Abstract: The pyrimido[1,2-a]indoles according to the invention are prepared by reacting appropriately substituted phenylacetic acid derivatives with phenylglycinols. The pyrimido[1,2-a]indoles can be used as active compounds in medicaments, in particular in medicaments with antiatherosclerotic activity.

Abstract: A class of pyrazolyl compounds is described for use in treating inflammation and inflammation related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R.sup.1 is selected from hydrido, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, C.sub.2 -C.sub.20 -alkynyl, C.sub.1 -C.sub.20 -haloalkyl, aryl-C.sub.1 -C.sub.20 -alkyl, heterocyclic-C.sub.1 -C.sub.20 -alkyl, heteroaryl-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -hydroxyalkyl, C.sub.1 -C.sub.10 -alkoxyalkyl, C.sub.1 -C.sub.20 -cyanoalkyl, C.sub.1 -C.sub.20 -aminoalkyl, C.sub.1 -C.sub.20 -alkylamino-C.sub.1 -C.sub.20 -alkyl, carboxy-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -alkoxycarbonyl-C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -alkylaminocarbonyl-C.sub.1 -C.sub.20 -alkyl, N-hydroxyaminocarbonyl-C.sub.1 -C.sub.20 -alkyl, N-hydroxy-N-C.sub.1 -C.sub.20 -alkyl-aminocarbonyl-C.sub.1 -C.sub.20 -alkyl, arylaminocarbonyl-C.sub.1 -C.sub.20 -alkyl and aminocarbonyl-C.sub.1 -C.sub.20 -alkyl;wherein R.sup.

Abstract: The present invention provides various novel oligonucleotide analogs having one or more properties that make the subject compounds superior to conventional oligonucleotides for use in procedures employing oligonucleotides. The compounds of the invention are oligonucleotide analogs in which the furanose ring of a naturally occurring nucleic acid is replaced with an amino acid or a modified amino alcohol residue. Some embodiments of the novel compounds of the invention are particularly useful for the antisense control of gene expression. The compounds of the invention may also be used as nucleic acid hybridization probes or as primers. Another aspect of the invention is to provide monomeric precursors of the oligonucleotide analogs of the invention. These monomeric precursors may be used to synthesize the subject polynucleotide analogs. Another aspect of the invention is to provide formulations of the subject polynucleotide analogs that are designed for the treatment or prevention of disease conditions.

Abstract: The compounds of the formula wherein A, R.sub.1, R.sub.3, X.sub.1, Y and Z are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses induced by CRF, such as stress and anxiety related disorders.

Abstract: The invention relates to a medicinal composition comprising a triazine derivative of the following general formula ?I! ##STR1## or a solvate thereof, or a salt thereof, as an active ingredient. In the above formula, R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen, unsubstituted or substituted alkyl aralkyl, or alkenyl, or jointly represent cyclic amino (NR.sup.1 R.sup.2) in combination with the adjacent nitrogen atom. The cyclic amino may contain nitrogen, oxygen, or sulfur as a ring member in addition to the adjacent nitrogen and may be further substituted. Excluded is the case in which NR.sup.1 R.sup.2 is NH.sub.2. The compound of the invention is useful as a therapeutic drug for hepatitis.

Abstract: Therapeutic compositions including a nonionic surfactant combined with long chain fatty acids, alkanes, amides or mono-unsaturated alcohols, particularly stearyl alcohol, erucyl alcohol, brassidyl alcohol, arachidyl alcohol, n-docosane, n-docosanoic acid, erucamide and stearic acid, or mixtures thereof, as active ingredients are disclosed. Methods of preventing or treating viral infections, treating skin or membrane inflammation or inhibiting cell proliferation using such compositions are disclosed.

Abstract: Disclosed is a novel near-infrared absorbing dye of formula: ##STR1## wherein X.sup.1, X.sup.2 independently represents --CR.sup.8 R.sup.9 --, --S--, --Se--, --NR.sup.10 --, --CH.dbd.CH-- or --O--;n is an integer of 2 or 3;R.sup.1 and R.sup.2 independently represent alkyl of 1 to 10 carbons or substituted alkyl of 1 to 10 carbons;R.sup.3 represents a ring chosen from a set consisting of aryl, substituted aryl, and a heterocyclic ring of a type present in photographic emulsions;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 independently represent hydrogen, alkyl of 1-10 carbons, substituted alkyl of 1-10 carbons, R.sup.4 and R.sup.5 taken together or R.sup.6 and R.sup.7 taken together can represent atoms necessary to form a 5 or 6-membered aliphatic ring, an aromatic six-membered ring, an aromatic 10-membered ring, a substituted aromatic six-member ring or a substituted aromatic 10-member ring;R.sup.8, R.sup.

Abstract: An optically active salt of 1,5-benzothiazepine compound of the formula (I) or (II): ##STR1## wherein each of Ring A and Ring B is a substituted or unsubstituted benzene ring, and R.sup.1 and R.sup.2 are the same or different and each is a lower alkyl group, can be prepared by resolving a racemic salt of 1,5-benzothiazepine compound of the formula (I) or (II) by means of preferential crystallization.

Abstract: A pharmaceutical compound having the formula: ##STR1## in which n is 1 or 2, m is 1 or 2, p is 1 to 6, q is 0 or 1 to 3,R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 alkyl,R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.3 and R.sup.4 together form an alkylene link of formula --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, or R.sup.4 and R.sup.5 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group,R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, carboxy, hydroxy, cyano, halo, trifluoromethyl, nitro or amino,the dotted line represents an optional double bond, andthe fluorine atom is attached at the 6 or 7-position;and salts and esters thereof.

Abstract: The invention provides novel ascomycins bearing one or more physiologically hydrolyzable and acceptable oxycarbonyl moieties or carboxy moieties, such compounds being found useful as pharmaceuticals, especially in the treatment of asthma an dermatitis. Methods of producing the compounds and pharmaceutical compositions comprising the compounds are also provided.

Abstract: Compounds of formula I are piperazinothiopyridines which are useful for controlling Helicobacter bacteria. They are useful as active compounds for treating diseases based on such bacteria, and are thus useful for making appropriate medicament compositions for administering to humans afflicted with diseases based on or caused by such bacteria.

Abstract: The novel heteroaryloxypyridines of formula I: ##STR1## (A, B, R.sub.1 and R.sub.2 are defined in the specification) show excellent selective herbicidal activity.The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.

Abstract: It is contemplated to provide an industrially adapted method for producing a dimerization product of acrylonitrile, which method is capable of producing a straight chain dimer of acrylonitrile efficiently at a high yield in a simple manner using a highly active catalyst exhibiting superior stability, without suffering from occurrence of difficulty removable by-products. In the method according to the present invention, acrylonitrile is subjected to dimerization in the presence of a ruthenium complex composed of a central atom of ruthenium and ligands including cyclopentadiene or its derivative coordinating thereto. The dimerization product, such as adiponitrile, 1,4-dicyanobutene or 1,4-dicyanobutadiene, is useful as an intermediate for producing hexamethylenediamine and adipic acid, both serving for the starting material of nylon 66, or as an intermediate for producing, for example, an antirusting agent and a vulcanization accelerator for rubbers.

Abstract: The compounds of formula: ##STR1## in which: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and A are as defined in the description, their optical isomers and N-oxides and addition salts thereof with a pharmaceutically acceptable acid or base, and their use as anti-tumour agents.

Abstract: The present invention generally relates to a textile softening composition which comprises, as the softening agent, a quaternary ammonium salt which comprises a mixture of mono-, di- and tri-ester components, wherein the amount of diester quaternary is greater than about 55% by weight, and the amount of triester quaternary is less than about 25% by weight based on the total amount of quaternary ammonium salt. The invention also relates to a process for preparing said softening agent.

Abstract: The dimesylate salt of cis-1-(3-ethoxyphenyl)-1-(4-phenylpiperazin-1-yl)4-methyl-cyclohexane has superior properties and is useful to treat physiological disorders associated with an excess of neuropeptide Y.

Abstract: Reaction products of an iridium (III) salt or a hydrate thereof, a diphosphine having secondary phosphine groups and a metal or ammonium chloride, bromide or iodide are excellent hydrogenation catalysts for ketimine. Using chiral diphosphines and prochiral ketimines, diastereoisomeric secondary amines are obtained in high optical yields.

Abstract: A compound having the formula R--S(O).sub.n CH.sub.2 CH.sub.2 CH.dbd.CF.sub.

Abstract: An imidazole derivative represented by general formula (I) or a salt thereof, having the effect of specifically inhibiting the growth of HIV as a pathogenic virus and being reduced in toxicity. In said formula R.sup.1 represents hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.7 alkenyl, C.sub.4 -C.sub.12 cycloalkylalkyl, etc.; R.sup.2 represents C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 acyl, hydroxyiminomethyl, hydrazonomethyl or --(CH.sub.2)n--R.sup.4 (R.sup.4 being halogeno, alkoxy, hydroxy, etc.; and n being an integer of 1 to 3); R.sup.3 represents substituted or unsubstituted C.sub.1 -C.sub.6 alkyl; X and Y represent each independently hydrogen, C.sub.1 -C.sub.3 alkyl, halogeno, or nitro; and Z represents S, SO, SO.sub.2 or CH.sub.2.

Abstract: A method of controlling gastric emptying in patients having an early non-insulin-dependent diabetic condition and exhibiting rapid gastric emptying comprising the administration of an effective gastric emptying controlling amount of a compound of Formula (I) ##STR1## or a physiologically acceptable salt or solvate thereof.