Abstract: Picornaviral 3C protease inhibitors of formula I, obtainable by chemical synthesis, that inhibit or block the biological activity of the picornaviral 3C protease are described. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Abstract: O-Benzyloxime ethers of the formula I where X is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano R3, R4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, N(R6)2, where R6 is H, alkyl, substituted or unsubstituted phenyl, —CO—N(R7)2, where R7 is H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylthio, substituted or unsubstituted hetaryl, substituted or unsubstituted hetaryloxy, substituted or unsubstituted hetarylthio, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocy

Abstract: The present invention relates to a process for the preparation of &ggr;-lactams of the general formula I 1

Abstract: The present invention provides compounds represented by the general formula (I): and a salt thereof, and anti-inflammatory agents and antitumor agents containing the compounds as the active ingredients.

Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to a process for the preparation of &ggr;-lactams of the general formula I The invention relates also to novel advantageous intermediates of the general formulae V, IV and II and their salts and their use. The compounds of the general formula I are obtained by cyclising compounds of the general formula II which can be prepared from the intermediate compounds V.

Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovis replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.

Abstract: The invention concerns a novel chemical process for the manufacture of methyl (2S)-2-[3R)-3-(N-[tert-butyloxycarbonyl]amino)-2-oxopyrrolidin-1-yl]propionate.

Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.

Abstract: An anhydrous crystal of a compound represented by the formula: R2—CH2CONH—R1 wherein R1 represents a substituted or non-substituted pyridyl group or substituted or non-substituted phenyl group and R2 represents a substituted or non-substituted 2-oxo-1-pyrrolidinyl group, characterized in that said crystal is substantially free from hygroscopicity. For example, by drying a hydrous crystal of said compound at a temperature of 80° C. or above under reduced pressure, an anhydrous crystal is provided that exhibits a weight increase of 1% or less when stored under the relative humidity of 83% at the temperature of 25° C. for 30 days. By using the anhydrous crystal for the manufacture of a medicament comprising the compound as an active ingredient, a product with a constant content of the active ingredient can be obtained.

Abstract: The subject of the invention is the compounds of formula (I):Q(CH.sub.2).sub.a --(X.sub.1).sub.b --Q.sub.1 --Q.sub.2 --C(X.sub.2)--N(R.sub.1)(R.sub.2) (I)in which:Q represents an aryl radical,X.sub.1 represents oxy, thio, sulphinyl or sulphonyl,X.sub.2 represents oxygen or sulphur,Q.sub.1 represents a cyclopropanediyl radical,Q.sub.2 represents an arylene radical,R.sub.1 and R.sub.2 represent:either a hydrogen atom or a hydrocarbon radicalor one of the groupsR.sub.3 --C.dbd.X.sub.3, (R.sub.3).sub.2 --P.dbd.X.sub.3, T.sub.2 --R.sub.5 or S(O).sub.j --N(R.sub.6)(R.sub.7)in which X.sub.3 represents an oxygen atom or a sulphur atom, T.sub.2 represents a bivalent oxy, carbonyl or oxycarbonyl group and j is equal to 0, 1 or 2,their preparation process and their use as pesticides.

Abstract: This invention relates to processes for the synthesis of various optically active amino pyrrolidinyl stereoisomers, or enantiomers, that may be attached to quinolonecarboxylic acids or naphthyridones. Processes and essential intermediates are disclosed and claimed for the synthesis of compounds represented by the structure shown in figure BG.sub.4-1, below. ##STR1## where R.sup.50, R.sup.6 and R.sup.9 are defined independently and are H, --(C.sub.1 -C.sub.8)alkyl, --(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.6 -C.sub.12 aryl), --(C.sub.1 -C.sub.8)alkyl-(C.sub.6 -C.sub.12 aryl), or the aryl or alkyl is substituted with one to three of the following groups, (C.sub.6 -C.sub.12 aryl), (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3) alkoxy, halogen, trifluoromethyl;where R.sup.2 is --(C.sub.1 -C.sub.8)alkyl, --(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.6 -C.sub.12 aryl), --(C.sub.1 -C.sub.8)alkyl-(C.sub.6 -C.sub.

Abstract: The present invention relates to a process for preparing (S)- and (R)-.alpha.-ethyl-2-oxo-1-pyrrolidineacetamide and (R)-.alpha.-ethyl-2-oxo-1-pyrrolidineacetamide. According to this process, the enantiomeric resolution of the racemic mixture of .alpha.-ethyl-2-oxo-1-pyrrolidineacetamide is carried out by simulated mobile bed chromatography, using at least three columns filled with chiral stationary phase.This process makes it possible to achieve good production efficiency on the industrial scale.

Abstract: What is described herein is a crosslinked polyvinylpyrrolidone (PVPP) copolymer of vinyl pyrrolidone (VP) and monomer derived from 1-vinyl-3-(E)-ethylidene pyrrolidone (EVP).

Abstract: The present invention relates to a compound of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are as defined above, to pharmaceutical compositions and methods of treatment.

Abstract: Compounds of formula (I) ##STR1## wherein the substituents are as defined herein, are antiparasitic agents.

Abstract: Levetiracetam is prepared by optical resolution of etiracetam by means of preparative high performance liquid chromatography or continuous simulated moving bed chromatographic system using silica gel supporting amylose tris(3,5-dimethylphenylcarbamate) as a packing material.

Abstract: For the treatment of cancer, inflammation, and other conditions associated with matrix metalloproteinases or that are mediated by TNF.alpha. or enzymes involved in the shedding of L-selectin, CD23, the TNF receptors, IL-1 receptors, or IL-6 receptors, disclosed are compounds of the general formulaB--X--(CH.sub.2).sub.m --(CR.sup.1 R.sup.2).sub.n --W--COY.

Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.

Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.

Abstract: There are described according to the invention, compounds of formula (XXII).sup.a (relative stereochemistry indicated), wherein R.sub.2 is as defined in the specification. Compounds of formula (XXII).sup.a are useful as intermediates in the production of pharmaceuticals useful in the treatment of chronic bronchitis.

Abstract: The present invention relates to double prodrugs of pharmacologically active glycoprotein IIb/IIIa antagonists of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of lower alkyl of about 2 to about 8 carbon atoms, cycloalkyl, and aralkyl; R is selected from the group consisting of alkoxy, ##STR2## wherein R.sup.50 is H or alkyl; and ##STR3## wherein R.sup.50 is H or alkyl; and pharmaceutically acceptable salts thereof.

Abstract: What is described herein is a crosslinked polyvinylpyrrolidone (PVPP) copolymer of vinyl pyrrolidone (VP) and monomer derived from 1-vinyl-3-(E)-ethylidene pyrrolidone (EVP).

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: 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: Provided are methods for the synthesis of N-cyclic maleamic acids and N-cyclic maleimide derivatives, as well as N-cyclic maleamic acids and N-cyclic maleimides synthesized thereby. The method for synthesis of an N-cyclic maleamic acid involves reacting an amino group-containing N-cyclic compound with maleic anhydride in acetic acid to obtain an N-cyclic maleamic acid. An N-cyclic maleimide can be formed by adding hexamethyldisilazane to an N-cyclic maleamic acid prepared according to the above-described method, thereby cyclizing a maleamic acid site of the N-cyclic maleamic acid. The described methods allow for the products to be obtained at high yields.

Abstract: This invention relates to processes for the synthesis of various optically active amino pyrrolidinyl stereoisomers, or enantiomers, that may be attached to quinolonecarboxylic acids or naphthyridones. Processes and essential intermediates are disclosed and claimed for the synthesis of compounds represented by the structure shown in figure BG.sub.4-1, below. ##STR1## where R.sup.50, R.sup.6 and R.sup.9 are defined independently and are H, --(C.sub.1 -C.sub.8)alkyl, --(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.6 -C.sub.12 aryl), --(C.sub.1 -C.sub.8) alkyl-(C.sub.6 -C.sub.12 aryl), or the aryl or alkyl is substituted with one to three of the following groups, (C.sub.6 -C.sub.12 aryl), (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3) alkoxy, halogen, trifluoromethyl;where R.sup.2 is --(C.sub.1 -C.sub.8)alkyl, --(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.1 -C.sub.8)alkyl-(C.sub.3 -C.sub.8)cycloalkyl, --(C.sub.6 -C.sub.12 aryl), --(C.sub.1 -C.sub.8)alkyl-(C.sub.6 -C.sub.

Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of 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 aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.

Abstract: The present invention discloses peptide aldehydes having a lactam group as part of the peptide backbone and having an original mimic group such as an amidinopiperidine or amidinophengyl tail. These compounds are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Abstract: A class of novel pyrroles is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.

Abstract: The present invention relates to novel N-(4-substituted-benzyl)-2-aminolactams as therapeutic agents, pharmaceutical compositions and a process of preparation.

Abstract: The present invention is directed to a composition containing the reaction product of:(A) a cyclic compound containing a 5, 6, or 7-member ring, the ring containing at least one nitrogen and at least one carbonyl group, at least one carbonyl group being adjacent to at least one said nitrogen;(B) an aldehyde or ketone of 1 to about 15 carbon atoms, or a reactive equivalent thereof; and(C) an etheramine represented by the formulaR.sup.4 (O(CH.sub.2 CH(R)O).sub.n --R.sup.3 --NH.sub.2).sub.y(C-I)wherein in formula (C-I), each n independently is a number from 0 to about 50; each R independently is selected from the group consisting of hydrogen, hydrocarbyl groups of 1 to about 16 carbon atoms, and mixtures thereof; R.sup.3 is selected from the group consisting of hydrocarbylene groups of about 2 to about 18 carbon atoms and groups represented by the formula ##STR1## wherein R.sup.5 and each R.sup.

Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of 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 aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.

Abstract: Compounds of the formula I ##STR1## are claimed, as are their preparation and use, in which the radicals R.sub.1, R.sub.2 and R.sub.3 are organic substituents, L is either a lactam or a cyclic amidine and X is an appropriate anion. The novel compounds are employed as bleach activators in cleaners and detergents which have a bleaching action.

Abstract: Conformationally constrained diacylglycerol analogues, pharmaceutical compositions comprising such analogues, and methods of using such analogues as agonists and antagonists of protein kinase C.

Abstract: An improved process for the catalytic hydrogenation of nitriles. The basic process comprises contacting the nitrile with hydrogen in the presence of a sponge or Raney cobalt catalyst under conditions for effecting conversion of the nitrile group to the primary amine. The improvement in the hydrogenation process resides in effecting the hydrogenation in the presence of a catalytic amount of lithium hydroxide and water. To achieve a catalytic amount of lithium hydroxide, the catalyst may be pretreated with the lithium hydroxide and/or the reaction may be carried out with the lithium hydroxide present in the reaction medium.

Abstract: An amidinonaphthyl derivative represented by the following general formula (I) which has coagulation factor X inhibiting action and is useful as an anti-thrombus agent and the like, a salt thereof, an intermediate thereof and a pharmaceutical composition which comprises the amidinonaphthyl derivative. An amidinonaphthyl derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof. ##STR1## (symbols in the formula have the following meanings; R.sup.1 : a hydrogen atom or a group represented by the formula --A--W--R.sup.4,A: a group represented by the formula ##STR2## a group represented by the formula ##STR3## or a group represented by the formula --SO.sub.2 --, X: an oxygen atom or a sulfur atom, W: a single bond or a group represented by the formula --NR.sup.5 --, R.sup.4 : a hydroxyl group, a lower alkoxy group, etc., R.sup.5 : a hydrogen atom, a carbamoyl group, a lower alkoxycarbonyl group, etc., R.sup.2 : a lower alkyl group, R.sup.

Abstract: A dye of Formula (1): ##STR1## wherein: D is a group of Formula (2): ##STR2## or a group of Formula (3): ##STR3## or a group of Formula (4): ##STR4## The variables are defined in the disclosures. The dyes and dye mixtures produce blue to green shades on synthetic textile materials such as polyester which have good build up and good light- and wet-fastness.

Abstract: An active engine mount system for supporting an engine on a vehicle body is used for controlling the vertical movement of the vehicle body produced by irregularities of the road surface. The engine mount system comprises an actuator interposed between the engine and the vehicle body for applying a vertical force to the vehicle body so that the vertical acceleration of the vehicle body for each given condition of the road surface may be minimized by adjusting a contribution of the mass of the engine to the mass of the vehicle body. The engine mount system may consist of a full active or semi active mount system. By detecting the road condition ahead of the vehicle, a particularly favorable result can be achieved.

Abstract: Herbicidally active phenyldiketone compounds of the formula I ##STR1## in which the substituents have the following meanings: L and M are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.1 -C.sub.4 -alkoxy, it being possible for these groups to be unsubstituted or substituted by one to five halogen atoms or C.sub.1 -C.sub.4 -alkoxy, or halogen, cyano, nitro, a group --(Y).sub.n --S(O).sub.m R.sup.7 or a group --(Y).sub.n --CO--R.sup.8,Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical which has one to three hetero atoms selected from the group consisting of oxygen, sulfur or nitrogen and which is unsubstituted or substituted by halogen, cyano, nitro, a group --CO--R.sup.8, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, di-C.sub.1 -C.sub.

Abstract: Pyrazol-4-ylbenzoyl compounds of the formula I ##STR1## where Z is a 5- or 6-membered heterocyclic saturated or unsaturated radical, Q is a pyrazole ring and L and M are as defined in the specification, their use as herbicidal compounds and to processes for preparing the compounds.

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.6, Q, W and X are as defined herein.

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: This invention relates to a 2-acylaminopropanol compound represented by the formula (I): ##STR1## (wherein R.sup.1 represents a phenyl group which may be substituted by 1 to 3 same or different substituents selected from alkyl, alkoxy, hydroxyl, hydroxyalkyl and nitro, R.sup.2 represents the following formula (II), (III), (IV), (V) or (VI), ##STR2## (wherein R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, m and p are those defined in the specification) R.sup.11 represents a hydrogen atom or a hydroxyl group, and n represents an integer of 3 to 15) or a pharmaceutically acceptable salt thereof.

Abstract: The invention is directed to an improved process for the preparation of spirocyclic lactams which utilizes diiodides in the spiro alkylation of lactams N-substituted with a tertiary amine group. The resultant spirocyclic lactams are useful in the production of various substituted azaspiranes which are useful as immunomodulatory agents.

Abstract: Process for preparing complex pesticidal 1-(haloaryl)heterocyclic compounds by reacting 1-(nitroaryl)heterocycles with metallic halide salts. 1-(Nitroaryl)pyrrole intermediates useful in said process.

Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.

Abstract: Compounds of the formula ##STR1## are inhibitors of peptide binding to major histocompatibility complex type II proteins and are useful in the treatment and prevention of autoimmune diseases including: rheumatoid arthritis, Type I diabetes, multiple sclerosis, lupus erythematosis, Graves disease and pemphigus. The present invention also provides novel compositions, methods of treatment employing the compounds of the present invention and methods of manufacture of the compounds of structural formula (I).

Abstract: The present invention provides novel hydroxamic acid derivatives represented by the compound of formula I ##STR1## or pharmaceutical acceptable salts thereof, wherein the compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, including collagenase, stromelysin, and gelatinase, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthrits, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis (invasion and growth), periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, and other diseases related to connective tissue degradation.