Patent classifications
C07D233/54
Process for the production of condensed imidazolo derivatives
The present invention relates to a process for providing the compound of formula I, comprising the step of reacting a compound of formula VII with a base in the presence of an alkaline- or alkaline earth metal salt (MX), wherein LG is a leaving group. The presence of an alkaline- or alkaline earth metal salt was surprisingly found to render said reaction highly reliable in terms of the yield and purity of the compound of formula I obtained. In a further aspect, the present invention relates to the compound of formula I, having less than an amount of 1.50% or less than an amount of 1.25% or less than an amount of 1.00% or less than an amount of 0.75% or less than an amount of 0.50% or less than an amount of 0.25% or less than an amount of 0.10% of the compound of formula VIII. ##STR00001##
2-AMINO-N-(ARYLSULFINYL)-ACETAMIDE COMPOUNDS AS INHIBITORS OF BACTERIAL AMINOACYL-TRNA SYNTHETASE
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(arylsulfinyl)-acetamide compounds that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-t RNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.
##STR00001##
Organic electroluminescent materials and devices
Novel Pt tetradentate complexes having PtO bond is disclosed. These complexes are useful as emitters in phosphorescent OLEDs.
Organic electroluminescent materials and devices
Novel Pt tetradentate complexes having PtO bond is disclosed. These complexes are useful as emitters in phosphorescent OLEDs.
5-(4,5-bis(4-bromophenyl)-2-(4-methoxyphenyl)-1H-imidazol-1-yl)pentanoic acid as an antimicrobial compound
An 5-(4,5-bis(4-bromophenyl)-2-(4-methoxyphenyl)-1H-imidazol-1-yl)pentanoic compound, its synthesis, and its use as an antimicrobial agent.
Heterocyclic inhibitors of PCSK9
This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, PCSK9, or a pharmaceutically acceptable salt, solvate, prodrug or polymorph thereof, and to compositions and formulations comprising such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I): ##STR00001##
wherein A, D and Q are described herein.
Compounds and methods for IDO and TDO modulation, and indications therefor
Disclosed are compounds of Formula I(a): ##STR00001## or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein R.sup.4, R.sup.5, R.sup.6, R.sup.7, G.sup.1, G.sup.2 and Ring A are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
Compounds and methods for IDO and TDO modulation, and indications therefor
Disclosed are compounds of Formula I(a): ##STR00001## or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein R.sup.4, R.sup.5, R.sup.6, R.sup.7, G.sup.1, G.sup.2 and Ring A are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS
The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.
BIODEGRADABLE LIPIDS FOR THE DELIVERY OF ACTIVE AGENTS
The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.