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1.发明授权Substituted cycloalkanecarboxylic acid derivatives as matrix metalloprotease inhibitors 失效取代的环烷烃羧酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5886022A
公开(公告)日：1999-03-23
申请号：US866568
申请日：1997-05-30
申请人： Harold Clinton Eugene Kluender , William Harrison Bullock , Brian Richard Dixon , Stephan Schneider , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin
发明人： Harold Clinton Eugene Kluender , William Harrison Bullock , Brian Richard Dixon , Stephan Schneider , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin
IPC分类号： C07C59/48 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C62/38 , C07C69/738 , C07C317/44 , C07C323/56 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/16 , C07D209/48 , C07D213/20 , C07D213/70 , C07D215/36 , C07D257/04 , C07D263/32 , C07D307/33 , C07D307/54 , C07D333/24 , C07D333/34 , C07F9/38 , A61K31/40 , A61K31/165 , C07C233/00 , C07D207/00
CPC分类号： C07D209/48 , C07C317/44 , C07C323/56 , C07C323/61 , C07C323/62 , C07C327/32 , C07C59/48 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C62/38 , C07C69/738 , C07D207/16 , C07D213/20 , C07D213/70 , C07D215/36 , C07D257/04 , C07D263/32 , C07D307/33 , C07D307/54 , C07D333/24 , C07D333/34 , C07F9/3882 , C07C2101/08 , C07C2101/14 , C07C2101/16 , C07C2102/44
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent g roup; x is 0, 1, or 2; the group D represents ##STR2## the subscript "e" is 2 or 3; the group R.sup.14 represents a variety of possible substituent groups of the cycloalkyl ring between D and G; the subscript "k" is 0-2; and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic occurring amino acids.
摘要翻译： 基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。 本发明的化合物具有通用化合物“IMAGE”，其中每个T是取代基; x为0,1或2; 组D表示
，下标“e”为2或3; 基团R14表示D和G之间环烷基环的各种可能的取代基; 下标“k”为0-2; 并且基团G表示M，其中M表示-CO 2 H，-CON（R 11）2或-CO 2 R 12; R13表示19个非环状氨基酸的任一侧链。 -
2.发明授权Substituted 4-biarylbutyric acid derivatives as matrix metalloprotease inhibitors 失效取代的4-联芳基丁酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5886043A
公开(公告)日：1999-03-23
申请号：US866778
申请日：1997-05-30
申请人： Harold Clinton Eugene Kluender , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , William Harrison Bullock
发明人： Harold Clinton Eugene Kluender , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , William Harrison Bullock
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , A61K31/235 , C07C59/74 , C07C67/76
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12, and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
摘要翻译： 基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。 本发明的化合物具有通用化合物“IMAGE”，其中每个T是取代基; x为0,1或2; 基团D表示基团R6表示D和G之间碳链上各种可能的取代基，基团G表示M，其中M表示-CO 2 H，-CON（R 11）2或 -CO 2 R 12，R 13表示19个非环状天然存在的氨基酸的任一侧链。
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3.发明授权
公开(公告)号：US5854277A
公开(公告)日：1998-12-29
申请号：US865639
申请日：1997-05-30
申请人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , William Harrison Bullock , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , Jill Elizabeth Wood , David Ross Brittelli
发明人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , William Harrison Bullock , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , Jill Elizabeth Wood , David Ross Brittelli
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , A61K31/38 , A61K31/41 , A61K31/415 , A61K31/435
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
摘要翻译： 基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。 本发明的化合物具有通用化合物“IMAGE”，其中每个T是取代基; x为0,1或2; 基团D表示基团R6表示D和G之间的碳链上的各种可能的取代基，基团G表示M，其中M表示-CO 2 H，-CON（R 11）2， 或-CO 2 R 12; R13表示19个非环状天然氨基酸的任一侧链。
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4.发明授权Substituted 4-biarylbutyric acid derivatives as matrix metalloprotease inhibitors 失效取代的4-联芳基丁酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5859047A
公开(公告)日：1999-01-12
申请号：US866798
申请日：1997-05-30
申请人： Harold Clinton Eugene Kluender , David Ross Brittelli , William Harrison Bullock , Kerry Jeanne Combs , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin
发明人： Harold Clinton Eugene Kluender , David Ross Brittelli , William Harrison Bullock , Kerry Jeanne Combs , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , A61K31/40 , A61K31/165 , A61K31/24 , C07D207/00
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituted group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
摘要翻译： 基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。 本发明的化合物具有通用化合物“IMAGE”，其中每个T是取代基; x为0,1或2; 基团D表示基团R6表示D和G之间的碳链上的各种可能的取代基，基团G表示M，其中M表示-CO 2 H，-CON（R 11）2， 或-CO 2 R 12; R13表示19个非环状天然氨基酸的任一侧链。
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5.发明授权Substituted cycloalkanecarboxylic acid derivatives as matrix metalloprotease inhibitors 失效取代的环烷烃羧酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5874473A
公开(公告)日：1999-02-23
申请号：US864666
申请日：1997-05-28
申请人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , Kerry Jeanne Combs , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , Jill Elizabeth Wood , Stephan Schneider
发明人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , Kerry Jeanne Combs , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , Jill Elizabeth Wood , Stephan Schneider
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , C07C321/00
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the subscript "e" is 2 or 3; the group R.sup.14 represents a variety of possible substituent groups on the cycloalkyl ring between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
摘要翻译： 基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。 本发明的化合物具有通用化合物“IMAGE”，其中每个T是取代基; x为0,1或2; 组D表示
，下标“e”为2或3; 基团R14表示D和G之间的环烷基环上各种可能的取代基，基团G表示M，其中M表示-CO 2 H，-CON（R 11）2或-CO 2 R 12; R13表示19个非环状天然氨基酸的任一侧链。 -
6.发明授权Substituted 5-biarylpentanoic acids and derivatives as matrix metalloprotease inhibitors 失效取代的5-二芳基戊酸及其衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US6166082A
公开(公告)日：2000-12-26
申请号：US57679
申请日：1998-04-09
申请人： Harold Clinton Eugene Kluender , Guenter Hans Heinz Herbert Benz , David Ross Brittelli , William Harrison Bullock , Kerry Jeanne Combs , Brian Richard Dixon , Stephan Schneider , Jill Elizabeth Wood , Michael Christopher VanZandt , Donald John Wolanin , Scott M. Wilhelm
发明人： Harold Clinton Eugene Kluender , Guenter Hans Heinz Herbert Benz , David Ross Brittelli , William Harrison Bullock , Kerry Jeanne Combs , Brian Richard Dixon , Stephan Schneider , Jill Elizabeth Wood , Michael Christopher VanZandt , Donald John Wolanin , Scott M. Wilhelm
IPC分类号： A61K31/192 , A61K31/4035 , A61K31/47 , A61K31/19 , A61K31/235 , A61K31/38 , C07C59/74 , C07D409/00
CPC分类号： A61K31/192 , A61K31/4035 , A61K31/47
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula(T).sub.x A--B--D--E--Gwherein A and B are aryl or heteroaryl rings; each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR1## the group E represents a three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents --M, ##STR2## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; andR.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids, and include pharmaceutically acceptable salts thereof.
摘要翻译： 基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。 本发明的化合物具有通式（T）xA-B-D-E-G，其中A和B是芳基或杂芳基环; 每个T是取代基; x为0,1或2; 基团D表示基团E表示带有一个至三个独立的或参与环形成的取代基的三个碳链，可能的结构在本文和权利要求中示出; 并且基团G表示-M，其中M表示-CO 2 H，-CON（R 11）2或-CO 2 R 12; R13表示19个非环状天然存在的氨基酸的任一侧链，并且包括其药学上可接受的盐。
-
7.发明授权Derivatives of substituted 4-biarylbutyric acid as matrix metalloprotease inhibitors 失效取代的4-联芳基丁酸的衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5789434A
公开(公告)日：1998-08-04
申请号：US539409
申请日：1995-11-06
申请人： Harold Clinton Eugene Kluender , Guenter Hans Heinz Herbert Benz , David Ross Brittelli , William Harrison Bullock , Kerry Jeanne Combs , Brian Richard Dixon , Stephan Schneider , Jill Elizabeth Wood , Michael Christopher VanZandt , Donald John Wolanin , Scott M. Wilhelm
发明人： Harold Clinton Eugene Kluender , Guenter Hans Heinz Herbert Benz , David Ross Brittelli , William Harrison Bullock , Kerry Jeanne Combs , Brian Richard Dixon , Stephan Schneider , Jill Elizabeth Wood , Michael Christopher VanZandt , Donald John Wolanin , Scott M. Wilhelm
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , A61K31/405 , A61K31/40
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The presently claimed compounds have the generalized formula ##STR1## in which each T represents a substituent group; x is 0, 1, or 2; D represents ##STR2## .delta. is 0 or 1; U' represents O, S, or N, with the proviso that when U' is N, then .delta.=0, and when U' is O or S, then .delta.=1; R.sup.14 is any of a variety of substituent groups; and G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12, R.sup.11 represents H or an alkyl group, R.sup.12 represents an alkyl group, and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids; and pharmaceutically acceptable salts thereof.
摘要翻译： 基质金属蛋白酶抑制剂，含有它们的药物组合物，以及使用它们治疗各种生理条件的方法。 目前要求保护的化合物具有其中每个T表示取代基的广义化学式“IMAGE”; x为0,1或2; D表示
delta为0或1; U'表示O，S或N，条件是当U'为N时，则δ= 0，当U'为O或S时，则δ= 1; R14是各种取代基中的任意一种; 和G表示M，其中M表示-CO 2 H，-CON（R 11）2或-CO 2 R 12，R 11表示H或烷基，R 12表示烷基，R 13表示任何侧链的M， 19个非环状天然存在的氨基酸; 及其药学上可接受的盐。 -
8.发明授权Substituted 4-biarylbutyric acid derivatives as matrix metalloprotease inhibitors 失效取代的4-联芳基丁酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5861428A
公开(公告)日：1999-01-19
申请号：US866680
申请日：1997-05-30
申请人： Harold Clinton Eugene Kluender , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , Jill Elizabeth Wood
发明人： Harold Clinton Eugene Kluender , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin , Jill Elizabeth Wood
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , A61K31/38 , A61K31/24 , A61K31/44
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaueutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each Tis a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 reresents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12, and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
摘要翻译： 用于基质金属蛋白酶的抑制剂，含有它们的制药组合物，以及使用它们处理各种生理条件的方法。 本发明的化合物具有通用化合物“IMAGE”，其中每个是取代基; x为0,1或2; 基团D表示
基团R6表示D和G之间的碳链上的各种可能的取代基，且基团G表示M，其中M表示-CO 2 H，-CON（R 11）2， 或-CO 2 R 12，R 13表示19个非环状天然存在的氨基酸的任一侧链。 -
9.发明授权Substituted 4-biarylbutyric acid derivatives as matrix metalloprotease inhibitors 失效取代的4-联芳基丁酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：US5861427A
公开(公告)日：1999-01-19
申请号：US866679
申请日：1997-05-30
申请人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , David Ross Brittelli , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin
发明人： Harold Clinton Eugene Kluender , Guenter Hans Herbert Heinz Benz , David Ross Brittelli , Brian Richard Dixon , Michael Christopher VanZandt , Scott McClelland Wilhelm , Donald John Wolanin
IPC分类号： A61K31/19 , A61K31/215 , A61K31/275 , A61K31/4035 , A61K31/47 , A61P35/00 , A61P43/00 , C07C17/12 , C07C17/16 , C07C17/20 , C07C22/04 , C07C25/18 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C57/38 , C07C59/48 , C07C59/56 , C07C59/68 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/145 , C07C69/616 , C07C69/63 , C07C69/712 , C07C69/738 , C07C69/757 , C07C205/34 , C07C205/56 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/18 , C07C235/84 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07D207/08 , C07D207/16 , C07D207/40 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/00 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/00 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07D498/04 , C07F9/141 , C07F9/40 , A61K31/40 , A61K31/535 , C07D241/00 , C07D265/30
CPC分类号： C07D207/08 , A61K31/4035 , A61K31/47 , C07C17/12 , C07C17/16 , C07C17/208 , C07C205/34 , C07C205/56 , C07C22/04 , C07C229/34 , C07C229/40 , C07C233/54 , C07C235/84 , C07C25/18 , C07C255/21 , C07C255/57 , C07C271/22 , C07C271/26 , C07C271/28 , C07C271/58 , C07C317/44 , C07C323/52 , C07C323/61 , C07C323/62 , C07C327/32 , C07C45/28 , C07C45/46 , C07C45/56 , C07C45/72 , C07C47/228 , C07C47/277 , C07C49/813 , C07C55/02 , C07C59/56 , C07C59/84 , C07C59/88 , C07C59/90 , C07C59/92 , C07C61/04 , C07C61/06 , C07C62/22 , C07C62/38 , C07C63/72 , C07C65/24 , C07C65/34 , C07C69/616 , C07C69/712 , C07C69/738 , C07C69/757 , C07D207/16 , C07D207/404 , C07D209/48 , C07D209/68 , C07D213/30 , C07D213/50 , C07D213/70 , C07D215/36 , C07D221/14 , C07D257/04 , C07D263/32 , C07D277/30 , C07D277/74 , C07D295/192 , C07D307/28 , C07D307/32 , C07D307/33 , C07D307/54 , C07D307/68 , C07D307/93 , C07D307/935 , C07D311/96 , C07D317/30 , C07D317/60 , C07D333/22 , C07D333/28 , C07D333/34 , C07D405/06 , C07D409/12 , C07D413/06 , C07D471/04 , C07D491/04 , C07F9/1415 , C07F9/4059 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要： Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
摘要翻译： 基质金属蛋白酶抑制剂，含有它们的药物组合物和使用它们的方法可以处理各种生理条件。 本发明的化合物具有通用化合物“IMAGE”，其中每个T是取代基; x为0,1或2; 基团D表示基团R6表示D和G之间的碳链上的各种可能的取代基，基团G表示M，其中M表示-CO 2 H，-CON（R 11）2， 或-CO 2 R 12; R13表示19个非环状天然氨基酸的任一侧链。
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10.发明授权1-pyrimidinylacetamide compounds which are inhibitors of human leukocyte elastase 失效作为人白细胞弹性蛋白酶抑制剂的1-嘧啶基乙酰胺化合物
公开(公告)号：US5736535A
公开(公告)日：1998-04-07
申请号：US375136
申请日：1995-01-19
申请人： Peter Robert Bernstein , Philip Duke Edwards , Andrew Shaw , Ashokkumar Bhikkappa Shenvi , Royston Martin Thomas , Chris Allan Veale , Peter Warner , Donald John Wolanin
发明人： Peter Robert Bernstein , Philip Duke Edwards , Andrew Shaw , Ashokkumar Bhikkappa Shenvi , Royston Martin Thomas , Chris Allan Veale , Peter Warner , Donald John Wolanin
IPC分类号： A61K38/55 , A61K38/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P29/00 , C07K5/06 , A61K31/69 , C07F5/02 , C07F5/04
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to certain novel substituted derivatives which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted derivatives, processes for preparing the substituted derivatives, pharmaceutical compositions containing such substituted derivatives and methods for their use.
摘要翻译： 本发明涉及作为人白细胞弹性蛋白酶（HLE）抑制剂（也称为人嗜中性粒细胞弹性蛋白酶（HNE））的式I的1-嘧啶基乙酰胺衍生物的某些新的取代衍生物，使其在这种抑制 是期望的，例如在药理学，诊断和相关研究中的研究工具以及涉及HLE的哺乳动物的疾病的治疗。 本发明还包括可用于合成这些取代衍生物的中间体，制备取代衍生物的方法，含有这种取代的衍生物的药物组合物及其使用方法。
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