CA2696349A1 - Heterocyclic inhibitors of necroptosis - Google Patents

Heterocyclic inhibitors of necroptosis Download PDF

Info

Publication number
CA2696349A1
CA2696349A1 CA2696349A CA2696349A CA2696349A1 CA 2696349 A1 CA2696349 A1 CA 2696349A1 CA 2696349 A CA2696349 A CA 2696349A CA 2696349 A CA2696349 A CA 2696349A CA 2696349 A1 CA2696349 A1 CA 2696349A1
Authority
CA
Canada
Prior art keywords
compound
pharmaceutically acceptable
stereoisomer
solvate
acceptable salt
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.)
Abandoned
Application number
CA2696349A
Other languages
English (en)
French (fr)
Inventor
Gregory D. Cuny
Xin Teng
Junying Yuan
Alexei Degterev
John A. Porco, Jr.
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boston University
Brigham and Womens Hospital Inc
Tufts University
Harvard University
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2696349A1 publication Critical patent/CA2696349A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Neurology (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)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • AIDS & HIV (AREA)
  • Vascular Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (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)
CA2696349A 2007-08-15 2008-08-15 Heterocyclic inhibitors of necroptosis Abandoned CA2696349A1 (en)

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 (1)

Publication Number Publication Date
CA2696349A1 true CA2696349A1 (en) 2009-02-19

Family

ID=40351022

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2696349A Abandoned CA2696349A1 (en) 2007-08-15 2008-08-15 Heterocyclic inhibitors of necroptosis

Country Status (5)

Country Link
US (5) US20090099242A1 (enExample)
EP (2) EP3034494A1 (enExample)
JP (1) JP5645663B2 (enExample)
CA (1) CA2696349A1 (enExample)
WO (1) WO2009023272A1 (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2384753T3 (en) 2003-08-29 2016-04-11 Brigham & Womens Hospital Hydantoin derivatives as inhibitors of cell necrosis
JP2009521454A (ja) * 2005-12-20 2009-06-04 プレジデント・アンド・フエローズ・オブ・ハーバード・カレツジ 化合物、スクリーニング、および処置方法
BRPI0923126A2 (pt) 2008-12-23 2021-09-08 President And Fellows Of Harvard College Compostos inibidores de molécula pequena de necroptose, uso e composição compreendendo os mesmos e método de diminuir necroptose
WO2011133964A2 (en) * 2010-04-23 2011-10-27 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving photoreceptor and retinal pigment epithelial cells
JP2013529595A (ja) 2010-06-11 2013-07-22 ローズ テクノロジーズ 第３級アミンのｎ−脱アルキル化方法
ES2645725T3 (es) 2010-06-11 2017-12-07 Rhodes Technologies Procesos catalizados por metales de transición para la preparación de compuestos de N-alilo y uso de los mismos
WO2012061045A2 (en) 2010-11-01 2012-05-10 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving retinal ganglion cells
WO2012125544A2 (en) 2011-03-11 2012-09-20 President And Fellows Of Harvard College Necroptosis inhibitors and methods of use therefor
JP6254090B2 (ja) * 2011-10-21 2017-12-27 マサチューセッツ・アイ・アンド・イア・インファーマリー 軸索再生および神経機能を促進するための方法および組成物
TWI648273B (zh) 2013-02-15 2019-01-21 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（三）
EP2968276A4 (en) 2013-03-15 2017-02-15 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
WO2016094846A1 (en) 2014-12-11 2016-06-16 President And Fellows Of Harvard College Inhibitors of cellular necrosis and related methods
AU2015371824B2 (en) 2014-12-24 2019-09-19 National Institute Of Biological Sciences, Beijing Necrosis inhibitors
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
IL247368A0 (en) 2016-08-18 2016-11-30 Yeda Res & Dev Diagnostic and therapeutic uses of exosomes
PT3788044T (pt) 2018-05-03 2023-08-31 Rigel Pharmaceuticals Inc Compostos inibidores de rip1 e métodos para preparar e usar os mesmos
KR102823195B1 (ko) 2018-05-03 2025-06-20 리겔 파마슈티칼스, 인크. Rip1 억제 화합물 및 이를 제조하고 사용하는 방법
CA3120726C (en) 2018-11-20 2023-05-09 Sironax Ltd Rip1 inhibitors
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
CR20220075A (es) 2019-09-06 2022-07-14 Rigel Pharmaceuticals Inc Compuestos inhibidores de rip1 y métodos para prepararlos y usarlos
EP4025574B1 (en) 2019-09-06 2025-05-07 Rigel Pharmaceuticals, Inc. Rip1 inhibitory compounds and methods for making and using the same
CN115298184B (zh) 2019-11-07 2025-01-28 里格尔药品股份有限公司 杂环rip1抑制化合物
AR121717A1 (es) 2020-04-02 2022-06-29 Rigel Pharmaceuticals Inc Inhibidores de rip1k
JP7760530B2 (ja) 2020-05-20 2025-10-27 シロナックス リミテッド． ピペラジン環状尿素類
US12612388B2 (en) 2020-05-20 2026-04-28 Sironax Ltd. Receptor-interacting protein 1 inhibitors including piperazine heterocyclic amide ureas
AR122703A1 (es) 2020-07-01 2022-09-28 Rigel Pharmaceuticals Inc Inhibidores de rip1k
EP4247332B1 (en) * 2020-11-19 2026-04-22 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
US20240294508A1 (en) 2021-05-20 2024-09-05 Sironax Ltd. Rip1 modulators including azetidine cyclic ureas, preparations, and uses thereof

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
EP0930305B1 (en) 1996-09-30 2003-05-14 Nihon Nohyaku Co., Ltd. 1,2,3-thiadiazole derivatives and salts thereof, disease controlling agents for agricultural and horticultural use, and method for the use thereof
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
EP0957099B1 (en) * 1998-04-15 2002-11-20 Pfizer Products Inc. Heterocyclic carboxamides
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
US7220773B2 (en) * 2001-04-19 2007-05-22 Dainippon Sumitomo Pharma Co., Ltd. Pyrrole derivative
DE10132686A1 (de) * 2001-07-05 2003-01-16 Boehringer Ingelheim Pharma Heteroarylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel
EP1438973A4 (en) 2001-10-05 2005-07-13 Ono Pharmaceutical Co MEANS FOR THE TREATMENT OF STRESS-RELATED DISEASES WITH MITOCHONDRIENE BENZODIAZEPINE RECEPTOR ANTAGONISTS
BRPI0307351B8 (pt) * 2002-02-12 2021-05-25 Smithkline Beecham Corp composto, composição farmacêutica, uso de um composto, e, processo para preparar um composto
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
US20060160794A1 (en) * 2003-06-12 2006-07-20 Amegadzie Albert K Tachykinin receptor antagonists
DK2384753T3 (en) 2003-08-29 2016-04-11 Brigham & Womens Hospital Hydantoin derivatives as inhibitors of cell necrosis
JP2007530595A (ja) * 2004-03-26 2007-11-01 バーテックス　ファーマシューティカルズ　インコーポレイテッド Ｅｒｋ２のピリジンインヒビターおよびそれらの使用
US8026237B2 (en) * 2004-07-30 2011-09-27 Exelixis, Inc. Pyrrole derivatives as pharmaceutical agents
US8518950B2 (en) * 2005-01-25 2013-08-27 Synta Pharmaceuticals Corp. 2-amido pyrazines for inflammation and immune related uses
EP1852428B1 (en) * 2005-02-24 2012-05-16 Nihon Nohyaku Co., Ltd. 4-cyclopropyl-1,2,3-thiadiazole compound, agrohorticultural plant disease controlling agent and method of using the same
JP2009521454A (ja) * 2005-12-20 2009-06-04 プレジデント・アンド・フエローズ・オブ・ハーバード・カレツジ 化合物、スクリーニング、および処置方法
JP2007186435A (ja) * 2006-01-12 2007-07-26 Astellas Pharma Inc ニコチンアミド誘導体
TWI444370B (zh) * 2006-01-25 2014-07-11 Synta Pharmaceuticals Corp 用於發炎及免疫相關用途之噻唑及噻二唑化合物
DK1984338T3 (da) * 2006-01-31 2013-04-22 Synta Pharmaceuticals Corp Pyridylphenylforbindelser til inflammations- og immunrelaterede anvendelser
AU2007227210A1 (en) * 2006-03-20 2007-09-27 Synta Pharmaceuticals Corp. Benzoimidazolyl-parazine compounds for inflammation and immune-related uses
CA2646886A1 (en) * 2006-03-23 2007-10-04 Synta Pharmaceuticals Corp. Benzimidazolyl-pyridine compounds for inflammation and immune-related uses
EP2076134A4 (en) 2006-10-10 2020-07-29 President and Fellows of Harvard College COMPOUNDS, SCREENS, AND TREATMENT METHODS
ATE461177T1 (de) * 2007-03-23 2010-04-15 Icagen Inc Ionenkanal-hemmer
WO2010075290A1 (en) 2008-12-22 2010-07-01 President And Fellows Of Harvard College Unsaturated heterocyclic inhibitors of necroptosis
BRPI0923126A2 (pt) 2008-12-23 2021-09-08 President And Fellows Of Harvard College Compostos inibidores de molécula pequena de necroptose, uso e composição compreendendo os mesmos e método de diminuir necroptose

Also Published As

Publication number Publication date
US8658689B2 (en) 2014-02-25
JP2010536761A (ja) 2010-12-02
WO2009023272A1 (en) 2009-02-19
US20090099242A1 (en) 2009-04-16
US20120309795A1 (en) 2012-12-06
US8278344B2 (en) 2012-10-02
EP2192838A4 (en) 2011-07-27
US9108955B2 (en) 2015-08-18
JP5645663B2 (ja) 2014-12-24
US20140128437A1 (en) 2014-05-08
EP2192838A1 (en) 2010-06-09
US20100317701A1 (en) 2010-12-16
US20160102053A1 (en) 2016-04-14
EP3034494A1 (en) 2016-06-22

Similar Documents

Publication Publication Date Title
US8278344B2 (en) Heterocyclic inhibitors of necroptosis
WO2010075290A1 (en) Unsaturated heterocyclic inhibitors of necroptosis
JP6178777B2 (ja) ネクロトーシスの小分子阻害剤
US9169234B2 (en) Sepiapterin reductase inhibitors for the treatment of pain
NZ588907A (en) Benzene or thiophene derivative and use thereof as vap-1 inhibitor
KR20010083637A (ko) 피롤로피리미디논 유도체와 이의 제조방법, 그리고 이의용도
JP2006241163A (ja) γ−セクレターゼ阻害剤としてのスルファミド
JP2022521081A (ja) Ｈｂｖ感染若しくはｈｂｖ誘導性疾患の治療において有用なアミド誘導体
GB2163746A (en) Ethylenediamine monoamide derivatives
RU2193554C2 (ru) Производные ароматических аминов, обладающих подавляющим оас действием, способ их получения и ингибитор ноас
CN109748914B (zh) 吡啶并嘧啶类化合物及其应用
LT3960B (en) Process for preparing hypoglycemic compounds
EP1966173B1 (fr) Derives heterocycliques, leur preparation et leur application en therapeutique.
EP4377298A1 (en) Protein secretion inhibitors
US20040186146A1 (en) Amide of r-2-(aminoaryl)-propionic acid for use in theprevention of leucocyte activation
AU2001246539A1 (en) Amides of R-2-(aminoaryl)-propionic acids for use in the prevention of leucocyte activation
KR20220005549A (ko) Hbv 감염 또는 hbv-유도성 질환의 치료에 유용한 아미드 유도체
CN102718727A (zh) Gk和ppar双重激动活性的芳基脲类衍生物

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20130731

FZDE Dead

Effective date: 20180504