C07H19/044

INDOLEACETIC ACID DERIVATIVE AND PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
20200095271 · 2020-03-26 ·

The present invention relates to an indoleacetic acid derivative and a preparation method and pharmaceutical use thereof. In particular, the present invention relates to a compound shown in general formula (I), a preparation method thereof, a pharmaceutical composition comprising the same, and a use thereof as a cough suppressant in treating a disease such as a cough. The definition of each substituent in the general formula (I) is the same as the definition in the specification.

##STR00001##

INDOLEACETIC ACID DERIVATIVE AND PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
20200095271 · 2020-03-26 ·

The present invention relates to an indoleacetic acid derivative and a preparation method and pharmaceutical use thereof. In particular, the present invention relates to a compound shown in general formula (I), a preparation method thereof, a pharmaceutical composition comprising the same, and a use thereof as a cough suppressant in treating a disease such as a cough. The definition of each substituent in the general formula (I) is the same as the definition in the specification.

##STR00001##

ASGPR-BINDING COMPOUNDS FOR THE DEGRADATION OF EXTRACELLULAR PROTEINS

Compounds and compositions that have an asialoglycoprotein receptor (ASGPR) binding ligand bound to an extracellular protein binding ligand for the selective degradation of the target extracellular protein in vivo to treat disorders mediated by the extracellular protein are described.

ARYL HYDROCARBON RECEPTOR MODULATORS
20190330201 · 2019-10-31 ·

The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts,

##STR00001## R is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3,

##STR00002##

two R.sub.a is independently H, or two R.sub.a together form O or NW.sub.3R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and CN, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.

ARYL HYDROCARBON RECEPTOR MODULATORS
20190330201 · 2019-10-31 ·

The disclosure discloses an aryl hydrocarbon receptor modulators of formula (I), and pharmaceutically acceptable salts,

##STR00001## R is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3,

##STR00002##

two R.sub.a is independently H, or two R.sub.a together form O or NW.sub.3R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring, or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom from N, O and S, or 4 to 7 membered non-aromatic heterocyclic ring containing 1 to 3 heteroatom from N, O and S and CN, which are with no substituent or substituted by 1 or 3 R; Q is R, or a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring containing 1 to 5 heteroatom selected from N, O and S, which are with no substituent or substituted by 1 or 3 R; R is R.sub.c connected with C or R.sub.N connected with N.

ARYL HYDROCARBON RECEPTOR MODULATOR
20190307731 · 2019-10-10 · ·

Disclosed is an aryl hydrocarbon receptor modulator of formula (I), and a pharmaceutically acceptable salt thereof, wherein

##STR00001##

R is H, CN, CH.sub.2(OH)R.sub.0, C.sub.mH.sub.2m+1, C.sub.nH.sub.2n-1, C.sub.nH.sub.2n-3,

##STR00002##

two R.sub.a are independently H or two R.sub.a together form O or NW.sub.3R.sub.1; A is a C.sub.6 to C.sub.10 aromatic ring unsubstituted or substituted with 1 to 3 R, or a C.sub.2-C.sub.10 heteroaromatic ring interrupted by 1 to 5 heteroatoms selected from N, O, and S or a 4 to 7 membered nonaromatic heterocyclic ring containing CN and interrupted by 1 to 3 heteroatoms selected from N, O, and S, with either one unsubstituted or substituted with 1 to 3 R; Q is R, or is a C.sub.6 to C.sub.10 aromatic ring or a C.sub.2 to C.sub.10 heteroaromatic ring unsubstituted or substituted with 1 to 3 R and interrupted by 1 to 5 heteroatoms selected from N, O, and S; and R is R.sub.c which is C-attached or R.sub.N which is N-attached. The compounds of formula (I) of the present invention can regulate AhR activity, and can be used to inhibit the growth of cancer cells and inhibit the metastasis and invasion of tumor cells.

Tetracyclic anthraquinone derivatives

Disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof, ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, n are defined as in the present application. Also disclosed is a method for treating cancer, comprising administering to a subject in need thereof a therapeutically effective amount of the compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The compound and a salt thereof according to the present application possess good anticancer and/or antitumor activity, and good water solubility and stability, as well as good tolerance in animal bodies. Also disclosed is a process for preparing a compound represented by formula (I) of the present application.

Tetracyclic anthraquinone derivatives

Disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof, ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W, n are defined as in the present application. Also disclosed is a method for treating cancer, comprising administering to a subject in need thereof a therapeutically effective amount of the compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The compound and a salt thereof according to the present application possess good anticancer and/or antitumor activity, and good water solubility and stability, as well as good tolerance in animal bodies. Also disclosed is a process for preparing a compound represented by formula (I) of the present application.

Immunomodulating beta-1,6-D-glucans

This invention relates to modifications of -1,6-D-glucans, e.g., structures according to Formula (I), and the ability of these compositions to modulate an immune response. ##STR00001##

Immunomodulating beta-1,6-D-glucans

This invention relates to modifications of -1,6-D-glucans, e.g., structures according to Formula (I), and the ability of these compositions to modulate an immune response. ##STR00001##