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: The invention concerns a series of novel 2-amino-monomethoxycyclohexyl amides having analgesic and neuroprotective activity. The compounds bind selectivity to the kappa opioid receptor. Pharmaceutical compositions containing the compounds, methods of using them, and processes for preparing them are also disclosed.

Abstract: Disclosed are novel 2'-alkylidenepyrimidine nucleoside derivatives represented by formula [I]: ##STR1## wherein R.sup.1 is an amino gorup or a hydroxy group, R.sup.2 is a hydrogen atom, a halogen atom or a lower alkyl group, R.sup.3 is a hydrogen atom or a lower alkyl group, and R.sup.4 is a hydrogen atom or a phosphate residue, or salts thereof.These novel compounds can be produced from uridine or cytidine derivatives by alkylidenating the 2'-position in the sugar moiety thereof with Wittig's reagent.Furthermore, the compounds have remarkable antiviral activities and therefore can provide novel antiviral agents.

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: 3,4-Dihydro-2H-benzo[b]pyrans of the formula I ##STR1## are described, in which R.sup.1 is H, OH, (C.sub.1 -C.sub.2)-alkoxy, (C.sub.1 -C.sub.2)-alkyl or NR.sup.4 R.sup.5,R.sup.4 and R.sup.5 being identical or different and representing H, (C.sub.1 -C.sub.2)-alkyl or (C.sub.1 -C.sub.3)-alkylcarbonyl,R.sup.2 and R.sup.3 are identical or different and are alkyl having 1-4 carbon atoms,Ar is an aromatic or heteroaromatic system which is unsubstituted or substituted,n is 1 or 2 andX is a (CH.sub.2).sub.r chain which can be interrupted by a heteroatom O, S or NR.sup.6, R.sup.6 being H or (C.sub.1 -C.sub.4)-alkyl andr being one of the numbers 2, 3, 4 or 5.Processes for the preparation of these compounds, their use and pharmaceutical products based on these compounds are also described.

Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 is cyano or nitro;R.sub.2 and R.sub.3 are independently hydrogen or lower alkyl; andR.sub.4 is alkyl; alkenyl; optionally substituted phenyl or phenyl lower alkyl; --(CH.sub.2).sub.m OR.sub.2 or --(CH.sub.2).sub.m N(R.sub.2).sub.2 ; wherein m is an integer of 1-5 and R.sub.2 is as defined above;or a pharmaceutically acceptable ester thereof; are smooth muscle relaxants, particularly useful in the treatment of hypertension.

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: The present invention relates to substituted cyclopentanone and cyclohexanone derivatives and substituted cyclopentenone and cyclohexenone derivatives, which are useful as intermediates for pharmaceutical products and agricultural chemicals and especially useful for the synthesis of prostaglandins, and also to a process for producing the same.

Abstract: N,N'-dimethyl aromatic diamines are prepared from the corresponding diprimary amines via a two step synthesis forming first the corresponding di-succinylimidomethylamine and then reductively cleaving the succinylimido group. The products are useful, e.g., as epoxy curing agents.

Abstract: In a first embodiment this invention relates to a process for preparing a white product which principally contains a bisimide. The process comprises: providing tetrabromophthalic anhydride and a solvent in a reaction vessel; forming, at a temperature within the range of from about 140.degree. C. to about 200.degree. C., a reaction mass by adding a diamine, a diamine salt or a mixture thereof to the solution, the formation of the reaction mass resulting in the production of a bisimide precipitate which becomes a component of the reaction mass; terminating the addition of the diamine when the molar ratio of the tetrabromophthalic anhydride initially present in the solution to the diamine or diamine salt added is substantially stoichiometric; cooking the bisimide precipitate to increase the average sphericity of the particles making up the bisimide precipitate; and recovering from the reaction mass, as the bisimide product, the cooked precipitate.

Abstract: The photooxidation of N,N'-substituted thioureas with oxygen in the presence of an acid-trapping agent gives N,N'-substituted carbodiimides. The carbodiimides can be converted into cyanoguanidines, which are suitable as latent curing agents for epoxy resins.

Abstract: In a first embodiment this invention relates to a process for preparing a white product which principally contains a bisimide. The process comprises: providing tetrabromophthalic anhydride and a solvent in a reaction vessel; forming, at a temperature within the range of from about 140.degree. C. to about 200.degree. C., a reaction mass by adding a diamine, a diamine salt or a mixture thereof to the solution, the formation of the reaction mass resulting in the production of a bisimide precipitate which becomes a component of the reaction mass; terminating the addition of the diamine when the molar ratio of the tetrabromophthalic anhydride initially present in the solution to the diamine or diamine salt added is substantially stoichiometric; cooking the bisimide precipitate to increase the average sphericity of the particles making up the bisimide precipitate; and recovering from the reaction mass, as the bisimide product, the cooked precipitate.

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: A process for preparing a compound of the formula: ##STR1## in an excellent yield with high purity, which comprises reacting a compound of the formula: ##STR2## with 3,4,5,6-tetrahydrophthalic anhydride in the presence of a catalyst system consisting of a nitrogen-containing base and a lower fatty acid.

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.