Abstract: A compound of Formula I includes a stereoisomer thereof and/or a salt thereof; wherein R1 is a substituted alkane group, a heterocylic group, or a pyridine group; X is hydrogen, a halogen, an amino acid residue, a substituted amino acid residue, an alkyl group, or an ester.
Abstract: An oral gel composition suitable for the treatment of oral leukoplakia comprising a combination of diclofenac with hyaluronic acid and methods of administering the oral gel that may include a device that prolongs contact time of the oral gel with the areas of the mucosa that are affected by oral leukoplakia.
Abstract: The present invention relates to: novel selenopsammaplin A and a derivative thereof, which have anticancer activity; a preparation method therefor; and a pharmaceutical composition containing the same as active ingredients and, more specifically, to: a novel compound selenopsammaplin A and a derivative thereof which exhibit more excellent anticancer activity since a disulfide moiety thereof is substituted with diselenide according to research on the structural activity of psammaplin A, which is known to have an effect of inhibiting the growth of cancer cells; a preparation method therefor; and a composition for preventing or treating cancer, containing the same as active ingredients. According to the present invention, the novel selenopsammaplin A and the derivative thereof exhibit excellent anticancer activity on various human cancer cell lines so as to be expected to be effectively usable in a pharmaceutical composition for cancer prevention and treatment.
Type:
Grant
Filed:
October 26, 2018
Date of Patent:
April 18, 2023
Assignee:
SEOUL NATIONAL UNIVERSITY R & DB FOUNDATION
Inventors:
Hyeung Geun Park, Sang Kook Lee, Hae Ju Han, Woong Sub Byun
Abstract: The present disclosure provides a therapeutic drug that is useful for the treatment of motor fluctuations (e.g., wearing-off) in Parkinson's disease. In particular, the present disclosure provides a composition and method for treating, improving, suppressing the progression, or preventing motor complications in Parkinson's disease, especially motor fluctuation, comprising tandospirone or a pharmaceutically acceptable salt thereof, wherein the tandospirone or a pharmaceutically acceptable salt thereof is parenterally administered.
Abstract: A first aspect of the invention relates to novel compounds and more precisely to novel bifunctional prodrugs and drugs. An additional aspect of the invention relates to antibody compound conjugates, wherein the compound is a claimed compound, and to pharmaceutical compositions containing the compound or antibody compound conjugate. The invention lastly relates to the use of this compound or antibody compound conjugates according to the invention in order to treat tumour diseases, particularly in mammals.
Abstract: A method for treating cancer is disclosed. The method comprises administering to a subject in need thereof, an effective amount of a pharmaceutical composition comprising monoethanolamine, its prodrug or hybrid molecule or a pharmaceutically acceptable salt thereof, and a pharmaceutically effective carrier. Also disclosed is a composition comprising monoethanolamine or a pharmaceutically acceptable salt thereof and a pharmaceutically effective carrier, wherein the pharmaceutical composition is formulated for oral, intravenous, intraperitoneal, subcutaneous, dermal, or intranasal administration.
Abstract: The present invention disclosed a crystal form of pyrazine-2(1H)-ketone compound and a preparation method therefor. Specifically disclosed is a method for preparing a compound of formula (II) and a crystal form thereof.
Abstract: Antifibrinolytic agents/drugs are applied to the concussive area of a patient's brain to counter the activation of a fibrinolytic process in the concussive area. Various techniques are described for administering the antifibrinolytic agent.
Abstract: A method of lowering cholesterol and/or PCSK9 levels in a subject in need thereof includes administering to the subject an ADH inhibitor, AKR inhibitor, and/or SNO-CoAR inhibitor at an amount(s) effective to reduce serum cholesterol and/or PCSK9 levels.
Type:
Grant
Filed:
September 21, 2018
Date of Patent:
February 14, 2023
Assignees:
CASE WESTERN RESERVE UNIVERSITY, UNIVERSITY HOSPITALS CLEVELAND MEDICAL CENTER
Abstract: Provided herein are triazacyclododecansulfonamide (“TCD”)-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer.
Abstract: Crystalline forms of upadacitinib and processes for preparation thereof are disclosed. The present disclosure also relates to pharmaceutical compositions containing the upadacitinib crystalline forms, use of the upadacitinib crystalline forms for preparing JAK1 inhibitor drugs, and use of the upadacitinib crystalline forms for preparing drugs treating rheumatoid arthritis, Crohn's disease, ulcerative colitis, atopic dermatitis and psoriatic arthritis. The crystalline forms of upadacitinib provided by the present disclosure have one or more improved properties compared with prior arts and have significant values for future drug optimization and development.
Abstract: Compositions and methods for the treatment of ocular diseases are disclosed. In accordance with one aspect of the instant invention, methods for treating, inhibiting (e.g., reducing), and/or preventing an ocular disease in a subject are provided. The methods comprise the administration of at least one inhibitor of the induction or activity of tryptophan degradation and/or of the downstream pathways that respond to this process. In a particular embodiment, the methods comprise the administration of an inhibitor of IDO1.
Type:
Grant
Filed:
January 10, 2020
Date of Patent:
January 31, 2023
Assignee:
Lankenau Institute for Medical
Research
Inventors:
Alexander J. Muller, Arturo Bravo-Nuevo, Arpita Mondal, Courtney Smith, Hollie E. Flick
Abstract: Compositions and methods for the treatment of ocular diseases are disclosed. In accordance with one aspect of the instant invention, methods for treating, inhibiting (e.g., reducing), and/or preventing an ocular disease in a subject are provided. The methods comprise the administration of at least one inhibitor of the induction or activity of tryptophan degradation and/or of the downstream pathways that respond to this process. In a particular embodiment, the methods comprise the administration of an inhibitor of IDO1.
Type:
Grant
Filed:
January 10, 2020
Date of Patent:
January 31, 2023
Assignee:
Lankenau Institute for Medical
Research
Inventors:
Alexander J. Muller, Arturo Bravo-Nuevo, Arpita Mondal, Courtney Smith, Hollie E. Flick
Abstract: The present invention relates to compounds as defined herein, which are activators of long form cyclic nucleotide phosphodiesterase-4 (PDE4) enzymes (isoforms) and to therapies using these activators. In particular, the invention relates to these activator compounds for use in a method for the treatment or prevention of disorders requiring a reduction of second messenger responses mediated by cyclic 3?,5?-adenosine monophosphate (cAMP).
Type:
Grant
Filed:
April 4, 2019
Date of Patent:
January 24, 2023
Assignee:
Mironid Limited
Inventors:
Julia Mary Adam, David Roger Adams, Santosh Shripad Kulkarni, Rahul Shripad Nandurdikar
Abstract: The present invention provides a therapeutic drug that is useful for levodopa induced dyskinesia in Parkinson's disease. In particular, the present invention provides a composition and method for treating, improving, delaying the progression, or preventing motor complications associated with levodopa therapy for Parkinson's disease, especially levodopa induced dyskinesia (PD-LID), comprising tandospirone or a pharmaceutically acceptable salt or prodrug thereof, wherein the tandospirone or a pharmaceutically acceptable salt or prodrug thereof is parenterally administered.
Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of prostaglandins or prostaglandin analogs which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent prostaglandins or prostaglandin analogs after crossing the biological barrier and thus can render treatments for the conditions that the parent prostaglandins or prostaglandin analogs can. Additionally, the HPPs are capable of reaching areas that parent prostaglandins or prostaglandin analogs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
Abstract: The present disclosure relates to certain amides and heterocyclic compounds and uses of these amides and heterocyclic compounds to inhibit Rho-associated protein kinases and treat diseases including autoimmune disorders, graft versus host disease (GVHD), inflammation, cardiovascular disorders, central nervous system disorders, and neoplastic disorders.
Abstract: Provided are compounds that target the nucleotide-binding oligomerization domain, leucine rich repeat containing X1 (NLRX1) pathway. The compounds can be used to treat conditions such as autoimmune diseases, allergic diseases, chronic and/or inflammatory central nervous system diseases, chronic and/or inflammatory respiratory diseases, cancer, and infectious diseases. Exemplary conditions include multiple sclerosis, asthma, Alzheimer's disease, Parkinson's disease, neuroinflammation resulting from, for example, stroke, traumatic brain injury, or spinal cord injury, chronic obstructive pulmonary disease, idiopathic pulmonary fibrosis, and inflammatory bowel disease.
Type:
Grant
Filed:
September 20, 2021
Date of Patent:
January 10, 2023
Assignee:
Landos Biopharma, Inc.
Inventors:
Josep Bassaganya-Riera, Andrew Leber, Nuria Tubau-Juni, Raquel Hontecillas
Abstract: There are provided new inhibitors of MDM2. Also provided are methods of synthesizing the agents, pharmaceutical formulations including the agents, and methods of using the agents to treat, ameliorate or cure diseases characterized by MDM2 over-expression or malfunction.
Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
Type:
Grant
Filed:
March 11, 2020
Date of Patent:
January 3, 2023
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Jeffery L. Kutok, David G. Winkler, Vito J. Palombella, Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Martin R. Tremblay