Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.

Abstract: This invention relates to compounds represented by the general formula [I] 1

Abstract: The present invention relates to the preparation of synthons that are used to form modules that, in turn, are used to form two-dimensional close-packed planar arrays, referred to as nanomembranes. In a presently preferred embodiment, a nanomembrane herein constitutes a filter.

Abstract: The invention concerns the use of aromatic compounds capable of binding with G-quadruplex structures to produce medicines with anti-telomerase effect. Said compounds correspond to formula (I) wherein: R1, R2 and R3, identical or different, represent a hydrogen atom, or a —CH2—NH—(CH2)n—X group, wherein n is an integer from 2 to 4, and X is selected among —NH2—, —N(CH3)2 radicals, a heterocyclic radical such as piperidyl, imidazolyl, morpholinyl radical, or an indole-type condensed heterocyclic radical, —Z represents CH or N, each compound comprising two nitrogen atoms in the Z positions. The invention is useful for producing anticancer medicines.

Abstract: The invention provides cannabinol derivatives and pharmaceutical preparations thereof.

Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombosis.

Abstract: The present invention provides methods for synthesizing novel tetrahydroquinoline derivatives that are useful for cancer chemotherapy and anti-viral applications. The present invention provides compounds useful for cancer chemotherapy and methods for the preparation of these compounds. The present invention also includes cancer chemotherapy methods.

Abstract: The present invention relates to a method for preparing 5- and 6-halomethyl quinoxalines. The method comprises contacting a 5- or 6-methyl quinoxaline with a halogenating agent in the presence of a radical initiator in a solvent selected from the group consisting of fluorobenzene, difluorobenzenes, trifluorobenzenes, chlorobenzene, dichlorobenzenes, trichlorobenzenes, &agr;, &agr;, &agr;-trifluorotoluene and &agr;, &agr;, &agr;-trichlorotoluene. The invention also relates to preparing 6-bromomethyl quinoxaline with N-bromosuccinimide in the presence of a radical initiator in 1,2-dichloroethane. The method for halogenating benzylic methyl groups may also be employed to halogenate a wide variety of halomethyl heterocyclic compounds.

Abstract: The invention provides polyflurinated aromatic or heterocyclic compounds comprising at least three ring sustitutents, at least one of which comprises a sulphurpentafluoride group and at least one of which comprises a labile group; methods for their preparation are also disclosed. Preferably, the compounds comprise either two sulphurpentafluoride groups or one sulphurpentafluoride group and one other polyflurinated group, such as a trifluoromethyl group. Said labile group preferably comprises an amino, bromo or nitro group. Said compounds are useful in the preparation of medicaments.

Abstract: The present invention relates to a method for preparing quinoxaline-5- and 6-carboxylic acids. The method comprises contacting an aqueous alkaline suspension of a 5- or 6-halomethyl quinoxaline with oxygen in the presence of a transition metal catalyst, to form the respective quinoxaline-5- or 6-carboxylic acid. The method for oxidizing benzylic methyl groups may also be employed to prepare a wide variety of heterocyclic carboxylic acid compounds.

Abstract: The N-oxides of the compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, arm novel active bronchial therapeutics.

Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel active bronchial therapeutics.

Abstract: The N-oxides of the compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel active bronchial therapeutics.

Abstract: The invention relates to a process of preparing a discotic liquid crystalline compound by intramolecular oxidative cyclisation of a diaryl compound in an organic solvent in the presence of a strong acid, characterized in that an oxidative agent comprising a chrom(VI)oxide derivative is used, to discotic liquid crystalline compounds obtainable from said process, to liquid crystalline media, (co)polymers or polymer networks with columnar phases comprising said discotic liquid crystalline compounds, and to the use of said discotic liquid crystalline compounds, liquid crystalline media or liquid crystalline (co)polymers with columnar phases for liquid crystal displays, optical elements like polarizers, compensators or colour filters, chemical sensors, charge transport materials, optical storage media, nonlinear optics, decorative pigments, adhesive or synthetic resins with anisotropic mechanical properties.

Abstract: A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, pplycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g.

Abstract: A compound represented by the formula 1, a salt, hydrate, solvate or stereoisomer thereof.

Abstract: The present invention relates to a method for preparing 5- and 6-halomethyl quinoxalines. The method comprises contacting a 5- or 6-methyl quinoxaline with a halogenating agent in the presence of a radical initiator in a solvent selected from the group consisting of fluorobenzene, difluorobenzenes, trifluorobenzenes, chlorobenzene, dichlorobenzenes, trichlorobenzenes, &agr;, &agr;, &agr;-trifluorotoluene and &agr;, &agr;, &agr;-trichlorotoluene. The method for halogenating benzylic methyl groups may also be employed to halogenate a wide variety of halomethyl heterocyclic compounds.

Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51 and Ar have the meanings indicated in the description, are novel active bronchial therapeutics.

Abstract: Compounds of formula (I), in which R1, R2, R3, R31, R4, R5, R51, R6, R13 and R20 have the meaning indicated in the description, are novel active bronchial therapeutics

Abstract: This invention provides a novel class of substituted 6(5H)phenanthridinone compounds. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereof are also described.

Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):

Abstract: The instant invention discloses a process for the preparation of compounds of formula I 1

Abstract: Novel anticancer agents of the phenanthridine class having a specific mechanism of action and cancer therapy methods are described, including the novel chemical compounds and their therapeutic use thereof in humans.

Abstract: Process for the preparation of compounds of formula (I), wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula (V), wherein the general symbols are as defined in claim 1, with carbon monoxide in the presence of a catalyst.

Abstract: A compound of the following formula:

Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.

Abstract: Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure In addition, methods of making and using the dyes as fluorescent labels are disclosed.

Abstract: Compounds of formula I pharmaceutically acceptable salts thereof and compositions of either are useful for treating conditions amenable to treatment with a phosphodiesterase inhibitor type 4.

Abstract: A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g.

Abstract: There are disclosed compounds of formula (I) and pharmaceutical acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions.

Abstract: Compounds of the formula I in which R1, R2, R3, R31, R4, R5, R51 and R6 have the meanings indicated in the description, are novel efficacious bronchial therapeutics.

Abstract: 5-Fluorophenanthridine derivatives and their use in liquid-crystalline mixtures 6-Fluorophenanthridine derivatives of the formula (I) ##STR1## in which G is --CF.dbd.N--,E.sup.1, E.sup.2, E.sup.3, E.sup.4, E.sup.5 and E.sup.6 are identical or different and are --CH--, --CF-- or --N--and R.sup.1 (--A.sup.1 --M.sup.1).sub.a (--A.sup.2 --M.sup.2).sub.b, (M.sup.3 --A.sup.3 --).sub.c (M.sup.4 --A.sup.4 --).sub.d R.sup.2 denote mesogenic radicalsare suitable as components for liquid-crystalline mixtures, especially ferroelectric mixtures.

Abstract: The present invention relates to the use of tetrahydroisoquinoline derivatives of the general formula: ##STR1## wherein: A is arylR.sup.1 is hydrogen, hydroxy, lower alkyl, lower alkoxy, R--CO-- or R--COO--, wherein R is lower alkyl;R.sup.2 is hydrogen, lower alkyl or cycloalkylR.sup.3 -R.sup.7 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy orR.sup.3 and R.sup.4 taken together are --(CH.sub.2).sub.n -- orR.sup.6 and R.sup.7 taken together are --OCH.sub.2 O-- andn is 3 or 4,as well as pharmaceutically acceptable salts for the manufacture of medicaments for the control or treatment of diseases which represent therapeutic indications for NMDA receptor subtype specific blockers.

Abstract: Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,and R.sup.2, R.sup.3, R.sup.4, X and Z are as defined in the specification, possess affinity for metabotropic glutamate receptors and are useful in the treatment of disorders of the central nervous system.

Abstract: Intercalator compounds of formula I-T.sub.m as defined herein are provided which are comprised of intercalator moieties, or substituted intercalator moieties, having one or more functionalized chains, or moieties, and which compounds provide a high affinity for binding to the DNA molecule and show reduced self-quenching, while providing superior transport kinetics. The compounds have been found to provide enhanced fluorescence when bound to a DNA molecule within a fluorescent flow cytometry environment which is about eight to ten times brighter in fluorescence than "bis" structure conventional intercalating agents and other known intercalating agents utilized in flow cytometry environment.

Abstract: The present invention relates to novel tricyclic tetrahydroquinoline compounds of the following formula, libraries containing such compounds, and to the generation of such combinatorial libraries composed of such compounds: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, n, and Y have the meanings provided.

Abstract: A phenanthridine derivative metal complex of formula 1 having a large absorption in the near-infrared range and a reduced absorption in the visible range, which phenanthridine derivative metal complex is used in a transparent recording medium: ##STR1## where M is a metal atom, and X is a negative ion.

Abstract: Fluorinated phenanthrene derivatives of the formula (I) ##STR1## in which the symbols and indices have the following meanings: E.sup.1, E.sup.2, E.sup.3, E.sup.4, E.sup.5 and E.sup.6 are identical or different and are --N--, --CF-- or --CH--;G is --CF.sub.2 CF.sub.2 -- or --CF.dbd.CF--;R.sup.1 and R.sup.2 are, for example, alkyl or alkoxy;M.sup.1, M.sup.2, M.sup.3 and M.sup.4 are, for example, O, --CO--O--, --O--CO-- or a single bond;A.sup.1 and A.sup.2 are, for example, 1,4-phenylene or pyrimidine-2,5-diyl;m and n are zero or one, but in total are not more than one,are suitable as components of liquid-crystalline mixtures.

Abstract: A method of fluorinating a heterocyclic organic compound comprises the step of reacting a heterocyclic compound with elemental fluorine in the presence of another halogen. The reaction may be conducted in the presence of a base.

Abstract: Non-naturally occuring dynemicin analogs are provided, which are useful as DNA cleaving agents, cytotoxic agents, and/or anti-tumor compounds. Methods of making dynemicin analogs are also provided.

Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

Abstract: Phenanthridine derivatives, and their use in liquid-crystalline mixturesA ferroelectric liquid-crystal mixture containing one or more phenanthridine derivatives of the formula (I) ##STR1## E.sup.1 and E.sup.2 are identical or different and are --N--, --CF-- or --CH--;R.sup.1 and R.sup.2 are identical or different and are, for example, a straight-chain or branched alkyl radical having 1 to 20 carbon atoms;Q is --CH.sub.2 --O--, --CO--O-- or a single bond;M.sup.1 and M.sup.2 are identical or different and are --CO--O--, --O--CO--, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --C.tbd.C--, or a single bond;A.sup.1 and A.sup.

Abstract: Novel acridinium esters that are useful, either alone or when incorporated into liposomes, as chemiluminescent agents in binding assays (e.g., immunoassays and gene probe assays) with improved-sensitivity are disclosed. In addition, the synthesis of these esters and their use in assays for detecting an analyte is described. In particular, assays for testosterone and the Rubella virus are disclosed.

Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in preventing the development of prostatic cancer, or preventing or treating the metastasis to bone of prostatic cancer.

Abstract: A quinone imine enediyne possessing cytotoxic activity towards cancer cells having the general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently the same or different and are H, Br, Cl, F, NH.sub.2, CO.sub.2 H, or OH or a linear or branched alkyl, etc.; wherein R.sub.4 is H, OH or a linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R.sub.5 is H, Br, Cl, F, O.dbd., OH or S--SR, or a linear or branched alkyl, etc.; wherein R.sub.6 is H, Br, Cl, F, CO.sub.2 H, OH or S--SR', or a linear or branched alkyl, etc; wherein R.sub.7 is H, OH or S--SR", or a linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl group; and wherein R, R' and R" are independently the same or different and are a linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl group.

Abstract: The present invention provides for the preparation of compounds,namely, 3-phenanthridinones and their derivatives and their unique ability to inhibit 5-alpha-reductase or their isozymes thereof in mammals enabling said compounds for treating hyperandrogenic conditions of acne, androgenic alopecia, male pattern baldness,female hirsutism,benign prostatic hyperplasia, prostatitis and prostatic cancer.

Abstract: Disclosed are novel cannabinoid (CB2) receptor agonists, their compositions, and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure, treating glaucoma, useful as antiinflammatory, immunosuppressive, analgesics agents, and as agents for treatment and prevention of emesis and nausea because of the activity on the cannabinoid receptor.

Abstract: Intercalator compounds are provided which are comprised of intercalator moieties, or substituted intercalator moieties, having one or more functionalized chains, or moieties, and which compounds provide a high affinity for binding to the DNA molecule and show reduced self-quenching, while providing superior transport kinetics. The compounds have been found to provide enhanced fluorescence when bound to a DNA molecule within a fluorescent flow cytometry environment which is about eight to ten times brighter in fluorescence than "bis" structure conventional intercalating agents and other known intercalating agents utilized in flow cytometry environment.

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: 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.