Abstract: Provided is a multi-arm polyethylene glycol derivative having a narrow molecular weight distribution. A multi-arm polyethylene glycol derivative represented by the formula (1): m[Z—YnCH2CH2OX—O-L-O—XOCH2CH2nY—Z]m??(1) wherein, L represents a group selected from a linear or branched alkylene, arylene, or cycloalkylene group having two or more carbon atoms and combinations thereof, which may have an ether bond in a chain; X represents a dehydroxylation residue of a linear sugar alcohol having 5 or 7 carbon atoms; m is the number of polyethylene glycol chains bonded to X and represents 4 or 6; n is the average addition molar number of oxyethylene groups and n represents an integer of 3 to 600; Y represents a single bond or an alkylene group which may have an ester bond, a urethane bond, an amide bond, an ether bond, a carbonate bond, a secondary amino group, a urea bond, a thioether bond or a thioester bond in a chain or at an end; and Z represents a chemically reactive functional group.
Abstract: The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them. Salt adducts of the invention and compositions comprising them may be used to in the treatment of diseases or disorders associated with or inflicted by alcohol consumption.
Abstract: A novel compound which has excellent ultraviolet-absorbing function (especially UVA absorbing function) and excellent hydrophilicity. A benzylidene azolidine derivative represented by structural formula (I) or a salt thereof. In structural formula (I), n represents an integer of 1-5; A1 represents O, S or N-A4; and each of A2, A3 and A4 independently represents a hydrogen atom, an alkyl group which may be substituted by a hydroxyl group and has 1-8 carbon atoms, or the like (provided that at least one of A2, A3 and A4 contains one or more hydroxyl groups). In this connection, when n is an integer of 2-5, the plurality of A3O— moieties may be the same as or different.
Abstract: This invention provides a platinum/carbon nanotube catalyst applicable to heterogeneous asymmetric hydrogenation, which is fabricated by supporting platinum on carbon nanotube carriers. The catalyst is prepared by the steps of: heating purified carbon nanotubes in nitric acid, filtering and washing the same with water until pH value of the filtrate becomes neutral, drying the carbon nanotubes; immersing the carbon nanotube carriers obtained in an aqueous chloroplatinic acid solution and carrying out ultrasonic treatment at room temperature; immersing the mixture of the carbon nanotubes and the aqueous chloroplatinic acid solution under stirring; drying the material by heating to 110° C. from room temperature and maintaining this temperature; grinding the product to fine powders, reducing the fine powders with an aqueous sodium formate solution under a heating condition, filtering and washing the product with deionized water, and drying the product.
Type:
Grant
Filed:
May 11, 2010
Date of Patent:
August 23, 2016
Assignee:
DALIAN INSTITUTE OF CHEMICAL PHYSICS, CHINESE ACADEMY OF SCIENCES
Abstract: The present invention relates to an economic process for preparing surface-reacted calcium carbonate. The present invention further relates to a surface-reacted calcium carbonate having an increased specific BET surface area, and the use of a process for adjusting the specific BET surface area.
Type:
Grant
Filed:
August 7, 2013
Date of Patent:
August 9, 2016
Assignee:
Omya International AG
Inventors:
Patrick A. C. Gane, Daniel E. Gerard, Joachim Schölkopf
Abstract: The present invention relates to an economic process for preparing surface-reacted calcium carbonate. The present invention further relates to a surface-reacted calcium carbonate having an increased specific BET surface area, and the use of a process for adjusting the specific BET surface area.
Type:
Grant
Filed:
June 26, 2014
Date of Patent:
August 2, 2016
Assignee:
Omya International AG
Inventors:
Patrick A.C. Gane, Daniel E. Gerard, Joachim Schölkopf
Abstract: Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.
Type:
Grant
Filed:
April 12, 2011
Date of Patent:
August 2, 2016
Assignee:
Supernus Pharmaceuticals, Inc.
Inventors:
Likan Liang, Padmanabh P. Bhatt, David Dain, Jean-Philippe Taquet, Aleksandr Pechenov, Alexei Tchesnokov, Reynold Mariaux
Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Grant
Filed:
October 16, 2013
Date of Patent:
July 19, 2016
Assignee:
Tolero Pharmaceuticals, Inc.
Inventors:
Koc-Kan Ho, Yong Xu, Michael David Saunders, Xiaohui Liu, Scott Albert Pearce, Kevin Bret Wright, Jason Marc Foulks, Kenneth Mark Parnell, Steven Brian Kanner, David Lee Vollmer, Jihua Liu
Abstract: Disclosed is a method for preparing a dinitrile compound. The method includes reacting an alcohol compound with a nitrile compound having a terminal carbon-carbon unsaturated bond under anhydrous conditions. A potassium alkoxide having 1 to 5 carbon atoms is used as a catalyst in the course of the reaction. According to the method, a high-purity dinitrile compound can be prepared in a simple manner within a short reaction time indicating high productivity.
Type:
Grant
Filed:
September 13, 2013
Date of Patent:
July 19, 2016
Assignee:
LG CHEM, LTD.
Inventors:
Byoung-Bae Lee, Jae-Seung Oh, You-Jin Shim, Yeon-Suk Hong
Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
Abstract: The invention is directed to the use of a compound of formula I as defined herein, a pharmaceutically acceptable salt thereof; or a pharmaceutical composition containing a compound of formula I, in treating a mammal, including a human, for a psychiatric disorder or condition selected from the group consisting of stroke, Huntington's disease and amyotrophic lateral sclerosis (ALS).
Type:
Grant
Filed:
July 28, 2015
Date of Patent:
July 5, 2016
Assignee:
MediSynergics, LLC
Inventors:
Dennis Michael Godek, Harry Ralph Howard
Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.
Type:
Grant
Filed:
December 7, 2012
Date of Patent:
July 5, 2016
Assignees:
Shenyang Pharmaceutical University, Shenyang Pharmaceutical University (Benxi) Pharmaceutical Science and Technology Co., Ltd.
Abstract: Isolated stereoisomeric forms of the compound (S)2-N(3-O-(propan 2-ol) -1-propyl-4-hydroxybenzene)-3-phenylpropylamide and uses in the treatment of pain.
Abstract: The present invention relates to a process for preparing a crystalline solid from glycine-N,N-diacetic acid derivatives (e.g., MGDA) of sufficiently low hygroscopicity, which is characterized in that at least one crystalline compound of the formula I is introduced as seed, and a spray granulation is carried out with at least one compound of the formula I, preferably followed by a heat treatment.
Abstract: The present invention is directed to pharmaceutical compositions comprising: (a) a cyclopolysaccharide and (b) a compound of Formula (I) or its pharmaceutical acceptable salt: wherein X1, X2, Q, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compositions.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
June 28, 2016
Assignee:
Purdue Pharmaceuticals Products L.P.
Inventors:
Yu Chen, Lan Yang, Feiyu Feng, Qiufu Ge, Dianwu Guo, Yi Chen
Abstract: Disclosed are as represented by Formula (I) a quinazoline derivative and a pharmaceutical acceptable salt thereof, or, an enantiomer, a non-enantiomer, a tautomer, a racemate, a solvate, a metabolic precursor, or a prodrug of both. Also disclosed are a preparation method therefor, an intermediate, a pharmaceutical composition having the quinazoline derivative, and an application thereof. The quinazoline derivative of the present invention is provided with improved anti-tumor activity.
Type:
Grant
Filed:
July 27, 2012
Date of Patent:
June 21, 2016
Assignees:
SHANGHAI PHARMACEUTICALS HOLDINGS CO., LTD., ZHEJIANG UNIVERSITY
Abstract: The present disclosure provides compositions, pharmaceutical preparations and methods for the diagnosis and treatment of cancers expressing a GLI polypeptide. The disclosed compositions and pharmaceutical preparations may comprise one or more pyrazolyl-containing compounds, or an analog or derivative thereof.
Type:
Grant
Filed:
July 20, 2012
Date of Patent:
June 21, 2016
Assignee:
The Regents of the University of California
Inventors:
Biao He, Michael Mann, David M. Jablons
Abstract: The invention is directed to compounds that are specific inhibitors of PKC delta, and methods and compositions for the treatment and prevention of cancers and other disorders. Compositions comprising compounds of the invention are used to treat cancers such as, for example, carcinoid and neuroendocrine tumors, malignant melanomas, pancreatic, gastrointestinal and lung cancers. Neuroendocrine tumor cell lines of pulmonary and gastrointestinal origin are surprisingly sensitive to PKC delta inhibition by the compounds of the invention. The invention is further directed to methods, compositions and kits containing compounds of the formulas (Ia), (IIa), (IIIa), (IVa), and (V) as disclosed and described in FIGS. 11 and 12.
Abstract: The invention relates to a compound described by a general formula (1), wherein each X independently can be OPO32?, OPSO22? or OSO3?; R1 comprises a solubility function such as a polyethylene glycol moiety and each X independently can be OPO32?, OPSO22?, ? or OSO3?; and Z is an alkyl chain comprising 1 to 3 carbon and/or hetero atoms. The invention further relates to polysulfate derivatives or mixed polyphosphate/sulphate derivatives of six-membered cyclic polyols for use in the therapy of infection by Clostridium difficile.
Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
Type:
Grant
Filed:
January 29, 2015
Date of Patent:
May 31, 2016
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst