C07D209/04

AGENT FOR INTRODUCING PROTECTING GROUP FOR HYDROXY GROUP AND/OR MERCAPTO GROUP

A novel agent for introducing a protecting group for a hydroxy group and/or a mercapto group that can be introduced and removed under mild conditions is provided. The agent for introducing a protecting group for a hydroxy group and/or mercapto group of a substrate compound having the hydroxy group and/or mercapto group is represented by the following formula (I), wherein A represents a ring structure having 1 to 5 rings in which two carbon atoms of an adjacent benzene ring are included, the ring structure comprises a substituted or unsubstituted five-membered ring or six-membered ring and optionally include a heterocycle; each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 is independently a hydrogen atom or a linear or branched alkyl group having 1 to 5 carbon atoms; and X is a halogen atom or OSO.sub.2R.sup.5 (R.sup.5=an aryl group or an alkyl group).

AGENT FOR INTRODUCING PROTECTING GROUP FOR HYDROXY GROUP AND/OR MERCAPTO GROUP

A novel agent for introducing a protecting group for a hydroxy group and/or a mercapto group that can be introduced and removed under mild conditions is provided. The agent for introducing a protecting group for a hydroxy group and/or mercapto group of a substrate compound having the hydroxy group and/or mercapto group is represented by the following formula (I), wherein A represents a ring structure having 1 to 5 rings in which two carbon atoms of an adjacent benzene ring are included, the ring structure comprises a substituted or unsubstituted five-membered ring or six-membered ring and optionally include a heterocycle; each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 is independently a hydrogen atom or a linear or branched alkyl group having 1 to 5 carbon atoms; and X is a halogen atom or OSO.sub.2R.sup.5 (R.sup.5=an aryl group or an alkyl group).

ELECTROLYTE SOLUTION AND ELECTROCHEMICAL DEVICE
20170309412 · 2017-10-26 · ·

The present invention aims to provide an electrolyte solution containing a quaternary ammonium salt as an electrolyte salt and is capable of providing an electrochemical device having a high capacitance retention and reducing generation of gas. The electrolyte solution of the present invention contains a solvent, a quaternary ammonium salt, and a nitrogen-containing unsaturated cyclic compound. The unsaturated cyclic compound is a nitrogen-containing unsaturated heterocyclic compound. The unsaturated cyclic compound excludes salts of the unsaturated cyclic compound and ionic liquids obtainable from the unsaturated cyclic compound.

Mitoketoscins: mitochondrial-based therapeutics targeting ketone metabolism in cancer cells

The present disclosure relates to compounds that bind to at least one of ACAT1/2 and OXCT1/2 and inhibit mitochondrial ATP production, referred to herein as mitoketoscins. Methods of screening compounds for mitochondrial inhibition and anti-cancer properties are disclosed. Also described are methods of using mitoketoscins to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitoketoscins to provide anti-aging benefits. Specific mitoketoscin compounds are also disclosed.

ACTIVE METABOLITE OF 1-[(2-BROMOPHENYL)SULFONYL]-5-METHOXY-3-[(4-METHYL-1-PIPERAZINYL)METHYL]-1H-INDOLE DIMESYLATE MONOHYDRATE AND DIMESYLATE DIHYDRATE SALT OF ACTIVE METABOLITE

The present invention is directed to active metabolite of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole dimesylate monohydrate of formula (I). The present invention is also directed to dimesylate dihydrate salt of formula (II). The compounds of formula (I) and formula (II) are useful in the treatment of various disorders that are related to 5-HT.sub.6 receptor antagonist.

ACTIVE METABOLITE OF 1-[(2-BROMOPHENYL)SULFONYL]-5-METHOXY-3-[(4-METHYL-1-PIPERAZINYL)METHYL]-1H-INDOLE DIMESYLATE MONOHYDRATE AND DIMESYLATE DIHYDRATE SALT OF ACTIVE METABOLITE

The present invention is directed to active metabolite of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole dimesylate monohydrate of formula (I). The present invention is also directed to dimesylate dihydrate salt of formula (II). The compounds of formula (I) and formula (II) are useful in the treatment of various disorders that are related to 5-HT.sub.6 receptor antagonist.

Benzenesulfonyl-Asymmetric Ureas and Medical Uses Thereof
20170275301 · 2017-09-28 ·

Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.

Compounds, substrates and methods related to histone deacetylases
09745613 · 2017-08-29 · ·

The invention relates to methods for the identification of compounds, peptides and proteins that can act as substrates for histone deacetylases. The invention further relates to compounds of Formula I:
F.sub.1-X.sub.1-L.sub.1-X.sub.2-P.sub.1-X.sub.3-G.sub.1  (Formula I)
The invention relates to the treatment of diseases or disorders mediated by ARID1A (BAF250A).

N-terminally modified linear and branched polyamine conjugated peptidomimetics as antimicrobials agents

N-terminally modified linear and branched polyamine conjugated peptidomimetics as antimicrobials agents. The invention relates to therapeutically viable antibacterial compositions based on ultra short mimetic of host defense cationic peptides (HDCPs). The invention relates to template based N-terminal modified di-peptidomimetics with or without modifications in polyamine backbone as new antibacterial agents. Most active peptidomimetics were bactericidal and caused a rapid decrease in viability of broad range of Gram-positive and Gram-negative bacterial strains in low micromolar concentration range including activity against clinically relevant pathogen methicillin resistant S. aureus (MRSA) andmethicillin resistant S. epidermidis(MRSE). Further the peptidomimetics were effective against MRSA biofilms (formation inhibition/killing of preformed biofilms) in vitro and were non toxic to human red blood cells and peripheral blood mononuclear cells. The molecules described in present invention do not develop resistance against MRSA under in vitro conditions and hence may be used as topical agents or in similar applications.

N-terminally modified linear and branched polyamine conjugated peptidomimetics as antimicrobials agents

N-terminally modified linear and branched polyamine conjugated peptidomimetics as antimicrobials agents. The invention relates to therapeutically viable antibacterial compositions based on ultra short mimetic of host defense cationic peptides (HDCPs). The invention relates to template based N-terminal modified di-peptidomimetics with or without modifications in polyamine backbone as new antibacterial agents. Most active peptidomimetics were bactericidal and caused a rapid decrease in viability of broad range of Gram-positive and Gram-negative bacterial strains in low micromolar concentration range including activity against clinically relevant pathogen methicillin resistant S. aureus (MRSA) andmethicillin resistant S. epidermidis(MRSE). Further the peptidomimetics were effective against MRSA biofilms (formation inhibition/killing of preformed biofilms) in vitro and were non toxic to human red blood cells and peripheral blood mononuclear cells. The molecules described in present invention do not develop resistance against MRSA under in vitro conditions and hence may be used as topical agents or in similar applications.