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    • 1. 发明专利
    • Drug resistance overcoming agent
    • 空值
    • JP3474941B2
    • 2003-12-08
    • JP25006794
    • 1994-09-19
    • ポーラ化成工業株式会社
    • 隆男 伊藤正彦 土屋孝雄 服部
    • C07D295/08A61K31/495A61K31/496A61K45/00A61P31/04A61P33/02A61P35/00A61P43/00C07D215/20C07D215/22
    • Y02A50/411
    • PURPOSE: To obtain a new compound useful as a medicinal resistance overcoming agent low in calcium antagonistic activity, provided with the resistance to chemotherapeutic agents, overcoming the medicinal resistance to cancers or pathogenic microbes and improving the therapeutic effect by chemotherapeutic agents. CONSTITUTION: This compound (a physiologically permissible salt thereof) is expressed by formula I [X and Y are each H or a halogen; R1 is a halogen, alkyl, alkyloxy, or monocyclic or bicyclic aromatic ring which may contain one nitrogen atom in the ring], e.g. 1-(3,3-diphenylpropyl)-4-[2- hydroxy-3-(quinolin-5-yloxy)propyl]piperazine. The compound of formula I is obtained by the following process: a compound of formula III is prepared by reaction of a halogen compound of formula II with piperazine; separately, an epoxy compound of formula V is formed by reaction between a compound of formula IV and an epihalohydrin in the presence of sodium hydride; and the compound of formula III and the epoxy compound of formula V are subjected to ring opening condensation reaction. The microbial infectious diseases associated with this compound are involved in Staphylococcus aureus, Plasmodium, Trypanosoma, etc.
    • 目的:获得一种新的化合物,可用作抗钙化拮抗作用的药物抵抗剂,具有抗化学治疗药物,克服对癌症或致病微生物的药用抗性,并改善化学治疗剂的治疗效果。 构成:该化合物(其生理上允许的盐)由式I表示[X和Y各自为H或卤素; R1是可以在环中含有一个氮原子的卤素,烷基,烷氧基或单环或双环芳环],例如。 1-(3,3-二苯基丙基)-4- [2-羟基-3-(喹啉-5-基氧基)丙基]哌嗪。 式I化合物通过以下方法获得:式III化合物通过式II的卤素化合物与哌嗪的反应来制备; 另外,通过式IV化合物与表卤代醇在氢化钠存在下反应形成式V的环氧化合物; 并使式III化合物和式V的环氧化合物进行开环缩合反应。 与该化合物相关的微生物感染性疾病涉及金黄色葡萄球菌,疟原虫,锥虫病等。
    • 8. 发明专利
    • Drug resistance overcoming agent
    • 空值
    • JP3474940B2
    • 2003-12-08
    • JP25003494
    • 1994-09-19
    • ポーラ化成工業株式会社
    • 隆男 伊藤正彦 土屋孝雄 服部
    • C07D295/18A61K31/495A61K31/496A61K45/00A61P31/04A61P33/02A61P35/00A61P43/00C07D215/20C07D215/22
    • Y02A50/411
    • PURPOSE: To obtain a new compound useful as medicinal resistance overcoming agent low in calcium antagonistic activity, provided with the resistance to chemotherapeutic agents, overcoming the medicinal resistance to cancers or pathogenic microbes and improving the therapeutic effect by chemotherapeutic agents. CONSTITUTION: This compound (a physiologically permissible salt thereof) is expressed by formula I [X and Y are each H or a halogen; (n) is 1-4; R1 is a halogen, 1-4C alkyl, 1-4C alkyloxy, or (nitro-substituted or N-contg.) monocyclic or bicyclic aromatic ring], e.g. 1-(2,2-diphenylethylcarbonyl)-4-[3-(7- chloroquinolin-4-yloxy)-2-hydroxypropyl]piperazine of formula II. The compound of formula I is obtained by the following process: a compound of formula IV is prepared by reaction of a halogen compound of formula III with piperazine; separately, an epoxy compound of formula V is formed by reaction between a compound of formula R OH and an epihalohydrin in the presence of sodium hydride; and the compound of formula IV and the epoxy compound of formula V are subjected to ring opening condensation reaction.
    • 目的:获得一种新的化合物,作为抗钙化拮抗作用的药物抵抗药物,具有抵抗化学治疗剂的作用,克服了对癌症或致病微生物的药用抗性,并提高了化疗药物的治疗效果。 构成:该化合物(其生理上允许的盐)由式I表示[X和Y各自为H或卤素; (n)为1-4; R1是卤素,1-4C烷基,1-4C烷氧基或(硝基取代或N-对 - )单环或双环芳族环],例如 4- [3-(4-氯喹啉-4-基氧基)-2-羟基丙基]哌嗪的1-(2,2-二苯基乙基羰基)-4- [ 式I的化合物通过以下方法获得:式IV的化合物通过式III的卤素化合物与哌嗪的反应来制备; 分别地,在氢化钠存在下,通过式R 1 OH的化合物与表卤代醇反应形成式Ⅴ的环氧化合物; 并且式Ⅳ化合物和式Ⅴ的环氧化合物进行开环缩合反应。