EA201791289A1 - Ингибиторы клеточного некроза и связанные с ними способы - Google Patents

Ингибиторы клеточного некроза и связанные с ними способы

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Publication number
EA201791289A1
EA201791289A1 EA201791289A EA201791289A EA201791289A1 EA 201791289 A1 EA201791289 A1 EA 201791289A1 EA 201791289 A EA201791289 A EA 201791289A EA 201791289 A EA201791289 A EA 201791289A EA 201791289 A1 EA201791289 A1 EA 201791289A1
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EA
Eurasian Patent Office
Prior art keywords
inhibitors
related methods
cellular necrosis
proposed
treatment
Prior art date
Application number
EA201791289A
Other languages
English (en)
Inventor
Цзюньин Юань
Ицзюнь Чжоу
Шань Цянь
Давэй Ма
Original Assignee
Президент Энд Феллоуз Оф Гарвард Колледж
Шанхай Инститьют Оф Органик Кемистри, Чайниз Академи Оф Сайенсиз
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 Президент Энд Феллоуз Оф Гарвард Колледж, Шанхай Инститьют Оф Органик Кемистри, Чайниз Академи Оф Сайенсиз filed Critical Президент Энд Феллоуз Оф Гарвард Колледж
Publication of EA201791289A1 publication Critical patent/EA201791289A1/ru

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
    • C07D233/76—Two oxygen atoms, e.g. hydantoin with substituted hydrocarbon radicals attached to the third ring carbon atom
    • C07D233/78—Radicals substituted by oxygen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Предложено соединение, имеющее следующую структуру (I):или его фармацевтически приемлемая соль, пролекарство, стереоизомер или таутомер. Предложены также родственные соединения, способы их получения и применение указанных соединений для лечения различных показаний, включая лечение некротических болезней клеток и/или воспаления.
EA201791289A 2014-12-11 2015-12-11 Ингибиторы клеточного некроза и связанные с ними способы EA201791289A1 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201410767595 2014-12-11
CN201410764426 2014-12-11
US201562105462P 2015-01-20 2015-01-20
US201562105475P 2015-01-20 2015-01-20
PCT/US2015/065349 WO2016094846A1 (en) 2014-12-11 2015-12-11 Inhibitors of cellular necrosis and related methods

Publications (1)

Publication Number Publication Date
EA201791289A1 true EA201791289A1 (ru) 2017-12-29

Family

ID=56108283

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201791289A EA201791289A1 (ru) 2014-12-11 2015-12-11 Ингибиторы клеточного некроза и связанные с ними способы

Country Status (14)

Country Link
US (3) US9944628B2 (ru)
EP (1) EP3229807A4 (ru)
JP (1) JP2017538712A (ru)
KR (1) KR20170123607A (ru)
CN (1) CN107530350A (ru)
AR (1) AR102981A1 (ru)
AU (1) AU2015360291A1 (ru)
CA (1) CA2970525A1 (ru)
EA (1) EA201791289A1 (ru)
IL (1) IL252827A0 (ru)
MX (1) MX2017007607A (ru)
SG (1) SG11201704764PA (ru)
TW (1) TW201632516A (ru)
WO (1) WO2016094846A1 (ru)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102316735A (zh) 2008-12-23 2012-01-11 哈佛大学校长及研究员协会 坏死性凋亡的小分子抑制剂
WO2012125544A2 (en) 2011-03-11 2012-09-20 President And Fellows Of Harvard College Necroptosis inhibitors and methods of use therefor
US9725452B2 (en) 2013-03-15 2017-08-08 Presidents And Fellows Of Harvard College Substituted indoles and pyrroles as RIP kinase inhibitors
EP3229807A4 (en) 2014-12-11 2018-10-17 President and Fellows of Harvard College Inhibitors of cellular necrosis and related methods
CN106619619A (zh) * 2017-01-06 2017-05-10 浙江大学 化合物hubin‑1在制备肝脏炎症性疾病预防和/或治疗药物中的用途
BR112019017738A2 (pt) 2017-02-27 2020-04-07 Glaxosmithkline Ip Dev Ltd combinação, composição farmacêutica, uso de uma combinação ou composição farmacêutica, método para tratar câncer em um humano, e, composto
BR112019023979A2 (pt) 2017-05-17 2020-06-09 Denali Therapeutics Inc compostos, composições e métodos
CN108191835A (zh) * 2018-01-09 2018-06-22 中国药科大学 一类新型的含吡咯环和吲哚啉结构rip1激酶抑制剂及其用途
CN110759895B (zh) * 2018-07-25 2020-10-27 浙江大学 新型rip1/rip3双靶点抑制剂及其在一药多靶疾病治疗中的用途
WO2020044206A1 (en) 2018-08-29 2020-03-05 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors for use in the treatment cancer
US20210147842A1 (en) * 2019-11-13 2021-05-20 President And Fellows Of Harvard College Methods and compositions for inhibiting necroptosis in neurovascular and/or neurodegenerative diseases or disorders
CN112263576A (zh) * 2020-09-30 2021-01-26 浙江大学 化合物zju-37在制备肝脏疾病预防和/或治疗药物中的应用

Family Cites Families (152)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1044508A (en) * 1911-04-21 1912-11-19 Ajax Forge Company Railway-frog.
BE789948A (fr) 1971-10-13 1973-04-11 Sandoz Sa Nouveaux derives du pyrazole, leur preparation et leur application comme medicaments
JPS5113156B2 (ru) 1972-10-21 1976-04-26
US4016037A (en) 1975-10-15 1977-04-05 Ajinomoto Co., Inc. Method for producing L-amino acid
US4110536A (en) 1977-04-18 1978-08-29 Miles Laboratories, Inc. Derivatives of 5-(indol-3-yl)hydantoin
DE2728523C2 (de) 1977-06-23 1986-02-27 Schering AG, 1000 Berlin und 4709 Bergkamen 4-Methyl-1,2,3-thiadiazol-5-carbonsäure-(cyclohexylmethyl)-amid, Mittel mit herbizider und wachstumsregulatorischer Wirkung enthaltend diese Verbindung sowie Verfahren zu seiner Herstellung
JPS55136279A (en) * 1979-04-09 1980-10-23 Ajinomoto Co Inc Preparation of tryptophan hydantoin
JPS5810074B2 (ja) 1979-07-18 1983-02-24 味の素株式会社 新規微生物
US4332952A (en) 1980-07-28 1982-06-01 Pfizer Inc. Hypoglycemic 5-substituted oxazolidine-2,4-diones
GB2080803B (en) 1980-07-28 1984-01-18 Pfizer Hypoglycemic 5-substituted oxazolidine-2,4-diones
DE3567460D1 (en) 1984-06-07 1989-02-16 Pfizer Ltd Dihydropyridines
JPS6122081A (ja) 1984-07-10 1986-01-30 Mitsui Toatsu Chem Inc ヒダントイン化合物の製造法
US4684735A (en) 1985-07-01 1987-08-04 Stauffer Chemical Company Promotion of raney nickel hydrogenation catalyst
JPH0623148B2 (ja) 1985-09-05 1994-03-30 三井東圧化学株式会社 Ｎ−アセチル−ｄｌ−アミノ酸の製造方法
CA1292840C (en) 1985-09-26 1991-12-03 David Harry Hawke Sequencing of peptides
JPH0659227B2 (ja) 1985-11-08 1994-08-10 三井東圧化学株式会社 Ｄ−α−アミノ酸の製造方法
JPS6225990A (ja) 1986-07-19 1987-02-03 Kanegafuchi Chem Ind Co Ltd Ｄ−α−アミノ酸類の製造方法
US4705864A (en) 1986-11-10 1987-11-10 The Standard Oil Company Aryl oxime derivatives of hydantoins
US4911931A (en) 1987-08-03 1990-03-27 Baylink David J Pharmaceutical combination for treatment of bone-wasting diseases
JP2661111B2 (ja) 1988-03-09 1997-10-08 三菱化学株式会社 Ｄ−Ｎ−カルバミル−α−アミノ酸の製造法
US4868061A (en) 1988-05-19 1989-09-19 The Standard Oil Company Olefinic aryl oxime derivatives of hydantoins
IE940525L (en) 1988-05-25 1989-11-25 Warner Lambert Co Known and selected novel arylmethylenyl derivatives of¹thiazolidinones, imidazolidinones and oxazolidinones useful¹as antiallergy agents and antiinflammatory agents
JPH0219363A (ja) 1988-07-06 1990-01-23 Fujisawa Pharmaceut Co Ltd イミダゾリジン誘導体
WO1990004183A1 (en) 1988-10-07 1990-04-19 Commonwealth Scientific And Industrial Research Organisation Method for preparation of thiohydantoins and for protein sequence analysis
EP0377083B1 (de) 1989-01-02 1993-09-22 Rütgerswerke Aktiengesellschaft Verfahren zur Herstellung von L-alpha-Aminosäuren
JPH054910A (ja) 1990-07-31 1993-01-14 Nikka Chem Co Ltd 化粧料組成物
EP0547178A4 (en) 1990-08-31 1994-07-06 Warner Lambert Co Novel cholecystokinin antagonists, their preparation and therapeutic use
JP2651755B2 (ja) 1991-03-01 1997-09-10 富士写真フイルム株式会社 ハロゲン化銀カラー写真感光材料
NZ286242A (en) 1991-03-26 1997-11-24 Csl Ltd Use of veterinary implant as a single dose vaccination system: rupturable polymer film coating around core of active agent and water soluble excipient
US5693643A (en) 1991-09-16 1997-12-02 Merck & Co., Inc. Hydantoin and succinimide-substituted derivatives of spiroindanylcamphorsulfonyl oxytocin antagonists
EP0533243B1 (en) 1991-09-16 1997-12-17 Merck & Co. Inc. Hydantoin and succinimide-substituted spiroindanylcamphorsulfonyl derivatives
CA2083891A1 (en) 1991-12-03 1993-06-04 Angus Murray Macleod Heterocyclic compounds, compositions containing them and their use in therapy
JP3163361B2 (ja) 1992-03-12 2001-05-08 味の素株式会社 ５−アルキルヒダントイン誘導体の製造法
ATE170516T1 (de) 1992-07-14 1998-09-15 Nippon Chemiphar Co Alkylendiaminderivate
US5574030A (en) 1992-07-14 1996-11-12 Nippon Chemiphar Co., Ltd. N-aminoalkyl-substituted nitrogen-containing five membered heterocyclic compounds
US5830854A (en) 1992-12-14 1998-11-03 Merck Sharp & Dohme, Limited Method of treating cystic fibrosis using a tachykinin receptor antagonist
US5338859A (en) 1993-02-12 1994-08-16 Hoechst Celanese Corporation Process for the production of calcium salts of hydantoic acids
EP0640594A1 (en) 1993-08-23 1995-03-01 Fujirebio Inc. Hydantoin derivative as metalloprotease inhibitor
DE69513832T2 (de) 1994-09-08 2000-04-13 Lilly Co Eli Exzitatorische aminosäure-rezeptor-antagonisten
AU4424496A (en) 1995-03-27 1996-10-16 Warner-Lambert Company A method for the synthesis of mixtures of compounds
US6166054A (en) 1995-03-31 2000-12-26 Nihon Nohyaku Co., Ltd. Agricultural and horticultural disease controller and a method for controlling the diseases
US5674734A (en) 1995-05-18 1997-10-07 President And Fellows Of Harvard College Cell death protein
DE19519717C1 (de) 1995-05-30 1996-08-22 Degussa Neuer Mikroorganismus, dessen Verwendung und Verfahren zur Herstellung von L-alpha-Aminosäuren
US6846839B1 (en) 1995-06-07 2005-01-25 Sugen, Inc. Methods for treating diseases and disorders related to unregulated angiogenesis and/or vasculogenesis
US5962478A (en) 1995-09-19 1999-10-05 Margolin; Solomon B. Inhibition of tumor necrosis factor α
WO1997015586A1 (en) 1995-10-23 1997-05-01 Tularik, Inc. Rip: novel human protein involved in tumor necrosis factor signal transduction, and screening assays
EP0907643B1 (en) 1996-04-24 2003-01-15 Novo Nordisk A/S Compounds with growth hormone releasing properties
DE69722019T2 (de) 1996-09-30 2003-11-27 Nihon Nohyaku Co Ltd 1,2,3-thiadiazol-derivate und ihre salze, mittel zur kontrolle von krankheiten in landwirtschaft und gartenbau und eine methode zu ihrer anwendung
US5859190A (en) 1997-02-04 1999-01-12 Trega Biosciences, Inc. Combinatorial libraries of hydantoin and thiohydantoin derivatives, methods of making the libraries and compounds therein
BR9811260A (pt) 1997-03-03 2000-08-08 Boehringer Ingelheim Pharma Pequenas moléculas úteis no tratamento de doença inflamatória
IL126024A0 (en) 1998-03-19 1999-05-09 Yeda Res & Dev Modulators of the function of receptors of the tnf/ngf receptor family and other proteins
EP0976326B1 (en) 1998-07-30 2003-05-02 Nihon Nohyaku Co., Ltd. Fungicidal composition containing a 1,2,3-tiadiazole derivative and its use
ATE240944T1 (de) 1998-09-22 2003-06-15 Degussa Verfahren zur herstellung von imidazolidin-2,4- dionen
US6020198A (en) 1998-09-25 2000-02-01 Isis Pharmaceuticals Inc. Antisense modulation of RIP-1 expression
AU754989B2 (en) 1998-11-16 2002-11-28 Nippon Zoki Pharmaceutical Co., Ltd. A therapeutic agent for intractable vasculitis
WO2001007048A1 (en) 1999-07-21 2001-02-01 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammatory disease
WO2001007044A1 (en) 1999-07-21 2001-02-01 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammatory disease
WO2001028493A2 (en) 1999-10-15 2001-04-26 President And Fellows Of Harvard College Small molecule inhibitors of necrosis
US6756394B1 (en) 1999-10-15 2004-06-29 President And Fellow Of Harvard College Small molecule inhibitors of necrosis
US6706766B2 (en) 1999-12-13 2004-03-16 President And Fellows Of Harvard College Small molecules used to increase cell death
AU2001244596A1 (en) 2000-03-30 2001-10-15 Rei Asakai Indolylpyrrole derivatives and cell death inhibitors
US20020155172A1 (en) 2000-04-07 2002-10-24 Junying Yuan Methods and compounds for decreasing cell toxicity or death
GB0011071D0 (en) 2000-05-08 2000-06-28 Novartis Ag Organic compounds
US6846643B2 (en) 2000-08-14 2005-01-25 Boehringer Ingelheim Pharmaceuticals, Inc. Methods and molecules useful for identifying molecules that bind LFA-1 and for determining receptor occupancy
US20020064736A1 (en) 2000-09-27 2002-05-30 Fuji Photo Film Co., Ltd. Dye-forming coupler, silver halide photographic light-sensitive material, and method for producing an azomethine dye
JP2002145192A (ja) 2000-11-07 2002-05-22 Yamaha Motor Co Ltd 水上乗物の燃料タンク構造
JP4529338B2 (ja) 2001-03-08 2010-08-25 味の素株式会社 ヒダントイナーゼをコードするｄｎａ、ｎ−カルバミル−ｌ−アミノ酸ハイドロラーゼをコードするｄｎａ、組み換えｄｎａ、形質転換された細胞、タンパク質の製造方法および光学活性アミノ酸の製造方法
EP1429763B1 (en) 2001-09-14 2007-05-30 Novo Nordisk A/S NOVEL LIGANDS FOR THE HisB10 Zn2+ SITES OF THE R-STATE INSULIN HEXAMER
AU2002363655A1 (en) 2001-11-14 2003-05-26 Novartis Ag Non-peptide somatostatin receptor ligands
MXPA04004830A (es) 2001-11-22 2004-07-30 Ono Pharmaceutical Co Compuestos derivados de piperidin-2-ona, y composiciones farmaceuticas que los contienen como ingredientes activos.
US6797708B2 (en) 2001-12-03 2004-09-28 Wyeth Inhibitors of cytosolic phospholipase A2
JP3659224B2 (ja) 2001-12-26 2005-06-15 村田機械株式会社 インターネットファクシミリ装置
AU2002359359A1 (en) 2001-12-28 2003-07-24 Somatocor Pharmaceuticals, Inc. Imidazolidin-2,4-dione derivatives as non-peptide somatostatin receptor ligands
AU2003215077A1 (en) 2002-02-11 2003-09-04 Wyeth Solution structure of rip dd and uses therof
WO2004023146A2 (en) 2002-09-06 2004-03-18 Mount Sinai Hospital Methods for assaying protein-protein interactions
JP2006517092A (ja) 2002-11-27 2006-07-20 アルテシアン セラピューティック，インコーポレイティド 心不全遺伝子の決定及び治療薬スクリーニング
ES2297227T3 (es) 2002-12-20 2008-05-01 Novo Nordisk A/S Composiciones farmaceuticas conteniendo insulina y ligandos del hexamero de insulina.
FR2850652B1 (fr) 2003-01-31 2008-05-30 Aventis Pharma Sa Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
GB0302671D0 (en) 2003-02-06 2003-03-12 Astrazeneca Ab Pharmaceutical formulations
US7320986B2 (en) 2003-03-07 2008-01-22 Abbott Labortories Fused tri and tetra-cyclic pyrazole kinase inhibitors
WO2004080480A1 (en) 2003-03-11 2004-09-23 Novo Nordisk A/S Pharmaceutical preparations comprising acid-stabilised insulin
EP1605967A1 (en) 2003-03-13 2005-12-21 Novo Nordisk A/S Novel nph insulin preparations
EP3081214A3 (en) 2003-08-29 2016-11-16 The Brigham And Women's Hospital, Inc. Inhibitors of cellular necrosis
JP4452914B2 (ja) 2003-09-08 2010-04-21 味の素株式会社 新規トランスポータタンパク質
WO2005028664A2 (en) 2003-09-17 2005-03-31 University Of Massachusetts Modulation of programmed necrosis
DE10342839A1 (de) 2003-09-17 2005-04-28 Symrise Gmbh & Co Kg Thiohydantoine zur Aufhellung von Haut oder Haar
US6887993B1 (en) 2003-11-12 2005-05-03 Kosan Biosciences, Inc. 11-O-methylgeldanamycin compounds
WO2005080372A1 (en) 2004-02-19 2005-09-01 Bayer Healthcare Ag Dihydropyridinone derivatives
US7935510B2 (en) 2004-04-30 2011-05-03 Intrexon Corporation Mutant receptors and their use in a nuclear receptor-based inducible gene expression system
GB0410379D0 (en) 2004-05-11 2004-06-16 Univ Leicester Treatment of cancer
ES2697524T3 (es) 2004-07-30 2019-01-24 Exelixis Inc Derivados de pirrol como agentes farmacéuticos
EP1851213A4 (en) 2005-02-10 2010-10-06 Merck Sharp & Dohme INHIBITORS OF MITOTIC KINESINE
WO2006103995A1 (ja) 2005-03-25 2006-10-05 Kaneka Corporation 光学活性α－アミノ酸誘導体の製造方法
KR20080039982A (ko) 2005-08-25 2008-05-07 쉐링 코포레이션 작용 선택적 알파2ｃ 아드레날린성 수용체 효능제로서의이미다졸 유도체
CN101304976A (zh) * 2005-10-11 2008-11-12 因特蒙公司 病毒复制抑制剂
EP1951706A1 (en) 2005-11-01 2008-08-06 Janssen Pharmaceutica N.V. Dihydroisoindolones as allosteric modulators of glucokinase
EP1968583A4 (en) 2005-12-20 2010-09-15 Harvard College COMPOUNDS, TESTS AND METHODS OF TREATMENT
AR056882A1 (es) 2006-02-01 2007-10-31 Bayer Cropscience Sa Derivados del fungicida n- cicloalquil- bencil- amida
US8007790B2 (en) 2006-04-03 2011-08-30 Stowers Institute For Medical Research Methods for treating polycystic kidney disease (PKD) or other cyst forming diseases
AU2007274283A1 (en) 2006-07-13 2008-01-17 4Sc Ag Benzopyranopyrazoles
CA2666060C (en) 2006-10-10 2015-02-03 President And Fellows Of Harvard College Thieno[2,3-d]pyrimidin-4-one compounds and methods of using the same
EP2150538B1 (en) * 2007-06-06 2012-03-28 DSM Sinochem Pharmaceuticals Netherlands B.V. Novel 5-substituted hydantoins
EP2192838A4 (en) 2007-08-15 2011-07-27 Harvard College HETEROCYCLIC NEKROPTOSIS HEMMER
CA2708281A1 (en) 2007-12-11 2009-08-27 Viamet Pharmaceuticals, Inc. Metalloenzyme inhibitors using metal binding moieties in combination with targeting moieties
CA2714183A1 (en) 2008-02-14 2009-08-20 F. Hoffmann-La Roche Ag Prediction of bone marrow toxicity
US20120061324A1 (en) * 2008-03-28 2012-03-15 Global Material Technologies, Inc. Element removal process and apparatus
US8304421B2 (en) 2008-09-30 2012-11-06 Vanderbilt University Indole compounds and their use as radiation sensitizing agents and chemotherapeutic agents
WO2010075290A1 (en) 2008-12-22 2010-07-01 President And Fellows Of Harvard College Unsaturated heterocyclic inhibitors of necroptosis
CN102316735A (zh) 2008-12-23 2012-01-11 哈佛大学校长及研究员协会 坏死性凋亡的小分子抑制剂
JP2010202575A (ja) 2009-03-03 2010-09-16 Takeda Chem Ind Ltd 複素環化合物
DE102009002044A1 (de) 2009-03-31 2010-10-07 Evonik Degussa Gmbh Dipeptide als Futtermitteladditive
JP5332882B2 (ja) 2009-04-30 2013-11-06 豊田合成株式会社 半導体発光素子
JP2010275229A (ja) 2009-05-28 2010-12-09 Ikutoku Gakuen ヒダントイン誘導体
CA2784807C (en) 2009-12-29 2021-12-14 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
AR080234A1 (es) 2010-02-25 2012-03-21 Marrone Bio Innovations Inc Cepa bacteriana aislada del genero burkholderia y metabolitos pesticidas del mismo
JP2013522292A (ja) 2010-03-16 2013-06-13 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド インダゾール化合物およびそれらの使用
JP2013523766A (ja) 2010-03-31 2013-06-17 グラクソ グループ リミテッド キナーゼ阻害剤としてのイミダゾリル‐イミダゾール
US20130137642A1 (en) 2010-04-23 2013-05-30 Demetrios Vavvas Methods and compositions for preserving photoreceptor and retinal pigment epithelial cells
WO2012061045A2 (en) 2010-11-01 2012-05-10 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving retinal ganglion cells
JP2014509852A (ja) 2011-03-07 2014-04-24 ジ・オハイオ・ステート・ユニバーシティ マイクロＲＮＡ−１５５（ｍｉＲ−１５５）により誘導される変異誘発活性は炎症および癌を結び付ける
WO2012154858A1 (en) 2011-05-09 2012-11-15 Whitehead Institute For Biomedical Research Chaperone interaction assays and uses thereof
CN102850252B (zh) 2011-06-30 2014-08-13 山东大学 一种3,5,5’-三取代乙内酰脲的制备方法
WO2013013826A1 (en) 2011-07-27 2013-01-31 Friedrich-Alexander-Universität Erlangen-Nürnberg Necroptosis inhibitors for the treatment of inflammatory diseases of the gastrointestinal tract
US9314328B2 (en) 2011-08-16 2016-04-19 W. L. Gore & Associates, Inc. Branched stent graft device and deployment
KR20160054627A (ko) 2011-08-27 2016-05-16 마론 바이오 이노베이션스, 인코포레이티드 부르크홀데리아 속의 단리된 박테리아 균주 및 그로부터의 살충 대사물-제제 및 용도
EP2773341A2 (en) * 2011-10-21 2014-09-10 Massachusetts Eye & Ear Infirmary Compositions comprising necrosis inhibitors, such as necrostatins, alone or in combination, for promoting axon regeneration and nerve function, thereby treating cns disorders
US8492556B2 (en) 2011-11-10 2013-07-23 Allergan, Inc. 2,5-Dioxoimidazolidin-1-yl-3-phenylurea derivatives as formyl peptide receptor like-1 (FPRL-1) receptor modulators
SG11201406837TA (en) 2012-05-04 2014-11-27 Novartis Ag Biomarkers for iap inhibitor therapy
SG11201408280YA (en) 2012-06-26 2015-01-29 Biovalence Sdn Bhd Anticancer treatment
US20150185215A1 (en) 2012-07-02 2015-07-02 Cell Assay Innovations, Inc. Cell-Based Assays For Post-Translational Enzyme Activity
JPWO2014126127A1 (ja) 2013-02-13 2017-02-02 国立大学法人北海道大学 ネクロプトーシス関連疾患の治療用医薬組成物及びその有効成分のスクリーニング方法
TWI637951B (zh) 2013-02-15 2018-10-11 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類
JP2016525873A (ja) 2013-02-27 2016-09-01 ザ・ブロード・インスティテュート・インコーポレイテッド Ｔ細胞バランス遺伝子発現、組成物およびその使用方法
WO2014152182A1 (en) 2013-03-15 2014-09-25 President And Fellows Of Harvard College Deuterated heterocyclic inhibitors of necroptosis
US9725452B2 (en) 2013-03-15 2017-08-08 Presidents And Fellows Of Harvard College Substituted indoles and pyrroles as RIP kinase inhibitors
HUE034308T2 (en) 2013-03-21 2018-02-28 Sanofi Aventis Deutschland Preparation of hydantoin-containing peptide products
US20160051629A1 (en) 2013-04-15 2016-02-25 Yeda Research And Development Co. Ltd. Inhibition of rip kinases for treating lysosomal storage diseases
GB201316651D0 (en) 2013-09-19 2013-11-06 Univ Southampton Asthma
JP6389896B2 (ja) 2013-09-23 2018-09-12 カール・ツァイス・エスエムティー・ゲーエムベーハー 多層ミラー
EP2857839A1 (en) 2013-10-01 2015-04-08 AIT Austrian Institute of Technology GmbH Breast cancer diagnostic method and means
WO2015077709A2 (en) 2013-11-22 2015-05-28 World Biotechnology LLC Method for harvesting organic compounds from genetically modified organisms
WO2015095449A1 (en) 2013-12-19 2015-06-25 Ptc Therapeutics, Inc. Methods for modulating the amount rna transcripts
EP3082820B1 (en) 2013-12-19 2022-07-20 PTC Therapeutics, Inc. Methods for modulating the amount of rna transcripts
US20150191511A1 (en) 2014-01-08 2015-07-09 World Biotechnology LLC Genetically Modified Organisms to Produce Organic Compounds
WO2015154197A1 (en) 2014-04-11 2015-10-15 Children's Hospital Of Eastern Ontario Research Institute Inc. Compositions and methods for glioblastoma treatment
JP2017526670A (ja) 2014-08-13 2017-09-14 マックス−プランク−ゲゼルシャフト ツール フェルデルンク デル ヴィッセンシャフテン エー．ファウ． ネクロトーシス（ｎｅｃｒｏｐｔｏｓｉｓ）の阻害による腫瘍転移の阻止
WO2016025129A1 (en) 2014-08-14 2016-02-18 Alhamadsheh Mamoun M Conjugation of pharmaceutically active agents with transthyretin ligands through adjustable linkers to increase serum half-life
WO2016044777A1 (en) 2014-09-18 2016-03-24 Abbvie Inc. Hat inhibitors and methods for their use
EP3017825A1 (en) 2014-11-06 2016-05-11 Ludwig-Maximilians-Universität München An inhibitor of the RIPK1-dependent necrosis pathway and a pharmaceutical composition comprising the same
EP3229807A4 (en) 2014-12-11 2018-10-17 President and Fellows of Harvard College Inhibitors of cellular necrosis and related methods
KR102596723B1 (ko) 2014-12-24 2023-11-01 내셔널 인스티튜트 오브 바이올로지칼 사이언시스, 베이징 괴사 억제제
JP6772141B2 (ja) 2014-12-24 2020-10-21 ナショナル・インスティチュート・オブ・バイオロジカル・サイエンシズ，ベイジン ネクローシス阻害薬

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