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1. 发明授权

US5407956A 2-amino-1,2,3,4-tetrahydronaphthalene derivatives active on the cardiovascular system, processes for their preparation and pharmaceutical compositions containing them 失效
标题翻译：在心血管系统上活性的2-氨基-1,2,3,4-四氢萘衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5407956A
公开(公告)日：1995-04-18
申请号：US32845
申请日：1993-03-17
申请人： Francesco Santangelo , Giorgio Bertolini , Cesare Casagrande , Francesco Marchini , Stefania Montanari , Claudio Semeraro
发明人： Francesco Santangelo , Giorgio Bertolini , Cesare Casagrande , Francesco Marchini , Stefania Montanari , Claudio Semeraro
IPC分类号： A61K31/135 , A61K31/165 , A61K31/215 , A61K31/66 , A61K31/675 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07C217/14 , C07C217/20 , C07C217/54 , C07C219/26 , C07C237/22 , C07C271/20 , C07C271/44 , C07D213/79 , C07F9/08 , C07F9/09
CPC分类号： C07C219/26 , C07C217/20 , C07C271/20 , C07C271/44 , C07C2102/10
摘要： Derivatives of 2-amino-1,2,3,4-tetrahydronaphthalene and their use in therapeutic field are described.The compounds are particularly useful in the treatment of arterial hypertension, cardiac decompensation and renal failure, in the treatment of peripheral arteriopathies and in cerebrovascular insufficiency.
摘要翻译：描述了2-氨基-1,2,3,4-四氢萘的衍生物及其在治疗领域中的应用。该化合物特别可用于治疗动脉高血压，心脏代偿失调和肾衰竭，用于治疗外周动脉病变和脑血管功能不全。

2. 发明授权

US5051432A Heterocyclic 1,4 dihydropyridine derivatives 失效
标题翻译：杂环1,4二氢吡啶衍生物
公开(公告)号：US5051432A
公开(公告)日：1991-09-24
申请号：US587159
申请日：1990-09-19
申请人： Claudio Semeraro , Dino Micheli , Daniele Pieraccioli , Giovanni Gaviraghi , Alan D. Borthwick
发明人： Claudio Semeraro , Dino Micheli , Daniele Pieraccioli , Giovanni Gaviraghi , Alan D. Borthwick
IPC分类号： A61K31/455 , A61P9/00 , A61P9/10 , C07D211/90
CPC分类号： C07D211/90
摘要： Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkyl group:R.sub.2 represents a group ##STR2## (where A is a bond or a methylene group and R.sub.7 is phenyl C.sub.1-4 alkyl; or R.sub.2 represents a group CH.sub.2 CH.sub.2 NR.sub.8 R.sub.9 (where R.sub.8 is hydrogen or C.sub.1-4 alkyl and R.sub.9 is C.sub.1-4 alkyl, phenyl C.sub.1-4 alkyl or benzoyl C.sub.1-4 alkyl); or R.sub.2 represents a C.sub.1-4 alkyl group substituted by nitrile.R.sub.3 represents a C.sub.1-6 straight or brached alkyl chain or alkoxy group;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substituent;R.sub.6 represents a halogen atom or a straight or branched C.sub.1-3 alkyl group.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion influx and thus may be useful for the treatment of cardiovascular disorders such as hypertension.
摘要翻译：化合物描述为式（I）其中R 1和R 4独立地表示C 1-4烷基：R 2表示基团（其中A是键或亚甲基，R 7是苯基C 1-4烷基 ;或R 2表示基团CH 2 CH 2 NR 8 R 9（其中R 8是氢或C 1-4烷基，R 9是C 1-4烷基，苯基C 1-4烷基或苯甲酰基C 1-4烷基）;或R 2表示被腈取代的C 1-4烷基 R 3表示C 1-6直链或直链烷基或烷氧基; R 5表示可被C 1-3烷基取代基取代的直链或支链C 1-13烷基或C 5-8环烷基; R 6表示卤素原子或直链或支链C 1-3烷基，由式（I）表示的化合物通过限制跨膜钙离子流入而减少细胞内钙离子浓度，因此可用于治疗心血管疾病如高血压。

3. 发明授权

US4963571A Pyridinedicarboxylic acid derivatives and pharmaceutical compositions 失效
标题翻译：吡啶二羧酸衍生物和药物组合物
公开(公告)号：US4963571A
公开(公告)日：1990-10-16
申请号：US272226
申请日：1988-11-16
申请人： Claudio Semeraro , Dino Micheli , Daniele Pieraccioli , Giovanni Gaviraghi , Alan D. Borthwick
发明人： Claudio Semeraro , Dino Micheli , Daniele Pieraccioli , Giovanni Gaviraghi , Alan D. Borthwick
IPC分类号： A61K31/455 , A61P9/00 , C07D211/90
CPC分类号： C07D211/90
摘要： Compounds are described of the formula ##STR1## wherein R.sub.1 and R.sub.4 independently represent a C.sub.1-4 alkyl group;R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight or branched alkyl chain or alkoxy group;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substituent;R.sub.6 represents a halogen atom or a straight or branched C.sub.1-3 alkyl group.R.sub.7 represents a C.sub.1-4 alkyl group [optionally substituted by hydroxy, C.sub.1-3 alkoxy or trifluoromethyl or by a group NR.sub.8 R.sub.9 where NR.sub.8 R.sub.9 forms a saturated 5 to 7 membered ring optionally containing an additional heleroatom which is oxygen]; or R.sub.7 represents a phenylC.sub.1-2 alkyl group in which the portion is optionally substituted by 1 to 3 C.sub.1-3 alkyl or C.sub.1-3 alkoxy groups or halogen atoms.The compounds representd by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion influx and thus may be useful for the treatment of cardiovascular disorders such as hypertension.

4. 发明授权

US4935548A 1.4-dihydropyridines 失效
标题翻译： 1,4-二氢吡啶
公开(公告)号：US4935548A
公开(公告)日：1990-06-19
申请号：US262240
申请日：1988-10-21
申请人： Claudio Semeraro , Dino Micheli , Daniele Pieraccioli , Giovanni Gaviraghi , Alan D. Borthwick
发明人： Claudio Semeraro , Dino Micheli , Daniele Pieraccioli , Giovanni Gaviraghi , Alan D. Borthwick
IPC分类号： A61K31/445 , A61K31/451 , A61P9/00 , C07D211/90
CPC分类号： C07D211/90
摘要： Compounds are described of the formula ##STR1## wherein R.sub.1 represents a formyl or nitrile group or a group OCH.sub.2 A where A represents hydroxy, C.sub.1-4 alkoxy or D(CH.sub.2).sub.n NR.sub.7 R.sub.8 (where R.sub.7 and R.sub.8 independently represent hydrogen or C.sub.1-4 alkyl and n is 2 or 3);R.sub.2 and R.sub.3 independently represent a C.sub.1-6 straight or branched alkyl chain or alkoxy group;R.sub.4 represents a C.sub.1-4 alkyl group;R.sub.5 represents a straight or branched chain C.sub.1-13 alkyl group or a C.sub.5-8 cycloalkyl group which may be substituted by a C.sub.1-3 alkyl substituent;R.sub.6 represents a halogen atom or a straight or branched C.sub.1-3 alkyl group.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion influx and thus may be useful for the treatment of cardiovascular disorders such as hypertension.
摘要翻译：描述式（I）的化合物，其中R1表示甲酰基或腈基或基团OCH2A，其中A表示羟基，C1-4烷氧基或D（CH2）nNR7R8（其中R7和R8独立地表示氢或C1- 4烷基，n为2或3）; R2和R3独立地表示C1-6直链或支链烷基链或烷氧基; R4代表C1-4烷基; R5表示可被C1-3烷基取代基取代的直链或支链C1-13烷基或C5-8环烷基; R 6表示卤素原子或直链或支链C 1-3烷基。由式（I）表示的化合物通过限制跨膜钙离子流入而降低细胞内钙离子浓度，因此可用于治疗心血管疾病如高血压。

5. 发明授权

US5994539A Mercapto acyl aminoacid derivatives endowed with dual ACE-NEP inhibitory activity, useful in the treatment of cardiovascular diseases 失效
标题翻译：巯基酰基氨基酸衍生物具有双重ACE-NEP抑制活性，可用于治疗心血管疾病
公开(公告)号：US5994539A
公开(公告)日：1999-11-30
申请号：US993567
申请日：1997-12-18
申请人： Franco Pellacini , Stefano Romagnano , Gabriele Norcini , Francesco Santangelo , Mario Fantucci , Claudio Semeraro
发明人： Franco Pellacini , Stefano Romagnano , Gabriele Norcini , Francesco Santangelo , Mario Fantucci , Claudio Semeraro
IPC分类号： A61P9/00 , C07C323/60 , C07C327/32 , C07D213/55 , C07D213/56 , C07D239/26 , C07D241/12 , C07D261/08 , C07D277/24 , C07D277/26 , C07D277/30 , C07D307/54 , C07D333/24 , C07D417/12 , A61K31/10 , A61K38/05 , C07C323/41
CPC分类号： C07C323/60 , C07C327/32 , C07D213/55 , C07D213/56 , C07D239/26 , C07D241/12 , C07D261/08 , C07D277/30 , C07D307/54 , C07D333/24 , C07D417/12
摘要： Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
摘要翻译：描述了其中R，R 1，R 2，R 3，R 4，m和n具有本说明书中报道的含义的方法及其制备方法和含有它们作为活性成分的药物组合物。式I化合物具有混合的ACE抑制和NEP抑制活性，可用于治疗心血管疾病。

6. 发明授权

US5716943A Phosphinic acid derivatives with metallopeptidase inhibitory activity 失效
标题翻译：具有金属肽酶抑制活性的次膦酸衍生物
公开(公告)号：US5716943A
公开(公告)日：1998-02-10
申请号：US671149
申请日：1996-06-06
申请人： Gabriele Norcini , Daniela Botta , Francesco Santangelo , Claudio Semeraro
发明人： Gabriele Norcini , Daniela Botta , Francesco Santangelo , Claudio Semeraro
IPC分类号： A61K31/66 , A61K31/665 , A61K31/67 , A61K31/675 , A61P9/00 , A61P43/00 , C07F9/30 , C07F9/58 , C07F9/6512 , C07F9/6539 , C07F9/655 , C07F9/6553 , C07F9/36
CPC分类号： C07F9/655345 , C07F9/301 , C07F9/588 , C07F9/65127 , C07F9/6539 , C07F9/65515 , C07F9/65517
摘要： Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and n have the meanings reported in the description are described. The compounds of formula I are endowed with a dual ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
摘要翻译：描述其中R，R 1，R 2，R 3，R 4和n具有说明书中报道的含义的式（I）的化合物。式I化合物具有双重ACE抑制和NEP抑制活性，可用于治疗心血管疾病。

7. 发明授权

US5070106A Compounds active on the cardiovascular system 失效
标题翻译：化合物在心脏血管系统上有活性
公开(公告)号：US5070106A
公开(公告)日：1991-12-03
申请号：US659542
申请日：1991-02-22
申请人： Cesare Casagrande , Gabriele Norcini , Francesco Santangelo , Claudio Semeraro
发明人： Cesare Casagrande , Gabriele Norcini , Francesco Santangelo , Claudio Semeraro
IPC分类号： A61K31/135 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/33 , A61K31/66 , A61P9/00 , A61P9/08 , A61P9/12 , A61P25/28 , C07C217/14 , C07C217/20 , C07C219/26 , C07C219/28 , C07C271/44 , C07D521/00 , C07F9/12
CPC分类号： C07C271/44 , C07C217/20 , C07F9/12 , C07C2102/10
摘要： Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2, R.sub.3, n, m, and p have the meanings reported in the specification), their preparation and the compositions for pharmaceutical use containing them as active ingredient are described.The compounds of formula I have dopaminergic vasodilator activity and they may be used in pharmaceutical field.

8. 发明授权

US4324788A Alkoxyalkylidenhydrazinopridazines and process for their preparation 失效
标题翻译：烷氧基亚氨基肼基吡嗪及其制备方法
公开(公告)号：US4324788A
公开(公告)日：1982-04-13
申请号：US142457
申请日：1980-04-21
申请人： Luciano Dorigotti , Giovanni Gaviraghi , Giorgio Pifferi , Mario Pinza , Claudio Semeraro
发明人： Luciano Dorigotti , Giovanni Gaviraghi , Giorgio Pifferi , Mario Pinza , Claudio Semeraro
IPC分类号： A61K31/50 , A61P9/08 , A61P9/12 , C07D237/22 , C07D405/12
CPC分类号： C07D237/22
摘要： There are described new alkoxyalkylidenhydrazinopyridazines having antihypertensive activity having the formula: ##STR1## wherein R is alkyl or cycloalkyl having up to 5 carbon atoms, optionally substituted with unsubstituted phenyl, substituted phenyl or cycloalkyl, R.sub.1 is hydrogen or alkyl having 1 to 3 carbon atoms and R.sub.2 is alkyl having 1 to 3 carbon atoms, a carboxylic group or phenyl and the process for their preparation.
摘要翻译：描述了具有抗高血压活性的新型烷氧基亚乙基肼哒嗪，具有下式：其中R是具有至多5个碳原子的烷基或环烷基，任选被未取代的苯基，取代的苯基或环烷基取代，R 1是氢或具有1至3个碳原子的烷基并且R 2是具有1至3个碳原子的烷基，羧基或苯基及其制备方法。

9. 发明授权

US06232348B1 Hydroxymethyl derivatives of 2-amino-1,2,3,4-tetrahydronaphthalene as cardiovascular agent 失效
标题翻译： 2-氨基-1,2,3,4-四氢萘的羟甲基衍生物作为心血管药
公开(公告)号：US06232348B1
公开(公告)日：2001-05-15
申请号：US09367358
申请日：1999-08-12
申请人： Stefania Montanari , Paolo Cavalleri , Francesco Santangelo , Cristina Fraire , Giancarlo Grancini , Napoletano Mauro , Francesco Marchini , Lorenzo Pradella , Claudio Semeraro
发明人： Stefania Montanari , Paolo Cavalleri , Francesco Santangelo , Cristina Fraire , Giancarlo Grancini , Napoletano Mauro , Francesco Marchini , Lorenzo Pradella , Claudio Semeraro
IPC分类号： A61K31135
CPC分类号： C07C215/64 , C07C317/32 , C07C2602/10
摘要： Compounds of formula (I) wherein R, R′, R″, R1, R2, R3, R4, R5, R6, X, Y, m, n, and p have the meanings reported in the description; and their pharmaceutically acceptable salts are described.
摘要翻译：其中R，R'，R“，R 1，R 2，R 3，R 4，R 5，R 6，X，Y，m，n和p具有说明书中报道的含义的式（I）及其药学上可接受的盐。

10. 发明授权

US6166051A Thiol derivatives with metallopeptidase (ACE/NEP) inhibitory activity 失效
标题翻译：具有金属肽酶（ACE / NEP）抑制活性的硫醇衍生物
公开(公告)号：US6166051A
公开(公告)日：2000-12-26
申请号：US91415
申请日：1998-06-23
申请人： Franco Pellacini , Stefano Romagnano , Gabriele Norcini , Francesco Santangelo , Claudio Semeraro
发明人： Franco Pellacini , Stefano Romagnano , Gabriele Norcini , Francesco Santangelo , Claudio Semeraro
IPC分类号： C07D213/55 , C07D277/30 , C07D333/24 , A61K31/44 , A61K31/426 , C07D213/04
CPC分类号： C07D333/24 , C07D213/55 , C07D277/30
摘要： Compounds of formula (I) wherein R, R.sub.1, R.sub.2, R.sub.3 have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases. ##STR1##
摘要翻译： PCT No.PCT / EP96 / 05496 Sec。 371日期1998年6月23日第 102（e）1998年6月23日PCT 1996年12月9日PCT PCT。公开号WO97 / 24341 日期1997年7月10日描述了其中R，R 1，R 2，R 3具有本说明书中报道的含义，其制备方法和含有它们作为活性成分的药物组合物的式（I）化合物。式（I）化合物具有混合的ACE抑制和NEP抑制活性，可用于治疗心血管疾病。

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