Abstract: The present application relates to novel fluorinated amide derivatives of Formula (I), to processes for preparing them, pharmaceutical compositions containing them, and their use thereof in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognitive disorders and memory deficits, as well as chronic and acute pain and other related CNS disorders.
Abstract: A class of compounds of monosulfonic phenyltetrazole, with the structure of 2-(R1 phenyl)-5 (2-sulfonic phenyl)-2H-tetrazole. The 2-sulfonic phenyl tetrazolium salt of this invention has advantages of low toxicity, short synthetic route, easy control of purity and quality. As the 2-sulfonic phenyl tetrazolium salts has almost no absorption at 450 nm where the reduzate has greater absorption, spectrophotometry can simply and rapidly determine the activity of glutamate dehydrogenase, or the content of NADH/NADPH.
Abstract: The present invention relates to compounds of formula I wherein R1? is CH3 R1 is methyl, ethyl, CF3, CH2OH, cyclopropyl or cyano, or R1? and R1 may form together a 1,1-dioxo-tetrahydro-thiophen-3-yl ring; R2 is hydrogen, methyl, ethyl, isopropyl, tertbutyl, cyclopropyl or CF3; R3 is Cl, F, CF3, methyl, methoxy, isopropyl or cyclopropyl; R4 is hydrogen, methyl, F or Cl; or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof for use in the treatment of schizophrenia, bipolar disorder, obsessive-compulsive disorder or autism spectrum disorder.
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
Type:
Grant
Filed:
April 12, 2019
Date of Patent:
March 3, 2020
Assignee:
Nimbus Lakshimi, Inc.
Inventors:
Craig E. Masse, Jeremy Robert Greenwood, Sayan Mondal, Scott D. Cowen, Thomas H. McLean
Abstract: Compositions for the inhibition of SUV39H1 methyltransferase activity and methods of use thereof are provided. The disclosed compositions may be used for treating certain types of cancer, inducing apoptosis in a cancer cell, increasing cell sensitivity to FasL-induced apoptosis, and overcoming cancer cell resistance to apoptosis and/or certain types of cancer immunotherapy.
Type:
Grant
Filed:
September 18, 2018
Date of Patent:
March 3, 2020
Assignees:
Augusta University Research Institute, Inc., Department of Veterans Affairs
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
Type:
Grant
Filed:
April 12, 2019
Date of Patent:
February 25, 2020
Assignee:
Nimbus Lakshimi, Inc.
Inventors:
Craig E. Masse, Jeremy Robert Greenwood, Sayan Mondal, Scott D. Cowen, Thomas H. McLean
Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
Type:
Grant
Filed:
May 26, 2017
Date of Patent:
February 18, 2020
Assignee:
Bristol-Myers Squibb Company
Inventors:
Natesan Murugesan, Peter W. Glunz, Mandar Shrikrishna Bodas, Navnath Dnyanoba Yadav, Venu Alla
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
Type:
Grant
Filed:
April 12, 2019
Date of Patent:
February 18, 2020
Assignee:
Nimbus Lakshimi, Inc.
Inventors:
Craig E. Masse, Jeremy Robert Greenwood, Sayan Mondal, Scott D. Cowen, Thomas H. McLean
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
Type:
Grant
Filed:
April 12, 2019
Date of Patent:
February 18, 2020
Assignee:
Nimbus Lakshimi, Inc.
Inventors:
Craig E. Masse, Jeremy Robert Greenwood, Sayan Mondal, Scott D. Cowen, Thomas H. McLean
Abstract: The present invention relates to a novel family of covalent kinases inhibitors. Compounds of this class have been found to have inhibitory activity against members of the Tec kinase family, particularly ITK, BTK, BMX, Tec and/or RLK. The present invention is directed to a compound of Formula I or pharmaceutically acceptable salt, solvate, solvate of salt, stereoisomer, tautomer, isotope, prodrug, complex or biologically active metabolite thereof and its use in therapy.
Type:
Grant
Filed:
September 22, 2016
Date of Patent:
February 18, 2020
Assignee:
GB005, INC.
Inventors:
Alain Laurent, Yannick Rose, Stephen J. Morris
Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
Type:
Grant
Filed:
August 28, 2018
Date of Patent:
February 11, 2020
Assignee:
REATA PHARMACEUTICALS, INC.
Inventors:
Eric Anderson, Xin Jiang, Melean Visnick
Abstract: The present invention relates to novel oxadiazoles of the formula I or an N-oxide and/or their agriculturally useful salts and to their use for controlling phytopathogenic fungi, or to a method for combating phytopathogenic harmful fungi, which process comprises treating the fungi or the materials, plants, the soil or seeds to be protected against fungal attack, with an effective amount of at least one compound of the formula I, or an N-oxide, or an agriculturally acceptable salt thereof; and to mixtures comprising at least one such compound and at least one further pesticidally active substance selected from the group consisting of herbicides, safeners, fungicides, insecticides, and plant growth regulators; and to agrochemical compositions comprising at least one such compound and to agrochemical compositions further comprising seeds.
Type:
Grant
Filed:
October 27, 2016
Date of Patent:
February 11, 2020
Assignee:
BASF SE
Inventors:
Christine Wiebe, Manuel Kretschmer, Wassilios Grammenos, Ana Escribano Cuesta, Maria Angelica Quintero Palomar, Ian Robert Craig, Erica Cambeis, Thomas Grote, Marcus Fehr, Tobias Mentzel, Bernd Mueller, Christian Harald Winter, Violeta Terteryan-Seiser, Jan Klaas Lohmann
Abstract: A benzotriazole-derived ? and ?-unsaturated amide compound used as TGF-?R1 inhibitor or a pharmaceutically acceptable salt thereof, the structure of the compound being as shown in formula (I).
Type:
Grant
Filed:
June 8, 2017
Date of Patent:
February 4, 2020
Assignees:
Genfleet Therapeutics (Shanghai) Inc., Medshine Discovery Inc.
Inventors:
Fei Sun, Lifang Wu, Charles Z. Ding, Guoping Hu, Jian Li, Shuhui Chen, Jianyu Lu
Abstract: The disclosure relates to dialkyl carbonates of branched alcohols and their use in cosmetic and/or pharmaceutical compositions. The disclosure more particularly relates to dialkyl carbonates in which the alkyl groups are both 2-propyl-1-heptyl groups.
Type:
Grant
Filed:
May 30, 2017
Date of Patent:
January 28, 2020
Assignee:
Cognis IP Management GmbH
Inventors:
Achim Ansmann, Bernd Boutty, Markus Dierker, Stefan Bruening, Rolf Kawa
Abstract: This invention relates to HIV-inhibiting compounds consisting of other Formulae I, II or III isatin derivatives, as shown below (Formulae I, II and III), whereby in Formulae I, II and III, R1 is selected from H, CH3 or Cl; R2 is selected from one of the following radicals: zidovudine, amprenavir or an acyclic phosphonate chain, as shown below. This invention also relates to the use and treatment method using the Formulae I, II and III compounds. According to this invention, these compounds are also used for the treatment of infections caused by HBV or co-infection caused by HIV and HBV.
Type:
Grant
Filed:
May 10, 2016
Date of Patent:
January 21, 2020
Assignee:
FUNDAÇĀO OSWALDO CRUZ
Inventors:
Nubia Boechat, Mônica Macedo Bastos, Thiago Moreno Lopes E Souza, Débora Inácio Leite, Alice Maria Rolim Bernardino
Abstract: The present invention provides 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
Type:
Grant
Filed:
August 1, 2018
Date of Patent:
January 21, 2020
Assignee:
H. Lundbeck A/S
Inventors:
Karsten Juhl, Mikkel Jessing, Morten Langgård, Paulo Jorge Vieira Vital, Mauro Marigo, Jan Kehler, Lars Kyhn Rasmussen
Abstract: Disclosed herein are novel compounds of formula (I) and (II), each of which may serve as a reagent to deliver nitric oxide (NO) and a therapeutic agent to treat NO-associated diseases. Also disclosed are a pharmaceutical composition comprising the compound of formula (I) or (II), a composite material comprising the compound of formula (I) or (II), and the uses thereof.
Abstract: The present invention relates to a compound represented by Formula (I): wherein -L- is —C(?X)—, or the like, —Z— is —NR5—, or the like, —ZA— is —NR5A—, or the like, —W— is —C(R8R9)n-, —WA— is —C(R3R4)m-, B is substituted or unsubstituted aromatic carbocyclyl, or the like, Y is a bond, or the like, the ring C is a substituted or unsubstituted aromatic heterocycle, or the like, R2 is a hydrogen atom, or the like, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.