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 EP94911239A priority patent/EP0691852B1/en
Priority to DE69433560T priority patent/DE69433560T2/de
Priority to AU63808/94A priority patent/AU682029B2/en
Priority to AT94911239T priority patent/ATE259661T1/de
Priority to CA002159610A priority patent/CA2159610C/en
Priority to JP52182794A priority patent/JP3900533B2/ja
Priority to US08/481,243 priority patent/US5985854A/en
Priority to SG9607743A priority patent/SG81890A1/en
Priority to KR1019950704313A priority patent/KR100400075B1/ko
Priority to NZ263208A priority patent/NZ263208A/en
Priority to HU9502866A priority patent/HU221678B1/hu
Priority to PCT/GB1994/000669 priority patent/WO1994022483A2/en
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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/10—Phosphatides, e.g. lecithin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A61K47/544—Phospholipids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (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
PCT/GB1994/000669 WO1994022483A2 (en) 1993-03-31 1994-03-30 Prodrugs with enhanced penetration into cells
JP52182794A JP3900533B2 (ja) 1993-03-31 1994-03-30 細胞への浸透増進プロドラッグ
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
AU63808/94A AU682029B2 (en) 1993-03-31 1994-03-30 Prodrugs with enhanced penetration into cells
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
EP94911239A EP0691852B1 (en) 1993-03-31 1994-03-30 Valproic acid covalently bonded to a lysophospholipid
US08/481,243 US5985854A (en) 1993-03-31 1994-03-30 Prodrugs with enhanced penetration into cells
DE69433560T DE69433560T2 (de) 1993-03-31 1994-03-30 Valproinsäure kovalent gebunden an einem lysophospholipid
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
HU9502866A HU221678B1 (hu) 1993-03-31 1994-03-30 Szupranormál intracelluláris enzimaktivitással összefüggő betegségek kezelésére alkalmas prodrugok
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 (ja)
EP (1) EP0691852B1 (ja)
JP (1) JP3900533B2 (ja)
KR (1) KR100400075B1 (ja)
AT (1) ATE259661T1 (ja)
AU (1) AU682029B2 (ja)
CA (1) CA2159610C (ja)
DE (1) DE69433560T2 (ja)
HU (1) HU221678B1 (ja)
IL (1) IL105244A (ja)
NZ (1) NZ263208A (ja)
SG (1) SG81890A1 (ja)
WO (1) WO1994022483A2 (ja)

Families Citing this family (36)

* 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
DE69535758D1 (de) * 1994-08-29 2008-07-03 Univ Wake Forest Lipid-analoge zur behandlung von viralen infektionen
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
AU6485496A (en) * 1995-07-14 1997-02-18 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
WO1998035701A1 (en) 1997-02-11 1998-08-20 Theramark Limited Drug targeting
WO1998041213A1 (en) * 1997-03-19 1998-09-24 Lxr Biotechnology Inc. Compositions containing lysophosphotidic acids which inhibit apoptosis and uses thereof
DE69840216D1 (de) 1997-08-08 2008-12-24 Celmed Oncology Usa Inc Verfahren und Zubereitungen um Resistenz gegen biologische oder chemische Therapien zu Überwinden
EP1240922B1 (en) * 1997-08-08 2008-11-12 Celmed Oncology (USA), Inc. Methods and compositions for overcoming resistance to biologic and chemotherapy
TWI244924B (en) * 1998-01-23 2005-12-11 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
IL147749A0 (en) * 1999-07-22 2002-08-14 Newbiotics Inc Methods for treating therapy-resistant tumors
US6683061B1 (en) * 1999-07-22 2004-01-27 Newbiotics, Inc. Enzyme catalyzed therapeutic activation
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
CZ20022507A3 (cs) * 2000-01-20 2003-01-15 Omegatech, Inc. Způsob chování králíků
AU2001257490A1 (en) * 2000-05-02 2001-11-12 Newbiotics, Inc. Improved beta-lactam antibiotics
US7309696B2 (en) 2000-10-19 2007-12-18 Wake Forest University Compositions and methods for targeting cancer cells
EP1359921A4 (en) 2001-01-19 2006-09-06 Newbiotics Inc METHOD FOR THE TREATMENT OF AUTOIMMUNE DISEASES AND INFLAMMATORY DISEASES
US8552054B2 (en) 2001-03-23 2013-10-08 Luitpold Pharmaceuticals, Inc. Fatty amine drug conjugates
EP1423107B1 (en) 2001-03-23 2012-05-09 Luitpold Pharmaceuticals, Inc. Fatty alcohol drug conjugates
AU2003211052A1 (en) 2002-02-11 2003-09-04 Vertex Pharmaceuticals Incorporated Phospholipids as 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
WO2014117176A1 (en) * 2013-01-28 2014-07-31 Lopez Hector L Methods of improving tolerability, pharmacodynamics, and efficacy of b-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 (ja) * 1900-01-01
DE3067662D1 (en) * 1980-01-16 1984-06-07 Lacer Sa New 2-halo-pyridines, their production and pharmaceutical compositions
US5223263A (en) * 1988-07-07 1993-06-29 Vical, Inc. Liponucleotide-containing liposomes
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
IT1201149B (it) * 1987-01-14 1989-01-27 Indena Spa Complessi di bioflavonoidi con fosfolipidi,loro preparazione,uso e composizioni farmaceutici e cosmetiche
WO1989005358A1 (en) * 1987-11-30 1989-06-15 University Of Iowa Research Foundation Dna and rna molecules stabilized by modifications of the 3'-terminal phosphodiester linkage and their use as nucleic acid probes and as therapeutic agents to block the expression of specifically targeted genes
DE3801587A1 (de) * 1988-01-21 1989-08-03 Hoechst Ag Neue aminosaeureglyceride, verfahren zu ihrer herstellung, sie enthaltende arzneimittel und deren verwendung
ES2055907T3 (es) * 1989-03-07 1994-09-01 Genentech Inc Conjugados covalentes de lipidos y oligonucleotidos.
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
AU7872491A (en) * 1990-05-07 1991-11-27 Vical, Inc. Lipid prodrugs of salicylate and nonsteroidal anti-inflammatory drugs
CH679856A5 (ja) * 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
CA2112803A1 (en) * 1991-07-12 1993-01-21 Karl Y. Hostetler 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
AU6380894A (en) 1994-10-24
WO1994022483A2 (en) 1994-10-13
HUT73669A (en) 1996-09-30
IL105244A0 (en) 1993-07-08
ATE259661T1 (de) 2004-03-15
HU221678B1 (hu) 2002-12-28
AU682029B2 (en) 1997-09-18
NZ263208A (en) 1997-06-24
JPH08508295A (ja) 1996-09-03
SG81890A1 (en) 2001-07-24
CA2159610C (en) 2008-05-20
US6136796A (en) 2000-10-24
US5985854A (en) 1999-11-16
DE69433560D1 (de) 2004-03-25
KR100400075B1 (ko) 2004-02-25
WO1994022483A3 (en) 1994-12-22
JP3900533B2 (ja) 2007-04-04
DE69433560T2 (de) 2004-12-16
EP0691852B1 (en) 2004-02-18
CA2159610A1 (en) 1994-10-01
HU9502866D0 (en) 1995-11-28
EP0691852A1 (en) 1996-01-17

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