- PYRAZOLOPYRIMIDINE DERIVATIVE AS SELECTIVE TRK INHIBITOR
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The present invention discloses a compound of formula (II), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to use thereof in preparing a medicament for treating solid tumor-related diseases.
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Paragraph 0113; 0114
(2021/08/05)
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- Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments
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Efficient syntheses of chiral fragments derived from chiral amino alcohols are described. Several unique scaffolds were readily accessed in 1-5 synthetic steps leading to 45 chiral fragments, including oxazolidinones, morpholinones, lactams, and sultams. These fragments have molecular weights ranging from 100 to 255 Da and are soluble in water (0.085 to >15 mM).
- Haftchenary, Sina,Nelson, Shawn D.,Furst, Laura,Dandapani, Sivaraman,Ferrara, Steven J.,Bo?kovi?, ?arko V.,Figueroa Lazú, Samuel,Guerrero, Adrian M.,Serrano, Juan C.,Crews, Demarcus K.,Brackeen, Cristina,Mowat, Jeffrey,Brumby, Thomas,Bauser, Marcus,Schreiber, Stuart L.,Phillips, Andrew J.
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supporting information
p. 569 - 574
(2016/10/06)
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- A concise and efficient synthesis of substituted morpholines
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A simple and efficient method has been developed for the synthesis of substituted morpholines by a sequence of coupling, cyclization, and reduction reactions of easily available amino alcohols and α-halo acid chlorides. Various mono-, di-, and trisubstituted morpholines, spiro morpholines, and ring-fused morpholines, as well as morpholine homologues, were synthesized in good to excellent yields by a single methodology under similar reaction conditions. The method was also used in a multigram synthesis of (3S)-3-methylmorpholine.
- Dugar, Sundeep,Sharma, Amit,Kuila, Bilash,Mahajan, Dinesh,Dwivedi, Sandeep,Tripathi, Vinayak
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supporting information
(2015/02/19)
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- AMINO HETEROARYL COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).
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Page/Page column 49
(2011/08/08)
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- PYRAZOLE DERIVATIVE
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A compound represented by Formula (I): wherein Ar1 represents Formula (II): Ar2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
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Page/Page column 149
(2010/11/27)
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- In vitro inhibition studies of phytoene desaturase by bleaching ketomorpholine derivatives
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The herbicidal activities of homochiral steroisomeric 5-methyl-2-(3-trifluoromethylbenzyl)-3-ketomorpholine derivatives were investigated in vitro as inhibitors of phytoene desaturase, a key enzyme in carotenoid biosynthesis. It was demonstrated that ketomorpholines are classical bleaching compounds which directly inhibit phytoene desaturase, accumulating phytoene at the expense of colored carotenoids. Ketomorpholines interact with phytoene desaturase in a noncompetitive manner with respect to phytoene. A structure-activity investigation for in vitro inhibition of phytoene desaturase activity revealed that the relative and absolute stereochemistry is important for optimum inhibition for the 5-methyl derivatives, and that the distance of the phenyl group from the ketomorpholine ring is critical for the inhibitory potential. The average herbicidal score on 7 weeds and the in vitro I50 values related very well with the exception of two compounds. It was postulated that the discrepancies may possibly occur through modification in plants to compounds that are either more or less active herbicides.
- Sandmann, Gerhard,Mitchell, Glynn
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p. 138 - 141
(2007/10/03)
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