Abstract: Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
Type:
Grant
Filed:
July 12, 2019
Date of Patent:
September 15, 2020
Assignee:
Gilead Sciences, Inc.
Inventors:
Evangelos Aktoudianakis, Aesop Cho, Michael Graupe, Lateshkumar Thakorlal Lad, Paulo A. Machicao Tello, Jonathan William Medley, Samuel E. Metobo, Devan Naduthambi, Barton W. Phillips, Scott Preston Simonovich, Peiyuan Wang, William J. Watkins, Jie Xu, Kin Shing Yang, Christopher Allen Ziebenhaus
Abstract: The present disclosure provides veterinary formulations comprising a therapeutically effective amount of a voriconazole and a polymer. The disclosure also provides methods, and kits for the treatment of disease, such as for treating a fungal infection in an animal utilizing the veterinary formulations.
Type:
Grant
Filed:
August 30, 2018
Date of Patent:
August 25, 2020
Inventors:
Sue H. Duran, Allison Stewart, William R. Ravis, Eva Abarca, Rosemary Cuming, Mariano Mora Pereira
Abstract: Disclosed herein are novel compounds and uses thereof. The present compounds may suppress the activity of farnesyl transferase and thus, may act as modulators of immune cells; therefor, they are useful for the development of a medicament for treating diseases that are associated with or caused by excessive levels of farnesyl transferase or immune response. Also disclosed herein are pharmaceutical compositions containing the present compounds.
Abstract: Novel compositions including bepotastine besilate and a corticosteroid are provided, compositions including at least about 0.008% w/v benzalkonium chloride, and compositions including hydroxypropylmethyl cellulose E15 LV.
Abstract: A non-aqueous topical solution composition of pharmaceutically acceptable salt of diclofenac is disclosed. The non-aqueous topical solution composition comprises therapeutically effective amount of pharmaceutically acceptable salt of diclofenac, solublizer, penetration enhancer and solvent, and optionally a humectant, counter irritant, additional penetration enhancer and anti-oxidants and a process for preparing the same.
Abstract: The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.
Abstract: A pharmaceutical composition for treatment of a pathological condition in a patient comprises, as a first component, a manganese complex of Formula I( ), and, as a second component, a non-manganese complex compound of Formula (I), optionally together with one or more physiologically acceptable carriers and/or excipients, wherein X, R, R, R, and R are as defined herein. Methods for treatment of a pathological condition in a patient, for example, a pathological condition caused by the presence of oxygen-derived free radicals, comprises administering to said patient the first component and the second component.
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:
September 13, 2017
Date of Patent:
May 12, 2020
Assignee:
Lawrence Livermore National Security
Inventors:
Sally J. DeNardo, Gerald L. DeNardo, Rodney L. Balhorn
Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
Type:
Grant
Filed:
October 10, 2018
Date of Patent:
May 12, 2020
Assignee:
Molecular Insight Pharmaceuticals, Inc.
Inventors:
John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
Type:
Grant
Filed:
March 14, 2016
Date of Patent:
May 5, 2020
Assignee:
Molecular Insight Pharmaceuticals, Inc.
Inventors:
John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
Abstract: The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
Abstract: Provided herein are quinolinone derivatives and their uses as antiviral drugs, for example, for treatment of HSV-1 infection. Also provided herein are pharmaceutically acceptable compositions comprising the quinolinone derivatives and the uses of the composition in the treatment of diseases caused by HSV-1 virus.
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: A compound useful as a Sirt2 or Sirt5 inhibitor having the formula (1) wherein: R1 is a hydrocarbon group having at least two carbon atoms connected by carbon-carbon bonds, wherein said hydrocarbon group is optionally endcapped by a neutral or anionic oxygen-containing group; R2a, R2b, and R2c are independently selected from hydrogen atom and hydrocarbon groups; X0, X1, X2, and X3 are independently selected from —(CH2)n—, —NR5—, —O—, —S—, and a bond, wherein n represents 1, 2, or 3, provided that at least one of X0-X3 is —(CH2)n—; and R3 and R4 are independently selected from the group consisting of hydrogen atom, hydrocarbon groups, biological groups, and protecting groups. Also described are pharmaceutical compositions of the inhibiting compounds, and methods of treatment by administration of the inhibiting compounds.
Abstract: The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.
Abstract: The present invention is directed to topical pharmaceutical compositions of Formula (If) or pharmaceutically acceptable salt thereof, which act as inhibitors of syk and/or JAK kinase activity. The described topical pharmaceutical compositions are useful in preventing or treating a number of conditions mediated at least in part by syk and/or JAK kinase activity.
Type:
Grant
Filed:
November 30, 2017
Date of Patent:
January 14, 2020
Assignee:
PORTOLA 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 present disclosure provides methods of treating glioblastoma multiform (GBM) in a subject in need thereof. Compositions for use in these methods are also provided.
Abstract: The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.
Abstract: Gold(I)-carbene complexes having a selenium donor ligand with anti-cancer activity and a method of treating cancer. Methods of treating cancer comprising administering the complexes are also provided.
Type:
Grant
Filed:
October 26, 2017
Date of Patent:
December 17, 2019
Assignee:
King Fahd University of Petroleum and Minerals
Inventors:
Adam A. A. Sulaiman, Mohammad Altaf, Anvarhusein A. Isab
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:
May 8, 2018
Date of Patent:
October 29, 2019
Assignee:
Novartis AG
Inventors:
Daniela Angst, Francois Gessier, Anna Vulpetti