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1. 发明授权

US08957056B2 Migrastatin analogs in the treatment of cancer 有权
公开(公告)号：US08957056B2
公开(公告)日：2015-02-17
申请号：US11597678
申请日：2005-05-25
申请人： Samuel J. Danishefsky , Christoph Gaul , Jón T. Njardarson , Malcolm A. S. Moore , Kaida Wu , David C. Dorn , Mihirbaran Mandal
发明人： Samuel J. Danishefsky , Christoph Gaul , Jón T. Njardarson , Malcolm A. S. Moore , Kaida Wu , David C. Dorn , Mihirbaran Mandal
IPC分类号： A61K31/395 , A61K31/335 , C07D313/00 , C07D225/02 , A61K31/365 , A61K31/435
CPC分类号： A61K31/395 , A61K31/365 , A61K31/435
摘要： In one aspect, the present invention provides a method for treating colon and/or ovarian cancer in a subject comprising administering to a subject in need thereof a compound of general formula (I): wherein R1-R6, R, -R, Q, Y1, Y2 and n are as defined herein, wherein the compound is present in an amount effective to inhibit colon and/or ovarian tumor metastasis.

2. 发明授权

US08188141B2 Isomigrastatin analogs in the treatment of cancer 失效
标题翻译：异麦地他汀类似物治疗癌症
公开(公告)号：US08188141B2
公开(公告)日：2012-05-29
申请号：US11663580
申请日：2005-09-23
申请人： Samuel J. Danishefsky , Mihirbaran Mandal , David C. Dorn , Malcolm A. S. Moore
发明人： Samuel J. Danishefsky , Mihirbaran Mandal , David C. Dorn , Malcolm A. S. Moore
IPC分类号： A61K31/38 , A61K31/335 , C07D337/00 , C07D309/00 , C07C49/00
CPC分类号： C07D313/00
摘要： The present invention provides compounds having formula (I): (I) wherein n, R1-R5, Ra-Rb, Q, Y1 and Y2 are as defined herein; and additionally provides methods for the synthesis thereof, compositions thereof, and methods for the use thereof in the treatment of various disorders including cancer, metastasis and disorders involving increased angiogenesis.
摘要翻译：本发明提供具有式（I）的化合物：（I）其中n，R 1 -R 5，R a -R b，Q，Y 1和Y 2如本文所定义; 并且另外提供其合成方法，其组合物及其用于治疗包括癌症，转移和涉及增加的血管发生的病症的各种疾病的方法。

3. 发明授权

US07384964B2 Synthesis of epothilones, intermediates thereto, analogues and uses thereof 有权
标题翻译：埃坡霉素的合成，其中间体，其类似物及其用途
公开(公告)号：US07384964B2
公开(公告)日：2008-06-10
申请号：US10921109
申请日：2004-08-18
申请人： Samuel J. Danishefsky , Alexey Rivkin , Fumihiko Yoshimura , Ting-Chao Chou , Ana E. Gabarda , Huajin Dong , Kaida Wu , Malcolm A. S. Moore , David Dorn
发明人： Samuel J. Danishefsky , Alexey Rivkin , Fumihiko Yoshimura , Ting-Chao Chou , Ana E. Gabarda , Huajin Dong , Kaida Wu , Malcolm A. S. Moore , David Dorn
IPC分类号： A61K31/428 , A61K31/427 , A61K31/422 , A61K31/423 , C07D417/04 , C07D413/04 , C07D417/06
CPC分类号： C07D417/06 , C07D413/06 , C07D493/04
摘要： The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).
摘要翻译：本发明提供式（I）化合物：如本文中一般性地和类别和亚类所述。本发明还提供包含式（I）化合物的药物组合物，并提供治疗癌症的方法，包括施用式（I）化合物。

4. 发明授权

US07875638B2 Synthesis of epothilones, intermediates thereto, analogues and uses thereof 有权
标题翻译：埃坡霉素的合成，其中间体，其类似物及其用途
公开(公告)号：US07875638B2
公开(公告)日：2011-01-25
申请号：US12135823
申请日：2008-06-09
申请人： Samuel J. Danishefsky , Alexey Rivkin , Fumihiko Yoshimura , Ting-Chao Chou , Ana E. Gabarda , Huajin Dong , Kaida Wu , Malcolm A. S. Moore , David Dorn
发明人： Samuel J. Danishefsky , Alexey Rivkin , Fumihiko Yoshimura , Ting-Chao Chou , Ana E. Gabarda , Huajin Dong , Kaida Wu , Malcolm A. S. Moore , David Dorn
IPC分类号： A61K31/427 , C07D417/06
CPC分类号： C07D417/06 , C07D493/04
摘要： The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).
摘要翻译：本发明提供式（I）化合物：如本文中一般性地和类别和亚类所述。本发明还提供包含式（I）化合物的药物组合物，并提供治疗癌症的方法，包括施用式（I）化合物。

5. 发明授权

US06403559B1 C-kit ligand-based method for expanding peripheral blood cell levels 失效
标题翻译：用于扩增外周血细胞水平的基于C-kit配体的方法
公开(公告)号：US06403559B1
公开(公告)日：2002-06-11
申请号：US09371261
申请日：1999-08-10
申请人： Peter Besmer , Jochen Buck , Malcolm A. S. Moore , Karl Nocka
发明人： Peter Besmer , Jochen Buck , Malcolm A. S. Moore , Karl Nocka
IPC分类号： A61K3804
CPC分类号： A61K31/7072 , A61K38/00 , A61K38/193 , A61K38/202 , C07K14/475 , C07K14/52 , C07K14/705 , C07K14/71 , C07K14/715 , C07K16/22 , C12N15/87 , A61K2300/00
摘要： A pharmaceutical composition which comprises the c-kit ligand (KL) purified by applicants or produced by applicants' recombinant methods in combination with other hematopoietic factors and a pharmaceutically acceptable carrier is provided as well as methods of treating patients which comprise administering to the patient the pharmaceutical composition of this invention. This invention provides combination therapies using c-kit ligand (KL) and a purified c-kit ligand (KL) polypeptide, or a soluble fragment thereof and other hematopoietic factors. It also provides methods and compositions for ex-vivo use of KL alone or in combination therapy. A mutated KL antagonist is also described. Such an antagonist may also be a small molecule. Antisense nucleic acids to KL as therapeutics are also described. Lastly, compositions and methods are described that take advantage of the role of KL in germ cells, mast cells and melanocytes.
摘要翻译：提供了包含通过申请人纯化或由申请人的重组方法与其他造血因子组合产生的c-kit配体（KL）和药学上可接受的载体的药物组合物，以及治疗患者的方法，其包括向患者施用本发明的药物组合物。本发明提供了使用c-kit配体（KL）和纯化的c-kit配体（KL）多肽或其可溶性片段和其他造血因子的组合疗法。它还提供单独使用KL或联合治疗的离体使用KL方法和组合物。还描述了突变的KL拮抗剂。这样的拮抗剂也可以是小分子。还描述了作为治疗剂的KL的反义核酸。最后，描述了利用KL在生殖细胞，肥大细胞和黑素细胞中的作用的组合物和方法。

6. 发明授权

US6114166A Human pluripotent hematopoietic colony stimulating factor and cell line producing same 失效
标题翻译：人类多能造血集落刺激因子和细胞系相同
公开(公告)号：US6114166A
公开(公告)日：2000-09-05
申请号：US996051
申请日：1997-12-22
申请人： Karl Welte , Erich Platzer , Janice L. Gabrilove , Roland Mertelsmann , Malcolm A. S. Moore
发明人： Karl Welte , Erich Platzer , Janice L. Gabrilove , Roland Mertelsmann , Malcolm A. S. Moore
IPC分类号： A61K38/00 , A61K38/18 , A61K38/19 , C07H21/04 , C07K1/14 , C07K1/18 , C07K1/22 , C07K1/30 , C07K14/435 , C07K14/475 , C07K14/52 , C07K14/53 , C07K14/535 , C07K14/575 , C12N5/08 , C12P21/02
CPC分类号： C07K14/53 , A61K38/00
摘要： Highly purified Pluripotent hematopoietic colony-stimulating factor (pluripotent CSF), a glycoprotein (MW 19,600) constitutively produced by human tumor cells has been highly purified from low serum-containing conditioned medium to apparant homogeneity. Pluripotent CSF supports the growth of human mixed colonies (CFU-GEMM), granulocyte-macrophage colonies (CFU-GM), early erythroid colonies (BFU-E) and induces differentiation of human leukemic cells. The specific activity of the purified pluripotent CSF in the CFU-GM assay is 1.5.times.10.sup.8 U/mg protein.
摘要翻译：高度纯化的多能造血集落刺激因子（多能性CSF），由人类肿瘤细胞组成型产生的糖蛋白（MW19,600）已被高纯度从含有低血清的条件培养基中提取至均匀性。多能CSF支持人混合菌落（CFU-GEMM），粒细胞 - 巨噬细胞集落（CFU-GM），早期红系菌落（BFU-E）的生长，并诱导人类白血病细胞的分化。纯化多能CSF在CFU-GM测定中的比活性为1.5×10 8 U / mg蛋白质。

7. 发明授权

US5935565A Method for increasing the level of stem cells in peripheral blood 失效
标题翻译：增加外周血干细胞水平的方法
公开(公告)号：US5935565A
公开(公告)日：1999-08-10
申请号：US478414
申请日：1995-06-07
申请人： Peter Besmer , Jochen Buck , Malcolm A. S. Moore , Karl Nocka
发明人： Peter Besmer , Jochen Buck , Malcolm A. S. Moore , Karl Nocka
IPC分类号： A61K8/00 , A61K8/64 , A61K38/00 , A61K38/17 , A61K38/18 , A61K38/19 , A61K39/395 , A61K48/00 , A61P7/00 , A61P7/06 , A61P11/00 , A61P25/00 , A61P31/12 , A61P35/02 , A61P37/08 , A61P43/00 , A61Q5/00 , A61Q7/00 , C07K14/00 , C07K14/475 , C07K14/52 , C07K14/705 , C07K14/71 , C07K14/715 , C07K16/00 , C07K16/22 , C07K19/00 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/87 , C12P21/02 , C12P21/08 , C12R1/91 , A61K45/05 , A61K37/00
CPC分类号： A61K31/7072 , A61K38/193 , A61K38/202 , C07K14/475 , C07K14/52 , C07K14/705 , C07K14/71 , C07K14/715 , C07K16/22 , C12N15/87 , A61K38/00
摘要： A pharmaceutical composition which comprises the c-kit ligand (KL) purified by applicants or produced by applicants' recombinant methods in combination with other hematopoietic factors and a pharmaceutically acceptable carrier is provided as well as methods of treating patients which comprise administering to the patient the pharmaceutical composition of this invention. This invention provides combination therapies using c-kit ligand (KL) and a purified c-kit ligand (KL) polypeptide, or a soluble fragment thereof and other hematopoietic factors. It also provides methods and compositions for ex-vivo use of KL alone or in combination therapy. A mutated KL antagonist is also described. Such an antagonist may also be a small molecule. Antisense nucleic acids to KL as therapeutics are also described. Lastly, compositions and methods are described that take advantage of the role of KL in germ cells, mast cells and melanocytes.
摘要翻译：提供了包含通过申请人纯化或由申请人的重组方法与其他造血因子组合产生的c-kit配体（KL）和药学上可接受的载体的药物组合物，以及治疗患者的方法，其包括向患者施用本发明的药物组合物。本发明提供了使用c-kit配体（KL）和纯化的c-kit配体（KL）多肽或其可溶性片段和其他造血因子的组合疗法。它还提供单独使用KL或联合治疗的离体使用KL方法和组合物。还描述了突变的KL拮抗剂。这样的拮抗剂也可以是小分子。还描述了作为治疗剂的KL的反义核酸。最后，描述了利用KL在生殖细胞，肥大细胞和黑素细胞中的作用的组合物和方法。

8. 发明授权

US5670146A Pharmacological preparations comprising human pluripotent hematopoietic colony stimulating factor 失效
标题翻译：包括人多能造血集落刺激因子的药理学制剂
公开(公告)号：US5670146A
公开(公告)日：1997-09-23
申请号：US480356
申请日：1995-06-07
申请人： Karl Welte , Erich Platzer , Janice L. Gabrilove , Roland Mertelsm , Malcolm A. S. Moore
发明人： Karl Welte , Erich Platzer , Janice L. Gabrilove , Roland Mertelsm , Malcolm A. S. Moore
IPC分类号： A61K38/00 , A61K38/18 , A61K38/19 , C07H21/04 , C07K1/14 , C07K1/18 , C07K1/22 , C07K1/30 , C07K14/435 , C07K14/475 , C07K14/52 , C07K14/53 , C07K14/535 , C07K14/575 , C12N5/08 , C12P21/02
CPC分类号： C07K14/53 , A61K38/00
摘要： Highly purified Pluripotent hematopoietic colony-stimulating factor (pluripotent CSF), a glycoprotein (MW 19,600) constitutively produced by human tumor cells has been highly purified from low serum-containing conditioned medium to apparant homogeneity. Pluripotent CSF supports the growth of human mixed colonies (CFU-GEMM), granulocyte-macrophage colonies (CFU-GM), early erythroid colonies (BFU-E) and induces differentiation of human leukemic cells. The specific activity of the purified pluripotent CSF in the CFU-GM assay is 1.5.times.10.sup.8 U/mg protein.
摘要翻译：高度纯化的多能造血集落刺激因子（多能性CSF），由人类肿瘤细胞组成型产生的糖蛋白（MW19,600）已被高纯度从含有低血清的条件培养基中提取至均匀性。多能CSF支持人混合菌落（CFU-GEMM），粒细胞 - 巨噬细胞集落（CFU-GM），早期红系菌落（BFU-E）的生长，并诱导人类白血病细胞的分化。纯化多能CSF在CFU-GM测定中的比活性为1.5×10 8 U / mg蛋白质。

9. 发明授权

US06838549B2 Human pluripotent hematopoietic colony stimulating factor, method of production and use 失效
标题翻译：人类多能造血集落刺激因子，生产和使用方法
公开(公告)号：US06838549B2
公开(公告)日：2005-01-04
申请号：US10117423
申请日：2002-04-04
申请人： Karl Welte , Erich Platzer , Janice L. Gabrilove , Roland Mertelsmann , Malcolm A. S. Moore
发明人： Karl Welte , Erich Platzer , Janice L. Gabrilove , Roland Mertelsmann , Malcolm A. S. Moore
IPC分类号： A61K38/00 , A61K38/18 , A61K38/19 , C07H21/04 , C07K1/14 , C07K1/18 , C07K1/22 , C07K1/30 , C07K14/435 , C07K14/475 , C07K14/52 , C07K14/53 , C07K14/535 , C07K14/575 , C12N5/08 , C12P21/02
CPC分类号： C07K14/53 , A61K38/00
摘要： Highly purified Pluripotent hematopoietic colony-stimulating factor (pluripotent CSF), a glycoprotein (MW 19,600) constitutively produced by human tumor cells has been highly purified from low serum-containing conditioned medium to apparant homogeneity. Pluripotent CSF supports the growth of human mixed colonies (CFU-GEMM), granulocyte-macrophage colonies (CFU-GM), early erythroid colonies (BFU-E) and induces differentiation of human leukemic cells. The specific activity of the purified pluripotent CSF in the CFU-GM assay is 1.5×108 U/mg protein.

10. 发明授权

US6001803A Composition of c-kit ligand, GM-CSF, and TNF-.alpha. and method of use 失效
标题翻译： c-kit配体，GM-CSF和TNF-α的组成及其使用方法
公开(公告)号：US6001803A
公开(公告)日：1999-12-14
申请号：US325240
申请日：1994-10-20
申请人： Peter Besmer , Jochen Buck , Malcolm A. S. Moore , Karl Nocka
发明人： Peter Besmer , Jochen Buck , Malcolm A. S. Moore , Karl Nocka
IPC分类号： A61K38/00 , A61K38/18 , A61K38/19 , A61K38/04 , C07K14/525 , C07K14/535
CPC分类号： A61K38/18 , A61K38/191 , A61K38/193 , C12N5/0639 , C12N5/0647 , C12N2501/125 , C12N2501/14 , C12N2501/21 , C12N2501/22 , C12N2501/2301 , C12N2501/2303 , C12N2501/2306 , C12N2501/25
摘要： A pharmaceutical composition which comprises the c-kit ligand (KL) purified by applicants or produced by applicants' recombinant methods in combination with other hematopoietic factors and a pharmaceutically acceptable carrier is provided as well as methods of treating patients which comprise administering to the patient the pharmaceutical composition of this invention. This invention provides combination therapies using c-kit ligand (KL) and a purified c-kit ligand (KL) polypeptide, or a soluble fragment thereof and other hematopoietic factors. It also provides methods and compositions for ex-vivo use of KL alone or in combination therapy. A mutated KL antagonist is also described. Such an antagonist may also be a small molecule. Antisense nucleic acids to KL as therapeutics are also described. Lastly, compositions and methods are described that take advantage of the role of KL in germ cells, mast cells and melanocytes.
摘要翻译：提供了包含通过申请人纯化或由申请人的重组方法与其他造血因子组合产生的c-kit配体（KL）和药学上可接受的载体的药物组合物，以及治疗患者的方法，其包括向患者施用本发明的药物组合物。本发明提供了使用c-kit配体（KL）和纯化的c-kit配体（KL）多肽或其可溶性片段和其他造血因子的组合疗法。它还提供单独使用KL或联合治疗的离体使用KL方法和组合物。还描述了突变的KL拮抗剂。这样的拮抗剂也可以是小分子。还描述了作为治疗剂的KL的反义核酸。最后，描述了利用KL在生殖细胞，肥大细胞和黑素细胞中的作用的组合物和方法。

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