Patent classifications
C07C235/82
Processes and Intermediates for Preparing a Macrocyclic Protease Inhibitor of HCV
A process for preparing [(1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising: (a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) with brucine or (1R,2S)-()-ephedrine, thus preparing the bis-brucine or bis-(1R,2S)-()-ephedrine salt of (V), and (b) precipitating selectively the bis-brucine or bis-(1R,2S)-()-ephedrine salt of (1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, while the bis-brucine or bis-(1R,2S)-()-ephedrine salt of [(1S,2S)-4-oxo-1,2-cyclopentanedicarboxylic acid stays in solution; (c) liberating the acid II by removal of brucine or (1R,2S)-()-ephedrine from the precipitated salt obtained in step (b).
THICKENING/STABILIZING AGENT AND THICKENED/STABILIZED COMPOSITION USING THE SAME
Provided is a compound that thickens and/or gelatinizes a fluid organic substance to a desired viscosity, or uniformly stabilizes a composition containing the fluid organic substance. Also provided are: a thickening/stabilizing agent including the compound, a thickened/stabilized composition including the thickening/stabilizing agent and a fluid organic substance, and a method for producing the composition. The compound according to the present invention is represented by Formula (1):
(R.sup.2HNOC).sub.4-nR.sup.1(CONHR.sup.3).sub.n(1)
where R.sup.1 is a group resulting from removing four hydrogen atoms from the structural formula of an aromatic hydrocarbon or cyclohexane; R.sup.2 is, independently in each occurrence, an aliphatic hydrocarbon group containing 1 to 4 carbon atoms; R.sup.3 is, independently in each occurrence, an aliphatic hydrocarbon group containing 6 or more carbon atoms; and n is an integer of 1 to 3.
THICKENING/STABILIZING AGENT AND THICKENED/STABILIZED COMPOSITION USING THE SAME
Provided is a compound that thickens and/or gelatinizes a fluid organic substance to a desired viscosity, or uniformly stabilizes a composition containing the fluid organic substance. Also provided are: a thickening/stabilizing agent including the compound, a thickened/stabilized composition including the thickening/stabilizing agent and a fluid organic substance, and a method for producing the composition. The compound according to the present invention is represented by Formula (1):
(R.sup.2HNOC).sub.4-nR.sup.1(CONHR.sup.3).sub.n(1)
where R.sup.1 is a group resulting from removing four hydrogen atoms from the structural formula of an aromatic hydrocarbon or cyclohexane; R.sup.2 is, independently in each occurrence, an aliphatic hydrocarbon group containing 1 to 4 carbon atoms; R.sup.3 is, independently in each occurrence, an aliphatic hydrocarbon group containing 6 or more carbon atoms; and n is an integer of 1 to 3.
Substituted aminobutyric derivatives as neprilysin inhibitors
The present invention provides a compound of formula I; ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Substituted aminobutyric derivatives as neprilysin inhibitors
The present invention provides a compound of formula I; ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Processes and intermediates for preparing a macrocyclic protease inhibitor of HCV
A process for preparing [(1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising: (a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) with brucine or (1R,2S)-()-ephedrine, thus preparing the bis-brucine or bis-(1R,2S)-()-ephedrine salt of (V), and (b) precipitating selectively the bis-brucine or bis-(1R,2S)-()-ephedrine salt of (1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, while the bis-brucine or bis-(1R,2S)-()-ephedrine salt of [(1S,2S)-4-oxo-1,2-cyclopentanedicarboxylic acid stays in solution; (c) liberating the acid II by removal of brucine or (1R,2S)-()-ephedrine from the precipitated salt obtained in step (b).
ARYLCYCLOHEXANEDIONE DERIVATIVE OR SALT THEREOF, PEST CONTROL AGENT CONTAINING SAID COMPOUND, AND METHOD FOR USING SAME
The invention provides compounds represented by the formula (1)
##STR00001##
wherein X and Y are oxygen atoms or sulfur atoms, Z is a hydroxyl group or the like, R.sup.1 and R.sup.2 are alkyl groups and the like, R.sup.4 and R.sup.5 are alkyl groups and the like, R.sup.3 and R.sup.6 are hydrogen atoms and the like, R.sup.7 is a substituted phenyl group or the like, and Q is an aryl group or the like, or salts thereof, pest control agents containing the compounds as active ingredients, and methods for use thereof.
ARYLCYCLOHEXANEDIONE DERIVATIVE OR SALT THEREOF, PEST CONTROL AGENT CONTAINING SAID COMPOUND, AND METHOD FOR USING SAME
The invention provides compounds represented by the formula (1)
##STR00001##
wherein X and Y are oxygen atoms or sulfur atoms, Z is a hydroxyl group or the like, R.sup.1 and R.sup.2 are alkyl groups and the like, R.sup.4 and R.sup.5 are alkyl groups and the like, R.sup.3 and R.sup.6 are hydrogen atoms and the like, R.sup.7 is a substituted phenyl group or the like, and Q is an aryl group or the like, or salts thereof, pest control agents containing the compounds as active ingredients, and methods for use thereof.
ARYL CYCLOHEXANEDIONE DERIVATIVE OR SALT THEREOF, PEST CONTROL AGENT CONTAINING SAME, AND METHOD FOR USE THEREOF
The invention provides compounds represented by the formula (1)
##STR00001## wherein X and Y are oxygen atoms or sulfur atoms, Z is a hydroxyl group or the like, R.sup.1 and R.sup.2 are hydrogen atoms and the like, R.sup.3 is a substituted phenyl group or the like, and Q is a substituted phenyl group or the like, or salts thereof, pest control agents containing the compounds as active ingredients, and methods for use thereof.
ARYL CYCLOHEXANEDIONE DERIVATIVE OR SALT THEREOF, PEST CONTROL AGENT CONTAINING SAME, AND METHOD FOR USE THEREOF
The invention provides compounds represented by the formula (1)
##STR00001## wherein X and Y are oxygen atoms or sulfur atoms, Z is a hydroxyl group or the like, R.sup.1 and R.sup.2 are hydrogen atoms and the like, R.sup.3 is a substituted phenyl group or the like, and Q is a substituted phenyl group or the like, or salts thereof, pest control agents containing the compounds as active ingredients, and methods for use thereof.