公开(公告)号：US4992437A

公开(公告)日：1991-02-12

申请号：US399550

申请日：1989-08-09

申请人： Yoichi Naka ,  Yukio Hitotsuyanagi ,  Keiichiro Haga ,  Masahiro Hosoya

发明人： Yoichi Naka ,  Yukio Hitotsuyanagi ,  Keiichiro Haga ,  Masahiro Hosoya

IPC分类号： A61K31/00 ,  A61K31/55 ,  A61P1/04 ,  C07D495/04 ,  C07D495/14

CPC分类号： C07D495/04

摘要： Thienodiazepine compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and respectively stand for a hydrogen atom, a halogen, an alkyl or an aralkyl, or mean a group wherein R.sup.1 and R.sup.2 combinedly together form a ring; R.sup.3 stands for an oxygen atom, R.sup.4 stands for a hydrogen atom, an alkyl, an alkenyl or a group of the formula --(CH.sub.2).sub.m COOR.sup.6 (wherein R.sup.6 l stands for a hydrogen atom, an alkyl, an alkenyl or an aralkyl and m stands for an integer of 1-6), or R.sup.3 and R.sup.4 stand for a group wherein R.sup.3 and R.sup.4 combinedly together form a group of the formula .dbd.N--N.dbd.C(R.sup.5)-- [wherein R.sup.5 stands for a hydrogen atom, an alkyl, an alkenyl, an aralkyl or a group of the formula --(CH.sub.2).sub.n COOR.sup.7 (wherein R.sup.7 stands for a hydrogen atom, an alkyl, an alkenyl or an aralkyl and n stands for an integer of 1-6)]; Ar and X are the same or different and respectively stand for an aryl or a heteroaryl; and p stands for an integer of 1-6, and their salts and their pharmaceutical use.These compounds possess an antagonistic action to cholecystokinin and gastrin and exhibit a durable pancreatic enzymes- and gastric acid-secretion-suppressive action, and therefore are useful as the medicaments acting on the central nervous system and peripheral nervous system and as the prophylactic or therapeutic medicines for pancreatic disorders and gastrointestinal ulcers.

公开(公告)号：US5439905A

公开(公告)日：1995-08-08

申请号：US66130

申请日：1993-05-27

申请人： Yoichi Naka ,  Keiichiro Haga ,  Masahiro Hosoya

发明人： Yoichi Naka ,  Keiichiro Haga ,  Masahiro Hosoya

IPC分类号： A61K31/55 ,  C07D495/04 ,  C07D495/14 ,  C07D487/04 ,  C07D495/00

CPC分类号： C07D495/04 ,  C07D495/14

摘要： Thienodiazepine compounds of the formula ##STR1## wherein each symbol is as defined in the specification, their pharmaceutically acceptable salts, and pharmaceutical compositions containing said compound.Since the compounds possess excellent antagonistic actions on cholecystokinin and gastrin, and exhibit potent and durable suppressive actions on pancreatic enzyme secretion and gastric acid secretion, they are useful as medicaments acting on the central nervous system and the peripheral nervous system, as well as prophylactic and therapeutic medicines for pancreatic disorders and gastrointestinal ulcers. Furthermore, they are expected to exhibit anti-dementia actions based on their antagonistic actions on cholecystokinin, and are useful as an anti-dementia.

摘要翻译： 其中每个符号如本说明书中所定义，其药学上可接受的盐和含有所述化合物的药物组合物的噻吩并二氮杂化合物。 由于该化合物对缩胆囊素和胃泌素具有优异的拮抗作用，并且对胰腺酶分泌和胃酸分泌具有有效和持久的抑制作用，因此它们可用作作用于中枢神经系统和周围神经系统的药物，以及预防和 用于胰腺疾病和胃肠溃疡的治疗药物。 此外，预期它们将基于它们对缩胆囊素的拮抗作用而表现出抗痴呆作用，并且可用作抗痴呆。

公开(公告)号：US5864039A

公开(公告)日：1999-01-26

申请号：US982389

申请日：1997-12-02

申请人： Takeshi Kawakita ,  Takanobu Kuroita ,  Takahiro Murozono ,  Hidetoshi Hakira ,  Keiichiro Haga ,  Katsuhiko Ito ,  Shuji Sonda ,  Toshio Kawahara ,  Kiyoshi Asano

发明人： Takeshi Kawakita ,  Takanobu Kuroita ,  Takahiro Murozono ,  Hidetoshi Hakira ,  Keiichiro Haga ,  Katsuhiko Ito ,  Shuji Sonda ,  Toshio Kawahara ,  Kiyoshi Asano

IPC分类号： C07D221/02 ,  C07D265/14

CPC分类号： C07D221/02 ,  C07D265/14

摘要： Benzoic acid compounds of the formula ##STR1## wherein each symbol is as defined in the specification, optical isomers thereof and pharmaceutically acceptable salts thereof; pharmaceutical composition comprising this compound and pharmaceutically acceptable additive; and serotonin 4 receptor agonists, gastrointestinal prokinetic agents and therapeutic agents for various gastrointestinal diseases, which comprise this compound as active ingredient. The compounds of the present invention have high and selective affinity for serotonin 4 receptor, and show agonistic effects thereon. Accordingly, they are useful medications for the prophylaxis and treatment of various gastrointestinal diseases, central nervous disorders, cardiac function disorders, urinary diseases, and the like, as well as useful anti-nociceptors for analgesic use which increase threshold of pain.

摘要翻译： 式（I）的苯甲酸化合物，其中每个符号如说明书中所定义，其光学异构体和其药学上可接受的盐; 包含该化合物和药学上可接受的添加剂的药物组合物; 和5-羟色胺4受体激动剂，胃肠促动素和各种胃肠道疾病的治疗剂，其包含该化合物作为活性成分。 本发明化合物对5-羟色胺4受体具有高选择性的亲和力，并且对其表现出激动作用。 因此，它们是用于预防和治疗各种胃肠道疾病，中枢神经障碍，心脏功能障碍，尿病等的有用药物，以及增加疼痛阈值的有用的止痛药用抗伤害感受器。

公开(公告)号：US5616581A

公开(公告)日：1997-04-01

申请号：US460666

申请日：1995-06-02

申请人： Takeshi Kawakita ,  Mitsuharu Sano ,  Yuko Yutoku ,  Yoshifumi Ikeda ,  Keiichiro Haga

发明人： Takeshi Kawakita ,  Mitsuharu Sano ,  Yuko Yutoku ,  Yoshifumi Ikeda ,  Keiichiro Haga

IPC分类号： C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C08G65/333 ,  A61K31/44 ,  A61K31/535

CPC分类号： C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C08G65/3332

摘要： A pyridine compound of the formula ##STR1## wherein R.sup.1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R.sup.2 and R.sup.3 are each a hydrogen, a halogen or an alkyl, --P.dbd.Q-- is --CH.dbd.CH--, --N.dbd.CH-- or --CH.dbd.N--, A is an oxygen atom, a sulfur atom or N(R.sup.4) wherein R.sup.4 is hydrogen, alkyl or the like, n is 0, 1 or 2, B is S(O)p wherein p is 0, 1 or 2, D is a single bond, an alkylene or the like and E is an alkoxyalkyl or --N(R.sup.6)(R.sup.7), and a pharmaceutically acceptable salt thereof have antibacterial activity against Helicobacter pylori, antiulcer activity, gastrointestinal cytoprotective activity, ulcer recurrence, relapse-preventive activity and gastric acid secretion-suppressive activity and are useful as pharmaceutical preparations.

摘要翻译： 式（I）的吡啶化合物其中R 1是氢，卤素，烷基，烷氧基等，R 2和R 3各自是氢，卤素或烷基，-P = Q-是 -CH = CH-，-N = CH-或-CH = N-，A是氧原子，硫原子或其中R4是氢，烷基等的N（R4），n是0,1或2， B是S（O）p，其中p是0,1或2，D是单键，亚烷基等，E是烷氧基烷基或-N（R6）（R7），其药学上可接受的盐具有抗菌性 针对幽门螺杆菌的活性，抗溃疡活性，胃肠细胞保护活性，溃疡复发，复发预防活性和胃酸分泌抑制活性，可用作药物制剂。

公开(公告)号：US5504082A

公开(公告)日：1996-04-02

申请号：US352183

申请日：1994-12-01

申请人： Takeshi Kawakita ,  Mitsuharu Sano ,  Yuko Yutoku ,  Yoshifumi Ikeda ,  Keiichiro Haga

发明人： Takeshi Kawakita ,  Mitsuharu Sano ,  Yuko Yutoku ,  Yoshifumi Ikeda ,  Keiichiro Haga

IPC分类号： C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C08G65/333 ,  A61K31/44 ,  A61K31/535 ,  C07D413/14

CPC分类号： C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C08G65/3332

摘要： A pyridine compound of the formula ##STR1## wherein R.sup.1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R.sup.2 and R.sup.3 are each a hydrogen, a halogen or an alkyl, --P.dbd.Q-- is --CH.dbd.CH--, --N.dbd.CH-- or --CH.dbd.N--, A is an oxygen atom, a sulfur atom or N(R.sup.4) wherein R.sup.4 is hydrogen, alkyl or the like, n is 0, 1 or 2, B is S(O)p wherein p is 0, 1 or 2, D is a single bond, an alkylene or the like and E is an alkoxyalkyl or --N(R.sup.6)(R.sup.7), and a pharmaceutically acceptable salt thereof have antibacterial activity against Helicobater pylori, antiulcer activity, gastrointestinal cytoprotective activity, ulcer recurrence, relapse-preventive activity and gastric acid secretion-suppressive activity and are useful as pharmaceutical preparations.

摘要翻译： 式（I）的吡啶化合物其中R 1是氢，卤素，烷基，烷氧基等，R 2和R 3各自是氢，卤素或烷基，-P = Q-是 -CH = CH-，-N = CH-或-CH = N-，A是氧原子，硫原子或其中R4是氢，烷基等的N（R4），n是0,1或2， B是S（O）p，其中p是0,1或2，D是单键，亚烷基等，E是烷氧基烷基或-N（R6）（R7），其药学上可接受的盐具有抗菌性 针对幽门螺旋杆菌的活性，抗溃疡活性，胃肠细胞保护活性，溃疡复发，复发预防活性和胃酸分泌抑制活性，可用作药物制剂。