194222-05-4Relevant articles and documents
Bioorthogonal Self-Immolative Linker Based on Grob Fragmentation
Avenoza, Alberto,Bernardes, Gon?alo J. L.,Busto, Jesús H.,Corzana, Francisco,Ferhati, Xhenti,García-Sanmartín, Josune,Garrido, Pablo,Guerreiro, Ana,Jiménez-Moreno, Ester,Martínez, Alfredo,Peregrina, Jesús M.,Salas-Cubero, Marina
supporting information, p. 8580 - 8584 (2021/11/17)
A self-immolative bioorthogonal conditionally cleavable linker based on Grob fragmentation is described. It is derived from 1,3-aminocyclohexanols and allows the release of sulfonate-containing compounds in aqueous media. Modulation of the amine pKa promo
THERAPEUTICALLY ACTIVE BICYCLIC-SULPHONAMIDES AND PHARMACEUTICAL COMPOSITIONS
-
Paragraph 0068, (2019/05/18)
Pharmaceutical compounds have a bicyclic-sulphonamide structure and pharmaceutical compositions including the compounds may be used in therapy as brain-cell-death protectants and may be used, for example, in the treatment of chronic neurodegenerative diseases. The compounds are active as inhibitors of N-acylethanolamine-hydrolysing acid amidase (NAAA) and may be used for the therapeutic treatment and prevention of pain and inflammatory disorders and other disorders which benefit from the modulation of fatty acid ethanolamides, particularly palmitoylethanolamide (PEA).
CYCLOHEXANE ANALOGUES AS GPR119 AGONISTS
-
, (2012/03/12)
This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and/or insulin sensitizers.