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AR049647A1 - Cis-imidazolinas - Google Patents

Cis-imidazolinas

Info

Publication number
AR049647A1
AR049647A1 ARP050102451A ARP050102451A AR049647A1 AR 049647 A1 AR049647 A1 AR 049647A1 AR P050102451 A ARP050102451 A AR P050102451A AR P050102451 A ARP050102451 A AR P050102451A AR 049647 A1 AR049647 A1 AR 049647A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
alkyl substituted
chosen
substituted
ring
Prior art date
Application number
ARP050102451A
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34969621&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR049647(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR049647A1 publication Critical patent/AR049647A1/es

Links

Classifications

    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente se refiere a compuestos derivados de cis-imidazolinas y a sales y ésteres farmacéuticamente aceptables de los mismos, a un proceso para su obtencion, a medicamentos que los contienen así como al uso de estos compuestos como agentes farmacéuticamente activos. Los compuestos presentan actividad antiproliferante y pueden ser especialmente utiles para al tratamiento del cáncer. Reivindicacion 1. Un compuesto de la formula (1) y las sales y ésteres farmacéuticamente aceptables del mismo. en la que R significa un anillo saturado o insaturado de 5 o 6 eslabones que contiene por lo menos un heteroátomo elegido entre S, N y O; y que está opcionalmente sustituido ppor un resto elegido entre alquilo inferior, cicloalquilo, -C(O)- R1, hidroxi, alquilo inferior sustituido por hidroxi, alquilo inferior sustituido por alcoxi inferior, alquilo inferior sustituido por -NH2, alquilo inferior sustituido por -SO2-alquilo inferior, alquilo inferior sustituido por -C(O)-R1, -NH- alquilo inferior, -N(alquilo inferior)2, -SO2-alquilo inferior, =O, -CH2C(O)CH3, o un anillo saturado de 5 o 6 eslabones que contiene 1, 2 o 3 heteroátomos elegidos entre S, N y O; R1 se elige entre H, alquilo inferior, -NH2, -NH-alquilo inferior, - N(alquilo inferior)2, alquilo inferior sustituido por hidroxi, alquilo inferior sustituido por NH2, o un anillo saturado de 5 o 6 eslabones que contiene 1, 2 o 3 heteroátomos elegidos entre S, N y O; X1 y X2 con independencia entre sí se eligen entre el grupo formado por H, alcoxi inferior, -CH2OCH3, -CH2OCH2CH3, -OCH"CF3, -OCH2CH2F; Y1 e Y2 con independencia entre sí se eligen entre el grupo formado por -Cl, -Br, -NO2, -C:::N, y -C:::CH; y la estereoquímica absoluta de la posicion 4 y 5 del anillo imidazolina es S y R respectivamente.
ARP050102451A 2004-06-17 2005-06-15 Cis-imidazolinas AR049647A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58044104P 2004-06-17 2004-06-17
US67419605P 2005-04-22 2005-04-22

Publications (1)

Publication Number Publication Date
AR049647A1 true AR049647A1 (es) 2006-08-23

Family

ID=34969621

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050102451A AR049647A1 (es) 2004-06-17 2005-06-15 Cis-imidazolinas

Country Status (16)

Country Link
US (1) US7893278B2 (es)
EP (1) EP1758868A1 (es)
JP (1) JP4809336B2 (es)
KR (1) KR100855929B1 (es)
AR (1) AR049647A1 (es)
AU (1) AU2005254643A1 (es)
BR (1) BRPI0512237A (es)
CA (1) CA2569598A1 (es)
IL (1) IL179730A0 (es)
MX (1) MXPA06014806A (es)
NO (1) NO20070295L (es)
NZ (1) NZ551659A (es)
RU (1) RU2408593C2 (es)
SG (1) SG148177A1 (es)
TW (1) TW200637828A (es)
WO (1) WO2005123691A1 (es)

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BRPI0607445A2 (pt) * 2005-03-16 2009-09-01 Hoffmann La Roche cis-2,4,5-triaril-imidazolinas e seu uso como medicamentos anti-cáncer
CN101316823B (zh) * 2005-12-01 2013-05-22 霍夫曼-拉罗奇有限公司 用作抗癌剂的作为p53和MDM2蛋白之间相互作用的抑制剂的2,4,5-三苯基咪唑啉衍生物
AU2007207052B2 (en) * 2006-01-18 2012-07-12 F. Hoffmann-La Roche Ag CIS-4, 5-biaryl-2-heterocyclic-imidazolines as MDM2 inhibitors
AU2007332493A1 (en) 2006-12-14 2008-06-19 Daiichi Sankyo Company, Limited Imidazothiazole derivatives
JP5649825B2 (ja) * 2007-01-31 2015-01-07 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド 安定化させたｐ５３ペプチドおよびその使用法
CA2682174C (en) 2007-03-28 2021-04-06 President And Fellows Of Harvard College Stitched polypeptides
US7625895B2 (en) 2007-04-12 2009-12-01 Hoffmann-Le Roche Inc. Diphenyl-dihydro-imidazopyridinones
JP2010527817A (ja) * 2007-05-21 2010-08-19 ダウ グローバル テクノロジーズ インコーポレイティド 被覆物体
US9072729B2 (en) * 2008-01-30 2015-07-07 Agency For Science, Technology And Research Method for treating fibrosis and cancer with imidazolium and imidazolinium compounds
EP2803356A1 (en) * 2008-03-31 2014-11-19 Agency for Science, Technology and Research Method for treating neurological disorders with imidazolium and imidazolinium compounds
EP2298778A4 (en) 2008-06-12 2011-10-05 Daiichi Sankyo Co Ltd IMIDAZOTHIAZOLE DERIVATE HAVING A CYCLIC STRUCTURE OF 4,7-DIAZASPIRO®2.5OCITANE
WO2010082612A1 (ja) 2009-01-16 2010-07-22 第一三共株式会社 プロリン環構造を有するイミダゾチアゾール誘導体
JO2998B1 (ar) 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
US8889863B2 (en) 2010-07-16 2014-11-18 Vanderbilt University Stereoselective methods, catalysts and intermediates for the synthesis of (−)-Nutlin-3 and related compounds
PL2603600T3 (pl) 2010-08-13 2019-06-28 Aileron Therapeutics, Inc. Makrocykle peptidomometyczne
ES2685175T3 (es) 2010-09-30 2018-10-05 St. Jude Children's Research Hospital Imidazoles sustituidos con arilo
WO2013049250A1 (en) 2011-09-27 2013-04-04 Amgen Inc. Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer
AR088392A1 (es) 2011-10-18 2014-05-28 Aileron Therapeutics Inc Macrociclos peptidomimeticos
CN104144695A (zh) 2012-02-15 2014-11-12 爱勒让治疗公司 三唑交联的和硫醚交联的拟肽大环化合物
RU2017145921A (ru) 2012-02-15 2019-02-21 Эйлерон Терапьютикс, Инк. Пептидомиметические макроциклы
KR20150082307A (ko) 2012-11-01 2015-07-15 에일러론 테라퓨틱스 인코포레이티드 이치환 아미노산 및 이의 제조 및 사용 방법
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US11407721B2 (en) 2013-02-19 2022-08-09 Amgen Inc. CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer
CA2902856C (en) 2013-02-28 2021-02-16 Amgen Inc. A benzoic acid derivative mdm2 inhibitor for the treatment of cancer
MX2015012427A (es) 2013-03-14 2016-01-12 Amgen Inc Compuestos de morfolinona de acido heteroarilo como inhibidores mdm2 para el tratamiento de cancer.
ES2875853T3 (es) 2013-03-15 2021-11-11 Univ Texas Método de tratar fibrosis
JOP20200296A1 (ar) 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط
IL286427B2 (en) 2014-01-28 2024-08-01 Mayo Found Medical Education & Res Inhibitors bcl-2 anti-apoptotic protein family members for treatment of non cancer pulmonary disease or an opthalmic disease
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
SG11201702175YA (en) 2014-09-24 2017-04-27 Aileron Therapeutics Inc Peptidomimetic macrocycles and formulations thereof
SG10201902594QA (en) 2014-09-24 2019-04-29 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof
KR20170129879A (ko) 2015-03-20 2017-11-27 에일러론 테라퓨틱스 인코포레이티드 펩티드모방 거대고리 및 이의 용도
CN108368161A (zh) 2015-09-10 2018-08-03 艾瑞朗医疗公司 作为mcl-1调节剂的拟肽大环化合物
SG10201913331VA (en) 2016-03-15 2020-03-30 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
AU2017233886B2 (en) 2016-03-15 2022-10-20 Oryzon Genomics, S.A. Combinations of LSD1 inhibitors for the treatment of hematological malignancies
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MXPA06013246A (es) 2004-05-18 2007-02-08 Hoffmann La Roche Nuevas imidazolinas cis.

Also Published As

Publication number Publication date
NZ551659A (en) 2010-08-27
US20050282803A1 (en) 2005-12-22
JP2008502620A (ja) 2008-01-31
TW200637828A (en) 2006-11-01
BRPI0512237A (pt) 2008-02-19
WO2005123691A1 (en) 2005-12-29
KR100855929B1 (ko) 2008-09-02
US7893278B2 (en) 2011-02-22
NO20070295L (no) 2007-01-17
KR20070027590A (ko) 2007-03-09
RU2408593C2 (ru) 2011-01-10
RU2007101275A (ru) 2008-07-27
AU2005254643A1 (en) 2005-12-29
SG148177A1 (en) 2008-12-31
JP4809336B2 (ja) 2011-11-09
MXPA06014806A (es) 2007-02-12
IL179730A0 (en) 2007-05-15
CA2569598A1 (en) 2005-12-29
EP1758868A1 (en) 2007-03-07

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