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1.发明授权Process for the preparation of cis, endo-2-azabicyclo-[3.3.0]-octane-3-carboxylic acids 失效顺式，内-2-氮杂双环[3.3.0] - 辛烷-3-羧酸的制备方法
公开(公告)号：US4879403A
公开(公告)日：1989-11-07
申请号：US267753
申请日：1988-11-02
IPC分类号： C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0222 , C07D209/52 , A61K38/00
摘要： Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
摘要翻译： 其中碳原子3上的羧基相对于顺式构型的双环体系位于内部位置的式I（I）化合物，其中R 1表示氢，烯丙基，乙烯基或 可以被保护的天然存在的α-氨基酸的侧链，R2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z表示氧，X表示烷基，烯基 或环烷基，或任选被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基单，二或三取代的芳基，或表示吲哚-3-基，其制备方法， 含有这些化合物的药剂及其用途。
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2.发明授权Cis, endo-2-azabicyclo-[3.3.0]-octane-3-carboxylic acids, a process for their preparation, agents containing these compounds and their use 失效（3.3.0）-OCTANE-3-羧酸，其制备方法，包含这些化合物的试剂及其用途
公开(公告)号：US5061722A
公开(公告)日：1991-10-29
申请号：US296513
申请日：1989-01-12
IPC分类号： C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0222 , C07D209/52 , A61K38/00
摘要： Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and 2 denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
摘要翻译： 其中碳原子3上的羧基相对于顺式构型的双环体系位于内部位置的式I（I）化合物，其中R 1表示氢，烯丙基，乙烯基或 可以被保护的天然存在的α-氨基酸的侧链，R2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z表示氧，X表示烷基，烯基 或环烷基，或任选被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基单，二或三取代的芳基，或表示吲哚-3-基，其制备方法， 含有这些化合物的药剂及其用途。
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3.发明授权
公开(公告)号：US4727160A
公开(公告)日：1988-02-23
申请号：US658902
申请日：1984-10-09
IPC分类号： C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0222 , C07D209/52 , A61K38/00
摘要： Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
摘要翻译： 其中碳原子3上的羧基相对于顺式构型的双环体系位于内部位置的式I（I）化合物，其中R 1表示氢，烯丙基，乙烯基或 可以被保护的天然存在的α-氨基酸的侧链，R2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z表示氧，X表示烷基，烯基 或环烷基，或任选被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基单，二或三取代的芳基，或表示吲哚-3-基，其制备方法， 含有这些化合物的药剂及其用途。
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4.发明授权Cis, endo-2-azabicyclo-[3.3.0]-octane-5-carboxylic acids 失效CIS，ENDO-2-AZABICYCLO-（3.3.0）-OCTANE-5-CARBOXYLIC ACIDS
公开(公告)号：US5053519A
公开(公告)日：1991-10-01
申请号：US318519
申请日：1989-02-28
IPC分类号： C07C227/08 , A61K31/40 , A61K31/403 , A61K38/00 , A61P9/12 , C07C227/10 , C07C227/16 , C07C229/36 , C07C237/06 , C07D209/52 , C07D451/04 , C07K5/02 , C07K5/06
CPC分类号： C07K5/0222 , C07D209/52 , A61K38/00
摘要： Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
摘要翻译： 其中碳原子3上的羧基相对于顺式构型的双环体系位于内部位置的式I（I）化合物，其中R 1表示氢，烯丙基，乙烯基或 可以被保护的天然存在的α-氨基酸的侧链，R2表示氢，烷基，烯基或芳烷基，Y表示氢或羟基，Z表示氢，或Y和Z表示氧，X表示烷基，烯基 或环烷基，或任选被烷基，烷氧基，羟基，卤素，硝基，氨基，烷基氨基，二烷基氨基或亚甲二氧基单，二或三取代的芳基，或表示吲哚-3-基，其制备方法， 含有这些化合物的药剂及其用途。
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公开(公告)号：US5684016A
公开(公告)日：1997-11-04
申请号：US445543
申请日：1995-05-22
IPC分类号： A61K38/00 , A61K38/55 , C07K5/02 , A61K31/47 , C07D217/26
CPC分类号： C07K5/0222 , A61K38/556
摘要： The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each denote hydrogen or an organic radical and R.sup.4 and R.sup.5, together with the atoms carrying them, form a mono-, bi- or tri-cyclic heterocyclic ring system. The invention furthermore relates to compounds of the formula I and agents containing these for use in the treatment of the abovementioned disease.
摘要翻译： 本发明涉及通过使用其中n为1或2的式I（I）的化合物治疗心功能不全的方法，R 1，R 2，R 2和R 3相同或不同，并且各自表示氢或有机基团 并且R4和R5与携带它们的原子一起形成单环，双环或三环杂环体系。 本发明还涉及式I化合物和含有这些化合物用于治疗上述疾病的药剂。
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6.发明授权Method of treating cardiac insufficiency using angiotensin-converting enzyme inhibitors 失效使用血管紧张素转换酶抑制剂治疗心功能不全的方法
公开(公告)号：US5403856A
公开(公告)日：1995-04-04
申请号：US188745
申请日：1994-01-31
IPC分类号： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , A61P43/00 , C07K5/02 , C07K5/06 , C12N9/99 , A61K31/40
CPC分类号： A61K38/556 , C07K5/0222 , Y10S514/913
摘要： The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each denote hydrogen or an organic radical and R.sup.4 R.sup.5, together with the atoms carrying them, form a mono-, bi- or tri-cyclic heterocyclic ring system. The invention furthermore relates to compounds of the formula I and agents containing these for use in the treatment of the abovementioned disease.
摘要翻译： 本发明涉及通过使用其中n为1或2的式I（I）的化合物治疗心功能不全的方法，R 1，R 2，R 2和R 3相同或不同，并且各自表示氢或有机基团 和R4 R5与携带它们的原子一起形成单环，双环或三环杂环体系。 本发明还涉及式I化合物和含有这些化合物用于治疗上述疾病的药剂。
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公开(公告)号：US5158959A
公开(公告)日：1992-10-27
申请号：US565900
申请日：1983-12-27
IPC分类号： A61K38/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/47 , A61K31/472 , A61P9/12 , C07D209/42 , C07D217/26 , C07D233/64 , C07D241/20 , C07D307/54 , C07D309/10 , C07D317/66 , C07D333/24 , C07D335/02 , C07D339/08 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/078 , C07K14/81
CPC分类号： C07K5/0222 , C07D217/26 , A61K38/00
摘要： What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.
摘要翻译： 所公开的是下式的氨基酸化合物，其中n为0或1，及其盐，所述化合物和具有降血压性质的盐; 制备化合物的方法; 含有该化合物或盐的药物组合物; 以及使用化合物和盐治疗高血压。
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公开(公告)号：US5747504A
公开(公告)日：1998-05-05
申请号：US709286
申请日：1996-09-06
CPC分类号： C07K5/0222 , A61K38/556
摘要： The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each denote hydrogen or an organic radical and R.sup.4 and R.sup.5, together with the atoms carrying them, form a mono-, bi- or tri-cyclic heterocyclic ring system. The invention furthermore relates to compounds of the formula I and agents containing these for use in the treatment of the abovementioned disease.
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9.发明授权Aminoacid derivatives, a process for their preparation, agents containing these compounds, and the use thereof 失效氨基酸衍生物，其制备方法，含有这些化合物的试剂及其用途
公开(公告)号：US5401766A
公开(公告)日：1995-03-28
申请号：US208443
申请日：1994-03-09
IPC分类号： A61K38/00 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/47 , A61K31/472 , A61P9/12 , C07D209/42 , C07D217/26 , C07D233/64 , C07D241/20 , C07D307/54 , C07D309/10 , C07D317/66 , C07D333/24 , C07D335/02 , C07D339/08 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/078 , C07K14/81 , C07D209/34 , A61K31/405
CPC分类号： C07K5/0222 , C07D217/26 , A61K38/00
摘要： Aminoacid derivatives of the formula I ##STR1## A , n, R.sup.1, R.sup.2 and R.sup.3 have the meanings given, and salts thereof, a process for their preparation, pharmaceutical preparations based on these compounds, and their use as medicaments.
摘要翻译： 式I的氨基酸衍生物A，n，R 1，R 2和R 3具有给定的含义及其盐，其制备方法，基于这些化合物的药物制剂及其作为药物的用途。
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公开(公告)号：US5162362A
公开(公告)日：1992-11-10
申请号：US565887
申请日：1983-12-27
IPC分类号： A61K38/00 , C07D217/26 , C07K5/02
CPC分类号： C07K5/0222 , C07D217/26 , A61K38/00
摘要： What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.
摘要翻译： 所公开的是下式的氨基酸化合物，其中n为0或1，及其盐，所述化合物和具有降血压性质的盐; 制备化合物的方法; 含有该化合物或盐的药物组合物; 以及使用化合物和盐治疗高血压。
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