PE20030717A1 - Cis-imidazolinas - Google Patents

Cis-imidazolinas

Info

Publication number
PE20030717A1
PE20030717A1 PE2002001225A PE2002001225A PE20030717A1 PE 20030717 A1 PE20030717 A1 PE 20030717A1 PE 2002001225 A PE2002001225 A PE 2002001225A PE 2002001225 A PE2002001225 A PE 2002001225A PE 20030717 A1 PE20030717 A1 PE 20030717A1
Authority
PE
Peru
Prior art keywords
phenyl
dihydro
imidazole
chloro
bis
Prior art date
Application number
PE2002001225A
Other languages
English (en)
Inventor
Norman Kong
Binh Thanh Vu
Emily Aijun Liu
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 PE20030717A1 publication Critical patent/PE20030717A1/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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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 And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE REFIERE A CIS IMIDAZOLINAS DE FORMULA I DONDE Z1, Z2, Z3 SON ALCOXI, CH2OCH3, CH2OCH2CH3; UNO DE Z1, Z2, Z3 ES H Y EL RESTO SON ALQUILO, ALCOXI, Cl, Br, F, CF3, CH2OCH3, OR2, COOQ, ENTRE OTROS; Q ES H, ALQUILO; UNO DE Z1, Z2, Z3 ES H Y EL RESTO FORMA UN ANILLO DE 5-6 MIEMBROS; R1 ES F OCH3, N(CH3)2, ANILLO INSATURADO DE 5 MIEMBROS; R2 ES UN ANILLO SATURADO DE 3-6 MIEMBROS; Y1, Y2 SON Cl, Br, NO2, C=N, C=CH. SON COMPUESTOS PREFERIDOS 4,5-BIS-(4-CLORO-FENIL)-2-(2,3,4-TRIMETOXI-FENIL)-4,5-DIHIDRO-1H-IMIDAZOL; 4,5-BIS-(4-CLORO-FENIL)-2-(2,3-DIMETOXI-FENIL)-4,5-DIHIDRO-1H-IMIDAZOL; 4,5-BIS-(4-CLORO-FENIL)-2-(4-ETOXI-2-ISOPROPOXI-FENIL)-4,5-DIHIDRO-1H-IMIDAZOL; ENTRE OTROS. LOS COMPUESTOS SON INHIBIDORES DE LA INTERACCION ENTRE MDM2 CON UN PEPTIDO SIMILAR A p53 (POTENTE INHIBIDOR DEL CICLO CELULAR QUE A NIVEL CELULAR ESTA REGULADO POR MDM2) Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE TRASTORNOS PROLIFERATIVOS, CANCER DE MAMA, COLON, PULMON, PROSTATA
PE2002001225A 2001-12-18 2002-12-13 Cis-imidazolinas PE20030717A1 (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
PE20030717A1 true PE20030717A1 (es) 2003-08-28

Family

ID=26992633

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002001225A PE20030717A1 (es) 2001-12-18 2002-12-13 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)

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* Cited by examiner, † Cited by third party
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US7132421B2 (en) 2003-06-17 2006-11-07 Hoffmann-La Roche Inc. CIS-imidazoles
MXPA05013465A (es) * 2003-06-17 2006-03-09 Hoffmann La Roche Cis-imidazolinas como inhibidores de mdm2.
BRPI0511328A (pt) * 2004-05-18 2007-12-04 Hoffmann La Roche cis-imidazolinas
JP2008500991A (ja) * 2004-05-29 2008-01-17 ７ティーエム ファーマ エイ／エス 医学的使用のためのｃｒｔｈ２レセプターリガンド
US7893278B2 (en) * 2004-06-17 2011-02-22 Hoffman-La Roche Inc. CIS-imidazolines
NZ561215A (en) 2005-02-22 2010-12-24 Univ Michigan Small molecule inhibitors of MDM2 and uses thereof
CN101160314B (zh) * 2005-02-22 2012-05-23 密执安州立大学董事会 Mdm2的小分子抑制剂以及其应用
EP1960368B1 (en) 2005-12-01 2015-05-06 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
KR101015073B1 (ko) * 2006-01-18 2011-02-16 에프. 호프만-라 로슈 아게 Ｍｄｍ2 억제제로서의시스-4,5-비아릴-2-헤테로시클릭-이미다졸린
US8614192B2 (en) 2006-07-28 2013-12-24 Leiden University Medical Center Method for treating ocular cancer
US8470785B2 (en) 2006-07-28 2013-06-25 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
WO2008072655A1 (ja) 2006-12-14 2008-06-19 Daiichi Sankyo Company, Limited イミダゾチアゾール誘導体
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
WO2009070650A1 (en) * 2007-11-26 2009-06-04 The Research Foundation Of State University Of New York Small molecule cancer treatments that cause necrosis in cancer cells but do not affect normal cells
EP2298778A4 (en) 2008-06-12 2011-10-05 Daiichi Sankyo Co Ltd IMIDAZOTHIAZOL DERIVATIVE WITH 4,7-DIAZASPIRO [2.5] OCTAN RING STRUCTURE
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
NZ600430A (en) 2009-11-12 2014-06-27 Univ Michigan Spiro-oxindole mdm2 antagonists
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
CA2813256A1 (en) 2010-09-30 2012-04-05 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
NZ611866A (en) 2010-11-12 2015-04-24 Univ Michigan Spiro-oxindole mdm2 antagonists
CN103635473B (zh) 2011-03-10 2016-08-17 第一三共株式会社 二螺吡咯烷衍生物
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
CA2858565A1 (en) * 2011-12-07 2013-07-04 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
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
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
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
US9993472B2 (en) 2014-01-28 2018-06-12 Unity Biotechnology, Inc. Treatment for osteoarthritis in a joint by administering a means for inhibiting MDM2
TWI750129B (zh) * 2015-08-03 2021-12-21 瑞士商諾華公司 作為血液學毒性生物標記之ｇｄｆ-１５
UA123786C2 (uk) 2016-04-06 2021-06-02 Дзе Ріджентс Оф Дзе Юніверсіті Оф Мічіган Деструктори білка mdm2
JP7001614B2 (ja) 2016-04-06 2022-02-03 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン リガンド依存性の標的タンパク質分解のための単官能性中間体
CN109152843A (zh) 2016-05-20 2019-01-04 豪夫迈·罗氏有限公司 Protac抗体缀合物及其使用方法
KR20200035944A (ko) 2017-06-16 2020-04-06 유니티 바이오테크놀로지, 인크. 약제학적 용도를 위해 에난티오머적으로 순수한 시스-이미다졸린 화합물을 제조하기 위한 합성 방법
SG11202103282YA (en) 2018-10-08 2021-04-29 Univ Michigan Regents Small molecule mdm2 protein degraders
BR112022018678A2 (pt) 2020-03-19 2022-11-01 Kymera Therapeutics Inc Degradadores de mdm2 e usos dos mesmos
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same

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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
BR0215156A (pt) 2004-10-19
US6617346B1 (en) 2003-09-09
CA2468783A1 (en) 2003-06-26
AU2002361986A1 (en) 2003-06-30
ES2307822T3 (es) 2008-12-01
KR100640707B1 (ko) 2006-10-31
UY27586A1 (es) 2003-06-30
PL370909A1 (en) 2005-05-30
JP2005515210A (ja) 2005-05-26
DE60227108D1 (de) 2008-07-24
TW200301696A (en) 2003-07-16
EP1463501A1 (en) 2004-10-06
WO2003051360A1 (en) 2003-06-26
CN1604778A (zh) 2005-04-06
ATE397925T1 (de) 2008-07-15
MXPA04005880A (es) 2004-09-13
AU2002361986B2 (en) 2008-04-10
RU2312101C2 (ru) 2007-12-10
AR037882A1 (es) 2004-12-09
PA8561801A1 (es) 2003-07-28
KR20040068289A (ko) 2004-07-30
EP1463501B1 (en) 2008-06-11
RU2004122404A (ru) 2005-05-27
JP4361798B2 (ja) 2009-11-11

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