Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists

    公开(公告)号:US07915448B2

    公开(公告)日:2011-03-29

    申请号:US12578061

    申请日:2009-10-13

    IPC分类号: C07C311/03 A61K31/18

    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.

    Bearing unit and rotary drive using the same
    33.
    发明授权
    Bearing unit and rotary drive using the same 有权
    轴承单元和旋转驱动使用相同

    公开(公告)号:US07775719B2

    公开(公告)日:2010-08-17

    申请号:US11584606

    申请日:2006-10-23

    IPC分类号: F16C32/06 H02K7/08

    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.

    摘要翻译: 用于可旋转地支撑轴(100)的轴承单元(90)包括具有允许轴穿过并延伸到外部的间隙的无缝保持构件(120),布置在保持构件内部的轴承(130) 为了可旋转地支撑轴以使其可径向旋转,安装在轴上的防轴释放构件(115)以便抵靠轴承,以防止轴在推动方向上滑落, 形成构件(113),其设置在所述保持构件的内部,以便确保所述防轴释放构件周围的空间。 轴承单元还可以包括润滑油密封构件,并且空间形成构件可以用于形成用于润滑油的通道,以防止润滑油泄漏。

    Bearing unit, and motor using same
    36.
    发明授权
    Bearing unit, and motor using same 失效
    轴承单元和电机使用相同

    公开(公告)号:US07073946B2

    公开(公告)日:2006-07-11

    申请号:US11185896

    申请日:2005-07-21

    IPC分类号: F16C32/06

    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.

    摘要翻译: 提供了一种轴承单元,其包括:轴(51),用于支撑可旋转的径向轴承(55)以沿周向支撑轴(51);止推轴承(66),用于在推动方向上支撑轴(51);以及 具有径向轴承(55)的壳体(56)和设置在其中的止推轴承(66),并且其中填充有粘性流体(57)。 壳体56除了形成在其中的轴插入孔65之外还具有密封结构,轴51被引入。 在轴(51)的外表面和轴插入孔(65)的内表面之间限定有足够宽度的间隙(69),以防止填充在壳体(56)中的粘性流体(57) 从后者泄漏出来。 壳体(56)通过模制合成树脂形成为一体式结构。

    Bearing unit, and motor using same
    37.
    发明授权
    Bearing unit, and motor using same 失效
    轴承单元和电机使用相同

    公开(公告)号:US07029179B2

    公开(公告)日:2006-04-18

    申请号:US10450851

    申请日:2002-10-18

    IPC分类号: F16C17/10

    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.

    摘要翻译: 提供了一个可旋转地支撑轴(51)的轴承单元。 它包括轴(51),用于沿周向支撑轴(51)的径向轴承(55),用于在轴的一个推力方向端支撑轴(51)的推力轴承(58),壳体 56),其中设置有径向轴承(55)和支撑在一起的轴(51)并且填充有粘性流体(67)的推力轴承(58),以及设置在壳体(56)内部的间隔件(65) 以在径向轴承(55)的端面和包括在轴(51)中的径向突起(54)的一侧之间保持间隙。 在与径向突起(54)的一侧相对的径向切口(55)的端面上形成有第一动态压力产生凹部(63),其通过粘性流体产生动态压力。 此外,在与径向突起(54)的另一侧相对的止推轴承(58)侧,形成有由粘性流体产生动态压力的第二动压产生凹部(64)。 当轴(51)旋转时,粘性流体通过第一和第二动压产生凹槽(63,64)循环,以分别在轴与径向和推力轴承之间产生动态压力。 如上所述设置的空间部件65能够高精度地分别控制径向突起54和第一动力产生凹部(63,64)之间的间隙。

    Bearing unit, and motor using same
    38.
    发明申请
    Bearing unit, and motor using same 失效
    轴承单元和电机使用相同

    公开(公告)号:US20050265641A1

    公开(公告)日:2005-12-01

    申请号:US11185896

    申请日:2005-07-21

    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.

    摘要翻译: 提供了一种轴承单元,其包括:轴(51),用于支撑可旋转的径向轴承(55)以沿周向支撑轴(51);止推轴承(66),以沿轴向方向支撑轴(51);以及 具有径向轴承(55)的壳体(56)和设置在其中的止推轴承(66),并且其中填充有粘性流体(57)。 壳体56除了形成在其中的轴插入孔65之外还具有密封结构,轴51被引入。 在轴(51)的外表面和轴插入孔(65)的内表面之间限定有足够宽度的间隙(69),以防止填充在壳体(56)中的粘性流体(57) 从后者泄漏出来。 壳体(56)通过模制合成树脂形成为一体式结构。

    Substituted benzylaminopiperidine compounds
    40.
    发明授权
    Substituted benzylaminopiperidine compounds 失效
    取代的苄基氨基哌啶化合物

    公开(公告)号:US06329396B1

    公开(公告)日:2001-12-11

    申请号:US09562144

    申请日:2000-05-01

    IPC分类号: C07D21156

    CPC分类号: C07D211/56

    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.

    摘要翻译: 本发明提供了可用于治疗胃肠道疾病的取代的苄基氨基哌啶化合物; 中枢神经系统(CNS)疾病; 炎性疾病; 呕吐 尿失禁 疼痛; 偏头痛 晒斑; 由幽门螺杆菌引起的疾病,病症和不良状况; 或血管生成,特别是在哺乳动物受试者,特别是人类中的CNS紊乱。