The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.

Provided are a compound represented by the following Formula (III), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt or solvate thereof used as a therapeutic agent for gout or hyperuricemia. (In the Formula (III), R.sup.1a, R.sup.2a, R.sup.6a, and R.sup.7a represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or a cyano group, R.sup.3a and R.sup.8a form a benzene ring or a 5-membered heteroaryl ring containing 1 to 3 heteroatoms, as a ring constituent element, selected from nitrogen atoms, oxygen atoms, and sulfur atoms together with two carbon atoms to which R.sup.3a and R.sup.8a are bonded, R.sup.4a and R.sup.5a form a benzene ring together with two carbon atoms to which R.sup.4a and R.sup.5a are bonded or represent any of the groups represented by R.sup.1a described above, W.sup.a represents CR.sup.10a or N, and where, R.sup.10a represents any of the groups represented by R.sup.1a, X.sup.a represents an oxygen atom or a sulfur atom, Y.sup.a represents an alkylene chain having 1 to 8 carbon atoms, and where, the alkylene chain may be substituted with an alkyl group having 1 to 8 carbon atoms and the alkylene chain may be a linear or branched alkylene chain, the branched alkylene chain may have a 3- to 7-membered ring formed by side chains bonded to carbon atoms which are the same as or different from each other, together with the carbon atoms to which the side chains are bonded and may have a double bond in the middle thereof, and Z.sup.a represents CO.sub.2H). ##STR00001##

Provided are a compound represented by the following Formula (III), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt or solvate thereof used as a therapeutic agent for gout or hyperuricemia. (In the Formula (III), R.sup.1a, R.sup.2a, R.sup.6a, and R.sup.7a represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or a cyano group, R.sup.3a and R.sup.8a form a benzene ring or a 5-membered heteroaryl ring containing 1 to 3 heteroatoms, as a ring constituent element, selected from nitrogen atoms, oxygen atoms, and sulfur atoms together with two carbon atoms to which R.sup.3a and R.sup.8a are bonded, R.sup.4a and R.sup.5a form a benzene ring together with two carbon atoms to which R.sup.4a and R.sup.5a are bonded or represent any of the groups represented by R.sup.1a described above, W.sup.a represents CR.sup.10a or N, and where, R.sup.10a represents any of the groups represented by R.sup.1a, X.sup.a represents an oxygen atom or a sulfur atom, Y.sup.a represents an alkylene chain having 1 to 8 carbon atoms, and where, the alkylene chain may be substituted with an alkyl group having 1 to 8 carbon atoms and the alkylene chain may be a linear or branched alkylene chain, the branched alkylene chain may have a 3- to 7-membered ring formed by side chains bonded to carbon atoms which are the same as or different from each other, together with the carbon atoms to which the side chains are bonded and may have a double bond in the middle thereof, and Z.sup.a represents CO.sub.2H). ##STR00001##

The present invention relates to compounds and compositions for inhibition of FASN, their synthesis, applications, and antidotes.

The present invention relates to compounds and compositions for inhibition of FASN, their synthesis, applications, and antidotes.

A compound having the formula (I):

##STR00001##

wherein: R.sup.1 is selected from the group consisting of: H, F, (C.sub.1-C.sub.6)alkoxy, and halo(C.sub.1-C.sub.6)alkyl; and R.sup.2 is an optionally substituted heteroaryl group, as well as processes for the preparation of the compound, and intermediate compounds.

A compound having the formula (I):

##STR00001##

wherein: R.sup.1 is selected from the group consisting of: H, F, (C.sub.1-C.sub.6)alkoxy, and halo(C.sub.1-C.sub.6)alkyl; and R.sup.2 is an optionally substituted heteroaryl group, as well as processes for the preparation of the compound, and intermediate compounds.

Disclosed are pnictogen-containing heterocyclic compounds of Formula (I)

##STR00001##

Each of R.sub.1, the heterocyclic ring H, A.sup.+, LG, and X.sup.? is defined herein. Also provided are methods of modifying a substrate using such a compound, conjugated biomolecules thus modified, and pharmaceutical compositions containing one of the conjugated biomolecules.

Disclosed are pnictogen-containing heterocyclic compounds of Formula (I)

##STR00001##

Each of R.sub.1, the heterocyclic ring H, A.sup.+, LG, and X.sup.? is defined herein. Also provided are methods of modifying a substrate using such a compound, conjugated biomolecules thus modified, and pharmaceutical compositions containing one of the conjugated biomolecules.

The invention provides methods for treating pain using compounds having the general formula:

##STR00001##

and pharmaceutically acceptable salts thereof, wherein the variables R.sup.A, subscript n, ring A, X.sup.2, L, subscript m, X.sup.1, ring D, R.sup.1, and R.sup.N have the meaning as described herein.