公开(公告)号：US5128346A

公开(公告)日：1992-07-07

申请号：US571945

申请日：1990-08-23

申请人： Alex M. Nadzan ,  James F. Kerwin ,  Chun W. Lin

发明人： Alex M. Nadzan ,  James F. Kerwin ,  Chun W. Lin

IPC分类号： C07C271/22 ,  C07C275/28 ,  C07D209/42 ,  C07D213/56 ,  C07D215/48 ,  C07D241/44 ,  C07D401/12 ,  C07K5/072

CPC分类号： C07D401/12 ,  C07C271/22 ,  C07C275/28 ,  C07D209/42 ,  C07D213/56 ,  C07D215/48 ,  C07D241/44 ,  C07K5/06104

摘要： A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are substituents; R.sub.6 is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is a bond, an alkylene group, an alkenylene group, an alkadienylene group or a heteroatom containing linking group; D is a substituted acyl group or tetrazolyl; Z is CO, C(S) or S(O).sub.2 ; Ar is a heterocyclic group; and n is 1 to 3.Also disclosed are a composition and a method for antagonizing CCK, a composition and method for treating or preventing gastrointestinal, central nervous, appetite regulating and pain regulating systems, a composition and method for treating or preventing hyperinsulinemia, methods of making the compounds and intermediates useful in making the compounds.

摘要翻译： 下式的化合物：其中R1和R2是取代基; R6是氢，低级烷基，环烷基，低级烯基，芳基烷基，（取代的芳基）烷基或（杂环）烷基; B是键，亚烷基，亚烯基，亚二烯基或含杂原子的连接基团; D是取代的酰基或四唑基; Z是CO，C（S）或S（O）2; Ar是杂环基; 还公开了拮抗CCK的组合物和方法，治疗或预防胃肠，中枢神经，食欲调节和疼痛调节系统的组合物和方法，治疗或预防高胰岛素血症的组合物和方法，方法 使得化合物和中间体可用于制备化合物。

公开(公告)号：US4971978A

公开(公告)日：1990-11-20

申请号：US234525

申请日：1988-08-22

申请人： Alex M. Nadzan ,  James F. Kerwin ,  Chun W. Lin

发明人： Alex M. Nadzan ,  James F. Kerwin ,  Chun W. Lin

IPC分类号： C07C271/22 ,  C07C275/28 ,  C07D209/42 ,  C07D213/56 ,  C07D215/48 ,  C07D241/44 ,  C07D401/12 ,  C07K5/072

CPC分类号： C07D401/12 ,  C07C271/22 ,  C07C275/28 ,  C07D209/42 ,  C07D213/56 ,  C07D215/48 ,  C07D241/44 ,  C07K5/06104

摘要： A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are substituents; R.sub.6 is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is a bond, an alkylene group, an alkenylene group, an alkadienylene group or a heteroatom containing linking group; D is a substituted acyl group or tetrazolyl; Z is CO, C(S) or S(O).sub.2 ; Ar is a heterocyclic group; and n is 1 to 3.Also disclosed are a composition and a method for antagonizing CCK, a composition and method for treating or preventing gastrointestinal, central nervous, appetite regulating and pain regulating systems, a composition and method for treating or preventing hyperinsulinemia, methods of making the compounds and intermediates useful in making the compounds.

公开(公告)号：US5270302A

公开(公告)日：1993-12-14

申请号：US713010

申请日：1991-06-17

申请人： Kazumi Shiosaki ,  Alex M. Nadzan ,  Hana Kopecka ,  Youe-Kong Shue ,  Mark W. Holladay ,  Chun W. Lin ,  Hugh N. Nellans

发明人： Kazumi Shiosaki ,  Alex M. Nadzan ,  Hana Kopecka ,  Youe-Kong Shue ,  Mark W. Holladay ,  Chun W. Lin ,  Hugh N. Nellans

IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/09 ,  C07K5/097 ,  C07K5/107 ,  C07K5/117 ,  C07K14/595 ,  A61K37/02 ,  C07K5/08 ,  C07K5/10

CPC分类号： C07K5/0215 ,  C07K14/595 ,  C07K5/0207 ,  C07K5/0815 ,  C07K5/0821 ,  C07K5/1016 ,  C07K5/1024 ,  A61K38/00

摘要： Selective and potent Type-A CCK receptor agonists of formula (I):X--Y--Z--Q (I)or a pharmaceutically acceptable salt thereof, wherein,X is selected from ##STR1## Y is selected from ##STR2## Z is ##STR3## and Q is ##STR4## or pharmaceutically-acceptable salts thereof, useful in the treatment of gastrointestinal disorders (including gallbladder disorders), central nervous system disorders, insulin-related disorders and pain, as well as in appetite regulation.

摘要翻译： 选择性和有效的式（I）的CCK受体激动剂：XYZQ（I）或其药学上可接受的盐，其中X选自 Y，其中Z是，Q是 可用于治疗胃肠道疾病（包括胆囊疾病），中枢神经系统疾病，胰岛素相关疾病和疼痛以及食欲调节中的“IMAGE”或其药学上可接受的盐。