CA2354142A1 - Reversible aqueous ph sensitive lipidizing reagents, compositions and methods of use - Google Patents

Reversible aqueous ph sensitive lipidizing reagents, compositions and methods of use Download PDF

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Publication number
CA2354142A1
CA2354142A1 CA002354142A CA2354142A CA2354142A1 CA 2354142 A1 CA2354142 A1 CA 2354142A1 CA 002354142 A CA002354142 A CA 002354142A CA 2354142 A CA2354142 A CA 2354142A CA 2354142 A1 CA2354142 A1 CA 2354142A1
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CA
Canada
Prior art keywords
group
compound
compound according
amino acid
branched
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Abandoned
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CA002354142A
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English (en)
French (fr)
Inventor
Wei-Chiang Shen
Hashem Heiati
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University of Southern California USC
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Publication of CA2354142A1 publication Critical patent/CA2354142A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/54Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and unsaturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/57Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C323/58Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton
    • C07C323/59Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton with acylated amino groups bound to the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/62Insulins
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/16Oxytocins; Vasopressins; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Furan Compounds (AREA)
CA002354142A 1998-12-10 1999-12-09 Reversible aqueous ph sensitive lipidizing reagents, compositions and methods of use Abandoned CA2354142A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11178498P 1998-12-10 1998-12-10
US60/111,784 1998-12-10
PCT/US1999/029119 WO2000034236A1 (en) 1998-12-10 1999-12-09 REVERSIBLE AQUEOUS pH SENSITIVE LIPIDIZING REAGENTS, COMPOSITIONS AND METHODS OF USE

Publications (1)

Publication Number Publication Date
CA2354142A1 true CA2354142A1 (en) 2000-06-15

Family

ID=22340445

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002354142A Abandoned CA2354142A1 (en) 1998-12-10 1999-12-09 Reversible aqueous ph sensitive lipidizing reagents, compositions and methods of use

Country Status (16)

Country Link
US (1) US6590071B1 (https=)
EP (1) EP1137631B1 (https=)
JP (1) JP4637362B2 (https=)
KR (1) KR100676419B1 (https=)
CN (1) CN1168711C (https=)
AR (1) AR021604A1 (https=)
AT (1) ATE265429T1 (https=)
AU (1) AU764035B2 (https=)
CA (1) CA2354142A1 (https=)
DE (1) DE69916885T2 (https=)
EA (1) EA200100652A1 (https=)
ES (1) ES2220141T3 (https=)
HK (1) HK1045681B (https=)
IL (2) IL143578A0 (https=)
TW (1) TWI242000B (https=)
WO (1) WO2000034236A1 (https=)

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* Cited by examiner, † Cited by third party
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US7048906B2 (en) 1995-05-17 2006-05-23 Cedars-Sinai Medical Center Methods of diagnosing and treating small intestinal bacterial overgrowth (SIBO) and SIBO-related conditions
US8541548B2 (en) * 1999-06-07 2013-09-24 Arrowhead Madison Inc. Compounds and methods for reversible modification of biologically active molecules
US7442764B2 (en) * 1999-06-07 2008-10-28 Mirns Bio Corporation Reversible modification of amine-containing compounds
US7019113B2 (en) * 1999-06-07 2006-03-28 Mirus Bio Corporation Reversible modification of membrane interaction
US20080281041A1 (en) 1999-06-07 2008-11-13 Rozema David B Reversibly Masked Polymers
US8137695B2 (en) * 2006-08-18 2012-03-20 Arrowhead Madison Inc. Polyconjugates for in vivo delivery of polynucleotides
KR100989647B1 (ko) 2001-09-24 2010-10-26 오레곤 헬스 앤드 사이언스 유니버시티 식습관의 변화
EP1474163A2 (en) 2002-01-10 2004-11-10 Imperial College Innovations Limited Modification of feeding behavior
US8008355B2 (en) * 2002-03-11 2011-08-30 Roche Madison Inc. Endosomolytic poly(vinyl ether) polymers
US8138383B2 (en) * 2002-03-11 2012-03-20 Arrowhead Madison Inc. Membrane active heteropolymers
WO2004048530A2 (en) * 2002-11-22 2004-06-10 Carnegie Mellon University Compositions and methods for the reversible capture of biomolecules
US20040151766A1 (en) * 2003-01-30 2004-08-05 Monahan Sean D. Protein and peptide delivery to mammalian cells in vitro
US20050054612A1 (en) * 2003-09-08 2005-03-10 Monahan Sean D. Delivery by labile hydrophobic modification of drugs
US20090074885A1 (en) * 2003-09-08 2009-03-19 Roche Madison Inc. Reversible Hydrophobic Modification of Drugs for Improved Delivery to Cells
FR2880627B1 (fr) * 2005-01-07 2007-05-18 Silab Sa Procede d'obtention d'un principe actif pour l'eclat du teint, principe actif obtenu et compositions associees
KR100726281B1 (ko) * 2006-07-31 2007-06-11 (주)아모레퍼시픽 신규 지방산 에스테르 화합물 및 이를 유효성분으로함유하는 당뇨 및 비만치료용 조성물
KR20090091145A (ko) * 2006-10-27 2009-08-26 웨이-치앙 션 지질화된 인터페론 및 이의 용도
TWI428346B (zh) 2006-12-13 2014-03-01 Imp Innovations Ltd 新穎化合物及其等對進食行為影響
WO2009059984A2 (en) * 2007-11-06 2009-05-14 F. Hoffmann-La Roche Ag Reversible hydrophobization of antitumor drugs for enhanced first-pass drug uptake

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US2962504A (en) * 1960-11-29 Production of maleic anhydride
US5144011A (en) * 1981-06-26 1992-09-01 Boston University Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers
US4631190A (en) 1981-06-26 1986-12-23 Shen Wei C Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers
US4480106A (en) * 1981-10-28 1984-10-30 Ciba-Geigy Corporation Process for the preparation of asymmetrically substituted maleic anhydrides, and asymmetrically substituted maleic anhydrides
US4542225A (en) * 1984-08-29 1985-09-17 Dana-Farber Cancer Institute, Inc. Acid-cleavable compound
US4764368A (en) 1984-08-29 1988-08-16 Dana-Farber Cancer Institute, Inc. Acid-cleavable compound
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US4889916A (en) 1985-11-19 1989-12-26 The Johns Hopkins University Protein label and drug delivery system
US4751286A (en) 1985-11-19 1988-06-14 The Johns Hopkins University Protein label and drug delivery system
GB2189698A (en) 1986-04-30 1987-11-04 Haessle Ab Coated omeprazole tablets
GB2189699A (en) 1986-04-30 1987-11-04 Haessle Ab Coated acid-labile medicaments
US4997913A (en) 1986-06-30 1991-03-05 Oncogen pH-sensitive immunoconjugates and methods for their use in tumor therapy
US5017693A (en) 1987-12-02 1991-05-21 Neorx Corporation Methods for introducing a sulfhydryl amino or hydroxyl groups to a compound
US5563250A (en) 1987-12-02 1996-10-08 Neorx Corporation Cleavable conjugates for the delivery and release of agents in native form
US5066490A (en) 1988-06-01 1991-11-19 The United States Of America As Represented By The Secretary Of The Department Of Health & Human Services Protein crosslinking reagents cleavable within acidified intracellular vesicles
US5140013A (en) * 1989-11-28 1992-08-18 Universite Laval Maleic anhydride derivatives used as conjugation agents of anti-tumor agents on desired carriers
FI101678B1 (fi) * 1990-12-31 1998-08-14 Akzo Nv Happolabiileja kytkentämolekyylejä
US5505931A (en) 1993-03-04 1996-04-09 The Dow Chemical Company Acid cleavable compounds, their preparation and use as bifunctional acid-labile crosslinking agents
US5907030A (en) * 1995-01-25 1999-05-25 University Of Southern California Method and compositions for lipidization of hydrophilic molecules
PL183698B1 (pl) * 1995-03-17 2002-06-28 Novo Nordisk As Pochodna insuliny, kompozycja farmaceutyczna i zastosowanie pochodnej insuliny
US5869602A (en) * 1995-03-17 1999-02-09 Novo Nordisk A/S Peptide derivatives
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Also Published As

Publication number Publication date
CN1350519A (zh) 2002-05-22
CN1168711C (zh) 2004-09-29
DE69916885D1 (de) 2004-06-03
WO2000034236A1 (en) 2000-06-15
JP2002531543A (ja) 2002-09-24
AR021604A1 (es) 2002-07-31
HK1045681A1 (en) 2002-12-06
EA200100652A1 (ru) 2001-12-24
HK1045681B (zh) 2005-05-20
EP1137631A1 (en) 2001-10-04
ES2220141T3 (es) 2004-12-01
DE69916885T2 (de) 2005-04-07
JP4637362B2 (ja) 2011-02-23
AU764035B2 (en) 2003-08-07
TWI242000B (en) 2005-10-21
US6590071B1 (en) 2003-07-08
KR20010080749A (ko) 2001-08-22
AU2355600A (en) 2000-06-26
KR100676419B1 (ko) 2007-02-05
ATE265429T1 (de) 2004-05-15
EP1137631B1 (en) 2004-04-28
IL143578A0 (en) 2002-04-21
IL143578A (en) 2006-07-05

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued