公开(公告)号：EP0475206A3

公开(公告)日：1992-08-05

申请号：EP91114542.3

申请日：1991-08-29

Applicant: ABBOTT LABORATORIES

Inventor： Winn, Martin ,  De, Biswanath ,  Zydowsky, Thomas M. ,  Kerkman, Daniel J. ,  De Bernardis, John F. ,  Rosenberg, Saul H. ,  Shiosaki, Kazumi ,  Basha, Fatima Z. ,  Tasker, Andrew S. ,  Von Geldern, Thomas W. ,  Kester, Jeffrey A. ,  Holleman, William H.

IPC: C07D403/12 ,  A61K31/44 ,  C07D401/12 ,  C07D239/42 ,  C07D257/04 ,  C07D405/14 ,  A61K31/495

CPC classification number: C07D239/42 ,  C07D257/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

Abstract: Novel pyrimidine, pyridine, pyridazine, pyrazine and triazine compounds are provided of the formula (I).
The compounds of the invention are useful for treating hypertension, edema, renal failure, congestive heart failure, psoriasis and glaucoma, and in the prevention and treatment of atherosclerosis or to treat gastrointestinal disorders associated with enhanced contractility and/or motility of intestinal smooth muscle or to treat contractile disorders of the uterus.

公开(公告)号：EP0365992A1

公开(公告)日：1990-05-02

申请号：EP89119329.4

申请日：1989-10-18

Applicant: ABBOTT LABORATORIES

Inventor： De, Biswanath ,  Dellaria, Joseph F. ,  Baker, William R. ,  Zydowsky, Thomas M. ,  Rosenberg, Saul H. ,  Jae, Hwan Soo

IPC: C07K5/02 ,  C07D211/14 ,  C07D295/15 ,  C07D295/30 ,  C07D295/195 ,  C07D241/08 ,  C07D403/04 ,  C07D403/06 ,  C07D405/14 ,  C07D411/12 ,  C07D411/14

CPC classification number: C07D233/64 ,  A61K38/00 ,  C07C2601/14 ,  C07D211/14 ,  C07D211/76 ,  C07D213/74 ,  C07D239/42 ,  C07D241/04 ,  C07D241/08 ,  C07D243/08 ,  C07D263/10 ,  C07D263/22 ,  C07D295/15 ,  C07D403/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07K5/06139

Abstract: A renin inhibiting compound of the formula:
wherein X is N, O or CH; R 1 is absent or a functional group; A and L are independently selected from absent, C = O, S0 2 and CH 2 ; D is C = O, S0 2 or CH 2 ; Y is N or CH; R 2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R 3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.

Abstract translation: 一种具有下式的肾素抑制化合物：其中X是N，O或CH; R1不存在或官能团; A和L独立地选自C = O，SO 2和CH 2; D为C = O，SO 2或CH 2; Y为N或CH; R2是氢，低级烷基或取代的烷基; Z是功能组; R3是低级烷基或取代的烷基; n为0或1; T是模拟血管紧张素原的Leu-Val切割位点; 或其药学上可接受的盐，酯或前药。

公开(公告)号：EP0475206A2

公开(公告)日：1992-03-18

申请号：EP91114542.3

申请日：1991-08-29

Applicant: ABBOTT LABORATORIES

Inventor： Winn, Martin ,  De, Biswanath ,  Zydowsky, Thomas M. ,  Kerkman, Daniel J. ,  De Bernardis, John F. ,  Rosenberg, Saul H. ,  Shiosaki, Kazumi ,  Basha, Fatima Z. ,  Tasker, Andrew S. ,  Von Geldern, Thomas W. ,  Kester, Jeffrey A. ,  Holleman, William H.

IPC: C07D403/12 ,  A61K31/44 ,  C07D401/12 ,  C07D239/42 ,  C07D257/04 ,  C07D405/14 ,  A61K31/495

CPC classification number: C07D239/42 ,  C07D257/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

Abstract: Novel pyrimidine, pyridine, pyridazine, pyrazine and triazine compounds are provided of the formula (I).

The compounds of the invention are useful for treating hypertension, edema, renal failure, congestive heart failure, psoriasis and glaucoma, and in the prevention and treatment of atherosclerosis or to treat gastrointestinal disorders associated with enhanced contractility and/or motility of intestinal smooth muscle or to treat contractile disorders of the uterus.

Abstract translation: 由式（I）提供新的嘧啶，吡啶，哒嗪，吡嗪和三嗪化合物。 本发明的化合物可用于治疗高血压，水肿，肾衰竭，充血性心力衰竭，牛皮癣和青光眼，以及预防和治疗动脉粥样硬化或治疗与增强的肠收缩力和/或运动性相关的胃肠道疾病 平滑肌或治疗子宫收缩性疾病。

公开(公告)号：EP0364804A1

公开(公告)日：1990-04-25

申请号：EP89118270.1

申请日：1989-10-03

Applicant: ABBOTT LABORATORIES

Inventor： Fung, Anthony K. L. ,  Plattner, Jacob J. ,  Baker, William R. ,  Armiger, Yoek-Lin ,  Rosenberg, Saul H. ,  De, Biswanath ,  Mantei, Robert A. ,  Boyd, Steven A. ,  Kempf, Dale J. ,  Sham, Hing Leung ,  Kleinert, Hollis D.

IPC: C07D211/30 ,  C07D211/44 ,  C07D295/185 ,  C07D307/12 ,  C07D401/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D411/12 ,  C07D413/12 ,  A61K31/445

CPC classification number: C07D233/64 ,  C07C237/08 ,  C07C317/28 ,  C07C323/58 ,  C07C2601/14 ,  C07D203/18 ,  C07D211/44 ,  C07D211/62 ,  C07D211/96 ,  C07D295/185 ,  C07D401/12 ,  C07D407/12 ,  C07D413/12

Abstract: A renin inhibiting compound of the formula:
wherein A is a substituent; R 1 is hydrogen, loweralkyl, substituted loweralkyl or loweralkenyl; X is CH 2 , CHOH, C(O), O, S, S(O), S0 2 , NH, N(O) or -P(O)O-; R 3 is loweralkyl, loweralkenyl or substituted loweralkyl; and T is mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.

Abstract translation: 一种下列化学式的肾素抑制化合物：其中A为取代基的 R1是氢，低级烷基，取代的低级烷基或低级烯基; X是CH 2，CHOH，C（O），O，S，S（O），SO 2，NH，N（O）或-P（O） R3是低级烷基，低级烯基或取代的低级烷基; 并且T是模拟血管紧张素原的Leu-Val切割位点; 或其药学上可接受的盐，酯或前药。