Patent classifications
C07D317/54
COMPOUNDS FOR TREATING PROSTATE CANCER
A compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of:
R.sup.20(Z).sub.b(Y).sub.c(R.sup.21).sub.aXR.sup.22R.sup.23 wherein R.sup.20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, or NR.sup.10, wherein R.sup.10 is H or alkyl; R.sup.21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is C(O) or S(O)(O); R.sup.22 is a moiety that includes at least one divalent amino radical; R.sup.23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; a is 0 or 1; b is 0 or 1; and c is 0 or 1; provided that if X is C(O) then Y is not S.
USE OF STIRIPENTOL AND THEIR DERIVATIVES FOR DECREASING URINARY OXALATE CONCENTRATION IN AN INDIVIDUAL
The present invention relates to a compound of formula (I): wherein: -n is 1 or 2; Z.sub.1, Z.sub.2 and Z.sub.3, identical or different, are selected from a hydrogen atom, a halogen atom and a (C.sub.1-C.sub.6)alkyl group; and R is an optionally substituted (C.sub.1-C.sub.6)alkyl group by one or more substituents chosen from a hydroxyl, an oxo and a thiol group; or one of its pharmaceutically acceptable salts; for use to decrease urinary oxalate concentration in an individual. The present invention further relates to a compound of formula (I) for use in the prevention and/or treatment of diseases and/or conditions related to a high urinary oxalate concentration in an individual.
##STR00001##
Method for synthesizing chiral beta-hydroxy acid ester compound
A method for synthesizing a chiral -hydroxy acid ester compound is disclosed. The method includes the steps of: using an aldehyde compound and a monoalkyl malonate as raw materials, using a metal and a chiral ligand as a catalyst to make the raw materials be directly and fully reacted in an organic solvent and form a reaction solution, and separating and purifying the reaction solution to obtain the highly stereoselective -hydroxy acid ester compound. The beneficial effects are mainly embodied in: 1. simple operation; 2. rapidly constructing a highly stereoselective -hydroxy acid ester skeleton structure molecule; 3. high reaction yield and good stereoselectivity. Therefore, the invention has high basic research significance, industrial production value and social economic benefit.
Compounds for treating prostate cancer
A compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: R.sup.20(Z).sub.b(Y).sub.c(R.sup.21).sub.aXR.sup.22R.sup.23 wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, or NR.sup.10, wherein R.sup.10 is H or alkyl; R.sup.21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is C(=0)- or S(=0)(=0)-; R.sup.22 is a moiety that includes at least one divalent amino radical; R.sup.23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; a is 0 or 1; b is 0 or 1; and c is 0 or 1; provided that if X is C(=0)- then Y is not S.
Compounds for treating prostate cancer
A compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: R.sup.20(Z).sub.b(Y).sub.c(R.sup.21).sub.aXR.sup.22R.sup.23 wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, or NR.sup.10, wherein R.sup.10 is H or alkyl; R.sup.21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, alkatrienyl, substituted alkatrienyl; X is C(=0)- or S(=0)(=0)-; R.sup.22 is a moiety that includes at least one divalent amino radical; R.sup.23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; a is 0 or 1; b is 0 or 1; and c is 0 or 1; provided that if X is C(=0)- then Y is not S.
AN IMPROVED PROCESS FOR THE PREPARATION OF DROXIDOPA AND ITS INTERMEDIATE
The present invention provides an improved process for preparation of L-threo-(2S,3R)-3-(3,4-dihydroxyphenyl)serine (I) (Droxidopa) and its salts; comprising (a) reaction of the aldehyde compound (III) (as described herein) with Metal complex (II) (as described herein), and (h) hydrolysis of the compound (IV) obtained from step (a) in presence of acid. The present invention also relates to a novel intermediates metal chiral complex (IV) for the preparation of Droxidopa.
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds that are useful for treating or preventing cancer.
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
The invention provides compounds that are useful for treating or preventing cancer.
N-hydroxylsulfonamide derivatives as nitroxyl donors
The disclosed subject matter provides N-hydroxylsulfonamide derivative compounds of formulae (I), (II) or (III) as drawn below, pharmaceutical compositions comprising such compounds, kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure. ##STR00001##
N-hydroxylsulfonamide derivatives as nitroxyl donors
The disclosed subject matter provides N-hydroxylsulfonamide derivative compounds of formulae (I), (II) or (III) as drawn below, pharmaceutical compositions comprising such compounds, kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure. ##STR00001##