179692-09-2Relevant articles and documents
A new synthethic approach to indazole synthesis
Baraldi, Pier Giovanni,Cacciari, Barbara,Spalluto, Giampiero,Romagnoli, Romeo,Braccioli, Giovanni,Zaid, Abdel Naser,De Pineda Las Infantas, Maria J.
, p. 1140 - 1142 (1997)
Stobbe condensation of 3-alkyl- or aryl-4-formylpyrazoles 3a-f with diethyl succinate in the presence of potassium f-butoxide, followed by intramolecular ring closure (Ac2O-NaOAc), afforded the corresponding indazole derivatives 5a-f in 65-85% overall yield. These compounds are good starting materials for transformation to biologically active molecules, such as new pyrazole analogs of the left-hand segment of the potent natural antineoplastic agent CC-1065.
HETEROCYCLICALLY SUBSTITUTED TRIFLUOROMETHYLPYRIMIDINONES AND THEIR USE
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Paragraph 0201, (2017/02/24)
The present application relates to novel heterocyclically substituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.
Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup
Devasthale, Pratik,Wang, Wei,Hernandez, Andres S.,Moore, Fang,Renduchintala, Kishore,Sridhar, Radhakrishnan,Pelleymounter, Mary Ann,Longhi, Daniel,Huang, Ning,Flynn, Neil,Azzara, Anthony V.,Rohrbach, Kenneth,Devenny, James,Rooney, Suzanne,Thomas, Michael,Glick, Susan,Godonis, Helen,Harvey, Susan,Cullen, Mary Jane,Zhang, Hongwei,Caporuscio, Christian,Stetsko, Paul,Grubb, Mary,Huang, Christine,Zhang, Lisa,Freeden, Chris,Li, Yi-Xin,Murphy, Brian J.,Robl, Jeffrey A.,Washburn, William N.
, p. 2793 - 2799 (2015/06/08)
Our investigation of the structure-activity and structure-liability relationships for dihydropyrrolopyrazol-6-one MCHR1 antagonists revealed that off-rate characteristics, inferred from potencies in a FLIPR assay following a 2 h incubation, can impact in