Abstract: The present invention relates to novel tetracyclic benzimidazole derivative compounds of the following formula: wherein R1 to R10 have the meanings described in here. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing tetracyclic benzimidazole derivative compounds.

Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.

Abstract: This invention provides [1,4]diazepino[6,7,1-jk]carbazole compounds of the formula: wherein: R1 and R2 are H, alkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, phenoyl or thiophenoyl; R3, R4, R5 and R6 are H, alkyl, cycloalkyl, alkoxy or cycloalkoxy; R7 is H or alkyl; R8 is H or alkyl; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, as well as methods and pharmaceutical compositions utilizing them for the treatment or prevention of disorders such as obsessive-compulsive disorder, depression, anxiety, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

Abstract: Pyrrolidine compounds of Formula I: 1

Abstract: The present invention provides medicines for treating cardiac insufficiency which contain as an active ingredient indane derivatives of formula (I) wherein R1 represents hydrogen atom, nitro group, cyano group, C1-6 alkylcarbonylamino, R2 and R3 each independently represent C1-6 alkyl group, R4 represents hydroxyl group or C1-6 alkylcarbonyloxy group or represents a bond or oxygen atom together with R5, R5 represents hydrogen atom or represents a bond or oxygen atom together with R4, R6 represents hydrogen atom, hydroxyl group or NR7R8, n means 0 or an integer of 1 to 4, X represents C═O, CH2, SO2 or NR16, Y represents NR17 when X is C═O, CH2 or SO2 and represents C═O when X is NR16, Z is absent when Y represents NR17 or represents NR18 when Y is C═O, W represents aromatic groups or lactam rings, or pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) 1

Abstract: Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I, A—B—D—E—F—G   (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Abstract: Acetyldinaline in combination with gemcitabine, a pharmaceutically acceptable salt thereof, capecitabine, or cisplatin is synergistic for treating cancer.

Abstract: Pharmaceutically active benzodiazapine compounds of formula (I) are disclosed. These compounds inhibit the vitronectin receptor and are useful for treatment of osteoporosis.

Abstract: A condensed thiophene compound of the formula (I) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the formula (I) of the present invention is useful as a novel antipsychotic agent which is effective for both positive symptoms and negative symptoms of schizophrenia, which is associated with less side effects such as extrapyramidal motor disorder and the like and which is less associated with serious side effects such as agranulocytosis and the like. In addition, this compound is also useful as a therapeutic agent of Alzheimer's disease and manic-depressive illness.

Abstract: This invention provides compounds of the formula: 1

Abstract: This invention provides compounds of formula I having the structure 1

Abstract: A triazolo-1,4-diazepine compound having the formula (I): wherein A represents CO, CO—B, or B, B represents a C1 to C6 alkylene group or a C2 to C6 alkylene group having an oxygen atom interposed in the middle thereof, X represents N—O or CH, n represents an integer of 2 to 6, R represents a hydroxyl group, a C1 to C6 lower alkyloxy group or a C1 to C6 lower alkylamino group, provided that these groups may be substituted with an N,N-dimethylamino group, an N,N-diethylamino group, a phenyl group, or a heterocyclic group, and R1 represents a hydrogen atom or a C1 to C3 lower alkyl group having both a PAF antagonistic action and a thromboxane synthesis inhibiting action, and a pharmaceutical composition containing the same as an active ingredient.

Abstract: The present invention relates to novel N12, N13-bridged sugar derivatives of indolylopyrrolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.

Abstract: This invention provides compounds of the formulae: 1

Abstract: The present invention is a compound of formula 1

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.

Abstract: The use of CCK-B antagonists for the treatment of sleep disorders.

Abstract: This invention provides a process for the preparation of 1, 2, 3, 4, 8, 9, 10, 10a-octahydro-7bH-cyclopenta[b][1,4]diazepino[6, 7, 1-hi]indole derivatives of the general formula: 1

Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.

Abstract: The invention concerns compounds of formula (I), in which R1, R2, R3 and R4 mean hydrogen or different substituents; X means hydrogen or halogen; Y means C1-6 alkoxy or X and Y together mean —O—(CH2)n—O—; n means 1, 2 or 3; and A together with nitrogen forms a saturated or unsaturated five-member heterocycle which can contain between 1 and 3 nitrogen atoms and/or an oxygen atom and/or one or two carbonyl groups. Owing to their non-competitive inhibiting of the AMPA receptors, these compounds can be used as medicaments for treating diseases of the central nervous system.

Abstract: The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example as anorectics and in the treatment or prophylaxis of type II diabetes.

Abstract: The invention relates to a method for treating pruritus by administering a therapeutically effective amount of a PAF antagonist to a mammal afflicted with pruritus. The PAF antagonists may, for example, be selected from synthetic PAF analogues, natural products isolated from plants having PAF antagonist activity, and triazolobenzodiazepines. The PAF antagonists are preferably applied topically to the afflicted site but systemic such as oral, parenteral, nasal and intrarectal administration, is also possible.

Abstract: A condensed thiophene compound of the formula (I) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the formula (I) of the present invention is useful as a novel antipsychotic agent which is effective for both positive symptoms and negative symptoms of schizophrenia, which is associated with less side effects such as extrapyramidal motor disorder and the like and which is less associated with serious side effects such as agranulocytosis and the like. In addition, this compound is also useful as a therapeutic agent of Alzheimer's disease and manic-depressive illness.

Abstract: Compounds of the formula (I): where X1, A, Ar1, X and R are as defined in the specification, and pharmaceutically-acceptable salts thereof, are new, and are useful as tachykinin inhibitors which act at the NK1, NK2 and NK3 receptors or a combination of two or more thereof.

Abstract: The invention provides compositions that include conjugates of a fatty acid molecule, preferably cis-docosahexaenoic acid, and clozapine. The conjugates are useful in treating psychological disorders such as schizophrenia.

Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl or C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or trihalomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.

Abstract: The present invention is directed to novel fused aryl and heteroaryl bridged indenopyrrolocarbazoles which are useful, inter alia, as therapeutic agents. The invention is also directed to methods for making and using the bridged indenopyrrolocarbazoles.

Abstract: This invention provides methods of of inhibiting mucin production in a mammal comprising administering to the mammal an RAR antagonist. Preferably, the RAR antagonist is an RAR.alpha. selective antagonist.In another aspect, this invention provides methods of inhibiting mucin gene expression in a human epithelial cell by contacting the cell with an RAR antagonist, preferably an RAR.alpha. selective antagonist.

Abstract: Novel indolocarbazole derivatives potentially useful for the treatment of dementias characterized by tau hyperphosphorylation [Alzheimer's disease (AD), frontal lobe degeneration (FLD), argyrophilic grains disease, subacute sclerotizing panencephalitis (SSPE) as a late complication of viral infections in the CNS], and cancer.

Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R.sup.1 represents hydrogen atom or a C.sub.1-6 alkyl group; R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-6 alkyl group, or R.sup.2 and R.sup.3 may combine together to represent a 5- or 6-membered cycloalkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.5 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group; x represents --NR.sup.7 --, --O--, --CHR.sup.7 -- or --S-- in which R.sup.7 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.

Abstract: A dosage form is disclosed for delivering an antiepileptic drug, which dosage form comprises for maintaining the integrity of the dosage form and of the antiepileptic drug.

Abstract: The invention refers to the composition of substances to prevent and treat endothelial cell-mediated disorders with pathological differentiation of endothelial cells, for example, in response to insulin, lipids, lipoproteins or LA-paf. The invention refers to simple methods to test and use antagonists against LA-paf, paf and very high affinity receptors on endothelial cells which can also be cultured on soluble particles for screening procedures. According to the invention genes producing very high affinity receptors, for example, in response to growth factors such as insulin. These genes can be transferred from adherent endothelial cell lines to soluble cells using standard procedures. Antagonists against LA-paf, paf and very high affinity receptors are administered by preference to healthy persons having risk factors to protect against aging and metabolic, genetic, chronicle, idiopathic, inflammatory or degenerative disorders.

Abstract: The invention relates to substituted 2,3-benzodiazepin-4-ones which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, CMV retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition enhancers.

Abstract: Tricyclic compound 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 process for preparing such compounds.

Abstract: The present invention provides methods for treating migraine headache. The methods useful according to the invention involve the treatment of patients who experience symptoms of migraine headache with compounds that directly or indirectly activate GABA.sub.A receptors.

Abstract: A hetrazepine of the formula given below and a pharmaceutical composition comprising a therapeutically effective amount of the hetrazepine and a pharmaceutically acceptable inert carrier are disclosed and are useful in treating disease in a warm-blooded animal induced by endogenously formed PAF; ##STR1## wherein the substituents are defined herein.

Abstract: Disclosed are novel 2-aryl-5,11-dihydro-6H-dipyrido?3,2-b:2',3'-e!?1,4!diazepines. These are useful in the of HIV infection. Exemplary compounds are:8-Ethyl-1-methyl-10-(4-pyrazolyl)imidazo?2',3':6,5!dipyrido?3,2-b:2',3'-e!? 1,4!diazepine;8-c-Propyl-1-methyl-10-(4-pyrazolyl)imidazo?2',3':6,5!dipyrido?3,2-b:2',3'- e!?1,4!diazepine;8-Ethyl-12-methyl-10-(4-pyrazolyl)imidazo?2',3':6,5!dipyrido?3,2-b:2',3'-e! ?1,4!diazepine; and,8-c-Propyl-12-methyl-10-(4-pyrazolyl)imidazo?2',3':6,5!dipyrido?3,2-b:2',3 '-e!?1,4!diazepine.

Abstract: N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## wherein R.sup.1 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.11, --C(NH)N(H)C(O)R.sup.9, or --C(NH)N(H)C(O)OR.sup.11 ;R.sup.2 and R.sup.3 are independently hydrogen, halo, lower alkyl, lower haloalkyl, aryl, --OR.sup.11, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, --N(R.sup.11)R.sup.12, --N(H)C(O)R.sup.11, or --N(H)S(O).sub.2 R.sup.11 ;R.sup.4 is halo, lower haloalkyl, imidazolyl, --C (NH)NH.sub.2, --C(NH)NHOR.sup.11, --C(NH)N(H)C(O)R.sup.9, --C(NH)N(H)C(O)OR.sup.11, --OR.sup.11, --C(O)R.sup.13, --(CH.sub.2).sub.n C(O)OR.sup.11 (where n is 0 to 6), --C(O)N(R.sup.11)R.sup.12, or --N(R.sup.11)R.sup.12 ;R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl, lower haloalkyl, 4-pyridinyl, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, or aryl (optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy and --N(R.sup.11)R.sup.12);R.sup.

Abstract: The present invention is a method for controlling ectoparasites. More particularly, the invention relates to a method of treatment in which the warm blooded animal is dosed with an ovicidally effective amount of a heterocyclic nitrogen compound selected from the group represented by the formula: ##STR1## wherein R.sub.1, is either one of the following groups: ##STR2## in which R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, and R.sub.17 are, the same or different, each a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 alkylthio group, a trifluoro methyl group or a vitro group, R.sub.18, R.sub.19, R.sub.20 and R.sub.21 are, the same or different, each a hydrogen atom or a methyl group, k is an integer of 0 to 1 and 1 is an integer of 0 to 3; R.sub.2 and R.sub.3 are, the same or different, each a hydrogen atom, a halogen atom or a methyl group; R.sub.4 is a halogen atom or a methyl group; R.sub.5 and R.sub.

Abstract: A tricylic benzodiazepine derivative that acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

Abstract: Thienotriazolodiazepine compounds of the formula (1) ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof, and pharmaceutical use thereof. The compounds of the present invention are useful as preventive and therapeutic drugs for inflammatory diseases and allergic diseases, in which cell adhesion is involved.

Abstract: A tricylic benzodiazepine derivative that acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

Abstract: The present invention relates to thienodiazepines of formula Ib: ##STR1## wherein U, V, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. This invention also relates to processes for preparing these thienodiazepines and their use in pharmaceutical compositions with PAF-antagonistic activity.

Abstract: The invention refers to the treatment and prevention of eosinophil-mediated diseases with paf antagonists and a procedure for determining their efficacy. According to the invention for treating and prevention a disease mediated by eosinophils a combination with an effective amount of at least one paf antagonist is administered to a subject requiring said treatment of allergy and inflammation, wherein the paf antagonist is a hydrophilic or non-hydrophilic triazolothieno-diazepine or a homologue thereof, a ginkgolide, a ginkgolide mixture or a synthetic ginkgolide derivate, or an analogue of the paf or a mixture with/of these compounds.

Abstract: The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity.This amino acid derivative is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or an acyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent;m and n represent each independently an integer of 0, 1 or 2 andJ represents a cyclic group having an angiotensin I-converting enzyme inhibition activity.

Abstract: Novel benzoheterocyclic compound of the formula (1): ##STR1## and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist or oxytocin antagonist.

Abstract: A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

Abstract: A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

Abstract: Nasal administration of benzodiazepines is described as providing improved therapeutic effects as compared to conventional delivery techniques. The compositions comprise a benzodiazepine hypnotic in a pharmaceutically acceptable nasal carrier.