Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.

Abstract: The present invention provides BACE inhibitors of Formula I: methods for their use, intermediates, and methods for their preparation.

Abstract: The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.

Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT*, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS or combinations thereof.

Abstract: The invention relates to antibacterial compounds of formula I wherein one or two of U, V, W, and X represent N, the rest represent CH or, in the case of X, may also represent CRa wherein Ra is fluorine; R1 represents alkoxy, halogen or cyano; R2 represents H, CH2OH, CH2N3, CH2NH2, alkylcarbonylaminomethyl or triazol-1-ylmethyl; R3 represents H, or, when n is 1, R3 may also represent OH, NH2, NHCOR6 or triazol-1-yl; A represents CR4; K represents O, NH, OCH2, NHCO, NHCH2, CH2NH, CH2CH2, CH?CH, CHOHCHOH or CHR5; R4 represents H or together with R5 forms a bond, or also R4 can represent OH when K is not O, NH, OCH2 or NHCO; R5 represents OH or together with R4 forms a bond; R6 represents alkyl; m is 0 or 1 and n is 0 or 1; and G is as defined in the description; and to salts of such compounds.

Abstract: Disclosed are benzothiazin derivatives of formula (I), preparation methods therefore, and treatment methods employing such compounds as antibacterial agents in treating infectious diseases of mammals caused by bacteria, especially diseases like tuberculosis and leprosy caused by mycobacteria: wherein R1, R2, R3, R4, R5, and R6, and other variables enumerated under one or more of R1, R2, R3, R4, R5, and R6 are as defined.

Abstract: The invention relates to antibacterial compounds of formula I wherein n is 0 or 1; R1 represents H or F; U represents CH2 or, provided n is 1, O or NH; “-----” is a bond or is absent; V represents CH or N when “-----” is a bond, or CH2 or NH when “-----” is absent; W represents CH or N; A represents —(CH—)p—NH—(CH2)q— wherein p is 1 and q is 1 or 2 or, provided U represents CH2 and n is 1, p may also be 0 and q is then 2; G represents one of the groups wherein Z represents N or CH and Q represents O or S; and Z0, Z1 and Z2 each represent CH, or Z0 and Z1 each represent CH and Z2 represents N, or Z0 represents CH, Z1 represents N and Z2 represents CH or N, or Z0 represents N and Z1 and Z2 each represent CH; and to salts of such compounds.

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

Abstract: The invention relates to compounds of Formula (I) wherein U, V, W, R1, R1b, A and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament for the prevention or treatment of a bacterial infection.

Abstract: The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.

Abstract: The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferable pharmaceutically acceptable salts, thereof, in which R, R1, R2, R3, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.

Abstract: A PLG copolymer material, termed a PLG(p) copolymer material, adapted for use in a controlled release formulation for a bioactive material is provided, wherein the formulation exhibits a reduced “initial burst” effect when introduced into the tissue of a patient in need thereof. A method of preparation of the PLG copolymer material is also provided, as are methods of use.

Abstract: The present invention relates to compounds of Formula (I) or salts thereof wherein R?, R2, R3, R4, R5, R6, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.

Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: Disclosed are compounds of Formulae 1 and 1a, N-oxides, and salts thereof, wherein R1, R1a, Y, and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Further disclosed is a method for preparing compounds of Formula 1 from compounds of Formula 1a.

Abstract: The invention relates to antibiotic ethanol or 1,2-ethanediol cyclohexyl derivatives of formula (I) wherein R1 represents (C1-C4)alkoxy; one or two of U, V, W and X represents) N and the remaining represent each independently CH or, in the case of V or X, may also represent CRa; Ra represents halogen; R2 represents H or OH; A represents CH2, CO, CH2CH?CH or COCH?CH; D represents a phenyl group optionally substituted one or two times by halogen atoms, or D represents a group of the formula (II) in which Q is oxygen or sulphur; and to salts of these derivatives of formula (I).

Abstract: The present invention is directed to methods for screening for metallohydrolase inhibitors using metal binding moieties in combination with targeting moieties.

Abstract: Bicyclic nitrogen containing compounds and their use as antibacterials.

Abstract: Compounds of formula (I) or formula (II) have anti-inflammatory activity and comprise a new class of NSAIDs. The compounds are useful for treating inflammatory diseases or disorders. The invention also provides pharmaceutical compositions containing these compounds, as well as methods of treating inflammatory diseases or disorders using compounds of formula (III) or formula (IV).

Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.

Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor.

Abstract: The present invention encompasses compounds of general Formula (1) wherein R2, R3, Q, W, X, Y and Z are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.

Abstract: The present invention relates to a pharmaceutical composition in a form of suspension for oral administration comprising valsartan or its pharmaceutically acceptable salts and at least one or two or more of the components selected from glycerol or syrup or the mixture thereof, a preservative, a buffer system and a suspending/stabilizing agent. The present invention further relates to the therapeutic uses of the pharmaceutical composition.

Abstract: The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition.

Abstract: The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.

Abstract: The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.

Abstract: The invention relates to novel N-heterocyclylphenyl-substituted cyclic ketoenols of the formula (I) in which CKE, W, X, Y and Z are as defined in the disclosure, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides. The invention further relates to selective herbicidal compositions comprising firstly the N-heterocyclylphenyl-substituted cyclic ketoenols and secondly a compound which improves crop plant tolerance.

Abstract: Amidine, thiourea and guanidine derivatives of appropriately substituted 2-aminobenzothiazoles, 2-amino-3,1-4H-benzothiazines and 3-amino-1,4-3H-benzothiazines, as understood from formula (I), the related pharmaceutically acceptable salts and solvates thereof: and the use of the products and the corresponding pharmaceutical formulations for the treatment of neurodegenerative pathologies such as cerebral ischemia, neurodegeneration induced by cranial trauma, Alzheimer's disease, Multiple Sclerosis and Amyotrophic Lateral Sclerosis.

Abstract: Tricyclic nitrogen-containing compounds of Formula (I) or pharmaceutically acceptable salts, solvates or N-oxides thereof: compositions containing them, their use in the treatment of tuberculosis, and methods for the preparation of such compounds.

Abstract: Naphthyridine and quinoline derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.

Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with hydroxysteroid dehydrogenases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.

Abstract: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.

Abstract: Antibacterial compounds including 3-amino-6-(1-amino-ethyl)-tetrahydropyran derivatives are provided, and methods of treatment or prevention of bacterial infection with such compounds are provided.

Abstract: The present invention provides pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also provided are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.

Abstract: In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as ?2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the ?2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.

Abstract: Non-peptidic renin inhibitors nitroderivatives of general formula (I): A1-(Xa—ONO2)j ??(I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndrome.

Abstract: [Problem] To provide a pharmaceutical, particularly a compound which can be used as an insulin secretion promoter or a preventive or therapeutic agent for diabetes mellitus and the like diseases in which GPR40 is concerned. [Means for resolution] It was found that novel carboxylic acid derivatives or salts thereof, characterized in that carboxylic acid is linked to a 6-membered monocyclic aromatic ring via two atoms and said aromatic ring is linked to a nitrogen-containing bicyclic ring via a linker, have excellent GPR40 receptor agonist action. In addition, since the carboxylic acid derivatives of the invention showed excellent insulin secretion promoting action and blood glucose reducing action, they are useful as an insulin secretion promoter and a preventive or therapeutic agent for diabetes mellitus.

Abstract: The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases.

Abstract: The present invention relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, to their use in the treatment of bacterial infections, and to their methods of preparation.

Abstract: The present invention is directed to substituted benzodiazepinones, benzoxazepinones and benzothiazepinones compounds that are sodium channel blockers useful for the treatment of chronic and neuropathic pain. The compounds of the present invention are also useful for the treatment of other conditions, including disorders of the CNS such as anxiety, depression, epilepsy, manic depression and bipolar disorder. This invention also provides pharmaceutical compositions comprising a compound of the present invention, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. This invention further comprises methods for the treatment of acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain and disorders of the CNS including, but not limited to, epilepsy, manic depression, depression, anxiety and bipolar disorder comprising administering the compounds and pharmaceutical compositions of the present invention.

Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials. Z1 and Z2 are independently selected from CH and N.

Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CRa, Ra being halogen, and, in the case of W, may also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH, or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, provided R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent(s) CRC and the remaining each represent CH, Rb being alkoxy, alkoxycarbonyl or alkoxyalkoxy and Rc being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are seleted from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to salts of

Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.

Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor.

Abstract: The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.

Abstract: The present invention relates to diaryl pyrimidine-2,4-diamines, pharmaceutical compositions thereof, and the use of the compounds and compositions for the inhibition of kinases. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.

Abstract: The invention relates to inhibitors of FtsZ polymerization and uses thereof.

Abstract: Naphthyridine and related derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.

Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.

Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.