Abstract: The compounds of the formula (I) wherein R is as defined in the disclosure, are prepared by bromination of compounds of the formula (II) by means of Br.sub.2 or HBr in the presence of H.sub.2 O.sub.2.

Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R.sub.1 is --CH.sub.3, --CH.sub.2 --O--R.sub.6, --OR.sub.6 or --COR.sub.7 ; R.sub.2 is --OR.sub.8, --SR.sub.8 or a polyether radical if in the latter case R.sub.4 is C.sub.1 -C.sub.20 alkyl and is in ortho or meta position relative to X--Ar; R.sub.3 is alkyl or R.sub.2 and R.sub.3 together form a cycle optionally interrupted by O or S; R.sub.4 is aryl radical; R.sub.5 is H, halogen, C.sub.1 -C.sub.20 alkyl or --OR.sub.8 ; R.sub.6 is H, alkyl or --COR.sub.9 ; R.sub.7 is H, alkyl, --N(r')(r") or --OR.sub.10 ; R.sub.8 is H, alkyl or --COR.sub.9 ; R.sub.9 is alkyl; R.sub.10 is H, C.sub.1 -C.sub.20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r' and r" are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R.sub.11 is H or --OR.sub.6 ; R.sub.

Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.

Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: The compounds according to the invention are substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides of formula I herein which exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are Factor Xa inhibitors. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, methods for their preparation and their use, which are for treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.

Abstract: This invention provides Ddz-amino acid pentafluorophenyl esters and Ddz-amino acid 3,4-dihydro-3-hydroxy-4-oxo-1,2,3-benzotriazine (ODhbt) esters and their side-chain protected derivatives. Preferred esters and derivatives are crystalline solids. The invention also provides (.alpha.,.alpha.-Dimethyl-3,5-dimethoxybenzyl)-p-methoxycarbonylphenylcarb onate, an improved reagent for the introduction of the Ddz group. Pfp and ODhbt esters of this invention have favorable coupling to racemization ratios and are particularly suited for automated solid-phase peptide synthesis. The invention relates in addition to methods of making the esters of this invention and to methods of using these esters in peptide synthesis.

Abstract: Arthropodicidal oxazoline derivatives and processes and intermediates for the preparation thereof are disclosed. The intermediates are racemic or enantiomerically enriched compounds having formula (I), wherein R and n are disclosed in the specification.

Abstract: Novel amine derivatives of the following general formula (I): ##STR1## (wherein) A may denote --(CH.sub.2)--O--, --(CH.sub.2).sub.2 --O--, or --(CH.sub.2).sub.2 --NH--;B may denote --(CH.sub.2).sub.2 --;R.sub.1 may denote a hydrogen atom, a halogen atom, a nitro group, a 1-pyrrolyl group, an acetamido group, an amino group or a dimethylamino group;R.sub.2 may denote a hydrogen atom or a nitro group;R.sub.3 and R.sub.4 may denote a hydrogen atom;R.sub.8a and R.sub.8b which are the same may denote a chlorine atom or a methoxy group;R.sub.9 may denote a hydrogen atom or an amino group;R may denote a methyl group; andX may denote a methanesulfonamido group, a 1-imidazolyl group or a nitro group or a salts thereof are useful as antiarrhythmic drugs.

Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

Abstract: This invention relates to novel formulations of salts of certain benzopyran compounds, to compositions containing them and their use in the treatment of certain disorders.

Abstract: The present invention provides illudin analogs of the general formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.

Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure ##STR1## wherein n is 1 to 5; X is N or C--R.sup.5 wherein R.sup.5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, and where X is N, R.sup.1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above acyl guanidines.

Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.

Abstract: There are described benzoylguanidines of the formula I ##STR1## having the definitions of R(1) to R(4) indicated in the text, and their pharmaceutically tolerable salts. They are obtained by reaction of a compound II ##STR2## with guanidine. They are outstanding agents for the treatment of disorders of the cardiovascular system.

Abstract: Methods and compositions for treating CF by mobilizing mutant forms of CFTR, which retain at least some functional activity, to the plasma membrane where they can mediate chloride ion transport are disclosed.

Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.

Abstract: A method for preparing a diarylalanine compound is provided. The method includes reacting a diarylaminopropanediol with a reducing agent to form a diarylaminopropanol compound and/or contacting a serine ester derivative with an aryl metal reagent to form diarylaminopropanediol. A diarylmethyloxazolidinone compound is also provided.

Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

Abstract: We proposed a novel compound having an activity of PGI.sub.2 receptor agonist.A phenoxyacetic acid derivative of the formula ##STR1## A is --C(R.sup.1).dbd.N.about.OR.sup.2, --CH(R)NH--OR.sup.2, --COE, --SO.sub.2 E, --CH.sub.2 --NR.sup.3 --Y, --Z--NR.sup.3 --CONR.sup.4 R.sup.5, --CH.sub.2 --OR.sup.6, --CO.sub.2 R.sup.6, --CH.sub.2 --O.about.N.dbd.CR.sup.7 R.sup.8, --CH.sub.2 --O--NHCHR.sup.7 R.sup.8, substituted by imidazolyl(methyl), pyrazolylmethyl, oxazolyl(methyl), thioxazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolylmethyl;T is alkylene, alkenylene, etc.;D is --CO.sub.2 R.sup.10, --CONR.sup.11 R.sup.12 ;E is (substitution) amino, hydradino;Y is substituted (thio) carbonyl, substituted sulfonyl;Z is --CH.dbd.N--, --CH.sub.2 NR.sup.3 --;R.sup.1, R.sup.3, R.sup.10 --R.sup.13 is each H or alkyl, etc.;R.sup.2, R.sup.4 --R.sup.9 is each H, alkyl or alkyl substituted by phenyl or hetero ring ,etc. and non-toxic salts thereof, non-toxic acid addition salts thereof, possess an agonistic on PGI.sub.

Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.

Abstract: The heterocyclic aryl-, alkyl- and cycloalkylacetamides are prepared by reacting the appropriately substituted acetic acids with amines, if appropriate in complexed form. The heterocyclic aryl-, alkyl- and cycloalkylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.

Abstract: A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: in which each A.sup.n is nitrogen or CR.sup.n (n=1-5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R.sup.1 to R.sup.5, if present, independently of one another are hydrogen, C.sub.1-4 -alkyl or aryl, also one of the substituents R.sup.1 to R.sup.5 can be a group of the formula --OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R.sup.6 is hydrogen or C.sub.1-4 -alkyl; and R.sup.7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of a palladium diphosphine complex. Compounds of this class, especially those in which one of the substituents R.sup.1 to R.sup.5 is an aryloxy group, are important herbicides.

Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.

Abstract: Substituted Indanylidineacetylguanidines, process for their preparation, their use as medicaments or diagnostic and medicaments containing them:Indanylidineacetylguanidines I ##STR1## and their pharmaceutically acceptable salts wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and X have the meanings given in the claims, are effective inhibitors of the cellular sodium/proton antiport (Na.sup.+ /H.sup.+ exchanger), which, in numerous diseases (essential hypertension, atherosclerosis, diabetes and the like) is also increased in those cells which are readily accessible for measurements, such as, for example, in erythrocytes, platelets or leukocytes. They are also advantageous for the preparation of a medicament for the treatment or prophylaxis of disorders of lipid metabolism.

Abstract: The hetero-linked phenylglycinolamides are prepared by reaction of the corresponding hetero-linked phenylacetic acids with appropriate phenylglycinols. The hetero-linked phenylglycinolamides are suitable as active compounds in medicaments.

Abstract: This invention relates to derivatives of 3,3-(disubstituted)cyclohexan-1-one monomers and related compounds which are useful for treating allergic and inflammatory diseases.

Abstract: The invention relates to novel cinnamamides, a process for their manufacture and their use as UV absorbers. The cinnamamides of the invention may be used as UV absorbers in a variety of engineered resins such as polyamides (especially nylon 6 and 6,6), polycarbonates, polyacetals, polysulfones, polyimides, polyaryletherketones, and polyesters, (especially PET and PBT), as well as, other polymers such as polyvinylchloride and polyolefins (polyethylenes and polypropylenes).

Abstract: Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them.Described are benzoylguanidines of the formula I ##STR1## where R(1) to R(3) are H, Hal, (cyclo)alkyl, N.sub.3, CN or OH, alkyloxy, phenyl, phenoxy or benzoyl, and their pharmacologically acceptable salts, but with the exception of the compounds benzoylguanidine, 4-chlorobenzoylguanidine, 3,4-dichlorobenzoylguanidine and 3- or 4-methylbenzoylguanidine.They are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group.

Abstract: A compound and method of making a compound for use as a diagnostic or therapeutic pharmaceutical comprises at least one functionalized hydroxyalkyl phosphine donor group and one or more sulfur or nitrogen donor and a metal combined with the ligand.

Abstract: The present invention relates to benzamidoxime derivatives represented by the formula ?I!; ##STR1## wherein R.sup.1 is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted C.sub.2 -C.sub.4 alkenyl or unsubstituted or substituted C.sub.2 -C.sub.4 alkynyl, R.sup.2 is phenyl optionally having substituents or heterocycle optionally having substituents, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are each independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio or the like, and r.sub.1 and r.sub.2 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or the like, having excellent fungicidal activity and being useful as a fungicide for agricultural and horticultural use, and methods for preparation thereof.

Abstract: Methods and compositions for treating CF by mobilizing mutant forms of CFTR, which retain at least some functional activity, to the plasma membrane where they can mediate chloride ion transport are disclosed.

Abstract: The invention provides certain amino acid conjugates of substituted 2-phenyl-N-?1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.

Abstract: Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.

Abstract: This invention relates to certain 1,4,4-(trsubstituted)cyclohex-1-ene dimers and rlated compounds which are useful in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).

Abstract: The present invention relates to novel dimers of 4.4-(disubstituted)cyclohexan-1-ol dimers and delated compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: A process for preparing polycyclic aromatic compounds, which comprises reactinga) an aromatic boron compound withb) an aromatic halogen compound or an aromatic perfluoroalkylsulfonate in the presence ofc) a base,d) a nickel or palladium catalyst,e) a phosphorus-containing ligand andf) a polyhydric alcohol, a sulfoxide or sulfone.The process gives high yields, in particular also in the coupling of chloroaromatics.

Abstract: Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C.sub.1 and C.sub.2 are carbon atoms which are part of an aromatic ring; W is alkoxyimino, alkoxymethylene or alkylthiomethylene; R.sub.1 is independently selected from the group consisting of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, wherein the alkyl or alkoxy are optionally substituted by halogen, and p is 0, 1, or 2; Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, NR.sub.2 wherein R.sub.2 is hydrogen or a lower aliphatic group, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 S(O)--, --OCH.sub.2 --, --SCH.sub.2 --, --S(O)CH.sub.2 --, --CH.sub.2 ON.dbd.C(R.sub.3)-- or --CH.dbd.NB wherein B is --O--CO--, --N.dbd.CR.sub.3, or --CR.sub.3 R.sub.4 -- wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 -C.sub.

Abstract: Novel trienoic compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.

Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: The present invention provides novel intermediates which are useful for the preparation of excitatory amino acid receptor antagonists. Further provided is a process to enatioselectively prepare hydroisoquinoline compounds with central nervous system activity.

Abstract: A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.

Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein Ar is a mono- or bicyclic aromatic group optionally containing one or two heteroatoms independently selected from nitrogen, oxygen and sulphur, said group being optionally substituted by one or more atoms or groups independently selected from halogen, nitro, amino, --NRR.sup.1 where R and R.sup.1 are independently selected from hydrogen, C.sub.1-8 alkyl and C.sub.1-8 alkanoyl, cyano, carboxyalkoxy, alkoxycarbonylalkoxy, C.sub.1-8 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-8 alkoxy (including cycloalkoxy and cycloalkylalkoxy), C.sub.

Abstract: The present invention describes compounds, methods and compositions effective to treat mast cell mediated inflammatory conditions, such as conjunctivitis, asthma and allergic rhinitis. The compounds of the invention comprise novel mono- and di-aminomethylbenzyl, aminobenzyl, guanidylbenzyl and benzyl tryptase inhibitors. The compositions for treating mast cell mediated inflammatory conditions include oral, inhalant and topical preparations as well as devices comprising such preparations.

Abstract: The present invention relates, by way of novel industrial products, to compounds which are structurally related to 15-deoxyspergualin and which have the formula ##STR1## in which: A is a single bond, a group --CH.sub.2 --, a group --CH.sub.2 O--, a group --CH.sub.2 NH--, a group --CH(OH)--, a group --CHF-- or a group --CH(OCH.sub.3)--, andn is equal to 6 or 8,and their addition salts.These novel compounds are useful especially as immunosuppressants. The invention further relates to the method of preparing said compounds.

Abstract: The peptides described are modified with the phosphine group and are useful for marking with .sup.99m Tc and .sup.186-188 Re or paramagnetic agents for use in diagnosis and radiotherapy; in particular chelating compounds having the co-ordinating sets PN.sub.2 X, where X is --S, --O, COO--, PN.sub.3, P.sub.2 N.sub.3 and P.sub.2 N.sub.2 are described.

Abstract: Disclosed herein is a process for producing a (2S,5S)-2,5-diamino-1,6-diphenyl-3-hexanone derivative represented by the formula (1): ##STR1## wherein R.sup.1 means a lower alkylcarbonyl group, a halogen-substituted lower alkylcarbonyl group, an arylcarbonyl group or a lower alkoxycarbonyl group, and R.sup.2 and R.sup.3 are identical with or different from each other and denote individually an aryl group or an alkoxy-substituted aryl group, which comprises subjecting a (2S)-2,5-diamino-1,6-diphenyl-4-hexen-3-one derivative represented by the formula (2): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the same meaning as defined above, to a hydrogenation reaction in the presence of a transition metal-containing catalyst.

Abstract: A method for preparing a diarylalanine compound is provided. The method includes reacting a diarylaminopropanediol with a reducing agent to form a diarylaminopropanol compound and/or contacting a serine ester derivative with an aryl metal reagent to form diarylaminopropanediol. A diarylmethyloxazolidinone compound is also provided.