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    Sulfonylamino acid derivatives
    1.
    发明授权
    Sulfonylamino acid derivatives 失效
    磺酰氨基酸衍生物

    公开(公告)号：US06177466B1

    公开(公告)日：2001-01-23

    申请号：US08688161

    申请日：1996-07-29

    申请人： Katsuhito Sakaki ,  Hidekazu Kanazawa ,  Tsuneyuki Sugiura ,  Tohru Miyazaki ,  Hiroyukii Ohno

    发明人： Katsuhito Sakaki ,  Hidekazu Kanazawa ,  Tsuneyuki Sugiura ,  Tohru Miyazaki ,  Hiroyukii Ohno

    IPC分类号： C07C31142

    CPC分类号： C07D213/81 ,  C07C311/19 ,  C07C311/29 ,  C07C311/46 ,  C07C311/47 ,  C07D209/20 ,  C07D213/55 ,  C07D233/64 ,  C07D307/71 ,  C07D333/38

    摘要： The present invention is related to: (i) matrix metalloproteinase inhibitors containing sulfonylamino acid derivatives of the formula (Ia): wherein R1 is hydrogen, C1-4 alkyl; R is hydrogen, C1-8 alkyl etc.; E is —CONR3—, in which R3 is hydrogen, C1-4 alkyl etc., —NR3CO—, —CO—O—, —O—CO— etc.; A is hydrogen, C1-8 alkyl, C3-7 cycloalkyl, or Ar; J is bond, C2-4 alkylene etc.; G is —(CH2)m— in which m is 2, 3 or 4, or in which R6 and R7 is hydrogen, C1-8 alkyl etc.; and non-toxic salts thereof, (ii) novel sulfonylamino acid derivatives of the formula (Ib): wherein all the symbols are the same meaning as (i); and non-toxic salts thereof, and (iii) process for the preparation of the compound of the formula (Ib). The compounds of the formula (Ia) are useful for prevention and/or treatment of diseases induced by overexpression and excess activity of MMP. The diseases such as above, for example, are rheumatoid, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cell, autoimmune disease (Crohn's disease, Sjogren's syndrome etc.), disease caused by vascular emigration or infiltration of leukocytes, arterialization.

    摘要翻译： 本发明涉及：（i）含有式（Ia）的磺酰氨基酸衍生物的基质金属蛋白酶抑制剂：其中R1是氢，C1-4烷基; R是氢，C 1-8烷基等; E是-CONR 3 - ，其中R 3是氢，C 1-4烷基等，-NR 3 CO-，-CO-O-，-O-CO-等; A是氢，C 1-8烷基，C 3-7环烷基或Ar; J为键，C2-4亚烷基等; G是 - （CH 2）m - ，其中m是2,3或4，其中R 6和R 7是氢，C 1-8烷基等; 和其无毒盐，（ii）式（Ib）的新型磺酰基氨基酸衍生物：其中所有符号与（i）相同; 和其无毒盐，和（iii）制备式（Ib）化合物的方法。 式（Ia）的化合物可用于预防和/或治疗由MMP的过度表达和过量活性诱导的疾病。 例如上述疾病是类风湿，关节炎，异常骨吸收，骨质疏松症，牙周炎，间质性肾炎，动脉硬化，肺气肿，肝硬化，角膜损伤，肿瘤细胞侵袭或生长的转移，自身免疫性疾病（Crohn's 疾病，干燥综合征等），血管移行或白细胞浸润引起的疾病，动脉化。

    Hydroxamic acid derivatives
    2.
    发明授权
    Hydroxamic acid derivatives 失效
    羟肟酸衍生物

    公开(公告)号：US6022893A

    公开(公告)日：2000-02-08

    申请号：US694473

    申请日：1996-08-07

    申请人： Katsuhito Sakaki ,  Hidekazu Kanazawa ,  Tsuneyuki Sugiura ,  Tohru Miyazaki ,  Hiroyukii Ohno

    发明人： Katsuhito Sakaki ,  Hidekazu Kanazawa ,  Tsuneyuki Sugiura ,  Tohru Miyazaki ,  Hiroyukii Ohno

    IPC分类号： C07C311/46 ,  C07D209/20 ,  C07D333/38 ,  C07C311/41 ,  A61K31/215

    CPC分类号： C07D333/38 ,  C07C311/46 ,  C07D209/20

    摘要： The present invention relates to:(i) hydroxamic acid derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, or C1-4 alkyl; R.sup.2 is hydrogen, C1-8 alkyl, phenyl, C1-4 alkyl substituted by phenyl; E is --CONR.sup.3 --, in which R.sup.3 is hydrogen, C1-4 alkyl, etc., --NR.sup.3 CO--, --CO--O--, --O--CO--etc.; A is hydrogen, C1-8 alkyl, C3-7 cycloalkyl, or Ar; J is bond, C2-4 alkylene etc.; G is --(CH.sub.2).sub.m --, in which m is 2, 3 or 4, or ##STR2## in which R.sup.6 and R.sup.7 is hydrogen, C1-8 alkyl etc.; and non-toxic salts thereof,ii) processes for the preparation thereof, andiii) pharmaceutical agents containing them.The compounds of formula (I) are useful for prevention and/or treatment of diseases induced by overexpression or excess activity of gelatinases, for example, rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cells, autoimmune disease (Crohn's disease, Sjogren's syndrome), disease caused by vascular emigration or infiltration of leukocytes or arterialization in animals including human beings, especially human beings.

    摘要翻译： 本发明涉及：（i）式（I）的异羟肟酸衍生物：其中R 1是氢或C 1-4烷基; R 2是氢，C 1-8烷基，苯基，被苯基取代的C 1-4烷基; E是-CONR 3 - ，其中R 3是氢，C 1-4烷基等，-NR 3 CO-，-CO-O-，-O-CO-等; A是氢，C 1-8烷基，C 3-7环烷基或Ar; J为键，C2-4亚烷基等; G为 - （CH 2）m - ，其中m为2,3或4，或其中R6和R7为氢，C1-8烷基等; 和其无毒盐，ii）其制备方法，和iii）含有它们的药剂。 式（I）化合物可用于预防和/或治疗由明胶酶的过表达或过度活性引起的疾病，例如类风湿病，关节炎，异常骨吸收，骨质疏松症，牙周炎，间质性肾炎，动脉硬化，肺气肿， 肝硬化，角膜损伤，肿瘤细胞侵袭或生长的转移，自身免疫性疾病（克罗恩病，干燥综合征），血管迁移或白细胞浸润引起的疾病或包括人类在内的动物，尤其是人类的动脉化。

    Method of treating disease with sulfonylamino acid derivatives
    4.
    发明授权
    Method of treating disease with sulfonylamino acid derivatives 失效
    用磺酰氨基酸衍生物治疗疾病的方法

    公开(公告)号：US06403644B1

    公开(公告)日：2002-06-11

    申请号：US09709439

    申请日：2000-11-13

    申请人： Katsuhito Sakaki ,  Hidekazu Kanazawa ,  Tsuneyuki Sugiura ,  Tohru Miyazaki ,  Hiroyukii Ohno

    发明人： Katsuhito Sakaki ,  Hidekazu Kanazawa ,  Tsuneyuki Sugiura ,  Tohru Miyazaki ,  Hiroyukii Ohno

    IPC分类号： C07C31142

    CPC分类号： C07D213/81 ,  C07C311/19 ,  C07C311/29 ,  C07C311/46 ,  C07C311/47 ,  C07D209/20 ,  C07D213/55 ,  C07D233/64 ,  C07D307/71 ,  C07D333/38

    摘要： The present invention is related to: (i) matrix metalloproteinase inhibitors containing sulfonylamino acid derivatives of the formula (Ia);  wherein R1 is hydrogen, C1-4 alkyl; R2 is hydrogen, C1-8 alkyl etc.; E is —CONR3—, in which R3 is hydrogen, C1-4 alkyl etc., —NR3CO—, —CO—O—, —O—CO— etc.; A is hydrogen, C1-8 alkyl, C3-7 cycloalkyl, or Ar; J is bond, C2-4 alkylene etc.; G is — (CH2)m—, in which m is 2, 3 or 4, or in which R6 and R7 is hydrogen, C1-8 alkyl etc.; and non-toxic salts thereof, (ii) sulfonylamino acid derivatives of the formula (Ib): wherein all the symbols are the same meaning as (i); and non-toxic salts thereof, and (iii) process for the preparation of the compound of the formula (Ib). The compounds of the formula (Ia) are useful for prevention and/or treatment of diseases induced by overexpression and excess activity of MMP. The diseases such as above, for example, are rheumatoid, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cell, autoimmune disease (Crohn's disease, Sjogren's syndrome etc.), disease caused by vascular emigration or infiltration of leukocytes, arterialization.

    摘要翻译： 本发明涉及：（i）含有式（Ia）的磺酰氨基酸衍生物的基质金属蛋白酶抑制剂; 其中R1是氢，C1-4烷基; R2是氢，C1-8烷基等; E是-CONR 3 - ，其中R 3是氢，C 1-4烷基等，-NR 3 CO-，-CO-O-，-O-CO-等; A是氢，C 1-8烷基，C 3-7环烷基或Ar; J为键，C2-4亚烷基等; G为 - （CH 2）m - ，其中m为2,3或4，其中R 6和R 7为氢，C 1-8烷基等; 和其无毒盐，（ii）式（Ib）的磺酰氨基酸衍生物：其中所有符号与（i）相同; 及其无毒盐，和（iii）制备式（Ib）化合物的方法。式（Ia）化合物可用于预防和/或治疗由过表达和过度活性引起的疾病 MMP。 例如上述疾病是类风湿，关节炎，异常骨吸收，骨质疏松症，牙周炎，间质性肾炎，动脉硬化，肺气肿，肝硬化，角膜损伤，肿瘤细胞侵袭或生长的转移，自身免疫性疾病（Crohn's 疾病，干燥综合征等），血管移行或白细胞浸润引起的疾病，动脉化。

    Map change detection device, map change detection method, and program
    6.
    发明授权
    Map change detection device, map change detection method, and program 有权
    地图变更检测装置，地图变更检测方法和程序

    公开(公告)号：US08116530B2

    公开(公告)日：2012-02-14

    申请号：US12125649

    申请日：2008-05-22

    申请人： Tohru Miyazaki

    发明人： Tohru Miyazaki

    IPC分类号： G06K9/00

    CPC分类号： G06K9/00637 ,  G06K9/00664 ,  G06K9/00704 ,  G06T7/20 ,  G06T2200/04 ,  G06T2207/10021 ,  G06T2207/10032 ,  G06T2207/30181

    摘要： Changes in houses and buildings on a two-dimensional map are detected using three-dimensional data obtained from stereo images. A change detection device that detects changes in features that are targets described on a map has a stereo processor, a feature height calculator, and a demolition and/or new building detector. The stereo processor is inputted with a plurality of images taken of predetermined regions from a plurality of different positions, and extracts digital surface model data representing surfaces of the regions in three-dimensional coordinates. The feature height calculator extracts feature heights where an elevation of ground level is subtracted from the digital surface model data extracted by the stereo processor. The demolition and/or new building detector detect changes in the feature that are the targets described on a map by comparing feature height data and map data. An elevation region extractor extracts an elevation region that is a set of points having a height greater than or equal to the predetermined value, compares the elevation region and the map data, and detects changes in the feature constituting the targets.

    摘要翻译： 使用从立体图像获得的三维数据检测二维地图上的房屋和建筑物的变化。 检测在地图上描述的目标的特征的变化的变化检测装置具有立体声处理器，特征高度计算器和拆除和/或新的建筑物检测器。 立体声处理器输入从多个不同位置拍摄的预定区域的多个图像，并且提取表示三维坐标中的区域的表面的数字表面模型数据。 特征高度计算器提取从由立体声处理器提取的数字表面模型数据中减去地平面高程的特征高度。 拆除和/​​或新建筑物检测器通过比较特征高度数据和地图数据来检测作为地图上描述的目标的特征的变化。 高程区域提取器提取高度大于或等于预定值的一组点的高程区域，比较高程区域和地图数据，并检测构成目标的特征的变化。

    Tetrazole compounds and pharmaceutical agents containing such derivative as an active ingredient
    7.
    发明授权
    Tetrazole compounds and pharmaceutical agents containing such derivative as an active ingredient 失效
    含有这种衍生物作为活性成分的四唑化合物和药剂

    公开(公告)号：US06376484B1

    公开(公告)日：2002-04-23

    申请号：US09572569

    申请日：2000-05-16

    申请人： Kazuyuki Ohmoto ,  Makoto Tanaka ,  Tohru Miyazaki ,  Hiroyuki Ohno

    发明人： Kazuyuki Ohmoto ,  Makoto Tanaka ,  Tohru Miyazaki ,  Hiroyuki Ohno

    IPC分类号： A61K3155

    CPC分类号： C07D257/04 ,  A61K38/00 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07K5/0205 ,  C07K5/06052 ,  C07K5/06139

    摘要： A tetrazole derivatives of formula (I) wherein R1 is H, alkyl, alkoxy, carbocyclic ring, hetero ring, alkyl or alkoxy substituted by carbocyclic ring or hetero ring, etc.; AA1 is bond or  AA2 is bond or  AA1 and AA2, together, may have the formula (a);  Y is the formula (b) (in which Tet ring is tetrazole; Z is alkylene, alkenylene, O, S, SO, SO2, NR26, methylene in alkylene replaced by O, S, —SO—, —SO2— or —NR26—; E is H, alkyl, COOR27 or  in which Cyc is carbocyclic ring or hetero ring); a non-toxic salt thereof, an acid addition salt thereof or a hydrate thereof which has a pharmaceutical agents as an active ingredient. The compound of the formula (I) has an inhibitory effect on interleukin-1&bgr; converting enzyme, therefore, they are useful for prevention and/or treatment of various kinds of inflammatory disease.

    摘要翻译： 式（I）的四唑衍生物，其中R 1为H，烷基，烷氧基，碳环，杂环，被碳环或杂环取代的烷基或烷氧基等; AA1是键或AA2是键或AA1和AA2，一起可以具有式（a）; Y是式（b）（其中Tet环是四唑; Z是亚烷基，亚烯基，O，S，SO，SO 2，NR 26，亚烷基被O，S，-SO-，-SO 2 - 或-NR 26 - ; E是H，烷基，COOR 27或其中Cyc是碳环或杂环）;其无毒盐，其酸加成盐或其水合物，其具有药剂作为活性成分。 式（I）的化合物对白细胞介素-1β转换酶具有抑制作用，因此可用于预防和/或治疗各种炎性疾病。