214541-51-2Relevant articles and documents
CYCLIC AMIDE DERIVATIVES AS INHIBITORS OF 11 - BETA - HYDROXYSTEROID DEHYDROGENASE AND USES THEREOF
-
, (2015/06/17)
The present invention relates to certain amide derivatives that have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.
CYCLIC AMIDE DERIVATIVES AS INHIBITORS OF 11 - BETA - HYDROXYSTEROID DEHYDROGENASE AND USES THEREOF
-
, (2013/09/12)
The present invention relates to certain amide derivatives that have the ability to inhibit 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and which are therefore useful in the treatment of certain disorders that can be prevented or treated by inhibition of this enzyme. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders. It is expected that the compounds of the invention will find application in the treatment of conditions such as non-insulin dependent type 2 diabetes mellitus (NIDDM), insulin resistance, obesity, impaired fasting glucose, impaired glucose tolerance, lipid disorders such as dyslipidemia, hypertension and as well as other diseases and conditions.
PPAR active compounds
-
, (2008/06/13)
Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
PPAR ACTIVE COMPOUNDS
-
Page 100-101, (2008/06/13)
Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
Heck cross-couplingg reaction of 3-iodoindazoles with methyl acrylate: A mild and flexible strategy to design 2-azatryptamines
Collot, Valérie,Varlet, Didier,Rault, Sylvain
, p. 4363 - 4366 (2007/10/03)
In order to design 2-azabioisosteres of tryptamine, serotonin or melatonin, the conditions of the Heck coupling reaction of 3-iodoindazoles with methyl acrylate are studied. This reaction authorizes the synthesis of 3-indazolylpropenoates as key intermediates to prepare 3-indazolylpropionic acids and 3-indazolylethylamines. The flexible synthetic strategy allows molecular diversity. (C) 2000 Elsevier Science Ltd.
Control of the Bacterial Wilt of Tomato Plants by a Derivative of 3-Indolepropionic Acid Based on Selective Actions on Ralstonia solanacearum
Matsuda, Kazuhiko,Toyoda, Hideyoshi,Nishio, Hitomi,Nishida, Takatsugu,Dohgo, Mitsue,Bingo, Miki,Matsuda, Yoshinori,Yoshida, Satoshi,Harada, Satoshi,Tanaka, Hiroshi,Komai, Koichiro,Ouchi, Seiji
, p. 4416 - 4419 (2007/10/03)
3-Indolepropionic acid (IPA)-related compounds having a benzo[b]thiophene or an indazole ring and derivatives having various substituents in the propionic acid moieties were tested for their antibacterial activity against Ralstonia solanacearum. Substitution of the indole ring for other aromatic rings resulted in lowered activity, whereas addition of a methyl or a trifluoromethyl group to the propionic acid moiety had little effect. Of the derivatives, 3-(3-indolyl)butanoic acid (3-IBA) was as active as IPA, exhibiting a 10-fold higher activity with the S configuration than with the R configuration. In contrast with the strong phytotoxicity of IPA, 3-IBA was able to suppress bacterial wilt without affecting the growth of tomato plants.