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公开(公告)号：US20050245508A1
公开(公告)日：2005-11-03
申请号：US11021640
申请日：2004-12-22
申请人： Michael Weller , Sundeep Dugar , Linda Higgins , David Liu , George Schreiner , Sarvaji Chakravarty
发明人： Michael Weller , Sundeep Dugar , Linda Higgins , David Liu , George Schreiner , Sarvaji Chakravarty
IPC分类号： A61K31/505 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/55
CPC分类号： A61K31/519 , A61K31/505 , A61K31/517 , A61K31/53 , A61K31/55
摘要： The invention concerns methods of treating malignant gliomas, by administering inhibitors of TGF-β the TGF-β signaling pathway, including molecules preferably binding to the type I TGF-β receptor (TGFβ-R1). Preferably, the inhibitors are non-peptide small molecules, including quinazoline derivatives. The invention also concerns methods for reversing the TGF-β-mediated effect on glioma cells to make them less refractile to signaling and other immune cells, comprising contacting a glioma cell or tissue in vivo or in vitro, with an inhibitor of TGF-β.
摘要翻译： 本发明涉及通过施用TGF-β的TGF-β信号转导途径的抑制剂，包括优选结合I型TGF-β受体（TGFβ-R1）的分子来治疗恶性胶质瘤的方法。 优选地，抑制剂是非肽小分子，包括喹唑啉衍生物。 本发明还涉及用于逆转TGF-β介导的对胶质瘤细胞的作用以使其对信号传导和其他免疫细胞的折射较少的方法，包括使体内或体外的胶质瘤细胞或组织与TGF-β的抑制剂接触。
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公开(公告)号：US20050171123A1
公开(公告)日：2005-08-04
申请号：US11053121
申请日：2005-02-07
申请人： Sarvajit Chakravarty , Sundeep Dugar , John Perumattam , George Schreiner , David Liu , John Lewicki
发明人： Sarvajit Chakravarty , Sundeep Dugar , John Perumattam , George Schreiner , David Liu , John Lewicki
IPC分类号： A61K31/517 , A61K31/519 , A61K31/5355 , A61K39/395 , A61P1/16 , A61P1/18 , A61P7/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/02 , A61P19/02 , A61P29/00 , A61P43/00 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/02 , A61K31/535 , A61K31/525
CPC分类号： C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要： The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.
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公开(公告)号：US20050220784A1
公开(公告)日：2005-10-06
申请号：US11136242
申请日：2005-05-23
申请人： Sarvajit Chakravarty , Sundeep Dugar , John Perumattam , George Schreiner , David Liu , John Lewicki
发明人： Sarvajit Chakravarty , Sundeep Dugar , John Perumattam , George Schreiner , David Liu , John Lewicki
IPC分类号： A61K31/517 , A61K31/519 , A61K31/5355 , A61K39/395 , A61P1/16 , A61P1/18 , A61P7/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/02 , A61P19/02 , A61P29/00 , A61P43/00 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/02
CPC分类号： C07D401/12 , A61K31/519 , C07D239/94 , C07D471/04
摘要： The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.
摘要翻译： 本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法，其中R 3是非干扰性取代基; 每个Z是CR 2或N，其中环A中不超过两个Z位是N，并且其中环A中的两个相邻Z位不能是N; 每个R 2独立地是非干扰取代基; L是连接体; n为0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环脂族，环状杂脂族，芳族或杂芳族部分的残基。
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4.发明申请Treatment of multiple myeloma by p38 MAP kinase and proteasome inhibition 审中-公开通过p38 MAP激酶和蛋白酶体抑制治疗多发性骨髓瘤公开(公告)号：US20060052390A1
公开(公告)日：2006-03-09
申请号：US11208055
申请日：2005-08-19
申请人： George Schreiner , Andrew Protter , Linda Higgins
发明人： George Schreiner , Andrew Protter , Linda Higgins
IPC分类号： A61K31/496 , A61K31/454
CPC分类号： A61K45/06 , A61K31/454 , A61K31/496 , A61K2300/00
摘要： The present invention provides a method to treat multiple myeloma by the co-administration of one or more p38 MAP kinase inhibitors with one or more proteosome inhibitors.
摘要翻译： 本发明提供了通过一种或多种p38 MAP激酶抑制剂与一种或多种蛋白酶体抑制剂共同给药来治疗多发性骨髓瘤的方法。
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公开(公告)号：US20050043212A1
公开(公告)日：2005-02-24
申请号：US10830834
申请日：2004-04-22
IPC分类号： A61K31/496 , A61K31/56 , A61K39/395 , A61K45/06 , C07D471/04 , A61K31/00 , G06F19/00 , G01N33/48 , G01N33/50
CPC分类号： A61K31/496 , A61K31/56 , A61K39/395 , A61K45/06 , C07D471/04 , Y02A50/412 , A61K2300/00
摘要： The invention is directed to methods and compositions that differentially inhibit the α-isoform of p38 MAP kinase.
摘要翻译： 本发明涉及差异抑制p38MAP激酶的α-同种型的方法和组合物。
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公开(公告)号：US20130171268A1
公开(公告)日：2013-07-04
申请号：US13489317
申请日：2012-06-05
IPC分类号： A61K31/455 , A61K31/573 , A61K45/06 , A61K31/353
CPC分类号： A61K31/455 , A61K31/353 , A61K31/573 , A61K36/185 , A61K36/82 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.
摘要翻译： 本发明涉及用于预防和/或治疗与线粒体功能相关的病症的组合物和方法。 在各个方面，本发明包括施用一种或多种选自以下的化合物：表儿茶素，表儿茶素衍生物，儿茶素，儿茶素衍生物，尼可地尔和尼可地尔衍生物，其量可以有效地改善由给药引起的线粒体毒性 化学，食品或药物。
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公开(公告)号：US20050129729A1
公开(公告)日：2005-06-16
申请号：US10951754
申请日：2004-09-27
申请人： George Schreiner
发明人： George Schreiner
IPC分类号： A61F20060101 , A61F2/00 , A61F2/02 , A61F2/06 , A61L31/16
CPC分类号： A61L31/16 , A61L2300/434
摘要： A coated stent or intra-luminal prosthesis containing a MAP kinase inhibitor controls, reduces, or prevents restenosis, inflammation, and complications associated with stent or intra-luminal prosthesis implantation and/or cardiovascular disease.
摘要翻译： 含有MAP激酶抑制剂的涂层支架或腔内假体控制，减少或预防与支架或腔内假体植入和/或心血管疾病相关的再狭窄，炎症和并发症。
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公开(公告)号：US20050113286A1
公开(公告)日：2005-05-26
申请号：US10931498
申请日：2004-08-31
IPC分类号： A61K31/381 , A61K31/4164 , A61K31/44 , A61K31/496 , A61K38/22 , A61K38/17
CPC分类号： A61K31/381 , A61K31/4164 , A61K31/44 , A61K31/496 , A61K38/2242
摘要： The present invention relates to methods for administration of natriuretic peptide that are especially useful for treatment of a CHF patient. The methods are characterized by the serial and intermittent administration of a composition that provides a dose of natriuretic peptide. The methods of the invention are also useful for the treatment of chronic CHF patients, especially chronically decompensated CHF patients.
摘要翻译： 本发明涉及用于治疗CHF患者特别有用的利尿钠肽的方法。 该方法的特征在于连续和间歇地施用提供剂量的利尿钠肽的组合物。 本发明的方法也可用于治疗慢性CHF患者，特别是慢性失代偿性CHF患者。
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公开(公告)号：US20050038017A1
公开(公告)日：2005-02-17
申请号：US10953981
申请日：2004-09-29
申请人： Andrew Wolff , George Schreiner , Evan Beckman , Glenn Smits
发明人： Andrew Wolff , George Schreiner , Evan Beckman , Glenn Smits
IPC分类号： A61K31/522 , A61K31/549 , A61K31/56
CPC分类号： A61K31/522 , A61K31/549 , A61K31/56 , A61K2300/00
摘要： Methods and compositions for restoring diuretic and renal function
摘要翻译： 恢复利尿和肾功能的方法和组合物
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公开(公告)号：US10052316B2
公开(公告)日：2018-08-21
申请号：US13489317
申请日：2012-06-05
IPC分类号： A61K31/455 , A61K36/82 , A61K45/06 , A61K31/353 , A61K31/573 , A61K36/185
CPC分类号： A61K31/455 , A61K31/353 , A61K31/573 , A61K36/185 , A61K36/82 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.
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