Abstract: The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.

Abstract: The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

Abstract: The invention provides certain compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein.

Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.

Abstract: Disclosed are C-ring modified tricyclic benzonaphthiridinone compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.

Abstract: A solid dispersion comprises, in essentially non-crystalline form, a kinase inhibitory compound, e.g., N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a cancer.

Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Abstract: The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

Abstract: The invention provides compounds and salts of Formula I and Formula which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

Abstract: Imidazoquinoline and imidazonaphthyridine compounds having a nitrogen-containing heterocyclyl substituent at the 5-, 6-, 7-, or 8-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

Abstract: Provided are compounds according to Formula (I): or stereoisomer, prodrug, polymorph, or pharmaceutically acceptable salt forms thereof, wherein X, Y, R1, R6, R7, and R8 are as defined, and which compounds are effective inhibitors of PI3-kinase and/or other medically and clinically relevant kinases. Also provided are pharmaceutical compositions and methods of using the compounds and compositions as PI3-kinase and kinase inhibitors. More particularly, the compounds of the invention provide treatments and therapeutics for human diseases regulated by, or associated with, the activity of, PI3-kinases and/or protein kinases, or mutant or variant forms thereof.

Abstract: The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. The substituents R, R5, R6, R7, R8 and R9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.

Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.

Abstract: The present invention is directed to oxazolobenzimidazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

Abstract: The present invention relates to new compounds of the formula (I), (II), or (III) wherein R1, R2, R3, R4, R5 and W are as defined herein, and pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloid disease, such as observed in Alzheimer's disease, infectious diseases, PAI-I related disease, and in the manufacture of medicaments for such treatment.

Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is alkoxy or halogen; W is CH or N; A is O or NH; B is CO or (CH2)q; G is a group having one of the three formulae below wherein Q represents O or S, Z represents CH or N, R2 represents halogen and R3 represents alkyl; m is 0 or 1; and n is 1 or 2; p is 0 or 1, provided m and p are not each 0; and q is 1 or 2; and salts of such compounds.

Abstract: Thiadiazole compounds, compositions, bioconjugates, and methods for targeting and photoactivation at target sites.

Abstract: The present invention is directed to oxazolobenzimidazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

Abstract: The present invention relates to novel GABAA/BzR ligands of the general formulas (I), (II) and (III) wherein R1 is selected from the group consisting of hydrogen, halogen, haloalkyl having 1-2 carbon atoms, alkoxy having 1 to 3 carbon atoms in the alkyl chain, alkyl having 1 to 3 carbon atoms, and nitro, and R2 is selected from the group consisting of hydrogen, halogen and alkyl having 1 to 2 carbon atoms, as well as the use of these compounds for treating anxiolytic, anticonvulsant, sedative-hypnotic and myorelaxant conditions as well as anxiogenic, somnolytic and convulsant conditions in mammals including pharmaceutical compositions comprising the same

Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.

Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: Novel luciferins, methods of making luciferins, and uses of the same are disclosed.

Abstract: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate protein kinase CK2 activity, Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.

Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.

Abstract: The invention provides compounds of Formula I: wherein R1-R6 are described in the Summary of the Invention; the pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKK?, IKK?, JNK2?2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFR?, PKA, PKB?, PKD2, Rsk1, SAPK2?, SAPK2?, SAPK3, SGK, Tie2 and TrkB kinases.

Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a prodrug ester thereof, or a pharmaceutically-acceptable salt thereof, in which: Z is heterocyclo or heteroaryl; -A is a 5- to 8-membered carbocyclic ring or a 5- to 8-membered heterocyclic ring; B1 and B2 rings are pyridyl rings, wherein the B1 and B2 rings are each fused to the A ring and the B1 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R1, R2, and R4, and the B2 ring is optionally substituted by one to three groups which are the same or different and are independently selected from R3, R7, and R3 71, J2, and J3 are at each occurrence the same or different and are independently -AIQA2-; Q is

Abstract: This invention relates to tetrahydropyranonaphthyridines derivatives having formula (III) or IV: and analogues of the tetrahydropyranonaphthyridines derivatives. The invention also relates to pharmaceutical compositions comprising these compounds and methods for treatment of tuberculosis using these compounds.

Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.

Abstract: Disclosed are fused heterocyclic compounds of Formula (I): or pharmaceutically-acceptable salts or stereoisomers thereof. Also disclosed are methods of using such compounds in the treatment of at least one androgen receptor-associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.

Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.

Abstract: Thiazolo[4,5-c]ring compounds, (e.g. thiazolopyridine, thiazoloquinoline, 6,7,8,9-tetrahydrothiazoloquinoline, thiazolonaphthyridine, and 6,7,8,9-tetrahydrothiazolonaphthyridine compounds) having an oxime or hydroxylamine substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.

Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J3, X, Z, and R1-R4 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

Abstract: Provided is a compound useful as an N-type Ca2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Ca2+ channels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings.

Abstract: Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.

Abstract: Compounds of the formula (I), in which E, R3, R4, R5, X, Y, W, Q1, Q2, Z, s and m have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.

Abstract: The present invention provides for thiazolopyridine-based tricyclic compounds having the formula (I), wherein R1, R2, R5, R6 and R7 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.

Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.

Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to radiolabelled compounds particularly 1-azabicyclo[2.2.2]octane compounds (i.e., quinuclidine compounds) which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express the ?7-nicotinic cholinergic receptor. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express ?7-nicotinic cholinergic receptor to which the compounds of the invention have an affinity.

Abstract: The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A1, A8, R2, R3, R5, R6, R7, and R9 are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa to Xe are each a carbon atom or a nitrogen atom, m is 0 to 2, and ring A to ring C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.

Abstract: The present invention relates to substituted thiazolyl- and oxazoyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.

Abstract: Compounds that are inhibitors of the unfolded protein response and endonuclease IRE1 are provided, together with compositions comprising such compounds, and methods for their use in the treatment of various disorders, such as cancer, autoimmune disorders, and diabetes. Also provided are packaged pharmaceuticals comprising these compositions. The compositions may be administered in combination with another therapeutic agent.

Abstract: Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: The present invention provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.

Abstract: Aryl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.

Abstract: The present invention comprises tetrazoloquinoline-compounds that are inhibitors of HCV. Compositions comprising the compounds in combination with a pharmaceutically acceptable carrier are also disclosed, as are methods of using the compounds and compositions to inhibit HCV infection of a cell, particular in the form of treating HCV infection in a mammal.

Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are provided as well as processes for the manufacture of such compounds. The compounds are useful in the treatment or prevention of inflammatory and allergic diseases.