Provided are a nonaqueous electrolyte capable of providing a nonaqueous electrolyte energy storage device with reduced direct current resistance and an increased capacity retention ratio after charge-discharge cycles, a nonaqueous electrolyte energy storage device including such a nonaqueous electrolyte, and a method for producing such a nonaqueous electrolyte energy storage device. One mode of the present invention is a nonaqueous electrolyte for an energy storage device, containing an additive represented by the following Formula (1) or Formula (2). In Formula (1), R.sup.1 to R.sup.4 are each independently a hydrogen atom or a group represented by NR, ORa, SRa, etc., with the proviso that at least one of R.sup.1 to R.sup.4 is a group represented by ORa, SRa, COORa, CORa, SO2Ra, or SO3Ra. In Formula (2), R.sup.5 to R.sup.7 are each independently a hydrogen atom or a group represented by NRb.sup.2, OR.sup.b, or SR.sup.b, with the proviso that at least one of R.sup.5 to R.sup.7 is a group represented by SRb.

##STR00001##

Provided are a nonaqueous electrolyte capable of providing a nonaqueous electrolyte energy storage device with reduced direct current resistance and an increased capacity retention ratio after charge-discharge cycles, a nonaqueous electrolyte energy storage device including such a nonaqueous electrolyte, and a method for producing such a nonaqueous electrolyte energy storage device. One mode of the present invention is a nonaqueous electrolyte for an energy storage device, containing an additive represented by the following Formula (1) or Formula (2). In Formula (1), R.sup.1 to R.sup.4 are each independently a hydrogen atom or a group represented by NR, ORa, SRa, etc., with the proviso that at least one of R.sup.1 to R.sup.4 is a group represented by ORa, SRa, COORa, CORa, SO2Ra, or SO3Ra. In Formula (2), R.sup.5 to R.sup.7 are each independently a hydrogen atom or a group represented by NRb.sup.2, OR.sup.b, or SR.sup.b, with the proviso that at least one of R.sup.5 to R.sup.7 is a group represented by SRb.

##STR00001##

The present invention relates to pyrimidone compounds used as Lp-PLA.sub.2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R.sub.1, R.sub.2, R.sub.3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA.sub.2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA.sub.2 enzyme. ##STR00001##

The present invention relates to pyrimidone compounds used as Lp-PLA.sub.2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R.sub.1, R.sub.2, R.sub.3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA.sub.2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA.sub.2 enzyme. ##STR00001##

A method of preparing an active agent or a salt thereof from a pro-drug first compound (1) comprising a propargyl group connected to an oxygen that is directly or indirectly connected to the active agent is provided, wherein the bond between the propargyl group and the oxygen is cleaved by reacting the first compound with palladium or gold, thereby releasing the active agent. Prodrug compositions suitable for use in the method are also provided.

A process for preparing, 1,1,3-trioxo-1,2-benzothiazole-6-carboxamide of formula (I) comprising: (a) oxidizing 2,5-dimethyl-benzenesulfonamide of formula (II) in the presence of an oxidizing agent to receive 2-sulfamoyl-terephthalic acid of formula (III); (b) converting the formed 2-sulfamoyl-terephthalic acid of formula (III) to receive 2-sulfamoyl-terephthalic acid derivative of formula (IV); and (c) reacting the resulting 2-sulfamoyl-terephthalic acid derivative of formula (IV) with ammonia (NH.sub.3) or ammonium containing-salt; wherein R represents OR or CI and R represents a branched or non-branched C.sub.1-C.sub.12 alkyl.

A compound represented by Formula (I): ##STR00001##
wherein ##STR00002##
or the like
Y.sup.1 is O or the like; Z.sup.1 is C(R.sup.4) or N; Z.sup.2a is C(R.sup.5a) or the like; Z.sup.3a is C(R.sup.6) or the like; R.sup.4, R.sup.5a and R.sup.6 are each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are each independently a hydrogen atom or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is ##STR00003##
or the like
Ring B is a 6-membered aromatic carbocycle or the like; R.sup.9a and R.sup.10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p1 is an integer from 0 to 3,
or a pharmaceutically acceptable salt thereof.

A compound represented by Formula (I): ##STR00001##
wherein ##STR00002##
or the like
Y.sup.1 is O or the like; Z.sup.1 is C(R.sup.4) or N; Z.sup.2a is C(R.sup.5a) or the like; Z.sup.3a is C(R.sup.6) or the like; R.sup.4, R.sup.5a and R.sup.6 are each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are each independently a hydrogen atom or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is ##STR00003##
or the like
Ring B is a 6-membered aromatic carbocycle or the like; R.sup.9a and R.sup.10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p1 is an integer from 0 to 3,
or a pharmaceutically acceptable salt thereof.

A compound represented by Formula (I):

Chemical Formula 1

##STR00001##

wherein
Chemical Formula 2

##STR00002##

or the like Y.sup.1 is O or the like; Z.sup.1 is C(R.sup.4) or N; Z.sup.2a is C(R.sup.5a) or the like; Z.sup.3a is C(R.sup.6) or the like; R.sup.4, R.sup.5a and R.sup.6 are each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are each independently a hydrogen atom or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is
Chemical Formula 3

##STR00003##

or the like Ring B is a 6-membered aromatic carbocycle or the like; R.sup.9a and R.sup.10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p is an integer from 0 to 3,
or a pharmaceutically acceptable salt thereof.

A compound represented by Formula (I):

Chemical Formula 1

##STR00001##

wherein
Chemical Formula 2

##STR00002##

or the like Y.sup.1 is O or the like; Z.sup.1 is C(R.sup.4) or N; Z.sup.2a is C(R.sup.5a) or the like; Z.sup.3a is C(R.sup.6) or the like; R.sup.4, R.sup.5a and R.sup.6 are each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are each independently a hydrogen atom or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is
Chemical Formula 3

##STR00003##

or the like Ring B is a 6-membered aromatic carbocycle or the like; R.sup.9a and R.sup.10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p is an integer from 0 to 3,
or a pharmaceutically acceptable salt thereof.