- 5-SULFAMOYL-2-HYDROXYBENZAMIDE DERIVATIVES
-
The invention is directed to substituted salicylamide derivatives. Specifically, the invention is directed to compounds according to Formula (I): wherein R, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, the treatment of HIV, autoimmune diseases, infections, atherosclerosis, and ischemia–reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
- -
-
Page/Page column 172
(2017/09/27)
-
- HETEROCYCLIC DERIVATIVES AND USE THEREOF
-
A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.
- -
-
Page/Page column 49
(2015/01/06)
-
- Extending the versatility of the Hemetsberger-Knittel indole synthesis through microwave and flow chemistry
-
Microwave, flow and combination methodologies have been applied to the synthesis of a number of substituted indoles. Based on the Hemetsberger-Knittel (HK) process, modifications allow formation of products rapidly and in high yield. Adapting the methodology allows formation of 2-unsubstituted indoles and derivatives, and a route to analogs of the antitumor agent PLX-4032 is demonstrated. The utility of the HK substrates is further demonstrated through bioconjugation and subsequent ring closure and via Huisgen type [3+2] cycloaddition chemistry, allowing formation of peptide adducts which can be subsequently labeled with fluorine tags.
- Ranasinghe, Nadeesha,Jones, Graham B.
-
p. 1740 - 1742
(2013/04/10)
-
- Bicyclic aromatic substituted pyridone derivative
-
Disclosed is a compound represented by the formula (I): Wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like; X1, X2 and X3 independently represent a methine group or a nitrogen atom; Y1 and Y3 independently represent a single bond, —O— or the like; Y2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methylene group or the like; L represents a single bond, a methylene group or the like; Z1 and Z2 independently represent a single bond, a C1-4 alkylene group or the like; Ar1 represents an aromatic carbocyclic ring or the like; and Ar2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.
- -
-
Page/Page column 46
(2009/10/30)
-
- CHEMICAL COMPOUNDS
-
The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.
- -
-
Page/Page column 133
(2009/01/24)
-
- BICYCLIC AROMATIC SUBSTITUTED PYRIDONE DERIVATIVE
-
Disclosed is a compound represented by the formula (I): wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like; X1, X2 and X3 independently represent a methine group or a nitrogen atom; Y1 and Y3 independently represent a single bond, -O- or the like; Y2 represents a lower alkylene group or the like; W1 to W4 independently represent a single bond, a methlene group or the like; L represents a single bond, a methylene group or the like; Z1 and Z2 independently represent a single bond, a C1-4 alkylene group or the like; Ar1 represents an aromatic carbocyclic ring or the like; and Ar2 represents a bicyclic aromatic carbocyclic ring or the like. The compound is useful as a pharmaceutical for a central disease, a cardiovascular disease or a metabolic disease.
- -
-
Page/Page column 73-74
(2010/11/26)
-
- Novel aromatic compounds possessing antifungal or antibacterial activity
-
The present invention provides novel compounds possessing antibacterial, antifungal, antiviral, anticancer, and/or antiparasitic activities. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds ar
- -
-
Page/Page column 35; 52
(2010/02/06)
-
- Synthesis of methyl 5- and 6-nitroindole-2-carboxylates by nitration of indoline-2-carboxylic acid
-
Indoline-2-carboxylic acid was transformed into 6-nitroindoline-2-carboxylic acid, the methyl ester of which was easily dehydrogenated by DDQ to methyl 6-nitroindole-2-carboxylate (total yield: 67%). Methyl 5-nitroindole-2-carboxylate was obtained by the nitration of methyl 1-acetylindoline-2-carboxylate acid followed by dehydrogenation with MnO2 in toluene in 40% total yield.
- Lavrenov, Sergei N.,Lakatosh, Sergei A.,Lysenkova, Ludmila N.,Korolev, Alexander M.,Preobrazhenskaya, Maria N.
-
p. 320 - 322
(2007/10/03)
-
- Substituted indoles as anti-AIDS pharmaceuticals
-
Substituted indoles of formula (I) STR1 are useful anti-AIDS pharmaceuticals.
- -
-
-
- Anti-aids piperazines
-
The present invention includes diaromatic substituted heterocyclic compounds (III) STR1 which are useful in treating individuals infected with the HIV virus. The invention includes certain previously generically disclosed anti-AIDS piperazinyl compounds (V) and a method of treating HIV infected individuals with the indoles of formula (V) and the anti-AIDS amines (X).
- -
-
-