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1. 发明授权

US4313950A Antireproductive tricyclic ortho-fused nitrogen containing compounds 失效
标题翻译：抗生素三环邻位稠合含氮化合物
公开(公告)号：US4313950A
公开(公告)日：1982-02-02
申请号：US230138
申请日：1981-01-30
申请人： Umberto Guzzi , Amedeo Omodei-Sale , Giulio Galliani
发明人： Umberto Guzzi , Amedeo Omodei-Sale , Giulio Galliani
IPC分类号： C07D217/24 , C07D223/16 , C07D471/04 , C07D487/04 , A61K31/47
CPC分类号： C07D223/16 , C07D217/24 , C07D471/04 , C07D487/04 , Y10S514/96
摘要： New tricyclic ortho-fused nitrogen containing compounds of the following formula: ##STR1## wherein R and R.sub.1 are independently selected from hydrogen, fluoro, chloro, bromo and (C.sub.1 -C.sub.4)alkoxy; A may be --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --(CH.sub.2).sub.3 --; X represents a nitrogen atom or the group CH; and salts therewith of pharmaceutically acceptable acids.The compounds possess an outstanding antireproductive utility.
摘要翻译：新的具有下式的三环邻 - 稠合氮化合物：其中R和R 1独立地选自氢，氟，氯，溴和（C 1 -C 4）烷氧基; A可以是-CH 2 - ， - CH 2 -CH 2 - ， - CH = CH - 或 - （CH 2）3 - ; X表示氮原子或基团CH; 以及其与药学上可接受的酸的盐。该化合物具有突出的抗生素效用。

2. 发明授权

US4275066A Antireproductive tricyclic ortho-fused nitrogen containing compounds 失效
标题翻译：抗生素三环邻位稠合含氮化合物
公开(公告)号：US4275066A
公开(公告)日：1981-06-23
申请号：US87371
申请日：1979-10-23
申请人： Umberto Guzzi , Amedeo Omodei-Sale' , Giulio Galliani
发明人： Umberto Guzzi , Amedeo Omodei-Sale' , Giulio Galliani
IPC分类号： A61K31/41 , A61K31/415 , A61K31/47 , A61K31/55 , A61P33/02 , C07D217/24 , C07D223/16 , C07D471/04 , C07D487/04
CPC分类号： C07D223/16 , C07D217/24 , C07D471/04 , C07D487/04 , Y10S514/96
摘要： New tricyclic ortho-fused nitrogen containing compounds of the following formula: ##STR1## wherein R and R.sub.1 are independently selected from hydrogen, fluoro, chloro, bromo and (C.sub.1 -C.sub.4)alkoxy; A may be --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --(CH.sub.2).sub.3 --; X represents a nitrogen atom or the group CH; and salts therewith of pharmaceutically acceptable acids.The compounds possess an outstanding antireproductive utility.
摘要翻译：新的具有下式的三环邻 - 稠合氮化合物：其中R和R 1独立地选自氢，氟，氯，溴和（C 1 -C 4）烷氧基; A可以是-CH 2 - ， - CH 2 -CH 2 - ， - CH = CH - 或 - （CH 2）3 - ; X表示氮原子或基团CH; 以及其与药学上可接受的酸的盐。该化合物具有突出的抗生素效用。

3. 发明申请

US20050222187A1 Use of benzoylalkyl-1,2,3,6-tetrahydropyridines 失效
标题翻译：苯甲酰烷基-1,2,3,6-四氢吡啶的使用
公开(公告)号：US20050222187A1
公开(公告)日：2005-10-06
申请号：US11135998
申请日：2005-05-24
申请人： Marco Baroni , Rosanna Cardamone , Jacqueline Fournier , Umberto Guzzi , Alessandra Ielmini
发明人： Marco Baroni , Rosanna Cardamone , Jacqueline Fournier , Umberto Guzzi , Alessandra Ielmini
IPC分类号： A61K31/44 , A61K31/4409 , A61K31/4418 , A61P25/00 , A61P43/00 , C07D211/70
CPC分类号： C07D211/70 , A61K31/4418
摘要： The invention relates to the use of compounds of formula for the preparation of medicines designed for the treatment of neuronal and cerebral disorders. The invention also relates to the compounds of formula: a process for their preparation and the pharmaceutical compositions containing them.
摘要翻译：本发明涉及式的化合物在制备用于治疗神经元和脑障碍的药物中的应用。本发明还涉及下式的化合物：其制备方法和含有它们的药物组合物。

4. 发明授权

US06649627B1 Phenoxylpropanolamines, method for the production thereof and pharmaceutical compositions containing the same 失效
标题翻译：苯氧基丙醇胺，其制备方法和含有它们的药物组合物
公开(公告)号：US06649627B1
公开(公告)日：2003-11-18
申请号：US09719640
申请日：2001-03-26
申请人： Roberto Cecchi , Tiziano Croci , Umberto Guzzi , Eric Marsault
发明人： Roberto Cecchi , Tiziano Croci , Umberto Guzzi , Eric Marsault
IPC分类号： A61K31445
CPC分类号： C07D303/22 , C07D307/42 , C07D401/04 , C07D401/06 , C07D405/14
摘要： The invention concerns compounds of formula (Ia) wherein R1a represents hydrogen, an —S(O)z —(C1-C4)Alk group, a —CO(C1-C4)Alk group, an —NHSO2—(C1-C4)Alk group, an NCHl (C1-C4) Alk group, a 2-furyl group or a halogen; R2 represents hydrogen or a (C1-C4)Alk group, a (C1-C4) alkoxyl group, a halogen, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NH2, —NHSO2(C1-C4)Alk; m and n are independently 0, 1 or 2; R3 and R4 independently represent hydrogen or a (C1-C4)Alk group; Z is 1 or 2 and their salts or solvates, the pharmaceutical compositions that contain them, the process for their preparation, and intermediate synthesis products.
摘要翻译：本发明涉及式（Ia）化合物，其中R 1a表示氢，-S（O）z - （C 1 -C 4）Alk基，-CO（C 1 -C 4）Alk基，-NHSO 2 - （C 1 -C 4）基团，NCH1（C1-C4）Alk基团，2-呋喃基或卤素; R2表示氢或（C1-C4）Alk基团，（C1-C4）烷氧基，卤素，-COOH， COO（C1-C4）Alk，-CN，-CONR3R4，-NO2，-SO2NH2，-NHSO2（C1-C4）Alk; m和n分别为0,1或2; R3和R4独立地表示氢或（C1 -C4）Alk基; Z为1或2及其盐或溶剂化物，含有它们的药物组合物，其制备方法和中间合成产物。

5. 发明授权

US06358965B1 Use of benzoylalkyl-1,2,3,6-tetrahydropyridines 失效
标题翻译：苯甲酰烷基-1,2,3,6-四氢吡啶的使用
公开(公告)号：US06358965B1
公开(公告)日：2002-03-19
申请号：US09331524
申请日：1999-08-05
申请人： Marco Baroni , Rosanna Cardamone , Jacqueline Fournier , Umberto Guzzi , Alessandra Ielmini
发明人： Marco Baroni , Rosanna Cardamone , Jacqueline Fournier , Umberto Guzzi , Alessandra Ielmini
IPC分类号： A61K31435
CPC分类号： C07D211/70 , A61K31/4418
摘要： The invention relates to the use of compounds of formula for the preparation of medicines designed for the treatment of neuronal and cerebral disorders. The invention also relates to the compounds of formula: a process for their preparation and the pharmaceutical compositions containing them.
摘要翻译：本发明涉及用于制备治疗神经元和脑疾病的药物的配方化合物的用途。本发明还涉及式的化合物：其制备方法和含有它们的药物组合物。

6. 发明授权

US6034090A 1-Phenylalkyl-1,2,3,6-tetrahydropyridines for treating Alzheimer's disease 失效
标题翻译： 1-苯基烷基-1,2,3,6-四氢吡啶用于治疗阿尔茨海默病
公开(公告)号：US6034090A
公开(公告)日：2000-03-07
申请号：US331006
申请日：1999-07-27
申请人： Marco Baroni , Rosanna Cardamone , Jacqueline Fournier , Umberto Guzzi
发明人： Marco Baroni , Rosanna Cardamone , Jacqueline Fournier , Umberto Guzzi
IPC分类号： A61K31/4418 , A61K31/444 , A61K31/445 , A61P25/28 , C07D211/70 , C07D213/36 , C07D401/04 , A61K31/44 , C07D211/72 , C07D213/22
CPC分类号： C07D401/04 , C07D211/70
摘要： The invention relates to compounds of the formula in which: Y is --CH-- or --N--; R.sub.1 is hydrogen, a halogen or a CF.sub.3, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy group; R.sub.2 is a methyl or ethyl group; R.sub.3 and R.sub.4 are each hydrogen or a (C.sub.1 -C.sub.3)alkyl; and X is:(a) a (C.sub.1 -C.sub.6)alkyl, a (C.sub.1 -C.sub.6)alkoxy, a (C.sub.3 -C.sub.7)carboxyalkyl, a (C.sub.1 -C.sub.4)alkoxy-carbonyl(C.sub.1 -C.sub.6)alkyl, a (C.sub.3 -C.sub.7)carboxyalkoxy or a (C.sub.1 -C.sub.4)alkoxycarbonyl-(C.sub.1 -C.sub.6)alkoxy;(b) a radical selected from (C.sub.3 -C.sub.7)cycloalkyl, (C.sub.3 -C.sub.7)cycloalkoxy, (C.sub.3 -C.sub.7)-cycloalkylmethyl, (C.sub.3 -C.sub.7)cycloalkylamino and cyclohexenyl, it being possible for said radical to be substituted by a halogen, hydroxyl, (C.sub.1 -C.sub.4)-alkoxy, carboxyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, amino or mono- or di-(C.sub.1 -C.sub.4)-alkylamino; or(c) a group selected from a phenyl, phenoxy, phenylamino, N-(C.sub.1 -C.sub.3)alkyl-phenylamino, phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulfonyl, phenylsulfinyl and styryl, it being possible for said group to be monosubstituted or polysubstituted on the phenyl group by a halogen, CF.sub.3, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, cyano, amino, mono- or di-(C.sub.1 -C.sub.4)alkyl-amino, (C.sub.1 -C.sub.4)acylamino, carboxyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, aminocarbonyl, mono- or di-(C.sub.1 -C.sub.4)alkylaminocarbonyl, amino(C.sub.1 -C.sub.4)alkyl, hydroxy(C.sub.1 -C.sub.4)alkyl or halogeno(C.sub.1 -C.sub.4)alkyl;to a method of preparing them and to the pharmaceutical compositions containing them. These compounds have neurotrophic and neuroprotective activity.
摘要翻译： PCT No.PCT / FR97 / 02286 Sec。 371日期：1999年7月27日 102（e）日期1997年7月27日PCT 1997年12月12日PCT PCT。第WO98 / 25903号公报日期：1998年6月18日本发明涉及下式的化合物，其中：Y为-CH-或-N-; R1是氢，卤素或CF3，（C1-C4）烷基或（C1-C4）烷氧基; R2是甲基或乙基; R3和R4各自为氢或（C1-C3）烷基; 并且X是：（a）（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 3 -C 7）羧基烷基，（C 1 -C 4）烷氧羰基（C 1 -C 6）烷基，（C 3 -C 7）羧基烷氧基或（C 1 -C 4）烷氧基羰基 - （C 1 -C 6）烷氧基; （c）选自（C 3 -C 7）环烷基，（C 3 -C 7）环烷氧基，（C 3 -C 7） - 环烷基甲基，（C 3 -C 7）环烷基氨基和环己烯基的基团，所述基团可以被卤素，羟基，（C 1 -C 4） - 烷氧基，羧基，（C 1 -C 4）烷氧基羰基，氨基或单 - 或二 - （C 1 -C 4） - 烷基氨基; 或（c）选自苯基，苯氧基，苯基氨基，N-（C1-C3）烷基 - 苯基氨基，苯基甲基，苯基乙基，苯基羰基，苯硫基，苯基磺酰基，苯基亚磺酰基和苯乙烯基的基团，所述基团可能是单取代的或通过卤素，CF 3，（C 1 -C 4）烷基，（C 1 -C 4）烷氧基，氰基，氨基，单 - 或二 - （C 1 -C 4）烷基 - 氨基，（C 1 -C 4）酰基氨基，羧基，（C 1 -C 4）烷氧基羰基，氨基羰基，单 - 或二 - （C 1 -C 4）烷基氨基羰基，氨基（C 1 -C 4）烷基，羟基（C 1 -C 4）烷基或卤代（C 1 -C 4）涉及制备它们的方法和含有它们的药物组合物。这些化合物具有神经营养和神经保护活性。

7. 发明授权

US5719308A Enzymatic process for the preparation of optically active tetralin derivatives 失效
标题翻译：用于制备光学活性四氢化萘衍生物的酶法
公开(公告)号：US5719308A
公开(公告)日：1998-02-17
申请号：US685488
申请日：1996-07-24
申请人： Roberto Cecchi , Laura Barzaghi , Umberto Guzzi
发明人： Roberto Cecchi , Laura Barzaghi , Umberto Guzzi
IPC分类号： C07C51/09 , C07C62/14 , C07C62/34 , C12P7/40 , C12P41/00 , C07C69/76
CPC分类号： C07C62/34 , C07C62/14 , C12P41/005 , C12P7/40
摘要： The present invention relates to an enzymatic process for the preparation of optically active tetrahydro-2-naphthoic acids from the corresponding racemic esters by reaction with a lipase.
摘要翻译：本发明涉及通过与脂肪酶反应从相应的外消旋酯制备光学活性的四氢-2-萘甲酸的酶法。

8. 发明授权

US5599941A N-substituted trifluoromethylphenyltetrahydropyridines process for the preparation thereof intermediates in said process and pharmaceutical compositions containing them 失效
标题翻译： N-取代的三氟甲基苯基四氢吡啶用于制备所述方法中的中间体和含有它们的药物组合物
公开(公告)号：US5599941A
公开(公告)日：1997-02-04
申请号：US455207
申请日：1995-05-31
申请人： Umberto Guzzi , Constantino Palmieri , Tiziano Croci
发明人： Umberto Guzzi , Constantino Palmieri , Tiziano Croci
IPC分类号： A61K31/435 , A61K31/44 , A61K31/4427 , A61P1/10 , A61P25/24 , A61P25/26 , C07D211/70 , C07D401/04 , C07D401/06
CPC分类号： C07D401/06 , C07D211/70
摘要： New N-substituted 4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridines useful in the treatment of intestinal motility disorders, of the following general formula ##STR1## wherein A represents a group -E-G or -L-M, where-E- is a straight or branched alkylene radical of from 2 to 4 carbon atoms,-G represents a radical selected from the group consisting of naphthyl mono-substituted with hydroxy or (C.sub.1 -C.sub.4)alkoxy; naphthyl di-substituted with hydroxy, (C.sub.1 -C.sub.4)alkoxy or (C.sub.1 -C.sub.4)alkyl; or napthyl substituted with methylenedioxy,-L- is a -Q-CH(OH)-- group wherein -Q- is a straight or branched alkylene radical of from 1 to 3 carbon atoms, and-M represents a radical selected from the group consisting of naphthyl; naphthyl mono- or di-substituted with hydroxy, (C.sub.1 -C.sub.4)alkoxy or (C.sub.1 -C.sub.4)alkyl or naphthyl substituted with methylenedioxy; pyridyl; or (C.sub.1 -C.sub.4)alkyl-pyridyl,and their salts with mineral or organic acids.
摘要翻译：用于治疗肠蠕动障碍的新N-取代的4-（3-三氟甲基苯基）-1,2,3,6-四氢吡啶，具有以下通式：其中A表示-EG或 - LM，其中-E-是具有2至4个碳原子的直链或支链亚烷基，-G表示选自由羟基或（C 1 -C 4）烷氧基单取代的萘基的基团; 被羟基，（C 1 -C 4）烷氧基或（C 1 -C 4）烷基二取代的萘基; 或被亚甲二氧基取代的萘基，-L-是-Q-CH（OH） - 基，其中-Q-是具有1至3个碳原子的直链或支链亚烷基，-M表示选自以下的基团：的萘基; 被羟基，（C 1 -C 4）烷氧基或被亚甲二氧基取代的（C 1 -C 4）烷基或萘基单 - 或二 - 取代的萘基; 吡啶基或（C 1 -C 4）烷基 - 吡啶基，以及它们与矿物或有机酸的盐。

9. 发明授权

US5410057A 1-heteroarylazetidines and -pyrrolidines 失效
标题翻译： 1-杂芳基氮杂环丁烷和吡咯烷
公开(公告)号：US5410057A
公开(公告)日：1995-04-25
申请号：US127038
申请日：1993-09-24
申请人： Marco Baroni , Umberto Guzzi , Antonina Giudice , Marco Landi , Vivian Mazza
发明人： Marco Baroni , Umberto Guzzi , Antonina Giudice , Marco Landi , Vivian Mazza
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/495 , A61K31/505 , A61P1/00 , A61P25/00 , A61P43/00 , C07D401/04 , C07D403/04 , C07D239/30 , C07D241/16
CPC分类号： C07D401/04 , C07D403/04
摘要： The present invention relates to new 1-heteroarylazetidines and new 1-heteroarylpyrrolidines endowed with 5-HT.sub.3 agonist activity of formula (IV): ##STR1## The substituents A, R', R.sub.1 and P, and the variables n and m, are as herein described.
摘要翻译：本发明涉及赋予式（IV）的5-HT 3激动剂活性的新的1-杂芳基氮杂环丁烷和新的1-杂芳基吡咯烷酮：（IV）取代基A，R'，R 1和P以及变量n和m ，如本文所述。

10. 发明授权

US5723611A Heteroarylpiperidines 失效
标题翻译：杂芳基哌啶
公开(公告)号：US5723611A
公开(公告)日：1998-03-03
申请号：US469523
申请日：1995-06-06
申请人： Marco Baroni , Tiziano Croci , Marco Landi , Umberto Guzzi , Dino Nisato
发明人： Marco Baroni , Tiziano Croci , Marco Landi , Umberto Guzzi , Dino Nisato
IPC分类号： A61K31/4427 , A61K31/445 , C07D401/04 , C07D239/42
CPC分类号： C07D401/04 , Y02P20/55
摘要： A compound of formula (VIII): ##STR1## in which Alk is a (C.sub.1 -C.sub.4)alkyl group, R.cndot. is hydrogen or a protecting group cleavable by hydrolysis and R is hydrogen, a protecting group cleavable by reduction or a heterocycle of structure (IX): ##STR2## in which Hal is a halogen atom and X, Y and Z are each --CH.dbd. or one of them is a nitrogen atom and the others are --CH.dbd., and its salts, R.cndot. being other than hydrogen if R is hydrogen or a group of structure (IX).
摘要翻译：式（VIII）化合物：其中Alk是（C1-C4）烷基，其中R是氢或被水解可裂解的保护基，R是氢，可以通过还原或结构（IX）的杂环：其中Hal为卤素原子，X，Y和Z各自为-CH =，或其中一个为氮原子，其余为-CH =，其盐，R不是氢，如果R是氢或结构（Ⅸ）。

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