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1
US10287245B2
Publication/Patent Number: US10287245B2
Publication Date: 2019-05-14
Application Number: 15/512,595
Filing Date: 2015-09-24
Assignee: BASF SE
Abstract: The present invention relates to a liquid thioether carboxylic acid ester, a process for the preparation of the liquid thioether carboxylic acid ester, an article comprising the liquid thioether carboxylic acid ester as well as a use of the liquid thioether carboxylic acid ester as a component or substantial part of an optical system, tunable lens, adaptive optical module and materials thereof, actuator, electro-active polymer, laser and all related products, optical liquid, cover glass, lens or container material, tiltable prism or optical calibration liquid or optical refractive index matching liquid and a use of the liquid thioether carboxylic acid ester as a component or substantial part of a color filter, window material, coating, varnish, lacquer, dye or pigment formulation, immersion liquid, ingredient or additive in a plastic material or ingredient or additive in a polymer. The present invention relates to a liquid thioether carboxylic acid ester, a process for the preparation of the liquid thioether carboxylic acid ester, an article comprising the liquid thioether carboxylic acid ester as well as a use of the liquid thioether carboxylic acid ester ...More ...Less
2
US10287249B2
Publication/Patent Number: US10287249B2
Publication Date: 2019-05-14
Application Number: 14/752,664
Filing Date: 2015-06-26
Abstract: A method of resolving a racemic mixture of (±)-Huperzine A to (−)-Huperzine A includes: separating the (−)-Huperzine A from the racemic mixture of (±)-Huperzine A by chiral high performance liquid chromatography (HPLC), the chiral HPLC being performed utilizing a mobile phase including a solution including an alcohol and one selected from dichloromethane, trichloromethane, and a mixture thereof, and the chiral HPLC being performed utilizing a chiral stationary phase including a polysaccharide derivative. A method of resolving a racemic mixture of (±)-Huperzine A to (−)-Huperzine A includes: separating the (−)-Huperzine A from the racemic mixture of (±)-Huperzine A by chiral high performance liquid chromatography (HPLC), the chiral HPLC being performed ...More ...Less
3
US10287257B2
Publication/Patent Number: US10287257B2
Publication Date: 2019-05-14
Application Number: 15/308,517
Filing Date: 2015-05-07
Abstract: Some of the embodiments of the present disclosure relate to a compound of the formula, and methods of preparing and using same.
4
US10287258B2
Publication/Patent Number: US10287258B2
Publication Date: 2019-05-14
Application Number: 15/708,634
Filing Date: 2017-09-19
Abstract: The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds. The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing ...More ...Less
5
US10287259B2
Publication/Patent Number: US10287259B2
Publication Date: 2019-05-14
Application Number: 15/457,587
Filing Date: 2017-03-13
Abstract: The present invention includes compounds useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention. The present invention includes compounds useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective ...More ...Less
6
US10287260B2
Publication/Patent Number: US10287260B2
Publication Date: 2019-05-14
Application Number: 14/780,616
Filing Date: 2014-03-28
Abstract: Provided is a material that, when compared with SAPd, exhibits the similar activity in cross-coupling (CC) reactions, can decrease the amount of catalytic metal that is mixed into the reaction product, and increases the number of times use can be repeated. Provided are a catalyst and a catalyst precursor that use a catalytic metal other than Pd and that exhibit the CC reaction activity similar to when Pd is used. Provided are a catalyst and a catalyst precursor that exhibit the similar CC reaction activity when using Pd or a catalytic metal other than Pd, without using a carrier such as metal and without using piranha solution. A composite wherein catalytic metal nanoparticles are dispersed in a continuous phase comprising a polymer having C2-6 alkylene group units and phenylene group units (an alkylene group unit being bonded to at least the first and fourth position of the phenylene group unit). The particle diameter of the catalytic metal nanoparticles is at most 20 nm. A composite structure including a substrate, and the aforementioned composite provided to the surface of the substrate. A method for manufacturing the composite structure by dehydrocondensating, in the presence of a catalytic metal compound, a benzene compound having at least two alkyl groups (two of the alkyl groups being at the first and fourth position) in order to form the composite on the substrate surface. Provided is a material that, when compared with SAPd, exhibits the similar activity in cross-coupling (CC) reactions, can decrease the amount of catalytic metal that is mixed into the reaction product, and increases the number of times use can be repeated. Provided are a ...More ...Less
7
US10287268B2
Publication/Patent Number: US10287268B2
Publication Date: 2019-05-14
Application Number: 15/327,705
Filing Date: 2015-07-21
Abstract: The present disclosure provides imidazolyl compounds of Formula (I) and methods of preparing the compounds. The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in treating or preventing a disease (e.g., proliferative disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein. The present disclosure provides imidazolyl compounds of Formula (I) and methods of preparing the compounds. The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in ...More ...Less
8
US10287275B2
Publication/Patent Number: US10287275B2
Publication Date: 2019-05-14
Application Number: 14/789,996
Filing Date: 2015-07-02
Abstract: The invention discloses 20,23-modified novel derivatives of 16-membered demycarosyltylonolide antibiotics, which are useful against bacterial and mycoplasmic pathogens in humans and animals. Also claimed are pharmaceutical compositions of such derivatives and their use in treating bacterial and mycoplasmic infections in humans and animals. The invention discloses 20,23-modified novel derivatives of 16-membered demycarosyltylonolide antibiotics, which are useful against bacterial and mycoplasmic pathogens in humans and animals. Also claimed are pharmaceutical compositions of such derivatives and their use in ...More ...Less
9
US10287276B2
Publication/Patent Number: US10287276B2
Publication Date: 2019-05-14
Application Number: 15/556,722
Filing Date: 2017-04-28
Abstract: The present invention provides compounds of the formula: (I) wherein: X is O or S; Q1 and Q2 are independently CR5 or N, provided at least one of Q1 and Q2 is N; Y is a direct bond or CH2; R1 is H, optionally substituted alkyl, alkenyl, alkynyl, cycloalkylalkyl, benzyl or oxetan-3-yl-CH2—; R2 is optionally substituted phenyl, pyridine, pyrimidine, pyrazine or pyridazine; R3 is alkyl or haloalkyl; R4 is optionally substituted pyridine, pyrimidine, pyrazine or pyridazine; R5 is H, alkyl, haloalkyl, cycloalkyl, alkoxy, alkoxyC(O)— or (alkoxy)2CH—; or a salt thereof. The compounds are useful for controlling ectoparasites on animals. The present invention provides compounds of the formula: (I) wherein: X is O or S; Q1 and Q2 are independently CR5 or N, provided at least one of Q1 and Q2 is N; Y is a direct bond or CH2; R1 is H, optionally substituted alkyl, alkenyl, alkynyl, cycloalkylalkyl, benzyl or ...More ...Less
10
US10287278B2
Publication/Patent Number: US10287278B2
Publication Date: 2019-05-14
Application Number: 15/539,590
Filing Date: 2015-12-22
Abstract: Novel chemokine CXCR1 and CXCR2 receptor antagonist compounds of general formula (I) are described. Also described, are pharmaceutical compositions including the compounds, and use of the compounds and the compositions for the treatment of chemokine-mediated pathologies, more specifically in the field of dermatology. Novel chemokine CXCR1 and CXCR2 receptor antagonist compounds of general formula (I) are described. Also described, are pharmaceutical compositions including the compounds, and use of the compounds and the compositions for the treatment of chemokine-mediated pathologies, more ...More ...Less
11
US10287279B2
Publication/Patent Number: US10287279B2
Publication Date: 2019-05-14
Application Number: 15/048,330
Filing Date: 2016-02-19
Abstract: A systematic screening has revealed a family of compounds that exhibit inhibitory effects on 12/15-lipoxygenase. Accordingly, the present invention relates to the use of these compounds for the inhibition of 12/15-lipoxygenase and for the treatment of a condition involving 12/15-lipoxygenase. Exemplary conditions include, but are not limited to, stroke, periventricular leukomalacia, cardiac arrest with resuscitation, atherosclerosis, Parkinson's disease, Alzheimer's disease, and breast cancer. A systematic screening has revealed a family of compounds that exhibit inhibitory effects on 12/15-lipoxygenase. Accordingly, the present invention relates to the use of these compounds for the inhibition of 12/15-lipoxygenase and for the treatment of a condition involving ...More ...Less
12
US10287285B2
Publication/Patent Number: US10287285B2
Publication Date: 2019-05-14
Application Number: 15/529,891
Filing Date: 2015-12-02
Abstract: The present invention relates to compounds of the formula I or II: (I) (II) processes for their preparation and their use as pharmaceutical agents or compositions in the treatment, of neurological disorders.
13
US10287287B2
Publication/Patent Number: US10287287B2
Publication Date: 2019-05-14
Application Number: 15/745,461
Filing Date: 2016-08-17
Abstract: The disclosure provides process developments and novel routes for the preparation of the NK-1 receptor antagonist, Compound (I) and intermediates in those routes.
14
US10287289B2
Publication/Patent Number: US10287289B2
Publication Date: 2019-05-14
Application Number: 14/776,366
Filing Date: 2014-03-12
Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts. The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process ...More ...Less
15
US10287290B2
Publication/Patent Number: US10287290B2
Publication Date: 2019-05-14
Application Number: 15/382,002
Filing Date: 2016-12-16
Abstract: The present invention provides compounds useful for treating or preventing a brain-related disease or disorder. The present invention further provides a method of treating or preventing a brain-related disease or disorder in a patient, comprising administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of modulating the activity of a monoamine transporter. The present invention provides compounds useful for treating or preventing a brain-related disease or disorder. The present invention further provides a method of treating or preventing a brain-related disease or disorder in a patient, comprising administering to the patient a ...More ...Less
16
US10287291B2
Publication/Patent Number: US10287291B2
Publication Date: 2019-05-14
Application Number: 15/680,424
Filing Date: 2017-08-18
Abstract: seco-Cyclopropapyrroloindole compounds of formula (I) where Hal, R1, R2, and R3 are as defined in the application, are potent anti-cancer agents that can be used in antibody-drug conjugates.
17
US10287292B2
Publication/Patent Number: US10287292B2
Publication Date: 2019-05-14
Application Number: 15/692,739
Filing Date: 2017-08-31
Abstract: Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient. Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in ...More ...Less
18
US10287297B2
Publication/Patent Number: US10287297B2
Publication Date: 2019-05-14
Application Number: 15/564,353
Filing Date: 2016-04-13
Abstract: Disclosed is a compound of formula (I) in which R1-R5 and X1 are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer and a method of treating diabetes.