Abstract: The present invention provides fluorine substituted tricyclic nucleosides of formula (I) wherein: the substituents are as defined in the claims. The present invention further provides oligomeric compounds prepared therefrom. Incorporation of one or more of the tricyclic nucleosides into an oligomeric compound enhances one or more properties of the oligomeric compound. Such oligomeric compounds can also be included in double stranded compositions.
Abstract: Triphenylethylene compounds of formula (II) as dual aromatase inhibitors and selective estrogen receptors modulators are described. Also described are methods for treating patients of breast cancers, and patients of breast cancer comorbid with osteoporosis, using the described triphenylethylence compounds or pharmaceutical formulations thereof.
Abstract: A method for producing a heterogeneous catalyst for use of synthesizing cyclic carbonates by reacting an epoxide and carbon dioxide in the presence of the catalyst. A method for making a catalyst that includes forming a catalyst precursor then reacting the catalyst precursor with a tertiary phosphine.
Type:
Grant
Filed:
April 22, 2014
Date of Patent:
December 5, 2017
Assignees:
National Institute of Advanced Industrial Science and Technology, MARUZEN PETROCHEMICAL CO., LTD.
Abstract: The invention relates to a process for the preparation of 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid of the formula (I) as well as intermediates thereof and pharmaceutical preparations thereof, comprising the step of reacting a compound of the formula (IV) with a compound of the formula (V), as defined in the specification, in the presence of a chiral silver- or copper catalyst.
Abstract: Provided are biphenyl derivatives having the structure of Formula 1: stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen, halogen, hydroxy, substituted or unsubstituted C1-C6 alkyl, or C1-C6 alkoxy; R2, R3 and R4 are each independently hydrogen, halogen, substituted or unsubstituted amino, nitro, cyano, hydroxy, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C1-C6 alkoxy, or —C(O)R6; R5 is hydrogen or C1-C6 alkyl; n is 0 or 1; and R6 is hydrogen or amino, methods for preparing the same, and a pharmaceutical composition containing the same.
Type:
Grant
Filed:
July 17, 2014
Date of Patent:
November 28, 2017
Assignee:
DONG-A ST CO., LTD
Inventors:
Soon-Hoe Kim, Weon-Bin Im, Chong-Hwan Cho, Sun-Ho Choi, Jung-Sang Park, Mi-Yeon Kim, Sung-Hak Choi, Min-Jung Lee, Kang-Hun Cho
Abstract: Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof. The present disclosure relates to novel compounds and to their use as agonists of the kappa opioid receptor. The disclosure also relates to methods for preparation of the compounds and to pharmaceutical compositions containing such compounds. Kappa opioid agonists that exhibit full agonist properties at the kappa opioid receptor have been widely shown to be efficacious in preclinical models of pain, particularly visceral pain.
Type:
Grant
Filed:
June 27, 2014
Date of Patent:
November 14, 2017
Assignee:
Nektar Therapeutics
Inventors:
Neel K. Anand, Franco J. Duarte, Wen Zhang, Zhongxu Ren
Abstract: The present invention describes methods and apparatuses for the synthesis of 5-(chloromethyl)-2-furaldehyde (CMF) from saccharides in pure or crude form, the method comprising: (a) continuously contacting saccharides in pure or crude form, hydrochloric acid, and an organic solvent, by way of a continuous, biphasic-flow reactor assembly at a temperature from about 60 degrees C. to about 200 degrees C. and pressures from about 1 atmosphere to about 20 atmospheres, such that CMF is produced; (b) separating 5-(chloromethyl)-2-furaldehyde by liquid/liquid and solid/liquid phase separation; (c) producing at least five kilograms per day with at least 50% yield. Embodiments of the present invention can produce CMF in a continuous fashion, with high yield and without degradation of CMF to such side products as 5-(hydroxymethyl)furfural (HMF), 2-(2-hydroxyacetyl)furan (HAF) and levulinic acid (LA).
Abstract: In various embodiments, the present invention provides fluorescent dyes that are linked to another species through an adaptor moiety. In an exemplary embodiment, the dye is linked to a polyphosphate nucleic acid through an adaptor. An adaptor can be a component of a linker. These conjugates find use in single molecule DNA sequencing and other applications. In various embodiments, the dye moiety is a cyanine dye. Cyanine dyes that are highly charged, such as those including multiple sulfonate, alkylsulfonate, carboxylate and/or alkylcarboxylate moieties are examples of cyanine dyes of use in the compounds of the invention.
Type:
Grant
Filed:
August 25, 2011
Date of Patent:
October 3, 2017
Assignee:
Pacific Biosciences of California, Inc.
Inventors:
Stephen Yue, Gene Shen, Louis Brogley, Lubomir Sebo, Jeffrey Wegener
Abstract: This invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding agent. The method described in this invention is advantageous for preparation of stably-linked conjugates of cell binding agents, such as antibodies with effector or reporter groups. This conjugation method provides in high yields conjugates of high purity and homogeneity that are without inter-chain cross-linking and inactivated linker residues.
Type:
Grant
Filed:
May 27, 2016
Date of Patent:
September 26, 2017
Assignee:
IMMUNOGEN, INC.
Inventors:
Brenda A. Kellogg, Rajeeva Singh, Ravi V. J. Chari
Abstract: The present invention discloses deuterated benzopyran compounds having structure features as shown in Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or prodrug molecules thereof. With excellent anti-inflammatory and analgesic effects and the capability to inhibit growth of tumor cells, such compounds are novel COX-2 selective inhibitors. The compounds and pharmaceutically acceptable salts thereof disclosed by the present application can be applied in preparing anti-inflammatory and analgesic drugs and drugs for treating or preventing tumors.
Type:
Grant
Filed:
June 14, 2016
Date of Patent:
September 26, 2017
Assignee:
Guangzhou Institutes of Biomedicine And Health, Chinese Academy of Sciences
Inventors:
Yanmei Zhang, John Jeffrey Talley, Mark G. Obukowicz, Zhengchao Tu, Micky Tortorella, Yican Wang, Jianqi Liu, Yan Chen, Xiaorong Liu, Xin Lu
Abstract: The present invention discloses deuterated benzopyran compounds having structure features as shown in Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or prodrug molecules thereof. With excellent anti-inflammatory and analgesic effects and the capability to inhibit growth of tumor cells, such compounds are novel COX-2 selective inhibitors. The compounds and pharmaceutically acceptable salts thereof disclosed by the present application can be applied in preparing anti-inflammatory and analgesic drugs and drugs for treating or preventing tumors.
Type:
Grant
Filed:
June 14, 2016
Date of Patent:
September 19, 2017
Assignee:
Guangzhou Institutes of Biomedicine And Health, Chinese Academy of Sciences
Inventors:
Yanmei Zhang, John Jeffrey Talley, Mark G. Obukowicz, Zhengchao Tu, Micky Tortorella, Yican Wang, Jianqi Liu, Yan Chen, Xiaorong Liu, Xin Lu
Abstract: The present invention relates to fungicidal N-cycloalkyl-N-[(fusedphenyl)methylene] carboxamide derivatives, for example, compounds of formula (I), and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control ofphytopathogenic fungi of plants using these compounds or their compositions.
Type:
Grant
Filed:
June 24, 2014
Date of Patent:
September 19, 2017
Assignee:
BAYER CROPSCIENCE AG
Inventors:
Peter Dahmen, Philippe Desbordes, Philippe Rinolfi, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann
Abstract: The invention relates to the compounds of related compounds, or pharmaceutically acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of mucositis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of mucus diseases related to painful inflammation and ulceration of the digestive tract lining and in the mouth.
Abstract: The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (B) [wherein R1 represents a C1-C4 alkyl group, and R2 represents a 2-hydroxyethyl group or a carboxymethyl group] as a production intermediate.
Type:
Grant
Filed:
February 12, 2016
Date of Patent:
September 19, 2017
Assignee:
Daiichi Sankyo Company, Limited
Inventors:
Masashi Watanabe, Hiroshi Nagasawa, Noritada Sato
Abstract: The technology described herein relates to pinacolyl boronate substituted stilbenes for the treatment of cancers, e.g. cancers expressing abnormally high levels of SREBP1.
Abstract: Disclosed herein are methods and compositions comprising compounds of formula (I) capable of normalizing neuronal calcium dyshomeostasis. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, Pick's disease, chronic traumatic encepholopathy, traumatic brain injury, stroke, cerebellar ataxia, multiple sclerosis, Down syndrome, and aging-related CNS disorders.
Type:
Grant
Filed:
May 19, 2015
Date of Patent:
August 8, 2017
Assignee:
Rosalind Franklin University of Medicine and Science
Inventors:
Grace E. Stutzmann, Russell Dahl, Christopher H. Kaiho
Abstract: A compound represented by general formula (1) a pharmaceutically acceptable salt thereof or a solvate thereof; wherein Ar represents an aryl group, or a 5- or 6-membered heteroaryl group containing a nitrogen atom, an oxygen atom or a sulfur atom; Y represents, for example, a hydrogen atom or a C1-C6 alkyl group; A represents a C1-C3 alkylene chain which may be substituted with two C1-C2 alkyl groups; X represents a hydrogen atom or a halogen atom; V represents an oxygen atom or a methylene chain; and R represents a group selected from the formulae below:
Abstract: A method for producing meta-xylylenediamines includes a reaction step in which monohalogenated benzenes, formaldehydes, and an amide compound having a primary amide group or a secondary amide group are allowed to react in the presence of an acidic liquid, a dehalogenation step in which the halogen atom derived from the monohalogenated benzenes is replaced with a hydrogen atom, and a deprotection step in which the primary amide group or the secondary amide group derived from the amide compound is converted to an amino group. In the reaction step, the acidic liquid contains inorganic acid, the equivalent ratio of the hydrogen atom of the inorganic acid relative to the monohalogenated benzenes is more than 16; the acidic liquid has an inorganic acid concentration of more than 80 mass %; and the reaction temperature is more than 40° C.
Abstract: The present invention includes methods for the synthesis of sphingomyelins and dihydrosphingomyelins. The present invention also includes methods for the synthesis of sphingosines and dihydrosphingosines. The present invention further includes methods for the synthesis of ceramides and dihydroceramides.
Type:
Grant
Filed:
March 15, 2013
Date of Patent:
July 18, 2017
Assignee:
Cerenis Therapeutics Holding SA
Inventors:
Daniela Carmen Oniciu, Stefan Heckhoff, Benoit Oswald, Peter Rebmann, Andreas Peer, Miguel Gonzalez, Patrik Sauter