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1. 发明申请

WO2003063927A2 COMPOSITIONS AND METHODS TO TREAT GASTROINTESTINAL DISORDERS 审中-公开
标题翻译：组合物和治疗胃肠疾病的方法
公开(公告)号：WO2003063927A2
公开(公告)日：2003-08-07
申请号：PCT/US2002/036857
申请日：2002-11-18
申请人： EISAI CO. LTD , IENI, John
发明人： IENI, John
IPC分类号： A61M
CPC分类号： A61K45/06 , A61K31/00 , A61K31/335 , A61K31/43 , A61K31/44 , A61K31/4439 , Y02A50/483 , A61K2300/00
摘要： The invention provides safe and effective methods for treating and preventing dysphagia, lower esophageal mucosal rings, esophageal strictures, achalasia, gastric mucosal injuries, and bacterial infections. The methods comprise administering at least one proton pump inhibitor, optionally in combination with antibacterial compounds. In one embodiment, the proton pump inhibitor is rabeprazole, a pharmaceutically acceptable salt thereof and/or a stereoisomer thereof.
摘要翻译：本发明提供了安全有效的治疗和预防吞咽困难，食管下段食管，食管狭窄，贲门失弛缓症，胃粘膜损伤和细菌感染的方法。所述方法包括施用至少一种质子泵抑制剂，任选地与抗菌化合物组合。在一个实施方案中，质子泵抑制剂是雷贝拉唑，其药学上可接受的盐和/或其立体异构体。

2. 发明申请

WO2003053221A3 METHODS USING PROTON PUMP INHIBITORS 审中-公开
公开(公告)号：WO2003053221A3
公开(公告)日：2003-07-03
申请号：PCT/US2002/040470
申请日：2002-12-18
申请人： EISAI CO. LTD , IENI, John
发明人： IENI, John
IPC分类号： A61K31/445
摘要： The invention provides methods of treating and preventing asthma, laryngitis, symptomatic gastroesophageal reflux disease, pregnancy-induced gastroesophageal reflux disease, noncardiac chest pains, coughing, apnea, dyspepsia, inflammatory bowel disease, irritable bowel syndrome, gastritis, stress ulcers, bleeding peptic ulcers, acute gastrointestinal bleeding, infectious enteritis, collagenous colitis, lymphocytic colitis, chronic diarrhea in immunocompromised patients, esophageal ulcers in immunocompromised patients, idiopathic gastric acid hypersecretion, gastroparesis, gastrointestinal motility disorders, Zollinger-Ellison syndrome, short bowel syndrome, emesis, regurgitation, early satiety, chronic sore throat, abdominal pain, abdominal bloating, nausea, sour stomach, diarrhea, constipation, bacterial infections, refractory ulcers, gastrointestinal disorders induced by NSAIDs, Barrett's esophagus, gastrointestinal disorders caused by steroids, gastrointestinal disorders induced by cholinergic compounds, and fungal or viral-induced ulcers in the gastrointestinal tract by administering a therapeutically effective amount of at least one proton pump to a patient in need thereof. The invention also provides on demand relief of symptoms associated with gastroesophageal reflux disease (GERD), and provides relief from symptoms caused by the consumption of excessive amounts of food and/or alcohol by administering a therapeutically effective amount of at least one proton pump inhibitor to a patient in need thereof. The invention also provides methods for treating parasitic infections, such as malaria, by administering a therapeutically effective amount of at least one proton pump inhibitor to a patient in need thereof.

3. 发明申请

WO2003053221A2 METHODS USING PROTON PUMP INHIBITORS 审中-公开
标题翻译：使用原子泵抑制剂的方法
公开(公告)号：WO2003053221A2
公开(公告)日：2003-07-03
申请号：PCT/US2002/040470
申请日：2002-12-18
申请人： EISAI CO. LTD , IENI, John
发明人： IENI, John
IPC分类号： A61B
CPC分类号： A61K31/415 , A61K31/135 , A61K31/445 , Y02A50/411
摘要： The invention provides methods of treating and preventing asthma, laryngitis, symptomatic gastroesophageal reflux disease, pregnancy-induced gastroesophageal reflux disease, noncardiac chest pains, coughing, apnea, dyspepsia, inflammatory bowel disease, irritable bowel syndrome, gastritis, stress ulcers, bleeding peptic ulcers, acute gastrointestinal bleeding, infectious enteritis, collagenous colitis, lymphocytic colitis, chronic diarrhea in immunocompromised patients, esophageal ulcers in immunocompromised patients, idiopathic gastric acid hypersecretion, gastroparesis, gastrointestinal motility disorders, Zollinger-Ellison syndrome, short bowel syndrome, emesis, regurgitation, early satiety, chronic sore throat, abdominal pain, abdominal bloating, nausea, sour stomach, diarrhea, constipation, bacterial infections, refractory ulcers, gastrointestinal disorders induced by NSAIDs, Barrett's esophagus, gastrointestinal disorders caused by steroids, gastrointestinal disorders induced by cholinergic compounds, and fungal or viral-induced ulcers in the gastrointestinal tract by administering a therapeutically effective amount of at least one proton pump to a patient in need thereof. The invention also provides on demand relief of symptoms associated with gastroesophageal reflux disease (GERD), and provides relief from symptoms caused by the consumption of excessive amounts of food and/or alcohol by administering a therapeutically effective amount of at least one proton pump inhibitor to a patient in need thereof. The invention also provides methods for treating parasitic infections, such as malaria, by administering a therapeutically effective amount of at least one proton pump inhibitor to a patient in need thereof.
摘要翻译：本发明提供治疗和预防哮喘，喉炎，症状性胃食管反流病，妊娠诱发的胃食管反流病，非心脏性胸痛，咳嗽，呼吸暂停，消化不良，炎性肠病，肠易激综合征，胃炎，应激性溃疡，出血性消化性溃疡急性胃肠道出血，感染性肠炎，胶原性结肠炎，淋巴细胞性结肠炎，免疫受损患者的慢性腹泻，免疫受损患者的食管溃疡，特发性胃酸分泌过多，胃轻瘫，胃肠动力障碍，佐林格 - 埃里森综合征，短肠综合征，呕吐，反流，早期饱腹感，慢性喉咙痛，腹痛，腹部腹胀，恶心，酸胃，腹泻，便秘，细菌感染，难治性溃疡，NSAIDs引起的胃肠道疾病，Barrett食管，由类固醇引起的胃肠道疾病，胃肠道疾病引起通过胆碱能化合物以及胃肠道中的真菌或病毒诱导的溃疡，通过向有需要的患者施用治疗有效量的至少一种质子泵。本发明还提供了与胃食管反流病（GERD）相关的症状的需求缓解，并且通过给予治疗有效量的至少一种质子泵抑制剂来缓解由消耗过量食物和/或酒精引起的症状有需要的患者。本发明还提供了通过向有需要的患者施用治疗有效量的至少一种质子泵抑制剂来提供治疗寄生虫感染如疟疾的方法。

4. 发明申请

WO2006127024A1 REAGENTS AND METHODS FOR LABELING TERMINAL OLEFINS 审中-公开
标题翻译：用于标记终端油脂的试剂和方法
公开(公告)号：WO2006127024A1
公开(公告)日：2006-11-30
申请号：PCT/US2005/030669
申请日：2005-08-29
申请人： EISAI CO. LTD. , HORSTMANN, Thomas, E. , LEWIS, Bryan, M.
发明人： HORSTMANN, Thomas, E. , LEWIS, Bryan, M.
IPC分类号： C07C11/02 , A61K51/00 , C07B59/00 , C07D493/22
CPC分类号： C07D407/14 , A61K51/0421 , A61K51/0453 , C07B59/00 , C07D493/22
摘要： In one aspect, the present invention provides a method for labeling a terminal olefin, the method comprising a step of treating a terminal olefin substrate having the structure: Formula (I); with a labeled ethylene reagent in the presence of a suitable catalyst under suitable olefin metathesis reaction conditions to form a labeled terminal olefin having the structure: Formula (II) wherein R A and R B are independently hydrogen, or an aliphatic, alicyclic, heteroaliphatic, heterocyclic, aryl or heteroaryl moiety, with the proviso that R A and R B are not each hydrogen, or R A and R B taken together with the carbon atom to which they are attached form an alicyclic or heterocyclic moiety; and in Formula (II), * denotes the presence of an isotopic label on the terminal carbon atom.
摘要翻译：一方面，本发明提供一种用于标记末端烯烃的方法，该方法包括处理具有以下结构的末端烯烃基材的步骤：式（I）; 在合适的烯烃复分解反应条件下，在合适的催化剂存在下用标记的乙烯试剂形成具有以下结构的标记的末端烯烃：式（II）其中R A和R B均为 SUP>独立地是氢或脂族，脂环族，杂脂族，杂环，芳基或杂芳基部分，条件是R A和R B不是每个氢，或与它们所连接的碳原子一起形成脂环族或杂环部分的R A和R B连接; 在式（II）中，*表示在末端碳原子上存在同位素标记。

5. 发明申请

WO2005069000A2 METHODS OF IDENTIFYING CYTOTOXIC EFFECTS IN QUIESCENT CELLS 审中-公开
标题翻译：鉴定细胞中细胞毒性作用的方法
公开(公告)号：WO2005069000A2
公开(公告)日：2005-07-28
申请号：PCT/US2005/001471
申请日：2005-01-13
申请人： EISAI CO. LTD. , LITTLEFIELD, Bruce, A. , SALVATO, Kathleen, A. , RUDOLPH-OWEN, Laura
发明人： LITTLEFIELD, Bruce, A. , SALVATO, Kathleen, A. , RUDOLPH-OWEN, Laura
IPC分类号： G01N33/50
CPC分类号： G01N33/5014
摘要： The present invention provides a system for measuring the cytotoxicity of a test compound against quiescent cells. The inventive methods and reagents may also be used to determine whether a compound, such as a chemotherapeutic agent, will have undesired toxicity toward normal tissues, which generally do not include a significant number of cells that are proliferating. Thus, the assay of the invention can be used to identify in vitro compounds that demonstrate a good therapeutic index, thus, accelerating the development of drugs that are clinically useful.
摘要翻译：本发明提供了一种用于测量测试化合物对静止细胞的细胞毒性的系统。本发明的方法和试剂也可用于确定化合物，例如化学治疗剂，对正常组织是否具有不希望的毒性，通常不包括大量增殖的细胞。因此，本发明的测定可以用于鉴定表现出良好治疗指数的体外化合物，从而加速临床有用的药物的开发。

6. 发明申请

WO2005030794A3 HEMIASTERLIN DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：WO2005030794A3
公开(公告)日：2005-04-07
申请号：PCT/US2004/030921
申请日：2004-09-22
申请人： EISAI CO. LTD. , KOWALCZYK, James, J. , KUZNETSOV, Galina , SCHILLER, Shawn , SELETSKY, Boris, M. , SPYVEE, Mark , YANG, Hu , CAMPAGNA, Silvio, A. , FANG, Francis, G.
发明人： KOWALCZYK, James, J. , KUZNETSOV, Galina , SCHILLER, Shawn , SELETSKY, Boris, M. , SPYVEE, Mark , YANG, Hu , CAMPAGNA, Silvio, A. , FANG, Francis, G.
IPC分类号： C07K5/00
摘要： The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R 1 -R 7 , X 1 , X 2 , R, Q, and n are as defined herein.

7. 发明申请

WO2003059898A2 EPONEMYCIN AND EPOXOMICIN ANALOGS AND USES THEREOF 审中-公开
标题翻译： EPONEMYCIN和EPOXOMICIN类似物及其用途
公开(公告)号：WO2003059898A2
公开(公告)日：2003-07-24
申请号：PCT/US2003/000390
申请日：2003-01-08
申请人： EISAI CO. LTD. , AGOULNIK, Sergei , AKASAKA, Kozo , FANG, Frank , HARMANGE, Jean-Christophe , HAWKINS, Lynn , JIANG, Yimin , JOHANNES, Charles , LI, Xiang-Yi , MCGUINNESS, Pamela , MURPHY, Erin , SCHILLER, Shawn , VERMEULEN, Mary , WU, Jiayi
发明人： AGOULNIK, Sergei , AKASAKA, Kozo , FANG, Frank , HARMANGE, Jean-Christophe , HAWKINS, Lynn , JIANG, Yimin , JOHANNES, Charles , LI, Xiang-Yi , MCGUINNESS, Pamela , MURPHY, Erin , SCHILLER, Shawn , VERMEULEN, Mary , WU, Jiayi
IPC分类号： C07D303/36
CPC分类号： C07D209/48 , A61K38/00 , C07D303/36 , C07D405/12 , C07D407/12 , C07F5/025 , C07F9/65502 , C07K5/06139
摘要： The present invention provides compounds having formula (I) : wherein R 1 -R 6 , A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.
摘要翻译：本发明提供具有式（I）的化合物：其中R 1 -R 6，A，J，D，E，G，Q，w，x，y和z如本文中所述的一般和类别和亚类所述，其药物组合物及其用于治疗癌症和/或炎症性疾病的方法，更一般地，作为蛋白酶体抑制剂。

8. 发明申请

WO2006076100A2 TUBULIN ISOTYPE SCREENING IN CANCER THERAPY USING HALICHONDRIN B ANALOGS 审中-公开
标题翻译：使用HALICHONDRIN B模拟物的癌症治疗中的TUBULIN同位素筛选
公开(公告)号：WO2006076100A2
公开(公告)日：2006-07-20
申请号：PCT/US2005/044421
申请日：2005-12-07
申请人： EISAI CO. LTD. , AGOULNIK, Sergei , KUZNETSOV, Galina , LITTLEFIELD, Bruce, A.
发明人： AGOULNIK, Sergei , KUZNETSOV, Galina , LITTLEFIELD, Bruce, A.
IPC分类号： G01N33/574 , A61K31/353
CPC分类号： A61K31/353 , G01N33/5091 , G01N33/574 , G01N33/57407 , G01N33/57496 , G01N2500/00 , Y10T436/143333
摘要： Chemotherapeutic agents that interfere with microtubule assembly or disassembly in the cell are potent inhibitors of cell replication. Examples of such agents include halichondrin B analogs. It has been shown that the susceptibility of certain cancers to analogs of halichondrin B correlates with the expression of particular tubulin isotypes or other microtubule-associated proteins such as MAP-4 and stathmin. Correlations such as these may be used in identifying patients suitable for treatment using a particular chemotherapeutic agent. Such a system avoids treating patients with cytotoxic compounds where there is a minimal or no effect on the cancer. The invention also provides a system of establishing these correlations for different compounds and cancer types. The system will be particularly useful in establishing correlations between anti-microtubule agents and cancers such as lung, breast, and ovarian cancer. Kits and reagents useful in practicing the invention are also provided.
摘要翻译：影响细胞中微管组装或分解的化学治疗剂是细胞复制的有效抑制剂。这些试剂的实例包括软骨素B类似物。已经显示某些癌症对软骨素B类似物的敏感性与特定的微管蛋白同种型或其它微管相关蛋白如MAP-4和stathmin的表达相关。诸如这些的相关性可以用于鉴定适合于使用特定化学治疗剂的治疗的患者。这样的系统避免了治疗患有细胞毒性化合物的患者，其中对癌症最小或没有影响。本发明还提供了一种为不同化合物和癌症类型建立这些相关性的系统。该系统将特别有用于建立抗微管剂和肺癌，乳腺癌和卵巢癌等癌症之间的相关性。还提供了可用于实践本发明的试剂盒和试剂。

9. 发明申请

WO2004078142A3 COMPOSITIONS AND METHODS FOR PREVENTING AND TREATING ENDOTOXIN-RELATED DISEASES AND CONDITIONS 审中-公开
公开(公告)号：WO2004078142A3
公开(公告)日：2004-09-16
申请号：PCT/US2004/006713
申请日：2004-03-05
申请人： EISAI CO. , LTD. , MCSHANE, James
发明人： MCSHANE, James
IPC分类号： C07D303/22
摘要： The invention provides pharmaceutical compositions for preventing and treating endotoxin-related diseases and conditions, as well as methods for making and using such compositions.

10. 发明申请

WO2003076424A1 MACROCYCLIC COMPOUNDS USEFUL AS PHARMACEUTICALS 审中-公开
标题翻译：大环化合物作为药物有用
公开(公告)号：WO2003076424A1
公开(公告)日：2003-09-18
申请号：PCT/US2003/007377
申请日：2003-03-07
申请人： EISAI CO. LTD. , BOIVIN, Roch , CHIBA, Kenichi , DAVIS, Heather, A. , DIEPITRO, Lucian , DU, Hong , EGUCHI, Yoshihito , FUJITA, Masanori , GILBERT, Sandra , GOTO, Masaki , HARMANGE, Jean, Christophe , INOUE, Atsushi , JIANG, Yimin , KAWADA, Megumi , KAWAI, Takatoshi , KAWAKAMI, Yoshiyuki , KIMURA, Akifumi , KOTAKE, Makoto , KUBOI, Yoshikazu , LEMELIN, Charles , LI, Xiang-Yi , MATSUSHIMA, Tomohiro , MIZUI, Yoshiharu , SAKURAI, Hideki , SCHILLER, Shawn , SHEN, Yongchun , SPYVEE, Mark , TANAKA, Isao , WANG, Yuan , YAMAMOTO, Satoshi , YONEDA, Naoki , KOBAYASHI, Seiichi
发明人： BOIVIN, Roch , CHIBA, Kenichi , DAVIS, Heather, A. , DIEPITRO, Lucian , DU, Hong , EGUCHI, Yoshihito , FUJITA, Masanori , GILBERT, Sandra , GOTO, Masaki , HARMANGE, Jean, Christophe , INOUE, Atsushi , JIANG, Yimin , KAWADA, Megumi , KAWAI, Takatoshi , KAWAKAMI, Yoshiyuki , KIMURA, Akifumi , KOTAKE, Makoto , KUBOI, Yoshikazu , LEMELIN, Charles , LI, Xiang-Yi , MATSUSHIMA, Tomohiro , MIZUI, Yoshiharu , SAKURAI, Hideki , SCHILLER, Shawn , SHEN, Yongchun , SPYVEE, Mark , TANAKA, Isao , WANG, Yuan , YAMAMOTO, Satoshi , YONEDA, Naoki , KOBAYASHI, Seiichi
IPC分类号： C07D313/00
CPC分类号： C07D405/12 , A61K31/335 , A61K31/36 , A61K31/395 , C07D231/12 , C07D233/56 , C07D249/08 , C07D313/00 , C07D401/12 , C07D491/04 , C07D491/044 , C07D493/04 , Y02A50/411
摘要： The present invention provides compounds having formula (I), and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R 1 -R 11 , t, X, Y, Z, and n are as defined herein.
摘要翻译：本发明提供具有式（I）的化合物，另外提供其合成方法及其用于治疗各种疾病（包括炎性或自身免疫性疾病）以及涉及恶性或增加血管发生的疾病的方法，其中R1-R1， t，X，Y，Z和n如本文所定义。

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