Abstract: Compounds of formula (1) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)-Q.

Abstract: The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor.

Abstract: Compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds in the treatment of cancer.

Abstract: Substituted heteroaromatic carboxamide and urea compounds corresponding to formula (i) processes for the preparation thereof, pharmaceutical compositions containing these compounds and also a method of using these compounds in pharmaceutical compositions for treating or inhibiting pain and other conditions mediated at least in part via the vanilloid receptor 1.

Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.

Abstract: A compound depicted by the formula below, or a pharmaceutically acceptable salt or solvate thereof. wherein, R1 represents (1) a C3-6 alkyl group, (2) a C1-6 alkyl group substituted with one or more substituent group(s) selected from those consisting a halogen atom, etc., (3) a C3-10 non-aromatic cyclic hydrocarbon group or a 5- to 6-membered non-aromatic heterocyclic group which respectively is optionally substituted with one or more substituent group(s) selected from those consisting an oxo group, etc., (4) an aromatic cyclic hydrocarbon group substituted with one or more substituent selected from the group consisting halogen atom and C1-4 alkoxy group; X represents NH, O, or S; Y represents CH or N; Z represents N or a C—R2; R2 represents (1) hydrogen atom, (2) a C1-6 alkyl group, a C2-6 alkenyl group or a C2-6 alkynyl group that respectively is optionally substituted with one or more substituent group(s) selected from among those consisting (a) a halogen atom, etc.

Abstract: The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases.

Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.

Abstract: The present invention provides, in part, compounds and compositions including a thiazole moiety, that may be useful, for example, for treating cancers, for example kidney cancer.

Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.

Abstract: The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonus spp., Acenetobacter spp., Mvraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotynebacterium, Bacillus spp., Enterobactericeae (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.

Abstract: A new class of alkylsulfinyl thiazolides is described. These compounds show strong activity against hepatitis viruses.

Abstract: The present invention relates to compounds capable of inhibiting and/or decreasing the activity of one or more cathepsins, thereby treating and/or preventing various disease states associated with one or more cysteine proteases including, but not limited to, cathepsins and papain-like cysteine proteases. Disease states treated and/or prevented by the compounds of the invention include, but are not limited to, mammalian parasitic diseases in which the parasite utilizes a critical cysteine protease from the papain family. Examples of parasitic diseases to be treated or prevented by the compounds of the invention include, but are not limited to, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, coccidiosis, giardiosis, cryptosporidiosis or schistosomiasis.

Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.

Abstract: The present invention relates to oxazolidinone derivatives of formula (I) wherein Y, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.

Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group while the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.

Abstract: The present disclosure provides a compound of general formula A useful as potential anti-tubercular agents.

Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.

Abstract: The present invention concerns methods for the production of pharmaceutical formulations of Epothilones suitable for being administered parenterally, such as intravenously.

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds of the following formula, wherein -A and —B are as defined herein (collectively referred to herein as 38TM compounds): The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.

Abstract: Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.

Abstract: This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such.

Abstract: The present invention provides compounds represented by the formula (Ie): and the formula (If): wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.

Abstract: Disclosed are methods of reducing serum glucose and triglyceride levels and for inhibiting angiogenesis, the methods comprising administration of substituted indolealkanoic acids to patients in need of such treatment. Also disclosed are such compounds useful in the treatment of angiogenesis, hyperglycemia, hyperlipidemia and chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds.

Abstract: The present invention provides a method for treating early morning akinesia, comprising continuous administration to a patient in need of such treatment a therapeutically effective amount of a dopamine agonist or a pharmaceutically acceptable salt, enantiomer, solvate, hydrate, polymorph or prodrug thereof.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.

Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.

Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.

Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.

Abstract: Physically and chemically stable aqueous suspensions of riluzole are disclosed together with the manufacturing methods thereof. Such aqueous suspensions comprise riluzole in particle form and at least a wetting agent, preferably a surfactant. Riluzole is in amounts from about 0.1% to about 20% w/v and has an average particle size lower than 200 ?m; such suspensions are devoid of the known local (mouth) anaesthetic effects of riluzole.

Abstract: The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.

Abstract: Compounds of formula (I) in free or salt or solvate form, wherein T has the meaning as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.

Abstract: The present invention relates to novel active compound combinations comprising, firstly, at least one known compound of the formula (I) in which R1 and A have the meanings given in the description and, secondly, at least one further known active compound from groups (2) to (27) listed in the description, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids and also phytopathogenic fungi.

Abstract: The present invention has an object to provide a novel agent for anti-neurodegenerative diseases and solves the object by providing an agent for anti-neurodegenerative diseases containing, as an effective ingredient, the compound(s) represented by the following General formula 1: wherein in General formula 1, R1 through R3 independently represent a hydrogen atom or an appropriate substituent; Z1 represents a heterocyclic ring and Z2 represents the same or different heterocyclic or aromatic ring as in Z1, wherein the heterocyclic and aromatic rings optionally have a substituent; represents an integer of 0, 1 or 2; p represents an integer of 0 or 1, with the proviso that p is 1 when o is 0 or 2, and p is 0 when o is 1; R1 and R2 do not exist when o is 0, while, when p is 0, R3 does not exist and the binding between the carbon atom to which R2 binds and Z2 is a single bond; X1? represents an appropriate counter anion and q represents an integer of 1 or 2.

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); Xa and Xb are each C, N, O or S; Xc and Xd are each C or N; m is 0-2; n is 1-3; ring A is a 5-membered ring optionally having substituent(s); ring B is a 6-membered ring optionally having substituent(s); and ring C is a 3- to 5-membered ring optionally having substituent(s), provided that when Xa, Xc and Xd are each C, then Xb is N or 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 methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R1, R2, R6, and R7 are defined herein.

Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.

Abstract: The present invention provides methods, compositions, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step methods using luminogenic molecules, e.g. luciferin or coelenterazines, that are cytochrome P450 substrates and that are also bioluminescent enzyme, e.g., luciferase, pro-substrates are provided. Upon addition of the luciferin derivative or other luminogenic molecule into a P450 reaction, the P450 enzyme metabolizes the molecule into a bioluminescent enzyme substrate, e.g., luciferin and/or luciferin derivative metabolite, in a P450 reaction. The resulting metabolite(s) serves as a substrate of the bioluminescent enzyme, e.g., luciferase, in a second light-generating reaction. Luminescent cytochrome P450 assays with low background signals and high sensitivity are disclosed and isoform selectivity is demonstrated.

Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).

Abstract: An oral once-daily pramipexole formulation, comprising an immediate-release component and a controlled-release component, is provided wherein in preferred embodiments, both the immediate-release component and the controlled-release component comprise pramipexole The formulation is preferably in the form of a coated bead A method of manufacturing said formulation is also provided.

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.

Abstract: Indole derivatives and analogous compounds and pharmaceutical compositions comprising the same are provided. Also provided are methods of using these compounds to inhibit tubulin polymerization in a cell associated with a proliferative disease or to treat cancer, metastatic cancer, resistant cancer or multidrug resistant cancer, including inter-alia: prostate cancer, breast cancer, melanoma, colon cancer and bladder cancer.

Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.

Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.