Abstract: This invention relates to certain 5-acyl-2-oxo-indole-3-carboxamides useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds. This invention also relates to pharmaceutical compositions comprising those 5-acyl-2-oxo-indole-3-carboxamides in combination with antidiabetes agents and methods of treating glycogen phosphorylase dependent diseases or conditions with such compositions.

Abstract: Compounds of the formula I ##STR1## in which B, D, E, R, W, Y, Z, b, c, d, e, f, g and have the meanings indicated in the claims, are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belongs to the group of integrins. The invention relates to the use of compounds of the formula I, and of pharmaceutical preparations which contain such compounds, for the treatment and prophylaxis of diseases which are caused by an un desired extent of leucocyte adhesion and/or leucocyte migration or which are associated therewith or in which cell--cell or cell-matrix interactions play a part which are based on interactions of VLA-4 receptors with their ligands, for example of inflammatory processes, rheumatoid arthritis or allergic disorders, and it also relates to the use of compounds of the formula I for the production of pharmaceuticals for use in such diseases. It further relates to novel compounds of the formula I.

Abstract: Photographic pyrazolotriazole dye forming coupler compound or coupler intermediate compounds can be readily prepared by inducing an elimination-addition reaction between certain pyrazolotriazole compounds and aromatic amines in the presence of an inorganic base or formate. Yields and purity are high, and reaction time is reduced with the specific set of conditions and reactants, and environmental impact from waste is reduced. The resulting compounds can be used themselves as photographic dye forming couplers or further reacted to prepare useful coupler compounds for photographic use.

Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.

Abstract: Described herein is a novel process to resolve a racemic compound into its optically active isomers without need for chemical transformation such as salt formation. The process advantageously utilizes polymers containing chiral moieties in their repeat units as well as exhibiting critical solution temperature behavior in a suitable solvent. An embodiment describes the resolution of tryptophan.

Abstract: A process for producing a lactam of the formula ##STR1## wherein 2-bromo-4 chloro butyryl bromide or 2,4-dibromo butyryl bromide is coupled with 4-aminobenzonitrile to produce 4-(2,4-bromobutyrylamino)-benzonitrile, which is combined with sodium hydroxide, potassium hydroxide or potassium carbonate to produce 4-(3-bromo-2-oxopyrrolidin-1-yl)benzonitrile which is subjected to an excess of ammonium hydroxide to produce compounds of the formula (I).

Abstract: 1-Aminopyrrolidine which is obtained by reacting hydrazine hydrate with a compound represented by the following formula (I):X.sup.1 --C.sub.4 H.sub.8 --X.sup.2 (I)wherein X.sup.1 and X.sup.2 are the same or different, and each represents a leaving group, in methanol; and a process for producing 1-aminopyrrolidine, comprising the step of reacting hydrazine hydrate with the above compound represented by formula (I) in methanol.

Abstract: Bifunctional compounds are characterized in that they have the following general formula: ##STR1## where n is zero or a whole number in the range 1 to 4, limits included, X is a substituent where the X groups are identical or different when n is a number from 2 to 4, and R is a divalent group.Use of these compounds as functionalising agents for a polyolefin by grafting the compound onto the paraffinic chain, or as compatibilising agents for incompatible polymers.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: An asymmetric dioxazine compound represented, when shown in free acid form, by the general formula (I): ##STR1## wherein T.sub.1 and T.sub.2 represent a hydrogen atom, a chlorine atom, a bromine atom, a lower alkyl group, a phenoxy group or others, A.sub.1 represents an alkyl group, a chlorine atom, a carboxyl group or others, A.sub.2 represents a hydrogen atom, an alkyl group, a chlorine atom, a carboxyl group or others, R represents a hydrogen atom or a lower alkyl group, X and Y represent a halogen atom, a fiber-reactive group or others, respectively, with the proviso that at least one of X and Y is a fiber-reactive group is provided.The compound is suitable for dyeing or printing of a fiber material or the like which has a hydroxy group and/or an amide group, and provides a blue-dyed product with various fastness, including particularly chlorine fastness.

Abstract: A process for preparing an activated carbon fiber composite material includes the steps of mixing carbon fibers, binder and water to form a slurry, molding the slurry to produce a green monolithic body, curing the monolithic body, carbonizing the cured monolith to produce a carbon fiber composite with an open, permeable structure and activating the composite. If pre-activated carbon fibers are utilized in the mixing step the carbonizing and activating steps are eliminated.

Abstract: In accordance with the present invention, there are provided improved methods for the preparation of maleimide monomers. This new method for the synthesis of maleimides is clearly superior to those documented in the prior art. Furthermore, the invention method utilizes materials with reduced toxicity, thus the overall process has a minimal impact on the environment. Thus, in accordance with the present invention, it has been discovered that certain amine salts can be successfully used to replace the polar, aprotic solvents cited in the prior art for the cyclodehydration of maleamic acids. The use of these salts provides competitive reaction times and product yields relative to results obtained with the polar, aprotic solvents. These salts have the advantage of having no vapor pressure and, therefore, have no possibility to co-distill with the water produced by the cyclodehydration reaction. Furthermore, such salts can be tailored to have desirable solubility characteristics (i.e.

Abstract: A process for preparing 2-oxindole includes catalytically reacting isatin with hydrazine hydrate in a polar solvent containing a dissolved weak base at an elevated temperature to form the 2-oxindole product.

Abstract: The present invention provides pyrazole compounds which are useful as nitrification inhibitors.

Abstract: Crystalline forms of atorvastatin and hydrates thereof are useful hypolipidemic and hypocholesterolemic agents.

Abstract: Calcium, magnesium, lidocaine and benzathine salts of 2-oxindole-1-carboxamides are useful for the treatment of joint disease by intra-articular administration.

Abstract: There is disclosed a process for producing hexahydrothieno[3,4-d]imidazole-2,4-diones of the formula (1): wherein R is the same or different and represents a lower alkyl group, an alkenyl group, an aryl group or an aralkyl group all of which may be substituted, which is characterized by the step of reacting hexahydrofuro[3,4-d]imidazole-2,4-diones of the formula (2): ##STR1## wherein R has the same meaning as described above with hydrogen sulfide in the presence of a basic compound and sulfur.

Abstract: The present invention is directed to the synthesis of useful products from the explosive trinitrotoluene. This substance has a limited shelf life as a reliable explosive and large quantities of it have and will become surplus. Ecologically safe, and preferably commercially useful ways of disposing of it are therefore much to be desired. In the present invention the end products are nitroindoles of the general formula 4-Z.sup.1,6-Z.sup.2 indole wherein Z.sup.1 and Z.sup.2 are the same or different and are halo or nitro provided at least one of said groups is nitro.

Abstract: Diphenyl-cyclopropene derivatives, their nontoxic, pharmaceutically acceptable acid addition salts and compositions are kapa opiods useful in the treatment of pain, inflammation, Parkinsonism, dystonia, cerebral ischemia, diuresis, asthma, psoriasis, irritable bowel syndrome and stroke.

Abstract: A compound represented by the formula (I): ##STR1## wherein R.sup.1 is an optionally substituted heterocyclic group; R.sup.2 is optionally substituted aryl or heterocyclic group; R.sup.3 is hydrogen, alkyl, alkenyl, or alkynyl; R.sup.4 is hydrogen, alkyl, alkoxy, halogen, nitro, cyano, or halogenated alkyl; M is oxygen, S(O).sub.i wherein i is 0, 1, or 2, NR.sup.5 wherein R.sup.5 is hydrogen, alkyl, or acyl, --Q--N.dbd.C(R.sup.6)--, --B--C(R.sup.8).dbd.N--, --CH.dbd.N--N.dbd.C(R.sup.9)--, or --CH.dbd.N--A--(CR.sup.10 R.sup.11)m--; and n is 0, 1, or 2, an intermediate for producing the same and an agrochemical composition containing the same as an active ingredient.