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11. 发明授权

US5374648A Indole derivatives and pharmaceutical use thereof 失效
标题翻译：吲哚衍生物及其药物用途
公开(公告)号：US5374648A
公开(公告)日：1994-12-20
申请号：US47429
申请日：1993-04-15
申请人： Alfredo Cugola , Giovanni Gaviraghi , Simone Giacobbe
发明人： Alfredo Cugola , Giovanni Gaviraghi , Simone Giacobbe
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/42 , C07D209/18 , A61K31/38 , C07D405/12
CPC分类号： C07D209/42 , Y02P20/55
摘要： The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.1 or COR.sub.1 wherein R.sub.1 represents hydroxy, methoxy, or amino; m is zero or an integer 1 or 2;A represents an ethynyl group or an optionally substituted ethenyl, orcyclopropyl group or a substituted ethenyl group;X represents --O-- or NH;R.sub.2 represents an aryl group and when X represents an oxygen atom R.sub.2 may also represent a hydrogen atom or an alkyl group; which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.
摘要翻译：本发明涉及式（I）的化合物，其中R表示选自卤素，烷基，烷氧基，氨基，烷基氨基，二烷基氨基，羟基，三氟甲基，三氟甲氧基，硝基，氰基，SO 2 R 1或COR 1中的基团，其中R 1表示羟基，甲氧基或氨基; m为零或整数1或2; A表示乙炔基或任选取代的乙烯基，或环丙基或取代的乙烯基; X表示-O-或NH; R2表示芳基，当X表示氧原子时，R2也可以表示氢原子或烷基; 它们是兴奋性氨基酸的拮抗剂，其制备方法及其在医学中的应用。

12. 发明授权

US5373018A Indole derivatives and pharmaceutical use thereof 失效
标题翻译：吲哚衍生物及其药物用途
公开(公告)号：US5373018A
公开(公告)日：1994-12-13
申请号：US46947
申请日：1993-04-15
申请人： Alfredo Cugola , Giovanni Gaviraghi
发明人： Alfredo Cugola , Giovanni Gaviraghi
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/30 , A61P43/00 , C07D20060101 , C07D209/42 , C07D209/18 , A61K31/535 , C07D413/12
CPC分类号： C07D209/42 , Y02P20/55
摘要： The invention relates to the compound of formula (I) ##STR1## wherein A represents an unsubstituted ethenyl group in the trans (E) configuration or a physiologically acceptable salt or metabilically labile ester thereof which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.
摘要翻译：本发明涉及式（I）化合物其中A表示反式（E）构型中的未取代的乙烯基或其生理学上可接受的盐或其稳定不稳定的酯，它们是兴奋性氨基酸的拮抗剂，其准备过程及其在医学中的应用。

13. 发明授权

US4806533A 1,4-Dihydro pyridine 3,5 dicarboxylic acid derivatives and compositions 失效
标题翻译： 1,4-二氢吡啶3.5二羧酸衍生物和组合物
公开(公告)号：US4806533A
公开(公告)日：1989-02-21
申请号：US16590
申请日：1987-02-19
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 , C07D211/90 , A61K31/535 , C07D401/06 , C07D413/06
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 phenyl 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 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R 1和R 4独立地表示C 1-4烷基; R2和R3独立地表示C1-6直链或支链烷基链或烷氧基; 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。 R 7表示C 1-4烷基[任选被羟基，C 1-3烷氧基或三氟甲基取代，或NR 8 R 9基团，其中NR 8 R 9形成饱和的5至7元环，任选地含有另外的氧原子是氧]。或R 7表示苯基C 1-2烷基，其中苯基部分任选被1至3个C 1-3烷基或C 1-3烷氧基或卤素原子取代。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。

14. 发明授权

US6071939A Medicaments for the treatment of hypertension 失效
标题翻译：药物治疗高血压
公开(公告)号：US6071939A
公开(公告)日：2000-06-06
申请号：US304884
申请日：1999-05-04
申请人： Giovanni Gaviraghi , Mauro Quartaroli
发明人： Giovanni Gaviraghi , Mauro Quartaroli
IPC分类号： A61K31/44 , A61K31/415
CPC分类号： A61K31/44
摘要： A composition comprising diethyl (E)-4-[2-[(tert-butyloxycarbonyl)vinyl]phenyl-1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate (lacidipine) and 4'-[[2-n-propyl-4-methyl-6 -(1-methylbenziimidazol-2-yl)-benzimidazol-1-yl]-methyl]-biphenyl-2 -carboxylic acid (telmisartan) or a physiologically functional derivative thereof.
摘要翻译：包含（E）-4- [2 - [（叔丁氧基羰基）乙烯基]苯基-1,4-二氢-2,6-二甲基吡啶-3,5-二羧酸二乙酯（拉西地平）和4' - [[2 - 正丙基-4-甲基-6-（1-甲基苯并咪唑-2-基） - 苯并咪唑-1-基] - 甲基] - 联苯-2-甲酸（替米沙坦）或其生理功能衍生物。

15. 发明授权

US5686461A Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US5686461A
公开(公告)日：1997-11-11
申请号：US507384
申请日：1995-09-18
申请人： Alfredo Cugola , Giovanni Gaviraghi , Fabrizio Micheli
发明人： Alfredo Cugola , Giovanni Gaviraghi , Fabrizio Micheli
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/435 , A61P25/00 , A61P43/00 , C07D209/42 , C07D453/02 , A61K31/44
CPC分类号： C07D209/42 , C07D453/02
摘要： The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R.sub.1 represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.3 or COR.sub.3 wherein R.sub.3 represents hydroxy, methoxy, or amino; m is zero or an integer 1 or 2; A represents an ethynyl group or an optionally substituted ethenyl group; X represents a bond or a C.sub.1-4 alkylene chain; R.sub.2 represents a bridged cycloalkyl or bridged heterocyclic group; which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.
摘要翻译： PCT No.PCT / EP94 / 00614 Sec。 371 1995年9月18日第 102（e）1995年9月18日PCT PCT 1994年3月3日PCT公布。公开号WO94 / 20465 日期：1994年9月15日本发明涉及式（I）化合物。其中R 1表示选自卤素，烷基，烷氧基，氨基，烷基氨基，二烷基氨基，羟基，三氟甲基，三氟甲氧基，硝基，氰基，SO 2 R 3或COR 3中的基团，其中R 3表示羟基，甲氧基或氨基; m为零或整数1或2; A表示乙炔基或任选取代的乙烯基; X表示键或C1-4亚烷基链; R 2表示桥连环烷基或桥连杂环基; 它们是兴奋性氨基酸的拮抗剂，其制备方法及其在医学中的应用。

16. 发明授权

US5455257A Lacidipine for the treatment of arteriosclerosis 失效
标题翻译：拉西地平用于治疗动脉硬化
公开(公告)号：US5455257A
公开(公告)日：1995-10-03
申请号：US94150
申请日：1993-08-11
申请人： Giovanni Gaviraghi
发明人： Giovanni Gaviraghi
IPC分类号： A61K31/455 , A61K31/44 , A61K31/4422 , A61P9/10
CPC分类号： A61K31/44
摘要： The invention relates to a method for the treatment of arteriosclerosis in a mammal which comprises administering to said mammal an effective amount of (E)-4-[2-[3-(1,1-dimethylethoxy)-3-oxo-1-propenyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid diethyl ester, lacidipine, as well as methods of treatment of arteriosclerosis which comprise administering to a mammal, especially a human, in need thereof, a pharmaceutical composition comprising lacidipine and a pharmaceutically acceptable carrier or excipient.
摘要翻译： PCT No.PCT / EP92 / 00276 Sec。 371日期：1993年8月11日 102（e）日期1993年8月11日PCT提交1992年2月8日PCT公布。出版物WO92 / 14460 PCT 本发明涉及一种治疗哺乳动物动脉硬化的方法，其包括向所述哺乳动物施用有效量的（E）-4- [2- [3-（1,1-二甲基乙氧基） -3-氧代-1-丙烯基]苯基] -1,4-二氢-2,6-二甲基-3,5-吡啶二羧酸二乙酯，拉西地平，以及治疗动脉硬化的方法，其包括向哺乳动物施用，特别是有需要的人，包含拉西地平和药学上可接受的载体或赋形剂的药物组合物。

17. 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。

18. 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.

19. 发明申请

US20080275028A1 Modulators or Alpha7 Nicotinic Acetylcholine Receptors and Therapeutic Uses Thereof 审中-公开
标题翻译：调节剂或α7烟碱乙酰胆碱受体及其治疗用途
公开(公告)号：US20080275028A1
公开(公告)日：2008-11-06
申请号：US11632545
申请日：2005-07-19
申请人： Giovanni Gaviraghi , Chiara Ghiron , Hendrik Bothmann , Renza Roncarati , Georg Christian Terstappenn
发明人： Giovanni Gaviraghi , Chiara Ghiron , Hendrik Bothmann , Renza Roncarati , Georg Christian Terstappenn
IPC分类号： A61K31/445 , C07D401/12 , C07D211/12 , C07D295/15 , C07D243/08 , C07D211/60 , C07D409/12 , C07D207/09 , A61P29/00 , A61P25/28 , A61P37/00 , A61P25/00 , A61K31/5375 , A61K31/55 , A61K31/551 , A61K31/496 , A61K31/495 , A61K31/4545
CPC分类号： C07D213/40 , C07D209/08 , C07D209/18 , C07D211/52 , C07D211/60 , C07D213/56 , C07D213/82 , C07D215/38 , C07D217/04 , C07D239/26 , C07D243/08 , C07D295/13 , C07D295/15 , C07D295/185 , C07D319/18 , C07D333/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/12
摘要： The present invention relates to compounds with α7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.
摘要翻译：本发明涉及具有α7nAChR激动活性的化合物，其制备方法，含有它们的药物组合物及其用于治疗神经，精神，认知，免疫学和炎症性疾病的用途。

20. 发明授权

US5162345A Heterocyclic compounds and their preparation and pharmaceutical formulation 失效
标题翻译：杂环化合物及其制备和药物制剂
公开(公告)号：US5162345A
公开(公告)日：1992-11-10
申请号：US673510
申请日：1990-08-20
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 , A61K31/495 , A61K31/535 , A61K31/54 , A61K31/55 , A61P3/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D211/90 , C07D401/06
CPC分类号： C07D401/06 , C07D211/90
摘要： Compounds are described of the formula: ##STR1## and physiologically acceptable salts thereof, in which R.sub.1 -R.sub.7 are defined hereinafter.The compounds represented by formula (I) reduce intracellular calcium ion concentration by limiting transmembranal calcium ion concentration and thus may be useful for the treatment of cardiovascular disorders such as hypertension.
摘要翻译：化合物由下式描述：其中R 1 -R 7在下文定义。由式（I）表示的化合物通过限制跨膜钙离子浓度来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。

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