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    Aryl (sulfide, sulfoxide and sulfone) derivatives and drugs containing the same as the active ingredient
    3.
    发明授权
    Aryl (sulfide, sulfoxide and sulfone) derivatives and drugs containing the same as the active ingredient 失效
    芳基（硫醚，亚砜和砜）衍生物和含有与活性成分相同的药物

    公开(公告)号：US06300514B1

    公开(公告)日：2001-10-09

    申请号：US09214116

    申请日：1999-01-15

    申请人： Kanji Takahashi ,  Tsuneyuki Sugiura

    发明人： Kanji Takahashi ,  Tsuneyuki Sugiura

    IPC分类号： C07C32100

    CPC分类号： C07K5/0812 ,  C07C317/44 ,  C07C317/46 ,  C07C317/50 ,  C07C323/52 ,  C07C323/59 ,  C07C323/60 ,  C07K5/06078

    摘要： Pharmaceutical composition containing aryl (sulfide, sulfoxide, sulfone) derivatives of the formula (1) and the salts thereof as active ingredient (wherein R1 is H, alkyl; R2 is COOR7, CONHOR8; E is —CONR9—, —NR9CO—, —OCO—,—COO—, —CH2—O—, —(CH2)2—, vinylene, ethynylene; J is bond, alkylene; A is H, alkyl, Ar, alkyl-OH ; R3, R4 is H, alkyl, COOR19, hydroxy, —NR20R21, Ar1 etc.); R5, R6 is H, methyl) and the novel aryl (sulfide, sulfoxide, sulfone) derivatives of the formula (I). The compounds of the formula (I) have inhibitory activity against matrix metalloproteinases, therefore, the compounds of the formula (I) are useful for prevention and/or treatment of rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, autoimmune diseases, diseases caused by vascular emigration or infiltration of leukocytes, arterialization etc.

    摘要翻译： 含有式（1）的芳基（硫醚，亚砜，砜）衍生物及其盐作为活性成分（其中R 1为H，烷基; R 2为COOR 7，CONHOR 8; E为-CONR 9 - ， - NR 9 CO-， - OCO - ， - COO-， - CH 2 -O - ， - （CH 2）2 - ，亚乙烯基，亚乙炔基; J是键，亚烷基; A是H，烷基，Ar，烷基-OH; R 3，R 4是H，烷基， COOR 19，羟基，-NR 20 R 21，Ar 1等）; R5，R6是H，甲基）和式（Ⅰ）的新型芳基（硫醚，亚砜，砜）衍生物。式（I）化合物对基质金属蛋白酶具有抑制活性，因此式 I）可用于预防和/或治疗类风湿病，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，自身免疫性疾病，血管迁移或白细胞浸润引起的疾病， 动脉化等

    Sulfonylamino acid derivatives
    4.
    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
    5.
    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。

    4-aminobutanoic acid derivatives and drugs containing these derivatives as the active ingredient
    6.
    发明授权
    4-aminobutanoic acid derivatives and drugs containing these derivatives as the active ingredient 失效
    4-氨基丁酸衍生物和含有这些衍生物作为活性成分的药物

    公开(公告)号：US06569899B1

    公开(公告)日：2003-05-27

    申请号：US09958093

    申请日：2001-10-05

    申请人： Kanji Takahashi ,  Tsuneyuki Sugiura

    发明人： Kanji Takahashi ,  Tsuneyuki Sugiura

    IPC分类号： A61K31166

    CPC分类号： C07C271/22 ,  C07B2200/07 ,  C07C229/22 ,  C07C233/63 ,  C07C233/83 ,  C07C233/84 ,  C07C233/87 ,  C07C235/52 ,  C07C255/57 ,  C07C255/60 ,  C07C259/06 ,  C07C259/08 ,  C07C2601/04 ,  C07C2601/14 ,  C07F9/3808

    摘要： Aminobutylic acid derivatives of the formula (I) wherein the symbols are as defined in specification; and non-toxic salts thereof. Because of inhibiting matrix metalloproteinase, the compounds of the formula (I) are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, osteoarthritis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, cornea ulcer, metastasis, invasion or growth of tumor cells, autoimmune disease, disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, arota aneurysm, endometriosis, restenosis after PTCA, unstable angina, acute myocardial infarction, transient ischemic attack.

    摘要翻译： 式（I）的氨基丁酸衍生物，其中符号如说明书中所定义; 及其无毒盐。 由于抑制基质金属蛋白酶，式（I）化合物可用于预防和/或治疗疾病，例如类风湿病，关节炎，骨关节炎，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，角膜溃疡，转移，肿瘤细胞的侵袭或生长，自身免疫性疾病，血管移行或白细胞浸润引起的疾病，动脉化，多发性硬化，动脉瘤，子宫内膜异位症，PTCA后再狭窄，不稳定心绞痛，急性心肌 梗死，短暂性脑缺血发作。

    Method of treating disease with sulfonylamino acid derivatives
    7.
    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。