On November 29, 2012, Prime, Michael; Courtney, Stephen Martin; Marston, Richard; Dominguez, Celia; MacDonald, Douglas; Wityak, John published a patent.Application In Synthesis of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride The title of the patent was Preparation of piperidin-4-yl substituted acrylamides as transglutaminase TG2 inhibitors. And the patent contained the following:
The title compounds I [A = (un)substituted (hetero)aryl, heterocycloalkyl; B = (un)substituted mono- or bicyclic heterocycloalkyl; R1 = H, NO2, COR (wherein R = H, alkyl, cycloalkyl, etc.), etc.; R2 = H or alkyl; R3-R5 = H, F, Cl, alkyl; p = 0-3; q = 0-1], were prepared E.g., a multi-step synthesis of the acrylamide II, starting from tert-Bu piperidin-4-ylcarbamate and 6-chloropyridine-3-sulfonyl chloride, was described. Exemplified compounds I were tested for human TG2 activity. Certain compounds I were found to have IC50 value less than 100 nM (no specific data given). Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington’s disease. Also described are methods of treatment which include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents. The experimental process involved the reaction of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride(cas: 879562-21-7).Application In Synthesis of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride
The Article related to piperidinyl acrylamide preparation transglutaminase tg2 inhibitor combination chemotherapy, neurodegenerative disorder huntington’s disease treatment piperidinyl acrylamide preparation and other aspects.Application In Synthesis of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles