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 aryl ketone compounds and compositions containing them which facilitate the delivery of active agents. The aryl ketone compounds have the formula or a salt thereof, where n=1 to 9, and R1 to R5 are independently hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, C2 to C4 alkenyl, halogen, hydroxyl, —NH—C(O)—CH3, or —O—C6H5.
Type:
Grant
Filed:
March 10, 2008
Date of Patent:
May 19, 2015
Assignee:
EMISPHERE TECHNOLOGIES, INC.
Inventors:
Parshuram Rath, Maria Isabel Gomez-Orellana
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
Abstract: The present invention provides dialkyl ether compounds and pharmaceutically acceptable salts thereof, compositions containing the same and one or more active agents, and methods of administering active agents with the same.
Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
Type:
Grant
Filed:
June 10, 2009
Date of Patent:
April 1, 2014
Assignee:
Emisphere Technologies, Inc.
Inventors:
Donald J. Sarubbi, Eugene N. Barantsevitch
Abstract: 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:
Grant
Filed:
May 25, 2012
Date of Patent:
February 25, 2014
Assignees:
Emisphere Technologies, Inc., Novartis AG
Inventors:
William Elliott Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Corvino, Moise Azria, Joseph Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph Zielinski
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:
Application
Filed:
August 20, 2013
Publication date:
January 30, 2014
Applicant:
Emisphere Technologies, Inc.
Inventors:
Robert Jason Herr, Louis Nickolaus Jungheim, John McNeill McGill, Kenneth Jeff Thrasher, Muralikrishna Valluri
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 invention relates to formulations that demonstrate the feasibility of oral absorption comprising glucose-like peptide-1 compounds and specified delivery agents, and to methods of stimulating GLP-1 receptor in a subject in need of such stimulation, by administration of the formulation of the present invention.
Type:
Application
Filed:
July 16, 2013
Publication date:
January 2, 2014
Applicant:
Emisphere Technologies, Inc.
Inventors:
Mohammed Amin KHAN, Bryan Edward Jones, John Mcneill McGill