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公开(公告)号：KR1020010045493A
公开(公告)日：2001-06-05
申请号：KR1019990048800
申请日：1999-11-05
Applicant: 한국과학기술연구원
IPC: C07F9/00
CPC classification number: C07F9/65815
Abstract: PURPOSE: A temperature-sensitive cyclic phosphazene trimer and its manufacturing method are provided. CONSTITUTION: The method for manufacturing a temperature-sensitive cyclic phosphazene trimer of the formula (1) comprises the steps of: i) reacting alcohol of the formula (2) with 1.5 equivalent of sodium or hydride sodium in solvent such as THF, benzene, or toluene to obtain a compound of the formula (3); ii) adding 3-4 equivalents of the compound of the formula (3) to solution containing solvent; iii) reacting the mixture in solution having dry-ice and acetone for 2-4 hours and for 10-12 hours at room temperature to obtain an intermediate of the formula (5); iv) reacting the intermediate in solution containing solvent such as triethylamine for 2-4 hours at room temperature and 40-60 deg.C for 1-3 days; and v) centrifuging the solution, eliminating sediments, and purifying the product. In the formula, R is an ethyl or benzyl group. m is an integer of 2, 7, 2, or 16. n is an integer of 0, 1, or 3.
Abstract translation: 目的：提供温度敏感的环磷腈三聚体及其制备方法。 构成：制备式（1）的温度敏感的环磷腈三聚体的方法包括以下步骤：i）使式（2）的醇与1.5当量的钠或氢化钠在溶剂如THF，苯， 或甲苯，得到式（3）的化合物; ii）向含溶剂的溶液中加入3-4当量的式（3）化合物; iii）使混合物在干冰和丙酮溶液中反应2-4小时，并在室温下反应10-12小时，得到式（5）的中间体; iv）使中间体在含溶剂如三乙胺的溶液中在室温和40-60℃下反应1-4天; 和v）离心溶液，消除沉淀物并净化产物。 在该式中，R是乙基或苄基。 m是2，7，2或16的整数.n是0,1或3的整数。
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公开(公告)号：KR1020010047025A
公开(公告)日：2001-06-15
申请号：KR1019990051049
申请日：1999-11-17
Applicant: 한국과학기술연구원
IPC: C08G79/02
CPC classification number: C08G79/025
Abstract: PURPOSE: A degradable polyphosphazene polymer having the phase transition behavior with temperature and its preparation method are provided, whose phase transition temperature and degradation velocity are controlled easily. CONSTITUTION: The polyphosphazene polymer is represented by the formula 1, wherein X represents O or N; NHR is depsipeptide and represents ethyl-2-(O-glycyl)glycolate or ethyl-2-(O-glycyl)lactate; NHR' is amino acid ethylester and represents NHCH(CH2CH2COOC2H5)COOC2H5 or phenylalanine ethylester; NHR'' represents glycine ethylester or alanine ethylester; a, b, c, d, e and f represent the mol of copolymer and are 0-1.0 and the sum of a, b, c, d, e and f is 1.0; and n represents the degree of polymerization and is 100-1,000. The method comprises the steps of reacting polydichlorophoaphazene of the formula 3 with an alkali metal salt of methoxy poly(ethylene glycol) of the formula 4 or aminomethoxy poly(ethylene glycol) of the formula 5 by the molar ratio of 1 : 0.3-1.5; reacting the product with depsipeptide (H2NR) and NH2CH(CH2CH2COOC2H5)COOC2H5 or phenylalanine ethylester (H2NR') by the molar ratio of 1 : 0.1-2 in organic solvent; and reacting the product with glycine ethylester or alanine ethylester (H2NR'') to obtain the polyphosphazene polymer of the formula 1.
Abstract translation: 目的：提供具有温度相变特性的可降解聚磷腈聚合物及其制备方法，其相变温度和降解速度易于控制。 构成：聚磷腈聚合物由式1表示，其中X表示O或N; NHR是脱肽，代表乙基-2-（O-甘氨酰）乙醇酸酯或乙基-2-（O-甘氨酰）乳酸酯; NHR'是氨基酸乙酯，代表NHCH（CH 2 CH 2 COOC 2 H 5）COOC 2 H 5或苯丙氨酸乙酯; NHR“表示甘氨酸乙酯或丙氨酸乙酯; a，b，c，d，e和f表示共聚物的摩尔数，为0-1.0，a，b，c，d，e和f的和为1.0; n表示聚合度，为100〜1,000。 该方法包括以下步骤：使式3的聚二氯代吡嗪与式4的甲氧基聚（乙二醇）的碱金属盐或式5的氨基甲氧基聚（乙二醇）摩尔比为1:0.3-1.5; 将产物与有机溶剂中的摩尔比为1：0.1-2的反式肽（H2NR）和NH2CH（CH2CH2COOC2H5）COOC2H5或苯丙氨酸乙酯（H2NR'）反应; 并使产物与甘氨酸乙酯或丙氨酸乙酯（H 2 NR“）反应，得到式1的聚磷腈聚合物。
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3.发明授权
公开(公告)号：KR100363394B1
公开(公告)日：2002-12-05
申请号：KR1020000048360
申请日：2000-08-21
Applicant: 한국과학기술연구원
IPC: C07F9/02
Abstract: 본 발명은 다음 화학식 1로 표시되는, 온도감응성을 갖는 신규한 고리형 포스파젠 삼량체-백금착물 복합체, 그 제조방법 및 그를 유효성분으로 함유하는 항암제 조성물에 관한 것이다.
식 중, m은 폴리(알콕시에틸렌글리콜)의 반복단위로서 2, 7, 및 12중에서 선택되고, n은 알킬사슬의 길이를 나타내며 0, 1, 2, 및 3의 값을 갖는다. x는 음이온 그룹인 아미노산 잔류기의 길이로서 0 (아미노말론산기), 1 (아스파르트산기), 및 2 (글루타민산기) 중에서 선택되며, A
2 는 2,2-디메틸-1,3-프로판디아민 (dmpda), 트란스(±)-1,2-디아미노시클로헥산 (dach) 또는 1,1-디아미노메틸시클로헥산 (dmach) 중에서 선택된 두자리 킬레이트형 아민이다.-
Patent Agency Ranking
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5.发明公开
公开(公告)号：KR1020020015180A
公开(公告)日：2002-02-27
申请号：KR1020000048360
申请日：2000-08-21
Applicant: 한국과학기술연구원
IPC: C07F9/02
CPC classification number: C07F9/65815 , C07F15/0093
Abstract: PURPOSE: Provided are a temperature sensitive phosphagen trimer-platinum complex, its producing method and a composition of an anticancer agent containing it as an active ingredient, thereby developing an anticancer agent which has an excellent anticancer activity with less toxicity. CONSTITUTION: The temperature sensitive phosphagen trimer-platinum complex is represented by formula(1), in which m is an integer of 2, 7 and 12; n is an integer of 0, 1, 2 and 3; x is an integer of 0, 1 and 2; A2 is double figures chelate amine selected from 2,2-dimethyl-1,3-propanediamine, 1,2-diaminocyclohexane or 1,1-diaminomthylcyclohexane. The method for producing the temperature sensitive phosphagen trimer-platinum complex comprises the steps of: hydrolyzing the intermediate of cyclic phosphagen trimer represented by the formula(2) with alkali earth metals of formula(3) or alkali metals of formula(4) to produce alkali earth metal salts of formula(5) or alkali metal salts of formula(6); and reacting the cyclic phosphagen trimer-alkali metal salts with (diamine) platinum (II) acidic salts of formula(7) in a ratio of 1:3.
Abstract translation: 目的：提供一种温敏磷酸三聚体 - 铂络合物，其制备方法和含有它作为活性成分的抗癌剂的组合物，从而开发出具有优异的抗癌活性和较低毒性的抗癌剂。 构成：温度敏感的磷酸酯三聚体 - 铂络合物由式（1）表示，其中m是2,7和12的整数; n是0,1,2和3的整数; x是0，1和2的整数; A2是选自2,2-二甲基-1,3-丙二胺，1,2-二氨基环己烷或1,1-二氨基乙基环己烷的双重数字螯合胺。 生产温敏磷酸三聚体 - 铂络合物的方法包括以下步骤：用式（3）的碱土金属或式（4）的碱金属水解由式（2）表示的环状磷酸酯三聚体的中间体，以产生 式（5）的碱土金属盐或式（6）的碱金属盐; 并使环状磷酸酯三聚体 - 碱金属盐与（二胺）式（7）的铂（II）酸性盐以1:3的比例反应。
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公开(公告)号：KR100259367B1
公开(公告)日：2000-06-15
申请号：KR1019980023695
申请日：1998-06-23
Applicant: 한국과학기술연구원
IPC: C08G79/02
Abstract: 다음 화학식 1로 표시되는 폴리포스파젠계 고분자 및 그의 제조방법이 제공된다.
[화학식 1]
본 발명에 따른 폴리포스파젠계 고분자는 온도감응성과 생체분해성을 동시에 가지므로 약물전달시스템을 중심으로 하는 의료용재료분야, 환경분야 및 화장품분야와 같은 다양한 분야에서 응용이 가능하며, 분자내 메톡시폴리에틸렌 및 아미노산에스테르의 조성, 메톡시폴리에틸렌글리콜의 분자량, 아미노산에스테르의 종류에 따라 폴리포스파젠계 고분자의 저임계용액온도와 분해속도를 응용목적에 맞게 조절할 수 있다.-
公开(公告)号：KR100321296B1
公开(公告)日：2002-03-18
申请号：KR1019990048800
申请日：1999-11-05
Applicant: 한국과학기술연구원
IPC: C07F9/00
CPC classification number: C07F9/65815
Abstract: 본발명은다음화학식 1로표시되는온도감응성을갖는신규한고리형포스파젠삼량체및 그의제조방법에관한것이다. (식중, HNA는아미노산기로서글라이신기(-NHCHCOO), 아미노말론산기(-NHCH(COO)), 아스파르트산기(-NHCH(CHCOO)COO), 및글루타민산기(-NHCH(CHCHCOO)COO) 중에서선택되며, R은에틸기또는벤질기중에서선택된다. m은폴리(알콕시에틸렌글리콜)의반복단위로서 2, 7, 12 및 16 중에서선택되고 n은알킬사슬의길이를나타내는정수로서 0, 1, 및 3 중에서선택됨)
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公开(公告)号：KR1020000002785A
公开(公告)日：2000-01-15
申请号：KR1019980023695
申请日：1998-06-23
Applicant: 한국과학기술연구원
IPC: C08G79/02
Abstract: PURPOSE: Polyphosphagen and temperature sensitive and biodegradable properties are given by substituting polydichlorophosphagen with methoxypolyethyleneglycol and amino acid ester. CONSTITUTION: The title compound(I) is manufactured. In formula, NHA is amino acid group selected from glycine(-NHCH2COO¬-), alanine(-NHCH(CH3)COO¬-), beta-alanine(-NHCH2CH2COO¬-), aminomalonic acid(-NHCH(COO¬-)2), aspartic acid(NHCH(CH2COO¬-)COO¬-), and glutamic acid(-NHCCH(CH2CH2COO¬-)COO¬-), R is methyl, ethyl, or benzyl, m is repeat unit of polyethyleneglycol and integer selected from 2, 7 and 16, x is 0.2-1.8 of mole content of polyethyleneglycol, and n is 10-100 of degree of polymerization.
Abstract translation: 目的：聚磷酸酯和温度敏感和可生物降解性质是用甲氧基聚乙二醇和氨基酸酯代替聚二氯磷酸酯。 构成：制备标题化合物（I）。 在式中，NHA是选自甘氨酸（-NHCH 2 COO-），丙氨酸（-NHCH（CH 3）COO-），β-丙氨酸（-NHCH 2 CH 2 COO-），氨基马来酸（-NHCH（COO-） 2），天冬氨酸（NHCH（CH 2 COO-）COO-））和谷氨酸（-NHCCH（CH 2 CH 2 COO-））COO-），R是甲基，乙基或苄基，m是聚乙二醇和整数的重复单元 选自2,7和16，x是聚乙二醇的摩尔含量为0.2-1.8，n为10-100聚合度。
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