60481-41-6Relevant academic research and scientific papers
COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF CYSTIC FIBROSIS
-
Page/Page column 43; 44, (2020/02/06)
The present invention relates to compounds of Formula (Ia) or pharmaceutically acceptable salts, hydrates, solvates, clathrates, polymorphs, stereoisomers thereof. It further discloses a pharmaceutical composition comprising the compounds of Formula (Ia) and the use of compounds of Formula (Ib), in particular to modulate CFTR protein or ABC protein activities.
An straightforward entry to new pyrazolo-fused dibenzo[1,4]diazepines
Hernandez, Susana,Moreno, Isabel,Sanmartin, Raul,Teresa Herrero, Maria,Dominguez, Esther
supporting information; experimental part, p. 2251 - 2257 (2011/04/26)
A series of novel pyrazolodibenzo[1,4]diazepines has been synthesized with good overall yields. The diarylpyrazole intermediates, with structure similarity to biologically relevant compounds such as currently marketed drugs like rimonabant or celecoxib, were prepared by a tandem sequence amine-exchange/ heterocyclization starting from readily available enaminones and arylhydrazines. The key step of this efficient methodology was Caryl-N bond construction, accomplished by a palladium-catalyzed intramolecular N-arylation reaction, which was conducted in both homogeneous and polymer-supported versions. Reaction scope of such protocols and recycling of the heterogeneous catalyst were also examined.
Toward safer processes for C-C biaryl bond construction: Catalytic direct C-H arylation and tin-free radical coupling in the synthesis of pyrazolophenanthridines
Hernandez, Susana,Moreno, Isabel,SanMartin, Raul,Gomez, German,Herrero, Maria Teresa,Dominguez, Esther
supporting information; experimental part, p. 434 - 441 (2010/03/30)
(Chemical Equation Presented) A series of pyrazolo[1,5-f]phenanthridine derivatives has been efficiently synthesized by a short, straightforward sequence. A tandem amine-exchange/heterocyclization of enaminones was successfully applied to the regioselective preparation of 1,5-diarylpyrazole intermediates with structure resemblance to relevant nonsteroidal anti-inflammatory drugs such as celecoxib or tepoxalin. The final key step, cyclization by intramolecular biaryl bond formation, was accomplished by two alternative methodologies: radical coupling and catalytic direct arylation via C-H activation. The scope and limitations of the two methodologies have been explored and their complementariness has been established. In addition, polymer-supported heterogeneous catalysts have been compared with homogeneous analogues. In the radical process, toxic tin derivatives have been avoided in order to employ environmentally safer protocols.
Extended Benzamide Derivatives as Modulators of the EP2 Receptor
-
Page/Page column 18-19, (2010/03/02)
The present invention relates to extended benzamide derivatives of the general formula I, to processes for preparation thereof and to use thereof for production of pharmaceutical compositions for treatment of disorders and indications associated with the
