公开(公告)号：EP0288640B1

公开(公告)日：1992-09-09

申请号：EP87309349.6

申请日：1987-10-22

申请人： SCHERING CORPORATION

发明人： Piwinsky, John J. ,  Green, Michael John ,  Ganguly, Ashit Kumar ,  Wong, Jesse Kwok-Keung ,  Katchen, Bernard ,  Cramer, Jeffrey Abbott

IPC分类号： C07D401/04 ,  A61K31/445

CPC分类号： C07D401/04

公开(公告)号：EP0116713A1

公开(公告)日：1984-08-29

申请号：EP83112756.8

申请日：1983-12-19

申请人： SCHERING CORPORATION

发明人： Kreutner, William ,  Green, Michael John ,  Saksena, Anil Kumar ,  Shue, Ho-Jane

IPC分类号： C07D311/92 ,  C07D409/04

CPC分类号： C07D409/04 ,  C07D311/92

摘要： This invention relates to a pharmaceutical composition eliciting an antiallergic andior bronchodilatory effect, which comprises a compound of general formula I
including the 5,6 and 6,7 dehydro derivatives, in the free form or in the form of its solvate,

wherein U is =O or (H,R 1 ) ;
V is =0 or (H,R 2 );
wherein R, is H or OR 11 , wherein R 11 is H or acyl, R 2 is H, OR 11 , OSO 2 R' or OR', wherein R' is alkyl; or when R, and R 2 are taken together they may form


R 3 is hydrogen, alkyl, CH 2 0H, CHO, CO 2 R 15 , -CH=CR 16 R 17 , -C≡C-R 18 , -CHOH-C≡C-R 19 ;
-CH=C=CHR 19 , -CH=H-OR 19 ,
wherein Z is O or
-CH=N-NDE or -CH(ZR 20 ) 2 wherein Z is defined as above;
R 4 is H or OH;
R 5 is OH; or when
R 4 and R 5 are taken together they may form
wherein Z is defined as above;
X is 0 or H'OR" wherein R" is H, carboxylic acyl or trifluoroacetyl;
Q is hydrogen, chlorine or bromine; or Q together with R 3 may form a bond between the carbon atoms of positions 12 and 13; whereby in the 5,6-dehydro-derivatives of formula I R 1 is H and in the 6,7-dehydro-derivatives of formula I R, and R 2 are H;
and wherein R 11 , R 13 , R 14 , T 15 , R 16 , R 17 . R 18 , R 19 , R 20 , A, B, D, and E are as defined in the claims.
Part of the compounds of formula I are new compounds.

摘要翻译： 本发明涉及的药物组合物在抗过敏和/或支气管扩张药的效果，该方法包括通式的化合物引发我... ...包括5.6和6.7脱氢衍生物，在自由形式或形式 其溶剂化物，...其中U是O或（H，R1）; ... V是O或（H，R2）; ...其中R1是H或OR 11，worin R 11是H或酰基，R 2是H，OR 11，OSO 2分钟或 OR分钟，worin R“是烷基; 或当R 1和R 2一起可形成它们... ... R3是氢，烷基，CH 2 OH，CHO，CO2R15， - CH = CR 16 R 17，-C IDENTICAL C-R18，-CHOH-C IDENTICAL C-R19; ... -CH = C = CHR19，-CH = H-OR19，... ... worin Z是O或S，... ... CN = N-NDE或... -CH（ZR20）2 worin Z为定义为 以上; ... R4是H或OH; R 5 ...是OH; 或当... R4和R5结合在一起它们可形成... ... worin Z的定义如上; ... X为O或H /或仲worinř秒为H，羧酸酰基或三氟乙酰基; ... Q是氢，氯 或溴; 或Q与R 3一起可形成位置12和13的碳原子之间的键; 由此式的5,6-脱氢衍生物I R1是H和在式-6,7-脱氢衍生物我R1和R2是H; ...和worin R11，R13，R14，T15，R16，R17， R18，R19，R20，A，B，D，和E如权利要求中限定。 式I的化合物的... 第一部分是新的化合物。

公开(公告)号：EP0288640A1

公开(公告)日：1988-11-02

申请号：EP87309349.6

申请日：1987-10-22

申请人： SCHERING CORPORATION

发明人： Piwinsky, John J. ,  Green, Michael John ,  Ganguly, Ashit Kumar ,  Wong, Jesse Kwok-Keung ,  Katchen, Bernard ,  Cramer, Jeffrey Abbott

IPC分类号： C07D401/04 ,  A61K31/445

CPC分类号： C07D401/04

摘要： Derivatives of 6,11-dihydro-11-(4-­piperidylidene)-5 H -benzo[5,6]cyclohepta[1,2-b]pyridine, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic activity, making them effective as anti-allergic compounds. Methods for preparing and using the compounds are also described.

摘要翻译： 6,11-二氢-11-（4-亚哌啶基）-5H-苯并[5,6]环庚[1,2-b]吡啶，和药学上可接受的盐和溶剂化物是游离缺失盘的衍生物，其具有抗过敏活性 ，使它们有效地作为抗过敏的化合物。 因此描述了用于制备和使用所述化合物的方法。