- Pyrimido-Benzimidazole Derivatives and the Use Thereof in the Form of Agonists and Antagonists of Melanocortin Receptors
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The invention relates to novel pyrimido-benzimidazole derivatives. Said products exhibit a good affinity for certain melanocortin receptor sub-types, in particular MC4 receptors. Said products represent a particular interest for treating pathological disorders and diseases associated with one or several melanocortin receptors. Pharmaceutical compositions containing said products and the use thereof for a drug preparation are also disclosed.
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Page/Page column 6; 7
(2009/09/05)
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- Pyrimidin-2-oxy-4-one and pyrimidin-2-oxy-4-thione derivatives
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Novel pyrimidin-4-one and pyrimidin-4-thione derivatives of formula (I) wherein A is phenyl, thienyl (including all 3 isomers), thiazolyl or pyridyl; X is oxygen or sulfur; R1is hydrogen, halogen or trimethylsilyl; R2is hydrogen, halogen or trimethysilyl; and at least one of R1and R2is not hydrogen; R3is C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6haloalkenyl, C2-C6alkynyl, C2-C6haloalkynyl, —(CH2)n—C3-C8cycloalkyl which are unsubstitituted or substituted by halogen, C1-C6alkyl or C1-C6haloalkyl, C1-C4alkoxy-C1-C6alkyl; C1-C4alkoxy-C2-C6alkenyl; C1-C4alkoxy-C2-C6alkenyl; C1-C4alkythio-C1-C6alkyl; C1-C4alkylthio-C2-C6alkenyl; C1-C4alkythio-C2-C6alkynyl; mono-C1-C4alkylamin-C1-C6alkyl; mono-C1-C4alkylamin-C1-C6alkenyl; mono-C1-C4alkylamin-C2-C6alkynyl; —(CH2)n—C1-C4alkoxy-C3-C6cycloalkyl; —(CH2)n—C1-C4alkylthio-C3-C6cycloalkyl; —(CH2)2-mono-C1-C4alkylamin-C3-C6cycloalkyl; or N═CR9R10; n is 1, 2, 3, or 4; R4, R5, R6, R7, and R8are each independently of the other hydrogen, C1-C4alkyl, C1-C4haloalkyl or halogen, wherein at least one of the substituents R4-R8must be different from hydrogen; and R9is hydrogen, C1-C6alkyl, C3-C7cycloalkyl, pyridyl, furyl, thienyl or phenyl which is unsubstituted or mono to pentasubstituted by halogen, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; R10is hydrogen, C1-C6alkyl, C3-C7cycloalkyl, pyridyl, furyl, thienyl or phenyl which is unsubstituted or mono to pentasubstituted by halogen, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; and at least one of R9and R10is not hydrogen. The novel compounds have plant-protective properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms, in particular fungi.
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