公开(公告)号：US5219855A

公开(公告)日：1993-06-15

申请号：US839737

申请日：1992-02-19

申请人： Ken-Ichi Saito ,  Akihiro Tobe ,  Heitaro Iwata ,  Akemichi Baba ,  Toshio Matsuda

发明人： Ken-Ichi Saito ,  Akihiro Tobe ,  Heitaro Iwata ,  Akemichi Baba ,  Toshio Matsuda

IPC分类号： A61K31/495 ,  A61K31/505 ,  C07D317/64 ,  C07D319/18 ,  C07D321/10 ,  C07D405/12

CPC分类号： C07D405/12 ,  A61K31/495 ,  A61K31/505 ,  C07D317/64 ,  C07D319/18 ,  C07D321/10

摘要： Disclosed herein are anxiolytic drugs containing as an active ingredient a piperazine derivative represented by the following general formula (I): ##STR1## wherein m represents an integer from 2 to 4,X represents ##STR2## Ar represents a pyridyl group, a pyrimidinyl group, or a phenyl group which may be substituted with halogen atom, trifluoromethyl group, alkoxy group or alkyl group, andR.sub.1, R.sub.2 and R.sub.3 which may be identical or different represent lower alkoxy groups, or R.sub.3 is a hydrogen atom and R.sub.1 when taken together with R.sub.2 forms ##STR3## (n=1, 2 or 3); and its acid addition salt.The anxiolytic drugs disclosed herein have the high binding capacities to 5-HT.sub.1A receptor which is one of the receptors for 5-hydroxytryptamine (5-HT), thereby exerting anxiolytic effects.

摘要翻译： 本文公开了含有作为活性成分的由以下通式（I）表示的哌嗪衍生物的抗焦虑药物：其中m表示2至4的整数，X表示Ar表示 吡啶基，嘧啶基或可被卤素原子，三氟甲基，烷氧基或烷基取代的苯基，并且可以相同或不同的R 1，R 2和R 3表示低级烷氧基，或者R 3为氢 原子和R1与R2一起形成（n = 1,2或3）; 及其酸加成盐。 本文公开的抗焦虑药物具有对5-HT1A受体的高结合能力，其为5-羟色胺（5-HT）的受体之一，从而发挥抗焦虑作用。

公开(公告)号：US5168099A

公开(公告)日：1992-12-01

申请号：US668480

申请日：1991-03-14

申请人： Heitaro Iwata ,  Akemichi Baba ,  Toshio Matsuda ,  Mitsuo Egawa ,  Akihiro Tobe ,  Kenichi Saito

发明人： Heitaro Iwata ,  Akemichi Baba ,  Toshio Matsuda ,  Mitsuo Egawa ,  Akihiro Tobe ,  Kenichi Saito

IPC分类号： A61K31/335 ,  A61K31/357 ,  A61P25/20 ,  C07D319/20 ,  C07D407/12

CPC分类号： C07D407/12 ,  C07D319/20

摘要： Optically active alkylenedioxybenzene derivatives of the formula: ##STR1## wherein m is an integer of 2-5, and n is an integer of 1-3, and acid addition salts thereof. A pharmaceutical composition containing a compound (I) or racemate, and a method of treating anxiety in a warm-blooded animal by administering the above compound (I) to said animal are also provided.

公开(公告)号：US5234948A

公开(公告)日：1993-08-10

申请号：US931340

申请日：1992-08-18

申请人： Heitaro Iwata ,  Akemichi Baba ,  Toshio Matsuda ,  Mitsuo Egawa ,  Akihiro Tobe ,  Kenichi Saito

发明人： Heitaro Iwata ,  Akemichi Baba ,  Toshio Matsuda ,  Mitsuo Egawa ,  Akihiro Tobe ,  Kenichi Saito

IPC分类号： C07D319/20 ,  C07D407/12

CPC分类号： C07D407/12 ,  C07D319/20

摘要： Optically active alkylenedioxybenzene derivatives of the formula: ##STR1## wherein m is an integer of 2-5, and n is an integer of 1-3, and acid addition salts thereof. A pharmaceutical composition containing a compound (I) or racemate, and a method of treating anxiety in a warm-blooded animal by administering the above compound (I) to said animal are also provided.

摘要翻译： 具有下式的光活性亚烷基二氧基苯衍生物：其中m是2-5的整数，n是1-3的整数，及其酸加成盐。 还提供了含有化合物（I）或外消旋体的药物组合物，以及通过向所述动物施用上述化合物（I）而在温血动物中治疗焦虑症的方法。

公开(公告)号：US20060069104A1

公开(公告)日：2006-03-30

申请号：US10509336

申请日：2003-04-03

申请人： Toshio Matsuda ,  Akemichi Baba ,  Yutaka Koyama

发明人： Toshio Matsuda ,  Akemichi Baba ,  Yutaka Koyama

IPC分类号： A61K31/495 ,  A61K31/445

CPC分类号： C07D295/32 ,  A61K31/495 ,  A61K38/4866

摘要： The present invention relates to an a neurotrophic factor production accelerator comprising, as an active ingredient, a compound represented by the formula (I) below: wherein R1 is lower alkyl, aryl, ar(lower)alkoxy, or a heterocyclic group, and the above groups may be substituted with halogen, R2 is a hydrogen atom or lower alkyl, R3 is cyclo(lower)alkyl, aryl or ar(lower)alkyl, and the above groups may be substituted with halogen, A is —CO—, —SO2— or lower alkylene, X is N or CH, Y is —CO—, —SO2— or —CONH—, a salt, a prodrug or a solvate thereof. According to the present invention, a neurotrophic factor production accelerator, which is useful for the prophylaxis or treatment of a motor nervous system or peripheral nervous system disease, can be provided.

摘要翻译： 本发明涉及一种神经营养因子生成促进剂，其包含作为活性成分的下式（I）表示的化合物：

公开(公告)号：US20060234936A1

公开(公告)日：2006-10-19

申请号：US11362927

申请日：2006-02-28

申请人： Akemichi Baba ,  Hitoshi Hashimoto ,  Norihito Shintani ,  Yukihiko Sugimoto

发明人： Akemichi Baba ,  Hitoshi Hashimoto ,  Norihito Shintani ,  Yukihiko Sugimoto

IPC分类号： A61K38/22 ,  A61K31/70 ,  A61K31/426 ,  A61K31/155 ,  A61K31/175

CPC分类号： G01N33/507 ,  A61K38/2278 ,  A61K45/06 ,  G01N33/5088 ,  A61K2300/00

摘要： There are provided PACAP which is a substance capable of inhibiting the hyperplasia of pancreatic cells and/or the hypersecretion of insulin by pancreatic cells, a method for inhibiting the hyperplasia of pancreatic cells and/or the hypersecretion of insulin by pancreatic cells in a human by PACAP administration, a pharmaceutical composition containing PACAP and, optionally, an anti-diabetic agent, and a method for evaluating a substance capable of inhibiting the hyperplasia of pancreatic cells and/or the hypersecretion of insulin by pancreatic cells relying on the expression of Reg IIIβ to be stimulated by PACAP as an index.

公开(公告)号：US20060154861A1

公开(公告)日：2006-07-13

申请号：US11257107

申请日：2005-10-25

申请人： Akemichi Baba ,  Hitoshi Hashimoto ,  Norihito Shintani ,  Yukihiko Sugimoto

发明人： Akemichi Baba ,  Hitoshi Hashimoto ,  Norihito Shintani ,  Yukihiko Sugimoto

IPC分类号： A61K38/22

CPC分类号： G01N33/507 ,  A61K38/2278 ,  A61K45/06 ,  G01N33/5088 ,  A61K2300/00

摘要： There are provided PACAP which is a substance capable of inhibiting the hyperplasia of pancreatic cells and/or the hypersecretion of insulin by pancreatic cells, a method for inhibiting the hyperplasia of pancreatic cells and/or the hypersecretion of insulin by pancreatic cells in a human by PACAP administration, a pharmaceutical composition containing PACAP and, optionally, an anti-diabetic agent, and a method for evaluating a substance capable of inhibiting the hyperplasia of pancreatic cells and/or the hypersecretion of insulin by pancreatic cells relying on the expression of Reg IIIβ to be stimulated by PACAP as an index.

摘要翻译： 提供了PACAP，其是能够抑制胰腺细胞增生和/或胰腺细胞分泌胰岛素的物质，抑制胰腺细胞增生的方法和/或胰腺胰腺细胞在人类中的过度分泌的方法 PACAP给药，含有PACAP的药物组合物和任选的抗糖尿病药物，以及依赖于Reg IIIbeta的表达来评估能够抑制胰腺细胞增生和/或胰腺胰岛素过度分泌的物质的方法 被PACAP刺激为指标。