Abstract: Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions comprising the novel compounds of Formula I and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
Type:
Grant
Filed:
January 27, 2017
Date of Patent:
November 10, 2020
Assignee:
Vitae Pharmaceuticals, LLC
Inventors:
David A. Claremon, Lawrence Wayne Dillard, Yi Fan, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Linghang Zhuang
Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.
Type:
Grant
Filed:
August 19, 2016
Date of Patent:
November 3, 2020
Inventors:
Thomas E. Barta, Jonathan William Bourne, Kyle D. Monroe, Michael M. Muehlemann, Anjali Pandey, Simeon Bowers
Abstract: Lincosamides of general formula I, where R1 is selected from C2-C8 alkyl or C2-C8 alkenyl; R3 is selected from OH, O(C1-C4 alkyl), SH, S(C1-C4 alkyl) or halogen; R4 is H or C1-C3 alkyl; each of R21, R22, R23, R24, R25 is independently selected from the group consisting of H, OH, C1-C4 alkyl, C1-C4 alkenyl, C1-C4 alkynyl, halogen, O(C1-C4 alkyl), O(C1-C4 alkenyl), O(C1-C4 alkynyl), NH2, N(C1-C4 alkyl)2, N(C1-C4 alkenyl)2, N(C1-C4 alkynyl)2; and pharmaceutically acceptable salts thereof. A method of preparation thereof, in particular a biosynthetic method using newly discovered functions of celesticetin biosynthetic proteins Ccb1 and/or Ccb2. Lincosamides of general formula I are suitable for use as antibacterial and antiprotozoal substances.
Type:
Grant
Filed:
March 9, 2018
Date of Patent:
November 3, 2020
Assignee:
MIKROBIOLOGYICKY USTAV AG CR, V. V. I.
Inventors:
Jiri Janata, Zdenek Kamenik, Stanislav Kadlcik, Lucie Najmanova, Radek Gazak
Abstract: The present invention relates to novel 5-(carboxamide)-1-phenyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
Type:
Grant
Filed:
May 2, 2017
Date of Patent:
October 27, 2020
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Marie-Pierre Collin-Kröpelin, Peter Kolkhof, Thomas Neubauer, Chantal Fürstner, Elisabeth Pook, Matthias Beat Wittwer, Klemens Lustig, Anja Buchmüller, Hanna Tinel, Karoline Dröbner, Thomas Mondritzki, Heiko Schirmer, Axel Kretschmer, Carsten Schmeck, Pierre Wasnaire, Hana Cernecka
Abstract: The present invention relates to novel Oxoalkyl-substituted 1-phenyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular and renal diseases.
Type:
Grant
Filed:
May 2, 2017
Date of Patent:
October 13, 2020
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Carsten Schmeck, Anna Engelen, Peter Kolkhof, Klemens Lustig, Elisabeth Pook, Pierre Wasnaire
Abstract: In alternative embodiments, the invention provides nucleophilic hydroxyimino-acetamido alkylamine antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nerve system (CNS). The hydroxyimino-acetamido alkylamines of the invention are designed to fit within AChE active center gorge dimensions, bind with reasonable affinity, and react with the conjugated phosphate atom in the gorge. The hydroxyimino-acetamido alkylamines of the invention are also designed to possess ionization states that govern affinity and reactivity for the two linked hAChE re-activation steps.
Type:
Grant
Filed:
July 11, 2019
Date of Patent:
October 13, 2020
Assignees:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE SCRIPPS RESEARCH INSTITUTE
Inventors:
Palmer Taylor, Zoran Radic, K. Barry Sharpless, Valery Fokin, Rakesh Sit
Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y, W, m, n, p and q are as defined herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
April 10, 2019
Date of Patent:
October 13, 2020
Assignee:
Hoffman-La Roche Inc.
Inventors:
Patrizio Mattei, Jerome Hert, Daniel Hunziker, Markus Rudolph, Petra Schmitz, Patrick Di Giorgio
Abstract: The present invention relates to a method for preparing dialkyl dicarbonates from the corresponding alkyl chloroformates using specific tertiary amines as catalysts.
Abstract: It is an object of the present invention to provide a novel triazole derivative. Further, it is another object of the present invention to provide a light-emitting element having high luminous efficiency with the use of the novel triazole derivative. Moreover, it is still another object of the present invention to provide a light-emitting device and electronic devices which have low power consumption. A light-emitting element having high luminous efficiency can be manufactured with the use of a triazole derivative which is a 1,2,4-triazole derivative, in which an aryl group or a heteroaryl group is bonded to each of 3-position, 4-position, and 5-position, and in which any one of the aryl group or heteroaryl group has a 9H-carbazol-9-yl group.
Type:
Grant
Filed:
May 23, 2016
Date of Patent:
September 29, 2020
Assignee:
Semiconductor Energy Laboratory Co., Ltd.
Inventors:
Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
Abstract: Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics with at least one reagent has significant potential in cancer treatment. Replication Protein A, the eukaryotic single-strand (ss) DNA binding protein, is essential for genomic maintenance and stability via roles in both DNA replication and repair. Reported herein are small molecules that inhibit the in vitro, in vivo, and cellular ssDNA binding activity of RPA, thereby disrupting the eukaryotic cell cycle, inducing cytotoxicity and increasing the efficacy of chemotherapeutic agents damage DNA, and/or disrupt its replication and/or function. These results provide new insights into the mechanism of RPA-ssDNA interactions in chromosome maintenance and stability. This represents a molecularly targeted eukaryotic DNA binding inhibitor and demonstrates the utility of targeting a protein-DNA interaction as a means of studying the cell cycle and providing a therapeutic strategy for cancer treatment.
Type:
Grant
Filed:
November 13, 2015
Date of Patent:
September 15, 2020
Assignee:
Indiana University Research and Technology Corporation
Abstract: The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
Type:
Grant
Filed:
September 15, 2016
Date of Patent:
September 8, 2020
Assignees:
Assembly Biosciences, Inc., INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
Inventors:
William Turner, Hans Maag, Samson Francis
Abstract: Substituted 1,2,3-triazoles as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.
Type:
Grant
Filed:
December 31, 2018
Date of Patent:
September 8, 2020
Assignee:
JANSSEN PHARMACEUTICA NV
Inventors:
Gang Chen, Christa C. Chrovian, Heather R. Coate, Curt A. Dvorak, Christine F. Gelin, Afton Hiscox, Michael A. Letavic, Jason C. Rech, Akinola Soyode-Johnson, Brice Stenne, Jessica L. Wall, Wei Zhang
Abstract: Dual function compounds are provided that may be inhibitors of histone deacetylase (HDAC) and activators of ataxia telangiectasia mutated (ATM). Pharmaceutical compositions and methods of use are also provided that utilize such compounds.
Type:
Grant
Filed:
March 3, 2016
Date of Patent:
August 18, 2020
Assignee:
Shuttle Pharmaceuticals, Inc.
Inventors:
Scott Grindrod, Mira Jung, Milton Brown, Anatoly Dritschilo
Abstract: The present disclosure is based, in part, on the discovery that disclosed compounds such as those having Formula (IVa), (Va), (IV), or (V) can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.
Type:
Grant
Filed:
December 23, 2015
Date of Patent:
August 11, 2020
Assignee:
Proteostasis Therapeutics, Inc.
Inventors:
Cecilia M. Bastos, Benito Munoz, Bradley Tait
Abstract: Dual function compounds are provided that may be inhibitors of histone deacetylase (HDAC) and activators of ataxia telangiectasia mutated (ATM). Pharmaceutical compositions and methods of use are also provided that utilize such compounds.
Type:
Grant
Filed:
November 6, 2017
Date of Patent:
August 4, 2020
Assignee:
Shuttle Pharmaceuticals, Inc.
Inventors:
Scott Grindrod, Mira Jung, Milton Brown, Anatoly Dritschilo
Abstract: A compound or a salt thereof represented by Formula (I). An LSD1 inhibitor containing the compound or a salt thereof as an active ingredient. A pharmaceutical composition containing the compound or salt thereof. An antitumor agent containing the compound or a salt thereof as an active ingredient.
Abstract: Compounds represented by Formula I are disclosed herein, wherein R, Ra and R1-R14 are as defined herein. Further disclosed are uses and methods utilizing said compounds for use in inhibiting an activity of PERK, and in treating a disease or disorder associated with aggregation-prone proteins, a disease or disorder in which downregulating an unfolded protein response is beneficial, and/or Huntington's disease.
Type:
Grant
Filed:
June 13, 2017
Date of Patent:
July 28, 2020
Assignee:
Ramot at Tel-Aviv University Ltd.
Inventors:
Gerardo Zelmar Lederkremer, Julia Leitman, Hagit Eiger, Daniel Offen, Javier Ganz, Moshe Portnoy
Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17?-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17?-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
June 7, 2018
Date of Patent:
July 21, 2020
Assignee:
FORENDO PHARMA LTD
Inventors:
Leena Hirvelä, Marjo Hakola, Tero Linnanen, Pasi Koskimies, Camilla Stjernschantz