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1. 发明授权

US5252749A Ethers of thienocyclopentanone oximes, their preparation and pharmaceutical compositions containing them 失效
标题翻译：噻吩环戊酮肟醚，其制备方法和含有它们的药物组合物
公开(公告)号：US5252749A
公开(公告)日：1993-10-12
申请号：US954530
申请日：1992-09-23
申请人： Alain Badorc , Jean Courregelongue , Daniel Ducros , Daniel Frehel , Antonina Giudice , Claudine Serradeil-Legal
发明人： Alain Badorc , Jean Courregelongue , Daniel Ducros , Daniel Frehel , Antonina Giudice , Claudine Serradeil-Legal
IPC分类号： A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/4535 , A61K31/5377 , A61P25/00 , A61P43/00 , C07D333/78 , C07D409/12 , A61K31/15
CPC分类号： C07D333/78 , C07D409/12
摘要： The compounds of the invention having the formula: ##STR1## in which: A, which is a ring condensed with cyclopentane, represents a substituted or unsubstituted thiophene ring, Q represents an alkylene chain, R.sub.1 and R.sub.2 each represent H or an alkyl, or they form, with the nitrogen atom to which they are linked, a saturated nitrogenous heterocyclic ring containing 5 to 7 atoms, R.sub.3 and R.sub.4 each represent H, alkyl, cycloalkyl, trifluoromethyl or an optionally substituted phenyl, thienyl or furyl group or R.sub.3 and R.sub.4 together form a (C.sub.5 -C.sub.8) cycloalkyl, as well as their addition salts with an acid and their quaternary ammonium derivatives.They can be used as medicines.
摘要翻译：具有下式的本发明化合物：其中：作为与环戊烷缩合的环的A表示取代或未取代的噻吩环，Q表示亚烷基链，R 1和R 2各自表示H或烷基，或它们与它们所连接的氮原子形成含有5至7个原子的饱和含氮杂环，R 3和R 4各自表示H，烷基，环烷基，三氟甲基或任选取代的苯基，噻吩基或呋喃基或R 3和 R4一起形成（C5-C8）环烷基，以及它们与酸及其季铵衍生物的加成盐。它们可以用作药物。

2. 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。

3. 发明授权

US4489079A Pharmaceutical compositions having a peripheral antagonistic action with respect to opiates 失效
标题翻译：对于鸦片剂具有周围拮抗作用的药物组合物
公开(公告)号：US4489079A
公开(公告)日：1984-12-18
申请号：US422568
申请日：1982-09-24
申请人： Antonina Giudice , Claude Moulineau , Luciano Manara , Paolo Carminati
发明人： Antonina Giudice , Claude Moulineau , Luciano Manara , Paolo Carminati
IPC分类号： A61K31/47 , A61K31/485 , A61P25/04 , A61P25/30 , C07D221/28
CPC分类号： C07D221/28 , A61K31/485
摘要： The present invention relates to a pharmaceutical composition having a peripheral antagonistic action with respect to opiates containing, as active ingredient, a haloallylate of levallorphan of formula: ##STR1## where X is chlorine, bromine or iodine, mixed with a pharmaceutical excipient.
摘要翻译：本发明涉及一种药物组合物，其具有关于含有作为活性成分的左旋兰烷的卤代烯丙基酯的鸦片剂的药物组合物，其中X是氯，溴或碘，其与药物赋形剂混合。

4. 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。

5. 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。

6. 发明授权

US5604245A Use of 4-amino-1-(2-pyridyl)piperidines for the preparation of a medicament for the treatment of conditions deriving from disorders of the serotoninergic systems mediated by 5-HT.sub.3 receptors 失效
标题翻译： 4-氨基-1-（2-吡啶基）哌啶用于制备用于治疗由5-HT 3受体介导的血清素能系统的病症的病症的药物的用途
公开(公告)号：US5604245A
公开(公告)日：1997-02-18
申请号：US858483
申请日：1992-03-27
申请人： G erard Le Fur , Alberto Bianchetti , Antonina Giudice , Tiziano Croci , Philippe Soubrie
发明人： G erard Le Fur , Alberto Bianchetti , Antonina Giudice , Tiziano Croci , Philippe Soubrie
IPC分类号： C07D401/04 , A61K31/44 , A61K31/4427 , A61K31/445 , A61P1/00 , A61P1/10 , A61P25/00 , A61P25/18 , A61P25/20 , A61P43/00
CPC分类号： A61K31/445 , A61K31/44
摘要： The present invention concerns the use of 4-amino-1-(2-pyridyl)piperidines of general formula (I') ##STR1## wherein R' represents hydrogen, a halogen atom, a methyl, methylthio, trifluoromethyl, trifluoromethylthio, (C.sub.1 -C.sub.3)alkoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, or phenoxy group optionally substituted with a halogen atom, a trifluoromethyl, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkylthio, or cyano group, or of a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment or prophylaxis of those conditions deriving from disorders of the serotoninergic systems wherein a serotoninergic action selectively mediated by the 5-HT.sub.3 receptors is required, e.g. affective disorders, anxiety, psychotic troubles, constipation.
摘要翻译：本发明涉及通式（I'）卤素原子的4-氨基-1-（2-吡啶基）哌啶，甲基，甲硫基，三氟甲基，三氟甲硫基，（C 1 -C 3）烷氧基，三氟甲氧基，2,2 ，（C 3 -C 3）烷基，（C 1 -C 3）烷氧基，（C 1 -C 3）烷硫基或氰基，或其药学上可接受的盐，任选被卤素原子取代的2-三氟乙氧基或苯氧基，用于制备用于治疗或预防源自5-羟色胺能系统疾病的那些病症的药物，其中需要由5-HT 3受体选择性介导的血清素能作用，例如情感障碍，焦虑症，精神障碍，便秘。

7. 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。

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