AR059040A1 - Cis-4, 5- biaril-2- heterociclico imidazolinas como inhibidores de la mdm 2 - Google Patents

Cis-4, 5- biaril-2- heterociclico imidazolinas como inhibidores de la mdm 2

Info

Publication number
AR059040A1
AR059040A1 ARP070100184A ARP070100184A AR059040A1 AR 059040 A1 AR059040 A1 AR 059040A1 AR P070100184 A ARP070100184 A AR P070100184A AR P070100184 A ARP070100184 A AR P070100184A AR 059040 A1 AR059040 A1 AR 059040A1
Authority
AR
Argentina
Prior art keywords
group
lower alkoxy
lower alkyl
nx3x4
substituted
Prior art date
Application number
ARP070100184A
Other languages
English (en)
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 AR059040A1 publication Critical patent/AR059040A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Procesos de obtencion, composiciones farmacéuticas y usos. Reivindicacion 1: El compuesto de la formula (1) y las sales y ésteres farmacéuticamente aceptables del mismo, en la que el anillo A es como se muestra en las formula (2) y (3); X1 se elige entre el grupo formado por alcoxi inferior y alcoxi inferior sustituido por trifluorometilo o F; X2 se elige entre el grupo formado por H, tioalquilo, alquilo inferior, alcoxi inferior, morfolino y -NX3X4; X3 y X4 con independencia entre sí se eligen entre el grupo formado por H, alquilo inferior, alquilo inferior sustituido por alcoxi inferior o ciano y alcoxi inferior; Y y Z con independencia entre sí se eligen entre el grupo formado por C y N; V1 y V2 con independencia entre sí se eligen entre el grupo formado por halogeno, ciano y acetileno; R se elige entre el grupo formado por piperidinilo sustituido por un heterociclo de cinco o seis eslabones, piperidinilo sustituido por -NX3X4 y por el compuesto de formula (4) en el que n es el numero 1 o 2; R1 puede ser uno o más sustituyentes elegidos entre el grupo formado por H, oxo, alquilo inferior sustituido por R2, C(O)R3 y -SO2-alquilo inferior; R2 se elige entre el grupo formado por hidroxi, alcoxi inferior, trifluorometilo, -ciano, -NH-SO2-alquilo inferior, -NH-C(O)-alquilo inferior, -C(O)-alquilo inferior, -C(O)R4, -C(O)-NX3X4, -SO2-alquilo inferior, -SO2-NX3X4; R3 se elige entre el grupo formado por un heterociclo de cinco eslabones, alquilo inferior, alcoxi inferior y alquilo inferior sustituido por alcoxi inferior; y R4 se elige entre el grupo formado por hidroxi, alcoxi inferior, morfolino y -NX3X4.
ARP070100184A 2006-01-18 2007-01-16 Cis-4, 5- biaril-2- heterociclico imidazolinas como inhibidores de la mdm 2 AR059040A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US75977006P 2006-01-18 2006-01-18

Publications (1)

Publication Number Publication Date
AR059040A1 true AR059040A1 (es) 2008-03-12

Family

ID=37983391

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070100184A AR059040A1 (es) 2006-01-18 2007-01-16 Cis-4, 5- biaril-2- heterociclico imidazolinas como inhibidores de la mdm 2

Country Status (12)

Country Link
US (1) US7705007B2 (es)
EP (1) EP1979338A1 (es)
JP (1) JP2009523751A (es)
KR (1) KR101015073B1 (es)
CN (1) CN101370799B (es)
AR (1) AR059040A1 (es)
AU (1) AU2007207052B2 (es)
BR (1) BRPI0710477A2 (es)
CA (1) CA2636824A1 (es)
IL (1) IL192635A0 (es)
TW (1) TW200738695A (es)
WO (1) WO2007082805A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20080091369A (ko) 2006-01-18 2008-10-10 암젠 인크 단백질 키나제 ｂ （ｐｋｂ） 억제제로서 티아졸 화합물
US7625895B2 (en) * 2007-04-12 2009-12-01 Hoffmann-Le Roche Inc. Diphenyl-dihydro-imidazopyridinones
WO2009047161A1 (en) * 2007-10-09 2009-04-16 F. Hoffmann-La Roche Ag Chiral cis-imidazolines
WO2011023677A1 (en) * 2009-08-26 2011-03-03 Novartis Ag Tetra-substituted heteroaryl compounds and their use as mdm2 and/or mdm4 modulators
US8017607B2 (en) * 2009-10-14 2011-09-13 Hoffmann-La Roche Inc. N-substituted-pyrrolidines as inhibitors of MDM2-P-53 interactions
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
WO2012105707A1 (en) 2011-01-31 2012-08-09 Tokyo University Of Science Educational Foundation Administrative Organization Method of treating ischemia/reperfusion injury
TW201429969A (zh) 2012-12-20 2014-08-01 Merck Sharp & Dohme 作爲ｈｄｍ２抑制劑之經取代咪唑吡啶
US20170216286A1 (en) 2014-01-28 2017-08-03 Mayo Foundation For Medical Education And Research Killing senescent cells and treating senescence-associated conditions using a src inhibitor and a flavonoid
AU2015211021B2 (en) 2014-01-28 2020-07-02 Buck Institute For Research On Aging Methods and compositions 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
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
EP3512831A4 (en) 2017-06-16 2019-07-31 Unity Biotechnology, Inc. SYNTHESIS PROCESS FOR THE PRODUCTION OF ENANTIOMERICALLY PURE CIS-IMIDAZOLINE COMPOUNDS FOR PHARMACEUTICAL USE
CN110563706B (zh) * 2019-08-29 2021-11-09 中国人民解放军第二军医大学 一种mdm2蛋白降解靶向嵌合体及其制备方法和应用
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same

Family Cites Families (7)

* 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
GB2351082A (en) 1999-06-18 2000-12-20 Lilly Forschung Gmbh Synthesis of Cyclic Substituted Amidines
RU2305095C2 (ru) * 2001-12-18 2007-08-27 Ф.Хоффманн-Ля Рош Аг Цис-2,4,5-трифенилимидазолины и фармацевтическая композиция на их основе
JP4361798B2 (ja) 2001-12-18 2009-11-11 エフ．ホフマン−ラ ロシュ アーゲー Ｍｄｍ２インヒビターとしてのシス−イミダゾリン
US7132421B2 (en) 2003-06-17 2006-11-07 Hoffmann-La Roche Inc. CIS-imidazoles
KR20080027969A (ko) * 2004-05-18 2008-03-28 에프. 호프만-라 로슈 아게 신규 ｃｉｓ-이미다졸린
US7893278B2 (en) * 2004-06-17 2011-02-22 Hoffman-La Roche Inc. CIS-imidazolines

Also Published As

Publication number Publication date
CN101370799A (zh) 2009-02-18
US20070167437A1 (en) 2007-07-19
US7705007B2 (en) 2010-04-27
CN101370799B (zh) 2012-09-05
JP2009523751A (ja) 2009-06-25
KR101015073B1 (ko) 2011-02-16
EP1979338A1 (en) 2008-10-15
IL192635A0 (en) 2009-02-11
TW200738695A (en) 2007-10-16
WO2007082805A1 (en) 2007-07-26
KR20080085045A (ko) 2008-09-22
AU2007207052A1 (en) 2007-07-26
AU2007207052B2 (en) 2012-07-12
BRPI0710477A2 (pt) 2011-08-16
CA2636824A1 (en) 2007-07-26

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