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31. 发明申请

WO2003072794A1 PROCESS TO PREPARE AND ISOLATE GELDANAMYCIN 审中-公开
标题翻译：制备和分离GELDANAMYCIN的方法
公开(公告)号：WO2003072794A1
公开(公告)日：2003-09-04
申请号：PCT/US2003/002686
申请日：2003-02-14
申请人： PHARMACIA & UPJOHN COMPANY , SHORT, Kevin, A. , CEGLAREK, John, A. , RYSENGA, Christopher, W. , SALMAN, Omar, A. , MANNES, Gregory, L. , GILLESPIE, Donald, L.
发明人： SHORT, Kevin, A. , CEGLAREK, John, A. , RYSENGA, Christopher, W. , SALMAN, Omar, A. , MANNES, Gregory, L. , GILLESPIE, Donald, L.
IPC分类号： C12P17/10
CPC分类号： C07D225/06 , C12P17/10
摘要： The present invention relates to a process of preparing geldanamycin by culturing Streptomyces hygroscopicus in an aqueous nutrient medium. The aqueous nutrient medium can comprise starch, a starch conversion enzyme, an assimilable source of protein and optionally a further assimilable source of carbon or can comprise an assimilable source of carbon and an assimilable source of protein. The present invention also relates to a process for the isolation and purification of geldanamycin.
摘要翻译：本发明涉及通过在含水营养培养基中培养吸水链霉菌来制备格尔德霉素的方法。含水营养培养基可以包括淀粉，淀粉转化酶，可同化的蛋白质来源和任选的可进一步同化的碳源，或者可以包含可同化的碳源和可同化的蛋白质来源。本发明还涉及分离和纯化格尔德霉素的方法。

32. 发明申请

WO2003066005A2 ANSAMYCINS HAVING IMPROVED PHARMACOLOGICAL AND BIOLOGICAL PROPERTIES 审中-公开
标题翻译：具有改善的药理和生物学特性的安息香
公开(公告)号：WO2003066005A2
公开(公告)日：2003-08-14
申请号：PCT/US2003/004283
申请日：2003-02-10
申请人： CONFORMA THERAPEUTICS CORPORATION , ZHANG, Lin , LE BRAZIDEC, Jean-Yves , BOEHM, Marcus, F. , MCHUGH, Sean, Konrad , FAN, Junhua , FRITZ, Lawrence, C. , BURROWS, Francis, J.
发明人： ZHANG, Lin , LE BRAZIDEC, Jean-Yves , BOEHM, Marcus, F. , MCHUGH, Sean, Konrad , FAN, Junhua , FRITZ, Lawrence, C. , BURROWS, Francis, J.
IPC分类号： A61K
CPC分类号： C07D225/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07F9/5535
摘要： Ansamycins and methods of preparing and using the same are described. At least some of these ansamycins exhibit one or more of improved aqueous formulation ability, chemical stability, and bioavailability. Some of the derivatives described are dimers. These and others described can include one or more solubilizing groups that have expected merit in rendering the overall compounds useful as drugs and prodrugs.
摘要翻译：描述了Ansamycins及其制备和使用方法。至少一些这些安莎霉素表现出一种或多种改进的水性制剂能力，化学稳定性和生物利用度。描述的一些衍生物是二聚体。这些和其他描述的可以包括一个或多个增溶基团，其具有预期的优点，使整个化合物可用作药物和前药。

33. 发明申请

WO02036574A1 GELDANAMYCIN DERIVATIVES USEFUL FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的GELDAAMYCIN衍生物
公开(公告)号：WO02036574A1
公开(公告)日：2002-05-10
申请号：PCT/US2001/044172
申请日：2001-11-06
IPC分类号： A61P35/00 , C07D225/06 , A61K31/395
CPC分类号： C07D225/06
摘要： A geldanamycin derivative of general formula (I) and in vitro and in vivo methods of selectively inhibiting Hsp90 in a cell without substantially inhibiting Grp94 comprising administering to a cell comprising Hsp90 and Grp94, or to a host including cells comprising Hsp90 and Grp94, respectively, the geldanamycin derivative in an amount sufficient to inhibit Hsp90 without substantially inhibiting Grp94, as well as in vitro and in vivo methods of inhibiting HIF-1 alpha in a cell comprising administering to a cell comprising HIF-1 alpha the geldanamycin derivative in an amount sufficient to inhibit HIF-1 alpha , and a method of treating or preventing cancer in a host comprising administering a geldanamycin derivative to a host in an amount sufficient to treat or prevent cancer.
摘要翻译：通常式（I）的格尔德霉素衍生物和在细胞中选择性抑制Hsp90的体外和/或体外方法，基本上不抑制Grp94，其包括向包含Hsp90和Grp94的细胞施用，或分别包含含有Hsp90和Grp94的细胞的宿主，其量足以抑制Hsp90而基本上不抑制Grp94，以及体内和体内抑制HIF-1α在细胞中的方法，包括以足以抑制HIF-1α的量施用包含HIF-1α的格尔德霉素衍生物的细胞，以及治疗或预防宿主中的癌症的方法，包括施用格尔德霉素衍生物到足以治疗或预防癌症的量的宿主。

34. 发明申请

WO02016369A2 NOVEL MACROCYCLES AND USES THEREOF 审中-公开
标题翻译：新的MACROCYCLES及其用途
公开(公告)号：WO02016369A2
公开(公告)日：2002-02-28
申请号：PCT/US2001/026577
申请日：2001-08-24
IPC分类号： A61P43/00 , C07D225/06 , C07D313/00 , C07D491/04 , C07D493/04 , A61K31/395
CPC分类号： C07D491/04 , C07D225/06 , C07D313/00 , C07D493/04
摘要： The present invention relates to compounds having the structure (1) (and pharmaceutically acceptable derivatives thereof), wherein R1-R4, Z, X, A-B, D-E, G-J, and K-L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.
摘要翻译：本发明涉及具有结构（1）的化合物及其药学上可接受的衍生物，其中R1-R4，Z，X，AB，DE，GJ和KL如本文所定义，其合成及其用途化合物作为治疗剂。

35. 发明申请

WO1996009299A1 DRUGS TO IMPROVED SYNAPTIC TRANSMISSION 审中-公开
标题翻译：药物改进的快速传输
公开(公告)号：WO1996009299A1
公开(公告)日：1996-03-28
申请号：PCT/US1995010454
申请日：1995-08-16
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , SUMIKAWA, Katumi , ITO, Ken-Ichi , McGAUGH, James, L.
IPC分类号： C07D313/00
CPC分类号： C07D225/06 , C07C69/732 , C07D225/04 , C07D313/00
摘要： Peripherally administered Brefeldin A and its analogs and derivatives are used to enhance learning and reverse memory dysfunction through induced long term potentiation in hippocampal tissues.
摘要翻译： Brefeldin A及其类似物和衍生物用于通过在海马组织中诱导的长期增强来增强学习和逆转记忆功能障碍。

36. 发明申请

WO2014107655A1 USE OF SMALL MOLECULE UNFOLDER PROTEIN RESPONSE MODULATORS TO TREAT TUMORS WITH ACTIVE SONIC HEDGEHOG (SSH) SIGNALING DUE TO SMOOTHENED (SMO) MUTATION 审中-公开
标题翻译：使用小分子单克隆蛋白质反应调节剂来处理带有主动SONIC HEDGEHOG（SSH）信号的肿瘤由于SMOOTHENED（SMO）突变
公开(公告)号：WO2014107655A1
公开(公告)日：2014-07-10
申请号：PCT/US2014/010321
申请日：2014-01-06
申请人： ST. JUDE CHILDREN'S RESEARCH HOSPITAL
发明人： OGDEN, Stacey , MARADA, Suresh
IPC分类号： C07D293/00 , A61K31/33
CPC分类号： A61K31/4166 , A61K31/365 , A61K31/395 , A61K31/416 , A61K38/1808 , C07D213/81 , C07D225/06 , C07D231/56 , C07D241/24 , C07D307/93 , C07D311/62 , C07D311/80 , C07D405/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D473/24 , C07D491/04
摘要： The present invention relates to methods for treating tumors having SMO mutations as well as diagnosing tumors with SMO mutations. The invention relates to methods for the treatment of cancer with ER stress-inducing compounds or UPR inducing compounds. The ER stress-inducing compounds or UPR inducing compounds might fill a clinical need for additional methods of targeting the Hh pathway, either in frontline combination therapy or in salvage therapy for relapsed patients who develop resistance to the available SMO inhibitor and offer a significant advantage over SMO-specific small molecules. Because ER stress modulators and UPR inducing compounds exploit a cellular process that is distinct from the Hh signaling pathway, their efficacy should be unaltered by acquired SMO mutation.
摘要翻译：本发明涉及用于治疗具有SMO突变的肿瘤以及用SMO突变诊断肿瘤的方法。本发明涉及用ER应激诱导化合物或UPR诱导化合物治疗癌症的方法。 ER应激诱导化合物或UPR诱导化合物可能填补了靶向Hh通路的其他方法的临床需求，无论是在前线联合治疗或针对发展对可用SMO抑制剂的抗性的复发患者的补救治疗中，并提供了超过 SMO特异性小分子。因为ER应激调节剂和UPR诱导化合物利用与Hh信号通路不同的细胞过程，因此获得性SMO突变的功效应不变。

37. 发明申请

WO2011150030A2 METHOD TO ALLEVIATE DIABETIC END STAGE RENAL DISEASE 审中-公开
标题翻译：解决糖尿病性末期肾病的方法
公开(公告)号：WO2011150030A2
公开(公告)日：2011-12-01
申请号：PCT/US2011/037866
申请日：2011-05-25
申请人： BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM , ZHANG, Bin-Xian
发明人： ZHANG, Bin-Xian
IPC分类号： A61K31/395 , C07D487/04 , A61P3/10 , A61P13/12
CPC分类号： A61K31/395 , C07D225/06
摘要： A method of alleviating end-stage renal disease (ESRD), comprising administering an effective amount of a geldanamycin derivative.
摘要翻译：一种缓解终末期肾病（ESRD）的方法，包括施用有效量的格尔德霉素衍生物。

38. 发明申请

WO2009091921A1 SYNTHESIS OF RESORCYLIC ACID LACTONES USEFUL AS THERAPEUTIC AGENTS 审中-公开
标题翻译：作为治疗剂有效的合成酸性乳酸
公开(公告)号：WO2009091921A1
公开(公告)日：2009-07-23
申请号：PCT/US2009/031149
申请日：2009-01-15
申请人： UNIVERSITE DE STRASBOURG , WINSSINGER, Nicolas , BARLUENGA, Sofia , KARPLUS, Martin
发明人： WINSSINGER, Nicolas , BARLUENGA, Sofia , KARPLUS, Martin
IPC分类号： A01N31/14 , A61K31/02
CPC分类号： C07D313/00 , A61K31/335 , A61K31/365 , A61K31/4025 , A61K31/435 , A61K31/4453 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D211/14 , C07D225/06 , C07D405/12 , C07D405/14 , Y02P20/55
摘要： Disclosed are macrocyclic compounds of formulae I, I', II, II', III, III', IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
摘要翻译：公开了式I，I'，II，II'，III，III'，IV和V的大环化合物，它们是昆金宁间苯二甲酸内酯的类似物，包含该化合物的药物组合物，以及包含该化合物的方法和用途治疗由激酶和热休克蛋白90 HSP90介导的疾病。

39. 发明申请

WO2008104812A3 C21-DE0XY ANSAMYCIN DERIVATIVES AS ANTITUMOR AGENTS 审中-公开
标题翻译： C21-DE0XY ANSAMYCIN衍生物作为抗菌剂
公开(公告)号：WO2008104812A3
公开(公告)日：2008-10-30
申请号：PCT/GB2008050150
申请日：2008-03-03
申请人： BIOTICA TECH LTD , MOSS STEVEN , MARTIN CHRISTINE , ZHANG MING
发明人： MOSS STEVEN , MARTIN CHRISTINE , ZHANG MING
IPC分类号： C07D225/06 , A61K31/395 , A61P35/00
CPC分类号： C07D225/06
摘要： According to the invention there are provided derivatives of a C21-deoxy ansamycin or salt thereof which contain a 1-hydroxyphenyl moiety bearing at position 3 an aminocarboxy substituent, in which position 5 and the aminocarboxy substituent at position 3 are connected by an aliphatic chain of varying length characterised in that the 1-hydroxy position of the phenyl ring is derivatised by an aminoalkyleneaminocarbonyl group, which alkylene group (which may optionally be substituted by alkyl groups) has a chain length of 2 or 3 carbon atoms, a phosphoric acid, or a phosphoric acid ester (such as an alkyl ester) group, or a salt thereof, and which derivatising group increases the water solubility and/or the bioavailability of the parent molecule. Such compounds are useful in therapy eg in the treatment of cancer and B-cell malignancies.
摘要翻译：根据本发明，提供了一种C21-脱氧安莎霉素或其盐的衍生物，其含有在位置3具有氨基羧基取代基的1-羟基苯基部分，其中位置5和位置3上的氨基羧基取代基通过脂族链连接变化的长度，其特征在于苯环的1-羟基位置被氨基亚烷基氨基羰基衍生，该亚烷基（其可以任选被烷基取代）具有2或3个碳原子的链长，磷酸或磷酸酯（例如烷基酯）或其盐，并且该衍生基增加了母体分子的水溶性和/或生物利用度。这样的化合物可用于治疗，例如治疗癌症和B细胞恶性肿瘤。

40. 发明申请

WO2007113269A3 15-DESMETHOXYMACBECIN DERIVATIVES FOR THE TREATMENT OF CANCER DISEASES 审中-公开
标题翻译：用于治疗癌症疾病的15-脱乙酰壳多糖衍生物
公开(公告)号：WO2007113269A3
公开(公告)日：2007-11-29
申请号：PCT/EP2007053130
申请日：2007-03-30
申请人： BIOTICA TECH LTD , GAISSER SABINE , MARTIN CHRISTINE , ZHANG MING , WILKINSON BARRIE , COATES NIGEL , NUR-E-ALAM MOHAMMED , GAITATZIS NIKOLAOS
发明人： GAISSER SABINE , MARTIN CHRISTINE , ZHANG MING , WILKINSON BARRIE , COATES NIGEL , NUR-E-ALAM MOHAMMED , GAITATZIS NIKOLAOS
IPC分类号： C07D225/06 , A61K31/395 , A61P35/00
CPC分类号： C07D225/06
摘要： The present invention relates to 15-desmethoxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and / or prophylaxis of cancer or B-cell malignancies.
摘要翻译：本发明涉及15-脱甲氧基锍类似物，其可用于，例如，在治疗癌症，B细胞恶性疟疾，真菌感染，中枢神经系统疾病和神经变性疾病，依赖于血管生成的疾病，自身免疫疾病和/或作为癌症的预防性预处理。本发明还提供了这些化合物的制备方法及其在医药中的用途，特别是用于治疗和/或预防癌症或B细胞恶性肿瘤的方法。

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