- TETRAHYDRO-BENZOAZEPINE GLYCOSIDASE INHIBITORS
-
Compounds of formula (I') wherein A, R1, R2, T1, T2, T3, T4, L, W, Z, R''', m and n have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
- -
-
Page/Page column 131-132
(2020/03/15)
-
- FUSED GLYCOSIDASE INHIBITORS
-
Compounds of formula (I), wherein A, Z, E, R1, R2, m and n have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
- -
-
Page/Page column 120
(2020/09/08)
-
- Meta C-H Arylation of Electron-Rich Arenes: Reversing the Conventional Site Selectivity
-
Controlling site selectivity of C-H activation without using a directing group remains a significant challenge. While Pd(II) catalysts modulated by a mutually repulsive pyridine-type ligand have been shown to favor the relatively electron-rich carbon centers of arenes, reversing the selectivity to favor palladation at the relatively electron-deficient positions has not been possible. Herein we report the first catalytic system that effectively performs meta C-H arylation of a variety of alkoxy aromatics including 2,3-dihydrobenzofuran and chromane with exclusive meta site selectivity, thus reversing the conventional site selectivity governed by native electronic effects. The identification of an effective ligand and modified norbornene (NBE-CO2Me), as well as taking advantage of the statistics, are essential for achieving the exclusive meta selectivity.
- Liu, Luo-Yan,Qiao, Jennifer X.,Yeung, Kap-Sun,Ewing, William R.,Yu, Jin-Quan
-
supporting information
p. 14870 - 14877
(2019/10/02)
-
- NOVEL PYRAZOLE DERIVATIVE AS ALK5 INHIBITOR AND USES THEREOF
-
The present disclosure relates to a novel substituted pyrazole derivative having an effect of inhibiting serine/threonine kinase activity targeting receptor ALK5 of TGF-β, and a pharmaceutical composition including the compound of the present disclosure as an active ingredient may be useful in preventing and/or treating cancers, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, pulmonary diseases, cardiovascular diseases or metabolic diseases, or other diseases associated with a decrease in TGF family signaling activity.
- -
-
Paragraph 0056; 0057
(2019/05/16)
-
- LINEAR GLYCOSIDASE INHIBITORS
-
Compounds of formula (I) wherein A, R, W, Q, L, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
- -
-
Page/Page column 68
(2019/03/14)
-
- GLYCOSIDASE INHIBITORS
-
Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
- -
-
Page/Page column 95
(2017/09/15)
-
- GLYCOSIDASE INHIBITORS
-
Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
- -
-
Page/Page column 80
(2017/09/15)
-
- ANTI-HCMV COMPOSITIONS AND METHODS
-
Novel compounds useful for treating and/or preventing HCMV infections are provided.
- -
-
-
- GLYCOSIDASE INHIBITORS
-
Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
- -
-
Page/Page column 80
(2016/03/22)
-
- PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF COMPLEX DISEASES AND THEIR DELIVERY BY INSERTABLE MEDICAL DEVICES
-
The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.
- -
-
Page/Page column 99-101
(2008/06/13)
-
- Tri-and bi-cyclic heteroaryl histamine-3 receptor ligands
-
Compounds of formula (I) wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R3b, R4, R5, L, X, X′, Y, Y′, Z, and Z′ are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
- -
-
Page/Page column 35
(2010/02/14)
-
- Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
-
Compounds of formula (I) wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R3b, R4, R5
- -
-
Page/Page column 35
(2010/02/14)
-
- The Thermolysis of Polyazapentadienes. Part 2. Formation of Quinoxalines from 5-Aryl-1-phenyl-1,2,5-triazapentadienes
-
Thermolysis in the gas phase of 5-(p-substituted phenyl)-1-phenyl-1,2,5-triazapentadienes at 600 deg C and 10-2 Torr gives 6-substituted quinoxalines.The yield is ca. 30 percent, and is independent of the electronic nature of the substituent.The corresponding 5-(o-substituted) derivatives give 5-substituted quinoxalines, though the yield is lower, and quinoxaline itself is a major contaminant, due to ipso attack and ejection of the substituent. 5-(m-Substituted) derivatives give mixtures of 5- and 6-substituted quinoxalines on pyrolysis.The 5-isomer is dominant for compounds with m-alkyl substituents, while the 6-isomer is the major product for those with electron-withdrawing or electron-donating m-substituents.
- McNab, Hamish
-
p. 1941 - 1946
(2007/10/02)
-