Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein W is CH.sub.3 --O-A.dbd.C--CO(V)CH.sub.3 ; n is 0 or 1;A is N or CH;V is O or NH;whereinY is O, S, NR.sub.1, or R.sub.6, the ring bond containing R.sub.4 and R.sub.5 is a single or double bond and R.sub.4 and R.sub.5 are independently selected from hydrogen and substituted or unsubstituted alkyl and aryl groups.

Abstract: The present invention is a pharmaceutical composition having a combination of an uricosuric agent such as probenecid or the like and an excitatory amino acid antagonist useful for treating a disease advantageously affected by treatment with an excitatory amino acid antagonist.

Abstract: The invention relates to 1,3-oxathiolane nucleoside analogues and their use in the treatment of viral infections. More specifically, this invention relates to (-)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidi n-2-one and pharmaceutically acceptable derivatives and pharmaceutical formulations thereof.

Abstract: The use of NMDA receptor antagonists or their physiologically compatible salts for preventing the development of tolerance during the long-term treatment with benzodiazepine-receptor-binding active ingredients as well as the combination of new pharmaceutical agents with benzodiazepine-receptor-binding active ingredients is described.

Abstract: This invention is related to compositions and methods for the treatment of central nervous system disorders comprising compounds of the general formula ##STR1## wherein X, Y, and the R groups are defined in the disclosure.

Abstract: The specification discloses methods for modulating cellular metabolism in a subject, modulating being desirable to mitigate a condition of the subject. Disclosed methods include processes for administering to said subject an effective amount of a compound of the formula ##STR1## wherein one and only one of R.sup.1 and R.sup.3 is a straight-chain or branched-chain .omega.-hydroxyalkyl (5-8C), or is a branched-chain (.omega.-1)-hydroxyalkyl (5-8C), or is an (.omega.-1)-oxoalkyl (5-8C), or is an (.omega., .omega.-1) or (.omega.-1, .omega.-2)-dihydroxyalkyl (5-8C), or is an alkenyl substituent (5-8C), and the other is alkyl (1-12C) optionally containing one or two non-adjacent oxygen atoms in place of C.

Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.

Abstract: 3-Phenylpyrrolidine compounds of the formula ##STR1## effectively inhibit phosphodiesterase (PDE) IV activities and can be used as medicaments for conditions such as asthma.

Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: The present invention is directed to a method for poteniating the therapeutic effects of selected NMDA antagonists.

Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## The new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) have a particularly pronounced activity against animal pests, in particular against insects and arachnids, and against weeds.

Abstract: The invention features an inhibitor of DP-IV, having the structure: ##STR1## wherein m is an integer between 0 and 10, inclusive; A and A' are L-amino acid residues such that the A in each repeating bracketed unit can be a different amino acid residue; the C bonded to B is in the L-configuration; the bonds between A and N, A' and C, and between A' and N are peptide bonds; and each X.sup.1 and X.sup.2 is, independently, a hydroxyl group or a group capable of being hydrolyzed to a hydroxyl group at physiological pH.

Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.

Abstract: The invention relates to cyclic imino derivatives of general formulaB--X.sub.5 --X.sub.4 --X.sub.3 --X.sub.2 --X.sub.1 --A--Y--E(I)whereinA, B, E, X.sub.2 to X.sub.5 and Y are defined as in claim 1, the stereoisomers, tautomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions which contain these compounds and processes for preparing them.

Abstract: Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.

Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.

Abstract: The invention relates to new phosphorylated aza compounds, to processes for their preparation and to their use as pesticides, in particular as soil-acting insecticides and nematicide.The new compounds have the general formula (I) ##STR1## in which R.sup.1 -R.sup.5, X and Y are defined as in the specification, with the exception of compound O-ethyl S-propyl 3-(6-chloro-3-pyridinylmethyl)-2-nitroimino-imidazolidine-1-thiophosphate.

Abstract: Heterocycle substituted imidazoles of Formula (I), which are useful as angiotensin-II antagonists, are disclosed: ##STR1##

Abstract: The use of the non-NMDA receptor antagonists quisqualate or kainate antagonists or their physiologically compatible salts for treatment of withdrawal symptoms after drug abuse as well as the combination of the new pharmaceutical agents with NMDA antagonists are described.

Abstract: Angiotensin II inhibition is exhibited by ##STR1## wherein: X is --CH.sub.2 -- or O;R is hydrogen, alkyl, aryl, cycloalkyl, aralkyl, or cycloalkylalkyl;R.sup.1 and R.sup.2 are each independently O or absent;R.sup.3 is hydrogen, alkyl, alkenyl, alkoxy, cycloalkyl, aryl, aralkyl, cycloalkylalkyl, halo, haloalkyl, or haloalkoxy;R.sup.4 is hydrogen, alkyl, alkenyl, alkoxy, aryl, cycloalkyl, aralkyl, cycloalkylalkyl, --R.sup.8 --OH, or --R.sup.8 CO.sub.2 R.sup.9 ;and the remaining symbols are as defined in the specification.

Abstract: Arthropodicidal tetrahydropyridazines of Formulae I and II, ##STR1## wherein Q,X,X.sup.1 Y, and G are as defined in the text, compositions containing them and their use in the control of arthropods.

Abstract: The present invention relates to novel heterocycle-substituted diphosphonic acids, and the pharmaceutically-acceptable salts and esters thereof, in which the diphosphonate-substituted carbon atom moiety is attached to a carbon atom in a nitrogen-containing six membered ring heterocycle, preferably a piperidine ring. The heterocycle-substituted diphosphonic acid compounds have the general structure: ##STR1## wherein Z is a nitrogen-containing six membered ring heterocycle moiety selected from piperidinyl, diazinyl and triazinyl; m, n and m+n are from 0 to 10; Q is a covalent bond or a moiety selected from oxygen, sulfur or nitrogen; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are substituent groups.The present invention further relates to pharmaceutical compositions containing these novel compounds. Finally this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical composition of the present invention.

Abstract: Sulphonylbenzyl-substituted imidazoles can be prepared by first reacting imidazolylaldehydes with sulphonylbenzyl compounds and then oxidising or reducing the aldehyde function in the customary manner.The sulphonylbenzyl-substituted imidazoles can be used as active compounds in medicaments.

Abstract: Compounds of the formula (I): ##STR1## in which the nitrogen-containing hetero ring portion is 1,4-dihydropyridine ring or a pyridine ring, R.sup.1 is only present when the nitrogen-containing hetero ring is a 1,4-dihydropyridine ring, and Z is a group of the formula (II): ##STR2## in which R.sup.4 and R.sup.5 may be the same or different and together may form one divalent group, are effective agents for enhancing the antitumor effect of antitumor drugs.

Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.

Abstract: Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT.sub.2) subtype useful in the treatment of cerebrovascular, cognitive, and CNS disorders; tachykinin receptor antagonists useful in the treatment of inflammatory diseases and pain or migraine; and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: The invention relates to 2,2-dimethylchroman-3-ol derivatives of the formula: ##STR1## in which: A, between N and CO, represents the group --CH.dbd.CH--E.dbd.CH-- or the group ##STR2## Z represents a halogen or a cyano, acetyl, trifluoroacetyl, nitro, alkylthio, carboxyl, phosphono, dial-koxyphosphoryl or alkoxycarbonyl group, the alkylthio and alkoxy groups containing from 1 to 3 carbon atoms;E represents a nitrogen atom or a group C(R.sub.4);R.sub.1 represents hydrogen, a methyl group or a hydroxyl group and R.sub.2 and R.sub.3 each independently represent hydrogen or a methyl group, it being possible for only one of the substituents R.sub.1, R.sub.2 and R.sub.3 to be methyl; andR.sub.4 represents a hydrogen atom, a halogen atom, a methyl group or a hydroxyl group;and to the pharmaceutically acceptable salts of the phosphono or carboxyl group.These derivatives have an antiarrhythmic, antiasthma and antihypertensive activity.

Abstract: The present invention relates to compositions and methods which are effective against alveolar bone resorption and enhance the ability of a tooth moved in orthodontic therapy to remain in its new position or to stay in its original position when adjacent teeth are moved.

Abstract: A compound of the formula (I): ##STR1## wherein W is a group of the formula:A--O--(CH.sub.2 .sub.n --wherein A is a cyclic group which may be substituted, n is an of 2 to 10, or W is a group of the formula:R.sup.1 --X--(CH.sub.2).sub.n' --wherein R.sup.1 is an alkyl group which may be substituted, X is an oxygen atom or a sulfur atom which may be oxidized, n' is an integer of 4 to 10; R.sup.2 is a hydrogen atom or a lower alkanoyl group; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and are a hydrogen atom or a lower alkyl group, or a salt thereof, is useful as a bone resorption inhibitor.

Abstract: A disubstituted piperazine compound having the formula ##STR1## wherein R.sup.1 is halogen, methoxy, C.sub.1-6 -alkyl or trifluoromethyl, and R.sup.2 is methyl or substituted C.sub.1-8 -alkyl, C.sub.3-8 -alkenyl or C.sub.3-8 -cycloalkyl, where substituents may be hydroxy-, keto- or oximino-groups in any position leading to a stable tertiary amine; or R.sup.2 is a straight or branched C.sub.1-8 -alkyl or C.sub.3-8 -alkenyl, which in any position may be substituted as above, but is terminally substituted with one of the following groups: cyano, optionally C.sub.1-4 -alkoxy-substituted C.sub.1-4 -alkoxy, dimethoxy, optiontionally substituted phenoxy, phosphonic acid, thienyl, furyl, oxazoline, isoxazole, oxadiazole, where the optional substitution is represented by C.sub.1-6 -alkyl or phenyl, provided that when cyano is the only substituent in R.sup.2, R.sup.2 must contain at least four carbon atoms, and pharmaceutically acceptable acid addition salts thereof.

Abstract: The present invention relates to the N-phosphonomethyl-biaryl substituted amino acid derivatives of formula I ##STR1## wherein X represents a direct bond, C.sub.1-4 -alkylene or C.sub.2 -C.sub.4 -alkenylene; R and R' represent independently hydrogen, carbocyclic aryl, 6-tetrahydronaphthyl, 5-indanyl, .alpha.-(trichloromethyl, carboxyl, esterified carboxyl or amidated carboxyl)substituted-(lower alkyl or aryl-lower alkyl), acyloxymethyl optionally monosubstituted on methyl carbon by C.sub.1-20 -alkyl, by C.sub.5 -C.sub.7 -cycloalkyl, by aryl or by aryl-lower alkyl; R.sub.1 represents monocyclic carbocyclic or monocyclic heterocyclic aryl; COR.sub.3 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; R.sub.2 and R.sub.

Abstract: Phosphine oxide-terminated allene-ene-yne compounds are disclosed that possess DNA-cleaving, antimicobial and tumor growth-inhibiting properties. Methods of making and using those compounds are also disclosed.

Abstract: Novel heterocycle substituted imidazoles of Formula (I), which are useful as angiotensin-II antagonists, are disclosed: ##STR1##

Abstract: The present invention relates to a method of preparing the antiviral compounds 2'-deoxy-5-fluoro-3'thiacytidine (FTC) and various prodrug analogues of FTC from inexpensive precursors with the option of introducing functionality as needed; methods of using these compounds, particularly in the prevention and treatment of AIDS; and the compounds themselves. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds and related compounds.

Abstract: Cyclophosphamides possessing anti-tumor activity and having the formula ##STR1## and salts thereof; wherein R is lower alkyl, aryl, aryl-lower alkyl or a nitrogen, sulfur or oxygen containing heterocyclic or heterocyclic lower alkyl, andR' is hydrogen, hydroxy or OOH with the proviso that when R' is hydrogen, R is other than methyl or phenyl and when R' is hydroxy, R is other than methyl.

Abstract: ULV plant protecting arthropodicidal formulation comprising alkyl aryl polyglycol ether as further additives in addition to the active ingredient(s) dissolved in the mixture of alphatic hydrocarbons and sunflower oil. The formulation according to the invention has an initial contact angle on the plant surface of >13.degree., after 20 minutes of >6.degree. and it is often 120 minutes still at least 2.degree..

Abstract: 1,5-Diaryl-3-substituted pyrazoles, a method of their preparation, compositions containing the same and methods of their use are disclosed. The pyrazoles are useful in alleviating inflammatory and cardiovascular disorders in mammals.

Abstract: The invention relates to the N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I ##STR1## wherein A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; R.sub.2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C.sub.5 -C.sub.

Abstract: The invention relates to new phosphonopyrrolidine- and piperidine-containing pseudopeptides, to a process for their preparation and to their use as medicaments, in particular as antiviral agents in human and veterinary medicine.

Abstract: The invention relates to topically adminstrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein each of R.sub.1 and R.sub.2 is halogen, or wherein R.sub.1 is hydrogen and R.sub.2 is Ar--S-- or Het.sub.1 --NH--, in which Ar is unsubstituted or substituted phenyl and Het.sub.1 is unsubstituted or substituted, monocyclic, 5- or 6-membered monoaza-, diaza- or thiaza-aryl that is bonded via a ring carbon atom, or wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is --A--R.sub.3, in which A is alkylene and, on the one hand, R.sub.3 is Het.sub.2, which is Het.sub.1 bonded via a ring carbon or ring nitrogen atom, or, on the other hand, R.sub.3 is hydrogen, or amino that is unsubsituted or mono- or di-substituted by identical or different substituents selected from alkyl, cycloalkyl, Ar-alkyl, Ar-O-alkyl, Ar-S-alkyl and Het.sub.

Abstract: Compounds of the formula (I): ##STR1## in which the nitrogen-containing hetero ring portion is a 1,4-dihydropyridine ring or a pyridine ring, R.sup.1 is only present when the nitrogen-containing hetero ring is a 1,4-dihydropyridine ring, and Z is either a CO.sub.2 R.sup.8 group or a group of the formula (II): ##STR2## in which R.sup.4 and R.sup.5 may be the same or different and together may form one divalent group, are effective agents for enhancing the antitumor effect or antitumor drugs.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 is hydrogen, halogen, methyl, methoxy or trifluoromethyl; n is 1 or 2; R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 alkyl which is substituted by halogen, cyano or methoxy, or is C.sub.2 -C.sub.5 alkenyl, C.sub.2 -C.sub.5 alkynyl, benzyl, COR.sub.5, CON(R.sub.5)R.sub.6, CSN(R.sub.5)R.sub.6, CO(OR.sub.6), CO(SR.sub.6), CS(SR.sub.5), SO.sub.2 R.sub.7, PO(OR.sub.6).sub.2 or Si(R.sub.6).sub.3 ; R.sub.3 and R.sub.4 independently of one another are hydrogen, C.sub.1 -C.sub.5 alkyl, CH.sub.2 OR.sub.6, cyclopropyl, methylcyclopropyl, C.sub.2 -C.sub.5 alkenyl, C.sub.2 -C.sub.5 alkynyl or C.sub.1 -C.sub.2 haloalkyl; R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 alkyl which is substituted by 1 to 3 halogens, C.sub.1 -C.sub.3 alkyl which is substituted or OR.sub.6 or SR.sub.6, or is C.sub.2 -C.sub.5 alkenyl, C.sub.2 -C.sub.5 alkenyl which is substituted by 1 to 3 halogens, C.sub.2 -C.sub.5 alkynyl, C.sub.3 -C.sub.

Abstract: The present invention is directed to a new class of 4-(oxoalkyl)phosphono, 4(oxime alkyl)phosphono, or 4-(hydrazine alkyl)phosphono, 2-piperazine carboxylic derivatives that are useful as NMDA antagonists

Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.

Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is an aromatic radical, n is 0, 1, 2 or 3, X is an oxy group, a thio group which can be oxidized or an imino group which is unsubstituted or has aliphatic substituents, alk.sub.1 and alk.sub.2 are identical or different divalent aliphatic radicals, and R.sub.2 is hydrogen or a monovalent aliphatic radical and salts thereof have properties which regulate calcium metabolism and can be employed for the treatment of diseases connected with disturbances in this metabolism. They are prepared, for example, by reacting a compound of the formula ##STR2## in which X.sub.3 is carboxyl with a phosphorylating agent and hydrolysing the primary product.

Abstract: The present invention provides compounds of the formula: ##STR1## The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them useful in treatment and prophylaxis of disorders of calcium metabolism.

Abstract: The invention is novel compounds of the formula: ##STR1## which are antagonists of platelet activating factor.

Abstract: Novel carboxamide compounds represented by the general formula (I) possess excellent activities for lowering lipids and thus they are useful as agents for treating and preventing various diseases (hyperlipidemia) such as hypercholesterolemia, hypertriglyceridemia, hyperphospholipidemia, hyperlipacidemia, and the like.

Abstract: The present invention provides diphosphonic acid derivatives of the general formula: ##STR1## according to claim 1. These compounds are useful for the treatment or prophylaxis of calcium metabolism disturbance or disease.