- VECTOR CONTROL COMPOSITIONS, METHODS AND PRODUCTS UTILIZING SAME
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The present inventions concerns use of a specific methoxyacrylate compound to control mosquitoes, and vector control products comprising that methoxyacrylate compound, in particular the invention relates to a substrate, to a composition, for controlling mosquitoes, and to a specific methoxyacrylate compound, processes for the synthesis of mosquitocidal methoxyacrylate compounds and new intermediates.
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Page/Page column 42; 43; 44
(2019/05/15)
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- Design and synthesis of dihydroisoquinolones for fragment-based drug discovery (FBDD)
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This study describes general synthesis aspects of fragments for FBDD, as illustrated by the dihydroisoquinolones 1-3. Previous Rh(iii) methodology is extended to incorporate amines, heteroatoms (N and S), and substituents (halogen, ester) as potential binding groups and/or synthetic growth points for fragment-to-lead elaboration.
- Palmer, Nick,Peakman, Torren M.,Norton, David,Rees, David C.
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p. 1599 - 1610
(2016/02/10)
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- Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series
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We have recently reported a novel approach to increase cytosolic glucokinase (GK) levels through the binding of a small molecule to its endogenous inhibitor, glucokinase regulatory protein (GKRP) these initial investigations culminated in the identification of 2-(4-((2S)-4-((6-amino-3- pyridinyl)sulfonyl)-2-(1-propyn-1-yl)-1-piperazinyl)phenyl)-1,1,1,3,3, 3-hexafluoro-2-propanol (1, AMG-3969), a compound that effectively enhanced GK translocation and reduced blood glucose levels in diabetic animals. Herein we report the results of our expanded SAR investigations that focused on modifications to the aryl carbinol group of this series. Guided by the X-ray cocrystal structure of compound 1 bound to hGKRP, we identified several potent GK-GKRP disruptors bearing a diverse set of functionalities in the aryl carbinol region. Among them, sulfoximine and pyridinyl derivatives 24 and 29 possessed excellent potency as well as favorable PK properties. When dosed orally in db/db mice, both compounds significantly lowered fed blood glucose levels (up to 58%).
- Nishimura, Nobuko,Norman, Mark H.,Liu, Longbin,Yang, Kevin C.,Ashton, Kate S.,Bartberger, Michael D.,Chmait, Samer,Chen, Jie,Cupples, Rod,Fotsch, Christopher,Helmering, Joan,Jordan, Steven R.,Kunz, Roxanne K.,Pennington, Lewis D.,Poon, Steve F.,Siegmund, Aaron,Sivits, Glenn,Lloyd, David J.,Hale, Clarence,St. Jean, David J.
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p. 3094 - 3116
(2014/05/06)
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- HETEROCYCLIC AMINO BERBAMINE DERIVATIVES, PREPARATION METHOD AND USE THEREOF
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The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.
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Paragraph 0095; 0099
(2013/07/25)
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- HETEROCYCLIC AMINOBERBAMINE DERIVATIVES, THE PREPARATION PROCESS AND USE THEREOF
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The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.
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Paragraph 0108
(2013/07/19)
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- SYNTHESIS OF HALOGENATED THIAZOLE DERIVATIVES OF OLIGO-N-METHYLPYRROLECARBOXAMIDE AND THEIR PHOTOCHEMICAL DNA CLEAVING ACTIVITIES
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Synthesis of various halogenated thiazole derivatives of oligo-N-methylpyrrolecarboxamide and their DNA cleaving activities under UV-A irradiation were described.
- Sakai, Yasuhiro,Matsumoto, Toyomi,Tanaka, Akie,Shibuya, Masayuki
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p. 565 - 573
(2007/10/02)
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