&OHgr;-amino-&agr;-hydroxycarboxylic acid derivatives having integrin &agr;&ngr;&bgr;3 antagonistic activity
    1.
    发明授权
    &OHgr;-amino-&agr;-hydroxycarboxylic acid derivatives having integrin &agr;&ngr;&bgr;3 antagonistic activity 失效
    具有整合素α2β3拮抗活性的ω-氨基-α-羟基羧酸衍生物

    公开(公告)号:US06750219B1

    公开(公告)日:2004-06-15

    申请号:US10048914

    申请日:2002-02-05

    IPC分类号: C07D40304

    CPC分类号: C07D239/42

    摘要: An objective of the present invention is to provide highly water-soluble compounds having integrin &agr;v&bgr;3 antagonistic activity. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts or solvates thereof: wherein A represents a two nitrogen atom-containing optionally substituted saturated or unsaturated five- to seven-membered heterocyclic group, which is optionally condensed with another carbocyclic ring or heterocyclic ring to form a bicyclic group, or —C(—NR1R2)(═NR3) wherein R1, R2, and R3 represent hydrogen, alkyl or the like; D represents a bond, >NR4, wherein R4 represents hydrogen or optionally substituted alkyl, —O—, or —S—; X and Z represent either CH or N; R7 and R8 represent C1-6 alkyl, halogen, oxygen or the like; Q represents >C═O, >CHR13 or >CHOR13 wherein R13 represents hydrogen or alkyl; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene having 1 to 3 carbon atoms; R10 and R11 represent hydrogen, alkyl or the like; m is an integer of 0 to 5; n is an integer of 0 to 4; and p and q are an integer of 1 to 3.

    摘要翻译: 本发明的目的是提供具有整合素α2拮抗活性的高水溶性化合物。 根据本发明的化合物是由式(I)表示的化合物及其药学上可接受的盐或溶剂化物:其中A表示两个含有氮原子的任选取代的饱和或不饱和的五至七元杂环基,其任选地稠合 与另一个碳环或杂环形成双环基团,或-C(-NR 1 R 2)(= NR 3)(其中R 1,R 2和R 3) 代表氢,烷基等; D表示键,NR 4,其中R 4表示氢或任选取代的烷基,-O-或-S-; X和Z表示CH或N; R 7和R 8表示C 1-6烷基,卤素,氧等; Q表示C = O,> CHR 13或CHOR 13,其中R 13表示氢或烷基; R 9表示氢,烷基等; J表示碳原子数1〜3的键或亚烷基。 R 10和R 11代表氢,烷基等; m为0〜5的整数。 n为0〜4的整数。 p和q为1〜3的整数。

    M-substituted benzoic acid derivatives having integrin alpha v beta 3 antagonistic activity
    2.
    发明申请
    M-substituted benzoic acid derivatives having integrin alpha v beta 3 antagonistic activity 审中-公开
    具有整合素αvβ3拮抗活性的M取代苯甲酸衍生物

    公开(公告)号:US20050059669A1

    公开(公告)日:2005-03-17

    申请号:US10944712

    申请日:2004-09-21

    摘要: An object of the present invention is to provide m-substituted benzoic acid derivatives having integrin αvβ3 antagonistic activity. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof, which are useful for the treatment or prevention of cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases, cancers and metastasis thereof, immunological diseases, osteopathy and other diseases: wherein A represents an optionally substituted heterocyclic group containing two nitrogen atoms, a bicylic group or the like; D represents a bond, >NR4, >CR5R6, O, S, or —NR4—CR5R6—; X represents CH or N; R7 and R8 represent hydroxyl, alkyl or the like; Q represents >C═O or the like; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene; R10 represents optionally substituted hydroxyl, amino or the like; R11 represents hydrogen, alkyl or the like; m is 0 to 5; n is 0 to 4; and p and q are each 0 to 3.

    摘要翻译: 本发明的目的是提供具有整合素α噬菌体拮抗活性的m取代苯甲酸衍生物。 根据本发明的衍生物是由式(I)表示的化合物或其药学上可接受的盐或溶剂化物,其可用于治疗或预防心血管疾病,血管生成相关疾病,脑血管疾病,癌症及其转移,免疫疾病 ,骨病和其他疾病:其中A表示任选取代的含有两个氮原子的杂环基团,二等基团等; D表示键,NR 4,CR 5 R 6,O,S或-NR 4 -CR 5 R 6 - 。 X表示CH或N; R 7和R 8代表羟基,烷基等; Q表示> C = O等; R 9表示氢,烷基等; J表示键或亚烷基; R 10表示任选取代的羟基,氨基等; R 11表示氢,烷基等; m为0〜5; n为0〜4; p和q各自为0〜3。

    Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists
    3.
    发明授权
    Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists 失效
    苯基哌嗪衍生物作为整合素α2β拮抗剂

    公开(公告)号:US06451800B1

    公开(公告)日:2002-09-17

    申请号:US09601176

    申请日:2000-07-28

    IPC分类号: A61K31497

    摘要: An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and therapeutic agents for treating integrin &agr;v&bgr;3-mediated diseases and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic ring containing two nitrogen atoms or the like; X and Z represent CH or a nitrogen atom; R4 and R5 represent alkyl, halogen or the like; Q represents >C=O, >CH2 or the like; R6 represents H, alkyl, aralkyl or the like; R7 represents H, alkynyl or the like; R8 represents H, substituted amino or the like; R9 represents H or alkyl; m is 0 to 5; n is 0 to 4; p is 2 or 3; and q is 0 or 1.

    摘要翻译: 本发明的目的是提供具有整合素α2拮抗活性,GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物,以及用于治疗整合素α1β介导的疾病和抑制血小板聚集的治疗剂。 根据本发明的衍生物是由式(I)表示的化合物或其药学上可接受的盐或溶剂化物:其中A表示含有两个氮原子等的5-至7-元杂环; X和Z表示CH或氮原子; R4和R5代表烷基,卤素等; Q表示> C = O,> CH2等; R6表示H,烷基,芳烷基等; R 7表示H,炔基等; R8表示H,取代的氨基等; R9代表H或烷基; m为0〜5; n为0〜4; p为2或3; q为0或1。

    Aminopiperidine derivates as integrin &agr;v&bgr;3 antagonists
    4.
    发明授权
    Aminopiperidine derivates as integrin &agr;v&bgr;3 antagonists 有权
    氨基哌啶衍生物作为整联蛋白α2β拮抗剂

    公开(公告)号:US06420558B1

    公开(公告)日:2002-07-16

    申请号:US09673017

    申请日:2000-10-10

    IPC分类号: C07D23902

    CPC分类号: C07D235/14 C07D401/12

    摘要: An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic group containing two nitrogen atoms or the like; D represents >NH2, >CH2 or the like; X and Z represent CH or a nitrogen atom; R7 and R8 represent alkyl, halogen or the like; Q represents >C═O, >CH2 or the like; R9 represents H, alkyl, aralkyl or the like; R10 represents H, alkynyl or the like; R11 represents H, substituted amino or the like; R12 represents H or alkyl; m is 0 to 5; n is 0 to 4; p and q are each 1 to 3; and r is 0 or 1.

    摘要翻译: 本发明的目的是提供具有整合素α噬菌体拮抗活性,细胞粘附抑制活性,GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物,以及用于治疗心血管疾病,血管发生相关疾病 脑血管疾病等,并用于抑制血小板聚集。 根据本发明的衍生物是由式(I)表示的化合物或其药学上可接受的盐或溶剂合物:其中A表示含有两个氮原子等的5-至7-元杂环基; D表示> NH 2,> CH 2等; X和Z表示CH或氮原子; R 7和R 8表示烷基,卤素等; Q表示> C = O,> CH2等; R 9表示H,烷基,芳烷基等; R 10表示H,炔基等; R11表示H,取代的氨基等; R 12表示H或烷基; m为0〜5; n为0〜4; p和q各自为1至3; r为0或1。

    Process for manufacturing silver halide color photographic light
sensitive material

    公开(公告)号:USH1167H

    公开(公告)日:1993-04-06

    申请号:US586682

    申请日:1990-09-24

    IPC分类号: G03C7/20 G03C1/035 G03C7/30

    摘要: A process for manufacturing a silver halide color photographic material is disclosed. The photographic material comprises a blue light-sensitive layer-unit, a green light-sensitive layer-unit and a red light-sensitive layer-unit in which at least one of the light-sensitive layer-units comprises two or three silver halide emulsion layers being substantially the same in spectral sensitivity and different in speed from each other. The manufacturing process comprises steps ofproducing a high-speed silver halide emulsion having a largest average grain size among the silver halide emulsions to be used in the at least one light sensitive layer-unit,chemically sensitizing the high-speed silver halide emulsion, producing a low-speed silver halide emulsion having a smaller average grain size than that of the high-speed emulsion,chemically sensitizing the low-speed emulsion,mixing the chemically sensitized high-speed and the chemically sensitized low-speed emulsion in a ratio of from 5:95 to 50:50 by weight in terms of silver, andcoating the chemically sensitized high-speed emulsion and the mixture of the chemically sensitized high-speed emulsion and the chemically sensitized low-speed emulsion to form the at least one light-sensitive layer-unit.The photographic material is improved in adaptability to fluctuation of processing conditions.

    Light-sensitive silver halide color photographic material having
cross-emulsion sensitive DIR compounds
    8.
    发明授权
    Light-sensitive silver halide color photographic material having cross-emulsion sensitive DIR compounds 失效
    具有交联敏感性化合物的感光银色彩色摄影材料

    公开(公告)号:US5156944A

    公开(公告)日:1992-10-20

    申请号:US559974

    申请日:1990-07-27

    IPC分类号: G03C7/30 G03C7/305

    摘要: There is disclosed a light-sensitive silver halide photographic material, having two or more light-sensitive silver halide emulsion layers different in color sensitivities on a support, at least one of the light-sensitive silver halide emulsion layer comprises monodispersed silver halide grains containing 8 to 30 mole % of silver halide in core or contains twinned crystal silver halide grains, at least two of the light-sensitive silver halide emulsion layers different in color sensitivities containing a DIR compound capable of releasing a developing inhibitor or developing inhibitor precursor through the reaction with the oxidized product of a developing agent, the developing inhibitor or developing inhibitor precursor released from the DIR compound being diffusive, wherein the following conditions A:DIR compounds are added and incorporated in the emulsion layers so that the developing inhibitor released from the DIR compound incorporated in one color-sensitive silver halide emulsion layer and the developing inhibitor released from the DIR compound incorporated in the other color-sensitive silver halide emulsion layer are reversed in developing inhibiting power when the DIR compounds to be incorporated in the respective light-sensitive silver halide emulsion layers are exchanged with each other, and also each DIR compound may have greater inhibiting power for the other light-sensitive silver halide emulsion layer rather than for the light-sensitive silver halide emulsion layer in which it is incorporated,is satisfied for the at least two light-sensitive silver halide emulsion layers different in color sensitivities.

    摘要翻译: 公开了一种感光卤化银照相材料,其具有在支持体上具有不同颜色敏感度的两种或更多种感光卤化银乳剂层,至少一种感光卤化银乳剂层包含单分散的卤化银颗粒,其含有8 至30摩尔%的核卤化银或含有孪晶的结晶卤化银颗粒,至少两种感光性卤化银乳剂层的颜色敏感度不同,其含有通过反应释放显影抑制剂或显影抑制剂前体的DIR化合物 与显影剂的氧化产物,从DIR化合物释放的显影抑制剂或显影抑制剂前体是扩散的,其中以下条件A:将DIR化合物加入并掺入乳液层中,使显影抑制剂从DIR化合物释放 并入一种颜色敏感的卤化银乳剂中 当并入相应的感光卤化银乳剂层中的DIR化合物彼此交换时,从引入另一个感光卤化银乳剂层中的DIR化合物释放的显影抑制剂和显影抑制力反转, 并且对于其它感光卤化银乳剂层而言,每个DIR化合物也可以具有更大的抑制力,而不是对于其中并入其的感光卤化银乳剂层,对于至少两种感光卤化银乳剂 层色彩敏感度不同。

    Intercar gangway for articulated cars
    9.
    发明授权
    Intercar gangway for articulated cars 失效
    Intercar通道用于铰链车

    公开(公告)号:US4903612A

    公开(公告)日:1990-02-27

    申请号:US293125

    申请日:1989-01-03

    IPC分类号: B62D53/00 B60D5/00 B61D17/20

    CPC分类号: B60D5/006 B61D17/20

    摘要: A corridor apparatus of an articulating section for use in articulated cars comprises: a pair of rectangular outer corridors respectively provided to end surfaces of car bodies to be articulated, in such a manner as to project therefrom and surround corridor entrances of the car bodies; a pair of rectangular inner corridors each adapted to partially fit with each of the outer corridors in a connected manner; and a pair of gate-shaped inner frames each connected to the other end of each of the inner corridors, the inner frames being fitted with each other such as to be swingable in the direction of the articulating section's corridor with lower ends thereof as a supporting point, wherein the rectangular outer corridors, the inner corridors, and the inner frames constitute peripheral walls of the articulating section's corridor, fitting portions of the outer corridors and the inner corridors are arranged to be rotatable around a center point of the articulating section's corridor, coupling portions of each of the inner corridors and each of the inner frames are adapted to move together with respect to movement in the direction of the articulating section's corridor and can be slid and displaced rative to each other with respect to a direction perpendicular to that of the articulating section's corridor.

    摘要翻译: 一种用于铰接式车辆的铰接部分的走廊装置包括:一对矩形外走廊,分别设置在待铰接的车身的端面上,以便从其突出并围绕轿厢体的走廊入口; 一对长方形的内部走廊,各自适于以连接的方式部分地与每个外部走廊配合; 以及一对各自连接到每个内部走廊的另一端的门形内框架,所述内框架彼此相配合,以便能够沿着所述关节部分走廊的方向摆动,其下端作为支撑 其中,所述矩形外走廊,所述内走廊和所述内框架构成所述关节部的走廊的周壁,所述外走廊和所述内走廊的嵌合部被布置成围绕所述关节部的走廊的中心点可旋转, 每个内部走廊和每个内部框架的联接部分适于相对于关节部分的走廊的方向移动而一起移动,并且可以相对于垂直于关节部分走廊的方向彼此相对滑动和移位 演讲部分的走廊。

    Silver halide photographic material
    10.
    发明授权
    Silver halide photographic material 失效
    卤化银照相材料

    公开(公告)号:US4554247A

    公开(公告)日:1985-11-19

    申请号:US579765

    申请日:1984-02-13

    IPC分类号: G03C1/06 G03C1/30 G03C7/388

    CPC分类号: G03C1/30 G03C1/06 G03C7/388

    摘要: A silver halide photographic material having as essential photographic layers at least one photosensitive silver halide emulsion layer and at least one non-sensitive hydrophilic colloidal layer on a support is disclosed. At least one of said photographic layers contains fine oil globules at a density of 1 or more, and a hardener having at least three functional groups is incorporated in at least one photographic layer containing said fine oil globules and/or at least one photographic layer which is farther from said support than the photographic layer containing said fine oil globules.

    摘要翻译: 公开了一种卤化银照相材料,其具有至少一个光敏卤化银乳剂层和支持体上的至少一个非敏感性亲水性胶体层作为基本照相层。 所述照相层中的至少一个包含密度为1或更大的细小油球,并且具有至少三个官能团的固化剂被引入至少一个含有所述细小油墨的照相层和/或至少一个摄影层, 比含有所述细小油球的照相层更远离所述载体。