发明公开
EP0116713A1 Novel labdane derivatives, process for the preparation thereof, and pharmaceutical compositions containing labdane derivatives
失效
半日花烷衍生物，它们的制备方法和含有半日花烷衍生物的药物制剂。
- 专利标题： Novel labdane derivatives, process for the preparation thereof, and pharmaceutical compositions containing labdane derivatives
- 专利标题（中）： 半日花烷衍生物，它们的制备方法和含有半日花烷衍生物的药物制剂。
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申请号： EP83112756.8申请日： 1983-12-19
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公开(公告)号： EP0116713A1公开(公告)日： 1984-08-29
- 发明人: Kreutner, William , Green, Michael John , Saksena, Anil Kumar , Shue, Ho-Jane
- 申请人： SCHERING CORPORATION
- 申请人地址： 2000 Galloping Hill Road Kenilworth New Jersey 07033 US
- 专利权人： SCHERING CORPORATION
- 当前专利权人： SCHERING CORPORATION
- 当前专利权人地址： 2000 Galloping Hill Road Kenilworth New Jersey 07033 US
- 代理机构： Antony, Fritz, Dr.
- 优先权： US453436 19821227; US542825 19831017
- 主分类号： C07D311/92
- IPC分类号： C07D311/92 ; C07D409/04
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.
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.
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