Abstract: A compound of the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each a hydrogen atom, a lower alkyl group, an ar(lower)alkyl group or an aryl group, or R.sub.1 and R.sub.2 may be combined together to form a lower alkylene group and/or R.sub.3 and R.sub.4 are combined together to form a lower alkylene group, or R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be combined together to form an o-phenylene group, X is a halogen atom and Y is an oxygen atom or a nitrogen atom substituted with lower alkyl or aryl, which is useful as an intermediate in the synthesis of 1.beta.-methylcarbapenem compounds valuable as antibiotics.

Abstract: Mazindol and other nonreinforcing dopamine uptake inhibitors are effective to lessen craving for abused substances.

Abstract: Disclosed are novel classes of anti-androgen including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.

Abstract: Method for inhibiting aldehyde dehydrogenase activity using daidzin as a selective inhibitor of ALDH-I activity. Because daidzin is a potent selective, yet reversible, inhibitor of ALDH-I activity, it is useful as a pharmaceutical composition in methods for the treatment of alcohol dependence (i.e., alcoholism) or alcohol abuse, for alcohol sensitization, for extinguishing an alcohol-drinking response, for suppressing an urge for alcohol, for inducing alcohol intolerance, for preventing alcoholism in an individual with or without a susceptibility or predisposition to alcoholism or alcohol abuse, and for limiting alcohol consumption in an individual whether or not genetically predisposed.

Abstract: A quaternized polymer for use as a cosmetic agent, has recurring units of the formula ##STR1## wherein R is lower alkyl or --CH.sub.2 --CH.sub.2 OH;R' is an aliphatic, alicyclic or arylaliphatic radical containing a maximum of 20 carbon atoms, or R and R' together with the nitrogen atom to which they are attached form a heterocycle capable of containing a heteroatom other than nitrogen;A is a divalent group selected from ##STR2## wherein x, y and t are whole numbers ranging from 0 to 11 such that the sum (x+y+t) is greater than or equal to 0 and lower than 18, and E and K represent hydrogen or an aliphatic radical having less than 18 carbon atoms,--(CH.sub.2).sub.n --S--(CH.sub.2).sub.n --, (3)--(CH.sub.2).sub.n --O--(CH.sub.2).sub.n --, (4)--(CH.sub.2).sub.n --S--S--(CH.sub.2).sub.n --, (5)--(CH.sub.2).sub.n --SO--(CH.sub.2).sub.n --, (6)--(CH.sub.2).sub.n --SO.sub.2 --(CH.sub.2).sub.

Abstract: Optically active oxazoline-carboxylic acid derivatives of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, an alkykl group which is substituted and has 1 to 20 carbon atoms, a cycloalkyl group, a cycloalkyl group which is substituted, a phenyl group, a phenyl group which is substituted, a vinyl group, a vinyl group which is substituted, an ethynyl group or an ethynyl group which is substituted;R.sup.2 represents a lower alkyl group having 1 to 4 carbon atoms or a benzyl group;R.sup.3 represents a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a phenyl group or a benzyl group,and a method for preparing the above compounds and derivatives thereof involving a reaction between an aldehyde and an isocyano-carboxylate in the presence of a catalyst mixture.

Abstract: The present invention provides modified oligonucleotides, wherein, amongst the first four bases on the 5'-end, they have the base sequence AT or TA and, bound to one of the two O.sup.- groups of the 5'-phosphate group of the first nucleotide at the 5'-end of said oligonucleotide, they contain a radical of the general formula: ##STR1## in which R.sub.4 is a spacer group and R.sub.1, R.sub.2 and R.sub.3 are hydrogen atoms or alkyl or alkoxy radicals containing up to 3 carbon atoms.These modified oligonucleotides can be used for blocking the replication and/or expression of genes which have a sequence complementary with the modified oligonucleotides.

Abstract: A method of preparing a substituted derivative of sphingosine comprising the steps of reducing serine methyl ester by a hydride reagent to form an aldehyde or aldehyde derivative, adding acetylide anions to the aldehyde to form an erythro-isomer or propargyl alcohol and inverting the propargyl alcohol by S.sub.N 2 inversion to form a threo-isomer. Either isomer can then be deprotected to form an alkyne with a 2-aminopropane 1,3-diol head group; this alkyne can be reduced to form sphingosine or a sphingosine derivitive which can be functionalized at the 4 and 5 positions to form a substituted derivative of sphingosine.

Abstract: The invention relates to a ruthenium complex having the formulaRu.sup.2+ L.sub.1 L.sub.2 L.sub.3 Iwherein L.sub.1, L.sub.2 and L.sub.3 are the same or different are equal to a bi- or polycyclic ligand with at least two nitrogen-containing heterocycles, whereby at least one of these ligands is substituted with at least one group conferring water-solubility, and whereby at least one of these ligands is substituted, optionally via a spacer group, with at least one reactive group, and whereby the ligands L.sub.1, L.sub.2 and L.sub.3 are attached to the ruthenium via nitrogen atoms.The invention is further related to such ruthenium complexes having coupled thereto an immunologically active material, for example, antigens, haptens or antibodies and to the use of said ruthenium complexes in fluorescence spectroscopy. Specific ligands L.sub.1, L.sub.2 and L.sub.3 which are useful in the ruthenium complexes of the invention are, e.g.

Abstract: 7-[1H-pyrrol-3-yl]-substituted 3,5-dihydroxyhept-6-enoic acids, 7-[1H-pyrrol-3-yl]-substituted 3,5-dihydroxyheptanoic acids of the formula I ##STR1## in which A, B, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the indicated meanings, and the corresponding .delta.-lactones of the formula II ##STR2## processes for the preparation of these compounds, their use as medicaments and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formulae I and II are described.

Abstract: This invention provides a series of novel heter-aliphatic carboxamides of formula I in which the group >Z--Y--X< is selected from >C.dbd.CH--N<, >N--CH.dbd.C<, >C.dbd.N--N< and >N--N.dbd.C< and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.

Abstract: An oligonucleotide probe for diagnosing predeposition or susceptibility to type I diabetes, capable of specifically hybridizing with the gene sequence3'-GCGGGCRARGRGGGGRGCAG-5'or5'-CGCCCGATACACCCCACGTC-3'wherein A is adenine, C is cytosine, G is guanine, T is thymine, and R is thymine or uracil. The probe may include at least 15 sequential nucleotides selected from the sequence5'-GCCCGATACACCCCCACGT-3'or3'-CGGGCRARGRGGGGGRGCA-5'The probe may be labeled with a detectable marker, such as an enzyme or biotin, and may be supplied in a diagnostic kit in combination with: a substratum capable of absorbing DNA or cells, a restriction enzyme, and/or a detergent.

Abstract: The invention relates to distamycin A analogs of the following formula ##STR1## wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from ##STR2## and -Het- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R.sub.1 and R.sub.2 is hydrogen and the other is an acylating moiety or R.sub.1 and R.sub.2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds.The compounds of the invention can be useful antitumor and antiviral agents.

Abstract: A novel aromatic bismaleimide of the formula (I): ##STR1## wherein X is ##STR2## where R.sub.1 R.sub.2, R.sub.3 and R.sub.4 are a hydrogen atom or a methyl group. The bismaleimide is prepared by reacting an aromatic diamine having the formula (II): ##STR3## wherein X is the same as in the formula (I), with maleic anhydride and then conducting the ring-closing reaction of the resultant aromatic bismaleamic acid.

Abstract: The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which n denotes 1, 2 or 3, R denotes acyl, and R.sup.1 denotes alkyl, cycloalkyl, aralkyl or another carboxyl protective group, which comprises radical cyclization of compounds of the formula II ##STR2## in which n, R and R.sup.1 are as defined above, and Hal denotes chlorine, bromine or iodine, to intermediates in this process, and to their use.

Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(.+-.)-5-(4-fluorophenyl)-2-(1-methylethyl)-N-4-diphenyl-1-[2-tetrah ydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-.alpha.-[2-methyl-1-oxopropyl]-.gamma.-oxo-N,.beta.-diphenylbenze nebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.

Abstract: New echiboline derivatives with opioid properties which are 6-hydroxy-9-methyl-echiboline derivatives having, in the 10-position, a hydrocarbon substituent of up to 4 carbon atoms--preferably a group R.CH.sub.2 -- (wherein R represents a hydrogen atom or a hydrocarbon group of up to 3 carbons) and especially a methyl, cyclopropyl-methyl or allyl group.These are made by dealkylating corresponding 6-alkoxy-9-methyl-10-substituted echibolines, thereby converting the 6-alkoxy group to a 6-hydroxy group, especially using boron tribromide as dealkylating reagent.Specific examples are 6-hydroxy-9,10-dimethyl-echiboline, 6-hydroxy-9-methyl-10-allyl-echiboline and 6-hydroxy-9-methyl-10-cyclopropylmethyl-echiboline.The compounds may be in free base or salt form, and be incorporated as active ingredient into pharmaceutical compositions.

Abstract: Substituted tetrahydrobenzothiazoles are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as dopamine agonists with selectivity for the presynaptic dopamine receptor and are useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.

Abstract: Amide-compounds represented by the formula (I): ##STR1## wherein R.sub.1 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino which can be substituted by lower alkyl, nitro, cyano, sulfamoyl which can be substituted by lower alkyl, R.sub.2 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino, nitro, wherein R.sub.1 and R.sub.2 can be combined to form methylenedioxy, R.sub.3 means hydrogen, lower alkyl, halogen, or amino, R.sub.4 and R.sub.5 may be the same or different and each represents lower alkyl or wherein R.sub.4 and R.sub.

Abstract: A process for the transvinylation of a vinyl derivative of a Bronsted acid with a different Bronsted acid which comprises providing a liquid phase mixture containing said vinyl derivative and said Bronsted acid in the presence of a ruthenium compound at a temperature at which transvinylation occurs and recovering as a product of transvinylation the vinyl derivative of the different Bronsted acid. The process is most favorably employed using carboxylic acids to make vinyl esters of carboxylic acids.