- IMIDAZO[1,2-A]PYRAZINE MODULATORS OF THE ADENOSINE A2A RECEPTOR
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The present invention relates to the compound of formula (I) and salts, stereoisomers, tautomers, isotopologues,or N-oxides thereof. The present invention is further concerned with the use of such a compound or salt, stereoisomer, tautomer, isotopologues,or N-oxide thereof as medicament and a pharmaceutical composition comprising said compound.
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Page/Page column 78
(2019/01/17)
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- CANCER TREATMENTS TARGETING CANCER STEM CELLS
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Disclosed are compounds, methods, compositions, and kits that allow for treating cancer by, e.g., targeting cancer stem cells. In some embodiments, the cancer is colorectal cancer, gastric cancer, gastrointestinal stromal tumor, ovarian cancer, lung cancer, breast cancer, pancreatic cancer, prostate cancer, testicular cancer, or lymphoma. In some embodiments, the cancer is liver cancer, endometrial cancer, leukemia, or multiple myeloma. The compounds utilized in the disclosure are of Formula (0), (O'), and (I):
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Paragraph 0331; 0524-0525
(2019/11/19)
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- HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES
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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.
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Paragraph 000170; 000184; 000196
(2016/05/02)
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- Heterocyclic compound with Wnt signal path inhibitory activity and application thereof
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The invention provides a heterocyclic compound with Wnt signal path inhibitory activity. The heterocyclic compound and chemically acceptable salt, isotope, isomer and a crystal structure thereof are provided with a structure shown as the general formula I (see the formula in the description). The invention further provides application of the heterocyclic compound with the Wnt signal path inhibitory activity. The heterocyclic compound with the Wnt signal path inhibitory activity serves as effective antagonist of a Wnt signal path, and can be used for treating or preventing diseases caused by abnormity of the Wnt signal path.
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Paragraph 0125; 0126; 0127
(2016/10/08)
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- ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME
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The present invention refers to novel compounds and is provided to improve quality of an organic electroluminescent including, the present invention according to compounds are organic layer for organic electroluminescence device, preferably light-emitting
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Paragraph 0114; 0115; 0116; 0117; 0118
(2016/10/31)
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- ORGANIC COMPOUNDS AND ORGANIC ELECTRO LUMINESCENCE DEVICE COMPRISING THE SAME
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The present invention relates to novel organic compounds represented by chemical formula 1 and an organic electro-luminescent device comprising the same. The organic compound is included in one or more organic layers and ideally a light emitting layer, thereby improving the light emitting efficiency, the driving voltage and the lifespan of the device.COPYRIGHT KIPO 2015
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Paragraph 0100-0103
(2016/10/24)
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- ORGANIC COMPOUNDS AND ORGANIC ELECTRO LUMINESCENCE DEVICE COMPRISING THE SAME
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The present invention relates to organic compounds and an organic electroluminescent device comprising the same. According to the present invention, the organic compounds can improve light emitting efficiency, driving voltage, lifespan, etc. of the organic electroluminescent device by being used in an organic layer, desirably a light emitting layer of the organic electroluminescent device. The compounds are represented by chemical formula 1.COPYRIGHT KIPO 2015
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Paragraph 0282; 0283; 0284
(2016/10/08)
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- NEW ORGANIC COMPOUNDS AND ORGANIC ELECTRO LUMINESCENCE DEVICE COMPRISING THE SAME
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The present invention refers to a fullerene derivative is denoted by chemical formula 1 a and is provided to improve quality of an organic electroluminescent including, a fullerene derivative is denoted by chemical formula 1 a at least one organic layer, preferably light-emitting layer by the inclusion of, the P-type semiconductor layer, , driving voltage, can be enhanced life: [Formula 1] (Said formula 1 in, R 1 to R 5 and Ar 1 each that are defined in the detailed description as).
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Paragraph 0117-0121
(2016/10/09)
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- NOVEL 3-INDOL SUBSTITUTED DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE
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The present invention relates to compound of Formula (I) or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula (I).
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Page/Page column 92; 93
(2016/01/12)
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- Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase
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Spleen tyrosine kinase (Syk) is an attractive drug target in autoimmune, inflammatory, and oncology disease indications. The most advanced Syk inhibitor, R406, 1 (or its prodrug form fostamatinib, 2), has shown efficacy in multiple therapeutic indications, but its clinical progress has been hampered by dose-limiting adverse effects that have been attributed, at least in part, to the off-target activities of 1. It is expected that a more selective Syk inhibitor would provide a greater therapeutic window. Herein we report the discovery and optimization of a novel series of imidazo[1,2-a]pyrazine Syk inhibitors. This work culminated in the identification of GS-9973, 68, a highly selective and orally efficacious Syk inhibitor which is currently undergoing clinical evaluation for autoimmune and oncology indications.
- Currie, Kevin S.,Kropf, Jeffrey E.,Lee, Tony,Blomgren, Peter,Xu, Jianjun,Zhao, Zhongdong,Gallion, Steve,Whitney, J. Andrew,Maclin, Deborah,Lansdon, Eric B.,Maciejewski, Patricia,Rossi, Ann Marie,Rong, Hong,Macaluso, Jennifer,Barbosa, James,Di Paolo, Julie A.,Mitchell, Scott A.
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p. 3856 - 3873
(2014/05/20)
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- NOVEL BI-RING PHENYL-PYRIDINES/PYRAZINES FOR THE TREATMENT OF CANCER
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The invention provides novel compounds having the general formula: wherein R1, R2 and R3 are as described herein, compositions including the compounds and methods of using the compounds.
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Page/Page column 66
(2014/07/07)
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- IMIDAZOPYRIDIN-2-ONE DERIVATIVES
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A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
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Page/Page column 23
(2011/04/24)
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- PYRAZOLOPYRIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
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Compounds of Formula (I), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer or inflammation mediated by lipid kinases. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 55
(2010/07/10)
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- BIARYL SUBSTITUTED DIAZABICYCLOALKANE DERIVATIVES
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The invention relates biaryl substituted diazabicycloalkanes of foraula (I), and more particularly bicycloheteroaryl substituted fused diazabicycloalkane derivatives, compositions comprising such compounds, and such compounds for use for treating or preve
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Page/Page column 42
(2009/06/27)
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- FUSED BICYCLOHETEROCYCLE SUBSTITUTED AZABICYCLIC ALKANE DERIVATIVES
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The invention relates to fused bicycloheterocycle substituted azabicyclic alkane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
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Page/Page column 16
(2008/06/13)
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- PROTEIN KINASE INHIBITORS
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Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
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Page/Page column 57-58
(2010/11/28)
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