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1. 发明专利

TW200730532A 作為化學輻射敏感劑之喜樹鹼衍生物 CAMPTOTHECIN DERIVATIVES AS CHEMORADIOSENSITIZING AGENTS 审中-公开
简体标题：作为化学辐射敏感剂之喜树碱衍生物 CAMPTOTHECIN DERIVATIVES AS CHEMORADIOSENSITIZING AGENTS
公开(公告)号：TW200730532A
公开(公告)日：2007-08-16
申请号：TW095138924
申请日：2006-10-20
申请人：加州太平洋醫療中心 CALIFORNIA PACIFIC MEDICAL CENTER , 西部天主教會保健團 CATHOLIC HEALTHCARE WEST, DOING BUSINESS AS ST. MARY'S MEDICAL CENTER
发明人：楊理希 YANG, LI-XI
IPC分类号： C07D , C07C , A61K
CPC分类号： C07D491/22 , A61K45/06
摘要：本發明揭示一種基於喜樹鹼之化合物,其可用於治療哺乳類個體之贅瘤(neoplasm),係藉由對該個體投與此化合物並組合輻射療法(即以輻射活性物質或自個體外來源輻射)以治療腫瘤。此基於喜樹鹼之化合物係藉由在喜樹鹼結構周圍設置至少一個親電子基而改質,以增進其與輻射療法組合之價値。本發明揭示新穎的基於喜樹鹼之化合物,其可藉由單獨投與該新穎化合物或與輻射療法組合而用於治療癌症。
095138924-p01.bmp
简体摘要：本发明揭示一种基于喜树碱之化合物,其可用于治疗哺乳类个体之赘瘤(neoplasm),系借由对该个体投与此化合物并组合辐射疗法(即以辐射活性物质或自个体外来源辐射)以治疗肿瘤。此基于喜树碱之化合物系借由在喜树碱结构周围设置至少一个亲电子基而改质,以增进其与辐射疗法组合之价値。本发明揭示新颖的基于喜树碱之化合物,其可借由单独投与该新颖化合物或与辐射疗法组合而用于治疗癌症。 095138924-p01.bmp

2. 发明专利

TWI402270B 作為化學輻射敏感劑之喜樹鹼衍生物有权
简体标题：作为化学辐射敏感剂之喜树碱衍生物
公开(公告)号：TWI402270B
公开(公告)日：2013-07-21
申请号：TW095138924
申请日：2006-10-20
申请人：莎特西灣醫院 , SUTTER WEST BAY HOSPITALS , 西部天主教會保健團(亦以聖瑪莉醫療中心之名營業) , CATHOLIC HEALTHCARE WEST, DOING BUSINESS AS ST. MARY'S MEDICAL CENTER
发明人：楊理希 , YANG, LI-XI
IPC分类号： C07D491/14 , C07C205/06 , A61K31/4745
CPC分类号： C07D491/22 , A61K45/06

3. 发明申请

WO2005014536A2 PODOPHYLLOTOXIN DERIVATIVES 审中-公开
标题翻译：四氢卟酚衍生物（PODOPHYLLOTOXIN DORIVATIVES）
公开(公告)号：WO2005014536A2
公开(公告)日：2005-02-17
申请号：PCT/US2004/021224
申请日：2004-06-30
申请人： CALIFORNIA PACIFIC MEDICAL CENTER , CATHOLIC HEALTHCARE WEST, doing business as ST. MARY'S MEDICAL CENTER , YANG, Li-Xi
发明人： YANG, Li-Xi
IPC分类号： C07D
CPC分类号： C07F9/6561 , C07D493/04
摘要： 4-0 esters of podophyllotoxin and 4’-demethylepipodophyllotoxin are provided. The compounds are 4-0 esters of an alkanoic acid or substituted alkanoic acid and podophyllotoxin and 4’-demethylepipodophyllotoxin. The compounds are useful for treating cancer.
摘要翻译：提供鬼臼毒素和4'-去甲表鬼臼毒素的4-0酯。化合物是链烷酸或取代的链烷酸和鬼臼毒素和4'-去甲表鬼臼毒素的4-0酯。该化合物可用于治疗癌症。

4. 发明申请

WO2005007076A2 COLCHICINE DERIVATIVES 审中-公开
标题翻译：醋酸衍生物
公开(公告)号：WO2005007076A2
公开(公告)日：2005-01-27
申请号：PCT/US2004/011593
申请日：2004-04-14
申请人： CALIFORNIA PACIFIC MEDICAL CENTER , CATHOLIC HEALTHCARE WEST, DOING BUSINESS AS ST. MARY'S MEDICAL CENTER , YANG, Li-Xi
发明人： YANG, Li-Xi
IPC分类号： A61K
CPC分类号： C07C323/41 , C07C323/42 , C07C323/60 , C07C2603/18 , C07C2603/24 , C07C2603/34 , C07D295/15 , C07H5/06
摘要： Certain N-deacetylcolchicine and N-deacetylthiocolchine derivatives are described wherein the 7-N position on the B ring is substituted with the group - C(O)-(CHR 4 ) m -AR, wherein m is an integer of 0-10, A is S, O, N or a covalent bond; R 1 is substituted phenyl or substituted benzoyl; optionally substituted cycloalkyl of 3-7 carbons; optionally substituted naphtyl; an optionally substituted imide ring; an optionally substituted 5 or 6 member heterocycle with at least one N, S, or O in the ring; or an optionally substituted fused heterocyclic or fused carboxyclic ring system; R 2 (at the 2-position of the A ring) is methoxy, hydroxy, or methylenedioxy when taken together with R 3 ; R 3 (at the 3-position of the A ring) is methoxy, hydroxy, a monosaccharide radical, or is methylenedioxy when taken together with R 2 ; and R 4 is H or is H or methyl when m is 1. Also dimers of such compounds are disclosed. When combined with suitable pharmaceutical excipients, these compounds are useful for treating various types of cancer.
摘要翻译：描述了某些N-去乙酰基秋水仙碱和N-脱乙酰硫代秋水仙碱衍生物，其中B环上的7-N位被基团-C（O） - （CHR 4））m -AR，其中m是0-10的整数，A是S，O，N或共价键; R 1是取代的苯基或取代的苯甲酰基; 任选取代的3-7个碳的环烷基; 任选取代的萘基; 任选取代的酰亚胺环; 在环中具有至少一个N，S或O的任选取代的5或6元杂环; 或任选取代的稠合杂环或稠合羧基环体系; R 2（在A环的2-位）是甲氧基，羟基或亚甲二氧基，当与R 3一起取代时; R 3（在A环的3-位）是甲氧基，羟基，单糖基团，或者是与亚甲基二氧基连在一起的亚甲二氧基; 并且当m为1时，R 4是H或者是H或甲基。还公开了这些化合物的二聚体。当与合适的药物赋形剂组合时，这些化合物可用于治疗各种类型的癌症。

5. 发明申请

WO2007048002A2 CAMPTOTHECIN DERIVATIVES AS CHEMORADIOSENSITIZING AGENTS 审中-公开
标题翻译：化学衍生物作为化学致敏剂
公开(公告)号：WO2007048002A2
公开(公告)日：2007-04-26
申请号：PCT/US2006/041175
申请日：2006-10-19
申请人： CALIFORNIA PACIFIC MEDICAL CENTER , CATHOLIC HEALTHCARE WEST, DOING BUSINESS AS ST. MARY'S MEDICAL CENTER , YANG, Li-Xi
发明人： YANG, Li-Xi
IPC分类号： A61K31/7052 , A61K31/4745 , C07D491/14
CPC分类号： C07D491/22 , A61K45/06
摘要： Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy.
摘要翻译：喜树碱类化合物可用于治疗哺乳动物受试者的肿瘤，其通过与受试者联合放射治疗，即用放射性物质治疗肿瘤或从受试者外部的来源辐射来治疗肿瘤。通过在喜树碱结构周围定位至少一个电子亲和基团来改进喜树碱类化合物，以增强其与放射治疗相结合的价值。公开了新的喜树碱类化合物，其可用于通过单独施用新化合物或与放射治疗组合来治疗癌症。

6. 发明申请

WO2003101406A1 HOMO-CAMPTOTHECIN DERIVATIVES 审中-公开
标题翻译： HOMO-CAMPTOTHECIN衍生物
公开(公告)号：WO2003101406A1
公开(公告)日：2003-12-11
申请号：PCT/US2003/017681
申请日：2003-06-03
申请人： CALIFORNIA PACIFIC MEDICAL CENTER , CATHOLIC HEALTHCARE WEST, DOING BUSINESS AS ST. MARY'S MEDICAL CENTER
发明人： YANG, Li-Xi
IPC分类号： A61K
CPC分类号： C07D491/22
摘要： C-20 esters of homo-camptothecin analogues are provided. The compounds are C 20 esters of an oxyalkanoic acid and homo-camptothecin, which are optionally substituted at the 7, 9, 10, 11, and 12 positions of the homo-camptothecin ring. The compounds are useful for treating cancer.
摘要翻译：提供了喜树碱类似物的C-20酯。这些化合物是在喜树碱环的7,9,10,11和12位任选被取代的氧代链烷酸和喜树碱的C 20酯。该化合物可用于治疗癌症。

7. 发明公开

EP1951231A2 CAMPTOTHECIN DERIVATIVES AS CHEMORADIOSENSITIZING AGENTS 有权
标题翻译：作为化学辐射致敏剂的吗啡啉衍生物
公开(公告)号：EP1951231A2
公开(公告)日：2008-08-06
申请号：EP06836448.8
申请日：2006-10-19
申请人： California Pacific Medical Center , Catholic Healthcare West, Doing Business as St. Mary's Medical Center
发明人： YANG, Li-Xi
IPC分类号： A61K31/44
CPC分类号： C07D491/22 , A61K45/06
摘要： Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy.
摘要翻译：通过将这种化合物与放射治疗组合给予受试者，即用放射性物质或来自受试者外部来源的放射线治疗肿瘤，基于喜树碱的化合物可用于治疗哺乳动物受试者的赘生物。基于喜树碱的化合物通过在喜树碱结构周围放置至少一个电子亲和基团来修饰，以提高其与放射疗法的组合价值。公开了新的基于喜树碱的化合物，其通过单独或与放射疗法组合施用新化合物用于治疗癌症。

8. 发明授权

EP1951231B1 CAMPTOTHECIN DERIVATIVES AS CHEMORADIOSENSITIZING AGENTS 有权
标题翻译：作为化学辐射致敏剂的吗啡啉衍生物
公开(公告)号：EP1951231B1
公开(公告)日：2013-07-31
申请号：EP06836448.8
申请日：2006-10-19
申请人： California Pacific Medical Center , Catholic Healthcare West, Doing Business as St. Mary's Medical Center
发明人： YANG, Li-Xi
IPC分类号： A61K31/44 , C07D491/22 , A61K45/06
CPC分类号： C07D491/22 , A61K45/06

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