226989-35-1Relevant articles and documents
Regioselective palladium-catalyzed C–H arylation of 4-alkoxy and 4-thioalkyl pyrazoles
Vernier, William F.,Gomez, Laurent
supporting information, p. 4587 - 4590 (2017/11/15)
A methodology for the palladium-catalyzed regioselective C–H arylation of electron rich pyrazoles has been developed. New ligands and mild conditions (70–90 °C) have been identified for this transformation. An intramolecular application of the methodology provided a novel synthetic route for the regioselective synthesis of 1,5-dihydroisochromeno[4,3-c]pyrazoles and 1,5-dihydroisothiochromeno[4,3-c]pyrazoles.
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives
Westaway, Susan M.,Preston, Alex G. S.,Barker, Michael D.,Brown, Fiona,Brown, Jack A.,Campbell, Matthew,Chung, Chun-Wa,Drewes, Gerard,Eagle, Robert,Garton, Neil,Gordon, Laurie,Haslam, Carl,Hayhow, Thomas G.,Humphreys, Philip G.,Joberty, Gerard,Katso, Roy,Kruidenier, Laurens,Leveridge, Melanie,Pemberton, Michelle,Rioja, Inma,Seal, Gail A.,Shipley, Tracy,Singh, Onkar,Suckling, Colin J.,Taylor, Joanna,Thomas, Pamela,Wilson, David M.,Lee, Kevin,Prinjha, Rab K.
, p. 1370 - 1387 (2016/03/05)
Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived from pyrido[3,4-d]pyrimidin-4(3H)-one. A number of exemplars such as compound 41 possess interesting activity profiles in KDM4C and KDM5C biochemical and target-specific, cellular mechanistic assays.
9H-PYRROLO-DIPYRIDINE DERIVATIVES
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, (2016/09/22)
The invention relates to 9H-pyrrolo-dipyridine derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.
HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS AND COMBINATIONS THEREOF
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, (2015/07/07)
Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
HISTONE DEMETHYLASE INHIBITORS
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Paragraph 00177; 00185, (2014/10/04)
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like
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.
QUINOLINONE DERIVATIVES
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Page/Page column 50-51, (2012/09/22)
The present invention relates to compounds of the formula (I), salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds as activators of AMPK.
GLUCAGON RECEPTOR MODULATORS
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Page/Page column 25, (2012/08/27)
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
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
, 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.
SMALL MOLECULE BRADYKININ B2 RECEPTOR MODULATORS
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Page/Page column 44, (2010/04/25)
The present invention is related to a compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein R1 is: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l), (m), (n), (o), (p), (q), (r), (s); R2 is C1, F, or methoxy; R3 is methyl, methoxy, hydroxymethyl, H, or absent; R4 is methyl, ethyl, HO, H, or absent; A1 is C or N; A2 is C or N; R6 is H or OH; R5 is: (t), (u), (v), (w), (x), (y), (z).