JP2005515210A5 - - Google Patents

Download PDF

Info

Publication number
JP2005515210A5
JP2005515210A5 JP2003552293A JP2003552293A JP2005515210A5 JP 2005515210 A5 JP2005515210 A5 JP 2005515210A5 JP 2003552293 A JP2003552293 A JP 2003552293A JP 2003552293 A JP2003552293 A JP 2003552293A JP 2005515210 A5 JP2005515210 A5 JP 2005515210A5
Authority
JP
Japan
Prior art keywords
och
ring
membered
membered saturated
independently selected
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.)
Granted
Application number
JP2003552293A
Other languages
English (en)
Other versions
JP4361798B2 (ja
JP2005515210A (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/EP2002/013905 external-priority patent/WO2003051360A1/en
Publication of JP2005515210A publication Critical patent/JP2005515210A/ja
Publication of JP2005515210A5 publication Critical patent/JP2005515210A5/ja
Application granted granted Critical
Publication of JP4361798B2 publication Critical patent/JP4361798B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Description

Z1, Z2又はZ3の1つは-Hであり、そして他の2つは、それらが置換されているベンゼン環からの2つの炭素原子及びそれらの間の結合と共に、S、N、及びOから選択された少なくとも1つのヘテロ原子を含む5−及び6−員の飽和環並びに5−及び6−員の不飽和環から選択された環を形成し、ここで
R1は、-F, -OCH3, -N(CH3)2, 及びS, N及びOから選択された少なくとも1つのヘテロ原子を含む不飽和5−員の環から選択され、
R2は、3−〜6−員の飽和環であり、そして
Y1及びY2は、-Cl, -Br, -NO2, -CN及び-CCHからそれぞれ独立して選択される]で表される化合物、及び医薬的に許容できるその塩及びエステルから選択された、少なくとも1つの化合物を提供する。
[式中、Z1, Z2及びZ3は、C1-C6アルコキシ、-CH2OCH3及び-CH2OCH2CH3からそれぞれ独立して選択されるか、あるいはZ1, Z2又はZ3の1つは-Hであり、そして他の2つは、C1-C6アルキル、C1-C6アルコキシ、-Cl、-Br、-F、-CF3、 -CH20CH3、-CH20CH2CH3、-OCH2CH2Rl、-CH2-モルホリノ、-OR2、-CH2R2、 -OCH2CF3、-OCH(CH3)CH20H 及び-COOQからそれぞれ独立して選択され、ここでQは-H及びC1-C6アルキルから選択され、又は
Z1, Z2又はZ3の1つは-Hであり、そして他の2つは、それらが置換されているベンゼン環からの2つの炭素原子及びそれらの間の結合と共に、S、N、及びOから選択された少なくとも1つのヘテロ原子を含む5−及び6−員の飽和環並びに5−及び6−員の不飽和環から選択された環を形成し、ここで
JP2003552293A 2001-12-18 2002-12-09 Mdm2インヒビターとしてのシス−イミダゾリン Expired - Fee Related JP4361798B2 (ja)

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 (3)

Publication Number Publication Date
JP2005515210A JP2005515210A (ja) 2005-05-26
JP2005515210A5 true JP2005515210A5 (ja) 2009-07-23
JP4361798B2 JP4361798B2 (ja) 2009-11-11

Family

ID=26992633

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2003552293A Expired - Fee Related JP4361798B2 (ja) 2001-12-18 2002-12-09 Mdm2インヒビターとしてのシス−イミダゾリン

Country Status (20)

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

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7132421B2 (en) 2003-06-17 2006-11-07 Hoffmann-La Roche Inc. CIS-imidazoles
AU2004253245B2 (en) * 2003-06-17 2010-02-11 F. Hoffmann-La Roche Ag CIS-imidazolines as MDM2 inhibitors
EP1753727B1 (en) * 2004-05-18 2008-11-19 F.Hoffmann-La Roche Ag Novel cis-imidazolines
JP2008500991A (ja) * 2004-05-29 2008-01-17 7ティーエム ファーマ エイ/エス 医学的使用のためのcrth2レセプターリガンド
US7893278B2 (en) * 2004-06-17 2011-02-22 Hoffman-La Roche Inc. CIS-imidazolines
AU2006216780B8 (en) 2005-02-22 2010-04-22 The Regents Of The University Of Michigan Small molecule inhibitors of MDM2 and uses thereof
NZ561215A (en) 2005-02-22 2010-12-24 Univ Michigan Small molecule inhibitors of MDM2 and uses thereof
KR20100129331A (ko) 2005-12-01 2010-12-08 에프. 호프만-라 로슈 아게 항암제로서 사용하기 위한 p53 및 mdm2 단백질 간 상호작용의 저해제로서의 2,4,5-트리페닐 이미다졸린 유도체
WO2007082805A1 (en) * 2006-01-18 2007-07-26 F. Hoffmann-La Roche Ag Cis-4, 5-biaryl-2-heterocyclic-imidazolines as mdm2 inhibitors
US8470785B2 (en) 2006-07-28 2013-06-25 St. Jude Children's Research Hospital Method for treating ocular cancer
US8614192B2 (en) 2006-07-28 2013-12-24 Leiden University Medical Center 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
EP2103619A4 (en) 2006-12-14 2011-11-23 Daiichi Sankyo Co Ltd IMIDAZOTHIAZOLDERIVATE
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
WO2009070650A1 (en) * 2007-11-26 2009-06-04 The Research Foundation Of State University Of New York Small molecule cancer treatments that cause necrosis in cancer cells but do not affect normal cells
WO2009151069A1 (ja) 2008-06-12 2009-12-17 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
CN102356085A (zh) 2009-01-16 2012-02-15 第一三共株式会社 具有脯氨酸环结构的咪唑并噻唑衍生物
JP2013510860A (ja) 2009-11-12 2013-03-28 ザ、リージェンツ、オブ、ザ、ユニバーシティ、オブ、ミシガン スピロ−オキシインドールmdm2アンタゴニスト
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
US20130225603A1 (en) * 2010-09-27 2013-08-29 Serrata Llc Mdm2 inhibitors for treatment of ocular conditions
US9266860B2 (en) 2010-09-30 2016-02-23 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
CA2817585A1 (en) 2010-11-12 2012-05-18 The Regents Of The University Of Michigan Spiro-oxindole mdm2 antagonists
DK2684880T3 (en) 2011-03-10 2018-05-22 Daiichi Sankyo Co Ltd DISPIROPYRROLIDINE DERIVATIVES
ES2624808T3 (es) 2011-05-11 2017-07-17 The Regents Of The University Of Michigan Antagonistas de MDM2 espirooxindólicos
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
EP2935263B1 (en) 2012-12-20 2018-12-05 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
SG11201606239UA (en) 2014-01-28 2016-08-30 Buck Inst For Res On Aging Methods and compositions for killing senescent cells and for treating senescence-associated diseases and disorders
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
US20190269675A1 (en) 2014-01-28 2019-09-05 Buck Institute for Research and Aging Treatment of parkinson's disease and other conditions caused or mediated by senescent astrocytes using small molecule senolytic agents
TWI804010B (zh) * 2015-08-03 2023-06-01 瑞士商諾華公司 作為血液學毒性生物標記之gdf-15
JP7037500B2 (ja) 2016-04-06 2022-03-16 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Mdm2タンパク質分解剤
AU2017246453A1 (en) 2016-04-06 2018-11-08 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
CN118436801A (zh) 2016-05-20 2024-08-06 豪夫迈·罗氏有限公司 Protac抗体缀合物及其使用方法
JP6848055B2 (ja) 2017-06-16 2021-03-24 ユニティ バイオテクノロジー インコーポレイテッド 薬学的使用のための鏡像異性的に純粋なシス‐イミダゾリン化合物を生成するための合成方法
WO2019195851A1 (en) 2018-04-06 2019-10-10 Oncolyze, Inc. Compositions for use in lysis of selective cancer cells
MX2021003999A (es) 2018-10-08 2021-06-23 Univ Michigan Regents Moleculas de bajo peso molecular degradadoras de la proteina mdm2.
IL296451B2 (en) 2020-03-19 2026-05-01 Kymera Therapeutics Inc MDM2 joints and their uses
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same
WO2024240858A1 (en) 2023-05-23 2024-11-28 Valerio Therapeutics Protac molecules directed against dna damage repair system and uses thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1175431A (en) * 1980-07-25 1984-10-02 Alfred Sallmann Tri-substituted imidazole derivatives, processes for their manufacture, pharmaceutical preparations containing them, and their use
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
WO1992003421A2 (en) 1990-08-17 1992-03-05 E.I. Du Pont De Nemours And Company Arthropodicidal pyrazolines, pyrazolidines and hydrazines
GB2351082A (en) * 1999-06-18 2000-12-20 Lilly Forschung Gmbh Synthesis of Cyclic Substituted Amidines

Similar Documents

Publication Publication Date Title
EA200300305A1 (ru) Альфа-арилэтаноламины и их применение в качестве агонистов бета-адренергических рецепторов
AR037882A1 (es) Cis-imidazolinas
AU2003217274A1 (en) Peroxisome proliferator activated receptor modulators
TW346485B (en) Substituted N-(indole-2-carbonyl)-glycinamides and derivatives as antidiabetic agents
EA200600348A1 (ru) Новые соединения
NO20060220L (no) Forbindelser med inhiberene aktivitet mot natriumavhengige transportorer
MY149463A (en) Novel compounds
AR038762A1 (es) Derivados de indolina, un proceso para su preparacion, composicion farmaceutica, proceso para la preparacion de dicha composicion y el uso de dichos derivados para la fabricacion de un medicamento
CA2249542A1 (en) Pyrazole derivatives, their preparation and their use in pharmaceuticals
JP2006523698A5 (ja)
IL185199A (en) Indole compounds and medications containing them for the prevention of and / or treatment of leucotriene colton disease
RU2394028C2 (ru) Производные бензилтриазолона в качестве ненуклеозидных ингибиторов обратной транскриптазы
WO2003024441A1 (en) Novel use of tricyclic compound
JP2005525392A5 (ja)
JP2008520811A5 (ja)
WO2003048130A3 (en) Peroxisome proliferator activated receptor agonists
CA2169737A1 (en) Endothelin antagonistic heteroaromatic ring-fused cyclopentene derivatives
JP2001525394A5 (ja)
JP2005525364A5 (ja)
AR044869A1 (es) Compuesto de dicetopiperazina, composicion farmaceutica que lo comprende, su uso para fabricar un medicamento y procedimiento para su preparacion
EA200500240A1 (ru) Новый способ синтеза соединений 1,3,4,5-тетрагидро-2h-3-бензазепин-2-она и применение при синтезе ивабрадина и его солей присоединения с фармацевтически приемлемой кислотой
DE69120603D1 (de) Isochromanderivate
EA200200973A1 (ru) Пиридазинилфенилгидразоны, применяемые при застойной сердечной недостаточности
DE602004024584D1 (de) Inhibitoren der nicht-nukleotidischen reversen transkriptase
JP2024037892A5 (ja)