Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein L1, A1, R1g, z, R2, R3, and R4 are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.

Abstract: The invention relates to a preservative comprising at least one isothiazolone, at least one quaternary ammonium compound, and at least one stabilizer selected from the group of sulphite salts, hydrogen sulphite salts, sulphite-releasing compounds and hydrogen-sulphite-releasing compounds, the presence of algicidal triazine being ruled out. The preservative inhibits the growth of fungi, algae and bacteria on or in alkaline coating compositions. The invention furthermore relates to a process for the preparation of the preservative, to its use in a coating composition, and to the preserved composition.

Abstract: Solid dosage formulations of nitazoxanide or a nitazoxanide analogue are provided that comprise a controlled release portion and an immediate release portion. The pharmaceutical composition is typically in the form of a bilayer solid oral dosage form comprising (a) a first layer comprising a first quantity of nitazoxanide or analogue thereof in a controlled release formulation; and (b) a second layer comprising a second quantity of nitazoxanide or analogue thereof in an immediate release formulation. Method of using the formulations in the treatment of hepatitis C are also provided.

Abstract: The present invention aims to provide a pharmaceutical composition effective for the treatment of cataract. A pharmaceutical composition for the treatment of cataract, containing a VAP-1 inhibitor as an active ingredient, particularly a pharmaceutical composition for the treatment of cataract, containing a compound represented by the formula (I) and the like as an active ingredient: R1—NH—X—Y—Z??(I) wherein each symbol is as defined in the description.

Abstract: One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.

Abstract: The invention relates to a series of thiazoline and oxazoline derivatives, compositions thereof, and methods of treating conditions and disorders using such compounds.

Abstract: The present invention concerns the compounds having the formula (I), N-oxides, salt, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by C1-6alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC1-6alkyl, carboxyl, C3-7cycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, —(R7a)n—M—R7b, Het1 and Het2; whereby the optional substituents on any amino function are independently selected from R5 and —A—R6; and on (ii) a nitrogen atom if present by hydroxy or —A—R6. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them.

Abstract: The invention provides classes of novel compounds that accelerate peptide loading to DR in the absence of DM and related pharmaceutical compositions. The invention also provides conjugates of these compounds with peptides, antigens or other MHC-based therapeutics, including peptides that self-catalyze their loading onto MHC Class II molecules. Methods are provided for modulating an immune response in a subject. Also disclosed are methods of using the novel compounds, e.g., in combination with MHC-based therapeutics, for the treatment of autoimmune diseases and for the manufacture of medicaments. Methods of improving loading of viral peptides and tumor peptides for enhancing the CD4 T cell response following vaccination against viruses or tumors, and related vaccines, are also provided.

Abstract: Compounds of formula (I) as defined herein: inhibit the formation of the ?-amyloid peptide (?-A4) and are, therefore, useful in the treatment of pathologies in which a ?-amyloid peptide (?-A4) formation inhibitor provides a therapeutic benefit. Particular such pathologies are senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy, cerebrovascular disorders, frontotemporal dementias and Pick's disease, post-traumatic dementias, pathologies linked to neuroinflammatory processes, Huntington's disease and Korsakov's syndrome.

Abstract: Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein X1 represents oxygen, etc., X2 represents oxygen, etc., R1 represents a group on Ring A such as alkylsulfonyl, etc., R2 represents C3-7 cyclic alkyl optionally substituted with a halogen, etc., R3 represents a substituent on Ring B such as lower alkyl, etc., formula (II): [Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III): [Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by R3 above, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C?N bond with the nitrogen atom of the ring], as well as their pharmaceutically acceptable salts.

Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and X have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: Disclosed are novel dipeptide analogs compounds of Formula (I), (II) or (III): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, or a prodrug thereof, which are inhibitors of factor XIa and/or plasma kallikrein, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of thrombotic diseases.

Abstract: The invention provides a novel class of compounds, 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 TrkA, TrkB, TrkC, PDGFR and c-kit.

Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.

Abstract: An in vitro method of screening for candidate compounds for the preventive or curative treatment of acne entails determination of the ability of a compound to inhibit the expression or the activity of TACE, and also to the administration of inhibitors of the expression or of the activity of this enzyme, in the treatment of acne.

Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate 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: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.

Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.

Abstract: The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I), where V, W, R1, R2, R3 and R4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Abstract: Compounds of the present disclosure are 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator. Processes of their preparation are also described in the disclosure. The disclosure also describes method to characterize partial glucokinase activators.

Abstract: A method of treating a glial cell related disorder in a mammalian subject includes administering a drug which enhances or prolongs GSK-3 ? or ? inactivation.

Abstract: Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases.

Abstract: The present invention relates to compositions and methods for the treatment of cancer patients with Traf2- and Nck-interacting kinase (TNIK) inhibitors. More particularly, the present invention relates to pharmaceutical compositions comprising TNIK inhibitor and a pharmaceutically acceptable carrier, and to methods for treating the TNIK inhibitor administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. And the present invention relates to a novel aminothiazole derivatives.

Abstract: (Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; R2 is halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group, —COR8, or the like; R3 and R4 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, —COR12, or the like) For example, provided are adenosine A2A receptor antagonists comprising, as the active ingredient, a thiazole derivative represented by a general formula (I), or a pharmaceutically acceptable salt thereof, and the like.

Abstract: The present invention concerns a compound of formula (I), or a pharmaceutically acceptable salt, or solvate thereof, wherein the groups Ri-Rs are defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.

Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.

Abstract: It is intended to provide a novel means of treating and diagnosing cancer by clarifying the participation of glycogen synthase kinase 3? (GSK3?) in the survival and proliferation of cancer mils. Namely, a method of suppressing the survival and proliferation of cancer cells by inhibiting the expression of GSK3? or the activity of the above-described enzyme having been activated by the phosphorylation at the 216th tyrosine residue thereof; and a method of developing a novel anticancer agent and a method of evaluating an anticancer agent based on the inhibitory effect as described above.

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

Abstract: A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, R1 represents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a C3-C6 cycloalkylsulfanyl group, a C3-C6 cycloalkylsulfinyl group, or a C3-C6 cycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).

Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.

Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L1 are defined in the specfication, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a, Rx, and n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

Abstract: The current invention is directed to methods of inducing the negative chemotaxis of a migratory cell comprising contacting the cell with a compound having the Formula (I), (II), (III) or (IV).

Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.

Abstract: The present application relates to cannabinoid receptor ligands of formula (I) wherein X1, A1, Rx, R2, R3, R4, and z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.

Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.

Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.

Abstract: The invention relates to compounds of the formula I A-B-Z ??I wherein the variables are as defined in the claims. The compounds are pro-drugs of A2A-receptor ligands with improved aqueous solubility, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.

Abstract: Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism: X1—Y1-Z1-W1??(I) wherein X1 is optionally substituted aryl, optionally substituted heteroaryl or the like; Y1 is —NRACO—(CH2)0-2— or the like (wherein RA is a hydrogen or the like); Z1 is optionally substituted phenylene or the like; and W1 is a group represented by the below formula: wherein R1, R2, R3, and R4 are each independently a hydrogen atom, optionally substituted lower alkyl or the like, a broken line (---) represents the presence or absence of bond.

Abstract: The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.

Abstract: A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.

Abstract: A method of treating viral infections by the administration of a halogenated benzamide derivative according to formula (III): in which R1 is a halogen atom, and R2-R6 are independently hydrogen, hydroxyl, C1-C4 alkyl, —C1-C4 alkoxy, acyloxy, nitro, halogen, —C(O)R7 where R7 is —C1-C4 alkyl, or, aromatic including salts and hydrates of these compounds.

Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity, including metabolic and inflammatory or immune associated diseases or disorders having the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups, R1, R2, R3, and/or R4, provided that (i) A is not tetrazole or (ii) if A is thienyl or furanyl then Z is selected from a group other than succinimido or thalimido; M is selected from alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl; Ma is a linker between C and M and is selected from a bond and C1-C3alkylene; Q is selected from (i) hydrogen, halogen, nitro, cyano, hydroxy, C1-4alkyl, and substituted C1-4 alkyl; or (ii) Q is combined with R6 and with the carbon atoms to wh

Abstract: Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is A1QA2-; Q is a bond, —C(?O)—, —OC(O)—, —C(?O)NR5—, —SOp—, —SOpNR5—, —C(O)O—, —NR5C(O)—, —OC(O)NR5—, —NR5C(O)O—, —S(O)pNR5C(O)—, —C(O)NR5S(O)p— —NR5S(O)p—, or —NR5C(?O)NR6—. Y is selected from hydrogen, C1-6alkyl, OR16, substituted C1-6alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A1 and A2 are independently selected from a bond, C1-3alkylene, or C1-3alkenylene, and R1-R11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.

Abstract: The present invention is concerned with novel sulfonamides of formula wherein R1, R2, R3, R4, R5, Ar, Ar1, Ar2, n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists that may be useful in the treatment of disorders, in which orexin pathways are involved.