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1. 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。

2. 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。

3. 发明申请

WO2003084978A1 STEROIDAL QUINOLS AS PRODRUGS OF ANTIOXIDANTS 审中-公开
标题翻译： STEROIDAL QUINOLS作为抗氧化剂的产品
公开(公告)号：WO2003084978A1
公开(公告)日：2003-10-16
申请号：PCT/US2003/009983
申请日：2003-04-01
申请人： UNIVERSITY OF FLORIDA , PROKAI, Laszlo , PROKAI, Katalin , SIMPKINS, James
发明人： PROKAI, Laszlo , PROKAI, Katalin , SIMPKINS, James
IPC分类号： C07J1/00
CPC分类号： A61K31/56 , A61K31/58 , C07J1/00
摘要： The present invention relates to novel estrogen-related steroidal quinols and their use as prodrugs for phenolic estrogens and estrogen analogs. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved distribution into tissues and penetration across the blood-brain barrier when compared to phenolic estrogens and estrogen analogs. (Formula I).
摘要翻译：本发明涉及新型雌激素相关甾体喹啉及其作为酚类雌激素和雌激素类似物前药的用途。当与酚类雌激素和雌激素类似物相比时，本发明的喹啉提供了改善的物理化学性质，增加的生物利用度和改善的组织分布以及穿过血脑屏障的渗透。（式I）。

4. 发明公开

EP1569648A1 PRODRUGS FOR USE A OPHTHALMIC AGENTS 审中-公开
标题翻译：使用眼药的前药
公开(公告)号：EP1569648A1
公开(公告)日：2005-09-07
申请号：EP03796804.7
申请日：2003-12-09
申请人： University of Florida , THE UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE CENTER AT FORT WORTH
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：本发明提供了一种机制，通过该机制甾族喹啉化合物赋予有益的眼科效应。主题化合物具有用于角膜穿透的亲脂 - 亲水平衡并且容易地被还原成母体酚类A-环类固醇化合物以提供针对各种眼部症状和病症的保护或治疗。根据本发明的化合物看起来作为提供针对眼部疾病的保护和/或治疗的前药是非常有利的。这些前药赋予脂质溶解度最适合于经角神经穿透并且容易地转化为内源性还原剂成活性酚A环类固醇化合物。就这些前体药物具有降低的女性化作用和全身毒性而言，预计它们对于保护或治疗眼睛免受例如白内障或青光眼等眼部疾病而没有不希望的（全身性）副作用）是非常有利的。

5. 发明授权

EP1490392B1 STEROIDAL QUINOLS AS PRODRUGS OF ANTIOXIDANTS 有权
标题翻译：甾体对苯二酚作为抗氧化剂的前兆
公开(公告)号：EP1490392B1
公开(公告)日：2007-02-14
申请号：EP03721508.4
申请日：2003-04-01
申请人： University of Florida Research Foundation, Inc.
发明人： PROKAI, Laszlo , PROKAI, Katalin , SIMPKINS, James
IPC分类号： C07J1/00
CPC分类号： A61K31/56 , A61K31/58 , C07J1/00
摘要： The present invention relates to novel estrogen-related steroidal quinols and their use as prodrugs for phenolic estrogens and estrogen analogs. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved distribution into tissues and penetration across the blood-brain barrier when compared to phenolic estrogens and estrogen analogs. (Formula I).

6. 发明公开

EP1490392A1 STEROIDAL QUINOLS AS PRODRUGS OF ANTIOXIDANTS 有权
标题翻译：甾体对苯二酚作为抗氧化剂的前兆
公开(公告)号：EP1490392A1
公开(公告)日：2004-12-29
申请号：EP03721508.4
申请日：2003-04-01
申请人： UNIVERSITY OF FLORIDA
发明人： PROKAI, Laszlo , PROKAI, Katalin , SIMPKINS, James
IPC分类号： C07J1/00
CPC分类号： A61K31/56 , A61K31/58 , C07J1/00
摘要： The present invention relates to novel estrogen-related steroidal quinols and their use as prodrugs for phenolic estrogens and estrogen analogs. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved distribution into tissues and penetration across the blood-brain barrier when compared to phenolic estrogens and estrogen analogs. (Formula I).

7. 发明公开

EP1673093A1 USE OF STEROIDAL QUINOLS FOR ESTROGEN REPLACEMENT THERAPY 审中-公开
标题翻译：甾体quinols的是雌激素替代疗法
公开(公告)号：EP1673093A1
公开(公告)日：2006-06-28
申请号：EP04788770.8
申请日：2004-09-15
申请人： UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC. , University of North Texas
发明人： PROKAI, Laszlo , PROKAI, Katalin , SIMPKINS, James, W.
IPC分类号： A61K31/565 , A61K31/566 , A61K31/567 , A61P5/30
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).

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