摘要:
The present invention provides compounds of formula (I), wherein both p's are one or two, R1 is generally heteroaryl or cycloalkyl, R2 is C3-6cycloalkyl or phenyl and R3 is heteroaryl, and pharmaceutically acceptable salts thereof, as GlyT1 inhibitors for treating schizophrenia, pharmaceutical compositions comprising the same and methods for their preparation.
摘要:
Compounds, pharmaceutical compositions, kits and methods are provided for use with histone deacetylases (HDACs) that comprise a compound of the formulae: wherein the variables are as defined herein.
摘要:
Compounds that may be used to inhibit histone deacetylase having the formula Z-Q-L-M or Z-L-M wherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0-10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.
摘要:
A class of 3-phenylimidazo[1,2-α]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译:一类3-苯基咪唑并[1,2-a]嘧啶衍生物,其在苯环的间位被被氧原子或-NH-键直接连接或桥连的任选取代的芳基或杂芳基取代, 并且在苯环上被烷基,三氟甲基,烷氧基或一个或两个卤原子,特别是氟取代,是GABA A A受体的选择性配体,特别是对α2和/或α3具有良好的亲和力 和/或其α5亚基,因此有益于治疗和/或预防中枢神经系统的不良状况,包括焦虑,抽搐和认知障碍。
摘要:
A class of 3-phenylimidazo(1,2-a)pyrimidine derivatives (of Formula I, or salt or prodrug thereof: I) wherein Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, CO2Ra, —CONRaRb or —CRa═NORb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group.), substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, are selective ligands for GABAA receptors, in particular having good affinity for the a2 and/or a3 and/or a5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要:
An image processing device and method for modifying images on an image processing device including a scanner configured to produce an image of at least one document having multiple pages, a communications interface configured to connect the image processing device to a server via a network, a display unit configured to display a preview image or a thumbnail image of at least one of the pages of the scanned document and a user interface configured to display a selectable graphical indicia corresponding to at least one operation for modifying the preview image or the at least one image of the scanned document.
摘要:
The apparatus and methods disclosed herein implement a convenient and efficient web-browser based search-and-retrieve mechanism that incorporates a more responsive search engine coupled with an integrated collection display. The browser-based search-and-retrieve mechanism allows a user to quickly and easily retrieve a list of search items from a large database, select certain desired items, while continually having access to a visual interface displaying the collection of previously selected items. While viewing the collection of previously selected items, the search engine interface allows for the retrieval and selection of additional items from the database. In the most preferred embodiments of the present invention, the browser-based search-and-retrieve mechanism takes the form of a shopping cart with enhanced search capabilities for optimized online shopping websites. By utilizing a master index and one or more helper indices, the required search and retrieval time for selecting items from large databases can be minimized.
摘要:
The present invention provides a compound of formula I, or an N-oxide thereof or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy;X2 represents hydrogen or halogen;Z represents hydrogen, halogen, cyano, cyanomethyl, trifluoromethyl, nitro, hydroxy, hydroxy(C1-6)alkyl, C1-6 alkoxy, C1-6 alkoxy(C1-6)alkyl, trifluoromethoxy, trifluoromethylthio, trifluoromethanesulfinyl, formyl, C2-6 alkoxycarbonyl, oxopyrrolidinyl, or an optionally substituted aryl, heteroaryl or heteroaryl(C1-6)alkoxy group; andR1 represents aryl or heteroaryl, either of which groups may be optionally substituted;pharmaceutical compositions comprising it, its use in therapy and methods of treatment of anxiety and/or depression using it.
摘要:
A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, being selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要:
The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.