Abstract: Compounds having the structural formula ##STR1## which inhibit the enzymatic activity of proteolytic enzymes, and processes for preparation thereof, method of use thereof in treatment of degenerative diseases and pharmaceutical compositions thereof are disclosed.

Abstract: A process for the preparation of a 2-aminobenzothiazol of the formula ( I ) ##STR1## in which R.sub.1 and R.sub.2 independently of each other are hydrogen, fluorine, chlorine, bromine or iodine, trifluoromethyl or C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or nitro groups, by conversion of an arylthiourea of the formula (II) in which R.sub.1 and R.sub.2 have the meaning mentioned, which comprises carrying out the conversion in 99 to 100% strength of sulfuric acid with continuous addition of catalytic amounts of bromine, hydrogen bromide or bromide in the form of aqueous solutions and using an arylthiourea of the formula (II) which contains 1 to 35% water.

Abstract: Biocidal isothiazolinone or isothiazolothione compounds are stabilized with an effective amount of a free-radical scavenger compound. Exemplary of the biocidal isothiazolones are 1,2-benzisothiazolin-3-one, 2-methyl-4-5-trimethylene-4-isothiazolin-3-one, 5-chloro-2-methyl-4-isothiazolin-3-one and 2-methyl-4-isothiazolin-3-one. Effective free-radical scavengers include 3,3-thiodipropionic acid.

Abstract: Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula 0010wherein:L is --O--, --S--, --SO-- or --SO.sub.2 --; m and n are each independently 0 or 1; R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl; R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; and R.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.

Abstract: In a process for the preparation of 2-mercaptobenzothiazole from aniline, sulfur and carbon disulfide under pressure and for separation of the 2-mercaptobenzothiazole from the crude reaction product by cooling and recycling the desirable intermediates and by-products into the reactor together with aniline, sulfur and carbon disulfide, the reaction is carried out using a residence time in the reactor of at least one hour to a time before the 2-mercaptobenzothiazole product thus-formed begins to decompose into undesirable intermediate products. A maximum hydrogen sulfide pressure is maintained on quenching to a temperature ranging between 220 and 280.degree. C. by mixing the crude reaction product with carbon disulfide at a temperature sufficient to obtain a homogeneous quenched mixture. The hydrogen sulfide is removed completely only after crystallization of the 2-mercaptobenzothiazole.

Abstract: Hydantocidin is a potent non-selective herbicidal natural product. This invention provides an efficient method for the enantioselective preparation of (+)-hydantocidin, analogs thereof and intermediates therefor.

Abstract: Compounds of formula (I): ##STR1## [in which: R.sup.1 and R.sup.2 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl, aromatic heterocyclic, cyano or halogen; R.sup.3 is hydrogen, optionally substituted alkyl, aralkyl or acyl; R.sup.4 and R.sup.5 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl or aromatic heterocyclic]; and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Abstract: 7-(Diphenylmethyl)oxy-9a-methoxymitosane is a novel intermediate for conversion into 7-amino and 7-oxy-9a-methoxymitosanes and is also useful for inhibiting mammalian tumor growth. The compound is prepared by reacting 7-hydroxy-9a-methoxymitosane with diazodiphenylmethane. In a preferred reaction, the compound is prepared from mitomycin C via 7-hydroxy-9a-methoxymitosane without drying (water removal). The intermediate is advantageously converted to the very effective anti-tumor agent 7-[2-(4-nitrophenyldithio)ethylamino]-9a-methoxymitosane in unexpectedly high yields using a two step process where the first step constitutes conversion to 7-[2-(2-pyridyldithio)ethylamino]-9a-methoxymitosane or 7-[2-(3-nitro-2-pyridyldithio)ethylamino]-9a-methoxymitosane.

Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.

Abstract: Novel mitomycin derivatives represented by the formula (I) are obtained by introducing a substituent at the 6-position. The mitomycin derivatives of the present invention have an antitumor activity.

Abstract: New azinoneutromethines of the formula ##STR1## in which the symbols used have the meaning given in the description, a process for their preparation and their use in thermal and photochromic recording materials, as nonlinear optical materials, as photoconductors in electrophotography and for dyeing fibres and woven fabrics of polyester and plastics.

Abstract: Antimicrobial compounds of the formula ##STR1## wherein R is hydrogen, halogen, or (C.sub.1 -C.sub.4)alkyl group;R.sub.1 is hydrogen or halogen; alternatively, R and R1 may be taken together with the carbons to which they are attached to form a 5- to 7-membered carbocyclic ring, said ring optionally being aromatic;R.sub.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl group; andR3 is hydrogen, substituted or unsubstituted (C.sub.1 -C.sub.18)alkyl, substituted or unsubstituted (C.sub.2 -C.sub.18)alkenyl, substituted or unsubstituted (C.sub.2 -C.sub.18)alkynyl, substituted or unsubstituted (C.sub.4 -C.sub.8)cycloalkyl or cycloalkenyl, substituted or unsubstituted (C.sub.6 -C.sub.10)aryl or arylalkyl group are disclosed.

Abstract: Preparation of biocidal polymers and copolymers based on free radical-polymerizable and copolymerizable ethylenically unsaturated monomers containing monomer units composed of BCM salts of ethylenically unsaturated carboxylic acids, sulfonic acids or phosphonic acids, solutions thereof and preferably aqueous dispersions thereof. Processes for their preparation and their use as fungicidal and algicidal impregnating agents, paints and finishing agents for scumbles and dispersion paints providing protection against blue staining on wood, for synthetic resin renderings, for exposed concrete paints and for textile finishing agents.

Abstract: The therapeutic use of new salts of physostigmine in the treatment of syndromes related to changes in cerebral metabolism in the elderly is described. The new salts of physostigmine, which are based on phosphatidic acid, are highly lipophilic and exhibit excellent bioavailability when administered orally, transcutaneously or transepidermally.

Abstract: Antimicrobial compounds of the formula ##STR1## wherein R is hydrogen, halogen or (C.sub.1 -C.sub.4)alkyl group;R.sub.1 is hydrogen or halogen; alternatively, R and R1 may be taken together with the carbons to which they are attached to form a 5- to 7-membered carbocyclic ring, said ring optionally being aromatic;R.sub.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl group; andR3 is hydrogen, substituted or unsubstituted (C.sub.1 -C.sub.18)alkyl, substituted or unsubstituted (C.sub.2 -C.sub.18)alkenyl, substituted or unsubstituted (C.sub.2 -C.sub.18)alkynyl, substituted or unsubstituted (C.sub.4 -C.sub.8)cycloalkyl or cycloalkenyl, substituted or unsubstituted (C.sub.6 -C.sub.10)aryl or arylalkyl group are disclosed.

Abstract: Bis-benzthiazolyl alkyl sulfenimides are produced by a process in which alkyl amines are reacted with optionally substituted 2-mercaptobenzthiazoles in the presence of oxygen or oxygen-containing gases and copper and/or copper compounds and in the presence of inert organic solvents.

Abstract: Compounds of the formula: ##STR1## wherein the substituents are as described in the specification, antagonize LTD.sub.4 action and thus, are useful in treating bronchial asthma, pulmonary anaphylaxis, cystic fibrosis, chronic bronchitis, bronchiectasis, respiratory distress syndrome and pulmonary oedema.

Abstract: N,O-bis(trimethylsilyl)acetamide is improved in thermal stability by adding about 0.01 to 5 mol % of a 2-mercaptobenzothiazole or a salt thereof thereto.

Abstract: Novel heterocyclic compounds shown by the general formula ##STR1## or the pharmaceutically acceptable salts thereof useful as medicament in particular as antagonist of slow reacting substance of anaphylaxis (SRS-A).

Abstract: There are provided methods for producing solid anhydrous methylolhydantoins. Initially, an aqueous stirrable medium is dehydrated and heated to yield a substantially anhydrous stirrable melt. The aqueous stirrable medium includes (A) a solute selected from the group consisting of (i) a dimethyloldimethylhydantoin, (ii) a hydantoin reactant, (iii) a formaldehyde source reactant, or (iv) a combination of any of the foregoing; and (B) optionally a catalyst. A molten system is then provided by adding, to the stirrable melt, a reactant mixture which includes (A)(i) the same or a different hydantoin reactant, (ii) a substantially anhydrous formaldehyde source reactant which may be the same as or different than the formaldehyde source reactant, or (iii) a combination thereof; and (B) optionally, the same or a different catalyst; wherein the molten system includes (i) at least one hydantoin reactant and (ii) at least one dehydrated formaldehyde source reactant or substantially anhydrous formaldehyde source reactant.