Patent classifications
C07J9/00
STAT3 AND ERK SIGNAL PATHWAY INHIBITOR AND USE THEREOF
The present invention relates to a chemical and pharmaceutical technology, and in particular to a STAT3 and ERK signal pathway inhibitor and a use thereof. The present invention provides a STAT3 and ERK signal pathway inhibitor. The inhibitor mainly consists of a mogroside and/or an analog thereof. The mogroside and the analog thereof inhibit the phosphorylation of a transcription factor STAT3 and the phosphorylation of an ERK. The method for preparing the mogroside and the analog has the characteristics of simpleness, strong operability and high purity of products. The present invention furtherprovides a use of the STAT3 and ERK signal pathway inhibitor in the preparation of drugs for treating tumors, which realizes the purposes of inhibiting the proliferation of cancer cells and promoting the apoptosis of cancer cells and has a very good inhibition effect on cancers.
POLYMERIZABLE POLAR COMPOUND, LIQUID CRYSTAL COMPOSITION, AND LIQUID CRYSTAL DISPLAY ELEMENT
Provided is a polar compound having high chemical stability, high capability of aligning liquid crystal molecules, high solubility in a liquid crystal composition, and a large voltage holding ratio when used in a liquid crystal display device. The compound is represented by formula (1):
##STR00001##
in which, for example, R.sup.1 is alkyl having 1 to 15 carbons; MES is a mesogen group having at least one ring; Sp.sup.1 is a single bond or alkylene having 1 to 10 carbons; M.sup.1 and M.sup.2 are hydrogen; and R.sup.2 is a group represented by formulas (1a) to (1c):
##STR00002##
in which, Sp.sup.2 and Sp.sup.a are a single bond or alkylene having 1 to 10 carbons; S.sup.1 is >CH—; S.sup.2 is >C<; and X.sup.1 is —OH.
POLYMERIZABLE POLAR COMPOUND, LIQUID CRYSTAL COMPOSITION, AND LIQUID CRYSTAL DISPLAY ELEMENT
Provided is a polar compound having high chemical stability, high capability of aligning liquid crystal molecules, high solubility in a liquid crystal composition, and a large voltage holding ratio when used in a liquid crystal display device. The compound is represented by formula (1):
##STR00001##
in which, for example, R.sup.1 is alkyl having 1 to 15 carbons; MES is a mesogen group having at least one ring; Sp.sup.1 is a single bond or alkylene having 1 to 10 carbons; M.sup.1 and M.sup.2 are hydrogen; and R.sup.2 is a group represented by formulas (1a) to (1c):
##STR00002##
in which, Sp.sup.2 and Sp.sup.a are a single bond or alkylene having 1 to 10 carbons; S.sup.1 is >CH—; S.sup.2 is >C<; and X.sup.1 is —OH.
Metathesis catalysts and methods thereof
The present application provides, among other things, compounds and methods for metathesis reactions. In some embodiments, the present disclosure provides methods for preparing alkenyl halide with regioselectivity and/or stereoselectivity. In some embodiments, the present disclosure provides methods for preparing alkenyl halide with regioselectivity and Z-selectivity. In some embodiments, the present disclosure provides methods for preparing alkenyl halide with regioselectivity and E-selectivity. In some embodiments, provided technologies are particularly useful for preparing alkenyl fluorides. In some embodiments, a provided compound useful for metathesis reactions has the structure of formula II-a. In some embodiments, a provided compound useful for metathesis reactions has the structure of formula II-b.
Metathesis catalysts and methods thereof
The present application provides, among other things, compounds and methods for metathesis reactions. In some embodiments, the present disclosure provides methods for preparing alkenyl halide with regioselectivity and/or stereoselectivity. In some embodiments, the present disclosure provides methods for preparing alkenyl halide with regioselectivity and Z-selectivity. In some embodiments, the present disclosure provides methods for preparing alkenyl halide with regioselectivity and E-selectivity. In some embodiments, provided technologies are particularly useful for preparing alkenyl fluorides. In some embodiments, a provided compound useful for metathesis reactions has the structure of formula II-a. In some embodiments, a provided compound useful for metathesis reactions has the structure of formula II-b.
NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.z4, R.sup.z5, R.sup.z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.
##STR00001##
NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.z4, R.sup.z5, R.sup.z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.
##STR00001##
NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME
The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
TGR5 MODULATORS AND METHODS OF USE THEREOF
The application relates to compounds of formula A:
##STR00001##
or a salt, solvate, ester, tautomer, amino acide conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
TGR5 MODULATORS AND METHODS OF USE THEREOF
The application relates to compounds of formula A:
##STR00001##
or a salt, solvate, ester, tautomer, amino acide conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.