Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]- amino) caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid.
Type:
Application
Filed:
November 23, 2020
Publication date:
March 11, 2021
Applicant:
Emisphere Technologies, Inc.
Inventors:
William Elliot Bay, Joseph Norman Bernadino, George Frederick Klein, Yi Ren, Pingsheng Zhang
Abstract: Disclosed are improved methods for the synthesis of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid. Certain compounds have been found useful for preventing the formation of a colored impurity when included in an ester hydrolysis reaction. Conducting ester hydrolysis in anaerobic conditions has also been found to minimize the formation of the color impurity. Also disclosed are improved methods for synthesizing the sodium salt of N-(8-[2-hydroxybenzoyl]-amino) caprylic acid.
Type:
Grant
Filed:
August 30, 2007
Date of Patent:
December 29, 2020
Assignee:
Emisphere Technologies, Inc.
Inventors:
William Elliot Bay, Joseph Norman Bernadino, George Frederick Klein, Yi Ren, Pingsheng Zhang
Abstract: The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.
Abstract: The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.
Abstract: The present invention provides phenylalkylcarboxylic acid compounds and compositions containing such compounds which facilitate the delivery of biologically active agents.
Abstract: The present invention relates to particular phenoxy alkyl diethanolamine and diisopropanolamine compounds for delivering biologically active agents to a target. These compounds are well suited for forming non-covalent mixtures with active agents for oral, intracolonic, pulmonary, and other routes of administration to animals.
Type:
Grant
Filed:
August 22, 2013
Date of Patent:
October 4, 2016
Assignee:
Emisphere Technologies, Inc.
Inventors:
Gabriela Mustata, Dahua Pan, David Gschneidner
Abstract: Methods of normalizing vitamin B12 levels in patients with low vitamin B12 and methods of normalizing intersubject variability in the treatment of such patients are described. Methods of reducing MMA and/or homocysteine levels, and pharmaceutical compositions useful to effect such changes are also described.
Abstract: The present invention relates to particular phenoxy alkyl diethanolamine and diisopropanolamine compounds for delivering biologically active agents to a target. These compounds are well suited for forming non-covalent mixtures with active agents for oral, intracolonic, pulmonary, and other routes of administration to animals.
Type:
Application
Filed:
August 22, 2013
Publication date:
November 12, 2015
Applicant:
Emisphere Technologies, Inc.
Inventors:
Gabriela Mustata, Dahua Pan, David Gschneidner
Abstract: The present invention provides a composition (e.g., a pharmaceutical composition) comprising at least one delivery agent compound and glucagon. Preferably, the composition includes a therapeutically effective amount of glucagon and the delivery agent compound. The composition of the present invention facilitates the delivery of glucagon and increases its bioavailability compared to administration without the delivery agent compound.
Type:
Grant
Filed:
July 17, 2006
Date of Patent:
March 10, 2015
Assignee:
Emisphere Technologies, Inc.
Inventors:
Nai Fang Wang, Puchun Liu, Steven Dinh, Michael M. Goldberg, Ehud Arbit
Abstract: Methods for treating impaired glucose tolerance and early and late stage diabetes in mammals, for prophylactically sparing ?-cell function, aiding in preventing ?-cell death, preventing the onset of overt diabetes in a mammal with type 2 diabetes, treating the current level of glycemic control dysfunction of a mammal with impaired glucose tolerance or diabetes, comprising orally administering insulin and a delivery agent that facilitates insulin absorption from the gastrointestinal tract at the time of or shortly before mealtime, e.g., within about 10 minutes prior to ingestion of a meal, on a chronic basis. The methods also comprise, in addition to administering a rapid-acting insulin to provide a first insulin peak, administering a slow acting insulin to provide a second insulin peak occurring at a later time but of a longer duration.
Type:
Grant
Filed:
March 21, 2014
Date of Patent:
February 24, 2015
Assignee:
Emisphere Technologies, Inc.
Inventors:
Ehud Arbit, Michael Goldberg, Shingai Majuru
Abstract: The present invention relates to an acyclovir formulation having improved bioavailability resulting in better efficacy and/or requiring less frequent administration.
Type:
Grant
Filed:
March 15, 2013
Date of Patent:
February 10, 2015
Assignee:
Emisphere Technologies, Inc.
Inventors:
Amy C. Adams, Brahma N. Singh, Nikhil Dhoot, Shingai Majuru
Abstract: The present invention provides delivery agent compounds, compositions containing delivery agent compounds and an active agent and methods for delivering active agents, such as biologically or chemically active agents.
Type:
Grant
Filed:
August 29, 2007
Date of Patent:
November 25, 2014
Assignee:
Emisphere Technologies Inc
Inventors:
Jun Liao, Pingwah Tang, David Gschneidner, Jonathan Maeyer
Abstract: Methods for treating impaired glucose tolerance and early and late stage diabetes in mammals, for prophylactically sparing ?-cell function, aiding in preventing ?-cell death, preventing the onset of overt diabetes in a mammal with type 2 diabetes, treating the current level of glycemic control dysfunction of a mammal with impaired glucose tolerance or diabetes, comprising orally administering insulin and a delivery agent that facilitates insulin absorption from the gastrointestinal tract at the time of or shortly before mealtime, e.g., within about 10 minutes prior to ingestion of a meal, on a chronic basis. The methods also comprise, in addition to administering a rapid-acting insulin to provide a first insulin peak, administering a slow acting insulin to provide a second insulin peak occurring at a later time but of a longer duration.
Type:
Application
Filed:
March 21, 2014
Publication date:
July 24, 2014
Applicant:
Emisphere Technologies, Inc.
Inventors:
Ehud ARBIT, Michael GOLDBERG, Shingai MAJURU
Abstract: The present invention provides pharmaceutical compositions comprising of at least one delivery agent and GLP-1. These pharmaceutical compositions facilitate the oral delivery of GLP-1, providing improved (e.g. increased) bioavailability of GLP-1 compared to administration of GLP-1 without a delivery agent.
Abstract: The present invention provides a topical composition comprising (a) at least one delivery agent compound and (b) a acyclovir compound. Methods of treatment, and methods of preparing the topical composition are also provided.
Abstract: The present invention relates to crystalline polymorphic forms of monosodium N-[8-(2-hydroxybenzoyl)amino]caprylate (“SNAC”), including two hydrates, a methanol solvate, and an ethanol solvate, of SNAC. More specifically, the present invention provide six polymorphic forms of SNAC (hereafter referred to as Forms I-VI). The present invention also provides an amorphous form of SNAC.
Abstract: The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide.
Type:
Grant
Filed:
August 20, 2013
Date of Patent:
July 1, 2014
Assignee:
Emisphere Technologies, Inc.
Inventors:
Robert J. Herr, Louis N. Jungheim, John M. McGill, Kenneth J. Thrasher, Muralikrishna Valluri
Abstract: Solid pharmaceutical compositions and methods of their use suitable for the oral delivery of pharmacologically active agents, e.g. peptides, comprising a therapeutically-effective amount of a pharmacologically active agent; a crospovidone or povidone; and a delivery agent for said pharmacologically active agent are disclosed. The compositions utilize micronized forms of the delivery agent which provides enhanced bioavailability of pharmacologically active agents, particularly calcitonin.
Type:
Grant
Filed:
April 15, 2013
Date of Patent:
June 10, 2014
Assignees:
Novartis AG, Emisphere Technologies, Inc.
Inventors:
Shoufeng Li, Anasuya Ashok Ghosh, Simon D. Bateman, Moise Azria, Alan E. Royce
Abstract: Methods for treating impaired glucose tolerance and early and late stage diabetes in mammals, for prophylactically sparing ?-cell function, aiding in preventing ?-cell death, preventing the onset of overt diabetes in a mammal with type 2 diabetes, treating the current level of glycemic control dysfunction of a mammal with impaired glucose tolerance or diabetes, comprising orally administering insulin and a delivery agent that facilitates insulin absorption from the gastrointestinal tract at the time of or shortly before mealtime, e.g., within about 10 minutes prior to ingestion of a meal, on a chronic basis. The methods also comprise, in addition to administering a rapid-acting insulin to provide a first insulin peak, administering a slow acting insulin to provide a second insulin peak occurring at a later time but of a longer duration.
Type:
Grant
Filed:
June 16, 2009
Date of Patent:
May 20, 2014
Assignee:
Emisphere Technologies, Inc.
Inventors:
Ehud Arbit, Michael Goldberg, Shingai Majuru