Abstract: The invention relates to furo[3,2-b]pyridines substituted at least in position 5 as inhibitors of protein kinases, regulators or modulators, methods of preparation thereof, pharmaceutical compositions containing the compounds, and pharmaceutical use of the compounds and compositions in the treatment of the diseases such as, for example, cancer or neurodegenerative diseases.
Abstract: The present invention is directed to crystalline addition salts of (i) 8-hydroxyquinolin-2(1H)-one derivatives and (ii) a dicarboxylic acid or a sulfimide, or a pharmaceutically acceptable solvates thereof.
Type:
Grant
Filed:
July 24, 2014
Date of Patent:
February 28, 2017
Assignee:
Almirall, S.A.
Inventors:
Montserrat Julia Jane, Francesc Carrera Carrera, Maria Prat Quiñones, Carlos Puig Duran, Francesca Pajuelo Lorenzo, Juan Antonio Perez Andres
Abstract: A process for preparing a compound represented by the following general formula (I) or a salt thereof, which comprises reacting lysine or a protective product thereof or a salt thereof with allysine or a protective product thereof in the presence of a specific trifluoromethane sulfonate to obtain a compound having pyridine ring or a salt thereof. (wherein, in the above-described general formula (I), one of R1 and R2 is —CH2CH2CH2CH(NH2)COOH group, and the other is hydrogen atom. And wherein, in the above-described general formula (I), one, or two or more of hydrogen atom, one, or two or more of carbon atom, or one, or two or more of nitrogen atom may be substituted with their isotope.
Abstract: Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminum salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.
Type:
Grant
Filed:
September 1, 2011
Date of Patent:
April 19, 2016
Assignee:
Novartis AG
Inventors:
Manmohan Singh, David A. G. Skibinski, Tom Yao-Hsiang Wu, Yongkai Li, Alex Cortez, Xiaoyue Zhang, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan, Kathy Yue
Abstract: The subject invention provides a mixture of crystalline laquinimod sodium particles, wherein (i) 90% or more of the total amount by volume of the laquinimod sodium particles have a size of 40 microns or less or (ii) 50% or more of the total amount by volume of the laquinimod sodium particles have a size of 15 microns or less, and wherein: a) the mixture has a bulk density of 0.2 g/mL to 0.4 g/mL; b) the mixture has a tapped density of 0.40 g/mL to 0.7 g/mL; c) an amount of heavy metal in the mixture is no more than 0.002% of heavy metal relative to the amount by weight of laquinimod sodium; d) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline (MCQ) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; e) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroqunoline-3-carboxylic acid (MCQCA) in the mixture is no more than 0.
Abstract: Provided in the present invention is a quinolyl-containing hydroxamic acid compound as shown in formula (I), at the same time also disclosed is the preparation method of the compound and the use thereof, and a pharmaceutical composition containing the quinolyl-containing hydroxamic acid compound. Such compounds are inhibitors of protein kinases and/or histone deacetylases, and can be used in the treatment of diseases caused by the abnormal activity of protein kinases and/or histone deacetylases, for example, tumors, etc.
Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
Type:
Grant
Filed:
January 29, 2014
Date of Patent:
June 9, 2015
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
Abstract: The present invention provides a solid of pitavastatin tert-butyl ester and process for its preparation. The present invention also provides a novel crystalline form of pitavastatin calcium, process for its preparation and pharmaceutical compositions comprising it.
Abstract: The invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts (in which formula R1 represents a hydrogen atom, lower alkyl group, lower alkenyl group, lower cycloalkyl group, aryl group, aralkyl group or heterocyclic group, wherein, the above groups are optionally substituted in ortho, meta and/or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R2 represents a hydrogen atom, lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted with one or more halogen atoms; R3 represents a lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted in ortho, meta or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R4 represents a hydrogen atom, lower alkyl group or any acidic functional group; n is 1 or 2).
Type:
Grant
Filed:
May 6, 2011
Date of Patent:
October 28, 2014
Assignees:
“AVIDIN” Kutato, Fejleszto es Kereskedelmi Korlatolt Felelossegu Tarsasag, UBICHEM Kutato Korlatolt Felelossegu Tarsasag
Inventors:
Laszlo Puskas, Csaba Szabo, Ivan Kanizsai, Mario Gyuris, Ramona Madacsi, Bela Ozsvari, Liliana Feher, Gabor Tamas
Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
Type:
Grant
Filed:
November 1, 2011
Date of Patent:
September 30, 2014
Assignee:
Portola Pharmaceuticals, Inc.
Inventors:
Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.
Type:
Grant
Filed:
August 21, 2012
Date of Patent:
February 4, 2014
Assignee:
Otsuka Pharmaceutical Co., Ltd.
Inventors:
Kenji Otsubo, Yuji Ochi, Masami Nakai, Atsushi Mori
Abstract: The present disclosure relates to a mesylate salt of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the ?2 receptor.
Type:
Grant
Filed:
December 15, 2009
Date of Patent:
October 22, 2013
Assignee:
Almirall, S.A.
Inventors:
Francesc Carrera Carrera, Carlos Puig Duran, Iolanda Marchueta Hereu, Enrique Moyes Valls