Abstract: The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.

Abstract: The present invention relates to benzofuran and benzothiophene derivatives and compositions containing such compounds for the production of medicaments for the treatment of cancers of the central nervous system as monotherapy or combination with other agents.

Abstract: This invention provides methods for treating in mammals asthma and asthmatic conditions using substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.

Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.

Abstract: The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. Formula I wherein: R1 is aminomethyl, (C1-C3 alkyl)aminomethyl, di(C1-C2 alkyl)aminomethyl, N-ethyl-N-methyl-aminomethyl, 1-aminoethyl, 1-((C1-C2 alkyl)amino)-ethyl, 3,3,3-trifluoro-propylaminomethyl, ethynyl, 2-hydroxy-ethoxy, 2-hydroxyethylaminomethyl, 2-cyanoethylaminomethyl, mopholin-4-ylmethyl, methoxymethoxymethyl, cyclopropyl, 1-azetidinylmethyl, 1-pyrrolidinylmethyl, or 1,3-dioxolan-2-yl; R2 is hydrogen or halo; R3 is hydrogen or halo; provided that at least one of R2 and R3 is hydrogen; R4 is hydrogen, methyl, or halo; and is a single bond that is either present or absent, or pharmaceutically acceptable salt thereof.

Abstract: For the purpose of providing a GSK-3? inhibitor containing an oxadiazole compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3?-related pathology or disease, the present invention provides a GSK-3? inhibitor containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

Abstract: The present invention refers to a modified release pharmaceutical composition comprising an in-situ gelling agent (=0.5 % w/w) and a gellation facilitating agent (e.g. calcium sulfate) in an amount of 2-17.5 % w/w. Additionally, the composition contains a release rate controlling polymer such as an acrylate and optionally a pH independent rate controlling polymer such as HPMC. A preferred active agent is mycophenolate mofetil. A process of making the above described composition is also disclosed.

Abstract: Pyrimidine compounds of the following formula: wherein R1, R2, R3, R4, R5, X, Q1, Q2, and Q3 are defined herein. Also disclosed is a method of treating cancer with one of these compounds.

Abstract: Disclosed herein are methods of treating neurodegenerative diseases comprising administering to the subject a compound having the structure: wherein ? and R1-R8 are described herein, or a compound having the structure: wherein Y, Z, and R21, R24, R25, and R31-R33 are described herein.

Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.

Abstract: The present invention provides methods for modulating an immune response by administering a composition comprising a Toll-like receptor agonist and an immune mediator which downregufates the expression of the anti-inflammatory cytokine IL-10 and upregulates the expression of the pro-inflammatory cytokine IL-12. The methods can be used to provide therapeutic treatment for cancerous conditions and infectious diseases.

Abstract: Disclosed are methods for inhibiting TNF? expression, IL-1? expression, iNOS expression, and NF-?B activity and methods for treating autoimmune disease, cancer, or atherosclerosis with a compound of the following formula:

Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.

Abstract: The object of the present invention is to provide a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and has superior properties such as efficacy, duration of activity, specificity, low toxicity and the like.

Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.

Abstract: The present invention provides a carbamoyl-type benzofuran derivative of the formula [1]: wherein Ring Z is a group of the formula: etc.; A is a single bond, and the like; Y is a cycloalkanediyl group, etc.; R4 and R5 are the same or different and each is an optionally substituted lower alkyl group, etc.; R1 is a halogen atom, etc.; Ring B of the formula: is an optionally substituted benzene ring; and R3 is a hydrogen atom. etc., or a pharmaceutically acceptable salt thereof, which is useful as an FXa inhibitor.

Abstract: This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.

Abstract: Benzothiophene compounds such as are DNA binding compounds exhibiting antibacterial activity.

Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.

Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, aryl, aralkyl, arylalkenyl, aryloxy-lower alkyl, heteroaryl, heteroaryl-lower alkyl, etc; R3, R4, R5 and R6 are each hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, lower alkoxy, hydroxy, aryl, etc; provided that at least one of R3, R4, R5 and R6 is other than hydrogen. Compound (I) of the present invention shows a potent adenosine A2A receptor antagonistic activity, and are useful for treating or preventing a disease mediated by adenosine A2A receptors such as motor function disorders, depression, anxiety disorders, cognitive function disorders, cerebral ischemia disorders, restless legs syndrome and the like.

Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to some 4, 5, 6, 7 tetrahydrobenzo[b]thiophene derivatives, wherein n is selected from 0, 1, 2, 3 or 4; m is selected from 0, 1 or 2; the dotted line represents either a single or a double bond; to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.

Abstract: Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as identified herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.

Abstract: An isoxazole derivative is provided. The isoxazole derivative has following formula: wherein R1, R2, R3, R4 and R5, independently, include hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis and cancer including an isoxazole derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Abstract: An isoflavone derivative is provided. The isoxazole derivative has following formula: wherein R1 and R2, independently, include C1-C12 alkyl optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy, and R3 includes hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis including an isoflavone derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.

Abstract: Phosphatidylinositol 3-kinases (PI3Ks) are known to be important regulators of signaling pathways. To determine whether PI3Ks are genetically altered in cancers, we analyzed the sequences of the P13K gene family and discovered that one family member, PIK3CA, is frequently mutated in cancers of the colon and other organs. The majority of mutations clustered near two positions within the P13K helical or kinase domains. PIK3CA represents one of the most highly mutated oncogenes yet identified in human cancers and is useful as a diagnostic and therapeutic target.

Abstract: Disclosed are novel isoflavone derivatives having the structure of Formula I which are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.

Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.

Abstract: The present invention is directed to molecules deriving from a 3-aryl-coumarine or 3-aryl-quinolin-2-one and having potent anti-proliferative and/or cytotoxic activity, especially against tumoral cells. The present invention also concerns the uses of these molecules in therapeutic application, for the treatment of different cancers. The invention also discloses the use of said compound for the manufacture of a medicament for treating cancer. The invention also concerns a process for inhibiting cell proliferation comprising contacting said cells with a compound of the invention.

Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.

Abstract: The present invention provides a method of preventing or treating one or more of the following medical conditions, or treating symptoms of one or more of the following medical conditions: amebic infections, giardiasis, estrogen deficient states, osteoporosis, cardiovascular heart disease, high cholesterol levels, hyperlipidemia, cancer by administering to a subject having, or predisposed to, one or more of the conditions, a therapeutically effective amount of a compound of the present invention and a pharmaceutically acceptable carrier.

Abstract: Disclosed are methods for inhibiting TNF? expression, IL-1? expression, iNOS expression, and NF-?B activity and methods for treating autoimmune disease, cancer, or atherosclerosis with a compound of the following formula:

Abstract: The present invention relates to compounds of formula I wherein X, A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.

Abstract: A combination of an mTOR inhibitor compound with one or more pharmaceutically active agents, for simultaneous, concurrent, separate or sequential use for preventing or treating a proliferative disease.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein R1, R2a, R2b, R2c, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.

Abstract: The present invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having anti-proliferative and antiangiogenic activities, as well as methods for treating various diseases associated with abnormal cell proliferation, including cancer, or associated with unregulated angiogenesis including growth and metastasis of solid tumors, ocular diseases and especially retinopathies, or arthritis, by administering said compounds. It further deals with pharmaceutical compositions comprising said compounds, more particularly useful to treat cancers (such as leukemia), ocular diseases and arthritis.

Abstract: The disclosure provides methods and compositions for treating a vascular, autoimmune, and/or inflammatory disease, or a condition associated therewith, with a dose of an inosine monophosphate dehydrogenase (IMPDH) inhibitor effective to treat the vascular, autoimmune and/or inflammatory disease, or associated condition but that does not produce immunosuppression sufficient to reduce the risk of allograft rejection. These lower doses of the immunosuppressant avoid the adverse consequences of severe immunosuppression while providing effective treatment of the vascular, autoimmune and/or inflammatory disease.

Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.

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

Abstract: The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R3-8, X3, X5, m, and n are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).

Abstract: The invention provides new oxazolidinone compounds of formula (I) wherein A is certain heterocycles optionally substituted; R1, R2, R3 and R4 are independently selected from —H and halogen; X is selected from O, S, NR9 and CR9R10; R9 and R10 having different meanings; Y is selected from O, S, SO, SO2, NO, NR12 and CR12R13; R12 and R13 having different meanings. It also provides different processes for the preparation of such compounds. Oxazolidinone compounds of formula (I) are active against Gram-positive and some Gram-negative human and veterinary pathogens with a weak monoamine oxidase (MAO) inhibitory activity. They are useful for the treatment of bacterial infections.

Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.

Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: This invention relates to the finding that inhibition of the catalytic subunit of DNA protein kinase (DNA-PKcs) increases the sensitivity of cancer cells that display an ATM deficient phenotype to DNA damaging therapies, such as irradiation or chemotherapy. Methods of treating cancers displaying an ATM deficient phenotype and methods of determining the susceptibility of a patient to such methods are provided.

Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.

Abstract: The present invention relates to compounds of formula I wherein X, A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.