226989-36-2Relevant academic research and scientific papers
5-(2-(2,5-DIFLUOROPHENYL)PYRROLIDIN-1 -YL)-3-(1H-PYRAZOL-1-YL)PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AND RELATED COMPOUNDS AS TRK KINASE INHIBITORS FOR TREATING CANCER
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, (2019/07/19)
The application relates to pyrazolo[1,5-a]pyrimidine derivatives of formula (IV) as Trk kinase inhibitors for treating cancer and inflammatory diseases
A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity
Filipski, Kevin J.,Bian, Jianwei,Ebner, David C.,Lee, Esther C.Y.,Li, Jian-Cheng,Sammons, Matthew F.,Wright, Stephen W.,Stevens, Benjamin D.,Didiuk, Mary T.,Tu, Meihua,Perreault, Christian,Brown, Janice,Atkinson, Karen,Tan, Beijing,Salatto, Christopher T.,Litchfield, John,Pfefferkorn, Jeffrey A.,Guzman-Perez, Angel
scheme or table, p. 415 - 420 (2012/02/16)
A novel series of glucagon receptor antagonists has been discovered. These pyrazole ethers and aminopyrazoles have lower molecular weight and increased polarity such that the molecules fall into better drug-like property space. This work has culminated in
Divergent synthesis and evaluation of inhibitory activities against cyclooxygenases-1 and -2 of natural withasomnines and analogues
Usami, Yoshihide,Watanabe, Ryo,Fujino, Yuiko,Shibano, Makio,Ishida, Chihiro,Yoneyama, Hiroki,Harusawa, Shinya,Ichikawa, Hayato
, p. 1550 - 1560 (2013/02/22)
The divergent synthesis of natural withasomnines and analogues was achieved from 4-hydroxypyrazoles, which was prepared via alkaline hydrolysis of the Baeyer-Villiger oxidation products from 4-formylpyrazoles. Key steps of this synthesis are regioselective Claisen rearrangement of 4-allyloxypyrazoles and the Suzuki-Miyaura coupling of 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl trifluoromethanesulfonate and commercially available arylboronic acids. The Suzuki-Miyaura coupling at the final step of this strategy enabled facile access to natural withasomnines and their analogues. The biological activities of the twelve synthesized compounds against cyclooxygenases-1 and -2 (COX-1 and COX-2) were evaluated.
Divergent synthesis of withasomnines via synthesis of 4-hydroxy-1H- pyrazoles and Claisen rearrangement of their 4-O-allylethers
Ichikawa, Hayato,Watanabe, Ryo,Fujino, Yuiko,Usami, Yoshihide
scheme or table, p. 4448 - 4451 (2011/09/19)
4-Hydroxypyrazoles were synthesized by the alkaline hydrolysis of the Baeyer-Villiger oxidation products of 4-formylpyrazoles. This new synthesis of 4-hydroxypyrazoles was applied to the divergent synthesis of withasomnine alkaloids in a unique strategy, for which the key steps included the regioselective Claisen rearrangement of their 4-O-allyl-4-hydroxy-1H-pyrazoles and a Suzuki coupling of 4-trifluoromethanesulfonyloxy-1H-pyrazoles and arylboronic acids.
SELECTIVE BETA3 ADRENERGIC AGONISTS
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, (2019/06/28)
The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective β 3 receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and methods of treating Type II diabetes and obesity, comprising administering to a mammal in need thereof compounds of formula (I) or a pharmaceutically acceptable salt thereof. The variables of formula (I) have the meanings defined herein.
SELECTIVE BETA3 ADRENERGIC AGONISTS
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, (2015/09/24)
The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective β 3 receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and methods of treating type II diabetes and obesity, comprising administering to a mammal in need thereof compounds of the Formula I:
