JP2015532287A - Ｉｒｅ１の調節 - Google Patents

Ｉｒｅ１の調節 Download PDF

Info

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
Authority
JP
Japan
Prior art keywords
substituted
unsubstituted
disease
ire1α
heteroaryl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2015534672A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015532287A5 (https=
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
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
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

Links

Images

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (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 (https=) 2016-12-08

Family

ID=50388979

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015534672A Pending JP2015532287A (ja) 2012-09-26 2013-09-26 Ｉｒｅ１の調節

Country Status (13)

Country Link
US (3) US10131668B2 (https=)
EP (1) EP2900673A4 (https=)
JP (1) JP2015532287A (https=)
KR (1) KR20150061651A (https=)
CN (1) CN104995192A (https=)
AU (1) AU2013323426A1 (https=)
BR (1) BR112015006828A8 (https=)
CA (1) CA2886240A1 (https=)
IL (1) IL237970A0 (https=)
MX (1) MX2015003874A (https=)
RU (1) RU2015115631A (https=)
SG (1) SG11201502331RA (https=)
WO (1) WO2014052669A1 (https=)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2024504707A (ja) * 2021-01-22 2024-02-01 コーネル ユニヴァーシティー リポフスチン細胞毒性から保護するための化合物の同定のための組成物及び方法
US12214036B2 (en) 2020-03-06 2025-02-04 Incyte Corporation Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2015003874A (es) 2012-09-26 2015-12-16 Univ California Modulacion de ire1.
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
CA3016161A1 (en) 2016-03-03 2017-09-08 Cornell University Small molecule ire1-alpha inhibitors
EP3548476A4 (en) 2016-12-02 2020-05-20 Quentis Therapeutics, Inc. SMALL MOLECULAR IRE1 INHIBITORS
US10392367B2 (en) 2017-06-01 2019-08-27 Quentis Therapeutics, Inc. IRE1 small molecule inhibitors
CA3064837A1 (en) 2017-06-01 2018-12-06 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
WO2020117634A1 (en) * 2018-12-03 2020-06-11 Cornell University Ire1 small molecule inhibitors
JP7539892B2 (ja) 2019-01-03 2024-08-26 ジェネンテック， インコーポレイテッド 癌疾患の処置のためのエンドリボヌクレアーゼのイノシトール要求酵素ｉ（ｉｒｅｉアルファ）の阻害剤としてのピリド－ピリミジノン化合物及びプテリジノン化合物
US20220194945A1 (en) * 2019-02-27 2022-06-23 Optikira, LLC Imidazolopyridine Compounds For IRE1 Inhibition
AU2020243376B2 (en) * 2019-03-15 2025-09-04 Alterity Therapeutics Limited Compounds for and methods of treating diseases
WO2020232403A1 (en) * 2019-05-15 2020-11-19 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
US12331054B2 (en) * 2019-08-29 2025-06-17 Hibercell, Inc. Perk inhibiting imidazolopyrazine compounds
KR20230118855A (ko) * 2020-11-13 2023-08-14 더 리전츠 오브 더 유니버시티 오브 캘리포니아 IRE1α 억제제 및 이의 용도
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
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
WO2013010380A1 (en) * 2011-07-19 2013-01-24 Merck Sharp & Dohme Corp. 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 (https=) 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
US5428125A (en) 1989-07-17 1995-06-27 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5442039A (en) 1989-07-17 1995-08-15 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
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
US5721356A (en) 1989-09-15 1998-02-24 Gensia, Inc. Orally active adenosine kinase inhibitors
US5795977A (en) 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
US5763597A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. Orally active adenosine kinase inhibitors
US5646128A (en) 1989-09-15 1997-07-08 Gensia, Inc. Methods for treating adenosine kinase related conditions
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
US5563257A (en) 1990-08-20 1996-10-08 Boehringer Mannheim Gmbh Phospholipid derivatives of nucleosides
DE4026265A1 (de) 1990-08-20 1992-02-27 Boehringer Mannheim Gmbh Neue phospholipid-derivate von nucleosiden, deren herstellung sowie deren verwendung als antivirale arzneimittel
US5561134A (en) 1990-09-25 1996-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
US5652366A (en) 1990-09-25 1997-07-29 Rhone-Poulenc Rorer Pharmaceuticals Inc. DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof
SG80526A1 (en) 1990-09-25 2001-05-22 Rhone Poulenc Rorer Int Compounds having antihypertensive and anti- ischemic properies
ATE141502T1 (de) 1991-01-15 1996-09-15 Alcon Lab Inc Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen
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
US5916891A (en) 1992-01-13 1999-06-29 Smithkline Beecham Corporation Pyrimidinyl imidazoles
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.
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
JPH07506252A (ja) 1992-04-24 1995-07-13 エス・アール・アイ・インターナシヨナル 真核細胞内でのイン・ビボ相同配列ターゲッティング
DE69328440T3 (de) 1992-06-19 2009-05-07 Honeywell, Inc., Minneapolis Infrarot kamera mit thermoelektrischer temperaturstabilisierung
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
EP0684953A4 (en) 1993-02-03 1999-12-22 Gensia Inc ADENOSINE KINASE INHIBITORS COMPRISING LYXOFURANOSYL DERIVATIVES.
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
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
JP4145955B2 (ja) 1994-09-29 2008-09-03 ノバルティス アクチェンゲゼルシャフト ピロロ〔２，３−ｄ〕ピリミジン及びその使用
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
ES2150113T3 (es) 1995-04-03 2000-11-16 Novartis Ag Derivados de pirazol y procedimientos para la preparacion de los mismos.
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
WO1996037777A1 (en) 1995-05-23 1996-11-28 Nelson Randall W Mass spectrometric immunoassay
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
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
WO1996040258A2 (en) 1995-06-07 1996-12-19 G.D. Searle & Co. Spironolactone and angiotensin ii antagonist combination therapy for treatment of congestive heart failure
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
DK0831910T3 (da) 1995-06-07 2002-05-21 Searle & Co Kombinationsterapi med epoxy-steroid aldosteronantagonist og angiotensin II-receptorantagonist til behandling af kongestivt hjertesvigt
US5665721A (en) 1995-06-07 1997-09-09 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
CA2245835A1 (en) 1995-06-14 1997-01-03 The Regents Of The University Of California Novel high affinity human antibodies to tumor antigens
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
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
DE19603576A1 (de) 1996-02-01 1997-08-07 Bayer Ag Acylierte 4-Amino und 4-Hydrazinopyrimidine
GB2310952B (en) 1996-03-05 1998-08-19 Mitsubishi Electric Corp Infrared detector
GB9611460D0 (en) 1996-06-01 1996-08-07 Ludwig Inst Cancer Res Novel lipid kinase
HUP9904567A3 (en) 1996-06-20 2001-10-29 Univ Texas Use of azo, thioalkyl, thiocarbonyl derivatives substituted by fused heterocycles and/or phenyl group for the preparation of pharmaceutical compositions stimulating bone growth
US5922753A (en) 1996-10-23 1999-07-13 Zymogenetics, Inc. Methods for treating bone deficit conditions with benzothiazole
US5948776A (en) 1996-10-23 1999-09-07 Zymogenetic, Inc. Compositions and methods for treating bone deficit conditions
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
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
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
EP0942925B1 (en) 1996-12-06 2006-11-22 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1 beta converting enzyme
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
AU755062B2 (en) 1997-02-07 2002-12-05 Princeton University Engineered protein kinases which can utilize modified nucleotide triphosphate substrates
US7863444B2 (en) 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
DK0970084T3 (da) 1997-03-19 2003-09-29 Abbott Gmbh & Co Kg Pyrrolo[2,3-d]pyrimidiner og deres anvendelse som inhibitorer for tyrosinkinase
AU7449598A (en) 1997-05-23 1998-12-11 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
ATE404539T1 (de) 1997-10-02 2008-08-15 Eisai R&D Man Co Ltd Kondensierte pyridinderivate
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
WO1999024432A1 (fr) 1997-11-12 1999-05-20 Mitsubishi Chemical Corporation Derives de purine et medicament les renfermant en tant qu'ingredient actif
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
CA2344249A1 (en) 1998-09-18 2000-03-30 Basf Aktiengesellschaft Pyrrolopyrimidines as protein kinase inhibitors
US6713474B2 (en) 1998-09-18 2004-03-30 Abbott Gmbh & Co. Kg Pyrrolopyrimidines as therapeutic agents
CA2344262A1 (en) 1998-09-18 2000-03-30 Basf Aktiengesellschaft 4-aminopyrrolopyrimidines as kinase inhibitors
DK1140938T3 (da) 1999-01-11 2003-12-22 Univ Princeton Højaffinitetsinhibitorer for målvalidering og anvendelser heraf
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
JP2003501429A (ja) 1999-06-03 2003-01-14 クノール・ゲー・エム・ベー・ハー ベンゾチアジノンおよびベンゾオキサジノン化合物
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
JP4831906B2 (ja) 1999-08-27 2011-12-07 ケモセントリックス， インコーポレイテッド Ｃｘｃｒ３機能を調節するための複素環式化合物および方法
AU780846B2 (en) 1999-09-16 2005-04-21 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
CA2385747A1 (en) 1999-09-17 2001-03-22 Gavin C. Hirst Pyrazolopyrimidines as therapeutic agents
EP1222187B1 (en) 1999-10-06 2004-09-22 Boehringer Ingelheim Pharmaceuticals Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
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
MXPA02009543A (es) 2000-03-29 2005-08-26 Abbott Gmbh & Co Kg Metodo para identificar inhibidores de tie-2.
US6613798B1 (en) 2000-03-30 2003-09-02 Curis, Inc. Small organic molecule regulators of cell proliferation
US7115653B2 (en) 2000-03-30 2006-10-03 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
ES2788383T3 (es) 2000-04-25 2020-10-21 Icos Corp Inhibidores de delta fosfatidilo-inositol 3-quinasa humana
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
US6777439B2 (en) 2000-05-30 2004-08-17 Advanced Research & Technology Institute, Inc. Compositions and methods for identifying agents which modulate PTEN function and PI-3 kinase pathways
NZ522839A (en) 2000-06-27 2004-11-26 Genelabs Tech Inc Novel 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
AU1312502A (en) 2000-10-11 2002-04-22 Pe Corp Ny Fluorescent nucleobase conjugates having anionic linkers
EP1578341A2 (en) 2000-10-11 2005-09-28 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
MXPA03005152A (es) 2000-12-11 2004-10-14 Tularik Inc Antogonista de cxcr3.
US7157487B2 (en) 2000-12-28 2007-01-02 Daiichi Pharmaceutical Co., Ltd. Vla-4 inhibitors
WO2002057425A2 (en) 2001-01-22 2002-07-25 Merck & Co., Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
US7105499B2 (en) 2001-01-22 2006-09-12 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
DE60239097D1 (de) 2001-03-02 2011-03-17 Gpc Biotech Ag Drei-hybrid-assaysystem
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
DE60218458T2 (de) 2001-05-08 2007-11-15 Kudos Pharmaceuticals Ltd. Isochinolinon derivate als parp inhibitoren
US7144903B2 (en) 2001-05-23 2006-12-05 Amgen Inc. CCR4 antagonists
US6777425B2 (en) 2001-06-13 2004-08-17 Genesoft Pharmaceuticals, Inc. Isoquinoline compounds having antiinfective activity
US20030236198A1 (en) 2001-06-13 2003-12-25 Genesoft, Inc. Antipathogenic benzamide compounds
EP1470119A4 (en) 2001-06-13 2005-10-19 Genesoft Pharmaceuticals Inc BENZOTHIOPHENE COMPOUNDS WITH ANTI-INFECTIOUS ACTIVITY
AU2002315389A1 (en) 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel pyrazolo-and pyrrolo-pyrimidines and uses thereof
EP1414443B1 (en) 2001-08-01 2006-11-15 Merck & Co., Inc. BENZIMIDAZO 4,5-f|ISOQUINOLINONE DERIVATIVES
WO2003020880A2 (en) 2001-08-03 2003-03-13 Abbott Laboratories Method of identifying inhibitors of lck
BR0211750A (pt) 2001-08-10 2004-10-13 Shionogi & Co 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
CA2458926A1 (en) 2001-09-13 2003-03-13 Genesoft Pharmaceuticals, Inc. Methods of treating infection by drug resistant bacteria
AUPR769501A0 (en) 2001-09-14 2001-10-11 Biomolecular Research Institute Limited Cytokine receptor 1
US7101884B2 (en) 2001-09-14 2006-09-05 Merck & Co., Inc. Tyrosine kinase inhibitors
TWI330183B (https=) 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
AU2002350217A1 (en) 2001-12-04 2003-06-17 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
WO2003059884A1 (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
US7064218B2 (en) 2001-12-26 2006-06-20 Genelabs Technologies, Inc. Aromatic compounds and poly(oxyalkylene) containing aromatic compounds 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
EP1503988B1 (de) 2002-03-26 2009-07-22 Biofrontera Discovery Gmbh Fredericamycin-derivate
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
WO2003090751A1 (en) 2002-04-26 2003-11-06 Pfizer Products Inc. Pyrimidine-2, 4, 6-trione metallo-proteinase inhibitors
US6794562B2 (en) 2002-05-01 2004-09-21 Stine Seed Farm, Inc. Soybean cultivar 0332143
WO2004039774A2 (en) 2002-05-23 2004-05-13 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2003106426A1 (en) 2002-06-14 2003-12-24 Cytokinetics, Inc. Compounds, compositions, and methods
RU2340605C2 (ru) 2002-06-27 2008-12-10 Ново Нордиск А/С Арилкарбонильные производные в качестве терапевтических средств
US7265111B2 (en) 2002-06-27 2007-09-04 Sanofi-Aventis Deutschland Gmbh Adenosine analogues and their use as pharmaceutical agents
BR0312023A (pt) 2002-06-27 2005-03-22 Novo Nordisk As Composto, composto ativador da glicose cinase, método para evitar a hipoglicemia, uso de um composto, e, composição farmacêutica
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
WO2004014377A1 (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
US20040048853A1 (en) 2002-08-21 2004-03-11 Gustave Bergnes Compounds, compositions, and methods
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
WO2004020610A2 (en) 2002-08-30 2004-03-11 President And Fellows Of Harvard College Methods and compositions for modulating xbp-1 activity
US7312341B2 (en) * 2002-09-09 2007-12-25 Cgi Pharmaceuticals, Inc. 6-aryl-imidazo[1,2-a] pyrazin-8-ylamines, method of making, and method of use thereof
JP4487774B2 (ja) 2002-09-30 2010-06-23 萬有製薬株式会社 ２−アミノベンズイミダゾール誘導体
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
ATE496893T1 (de) 2002-12-20 2011-02-15 X Ceptor Therapeutics Inc Isochinolinonderivate und deren verwendung als medikamente
US7247736B2 (en) 2002-12-23 2007-07-24 4Sc Ag Method of identifying inhibitors of DHODH
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
CA2517942A1 (en) 2003-03-06 2004-09-16 Dsm Ip Assets B.V. 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
US7217794B2 (en) 2003-04-02 2007-05-15 Daiamed, Inc. Compounds and methods for treatment of thrombosis
WO2004100868A2 (en) 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
DE602004022819D1 (de) 2003-06-06 2009-10-08 Vertex Pharma Von atp-bindende kassette transportern
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
US7501538B2 (en) 2003-08-08 2009-03-10 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
WO2005016348A1 (en) 2003-08-14 2005-02-24 Icos Corporation Method of inhibiting immune responses stimulated by an endogenous factor
US20050054614A1 (en) 2003-08-14 2005-03-10 Diacovo Thomas G. Methods of inhibiting leukocyte accumulation
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
CA2546192C (en) 2003-11-17 2010-04-06 Pfizer Products Inc. Pyrrolopyrimidine compounds useful in treatment of cancer
EP1692112A4 (en) 2003-12-08 2008-09-24 Cytokinetics Inc COMPOUNDS, COMPOSITIONS, AND METHODS
CA2548951A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
US7569571B2 (en) 2003-12-23 2009-08-04 Novartis Ag Substituted pyrazolo [3,4-d]pyrimidines as cytokine modulators
US20050239809A1 (en) 2004-01-08 2005-10-27 Watts Stephanie W Methods for treating and preventing hypertension and hypertension-related disorders
JP2007520559A (ja) 2004-02-03 2007-07-26 アボット・ラボラトリーズ 治療薬としてのアミノベンゾオキサゾール類
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
WO2005080394A1 (en) 2004-02-24 2005-09-01 Bioaxone Therapeutique Inc. 4-substituted piperidine derivatives
KR100843526B1 (ko) 2004-02-27 2008-07-03 에프. 호프만-라 로슈 아게 피라졸의 접합 유도체
TW200538453A (en) 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
BRPI0510305A (pt) 2004-04-30 2007-10-02 Takeda Pharmaceutical composto ou um sal do mesmo, pródroga ou um sal da mesma, agente farmacêutico, método de produção do composto ou um sal do mesmo, inibidor de metaloproteinase de matriz ou um sal do mesmo ou uma pródroga do mesmo, método de inibir uma metaloproteinase de matriz, e, uso de um composto ou de um sal do mesmo ou de uma pródroga do mesmo
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
CA2730540A1 (en) 2004-05-13 2005-12-01 Vanderbilt University Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis
SI2612862T1 (sl) 2004-05-13 2017-04-26 Icos Corporation Kinazolini kot inhibitorji humane fosfatidilinozitol 3-kinaze delta
JP2008500338A (ja) 2004-05-25 2008-01-10 イコス・コーポレイション 造血細胞の異常増殖を治療及び／又は予防する方法
MXPA06013805A (es) 2004-05-27 2007-02-02 Pfizer Prod Inc Derivados de pirrolopirimidina de utilidad en el tratamiento contra el cancer.
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
US7622451B2 (en) 2004-11-03 2009-11-24 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
WO2006050501A2 (en) 2004-11-03 2006-05-11 University Of Kansas Novobiocin analogues as anticancer agents
US8212011B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
US9512125B2 (en) 2004-11-19 2016-12-06 The Regents Of The University Of California Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents
US8143257B2 (en) 2004-11-23 2012-03-27 Ptc Therapeutics, Inc. Substituted phenols as active agents inhibiting VEGF production
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
WO2006089106A2 (en) 2005-02-17 2006-08-24 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
US7579348B2 (en) 2005-02-25 2009-08-25 Pgxhealth, 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
RU2007138264A (ru) 2005-03-17 2009-09-10 Новартис АГ (CH) N-[3-(1-АМИНО-5,6,7,8-ТЕТРАГИДРО-2,4,4b-ТРИАЗАФЛУОРЕН-9-ИЛ)ФЕНИЛ]БЕНЗАМИДЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ТИРОЗИН/ТРЕОНИНКИНАЗ, ПРЕЖДЕ ВСЕГО КИНАЗ В-RAF
RU2007140733A (ru) 2005-04-06 2009-05-20 Айрм Ллк (Bm) Диариламинсодержащие соединения и композиции, и их применение в качестве модуляторов ядерных рецепторов стероидного гормона
KR100781704B1 (ko) 2005-04-20 2007-12-03 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
JP5033119B2 (ja) 2005-04-25 2012-09-26 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング キナーゼ阻害剤としての新規アザ複素環化合物
WO2006114064A2 (en) 2005-04-25 2006-11-02 Institute Of Organic Chemistry And Biochemistry Ofthe Academy Of Sciences Of The Czech Republic Use of compounds to enhance processivity of telomerase
BRPI0612112A8 (pt) 2005-06-22 2017-12-26 Chemocentryx Inc composto, composição farmacêutica, e, método de tratar doenças ou condições mediadas por ccr1.
CA2612585A1 (en) 2005-06-27 2007-01-04 Amgen Inc. Anti-inflammatory aryl nitrile compounds
JP2009500437A (ja) 2005-07-11 2009-01-08 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
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
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
RU2008110941A (ru) 2005-08-25 2009-09-27 Ф.Хоффманн-Ля Рош Аг (Ch) ИНГИБИТОРЫ КИНАЗЫ p38 МАР И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
US20080318942A1 (en) 2005-09-01 2008-12-25 Bioagency Ag Fredericamycin Derivatives
CA2624220A1 (en) 2005-09-29 2007-04-12 Wyeth 1- (1h- indol- 1-yl) -3- (methylamino) -1- phenylpropan-2-ol derivatives and related compounds as modulators of the monoamine reuptake for the treatment of vasomotor symptoms (vms)
EP2385053B1 (en) 2005-11-17 2013-10-02 OSI Pharmaceuticals, Inc. Intermediates for the preparation of fused bicyclic mTOR inhibitors
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
JP2009520028A (ja) 2005-12-19 2009-05-21 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 Ｉｇｆｒ抑制剤および抗癌剤の併用
TW200801008A (en) 2005-12-29 2008-01-01 Abbott Lab Protein kinase inhibitors
WO2007089669A2 (en) 2006-01-26 2007-08-09 Wyeth Processes for the preparation of compounds which modulate cell proliferation
US7659283B2 (en) 2006-02-14 2010-02-09 Vertex Pharmaceuticals Incorporated Pyrrolo [3,2-C] pyridines useful as inhibitors of protein kinases
AU2007220039A1 (en) 2006-02-27 2007-09-07 The Board Of Trustees Of The Leland Stanford Junior University Inhibitors of the unfolded protein response and methods for their use
BRPI0708615A2 (pt) 2006-03-07 2011-06-07 Array Biopharma Inc compostos de pirazol heterobicìclicos e métodos de uso
EP2004683B1 (en) 2006-03-24 2016-05-11 Biogen Hemophilia Inc. Pc5 as a factor ix propeptide processing enzyme
CA2647543A1 (en) 2006-03-29 2007-11-08 Foldrx Pharmaceuticals, Inc. Inhibition of alpha-synuclein toxicity
WO2007114926A2 (en) 2006-04-04 2007-10-11 The Regents Of The University Of 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
EP2322525B1 (en) 2006-04-21 2013-09-18 Novartis AG Purine derivatives for use as adenosin A2A receptor agonists
GB0607948D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
WO2007125315A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical compounds
EP2037931A2 (en) 2006-04-25 2009-03-25 Astex Therapeutics Limited Pharmaceutical combinations of pk inhibitors and other active agents
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
ES2344760T3 (es) 2006-07-20 2010-09-06 Amgen Inc. Compuestos de piridona sustituidos y metodo de uso.
WO2008023357A1 (en) 2006-08-22 2008-02-28 Technion Research And Development Foundation Ltd. Heterocyclic derivatives binding to the peripheral-type benzodiazepine receptor (pbr)
JP2010501593A (ja) 2006-08-24 2010-01-21 セレネックス， インコーポレイテッド イソキノリン、キナゾリンおよびフタラジン誘導体
US7956064B2 (en) 2006-09-01 2011-06-07 Cylene Pharmaceuticals, Inc. Fused tricyclic compounds as serine-threonine protein kinase and PARP 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
WO2008037477A1 (en) 2006-09-29 2008-04-03 Novartis Ag Pyrazolopyrimidines as p13k lipid kinase inhibitors
EP2077267A4 (en) 2006-10-18 2010-04-07 Takeda Pharmaceutical CONDENSED HETEROCYCLIC COMPOUND
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
KR20090087027A (ko) 2006-11-13 2009-08-14 일라이 릴리 앤드 캄파니 염증 질환 및 암의 치료를 위한 티에노피리미디논
WO2008063625A2 (en) 2006-11-20 2008-05-29 Adolor Corporation Pyridine compounds and methods of their use
CN101611007A (zh) 2006-12-20 2009-12-23 先灵公司 新颖的jnk抑制剂
EP2114925B8 (en) 2006-12-22 2013-04-10 Industrial Research Limited Azetidine analogues of nucleosidase and phosphorylase inhibitors
CN101622001A (zh) 2007-01-26 2010-01-06 Irm责任有限公司 作为激酶抑制剂用于治疗疟原虫相关疾病的嘌呤化合物和组合物
US8586619B2 (en) 2007-03-12 2013-11-19 Vm Therapeutics Llc Agents of calcium ion channel modulators
RS53151B (sr) 2007-03-23 2014-06-30 Amgen Inc. 3-supstituisani derivati hinolina ili hinoksalina i njihova upotreba kao inhibitora fosfatidilinozitol 3-kinaze (pi3k)
EA017389B1 (ru) 2007-03-23 2012-12-28 Амген Инк. Гетероциклические соединения и их применение
WO2008118454A2 (en) 2007-03-23 2008-10-02 Amgen Inc. Derivatives of quinoline or benzopyrazine and their uses for the treatment of (inter alia) inflammatory diseases, autoimmune diseases or various kinds of cancer
US7867983B2 (en) 2007-03-29 2011-01-11 The University Of Connecticut Methods to protect skeletal muscle against injury
WO2008125207A1 (en) 2007-04-13 2008-10-23 Sanofi-Aventis A transition metal catalyzed synthesis of n-aminoindoles
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
WO2008147852A1 (en) 2007-05-22 2008-12-04 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
BRPI0813273A2 (pt) 2007-06-26 2014-12-30 Sanofi Aventis Síntese catalisada por metal regiosseletivo de benzimidazóis e azabenzimidazóis anelados
EP2170274A1 (en) 2007-07-02 2010-04-07 Technion Research and 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
CA2696113A1 (en) 2007-08-10 2009-04-02 Burnham Institute For Medical Research Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof
WO2009023718A2 (en) 2007-08-13 2009-02-19 Metabasis Therapeutics, Inc. Novel activators of glucokinase
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
WO2009050506A2 (en) 2007-10-15 2009-04-23 Astrazeneca Ab Combination 059
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
US20100331297A1 (en) 2007-11-07 2010-12-30 Foldrx Pharmaceuticals, Inc. Modulation of protein trafficking
CA2716334A1 (en) 2007-11-13 2009-05-22 Icos Corporation Inhibitors of human phosphatidyl-inositol 3-kinase delta
US20090163481A1 (en) 2007-12-13 2009-06-25 Murphy Brian J 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
EP3613743B1 (en) 2008-01-04 2022-03-16 Intellikine, LLC Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives
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
JP2011510018A (ja) 2008-01-18 2011-03-31 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 癌治療のためのイミダゾピラジノール誘導体
CN101983062A (zh) 2008-02-07 2011-03-02 吉利德帕洛阿尔托股份有限公司 提高abca-1的化合物及其用途
EP2244709A4 (en) 2008-02-07 2012-02-29 Synta Pharmaceuticals Corp TOPICAL FORMULATIONS FOR THE TREATMENT OF PSORIASIS
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
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
ES2413806T3 (es) 2008-03-20 2013-07-17 Amgen Inc. Moduladores de la aurora cinasa y método de uso
US20090312406A1 (en) 2008-06-12 2009-12-17 Hsing-Pang Hsieh Coumarin compounds and their use for treating viral infection
JP5788316B2 (ja) 2008-07-08 2015-09-30 インテリカイン， エルエルシー キナーゼインヒビターおよび使用方法
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
JP2011528368A (ja) 2008-07-16 2011-11-17 シェーリング コーポレイション 二環式ヘテロ環誘導体およびｇｐｃｒモジュレーターとしてのその使用
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US9284297B2 (en) 2008-08-11 2016-03-15 President And Fellows Of Harvard College Halofuginone analogs for inhibition of tRNA synthetases and uses thereof
WO2010039534A2 (en) 2008-09-23 2010-04-08 Georgetown University Viral and fungal inhibitors
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine 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
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
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
HRP20160967T1 (hr) 2009-10-06 2016-10-07 Millennium Pharmaceuticals, Inc. Heterociklički spojevi korisni kao pdk1 inhibitori
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
EP2555768B1 (en) 2010-04-05 2018-08-29 Fosun Orinove Pharmatech, Inc. Ire-1 inhibitors
CA2799579A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
WO2012064774A1 (en) 2010-11-10 2012-05-18 The Board Of Trustees Of The Leland Stanford Junior University An ire1alpha endonuclease specific inhibitor with cytotoxic activity
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
MX370814B (es) 2011-09-02 2020-01-08 Univ California Pirazolo[3,4-d]pirimidinas sustituidas y usos de las mismas.
MX2015003874A (es) 2012-09-26 2015-12-16 Univ California Modulacion de ire1.
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
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
WO2013010380A1 (en) * 2011-07-19 2013-01-24 Merck Sharp & Dohme Corp. 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 *

Cited By (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11136326B2 (en) 2015-08-26 2021-10-05 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
JP2024133478A (ja) * 2016-03-28 2024-10-02 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
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
JP7834804B2 (ja) 2016-03-28 2026-03-24 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
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
US12415809B2 (en) 2016-03-28 2025-09-16 Incyte Corporation Pyrrolotriazine compounds as tam inhibitors
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
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
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
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
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
US12214036B2 (en) 2020-03-06 2025-02-04 Incyte Corporation Combination therapy comprising AXL/MER and PD-1/PD-L1 inhibitors
JP2024504707A (ja) * 2021-01-22 2024-02-01 コーネル ユニヴァーシティー リポフスチン細胞毒性から保護するための化合物の同定のための組成物及び方法

Also Published As

Publication number Publication date
US20210155626A1 (en) 2021-05-27
SG11201502331RA (en) 2015-04-29
US10131668B2 (en) 2018-11-20
WO2014052669A1 (en) 2014-04-03
US10822340B2 (en) 2020-11-03
EP2900673A4 (en) 2016-10-19
RU2015115631A (ru) 2016-11-20
CN104995192A (zh) 2015-10-21
IL237970A0 (en) 2015-05-31
US20190084989A1 (en) 2019-03-21
EP2900673A1 (en) 2015-08-05
AU2013323426A1 (en) 2015-04-23
US20160024094A1 (en) 2016-01-28
CA2886240A1 (en) 2014-04-03
KR20150061651A (ko) 2015-06-04
BR112015006828A2 (pt) 2017-07-04
US11613544B2 (en) 2023-03-28
MX2015003874A (es) 2015-12-16
BR112015006828A8 (pt) 2019-09-17

Similar Documents

Publication Publication Date Title
US11613544B2 (en) Substituted imidazo[1,5-a]pyrazines for modulation of IRE1
US20170165259A1 (en) Combined modulation of ire1
JP4500055B2 (ja) ピラゾロ［１，５−ａ］ピリミジン誘導体およびそれを含有するＮＡＤ（Ｐ）Ｈオキシダーゼ阻害剤
CN101827593B (zh) 用于治疗(特别是)囊性纤维化的异噻唑并吡啶酮
US20230049952A1 (en) Methods and compounds for restoring mutant p53 function
EP3104706B1 (en) Compositions and methods using the same for treatment of neurodegenerative and mitochondrial disease
US20230210853A1 (en) Targeted nek7 inhibition for modulation of the nlrp3 inflammasome
JP2016510764A (ja) 混合系キナーゼ阻害剤および治療法
KR20010042804A (ko) 비티케이 억제제와 그들의 동정 방법 및 용도
JPWO2015115355A1 (ja) 抗がん剤組成物
JP7163180B2 (ja) ３－ヒドロキシ－キナゾリン－２，４－ジオン誘導体およびヌクレアーゼ調節因子としてのこの使用
WO2019169306A1 (en) Compounds, compositions, and methods for suppressing toxic endoplasmic reticulum stress
KR20200019228A (ko) 신경퇴행성 및 미토콘드리아 질환의 치료를 위한 조성물 및 이를 사용하는 방법
JP2019038848A (ja) 白血病を予防および治療するためのマレイミド誘導体の使用
CN112469409B (zh) 用于治疗疾病状态和病症的对映异构体纯的gper激动剂
EP4023647B1 (en) Imidazopyridine derivative and pharmaceutical composition comprising same as active ingredient
WO2017210559A1 (en) Compounds and methods for treating fibrosis or cancer
JP2026067907A (ja) 神経変性疾患及びミトコンドリア病の治療用の組成物ならびにその使用方法
CN114426541A (zh) 氮杂芳基化合物及其用途
HK40009984A (en) Erbb inhibitors and uses thereof
HK1146934B (en) Modulators of cystic fibrosis transmembrane conductance regulator

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160926

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20160926

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20160926

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20170810

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20171010

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180110

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180703

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20190212