Patent classifications
C07D295/26
KDM1A inhibitors for the treatment of disease
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
KDM1A inhibitors for the treatment of disease
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
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.
SULFUR (VI) FLUORIDE COMPOUNDS AND METHODS FOR THE PREPARATION THEREOF
This application describes a compound represented by Formula (I):
##STR00001##
wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X.sup.1 is a covalent bond or CH.sub.2CH.sub.2, X.sup.2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.
SULFUR (VI) FLUORIDE COMPOUNDS AND METHODS FOR THE PREPARATION THEREOF
This application describes a compound represented by Formula (I):
##STR00001##
wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X.sup.1 is a covalent bond or CH.sub.2CH.sub.2, X.sup.2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.
ACTINIC RAY-SENSITIVE OR RADIATION-SENSITIVE RESIN COMPOSITION, RESIST FILM, PATTERN FORMING METHOD, AND METHOD FOR MANUFACTURING ELECTRONIC DEVICE
The present invention provides an actinic ray-sensitive or radiation-sensitive resin composition with which a pattern having an excellent pattern collapse suppressing property and excellent LWR performance can be obtained. In addition, the present invention also provides a resist film, a pattern forming method, and a method for manufacturing an electronic device, each regarding the actinic ray-sensitive or radiation-sensitive resin composition. The actinic ray-sensitive or radiation-sensitive resin composition of the present invention includes a resin whose solubility in a developer is changed by the action of an acid, a photoacid generator represented by General Formula (b1), and a solvent, in which the photoacid generator represented by General Formula (b1) is a compound that generates an acid having a pka of 1.0 or less upon irradiation with actinic rays or radiation
##STR00001##
ACTINIC RAY-SENSITIVE OR RADIATION-SENSITIVE RESIN COMPOSITION, RESIST FILM, PATTERN FORMING METHOD, AND METHOD FOR MANUFACTURING ELECTRONIC DEVICE
The present invention provides an actinic ray-sensitive or radiation-sensitive resin composition with which a pattern having an excellent pattern collapse suppressing property and excellent LWR performance can be obtained. In addition, the present invention also provides a resist film, a pattern forming method, and a method for manufacturing an electronic device, each regarding the actinic ray-sensitive or radiation-sensitive resin composition. The actinic ray-sensitive or radiation-sensitive resin composition of the present invention includes a resin whose solubility in a developer is changed by the action of an acid, a photoacid generator represented by General Formula (b1), and a solvent, in which the photoacid generator represented by General Formula (b1) is a compound that generates an acid having a pka of 1.0 or less upon irradiation with actinic rays or radiation
##STR00001##
FLUOROSULFONYL-CONTAINING COMPOUND, INTERMEDIATE THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF
Disclosed in the present invention were a fluorosulfonyl-containing compound, an intermediate thereof, a preparation method therefor and use thereof. The fluorosulfonyl-containing compound disclosed in the present invention comprises a cation and an anion, the cation being as shown in Formula (1). The fluorosulfonyl-containing compound of the present invention can react with a substrate to efficiently synthesize a fluorosulfonylation product, has low toxicity, was simple to prepare, was convenient to use, and was in a solid stable state at normal temperature. Furthermore, the compound has a wide range of adaptable substrates, including phenolic compounds and amine compounds, and was the only solid form agent that can achieve such a chemical conversion, and therefore has important academic and application value.
##STR00001##
ARYL-SULFONAMIDE AND ARYL-SULFONE DERIVATIVES AS TRPML MODULATORS
The new arylsulfonamide and arylsulfone derivatives are modulators of TRPML and are useful in treating disorders related to TRPML activities and lysosome functions such as acid-related disorders and cancer.