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: The novel specific immunophilin ligands of the general formula I have an antiasthmatic and immunosuppressive action and are suitable for the preparation of drugs.

Abstract: Aromatic maleimides and methods using the same are disclosed. Polymerization of compositions which include the compounds of the invention may be activated by irradiating the composition with radiation.

Abstract: Caprolactam and hexamethylenediamine are prepared simultaneously starting from adiponitrile.

Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-.beta.-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-.beta.-lactones, and analogs thereof and their use as proteosome inhibitors.

Abstract: A method for producing pyrrolidine derivatives such as 3,4-epoxypyrrolodines, 3-pyrrolidols and the like, by oxidizing 3-pyrrolines with at least one peroxide in the presence of at least one acid is disclosed. The 3-pyrrolines are produced by deriving cis-2-butene compounds from cis-2-butene-1,4-diols and performing a cyclization between the cis-2-butene derivatives and at least one primary amine. The method may be performed as a one-pot synthesis and may be performed as a continuous reaction.

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: Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. ##STR1## In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z in which X.sub.1 =single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH.sub.2 radicals to be substituted; Z represents carboxyl, COOR.sub.6 (R.sub.6 =alkyl), CON(R.sub.7)(R.sub.8) (R.sub.7 =hydrogen or alkyl and R.sub.8 =hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR.sub.9).sub.2 (R.sub.9 =hydrogen or alkyl), an --NH--CO--T (T=hydrogen or optionally substituted alkyl) radical, or else--a ##STR2## radical, R.sub.1 and R.sub.

Abstract: A compound of the formula ##STR1## where R.sup.1 is the radical of the formula II or III ##STR2## is suitable for the production of a pharmaceutical for the treatment of inflammations, carcinomatous diseases, or autoimmune diseases. A compound of the formula IV ##STR3## is suitable for the production of specific antibodies against a compound of the formula I for the discovery of specific-binding proteins from cell extracts, serum, blood, or synovial fluids, for the purification of proteins, for the modification of microtiter plates, or for the preparation of chromatography material, in particular of affinity chromatography material, and for use in diagnostics.

Abstract: Substituted phthalimidocinnamic acid derivatives I ##STR1## where R.sup.1 is H or C.sub.1 -C.sub.4 -alkyl;R.sup.2 is H or halogen;R.sup.3 is CN, NO.sub.2, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkoxy or C.sub.1 -C.sub.6 -haloalkoxy;R.sup.4 is H, CN, NO.sub.2, halogen or C.sub.1 -C.sub.6 -alkyl;R.sup.5 is H, 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.6 -haloalkyl, C.sub.1 -C.sub.6 -cyanoalkyl, C.sub.1 -C.sub.6 -hydroxyalkyl, C.sub.1 -C.sub.6 -mercaptoalkyl, C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkylthio-C.sub.1 -C.sub.6 -alkyl;R.sup.6 is one of the radicals stated under R.sup.5 or CN, NO.sub.2, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -haloalkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -haloalkylthio, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.6 -alkyl, (C.sub.1 -C.sub.6 -alkoxy) carbonyl-C.sub.1 -C.sub.6 -alkyl, hydroxycarbonyl-C.sub.1 -C.sub.

Abstract: Disclosed are hydroxamic and carboxylic acid derivatives which are useful inhibitors of matrix metalloproteinase and/or TNF.alpha.-mediated diseases, including degenerative diseases and certain cancers.

Abstract: Ethers of polyalkyl or polyalkenyl N-hydroxyalkyl succinimides having the formula: ##STR1## or a fuel soluble salt thereof. The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.

Abstract: The present invention relates to novel 3-(cyclohexano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.

Abstract: The invention is concerned with a new process for the preparation of compounds of formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkoxy, cycloalkyl, cycloalkenyl, cycloalkyl-lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; the lower alkyl, cycloalkyl, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl and the heterocyclyl moieties being unsubstituted or substituted with at least one group selected from carboxy, amino, carbamoyl, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen, aminomethyl, mercapto, trifluoromethyl and trichloroethyl.The compounds prepared according to above mentioned process are useful in the preparation of cephem, isoxacephem and carbacephem derivatives.

Abstract: The invention is directed at novel fluorinated amide compounds of formula (1): ##STR1## wherein Rf is a divalent perfluoroalkylene or perfluoropolyether group, X is a group of formula (2), (3) or (4), and m is an integer inclusive of 0. ##STR2## R.sup.1 is a monovalent hydrocarbon group, and R.sup.2 is a divalent hydrocarbon group. These compounds can be used to obtain elastomers or cured resins having a high fluorine content and a low surface energy, making them effective as starting materials in the production of chemical and solvent-resistant elastomeric materials, parting agents, and water repellents.

Abstract: Compounds with fungicidal properties are presented having the formula ##STR1## wherein m and n are 0 or 1; X is hydrogen, halo, (C.sub.1 -C.sub.4)alkyl or alkoxy; Z is (C.sub.1 -C.sub.12) alkyl or haloalkyl; R, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently hydrogen, a halogen, lower alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, arylcycloalkyl, or heterocyclyl, optionally substituted with one or more halogen atoms.

Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group,Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--,--C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)X.sub.2 --CH.sub.2 --C*H(OH)--CH.sub.2 --NH--CO--R.sub.N (VIIIA)and processes for production of pharmacologically useful oxazolidinones.

Abstract: A compound having the formula, ##STR1## or any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof;whereinR is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; andR.sup.4 isphenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl;3,4-methylenedioxyphenyl;benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl and aryl;heteroaryl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.

Abstract: This invention relates to .alpha.-ketoamide inhibitors of multicatalytic protease (MCP), to compositions including such inhibitors, and to methods for the use of MCP inhibitors. The MCP inhibitors of the present invention are useful, for example, to retard loss of muscle mass incident to various physiological states.