COMPOUND HAVING TAFIA INHIBITORY ACTIVITY
    1.
    发明申请
    COMPOUND HAVING TAFIA INHIBITORY ACTIVITY 审中-公开
    具有TAFIA抑制活性的化合物

    公开(公告)号:US20110213143A1

    公开(公告)日:2011-09-01

    申请号:US13126685

    申请日:2009-10-28

    CPC分类号: C07D471/04 C07D487/04

    摘要: Provided are compounds having superior TAFIa inhibitory activity. Specifically, there are provided compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: wherein A is a benzene ring or a pyridine ring; X is the formula —(CH2)—, the formula —(CH2)2—, an oxygen atom, a nitrogen atom or a single bond; Y is the formula —(CH2)3—NH—R3, the formula —(CH2)4—NH—R3 or a 2-aminopyridyl group; R3 is a hydrogen atom, a C1-6 alkyl group, or the formula —CO2R4; R4 is a C1-6 alkyl group, the formula —CHR5OC(O)R6, or a substituent having the structure represented by the following formula Ia; R5 is a C1-6 alkyl group; R6 is a C1-6 alkyl group, a C3-8 cycloalkyl group, or a phenyl group; R7 is a C1-6 alkyl group or a phenyl group; R1 is a hydrogen atom, a halogen atom, a C1-4 alkyl group substituted by 1-3 halogen atoms, a C1-10 alkyl group, a C1-8 alkoxy group, a C3-8 cycloalkyl group, a C3-8 cycloalkoxy group, a C4-14 cycloalkylalkyl group, or a phenyl group; R2 is CO2R8, or a tetrazolyl group; R8 is a hydrogen atom, a C1-10 alkyl group, or a substituent having the structure represented by the following formula Ib or Ic; m and n are each an integer of zero or one.

    摘要翻译: 提供具有优异TAFIa抑制活性的化合物。 具体地,提供由下式(I)表示的化合物或其药学上可接受的盐:其中A是苯环或吡啶环; X是式 - (CH 2) - ,式 - (CH 2)2 - ,氧原子,氮原子或单键; Y是式 - (CH2)3-NH-R3,式 - (CH2)4-NH-R3或2-氨基吡啶基; R 3是氢原子,C 1-6烷基或式-CO 2 R 4; R4是C1-6烷基,式-CHR5OC(O)R6或具有由下式Ia表示的结构的取代基; R5是C1-6烷基; R6是C1-6烷基,C3-8环烷基或苯基; R7是C1-6烷基或苯基; R1是氢原子,卤素原子,被1-3个卤素原子取代的C1-4烷基,C1-10烷基,C1-8烷氧基,C3-8环烷基,C3-8环烷氧基 基团,C4-14环烷基烷基或苯基; R2是CO2R8或四唑基; R8是氢原子,C1-10烷基或具有由下式Ib或Ic表示的结构的取代基; m和n分别为0或1的整数。

    COMPOUNDS HAVING TAFIa INHIBITORY ACTIVITY
    2.
    发明申请
    COMPOUNDS HAVING TAFIa INHIBITORY ACTIVITY 审中-公开
    具有TAFIA抑制活性的化合物

    公开(公告)号:US20120172598A1

    公开(公告)日:2012-07-05

    申请号:US13496625

    申请日:2010-09-17

    IPC分类号: C07D471/04

    CPC分类号: C07D471/04 A61K31/4745

    摘要: The present invention provides compounds having superior TAFIa inhibitory activity. They are dihydroimidazoquinoline compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: wherein R is a hydrogen atom or a C1-10 alkyl group; R1 is a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group or a substituent having the structure represented by the following formula Ia or Ib: where R3 is a C1-6 alkyl group; R4 is a C1-6 alkyl group, a C3-8 cycloalkyl group, or a benzyl group; and R2 is a hydrogen atom or a substituent having the structure represented by the following formula Ic or Id:

    摘要翻译: 本发明提供具有优异TAFIa抑制活性的化合物。 它们是由下式(I)表示的二氢咪唑并喹啉化合物或其药学上可接受的盐:其中R是氢原子或C1-10烷基; R1是氢原子,C1-10烷基,C3-8环烷基或具有由下式Ia或Ib表示的结构的取代基:其中R3是C1-6烷基; R4是C1-6烷基,C3-8环烷基或苄基; 并且R 2是氢原子或具有由下式Ic或Id表示的结构的取代基:

    Core structure of heat exchanger
    3.
    发明授权
    Core structure of heat exchanger 失效
    热交换器的核心结构

    公开(公告)号:US07007745B2

    公开(公告)日:2006-03-07

    申请号:US10809484

    申请日:2004-03-26

    IPC分类号: F28F9/04

    摘要: In a core structure of a heat exchanger, tubes and corrugated fins are alternately arranged between seat plates arranged opposite to each other with a predetermined space interposed therebetween. End portions of the tubes are inserted into tube holes formed respectively in each of the top and bottom seat plates to be fixed. On the seat plates, there are provided connection portions having wall portions slanting from main body portions thereof toward the tube holes. When a thickness of the tubes is 0.13 mm to 0.23 mm, a slant angle θ of the wall portions of the connection portions is set to satisfy: slant angle θ (°)≧25χ(thickness (mm) of sheet plate)+(−125χ(thickness (mm) of tube)+25).

    摘要翻译: 在热交换器的芯结构中,管和波纹翅片交替地布置在彼此相对布置的间隔开的预定间隔的座板之间。 管的端部插入分别形成在每个顶板和底座板中的管孔中,以固定。 在座板上设有连接部分,其连接部分具有从其主体部分向管孔倾斜的壁部分。 当管的厚度为0.13mm至0.23mm时,连接部的壁部的倾斜角θ设定为:倾斜角θ(°)> = 25chi(板的厚度(mm))+( -125chi(管的厚度(mm))+25)。

    Core structure of heat exchanger
    4.
    发明授权
    Core structure of heat exchanger 有权
    热交换器的核心结构

    公开(公告)号:US06932152B2

    公开(公告)日:2005-08-23

    申请号:US10806321

    申请日:2004-03-23

    IPC分类号: B21D28/24 F28F9/02 F28F9/18

    摘要: In a core structure of a heat exchanger, tubes and corrugated fins are alternately arranged between seat plates arranged opposite to each other with a predetermined space interposed therebetween. Both end portions of the tubes are inserted into tube holes of connection portions formed respectively in each of the top and bottom seat plates to be fixed. On the seat plates, there are provided connection portions on which are formed wall portions slanting from main body portions thereof toward the tubes and vulnerable portions formed thinner than the seat plates and in series on the wall portions and absorb thermal stress of the seat plates against the tubes by bending.

    摘要翻译: 在热交换器的芯结构中,管和波纹翅片交替地布置在彼此相对布置的间隔开的预定间隔的座板之间。 管的两端部插入分别形成在每个顶板和底座板中的连接部分的管孔中,以固定。 在座板上设有连接部分,其上形成有从其主体部分朝向管子倾斜的壁部分,并且脆弱部分形成为比座板更薄并且串联在壁部上并且吸收座板的热应力抵抗 管弯曲。

    Method for implementation of power calculation on a fixed-point processor using table lookup and linear approximation
    5.
    发明授权
    Method for implementation of power calculation on a fixed-point processor using table lookup and linear approximation 失效
    使用表查找和线性近似在定点处理器上实现功率计算的方法

    公开(公告)号:US06779015B1

    公开(公告)日:2004-08-17

    申请号:US09722086

    申请日:2000-11-24

    IPC分类号: G06F738

    CPC分类号: G06F7/556

    摘要: A method for calculating the power of an integer raised to a constant real number. The method may be used to process digital signals, which are encoded in such a fashion as to require such processing. An embodiment of the present invention first receives a segment of a bitstream. Next, the process determines whether an integer value of the segment is within a look-up table. The look-up table contains a list of integers and a corresponding list of the integers raised to the power of a real number. If the integer value is within the look-up table, the process indexes the look-up table with the integer value to determine substantially the value of the integer raised to the real power. If, however, the integer value is not within the look-up table, the process indexes the table with a plurality of integers which are within the table to approximate the value of the segment from the bitstream raised to the real power. The process repeats these steps for each segment in the signal bitstream.

    摘要翻译: 一种用于计算整数增加到恒定实数的幂的方法。 该方法可以用于处理数字信号,这些信号以需要这种处理的方式进行编码。 本发明的实施例首先接收比特流的片段。 接下来,该处理确定片段的整数值是否在查找表内。 查找表包含整数列表和相应的整数列表,提供给实数的幂。 如果整数值在查找表中,则该进程将使用整数值对查找表进行索引,以确定实际提供给实际功率的整数的值。 然而,如果整数值不在查找表内,则该过程用表内的多个整数对该表进行索引,以将该段的值从比特流提升到实际功率。 该过程对信号比特流中的每个段重复这些步骤。

    Pyripyropene derivative having ACAT2 inhibiting activity and stable to metabolizing enzymes
    6.
    发明授权
    Pyripyropene derivative having ACAT2 inhibiting activity and stable to metabolizing enzymes 有权
    具有ACAT2抑制活性并且对代谢酶稳定的吡哆醛衍生物

    公开(公告)号:US09187492B2

    公开(公告)日:2015-11-17

    申请号:US13638332

    申请日:2011-03-25

    摘要: A compound effective in prevention and treatment of arteriosclerosis with a mechanism different from that of statin drugs has the following formula or a pharmaceutically acceptable salt, solvate, or hydrate thereof: wherein R1 is an aliphatic, alicyclic, or aromatic acyloxy group, or a group of the formula —O—CH(R7)—R8 where R7 is a lower alkoxy group and R8 is an aryl group, and R2 is carboxyl, a lower alkoxycarbonyl group, or an arylmethylcarbamoyl group, or a —CH2-acyloxy group and R3 is an aliphatic, alicyclic or aromatic acyloxy group, provided that at least one of R4 and R3 is a group other than acetoxy, or R2 and R3 taken together form a group of the formula —O—CH(R5)—O— where R5 is an aryl group.

    摘要翻译: 具有与他汀类药物不同的机制预防和治疗动脉硬化的化合物具有下式或其药学上可接受的盐,溶剂合物或水合物:其中R1是脂族,脂环族或芳族酰氧基或基团 的式-O-CH(R7)-R8,其中R7是低级烷氧基,R8是芳基,R2是羧基,低级烷氧基羰基或芳基甲基氨基甲酰基,或-CH2-酰氧基和R3 是脂族,脂环族或芳香族酰氧基,条件是R 4和R 3中的至少一个是除乙酰氧基以外的基团,或者R 2和R 3一起形成式-O-CH(R 5)-O-基团,其中R 5 是芳基。

    Pyripyropene Derivative Having ACAT2 Inhibiting Activity and Stable to Metabolizing Enzymes
    7.
    发明申请
    Pyripyropene Derivative Having ACAT2 Inhibiting Activity and Stable to Metabolizing Enzymes 有权
    具有ACAT2抑制活性和稳定代谢酶的吡哆醛衍生物

    公开(公告)号:US20130085163A1

    公开(公告)日:2013-04-04

    申请号:US13638332

    申请日:2011-03-25

    IPC分类号: C07D493/14 C07D493/04

    摘要: A compound effective in prevention and treatment of arteriosclerosis with a mechanism different from that of statin drugs has the following formula or a pharmaceutically acceptable salt, solvate, or hydrate thereof: wherein R1 is an aliphatic, alicyclic, or aromatic acyloxy group, or a group of the formula —13—O—CH(R7)—R8 where R7 is a lower alkoxy group and R8 is an aryl group, and R2 is carboxyl, a lower alkoxycarbonyl group, or an arylmethylcarbamoyl group, or a —CH2-acyloxy group and R3 is an aliphatic, alicyclic or aromatic acyloxy group, provided that at least one of R4 and R3 is a group other than acetoxy, or R2 and R3 taken together form a group of the formula —O—CH(R5)—O— where R5 is an aryl group.

    摘要翻译: 具有与他汀类药物不同的机制预防和治疗动脉硬化的化合物具有下式或其药学上可接受的盐,溶剂化物或水合物:其中R1是脂族,脂环族或芳族酰氧基或基团 的式-13-O-CH(R7)-R8,其中R7是低级烷氧基,R8是芳基,R2是羧基,低级烷氧基羰基或芳基甲基氨基甲酰基或-CH2-酰氧基 并且R 3是脂族,脂环族或芳族酰氧基,条件是R 4和R 3中的至少一个是除乙酰氧基以外的基团,或者R 2和R 3一起形成式-O-CH(R 5)-O- 其中R5是芳基。