Abstract: The present invention provides a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, which comprises the solid preparation and an environment-controlling agent packaged together. The packaged product of present invention is useful as a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, with which discoloration of the solid preparation is suppressed, and superior storage stability of the solid preparation is obtained.
Abstract: The disclosures herein provide compounds of Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI and Formula VII or its pharmaceutical acceptable compositions and salts, as well as polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. The pharmaceutical compositions may be formulated for oral administration, delayed release or sustained release, transmucosal, syrup, topical, parenteral administration, injection, subdermal, oral solution, rectal administration, nanoparticle, buccal administration or transdermal administration. Such compositions may be used to treatment of urea cycle disorders and gout or its associated complications.
Abstract: The present invention relates to new thiadiazolidinediones of formula (I), or any pharmaceutically acceptable salt, solvate or prodrug thereof, and its use in the treatment of a disease in which glycogen synthase kinase 3 (GSK-3) is involved, particularly neurodegenerative diseases, inflammatory and autoimmune diseases and cardiovascular disorders. Additionally, there is provided a process for preparing such compounds, as well as pharmaceutical compositions comprising them.
Type:
Grant
Filed:
May 16, 2016
Date of Patent:
October 18, 2016
Assignee:
ASD THERAPEUTICS PARTNERS, LLC
Inventors:
Miguel Medina Padilla, Juan Manuel Domínguez Correa, Javier de Cristobal Blanco, Ana Fuertes Huerta, Jorge Sánchez-Quesada, Javier López Ogalla, Susana Herrero Santos, María Ángeles Pérez de la Cruz Moreno, Olga Martínez Montero, Beatriz Rodríguez Salguero, Francisco Palomo Nicolau
Abstract: The present invention relates to a novel 2-aminothiazole derivative, N-(5-(4-fluorophenyl)thiazole-2-il)-3-(furan-2-il)propane amide and to a use thereof as an anti-cancer drug. It is verified that the compound of the present invention has highly superior cancer cell-specific cytotoxic activity and in-vivo anti-cancer activity for inhibiting the growth of tumors in an animal model for cancer disease, and therefore can be developed as an anti-cancer candidate substance.
Type:
Grant
Filed:
October 30, 2012
Date of Patent:
October 4, 2016
Assignee:
Chung-Ang University Industry-Academic Cooperation Foundation
Abstract: The present invention pertains to a compound represented by a formula (I) and a method for producing thereof (in the formula, Ax is an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, Ay is a hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a cycloalkyl group, an alkenyl group having 2 to 18 carbon atoms, an organic group having 2 to 30 carbon atoms that includes at least one aromatic ring selected from a group consisting of an aromatic hydrocarbon ring and an aromatic hetero ring, or the like. Ax and Ay optionally bond to each other to form a ring, and Q is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like.).
Type:
Grant
Filed:
April 27, 2012
Date of Patent:
September 20, 2016
Assignee:
ZEON CORPORATION
Inventors:
Kei Sakamoto, Kumi Okuyama, Yasushi Nakano
Abstract: Disclosed are an alpha 7 nAChR receptor modulator compound, 4-(5-(4-chlorophenyl)-2-(2-cyclopropylacetyl)-1,4-dimethyl-1H-pyrrol-3-yljbenzenesulfonamide, its tautomeric form, its pharmaceutically acceptable salts, pharmaceutical compositions comprising the compound or a salt thereof, and a method of treating various diseases, disorders or conditions, for example, Alzheimer's disease, mild cognitive impairment, senile dementia, vascular dementia, dementia of Parkinson's disease, and attention deficit disorder.
Abstract: The invention relates to a novel class of (S)-2?-vinyl-substituted-abscisic acid derivatives, and to methods of synthesizing and using the derivatives.
Type:
Grant
Filed:
April 15, 2016
Date of Patent:
September 20, 2016
Assignee:
Valent BioSciences Corporation
Inventors:
Gary T. Wang, Daniel F. Heiman, Gregory D. Venburg, Joseph Lustig, Marci Ann Surpin, Robert Erwin Fritts, Jr., Franklin Paul Silverman, Derek D. Woolard
Abstract: The present invention provides an organic dye, a process for producing the same and the use thereof. The organic dye has the structure of formula (I) or formula (II). The regulation of the molecular energy levels and three-dimensional structures are achieved by ring-merging phenanthrocarbazole and an electron-rich thiophene unit as well as by selecting appropriate substituents. Thereby, when the organic dye of the present invention is applied to a dye-sensitized solar cell, the power conversion efficiency of the dye-sensitized solar cell is greatly improved. Meanwhile, the raw materials for the process according to the present invention have plenty of sources with low costs, so that a commercial production can be effected.
Type:
Grant
Filed:
October 14, 2015
Date of Patent:
September 20, 2016
Assignee:
Changchun Institute of Applied Chemistry Chinese Academy of Sciences
Abstract: A novel method for preparing 3-chlorocarbohydroxymoyl-4-nitro-1,2,5-oxadiazole by reacting 4-amino-3-chlorocarbohydroxymoyl-1,2,5-oxadiazole with H2O2 and a tungsten based catalyst and use of the prepared 3-chlorocarbohydroxymoyl-4-nitro-1,2,5-oxadiazole for synthesizing 3,4-Bis(4-nitro-1,2,5-oxadizaol-3-yl)-1,2,5-oxadiazole-N-oxide (DNTF).
Type:
Grant
Filed:
March 4, 2016
Date of Patent:
September 13, 2016
Assignee:
The United States of America as Represented by the Secretary of the Army
Inventors:
Reddy S. Damavarapu, Raja G. Duddu, John H. Hoare
Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
Type:
Grant
Filed:
November 21, 2006
Date of Patent:
September 13, 2016
Assignee:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
Abstract: This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).
Type:
Grant
Filed:
January 25, 2013
Date of Patent:
September 6, 2016
Assignee:
H. LUNDBECK A/S
Inventors:
Niels Svenstrup, Klaus Bæk Simonsen, Lars Kyhn Rasmussen, Karsten Juhl, Morten Langgård, Kate Wen, Yazhou Wang
Abstract: There are provided substituted 3-phenyl-isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly(ADP-ribose) polymerase PARP-1 with respect to poly(ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
November 20, 2012
Date of Patent:
August 23, 2016
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L. a corporation
Abstract: Provided are a compound represented by Formula I, a pharmaceutically acceptable salt thereof, or a solvate thereof; and a pharmaceutical composition for cancer treatment and a pharmaceutical composition for a radiation sensitizer for cancer treatment, each pharmaceutical composition including the compound of Formula I, the pharmaceutically acceptable salt thereof, or the solvate thereof: wherein, in Formula I, —R1 is a C1-C3 alkoxy, ?O, or —OH, and —R2 is a 5- or 6-membered heteroaryl including 1 to 2 hetero atoms selected from nitrogen and oxygen, wherein a carbon of the 5- or 6-membered heteroaryl is optionally substituted with a C1-C3 alkyl a C1-C3 alkoxy, or hydroxy.
Type:
Grant
Filed:
January 11, 2016
Date of Patent:
August 23, 2016
Assignee:
Korea Institute of Radiological & Medical Sciences
Inventors:
Sung Hee Hong, In Seok Hong, Kee Ho Lee
Abstract: The present invention discloses a process for the recovery of betaines from electrodialysis (ED) waste streams, whereby said waste streams are treated with a pressure driven membrane process.
Type:
Grant
Filed:
February 3, 2010
Date of Patent:
August 16, 2016
Assignee:
Lonza Ltd.
Inventors:
Markus Bicker, Miguel Angel Caraucán Dávila
Abstract: The present invention relates to a process for hydrogenating a substrate comprising a carbon-heteroatom double bond, the process comprising the step of reacting the substrate with hydrogen gas in the presence of a hydrogenation catalyst, wherein the hydrogenation catalyst is a complex of formula (I): R1-10, A and Hal are as defined in the specification. The present invention also provides processes for the preparation of the complex of formula (I) and intermediates thereof.
Type:
Grant
Filed:
March 17, 2010
Date of Patent:
August 16, 2016
Assignee:
Johnson Matthey Public Limited Company
Inventors:
Alan Dyke, Damian Mark Grainger, Jonathan Alan Medlock, Hans Guenter Nedden, Jacques Jean Marie Le Paih, Stephen James Roseblade, Andreas Seger, Vilvanathan Sivakumar, Antonio Zanotti-Gerosa
Abstract: The invention relates to a new process for producing NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a ?-amino-?-biphenyl-?-methylalkanoic acid, or acid ester, backbone. In detail, the new processes, according to the present invention, are ultimately related to the synthesis of intermediates to prepare the above NEP inhibitors, namely compounds according to formula (1), or salt thereof, wherein R1 and R2 are, independently of each other, hydrogen or a nitrogen protecting group, and R3 is a carboxyl group or an ester group, preferably carboxyl group or alkyl ester.
Type:
Grant
Filed:
November 12, 2015
Date of Patent:
August 2, 2016
Assignee:
NOVARTIS AG
Inventors:
David Hook, Bernard Riss, Daniel Kaufmann, Matthias Napp, Erhard Bappert, Philippe Polleux, Jonathan Medlock, Antonio Zanotti-Gerosa
Abstract: The present invention relates to azetidine amide derivatives derivatives of formula (I) wherein rings A1 A2 and A3 are as described in the description, to pharmaceutically acceptable salts thereof, to their preparation, to pharmaceutical compositions containing one or more compounds of formula (I), and to their use as pharmaceuticals, especially to their use as orexin receptor antagonists.
Type:
Grant
Filed:
March 11, 2014
Date of Patent:
August 2, 2016
Assignee:
ACTELION PHARMACEUTICALS LTD.
Inventors:
Martin Bolli, Christoph Boss, Christine Brotschi, Bibia Heidmann, Thierry Sifferlen, Jodi T. Williams
Abstract: Processes for purifying diketopyrrolopyrrole (DPP) copolymers are disclosed. An organic phase containing the DPP copolymer is treated with an aqueous ammonia solution and then with a palladium scavenger. The DPP copolymer is then isolated, and has a very low palladium content. The resulting DPP copolymer has high mobility.
Type:
Grant
Filed:
January 31, 2014
Date of Patent:
July 26, 2016
Assignee:
XEROX CORPORATION
Inventors:
Anthony James Wigglesworth, Yiliang Wu, Cuong Vong
Abstract: The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
Type:
Grant
Filed:
June 17, 2015
Date of Patent:
July 19, 2016
Assignee:
CORSAIR PHARMA, INC.
Inventors:
Xiaoming Zhang, Meenakshi S. Venkatraman, Cyrus K. Becker
Abstract: The present invention discloses compounds of Formula (I): wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
Type:
Grant
Filed:
February 27, 2014
Date of Patent:
July 5, 2016
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean-Marc Plancher, Robert James Weikert