Abstract: The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I): wherein Y1 represents N or C(R4); Y2 represents N or C(R5); R4 and R5 independently represent an alkyl group, a hydrogen atom etc.; one of R1 and R2 represents an optionally substituted aryl group, an alkoxy group or an optionally substituted heterocyclic group; the other of R1 and R2 represents a haloalkyl group, a cyano group, a halogen atom etc.; and R3 represents a 5-tetrazolyl group or a carboxy group, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same as an active ingredient.

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.

Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.

Abstract: Compounds of formula (I): [in which: X is a group of formula >CR1R2 or >SO2; Y is a group of formula >NH or >CR1R2; Z is a group of formula >C?O or >CH2 or a direct bond; R1 is hydrogen and R2 is hydrogen, carboxy or hydroxy; or R1 and R2 together represent an oxo group, a methylenedioxy group or a hydroxyimino group; R3 is hydrogen or lower alkyl; R4 represents two hydrogen atoms, or an oxo or hydroxyimino group; R5 is hydrogen, lower alkyl or halogen; R6 is hydrogen, lower alkoxy or carboxy; R7 and R8 are each hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts and esters thereof can be used for the treatment or prophylaxis of acute or chronic neurodegenerative diseases or conditions such as Alzheimer's Disease, Parkinson's Disease, Huntington's Chorea, Multiple Sclerosis or the sequelae to acute ischaemic events such as heart attack, stroke or head injury and for protection against ischaemic damage to tissues of peripheral organs.

Abstract: Novel epoxy compounds having imide structures represented by general formula (I) or general formula (II) below, and having an allyl group in the same molecule, as well as a process for their production.

Abstract: The invention relates to a nitrogen heterocycle compound of formula 1: Also disclosed are a method of synthesizing the compound and use of the compound for treating various diseases and conditions.

Abstract: The present invention is directed to substituted 4H-chromenes and analogs thereof, represented by the Formula (I): wherein R1, R3-R5, A, D, Y and Z are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: The present application describes deuterium-enriched SDX-101, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: 3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Such compounds are useful for modulating activity of a 5-HT1A receptor (agonizing or antagonizing) in a patient. These compounds are further useful for inhibiting binding to a serotonin receptor. Methods of using the 3-amino chroman and 2-amino tetralin compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety, are also disclosed.

Abstract: The present invention provides a prophylactic or therapeutic agent for irritable bowel syndrome, which comprises a compound represented by formula (I): wherein, R1 represents an optionally substituted hydrocarbon group, etc., R2 represents a hydrogen atom or an optionally substituted hydrocarbon group, R3 represents a hydrogen atom, an optionally substituted hydrocarbon group, etc., X represents CHR4, NR4, CO, O or S (wherein, R4 represents a hydrogen atom, an optionally substituted hydrocarbon group, etc.), Y represents C, CH or N, represents a single bond or double bond, ring A represents an optionally substituted 5- to 7-membered oxygen-containing heterocyclic ring, ring B represents an optionally substituted benzene ring, and m represents an integer of 1 to 4, or a salt thereof.

Abstract: The present invention relates to novel thiosulfonates derivatives. The present invention also provides methods for preventing, treating and/or reducing inflammation-associated diseases in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous or cutaneous systems as well as infective and tumoral diseases employing said compounds.

Abstract: The present invention is directed to substituted 4H-chromenes, 2H-chromenes, chromans and analogs thereof, represented by the general Formula (I) wherein R5, A, B, X, Y, Z and dotted lines are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: The invention provides novel compounds useful as intermediates for the production of polymethine compounds containing a desired counter ion with high purity and in high yields. Thus provided are polymethine ether compounds of the general formula (I) given below and a method of producing polymethine compounds which comprises bringing those compounds into contact with an acid. In the above formula, R represents an alkyl group, an alkoxyalkyl group or an aryl group which may optionally be substituted, R1 and R2 each independently represents a hydrogen atom, halogen atom, nitro group, alkyl group, alkoxyalkyl group, alkoxy group or alkoxyalkoxy group and R1 and R2 may be bound to each other to form a ring; R3 represents an alkyl group, which may optionally be substituted; L is an alkylene group required for the formation of a ring structure; and X represents a hydrogen atom, halogen atom, alkoxy group, aryloxy group, alkylthio group, arylthio group or substituted amino group.

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytotoxic drugs in a targeted fashion.

Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).

Abstract: A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system, cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea

Abstract: Improved synthesis of seco(?)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2-dihydro-3H-benz(e)indole): and improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.

Abstract: A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea

Abstract: A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.

Abstract: Anlogs of ningalin B lacking inherent cytotoxic activity may be employed to reverse multi-drug resistant (MDR) phenotype and to resensitize transformed cells, including a human colon cancer cell line (HCT116/VM46), with respect to a variety of cytotoxic agents, e.g., vinblastine and doxorubicin. In many instances, resensitization is achieved at lower doses than the prototypical agent verapamil. Total synthesis of ningalin B and its analogs was achieved using a concise, efficient approach based on a heterocyclic azadiene Diels-Alder strategy (1,2,4,5-tetrazine?1,2-diazine?pyrrole) ideally suited for construction of the densely functionalized pyrrole core found in the natural product is detailed.

Abstract: The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.

Abstract: A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea

Abstract: The present invention provides compounds and methods of administering compounds to a subject that can reduce ?APP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce ?APP production and that is not tocix in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease ?APP production.

Abstract: Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.

Abstract: Substituted pyranoindoles useful for lowering and controlling IOP and glaucoma are disclosed.

Abstract: A compound represented by the formula (I): or a salt thereof exhibits excellent inhibitory activity of lipid peroxidation and is useful as an agent for inhibiting lipoperoxide production, wherein ring A denotes a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, B ring denotes a benzene ring which may be further substituted, C ring denotes a dihydrofuran ring which may be further substituted, and R denotes hydrogen atom or an acyl group.

Abstract: A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, alkylsulfonyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, a

Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.

Abstract: Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

Abstract: A compound represented by the formula: wherein Ring A is a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, Ring B is benzene ring which is further substituted, Ring C is a dihydrofuran-ring which may be further substituted and R is hydrogen atom or an acyl group or a salt thereof has an excellent lipid peroxidation inhibitory activity and is useful as a lipid peroxidation inhibitor.

Abstract: The present invention provides selective kinase inhibitors of formula (I)

Abstract: The present invention relates to the use of an EP4 receptor ligand in the manufacture of a medicament for use in the treatment of neuropathic pain, colon cancer, migraine, and for increasing the latency of HIV infection.

Abstract: Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems; (wherein R1 is hydrogen; R2 is hydrogen or lower alkyl; R3 is hydrogen, —COOR12 and so on; R4 is hydrogen, lower alkyl and so on, or R3 and R4 taken together may form ?O or ?S; R5 is hydrogen, or R3 and R5 taken together may form a bond; R6 is hydrogen, —COOR24 and so on; R7 is hydrogen, halogen, lower alkyl and so on; R8 is hydrogen, lower alkyl, cycloalkyl and so on; R9, R10 and R11 are each independently hydrogen, halogen, lower alkyl and so on).

Abstract: The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor &bgr; agonists. Such agonists are useful for the treating Estrogen Receptor &bgr; mediated diseases such as prostate cancer.

Abstract: This invention relates to compounds of Formula I or stereoisomers, pharmaceutically acceptable salts or prod rugs thereof or a pharmaceutically acceptable salts of the prodrugs. This invention also relates to pharmaceutical compositions comprising a compound of Formula I, and to methods of treatment of diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, or tissue ischemia.

Abstract: Disclosed are substituted indoles, pharmaceutical compositions containing such indoles, and their use in treating or preventing PPAR-&ggr; mediated diseases or conditions, such as osteopenia, osteoporosis, cancer, diabetes and atherosclerosis.

Abstract: The present invention provides substituted thiophene carboxamide compounds having structural Formula I and isomers, tautomers, polymorphs, carriers, prodrugs, and pharmaceutically acceptable salts thereof, compositions comprising such, and methods for treating diseases associated with kinase activity. More specifically, the present invention provides methods of treatment of a variety of diseases associated with IKK2 including the treatment of inflammation, other inflammation-associated disorders, such as, as an analgesic in the treatment of pain and headaches, arthritis, including but not limited to rheumatoid arthritis, asthma, gastrointestinal conditions such as inflammatory bowel disease, vascular diseases, viral infections such as AIDS, and cancer.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems.

Abstract: Anlogs of ningalin B lacking inherent cytotoxic activity may be employed to reverse multi-drug resistant (MDR) phenotype and to resensitize transformed cells, including a human colon cancer cell line (HCT116/VM46), with respect to a variety of cytotoxic agents, e.g., vinblastine and doxorubicin. In many instances, resensitization is achieved at lower doses than the prototypical agent verapamil. Total synthesis of ningalin B and its analogs was achieved using a concise, efficient approach based on a heterocyclic azadiene Diels-Alder strategy (1,2,4,5-tetrazine → 1,2-diazine → pyrrole) ideally suited for construction of the densely functionalized pyrrole core found in the natural product is detailed.

Abstract: The present invention relates to a group of aza-thioxanthenone compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-thioxanthenone compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.

Abstract: A method for the preparation of a compound of general Formula: 1

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.

Abstract: The invention relates to novel peptide derivatives, called memno peptides, of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8 and (A)n have the meaning herein, obtainable by cultivation of Memnoniella echinata FH2272, DSM 13195 or mutants and variants of this, a process for their preparation and the use of the compounds as pharmaceuticals, for example against cardiac insufficiency.

Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.

Abstract: There is disclosed novel fused thiophene derivatives as prophylactic and therapeutic drugs for bone or articular diseases, industrially advantageous processes for production thereof, and novel production intermediates.

Abstract: The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description

Abstract: The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.

Abstract: The present invention relates to a compound having a tricyclic amine substituent which may have various substituents, the compound being represented by formula (I), a salt or hydrate thereof, and a hydrate of the salt and a drug containing them as an active ingredient. They exhibit excellent antimicrobial activity against Gram negative bacteria and Gram positive bacteria with a satisfactory fate and safety and are useful in the treatment of infectious diseases.

Abstract: The present invention provides compounds of formula (I): 1