TWI433677B - 雜環化合物及其用途 - Google Patents

雜環化合物及其用途 Download PDF

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Publication number
TWI433677B
TWI433677B TW097120571A TW97120571A TWI433677B TW I433677 B TWI433677 B TW I433677B TW 097120571 A TW097120571 A TW 097120571A TW 97120571 A TW97120571 A TW 97120571A TW I433677 B TWI433677 B TW I433677B
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Taiwan
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compound
group
cancer
disease
nhc
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TW097120571A
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English (en)
Chinese (zh)
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TW200908983A (en
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Juswinder Singh
Shomir Ghosh
Arthur F Kluge
Russell C Petter
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Avila Therapeutics Inc
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • 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
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    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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    • 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
    • C07D401/14—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 three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • 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
    • C07D417/14—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 three or more hetero rings

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
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  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
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  • Hospice & Palliative Care (AREA)
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TW097120571A 2007-06-04 2008-06-03 雜環化合物及其用途 TWI433677B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US94187307P 2007-06-04 2007-06-04
US97204807P 2007-09-13 2007-09-13

Publications (2)

Publication Number Publication Date
TW200908983A TW200908983A (en) 2009-03-01
TWI433677B true TWI433677B (zh) 2014-04-11

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TW097120571A TWI433677B (zh) 2007-06-04 2008-06-03 雜環化合物及其用途

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US (4) US8242271B2 (enExample)
EP (1) EP2152079A4 (enExample)
JP (3) JP5526020B2 (enExample)
CA (1) CA2689989A1 (enExample)
TW (1) TWI433677B (enExample)
WO (1) WO2008151183A1 (enExample)

Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI433677B (zh) * 2007-06-04 2014-04-11 Avila Therapeutics Inc 雜環化合物及其用途
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
EP2361248B1 (en) 2008-06-27 2018-09-19 Celgene CAR LLC Heteroaryl compounds and uses thereof
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
CN105574346A (zh) * 2008-09-05 2016-05-11 新基阿维罗米克斯研究公司 多肽偶联物与不可逆抑制剂的设计方法和检测方法
AU2009298888A1 (en) 2008-09-23 2010-04-08 Georgetown University 1,2-benzisothiazolinone and isoindolinone derivatives
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Ｅｇｆｒ阻害剤及び疾患の治療方法
EP2440058A4 (en) 2009-06-12 2012-11-21 Dana Farber Cancer Inst Inc MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
CN101928277B (zh) * 2009-06-24 2012-09-19 浙江九洲药业股份有限公司 4-甲基-3-[[4-(3-吡啶基)-2-嘧啶基]氨基]安息香酸的制备方法、相关中间体及其应用
CN102548987B (zh) * 2009-07-14 2014-04-16 江苏迈度药物研发有限公司 作为激酶抑制剂的氟取代化合物及其使用方法
WO2011031896A2 (en) * 2009-09-09 2011-03-17 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
US9556426B2 (en) * 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
CA2784807C (en) 2009-12-29 2021-12-14 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
CN102812167A (zh) 2009-12-30 2012-12-05 阿维拉制药公司 蛋白的配体-介导的共价修饰
NZ607845A (en) 2010-08-10 2015-03-27 Celgene Avilomics Res Inc Besylate salt of a btk inhibitor
EP2635285B1 (en) 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2012061299A1 (en) 2010-11-01 2012-05-10 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
US8796255B2 (en) 2010-11-10 2014-08-05 Celgene Avilomics Research, Inc 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
US9428472B2 (en) 2011-08-16 2016-08-30 Georgetown University Methods of treating bacterial infections with 1,2-benzisothiazolinone and isoindolinone derivatives
EP2770830A4 (en) 2011-10-28 2015-05-27 Celgene Avilomics Res Inc METHODS OF TREATING A DISEASE OR DISEASE ASSOCIATED WITH TYROSINE KINASE BTK (BRUTON'S TYROSINE KINASE)
WO2013074986A1 (en) 2011-11-17 2013-05-23 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
MX356753B (es) 2012-03-15 2018-06-12 Celgene Avilomics Res Inc Formas solidas de un inhibidor de cinasa del receptor del factor de crecimiento epidermico.
PT2825042T (pt) 2012-03-15 2018-11-16 Celgene Car Llc Sais de um inibidor de cinases do recetor do fator de crescimento epidérmico
AU2013204563B2 (en) 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US10000483B2 (en) 2012-10-19 2018-06-19 Dana-Farber Cancer Institute, Inc. Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US9126950B2 (en) 2012-12-21 2015-09-08 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2014124230A2 (en) 2013-02-08 2014-08-14 Celgene Avilomics Research, Inc. Erk inhibitors and uses thereof
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
KR101665301B1 (ko) 2013-08-07 2016-10-11 카딜라 핼쓰캐어 리미티드 야누스 키나제의 억제제로서 n-시아노메틸아미드
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
JP6491202B2 (ja) 2013-10-18 2019-03-27 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
EP3489232A3 (en) 2014-04-04 2019-07-31 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2016020791A1 (en) * 2014-08-05 2016-02-11 Novartis Ag Ckit antibody drug conjugates
ES2741785T3 (es) 2014-08-13 2020-02-12 Celgene Car Llc Formas y composiciones de un inhibidor de ERK
EP3236959B1 (en) 2014-12-23 2025-09-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2978518C (en) 2015-03-27 2023-11-21 Nathanael S. Gray Inhibitors of cyclin-dependent kinases
CA2986441A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
US10011611B2 (en) 2015-08-14 2018-07-03 Reaction Biology Corp. Histone deacetylase inhibitors and methods for use thereof
JP7028766B2 (ja) 2015-09-09 2022-03-02 ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼの阻害剤
MA46205A (fr) * 2016-09-08 2019-07-17 Sabila Biosciences Llc Composés 1,2-dithiolane utiles dans la neuroprotection, les maladies et les états auto-immuns et cancéreux
CN107805240A (zh) * 2016-09-08 2018-03-16 中国科学院合肥物质科学研究院 一种新型的pdgfr激酶抑制剂及其用途
GB201616511D0 (en) 2016-09-29 2016-11-16 Mission Therapeutics Limited Novel compounds
GB201616627D0 (en) 2016-09-30 2016-11-16 Mission Therapeutics Limited Novel compounds
GB201708652D0 (en) 2017-05-31 2017-07-12 Mission Therapeutics Ltd Novel compounds and uses
CN110831936B (zh) 2017-06-20 2023-03-28 特殊治疗有限公司 具有dub抑制剂活性的取代氰基吡咯烷
WO2019236890A1 (en) * 2018-06-07 2019-12-12 Disarm Therapeutics, Inc. Inhibitors of sarm1
CN108623490A (zh) * 2018-06-22 2018-10-09 苏州市贝克生物科技有限公司 (2z)-4-(二甲基氨基)-2-丁烯酸盐酸盐的合成方法
WO2020005807A1 (en) 2018-06-25 2020-01-02 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
EP3897670A4 (en) 2018-12-19 2022-09-07 Disarm Therapeutics, Inc. MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
GB201905371D0 (en) 2019-04-16 2019-05-29 Mission Therapeutics Ltd Novel compounds
GB201905375D0 (en) 2019-04-16 2019-05-29 Mission Therapeutics Ltd Novel compounds
JP7289375B2 (ja) * 2019-06-06 2023-06-09 ディスアーム セラピューティクス， インコーポレイテッド Ｓａｒｍ１の阻害剤
GB201912674D0 (en) 2019-09-04 2019-10-16 Mission Therapeutics Ltd Novel compounds
CN111253335B (zh) * 2020-03-12 2023-06-06 浙江扬帆新材料股份有限公司 一种n-取代苯并异噻唑啉-3-酮衍生物的新合成方法
CN111269217B (zh) * 2020-04-07 2021-01-08 苏州信诺维医药科技有限公司 一种嘧啶胺类化合物、其制备方法及应用
KR20230006487A (ko) 2020-04-08 2023-01-10 미션 테라퓨틱스 엘티디 Usp30 억제제로서의 활성을 갖는 n-시아노피롤리딘
MX2022014429A (es) 2020-05-28 2022-12-07 Mission Therapeutics Ltd N-cianopirrolidinas con actividad como inhibidores de usp30.
US20230303547A1 (en) 2020-06-04 2023-09-28 Mission Therapeutics Limited N-cyanopyrrolidines with activity as usp30 inhibitors
HUE072598T2 (hu) 2020-06-08 2025-11-28 Mission Therapeutics Ltd 1-(5-(2-cianopiridin-4-il)oxazol-2-karbonil)-4-metilhexahidropirrolo[3,4-B]pirrol-5(1H)-karbonitril felhasználásra, mint USP30 inhibitor, mitokondriális diszfunkció, rák és fibrózisok kezelésében
GB202016800D0 (en) 2020-10-22 2020-12-09 Mission Therapeutics Ltd Novel compounds
EP4441044A1 (en) 2021-12-01 2024-10-09 Mission Therapeutics Limited Substituted n-cyanopyrrolidines with activity as usp30 inhibitors
CA3260486A1 (en) * 2022-07-19 2024-01-25 Chiesi Farm Spa HETEROARYL DERIVATIVES USED AS DDR INHIBITORS

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
GB0022438D0 (en) * 2000-09-13 2000-11-01 Novartis Ag Organic Compounds
US20040157855A1 (en) * 2001-04-05 2004-08-12 Michael Heinrich Use of n-phenyl-2-pyrimidineamine derivativea against mast cell-based diseases like allergic disorders
CA2446939C (en) * 2001-05-16 2005-08-02 Matthias Stein-Gerlach Pyridylpyrimidine derivatives as effective compounds against prion diseases
US6878697B2 (en) * 2001-06-21 2005-04-12 Ariad Pharmaceuticals, Inc. Phenylamino-pyrimidines and uses thereof
PT1442024E (pt) 2001-11-01 2008-06-12 Janssen Pharmaceutica Nv Derivados aminobenzamida como inibidores da glicogénio sintase quinase 3$g(b)
CA2463822A1 (en) * 2001-11-01 2003-05-08 Janssen Pharmaceutica N.V. Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors)
GB0201508D0 (en) * 2002-01-23 2002-03-13 Novartis Ag Organic compounds
GB0202873D0 (en) * 2002-02-07 2002-03-27 Novartis Ag Organic compounds
GB0215676D0 (en) * 2002-07-05 2002-08-14 Novartis Ag Organic compounds
WO2004013633A2 (en) * 2002-07-29 2004-02-12 Axxima Pharmaceuticals Ag Method for isolating atp binding proteins by means of immobolized protein inhibitors
MY139563A (en) * 2002-09-04 2009-10-30 Bristol Myers Squibb Co Heterocyclic aromatic compounds useful as growth hormone secretagogues
CA2439440A1 (en) * 2002-09-05 2004-03-05 Emory University Treatment of tuberous sclerosis associated neoplasms
GB0222514D0 (en) * 2002-09-27 2002-11-06 Novartis Ag Organic compounds
US7279576B2 (en) * 2002-12-31 2007-10-09 Deciphera Pharmaceuticals, Llc Anti-cancer medicaments
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
WO2005065074A2 (en) 2003-09-09 2005-07-21 Temple University Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
GB0325031D0 (en) * 2003-10-27 2003-12-03 Novartis Ag Organic compounds
WO2005049021A1 (en) 2003-11-03 2005-06-02 Oy Helsinki Transplantation R & D Ltd Materials and methods for inhibiting neointimal hyperplasia
JPWO2005063720A1 (ja) 2003-12-25 2007-07-19 日本新薬株式会社 アミド誘導体及び医薬
JPWO2005063709A1 (ja) * 2003-12-25 2007-07-19 日本新薬株式会社 アミド誘導体及び医薬
DE602005023587D1 (de) 2004-01-21 2010-10-28 Univ Emory Zusammensetzungen und verwendung von tyrosinkinase-hemmern zur behandlung von pathogenen infektionen
EP1751136B1 (en) * 2004-05-07 2014-07-02 Amgen Inc. Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer
WO2005115385A1 (en) 2004-05-24 2005-12-08 Ab Science Use of c-kit inhibitors for treating acne
WO2006017353A2 (en) 2004-07-13 2006-02-16 GOVERNMENT OF THE UNITED STATES, as represented byTHE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES Treatment of viral infections
CA2578122A1 (en) 2004-08-27 2006-03-02 Gpc Biotech Ag Pyrimidine derivatives
KR101325424B1 (ko) 2005-01-28 2013-11-04 노파르티스 아게 Ｔｉｅ-2 키나제 활성의 조절에 반응하는 질환의 치료를위한 피리미딜아미노벤즈아미드의 용도
MX2007011866A (es) 2005-02-25 2007-10-10 Novartis Ag Combinacion farmaceutica de inhibidores de bcr-abl y raf.
JP5129123B2 (ja) 2005-05-02 2013-01-23 ノバルティス アーゲー 全身性肥満細胞症の処置のためのピリミジルアミノベンズアミド誘導体の使用
SA06270147B1 (ar) 2005-06-09 2009-12-22 نوفارتيس ايه جي عملية لتخليق 5-(مثيل–1h–إيميدازول–1-يل )–3-(ثلاثي فلـورو مثيل)–بنزامـين
CA2615579A1 (en) 2005-07-20 2007-01-25 Novartis Ag Combination comprising a pyrimidylaminobenzamides and a flt-3 inhibitor for treating proliferative diseases
KR100674813B1 (ko) 2005-08-05 2007-01-29 일양약품주식회사 Ｎ-페닐-2-피리미딘-아민 유도체 및 그의 제조방법
CN101321532B (zh) 2005-12-06 2011-06-29 诺瓦提斯公司 用于治疗神经纤维瘤病的嘧啶基氨基苯甲酰胺衍生物
KR20120049397A (ko) * 2006-11-03 2012-05-16 노파르티스 아게 단백질 키나제 억제제로서의 화합물 및 조성물
TWI433677B (zh) * 2007-06-04 2014-04-11 Avila Therapeutics Inc 雜環化合物及其用途
CN105574346A (zh) * 2008-09-05 2016-05-11 新基阿维罗米克斯研究公司 多肽偶联物与不可逆抑制剂的设计方法和检测方法

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