EA199800184A1 - Соединение бензимидазола - Google Patents

Соединение бензимидазола

Info

Publication number
EA199800184A1
EA199800184A1 EA199800184A EA199800184A EA199800184A1 EA 199800184 A1 EA199800184 A1 EA 199800184A1 EA 199800184 A EA199800184 A EA 199800184A EA 199800184 A EA199800184 A EA 199800184A EA 199800184 A1 EA199800184 A1 EA 199800184A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
dna
group
benzimidazole
chchoh
Prior art date
Application number
EA199800184A
Other languages
English (en)
Other versions
EA000999B1 (ru
Inventor
Роджер Джон Гриффин
Элан Хилари Калверт
Никола Джэйн Кертин
Дэвид Ричард Ньюэлл
Бернард Томас Голдинг
Original Assignee
Ньюкастл Юниверсити Венчерз Лимитед
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
Priority claimed from GBGB9515843.2A external-priority patent/GB9515843D0/en
Priority claimed from GBGB9611245.3A external-priority patent/GB9611245D0/en
Application filed by Ньюкастл Юниверсити Венчерз Лимитед filed Critical Ньюкастл Юниверсити Венчерз Лимитед
Publication of EA199800184A1 publication Critical patent/EA199800184A1/ru
Publication of EA000999B1 publication Critical patent/EA000999B1/ru

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/10Radicals substituted by halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/12Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/14Radicals substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Data Exchanges In Wide-Area Networks (AREA)
  • Saccharide Compounds (AREA)

Abstract

В настоящем изобретении раскрыт ряд соединений бензимидазол-4-карбоксамида (1)которые являются сильнодействующими ингибиторами поли(ADP-рибоза)полимеразы-фермента, восстанавливающими ДНК или PARP фермент (ЕС 2.4.2.30), и которые являются полезными терапевтическими соединениями для использования в сочетании с ДНК-повреждающими цитотоксическими лекарственными средствами или радиотерапией для того, чтобы усилить действия последних. В формуле (1) R и R', каждый независимо может быть выбран из водорода, алкильной, гидроксиалкильной (например, CHCHOH), ацильной (например, ацетил или бензоил) или необязательно замещенной арильной (например, фенил) или аралкильной (например, бензил или карбоксибензил) группы. R обычно представляет замещенную фенильную группу в большинстве предпочтительных соединений. Соединения можно использовать также в форме фармацевтически приемлемых солей или пролекарств.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA199800184A 1995-08-02 1996-07-30 Соединение бензимидазола EA000999B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9515843.2A GB9515843D0 (en) 1995-08-02 1995-08-02 Benzimidazole compounds
GBGB9611245.3A GB9611245D0 (en) 1996-05-30 1996-05-30 Benzimidazole compounds
PCT/GB1996/001832 WO1997004771A1 (en) 1995-08-02 1996-07-30 Benzimidazole compounds

Publications (2)

Publication Number Publication Date
EA199800184A1 true EA199800184A1 (ru) 1998-10-29
EA000999B1 EA000999B1 (ru) 2000-08-28

Family

ID=26307504

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199800184A EA000999B1 (ru) 1995-08-02 1996-07-30 Соединение бензимидазола

Country Status (26)

Country Link
US (2) US6100283A (ru)
EP (1) EP0841924B1 (ru)
JP (1) JPH11510154A (ru)
KR (1) KR100447539B1 (ru)
CN (1) CN1159007C (ru)
AP (1) AP866A (ru)
AT (1) ATE225173T1 (ru)
AU (1) AU714873B2 (ru)
BR (1) BR9610051A (ru)
CA (1) CA2225465A1 (ru)
CZ (1) CZ30398A3 (ru)
DE (1) DE69624115T2 (ru)
DK (1) DK0841924T3 (ru)
EA (1) EA000999B1 (ru)
ES (1) ES2183004T3 (ru)
HU (1) HUP9901092A3 (ru)
IL (1) IL123147A (ru)
MX (1) MX9800927A (ru)
NO (1) NO317033B1 (ru)
NZ (1) NZ313713A (ru)
OA (1) OA10661A (ru)
PL (1) PL324869A1 (ru)
PT (1) PT841924E (ru)
SK (1) SK13598A3 (ru)
TR (1) TR199800127T1 (ru)
WO (1) WO1997004771A1 (ru)

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2776291B1 (fr) * 1998-03-18 2000-06-16 Pf Medicament Nouveaux derives bis-benzamides, leur procede de fabrication, les compositions pharmaceutiques les contenant et leur utilisation comme medicament
US6919366B2 (en) * 1998-05-22 2005-07-19 Avanir Pharmaceuticals Benzimidazole derivatives as modulators of IgE
US6911462B2 (en) * 1998-05-22 2005-06-28 Avanir Pharmaceuticals Benzimidazole compounds for regulating IgE
UA65635C2 (ru) 1998-09-03 2004-04-15 Н-Гене Кутато Кфт. НЕНАСЫЧЕННЫЕ ПРОИЗВОДНЫЕ ГИДРОКСИМОВОЙ КИСЛОТЫ, ИМЕЮЩИЕ СВОЙСТВА ИНГИБИТОРОВ NAD<sup>+-ADP-РИБОЗИЛТРАНСФЕРАЗЫ
BR9915013A (pt) 1998-11-03 2001-08-07 Basf Ag Composto, uso dos mesmos, processo para preparar os mesmos, droga, e, método para detecção in vitro para inibidores parp
BR9915381A (pt) * 1998-11-17 2001-08-14 Basf Ag Uso de um composto, e, composto
DE19916460B4 (de) * 1999-04-12 2006-12-21 Abbott Gmbh & Co. Kg Substituierte Benzimidazole, deren Herstellung und Anwendung
HUP0200749A3 (en) 1998-11-27 2003-03-28 Basf Ag Substituted benzimidazoles and their use as parp inhibitors and process for their preparation
PT1140936E (pt) * 1999-01-11 2004-06-30 Agouron Pharma Inibidores triciclicos de poli(adp-ribose) polimerases
FR2788518B1 (fr) * 1999-01-14 2001-03-02 Centre Nat Rech Scient Nouveaux carbamates actives stables, leur procede de preparation et leur utilisation pour la preparation d'urees
DE19918211A1 (de) 1999-04-22 2000-10-26 Basf Ag Cycloalkylsubstituierte Benzimidazole, deren Herstellung und Anwendung
DE19920936A1 (de) * 1999-05-07 2000-11-09 Basf Ag Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung
ECSP003637A (es) * 1999-08-31 2002-03-25 Agouron Pharma Inhibidores triciclicos de poli (adp-ribosa) polimerasas
AU7314200A (en) * 1999-09-17 2001-04-24 Yamanouchi Pharmaceutical Co., Ltd. Benzimidazole derivatives
DE19946289A1 (de) * 1999-09-28 2001-03-29 Basf Ag Benzodiazepin-Derivate, deren Herstellung und Anwendung
US6759425B2 (en) 1999-10-21 2004-07-06 Avanir Pharmaceuticals Benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
IT1315267B1 (it) * 1999-12-23 2003-02-03 Novuspharma Spa Derivati di 2-(1h-indol-3-il)-2-oxo-acetammidi ad attivita'antitumorale
DE50112961D1 (de) * 2000-02-01 2007-10-18 Abbott Gmbh & Co Kg Heterozyklische verbindungen und deren anwendung als parp-inhibitoren
DE10021468A1 (de) * 2000-05-04 2001-11-08 Basf Ag Verwendung von PARP-Inhibitoren in kosmetischen Zubereitungen
DE10022925A1 (de) * 2000-05-11 2001-11-15 Basf Ag Substituierte Indole als PARP-Inhibitoren
ATE369853T1 (de) * 2001-03-12 2007-09-15 Avanir Pharmaceuticals Benzimidazolderivate zur ige-modulierung und zellproliferationshemmung
US7072771B2 (en) * 2001-06-07 2006-07-04 University Of Kentucky Research Foundation Selective PARP-1 targeting for designing chemo/radio sensitizing agents
AU2002334355A1 (en) * 2001-09-06 2003-03-18 Prochon Biotech Ltd. Protein tyrosine kinase inhibitors
DE10201240A1 (de) * 2002-01-15 2003-07-24 Bayer Ag Substituierte Alkyluracile und ihre Verwendung
TW200304820A (en) * 2002-03-25 2003-10-16 Avanir Pharmaceuticals Use of benzimidazole analogs in the treatment of cell proliferation
US20040034078A1 (en) * 2002-06-14 2004-02-19 Agouron Pharmaceuticals, Inc. Benzimidazole inhibitors of poly(ADP-ribosyl) polymerase
TWI276631B (en) * 2002-09-12 2007-03-21 Avanir Pharmaceuticals Phenyl-aza-benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
AU2003270426A1 (en) 2002-09-12 2004-04-30 Avanir Pharmaceuticals PHENYL-INDOLE COMPOUNDS FOR MODULATING IgE AND INHIBITING CELLULAR PROLIFERATION
JP2006515013A (ja) * 2003-01-23 2006-05-18 クリスタルジェノミクス、インコーポレイテッド グリコーゲン合成酵素キナーゼ3β活性抑制剤、組成物及びその製造方法
CA2522562C (en) * 2003-04-17 2013-09-03 Janssen Pharmaceutica N.V. 2-phenyl-benzimidazol and 2-phenyl-imidazo-`4,5!-pyridine derivatives as checkpoint kinase cds1 (chk2) inhibitors for the treatment of cancer
JP2007501618A (ja) * 2003-08-08 2007-02-01 アバニール・ファーマシューティカルズ タンパク質輸送の選択的薬理学的阻害、および関連した、ヒト疾患を治療する方法
US7728026B2 (en) 2005-04-11 2010-06-01 Abbott Laboratories, Inc. 2-substituted-1 h-benzimidazile-4-carboxamides are PARP inhibitors
TWI375673B (en) 2005-04-11 2012-11-01 Abbott Lab 1h-benzimidazole-4-carboxamides substituted with a quaternary carbon at the 2-position are potent parp inhibitors
SG164368A1 (en) 2005-07-18 2010-09-29 Bipar Sciences Inc Treatment of cancer
CA2629376C (en) 2005-11-14 2015-06-09 Centre National De La Recherche Scientifique - Cnrs Inhibitors of parp activity and uses thereof
TW200736229A (en) 2005-11-15 2007-10-01 Abbott Lab Substituted 1H-benzimidazole-4-carboxamides are potent PARP inhibitors
WO2007084532A2 (en) * 2006-01-17 2007-07-26 Abbott Laboratories Combination therapy with parp inhibitors
US20080280867A1 (en) * 2006-01-17 2008-11-13 Abbott Laboratories Combination therapy with parp inhibitors
US20090029966A1 (en) * 2006-01-17 2009-01-29 Abbott Laboratories Combination therapy with parp inhibitors
US20080146638A1 (en) * 2006-01-17 2008-06-19 Abbott Laboratories Combination therapy with parp inhibitors
US20080293795A1 (en) * 2006-01-17 2008-11-27 Abbott Laboratories Combination therapy with parp inhibitors
CA2647545C (en) * 2006-04-03 2016-02-23 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Amide substituted indazole and benzotriazole derivatives as poly(adp-ribose)polymerase (parp) inhibitors
ATE553104T1 (de) 2006-05-02 2012-04-15 Abbott Lab Substituierte 1h-benzimidazol-4-carboxamide als potente parp-hemmer
US20080262062A1 (en) * 2006-11-20 2008-10-23 Bipar Sciences, Inc. Method of treating diseases with parp inhibitors
WO2008030891A2 (en) 2006-09-05 2008-03-13 Bipar Sciences, Inc. Inhibition of fatty acid synthesis by parp inhibitors and methods of treatment thereof
CA2662517A1 (en) 2006-09-05 2008-03-13 Jerome Moore Treatment of cancer
US20080076778A1 (en) * 2006-09-05 2008-03-27 Bipar Sciences, Inc. Methods for designing parp inhibitors and uses thereof
PL2109608T3 (pl) 2007-01-10 2011-08-31 Msd Italia Srl Indazole podstawione grupą amidową jako inhibitory polimerazy poli(ADP-rybozy)-(PARP)
US8067613B2 (en) 2007-07-16 2011-11-29 Abbott Laboratories Benzimidazole poly(ADP ribose)polymerase inhibitors
US20090062268A1 (en) * 2007-08-27 2009-03-05 Lead Therapeutics, Inc. Novel inhibitors of poly(adp-ribose)polymerase (parp)
JP2011500684A (ja) * 2007-10-19 2011-01-06 バイパー サイエンシズ,インコーポレイティド ベンゾピロン系parp阻害剤を用いる癌の処置方法および組成物
US7732491B2 (en) 2007-11-12 2010-06-08 Bipar Sciences, Inc. Treatment of breast cancer with a PARP inhibitor alone or in combination with anti-tumor agents
NZ586675A (en) 2008-01-08 2012-04-27 Merck Sharp & Dohme Pharmaceutically acceptable salts of 2-{ 4-[(3s)-piperidin-3- yl]phenyl} -2h-indazole-7-carboxamide
CN101999002A (zh) * 2008-02-04 2011-03-30 彼帕科学公司 诊断和治疗parp-介导的疾病的方法
WO2010083199A1 (en) 2009-01-19 2010-07-22 Abbott Laboratories Benzthiazole inhibitors of poly(adp-ribose)polymerase
ES2523503T3 (es) * 2010-03-04 2014-11-26 Bayer Intellectual Property Gmbh 2-Amidobencimidazoles sustituidos con fluoroalquilo y su uso para el aumento de la tolerancia al estrés en plantas
CN102417483A (zh) * 2010-09-27 2012-04-18 中国药科大学 作为parp抑制剂的2-苯基-1h-苯并咪唑-4-甲酸酯衍生物
EP2561759A1 (en) 2011-08-26 2013-02-27 Bayer Cropscience AG Fluoroalkyl-substituted 2-amidobenzimidazoles and their effect on plant growth
CN103130723B (zh) * 2011-11-30 2015-01-14 成都地奥制药集团有限公司 一种多聚(adp-核糖)聚合酶抑制剂
CN102627610B (zh) * 2012-04-11 2014-06-25 江苏先声药物研究有限公司 一类苯并咪唑类衍生物及其应用
JP2015532650A (ja) 2012-09-05 2015-11-12 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 非生物的植物ストレスに対する活性物質としての置換された2−アミドベンズイミダゾール類、2−アミドベンゾオキサゾール類および2−アミドベンゾチアゾール類またはそれらの塩の使用
CN104140426B (zh) * 2013-05-07 2017-02-01 上海汇伦生命科技有限公司 嘧啶并咪唑类化合物、其药物组合物及其制备方法和用途
CN104230896A (zh) * 2013-06-17 2014-12-24 上海汇伦生命科技有限公司 苯并咪唑-2-哌嗪杂环类化合物、其药物组合物及其制备方法和用途
CN107556288A (zh) * 2016-07-01 2018-01-09 山东大学齐鲁医院 一种治疗转移性肿瘤的药物化合物
WO2018022851A1 (en) 2016-07-28 2018-02-01 Mitobridge, Inc. Methods of treating acute kidney injury
WO2018085359A1 (en) 2016-11-02 2018-05-11 Immunogen, Inc. Combination treatment with antibody-drug conjugates and parp inhibitors
US10933069B2 (en) * 2018-01-05 2021-03-02 Cybrexa 1, Inc. Compounds, compositions, and methods for treatment of diseases involving acidic or hypoxic diseased tissues
WO2019195658A1 (en) 2018-04-05 2019-10-10 Dana-Farber Cancer Institute, Inc. Sting levels as a biomarker for cancer immunotherapy
PE20210652A1 (es) 2018-04-13 2021-03-26 Hoffmann La Roche Moleculas de union a antigeno dirigidas a her2 que comprenden 4-1bbl
TW202116778A (zh) 2019-07-10 2021-05-01 美商斯布雷克薩二號公司 作為治療劑之細胞毒素之肽結合物
EP3996749A1 (en) 2019-07-10 2022-05-18 Cybrexa 3, Inc. Peptide conjugates of microtubule-targeting agents as therapeutics
US20220305048A1 (en) 2019-08-26 2022-09-29 Dana-Farber Cancer Institute, Inc. Use of heparin to promote type 1 interferon signaling
CN111793034B (zh) * 2020-07-24 2021-11-19 华中科技大学 苯并咪唑盐衍生物与制备抗肿瘤药物的应用
CR20230378A (es) 2021-01-08 2023-10-27 Cybrexa 2 Inc Proceso para preparar un resto enlazador de conjugados
WO2022155172A1 (en) 2021-01-13 2022-07-21 Cybrexa 3, Inc. Peptide conjugates of therapeutics

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1087561A (en) * 1963-02-16 1967-10-18 Fisons Pest Control Ltd Fluorinated benzimidazoles and compositions containing them
DE3346575A1 (de) * 1983-12-23 1985-07-04 Dr. Karl Thomae Gmbh, 7950 Biberach Neue benzimidazole, ihre herstellung und diese verbindungen enthaltende arzneimittel
DE3522230A1 (de) * 1985-06-21 1987-01-02 Thomae Gmbh Dr K Neue 2-arylimidazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
GB8822483D0 (en) * 1988-09-24 1988-10-26 Medical Res Council Developments relating to mas oncogene
GB8904174D0 (en) * 1989-02-23 1989-04-05 British Bio Technology Compounds
IE70593B1 (en) * 1989-09-29 1996-12-11 Eisai Co Ltd Biphenylmethane derivative the use of it and pharmacological compositions containing same
IL95975A (en) * 1989-10-24 1997-06-10 Takeda Chemical Industries Ltd N-benzyl- 2-alkylbenzimidazole derivatives, their production and pharmaceutical compositions containing them
CA2093125C (en) * 1990-10-02 2003-12-16 Warner-Lambert Company Angiotensin ii antagonists
US5216003A (en) * 1992-01-02 1993-06-01 G. D. Searle & Co. Diacid-containing benzimidazole compounds for treatment of neurotoxic injury
AU675484B2 (en) * 1993-03-24 1997-02-06 Neurosearch A/S Benzimidazole compounds, their use and preparation
US5824696A (en) * 1993-09-01 1998-10-20 Smithkline Beecham Corporation Medicaments
US5735973A (en) * 1993-12-20 1998-04-07 Tamura Kaken Corporation Printed circuit board surface protective agent
US5821258A (en) * 1994-12-27 1998-10-13 Mitsui Chemicals, Inc. Phenylbenzimidazole derivatives

Also Published As

Publication number Publication date
KR100447539B1 (ko) 2004-11-10
NZ313713A (en) 2001-03-30
WO1997004771A1 (en) 1997-02-13
NO317033B1 (no) 2004-07-26
DE69624115D1 (de) 2002-11-07
EP0841924B1 (en) 2002-10-02
AP866A (en) 2000-08-17
CN1159007C (zh) 2004-07-28
TR199800127T1 (xx) 1998-04-21
SK13598A3 (en) 1998-06-03
NO980414D0 (no) 1998-01-30
AU714873B2 (en) 2000-01-13
MX9800927A (es) 1998-10-31
NO980414L (no) 1998-04-02
BR9610051A (pt) 1999-12-21
CN1195985A (zh) 1998-10-14
KR19990036086A (ko) 1999-05-25
ATE225173T1 (de) 2002-10-15
US6310082B1 (en) 2001-10-30
US6100283A (en) 2000-08-08
OA10661A (en) 2002-11-25
PL324869A1 (en) 1998-06-22
ES2183004T3 (es) 2003-03-16
CA2225465A1 (en) 1997-02-13
AP9801183A0 (en) 1998-01-31
DK0841924T3 (da) 2003-02-10
IL123147A (en) 2004-02-19
EP0841924A1 (en) 1998-05-20
JPH11510154A (ja) 1999-09-07
EA000999B1 (ru) 2000-08-28
IL123147A0 (en) 1998-09-24
PT841924E (pt) 2003-02-28
CZ30398A3 (cs) 1998-06-17
HUP9901092A3 (en) 2001-11-28
HUP9901092A2 (hu) 1999-07-28
AU6624096A (en) 1997-02-26
DE69624115T2 (de) 2003-06-18

Similar Documents

Publication Publication Date Title
EA199800184A1 (ru) Соединение бензимидазола
TR200201505T2 (tr) Terapötik maddeler olarak pirazolopirimidinler
ES2135707T3 (es) Analogos de la benzamida, utiles como inhibidores de la enzima parp (adp-ribosiltransferasa, adprt) de reparacion del adn.
TR200100432T2 (tr) Hepatit C inhibitörü tri-peptidler
CR6682A (es) Inhibidores no peptidicos de la union celular dependiente de vla-4 utiles en el tratamiento de enfermedades inflamatorios, autoinmunes y respiratorias
NZ335013A (en) Compositions comprising cytosine derivatives for the treatment of cancer
TR200001279T2 (tr) Poli (ADP-riboz) polimeraz (&#34;PARP&#34;) inhibitörleri, nevral ve kardiyovasküler doku hasarının tedavisi için yöntemler ve farmasötik bileşimler.
HUP9904361A2 (hu) Izobutil-gaba és származékai alkalmazása fájdalom kezelésére
BR9712085A (pt) Inibidores de metaloprotease heterocìclicos
ES2181853T3 (es) Tratamiento del tinnitus empleando agentes neuroprotectores.
FI971934A0 (fi) Asyloituja bentsyyliglykosideja sileälihassolulisääntymisen inhibiittoreina
EA200000204A1 (ru) Производные пирролопирролона в качестве ингибиторов эластазы нейтрофилов
CO4410330A1 (es) Nuevos derivados de bencimidazol farmacologicamente activos y sus sales de adicion acida
DK1000034T3 (da) Substituerede 6-alkylphenanthridiner
ATE229800T1 (de) Guanidino proteiase inhibitoren
PT1098885E (pt) Compostos de imidazole e sua utilizacao como inibidores da desaminase de adenosina
DE69619259D1 (de) Amidin- und isothioharnstoffderivate als inhibitoren der stickstoffoxid-synthase
ES2182090T3 (es) Nuevos derivados de pirrol.
BR0014759A (pt) Inibidores de metaloprotease beta dissubstituìdos
FI880548A0 (fi) Menetelmä farmakologisesti aktiivisten 2-amino-N-(1,2-difenyylietyyli)asetamidijohdannaisten valmistamiseksi
EA200000352A1 (ru) Простые бисэфиры 1-окса, аза и тианафталин-2-онов в качестве ингибиторов фосфоламбана
ES2173634T3 (es) Compuestos heterociclicos que presentan actividad inhibidora de mmp y tnf.
MX9704299A (es) Derivados de bencimidazol.
HUP0202237A2 (hu) Amin, módosított pszeudomicin vegyületek, azokat tartalmazó gyógyászati készítmény és alkalmazásuk

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU