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1. 发明申请

WO1995009620A1 SULFOXIMINE AND SULFODIIMINE MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： SULFOXIMINE和SULFODIIMINE MATRIX金属蛋白酶抑制剂
公开(公告)号：WO1995009620A1
公开(公告)日：1995-04-13
申请号：PCT/US1994011164
申请日：1994-10-03
申请人： FLORIDA STATE UNIVERSITY
发明人： FLORIDA STATE UNIVERSITY , SCHWARTZ, Martin, A. , WART, Hal, Van
IPC分类号： A61K31/16
CPC分类号： C07D233/64 , A61K38/00 , C07C381/10 , C07D209/18 , C07D263/26 , C07D403/12 , C07K5/06 , C07K5/06078 , Y10S514/824 , Y10S514/825 , Y10S514/843 , Y10S514/912
摘要： Novel sulfoximine and sulfodiimine matrix metalloproteinase inhibitors of formula (I), wherein: R is selected from the group consisting of lower-alkyl, hydroxy lower-alkyl, amino lower-alkyl, carbamoyl lower-alkyl, lower-alkyl carbonyl, lower-alkyoxyalkyl, aralkyl and heteroaralkyl; X is NH or O; R is selected from the group consisting of hydrogen, lower-alkyl and aralkyl; R is selected from the group consisting of hydrogen, lower-alkyl, amino lower-alkyl, guanyl lower-alkyl, aralkyl and heteroaralkyl; and R is selected from the group consisting of lower alkyl, aralkyl and -CH(R )-C(O)NH2, wherein R is selected from the group consisting of hydrogen, lower-alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, hydroxymethyl, 1-hydroxyethyl, mercapto lower-alkyl and methylthio lower-alkyl; useful for modulating physiological functions or treating diseases and disease conditions associated with matrix metalloproteinase modulation.
摘要翻译：式（I）的新型磺酰亚胺和亚磺酰亚胺基质金属蛋白酶抑制剂，其中：R 1选自低级烷基，羟基低级烷基，氨基低级烷基，氨基甲酰基低级烷基，低级烷基羰基，低级烷氧基烷基，芳烷基和杂芳烷基; X是NH或O; R 2选自氢，低级烷基和芳烷基; R 3选自氢，低级烷基，氨基低级烷基，鸟烷基低级烷基，芳烷基和杂芳烷基; 和R 4选自低级烷基，芳烷基和-CH（R 5）-C（O）NH 2，其中R 5选自氢，低级烷基，氨基低级烷基，鸟嘌呤低级烷基，咪唑基烷基，羟甲基，1-羟乙基，巯基低级烷基和甲硫基低级烷基; 可用于调节生理功能或治疗与基质金属蛋白酶调节相关的疾病和疾病状况。

2. 发明申请

WO2005032541A1 SUBSTITUTED HETEROCYCLIC MERCAPTOSULFIDE INHIBITORS 审中-公开
标题翻译：取代的杂环化合物抑制剂
公开(公告)号：WO2005032541A1
公开(公告)日：2005-04-14
申请号：PCT/US2004/031847
申请日：2004-09-29
申请人： FLORIDA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , SCHWARTZ, Martin, A. , JIN, Yonghao , HURST, Douglas, R. , SANG, Qing-Xiang
发明人： SCHWARTZ, Martin, A. , JIN, Yonghao , HURST, Douglas, R. , SANG, Qing-Xiang
IPC分类号： A61K31/341
CPC分类号： C07D491/04 , C07D207/12 , C07D403/06
摘要： Novel substituted heterocyclic mercaptosulfide compounds, precursors, and derivatives, the methods for the preparation, and pharmaceutical compositions of these compounds are described in this invention. These compounds are developed and tested to be potent and relatively selective inhibitors of matrix metalloproteinases (MMPs), e.g. membrane type 1 MMP, gelatinase B, gelatinase A, collagenases, matrilysins, metalloelastase, and stromelysin-1. These inhibitors will be used for the control of physiological and pathological processes in which metalloproteases play a significant role. These inhibitors can be used for human beings, animals, and other organisms.
摘要翻译：本发明描述了新型取代的杂环巯基硫化物化合物，前体和衍生物，制备方法和这些化合物的药物组合物。开发和测试这些化合物是基质金属蛋白酶（MMP）的有效和相对选择性抑制剂，例如，膜1型MMP，明胶酶B，明胶酶A，胶原酶，母液溶蛋白，金属弹性蛋白酶和基质溶素-1。这些抑制剂将用于控制金属蛋白酶发挥重要作用的生理和病理过程。这些抑制剂可用于人，动物和其他生物。

3. 发明申请

WO1995009833A1 MERCAPTOSULFIDE METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译： MERCAPTOSULFIDE金属蛋白酶抑制剂
公开(公告)号：WO1995009833A1
公开(公告)日：1995-04-13
申请号：PCT/US1994011165
申请日：1994-10-03
申请人： FLORIDA STATE UNIVERSITY
发明人： FLORIDA STATE UNIVERSITY , SCHWARTZ, Martin, A. , WART, Hal, Van
IPC分类号： C07C233/03
CPC分类号： C07D209/48 , C07C323/60 , C07D209/18 , C07D233/64
摘要： Novel mercaptosulfide matrix metalloproteinase inhibitors of formula (I), wherein n is 0 or 1; R is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN (lower alkyl), TsNH (lower alkyl); and R is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN (lower alkyl), TsNH (lower alkyl); or R and R together are -CH2-CH2-CH2-; R is selected from the group consisting of hydrogen, lower alkyl, aralkyl and heteroaralkyl; and R is selected from the group consisting of hydrogen, lower alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, aralkyl and 2-indolylmethyl; and R is selected from the group consisting of lower alkyl, aralkyl and -CH(R )-C(O)NH2, wherein R is selected from the group consisting of hydrogen, lower-alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, hydroxymethyl, 1-hydroxyethyl, mercapto lower-alkyl, and methylthio lower-alkyl; or a pharmaceutically acceptable ester, ether or salt thereof, useful for treating diseases and disease conditions associated with matrix metalloproteinase modulation.
摘要翻译：式（I）的新巯基硫化物基质金属蛋白酶抑制剂，其中n为0或1; R 1选自氢，低级烷基，氨基低级烷基，氨基甲酰基低级烷基，PhtN（低级烷基），TsNH（低级烷基）; 和R 2选自氢，低级烷基，氨基低级烷基，氨基甲酰基低级烷基，PhtN（低级烷基），TsNH（低级烷基）; 或R 1和R 2一起是-CH 2 -CH 2 -CH 2 - ; R 3选自氢，低级烷基，芳烷基和杂芳烷基; R 4选自氢，低级烷基，氨基低级烷基，脒基低级烷基，咪唑基烷基，芳烷基和2-吲哚基甲基; 和R 5选自低级烷基，芳烷基和-CH（R 6）-C（O）NH 2，其中R 6选自氢，低级烷基，氨基低级烷基，鸟嘌呤低级烷基，咪唑基烷基，羟甲基，1-羟乙基，巯基低级烷基和甲硫基低级烷基; 或其药学上可接受的酯，醚或其盐，其可用于治疗与基质金属蛋白酶调节相关的疾病和疾病状况。

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