公开(公告)号：EP1056704A1

公开(公告)日：2000-12-06

申请号：EP99907161.6

申请日：1999-02-19

申请人： The Regents of the University of California ,  McMorris, Trevor C. ,  Kelner, Michael J.

发明人： MCMORRIS, Trevor, C. ,  KELNER, Michael, J.

IPC分类号： C07C49/497 ,  C07C49/517 ,  C07C69/16 ,  C07C69/18 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07D207/16 ,  C07K5/065 ,  A61K31/12 ,  A61K31/16 ,  A61K31/195 ,  A61K31/25 ,  A61K38/05

CPC分类号： C07C69/013 ,  A61K38/00 ,  C07C49/737 ,  C07C49/753 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07D207/16 ,  C07K5/0215 ,  C07K5/081 ,  C07K5/1013 ,  Y02A50/395

摘要： The present invention provides illudin analogs of the general formula I:wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.

公开(公告)号：EP0915819B1

公开(公告)日：2004-05-26

申请号：EP97932586.7

申请日：1997-07-14

申请人： The Regents of the University of California

发明人： MCMORRIS, Trevor, C. ,  KELNER, Michael, J.

IPC分类号： C07C49/737 ,  C07C49/755 ,  C07H15/18 ,  C07C69/007 ,  C07C323/22 ,  C07C323/52 ,  C07C39/225 ,  C07F7/18 ,  C07C49/757 ,  C07C205/45 ,  A61K31/12

CPC分类号： C07D317/72 ,  C07C35/37 ,  C07C39/17 ,  C07C49/737 ,  C07C49/755 ,  C07C49/757 ,  C07C59/90 ,  C07C69/007 ,  C07C69/96 ,  C07C205/45 ,  C07C323/22 ,  C07C323/52 ,  C07C323/58 ,  C07C2601/14 ,  C07C2603/94 ,  C07D233/54 ,  C07D319/08 ,  C07F7/1856 ,  C07H15/18

摘要： The present invention provides illudin analogs of general formula (I) where R1 is (CH2)n-X-Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C1-C8)alkyl, (C6-C10)aryl, (C6-C10)aryl(C1-C4)alkyl or cyclo(C3-C6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R2 is absent; or R1 and R2 together comprise a 5-7-membered cyclic ring; R3 is (C1-C4)alkyl or H; R4 is H, SCH2CO2(C1-C4)alkyl, O-(C5-C12)aryl or -S-(C5-C12)aryl; R5 is H, OH or absent; R6 is (C1-C4)alkyl or absent; R7 is OH or OSi((C1-C4)alkyl)3; or R6 and R7 together are ethylenedioxy; R8 is optionally substituted (C1-C4)alkyl; and the bonds represented by ----- are individually present or absent. The invention further provides dimers comprising analogs for formula (I).

公开(公告)号：EP1056704B1

公开(公告)日：2003-05-02

申请号：EP99907161.6

申请日：1999-02-19

申请人： The Regents of the University of California

发明人： MCMORRIS, Trevor, C. ,  KELNER, Michael, J.

IPC分类号： C07C49/497 ,  C07C49/517 ,  C07C69/16 ,  C07C69/18 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07D207/16 ,  C07K5/065 ,  A61K31/12 ,  A61K31/16 ,  A61K31/195 ,  A61K31/25 ,  A61K38/05

CPC分类号： C07C69/013 ,  A61K38/00 ,  C07C49/737 ,  C07C49/753 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07D207/16 ,  C07K5/0215 ,  C07K5/081 ,  C07K5/1013 ,  Y02A50/395

摘要： The present invention provides illudin analogs of the general formula I:wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.

公开(公告)号：EP0915819A1

公开(公告)日：1999-05-19

申请号：EP97932586.0

申请日：1997-07-14

申请人： The Regents of the University of California

发明人： MCMORRIS, Trevor, C. ,  KELNER, Michael, J.

IPC分类号： C07D233 ,  A61K9 ,  A61K31 ,  A61P35 ,  C07C35 ,  C07C39 ,  C07C49 ,  C07C59 ,  C07C69 ,  C07C205 ,  C07C323 ,  C07D317 ,  C07D319 ,  C07F7 ,  C07H15

CPC分类号： C07D317/72 ,  C07C35/37 ,  C07C39/17 ,  C07C49/737 ,  C07C49/755 ,  C07C49/757 ,  C07C59/90 ,  C07C69/007 ,  C07C69/96 ,  C07C205/45 ,  C07C323/22 ,  C07C323/52 ,  C07C323/58 ,  C07C2601/14 ,  C07C2603/94 ,  C07D233/54 ,  C07D319/08 ,  C07F7/1856 ,  C07H15/18

摘要： The present invention provides illudin analogs of general formula (I) where R1 is (CH2)n-X-Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C1-C8)alkyl, (C6-C10)aryl, (C6-C10)aryl(C1-C4)alkyl or cyclo(C3-C6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R2 is absent; or R1 and R2 together comprise a 5-7-membered cyclic ring; R3 is (C1-C4)alkyl or H; R4 is H, SCH2CO2(C1-C4)alkyl, O-(C5-C12)aryl or -S-(C5-C12)aryl; R5 is H, OH or absent; R6 is (C1-C4)alkyl or absent; R7 is OH or OSi((C1-C4)alkyl)3; or R6 and R7 together are ethylenedioxy; R8 is optionally substituted (C1-C4)alkyl; and the bonds represented by ----- are individually present or absent. The invention further provides dimers comprising analogs for formula (I).

摘要翻译： 本发明提供通式（I）的illudin类似物，其中R 1是（CH 2）n -X-Y或H; n为0〜4; X为O或S或N或不存在; 并且Y是任选地包含一个或多个杂原子的任选取代的（C 1 -C 8）烷基，（C 6 -C 10）芳基，（C 6 -C 10）芳基（C 1 -C 4）烷基或环（C 3 -C 6） 当n为2-4时，单糖，氨基酸残基或H; R2不存在 或者R 1和R 2一起包含5-7元环; R3是（C1-C4）烷基或H; R4是H，SCH2CO2（C1-C4）烷基，O-（C5-C12）芳基或-S-（C5-C12）芳基; R5为H，OH或不存在; R6是（C1-C4）烷基或不存在; R7是OH或OSi（（C1-C4）烷基）3; 或R6和R7一起是亚乙二氧基; R8是任选取代的（C 1 -C 4）烷基，并且由----表示的键单独存在或不存在。 本发明还提供包含式（I）的类似物的二聚体。