Abstract: A pyrrolidylthiocarbapenem derivative represented by Formula I is provided: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2, R.sup.3 and R.sup.4 are hydrogen, lower alkyl which can be substituted or an amino protecting group independently, or R.sup.2 and R.sup.3 together with a nitrogen atom to which R.sup.2 and R.sup.3 are bonded form a saturated or unsaturated cyclic group, or R.sup.2 and R.sup.4, or R.sup.3 and R.sup.4 together with two nitrogen atoms and one sulfur atom in the sufamide group form a saturated or unsaturated cyclic group; each cyclic group can further include at least one atom selected from the group consisting of oxygen, sulfur and nitrogen, and each cyclic group can be substituted; X.sup.1 is hydrogen or a hydroxy protecting group; X.sup.2 is hydrogen, a carboxy protecting group, an ammonio group, an alkali metal or an alkaline-earth metal; and Y.sup.2 is hydrogen or an amino protecting group.

Abstract: Compounds, topical compositions and methods useful for preventing the penetration of toxic chemicals through the skin of a mammal are disclosed.The compounds of the invention provide an enhanced barrier for the skin of a mammal to further inhibit or decrease the passage of bioactive agents through the skin of a mammal either from the outside environment into the systems of said mammal or from the mammal into the outside environment.

Abstract: A meso-monoiodo-substituted tetramacrocyclic compound having the formula (I): ##STR1## wherein: each of A through D is independently a 5-membered, nitrogen-containing ring having the members necessary to complete a porphyrin, chlorin, bacteriochlorin or isobacteriochlorin nucleus;R.sub.1 through R.sub.8 are independently a hydrogen atom, a lower alkyl group, a lower alkyl carboxylic acid or acid ester group, keto, hydroxy, nitro, amino, or a group that, taken together with another ring, ring substituent or meso-substituent, forms a fused 5- or 6-membered ring; andeach of S.sup.1 through S.sup.3 is H, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, a substituted or unsubstituted aromatic ring, or a substituted or unsubstituted heterocyclic ring. A method for synthesizing the compound comprises the step of iodinating a corresponding unhalogenated, de-metallated tetramacrocyclic compound, followed by metallating.

Abstract: Benzothiophene, benzofuran and indole-thiazepinones, oxazepinones, and diazepinones are effective therapeutic agents for treating viral diseases, including those caused by herpesvirus and HIV.

Abstract: The present invention relates to a process for preparing a cephem derivative represented by the following formula (I): ##STR1## useful as an intermediate for the preparation of antibiotics.

Abstract: Novel compounds of the formula ##STR1## in which --Y--Z--, R.sup.1 R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X have the meaning indicated and their salts show endothelin receptor-antagonistic properties.

Abstract: A process for the preparation of .epsilon.-caprolactam and .epsilon.-caprolactam precursors, starting from the corresponding 5-formylvalerate ester, ammonia and hydrogen in the presence of a hydrogenation catalyst is disclosed, wherein in a step (a) 5-formylvalerate ester is reacted with ammonia under non-hydrogenating conditions, and in a step (b) the reaction product obtained in step (a) is converted to .epsilon.-caprolactam and the .epsilon.-caprolactam precursor(s) under hydrogenating conditions, in the presence of ammonia.

Abstract: A process for the manufacture of 4H-imidazo?1,5-a!?1,4!benzodiazepine derivatives of formula I ##STR1## wherein R.sup.1 is phenyl or mono- or disubstituted phenyl;R.sup.2 is hydrogen, halogen, nitro, cyano, trifluoromethyl or lower alkyl;R.sup.3 is hydrogen or lower alkyl; andR.sup.4 is hydrogen or lower alkyland of pharmaceutically usable salts of these compounds by decarboxylating a 4H-imidazo?1,5-a!?1,4!benzodiazepinecarboxylic acid of formula II ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the above significances, at elevated temperature and under elevated pressure in the presence of an organic solvent. The compounds of formula I and their pharmaceutically usable acid addition salts are known muscle relaxants, sedatives and anticonvulsants.

Abstract: The description relates to bicyclene derivatives of formula (I) in which A, B, D, E, G, K, L, R.sup.1, R.sup.2, Z.sup.1 and Z.sup.2 have the meanings given in the description, and their production. These compounds are suitable for treating diseases.

Abstract: Substituted compounds of the FK-506 Type. These compounds are useful for the same or essentially the same purposes as FK-506 and are applied in the same or a similar manner. These compounds are immunosuppressants and useful for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. Still other uses are described in the disclosure.

Abstract: A process for preparing caprolactam by cyclization of 6-aminocapronitrile in the presence of water at elevated temperature and in the presence or absence of a catalyst and a solvent, comprisesa) removing from the cyclization reaction effluent ("reaction effluent I") caprolactam and all components boiling higher than caprolactam ("high boilers"),b) treating the high boilers of stage a) with phosphoric acid and/or polyphosphoric acid at from 200 to 350.degree. C. to obtain a reaction effluent II, andc) removing caprolactam formed and any 6-aminocapronitrile from reaction effluent II of stage b) to obtain separation from unconverted high boilers and acid used.

Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.

Abstract: This invention relates to benzodiazepine derivatives which are useful as drugs exhibiting antagonism at the gastrin and/or CCK-B receptor, and to their production.

Abstract: Salinamides A and B are disclosed. These two bicyclic depsipeptides are produced by fermentation of a specific marine actinomycete, a Streptomyces sp, (CNB-091) in saltwater-based media. Salinamides A and B are useful as anti-biotic and anti-inflammatory agents.

Abstract: The present invention relates to UCF116 compounds represented by the formula (I) : ##STR1## wherein an example of Q.sup.1 representation is ##STR2## and an example of Q.sup.2 representation is ##STR3## which have antibacterial and antitumor activity and are useful as antibacterial and antitumor agents.

Abstract: The invention is a highly efficient synthesis for making compounds of formula (iv) wherein R is C.sub.1-4 alkyl or benzyl; and R.sup.1, when present, is C.sub.1-4 alkyl, OH, O--C.sub.1-4 alkyl, or S--C.sub.1-4 alkyl; which are useful intermediates for making compounds such as those represented in formula (I).

Abstract: The tricyclic benzazepine and benzothiazepine derivatives represented by the formula (I) and pharmacologically acceptable salts thereof are disclosed. ##STR1## wherein Z represents CO, --CR.sup.6 R.sup.7 -- or --S(O).sub.n, R represents hydrogen, alkyl, phenylalkyl, or a protective group of a triazole ring, R.sup.1 -R.sup.5 represent hydrogen, alkyl, alkenyl, alkoxy, amino, oxim or hydroxyl. These compounds have anti-allergic effect and are useful for the treatment and prophylaxis of allergic diseases.

Abstract: The invention relates to compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof having gastrin and/or CCK-B antagonist activity.

Abstract: This invention relates to substituted cyclic ureas and derivatives thereof, including compounds of formula (II): ##STR1## said compounds being useful as inhibitors of HIV protease. The present invention also relates to pharmaceutical compositions comprising such compounds and to method of using these compounds for the treatment HIV infection. The present invention also relates to the use of such compounds in processes for the identification of HIV protease inhibitors and for the inhibition or detection of HIV in a bodily fluid sample.

Abstract: The invention relates to substituted 3-amino-1-arylalkyl-benzazepin-2-ones of the general formula ##STR1## wherein the substituents are defined in the specification; or salts thereof; to processes for the preparation thereof; and to the use thereof as well as to pharmaceutical compositions that comprise compounds of formula (I) or pharmaceutically acceptable salts thereof.