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
Inventor
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
    • 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
    • A61K31/435—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
    • A—HUMAN NECESSITIES
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07D401/06—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
    • 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
    • C07D401/14—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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
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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
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/14—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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  • Engineering & Computer Science (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Psychiatry (AREA)
  • Obesity (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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Family Applications (1)

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

Country Status (6)

Country Link
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 (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8242271B2 (en) * 2007-06-04 2012-08-14 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
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
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 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
SG193859A1 (en) * 2008-09-05 2013-10-30 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
US9040715B2 (en) 2008-09-23 2015-05-26 Georgetown University 1,2-benzisothiazolinone and isoindolinone derivatives
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
JP6073677B2 (ja) 2009-06-12 2017-02-01 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 縮合複素環式化合物およびそれらの使用
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
WO2011008788A1 (en) * 2009-07-14 2011-01-20 Dawei Zhang Fluoro-substituted compounds as kinase inhibitors and methods of use thereof
PH12012500491A1 (en) * 2009-09-09 2018-03-21 Celgene Avilomics Res Inc P13 kinase inhibitors and uses thereof
SG179172A1 (en) * 2009-09-16 2012-04-27 Avila Therapeutics Inc Protein kinase conjugates and inhibitors
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
BR112012015721A2 (pt) 2009-12-30 2017-09-26 Avila Therapeutics Inc modificação covalente de proteínas dirigida por ligante
WO2012021444A1 (en) 2010-08-10 2012-02-16 Avila Therapeutics, Inc. Besylate salt of a btk inhibitor
TWI632134B (zh) 2010-11-01 2018-08-11 阿維拉製藥公司 雜環化合物及其用途
EP2635285B1 (en) 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
ES2665013T3 (es) 2010-11-10 2018-04-24 Celgene Car Llc Inhibidores de EGFR selectivos de mutante y usos de los mismos
WO2012151561A1 (en) 2011-05-04 2012-11-08 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
JP2014532658A (ja) 2011-10-28 2014-12-08 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 ブルトン型チロシンキナーゼ疾患または障害を治療する方法
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
RU2711077C9 (ru) 2012-03-15 2020-08-11 Селджен Кар Ллс Соли ингибитора киназы рецептора эпидермального фактора роста
CA2866852C (en) 2012-03-15 2020-12-29 Celgene Avilomics Research, Inc. Solid forms of an epidermal growth factor receptor kinase inhibitor
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
EP2909194A1 (en) 2012-10-18 2015-08-26 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
WO2014100748A1 (en) 2012-12-21 2014-06-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
EA201591051A1 (ru) 2013-02-08 2016-06-30 Селджен Авиломикс Рисерч, Инк. Ингибиторы erk и варианты их применения
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
DK3030561T3 (en) 2013-08-07 2017-03-27 Cadila Healthcare Ltd N-CYANOMETHYLAMIDES AS INHIBITORS OF JANUS KINASE
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
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
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
AU2015240535A1 (en) 2014-04-04 2016-10-20 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged 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
JP6854762B2 (ja) 2014-12-23 2021-04-07 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７（ｃｄｋ７）の阻害剤
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
WO2017030892A1 (en) 2015-08-14 2017-02-23 Reaction Biology Corp. Histone deacetylase inhibitors and methods for use thereof
AU2016319125B2 (en) 2015-09-09 2021-04-08 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2018049127A1 (en) * 2016-09-08 2018-03-15 Sabila Biosciences Llc 1,2-dithiolane compounds useful in neuroprotection, autoimmune and cancer diseases and conditions
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
WO2018234775A1 (en) 2017-06-20 2018-12-27 Mission Therapeutics Limited Substituted cyanopyrrolidines with activity as dub inhibitors
CN120398784A (zh) * 2018-06-07 2025-08-01 达萨玛治疗公司 Sarm1抑制剂
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
US12187701B2 (en) 2018-06-25 2025-01-07 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
CA3123215C (en) 2018-12-19 2024-04-02 Disarm Therapeutics, Inc. Inhibitors of sarm1 in combination with neuroprotective agents
US12281126B2 (en) 2018-12-28 2025-04-22 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
CN113950326B (zh) * 2019-06-06 2025-04-29 达萨玛治疗公司 Sarm1抑制剂
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
BR112022020058A2 (pt) 2020-04-08 2022-11-22 Mission Therapeutics Ltd N-cianopirrolidinas com atividade como inibidores de usp30
BR112022020644A2 (pt) 2020-05-28 2022-12-06 Mission Therapeutics Ltd Derivados de n-(1-ciano-pirrolidin-3-il)-5-(3-(trifluorometil)fenil) oxazol-2-carboxamida e os correspondentes derivados de oxadiazol como inibidores de usp30 para o tratamento de disfunção mitocondrial
MX2022015254A (es) 2020-06-04 2023-01-11 Mission Therapeutics Ltd N-cianopirrolidinas con actividad como inhibidores de peptidasa especifica de ubiquitina 30.
FI4161929T3 (fi) 2020-06-08 2025-07-30 Mission Therapeutics Ltd 1-(5-(2-syaanipyridin-4-yyli)oksatsoli-2-karbonyyli)-4-metyyliheksahydropyrrolo[3,4-b]pyrroli-5(1h)-karbonitriili usp30-inhibiittorina käytettäväksi mitokondrioiden toimintahäiriön, syövän ja fibroosin hoitamisessa
GB202016800D0 (en) 2020-10-22 2020-12-09 Mission Therapeutics Ltd Novel compounds
JP2024544660A (ja) 2021-12-01 2024-12-03 ミッション セラピューティクス リミティド Ｕｓｐ３０阻害剤としての活性を有する置換ｎ－シアノピロリジン
MA71541A (fr) * 2022-07-19 2025-05-30 Chiesi Farmaceutici S.P.A. Dérivés d'hétéroaryle en tant qu'inhibiteurs de ddr
GB202408928D0 (en) 2024-06-21 2024-08-07 Mission Therapeutics Ltd Novel compounds

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
AU2002315388A1 (en) * 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel phenylamino-pyrimidines and uses thereof
PL369259A1 (en) * 2001-11-01 2005-04-18 Janssen Pharmaceutica N.V. Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors)
ES2303565T3 (es) 2001-11-01 2008-08-16 Janssen Pharmaceutica Nv Derivados de aminobenzamida como inhibidores de la glucogeno sintasa cinasa 3beta.
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
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
US7279576B2 (en) * 2002-12-31 2007-10-09 Deciphera Pharmaceuticals, Llc Anti-cancer 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
PL1702917T3 (pl) * 2003-12-25 2018-02-28 Nippon Shinyaku Co., Ltd. Pochodna amidowa i lek
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
EP2233174B1 (en) 2004-01-21 2016-07-20 Emory University Compositions and use of tyrosine kinase inhibitors to treat pathogenic infection
AU2005245386B2 (en) * 2004-05-07 2008-11-27 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
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
CN101203224B (zh) 2005-01-28 2010-11-03 诺瓦提斯公司 嘧啶基氨基苯甲酰胺在制备治疗对Tie-2激酶活性的调节有响应的疾病的药物中的用途
US20080207658A1 (en) 2005-02-25 2008-08-28 Manley Paul W Pharmaceutical Combination of Bcr-Abl and Raf Inhibitors
WO2006119154A1 (en) 2005-05-02 2006-11-09 Novartis Ag Use of pyrimidylamimobenzamide derivatives for the treatment of systematic mastocytosis
SA06270147B1 (ar) 2005-06-09 2009-12-22 نوفارتيس ايه جي عملية لتخليق 5-(مثيل–1h–إيميدازول–1-يل )–3-(ثلاثي فلـورو مثيل)–بنزامـين
JP2009501766A (ja) 2005-07-20 2009-01-22 ノバルティス アクチエンゲゼルシャフト 増殖性疾患の処置のためのピリミジルアミノベンズアミドおよびＦｌｔ−３阻害剤を含む組合せ剤
KR100674813B1 (ko) 2005-08-05 2007-01-29 일양약품주식회사 Ｎ-페닐-2-피리미딘-아민 유도체 및 그의 제조방법
AU2006323992B2 (en) 2005-12-06 2010-07-08 Novartis Ag Pyrimidylaminobenzamide derivatives for the treatment of neurofibromatosis
AU2007317349B2 (en) * 2006-11-03 2011-10-20 Irm Llc Compounds and compositions as protein kinase inhibitors
US8242271B2 (en) * 2007-06-04 2012-08-14 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
SG193859A1 (en) * 2008-09-05 2013-10-30 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors

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