IL105244A - Prodrugs with enhanced penetration into cells - Google Patents

Prodrugs with enhanced penetration into cells

Info

Publication number
IL105244A
IL105244A IL10524493A IL10524493A IL105244A IL 105244 A IL105244 A IL 105244A IL 10524493 A IL10524493 A IL 10524493A IL 10524493 A IL10524493 A IL 10524493A IL 105244 A IL105244 A IL 105244A
Authority
IL
Israel
Prior art keywords
activity
cells
intracellular enzyme
glycerophosphoryl
choline
Prior art date
Application number
IL10524493A
Other languages
English (en)
Other versions
IL105244A0 (en
Inventor
Alexander Kozak
Original Assignee
Dpharm 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 Dpharm Ltd filed Critical Dpharm Ltd
Priority to IL10524493A priority Critical patent/IL105244A/xx
Publication of IL105244A0 publication Critical patent/IL105244A0/xx
Priority to KR1019950704313A priority patent/KR100400075B1/ko
Priority to AU63808/94A priority patent/AU682029B2/en
Priority to CA002159610A priority patent/CA2159610C/en
Priority to PCT/GB1994/000669 priority patent/WO1994022483A2/en
Priority to HU9502866A priority patent/HU221678B1/hu
Priority to EP94911239A priority patent/EP0691852B1/de
Priority to NZ263208A priority patent/NZ263208A/en
Priority to AT94911239T priority patent/ATE259661T1/de
Priority to US08/481,243 priority patent/US5985854A/en
Priority to SG9607743A priority patent/SG81890A1/en
Priority to JP52182794A priority patent/JP3900533B2/ja
Priority to DE69433560T priority patent/DE69433560T2/de
Priority to US09/270,392 priority patent/US6136796A/en
Priority to US09/777,324 priority patent/US6355629B2/en
Publication of IL105244A publication Critical patent/IL105244A/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/08Esters of oxyacids of phosphorus
    • C07F9/09Esters of phosphoric acids
    • C07F9/10Phosphatides, e.g. lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A61K47/544Phospholipids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
IL10524493A 1993-03-13 1993-03-31 Prodrugs with enhanced penetration into cells IL105244A (en)

Priority Applications (15)

Application Number Priority Date Filing Date Title
IL10524493A IL105244A (en) 1993-03-31 1993-03-31 Prodrugs with enhanced penetration into cells
DE69433560T DE69433560T2 (de) 1993-03-31 1994-03-30 Valproinsäure kovalent gebunden an einem lysophospholipid
EP94911239A EP0691852B1 (de) 1993-03-31 1994-03-30 Valproinsäure kovalent gebunden an einem lysophospholipid
AT94911239T ATE259661T1 (de) 1993-03-31 1994-03-30 Valproinsäure kovalent gebunden an einem lysophospholipid
CA002159610A CA2159610C (en) 1993-03-31 1994-03-30 Prodrugs with enhanced penetration into cells
PCT/GB1994/000669 WO1994022483A2 (en) 1993-03-31 1994-03-30 Prodrugs with enhanced penetration into cells
HU9502866A HU221678B1 (hu) 1993-03-31 1994-03-30 Szupranormál intracelluláris enzimaktivitással összefüggő betegségek kezelésére alkalmas prodrugok
KR1019950704313A KR100400075B1 (ko) 1993-03-31 1994-03-30 세포로의침투가개선된약제
NZ263208A NZ263208A (en) 1993-03-31 1994-03-30 Pharmaceutically acceptable prodrug which is a covalent conjugate of an active and an intracellular transporting adjuvant, having a scission-sensitive covalent bond
AU63808/94A AU682029B2 (en) 1993-03-31 1994-03-30 Prodrugs with enhanced penetration into cells
US08/481,243 US5985854A (en) 1993-03-31 1994-03-30 Prodrugs with enhanced penetration into cells
SG9607743A SG81890A1 (en) 1993-03-31 1994-03-30 Compounds for treating a condition or disease in a human related to supranormal intracellular enzyme activity
JP52182794A JP3900533B2 (ja) 1993-03-31 1994-03-30 細胞への浸透増進プロドラッグ
US09/270,392 US6136796A (en) 1993-03-13 1999-03-16 Prodrugs with enhanced penetration into cells
US09/777,324 US6355629B2 (en) 1993-03-31 2001-02-06 Prodrugs with enhanced penetration into cells

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IL10524493A IL105244A (en) 1993-03-31 1993-03-31 Prodrugs with enhanced penetration into cells

Publications (2)

Publication Number Publication Date
IL105244A0 IL105244A0 (en) 1993-07-08
IL105244A true IL105244A (en) 2003-07-31

Family

ID=11064681

Family Applications (1)

Application Number Title Priority Date Filing Date
IL10524493A IL105244A (en) 1993-03-13 1993-03-31 Prodrugs with enhanced penetration into cells

Country Status (13)

Country Link
US (2) US5985854A (de)
EP (1) EP0691852B1 (de)
JP (1) JP3900533B2 (de)
KR (1) KR100400075B1 (de)
AT (1) ATE259661T1 (de)
AU (1) AU682029B2 (de)
CA (1) CA2159610C (de)
DE (1) DE69433560T2 (de)
HU (1) HU221678B1 (de)
IL (1) IL105244A (de)
NZ (1) NZ263208A (de)
SG (1) SG81890A1 (de)
WO (1) WO1994022483A2 (de)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5714167A (en) * 1992-06-15 1998-02-03 Emisphere Technologies, Inc. Active agent transport systems
US5827819A (en) * 1990-11-01 1998-10-27 Oregon Health Sciences University Covalent polar lipid conjugates with neurologically active compounds for targeting
US6916489B2 (en) 1992-06-15 2005-07-12 Emisphere Technologies, Inc. Active agent transport systems
JP4259611B2 (ja) * 1994-08-29 2009-04-30 ウェイク フォレスト ユニバーシティ ウィルス感染を治療するための脂質アナログ
US7135584B2 (en) * 1995-08-07 2006-11-14 Wake Forest University Lipid analogs for treating viral infections
US6313106B1 (en) * 1995-06-07 2001-11-06 D-Pharm Ltd. Phospholipid derivatives of valproic acid and mixtures thereof
WO1997003701A2 (en) * 1995-07-14 1997-02-06 Glycotech Corp. Compounds and methods for treatment of egf receptor associated cancers and purification of the egf receptor
US6350780B1 (en) * 1995-07-28 2002-02-26 Allergan Sales, Inc. Methods and compositions for drug delivery
US5795909A (en) 1996-05-22 1998-08-18 Neuromedica, Inc. DHA-pharmaceutical agent conjugates of taxanes
US6576636B2 (en) 1996-05-22 2003-06-10 Protarga, Inc. Method of treating a liver disorder with fatty acid-antiviral agent conjugates
ATE247984T1 (de) 1997-02-11 2003-09-15 Univ Manchester Bioreduktive konjugate zur gezielten wirkstoffzufuhr
DE69836972D1 (de) * 1997-03-19 2007-03-15 Sky High Llc Lysophophasäure enthaltende zusammensetzungen die die apoptose hemmen und deren verwendung
EP1240922B1 (de) * 1997-08-08 2008-11-12 Celmed Oncology (USA), Inc. Verfahren und Zubereitungen um Resistenz gegen biologische oder chemische Therapien zu Überwinden
WO1999008110A1 (en) 1997-08-08 1999-02-18 Newbiotics, Inc. Methods and compositions for overcoming resistance to biologic and chemotherapy
IL137164A0 (en) * 1998-01-23 2001-07-24 Newbiotics Inc Enzyme catalyzed therapeutic agents
US7462605B2 (en) 1998-01-23 2008-12-09 Celmed Oncology (Usa), Inc. Phosphoramidate compounds and methods of use
US7235583B1 (en) 1999-03-09 2007-06-26 Luitpold Pharmaceuticals, Inc., Fatty acid-anticancer conjugates and uses thereof
US6683061B1 (en) * 1999-07-22 2004-01-27 Newbiotics, Inc. Enzyme catalyzed therapeutic activation
BR0012676A (pt) * 1999-07-22 2003-07-01 Newbiotics Inc Métodos para tratamento de tumores resistentes a terapia
IL131887A0 (en) 1999-09-14 2001-03-19 Dpharm Ltd Phospholipid prodrugs of anti-proliferative drugs
US6670341B1 (en) 1999-10-28 2003-12-30 Wake Forest University Health Sciences Compositions and methods for double-targeting virus infections and targeting cancer cells
US7026469B2 (en) 2000-10-19 2006-04-11 Wake Forest University School Of Medicine Compositions and methods of double-targeting virus infections and cancer cells
US6568351B1 (en) * 2000-01-20 2003-05-27 Martek Biosciences Boulder Corporation Methods for raising rabbits
WO2001083492A1 (en) * 2000-05-02 2001-11-08 Newbiotics, Inc. Improved beta-lactam antibiotics
US7309696B2 (en) 2000-10-19 2007-12-18 Wake Forest University Compositions and methods for targeting cancer cells
US7138388B2 (en) 2001-01-19 2006-11-21 Celmed Oncology (Usa), Inc. Methods to treat autoimmune and inflammatory conditions
ES2387562T3 (es) 2001-03-23 2012-09-26 Luitpold Pharmaceuticals, Inc. Conjugados alcohol graso-medicamento
EP1427407A4 (de) 2001-03-23 2005-05-11 Luitpold Pharm Inc Fettamin-arzneimittel-konjugate
US7410956B2 (en) 2002-02-11 2008-08-12 Vertex Pharmaceuticals Incorporated Caspase inhibitor prodrugs
US20050187191A1 (en) * 2004-02-20 2005-08-25 Kucera Louis S. Methods and compositions for the treatment of respiratory syncytial virus
USD692565S1 (en) * 2010-06-03 2013-10-29 Smith & Nephew, Inc. Organ protection layer
CA140188S (en) 2010-10-15 2011-11-07 Smith & Nephew Medical dressing
CA140189S (en) 2010-10-15 2011-11-07 Smith & Nephew Medical dressing
CA2903000C (en) * 2013-01-28 2021-10-12 Hector L. Lopez Methods of improving tolerability, pharmacodynamics, and efficacy of .beta.-alanine and use therefor
CN108659038B (zh) * 2017-03-31 2022-01-11 江苏恩华药业股份有限公司 1-硬脂酰-2-丙戊酰-sn-甘油-3-磷脂酰胆碱的多晶型物及制备方法
CN110407867A (zh) * 2018-04-28 2019-11-05 江苏恩华药业股份有限公司 丙戊酸磷脂衍生物的新晶型及其制备方法
CN111334369B (zh) * 2020-03-11 2022-10-21 陕西科技大学 一种酶法制备卵磷脂型pufa的方法

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR244F (de) * 1900-01-01
ATE7295T1 (de) * 1980-01-16 1984-05-15 Lacer, S.A. 2-halo-pyridine, ihre herstellung und pharmazeutische zusammensetzungen.
US5223263A (en) * 1988-07-07 1993-06-29 Vical, Inc. Liponucleotide-containing liposomes
IT1201149B (it) * 1987-01-14 1989-01-27 Indena Spa Complessi di bioflavonoidi con fosfolipidi,loro preparazione,uso e composizioni farmaceutici e cosmetiche
IT1201151B (it) * 1987-01-14 1989-01-27 Indena Spa Complessi fosfolipidici con estratti da vitis vinifera,procedimento per la loro preparazione e composizioni che li cntengono
ATE151467T1 (de) * 1987-11-30 1997-04-15 Univ Iowa Res Found Durch modifikationen an der 3'-terminalen phosphodiesterbindung stabilisierte dna moleküle, ihre verwendung als nukleinsäuresonden sowie als therapeutische mittel zur hemmung der expression spezifischer zielgene
DE3801587A1 (de) * 1988-01-21 1989-08-03 Hoechst Ag Neue aminosaeureglyceride, verfahren zu ihrer herstellung, sie enthaltende arzneimittel und deren verwendung
CA2049028A1 (en) * 1989-03-07 1990-09-08 Genentech, Inc. Covalent conjugates of lipid and oligonucleotide
JPH03133987A (ja) * 1989-10-18 1991-06-07 Kowa Yakuhin Kogyo Kk 2‐マイトマイシンc‐スクシニル‐1,3‐ジパルミトイルグリセロールおよびその製造法
JPH03275625A (ja) * 1990-03-23 1991-12-06 Nippon Oil & Fats Co Ltd 制癌剤およびその製造法
WO1991016920A1 (en) * 1990-05-07 1991-11-14 Vical, Inc. Lipid prodrugs of salicylate and nonsteroidal anti-inflammatory drugs
CH679856A5 (de) * 1990-07-04 1992-04-30 Lonza Ag
US5149794A (en) * 1990-11-01 1992-09-22 State Of Oregon Covalent lipid-drug conjugates for drug targeting
WO1992017185A1 (en) * 1991-03-29 1992-10-15 University Of Florida Targeted drug delivery via mixed phosphate derivatives
AU668873B2 (en) * 1991-07-12 1996-05-23 Chimerix, Inc. Antiviral liponucleosides: treatment of hepatitis B
US6015834A (en) * 1992-10-20 2000-01-18 Toronto Neuroprotection Group In vivo treatment of mammalian cells with a cell membrane permeant calcium buffer

Also Published As

Publication number Publication date
WO1994022483A2 (en) 1994-10-13
US6136796A (en) 2000-10-24
HUT73669A (en) 1996-09-30
CA2159610A1 (en) 1994-10-01
DE69433560D1 (de) 2004-03-25
AU682029B2 (en) 1997-09-18
US5985854A (en) 1999-11-16
IL105244A0 (en) 1993-07-08
EP0691852B1 (de) 2004-02-18
EP0691852A1 (de) 1996-01-17
AU6380894A (en) 1994-10-24
JP3900533B2 (ja) 2007-04-04
KR100400075B1 (ko) 2004-02-25
NZ263208A (en) 1997-06-24
WO1994022483A3 (en) 1994-12-22
ATE259661T1 (de) 2004-03-15
HU9502866D0 (en) 1995-11-28
JPH08508295A (ja) 1996-09-03
HU221678B1 (hu) 2002-12-28
CA2159610C (en) 2008-05-20
SG81890A1 (en) 2001-07-24
DE69433560T2 (de) 2004-12-16

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