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1. 发明申请

US20090149516A1 Synthesis of Epothilones, Intermediates Thereto, Analogues and Uses Thereof 有权
标题翻译：埃坡霉素，其中间体的合成，其类似物及用途
公开(公告)号：US20090149516A1
公开(公告)日：2009-06-11
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 , A61P35/00
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。

2. 发明申请

US20090124662A1 Migrastatin analogs in the treatment of cancer 失效
标题翻译：米舍他汀类似物治疗癌症
公开(公告)号：US20090124662A1
公开(公告)日：2009-05-14
申请号：US11597678
申请日：2006-05-25
申请人： Samuel J. Danishefsky , Christoph Gaul , Jon T. Njardarson , Malcolm A.S. Moore , Kaida Wu , David C. Dorn , Mihirbaran Mandal
发明人： Samuel J. Danishefsky , Christoph Gaul , Jon T. Njardarson , Malcolm A.S. Moore , Kaida Wu , David C. Dorn , Mihirbaran Mandal
IPC分类号： A61K31/4523 , A61P35/00 , A61P25/00
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.
摘要翻译：一方面，本发明提供了一种用于治疗受试者中结肠和/或卵巢癌的方法，包括向有需要的受试者施用通式（I）的化合物：其中R1-R6，R，-R，Q， Y1，Y2和n如本文所定义，其中化合物以有效抑制结肠和/或卵巢肿瘤转移的量存在。

3. 发明申请

US20090054488A1 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：US20090054488A1
公开(公告)日：2009-02-26
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： A61K31/4523 , C07D405/02 , A61P35/00 , A61P9/00 , A61P37/00 , A61P7/00 , A61P31/00
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。

4. 发明授权

US07998938B2 Cancer treatment by combined inhibition of proteasome and telomerase activities 有权
标题翻译：癌症治疗联合抑制蛋白酶体和端粒酶活性
公开(公告)号：US07998938B2
公开(公告)日：2011-08-16
申请号：US11918581
申请日：2006-04-14
申请人： Malcolm A.S. Moore , Allison C. Chin
发明人： Malcolm A.S. Moore , Allison C. Chin
IPC分类号： A16K48/00
CPC分类号： C12N15/1137 , A61K31/454 , A61K45/06 , C12N2310/11 , C12N2310/3145 , C12N2310/3515 , C12Y207/07049 , A61K2300/00
摘要： A method and kit for inhibiting the proliferation of cancer cells are disclosed, based on a combination of a proteasome inhibitor and a telomerase inhibitor. When used in cancer therapy, the two compounds in combination enhance the anti-cancer treatment efficacy obtained with the proteasome inhibitor alone or the telomerase inhibitor alone. Preferably, efficacy is supraadditive or synergistic in nature relative to the combined effects of the individual agents, with minimal exacerbation of side effects.
摘要翻译：基于蛋白酶体抑制剂和端粒酶抑制剂的组合，公开了抑制癌细胞增殖的方法和试剂盒。当用于癌症治疗时，两种化合物组合增强了单独使用蛋白酶体抑制剂或单独使用端粒酶抑制剂获得的抗癌治疗功效。优选地，相对于各个试剂的组合效应，效力是相对于辅助的或协同的，并且副作用的加剧最小化。

5. 发明申请

US20080152652A1 Ligand for the c-kit receptor and methods of use thereof 审中-公开
标题翻译： c-kit受体的配体及其使用方法
公开(公告)号：US20080152652A1
公开(公告)日：2008-06-26
申请号：US11890212
申请日：2007-08-03
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： A61K39/395 , A61P35/00
CPC分类号： A61K38/193 , A61K38/2006 , A61K38/2026 , C07K14/475 , C07K16/22 , 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. 发明申请

US20150030583A1 Methods of Treating Serosal Cancer 审中-公开
标题翻译：治疗血清癌的方法
公开(公告)号：US20150030583A1
公开(公告)日：2015-01-29
申请号：US14009176
申请日：2012-03-30
申请人： Malcolm A.S. Moore , Server A. Ertem
发明人： Malcolm A.S. Moore , Server A. Ertem
IPC分类号： A61K38/48 , A61K47/48 , A61K31/337 , A61K31/4045 , A61N5/10 , A61K31/165 , A61K31/365 , A61K31/03 , G01N33/50 , A61K38/47 , A61K31/5377
CPC分类号： A61K38/4886 , A61K31/03 , A61K31/16 , A61K31/165 , A61K31/23 , A61K31/337 , A61K31/365 , A61K31/4045 , A61K31/5377 , A61K38/47 , A61K45/06 , A61K47/60 , A61N5/1001 , C12Y302/01035 , C12Y304/24007 , G01N33/5011 , G01N2800/52 , G01N2800/7028 , A61K2300/00
摘要： The discovery of clonally pure populations of serosal cancer stem cells (CSCs) as well as methods of producing CSCs, culturing the CSCs and using them in screening assays, has lead to the development of methods of treating serosal and ovarian cancers by targeting removal or inhibition of the glycocalyx coat surrounding such cells, and includes combination therapies using particular chemotherapeutics in conjunction with glycocalyx inhibitors, as well as the same new chemotherapy treatments without targeting the glycocalyx, where the chemotherapeutic agent is any one of LBH-589 (Panobinostat), NVP-AUY922, LAQ824 (NVP-LAQ824, Dacinostat), colchicine, brefeldin A, diphenyleneiodonium chloride, any combination thereof or another agent identified herein. These treatment methods of the invention can also be used in combination with radiation treatment or other conventional cancer therapy.
摘要翻译：克隆纯化的浆细胞癌干细胞（CSCs）的发现以及产生CSCs的方法，培养CSCs并在筛选测定中使用它们，导致通过靶向去除或抑制来治疗浆膜和卵巢癌的方法的发展包括围绕这样的细胞的糖萼胶衣，并且包括使用特定化学治疗剂结合糖萼抑制剂的组合疗法，以及不针对糖萼的相同的新化学疗法治疗，其中化学治疗剂是LBH-589（Panobinostat），NVP -AUY922，LAQ824（NVP-LAQ824，Dacinostat），秋水仙碱，布雷菲德菌素A，二苯基碘鎓氯化物，其任何组合或本文鉴定的另一种药剂。本发明的这些治疗方法也可以与放射治疗或其他常规癌症治疗组合使用。

7. 发明申请

US20120219506A1 Catenae: Serosal Cancer Stem Cells 审中-公开
标题翻译： Catenae：Serosal Cancer干细胞
公开(公告)号：US20120219506A1
公开(公告)日：2012-08-30
申请号：US13508110
申请日：2010-11-05
申请人： Malcolm A.S. Moore , Server A. Ertem
发明人： Malcolm A.S. Moore , Server A. Ertem
IPC分类号： A61K49/00 , A61K38/46 , C12Q1/68 , G01N33/574 , C12Q1/34 , C12Q1/37 , C12Q1/02 , C12Q1/06 , C12P1/00 , C12N5/00 , C12N5/02 , C12N15/63 , C07K14/435 , C07H21/04 , A61P35/00 , C07H21/02 , A61K38/54
CPC分类号： C12N5/0695 , A01K2207/12 , A01K2267/0331 , C12N9/1051
摘要： The present invention relates to a clonally pure population of serosal cancer stem cells (CSCs) as well as methods of producing and culturing the CSCs and uses thereof. The CSCs form catenae (free floating chains of cells) which have a glycocalyx coat of hyaluronan and proteoglycans. This discovery has lead to the development of methods of treating serosal and ovarian cancers by targeting removal or inhibition of glycocalyx formation, including combination therapies using chemotherapeutics in conjunction with glycocalyx inhibitors. The invention also provides drug screening assays for identifying compounds effective against these CSCs as well as other serosal cancer cells. Methods to use catena gene signatures, protein and surface antigens are provided for monitoring patient samples for the presence of serosal cancer stem cells.
摘要翻译：本发明涉及克隆纯化的浆细胞癌干细胞群（CSCs）以及生产和培养CSCs的方法及其应用。 CSCs形成具有透明质酸和蛋白聚糖的糖萼层的悬链（游离的细胞链）。这一发现导致通过靶向去除或抑制糖萼形成来治疗浆膜和卵巢癌的方法的开发，包括使用化学治疗剂与糖萼抑制剂结合的组合疗法。本发明还提供用于鉴定对这些CSC以及其它浆膜癌细胞有效的化合物的药物筛选测定。提供使用catena基因特征，蛋白质和表面抗原的方法来监测患者样品中是否存在浆膜癌干细胞。

8. 发明授权

US5767074A Compositions of soluble C-kit ligand and hematopoietic factors 失效
标题翻译：可溶性C-kit配体和造血因子的组成
公开(公告)号：US5767074A
公开(公告)日：1998-06-16
申请号：US341456
申请日：1994-11-17
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 , A61K38/17 , A61K38/18 , A61K38/19 , C07K14/475 , C07K14/52 , C07K14/705 , C07K14/71 , C07K14/715 , C07K16/22 , C12N15/87 , A61K38/04 , C07K14/435
CPC分类号： C12N15/87 , A61K38/193 , A61K38/2006 , A61K38/202 , A61K38/204 , C07K14/475 , C07K14/52 , C07K14/705 , C07K14/71 , C07K14/715 , C07K16/22 , 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。

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