Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl 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 the treatment or prophylaxis of neurological injury and neurodegenerative disorders.

Abstract: The present invention provides NPY-5 receptor antagonists having a Formula (I) 1

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

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: This invention pertains to the discovery of a novel family of thiolesters and uses thereof. Also provided for are viricidal compounds and pharmaceutical formulations comprising these novel thiolesters. The invention also provides thiolester-inactivated viruses and thiolester-complexed viral proteins.

Abstract: Compounds of the formula I, in which Het is an unsubstituted or R6-and/or R7-sustituted pyrrolyl, furanyl, thiophenyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, thiadiazolyl, pyrimidinyl, pyrazinyl or pyridazinyl radical, or an unsubstituted or R6-and/or R7-substituted fused bi-or tricyclic ring system comprising at least one aromatic ring and up to 4 heteroatoms—selected from the group consisting of O(oxygen), S(sulphur) or N(nitrogen)—which is bonded to the phenanthridinyl radical via one of the rings comprising one or more rheteroatoms, areactive PDE4 inhibitors.

Abstract: The present invention provides methods of modulating neurotrophic factor-associated activity, especially CNTF-associated levels and activity, using aldose reductase inhibitors. These methods are especially useful in individuals suffering from, or at risk of developing, neurological disorders, including neurodegenerative disorders. The invention also provides methods of palliating neurological disorders and delaying development of neurological disorders using aldose reductase inhibitors.

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 present invention relates to protoberberine derivatives which inhibit the activity of mitogen-activated protein kinase. More specifically, the present invention is directed to protoberberine derivatives which inhibit the activity of Wis1 and Spc1 kinase in intracellular signal transduction cascade wherein mitogen-activated protein kinase (MAPK) is involved.

Abstract: The present invention relates to compounds, compositions and methods for the prevention or treatment of mycobacterium infections. The compounds are naturally occurring and synthetic biflavonoids, flavonoids, chalcones and chalcone like compounds. The compounds were screened for anti-mycobacterium activity. Of the compounds showing anti-mycobacterium activity, eight were identified as particularly potent, exhibiting greater than 90% inhibition of the growth of Mtb at a concentration of 12.5 &mgr;g/mL. The actual minimum inhibitory concentrations (MIC), defined as the lowest concentration inhibiting 99% of the inoculum, for the preferred compounds ranged from 6.8 to 48.3 &mgr;M.

Abstract: The use of phanquinone for the manufacture of a pharmaceutical composition for the prevention or the treatment of Alzheimer's disease is disclosed. Also methods of treatment or prevention of Alzheimer's disease are disclosed.

Abstract: N-oxides of the compounds of formula (I) in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, or in which R1 and R2 together are a 1-2C-alkylenedioxy group, R6 is an R7- and R8-substituted phenyl radical, they are active bronchial therapeutics.

Abstract: The reduced (or ‘leuco’) forms of certain pharmaceutically active compounds can be used for the treatment or pro-phylaxis methaemoglobinaemia or of a disease or disorder associated with or resulting from oxidative stress, such as Alzheimer's disease, motor neurone disease, Lewy Body disease, Pick's disease, Progressive Supranuclear Palsy, ischaemia, myocardial infarction, acute lung injury, stroke, Parkinson's disease or haemolysis and anaemia in acute falciparum malaria.

Abstract: Compounds according to formula I: T1—L—T2   (I), wherein T1 is a taxoid group, preferably of Formula II: wherein R1 is C6H5; R2 is O; L is a linking group; and T2 is a substituent selected from the group consisting of epipodophyllotoxin, amsacrine, ellipticine, anthracycline antibiotic, mitoxantrone, and colchicine groups, and pharmaceutically acceptable salts thereof, are provided herein. The compounds are useful in, among other things, treating tumors or cancer in subjects in need thereof, inducing cellular differentiation, and inhibiting cellular mitosis.

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

Abstract: The present invention discloses novel sulfenate derivatives and their bioconjugates for phototherapy of tumors and other lesions. The sulfenates of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photofragmentation of the sulfenate moiety, with the tissue of interest.

Abstract: The invention is directed to a method of modulating paraptotic cell death in a cell by contacting the cell with an effective amount of a compound selected from the group consisting of ceramide, Tumor Necrosis Factor (TNF), caspase-7, caspase-8, &agr;-amino-3-hydroxy-5-methyl-4-isoxazole proprionic acid (AMPA), kainic acid and glutamic acid, wherein the effective amount of the compound induces paraptotic death of the cell. The invention further is directed to a method of inhibiting paraptotic cell death in a cell by contacting the cell with an effective amount of a compound selected from the group consisting of Alg-2-interacting protein 1 (AIP-1), Jun N-terminal kinase 1 (JNK1) neutralizing agent, Jun N-terminal kinase 2 (JNK2) neutralizing agent, TNF Receptor-Associated Factor 2 (TRAF2) neutralizing agent, ortho-phenanthroline and the JNK inhibitor SP 600125, wherein the effective amount of the compound inhibits paraptotic death of the cell.

Abstract: N-oxides of the compounds of formula (I) in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, or in which R1 and R2 together are a 1-2C-alkylenedioxy group, R6 is an R7- and R8-substituted phenyl radical, they are active bronchial therapeutics.

Abstract: Compositions having synergistic effective amounts of one or more antibacterial agents, a nitroimidazole, and an antifungal agent effective against a Candida species. The compositions are particularly useful in the treatment of genitourinary infections.

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: 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: 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: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.

Abstract: The invention features methods for inhibiting immunostimulatory DNA-associated immune responses, through the administration of specific compounds of the general class of 9-aminoacridines and 4-aminoquiniolines. The invention also features methods of screening compounds useful in inhibiting immunostimulatory DNA-induced immune responses.

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: 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 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: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.

Abstract: A method for the treatment or prophylaxis of diseases treatable or preventable by potentiating the effect of a neurotrophin by administering a therapeutically effective amount of a 6(5H)-phenanthridinone derivative represented by the 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: The invention relates to the identification of pharmacological agents to be used in the treatment of Alzheimer's disease and related pathological conditions and compositions for treatment of conditions caused by amyloidosis, A&bgr;-mediated formation of ROS, or both, such as Alzheimer's disease, are disclosed.

Abstract: The invention features methods for inhibiting immunostimulatory DNA-associated immune responses, through the administration of specific compounds of the general class of 9-aminoacridines and 4-aminoquinolines. The invention also features methods of screening compounds useful in inhibiting immunostimulatory DNA-induced immune responses.

Abstract: The invention relates to compounds of formula (I), as defined herein. The invention also relates to the use of the inventive compounds for treatment of a disease caused by the effects of nitrogen monoxide in pathological conditions.

Abstract: Compounds, compositions containing compounds, methods of using compounds, and processes of making compounds, of formula I containing at least one ring nitrogen: 1

Abstract: The invention concerns new guanidine derivatives of formula (I), methods of preparing them and their use in drugs containing such compounds.

Abstract: The present invention provides for the combined use of 5&agr;-reductase inhibitors together with calcium channel blockers for the treatment of benign prostatic hyperplasia (BPH), prostate cancer, prostatitis, hematuria, and other androgen related disorders, including prostatitis and the prevention of prostate cancer. This invention provides a method of treatment which is useful in the treatment of benign prostatic hyperplasia, prostatitis, and/or the prevention and treatment of prostatic cancer, as well as in the treatment of prostatitis and hematuria. This invention also provides a pharmaceutical composition which is useful in the treatment of benign prostatic hyperplasia, prostatitis, hematuria and/or the prevention and treatment of prostatic cancer, wherein the pharmaceutical composition comprises the combination of a 5&agr;-reductase inhibitor and a calcium channel blocking agent.

Abstract: Compounds or compositions containing compounds of the formula A-(X1—NO2)to or salts thereof, for the preparation of antithrombotic medications wherein “to” is the integer 1 or 2X1 is an alkylene connecting bridge and “A” is the residue of timolol or analapril.

Abstract: The invention features methods for inhibiting immunostimulatory DNA-associated immune responses, through the administration of specific compounds of the general class of 9-aminoacridines and 4-aminoquiniolines. The invention also features methods of screening compounds useful in inhibiting immunostimulatory DNA-induced immune responses.

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: Methods and compositions for treating pathogens in material are described, including methods of decontaminating human fluids prior to processing in the clinical laboratory and methods for decontaminating blood products prior to in vivo use. The techniques handle large volumes of human serum without impairing the testing results.

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: The invention relates to compounds of formula (I): wherein R1, R2, R3, R31, R4, R5, R51 and R6 are as defined in the specification. The compounds are phosphodiesterase inhibitors. Also disclosed are pharmaceutical compositions and methods of use of the compounds.

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: Combination of low doses of irradiation and chelerythrine results in increased apoptosis in tumor cells. The doses of either irradiation or chelerythrine alone are such that increased apoptosis or decreased tumor growth or proliferation would not be expected.