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

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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First Claim

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Patent Owner(s)

Patent OwnerAddressTotal Patents
EMISPHERE TECHNOLOGIES, INC.TARRYTOWN, NY146

International Classification(s)

  • [Classification Symbol]
  • [Patents Count]

Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Barantsetvich, Evgueni N New Rochelle, NY 1 88
Milstein, Sam J Larchmont, NY 60 1520

Cited Art

Patent Info (Count) # Cites Year
 
EMISPHERE TECHNOLOGIES, INC. (5)
4,446,138 Method and composition for reducing weight 66 1982
4,925,673 Delivery systems for pharmacological agents encapsulated with proteinoids 256 1987
4,895,725 Microencapsulation of fish oil 97 1988
4,976,968 Anhydrous delivery systems for pharmacological agents 115 1989
4,983,402 Orally administerable ANF 79 1989
 
BIOMATERIALS UNIVERSE, INC. (1)
5,100,669 Polylactic acid type microspheres containing physiologically active substance and process for preparing the same 168 1989
 
BOEHRINGER BIOCHEMIA ROBIN S.P.A. (1)
4,753,804 Granular dietetic product based on amino acids and process for their preparation 75 1985
 
CESKOSLOVENSKA AKADEMIE VED (1)
4,745,161 Soluble and biodegradable polyamino acid activated for bonding of biologically active compound 84 1986
 
DAINIPPON PHARMACEUTICAL CO., LTD. (1)
4,348,384 Pharmaceutical composition for oral administration containing coagulation factor VIII or IX 109 1981
 
JAPAN ATOMIC ENERGY RESEARCH INSTITUTE (1)
4,483,807 Process for producing a slow release composite 75 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 85 1981
 
MITSUI TOATSU CHEMICALS, INC. (1)
4,835,312 Production process of N-substituted amide compounds 94 1986
 
MORELLE, JEAN V. (1)
5,066,487 Antisudoral composition comprising dibasic aluminium salts of acylated amino acids 87 1989
 
NORDISK INSULINLABORATORIUM (1)
4,183,849 Therapeutic insulin preparation and a process for the production of a stable insulin preparation with protracted effect 73 1977
 
NURTURE BIOTECH INC. A DE CORP. (1)
5,055,300 Time release protein 99 1989
 
REPLIGEN CORPORATION (1)
4,352,883 Encapsulation of biological material 405 1979
 
SANOFI, A FRENCH CORP. (1)
5,204,099 Cosmetic composition containing amino acid copolymers which is useful as a moisturizer 99 1991
 
THE NISSHIN OIL MILLS, LTD. (1)
4,757,007 Process for preparing hydrolyzed products of soy protein 74 1985
 
THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION (1)
4,608,278 Small particule formation and encapsulation 87 1984
 
TOYO JOZO KABUSHIKI KAISHA (1)
4,873,087 Suppository preparation having excellent absorption property 97 1982
 
YEN, RICHARD C.K. (1)
5,069,936 Manufacturing protein microspheres 154 1989
 
OTHER [CHECK PATENT PROFILE FOR ASSIGNMENT INFORMATION] (1)
5,250,236 Method for producing solid lipid microspheres having a narrow size distribution 82 1991

Patent Citation Ranking

Forward Cites

Patent Info (Count) # Cites Year
 
EMISPHERE TECHNOLOGIES, INC. (66)
5,792,451 Oral drug delivery compositions and methods 84 1994
5,629,020 Modified amino acids for drug delivery 94 1994
5,972,387 Modified hydrolyzed vegetable protein microspheres and methods for preparation and use thereof 17 1994
5,709,861 Compositions for the delivery of antigens 62 1995
5,650,386 Compositions for oral delivery of active agents 85 1995
5,958,457 Compositions for the delivery of antigens 38 1995
6,180,140 Modified amino acids for drug delivery 29 1995
5,766,633 Oral drug delivery compositions and methods 60 1995
5,811,127 Desferrioxamine oral delivery system 54 1996
6,099,856 Active agent transport systems 41 1996
6,100,298 Compounds and compositions for delivering active agents 31 1997
6,001,347 Compounds and compositions for delivering active agents 42 1997
5,989,539 Compounds and compositions for delivering active agents 32 1997
5,965,121 Compounds and compositions for delivering active agents 34 1997
5,955,503 Compounds and compositions for delivering active agents 26 1997
5,866,536 Compounds and compositions for delivering active agents 53 1997
6,313,088 8-[(2-hydroxy-4-methoxy benzoyl) amino]-octanoic acid compositions for delivering active agents 22 1997
6,090,958 Compounds and compositions for delivering active agents 36 1997
6,060,513 Compounds and compositions for delivering active agents 36 1997
5,990,166 Compounds and compositions for delivering active agents 37 1997
5,939,381 Compounds and compositions for delivering active agents 27 1997
5,879,681 Compounds and compositions for delivering active agents 35 1997
5,876,710 Compounds and compositions for delivering active agents 34 1997
5,804,688 Compounds and compositions for delivering active agents 33 1997
6,344,213 Compounds and compositions for delivering active agents 24 1997
6,071,510 Modified amino acids and compositions comprising the same for delivering active agents 38 1997
5,863,944 Compounds and compositions for delivering active agents 38 1997
5,962,710 Method of preparing salicyloylamino acids 27 1997
6,375,983 Microencapsulated fragrances and method for preparation 12 1997
6,221,367 Active agent transport systems 33 1997
6,348,207 Orally deliverable supramolecular complex 17 1997
6,245,359 Active agent transport systems 29 1997
6,071,538 Oral delivery composition comprising supramolecular complex 35 1997
6,100,285 Method of solubilizing itraconazole 25 1997
6,084,112 Method for preparing .omega.-aminoalkanoic acid derivatives from cycloalkanones 19 1997
6,413,550 Proteinoid carriers and methods for preparation and use thereof 8 1998
6,391,303 Methods and compositions for inducing oral tolerance in mammals 11 1999
6,428,780 Compounds and compositions for delivering active agents 14 1999
6,991,798 Compounds and compositions for delivering active agents 0 1999
6,461,545 Method of solubilizing and encapsulating itraconazole 2 2000
6,346,242 Compounds and compositions for delivering active agents 21 2000
6,242,495 Compounds and compositions for delivering active agents 29 2000
7,279,597 Phenyl amine carboxylic acid compounds and compositions for delivering active agents 0 2000
7,129,274 Phenoxy carboxylic acid compounds and compositions for delivering active agents 1 2000
7,151,191 Compounds and compositions for delivering active agents 0 2001
6,642,411 Compounds and compositions for delivering active agents 13 2001
6,440,929 Pulmonary delivery of active agents 13 2001
6,610,329 Compositions for the delivery of antigens 15 2001
6,461,643 Oral drug delivery compositions and methods 17 2001
7,351,741 Compounds and compositions for delivering active agents 2 2001
6,646,162 Compounds and compositions for delivering active agents 14 2001
6,623,731 Compounds and compositions for delivering active agents 12 2001
6,525,020 Compounds and compositions for delivering active agents 12 2001
6,960,355 Compounds and compositions for delivering active agents 0 2001
7,084,279 Oxadiazole compounds and compositions for delivering active agents 2 2002
6,663,887 Compounds and compositions for delivering active agents 11 2002
6,693,208 Compounds and compositions for delivering active agents 14 2002
6,916,489 Active agent transport systems 0 2002
7,208,483 Polymeric delivery agents and delivery agent compounds 0 2003
7,186,414 Compounds and compositions for delivering active agents 0 2005
7,553,872 Compounds and compositions for delivering active agents 0 2006
8,410,309 Phenoxy carboxylic acid compounds and compositions for delivering active agents 0 2006
7,744,910 Compounds and compositions for delivering active agents 0 2006
7,977,506 Compounds and compositions for delivering active agents 0 2006
7,951,971 Phenoxy carboxylic acid compounds and compositions for delivering active agents 0 2008
7,939,494 Method for administering GLP-1 molecules 0 2009
 
SHIRE LLC (6)
6,716,452 Active agent delivery systems and methods for protecting and administering active agents 40 2000
7,018,654 Pharmaceutical composition containing an active agent in an amino acid copolymer structure 2 2001
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
 
MANNKIND CORPORATION (5)
5,976,569 Diketopiperazine-based delivery systems 42 1997
6,395,774 Carbon-substituted diketopiperazine delivery systems 26 2001
6,906,030 Carbon-substituted diketopiperazine delivery systems 2 2003
7,276,534 Carbon-substituted diketopiperazine delivery systems 8 2005
8,133,514 Carbon-substituted diketopiperazine delivery systems 0 2009
 
NOVARTIS AG (5)
7,384,982 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 1 2003
7,659,311 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 4 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
8,207,227 Disodium salts, monohydrates, and ethanol solvates for delivering active agents 0 2011
 
BAXTER INTERNATIONAL INC. (3)
6,090,925 Macromolecular microparticles and methods of production and use 78 1996
5,981,719 Macromolecular microparticles and methods of production and use 68 1998
6,268,053 Macromolecular microparticles and methods of production and use 68 2000
 
VIRGINIA COMMONWEALTH UNIVERSITY (2)
6,627,228 Polymeric delivery agents and delivery agents compounds 20 2001
7,727,558 Polymeric delivery agents and delivery agent compounds 0 2007
 
MHR INSTITUTIONAL PARTNERS IIA LP (1)
7,417,022 Compounds and compositions for delivering active agents 0 2005