Abstract: There is disclosed antibody molecules containing at least one CDR derived from a mouse monoclonal antibody having specificity for human TNF?. There is also disclosed a CDR grafted antibody wherein at least one of the CDRs is a hybrid CDR. Further disclosed are DNA sequences encoding the chains of the antibody molecules, vectors, transformed host cells and uses of the antibody molecules in the treatment of diseases mediated by TNF?.

Abstract: Single isomer methylphenidate, selected from the d- and l-threo-enantiomers, has been obtained in purified form, to the extent of less than 2% by weight of a contaminant selected from resolving agent and ritalinic acid. This is achieved by resolution of a mixture of enantiomers using an O,O′-diaroyltartaric acid as resolving agent.

Abstract: 1-Alkyl-substituted-quinolone-3-carboxamides have therapeutic utility via inhibition of Phosphodiesterase IV esterase and/or Tumour Necrosis Factor activity. The compounds of the invention have the general formula (I): ##STR1## The compounds of the invention encompassed by formula (I) include enantiomers, diastereoisomers and mixtures, including racemic mixtures.

Abstract: Described herein are compounds of formula (I): ##STR1## which have MMP and TNF inhibitory activity.

Abstract: The present invention concerns novel mercaptoalkylpeptidyl compounds of formula (I) which are useful inhibitors of matrix metalloproteinase and/or TNF-mediated diseases including degenerative diseases and certain cancers. The invention also concerns methods of treating patients suffering from disorders or diseases which can be attributed to or are associated with matrix metalloproteinase or TNF activity.

Abstract: An optically-purified enantiomer of the lactone 4-hydroxy-2-oxabicyclo-?3.3.0!oct-7-en-3-one or an acylate thereof can be obtained by biotransformation. It is a useful synthon in the preparation of an enantiomer of 3-hydroxymethyl-2-hydroxycyclopentene that can be used to prepare carbocyclic nucleosides as a desired enantiomer.

Abstract: The subject invention pertains to quinolinesulfonamides. The subject compounds can be used to treat disease states, such as those that are associated with proteins that mediate cellular activity, for example, by inhibiting phosphodiesterase IV (PDE IV) or tumor necrosis factor (TNF). The invention also pertains to methods of treating disease states, including those states capable of being modulated by inhibition of PDE IV or TNF.

Abstract: 1,3-Disubstituted-zanthines have therapeutic utility via TNF or phosphodiesterase inhibition.

Abstract: A process for the racemization of an enantiomerically-enriched compound of formula (3), comprises treatment of enantiomerically-enriched (3) with a base to obtain anion (4), optionally in protonated form, which is then combined with CH.sub.2 =CH--Y.sup.1 to form racemic (3), ##STR1## wherein Ar=aryl or heteroaryl; Ak=C.sub.1-20 alkyl; X=CN, CO.sub.2 R, CONR.sup.1 R.sup.2, and COR; Y and Y.sup.1 are independently selected from CN, CO.sub.2 R, CONR.sup.1 R.sup.2 and R, R.sub.1 and R.sub.2 are independently selected from H and C.sub.1-20 alkyl; optionally as a salt thereof.This racemization process can be used as part of an efficient synthesis of enantiomerically-enriched verapamil or aminoglutethimide.

Abstract: The subject invention pertains to a process for the resolution of etodolac comprising the use of the resolving agent glucamine or a N-(C.sub.1-4 alkyl)-glucamine. The subject invention also concerns a process for converting a single enantiomer of etodolac into the racemate. The method comprises forming all ester of the carboxylate function of the enantiomer and treating with an acid or base.

Abstract: The subject invention concerns novel compounds of the general formula (i) ##STR1## that are useful in treating disease states, such as those states associated with proteins that mediate cellular activity. The compounds of the subject invention can be used, for example, to inhibit tumor necrosis factor and/or phosphodiesterase IV, The subject invention also concerns methods for treating disease states using the compounds of the invention.

Abstract: A compound of formula (I) ##STR1## or a pharmaceutically-acceptable salt, solvate or hydrate thereof.

Abstract: A process for the racemisation of an optically-enriched piperidine-2-carboxanilide compound, comprises heating the compound in the presence of an alkanoic or arylalkanoic acid. A process for the asymmetric transformation of such a compound comprises heating the compound in the presence of an acid as defined above, a chiral acid resolving agent and an inert cosolvent.

Abstract: A process for preparing levobupivacaine, racemic bupivacaine or another N-alkyl analogue thereof, comprises chlorinating pipecolic acid hydrochloride, amidation of the resultant pipecolyl chloride hydrochloride in solvent, without isolation, with 2,6-dimethylaniline, and alkylation of the resultant pipecolic acid 2,6-xylidide. Alternatively, the alkylation may be followed by the amidation.

Abstract: 1-Alkyl-substituted-quinolone-3-carboxamides have therapeutic utility via inhibition of Phosphodiesterase IV esterase and/or Tumor Necrosis Factor activity.

Abstract: A process for the product of a 2,3-cis-dihydroxycycloalkane-1-carboxamide, comprises dihydroxylation of the corresponding cycloalkene-1-carboxamide. Some products are new. The stereoselective dihydroxylation is surprising.

Abstract: Compounds of formula I ##STR1## where n=0-2;R.sup.1 is H, NH.sub.2 or a halogen;R.sup.2 is H or NH.sub.2 ;R.sup.3 is any of the four groups ##STR2## where m=0 or 1; andX is O, NR.sup.5, or S(O).sub.0-2 and, in group (b), the X's may be the same or different.Compounds of the invention have utility as inhibitors of purine nucleoside phosphyorylase (PNP).

Abstract: An enzyme is provided which has acylase activity capable of hydrolyzing N-acetyl-(R,S)-pipecolic acid stereoselectively to give (S)-pipecolic acid, wherein this activity is greater than that on N-acetyl-S-proline, at pH 7.5, 25.degree. C., and substrate concentration 20 g/l, in 75 mM Tris buffer. The enzyme is obtainable from the species of Alcaligenes denitrificans deposited as NCIMB 40587. A microorganism having therein the enzyme also is provided, as is a process for preparing (S)-pipecolic acid comprising contacting a mixture of enantiomers of an N-acyl-pipe colic acid with the enzyme or microorganism.

Abstract: 3,4-Disubstituted-phenylsulphonamides have therapeutic utility via TNF or phosphodiesterase inhibition.

Abstract: The individual enantiomers of the compounds (Ia), (Ib), (IIa) or (IIb), optionally substituted by non-interfering substituent(s). The novel enantiomers can be obtained by biotransformation. The (Ia) or (IIa) compounds can be used for the synthesis of chiral carbocyclic nucleosides.