摘要:
Disclosed are ursodeoxycholic acid derivatives having an increased solubility in water, and methods for producing the derivatives. To produce the derivatives, ursodeoxycholic acid is protected at its carboxyl group with a benzyl group, then reacted with tetrabenzyl-acetic acid-oxyglucoside of the following formula (1), and de-benzylated; or ursodeoxycholic acid is protected at its hydroxyl group with a t-butyldimethylsilyl group, then reacted with tetrabenzyl-2-hydroxyethyloxyglucoside of the following formula (2), and de-t-butyldimethylsilylated and de-benzylated. ##STR1##
摘要:
An object of the invention is to develop galactose or mannose derivatives of docetaxel, etc. having improved solubility and physiological activity, to alleviate burden imposed on patients and to provide effective therapeutic drug for tumors. The present invention provides taxoid derivatives comprising any of paclitaxel, docetaxel and 10-deacetyl-baccatin III to which galactose or mannose is linked through a spacer, and methods for producing taxoid derivatives comprising reacting paclitaxel, docetaxel or 10-deacetyl-baccatin III with tetrabenzyl acetyloxygalactoside or tetrabenzyl acetyloxymannoside, subjecting the product to debenzylation reaction, and optionally to detriethylsilylation reaction.
摘要:
The object of the invention is to develop baccatin derivatives useful for preparing taxoid compounds such as paclitaxel and a process for the producing the same. The invention provides baccatin derivatives represented by the general formula (I) as well as a process for producing baccatin derivatives represented by the general formula (I) above, which comprises allowing a baccatin represented by the general formula (II) to react with a &bgr;-ketoester in the absence of a catalyst or in the presence of a tin compound or an amine base, preferably under reduced pressure.
摘要:
A taxoid compound represented by general formula (I) ##STR1## where the symbols R.sup.1, R.sup.2, R.sup.3, R.sup.4, Bz, and Ac have specified meanings. Also, a method for producing the taxoid derivative from a baccatin derivative having a .beta.-ketoester group at the 13-position by transesterification and a method for producing taxoid compound such as paclitaxel from the taxoid derivative under mild condition are disclosed.
摘要:
A sugar derivative wherein a hydroxy-carboxylic acid is combined to a position 1 of a sugar via ether linkage, and other hydroxyl groups are protected with a protective groups. A method of producing the sugar derivative, comprises allowing glycolic ester to react with a compound so as to combine said glycolic ester at the position 1 of the sugar skeleton, and then saponifying, said compound has on the position 1 any of hydroxyl group, halogen atom and sulfur atom with a substitutent group, and has other hydroxyl groups being protected with a protective groups.
摘要:
A taxoid derivative wherein sugar is combined with any one of paclitaxel, docetaxel and 10-deacetyl-bacatin III via a spacer. A method of producing the taxoid derivative comprises protecting hydroxyl groups at specific position of paclitaxel or docetaxel by protective compound followed by reacting with tetrabenzyl acetyloxyglucoside, and then carrying out debenzyl and detriethylsilyl reactions. A method of producing the taxoid derivative comprises reacting paclitaxel or docetaxel with tetrabenzyl acetyloxyglucoside, and then carrying out debenzyl reaction.
摘要:
A coupling structure for a piston used in a fluid-pressure cylinder. The piston in the fluid-pressure cylinder includes a piston hole that runs through a central part of the piston in an axial direction thereof. One end of a piston rod and a coupling body coupled to the one end are inserted into the piston hole. The coupling body includes: a main part that contacts the one end of the piston rod; and an angled part formed around the main part and inclined at a prescribed angle with respect thereto. When the coupling body is subjected to pressure inside the piston hole, the diameter of the coupling body increases and a pointed edge of the angled part engages with an inner surface of the piston hole such that the coupling body couples the piston and the piston rod.
摘要:
Apparatus and method for image coding may group code units corresponding to an image based on a same at least one parameter of each of the code units. Each group of code units which is grouped includes code units of which values of the same at least one parameter are the same. In addition, the code units of each group of code units which is grouped are entropy coded in parallel.
摘要:
A die fabricated based on reference model data is corrected, and the corrected die is measured with a measuring instrument to provide three-dimensional measured die data. Noise areas in the three-dimensional measured die data are identified and removed using a computer. The three-dimensional measured die data and the model data are placed in proximity to each other, and a stacking and deforming process is performed in order to project a model surface represented by the model data onto a measured data surface represented by the three-dimensional measured die data. The stacking and deforming process is performed only within a range of the model surface that corresponds to an area in which the die is corrected. Portions of the three-dimensional measured die data from which noise areas have been removed are complemented by the model data.
摘要:
In an alignment conveyor apparatus including an input conveyor (1), an output conveyor (2) with a flap sensor (14), a single or a plurality of alignment conveyors (3), a product sensor (12), and a control unit (7), the control unit (7) includes an alignment conveyor controller (71) and an output conveyor controller (72), the alignment conveyor controller (71) includes a product position manager (712), a position correction calculator (713), and a position correction instruction creator (715), the output conveyor controller (72) includes an output conveyor position manager (721).