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1. 发明授权

US06544997B1 4-(aminomethyl)-piperidine benzamides for treating gastrointestinal disorders 有权
标题翻译：用于治疗胃肠道疾病的4-（氨基甲基） - 哌啶苯甲酰胺
公开(公告)号：US06544997B1
公开(公告)日：2003-04-08
申请号：US09857905
申请日：2001-06-08
申请人： Jean-Paul René Marie André Bosmans , Ann Louise Gabriëlle Meulemans , Michel Anna Jozef De Cleyn , Henricus Jacobus Maria Gijsen
发明人： Jean-Paul René Marie André Bosmans , Ann Louise Gabriëlle Meulemans , Michel Anna Jozef De Cleyn , Henricus Jacobus Maria Gijsen
IPC分类号： C07D40512
CPC分类号： C07D405/12 , C07D405/14 , Y02P20/55
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, —R1—R2— is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl or hydroxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, oxoC5-6cycloalkyl, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, amino, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, oxoC5-6cycloalkyl, aryl or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy, hydroxy or aryl; Y is a direct bond or NR10; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating or preventing gastrointestinal disorders.
摘要翻译：本发明的式（I）化合物是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，-R1-R2-是下式的二价基团：其中在所述二价基团中一个或两个氢原子可以被C 1-6烷基或羟基取代; R3是氢或卤素; R4是氢或C1-6烷基; R5是氢或C1-6烷基; L是C 3-6环烷基，C 5-6环烷基，C 2-6烯基或L是式-Alk-R 6 - ，Alk-X-R 7，-Alk-YC（= O）-R 9或-Alk-YC = O）-NR 11 R 12，其中每个Alk是C 1-12烷二基; R6为氢，氨基，氰基，C1-6烷基磺酰氨基，C3-6环烷基，氧代C 5-6环烷基，芳基或杂环环系; R 7是氢，C 1-6烷基，羟基C 1-6烷基，C 3-6环烷基，芳基或杂环环系; X是O，S，SO 2或NR 8; 所述R8为氢或C1-6烷基; R9是氢，C1-6烷基，C3-6环烷基，C1-6烷氧基，羟基或芳基; Y是直接键或NR10; 所述R 10为氢或C 1-6烷基; R 11和R 12各自独立地为氢，C 1-6烷基，C 3-6环烷基或R 11和R 12与氮原子结合可以形成任选取代的吡咯烷基，哌啶基，哌嗪基或4-吗啉基环。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗或预防胃肠道疾病。

2. 发明授权

US07205410B2 4-(aminomethyl)-piperidine benzamides for treating gastrointestinal disorders 有权
标题翻译：用于治疗胃肠道疾病的4-（氨基甲基） - 哌啶苯甲酰胺
公开(公告)号：US07205410B2
公开(公告)日：2007-04-17
申请号：US10353307
申请日：2003-01-29
申请人： Jean-Paul René Marie André Bosmans , Ann Louise Gabriëlle Meulemans , Michel Anna Jozef De Cleyn , Henricus Jacobus Maria Gijsen
发明人： Jean-Paul René Marie André Bosmans , Ann Louise Gabriëlle Meulemans , Michel Anna Jozef De Cleyn , Henricus Jacobus Maria Gijsen
IPC分类号： C07D401/00
CPC分类号： C07D405/12 , C07D405/14 , Y02P20/55
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, —R1—R2— is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl or hydroxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, oxoC5-6cycloalkyl, C2-6alkenyl, or L is a radical of formula -Alk-R6—, Alk-X—R7, -Alk-Y—C(═O)—R9, or -Alk-Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, amino, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, oxoC5-6cycloalkyl, aryl or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy, hydroxy or aryl; Y is a direct bond or NR10; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating or preventing gastrointestinal disorders.
摘要翻译：式的化合物的本发明

3. 发明授权

US06635643B2 Bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives 有权
标题翻译： 3-或4-取代的4-（氨基甲基） - 哌啶衍生物的双环苯甲酰胺
公开(公告)号：US06635643B2
公开(公告)日：2003-10-21
申请号：US09791227
申请日：2001-02-22
申请人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
发明人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
IPC分类号： A61K31495
CPC分类号： C07D211/42 , C07D211/44 , C07D401/06 , C07D405/06 , C07D405/12 , C07D405/14 , Y02P20/55
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)— NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
摘要翻译：本发明的式（I）化合物是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，R 1和R 2一起形成下式的二价基团，其中在所述二价基团一个或两个氢原子可以被C 1-6烷基取代; R 3是氢或卤素; R 4是氢或C 1-6烷基; R 5是氢或C 1-6烷基; L是C3-6环烷基，C5-6环烷酮，C2-6烯基或L是式-Alk-R6，Alk-XR7，-Alk-YC（= O）-R9的基团，或-Alk-YC（= O）-NR 11 R 12，其中每个Alk是C 1-12烷二基; R 6是氢，氰基，C 1-6烷基磺酰基氨基，C 3-6环烷基，C 5-6环烷酮或杂环体系; R 7是氢，C 1-6烷基，羟基C 1-6烷基，C 3-6环烷基或杂环环系; X是O，SO 2或NR 8; 所述R 8为氢或C 1-6烷基; R 9是氢，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基或羟基; Y是NR 10或直接键; 所述R 10为氢或C 1-6烷基; R 11和R 12各自独立地为氢，与氮原子结合的C 1-6烷基，C 1-6烷基或R 11和R 12可以形成任选取代的吡咯烷基，哌啶基，哌嗪基或4- 吗啉基环。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与胃排空的损伤相关的病症。

4. 发明授权

US06452013B1 Gastrokinetic monocyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives 有权
标题翻译： 3-或4-取代的4-（氨基甲基） - 哌啶衍生物的胃动力单环苯甲酰胺
公开(公告)号：US06452013B1
公开(公告)日：2002-09-17
申请号：US09462287
申请日：2000-01-05
申请人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
发明人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
IPC分类号： C07D21100
CPC分类号： C07D211/42 , C07D211/44 , C07D401/06 , C07D405/06 , C07D405/12 , C07D405/14 , Y02P20/55
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyl-oxy; R2 is hydrogen, C1-6alkyl C1-6alkyloxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, -Alk-Y—C(═O)—R9, or -Alk-Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
摘要翻译：本发明的式（I）化合物是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，R 1是C 1-6烷氧基，C 2-6烯氧基或C 2-6炔基氧基; R2是氢，C1-6烷基C1-6烷氧基; R3是氢或卤素; R4是氢或C1-6烷基; R5是氢或C1-6烷基; L是C3-6环烷基，C5-6环烷酮，C2-6烯基或L是式-Alk-R6-，Alk-X-R7，-Alk-YC（= O）-R9或-Alk-YC（ = O）-NR 11 R 12，其中每个Alk是C 1-12烷二基; R6为氢，氰基，C1-6烷基磺酰基氨基，C3-6环烷基，C5-6环烷酮或杂环环系; R7是氢，C1-6烷基，羟基C1-6烷基，C3-6环烷基或杂环环系; X是O，S，SO 2或NR 8; 所述R8为氢或C1-6烷基; R9是氢，C1-6烷基，C3-6环烷基，C1-6烷氧基或羟基; Y是NR10或直接键; 所述R 10为氢或C 1-6烷基; R 11和R 12各自独立地为氢，C 1-6烷基，C 3-6环烷基或R 11和R 12与氮原子结合可以形成任选取代的吡咯烷基，哌啶基，哌嗪基或4-吗啉基环。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与胃排空的损伤相关的病症。

5. 发明授权

US08263592B2 Equilibrative nucleoside transporter ENT1 inhibitors 有权
标题翻译：平衡核苷转运蛋白ENT1抑制剂
公开(公告)号：US08263592B2
公开(公告)日：2012-09-11
申请号：US12742807
申请日：2008-11-13
申请人： Jean-Paul René Marie André Bosmans , Didier Jean-Claude Berthelot , Serge Maria Aloysius Pieters , Bie Maria Pieter Verbist , Michel Anna Jozef De Cleyn
发明人： Jean-Paul René Marie André Bosmans , Didier Jean-Claude Berthelot , Serge Maria Aloysius Pieters , Bie Maria Pieter Verbist , Michel Anna Jozef De Cleyn
IPC分类号： C07D498/10 , A61K31/537
CPC分类号： C07D498/10 , C07D491/10
摘要： The present invention is related to novel compounds of formula (I) having equilibrative nucleoside transporter ENT1 inhibiting properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the inhibition of ENT1 receptors in animals, in particular humans.
摘要翻译：本发明涉及具有平衡核苷转运蛋白ENT1抑制性质的新型式（I）化合物，包含这些化合物的药物组合物，用于制备这些化合物的化学方法及其用于治疗与动物中ENT1受体的抑制有关的疾病，特别是人类。

6. 发明授权

US08063070B2 Bicyclic benzamides of 3-or 4-substituted 4-(aminomethyl)-piperidine derivatives 有权
标题翻译： 3-或4-取代的4-（氨基甲基） - 哌啶衍生物的双环苯甲酰胺
公开(公告)号：US08063070B2
公开(公告)日：2011-11-22
申请号：US12773183
申请日：2010-05-04
申请人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
发明人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
IPC分类号： A61K31/445 , A61K31/496 , C07D401/00 , C07D211/06 , C07D237/26
CPC分类号： C07D211/42 , C07D211/44 , C07D401/06 , C07D405/06 , C07D405/12 , C07D405/14 , Y02P20/55
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
摘要翻译：式（I）化合物的本发明是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与胃排空的损伤相关的病症。

7. 发明授权

US06750349B2 Gastrokinetic monocyclic benzamides of 3-or 4-substituted 4-(aminoethyl)-piperidine derivatives 有权
标题翻译： 3-或4-取代的4-（氨基乙基） - 哌啶衍生物的胃动力单环苯甲酰胺
公开(公告)号：US06750349B2
公开(公告)日：2004-06-15
申请号：US10162802
申请日：2002-06-05
申请人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
发明人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
IPC分类号： A61K21100
CPC分类号： C07D211/42 , C07D211/44 , C07D401/06 , C07D405/06 , C07D405/12 , C07D405/14 , Y02P20/55
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyl-oxy; R2 is hydrogen, C1-6alkyl C1-6alkyloxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk-X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
摘要翻译：本发明的式（I）化合物是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，R 1是C 1-6烷氧基，C 2-6烯基氧基或C 2-6炔基氧基; R 2是氢，C 1-6烷基C 1-6烷氧基; R 3是氢或卤素; R 4是氢或C 1-6烷基; R 5是氢或C 1-6烷基; L是C3-6环烷基，C5-6环烷酮，C2-6烯基或L是式-Alk-R6，Alk-XR7，-Alk-YC（= O）-R9的基团，，或-Alk-YC（= O）-NR 11 R 12，其中每个Alk是C 1-12烷二基; R 6是氢，氰基，C 1-6烷基磺酰基氨基，C 3-6环烷基，C 5-6环烷酮或杂环体系; R 7是氢，C 1-6烷基，羟基C 1-6烷基，C 3-6环烷基或杂环环系; X是O，S，SO 2或NR 8; 所述R 8为氢或C 1-6烷基; R 9是氢，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基或羟基; Y是NR 10或直接键; 所述R 10为氢或C 1-6烷基; R 11和R 12各自独立地为氢，与氮原子结合的C 1-6烷基，C 1-6烷基或R 11和R 12可以形成任选取代的吡咯烷基，哌啶基，哌嗪基或4- 吗啉基环。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与胃排空的损伤相关的病症。

8. 发明授权

US07790750B2 Bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives 有权
标题翻译： 3-或4-取代的4-（氨基甲基） - 哌啶衍生物的双环苯甲酰胺
公开(公告)号：US07790750B2
公开(公告)日：2010-09-07
申请号：US11584732
申请日：2006-10-20
申请人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
发明人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
IPC分类号： A61K31/445 , C07D407/02
CPC分类号： C07D211/42 , C07D211/44 , C07D401/06 , C07D405/06 , C07D405/12 , C07D405/14 , Y02P20/55
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula -Alk-R6—, Alk-X—R7, -Alk-Y—C(═O)—R9, or -Alk-Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, or R11 and R12 combined with the nitrogen atom may form an optionally substituted pyrrolidinyl, piperidinyl, piperazinyl or 4-morpholinyl ring. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
摘要翻译：式（I）化合物的本发明是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，R1和R2一起形成下式的二价基团：其中在所述二价基团中，一个或两个氢原子可以被C 1-6烷基取代; R3是氢或卤素; R4是氢或C1-6烷基; R5是氢或C1-6烷基; L是C3-6环烷基，C5-6环烷酮，C2-6链烯基或L是式-Alk-R6-，Alk-X-R7，-Alk-Y-C（= O）-R9或-Alk- Y-C（= O）-NR 11 R 12，其中每个Alk是C 1-12烷二基; R6为氢，氰基，C1-6烷基磺酰基氨基，C3-6环烷基，C5-6环烷酮或杂环环系; R7是氢，C1-6烷基，羟基C1-6烷基，C3-6环烷基或杂环环系; X是O，S，SO 2或NR 8; 所述R8为氢或C1-6烷基; R9是氢，C1-6烷基，C3-6环烷基，C1-6烷氧基或羟基; Y是NR10或直接键; 所述R 10为氢或C 1-6烷基; R 11和R 12各自独立地为氢，C 1-6烷基，C 3-6环烷基或R 11和R 12与氮原子结合可以形成任选取代的吡咯烷基，哌啶基，哌嗪基或4-吗啉基环。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与胃排空的损伤相关的病症。

9. 发明申请

US20100210657A1 Bicyclic Benzamides of 3-or 4-Substituted 4-(Aminomethyl)-Piperidine Derivatives 有权
标题翻译： 3-或4-取代的4-（氨基甲基）哌啶衍生物的双环苯甲酰胺
公开(公告)号：US20100210657A1
公开(公告)日：2010-08-19
申请号：US12773183
申请日：2010-05-04
申请人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
发明人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef De Cleyn , Michel Surkyn
IPC分类号： A61K31/4525 , C07D405/12 , C07D405/14 , A61K31/453 , A61K31/502 , A61K31/501 , A61P1/00
CPC分类号： C07D211/42 , C07D211/44 , C07D401/06 , C07D405/06 , C07D405/12 , C07D405/14 , Y02P20/55
摘要： The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
摘要翻译：式（I）化合物的本发明是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与胃排空的损伤相关的病症。

10. 发明授权

US07652040B2 Aminosulfonyl substituted 4-(aminomethyl)-piperidine benzamides as 5HT4-antagonists 有权
标题翻译：氨基磺酰基取代的4-（氨基甲基） - 哌啶苯甲酰胺作为5HT4拮抗剂
公开(公告)号：US07652040B2
公开(公告)日：2010-01-26
申请号：US10560300
申请日：2004-06-10
申请人： Jean-Paul René Marie André Bosmans , Henricus Jacobus Maria Gijsen , Laurence Anne Mevellec
发明人： Jean-Paul René Marie André Bosmans , Henricus Jacobus Maria Gijsen , Laurence Anne Mevellec
IPC分类号： A61K31/445 , C07D405/12
CPC分类号： C07D405/12
摘要： The present invention is concerned with novel compounds of formula (I) having 5HT4-antagonistic properties. The invention further relates to methods for preparing such novel compounds, pharmaceutical compositions comprising said novel compounds as well as the use as a medicine of said compounds.
摘要翻译：本发明涉及具有5HT4拮抗性质的新型式（I）化合物。本发明还涉及制备这些新化合物的方法，包含所述新化合物的药物组合物以及用作所述化合物的药物。

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