- Novel S1P1 receptor agonists - Part 2: From bicyclo[3.1.0] hexane-fused thiophenes to isobutyl substituted thiophenes
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Previously, we reported on the discovery of a novel series of bicyclo[3.1.0]hexane fused thiophene derivatives that serve as potent and selective S1P1 receptor agonists. Here, we discuss our efforts to simplify the bicyclohexane fused thiophene
- Bolli, Martin H.,Velker, J?rg,Müller, Claus,Mathys, Boris,Birker, Magdalena,Bravo, Roberto,Bur, Daniel,De Kanter, Ruben,Hess, Patrick,Kohl, Christopher,Lehmann, David,Meyer, Solange,Nayler, Oliver,Rey, Markus,Scherz, Michael,Steiner, Beat
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supporting information
p. 78 - 97
(2014/02/14)
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- Thiophene derivatives as S1P1/EDGE1 receptor agonists
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The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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Page/Page column 9
(2010/03/31)
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- NOVEL THIOPHENE DERIVATIVES
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The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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Page/Page column 25-26
(2008/06/13)
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- Phosphorylamides, their preparation and use
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A phosphorylamide derivative represented by the general formula (I): STR1 wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.
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- TETRACYCLIC COMPOUNDS AS DOPAMINE AGONISTS
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A tetracyclic compound of the formula: STR1 wherein A and the atoms to which it is attached and the optional double bond represent a mono-or di-heterocyclic ring selected from: STR2 wherein R 1, R. sup.2, R 3, R 4 and X are specifically defined, which compounds are useful in the treatment of dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of substance abuse and other addictive behavior disorders, cognitive impairment and attention deficit disorder.
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- Generation and Synthetic Utility of Dianions Derived from Thiophencarboxylic Acids
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Thiophen-2- and -3-carboxylic acid are rapidly and regioselectively metallated by lithium di-isopropylamide in tetrahydrofuran at -78 deg C.The resulting dianionic species react with a range of electrophiles to give the expected thiophencarboxylic acid homologues in good-to-excellent yields.
- Knight, David W.,Nott, Andrew P.
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p. 791 - 794
(2007/10/02)
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- Formation and reactivity of dianions derived from 2- and 3-thiophencarboxylic acids
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Dianions (3) and (6) can be generated in high yield from the corresponding thiophencarboxylic acids with lithium diisopropylamide and react with a number of representative electrophiles to give fair to good yields of 5-substituted-thiophen-2-carboxylic acids and 2-substituted thiophen-3-carboxylic acids respectively.
- Knght, David W.,Nott, Andrew P.
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p. 5051 - 5054
(2007/10/02)
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