-
公开(公告)号：US07655695B2
公开(公告)日：2010-02-02
申请号：US11997432
申请日：2006-08-03
IPC分类号： A61K31/27 , A61K31/17 , A61K31/13 , C07C271/18 , C07C271/22 , C07C239/14 , C07C239/18 , C07C275/22 , C07C275/24 , C07C335/10
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。
-
公开(公告)号：US07141603B2
公开(公告)日：2006-11-28
申请号：US11151013
申请日：2005-06-13
IPC分类号： A61K31/335 , C07D317/72 , C07C49/453
CPC分类号： C07C49/737 , A61K38/063 , A61K38/08 , C07B2200/07 , C07C49/753 , C07C69/007 , C07C323/58 , C07C323/59 , C07C323/60 , C07C2603/94 , C07D207/16 , C07K5/06078 , C07K5/0812 , C07K5/1016
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R 1，R 2，R 3，R 4， R 5，R 6，R 7和R 7具有本说明书中定义的任何值及其药学上可接受的盐，如 以及包含式I或II化合物的药物组合物，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化合物抑制肿瘤生长或治疗癌症的方法。
-
公开(公告)号：US06639105B2
公开(公告)日：2003-10-28
申请号：US10134260
申请日：2002-04-29
IPC分类号： C07C22952
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; R 3为（C 1 -C 4）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）烷基; 由 - 代表的债券单独存在或不存在。 本发明还提供包含式（I）的类似物的二聚体。
-
公开(公告)号：US06380403B1
公开(公告)日：2002-04-30
申请号：US09501151
申请日：2000-02-09
IPC分类号： C07D49300
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R 1和R 2一起包含5-7元环; R 3为（C 1 -C 4）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）烷基; 由-----表示的债券单独存在或不存在。 本发明还提供包含式（I）的类似物的二聚体。
-
公开(公告)号：US6025328A
公开(公告)日：2000-02-15
申请号：US26633
申请日：1998-02-20
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 , A61K31/70 , A61K38/04 , C07C49/543 , C07K7/00
CPC分类号： C07C69/013 , C07C323/58 , C07C323/59 , C07C323/60 , C07C49/737 , C07C49/753 , C07D207/16 , C07K5/0215 , C07K5/081 , C07K5/1013 , A61K38/00
摘要： The present invention provides illudin analogs of the general formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 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：US5523490A
公开(公告)日：1996-06-04
申请号：US332940
申请日：1994-11-01
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 , C07C211/00
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 compound to inhibit tumor cell growth in a subject in need of said therapy is provided, wherein said compound has the structure: ##STR1## wherein R is selected from the group consisting of: ##STR2## Tumor cells sensitive to inhibition by said compound are 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： 提供了一种抑制需要所述治疗的受试者的肿瘤细胞生长的化合物，其中所述化合物具有以下结构：其中R选自下列组成的组：
肿瘤细胞对 所述化合物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。 -
公开(公告)号：US07713939B2
公开(公告)日：2010-05-11
申请号：US11955247
申请日：2007-12-12
IPC分类号： A61K31/10 , A61K31/215 , A61K31/7004
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。
-
公开(公告)号：US07629380B2
公开(公告)日：2009-12-08
申请号：US11600375
申请日：2006-11-16
IPC分类号： A61K31/335 , C07D317/72 , C07C49/453
CPC分类号： C07C49/737 , A61K38/063 , A61K38/08 , C07B2200/07 , C07C49/753 , C07C69/007 , C07C323/58 , C07C323/59 , C07C323/60 , C07C2603/94 , C07D207/16 , C07K5/06078 , C07K5/0812 , C07K5/1016
摘要： The present invention provides compounds 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的化合物：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化合物的药物组合物 ，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化合物抑制肿瘤生长或治疗癌症的方法。
-
公开(公告)号：US20080306013A1
公开(公告)日：2008-12-11
申请号：US11955247
申请日：2007-12-12
IPC分类号： A61K31/122 , A61K31/357 , A61K31/7028 , A61K31/4164 , A61P35/04
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---代表的债券单独存在或不存在。 本发明还提供包含式（I）的类似物的二聚体。
-
公开(公告)号：US06987193B2
公开(公告)日：2006-01-17
申请号：US10694533
申请日：2003-10-27
IPC分类号： C07D493/10 , C07C62/06 , C07C49/11
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。
-
-
-
-
-
-
-
-
-
搜索结果
28 条记录 (耗时 0.025 秒)
