Abstract: The present invention relates to a process for stereoselective cycloaddition reactions which generally comprises a cycloaddition reaction between a pair of substrates, each either chiral or prochiral, that contain reactive &pgr;-systems, in the presence of a non-racemic chiral catalyst, to produce a stereoisomerically enriched product. The present invention also relates to novel asymmetric catalyst complexes comprising a metal and an asymmetric tridentate ligand.

Abstract: The present invention relates to cyclic ketones represented by the following formula and to drugs in which an effective component is such a cyclic ketone or a pharmacologically acceptable salt thereof. The cyclic ketones of the present invention encourage the production of blood platelets, leukocytes and erythrocytes, and can be employed in the prevention or treatment of cytopaenia brought about by cancer chemotherapy, radiotherapy or drug therapy, or by immunological abnormality, anaemia and the like.

Abstract: This document describes a novel and practically excellent process for the preparation of optically active compounds, such as optically active alcohols or amines which are useful for various applications, for example, as synthetic intermediates of pharmaceuticals, liquid crystal materials, and reagents for optical resolution, wherein a hydrogen transfer type asymmetric reduction is carried out in the presence of both a transition metal complex and an optically active nitrogen compound or a transition metal complex having an optically active nitrogen compounds as an asymmetric ligand, and a hydrogen-donating organic or inorganic compound.

Abstract: This invention is to provide a compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: ##STR2## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.

Abstract: A process for producing a compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen or alkyl, and R is hydrogen or alkyl, which comprises removing the protective group (P) of hydroxyl of a compound of the formula (II): ##STR2## wherein P is a protective group of hydroxyl, .about. indicates an E-isomer, Z-isomer or a mixture thereof, and the other symbols are as defined above; and an intermediate for the production of the compound of the formula (I).

Abstract: The present invention relates to a process for stereoselective cycloaddition reactions which generally comprises a cycloaddition reaction between a pair of chiral or prochiral substrates that contain reactive .pi.-systems, in the present of a non-racemic chiral catalyst, to produce a stereoisomerically enriched product.

Abstract: This invention relates to ketones represented by the following formula ##STR1## and to drugs in which such a ketone or pharmacologically acceptable salt thereof is an effective component.The ketones of the present invention encourage the production of platelets, red blood cells, white blood cells and the like, and can be used to prevent or treat cytopaenia brought about by cancer chemotherapy, radiotherapy, bone marrow transplantation and drug therapy, or by immunological abnormality or anaemia, and the like.

Abstract: This invention relates to compositions, compounds and methods for lightening skin, using active compounds having the structure: ##STR1## wherein: (i) each X is, independently, selected from the group consisting of halo, alkyl, substituted alkyl, aryl, OR, OCOR, COR, CONRR COOR, CN, SR, SOR, SO.sub.2 R, SO.sub.3 R and NRR, wherein X is other than hydroxy, amino and thio, if this X is attached ortho to the phenol hydroxy;(ii) m is an integer from 0 to 4;(iii) each R' and each R" is, independently, selected from the group consisting of hydrogen, halo, alkyl, substituted alkyl, aryl, OR, OCOR, OCRROR, COR, CR(OR)OR, CONRR, COOR, CRROR, CN, SR, and NRR; wherein halo, when it appears, is other than geminal to a hydroxy, NH.sub.

Abstract: Compounds of formula (I) ##STR1## and the salts of these compounds, are efficacious PDE (phosphodiesterase) inhibitors.

Abstract: The present invention relates to new 3-aryl-4-hydroxy-.DELTA..sup.3 -dihydrofuranone derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded form an unsubstituted or substituted 5- to 7-membered ring which is interrupted by at least one hetero atom,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number 0, 1, 2 or 3,G represents hydrogen (a) or one of the groups ##STR2## E represents a metal ion equivalent or an ammonium ion, L represents oxygen or sulphur,M represents oxygen or sulphur andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in the description, to processes for their preparation, and to their use as pesticides.

Abstract: Cyclic sulphones of formula (I) are disclosed, in which: R.sup.1 and R.sup.2 each independently of one another stand for H, A, CF.sub.3, CH.sub.2 F, CHF.sub.2, C.sub.2 F.sub.5, Hal, OH, OA, NH.sub.2, NHA, NA.sub.2, NO.sub.2 or CN; X stands for CR.sup.4 R.sup.5, C.dbd.Z, O, S, NH, NA or NR.sup.3 ; Y stands for CR.sup.6 R.sup.7, C.dbd.Z, O, NH, NA, or NR.sup.3 ; Z stands for O, S, NH, NA, NOH, NOA, CH.sub.2, CHA or CA.sub.2 ; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently of one another stand for H, A, R.sup.3, Hal, OH, OA, SH, SA, NH.sub.2, NHA or NA.sub.2, or alternatively, R.sup.5 and R.sup.6 or R.sup.7 and R.sup.8 can together represent a bond, only one such bond being present in each molecule; R.sup.4 and R.sup.5 together can also stand for O--(CH.sub.2).sub.2 --O or O--(CH.sub.2).sub.3 --O; R.sup.8 and R.sup.9 each independently of one another stand for H or A; A stands for alkyl with 1-6 C atoms; Hal stands for F, Cl, Br or I; and R.sup.

Abstract: A stain for a nucleic acid characterized by containing, as an effective component, a pyrylium salt compound having Y as a negative portion and a pyrylium ring or a pyrylium-similar ring, wherein the ring is comprised of X selected from O, S, Se and Te as a hetero atom and has substituents R.sup.1, R.sup.2 and R.sup.3, wherein each of R.sup.1 and R.sup.2 is independently a hydrogen atom, sulfonate group, amino group, substituted or unsubstituted aryl group, etc., R.sup.3 is -A or -L-A, L is -L.sup.1 -, -L.sup.2 -L.sup.3 - or -L.sup.4 -L.sup.5 -L.sup.6 -, and each of L.sup.1 to L.sup.6 is independently --(CH.dbd.CH)--, a divalent group derived from the substituted or unsubstituted aryl group, etc., A is a substituted or unsubstituted aryl group, etc., and Y.sup.- is an anion.

Abstract: This invention relates to substituted heterocyclic benzocycloalkenes of general formula I or pharmaceutically acceptable salts thereof, to a method of producing them and to their use as analgesics.

Abstract: The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.

Abstract: Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.

Abstract: A triketone compound of the following formula: ##STR1## wherein Y.sup.1 is C.sub.1 to C.sub.4 alkyl, a halogen or a C.sub.1 to C.sub.4 haloalkyl; each of Y.sup.2 and Y.sup.3 is independently C.sub.1 to C.sub.4 alkyl; Y.sup.4 is hydrogen, C.sub.1 to C.sub.4 alkyl or a halogen; n is 0, 1 or 2; p is 0 or 1; each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently hydrogen, C.sub.1 to C.sub.4 alkyl or phenyl; or when p is 1, either R.sup.1 or R.sup.2 and either R.sup.3 or R.sup.4 optionally bond to each other to form an intramolecular double bond; and X is a group of the formula ##STR2## in which each of R.sup.5 and R.sup.6 is independently a hydrogen atom, a C.sub.1 to C.sub.4 alkyl group or a phenyl group. The triketone compound is useful as a herbicide to control a broad range of upland weeks at a low dosage without causing phytotoxicity on corn.

Abstract: The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia.

Abstract: Dyes comprising an inner salt of a compound of the formula:Q.sup.1 =Z-Q.sup.2wherein:Q.sup.1 is a 4-(benz[b]-4H-pyrylium)methylidene, 4-(benz[b]-4H-thiopyrylium)methylidene or 4-(benz[b]-4H-selenopyrylium)methylidene grouping;Z is a 1,3-(2-hydroxy-4-oxo-2-cyclobutylidene) hydroxide or 1,3-(2-hydroxy-4,5-dioxo-2-cyclopentylidene) hydroxide ring; andQ.sup.2 is a 4-(benz[b]-4H-pyran-4-ylidene)methyl, 4-(benz[b]-4H-thiopyran-4-ylidene)methyl or 4-(benz[b]-4H-selenopyran-4-ylidene)methyl grouping;wherein at least one of the groupings Q.sup.1 and Q.sup.

Abstract: The invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists of formula I and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LBT.sub.4 antagonists. The compounds of the invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruitus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma and other conditions where marked neutrophil infiltration occurs.

Abstract: Novel cyclic amino acids of formula (Ia) or (Ib) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders.

Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.

Abstract: Process for the preparation of 6-(substitutedaminopropionyl)-derivatives of forskolinProcess for the manufacture of 6.beta.

Abstract: A process for producing a compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen or alkyl, and R is hydrogen or alkyl, which comprises removing the protective group (P) of hydroxyl of a compound of the formula (II): ##STR2## wherein P is a protective group of hydroxyl, .about. indicates an E-isomer, Z-isomer or a mixture thereof, and the other symbols are as defined above; and an intermediate for the production of the compound of the formula (I).

Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

Abstract: A process for preparing oxiranemethane derivatives which are useful as intermediates for preparing aspartyl protease inhibitors comprising the steps of activating an aminodiol, acylating the aminodiol and reacting the acylated aminodiol with a base to form an epoxy compound.

Abstract: The present invention relates to a novel process for preparing cis-4-O-protected-substituted-2-cyclopentenol derivatives comprising, a) dissolving a 4-O-protected-2-cyclopentenone in a suitable organic solvent; and b) treating the solution with a suitable Lewis acid and a suitable reducing agent at a temperature of from about -100.degree. C. to about 20.degree. C. The cis-4-O-protected-substituted-2-cyclopentenol derivatives are useful intermediates in the preparation of various cyclopentanyl and cyclopentenyl purine analogs which are useful as immunosuppressants and in the preparation of various prostaglandins.

Abstract: The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.

Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.

Abstract: The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.

Abstract: The present invention is concerned with diaryl compounds of formula (l) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.

Abstract: A bicyclic sulfur compound of the following formula: ##STR1## wherein X.sup.1 is selected from the group consisting of C.sub.1 -C.sub.4 alkyl, halogen, C.sub.1 -C.sub.4 haloalkyl, C.sub.2 -C.sub.4 alkoxyalkyl, C.sub.1 -C.sub.4 alkoxy and C.sub.1 -C.sub.4 haloalkoxy; each of X.sup.2 and X.sup.3 is independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 haloalkyl; X.sup.4 is selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl and C.sub.1 -C.sub.4 alkoxy; each of X.sup.5, X.sup.6, X.sup.7 and X.sup.8 is independently hydrogen or C.sub.1 -C.sub.4 alkyl; or X.sup.2 and X.sup.5 can combine to form an unsaturated double bond; or X.sup.5 and X.sup.7 can combine to form an unsaturated bond; p is an integer of 0 or 1; and n is an integer of 0, 1 or 2; or a salt thereof.

Abstract: There is described a process for preparing 3-(2-thienylthio)butyric acid by converting a compound having the formula (III): ##STR1## wherein R is a straight chain or branched C.sub.1 to C.sub.4 alkyl group, whereby the production of 3-(3-thienylthio)butyric acid as a by-product which is the position isomer can be controlled to at most 0.1 mol %. 3-(2-Thienylthio)butyric acid is a useful compound as an intermediate for a medicinal compound.

Abstract: Compounds of the formula ##STR1## where R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently are H or lower alkyl of 1 to 10 carbons; R.sub.5 is lower alkyl of 1 to 10 carbons, fluoro, chloro, bromo, iodo, nitro, or fluoroalkyl having 1 to 10 carbons; m is an integer having the value of 1-4; n is an integer having the value of 0-4; Y is phenyl or a heteroaryl group selected from a group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl and oxazolyl, said Y group being optionally substituted with one or more R.sub.5 group; A is (CH.sub.2).sub.p where p is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.

Abstract: A cyanoketone derivatives of the following formula (1) ##STR1## which are characterized by excellent herbicidal activity and effectiveness against a variety of broad leafed weeds, including barnyard grass, green foxtail, velvet leaf, livid amaranth and hairy beggar ticks.

Abstract: The present invention relates to novel N-phenylacetamino nitriles of the general formula (I), ##STR1## in which R.sup.1 represents hydrogen, or represents alkyl, alkenyl, cycloalkyl, aryl or heterocyclyl which are in each case optionally substituted, andR.sup.2 represents hydrogen, or represents alkyl which is optionally substituted, orR.sup.1 and R.sup.2, together with the carbon atom to which they are bonded, represent cycloalkyl or heterocyclyl which are in each case optionally substituted,R.sup.3 represents halogen, alkyl or alkoxy,R.sup.4 represents hydrogen, halogen, alkyl, halogenoalkyl or alkoxy,R.sup.5 represents halogen, alkyl or alkoxy, andm represents a number 0, 1, 2 or 3, processes for their preparation and their use for the preparation of agents for controlling pests.

Abstract: Novel onium borates of an element of Groups 15 to 17 of the Periodic Table, or borates of an organometallic complex of an element of Groups 4 to 10 of the Periodic Table, well suited for the photochemical/electron beam cationic initiation of polymerization/crosslinking, the anionic borate moiety of which having the formula:[BX.sub.a R.sub.b ].sup.-in which a and b are integers ranging from 0 to 4 and a+b=4; the symbols X are each a halogen atom when a ranges up to 3 and an OH functional group when a ranges up to 2; and the symbols R, which may be identical or different, are each a phenyl radical substituted by at least one element or electron-withdrawing substituent or by at least two halogen atoms, or an aryl radical containing at least two aromatic ring members, or such aryl radical bearing at least one electron-withdrawing substituent.

Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are 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 ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

Abstract: Derivatives and analogues of 2-deoxy-2,3-didehydro-N-acetyl neuraminic acid, pharmaceutical formulations thereof, methods for their preparation and their use in the treatment of viral infections, in particular influenza, are described.

Abstract: This invention relates to novel (Z,Z), (Z,E) and (E,Z) olefin isomers of substituted benzylidene cycloketones and their pharmaceutically acceptable salts. The compounds of the invention are potent factor Xa inhibitors thereby acting as anticoagulants useful in a number of thrombotic disease states. Pharmaceutical compositions are proposed for the compounds.

Abstract: Disclosed herein are cyanoketone derivatives of the following formula (1) ##STR1## such as 1-cyano-1-piperidinocarbonyl-3-[4-(2-chloro-4-trifluoromethylphenoxy)pheno xy]-2-butanone, 1-cyano-1-piperidinocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-pyridyloxy )phenoxy]-2-butanone, 1-cyano-1-(N-methyl-N-dichlorophenyl)aminocarbonyl-3-[4-(2-quinoxalyloxy)p henoxy]-2-butanone, 1-cyano-1-(N,N-dibutyl)aminocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-py ridyloxy)phenoxy-2-butanone, and the like, which are characterized by excellent herbicidal activity and effectiveness against a variety of gramineous weeds.

Abstract: Novel guanidino-substituted compounds are described having the following general formula (I): ##STR1## in which X may be carbon, oxygen, nitrogen or sulfur; R.sub.1 may be H, OH, linear or branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine, lower alkyl-thio, hydroxy substituted lower alkoxy, lower alkoxy-alkoxy substituted lower alkoxy, hydroxy substituted lower alkyl-amine, alkoxy substituted lower alkyl-amine and terminally guanidino-substituted linear of branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine or lower alkyl-thio; and R.sub.2 and R.sub.3 are independently one of linear or branched lower alkyl, alkoxy, alkyl-substituted alkoxy and alkylamine.These compounds have been found to inhibit effectively herpesvirus replication. Particularly preferred compounds in accordance with formula (I) for this purpose are guanidino-substituted sugar derivatives.

Abstract: A stain for a nucleic acid characterized by containing, as an effective component, a pyrylium salt compound having Y as a negative portion and a pyrylium ring or a pyrylium-similar ring, wherein the ring is comprised of X selected from O, S, Se and Te as a hetero atom and has substituents R.sup.1, R.sup.2 and R.sup.3, wherein each of R.sup.1 and R.sup.2 is independently a hydrogen atom, sulfonate group, amino group, substituted or unsubstituted aryl group, etc., R.sup.3 is -A or -L-A, L is -L.sup.1 -, -L.sup.2 -L.sup.3 - or -L.sup.4 -L.sup.5 -L.sup.6 -, and each of L.sup.1 to L.sup.6 is independently --(CH.dbd.CH)--, a divalent group derived from the substituted or unsubstituted aryl group, etc., A is a substituted or unsubstituted aryl group, etc., and Y.sup.- is an anion.

Abstract: A sulfone charge transport agent and a multilayered electrophotographic element in which at least one of said layers includes polymeric binder and the sulfone charge transport agent. The general structure of the charge transport agent is: ##STR1## R is alkyl or cycloalkyl having from 1 to about 10 carbons, or aryl or heteroaryl having a total of carbons and heteroatoms of from 6 to about 12. T is alkyl having from 1 to 4 carbons.

Abstract: Mixtures of optically active cyclohexenone oxime ethers having R- and S-configuration in the oxime ether moiety of the formula I ##STR1## (R.sup.1 =C.sub.1 -C.sub.6 -alkyl; ##STR2## X=C.sub.1-C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl; m=0-3 or 1-4 where all X's are halogen;n=0-3 or 1-5 where all X's are halogen;R.sup.2 =C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkenyl, substituted or unsubstituted 5-membered saturated heterocyclic structure, substituted or unsubstituted 6- or 7-membered heterocyclic structure, substituted or unsubstituted 5-membered heteroaromatic structure, substituted or unsubstituted phenyl or pyridyl)and their agriculturally useful salts and esters with C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids.

Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 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(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.

Abstract: The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier.

Abstract: Compounds of Formula 1 ##STR1## wherein X is S or O; R.sub.1 -R.sub.5, m, o, X, Y, A, B are as defined in the specification.

Abstract: This invention is directed to 1-alkoxy-2-(alkoxy- or cycloalkyloxy-)-4-(cyclothioalkyl- or cyclothioalkenyl-)benzene compounds that inhibit cyclic AMP phosphodiesterase or tumor necrosis factor (TNF) and are useful in treating patients suffering from disease state capable of being modulated by inhibiting production of cyclic AMP phosphodiesterase or TNF by administering the compound to the patient. The invention is also directed to the preparation of these compounds, pharmaceutical compositions containing these compounds and methods for their pharmaceutical use.

Abstract: In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.