- Synthesis of a Series of Diaminoindoles
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A selection of 3,4-diaminoindoles were required for a recent drug discovery project. To this end, a 10-step synthesis was developed from 4-nitroindole. This synthesis was subsequently adapted and used to synthesize 3,5-; 3,6-; and 3,7-diaminoindoles from
- Martin, James S.,Mackenzie, Claire J.,Gilbert, Ian H.
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p. 11333 - 11340
(2021/09/02)
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- NEW SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS
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The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1 ), and their use as pharmaceutical compositions.
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Page/Page column 116
(2008/12/07)
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- NOVEL FUSED PYRROLE DERIVATIVE
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Disclosed is a compound represented by the formula (1) below which is useful as a glucocorticoid receptor function regulating agent, an anti-inflammatory drug or an antidiabetic drug, or a pharmaceutically acceptable salt thereof. (1) [In the formula, R1 represents an aralkyl group or the like; R2 represents a hydrogen atom or the like; -W4=W5-W6=W7- represents a group expressed as the following formula: -CR4=CR5-CR6=CR7- (wherein R4, R5, R6 and R7 independently represent a group expressed as the following formula: -E-A (wherein E represents a single bond and A represents a hydrogen atom, a nitro group or the like)) or the like; R8 represents a group expressed as the following formula: -OR11 (wherein R11 represents a hydrogen atom or the like) or the like; R9 represents a trifluoromethyl group or the like; and R10 represents a group expressed as the following formula: -[C(R13)R14]n-R15 (wherein R13 and R14 independently represent a hydrogen atom or the like, n represents an integer of 0-10, and R15 represents a group expressed as the following formula: -N(R18)R19 (wherein R18 and R19 represent a monocyclic nitrogen-containing heterocyclic ring or the like together with a nitrogen atom to which they are bonded) or the like).]
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Page/Page column 69
(2010/11/26)
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- Indole-3-carboxamides as glucokinase activators
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The present invention provides glucokinase activators of formula I: wherein R1, R2 and R3 are defined in the specification. Glucokinase activators are useful for increasing insulin secretion in the treatment of type II diabetes.
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