GB0226583D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
AU2003278529A1 (en) 2002-11-21 2004-06-15 Pfizer Products Inc. 3-amino-piperidine derivatives and processes for their preparation
NZ539901A (en) 2002-11-26 2007-09-28 Pfizer Prod Inc Method of treatment of transplant rejection
DE60326646D1 (de) 2002-12-18 2009-04-23 Vertex Pharma Benzisoxazolderivate, die sich als inhibitoren von proteinkinasen eigen
CA2523125A1 (en) 2003-03-25 2004-10-14 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
JP2006522125A (ja) 2003-03-25 2006-09-28 バーテックス　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のインヒビターとして有用なチアゾール
AU2004230841A1 (en) 2003-04-03 2004-10-28 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
OA13050A (en) 2003-04-29 2006-11-10 Pfizer Ltd 5,7-diaminopyrazolo [4,3-D] pyrimidines useful in the treatment of hypertension.
AU2003232650A1 (en) 2003-05-06 2004-11-26 Il Yang Pharm Co., Ltd. N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
US7504429B2 (en) 2003-07-24 2009-03-17 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2005012294A1 (en) 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
JP2007500178A (ja) 2003-07-30 2007-01-11 サイクラセル・リミテッド プロテインキナーゼ阻害剤としてのピリジニルアミノ−ピリミジン誘導体
EP1648875A1 (en) 2003-07-30 2006-04-26 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
EA200600225A1 (ru) 2003-08-14 2006-08-25 Пфайзер Инк. Производные пиперазина для лечения вич инфекций
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
KR100777885B1 (ko) 2003-10-03 2007-11-28 화이자 인코포레이티드 Ｈｉｖ 및 염증 치료를 위한 ｃｃｒ5 수용체 길항제 활성을갖는 이미다조피리딘 치환된 트로판 유도체
US7169781B2 (en) 2003-10-17 2007-01-30 Hoffmann-La Roche Inc. Imidazole derivatives and their use as pharmaceutical agents
TW200528101A (en) 2004-02-03 2005-09-01 Astrazeneca Ab Chemical compounds
GB0402653D0 (en) 2004-02-06 2004-03-10 Cyclacel Ltd Compounds
CA2564355C (en) 2004-05-07 2012-07-03 Amgen Inc. Protein kinase modulators and method of use
GB0411791D0 (en) 2004-05-26 2004-06-30 Cyclacel Ltd Compounds
JP2008510766A (ja) 2004-08-27 2008-04-10 ゲーペーツェー ビオテック アーゲー ピリミジン誘導体
SI1814878T1 (sl) 2004-11-24 2012-06-29 Rigel Pharmaceuticals Inc Spojine spiro-2,4-pirimidindiamina in njihova uporaba
ES2325035T3 (es) 2004-12-21 2009-08-24 Smithkline Beecham Corporation Inhibidores de quinasa erbb de 2-pirimidinil pirazolopiridina.
AU2006206458B2 (en) 2005-01-19 2012-10-25 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
GB0504753D0 (en) 2005-03-08 2005-04-13 Astrazeneca Ab Chemical compounds
US20080194561A1 (en) 2005-07-26 2008-08-14 Jerry Leroy Adams Compounds
US20080242667A1 (en) 2005-08-26 2008-10-02 Smithkline Beecham Corporation Pyrimidinyl-Pyrazole Inhibitors of Aurora Kinases
US7884119B2 (en) 2005-09-07 2011-02-08 Rigel Pharmaceuticals, Inc. Triazole derivatives useful as Axl inhibitors
DE102005048072A1 (de) 2005-09-24 2007-04-05 Bayer Cropscience Ag Thiazole als Fungizide
GB0520955D0 (en) 2005-10-14 2005-11-23 Cyclacel Ltd Compound
US7803806B2 (en) * 2005-11-03 2010-09-28 Sgx Pharmaceuticals, Inc. Pyrimidinyl-thiophene kinase modulators
JP5103403B2 (ja) 2005-12-05 2012-12-19 スミスクライン ビーチャム コーポレーション ２−ピリミジニルピラゾロピリジンＥｒｂＢキナーゼ阻害剤
WO2007132221A1 (en) 2006-05-12 2007-11-22 Cyclacel Limited Combined anticancer pyrimidine-thiazole aurora kinase inhibitors
WO2008045978A1 (en) 2006-10-10 2008-04-17 Rigel Pharmaceuticals, Inc. Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors
WO2008080134A2 (en) 2006-12-22 2008-07-03 Rigel Pharmaceuticals, Inc. 4-amin0-2- (hetero) arylamino-5- (hetero) arylthiazoles useful as axl inhibitors
EP2078010B1 (en) 2006-12-29 2014-01-29 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
US8012965B2 (en) 2006-12-29 2011-09-06 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
WO2008083353A1 (en) 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
JP2010514810A (ja) 2006-12-29 2010-05-06 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 Ａｘｌインヒビターとして有用な置換トリアゾール
CA2710046C (en) 2006-12-29 2016-02-09 Rigel Pharmaceuticals, Inc. N3-heteroaryl substituted triazoles and n5-heteroaryl substituted triazoles useful as axl inhibitors
KR101566840B1 (ko) 2007-03-12 2015-11-06 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 페닐 아미노 피리미딘 화합물 및 이의 용도
CN101932580B (zh) * 2007-06-01 2013-05-22 葛兰素史密丝克莱恩有限责任公司 咪唑并吡啶激酶抑制剂
EP2205592B1 (en) 2007-10-26 2013-05-08 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
HUE030912T2 (en) 2008-02-15 2017-06-28 Rigel Pharmaceuticals Inc Pyrimidine-2-amine compounds and their use as inhibitors of yak kinases
JP5613156B2 (ja) 2008-07-09 2014-10-22 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 Ａｘｌ阻害剤として有用な架橋二環ヘテロアリール置換トリアゾール
ES2537480T3 (es) 2008-07-09 2015-06-08 Rigel Pharmaceuticals, Inc. Triazoles sustituidos con heteroarilo policíclicos útiles como inhibidores de Axl
PL2387395T3 (pl) 2009-01-16 2015-03-31 Rigel Pharmaceuticals Inc Inhibitory Axl do zastosowania w terapii skojarzonej do zapobiegania, leczenia lub postępowania z nowotworem przerzutowym

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007089768A2 (en) * 2006-01-30 2007-08-09 Exelixis, Inc. 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and pharmaceutical compositions containing them
WO2008003766A2 (en) * 2006-07-06 2008-01-10 Boehringer Ingelheim International Gmbh 4-heter0cycl0alkylpyri(mi)dines, process for the preparation thereof and their use as medicaments

Also Published As

Publication number Publication date
JP2011512361A (ja) 2011-04-21
PT2265607T (pt) 2017-03-08
US9624229B2 (en) 2017-04-18
JP5711537B2 (ja) 2015-05-07
HRP20170317T1 (hr) 2017-04-21
LT2265607T (lt) 2017-03-27
KR20100124292A (ko) 2010-11-26
AU2009214440A1 (en) 2009-08-20
AU2009214440B2 (en) 2014-09-25
HUE030912T2 (en) 2017-06-28
EP2265607B1 (en) 2016-12-14
NZ587589A (en) 2012-10-26
CN102007124B (zh) 2014-06-18
EP2265607A1 (en) 2010-12-29
WO2009103032A1 (en) 2009-08-20
US8309566B2 (en) 2012-11-13
ES2617622T3 (es) 2017-06-19
CA2715658C (en) 2016-07-19
MX2010008926A (es) 2011-02-23
IL207609A (en) 2015-08-31
JP2015061846A (ja) 2015-04-02
IL207609A0 (en) 2010-12-30
SI2265607T1 (sl) 2017-06-30
DK2265607T3 (en) 2017-03-13
US20130018041A1 (en) 2013-01-17
US20090258864A1 (en) 2009-10-15
CN102007124A (zh) 2011-04-06
CA2715658A1 (en) 2009-08-20
US8735418B2 (en) 2014-05-27
CY1118969T1 (el) 2018-01-10
US20140213585A1 (en) 2014-07-31
PL2265607T3 (pl) 2017-07-31

Similar Documents

Publication Publication Date Title
KR101700454B1 (ko) 피리미딘-2-아민 화합물 및 ｊａｋ 키나제 억제제로서의 그의 용도
US11053215B2 (en) Heterocyclic compounds useful as Pim kinase inhibitors
AU2012295802B2 (en) Tricyclic heterocyclic compounds and JAK inhibitors
US9932343B2 (en) Fused tricyclic benzimidazoles derivatives as modulators of TNF activity
US12281122B1 (en) PI3K inhibitors
US8962596B2 (en) 5,7-substituted-imidazo[1,2-C]pyrimidines as inhibitors of JAK kinases
US10703748B2 (en) Diazanaphthalen-3-yl carboxamides and preparation and use thereof
AU2018373258B2 (en) Substituted furanopyrimidine compounds as PDE1 inhibitors
MX2012010050A (es) Inhibidores de pirrolopirazina cinasa.
US20250002507A1 (en) 7,8-dihydro-5h-1,6-naphthyridine derivatives as positive allosteric modulators of the muscarinic acetylcholine receptor m4 for treating neurological and psychiatric disorders
US20230203010A1 (en) Bicyclic amine cdk12 inhibitors
CN119053596A (zh) 作为激酶抑制剂的杂环化合物、其组合物及使用方法
HK1150606A (en) Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases
HK1150606B (en) Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases
KR20250174938A (ko) 무스카린성 아세틸콜린 수용체 m4의 양성 알로스테릭 조절제로서의 티아졸로피리딘 유도체
KR20250172652A (ko) 신경학적 및 정신의학적 장애의 치료에 유용한 무스카린성 아세틸콜린 수용체 m4의 양성 알로스테릭 조절제로서의 1,6-나프티리딘 유도체

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

R15-X000 Change to inventor requested

St.27 status event code: A-3-3-R10-R15-oth-X000

R16-X000 Change to inventor recorded

St.27 status event code: A-3-3-R10-R16-oth-X000

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

FPAY Annual fee payment

Payment date: 20200109

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20230121

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20230121