公开(公告)号：US06852734B2

公开(公告)日：2005-02-08

申请号：US10275111

申请日：2001-05-01

申请人： Yasuo Yamamoto ,  Kenzo Hariyama ,  Yumiko Yanagisawa ,  Sojiro Shiokawa ,  Takumi Takeyasu ,  Osami Takenouchi ,  Hidenori Kasai

发明人： Yasuo Yamamoto ,  Kenzo Hariyama ,  Yumiko Yanagisawa ,  Sojiro Shiokawa ,  Takumi Takeyasu ,  Osami Takenouchi ,  Hidenori Kasai

IPC分类号： A61K31/4045 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/5377 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D401/06 ,  C07D405/06 ,  C07D405/14 ,  C07D471/04 ,  A61K31/47 ,  C07D209/02 ,  C07D215/16 ,  C07D491/02 ,  C07D515/02

CPC分类号： C07D401/06 ,  A61K31/4045 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/5377 ,  C07D405/06 ,  C07D405/14 ,  C07D471/04

摘要： According to this invention, there is provided an indole derivative having the general formula (I) wherein A is an oxygen atom or a nitrogen atom which nitrogen atom is optionally substituted with an alkyl group, and (i) R1 and R2 each stand for a hydrogen atom or an alkyl group, independently, or (ii) R1 and R2 as taken together form a cycloalkyl group or an aromatic ring, or (iii) R1 and R2 as taken together form a heterocyclic ring, and R3 is a hydrogen atom, a (C1-C10)alkyl group or others, R4 is a substituted alkyl group and R5 is a hydrogen atom, a halogen atom, an alkyl group or an alkoxy group and so on, as novel compounds by a novel chemical synthetic process. The indole derivative of formula (I) exhibits a useful chymase inhibitory activity.

摘要翻译： 根据本发明，提供了具有通式（I）的吲哚衍生物，其中A是氧原子或氮原子，其氮原子任选地被烷基取代，和（i）R 1和R 2， 每个代表氢原子或烷基，独立地或（ii）R 1和R 2一起形成环烷基或芳环，或（iii）R 1和R 2 一起形成杂环，R 3为氢原子，（C1-C10）烷基等，R 4为取代烷基，R 5为氢原子 ，卤素原子，烷基或烷氧基等，作为新化合物，通过新的化学合成方法。 式（I）的吲哚衍生物显示出有用的胃促胰酶抑制活性。

公开(公告)号：US07045516B1

公开(公告)日：2006-05-16

申请号：US09856372

申请日：1999-11-19

申请人： Sojiro Shiokawa ,  Yasuo Sato ,  Masaaki Izumi ,  Satoshi Yoshida ,  Tomoko Ito ,  Tetsutaro Niisato ,  Hiroshi Murakami

发明人： Sojiro Shiokawa ,  Yasuo Sato ,  Masaaki Izumi ,  Satoshi Yoshida ,  Tomoko Ito ,  Tetsutaro Niisato ,  Hiroshi Murakami

IPC分类号： A61P1/00 ,  A61K31/55 ,  C07D243/08

CPC分类号： C07D413/04 ,  Y02P20/55

摘要： A compound represented by the following general formula (1): wherein R1 represents a halogen atom, R2 represents hydrogen atom or a lower alkyl group, and R3 represents hydrogen atom, a lower alkyl group, a lower alkoxyl group, a hydroxy lower alkyl group, a halogen atom, or a substituted or unsubstituted amino group, wherein a substituent on the amino group is selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkylcarbonyl group, and an amino protective group, or a salt thereof. The compound of the present invention or a salt thereof is useful as an active ingredient of medicaments for preventive and/or therapeutic treatment of conditions of irritable bowel syndrome and digestive tract functional disorder, or condition of diarrhea.

摘要翻译： 由以下通式（1）表示的化合物：其中R 1表示卤素原子，R 2表示氢原子或低级烷基，R“ 3表示氢原子，低级烷基，低级烷氧基，羟基低级烷基，卤素原子或取代或未取代的氨基，其中氨基上的取代基选自 的低级烷基，低级烯基，低级烷基羰基和氨基保护基，或其盐。 本发明的化合物或其盐可用作预防和/或治疗肠易激综合征，消化道功能紊乱或腹泻状况的药物的活性成分。