666735-07-5

Upstream product

• 541-41-3 chloroformic acid ethyl ester 
• 918492-64-5 (3-bromo-4-methoxyphenyl)-methylidene(2,2-dimethoxyethyl)amine 
• 34841-06-0 3-bromo-4-methoxybenzylaldehyde 
• 22483-09-6 2,2-dimethoxyethylamine 

Relevant academic research and scientific papers

2-(INDAZOL-5-YL)-6-(PIPERIDIN-4-YL)-1,7-NAPHTHYRIDINE DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS FOR SPLICING NUCLEIC ACIDS AND FOR THE TREATMENT OF PROLIFERATIVE DISEASES

The present disclosure features compounds of formula (l-a) and of formula (II) and pharmaceutical compositions thereof. The present disclosure further discloses the compounds of formula (I- a) and (II) and their compositions for use in methods of modulating nucleic acid splicing, e.g., splicing of a pre-mRNA, as well as said compounds for use in methods of treating e.g.: ? proliferative diseases, such as e.g. cancer, benign neoplasms or angiogenesis, ? neurological diseases or disorders, such as e.g. Huntington's disease, ? autoimmune diseases or disorders, immunodeficiency diseases or disorders, lysosomal storage disease or disorder, cardiovascular diseases or disorders, metabolic diseases or disorders, respiratory diseases or disorders, renal diseases or disorders, or infectious diseases. Exemplary compounds are e.g. 2-(indazol-5-yl)-6-(piperidin-4-yl)-l,7- naphthyridine derivatives and similar compounds.

COMPOSITIONS FOR MODULATING SPLICING

Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.

METHODS AND COMPOSITIONS FOR MODULATING SPLICING

Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.

Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors

Protein kinase C iota (PKC-i) is an atypical kinase implicated in the promotion of different cancer types. A biochemical screen of a fragment library has identified several hits from which an azaindole-based scaffold was chosen for optimization. Driven by a structure-activity relationship and supported by molecular modeling, a weakly bound fragment was systematically grown into a potent and selective inhibitor against PKC-i.

ARYLOXYACETYLINDOLES AND ANALOGS AS ANTIBIOTIC TOLERANCE INHIBITORS

The disclosure provides compounds and pharmaceutical compositions of aryloxyacetylindoles compounds and analogs useful for treating chronic and acute bacterial infections. Certain of the compounds are compounds of general Formula (I) (I) or a pharmaceutically acceptable salt or prodrug thereof. Certain compounds of this disclosure are MvfR inhibitors. MvfR inhibitors reduce the formation of antibiotic tolerant bacterial strains and are useful for treating Gram-negative bacterial infections and reducing the virulence of Pseudomonas aeruginosa. Methods of treating bacterial infections in a subject, including Pseudomonas aeruginosa infections, are also provided by the disclosure.

ISOQUINOLINE DERIVATIVES AS INHIBITORS OF RHO-KINASE

The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I); useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.