Abstract: The invention is a compound of the formula 1

Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with (derivatised) hydroxyalkyl substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.

Abstract: The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with (derivatised) hydroxyalkyl substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.

Abstract: Compounds according to Formula (I) or a salt thereof are selective ligands for GABAA receptors useful for treatment of disorders of the central nervous system:

Abstract: Aminophosphonates alpha substituted by phenol groups, of formula (I) have lipoprotein(a) lowering activity.

Abstract: Bisphosphonate conjugates capable of releasing antibacterial and/or cytotoxic components upon binding with bone tissue. Such conjugates are useful in the treatment and prevention of bone cancer, bone infections and other bone-related diseases. Bisphosphonate conjugates are also delivery vehicles for use in delivering pharmaceutical compositions to bone tissue. Methods of synthesizing novel bisphosphonates and pharmaceutical compositions incorporating the same, and medical uses for such compositions, are provided. Compositions of the present invention include bone-seeking radio isotope conjugates for use in imaging and therapy.

Abstract: Substituted 1H-Pyridinyl-2-ones are useful as GABAA-Alpha 2/3 ligands.

Abstract: Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: wherein n is 0 or an integer; X is O or S, CH2, CH-halogen, CH—N3, or C═CH2; Q and U are independently selected from: O, S, and CH(Ra) wherein Ra is hydrogen, OH, halogen, N3 ,NH2, SH, carboxyl, C1-6 alkyl or Ra is CH2(Rb) wherein Rb is hydrogen, OH, SH, NH2, C1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond; Z is selected from: O, a C1-6 alkoxy, a C1-6 thioalkyl, a C1-6 aminoalkyl, (CH2)m wherein m is 0 or an integer, and N(Rc)2 wherein both Rc are independently hydrogen or a C1-6 alkyl; and R2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.

Abstract: The present invention relates to certain optionally ring substituted pyridinylaminomethylidene bisophosphonic acid tetralkyl esters (I) and their use for the treatment of bone diseases, such as osteolytic bone diseases due to malignancy, Paget's disease and primary and secondary osteoporosis.

Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Abstract: Novel aminomethylphosphine ligands have particular substituents on the central carbon atom. Such ligands form coordination complexes that may be catalysts for the polymerization of monomers or other catalytic induced reactions.

Abstract: Activating groups for cyanine dyes used to label chain terminators in nucleotide sequencing, based on N-hydroxyphthalimide, are disclosed. From these activating groups, activated dyes of the present Invention are prepared which react with the derivitized nucleotide chain terminators to give a labeled chain terminator of the present Invention. The activating groups of the present Invention allow the dye-chain terminator reaction to occur at a much higher yield and with much greater selectivity for the mono-substituted product, compared with the prior art.

Abstract: Compounds of formula ##STR1## wherein R and R' are each independently of the other hydrogen, C.sub.1 -C.sub.18 alkyl, COR.sub.1, COR.sub.2 or COOR.sub.1,X and X' are each independently of the other hydrogen, halogen, OH, NH.sub.2, COOH, C.sub.1 -C.sub.18 -alkyl, isocyclic or heterocyclic aromatic radicals, OR.sub.3, OCOR.sub.3, OCOR.sub.4, OCOR.sub.3, NHR.sub.3, N(R.sub.3).sub.2, NHCOR.sub.3, NHCOR.sub.4 or NHCOOR.sub.3,Y and Y' are each independently of the other hydrogen, halogen, OH, NH.sub.2, nitro, cyano, C.sub.1 -C.sub.18 alkyl, isocyclic or heterocyclic aromatic radicals, COR.sub.5, COR.sub.6, COOR.sub.5, COOR.sub.6, CONH.sub.2, SO.sub.2 R.sub.5, SO.sub.2 R.sub.6, SO.sub.2 NH.sub.2, SO.sub.3 H, PO(OR.sub.5).sub.2 or PO(OH).sub.2, andZ and Z' are each independently of the other hydrogen, halogen, OH, NH.sub.2, COOH, cyano, C.sub.1 -C.sub.18 alkyl, isocyclic or heterocyclic aromatic radicals, OR.sub.7, OR.sub.8, OCOR.sub.7, OCOR.sub.8, OCOOR.sub.7, NHR.sub.7, N(R.sub.7).sub.2, NHR.sub.8, CONH.sub.

Abstract: The invention relates to a method for the production of magnesium pyridoxal-5'-phosphate glutamate, in which pyridoxine or an acid addition salt thereof is oxidised with manganese (IV) oxide to pyridoxal; pyridoxal is reacted with p-phenetidine under formation of the Schiff's base p-phenetidyl-pyridoxal; p-phenedityl-pyridoxal is selectively phosphorylated on the 5'-hydroxymethyl group under formation of p-phenetidyl-pyridoxal-5'-phosphate; p-phenetidyl-pyridoxal-5'-phosphate is hydrolysed under formation of an alkali metal salt of pyridoxal-5'-phosphate; the alkali metal ions are removed in order to obtain pyridoxal-5'-phosphate; pyridoxal-5'-phosphate is reacted with a reaction product of a magnesium alcoholate and L-glutarnic acid; and the formed magnesium pyridoxal-5'-phosphate glutamate is isolated. Furthermore, the invention relates to intermediate products obtained with this method.

Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid variety and for the prevention of allergically induced diseases.

Abstract: A heterocyclic aromatic halide or an aryl halide is reacted with an amine compound in the presence of a base to give a heterocyclic aromatic amine or an arylamine, respectively. In this reaction, a catalyst comprising a palladium compound and a tertiary phosphine is used for the preparation of a heterocyclic aromatic amine, and a catalyst comprising a palladium compound and a trialkylphosphine is used for the preparation of an arylamine.

Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group, Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--, --C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.

Abstract: A phosphorus ester oligomer having the structure: ##STR1## wherein A can be the same or different in each monomeric unit and each is independently selected from the group consisting of oxygen, sulfur, lower alkyl, alkyl- or aryl-substituted amino and aminoalkyl; B.sub.1 and B.sub.2 can be the same or different and each is independently selected from hydrogen, lower alkyl, a labelling group, a protecting group, a phosphoramidate or a phosphomonoester; R.sub.1 can be the same or different in each monomeric unit, and in at least one of the non-nucleotide monomeric units, R.sub.

Abstract: The present invention relates to certain optionally ring substituted pyridinylaminomethylidene bisphosphonic acid tetralkyl esters (I) and their use for the treatment of bone diseases, such as osteolytic bone diseases due to malignancy, Paget's disease and primary and secondary osteoporosis.

Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, infectious urinary tract stones, and bone cancer, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.

Abstract: Novel oligomeric compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, are disclosed as stabilisers for protecting organic material against oxidative, thermal or light-induced degradation.

Abstract: Acetic acid derivatives of the formula ##STR1## wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.

Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.

Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, andB is a purine or pyrimidine base.

Abstract: Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A compound of formula (VI) ##STR2## wherein X is halogen, Y is S-phenyl, Se-phenyl or halogen and B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, 2-acetamido-6-diphenylcarbamoylpurine, 6-N-dimethylamino-methyladenine or 6-N-pivaloyladenine.

Abstract: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R.sup.1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).

Abstract: The invention relates to novel oligomeric compounds of the formula I ##STR1## in which L is a group of the formula ##STR2## where the oxygen in the group L is in each case bonded to the phosphorus in the recurring structural units and the radical R.sub.2 or the carbon in the 4-position of the piperidinyl ring in the group L is in each case bonded to the oxygen in the recurring structural units; and the general symbols are as defined in claim 1, as stabilizers for organic materials against oxidative, thermal or light-induced degradation.

Abstract: A process for continuously producing alkylpyrophosphonate, alkylpyrophosphate and multimers thereof and for producing 4-amino-1-hydroxyalkylidene-1,1-bisphosphonic acids or salts thereof.

Abstract: A compound of the formula (I) or (II): ##STR1## where R.sup.1, R.sup.2, R.sup.5 and R.sup.6 are the same or different and represent a hydrogen atom or a halogen atom and R.sup.1 and R.sup.2 may combine to form a ring; R.sup.3, and R.sup.4 are the same or different and represent a hydrogen atom, a halogen atom, a benzoyl group, a group of the formula --L(CH.sub.2).sub.n R.sup.8 where n is 1 to 8, R.sup.8 is a hydrogen, hydroxy, amino, dialkylamino, --COR.sup.16 or --COOR.sup.14 where R.sup.16 is a hydrogen, chlorine, COCl, C.sub.1 -C.sub.8 alkyl, --NR.sub.2 or aryl and R.sup.14 is a hydrogen, C.sub.1 -C.sub.8 alkyl, aryl, COR, 2,4-dinitrophenyl, N-imido or --NR.sub.2 and L is a direct bond or C.dbd.O; W is .dbd.O; W.sup.1 is hydrogen or --OR.sup.9, where R.sup.9 is hydrogen, C.sub.1 -C.sub.8 alkyl, acyl or a group of the formula --(CH.sub.2).sub.n R.sup.10 where n is 1 to 8 and R.sup.10 is amino, dialkylamino, hydroxy, acryloyl or methacryloyl; Y is oxygen, sulfur, selenium, tellurium, C.dbd.O, or >N--R.

Abstract: The invention provides lanthanide chelates capable of intense luminescence. The celates comprise a lanthanide chelator covalently joined to a coumarin-like or quinolone-like sensitizer. Exemplary sensitzers include 2- or 4-quinolones, 2- or 4-coumarins, or derivatives thereof e.g. carbostyril 124 (7-amino-4-methyl-2-quinolone), coumarin 120 (7-amino-4-methyl-2-coumarin), coumarin 124 (7-amino-4-(trifluoromethyl)-2-coumarin), aminomethyltrimethylpsoralen, etc.The chelates form high affinity complexes with lanthanides, such as terbium or europium, through chelator groups, such as DTPA. The chelates may be coupled to a wide variety of compounds to create specific labels, probes, diagnostic and/or therapeutic reagents, etc. The chelates find particular use in resonance energy transfer between chelate-lanthanide complexes and another luminescent agent, often a fluorescent non-metal based resonance energy acceptor.

Abstract: Aminovinylphosphonic esters I ##STR1## where R.sup.1 is cyano, a radical of the formula --CO--OR.sup.6 or a group of the formula ##STR2## R.sup.2, R.sup.3 and R.sup.6 are C.sub.1 -C.sub.20 -alkyl, C.sub.5 -C.sub.8 -cycloalkyl, C.sub.7 -C.sub.18 -aralkyl, phenyl or tolyl,R.sup.4 is an unsubstituted or substituted phenyl or heterocyclic group defined belowR.sup.5 is hydrogen or C.sub.1 -C.sub.12 -alkyl,R.sup.7 is hydrogen, C.sub.1 -C.sub.6 -alkyl, formyl, C.sub.2 -C.sub.6 -alkanoyl, C.sub.1 -C.sub.12 -alkoxy, C.sub.5 - or C.sub.6 -cycloalkoxy, cyanomethyl, 2-hydroxyethyl, benzyl or a radical of the formula --CR.sup.8 .dbd.CH--CO--OR.sup.6,R.sup.8 is hydrogen, C.sub.1 -C.sub.6 -alkyl or a radical of the formula --CO--OR.sup.6, andX is oxygen or NH, are used as light, oxygen and heat stabilizers for organic material.

Abstract: The invention concerns tachykinin antagonists. The compounds are alcohols, amines and prodrugs of nonpeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included.The compounds are expected to be especially useful in asthma, multiple sclerosis, rheumatoid arthritis, the management of pain, migraine, and antiemetic agents.

Abstract: The present invention relates to the phosphono-alkylamino-substituted tetrazole derivatives of formula I ##STR1## and tautomers thereof wherein R.sub.1 is (carbocyclic or heterocyclic) aryl-C.sub.1 -C.sub.4 -alkyl; X is phenylene, phenylene substituted by lower alkoxy, lower-alkyl, halogen or trifluoromethyl or X.sub.1 is ethynylene; R.sub.2 is carbocyclic or heterocyclic aryl; pharmaceutically acceptable mono- or di-ester derivatives thereof in which one or both of the acidic hydroxy groups of the phosphono functional group are esterified in form of a pharmaceutically acceptable mono- or di-ester, and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of endothelin-converting enzyme by administration of said compounds to mammals in need of such treatment.

Abstract: The present invention relates to 1-H-3-phenyl-5-cyloalkylpyrrolidine-2,4-diones of the formula (I) ##STR1## in which A represents optionally substituted cycloalkyl andB represents hydrogen or optionally substituted alkyl,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 the groups ##STR2## These compounds possess herbicidal and pesticidal activity.

Abstract: Compounds of formula (I), in which the groups R are hydrogen or C.sub.1-4 alkyl, n is from 2 to 4, X is alkylene, poly(ethoxy) or an aryl-containing group, Y is a valence bond or a divalent functional or heterocyclic group or a trivalent alkylene group, and Z is a sulphur-containing group which contains a thiol or disulphide group are useful to provide biocompatible treatments of metal surfaces, such as silver and gold surfaces. Processes for the preparation of the compounds, intermediates useful in such processes, articles having a metal surface treated with such compounds and processes of rendering metal surfaces biocompatible which comprise treating the metal surfaces with them.

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

Abstract: The present invention provides a phosphonic diester derivative of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and they each represent a hydrogen atom, a lower alkyl group, a halogen atom, a cyano group, a hydroxyl group, or a lower alkoxy group optionally having a halogen atom, a phenyl group or a hydroxypiperidino group as a substituent; R.sup.4 represents a hydrogen atom, a lower alkoxy group, a halogen atom, or a lower alkyl group optionally having a halogen atom or a cyano group as a substituent; and R.sup.5 and R.sup.6 are the same or different and they each represent a hydrogen atom or a lower alkyl group.The derivative of the present invention has excellent hypolipidemic, vasodepressor and hypoglycemic activities and is useful as therapeutic and preventive agents for hyperlipidemic diseases, hypertension and diabetes.

Abstract: The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.

Abstract: A bisphosphonic acid derivative of the general formula (I): ##STR1## wherein A is an optionally substituted cyclic group; R.sup.1 is hydrogen atom or a lower alkanoyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen atom or a lower alkyl group; m is 0, 1 or 2; and n is an integer from 2 to 10, or a salt thereof is disclosed. A process for its production and a bone resorption inhibitor containing the compound of the general formula (I) or a salt thereof are also disclosed.

Abstract: Dialkyl-1-H-3-(2,4-dimethylphenyl)-pyrrolidine-2,4-diones of the formula (I) ##STR1## in which A represents alkyl which is optionally substituted by halogen andB represents C.sub.2 -C.sub.10 -alkyl orA and B together with the carbon atom to which they are bonded represent an unsubstituted cycle,G represents hydrogen (a) or the groups ##STR2## E represents a metal ion equivalent or an ammonium ion, L and M represent oxygen and/or sulphur. These compounds possess herbicidal and pesticidal activity.

Abstract: The present invention relates to novel aminophosphonate derivatives substituted in .alpha. position by phenol groups, of formula (I): ##STR1## in which: X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2, A, B, Z and n are defined in claim 1, as well as their preparations and the pharmaceutical compositions comprising them.

Abstract: Substituted 4-phenyl-pyridones and 4-phenyl-2-alkoxypyridines are prepared by reducing corresponding 4-phenyl-pyridone and 4-phenyl-2-alkoxypyridine derivatives. The substituted 4-phenyl-pyridones and 4-phenyl-2-alkoxypyridines can be employed as active compounds in medicaments, in particular for the treatment of hyperlipoproteinaemia.

Abstract: New substituted pyridines are prepared by reducing suitably substituted pyridine derivatives. The new substituted pyridines are suitable as active compounds in pharmaceuticals, in particular for the treatment of hyperlipoproteinaemia.

Abstract: Novel oligomeric compounds of formula I ##STR1## wherein L is a group of formula ##STR2## wherein the oxygen atom in the group L is attached to the phosphorus atom in the structural repeating unit, and R.sub.5 or the carbon atom in 4-position of the piperidinyl ring in the group L is attached to the oxygen atom in the structural repeating unit, and the remaining symbols are as defined in claim 1, are disclosed as stabilizers for protecting organic material against oxidative, thermal or light-induced degradation.

Abstract: The present invention relates to quaternary nitrogen-containing phosphonate compounds, and the pharmaceutically-acceptable salts and esters thereof and having the general structure: ##STR1## wherein R.sup.1, R.sup.2, R.sup.5 and R.sup.8 are defined in claim 1, m and n are integers from 0 to 10; m+n is from 0 to 10;Z is a saturated, unsaturated, or aromatic, monocyclic or polycyclic carbocycle or monocyclic or polycyclic heterocycle containing one or more heteroatoms selected from O, S, or N, wherein at least one heteroatom is a quaternary nitrogen atom;R is COOH; PO.sub.3 H.sub.2 ; SO.sub.3 H; or P(O)(OH)R.sub.4, wherein R.sub.4 is substituted or unsubstituted alkyl of 1-8 carbon atoms;The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients.

Abstract: The present invention relates to 2,2-dimethylchromene derivatives of the formula: ##STR1## in which Z represents a halogen atom or a cyano, nitro, acetyl, phosphono or dialkoxyphosohoryl group, the alkoxy group containing 1 to 3 carbon atoms, and the pharmaceutically acceptable salts of the phosphono group.These compounds show an antihypertensive and antiarrythmic activity.The present invention also relates to a process for the preparation of said compounds and to the pharmaceutical compositions in which the are present.

Abstract: A bisphosphonic acid derivative of the general formula (I): ##STR1## wherein A is an optionally substituted cyclic group; R.sup.1 is hydrogen atom or a lower alkanoyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen atom or a lower alkyl group; m is 0, 1 or 2; and n is an integer from 2 to 10, or a salt thereof is disclosed. A process for its production and a bone resorption inhibitor containing the compound of the general formula (I) or a salt thereof are also disclosed.

Abstract: There are provided novel 5(and/or 6)substituted 2-(2-imidazolin-2-yl) and 2-(2-imidazolidinyl)nicotinic acids, esters and salts, which are useful as herbicidal agents. There are also provided novel substituted pyrrolopyridine acetonitriles, pyrrolopyridine acetamides, imidazopyrrolopyridinediones and carbamoylnicotinic acid esters, that are useful as intermediates for the preparation of the above said herbicidal agents.

Abstract: Compounds of the formula I ##STR1## in which x is 1, 2 or 3, and, if x=1, R.sup.1 is C.sub.1 -C.sub.30 alkyl, C.sub.1 -C.sub.18 alkyl substituted by halogen, --COOR.sup.2, --CN, --NR.sup.3 R.sup.4 or by --CONR.sup.3 R.sup.4, C.sub.2 -C.sub.18 alkyl which is interrupted by --NR.sup.5 --, --O-- or --S--, C.sub.3 -C.sub.18 alkenyl, C.sub.5 -C.sub.12 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, phenyl which is unsubstituted or substituted by C.sub.1 -C.sub.12 alkyl, halogen, phenyl-C.sub.1 -C.sub.4 alkyl and/or C.sub.1 -C.sub.4 alkoxy, or R.sub.1 is naphthyl, a radical of the formula ##STR2## R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.12 cycloalkyl or phenyl-C.sub.1 -C.sub.4 alkyl, R.sup.6 is hydrogen, methyl, allyl or benzyl, R.sup.7 is hydrogen or --OR.sup.9, R.sup.8 is hydrogen or methyl, R.sup.9 is hydrogen or C.sub.1 -C.sub.30 alkyl, R.sup.10 and R.sup.11, independently of one another, are hydrogen or C.sub.1 -C.sub.