DE69633398D1 - Betulinsäure-derivate und ihre verwendungen - Google Patents

Betulinsäure-derivate und ihre verwendungen

Info

Publication number
DE69633398D1
DE69633398D1 DE69633398T DE69633398T DE69633398D1 DE 69633398 D1 DE69633398 D1 DE 69633398D1 DE 69633398 T DE69633398 T DE 69633398T DE 69633398 T DE69633398 T DE 69633398T DE 69633398 D1 DE69633398 D1 DE 69633398D1
Authority
DE
Germany
Prior art keywords
betulinic acid
acid derivatives
substd
opt
dotted line
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
DE69633398T
Other languages
English (en)
Other versions
DE69633398T2 (de
DE69633398T8 (de
Inventor
Kuo-Hsiung Lee
Yoshiki Kashiwada
Fumio Hashimoto
Mark Cosentino
Mark Manak
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of North Carolina at Chapel Hill
Panacos Pharmaceuticals Inc
Original Assignee
BIOTECH RES LAB ROCKVILLE
University of North Carolina at Chapel Hill
University of North Carolina System
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 BIOTECH RES LAB ROCKVILLE, University of North Carolina at Chapel Hill, University of North Carolina System filed Critical BIOTECH RES LAB ROCKVILLE
Application granted granted Critical
Publication of DE69633398D1 publication Critical patent/DE69633398D1/de
Publication of DE69633398T2 publication Critical patent/DE69633398T2/de
Publication of DE69633398T8 publication Critical patent/DE69633398T8/de
Active legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
DE69633398T 1995-06-05 1996-06-05 Betulinsäure-derivate und ihre verwendungen Active DE69633398T8 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/463,071 US5679828A (en) 1995-06-05 1995-06-05 Betulinic acid and dihydrobetulinic acid derivatives and uses therefor
US463071 1995-06-05
PCT/US1996/009485 WO1996039033A1 (en) 1995-06-05 1996-06-05 Betulinic acid derivatives and uses therefor

Publications (3)

Publication Number Publication Date
DE69633398D1 true DE69633398D1 (de) 2004-10-21
DE69633398T2 DE69633398T2 (de) 2005-09-22
DE69633398T8 DE69633398T8 (de) 2006-01-12

Family

ID=23838749

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69633398T Active DE69633398T8 (de) 1995-06-05 1996-06-05 Betulinsäure-derivate und ihre verwendungen

Country Status (10)

Country Link
US (1) US5679828A (de)
EP (2) EP0857018B1 (de)
AT (1) ATE275823T1 (de)
AU (1) AU6328896A (de)
CA (1) CA2223513C (de)
DE (1) DE69633398T8 (de)
DK (1) DK0857018T3 (de)
ES (1) ES2231818T3 (de)
PT (1) PT857018E (de)
WO (1) WO1996039033A1 (de)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5962527A (en) * 1995-03-21 1999-10-05 The Board Of Trustees Of The University Of Illinois Method and composition for treating cancers
US5869535A (en) * 1995-03-21 1999-02-09 The Board Of Trustees Of The University Of Illinois Method and composition for selectively inhibiting melanoma
EP0902685A1 (de) * 1997-01-24 1999-03-24 Marigen S.A. Ultramikroemulsionen aus spontan dispergierbaren konzentraten enthaltend antitumoral, antiviral und antiparasitär wirksame ester von pentacyclischen triterpenen
US5750578A (en) * 1997-02-11 1998-05-12 Regents Of The University Of Minnesota Use of betulin and analogs thereof to treat herpesvirus infection
EP0988311B9 (de) * 1997-06-04 2004-12-15 Cornell Research Foundation, Inc. Betulinolderivate
US6228850B1 (en) * 1997-09-30 2001-05-08 Dabur Research Foundation Antiangiogenic activity of betulinic acid and its derivatives
US6670345B1 (en) * 1997-09-30 2003-12-30 Dabur Research Foundation Betulinic acid derivatives for inhabiting cancer growth and process for the manufacture of betulinic acid
US6048847A (en) * 1997-09-30 2000-04-11 Dabur Research Foundation Use of betulinic acid and its derivatives for inhibiting cancer growth and a method of monitoring this
AU762404B2 (en) * 1998-03-02 2003-06-26 Panacos Pharmaceuticals, Inc. Acylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof
US6303589B1 (en) * 1998-12-08 2001-10-16 Micro Flo Company Pentacyclic triterpenes
US6369101B1 (en) 1999-02-26 2002-04-09 Regents Of The University Of Minnesota Therapeutic method to treat herpes virus infection
US6392070B1 (en) * 1999-08-10 2002-05-21 Regents Of The University Of Minnesota Birch bark processing and the isolation of natural products from birch bark
DE69917684T2 (de) * 1999-09-09 2005-07-21 Dabur Research Foundation, Sahibabad Betulinsäure-derivate mit antiangiogener wirkung, verfahren zur herstellung solcher derivate und deren verwendung für die behandlung tumorassoziierter angiogenese
WO2002091858A1 (en) * 2001-05-11 2002-11-21 University Of Ottawa Anxiolytic marcgraviaceae compositions containing betulinic acid, betulinic acid derivatives, and methods
US20040131629A1 (en) * 2002-09-26 2004-07-08 Panacos Pharmaceuticals, Inc. Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof
US7365221B2 (en) * 2002-09-26 2008-04-29 Panacos Pharmaceuticals, Inc. Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof
CA2514563A1 (en) * 2003-01-29 2004-08-19 Panacos Pharmaceuticals, Inc. Inhibition of hiv-1 replication by disruption of the processing of the viral capsid-spacer peptide 1 protein
US7537765B2 (en) * 2003-01-29 2009-05-26 Panacos Pharmaceuticals, Inc. Inhibition of HIV-1 replication by disruption of the processing of the viral capsid-spacer peptide 1 protein
US7026305B2 (en) * 2003-04-14 2006-04-11 Meharry Medical College Anti-HIV agents with dual sites of action
EP1730163A4 (de) * 2004-03-17 2009-12-30 Panacos Pharmaceuticals Inc Pharmazeutische salze von 3-o-(3,3-dimethylsuccinyl)betulinsäure
CN100591688C (zh) * 2004-03-17 2010-02-24 帕纳克斯医药公司 3-0-(3＇,3＇-二甲基琥珀酰基)桦木酸的药用盐
US20060019934A1 (en) * 2004-05-20 2006-01-26 Saxena Brij B Anti-HIV-1 activity of betulinol derivatives
MXPA06013698A (es) * 2004-05-24 2007-08-15 Panacos Pharmaceuticals Inc Inhibicion de replicacion de virus 1 de inmunodeficiencia humana (vih-1) por interrupcion del procesamiento de la proteina de capsida-peptido separador 1 viral.
US20060154904A1 (en) 2004-09-10 2006-07-13 Cornell Research Foundation, Inc. Betulinol derivatives as anti-HIV agents
TW200628161A (en) * 2004-11-12 2006-08-16 Panacos Pharmaceuticals Inc Novel betulin derivatives, preparation thereof and use thereof
RU2007141631A (ru) * 2005-04-12 2009-05-20 Панакос Фармасьютикалз, Инк. (Us) Полиморфы ди-n-метил-d-глюкамина 3-о-(3',3'-диметилсукцинил)бетулиновой кислоты
EP1893629A4 (de) * 2005-06-22 2008-12-17 Myriad Genetics Inc Antivirale verbindungen
AU2006333084A1 (en) * 2005-12-16 2007-07-12 Panacos Pharmaceuticals, Inc. Preparation of pharmaceutical salts of 3-O-(3',3'-dimethylsuccinyl) betulinic acid
WO2007114978A2 (en) * 2006-02-09 2007-10-11 Boehringer Ingelheim International Gmbh Method for treating hiv infection through co-administration of tipranavir and pa-457
US20070232577A1 (en) * 2006-03-23 2007-10-04 Advanced Life Sciences, Inc. Synthetic pentacyclic triterpenoids and derivatives of betulinic acid and betulin
US20080039428A1 (en) * 2006-06-29 2008-02-14 Panacos Pharmaceuticals, Inc. Antiretroviral combination therapy
US20090105203A1 (en) * 2006-10-16 2009-04-23 Myriad Genetics, Incorporated Compounds for treating viral infections
WO2008057420A2 (en) 2006-11-03 2008-05-15 Panacos Pharmaceuticals, Inc. Extended triterpene derivatives
US20110152229A1 (en) * 2006-11-22 2011-06-23 Duke University Betulinic acid derivatives as anti-hiv agents
US9067966B2 (en) 2009-07-14 2015-06-30 Hetero Research Foundation, Hetero Drugs Ltd. Lupeol-type triterpene derivatives as antivirals
PL2576586T3 (pl) * 2010-06-04 2016-01-29 Bristol Myers Squibb Co C-28 amidy zmodyfikowanych pochodnych kwasu C-3 betulinowego jako inhibitory dojrzewania HIV
EA022393B1 (ru) * 2010-06-04 2015-12-30 Бристол-Майерс Сквибб Компани С-3 модифицированные производные бетулиновой кислоты в качестве ингибиторов созревания вич
RU2448115C1 (ru) * 2010-12-20 2012-04-20 Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Новосибирский национальный исследовательский государственный университет" (Новосибирский государственный университет (НГУ) Гидрированная бетулоновая кислота и ее амиды как противоопухолевые средства тритерпеновой природы
EA022470B1 (ru) 2011-01-31 2016-01-29 Бристол-Маерс Сквибб Компани C-17 и c-3 модифицированные тритерпеноиды с ингибиторной активностью созревания вич
PL2670764T3 (pl) 2011-01-31 2016-02-29 Bristol Myers Squibb Co C-28 aminy zmodyfikowanych C-3 pochodnych kwasu betulinowego jako inhibitory dojrzewania HIV
KR20140069167A (ko) 2011-09-21 2014-06-09 브리스톨-마이어스 스큅 컴퍼니 항바이러스 활성을 갖는 신규 베툴린산 유도체
US8906889B2 (en) 2012-02-15 2014-12-09 Bristol-Myers Squibb Company C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity
US8889854B2 (en) 2012-05-07 2014-11-18 Bristol-Myers Squibb Company C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity
CN103768078B (zh) 2012-10-22 2019-02-05 北京大学 三萜衍生物及其抗流感用途
WO2014105926A1 (en) 2012-12-31 2014-07-03 Hetero Research Foundation Novel betulinic acid proline derivatives as hiv inhibitors
CA2900124A1 (en) 2013-02-06 2014-08-14 Bristol-Myers Squibb Company C-19 modified triterpenoids with hiv maturation inhibitory activity
JP6186012B2 (ja) 2013-02-25 2017-08-23 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｃ−３アルキルおよびアルケニル修飾ベツリン酸誘導体
HUE051719T2 (hu) 2014-04-11 2021-03-29 Viiv Healthcare Uk No 4 Ltd Triterpenoidok HIV érésgátló aktivitással, amelyek a 3-helyzetben egy halogénalkil-szubsztituenst hordozó nem-aromás gyûrûvel helyettesítettek
WO2015195776A1 (en) 2014-06-19 2015-12-23 Bristol-Myers Squibb Company Betulinic acid derivatives with hiv maturation inhibitory activity
US20170129916A1 (en) 2014-06-26 2017-05-11 Hetero Research Foundation Novel betulinic proline imidazole derivatives as hiv inhibitors
US9969767B2 (en) 2014-11-14 2018-05-15 VIIV Healthcare UK (No.5) Limited Oxolupene derivatives
CA2967684A1 (en) 2014-11-14 2016-05-19 VIIV Healthcare UK (No.5) Limited C17-aryl substituted betulinic acid analogs
MA40886B1 (fr) 2015-02-09 2020-03-31 Hetero Research Foundation Nouveau triterpénone en c-3 avec des dérivés d'amide inverse en c-28 en tant qu'inhibiteurs du vih
WO2016147099A2 (en) 2015-03-16 2016-09-22 Hetero Research Foundation C-3 novel triterpenone with c-28 amide derivatives as hiv inhibitors
PL227790B1 (pl) 2015-08-13 2018-01-31 Slaski Univ Medyczny W Katowicach Fosfoniany acetylenowych pochodnych betuliny o działaniu przeciwnowotworowym, sposób ich wytwarzania i zastosowanie.
AR107512A1 (es) 2016-02-04 2018-05-09 VIIV HEALTHCARE UK Nº 5 LTD Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1
EP3606532A4 (de) * 2017-04-06 2020-11-18 Derm-Biome Pharmaceuticals Inc. Zusammensetzungen und verfahren zur behandlung von infektionen und neuen kosmetischen zubereitungen
PL237998B1 (pl) 2018-05-28 2021-06-28 Narodowy Inst Lekow Fosfonowe pochodne kwasu 3-karboksyacylobetulinowego, sposób ich otrzymywania oraz ich zastosowanie
NZ769842A (en) 2018-06-29 2023-01-27 Dfh Therapeutics Triterpene amine derivatives

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1415601A (en) * 1973-03-14 1975-11-26 Biorex Laboratories Ltd Dihydrobetulinic acid derivatives
FR2683531B1 (fr) * 1991-11-13 1993-12-31 Rhone Poulenc Rorer Sa Nouveaux derives du lupane, leur preparation et les compositions pharmaceutiques qui les contiennent.
US5643884A (en) * 1993-08-09 1997-07-01 Glycomed Incorporated Lupane triterpenoid derivatives

Also Published As

Publication number Publication date
ATE275823T1 (de) 2004-10-15
PT857018E (pt) 2005-01-31
WO1996039033A1 (en) 1996-12-12
EP0857018A4 (de) 2002-10-23
EP1397957A2 (de) 2004-03-17
CA2223513C (en) 2009-03-24
DK0857018T3 (da) 2004-11-29
ES2231818T3 (es) 2005-05-16
DE69633398T2 (de) 2005-09-22
CA2223513A1 (en) 1996-12-12
AU6328896A (en) 1996-12-24
DE69633398T8 (de) 2006-01-12
EP0857018A1 (de) 1998-08-12
US5679828A (en) 1997-10-21
EP0857018B1 (de) 2004-09-15

Similar Documents

Publication Publication Date Title
DE69633398D1 (de) Betulinsäure-derivate und ihre verwendungen
TR199700844T1 (xx) Pirazolil-Benzoil T�revleri.
UA35592C2 (uk) Похідні оцтової кислоти
DK210688A (da) 4-demethoxy-4-amino-anthracyclinderivater
SE8604089D0 (sv) 2-oxo-1-//(substituerad sulfonyl)amino/karbonyl/-azetidiner
FI911286A0 (fi) Kemiska foereningar.
DE3485100D1 (de) Topische antibiotische zusammensetzung zur behandlung der schleimhaeute.
AU6872687A (en) Unsaturated amino acids
AU590042B2 (en) Benzazecine Derivatives
FI951992A0 (fi) Uusia substituoituja atsetidinoneja anti-inflammatorisina ja antidegeneratiivisina aineina
ES8604604A1 (es) Un procedimiento para la produccion de 3,3",4"-tri-o-acilespiramicina i"-.
DE69014196D1 (de) 3,6-diamino-2,5-pyrazindicarbonitril und ihre herstellung.
ES2181858T3 (es) Procedimiento de preparacion de (met)acrilato de alquilimidazolidona.
TR199801366T2 (en) �zooksasefem t�revleri.
TR199901956T2 (xx) 4H-4-Okso-kinolizin-3-karboksilik asit t�revlerinin haz�rlanmas� i�in bir i�lem.
JPS5346984A (en) Oxazolidine derivatives
IT1226143B (it) 1,2 di o acil glicerofosfato l carnitina estere e suoi derivati, procedimento per la sua preparazione e composizioni farmaceutiche che li contengono.
IT1226142B (it) 1,2 di o acil glicerodifosfato di l carnitina estere e suoi derivati, procedimento per la sua preparazione e composizioni farmaceutiche che lo contengono.
ES8604885A2 (es) Mejoras en el objeto de la patente de invencion n 527.268 que se refiere a procedimiento de obtencion de nuevos derivados imidazolicos del acido 2-hidroxibenzoico
SE9601483L (sv) Beredning av komposition

Legal Events

Date Code Title Description
8327 Change in the person/name/address of the patent owner

Owner name: UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, CHAPE

Owner name: PANACOS PHARMACEUTICALS, INC., GAITHERSBURG, MD.,

8364 No opposition during term of opposition
8327 Change in the person/name/address of the patent owner

Owner name: UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, C, US

Owner name: PANACOS PHARMACEUTICALS, INC., GAITHERSBURG, M, US