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1. 发明申请

US20060111389A1 Therapeutic acridone and acridine compounds 失效
标题翻译：治疗吖啶酮和吖啶化合物
公开(公告)号：US20060111389A1
公开(公告)日：2006-05-25
申请号：US11157977
申请日：2005-06-22
申请人： Stephen Neidle , Richard Harrison , Lloyd Kelland , Sharon Gowan , Martin Read , Anthony Reszka
发明人： Stephen Neidle , Richard Harrison , Lloyd Kelland , Sharon Gowan , Martin Read , Anthony Reszka
IPC分类号： C07D219/04 , A61K31/473
CPC分类号： C07D219/08 , C07D219/06 , C07D219/10
摘要： The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ═O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones): or, (b) K is a 9-substituent. L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula —N(RN)Q, wherein: RN is an amino substituent and is hydrogen. C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.
摘要翻译：本发明涉及式（I）的吖啶酮和吖啶化合物，其中：（a）K是-O，L是-H，α是单键，β是双键，γ是单键（吖啶酮）：或（b）K为9-取代基。 L不存在，α是双键，β是单键，γ是双键，并且其中：J 1是2-或3-取代基; J 2是6-或7-取代基; J 1和J 2各自各自独立地是式-NHCO（CH 2 CH 2）n NR n的基团，其中：n为1至5的整数;其中n为1至5的整数; 且R 1和R 2独立地为氢，C 1-7烷基，C 3-20杂环基或C 5-20-20芳基或R 1和R 2与它们所连接的氮原子一起形成一个具有3至8个环原子的杂环; 并且其中当K是9-取代基时，K是式-N（R“N”）Q的基团，其中：R N是氨基取代基，并且是氢。 C 1-7烷基，C 3-20杂环基或C 5-20-20芳基; 且Q为C 1-7烷基，C 3-20杂环基或C 5-20芳基，且为任选取代的; 和其药学上可接受的盐，酯，酰胺，溶剂合物，水合物及其保护形式。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制端粒酶调节细胞增殖以及治疗增殖性疾病如癌症的用途。

2. 发明申请

US20050070568A1 Therapeutic acridone and acridine compounds 失效
标题翻译：治疗吖啶酮和吖啶化合物
公开(公告)号：US20050070568A1
公开(公告)日：2005-03-31
申请号：US10501474
申请日：2003-01-14
申请人： Stephen Neidle , Richard Harrison , Lloyd Kelland , Sharon Gowan , Martin Read , Anthony Reszka
发明人： Stephen Neidle , Richard Harrison , Lloyd Kelland , Sharon Gowan , Martin Read , Anthony Reszka
IPC分类号： A61K31/473 , A61P35/00 , A61P43/00 , C07D219/04 , C07D219/08 , C07D219/10 , C07D219/12
CPC分类号： C07D219/08 , C07D219/10
摘要： This invention pertains to certain acridine and acridine compounds of the formula (1) which inhibit telomerase, regulate cell proliteration, etc., and/or treat cancer proliferative conditions, etc.: wherein either: (a) K is ═O, L is —H, alpha single bond beta is a double bond, gamma is a single bond (acridines); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each a group of the formula —N(RN)—W, wherein: RN is a nitrogen substituent and is hydrogen, C1-7alkyl, C3-20 heterocyclyl, or C5-20aryl, and is optionally substituted; and, W is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substitute; and wherein when K is a 9-substituent, K is a group of the formula —N(RN)-Q, wherein: RN is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, etc., and/or in the treatment of cancer, proliferative conditions, etc.
摘要翻译：本发明涉及抑制端粒酶，调节细胞增殖等的某些式（1）的吖啶和吖啶化合物，和/或治疗癌症增殖病症等。其中：（a）K为= O，L为 -H，α单键β是双键，γ是单键（吖啶）; 或（b）K是9取代基，L不存在，α是双键，β是单键，γ是双键（吖啶）; 并且其中：J 1是2-或3-取代基; J 2是6-或7-取代基; J 1和J 2各自为式-N（R N）-W的基团，其中：R N为氮取代基且为氢，C 1-7烷基，C 3-20杂环基，或C 5-20芳基，并且任选被取代; 并且W是C 1-7烷基，C 3-20杂环基或C 5-20芳基，并且任选被取代; 并且其中当K是9-取代基时，K是式-N（R N）-Q的基团，其中：R N是氨基取代基并且是氢，C 1-7烷基，C 3-20杂环基，或C5-20芳基; 且Q为C 1-7烷基，C 3-20杂环基或C 5-20芳基，并且任选被取代; 和其药学上可接受的盐，酯，酰胺，溶剂合物，水合物及其保护形式。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制端粒酶，调节细胞增殖等，和/或治疗癌症，增殖性条件等

3. 发明申请

US20080319001A1 Cancer Treatment Using Specific 3,6,9-Substituted Acridines 审中-公开
标题翻译：使用特定3,6,9取代的吖啶的癌症治疗
公开(公告)号：US20080319001A1
公开(公告)日：2008-12-25
申请号：US11886128
申请日：2006-03-02
申请人： Christina Martins , Stephen Neidle , Mekala Gunaratnam , John Stuart , Lloyd Kelland
发明人： Christina Martins , Stephen Neidle , Mekala Gunaratnam , John Stuart , Lloyd Kelland
IPC分类号： A61K31/438 , C07D401/14 , A61P35/00
CPC分类号： C07D219/10
摘要： The present invention relates to a 3,6,9 acridine compound and optionally substituted derivatives thereof that may be useful in the treatment of cancer. The invention also provides compositions comprising the compounds and uses thereof. Formula (I) wherein each of R1, R2, R3, R4 and R5 is either fluorine or is not present (i.e. represents a hydrogen atom); n represents 1 or 2.
摘要翻译：本发明涉及可用于治疗癌症的3,6,9吖啶化合物及其任选取代的衍生物。本发明还提供包含该化合物及其用途的组合物。式（I）其中R 1，R 2，R 3，R 4和R 5各自为氟或不存在（即表示氢原子）; n表示1或2。

4. 发明申请

US20100104565A1 COMBINATIONS COMPRISING DMXAA FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：包含DMXAA治疗癌症的组合
公开(公告)号：US20100104565A1
公开(公告)日：2010-04-29
申请号：US12064632
申请日：2006-08-25
申请人： Colin Green , Lloyd Kelland , Sally Kelland , Gail Rowlinson-Brusza
发明人： Colin Green , Lloyd Kelland , Sally Kelland , Gail Rowlinson-Brusza
IPC分类号： A61K39/395 , A61K31/352 , A61P35/00 , A61K31/517 , A61K31/5377
CPC分类号： A61K31/5377 , A61K31/352 , A61K31/517 , A61K39/395 , A61K39/39541 , A61K2300/00
摘要： The present invention relates to combinations of the xanthenone acetic acids class such as 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and EGFR signalling pathway inhibitors. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations.
摘要翻译：本发明涉及呫吨酮类乙酸类，例如5,6-二甲基呫吨酮-4-乙酸（DMXAA）和EGFR信号通路抑制剂的组合。更具体地，本发明涉及这样的组合在治疗癌症中的用途以及含有这些组合的药物组合物。

5. 发明申请

US20100297112A1 COMBINATIONS COMPRISING DMXAA FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：包含DMXAA治疗癌症的组合
公开(公告)号：US20100297112A1
公开(公告)日：2010-11-25
申请号：US12064633
申请日：2006-08-25
申请人： Colin Green , Lloyd Kelland , Gail Rowlinson-Bruza
发明人： Colin Green , Lloyd Kelland , Gail Rowlinson-Bruza
IPC分类号： A61K39/395 , A61P35/00 , A61K31/352
CPC分类号： A61K31/337 , A61K31/352 , A61K39/395 , A61K2300/00
摘要： The present invention relates to combinations of compounds such as compounds of the xanthenone acetic acid class such as 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and vascular endothelial growth factor binders, in particular the monoclonal antibody Avastin™ (bevacizumab). More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical formulations containing such combinations.
摘要翻译：本发明涉及化合物如呫吨酮乙酸类化合物如5,6-二甲基呫吨酮-4-乙酸（DMXAA）和血管内皮生长因子结合剂，特别是单克隆抗体Avastin TM（贝伐珠单抗））的组合。更具体地说，本发明涉及这样的组合在治疗癌症中的用途以及含有这种组合的药物制剂。

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