公开(公告)号：EP0243959A1

公开(公告)日：1987-11-04

申请号：EP87106266.7

申请日：1987-04-29

申请人： Dainippon Pharmaceutical Co., Ltd.

发明人： Kon, Tatsuya ,  Kato, Shiro ,  Morie, Toshiya ,  Ohno, Kazunori ,  Hino, Katsuhiko ,  Karasawa, Tadahiko ,  Yoshida, Naoyuki

IPC分类号： C07D265/30 ,  C07D267/08 ,  C07D413/12 ,  C07D409/12 ,  A61K31/535 ,  A61K31/55

CPC分类号： C07D265/30 ,  C07D267/10 ,  C07D413/06 ,  C07D413/12

摘要： The subject matter of the invention are compounds of the formula:
wherein R, R 1 , R 2 , R 3 , R 4 , R 5 , X and m and n are defined as in the patent claims, and acid additional salts, quaternary ammonium salts and N-oxide derivatives thereof, processes for preparation thereof, and pharmaceutical compositions containing the same. Said compounds, salts and N-oxide derivatives thereof show excellent gastro-intestinal motility enhancing activity.

摘要翻译： 本发明的主题是下式的化合物：其中R，R 1，R 2，R 3，R 4，R 5，X和m和n如专利权利要求中所定义，其中R，R 1，R 2，R 3， 其N-氧化物衍生物，其制备方法和含有它们的药物组合物。 所述化合物，其盐和N-氧化物衍生物显示优异的胃肠蠕动增强活性。

公开(公告)号：EP0358903A3

公开(公告)日：1992-03-04

申请号：EP89113776.2

申请日：1989-07-26

申请人： DAINIPPON PHARMACEUTICAL CO., LTD.

发明人： Kon, Tatsuya ,  Kato, Shiro ,  Morie, Toshiya ,  Karasawa, Tadahiko ,  Yoshida, Naoyuki

IPC分类号： C07D243/08 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D239/04 ,  C07D245/02 ,  C07D403/04 ,  A61K31/505 ,  A61K31/55

CPC分类号： C07D401/14 ,  C07D243/08 ,  C07D403/12 ,  C07D405/14

摘要： An indazole-3-carboxylic acid derivative represented by the following general formula (I) or its physiologically acceptable acid addition salt or quaternary ammonium salt,

wherein Y represents -NH- or -O-; R₁ and R₂ are identical or different and each represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group, or R₁ and R₂, taken together, form a lower alkylene group; R₃ represents a hydrogen atom, a lower alkyl group, or a phenyl group; R₄ represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group; R₅ represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group, a nitro group, an amino group or an acylamino group; m represents a number of 1, 2, 3 or 4; n represents a number of 1, 2 or 3; and p represents a number of 1, 2, 3 or 4. This compound is useful as a potent and selective antagonist of serotonin 3 (5-HT₃) receptor.

公开(公告)号：EP0243959B1

公开(公告)日：1992-08-19

申请号：EP87106266.7

申请日：1987-04-29

申请人： Dainippon Pharmaceutical Co., Ltd.

发明人： Kon, Tatsuya ,  Kato, Shiro ,  Morie, Toshiya ,  Ohno, Kazunori ,  Hino, Katsuhiko ,  Karasawa, Tadahiko ,  Yoshida, Naoyuki

IPC分类号： C07D265/30 ,  C07D267/08 ,  C07D413/12 ,  C07D409/12 ,  A61K31/535 ,  A61K31/55

CPC分类号： C07D265/30 ,  C07D267/10 ,  C07D413/06 ,  C07D413/12

公开(公告)号：EP0358903A2

公开(公告)日：1990-03-21

申请号：EP89113776.2

申请日：1989-07-26

申请人： DAINIPPON PHARMACEUTICAL CO., LTD.

发明人： Kon, Tatsuya ,  Kato, Shiro ,  Morie, Toshiya ,  Karasawa, Tadahiko ,  Yoshida, Naoyuki

IPC分类号： C07D243/08 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D239/04 ,  C07D245/02 ,  C07D403/04 ,  A61K31/505 ,  A61K31/55

CPC分类号： C07D401/14 ,  C07D243/08 ,  C07D403/12 ,  C07D405/14

摘要： An indazole-3-carboxylic acid derivative represented by the following general formula (I) or its physiologically acceptable acid addition salt or quaternary ammonium salt,

wherein Y represents -NH- or -O-; R₁ and R₂ are identical or different and each represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group, or R₁ and R₂, taken together, form a lower alkylene group; R₃ represents a hydrogen atom, a lower alkyl group, or a phenyl group; R₄ represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group; R₅ represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group, a nitro group, an amino group or an acylamino group; m represents a number of 1, 2, 3 or 4; n represents a number of 1, 2 or 3; and p represents a number of 1, 2, 3 or 4.
This compound is useful as a potent and selective antagonist of serotonin 3 (5-HT₃) receptor.

摘要翻译： 由下列通式（I）表示的吲唑-3-羧酸衍生物或其生理上可接受的酸加成盐或季铵盐，其中Y表示-NH-或-O-; R1和R2相同或不同，各自表示氢原子，低级烷基，取代的低级烷基，环烷基，低级烯基，环烯基，低级炔基，未取代或取代的芳基低级 烷基，低级烷氧基羰基，未取代或取代的芳烷氧基羰基或酰基，或R 1和R 2一起形成低级亚烷基; R3表示氢原子，低级烷基或苯基; R4表示氢原子，低级烷基，取代的低级烷基，环烷基，低级烯基，环烯基，低级炔基，未取代或取代的芳基 - 低级烷基，低级烷氧基羰基， 未取代或取代的芳烷氧基羰基或酰基; R5表示氢原子，卤素原子，低级烷基，低级烷氧基，羟基，三氟甲基，硝基，氨基或酰氨基; m表示1,2,3或4的数字; n表示1,2或3的数; 并且p代表1,2,3或4.这种化合物可用作血清素3（5-HT3）受体的有效和选择性拮抗剂。