CR9980A - Imidazolinas 4,4,5,5 tetrasustituidas - Google Patents

Imidazolinas 4,4,5,5 tetrasustituidas

Info

Publication number
CR9980A
CR9980A CR9980A CR9980A CR9980A CR 9980 A CR9980 A CR 9980A CR 9980 A CR9980 A CR 9980A CR 9980 A CR9980 A CR 9980A CR 9980 A CR9980 A CR 9980A
Authority
CR
Costa Rica
Prior art keywords
tetrasustituidas
imidazolins
esters
compound
formula
Prior art date
Application number
CR9980A
Other languages
English (en)
Inventor
Qingjie Ding
Bradford James Graves
Norman Kong
Jin-Jun Liu
Allen John Lovey
Giacomo Pizzolato
John Lawson Roberts
Sung-Sau So
Thanh Vu-Binh
Peter Michael Wovkulich
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 CR9980A publication Critical patent/CR9980A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/20—Heterocyclic 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
    • C07D233/22—Radicals substituted by oxygen atoms
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/20—Heterocyclic 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
    • C07D233/26—Radicals substituted by carbon atoms having three bonds to hetero atoms
    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se proporciona un compuesto de fórmula I y las sales y ésteres farmacéuticamente aceptables del mismo, en el que X1, X2, R1, R2, R3, R4, R5 y R6 se describen aquí. Los compuestos muestran actividad como agentes antitumorales.
CR9980A 2005-12-01 2008-05-16 Imidazolinas 4,4,5,5 tetrasustituidas CR9980A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US74122305P 2005-12-01 2005-12-01
US85274706P 2006-10-19 2006-10-19

Publications (1)

Publication Number Publication Date
CR9980A true CR9980A (es) 2008-06-18

Family

ID=37866229

Family Applications (1)

Application Number Title Priority Date Filing Date
CR9980A CR9980A (es) 2005-12-01 2008-05-16 Imidazolinas 4,4,5,5 tetrasustituidas

Country Status (17)

Country Link
US (1) US7851626B2 (es)
EP (3) EP2311814A1 (es)
JP (1) JP4870778B2 (es)
KR (2) KR20100129331A (es)
CN (1) CN101316823B (es)
AR (1) AR057990A1 (es)
AU (1) AU2006319248B2 (es)
BR (1) BRPI0619236A2 (es)
CA (1) CA2630410C (es)
CR (1) CR9980A (es)
ES (1) ES2538714T3 (es)
MA (1) MA31550B1 (es)
NO (1) NO20082389L (es)
NZ (1) NZ568285A (es)
RU (1) RU2442779C2 (es)
TW (1) TWI326681B (es)
WO (1) WO2007063013A1 (es)

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EA201070233A1 (ru) * 2007-07-06 2010-08-30 Паратек Фармасьютикалс, Инк. Способы синтеза замещённых соединений тетрациклина (варианты)
MX2010003868A (es) 2007-10-09 2010-04-27 Hoffmann La Roche Cis-imidazolinas quirales.
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FR2967072B1 (fr) 2010-11-05 2013-03-29 Univ Dundee Procede pour ameliorer la production de virus et semences vaccinales influenza
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CA2850166C (en) 2011-09-27 2019-12-03 Amgen Inc. Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer
WO2013062923A1 (en) 2011-10-28 2013-05-02 Merck Sharp & Dohme Corp. MACROCYCLES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF
WO2013090645A1 (en) 2011-12-13 2013-06-20 Buck Institute For Research On Aging Methods for improving medical therapies
EP2793890B1 (en) 2011-12-21 2016-09-07 Merck Sharp & Dohme Corp. Substituted piperidines as hdm2 inhibitors
US9216170B2 (en) 2012-03-19 2015-12-22 Hoffmann-La Roche Inc. Combination therapy for proliferative disorders
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TWI654180B (zh) 2012-06-29 2019-03-21 美商艾佛艾姆希公司 殺真菌之雜環羧醯胺
US9901080B2 (en) 2012-08-23 2018-02-27 Buck Institute For Research On Aging Transgenic mouse having a transgene that converts a prodrug into a cytotoxic compound in senescent cells
US9901081B2 (en) 2012-08-23 2018-02-27 Buck Institute For Research On Aging Transgenic mouse for determining the role of senescent cells in cancer
WO2014082889A1 (en) * 2012-11-28 2014-06-05 F. Hoffmann-La Roche Ag Novel imidazolines as dual inhibitors of mdm2 and mdmx
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US8846657B2 (en) 2012-12-20 2014-09-30 Merck Sharp & Dohme Corp. Substituted imidazopyridines as HDM2 inhibitors
CN103012272B (zh) * 2012-12-21 2015-01-28 江苏国泰超威新材料有限公司 一种咪唑啉化合物的制备方法
US11407721B2 (en) 2013-02-19 2022-08-09 Amgen Inc. CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer
WO2014134201A1 (en) 2013-02-28 2014-09-04 Amgen Inc. A benzoic acid derivative mdm2 inhibitor for the treatment of cancer
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JP6461126B2 (ja) * 2013-07-03 2019-01-30 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｍｄｍ２アンタゴニストを用いた患者のがん治療法をパーソナライズするためのｍｒｎａベースの遺伝子発現
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EP3099380B1 (en) 2014-01-28 2021-08-11 Buck Institute for Research on Aging Methods and compositions for killing senescent cells and for treating senescence-associated diseases and disorders
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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
CN110088081A (zh) 2017-06-16 2019-08-02 尤尼蒂生物技术公司 制备用于药物用途的对映纯顺式-咪唑啉化合物的合成方法
CN112236162A (zh) 2018-04-06 2021-01-15 昂科莱奇公司 用于裂解选择性癌细胞的组合物
KR102039696B1 (ko) 2018-04-23 2019-11-04 충남대학교산학협력단 세포내 결핵균 제어를 위한 p53 발현 조절 가능한 조성물 (K279-1558) 또는 방법
CN114075121B (zh) * 2020-08-19 2025-08-29 中国科学院上海有机化学研究所 一类偶氮化合物的制备方法及其用途
KR102622992B1 (ko) 2021-03-29 2024-01-10 주식회사 퓨전바이오텍 이미다졸린 유도체 및 이의 중간체 제조방법
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Also Published As

Publication number Publication date
CN101316823B (zh) 2013-05-22
EP1960368B1 (en) 2015-05-06
KR20080072894A (ko) 2008-08-07
CA2630410C (en) 2014-02-25
NO20082389L (no) 2008-08-18
TW200804297A (en) 2008-01-16
BRPI0619236A2 (pt) 2011-09-20
AU2006319248A1 (en) 2007-06-07
JP4870778B2 (ja) 2012-02-08
CN101316823A (zh) 2008-12-03
TWI326681B (en) 2010-07-01
ES2538714T3 (es) 2015-06-23
CA2630410A1 (en) 2007-06-07
RU2442779C2 (ru) 2012-02-20
EP2311814A1 (en) 2011-04-20
NZ568285A (en) 2011-08-26
HK1126216A1 (en) 2009-08-28
US20070129416A1 (en) 2007-06-07
MA31550B1 (fr) 2010-08-02
KR20100129331A (ko) 2010-12-08
EP1960368A1 (en) 2008-08-27
EP2130822A1 (en) 2009-12-09
JP2009517439A (ja) 2009-04-30
AU2006319248B2 (en) 2012-09-27
RU2008126383A (ru) 2010-01-10
US7851626B2 (en) 2010-12-14
WO2007063013A1 (en) 2007-06-07
KR101109437B1 (ko) 2012-01-31
AR057990A1 (es) 2008-01-09

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