PA8561801A1 - Cis-imidazolinas - Google Patents

Cis-imidazolinas

Info

Publication number
PA8561801A1
PA8561801A1 PA20028561801A PA8561801A PA8561801A1 PA 8561801 A1 PA8561801 A1 PA 8561801A1 PA 20028561801 A PA20028561801 A PA 20028561801A PA 8561801 A PA8561801 A PA 8561801A PA 8561801 A1 PA8561801 A1 PA 8561801A1
Authority
PA
Panama
Prior art keywords
imidazolins
cis
peptiera
formula
sproports
Prior art date
Application number
PA20028561801A
Other languages
English (en)
Inventor
Norman Kong
Emily Aijun Liu
Binh Thanh Vu
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 PA8561801A1 publication Critical patent/PA8561801A1/es

Links

Classifications

    • 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
    • C07D405/04—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 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
    • A61K31/41—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
    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

LA PRESENTE INVENCION SPROPORCIONA COMPUESTOS DE ACUERDO CON LA FORMULA I Y FORMULA II Y SALES Y ESTERES FARMACEUTICAMENTE ACEPTABLES DE LOS MISMOS, CON LAS DENOMINACIONES PROPORCIONADAS AQUI Y QUE INHIBEN LA INTERACCION DE LA PROTEINA MDM2 CON UN PEPTIDO DE TIPO P53 Y CON ACTIVIDAD ANTIPROLIFERATIVA.
PA20028561801A 2001-12-18 2002-12-17 Cis-imidazolinas PA8561801A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34172901P 2001-12-18 2001-12-18
US39087602P 2002-06-21 2002-06-21

Publications (1)

Publication Number Publication Date
PA8561801A1 true PA8561801A1 (es) 2003-07-28

Family

ID=26992633

Family Applications (1)

Application Number Title Priority Date Filing Date
PA20028561801A PA8561801A1 (es) 2001-12-18 2002-12-17 Cis-imidazolinas

Country Status (20)

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

Families Citing this family (41)

* 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
KR100832277B1 (ko) * 2004-05-18 2008-05-26 에프. 호프만-라 로슈 아게 신규 ｃｉｓ-이미다졸린
AU2005247110B2 (en) * 2004-05-29 2010-08-26 7Tm Pharma A/S CRTH2 receptor ligands for medicinal uses
US7893278B2 (en) * 2004-06-17 2011-02-22 Hoffman-La Roche Inc. CIS-imidazolines
US7759383B2 (en) 2005-02-22 2010-07-20 The Regents Of The University Of Michigan Small molecule inhibitors of MDM2 and the uses thereof
EA019566B1 (ru) * 2005-02-22 2014-04-30 Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган Низкомолекулярные ингибиторы mdm2
WO2007063013A1 (en) 2005-12-01 2007-06-07 F. Hoffmann-La Roche Ag 2,4,5-triphenyl imidazoline derivatives as inhibitors of the interaction between p53 and mdm2 proteins for use as anticancer agents
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
WO2008014216A1 (en) 2006-07-28 2008-01-31 St. Jude Children's Research Hospital 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
KR20090090383A (ko) 2006-12-14 2009-08-25 다이이찌 산쿄 가부시키가이샤 이미다조티아졸 유도체
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
US9539327B2 (en) * 2007-11-26 2017-01-10 The Research Foundation For The State University Of New York Small molecule cancer treatments that cause necrosis in cancer cells but do not affect normal cells
JPWO2009151069A1 (ja) 2008-06-12 2011-11-17 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
PT2380892E (pt) 2009-01-16 2014-06-09 Daiichi Sankyo Co Ltd Derivado de imidazotiazole compreendendo uma estrutura de anel prolina
BR112012011317A2 (pt) 2009-11-12 2019-09-24 Univ Michigan Regents antagonistas espiro-oxindóis de mdm2
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
WO2012047587A2 (en) * 2010-09-27 2012-04-12 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
JP2014500870A (ja) 2010-11-12 2014-01-16 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
WO2012121361A1 (ja) 2011-03-10 2012-09-13 第一三共株式会社 ジスピロピロリジン誘導体
JP2014513699A (ja) 2011-05-11 2014-06-05 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
KR101384683B1 (ko) * 2011-10-27 2014-04-11 한국생명공학연구원 ｍｄｍ２－결합 모티프를 포함하는 펩타이드 및 이의 용도
US9937178B2 (en) 2011-12-07 2018-04-10 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
ES2707305T3 (es) 2012-12-20 2019-04-03 Merck Sharp & Dohme Imidazopiridinas sustituidas como inhibidores de HDM2
CN106163557B (zh) 2014-01-28 2020-07-14 巴克老龄化研究所 用于杀死衰老细胞和用于治疗衰老相关疾病和病症的方法和组合物
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
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
CN113788818A (zh) 2016-04-06 2021-12-14 密执安大学评议会 Mdm2蛋白质降解剂
US10759808B2 (en) 2016-04-06 2020-09-01 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
EP3458101B1 (en) 2016-05-20 2020-12-30 H. Hoffnabb-La Roche Ag Protac antibody conjugates and methods of use
AU2017418538B2 (en) 2017-06-16 2021-10-21 Unity Biotechnology, Inc. Synthesis method for producing enantiomerically pure cis-imidazoline compounds for pharmaceutical use
CA3112591A1 (en) 2018-10-08 2020-04-16 The Regents Of The University Of Michigan Small molecule mdm2 protein degraders
CN115776887A (zh) 2020-03-19 2023-03-10 凯麦拉医疗公司 Mdm2降解剂和其用途
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same

Family Cites Families (3)

* 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
EP0543930A1 (en) 1990-08-17 1993-06-02 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

Also Published As

Publication number Publication date
EP1463501A1 (en) 2004-10-06
PL370909A1 (en) 2005-05-30
ES2307822T3 (es) 2008-12-01
PE20030717A1 (es) 2003-08-28
AU2002361986B2 (en) 2008-04-10
KR100640707B1 (ko) 2006-10-31
WO2003051360A1 (en) 2003-06-26
RU2312101C2 (ru) 2007-12-10
CA2468783A1 (en) 2003-06-26
JP2005515210A (ja) 2005-05-26
MXPA04005880A (es) 2004-09-13
ATE397925T1 (de) 2008-07-15
US6617346B1 (en) 2003-09-09
CN1604778A (zh) 2005-04-06
JP4361798B2 (ja) 2009-11-11
DE60227108D1 (de) 2008-07-24
EP1463501B1 (en) 2008-06-11
TW200301696A (en) 2003-07-16
RU2004122404A (ru) 2005-05-27
KR20040068289A (ko) 2004-07-30
AR037882A1 (es) 2004-12-09
AU2002361986A1 (en) 2003-06-30
UY27586A1 (es) 2003-06-30
BR0215156A (pt) 2004-10-19

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