Abstract: Disclosed is a benzyl-oxathiazine derivative, as shown in Formula I, the derivative being substituted with adamantane or noradamantane: the variables of which are as described herein; also disclosed is a method of preparation and use of same.
Type:
Grant
Filed:
March 7, 2012
Date of Patent:
August 19, 2014
Assignee:
SANOFI
Inventors:
Thomas Boehme, Kurt Ritter, Christian Engel, Torsten Haack, Stefan Guessregen, Georg Tschank
Abstract: The present invention provides benzoxazine containing propargyl group as formula (I): wherein and The present invention provides a method of preparing a compound of formula (I). The present invention also provides a flame resistant resin.
Type:
Grant
Filed:
April 22, 2013
Date of Patent:
August 12, 2014
Assignee:
Chung Shan Institute of Science and Technology, Armaments Bureau, M.N.D
Inventors:
Wen-Chiung Su, Ching-Hsuann Lin, Chu-Ming Huang
Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof, wherein X1, X2, X3, X4, J, K, L, X5, X6, Rb, G2, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Type:
Grant
Filed:
March 22, 2012
Date of Patent:
August 12, 2014
Assignee:
AbbVie Inc.
Inventors:
Arthur Gomtsyan, Jerome F. Daanen, Gregory A. Gfesser, Michael E. Kort, Chih-Hung Lee, Heath A. McDonald, Pamela S. Puttfarcken, Eric A. Voight, Philip R. Kym
Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.
Type:
Grant
Filed:
March 12, 2013
Date of Patent:
August 12, 2014
Assignee:
Eisai R&D Management Co., Ltd.
Inventors:
Branko Mitasev, Dae-Shik Kim, Huiming Zhang, Matthew J. Schnaderbeck, Christopher N. Farthing
Abstract: Novel methods and compounds for treating Alzheimer's Disease are provided. In one aspect, the invention provides methods for treating Alzheimer's Disease by administering certain phenothiazine derivatives. In one embodiment, the methods include administering an effective amount of a 3-oxo-7-dialkyl-amino-phenothiazine derivative, or 3-oxo-7-dialkyl-amino-phenothiazine. In another embodiment, the invention provides methods for treating Alzheimer's Disease by administering an effective amount of a 3,7-diazetidin-1-yl-phenothiazine or a derivative thereof. In another aspect, the invention provides novel azetidinyl phenothiazine compounds.
Abstract: The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria.
Type:
Grant
Filed:
November 21, 2011
Date of Patent:
August 5, 2014
Assignee:
Ecole Polytechnique Federale de Lausanne (EPFL)
Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3, G1, G2, and m are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating inflammatory disorders, cardiovascular disease, cancer, and other conditions associated with PI3K?.
Type:
Grant
Filed:
February 24, 2012
Date of Patent:
July 29, 2014
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Edcon Chang, Tony Gibson, Bohan Jin, Nicholas Scorah, Qing Dong
Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
Type:
Grant
Filed:
June 4, 2013
Date of Patent:
July 22, 2014
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
Abstract: Compounds and methods for preventing and treating viral infections are provided. In some embodiments, novel compounds broad-spectrum antiviral activity are provided. In more specific embodiments, the compounds and methods are effective against viruses such as Venezuelan Equine Encephalitis, West Nile Virus, and respiratory viruses including the common cold.
Type:
Grant
Filed:
May 2, 2011
Date of Patent:
July 22, 2014
Assignee:
Prosetta Antiviral Inc.
Inventors:
Clarence R. Hurt, Vishwanath Lingappa, Beverly Freeman, Andy Atuegbu, Anatoliy Kitaygorodskyy
Abstract: Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.
Type:
Grant
Filed:
August 16, 2011
Date of Patent:
July 22, 2014
Assignee:
Gruenenthal GmbH
Inventors:
Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
Abstract: The present invention provides compounds of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
Type:
Grant
Filed:
May 9, 2012
Date of Patent:
July 22, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Hans Hilpert, Robert Narquizian, Emmanuel Pinard, Alessandra Polara, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
Abstract: The instant invention relates to novel solid forms of the compound of formula (I) as well as solvates, inclusion complexes with other suitable compounds, processes for their manufacture, pharmaceutical compositions containing these solid forms, and their use as pharmaceuticals.
Type:
Grant
Filed:
October 12, 2012
Date of Patent:
July 22, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Pascal Dott, Olaf Grassmann, Michael Kammerer, Joachim Manns, Urs Schwitter, Andrew Thomas, Nicole Wyttenbach
Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
Abstract: The present invention provides an imidazooxazine compound represented by Formula (I) or a salt thereof, wherein A, B, C, and D are as defined in the specification.
Abstract: Benzenesulfonamide compounds having a structure of the following general formula (I) are described. Also described, are methods for synthesizing the compounds, and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
Abstract: The present invention provides compounds of Formula I: wherein A is selected from the group consisting of; R1 is H or F; R2 is H, —CH2OH, C1-C3 alkyl, R3 is H, F, or CN; R4 is H, F; or CN; and R5 is H, —CH3, or —OCH3; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
December 4, 2013
Date of Patent:
July 8, 2014
Assignee:
Eli Lilly and Company
Inventors:
James Peter Beck, Steven James Green, Jose Eduardo Lopez, Brian Michael Mathes, Dustin James Mergott, Warren Jaye Porter, Zoran Rankovic, Yuan Shi, Brian Morgan Watson, Leonard Larry Winneroski, Jr.
Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is CR3, and A is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
Abstract: Crystal forms of sulfonylurea compound and method for producing the same. It has been found that a sulfonylurea compound of Formula (1): has two types of crystal polymorphisms and four types of pseudo crystal polymorphisms. A production method of each crystal form of the sulfonylurea compound of Formula (1) through recrystallization or solvate has been also found. In addition, a suspension of a composition containing the crystal that is improved in storage stability is provided.
Abstract: Three dihydrate forms B, C and D and a monohydrate form E of methylthioninium chloride are described. Forms B, C, D and E can be prepared under controlled humidity and temperature from methylthioninium chloride with higher water content or conversion of a hydrate. The hydrates can be incorporated in pharmaceutical compositions.
Abstract: Novel compounds, methods, and compositions for treating various viral infections are described. In some embodiments the novel compounds of the invention are 3-oxo-phenothiazine derivatives; more specific embodiments include 3-oxo-phenothiazine derivatives having substituents at the 1-, 7-, and 9-positions of the phenothiazine parent ring. In other embodiments, the invention provides compositions and methods for treating viral infections, especially HIV.
Type:
Grant
Filed:
March 16, 2012
Date of Patent:
June 24, 2014
Assignee:
Prosetta Antiviral Inc.
Inventors:
Clarence R. Hurt, Vishwanath Lingappa, Beverly Freeman, Andy Atuegbu, Anatoliy Kitaygorodorskyy