[go: up one dir, main page]

WO1993001203A1 - Derive d'amphotericine antimycosique - Google Patents

Derive d'amphotericine antimycosique Download PDF

Info

Publication number
WO1993001203A1
WO1993001203A1 PCT/GB1992/001209 GB9201209W WO9301203A1 WO 1993001203 A1 WO1993001203 A1 WO 1993001203A1 GB 9201209 W GB9201209 W GB 9201209W WO 9301203 A1 WO9301203 A1 WO 9301203A1
Authority
WO
WIPO (PCT)
Prior art keywords
decarboxy
ascorbate salt
hydroxymethylamphotericin
amphotericin
ascorbate
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.)
Ceased
Application number
PCT/GB1992/001209
Other languages
English (en)
Inventor
David Timothy Macpherson
Alexander Richard Greenless
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.)
SmithKline Beecham Ltd
Original Assignee
SmithKline Beecham Ltd
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 SmithKline Beecham Ltd filed Critical SmithKline Beecham Ltd
Publication of WO1993001203A1 publication Critical patent/WO1993001203A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins

Definitions

  • EP-A-0375222 (Beecham Group p.l.c.) discloses a class of compounds which are described as possessing anti-fungal activity.
  • One compound which is specifically mentioned in this patent specification is Example 4 i.e. 16-decarboxy-16-hydroxymethylamphotericin B. This compound is only described as the free base which has been found to possess poor solubility in aqueous media.
  • the present invention further provides the L- ascorbate salt of 16- decarboxy-16-hydroxymethylamphotericin B in substantially pure form.
  • the L- ascorbate salt or 16-decarboxy-16- hydroxymethylamphotericin B can be administered alone, but will generally be administered in admixture with a pharmaceutical carrier selected with regard to the intended route of administration and standard pharmaceutical practice.
  • a pharmaceutical carrier selected with regard to the intended route of administration and standard pharmaceutical practice.
  • it may be administered orally in the form of a tablet containing such excipients as starch or lactose, or in a capsule or ovule either alone or in admixture with excipients, or in the form of an elixir or suspension containing a flavouring or colouring agent.
  • It may be injected parenterally, for example, intravenously, intramuscularly or subcutaneously.
  • parenteral administration it is best used in the form of a sterile aqueous solution which may contain other substances, for example, enough salts or glucose to make the solution isotonic
  • a compound for use as an active therapeutic substance is intended for use in the treatment of disorders in animals including humans.
  • the L- ascorbate salt of 16-decarboxy-16- hydroxymethylamphotericin B has anti-fungal activity and is potentially useful in combating fungal infections in animals including humans.
  • the present invention further provides the L- ascorbate salt of 16-decarboxy-16-hydroxymethylamphotericin B for use in the treatment of fungal infections.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention se rapporte au sel de L-ascorbate de 16-décarboxy-16-hydroxyméthylamphotéricine B, à un procédé de préparation et à son utilisation comme agent antimycosique.
PCT/GB1992/001209 1991-07-11 1992-07-03 Derive d'amphotericine antimycosique Ceased WO1993001203A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9114949.2 1991-07-11
GB919114949A GB9114949D0 (en) 1991-07-11 1991-07-11 Novel compounds

Publications (1)

Publication Number Publication Date
WO1993001203A1 true WO1993001203A1 (fr) 1993-01-21

Family

ID=10698172

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB1992/001209 Ceased WO1993001203A1 (fr) 1991-07-11 1992-07-03 Derive d'amphotericine antimycosique

Country Status (7)

Country Link
AU (1) AU2230892A (fr)
GB (1) GB9114949D0 (fr)
IE (1) IE922264A1 (fr)
MX (1) MX9204031A (fr)
PT (1) PT100671B (fr)
TW (1) TW199894B (fr)
WO (1) WO1993001203A1 (fr)

Cited By (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7960506B2 (en) 2006-12-14 2011-06-14 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US7981998B2 (en) 2006-12-14 2011-07-19 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US7981999B2 (en) 2007-02-23 2011-07-19 Aileron Therapeutics, Inc. Triazole macrocycle systems
US9096684B2 (en) 2011-10-18 2015-08-04 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9527896B2 (en) 2007-01-31 2016-12-27 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
US9604919B2 (en) 2012-11-01 2017-03-28 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
US9951099B2 (en) 1999-05-18 2018-04-24 President And Fellows Of Harvard College Stabilized compounds having secondary structure motifs
US9957299B2 (en) 2010-08-13 2018-05-01 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10022422B2 (en) 2009-01-14 2018-07-17 Alleron Therapeutics, Inc. Peptidomimetic macrocycles
US10023613B2 (en) 2015-09-10 2018-07-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles as modulators of MCL-1
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10213477B2 (en) 2012-02-15 2019-02-26 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10227380B2 (en) 2012-02-15 2019-03-12 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
US10253067B2 (en) 2015-03-20 2019-04-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10301351B2 (en) 2007-03-28 2019-05-28 President And Fellows Of Harvard College Stitched polypeptides
US10300109B2 (en) 2009-09-22 2019-05-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10471120B2 (en) 2014-09-24 2019-11-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10905739B2 (en) 2014-09-24 2021-02-02 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and formulations thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0375223A2 (fr) * 1988-12-19 1990-06-27 Beecham Group Plc Dérivés de l'amphotéricine B, leur préparation et leur utilisation comme médicaments
EP0375222A2 (fr) * 1988-12-19 1990-06-27 Beecham Group Plc Dérivés d'amphotericin B
EP0431874A1 (fr) * 1989-12-08 1991-06-12 Beecham Group p.l.c. Nouveaux composés
EP0431870A1 (fr) * 1989-12-08 1991-06-12 Beecham Group p.l.c. DÀ©rivés d'amphotéricine B

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0375223A2 (fr) * 1988-12-19 1990-06-27 Beecham Group Plc Dérivés de l'amphotéricine B, leur préparation et leur utilisation comme médicaments
EP0375222A2 (fr) * 1988-12-19 1990-06-27 Beecham Group Plc Dérivés d'amphotericin B
EP0431874A1 (fr) * 1989-12-08 1991-06-12 Beecham Group p.l.c. Nouveaux composés
EP0431870A1 (fr) * 1989-12-08 1991-06-12 Beecham Group p.l.c. DÀ©rivés d'amphotéricine B

Cited By (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10487110B2 (en) 1999-05-18 2019-11-26 President And Fellows Of Harvard College Stabilized compounds having secondary structure motifs
US9951099B2 (en) 1999-05-18 2018-04-24 President And Fellows Of Harvard College Stabilized compounds having secondary structure motifs
US8609809B2 (en) 2006-12-14 2013-12-17 Aileron Thraputics, Inc. Bis-sulfhydryl macrocyclization systems
US9175056B2 (en) 2006-12-14 2015-11-03 Alleron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US10328117B2 (en) 2006-12-14 2019-06-25 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US7960506B2 (en) 2006-12-14 2011-06-14 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US9675661B2 (en) 2006-12-14 2017-06-13 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US7981998B2 (en) 2006-12-14 2011-07-19 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US9527896B2 (en) 2007-01-31 2016-12-27 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
US9957296B2 (en) 2007-02-23 2018-05-01 Aileron Therapeutics, Inc. Triazole macrocycle systems
US8637686B2 (en) 2007-02-23 2014-01-28 Aileron Therapeutics, Inc. Triazole macrocycle systems
US9023988B2 (en) 2007-02-23 2015-05-05 Aileron Therapeutics, Inc. Triazole macrocycle systems
US7981999B2 (en) 2007-02-23 2011-07-19 Aileron Therapeutics, Inc. Triazole macrocycle systems
US9493509B2 (en) 2007-02-23 2016-11-15 Aileron Therapeutics, Inc. Triazole macrocycle systems
US10030049B2 (en) 2007-02-23 2018-07-24 Aileron Therapeutics, Inc. Triazole macrocycle systems
US10301351B2 (en) 2007-03-28 2019-05-28 President And Fellows Of Harvard College Stitched polypeptides
US10022422B2 (en) 2009-01-14 2018-07-17 Alleron Therapeutics, Inc. Peptidomimetic macrocycles
US10300109B2 (en) 2009-09-22 2019-05-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9957299B2 (en) 2010-08-13 2018-05-01 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9522947B2 (en) 2011-10-18 2016-12-20 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9096684B2 (en) 2011-10-18 2015-08-04 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10308699B2 (en) 2011-10-18 2019-06-04 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10213477B2 (en) 2012-02-15 2019-02-26 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10227380B2 (en) 2012-02-15 2019-03-12 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
US10669230B2 (en) 2012-11-01 2020-06-02 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
US9845287B2 (en) 2012-11-01 2017-12-19 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
US9604919B2 (en) 2012-11-01 2017-03-28 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
US10471120B2 (en) 2014-09-24 2019-11-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10905739B2 (en) 2014-09-24 2021-02-02 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and formulations thereof
US10253067B2 (en) 2015-03-20 2019-04-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10023613B2 (en) 2015-09-10 2018-07-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles as modulators of MCL-1

Also Published As

Publication number Publication date
MX9204031A (es) 1993-01-01
PT100671B (pt) 1999-07-30
TW199894B (fr) 1993-02-11
IE922264A1 (en) 1993-01-13
GB9114949D0 (en) 1991-08-28
PT100671A (pt) 1993-10-29
AU2230892A (en) 1993-02-11

Similar Documents

Publication Publication Date Title
WO1993001203A1 (fr) Derive d'amphotericine antimycosique
CA1057754A (fr) Antihypertenseurs
KR20010072080A (ko) 페닐아졸 화합물, 그의 제조 방법 및 고지혈증용 약제
CN114763324A (zh) 一种脂质化合物及脂质体与药物组合物
US4724238A (en) Method of treating inflammatory diseases with labdan derivatives
CN112812099B (zh) 一种用于治疗消化性溃疡的化合物及其制法和用途
US4340760A (en) Monophenylamine derivatives
EP0375222B1 (fr) Dérivés d'amphotericin B
KR0185200B1 (ko) 폴리엔 마크로라이드 유도체
EP0906309B1 (fr) Forme modifiee de l'hydrochlorure de l'acide r(-)-n-(4,4-di(3-methylthien-2-yl)but-3-enyl)-nipecotique
US7049301B2 (en) Quercetin derivatives and their medical usages
WO1998043638A1 (fr) Agent therapeutique pour maladies auto-immunes
KR20010040292A (ko) (ｅ)-3-[1-ｎ-부틸-5-[2-(2-카르복시페닐)메톡시-4-클로로페닐]-1ｈ-피라졸-4-일]-2-[(5-메톡시-2,3-디히드로벤조푸란-6-일)메틸]-프로-2-펜산 모노아르기닌일 염
KR880001865B1 (ko) 4-(1-이미다졸일메틸)신남산 하이드로클로라이드 모노하이드레이트의 제조방법
EP1118324A1 (fr) Analgésique, contenant un dérivé d'acide cyclobutane dicarboxylique
US4755601A (en) Nonyl prenyl-N heterocyclics
US4322555A (en) Nonaprenylamine derivatives
EP0003286B1 (fr) Dérivés d'alcaloides ergopeptidiques, procédé pour leur préparation et compositions pharmaceutiques les contenant
JP3117251B2 (ja) １４−Ｏ−ｐ−クロロベンゾイルアコニンおよび鎮痛・抗炎症剤
US4297487A (en) Phosphonium salts
HU201082B (en) Enolethers of 6-chloro-4-hydroxy-2-methyl-N-(2-pyridyl)-2H-thieno(2,3-e)-1,2-thiazin-3-carboxylic acid amide-1,1-dioxide, a process for their preparation and their use.
DE2004301A1 (de) Phenylserinderivate
JP2790335B2 (ja) 共役γ―オキシブテノライド化合物およびこれを有効成分とする抗潰瘍剤
JPH062748B2 (ja) 新規ヒダントイン誘導体及び該化合物を有効成分として含有する医薬組成物
HUT62579A (en) Process for producing 5,7-dihydroxy-2-methyl-8-/4-(3-hydroxy)-1-(1-propyl)-piperidinyl/-4h-benzopyran-4-one and pharmaceutical compositions comprising such compound as active ingredient

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AU CA JP KR US

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): AT BE CH DE DK ES FR GB GR IT LU MC NL SE

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
NENP Non-entry into the national phase

Ref country code: CA

122 Ep: pct application non-entry in european phase