C07D271/07

SSAO inhibitor

The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof. ##STR00001##

MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X4 AND RELATED PRODUCTS AND METHODS

Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I).

##STR00001##

or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

OXADIAZOLE DERIVATIVES FOR THE TREATMENT OF GENETIC DISEASES DUE TO NONSENSE MUTATIONS

Are disclosed oxadiazole derivatives, their use as medicaments and in particular for the treatment of diseases associated with the presence of a nonsense mutation in the gene or a premature stop codon in the mRNA, pharmaceutical formulation comprising said oxadiazole derivatives and prodrug or mixture thereof and the methods for the preparation of said Oxadiazole derivatives.

OXADIAZOLE DERIVATIVES FOR THE TREATMENT OF GENETIC DISEASES DUE TO NONSENSE MUTATIONS

Are disclosed oxadiazole derivatives, their use as medicaments and in particular for the treatment of diseases associated with the presence of a nonsense mutation in the gene or a premature stop codon in the mRNA, pharmaceutical formulation comprising said oxadiazole derivatives and prodrug or mixture thereof and the methods for the preparation of said Oxadiazole derivatives.

Antitumor Agent

The present invention provides a method of enhancing an antitumor effect by a compound strongly inhibiting ribonucleotide reductase (RNR) or a salt thereof.

A combination formulation involving combined administration of a sulfonamide compound represented by Formula (I) [In the formula, X.sup.1 represents an oxygen atom or the like; X.sup.2 represents an oxygen atom; X.sup.3 represents NH; X.sup.4 represents a hydrogen atom or the like; R.sup.1 represents C(R.sup.11) (R.sup.12) or the like; R.sup.11 and R.sup.12 are the same or different and each represents a hydrogen atom or the like; R.sup.2 represents an optionally substituted C6-C14 aromatic hydrocarbon group or the like; R.sup.3 represents an optionally substituted C6-C14 aromatic hydrocarbon group or the like; R.sup.4 represents a hydrogen atom or the like] or a salt thereof, having RNR inhibitory activity, and other antitumor agent(s).

Sulfonamide Compound or Salt Thereof

The present invention provides a novel sulfonamide compound having a ribonucleotide reductase inhibitory activity or a salt thereof, and a pharmaceutical composition containing the same as an active ingredient.

A compound represented by Formula (I) [wherein, X.sup.1 represents an oxygen atom or the like; X.sup.2 represents an oxygen atom; X.sup.3 represents NH; X.sup.4 represents a hydrogen atom or the like; R.sup.1 represents C(R.sup.11)(R.sup.12) or the like; R.sup.11 and R.sup.12 are the same or different and each represents a hydrogen atom or the like; R.sup.2 represents an optionally substituted C.sup.6-C.sup.14 aromatic hydrocarbon group or the like; R.sup.3 represents an optionally substituted C.sup.6-C.sup.14 aromatic hydrocarbon group or the like; R.sup.4 represents a hydrogen atom or the like] or a salt thereof.

Sulfonamide Compound or Salt Thereof

The present invention provides a novel sulfonamide compound having a ribonucleotide reductase inhibitory activity or a salt thereof, and a pharmaceutical composition containing the same as an active ingredient.

A compound represented by Formula (I) [wherein, X.sup.1 represents an oxygen atom or the like; X.sup.2 represents an oxygen atom; X.sup.3 represents NH; X.sup.4 represents a hydrogen atom or the like; R.sup.1 represents C(R.sup.11)(R.sup.12) or the like; R.sup.11 and R.sup.12 are the same or different and each represents a hydrogen atom or the like; R.sup.2 represents an optionally substituted C.sup.6-C.sup.14 aromatic hydrocarbon group or the like; R.sup.3 represents an optionally substituted C.sup.6-C.sup.14 aromatic hydrocarbon group or the like; R.sup.4 represents a hydrogen atom or the like] or a salt thereof.

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

COMPOUND HAVING STAT3 INHIBITORY ACTIVITY AND USE THEREOF
20200354327 · 2020-11-12 ·

The present invention relates to a compound exhibiting STAT3 inhibitory activity, or a pharmaceutically acceptable salt, solvate or hydrate of the same, and pharmaceutical uses of these. The compounds of the present invention efficiently inhibit the abnormal activity of STAT3 associated with various diseases and thus can be usefully utilized for the prevention and treatment of various STAT3-related diseases associated with cancer, autoimmune diseases, inflammatory diseases and the like.