Abstract: A bile acid derivative having carcinostatic activity represented by the following formula (1): ##STR1## wherein each of R.sub.1 and R.sub.2 is a hydrogen atom or a hydroxyl group, R.sub.3 is a hydroxyl group, benzyloxyl group or --NH--CH.sub.2n R.sub.5 (wherein R.sub.5 is a carboxyl group or sulfonyl group, and n represents the integer of 1 or 2), X is a halogen atom, R.sub.4 is a hydrogen atom or XCH.sub.2 CH.sub.2 --,.chi. is an .alpha.-bond, and .chi. is an .alpha.- or .beta.-bond is produced by the steps (a) and (b), the steps (a), (b) and (c), or the steps (a), (b), (c) and (d) described below:(a) causing an active carbonation reagent to react with a bile acid derivative wherein the carboxyl group is esterified;(b) causing an aminoalkylhalide to react with the active carbonated product obtained;(c) subjecting the bile acid derivative obtained in the above steps (a) and (b) to hydrolysis; and(d) causing the above hydrolyzate to react with an aminoalkyl derivative in the presence of a condensing agent.
Type:
Grant
Filed:
January 28, 1987
Date of Patent:
December 27, 1988
Assignee:
Wakunaga Seiyaku Kabushiki Kaisha
Inventors:
Shunsou Hatono, Akira Yazaki, Susumu Yoshida
Abstract: An oligonucleotide derivative having an amino group protected with an eliminatable group bonded through a phosphate group and a spacer with an appropriate length to the 5'-end of an oligonucleotide protected suitably at the 3'-hydroxyl group and the base moiety of the nucleotide, and an immobilized oligonucleotide derivative having a Sepharose carrier bonded to the amino group in place of said protective group are disclosed. Methods for production of these derivatives are also disclosed.
Abstract: [21-Leucine] human urogastrone, hUG, comprising a polypeptide represented by the specified amino acid sequence has been found to be equivalent to the known hUG which has 21-Met and is disclosed together with its syntheses. Double-stranded polydeoxyribonucleotides comprising a structural gene for expressing the hUG, a recombinant plasmid comprising a structural gene for expressing the hUG, and E. coli transformed by the recombinant plasmid are also disclosed. Thanks to the substitution of Met in the known hUG by Leu, the peptide of hUG can now be produced by a conventional or typical method in which a genetically engineered precursor fused polypeptide is cleaved by cyanogen bromide at Met in the fused polypeptide.
Abstract: An oligonucleotide derivative having an amino group protected with an eliminatable group bonded through a phosphate group and a spacer with an appropriate length to the 5'-end of an oligonucleotide protected suitably at the 3'-hydroxyl group and the base moiety of the nucleotide, and an immobilized oligonucleotide derivative having a Sepharose carrier bonded to the amino group in place of said protective group are disclosed. Methods for production of these derivatives are also disclosed.
Abstract: Biotin- or 2,4-dinitrophenyl-oligodeoxyribonucleotide derivatve represented by the formula shown below and its preparation method is disclosed: ##STR1## wherein: R is ##STR2## m and n are each 0 or a natural number; R.sup.1 is a straight or branched hydrocarbon residue; and B is a base constituting the nucleotide (in which when a plural number of B exist, they may be either identical or different). This compound is useful for use as a nonradioactive affinity probe for nucleic acid or a primer.