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 provides phenylalkylcarboxylic acid compounds and compositions containing such compounds which facilitate the delivery of biologically active agents.
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 provides a topical composition comprising (a) at least one delivery agent compound and (b) a cromoglycic acid compound. Methods of treatment, and methods of preparing the topical composition are also provided.
Type:
Grant
Filed:
May 19, 2005
Date of Patent:
November 22, 2016
Assignee:
EMISPHERE TECHNOLOGIES, INC.
Inventors:
Puchun Liu, Steven Dinh, Ehud Arbit, Michael M. Goldberg
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 iron levels, treating iron deficiency and disorders related thereto, such as anemia, as described. Pharmaceutical compositions effective for such treatments are also described.
Type:
Grant
Filed:
June 9, 2011
Date of Patent:
August 2, 2016
Assignee:
EMISPHERE TECHNOLOGIES, INC.
Inventors:
Gary M. Riley, Parshuram Rath, Michael Novinski
Abstract: The present invention provides a composition (e.g., a pharmaceutical composition) comprising at least one delivery agent compound and at least one of peptide YY (PYY) and a PYY agonist. Preferably, the composition includes a therapeutically effective amount of peptide YY or the PYY agonist and the delivery agent compound. The composition of the present invention facilitates the delivery of PYY, a PYY agonist, or a mixture thereof and increases its bioavailability compared to administration without the delivery agent compound. PPY and PYY agonists possess activity as agents to reduce nutrient availability, including reduction of food intake.
Type:
Grant
Filed:
July 12, 2005
Date of Patent:
July 26, 2016
Assignee:
EMISPHERE TECHNOLOGIES, INC.
Inventors:
Steven Dinh, Huaizhen Wang, Maria Isabel Gomez-Orellana
Abstract: The present invention provides novel solid pharmaceutical dosage forms for oral administration comprising a bisphosphonate, or a pharmaceutically acceptable salt thereof, which bisphosphonate is present in an amount not therapeutically effective when the bisphosphonate is orally administered alone, and a modified amino acid carrier, or a pharmaceutically acceptable salt thereof, which modified amino acid carrier is present in an amount effective to facilitate absorption of the bisphosphonate in the gastrointestinal tract such that the bisphosphonate is therapeutically effective. The ratio of bisphosphonate to modified amino acid carrier is from about 1:30 to about 1:1, respectively. These novel solid pharmaceutical dosage forms are useful in the treatment or control of bone diseases and particular disorders in calcium metabolism, including, for example, osteoporosis, hypercalcaemia of cancer, and the treatment of metastatic bone pain.
Type:
Grant
Filed:
July 16, 2009
Date of Patent:
June 21, 2016
Assignee:
EMISPHERE TECHNOLOGIES, INC.
Inventors:
Hashim Ahmed, Lewis Bender, Martin Howard Infeld, Shingai Majuru, Wantanee Phuapradit, Navnit Hargovindas Shah, Zhongshui Yu
Abstract: The present invention relates to stable pharmaceutical formulations that include a delivery agent and/or pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
June 28, 2007
Date of Patent:
June 14, 2016
Assignee:
EMISPHERE TECHNOLOGIES, INC.
Inventors:
Shingai Majuru, Moses O. Oyewumi, Mehmet Tahir Gurler
Abstract: The present invention relates to pharmaceutical formulations containing a pharmaceutically acceptable gallium salt (such as gallium nitrate), a delivery agent, and optionally, one or more chemotherapeutic agents and/or adjunctive chemotherapeutic agents.
Type:
Grant
Filed:
December 29, 2005
Date of Patent:
May 24, 2016
Assignee:
EMISPHERE TECHNOLOGIES, INC.
Inventors:
Lewis Bender, Bavani Shankar, Catherina O'Shaughnessy
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: 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 crystalline polymorphic forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, pharmaceutical compositions containing the same, methods of preparing the same, and methods for facilitating the delivery of active agents with the same.
Type:
Grant
Filed:
April 5, 2013
Date of Patent:
January 19, 2016
Assignee:
EMISPHERE TECHNOLOGIES, INC.
Inventors:
Nikhil Dhoot, Steven Dinh, Shingai Majuru, William Elliott Bay, JoAnne P. Corvino, Doris C. O'Toole
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:
November 18, 2016
Date of Patent:
August 18, 2020
Assignee:
EMISPHERE TECHNOLOGIES INC.
Inventors:
Jun Liao, Pingwah Tang, David Gschneidner, Jonathan Maeyer