- KINASE ANTAGONISTS AND METHODS FOR MAKING AND USING THEM
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Disclosed herein are small molecule compounds that are SGK1 antagonists, formulations and pharmaceutical compositions comprising the compounds, and methods of making and using them, for treating, ameliorating, preventing, reversing or slowing the progression of: a cancer, a tumor, a metastasis or a dysplastic or a dysfunctional cell condition responsive to inhibition of a kinase enzyme of the AGC group of kinases including SGK1, by administration of an AGC kinase inhibitor or antagonist.
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Page/Page column 127; 129
(2020/02/19)
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- PYRAZINE CARBAMATES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
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Pyridine carbamates, pharmaceutical compositions containing pyridine carbamates, and uses of the pyridine carbamates and pharmaceutical compositions for modulating GluN2B receptors and for treating diseases, disorders, and medical conditions mediated by GluN2B receptor activity.
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Paragraph 0172; 0222; 0224; 0235-0236
(2020/12/25)
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- SUBSTITUTED HETEROAROMATIC PYRAZOLO-PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
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Substituted Pyrazolo-pyridines as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B receptor activity.
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Page/Page column 93-94
(2020/12/30)
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- PYRIDINE CARBAMATES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
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Pyridine carbamates, pharmaceutical compositions containing pyridine carbamates, and uses of the pyridine carbamates and pharmaceutical compositions for modulating GluN2B receptors and for treating diseases, disorders, and medical conditions mediated by G
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Page/Page column 79-80
(2020/12/30)
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- SUBSTITUTED PYRAZOLO[4,3-b]PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
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Substituted pyrazolo[4,3-b]pyridines as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B rece
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Page/Page column 62
(2020/12/30)
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- SUBSTITUTED PYRAZOLO[4,3-b]PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
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Substituted pyrazolo[4,3-b]pyridines as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B receptor activity.
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Paragraph 0279; 0280
(2020/12/25)
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- PYRAZINE CARBAMATES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
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Pyridine carbamates, pharmaceutical compositions containing pyridine carbamates, and uses of the pyridine carbamates and pharmaceutical compositions for modulating GluN2B receptors and for treating diseases, disorders, and medical conditions mediated by GluN2B receptor activity.
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Page/Page column 53
(2020/12/30)
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- SUBSTITUTED PYRAZOLO-PYRAZINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
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Substituted PYRAZOLO-PYRAZINES as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B receptor a
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Page/Page column 57-58
(2020/12/30)
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- SUBSTITUTED PYRAZOLO-PYRIDINE AMIDES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
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Substituted Pyrazolo-pyridines as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B receptor activity.
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Page/Page column 103
(2020/12/30)
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- SUBSTITUTED PYRIDINE AND PYRIMIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
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Substituted pyrimidine and pyridines as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.
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Paragraph 0348-0351
(2019/10/20)
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- PYRIDINE SULFONAMIDES
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The present invention provides compounds of Formula (I), as defined in the specification, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders, cough, or itch. Also provided are pharmaceutical compositions containing compounds of the present invention.
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- Bicyclic ketone sulfonamide compounds
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The present invention provides compounds of a formula (I), wherein a formula (II) is defined in the specification, and provides an enantiomer, diastereomer, atropisomer thereof, or a mixture thereof,or pharmaceutically acceptable salts thereof, that are i
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Paragraph 1143-1145
(2018/01/20)
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- HETEROCYCLIC COMPOUNDS AND THEIR USE AS INHIBITORS OF PI3K ACTIVITY
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Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia ( T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
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Page/Page column 189
(2012/01/15)
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- Substituted imidazol-pyridazine derivatives
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The present invention relates to compounds of formula wherein A is an unsubstituted or substituted cyclic group; and R is hydrogen or lower alkyl; or a pharmaceutically acceptable acid addition salt thereof. These compounds are NMDA NR-2B receptor subtype specific blockers and are useful in the treatment of neurodegeneration, depression and pain.
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- Imidazole derivatives
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Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.
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