Abstract: 6-Heterocyclic-4-amino-1,2,2a,3,4,5-hexahydrobenz?cd!indoles are provided which are useful in modifying the function of serotonin in mammals.

Abstract: Acridinium sulfonylamides and isomers, such as phenanthridinium sulfonylamides, may be employed in applications including chemiluminmescent immunoassays. Methods for synthesis of these compounds include contacting an amine with a sulfonylhalide to form a sulfonamide and acylating with an activated carboxylic acid of an acridine or isomer thereof. The N-sulfonyl-9-acridinium carboxamide and isomers may be conjugated to antigens, haptens, antibodies, and nucleic acids for use in chemiluminescent assays.

Abstract: Novel 5-HT.sub.3 receptor antagonist compounds having following formula (I) ##STR1## wherein n is 1, 2 or 3;each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N (R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7) N--SO.sub.2 group, in which each of R6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is an imidazolyl group of formula ##STR2## wherein each of R.sub.8 and R.sub.10 which may be the same or different is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.9 is hydrogen, C.sub.1 -C.sub.6 alkyl or a nitrogen protecting group; and the pharmaceutically acceptable salts thereof, are disclosed.

Abstract: Chemiluminescent acridinium derivatives of the formula I ##STR1## in which R.sup.4 represents a radical of the formula II or III ##STR2## and A.sup..theta., X--, R.sup.1 -R.sup.3, R.sup.5 and R.sup.6 have the stated meanings, as well as processes for the preparation of the compounds of the formula (I) and the use thereof in chemiluminescence immunoassays.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen orCOCH.sub.2 --S--CH.sub.2 CH.sub.2 --O--CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.n --CH.sub.2 --O--CH.sub.2 CH.sub.2 --OCH.sub.3 ; and n=8-450; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

Abstract: Compounds of formulaA(B).sub.x, (I),wherein x is an integer from 1 to 4,A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, isoindolinone, isoindoline, dioxazine, phthalocyanine or azo series, which radical contains x N-atoms attached to B, preferably with at least one directly adjacent or conjugated carbonyl group,B is a group of formula ##STR1## and, if x is 2, 3 or 4, may also be one, two or three hydrogen atoms. The symbols Q, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, Z, m und n, are as defined in claim 1. These carbamate group-containing soluble chromophores are distinguished by outstanding solid state fluorescence in the UV range as well as the by ease with which they can be converted to the corresponding pigments in the substrate in which they are incorporated.

Abstract: The present invention provides a process for preparing a (4S,5R)-2,4-diphenyl-5-carboxy-oxazoline derivative, which can serve as a taxol side-chain precursor, from the treatment of a (2R,3S)-alkyl trans-3-phenyl-2,3-epoxypropionate derivative with benzonitrile in the presence of a strong acid.

Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumor activity and a high degree of safety, and can be applied as an antitumor medicine for curing tumors of various kinds.

Abstract: The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase, particularly 5.alpha.-reductase type 1. The compounds of formula I are useful in the systemic, including oral, or parenteral or topical treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia which includes female and male pattern baldness, female hirsutism, benign prostafic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as in the treatment of prostatitis. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis are provided, as well as pharmaceutical compositions for the compounds of formula I.

Abstract: Compounds with fungicidal properties having formula I ##STR1## wherein W is CH.sub.3 --O--A.dbd.C(-)--CO(V)CH.sub.3 ;A is N or CH;V is O or NH;R.sub.4 and R.sub.5 are independently selected from hydrogen and substituted or unsubstituted alkyl and aryl groups and Q is substituted or unsubstituted aryl groups.

Abstract: Novel carbocyclic compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.

Abstract: Certain 1-(benzyl or 5-benzofuranylmethyl)-1-hydroxyurea derivatives are useful as hypoglycemic and hypocholesterolemic agents.

Abstract: A novel crystal modification of the compound 2,4-diamino-6-hydroxymethylpteridine hydrobromide and a process for its preparation and its use for preparing methotrexate. The novel crystal modification of 2,4-diamino-6-hydroxymethylpteridine hydrobromide is distinguished in particular by the fact that only one equivalent of the brominating agent triphenylphosphine dibromide is needed for brominating the 6-hydroxymethyl group. No reaction with the amino groups in the 2 and 4 positions takes place. This facilitates the reaction to give 2,4-diamino-6-pteridinyl derivatives such as methotrexate.

Abstract: Described are new delta-17 and delta-20 olefic and saturated 17.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and related compounds and the use of such compounds as 5.alpha.-reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenic related disorders.

Abstract: 1,2-di-substituted indan expressed by general formula (I) wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, Y is a halogen atom, and X and Y can be in either cis- or trans-configuration forming either a racemic body or an optically active substance; or 1,2-di-substituted indan expressed by general formula (I') wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, and X and OH group can be in either cis- or trans-configuration forming either a racemic body or an optically-active substance; or cis-1,2-epoxyindan expressed by general formula (VI) wherein R is phenyl or a lower alkyl group, oxazoline ring is in cis-configuration forming either a racemic body or an optically active substance is reacted, under an acidic condition, with a nitrile expressed by general formula (II) wherein R is phenyl or a lower alkyl group to produce cis-1-aminoindan-2-ol

Abstract: This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.

Abstract: This invention relates to certain triazolopyrimidine derivatives of the general formula ##STR1## in which R.sup.1 represents an optionally substituted alkyl, alkenyl, alkynyl, alkadienyl, cycloalkyl, bicycloalkyl or heterocyclyl group; R.sup.2 represents a hydrogen atom or an alkyl group; or R.sup.1 and R.sup.2 together with the interjacent nitrogen atom represent an optionally substituted cycloalkyl or heterocyclic ring; R.sup.3 represents an optionally substituted cycloalkyl or heterocyclyl group; and R.sup.4 represents a hydrogen or halogen atom or a group --NR.sup.5 R.sup.6 where R.sup.5 represents a hydrogen atom or an amino, alkyl, cycloalkyl or bicycloalkyl group and R.sup.6 represents a hydrogen atom or an alkyl group; processes for their preparation; compositions containing such compounds and their use as fungicides.

Abstract: A process is described for the synthesis of nalbuphine. The process results in a product having very low levels of the undesirable .beta.-epimer. The process is a five-step synthesis that begins with a compound such as an N,O.sup.3 -bis (alkoxycarbonyl) -14-hydroxynormorphinone.

Abstract: 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz-?cd!indoles are provided which are useful in modifying the function of serotonin in mammals.

Abstract: Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: ##STR1## ?wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR.sup.1 (wherein R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and A {wherein A is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or OR.sup.2 (wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group)}, is C.sub.1 -C.sub.8 alkylene wherein one carbon atom on the straight chain is substituted with one OR.sup.1 group (wherein R.sup.1 is the same as defined above), and Z.sup.1 and Z.sup.2 are independently a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a OR.sup.1 group (wherein R.sup.1 is the same as defined above)!.