Patents by Inventor Benjamin R. Yerxa
Benjamin R. Yerxa 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).
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Publication number: 20130344139Abstract: A method and preparation for reducing dry eye symptoms and promoting tear secretion in a subject in need of such treatment is disclosed. The method is useful in treating dry eye diseases. The method is also useful in reducing contact lens intolerance in the eyes. The method comprises administering to the eyes of a subject in need thereof a non-drying antihistamine compound, such as epinastine hydrochloride, in an amount effective to reduce dry eye symptoms and stimulate tear fluid secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the compound include topical administration via a liquid, gel, cream, or as part of a contact lens or a continuous or selective release device; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form, injectable, intra-operative instillation or suppository form.Type: ApplicationFiled: August 29, 2013Publication date: December 26, 2013Inventors: Benjamin R. Yerxa, Jason L. Vittitow, John C. Ice, Ramesh Krisnamoorthy
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Patent number: 8097600Abstract: A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5?-triphosphate (UTP), dinucleotides, cytidine 5?-triphosphate (CTP), adenosine 5?-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: GrantFiled: June 28, 2010Date of Patent: January 17, 2012Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
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Patent number: 8008274Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The present invention also provides a method of treating cystic fibrosis. The present invention also provides a method of treating sinusitis. The present invention further provides P1-(2?-deoxycytidine 5?-)P4-(uridine 5?-)tetraphosphate, tetra-(alkali metal) salts such as tetrasodium, tetralithium, tetrapotassium, and mixed (tetra-alkali metal) salts.Type: GrantFiled: May 6, 2009Date of Patent: August 30, 2011Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Ward M. Peterson, Janet L. Rideout, William Pendergast
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Patent number: 7939510Abstract: The present invention are directed to P1,P4-di(uridine 5?-)tetraphosphate, tetra-alkali metal salts such as tetrasodium, tetralithium, tetrapotassium, and mixed tetra-alkali metal cations thereof. The tetra alkali metal salts of P1,P4-di(uridine 5?-)tetraphosphate are water-soluble, nontoxic, and easy to handle during manufacture. These tetra-monovalent alkali metal salts are more resistant to hydrolysis than the mono-, di-, or tri-acid salts, therefore, they provide an improved stability and a longer shelf life for storage. The present invention also provides methods for the synthesis of P1,P4-di(uridine 5?-)tetraphosphate, and its pharmaceutically acceptably acceptable salts thereof, and demonstrates the applicability to the production of large quantities. The methods substantially reduce the time required to synthesize diuridine tetraphosphate, for example, to three days or less.Type: GrantFiled: April 27, 2009Date of Patent: May 10, 2011Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Edward G. Brown
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Publication number: 20100330164Abstract: A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5?-triphosphate (UTP), dinucleotides, cytidine 5?-triphosphate (CTP), adenosine 5?-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: ApplicationFiled: June 28, 2010Publication date: December 30, 2010Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
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Patent number: 7759322Abstract: A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5?-triphosphate (UTP), dinucleotides, cytidine 5?-triphosphate (CTP), adenosine 5?-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: GrantFiled: June 20, 2007Date of Patent: July 20, 2010Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
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Publication number: 20090326050Abstract: The present invention are directed to P1,P4-di(uridine 5?-)tetraphosphate, tetra-alkali metal salts such as tetrasodium, tetralithium, tetrapotassium, and mixed tetra-alkali metal cations thereof. The tetra alkali metal salts of P1,P4-di(uridine 5?-)tetraphosphate are water-soluble, nontoxic, and easy to handle during manufacture. These tetra-monovalent alkali metal salts are more resistant to hydrolysis than the mono-, di-, or tri-acid salts, therefore, they provide an improved stability and a longer shelf life for storage. The present invention also provides methods for the synthesis of P1,P4-di(uridine 5?-)tetraphosphate, and its pharmaceutically acceptably acceptable salts thereof, and demonstrates the applicability to the production of large quantities. The methods substantially reduce the time required to synthesize diuridine tetraphosphate, for example, to three days or less.Type: ApplicationFiled: April 27, 2009Publication date: December 31, 2009Inventors: Benjamin R. Yerxa, Edward G. Brown
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Publication number: 20090306010Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The present invention also provides a method of treating cystic fibrosis. The present invention also provides a method of treating sinusitis. The present invention further provides P1-(2?-deoxycytidine 5?-)P4-(uridine 5?-)tetraphosphate, tetra-(alkali metal) salts such as tetrasodium, tetralithium, tetrapotassium, and mixed (tetra-alkali metal) salts.Type: ApplicationFiled: May 6, 2009Publication date: December 10, 2009Inventors: Benjamin R. Yerxa, Ward M. Peterson, Janet L. Rideout, William Pendergast
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Patent number: 7612047Abstract: The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.Type: GrantFiled: September 10, 2008Date of Patent: November 3, 2009Assignee: Inspire Pharmaceuticals, Inc.Inventors: James G. Douglass, III, Benjamin R. Yerxa, Sammy R. Shaver, Ward M. Peterson, Edward G. Brown, Christopher S. Crean, José L. Boyer
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Patent number: 7531525Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The present invention also provides a method of treating cystic fibrosis. The present invention further provides P1-(2?-deoxycytidine 5?-)P4-(uridine 5?-) tetraphosphate, tetra-(alkali metal) salts such as tetrasodium, tetralithium, tetrapotassium, and mixed (tetra-alkali metal) salts. The present further provides a pharmaceutical formulation comprising a P1-(2?-deoxycytidine 5?-)P4-(uridine 5?-) tetraphosphate, tetra-(alkali metal) salt, in a pharmaceutically acceptable carrier.Type: GrantFiled: March 23, 2007Date of Patent: May 12, 2009Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Ward M. Peterson, Janet L. Rideout, William Pendergast
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Patent number: 7528119Abstract: The present invention are directed to P1,P4-di(uridine 5?-)tetraphosphate, tetra-alkali metal salts such as tetrasodium, tetralithium, tetrapotassium, and mixed tetra-alkali metal cations thereof. The tetra alkali metal salts of P1,P4-di(uridine 5?-)tetraphosphate are water-soluble, nontoxic, and easy to handle during manufacture. These tetra-monovalent alkali metal salts are more resistant to hydrolysis than the mono-, di-, or tri-acid salts, therefore, they provide an improved stability and a longer shelf life for storage. The present invention also provides methods for the synthesis of P1,P4-di(uridine 5?-)tetraphosphate, and its pharmaceutically acceptably acceptable salts thereof, and demonstrates the applicability to the production of large quantities. The methods substantially reduce the time required to synthesize diuridine tetraphosphate, for example, to three days or less.Type: GrantFiled: July 14, 2006Date of Patent: May 5, 2009Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Edward G. Brown
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Publication number: 20090076256Abstract: The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Inventors: James G. Douglass, III, Benjamin R. Yerxa, Sammy R. Shaver, Ward M. Peterson, Edward G. Brown, Christopher S. Crean, Jose L. Boyer
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Patent number: 7435724Abstract: The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.Type: GrantFiled: November 21, 2005Date of Patent: October 14, 2008Assignee: Inspire Pharmaceutical, Inc.Inventors: James G. Douglass, III, Benjamin R. Yerxa, Sammy R. Shaver, Ward M. Peterson, Edward G. Brown, Christopher S. Crean, José L. Boyer
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Patent number: 7432252Abstract: The present invention provides a method of stimulating cervical and vaginal secretions in a mammal by treatment with P2Y2 and/or P2Y4 purinergic receptor agonists. Treatment of vaginal dryness associated with menopause, chemotherapy, and various disease states as well as the treatment of vulvar pain is discussed. Suitable agonists such as UTP, CTP, ATP, dinucleotides and analogs thereof are disclosed.Type: GrantFiled: March 20, 2000Date of Patent: October 7, 2008Assignee: Inspire Pharmaceuticals, Inc.Inventors: William Pendergast, Sammy Ray Shaver, David J. Drutz, Janet L. Rideout, Benjamin R. Yerxa
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Publication number: 20080214490Abstract: The present invention provides a method of stimulating cervical and vaginal secretions in a mammal by treatment with P2Y2 and/or P2Y4 purinergic receptor agonists. Treatment of vaginal dryness associated with menopause, chemotherapy, and various disease states as well as the treatment of vulvar pain is discussed. Suitable agonists such as UTP, CTP, ATP, dinucleotides and analogs thereof are disclosed.Type: ApplicationFiled: March 6, 2008Publication date: September 4, 2008Applicant: Inspire Pharmaceuticals, Inc.Inventors: William Pendergast, Sammy Ray Shaver, David J. Drutz, Janet L. Rideout, Benjamin R. Yerxa
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Patent number: 7256183Abstract: The present invention provides a method of preventing or treating an inflammatory disease, including but not limited to, sinusitis, rhinitis, conjunctivitis, asthma, dermatitis, inflammatory bowel disease, inflammatory collagen vascular diseases, glomerulonephritis, inflammatory skin diseases, and sarcoidosis. The method comprises administrating to a subject a pharmaceutical formulation comprising a nucleotide receptor agonist, such as nucleoside diphosphate, nucleoside triphosphate, or dinucleoside polyphosphate, according to general formula Ia, Ib, IIa, IIb, or III. Preferred indications of the present invention are perennial allergic rhinitis, seasonal allergic rhinitis, infectious allergic rhinitis, and allergic conjunctivitis.Type: GrantFiled: November 6, 2002Date of Patent: August 14, 2007Assignee: Inspire Pharmaceuticals, Inc.Inventors: Ward M. Peterson, Benjamin R. Yerxa
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Patent number: 7247623Abstract: A method and preparation for reducing dry eye symptoms and promoting tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the eyes of the subject a non-drying antihistamine compound, such as epinastine hydrochloride, in an amount effective to reduce dry eye symptoms and stimulate tear fluid secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the compound include topical administration via a liquid, gel, cream, or as part of a contact lens or a continuous or selective release device; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: GrantFiled: August 10, 2006Date of Patent: July 24, 2007Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Jason L. Vittitow, John C. Ice, Jr.
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Patent number: 7235535Abstract: A method and preparation for enhancing drainage of lacrimal system in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5?-triphosphate (UTP), dinucleotides, cytidine 5?-triphosphate (CTP), adenosine 5?-triphosphate (ATP), or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion and enhance drainage of the lacrimal system. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: GrantFiled: April 25, 2005Date of Patent: June 26, 2007Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
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Patent number: 7223744Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The pharmaceutical formulation useful in this invention comprises a P2Y receptor agonist with enhanced resistance to extracellular hydrolysis, such as dinucleoside polyphosphate compounds, or hydrolysis-resistant mononucleoside triphosphate salts. The present invention also provides P1-(2?-deoxycytidine 5?-)P4-(uridine 5?-)tetraphosphate, tetra-(alkali metal) salts such as tetrasodium, tetralithium, tetrapotassium, and mixed (tetra-alkali metal) salts.Type: GrantFiled: October 7, 2004Date of Patent: May 29, 2007Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Ward M. Peterson, Janet L. Rideout, William Pendergast
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Patent number: 7132408Abstract: This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y12 receptor antagonist compound, wherein said amount is effective to bind the P2Y12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y12 receptor antagonist compounds useful for this invention include mononucleoside 5?-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates of general Formula I, or salts thereof. The present invention also provides novel compounds of mononucleoside 5?-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates. The present invention further provides pharmaceutical formulations comprising mononucleoside 5?-monophosphates, mononucleoside polyphosphates, or dinucleoside polyphosphates.Type: GrantFiled: March 30, 2004Date of Patent: November 7, 2006Assignees: Inspire Pharmaceuticals, Inc., University of North CarolinaInventors: José L. Boyer, James G. Douglass, III, Sammy R. Shaver, Krzysztof Bednarski, Benjamin R. Yerxa, Gillian M. Olins