- Selenium-catalyzed intramolecular atom- And redox-economical transformation ofo-nitrotoluenes into anthranilic acids
-
Anthranilic acids (AAs) are significant basic chemicals used in pharmaceuticals, agrochemicals, dyes, fragrances,etc. Superfluous steps are always involved in obtaining AAs. Herein, we demonstrate a straightforward strategy to transform abundanto-nitrotoluenes into biologically and pharmaceutically significant AAs without any extra reductants, oxidants and protecting groups. Various sensitive groups, such as halogens, sulfide, aldehyde, pyridines, quinolines,etc., can be tolerated in this transformation. A hundred-gram-scale operation is realized efficiently with almost quantitative selenium recycling. Further mechanistic studies and DFT calculations disclosed the proposed atom-exchange processes and the key roles of the selenium species.
- Jiang, Xuefeng,Li, Yiming,Lin, Zhenyang,Wang, Yuhong,Yang, Tilong
-
supporting information
p. 2986 - 2991
(2021/05/05)
-
- PAPD5 INHIBITORS AND METHODS OF USE THEREOF
-
The present application provides compounds that are PAPD5 inhibitors and are useful in treating a variety of conditions such as cancer, telomere diseases, and aging-related and other degenerative disorders.
- -
-
Page/Page column 160-161
(2020/11/03)
-
- Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease
-
Agonists of the cannabinoid receptor 1 (CB1) have been suggested as possible treatments for a range of medical disorders including gastroesophageal reflux disease (GERD). While centrally acting cannabinoid agonists are known to produce psychotropic effects, it has been suggested that the CB1 receptors in the periphery could play a significant role in reducing reflux. A moderately potent and highly lipophilic series of 2-aminobenzamides was identified through focused screening of GPCR libraries. Development of this series focused on improving potency and efficacy at the CB1 receptor, reducing lipophilicity and limiting the central nervous system (CNS) exposure while maintaining good oral absorption. Improvement of the series led to compounds having excellent potency at the CB1 receptor and high levels of agonism, good physical and pharmacokinetic properties, and low penetration into the CNS. A range of compounds demonstrated a dose-dependent inhibition of transient lower esophageal sphincter relaxations in a dog model.
- Plowright, Alleyn T.,Nilsson, Karolina,Antonsson, Madeleine,Amin, Kosrat,Broddefalk, Johan,Jensen, J?rgen,Lehmann, Anders,Jin, Shujuan,St-Onge, Stephane,Tomaszewski, Miros?aw J.,Tremblay, Maxime,Walpole, Christopher,Wei, Zhongyong,Yang, Hua,Ulander, Johan
-
p. 220 - 240
(2013/02/25)
-
- NEW COMPOUNDS
-
The present invention relates to compounds of formula (I) [Chemical formula should be inserted here. Please see paper copy] as well as pharmaceutically acceptable salts and pharmaceutical compositions including the compounds are prepared or thereof: wherein, A1, A2, R1, R2, R3, R4, and R5 and n are as defined in the specification. The compounds of formula (I) are useful in therapy.
- -
-
Page/Page column 43
(2008/06/13)
-
- THERAPEUTIC COMPOUNDS: PYRIDINE AS SCAFFOLD
-
Compounds of formulas I, IA, and IB or IC or pharmaceutically acceptable salts thereof: wherein A, A1, A2, A3, A4, R2, R3, R4 and n are as defined in the specifications well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
- -
-
Page/Page column 212-213
(2010/02/14)
-