- AFURESERTIB: Protein kinase B (PKB) inhibitor Oncolytic
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The phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) signaling pathway plays key roles in cellular proliferation and survival. Mutations and alterations in this signal transduction pathway have been described in a variety of solid and hematopoietic malignancies, which may contribute to perpetuation of the disease in a number of ways. Increasing interest in targeting particular facets of this signaling cascade has led to the development of a number of novel anticancer agents, including afuresertib (GSK-2110183), an orally bioavailable pan-inhibitor of the RAC-alpha serine/threonine protein kinase, also referred to as protein kinase B or proto-oncogene c-Akt. The present review summarizes the preclinical and pharmacological aspects of afuresertib and early clinical experience.
- Conkel,Benson
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p. 541 - 546
(2014/12/11)
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- ISOINDOLINONE AND PYRROLOPYRIDINONE DERIVATIVES AS AKT INHIBITORS
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The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the act
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Paragraph 0246; 0247
(2013/04/24)
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- INHIBITORS OF AKT ACTIVITY
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Invented are novel pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 33
(2010/01/30)
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- INHIBITORS OF AKT ACTIVITY
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Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 32; 33
(2010/01/30)
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- INHIBITORS OF AKT ACTIVITY
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Invented are novel hetero-pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 29
(2010/01/30)
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- INHIBITORS OF AKT ACTIVITY
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Invented are novel substituted pyridine compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 8; 32
(2009/04/25)
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- 3-SUBSTITUTED-[1,2,3]BENZOTRIAZINONE COMPOUNDS FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
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This invention relates to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors. These brain networks are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias and in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia and affective disorders. In a particular aspect, the present invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.
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- Observation of a new dimeric amino acid derivative in the reaction of methyl N-BOC-(S)-(3-fluorophenyl)alanate with DIBAL-H and lithio ethyl propiolate
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A novel amino acid dimer 9a was isolated while trying to apply a known reduction/nucleophilic addition sequence. This dimer provided information both on the mechanism of the process and on the dependence of the desired reaction on the stoichiometry of rea
- Jasys, V.John,Urban, Frank J.
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p. 361 - 363
(2007/10/03)
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