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1. 发明申请

WO2003084303A2 ANTAGONISTS OF RF-AMIDE NEUROPEPTIDES 审中-公开
标题翻译： RF酰胺神经病毒的拮抗剂
公开(公告)号：WO2003084303A2
公开(公告)日：2003-10-16
申请号：PCT/US2003/008820
申请日：2003-03-24
申请人： UNIVERSITY OF FLORIDA , PROKAI, Laszlo
发明人： PROKAI, Laszlo
IPC分类号： C07C311/39
CPC分类号： C07C311/39
摘要： Disclosed are compounds having the formula: (I) where (II). Dashed lines: optional; conformational constraint by (CH 2 ) n , n=1-3, R’ =H or O(=) as well as pharmaceuticals compositions and methods for the treatment of opiate addiction, opiate dependence, opiate tolerance, opiate related abstinence syndrome, nicotine addiction and obesity based thereon.
摘要翻译：公开了具有下式的化合物：（I）其中（II）。虚线：可选; （CH 2）n，n = 1-3，R'= H或O（=）的构象约束以及用于治疗阿片成瘾，阿片依赖性，阿片剂耐受性，鸦片相关禁欲综合征，尼古丁成瘾的药物组合物和方法和基于此的肥胖。

2. 发明申请

WO2006122237A2 IMAGING OF NEURAL AND ORGAN INJURY OR DAMAGE 审中-公开
标题翻译：神经损伤或损伤成像
公开(公告)号：WO2006122237A2
公开(公告)日：2006-11-16
申请号：PCT/US2006/018222
申请日：2006-05-11
申请人： UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC. , WANG, Kevin, Ka-Wang , HAYES, Ronald, L. , BAXTER, Lewis, R. , PROKAI, Laszlo
发明人： WANG, Kevin, Ka-Wang , HAYES, Ronald, L. , BAXTER, Lewis, R. , PROKAI, Laszlo
IPC分类号： A61K51/00
CPC分类号： A61K51/04 , A61K51/08 , A61K51/088
摘要： In vivo determination of regional damage with neural and organ injury specific imaging agents. Rapid, and non-invasive imaging compositions and methods for assessment of the extent of neurotoxic cell loss or nervous system damage resulting from nervous system injury due to ischemia, stroke, trauma, chemical or electrical insult, acute drug overdose or exposure to substance abuse (such as "recreational drugs") infection or other insults. The same or similar rapid, and non-invasive imaging compositions and methods for assessment of the extent of the organ injury comprises any damage;, injury or infection, functional failure to specific organs such as liver, kidney, prostate, lung, skeletal muscle, heart, pancreas, stomach, small and large intestine, bladder and the reproductive system as well as damage, injury or infection, functional failure to multi-organs, trauma-hemorrhagic shock and sepsis, hi particular, neural and organ damage is detected via protease inhibitor-based radionuclide- labeled imaging ligand binding to overactivated proteases (calpains, caspases, cathepsins, proteasome, metalloproteases, granzyme B or other proteases) that are specific to neural or organ injury or damage.
摘要翻译：体内

3. 发明申请

WO2006039456A1 ISOTOPE LABELED DINITROPHENYLHYDRAZINES AND METHODS FOR USE 审中-公开
标题翻译：同位素标记的DINITROPHENYLHYDRAZINES和使用方法
公开(公告)号：WO2006039456A1
公开(公告)日：2006-04-13
申请号：PCT/US2005/035131
申请日：2005-09-29
申请人： UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC. , UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE CENTER AT FORT WORTH , PROKAI, Laszlo , FORSTER, Michael, J.
发明人： PROKAI, Laszlo , FORSTER, Michael, J.
IPC分类号： G01N33/60
CPC分类号： G01N33/60 , Y10T436/143333
摘要： The subject invention provides novel isotope-labeled dinitrophenylhydrazines (DNPHs) and methods for their use in detecting and/or quantifying carbonyl groups in proteins and other analytes. In particular, the present invention provides novel methods for identifying biomarkers of oxidative stress, which can be used to either forecast or detect diseases and/or conditions associated with oxidative stress. In one embodiment of the invention, isotope-labeled DNPHs are derived from [ 13 C 6 ]chlorobenzene.
摘要翻译：本发明提供新型同位素标记的二硝基苯肼（DNPH）及其用于检测和/或定量蛋白质和其它分析物中的羰基的方法。特别地，本发明提供用于鉴定氧化应激生物标志物的新方法，其可用于预测或检测与氧化应激相关的疾病和/或病症。在本发明的一个实施方案中，同位素标记的DNPH衍生自[13 C 6 C]氯苯。

4. 发明申请

WO2006034370A2 SYSTEMS AND METHODS FOR EVALUATING ENZYME COMPETENCY 审中-公开
标题翻译：用于评估酶能力的系统和方法
公开(公告)号：WO2006034370A2
公开(公告)日：2006-03-30
申请号：PCT/US2005033883
申请日：2005-09-20
申请人： UNIV FLORIDA , MELKER RICHARD J , MOREY TIMOTHY E , PROKAI LASZLO , DENNIS DONN M
发明人： MELKER RICHARD J , MOREY TIMOTHY E , PROKAI LASZLO , DENNIS DONN M
IPC分类号： C12Q1/26 , C12Q1/00
CPC分类号： C12Q1/00 , C12Q1/26
摘要： The present invention provides systems and methods for determining enzymatic competency, which is important in determining whether a patient may suffer an adverse drug reaction, has a disease associated with defects in specific enzymatic function, and/or has an enzyme defect that is likely to cause pathophysiology. As contemplated herein, a parent molecular entity is administered to a patient in whom enzymatic competency is to be determined. A sample of the patient's bodily fluid is exposed to a sensor of the invention to distinguish, detect, and quantify a detectable entity in the bodily fluid. Sensor-acquired data regarding the detectable entity is used to determine enzymatic competency. Preferably, a sample of a patient's exhaled breath is collected and exposed to the sensor of the invention. Types of sensor systems of the invention include, but are not limited to, surface resonance arrays; microelectromechanical sensors (such as microcantilever-based technology); molecularly imprinted polymer sensors; amplifying fluorescent sensor technology; aptamer-based sensor technology; SAW sensors; infrared sensors; fuel cells; chemical reactors; and pH sensitive sensors.
摘要翻译：本发明提供了用于确定酶能力的系统和方法，其在确定患者是否可能遭受不良药物反应，具有与特定酶功能缺陷相关的疾病和/或具有可能引起酶缺陷的酶缺陷病理生理学。如本文所考虑的，母体分子实体被施用于待确定酶促能力的患者。将患者体液的样本暴露于本发明的传感器以区分，检测和量化体液中的可检测实体。使用传感器获取的关于可检测实体的数据来确定酶促能力。优选地，患者呼出气的样本被收集并暴露于本发明的传感器。本发明的传感器系统的类型包括但不限于表面共振阵列; 微机电传感器（如基于微悬臂梁的技术）; 分子印迹聚合物传感器; 放大荧光传感器技术; 基于适配子的传感器技术; 声表面波传感器; 红外传感器; 燃料电池; 化学反应器; 和pH敏感传感器。

5. 发明申请

WO2005027912A1 STEROIDAL QUINOLS AND THEIR USE FOR ESTROGEN REPLACEMENT THERAPY 审中-公开
标题翻译： STEROIDAL QUINOLS及其用于ESTROGEN替代治疗的用途
公开(公告)号：WO2005027912A1
公开(公告)日：2005-03-31
申请号：PCT/US2004/030242
申请日：2004-09-15
申请人： UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC. , UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE CENTER AT FORT WORTH , PROKAI, Laszlo , PROKAI, Katalin , SIMPKINS, James, W.
发明人： PROKAI, Laszlo , PROKAI, Katalin , SIMPKINS, James, W.
IPC分类号： A61K31/565
CPC分类号： A61K31/56 , A61K31/565 , A61K31/566 , A61K31/567 , A61K31/58
摘要： The present invention relates to novel estrogen-related steroidal quinols and their use as drugs for estrogen replacement therapy. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved distribution into tissues, bone, in the cardiovascular system, and in the CNS (central nervous system) with only a slight estrogenic action or no estrogenic action in the uterus. The compounds are suitable for the production of pharmaceutical agents for use in numerous indications (for example, estrogen replacement therapy, prevention and treatment of osteoporosis).
摘要翻译：本发明涉及新型雌激素相关甾体喹啉及其用作雌激素替代疗法的药物。本发明的喹啉提供了改善的物理化学性质，增加的生物利用度，并且改善了分布到组织，骨骼，心血管系统和CNS（中枢神经系统）中，仅具有轻微的雌激素作用或在子宫内无雌激素作用。该化合物适用于生产用于多种适应症（例如，雌激素替代疗法，预防和治疗骨质疏松症）的药剂。

6. 发明申请

WO2004069248A1 PRODRUGS FOR USE A OPHTHALMIC AGENTS 审中-公开
标题翻译： PRODRUGS使用眼科药剂
公开(公告)号：WO2004069248A1
公开(公告)日：2004-08-19
申请号：PCT/US2003/038987
申请日：2003-12-09
申请人： UNIVERSITY OF FLORIDA , UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE CENTER , PROKAI, Laszlo , PROKAI, Katalin , SIMPKINS, James , AGARWAL, Neeraj
发明人： PROKAI, Laszlo , PROKAI, Katalin , SIMPKINS, James , AGARWAL, Neeraj
IPC分类号： A61K31/47
CPC分类号： A61K31/566 , A61K31/565 , C07J1/0059
摘要： The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcorneal penetration and are readily reduced into parent phenolic A-ring steroid compounds to provide protection or treatment against various ocular symptoms and disorders. The compounds according to the subject invention appear to be highly advantageous as prodrugs to provide protection and/or treatment against ocular disorders. These prodrugs confer lipid solubility optimal for transocorneal penetration and are readily converted to endogenous reducing agents into active phenolic A-ring steroid compounds. To the extent that these prodrugs have reduced feminizing effects and systemic toxicity, they would be expected to be quite advantageous for protecting or treating the eye against ocular disorders such as cataract or glaucoma without undesired (systemic) side effects).
摘要翻译：本发明提供了一种使甾体喹啉化合物赋予有益的眼科效果的机制。本发明化合物具有用于经角膜穿透的亲脂亲水平衡，并且易于还原成亲本酚A型类固醇化合物以提供针对各种眼部症状和障碍的保护或治疗。根据本发明的化合物似乎是非常有利的作为前药以提供对眼部疾病的保护和/或治疗。这些前药赋予了对于经角膜穿透最佳的脂质溶解性，并且容易地转化成内源性还原剂成活性酚A型类固醇化合物。在这些前药具有降低的女性化作用和全身毒性的程度上，预期它们对于保护或治疗眼睛免于眼部疾病如白内障或青光眼而没有不期望（全身）副作用）是非常有利的。

7. 发明申请

WO2003089459A2 THYROTROPIN-RELEASING HORMONE ANALOGUES AND THEIR THERAPEUTIC APPLICATIONS 审中-公开
标题翻译：甲状腺激素释放激素类似物及其治疗应用
公开(公告)号：WO2003089459A2
公开(公告)日：2003-10-30
申请号：PCT/US2003/012223
申请日：2003-04-21
申请人： UNIVERSITY OF FLORIDA , PROKAI, Laszlo
发明人： PROKAI, Laszlo
IPC分类号： C07K5/06
CPC分类号： C07K5/0821 , C07K5/06139
摘要： The present invention relates to novel metabolically stable and centrally active TRH analogues and prodrug forms of these analogues, wherein a functional portion of TRH is substituted with a pyridinium moiety or an ester moiety. Methods of synthesis and use of the TRH analogues and associated prodrugs are also provided.
摘要翻译：本发明涉及这些类似物的新型代谢稳定和中枢活性TRH类似物和前药形式，其中TRH的功能部分被吡啶鎓部分或酯部分取代。还提供了合成和使用TRH类似物和相关前体药物的方法。

8. 发明申请

WO2010057203A2 HDL PARTICLES FOR DELIVERY OF NUCLEIC ACIDS 审中-公开
标题翻译：用于输送核酸的HDL颗粒
公开(公告)号：WO2010057203A2
公开(公告)日：2010-05-20
申请号：PCT/US2009/064834
申请日：2009-11-17
申请人： THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM , SOOD, Anil, K. , LACKO, Andras, G. , LOPEZ-BERESTEIN, Gabriel , MANGALA, Lingegowda, S. , MCCONATHY, Walter, J. , PROKAI, Laszlo , NAIR, Maya, P. , UNT HEALTH SCIENCE CENTER AT FORT WORTH , TEXAS TECH UNIVERSITY SYSTEM
发明人： SOOD, Anil, K. , LACKO, Andras, G. , LOPEZ-BERESTEIN, Gabriel , MANGALA, Lingegowda, S. , MCCONATHY, Walter, J. , PROKAI, Laszlo , NAIR, Maya, P.
IPC分类号： C07K14/775 , C07H21/00 , A61P35/00
CPC分类号： C07K14/775 , A61K47/6911 , A61K48/0041 , C12N15/111 , C12N15/88 , C12N2320/32
摘要： Disclosed are high density lipoprotein-nucleic acid particles, wherein the particles include (a) an apolipoprotein; (b) a nucleic acid component comprising a therapeutic nucleic acid segment; and (c) a polypeptide comprising a positively charged region, wherein the positively-charged region of the polypeptide associates with the nucleic acid component. Also disclosed are pharmaceutical compositions that include a) an apolipoprotein; (b) a nucleic acid component comprising a therapeutic nucleic acid segment; and (c) a polypeptide comprising a positively charged region. Methods that concern the particles and pharmaceutical compositions of the present invention are also set forth, as well as kits.
摘要翻译：公开了高密度脂蛋白 - 核酸颗粒，其中颗粒包括（a）载脂蛋白; （b）包含治疗性核酸片段的核酸组分; 和（c）包含带正电荷区域的多肽，其中所述多肽的带正电区域与核酸组分结合。还公开了药物组合物，其包括a）载脂蛋白; （b）包含治疗性核酸片段的核酸组分; 和（c）包含带正电荷区域的多肽。还阐述了涉及本发明的颗粒和药物组合物的方法以及试剂盒。

9. 发明申请

WO2006122237A3 IMAGING OF NEURAL AND ORGAN INJURY OR DAMAGE 审中-公开
标题翻译：神经损伤或损伤成像
公开(公告)号：WO2006122237A3
公开(公告)日：2009-04-09
申请号：PCT/US2006018222
申请日：2006-05-11
申请人： UNIV FLORIDA , WANG KEVIN KA-WANG , HAYES RONALD L , BAXTER LEWIS R , PROKAI LASZLO
发明人： WANG KEVIN KA-WANG , HAYES RONALD L , BAXTER LEWIS R , PROKAI LASZLO
IPC分类号： A61K49/00
CPC分类号： A61K51/04 , A61K51/08 , A61K51/088
摘要： In vivo determination of regional damage with neural and organ injury specific imaging agents. Rapid, and non-invasive imaging compositions and methods for assessment of the extent of neurotoxic cell loss or nervous system damage resulting from nervous system injury due to ischemia, stroke, trauma, chemical or electrical insult, acute drug overdose or exposure to substance abuse (such as "recreational drugs") infection or other insults. The same or similar rapid, and non-invasive imaging compositions and methods for assessment of the extent of the organ injury comprises any damage;, injury or infection, functional failure to specific organs such as liver, kidney, prostate, lung, skeletal muscle, heart, pancreas, stomach, small and large intestine, bladder and the reproductive system as well as damage, injury or infection, functional failure to multi-organs, trauma-hemorrhagic shock and sepsis, hi particular, neural and organ damage is detected via protease inhibitor-based radionuclide- labeled imaging ligand binding to overactivated proteases (calpains, caspases, cathepsins, proteasome, metalloproteases, granzyme B or other proteases) that are specific to neural or organ injury or damage.
摘要翻译：用神经和器官损伤特异性成像剂进行体内区域损伤测定。用于评估由于缺血，中风，创伤，化学或电气侮辱，急性药物过量或暴露于药物滥用引起的神经系统损伤引起的神经毒性细胞损失或神经系统损伤的程度的快速和非侵入性成像组合物和方法（如“娱乐性药物”）感染或其他侮辱。用于评估器官损伤程度的相同或相似的快速和非侵入性成像组合物和方法包括任何损伤，损伤或感染，对特定器官如肝，肾，前列腺，肺，骨骼肌，心脏，胰腺，胃，小肠和大肠，膀胱和生殖系统以及损伤，损伤或感染，多器官功能衰竭，创伤性出血性休克和败血症。特别是通过蛋白酶检测神经和器官损伤基于抑制剂的放射性核素标记的成像配体与特异于神经或器官损伤或损伤的过度活化的蛋白酶（钙蛋白酶，半胱天冬酶，组织蛋白酶，蛋白酶体，金属蛋白酶，粒酶B或其他蛋白酶）结合。

10. 发明申请

WO2007103474A2 DRUG ADHERENCE MONITORING SYSTEM 审中-公开
标题翻译：药物辅助监测系统
公开(公告)号：WO2007103474A2
公开(公告)日：2007-09-13
申请号：PCT/US2007/005890
申请日：2007-03-07
申请人： UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC. , DENNIS, Donn, Michael , MELKER, Richard, J. , BOOTH, Matthew, M. , PROKAI, Laszlo
发明人： DENNIS, Donn, Michael , MELKER, Richard, J. , BOOTH, Matthew, M. , PROKAI, Laszlo
IPC分类号： A61K49/00 , G01N33/497
CPC分类号： A61B5/082 , A61B5/0022 , A61B5/0071 , A61B5/0075 , A61B5/14532 , A61B5/4839 , A61B5/746 , A61B2562/028 , A61K49/0002 , A61K49/0004
摘要： The present invention provides novel methods for monitoring subject adherence in taking prescribed drugs by detecting markers in exhaled breath after a subject takes the prescribed drug. In particular, the present invention provides novel methods for making additives that are combined with the drug(s). Upon biological breakdown of the drug/additive formulation in a subject's body, markers resulting directly from the biological breakdown of the additives are detected in exhaled breath using sensor technology. In certain embodiments of the invention, the drug adherence monitoring systems and methods include a reporting system capable of tracking subject compliance (either remotely or proximately) and of providing necessary alerts to the subject, caregiver, healthcare provider, and the like.
摘要翻译：本发明提供了在受试者服用规定的药物后通过检测呼出呼吸中的标记物来监测受试者依从性的新方法。特别地，本发明提供了制备与药物组合的添加剂的新方法。在受试者的身体中药物/添加剂制剂的生物分解时，直接由添加剂的生物分解产生的标记物使用传感器技术在呼气中检测。在本发明的某些实施方案中，药物依从性监测系统和方法包括能够跟踪受试者遵从性（远程或近似）并向对象，看护者，医疗保健提供者等提供必要的警报的报告系统。

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