29482-57-3Relevant academic research and scientific papers
ANTIVIRAL TRIAZOLE DERIVATIVES
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Page/Page column 76-77, (2014/08/07)
The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
Modulation of cAMP-specific PDE without emetogenic activity: New sulfide-like PDE7 inhibitors
García, Ana M.,Brea, José,Morales-García, Jose A.,Perez, Daniel I.,González, Alejandro,Alonso-Gil, Sandra,Gracia-Rubio, Irene,Ros-Simó, Clara,Conde, Santiago,Cadavid, María Isabel,Loza, María Isabel,Perez-Castillo, Ana,Valverde, Olga,Martinez, Ana,Gil, Carmen
, p. 8590 - 8607 (2014/12/11)
A forward chemical genetic approach was followed to discover new targets and lead compounds for Parkinson's disease (PD) treatment. By analysis of the cell protection produced by some small molecules, a diphenyl sulfide compound was revealed to be a new phosphodiesterase 7 (PDE7) inhibitor and identified as a new hit. This result allows us to confirm the utility of PDE7 inhibitors as a potential pharmacological treatment of PD. On the basis of these data, a diverse family of diphenyl sulfides has been developed and pharmacologically evaluated in the present work. Moreover, to gain insight into the safety of PDE7 inhibitors for human chronic treatment, we evaluated the new compounds in a surrogate emesis model, showing nonemetic effects.
The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors
Yan, Xuelei,Wang, Zhulun,Sudom, Athena,Cardozo, Mario,Degraffenreid, Michael,Di, Yongmei,Fan, Pingchen,He, Xiao,Jaen, Juan C.,Labelle, Marc,Liu, Jinsong,Ma, Ji,McMinn, Dustin,Miao, Shichang,Sun, Daqing,Tang, Liang,Tu, Hua,Ursu, Stefania,Walker, Nigel,Ye, Qiuping,Powers, Jay P.
scheme or table, p. 7071 - 7075 (2011/01/03)
In this communication, human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11β-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent efficacy in a non-human primate ex vivo pharmacodynamic model.
Aniline derivatives
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, (2008/06/13)
The invention concerns aniline derivatives of formula I STR1 wherein m is 1, 2 or 3, n is 0, 1, 2 or 3, Q is phenyl or naphthyl or a 5- or 6-membered heteroaryl moiety containing 1, 2 or 3 heteroatoms selected from oxygen, nitrogen and sulfur, and X, R1 and R2 are defined in the claims; or pharmaceutical compositions containing them, and the methods of using the compounds as tyrosine kinase inhibitors and for the treatment of proliferative diseases such as cancer.
Structure-based design of substituted diphenyl sulfones and sulfoxides as lipophilic inhibitors of thymidylate synthase
Jones, Terence R.,Webber, Stephen E.,Varney, Michael D.,Reddy, M. Rami,Lewis, Kathleen K.,Kathardekar, Vinit,Mazdiyasni, Hormoz,Deal, Judith,Nguyen, Dzuy,Welsh, Katharine M.,Webber, Stephanie,Johnston, Amanda,Matthews, David A.,Smith, Ward W.,Janson, Cheryl A.,Bacquet, Russell J.,Howland, Eleanor F.,Booth, Carol L. J.,Herrmann, Steven M.,Ward, Robert W.,White, Jennifer,Bartlett, Charlotte A.,Morse, Cathy A.
, p. 677 - 683 (2007/10/03)
Six new diphenyl sulfoxide and five new diphenyl sulfones were designed, synthesized, and tested for their inhibition of human and Escherichia coli thymidylate synthase (TS) and of the growth of cells in tissue culture. The best sulfoxide inhibitor of hum
