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1. 发明申请

US20110033458A1 COMBINATIONS COMPRISING EPOTHILONES AND PHARMACEUTICAL USES THEREOF 审中-公开
标题翻译：包含EPOTHILONES及其药物用途的组合
公开(公告)号：US20110033458A1
公开(公告)日：2011-02-10
申请号：US12908533
申请日：2010-10-20
申请人： John Arthur Hohneker , Julie Ann Miller , John David Rothermel , Markus Wartmann
发明人： John Arthur Hohneker , Julie Ann Miller , John David Rothermel , Markus Wartmann
IPC分类号： A61K39/395 , A61K31/427 , A61P35/00
CPC分类号： C07K16/3015 , A61K31/426 , A61K31/427 , A61K39/39558 , A61K45/06 , A61K2039/505 , C07D417/06 , A61K2300/00
摘要： The invention relates to a pharmaceutical combination which comprises (a) a HER-1 or a HER-2 antibody or (b) at least one antineoplastic agent selected from the group consisting of aromatase inhibitors, antiestrogens, topoisomerase I inhibitors, topoisomerase II inhibitors, microtubule active agents, protein kinase C inhibitors, anti-angiogenic compounds, gonadorelin agonists, anti-androgens, histone deacetylase inhibitors and S-adenosylmethionine decarboxylase inhibitors; and (c) an epothilone derivative of formula I and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular, for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
摘要翻译：本发明涉及药物组合，其包含（a）HER-1或HER-2抗体或（b）至少一种抗肿瘤剂，其选自芳香酶抑制剂，抗雌激素，拓扑异构酶I抑制剂，拓扑异构酶II抑制剂，微管活性剂，蛋白激酶C抑制剂，抗血管生成化合物，促性腺激素激动剂，抗雄激素，组蛋白脱乙酰酶抑制剂和S-腺苷甲硫氨酸脱羧酶抑制剂; 和（c）式I的埃坡霉素衍生物和任选的至少一种用于同时，分别或顺序使用的药学上可接受的载体，特别是用于治疗增殖性疾病，特别是实体肿瘤疾病; 包含这种组合的药物组合物; 使用这种组合来制备用于治疗增殖性疾病的药物; 包括作为用于同时，分开或顺序使用的组合制剂的组合的商业包装或产品; 以及治疗温血动物，特别是人的方法。

2. 发明申请

US20060223867A1 Cancer treatment with epothilones 失效
公开(公告)号：US20060223867A1
公开(公告)日：2006-10-05
申请号：US11406896
申请日：2006-04-19
申请人： Terence O'Reilly , Markus Wartmann , Manuel Litchman , Pamela Cohen
发明人： Terence O'Reilly , Markus Wartmann , Manuel Litchman , Pamela Cohen
IPC分类号： A61K31/427
CPC分类号： A61K31/425
摘要： The invention relates to the treatment of a proliferative disease, especially according to certain treatment regimens, with an epothilone, especially with epothilone A and more preferably epothilone B; as well as to the treatment of certain cancers with such an epothilone.

3. 发明授权

US08008330B2 Combinations comprising epothilones and pharmaceutical uses thereof 失效
标题翻译：包含埃坡霉素及其药物用途的组合
公开(公告)号：US08008330B2
公开(公告)日：2011-08-30
申请号：US12549947
申请日：2009-08-28
申请人： TianLing Chen , Diane Greeley , John David Rothermel , Markus Wartmann , Jeanette Marjorie Wood
发明人： TianLing Chen , Diane Greeley , John David Rothermel , Markus Wartmann , Jeanette Marjorie Wood
IPC分类号： A61K31/427 , A61K31/28
CPC分类号： A61K31/663 , A61K31/427 , A61K31/502 , A61K31/555 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The invention relates to a combination which comprises (a) a bisphosphonate, a platinum compound or a vasculostatic compound and (b) an epothilone derivative of formula I wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl, and Z is O or a bond, in which the active ingredients (a) and (b) are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition, a commercial package or product comprising such a combination; the use of such a combination for the preparation of a medicament for the delay of progression or treatment of a proliferative disease and to a method of treatment of a warm-blooded animal.
摘要翻译：本发明涉及一种组合，其包含（a）二膦酸盐，铂化合物或血管保护性化合物和（b）式I的埃坡霉素衍生物，其中A表示O或NRN，其中RN为氢或低级烷基，R为氢或低级烷基和Z是O或键，其中活性成分（a）和（b）在每种情况下以游离形式或以药学上可接受的盐和任选的至少一种药学上可接受的载体的形式存在，单独或顺序使用，特别是用于延缓进展或治疗增殖性疾病，特别是实体肿瘤疾病; 药物组合物，商业包装或包含这种组合的产品; 使用这种组合来制备用于延缓进展或治疗增殖性疾病的药物以及治疗温血动物的方法。

4. 发明申请

US20090191264A1 EPOTHILONE COMPOSITIONS 审中-公开
标题翻译： EPOTHILONE组合物
公开(公告)号：US20090191264A1
公开(公告)日：2009-07-30
申请号：US12417717
申请日：2009-04-03
申请人： Jean-Claude Sonntag , Markus Wartmann , Karl-Heinz Altmann
发明人： Jean-Claude Sonntag , Markus Wartmann , Karl-Heinz Altmann
IPC分类号： A61K9/127 , A61K31/425
CPC分类号： A61K9/127 , A61K9/1271 , A61K31/427
摘要： This invention provides liposomal compositions comprising an epothilone.
摘要翻译：本发明提供包含埃坡霉素的脂质体组合物。

5. 发明申请

US20080131884A1 Tubulin Mutation Diagnostic 审中-公开
标题翻译：微管蛋白突变诊断
公开(公告)号：US20080131884A1
公开(公告)日：2008-06-05
申请号：US11718957
申请日：2005-11-10
申请人： Kenneth Wayne Culver , Markus Wartmann , Stan Lilleberg , Jian Zhu
发明人： Kenneth Wayne Culver , Markus Wartmann , Stan Lilleberg , Jian Zhu
IPC分类号： A61K48/00 , A61P43/00 , C07H21/04 , C07K16/00 , C12Q1/68 , G01N33/53
CPC分类号： C12Q1/6883 , C07K14/47 , C12Q2600/106 , C12Q2600/156 , G01N33/5008 , G01N33/5011 , G01N33/68 , G01N33/6848 , G01N2800/52
摘要： The present invention relates to methods for determining the potential of a subject to respond to a particular therapeutic agent, by determining the presence of one or more nucleotide or amino acid variants in the β-tubulin gene or protein. Also provided are methods for treating subjects whose potential to respond to a therapeutic agent has been evaluated. For use in the methods of the invention, there are provided variants of the β-tubulin gene, variants of the β-tubulin protein, nucleic acid molecules and agents which bind to the variant β-tubulin nucleic acid molecules and variant β-tubulin protein, respectively, and kits comprising the same.
摘要翻译：本发明涉及通过测定β-微管蛋白基因或蛋白质中一个或多个核苷酸或氨基酸变体的存在来确定受试者对特定治疗剂作出反应的潜力的方法。还提供了用于治疗对治疗剂有响应的潜能的方法。为了用于本发明的方法，提供β-微管蛋白基因的变体，β-微管蛋白的变体，结合变体β-微管蛋白核酸分子和变体β-微管蛋白的核酸分子和试剂，以及包含其的试剂盒。

6. 发明授权

US07612052B2 Combinations comprising epothilones and pharmaceutical uses thereof 失效
标题翻译：包含埃坡霉素及其药物用途的组合
公开(公告)号：US07612052B2
公开(公告)日：2009-11-03
申请号：US12019294
申请日：2008-01-24
申请人： John David Rothermel , Markus Wartmann , Jeanette Marjorie Wood
发明人： John David Rothermel , Markus Wartmann , Jeanette Marjorie Wood
IPC分类号： A61K31/66 , A61K31/425 , A61K31/28
CPC分类号： A61K31/663 , A61K31/427 , A61K31/502 , A61K31/555 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The invention relates to a combination which comprises (a) a bisphosphonate, a platinum compound or a vasculostatic compound and (b) an epothilone derivative of formula I wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl, and Z is O or a bond, in which the active ingredients (a) and (b) are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition, a commercial package or product comprising such a combination; the use of such a combination for the preparation of a medicament for the delay of progression or treatment of a proliferative disease and to a method of treatment of a warm-blooded animal.
摘要翻译：本发明涉及一种组合，其包含（a）二膦酸盐，铂化合物或血管保护性化合物和（b）式I的埃坡霉素衍生物，其中A表示O或NRN，其中RN为氢或低级烷基，R为氢或低级烷基和Z是O或键，其中活性成分（a）和（b）在每种情况下以游离形式或以药学上可接受的盐和任选的至少一种药学上可接受的载体的形式存在，单独或顺序使用，特别是用于延缓进展或治疗增殖性疾病，特别是实体肿瘤疾病; 药物组合物，商业包装或包含这种组合的产品; 使用这种组合来制备用于延缓进展或治疗增殖性疾病的药物以及治疗温血动物的方法。

7. 发明申请

US20090202541A1 COMBINATION COMPRISING N-{5-[4-(4-METHYL-PIPERAZINO-METHYL)-BENZOYLAMIDO]-2-METHYLPHENYL)-4-(3-PYRIDYL)-2PYRIMIDINE-AMINE AND A CHEMOTHERAPEUTIC AGENT 审中-公开
标题翻译：包含N- {5- [4-（4-甲基 - 哌嗪基 - 甲基） - 苯甲酰氨基] -2-甲基苯基）-4-（3-吡啶基）-2-嘧啶胺和化学代谢物的组合
公开(公告)号：US20090202541A1
公开(公告)日：2009-08-13
申请号：US12423079
申请日：2009-04-14
申请人： Christian Bruns , Elisabeth Buchdunger , Terence O'Reilly , Sandra Leta Silberman , Markus Wartmann , Gisbert Weckbecker
发明人： Christian Bruns , Elisabeth Buchdunger , Terence O'Reilly , Sandra Leta Silberman , Markus Wartmann , Gisbert Weckbecker
IPC分类号： A61K31/506 , A61K39/395 , A61K31/704 , A61P35/00
CPC分类号： A61K45/06 , A61K31/506
摘要： A method of treating a warm-blooded animal, especially a human, having a proliferative disease or acute or chronic transplant rejection comprising administering to the animal a combination which comprises (a) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and (b) a chemotherapeutic agent selected from antineoplastic agents, especially as defined herein, and agents effective in treating acute or chronic transplant rejection; a combination comprising (a) and (b) as defined above and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease.
摘要翻译：一种治疗具有增殖性疾病或急性或慢性移植排斥反应的温血动物，特别是人的方法，包括向动物施用包含（a）N- {5- [4-（4-甲基 - 哌嗪子基） - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺和（b）选自抗肿瘤剂，特别是本文所定义的化学治疗剂和有效治疗急性或慢性的药物移植排斥反应包含如上定义的（a）和（b）和任选的至少一种用于同时，分开或顺序使用的药学上可接受的载体的组合，特别是用于延缓进展或治疗增殖性疾病，特别是实体肿瘤疾病。

8. 发明申请

US20090069394A1 CANCER TREATMENT WITH EPOTHILONES 审中-公开
标题翻译：癌症治疗与EPOTHILONES
公开(公告)号：US20090069394A1
公开(公告)日：2009-03-12
申请号：US12269293
申请日：2008-11-12
申请人： Clifford Dilea , Paul M.J. Mcsheehy , Sauveur-Michel Maira , Chiaki Tanaka , Markus Wartmann
发明人： Clifford Dilea , Paul M.J. Mcsheehy , Sauveur-Michel Maira , Chiaki Tanaka , Markus Wartmann
IPC分类号： A61K31/427 , A61P35/00
CPC分类号： A61K45/06 , A61K31/426 , A61K31/427 , A61K2300/00
摘要： The present invention relates to an in vivo regimen for the treatment of a proliferative disease, including non small cell lung carcinoma, where an epothilone, including epothiline B, is administered in a loading dose followed by at least one maintenance doses.
摘要翻译：本发明涉及一种用于治疗增殖性疾病的体内方案，包括非小细胞肺癌，其中埃坡霉素（包括依托泊苯B）以负载剂量施用，随后至少一次维持剂量施用。

9. 发明申请

US20050227300A1 Use of alpha-tubulin acetylation levels as a biomarker for protein deacetylase inhibitors 审中-公开
标题翻译：使用α-微管蛋白乙酰化水平作为蛋白质脱乙酰酶抑制剂的生物标志物
公开(公告)号：US20050227300A1
公开(公告)日：2005-10-13
申请号：US10497333
申请日：2002-12-06
申请人： Peter Atadja , Sjouke Hoving , Harry Towbin , Heather Walker , Markus Wartmann , Lakshmi Yeleswarapu
发明人： Peter Atadja , Sjouke Hoving , Harry Towbin , Heather Walker , Markus Wartmann , Lakshmi Yeleswarapu
IPC分类号： A61K49/00 , C12Q1/02 , C12Q1/48 , C12R1/91 , G01N27/447 , G01N33/15 , G01N33/50 , G01N33/574
CPC分类号： G01N33/5011 , G01N33/574 , G01N2333/916 , G01N2500/10
摘要： The invention relates to a novel method for evaluating the antiproliferative activity of protein deacetylase inhibiting compounds and microtubule interacting agents, as well as a method for screening for compounds that inhibit cell growth or growth of tumors. The invention additionally provides a method for monitoring the progress of treatment against cellular growth or the growth of tumors.
摘要翻译：本发明涉及一种用于评价蛋白质脱乙酰酶抑制化合物和微管相互作用剂的抗增殖活性的新方法，以及用于筛选抑制肿瘤细胞生长或生长的化合物的方法。本发明另外提供了用于监测针对细胞生长或肿瘤生长的治疗进展的方法。

10. 发明申请

US20050165071A1 Cancer treatment with epothilones 失效
标题翻译：用埃坡霉素治疗癌症
公开(公告)号：US20050165071A1
公开(公告)日：2005-07-28
申请号：US11089269
申请日：2005-03-24
申请人： Terence O'Reilly , Markus Wartmann , Manuel Litchman , Pamela Cohen
发明人： Terence O'Reilly , Markus Wartmann , Manuel Litchman , Pamela Cohen
IPC分类号： C07D493/04 , A61K31/425 , A61K31/427 , A61P35/00
CPC分类号： A61K31/425
摘要： The invention relates to the treatment of a proliferative disease, especially according to certain treatment regimens, with an epothilone, especially with epothilone A and more preferably epothilone B; as well as to the treatment of certain cancers with such an epothilone.
摘要翻译：本发明涉及治疗增殖性疾病，特别是根据某些治疗方案，与埃坡霉素，特别是埃坡霉素A，更优选埃坡霉素B; 以及用这种埃坡霉素治疗某些癌症。

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