摘要:
The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.
摘要:
This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6) alkyl, halo(C1-C6) alkyl, hydroxy(C1-C6) alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6)alkyl]NH—, [(C1-C6)alkyl]2N—, H2N—(C1-C6)alkoxy, (C1-C6)alkyl-NH—(C1-C6)alkoxy, [(C1-C6)alkyl]2N(C1-C6)alkoxy; H2N—(C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkyl-NH—(C1-C6)alkoxy-(C1-C6)alkyl, [(C1-C6)alkyl]2N(C1-C6)alkoxy-(C1-C6)alkyl or 5- or 6- membered heterocyclic ring containing at least one nitrogen atom; R8 represents halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, halo(C1-C6)alkylsulfonyl, halo(C1-C6)alkylsulfinyl, halo(C1-C6)alkoxy, halo(C1-C6)alkylthio, [(C1-C6)alkyl]NH— or [(C1-C6)alkyl]2N—; or R7 and R8, when E is CR9, are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy and hydroxy(C1-C6)alkyl; and R12 represents hydrogen, halogen, (C1-C6)alkyl or hydroxy(C1-C6)alkyl; or a pharmaceutically acceptable salt or solvate thereof.
摘要:
A bearing unit (90) for rotatably supporting a shaft (100) comprises a seamless holding member (120) with a gap allowing a shaft to run through and extend to the outside, a bearing (130) arranged in the inside of the holding member to rotatably support the shaft so as to make it radially revolvable, an anti-shaft-release member (115) fitted to the shaft so as to abut the bearing in order to prevent the shaft from slipping away in the thrusting direction and a space-forming member (113) arranged in the inside of the holding member so as to secure a space around the anti-shaft-release member. A bearing unit may further comprise an lubricating oil seal member and the space-forming member may be used to form a passage way for lubricating oil to prevent lubricating oil from leaking.
摘要:
Compounds of the general formula (I): pharmaceutical compositions comprising a compound of general formula (I); and methods of treating disease conditions caused by overactivation of the VR1 receptor by administering a compound of general formula (I) to a subject.
摘要:
A bearing unit (90) for rotatably supporting a shaft (100) comprises a seamless holding member (120) with a gap allowing a shaft to run through and extend to the outside, a bearing (130) arranged in the inside of the holding member to rotatably support the shaft so as to make it radially revolvable, an anti-shaft-release member (115) fitted to the shaft so as to abut the bearing in order to prevent the shaft from slipping away in the thrusting direction and a space-forming member (113) arranged in the inside of the holding member so as to secure a space around the anti-shaft-release member. A bearing unit may further comprise an lubricating oil seal member and the space-forming member may be used to form a passage way for lubricating oil to prevent lubricating oil from leaking.
摘要:
A bearing unit is provided which includes a shaft (51) to support rotatably, radial bearing (55) to support the shaft (51) circumferentially, a thrust bearing (66) to support the shaft (51) in the direction of thrusting, and a housing (56) having the radial bearing (55) and thrust bearing (66) disposed therein and in which a viscous fluid (57) is filled. The housing (56) has a sealed structure except for a shaft insertion hole (65) formed therein and through which the shaft 51 is introduced. Between the outer surface of the shaft (51) and the inner surface of the shaft insertion hole (65), there is defined a gap (69) having a sufficient width to prevent the viscous fluid (57) filled in the housing (56) from leaking out of the latter. The housing (56) is formed as a one-piece structure by molding a synthetic resin.
摘要:
A bearing unit is provided which supports a shaft (51) rotatably. It includes the shaft (51), a radial bearing (55) to support the shaft (51) circumferentially, a thrust bearing (58) to support the shaft (51) at one of thrusting-directional ends of the latter, a housing (56) having disposed therein the radial bearing (55) and thrust bearing (58) supporting together the shaft (51) and which is filled with a viscous fluid (67), and a spacer member (65) disposed inside the housing (56) to keep a gap defined between the end face of the radial bearing (55) and one side of a radial projection (54) included in the shaft (51). On the end face of the radial breading (55) opposite to one side of the radial projection (54), there is formed a first dynamic pressure producing recess (63) which produces a dynamic pressure by the viscous fluid. Also, on the side of the thrust bearing (58) opposite to the other side of the radial projection (54), there is formed a second dynamic pressure producing recess (64) which produces a dynamic pressure by the viscous fluid. As the shaft (51) rotates, the viscous fluid is circulated through the first and second dynamic pressure producing recesses (63, 64) to produce a dynamic pressure between the shaft and the radial and thrust bearings, respectively. The space member (65) provided as above permits to control the gap between the radial projection (54) and first and second dynamic pressure producing recesses (63, 64), respectively, with a high accuracy.
摘要:
A bearing unit is provided which includes a shaft (51) to support rotatably, radial bearing (55) to support the shaft (51) circumferentially, a thrust bearing (66) to support the shaft (51) in the direction of thrusting, and a housing (56) having the radial bearing (55) and thrust bearing (66) disposed therein and in which a viscous fluid (57) is filled. The housing (56) has a sealed structure except for a shaft insertion hole (65) formed therein and through which the shaft 51 is introduced. Between the outer surface of the shaft (51) and the inner surface of the shaft insertion hole (65), there is defined a gap (69) having a sufficient width to prevent the viscous fluid (57) filled in the housing (56) from leaking out of the latter. The housing (56) is formed as a one-piece structure by molding a synthetic resin.
摘要:
A bearing unit comprises a shaft, a radial bearing for supporting the shaft in a peripheral rotation direction of the shaft, a thrust bearing supporting an end of the shaft in a thrust direction of the shaft, a housing made of a molded body of a synthetic resin, inside of which housing the radial bearing and the thrust bearing are arranged, the housing having a sealed configuration except for a shaft insertion hole, through which the shaft is inserted, a slip-out preventing member provided on an end side of the radial bearing at which the thrust bearing is provided, the slip-out preventing member preventing the shaft from slipping out from the radial bearing, and a viscous fluid filled in the housing. The slip-out preventing member is made of a material having a thermal deformation temperature higher than a temperature applied to the slip-out preventing member upon molding of the housing.
摘要:
The invention provides a substituted benzylaminopiperidine compounds that are useful in the treatment of gastrointestinal disorders; central nervous system (CNS) disorders; inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by Heliobacter pylori; or angiogenesis, especially CNS disorders in a mammalian subject, especially in humans.