Abstract: The present invention relates to a single-pot method for preparing dialkyl carbonates, the method comprises reaction of alkylene oxide with aliphatic or cyclic aliphatic alcohol, using wood ash catalyst, under CO2 pressure and heating the reaction mixture thereof to obtain dialkyl carbonates.
Abstract: The present invention provides an isopropanol solvate of enzalutamide. The present invention also provides a process for the preparation of androgen receptor antagonist. In particular, the present invention provides a process for the preparation of enzalutamide or its pharmaceutically acceptable salts, hydrates, solvates, polymorphs or intermediates thereof.
Abstract: The invention provides compounds, compositions, and methods for the treatment of diseases, disorders, or conditions that are modulated by matrix metalloproteinases (MMPs). The compounds can be selective MMP inhibitors, for example, selective inhibitors of MMP-2, MMP-9, and/or MMP-14. The disease, disorder, or condition can include, for example, stroke, neurological disorders, ophthalmological disorders, or wounds, such as chronic wounds or diabetic wounds.
Abstract: Derivatives of Sydnonimine and its analogues, which bind selectively to dopamine transporter (DAT) proteins are useful for treating and delaying the progression of disorders and illnesses that are alleviated by inhibiting dopamine reuptake.
Type:
Grant
Filed:
March 27, 2013
Date of Patent:
March 28, 2017
Assignee:
Caliper Life Sciences, Inc.
Inventors:
Hao Chen, Ming Liu, Qi Su, Manish Raisinghani
Abstract: The invention provides compounds of formula I: and salts thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating cancer using compounds of formula I.
Type:
Grant
Filed:
August 30, 2012
Date of Patent:
March 21, 2017
Assignees:
Wayne State University, Regents of the University of Michigan, Department of Veteran Affairs
Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
Type:
Grant
Filed:
September 20, 2016
Date of Patent:
March 14, 2017
Assignee:
ACHILLION PHARMACEUTICALS, INC.
Inventors:
Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
Abstract: Heterocyclic compounds that modulate C3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts.
Abstract: The invention provides novel compounds having the general formula: wherein A, R1 and R2 are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
July 31, 2014
Date of Patent:
March 7, 2017
Assignee:
Genentech, Inc.
Inventors:
Huifen Chen, Terry Crawford, Steven R. Magnuson, Chudi Ndubaku, Lan Wang
Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exhacerbated respiratory disorders and urological disorders.
Type:
Grant
Filed:
December 19, 2012
Date of Patent:
March 7, 2017
Assignee:
DOMPÉ FARMACEUTICI S.P.A.
Inventors:
Alessio Moriconi, Gianluca Bianchini, Sandro Colagioia, Laura Brandolini, Andrea Aramini, Chiara Liberati, Silvia Bovolenta
Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
October 28, 2012
Date of Patent:
March 7, 2017
Assignee:
Vanderbilt University
Inventors:
Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
Abstract: Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed.
Type:
Grant
Filed:
August 4, 2015
Date of Patent:
March 7, 2017
Assignee:
Cardiome Pharma Corp.
Inventors:
Bertrand M. C. Plouvier, Doug Ta Hung Chou, Grace Jung, Lewis Siu Leung Choi, Tao Sheng, Anthony G. M. Barrett, Marco S. Passafaro, Martin Kurz, Daniel Moeckli, Pirmin Ulmann, Alfred Hedinger
Abstract: The instant application describes novel compounds that modulate (in particular, inhibit) Sirt2, with structures according to Formulas (1) and (2) provided herein. The invention is also directed to pharmaceutical compositions thereof, methods of treatment (i.e., cancer and neurodegenerative disease) by administration of the modulating compounds, assay methods for finding modulators of Sirt2, and kits for practicing the assay method.
Abstract: N-substituted 3,3-dinitroazetidine, represented by the following Chemical Formula I, as an energetic plasticizer, and a method for preparing the same through a coupling reaction in which the energetic material 3,3-dinitroazetidine or an acid salt thereof serves as a nucleophile for the ?,?-unsaturated carbonyl compound as a substrate are provided. wherein R1 and R2 are each independently alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, hydroxy, nitro, or a halogen atom, wherein the substituent of the substituted radicals is selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, alkoxy, thioalkyl, amino, nitro, hydroxy, a halogen atom, and a combination thereof.
Type:
Grant
Filed:
September 3, 2015
Date of Patent:
February 21, 2017
Assignee:
AGENCY FOR DEFENSE DEVELOPMENT
Inventors:
Seung-Hee Kim, Jinseuk Kim, Chang-Woo Cho
Abstract: The invention relates to novel oxazolidinone compound. More particularly, the invention relates to novel [(S)—N-[[3-[4-fluoro-3-morpholino phenyl]-2-oxooxazolidin-5-yl] methyl] acetamide] compound of Formula-I which was disclosed in Indian Patent Application No. 5063/CHE/2013 and corresponding PCT/IN2014/000018. The compound is a broad spectrum antimicrobial agent effective against Multi-Drug Resistant S. Maltophilia pathogen and a large number of gram positive and gram negative pathogens. The compound has shown excellent biological activities against S. Maltophilia which has developed resistance against a large number of antibiotics including some of the known and widely used oxazolidinone derivatives.
Abstract: There are provided an ionic liquid having ether group(s) in which a copper(I) compound is included, a method for preparing the same, and a method for removing traces amounts of acetylene-based hydrocarbon compounds included in olefin by absorption or extraction using the same. When the disclosed solution is used, oxidation of Cu(I) to Cu(II) is prevented since CuX is stabilized by the ionic liquid. Thus, selective removal efficiency of acetylenic compounds is improved greatly while the removal performance is retained for a long period of time. Further, since the solution according to the present disclosure is applicable as an extractant as well as an absorbent, the associated operation is simple and apparatus cost can be decreased.
Type:
Grant
Filed:
June 19, 2014
Date of Patent:
February 21, 2017
Assignee:
Kolon Industries, Inc.
Inventors:
Hyun Joo Lee, Byoung Sung Ahn, Hoon Sik Kim, Jin-Hyung Kim, Gyeong Taek Gong
Abstract: The invention relates to hexahydropentaleno derivatives, the preparation method and use in medicine thereof, and in particular to hexahydropentaleno derivatives or stereo-isomers or pharmaceutically acceptable salts thereof as shown in general formula (I), and to the preparation method therefor and pharmaceutical compositions comprising the derivatives, and to the use thereof as a therapeutical agent, especially as a DPP-IV inhibitor. The definition of each substituent in formula (I) is the same as the definition in the description.
Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogs thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.
Type:
Grant
Filed:
June 27, 2014
Date of Patent:
February 7, 2017
Assignee:
Fibrotech Therapeutics PTY LTD
Inventors:
Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
Abstract: The present invention provides (R)-5-(3-((2-(1,2,4-oxadiazol-3-yl)propan-2-yl)carbamoyl)phenyl)-6-(sec-butyl)-2-(4-fluorophenyl)-N-methylbenzofuran-3-carboxamide (formula I), including pharmaceutically acceptable salts, as well as compositions and methods of using the compound. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
Type:
Grant
Filed:
December 8, 2014
Date of Patent:
January 31, 2017
Assignee:
Bristol-Myers Squibb Company
Inventors:
Kap-Sun Yeung, Katharine A. Grant-Young
Abstract: The present invention relates to polymers comprising a repeating unit of the formula (I), and their use as organic semiconductor in organic electronic devices, especially in organic photovoltaics and photodiodes, or in a device containing a diode and/or an organic field effect transistor. The polymers according to the invention can have excellent solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the polymers according to the invention are used in organic field effect transistors, organic photovoltaics (solar cells) and photodiodes.
Type:
Grant
Filed:
December 2, 2013
Date of Patent:
January 24, 2017
Assignee:
BASF SE
Inventors:
Matthias Welker, Mathieu G. R. Turbiez, Natalia Chebotareva, Hans Jürg Kirner