Prodrug derivatives of acids using alcohols with homotopic hydroxy groups and methods for their preparation and use
申请人:deLong A. Mitchell
公开号:US20070254920A1
公开(公告)日:2007-11-01
This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula
wherein
is a biologically-active moiety comprising a carboxylic acid functional group, and R
b
is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof.
这项发明涉及新型同位素前药、药物以及其制备、测试和使用方法。在一个实施例中,同位素前药具有一般公式
其中
是包含羧酸官能团的生物活性基团,而 R
b
是通过羧酸官能团与生物活性基团形成酯键的同位对称醇,以及其光学异构体、对映异构体、药用可接受盐、生物水解酰胺、酯、亚酰胺及其组合物。
Ophthamological drugs
申请人:Toone J. Eric
公开号:US20060135609A1
公开(公告)日:2006-06-22
The present invention relates generally to ophthamological drugs. More specifically, the inventon relates to a method of modifying (derivatizing) ophthamological drugs so as to increase their penetration through the cornea. The invention also relates to drugs modified (derivatized) in accordance with the instant method and to the use of same in treating conditions associated with elevated intraocular pressure, particularly, glaucoma.
The invention relates to novel substituted thien-3-yl-sulphonylamino(thio)carbonyl-triazolin(ethi)ones of the general formula (I)
in which
Q
1
, Q
2
, R
1
, R
2
, R
3
and R
4
are each as defined in the description, and to salts of the compounds according to formula (I), to processes and to novel intermediates for their preparation and to their use as herbicides.
The present invention relates generally to ophthamological drugs. More specifically, the invention relates to a method of modifying (derivatizing) ophthamological drugs so as to increase their penetration through the cornea. The invention also relates to drugs modified (derivatized) in accordance with the instant method and to the use of same in treating conditions associated with elevated intraocular pressure, particularly, glaucoma.