The presently disclosed subject matter is directed to novel compounds of Formula I, Formula II, and Formula III, and stereoisomers thereof, and flavor compositions comprising the novel compounds.

The presently disclosed subject matter is directed to novel compounds of Formula I, Formula II, and Formula III, and stereoisomers thereof, and flavor compositions comprising the novel compounds.

The present invention relates to N-(5-arylamido-2-methylphenyl)-5-methylisoquoxazole-4-carboxamide derivative, or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising same. The compound according to the present invention exhibits an FMS kinase inhibitory activity and thus can be used as pharmaceutical composition for preventing and treating diseases associated therewith.

The present invention relates to N-(5-arylamido-2-methylphenyl)-5-methylisoquoxazole-4-carboxamide derivative, or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising same. The compound according to the present invention exhibits an FMS kinase inhibitory activity and thus can be used as pharmaceutical composition for preventing and treating diseases associated therewith.

Non-lactone carbocyclic and heterocyclic antagonists and agonists of bacterial quorum sensing. Pharmaceutical composition containing antagonists. Methods employing antagonists and agonists for modulation of quorum sensing. Compounds are exemplified by those of formula:
A-[Z].sub.n-L1-[Y].sub.q-W-[V].sub.m-L2-HG,
where A is an acyclic aliphatic group, and HG is an optionally substituted phenyl group. Compounds include those where m and n are both 0, W is —NH—, Y is present and is —CO—CH.sub.2—CO—, and L1 and L2 independently are —[CH.sub.2].sub.p1— and —[CH.sub.2].sub.p2—, where p1 and p2, independently, are 0 or integers ranging from 1-10.

Non-lactone carbocyclic modulators of bacterial quorum sensing. Pharmaceutical composition containing such modulators. Methods employing such modulators for modulation of quorum sensing. Compounds are exemplified by those of formula:
A-[Z].sub.n-L1-[Y]NH-L2-HG,
where A is an optionally substituted aryl or heteroaryl group having one or two 5- or 6-member rings with up to 1-3 heteroatoms in a ring, or a substituted or unsubstituted C1-C12 acyclic aliphatic group and HG is an optionally substituted cyclopentyl group. Compounds include those where n is 1 or 0, Z is CO, OCO, COO, NHCO, CONH, NHCONH, O, S, or NH.sub.2, Y is NHCO, COCH.sub.2C(Y1)-, or SO.sub.2, where Y1 is OH, SH, NH.sub.2 or F; and L1 and L2 independently are [CH.sub.2]p1- and [CH.sub.2]p2-, where p1 and p2, independently, are 0 or integers ranging from 1-3.

Non-lactone carbocyclic modulators of bacterial quorum sensing. Pharmaceutical composition containing such modulators. Methods employing such modulators for modulation of quorum sensing. Compounds are exemplified by those of formula:
A-[Z].sub.n-L1-[Y]NH-L2-HG,
where A is an optionally substituted aryl or heteroaryl group having one or two 5- or 6-member rings with up to 1-3 heteroatoms in a ring, or a substituted or unsubstituted C1-C12 acyclic aliphatic group and HG is an optionally substituted cyclopentyl group. Compounds include those where n is 1 or 0, Z is CO, OCO, COO, NHCO, CONH, NHCONH, O, S, or NH.sub.2, Y is NHCO, COCH.sub.2C(Y1)-, or SO.sub.2, where Y1 is OH, SH, NH.sub.2 or F; and L1 and L2 independently are [CH.sub.2]p1- and [CH.sub.2]p2-, where p1 and p2, independently, are 0 or integers ranging from 1-3.

The present invention relates to the compounds of formula (I) below:

##STR00001##

wherein: X represents an oxygen atom, a sulfur atom, a nitrogen atom or a CH radical, The bond XY and Y are absent if X represents an oxygen or sulfur atom, the bond XY and Y are present if X represents a nitrogen atom or a CH radical, When present, Y represents a group R if X represents a nitrogen atom, a hydrogen atom or a group NR.sup.1R.sup.2 if X represents a CH radical, (Het)Ar is an aromatic ring selected from the group consisting of aryl and heteroaryl groups, R.sup.3, R.sup.4, R.sup.5, R.sup.6 represent, independently of one another, a hydrogen atom, a halogen atom, a NR.sup.12R.sup.13, a SR.sup.14 group, a OR.sup.14 group or a CF.sub.3 group, When Y is NR.sup.1R.sup.2, the groups NR.sup.1R.sup.2 and (Het)Ar are in the cis-conformation,
or a pharmaceutically acceptable salt thereof,
for use in the treatment of proliferative diseases, infectious diseases, allergies, inflammation and/or asthma.

It is provided a process for the preparation of bimatoprost, which comprises: a) reacting a compound of formula (III) with ethylamine in the presence of a suitable solvent; and b) deprotecting compound obtained in step a) to obtain bimatoprost, wherein R.sup.1 is selected from (C.sub.1-C.sub.16)alkyl, (C.sub.1C.sub.16)haloalkyl, (C.sub.2-C.sub.16)alkenyl, (C.sub.2-C.sub.16)haloalkenyl, (C.sub.1-C.sub.16)alkoxy(C.sub.1-C.sub.16)alkyl, aryl, (C.sub.1-C.sub.16)alkylaryl, allyl, (CH.sub.2CH.sub.2O).sub.nCH.sub.3 wherein n=1, 2, 3 or 4, and CH(OCH.sub.2CH.sub.2).sub.2; R.sub.2 is selected from H, (C.sub.1-C.sub.16)alkyl, (C.sub.1-C.sub.16)haloalkyl, (C.sub.2-C.sub.16)alkenyl, (C.sub.2-C.sub.16)haloalkenyl, (C.sub.1-C.sub.16)alkoxy(CrC.sub.16)alkyl, aryl, (C.sub.1-C.sub.16)alkylaryl, allyl; or, alternatively, R.sup.1 and R.sup.2 taken together are selected from CH.sub.2CH.sub.2CH.sub.2, CH.sub.2CH.sub.2, OCH.sub.2CH.sub.2, and OCHCH. There are also provided intermediates useful in such preparation process. ##STR00001##

It is provided a process for the preparation of bimatoprost, which comprises: a) reacting a compound of formula (III) with ethylamine in the presence of a suitable solvent; and b) deprotecting compound obtained in step a) to obtain bimatoprost, wherein R.sup.1 is selected from (C.sub.1-C.sub.16)alkyl, (C.sub.1C.sub.16)haloalkyl, (C.sub.2-C.sub.16)alkenyl, (C.sub.2-C.sub.16)haloalkenyl, (C.sub.1-C.sub.16)alkoxy(C.sub.1-C.sub.16)alkyl, aryl, (C.sub.1-C.sub.16)alkylaryl, allyl, (CH.sub.2CH.sub.2O).sub.nCH.sub.3 wherein n=1, 2, 3 or 4, and CH(OCH.sub.2CH.sub.2).sub.2; R.sub.2 is selected from H, (C.sub.1-C.sub.16)alkyl, (C.sub.1-C.sub.16)haloalkyl, (C.sub.2-C.sub.16)alkenyl, (C.sub.2-C.sub.16)haloalkenyl, (C.sub.1-C.sub.16)alkoxy(CrC.sub.16)alkyl, aryl, (C.sub.1-C.sub.16)alkylaryl, allyl; or, alternatively, R.sup.1 and R.sup.2 taken together are selected from CH.sub.2CH.sub.2CH.sub.2, CH.sub.2CH.sub.2, OCH.sub.2CH.sub.2, and OCHCH. There are also provided intermediates useful in such preparation process. ##STR00001##