公开(公告)号：US5401767A

公开(公告)日：1995-03-28

申请号：US997266

申请日：1992-12-21

申请人： Robert D. Sindelar ,  Barton J. Bradbury ,  Teodoro Kaufman ,  Stephen H. Ip ,  Henry C. Marsh, Jr.

发明人： Robert D. Sindelar ,  Barton J. Bradbury ,  Teodoro Kaufman ,  Stephen H. Ip ,  Henry C. Marsh, Jr.

IPC分类号： C07D307/94 ,  A61K31/335 ,  A61K31/16 ,  A61K31/34

CPC分类号： C07D307/94 ,  Y10S514/825 ,  Y10S514/885

摘要： The present invention is directed to compounds which suppress immune responses and/or selectively inhibit complement. These compounds contain an aromatic ring and are substituted dihydrobenzofurans, spirobenzofuran-2(3H)-cycloalkanes, and their open chain intermediates. The compounds of the present invention, and the pharmaceutically acceptable salts thereof, interrupt the proteolytic processing of C5 to bioactive components, exhibit immunosuppressive activities, and have therapeutic utility in the amelioration of disease and disorders mediated by complement and/or immune activity.

公开(公告)号：US5366986A

公开(公告)日：1994-11-22

申请号：US623849

申请日：1990-12-06

申请人： Robert D. Sindelar ,  Barton J. Bradbury ,  Teodoro S. Kaufman ,  Stephen H. Ip ,  Henry C. Marsh, Jr. ,  Chew Lee

发明人： Robert D. Sindelar ,  Barton J. Bradbury ,  Teodoro S. Kaufman ,  Stephen H. Ip ,  Henry C. Marsh, Jr. ,  Chew Lee

IPC分类号： A61K31/34 ,  A61P37/06 ,  C07D307/94 ,  C07D493/04 ,  A61K31/42 ,  A61K31/41

CPC分类号： C07D307/94

摘要： The present invention is directed to compounds which suppress immune responses and/or selectively inhibit complement. These compounds contain an aromatic ring and are substituted dihydrobenzofurans, spirobenzofuran-2(3H)-cycloalkanes, and their open chain intermediates. The compounds of the present invention, and the phamaceutically acceptable salts thereof, interrupt the proteolytic processing of C5 to bioactive components, exhibit immunosuppressive activites, and have therapeutic utility in the amelioration of disease and disorders mediated by complement and/or immune activity.

摘要翻译： 本发明涉及抑制免疫应答和/或选择性抑制补体的化合物。 这些化合物含有芳环，是取代的二氢苯并呋喃，螺苯并呋喃-2（3H） - 环烷烃及其开链中间体。 本发明的化合物及其药学上可接受的盐中断了C5对生物活性成分的蛋白水解加工，表现出免疫抑制活性，并且具有改善由补体和/或免疫活性介导的疾病和病症的治疗效用。

公开(公告)号：US5173499A

公开(公告)日：1992-12-22

申请号：US182275

申请日：1988-04-15

申请人： Robert D. Sindelar ,  Barton J. Bradbury ,  Teodoro Kaufman ,  Stephen H. Ip ,  Henry C. Marsh, Jr.

发明人： Robert D. Sindelar ,  Barton J. Bradbury ,  Teodoro Kaufman ,  Stephen H. Ip ,  Henry C. Marsh, Jr.

IPC分类号： C07D307/94

CPC分类号： C07D307/94 ,  Y10S514/825 ,  Y10S514/885

摘要： The present invention is directed to compounds which suppress immune responses and/or selectively inhibit complement. These compounds contain an aromatic ring and are substituted dihydrobenzofurans, spirobenzofuran-2(3H)-cycloalkanes, and their open chain intermediates. The compounds of the present invention, and the pharmaceutically acceptable salts thereof, interrupt the proteolytic processing of C5 to bioactive components, exhibit immunosuppressive activities, and have therapeutic utility in the amelioration of disease and disorders mediated by complement and/or immune activity.

摘要翻译： 本发明涉及抑制免疫应答和/或选择性抑制补体的化合物。 这些化合物含有芳环，是取代的二氢苯并呋喃，螺苯并呋喃-2（3H） - 环烷烃及其开链中间体。 本发明的化合物及其药学上可接受的盐中断了C5对生物活性成分的蛋白水解加工，表现出免疫抑制活性，并且具有改善由补体和/或免疫活性介导的疾病和病症的治疗效用。