Abstract: Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain.

Abstract: The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent having the property of being selective ligands for the dopamine D3 receptor. These selective D3 ligands are useful as medicines in neuropsychiatry, in particular in the treatment of psychotic or depressive states, or in the treatment of motor disorders, such as dyskinesia or essential tremor. They are furthermore useful in the treatment of dependency on nicotine, cocaine, alcohol, opioids and for facilitating withdrawal in drug-dependent individuals.

Abstract: The present invention relates to compounds of the general formula IC wherein R2, R?, R?, R3, R6, X1 and X1? are as defined herein and pharmaceutically active acid addition salts thereof. Compounds of the invention are useful for the treatment of neurological and neuropsychiatric disorders.

Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, and depression. This invention could also be used for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.

Abstract: Compounds of Formula I wherein R1, A, R2, R3, R4, R5, n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Abstract: The present invention relates to sustained-release tablet formulations of piperazine-piperidine compounds, which can be useful in treating central nervous system disorders; to processes for their preparation; and to methods of using them.

Abstract: The invention provides compositions, pharmaceutical preparations, and methods for modulating angiogenesis and/or cell migration in a subject having a cellular proliferative disease (e.g., cancer), or a disease or condition amenable to treatment by enhancing cellular proliferation and cell migration (e.g., angiogenesis), by modulating the activity of an aquaporin, such as aquaporin-1. The compositions and pharmaceutical preparations of the invention may comprise one or more of compounds that modulate the activity of aquaporin-1.

Abstract: This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.

Abstract: The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.

Abstract: Compounds of the formula: wherein: n is an integer from 1-3; X is N, CH, provided that when X is N, n is 2 or 3; R is alkyl of 1 to 3 carbon atoms; R1 is 2,4-diCl, 5-OMe; 2,4-diCl; 3,4,5-tri-OMe; 2-Cl, 5-OMe; 2-Me, 5-OMe; 2,4-di-Me; 2,4-diMe-5-OMe, 2,4-diCl, 5-OEt; R2 is alkyl of 1 to 2 carbon atoms, and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to controlled-release beads comprising diquinoline-substituted piperazine-piperidine compounds, such as 5-fluoro-8-{4-[4-[(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl}quinoline, or pharmaceutically acceptable salts thereof; to multiple particulate formulations comprising such beads; to methods of preparing such beads; and to methods of treating 5-HT1A-related disorders using such beads and/or multiple particulate formulations.

Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).

Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of a bacterial disease including a mycobacterial disease, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of bacterial diseases and a process for preparing the claimed compounds.

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 novel compounds which are JAK3 Kinase inhibitors, methods for their preparation and pharmaceutical compositions comprising them.

Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma.

Abstract: This invention provides compounds of Formula I, including pharmaceutically acceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

Abstract: The present invention relates to crystalline forms of the 5-HT1A binding agent 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline, as well as pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The invention relates to compounds of formula (I) wherein: either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH—, or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, —NH—, —S—, —CH2— or a direct bond; Z is linked to any one of G1, G2, G3 and G4; n is an integer from 0 to 5; m is an integer from 0 to 3; Ra represents hydrogen or fluoro; Rb, R1 and R2 are defined herein and salt thereof, process for the preparation so such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of a compound of formula I in the manufacture of a medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of diseases states including cancer and rheumatoid arthritis.

Abstract: Disclosed are piperazine bis-amide derivatives useful as antagonists of the orexin receptor and pharmaceutical compositions containing the same.

Abstract: The present invention provides compounds that demonstrate protective effects on target cells from HIV infection in a manner as to bind to chemokine receptor, and which affect the binding of the natural ligand or chemokine to a receptor such as CXCR4 of a target cell.

Abstract: Compounds of formula I in free or salt form, wherein Ar, R1, R2, R3, X and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type IV (PDE4) and are of use in the treatment of inflammatory and/or allergic diseases.

Abstract: The invention pertains to heteroaromatic compounds of the formula I, as defined herein, that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.

Abstract: The present invention provides compounds useful as therapeutic agent for treating glaucoma and methods for treating glaucoma. That is, a therapeutic agent for treating glaucoma containing, as an active ingredient, a compound represented by formula (1) below is synthesized, and the therapeutic agent is administered in the form of eye drops to a glaucoma patient. Thus, the intraocular pressure is reduced. In the above formula, ring A represents a 5- to 11-membered cyclic amino group, which may have a substituted group, and X represents a halogen.

Abstract: The invention provides compounds of formula (I) wherein n, p, q, X, R1, R2, R3, R4, R5 and R6 are as defined in the specification; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine compounds, pharmaceutical compositions containing such substituted 1-propiolylpiperazine compounds, and the use of such substituted 1-propiolylpiperazine compounds for modulating mGluR5 receptor activity or for treating or inhibiting pain and various other conditions, especially conditions at least partly mediated by the mGluR5 receptor.

Abstract: The present invention provides novel salt and hydrate crystal forms of (2R)-anti-5-{3-[4-(10,11-difluoromethano-dibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy}quinoline 2.5 hydrochloride.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression or anxiety, are also disclosed.

Abstract: Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such composition in the treatment and/or prevention of serotonin-related disorders, such as depression and anxiety, are also disclosed. In addition, processes for the preparation of benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives are disclosed.

Abstract: The present invention relates to dopamine D4 ligands having the general formula I wherein R1-R10, W, X, Y1-Y4, and n are as described herein. The compounds of the invention are potent dopamine D4 receptor ligands.

Abstract: An antibacterial formulation suitable for injection into animals containing approximately 2-10% w/v difloxacin HCl, L-arginine base, propylene glycol, ethanol and/or benzyl alcohol, and water. The formulation is a solution having a pH of form 9 to 10. The formulation produces little or no tissue damage or irritation at the injection site.

Abstract: The present invention relates to compounds of the general formula I wherein R1 is the group and R2, R?, R?, R3, R4, R5, R6, R7, X1, X1?, X2, and N are as defined in the specification. Compounds of the invention are useful for the treatment of neurological and neuropsychiatric disorders.

Abstract: Compounds of the general formula (I): wherein R1, R2, R3 and R4 are as described in the specification. Further included are pharmaceutical compositions comprising the compounds, processes for their preparation, as well as the use of the compounds for the preparation of a medicament which particularly acts on the central nervous system, particularly for use as anti-obesity agents.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH2 or oxygen and is a single bond; or X is nitrogen, Y is CH2 and is a single bond; R 1 is halogen, cyano, or C1-6 alkoxy; a is 0,1, 2 or 3 ; b is 0 or 1 ; R 2 is hydrogen, C1-6 alkyl, C1-6 alkanoyl, fluoroC1-6 alkanoyl, C1-6 alkylsulfonyl, fluoroC1-6 alkylsulfonyl, carbamoyl, C1-6 alkylcarbamoyl or arylC1-6 alkyl; and R 3 , together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.

Abstract: Compounds of the formula: wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase.

Abstract: The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (wherein R1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like, R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like, R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, and n: 0 or 1).

Abstract: The invention provides compounds of the general formula: wherein X is selected from the group consisting of oxygen, sulfur and nitrogen-containing groups selected from azine, oxime, hydrazone, aromatic hydrazone, aliphatic hydrazone, semicarbazone, guanidinyl group, and aliphatic or aromatic imines; Y is selected from the group of halogens; R1 and R2 are independently selected from the group consisting of H, lower alkyl group (of C1 up to C6), lower hydroxyalkyl group (of C1 up to C6), lower O-alkyl group (of C1 up to C6), lower alkylcarbonyl group (of C2 up to C6), lower alkyloxycarbonyl group (of C1 up to C6), haloalkylcarbonyl group (of C1 up to C6), or arylsulfonyl group, and their pharmaceutically acceptable salts. The compounds are useful as active ingredients in pharmaceutical compositions. The invention relates to the use of the said compounds as a medicament, in particular as an antibiotic.

Abstract: The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system.

Abstract: This invention relates to compounds of the formula 1 wherein G, D, A, Z, Q, X, Y, R1, and R4 through R7 are defined as in the specification, processes for preparing the same and intermediates used in making the same, and pharmaceutical compositions containing such compounds and their use in the treatment of central nervous system disorders and other disorders.

Abstract: Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system

Abstract: A cyclic diamine compound of formula (1): wherein R1 and R2 are individually a hydrogen atom or a methoxy group, provided R1 is a methoxy group when R2 is a hydrogen atom, or a hydrogen atom when R2 is a methoxy group; A is an oxygen atom, a sulfur atom, CH?CH, CH?N or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; B is a nitrogen atom, CH or CR4, in which R4 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; m is 1 or 2; and n is a number of 1 to 5, an acid-addition salt thereof, or a hydrate thereof. The compound has inhibitory effects on cell adhesion and is useful for treatment of allergy, asthma, rheumatism, arteriosclerosis, and inflammation.

Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useflul in the treatment of diabetes.

Abstract: Selected substituted piperazine compounds of Formula I are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. 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 compounds of the formula 1 wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.

Abstract: The present invention provides piperazinyl phenylethyl amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and B are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said piperazinyl phenylethyl amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain, and anxiety.

Abstract: The invention encompasses a series of benzothiazole compounds which inhibit HIV entry and are useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for using these compounds.

Abstract: Compounds of the following formula: where m, n, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.