PATENTSCOPE: EN_ALL:nmr AND PA:novartis

AZABICYCLO AND DIAZEPINE DERIVATIVES FOR TREATING OCULAR DISORDERS (Fri, 10 May 2019)
The present invention provides in one aspect azabicycio and diazepine derivatives useful as modulators of muscarinic receptors. In another aspect, the present invention provides pharmaceutical compositions for treating ocular diseases, the compositions comprising at least one muscarinic receptor modulator. Formulae (I) & (II):
>> Read More

AZABICYCLO AND DIAZEPINE DERIVATIVES FOR TREATING OCULAR DISORDERS (Fri, 10 May 2019)
The present invention provides in one aspect azabicycio and diazepine derivatives useful as modulators of muscarinic receptors. In another aspect, the present invention provides pharmaceutical compositions for treating ocular diseases, the compositions comprising at least one muscarinic receptor modulator. Formulae (I) & (II):
>> Read More

POLYCYCLIC HERG ACTIVATORS (Fri, 10 May 2019)
The present invention provides a compound of formula (I), in which R1, R2, X and R3 are defined in the summary of the invention, or a pharmaceutically acceptable salt thereof Formula (I); a method for manufacturing the compounds of the invention, and its therapeutic uses linked to the hERG activation. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> Read More

FORMULATION COMPRISING OXAZOLIDIN-2-ONE-PYRIMIDINE DERIVATIVE (Fri, 10 May 2019)
The present invention relates to novel topical pharmaceutical compositions comprising an oxazolidin-2-one-pyrimidine compound of formula (I), a method of manufacturing such compositions, as well as uses of such compositions. The present invention also relates to a novel crystalline form of the compound of formula (I).
>> Read More

POLYCYCLIC HERG ACTIVATORS (Fri, 10 May 2019)
The present invention provides a compound of formula (I), in which R1, R2 and R3 are defined in the Summary of the Invention, or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses linked to hERG activation. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
>> Read More

ANTI-CAR COMPOSITIONS AND METHODS (Fri, 10 May 2019)
The invention provides compositions and methods for treating conditions or diseases associated with expression of a target chimeric antigen receptor (CAR) as described herein. The invention also relates to an anti-target CAR specific to the target CAR as described herein, vectors encoding the same, and recombinant T cells comprising the anti-target CARs of the present invention. The invention also includes methods of administering a genetically modified T cell expressing an anti-target CAR as described herein.
>> Read More

COMPOSITIONS AND METHODS FOR SELECTIVE PROTEIN DEGRADATION (Fri, 26 Apr 2019)
The invention provides compositions including a fusion polypeptide and methods for making a fusion polypeptide that includes a COF1/CRBN-binding polypeptide, COF2/CRBN-binding polypeptide, or COF3/CRBN-binding polypeptide and a heterologous polypeptide of interest.
>> Read More

RAPAMYCIN DERIVATIVES (Fri, 05 Apr 2019)
The disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts, and compositions thereof, wherein the substituents are as defined herein. Also provided are methods of making compounds of formula (I), and methods involving the compounds or compositions for treating disorders and diseases described herein.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More

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.
>> Read More