1085699-23-5Relevant articles and documents
PYRROLO[1,2-A]PYRIMIDINYL CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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Paragraph 00369, (2017/11/04)
The invention provides substituted pyrrolo[1,2-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrrolo[1,2-a]pyrimidinyl carboxamide compounds described herein include substituted 2-heterocyclyl-4-alkyl-pyrrolo[1,2-a]pyrimidine-8-carboxarnide compounds and variants thereof.
TiCl4/Et3N-Mediated Condensation of Acetate and Formate Esters: Direct Access to β-Alkoxy- and β-Aryloxyacrylates
álvarez-Calero, José María,Jorge, Zacarías D.,Massanet, Guillermo M.
supporting information, p. 6344 - 6347 (2016/12/23)
A methodology to build (E)-β-alkoxy- and (E)-β-aryloxyacrylate moieties from acetate and formate esters promoted by the TiCl4/Et3N system is presented. The reaction is compatible with a broad range of structural skeletons and elapses through an unusual condensation pathway. Taking into account the obtained results, we propose a plausible mechanism involving a bimetallic titanium intermediate for this type of transformation.
Pyrazolo[1,5-A]pyrimidines as antiviral agents
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Page/Page column 238, (2016/04/20)
The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study
Mackman, Richard L.,Sangi, Michael,Sperandio, David,Parrish, Jay P.,Eisenberg, Eugene,Perron, Michel,Hui, Hon,Zhang, Lijun,Siegel, Dustin,Yang, Hai,Saunders, Oliver,Boojamra, Constantine,Lee, Gary,Samuel, Dharmaraj,Babaoglu, Kerim,Carey, Anne,Gilbert, Brian E.,Piedra, Pedro A.,Strickley, Robert,Iwata, Quynh,Hayes, Jaclyn,Stray, Kirsten,Kinkade, April,Theodore, Dorothy,Jordan, Robert,Desai, Manoj,Cihlar, Tomas
, p. 1630 - 1643 (2015/04/27)
GS-5806 is a novel, orally bioavailable RSV fusion inhibitor discovered following a lead optimization campaign on a screening hit. The oral absorption properties were optimized by converting to the pyrazolo[1,5-a]-pyrimidine heterocycle, while potency, metabolic, and physicochemical properties were optimized by introducing the para-chloro and aminopyrrolidine groups. A mean EC50 = 0.43 nM was found toward a panel of 75 RSV A and B clinical isolates and dose-dependent antiviral efficacy in the cotton rat model of RSV infection. Oral bioavailability in preclinical species ranged from 46 to 100%, with evidence of efficient penetration into lung tissue. In healthy human volunteers experimentally infected with RSV, a potent antiviral effect was observed with a mean 4.2 log10 reduction in peak viral load and a significant reduction in disease severity compared to placebo. In conclusion, a potent, once daily, oral RSV fusion inhibitor with the potential to treat RSV infection in infants and adults is reported.
PYRAZOLO[1,5-A]PYRIMIDINES AS ANTIVIRAL AGENTS
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Paragraph 0542; 0543; 0544, (2013/07/05)
The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT
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Paragraph 0412-0413, (2013/10/22)
Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections
[1-(1,4-Benzodioxan-2-yl)-4-(4-aminopyrimidin-2-yl]piperazines useful as anti-depressants
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, (2008/06/13)
Novel [1-(1,4-benzodioxan-2-yl)-4-(4-aminopyrimidin-2-yl]piperazines having the general formula STR1 wherein: R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and lower alkyl; X and Y are independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy or halogen; and n is either 0, 1 or 2 and the pharmaceutically acceptable acid addition salts thereof are useful as anti-depressants.