JP5957003B2 - 変異体選択的ｅｇｆｒ阻害剤およびその使用 - Google Patents

変異体選択的ｅｇｆｒ阻害剤およびその使用 Download PDF

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JP5957003B2
JP5957003B2 JP2013538820A JP2013538820A JP5957003B2 JP 5957003 B2 JP5957003 B2 JP 5957003B2 JP 2013538820 A JP2013538820 A JP 2013538820A JP 2013538820 A JP2013538820 A JP 2013538820A JP 5957003 B2 JP5957003 B2 JP 5957003B2
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egfr
compound
composition
variant
pharmaceutically acceptable
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JP2013542256A (ja
JP2013542256A5 (OSRAM
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クワンホー リー，
クワンホー リー，
デチャン ニュー，
デチャン ニュー，
マシュー フランク バエブスキー，
マシュー フランク バエブスキー，
Original Assignee
セルジーン アヴィロミクス リサーチ， インコーポレイテッド
セルジーン アヴィロミクス リサーチ， インコーポレイテッド
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    • 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
    • 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
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00—Antineoplastic 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
    • 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
    • C12Y207/10—Protein-tyrosine kinases (2.7.10)

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2013538820A 2010-11-10 2011-11-08 変異体選択的ｅｇｆｒ阻害剤およびその使用 Expired - Fee Related JP5957003B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US41238810P 2010-11-10 2010-11-10
US61/412,388 2010-11-10
US201161534330P 2011-09-13 2011-09-13
US61/534,330 2011-09-13
PCT/US2011/059726 WO2012064706A1 (en) 2010-11-10 2011-11-08 Mutant-selective egfr inhibitors and uses thereof

Publications (3)

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JP2013542256A JP2013542256A (ja) 2013-11-21
JP2013542256A5 JP2013542256A5 (OSRAM) 2014-11-27
JP5957003B2 true JP5957003B2 (ja) 2016-07-27

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JP2013538820A Expired - Fee Related JP5957003B2 (ja) 2010-11-10 2011-11-08 変異体選択的ｅｇｆｒ阻害剤およびその使用

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US (3) US8796255B2 (OSRAM)
EP (1) EP2637502B1 (OSRAM)
JP (1) JP5957003B2 (OSRAM)
ES (1) ES2665013T3 (OSRAM)
WO (1) WO2012064706A1 (OSRAM)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2300013T5 (pl) 2008-05-21 2025-04-28 Takeda Pharmaceutical Company Limited Pochodne fosforu jako inhibitor kinazy
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
TWI458721B (zh) 2008-06-27 2014-11-01 Celgene Avilomics Res Inc 雜芳基化合物及其用途
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
RU2013109393A (ru) 2010-08-10 2014-09-20 Сэлджин Авиаломикс Ресеарч, Инк. Безилатная соль ингибитора втк
BR112013008816A2 (pt) * 2010-10-14 2016-06-28 Ariad Pharma Inc método de tratamento de câncer direcionado ao egfr resistente à erlotinibe ou gefitinibe, ou uso de um sal farmacêuticamente aceito em um indivíduo
EP2635285B1 (en) 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CA2815858C (en) 2010-11-01 2018-10-16 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
CA2853498A1 (en) 2011-10-28 2013-05-02 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
CN110194748A (zh) 2012-01-13 2019-09-03 艾森生物科学公司 杂环化合物及其作为抗癌药的用途
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
BR112014022789B1 (pt) 2012-03-15 2022-04-19 Celgene Car Llc Formas sólidas de um inibidor de quinase de receptor do fator de crescimento epidérmico, composição farmacêutica e usos do mesmo
RU2711077C9 (ru) 2012-03-15 2020-08-11 Селджен Кар Ллс Соли ингибитора киназы рецептора эпидермального фактора роста
LT2840080T (lt) * 2012-04-17 2018-02-12 Fujifilm Corporation Heterociklinis junginys, turintis azotą, arba jo druska
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
WO2014100748A1 (en) 2012-12-21 2014-06-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
EP2953457B1 (en) 2013-02-08 2020-04-08 Celgene CAR LLC Erk inhibitors and uses thereof
WO2014134308A1 (en) 2013-03-01 2014-09-04 Amgen Inc. Substituted 7-oxo-pyrido [2, 3-d] pyrimidines and their use for the treatment of egfr / erbb2 related disorders
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
AU2014287016B2 (en) * 2013-07-11 2018-11-01 Acea Biosciences Inc. Pyrimidine derivatives as kinase inhibitors
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
EP3059227B1 (en) 2013-10-16 2019-06-26 FUJIFILM Corporation Salt of nitrogen-containing heterocyclic compound or crystal thereof, pharmaceutical composition, and flt3 inhibitor
UA115388C2 (uk) * 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2015158310A1 (zh) * 2014-04-18 2015-10-22 山东轩竹医药科技有限公司 一种酪氨酸激酶抑制剂及其用途
CN104130265B (zh) * 2014-04-29 2017-01-25 苏州景泓生物技术有限公司 一种含有螺环或桥环的嘧啶类化合物
EP3179858B1 (en) 2014-08-13 2019-05-15 Celgene Car Llc Forms and compositions of an erk inhibitor
BR112017003186A2 (pt) 2014-08-22 2017-11-28 Fujifilm Corp composição farmacêutica para tratamento de cancer positivo para mutação em flt3, inibidor de flt3 mutante e usos dos mesmos
CN105884695B (zh) * 2015-02-13 2019-02-26 山东轩竹医药科技有限公司 杂环衍生物类酪氨酸激酶抑制剂
CN105985318A (zh) * 2015-02-15 2016-10-05 宁波文达医药科技有限公司 作为t790变异抑制剂的嘧啶衍生物
JP6412471B2 (ja) 2015-07-15 2018-10-24 富士フイルム株式会社 含窒素複素環化合物の製造方法およびその中間体
CN106554347B (zh) 2015-09-25 2020-10-30 浙江博生医药有限公司 Egfr激酶抑制剂及其制备方法和应用
RU2018115334A (ru) 2015-10-09 2019-11-11 Ацея Терапьютикс, Инк. Фармацевтические соли, физические формы и композиции пирролопиримидиновых ингибиторов киназ, и способы их получения
CN105198821B (zh) * 2015-10-26 2017-12-05 苏州明锐医药科技有限公司 洛昔替尼的制备方法
CN108137544B (zh) * 2015-12-10 2022-01-04 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
CA3059072A1 (en) 2017-04-07 2018-10-11 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
EP3849538A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies

Family Cites Families (160)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8608335D0 (en) 1986-04-04 1986-05-08 Pfizer Ltd Pharmaceutically acceptable salts
JPH0741461A (ja) 1993-05-27 1995-02-10 Eisai Co Ltd スルホン酸エステル誘導体
CA2214685C (en) 1995-03-10 2008-05-20 Berlex Laboratories, Inc. Benzamidine derivatives their preparation and their use as anti-coagulants
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
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
WO1999031073A1 (en) 1997-12-15 1999-06-24 Yamanouchi Pharmaceutical Co., Ltd. Novel pyrimidine-5-carboxamide derivatives
US6303652B1 (en) 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
EP1107957B1 (en) 1998-08-29 2006-10-18 AstraZeneca AB Pyrimidine compounds
AU762523C (en) 1998-11-10 2004-02-12 Janssen Pharmaceutica N.V. HIV replication inhibiting pyrimidines
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
US6127376A (en) 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
WO2000046203A2 (en) 1999-02-04 2000-08-10 Millennium Pharmaceuticals, Inc. G-protein coupled heptahelical receptor binding compounds and methods of use thereof
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
ATE247645T1 (de) 1999-06-29 2003-09-15 Egyt Gyogyszervegyeszeti Gyar Neue piperazinylalkylthiopyrimidine derivate, diese enthaltende pharmazeutische zusammenstellungen und verfahren zu deren herstellung
JP4794793B2 (ja) 1999-12-28 2011-10-19 ファーマコペイア， インコーポレイテッド Ｎ−ヘテロ環ＴＮＦ−α発現阻害剤
US20030004174A9 (en) 2000-02-17 2003-01-02 Armistead David M. Kinase inhibitors
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
EP1282607B1 (en) 2000-05-08 2015-11-11 Janssen Pharmaceutica NV Prodrugs of hiv replication inhibiting pyrimidines
CA2417500C (en) 2000-07-28 2008-11-18 Georgetown University Medical Center Erbb-2 selective small molecule kinase inhibitors
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
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
EA007298B1 (ru) 2001-11-01 2006-08-25 Янссен Фармацевтика Н.В. Гетероариламины в качестве ингибиторов гликогенсинтаза-киназы 3-бета (ингибиторов gsk3)
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US7459455B2 (en) 2002-02-08 2008-12-02 Smithkline Beecham Corporation Pyrimidine compounds
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
WO2003081210A2 (en) 2002-03-21 2003-10-02 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
US20040002395A1 (en) 2002-06-27 2004-01-01 Poynor Raymond L. Bridge weight for metal wood golf club
ATE451104T1 (de) 2002-07-29 2009-12-15 Rigel Pharmaceuticals Inc Verfahren zur behandlung oder pruvention von autoimmunkrankheiten mit 2,4-pyrimidindiamin- verbindungen
CA2439440A1 (en) 2002-09-05 2004-03-05 Emory University Treatment of tuberous sclerosis associated neoplasms
AU2002951853A0 (en) 2002-10-04 2002-10-24 Commonwealth Scientific And Industrial Research Organisation Crystal structure of erbb2 and uses thereof
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
KR20110132482A (ko) 2003-02-07 2011-12-07 얀센 파마슈티카 엔.브이. Ｈｉｖ 감염 예방용 피리미딘 유도체
EP1597251B1 (en) 2003-02-20 2009-06-10 SmithKline Beecham Corporation Pyrimidine compounds
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
US20050043233A1 (en) 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
US7504396B2 (en) 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
ES2421139T3 (es) 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
EP1663242B1 (en) 2003-08-07 2011-04-27 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents
DK2287156T3 (da) 2003-08-15 2013-08-26 Novartis Ag 2,4-Di(phenylamino)-pyrimidiner egnede i behandling af neoplastiske sygdomme, inflammatoriske lidelser og lidelser i immunsystemet
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
JP2007505858A (ja) 2003-09-18 2007-03-15 ノバルティス アクチエンゲゼルシャフト 増殖性障害の処置に有用な２，４−ジ（フェニルアミノ）ピリミジン
JP2007514775A (ja) 2003-12-19 2007-06-07 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 １−（２，４−ピリミジンジアミノ）−２−シクロペンタンカルボキサイミド合成中間体の立体異性体および立体異性体混合物
KR101164541B1 (ko) 2004-01-12 2012-07-10 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 선택적 키나제 저해제
AU2005206541A1 (en) 2004-01-16 2005-08-04 Wyeth Quinoline intermediates of receptor tyrosine kinase inhibitors and the synthesis thereof
EP1735268B1 (en) 2004-03-15 2012-02-15 Eli Lilly And Company Opioid receptor antagonists
WO2005105988A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
CA2566531A1 (en) 2004-05-18 2005-12-15 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
EP3042964A1 (en) 2004-06-04 2016-07-13 Genentech, Inc. Egfr mutations
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
WO2006034473A2 (en) 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyrimidine compounds, process for their preparation and compositions containing them
CA2573976C (en) 2004-09-30 2014-04-29 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 5-carbo- or heterocyclic substituted pyrimidines
AU2005295788A1 (en) 2004-10-13 2006-04-27 Wyeth N-benzenesulfonyl substituted anilino-pyrimidine analogs
US20060088471A1 (en) 2004-10-20 2006-04-27 Proteolix, Inc. Compounds for enzyme inhibition
TW200628463A (en) 2004-11-10 2006-08-16 Synta Pharmaceuticals Corp Heteroaryl compounds
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
WO2006068770A1 (en) 2004-11-24 2006-06-29 Rigel Pharmaceuticals, Inc. Spiro-2, 4-pyrimidinediamine compounds and their uses
EP1841760B1 (en) 2004-12-30 2011-08-10 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
EP1856053A1 (en) 2005-01-14 2007-11-21 Millennium Pharmaceuticals, Inc. Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity
EP2161275A1 (en) 2005-01-19 2010-03-10 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
US8067175B2 (en) 2005-02-11 2011-11-29 Memorial Sloan-Kettering Cancer Center Methods and compositions for detecting a drug resistant EGFR mutant
AU2006227628A1 (en) 2005-03-16 2006-09-28 Targegen, Inc. Pyrimidine compounds and methods of use
DE102005016634A1 (de) 2005-04-12 2006-10-19 Merck Patent Gmbh Neuartige Aza-Hetercyclen als Kinase-Inhibitoren
WO2007027238A2 (en) 2005-05-03 2007-03-08 Rigel Pharmaceuticals, Inc. Jak kinase inhibitors and their uses
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
WO2006128172A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating b cell regulated autoimmune disorders
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7491732B2 (en) 2005-06-08 2009-02-17 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
JP5376950B2 (ja) 2005-10-21 2013-12-25 エクセリクシス， インク． カゼインキナーゼｉｉ（ｃｋ２）モジュレーターとしてのピリミジオン類
NZ592990A (en) 2005-11-01 2013-01-25 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007056151A2 (en) 2005-11-03 2007-05-18 Irm Llc Protein kinase inhbitors
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
US20080318989A1 (en) 2005-12-19 2008-12-25 Burdick Daniel J Pyrimidine Kinase Inhibitors
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
KR20080110998A (ko) 2006-01-30 2008-12-22 엑셀리시스, 인코포레이티드 Ｊａｋ­２ 조절자로서 ４­아릴­２­아미노­피리미딘 또는 4­아릴­２­아미노알킬­피리미딘 및 이들을 포함하는 약제학적 조성물
US7659280B2 (en) 2006-02-17 2010-02-09 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
WO2007098507A2 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
BRPI0709690B8 (pt) 2006-03-30 2021-05-25 Janssen R & D Ireland 5-amido pirimidinas substituídas e composição farmacêutica que as compreende
ATE482953T1 (de) 2006-03-30 2010-10-15 Tibotec Pharm Ltd Hiv-inhibierende 5-(hydroxymethylen- und aminomethylen) substituierte pyrimidine
GB0608386D0 (en) 2006-04-27 2006-06-07 Senexis Ltd Compounds
CA2650035C (en) 2006-04-27 2015-02-03 Intezyne Technologies, Inc. Poly (ethylene glycol) containing chemically disparate endgroups
US8604031B2 (en) 2006-05-18 2013-12-10 Mannkind Corporation Intracellular kinase inhibitors
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
CA2656290A1 (en) 2006-07-05 2008-01-10 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
WO2008009458A1 (en) 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
DE102006041382A1 (de) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren
PT2201840E (pt) 2006-09-22 2012-02-14 Pharmacyclics Inc Inibidores da tirosina quinase de bruton
WO2008049123A2 (en) 2006-10-19 2008-04-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine derivatives as inhibitors of jak kinases for the treatment of autoimmune diseases
EP2089391B1 (en) 2006-11-03 2013-01-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
US8163902B2 (en) 2006-11-21 2012-04-24 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
KR101149295B1 (ko) 2006-12-08 2012-07-05 아이알엠 엘엘씨 단백질 키나제 억제제로서의 화합물
CA2670645A1 (en) 2006-12-19 2008-07-03 Genentech, Inc. Pyrimidine kinase inhibitors
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
CN101573342A (zh) 2006-12-29 2009-11-04 泰博特克药品有限公司 抑制hiv的5,6-取代的嘧啶类化合物
KR20090094073A (ko) 2006-12-29 2009-09-03 티보텍 파마슈티칼즈 리미티드 Ｈｉｖ를 억제하는 6-치환된 피리미딘
AR065015A1 (es) 2007-01-26 2009-05-13 Smithkline Beecham Corp Derivados de antranilamida, composiciones farmaceuticas que los contienen, y usos para el tratamiento del cancer
AU2008210266B2 (en) 2007-01-31 2013-09-05 Ym Biosciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
DE102007010801A1 (de) 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
CN101677554A (zh) 2007-03-20 2010-03-24 史密丝克莱恩比彻姆公司 化合物
CN101686675A (zh) 2007-03-20 2010-03-31 史密丝克莱恩比彻姆公司 化合物
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
US20120065201A1 (en) 2007-03-28 2012-03-15 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
CA2689989A1 (en) 2007-06-04 2008-12-11 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
WO2009012421A1 (en) 2007-07-17 2009-01-22 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
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
CA2696824A1 (en) 2007-08-28 2009-03-12 Irm Llc Compounds and compositions as kinase inhibitors
WO2009029682A1 (en) 2007-08-28 2009-03-05 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
CA2702674C (en) 2007-10-19 2016-05-03 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
CA2710118A1 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
AU2009215430B2 (en) 2008-02-22 2015-02-12 Rigel Pharmaceuticals, Inc. Use of 2,4-pyrimidinediamines for the treatment of atherosclerosis
EP2276747A1 (en) 2008-03-11 2011-01-26 Cellzome Limited Sulfonamides as zap-70 inhibitors
US8205348B2 (en) 2008-03-19 2012-06-26 Zashiki-Warashi Manufacturing Inc. Tile spacer and holder therefor
CL2009000600A1 (es) 2008-03-20 2010-05-07 Bayer Cropscience Ag Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas.
WO2009127642A2 (en) 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
JP2011518836A (ja) 2008-04-24 2011-06-30 インサイト・コーポレイション 大環状化合物およびそれらのキナーゼ阻害剤としての使用
PL2300013T5 (pl) 2008-05-21 2025-04-28 Takeda Pharmaceutical Company Limited Pochodne fosforu jako inhibitor kinazy
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
TWI458721B (zh) 2008-06-27 2014-11-01 Celgene Avilomics Res Inc 雜芳基化合物及其用途
AU2009270856B2 (en) 2008-07-16 2013-07-25 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors
WO2010025833A1 (de) 2008-09-03 2010-03-11 Bayer Cropscience Ag Alkoxy- und alkylthio-substituierte anilinopyrimidine
US20110245156A1 (en) 2008-12-09 2011-10-06 Cytokine Pharmasciences, Inc. Novel antiviral compounds, compositions, and methods of use
CA2965031C (en) 2009-01-15 2018-12-04 F. Hoffmann-La Roche Ag Antibodies against phosphorylated tyrosines on erythropoietin receptor (epor)
WO2010112210A1 (en) 2009-04-03 2010-10-07 Cellzome Ag Methods for the identification of kinase interacting molecules and for the purification of kinase proteins
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
DK2428508T3 (en) 2009-05-08 2016-02-01 Astellas Pharma Inc Diamino heterocyclic carboxamide COMPOUND
CA2763720A1 (en) 2009-06-18 2010-12-23 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
US7741330B1 (en) 2009-10-12 2010-06-22 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase
WO2011079231A1 (en) 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
WO2011140338A1 (en) 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
EA201890869A3 (ru) 2010-06-03 2019-03-29 Фармасайкликс, Инк. Применение ингибиторов тирозинкиназы брутона (btk)
US20120071497A1 (en) 2010-06-03 2012-03-22 Pharmacyclics, Inc. Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
RU2013109393A (ru) 2010-08-10 2014-09-20 Сэлджин Авиаломикс Ресеарч, Инк. Безилатная соль ингибитора втк
US20130317029A1 (en) 2010-11-01 2013-11-28 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
EP2635285B1 (en) 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CA2815858C (en) 2010-11-01 2018-10-16 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
CN102558149A (zh) 2010-12-29 2012-07-11 中国医学科学院药物研究所 嘧啶衍生物、及其制法和药物组合物与用途
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
ES2770550T3 (es) 2011-05-17 2020-07-02 Univ California Inhibidores de quinasa
KR102054468B1 (ko) 2011-10-19 2019-12-11 파마싸이클릭스 엘엘씨 브루톤 티로신 인산화효소(btk)의 억제제의 용도
CN103159742B (zh) 2011-12-16 2015-08-12 北京韩美药品有限公司 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用
CA2890111A1 (en) 2012-11-02 2014-05-08 Pharmacyclics, Inc. Tec family kinase inhibitor adjuvant therapy
AR097204A1 (es) 2013-08-02 2016-02-24 Pharmacyclics Inc Métodos de tratamiento de tumores sólidos

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