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1. 发明申请

WO1996040245A1 IMPROVED DELIVERY OF DIAGNOSTIC AND THERAPEUTIC AGENTS TO A TARGET SITE 审中-公开
标题翻译：改进诊断和治疗药物到目标网站
公开(公告)号：WO1996040245A1
公开(公告)日：1996-12-19
申请号：PCT/US1996008696
申请日：1996-06-07
申请人： IMMUNOMEDICS, INC.
发明人： IMMUNOMEDICS, INC. , GRIFFITHS, Gary, L. , HANSEN, Hans, J. , GOVINDAN, Serengulam
IPC分类号： A61K39/395
CPC分类号： B82Y5/00 , A61K41/0095 , A61K47/665 , A61K47/6893 , A61K47/6897 , A61K47/6898 , A61K49/0017 , A61K51/1078 , A61K51/1093 , A61K2121/00 , A61K2123/00 , G01N33/531 , G01N33/534 , G01N33/574 , G01N33/686 , Y10S424/90
摘要： An in vivo method for delivering a diagnostic or therapeutic agent to a target site in a mammal, wherein a targeting species including a targeting moiety and a diagnostic or therapeutic agent or a binding site for a subsequently administered diagnostic or therapeutic agent conjugate, the targeting moiety having a primary binding site whereby it specifically binds to the target, is administered and allowed to accrete at the target site, is improved by injecting into the circulatory system of the mammal a clearing agent that binds to the primary binding site of the targeting species, whereby non-localized primary targeting species is cleared from circulation. The method is especially useful in pretargeting methods because the clearing agent does not remove the primary targeting species or block secondary binding sites of the primary targeting species.
摘要翻译：用于将诊断或治疗剂递送至哺乳动物的靶位点的体内方法，其中包括靶向部分和诊断或治疗剂的靶向物质或用于随后施用的诊断或治疗剂缀合物的结合位点靶向部分通过向哺乳动物的循环系统注射与靶向物种的主要结合位点结合的结合剂，改善其具有与靶标特异性结合的主要结合位点，并且允许其在目标位点被吸收，从而非局部化的主要靶向物质从循环中清除。该方法在预靶向方法中特别有用，因为清除剂不除去主要靶向物种的主要靶向物种或阻断二级结合位点。

2. 发明申请

WO1995006053A1 TRIS(SUBSTITUTED PHENYL)BISMUTH DERIVATIVE 审中-公开
标题翻译： TRIS（取代苯乙烯）双酚衍生物
公开(公告)号：WO1995006053A1
公开(公告)日：1995-03-02
申请号：PCT/JP1994001381
申请日：1994-08-22
申请人： NISSAN CHEMICAL INDUSTRIES, LTD. , SUZUKI, Hitomi , MAEDA, Kouichi , TANIKAWA, Keizo , MIYAJI, Katsuaki
发明人： NISSAN CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07F09/94
CPC分类号： A61K49/04 , C07F9/94 , Y10S424/90
摘要： A tris(substituted phenyl)bismuth derivative represented by general formula (I) and, if any, a pharmaceutically acceptable salt thereof, wherein X represents Y -NR R [wherein Y represents -SO2- or -C(=O)-; and R and R represent each independently hydrogen, C1-C4 alkyl or A-Z (wherein A represents alkylene which has 2-6 carbon atoms in total and may have a branch having at least two carbon atoms, and Z represents OR (wherein R represents SiR R R (wherein R , R and R represent each independently C1-C4 alkyl or phenyl), hydrogen or C1-C4 alkyl) or NR R (wherein R and R represent each independently hydrogen or C1-C4 alkyl)), provided the case where R and R are both hydrogen atoms is excepted], -O-CHR -OR (wherein R represents C1-C4 alkyl, and R is as defined above) or Y -A-Z [wherein Y represents O, -S(O)n- (wherein n represents an integer of 0 or 2) or -NR - (wherein R is as defined above), and A and Z are each as defined above]; and X and X represent each independently hydrogen or any substituent defined above with respect to X . This compound has an excellent performance as a radio-logical contrast medium and is useful as an X-ray contrast medium for injecting into a blood vessel, urinary tract, and so forth.
摘要翻译：由通式（I）表示的三（取代的苯基）铋衍生物和（如果有的话）其药学上可接受的盐，其中X 1表示Y 1 -NR 1 R 2 [其中Y 1 >表示-SO 2 - 或-C（= O） - ; 并且R 1和R 2各自独立地表示氢，C 1 -C 4烷基或AZ（其中A表示总共具有2-6个碳原子并且可具有至少两个碳原子的支链的亚烷基，Z表示 OR 3（其中R 3表示SiR 4 R 5 R 6（其中R 4，R 5和R 6各自独立地为C 1 -C 4烷基或苯基），氢或C 1 -C 4烷基）或NR 7 R 8（其中R 7和R 8各自独立地表示氢或C 1 -C 4烷基）），条件是其中R 1和R 2， 2>均为氢原子除外]，-O-CHR 7 -OR 9（其中R 9表示C 1 -C 4烷基，R 7如上定义）或Y 2 - AZ [其中Y 2表示O，-S（O）n - （其中n表示0或2的整数）或-NR 1 - （其中R 1如上所定义），A和 Z各自如上所定义）; X 2和X 3各自独立地表示氢或相对于X 1定义的任何取代基。该化合物作为无线电逻辑造影剂具有优异的性能，并且可用作用于注射到血管，尿道等中的X射线造影剂。

3. 发明申请

WO1994020147A1 SMALL ANIMAL METASTASIS MODEL 审中-公开
标题翻译：小动物地质模型
公开(公告)号：WO1994020147A1
公开(公告)日：1994-09-15
申请号：PCT/US1994000714
申请日：1994-01-18
申请人： SYSTEMIX, INC.
发明人： SYSTEMIX, INC. , NAMIKAWA, Reiko , KYOIZUMI, Seishi , SHTIVELMAN, Emilya , McCUNE, Joseph, M.
IPC分类号： A61K49/00
CPC分类号： A01K67/0271 , A61K49/0008 , Y10S424/90
摘要： A method for initiating metastasis of human tumor cells under experimental conditions is provided. Immunocompromised non-human mammals having a viable, xenogeneic organ or tissue are used as a host for human tumor cells. The cells are introduced into the chimeric animal after the solid tissue is implanted and are then able to grow and metastasize as they would in situ. Therapeutic regimens may be evaluated in this system to determine efficacy against metastatic processes.
摘要翻译：提供了一种在实验条件下启动人肿瘤细胞转移的方法。具有活的异种器官或组织的免疫受损的非人哺乳动物用作人肿瘤细胞的宿主。在植入固体组织后，将细胞导入嵌合动物体内，然后能像原位一样生长和转移。可以在该系统中评估治疗方案以确定对转移过程的功效。

4. 发明申请

WO2003034803A2 METHODS FOR DETERMINING TOXICITY REVERSING AGENTS 审中-公开
标题翻译：确定毒性反转剂的方法
公开(公告)号：WO2003034803A2
公开(公告)日：2003-05-01
申请号：PCT/IB2002/005160
申请日：2002-10-18
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , SHIVE, Gwyn , PETTIT, Flora, H.
发明人： PETTIT, Flora, H.
IPC分类号： G01N33/50
CPC分类号： G01N33/5008 , G01N33/5014 , G01N33/5047 , G01N33/5088 , Y10S424/90
摘要： Disclosed are methods for assessment of the ability of substances to ameliorate the toxic-effects of compounds based on a lymphocyte culture assay. The lymphocyte assay is a repeatable and quantitative assay for lymphocyte growth in a chemically defined media in which specific compounds with potential toxicity and substances with potential abilities to ameliorate the toxicity can be added to determine specific and individualized requirements for such substances. Also disclosed are methods for ameliorating side-effects by administering to a patient undergoing therapy with a drug that has a toxic-effect, a substance identified by the methods of the invention. Further provided is a composition that ameliorates the toxic-effect of the statin family of drugs. Methods and processes for partially purifying and/or isolating this composition are also provided. Thus, the methods of the invention not only provide substances for reversal of compound-toxicity but also provide methods for pre-approving compounds for human use.
摘要翻译：公开了用于评估物质基于淋巴细胞培养测定法来改善化合物的毒性作用的能力的方法。淋巴细胞测定是化学上确定的培养基中的淋巴细胞生长的可重复和定量测定法，其中可以加入具有潜在毒性的具体化合物和具有改善毒性的潜在能力的物质以确定这些物质的具体和个性化的要求。还公开了通过给具有毒性作用的药物进行治疗的患者给药以及通过本发明的方法鉴定的物质来改善副作用的方法。还提供了改善他汀类药物家族的毒性作用的组合物。还提供了用于部分纯化和/或分离该组合物的方法和方法。因此，本发明的方法不仅提供用于逆转化合物毒性的物质，而且还提供了用于人们使用的预认合化合物的方法。

5. 发明申请

WO1995033494A1 EMULSIONS OF PARAMAGNETIC CONTRAST AGENTS FOR MAGNETIC RESONANCE IMAGING (MRI), CONTAINING AN ORGANIC CHELATOR HAVING AN UNSATURATED ALIPHATIC GROUP 审中-公开
标题翻译：用于磁共振成像（MRI）的参与对比剂的乳剂，含有不饱和脂肪组的有机教练
公开(公告)号：WO1995033494A1
公开(公告)日：1995-12-14
申请号：PCT/US1995006818
申请日：1995-05-31
申请人： HEMAGEN/PFC
发明人： HEMAGEN/PFC , CACHERIS, William, P. , KAUFMAN, Robert, J. , RICHARD, Thomas, J. , GRABIAK, Raymond, C.
IPC分类号： A61K49/00
CPC分类号： A61K49/1806 , Y10S424/90 , Y10S514/836 , Y10S514/938 , Y10T436/24
摘要： Emulsions of paramagnetic contrast agents and processes of making and using them are disclosed. The emulsions contain water, a dispersed oil phase and a complex of a paramagnetic metal ion and an organic chelator having a C10-C30 unsaturated aliphatic group. The emulsions are very stable and therapeutically acceptable for intravenous administration to enhance MRI.
摘要翻译：公开了顺磁造影剂的乳液及其制造和使用的方法。乳液含有水，分散油相和顺磁性金属离子与具有C10-C30不饱和脂族基团的有机螯合剂的络合物。对于静脉内施用，乳剂非常稳定和治疗上可接受以增强MRI。

6. 发明申请

WO03034803A8 METHODS FOR DETERMINING TOXICITY REVERSING AGENTS 审中-公开
标题翻译：确定毒性反转剂的方法
公开(公告)号：WO03034803A8
公开(公告)日：2003-11-27
申请号：PCT/IB0205160
申请日：2002-10-18
申请人： UNIV TEXAS , PETTIT FLORA H , SHIVE GWYN HF
发明人： SHIVE WILLIAM DI , PETTIT FLORA H
IPC分类号： G01N33/50 , C12Q1/02 , C12Q1/00
CPC分类号： G01N33/5008 , G01N33/5014 , G01N33/5047 , G01N33/5088 , Y10S424/90
摘要： Disclosed are methods for assessment of the ability of substances to ameliorate the toxic-effects of compounds based on a lymphocyte culture assay. The lymphocyte assay is a repeatable and quantitative assay for lymphocyte growth in a chemically defined media in which specific compounds with potential toxicity and substances with potential abilities to ameliorate the toxicity can be added to determine specific and individualized requirements for such substances. Also disclosed are methods for ameliorating side-effects by administering to a patient undergoing therapy with a drug that has a toxic-effect, a substance identified by the methods of the invention. Further provided is a composition that ameliorates the toxic-effect of the statin family of drugs. Methods and processes for partially purifying and/or isolating this composition are provided. Thus, the methods of the invention not only provide substances for reversal of compound-toxicity but also provide methods for pre-approving compounds for human use. Figure (1) illustrates lipitor toxicity.
摘要翻译：公开了用于评估物质基于淋巴细胞培养测定法来改善化合物的毒性作用的能力的方法。淋巴细胞测定是化学上确定的培养基中的淋巴细胞生长的可重复和定量测定法，其中可以加入具有潜在毒性的具体化合物和具有改善毒性的潜在能力的物质以确定这些物质的具体和个性化的要求。还公开了通过给具有毒性作用的药物进行治疗的患者给药以及通过本发明的方法鉴定的物质来改善副作用的方法。还提供了改善他汀类药物家族的毒性作用的组合物。提供了用于部分纯化和/或分离该组合物的方法和方法。因此，本发明的方法不仅提供用于逆转化合物毒性的物质，而且还提供了用于人们使用的预认合化合物的方法。图（1）说明了脂质毒性。

7. 发明申请

WO1996019487A1 ORGANOBISMUTH DERIVATIVES AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：有机原料衍生物及其生产方法
公开(公告)号：WO1996019487A1
公开(公告)日：1996-06-27
申请号：PCT/JP1995002551
申请日：1995-12-13
申请人： NISSAN CHEMICAL INDUSTRIES, LTD. , SUZUKI, Hitomi , TANIKAWA, Keizo , MIYAJI, Katsuaki , SUZUKI, Nobuhiro
发明人： NISSAN CHEMICAL INDUSTRIES, LTD.
IPC分类号： C07F09/94
CPC分类号： C07F9/94 , A61K49/04 , Y10S424/90
摘要： An organobismuth derivative represented by general formula (I), a salt thereof, and a contrast medium containing the same as the active ingredient: wherein, X represents Y NR R , wherein Y represents -SO2- or -C(O)-, R represents C3-6 alkyl having 2 to 5 hydroxyl groups, R represents hydrogen, C1-6 alkyl optionally having 1 to 5 hydroxyl groups or C1-5 acyl, or R and R together may form C2-6 cycloalkylene optionally having 1 to 4 hydroxyl groups; X and X each independently represent hydrogen, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylsulfonyl, C1-4 alkylcarbonyl, nitro or cyano, or has the same meaning as that of X ; and each of the above hydroxyl groups may be protected.
摘要翻译：一种由通式（I）表示的有机铋衍生物及其盐及含有其的活性成分的造影剂：其中X 1表示Y 1 NR 1 R 2，其中Y < 1表示-SO 2 - 或-C（O） - ，R 1表示具有2至5个羟基的C 3-6烷基，R 2表示氢，任选具有1至5个羟基的C 1-6烷基或C 1 -5酰基或R 1和R 2一起可以形成任选具有1至4个羟基的C 2-6亚环烷基; X 2和X 3各自独立地表示氢，C 1-4烷基，C 1-4烷氧基，C 1-4烷基磺酰基，C 1-4烷基羰基，硝基或氰基，或具有与X 1相同的含义。 ; 并且上述羟基中的每一个可以被保护。

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