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公开(公告)号：US06569855B2
公开(公告)日：2003-05-27
申请号：US09888675
申请日：2001-06-25
申请人： Michael George Natchus , Biswanath De , Stanislaw Pikul , Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Menyan Cheng
发明人： Michael George Natchus , Biswanath De , Stanislaw Pikul , Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Menyan Cheng
IPC分类号： A61K31401
CPC分类号： C07D207/42
摘要： The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译： 本发明提供了可用作金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，本发明涉及具有式（I）结构的化合物。还公开了使用这些化合物或含有它们的药物组合物治疗以金属蛋白酶活性为特征的疾病的化合物，药物组合物和方法。
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公开(公告)号：US06417219B1
公开(公告)日：2002-07-09
申请号：US08918317
申请日：1997-08-26
申请人： Michael George Natchus , Biswanath De , Stanislaw Pikul , Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Menyan Cheng
发明人： Michael George Natchus , Biswanath De , Stanislaw Pikul , Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Menyan Cheng
IPC分类号： A61K31401
CPC分类号： C07D207/42
摘要： The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译： 本发明提供了可用作金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，本发明涉及具有式（I）结构的化合物。还公开了使用这些化合物或含有它们的药物组合物治疗以金属蛋白酶活性为特征的疾病的化合物，药物组合物和方法。
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公开(公告)号：US06197770B1
公开(公告)日：2001-03-06
申请号：US09517080
申请日：2000-03-01
申请人： Michael George Natchus , Roger Gunnard Bookland , Neil Gregory Almstead , Stanislaw Pikul , Biswanath De , Menyan Cheng
发明人： Michael George Natchus , Roger Gunnard Bookland , Neil Gregory Almstead , Stanislaw Pikul , Biswanath De , Menyan Cheng
IPC分类号： A61K315375
CPC分类号： C07D207/337 , A61K31/5375 , C07C311/21 , C07C311/29 , C07C311/42 , C07C311/46 , C07C311/47 , C07C323/58 , C07C323/67 , C07D209/42 , C07D213/55 , C07D213/81 , C07D213/82 , C07D285/135 , C07D295/088 , C07D295/145 , C07D295/185 , C07D295/192 , C07D295/195 , C07D295/26 , C07D307/54 , C07D317/48 , C07D333/24 , C07D333/34 , C07D413/04
摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where X, W, Z, A, G, R1, R2, R3, R4, R5, R5′ and k have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof Also described are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
摘要翻译： 公开了作为金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，这些化合物具有下式（I）的结构：其中X，W，Z，A，G，R 1，R 2，R 3，R 4，R 5，R 5'和k具有说明书中描述的含义。 本发明还包括上式的光学异构体，非对映异构体和对映异构体及其药学上可接受的盐，生物水解性酰胺，酯和酰亚胺。还描述了包含这些化合物的药物组合物，以及使用该化合物治疗或预防金属蛋白酶相关性疾病的方法 化合物或药物组合物。
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公开(公告)号：US06872742B2
公开(公告)日：2005-03-29
申请号：US10186531
申请日：2002-07-01
申请人： Michael George Natchus , Biswanath De , Stanislaw Pikul , Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Menyan Cheng
发明人： Michael George Natchus , Biswanath De , Stanislaw Pikul , Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Menyan Cheng
IPC分类号： C07D207/42 , A61K31/40
CPC分类号： C07D207/42
摘要： The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译： 本发明提供了可用作金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，本发明涉及具有式（I）结构的化合物。还公开了使用这些化合物或含有它们的药物组合物治疗以金属蛋白酶活性为特征的疾病的化合物，药物组合物和方法。
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公开(公告)号：US06858628B2
公开(公告)日：2005-02-22
申请号：US10308780
申请日：2002-12-03
申请人： Michael George Natchus , Biswanath De , Stanislaw Pikul , Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Menyan Cheng
发明人： Michael George Natchus , Biswanath De , Stanislaw Pikul , Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Menyan Cheng
IPC分类号： A23G4/00 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/42 , A61K31/428 , A61K31/4439 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/541 , A61P1/02 , A61P1/04 , A61P3/12 , A61P9/00 , A61P17/00 , A61P19/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D207/16 , C07D207/42 , C07D207/48 , C07D211/60 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/04 , C07D211/30 , C07D211/40
CPC分类号： C07D207/42
摘要： The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
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公开(公告)号：US06218389B1
公开(公告)日：2001-04-17
申请号：US09127678
申请日：1998-07-31
申请人： Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Rimma Sandler Bradley , Rodney Dean Bush , Biswanath De , Michael George Natchus , Stanislaw Pikul
发明人： Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Rimma Sandler Bradley , Rodney Dean Bush , Biswanath De , Michael George Natchus , Stanislaw Pikul
IPC分类号： A61K31535
CPC分类号： C07D207/412 , C07C311/14 , C07C311/19 , C07C311/29 , C07C317/48 , C07C323/60 , C07C323/61 , C07C2601/14 , C07C2602/42 , C07D209/48 , C07D211/54 , C07D211/84 , C07D213/82 , C07D233/74 , C07D277/46 , C07D309/08 , C07D335/02 , C07F9/36 , Y10S514/824 , Y10S514/825 , Y10S514/826 , Y10S514/887 , Y10S514/902 , Y10S514/903
摘要： The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译： 本发明提供了权利要求中描述的式的化合物或其旋光异构体，非对映异构体或对映异构体，或其药学上可接受的盐或可生物水解的酰胺，酯或酰亚胺可用作金属蛋白酶的抑制剂。还公开了药物组合物和 使用这些化合物治疗以金属蛋白酶活性为特征的疾病，病症和病症的方法或含有它们的药物组合物。
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公开(公告)号：US06329418B1
公开(公告)日：2001-12-11
申请号：US09274564
申请日：1999-03-23
申请人： Menyan Cheng , Michael George Natchus , Biswanath De , Neil Gregory Almstead , Yetunde Olabisi Taiwo , Stanislaw Pikul
发明人： Menyan Cheng , Michael George Natchus , Biswanath De , Neil Gregory Almstead , Yetunde Olabisi Taiwo , Stanislaw Pikul
IPC分类号： A61K3140
CPC分类号： C07D401/12 , C07D207/48 , C07D403/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The invention provides compounds which are potent inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to compounds having a structure according to the following Formula (I): wherein R1, R2, X, Z, m, and n are defined below. to This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of diseases and conditions which are characterized by unwanted metalloprotease activity. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for metalloprotease-related maladies using these compounds or the pharmaceutical compositions containing them.
摘要翻译： 本发明提供了作为金属蛋白酶的有效抑制剂的化合物，其有效治疗以这些酶的过度活性为特征的病症。 特别地，本发明涉及具有根据下式（I）的结构的化合物：其中R1，R2，X，Z，m和n定义如下。本发明还包括光学异构体，非对映异构体和对映异构体 上式，及其可药用盐，生物可水解酰胺，酯和酰亚胺。 本发明的化合物可用于治疗以不需要的金属蛋白酶活性为特征的疾病和病症。 因此，本发明还提供包含这些化合物的药物组合物。 本发明还提供了使用这些化合物或含有它们的药物组合物治疗金属蛋白酶相关疾病的方法。
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公开(公告)号：US06762198B2
公开(公告)日：2004-07-13
申请号：US10396775
申请日：2003-03-25
IPC分类号： A61K3142
CPC分类号： C07D213/70 , C07C311/29 , C07C317/48 , C07C323/58 , C07D213/65 , C07D233/84 , C07D235/28 , C07D239/95 , C07D249/10 , C07D257/04 , C07D263/58 , C07D271/113 , C07D277/74 , C07D285/08 , C07D307/38 , C07D311/16 , C07D333/34 , C07D413/04 , C07D473/36
摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where J, M, Q, T, W, X, Z, R1, R2, R3, R4, R4′, R5, R6, R6′, R7, m, and n have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also disclosed are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
摘要翻译： 公开了作为金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。 特别地，该化合物具有根据下式（I）的结构：其中J，M，Q，T，W，X，Z，R 1，R 2，R 3，R 4 R 4，R 5，R 6，R 6'，R 7，m和n具有说明书中所述的含义。 本发明还包括上式的光学异构体，非对映异构体和对映异构体及其药学上可接受的盐，可生物水解的酰胺，酯和酰亚胺。 还公开了包含这些化合物的药物组合物，以及使用该化合物或药物组合物治疗或预防金属蛋白酶相关疾病的方法。
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公开(公告)号：US06566381B1
公开(公告)日：2003-05-20
申请号：US09516743
申请日：2000-03-01
IPC分类号： A61K3142
CPC分类号： C07D213/70 , C07C311/29 , C07C317/48 , C07C323/58 , C07D213/65 , C07D233/84 , C07D235/28 , C07D239/95 , C07D249/10 , C07D257/04 , C07D263/58 , C07D271/113 , C07D277/74 , C07D285/08 , C07D307/38 , C07D311/16 , C07D333/34 , C07D413/04 , C07D473/36
摘要： Heterocyclic substituted compounds having the general structure: which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.
摘要翻译： 具有一般结构的杂环取代的化合物：其是金属蛋白酶的抑制剂，并且其有效地处理以这些酶的过量活性为特征的条件。
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公开(公告)号：US06545038B1
公开(公告)日：2003-04-08
申请号：US09707212
申请日：2000-11-06
申请人： Biswanath De , Stanislaw Pikul , Menyan Cheng , Neil Gregory Almstead , Randall Stryker Matthews , Michael George Natchus , Yetunde Olabisi Taiwo
发明人： Biswanath De , Stanislaw Pikul , Menyan Cheng , Neil Gregory Almstead , Randall Stryker Matthews , Michael George Natchus , Yetunde Olabisi Taiwo
IPC分类号： A61K31675
CPC分类号： C07D265/30 , C07D223/06 , C07D241/04 , C07D241/08 , C07D279/12 , C07D281/00 , C07D281/06 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/12 , Y02P20/582
摘要： The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译： 本发明提供了权利要求中描述的式的化合物或其旋光异构体，非对映异构体或对映异构体，或其药学上可接受的盐或可生物水解的酰胺，酯或酰亚胺可用作金属蛋白酶的抑制剂。还公开了药物组合物和 使用这些化合物治疗以金属蛋白酶活性为特征的疾病，病症和病症的方法或含有它们的药物组合物。
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