861965-63-1Relevant articles and documents
2-ALKENYL-3-AMINOTHIOPHENE DERIVATIVE AND METHOD FOR PRODUCING THE SAME
-
Page/Page column 11, (2009/01/24)
Disclosed is a method for commercially producing 2-alkenyl-3-aminothiophene derivatives, which are useful as intermediates for agricultural chemicals, at low cost. Specifically disclosed is a method for introducing alkenyl groups into the 2-position of 3-aminothiophene derivatives by reacting 3-aminothiophene derivatives represented by the general formula (2) below or salts thereof with a ketone represented by the general formula (1) below without using a protecting group. Also specifically disclosed are 2-alkenyl-3-aminothiophene derivatives (3a) to (3d) which are useful as intermediates for agricultural chemicals,
New R/S-3,4-dihydro-2,2-dimethyl-2H-1-benzopyrans as KATP channel openers: Modulation of the 4-position
Florence, Xavier,Sebille, Sophie,Tullio, Pascal de,Lebrun, Philippe,Pirotte, Bernard
experimental part, p. 7723 - 7731 (2010/03/04)
The present work aimed at exploring a series of diversely 4-arylthiourea-substituted R/S-3,4-dihydro-2,2-dimethyl-6-halo-2H-1-benzopyrans structurally related to (±)-cromakalim. These new compounds were examined in vitro as putative potassium channel openers (PCOs) on rat pancreatic islets (inhibition of insulin release) as well as on rat aorta rings (relaxation of aorta ring) and their activity was compared to that of the reference KATP channel activators (±)-cromakalim, (±)-pinacidil, diazoxide and of previously reported cromakalim analogues. Structure-activity relationships indicated that the most pronounced inhibitory activity on the insulin secretory process was obtained with molecules bearing a strong meta- or para-electron-withdrawing group (CN or NO2) on the phenyl ring of the arylthiourea moiety at the 4-position of the benzopyran nucleus (compounds 12-23). Among those, R/S-6-chloro-4-(4-cyanophenylaminothiocarbonylamino)-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran (16) was found to be the most potent benzopyran-type inhibitor of insulin release ever described. Most of these original benzopyran derivatives show increased selectivity for pancreatic versus vascular tissue. Radioisotopic investigations indicated that these new compounds activated pancreatic KATP channels.
SUBSTITUTED AMIDE DERIVATIVES AS PROTEIN KINASE INHIBITORS
-
Page/Page column 151-152, (2008/06/13)
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.