US Patent No: 5,451,410

Number of patents in Portfolio can not be more than 2000

Modified amino acids for encapsulating active agents

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Abstract

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Modified amino acids and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described. The modified amino acids are preparable by reacting single amino acids or mixtures of two or more kinds of amino acids with an amino modifying agent such as benzene sulfonyl chloride, benzoyl chloride, and hippuryl chloride. The modified amino acids form encapsulating microspheres in the presence of the active agent under sphere-forming conditions. Alternatively, the modified amino acids may be used as a carrier by simply mixing the amino acids with the active agent. The modified amino acids are particularly useful in delivering peptides, e.g. insulin or calmodulin, or other agents which are sensitive to the denaturing conditions of the gastrointestinal tract.

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Patent Owner(s)

Patent OwnerAddressTotal Patents
EMISPHERE TECHNOLOGIES, INC.TARRYTOWN, NY142

International Classification(s)

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Barantsetvich, Evgueni N New Rochelle, NY 1 102
Milstein, Sam J Larchmont, NY 59 2117

Cited Art Landscape

Patent Info (Count) # Cites Year
 
Other [Check patent profile for assignment information] (1)
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Emisphere Technologies, Inc. (5)
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JAPAN ATOMIC ENERGY RESEARCH INSTITUTE (1)
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CESKOSLOVENSKA AKADEMIE VED (1)
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The Nisshin Oil Mills, Ltd. (1)
* 4,757,007 Process for preparing hydrolyzed products of soy protein 77 1985
 
NURTURE BIOTECH INC. A DE CORP. (1)
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DAINIPPON PHARMACEUTICAL CO., LTD. (1)
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Biomaterials Universe, Inc. (1)
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BOEHRINGER BIOCHEMIA ROBIN S.P.A. (1)
* 4,753,804 Granular dietetic product based on amino acids and process for their preparation 79 1985
 
THE OHIO STATE UNIVERSITY (1)
* 4,608,278 Small particule formation and encapsulation 95 1984
 
MITSUI TOATSU CHEMICALS, INC. (1)
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Toyo Jozo Kabushiki Kaisha (1)
* 4,873,087 Suppository preparation having excellent absorption property 106 1982
 
Kyoto Yakuhin Kogyo Kabushiki Kaisha (1)
* 4,442,090 Absorption-promoting compounds, compositions thereof with pharmaceuticals and/or bases for rectal administration and method of use 87 1981
 
SANOFI, A FRENCH CORP. (1)
* 5,204,099 Cosmetic composition containing amino acid copolymers which is useful as a moisturizer 101 1991
 
PTLNV, LLC, SERIES ONE (1)
* 5,069,936 Manufacturing protein microspheres 172 1989
 
MORELLE, JEAN V. (1)
* 5,066,487 Antisudoral composition comprising dibasic aluminium salts of acylated amino acids 89 1989
* Cited By Examiner

Patent Citation Ranking

Forward Cite Landscape

Patent Info (Count) # Cites Year
 
Emisphere Technologies, Inc. (81)
5,792,451 Oral drug delivery compositions and methods 105 1994
* 5,629,020 Modified amino acids for drug delivery 119 1994
5,972,387 Modified hydrolyzed vegetable protein microspheres and methods for preparation and use thereof 19 1994
5,709,861 Compositions for the delivery of antigens 73 1995
5,650,386 Compositions for oral delivery of active agents 111 1995
5,958,457 Compositions for the delivery of antigens 44 1995
6,180,140 Modified amino acids for drug delivery 34 1995
5,766,633 Oral drug delivery compositions and methods 78 1995
5,811,127 Desferrioxamine oral delivery system 65 1996
6,099,856 Active agent transport systems 58 1996
6,100,298 Compounds and compositions for delivering active agents 44 1997
6,001,347 Compounds and compositions for delivering active agents 55 1997
5,989,539 Compounds and compositions for delivering active agents 45 1997
5,965,121 Compounds and compositions for delivering active agents 48 1997
5,955,503 Compounds and compositions for delivering active agents 37 1997
5,866,536 Compounds and compositions for delivering active agents 77 1997
6,313,088 8-[(2-hydroxy-4-methoxy benzoyl) amino]-octanoic acid compositions for delivering active agents 30 1997
6,090,958 Compounds and compositions for delivering active agents 45 1997
6,060,513 Compounds and compositions for delivering active agents 44 1997
5,990,166 Compounds and compositions for delivering active agents 46 1997
5,939,381 Compounds and compositions for delivering active agents 34 1997
5,879,681 Compounds and compositions for delivering active agents 43 1997
5,876,710 Compounds and compositions for delivering active agents 41 1997
5,804,688 Compounds and compositions for delivering active agents 40 1997
6,344,213 Compounds and compositions for delivering active agents 31 1997
6,071,510 Modified amino acids and compositions comprising the same for delivering active agents 52 1997
5,863,944 Compounds and compositions for delivering active agents 45 1997
5,962,710 Method of preparing salicyloylamino acids 30 1997
6,375,983 Microencapsulated fragrances and method for preparation 19 1997
6,221,367 Active agent transport systems 41 1997
6,348,207 Orally deliverable supramolecular complex 26 1997
6,245,359 Active agent transport systems 46 1997
6,071,538 Oral delivery composition comprising supramolecular complex 42 1997
6,100,285 Method of solubilizing itraconazole 27 1997
6,084,112 Method for preparing .omega.-aminoalkanoic acid derivatives from cycloalkanones 21 1997
6,413,550 Proteinoid carriers and methods for preparation and use thereof 11 1998
6,391,303 Methods and compositions for inducing oral tolerance in mammals 14 1999
6,428,780 Compounds and compositions for delivering active agents 21 1999
6,991,798 Compounds and compositions for delivering active agents 2 1999
6,461,545 Method of solubilizing and encapsulating itraconazole 4 2000
6,346,242 Compounds and compositions for delivering active agents 25 2000
6,242,495 Compounds and compositions for delivering active agents 40 2000
7,279,597 Phenyl amine carboxylic acid compounds and compositions for delivering active agents 3 2000
7,129,274 Phenoxy carboxylic acid compounds and compositions for delivering active agents 3 2000
* 2001/0039,258 Active agent transport systems 3 2001
7,151,191 Compounds and compositions for delivering active agents 3 2001
6,642,411 Compounds and compositions for delivering active agents 17 2001
6,440,929 Pulmonary delivery of active agents 16 2001
6,610,329 Compositions for the delivery of antigens 18 2001
6,461,643 Oral drug delivery compositions and methods 21 2001
7,351,741 Compounds and compositions for delivering active agents 9 2001
6,646,162 Compounds and compositions for delivering active agents 18 2001
6,623,731 Compounds and compositions for delivering active agents 16 2001
6,525,020 Compounds and compositions for delivering active agents 15 2001
6,960,355 Compounds and compositions for delivering active agents 1 2001
7,084,279 Oxadiazole compounds and compositions for delivering active agents 3 2002
6,663,887 Compounds and compositions for delivering active agents 14 2002
6,693,208 Compounds and compositions for delivering active agents 17 2002
6,916,489 Active agent transport systems 1 2002
* 2003/0133,953 Active agent transport systems 2 2002
7,208,483 Polymeric delivery agents and delivery agent compounds 1 2003
* 2003/0225,300 Compounds and compositions for delivering active agents 7 2003
* 2004/0048,777 Compounds and compositions for delivering active agents 3 2003
* 2004/0068,013 Compounds and compositions for delivering active agents 3 2003
* 2005/0148,497 Method for administering glp-1 molecules 21 2004
7,186,414 Compounds and compositions for delivering active agents 2 2005
7,553,872 Compounds and compositions for delivering active agents 2 2006
8,410,309 Phenoxy carboxylic acid compounds and compositions for delivering active agents 0 2006
* 2007/0049,557 Solid pharmaceutical dosage forms comprising bisphosphonates and modified amino acid carriers 4 2006
7,744,910 Compounds and compositions for delivering active agents 3 2006
* 2007/0010,422 COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS 0 2006
7,977,506 Compounds and compositions for delivering active agents 0 2006
8,927,015 Formulations for delivering insulin 0 2007
8,895,777 Compounds and compositions for delivering active agents 0 2007
7,951,971 Phenoxy carboxylic acid compounds and compositions for delivering active agents 0 2008
7,939,494 Method for administering GLP-1 molecules 1 2009
8,686,154 Compounds and compositions for delivering active agents 0 2009
8,785,381 Oral GLP-1 formulations 0 2009
* 2010/0016,229 Oral GLP-1 Formulations 4 2009
* 2009/0281,064 SOLID PHARMACEUTICAL DOSAGE FORMS COMPRISING BISPHOSPHONATES AND MODIFIED AMINO ACID CARRIERS 6 2009
8,492,330 Formulation comprising GLP-1 0 2011
 
Other [Check patent profile for assignment information] (1)
* 2009/0286,735 METHOD FOR ADMINISTERING GLP-1 MOLECULES 2 2009
 
ALNIS BIOSCIENCES, INC. (1)
* 2004/0126,900 High affinity peptide- containing nanoparticles 12 2003
 
ManKind Corporation (1)
9,192,675 Dry powder inhaler and system for drug delivery 0 2013
 
IRONWOOD PHARMACEUTICALS, INC. (2)
8,802,628 Stable solid formulation of a GC-C receptor agonist polypeptide suitable for oral administration 1 2009
8,748,573 Formulations comprising linaclotide 1 2010
 
SHIRE LLC (7)
6,716,452 Active agent delivery systems and methods for protecting and administering active agents 48 2000
7,018,654 Pharmaceutical composition containing an active agent in an amino acid copolymer structure 6 2001
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8,133,881 Carbohydrate conjugates to prevent abuse of controlled substances 0 2005
8,106,016 Compounds and compositions for prevention of overdose of oxycodone 0 2006
8,394,813 Active agent delivery systems and methods for protecting and administering active agents 0 2008
8,343,927 Pharmaceutical compositions for prevention of overdose or abuse 0 2010
 
NOVARTIS AG (9)
7,384,982 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 3 2003
* 2004/0106,825 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 4 2003
7,659,311 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 5 2008
* 2008/0269,134 DISODIUM SALTS, MONOHYDRATES, AND ETHANOL SOLVATES FOR DELIVERING ACTIVE AGENTS 0 2008
8,003,697 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 0 2009
7,915,314 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 0 2009
* 2010/0099,621 DISODIUM SALTS, MONOHYDRATES, AND ETHANOL SOLVATES FOR DELIVERING ACTIVE AGENTS 2 2009
8,207,227 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 0 2011
8,658,695 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 0 2012
 
Ironwwod Pharmaceuticals, Inc. (1)
8,933,030 Treatments for gastrointestinal disorders 0 2011
 
MHR Institutional Partners IIA LP (3)
* 2005/0042,274 Compounds and compositions for delivering active agents 0 2003
* 2005/0255,138 Active agent transport systems 0 2005
7,417,022 Compounds and compositions for delivering active agents 1 2005
 
VIRGINIA COMMONWEALTH UNIVERSITY (3)
6,627,228 Polymeric delivery agents and delivery agents compounds 29 2001
7,727,558 Polymeric delivery agents and delivery agent compounds 0 2007
* 2007/0141,022 POLYMERIC DELIVERY AGENTS AND DELIVERY AGENT COMPOUNDS 1 2007
 
D-DUE DIVISIONE LASER S.R.L. (1)
* 2010/0239,658 GALLIUM NITRATE FORMULATIONS 0 2007
 
NEC CORPORATION (1)
* 2005/0188,038 Method, device and computer readable medium for classifying electronic mails 97 2005
 
MANNKIND CORPORATION (10)
5,976,569 Diketopiperazine-based delivery systems 90 1997
6,395,774 Carbon-substituted diketopiperazine delivery systems 59 2001
6,906,030 Carbon-substituted diketopiperazine delivery systems 11 2003
* 2003/0198,658 Carbon-substituted diketopiperazine delivery systems 2 2003
7,276,534 Carbon-substituted diketopiperazine delivery systems 29 2005
* 2008/0008,764 CARBON-SUBSTITUTED DIKETOPIPERAZINE DELIVERY SYSTEMS 1 2007
8,133,514 Carbon-substituted diketopiperazine delivery systems 5 2009
9,241,903 Method for improving the pharmaceutic properties of microparticles comprising diketopiperazine and an active agent 0 2013
9,283,193 Method of drug formulation based on increasing the affinity of crystalline microparticle surfaces for active agents 0 2014
9,220,687 Substituted diketopiperazine analogs for use as drug delivery agents 0 2014
 
BAXTER INTERNATIONAL INC. (3)
6,090,925 Macromolecular microparticles and methods of production and use 120 1996
5,981,719 Macromolecular microparticles and methods of production and use 110 1998
6,268,053 Macromolecular microparticles and methods of production and use 91 2000
 
TORREY PINES INSTITUTE FOR MOLECULAR STUDIES (1)
9,233,159 Methods and compositions for treating pain 0 2012
* Cited By Examiner