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公开(公告)号：US5554756A
公开(公告)日：1996-09-10
申请号：US391380
申请日：1995-02-17
IPC分类号： A61K31/13 , A61K31/33 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/495 , A61K38/00 , A61P31/12 , A61P43/00 , C07C237/10 , C07C237/22 , C07C291/02 , C07C311/05 , C07C311/18 , C07C317/48 , C07C323/60 , C07D207/16 , C07D209/42 , C07D209/48 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/04 , C07D277/06 , C07D279/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D521/00 , C07K5/02 , C07D211/32
CPC分类号： C07D401/12 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/06 , C07D279/06 , C07D403/12 , C07D471/04 , C07K5/021
摘要： Compositions containing compounds ##STR1## and their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment or prophylaxis of viral infections. They can be manufactured according to generally known procedures.
摘要翻译： 含有化合物的组合物及其药学上可接受的酸加成盐抑制病毒来源的蛋白酶，并且可以用作治疗或预防病毒感染的药物。 它们可以根据通常已知的方法制造。
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公开(公告)号：US5157041A
公开(公告)日：1992-10-20
申请号：US362621
申请日：1989-06-05
IPC分类号： A61K31/13 , A61K31/33 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/495 , A61K38/00 , A61P31/12 , A61P43/00 , C07C237/10 , C07C237/22 , C07C291/02 , C07C311/05 , C07C311/18 , C07C317/48 , C07C323/60 , C07D207/16 , C07D209/42 , C07D209/48 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/04 , C07D277/06 , C07D279/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D521/00 , C07K5/02
CPC分类号： C07D401/12 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/06 , C07D279/06 , C07D403/12 , C07D471/04 , C07K5/021
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, cycloalkylcarbonyl, aralkanoyl, aroyl, heterocyclylcarbonyl, alkylsulphonyl, arylsulphonyl, monoaralkylcarbamoyl, cinnamoyl or .alpha.-aralkoxycarbonylaminoalkanoyl and R.sup.2 is hydrogen or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent a cyclic imide group of the formula ##STR2## in which P and Q together represent an aromatic system; R.sup.3 is alkyl, cycloalkyl, aryl, aralkyl, heterocyclylalkyl, cyanoalkyl, alkyl- sulphinylalkyl, carbamoylalkyl or alkoxycarbonylalkyl or, when n stands for zero, R.sup.3 can also represent alkylthioalkyl or, when n stands for 1, R.sup.3 can also represent alkylsulphonylalkyl; R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; R.sup.5 is hydrogen and R.sup.6 is hydroxy or R.sup.5 and R.sup.6 together represent oxo; R.sup.7 and R.sup.8 together represent a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycar- bonyl)--, --N(alkyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring; and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR3## in which R.sup.10 and R.sup.11 each represent alkyl; and their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment or prophylaxis of viral infections. They can be manufactured according to generally known procedures.
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公开(公告)号：US5620987A
公开(公告)日：1997-04-15
申请号：US398478
申请日：1995-04-10
IPC分类号： A61K31/13 , A61K31/33 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/495 , A61K38/00 , A61P31/12 , A61P43/00 , C07C237/10 , C07C237/22 , C07C291/02 , C07C311/05 , C07C311/18 , C07C317/48 , C07C323/60 , C07D207/16 , C07D209/42 , C07D209/48 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/04 , C07D277/06 , C07D279/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D521/00 , C07K5/02 , C07D217/16
CPC分类号： C07D401/12 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/06 , C07D279/06 , C07D403/12 , C07D471/04 , C07K5/021
摘要： Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and --N(R.sup.7)--CH(R.sup.8)(R.sup.9) are as claimed herein or their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment of viral infections. They can be manufactured according to generally known procedures.
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公开(公告)号：US5446161A
公开(公告)日：1995-08-29
申请号：US916812
申请日：1992-07-20
IPC分类号： A61K31/13 , A61K31/33 , A61K31/40 , A61K31/401 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/425 , A61K31/426 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/495 , A61K38/00 , A61P31/12 , A61P43/00 , C07C237/10 , C07C237/22 , C07C291/02 , C07C311/05 , C07C311/18 , C07C317/48 , C07C323/60 , C07D207/16 , C07D209/42 , C07D209/48 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/04 , C07D277/06 , C07D279/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D521/00 , C07K5/02 , C07D211/40 , C07D211/36 , C07D211/56
CPC分类号： C07D401/12 , C07D207/16 , C07D209/42 , C07D209/52 , C07D211/60 , C07D215/48 , C07D217/26 , C07D241/04 , C07D277/06 , C07D279/06 , C07D403/12 , C07D471/04 , C07K5/021
摘要： Compounds of the formula ##STR1## wherein and their pharmaceutically acceptable acid addition salts inhibit proteases of vital origin and can be used as medicaments for the treatment or prophylaxis of viral infections. They can be manufactured according to generally known procedures.
摘要翻译： 式Ⅰ的化合物及其药学上可接受的酸加成盐抑制重要起源的蛋白酶，并可用作治疗或预防病毒感染的药物。 它们可以根据通常已知的方法制造。
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公开(公告)号：US5571920A
公开(公告)日：1996-11-05
申请号：US592796
申请日：1996-01-26
IPC分类号： C07D209/48 , C07C247/04 , C07C247/06 , C07C247/10 , C07D217/26 , C07D303/36 , C07D327/10 , C07D333/36 , C07D401/06 , C07D405/06 , C07D217/00
CPC分类号： C07C247/04 , C07C247/06 , C07C247/10 , C07D209/48 , C07D217/26 , C07D303/36 , C07D327/10 , C07D401/06 , C07D405/06
摘要： Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
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公开(公告)号：US5488115A
公开(公告)日：1996-01-30
申请号：US439612
申请日：1995-05-12
IPC分类号： C07D209/48 , C07C247/04 , C07C247/06 , C07C247/10 , C07D217/26 , C07D303/36 , C07D327/10 , C07D333/36 , C07D401/06 , C07D405/06
CPC分类号： C07C247/04 , C07C247/06 , C07C247/10 , C07D209/48 , C07D217/26 , C07D303/36 , C07D327/10 , C07D401/06 , C07D405/06
摘要： Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
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公开(公告)号：US5580999A
公开(公告)日：1996-12-03
申请号：US439611
申请日：1995-05-12
IPC分类号： C07D209/48 , C07C247/04 , C07C247/06 , C07C247/10 , C07D217/26 , C07D303/36 , C07D327/10 , C07D333/36 , C07D401/06 , C07D405/06
CPC分类号： C07C247/04 , C07C247/06 , C07C247/10 , C07D209/48 , C07D217/26 , C07D303/36 , C07D327/10 , C07D401/06 , C07D405/06
摘要： Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, -N(alkoxycarbonyl)-,-N(acyl)- or --S--or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
摘要翻译： 式（I）的新型醇，其中R a是叠氮基或邻苯二甲酰亚氨基，R 4是烷基，环烷基，环烷基烷基，芳基或芳烷基，R 7和R 8一起是任选地被羟基，烷氧基羰基氨基或酰氨基取代的三亚甲基或四亚甲基， 其中一个-CH 2 - 基团被-NH-， - N（烷氧基羰基） - ， - N（酰基） - 或-S-取代，或带有稠合环烷烃，芳族或杂芳族环，R9是烷氧基羰基，单烷基氨基甲酰基，单烷基氨基甲酰基 单芳基氨基甲酰基或其中R10和R11各自为烷基的式“IMAGE”的基团以及其制备方法进行了描述。 这些醇可用作中间体，例如在制备具有抗病毒活性的氨基酸衍生物中。
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公开(公告)号：US5516913A
公开(公告)日：1996-05-14
申请号：US439604
申请日：1995-05-12
IPC分类号： C07D209/48 , C07C247/04 , C07C247/06 , C07C247/10 , C07D217/26 , C07D303/36 , C07D327/10 , C07D333/36 , C07D401/06 , C07D405/06 , C07D217/04
CPC分类号： C07C247/04 , C07C247/06 , C07C247/10 , C07D209/48 , C07D217/26 , C07D303/36 , C07D327/10 , C07D401/06 , C07D405/06
摘要： Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
摘要翻译： 式（I）的新型醇，其中R a是叠氮基或邻苯二甲酰亚氨基，R 4是烷基，环烷基，环烷基烷基，芳基或芳烷基，R 7和R 8一起是任选地被羟基，烷氧基羰基氨基或酰氨基取代的三亚甲基或四亚甲基， 其中一个-CH 2 - 基团被-NH-， - N（烷氧基羰基） - ， - N（酰基） - 或-S-取代，或带有稠合环烷烃，芳族或杂芳环，并且R 9是烷氧基羰基，单烷基氨基甲酰基，单烷基氨基甲酰基 单芳基氨基甲酰基或其中R10和R11各自为烷基的式“IMAGE”的基团以及其制备方法进行了描述。 这些醇可用作中间体，例如在制备具有抗病毒活性的氨基酸衍生物中。
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公开(公告)号：US5508430A
公开(公告)日：1996-04-16
申请号：US439606
申请日：1995-05-12
IPC分类号： C07D209/48 , C07C247/04 , C07C247/06 , C07C247/10 , C07D217/26 , C07D303/36 , C07D327/10 , C07D333/36 , C07D401/06 , C07D405/06 , C07D209/02
CPC分类号： C07C247/04 , C07C247/06 , C07C247/10 , C07D209/48 , C07D217/26 , C07D303/36 , C07D327/10 , C07D401/06 , C07D405/06
摘要： Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
摘要翻译： 式（I）的新型醇，其中R a是叠氮基或邻苯二甲酰亚氨基，R 4是烷基，环烷基，环烷基烷基，芳基或芳烷基，R 7和R 8一起是任选地被羟基，烷氧基羰基氨基或酰氨基取代的三亚甲基或四亚甲基， 其中一个-CH 2 - 基团被-NH-， - N（烷氧基羰基） - ， - N（酰基） - 或-S-取代，或带有稠合环烷烃，芳族或杂芳环，并且R 9是烷氧基羰基，单烷基氨基甲酰基，单烷基氨基甲酰基 单芳基氨基甲酰基或其中R10和R11各自为烷基的式“IMAGE”的基团以及其制备方法进行了描述。 这些醇可用作中间体，例如在制备具有抗病毒活性的氨基酸衍生物中。
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公开(公告)号：US5451678A
公开(公告)日：1995-09-19
申请号：US128978
申请日：1993-09-29
IPC分类号： C07D209/48 , C07C247/04 , C07C247/06 , C07C247/10 , C07D217/26 , C07D303/36 , C07D327/10 , C07D333/36 , C07D401/06 , C07D405/06 , C07D217/00
CPC分类号： C07C247/04 , C07C247/06 , C07C247/10 , C07D209/48 , C07D217/26 , C07D303/36 , C07D327/10 , C07D401/06 , C07D405/06
摘要： Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)-, --N(acyl)- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.
摘要翻译： 式（I）的新型醇，其中R a是叠氮基或邻苯二甲酰亚氨基，R 4是烷基，环烷基，环烷基烷基，芳基或芳烷基，R 7和R 8一起是任选地被羟基，烷氧基羰基氨基或酰氨基取代的三亚甲基或四亚甲基， 其中一个-CH 2 - 基团被-NH-， - N（烷氧基羰基） - ， - N（酰基） - 或-S-取代，或带有稠合环烷烃，芳族或杂芳环，并且R 9是烷氧基羰基，单烷基氨基甲酰基，单烷基氨基甲酰基 ，单芳基氨基甲酰基或其中R10和R11e为烷基的式“IMAGE”的基团以及其制备方法。 这些醇可用作中间体，例如在制备具有抗病毒活性的氨基酸衍生物中。
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