Patents Examined by Kristin Bianchi
  • Patent number: 8569361
    Abstract: The embodiments herein provide a composition and a method of synthesizing a composition comprising an aliphatic amino acid biosynthesis inhibitor having an antifungal activity. The composition comprises 2-oxo-2H-chromen-7-yl propiolate, diethyl-hex-2-en-4-yne-dioate and dinonyl-hex-2-en-4-yne-dioate. The composition inhibits a biosynthesis of an aliphatic amino acid in a fungal biological system. The aliphatic amino acid is selected from a group consisting of leucine, isoleucine and valine. The composition is used with a concentration of 0-200 ?g/ml. The method comprises mixing solutions of dicyclohexylcarbodiimide (DCC) and Dimethylaminopyridine (DMAP) with alcohol, acetylene carboxylic acid and dichloromethane to obtain a mixture which is stirred filtered and washed with ether. The solvents are evaporated to obtain a residue that is dissolved in dichloromethane and stirred with a catalyst. The extra solvents are evaporated to obtain the derivative compound and purified by silica gel column chromatography.
    Type: Grant
    Filed: June 17, 2012
    Date of Patent: October 29, 2013
    Inventors: Soroush Sardari, Vahid Khalaj, Mahdieh Mahboobi Khomeini, Parisa Azerang
  • Patent number: 8541397
    Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: February 5, 2013
    Date of Patent: September 24, 2013
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita Bhat, Evelyn Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
  • Patent number: 8541412
    Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: September 24, 2013
    Assignee: Les Laboratoires Servier
    Inventors: Jean-Claude Ortuno, Alexis Cordi, Imre Fejes, Vincent Lacoste, Pauline Lacoste
  • Patent number: 8513233
    Abstract: The present invention disclosed compounds of Structural Formula (I), and enantiomer, racemic body, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein variable groups are as defined within, as well as methods for preparing such compounds. The compounds are useful as PPAR? agonist, through activating PPAR-RXR heterodimers that interacts with specific DNA response elements within promoter regions of target gene, particularly in the treatment and prevention of polycystic kidney and cancer.
    Type: Grant
    Filed: October 11, 2007
    Date of Patent: August 20, 2013
    Assignee: Shanghai Institute of Materia Medica, CAS
    Inventors: Jianhua Shen, Changlin Mei, Hualiang Jiang, Bin Dai, Yangliang Ye, Xishan Xiong, Jing Tang, Lili Fu
  • Patent number: 8507511
    Abstract: The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. formula (I).
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: August 13, 2013
    Assignee: Ingenium Pharmaceuticals GmbH
    Inventors: Heike Schauerte, Hans Allgeier, Michael A. Pleiss, Martin Augustin, Gisela Peraus, Gabriele Stumm, Philipp Wabnitz
  • Patent number: 8507493
    Abstract: The present invention relates to inhibitors of 11-?-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: August 13, 2013
    Assignee: AbbVie Inc.
    Inventors: Sridhar Peddi, Meena V. Patel, Jeffrey J. Rohde
  • Patent number: 8501714
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: August 6, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Patent number: 8501953
    Abstract: Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: August 6, 2013
    Assignee: Agios Pharmaceuticals, Inc
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders
  • Patent number: 8492415
    Abstract: The present invention relates to novel heterocyclic compounds, including oxadiazole compounds, pharmaceutical compositions and their use in the inhibition of reverse transcriptase and the treatment of HIV (1 and 2) infections, AIDS and ARC and other viral infections.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: July 23, 2013
    Assignee: Yale University
    Inventor: William L. Jorgensen
  • Patent number: 8486933
    Abstract: Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein L1, R1, R2, R3, R4, R5, and m are defined in the description. Methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as IGF-1R are also disclosed.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: July 16, 2013
    Assignee: AbbVie Inc.
    Inventors: Gary T. Wang, Robert A. Mantei, Scott A. Erickson, Steve D. Fidanze, George S. Sheppard, Jieyi Wang, Randy L. Bell
  • Patent number: 8486919
    Abstract: The present invention provides a compound that has a high whitening effect and is excellent in safety and stability and provides an external preparation for skin comprising the same. The compound of the present invention is a 4-alkylresorcinol derivative represented by formula (1) or a salt thereof: wherein R1 is a branched or cyclic alkyl group of 3 to 7 carbon atoms or a linear alkyl group of 2 to 5 carbon atoms; R2 and R3 are each independently a hydrogen atom or a group represented by —P(O)(OR4)(OR5), and at least one of R2 and R3 is a group represented by —P(O)(OR4)(OR5); and R4 and R5 are each independently a hydrogen atom or a linear or branched alkyl group of 2 to 5 carbon atoms.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: July 16, 2013
    Assignee: Shiseido Company, Ltd.
    Inventors: Hirotada Fukunishi, Rikako Suzuki, Kiyoshi Sato, Masaru Suetsugu
  • Patent number: 8481543
    Abstract: A compound, particularly an antimalarial compound, according to formula I: or a pharmaceutically acceptable salt thereof, wherein: X is an electron-withdrawing group; A is an optionally substituted alkanediyl or an optionally substituted cycloalkanediyl that includes 2 to 5 carbon atoms; and R1 and R2 are each individually H, tert-butyl, isopropyl, or optionally substituted cycloalkyl.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: July 9, 2013
    Assignees: Oregon Health & Science University, The United States of America as represented by the Department of Veterans Affairs
    Inventors: Michael K. Riscoe, Rolf W. Winter, David J. Hinrichs
  • Patent number: 8481748
    Abstract: Provided herein are ruthenium complexes of Formula I, and processes of preparation thereof. Also provided are methods of their use as a metathesis catalyst.
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: July 9, 2013
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Florence Marie-Emilie Bonnaterre, Dominique Surleraux
  • Patent number: 8481763
    Abstract: A process is provided for preparing dronedarone or pharmaceutically acceptable salts thereof. The process comprises reacting 5-amino-2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)benzofuran (compound A) with methanesulfonyl chloride without any catalyst to provide crude dronedarone hydrochloride, which is purified to afford highly pure product. Then, the dronedarone hydrochloride can be converted to highly pure dronedarone through treatment with an alkaline solvent, the dronedarone can be further converted to other pharmaceutically acceptable salts of dronedarone. In this process, acylation between compound A and methanesulfonyl chloride is carried out successfully and the formation of the dimethylsulfonyl by-product is inhibited.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 9, 2013
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Xianshan Hou, Yongjiang Chen
  • Patent number: 8476274
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: July 2, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
  • Patent number: 8476432
    Abstract: The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvastatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2—N—O—R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: July 2, 2013
    Assignee: Yuhan Corporation
    Inventors: Hyun Ju, Sang-Sun Joung, Hyun-Jik Yi, Ja-Heouk Khoo, Jong-Chul Lim, Jae-Gyu Kim
  • Patent number: 8476433
    Abstract: The present invention relates to the field of chemical-pharmaceutical industry and medicine. An agent, exhibiting the properties of a cognitive function promoter, was selected from 1,3-dimethyl-5-[(4-pyridylamino)methylene]barbituric acid and 4-amino-1-(3-nitro-2-oxo-1-pheny-1,2-dihydro-1,6-naphthyridin-5-yl)pyridinium chloride. The compounds, that are proposed as agents, exhibit potent biological activity.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: July 2, 2013
    Assignee: Unikorm
    Inventors: Valery Aleksandrovich Parshin, Tatyana Vasilyevna Golovko, Nelya Zarifovna Tugusheva, Marina Igorevna Medvedeva, Vladimir Vladimirovich Granik
  • Patent number: 8476288
    Abstract: The invention provides salts of 4-(dimethylamino)butyl 2-(4-((2-amino-4-methyl-6-(pentylamino)pyrimidin-5-yl)methyl)phenyl)acetate, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: July 2, 2013
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Nicholas James Bennett, Thomas McInally, Austen Pimm, Yoshiaki Isobe
  • Patent number: 8470821
    Abstract: Compounds active on phosphodiesterase PDE4B are provided. Also provided herewith are compositions useful for treatment of PDE4B-mediated diseases or conditions, and methods for the use thereof.
    Type: Grant
    Filed: July 20, 2009
    Date of Patent: June 25, 2013
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Hanna Cho, Bruce England, Sam Gillette, Dean R. Artis, Rebecca Zuckerman, Chao Zhang
  • Patent number: 8470810
    Abstract: The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C6-alkyl, C,-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6 alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2
    Type: Grant
    Filed: August 25, 2010
    Date of Patent: June 25, 2013
    Assignee: Abbott GmbH & Co. KG
    Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry, Gisela Backfisch, Armin Beyerbach, Wilfried Lubisch