- Benzothiophene-flanked diketopyrrolopyrrole polymers: Impact of isomeric frameworks on carrier mobilities
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Exploring new building blocks for solution-processable polymeric semiconductors has attracted much attention. We herein develop two isomeric benzothiophene-flanked diketopyrrolopyrrole polymers with different linkage positions and further systematically study the electronic structures, optical properties, and field-effect characteristics. Both polymers exhibit typical p-type transport characteristics with the highest mobility being up to 0.80 cm2 V-1 s-1. Our results suggest that the isomeric backbones for conjugated polymers greatly affect charge transport properties.
- Huang, Jianyao,Liu, Xiaotong,Gao, Dong,Wei, Congyuan,Zhang, Weifeng,Yu, Gui
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p. 83448 - 83455
(2016/10/22)
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- Novel 1-Heteroaryl-3-Azabicyclo[3.1.0]Hexanes Methods For Their Preparation And Their Use As Medicaments
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The invention provides novel 1-heteroaryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervo
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Paragraph 0310; 0311
(2014/10/16)
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- CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, R0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from -(C1-C4) alkylene-, -S-, -CH(OH)-, or -O-; A is methylene, -S-, -O-, or -NH-; and the other substituents are as defined in the claims.
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Page/Page column 63
(2008/06/13)
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- Potent, orally active aldose reductase inhibitors related to zopolrestat: Surrogates for benzothiazole side chain
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A broad structure-activity program was undertaken in search of effective surrogates for the key benzothiazole side chain of the potent aldose reductase inhibitor, zopolrestat (1). A structure-driven approach was pursued, which spanned exploration of three areas: (1) 5/6 fused heterocycles such as benzoxazole, benzothiophene, benzofuran, and imidazopyridine; (2) 5- membered heterocycles, including oxadiazole, oxazole, thiazole, and thiadiazole, with pendant aryl groups, and (3) thioanilide as a formal equivalent of benzothiazole. Several benzoxazole- and 1,2,4-oxadiazole- derived analogues were found to be potent inhibitors of aldose reductase from human placenta and were orally active in preventing sorbitol accumulation in rat sciatic nerve, in an acute test of diabetic complications. 3,4-Dihydro-4- oxo-3-[(5,7-difluoro-2-benzoxazolyl)methyl]-1-phthalazineacetic acid (124) was the best of the benzoxazole series (IC50 = 3.2 x 10-9 M); it suppressed accumulation of sorbitol in rat sciatic nerve by 78% at an oral dose of 10 mg/kg. Compound 139, 3,4-dihydro-4-oxo-3-[[(2-fluorophenyl)-1,2,4- oxadiazol-5-yl]methyl]-1-phthalazineacetic acid, with IC50 -8 M, caused a 69% reduction in sorbitol accumulation in rat sciatic nerve at an oral dose of 25 mg/kg. The thioanilide side chain featured in 3-[2-[[3- (trifluoromethyl)phenyl]amino]-2-thioxoethyl]-3,4-dihydro-4-oxo-1- phthalazineacetic acid (195) proved to be an effective surrogate for benzothiazole. Compound 195 was highly potent in vitro (IC50 = 5.2 x 10-8 M) but did not show oral activity when tested at 100 mg/kg. Additional structure-activity relationships encompassing a variety of heterocyclic side chains are discussed.
- Mylari,Beyer,Scott,Aldinger,Dee,Siegel,Zembrowski
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p. 457 - 465
(2007/10/02)
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