Abstract: A method of treating cancer in a subject includes administering to the subject a therapeutically effective amount of a small molecule agonist of EphA2 receptor protein, the small molecule having a general formula: A-L-X-Z (I).
Abstract: The present invention aims to provide a novel low-molecular-weight compound showing an orexin receptor agonist activity and expected to be useful as a prophylactic or therapeutic agent for narcolepsy and the like. The present invention provides a compound represented by the formula (I): wherein each symbol is as described in the description, or a pharmaceutically acceptable acid addition salt thereof, which has an orexin receptor agonist activity, and an orexin receptor agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.
Type:
Grant
Filed:
December 11, 2018
Date of Patent:
June 13, 2023
Assignees:
University of Tsukuba, BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
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:
October 22, 2021
Date of Patent:
June 13, 2023
Assignee:
Novartis AG
Inventors:
Daniela Angst, François Gessier, Anna Vulpetti
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:
February 28, 2023
Assignee:
Genentech, Inc.
Inventors:
Paroma Chakravarty, Chong Han, Sean M. Kelly, Karthik Nagapudi, Scott Savage
Abstract: It is provided a pharmaceutical composition comprising 3-beta-hydroxy-5-alpha-pregnan-20-one, at least one sterol or an ester thereof and a mixture of acylglycerols with a solid fat content of less than 25% at 25° C. and 0% at 37° C. In addition it is provided a method for preparing the pharmaceutical composition.
Abstract: The present invention discloses a composition comprising 70%-80% w/w tetrahydrocurcuminoids, 10%-20% w/w hexahydrocurcuminoids and 5%-10% w/w octahydrocurcuminoids and its therapeutic application. More specifically, the present invention discloses the use of a composition comprising 70%-80% w/w tetrahydrocurcuminoids, 10%-20% w/w hexahydrocurcuminoids and 5%-10% w/w octahydrocurcuminoids in the therapeutic management of interstitial lung disease or lung fibrosis.
Type:
Grant
Filed:
October 15, 2020
Date of Patent:
November 8, 2022
Assignee:
SAMI-SABINSA GROUP LIMITED
Inventors:
Muhammed Majeed, Kalyanam Nagabhushanam, Lakshmi Mundkur, Rajendran Ramanujam
Abstract: Neuropeptide FF receptor modulators based on a proline scaffold are provided which offer NPFF receptor potencies in the nanomolar range and antagonistic selectivity for the NPFF1 receptor. Methods, compounds and compositions for modulating the function of neuropeptide FF receptors are provided for pharmacotherapies capable of influencing conditions or disorders affected by the neuropeptide FF receptors.
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:
May 15, 2020
Date of Patent:
October 18, 2022
Assignee:
TIMBER PHARMACEUTICALS LLC
Inventors:
Zachary Rome, Charles Rodney Greenaway Evans, Marc Barry Brown, Francesco Caserta
Abstract: The present invention relates to a composition for preventing, alleviating or treating inflammatory diseases, comprising, as an active ingredient, an acylhydrazone derivative compound, a stereoisomer thereof or a pharmaceutically acceptable salt thereof. an acylhydrazone derivative compound, a stereoisomer thereof or a pharmaceutically acceptable salt thereof, of the present invention, effectively inhibits inflammatory cytokines and inflammatory signaling pathways, thereby effectively alleviating symptoms of inflammatory diseases such as dermatitis. Therefore, the composition according to the present invention may be effectively used for the prevention, alleviation or treatment of inflammatory diseases.
Type:
Grant
Filed:
January 11, 2019
Date of Patent:
September 20, 2022
Assignee:
Korea Research Institute Of Bioscience And Biotechnology
Inventors:
Bo Yeon Kim, Joonsung Hwang, Nak Kyun Soung, Jong Seog Ahn, Kyung Ho Lee, Jiyun Mun, Srinivasrao Ganipisetti, Hyunjoo Cha, Mija Ahn, Hee Gu Lee, Jae-Hyuk Jang, In Ja Ryoo, Sung-Kyun Ko
Abstract: The present invention relates to a method of treating PIK3CA-Related Overgrowth Spectrum (PROS) more particularly, Congenital, Lipomatous, Overgrowth, Vascular Malformations, Epidermal Nevi and Spinal/Skeletal Anomalies and/or Scoliosis (CLOVES) 10 syndrome. To date, there are no specific treatments for patients and no animal models of PROS to better understand the physiopathology of the disorder. Inventors developed a genetic mouse model of PROS that recapitulates the human disease and demonstrated the efficacy of BYL719. Based on these results they treated two patients, one adult and one child, with severe CLOVES syndrome using BYL719. The drug had a robust efficiency on disease in the 15 two patients inducing quick recovery of all affected organs. Thus, the invention relates to a method of treating PROS in a subject in need thereof comprising the step of administrating the subject with a therapeutically effective amount of BYL719.
Abstract: The present invention is directed to methods of treating multiple myeloma by administering a compound of Formula (I) or pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 26, 2019
Date of Patent:
August 16, 2022
Assignee:
Alexion Pharmaceuticals, Inc.
Inventors:
Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Yonghong Song, Qing Xu, Wolin Huang, Chandrasekar Venkataramani, Jack W. Rose, Anjali Pandey
Abstract: The application refers to a novel combination treatment/combination medicament for PF-ILD treatment, comprising as a first combination partner a therapeutically effective amount of Nintedanib or a pharmaceutically acceptable salt thereof and as a second combination partner a therapeutically effective amount of a PDE4B-inhibitor of formula I wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center or a pharmaceutically acceptable salt thereof. Hereby the second combination partner is preferably a therapeutically effective amount of the PDE4B-inhibitor of formula III or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
October 22, 2018
Date of Patent:
August 9, 2022
Assignee:
Boehringer Ingelheim Internatinal GmbH
Inventors:
Franziska Elena Herrmann, Peter Nickolaus, Stefan Ludwig Michael Wollin
Abstract: The disclosure generally relates to compounds, 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:
December 30, 2020
Date of Patent:
July 19, 2022
Assignee:
Institute for Cancer Research
Inventors:
Mark D. Andrake, Anna Marie Skalka, George W. Merkel
Abstract: Disclosed are compositions, methods of treatment using the compositions and methods of preparing the compositions for the treatment of eczema. The compositions may include propionic acid and/or non-steroidal esters of propionic acid. The compositions may further include a corticosteroid, immunomodulator, antibiotic, antibody, colloidal oatmeal, conditioned media prepared by bacterial fermentation, short chain fatty acids, picolinic acid, or emollient. The method of treatment may include analysis of the skin microbiome.
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.