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    Helianthrone derivatives as anti-cancer agents
    1.
    发明授权
    Helianthrone derivatives as anti-cancer agents 失效
    海龙龙衍生物作为抗癌剂

    公开(公告)号：US06229048B1

    公开(公告)日：2001-05-08

    申请号：US09494296

    申请日：2000-01-31

    申请人： Yehuda Mazur ,  Gad Lavie

    发明人： Yehuda Mazur ,  Gad Lavie

    IPC分类号： C07C23900

    CPC分类号： A61K31/122 ,  C07C46/00 ,  C07C50/36 ,  C07C65/40 ,  C07C69/95 ,  C07C2603/54

    摘要： A method for treating cancer comprising administering a 1,3,4,6-tetrahydroxy-helianthrone derivative. The compounds can be used in the absence of light irradiation or for photodynamic therapy of solid tumors wherein the tumor site is subjected to light irradiation after administration of the active ingredient. A preferred compound is 10,13-dimethyl-1,3,4,6-tetrahydroxy-helianthrone.

    摘要翻译： 一种治疗癌症的方法，包括给予1,3,4,6-四羟基 - 向日葵粉衍生物。 该化合物可以在不存在光照射的情况下使用，也可以用于实施肿瘤的光动力学治疗，其中在施用活性成分后肿瘤部位进行光照射。 优选的化合物是10,13-二甲基-1,3,4,6-四羟基 - 向日葵。

    Preparation of derivatives of cholesterol
    3.
    发明授权
    Preparation of derivatives of cholesterol 失效
    胆固醇衍生物的制备

    公开(公告)号：US3963765A

    公开(公告)日：1976-06-15

    申请号：US487432

    申请日：1974-07-11

    申请人： Yehuda Mazur ,  Avner Rotman

    发明人： Yehuda Mazur ,  Avner Rotman

    IPC分类号： C07J9/00

    CPC分类号： C07J9/00

    摘要： Process for the production of hydroxylated derivatives of cholesterol and 7-dehydrocholesterol which comprises subjecting a saturated unsubstituted or substituted derivative of cholestane, dissolved in a suitable solvent, in the presence of peracetic acid, to irradiation with ultra-violet radiation of a wavelength below 350m.mu. , or heating in a suitable solvent, separating the reaction products, which if desired, are converted to other derivatives, and recovering the residue of the starting material. Novel derivatives are obtained and these are: 3.beta.-acetoxy,25-hydroxy,5.alpha.-cholestane; 3.beta.-acetoxy, 5.alpha.,25-dihydroxy cholestane; 3.beta.,5.alpha.,25-trihydroxy cholestane; 3-keto, 5.alpha.,25-dihydroxy cholestane; 3-keto,25-hydroxy-.DELTA..sup.4 -cholestane; 3.beta.,25-diacetoxy-5.alpha.-hydroxy-cholestane; 3.beta.-acetoxy, 25-trichloroacetoxy-5.alpha.-hydroxy-cholestane, 25-trichloroacetoxy-cholesterol and 25-acetoxy-cholesterol.

    摘要翻译： 用于生产胆固醇和7-脱氢胆固醇的羟基化衍生物的方法，其包括在过乙酸存在下使溶解在合适溶剂中的饱和的未取代或取代的胆甾烷的衍生物经过饱和的溶解在合适溶剂中的衍生物照射波长低于350μm的紫外线辐射 或在合适的溶剂中加热，将反应产物分离，如果需要，将其转化为其它衍生物，并回收原料残余物。 得到新的衍生物，它们是：3β-乙酰氧基，25-羟基，5α-胆甾烷; 3β-乙酰氧基，5α，25-二羟基胆甾烷; 3β，5α，25-三羟基胆甾烷; 3-keto，5α，25-二羟基胆甾烷; 3-酮基，25-羟基-DTA4-胆甾烷; 3β，25-二乙酰氧基-5α-羟基 - 胆固醇; 3β-乙酰氧基，25-三氯乙酰氧基-5α-羟基 - 胆固醇，25-三氯乙酰氧基 - 胆固醇和25-乙酰氧基 - 胆固醇。

    Helianthrone derivatives as anti-cancer agents
    4.
    发明授权
    Helianthrone derivatives as anti-cancer agents 有权
    海龙龙衍生物作为抗癌剂

    公开(公告)号：US06867235B2

    公开(公告)日：2005-03-15

    申请号：US10209427

    申请日：2002-07-30

    申请人： Yehuda Mazur ,  Gad Lavie

    发明人： Yehuda Mazur ,  Gad Lavie

    IPC分类号： A61K31/122 ,  A61K31/136 ,  A61K31/235 ,  A61K31/195 ,  A61K31/12

    CPC分类号： A61K31/136 ,  A61K31/122 ,  A61K31/235

    摘要： Hypericin, helianthrone and derivatives thereof of general formula (I) wherein the dotted line between positions 11 and 12 represent an optional C11-C12 bond; R is independently selected from the group consisting of hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; R′ is independently selected from the group consisting of hydroxy and C1-C10 alkoxy; R″ is independently selected from the group consisting of hydrogen, hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; and R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen, hydroxy, chloro, bromo, C1-C10 alkyl, C1-C10 alkoxy, and C1-C10 alkoxycarbonyl, provided that R″ is not hydrogen when there is a C11-C12 bond, are useful as inhibitors of angiogenesis and can be used to prevent formation of metastases and restenosis and for the treatment of angiogenesis-associated ophthalmologic disorders. In addition, the helianthrones of formula (I) can be used for the treatment of tumors in the absence of light irradiation. New compounds include those of formula I which are other than hypericin and known hypericin derivatives and there is either a C11-C12 bond or at least one R″ is other than hydrogen.

    摘要翻译： 通式（I）的金丝桃素，向日葵及其衍生物，其中位置11和12之间的虚线代表任选的C 11 -C 12键; R独立地选自羟基，C 1 -C 10烷氧基，NH-C 1 -C 10烷基和NH-羟基（C 1 -C 10）烷基; R'独立地选自羟基和C 1 -C 10烷氧基; R“独立地选自氢，羟基，C 1 -C 10烷氧基，NH-C 1 -C 10烷基和NH-羟基（C 1 -C 10）烷基; R 1，R 2，R 3，R 4，R 5和R 6独立地选自氢，羟基，氯，溴，C 1 -C 10烷基，C 1 -C 10烷氧基和C 1 -C 10烷氧基羰基，条件是R“ 当存在C11-C12键时，不是氢，可用作血管发生的抑制剂，可用于预防转移和再狭窄的形成以及用于治疗血管发生相关的眼科疾病。 此外，式（I）的长方体可用于在不存在光照射的情况下治疗肿瘤。 新化合物包括除金丝桃素和已知金丝桃素衍生物之外的式I的那些，并且存在C 11 -C 12键或至少一个R“不是氢。

    Helianthrone derivatives as anti-cancer agents
    5.
    发明申请
    Helianthrone derivatives as anti-cancer agents 审中-公开
    海龙龙衍生物作为抗癌剂

    公开(公告)号：US20050038115A1

    公开(公告)日：2005-02-17

    申请号：US10948212

    申请日：2004-09-24

    申请人： Yehuda Mazur ,  Gad Lavie

    发明人： Yehuda Mazur ,  Gad Lavie

    IPC分类号： A61K31/122 ,  A61K31/136 ,  A61K31/235 ,  A61K31/225 ,  A61K31/12 ,  A61K31/137

    CPC分类号： A61K31/136 ,  A61K31/122 ,  A61K31/235

    摘要： Hypericin and helianthrone derivatives of general formula (I) wherein the dotted line between positions 11 and 12 represent an optional C11-C12 bond; R is independently selected from the group consisting of hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; R′ is independently selected from the group consisting of hydroxy and C1-C10 alkoxy; R″ is independently selected from the group consisting of hydrogen, hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; and R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen, hydroxy, chloro, bromo, C1-C10 alkyl, C1-C10 alkoxy, and C1-C10 alkoxycarbonyl, provided that R″ is not hydrogen when there is a C11-C12 bond and when there is a C11-C12 bond and both R′ are hydroxy, both R″ groups are not hydroxy. These compounds and pharmaceutical compositions containing them as active agents are useful as inhibitors of angiogenesis and can be used to prevent formation of metastases and restenosis and for the treatment of angiogenesis-associated ophthalmologic disorders. In addition, the helianthrone derivatives of formula (I) can be used for the treatment of tumors in the absence of light irradiation.

    摘要翻译： 通式（I）的金丝桃素和helianthrone衍生物，其中位置11和12之间的虚线表示任选的C 11 -C 12键; R独立地选自羟基，C 1 -C 10烷氧基，NH-C 1 -C 10烷基和NH-羟基（C 1 -C 10）烷基; R'独立地选自羟基和C 1 -C 10烷氧基; R“独立地选自氢，羟基，C 1 -C 10烷氧基，NH-C 1 -C 10烷基和NH-羟基（C 1 -C 10）烷基; R 1，R 2，R 3，R 4，R 5和R 6独立地选自氢，羟基，氯，溴，C 1 -C 10烷基，C 1 -C 10烷氧基和C 1 -C 10烷氧基羰基，条件是R“ 当存在C 11 -C 12键时不是氢，当存在C 11 -C 12键并且两个R'都是羟基时，两个R“不是羟基。 含有它们作为活性剂的这些化合物和药物组合物可用作血管发生的抑制剂，并且可用于预防转移和再狭窄的形成和用于治疗血管生成相关性眼科疾病。 此外，式（I）的龙眼酮衍生物可用于在不存在光照射的情况下治疗肿瘤。

    Phenothiazinium salts and their use for disinfecting aqueous effluents
    6.
    发明授权
    Phenothiazinium salts and their use for disinfecting aqueous effluents 失效
    吩噻嗪鎓盐及其用于消毒含水废水的用途

    公开(公告)号：US5220009A

    公开(公告)日：1993-06-15

    申请号：US691313

    申请日：1991-04-25

    申请人： Yehuda Mazur ,  Aureliu Acher ,  Lea Shragina ,  Moshe Avramoff

    发明人： Yehuda Mazur ,  Aureliu Acher ,  Lea Shragina ,  Moshe Avramoff

    IPC分类号： A61L2/18 ,  C07D279/18 ,  C07H15/26

    CPC分类号： C07H15/26 ,  C07D279/18

    摘要： Novel 3,7-disubstituted phenothiazinium salts are active in the photochemical disinfection of aqueous effluents. The novel salts are of the general formula ##STR1## wherein: either R.sub.1 is a saccharide residue;R.sub.2 is alkyl, cycloalkyl, aryl, aralkyl or heterocyclyl, any alkyl or alkylene chain being optionally interrupted by one or more heteroatoms, and Y is alkylene optionally substituted by alkyl, cycloalkyl, aryl or aralkyl; orR.sub.1 and R.sub.2 are each methyl and Y is a bond; and when R.sub.1 is a saccharide residue X is an anion selected from halogen, R.sub.3 CO.sub.2.sup.-, R.sub.3 SO.sub.3.sup.- and R.sub.3 OSO.sub.3.sup.-, wherein R.sub.3 is alkyl, cycloalkyl, aryl, aralkyl or heterocyclyl, andwhen R.sub.1 and R.sub.2 are each methyl, X is an anion selected from R.sub.3 SO.sub.3.sup.-, R.sub.3 OSO.sub.3.sup.- wherein R.sub.3 is as defined above and R.sub.4 CO.sub.2.sup.-, wherein R.sub.4 is an aldose or ketose residue, an N-protected .alpha.-amino acid residue or a .omega.-carboxy-.alpha.-amino acid residue.

    摘要翻译： 新型3,7-二取代吩噻嗪鎓盐在含水废水的光化学消毒中具有活性。 所述新型盐具有通式为：其中：R1是糖残基; R 2是烷基，环烷基，芳基，芳烷基或杂环基，任选的烷基或亚烷基链任选被一个或多个杂原子中断，Y是任选被烷基，环烷基，芳基或芳烷基取代的亚烷基; 或R 1和R 2各自为甲基，Y为键; 当R1是糖残基时，X是选自卤素，R3CO2-，R3SO3-和R3OOSO3-的阴离子，其中R3是烷基，环烷基，芳基，芳烷基或杂环基，当R1和R2各自是甲基时，X是阴离子 选自R3SO3-，R3OSO3-，其中R3如上定义，R4CO2-，其中R4是醛糖或酮糖残基，N-保护的α-氨基酸残基或ω-羧基-α-氨基酸残基。

    Process for the production of 1.alpha.-hydroxy provitamin D.sub.3 and 1.alpha.-hydroxy vitamin D.sub.3
    7.
    发明授权
    Process for the production of 1.alpha.-hydroxy provitamin D.sub.3 and 1.alpha.-hydroxy vitamin D.sub.3 失效
    制备1 {60-羟基维生素D {HD 3 {B和1 {60-羟基维生素D {HD 3

    公开(公告)号：US3966777A

    公开(公告)日：1976-06-29

    申请号：US622647

    申请日：1975-10-15

    申请人： Yehuda Mazur ,  Dalia Freeman ,  Aureliu J. Acher

    发明人： Yehuda Mazur ,  Dalia Freeman ,  Aureliu J. Acher

    IPC分类号： C07J9/00 ,  C07J41/00

    CPC分类号： C07J9/00 ,  C07J41/0005 ,  Y10S514/904

    摘要： A process for the production of 1.alpha.-hydroxy provitamin D.sub.3 which comprises treating 1.alpha., 2.alpha.-epoxy-cholesta-4,6-diene-3-one at a low temperature with liquid ammonia; with ammonium chloride and with lithium metal to produce 1.alpha.,3.beta.-dihydroxycholest-6-ene, converting this to the corresponding 1.alpha.,3.beta.-di(lower alkanoyl) derivative, reacting the latter with bromine to give 1.alpha.,3.beta.-di(lower alkanoyloxy) 6.beta.,7.alpha.-dibromocholestane, which is dehydrobrominated to give 1.alpha.,3.beta.-di(lower alkanoyloxy)-cholesta-5,7-diene, which is converted to the desired provitamin. The 1.alpha.,3.beta.-di(lower alkanoyloxy)cholest-6-ene can be oxidized to the corresponding 5-ene-7-one, which is converted to the 7-p-toluenesulfonyl hydrazone derivative, which is converted to the 1.alpha.-hydroxy provitamin D.sub.3 di(lower alkanoyloxy) derivative or to the 1.alpha.-hydroxy provitamin D.sub.3. Novel compounds are 1.alpha.,3.beta.-dihydroxy-cholest-6-ene, its di(lower alkanoyloxy) derivative; 1.alpha.,3.beta.-di(lower alkanoyloxy)-6.beta.,7.alpha.-dibromocholestane; 1.alpha.,3.beta.-diacetoxycholest-5-ene-7-one and the corresponding 7-p-toluenesulfonylhydrazone derivative.

    摘要翻译： 一种生产1α-羟基维生素D3的方法，其包括在低温下用液氨处理1α，2α-环氧 - 胆甾烯-4,6-二烯-3-酮; 与氯化铵和锂金属反应生成1α，3β-二羟基胆甾-6-烯，将其转化成相应的1α，3β-二（低级烷酰基）衍生物，使后者与溴反应，得到1α，3 β-di（低级烷酰氧基）6β，7α-二溴胆固醇，其被脱溴化得到1α，3β-二（低级链烷酰氧基） - 胆甾-5,7-二烯，其转化为所需的维生素。 1α，3β-二（低级烷酰氧基）胆甾-6-烯可以被氧化成相应的5-烯-7-酮，转化为7-对甲苯磺酰腙衍生物，转化为1 α-羟基维生素D3二（低级烷酰氧基）衍生物或1α-羟基维生素D3。 新型化合物为1α，3β-二羟基胆甾-6-烯，其二（低级烷酰氧基）衍生物; 1α，3β-二（低级烷酰氧基）-6β，7α-二溴胆固醇; 1α，3β-二乙酰氧基胆甾-5-烯-7-酮和相应的7-对甲苯磺酰腙衍生物。

    Antiviral agents
    9.
    发明授权
    Antiviral agents 失效
    抗病毒剂

    公开(公告)号：US06576784B1

    公开(公告)日：2003-06-10

    申请号：US08068379

    申请日：1993-05-27

    申请人： Yehuda Mazur ,  Gad Lavie ,  Daniel Meruelo ,  David Lavie

    发明人： Yehuda Mazur ,  Gad Lavie ,  Daniel Meruelo ,  David Lavie

    IPC分类号： C07C6976

    CPC分类号： C07C69/00 ,  C07C2603/00

    摘要： Novel antiviral (including antiretroviral) compounds are mono- or dicarboxylic acid esters of hypericin in which one or both of the methyl groups of hypericin are substituted by carboxylic acid ester groups of the formula COOR3 in which R3 is alkyl, the chain of which is optionally interrupted by one or more oxygen or sulphur atoms. R3 is preferably methyl, ethyl, propyl, butyl, 2-methoxyethyl or 2-(2-methoxyethoxy)ethyl. The compounds may be formulated into pharmaceutical compositions and may be used in any manner which has previously been known for hypericin.

    摘要翻译： 新型抗病毒药（包括抗逆转录酶病毒）化合物是金丝桃素的单酸或二羧酸酯，其中金丝桃碱的一个或两个甲基被式COOR3的羧酸酯基取代，其中R3是烷基，其链可任选地 被一个或多个氧或硫原子中断。 R3优选为甲基，乙基，丙基，丁基，2-甲氧基乙基或2-（2-甲氧基乙氧基）乙基。 化合物可以配制成药物组合物，并且可以以先前已知为金丝桃素的任何方式使用。