PATENTSCOPE: EN_ALL:nmr AND PA:GlaxoSmithKline

COMPOUNDS USEFUL IN HIV THERAPY (Fri, 10 May 2019)
The invention relates to compounds of Formulas (I), (II) and (III) salts thereof, pharmaceutical compositions thereof, as well as methods of treating, curing or preventing HIV in subjects.
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MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE (Fri, 10 May 2019)
Provided are IDO1 inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
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METHODS FOR ADMINISTERING STING AGONISTS (Fri, 12 Apr 2019)
The present invention relates to methods of treating disease states, including cancer, in a human comprising systemically administering a STING agonist, or a pharmaceutically acceptable salt thereof, to said human.
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MODULATORS OF STIMULATOR OF INTERFERON GENES (STING) (Fri, 12 Apr 2019)
Disclosed are compounds having the formula: (I) wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, R17, Rx, and Ry are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
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BENZOFURAN DERIVATIVES AND THEIR USE AS BROMODOMAIN INHIBITORS (Fri, 12 Apr 2019)
The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
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2,3-DIHYDROBENZOFURANS AS BOROMODOMAIN INHIBITORS (Fri, 12 Apr 2019)
The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
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MODULATORS OF STIMULATOR OF INTERFERON GENES (STING) USEFUL IN TREATING HIV (Fri, 12 Apr 2019)
Disclosed are compounds having the formula: (I-N) wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, and R17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof, along with combinations thereof, all of which are useful in HIV therapies.
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CHEMICAL COMPOUNDS (Fri, 12 Apr 2019)
Compounds of Formula (I), specifically hepatitis B virus and/or hepatitis D virus inhibitors, more specifically compounds that inhibit HBe antigen and HBs antigen in a subject, for the treatment of viral infections, and methods of preparing and using such compounds.
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ROR-GAMMA INHIBITORS (Fri, 05 Apr 2019)
The present invention relates to compounds of formula I and pharmaceutical compositions comprising compounds of formula I. Compounds of Formula I are useful in treatment of inflammatory, metabolic or autoimmune diseases which are mediated by RORy.
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COMBINATION TREATMENT FOR CANCER (Fri, 22 Mar 2019)
Disclosed herein is a method of treating cancer, such as multiple myeloma, involving the combination of an anti-BCMA antigen binding protein (e.g., an anti-BCMA antibody) and an immunomodulatory drug (e.g. pomalidomide or lenalidomide). The combinations can also include an anti-inflammatory compound (e.g. dexamethasone).
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COMBINATION TREATMENT FOR CANCER (Fri, 22 Mar 2019)
Disclosed herein is a method of treating cancer, such as multiple myeloma, involving the combination of an anti-BCMA antigen binding protein (e.g., an anti-BCMA antibody) and a proteasome inhibitor (e.g. bortezomib). The combinations can also include an anti-inflammatory compound (e.g. dexamethasone).
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CHEMICAL COMPOUNDS (Fri, 22 Mar 2019)
The invention is directed to substituted salicylamide derivatives. Specifically, the invention is directed to compounds according to FormµLa (I): wherein R, R1,P, X, Y, and Z are as defined herein; or a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of CD73 and can be usefµL in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, the treatment of HIV, autoimmune diseases, infections, atherosclerosis, and ischemia–reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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5-(1 H-BENZO[D]IMIDAZO-2-YL)-PYRIDIN-2-AMINE AND 5-(3H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-PYRIDIN-2-AMINE DERIVATIVES AS C-MYC AND P300/CBP HISTONE ACETYLTRANSFERASE INHIBITORS FOR TREATING CANCER (Fri, 15 Mar 2019)
The invention is directed to substituted 5-(1H-benzo[d]imidazo-2-yl)- pyridin-2-amine and 5-(3H-imidazo[4,5-b]pyridin-6-yl)-pyridin-2-amine derivatives. Specifically, the invention is directed to compounds according to Formula (lb) wherein R', R2', R3', R4', Rs', R6', R7', and X1' are as defined herein; or a salt thereof including a pharmaceutically acceptable salt thereof. The compounds of the invention decrease MYC protein (c-MYC) in cells and/or inhibit p300/CBP histone acetyltransferase and can be useful in the treatment of cardiac hypertrophy, diabetes, obesity & nonalcoholic fatty liver disease, HIV, polycystic kidney disease, inflammatory diseases, ankylosing spondylitis, psoriasis, psoriatic arthritis, rheumatoid arthritis, Crohn's disease, multiple sclerosis, cancer and pre-cancerous syndromes, and diseases associated with dysregulation of Myc or inhibition of p300/CBP histone acetyltransferase. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention still further discloses methods of reducing MYC protein (c-MYC) in cells and inhibiting p300/CBP histone acetyltransferase activity, and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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NOVEL COMPOUNDS (Fri, 22 Feb 2019)
The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by mycobacterium, such as tuberculosis.
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NOVEL TETRAZOLE COMPOUNDS AND THEIR USE IN THE TREATMENT OF TUBERCULOSIS (Fri, 22 Feb 2019)
The invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by mycobacterium, such as tuberculosis.
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NOVEL COMPOUNDS (Fri, 22 Feb 2019)
The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by mycobacterium, such as tuberculosis.
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NOVEL COMPOUNDS (Fri, 22 Feb 2019)
The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by mycobacterium, such as tuberculosis
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INDAZOLE DERIVATIVES USEFUL AS PERK INHIBITORS (Fri, 01 Feb 2019)
The invention is directed to substituted indazole derivatives and uses thereof. Specifically, the invention is directed to compounds according to Formula I and the use of compounds of Formula (I) in treating disease states (I) wherein R1, R2, R3, R4, R5, are as defined herein; or a salt thereof including a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, Parkinson disease, diabetes, metabolic syndrome, metabolic disorders, Huntington's disease, Creutzfeldt-Jakob Disease, and related prion diseases, fatal familial insomnia, Gerstmann-Straussler-Scheinker syndrome, and related prion diseases, amyotrophic lateral sclerosis, progressive supranuclear palsy, myocardial infarction, cardiovascular disease, inflammation, organ fibrosis, chronic and acute diseases of the liver, fatty liver disease, liver steatosis, liver fibrosis, chronic and acute diseases of the lung, lung fibrosis, chronic and acute diseases of the kidney, kidney fibrosis, chronic traumatic encephalopathy (CTE), neurodegeneration, dementias, frontotemporal dementias, tauopathies, Pick's disease, Neimann-Pick's disease, amyloidosis, cognitive impairment, atherosclerosis, ocular diseases, neurological disorders, pain, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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PYRIDINE-3-SULFONAMIDE COMPOUNDS AS PI3-KINASE INHIBITORS (Fri, 01 Feb 2019)
The invention is directed to compounds of formula (I) and salts thereof. The compounds are inhibitors of kinase activity, in particular PI3-kinase activity.
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IMMUNOGENIC COMPOSITION (Fri, 25 Jan 2019)
The disclosure provides synthetic (e.g. recombinant) pneumococcal saccharides comprising one or more repeat unit(s) →4)-β-D-Glcp-(1→4)-[Gro-(2→P→3)]-β-D-Galp-(1→4)-β-L-Rhap- (1→. Also provided are conjugates comprising a →4)-β-D-Glcp-(1→4)-[Gro-(2→P→3)]-β-D- Galp-(1→4)-β-L-Rhap-(1→, immunogenic compositions, vaccines and their use in preventing or treating infection by Streptococcus pneumoniae.
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