公开(公告)号：US06608070B1

公开(公告)日：2003-08-19

申请号：US09355494

申请日：1999-07-28

申请人： Kazunari Nakao ,  Rodney William Stevens ,  Kiyoshi Kawamura ,  Chikara Uchida ,  Hiroki Koike ,  Stephane Caron

发明人： Kazunari Nakao ,  Rodney William Stevens ,  Kiyoshi Kawamura ,  Chikara Uchida ,  Hiroki Koike ,  Stephane Caron

IPC分类号： A01N4390

CPC分类号： C07D401/06 ,  C07D209/18 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/10 ,  C07D409/06 ,  C07D409/10 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10

摘要： This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the following: (a) an optionally substituted phenyl, (b) an optionally substituted 6-membered monocyclic aromatic group containing one, two, three or four nitrogen atom(s), (c) an optionally substituted 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, (d) an optionally substituted C3-7 cycloalkyl and (e) an optionally substituted benzo-fuzed heterocycle; R1 is hydrogen, C1-4 alkyl or halo; R2 and R3 are independently hydrogen, OH, C1-4 alkoxy, C1-4 alkyl or C1-4 alkyl substituted with halo, OH, C1-4 alkoxy or CN; X is independently selected from H, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 alkyl)amino and CN; and n is 0, 1, 2, 3 and 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐，其中Z是OH，C 1-6烷氧基，-NR 2 R 3或杂环; Q选自以下：（a）任选取代的苯基，（b）含有一个，两个，三个或四个氮原子的任选取代的6元单环芳族基团，（c）任选取代的5元 含有一个选自O，S和N的杂原子，并且除了所述杂原子之外任选含有一个，两个或三个氮原子的单环芳基，（d）任选取代的C 3-7环烷基和（e）任选取代的苯并 杂环杂环 R1是氢，C1-4烷基或卤素; R2和R3独立地是氢，OH，C1-4烷氧基，C1-4烷基或被卤素，OH，C1-4烷氧基或CN取代的C1-4烷基; X独立地选自H，卤素，C 1-4烷基，卤素取代的C 1-4烷基，OH，C 1-4烷氧基，卤素取代的C 1-4烷氧基，C 1-4烷硫基，NO 2，NH 2，二（C 1 -4烷基）氨基和CN; 并且n为0,1,2,3和4.本发明还提供了可用于治疗前列腺素作为病原体的医疗状况的药物组合物。

公开(公告)号：US06277878B1

公开(公告)日：2001-08-21

申请号：US09383353

申请日：1999-08-26

申请人： Kazunari Nakao ,  Rodney W. Stevens ,  Kiyoshi Kawamura ,  Chikara Uchida

发明人： Kazunari Nakao ,  Rodney W. Stevens ,  Kiyoshi Kawamura ,  Chikara Uchida

IPC分类号： A61K31404

CPC分类号： C07D401/06 ,  C07D209/40 ,  C07D405/06 ,  Y02P20/55

摘要： This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein R1 is H or C1-4 alkyl; R2 is C(═L′)R3 or So2R4; Y is a direct bond or C1-4 alkylene; L and L′ are independently oxygen or sulfur; Q is selected from the following: C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted phenyl or naphthyl, optionally substituted 5 or 6-membered monocyclic aromatic group; R3 is —OR6, —NR7R8, N(OR1)R7 or a group of formula: Z is a direct bond, O, S or NR5; R4 is C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted phenyl or naphthyl; R5 is C1-4 alkyl or halo-substituted C1-4 alkyl; R6 is C1-4 alkyl C3-7 cycloalkyl, C1-4 alkyl-C3-7 cycloalkyl, halo-substituted C1-4 alkyl, optionally substituted C1-4 alkyl-phenyl or phenyl; R7 and R8 are each selected from the following: H, optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted C1-4 alkyl-C3-7 cycloalkyl, and optionally substituted C1-4 alkyl-phenyl or phenyl; X is each selected from halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 alkyl)amino and CN; n is 0, 1, 2 or 3; and r is 1, 2 or 3. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐，其中R 1是H或C 1-4烷基; R2是C（= L'）R3或So2R4; Y是直接键或C1-4亚烷基; L和L'独立地是氧或硫; Q选自以下：C 1-6烷基，卤素取代的C 1-4烷基，任选取代的C 3-7环烷基，任选取代的苯基或萘基，任选取代的5或6元单环芳基; R 3是-OR 6， NR7R8，N（OR1）R7或下式的基团：Z是直接键，O，S或NR5; R 4是C 1-6烷基，卤素取代的C 1-4烷基，任选取代的苯基或萘基; R5是C1-4烷基或卤素取代的C1-4烷基; R 6是C 1-4烷基C 3-7环烷基，C 1-4烷基-C 3-7环烷基，卤素取代的C 1-4烷基，任选取代的C 1-4烷基 - 苯基或苯基; R 7和R 8各自选自如下：H，任选取代的C 1-6烷基，任选取代的C 3-7环烷基，任选取代的C 1-4烷基-C 3-7环烷基和任选取代的C 1-4烷基 - 苯基或苯基; X选自卤素，C 1-4烷基，卤素取代的C 1-4烷基，OH，C 1-4烷氧基，卤素取代的C 1-4烷氧基，C 1-4烷硫基，NO 2，NH 2，二（C 1-4） 烷基）氨基和CN; n为0,1,2或3; 并且r为1,2或3.本发明还提供了可用于治疗前列腺素作为病原体的医学病症的药物组合物。

公开(公告)号：US20080255113A1

公开(公告)日：2008-10-16

申请号：US10595948

申请日：2004-11-10

申请人： Tomoki Kato ,  Kiyoshi Kawamura ,  Mikio Morita ,  Chikara Uchida

发明人： Tomoki Kato ,  Kiyoshi Kawamura ,  Mikio Morita ,  Chikara Uchida

IPC分类号： A61K31/5377 ,  C07D405/14 ,  A61K31/4709 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

CPC分类号： C04B35/632 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

摘要： This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α1; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

摘要翻译： 本发明提供式（I）化合物：其中Het表示具有一个氮原子的杂环基团，B直接与该碳原子结合，并且具有4至7个碳原子，所述杂环基团未被取代或被1至4个取代基取代 独立地选自取代基α1， A表示具有1至4个碳原子的亚烷基; B表示共价键或具有1至5个碳原子的亚烷基; R 1表示异丙基，正丙基或环戊基; R 2表示甲基，氟原子或氯原子; R 3独立地表示（i）氧代基，羟基，氨基，烷基氨基或羧基; （ii）具有3至8个碳原子的环烷基，所述环烷基被1至5个取代基取代，或（iii）具有3至8个原子的杂环基，所述杂环基未被取代或被1 至5个取代基，n为1,2或3，或其药学上可接受的盐。 这些化合物具有5-HT 4受体激动活性，因此可用于治疗哺乳动物，特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。

公开(公告)号：US20100273794A1

公开(公告)日：2010-10-28

申请号：US12831713

申请日：2010-07-07

申请人： Yasuhiro Katsu ,  Satoru Iguchi ,  Hiroki Sone ,  Chikara Uchida ,  Takashi Kojima

发明人： Yasuhiro Katsu ,  Satoru Iguchi ,  Hiroki Sone ,  Chikara Uchida ,  Takashi Kojima

IPC分类号： A61K31/5377 ,  C07D211/26 ,  A61K31/454 ,  C07D413/14 ,  A61P1/04 ,  A61P1/00 ,  A61P9/00 ,  A61P25/06 ,  A61P25/28 ,  A61P29/00

CPC分类号： C07D413/14 ,  C04B35/632 ,  C07D401/12 ,  C07D405/06 ,  C07D405/14

摘要： This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，以及含有这些化合物的组合物以及这些化合物在制备胃食管反流疾病，胃肠道疾病，胃动力障碍，非溃疡的药物中的用途 消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病，心力衰竭，心脏 心律失常，糖尿病和呼吸暂停综合征。 这些化合物具有5-HT 4受体激动活性，因此可用于治疗哺乳动物特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。

公开(公告)号：US20080108660A1

公开(公告)日：2008-05-08

申请号：US11971265

申请日：2008-01-09

申请人： Koji Ando ,  Satoru Iguchi ,  Noriaki Murase ,  Yoshinori Murata ,  Toyoharu Numata ,  Hiroki Sone ,  Chikara Uchida ,  Tatsuo Ueki

发明人： Koji Ando ,  Satoru Iguchi ,  Noriaki Murase ,  Yoshinori Murata ,  Toyoharu Numata ,  Hiroki Sone ,  Chikara Uchida ,  Tatsuo Ueki

IPC分类号： A61K31/445 ,  C07D403/02 ,  A61P1/00 ,  C07D211/06 ,  A61K31/4164

CPC分类号： C07D401/12 ,  C07D211/26 ,  C07D401/06 ,  C07D401/14 ,  C07D405/06 ,  C07D405/14

摘要： This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.

摘要翻译： 本发明涉及式（I）化合物：其中R 1，R 2，R 3，A和m各自如上所述 本文或其药学上可接受的盐或溶剂合物，以及含有这些化合物的组合物以及这些化合物在治疗由5-HT 4受体活性介导的病症中的用途，所述活性例如但不限于， 胃食管反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐， 偏头痛，神经系统疾病，疼痛，心血管疾病如心力衰竭和心律失常，糖尿病和呼吸暂停综合征。

公开(公告)号：US08816090B2

公开(公告)日：2014-08-26

申请号：US11814588

申请日：2006-02-15

申请人： Hirohide Noguchi ,  Isao Sakurada ,  Chikara Uchida ,  Nobuaki Waizumi

发明人： Hirohide Noguchi ,  Isao Sakurada ,  Chikara Uchida ,  Nobuaki Waizumi

IPC分类号： C07D261/20 ,  A61K31/4439

CPC分类号： C07D413/12 ,  C07D413/14

摘要： This invention relates to compounds of the formula (I): wherein A, B, R1, R4, m, and n are each as described herein or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central 10 nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.

摘要翻译： 本发明涉及式（I）的化合物：其中A，B，R 1，R 4，m和n各自如本文所述或其药学上可接受的盐，以及含有这些化合物的组合物和这些化合物在 治疗由5-HT4受体活性介导的病症，例如但不限于胃食管反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎 ，胃肠疾病，恶心，中枢10神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心力衰竭和心律失常等心血管疾病，糖尿病和呼吸暂停综合征。

公开(公告)号：US07776885B2

公开(公告)日：2010-08-17

申请号：US10933629

申请日：2004-09-02

申请人： Yasuhiro Katsu ,  Satoru Iguchi ,  Hiroki Sone ,  Chikara Uchida ,  Takashi Kojima

发明人： Yasuhiro Katsu ,  Satoru Iguchi ,  Hiroki Sone ,  Chikara Uchida ,  Takashi Kojima

IPC分类号： A61K31/454 ,  C07D471/04

CPC分类号： C07D413/14 ,  C04B35/632 ,  C07D401/12 ,  C07D405/06 ,  C07D405/14

摘要： This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，以及含有这些化合物的组合物以及这些化合物在制备胃食管反流疾病，胃肠道疾病，胃动力障碍，非溃疡的药物中的用途 消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病，心力衰竭，心脏 心律失常，糖尿病和呼吸暂停综合征。 这些化合物具有5-HT 4受体激动活性，因此可用于治疗哺乳动物特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。

公开(公告)号：US06624162B2

公开(公告)日：2003-09-23

申请号：US10251109

申请日：2002-09-20

申请人： Chikara Uchida ,  Hirohide Noguchi ,  Alan Stobie ,  Geoffrey Gymer ,  David Fenwick

发明人： Chikara Uchida ,  Hirohide Noguchi ,  Alan Stobie ,  Geoffrey Gymer ,  David Fenwick

IPC分类号： A61K31437

CPC分类号： C07D471/04

摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein R1 is hydrogen, halo or alkyl; R2 and R3 are independently hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl or hydroxyalkyl; or R2 and R3 taken together with the nitrogen atom to which they are attached may form hetrocyclic; R4 is hydrogen, halo, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R5 is hydrogen, halo, alkyl alkenyl, alkynyl, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R6 is hydrogen, alkyl or alkoxyalkyl; X is NR9 wherein R9 is hydrogen or alkyl; and Y is (CR7R8)n wherein n is an integer from 0 to 5. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, Functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，其中R 1是氢，卤素或烷基; R 2和R 3独立地是氢，烷基，烯基，炔基，氨基烷基或羟烷基; 或R 2和R 3与它们所连接的氮原子一起可以形成环状的; R 4是氢，卤素，酰基，氨基，酰氨基，芳基，芳基烷基或杂芳基; R 5是氢，卤素，烷基烯基，炔基，酰基，氨基，酰氨基，芳基，芳基烷基或杂芳基; R 6是氢，烷基或烷氧基烷基; X是NR 9，其中R 9是氢或烷基; 并且Y是（CR 7 R 8）n，其中n是0至5的整数。这些化合物具有5-HT 4受体结合活性，因此可用于治疗胃食管反流病，非溃疡性消化不良 ，功能性消化不良，肠易激综合征等。 本发明还提供了包含上述化合物的药物组合物。

公开(公告)号：US07595329B2

公开(公告)日：2009-09-29

申请号：US11153757

申请日：2005-06-14

申请人： Koji Ando ,  Satoru Iguchi ,  Noriaki Murase ,  Yoshinori Murata ,  Toyoharu Numata ,  Hiroki Sone ,  Chikara Uchida ,  Tatsuo Ueki

发明人： Koji Ando ,  Satoru Iguchi ,  Noriaki Murase ,  Yoshinori Murata ,  Toyoharu Numata ,  Hiroki Sone ,  Chikara Uchida ,  Tatsuo Ueki

IPC分类号： A61K31/445 ,  C07D401/12

CPC分类号： C07D401/12 ,  C07D211/26 ,  C07D401/06 ,  C07D401/14 ,  C07D405/06 ,  C07D405/14

摘要： This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.

摘要翻译： 本发明涉及式（I）化合物：其中R 1，R 2，R 3，A和m各自如本文所述，或其药学上可接受的盐或溶剂化物，以及含有这些化合物的组合物和这些化合物在治疗中的用途 由5-HT4受体活性介导的病症，例如但不限于胃食管反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食道炎， 胃肠疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病如心力衰竭和心律失常，糖尿病和呼吸暂停综合征。

公开(公告)号：US06951867B2

公开(公告)日：2005-10-04

申请号：US10667182

申请日：2003-09-17

申请人： Yasuhiro Katsu ,  Kana Kon-I ,  Mikio Morita ,  Hirohide Noguchi ,  Chikara Uchida

发明人： Yasuhiro Katsu ,  Kana Kon-I ,  Mikio Morita ,  Hirohide Noguchi ,  Chikara Uchida

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P1/04

CPC分类号： C07D471/04

摘要： This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt, amide or ester thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom, etc.; R3 represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of R3 is substituted by at least one substituent selected from the group consisting of substituents α; said substituents α is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents α, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐，酰胺或酯，其中R 1表示氢原子或卤素原子; R 2表示氢原子等; R 3表示具有1至10个碳原子的烷基; 所述R 3的烷基被至少一个选自取代基α的取代基取代; 所述取代基α是芳基，羟基，氧代等; 所述芳基具有6至10个碳原子; 所述芳基是未取代的或被至少一个具有1至6个碳原子的烷基取代; 所述杂环基和所述杂环羰基的杂环部分，两个取代基α为含有1至4个选自氮原子，氧原子和硫原子的杂原子的5至10元环基这些化合物具有5-HT 受体结合活性，因此可用于治疗哺乳动物，特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。 本发明还提供了包含上述化合物的药物组合物。