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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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2.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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5.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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公开(公告)号：US4624962A
公开(公告)日：1986-11-25
申请号：US697340
申请日：1985-02-01
IPC分类号： C07C275/16 , C07C67/00 , C07C239/00 , C07C275/24 , C07C279/14 , C07C301/00 , C07C303/40 , C07C311/30 , C07C313/00 , C07C315/04 , C07C317/50 , C07C323/44 , C07C323/57 , C07C323/59 , C07D207/16 , C07D207/22 , C07D209/20 , C07D209/42 , C07D209/52 , C07D211/60 , C07D213/55 , C07D217/12 , C07D217/26 , C07D223/06 , C07D231/12 , C07D233/54 , C07D277/06 , C07D333/24 , C07D333/60 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/04 , C07D495/04 , A61K31/40
CPC分类号： C07D231/12 , C07C275/24 , C07C323/44 , C07D207/16 , C07D207/22 , C07D209/20 , C07D209/42 , C07D209/52 , C07D211/60 , C07D213/55 , C07D217/26 , C07D223/06 , C07D233/64 , C07D277/06 , C07D333/24 , C07D333/60 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/04 , C07D495/04 , C07C2101/04 , C07C2101/08
摘要： Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.sup.6 denotes hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, optionally monosubstituted or disubstituted phenyl or naphthyl, their salts, a process for their preparation and their use as medicaments.
摘要翻译： 式I的化合物其中n表示0-3，R1和R1'相同或不同，表示氢，烷基或链烯基，苯基或苄基，各自根据需要取代; R2表示氢，烷基或烯基; R3表示氢，烷基，羟基烷基，烷氧基烷基或氨基烷基，烷酰基氨基烷基，胍基烷基，咪唑基烷基，吲哚基烷基，巯基烷基或烷硫基烷基，苯基烷基，羟基苯基烷基，苯氧基烷基或苯硫基烷基，或R2和R3与携带它们的C和N原子一起表示饱和 或不饱和的4至8元单环或8至10元双环的单环或杂环，任选被羟基，具有1至3个C原子的烷氧基或烷基单取代或二取代，R4表示氢，烷基，烯基，链烯基，炔基， 链烯基或烷撑基，环烷基，苯基，苄基，苯乙基或苯基丙基，它们各自可以任选被单取代或二取代; R5表示氢或烷基，羟基或烷氧基，R6表示氢，任选取代的烷基，环烷基，烯基，任选单取代或二取代的苯基或萘基，它们的盐，其制备方法及其作为药物的用途。
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公开(公告)号：US4515803A
公开(公告)日：1985-05-07
申请号：US413663
申请日：1982-09-01
IPC分类号： C07C275/16 , C07C67/00 , C07C239/00 , C07C275/24 , C07C279/14 , C07C301/00 , C07C303/40 , C07C311/30 , C07C313/00 , C07C315/04 , C07C317/50 , C07C323/44 , C07C323/57 , C07C323/59 , C07D207/16 , C07D207/22 , C07D209/20 , C07D209/42 , C07D209/52 , C07D211/60 , C07D213/55 , C07D217/12 , C07D217/26 , C07D223/06 , C07D231/12 , C07D233/54 , C07D277/06 , C07D333/24 , C07D333/60 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/04 , C07D495/04 , C07D209/12
CPC分类号： C07D231/12 , C07C275/24 , C07C323/44 , C07D207/16 , C07D207/22 , C07D209/20 , C07D209/42 , C07D209/52 , C07D211/60 , C07D213/55 , C07D217/26 , C07D223/06 , C07D233/64 , C07D277/06 , C07D333/24 , C07D333/60 , C07D401/12 , C07D403/12 , C07D409/12 , C07D471/04 , C07D495/04 , C07C2101/04 , C07C2101/08
摘要： Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxyphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.sup.6 denotes hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, optionally monosubstituted or disubstituted phenyl or naphthyl,their salts, a process for their preparation and their use as medicaments.
摘要翻译： 式I的化合物其中n表示0-3，R1和R1'相同或不同，表示氢，烷基或链烯基，苯基或苄基，各自根据需要取代; R2表示氢，烷基或烯基; R3表示氢，烷基，羟基烷基，烷氧基烷基或氨基烷基，烷酰基氨基烷基，胍基烷基，咪唑基烷基，吲哚基烷基，巯基烷基或烷硫基烷基，苯基烷基，羟基苯基烷基，苯氧基烷基或苯硫基烷基，或R2和R3与携带它们的C和N原子一起表示饱和 或不饱和的4至8元单环或8至10元双环的单环或杂环，任选被羟基，具有1至3个C原子的烷氧基或烷基单取代或二取代，R4表示氢，烷基，烯基，链烯基，炔基， 链烯基或烷撑基，环烷基，苯基，苄基，苯乙基或苯基丙基，它们各自可以任选被单取代或二取代; R5表示氢或烷基，羟基或烷氧基，R6表示氢，任选取代的烷基，环烷基，烯基，任选单取代或二取代的苯基或萘基，它们的盐，其制备方法及其作为药物的用途。
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9.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：US5744496A
公开(公告)日：1998-04-28
申请号：US359860
申请日：1994-12-20
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 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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10.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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