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    • 1. 发明公开
      EP2054384A4 POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF ARYL- AND HETEROARYLPROPIONIC ACIDS WITH VERY FAST SKIN PENETRATION RATE 无效 转让
    • POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF ARYL- AND HETEROARYLPROPIONIC ACIDS WITH VERY FAST SKIN PENETRATION RATE
    • 带正电荷的芳基的水溶性前药和HETEROARYLPROPIONSÄUREN具有非常快HAUTDURCHDRINGUNGSRATE
    • EP2054384A4
    • 2010-11-03
    • EP06795662
    • 2006-08-15
    • TECHFIELDS BIOCHEM CO LTD , YU CHONGXI
    • YU CHONGXI , XU LINA
    • C07D209/12 , C07D209/82 , C07D263/57 , C07D491/04
    • C07D333/22 , C07D209/08 , C07D209/46 , C07D209/88 , C07D263/57 , C07D333/32 , C07D491/04
    • The novel positively charged pro-drugs of aryl- and heteroarylpropionic acids in the general formula (1) 'Structure 1' and general formula (2) 'Structure 2' were designed and synthesized. The compounds of the general formula (1) 'Structure 1' and general formula (2) 'Structure 2' indicated above can be prepared from functional derivatives of naproxen, suprofen, a- methyl-(p-chlorobenzoyl)-5-methoxy-2-methylindole 3-acetic acid, flurbiprofen, carprofen, pranoprofen, benoxaprofen, alminoprofen, tiaprofenic acid, pirprofen, zaltoprofen, bermoprofen, loxoprofen, indoprofen, fenclorac, oxaprozin, fenbufen, orpanoxin, ketorolac, clidanac, and related compounds, (for example acid halides or mixed anhydrides), by reaction with suitable alcohols, thiols, or amines. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs, but also bonds to the negative charge on the phosphate head group of membranes and pushes the pro-drug into the cytosol. The results suggest that the pro-drugs diffuses through human skin -100-130 times faster than do their parent drugs. It takes 2-4 hours for naproxen, suprofen, a- methyl-(p-chlorobenzoyl)-5-methoxy-2-methylindole 3-acetic acid, flurbiprofen, carprofen, pranoprofen, benoxaprofen, alminoprofen, tiaprofenic acid, pirprofen, zaltoprofen, bermoprofen, loxoprofen, indoprofen, fenclorac, oxaprozin, fenbufen, orpanoxin, ketorolac, clidanac, and related compounds to reach the peak plasma level when they are taken orally, but these prodrugs only took about 40-50 minutes to reach the peak plasma level when they are taken transdermally. In plasma, more than 90% of these pro-drugs can change back to the drug in a few minutes. The prodrugs can be used medicinally in treating any NS AIAs-treatable conditions in humans or animals. The prodrugs can be administered not only orally, but also transdermally for any kind of medical treatments and avoid most of the side effects of NSAIAs, most notably GI disturbances such as dyspepsia, gastroduodenal bleeding, gastric ulcerations, and gastritis. Controlled transdermal administration systems of the prodrugs enable naproxen, suprofen, a- methyl-(p-chlorobenzoyl)-5-methoxy-2-methylindole 3-acetic acid, flurbiprofen, carprofen, pranoprofen, benoxaprofen, alminoprofen, tiaprofenic acid, pirprofen, zaltoprofen, bermoprofen, loxoprofen, indoprofen, fenclorac, oxaprozin, fenbufen, orpanoxin, ketorolac, clidanac, and related compounds to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of NSAIAs. Another great benefit of transdermal administration of these pro-drugs is that administering medication, especially to children, will be much easier.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 4. 发明公开
      EP2061749A4 POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF ACETAMINOPHEN AND RELATED COMPOUNDS WITH VERY FAST SKIN PENETRATION RATE 失效 转让
    • POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF ACETAMINOPHEN AND RELATED COMPOUNDS WITH VERY FAST SKIN PENETRATION RATE
    • 正面装，对乙酰氨基酚及相关化合物的水溶性前体药物具有非常高的皮肤渗透速率
    • EP2061749A4
    • 2010-12-29
    • EP06795894
    • 2006-09-03
    • TECHFIELDS BIOCHEM CO LTD , YU CHONGXI
    • YU CHONGXI , XU LINA
    • C07C233/25 , A61K31/167 , A61K31/22 , A61P11/06 , A61P17/00 , A61P27/06 , A61P27/16 , A61P29/00 , A61P35/00
    • C07C233/25
    • The novel positively charged pro-drugs of acetaminophen, acetaminosalol, and related compounds in the general formula (1) 'Structure 1' were designed and synthesized. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs, but also bonds to the negative charge on the phosphate head group of membranes and pushes the pro-drug into the cytosol. The results suggest that the pro-drugs diffuses through human skin ˆ¼150 times faster than does acetaminophen, acetaminosalol, and related compounds. It takes 1-2 hours for acetaminophen and acetaminosalol, and related compounds to reach the peak plasma level when they are taken orally, but these prodrugs only took about ˆ¼50 minutes to reach the peak plasma level when they are taken transdermally. In plasma, more than 90% of these pro-drugs can be changed back to the parent drugs in a few minutes. The prodrugs can be used medicinally for treating any NSAIAs-treatable conditions in humans or animals. The prodrugs can be administered not only orally, but also transdermally for any kind of medical treatments and avoid most of the side effects of NSAIAs. Controlled transdermal administration systems of the prodrugs enables acetaminophen, acetaminosalol, and related compounds to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of acetaminophen, acetaminosalol, and related compounds. Another great benefit of transdermal administration of these pro-drugs is that administering medication, especially to children, will be much easier.
    • 新颖的带正电荷的对乙酰氨基酚，acetaminosalol，和相关化合物的前体药物的通式（1）“结构1”，设计并合成英寸 毕业论文前药带正电荷的氨基不仅大大增加了药物的溶解度，因此而债券对磷酸头基膜的负电荷和推动有利于药物进入细胞质。 结果表明确实亲药物通过人体皮肤弥漫性比确实对乙酰氨基酚，acetaminosalol和相关化合物更快¼150倍。 这需要1-2个小时对乙酰氨基酚和acetaminosalol，和相关的化合物达到峰值血浆水平的时候都采取口头，但只有论文的前药大约过了¼50分钟达到峰值血浆水平时，他们采取了皮。 在血浆中，90％以上的合成前体药物可以在几分钟内被改回母体药物。 前体药物可入药用于治疗人或动物的任何NSAIAs可治疗的条件。 前体药物不仅可以口服，但如此透皮任何形式的药物治疗和避免大多数的NSAIAs的副作用。 前药的控制透皮给药系统允许对乙酰氨基酚，acetaminosalol，对乙酰氨基酚和相关化合物以达到最佳不断治疗血液水平，以增加效率和减少的，acetaminosalol副作用，和相关化合物。 毕业论文的前体药物透皮给药的另一大好处是没有管理的药物，尤其是爱孩子，会容易得多。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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