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141. 发明申请

WO2010036404A2 NOVEL RETINAMIDE RETINOIC ACID METABOLISM BLOCKING AGENTS 审中-公开
标题翻译：新型抗真菌酸代谢阻断剂
公开(公告)号：WO2010036404A2
公开(公告)日：2010-04-01
申请号：PCT/US2009/043109
申请日：2009-05-07
申请人： UNIVERSITY OF MARYLAND, BALTIMORE , NJAR, Vincent C. O. , GEDIYA, Lalji K. , KHANDELWAL, Aakanksha
发明人： NJAR, Vincent C. O. , GEDIYA, Lalji K. , KHANDELWAL, Aakanksha
IPC分类号： C07D233/60 , C07D487/12 , C07D233/56 , A61P35/00 , A61K31/4164
CPC分类号： C07D233/56 , A61K31/41 , A61K31/4164 , A61K31/4196 , A61K31/519 , A61K31/53 , C07D233/60 , C07D249/02 , C07D251/02 , C07D487/04
摘要： Retinoic acid metabolism blocking agents (RAMBAs). The RAMBAs may be used for treatment of cancer, including breast and prostate cancers. Methods for preparing novel retinamide RAMBAs. The methods include reacting RAMBAs with terminal polar carboxylic acid group with a variety of amines in the presence of suitable coupling reagents. The retinamide RAMBAs are potent inhibitors of the growth of prostate and breast cancer cells and may be useful for the treatment of these diseases in humans.
摘要翻译：视黄酸代谢阻断剂（RAMBA）。 RAMBAs可用于治疗癌症，包括乳腺癌和前列腺癌。新型视黄醛RAMBA的制备方法。所述方法包括在合适的偶联剂存在下使RAMBA与末端极性羧酸基团与多种胺反应。视网膜酰胺RAMBAs是前列腺和乳腺癌细胞生长的有效抑制剂，可用于治疗人类中的这些疾病。

142. 发明申请

WO2010033560A2 SUR1 INHIBITORS FOR THERAPY 审中-公开
标题翻译： SUR1治疗抑制剂
公开(公告)号：WO2010033560A2
公开(公告)日：2010-03-25
申请号：PCT/US2009/057111
申请日：2009-09-16
申请人： UNIVERSITY OF MARYLAND, BALTIMORE , SIMARD, J., Marc
发明人： SIMARD, J., Marc
IPC分类号： A61K31/17 , A61K31/415 , A61P9/10 , A61K48/00 , A61P29/00
CPC分类号： A61K31/17 , A61K31/415
摘要： Methods and compositions are provided that are utilized for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN). In particular, the methods and compositions are inhibitors of a particular NCca-ATP channel and include, for example, inhibitors of SUR1 and/or inhibitors of TRPM4. Kits for treatment and/or prevention of intraventricular hemorrhage or progressive hemorrhagic necrosis (PHN), particularly following spinal cord injury, are also provided. The present invention also concerns treatment and/or prevention of intraventricular hemorrhage in infants, including premature infants utilizing one or more inhibitors of the channel is provided to the infant, for example to brain cells of the infant.
摘要翻译：提供了用于治疗和/或预防脑室内出血或进行性出血性坏死（PHN）的方法和组合物。特别地，所述方法和组合物是特定NCca-ATP通道的抑制剂，并且包括例如SUR1抑制剂和/或TRPM4抑制剂。还提供了用于治疗和/或预防脑室内出血或进行性出血性坏死（PHN）的试剂盒，特别是脊髓损伤后。本发明还涉及婴儿的脑室内出血的治疗和/或预防，其中包括使用一种或多种通道抑制剂的早产儿，例如婴儿的脑细胞。

143. 发明申请

WO2010025259A1 METHOD OF TREATING ORGANOPHOSPHOROUS POISONING 审中-公开
标题翻译：治疗有机磷的方法
公开(公告)号：WO2010025259A1
公开(公告)日：2010-03-04
申请号：PCT/US2009/055208
申请日：2009-08-27
申请人： UNIVERSITY OF MARYLAND, BALTIMORE , THE GOVERNMENT OF THE UNITED STATES, AS REPRESENTED BY THE SECRETARY OF THE ARMY , ALBUQUERQUE, Edson X. , ADLER, Michael , PEREIRA, Edna F.R.
发明人： ALBUQUERQUE, Edson X. , ADLER, Michael , PEREIRA, Edna F.R.
IPC分类号： A01N43/46
CPC分类号： A61K31/55 , A61K31/46 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to various methods for treating organophosphorus poisoning in an animal that is at risk of exposure to an organophosphorus compound or preventing organophosphorus poisoning in an animal that has been exposed to an organophosphorus compound, by administering a therapeutically effective amount of galantamine or a salt thereof, or a biologically active analog, derivative, fragment or variant thereof.
摘要翻译：本发明涉及通过施用治疗有效量的加兰他敏或在治疗有效量的加兰他敏或其它有机磷化合物暴露于有机磷化合物的动物中，有机磷暴露于有机磷化合物或预防有机磷中毒的动物中治疗有机磷中毒的各种方法其盐或其生物活性的类似物，衍生物，片段或变体。

144. 发明申请

WO2010022089A2 DERIVATIVES OF APF AND METHODS OF USE 审中-公开
标题翻译： APF的衍生物和使用方法
公开(公告)号：WO2010022089A2
公开(公告)日：2010-02-25
申请号：PCT/US2009/054207
申请日：2009-08-18
申请人： UNIVERSITY OF MARYLAND, BALTIMORE , THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , KEAY, Susan, K. , SZEKELY, Zoltan , MICHEJDA, Maria , KACZMAREK, Piotr
发明人： KEAY, Susan, K. , SZEKELY, Zoltan , KACZMAREK, Piotr
IPC分类号： A61K38/14 , A61P35/00
CPC分类号： A61K38/14
摘要： Derivatives of bladder epithelial antiproliferative factor and methods of using them are disclosed. In specific embodiments, the glycopeptide compositions are useful for the treatment and/or prevention of medical conditions, including cancer. In other embodiments, there are compositions and methods related to treatment of bladder conditions. In particular embodiments, the glycopeptide comprises D-pipecolic acid or L-pipecolic acid.
摘要翻译：公开了膀胱上皮抗增生因子的衍生物及其使用方法。在具体实施方案中，糖肽组合物可用于治疗和/或预防包括癌症在内的医学病症。在其它实施方案中，存在与治疗膀胱状况相关的组合物和方法。在具体实施方案中，糖肽包含D-哌啶酸或L-哌啶酸。

145. 发明申请

WO2009155335A3 CONJUGATES OF 19F MR IMAGING TRACERS AND CHEMOTHERAPEUTIC AGENTS FOR DRUG QUANTIFICATION AND DRUG DOSE INDIVIDUALIZATION 审中-公开
公开(公告)号：WO2009155335A3
公开(公告)日：2009-12-23
申请号：PCT/US2009/047648
申请日：2009-06-17
申请人： UNIVERSITY OF MARYLAND, BALTIMORE , UNIVERSITY OF MARYLAND, COLLEGE PARK , YU, Yihua
发明人： YU, Yihua
IPC分类号： A61K49/06 , A61K31/513 , A61P35/00 , A61K47/48
摘要： A therapeutic agent formed of a magnetic resonance imaging tracer conjugated with a chemotherapeutic agent. The therapeutic agents can be used in measuring drug delivery to a target tissue. The therapeutic agents allow for therapeutic MRI, in which 19 F MRI techniques are used to detect, monitor, evaluate, and/or adjust chemotherapeutic drug dosage levels in a patient or a targeted tissue thereof.

146. 发明申请

WO2009149339A2 P53 ACTIVATOR PEPTIDES 审中-公开
公开(公告)号：WO2009149339A2
公开(公告)日：2009-12-10
申请号：PCT/US2009/046392
申请日：2009-06-05
申请人： UNIVERSITY OF MARYLAND, BALTIMORE , LU, Wuyuan , ZELLA, Davide , LIU, Min , LI, Changqing
发明人： LU, Wuyuan , ZELLA, Davide , LIU, Min , LI, Changqing
IPC分类号： C07K14/00 , C07K2/00 , C07K4/00 , C07K1/00 , C07K14/435 , C07K14/46 , C07K14/47
CPC分类号： C07K14/43522
摘要： The present invention relates to novel polypeptides that activate p53, and the polynucleotides encoding these p53 activator peptides. The present invention also relates to pharmaceutical compositions comprising the p53 activator peptides as well as methods of treating abnormal conditions, such as malignant tumors, with the methods comprising administering the pharmaceutical compositions of the present invention to a subject in need of treatment thereof.
摘要翻译：本发明涉及活化p53的新型多肽，以及编码这些p53活化肽的多核苷酸。本发明还涉及包含p53激活剂肽的药物组合物以及治疗异常病症如恶性肿瘤的方法，包括将本发明的药物组合物施用于需要治疗的受试者。

147. 发明申请

WO2009114658A3 ANDROGEN RECEPTOR INACTIVATION CONTRIBUTES TO ANTITUMOR EFFICACY OF CYP17 INHIBITORS IN PROSTATE CANCER 审中-公开
公开(公告)号：WO2009114658A3
公开(公告)日：2009-09-17
申请号：PCT/US2009/036891
申请日：2009-03-12
申请人： UNIVERSITY OF MARYLAND, BALTIMORE , NJAR, Vincent, C.O. , BRODIE, Angela
发明人： NJAR, Vincent, C.O. , BRODIE, Angela
IPC分类号： A61K31/568 , A61P35/00 , A61P15/00
摘要： Provided are methods of inhibiting CYP17 in a mammal, such as a human, that include administering an effective amount of at least one CYP17 inhibitor, such as VN/124-1, VN/125-1, VN/85-1, VN/87-1 and/or VN/108-1 to the mammal. Also provided are methods of down regulating androgen receptor (AR) protein expression and methods of antagonizing AR in a mammal that include administering to the mammal an effective amount of at least one active ingredient selected from VN/124-1, VN/125-1, VN/85-1, VN/87-1 and VN/108-1. Also provided are methods of treating prostate cancer and methods of suppressing or preventing prostate tumor growth by administering such compounds to a mammal.

148. 发明申请

WO2009064836A2 KYNURENINE-AMINOTRANSFERASE INHIBITORS 审中-公开
标题翻译：吉林 - 氨基转移酶抑制剂
公开(公告)号：WO2009064836A2
公开(公告)日：2009-05-22
申请号：PCT/US2008/083321
申请日：2008-11-13
申请人： UNIVERSITY OF MARYLAND, BALTIMORE , MITSUBISHI TANABE PHARMA CORPORATION , SCHWARCZ, Robert , KAJII, Yasushi , ONO, Shin-ichiro
发明人： SCHWARCZ, Robert , KAJII, Yasushi , ONO, Shin-ichiro
IPC分类号： C07D401/10
CPC分类号： C07D498/06 , C07D215/56 , C07D401/04
摘要： Compounds of formula (I) : prodrug derivatives and/or pharmaceutically acceptable salt thereof, selectively inhibit the enzyme kynurenine aminotransferase, thereby reducing the synthesis of kynurenic acid. The compounds are used for the treatment of psychiatric and neurological diseases which benefit from an increase in glutamatergic and/or cholinergic neurotransmission, such as schizophrenia, depression, bipolar illness, anxiety and Alzheimer's disease. Furthermore, the compounds of the invention are useful for stimulating attention, memory and other cognitive processes in normal individuals of any age, including children, adolescents and the elderly. Additionally, the compounds of the invention are also useful for treatment of patients suffering from malaria by preventing parasite gametogenesis and fertility based on reduction of xanthurenic acid formation from its bioprecursor 3 -hydroxy kynurenine.
摘要翻译：式（I）化合物：前药衍生物和/或其药学上可接受的盐，选择性地抑制犬尿氨酸转氨酶的酶，从而减少犬尿酸的合成。这些化合物用于治疗由谷氨酸能和/或胆碱能神经传递如精神分裂症，抑郁症，双相性疾病，焦虑和阿尔茨海默病的增加而受益的精神和神经疾病。此外，本发明的化合物可用于刺激任何年龄的正常个体，包括儿童，青少年和老年人的注意力，记忆力和其他认知过程。此外，本发明的化合物还可用于治疗患有疟疾的患者，其基于从其生物前体3-羟基犬尿苷中减少黄嘌呤酸形成，通过预防寄生虫配子形成和生育力。

149. 发明申请

WO2009045852A1 DETERMINATION OF SITE OF ORIGIN FOR A NATURAL ELECTRICAL PULSE IN A LIVING BODY 审中-公开
标题翻译：确定生命体内自然电脉冲原始位点
公开(公告)号：WO2009045852A1
公开(公告)日：2009-04-09
申请号：PCT/US2008/077708
申请日：2008-09-25
申请人： UNIVERSITY OF MARYLAND, BALTIMORE , SABA, Magdi M. , SHOROFSKY, Stephen R.
发明人： SABA, Magdi M. , SHOROFSKY, Stephen R.
IPC分类号： A61B5/0464 , A61B5/04
CPC分类号： A61B5/0464 , A61B5/04011
摘要： Techniques include determining a first vector of temporal changes in electrical data measured at multiple electrical sensors positioned at corresponding locations on a surface of a living body due to a natural electrical pulse. A different vector of temporal changes in electrical data measured at the same electrical sensors is determined due to each stimulated signal of multiple stimulated signals within the living body. Stimulated position data is received, which indicates a different corresponding position within the living body where each of the stimulated signals originates. The site of origin of the natural electrical pulse is determined based on the first vector and the multiple different vectors and the stimulated position data. Among other applications, these techniques allow the rapid, automatic determination of the site of origin of ventricular tachycardia arrhythmia (VT).
摘要翻译：技术包括确定由于自然电脉冲而在位于生物体表面上的相应位置处的多个电传感器处测量的电数据的时间变化的第一矢量。由于在活体内的多个受激信号的每个受激信号，确定在相同的电传感器处测量的电数据的时间变化的不同矢量。受刺激的位置数据被接收，其表示生物体内每个受激信号起源的不同对应位置。基于第一矢量和多个不同矢量以及受刺激的位置数据确定自然电脉冲的原点。在其他应用中，这些技术允许快速，自动确定室性心动过速心律失常（VT）的起源部位。

150. 发明申请

WO2009038729A2 COMPOSITIONS AND METHODS UTILIZING FIBRIN BETA CHAIN FRAGMENTS OF THE BBETA CHAIN OF FIBRINOGEN 审中-公开
标题翻译：使用FIBRINOGEN BBETA链的纤维素链片段的组合物和方法
公开(公告)号：WO2009038729A2
公开(公告)日：2009-03-26
申请号：PCT/US2008/010832
申请日：2008-09-17
申请人： RegeneRx Biopharmaceuticals, Inc. , University Of Maryland, Baltimore , MEDVED, Leonid , ZHANG, Li , YAKOVLEV, Sergiy , GOLDSTEIN, Allan L. , CROCKFORD, David
发明人： MEDVED, Leonid , ZHANG, Li , YAKOVLEV, Sergiy , GOLDSTEIN, Allan L. , CROCKFORD, David
IPC分类号： C12N9/68
CPC分类号： C07K14/75
摘要： A composition including a peptide sequence of the formula βX1-X2, the peptide sequence corresponding to an amino acid sequence of a fibrin beta chain fragment of a Bbeta chain of fibrinogen, wherein X1 represents an N-terminal end of the peptide sequence, and X2 represents a C-terminal end of the peptide sequence, wherein the peptide sequence includes additional amino acids between X1 and X2, wherein the peptide sequence may contain a non-naturally occurring amino acid residue, wherein the peptide sequence is other than a wild-type β15-42 monomer sequence per se, and wherein the peptide sequence is other than (β15-66) 2 dimer having two chains with each chain limited to wild type amino acids β15-65 and each chain further including a non-naturally occurring Gly at position 66 of each chain. Methods for treatment and pharmaceutical combinations may include a polypeptide agent such as Thymosin beta 4. In such methods and combinations, a dimer of the peptide sequence may include amino acids 15-66 of the fibrin beta chain.
摘要翻译：一种组合物，其包含式ßX1-X2的肽序列，所述肽序列对应于纤维蛋白原Bbeta链的纤维蛋白β链片段的氨基酸序列，其中X1表示肽序列的N末端，X2 表示肽序列的C-末端，其中所述肽序列包括X1和X2之间的另外的氨基酸，其中所述肽序列可以含有非天然存在的氨基酸残基，其中所述肽序列不是野生型 ß15-42单体序列本身，并且其中所述肽序列不同于具有两条链的（ß15-66）2二聚体，每条链限于野生型氨基酸ß15-65，并且每条链还包含非天然存在的Gly 每个链的位置66。用于治疗和药物组合的方法可以包括多肽试剂例如胸腺素β4。在这些方法和组合中，肽序列的二聚体可以包括纤维蛋白β链的氨基酸15-66。

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