Patents by Inventor Nicholas S. Bodor

Nicholas S. Bodor has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • CLADRIBINE FORMULATIONS FOR IMPROVED ORAL AND TRANSMUCOSAL DELIVERY
    Publication number: 20110015145
    Abstract: Provided are compositions of cladribine and cyclodextrin which are especially suited for the oral and buccal administration of cladribine.
    Type: Application
    Filed: September 27, 2010
    Publication date: January 20, 2011
    Applicant: Ares Trading S.A.
    Inventor: Nicholas S. Bodor
  • Enhancement of activity and/or duration of action of selected anti-inflammatory steroids for topical or other local application
    Patent number: 7776846
    Abstract: Methods and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17?-alkoxy-11?-hydroxyandrost-4-en-3-one-17?-carboxylate type and the corresponding ?1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or ?-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: August 17, 2010
    Inventor: Nicholas S. Bodor
  • Transporter-enhanced corticosteroid activity and methods and compositions for treating dry eye
    Patent number: 7691811
    Abstract: Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17?-alkoxycarbonyloxy-11?-hydroxyandrost-4-cn-3-one-17?-carboxylate type and the corresponding ?1,4-compounds are described. The enhancing agents have the formula: wherein Z1 is carbonyl, ?-hydroxymethylene or methylene; R2 is H, —OH or —OCOR3 wherein R3 is C1-5 alkyl; Y is —OH, —SH or —OCOR4 wherein R4 is C1-5 alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated. Ophthalmic administration in the treatment of dry eye is specifically targeted.
    Type: Grant
    Filed: November 20, 2007
    Date of Patent: April 6, 2010
    Inventor: Nicholas S. Bodor
  • Transporter enhanced corticosteroid activity
    Patent number: 7687484
    Abstract: Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17?-alkoxycarbonyloxy-11?-hydroxyandrost-4-en-3-one-17?-carboxylate type and the corresponding ?1,4-compounds are described. The enhancing agents have the formula: wherein Z1 is carbonyl, ?-hydroxymethylene or methylene; R2 is H, —OH or —OCOR3 wherein R3 is C1-C5 alkyl; Y is —OH, —SH or —OCOR4 wherein R4 is C1-C5 alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated.
    Type: Grant
    Filed: May 22, 2007
    Date of Patent: March 30, 2010
    Inventor: Nicholas S. Bodor
  • SOFT ANTICHOLINERGIC ESTERS
    Publication number: 20090263341
    Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
    Type: Application
    Filed: June 30, 2009
    Publication date: October 22, 2009
    Inventor: Nicholas S. Bodor
  • SOFT ANTICHOLINERGIC ZWITTERIONS
    Publication number: 20090257969
    Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
    Type: Application
    Filed: April 6, 2009
    Publication date: October 15, 2009
    Inventor: Nicholas S. Bodor
  • ENHANCEMENT OF ACTIVITY AND/OR DURATION OF ACTION OF SOFT ANTI-INFLAMMATORY STEROIDS FOR TOPICAL OR OTHER LOCAL APPLICATION
    Publication number: 20090239833
    Abstract: Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17?-alkoxycarbonyloxy-11?-hydroxyandrost-4-en-3-one-17?-carboxylate type and the corresponding ?1,4-compounds are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or ?-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.
    Type: Application
    Filed: June 9, 2009
    Publication date: September 24, 2009
    Inventor: Nicholas S. Bodor
  • Soft anticholinergic esters
    Patent number: 7576210
    Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
    Type: Grant
    Filed: June 12, 2008
    Date of Patent: August 18, 2009
    Inventor: Nicholas S. Bodor
  • Enhancement of activity and/or duration of action of soft anti-inflammatory steroids for topical or other local application
    Patent number: 7560448
    Abstract: Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17?-alkoxycarbonyloxy-11?-hydroxyandrost-4-en-3-one-17?-carboxylate type and the corresponding ?1,4-compounds are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or ?-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.
    Type: Grant
    Filed: June 17, 2004
    Date of Patent: July 14, 2009
    Inventor: Nicholas S. Bodor
  • Soft anticholinergic zwitterions
    Patent number: 7538219
    Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
    Type: Grant
    Filed: June 12, 2008
    Date of Patent: May 26, 2009
    Inventor: Nicholas S. Bodor
  • SOFT ANTICHOLINERGIC ESTERS
    Publication number: 20090075954
    Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
    Type: Application
    Filed: June 12, 2008
    Publication date: March 19, 2009
    Inventor: Nicholas S. BODOR
  • ENHANCEMENT OF ACTIVITY AND/OR DURATION OF ACTION OF SELECTED ANTI-INFLAMMATORY STEROIDS FOR TOPICAL OR OTHER LOCAL APPLICATION
    Publication number: 20080261930
    Abstract: Methods and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17?-alkoxy-11?-hydroxyandrost-4-en-3-one-17?-carboxylate type and the corresponding ?1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or ?-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.
    Type: Application
    Filed: June 26, 2008
    Publication date: October 23, 2008
    Inventor: Nicholas S. Bodor
  • SOFT ANTICHOLINERGIC ZWITTERIONS
    Publication number: 20080242651
    Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
    Type: Application
    Filed: June 12, 2008
    Publication date: October 2, 2008
    Inventor: Nicholas S. BODOR
  • Enhancement of activity and/or duration of action of selected anti-inflammatory steroids for topical or other local application
    Patent number: 7419971
    Abstract: Methods and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17?-alkoxy-11?-hydroxyandrost-4-en-3-one-17?-carboxylate type and the corresponding ?1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or ?-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.
    Type: Grant
    Filed: June 17, 2004
    Date of Patent: September 2, 2008
    Inventor: Nicholas S. Bodor
  • Soft anticholinergic zwitterions
    Patent number: 7417147
    Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
    Type: Grant
    Filed: November 13, 2006
    Date of Patent: August 26, 2008
    Inventor: Nicholas S. Bodor
  • TRANSPORTER-ENHANCED CORTICOSTEROID ACTIVITY AND METHODS AND COMPOSITIONS FOR TREATING DRY EYE
    Publication number: 20080194468
    Abstract: Methods and compositions for enhancing the activity and/or duration of action of loteprednol etabonate and other soft anti-inflammatory steroids of the haloalkyl 17?-alkoxycarbonyloxy-11?-hydroxyandrost-4-cn-3-one-17?-carboxylate type and the corresponding ?1,4-compounds are described. The enhancing agents have the formula: wherein Z1 is carbonyl, ?-hydroxymethylene or methylene; R2 is H, —OH or —OCOR3 wherein R3 is C1-5 alkyl; Y is —OH, —SH or —OCOR4 wherein R4 is C1-5 alkyl, cyclopentylethyl or diethylaminoethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated. Ophthalmic administration in the treatment of dry eye is specifically targeted.
    Type: Application
    Filed: November 20, 2007
    Publication date: August 14, 2008
    Inventor: Nicholas S. Bodor
  • Soft anticholinergic esters
    Patent number: 7399861
    Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.
    Type: Grant
    Filed: November 13, 2006
    Date of Patent: July 15, 2008
    Inventor: Nicholas S. Bodor
  • Inactive metabolite approach to soft drug design
    Patent number: 6610675
    Abstract: The invention provides novel soft steroidal anti-inflammatory agents, pharmaceutical compositions containing said agents, and methods of administering same to mammals in the treatment of inflammation. Preferred compounds of the invention include haloalkyl 17&agr;-alkoxycarbonyloxy-11&bgr;-hydroxyandrost-4-en-3-one-17&bgr;-carboxylates and the corresponding &Dgr;1,4 compounds, optionally bearing 6&agr;- and/or 9&agr;-fluorine and 16&agr;- or 16&bgr;-methyl substituents. Especially preferred compounds include haloalkyl 17&agr;-alkoxycarbonyloxy-9&agr;-fluoro-11&bgr;-hydroxy-16-methylandrosta-1,4-dien-3-one-17&bgr;-carboxylates.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: August 26, 2003
    Inventor: Nicholas S. Bodor
  • Androstene derivatives
    Patent number: 5981517
    Abstract: The invention provides new androstene derivatives having anti-inflammatory activity, pharmaceutical compositions containing them, and methods of administering them to warm-blooded animals in the treatment of inflammation. The active compounds are alkyl 17.alpha.-dichloroacetoxy-11.beta.-hydroxyandrosta-1,4-dien-3-one-17.beta. -carboxylates and related androstenes.
    Type: Grant
    Filed: April 24, 1997
    Date of Patent: November 9, 1999
    Assignee: Soft Drugs, Inc.
    Inventor: Nicholas S. Bodor
  • Redox amino acids and peptides containing them
    Patent number: 5639885
    Abstract: The invention provides novel amino acids and peptides containing them which comprise a dihydropyridine.revreaction.pyridinium salt-type redox system and which provide site-specific and sustained delivery of pharmacologically active peptides to the brain. These new amino acids contain a redox system appended directly or via an alkylene bridge to the carbon atom adjacent to the carboxyl carbon and may be incorporated into a peptide chain at a variety of positions, including non-terminal positions.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: June 17, 1997
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor