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公开(公告)号:US06696441B1
公开(公告)日:2004-02-24
申请号:US09637531
申请日:2000-08-11
IPC分类号: A61K31425
CPC分类号: C07D513/04 , A61K31/519 , C07D487/04
摘要: The present invention provides compounds that act to suppress p53 activity in mammalian cells, and a method to effectively suppress p53 activity in the cells of a mammal subject to a stress or pathology that is ameliorated by such suppression.
摘要翻译: 本发明提供了用于抑制哺乳动物细胞中p53活性的化合物,以及有效抑制经受这种抑制而改善的应激或病理学的哺乳动物细胞中p53活性的方法。
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公开(公告)号:US07361680B2
公开(公告)日:2008-04-22
申请号:US11467472
申请日:2006-08-25
IPC分类号: A61K31/407 , C07D471/04
CPC分类号: A61K31/407 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/675 , A61K31/7056 , G01N33/57434 , G01N2800/52
摘要: The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.
摘要翻译: 本发明提供了可用于抑制癌症或使癌细胞对化学治疗剂,辐射或其它抗癌治疗敏感的新型吲哚衍生物。
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公开(公告)号:US07151100B1
公开(公告)日:2006-12-19
申请号:US09634207
申请日:2000-08-09
IPC分类号: A61K31/535 , A61P35/02 , C07D413/00 , C07D491/052 , C01B25/16
CPC分类号: A61K31/535 , A61K45/06 , A61K2300/00
摘要: The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.
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公开(公告)号:US07129262B2
公开(公告)日:2006-10-31
申请号:US11013955
申请日:2004-12-16
IPC分类号: A61K31/407 , C07D471/14
CPC分类号: C07D491/04
摘要: The present invention provides novel indole derivatives useful to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other anti-cancer treatments.
摘要翻译: 本发明提供了可用于抑制癌症或使癌细胞对化学治疗剂,辐射或其它抗癌治疗敏感的新型吲哚衍生物。
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5.
公开(公告)号:US07189752B2
公开(公告)日:2007-03-13
申请号:US10753665
申请日:2004-01-08
IPC分类号: A61K31/40
CPC分类号: G01N33/5011 , A61K31/198 , A61K31/407 , A61K45/06 , Y10S514/908 , Y10S514/922 , A61K2300/00
摘要: A method of treating cancer is provided comprising administering an amount of etodolac or analog theteof to a subject afflicted with leukemia that is effective to reduce the viability and/or to sensitize leukemia cells to an anti-cancer agent.
摘要翻译: 提供了一种治疗癌症的方法,包括将一定量的依托度酸或类似物施用于有效降低生存力和/或使白血病细胞对抗癌剂敏感的白血病患者。
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公开(公告)号:US07105560B1
公开(公告)日:2006-09-12
申请号:US09589476
申请日:2000-06-07
IPC分类号: A61K31/40
CPC分类号: G01N33/5011 , A61K31/198 , A61K31/407 , A61K45/06 , Y10S514/908 , A61K2300/00
摘要: A method of treating multiple myeloma (MM) is provided comprising administering an amount of etodolac to a subject afflicted with MM that is effective to selectively reduce the viability of and/or to sensitize the cancer cells to an anti-cancer agent.
摘要翻译: 提供一种治疗多发性骨髓瘤(MM)的方法,包括向患有MM的受试者施用一定量的有效选择性降低癌细胞对抗癌剂的活力和/或使癌细胞敏感的一定量的依托度酸。
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公开(公告)号:US07105561B2
公开(公告)日:2006-09-12
申请号:US10236221
申请日:2002-09-05
IPC分类号: A61K31/40
CPC分类号: G01N33/5011 , A61K31/198 , A61K31/407 , A61K45/06 , Y10S514/908 , Y10S514/922 , A61K2300/00
摘要: A method of treating cancer is provided comprising administering an amount of etodolac to a subject afflicted with cancer that is effective to reduce the viability and/or to sensitize the cancer to an anti-cancer agent.
摘要翻译: 提供了一种治疗癌症的方法,包括向有效降低活力的癌症患者施用一定量的依托止酸,和/或使癌症对抗癌剂敏感。
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8.
公开(公告)号:US06545034B1
公开(公告)日:2003-04-08
申请号:US09360020
申请日:1999-07-23
IPC分类号: A61K3140
CPC分类号: G01N33/5011 , A61K31/198 , A61K31/407 , A61K45/06 , Y10S514/908 , Y10S514/922 , A61K2300/00
摘要: A method of treating cancer is provided comprising administering an amount of etodolac to a subject afflicted with cancer that is effective to reduce the viability and/or to sensitize the cancer to an anti-cancer agent.
摘要翻译: 提供了一种治疗癌症的方法,包括向有效降低活力的癌症患者施用一定量的依托止酸,和/或使癌症对抗癌剂敏感。
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公开(公告)号:US07211599B2
公开(公告)日:2007-05-01
申请号:US10667208
申请日:2003-09-19
CPC分类号: A61K31/12 , A61K31/18 , A61K31/40 , A61K31/407 , A61K31/4745 , A61K31/496 , A61K31/50 , A61K31/56 , A61K31/675 , A61K31/7052
摘要: The present invention provides a therapeutic method to treat non-malignant diseases characterized by the excessive tissue growth, e.g., hyperplastic diseases, comprising administering to a mammal (e.g., human) afflicted with excessive tissue growth, an effective amount of a derivative of an indole compound of formula (I):formula (I): wherein R1 is lower alkyl, (hydroxy)lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, phenyl, benzyl or 2-thienyl; R2, R3, R4 and R5 are the same or different and are each hydrogen or lower alkyl; each R6 is individually hydrogen, lower alkyl, hydroxy, (hydroxy)lower alkyl, lower alkoxy, benzyloxy, lower alkanoyloxy, nitro or halo, R7 is hydrogen, lower alkyl or lower alkenyl, X is oxy and thio, Y is carbonyl, —(CH2)1-3—, —(C1-C3)alkyl(CO)—, or —(CH2)1-3SO2—; Z is hydroxy, lower alkoxy, (C2-C4)acyloxy, —N(R8)(R9), phenylamino, (ω-(4-pyridyl)(C2-C4 alkoxy), (ω-((R8)(R9)amino)(C2-C4 alkoxy), an amino acid ester of (ω-(HO)(C2-C4))alkoxy, —N(R8)CH(R8)CO2H, 1′-D-glucuronyloxy, —SO3H, —PO4H2, —N(NO)(OH), —SO2NH2, —PO(OH)(NH2), —OCH2CH2N(CH3)3+, or tetrazolyl; wherein R8 and R9 are each H, (C1-C3)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R8), S or nonperoxide O; n is 0, 1, 2, or 3; wherein R8 and R9 are each H, (C1-C3)alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R8), S or nonperoxide O; each alkyl or phenyl group of R1, R2, R3, R4, R5, R6, R7 and Z is optionally substituted with 1, 2, or 3 (C1-C4)alkyl groups; or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US20090324551A1
公开(公告)日:2009-12-31
申请号:US12064529
申请日:2006-08-21
申请人: Dennis A. Carson , Kenji Takabayshi , Suzanne Grimshaw , Howard B. Cottam , Michael Chan , Christina C.N. Wu
发明人: Dennis A. Carson , Kenji Takabayshi , Suzanne Grimshaw , Howard B. Cottam , Michael Chan , Christina C.N. Wu
IPC分类号: A61K45/00 , C07D473/00 , A61K31/522 , C12N1/20 , C12N7/00 , A61P35/00
CPC分类号: C07D473/16 , C07D473/18 , C07D473/24 , C07D473/34
摘要: The present invention provides for TLR agonist conjugates (compounds) and compositions, as well as methods of using them. The compounds of the invention are broad-spectrum, long-lasting, and non-toxic combination of synthetic immunostimulatory agents, which are useful for activating the immune system of a mammal, preferably a human and can help direct the pharmacophore to the receptor within the endosomes of target cells and enhance the signal transduction induced by the pharmacophore.
摘要翻译: 本发明提供了TLR激动剂缀合物(化合物)和组合物,以及使用它们的方法。 本发明的化合物是合成免疫刺激剂的广谱,持久和无毒组合,其可用于激活哺乳动物,优选人的免疫系统,并且可以帮助将药效团引导至受体内的受体 靶细胞的内体,并增强由药效团诱导的信号转导。
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