Abstract: The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO.sub.2 R', NO.sub.2, NH.sub.2, NHR', N(R).sub.2, NHC(O)R', CN, halogen, .dbd.O, C(.dbd.O)H, C(.dbd.O)R', CO.sub.2 H, CO.sub.2 R', C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic;wherein each of the R' groups is independently selected from the group consisting of H, OH, NH.sub.2, NO.sub.2, SH, CN, halogen, .dbd.O, C(.dbd.O)H, C(.dbd.O)CH.sub.3, CO.sub.2 H, CO.sub.2 CH.sub.3, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl, aryl, aralkyl, and heteroaromatic;wherein each dotted circle represents one, two or three optional double bonds;wherein R.sub.

Abstract: A compound which is a bis(acridinecarboxamide) or bis(phenazinecarboxamide) derivative of formula (I): ##STR1## wherein each X, which may be the same or different in a given molecule, is --CH.dbd. or --N.dbd. each of R.sub.1 to R.sub.4 which may be the same or different, H, C.sub.1 -C.sub.4 alkyl, OH, SH, NH.sub.2, C.sub.1 -C.sub.4 alkoxy, aryloxy, NHR, N(R).sub.2, SR, SO.sub.2 R wherein R is C.sub.1 -C.sub.4 alkyl, CF.sub.3, NO.sub.2 or halogen, or R.sub.1 and R.sub.2 together form a methylenedioxy group; each of R.sub.5 and R.sub.6, which may be the same or different, is H or C.sub.1 -C.sub.4 alkyl; Z is (CH.sub.2).sub.n, (CH.sub.2).sub.n O(CH.sub.2).sub.n, (CH.sub.2).sub.n N(R.sub.7)(CH.sub.2).sub.n, (CH.sub.2).sub.n N(R.sub.7)(CH.sub.2).sub.m N(R.sub.7)(CH.sub.2).sub.n or (CH.sub.2).sub.n N(CH.sub.2 CH.sub.2).sub.2 N(CH.sub.2).sub.n wherein R.sub.7 is H or C.sub.1 -C.sub.

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract: A novel compound which is a .delta.-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.

Abstract: Disclosed are biologically active, non-indole-containing compounds referred to as fused isoindolones, which are represented by the following general formula: ##STR1## The fused indolones can be obtained by complete chemical synthesis. Methods for making and using the fused isoindolones are disclosed.

Abstract: The present invention is directed to a synthetic process for the formation of ecteinascidin compounds and related structures, such as the saframycins. In one particularly preferred embodiment, the present invention provides a synthetic route for the formation of ecteinascidin 743 (1), ##STR1## an exceedingly potent and rare marine-derived antitumor agent which is slated for clinical trials. The process of this invention is enantio- and stereocontrolled, convergent and short. Also disclosed are novel process intermediates, useful not only in the total synthesis of ecteinascidin 743, but also other known ecteinascidin compounds, including derivatives and analogs thereof.

Abstract: Stable, electroactive material which when a potential is applied from the outside is subjected to one or more reversible redox reactions, for use in devices with an electrochromic display or another electrochromic color change or in batteries.The material comprises a condensed ring structure, the oxidized form of which is of the formula ##STR1## in which R.sub.1, R.sub.2, X, and A may have any meaning with the proviso that the condensed ring structure maintains the reversible properties.The material can be prepared by various processes and it is suited for use as electrochromic material for use in devices with an electrochromic display or as coating on windows because it presents a distinct and easily visible color change when it is subjected to a potential. In addition, the material is suited for use in rechargeable batteries because is possesses an excellent capacity and reversibility.

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract: The invention relates to an addition compound which is obtainable by reaction of a diamine of the formula I, ##STR1## where R.sup.1 is (C.sub.2 -C.sub.4)-alkylene or 1,2- or 1,3-cyclo-(C.sub.3 -C.sub.7)-alkylene andR.sup.2 and R.sup.3, which are identical or different, are (C.sub.1 -C.sub.3)-alkyl or hydrogen orR.sup.2 and R.sup.3 together are (C.sub.2 -C.sub.4)-alkylene, with fullerenes C.sub.60 and/or C.sub.70. The fullerene derivatives are useful as electrically conducting materials.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.

Abstract: Aminoureidofullerene and aminothioureidofullerene derivatives and the process for the preparation thereof Aminoureido and aminothioureido compounds of the fullerenes C.sub.60 and/or C.sub.70 and processes for the preparation thereof and use thereof are described.

Abstract: Compounds 31668P and 31668U, a process for their production and their use.Compound 31668P and compound 31668U with the formulae ##STR1## have an antibiotic and an antitumor action.

Abstract: Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein n is 1, 2 or 3; m is 0, 1 or 2; R.sup.1 and R.sup.2 are independently H, lower alkyl, cycloalkyl, aryl, heteroaryl or heteroaryl-alkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 4- to 8-membered ring; R.sup.3 is monocyclic heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.

Abstract: 7-(substituted)piperazinyl-1-ethyl-6-fluoro-4-oxo-3-quinolinecarboxylic acids, the pharmacologically acceptable salts thereof, compositions containing them, processes and intermediates for producing them, and methods of using them to treat bacterial infections in warm-blooded animals.

Abstract: As a result of the action of electron acceptors, for example chlorine, bromine and/or iodine, on compositions containing a linear, branched or structurally crosslinked polymer and an unsubstituted or substituted tetrathionaphthalene, tetraselenonaphthalene, tetratelluronaphthalene, tetrathiotetracene, tetraselenotetracene or tetratellurotetracene, electrical conductivity is imparted to the compositions through the formation of charge-transfer complexes. These compositions are suitable for the production of mouldings, filaments, fibres, coatings and composite materials which have an antistatic finish or are electrically conducting.

Abstract: Compounds of the formula: ##STR1## where R.sup.2 contains certain aryls or heteroaryls are effective leukotriene inhibitors.

Abstract: Paraherquamide and dihydroparaherquamide, known compounds, are disclosed as having antiparasitic activity. The compounds are fungal metabolites isolated from the known fungus Penicillium paraherquei, and from a newly isolated strain of Penicillium charlesii. Compositions including paraherquamide and dihydroparaherquamide as the active ingredient thereof for antiparasitic uses against endo and ecto parasites are also disclosed, as well as processes for the preparation of paraherquamide from the newly isolated fungus.

Abstract: Disclosed are DC-52 derivatives represented by the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents hydrogen or hydroxyl, X represents hydroxyl and Y represents cyano and Z represents carboxyl or hydroxymethyl, or pharmacologically acceptable salts thereof. The DC-52 derivatives are useful as antitumor agents.

Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.

Abstract: Disclosed are DC-52 derivatives represented by the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents hydrogen or hydroxyl, X represents hydroxyl and Y represents cyano and Z represents carboxyl or hydroxymethyl, or pharmacologically acceptable salts thereof. The DC-52 derivatives are useful as antitumor agents.

Abstract: Bisamide and bisurethane bisphenols and bishaloformates are prepared by the reaction of amines with dicarboxylic acid halides or bisphenol bishaloformates. They are useful as intermediates for the preparation of cyclic heterocarbonates, which may in turn be converted to linear copolycarbonates.

Abstract: This invention relates to novel ortho-(azinyl)-benzenesulfonamides, such as N[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-2-(2-pyridinyl)benzenes ulfonamide, and their use as pre-emergent or post-emergent herbicides or plant growth regulants.

Abstract: This invention relates to novel ortho-(azinyl)benzenesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-2-(2-pyridinyl)benzene sulfonamide, and their use as pre-emergent or post-emergent herbicides or plant growth regulants.

Abstract: Quaternary sulfoalkyl or sulfoalkenyl salts of tertiary amine bases are prepared by reacting the tertiary amine bases at elevated temperatures with a hydroxy alkane sulfonic acid or a hydroxyalkene sulphonic acid.

Abstract: Novel substituted 2,3-alkylene bis (oxy) benzamides and derivatives thereof are disclosed. Also disclosed is a method for producing said compounds. The compounds have anxiolytic, psychostimulant, disinhibiting and thymoanaleptic properties useful therapeutically in the psychofunctional field, particularly in gastro-enterology, cardiology, urology, rheumatology and gynaecology.

Abstract: Polycyclic chlorinated amines resulting from cycloadditions useful as insecticides.

Abstract: New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.