Abstract: The present invention relates to a cholesteryl ester transfer protein (CETP) inhibitor: (hereinafter referred to as Compound A) for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, in particular hyperlipidemia or mixed dyslipidemia. A further aspect of the present invention relates to a pharmaceutical composition for use in the treatment of subjects suffering from or having an increased risk for cardiovascular diseases, wherein the composition comprises a therapeutically effective amount of said Compound A CETP inhibitor.
Type:
Grant
Filed:
February 5, 2014
Date of Patent:
May 19, 2020
Assignee:
DEZIMA PHARMA BV
Inventors:
John Ford, Patrick Round, John Kastelein, Atsuhiro Kawaguchi, Koichi Tomiyasu, Kozo Oka
Abstract: The disclosure provides methods and compositions for providing shatter formulations taking the form of crystalline polymorphs, where methods of preparation include preparing tetrahydrocannabinol acid (THCA) powder followed by decarboxylating THCA and removal of terpenes.
Type:
Grant
Filed:
September 10, 2018
Date of Patent:
May 19, 2020
Assignee:
Scientific Holdings, LLC
Inventors:
Jeffrey Charles Raber, Bradley J. Douglass
Abstract: Method of treating endometriosis and related indications, comprising the administration of Pro-EGCG, a synthetic and derivative product of epigallocatechin-3-gallate [(?)-EGCG]. Use of PRO-EGCG in the manufacture of a medicament for treating endometriosis and related indications. Pro-EGCG for use in the treatment of endometriosis and related indications.
Abstract: The present invention relates to compounds of formula I wherein R, R4 and Q are each as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 pathway (HSF1 pathway). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
Type:
Grant
Filed:
April 1, 2016
Date of Patent:
May 12, 2020
Assignee:
Cancer Research Technology Limited
Inventors:
Keith Jones, Matthew Cheeseman, Nicola Chessum, Elisa Pasqua, Lindsay Evans, Michael Tucker, Birgit Wilding, Ngai Yi Mok
Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.
Type:
Grant
Filed:
October 1, 2015
Date of Patent:
May 5, 2020
Assignee:
MERCK PATENT GMBH
Inventors:
Markus Klein, Oliver Schadt, Philipp Haselmayer, Michael Busch
Abstract: This invention provides compound having a structure of Formulas: Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide.
Type:
Grant
Filed:
May 30, 2019
Date of Patent:
April 28, 2020
Assignees:
THE UNIVERSITY OF BRITISH COLUMBIA, SIMON FRASER UNIVERSITY
Inventors:
Paul Rennie, Artem Tcherkassov, Robert N. Young, Christophe M. Andre
Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R6, X1, and X2 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising compounds of formula (I).
Type:
Grant
Filed:
April 14, 2017
Date of Patent:
April 28, 2020
Assignee:
AbbVie Inc.
Inventors:
Lisa A. Hasvold, Dachun Liu, Keith F. McDaniel, John Pratt, George Sheppard, Le Wang
Abstract: The present invention provides crystalline forms of Deutetrabenazine. Specific crystalline forms provided by the present invention include Deutetrabenazine Form APO-I, a co-crystal of Deutetrabenazine and quercetin, and Deutetrabenazine Form APO-II, a co-crystal of Deutetrabenazine and luteolin. Also provided are pharmaceutical compositions including the Deutetrabenazine crystalline forms, and the use of these forms in the treatment of tardive dyskinesia and chorea associated with Huntington's disease.
Type:
Grant
Filed:
May 13, 2019
Date of Patent:
April 28, 2020
Assignee:
Apotex Inc.
Inventors:
Fabio E. S. Souza, Bahareh Khalili, Allan W. Rey
Abstract: The invention relates to a succinate dehydrogenase inhibitor or a prodrug and/or a pharmaceutically acceptable salt thereof for use in the treatment or prevention of reperfusion injury, such as ischemia-reperfusion injury, by inhibiting the accumulation of succinate, wherein the inhibitor or prodrug and/or pharmaceutically acceptable salt thereof is a cell-permeable reversible inhibitor of succinate dehydrogenase.
Type:
Grant
Filed:
July 3, 2015
Date of Patent:
March 31, 2020
Inventors:
Edward Chouchani, Thomas Krieg, Michael Patrick Murphy, Lorraine Work, Christian Frezza, Kourosh Saeb-Parsy
Abstract: A method for producing a catalyst effective in the oxidative conversion of ethylene to ethylene oxide, the method comprising: (i) impregnating a porous refractory carrier with a sub-catalytic level of silver ion in a range of 0.1 wt % to 1 wt % of silver by weight of the carrier and silver, and at least partially reducing said silver ion to elemental silver to produce a low-silver catalyst precursor having isolated silver atoms or silver nanoparticles on surfaces of said refractory carrier; and (ii) further impregnating the low-silver catalyst precursor with a catalytic amount of silver ion of at least 10 wt % total amount of silver and at least one promoting species by weight of the carrier and silver, and subjecting the further impregnated carrier to an elevated temperature of at least 200° C. to completely reduce silver ion to elemental silver in the carrier. The low-silver catalyst precursor produced in step (i) is also described in detail.
Abstract: The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds, and compositions (including pharmaceutical compositions) that include these compounds. The subject compounds and compositions are useful for inhibition of at least one histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer or neoplastic disease, such as prostate cancer, breast cancer, bladder cancer, lung cancer, melanoma, retinoblastoma, or multiple endocrine neoplasia type 1.
Abstract: Disclosed herein are methods for obtaining N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)phenylmethyl) carbamide (pimavanserin) comprising the step of contacting an intermediate according to Formula (A) or a salt thereof, with an intermediate Formula B, or a salt thereof, to produce pimavanserin or a salt thereof wherein Y is —ORi or —NR2aR2b; R3 is hydrogen or substituted or unsubstituted heteroalicyclyl, R4 is substituted or unsubstituted aralkyl; X is —OR22 or —NR23R24; (wherein R22 is hydrogen or substituted or unsubstituted C1-6alkyl and one of R23 and R24 is hydrogen and the other is hydrogen or N-methylpiperidin-4-yl); and R21 is —OCH2CH(CH3)2 or F; Also disclosed herein is the tartrate salt of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N?-(4-(2-methylpropyloxy)phenylmethyl) carbamide and methods for obtaining the salt.
Type:
Grant
Filed:
July 19, 2016
Date of Patent:
March 24, 2020
Assignee:
ACADIA Pharmaceuticals Inc.
Inventors:
Marlon Carlos, Sagun Tandel, Roger Olsson, Mikael Hillgren, Matthew J. Fleming, Andreas Philipp Boudier, Beat T. Weber
Abstract: The present disclosure is directed to generally methods for treating mammographic breast density and/or breast stiffness in a patient in need thereof, such as a premenopausal or perimenopausal patient, comprising the administration of an effective amount of androgenic agent and an effective amount of an aromatase inhibitor. These methods may also be useful in post-menopausal woman.
Abstract: Provided herein is technology relating to deuterated amlexanox and particularly, but not exclusively, to compositions comprising deuterated amlexanox, methods of producing deuterated amlexanox, and uses of deuterated amlexanox.
Type:
Grant
Filed:
April 16, 2018
Date of Patent:
March 17, 2020
Assignee:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Inventors:
Alan R. Saltiel, Hollis D. Showalter, Scott Larsen
Abstract: Implantable devices including a biocompatible matrix configured for long term location in adipose tissue and a biologically active agent that can be carried by the matrix and delivered to the adipose tissue following implant therein. The biologically active agent can include a modulator or a precursor thereof that can directly or indirectly modify the gene expression of adipose cells, e.g., adipocytes, and thereby modify the presence or quantity of one or more expression products of the adipose tissue that may act locally on distant from the implant site in an endocrine fashion. Modulators can include small molecules (e.g., resveratrol), polynucleotides (e.g., RNAi), or polypeptides (e.g., antibodies or functional fragments thereof).
Abstract: Object of the present invention are dimer impurities of the active ingredient Apixaban, analytical methods for identifying and/or quantifying them and a synthetic method for removing or limiting said impurities from Apixaban and synthetic precursors thereof.
Type:
Grant
Filed:
June 28, 2019
Date of Patent:
March 17, 2020
Assignee:
F.I.S.-FABBRICA ITALIANA SINTETICI S.P.A.
Inventors:
Elena Brasola, Filippo Tomasi, Loris Peruzzi
Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
Type:
Grant
Filed:
August 22, 2018
Date of Patent:
March 17, 2020
Assignees:
RHIZEN PHARMACEUTICALS SA, INCOZEN THERAPEUTICS PVT. LTD.
Inventors:
Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop K. Vakkalanka
Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X, Y, R1, R2, R3a, R3b, R4a, R4b and R5 are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
Type:
Grant
Filed:
March 12, 2018
Date of Patent:
March 3, 2020
Assignee:
eFFECTOR Therapeutics, Inc.
Inventors:
Justin T. Ernst, Siegfried H. Reich, Paul A. Sprengeler, Chinh Viet Tran, Garrick Kenneth Packard, Alan X. Xiang, Christian Nilewski, Theo Michels
Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.
Type:
Grant
Filed:
January 9, 2018
Date of Patent:
February 25, 2020
Assignee:
GALAPAGOS NV
Inventors:
Steven Emiel Van der Plas, Hans Kelgtermans, Sébastien Jean Jacques Cédric Dropsit Montovert, Sébastien Laurent Xavier Martina, Martin James Inglis Andrews