CAS: 63-45-6; N4-(6-Methoxyquinolin-8-yl)Pentane-1,4-Diamine Bis(Phosphate)

上下游产品

CAS号90-34-6 伯氨喹 | CAS号88755-75-3 2,2,2-trifluoro...

伯氨喹置于磷酸体系中,用 乙醚 作为反应溶剂,化学反应生成 磷酸伯氨喹
参考文献:伯氨喹糖结合物的合成作为潜在的组织裂殖杀伤剂.
标题:伯氨喹糖结合物的合成作为潜在的组织裂殖杀伤剂.
摘要:Primaquine(pq)是唯一一种可通过消除寄生虫的休眠肝脏形式(次生子)来预防因间日疟原虫和卵形疟原虫引起的疟疾复发的药物.与pq限值相关的副作用是用于治疗疟疾.为了克服过早的氧化脱氨基作用并延长药物在生物系统中的寿命,通过将伯氨喹与己糖在磷酸盐缓冲液中偶联,合成了新型的pq糖缀合物.杂合分子的糖类部分被认为可以将药物引导至子裂殖体所在的肝脏.所有合成的化合物均已得到充分表征,并评估了其自由基治疗活性.这三种化合物是葡萄糖苷(15A),测试了高活性的半乳糖苷(15B)和甘露糖苷(15C)在恒河猴中的活性,其中活性最高的化合物15B的活性是标准药物pq二磷酸酯(3.861 Mmol)的两倍(在1.92 Mmol / Kg时具有100%的自由基治疗活性) /公斤).有人提出,这些研究的结果可能有利于开发一种新型的有效的组织防裂剂抗疟疾化合物.
DOI:10.1111/cbdd.12944

专利信息

专利号:US-7253177-B2
优先权日:2004-10-22
标 题:Synthesis and antimalarial activity of pyrrolo[3,2-f]quinazoline-1,3-diamine derivatives
发明人：LIN AI J; GUAN JIAN; ZHANG QUAN; SKILLMAN DONALD R
权利人:US ARMY
摘要:The invention relates to derivatives of pyrroloquinazolinediamine, more specifically derivatives of 7-(substituted)-7H-pyrrolo[3,2-F] quinazoline-1,3-diamines that are non-toxic and are also effective in the treatment of malaria, including P. falciparum and P. vivax strains. The derivatives are certain carbamate derivatives, succinimide derivatives, alkylcarboxamides derivatives and acetamide derivative, phthalimides, alkylamines and all other amide and imide derivatives and their 1-hydroxy analogs. The derivatives of the present invention are also soluble in common organic solvents to facilitate the purification in a large scale synthesis of the composition.

专利号:WO-2012149093-A1
优先权日:2011-04-26
标 题 :2-guanidino-4-oxo-imidazoline derivatives as antimalarial agents, synthesis and methods of use thereof
发明人：LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T
权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF ARMY; LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T
摘要:The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.

专利号:US-2006287257-A1
优先权日:2005-06-20
标 题 :Pharmaceutical compositions to treat diseases caused by mycobacterium
发明人：STOCKEL RICHARD F
权利人:STOCKEL RICHARD F
摘要:The invention teaches the synthesis of pharmaceutical composition and methods of synthesis to treat people and animals infected with a pathogenic mycobacterium. In particular the compositions of this invention are suitable for the treatment of tuberculosis, malaria, and other infections diseases caused by mycobacterium.

专利号:US-2008051323-A1
优先权日:2004-08-21
标 题 :Chloroquine drug compositions and methods for their synthesis
发明人：KOSAK KENNETH M
权利人:KOSAK KENNETH M
摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.

专利号:US-2007060499-A1
优先权日:2005-09-15
标 题 :Chloroquine combination drugs and methods for their synthesis
发明人：KOSAK KENNETH M
权利人:KOSAK KENNETH M
摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.

专利号:US-2007166281-A1
优先权日:2004-08-21
标题 :Chloroquine coupled antibodies and other proteins with methods for their synthesis
发明人：KOSAK KENNETH M
权利人:KOSAK KENNETH M
摘要:This invention discloses compositions of chloroquine-coupled active agents such as therapeutic antibodies or insulin, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the drug is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a drug directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing the drug for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and antibody or insulin to their site of action.