WO1993025197A1 - Compositions and methods for enhanced drug delivery - Google Patents

Compositions and methods for enhanced drug delivery Download PDF

Info

Publication number
WO1993025197A1
WO1993025197A1 PCT/US1993/005631 US9305631W WO9325197A1 WO 1993025197 A1 WO1993025197 A1 WO 1993025197A1 US 9305631 W US9305631 W US 9305631W WO 9325197 A1 WO9325197 A1 WO 9325197A1
Authority
WO
Grant status
Application
Patent type
Prior art keywords
ml
pharmaceutical agent
mg
chemical
mmol
Prior art date
Application number
PCT/US1993/005631
Other languages
English (en)
French (fr)
Inventor
Ron L. Hale
Amy Lu
Dennis Solas
Harold E. Selick
Kevin R. Oldenburg
Alejandro C. Zaffaroni
Original Assignee
Affymax Technologies N.V.
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

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET 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
    • A61K47/541Organic ions forming an ion pair complex with the pharmacologically or therapeutically active agent
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET 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
    • A61K47/69Medicinal 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6957Medicinal 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a device or a kit, e.g. stents or microdevices
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0002Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0009Galenical forms characterised by the drug release technique; Application systems commanded by energy involving or responsive to electricity, magnetism or acoustic waves; Galenical aspects of sonophoresis, iontophoresis, electroporation or electroosmosis
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B82NANOTECHNOLOGY
    • B82YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
PCT/US1993/005631 1992-06-12 1993-06-11 Compositions and methods for enhanced drug delivery WO1993025197A1 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
US89821992 true 1992-06-12 1992-06-12
US07/898,219 1992-06-12
US946393 true 1993-01-27 1993-01-27
US08/009,463 1993-01-27

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP19930915319 EP0647133A4 (en) 1992-06-12 1993-06-11 Compositions and methods for enhanced drug delivery.

Publications (1)

Publication Number Publication Date
WO1993025197A1 true true WO1993025197A1 (en) 1993-12-23

Family

ID=26679515

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1993/005631 WO1993025197A1 (en) 1992-06-12 1993-06-11 Compositions and methods for enhanced drug delivery

Country Status (2)

Country Link
EP (1) EP0647133A4 (it)
WO (1) WO1993025197A1 (it)

Cited By (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0678297A1 (en) * 1994-02-25 1995-10-25 Bristol-Myers Squibb Company Iontophoretic transdermal delivery of deoxyspergualin compounds
FR2727117A1 (fr) * 1994-11-18 1996-05-24 Geffard Michel Utilisation de conjugues de la polylysine pour la preparation de medicaments utiles dans le traitement des maladies neurodegeneratives et des affections degeneratives a caractere autoimmun
WO1996039422A2 (en) * 1995-06-06 1996-12-12 Alza Corporation Modification of polypeptide drugs to increase electrotransport flux
WO1996039423A2 (en) * 1995-06-06 1996-12-12 Alza Corporation A method for increasing the electrotransport flux of polypeptides
EP0773719A1 (en) * 1994-07-29 1997-05-21 Emory University Compositions for targeting materials to cells containing androgen receptors
EP0796841A1 (en) * 1996-03-20 1997-09-24 Sigma-Tau Industrie Farmaceutiche Riunite S.p.A. Bis alkanoyl esters of carnitine having bactericidal, fungicidal and antiprotozoal activity
US5721226A (en) * 1993-03-10 1998-02-24 Magainin Pharmaceuticals Inc. Method for inhibiting angiogenesis using squalamine and squalamine steroid derivatives
US5763430A (en) * 1995-06-07 1998-06-09 Magainin Pharmaceuticals Inc. Method of treating a viral infection by administering a steroid compound
US5792635A (en) * 1995-06-07 1998-08-11 Magainin Pharmaceuticals, Inc. Method of inhibiting the sodium/proton exchanger NHE3 and method of inhibiting growth by administering squalamine
US5795885A (en) * 1995-06-07 1998-08-18 Magainin Pharmaceuticals Inc. Method of inhibiting profileration of cells by administering an aminosterol compound
US5840936A (en) * 1995-06-07 1998-11-24 Magainin Pharmaceuticals Inc. Aminosterol compounds useful as inhibitors of the sodium/proton exchanger (NHE)
US5840740A (en) * 1995-06-07 1998-11-24 Magainin Pharmaceuticals Inc. Aminosterol compounds and a method of treating infection using the aminosterol compounds
US5847172A (en) * 1995-06-07 1998-12-08 Magainin Pharmaceuticals Inc. Certain aminosterol compounds and pharmaceutical compositions including these compounds
US5856535A (en) * 1994-08-18 1999-01-05 Magainin Pharmaceuticals, Inc. Aminosterol ester compounds
US5874597A (en) * 1995-06-07 1999-02-23 Magainin Pharmaceuticals, Inc. Certain aminosterol compounds and pharmaceutical compositions including these compounds
WO1999059957A1 (en) * 1998-05-15 1999-11-25 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase
US5994336A (en) * 1995-06-07 1999-11-30 Magainin Pharmaceuticals Inc. Method of inhibiting proliferation of cells by administering an aminosterol compound
US6143738A (en) * 1995-06-07 2000-11-07 Magainin Pharmaceuticals, Inc. Therapeutic uses for an aminosterol compound
US6147060A (en) * 1996-04-26 2000-11-14 Magainin Pharmaceuticals Treatment of carcinomas using squalamine in combination with other anti-cancer agents
US6262283B1 (en) 1996-12-06 2001-07-17 Magainin Pharmaceuticals Inc. Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin D analogs, and other compounds
US6333189B1 (en) 1996-06-06 2001-12-25 Alza Corporation Method of making an electrotransport device
US6596712B2 (en) 1996-04-26 2003-07-22 Genaera Corporation Treatment of carcinomas using squalamine in combination with other anti-cancer agents or modalities
US6610841B1 (en) 1997-12-18 2003-08-26 Gilead Sciences, Inc. Nucleotide-based prodrugs
WO2004067546A1 (de) * 2003-01-28 2004-08-12 Helmut Kasch Tetraalkylammoniumsalze vom kohlensäureestertyp, verfahren zu ihrer herstellung und diese verbindungen enthaltende pharmazeutische zusammensetzungen
US6818787B2 (en) 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US6833140B2 (en) 2001-06-11 2004-12-21 Xenoport, Inc. Orally administered dosage forms of GABA analog prodrugs having reduced toxicity
US6933383B2 (en) 2000-04-12 2005-08-23 Genaera Corporation Regioselective and stereoselective oxidation of fused ring systems useful for the preparation of aminosterols
US6956060B2 (en) 1990-01-03 2005-10-18 Teva Pharmaceutical Industries, Ltd. Use of R-enantiomer of N-propargyl-1-aminoindan, salts, and compositions thereof
US7186855B2 (en) 2001-06-11 2007-03-06 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
EP0814789B2 (en) 1995-03-02 2008-01-09 R.P. Scherer Technologies, Inc. Pharmaceutical compositions comprising monoamine oxidase b inhibitors
WO2008013860A2 (en) * 2006-07-28 2008-01-31 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of alpha-amino acids, methods of synthesis and use
JP2008530007A (ja) * 2005-02-04 2008-08-07 アメリカ合衆国 ナンドロロン17β−カーボネート
JP2010505936A (ja) * 2006-10-11 2010-02-25 テックフィールズ バイオケム カンパニー リミテッド 非常に高い皮膚浸透率を有するオキシカム及び関連化合物の正荷電水溶性プロドラッグ
JP2010516802A (ja) * 2007-01-31 2010-05-20 チョンシー ユー 皮膚浸透率の非常に高い1H−イミダゾ[4,5−c]キノリン−4−アミン及び関連化合物の正に荷電した水溶性プロドラッグ
JP2010518071A (ja) * 2007-02-13 2010-05-27 カウンシル オブ サイエンティフィック アンド インダストリアル リサーチ 抗癌剤として有用な新規のカチオン性17α−置換−エストラジオール誘導体
JP2011503188A (ja) * 2007-11-14 2011-01-27 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアThe Regents of The University of California ステロール修飾両親媒性脂質
US8048917B2 (en) 2005-04-06 2011-11-01 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US8071737B2 (en) 1995-05-04 2011-12-06 Glead Sciences, Inc. Nucleic acid ligand complexes
US8431576B2 (en) 2009-06-25 2013-04-30 Alkermes Pharma Ireland Limited Heterocyclic compounds for the treatment of neurological and psychological disorders
US8592427B2 (en) 2010-06-24 2013-11-26 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
EP2670763A1 (en) * 2011-02-02 2013-12-11 Suzhou Neupharma Co., Ltd Certain chemical entities, compositions, and methods
US8686009B2 (en) 2009-06-25 2014-04-01 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds
JP2014514300A (ja) * 2011-04-08 2014-06-19 スファエラ ファーマ ピーティーイー リミテッド 置換メチルホルミル試薬並びに化合物の物理化学的性質及び/又は薬物動態学的性質を改質するためのそれらの使用方法
US8795725B2 (en) 2004-11-04 2014-08-05 Xenoport, Inc. GABA analog prodrug sustained release oral dosage forms
WO2014181085A1 (en) 2013-05-09 2014-11-13 Kenneth Dawson Bagshawe Tumour therapy
US8969337B2 (en) 2011-12-15 2015-03-03 Alkermes Pharma Ireland Limited Prodrugs of secondary amine compounds
US8993550B2 (en) 2010-01-15 2015-03-31 Suzhou Neupharma Co., Ltd. Certain chemical entities, compositions, and methods
US9018197B2 (en) 2010-08-28 2015-04-28 Suzhou Neupharma Co. Ltd. Tetradecahydro-1H-cyclopenta[a]phenanthrene compounds, compositions, and related methods of use
US9034867B2 (en) 2011-03-18 2015-05-19 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising sorbitan esters
US9193685B2 (en) 2012-09-19 2015-11-24 Alkermes Pharma Ireland Limited Pharmaceutical compositions having improved storage stability
US9340570B2 (en) 2012-04-29 2016-05-17 Neupharma, Inc. Certain chemical entities, compositions, and methods
US9371284B2 (en) 2007-06-04 2016-06-21 Techfields Pharma Co., Ltd. Pro-drugs of NSAIAS with very high skin and membranes penetration rates and their new medicinal uses
US9452131B2 (en) 2014-03-20 2016-09-27 Alkermes Pharma Ireland Limited Aripiprazole formulations having increased injection speeds
CN104151452B (zh) * 2014-07-16 2017-02-01 西北大学 聚n‑(2‑羟丙基)甲基丙烯酰胺‑氯尼达明大分子前药及其制备方法
US9872846B2 (en) 2006-07-09 2018-01-23 Techfields Pharma Co., Ltd. High penetration compositions and uses thereof
US9993556B2 (en) 2012-03-19 2018-06-12 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising fatty glycerol esters
US9999670B2 (en) 2012-03-19 2018-06-19 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising benzyl alcohol
US10004807B2 (en) 2012-03-19 2018-06-26 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising fatty acid esters

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4963367A (en) * 1984-04-27 1990-10-16 Medaphore, Inc. Drug delivery compositions and methods
US5085749A (en) * 1989-03-14 1992-02-04 Massachusetts Institute Of Technology Dynamically controlled membrane

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3023206A1 (de) * 1979-11-02 1982-01-14 Efeka Friedrich & Kaufmann Gmb Indometacin-ester, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
US4386026A (en) * 1981-04-20 1983-05-31 Merck & Co., Inc. Cell-specific glycopeptide ligands
US4866040A (en) * 1986-01-06 1989-09-12 Alfred Stracher Aminocarnitine directed pharmaceutical agents
US5042975A (en) * 1986-07-25 1991-08-27 Rutgers, The State University Of New Jersey Iontotherapeutic device and process and iontotherapeutic unit dose
EP0289262A3 (en) * 1987-04-27 1989-05-31 Syntex Pharmaceuticals International Limited Omega-quaternary ammonium alkyl esters and thioesters of acidic nonsteroidal antiinflammatory drugs
JPH06501448A (it) * 1989-12-26 1994-02-17

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4963367A (en) * 1984-04-27 1990-10-16 Medaphore, Inc. Drug delivery compositions and methods
US5085749A (en) * 1989-03-14 1992-02-04 Massachusetts Institute Of Technology Dynamically controlled membrane

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
See also references of EP0647133A4 *
Textbook of Biochemistry (WEST) 1966, 4th edition, see pages 169, 170. *

Cited By (103)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6956060B2 (en) 1990-01-03 2005-10-18 Teva Pharmaceutical Industries, Ltd. Use of R-enantiomer of N-propargyl-1-aminoindan, salts, and compositions thereof
US5721226A (en) * 1993-03-10 1998-02-24 Magainin Pharmaceuticals Inc. Method for inhibiting angiogenesis using squalamine and squalamine steroid derivatives
US5733899A (en) * 1993-03-10 1998-03-31 Magainin Pharmaceuticals Inc. Method for treating infection using steroid based pharmaceutical compositions
EP0678297A1 (en) * 1994-02-25 1995-10-25 Bristol-Myers Squibb Company Iontophoretic transdermal delivery of deoxyspergualin compounds
EP0773719A1 (en) * 1994-07-29 1997-05-21 Emory University Compositions for targeting materials to cells containing androgen receptors
US6468981B1 (en) 1994-07-29 2002-10-22 Emory University Compositions and methods for targeting pharmaceutically active materials to cells containing androgen receptors
EP0773719A4 (en) * 1994-07-29 1998-09-02 Univ Emory Compositions for targeting materials to cells containing androgen receptors
US5856535A (en) * 1994-08-18 1999-01-05 Magainin Pharmaceuticals, Inc. Aminosterol ester compounds
US6114388A (en) * 1994-11-18 2000-09-05 Geffard; Michel Monofunctional and/or polyfunctional polylysine conjuages
WO1996015810A1 (fr) * 1994-11-18 1996-05-30 Michel Geffard Conjugues monofonctionnels et/ou polyfonctionnels de la polylysine
FR2727117A1 (fr) * 1994-11-18 1996-05-24 Geffard Michel Utilisation de conjugues de la polylysine pour la preparation de medicaments utiles dans le traitement des maladies neurodegeneratives et des affections degeneratives a caractere autoimmun
EP0814789B2 (en) 1995-03-02 2008-01-09 R.P. Scherer Technologies, Inc. Pharmaceutical compositions comprising monoamine oxidase b inhibitors
US8071737B2 (en) 1995-05-04 2011-12-06 Glead Sciences, Inc. Nucleic acid ligand complexes
GB2317179B (en) * 1995-06-06 1999-07-28 Alza Corp Modification of polypeptide drugs to increase electrotransport flux
BE1009704A3 (fr) * 1995-06-06 1997-07-01 Alza Corp Modification de medicaments a base de polypeptide pour augmenter un flux d'electrotransport.
GB2316083A (en) * 1995-06-06 1998-02-18 Alza Corp A method for increasing the electrotransport flux of polypeptides
NL1003283C2 (nl) * 1995-06-06 1997-05-02 Alza Corp Modificatie van een polypeptide voor het vergroten van de elektro- transport-flux en toepassing daarvan als geneesmiddel.
GB2317179A (en) * 1995-06-06 1998-03-18 Alza Corp Modification of polypeptide drugs to increase electrotransport flux
NL1003284C2 (nl) * 1995-06-06 1997-03-20 Alza Corp Werkwijze voor het vergroten van de elektrotransport-flux van polypeptiden.
US5747453A (en) * 1995-06-06 1998-05-05 Alza Corporation Method for increasing the electrotransport flux of polypeptides
US7324846B2 (en) 1995-06-06 2008-01-29 Alza Corp. Method of enchancing electrontransport polypeptide flux by amino acid substitution with histidine
WO1996039422A3 (en) * 1995-06-06 1997-03-06 Alza Corp Modification of polypeptide drugs to increase electrotransport flux
WO1996039423A3 (en) * 1995-06-06 1997-01-30 Alza Corp A method for increasing the electrotransport flux of polypeptides
FR2735133A1 (fr) * 1995-06-06 1996-12-13 Alza Corp Procede de preparation d'un analogue de polypeptide a electro-transportabilite amelioree a travers la peau et son utilisation
FR2735132A1 (fr) * 1995-06-06 1996-12-13 Alza Corp Medicament polypeptidique modifie, composition et dispositif d'administration par electrotransport le contenant
US6313092B1 (en) 1995-06-06 2001-11-06 Alza Corporation Method for increasing the electrotransport flux of polypeptides
WO1996039423A2 (en) * 1995-06-06 1996-12-12 Alza Corporation A method for increasing the electrotransport flux of polypeptides
WO1996039422A2 (en) * 1995-06-06 1996-12-12 Alza Corporation Modification of polypeptide drugs to increase electrotransport flux
GB2316083B (en) * 1995-06-06 2000-01-19 Alza Corp A method for increasing the electrotransport flux of polypeptides
BE1009752A5 (fr) * 1995-06-06 1997-07-01 Alza Corp Procede pour augmenter le flux d'electrotransport de polypeptides.
US5840936A (en) * 1995-06-07 1998-11-24 Magainin Pharmaceuticals Inc. Aminosterol compounds useful as inhibitors of the sodium/proton exchanger (NHE)
US5994336A (en) * 1995-06-07 1999-11-30 Magainin Pharmaceuticals Inc. Method of inhibiting proliferation of cells by administering an aminosterol compound
US5874597A (en) * 1995-06-07 1999-02-23 Magainin Pharmaceuticals, Inc. Certain aminosterol compounds and pharmaceutical compositions including these compounds
US5847172A (en) * 1995-06-07 1998-12-08 Magainin Pharmaceuticals Inc. Certain aminosterol compounds and pharmaceutical compositions including these compounds
US6143738A (en) * 1995-06-07 2000-11-07 Magainin Pharmaceuticals, Inc. Therapeutic uses for an aminosterol compound
US5795885A (en) * 1995-06-07 1998-08-18 Magainin Pharmaceuticals Inc. Method of inhibiting profileration of cells by administering an aminosterol compound
US5792635A (en) * 1995-06-07 1998-08-11 Magainin Pharmaceuticals, Inc. Method of inhibiting the sodium/proton exchanger NHE3 and method of inhibiting growth by administering squalamine
US5840740A (en) * 1995-06-07 1998-11-24 Magainin Pharmaceuticals Inc. Aminosterol compounds and a method of treating infection using the aminosterol compounds
US5763430A (en) * 1995-06-07 1998-06-09 Magainin Pharmaceuticals Inc. Method of treating a viral infection by administering a steroid compound
EP0796841A1 (en) * 1996-03-20 1997-09-24 Sigma-Tau Industrie Farmaceutiche Riunite S.p.A. Bis alkanoyl esters of carnitine having bactericidal, fungicidal and antiprotozoal activity
US6147060A (en) * 1996-04-26 2000-11-14 Magainin Pharmaceuticals Treatment of carcinomas using squalamine in combination with other anti-cancer agents
US6596712B2 (en) 1996-04-26 2003-07-22 Genaera Corporation Treatment of carcinomas using squalamine in combination with other anti-cancer agents or modalities
US6333189B1 (en) 1996-06-06 2001-12-25 Alza Corporation Method of making an electrotransport device
US6262283B1 (en) 1996-12-06 2001-07-17 Magainin Pharmaceuticals Inc. Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin D analogs, and other compounds
US6610866B2 (en) 1996-12-06 2003-08-26 Magainin Pharmaceuticals, Inc. Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin D analogs, and other compounds
US6610841B1 (en) 1997-12-18 2003-08-26 Gilead Sciences, Inc. Nucleotide-based prodrugs
EP1484313A1 (en) * 1998-05-15 2004-12-08 Sigma-Tau Industrie Farmaceutiche Riunite S.p.A. Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase
USRE40861E1 (en) 1998-05-15 2009-07-21 Sigma-Tau Industrie Farmaceutiche Reunite S.p.A. Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase
WO1999059957A1 (en) * 1998-05-15 1999-11-25 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase
USRE41226E1 (en) 1998-05-15 2010-04-13 Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. Compounds having reversible inhibiting activity of carnitine palmitoyl-transferase
US6933383B2 (en) 2000-04-12 2005-08-23 Genaera Corporation Regioselective and stereoselective oxidation of fused ring systems useful for the preparation of aminosterols
US7728157B2 (en) 2000-04-12 2010-06-01 Ohr Pharmaceutical Inc. Regioselective and stereoselective oxidation of fused ring systems useful for the preparation of aminosterols
US7186855B2 (en) 2001-06-11 2007-03-06 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US9238616B2 (en) 2001-06-11 2016-01-19 Xenoport, Inc. Prodrugs of gaba analogs, compositions and uses thereof
US7790708B2 (en) 2001-06-11 2010-09-07 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US8168623B2 (en) 2001-06-11 2012-05-01 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US6972341B2 (en) 2001-06-11 2005-12-06 Xeno Port, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US6833140B2 (en) 2001-06-11 2004-12-21 Xenoport, Inc. Orally administered dosage forms of GABA analog prodrugs having reduced toxicity
US6818787B2 (en) 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
WO2004067546A1 (de) * 2003-01-28 2004-08-12 Helmut Kasch Tetraalkylammoniumsalze vom kohlensäureestertyp, verfahren zu ihrer herstellung und diese verbindungen enthaltende pharmazeutische zusammensetzungen
US8906412B2 (en) 2004-11-04 2014-12-09 Xenoport, Inc. GABA analog prodrug sustained release oral dosage forms
US8795725B2 (en) 2004-11-04 2014-08-05 Xenoport, Inc. GABA analog prodrug sustained release oral dosage forms
JP2008530007A (ja) * 2005-02-04 2008-08-07 アメリカ合衆国 ナンドロロン17β−カーボネート
US8048917B2 (en) 2005-04-06 2011-11-01 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US9872846B2 (en) 2006-07-09 2018-01-23 Techfields Pharma Co., Ltd. High penetration compositions and uses thereof
US7799829B2 (en) 2006-07-28 2010-09-21 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use
US7531572B2 (en) 2006-07-28 2009-05-12 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of α-amino acids, methods of synthesis and use
WO2008013860A2 (en) * 2006-07-28 2008-01-31 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of alpha-amino acids, methods of synthesis and use
WO2008013860A3 (en) * 2006-07-28 2008-03-13 Xuedong Dai Acyloxyalkyl carbamate prodrugs of alpha-amino acids, methods of synthesis and use
JP2010505936A (ja) * 2006-10-11 2010-02-25 テックフィールズ バイオケム カンパニー リミテッド 非常に高い皮膚浸透率を有するオキシカム及び関連化合物の正荷電水溶性プロドラッグ
JP2010516802A (ja) * 2007-01-31 2010-05-20 チョンシー ユー 皮膚浸透率の非常に高い1H−イミダゾ[4,5−c]キノリン−4−アミン及び関連化合物の正に荷電した水溶性プロドラッグ
US8349866B2 (en) 2007-01-31 2013-01-08 Chongxi Yu High penetration prodrug compositions of 1H-imidazo[4,5-C]quinolin-4-amines and 1H-imidazo[4,5-C]quinolin-4-amine-related compounds
US9567329B2 (en) 2007-01-31 2017-02-14 Techfields Pharma Co., Ltd. High penetration prodrug compositions of 1H-imidazo[4,5-c]quinolin-4-amines and 1H-imidazo[4,5-c]quinolin-4-amine-related compounds and uses thereof
JP2010518071A (ja) * 2007-02-13 2010-05-27 カウンシル オブ サイエンティフィック アンド インダストリアル リサーチ 抗癌剤として有用な新規のカチオン性17α−置換−エストラジオール誘導体
US9371284B2 (en) 2007-06-04 2016-06-21 Techfields Pharma Co., Ltd. Pro-drugs of NSAIAS with very high skin and membranes penetration rates and their new medicinal uses
JP2011503188A (ja) * 2007-11-14 2011-01-27 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアThe Regents of The University of California ステロール修飾両親媒性脂質
US8686009B2 (en) 2009-06-25 2014-04-01 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds
US8431576B2 (en) 2009-06-25 2013-04-30 Alkermes Pharma Ireland Limited Heterocyclic compounds for the treatment of neurological and psychological disorders
US10023537B2 (en) 2009-06-25 2018-07-17 Alkermes Pharma Ireland Limited Heterocyclic compounds for the treatment of neurological and psychological disorders
US9814735B2 (en) 2010-01-15 2017-11-14 Suzhou Neupharma Co., Ltd Certain chemical entities, compositions, and methods
US8993550B2 (en) 2010-01-15 2015-03-31 Suzhou Neupharma Co., Ltd. Certain chemical entities, compositions, and methods
US9399659B2 (en) 2010-01-15 2016-07-26 Suzhou Neupharma Co., Ltd Certain chemical entities, compositions, and methods
US8592427B2 (en) 2010-06-24 2013-11-26 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
US9018197B2 (en) 2010-08-28 2015-04-28 Suzhou Neupharma Co. Ltd. Tetradecahydro-1H-cyclopenta[a]phenanthrene compounds, compositions, and related methods of use
EP2670763A1 (en) * 2011-02-02 2013-12-11 Suzhou Neupharma Co., Ltd Certain chemical entities, compositions, and methods
US9493503B2 (en) 2011-02-02 2016-11-15 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2670763A4 (en) * 2011-02-02 2014-11-12 Suzhou Neupharma Co Ltd Certain chemical entities, compositions, and methods
US9351976B2 (en) 2011-03-18 2016-05-31 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising sorbitan esters
US9034867B2 (en) 2011-03-18 2015-05-19 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising sorbitan esters
JP2014514300A (ja) * 2011-04-08 2014-06-19 スファエラ ファーマ ピーティーイー リミテッド 置換メチルホルミル試薬並びに化合物の物理化学的性質及び/又は薬物動態学的性質を改質するためのそれらの使用方法
US8969337B2 (en) 2011-12-15 2015-03-03 Alkermes Pharma Ireland Limited Prodrugs of secondary amine compounds
US10004807B2 (en) 2012-03-19 2018-06-26 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising fatty acid esters
US9999670B2 (en) 2012-03-19 2018-06-19 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising benzyl alcohol
US9993556B2 (en) 2012-03-19 2018-06-12 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising fatty glycerol esters
US9340570B2 (en) 2012-04-29 2016-05-17 Neupharma, Inc. Certain chemical entities, compositions, and methods
US9676813B2 (en) 2012-04-29 2017-06-13 Neupharma, Inc. Certain steroids and methods for using the same in the treatment of cancer
US10065986B2 (en) 2012-04-29 2018-09-04 Neupharma, Inc. Certain chemical entities, compositions, and methods
US9861699B2 (en) 2012-09-19 2018-01-09 Alkermes Pharma Ireland Limited Pharmaceutical compositions having improved storage stability
US9193685B2 (en) 2012-09-19 2015-11-24 Alkermes Pharma Ireland Limited Pharmaceutical compositions having improved storage stability
WO2014181085A1 (en) 2013-05-09 2014-11-13 Kenneth Dawson Bagshawe Tumour therapy
US9526726B2 (en) 2014-03-20 2016-12-27 Alkermes Pharma Ireland Limited Aripiprazole formulations having increased injection speeds
US9452131B2 (en) 2014-03-20 2016-09-27 Alkermes Pharma Ireland Limited Aripiprazole formulations having increased injection speeds
CN104151452B (zh) * 2014-07-16 2017-02-01 西北大学 聚n‑(2‑羟丙基)甲基丙烯酰胺‑氯尼达明大分子前药及其制备方法

Also Published As

Publication number Publication date Type
EP0647133A4 (en) 1997-10-29 application
EP0647133A1 (en) 1995-04-12 application

Similar Documents

Publication Publication Date Title
US5258499A (en) Liposome targeting using receptor specific ligands
US6815542B2 (en) Nucleoside compounds and uses thereof
US6071890A (en) Organ-specific targeting of cationic amphiphile/DNA complexes for gene therapy
US5840710A (en) Cationic amphiphiles containing ester or ether-linked lipophilic groups for intracellular delivery of therapeutic molecules
Kalia et al. Iontophoretic drug delivery
US6379698B1 (en) Fusogenic lipids and vesicles
US5814603A (en) Compounds with PTH activity
US5948925A (en) Cationic amphiphiles containing linkers derived from neutral or positively charged amino acids
US7109165B2 (en) Conjugates and compositions for cellular delivery
US5811406A (en) Dry powder formulations of polynucleotide complexes
US5767099A (en) Cationic amphiphiles containing amino acid or dervatized amino acid groups for intracellular delivery of therapeutic molecules
US6011020A (en) Nucleic acid ligand complexes
US4310505A (en) Lipid vesicles bearing carbohydrate surfaces as lymphatic directed vehicles for therapeutic and diagnostic substances
Naik et al. Transdermal drug delivery: overcoming the skin’s barrier function
US5851536A (en) Therapeutic delivery using compounds self-assembled into high axial ratio microstructures
US20030119724A1 (en) Ligands to enhance cellular uptake of biomolecules
US20030130186A1 (en) Conjugates and compositions for cellular delivery
US6395713B1 (en) Compositions for the delivery of negatively charged molecules
US20050234232A1 (en) Novel compositions for the delivery of negatively charged molecules
US6670341B1 (en) Compositions and methods for double-targeting virus infections and targeting cancer cells
US5977084A (en) Self-assembling polynucleotide delivery method
US6733777B2 (en) Cationic reagents of transfection
US20050181037A1 (en) Cardiolipin compositions their methods of preparation and use
US6165458A (en) Composition and method for dermal and transdermal administration of a cytokine
US6610841B1 (en) Nucleotide-based prodrugs

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AT AU BB BG BR CA CH CZ DE DK ES FI GB HU JP KP KR LK LU MG MN MW NL NO NZ PL PT RO RU SD SE SK UA 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 IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWE Wipo information: entry into national phase

Ref document number: 1993915319

Country of ref document: EP

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWP Wipo information: published in national office

Ref document number: 1993915319

Country of ref document: EP

NENP Non-entry into the national phase in:

Ref country code: CA

WWW Wipo information: withdrawn in national office

Ref document number: 1993915319

Country of ref document: EP