公开(公告)号：US5321031A

公开(公告)日：1994-06-14

申请号：US950379

申请日：1992-09-23

Applicant: Sundeep Dugar

Inventor： Sundeep Dugar

IPC: C07D295/12 ,  A61K31/165 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61P9/10 ,  A61P43/00 ,  C07C231/10 ,  C07C233/09 ,  C07D211/44 ,  C07D211/58 ,  C07D211/72 ,  C07D211/74 ,  C07D221/20 ,  C07D295/125 ,  C07D295/18 ,  C07D295/185 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113 ,  A61K31/44 ,  C07C233/01 ,  C07D241/04

CPC classification number: C07D221/20 ,  C07C233/09 ,  C07D211/44 ,  C07D211/58 ,  C07D211/72 ,  C07D211/74 ,  C07D295/125 ,  C07D295/185 ,  C07D491/10 ,  C07C2101/14

Abstract: Amides of the formula ##STR1## wherein: R.sup.1 is A and R.sup.2 is B; R.sup.1 is B and R.sup.2 is A; or R.sup.1 and R.sup.2 are independently selected from the group B;A is phenyl, substituted phenyl, heteroaryl, or substituted heteroaryl;B is cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl;R.sup.3 is an alkyl chain of 1 to 25 carbon atoms, branched or straight; an alkenyl chain of 2 to 25 carbon atoms, branched or straight; a substituted alkyl chain; a substituted alkenyl chain; an interrupted alkyl chain; an interrupted alkenyl chain; a substituted interrupted alkyl chain; or a substituted interrupted alkenyl chain;R.sup.4 is hydrogen, lower alkyl, phenyl, Q-substituted phenyl, heteroaryl or Q-substituted heteroaryl;R.sup.6 and R.sup.7 are both H, or R.sup.6 and R.sup.7 together represent =O;or a pharmaceutically acceptable salt thereof;useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.

Abstract translation: 下式的酰胺：其中：R1是A，R2是B; R1为B，R2为A; 或R 1和R 2独立地选自B组; A是苯基，取代的苯基，杂芳基或取代的杂芳基; B是环烷基，取代的环烷基，杂环烷基或取代的杂环烷基; R3是1至25个碳原子的烷基链，分支或直链; 2至25个碳原子的链烯基，分支或直链; 取代的烷基链; 取代烯基链; 中断的烷基链; 中断的烯基链; 取代的中断的烷基链; 或取代的中断的烯基链; R4是氢，低级烷基，苯基，Q-取代的苯基，杂芳基或Q-取代的杂芳基; R6和R7均为H或R6，R7一起表示= O; 或其药学上可接受的盐; 可用作酰基辅酶A的抑制剂：胆固醇酰基转移酶，因此用于治疗动脉粥样硬化。

公开(公告)号：US5149709A

公开(公告)日：1992-09-22

申请号：US547644

申请日：1990-07-03

Applicant: John Clader ,  Sundeep Dugar ,  Timothy Kogan ,  Bradley Tait ,  Wayne Vaccaro

Inventor： John Clader ,  Sundeep Dugar ,  Timothy Kogan ,  Bradley Tait ,  Wayne Vaccaro

IPC: C07C233/18 ,  C07C233/20 ,  C07C233/22 ,  C07C233/36 ,  C07C233/38 ,  C07C233/40 ,  C07C233/49 ,  C07C233/51 ,  C07C235/50 ,  C07C237/22 ,  C07C271/22 ,  C07C311/08

CPC classification number: C07C233/20 ,  C07C233/18 ,  C07C233/22 ,  C07C233/36 ,  C07C233/38 ,  C07C233/40 ,  C07C233/49 ,  C07C233/51 ,  C07C235/50 ,  C07C237/22 ,  C07C271/22 ,  C07C311/08 ,  Y10S514/824

Abstract: Amides of the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently heteroaryl, X-substituted heteroaryl, X-substituted phenyl, N-substituted triazinyl or N-substituted imidazolyl;and in addition, one of R.sub.1 and R.sub.2 can be as defined above and the other can be phenyl;R.sub.3 is an alkyl chain of 2 to 25 carbon atoms, saturated or unsaturated; an alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl; an alkyl chain as defined interrupted by one or more groups independently selected from the group consisting of --O--, --S--, --SO--, --SO.sub.2 --, --NH--, --N(lower alkyl)--, --C(O)--, phenylene, X-substituted phenylene, heteroarylene and X-substituted heteroarylene; or an interrupted alkyl chain as defined substituted by one or more substituents selected from the group consisting of phenyl, X-substituted phenyl, heteroaryl and X-substituted heteroaryl;R.sub.4 is hydrogen, lower alkyl, phenyl, X-substituted phenyl, heteroaryl or X-substituted heteroaryl; or a pharmaceutically acceptable salt thereof, useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.

Abstract translation: 其中R 1和R 2独立地是杂芳基，X取代的杂芳基，X取代的苯基，N-取代的三嗪基或N-取代的咪唑基; 此外，R 1和R 2中的一个可以如上所定义，另一个可以是苯基; R3是2至25个碳原子的饱和或不饱和的烷基链; 由一个或多个选自苯基，X取代的苯基，杂芳基和X取代的杂芳基的取代基取代的烷基链; 由一个或多个独立地选自-O - ， - S - ， - SO - ， - SO 2 - ， - NH - ， - N（低级烷基） - ， - C ） - ，亚苯基，X取代亚苯基，亚杂芳基和X取代亚杂芳基; 或被一个或多个选自苯基，X取代的苯基，杂芳基和X取代的杂芳基的取代基取代的间断的烷基链; R4是氢，低级烷基，苯基，X取代的苯基，杂芳基或X取代的杂芳基; 或其药学上可接受的盐，其可用作酰基辅酶A的抑制剂：胆固醇酰基转移酶，因此用于治疗动脉粥样硬化。