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
The Brigham and Women's 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)
  • 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)
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) EP2192838A4 (enExample)
JP (1) JP5645663B2 (enExample)
CA (1) CA2696349A1 (enExample)
WO (1) WO2009023272A1 (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2004315596B2 (en) * 2003-08-29 2011-11-24 President And Fellows Of Harvard College Inhibitors of cellular necrosis
CA2633500A1 (en) * 2005-12-20 2007-07-05 President And Fellows Of Harvard College Compounds, screens, and methods of treatment
WO2010075561A1 (en) 2008-12-23 2010-07-01 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
TWI471289B (zh) 2010-06-11 2015-02-01 Rhodes Technologies 使三級胺進行n-脫烷反應之方法
CA2936749C (en) 2010-06-11 2019-07-09 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
WO2012125544A2 (en) 2011-03-11 2012-09-20 President And Fellows Of Harvard College Necroptosis inhibitors and methods of use therefor
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
TWI648274B (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 (二)
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
WO2016094846A1 (en) 2014-12-11 2016-06-16 President And Fellows Of Harvard College Inhibitors of cellular necrosis and related methods
WO2016101887A1 (en) 2014-12-24 2016-06-30 National Institute Of Biological Sciences, Beijing Necrosis inhibitors
EP3224237B1 (en) * 2014-12-24 2024-09-11 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
SI3788044T1 (sl) 2018-05-03 2023-12-29 Rigel Pharmaceuticals, Inc. Spojine, ki zavirajo RIP1 in postopki za njihovo izdelavo in uporabo
PL3788045T3 (pl) 2018-05-03 2023-10-09 Rigel Pharmaceuticals, Inc. Związki hamujące rip1 oraz sposoby ich wytwarzania i wykorzystania
KR102810898B1 (ko) 2018-11-20 2025-05-23 시로낙스 엘티디 Rip1 억제제
BR112021009610A2 (pt) 2018-11-20 2021-08-10 Sironax Ltd composto, composição farmacêutica, uso de um composto ou composição, e, método de inibir necrose, ferroptose, rip1 humana ou indicações relacionadas
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
ES3043457T3 (en) 2019-09-06 2025-11-25 Rigel Pharmaceuticals Inc Rip1 inhibitory compounds and methods for making and using the same
AU2020341708B2 (en) 2019-09-06 2024-01-04 Rigel Pharmaceuticals, Inc. RIP1 inhibitory compounds and methods for making and using the same
SMT202600151T1 (it) 2019-11-07 2026-05-12 Rigel Pharmaceuticals Inc Composti eterociclici inibitori di rip1
AR121717A1 (es) 2020-04-02 2022-06-29 Rigel Pharmaceuticals Inc Inhibidores de rip1k
CN115916755A (zh) 2020-05-20 2023-04-04 维泰瑞隆有限公司 氮杂环丁烷环状脲
IL298189A (en) 2020-05-20 2023-01-01 Sironax Ltd Receptor-interacting protein 1 inhibitors including piperazine heterocyclic amide ureas
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
TWI824259B (zh) 2020-07-01 2023-12-01 美商雷傑製藥公司 Rip1k抑制劑
MX2023005822A (es) * 2020-11-19 2023-05-31 Acousia Therapeutics Gmbh Composicion de gel no acuoso.
TW202300490A (zh) 2021-03-11 2023-01-01 美商雷傑製藥公司 雜環rip1激酶抑制劑
JP2024517504A (ja) 2021-05-20 2024-04-22 シロナックス リミテッド. アゼチジン環状尿素を含めたrip1調節物質、その調製、及び使用
JP2025510009A (ja) 2022-02-28 2025-04-14 シロナックス リミテッド. Rip1調節物質、その調製、及び使用

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
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
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
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
ATE238661T1 (de) * 1998-07-30 2003-05-15 Nihon Nohyaku Co Ltd Fungizide zusammensetzung enthaltend ein 1,2,3- thiadiazolderivat sowie deren verwendung
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
CN100369898C (zh) * 2002-02-12 2008-02-20 史密丝克莱恩比彻姆公司 用作p38抑制剂的烟酰胺衍生物
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
AU2004315596B2 (en) * 2003-08-29 2011-11-24 President And Fellows Of Harvard College Inhibitors of cellular necrosis
WO2005100342A1 (en) * 2004-03-26 2005-10-27 Vertex Pharmaceuticals, Incorporated Pyridine inhibitors of erk2 and uses thereof
PT1773768T (pt) * 2004-07-30 2018-11-30 Exelixis Inc Derivados de pirrol como agentes farmacêuticos
AU2006208045B2 (en) * 2005-01-25 2012-08-30 Synta Pharmaceuticals Corp. Compounds for inflammation and immune-related uses
US7786040B2 (en) * 2005-02-24 2010-08-31 Nihon Nohyaku Co., Ltd. 4-cyclopropyl-1,2,3,-thiadiazole compound, agrohorticultural plant disease controlling agent and method of using the same
CA2633500A1 (en) 2005-12-20 2007-07-05 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
AU2007211276B2 (en) * 2006-01-31 2013-06-06 Synta Pharmaceuticals Corp. Pyridylphenyl compounds for inflammation and immune-related uses
CA2645434A1 (en) * 2006-03-20 2007-09-27 Synta Pharmaceutical Corp. Benzoimidazolyl-parazine compounds for inflammation and immune-related uses
AU2007230911A1 (en) * 2006-03-23 2007-10-04 Synta Pharmaceuticals Corp. Benzimidazolyl-pyridine compounds for inflammation and immune-related uses
JP5366812B2 (ja) 2006-10-10 2013-12-11 プレジデント アンド フェロウズ オブ ハーバード カレッジ 化合物、スクリーニング、および治療方法
CL2008000835A1 (es) 2007-03-23 2008-10-03 Icagen Inc Pfizer Ltd Compuestos derivados de sulfonamidas, inhibidores de los canales de calcio; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del dolor, sindrome de intestino irritable, enfermedad de crohn, taquiarritm
WO2010075290A1 (en) 2008-12-22 2010-07-01 President And Fellows Of Harvard College Unsaturated heterocyclic inhibitors of necroptosis
WO2010075561A1 (en) 2008-12-23 2010-07-01 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis

Also Published As

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

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
GB2163746A (en) Ethylenediamine monoamide derivatives
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
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