摘要:
The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m— and —(CH2)n— respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR3R4, —SO2NR3R4, —(CH2)pNR3R4, —(CH2)pNR3COR4, optionally substituted aryl ring, optionally substituted heteroaryl ring, a fused bicyclic heteroaromatic ring system or optionally substituted heterocyclyl ring; Ar1 represents optionally substituted heteroaryl ring; Ar2 represents optionally substituted aryl ring or optionally substituted heteroaryl ring; Z represents —(CH2)qX— wherein the —(CH2)q— group is attached to Ar2, or —X(CH2)q— wherein X is attached to Ar2, and wherein any of the —CH2— groups may be optionally substituted by one or more C1-6alkyl groups; X represents oxygen, —CH(OR5)—, —NR5— or —CH2— wherein the —CH2— group may be optionally substituted by one or more C1-6alkyl groups; R3 and R4 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; R5 represents hydrogen or C1-6alkyl; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; q independently represents an integer selected from 0, 1, 2 and 3; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that when Ar1 is a pyridyl group, and Z is —CH2X— where X is attached to the Ar1 group, X is selected from —CH(OR5)—, —NR5— and —CH2— wherein the —CH2— group may be optionally substituted by one or more C1-6alkyl groups. The compounds of formula (I) are useful in therapy, in particular as antipsychotic agents.
摘要:
The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m—and —(CH2)n-respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8—(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl; R3 represents hydrogen or C1-6alkyl; R4 represents optionally substituted aryl or optionally substituted heteroaryl; R5 and R6each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pOC3-6cycloalkyl, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8, —(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl; R7 and R8 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; and either: Z represents —CR9R10X— or —XCR9R10— and X represents oxygen, sulfur, —SO— or —SO2, or Z represents —CONR11— or —NR9CO— and X represents —CH2—, oxygen, sulfur, —SO— or —SO2; R9 and R10 each independently represent hydrogen, C1-6alkyl or fluoro; R11 represents hydrogen or C1-6alkyl; or a pharmaceutically acceptable salt or solvate thereof. The compounds of the invention are useful in therapy, in particular as antipsychotic agents.
摘要:
The invention provides compounds of formula (I) wherein A and B represent the groups CH2)m— and CH2)n— respectively; R1 represents hydrogen or C1-4alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pC3-6cycloalkyloxy, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S-C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8, —(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; R3 represents hydrogen or C1-6alkyl; R4 represents halogen, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl or —(CH2)pC3-6cycloalkyloxy; R5 and R6 each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pC3-6cycloalkyloxy, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, —(CH2)pNR7R8, —(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; R7 and R8 each independently represent hydrogen or C1-6alkyl; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that the compounds 4-methyl-N-(1,2,3,4-tetrahydroisoquinolin-6-yl)-benzenesulfonamide, 7-(4-chlorophenyl)sulfonamido-1,2,3,4-tetrahydroisoquinoline hydrochloride and N-(2-ethyl-5-isoindolinyl)-p-toluenesulfonamide are excluded. The compounds are useful in therapy, in particular as antipsychotic agents.
摘要:
The invention provides compounds of formula (I) wherein A and B represent the groups —(CH2)m- and —(CH2)n-respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C3-7cycloalkylC1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pC3-6cycloalkyloxy, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, C1-6alkylsulfonyloxy, C1-6alkylsulfonylC1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, C1-6alkylsulfonamido, C1-6alkylsulfonamidoC1-6alkyl, —(CH2)pNR7R8, C1-6alkylamidoC1-6alkyl, —(CH2)pNR7COR8, arylsulfonyl, arylsulfonyloxy, arylsulfonylC1-6alkyl, arylsulfonamido, arylcarboxamido, arylsulfonamidoC1-6alkyl, arylcarboxamidoC1-6alkyl, aroyl, aroylC1-6alkyl, arylC1-6alkanoyl, —SO2NR7R8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl, or a group CONR7R8 or SO2NR7R8 wherein R7 and R8 together may be fused to form a 5- 7-membered aromatic or non-aromatic heterocyclic ring optionally interrupted by an O or S atom; R3 represents hydrogen or C1-6alkyl; Ar represents optionally substituted phenyl or optionally substituted monocyclic heteroaryl group; R4 represents optionally substituted aryl or optionally substituted heteroaryl; R7 and R8 each independently represent hydrogen, C1-6alkyl or together form a 5- to 7-membered heterocyclic ring; Z represents a bond, an oxygen atom or C1-6alkyl; Y represents hydrogen or C1-6alkyl; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; q represents an integer from 1 to 3; r represents an integer from 1 to 4; or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful in therapy, in particular as antipsychotic agents.
摘要:
Compounds of formula (I) and salts and solvates are provided: wherein R4 is fluoro, R5 is selected from hydrogen, halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C1-6alkoxy, and C1-6alkoxy substituted with one or more fluorine atoms; and R6 is selected from halogen, cyano, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6alkoxy and C1-6alkoxy substituted with one or more fluorine atoms, and Q is hydrogen or C1-6alkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
摘要:
The invention provides a method of handover from an active network to a selected one of a plurality of potential other networks. In addition to the overall solution, the solution proposed has several individual aspects. All subsidiary aspects are related to the common problem mentioned above and sharing the underlying common solution concept of implementing a system in which selective handover is possible and in which a list of available other networks provided by an active network can be handled and selection made by a terminal, so that neighbor cell information can be transmitted based on expressed terminal preferences.
摘要:
An accessory rack for mounting on a vehicle is described. In an embodiment, the accessory rack includes an anchor that mounts to the frame and a stand that is supported by the anchor so as to provide a strong yet compact accessory rack. The small size provides potential benefits in the reduction of fuel consumption and/or reductions in wind noise in the event the user does not remove the accessory rack from the vehicle during periods of disuse. The accessory rack may include a stand configured to support standard sized carriers while providing improved ergonomics during installation of objects onto the carrier.
摘要:
The present invention relates to a naturally-occurring growth hormone mutation; to a method for detecting it and its use in screening patients for growth hormone dysfunction or for producing variant proteins suitable for treating such irregularities.
摘要:
The present invention is directed to a lubricating oil composition, a diesel engine comprising a lubricating oil composition, and a method of lubricating a diesel engine provided with an exhaust gas recirculation system, comprising lubricating said engine with a lubricating oil composition comprising an oil of lubricating viscosity, and a polymeric N-dispersant booster comprising monomer units of: a) 0 to 40 wt. % of one or more ethylenically unsaturated ester compounds of formula (I) wherein R is equal to H or CH3, R1 represents a linear or branched alkyl group with 1 to 5 carbon atoms, R2 and R3 independently represent H or a group of the formula —COOR′, wherein R′ is H or an alkyl group with 1 to 5 carbon atoms, b) 10 to 98 wt. % of one or more ethylenically unsaturated ester compounds of formula (II) wherein R is equal to H or CH3, R4 represents a linear or branched alkyl group with 6 to 15 carbon atoms, R5 and R6 independently represent H or a group of the formula —COOR″, wherein R″ is H or an alkyl group with 6 to 15 carbon atoms, c) 0 to 30 wt. % of one or more ethylenically unsaturated ester compounds of formula (III) wherein R is equal to H or CH3, R7 represents a linear or branched alkyl group with 16 to 30 carbon atoms, R8 and R9 independently represent H or a group of the formula —COOR′″, wherein R′″ is H or an alkyl group with 16 to 30 carbon atoms, d) 0 to 30 wt. % vinyl monomers, e) 7 to 25 wt. % of at least one N— dispersant monomer, wherein a)-e) add up to 100 wt. %.
摘要:
A method for control of packet data transmissions in a TDMA wireless network to provide for additional choices in the allocation of communication channels. Measurement and recovery periods are re-assigned to avoid conflicts in operating conditions. The re-assignments for the GPRS system may be reduced to a simple formula.