Described herein is a process for antibiotic development comprising: (a) generating a compound of formula (III): ##STR00001##
or a salt or stereoisomer or prodrug thereof; wherein R.sup.1-R.sup.3 and R.sup.5-R.sup.10 are independently selected from H, alkyl group, substituted alkyl group, halogen, OH, NH.sub.2, or SH; R.sup.4 is H, alkyl group or substituted alkyl group; X.sup.1-X.sup.2 are independently selected from ═O, ═S, ═NH, H, alkyl, halogen, OH, SH, or NH.sub.2; W is a saturated acyclic hydrocarbon chain of 1 to 15 carbon atoms; and Z is a neutral or positively charged organic group comprising a nitrogen or phosphorus atom; and; and (b) determining efficacy of the compound to inhibit growth of a bacteria. Systems of drug development of these antibiotic compounds are also described.

New 2-deoxy-2,3-dehydro-sialic acids and 2,7-anhydro-sialic acids, which are useful as sialidase inhibitors, and enzymatic methods for preparing them are disclosed. The methods include forming a reaction mixture comprising a glycoside acceptor, a sialic acid donor, and a sialyltransferase; maintaining the reaction mixture under conditions sufficient to form a sialoside; and contacting the sialoside with a Streptococcus pneumoniae sialidase to form the sialic acid product. Methods for the inhibition and sialidases and the treatment of cancer and infectious diseases are also disclosed.

A polymerizable compound represented by formula (1). In formula (1), one of eight hydrogen atoms is substituted by a (meth)acryloyloxy group, and the rest seven hydrogen atoms are independently non-substituted or substituted by a saturated hydrocarbon group having 1 to 10 carbons. ##STR00001##

A polymerizable compound represented by formula (1). In formula (1), one of eight hydrogen atoms is substituted by a (meth)acryloyloxy group, and the rest seven hydrogen atoms are independently non-substituted or substituted by a saturated hydrocarbon group having 1 to 10 carbons. ##STR00001##

The present invention relates to toluenesulfonic acid addition salt crystals of 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3′,4′: 4,5]pyrrolo[1,2,3 -de]quinoxalin-8(7H)-yl)-1-(4-fluorophenyl)-1-butanone, and methods of using such crystals as 5-hydroxytryptamine 2 receptor agonists and antagonists in treating disorders of the central nervous system.

This present invention relates to a catalyst composition for a production process of δ-lactone from carbon dioxide and 1,3-butadiene that can efficiently catalyze the synthesis reaction of δ-lactone with good selectivity of δ-lactone, wherein said catalyst composition comprising: a) palladium metal complexes as shown in structure (I) [Formula should be inserted here] wherein, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents a group selected from a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an amine group, or optionally an alkenyl group, an alkynyl group, a phenyl group, a benzyl group, or a cyclic hydrocarbon group comprising a hetero atom; and b) phosphorus compound selected from a phosphine group having a general formula [Formula should be inserted here], wherein R.sup.5 is selected from an alkyl group, a cycloalkyl group, or an aryl group. ##STR00001##

This present invention relates to a catalyst composition for a production process of δ-lactone from carbon dioxide and 1,3-butadiene that can efficiently catalyze the synthesis reaction of δ-lactone with good selectivity of δ-lactone, wherein said catalyst composition comprising: a) palladium metal complexes as shown in structure (I) [Formula should be inserted here] wherein, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents a group selected from a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an amine group, or optionally an alkenyl group, an alkynyl group, a phenyl group, a benzyl group, or a cyclic hydrocarbon group comprising a hetero atom; and b) phosphorus compound selected from a phosphine group having a general formula [Formula should be inserted here], wherein R.sup.5 is selected from an alkyl group, a cycloalkyl group, or an aryl group. ##STR00001##

Drug conjugates of formula [D-(X)b-(AA)w-(L)-]n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, wherein: A is selected from (II) and (III) R.sub.1, R.sub.2 and R.sub.3 is H, OR.sub.a, OCOR.sub.a, OCO—OR.sub.a, alkyl, alkenyl, alkynyl, etc.; R.sub.3′ is, COR.sub.a, COOR.sub.a, CONR.sub.aR.sub.b, etc; each of R.sub.4 to R.sub.10 and R.sub.12 is alkyl, alkenyl or alkynyl; R.sub.11 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl, or R.sub.11 and R.sub.12+N+C atoms to which they are attached may form a heterocyclic group; each of R.sub.13 and R.sub.14 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl; each R.sub.a and R.sup.b is H, alkyl, alkenyl, alkynyl, etc.; each dotted line represents an optional additional bond; X is an extending group; AA is an amino acid unit; L is a linker group; w is 0 to 12; b is 0 or 1; A bis a moiety comprising at least one antigen binding site, and n is the ratio of the group [D-(X).sub.b-(AA).sub.w-(L)-] to the moiety comprising at least one antigen binding site and is in the range from 1 to 20, are useful in the treatment of cancer. ##STR00001##

Drug conjugates of formula [D-(X)b-(AA)w-(L)-]n-Ab wherein: D is a drug moiety having the following formula (I) or a pharmaceutically acceptable salt, ester, solvate, tautomer or stereoisomer thereof, wherein: A is selected from (II) and (III) R.sub.1, R.sub.2 and R.sub.3 is H, OR.sub.a, OCOR.sub.a, OCO—OR.sub.a, alkyl, alkenyl, alkynyl, etc.; R.sub.3′ is, COR.sub.a, COOR.sub.a, CONR.sub.aR.sub.b, etc; each of R.sub.4 to R.sub.10 and R.sub.12 is alkyl, alkenyl or alkynyl; R.sub.11 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl, or R.sub.11 and R.sub.12+N+C atoms to which they are attached may form a heterocyclic group; each of R.sub.13 and R.sub.14 is H, COR.sub.a, COOR.sub.a, alkyl, alkenyl or alkynyl; each R.sub.a and R.sup.b is H, alkyl, alkenyl, alkynyl, etc.; each dotted line represents an optional additional bond; X is an extending group; AA is an amino acid unit; L is a linker group; w is 0 to 12; b is 0 or 1; A bis a moiety comprising at least one antigen binding site, and n is the ratio of the group [D-(X).sub.b-(AA).sub.w-(L)-] to the moiety comprising at least one antigen binding site and is in the range from 1 to 20, are useful in the treatment of cancer. ##STR00001##

The invention relates to a process for the manufacture of the crystalline compound according to formula (I) comprising the steps (a) deacetylating the final intermediate (FI), (b) forming the crystalline compound according to formula (I) by reacting the deacetylated final intermediate of step (a) with L-proline and water and isolating the final reaction product; processes of manufacturing intermediates thereof; process intermediates and their uses in the processes according to the present invention.