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Water soluble porphyrin Platinum compounds with high tumor selectivity and its use in preparing medicine for the treatment of benign and malignant tumor Diseases

机译:具有高肿瘤选择性的水溶性卟啉铂化合物及其在制备治疗良性和恶性肿瘤疾病的药物中的用途

摘要

Soluble compounds containing porfirin and drugs for the treatment of tumors (benign and malignant). Drugs, including compounds. In particular, these compounds are suitable for photodynamic antitumor therapy. 1. Claim 1: according to formula (1): R is a platinum derivative of formula compound (2) and a platinum derivative of tetrahydrofluorocarbon (a);n = 1-20; X is O, S, NH, N-alkyl; R2 / R3 are H, alkyl, aryl, aralkyl, hetaryl, hetarylalkyl, cycloalkyl; R4 is H, alkyl, aryl, aralkyl, hetaryl, hetarylalkyl, cycloalkyl; R5 is H, alkyl, O-alkyl, S-alkyl, halogen, nitro, cyano, amino, substituted amino; R6 is H, alkyl, O-alkyl, S-alkyl, halogen, nitro, cyano, amino, substituted amino; and according to formula (3);R is a formula compound (4);n = 1-20; X is O, S, NH, N-alkyl; R1 / R2 / R3 / R4 are H, alkyl, aryl, aralkyl, hetaryl, hetarylalkyl, cycloalkyl; or R2-Z-R3, Z is (CH2) n, n = 0-6; R1 / R4 is H, - (CH2) n-COOR8, n = 0-6; R5 is H, alkyl, aryl, aralkyl, hetaryl, hetarylalkyl, cycloalkyl; R6 is H, alkyl, O-alkyl, S-alkyl, halogen, nitro, cyano, amino, substituted amino; R7 is H, alkyl, O-alkyl, S-alkyl, halogen, nitro, cyano, amino, substituted amino; R8 is H, alkyl; and (b) platinum-type derivatives with hematoporphyrin according to formula (5);R2 / R3 is h, asphalt, arilo, aralquilo, hetario, hetarilalquilo, ciclalquilo, R4 is h, asphalt, cyclopropylus, R5 is h, asphalt, cyclopropylus, R6 is h, asphalt, arilo, aralquilo, hetario, hetarilalquilo, cyclopropylus; formula is (6);R1 / R2 / R3 / R4 are H, alkyl, aryl, aralkyl, hetaryl, hetarylalkyl, cycloalkyl or R2-Z-R4, with Z being (CH2) n, n = 0-6; or R1 / R3 is H, - (CH2) n-COOR6, n = 0-6; R4 / R5 are H, alkyl, aryl, aralkyl, hetaryl, hetarylalkyl, cycloalkyl; R6 are H, alkyl, aryl, aralkyl, hetaryl, hetarylalkyl, cycloalkyl; R7 are H, alkyl, aryl, aralkyl, hetaryl, hetarylalkyl, cycloalkyl.
机译:含有卟啉和药物的可溶性化合物,用于治疗肿瘤(良性和恶性)。药物,包括化合物。这些化合物尤其适用于光动力抗肿瘤治疗。 1.根据式(1)的化合物:R是式化合物(2)的铂衍生物和四氢氟烃的铂衍生物(a); n = 1-20;和n = 1-20。 X是O,S,NH,N-烷基; R2 / R3为H,烷基,芳基,芳烷基,杂芳基,杂芳基烷基,环烷基; R4为H,烷基,芳基,芳烷基,杂芳基,杂芳基烷基,环烷基; R5是H,烷基,O-烷基,S-烷基,卤素,硝基,氰基,氨基,取代的氨基; R6为H,烷基,O-烷基,S-烷基,卤素,硝基,氰基,氨基,取代的氨基;且根据式(3); R为式化合物(4); n = 1-20;和X是O,S,NH,N-烷基; R1 / R2 / R3 / R4为H,烷基,芳基,芳烷基,杂芳基,杂芳基烷基,环烷基;或R 2 -Z-R 3,Z为(CH 2)n,n = 0-6; R1 / R4为H,-(CH2)n-COOR8,n = 0-6; R5为H,烷基,芳基,芳烷基,杂芳基,杂芳基烷基,环烷基; R6为H,烷基,O-烷基,S-烷基,卤素,硝基,氰基,氨基,取代的氨基; R7为H,烷基,O-烷基,S-烷基,卤素,硝基,氰基,氨基,取代的氨基; R 8是H,烷基; (b)具有根据式(5)的血卟啉的铂类衍生物; R2 / R3为h,沥青,arilo,alalquilo,hetario,hetarilalquilo,ciclalquilo,R4为h,沥青,环丙基,R5为h,沥青,环丙基,R 6为h,沥青,芳基,阿拉基洛,杂芳基,戊基铝基,环丙基;式为(6); R 1 / R 2 / R 3 / R 4为H,烷基,芳基,芳烷基,杂芳基,杂芳基烷基,环烷基或R 2 -Z-R 4,其中Z为(CH 2)n,n = 0-6。或者R1 / R3为H,-(CH2)n-COOR6,n = 0-6; R4 / R5为H,烷基,芳基,芳烷基,杂芳基,杂芳基烷基,环烷基; R6为H,烷基,芳基,芳烷基,杂芳基,杂芳基烷基,环烷基; R 7为H,烷基,芳基,芳烷基,杂芳基,杂芳基烷基,环烷基。

著录项

  • 公开/公告号AR038479A1

    专利类型

  • 公开/公告日2005-01-19

    原文格式PDF

  • 申请/专利权人 ZENTARIS GMBH;

    申请/专利号AR2003P100329

  • 发明设计人

    申请日2003-02-03

  • 分类号C07D487/00;C07F15/00;A61K31/4025;A61P35/00;

  • 国家 AR

  • 入库时间 2022-08-21 22:18:54

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