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1. 发明申请

WO2012119265A1 NOVEL ESTERS OF 4,9-DIHYDROXY-NAPHTHO[2,3-b]FURANS FOR DISEASE THERAPIES 审中-公开
标题翻译： 4,9-二羟基萘并[2,3-b]氟虫病治疗疾病新药
公开(公告)号：WO2012119265A1
公开(公告)日：2012-09-13
申请号：PCT/CN2011/000357
申请日：2011-03-04
申请人： ZHOUSHAN HAIZHONGZHOU XINSHENG PHARMACEUTICALS CO., LTD. , JIANG, Zhiwei , WANG, Aijin , HU, Hongwei , XU, Jiali , HU, Yuesong , LI, Xian , YE, Yan , WANG, Jie , LI, Qinglong
发明人： JIANG, Zhiwei , WANG, Aijin , HU, Hongwei , XU, Jiali , HU, Yuesong , LI, Xian , YE, Yan , WANG, Jie , LI, Qinglong
IPC分类号： C07D307/92 , A61K31/343 , A61P3/04 , A61P3/10 , A61P3/00 , A61P25/28 , A61P35/00 , A61P43/00
CPC分类号： C07D307/92 , A61K31/343 , A61K31/665 , A61K45/06 , C07F9/65517
摘要： The present invention discloses esters of 4,9-dihydroxy-naphtho[2,3-b]furans and methods of making and using the same. The present invention also discloses conversion of the esters into therapeutically active 4,9-dihydroxy-naphtho[2,3-b]furans in vivo . The present invention furthermore discloses pharmaceutical compositions comprising the esters of 4,9- dihydroxy-naphtho[2,3-b]furans for the treatment of various indications including proliferative diseases.
摘要翻译：本发明公开了4,9-二羟基 - 萘并[2,3-b]呋喃的酯及其制备和使用方法。本发明还公开了在体内将酯转化为治疗活性的4,9-二羟基 - 萘并[2,3-b]呋喃。本发明还公开了包含4,9-二羟基 - 萘并[2,3-b]呋喃的酯的药物组合物，用于治疗各种适应症，包括增殖性疾病。

2. 发明申请

WO2012024818A1 NOVEL ANPHTHOQUINONES FOR DISEASE THERAPIES 审中-公开
标题翻译：用于疾病治疗的新型药物
公开(公告)号：WO2012024818A1
公开(公告)日：2012-03-01
申请号：PCT/CN2010/001288
申请日：2010-08-24
申请人： ZHOUSHAN HAIZHONGZHOU XINSHENG PHARMACEUTICALS CO., LTD. , JIANG, Zhiwei , WANG, Aijin , LI, Xian , LI, Qinglong , HU, Hongwei , XU, Jiali , HU, Yuesong , YE, Yan
发明人： JIANG, Zhiwei , WANG, Aijin , LI, Xian , LI, Qinglong , HU, Hongwei , XU, Jiali , HU, Yuesong , YE, Yan
IPC分类号： C07D307/92 , C07D333/74 , A61K31/343 , A61K31/381 , A61P35/00
CPC分类号： A61K31/343 , A61K45/06 , C07D307/92
摘要： Naphtho[2,3-b]furan-4,9-diones and naphtho[2,3-b]thiophene-4,9-diones, the preparation methods and uses thereof are disclosed. The pharmaceutical compositions comprising such compounds for the treatment of various indications including proliferative diseases are also disclosed.
摘要翻译：萘并[2,3-b]呋喃-4,9-二酮和萘并[2,3-b]噻吩-4,9-二酮，其制备方法和用途被公开。还公开了包含用于治疗包括增殖性疾病在内的各种适应症的化合物的药物组合物。

3. 发明申请

WO1996037506A1 METHOD OF TRITIUM LABELING OLIGONUCLEOTIDES 审中-公开
标题翻译：三角标记寡核苷酸的方法
公开(公告)号：WO1996037506A1
公开(公告)日：1996-11-28
申请号：PCT/US1996007304
申请日：1996-05-21
申请人： HYBRIDON, INC. , TAN, Weitian , IYER, Radhakrishnan, P. , JIANG, Zhiwei , YU, Dong , AGRAWAL, Sudhir
发明人： HYBRIDON, INC.
IPC分类号： C07H21/00
CPC分类号： A61K51/0491 , C07H21/00
摘要： The present invention comprises a novel method of incorporating a tritium label at one or more predetermined sites within an oligonucleotide. In particular, the method comprises contacting a nascent, support-bound oligonucleotide having a free 5' hydroxyl group with a suitable oxidizing agent to oxidize the alcohol to an aldehyde, followed by reducing the aldehyde thereby formed with a suitable tritium-labeled reducing agent such as [ H]NaBH4 to yield the 5' terminal alcohol with a 5' tritium label. Normal automated synthesis can then be continued to yield the oligonucleotide of desired length having the tritium label in the desired location. The oligonucleotides thereby produced have higher specific activity than those previously known in the art. Accordingly, in a second aspect, the present invention provides oligonucleotides having high specific activity. The oligonucleotides of the present invention are useful for determining the pharmacokinetics and biodistribution of their non-radiolabeled counterparts, both in vitro and in vivo.
摘要翻译：本发明包括在寡核苷酸内的一个或多个预定位点掺入氚标记的新方法。特别地，该方法包括将具有游离的5'羟基的新生支持结合的寡核苷酸与合适的氧化剂接触以将醇氧化成醛，然后用适当的氚标记的还原剂形成还原醛，作为[3 H] NaBH 4，得到具有5'氚标记的5'末端醇。然后可以继续进行正常的自动化合成，得到所需长度的寡核苷酸，其中所述氚标记位于所需位置。由此产生的寡核苷酸比本领域已知的寡核苷酸具有更高的比活性。因此，在第二方面，本发明提供具有高比活性的寡核苷酸。本发明的寡核苷酸可用于在体外和体内测定其非放射性标记的对应物的药代动力学和生物分布。

4. 发明申请

WO2018196003A1 MOTOR VENTILATION STRUCTURE AND MOTOR 审中-公开
公开(公告)号：WO2018196003A1
公开(公告)日：2018-11-01
申请号：PCT/CN2017/082616
申请日：2017-04-28
申请人： SIEMENS AKTIENGESELLSCHAFT , JIANG, Zhiwei
发明人： JIANG, Zhiwei
IPC分类号： H02K9/08 , F24F11/00 , H02K5/20 , F04D25/08 , F04D29/30
CPC分类号： H02K5/20 , H02K9/08
摘要： The motor ventilation structure (20) is disposed inside a housing (31) of the motor (30), and the motor (30) is provided with a drive end (301) and a non-drive end (302) opposite to the drive end. The motor ventilation structure (20) includes: a first air baffle (21), located on the drive end (301), where the first air baffle (21) is spaced from a side wall of the housing of the motor (30), so as to form an accommodation space (210) with the housing (31); a ventilation pipe (22), fixed on the first air baffle (21), where the ventilation pipe (22) extends from the non-drive end (302) of the motor (30) to the drive end (301) of the motor (30) and is in communication with the accommodation space (210); and a double-suction fan (23), fixedly sleeved on a rotation shaft (32) of the motor (30) and disposed on one side, close to the non-drive end (302), of the first air baffle (21), where the double-suction fan (23) is configured to extract air from the non-drive end (302) to the drive end (301), and extract air in the accommodation space (210) and air for axial-radial cooling out of the housing (31) of the motor (30). The motor ventilation structure (20) and the motor (30) may ensure that a bearing of the drive end of the motor (30) has an appropriate temperature, and may achieve relatively high heat dissipation efficiency.

5. 发明申请

WO2004045557A3 NOVEL LAPACHONE COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：新型LAPACHONE化合物及其使用方法
公开(公告)号：WO2004045557A3
公开(公告)日：2004-08-12
申请号：PCT/US0337219
申请日：2003-11-18
申请人： ARQULE INC , JIANG ZHIWEI , REDDY DASHARATHA , ACKERMAN SAMUEL K , SALVESEN JUNE
发明人： JIANG ZHIWEI , REDDY DASHARATHA , ACKERMAN SAMUEL K , SALVESEN JUNE
IPC分类号： A61K20060101 , A61K31/38 , A61K31/382 , A61K31/385 , C07D307/92 , C07D311/92 , C07D327/06 , C07D333/74 , C07D335/08 , C07D335/10
CPC分类号： C07D335/08 , C07D307/92 , C07D311/92 , C07D327/06 , C07D333/74
摘要： The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of psoriasis or cancer or precancerous conditions.
摘要翻译：本发明提供了拉帕酮类似物和衍生物及其使用方法。这些化合物可以用于治疗或预防细胞增殖障碍的药物组合物中。这些化合物也可用于治疗或预防牛皮癣或癌症或癌前病症。

6. 发明申请

WO03011224A3 PHARMACEUTICAL COMPOSITIONS CONTAINING BETA-LAPACHONE, OR DERIVATIVES OR ANALOGS THEREOF, AND METHODS OF USING SAME 审中-公开
标题翻译：含有BETA-LAPACHONE或衍生物或其类似物的药物组合物及其使用方法
公开(公告)号：WO03011224A3
公开(公告)日：2003-05-08
申请号：PCT/US0224262
申请日：2002-07-31
申请人： CYCLIS PHARMACEUTICALS INC , JIANG ZHIWEI , REDDY DASHARATHA G
发明人： JIANG ZHIWEI , REDDY DASHARATHA G
IPC分类号： C07D311/78 , A61K9/08 , A61K9/19 , A61K31/337 , A61K31/352 , A61K47/10 , A61K47/24 , A61K47/30 , A61K47/32 , A61K47/34 , A61K47/40 , A61K47/44 , A61P17/06 , A61P35/00 , A61K31/35 , A61K31/335
CPC分类号： A61K9/0019 , A61K31/337 , A61K31/352 , A61K47/10 , A61K47/24 , A61K47/32 , Y10S514/937 , Y10S514/941 , Y10S514/97 , A61K2300/00
摘要： Beta-lapachone, which is poorly soluble in most pharmaceutically acceptable solvents, has demonstrated significant antineoplastic activity against human cancer lines. The present invention overcomes this significant limitation by teaching novel pharmaceutical compositions comprising a therapeutically effective amount of Beta-lapachone, or a derivative or analog thereof, and a pharmaceutically acceptable solubilizing carrier molecule, which may be at water-solubilizing carrier molecule such as hydroxypropyl- beta -cyclodextrin, or an oil-based solubilizing carrier molecule, for enhancing the solubility of Beta-lapachone in aqueous solution. The therapeutically effective amount of Beta-lapachone, or a derivative or analog thereof, may be complexed with the pharmaceutically acceptable solubilizing carrier molecule in aqueous solution. The novel pharmaceutical compositions may be administered with a second anticancer agent or in combination with radiation therapy. A formulation of Beta-lapachone or a derivative or analog thereof, complexed with a pharmaceutically acceptable solubilizing carrier molecule, wherein the complex can be freeze-dried and when subsequently reconstituted in aqueous solution is substantially soluble is also disclosed. Emulsions of Beta-Lapachone in a pharmaceutically acceptable fat emulsion vehicle are also provided. Also disclosed are methods for treating cancer by administering to a patient the novel pharmaceutical compositions and formulations. Pharmaceutical kits are also provided.
摘要翻译：在大多数药学上可接受的溶剂中溶解性差的β-吡拉酮已经证明对人类癌细胞系具有显着的抗肿瘤活性。本发明通过教导新颖的药物组合物来克服这个显着的限制，该药物组合物包含治疗有效量的β-吡拉酮或其衍生物或类似物，以及药学上可接受的增溶载体分子，其可以在水溶性载体分子例如羟丙基 - β-环糊精或油基增溶载体分子，用于提高β-萘酮在水溶液中的溶解度。 β-吡拉酮或其衍生物或类似物的治疗有效量可与药学上可接受的增溶载体分子在水溶液中络合。新型药物组合物可以与第二抗癌剂一起施用或与放射治疗组合施用。与药学上可接受的增溶载体分子络合的β-拉帕酮或其衍生物或类似物的制剂，其中所述复合物可以冷冻干燥，并且当随后在水溶液中重构时基本上可溶。还提供了在药学上可接受的脂肪乳剂中的β-拉帕酮的乳液。还公开了通过向患者施用新的药物组合物和制剂来治疗癌症的方法。还提供药物包。

7. 发明申请

WO02059103A9 SYNTHESIS OF BETA-LAPACHONE AND ITS INTERMEDIATES 审中-公开
标题翻译： BETA-LAPACHONE及其中间体的合成
公开(公告)号：WO02059103A9
公开(公告)日：2003-01-03
申请号：PCT/US0202359
申请日：2002-01-23
申请人： CYCLIS PHARMACEUTICALS INC , JIANG ZHIWEI , HOGELAND JANE
发明人： JIANG ZHIWEI , HOGELAND JANE
IPC分类号： C07D311/92 , C07B61/00 , C07D311/78 , C07D311/72
CPC分类号： C07D311/78
摘要： A novel process for synthesizing beta -lapachone (beta-lapachone), an agent that has demonstrated significant antineoplastic activity against human cancer lines. The process comprises the conversion of starting material, 2-hydroxy-1,4-naphothoquinone into beta -lapachone intermediate, lapachol. The lapachol is then converted to beta -lapachone by treatment with sulfuric acid and purified by recrystallization from ethanol. This novel process is extremely simple and provides beta -lapachone in excellent quality and high yield.
摘要翻译： β-拉帕酮（β-lapachone）的合成新方法，该试验已显示出对人类癌细胞系具有显着的抗肿瘤活性。该方法包括将起始物质2-羟基-1,4-辛氧基醌转化为β-Lapapone中间体，Lapanhol。然后通过用硫酸处理将皮肤胆固醇转化成β-papone，并通过乙醇重结晶纯化。这种新颖的方法非常简单，提供了优质和高产量的β-lapachone。

8. 发明申请

WO2013166618A1 PRODRUGS OF 4,9-DIHYDROXY-NAPHTHO[2,3-b]FURANS FOR CIRCUMVENTING CANCER MULTIDRUG RESISTANCE 审中-公开
标题翻译： 4,9-二羟基萘并[2,3-b]呋喃类抗癌多药耐药性的研究进展
公开(公告)号：WO2013166618A1
公开(公告)日：2013-11-14
申请号：PCT/CN2012/000618
申请日：2012-05-08
申请人： ZHOUSHAN HAIZHONGZHOU XINSHENG PHARMACEUTICALS CO., LTD. , JIANG, Zhiwei , HU, Yuesong , WANG, Jie , YE, Yan , LI, Xian , XU, Hairong , YANG, Huanhuan , FU, Yaner
发明人： JIANG, Zhiwei , HU, Yuesong , WANG, Jie , YE, Yan , LI, Xian , XU, Hairong , YANG, Huanhuan , FU, Yaner
IPC分类号： C07D307/92 , A61K31/343 , A61P35/00
CPC分类号： A61K31/343
摘要： The present invention discloses use of prodrug of 4,9-dihydroxy-naphtho[2,3-b]furan derivative for circumventing cancer multidrug resistance. The present invention also discloses use of prodrug of 4,9-dihydroxy-naphtho[2,3-b]furan derivative for the treatment of various types of cancers exhibiting multidrug resistance phenomenon. The present invention further discloses use of the pharmaceutically acceptable composition comprising prodrug of 4,9- dihydroxy-naphtho[2,3-b]furan derivative and method of using said composition in the treatment of various types of cancers exhibiting multidrug resistance phenomenon.
摘要翻译：本发明公开了4,9-二羟基 - 萘并[2,3-b]呋喃衍生物的前药用于避免癌症多药耐药性。本发明还公开了4,9-二羟基 - 萘并[2,3-b]呋喃衍生物的前药用于治疗表现出多药耐药现象的各种类型的癌症。本发明还公开了包含4,9-二羟基 - 萘并[2,3-b]呋喃衍生物的前药的药学上可接受的组合物的用途和使用该组合物治疗表现出多药耐药现象的各种类型的癌症的方法。

9. 发明申请

WO2013120229A1 METHOD FOR PREPARING AQUEOUS MANO PARTICLE SUSPENSIONS OF DERIVATIVES OF 4,9-DIHYDROXY-NAPHTHO[2,3-b]FURAN ALIPHATIC ACID ESTERS 审中-公开
标题翻译：制备4,9-二羟基 - 萘并[2,3-b]呋喃二酸酯衍生物的水溶性颗粒悬浮液的方法
公开(公告)号：WO2013120229A1
公开(公告)日：2013-08-22
申请号：PCT/CN2012/000190
申请日：2012-02-17
申请人： ZHOUSHAN HAIZHONGZHOU XINSHENG PHARMACEUTICALS CO., LTD. , JIANG, Zhiwei , LI, Xian , XU, Hairong , YE, Yan , HU, Hongwei , YANG, Huanhuan
发明人： JIANG, Zhiwei , LI, Xian , XU, Hairong , YE, Yan , HU, Hongwei , YANG, Huanhuan
IPC分类号： A61K31/343 , A61K9/10 , A61J3/00 , C07D307/92 , A61P3/04 , A61P3/10 , A61P3/00 , A61P25/28 , A61P35/00 , A61P43/00
CPC分类号： A61K9/10 , A61K9/1075 , A61K9/5146 , A61K31/343 , C07D307/92
摘要： Disclosed is a method for preparing aqueous nanoparticle suspensions of derivatives of 4,9-dihydroxy-naphtho[2,3-b]furan aliphatic acid esters. The compositions and the uses of the aqueous nanoparticle suspensions prepared according to the method as described herein are also disclosed.
摘要翻译：公开了一种制备4,9-二羟基 - 萘并[2,3-b]呋喃脂肪酸酯衍生物的水性纳米颗粒悬浮液的方法。还公开了根据本文所述的方法制备的纳米颗粒水悬浮液的组合物和用途。

10. 发明申请

WO2009036059A3 NOVEL STAT3 PATHWAY INHIBITORS AND CANCER STEM CELL INHIBITORS 审中-公开
公开(公告)号：WO2009036059A3
公开(公告)日：2009-03-19
申请号：PCT/US2008/075848
申请日：2008-09-10
申请人： BOSTON BIOMEDICAL, INC. , JIANG, Zhiwei , LI, Chiang, Jia , LI, Wei , LEGGETT, David
发明人： JIANG, Zhiwei , LI, Chiang, Jia , LI, Wei , LEGGETT, David
IPC分类号： A61K31/505 , A61K31/55 , A61K38/17
摘要： The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrent Stat3 pathway activity; to pharmaceutical compositions containing such compounds.

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