C07D207/06

C7-Fluoro Substituted Tetracycline Compounds

The present invention is directed to a compound represented by Structural Formula (A):

##STR00001##

or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

SMALL LIPOPEPTIDOMIMETIC INHIBITORS OF GHRELIN O-ACYL TRANSFERASE
20170275249 · 2017-09-28 ·

Compositions and methods are disclosed that relate to small molecule lipopeptidomimetic inhibitors of mammalian ghrelin O-acyl transferase (GOAT). Compounds of general Formula (I) and substructures thereof, i.e., Formulae (II), (IIa), (IIa1), (IIa2), (IIb), (IIb1), (IIb2), (IIc) and (III), are shown to exhibit potent inhibition of the octanoylation of ghrelin peptide, where the resulting non-octanoylated (des-acyl) form of ghrelin lacks GHSr ligand activity that is associated with weight gain and insulin resistance. These and related embodiments will find uses for treating subjects known to have, or suspected of being at risk for having, a condition that would benefit from a decreased level of acylated ghrelin peptide, such as type II diabetes, impaired glucose tolerance, insulin resistance, Prader-Willi syndrome (PWS) and obesity.

SMALL LIPOPEPTIDOMIMETIC INHIBITORS OF GHRELIN O-ACYL TRANSFERASE
20170275249 · 2017-09-28 ·

Compositions and methods are disclosed that relate to small molecule lipopeptidomimetic inhibitors of mammalian ghrelin O-acyl transferase (GOAT). Compounds of general Formula (I) and substructures thereof, i.e., Formulae (II), (IIa), (IIa1), (IIa2), (IIb), (IIb1), (IIb2), (IIc) and (III), are shown to exhibit potent inhibition of the octanoylation of ghrelin peptide, where the resulting non-octanoylated (des-acyl) form of ghrelin lacks GHSr ligand activity that is associated with weight gain and insulin resistance. These and related embodiments will find uses for treating subjects known to have, or suspected of being at risk for having, a condition that would benefit from a decreased level of acylated ghrelin peptide, such as type II diabetes, impaired glucose tolerance, insulin resistance, Prader-Willi syndrome (PWS) and obesity.

Electrolyte salt and electrolyte for electricity storage device, and electricity storage device
09738666 · 2017-08-22 · ·

Provided is an electrolyte salt comprising a quaternary ammonium cation indicated by formula (1) and a trimethylsilyl alkanesulfonate anion indicated by formula (2). ##STR00001##
(In the formula, R.sup.1-R.sup.4 each independently indicate a C1-4 alkyl group or an alkoxyalkyl group indicated by —(CH.sub.2).sub.n—OR. Any two among R.sup.1-R.sup.4 can mutually bond and form a ring together with a nitrogen atom to which same have bonded. The remaining two can mutually bond and form a spiro ring having a nitrogen atom as the spiro atom therefor. R indicates a methyl group or an ethyl group. n indicates 1 or 2 and m indicates 2 or 3.)

Electrolyte salt and electrolyte for electricity storage device, and electricity storage device
09738666 · 2017-08-22 · ·

Provided is an electrolyte salt comprising a quaternary ammonium cation indicated by formula (1) and a trimethylsilyl alkanesulfonate anion indicated by formula (2). ##STR00001##
(In the formula, R.sup.1-R.sup.4 each independently indicate a C1-4 alkyl group or an alkoxyalkyl group indicated by —(CH.sub.2).sub.n—OR. Any two among R.sup.1-R.sup.4 can mutually bond and form a ring together with a nitrogen atom to which same have bonded. The remaining two can mutually bond and form a spiro ring having a nitrogen atom as the spiro atom therefor. R indicates a methyl group or an ethyl group. n indicates 1 or 2 and m indicates 2 or 3.)

Photolabile pro-fragrances

Fragrances that provide a scent of freshness tend to be volatile and are therefore not very economical when used in typical applications such as washing or cleaning processes, so they have to be used in relatively large quantities to be able to produce adequate effects. The disclosed photolabile pro-fragrances provide a much longer-lasting sense of fragrance, in particular with a scent of freshness, when used in typical applications, thus allowing said fragrances to be used economically.

Photolabile pro-fragrances

Fragrances that provide a scent of freshness tend to be volatile and are therefore not very economical when used in typical applications such as washing or cleaning processes, so they have to be used in relatively large quantities to be able to produce adequate effects. The disclosed photolabile pro-fragrances provide a much longer-lasting sense of fragrance, in particular with a scent of freshness, when used in typical applications, thus allowing said fragrances to be used economically.

METHOD FOR MAKING PROPENAMIDE COMPOUND

A compound of formula (I),

##STR00001##

wherein R.sup.1 is an optionally substituted aryl or an optionally substituted heteroaryl, R.sup.2 is an optionally substituted aryl or an optionally substituted heteroaryl, and R.sup.3 is an optionally substituted alkylamino, an optionally substituted cycloalkylamino, an optionally substituted arylamino, an optionally substituted heterocyclylamino, an optionally substituted heterocyclyl, and an optionally substituted dialkylamino. A pharmaceutical composition which includes the compound of formula (I) and a pharmaceutically acceptable carrier and/or excipient. A method of treating colorectal cancer in a subject, whereby a therapeutically effective amount of the compound of formula (I) is administered to the subject.

METHOD FOR MAKING PROPENAMIDE COMPOUND

A compound of formula (I),

##STR00001##

wherein R.sup.1 is an optionally substituted aryl or an optionally substituted heteroaryl, R.sup.2 is an optionally substituted aryl or an optionally substituted heteroaryl, and R.sup.3 is an optionally substituted alkylamino, an optionally substituted cycloalkylamino, an optionally substituted arylamino, an optionally substituted heterocyclylamino, an optionally substituted heterocyclyl, and an optionally substituted dialkylamino. A pharmaceutical composition which includes the compound of formula (I) and a pharmaceutically acceptable carrier and/or excipient. A method of treating colorectal cancer in a subject, whereby a therapeutically effective amount of the compound of formula (I) is administered to the subject.

CATIONIC LIPID
20170224619 · 2017-08-10 · ·

The present invention provides a cationic lipid represented by the formula (I)

##STR00001##

wherein R.sup.1 and R.sup.2 each represents alkyl having 8 to 24 carbon atoms or the like; R.sup.3 represents a hydrogen atom, alkyl having 1 to 3 carbon atoms, the formula (A)

##STR00002##

wherein R.sup.4 and R.sup.5 each represents a hydrogen atom or the like, and n.sup.3 represents an integer from 2 to 6, or the formula (B)

##STR00003##

wherein R.sup.6 and R.sup.7 each represents a hydrogen atom or the like, and n.sup.4 represents an integer from 1 to 6; n.sup.1 represents an integer from 0 to 4; and n.sup.2 represents an integer from 1 to 4, provided that the case where n.sup.1 is 0 and n.sup.2 is 1 is excluded, and a composition which contains the cationic lipid and a nucleic acid, or the like.