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1. 发明授权

US5552408A Benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-ht receptor antagonists 失效
标题翻译：可用作5-ht受体拮抗剂的苯并咪唑啉-2-氧代-1-羧酸衍生物
公开(公告)号：US5552408A
公开(公告)日：1996-09-03
申请号：US432338
申请日：1994-05-01
申请人： Marco Turconi , Arturo Donetti , Ernesto Montagna , Massimo Nicola , Annamaria Uberti , Rosamaria Micheletti , Antonio Giachetti
发明人： Marco Turconi , Arturo Donetti , Ernesto Montagna , Massimo Nicola , Annamaria Uberti , Rosamaria Micheletti , Antonio Giachetti
IPC分类号： C07D401/12 , C07D451/12 , C07D451/14 , C07D453/02 , C07D453/06 , C07D487/08 , A61K31/46
CPC分类号： C07D401/12 , C07D451/12 , C07D451/14 , C07D453/02 , C07D453/06 , C07D487/08
摘要： A method for treating a human host suffering from psychosis, which method comprises administering to such host a therapeutically effective amount of a compound of the formula I ##STR1## wherein the radicals are defined in claim 1.
摘要翻译：用于治疗患有精神病的人宿主的方法，该方法包括向所述宿主施用治疗有效量的式I（I）化合物，其中所述基团如权利要求1所定义。

2. 发明授权

US5358954A Benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-HT receptor antagonists 失效
标题翻译：可用作5-HT受体拮抗剂的苯并咪唑啉-2-氧代-1-羧酸衍生物
公开(公告)号：US5358954A
公开(公告)日：1994-10-25
申请号：US33675
申请日：1993-03-16
申请人： Marco Turconi , Arturo Donetti , Ernesto Montagna , Massimo Nicola , Annamaria Uberti , Rosamaria Micheletti , Antonio Giachetti
发明人： Marco Turconi , Arturo Donetti , Ernesto Montagna , Massimo Nicola , Annamaria Uberti , Rosamaria Micheletti , Antonio Giachetti
IPC分类号： C07D401/12 , C07D451/12 , C07D451/14 , C07D453/02 , C07D453/06 , C07D487/08 , A61K31/46
CPC分类号： C07D401/12 , C07D451/12 , C07D451/14 , C07D453/02 , C07D453/06 , C07D487/08
摘要： Pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid compounds which are useful for treating a human host suffering from anxiety.
摘要翻译：可用于治疗患有焦虑的人宿主的药理学活性苯并咪唑啉-2-氧代-1-羧酸化合物。

3. 发明授权

US5223511A Benzimidazoline-2-oxo-1-carboxylic acid compounds useful as 5-HT receptor antagonists 失效
标题翻译：可用作5-HT受体拮抗剂的苯并咪唑啉-2-氧代-1-羧酸化合物
公开(公告)号：US5223511A
公开(公告)日：1993-06-29
申请号：US845891
申请日：1992-03-04
申请人： Marco Turconi , Arturo Donetti , Ernesto Montagna , Massimo Nicola , Annamaria Uberti , Rosamaria Micheletti , Antonio Giachetti
发明人： Marco Turconi , Arturo Donetti , Ernesto Montagna , Massimo Nicola , Annamaria Uberti , Rosamaria Micheletti , Antonio Giachetti
IPC分类号： C07D401/12 , C07D451/12 , C07D451/14 , C07D453/02 , C07D453/06 , C07D487/08
CPC分类号： C07D401/12 , C07D451/12 , C07D451/14 , C07D453/02 , C07D453/06 , C07D487/08
摘要： New pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid derivatives which are 5-HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents of the following formula: ##STR1##wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sub.1 is hydrogen; R.sub.2 is hydrogen, halogen or C.sub.1-6 alkoxy; Y is oxygen or N--R.sub.3 in which R.sub.3 is hydrogen; A is a group selected from: ##STR2##wherein p is 1; r is 0, 2 or 3: R.sub.4 is hydrogen; R.sub.5 is hydrogen, C.sub.1-6 alkyl, or R.sub.5 is a group of the formula --CR.sub.6 =N--R.sub.7 wherein R.sub.6 is hydrogen, C.sub.1-4 alkyl or amino and R.sub.7 is hydrogen or C.sub.1-6 alkyl; or a pharmaceutically acceptable acid addition salt thereof.The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions contained in them are also described.
摘要翻译：新的药理学活性苯并咪唑啉-2-氧代-1-羧酸衍生物，其是可用作止吐剂的5-HT受体拮抗剂和作为下式的胃促动力剂：其中R是氢，C 1-6烷基，C 2-6烯基或C 2-6炔基; R1是氢; R2是氢，卤素或C1-6烷氧基; Y是氧或N-R3，其中R3是氢; （a）选自下列的组：（a）（b）（c）（d）其中p为1; r为0,2或3：R4为氢; R5是氢，C1-6烷基或R5是式-CR6 = N-R7的基团，其中R6是氢，C1-4烷基或氨基，R7是氢或C1-6烷基; 或其药学上可接受的酸加成盐。还描述了制备式（I）化合物的方法以及其中所含的药物组合物。

4. 发明授权

US5047410A Indolyl derivatives and their use as 5-HT.sub.3, receptor antagonists 失效
标题翻译：吲哚衍生物及其作为5-HT3受体拮抗剂的用途
公开(公告)号：US5047410A
公开(公告)日：1991-09-10
申请号：US378958
申请日：1989-07-12
申请人： Arturo Donetti , Marco Turconi , Massimo Nicola , Rosamaria Micheletti
发明人： Arturo Donetti , Marco Turconi , Massimo Nicola , Rosamaria Micheletti
IPC分类号： C07C205/08 , A61K31/155 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/46 , A61P1/00 , A61P1/06 , A61P25/04 , A61P25/06 , A61P25/20 , A61P43/00 , C07C257/10 , C07C257/12 , C07C261/04 , C07C279/36 , C07C281/16 , C07D207/08 , C07D209/42 , C07D211/46 , C07D215/54 , C07D231/56 , C07D401/12 , C07D403/12 , C07D409/12 , C07D451/02 , C07D451/04 , C07D451/06 , C07D451/12 , C07D451/14 , C07D471/04 , C07D471/08
CPC分类号： C07D451/04 , C07C257/12 , C07C261/04 , C07C279/36 , C07D211/46 , C07D401/12 , C07D451/06 , C07D451/12 , C07D451/14
摘要： New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.

5. 发明授权

US4973592A 1,3-diazocycloalkenes as muscarinic receptor blocking agents 失效
标题翻译： 1,3-二氮杂环烯烃作为毒蕈碱受体阻断剂
公开(公告)号：US4973592A
公开(公告)日：1990-11-27
申请号：US243942
申请日：1988-09-13
申请人： Massimo Nicola , Arturo Donetti , Enzo Cereda , Marco Turconi , Giovanni B. Schiavi , Rosamaria Micheletti
发明人： Massimo Nicola , Arturo Donetti , Enzo Cereda , Marco Turconi , Giovanni B. Schiavi , Rosamaria Micheletti
IPC分类号： C07D233/14 , A61K31/415 , A61K31/4166 , A61K31/505 , A61P1/00 , A61P1/04 , A61P1/10 , A61P1/12 , A61P35/00 , A61P43/00 , C07D233/06 , C07D233/10 , C07D233/18 , C07D233/22 , C07D233/26 , C07D233/32 , C07D233/46 , C07D233/48 , C07D233/52 , C07D239/06 , C07D239/08 , C07D239/24 , C07D243/04
CPC分类号： C07D239/06 , C07D233/48 , C07D239/24
摘要： New pharmacologically active heterocyclic derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders, of the following formula ##STR1## wherein the substituents are defined hereinbelow.

6. 发明授权

US5252570A Amidino and guanidino derivatives 失效
标题翻译：脒基和胍基衍生物
公开(公告)号：US5252570A
公开(公告)日：1993-10-12
申请号：US707528
申请日：1991-05-30
申请人： Arturo Donetti , Marco Turconi , Massimo Nicola , Rosamaria Micheletti
发明人： Arturo Donetti , Marco Turconi , Massimo Nicola , Rosamaria Micheletti
IPC分类号： C07C257/12 , C07C261/04 , C07C279/36 , C07D211/46 , C07D401/12 , C07D451/04 , C07D451/06 , C07D451/12 , C07D451/14 , A61K31/435 , C07D221/02
CPC分类号： C07D451/04 , C07C257/12 , C07C261/04 , C07C279/36 , C07D211/46 , C07D401/12 , C07D451/06 , C07D451/12 , C07D451/14
摘要： New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## wherein the substituents are defined hereinbelow in the specification, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.
摘要翻译：新的药理学活性的脒基和胍基衍生物，其是用作下列通式（I）的止吐剂，胃促动力和抗偏头痛剂的5-HT 3受体拮抗剂，其中取代基在本说明书中定义，该化合物是可用作止吐胃促动力和抗偏头痛药物的5-HT 3受体拮抗剂。

7. 发明授权

US08269022B2 Polymorphs of enantiopure erdosteine 有权
标题翻译：对映体素奥曲斯汀的多态性
公开(公告)号：US08269022B2
公开(公告)日：2012-09-18
申请号：US12742679
申请日：2008-11-10
申请人： Pier Andrea Gatti , Matteo Zacche′ , Massimo Nicola
发明人： Pier Andrea Gatti , Matteo Zacche′ , Massimo Nicola
IPC分类号： C07D333/32
CPC分类号： C07D333/36
摘要： The present invention provides novel crystalline polymorphs of enantiopure Erdosteine, referred to as Form I and Form II, and processes for the preparation thereof.
摘要翻译：本发明提供了新的结构多晶型物，称为I型和II型对映体纯的二十一碳精，以及其制备方法。

8. 发明授权

US4579861A Aryloxypropanolamine derivatives, pharmaceutical compositions and adrenegic thereof 失效
标题翻译：丙烯酰氧基丙醇胺衍生物，药物组合物和其辅料
公开(公告)号：US4579861A
公开(公告)日：1986-04-01
申请号：US568598
申请日：1984-01-06
申请人： Cesare Casagrande , Massimo Nicola
发明人： Cesare Casagrande , Massimo Nicola
IPC分类号： A61K31/415 , A61K31/4166 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P25/02 , C07D233/72 , C07D303/22 , C07D405/04 , C07D233/30
CPC分类号： C07D303/22 , C07D233/72 , C07D405/04
摘要： Compounds having general formula I ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower alkoxy, alkyl enoxy, halogen, cyano, carboxyamido or ureido group optionally separated from the phenyl ring by a methylene or ethylene bridge;R.sub.2 is hydrogen, halogen, lower alkyl or alkoxy;R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or R.sub.2 and R.sub.3, taken together, are a methylendioxy group;R.sub.4 is hydrogen or lower alkyl,endowed with remarkable cardioselective .beta.-adrenolytic properties, are described.The process for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：具有通式I的化合物其中R 1为氢，低级烷基，低级烷氧基，烷氧基，卤素，氰基，羧基酰胺基或脲基，任选地通过亚甲基或乙烯桥与苯环分离; R2是氢，卤素，低级烷基或烷氧基; R 3是氢，卤素，低级烷基，低级烷氧基或R 2和R 3一起是甲基二氧基; R4是氢或低级烷基，具有显着的心脏选择性β-肾上腺素能性质。还描述了其制备方法和含有它们的药物组合物。

9. 发明授权

US5525628A Salts of a glutathione alkylester and anaminoacids 失效
标题翻译：谷胱甘肽烷基酯和氨基酸的盐
公开(公告)号：US5525628A
公开(公告)日：1996-06-11
申请号：US193140
申请日：1994-11-28
申请人： Massimo Nicola , Marco Inglesi , Giancarlo B. Fregnan , Guido Vandoni
发明人： Massimo Nicola , Marco Inglesi , Giancarlo B. Fregnan , Guido Vandoni
IPC分类号： C07K5/08 , A61K38/00 , C07K5/02 , A61K31/195
CPC分类号： C07K5/0215 , A61K38/00
摘要： Crystalline non-hygroscopic salt of glutathione alkylester of the formula (I) ##STR1## wherein AA is an amino acid are disclosed.
摘要翻译： PCT No.PCT / EP93 / 01462 Sec。 371日期：1994年11月28日 102（e）日期1994年11月28日PCT提交1993年6月9日PCT公布。第WO93 / 25573号公报日期：1993年12月23日。公开了式（I）的谷胱甘肽烷基酯的结晶非吸湿盐，其中AA是氨基酸。

10. 发明授权

US4508719A Hydroxyimino and alkoxyimino derivatives of 1,4-dihydropyridine and anti-hypertensive compositions 失效
标题翻译： 1,4-二氢吡啶和抗高血压组合物的羟基亚氨基和烷氧基亚氨基衍生物
公开(公告)号：US4508719A
公开(公告)日：1985-04-02
申请号：US498248
申请日：1983-05-26
申请人： Silvia Z. Tricerri , Cesare Casagrande , Franco De Marchi , Massimo Nicola
发明人： Silvia Z. Tricerri , Cesare Casagrande , Franco De Marchi , Massimo Nicola
IPC分类号： C07D209/48 , C07D211/90 , A61K31/535 , A61K31/455 , C07D211/82 , C07D413/12
CPC分类号： C07D209/48 , C07D211/90
摘要： Compounds of formula I: ##STR1## are described in which R.sup.1 is a linear or branched alkyl radical containing between 1 and 5 carbon atoms, the alkyl radical being unsubstituted or substituted by an alkoxy group; R.sup.2 is an unsubstituted phenyl of phenyl substituted by a nitro group; R.sup.3 is hydrogen or a linear or branched alkyl residue containing between 1 and 4 carbon atoms, the alkyl radical being unsubstituted or substituted by at least one alkoxy or fluorine atom or both alkoxy and fluorine atoms; R.sup.4 is hydrogen or a linear or branched alkyl containing between 1 and 4 carbon atoms, the alkyl radical being unsubstituted or substituted by alkoxy, carbalkoxy, dialkylamino, 1-aryl or 1-heteroarylpiperazinyl, aryl or a monocyclic 5 or 6 membered heterocycle in which at least one of the heteroatoms is N,O,S such as 1-piperidinyl, 4-morpholinyl or R.sub.4 is alkenyl or cyclo(C.sub.3 -C.sub.6)alkyl; and enantiomers, racemates, diastereoisomers and isomers (E) and (Z) and their salts with pharmaceutically acceptable acids.The novel compounds exhibit calcium-antagonistic activity.
摘要翻译：描述了式I化合物：其中R 1是含有1至5个碳原子的直链或支链烷基，该烷基是未取代的或被一个烷氧基取代; R2是被硝基取代的苯基的未取代的苯基; R3是氢或含有1至4个碳原子的直链或支链烷基，烷基是未取代的或被至少一个烷氧基或氟原子或烷氧基和氟原子所取代; R4是氢或含有1至4个碳原子的直链或支链烷基，该烷基是未取代的或被烷氧基，烷氧基，二烷基氨基，1-芳基或1-杂芳基哌嗪基，芳基或单环5或6元杂环取代，其中至少一个杂原子是N，O，S如1-哌啶基，4-吗啉基或R4是烯基或环（C 3 -C 6）烷基; 和对映异构体，外消旋体，非对映异构体和异构体（E）和（Z）及其与药学上可接受的酸的盐。新化合物显示钙拮抗活性。

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