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1. 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。

2. 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。

3. 发明授权

US5510367A Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US5510367A
公开(公告)日：1996-04-23
申请号：US351762
申请日：1994-12-08
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
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。

4. 发明授权

US5374649A 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：US5374649A
公开(公告)日：1994-12-20
申请号：US47430
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
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 A represents an unsubstituted ethenyl, group in the trans configuration, R.sub.1 represents a substituted phenyl 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化合物。其中A代表未取代的乙烯基，反式构型中的基团，R1代表兴奋性氨基酸拮抗剂的取代苯基，其制备方法及其在药物中的应用。

5. 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。

6. 发明授权

US5407931A Derivatives of 1-azatricyclo[7.2.03,8]undec-2-ene-2-carboxyclic acid 失效
标题翻译： 1-氮杂三环[7.2.03,8]十一碳-2-烯-2-羧酸的衍生物
公开(公告)号：US5407931A
公开(公告)日：1995-04-18
申请号：US578948
申请日：1990-09-07
申请人： Bruno Tamburini , Alcide Perboni , Tino Rossi , Daniele Donati , Daniele Andreotti , Giovanni Gaviraghi , Roberto Carlesso , Claudio Bismara
发明人： Bruno Tamburini , Alcide Perboni , Tino Rossi , Daniele Donati , Daniele Andreotti , Giovanni Gaviraghi , Roberto Carlesso , Claudio Bismara
IPC分类号： C07D487/04 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/407 , A61P31/04 , C07C45/71 , C07C49/753 , C07D205/08 , C07D477/00 , C07D487/00 , C07F7/18 , A01N43/00
CPC分类号： C07D477/00 , C07C45/71 , C07C49/753 , C07D205/08 , C07F7/186 , Y02P20/55
摘要： The invention relates to heterocyclic derivatives having antibacterial activity, to processes for their preparation, to compositions containing them, and to their medicinal uses. The derivatives according to the invention have the following general formula: ##STR1##
摘要翻译：本发明涉及具有抗菌活性的杂环衍生物，其制备方法，含有它们的组合物及其药用用途。根据本发明的衍生物具有以下通式：

7. 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。

8. 发明授权

US08865704B2 Wnt pathway antagonists 有权
标题翻译： Wnt途径拮抗剂
公开(公告)号：US08865704B2
公开(公告)日：2014-10-21
申请号：US13500582
申请日：2010-10-06
申请人： Maurizio Varrone , Arianna Nencini , Joanna Margaret Quinn , Andrea Caricasole , Annette Cornelia Bakker , Giovanni Gaviraghi , Massimilano Salerno
发明人： Maurizio Varrone , Arianna Nencini , Joanna Margaret Quinn , Andrea Caricasole , Annette Cornelia Bakker , Giovanni Gaviraghi , Massimilano Salerno
IPC分类号： C07D217/14 , C07D235/26 , C07D239/22 , C07D239/80 , C07D239/96 , A61K31/4166 , A61K31/4184 , A61K31/437 , A61K31/472 , A61K31/517 , A61K31/5377 , A61K31/5513 , C07D471/04 , C07D417/12 , C07D243/10 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/08 , C07D401/12 , C07D405/12
CPC分类号： C07D217/14 , C07D235/26 , C07D239/22 , C07D239/80 , C07D239/96 , C07D243/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/08 , C07D417/12 , C07D471/04
摘要： The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.
摘要翻译：本发明涉及本文所述的已知和新型式（I）化合物及其药物组合物。式（I）化合物对Wnt途径具有抑制作用，因此可用于制备药物，特别是用于治疗癌症。

9. 发明授权

US5587374A 10(1-hydroxyethyl)-11-oxo-1-azatricyclo/7.2.0.0..sup.3.8/ undec-2-ene-2-carboxylic acid esters and a process for preparing thereof 失效
标题翻译： 10（1-羟乙基）-11-氧代-1-氮杂三环/ 7.2.0.0.3.8 /十一碳-2-烯-2-羧酸酯及其制备方法
公开(公告)号：US5587374A
公开(公告)日：1996-12-24
申请号：US388515
申请日：1995-02-14
申请人： Alcide Perboni , Tino Rossi , Giovanni Gaviraghi , Giorgio Tarzia , Antonella Ursini
发明人： Alcide Perboni , Tino Rossi , Giovanni Gaviraghi , Giorgio Tarzia , Antonella Ursini
IPC分类号： A61K31/40 , A61K31/397 , A61K31/407 , A61P31/04 , C07D477/00 , C07D487/04 , C07D487/00 , A61K31/395
CPC分类号： C07D477/00
摘要： A compound of the formula 1-cyclohexyloxycarbonyloxethyl (4S, 8S, 9R 10S, 12R)-4-methoxy-10-(1-hydroxyethyl)-11-oxo-1-azatricyclo[7.2.0.0..sup.3,8 ]undec-2-ene-2-carboxylate which is useful as a pharmaceutical composition to treat bacterial infection.
摘要翻译：式1-环己基氧基羰基氧基乙基（4S，8S，9R 10S，12R）-4-甲氧基-10-（1-羟乙基）-11-氧代-1-氮杂环[7.2.0.0.3,8]十一烷-2 烯-2-羧酸盐，其可用作治疗细菌感染的药物组合物。

10. 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。

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