Abstract:
A process for preparing [(1 R ,2 R )-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 (1 R ,2 R )-4-oxo-1,2-cyclopentanedicarboxylic acid II, while the bis-brucine or bis-( 1R,2S ) - (-)-ephedrine salt of [(1 S ,2 S )-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).
Abstract:
The present invention provides processes for preparing a prostacyclin analogue of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R10 is a linear or branched C1-6 alkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound.
Abstract:
A compound which has cytokine production inhibitory activity and is useful for the treatment of diseases in which cytokine participates. The compound is represented by the following general formula (I) [wherein A represents an optionally substituted cyclic compound group; the partial structure -D---E- represents -CH2CH2- or -CH=CH-; W represents -CH2-, -CH2CH2-, -CH=CH-, or -CH=; the partial structure >X---Y- represents >CH-(CH2)n-, >C=CH-, >CH-CH2-CH(OH)-, >CH-CH2-C(=O)-, >CH-O-, or >CH-O-CO-, provided that when W is -CH=, then X---Y- represents C-(CH2)p-; Z represents a divalent aliphatic hydrocarbon group; R?1 and R2¿ are the same or different and each represents hydrogen, hydroxy, alkoxy, or alkoxyalkoxy; and m is 0 or 1]. (I)
Abstract:
This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.
Abstract:
Methods for preparing substituted aromatic carboxylic acid esters are described. In particular, the invention relates a method for preparing a nitro-substituted aromatic carboxylic acid ester of Formula (A). Additionally the invention relates to a method for preparing a thioether-substituted aromatic carboxylic acid ester of Scheme (B). Such aryl esters are useful in the preparation of various agrochemicals and agrochemical intermediates.
Abstract:
The present invention relates to a bioreactive agent comprising a detectable moiety linked to a photo-reactive moiety, wherein said photoreactive moiety comprises at least one group covalently bound to a substrate to form a conjugate that can be selectively photocleaved to release said substrate, wherein said substrate is selected from proteins, peptides, amino acids, lipids, cells, virus particles, fatty acids, nucleic acids, nucleotides, nucleosides, oligonucleotides, polysaccharides and inorganic molecules.
Abstract:
Fuel compositions containing a major amount of hydrocarbons boiling in the gasoline or diesel range and an effective deposit-controlling amount of a poly(oxyalkylene) aromatic ester having formula (I) where A1 is nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms; R1 and R2 are independently hydrogen, hydroxy, lower alkyl, or lower alkoxy; R3 and R4 are independently hydrogen or lower alkyl, and each R3 and R4 is independently selected in each -O-CHR3-CHR4- unit; R5 is hydrogen, alkyl having 1 to 100 carbon atoms, phenyl, aralkyl having 7 to 100 carbon atoms or alkaryl having 7 to 100 carbon atoms, or an acyl group of formula (a) or (b) where R6 is alkyl having 1 to 30 carbon atoms, phenyl, aralkyl having 7 to 36 carbon atoms or alkaryl having 7 to 36 carbon atoms; R7 and R8 are independently hydrogen, hydroxy, lower alkyl, or lower alkoxy; A2 is a nitro, amino, N-alkylamino wherein the alkyl group contains 1 to 6 carbon atoms, or N,N-dialkylamino wherein each alkyl group independently contains 1 to 6 carbon atoms; n is an integer from 5 to 100; and x and y are each independently integers from 0 to 10.