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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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MX2009006397A (es) 2006-12-14 2009-08-13 Daiichi Sankyo Co Ltd Derivados de imidazotiazol.
WO2008095063A1 (en) 2007-01-31 2008-08-07 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
ES2430067T3 (es) 2007-03-28 2013-11-18 President And Fellows Of Harvard College Polipéptidos cosidos
US7625895B2 (en) 2007-04-12 2009-12-01 Hoffmann-Le Roche Inc. Diphenyl-dihydro-imidazopyridinones
ES2375508T3 (es) * 2007-05-21 2012-03-01 Dow Global Technologies Llc Objetos recubiertos.
EP2249832A4 (en) * 2008-01-30 2011-12-21 Agency Science Tech & Res METHOD FOR THE TREATMENT OF FIBROSIS AND CANCER WITH IMIDAZOLIUM AND IMIDAZOLINI COMPOUNDS
EP2271338A4 (en) * 2008-03-31 2011-05-04 Agency Science Tech & Res METHOD FOR THE TREATMENT OF NEUROLOGICAL ILLNESSES WITH IMIDAZOLIUM AND IMIDAZOLIUM COMPOUNDS
EP2298778A4 (en) 2008-06-12 2011-10-05 Daiichi Sankyo Co Ltd IMIDAZOTHIAZOL DERIVATIVE WITH 4,7-DIAZASPIRO [2.5] OCTAN RING STRUCTURE
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
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
DK2603600T3 (da) 2010-08-13 2019-03-04 Aileron Therapeutics Inc Peptidomimetiske makrocyklusser
CA2813256A1 (en) 2010-09-30 2012-04-05 St. Jude Children's Research Hospital Aryl-substituted imidazoles
EP2760845B1 (en) 2011-09-27 2016-11-16 Amgen Inc. Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer
CA2852468A1 (en) 2011-10-18 2013-04-25 Aileron Therapeutics, Inc. Peptidomimetic macrocyles
SG10201606775YA (en) 2012-02-15 2016-10-28 Aileron Therapeutics Inc Peptidomimetic macrocycles
HK1205454A1 (en) 2012-02-15 2015-12-18 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
CA2887285A1 (en) 2012-11-01 2014-05-08 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
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
US11407721B2 (en) 2013-02-19 2022-08-09 Amgen Inc. CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer
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AU2014236812B2 (en) 2013-03-14 2018-03-01 Amgen Inc. Heteroaryl acid morpholinone compounds as MDM2 inhibitors for the treatment of cancer
ES2993671T3 (en) 2013-03-15 2025-01-03 Univ Texas Peptide fttftvt for use in treating fibrosis
JOP20200296A1 (ar) 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط
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
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
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
EP3669881B1 (en) 2014-01-28 2022-03-30 Buck Institute for Research on Aging Compositions for use in the treatment of senescence-assiocated eye disease and disorders
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JP2017533889A (ja) 2014-09-24 2017-11-16 エルロン・セラピューティクス・インコーポレイテッドＡｉｌｅｒｏｎ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． ペプチド模倣大環状分子およびその使用
JP2018516844A (ja) 2015-03-20 2018-06-28 エルロン・セラピューティクス・インコーポレイテッドＡｉｌｅｒｏｎ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． ペプチド模倣大環状分子およびその使用
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CN109195593A (zh) 2016-03-15 2019-01-11 奥莱松基因组股份有限公司 用于治疗实体瘤的lsd1抑制剂的组合
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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

Also Published As

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

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