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    • 2. 发明授权
    • Prodrugs for use as ophthalmic agents
    • 用作眼科剂的前药
    • US07186707B2
    • 2007-03-06
    • US10731528
    • 2003-12-09
    • Laszlo ProkaiKatalin ProkaiJames SimpkinsNeeraj Agarwal
    • Laszlo ProkaiKatalin ProkaiJames SimpkinsNeeraj Agarwal
    • A61K31/56C07J1/00
    • A61K31/57A61K31/56A61K31/58C07J1/00
    • 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).
    • 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为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。
    • 4. 发明授权
    • Prodrugs for use as ophthalmic agents
    • 用作眼科剂的前药
    • US07572781B2
    • 2009-08-11
    • US11706617
    • 2007-02-15
    • Laszlo ProkaiKatalin ProkaiJames SimpkinsNeeraj Agarwal
    • Laszlo ProkaiKatalin ProkaiJames SimpkinsNeeraj Agarwal
    • A61K31/56C07J1/00
    • A61K31/57A61K31/56A61K31/58C07J1/00
    • 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).
    • 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为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。
    • 5. 发明申请
    • Prodrugs for use as ophthalmic agents
    • 用作眼科剂的前药
    • US20070155711A1
    • 2007-07-05
    • US11706617
    • 2007-02-15
    • Laszlo ProkaiKatalin ProkaiJames SimpkinsNeeraj Agarwal
    • Laszlo ProkaiKatalin ProkaiJames SimpkinsNeeraj Agarwal
    • A61K31/57
    • A61K31/57A61K31/56A61K31/58C07J1/00
    • The subject invention provides a mechanism by which steroidal quinol compounds confer beneficial ophthalmic effects. The subject compounds possess a lipophilic-hydrophilic balance for transcomeal 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 transocomeal 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).
    • 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。 主题化合物具有亲和亲水平衡,用于转导穿透,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。 这些前体药物赋予脂质溶解度最佳用于经胚胎穿透,并且容易地转化为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。