
US Patent No: 6,858,580
Number of patents in Portfolio can not be more than 2000
Mixtures of drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
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Feb 22, 2005
Issued date -
Jun 4, 2001
filing date -
09/873,797
serial no -
In Force
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Abstract
A non-polydispersed mixture of conjugates in which each conjugate in the mixture comprises a drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may result in less inter-subject variability than polydispersed mixtures of similar conjugates.
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First Claim
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International Classification(s)
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Cited Art
| Patent Info | (Count) | # Cites | Year |
|---|---|---|---|
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| 4,839,341 Stabilized insulin formulations | 49 | 1987 | |
| 5,304,473 A-C-B proinsulin, method of manufacturing and using same, and intermediates in insulin production | 50 | 1991 | |
| 5,457,066 Process for transforming a human insulin precursor to human insulin | 36 | 1992 | |
| 5,461,031 Monomeric insulin analog formulations | 52 | 1994 | |
| 5,504,188 Preparation of stable zinc insulin analog crystals | 40 | 1994 | |
| 5,646,242 Selective acylation of epsilon-amino groups | 40 | 1994 | |
| 5,693,609 Acylated insulin analogs | 49 | 1994 | |
| 5,747,642 Monomeric insulin analog formulations | 41 | 1995 | |
| 5,631,347 Reducing gelation of a fatty acid-acylated protein | 35 | 1995 | |
| 5,700,904 Preparation of an acylated protein powder | 57 | 1995 | |
| 5,952,297 Monomeric insulin analog formulations | 39 | 1997 | |
| 5,922,675 Acylated Insulin Analogs | 55 | 1997 | |
| 6,034,054 Stable insulin formulations | 44 | 1998 | |
| 6,268,335 Insoluble insulin compositions | 34 | 1998 | |
| 6,051,551 Method for administering acylated insulin | 46 | 1998 | |
| 6,335,316 Method for administering acylated insulin | 48 | 2000 | |
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| 5,122,614 Active carbonates of polyalkylene oxides for modification of polypeptides | 280 | 1990 | |
| 5,312,808 Fractionation of polyalkylene oxide-conjugated hemoglobin solutions | 47 | 1992 | |
| 5,468,478 Conjugates of superoxide dismutage coupled to high molecular weight polyalkylene glycols | 122 | 1993 | |
| 5,643,575 Non-antigenic branched polymer conjugates | 255 | 1993 | |
| 5,612,460 Active carbonates of polyalkylene oxides for modification of polypeptides | 132 | 1994 | |
| 5,567,422 Azlactone activated polyalkylene oxides conjugated to biologically active nucleophiles | 97 | 1994 | |
| 5,405,877 Cyclic imide thione activated polyalkylene oxides | 56 | 1994 | |
| 5,650,388 Fractionated polyalkylene oxide-conjugated hemoglobin solutions | 37 | 1995 | |
| 5,637,749 Aryl imidate activated polyalkylene oxides | 76 | 1995 | |
| 5,738,846 Interferon polymer conjugates and process for preparing the same | 75 | 1995 | |
| 5,681,567 Method of preparing polyalkylene oxide carboxylic acids | 65 | 1996 | |
| 5,969,040 Factor IX -- polymeric conjugates | 77 | 1996 | |
| 5,902,588 Non-antigenic amine derived polymers and polymer conjugates | 48 | 1997 | |
| 6,177,087 Non-antigenic amine derived polymers and polymer conjugates | 48 | 1998 | |
| 6,113,906 Water-soluble non-antigenic polymer linkable to biologically active material | 118 | 1998 | |
| 6,042,822 Interferon polymer conjugates | 43 | 1999 | |
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| 4,946,828 Novel insulin peptides | 62 | 1987 | |
| 5,164,366 Human insulin analogues | 50 | 1989 | |
| 5,202,415 Insulin precursors | 26 | 1990 | |
| 5,157,021 Insulin derivatives and pharmaceutical preparations containing these derivatives | 29 | 1990 | |
| 5,750,497 Acylated insulin | 35 | 1995 | |
| 5,948,751 X14-mannitol | 46 | 1997 | |
| 5,866,538 Insulin preparations containing NaCl | 33 | 1997 | |
| 5,905,140 Selective acylation method | 31 | 1997 | |
| 6,251,856 Insulin derivatives | 31 | 1997 | |
| 5,898,028 Method for producing powder formulation comprising an insulin | 91 | 1998 | |
| 6,043,214 Method for producing powder formulation comprising an insulin | 34 | 1998 | |
| 6,310,038 Pulmonary insulin crystals | 42 | 1998 | |
| 6,211,144 Stable concentrated insulin preparations for pulmonary delivery | 40 | 1999 | |
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| 5,162,430 Collagen-polymer conjugates | 261 | 1989 | |
| 5,324,775 Biologically inert, biocompatible-polymer conjugates | 153 | 1992 | |
| 5,328,955 Collagen-polymer conjugates | 163 | 1992 | |
| 5,292,802 Collagen-polymer tubes for use in vascular surgery | 138 | 1992 | |
| 5,308,889 Dehydrated collagen-polymer strings | 129 | 1992 | |
| 5,413,791 Collagen-polymer conjugates | 52 | 1994 | |
| 5,523,348 Method of preparing collagen-polymer conjugates | 36 | 1994 | |
| 5,446,091 Collagen-polymer conjugates containing an ether linkage | 44 | 1995 | |
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| 5,658,878 Therapeutic preparation for inhalation | 55 | 1995 | |
| 5,747,445 Therapeutic preparation for inhalation | 75 | 1996 | |
| 6,004,574 Powder formulations containing melezitose as a diluent | 40 | 1996 | |
| 5,952,008 Processes for preparing compositions for inhalation | 84 | 1997 | |
| 6,165,976 Therapeutic preparation for inhalation | 37 | 1998 | |
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| 5,506,203 Systemic administration of a therapeutic preparation | 123 | 1994 | |
| 5,518,998 Therapeutic preparation for inhalation | 118 | 1994 | |
| 6,306,440 Therapeutic preparation for inhalation | 35 | 1997 | |
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| 5,681,811 Conjugation-stabilized therapeutic agent compositions, delivery and diagnostic formulations comprising same, and method of making and using the same | 91 | 1995 | |
| 6,191,105 Hydrophilic and lipophilic balanced microemulsion formulations of free-form and/or conjugation-stabilized therapeutic agents such as insulin | 48 | 1997 | |
| 6,309,633 Amphiphilic drug-oligomer conjugates with hydroyzable lipophile components and methods for making and using the same | 90 | 1999 | |
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| 4,684,524 Rate controlled dispenser for administering beneficial agent | 80 | 1985 | |
| 4,717,566 Dosage system and method of using same | 73 | 1986 | |
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| 5,444,041 Convertible microemulsion formulations | 85 | 1992 | |
| 5,707,648 Transparent liquid for encapsulated drug delivery | 73 | 1995 | |
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| 4,917,888 Solubilization of immunotoxins for pharmaceutical compositions using polymer conjugation | 125 | 1987 | |
| 5,089,261 Preparation of a polymer/interleukin-2 conjugate | 76 | 1989 | |
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| 5,942,248 Pharmaceutical composition containing a low detergent effect bile salt and an active compound that undergoes biliary excretion and/or enterohepatic recycling | 40 | 1995 | |
| 5,968,549 Solubilisation aids | 27 | 1997 | |
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| 5,415,872 Compositions of gastric acid-resistant microspheres containing salts of bile acids | 35 | 1993 | |
| 5,405,621 Compositions of gastric acid-resistant microspheres containing buffered bile acids | 31 | 1993 | |
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| 5,597,797 Method for treatment or prevention of obesity | 77 | 1993 | |
| 6,057,292 Method for inhibiting growth hormone action | 65 | 1998 | |
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| 5,359,030 Conjugation-stabilized polypeptide compositions, therapeutic delivery and diagnostic formulations comprising same, and method of making and using the same | 109 | 1993 | |
| 5,438,040 Conjugation-stabilized polypeptide compositions, therapeutic delivery and diagnostic formulations comprising same, and method of making and using the same | 81 | 1994 | |
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| 4,849,405 Oral insulin and a method of making the same | 43 | 1986 | |
| 4,963,526 Oral insulin and a method of making the same | 43 | 1988 | |
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| 4,229,438 Nonapeptides | 45 | 1979 | |
| 4,277,394 Tetrapeptidehydrazide derivatives | 34 | 1979 | |
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| 4,348,387 Method and system for the controlled release of biologically active substances to a body fluid | 37 | 1979 | |
| 4,469,681 Method and system for the controlled release of biologically active substances to a body fluid | 32 | 1981 | |
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| 5,206,219 Oral compositions of proteinaceous medicaments | 127 | 1991 | |
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| 4,253,998 Peptides related to somatostatin | 32 | 1979 | |
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| 5,714,639 Double metal cyanide catalysts and methods for making them | 31 | 1997 | |
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| 5,830,853 Systemic administration of a therapeutic preparation | 106 | 1996 | |
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| 5,763,396 Method of treating or preventing type 1 diabetes by oral administration of insulin | 36 | 1995 | |
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| 5,099,074 Process for the preparation of polyether glycols | 26 | 1990 | |
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| 5,866,584 Therapeutic process for the treatment of the pathologies of type II diabetes | 21 | 1995 | |
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| 4,797,288 Novel drug delivery system | 101 | 1985 | |
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| 4,994,439 Transmembrane formulations for drug administration | 104 | 1989 | |
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| 5,550,188 Polymer conjugates ophthalmic devices comprising collagen-polymer conjugates | 54 | 1995 | |
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| 5,606,038 Amphiphilic polyene macrolide antibiotic compounds | 29 | 1995 | |
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| 5,286,637 Biologically active drug polymer derivatives and method for preparing same | 86 | 1993 | |
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| 6,063,761 Hepatoselective pharmaceutical actives | 33 | 1998 | |
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| 4,698,264 Particulate composition and process for making same | 75 | 1985 | |
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| 5,981,709 .alpha.-interferon-polymer-conjugates having enhanced biological activity and methods of preparing the same | 39 | 1997 | |
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| 6,025,235 Short channel transistor having resistive gate extensions | 26 | 1998 | |
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| 4,579,730 Pharmaceutical compositions containing insulin | 58 | 1984 | |
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| 5,843,866 Pesticidal compositions comprising solutions of polyurea and/or polyurethane | 14 | 1996 | |
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| 5,962,267 Proinsulin derivative and process for producing human insulin | 35 | 1996 | |
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| 4,622,392 Thiophospholipid conjugates of antitumor agents | 52 | 1984 | |
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| 5,889,153 Protein or polypeptide, method for producing the same and intermediate compound therefor | 18 | 1997 | |
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| 4,935,246 Process for the coating of granules | 99 | 1988 | |
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| 5,849,860 Polyethylene-protein conjugates | 77 | 1995 | |
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| 4,410,547 Sorbic acid-containing powder or granules | 33 | 1981 | |
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| 5,854,208 Hepatoselective pharmaceutical actives | 35 | 1996 | |
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| 6,342,225 Pharmaceutical active conjugates | 36 | 2000 | |
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| 4,338,306 Adjuvant for promoting absorption of pharmacologically active substances through the rectum | 41 | 1980 | |
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| 4,772,471 Aqueous dispersions of lipid spheres and compositions containing the same | 95 | 1979 | |
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| 4,840,799 Process for preparing rapidly disintegrating granulates | 82 | 1987 | |
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| 6,248,363 Solid carriers for improved delivery of active ingredients in pharmaceutical compositions | 271 | 1999 | |
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| 5,013,556 Liposomes with enhanced circulation time | 452 | 1989 | |
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| 5,985,263 Substantially pure histidine-linked protein polymer conjugates | 65 | 1997 | |
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| 4,957,910 Method and composition for the treatment and prevention of viral infections | 33 | 1988 | |
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| 5,932,462 Multiarmed, monofunctional, polymer for coupling to molecules and surfaces | 312 | 1995 | |
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| 4,554,101 Identification and preparation of epitopes on antigens and allergens on the basis of hydrophilicity | 252 | 1983 | |
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| 4,585,745 Dielectric ceramic composition for high frequency purposes | 9 | 1984 | |
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| 5,856,451 Method for reducing respiratory allergenicity | 53 | 1997 | |
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| 5,055,300 Time release protein | 99 | 1989 | |
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| 5,283,236 Systemic delivery of polypeptides through the eye | 31 | 1992 | |
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| 5,349,052 Process for fractionating polyethylene glycol (PEG)-protein adducts and an adduct for PEG and granulocyte-macrophage colony stimulating factor | 70 | 1993 | |
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| 6,258,377 Hydrophobic preparations containing medium chain monoglycerides | 47 | 1998 | |
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| 5,298,410 Lyophilized formulation of polyethylene oxide modified proteins with increased shelf-life | 54 | 1993 | |
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| 4,472,382 Treatment method | 90 | 1983 | |
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| 5,545,618 GLP-1 analogs useful for diabetes treatment | 156 | 1993 | |
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| 5,874,111 Process for the preparation of highly monodispersed polymeric hydrophilic nanoparticles | 62 | 1997 | |
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| 5,055,304 Stabilized pharmaceutical composition and method of producing same | 40 | 1989 | |
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| 5,529,915 Lyophilized polyethylene oxide modified protein and polypeptide complexes with cyclodextrin | 86 | 1995 | |
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| 5,824,638 Oral insulin delivery | 52 | 1995 | |
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| 6,093,391 Peptide copolymer compositions | 60 | 1998 | |
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| 5,320,840 Continuous release pharmaceutical compositions | 46 | 1991 | |
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| 4,963,367 Drug delivery compositions and methods | 221 | 1987 | |
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| 5,830,918 Nonpeptide insulin receptor agonists | 33 | 1997 | |
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| 5,093,198 Adjuvant-enhanced sustained release composition and method for making | 42 | 1989 | |
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| 4,223,163 Process for making ethoxylated fatty alcohols with narrow polyethoxy chain distribution | 47 | 1976 | |
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| 4,801,575 Chimeric peptides for neuropeptide delivery through the blood-brain barrier | 142 | 1986 | |
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| 5,766,620 Buccal delivery of glucagon-like insulinotropic peptides | 68 | 1995 | |
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| 5,693,769 Glycosylated steroid derivatives for transport across biological membranes and process for making and using same | 36 | 1994 | |
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| 5,907,030 Method and compositions for lipidization of hydrophilic molecules | 26 | 1995 | |
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| 6,323,311 Synthesis of insulin derivatives | 34 | 1999 | |
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| 5,853,748 Pharmaceutical compositions | 51 | 1997 | |
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| 4,744,976 Erodible matrix for sustained release bioactive composition | 52 | 1986 | |
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| 6,200,602 Composition for enhanced uptake of polar drugs from the colon | 56 | 1998 | |
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| 6,011,008 Conjugates of biologically active substances | 45 | 1998 | |
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| 5,428,128 Site specific synthesis of conjugated peptides | 57 | 1994 | |
| 6,506,730 Nasal transmucosal delivery of peptide conjugated with biocompatible polymers | 28 | 2000 | |
Patent Citation Ranking
Maintenance Fees
| Fee | Large entity fee | small entity fee | micro entity fee | due date |
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| 11.5 Year Payment | $7400.00 | $3700.00 | $1850.00 | Aug 22, 2016 |
| Fee | Large entity fee | small entity fee | micro entity fee |
|---|---|---|---|
| Surcharge - 11.5 year - Late payment within 6 months | $160.00 | $80.00 | $40.00 |
| Surcharge after expiration - Late payment is unavoidable | $700.00 | $350.00 | $175.00 |
| Surcharge after expiration - Late payment is unintentional | $1,640.00 | $820.00 | $410.00 |