Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.

Abstract: Disclosed is a method for treating a symptom of M. tuberculosis infection in a subject, comprising administering the patient with an effective amount of (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)zetidin-2-one (EZETIMIBE). In the preferred embodiments, EZETIMIBE is capable of significantly inhibiting the survival and proliferation of Mycobacterium tuberculosis in the monocytes. The anti-tuberculous effect of EZETIMIBE is partly through stimulating CD13 leading to monocytes activation and thus bacterial killing of Mycobacterium tuberculosis, and partly through depleting the intracellular nutrition necessary for the survival of Mycobacterium tuberculosis. It is also proved that EZETIMIBE is capable of directly killing Mycobacterium tuberculosis outside cells.

Abstract: The present invention relates to a process for preparing polyisocyanates by oligomerization of isocyanates.

Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.

Abstract: Provided are compounds of Formula I, R1-L1-A-L2-R2??(I), and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein A, L1, L2, R1 and R2 are defined herein. The present invention also provides a pharmaceutical composition and methods of using such compounds. The compounds are useful for therapy and/or prophylaxis in a patient, and in particular to inhibitors of Soluble Epoxide Hydrolase (sEH).

Abstract: Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria.

Abstract: The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Pharmaceutical compositions of the invention include sulfamide derivatives having a disease-modifying action in the treatment of diseases associated with excitotoxicity and accompanying oxidative stress that include epilepsy, Alzheimer's disease, and any neurodegenerative disease involving glutamate toxicity.

Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.

Abstract: This invention relates to the hydrochloride salt of 5-[3-{3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenyl-hexanamide or derived form thereof and its use as a medicament.

Abstract: The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.

Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.

Abstract: The present invention relates to compounds of Formula (I) that are have activity as S1P1 receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.

Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (I) and its therapeutic use.

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.

Abstract: The invention relates to the use of specific pyridines as catalysts for the dimerization of isocyanates (uretdione formation) and a process for preparing polyisocyanates having a high content of uretdione groups.

Abstract: An alkyl ether derivative represented by the general formula: wherein each of R1 and R2 represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 is an alkylamino group, an amino group, a hydroxyl group or the like; the ring A is a 5-membered or 6-membered heteroaromatic ring or a benzene ring; each of m and n is an integer of 1 to 6; and p is an integer of 1 to 3, or its salt has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.

Abstract: Compositions comprising anti-fibrotic agent(s) and/or polymeric compositions can be used in various medical applications including the prevention of surgical adhesions, treatment of inflammatory arthritis, treatment of scars and keloids, the treatment of vascular disease, and the prevention of cartilage loss.

Abstract: Disclosed is an agent comprising a benzothiophene alkyl ether derivative represented by the general formula below or a salt thereof: wherein R1 and R2 independently represent at least one group selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, an amino group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 represents an alkylamino group which may be substituted or an amino or hydroxyl group which may be protected; and m and n independently represent an integer ranging from 1 to 6. The agent is useful as a neurogenesis inducer or a therapeutic agent for neuropathy.

Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).

Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.

Abstract: The invention relates to a novel method for the synthesis of N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5 -difluorophenyl)methylsulfonamide.

Abstract: The present invention relates to novel 3-phenyl-azetidine derivatives, useful for modulating extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders. In other aspects the invention relates to pharmaceutical compositions comprising the 3-phenyl-azetidine derivatives of the invention and to the use of these compounds for therapeutic applications.

Abstract: The invention relates to a process for preparing polyisocyanates having a high uretdione group content by phosphine-catalysed isocyanate oligomerization in the presence of organic carbonates and/or nitriles.

Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

Abstract: The present invention relates to novel 3-phenyl-azetidine derivatives, useful for modulating dopamine neurotransmission and extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders. In other aspects the invention relates to pharmaceutical compositions comprising the 3-phenyl-azetidine derivatives of the invention and to the use of these compounds for therapeutic applications. X is OH; R1 is F or Cl; R2 is H, F or Cl; and R3 is n-Pr, i-Pr, n-Bu, i-Bu, s-Bu or t-Bu.

Abstract: A low viscosity polyisocyanate composition containing at least one isocyanate dimer having a uretidinedione unit is prepared from a reaction medium containing at least one isocyanate monomer in which the isocyanate groups are borne by sp3 carbon atoms. The reaction medium is heated, in the absence of a dimerization catalyst, to a temperature of at least 50° C. and not more than 200° C. for a period of not more than 24 hours.

Abstract: The invention relates to a process for the preparation of liquid, storage-stable isocyanate mixtures which are characterized by a low color number and which contain carbodiimide (CD) and/or uretonimine (UI) groups. This invention also relates to the isocyanate mixtures obtained by this process, to their use for the preparation of blends with further isocyanates, and to the preparation of prepolymers containing isocyanate groups and of polyurethane plastics, preferably polyurethane foams from these isocyanate mixtures.

Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract: Certain biphenyl compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.

Abstract: The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.

Abstract: The invention relates to heterosubstituted N-thiolated beta-lactams, compositions comprising these compounds, methods for their production, and methods of use as antibiotics to inhibit the growth of bacteria. In one embodiment, the compounds have the structure shown in formula (A) or formula (B) or formula (C): wherein the R groups are as defined in the specification. The antibacterial agents of the invention can be administered to a human or animal to treat or inhibit bacterial infection, such as that of Staphylococcus species, including methicillin-resistant Staphylococcus aureus (MRSA).

Abstract: A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula: wherein X1 represents a halogen atom, is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.

Abstract: Disclosed is a benzothiophene oxide derivative represented by the general formula (wherein R1 and R2 are the same or different and each represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkenyl group, an amino group, a heterocyclic group, an amino group, a hydroxyl group, a carboxyl group, an oxo group and the like; R3 represents an alkylamino group, an amino group, a hydroxyl group or the like; and m and n are the same or different and each represents an integer of 1-6) or a salt thereof, which is useful as a prodrug of a benzothiophene derivative or a salt thereof.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.

Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/ or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.

Abstract: The present invention relates to a process for making 6-substituted-1-(2H)-isoquinolinone derivatives of formula (I) wherein R1 and n are as described in the specification. The present invention further relates to novel intermediates which are used in the process according to the invention and to processes for preparing such intermediates.

Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.

Abstract: The invention relates to a process for the preparation of liquid, storage-stable isocyanate mixtures of low color number containing carbodiimide (CD) and/or uretonimine (UI) groups, the isocyanate mixtures obtainable by this process and the use thereof for the preparation of blends with further isocyanates and for the preparation of prepolymers containing isocyanate groups and of polyurethane plastics, preferably polyurethane foams.

Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.

Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

Abstract: There is provided a compound of formula (I) wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically-acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g., thrombosis) or as anticoagulants.

Abstract: A method produces a uretonimine-modified isocyanate composition having increased low-temperature tolerance. The method comprises providing a first polyisocyanate composition having two or more isocyanate groups and comprising 4,4?-diphenylmethane diisocyanate (MDI) and reacting the first polyisocyanate composition at a temperature of from about 90° C. to about 115° C. and in the presence of a catalyst such that the isocyanate groups form carbodiimides for forming uretonimine and uretonimine oligomers. The reaction of the first polyisocyanate composition is quenched with a quenching agent to produce an intermediate composition having an intermediate isocyanate value of from about 21.0 to about 26.0. The intermediate composition is blended with a second isocyanate composition to form a stable uretonimine-modified isocyanate composition.

Abstract: The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.

Abstract: A modified release pharmaceutical composition comprising, as active ingredient, a compound of formula (I), wherein R1 represents C1-2 alkyl substituted by one or more fluoro substituents; R2 represents hydrogen, hydroxy, methoxy or ethoxy, and n represents 0, 1 or 2; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable diluent or carrier; provided that the formulation may only contain iota-carageenan and a neutral gelling polymer when the compound of formula (I) is in the form of a salt; such formulations being of use for the treatment of a cardiovascular disorder.

Abstract: The present invention relates to pyrazine substituted pyrrolopyridines which are inhibitors of JAK kinases (JAK1, JAK2, JAK3 and/or TYK2) and/or PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer.

Abstract: An alkyl ether represented by the general formula: or its salt. This compound has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.