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1. 发明授权

US06403644B1 Method of treating disease with sulfonylamino acid derivatives 失效
标题翻译：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。

2. 发明授权

US06177466B1 Sulfonylamino acid derivatives 失效
标题翻译：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。

3. 发明授权

US6022893A Hydroxamic acid derivatives 失效
标题翻译：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。

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