Abstract: There is provided a FAAH inhibitor and a prophylactic or therapeutic agent for cerebrovascular disorders or sleep disorders comprising it. The prophylactic or therapeutic agent comprises a compound of the formula (I0): wherein Z is oxygen or sulfur; R1 is aryl which may be substituted, or a heterocyclic group which may be substituted; R1a is a hydrogen atom, a hydrocarbon group which may be substituted, hydroxyl, etc.; R2 is piperidin-1,4-diyl which may be substituted, or piperazin-1,4-diyl which may be substituted; R3 is a group formed by eliminating two hydrogen atoms from a 5-membered aromatic heterocyclic group having 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur, which may be further substituted, —CO—, etc.; and R4 is a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; or a salt thereof.

Abstract: A preventive, therapeutic or improving agent for diseases against which activation of the thrombopoietin receptor is effective or a platelet increasing agent, which contains a thrombopoietin receptor activator represented by the formula (1): [wherein each of R1 and R3 is independently a hydrogen atom, SO3H, a C1-6 alkyl group, a C1-6 alkylcarbonyl group or a C6-18 arylcarbonyl group (the C1-6 alkyl group, the C1-6 alkylcarbonyl group and the C6-18 arylcarbonyl group may be optionally substituted with a halogen atom, a hydroxyl group, a C2-6 alkenyl group, a C1-6 alkoxy group, a C1-6 alkoxycarbonyl group, a C6-18 aryl group, a 2-pyridyl group, a 3-pyridyl group, a 4-pyridyl group, a 2-furanyl group, a 3-furanyl group, a 2-thienyl group, a 3-thienyl group or NR9R10) , and each of R2, R4 and Ra is independently a hydrogen atom, a hydroxyl group or a C1-6 alkoxy group].

Abstract: Morphologically stabilized amorphous aripiprazole and process for preparing the same.

Abstract: A patient suffering from an endobronchial infection is treated by administering to the patient for inhalation a dose of less than about 4.0 ml of a nebulized aerosol formulation comprising from about 60 to about 200 mg/ml of an aminoglycoside antibiotic, such as tobramycin, in a physiologically acceptable carrier in a time period of less than about 10 minutes. Unit dose devices for storage and delivery of the aminoglycoside antibiotic formulations are also provided.

Abstract: Diaza heterocyclic sulfonamide derivatives according to formula I have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R7, R8, R9, R10, R11, R12, R13, X, Y1, Y2, m, and n are set forth in the description.

Abstract: A process for preparing phenyl iso(thio)cyanates of the formula I in which a compound of the formula II or its HCl adduct is reacted with a phosgenating agent where W is oxygen or sulfur and Ar and A are as defined in claim 1 is described. Moreover, the invention relates to the use of the phenyl iso(thio)cyanates for preparing crop protection agents.

Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.

Abstract: A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group whic

Abstract: The invention provides new and useful analogs of 4-amino-thalidomide. These analogs include S(?)-4-amino-thalidomide and R(+)-4-amino-thalidomide. The invention also provides processes for making these analogs. Further, the invention provides methods for inhibiting angiogenesis and treating angiogenesis-associated diseases, including cancer and macular degeneration, by administering these compounds.

Abstract: The invention relates to a method of deriving a peptidomimetic of a biologically active metallopeptide, wherein the peptidomimetic includes at least one non-peptide ring structure defining a template space superimposable on a corresponding defined template space of the metallopeptide, and where the peptidomimetic further includes at least two elements independently including an amino acid residue, amino acid side chain moiety or derivative thereof, the elements defining and occupying a similar descriptor space as corresponding elements of the metallopeptide. The invention further relates to peptidomimetics with a template space heterocyclic ring structure, including 5-, 6- and 8-membered and 5-5- and 6-5-bicyclic fused ring structure melanocortin receptor-specific peptidomimetics.

Abstract: Morphologically stabilized amorphous aripiprazole and process for preparing the same.

Abstract: There is provided a process for efficiently producing an anti form of an optically active ?-hydroxy-?-aminocarboxylic acid derivative that is useful as an intermediate for pharmaceuticals and agrochemicals. The process for producing optically active ?-hydroxy-?-aminocarboxylic acid derivative of formula (2) or (3) wherein R1 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, R2 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, characterized by comprising subjecting an ?-aminoacyl acetic acid ester compound of formula (1) wherein R1 and R2 have the same meaning as the above, to hydrogenation by catalytic asymmetric hydrogenation in the presence of an acid.

Abstract: Compounds of Formula I and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.

Abstract: Thiol ester compositions, methods of making the thiol ester compositions, and methods of using the thiol ester compositions are provided. In some embodiments, the thiol ester compositions include thiol esters, hydroxy thiol esters and cross-linked thiol esters. The thiol ester composition can be used to produce cross-linked thiol esters, sulfonic acid-containing esters, sulfonate containing esters and thioacrylate containing esters. The thiol ester compositions can be used to produce polythiourethanes. The polythiourethanes can be used in fertilizers and fertilizer coatings.

Abstract: The present invention relates to a process for purification of novel polymorphic form of Gatifloxacin which comprises dissolving Gatifloxacin in about 15-50 volumes of methanol, removing insolubles if any, adding organic base to the solution, maintaining the solution at temperature of 30° C. to 70° C., for about 20 min to 4 hrs, followed by gradual cooling and maintaining the reaction mass to ?10 to 20° C. for about 1-4 hrs, isolation and drying at temperature of about 45° C. to 65° C.

Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S.

Abstract: Perfluorocarbons are used to control nitric oxide metabolism, either to inhibit nitric oxide activity or to potentiate the effects of nitric oxide. Perfluorocarbons can be used, for example, to treat hypotension and vasoplegia in septic shock, to protect against myocardial ischemia-reperfusion injury, to treat hypertension, and to provide antiplatelet effects.

Abstract: A new pharmaceutical compound for treating central nervous disorders, the compound comprising a therapeutically effective amount of valproic acid or pharmaceutically acceptable derivative thereof covalently bonded to myo-inositol. The invention also provides a composition, method for treating a patient and a method for obtaining the compound.

Abstract: An alkylene carbonate and an alkanol are subjected to transesterification to yield a dialkyl carbonate and alkanediol in a process comprising (a) introducing the alkylene carbonate and an alkanol feedstock into a reaction zone to react in the presence of a transesterification catalyst to yield an alkanediol-rich stream and a stream comprising dialkyl carbonate and alkanol, which streams are separated; (b) passing the stream comprising dialkyl carbonate and alkanol to an extractive distillation zone in which an extractant is added to the stream; (c) obtaining from the extractive distillation zone an alkanol-rich vapor stream and a bottom stream containing the extractant and the dialkyl carbonate; (d) separating the bottom stream from step (c) in a second non-extractive distillation zone to yield a dialkyl carbonate-rich top stream and a extractant-rich bottom stream; and (e) at least partly recycling the extractant-rich bottom stream to the extractive distillation zone, wherein the extractant-rich bottom str

Abstract: The present invention relates to piperazinone compounds, pharmaceutical compositions containing those compounds and methods of treating tumors and cancer, among other disease states and conditions in mammalian patients, especially including humans.