DIAMINE CROSSLINKING AGENTS, CROSSLINKED ACIDIC POLYSACCHARIDES AND MEDICAL MATERIALS
申请人:Seikagaku Corporation
公开号:US20170001948A1
公开(公告)日:2017-01-05
The invention provides a diamine crosslinking agent for acidic polysaccharides consisting of a diamine compound having a primary amino group at both terminals and an ester or thioester bond in the molecule, wherein the number of atom in the linear chain between at least one of the amino groups and the carbonyl carbon in the ester or thioester is 1 to 5; in particular, a diamine crosslinking agent for acidic polysaccharides which is represented by the general formula (I) below:
[the symbols in the formula are as described in the specification]; a crosslinked acidic polysaccharide obtained by forming crosslinks by amide bonding between the amino groups in the diamine crosslinking agent and carboxyl groups in an acidic polysaccharide; and a medical material including the crosslinked product.
Novel quinolinecarboxylic acid derivatives, use thereof, antibacterial agent containing the same, process for preparing said compounds and intermediate compound
申请人:KANEBO LTD.
公开号:EP0472826A2
公开(公告)日:1992-03-04
Novel quinolinecarboxylic acid derivatives of the formula:
wherein Z is
in which R¹ is hydrogen atom, a halogen atom, hydroxy or a lower alkyloxy; R² is a halogen atom, hydroxy or a lower alkyloxy; R³ is a lower alkyl; and R⁴ is hydroxy or a di(lower alkyl)amino, and a pharmaceutically acceptable salt thereof, which have excellent antibacterial activities and are useful as an antibacterial agent, a pharmaceutical composition containing the same, and process for preparing the same. This invention relates also to the intermediate compound used for preparing the novel quinolinecarboxylic acid derivative.
式中的新型喹啉羧酸衍生物:
其中 Z 是
其中 R¹ 是氢原子、卤素原子、羟基或低级烷氧基;R² 是卤素原子、羟基或低级烷氧基;R³ 是低级烷基;R⁴ 是羟基或二(低级烷基)氨基,及其药学上可接受的盐;这些衍生物具有优异的抗菌活性,可用作抗菌剂,含有这些衍生物的药物组合物,以及制备这些衍生物的工艺。本发明还涉及用于制备新型喹啉羧酸衍生物的中间体化合物。
Diamine crosslinking agents, crosslinked acidic polysaccharides and medical materials
申请人:Seikagaku Corporation
公开号:US10919840B2
公开(公告)日:2021-02-16
The invention provides a diamine crosslinking agent for acidic polysaccharides consisting of a diamine compound having a primary amino group at both terminals and an ester or thioester bond in the molecule, wherein the number of atom in the linear chain between at least one of the amino groups and the carbonyl carbon in the ester or thioester is 1 to 5; in particular, a diamine crosslinking agent for acidic polysaccharides which is represented by the general formula (I) below:
[the symbols in the formula are as described in the specification]; a crosslinked acidic polysaccharide obtained by forming crosslinks by amide bonding between the amino groups in the diamine crosslinking agent and carboxyl groups in an acidic polysaccharide; and a medical material including the crosslinked product.
Development of Dual-Acting Agents for Thromboxane Receptor Antagonism and Thromboxane Synthase Inhibition. 3. Synthesis and Biological Activities of Oxazolecarboxamide-Substituted ω-Phenyl-ω-(3-pyridyl)alkenoic Acid Derivatives and Related Compounds
作者:Kumiko Takeuchi、Todd J. Kohn、Timothy A. True、Dale E. Mais、James H. Wikel、Barbara G. Utterback、Virginia L. Wyss、Joseph A. Jakubowski
DOI:10.1021/jm980173n
日期:1998.12.1
A novel series of oxazolecarboxamide-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acid derivatives was discovered as potent dual-acting agents to block the TXA(2) receptor and to inhibit the thromboxane synthase (TRA/TSI). Synthesis, structure-activity relationship (SAR), and in vitro and in vivo pharmacology of this series of compounds are described. Modification of the series revolved around the oxazole moiety to increase the hydrophilicity of the compounds and to correlate the biological activity with lipophilicity of the compounds. The most potent in the series was (E)-7-[4-[4-[[(4-cyclohexylbutyl)amino]carbonyl]-2-oxazolyl]phenyl]-7-(3-pyridyl)hept-6-enoic acid (14) with K-d = 9.9 +/- 0.4 nM for the thromboxane receptor antagonism and IC50 = 55.0 +/- 17.9 nM for thromboxane synthase inhibition. The compound 14 was a selective TRA/TSI which exhibited desirable characteristics for oral activity, "shunt" effect to elevate PGI(2) level, and absence of agonist activity.