Patents by Inventor William E. Bay
William E. Bay 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).
-
Publication number: 20180338923Abstract: Oral insulin formulations and processes for preparing oral insulin formulations are provided.Type: ApplicationFiled: January 19, 2018Publication date: November 29, 2018Inventors: Halina LEVCHIK, Moses OYEWUMI, Shingai MAJURU, William E. BAY, Jun LIAO, Puchun LIU, Steven DINH, Nikhil DHOOT
-
Publication number: 20150190344Abstract: Oral insulin formulations and processes for preparing oral insulin formulations are provided.Type: ApplicationFiled: January 5, 2015Publication date: July 9, 2015Inventors: Halina LEVCHIK, Moses Oyewumi, Shingai Majuru, William E. Bay, Jun Liao, Puchun Liu, Steven Dinh, Nikhil Dhoot
-
Publication number: 20120264834Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.Type: ApplicationFiled: May 25, 2012Publication date: October 18, 2012Applicants: NOVARTIS AG, Emisphere Technologies, Inc.Inventors: William E. BAY, Rajesh K. AGARWAL, Kiran CHAUDHARY, Shingai MAJURU, Michael M. GOLDBERG, JoAnne P. CORVINO, Moise AZRIA, Joseph M. AULT, Simon D. BATEMAN, Subash PATEL, Joseph SIKORA, Rebecca F. YANG, Joseph L. ZIELINSKI
-
Patent number: 8207227Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: GrantFiled: March 22, 2011Date of Patent: June 26, 2012Assignees: Emisphere Technologies, Inc., Novartis AGInventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Michael M. Goldberg, Joanne P. Corvino, Shingai Majuru, Moise Azria, Joseph Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph Zielinski
-
Publication number: 20110251125Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: ApplicationFiled: March 22, 2011Publication date: October 13, 2011Applicants: Novartis AG, Emisphere Technologies, Inc.Inventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, Joanne P. Corvino, Moise Azria, Joseph M. Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph L. Zielinski
-
Publication number: 20100099621Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: ApplicationFiled: December 18, 2009Publication date: April 22, 2010Applicants: EMISPHERE TECHNOLOGIES, INC., NOVARTIS AGInventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Corvino, Moise Azria, Joseph M. Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph L. Zielinski
-
Publication number: 20080269134Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: ApplicationFiled: April 29, 2008Publication date: October 30, 2008Applicants: Emisphere Technologies, Inc., Novartis AGInventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Corvino, Moise Azria, Joseph M. Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph L. Zielinski
-
Patent number: 7384982Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein R1, R2, R3, and R4 are indepedently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substitued or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above.Type: GrantFiled: July 7, 2003Date of Patent: June 10, 2008Assignees: Emisphere Technologies, Inc., Novartis AGInventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Russo, Mosise Azria, Joseph M. Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph L Zielinski
-
Patent number: 7351741Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provide as well.Type: GrantFiled: June 29, 2001Date of Patent: April 1, 2008Assignee: Emisphere Technologies, Inc.Inventors: John J. Weidner, Bruce F. Variano, Shingai Majuru, Satej Bhandarkar, William E. Bay, Lynn Sheilds
-
Patent number: 7262325Abstract: The present invention provides a fast, high yield method for preparing salicylamide intermediates. The method comprises reacting a C4 or higher alkyl ester of salicylic acid or derivative thereof with at least one amine selected from the group consisting of monoalkylamines, dialkylamines, ammonia, and any combination of any of the foregoing in alcohol to yield the salicylamide. The C4 or higher alkyl ester of salicylic acid or a derivative thereof is preferably prepared by reacting salicylic acid or a derivative thereof with a C4 or higher alcohol in presence of at least one of sulfuric acid, a sulfonic acid, and a mineral acid. This process for preparing salicylamide intermediates from salicylic acid or derivative thereof generally has a cycle time of about 2 days, and yields about 95% of a 99% pure material. In comparison, when a C3 or lower alkyl ester is used in lieu of the C4 or higher alkyl ester, the process generally has a cycle time of 7–9 days and yields about 60% of a 95% pure material.Type: GrantFiled: June 4, 2001Date of Patent: August 28, 2007Assignee: Emisphere Technologies, Inc.Inventors: William E. Bay, JoAnne P. Corvino
-
Patent number: 7169776Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.Type: GrantFiled: January 19, 2005Date of Patent: January 30, 2007Assignee: Emisphere Technologies, Inc.Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
-
Patent number: 6900344Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.Type: GrantFiled: March 21, 2001Date of Patent: May 31, 2005Assignee: Emisphere Technologies, Inc.Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
-
Publication number: 20040106825Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water.Type: ApplicationFiled: July 7, 2003Publication date: June 3, 2004Applicant: Emisphere Technologies, Inc.Inventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Russo
-
Publication number: 20040048777Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provide as well.Type: ApplicationFiled: June 25, 2003Publication date: March 11, 2004Inventors: John J Weidner, Bruce F Variano, Shingai Majuru, Satej Bhandarkar, William E Bay, Lynn Sheilds
-
Publication number: 20030216593Abstract: The present invention provides a fast, high yield method for preparing salicylamide intermediates. The method comprises reacting a C4 or higher alkyl ester of salicylic acid or derivative thereof with at least one amine selected from the group consisting of monoalkylamines, dialkylamines, ammonia, and any combination of any of the foregoing in alcohol to yield the sali-cylamide. The C4 or higher alkyl ester of salicylic acid or a derivative thereof is preferably prepared by reacting salicylic acid or a derivative thereof with a C4 or higher alcohol in presence of at least one of sulfuric acid, a sulfonic acid, and a mineral acid. This process for preparing salicylamide intermediates from salicylic acid or derivative thereof generally has a cycle time of about 2 days, and yields about 95% of a 99% pure material. In comparison, when a C3 or lower alkyl ester is used in lieu of the C4 or higher alkyl ester, the process generally has a cycle time of 7-9 days and yields about 60% of a 95% pure material.Type: ApplicationFiled: December 2, 2002Publication date: November 20, 2003Inventors: William E. Bay, JoAnne P. Corvino
-
Publication number: 20030096992Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.Type: ApplicationFiled: September 20, 2002Publication date: May 22, 2003Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
-
Patent number: 6399798Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide (hereinafter referred to as a “protected/activated salicylamide”). The method comprises the steps of (a) alkylating the protected/activated salicylamide with an alkylating agent to form a protected/activated alkylated salicylamide, and (b) deprotecting and deactivating the protected/activated alkylated salicylamide, simultaneously or in any order, to form the alkylated salicylamide. The alkylated salicylamides prepared by this method are suitable for use in compositions for delivering active agents via oral or other routes of administration to animals.Type: GrantFiled: August 3, 2001Date of Patent: June 4, 2002Assignee: Emisphere Technologies, Inc.Inventors: David Gschneidner, Joseph N. Bernadino, William E. Bay
-
Publication number: 20020065255Abstract: The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water.Type: ApplicationFiled: September 24, 2001Publication date: May 30, 2002Applicant: EMISPHERE TECHNOLOGIES, INC.Inventors: William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Russo
-
Publication number: 20020013497Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide (hereinafter referred to as a “protected/activated salicylamide”). The method comprises the steps of (a) alkylating the protected/activated salicylamide with an alkylating agent to form a protected/activated alkylated salicylamide, and (b) deprotecting and deactivating the protected/activated alkylated salicylamide, simultaneously or in any order, to form the alkylated salicylamide. The alkylated salicylamides prepared by this method are suitable for use in compositions for delivering active agents via oral or other routes of administration to animals.Type: ApplicationFiled: August 3, 2001Publication date: January 31, 2002Applicant: EMISPHERE TECHNOLOGIES, INC.Inventors: David Gschneidner, Joseph N. Bernadino, William E. Bay
-
Patent number: 5556971Abstract: A process is provided for preparing isocyanate and isocyanate-based 1,3,5-triazine derivatives by the direct phosgenation of (at least tris-unsubstituted amino)-1,3,5-triazines.Type: GrantFiled: May 6, 1994Date of Patent: September 17, 1996Assignee: Cytec Technology Corp.Inventors: William E. Bay, William F. Jacobs, III, David Gschneidner, Ram B. Gupta