- COMPOUNDS AND METHOD OF USE
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This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.
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Paragraph 1121
(2019/09/06)
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- N1-PHENYLPROPANE-1,2-DIAMINE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS
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Disclosed are compounds of Formula A-1, or a salt thereof: Formula A-1, where J, K, Q and R1 are as defined herein, which compounds have properties for inhibiting sodium ion channels found in peripheral and sympathetic neurons. Also described are pharmace
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Paragraph 0188-0189
(2017/10/30)
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- Discovery of Novel, Orally Bioavailable β-Amino Acid Azaindole Inhibitors of Influenza PB2
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In our efforts to develop novel small-molecule inhibitors for the treatment of influenza, we utilized molecular modeling and the X-ray crystal structure of the PB2 subunit of the influenza polymerase to optimize a series of acyclic β-amino acid inhibitors, highlighted by compound 4. Compound 4 showed good oral exposure in both rat and mouse. More importantly, it showed strong potency versus multiple influenza-A strains, including pandemic 2009 H1N1 and avian H5N1 strains and showed a strong efficacy profile in a mouse influenza model even when treatment was initiated 48 h after infection. Compound 4 offers good oral bioavailability with great potential for the treatment of both pandemic and seasonal influenza.
- Farmer, Luc J.,Clark, Michael P.,Boyd, Michael J.,Perola, Emanuele,Jones, Steven M.,Tsai, Alice,Jacobs, Marc D.,Bandarage, Upul K.,Ledeboer, Mark W.,Wang, Tiansheng,Deng, Hongbo,Ledford, Brian,Gu, Wenxin,Duffy, John P.,Bethiel, Randy S.,Shannon, Dean,Byrn, Randal A.,Leeman, Joshua R.,Rijnbrand, Rene,Bennett, Hamilton B.,O’Brien, Colleen,Memmott, Christine,Nti-Addae, Kwame,Bennani, Youssef L.,Charifson, Paul S.
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supporting information
p. 256 - 260
(2017/03/08)
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- Substituted pyrazolylpyrazole derivative and use thereof as herbicide
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The invention provides a compound which can effectively control major weeds having higher leaf ages which become a practical problem. Disclosed is a specific pyrazolylpyrazole derivative which is represented by formula (I) and can solve the above-mentioned problem.
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Paragraph 0076; 0077
(2016/10/07)
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- Fused ring compound and use thereof
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The present invention provides a compound represented by the formula: wherein the symbols are as described in the specification, or a salt thereof, which is useful for preventing/treating eicosanoid-associated diseases such as atherosclerosis, diabetes, obesity, atherothrombosis, asthma, fever, pain, cancer, rheumatism, osteoarthritis and atopic dermatitis, and which has an excellent pharmacological action, physicochemical properties, etc.
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Page/Page column 40
(2010/08/07)
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- Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
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Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
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- Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds
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Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
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- Reduction of Cyclopropanecarboxylic Acids by Borane, a Chemoselective Reaction Sensitive to Steric Interactions and Reaction Conditions
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A number of cyclopropanecarboxylic acids have been reduced by borane in tetrahydrofuran to the corresponding cyclopropyl alcohols. The yield was sensitive to the steric influence of the substituents attached to the ring, the reaction temperature, and the
- Sydnes, Leiv K.,Pereira, Paula F. F.,Sandberg, Marcel,Oevreboe, Hans H.
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p. 464 - 474
(2007/10/03)
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- Compounds for inhibiting β-amyloid peptide release and/or its synthesis
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Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis.
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- Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
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Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
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- Compounds for inhibiting β-amyloid peptide release and/or its synthesis
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Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis.
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- N-(aryl/heteroarylacetyl) amino acid esters, pharmaceutical compositions comprising same, and methods for use
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Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
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- NEW ORGANOCOPPER REAGENTS PREPARED UTILIZING HIGHLY REACTIVE COPPER
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Highly reactive copper solutions have been prepared by the lithium naphthalide reduction of copper(I) iodide/trialkylphosphine complexes.These activated copper solutions will react with organic halides under very mild conditions to form stable organocopper reagents.Significantly, the organocopper reagents can contain considerable functionalities such as ester, nitrile, chloride, epoxide, and ketone groups.These functionalized organocopper species undergo many reactions typical of other organocopper species.Intermolecular 1,4-additions, epoxide-opening reactions, and ketone formation with acid chlorides have been successfully achieved.In addition, this methodology has been applied to an intramolecular epoxide-cleavage reaction.The influence of the connecting chain length, substitution pattern, reaction solvent, and CuI/phosphine complex upon the regioselectivity of the intramolecular cyclization is described.
- Rieke, Reuben D.,Wehmeyer, Richard M.,Wu, Tse-Chong,Ebert, Greg W.
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p. 443 - 454
(2007/10/02)
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- DIRECT FORMATION OF EPOXYALKYLCOPPER REAGENTS FROM ACTIVATED COPPER AND EPOXYALKYL BROMIDES AND THEIR INTRAMOLECULAR CYCLIZATIONS
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Epoxyalkylcopper compounds have readily been prepared by the direct oxidative addition of active copper to epoxyalkyl halides.The intramolecular cyclization of the epoxyalkylcopper reagents via an epoxide cleavage process is described.Significantly, many functional groups can be present in the bromoepoxides yielding highly functionalized carbocycles.The regioselectivity of this cyclizations is affected by the connecting chain length, substitution pattern, reaction solvent, and the CuI-phosphine complex used to generate the copper.
- Wu, Tse-Chong,Rieke, Reuben D.
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p. 6753 - 6756
(2007/10/02)
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- LEWIS ACID-INDUCED REACTION OF γ,δ-EPOXY TIN COMPOUNDS
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γ,δ-Epoxy tin compounds underwent divergent reactions depending upon the substitution pattern of the substrates as well as upon Lewis acids used as the inducer.
- Sato, Tadashi,Watanabe, Masami,Murayama, Eigoro
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p. 781 - 788
(2007/10/02)
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- Conformational Analysis of the Cyclopropylacyl, Oxiranylacyl, and Aziridinylacyl Radicals by Electron Spin Resonance Spectroscopy
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A series of ring-substituted cyclopropylacyl, oxiran-2-ylacyl, and aziridin-2-ylacyl radicals have been prepared principally by the reaction of photolytically generated t-butoxyl radicals with the corresponding aldehydes.The e.s.r. spectra show that the cyclopropylacyl ?-radicals exist in s-cis- and s-trans-conformations of approximately equal stability, in which the plane of the acyl group bisects the ring (as it does in the parent aldehyde), and simulation of the spectra through the region of intermediate rates of exchange show that the barrier to rotation is ca. 17.5 kJ*mol-1.The behaviour of the trans-2-ethoxycarbonylcyclopropylacyl and 2,2-dimethylcyclopropylacyl radicals is similar.The oxiranylacyl and trans-3-methyloxiranylacyl radicals exist in the same two conformations with a rather lower barrier, and the N-alkylaziridinylacyl radicals appear to have a lower barrier still.
- Davies, Alwyn G.,Sutcliffe, Roger
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p. 1483 - 1488
(2007/10/02)
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