TRIAZOLE DERIVATIVE
    1.
    发明申请
    TRIAZOLE DERIVATIVE 审中-公开
    三唑衍生物

    公开(公告)号:US20110269960A1

    公开(公告)日:2011-11-03

    申请号:US13180011

    申请日:2011-07-11

    CPC分类号: C07D249/08

    摘要: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).

    摘要翻译: 本发明的目的是提供具有抑制S1P与其受体Edg-1(S1P1)结合的作用的化合物,可用作药物化合物。 化合物或其药学上可接受的盐,其化合物由下式表示(其中A表示氧原子,硫原子,由式-SO-表示的基团,由式-SO2-表示的基团等) R1表示氢原子,具有1-6个碳原子的烷基等,R1A表示氢原子等,R2表示具有1-6个碳原子的烷基,具有3-6个碳原子的环烷基 原子等,R 3表示芳基,R 4表示氢原子或具有1-6个碳原子并且任选被羧基取代的烷基,R 5表示具有1-10个碳原子的烷基,环烷基 具有3-8个碳原子的基团,任选取代的芳基等)。

    Triazole derivative
    2.
    发明授权
    Triazole derivative 失效
    三唑衍生物

    公开(公告)号:US08022091B2

    公开(公告)日:2011-09-20

    申请号:US12278054

    申请日:2007-02-05

    CPC分类号: C07D249/08

    摘要: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2—, or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, R3 represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-10 carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).

    摘要翻译: 本发明的目的是提供具有抑制S1P与其受体Edg-1(S1P1)结合的作用的化合物,可用作药物化合物。 化合物或其药学上可接受的盐,其化合物由下式表示(其中A表示氧原子,硫原子,由式-SO-表示的基团,由式-SO2-表示的基团等) R1表示氢原子,具有1-6个碳原子的烷基等,R1A表示氢原子等,R2表示具有1-6个碳原子的烷基,具有3-6个碳原子的环烷基 原子等,R 3表示芳基,R 4表示氢原子或具有1-6个碳原子并且任选被羧基取代的烷基,R 5表示具有1-10个碳原子的烷基,环烷基 具有3-8个碳原子的基团,任选取代的芳基等)。

    TRIAZOLE DERIVATIVE
    3.
    发明申请
    TRIAZOLE DERIVATIVE 失效
    三唑衍生物

    公开(公告)号:US20100041655A1

    公开(公告)日:2010-02-18

    申请号:US12278054

    申请日:2007-02-05

    CPC分类号: C07D249/08

    摘要: An object of the present invention is to provide a compound having an action of inhibiting binding between S1P and its receptor, Edg-1 (S1P1), and is useful as a pharmaceutical compound. A compound or a pharmaceutically acceptable salt thereof, which compound is represented by the formula below (where A represents an oxygen atom, a sulfur atom, a group represented by Formula —SO—, a group represented by Formula —SO2— or the like, R1 represents a hydrogen atom, an alkyl group having 1-6 carbon atoms, or the like, R1A represents a hydrogen atom or the like, R2 represents an alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-6 carbon atoms, or the like, represents an aryl group, R4 represents a hydrogen atom or an alkyl group having 1-6 carbon atoms and optionally substituted with a carboxyl group, and R5 represents an alkyl group having 1-carbon atoms, a cycloalkyl group having 3-8 carbon atoms, an aryl group which is optionally substituted, or the like).

    摘要翻译: 本发明的目的是提供具有抑制S1P与其受体Edg-1(S1P1)结合的作用的化合物,可用作药物化合物。 一种化合物或其药学上可接受的盐,该化合物由下式表示(其中A表示氧原子,硫原子,由式-SO-表示的基团,由式-SO2-等表示的基团, R1表示氢原子,具有1-6个碳原子的烷基等,R1A表示氢原子等,R2表示具有1-6个碳原子的烷基,具有3-6个碳原子的环烷基 等表示芳基,R 4表示氢原子或具有1-6个碳原子并且任选被羧基取代的烷基,R 5表示具有1个碳原子的烷基,环烷基具有3个 -8个碳原子,任选取代的芳基等)。

    Triazole derivative
    4.
    发明授权
    Triazole derivative 失效
    三唑衍生物

    公开(公告)号:US08022225B2

    公开(公告)日:2011-09-20

    申请号:US11659103

    申请日:2005-08-04

    IPC分类号: C07D249/12 C07D249/08

    摘要: A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P1), and is useful as a pharmaceutical product. [where A represents a sulfur atom, an oxygen atom, a formula —SO— or a formula —SO2—; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms or the like; R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a phenyl group or the like; R5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and R6 represents an alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group].

    摘要翻译: 由下式(I)表示的化合物或其药学上可接受的盐具有抑制S1P与其受体Edg-1(S1P1)结合的作用,可用作药物。 [其中A表示硫原子,氧原子,式-SO-或式-SO 2 - ; R1表示氢原子,碳原子数1〜6的烷基等; R2表示碳原子数1〜6的烷基,碳原子数3〜8的环烷基等; R3表示氢原子或碳原子数1〜6的烷基。 R4表示氢原子,碳原子数1〜6的烷基,苯基等; R5表示氢原子或碳原子数1〜6的烷基。 R6表示碳原子数1〜6的烷基,苯基或取代苯基]。

    Triazole derivative
    5.
    发明申请
    Triazole derivative 失效
    三唑衍生物

    公开(公告)号:US20090131438A1

    公开(公告)日:2009-05-21

    申请号:US11659103

    申请日:2005-08-04

    摘要: A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P1), and is useful as a pharmaceutical product. [where A represents a sulfur atom, an oxygen atom, a formula —SO— or a formula —SO2—; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms or the like; R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a phenyl group or the like; R5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and R6 represents an alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group].

    摘要翻译: 由下式(I)表示的化合物或其药学上可接受的盐具有抑制S1P与其受体Edg-1(S1P1)结合的作用,可用作药物。 [其中A表示硫原子,氧原子,式-SO-或式-SO 2 - ; R1表示氢原子,碳原子数1〜6的烷基等; R2表示碳原子数1〜6的烷基,碳原子数3〜8的环烷基等; R3表示氢原子或碳原子数1〜6的烷基。 R4表示氢原子,碳原子数1〜6的烷基,苯基等; R5表示氢原子或碳原子数1〜6的烷基。 R6表示碳原子数1〜6的烷基,苯基或取代苯基]。

    Thiazole derivative
    6.
    发明申请
    Thiazole derivative 失效
    噻唑衍生物

    公开(公告)号:US20070154428A1

    公开(公告)日:2007-07-05

    申请号:US10591614

    申请日:2005-03-04

    摘要: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula. The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.

    摘要翻译: 由下式表示的噻唑咪唑衍生物或其药学上可接受的盐,以及ALK5抑制剂,秃发治疗剂或具有上述作为活性成分的毛发生长剂,其中:X 1和X 2 2个彼此不同,表示硫原子或碳原子; R 1表示苯基; 取代的苯基; 与杂芳环稠合的苯基; 吡啶基; 或与杂芳环稠合的吡啶基; R 2表示氢原子,卤素原子,具有1至6个碳原子的烷基,具有1至5个被1至5个卤素原子取代的碳原子的烷基,具有1个 至6个碳原子,具有1至5个碳原子的烷酰基或具有1至6个碳原子的羟烷基,A表示由下式表示的基团。 本发明提供了抗ALK5的抑制物质,其为TGF-β1型受体,并且基于其新的活性提供毛发生长刺激剂或毛发生长剂。

    Thiazole derivative
    7.
    发明授权
    Thiazole derivative 失效
    噻唑衍生物

    公开(公告)号:US07678810B2

    公开(公告)日:2010-03-16

    申请号:US10591614

    申请日:2005-03-04

    摘要: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula. The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.

    摘要翻译: 由下式表示的噻唑咪唑衍生物或其药学上可接受的盐,以及ALK5抑制剂,秃发治疗剂或具有上述作为活性成分的毛发生长剂,其中:X1和X2彼此不同,表示 硫原子或碳原子; R1表示苯基; 取代的苯基; 与杂芳环稠合的苯基; 吡啶基; 或与杂芳环稠合的吡啶基; R2表示氢原子,卤素原子,碳原子数1〜6的烷基,碳原子数1〜5的碳原子数1〜5的烷基,碳原子数1〜6的烷氧基,烷氧基 具有1至5个碳原子,或具有1至6个碳原子的羟烷基,A表示由下式表示的基团。 本发明提供一种抗ALK5抑制物质,其为TGF- I型受体,并且基于其新的活性提供毛发生长兴奋剂或毛发生长剂。

    Aminobenzoic acid derivatives
    9.
    发明授权
    Aminobenzoic acid derivatives 失效
    氨基苯甲酸衍生物

    公开(公告)号:US06720424B1

    公开(公告)日:2004-04-13

    申请号:US10019525

    申请日:2002-01-02

    IPC分类号: C07D21172

    摘要: Aminobenzoic acid derivatives represented by Formula (1) as follows: (wherein, R1 represents a hydrogen atom, a C1-6alkyl group, or the like; R2 represents a hydrogen atom, a C1-6alkyl group, or the like; R3 represents a C8-25alkyl group, or the like; R4 represents a hydrogen atom or a group represented by OR9 or CO2R10 (wherein R9 and R10 represent a hydrogen atom or a C1-6 alkyl group); A represents a group represented by S(O)qR15 (wherein q is 0, 1, or 2, R15 represents a C1-6alkyl group, a phenyl C1-3alkyl group, or a group represented by (CH2)mOR16 (wherein m is 2 or 3, and R16 represents a hydrogen atom or a methoxymethyl group), or the like; X represents O, a single bond, CH═CH, or a group represented by NR27 (wherein R27 represents a hydrogen atom or a t-butoxycarbonyl group); Y represents O, CONH, NHCO, or a group represented by NR28 (wherein R28 represents a hydrogen atom or a t-butoxycarbonyl group); and n is an integer of 0 to 15) or pharmaceutically acceptable salts of the same are employed as VEGF receptor antagonists, and in particular as therapeutic agents for the diseases in which VEGF is involved.

    摘要翻译: 式(1)表示的氨基苯甲酸衍生物如下:(其中,R 1表示氢原子,C 1-6烷基等; R 2表示氢原子,C 1-6烷基或 R 3表示氢原子或由OR 9或CO 2 R 10表示的基团(其中R 9和R 10分别表示碳原子数3〜10的烷基, >表示氢原子或C 1-6烷基); A表示由S(O)q R 15表示的基团(其中q为0,1或2,R 15为C 1-6烷基, 苯基C 1-3烷基或由(CH 2)mOR 16表示的基团(其中m为2或3,R 16表示氢原子或甲氧基甲基)等; X表示O, 单键,CH = CH或由NR 27表示的基团(其中R 27表示氢原子或叔丁氧基羰基); Y表示O,CONH,NHCO或由NR a表示的基团, 28>(其中R 28表示氢原子或叔丁氧基羰基),n为0〜15的整数)或药物 其可接受的盐用作VEGF受体拮抗剂,特别是作为涉及VEGF的疾病的治疗剂。

    System and method of load balancing for ethernet link aggregation
    10.
    发明授权
    System and method of load balancing for ethernet link aggregation 有权
    以太网链路聚合的负载均衡的系统和方法

    公开(公告)号:US09237091B2

    公开(公告)日:2016-01-12

    申请号:US13529371

    申请日:2012-06-21

    摘要: A system and method of transmitting data across a first link aggregation formed by an intermediate switch and a downstream switch, the intermediate switch adopting a Media-Access Card (MAC)-address-based load sharing algorithm for distributing traffic among links to the downstream switch interfaced with a final destination device. The method comprises: receiving a packet having a MAC header and an IP header at an input port of an upstream switch for transmission from the upstream switch to the intermediate switch, the upstream switch and intermediate switch forming a second link aggregation; re-writing, at the upstream switch, the source MAC address of the received packet to a different source address; sending the packet through the second link aggregation to the intermediate switch, the intermediate switch implementing the load sharing algorithm for sending the packet to the downstream switch along a link through the first link aggregation to the destination device.

    摘要翻译: 一种通过中间交换机和下游交换机形成的第一链路聚合发送数据的系统和方法,所述中间交换机采用基于媒体接入卡(MAC)地址的负载分担算法,用于在下游交换机的链路之间分配业务 与最终目的地设备连接。 该方法包括:在上游交换机的输入端口接收具有MAC报头和IP报头的分组,从上游交换机向中间交换机发送,上游交换机和中间交换机形成第二链路聚合; 在上游交换机上重新写入接收到的数据包的源MAC地址到不同的源地址; 将所述分组通过所述第二链路聚合发送到所述中间交换机,所述中间交换机实现负载分担算法,用于通过所述第一链路聚合向所述目的设备沿着链路向所述下游交换机发送所述分组。