BR0215156A - Cis-imidazolinas como inibidores de mdm 2 - Google Patents

Cis-imidazolinas como inibidores de mdm 2

Info

Publication number
BR0215156A
BR0215156A BR0215156-1A BR0215156A BR0215156A BR 0215156 A BR0215156 A BR 0215156A BR 0215156 A BR0215156 A BR 0215156A BR 0215156 A BR0215156 A BR 0215156A
Authority
BR
Brazil
Prior art keywords
mdm
cis
inhibitors
imidazolines
formula
Prior art date
Application number
BR0215156-1A
Other languages
English (en)
Inventor
Norman Kong
Emily Aijun Liu
Binh Thanh Vu
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR0215156A publication Critical patent/BR0215156A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/22Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/26Radicals substituted by carbon atoms having three bonds to hetero atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"CIS-IMIDAZOLINAS COMO INIBIDORES DE MDM 2". A presente invenção refere-se a compostos de acordo com a fórmula I e fórmula II e seus sais e ésteres farmaceuticamente aceitáveis, contendo as designações fornecidas aí e que inibem a interação de proteína MDM2 com peptídeo semelhante a p53 e tem atividade antiproliferativa (I) (II).
BR0215156-1A 2001-12-18 2002-12-09 Cis-imidazolinas como inibidores de mdm 2 BR0215156A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34172901P 2001-12-18 2001-12-18
US39087602P 2002-06-21 2002-06-21
PCT/EP2002/013905 WO2003051360A1 (en) 2001-12-18 2002-12-09 Cis-imidazolines as mdm2 inhibitors

Publications (1)

Publication Number Publication Date
BR0215156A true BR0215156A (pt) 2004-10-19

Family

ID=26992633

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0215156-1A BR0215156A (pt) 2001-12-18 2002-12-09 Cis-imidazolinas como inibidores de mdm 2

Country Status (20)

Country Link
US (1) US6617346B1 (pt)
EP (1) EP1463501B1 (pt)
JP (1) JP4361798B2 (pt)
KR (1) KR100640707B1 (pt)
CN (1) CN1604778A (pt)
AR (1) AR037882A1 (pt)
AT (1) ATE397925T1 (pt)
AU (1) AU2002361986B2 (pt)
BR (1) BR0215156A (pt)
CA (1) CA2468783A1 (pt)
DE (1) DE60227108D1 (pt)
ES (1) ES2307822T3 (pt)
MX (1) MXPA04005880A (pt)
PA (1) PA8561801A1 (pt)
PE (1) PE20030717A1 (pt)
PL (1) PL370909A1 (pt)
RU (1) RU2312101C2 (pt)
TW (1) TW200301696A (pt)
UY (1) UY27586A1 (pt)
WO (1) WO2003051360A1 (pt)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2354649C2 (ru) * 2003-06-17 2009-05-10 Ф.Хоффманн-Ля Рош Аг Цис-имидазолины в качестве ингибиторов mdm2
US7132421B2 (en) 2003-06-17 2006-11-07 Hoffmann-La Roche Inc. CIS-imidazoles
JP4814228B2 (ja) * 2004-05-18 2011-11-16 エフ.ホフマン−ラ ロシュ アーゲー 新規cis−イミダゾリン
US8022063B2 (en) * 2004-05-29 2011-09-20 7Tm Pharma A/S CRTH2 receptor ligands for medicinal uses
US7893278B2 (en) * 2004-06-17 2011-02-22 Hoffman-La Roche Inc. CIS-imidazolines
CN102627649B (zh) * 2005-02-22 2015-03-25 密执安州立大学董事会 Mdm2的小分子抑制剂以及其应用
NZ561215A (en) 2005-02-22 2010-12-24 Univ Michigan Small molecule inhibitors of MDM2 and uses thereof
NZ568285A (en) 2005-12-01 2011-08-26 Hoffmann La Roche 2,4,5-triphenyl imidazoline derivatives as inhibitors of the interaction between P53 and MDM2 proteins for use as anticancer agents
BRPI0710477A2 (pt) * 2006-01-18 2011-08-16 Hoffmann La Roche cis-4, 5- biarila - 2- imidazolinas heterocìclicas como inibidores da mdm2
US8614192B2 (en) 2006-07-28 2013-12-24 Leiden University Medical Center Method for treating ocular cancer
US8470785B2 (en) 2006-07-28 2013-06-25 St. Jude Children's Research Hospital Method for treating ocular cancer
US8222288B2 (en) 2006-08-30 2012-07-17 The Regents Of The University Of Michigan Small molecule inhibitors of MDM2 and the uses thereof
WO2008072655A1 (ja) 2006-12-14 2008-06-19 Daiichi Sankyo Company, Limited イミダゾチアゾール誘導体
US7625895B2 (en) * 2007-04-12 2009-12-01 Hoffmann-Le Roche Inc. Diphenyl-dihydro-imidazopyridinones
CA2701932C (en) 2007-10-09 2015-10-20 F. Hoffmann-La Roche Ag Chiral cis-imidazolines
US9539327B2 (en) * 2007-11-26 2017-01-10 The Research Foundation For The State University Of New York Small molecule cancer treatments that cause necrosis in cancer cells but do not affect normal cells
JPWO2009151069A1 (ja) 2008-06-12 2011-11-17 第一三共株式会社 4,7−ジアザスピロ[2.5]オクタン環構造を有するイミダゾチアゾール誘導体
BRPI1007334A2 (pt) 2009-01-16 2016-02-10 Daiichi Sankyo Co Ltd composto, inibidor, medicamento, composição farmacêutica, uso de um composto, agente anticâncer,e , método para tratar câncer.
WO2011060049A2 (en) 2009-11-12 2011-05-19 The Regents Of The University Of Michigan Spiro-oxindole mdm2 antagonists
US10159669B2 (en) * 2010-03-02 2018-12-25 Ian H. Chan Individual and combination of mdivi-1 and nutlin-3 for topical or intravitreal ophthalmic use
WO2012047587A2 (en) * 2010-09-27 2012-04-12 Serrata, Llc Mdm2 inhibitors for treatment of ocular conditions
CA2813256A1 (en) 2010-09-30 2012-04-05 St. Jude Children's Research Hospital Aryl-substituted imidazoles
FR2967072B1 (fr) 2010-11-05 2013-03-29 Univ Dundee Procede pour ameliorer la production de virus et semences vaccinales influenza
UA109464C2 (uk) 2010-11-12 2015-08-25 Дзе Ріджентс Оф Дзе Юніверсіті Оф Мічіган Спірооксіндольні антагоністи mdm2
EP2684880B1 (en) 2011-03-10 2018-02-28 Daiichi Sankyo Company, Limited Dispiropyrrolidine derivative
CA2835422C (en) 2011-05-11 2016-10-11 The Regents Of The University Of Michigan Spiro-oxindole mdm2 antagonists
KR101384683B1 (ko) * 2011-10-27 2014-04-11 한국생명공학연구원 mdm2-결합 모티프를 포함하는 펩타이드 및 이의 용도
CA2858565A1 (en) 2011-12-07 2013-07-04 Duke University Methods of identifying and using mdm2 inhibitors
TWI586668B (zh) 2012-09-06 2017-06-11 第一三共股份有限公司 二螺吡咯啶衍生物之結晶
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
WO2015116735A1 (en) 2014-01-28 2015-08-06 Mayo Foundation For Medical Education And Research Methods and combinations for killing senescent cells and for treating senescence-associated diseases and disorders
US10328058B2 (en) 2014-01-28 2019-06-25 Mayo Foundation For Medical Education And Research Treating atherosclerosis by removing senescent foam cell macrophages from atherosclerotic plaques
SG10201805670QA (en) 2014-01-28 2018-08-30 Buck Inst Res Aging Methods and compositions for killing senescent cells and for treating senescence-associated diseases and disorders
TWI750129B (zh) * 2015-08-03 2021-12-21 瑞士商諾華公司 作為血液學毒性生物標記之gdf-15
EP3440082A1 (en) 2016-04-06 2019-02-13 The Regents of The University of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
CN113788818A (zh) 2016-04-06 2021-12-14 密执安大学评议会 Mdm2蛋白质降解剂
JP2019522633A (ja) 2016-05-20 2019-08-15 ジェネンテック, インコーポレイテッド Protac抗体コンジュゲート及び使用方法
KR20200035944A (ko) 2017-06-16 2020-04-06 유니티 바이오테크놀로지, 인크. 약제학적 용도를 위해 에난티오머적으로 순수한 시스-이미다졸린 화합물을 제조하기 위한 합성 방법
CN112912143A (zh) 2018-10-08 2021-06-04 美国密歇根州立大学试剂中心 小分子mdm2蛋白降解剂
TW202200543A (zh) 2020-03-19 2022-01-01 美商凱麥拉醫療公司 Mdm2降解劑及其用途
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH02101065A (ja) * 1988-10-06 1990-04-12 Tanabe Seiyaku Co Ltd イミダゾリン誘導体及びその製法
JPH06500333A (ja) 1990-01-09 1994-01-13 イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー 殺節足動物性のピラゾリン類、ピラゾリジン類およびヒドラジン類
GB2351082A (en) * 1999-06-18 2000-12-20 Lilly Forschung Gmbh Synthesis of Cyclic Substituted Amidines

Also Published As

Publication number Publication date
AR037882A1 (es) 2004-12-09
KR20040068289A (ko) 2004-07-30
PL370909A1 (en) 2005-05-30
PE20030717A1 (es) 2003-08-28
US6617346B1 (en) 2003-09-09
PA8561801A1 (es) 2003-07-28
RU2312101C2 (ru) 2007-12-10
UY27586A1 (es) 2003-06-30
EP1463501B1 (en) 2008-06-11
RU2004122404A (ru) 2005-05-27
EP1463501A1 (en) 2004-10-06
JP4361798B2 (ja) 2009-11-11
TW200301696A (en) 2003-07-16
CA2468783A1 (en) 2003-06-26
AU2002361986A1 (en) 2003-06-30
MXPA04005880A (es) 2004-09-13
ATE397925T1 (de) 2008-07-15
JP2005515210A (ja) 2005-05-26
CN1604778A (zh) 2005-04-06
ES2307822T3 (es) 2008-12-01
KR100640707B1 (ko) 2006-10-31
DE60227108D1 (de) 2008-07-24
WO2003051360A1 (en) 2003-06-26
AU2002361986B2 (en) 2008-04-10

Similar Documents

Publication Publication Date Title
BR0215156A (pt) Cis-imidazolinas como inibidores de mdm 2
PA8561901A1 (es) Cis-imidazolinas
BR0205890A (pt) Pirazolopirimidinas como agentes terapêuticos
BR0205889A (pt) Pirazolopirimidinas como agentes tepapêuticos
CY1106522T1 (el) Ετepοκυκλικη ενωση και αντικαρκινικο μεσο που πepιεχει την ιδια ως δραστικο συστατικο
BR9815518A (pt) Agentes antibacterianos de oxazolidinona tendo funcionalidade de tiocarbonila
DE69919397D1 (de) Thrombin-inhibitoren
TR200302242T2 (tr) Protein kinaz önleyicileri olarak pirolopirimidinler
TR199902606T2 (xx) Farnesil transferaz� engelleyici kinazolinonlar.
BR0115452A (pt) Compostos tendo atividade fungicida e processos para fabricação e uso dos mesmos
ECSP034850A (es) Sal citrato de 5, 8, 14-triazatetraciclo [10.3.1.02,11.04,9] hexadeca-2 (11),3,5,7,9-pentaeno y composiciones farmaceuticas de la misma
TR200200579T2 (tr) Amino-tirazolpiridin türevleri.
BR0109836A (pt) Processo de sìntese de perindopril e de seus sais farmaceuticamente aceitáveis
BR9901491A (pt) 7-hetero-biciclo [2.2.1] - heptanos.
BR0001468A (pt) ácidos dioxiciclopentil hidroxânicos
BR0114252A (pt) Derivados de nitrosodifenilamina
BR0212069A (pt) Agentes antidiabéticos orais
BR0101230A (pt) Processo para a preparação de11-amino-3-cloro-6,11-diidro-5-5-dioxo-6-metil-dibenzo[c,f][1,2]tiazepina e aplicação para a sìntese detianeptina
BRPI0411841A (pt) cis-2,4,5-triaril-imidazolinas
BR0317383A (pt) Metabólitos agonista de vasopressina biologicamente ativos
BRPI0411597A (pt) cis-imidazolinas como inibidores de mdm2
BR0115139A (pt) Compostos bis-heterocìclicos com atividade antitumor e quimiossensibilizante
BR9810433A (pt) Composições anti-helmìnticas
TR199902055T2 (xx) Kinoksalindiyonlar.
DE59803437D1 (de) Aldehydfreie desinfektionsmittel für flächen und instrumente

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 9A ANUI DADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: NAO APRESENTADA A GUIA DE CUMPRIMENTO DE EXIGENCIA. REFERENTE A 9A ANUIDADE.