C07D513/02

Optically active 2-hydroxy tetrahydrothienopyridine derivatives, preparation method and use in manufacture of medicament thereof

Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.

COMPOUNDS FOR THE MODULATION OF MYC ACTIVITY

The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.

##STR00001##

COMPOUNDS FOR THE MODULATION OF MYC ACTIVITY

The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.

##STR00001##

NUCLEIC ACID MODIFYING AGENTS AND USES THEREOF

In some aspects, the disclosure provides compounds comprising nucleic acid modifying moieties, such as nucleic acid binding dyes comprising activatable groups. In some aspects, the disclosure provides nucleic acid probes comprising compounds of the disclosure, and methods of making the same. In some aspects, the disclosure provides methods of using compounds of the disclosure, such as methods of labeling and/or detecting non-viable organisms or non-viable cells, and methods of detecting contamination or infection.

NUCLEIC ACID MODIFYING AGENTS AND USES THEREOF

In some aspects, the disclosure provides compounds comprising nucleic acid modifying moieties, such as nucleic acid binding dyes comprising activatable groups. In some aspects, the disclosure provides nucleic acid probes comprising compounds of the disclosure, and methods of making the same. In some aspects, the disclosure provides methods of using compounds of the disclosure, such as methods of labeling and/or detecting non-viable organisms or non-viable cells, and methods of detecting contamination or infection.

Benzobis (thiadiazole) derivative, ink comprising same, and organic electronic device comprising same

A benzobis(thiadiazole) derivative represented by the following general formula (1): ##STR00001## in which R.sup.1 represents a linear or branched alkyl group, or any one of the groups of the following formula (2): ##STR00002##
in which R represents a linear or branched alkyl group; R.sup.2 represents a hydrogen atom; and R.sup.3 represents a hydrogen atom, a linear or branched alkyl group, or any one of the groups of the formula (2);
with the proviso that at least one of R.sup.1 and R.sup.3 represents any one of the groups of the formula (2); and two R.sup.1 groups, two R.sup.2 groups, and two R.sup.3 groups may be the same as, or different from each other.

Benzobis (thiadiazole) derivative, ink comprising same, and organic electronic device comprising same

A benzobis(thiadiazole) derivative represented by the following general formula (1): ##STR00001## in which R.sup.1 represents a linear or branched alkyl group, or any one of the groups of the following formula (2): ##STR00002##
in which R represents a linear or branched alkyl group; R.sup.2 represents a hydrogen atom; and R.sup.3 represents a hydrogen atom, a linear or branched alkyl group, or any one of the groups of the formula (2);
with the proviso that at least one of R.sup.1 and R.sup.3 represents any one of the groups of the formula (2); and two R.sup.1 groups, two R.sup.2 groups, and two R.sup.3 groups may be the same as, or different from each other.

Furanone derivative

To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I): ##STR00001##
wherein A represents COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.

Indoles as respiratory syncytial virus antiviral agents

Indoles having inhibitory activity on RSV replication and having the formula I ##STR00001##
the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.

Treatment of pancreatic and related cancers with 5-acyl-6,7-dihydrothieno[3,2-c]pyridines

Methods for inhibiting the growth of pancreatic cancer cells or other cancer cells driven by Sonic hedgehog are disclosed. The method involves exposing the cells to 5-acyl-6,7-dihydrothieno[3,2-c]pyridines of formula I ##STR00001##