Abstract:
The invention discloses compounds of formula ( II ): and methods of making the compounds, which are VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Abstract:
Disclosed A process for making ABT-263 (7) an apoptosis promoter having the proper chemical name: N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide, comprising: (a) reacting 4,4-dimethylcyclohexanone, an alkyl formate and a first base to provide (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone and isolating or not isolating the (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone; (b) reacting the (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone, a second base and a first silyl ether protecting group reagent to provide a first protected (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone and isolating or not isolating the first protected (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone; (c) reacting the first protected (2E)-2-(hydroxymethylene)-4,4-dimethylcyclohexanone and 4-chlorophenyl magnesium bromide to provide the first protected (2E)-1-(4-chlorophenyl)-2-(hydroxymethylene)-4,4-dimethylcyclohexanol; and isolating or not isolating the first protected (2E)-1-(4-chlorophenyl)-2-(hydroxymethylene)4,4-dimethylcyclohexanol; and (d) reacting the first protected (2E)-1-(4-chlorophenyl)-2-(hydroxymethylene)-4,4-dimethylcyclohexanol and a first acid to provide 2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-ene-1-carbaldehyde and isolating or not isolating the 2-(4-chlorophenyl)5,5-dimethylcyclohex-1-ene-1-carbaldehyde; (e) reacting 2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-ene-1-carbaldehyde, ethyl 4-piperazin-1-ylbenzoate and a first reducing agent and isolating or not isolating the ethyl 4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoate; (f) reacting ethyl 4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoate and an aqueous third base, and isolating or not isolating the 4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoic acid; and (g) reacting 4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoic acid, 4-(((1R)-3-morpholin-4-yl-1-((phenylthio)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide, a first coupling reagent, and, optionally; a first auxiliary coupling reagent and isolating or not isolating the N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1- ((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide.
Abstract:
Disclosed are Uracil or Thymine derivatives of formula (I) examples of which are: (E)-N-(4-(3-tert-butyl-5-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-2-methoxystyryl)phenyl)methanesulfonamide; (E)-N-(4-(3-tert-butyl-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methoxystyryl)phenyl)methanesulfonamide (Z)-N-(4-(2-(3-tert-butyl-5-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-2-methoxyphenyl)-1-chlorovinyl)phenyl)methanesulfonamide; (E)-1-(3-tert-butyl-5-(4-fluorostyryl)-4-methoxyphenyl) dihydropyrimidine-2,4(1H,3H)-dione; The compounds are for use in treating Hepatitis C
Abstract:
Раскрытыоктагидропирроло[3,4-b]пиррольныепроизводныеформулы I и II, пригодныедлялечениясостоянийилирасстройств, которыепредотвращаютсяилиоблегчаютсяс помощьюлигандоврецепторагистамина-3.Раскрытыоктагидропирроло[3,4-b]пиррольныесоединения, применениетакихсоединений, композиции, содержащиеэтисоединения, испособыполучениятакихсоединений.
Abstract:
Se describe una composición farmacéutica que se puede suministrar por vía oral que comprende un compuesto inhibidor de proteína de la familia de Bcl-2, por ejemplo, ABT-263, un antioxidante de tipo chalcógeno más pesado y un vehículo lípido sustancialmente no acuoso, en la cual dicho compuesto y dicho antioxidante están en solución en el vehículo. La composición es apropiada para administración por vía oral a un individuo en necesidad de lo mismo para tratamiento de una enfermedad caracterizada por sobreexpresión de una o más proteínas anti-apoptóticas de la familia de BcI-2, por ejemplo cáncer.