Abstract: Compounds of the formula I; useful for the treatment of pain wherein A, Z, B, R1, X and D are as defined in the specification, methods of making such compounds, methods of using such compounds and pharmaceutical compositions containing such compounds.

Abstract: Alpha-substituted pyridazino-quinoline compounds of formula Ia useful for the treatment of strokes and neurodegenerative disorders: wherein R1 is selected from a variety of substituents including halogen, (C1-C4)alkyl and nitro; R2 is selected from cycloalkyl moieties of 5-7 carbon atoms and the groups R2′ and R2″ as defined in the specification, a dashed bond indicates a single or double bond, and R7 is selected from H and CO(C1-C3)alkyl.

Abstract: Biocidal proteins capable of isolation from seeds have been characterized. The proteins have an amino acid sequence containing the common cysteine/glycine domain of Chitin-binding Plant Proteins but show substantially better activity against pathogenic fungi, a higher ratio of basic amino acids to acidic amino acids, and/or antifungal activity which results in increased hyphal branching. Antimicrobial proteins isolated from Amaranthus, Capsicum, Briza and related species are provided. The proteins show a wide range of antifungal activity and are active against Gram-positive bacteria. DNA encoding the proteins may be isolated and incorporated into vectors. Plants may be transformed with this DNA. The proteins find agricultural or pharmaceutical application as antifungal or antibacterial agents. Transgenic plants expressing the protein will show increased disease resistance.

Abstract: The present invention relates to carbapenems and provides a compound of the formula (I): or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R2 is hydrogen or C1-4alkyl; R3 is hydrogen or C1-4alkyl; R4 and R5 are the same or different and are selected from hydrogen, halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, C1-4alkoxycarbonyl, aminosulphonyl, C1-4alkylaminosulphonyl, di-C1-4-alkylaminosulphonyl, carbamoyl, C1-4alkylcarbamoyl, di-C1-4 alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C1-4alkylamino, di-C1-4alkylamino, C1-4alkanoylamino, C1-4alkanoyl(N—C1-4alkyl)amino, C1-4alkanesulphonamido and C1-4alkylS(O)n— wherein n is zero; one or two: with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to —NR3—.

Abstract: Compounds of formula I useful for inhibiting the pain enhancing effects of E-type prostaglandins are disclosed wherein A is a ring system in which the —CH(R3)N(R2)B—R1 and —OR4 groups are positioned in a 1,2 relationship to one another on ring carbon atoms. B is a ring system having R1 in a 1,3 or 1,4 relationship with the —CH(R1)N(R2)— linking group. A, B, R1, R2, R3 and R4 are as defined in the specification and may be substituted. Also disclosed are pharmaceutically-acceptable salts, in vivo-hydrolysable esters and amides of compounds of formula I, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and the use of such compounds as therapeutic agents.

Abstract: The invention concerns a compound of the formula (I): wherein, for example: R1 is of the formula —NHC(═O)Rb wherein Rb is, for example, (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; R2 and R3 are hydrogen or fluoro; D is O; R4 and R5 are hydrogen, (1-4C)alkyl or AR-oxymethyl; AR is phenyl or phenyl(1-4C)alkyl; R6 is hydrogen; >A—B— is of the formula >C═C(Ra)—, >CHCHRa—, or >C(OH)CHRa— (> represents two single bonds) wherein Ra is hydrogen or (1-4C)alkyl; and pharmaceutically-acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.

Abstract: The invention concerns compounds of formula (I), wherein: A is a 5 membered heteroaryl ring, a bicyclic benzo system containing such a 5 membered heteroaryl ring or a bicyclic or tricyclic heteroaryl ring system with at least one bridgehead nitrogen and optionally a further 1-3 heteroatoms chosen from oxygen, sulfur and nitrogen; R1 is, for example, hydroxy, halo, amino, nitro, cyano, carboxy, thiol, C1-4alkanoyloxy, C1-4alkoxycarbonyl, dimethylaminomethyleneaminocarbonyl, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, optionally substituted phenyl, an optionally substituted 5- or 6-membered heteroaryl ring or hydroxyC1-4alkyl; n is 0-6; R2 and R3 are independently hydrogen or fluoro; R4 is, for example, C1-4alkyl; pharmaceutically acceptable salts and in vivo hydrolysable ester thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.

Abstract: An isolated and purified human protein activator of apoptosis is described. A cDNA sequence which encodes the native kinase of death is disclosed as well as the structural coding region and the amino acid residue sequence. Methods are provided which employ the sequences to identify compounds that modulate the biological and/or pharmacological activity of the activator and hence regulate apoptosis. Biologically-effective antisense molecules, as well as dominant negative mutant versions of the apoptosis activator are described which are suitable for therapeutic use. The invention is also drawn toward the study, prevention, diagnosis, and treatment of pathophysiological disorders related to apoptosis.

Abstract: A novel human signal-transduction kinase polypeptide is described which is expressed at a particularly high level in human leukocytes. A full length cDNA which encodes the novel stress-activated serine/threonine kinase polypeptide is disclosed as well as the interior structural region and the amino acid residue sequence of the native biological molecule. Methods are provided to identify compounds that modulate the biological activity of the human Ste20-like stress-activated serine/threonine signal transduction kinase.

Abstract: An enzymatic process for preparing amides of Formula I wherein X, E and * have the meanings defined in the specification. Chiral intermediates useful for preparing compound of Formula I and enzymatic processes for preparing such chiral intermediates are also described.

Abstract: A compound library comprises a plurality of different units each comprising a solid support with which is associated a single member of the compound library, each solid support has a defined chemical composition which acts as an intrinsic label capable of identifying the first reaction choice in the synthesis of the associated member of the compound library.

Abstract: The invention concerns pharmaceutically useful compounds of the formula I, in which A1, A2, A3, A4, B1, m, Ar, W, X, Y, Z and R1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Abstract: The invention concerns a compound of formula (I) wherein for example R1 is of the formula —NHC(═O)Ra wherein Ra is hydrogen, or (1-4C)alkyl; R2 and R3 are independently hydrogen or fluoro, R4 is hydrogen, (1-4C)alkyl, halo or trifluoromethyl; R5 and R6 are, for example, independently hydrogen, (1-4C)alkyl, an acetylene of the formula -≡-H or -≡-(1-4C)alkyl, or a group of formula (IA) wherein, for example, Z is hydrogen or (1-4C)alkyl; X and Y are (1-4C)alkyl, halo, cyano, phenyl or heteroaryl; provided that X, Y and Z do not define a (2-4C)alkenyl group and provided that at least one of R5 and R6 is a group of formula (IA) or an acetylene of the formula -≡-H or -≡-(1-4C)alkyl; and pharmaceutically acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.

Abstract: An ink comprising water, a water-dissipatable polymer and one or more dyes of Formula (1): wherein: R1 is H or a substituent; R2 and R3 are each independently optionally substituted alkyl, aryl or aralkyl, or R2 and R3 together with the carbon atom to which they are attached form an optionally substituted ring; R4 is H or optionally substituted alkyl, aryl or aralkyl; and D is an optionally substituted arylene group. Also claimed are the dyes of Formula (1), ink jet printing processes and cartridges containing the inks.

Abstract: The present invention provides an improved process for preparing (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VIl) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.

Abstract: The present invention provides a method of producing a transformed banana plant (genus,Musa), in particular by tranforming embroygenic material, or the somatic embryos derived from a banana plant, through incubation with Agrobacterium cells carrying exogenous DNA sequence(s), and obtaining regenerated plants.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, m and M have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The present invention relates to particular forms of a novel 1-substituted-N-?2-methyl-1-(trifluoroacetyl)propyl!pyrrolidine-2-carboxam ide which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes pharmaceutical compositions containing such forms, processes for preparing the forms and intermediates useful in the synthesis of the forms.

Abstract: A method for treatment of tumors to which antibody A5B7 binds is disclosed. A5B7 is a monoclonal antibody which binds to carcinoembryonic antigen. The method comprises administering to a host in need of such treatment an effective amount of a system which comprises a conjugate comprising: antibody A5B7 or a humanized version of A5B7 linked to an enzyme selected from the group consisting of carboxypeptidase G2 (CPG2), nitroreductase, a human enzyme, a non-human enzyme rendered non-immunogenic in man and a humanized catalytic antibody; and a prodrug convertible under the influence of the conjugate into a cytotoxic drug.