公开(公告)号：EP0719779A1

公开(公告)日：1996-07-03

申请号：EP95921127.7

申请日：1995-06-07

申请人： Eisai Co., Ltd.

发明人： OINUMA, Hitoshi ,  SUDA, Shinji ,  YONEDA, Naoki Tsukubasakuradanchi 906-306 ,  KOTAKE, Makoto ,  MIZUNO, Masanori ,  MATSUSHIMA, Tomohiro ,  FUKUDA, Yoshio ,  SAITO, Mamoru ,  MATSUOKA, Toshiyuki ,  ADACHI, Hideyuki ,  NAMIKI, Masayuki ,  SUDO, Takeshi ,  MIYAKE, Kazutoshi ,  OKITA, Makoto

IPC分类号： C07D513/04 ,  C07D277/06 ,  C07D211/60 ,  A61K31/425

CPC分类号： C07D513/04 ,  A61K38/00 ,  C07K5/06139 ,  Y02P20/55

摘要： The present invention relates to a substituted thiazolo[3,2-a]azepine derivative having inhibitory activity against angiotensin I converting enzyme and neutral endpeptidase.
The above substituted thiazolo[3,2-a]azepine derivative is represented by the following general formula (I):

   (wherein R1 represents a hydrogen atom or a protecting group of a thiol group; R2 represents a hydrogen atom, a lower alkyl group, an aryl group which may have a substituent, a hetroaryl group which may have a substituent, a lower alkoxyl group or a lower alkylthio group; R3, R4 and R5 may be the same or different from one another and represent each a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a lower alkylthio group or the like, with the proviso that the case wherein all of R3, R4 and R5 are hydrogen atoms are excepted;
   R6 and R7 may be the same or different from each other and represent each a hydrogen atom or a lower alkyl group; R8 represents a hydrogen atom or a protecting group of a carboxyl group; and
   m and m are each independently 0 or, 1 or 2).

摘要翻译： 本发明涉及对血管紧张素I转换酶和中性内肽酶具有抑制活性的取代噻唑并[3,2-a]氮杂衍生物。 上述取代的噻唑并[3,2-a]吖庚因衍生物由以下通式（I）表示：（其中R1表示氢原子或硫醇基的保护基; R2表示氢原子，低级烷基， 可以具有取代基的芳基，可以具有取代基的杂芳基，低级烷氧基或低级烷硫基; R3，R4和R5可以相同或不同，表示氢原子， 低级烷基，低级烷氧基，低级烷硫基等，条件是其中R3，R4和R5全部为氢原子的情况除外; R6和R7可以相同或不同， 表示氢原子或低级烷基; R8表示氢原子或羧基的保护基; m和m各自独立地为0或1或2）。

公开(公告)号：EP0719779B1

公开(公告)日：2003-11-19

申请号：EP95921127.7

申请日：1995-06-07

申请人： Eisai Co., Ltd.

发明人： OINUMA, Hitoshi ,  SUDA, Shinji ,  YONEDA, Naoki Tsukubasakuradanchi 906-306 ,  KOTAKE, Makoto ,  MIZUNO, Masanori ,  MATSUSHIMA, Tomohiro ,  FUKUDA, Yoshio ,  SAITO, Mamoru ,  MATSUOKA, Toshiyuki ,  ADACHI, Hideyuki ,  NAMIKI, Masayuki ,  SUDO, Takeshi ,  MIYAKE, Kazutoshi ,  OKITA, Makoto

IPC分类号： C07D513/04 ,  C07D277/06 ,  C07D211/60 ,  A61K31/425

CPC分类号： C07D513/04 ,  A61K38/00 ,  C07K5/06139 ,  Y02P20/55

摘要： A substituted thiazolo[3,2-α]azepine derivative represented by general formula (I) and having the effect of inhibiting an agiotensin I-converting enzyme and an atrial natriuretic peptide hydrolase, wherein R1 represents hydrogen or a thiol-protective group; R2 represents hydrogen, lower alkyl, optionally substituted aryl, optionally substituted heteroaryl, lower alkoxy or lower alkylthio; R?3, R4 and R5¿ represent each independently hydrogen, lower alkyl, lower alkoxy, lower alkylthio, etc., provided the case where all of R?3, R4 and R5¿ are hydrogen atoms at the same time is excepted; R?6 and R7¿ represent each independently hydrogen or lower alkyl; R8 represents hydrogen or a carboxyl-protective group; and m and n represent each independently 0, 1 or 2.

公开(公告)号：EP0671172A1

公开(公告)日：1995-09-13

申请号：EP94917799.2

申请日：1994-06-10

申请人： Eisai Co., Ltd.

发明人： OINUMA, Hitoshi ,  SUDA, Shinji ,  YONEDA, Naoki Tsukubasakuradanchi 906-306 ,  KOTAKE, Makoto ,  HAYASHI, Kenji ,  MIYAKE, Kazutoshi ,  MORI, Nobuyuki ,  SAITO, Mamoru ,  MATSUOKA, Toshiyuki ,  NAMIKI, Masayuki ,  SUDO, Takeshi ,  SOUDA, Shigeru

IPC分类号： A61K31/47 ,  A61K31/55 ,  A61K38/00

CPC分类号： C07D209/48 ,  A61K31/40 ,  A61K31/42 ,  A61K31/44 ,  A61K31/55 ,  C07D223/16 ,  C07D243/12 ,  C07D267/14 ,  C07D281/10 ,  C07D401/06 ,  C07D409/06 ,  C07D471/04 ,  C07D487/04 ,  C07D495/14 ,  C07D513/04 ,  C07K5/06139

摘要： An amino acid derivative having an angiotensin I-converting enzyme inhibitor activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibitor activity, and represented by general formula (I) wherein R¹ represents hydrogen or acyl; R² represents hydrogen, lower alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; m and n represent each independently an integer of 0.1 or 2; and J represents a cyclic group having an angiotensin I-converting enzyme inhibitor activity.

摘要翻译： 一种具有血管紧张素I转换酶抑制剂活性，加压素拮抗作用和心房钠尿肽水解酶抑制剂活性的氨基酸衍生物，其通式（I）表示，其中R 1代表氢或酰基; R 2代表氢，低级烷基，环烷基，任选取代的芳基，任选取代的杂芳基，任选取代的芳基烷基或任选取代的杂芳基烷基; m和n各自独立地表示0.1或2的整数; J表示具有血管紧张素I转换酶抑制剂活性的环状基团。