Non-thiazolidinedione antihyperglycemic agents. Part 4: synthesis of ( )-, (R)-(+)- and (S)-(-)-enantiomers of 2-oxy-3-arylpropanoic acids

. Haigh, David; Birrell, Helen C.; Cantello, Barrie C. C.; Hindley, Richard M.; Ramaswamy, Anantha; Rami, Harshad K.; Stevens, Nicola C. Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, Essex, UK. Tetrahedron: Asymmetry (1999), 10(7), 1335-1351. Publisher: Elsevier Science Ltd., CODEN: TASYE3 ISSN: 0957-4166. Journal written in English. CAN 131:144536 AN 1999:369513 CAPLUS (Copyright (C) 2009 ACS on SciFinder (R)) Abstract The synthesis of a new series of potent 2-oxy-3-arylpropanoic acid antihyperglycemic agents in both racemic and non-racemic form is described. (the biol. activity of these compds. was not reported here). Resoln. of racemic acids is accomplished via amide formation with either (S)-2-phenylglycinol or (S)-4-benzyl-2-oxazolidinone as complementary resolving agents. The target compds. were ?-alkoxy-4-[2-[(2-benzoxazolyl)amino]ethoxy]benzenepropanoic acid derivs.

Facile biocatalytic reduction of the carbon-carbon double bond of 5-benzylidenethiazolidine-2,4-diones. Synthesis of ( )-5-(4-{2-[methyl(2-pyridyl)amino]ethoxy}benzyl)thiazolidine-2,4-dione (BRL 49653), its (R)-(+)-enantiomer and analogs.

Cantello, Barrier C. C.; Eggleston, Drake S.; Haigh, David; Haltiwanger, R. Curtis; Heath, Catherine M.; Hindley, Richard M.; Jennings, Keith R.; Sime, John T.; Woroniecki, Stefan R. SmithKline Beecham Pharmaceuticals, Surrey, UK. Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1994), (22), 3319-24. Publisher: Royal Society of Chemistry, CODEN: JCPRB4 ISSN: 0300-922X. Journal written in English. CAN 122:105736 AN 1995:237497 CAPLUS (Copyright (C) 2009 ACS on SciFinder (R)) Abstract A novel biotransformation system for the redn. of carbon-carbon double bonds in 5-benzylidenethiazolidine-2,4-diones to give the corresponding 5-benzylthiazolidine-1,4-diones, using whole cells of red yeasts, is described. These reduced compds., which are recovered in good yield, are of potential use in the treatment of non-insulin dependent diabetes mellitus. The mild reaction conditions developed allow redn. of 5-benzylidenethiazolidine-2,4-diones contg. other functionalities which are not compatible with alternative redn. methods. The biocatalytic redn. is enantioselective and the synthesis of R-(+)-5-(4-{2-[methyl(2-pyridyl)amino]ethoxy}benzyl)thiazolidine-2,4-dione by Rhodotorula rubra CBS 6469 and structure confirmation by X-ray crystallog. is detailed. Optimization of reaction conditions (including immobilization) for these whole cell redn. system is described.

Eochaid ua Flainn is Eochaid ua Flannucáin: Súil Úr ar an bhFianaise

The evidence for two poets on record in the tenth century is reconsidered. The argument is made that they can be identified as one person, the poet Eochaid ua Flannucáin, a member of the religious community of Armagh and founder of a dynasty which governed the centre of the Irish church for over 150 years.

Lacustrine evidence of Holocene environmental change from three Faroese lakes: a multiproxy XRF and stable isotope study

The vegetation history of the Faroe Islands has been investigated in numerous studies all broadly showing that the early-Holocene vegetation of the islands largely consisted of fellfield with gravely and rocky soils formed under a continental climate which shifted to an oceanic climate around 10,000 cal yr BP when grasses, sedges and finally shrubs began to dominant the islands. Here we present data from three lake sediment cores and show a much more detailed history from geochemical and isotope data. These data show that the Faroe Islands were deglaciated by the end of Younger Dryas (11,700 10,300 cal yr BP), at this time relatively high sedimentation rates with high delta C-13 imply poor soil development. delta C-13, Ti and chi data reveal a much more stable and warm mid-Holocene until 7410 cal yr BP characterised by increasing vegetation cover and build up of organic soils towards the Holocene thermal maximum around 7400 cal yr BP. The final meltdown of the Laurentide ice sheet around 7000 cal yr BP appears to have impacted both ocean and atmospheric circulation towards colder conditions on the Faroe Islands. This is inferred by enhanced weathering and increased deposition of surplus sulphur (sea spray) and erosion in the highland lakes from about 7400 cal yr BP. From 4190 cal yr BP further cooling is believed to have occurred as a consequence for increased soil erosion due to freeze/thaw sequences related to oceanic and atmospheric variability. This cooling trend appears to have advanced further from 3000 cal yr BR A short period around 1800 cal yr BP appears as a short warm and wet phase in between a general cooling characterised by significant soil erosion lasting until 725 cal yr BP. Interestingly, increased soil erosion seems to have begun at 1360 cal yr BP, thus significantly before the arrival of the first settlers on the Faroe Island around 1150 cal yr BP, although additional erosion took place around 1200 cal yr BP possibly as a consequence of human activities. Hence it appears that if humans caused a change in the Faroe landscape in terms of erosion they in fact accelerated a process that had already started. Soil erosion was a dominant landscape factor during the Little Ice Age, but climate related triggers can hardly be distinguished from human activities. (c) 2010 Elsevier Ltd. All rights reserved.

Intellectual Property management in publicly funded R&D centres—A comparison of university-based and company-based research centres

Recent thinking on open innovation and the knowledge-based economy have stressed the importance of external knowledge sources in stimulating innovation. Policy-makers have recognised this, establishing publicly funded Centres of R&D Excellence with the objective of stimulating industry–science links and localised innovation spillovers. Here, we examine the contrasting IP management practices of a group of 18 university- and company-based R&D centres supported by the same regional programme. Our analysis covers all but one of the Centres supported by the programme and suggests marked contrasts between the IP strategies of the university-based and company-based centres. This suggests the potential for very different types of knowledge spillovers from publicly funded R&D centres based in different types of organisations, and a range of alternative policy approaches to the future funding of R&D centres depending on policy-makers’ objectives.