Abstract: A surfactant which is the reaction product of a hydrocarbyl-substituted succinic anhydride or a reactive equivalent thereof with at least one water-dispersible amine-terminated poly(oxyalkylene), is effective for use in soil remediation.

Abstract: Substituted pyrrole derivatives of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

Abstract: Boron heterocycle steroid mimics are provided that are useful as pharmaceutical agents, particularly in the treatment of estrogen-dependent disorders such as estrogen-dependent cancers. The compounds are also useful in diagnostic techniques such as magnetic resonance imaging (MRI) and magnetic resonance spectroscopy (MRS), in boron neutron capture therapy, and in fluorescence emission-based modalities. Pharmaceutical formulations and methods of using the novel compounds are provided as well.

Abstract: A method for the preparation of .beta.-amino acid compounds is provided. The method includes contacting an amine nucleophile with an .alpha.,.beta.-unsaturated amide compound in the presence of a chiral Lewis acid complex. The chiral Lewis acid complex is formed from an azophilic metal salt and a chiral bisoxazolinylmethane compound. The selective amidolysis of one enantiomer of the .beta.-aminoamide product is also described.

Abstract: Disclosed herein are an imidazole derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 is a hydrogen atom, or an alkyl, alkoxy or alkoxycarbonyl group, and R.sup.2, R.sup.3 and R.sup.4 are the same or different from one another and are independently a hydrogen or halogen atom, an alkyl, halogenoalkyl, hydroxyl or alkoxy group, or the like, or a salt thereof, and a medicine comprising such a compound. The compound specifically suppresses the production of particular cytokine and is hence useful as an active ingredient for immune function modulators and the like.

Abstract: Compounds of the formula (I): ##STR1## and their pharmaceutically acceptable compositions are useful in inhibiting the activity of cyclic guanosine 3',5'-monophosphate phosphodiesterase.

Abstract: Process for the preparation of etodolac, comprising the following steps:a) reacting 7-ethyl-tryptophol of formula (II) with methyl 3-oxo-pentanoate of formula (III) thereby obtaining methyl 1,8-diethyl-1,3,4,9-tetrahydropyrano [3,4-bis] indole-1-acetate of formula (IV) in an apolar solvent;b) hydrolyzing the compound of formula (IV) to etodolac (I),wherein step (a) is carried out at a temperatures of between -20.degree. C. and +50.degree. C. in the presence of a concentrated mineral acid, the molar ratio of the inorganic acid to 7-ethyl-tryptophol being comprised between 0.5 and 5.

Abstract: The invention relates to derivatives of general formula I ##STR1## The invention also relates to pharmaceutical and cosmetic compositions comprising derivatives of general formula I.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the vitronectin receptors .alpha..nu..beta.3 and/or .alpha..nu..beta.5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, viral disease, and tumor growth.

Abstract: This invention relates to lactam and thiolactam derivatives having useful anticonvulsant and anxiolytic activity, pharmaceutical compositions containing these compounds and therapeutic applications using such compositions.

Abstract: A process for the production of a Mannich reagent comprises reacting formaldehyde, especially paraformaldehyde, with a secondary amine in the complete or almost complete absence of a solvent. An alternative comprises reacting a diaminomethane produced from a secondary amine, formaldehyde, especially paraformaldehyde, as well as water with one another in about equimolar amounts. The invention is also concerned with a process for the aminomethylation of .delta.-tocopherol or of tocopherol mixtures containing this and comprises using a Mannich reagent which has been produced in the above manner. After completion of this aminomethylation process excess Mannich reagent can be separated by distillation and can be reacted with water and formaldehyde, especially paraformaldehyde, in order to regenerate further Mannich reagent suitable for use in the aminomethylation, this regeneration representing a further aspect of the invention. Finally, the invention includes certain novel bis(aminomethyl)-.gamma.-tocopherols.

Abstract: The present application describes novel lactams and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.

Abstract: The compounds of the instant invention as those of Formula I ##STR1## or a pharmaceutically acceptable salt thereof are peripherally selective kappa opioid agonists that are useful in treating pain, inflammation, psoriasis and irritable bowel syndrome.

Abstract: Substituted 4,5-di(trifluoromethyl)pyrazoles I ##STR1## and salts thereof, Use: as herbicides; for the desiccation/defoliation of plants.

Abstract: This invention relates to novel compounds and derivatives thereof containing a trioxepane protected diol in addition to a hydrazone, hydrazine, amine, or cyclic urea moiety; methods for the preparation of said compounds; and the use of said compounds in processes to prepare human immunodeficiency virus (HIV) protease inhibitors which effectively inhibit HIV. The novel compounds provided by this invention have the formulae: ##STR1## wherein the substituents are as defined herein.

Abstract: Novel indole and azaindole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described: ##STR1## and pharmaceutically acceptable prodrugs and salts thereof.

Abstract: There is provided amino acid derivative formula I, ##STR1## wherein p, q, R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

Abstract: Aziridines may be subjected to a cyclooligomerization reaction to produce polyazacycloalkane compounds useful for example in the preparation of chelating agents for use in diagnostic imaging contrast agents. N-benzyl-aziridine in particular is useful as it can be cyclotetramerized and debenzylated to yield cyclen, a key intermediate in chelating agent preparation. The invention provides a particularly attractive route to production of N-benzyl and other N-arylmethyl aziridines of formula (I) where each R.sub.1 is independently hydrogen or a group AR and Ar is an optionally substituted phenyl group. The process comprises reacting a purified N-arylmethylethanolaminesulphonate ester with a base. N-arylmethyl-ethanolamine sulphonate ester of the formula R'NHCH.sub.2 CH.sub.2 OSO.sub.3 H, wherein the N-arylmethyl group R' is an N-(bisarylmethyl) or N-(triarylmethyl) group, as intermediates. In a further aspect, the invention provides compounds of formula (II) ##STR1## where Ar and R.sub.

Abstract: Xanthines of the formula I ##STR1## are useful in producing a superadditive increase in immunosuppressive action when combined with immunosuppressive compounds such as CysA or FK506.

Abstract: A compound of the formula:Ar.sub.1 --B--Ar.sub.2wherein Ar.sub.1 is unsubstituted or substituted phenyl, thienyl, furanyl, or pyrrolyl, in which each substituent of the substituted phenyl, substituted thienyl, substituted furanyl, and substituted pyrrolyl, independently, is aldehyde, acyl, ester, carboxyl, amido, nitrile, nitro, cyano, acetal, ketal, oxoalkyl, aminoalkyl, hydroxyalkyl, haloalkyl, iminoalkyl, acid halide, aminoalkylaminoalkyl, aminoalkylaminoalkylamino, hydroxyalkylaminoalkyl, or hydroxyalkylaminoalkylaminoalkyl; B is, --CH.dbd.CH--, or --C C--, in which R is H, alkyl, hydroxyl, alkoxy, ester, aldehyde, hydroxyalkyl, aminoalkyl, carboxyl, --CH(OR.sub.1).sub.2, or NR.sub.2 R.sub.3, where each R.sub.1, independently, is H, alkyl, or acyl; and each of R.sub.2 and R.sub.3, independently, is H, alkyl, hydroxyalkyl, or aminoalkyl; and Ar.sub.