Abstract: The invention provides novel amino acids and peptides containing them which comprise a dihydropyridine.revreaction.pyridinium salt-type redox system and which provide site-specific and sustained delivery of pharmacologically active peptides to the brain. These new amino acids contain a redox system appended directly or via an alkylene bridge to the carbon atom adjacent to the carboxyl carbon and may be incorporated into a peptide chain at a variety of positions, including non-terminal positions.

Abstract: Novel 2-alkyl carbinol derivatives of deoxynojirimycin (DNJ) and the chemical synthesis of these derivatives and intermediates therefor from DNJ and their method of inhibiting lentiviruses are disclosed.

Abstract: The invention relates to compounds of formula ##STR1## wherein Ar is mono- or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole;Het is ##STR2## R is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is as defined above;R.sub.2 is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar)R.sub.1 R.sub.2 group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.

Abstract: Novel 2-alkyl carbinol derivatives of deoxynojirimycin (DNJ) and the chemical synthesis of these derivatives and intermediates therefor from DNJ and their method of inhibiting lentiviruses are disclosed.

Abstract: 3-Heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1H)quinolone derivatives of formula I ##STR1## wherein the radicals R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently of the others hydrogen, an aliphatic hydrocarbon radical, free or etherified hydroxy, mercapto or etherified and/or oxidised mercapto, unsubstituted or aliphaticaliy substituted amino, nitro, free or esterified or amidated carboxy, cyano, free or amidated sulfamoyl, halogen or trifluoromethyl, X is oxy or optionally oxidised thio, A is a divalent aliphatic radical and R.sub.

Abstract: The invention relates to a new process for the preparation of chloromethylpyridines of the general formula (I) ##STR1## in which X.sup.1 represents hydrogen, halogen or alkyl,characterized in that pyridine derivatives of the general formula (II) ##STR2## in which R.sup.1 and X.sup.1 have the meaning given in the description,are reacted by means of a formamide derivative of the general formula (III) ##STR3## in which R.sup.2 and R.sup.3 are identical or different and represent alkyl or cycloalkyl or together represent alkanediyl,and with a chlorinating agent, if appropriate in the presence of a diluent, at temperatures between 20.degree. and 120.degree. C. The invention furthermore relates to new pyridine derivatives of the formula (II) and their preparation.

Abstract: A compound of the formula ##STR1## wherein: Z is aryl, substituted aryl, phenyl-lower-alkyl, hetero-aryl, substituted heteroaryl, heterocycloalkyl, heterocyclocalkyl-lower-alkyl, hetero-aryl-lower-alkyl wherein one or more hydrogens of aryl and heteroaryl is optionally replaced by A and B;Y is lower cycloalkyl, aryl, phenyl-lower-alkyl, hetero-aryl, heterocycloalkyl, heterocyclocalkyl-lower-alkyl, hetero-aryl-lower-alkyl wherein one or more hydrogens of aryl and heteroaryl is optionally replaced by A and B;X is CONH.sub.2, CONHOH, tetrazole, SO.sub.2 N(R).sub.2, PO(OH).sub.2, CON(R).sub.2, or CONR--CHR--CO--A or CONR--(CHR).sub.n --A;A and B is independently H, OH, OR, halo, CF.sub.3, lower alkyl, N(R).sub.2, CON(R).sub.2, SR, NHSO.sub.2 R, hydroxy-lower-alkyl, NHCOR, NRSO.sub.2 CF.sub.3, OSO.sub.2 CF.sub.3, or CN;R is H, lower-alkyl, phenyl-lower-alkyl, hydroxy-lower-alkyl, CO-lower-alkyl, or CO--(CH.sub.2).sub.n --aryl; andn is 1, 2, or 3, and a pharmaceutically acceptable salt thereof.

Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a substituted or unsubstituted 4-hydroxy-3-nitro-1,2-dihydroquinolin-2-one or pharmaceutically acceptable salts thereof which have high binding to the glycine receptor.

Abstract: The invention relates to compounds of the formula I, to a process for their preparation and to their use as pharmaceuticals. ##STR1## In particular, the compounds are used as inhibitors of prolyl-4-hydroxylase and as inhibitors of collagen biosynthesis, as pharmaceuticals against fibrotic diseases of the liver, the lung and the skin.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and --N(R.sup.7)--CH(R.sup.8)(R.sup.9) are as claimed herein or their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment of viral infections. They can be manufactured according to generally known procedures.

Abstract: A novel, simple, high-yield process for the production of 2,3,5,6-tetrachloropyridine comprises reacting an ester of 2,2,4-trichloro-4-cyanobutyric acid with excess phosphorus oxychloride in the presence of a catalytic amount of hydrogen chloride and optionally in the presence of an aprotic inert solvent, at a temperature of 100.degree.-160.degree. C., preferably at 120.degree.-140.degree. C. for about 5-10 hours, under elevated pressure, if necessary.

Abstract: Compounds of the formula ##STR1## where the symbols are defined as in the specification.

Abstract: A process is provided for producing diastereoisomer A or a pharmaceutically acceptable acid addition salt of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl) ester 5-methyl ester which comprises subjecting a mixture of diastereoisomers A and B of 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-(1-benzylpyrrolidin-3-yl) ester 5-methyl ester to column chromatography using silica gel as a carrier and a mixture of ethyl acetate and acetic acid as an eluant, and then separating the acetate of diastereoisomer A from the eluate, or treating the acetate with a base, or further treating the resulting diastereoisomer A with a pharmaceutically acceptable acid.

Abstract: The invention relates 2,4- and 2,5-bistetrazolylpyridines. Said compounds inhibit the enzymes proline hydroxylase and lysine hydroxylase and bring about a selective inhibition of collagen biosynthesis. They are used as fibrosuppressants and immunosuppressants.

Abstract: A class of 2-(1H)-quinolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof ##STR1## wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercaptomethyl)cyclopropaneacetic acid with a compound of formula (II) ##STR2## wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I).

Abstract: Compounds of the formula XI, wherein R, R.sub.4, R.sub.8 and R.sub.38 are as defined in claim 1, are useful as intermediates in the preparation of compounds of formula I. Mixtures of a herbicidally effective amount of a pyridylsulfonylurea of formula I, ##STR1## wherein R, R.sub.1, R.sub.2 and A are as defined in the specification and of a herbicide-antagonistically effective amount of a sulfamoylphenylurea of formula II, ##STR2## wherein R.sub.7 to R.sub.11 and A.sub.2 are as defined in the specification are very suitable for controlling weeds in crops of useful plants, especially maize and sugar cane.

Abstract: The present invention describes novel cyclic diol derivatives represented by formula I and II: ##STR1## in which Y represents O, S, SO, SO.sub.2, (CH.sub.2).sub.m wherein m is zero or an integer of 1 to 5, or NR.sup.a group wherein R.sup.a is hydrogen, lower alkyl, lower alkoxycarbonyl, aryl, arylalkyl or acyl;R.sup.1 represents an alkyl or alkylcarbamoyl group;R.sup.2 represents a group having formula T--(CH.sub.2).sub.n --V (X.sup.-)q, wherein T refers to a simple covalent bond, a CO, PO.sub.3.sup.-, C(O)O, or CONR.sup.b group wherein R.sup.b is hydrogen, lower alkyl or acyl;n refers to an integer of from 1 to 10;V represents either (i) the group indicated by formula --.sup.+ NR.sup.5 R.sup.6 R.sup.7 wherein R.sup.5, R.sup.6 and R.sup.7 stands for identical or different lower alkyl group, or two or three of R.sup.5, R.sup.6 and R.sup.7 taken together with the adjacent nitrogen form heterocyclic ammonio group, or (ii) the group indicated by the formula ##STR2## wherein R.sup.

Abstract: A class of chemical compounds comprising a 2(1H)-quinolone moiety and a substituted heterocyclic moiety, linked via the 3-position of the 2(1H)-quinolone moiety by a methylene group, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs.

Abstract: The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a tricyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.