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1. 发明授权

US5595994A 1-Halopyrazin- and 1-halopyrimidin-4-amino-4-alkylpiperidines 失效
标题翻译： 1-卤代吡嗪和1-卤代嘧啶-4-氨基-4-烷基哌啶
公开(公告)号：US5595994A
公开(公告)日：1997-01-21
申请号：US469511
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 , A61K31/505 , C07D239/42
CPC分类号： C07D401/04 , Y02P20/55
摘要： The present invention relates to novel heteroarylpiperidines of formula (I): ##STR1## in which Hal is a halogen atom, Alk is a C.sub.1-4 alkyl group and one of X, Y and Z is a nitrogen atom while the others are .dbd.CH--, and their salts. These compounds are useful as 5-HT.sub.3 agonists.
摘要翻译：本发明涉及式（I）的新型杂芳基哌啶：其中Hal为卤素原子，Alk为C1-4烷基，X，Y和Z之一为氮原子，其余为 = CH-及其盐。这些化合物可用作5-HT 3激动剂。

2. 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）。

3. 发明授权

US5502063A 1-halopyridin-4-amino-4-alkylpiperidines 失效
标题翻译： 1-卤代吡啶-4-氨基-4-烷基哌啶
公开(公告)号：US5502063A
公开(公告)日：1996-03-26
申请号：US319595
申请日：1994-10-07
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 , A61K31/44
CPC分类号： C07D401/04 , Y02P20/55
摘要： The present invention relates to novel heteroarylpiperidines of formula (I): ##STR1## in which Hal is a halogen atom, Alk is a C.sub.1 -C.sub.4 alkyl group and X, Y and Z are each --CH.dbd. and their salts, to a process for their preparation and to their use as drugs active as 5-HT.sub.3 agonists.
摘要翻译：本发明涉及式（I）的新的杂芳基哌啶：其中Hal是卤素原子，Alk是C1-C4烷基，X，Y和Z各自是-CH =，它们的盐，作为其制备方法和用作作为5-HT 3激动剂活性的药物。

4. 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。

5. 发明授权

US5576320A 1-heteruarylazetidines and -pyrrolidines, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译： 1-杂芳基氮杂环丁烷和吡咯烷，其制备方法和含有它们的药物组合物
公开(公告)号：US5576320A
公开(公告)日：1996-11-19
申请号：US466912
申请日：1995-06-06
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 , A61K31/50
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 (I): ##STR1## in which A is --CH.dbd.N-- or --N.dbd.CH--; R is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, cyano, carboxamido, trifluoromethyl, a vinyl group, a formyl group, a carboxyl group in free, salt or esterified form, hydroxyl, hydroxymethyl, mercapto, amine, mono- or di-(C.sub.1-4 alkyl)amino, aminomethyl, mono- or di(C.sub.1-4 alkyl)aminomethyl, 1-piperido, 1-pyrrolidino, 1-piperazino or 4-(C.sub.1-4 alkyl)-1-piperazino, where R may replace any one of the hydrogen atoms of the heteroaryl nucleus;R.sub.1 is hydrogen or a methyl group;R.sub.2 and R.sub.3, which are identical or different, are hydrogen or C.sub.1-4 alkyl;n is 1 or 2; m is 0 or 1; and m+n.gtoreq.2;and addition salts with inorganic or organic acids of the compounds of formula (I). The invention also relates to pharmaceutical compositions containing these compounds, as well as to methods of treatment or prophylaxis of disorders which involve the peripheral or central serotoninergic systems.
摘要翻译：本发明涉及新的1-杂芳基氮杂环丁烷和赋予式（I）的5-HT 3激动剂活性的新的1-杂芳基吡咯烷酮：其中A是-CH = N-或-N = CH-; R是氢，卤素，C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，氰基，甲酰氨基，三氟甲基，乙烯基，甲酰基，游离的羧基，盐或酯化形式，羟基，羟甲基，巯基，胺，单 - 或二 - （C 1-4烷基）氨基，氨基甲基，一或二（C 1-4烷基）氨基甲基，1-哌啶基，1-吡咯烷子基，1-哌嗪基或4-（C 1-4烷基）-1-哌嗪基，其中R可以代替杂芳基核的任何一个氢原子; R1是氢或甲基; R2和R3相同或不同，为氢或C1-4烷基; n为1或2; m为0或1; 和m + n> / = 2; 和与式（I）化合物的无机酸或有机酸的加成盐。本发明还涉及含有这些化合物的药物组合物，以及治疗或预防涉及周围或中枢血清素能系统的病症的方法。

6. 发明授权

US5565474A 1-heteroarylazetidines and -pyrrolidines process for their preparation and pharmaceutical compositions containing them 失效
标题翻译： 1-杂芳基氮杂环丁烷和吡咯烷的制备方法和含有它们的药物组合物
公开(公告)号：US5565474A
公开(公告)日：1996-10-15
申请号：US368915
申请日：1995-01-05
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
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 (I): ##STR1## in which A is --CH=CH--; R is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, cyano, carboxamido, trifluoromethyl, a vinyl group, a formyl group, a carboxyl group in free, salt or esterified form, hydroxyl, hydroxymethyl, mercapto, amino, mono- or di-(C.sub.1-4 alkyl)amino, aminomethyl, mono- or di(C.sub.1-4 alkyl)aminomethyl, 1-piperido, 1-pyrrolidino, 1-piperazino or 4-(C.sub.1-4 alkyl)-1-piperazino, where R may replace any one of the hydrogen atoms of the heteroaryl nucleus;R.sub.1 is hydrogen or a methyl group;R.sub.2 and R.sub.3, which are identical or different, are hydrogen or C.sub.1-4 alkyl;n is 1 or 2; m is 0 or 1; and m+n.gtoreq.2;and addition salts with inorganic or organic acids of the compounds of formula (I). The invention also relates to pharmaceutical compositions containing these compounds, as well as to methods of treatment or prophylaxis of disorders which involve the peripheral or central serotoninergic systems.
摘要翻译：本发明涉及新的1-杂芳基氮杂环丁烷和赋予式（I）的5-HT 3激动剂活性的新的1-杂芳基吡咯烷酮：其中A是-CH = CH-; R是氢，卤素，C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，氰基，甲酰氨基，三氟甲基，乙烯基，甲酰基，游离的羧基，盐或酯化形式，羟基，羟甲基，巯基，氨基，单 - 或二 - （C 1-4烷基）氨基，氨基甲基，一或二（C 1-4烷基）氨基甲基，1-哌啶基，1-吡咯烷子基，1-哌嗪基或4-（C 1-4烷基）-1-哌嗪基，其中R可以代替杂芳基核的任何一个氢原子; R1是氢或甲基; R2和R3相同或不同，为氢或C1-4烷基; n为1或2; m为0或1; 和m + n> / = 2; 和与式（I）化合物的无机酸或有机酸的加成盐。本发明还涉及含有这些化合物的药物组合物，以及治疗或预防涉及周围或中枢血清素能系统的病症的方法。

7. 发明授权

US5447931A New therapeutic use of heterocyclylpiperazines as 5-HT.sub.3 agonists and new compounds 失效
标题翻译：杂环基哌嗪作为5-HT3激动剂和新化合物的新治疗用途
公开(公告)号：US5447931A
公开(公告)日：1995-09-05
申请号：US344629
申请日：1994-11-17
申请人： Marco Baroni , Umberto Guzzi , Antonina Giudice , Marco Landi
发明人： Marco Baroni , Umberto Guzzi , Antonina Giudice , Marco Landi
IPC分类号： A61K31/495 , A61K31/505 , A61P1/12 , A61P25/18 , A61P25/20 , A61P37/00 , C07D213/74 , C07D239/42 , C07D241/20 , C07D253/07 , C07D401/04 , C07D241/02 , C07D403/04
CPC分类号： A61K31/495 , A61K31/505 , C07D213/74
摘要： New therapeutic use of some heterocyclylpiperazines of formula (I) ##STR1## wherein R represents hydrogen or (C.sub.1 -C.sub.4)alkyl, R.sub.1 represents hydrogen or a methyl group, R.sub.2 represents hydrogen or a halogen atom; X et Y represent each --CH.dbd., or one is --CH.dbd. and the other is --N.dbd., as well as their pharmaceutically acceptable salts for the preparation of a medicament for the treatment or prophylaxis of the pathological conditions which can be improved by 5-HT.sub.3 mediated selective agonism and new compounds deriving from this chemical class.
摘要翻译：式（I）的一些杂环基哌嗪的新治疗用途其中R表示氢或（C1-C4）烷基，R1表示氢或甲基，R2表示氢或卤素原子; X和Y表示每个-CH =，或一个是-CH =，另一个是-N =，以及它们的药学上可接受的盐，用于制备用于治疗或预防可通过以下方式改善的病理状况的药物 5-HT3介导的选择性激动剂和衍生自该化学类的新化合物。

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