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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:US07816352B2
公开(公告)日:2010-10-19
申请号:US11885463
申请日:2006-03-10
IPC分类号: A61K31/535 , A61K31/47 , A61K31/497 , C07D213/56 , C07D217/00 , C07D215/38
CPC分类号: C07D513/04 , C07D213/20 , C07D215/227
摘要: The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.
摘要翻译: 本发明提供了用作选择剂以防止无意的细胞死亡或组织损伤并可以减轻癌症治疗的副作用的化合物,例如口腔粘膜炎,脱发,胃肠上皮损伤引起的腹泻和骨髓抑制 。 此外,当细胞死亡是由受损细胞的信号引起的,例如作为创伤事件或缺血发作的结果产生的信号,这些化合物可用于防止过早的细胞死亡。
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公开(公告)号:US20080280903A1
公开(公告)日:2008-11-13
申请号:US11885463
申请日:2006-03-10
IPC分类号: A61K31/5377 , C07D213/02 , A61K31/4439 , A61K31/44 , C07D401/02 , C07D403/02 , A61K31/497 , A61K31/4545 , A61P43/00 , C07D413/02
CPC分类号: C07D513/04 , C07D213/20 , C07D215/227
摘要: The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.
摘要翻译: 本发明提供了用作选择剂以防止无意的细胞死亡或组织损伤并可以减轻癌症治疗的副作用的化合物,例如口腔粘膜炎,脱发,胃肠上皮损伤引起的腹泻和骨髓抑制 。 此外,当细胞死亡是由受损细胞的信号引起的,例如作为创伤事件或缺血发作的结果产生的信号,这些化合物可用于防止过早的细胞死亡。
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