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1. 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。

2. 发明授权

US07498347B2 Hydroxycarbonylphenyl substituted 4-(aminomethyl)-piperidine benzamides as 5HT4 antagonists 有权
标题翻译：羟基羰基苯基取代的4-（氨基甲基） - 哌啶苯甲酰胺为5HT4拮抗剂
公开(公告)号：US07498347B2
公开(公告)日：2009-03-03
申请号：US10560555
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种新化合物的方法，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。

3. 发明授权

US06395742B1 2,4-diaminopyrimidine derivatives 有权
标题翻译： 2,4-二氨基嘧啶衍生物
公开(公告)号：US06395742B1
公开(公告)日：2002-05-28
申请号：US09667458
申请日：2000-09-22
申请人： Jean-Paul René Marie André Bosmans , Christopher John Love , Guy Rosalia Eugène Van Lommen
发明人： Jean-Paul René Marie André Bosmans , Christopher John Love , Guy Rosalia Eugène Van Lommen
IPC分类号： C07D40112
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl or C3-6alkenediyl; R1 is hydrogen or C1-4alkyl; R2 and R3 each independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; or R2 and R3 may also be taken together with the nitrogen atom to which they are attached, thus forming a pyrrolidine, a piperidine or a perhydro azepine ring; R4 is hydrogen or halo; Q is aryl, aryloxy, di(aryl)methyl or heteroaryl; aryl is naphthyl or phenyl, said naphthyl and phenyl may optionally be substituted; and heteroaryl is quinolinyl, isoquinolinyl, pyridinyl, thienyl, indolyl, 2,3-dihydro-1,4-benzodioxinyl, 2,3-dihydro-benzofuranyl or benzodioxolanyl; said heteroaryls may optionally be substituted; it further relates to processes for their preparation, compositions comprising them as well as their use as a medicine; compounds of formula (I) containing a radioactive isotope; a process of marking dopamine D4 receptor sites; and a process for imaging an organ are disclosed.
摘要翻译：本发明涉及配制N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中Alk是C 1-6烷二基或C 3-6亚烯基; R1是氢或C1-4烷基; R2和R3各自独立地为氢，C1-6烷基或C3-7环烷基; 或者R 2和R 3也可以与它们所连接的氮原子一起，从而形成吡咯烷，哌啶或全氢吖庚因环; R4是氢或卤素; Q是芳基，芳氧基，二（芳基）甲基或杂芳基; 芳基是萘基或苯基，所述萘基和苯基可任选被取代; 异喹啉基，吡啶基，噻吩基，吲哚基，2,3-二氢-1,4-苯并二氧杂环戊烯基，2,3-二氢 - 苯并呋喃基或苯并二氧杂环戊烷基; 所述杂芳基可任选被取代; 它还涉及它们的制备方法，包含它们的组合物以及它们作为药物的用途; 含有放射性同位素的式（I）化合物; 标记多巴胺D4受体位点的过程; 并且公开了用于成像器官的方法。

4. 发明授权

US07638535B2 4-(aminomethyl)-piperidine benzamides as 5HT4-antagonists 有权
标题翻译： 4-（氨基甲基） - 哌啶苯甲酰胺作为5HT4拮抗剂
公开(公告)号：US07638535B2
公开(公告)日：2009-12-29
申请号：US10560479
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
CPC分类号： C07D405/12 , C07D405/14
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种新化合物的方法，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。

5. 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。

6. 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。

7. 发明授权

US07732464B2 Heterocyclic substituted 4-(aminomethyl)-piperidine benzamides as 5HT4-antagonists 有权
标题翻译：杂环取代的4-（氨基甲基） - 哌啶苯甲酰胺作为5HT4拮抗剂
公开(公告)号：US07732464B2
公开(公告)日：2010-06-08
申请号：US10560486
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 , C07D405/14
CPC分类号： C07D405/12 , C07D405/14 , C07D413/14
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种新化合物的方法，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。

8. 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。

9. 发明授权

US06310077B1 Enterokinetic benzamide 有权
标题翻译：肠动蛋白苯甲酰胺
公开(公告)号：US06310077B1
公开(公告)日：2001-10-30
申请号：US09325865
申请日：1999-06-04
申请人： Georges H. P. Van Daele , Jean-Paul René Marie André Bosmans , Joannes Adrianus Jacobus Schuurkes
发明人： Georges H. P. Van Daele , Jean-Paul René Marie André Bosmans , Joannes Adrianus Jacobus Schuurkes
IPC分类号： A61K31445
CPC分类号： C07D405/12
摘要： The present invention is concerned with a novel benzamide of formula (I). Pharmaceutical compositions comprising said novel compounds, process for preparing compounds and compositions, and the use thereof as a medicine, in particular in the treatment of conditions involving a decreased motility of the intestine are described.
摘要翻译：本发明涉及式（I）的新型苯甲酰胺。包含所述新化合物的药物组合物，制备化合物和组合物的方法及其作为药物的用途，特别是在治疗涉及描述肠。

10. 发明授权

US08318742B2 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：US08318742B2
公开(公告)日：2012-11-27
申请号：US13237330
申请日：2011-09-20
申请人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef DeCleyn , Michel Surkyn
发明人： Jean-Paul René Marie André Bosmans , Michel Anna Jozef DeCleyn , Michel Surkyn
IPC分类号： A61K31/445 , 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。

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