Abstract: This invention provides novel polydentate selective high affinity ligands (SHALs) that can be used in a variety of applications in a manner analogous to the use of antibodies. SHALs typically comprise a multiplicity of ligands that each bind different region son the target molecule. The ligands are joined directly or through a linker thereby forming a polydentate moiety that typically binds the target molecule with high selectivity and avidity.
Type:
Grant
Filed:
April 8, 2020
Date of Patent:
March 29, 2022
Assignees:
Lawrence Livermore National Security, LLC, The Regents of the University of California
Inventors:
Sally J. DeNardo, Gerald L. DeNardo, Rodney L. Balhorn
Abstract: The present invention provides pharmaceutical compositions comprising cannabinoids and N-acylethanolamines, and methods for their use in preventing and treating a variety of cannabinoid-treatable conditions.
Abstract: Neuro-enhancing agents, compositions and methods are disclosed herein. Preferred neuro-enhancing agents of the present invention include progesterone and metabolites of progesterone, such as 3?-hydroxy-5?-pregnan-20-one (THP). These agents yield neuro-enhancing effects on neural cells that include neural progenitor and/or stem cells, whereby the agents stimulate mitosis of neural progenitor cells, stimulate neurite growth and organization, protect against neural loss, or one or more of these neural processes. Thus, the neuro-enhancing agents, compositions and methods disclosed herein are useful to reverse or prevent neurological disease or defects associated with neural loss or degeneration, such as Alzheimer's disease, neurological injuries, including injuries resulting from radiation therapy, and age-related neurological decline, including impairments in memory and learning.
Abstract: The present invention provides pharmaceutical compositions comprising cannabinoids and N-acylethanolamines, and methods for their use in preventing and treating a variety of cannabinoid-treatable conditions.
Abstract: The present invention provides pharmaceutical compositions comprising cannabinoids and N-acylethanolamines, and methods for their use in preventing and treating a variety of cannabinoid-treatable conditions.
Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of 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 thereof are also provided.
Type:
Grant
Filed:
December 3, 2019
Date of Patent:
December 7, 2021
Assignee:
REATA PHARMACEUTICALS, INC.
Inventors:
Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
Abstract: The present invention describes new amino pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
Type:
Grant
Filed:
September 16, 2019
Date of Patent:
November 23, 2021
Assignee:
Novartis AG
Inventors:
Daniela Angst, Francois Gessier, Anna Vulpetti
Abstract: The present invention encompasses a stabilized parasiticidal granule composition comprising a macrocyclic lactone compound and an insect growth regulator. The invention also encompasses methods of making and methods of using the granule for treating, controlling or preventing parasitic infestation or parasitic infection in an animal.
Type:
Grant
Filed:
June 25, 2018
Date of Patent:
October 19, 2021
Assignee:
BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC.
Abstract: The invention relates to methods of diagnosis, control and prophylaxis of inflammation and mitigation of inflammatory conditions, particularly arthritis and joint pain, in canines, comprising measuring inflammatory biomarkers wherein elevated levels of the biomarkers in blood correlates to reduced inflammation and reduced levels in blood correlates to increase level in the tissues. The invention further provides a method to treat or control inflammation comprising administering a diet comprising increased levels of one or more of DHA, EPA, vitamin C, vitamin E, and/or L-carnitine.
Abstract: Disclosed are a pharmaceutical use of a gold cluster and a substance containing the gold cluster and the preparation method and use thereof. The gold cluster and substance containing the gold cluster can inhibit the aggregation of A? and ?-syn, has excellent effects on the levels of cell models and animal models, and can be used to prepare drugs for preventing and treating Alzheimer's disease and/or Parkinson's disease.
Abstract: Described herein, are personal care compositions comprising taurine in combination with arginine and glycine, and methods for using the compositions to effect reduction of skin irritation and or inflammation, and/or improving barrier repair of the skin.
Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.
Type:
Grant
Filed:
May 15, 2020
Date of Patent:
June 8, 2021
Assignee:
Genentech, Inc.
Inventors:
Paroma Chakravarty, Chong Han, Sean M. Kelly, Karthik Nagapudi, Scott Savage
Abstract: Disclosed are a pharmaceutical use of a gold cluster and a substance containing the gold cluster and the preparation method and use thereof. The gold cluster and substance containing the gold cluster can inhibit the aggregation of A? and ?-syn, has excellent effects on the levels of cell models and animal models, and can be used to prepare drugs for preventing and treating Alzheimer's disease and/or Parkinson's disease.
Abstract: The present invention provides a compound having a particular chemical structure or a pharmacologically acceptable salt thereof which has an excellent inhibitory effect on EZH1 and/or EZH2 activity. The present invention provides a compound having a 1, 3-benzodioxole structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, or a pharmaceutical composition comprising the compound (wherein R1, R2, R3, R4, R5, R6, and V in the formula (I) are each as defined in the present specification).
Abstract: Provided herein are novel isotretinoin formulations that provide an enhanced targeted dermal delivery system for the drug isotretinoin with improved thermodynamic activity using no to a small level of ethanol relative to existing isotretinoin gel products, and methods for treatment of ichthyosis and other skin conditions using the same.
Type:
Grant
Filed:
October 26, 2016
Date of Patent:
March 2, 2021
Assignee:
Timber Pharmaceuticals LLC
Inventors:
Zachary Rome, Charles Rodney Greenaway Evans, Marc Barry Brown, Francesco Caserta
Abstract: The disclosure generally relates to compounds of formulas (I) and (II)7 including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV-1 integrase, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
Type:
Grant
Filed:
January 26, 2018
Date of Patent:
January 12, 2021
Assignee:
Institute for Cancer Research
Inventors:
Mark D. Andrake, Anna Marie Skalka, George W. Merkel
Abstract: Described is a dihydroartemisinin-steroid conjugate of formula (I), or a pharmaceutically acceptable salt thereof, where position 10 of dihydroartemisinin is linked to the steroid through a linker X. This application further provides a preparation method of the dihydroartemisinin-steroid conjugate and an application of the dihydroartemisinin-steroid conjugate in the preparation of a drug for treating cancer. The dihydroartemisinin-steroid conjugate of the invention exhibits potent inhibitory activity against various tumor cells and low cytotoxicity, moreover, the conjugate is capable of penetrating the blood-brain barrier, having a broad application prospect.
Type:
Grant
Filed:
October 18, 2019
Date of Patent:
January 5, 2021
Assignee:
YUNBAIYAO ZHENGWU SCIENCE AND TECHNOLOGY (SHANGHAI) CO., LTD.
Abstract: This invention provides novel polydentate selective high affinity ligands (SHALs) that can be used in a variety of applications in a manner analogous to the use of antibodies. SHALs typically comprise a multiplicity of ligands that each bind different region son the target molecule. The ligands are joined directly or through a linker thereby forming a polydentate moiety that typically binds the target molecule with high selectivity and avidity.
Type:
Grant
Filed:
February 28, 2019
Date of Patent:
December 29, 2020
Assignees:
LAWRENCE LIVERMORE NATIONAL SECURITY, LLC, THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors:
Sally J. DeNardo, Gerald L. DeNardo, Rodney L. Balhorn
Abstract: The present invention relates to the use of substituted pyrazole derivatives to modulate tropomyosin-related kinase (Trk) family protein kinase, and the use of the substituted pyrazole derivatives for the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
Type:
Grant
Filed:
May 30, 2018
Date of Patent:
October 13, 2020
Assignee:
NANTBIO, INC.
Inventors:
Chunlin Tao, Qinwei Wang, Sharif Asad, Paul Weingarten, Sherry Ci
Abstract: In this study, we capitalized on the antimicrobial property and low oral bioavailability of known salicylanilide anthelmintics (closantel, rafoxanide, niclosamide, oxyclozanide) to target the gut pathogen. The anthelmintics displayed excellent potency against C. difficile strains 630 and 4118 (with MIC values as low as 0.06-0.13 ?g/mL for rafoxanide) via a membrane depolarization mechanism, interestingly, closantel, rafoxanide and compound 8 were bactericidal against logarithmic- and stationary-phase cultures of the BI/NAP1/027 strain 4118. Further evaluation of the salicylanilides showed their preferential activity against Gram-positive over Gram-negative bacteria. Moreover, the salicylanilides were non-hemolytic and were non-toxic to mammalian cell lines HepG2 and HEK 293T/17 within the range of their in vitro MICs and MBCs. The salicylanilide anthelmintics exhibit desirable bactericidal and pharmacokinetic properties and are amenable to repositioning as anti-C. difficile agents.