JP5645663B2 - ネクロトーシスのヘテロ環式抑制剤 - Google Patents

ネクロトーシスのヘテロ環式抑制剤 Download PDF

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JP5645663B2
JP5645663B2 JP2010521050A JP2010521050A JP5645663B2 JP 5645663 B2 JP5645663 B2 JP 5645663B2 JP 2010521050 A JP2010521050 A JP 2010521050A JP 2010521050 A JP2010521050 A JP 2010521050A JP 5645663 B2 JP5645663 B2 JP 5645663B2
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pharmaceutically acceptable
solvate
stereoisomer
acceptable salt
compound
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JP2010536761A (ja
JP2010536761A5 (OSRAM
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キュニー，グレゴリー，ディー．
テン，ツィン
ユアン，ジュニング
デグテレフ，アレクシ
ポルコ，ジョン，エー．，ジュニア
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Brigham and Womens Hospital Inc
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Brigham and Womens Hospital Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P9/10—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
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/06—1,2,3-Thiadiazoles; Hydrogenated 1,2,3-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three 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
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
    • C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
JP2010521050A 2007-08-15 2008-08-15 ネクロトーシスのヘテロ環式抑制剤 Active JP5645663B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US95596607P 2007-08-15 2007-08-15
US60/955,966 2007-08-15
US3817508P 2008-03-20 2008-03-20
US61/038,175 2008-03-20
PCT/US2008/009793 WO2009023272A1 (en) 2007-08-15 2008-08-15 Heterocyclic inhibitors of necroptosis

Publications (3)

Publication Number Publication Date
JP2010536761A JP2010536761A (ja) 2010-12-02
JP2010536761A5 JP2010536761A5 (OSRAM) 2011-09-29
JP5645663B2 true JP5645663B2 (ja) 2014-12-24

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Country Status (5)

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US (5) US20090099242A1 (OSRAM)
EP (2) EP3034494A1 (OSRAM)
JP (1) JP5645663B2 (OSRAM)
CA (1) CA2696349A1 (OSRAM)
WO (1) WO2009023272A1 (OSRAM)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2536622C (en) 2003-08-29 2014-02-11 The Brigham And Women's Hospital, Inc. Inhibitors of cellular necrosis
AU2006331754B9 (en) * 2005-12-20 2013-07-11 President And Fellows Of Harvard College Compounds, screens, and methods of treatment
AU2009329879A1 (en) 2008-12-23 2011-08-11 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis
US20130137642A1 (en) 2010-04-23 2013-05-30 Demetrios Vavvas Methods and compositions for preserving photoreceptor and retinal pigment epithelial cells
WO2011154826A1 (en) 2010-06-11 2011-12-15 Rhodes Technologies Process for n-dealkylation of tertiary amines
WO2011154827A2 (en) 2010-06-11 2011-12-15 Rhodes Technologies Transition metal-catalyzed processes for the preparation of n-allyl compounds and use thereof
US20140024598A1 (en) 2010-11-01 2014-01-23 Demetrios Vavvas Methods and compositions for preserving retinal ganglion cells
US9643977B2 (en) 2011-03-11 2017-05-09 President And Fellows Of Harvard College Necroptosis inhibitors and methods of use therefor
CA2888805C (en) 2011-10-21 2020-07-14 Massachusetts Eye And Ear Infirmary Methods and compositions for promoting axon regeneration and nerve function
TWI638815B (zh) 2013-02-15 2018-10-21 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（一）
WO2014145022A1 (en) 2013-03-15 2014-09-18 President And Fellows Of Harvard College Hybrid necroptosis inhibitors
CN103535358B (zh) * 2013-10-18 2015-04-15 孙家隆 一组邻位取代苯甲酰化合物的杀菌剂用途
AR102981A1 (es) 2014-12-11 2017-04-05 Harvard College Inhibidores de la necrosis celular y métodos de preparación de los mismos
CN107108467B (zh) * 2014-12-24 2022-08-19 北京生命科学研究所 细胞坏死抑制剂
EP3224245B1 (en) 2014-12-24 2018-09-12 National Institute Of Biological Sciences, Beijing Necrosis inhibitors
IL247368A0 (en) 2016-08-18 2016-11-30 Yeda Res & Dev Diagnostic and therapeutic uses of exosomes
US10975064B2 (en) 2018-05-03 2021-04-13 Rigel Pharmaceuticals, Inc. RIP1 inhibitory compounds and methods for making and using the same
JP2021523226A (ja) 2018-05-03 2021-09-02 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｒｉｐ１阻害剤化合物並びにそれを製造及び使用するための方法
CN113272272B (zh) 2018-11-20 2023-04-07 圣瑞诺有限公司 Rip1抑制剂
CN111978311B (zh) * 2019-05-21 2024-05-31 中国科学院上海有机化学研究所 一类细胞程序性坏死抑制剂及其制备方法和用途
BR112022002580A2 (pt) 2019-09-06 2022-07-19 Rigel Pharmaceuticals Inc Compostos inibitórios de rip1 e métodos para preparação e uso dos mesmos
PH12022550537A1 (en) 2019-09-06 2023-03-20 Rigel Pharmaceuticals Inc Rip1 inhibitory compounds and methods for making and using the same.
FI4055021T3 (fi) 2019-11-07 2025-12-16 Rigel Pharmaceuticals Inc Heterosyklisiä rip1:tä estäviä yhdisteitä
AR121717A1 (es) 2020-04-02 2022-06-29 Rigel Pharmaceuticals Inc Inhibidores de rip1k
EP4153582A4 (en) 2020-05-20 2024-06-19 Sironax Ltd. PIPERAZINE-TYPE CYCLIC UREAS
TWI824259B (zh) 2020-07-01 2023-12-01 美商雷傑製藥公司 Rip1k抑制劑
EP4247332A1 (en) * 2020-11-19 2023-09-27 Acousia Therapeutics GmbH Non-aqueous gel composition
TW202300490A (zh) 2021-03-11 2023-01-01 美商雷傑製藥公司 雜環rip1激酶抑制劑

Family Cites Families (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US4356787A (en) 1977-12-30 1982-11-02 Harley Richard C Float construction
CA2268129C (en) * 1996-09-30 2003-03-11 Nihon Nohyaku Co., Ltd. 1,2,3-thiadiazole derivatives or salts thereof and agrohorticultural disease controller and method for using the same
JPH10152482A (ja) * 1996-09-30 1998-06-09 Nippon Nohyaku Co Ltd １，２，３−チアジアゾール誘導体又はその塩類及び農園芸用病害防除剤ならびにその使用方法
PT957099E (pt) * 1998-04-15 2003-02-28 Pfizer Prod Inc Carboxamidas heterociclicas
EP0976326B1 (en) 1998-07-30 2003-05-02 Nihon Nohyaku Co., Ltd. Fungicidal composition containing a 1,2,3-tiadiazole derivative and its use
JP2000103710A (ja) * 1998-07-30 2000-04-11 Nippon Nohyaku Co Ltd 殺菌剤組成物及びその使用方法
US6756394B1 (en) * 1999-10-15 2004-06-29 President And Fellow Of Harvard College Small molecule inhibitors of necrosis
US6420400B1 (en) * 2000-04-07 2002-07-16 Kinetek Pharmaceuticals, Inc. Antiproliferative 1,2,3-thiadiazole compounds
DE60227655D1 (de) * 2001-04-19 2008-08-28 Dainippon Sumitomo Pharma Co Pyrrolderivat
DE10132686A1 (de) * 2001-07-05 2003-01-16 Boehringer Ingelheim Pharma Heteroarylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel
WO2003030937A1 (en) * 2001-10-05 2003-04-17 Ono Pharmaceutical Co., Ltd. Remedies for stress diseases comprising mitochondrial benzodiazepine receptor antagonists
ES2295553T3 (es) 2002-02-12 2008-04-16 Smithkline Beecham Corporation Derivados de nicotinamida utiles como inhibidores de p38.
DE10261131A1 (de) * 2002-12-20 2004-07-01 Grünenthal GmbH Substituierte 5-Aminomethyl-1H-pyrrol-2-carbonsäureamide
GB0302671D0 (en) * 2003-02-06 2003-03-12 Astrazeneca Ab Pharmaceutical formulations
WO2005000821A1 (en) * 2003-06-12 2005-01-06 Eli Lilly And Company Tachykinin receptor antagonists
CA2536622C (en) * 2003-08-29 2014-02-11 The Brigham And Women's Hospital, Inc. Inhibitors of cellular necrosis
US7462612B2 (en) * 2004-03-26 2008-12-09 Vertex Pharmaceuticals Incorporated Pyridine inhibitors of ERK2 and uses thereof
SG155188A1 (en) * 2004-07-30 2009-09-30 Exelixis Inc Pyrrole derivatives as pharmaceutical agents
CN101163478B (zh) * 2005-01-25 2013-11-27 幸讬制药公司 用于炎症及免疫相关用途之化合物
KR101206317B1 (ko) * 2005-02-24 2012-11-29 니혼노야쿠가부시키가이샤 4-시클로프로필-1,2,3-티아디아졸 화합물 및 농원예용 식물병해 방제제 그리고 그 사용 방법
AU2006331754B9 (en) * 2005-12-20 2013-07-11 President And Fellows Of Harvard College Compounds, screens, and methods of treatment
JP2007186435A (ja) * 2006-01-12 2007-07-26 Astellas Pharma Inc ニコチンアミド誘導体
JP2009524677A (ja) * 2006-01-25 2009-07-02 シンタ ファーマシューティカルズ コーポレーション 炎症および免疫関連使用用のチアゾールおよびチアジアゾール化合物
PL1984338T3 (pl) * 2006-01-31 2013-06-28 Synta Pharmaceuticals Corp Związki pirydylofenylowe do zastosowań związanych z zapaleniami i odpornością
WO2007109362A2 (en) * 2006-03-20 2007-09-27 Synta Pharmaceuticals Corp. Benzoimidazolyl-parazine compounds for inflammation and immune-related uses
JP2009530409A (ja) * 2006-03-23 2009-08-27 シンタ ファーマシューティカルズ コーポレーション 炎症及び免疫関連使用用のベンゾイミダゾリル−ピリジン化合物
US20100087453A1 (en) 2006-10-10 2010-04-08 President And Fellows Of Harvard College Compounds, screens, and methods of treatment
JP5361857B2 (ja) 2007-03-23 2013-12-04 ファイザー・リミテッド イオンチャネルの阻害剤
WO2010075290A1 (en) 2008-12-22 2010-07-01 President And Fellows Of Harvard College Unsaturated heterocyclic inhibitors of necroptosis
AU2009329879A1 (en) 2008-12-23 2011-08-11 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis

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US20090099242A1 (en) 2009-04-16
US20140128437A1 (en) 2014-05-08
EP2192838A1 (en) 2010-06-09
JP2010536761A (ja) 2010-12-02
US8278344B2 (en) 2012-10-02
CA2696349A1 (en) 2009-02-19
US20120309795A1 (en) 2012-12-06
US9108955B2 (en) 2015-08-18
US8658689B2 (en) 2014-02-25
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