JP2015532287A - Ｉｒｅ１の調節 - Google Patents

Ｉｒｅ１の調節 Download PDF

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Publication number
JP2015532287A
JP2015532287A JP2015534672A JP2015534672A JP2015532287A JP 2015532287 A JP2015532287 A JP 2015532287A JP 2015534672 A JP2015534672 A JP 2015534672A JP 2015534672 A JP2015534672 A JP 2015534672A JP 2015532287 A JP2015532287 A JP 2015532287A
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Prior art keywords
substituted
unsubstituted
disease
ire1α
heteroaryl
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JP2015534672A
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Japanese (ja)
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JP2015532287A5 (cg-RX-API-DMAC7.html
Inventor
バッキーズ，ブラッドリー・ジェイ
マリー，ダスティン・ジェイ
オークス，スコット・エイ
パパ，フェロツ・アール
ペレラ，ガヤニ
ワン，リークン
Original Assignee
ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア
ユニバーシティ オブ ワシントン スルー イッツ センター フォー コマーシャリゼーション
ユニバーシティ オブ ワシントン スルー イッツ センター フォー コマーシャリゼーション
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Application filed by ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア, ユニバーシティ オブ ワシントン スルー イッツ センター フォー コマーシャリゼーション, ユニバーシティ オブ ワシントン スルー イッツ センター フォー コマーシャリゼーション filed Critical ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア
Publication of JP2015532287A publication Critical patent/JP2015532287A/ja
Publication of JP2015532287A5 publication Critical patent/JP2015532287A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2015534672A 2012-09-26 2013-09-26 Ｉｒｅ１の調節 Pending JP2015532287A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201261706037P 2012-09-26 2012-09-26
US61/706,037 2012-09-26
US201361783965P 2013-03-14 2013-03-14
US61/783,965 2013-03-14
US201361831088P 2013-06-04 2013-06-04
US61/831,088 2013-06-04
PCT/US2013/062039 WO2014052669A1 (en) 2012-09-26 2013-09-26 Modulation of ire1

Publications (2)

Publication Number Publication Date
JP2015532287A true JP2015532287A (ja) 2015-11-09
JP2015532287A5 JP2015532287A5 (cg-RX-API-DMAC7.html) 2016-12-08

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Family Applications (1)

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JP2015534672A Pending JP2015532287A (ja) 2012-09-26 2013-09-26 Ｉｒｅ１の調節

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US (3) US10131668B2 (cg-RX-API-DMAC7.html)
EP (1) EP2900673A4 (cg-RX-API-DMAC7.html)
JP (1) JP2015532287A (cg-RX-API-DMAC7.html)
KR (1) KR20150061651A (cg-RX-API-DMAC7.html)
CN (1) CN104995192A (cg-RX-API-DMAC7.html)
AU (1) AU2013323426A1 (cg-RX-API-DMAC7.html)
BR (1) BR112015006828A8 (cg-RX-API-DMAC7.html)
CA (1) CA2886240A1 (cg-RX-API-DMAC7.html)
IL (1) IL237970A0 (cg-RX-API-DMAC7.html)
MX (1) MX2015003874A (cg-RX-API-DMAC7.html)
RU (1) RU2015115631A (cg-RX-API-DMAC7.html)
SG (1) SG11201502331RA (cg-RX-API-DMAC7.html)
WO (1) WO2014052669A1 (cg-RX-API-DMAC7.html)

Cited By (8)

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JP2019510043A (ja) * 2016-03-28 2019-04-11 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｔａｍ阻害剤としてのピロロトリアジン化合物
JP2020532589A (ja) * 2017-09-01 2020-11-12 オプティキラ リミテッド ライアビリティ カンパニー Ｉｒｅ１阻害のための化合物および組成物
US11104682B2 (en) 2017-09-27 2021-08-31 Incyte Corporation Salts of TAM inhibitors
US11136326B2 (en) 2015-08-26 2021-10-05 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
US11241438B2 (en) 2018-06-29 2022-02-08 Incyte Corporation Formulations of an AXL/MER inhibitor
JP2022521784A (ja) * 2019-02-27 2022-04-12 オプティキラ リミテッド ライアビリティ カンパニー Ｉｒｅ１阻害のためのピラゾロピリジン化合物
JP2023100744A (ja) * 2017-11-10 2023-07-19 コーネル・ユニバーシティー 低分子ｉｒｅ１阻害剤
US12214036B2 (en) 2020-03-06 2025-02-04 Incyte Corporation Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20150061651A (ko) 2012-09-26 2015-06-04 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 Ire1의 조절
WO2015178770A1 (en) 2014-05-19 2015-11-26 Stichting Het Nederlands Kanker Instituut Compositions for cancer treatment
WO2016004254A1 (en) * 2014-07-01 2016-01-07 The Regents Of The University Of California Combined modulation of ire1
WO2017152117A1 (en) 2016-03-03 2017-09-08 Cornell University Small molecule ire1-alpha inhibitors
US10934275B2 (en) 2016-12-02 2021-03-02 Cornell University IRE1 small molecule inhibitors
CA3064837A1 (en) 2017-06-01 2018-12-06 Quentis Therapeutics, Inc. Ire1 small molecule inhibitors
US10392367B2 (en) 2017-06-01 2019-08-27 Quentis Therapeutics, Inc. IRE1 small molecule inhibitors
CN107446952B (zh) * 2017-07-31 2020-04-28 苏州大学附属儿童医院 一种用于肠外营养相关性肝病药物的制备方法
TWI831829B (zh) * 2018-09-12 2024-02-11 美商建南德克公司 苯氧基-吡啶基-嘧啶化合物及使用方法
US11945784B2 (en) 2018-12-03 2024-04-02 Cornell University IRE1 small molecule inhibitors
TWI748317B (zh) 2019-01-03 2021-12-01 美商建南德克公司 吡啶并－嘧啶酮與喋啶酮化合物及使用方法
WO2020176761A1 (en) * 2019-02-27 2020-09-03 Optikira, LLC Imidazolopyrazine compounds for ire1 inhibition
EP3938364B1 (en) * 2019-03-15 2023-08-23 Alterity Therapeutics Limited Compounds for and methods of treating diseases
US12479818B2 (en) 2019-05-15 2025-11-25 Cornell University Treatment of fibrosis with IRE1 small molecule inhibitors
CN112409361B (zh) * 2019-08-23 2022-08-16 山东轩竹医药科技有限公司 Tam抑制剂及其用途
WO2021041970A1 (en) * 2019-08-29 2021-03-04 Hibercell, Inc. Perk inhibiting imidazolopyrazine compounds
JP2023550053A (ja) * 2020-11-13 2023-11-30 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア Ｉｒｅ１アルファ阻害剤及びその使用
AU2022210355A1 (en) * 2021-01-22 2023-08-10 Cornell University Compositions and methods for the identification of compounds that protect against lipofuscin cytotoxicity
CN115969855B (zh) * 2022-12-15 2024-01-26 中国人民解放军空军军医大学 Apy29在制备rsk4激酶抑制剂中的用途

Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005506350A (ja) * 2001-10-18 2005-03-03 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン阻害薬としての１，４−二置換ベンゾ−縮合尿素化合物
JP2007509060A (ja) * 2003-10-15 2007-04-12 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド イミダゾピラジンチロシンキナーゼ阻害剤
WO2007064993A2 (en) * 2005-12-02 2007-06-07 Osi Pharmaceuticals, Inc. Bicyclic protein kinase inhibitors
JP2007531754A (ja) * 2004-04-02 2007-11-08 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド ６，６−二環置換されたヘテロ二環式タンパク質キナーゼ阻害剤
JP2008517890A (ja) * 2004-10-22 2008-05-29 キャンサー・リサーチ・テクノロジー・リミテッド 治療化合物としての、イミダゾ［４，５−ｂ］ピリジン−２−オンおよびオキサゾロ［４，５−ｂ］ピリジン−２−オン化合物ならびにそれらの類似体
JP2009530285A (ja) * 2006-03-13 2009-08-27 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド Ｅｇｆｒキナーゼ阻害剤およびｅｇｆｒキナーゼ阻害剤の効果に対し腫瘍細胞を感作する薬剤を用いる併用治療
JP2010526833A (ja) * 2007-05-09 2010-08-05 アボット・ラボラトリーズ タンパク質キナーゼ阻害薬としての縮合複素環化合物
JP2011520970A (ja) * 2008-05-19 2011-07-21 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド 置換されたイミダゾピラジン類およびイミダゾトリアジン類
WO2011094628A1 (en) * 2010-01-28 2011-08-04 University Of Washington Compositions and methods for treating toxoplasmosis. cryptosporidiosis and other apicomplexan protozoan related diseases
JP2012505916A (ja) * 2008-10-16 2012-03-08 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 融合環ヘテロアリールキナーゼ阻害剤
WO2013010380A1 (en) * 2011-07-19 2013-01-24 Merck Sharp & Dohme Corp. Btk inhibitors
WO2013010868A1 (en) * 2011-07-19 2013-01-24 Msd Oss B.V. 4 - imidazopyridazin- 1 -yl-benzamides and 4 - imidazotriazin- 1 - yl - benzamides as btk- inhibitors

Family Cites Families (347)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB812366A (en) 1955-08-18 1959-04-22 Wellcome Found Improvements in and relating to derivatives of pyrimidine and the preparation thereof
GB937725A (en) 1960-05-11 1963-09-25 Ciba Ltd Pyrazolo[3:4-d]pyrimidines
JPS5256693Y2 (cg-RX-API-DMAC7.html) 1973-05-14 1977-12-21
IT1153216B (it) 1981-10-16 1987-01-14 Schering Ag Procedimento per la preparazione di composti cianoeterociclici
DE3406533A1 (de) 1984-02-23 1985-08-29 Boehringer Mannheim Gmbh, 6800 Mannheim Verwendung von adenosin-derivaten als antiallergica und arzneimittel, die diese enthalten
US5310731A (en) 1984-06-28 1994-05-10 Whitby Research, Inc. N-6 substituted-5'-(N-substitutedcarboxamido)adenosines as cardiac vasodilators and antihypertensive agents
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
JPS61109797A (ja) 1984-11-01 1986-05-28 Yuki Gosei Yakuhin Kogyo Kk 標識化ヌクレオチドおよび標識化ポリヌクレオチド
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
US5010175A (en) 1988-05-02 1991-04-23 The Regents Of The University Of California General method for producing and selecting peptides with specific properties
WO1990003370A1 (en) 1988-09-28 1990-04-05 Microprobe Corporation DERIVATIVES OF PYRAZOLO[3,4-d]PYRIMIDINE
US5442039A (en) 1989-07-17 1995-08-15 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5428125A (en) 1989-07-17 1995-06-27 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5721356A (en) 1989-09-15 1998-02-24 Gensia, Inc. Orally active adenosine kinase inhibitors
US5646128A (en) 1989-09-15 1997-07-08 Gensia, Inc. Methods for treating adenosine kinase related conditions
US5795977A (en) 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
US5674998A (en) 1989-09-15 1997-10-07 Gensia Inc. C-4' modified adenosine kinase inhibitors
US5763596A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. C-4' modified adenosine kinase inhibitors
US5763597A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. Orally active adenosine kinase inhibitors
GB9009542D0 (en) 1990-04-27 1990-06-20 Beecham Group Plc Novel compounds
IE66205B1 (en) 1990-06-14 1995-12-13 Paul A Bartlett Polypeptide analogs
US5650489A (en) 1990-07-02 1997-07-22 The Arizona Board Of Regents Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof
GB9113137D0 (en) 1990-07-13 1991-08-07 Ici Plc Thioxo heterocycles
DE4026265A1 (de) 1990-08-20 1992-02-27 Boehringer Mannheim Gmbh Neue phospholipid-derivate von nucleosiden, deren herstellung sowie deren verwendung als antivirale arzneimittel
US5563257A (en) 1990-08-20 1996-10-08 Boehringer Mannheim Gmbh Phospholipid derivatives of nucleosides
US5561134A (en) 1990-09-25 1996-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
DK0550631T3 (da) 1990-09-25 1997-01-20 Rhone Poulenc Rorer Int Forbindelser med blodtrykssænkende virkning og virkning mod iskæmi
US5652366A (en) 1990-09-25 1997-07-29 Rhone-Poulenc Rorer Pharmaceuticals Inc. DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof
DK0495421T3 (da) 1991-01-15 1996-12-09 Alcon Lab Inc Anvendelse af carragenaner i topiske ophthalmiske sammensætninger
GB9103839D0 (en) 1991-02-23 1991-04-10 Smithkline Beecham Plc Pharmaceuticals
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
MX9300141A (es) 1992-01-13 1994-07-29 Smithkline Beecham Corp Compuestos de imidazol novedosos, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen.
US5916891A (en) 1992-01-13 1999-06-29 Smithkline Beecham Corporation Pyrimidinyl imidazoles
DE4204032A1 (de) 1992-02-12 1993-08-19 Boehringer Mannheim Gmbh Neue liponucleotide, deren herstellunmg sowie deren verwendung als antivirale arzneimittel
DE4204031A1 (de) 1992-02-12 1993-08-19 Boehringer Mannheim Gmbh Neue lipidphosphonsaeure-nucleosid-konjugate sowie deren verwendung als antivirale arzneimittel
WO1993018035A1 (en) 1992-03-04 1993-09-16 Abbott Laboratories Angiotensin ii receptor antagonists
JP2737518B2 (ja) 1992-03-16 1998-04-08 富士通株式会社 赤外線検知器の冷却構造
US5573905A (en) 1992-03-30 1996-11-12 The Scripps Research Institute Encoded combinatorial chemical libraries
GB9208135D0 (en) 1992-04-13 1992-05-27 Ludwig Inst Cancer Res Polypeptides having kinase activity,their preparation and use
WO1993022443A1 (en) 1992-04-24 1993-11-11 Sri International In vivo homologous sequence targeting in eukaryotic cells
KR100271083B1 (ko) 1992-06-19 2000-11-01 데이비드 에스. 호이리스 열전 온도 안정화를 갖는 적외선 카메라(Infrared Camera with Thermoelectric Temperature Stabilization)
US6057305A (en) 1992-08-05 2000-05-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiretroviral enantiomeric nucleotide analogs
US5288514A (en) 1992-09-14 1994-02-22 The Regents Of The University Of California Solid phase and combinatorial synthesis of benzodiazepine compounds on a solid support
TW370529B (en) 1992-12-17 1999-09-21 Pfizer Pyrazolopyrimidines
IL108523A0 (en) 1993-02-03 1994-05-30 Gensia Inc Pharmaceutical compositions containing adenosine kinase inhibitors for preventing or treating conditions involving inflammatory responses and pain
AU673055B2 (en) 1993-02-03 1996-10-24 Gensia, Inc. Adenosine kinase inhibitors comprising lyxofuranosyl derivatives
US5679683A (en) 1994-01-25 1997-10-21 Warner-Lambert Company Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5593853A (en) 1994-02-09 1997-01-14 Martek Corporation Generation and screening of synthetic drug libraries
US5539083A (en) 1994-02-23 1996-07-23 Isis Pharmaceuticals, Inc. Peptide nucleic acid combinatorial libraries and improved methods of synthesis
US6632789B1 (en) 1994-04-29 2003-10-14 The United States Of America As Represented By The Secretary Of The Navy Methods for modulating T cell responses by manipulating intracellular signal transduction
DE4418690A1 (de) 1994-05-28 1996-01-11 Boehringer Mannheim Gmbh Neue Lipidester von Nucleosid-Monophosphaten und deren Verwendung als immunsuppressive Arzneimittel
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
NZ293249A (en) 1994-09-29 1999-04-29 Novartis Ag 4-amino-5,7-diaryl-pyrrolo[2,3-d]pyrimidines and their use
US6323201B1 (en) 1994-12-29 2001-11-27 The Regents Of The University Of California Compounds for inhibition of ceramide-mediated signal transduction
US6312894B1 (en) 1995-04-03 2001-11-06 Epoch Pharmaceuticals, Inc. Hybridization and mismatch discrimination using oligonucleotides conjugated to minor groove binders
DK0819129T3 (da) 1995-04-03 2000-10-23 Novartis Ag Pyrazolderivater og fremgangsmåde til deres fremstilling
US5977061A (en) 1995-04-21 1999-11-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic N6 - substituted nucleotide analagues and their use
JPH08295667A (ja) 1995-04-27 1996-11-12 Takeda Chem Ind Ltd 複素環化合物、その製造法および剤
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
WO1996037777A1 (en) 1995-05-23 1996-11-28 Nelson Randall W Mass spectrometric immunoassay
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
CZ297975B6 (cs) 1995-06-07 2007-05-09 G. D. Searle & Co. Farmaceutická kombinace antagonisty receptoru proangiotensin II a epoxymexrenonu pro lécení kardiovaskulárních poruch
WO1996040256A1 (en) 1995-06-07 1996-12-19 G.D. Searle & Co. Method to treat cardiofibrosis with a combination of an angiotensin ii antagonist and spironolactone
US5665721A (en) 1995-06-07 1997-09-09 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
DE69620756T2 (de) 1995-06-07 2002-11-14 G.D. Searle & Co., Chicago Kombinationstherapie zur behandlung des kongestiven herzversagens mit spironolacton und angiotensin ii-antagonist
ATE483733T1 (de) 1995-06-14 2010-10-15 Univ California Hochaffine humane antikörper gegen tumorantigene
US5763885A (en) 1995-12-19 1998-06-09 Loral Infrared & Imaging Systems, Inc. Method and apparatus for thermal gradient stabilization of microbolometer focal plane arrays
GB9521987D0 (en) 1995-10-26 1996-01-03 Ludwig Inst Cancer Res Phosphoinositide 3-kinase modulators
JPH09143163A (ja) 1995-11-29 1997-06-03 Fuji Photo Film Co Ltd 含窒素ヘテロ芳香族アミド類の製造方法
US5747235A (en) 1996-01-26 1998-05-05 Eastman Kodak Company Silver halide light sensitive emulsion layer having enhanced photographic sensitivity
DE19603576A1 (de) 1996-02-01 1997-08-07 Bayer Ag Acylierte 4-Amino und 4-Hydrazinopyrimidine
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
US5914488A (en) 1996-03-05 1999-06-22 Mitsubishi Denki Kabushiki Kaisha Infrared detector
GB9611460D0 (en) 1996-06-01 1996-08-07 Ludwig Inst Cancer Res Novel lipid kinase
KR20000022040A (ko) 1996-06-20 2000-04-25 보오드 오브 리젠츠, 더 유니버시티 오브 텍사스 시스템 약학적 활성 제제를 제공하기 위한 화합물, 방법 및 그의 용도
US6251901B1 (en) 1996-10-23 2001-06-26 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US6342514B1 (en) 1996-10-23 2002-01-29 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5919808A (en) 1996-10-23 1999-07-06 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5922753A (en) 1996-10-23 1999-07-13 Zymogenetics, Inc. Methods for treating bone deficit conditions with benzothiazole
US5994358A (en) 1996-10-23 1999-11-30 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US6153631A (en) 1996-10-23 2000-11-28 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5948776A (en) 1996-10-23 1999-09-07 Zymogenetic, Inc. Compositions and methods for treating bone deficit conditions
US5990169A (en) 1996-10-23 1999-11-23 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5965573A (en) 1996-10-23 1999-10-12 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5858753A (en) 1996-11-25 1999-01-12 Icos Corporation Lipid kinase
JP4094066B2 (ja) 1996-12-06 2008-06-04 バーテックス ファーマシューティカルズ インコーポレイテッド インターロイキン−１β変換酵素のインヒビター
US6093737A (en) 1996-12-30 2000-07-25 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JPH10206995A (ja) 1997-01-21 1998-08-07 Konica Corp ハロゲン化銀写真感光材料
DE69825066T2 (de) 1997-02-07 2005-08-25 Princeton University Gentechnisch hergestellte Proteinkinasen, welche modifizierte Nukleotidtriphosphatsubstrate verwenden können
EP0970084B1 (en) 1997-03-19 2003-06-04 Basf Aktiengesellschaft Pyrrolo 2,3d]pyrimidines and their use as tyrosine kinase inhibitors
US7863444B2 (en) 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
EP0983768A1 (en) 1997-05-23 2000-03-08 Nippon Shinyaku Co., Ltd. Medicinal composition for prevention or treatment of hepatopathy
US6207679B1 (en) 1997-06-19 2001-03-27 Sepracor, Inc. Antimicrobial agents uses and compositions related thereto
EP1020445B1 (en) 1997-10-02 2008-08-13 Eisai R&D Management Co., Ltd. Fused pyridine derivatives
US6649631B1 (en) 1997-10-23 2003-11-18 The Board Of Regents Of The University Of Texas System Compositions and methods for treating bone deficit conditions
CA2309350C (en) 1997-11-12 2007-04-03 Mitsubishi Chemical Corporation Purine derivatives and medicaments comprising the same as active ingredient
US6191170B1 (en) 1998-01-13 2001-02-20 Tularik Inc. Benzenesulfonamides and benzamides as therapeutic agents
US7715989B2 (en) 1998-04-03 2010-05-11 Elitech Holding B.V. Systems and methods for predicting oligonucleotide melting temperature (TmS)
US6127121A (en) 1998-04-03 2000-10-03 Epoch Pharmaceuticals, Inc. Oligonucleotides containing pyrazolo[3,4-D]pyrimidines for hybridization and mismatch discrimination
JP2000072773A (ja) 1998-08-28 2000-03-07 Zeria Pharmaceut Co Ltd プリン誘導体
US6713474B2 (en) 1998-09-18 2004-03-30 Abbott Gmbh & Co. Kg Pyrrolopyrimidines as therapeutic agents
HUP0200403A3 (en) 1998-09-18 2004-07-28 Abbott Gmbh & Co Kg Pyrrolopyrimidines as protein kinase inhibitors, pharmaceutical compositions containing them and their use
DE69928414T2 (de) 1998-09-18 2006-08-03 Abbott Gmbh & Co. Kg 4-aminopyrrolopyrimidine als kinaseinhibitoren
EP1140938B1 (en) 1999-01-11 2003-08-27 Princeton University High affinity inhibitors for target validation and uses thereof
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
EP1040831A3 (en) 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
SE515856C2 (sv) 1999-05-19 2001-10-22 Ericsson Telefon Ab L M Bärare för elektronikkomponenter
IL146474A0 (en) 1999-06-03 2002-07-25 Knoll Gmbh Benzothiazinone and benzoxazinone compounds
US6387894B1 (en) 1999-06-11 2002-05-14 Pfizer Inc. Use of CRF antagonists and renin-angiotensin system inhibitors
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB9919588D0 (en) 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
AU7080500A (en) 1999-08-27 2001-03-26 Chemocentryx, Inc. Compounds and methods for modulating cxcr3 function
CA2385736C (en) 1999-09-16 2011-11-15 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
JP2003509428A (ja) 1999-09-17 2003-03-11 アボツト・ゲー・エム・ベー・ハー・ウント・コンパニー・カーゲー 治療薬としてのピラゾロピリミジン
DE60014130T2 (de) 1999-10-06 2006-03-09 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Heterocyclische verbindungen verwendbar als tyrosinkinase inhibitoren
US6506769B2 (en) 1999-10-06 2003-01-14 Boehringer Ingelheim Pharmaceuticals, Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
US6472153B1 (en) 1999-10-26 2002-10-29 Epoch Biosciences, Inc. Hybridization-triggered fluorescent detection of nucleic acids
JP2001151635A (ja) 1999-11-19 2001-06-05 Lion Corp 水中油型乳化皮膚外用剤
US6660845B1 (en) 1999-11-23 2003-12-09 Epoch Biosciences, Inc. Non-aggregating, non-quenching oligomers comprising nucleotide analogues; methods of synthesis and use thereof
GB0002032D0 (en) 2000-01-28 2000-03-22 Zeneca Ltd Chemical compounds
US7217722B2 (en) 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
WO2001072751A1 (en) 2000-03-29 2001-10-04 Knoll Gesellschaft Mit Beschraenkter Haftung Pyrrolopyrimidines as tyrosine kinase inhibitors
HK1053844A1 (zh) 2000-03-29 2003-11-07 Knoll Gmbh 鉴定tie-2抑制剂的方法
US7115653B2 (en) 2000-03-30 2006-10-03 Curis, Inc. Small organic molecule regulators of cell proliferation
US6613798B1 (en) 2000-03-30 2003-09-02 Curis, Inc. Small organic molecule regulators of cell proliferation
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
SI3029041T1 (sl) 2000-04-25 2020-08-31 Icos Corporation Inhibitorji humane delta fosfatidil-inozitol 3-kinaze
JP2002037787A (ja) 2000-05-16 2002-02-06 Kyowa Hakko Kogyo Co Ltd ［１，２，４］トリアゾロ［１，５−ｃ］ピリミジン誘導体の製造法
WO2001091699A2 (en) 2000-05-30 2001-12-06 Advanced Research & Technology Institute Compositions and methods for identifying agents which modulate pten function and pi-3 kinase pathways
US6849713B2 (en) 2000-06-27 2005-02-01 Genelabs Technologies, Inc. Compounds possessing antibacterial, antifungal or antitumor activity
US6534691B2 (en) 2000-07-18 2003-03-18 E. I. Du Pont De Nemours And Company Manufacturing process for α-olefins
WO2002030944A2 (en) 2000-10-11 2002-04-18 Applera Corporation Fluorescent nucleobase conjugates having anionic linkers
WO2002030358A2 (en) 2000-10-11 2002-04-18 Tularik Inc. Modulation of ccr4 function
JP2002131859A (ja) 2000-10-19 2002-05-09 Konica Corp 撮影用赤外感光性ハロゲン化銀写真感光材料及び赤外感光性ハロゲン化銀乳剤
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
CN1575177A (zh) 2000-12-11 2005-02-02 图拉里克公司 Cxcr3拮抗剂
CA2430978C (en) 2000-12-28 2012-05-15 Daiichi Pharmaceutical Co., Ltd. Vla-4 inhibitors
BR0206614A (pt) 2001-01-22 2004-02-17 Merck & Co Inc Composto, composição farmacêutica, método para inibir a polimerase viral de rna dependente de rna e/ou inibir a replicação viral de rna dependente de rna, método para tratar uma infecção viral de rna dependente de rna, e, uso de um composto
US7105499B2 (en) 2001-01-22 2006-09-12 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
CA2439263C (en) 2001-03-02 2012-10-23 Frank Becker Three hybrid assay system
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
US7250569B2 (en) 2001-04-26 2007-07-31 New York University School Of Medicine Method for dissolving nanostructural materials
US6664269B2 (en) 2001-05-08 2003-12-16 Maybridge Plc Isoquinolinone derivatives
WO2002094264A1 (en) 2001-05-23 2002-11-28 Tularik Inc. Ccr4 antagonists
CA2450628A1 (en) 2001-06-13 2002-12-19 Genesoft Pharmaceuticals, Inc. Benzothiophene compounds having antiinfective activity
WO2002100832A1 (en) 2001-06-13 2002-12-19 Genesoft Pharmaceuticals, Inc. Isoquinoline compounds having antiinfective activity
US20030236198A1 (en) 2001-06-13 2003-12-25 Genesoft, Inc. Antipathogenic benzamide compounds
US20030114467A1 (en) 2001-06-21 2003-06-19 Shakespeare William C. Novel pyrazolo- and pyrrolo-pyrimidines and uses thereof
AU2002355732B2 (en) 2001-08-01 2006-11-09 Merck Sharp & Dohme Corp. Benzimidazo[4,5-f]isoquinolinone derivatives
AU2002327422A1 (en) 2001-08-03 2003-03-18 Abbott Laboratories Method of identifying inhibitors of lck
ES2572030T3 (es) 2001-08-10 2017-07-19 Shionogi & Co., Ltd. Agente antiviral
JP2003073357A (ja) 2001-09-03 2003-03-12 Mitsubishi Pharma Corp アミド化合物を含有するＲｈｏキナーゼ阻害剤
WO2003024969A1 (en) 2001-09-14 2003-03-27 Merck & Co., Inc. Tyrosine kinase inhibitors
AU2002368274A1 (en) 2001-09-13 2004-06-03 Genesoft, Inc. Methods of treating infection by drug resistant bacteria
AUPR769501A0 (en) 2001-09-14 2001-10-11 Biomolecular Research Institute Limited Cytokine receptor 1
TWI330183B (cg-RX-API-DMAC7.html) 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
US7319858B2 (en) 2001-11-16 2008-01-15 Cingular Wireless Ii, Llc System and method for querying message information
WO2003048081A2 (en) 2001-12-04 2003-06-12 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
CA2469435A1 (en) 2001-12-21 2003-07-24 X-Ceptor Therapeutics, Inc. Modulators of lxr
JP4085237B2 (ja) 2001-12-21 2008-05-14 日本電気株式会社 携帯電話の利用契約システムと通信方法
AU2002364209A1 (en) 2001-12-26 2003-07-24 Genelabs Technologies, Inc. Polyamide derivatives possessing antibacterial, antifungal or antitumor activity
US7414036B2 (en) 2002-01-25 2008-08-19 Muscagen Limited Compounds useful as A3 adenosine receptor agonists
WO2003082341A1 (en) 2002-03-22 2003-10-09 Cellular Genomics, Inc. AN IMPROVED FORMULATION OF CERTAIN PYRAZOLO[3,4-d] PYRIMIDINES AS KINASE MODULATORS
US8247424B2 (en) 2002-03-26 2012-08-21 Zentopharm Gmbh Fredericamycin derivatives
US7166293B2 (en) 2002-03-29 2007-01-23 Carlsbad Technology, Inc. Angiogenesis inhibitors
DE10217046A1 (de) 2002-04-17 2003-11-06 Bioleads Gmbh Fredericamycin-Derivate
JP2005529889A (ja) 2002-04-26 2005-10-06 ファイザー・プロダクツ・インク ピリミジン−２，４，６−トリオンメタロ−プロテイナーゼ阻害剤
US6794562B2 (en) 2002-05-01 2004-09-21 Stine Seed Farm, Inc. Soybean cultivar 0332143
EP1517904A4 (en) 2002-05-23 2007-02-21 Merck & Co Inc INHIBITORS OF MITOTIC KINESINE
JP2005538062A (ja) 2002-06-14 2005-12-15 サイトキネティクス・インコーポレーテッド 化合物、組成物、および方法
US7265111B2 (en) 2002-06-27 2007-09-04 Sanofi-Aventis Deutschland Gmbh Adenosine analogues and their use as pharmaceutical agents
KR101124245B1 (ko) 2002-06-27 2012-07-02 노보 노르디스크 에이/에스 치료제로서 아릴 카르보닐 유도체
PL215132B1 (pl) 2002-06-27 2013-10-31 Novo Nordisk As Pochodna arylokarbonylowa jako srodek terapeutyczny, jej zastosowanie i kompozycja farmaceutyczna ja zawierajaca
DE10230917A1 (de) 2002-07-09 2004-02-05 Bioleads Gmbh Fredericamycin-Derivate
AU2003249244A1 (en) 2002-07-15 2004-02-02 Combinatorx, Incorporated Methods for the treatment of neoplasms
CA2494048A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc 4-hydroxyquinoline derivatives as matrix metalloproteinase inhibitors
JP4646626B2 (ja) 2002-08-16 2011-03-09 アストラゼネカ アクチボラグ ホスホイノシチド３−キナーゼβの阻害
JP2005536553A (ja) 2002-08-21 2005-12-02 サイトキネティクス・インコーポレーテッド 化合物、組成物および方法
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
EP1572944A4 (en) 2002-08-30 2007-12-26 Harvard College METHOD AND COMPOSITIONS FOR MODULATING THE ACTIVITY OF XBP-1
AU2003270489A1 (en) * 2002-09-09 2004-03-29 Cellular Genomics, Inc. 6-ARYL-IMIDAZO(1,2-a)PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
AU2003266668A1 (en) 2002-09-30 2004-04-23 Banyu Pharmaceutical Co., Ltd. 2-aminobenzimidazole derivative
JP2004161716A (ja) 2002-11-15 2004-06-10 Takeda Chem Ind Ltd Ｊｎｋ阻害剤
UA80171C2 (en) 2002-12-19 2007-08-27 Pfizer Prod Inc Pyrrolopyrimidine derivatives
AU2003301020A1 (en) 2002-12-20 2004-07-22 Sankyo Company, Limited Isoquinolinone derivatives and their use as therapeutic agents
US7071355B2 (en) 2002-12-23 2006-07-04 4 Sc Ag Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
US7365094B2 (en) 2002-12-23 2008-04-29 4Sc Ag Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
US7247736B2 (en) 2002-12-23 2007-07-24 4Sc Ag Method of identifying inhibitors of DHODH
US20060135790A1 (en) 2003-03-06 2006-06-22 Hyett David J Process for the preparation of an alpha-amino carbonyl compound
US7550590B2 (en) 2003-03-25 2009-06-23 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
GB0306907D0 (en) 2003-03-26 2003-04-30 Angiogene Pharm Ltd Boireductively-activated prodrugs
WO2004103270A2 (en) 2003-04-02 2004-12-02 Suntory Pharmaceutical Research Laboratories Llc Compounds and methods for treatment of thrombosis
WO2004100868A2 (en) 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
WO2004111014A1 (en) 2003-06-06 2004-12-23 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
US7429596B2 (en) 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
WO2005002585A1 (en) 2003-07-02 2005-01-13 Warner-Lambert Company Llc Combination of an allosteric inhibitor of matrix metalloproteinase-13 and a ligand to an alpha-2-delta receptor
GB0317951D0 (en) 2003-07-31 2003-09-03 Trigen Ltd Compounds
WO2005014534A1 (en) 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
US20050054614A1 (en) 2003-08-14 2005-03-10 Diacovo Thomas G. Methods of inhibiting leukocyte accumulation
US20050043239A1 (en) 2003-08-14 2005-02-24 Jason Douangpanya Methods of inhibiting immune responses stimulated by an endogenous factor
EP1656378A4 (en) 2003-08-15 2011-05-11 Irm Llc COMPOUNDS AND COMPOSITIONS INHIBITING TYROSINE KINASE RECEPTOR ACTIVITY
US7390820B2 (en) 2003-08-25 2008-06-24 Amgen Inc. Substituted quinolinone derivatives and methods of use
WO2005044181A2 (en) 2003-09-09 2005-05-19 Temple University-Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
GB0322409D0 (en) 2003-09-25 2003-10-29 Astrazeneca Ab Quinazoline derivatives
AU2004289303A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
JP2007511596A (ja) 2003-11-17 2007-05-10 ファイザー・プロダクツ・インク 癌の治療において有用なピロロピリミジン化合物
WO2005061460A1 (en) 2003-12-08 2005-07-07 Cytokinetics, Inc. Compounds, compositions, and methods
EP1715871A1 (en) 2003-12-22 2006-11-02 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
ATE457313T1 (de) 2003-12-23 2010-02-15 Novartis Ag Bicyclische heterocyclische p-38-kinase- inhibitoren
CA2552664A1 (en) 2004-01-08 2005-07-28 Michigan State University Methods for treating and preventing hypertension and hypertension-related disorders
WO2005074603A2 (en) 2004-02-03 2005-08-18 Abbott Laboratories Aminobenzoxazoles as therapeutic agents
UA83416C2 (en) 2004-02-13 2008-07-10 Баниу Фармасьютикал Ко., Лтд. Fused ring 4-oxopyrimidine derivative
US20050187418A1 (en) 2004-02-19 2005-08-25 Small Brooke L. Olefin oligomerization
JP2007523202A (ja) 2004-02-24 2007-08-16 ビオアクソン・テラプティーク・インコーポレーテッド ４置換ピペリジン誘導体
CA2557575A1 (en) 2004-02-27 2005-09-15 F. Hoffmann-La Roche Ag Fused derivatives of pyrazole
TW200538453A (en) 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
AU2005238386A1 (en) 2004-04-30 2005-11-10 Takeda Pharmaceutical Company Limited Heterocyclic amide compound and use thereof as an MMP-13 inhibitor
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
WO2005113556A1 (en) 2004-05-13 2005-12-01 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
CA2566436C (en) 2004-05-13 2011-05-10 Vanderbilt University Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis
WO2005117889A1 (en) 2004-05-25 2005-12-15 Icos Corporation Methods for treating and/or preventing aberrant proliferation of hematopoietic
JP4842929B2 (ja) 2004-05-27 2011-12-21 ファイザー・プロダクツ・インク 癌治療に有用なピロロピリミジン誘導体
CA2569406A1 (en) 2004-06-04 2005-12-22 Icos Corporation Methods for treating mast cell disorders
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006038865A1 (en) 2004-10-01 2006-04-13 Betagenon Ab Nucleotide derivatives for the treatment of type 2 diabetes and other disorders
US8212012B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues having modified sugar moieties
US7608594B2 (en) 2004-11-03 2009-10-27 University Of Kansas Novobiocin analogues as anticancer agents
US8212011B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues
US7622451B2 (en) 2004-11-03 2009-11-24 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
WO2006068760A2 (en) 2004-11-19 2006-06-29 The Regents Of The University Of California Anti-inflammatory pyrazolopyrimidines
EP1817025A2 (en) 2004-11-23 2007-08-15 PTC Therapeutics, Inc. Tetrahydrocarbazoles as active agents for inhibiting vegf production by translational control
US20060156485A1 (en) 2005-01-14 2006-07-20 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
US20080287469A1 (en) 2005-02-17 2008-11-20 Diacovo Thomas G Phosphoinositide 3-Kinase Inhibitors for Inhibiting Leukocyte Accumulation
WO2006091897A2 (en) 2005-02-25 2006-08-31 Adenosine Therapeutics, Llc Derivatives of 8-substituted xanthines
US20090124654A1 (en) 2005-03-01 2009-05-14 Mjalli Adnan M M Aryl and Heteroaryl Compounds, Compositions, Methods of Use
WO2006102079A1 (en) 2005-03-17 2006-09-28 Novartis Ag N- [3- (1-amin0-5, 6, 7, 8-tetrahydro-2 , 4, 4b-triazafluoren-9-yl)-phenyl] benzamides as tyrosine/threonine kinase inhibitors, in particular b-raf kinase
MX2007012449A (es) 2005-04-06 2007-12-05 Irm Llc Compuestos y composiciones que contienen diaril-amina, y su uso como moduladores de los receptores nucleares de hormonas esteroideas.
KR100781704B1 (ko) 2005-04-20 2007-12-03 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
CA2606399A1 (en) 2005-04-25 2006-11-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Scienc Es Of The Czech Republic Use of compounds to enhance processivity of telomerase
EP1874769B1 (de) 2005-04-25 2011-09-14 Merck Patent GmbH Neuartige aza-heterozyklen als kinase-inhibitoren
PL1906965T3 (pl) 2005-06-22 2015-10-30 Chemocentryx Inc Związki azaindazolowe i sposoby zastosowania
CA2612585A1 (en) 2005-06-27 2007-01-04 Amgen Inc. Anti-inflammatory aryl nitrile compounds
BRPI0615522A2 (pt) 2005-07-11 2012-04-10 Devgen Nv derivados da amida como inibidores da quinase
JP2009505948A (ja) 2005-07-11 2009-02-12 デブジェン エヌブイ キナーゼ阻害剤としてのアミド誘導体
GB0516723D0 (en) 2005-08-15 2005-09-21 Novartis Ag Organic compounds
JP2009506006A (ja) 2005-08-25 2009-02-12 エフ．ホフマン−ラ ロシュ アーゲー ｐ３８ＭＡＰキナーゼ阻害剤およびその使用方法
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
EP1919873A1 (de) 2005-09-01 2008-05-14 BioAgency AG Fredericamycin-derivate
JP2009510066A (ja) 2005-09-29 2009-03-12 ワイス 血管運動症状（ｖｍｓ）の治療のためのモノアミン再取り込みのモジュレータである１−（１ｈ−インドール−１−イル）−３−（メチルアミノ）−１−フェニルプロパン−２−オール誘導体および関連の化合物
CN102936250B (zh) 2005-11-17 2014-07-09 Osi医药有限责任公司 稠合双环mTOR抑制剂
AU2006316321A1 (en) 2005-11-22 2007-05-31 Merck & Co., Inc. Indole orexin receptor antagonists
WO2007066189A2 (en) 2005-12-09 2007-06-14 Pfizer Products Inc. Salts, prodrugs and formulations of 1-[5-(4-amino-7-isopropyl-7h-pyrrolo[2,3-d]pyrimidine-5-carbonyl)-2-methoxy-phenyl]-3-(2,4-dichloro-phenyl)-urea
US20080299113A1 (en) 2005-12-19 2008-12-04 Arnold Lee D Combined treatment with and composition of 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitor and anti-cancer agents
CN101389630A (zh) 2005-12-29 2009-03-18 艾博特公司 蛋白激酶抑制剂
WO2007089669A2 (en) 2006-01-26 2007-08-09 Wyeth Processes for the preparation of compounds which modulate cell proliferation
WO2007095223A2 (en) 2006-02-14 2007-08-23 Vertex Pharmaceuticals Incorporated Pyrrolo(3,2-c) pyridines useful as inhibitors of protein kinases
EP1999303A4 (en) 2006-02-27 2010-09-08 Univ Leland Stanford Junior METHOD FOR IDENTIFYING UPR INHIBITORS
RU2008139599A (ru) 2006-03-07 2010-04-20 Эррэй Биофарма Инк. (Us) Гетеробициклические производные пиразола и способы их применения
HUE030567T2 (en) 2006-03-24 2017-05-29 Biogen Hemophilia Inc PC5 is a factor IX propeptide processing enzyme
WO2007126841A2 (en) 2006-03-29 2007-11-08 Foldrx Pharmaceuticals, Inc. Inhibition of alpha-synuclein toxicity
GB2453058A (en) 2006-04-04 2009-03-25 Univ California Kinase antagonists
WO2007121453A2 (en) 2006-04-17 2007-10-25 The Regents Of The University Of California 2-hydroxy-1-oxo 1,2 dihydro isoquinoline chelating agents
AU2007241343B2 (en) 2006-04-21 2011-09-01 Novartis Ag Purine derivatives for use as adenosin A2A receptor agonists
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607948D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
WO2007125310A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical combinations of pk inhibitors and other active agents
WO2007125315A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical compounds
DE102006020327A1 (de) 2006-04-27 2007-12-27 Bayer Healthcare Ag Heterocyclisch substituierte, anellierte Pyrazol-Derivate und ihre Verwendung
WO2007135398A1 (en) 2006-05-22 2007-11-29 Astrazeneca Ab Indole derivatives
GB0610242D0 (en) 2006-05-23 2006-07-05 Novartis Ag Organic compounds
GB0610317D0 (en) 2006-05-24 2006-07-05 Medical Res Council Antiparasitic compounds and compositions
CA2658462C (en) 2006-07-20 2011-09-27 Amgen Inc. Substituted pyridone compounds and methods of use
EP2061764B1 (en) 2006-08-22 2014-07-02 Technion Research & Development Foundation LTD. Heterocyclic derivatives binding to the peripheral-type benzodiazepine receptor (pbr)
US7678803B2 (en) 2006-08-24 2010-03-16 Serenex, Inc. Quinazoline derivatives for the treatment of cancer
CA2974246C (en) 2006-09-01 2020-02-25 Senhwa Biosciences, Inc. Tricyclic heteroaryl compounds and their use as protein modulators
WO2008025755A1 (de) 2006-09-01 2008-03-06 Basf Se Verwendung von n-haltigen heterozyklen in dermokosmetika
EP1903044A1 (en) 2006-09-14 2008-03-26 Novartis AG Adenosine Derivatives as A2A Receptor Agonists
DE602007013441D1 (de) 2006-09-29 2011-05-05 Novartis Ag Pyrazolopyrimidine als pi3k-lipidkinasehemmer
JP5306818B2 (ja) 2006-10-18 2013-10-02 武田薬品工業株式会社 縮合複素環化合物
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
SG178786A1 (en) 2006-11-13 2012-03-29 Lilly Co Eli Thienopyrimidinones for treatment of inflammatory disorders and cancers
WO2008063625A2 (en) 2006-11-20 2008-05-29 Adolor Corporation Pyridine compounds and methods of their use
EP2132178B1 (en) 2006-12-20 2015-08-19 Merck Sharp & Dohme Corp. Jnk inhibitors
ATE553105T1 (de) 2006-12-22 2012-04-15 Ind Res Ltd Azetidin-analoge ais nucleosidase- und phosphorylase-hemmer
CA2676138A1 (en) 2007-01-26 2008-08-07 Irm Llc Compounds and compositions as kinase inhibitors
WO2008112715A2 (en) 2007-03-12 2008-09-18 Vm Discovery Inc. Novel agents of calcium ion channel modulators
AU2008231384B2 (en) 2007-03-23 2011-09-15 Amgen Inc. Heterocyclic compounds and their use
PL2139882T3 (pl) 2007-03-23 2014-05-30 Amgen Inc 3-podstawione pochodne chinoliny lub chinoksaliny i ich zastosowanie jako inhibitorów 3-kinazy fosfatydyloinozytolu (pi3k)
PT2137186E (pt) 2007-03-23 2016-03-30 Amgen Inc Compostos heterocíclicos e suas utilizações
WO2008156513A2 (en) 2007-03-29 2008-12-24 University Of Connecticut Methods to protect skeletal muscle against injury
CN101657422A (zh) 2007-04-13 2010-02-24 塞诺菲-安万特股份有限公司 过渡金属催化的n-氨基吲哚的合成
CN101636397B (zh) 2007-04-13 2012-06-13 中国人民解放军军事医学科学院毒物药物研究所 脲类化合物、其制备方法及其医药用途
JP2010163361A (ja) 2007-04-27 2010-07-29 Dainippon Sumitomo Pharma Co Ltd キノリン誘導体
WO2008141140A1 (en) * 2007-05-09 2008-11-20 Abbott Laboratories Condensed heterocyclic compounds as inhibitors of protein kinases
US7960353B2 (en) 2007-05-10 2011-06-14 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
US20090214529A9 (en) 2007-05-22 2009-08-27 Taigen Biotechnology Co., Ltd. Kinesin inhibitors
EP2520561B1 (en) 2007-06-08 2016-02-10 MannKind Corporation IRE-1A Inhibitors
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
WO2009000412A1 (en) 2007-06-26 2008-12-31 Sanofi Aventis A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles
WO2009004621A1 (en) 2007-07-02 2009-01-08 Technion Research & Development Foundation Ltd. Compositions, articles and methods comprising tspo ligands for preventing or reducing tobacco-associated damage
RU2345996C1 (ru) 2007-07-17 2009-02-10 Андрей Александрович Иващенко Аннелированные азагетероциклические амиды, включающие пиримидиновый фрагмент, способ их получения и применения
US20090053192A1 (en) 2007-08-10 2009-02-26 Burnham Institute For Medical Research Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof
BRPI0815557A2 (pt) 2007-08-13 2015-02-18 Metabasis Therapeuticas Inc Atividaores de glicocinase
JP5227965B2 (ja) 2007-10-03 2013-07-03 独立行政法人理化学研究所 ニトロトリアゾール誘導体、およびそれを用いる化合物の製造方法
BRPI0818426A2 (pt) 2007-10-15 2017-06-13 Astrazeneca Ab produto de combinação, uso de um produto de combinação, e, método para tratar câncer
JP5256693B2 (ja) 2007-10-31 2013-08-07 信越化学工業株式会社 酸化チタン系光触媒薄膜の製造法
CA2705303A1 (en) 2007-11-07 2009-05-14 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
SG185996A1 (en) 2007-11-13 2012-12-28 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
CA2708391A1 (en) 2007-12-13 2009-06-25 Sri International Ppar-delta ligands and methods of their use
US7960397B2 (en) 2007-12-28 2011-06-14 Institute Of Experimental Botany, Academy Of Sciences Of The Czech Republic 6,9-disubstituted purine derivatives and their use as cosmetics and cosmetic compositions
CN104926815B (zh) 2008-01-04 2017-11-03 英特利凯恩有限责任公司 某些化学实体、组合物和方法
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
JP2011509305A (ja) 2008-01-09 2011-03-24 ピージーエックスヘルス、リミテッド、ライアビリティー、カンパニー Ａ２ａｒアゴニストによる神経障害性疼痛の髄腔内治療
WO2009091939A1 (en) 2008-01-18 2009-07-23 Osi Pharmaceuticals, Inc. Imidazopyrazinol derivatives for the treatment of cancers
WO2009100406A2 (en) 2008-02-07 2009-08-13 Synta Pharmaceuticals Corp. Topical formulations for the treatment of psoriasis
JP2011511802A (ja) 2008-02-07 2011-04-14 ギリアード・パロ・アルト・インコーポレイテッド Ａｂｃａ−１を上昇させる化合物およびかかる化合物の使用方法
TWI444384B (zh) 2008-02-20 2014-07-11 Gilead Sciences Inc 核苷酸類似物及其在治療惡性腫瘤上的用途
WO2009114874A2 (en) 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
JP2011515401A (ja) 2008-03-20 2011-05-19 アムジエン・インコーポレーテツド オーロラキナーゼモジュレーターおよび使用方法
US20090312406A1 (en) 2008-06-12 2009-12-17 Hsing-Pang Hsieh Coumarin compounds and their use for treating viral infection
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
WO2010006086A2 (en) 2008-07-08 2010-01-14 Intellikine, Inc. Kinase inhibitors and methods of use
US20110118286A1 (en) 2008-07-16 2011-05-19 Santhosh Francis Neelamkavil Bicyclic heterocycle derivatives and their use as gpcr modulators
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
CA2737219C (en) 2008-08-11 2017-02-28 Tracy Keller Halofuginone analogs for inhibition of trna synthetases and uses thereof
EP2344481B9 (en) 2008-09-23 2014-12-31 Georgetown University Viral and fungal inhibitors
EP2346508B1 (en) 2008-09-26 2016-08-24 Intellikine, LLC Heterocyclic kinase inhibitors
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
WO2010059593A1 (en) 2008-11-18 2010-05-27 Intellikine, Inc. Methods and compositions for treatment of ophthalmic conditions
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
CN101602768B (zh) 2009-07-17 2012-05-30 河南省农科院农副产品加工研究所 一种芝麻素和芝麻林素的提纯方法
KR102097664B1 (ko) 2009-10-06 2020-04-06 밀레니엄 파머슈티컬스 인코퍼레이티드 Ｐｄｋ１ 저해제로서 유용한 헤테로시클릭 화합물
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
CN110172051B (zh) 2010-04-05 2023-03-07 复星弘创(苏州)医药科技有限公司 IRE-1α抑制剂
WO2011146882A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
US8993617B2 (en) 2010-11-10 2015-03-31 The Board Of Trustees Of The Leland Stanford Junior University Ire1alpha endonuclease specific inhibitor with cytotoxic activity
TWI592411B (zh) 2011-02-23 2017-07-21 英特爾立秦有限責任公司 激酶抑制劑之組合及其用途
EP2751112B1 (en) 2011-09-02 2019-10-09 The Regents of The University of California Substituted pyrazolo[3,4-d]pyrimidines and uses thereof
KR20150061651A (ko) 2012-09-26 2015-06-04 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 Ire1의 조절
WO2016004254A1 (en) 2014-07-01 2016-01-07 The Regents Of The University Of California Combined modulation of ire1

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005506350A (ja) * 2001-10-18 2005-03-03 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン阻害薬としての１，４−二置換ベンゾ−縮合尿素化合物
JP2007509060A (ja) * 2003-10-15 2007-04-12 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド イミダゾピラジンチロシンキナーゼ阻害剤
JP2007531754A (ja) * 2004-04-02 2007-11-08 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド ６，６−二環置換されたヘテロ二環式タンパク質キナーゼ阻害剤
JP2008517890A (ja) * 2004-10-22 2008-05-29 キャンサー・リサーチ・テクノロジー・リミテッド 治療化合物としての、イミダゾ［４，５−ｂ］ピリジン−２−オンおよびオキサゾロ［４，５−ｂ］ピリジン−２−オン化合物ならびにそれらの類似体
WO2007064993A2 (en) * 2005-12-02 2007-06-07 Osi Pharmaceuticals, Inc. Bicyclic protein kinase inhibitors
JP2009530285A (ja) * 2006-03-13 2009-08-27 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド Ｅｇｆｒキナーゼ阻害剤およびｅｇｆｒキナーゼ阻害剤の効果に対し腫瘍細胞を感作する薬剤を用いる併用治療
JP2010526833A (ja) * 2007-05-09 2010-08-05 アボット・ラボラトリーズ タンパク質キナーゼ阻害薬としての縮合複素環化合物
JP2011520970A (ja) * 2008-05-19 2011-07-21 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド 置換されたイミダゾピラジン類およびイミダゾトリアジン類
JP2012505916A (ja) * 2008-10-16 2012-03-08 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 融合環ヘテロアリールキナーゼ阻害剤
WO2011094628A1 (en) * 2010-01-28 2011-08-04 University Of Washington Compositions and methods for treating toxoplasmosis. cryptosporidiosis and other apicomplexan protozoan related diseases
WO2013010380A1 (en) * 2011-07-19 2013-01-24 Merck Sharp & Dohme Corp. Btk inhibitors
WO2013010868A1 (en) * 2011-07-19 2013-01-24 Msd Oss B.V. 4 - imidazopyridazin- 1 -yl-benzamides and 4 - imidazotriazin- 1 - yl - benzamides as btk- inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
WANG, LIKUN ET AL.: "Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors", NATURE CHEMICAL BIOLOGY, vol. 8, no. 12, JPN7017003286, 2012, pages 982 - 989, ISSN: 0003658648 *

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Publication number Priority date Publication date Assignee Title
US11136326B2 (en) 2015-08-26 2021-10-05 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
US12415809B2 (en) 2016-03-28 2025-09-16 Incyte Corporation Pyrrolotriazine compounds as tam inhibitors
JP2019510043A (ja) * 2016-03-28 2019-04-11 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｔａｍ阻害剤としてのピロロトリアジン化合物
JP7034084B2 (ja) 2016-03-28 2022-03-11 インサイト・コーポレイション Ｔａｍ阻害剤としてのピロロトリアジン化合物
JP2022084663A (ja) * 2016-03-28 2022-06-07 インサイト・コーポレイション Ｔａｍ阻害剤としてのピロロトリアジン化合物
US11591338B2 (en) 2016-03-28 2023-02-28 Incyte Corporation Pyrrolotriazine compounds as TAM inhibitors
JP7271750B2 (ja) 2016-03-28 2023-05-11 インサイト・コーポレイション Ｔａｍ阻害剤としてのピロロトリアジン化合物
JP2020532589A (ja) * 2017-09-01 2020-11-12 オプティキラ リミテッド ライアビリティ カンパニー Ｉｒｅ１阻害のための化合物および組成物
US11649237B2 (en) 2017-09-01 2023-05-16 Optikira Llc Substituted imidazo[1,5-a]pyrazines for IRE1 inhibition
US11104682B2 (en) 2017-09-27 2021-08-31 Incyte Corporation Salts of TAM inhibitors
US12187730B2 (en) 2017-09-27 2025-01-07 Incyte Corporation Salts of TAM inhibitors
JP7535335B2 (ja) 2017-11-10 2024-08-16 コーネル・ユニバーシティー 低分子ｉｒｅ１阻害剤
JP2023100744A (ja) * 2017-11-10 2023-07-19 コーネル・ユニバーシティー 低分子ｉｒｅ１阻害剤
US11241438B2 (en) 2018-06-29 2022-02-08 Incyte Corporation Formulations of an AXL/MER inhibitor
US11918585B2 (en) 2018-06-29 2024-03-05 Incyte Corporation Formulations of an AXL/MER inhibitor
US12318389B2 (en) 2018-06-29 2025-06-03 Incyte Corporation Formulations of an AXL/MER inhibitor
JP2022521784A (ja) * 2019-02-27 2022-04-12 オプティキラ リミテッド ライアビリティ カンパニー Ｉｒｅ１阻害のためのピラゾロピリジン化合物
US12214036B2 (en) 2020-03-06 2025-02-04 Incyte Corporation Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors

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