US20030229010A1 - Oral insulin-oligomer conjugates - Google Patents

Oral insulin-oligomer conjugates Download PDF

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Publication number
US20030229010A1
US20030229010A1 US10/448,535 US44853503A US2003229010A1 US 20030229010 A1 US20030229010 A1 US 20030229010A1 US 44853503 A US44853503 A US 44853503A US 2003229010 A1 US2003229010 A1 US 2003229010A1
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United States
Prior art keywords
insulin
polymer
conjugate
microemulsion
therapeutic agent
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.)
Abandoned
Application number
US10/448,535
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English (en)
Inventor
Nnochiri Ekwuribe
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.)
Biocon Ltd
Original Assignee
Ekwuribe Nnochiri Nkem
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
Priority claimed from US08/059,701 external-priority patent/US5359030A/en
Priority claimed from US08/509,422 external-priority patent/US5681811A/en
Application filed by Ekwuribe Nnochiri Nkem filed Critical Ekwuribe Nnochiri Nkem
Priority to US10/448,535 priority Critical patent/US20030229010A1/en
Publication of US20030229010A1 publication Critical patent/US20030229010A1/en
Assigned to BIOCON LIMITED reassignment BIOCON LIMITED SECURITY AGREEMENT Assignors: NOBEX CORPORATION
Assigned to BIOCON LIMITED reassignment BIOCON LIMITED ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: NOBEX CORPORATION
Abandoned legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/96—Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates
    • 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1077—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/62—Insulins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Zoology (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Wood Science & Technology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dispersion Chemistry (AREA)
  • Endocrinology (AREA)
  • Biotechnology (AREA)
  • Toxicology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
US10/448,535 1993-05-10 2003-06-02 Oral insulin-oligomer conjugates Abandoned US20030229010A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US10/448,535 US20030229010A1 (en) 1993-05-10 2003-06-02 Oral insulin-oligomer conjugates

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US08/059,701 US5359030A (en) 1993-05-10 1993-05-10 Conjugation-stabilized polypeptide compositions, therapeutic delivery and diagnostic formulations comprising same, and method of making and using the same
US08/276,890 US5438040A (en) 1993-05-10 1994-07-19 Conjugation-stabilized polypeptide compositions, therapeutic delivery and diagnostic formulations comprising same, and method of making and using the same
US08/509,422 US5681811A (en) 1993-05-10 1995-07-31 Conjugation-stabilized therapeutic agent compositions, delivery and diagnostic formulations comprising same, and method of making and using the same
US08/958,383 US6191105B1 (en) 1993-05-10 1997-10-27 Hydrophilic and lipophilic balanced microemulsion formulations of free-form and/or conjugation-stabilized therapeutic agents such as insulin
US61420300A 2000-07-12 2000-07-12
US10/448,535 US20030229010A1 (en) 1993-05-10 2003-06-02 Oral insulin-oligomer conjugates

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
US61420300A Continuation 1993-05-10 2000-07-12

Publications (1)

Publication Number Publication Date
US20030229010A1 true US20030229010A1 (en) 2003-12-11

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ID=27369707

Family Applications (3)

Application Number Title Priority Date Filing Date
US08/958,383 Expired - Fee Related US6191105B1 (en) 1993-05-10 1997-10-27 Hydrophilic and lipophilic balanced microemulsion formulations of free-form and/or conjugation-stabilized therapeutic agents such as insulin
US10/448,524 Abandoned US20030229006A1 (en) 1993-05-10 2003-05-30 Amphiphilic oligomers
US10/448,535 Abandoned US20030229010A1 (en) 1993-05-10 2003-06-02 Oral insulin-oligomer conjugates

Family Applications Before (2)

Application Number Title Priority Date Filing Date
US08/958,383 Expired - Fee Related US6191105B1 (en) 1993-05-10 1997-10-27 Hydrophilic and lipophilic balanced microemulsion formulations of free-form and/or conjugation-stabilized therapeutic agents such as insulin
US10/448,524 Abandoned US20030229006A1 (en) 1993-05-10 2003-05-30 Amphiphilic oligomers

Country Status (1)

Country Link
US (3) US6191105B1 (US20030229010A1-20031211-C00007.png)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040203081A1 (en) * 2002-11-26 2004-10-14 James Kenneth D. Natriuretic compounds, conjugates, and uses thereof
US20080021005A1 (en) * 2004-04-01 2008-01-24 Cardiome Pharma Corp. Pegylated Ion Channel Modulating Compounds
US20080139392A1 (en) * 2006-12-12 2008-06-12 Edgar Joel Acosta-Zara Linker-Based Lecithin Microemulsion Delivery Vehicles
US20080207505A1 (en) * 2005-01-12 2008-08-28 James Kenneth D Bna Conjugates and Methods of Use
US20090036353A1 (en) * 2005-01-27 2009-02-05 Novo Nordisk A/S Insulin Derivatives Conjugated with Structurally Well Defined Branched Polymers
US20090176691A1 (en) * 2007-12-19 2009-07-09 Farid Bennis Pharmaceutical Compositions Containing at Least One Protein Active Ingredient Protected From Digestive Enzymes
US7651996B2 (en) 2003-12-08 2010-01-26 Cpex Pharmaceuticals, Inc. Pharmaceutical compositions and methods for insulin treatment
WO2010059204A1 (en) * 2008-11-18 2010-05-27 University Of Medicine And Dentistry Of New Jersey Methods and compositions for treating obesity and related disorders
US9260501B2 (en) 2006-10-27 2016-02-16 Novo Nordisk A/S Peptide extended insulins
US9682153B2 (en) 2008-09-19 2017-06-20 Nektar Therapeutics Polymer conjugates of therapeutic peptides

Families Citing this family (177)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7070799B1 (en) * 1998-02-10 2006-07-04 Generex Pharmaceuticals, Inc. Method for administering insulin to the buccal region
US6703381B1 (en) * 1998-08-14 2004-03-09 Nobex Corporation Methods for delivery therapeutic compounds across the blood-brain barrier
GB9819382D0 (en) * 1998-09-04 1998-10-28 Cerebrus Ltd Chemical compounds I
US7169889B1 (en) * 1999-06-19 2007-01-30 Biocon Limited Insulin prodrugs hydrolyzable in vivo to yield peglylated insulin
US6638906B1 (en) 1999-12-13 2003-10-28 Nobex Corporation Amphiphilic polymers and polypeptide conjugates comprising same
US7105154B2 (en) * 2000-07-19 2006-09-12 Pepgen Corporation Method of treatment using interferon-tau
US6867183B2 (en) * 2001-02-15 2005-03-15 Nobex Corporation Pharmaceutical compositions of insulin drug-oligomer conjugates and methods of treating diseases therewith
US7060675B2 (en) * 2001-02-15 2006-06-13 Nobex Corporation Methods of treating diabetes mellitus
US6835802B2 (en) 2001-06-04 2004-12-28 Nobex Corporation Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties
US7713932B2 (en) 2001-06-04 2010-05-11 Biocon Limited Calcitonin drug-oligomer conjugates, and uses thereof
US6828305B2 (en) * 2001-06-04 2004-12-07 Nobex Corporation Mixtures of growth hormone drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
US6713452B2 (en) 2001-06-04 2004-03-30 Nobex Corporation Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
US6828297B2 (en) * 2001-06-04 2004-12-07 Nobex Corporation Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
CN1335182A (zh) * 2001-08-08 2002-02-13 华中科技大学 胰岛素口腔喷剂及其制备工艺
US6913903B2 (en) * 2001-09-07 2005-07-05 Nobex Corporation Methods of synthesizing insulin polypeptide-oligomer conjugates, and proinsulin polypeptide-oligomer conjugates and methods of synthesizing same
US7030082B2 (en) * 2001-09-07 2006-04-18 Nobex Corporation Pharmaceutical compositions of drug-oligomer conjugates and methods of treating disease therewith
US7196059B2 (en) * 2001-09-07 2007-03-27 Biocon Limited Pharmaceutical compositions of insulin drug-oligomer conjugates and methods of treating diseases therewith
US7166571B2 (en) * 2001-09-07 2007-01-23 Biocon Limited Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same
US7312192B2 (en) * 2001-09-07 2007-12-25 Biocon Limited Insulin polypeptide-oligomer conjugates, proinsulin polypeptide-oligomer conjugates and methods of synthesizing same
US6770625B2 (en) 2001-09-07 2004-08-03 Nobex Corporation Pharmaceutical compositions of calcitonin drug-oligomer conjugates and methods of treating diseases therewith
US7026440B2 (en) 2001-11-07 2006-04-11 Nektar Therapeutics Al, Corporation Branched polymers and their conjugates
ATE424815T1 (de) * 2001-12-03 2009-03-15 Dor Biopharma Inc Stabilisierte umkehr-mizellen-zusammensetzungen und ihre verwendung
JP2006501137A (ja) * 2002-01-16 2006-01-12 ペプジェン コーポレイション インターフェロン−τの経口投与
US6899890B2 (en) * 2002-03-20 2005-05-31 Kv Pharmaceutical Company Bioadhesive drug delivery system
US20040121406A1 (en) * 2002-05-23 2004-06-24 Wilson Constance Neely Methods and formulations for increasing the affinity of a1 adenosine receptor ligands for the a1 adenosine receptor
DE10226990A1 (de) * 2002-06-18 2004-03-18 Sanguibiotech Ag Topisch applizierbare Mikro-Emulsionen mit binärer Phasen- und Wirkstoffdifferenzierbarkeit, deren Herstellung und deren Verwendung, insbesondere zur Versorgung der Haut mit bioverfügbarem Sauerstoff
US7648962B2 (en) * 2002-11-26 2010-01-19 Biocon Limited Natriuretic compounds, conjugates, and uses thereof
US7655618B2 (en) 2002-12-27 2010-02-02 Diobex, Inc. Compositions and methods for the prevention and control of insulin-induced hypoglycemia
KR20050086948A (ko) * 2002-12-27 2005-08-30 디오벡스, 인코포레이티드 인슐린으로 인한 저혈당증을 예방하고 조절하기 위한조성물 및 방법
US6900058B2 (en) * 2003-03-11 2005-05-31 Bionostics, Inc. Control solution for photometric analysis
US7749954B2 (en) 2003-07-23 2010-07-06 Novartis Ag Use of calcitonin in osteoarthritis
WO2005063156A1 (en) * 2003-12-22 2005-07-14 Shear/Kershman Laboratories, Inc. Oral peptide delivery system with improved bioavailability
KR100638041B1 (ko) 2003-12-24 2006-10-23 주식회사 삼양사 수용성 약물의 경구투여용 나노입자 조성물 및 그의제조방법
US8329958B2 (en) * 2004-07-02 2012-12-11 Biocon Limited Combinatorial synthesis of PEG oligomer libraries
CA2910494C (en) 2004-07-19 2018-10-23 Biocon Limited Insulin-oligomer conjugates, formulations and uses thereof
WO2006113505A2 (en) 2005-04-15 2006-10-26 Clarus Therapeutics, Inc. Pharmaceutical delivery systems for hydrophobic drugs and compositions comprising same
US8492369B2 (en) 2010-04-12 2013-07-23 Clarus Therapeutics Inc Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same
US20060257355A1 (en) * 2005-05-10 2006-11-16 Abiomed, Inc. Impregnated polymer compositions and devices using them
EP1931665A1 (en) 2005-09-20 2008-06-18 Schering Corporation 1-[[1-[(2-amin0-6-methyl-4-pyridinyl)methyl]-4-flu0r0-4-piperidinyl,]carbonyl]-4-[2-(2-pyridinyl)-3h-imidaz0[4, 5-b]pyridin-3-yl]piperidine useful as histamine h3 antagonist
CA2626933C (en) 2005-11-17 2015-12-29 Novartis Ag Pharmaceutical composition
EP2063708A2 (en) * 2006-09-08 2009-06-03 Merck & Co., Inc. Liquid pharmaceutical formulations for oral administration of a cgrp antagonist
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
CA2688161C (en) 2007-06-04 2020-10-20 Kunwar Shailubhai Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
WO2009017662A2 (en) * 2007-07-27 2009-02-05 Immuneregen Biosciences, Inc. Method of using substance p analogs for treatment amelioration of myelodysplastic syndrome
WO2009042064A2 (en) 2007-09-21 2009-04-02 Nektar Therapeutics Al, Corporation Oligomer-nucleoside phosphate conjugates
MX2010003979A (es) * 2007-10-16 2010-06-02 Biocon Ltd Composicion farmaceutica oralmente administrable y proceso para su preparacion.
AU2008317057B8 (en) 2007-10-22 2014-02-13 Merck Sharp & Dohme Corp. Bicyclic Heterocycle Derivatives and their use as modulators of the activity of GPR119
CA2724426A1 (en) 2008-05-19 2009-11-26 Schering Corporation Bicyclic heterocycle derivatives and use thereof as gpr119 modulators
ES2522968T3 (es) 2008-06-04 2014-11-19 Synergy Pharmaceuticals Inc. Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
AU2009270971A1 (en) 2008-07-16 2010-01-21 Schering Corporation Bicyclic Heterocycle Derivatives and use thereof as GPR119 modulators
ES2624828T3 (es) 2008-07-16 2017-07-17 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros
WO2010027567A2 (en) 2008-07-23 2010-03-11 Schering Corporation Tricyclic spirocycle derivatives and methods of use thereof
EP2350020B1 (en) 2008-10-03 2014-08-13 Merck Sharp & Dohme Corp. Spiro-imidazolone derivatives as glucagon receptor antagonists
WO2010045306A2 (en) 2008-10-16 2010-04-22 Schering Corporation Azine derivatives and methods of use thereof
US8603999B2 (en) 2008-12-05 2013-12-10 Commonwealth Scientific And Industrial Research Organisation Amphiphile prodrugs
WO2010075068A1 (en) 2008-12-16 2010-07-01 Schering Corporation Pyridopyrimidine derivatives and methods of use thereof
WO2010075069A1 (en) 2008-12-16 2010-07-01 Schering Corporation Bicyclic pyranone derivatives as nicotinic acid receptor agonists
EP2379564A1 (en) 2008-12-19 2011-10-26 Schering Corporation Bicyclic heterocyclic derivatives and methods of use thereof
WO2010071822A1 (en) 2008-12-19 2010-06-24 Schering Corporation Piperidine and piperazine derivatives and methods of use thereof
EP2382203B1 (en) 2008-12-23 2015-01-14 Merck Sharp & Dohme Corp. Bicyclic heterocycle derivatives and methods of use thereof
JP2012513469A (ja) 2008-12-23 2012-06-14 シェーリング コーポレイション ピリミジン誘導体及びその使用法
WO2010075273A1 (en) 2008-12-23 2010-07-01 Schering Corporation Bicyclic heterocycle derivatives and methods of use thereof
EP2397152B1 (en) 2009-02-12 2014-05-28 Proyecto de Biomedicina Cima, S.L. Use of cardiotrophin- 1 for the treatment of metabolic diseases
AR075858A1 (es) 2009-03-18 2011-05-04 Schering Corp Compuestos biciclicos como inhibidores de diacilglicerol aciltransferasa
AR076024A1 (es) 2009-04-03 2011-05-11 Schering Corp Derivados de heterociclos biciclicos puenteados y metodos de uso de los mismos
EP2414348B1 (en) 2009-04-03 2013-11-20 Merck Sharp & Dohme Corp. Bicyclic piperidine and piperazine derivatives as gpcr modulators for the treatment of obesity, diabetes and other metabolic disorders
EP2440553B1 (en) 2009-06-12 2017-08-23 Merck Sharp & Dohme Corp. Thiophenes as glucagon receptor antagonists, compositions, and methods for their use
US20120172369A1 (en) 2009-09-14 2012-07-05 Ting Pauline C Inhibitors of diacylglycerol acyltransferase
US8759357B2 (en) 2009-10-08 2014-06-24 Merck Sharp & Dohme Corp. Inhibitors of fatty acid binding protein (FABP)
AU2010313469A1 (en) 2009-10-29 2012-06-07 Merck Sharp & Dohme Corp. Bridged Bicyclic Piperidine Derivatives and methods of use thereof
WO2011062889A1 (en) 2009-11-23 2011-05-26 Schering Corporation Pyrimidine ether derivatives and methods of use thereof
US20120232073A1 (en) 2009-11-23 2012-09-13 Santhosh Francis Neelamkavil Fused bicyclic pyrimidine derivatives and methods of use thereof
EP2503887B1 (en) 2009-11-24 2016-01-06 Merck Sharp & Dohme Corp. Substituted biaryl derivatives and methods of use thereof
WO2011153323A2 (en) 2010-06-02 2011-12-08 Alnylam Pharmaceuticals, Inc. Compositions and methods directed to treating liver fibrosis
US20130156720A1 (en) 2010-08-27 2013-06-20 Ironwood Pharmaceuticals, Inc. Compositions and methods for treating or preventing metabolic syndrome and related diseases and disorders
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
EP2649182A4 (en) 2010-12-10 2015-05-06 Alnylam Pharmaceuticals Inc COMPOSITIONS AND METHOD FOR INCREASING AN ERYTHROPOIETIN (EPO) PREPARATION
WO2012079046A2 (en) 2010-12-10 2012-06-14 Alnylam Pharmaceuticals, Inc. Compositions and methods for inhibiting expression of klf-1 and bcl11a genes
KR102481317B1 (ko) 2011-03-29 2022-12-26 알닐람 파마슈티칼스 인코포레이티드 Tmprss6 유전자의 발현을 억제하기 위한 조성물 및 방법
EP2526971A1 (en) * 2011-05-25 2012-11-28 ArisGen SA Mucosal delivery of drugs
AU2012262139B2 (en) 2011-06-02 2017-02-23 Children's Medical Center Corporation Methods and uses for ex vivo tissue culture systems
CA2839896A1 (en) 2011-06-21 2012-12-27 Alnylam Pharmaceuticals, Inc. Assays and methods for determining activity of a therapeutic agent in a subject
MX345095B (es) 2011-06-21 2017-01-17 Alnylam Pharmaceuticals Inc Composiciones de arni similares a angiopoyetina 3 (angptl3) y metodos para su uso.
EP3597750B1 (en) 2011-06-23 2022-05-04 Alnylam Pharmaceuticals, Inc. Serpina1 sirnas: compositions of matter and methods of treatment
JP2014527036A (ja) 2011-06-27 2014-10-09 ザ ジャクソン ラボラトリー 癌および自己免疫疾患の処置のための方法および組成物
US20140328811A1 (en) 2011-08-01 2014-11-06 Alnylam Pharmaceuticals, Inc. Method for improving the success rate of hematopoietic stem cell transplants
US9133461B2 (en) 2012-04-10 2015-09-15 Alnylam Pharmaceuticals, Inc. Compositions and methods for inhibiting expression of the ALAS1 gene
US9127274B2 (en) 2012-04-26 2015-09-08 Alnylam Pharmaceuticals, Inc. Serpinc1 iRNA compositions and methods of use thereof
WO2014057522A1 (en) 2012-10-12 2014-04-17 Mochida Pharmaceutical Co., Ltd. Compositions and methods for treating non-alcoholic steatohepatitis
KR102096014B1 (ko) 2012-12-05 2020-04-03 알닐람 파마슈티칼스 인코포레이티드 PCSK9 iRNA 조성물 및 그 사용 방법
KR102342916B1 (ko) 2013-03-14 2021-12-24 알닐람 파마슈티칼스 인코포레이티드 보체 성분 Ｃ5 ｉＲＮＡ 조성물 및 그 이용 방법
EP2970384A1 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
US10441560B2 (en) 2013-03-15 2019-10-15 Mochida Pharmaceutical Co., Ltd. Compositions and methods for treating non-alcoholic steatohepatitis
US9486494B2 (en) 2013-03-15 2016-11-08 Synergy Pharmaceuticals, Inc. Compositions useful for the treatment of gastrointestinal disorders
EP2968245B1 (en) 2013-03-15 2021-05-05 Mochida Pharmaceutical Co., Ltd. Compositions and methods for treating non-alcoholic steatohepatitis
US9937231B2 (en) 2013-03-27 2018-04-10 The General Hospital Corporation Methods and agents for treating Alzheimer's disease
AR096203A1 (es) 2013-05-06 2015-12-16 Alnylam Pharmaceuticals Inc Dosificaciones y métodos para administrar moléculas de ácido nucleico formuladas en lípidos
EP3587578A1 (en) 2013-05-22 2020-01-01 Alnylam Pharmaceuticals, Inc. Tmprss6 irna compositions and methods of use thereof
PT2999785T (pt) 2013-05-22 2018-07-09 Alnylam Pharmaceuticals Inc Composições de irna de serpina1 e métodos de uso das mesmas
JP6606491B2 (ja) 2013-06-05 2019-11-13 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼｃの超高純度アゴニスト、その作成および使用方法
MX2015017123A (es) 2013-06-14 2016-08-03 Invictus Oncology Pvt Ltd Compuestos de platino a base de lipido y nanoparticulas.
WO2015050990A1 (en) 2013-10-02 2015-04-09 Alnylam Pharmaceuticals, Inc. Compositions and methods for inhibiting expression of the lect2 gene
US10119143B2 (en) 2013-10-04 2018-11-06 Alnylam Pharmaceuticals, Inc. Compositions and methods for inhibiting expression of the ALAS1 gene
CN105814205B (zh) 2013-12-12 2019-11-19 阿尔尼拉姆医药品有限公司 补体成分iRNA组合物及其使用方法
WO2015100406A1 (en) 2013-12-26 2015-07-02 Clarus Therapeutics, Inc. Use of oral pharmaceutical products combining testosterone esters with hypolipidemic agents
EA201691587A1 (ru) 2014-02-11 2017-01-30 Элнилэм Фармасьютикалз, Инк. КОМПОЗИЦИИ НА ОСНОВЕ iRNA ДЛЯ КЕТОГЕКСОКИНАЗЫ (KHK) И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
WO2015153730A2 (en) * 2014-04-02 2015-10-08 The Regents Of The University Of California Synthetic catalytic mimics of esterases, lipases or desaturases
TW201607559A (zh) 2014-05-12 2016-03-01 阿尼拉製藥公司 治療ｓｅｒｐｉｎｃ１相關疾患之方法和組成物
KR20220087576A (ko) 2014-05-22 2022-06-24 알닐람 파마슈티칼스 인코포레이티드 안지오텐시노겐 (ａｇｔ) ｉｒｎａ 조성물 및 이의 사용 방법
EP3191591A1 (en) 2014-09-12 2017-07-19 Alnylam Pharmaceuticals, Inc. Polynucleotide agents targeting complement component c5 and methods of use thereof
JOP20200115A1 (ar) 2014-10-10 2017-06-16 Alnylam Pharmaceuticals Inc تركيبات وطرق لتثبيط التعبير الجيني عن hao1 (حمض أوكسيداز هيدروكسيلي 1 (أوكسيداز جليكولات))
EP3207138B1 (en) 2014-10-17 2020-07-15 Alnylam Pharmaceuticals, Inc. Polynucleotide agents targeting aminolevulinic acid synthase-1 (alas1) and uses thereof
EP3212794B1 (en) 2014-10-30 2021-04-07 Genzyme Corporation Polynucleotide agents targeting serpinc1 (at3) and methods of use thereof
JOP20200092A1 (ar) 2014-11-10 2017-06-16 Alnylam Pharmaceuticals Inc تركيبات iRNA لفيروس الكبد B (HBV) وطرق لاستخدامها
EP3221451A1 (en) 2014-11-17 2017-09-27 Alnylam Pharmaceuticals, Inc. Apolipoprotein c3 (apoc3) irna compositions and methods of use thereof
US20160151511A1 (en) 2014-12-02 2016-06-02 Antriabio, Inc. Proteins and protein conjugates with increased hydrophobicity
TW201702218A (zh) 2014-12-12 2017-01-16 美國杰克森實驗室 關於治療癌症、自體免疫疾病及神經退化性疾病之組合物及方法
EP3247386A4 (en) 2015-01-20 2018-10-03 The Children's Medical Center Corporation Anti-net compounds for treating and preventing fibrosis and for facilitating wound healing
JP2018510621A (ja) 2015-02-13 2018-04-19 アルナイラム ファーマシューティカルズ， インコーポレイテッドＡｌｎｙｌａｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． パタチン様ホスホリパーゼドメイン含有３（ＰＮＰＬＡ３）ｉＲＮＡ組成物およびその使用方法
US10745702B2 (en) 2015-04-08 2020-08-18 Alnylam Pharmaceuticals, Inc. Compositions and methods for inhibiting expression of the LECT2 gene
CA2982450A1 (en) 2015-04-13 2016-10-20 Alnylam Pharmaceuticals, Inc. Angiopoietin-like 3 (angptl3) irna compositions and methods of use thereof
WO2016196017A1 (en) 2015-06-04 2016-12-08 Antriabio, Inc. Amine pegylation methods for the preparation of site-specific protein conjugates
WO2016201301A1 (en) 2015-06-12 2016-12-15 Alnylam Pharmaceuticals, Inc. Complement component c5 irna compositions and methods of use thereof
EP3310918B1 (en) 2015-06-18 2020-08-05 Alnylam Pharmaceuticals, Inc. Polynucleotide agents targeting hydroxyacid oxidase (glycolate oxidase, hao1) and methods of use thereof
WO2016209862A1 (en) 2015-06-23 2016-12-29 Alnylam Pharmaceuticals, Inc. Glucokinase (gck) irna compositions and methods of use thereof
US10494632B2 (en) 2015-07-10 2019-12-03 Alnylam Pharmaceuticals, Inc. Insulin-like growth factor binding protein, acid labile subunit (IGFALS) compositions and methods of use thereof
WO2017040078A1 (en) 2015-09-02 2017-03-09 Alnylam Pharmaceuticals, Inc. PROGRAMMED CELL DEATH 1 LIGAND 1 (PD-L1) iRNA COMPOSITIONS AND METHODS OF USE THEREOF
EP3350328A1 (en) 2015-09-14 2018-07-25 Alnylam Pharmaceuticals, Inc. Polynucleotide agents targeting patatin-like phospholipase domain containing 3 (pnpla3) and methods of use thereof
WO2017064657A1 (en) 2015-10-16 2017-04-20 Invictus Oncology Pvt. Ltd. Fluorescent anticancer platinum drugs
IL259795B2 (en) 2015-12-07 2024-04-01 Genzyme Corp Methods and preparations for the treatment of diseases related to SERPINC1
EP3387129A1 (en) 2015-12-10 2018-10-17 Alnylam Pharmaceuticals, Inc. STEROL REGULATORY ELEMENT BINDING PROTEIN (SREBP) CHAPERONE (SCAP) iRNA COMPOSITIONS AND METHODS OF USE THEREOF
MA45295A (fr) 2016-04-19 2019-02-27 Alnylam Pharmaceuticals Inc Composition d'arni de protéine de liaison de lipoprotéines haute densité (hdlbp/vigiline) et procédés pour les utiliser
EP3469083A1 (en) 2016-06-10 2019-04-17 Alnylam Pharmaceuticals, Inc. COMPLEMENT COMPONENT C5 iRNA COMPOSITIONS AND METHODS OF USE THEREOF FOR TREATING PAROXYSMAL NOCTURNAL HEMOGLOBINURIA (PNH)
TWI788312B (zh) 2016-11-23 2023-01-01 美商阿尼拉製藥公司 絲胺酸蛋白酶抑制因子Ａ１ ｉＲＮＡ組成物及其使用方法
SG10201913552UA (en) 2016-12-16 2020-03-30 Alnylam Pharmaceuticals Inc Methods for treating or preventing ttr-associated diseases using transthyretin (ttr) irna compositions
AU2018301477A1 (en) 2017-07-13 2020-02-27 Alnylam Pharmaceuticals Inc. Lactate dehydrogenase a (LDHA) iRNA compositions and methods of use thereof
WO2019089922A1 (en) 2017-11-01 2019-05-09 Alnylam Pharmaceuticals, Inc. Complement component c3 irna compositions and methods of use thereof
US20200385719A1 (en) 2017-11-16 2020-12-10 Alnylam Pharmaceuticals, Inc. Kisspeptin 1 (kiss1) irna compositions and methods of use thereof
WO2019100039A1 (en) 2017-11-20 2019-05-23 Alnylam Pharmaceuticals, Inc. Serum amyloid p component (apcs) irna compositions and methods of use thereof
US20200308588A1 (en) 2017-12-18 2020-10-01 Alnylam Pharmaceuticals, Inc. High mobility group box-1 (hmgb1) irna compositions and methods of use thereof
US20210348162A1 (en) 2018-08-16 2021-11-11 Alnylam Pharmaceuticals, Inc. Compositions and methods for inhibiting expression of the lect2 gene
CN112424355A (zh) 2018-09-18 2021-02-26 阿尔尼拉姆医药品有限公司 己酮糖激酶(KHK)iRNA组合物及其使用方法
US10913951B2 (en) 2018-10-31 2021-02-09 University of Pittsburgh—of the Commonwealth System of Higher Education Silencing of HNF4A-P2 isoforms with siRNA to improve hepatocyte function in liver failure
WO2021030522A1 (en) 2019-08-13 2021-02-18 Alnylam Pharmaceuticals, Inc. SMALL RIBOSOMAL PROTEIN SUBUNIT 25 (RPS25) iRNA AGENT COMPOSITIONS AND METHODS OF USE THEREOF
CN114616331A (zh) 2019-09-03 2022-06-10 阿尔尼拉姆医药品有限公司 抑制lect2基因表达的组合物和方法
WO2021067747A1 (en) 2019-10-04 2021-04-08 Alnylam Pharmaceuticals, Inc. Compositions and methods for silencing ugt1a1 gene expression
US20230040920A1 (en) 2019-11-01 2023-02-09 Alnylam Pharmaceuticals, Inc. Compositions and methods for silencing dnajb1-prkaca fusion gene expression
AR120341A1 (es) 2019-11-01 2022-02-09 Alnylam Pharmaceuticals Inc COMPOSICIONES DE AGENTES DE ARNi CONTRA LA HUNTINGTINA (HTT) Y SUS MÉTODOS DE USO
BR112022011417A2 (pt) 2019-12-13 2022-08-30 Alnylam Pharmaceuticals Inc Composições do agente de irna da fase de leitura aberta 72 do cromossomo humano 9 (c9orf72) e métodos de uso das mesmas
WO2021154941A1 (en) 2020-01-31 2021-08-05 Alnylam Pharmaceuticals, Inc. Complement component c5 irna compositions for use in the treatment of amyotrophic lateral sclerosis (als)
KR20220140593A (ko) 2020-02-10 2022-10-18 알닐람 파마슈티칼스 인코포레이티드 Vegf-a 발현을 사일런싱하기 위한 조성물 및 방법
WO2021178607A1 (en) 2020-03-05 2021-09-10 Alnylam Pharmaceuticals, Inc. Complement component c3 irna compositions and methods of use thereof for treating or preventing complement component c3-associated diseases
WO2021188611A1 (en) 2020-03-18 2021-09-23 Alnylam Pharmaceuticals, Inc. Compositions and methods for treating subjects having a heterozygous alanine-glyoxylate aminotransferase gene (agxt) variant
JP2023519274A (ja) 2020-03-26 2023-05-10 アルナイラム ファーマシューティカルズ， インコーポレイテッド コロナウイルスｉＲＮＡ組成物およびその使用方法
US20230190785A1 (en) 2020-03-30 2023-06-22 Alnylam Pharmaceuticals, Inc. Compositions and methods for silencing dnajc15 gene expression
US20230295622A1 (en) 2020-04-06 2023-09-21 Alnylam Pharmaceuticals, Inc. Compositions and methods for silencing myoc expression
WO2021206922A1 (en) 2020-04-07 2021-10-14 Alnylam Pharmaceuticals, Inc. Transmembrane serine protease 2 (tmprss2) irna compositions and methods of use thereof
EP4133076A1 (en) 2020-04-07 2023-02-15 Alnylam Pharmaceuticals, Inc. Angiotensin-converting enzyme 2 (ace2) irna compositions and methods of use thereof
JP2023521094A (ja) 2020-04-07 2023-05-23 アルナイラム ファーマシューティカルズ， インコーポレイテッド Ｓｃｎ９ａ発現をサイレンシングするための組成物および方法
JP2023523993A (ja) 2020-04-27 2023-06-08 アルナイラム ファーマシューティカルズ， インコーポレイテッド アポリポタンパク質Ｅ（ＡｐｏＥ）ｉＲＮＡ剤組成物およびその使用方法
EP4153746A1 (en) 2020-05-21 2023-03-29 Alnylam Pharmaceuticals, Inc. Compositions and methods for inhibiting marc1 gene expression
EP4162050A1 (en) 2020-06-09 2023-04-12 Alnylam Pharmaceuticals, Inc. Rnai compositions and methods of use thereof for delivery by inhalation
EP4217489A1 (en) 2020-09-24 2023-08-02 Alnylam Pharmaceuticals, Inc. Dipeptidyl peptidase 4 (dpp4) irna compositions and methods of use thereof
WO2022076291A1 (en) 2020-10-05 2022-04-14 Alnylam Pharmaceuticals, Inc. G protein-coupled receptor 75 (gpr75) irna compositions and methods of use thereof
AU2021365822A1 (en) 2020-10-21 2023-06-08 Alnylam Pharmaceuticals, Inc. Methods and compositions for treating primary hyperoxaluria
EP4232582A1 (en) 2020-10-23 2023-08-30 Alnylam Pharmaceuticals, Inc. Mucin 5b (muc5b) irna compositions and methods of use thereof
CA3201452A1 (en) 2020-12-01 2022-06-09 Alnylam Pharmaceuticals, Inc. Methods and compositions for inhibition of hao1 (hydroxyacid oxidase 1 (glycolate oxidase)) gene expression
WO2022174000A2 (en) 2021-02-12 2022-08-18 Alnylam Pharmaceuticals, Inc. Superoxide dismutase 1 (sod1) irna compositions and methods of use thereof for treating or preventing superoxide dismutase 1- (sod1-) associated neurodegenerative diseases
WO2022182864A1 (en) 2021-02-25 2022-09-01 Alnylam Pharmaceuticals, Inc. Prion protein (prnp) irna compositions and methods and methods of use thereof
WO2022192519A1 (en) 2021-03-12 2022-09-15 Alnylam Pharmaceuticals, Inc. Glycogen synthase kinase 3 alpha (gsk3a) irna compositions and methods of use thereof
AR125230A1 (es) 2021-03-29 2023-06-28 Alnylam Pharmaceuticals Inc COMPOSICIONES DE AGENTES DE ARNi CONTRA HUNTINGTINA (HTT) Y SUS MÉTODOS DE USO
WO2022245583A1 (en) 2021-05-18 2022-11-24 Alnylam Pharmaceuticals, Inc. Sodium-glucose cotransporter-2 (sglt2) irna compositions and methods of use thereof
IL308743A (en) 2021-06-04 2024-01-01 Alnylam Pharmaceuticals Inc Compositions of human chromosome 9 open reading frame 72 iRNA factor (C9ORF72) and methods of using them
TW202333748A (zh) 2021-07-19 2023-09-01 美商艾拉倫製藥股份有限公司 用於處置具有或有風險發展非原發性高草酸鹽尿疾病或病症的個體的方法及組成物
WO2023076450A2 (en) 2021-10-29 2023-05-04 Alnylam Pharmaceuticals, Inc. HUNTINGTIN (HTT) iRNA AGENT COMPOSITIONS AND METHODS OF USE THEREOF
WO2023141314A2 (en) 2022-01-24 2023-07-27 Alnylam Pharmaceuticals, Inc. Heparin sulfate biosynthesis pathway enzyme irna agent compositions and methods of use thereof
WO2024059165A1 (en) 2022-09-15 2024-03-21 Alnylam Pharmaceuticals, Inc. 17b-hydroxysteroid dehydrogenase type 13 (hsd17b13) irna compositions and methods of use thereof

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5773581A (en) * 1990-07-23 1998-06-30 Zeneca Limited Conjugate of a solution stable G-CSF derivative and a water-soluble polymer
US6506730B1 (en) * 1999-08-17 2003-01-14 Kang Choon Lee Nasal transmucosal delivery of peptide conjugated with biocompatible polymers
US20030027748A1 (en) * 2001-06-04 2003-02-06 Ekwuribe Nnochiri N. Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
US20030060606A1 (en) * 2001-06-04 2003-03-27 Ekwuribe Nnochiri N. Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
US20030153488A1 (en) * 1998-01-21 2003-08-14 Georgia Tech Research Corporation Method for reducing inflammation and inducing an analgesic effect and compounds thereof
US20060100137A1 (en) * 2001-02-15 2006-05-11 Ekwuribe Nnochiri N Methods of treating diabetes mellitus

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2769838A (en) * 1953-11-20 1956-11-06 Ciba Pharm Prod Inc Polyglycol ether acid anilides
US3256153A (en) 1963-02-08 1966-06-14 Smith Kline French Lab Method of stabilizing wax-fat coating materials and product thereof
US4003792A (en) 1967-07-01 1977-01-18 Miles Laboratories, Inc. Conjugates of acid polysaccharides and complex organic substances
US4044196A (en) 1972-03-30 1977-08-23 Bayer Aktiengesellschaft Crosslinked copolymers of α,β-olefinically unsaturated dicarboxylic anhydrides
US4179337A (en) 1973-07-20 1979-12-18 Davis Frank F Non-immunogenic polypeptides
FR2408387A2 (fr) 1975-06-30 1979-06-08 Oreal Compositions a base de dispersions aqueuses de spherules lipidiques
JPS53116315A (en) 1977-03-17 1978-10-11 Ueno Seiyaku Oyo Kenkyujo Kk Powder or granular containing improved sorbinic acid
ATE37983T1 (de) * 1982-04-22 1988-11-15 Ici Plc Mittel mit verzoegerter freigabe.
US4698264A (en) 1982-08-02 1987-10-06 Durkee Industrial Foods, Corp. Particulate composition and process for making same
US4585754A (en) 1984-01-09 1986-04-29 Valcor Scientific, Ltd. Stabilization of proteins and peptides by chemical binding with chondroitin
US4684524A (en) 1984-03-19 1987-08-04 Alza Corporation Rate controlled dispenser for administering beneficial agent
US4717566A (en) 1984-03-19 1988-01-05 Alza Corporation Dosage system and method of using same
US4963367A (en) 1984-04-27 1990-10-16 Medaphore, Inc. Drug delivery compositions and methods
US4849405A (en) 1984-05-09 1989-07-18 Synthetic Blood Corporation Oral insulin and a method of making the same
US4622392A (en) 1984-06-21 1986-11-11 Health Research Inc. (Roswell Park Division) Thiophospholipid conjugates of antitumor agents
US4629621A (en) 1984-07-23 1986-12-16 Zetachron, Inc. Erodible matrix for sustained release bioactive composition
US4797288A (en) 1984-10-05 1989-01-10 Warner-Lambert Company Novel drug delivery system
SE457326B (sv) 1986-02-14 1988-12-19 Lejus Medical Ab Foerfarande foer framstaellning av en snabbt soenderfallande kaerna innehaallande bl a mikrokristallin cellulosa
US5093198A (en) 1987-06-19 1992-03-03 Temple University Adjuvant-enhanced sustained release composition and method for making
DE3721721C1 (de) 1987-07-01 1988-06-09 Hoechst Ag Verfahren zur Umhuellung von Granulaten
DE3818435A1 (de) * 1988-02-19 1989-08-31 Hoechst Ag Optisch aktive rhodiumkomplexe von 3,4-bis(diarylphosphino)-pyrrolidinen und ihre verwendung zur herstellung von phosphinothricin durch asymmetrische hydrierung
JPH01308231A (ja) 1988-06-03 1989-12-12 Takeda Chem Ind Ltd 安定化された医薬組成物および製造法
US5055300A (en) 1988-06-17 1991-10-08 Basic Bio Systems, Inc. Time release protein
US5108568A (en) * 1989-07-07 1992-04-28 The United States Of America As Represented By The Administrator Of The National Aeronautics And Space Administration Controlled method of reducing electrophoretic mobility of macromolecules, particles or cells
US5013556A (en) 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
EP0580778B1 (en) * 1991-04-19 1999-08-11 LDS Technologies, Inc. Convertible microemulsion formulations
CH683149A5 (fr) 1991-07-22 1994-01-31 Debio Rech Pharma Sa Procédé pour la préparation de microsphères en matériau polymère biodégradable.
US5206219A (en) * 1991-11-25 1993-04-27 Applied Analytical Industries, Inc. Oral compositions of proteinaceous medicaments
EP0736041B1 (en) * 1993-11-17 2006-02-08 Athena Neurosciences, Inc. Transparent liquid for encapsulated drug delivery
US5932462A (en) 1995-01-10 1999-08-03 Shearwater Polymers, Inc. Multiarmed, monofunctional, polymer for coupling to molecules and surfaces

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5773581A (en) * 1990-07-23 1998-06-30 Zeneca Limited Conjugate of a solution stable G-CSF derivative and a water-soluble polymer
US20030153488A1 (en) * 1998-01-21 2003-08-14 Georgia Tech Research Corporation Method for reducing inflammation and inducing an analgesic effect and compounds thereof
US6506730B1 (en) * 1999-08-17 2003-01-14 Kang Choon Lee Nasal transmucosal delivery of peptide conjugated with biocompatible polymers
US20060100137A1 (en) * 2001-02-15 2006-05-11 Ekwuribe Nnochiri N Methods of treating diabetes mellitus
US20030027748A1 (en) * 2001-06-04 2003-02-06 Ekwuribe Nnochiri N. Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
US20030060606A1 (en) * 2001-06-04 2003-03-27 Ekwuribe Nnochiri N. Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040203081A1 (en) * 2002-11-26 2004-10-14 James Kenneth D. Natriuretic compounds, conjugates, and uses thereof
US7662773B2 (en) 2002-11-26 2010-02-16 Biocon Limited Natriuretic compounds, conjugates, and uses thereof
US7651996B2 (en) 2003-12-08 2010-01-26 Cpex Pharmaceuticals, Inc. Pharmaceutical compositions and methods for insulin treatment
US20080021005A1 (en) * 2004-04-01 2008-01-24 Cardiome Pharma Corp. Pegylated Ion Channel Modulating Compounds
US7786119B2 (en) 2004-04-01 2010-08-31 Cardiome Pharma Corp. Drug conjugates of ion channel modulating compounds
US20100273724A1 (en) * 2004-04-01 2010-10-28 Cardiome Pharma Corp. Pegylated ion channel modulating compounds
US20080207505A1 (en) * 2005-01-12 2008-08-28 James Kenneth D Bna Conjugates and Methods of Use
US20090036353A1 (en) * 2005-01-27 2009-02-05 Novo Nordisk A/S Insulin Derivatives Conjugated with Structurally Well Defined Branched Polymers
US9260501B2 (en) 2006-10-27 2016-02-16 Novo Nordisk A/S Peptide extended insulins
US20080139392A1 (en) * 2006-12-12 2008-06-12 Edgar Joel Acosta-Zara Linker-Based Lecithin Microemulsion Delivery Vehicles
US9918934B2 (en) * 2006-12-12 2018-03-20 Edgar Joel Acosta-Zara Linker-based lecithin microemulsion delivery vehicles
US8309123B2 (en) * 2007-12-19 2012-11-13 Farid Bennis Pharmaceutical compositions and methods for the oral delivery of insulin
US20090176691A1 (en) * 2007-12-19 2009-07-09 Farid Bennis Pharmaceutical Compositions Containing at Least One Protein Active Ingredient Protected From Digestive Enzymes
US9682153B2 (en) 2008-09-19 2017-06-20 Nektar Therapeutics Polymer conjugates of therapeutic peptides
US20110230435A1 (en) * 2008-11-18 2011-09-22 Vatner Stephen F Methods and Compositions for Treating Obesity and Related Disorders
US8440640B2 (en) 2008-11-18 2013-05-14 University Of Medicine And Dentistry Of New Jersey Methods and compositions for treating obesity and related disorders
WO2010059204A1 (en) * 2008-11-18 2010-05-27 University Of Medicine And Dentistry Of New Jersey Methods and compositions for treating obesity and related disorders

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