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：EP0461353A1

公开(公告)日：1991-12-18

申请号：EP91104766.0

申请日：1991-03-26

Applicant: ABBOTT LABORATORIES

Inventor： Basha, Fatima Z. ,  De Bernardis, John F. ,  Altenbach, Robert J.

IPC: C07D209/62 ,  C07D221/10 ,  C07D223/14 ,  C07D491/04 ,  A61K31/47

CPC classification number: C07D491/04 ,  C07D209/62 ,  C07D221/10 ,  C07D223/14

Abstract: Compounds of the formula:
or a pharmaceutically acceptable salt thereof,

wherein m is 0, 1 or 2 and n is 0 or 1;
R 1 is hydrogen or lower alkyl;
R 2 is C 1 -C 6 -alkyl substituted with a heterocyclic group or C 7 -C 16 -arylalkyl, wherein the aryl group is unsubstituted or substituted with from one to three non-hydrogen members independently selected from the group consisting of halogen, C 1 -C 6 -alkyl, halo-C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, hydroxy, amino and C 1 -C 6 -alkylamino;
R 3 , R 4 , R 5 and R 6 are independently selected from the group consisting of hydrogen, C 1 -C 6 -alkoxy, C 1 -C 6 -alkyl, halogen, and halo-C 1 -C 6 -alkyl, or any two of R 3 , R 4 , R 5 and R 6 taken together form a methylenedioxy group; and
R 7 is hydrogen or C 1 -C 6 -alkyl.

These compounds are useful as inhibitors of the neuronal uptake of biogenic amines and for the treatment of affective disorders, such as, for example, depression.

Abstract translation: 下式的化合物：其中m为0,1或2，n为0或1; R 1是氢或低级烷基; R 2是被杂环基或C 7 -C 16 - 芳基烷基取代的C 1 -C 6烷基，其中芳基是未取代的或被一至三个独立地选自卤素，C1- C 1 -C 6烷基，卤代-C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，羟基，氨基和C 1 -C 6烷基氨基; R 3，R 4，R 5和R 6独立地选自氢，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷基，卤素和卤代-C 1 -C 6 - 烷基或R 3，R 4，R 5和R 6中的任何两个一起形成亚甲二氧基; R 7是氢或C 1 -C 6烷基。 这些化合物可用作生物胺的神经元摄取和治疗情感障碍（例如抑郁症）的抑制剂。

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。