PATENTSCOPE: EN_ALL:nmr AND PA:novartis

DIPHENYL DERIVATIVES AND USES THEREOF (Fri, 22 Mar 2019)
The present disclosure provides a compound of formula (I): (I); or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeletal muscle loss, organ degeneration, tissue damage, neurodegeneration, and muscular atrophy. The disclosure further provides pharmaceutical compositions and combinations. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
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3-(1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF (Fri, 01 Mar 2019)
The present disclosure provides a compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein R1,R2, Rx, XI, n, nl, and q are as defined herein, methods of making and use for the treatment of IKAROS Family Zinc Finger 2 (IKZF2)-dependent diseases or disorders or where reduction of IKZF2 or IKZF4 protein levels can ameliorate a disease or disorder.
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PROCESS FOR PREPARING 1 -(((Z)-(1 -(2-AMINOTHIAZOL-4-YL)-2-OXO-2-(((3S,4R)-2-OXO-4-((2-OXOOXAZOLIDIN-3-Y L)METHYL)-1 -SULFOAZETIDIN-3- YL)AMINO)ETHYLIDENE)AMINO)OXY)CYCLOPROPANE CARBOXYLIC ACID (Fri, 08 Feb 2019)
The present invention provides a process of synthesizing 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)-1-sulfoazetidin-3 yl)amino)ethylidene)amino)oxy)cyclopropanecarboxylic acid (referred to herein as Compound X), or a salt thereof, or a solvate including hydrate thereof, and/or intermediates thereof, and the use of intermediates for preparing Compound X. In particular, the process relates to the preparation of Compound X using dynamic kinetic resolution (DKR) and asymmetric catalytic reduction, thereby providing an improved route to 1-(((Z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)-1-sulfoazetidin-3 yl)amino)ethylidene)amino)oxy)cyclopropanecarboxylic acid (Compound X) and compositions containing said compound, including the arginine salt, sodium salt and hydrated solid forms of Compound X.
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INDOLE DERIVATIVES AND USES THEREOF (Fri, 01 Feb 2019)
The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeletal muscle loss, organ degeneration, tissue damage, neurodegeneration, and muscular atrophy. The disclosure further provides pharmaceutical compositions and combinations. The present disclosure also relates to the use of such compounds for research or other non- therapeutic purposes.
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SUBSTITUTED 5-CYANOINDOLE COMPOUNDS AND USES THEREOF (Fri, 28 Dec 2018)
A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for the treatment of lysine (K)-specific demethylase 1A (LSD1) - mediated diseases or disorders, Formula (I), wherein R1, R2, R3, R4, and R5 are as defined herein.
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5,6-FUSED-BICYCLIC COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 21 Dec 2018)
The present invention provides a compound of Formula (I), or a pharmaceutically acceptable salt or stereoisomer thereof; (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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COMPOUNDS AND COMPOSITIONS FOR INDUCING CHONDROGENESIS (Fri, 14 Dec 2018)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds; and methods of using such compounds for treating joint damage or injury in a mammal, for inducing hyaline cartilage production or for inducing differentiation of chondrogenic progenitor cells into mature chondrocytes.
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CRYSTALLINE FORMS OF 5-BROMO-2,6-DI(1 H-PYRAZOL-1-YL)PYRIMIDIN-4-AMINE AND NEW SALTS (Fri, 07 Dec 2018)
This application relates to various crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1- yl)pyrimidin-4-amine and salt thereof, as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water ("hydrates"). These materials are useful in the treatment of various diseases, including carcinomas, specifically lung cancer and more specifically non-small cell lung cancer.
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5,6-FUSED-BICYCLIC COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 07 Dec 2018)
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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ANTIBODY-CYTOKINE ENGRAFTED PROTEINS AND METHODS OF USE (Fri, 30 Nov 2018)
The present invention provides antibody cytokine engrafted (ACE) proteins, including those that stimulate intracellular signaling, and are useful in the treatment of cancer, immunotherapy and metabolic disorders. In particular, the provided ACE protein compositions provide preferred biological effects over wild type cytokine proteins. For example, the provided ACE proteins can convey improved half-life, stability and produceability over the corresponding recombinant cytokine formulations.
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TRICYCLIC 2-QUINOLINONES AS ANTIBACTERIALS (Fri, 09 Nov 2018)
This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof that are useful as antibacterial agents. The compounds are useful as inhibitors of bacterial gyrase activity and of bacterial infections, and have the structure of Formula (I): as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.
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ANTIBODY CONJUGATES COMPRISING TOLL-LIKE RECEPTOR AGONIST AND COMBINATION THERAPIES (Fri, 02 Nov 2018)
Provided herein are antibody conjugates comprising toll-like receptor agonists and the use of such conjugates for the treatment of cancer. In some embodiments, the conjugates comprise anti-HER2 antibodies. In some embodiments, the conjugates are used in combination with a second therapeutic agent.
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ANTIBODY CONJUGATES COMPRISING STING AGONIST (Fri, 02 Nov 2018)
Provided herein are immunoconjugates comprising STING agonists. Also disclosed are methods of making the immunoconjugates and methods of treating cancer using the immunoconjugates.
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6-6 FUSED BICYCLIC HETEROARYL COMPOUNDS AND THEIR USE AS LATS INHIBITORS (Fri, 02 Nov 2018)
The present invention is related to 6-6 Fused Bicyclic Heteroaryl Compounds of the Formula A2 or A1 and their Use as LATS Inhibitors, or a salt, stereoisomer or pharmaceutical composition thereof; wherein the variables are as defined herein (A1 & A2). The present invention further relates to a method of LATS inhibition in a cell population using a compound of Formula A1, or a salt, stereoisomer or pharmaceutical composition thereof. The present invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, their use in the treatment and management of diseases or disorders.
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FUSED INDAZOLE PYRIDONE COMPOUNDS AS ANTIVIRALS (Fri, 02 Nov 2018)
The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus, and reducing the occurrence of serious conditions associated with HBV.
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BIS 2'-5'-RR-(3'F-A)(3'F-A) CYCLIC DINUCLEOTIDE COMPOUND AND USES THEREOF (Fri, 02 Nov 2018)
The present invention provides the cyclic dinucleotide compound 2'2'-RR-(3'F-A)(3'F- A) as a highly active immune stimulator that activates DCs via the cytoplasmic receptor known as STING (Stimulator of Interferon Genes), and compositions and uses thereof.
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SUSTAINED RELEASE DELIVERY SYSTEMS COMPRISING TRACELESS LINKERS (Fri, 26 Oct 2018)
Described herein are drug delivery systems for delivering biologically active agents comprising primary or secondary amines, or a ring nitrogen atom of an azaheteroaryl ring, pharmaceutically acceptable salts thereof, drug delivery reagents related thereto, pharmaceutical compositions comprising the drug delivery systems, and the use of the drug delivery systems as sustained release therapeutics.
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ISOXAZOLE CARBOXAMIDE COMPOUNDS AND USES THEREOF (Fri, 28 Sep 2018)
A compound of Formula (I)) or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating hearing loss or balance disorder: Formula (I) wherein R1 through R3, and L are as defined herein.
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BIOMARKERS AND CAR T CELL THERAPIES WITH ENHANCED EFFICACY (Fri, 28 Sep 2018)
The invention provides compositions and methods improved CAR T cell therapies. Specifically, the invention provides cells with altered expression and/or function of one or more genes, e.g., associated with Tet2, and methods of use therefore. The invention further provides inhibitors of the one or more genes and methods of use therefore in connection with CAR T cells.
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SHP INHIBITOR COMPOSITIONS AND USES FOR CHIMERIC ANTIGEN RECEPTOR THERAPY (Sat, 08 Sep 2018)
Compositions and methods for treating diseases associated with expression of a cancer associated antigen are disclosed. The invention also relates to chimeric antigen receptor (CAR) specific to a cancer associated antigen as described herein, SHP inhibitory molecules, vectors encoding the same, and recombinant immune effector cells comprising the CARs and SHP inhibitory molecules. Methods of administering a genetically modified immune effector cell expressing a CAR that comprises an antigen binding domain that binds to a cancer associated antigen and a SHP inhibitory polypeptide are also disclosed.
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