JP5808826B2 - 複素環化合物およびその使用 - Google Patents

複素環化合物およびその使用 Download PDF

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JP5808826B2
JP5808826B2 JP2013555580A JP2013555580A JP5808826B2 JP 5808826 B2 JP5808826 B2 JP 5808826B2 JP 2013555580 A JP2013555580 A JP 2013555580A JP 2013555580 A JP2013555580 A JP 2013555580A JP 5808826 B2 JP5808826 B2 JP 5808826B2
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substituted
unsubstituted
alkyl
limited
heteroaryl
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JP2014506601A5 (enExample
JP2014506601A (ja
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ピンダ レン,
ピンダ レン,
イー リュー,
イー リュー,
リャンシェン リー,
リャンシェン リー,
カトリーナ チャン,
カトリーナ チャン,
トロイ エドワード ウィルソン,
トロイ エドワード ウィルソン,
サイモン フレイザー キャンベル,
サイモン フレイザー キャンベル,
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インテリカイン, エルエルシー
インテリカイン, エルエルシー
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    • C07ORGANIC CHEMISTRY
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    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
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    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
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  • Health & Medical Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2013555580A 2011-02-23 2012-02-23 複素環化合物およびその使用 Expired - Fee Related JP5808826B2 (ja)

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US201161445999P 2011-02-23 2011-02-23
US61/445,999 2011-02-23
PCT/US2012/026406 WO2012116237A2 (en) 2011-02-23 2012-02-23 Heterocyclic compounds and uses thereof

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JP2014506601A JP2014506601A (ja) 2014-03-17
JP2014506601A5 JP2014506601A5 (enExample) 2015-07-02
JP5808826B2 true JP5808826B2 (ja) 2015-11-10

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EP (1) EP2678016B1 (enExample)
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Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
CN104619709B (zh) 2012-07-13 2016-11-09 Ucb生物制药私人有限公司 作为tnf活性调节剂的咪唑并吡啶衍生物
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
WO2014072937A1 (en) 2012-11-08 2014-05-15 Rhizen Pharmaceuticals Sa Pharmaceutical compositions containing a pde4 inhibitor and a pi3 delta or dual pi3 delta-gamma kinase inhibitor
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
EP3105218B1 (en) 2014-02-13 2019-09-25 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
JP6602779B2 (ja) 2014-02-13 2019-11-06 インサイト・コーポレイション Lsd1阻害剤としてのシクロプロピルアミン類
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
CN105503877A (zh) 2014-09-24 2016-04-20 和记黄埔医药(上海)有限公司 咪唑并哒嗪类化合物及其用途
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP4406616A3 (en) 2014-11-06 2024-11-06 Bial-R&D Investments, S.A. Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders
US20170333435A1 (en) 2014-11-06 2017-11-23 Lysosomal Therapeutics Inc. Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
US20180185368A1 (en) 2014-11-06 2018-07-05 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
AU2015366202B2 (en) 2014-12-19 2020-01-02 Janssen Pharmaceutica Nv Heterocyclyl linked imidazopyridazine derivatives as PI3Kbeta inhibitors
KR20170095239A (ko) 2014-12-19 2017-08-22 얀센 파마슈티카 엔.브이. PI3Kβ 저해제로서의 이미다조피리다진 유도체
TWI699355B (zh) 2014-12-24 2020-07-21 美商基利科學股份有限公司 喹唑啉化合物
BR112017013440A2 (pt) 2014-12-24 2018-01-09 Gilead Sciences, Inc. compostos de isoquinolina para o tratamento de hiv
SG11201705192PA (en) 2014-12-24 2017-07-28 Gilead Sciences Inc Fused pyrimidine compounds for the treatment of hiv
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
EP3317278B1 (en) 2015-07-01 2021-04-14 Crinetics Pharmaceuticals, Inc. Somatostatin modulators and uses thereof
MY189367A (en) 2015-08-12 2022-02-08 Incyte Corp Salts of an lsd1 inhibitor
CN105130984B (zh) * 2015-09-23 2017-03-29 前湾医药科技(深圳)有限公司 一种咪唑并吡啶类化合物与在制备pi3k抑制剂中的应用
BR112018007068B1 (pt) 2015-10-09 2024-01-02 Janssen Pharmaceutica N.V. Derivados de quinoxalina e piridopirazina como inibidores de pi3kbeta, seu uso e composição farmacêutica que os compreende
KR102483020B1 (ko) 2016-03-28 2023-01-04 인사이트 코포레이션 Tam 저해제로서의 피롤로트리아진 화합물
EP3440081A4 (en) 2016-04-06 2019-09-18 Lysosomal Therapeutics Inc. PYRROLO [1,2-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER
CA3020305A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics Inc. Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
AU2017246455B2 (en) 2016-04-06 2021-09-30 Bial - R&D Investments, S.A. Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
TWI833686B (zh) 2016-04-22 2024-03-01 美商英塞特公司 Lsd1 抑制劑之調配物
WO2017192931A1 (en) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. SUBSTITUTED IMDAZO[1,2-α]PYRIDINES, SUBSTITUTED IMIDAZO[1,2-α]PYRAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
KR102530515B1 (ko) 2016-05-05 2023-05-09 비알 - 알&디 인베스트먼츠, 에스.에이. 치환된 이미다조[1,2-b]피리다진, 치환된 이미다조[1,5-b]피리다진, 관련 화합물, 및 의학적 장애의 치료에서의 그의 용도
HRP20210508T1 (hr) 2016-06-16 2021-05-28 Janssen Pharmaceutica Nv Biciklički derivati piridina, pirazina i pirimidina kao inhibitori pi3k beta
CA3025746A1 (en) 2016-06-16 2017-12-21 Janssen Pharmaceutica Nv Azabenzimidazole derivatives as pi3k beta inhibitors
EP4302834A3 (en) 2016-07-12 2024-07-17 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
US11352328B2 (en) 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
JP7240319B2 (ja) 2017-01-23 2023-03-15 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての二環式化合物
WO2018178280A1 (en) 2017-03-29 2018-10-04 Janssen Pharmaceutica Nv Quinoxaline and pyridopyrazine derivatives as pi3k-beta inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3658560A4 (en) 2017-07-25 2021-01-06 Crinetics Pharmaceuticals, Inc. SOMATOSTAT IN MODULATORS AND USES THEREOF
TW201930292A (zh) 2017-10-12 2019-08-01 美商銳新醫藥公司 作為變構shp2抑制劑的吡啶、吡嗪和三嗪化合物
CN107935918A (zh) * 2017-11-15 2018-04-20 山东潍坊润丰化工股份有限公司 一种百草枯的制备方法
JP7361693B2 (ja) 2017-12-15 2023-10-16 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての多環式化合物
TWI877770B (zh) 2018-02-27 2025-03-21 美商英塞特公司 作為a2a / a2b抑制劑之咪唑并嘧啶及三唑并嘧啶
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
EP3810610A1 (en) 2018-05-18 2021-04-28 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
CA3102279A1 (en) 2018-06-01 2019-12-05 Cornell University Combination therapy for pi3k-associated disease or disorder
WO2020010197A1 (en) 2018-07-05 2020-01-09 Incyte Corporation Fused pyrazine derivatives as a2a / a2b inhibitors
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US12590298B2 (en) 2019-10-18 2026-03-31 The Regents Of The University Of California Ex vivo tumor angiogenesis model
KR20220087497A (ko) 2019-10-18 2022-06-24 더 리전츠 오브 더 유니버시티 오브 캘리포니아 병원성 혈관을 표적화하기 위한 화합물 및 방법
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Fgfr阻害剤の誘導体
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
CR20230057A (es) 2020-07-02 2023-08-15 Incyte Corp Compuestos tríciclicos de urea como inhibidores de jak2 v617f
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
AR125273A1 (es) 2021-02-25 2023-07-05 Incyte Corp Lactamas espirocíclicas como inhibidores de jak2 v617f
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
AU2023235313A1 (en) 2022-03-17 2024-10-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
CA3259052A1 (en) * 2022-06-10 2023-12-14 Pikavation Therapeutics, Inc. HETEROCYCLIC COMPOUNDS USED AS PI3K.ALPHA INHIBITORS.
CN116425743B (zh) * 2022-12-30 2025-06-17 贵州医科大学 一种作为PI3Kα激酶抑制剂的苯并杂环类化合物及其制备方法与应用

Family Cites Families (193)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2313993A (en) 1939-02-04 1943-03-16 Chromogen Inc Organic sulphur and selenium compounds
GB1219606A (en) 1968-07-15 1971-01-20 Rech S Et D Applic Scient Soge Quinuclidinol derivatives and preparation thereof
US3657744A (en) 1970-05-08 1972-04-25 Univ Minnesota Method for fixing prosthetic implants in a living body
FR2102541A5 (enExample) 1970-08-07 1972-04-07 Aquitaine Total Organico
US4733665C2 (en) 1985-11-07 2002-01-29 Expandable Grafts Partnership Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5040548A (en) 1989-06-01 1991-08-20 Yock Paul G Angioplasty mehtod
US5350395A (en) 1986-04-15 1994-09-27 Yock Paul G Angioplasty apparatus facilitating rapid exchanges
US5061273A (en) 1989-06-01 1991-10-29 Yock Paul G Angioplasty apparatus facilitating rapid exchanges
US4748982A (en) 1987-01-06 1988-06-07 Advanced Cardiovascular Systems, Inc. Reinforced balloon dilatation catheter with slitted exchange sleeve and method
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
CA1322628C (en) 1988-10-04 1993-10-05 Richard A. Schatz Expandable intraluminal graft
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
GB8916480D0 (en) 1989-07-19 1989-09-06 Glaxo Group Ltd Chemical process
US5674278A (en) 1989-08-24 1997-10-07 Arterial Vascular Engineering, Inc. Endovascular support device
US6344053B1 (en) 1993-12-22 2002-02-05 Medtronic Ave, Inc. Endovascular support device and method
US5292331A (en) 1989-08-24 1994-03-08 Applied Vascular Engineering, Inc. Endovascular support device
GB8923590D0 (en) 1989-10-19 1989-12-06 Pfizer Ltd Antimuscarinic bronchodilators
US5395855A (en) 1990-05-07 1995-03-07 Ciba-Geigy Corporation Hydrazones
US5591762A (en) 1991-02-06 1997-01-07 Dr. Karl Thomae Gmbh Benzimidazoles useful as angiotensin-11 antagonists
PT100441A (pt) 1991-05-02 1993-09-30 Smithkline Beecham Corp Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso
US5480883A (en) 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5451700A (en) 1991-06-11 1995-09-19 Ciba-Geigy Corporation Amidino compounds, their manufacture and methods of treatment
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
JP3192424B2 (ja) 1992-04-02 2001-07-30 スミスクライン・ビーチャム・コーポレイション アレルギーまたは炎症疾患の治療用化合物
US5552438A (en) 1992-04-02 1996-09-03 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
JP3251587B2 (ja) 1992-04-02 2002-01-28 スミスクライン・ビーチャム・コーポレイション 炎症疾患の治療および腫瘍壊死因子の産生阻害に有用な化合物
TW225528B (enExample) 1992-04-03 1994-06-21 Ciba Geigy Ag
AU687727B2 (en) 1992-10-28 1998-03-05 Genentech Inc. Vascular endothelial cell growth factor antagonists
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
GB9414208D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
GB9414193D0 (en) 1994-07-14 1994-08-31 Glaxo Group Ltd Compounds
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
DE69536015D1 (de) 1995-03-30 2009-12-10 Pfizer Prod Inc Chinazolinone Derivate
ES2153031T4 (es) 1995-04-20 2001-05-16 Pfizer Derivados del acido arilsulfonil hidroxamico como inhibidores de mmp y tnf.
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
SI9620103A (sl) 1995-07-06 1998-10-31 Novartis Ag Pirolopirimidini in postopki za njihovo pripravo
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
EA001595B1 (ru) 1996-04-12 2001-06-25 Варнер-Ламберт Компани Необратимые ингибиторы тирозинкиназ
CA2258548C (en) 1996-06-24 2005-07-26 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
KR20000067904A (ko) 1996-07-18 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 매트릭스 메탈로프로테아제의 포스피네이트계 억제제
KR20000068248A (ko) 1996-08-23 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 아릴설포닐아미노 하이드록삼산 유도체
DE19638745C2 (de) 1996-09-11 2001-05-10 Schering Ag Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR)
EP0954315A2 (en) 1996-09-13 1999-11-10 Sugen, Inc. Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
TW528755B (en) 1996-12-24 2003-04-21 Glaxo Group Ltd 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives
JP3338064B2 (ja) 1997-01-06 2002-10-28 ファイザー・インク 環状スルホン誘導体
NZ336840A (en) 1997-02-03 2001-01-26 Pfizer Prod Inc Arylsulfonylamino hydroxamic acid derivatives useful in the treatment of tumor necrosis factor and matrix metalloproteinase mediated diseases
JP2000507975A (ja) 1997-02-07 2000-06-27 ファイザー・インク N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
EP0960098A1 (en) 1997-02-11 1999-12-01 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
CA2299355C (en) 1997-08-08 2005-09-27 Pfizer Products Inc. Aryloxyarylsulfonylamino hydroxamic acid derivatives
US6166037A (en) 1997-08-28 2000-12-26 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
WO1999016766A1 (en) 1997-10-01 1999-04-08 Kyowa Hakko Kogyo Co., Ltd. Benzodioxole derivatives
GB9723589D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723566D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9723590D0 (en) 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
YU44900A (sh) 1998-01-31 2003-01-31 Glaxo Group Limited Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola
AR017457A1 (es) 1998-02-14 2001-09-05 Glaxo Group Ltd Compuestos derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol, procesos para su preparacion, composiciones que los contienen y su uso en terapia para el tratamiento de enfermedades inflamatorias.
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
GB9813565D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
GB9813540D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
JP3933870B2 (ja) 1998-06-23 2007-06-20 グラクソ グループ リミテッド 2−(プリン−9−イル)−テトラヒドロフラン−3,4−ジオール誘導体
GB9813535D0 (en) 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
BR9815931A (pt) 1998-06-30 2001-02-20 Dow Chemical Co Polióis poliméricos, um processo para sua produção, e espuma de poliuretanoobtida
PT1107964E (pt) 1998-08-11 2010-06-11 Novartis Ag Derivados de isoquinolina com actividade inibidora da angiogénese
DE69932173T2 (de) 1998-10-16 2007-06-06 Pfizer Inc. Adeninderivate
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
DK1140173T4 (da) 1998-12-22 2013-06-10 Genentech Inc Vaskulære endothelcellevækstfaktorantagonister og anvendelser deraf
CN1660840A (zh) 1999-03-30 2005-08-31 诺瓦提斯公司 治疗炎性疾病的酞嗪衍生物
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
SK287418B6 (sk) 1999-05-04 2010-09-07 Schering Corporation Farmaceutický prípravok s obsahom CCR5 antagonistov a súprava s obsahom tohto prípravku
KR100439357B1 (ko) 1999-05-04 2004-07-07 쉐링 코포레이션 Ccr5 길항제로서 유용한 피페리딘 유도체
YU25500A (sh) 1999-05-11 2003-08-29 Pfizer Products Inc. Postupak za sintezu analoga nukleozida
GB9913932D0 (en) 1999-06-15 1999-08-18 Pfizer Ltd Purine derivatives
US6322771B1 (en) 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
CA2715683A1 (en) 1999-08-21 2001-03-01 Nycomed Gmbh Synergistic combination
CO5180581A1 (es) 1999-09-30 2002-07-30 Pfizer Prod Inc Compuestos para el tratamiento de la isquemia ciones farmaceuticas que los contienen para el tratamiento de la isquemia
GB9924361D0 (en) 1999-10-14 1999-12-15 Pfizer Ltd Purine derivatives
GB9924363D0 (en) 1999-10-14 1999-12-15 Pfizer Central Res Purine derivatives
GB0003960D0 (en) 2000-02-18 2000-04-12 Pfizer Ltd Purine derivatives
GEP20084317B (en) 2000-04-25 2008-02-25 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
TWI227240B (en) 2000-06-06 2005-02-01 Pfizer 2-aminocarbonyl-9H-purine derivatives
GB0015727D0 (en) 2000-06-27 2000-08-16 Pfizer Ltd Purine derivatives
KR100751981B1 (ko) 2000-06-27 2007-08-28 라보라토리오스 살바트, 에스.에이. 아릴알킬아민으로부터 유도된 카바메이트
GB0015876D0 (en) 2000-06-28 2000-08-23 Novartis Ag Organic compounds
DE10038639A1 (de) 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
SI1775305T1 (sl) 2000-08-05 2015-01-30 Glaxo Group Limited S-fluorometil ester 6alfa,9alfa-difluoro-17alfa-((2-furanilkarboksil)oksi)- 11beta-hidroksi-16alfa-metil-3-okso-androst-1,4-dien-17-karbotiojske kisline kot protivnetno sredstvo
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
GB0022695D0 (en) 2000-09-15 2000-11-01 Pfizer Ltd Purine Derivatives
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
DE60131015T2 (de) 2000-12-15 2008-07-10 Vertex Pharmaceuticals Inc., Cambridge Bakterielle gyrase-hemmer und deren verwendung
NZ526580A (en) 2000-12-22 2005-04-29 Almirall Prodesfarma Ag Quinuclidine carbamate derivatives and their use as M3 antagonists
DE60121813T2 (de) 2000-12-28 2007-09-20 Almirall Ag Neue chinuclidinderivate und medizinische zusammensetzungen, die diese verbindungen enthalten
EP1241176A1 (en) 2001-03-16 2002-09-18 Pfizer Products Inc. Purine derivatives for the treatment of ischemia
KR100831534B1 (ko) 2001-04-30 2008-05-22 글락소 그룹 리미티드 17.알파 위치에 시클릭 에스테르기를 지닌 항염증성의안드로스탄의 17.베타.-카르보티오에이트 에스테르 유도체
TWI238824B (en) 2001-05-14 2005-09-01 Novartis Ag 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives
WO2002096462A1 (en) 2001-05-25 2002-12-05 Pfizer Inc. An adenosine a2a receptor agonist and an anticholinergic agent in combination for treating obstructive airways diseases
ES2307751T3 (es) 2001-06-12 2008-12-01 Glaxo Group Limited Nuevos esteres heterociclicos centi-inflamatorios 17 alfa de derivados 17 beta de carbotioato de androstano.
DK2327765T3 (en) 2001-06-21 2015-07-13 Basf Enzymes Llc nitrilases
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
CN1571787A (zh) 2001-10-17 2005-01-26 Ucb公司 奎宁环衍生物、制备它们的方法和它们作为m2和/或m3毒蕈碱受体抑制剂的用途
GB0125259D0 (en) 2001-10-20 2001-12-12 Glaxo Group Ltd Novel compounds
AR037517A1 (es) 2001-11-05 2004-11-17 Novartis Ag Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria
AU2002356759A1 (en) 2001-12-01 2003-06-17 Glaxo Group Limited 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents
JP4505227B2 (ja) 2001-12-20 2010-07-21 キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ 1−アルキル−1−アゾニアビシクロ[2.2.2]オクタンカルバメート誘導体およびムスカリンレセプターアンタゴニストとしてのそれらの使用
AU2003202044A1 (en) 2002-01-15 2003-09-09 Glaxo Group Limited 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents
AU2003201693A1 (en) 2002-01-21 2003-09-02 Glaxo Group Limited Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents
GB0202216D0 (en) 2002-01-31 2002-03-20 Glaxo Group Ltd Novel compounds
WO2003082787A1 (en) 2002-03-26 2003-10-09 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
CA2478156C (en) 2002-03-26 2011-02-15 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
EP1496911B1 (en) 2002-04-10 2007-12-19 University Of Virginia Patent Foundation Use of a combination comprising a2a adenosine receptor agonists and anti-pathogenic agents for the treatment of inflammatory diseases
ES2206021B1 (es) 2002-04-16 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirrolidinio.
ES2201907B1 (es) 2002-05-29 2005-06-01 Almirall Prodesfarma, S.A. Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos.
DE10224888A1 (de) 2002-06-05 2003-12-24 Merck Patent Gmbh Pyridazinderivate
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10225574A1 (de) 2002-06-10 2003-12-18 Merck Patent Gmbh Aryloxime
DE10227269A1 (de) 2002-06-19 2004-01-08 Merck Patent Gmbh Thiazolderivate
ATE356808T1 (de) 2002-06-25 2007-04-15 Merck Frosst Canada Ltd 8-(biaryl)chinolin-pde4-inhibitoren
AU2003281219A1 (en) 2002-07-02 2004-01-23 Bernard Cote Di-aryl-substituted-ethane pyridone pde4 inhibitors
ES2204295B1 (es) 2002-07-02 2005-08-01 Almirall Prodesfarma, S.A. Nuevos derivados de quinuclidina-amida.
JP4503436B2 (ja) 2002-07-08 2010-07-14 ファイザー・プロダクツ・インク 糖質コルチコイド受容体のモジュレーター
PE20050130A1 (es) 2002-08-09 2005-03-29 Novartis Ag Compuestos organicos
US20060166995A1 (en) 2002-08-10 2006-07-27 Altana Pharma Ag Piperidine-n-oxide-derivatives
BR0313330A (pt) 2002-08-10 2005-06-14 Altana Pharma Ag Piperidina-ftalazonas substituìdas com pirrolidinadiona como inibidores de pde4
EP1556369A1 (en) 2002-08-10 2005-07-27 ALTANA Pharma AG Pyridazinone-derivatives as pde4 inhibitors
WO2004018449A1 (en) 2002-08-10 2004-03-04 Altana Pharma Ag Piperidine-derivatives as pde4 inhibitors
RS20050117A (sr) 2002-08-17 2007-06-04 Altana Pharma Ag., Novi benzonaftiridini
CA2495597A1 (en) 2002-08-17 2004-03-04 Altana Pharma Ag Novel phenanthridines
SE0202483D0 (sv) 2002-08-21 2002-08-21 Astrazeneca Ab Chemical compounds
EP1534675B1 (en) 2002-08-23 2009-02-25 Ranbaxy Laboratories, Ltd. Fluoro and sulphonylamino containing 3,6-disubstituted azabicyclo¬3.1.0 hexane derivatives as muscarinic receptor antagonists
ATE353217T1 (de) 2002-08-29 2007-02-15 Altana Pharma Ag 3-hydroxy-6-phenylphenanthridine als pde-4 inhibitoren
JP4587294B2 (ja) 2002-08-29 2010-11-24 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング Pde4インヒビターとしての2−ヒドロキシ−6−フェニルフェナントリジン
CA2497903A1 (en) 2002-09-18 2004-04-01 Ono Pharmaceutical Co., Ltd. Triazaspiro[5.5]undecane derivatives and drugs comprising the same as the active ingredient
JP2006096662A (ja) 2002-09-18 2006-04-13 Sumitomo Pharmaceut Co Ltd 新規6−置換ウラシル誘導体及びアレルギー性疾患の治療剤
JP2004107299A (ja) 2002-09-20 2004-04-08 Japan Energy Corp 新規1−置換ウラシル誘導体及びアレルギー性疾患の治療剤
DE10246374A1 (de) 2002-10-04 2004-04-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EA010408B1 (ru) 2002-10-23 2008-08-29 Гленмарк Фармасьютикалс Лтд. Трициклические соединения для лечения воспалительных и аллергических нарушений, способы их приготовления и содержащие их фармацевтические составы
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
DE10253220A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
DE10253282A1 (de) 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
DE10253426B4 (de) 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
EP1648455A4 (en) 2003-07-23 2009-03-04 Exelixis Inc MODULATORS OF ALK PROTEIN (ANAPLASTIC LYMPHOMA KINASE) AND METHODS OF USE
AR046845A1 (es) 2003-11-21 2005-12-28 Novartis Ag Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas
KR100629060B1 (ko) 2004-08-11 2006-09-26 주식회사 엘지화학 새로운 벤즈이미다졸계 화합물
EP2343303A1 (de) 2004-10-07 2011-07-13 Boehringer Ingelheim International GmbH PI3-Kinase Inhibitoren
CN101384586A (zh) 2006-02-14 2009-03-11 诺华公司 Pi-3激酶抑制剂及其应用方法
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
TWI498332B (zh) 2006-04-26 2015-09-01 Hoffmann La Roche 作為pi3k抑制劑之嘧啶衍生物及相關製備方法、醫藥組合物、用途、套組及產物
PL2057148T3 (pl) 2006-07-31 2010-06-30 Rottapharm Spa Amidynowe pochodne 2-heteroarylochinazolin i chinolin, silne środki przeciwbólowe i środki przeciwzapalne
EP2066653B1 (en) 2006-08-03 2012-09-12 Rottapharm S.p.A. 6-1h-imidazo-quinazoline and quinolines derivatives, new potent analgesics and anti-inflammatory agents
BRPI0716239A2 (pt) 2006-08-30 2013-08-13 Cellzome Ltd derivados de triazol como inibidores de cinase
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
EP2140492A1 (en) 2007-03-27 2010-01-06 Sandisk 3D LLC Memory cell comprising a carbon nanotube fabric element and a steering element and methods of forming the same
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
WO2008152394A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
TW200911798A (en) 2007-08-02 2009-03-16 Amgen Inc PI3 kinase modulators and methods of use
EP2217601A1 (en) 2007-11-08 2010-08-18 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyridazines for use as protein kinase inhibitors
AU2008328882A1 (en) 2007-11-27 2009-06-04 Cellzome Limited Amino triazoles as PI3K inhibitors
US8153813B2 (en) 2007-12-20 2012-04-10 Abbott Laboratories Benzothiazole and benzooxazole derivatives and methods of use
US8987280B2 (en) 2008-01-30 2015-03-24 Genentech, Inc. Pyrazolopyrimidine PI3K inhibitor compounds and methods of use
US20090192176A1 (en) 2008-01-30 2009-07-30 Wyeth 1H-PYRAZOLO[3,4-D]PYRIMIDINE, PURINE, 7H-PURIN-8(9H)-ONE, 3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE, AND THIENO[3,2-D]PYRIMIDINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES
WO2010008847A2 (en) 2008-06-24 2010-01-21 Takeda Pharmaceutical Company Limited Pi3k/m tor inhibitors
JP2011528337A (ja) * 2008-07-18 2011-11-17 サノフイ−アベンテイス 新規トリアゾロ[4,3−a]ピリジン誘導体、これらの調製方法、医薬としてのこれらの使用、医薬組成物および、特にmet阻害剤としての、新規使用
CA2738429C (en) * 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
US8476431B2 (en) * 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
PL2716157T3 (pl) 2008-12-08 2017-06-30 Gilead Connecticut, Inc. Imidazopirazynowe inhibitory Syk
JP2012521988A (ja) 2009-03-23 2012-09-20 シーメンス メディカル ソリューションズ ユーエスエー インコーポレイテッド 神経学的障害を検知するためのイメージング剤
EP2430013B1 (en) * 2009-05-13 2014-10-15 Amgen Inc. Heteroaryl compounds as pikk inhibitors
CN102459248A (zh) * 2009-05-26 2012-05-16 埃克塞里艾克西斯公司 作为PI3K/mTOR抑制剂的苯并氧杂环庚三烯以及它们使用与制造方法
NZ598220A (en) 2009-08-17 2014-02-28 Intellikine Llc Heterocyclic compounds and uses thereof
CN103153062B (zh) 2010-05-24 2015-07-15 因特利凯有限责任公司 杂环化合物及其用途
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof

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