Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula Y--CO--AA.sup.2 --AA.sup.1 --CO--NH--X. Processes for the synthesis of peptidyl .alpha.-ketoamide derivatives.

Abstract: A novel silver halide photographic material is disclosed, which comprises at least one methine dye represented by the following formula (I): ##STR1## wherein Z.sub.1 and Z.sub.2 each represents an atomic group required for the formation of a 5- or 6-membered nitrogen-containing heterocyclic nucleus; R.sub.1 represents an alkyl, aryl or heterocyclic group; R.sub.2 and R.sub.3 each represents an alkyl group, with the proviso that at least one of R.sub.2 and R.sub.3 represents an alkyl group substituted by an alkoxy or aryloxy group; L.sub.1, L.sub.2, L.sub.3, L.sub.4, L.sub.5, L.sub.6, and L.sub.7 each represents a methine group which may be substituted or unsubstituted; n.sub.1 and n.sub.2 each represents an integer 0 or 1; M represents a charge neutralizing ion; and m represents 0 or a higher number required for the neutralization of electric charge in the dye.

Abstract: Novel ruthenium complexes for use as immunosuppressive agents to prevent or significantly reduce graft rejection in organ and bone marrow transplantation are described. The ruthenium complexes can also be used as an immunosuppressant drug for T-lymphocyte mediated autoimmune diseases, such as diabetes, and may be useful in alleviating psoriasis and contact dermatitis.

Abstract: A treatment for stabilizing an isothiazolone compound comprising adding to the compound a stabilizing amount of a metal salt, wherein the cation of the metal salt is an alkali metal, and the anion is selected from the group consisting of acetate, citrate, phosphate and borate.

Abstract: The present invention relates to a compound of formulaW--X--Q--Y--CH(R.sup.1)--O--N.dbd.C(R.sup.2)--A--COMor a pharmaceutically acceptable salt thereof wherein W is optionally substituted aryl or heteroaryl; X is a valence bond, or methylene, divalent alkylene, alkenylene, alkynylene or alkyloxy; Q is a valence bond, or --O--, --S--, >NR.sup.4 or >NCOR.sup.5 ; Y is optionally substituted phenyl, biphenyl, naphthyl, tetrahydronaphthyl, indolyl, pyridyl, or benzo b!thienyl, thienyl, thiazolyl, or thiazolylphenyl; R.sup.1 is alkyl, cycloalkyl, alkoxyalkyl, aryl or arylalkyl, heteroaryl or heteroarylalkyl; R.sup.2 is hydrogen, alkyl or hydroxyalkyl; A is a valence bond or is selected from alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, pyridylene, thienylene and furylene; and M is a pharmaceutically acceptable, metabolically cleavable group, --OR.sup.6, --NR.sup.6 R.sup.

Abstract: A compound having the formula: ##STR1## wherein Ar, R.sup.4 and R.sup.5 are defined herein have pharmaceutical utility as proteolytic enzyme inhibitors.

Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.

Abstract: The invention relates to the use of 1-thiocarbamoyl-5-hydroxypyrazoles of the general formula ##STR1## in which the substituents denote the radicals mentioned in the description, as pharmaceutical agents for combating septic shock and the consequences thereof.

Abstract: A method for producing an alkylthiobenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of an alkylthiobenzamide with a halogen in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent and a subsequent reaction with a halogen; and a method for producing a 1,2-benzisothiazol-3-one by carrying out a reaction of a 2-(alkylthio)benzamide with a halogenating agent.

Abstract: Disclosed are a benzothiazolesulfonamide derivative represented by the formula (I) or a pharmaceutically acceptable acid addition salt thereof ##STR1## wherein A represents a lower alkylene group which is unsubstituted or substituted; R.sup.1 represents a hydrogen atom or a lower alkyl group; each of R.sup.2 and R.sup.3 independently represents a hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 are bonded together to form a lower alkylene group which is unsubstituted or substituted; and R.sup.4 represents a hydrogen atom, a lower alkyl group, an amidino group, or a phenyl-substituted lower alkyl group, wherein the lower alkyl group is substituted or unsubstituted, and the phenyl group is unsubstituted or substituted with a lower alkyl group, a lower alkoxy group, a halogen atom or a methylenedioxy group;a method for preparing the same; and a pharmaceutical composition comprising the same.

Abstract: The present invention relates to a process for the preparation of compounds of the general formula I ##STR1## in which R.sup.1 and R.sup.2 are defined as stated in claim 1, characterized in that a 1,1,1-tris(hydroxymethyl)-(C.sub.2 -C.sub.5)-alkane or 2,2-bis(hydroxymethyl)-1,3-propanediol is reacted with vinylphosphonic anhydride.

Abstract: The invention relates to substituted 1-naphthyl-3-pyrazolecarboxamides of formula I: ##STR1## Application: These compounds are useful for the treatment of neuropsychiatric disorders, especially those associated with a dysfunction of the dopaminergic systems.

Abstract: A liquid concentrate comprises between about 4 and about 25 wt % of an isothiazolinone compound or mixture of isothiazolinone compounds between about 25 and about 88 wt % of a plasticizer in which said isothiazolinone compound is soluble and between about 8 and about 50 wt % of a C.sub.6 -C.sub.12 monoalkylphenol(s) which stabilizes the concentrate against crystallization and/or freezing at sub-freezing conditions.

Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.

Abstract: A novel triazole derivative for use in an insecticide or an acaricide has a general formula [I]: ##STR1## (wherein R.sup.1 is an alkyl group, X is a hydrogen atom, a halogen atom or the like, n is an integer of 1-5, A is an oxygen atom, a sulfur atom or the like, k is 0 or 1, R.sup.2 is a hydrogen atom, a halogen atom or the like, m is an integer of 1-5) and controls various injurious insects and mites, particularly mites and aphids without damaging crops.

Abstract: This invention relates to N,N'-disubstituted-N,N'-diacylhydrazines which are useful as insecticides, compositions containing those compounds and methods of their use. This invention also relates to the production of intermediates useful in the production of such compounds.The compounds of this invention may be represented by the formula ##STR1## wherein R.sup.1 is cyano or H,R.sup.2 is branched alkyl,B is aryl or substituted aryl,R.sup.a is H or a variety of substituents, andZ forms a fused 5-member heterocyclic ring.

Abstract: The present invention provides a method of stabilizing solutions of 3-isothiazolone compound(s) selected from the group consisting of 5-chloro-2-methyl-3-isothiazolone, 2-methyl-3-isothiazolone, and mixtures thereof in water free of nitrate or nitrite by the use of extremely low levels of copper ion, and compositions comprising water solutions of 3-isothiazolone compound(s) selected from the group consisting of 5-chloro-2-methyl-3-isothiazolone, 2-methyl-3-isothiazolone, and mixtures thereof, and extremely low levels copper ion.

Abstract: There is provided an efficient single step process to produce 4-aryl-2-perfluoroalkyl-3-oxazolin-5-one from arylglycine and a perfluoroacylating agent in the presence of a phosphorous trihalide and a solvent.The oxazolinone is a key intermediate in the production of insecticidal, nematicidal and acaricidal arylpyrrole compounds.

Abstract: Methods and compositions are described for immobilizing anti-ligands, such as antibodies or antigens, hormones or hormone receptors, oligonucleotides, and polysaccharides on surfaces of solid substrates for various uses. The methods provide surfaces covered with caged binding members which comprise protecting groups capable of being removed upon application of a suitable energy source. Spatially addressed irradiation of predefined regions on the surface permits immobilization of anti-ligands at the activated regions on the surface. Cycles of irradiation on different regions of the surface and immobilization of different anti-ligands allows formation of an immobilized matrix of anti-ligands at defined sites on the surface. The immobilized matrix of anti-ligands permits simultaneous screenings of a liquid sample for ligands having high affinities for certain anti-ligands of the matrix. A preferred embodiment of the invention involves attaching photoactivatable biotin derivatives to a surface.

Abstract: Arthropodicidal compounds, compositions and methods of use of compounds having formula (I) wherein A, G, Z and R.sup.1 to R.sup.4, are as defined in the text.