公开(公告)号：EP0323042A1

公开(公告)日：1989-07-05

申请号：EP88311422.5

申请日：1988-12-02

申请人： FISONS plc

发明人： Cooper, Martin Edward ,  Donald, David Keith ,  Hardern, David Norman

IPC分类号： C07H19/01 ,  C07D498/18 ,  C07D498/22 ,  A61K31/70 ,  A61K31/33

CPC分类号： C07D498/18 ,  C07D498/22 ,  C07H19/01

摘要： Compounds of formula I
in which [R¹ and R²], [R³ and R⁴] and [R⁵ and R⁶] represent a carbon-carbon bond or two hydrogen atoms;
R² additionally represents alkyl;
R⁷, R⁸ and R⁹ represent groups including H or OH,
R¹⁰ has various significances including alkyl and alkenyl;
X and Y represent groups including O and (H,OH);
R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²² and R²³ represent H or alkyl;
R²⁰ and R²¹ represent groups including O, (H,OH) and (H,O-alkyl),
n is 1, 2, or 3,
and in addition, Y, R¹⁰ and R²³, together with the carbon atoms to which they are attached, may represent a neterocyclic ring,
(with certain provisos) are described.
Processes for making the compounds and pharmaceutical formulations containing them, eg for use as immunosuppressive agents, are also described.

摘要翻译： 其中[R 1和R 2]，[R 3和R 4]和[R 5和R 6]表示碳 - 碳键的式I化合物 或两个氢原子; R 2另外表示烷基; R 7，R 8和R 9表示包括H或OH的基团，R 1'具有各种含义，包括烷基和烯基; X和Y表示包括O和（H，OH）的基团; R 1，R 1，R 5，R 1，R 6，R 1，R 7，R 1，R 9， 2> 2和R 2 <3>代表H或烷基; R 2，R 2和R 2表示包括O，（H，OH）和（H，O-烷基），n为1,2或3的基团，另外，Y，R lt; 1＆gt;和＆lt; 2＆gt; 3＆gt;与它们所连接的碳原子一起可以表示杂环，（具有一定条件）。 还描述了制备含有它们的化合物和药物制剂的方法，例如用作免疫抑制剂。

公开(公告)号：EP0413532A2

公开(公告)日：1991-02-20

申请号：EP90308853.2

申请日：1990-08-10

申请人： FISONS plc

发明人： Donald, David Keith ,  Hardern, David Norman ,  Cooper, Martin Edward ,  Furber, Mark

IPC分类号： C07H19/01 ,  A61K31/70

CPC分类号： C07H19/01

摘要： There are described compounds of formula I,
wherein R¹ represents H or OH; R² represents H; in addition, R¹ and R² may together represent a second carbon-carbon bond between the carbon atoms to which they are attached; R³ represents OH or OCH₃; X represents O or (H,OH); and Y represents O or N-OR⁴, in which R⁴ represents H or alkyl C₁₋₆; provided that when R¹ is OH, R² is H and X is O, then Y does not represent O.
Processes for their production and compositions containing them, eg for use as immunosuppressive agents, are also described.

摘要翻译： 描述了式I的化合物，其中R 1表示H或OH; R 2表示H; 此外，R 1和R 2可以一起表示它们所连接的碳原子之间的第二个碳 - 碳键; R 3表示OH或OCH 3; X表示O或（H，OH）; 并且Y表示O或N-OR 4，其中R 4表示H或烷基C1-6; 条件是当R 1为OH时，R 2为H且X为O，则Y不为O。还描述了其制备方法和含有它们的组合物，例如用作免疫抑制剂。

公开(公告)号：EP0444829A2

公开(公告)日：1991-09-04

申请号：EP91301431.2

申请日：1991-02-22

申请人： FISONS plc ,  FUJISAWA PHARMACEUTICAL CO., LTD.

发明人： Cooper, Martin Edward ,  Donald, David Keith ,  Tanaka, Hirokazu

IPC分类号： C07C69/738 ,  C07C213/10 ,  C07C233/10 ,  C07C59/72 ,  C07C59/90 ,  C07D309/30 ,  A61K31/365 ,  A61K31/215

CPC分类号： C07D309/30 ,  C07C69/734 ,  C07C69/738 ,  C07C235/30 ,  C07C403/20 ,  C07C2601/14

摘要： Compounds of formula I,

wherein R¹ represents H, OH, protected OH or alkoxy; R² represents H; R³ represents O or (H,OH); R⁴ represents methyl, ethyl, propyl or allyl; R⁵ represents OH, protected OH or alkoxy; R⁶ represents OH; R⁷ represents OH, alkoxy or NR⁸R⁹ where R⁸ and R⁹ independently represent H, alkyl or aryl; in addition, R¹ and R² may together represent a second bond between the carbon atoms to which they are attached; and R⁶ and R⁷ may together represent O; and pharmaceutically acceptable salts thereof; are useful inter alia as immunosuppressive agents. The invention also provides the novel compounds of formula I.

摘要翻译： 式I化合物，其中R 1表示H，OH，保护的OH或烷氧基; R 2表示H; R 3表示O或（H，OH）; R 4代表甲基，乙基，丙基或烯丙基; R 5表示OH，保护的OH或烷氧基; R 6表示OH; R 7表示OH，烷氧基或NR 8 R 9，其中R 8和R 9独立地表示H，烷基或芳基; 此外，R 1和R 2可以一起代表它们所连接的碳原子之间的第二键; R 6和R 7可以一起表示O; 及其药学上可接受的盐; 尤其可用作免疫抑制剂。 本发明还提供了新的式I化合物。

公开(公告)号：EP0444829A3

公开(公告)日：1992-06-03

申请号：EP91301431.2

申请日：1991-02-22

申请人： FISONS plc ,  FUJISAWA PHARMACEUTICAL CO., LTD.

发明人： Cooper, Martin Edward ,  Donald, David Keith ,  Tanaka, Hirokazu

IPC分类号： C07C69/738 ,  C07C213/10 ,  C07C233/10 ,  C07C59/72 ,  C07C59/90 ,  C07D309/30 ,  A61K31/365 ,  A61K31/215

CPC分类号： C07D309/30 ,  C07C69/734 ,  C07C69/738 ,  C07C235/30 ,  C07C403/20 ,  C07C2601/14

摘要： Compounds of formula I,

wherein R¹ represents H, OH, protected OH or alkoxy; R² represents H; R³ represents O or (H,OH); R⁴ represents methyl, ethyl, propyl or allyl; R⁵ represents OH, protected OH or alkoxy; R⁶ represents OH; R⁷ represents OH, alkoxy or NR⁸R⁹ where R⁸ and R⁹ independently represent H, alkyl or aryl; in addition, R¹ and R² may together represent a second bond between the carbon atoms to which they are attached; and R⁶ and R⁷ may together represent O; and pharmaceutically acceptable salts thereof; are useful inter alia as immunosuppressive agents. The invention also provides the novel compounds of formula I.

摘要翻译： 式I化合物，其中R 1表示H，OH，保护的OH或烷氧基; R 2表示H; R 3表示O或（H，OH）; R 4代表甲基，乙基，丙基或烯丙基; R 5表示OH，保护的OH或烷氧基; R 6表示OH; R 7表示OH，烷氧基或NR 8 R 9，其中R 8和R 9独立地表示H，烷基或芳基; 此外，R 1和R 2可以一起代表它们所连接的碳原子之间的第二键; R 6和R 7可以一起表示O; 及其药学上可接受的盐; 尤其可用作免疫抑制剂。 本发明还提供了新的式I化合物。

公开(公告)号：EP0413532A3

公开(公告)日：1991-05-15

申请号：EP90308853.2

申请日：1990-08-10

申请人： FISONS plc

发明人： Donald, David Keith ,  Hardern, David Norman ,  Cooper, Martin Edward ,  Furber, Mark

IPC分类号： C07H19/01 ,  A61K31/70

CPC分类号： C07H19/01

摘要： There are described compounds of formula I,
wherein R¹ represents H or OH; R² represents H; in addition, R¹ and R² may together represent a second carbon-carbon bond between the carbon atoms to which they are attached; R³ represents OH or OCH₃; X represents O or (H,OH); and Y represents O or N-OR⁴, in which R⁴ represents H or alkyl C₁₋₆; provided that when R¹ is OH, R² is H and X is O, then Y does not represent O. Processes for their production and compositions containing them, eg for use as immunosuppressive agents, are also described.