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1. 发明授权

US06323181B1 Antitumor agents 有权
标题翻译：抗肿瘤剂
公开(公告)号：US06323181B1
公开(公告)日：2001-11-27
申请号：US09386555
申请日：1999-08-31
申请人： Trevor C. McMorris , Michael J. Kelner
发明人： Trevor C. McMorris , Michael J. Kelner
IPC分类号： A61K3112
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.
摘要翻译：本发明提供通式I的illudin类似物：其中R1，R2，R3，R4，R5和R6具有说明书中定义的任何值及其药学上可接受的盐，以及包含式 I，可用于制备式I化合物的中间体和方法，以及通过施用一种或多种式I化合物来抑制肿瘤生长或治疗癌症的方法。

2. 发明授权

US5439942A Method of treating certain tumors using illudin analogs 失效
标题翻译：使用illudin类似物治疗某些肿瘤的方法
公开(公告)号：US5439942A
公开(公告)日：1995-08-08
申请号：US606511
申请日：1990-10-31
申请人： Michael J. Kelner , Trevor C. McMorris , Raymond Taetle
发明人： Michael J. Kelner , Trevor C. McMorris , Raymond Taetle
IPC分类号： A61K31/12 , A61K31/215 , A61K31/22 , A61K31/27 , A61P35/00 , C07C45/45 , C07C45/46 , C07C45/65 , C07C45/67 , C07C49/665 , C07C49/67 , C07C49/683 , C07C49/727 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/755 , C07C69/007 , C07C69/757 , C07C271/12
CPC分类号： C07C271/12 , A61K31/12 , A61K31/215 , A61K31/22 , A61K31/27 , C07C45/455 , C07C45/46 , C07C45/65 , C07C45/673 , C07C49/67 , C07C49/683 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/755 , C07C69/007 , C07C2103/94
摘要： A method of inhibiting certain tumor cell growth in a subject is provided comprising contacting the tumor with a therapeutic amount of an illudin S or illudin M analog having the structure ##STR1## wherein the analog is capable of inhibiting tumor cell growth without excessive toxicity to the subject and whereinR.sub.1 is hydrogen;R.sub.2 is methyl; andR.sub.3 is hydroxy.
摘要翻译：提供了抑制受试者中某些肿瘤细胞生长的方法，包括使肿瘤与治疗量的具有结构“IMAGE”的伊洛匹因S或illudin M类似物接触，其中该类似物能够抑制肿瘤细胞生长而不会对并且其中R 1是氢; R2是甲基; 并且R 3是羟基。

3. 发明授权

US06548679B1 Antitumor agents 有权
标题翻译：抗肿瘤剂
公开(公告)号：US06548679B1
公开(公告)日：2003-04-15
申请号：US09641191
申请日：2000-08-17
申请人： Trevor C. McMorris , Michael J. Kelner
发明人： Trevor C. McMorris , Michael J. Kelner
IPC分类号： A61K315375
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 compounds of general formula I or II: wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.
摘要翻译：本发明提供通式I或II的化合物：其中R1，R2，R3，R4，R5，R6和R7具有说明书中定义的任何值及其药学上可接受的盐，以及包含化合物式I或II的化合物，可用于制备式I或II化合物的中间体和方法，以及通过施用一种或多种式I或II化合物来抑制肿瘤生长或治疗癌症的方法。

4. 发明授权

US6069283A Illudin analogs useful as antitumor agents 失效
标题翻译：伊洛替丁类似物作为抗肿瘤剂有用
公开(公告)号：US6069283A
公开(公告)日：2000-05-30
申请号：US241172
申请日：1999-02-01
申请人： Trevor C. McMorris , Michael J. Kelner
发明人： Trevor C. McMorris , Michael J. Kelner
IPC分类号： C07D233/64 , A61K9/08 , A61K9/48 , A61K31/122 , A61K31/19 , A61K31/215 , A61K31/357 , A61K31/36 , A61K31/695 , A61K31/7028 , A61P35/00 , C07C35/37 , C07C39/17 , C07C49/727 , C07C49/737 , C07C49/743 , C07C49/753 , C07C49/755 , C07C49/757 , C07C59/90 , C07C69/007 , C07C69/16 , C07C69/96 , C07C205/45 , C07C323/22 , C07C323/52 , C07C323/58 , C07D233/54 , C07D317/72 , C07D319/08 , C07F7/18 , C07H15/18 , C07C49/105
CPC分类号： C07D317/72 , C07C205/45 , C07C323/22 , C07C323/52 , C07C323/58 , C07C35/37 , C07C39/17 , C07C49/737 , C07C49/755 , C07C49/757 , C07C59/90 , C07C69/007 , C07C69/96 , C07D233/54 , C07D319/08 , C07F7/1856 , C07H15/18 , C07C2101/14 , C07C2103/94
摘要： The present invention provides illudin analogs of the general formula (I): ##STR1## where R.sub.1 is (CH.sub.2).sub.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 (C.sub.1 -C.sub.8)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.4)alkyl or cyclo(C.sub.3 -C.sub.6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4;R.sub.2 is absent; or R.sub.1 and R.sub.2 together comprise a 5-7 membered cyclic ring;R.sub.3 is (C.sub.1 -C.sub.4)alkyl or H; R.sub.4 is H, SCH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl, O--(C.sub.5 -C.sub.12)aryl or --S--(C.sub.5 -C.sub.12)aryl; R.sub.5 is H, OH or absent; R.sub.6 is (C.sub.1 -C.sub.4)alkyl or absent; R.sub.7 is OH or OSi((C.sub.1 -C.sub.4)alkyl).sub.3 ; orR.sub.6 and R.sub.7 together are ethylenedioxy;R.sub.8 is optionally substituted (C.sub.1 -C.sub.4)alkyl; andthe bonds represented by ----- are individually present or absent. The invention further provides dimers comprising analogs of formula (I).
摘要翻译：本发明提供通式（I）的illudin类似物：其中R1是（CH2）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; 而-----表示的债券是单独存在或不存在的。本发明还提供包含式（I）的类似物的二聚体。

5. 发明授权

US5932553A Illudin analogs useful as antitumor agents 失效
标题翻译：伊洛替丁类似物作为抗肿瘤剂有用
公开(公告)号：US5932553A
公开(公告)日：1999-08-03
申请号：US683687
申请日：1996-07-18
申请人： Trevor C. McMorris , Michael J. Kelner
发明人： Trevor C. McMorris , Michael J. Kelner
IPC分类号： C07D233/64 , A61K9/08 , A61K9/48 , A61K31/122 , A61K31/19 , A61K31/215 , A61K31/357 , A61K31/36 , A61K31/695 , A61K31/7028 , A61P35/00 , C07C35/37 , C07C39/17 , C07C49/727 , C07C49/737 , C07C49/743 , C07C49/753 , C07C49/755 , C07C49/757 , C07C59/90 , C07C69/007 , C07C69/16 , C07C69/96 , C07C205/45 , C07C323/22 , C07C323/52 , C07C323/58 , C07D233/54 , C07D317/72 , C07D319/08 , C07F7/18 , C07H15/18 , A61K31/12 , A61K31/70
CPC分类号： C07D317/72 , C07C205/45 , C07C323/22 , C07C323/52 , C07C323/58 , C07C35/37 , C07C39/17 , C07C49/737 , C07C49/755 , C07C49/757 , C07C59/90 , C07C69/007 , C07C69/96 , C07D233/54 , C07D319/08 , C07F7/1856 , C07H15/18 , C07C2101/14 , C07C2103/94
摘要： The present invention provides illudin analogs of the general formula (I): ##STR1## where R.sub.1 is (CH.sub.2).sub.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 (C.sub.1 -C.sub.8)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.4)alkyl or cyclo(C.sub.3 -C.sub.6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R.sub.2 is absent; or R.sub.1 and R.sub.2 together comprise a 5-7 membered cyclic ring;R.sub.3 is (C.sub.1 -C.sub.4)alkyl or H; R.sub.4 is H, SCH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl, O--(C.sub.5 --C.sub.12)aryl or --S--(C.sub.5 -C.sub.12)aryl; R.sub.5 is H, OH or absent; R.sub.6 is (C.sub.1 -C.sub.4)alkyl or absent; R.sub.7 is OH or OSi((C.sub.1 -C.sub.4)alkyl).sub.3 ; orR.sub.6 and R.sub.7 together are ethylenedioxy;R.sub.8 is optionally substituted (C.sub.1 -C.sub.4)alkyl; andthe bonds represented by -- are individually present or absent. The invention further provides dimers comprising analogs of formula (I).
摘要翻译：本发明提供通式（I）的illudin类似物：其中R1是（CH2）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; 由 - 表示的债券是单独存在或不存在的。本发明还提供包含式（I）的类似物的二聚体。

6. 发明申请

US20080306147A1 Illudin Analogs Useful as Anticancer Agents 有权
标题翻译： Illudin类似物作为抗癌剂有用
公开(公告)号：US20080306147A1
公开(公告)日：2008-12-11
申请号：US11997432
申请日：2006-08-03
申请人： Trevor C. McMorris , Michael J. Kelner
发明人： Trevor C. McMorris , Michael J. Kelner
IPC分类号： A61K31/27 , C07C275/04 , A61K31/17 , A61P35/00 , C07C335/02 , C07C271/06
CPC分类号： C07C275/26 , C07C2603/97
摘要： Acylfulvene analogs, which inhibit tumor growth, especially solid tumor growth, and which have an adequate therapeutic index to be effective for in vivo treatment are provided herein. The compounds described herein are useful as anti-neoplastic agents, i.e., to inhibit tumor cell growth in vitro or in vivo, in mammalian hosts, such as humans or animals, e.g., domestic animals, and are effective against solid tumors, hematologic malignancies and multi-drug resistant cancers/tumors. The present compounds can be used alone or they can be used in combination with one or more anti-cancer or anti-tumor agents.
摘要翻译：本文提供了抑制肿瘤生长，特别是实体瘤生长的，具有足够的治疗指数以有效体内治疗的酰基类似物。本文所述的化合物可用作抗肿瘤剂，即在体内或体内抑制哺乳动物宿主例如人或动物（例如家畜）中的肿瘤细胞生长，并且可有效抵抗实体瘤，血液恶性肿瘤和多药耐药性癌症/肿瘤。本发明化合物可以单独使用，也可以与一种或多种抗癌剂或抗肿瘤剂组合使用。

7. 发明授权

US07329759B2 Illudin analogs useful as antitumor agents 失效
标题翻译：伊洛替丁类似物作为抗肿瘤剂有用
公开(公告)号：US07329759B2
公开(公告)日：2008-02-12
申请号：US11312236
申请日：2005-12-20
申请人： Trevor C. McMorris , Michael J. Kelner
发明人： Trevor C. McMorris , Michael J. Kelner
IPC分类号： C07D233/54 , C07C62/24 , C07C215/02
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 , C07F7/1804 , C07H15/18
摘要： The present invention provides illudin analogs of the 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 of formula (I).
摘要翻译：本发明提供了通式（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; 和Y是任选取代的（C 1 -C 8 - ）烷基，（C 6 -C 10）烷基，芳基（C 6 -C 10）芳基（C 1 -C 4 -C 4）烷基或环（C（C 1 -C 6）任选地包含一个或多个杂原子的C 3 -C 6烷基; 当n为2-4时，单糖，氨基酸残基或H; R 2不存在; 或R 1和R 2一起包含5-7元环; R 3是（C 1 -C 4 -C 4）烷基或H; R 4是H，SCH 2 CO 2（C 1 -C 4））烷基，O-（C 5 -C 12 - ）芳基或-S-（C 5 -C 12））芳基; R 5是H，OH或不存在; R 6是（C 1 -C 4 -C 4）烷基或不存在; R 7是OH或OSi（（C 1 -C 4 -C 4烷基）烷基）3。或R 6和R 7一起是亚乙二氧基; R 8是任选取代的（C 1 -C 4 -C 4）烷基; 而-----表示的债券是单独存在或不存在的。本发明还提供包含式（I）的类似物的二聚体。

8. 发明授权

US06855696B2 Antitumor agents 有权
标题翻译：抗肿瘤剂
公开(公告)号：US06855696B2
公开(公告)日：2005-02-15
申请号：US10013009
申请日：2001-11-05
申请人： Trevor C. McMorris , Michael J. Kelner
发明人： Trevor C. McMorris , Michael J. Kelner
IPC分类号： A61K31/12 , A61K31/16 , A61K31/195 , A61K31/25 , A61K38/00 , A61P35/00 , C07C49/737 , C07C49/753 , C07C69/013 , C07C69/16 , C07C69/18 , C07C323/58 , C07C323/59 , C07C323/60 , C07D207/16 , C07K5/02 , C07K5/065 , C07K5/083 , C07K5/103 , A61K38/05 , A61K38/06
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.
摘要翻译：本发明提供通式I的illudin类似物：其中R1，R2，R3，R4，R5和R6具有说明书中定义的任何值及其药学上可接受的盐，以及包含式 I，可用于制备式I化合物的中间体和方法，以及通过施用一种或多种式I化合物来抑制肿瘤生长或治疗癌症的方法。

9. 发明授权

US5563176A Illudin analogs useful as antitumor agents 失效
标题翻译：伊洛替丁类似物作为抗肿瘤剂有用
公开(公告)号：US5563176A
公开(公告)日：1996-10-08
申请号：US276169
申请日：1994-07-15
申请人： Michael J. Kelner , Trevor C. McMorris , Raymond Taetle
发明人： Michael J. Kelner , Trevor C. McMorris , Raymond Taetle
IPC分类号： A61K39/395 , A61K31/12 , A61K31/122 , A61K31/215 , A61K31/22 , A61K31/27 , A61P35/00 , A61P35/02 , C07C45/45 , C07C45/46 , C07C45/65 , C07C45/67 , C07C49/67 , C07C49/683 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/755 , C07C69/007 , C07C69/16 , C07C69/63 , C07C69/732 , C07C69/76 , C07C271/10 , C07C271/12 , C07C49/403
CPC分类号： A61K31/12 , A61K31/215 , A61K31/22 , A61K31/27 , C07C271/12 , C07C45/455 , C07C45/46 , C07C45/65 , C07C45/673 , C07C49/67 , C07C49/683 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/755 , C07C69/007 , C07C2103/94
摘要： Antineoplastic illudin analogs are provided of the formula: wherein R.sub.4, R.sub.5 and R.sub.6 are (C.sub.1 -C.sub.4)alkyl, Y is H, (C.sub.1 -C.sub.3)alkyl, (R.sub.4)R.sub.5)(R.sub.6)Si or alkanoyl ((C.sub.1 -C.sub.4)alkylC(O)) and R is CH.sub.2 OH, halo, benzyl optionally substituted with OY, or alkanoylmethyl (CH.sub.2 OC(O)R.sub.7), wherein R.sub.7 is (C.sub.1 -C.sub.4)alkyl, (C.sub.6 -C.sub.2)aryl or N(X).sub.2, wherein each X is H or (C.sub.1 -C.sub.4)alkyl, and the pharmaceutically-acceptable salts thereof.
摘要翻译：抗肿瘤性illudin类似物由下式提供：其中R4，R5和R6是（C1-C4）烷基，Y是H，（C1-C3）烷基，（R4）R5）（R6）Si或烷酰基（（ C1-C4）烷基C（O）），R是CH2OH，卤素，任选被OY取代的苄基或烷酰基甲基（CH2OC（O）R7），其中R7是（C1-C4）烷基，（C6-C2）（X）2，其中每个X是H或（C 1 -C 4）烷基，及其药学上可接受的盐。

10. 发明授权

US5439936A Method of treating certain tumors using illudin analogs 失效
标题翻译：使用illudin类似物治疗某些肿瘤的方法
公开(公告)号：US5439936A
公开(公告)日：1995-08-08
申请号：US15179
申请日：1993-02-09
申请人： Michael J. Kelner , Trevor C. McMorris , Raymond Taetle
发明人： Michael J. Kelner , Trevor C. McMorris , Raymond Taetle
IPC分类号： A61K39/395 , A61K31/12 , A61K31/122 , A61K31/215 , A61K31/22 , A61K31/27 , A61P35/00 , A61P35/02 , C07C45/45 , C07C45/46 , C07C45/65 , C07C45/67 , C07C49/67 , C07C49/683 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/755 , C07C69/007 , C07C69/16 , C07C69/63 , C07C69/732 , C07C69/76 , C07C271/10 , C07C271/12
CPC分类号： C07C271/12 , A61K31/12 , A61K31/215 , A61K31/22 , A61K31/27 , C07C45/455 , C07C45/46 , C07C45/65 , C07C45/673 , C07C49/67 , C07C49/683 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/755 , C07C69/007 , C07C2103/94
摘要： A therapeutic method is provided to inhibit tumor cell growth in a subject in need of said therapy is provided, comprising parenterally administering a therapeutic amount of a compound in a pharmaceutically acceptable carrier, wherein said compound has the structure: ##STR1## wherein R is selected from the group consisting of: ##STR2## and wherein said tumor cell is sensitive to inhibition by said compound and is selected from the group consisting of a myeloid leukemia cell, a T-cell leukemia cell, a lung carcinoma cell, an ovarian carcinoma cell, and a breast carcinoma cell.
摘要翻译：提供了一种用于抑制需要所述治疗的受试者的肿瘤细胞生长的治疗方法，其包括在药学上可接受的载体中肠胃外施用治疗量的化合物，其中所述化合物具有以下结构：其中R被选择来自由以下组成的组：，其中所述肿瘤细胞对所述化合物的抑制敏感，并且选自骨髓性白血病细胞，T细胞白血病细胞，肺癌细胞，卵巢癌细胞和乳腺癌细胞。

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