Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin.

Abstract: A novel 2-(substituted phenyl)-2-alkoxyiino-N-alkylacetamide compounds having a wide fungicidal spectrum and especially an excellent activity of controlling Pseudocercosporella herpotrichoides; and a composition containing the compound for controlling Pseudocercosporella herpotrichoides.

Abstract: Compounds of the formula ##STR1## in which the symbols are as defined herein, inhibit the activity of endothelin.

Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.

Abstract: A compound, composition, and method for controlling Take-all disease of plants by applying to the seed prior to planting, a fungicide of the formula: ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring which is pyridine; R and n are defined herein; A is selected from the group consisting of --C(O)--SR.sub.3, --NH--C(X)R.sub.4, --C(.dbd.NR.sub.3)--XR.sub.7, and --C(X)-amine wherein the amine is substituted with with an alkylaminocarbonyl and a hydrogen or wherein the amine has a first and a second amine substituent defined herein; B is --W.sub.m --Q(R.sub.2).sub.3 or selected from 0-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ; Q is C, Si, Ge, or Sn; W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W may also be selected from --N(R.sub.3).sub.m H(.sub.1-m)--, --S(O)p--, and --O--; X is O or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R.sub.

Abstract: Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or ?(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.

Abstract: Described are 3-hydroxypyridin-4-ones of formula I ##STR1## wherein R.sub.1 -R.sub.4, A and B are as defined in the description. The compounds have valuable pharmaceutical properties and are especially effective as chelators of iron. They can be used to treat excess iron in the bodies of warm-blooded animals.

Abstract: The present invention relates to the carbocyclic diarylmethylene derivatives of formula (I): ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.

Abstract: The present invention relates to novel 1-hydroxy-6-substituted pyridine-2-one and 1-hydroxy-6-substituted pyridine-2-thione compounds. Also disclosed is a process for producing the compound(s) and an antimicrobial composition comprising the compound(s) and at least one component selected from the group consisting of soaps, adhesives, coatings, elastomers, sealants, shampoos, skin care medicaments, cosmetics, paints and other polymer compositions.

Abstract: The product 3-amino-2-(4-methoxyphenoxy)pyridine and its pharmaceutically suitable salts, in particular the hydrochloride, are novel products which are prepared by catalytic hydrogenation of 2-(4-methoxyphenoxy)-3-nitropyridine, optionally in the presence of the acid corresponding to the salt. Its pharmaceutical compositions containing sufficient amounts of suitable auxiliaries for its topical administration prove particularly useful in therapy for the treatment of inflammatory skin diseases. The tests for dermatological action with the aid of TPA-induced mouse ear oedema and of carragenan-induced rat paw oedema show that the product is very much more active by the topical route than ibuprofen and nimesulide, two known anti-inflammatory active compounds, of which the first is very widely known and the second structurally related.

Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.

Abstract: Substituted pyridines, their preparation, and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## and to salts thereof in which 1, 2, 3 or 4 of the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are an aliphatic, alicyclic or araliphatic radical bonded by a --O--CH.sub.2 -- or --O--CO--, and the remaining ones of these radicals are H, halogen or an aliphatic or aromatic radical, X is O, S or optionally substituted imino, Y is a bond or a bivalent radical and Z is an aromatic radical or optionally substituted cycloalkyl or cycloalkenyl. The invention furthermore relates to processes for their preparation and to their use as pesticides, in particular as insecticides, acaricides and fungicides.

Abstract: This invention relates to a compound of formula 1 ##STR1## or an N-oxide, or a pharmaceutically acceptable salt, where A is CH.sub.2 and Z is S(O).sub.q where q is 0, 1 or 2, CH.sub.2, CHOH, CO, NR.sub.x, or O, orA is C.dbd.O and Z is NR.sub.x ;m is 0-5;R.sub.x is hydrogen or lower alkyl;R is C.sub.1 to C.sub.20 -aliphatic, unsubstituted or substituted five-membered heteroaryl-C.sub.1 to C.sub.10 -aliphatic-O--, unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic where substituted p from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo, or R is C.sub.1 to C.sub.20 -aliphatic-O--, or R is unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic-O-- where substituted phenyl has one or more radicals selected from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo;R.sub.1 is R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)CHO, --(C.sub.1 to C.sub.5 aliphatic)CH.sub.2 OR.sub.5;R.sub.2 and R.sub.

Abstract: Glucosidase I inhibitors as therapeutic agents for combatting nondefective retroviral pathogens, including the aetiological agents of AIDS and feline leukemia. Administration of a processing glucosidase I inhibitor, preferably castanospermine, interrupts the replication of the retrovirus in infected cells, alleviates pathogenic effects associated with the presentation of vital env glycoproteins on infected cells, and may furthermore prevent infection of target cells by interrupting expression of endogenous receptors recognized by the virion.

Abstract: Disclosed is a series of improved metal chelating agents, which are highly effective upon both injection and oral administration; several of the most effective are of low toxicity. These chelating agents incorporate within their structure 1-hydroxy-2-pyridinone (1,2-HOPO) and 3-hydroxy-2-pyridinone (3,2-HOPO) moieties with a substituted carbamoyl group ortho to the hydroxy or oxo groups of the hydroxypyridinone ring. The electron-withdrawing carbamoyl group increases the acidity of the hydroxypyridinones. In the metal complexes of said chelating agents, the amide protons form very strong hydrogen bonds with its adjacent HOPO oxygen donor, making these complexes very stable at physiological conditions. The terminal N-substituents provides a certain degree of lipophilicity to said 3,2-HOPO, increasing oral activity.

Abstract: Novel antifungal and antitumor agents having the formula ##STR1## as well as pharmaceutically acceptable salts, esters, amides and pro-drugs thereof, wherein R is selected from the group consisting of ##STR2## Also disclosed are pharmaceutical compositions comprising such compounds, and methods of treatment and processes of manufacture relating thereto.

Abstract: A pharmaceutical or cosmetic composition is disclosed comprising in combination a retinoid and a sterol capable of inhibiting the biosynthesis of cholesterol resulting in a synergistic effect in the treatment of disorders of epidermic keratinization, proliferation and/or sebaceous function.

Abstract: There are provided substituted acid amide, arylhydrazone compounds (amidrazones) of formula I ##STR1## the use thereof for the control of insect and acarid pests and methods and compositions for the protection of crops from the damage and loss caused by said pests.

Abstract: This invention provides amide compounds as inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT), pharmaceutical compositions containing such compounds, processes for the preparation of such compounds, and the use of such compounds as antihypercholesterolemic and/or antiatherosclerotic agents.

Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification,and a medicinal product containing said compound for treating a disorder of the melatoninergic system.

Abstract: This invention provides a composition, method and kit for potentiating the antitumor effect of tegafur and reducing the side effects of tegafur, comprising a compound of the formula ##STR1## wherein X is a halogen atom or a cyano group and oxonic acid or a pharmaceutically acceptable salt thereof, and also provides a composition, method and kit for treating a tumor, comprising tegafur, a compound of the formula (I) and oxonic acid or a pharmaceutically acceptable salt thereof.

Abstract: A combination medication containing flupirtin and morphine for the treatment of pain and the prevention of morphine dependence

Abstract: Combating fungi with substituted amine acid derivatives of the formula ##STR1## in which R.sup.1 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, halogenoalkinyl, cycloalkyl or cycloalkenyl,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and represent hydrogen, cycloalkyl or alkyl, orR.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a cycloalkyl ring, andR.sup.6 represents hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, unsubstituted or substituted phenylalkyl, unsubstituted or substituted phenyl or unsubstituted or substituted cycloalkyl, or represents unsubstituted or substituted heterocyclyl or heterocyclylalkyl,orR.sup.5 and R.sup.6, together with the nitrogen atom to which they are bonded, represent a heterocyclyl radical, which can contain further hetero atoms.

Abstract: This invention relates to 1-aryl-3-pyridinyl-2-propene-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.

Abstract: 3-Hydroxypyridin-4-ones of formula (I) ##STR1## in which R.sub.1 is a methyl, ethyl, 2-(.alpha.-methylpropionyloxy)ethyl or 2-pivoloyloxyethyl group and R.sub.2, R.sub.3 and R.sub.4 are each separately selected from hydrogen and methyl, ethyl, 2-(.alpha.-methylpropionyloxy)ethyl and 2-pivaloyloxyethyl groups with the provisos that (a) one only of R.sub.1 to R.sub.4 is either a 2-(.alpha.-methylpropionyloxy)ethyl group or a 2-pivaloyloxyethyl group, (b) at least one of R.sub.2 and R.sub.3 is other than hydrogen and (c) the total number of carbon atoms in R.sub.1 to R.sub.4 is no more than eleven, and physiologically acceptable salts thereof are of use in therapy, particularly in the treatment of conditions in which there is a toxic concentration of a metal, for example iron, in the body.

Abstract: This invention relates to derivatives of acrylic acid useful in agriculture (especially as fungicides but also as plant growth regulators, insecticides and nematocides), to processes for preparing them, to agricultural (especially fungicidal) compositions containing them, and to methods of using them to combat fungi, especially fungal infections in plants, to regulate plant growth and to kill or control insect or nematode pests.The invention provides a compound having the formula (I): ##STR1## and stereoisomers thereof, wherein W is a substituted pyridinyl or substituted pyrimidinyl group linked to A by any of its ring carbon atoms; A is either an oxygen atom or S(O).sub.n wherein n is 0, 1 or 2; X, Y and Z, which are the same or different, are hydrogen or halogen atoms, or hydroxy, optionally substituted alkyl (including haloalkyl), optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy.

Abstract: A synergistic antimicrobial composition comprising 2-mercaptopyridine N-oxide, and salts thereof, and iodopropargyl butylcarbamate in a ratio to each other which exhibits synergism is disclosed.

Abstract: A compound having the formula ##STR1## which is an anti-fungal agent is described. The producing organism Colletotricum accutatum is also described, along with a method of production.

Abstract: The invention relates to compounds of the formula ##STR1## wherein Z, X, Q, Y, W, and W' are as described herein. These compounds have antiviral activity, and certain of these compounds have antiinflammatory activity and are PAF inhibitors.

Abstract: A composition comprising (a) a metal salt or complex with an organic compound of the general formula ##STR1## and (b) an oxy-phosphorus compound where W may be --SH or an optionally substituted hydrocarbyl group, Q is --OH, hydrogen or optionally substituted hydrocarbyl and Z is hydrogen or optionally substituted hydrocarbyl and Q and Z or Z and W may complete a ring. The compounds are typically metal complexes of thiohydroxamic acids or dithiocarbamates. The metal is typically zinc. The compositions exhibit improved aqueous solubility compared with the metal complexes alone, and can be used as industrial biocides, especially fungicides and particularly in paint films and latices.

Abstract: The invention provides compounds represented by the following formula (I) ##STR1## or a pharmaceutically acceptable salts thereof wherein A represents ##STR2## B represents a carboxy or tetrazolyl group; and X represents --O--, --NH-- or --S(O).sub.t --.The compounds possess angiotensin II antagonism, and may be used as an antihypertensive agent, a therapeutic agent to congestive heart failure, an antianxiety agent and a cognitive enhancing agent.

Abstract: Compounds of the formula ##STR1## wherein R is hydrogen; C.sub.1-8 alkyl; C.sub.2-8 alkenyl; C.sub.3-8 alkadienyl; C.sub.2-8 alkynyl; C.sub.4-8 alkadiynyl; C.sub.2-10 (alkoxyalkyl); C.sub.2.sub.2-10 (alkylthioalkyl); C.sub.3-8 cycloalkyl and C.sub.4-12 (cycloalkylalkyl); optionally substituted by 1 to 6 halos,R.sup.1 is hydrogen or C.sub.1-8 alkyl,R.sup.2 is hydrogen, C.sub.1-8 alkyl or halo,R.sup.3 is ##STR2## wherein each R.sup.5 and R.sup.6, are independently hydrogen, halo, C.sub.1-8 alkyl, optionally substituted by 1 to 6 halos, C.sub.1-8 alkoxy, C.sub.1-8 alkylthio or nitro,W is --O--, --S--, --NR.sup.4 -- or --CO--,W.sup.1 is --O--, --S--, --SO--, --SO.sub.2 --, --NR.sup.4 -- or --CO--,X is --O--, --S--, --NR.sup.4 -- or ##STR3## wherein R.sup.1 is hydrogen or C.sub.1-8 alkyl,Z is hydrogen, C.sub.1-8 alkyl optionally substituted by 1 to 6 halos,m is 0 or 1,m' is 0 or 1, andn is 0, 1 or 2,wherein each R.sup.4 is independently hydrogen or C.sub.1-8 alkyl, said compounds are useful as pesticides, i.e.

Abstract: Compounds of the structure ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl radicals of 1-6 carbon atoms, the phenyl radical, and the benzyl radical; and wherein R' is selected from the group consisting of the phthalimido radical and the succinimido radical and of the structure ##STR2## wherein X is CH.sub.2 or C.dbd.O; R" is H, --CH.sub.2 CH.sub.3, --C.sub.6 H.sub.5, --CH.sub.2 C.sub.6 H.sub.5, --CH.sub.2 CH.dbd.CH.sub.2, or ##STR3## and hydrolysis products of said compounds wherein R" is H and the piperidino ring or both the piperidino and the imido ring are hydrolyzed are useful for the control of abnormal concentrations of TNF .alpha. manifested in septic shock, cachexia and HIV infection without substantially effecting the concentration of other cytokines.

Abstract: .alpha.-Arylacrylates substituted by a heterocyclic radical and of the general formula I ##STR1## where R.sup.1 is alkoxy or alkylthio, R.sup.2 is alkyl, Het is quinolyl, which is unsubstituted or substituted, A is oxygen and n is 1, and their plant-tolerated acid addition salts and metal complexes, and the N-oxides of the heterocyclic compounds, and fungicides containing these compounds.

Abstract: Highly concentrated emulsifiable concentrates of neophanes and azaneophanes for use in plant protectionHighly concentrated emulsifiable concentrates of compounds of the general formula I ##STR1## in which A, B=independently of one another CH, CR.sub.4 or N,X=CH.sub.2, O or S,Y=CH or N,Z=H or F,R.sub.1 and R.sub.4 =independently of one another H, halogen, (C.sub.1 -C.sub.3)-alkyl, (C.sub.1 -C.sub.3)-halogenoalkyl, (C.sub.1 -C.sub.3)-alkoxy, (C.sub.1 -C.sub.3)-halogenoalkoxy, (C.sub.1 -C.sub.4)-alkylthio or (C.sub.1 -C.sub.4)-halogenoalkylthio, or R.sub.1 and R.sub.4 together=--CH.sub.2 --O--CH.sub.2 --;R.sub.2 =H, (C.sub.1 -C.sub.3)-alkyl, ethynyl, vinyl, halogen or cyano,R.sub.3 =H, halogen, (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.3)-alkoxy andM=C or Si, which contain a combination of an anionic and a nonionic emulsifier with a (C.sub.2 -C.sub.16)-alkanol.also have, in addition to a very good spontaneous emulsiliability, a very high emulsion stability.

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein A, B and E are individually selected from the group consisting of .dbd.CH-- and .dbd.N-- with at least one being .dbd.N--, R is selected from the group consisting of cycloalkyl of 3 to 6 carbon atoms, and alkenyl and alkynyl of 2 to 6 carbon atoms, R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.2 and R.sub.3 together are --O--CH.sub.2 --O-- or are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, --CN, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, --COR.sub.4, --(CH.sub.2).sub.m --CX.sub.3, --O--(CH.sub.2).sub.m --CX.sub.3, --S--(CH.sub.2).sub.m --CX.sub.3, --O--(CX.sub.2).sub.m --CX.sub.3 and --S--(CX.sub.2).sub.m --CX.sub.3, R.sub.

Abstract: 4-Aralkylpyridines, for example 4-[3-[4-[(1-methylethyl)oxy]phenyl]propyl]pyridine, are active against nematodes.

Abstract: Antimycotics containing a compound of the formula ##STR1## where .dbd.Y is .dbd.CH--OCH.sub.3, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3, .dbd.CH--SCH.sub.3 or .dbd.N--OCH.sub.3, and X is oxygen, or X may also be NH if Y is .dbd.N--OCH.sub.3,Z is halogen, nitro, cyano, unsubstituted or substituted organic radicals, OR.sup.12, SR.sup.13, SOR.sup.14, SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22 R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--N.dbd.CR.sup.27 R.sup.28 andU, V, W can be hydrogen or one of the meanings given for Z, or where two of Z, U, V and W in adjacent positions on the phenyl ring can form an unsubstituted or substituted five- or six-membered, aromatic or aliphatic ring which may contain one to three hetero atoms (N, S, O), and R.sup.12 to R.sup.26 are identical or different and are hydrogen, unsubstituted or substituted organic radicals,are used for controlling mycoses.

Abstract: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.

Abstract: 3-Hydroxypyridin-4-ones of formula (I) ##STR1## in which R.sub.1 is a C.sub.3 or C.sub.4 hydroxyalkyl group in which the hydroxy group is terminally substituted on the alkyl group, R.sub.2 is methyl or ethyl and R.sub.3 and R.sub.4 are each separately hydrogen, methyl or ethyl but with the proviso that the total number of carbon atoms in R.sub.1 to R.sub.4 is no more than six, the compound optionally being in the form of a physiologically acceptable salt and/or pro-drug thereof, are of value for the treatment of conditions caused by iron dependent parasites, particularly malaria.

Abstract: Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined in the specification, A and B may be the same or different from each other and each represents .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and may be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded, or pharmacologically acceptance salts of them.

Abstract: A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occurring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein a R.sub.24 is the side chain of any of the naturally occurring amino acids, --CH.sub.2 SH, --CH.sub.2 Cl, --CH.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.

Abstract: Compounds of formula I ##STR1## in which the substituted R has the given meaning, have an antimalarial and a antiviral activity.

Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein V is an oxygen or a sulphur atom; X and Y, which may be the same or different, are hydrogen or halogen atoms, or optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkynyl, haloalkyl, alkoxy, haloalkoxy, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, nitrile, --CO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, or --COR.sup.6 groups; or the groups X and Y, when they are in adjacent positions on the phenyl ring, may join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; and Z is optionally substituted methylene, optionally substituted amino, oxygen or sulphur and when Z is a substituted methylene group, the substituent may join the 2-position of the phenyl ring to form a non-aromatic fused ring; R.sup.1 and R.

Abstract: 4-Hydroxypyridine derivative represented by the following formula ##STR1## wherein R represents a methyl group or an isopropyl group, and the method for preparing the derivative comprising the step of cultivating a strain belonging to Streptomyces karnatakensis are disclosed. Also disclosed are the pharmaceutical composition comprising the same and a method for treating circulatory diseases comprising the step of administering said compound to a patient.

Abstract: Compounds of formula ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl, R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl and R.sub.4 is C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl or --CH.sub.2 CH.sub.2 COOR.sub.7, or R.sub.3 and R.sub.4 together are --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --, R.sub.5 is hydrogen, C.sub.1 -C.sub.4 alkyl, ##STR2## --CH.sub.2 OCH.sub.3, --CN, --COOR.sub.7 or ##STR3## R.sub.6 is hydrogen, chlorine, methyl or nitro, R.sub.7 and R.sub.8 are each methyl or ethyl, A is an unsubstituted or mono- to tetra-substituted, aromatic or non-aromatic, monocyclic or bicyclic, heterocyclic radical, one or two substituents being selected from the group consisting of C.sub.1 -C.sub.3 haloalkyl, cyclopropyl, halocyclopropy, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, C.sub.2 -C.sub.3 haloalkenyl, C.sub.2 -C.sub.3 haloalkynyl, C.sub.1 -C.sub.3 haloalkoxy, C.sub.

Abstract: The present invention relates to compositions and method for inhibiting nonenzymatic cross-linking (protein aging) which contain diaminopyridines and derivates thereof. Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.

Abstract: This invention relates to a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH--or --CH.dbd.N--; wherein R.sub.1 is alkyl, alkenyl or alkynyl of about 1 to 20 carbon atoms; wherein R is --CO.sub.2 R.sup.2, tetrazole, methylsulfonamide or benzenesulfonamide, wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or a pharmaceutically acceptable cation and R.sup.3 is hydroxyl or halogen, having utility as LTB.sub.4 synthesis inhibitors.

Abstract: Compounds which are a 1-hydroxypyrid-2-one in which one or more of the hydrogen atoms attached to ring carbon atoms are replaced by a substituent selected from aliphatic acyl, aliphatic amide, aliphatic amine, carboxy, cyano, aliphatic ester, halogen, hydroxy and sulpho groups, alkoxy groups and alkoxy groups substituted by an alkoxy, aliphatic amide, aliphatic amine, aliphatic ester, halogen or hydroxy group, aliphatic hydrocarbon groups and aliphatic hydrocarbon groups substituted by an alkoxy, aliphatic ester, halogen or hydroxy group, but excluding compounds in which said replacement of hydrogen atoms in the compound is effected only by substituents selected from aliphatic hydrocarbon groups, halogen groups and aliphatic hydrocarbon groups substituted by a halogen group, or a salt thereof containing a physiolgically acceptable ion or ions, are of value in the treatment of patients having a toxic concentration of a metal, particularly iron, in the body whilst the iron complexes of such compounds are of val