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25 条记录 (耗时 0.194 秒)

    Tumor inhibiting gallium compounds
    11.
    发明授权
    Tumor inhibiting gallium compounds 失效
    肿瘤抑制镓化合物

    公开(公告)号：US07019156B2

    公开(公告)日：2006-03-28

    申请号：US10678292

    申请日：2003-10-03

    申请人： Bernhard Keppler

    发明人： Bernhard Keppler

    IPC分类号： C07F5/00 ,  A61K31/555 ,  A01N55/02

    CPC分类号： C07D213/53

    摘要： The invention relates to a compound of the general formula (I) where R1, R2, R3, R4, R1′, R2′, R3′ and R4′ are independently of one another hydrogen, C1–C15-alkyl, C2–C15-alkenyl, C2–C15-alkinyl, C3–C16-cycloalkyl, C3–C16-cycloalkenyl, aryl or a heterocyclus which in each case can be substituted or unsubstituted, Y is a physiologically compatible anion, and n is 1 or 2, as well as its application to the prophylaxis and/or tretment of cancer illnesses.

    摘要翻译： 本发明涉及通式（I）的化合物，其中R 1，R 2，R 3，R 4， R 1，R 2，R 3和R 4独立地为 另一个氢，C 1 -C 15 - 烷基，C 2 -C 15 - 烯基，C 2 -C 15 - C 1 -C 15烷基，C 3 -C 16 - 环烷基，C 3〜 芳基或杂环，其各自可以是取代或未取代的，Y是生理上相容的阴离子，n是1或2，以及其在预防中的应用 和/或缓解癌症疾病。

    Tumor-inhibiting platinum (II) oxalate complexes
    12.
    发明申请
    Tumor-inhibiting platinum (II) oxalate complexes 失效

    公开(公告)号：US20050143455A1

    公开(公告)日：2005-06-30

    申请号：US11011433

    申请日：2004-12-14

    申请人： Bernhard Keppler

    发明人： Bernhard Keppler

    IPC分类号： A61K31/282 ,  A61P35/00 ,  C07C55/07 ,  C07C211/36 ,  C07F9/00 ,  C07F15/00 ,  A61K31/28

    CPC分类号： C07F9/005

    摘要： A tumor-inhibiting platinum (II) oxalate complex and its use as a therapeutic agent are provided, in particular as a tumor-inhibiting medicament. The complex may be compounds of the general formula (I), wherein the substituents R1, R1′, R2, R2′, R3, R3′, R4, and R4′ are independently selected from the group consisting of hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl and unsubstituted or substituted alkylaryl radicals, the substituents R5, R5′, R6, and R6′ are independently selected from the group consisting of hydrogen, unsubstituted or substituted alkyl, and unsubstituted or substituted alkenyl radicals, and wherein optionally in each case at least two of the substituents R1, R1′, R2, R2′, R3, R3′, R4, and R4′ can form with one another at least one unsubstituted or substituted alkylene, unsubstituted or substituted alkenylene radical or an unsubstituted or substituted aromatic ring, and wherein optionally at least one of the carbon atoms of the cyclohexane ring bearing the substituents R1, R1′, R2, R2′, R3, R3′, R4, and R4′ is replaced by a heteroatom, and if the heteroatom is oxygen, the substituents R1, R1′, R2, R2′, R3, R3′, R4, and R4′ can additionally be hydroxy radicals, and pharmaceutically compatible salts of them, provided that at least one of the substituents R1, R1′, R2, R2′, R3, R3′, R4, or R4′ is not equal to hydrogen and the substituents R1 or R1′ and R4 or R4′ do not form any unsubstituted C1-2-alkylene radical with one another.

    Platinum(II) and platinum(IV) complexes and their use
    14.
    发明申请
    Platinum(II) and platinum(IV) complexes and their use 审中-公开
    铂（II）和铂（IV）配合物及其用途

    公开(公告)号：US20050026896A1

    公开(公告)日：2005-02-03

    申请号：US10786924

    申请日：2004-02-24

    申请人： Bernhard Keppler

    发明人： Bernhard Keppler

    IPC分类号： A61P35/00 ,  C07F15/00 ,  A61K31/555 ,  A61K31/28

    CPC分类号： C07F15/0093

    摘要： Platinum(II) complexes are provided selected from the group consisting of compounds of the general formulae I to IV and physiologically acceptable addition salts thereof, wherein the radicals R1 to R4, R1′ to R3′, X, X′, Y, a, i, k and n are defined as in the description, and mixtures of the compounds for use as prophylactic and/or therapeutic agents for the treatment of diseases, and cytostatic platinum complexes with the general formulae [PtII(NH3)n(A)n(Z)2-n] or [PtIV(NH3)n(A)n(Z)2-nX2]and [PtII(A)1(Z)2] or [PtIV(A)1(Z)2X2]wherein A, Z and n are as defined in the description.

    摘要翻译： 铂（II）络合物选自由通式I至IV的化合物及其生理上可接受的加成盐组成的组，其中基团R 1至R 4，R 1至R 3 '，X，X'，Y，a，i，k和n如描述中所定义，并且用作治疗疾病的预防和/或治疗剂的化合物和与 通式[Pt II（NH 3）n（A）n（Z）2-n]或[PtⅣ（NH 3）n（A）n（Z）2-nX 2]和[ A）1（Z）2]或[PtⅣ（A）1（Z）2X2]其中A，Z和n如说明书中所定义。

    Lectin conjugates
    17.
    发明申请
    Lectin conjugates 审中-公开
    凝集素缀合物

    公开(公告)号：US20060251580A1

    公开(公告)日：2006-11-09

    申请号：US11294963

    申请日：2005-12-06

    申请人： Bernhard Keppler ,  Paul Debbage ,  Wolfgang Buchberger

    发明人： Bernhard Keppler ,  Paul Debbage ,  Wolfgang Buchberger

    IPC分类号： A61K51/00 ,  A61K49/10 ,  C07K14/47 ,  C07K16/46

    CPC分类号： A61K49/14 ,  A61K49/085 ,  A61K49/1863 ,  A61K49/1881 ,  B82Y5/00

    摘要： A conjugate includes at least one target-seeking unit, which specifically binds to receptors on the surface of endothelial cells, and at least one effector unit which is coupled to the unit by a linker. The effector unit exhibits at least one signal unit and optionally at least one therapeutic active substance. The target-seeking unit includes a lectin or a fragment or derivative thereof, wherein the lectin is not L-selectin and the signal unit includes a lanthanide ion.

    摘要翻译： 缀合物包括与内皮细胞表面上的受体特异性结合的至少一个寻靶单位，以及通过连接体与该单元偶联的至少一个效应子单元。 效应器单元表现出至少一个信号单元和任选的至少一种治疗活性物质。 靶寻求单元包括凝集素或其片段或衍生物，其中所述凝集素不是L-选择素，并且所述信号单元包括镧系元素离子。

    Mental complexes having an antineoplastic action, and medicaments containing these complexes
    18.
    发明授权
    Mental complexes having an antineoplastic action, and medicaments containing these complexes 失效
    具有抗肿瘤作用的精神复合物，以及含有这些复合物的药物

    公开(公告)号：US4578401A

    公开(公告)日：1986-03-25

    申请号：US491337

    申请日：1983-04-29

    申请人： Heimo Keller ,  Bernhard Keppler ,  Uwe Kruger ,  Rudolf Linder

    发明人： Heimo Keller ,  Bernhard Keppler ,  Uwe Kruger ,  Rudolf Linder

    IPC分类号： A61K9/14 ,  A61K9/18 ,  A61K31/28 ,  A61K31/74 ,  A61P35/00 ,  C07F7/00 ,  C07F7/28 ,  A01N55/04 ,  A61K31/32

    CPC分类号： A61K31/28 ,  A61K31/74 ,  A61K9/145 ,  A61K9/146 ,  C07F7/006

    摘要： Metal complexes of the general formula I[R.sup.1 (CH.sub.2).sub.m C(O)CR.sup.3 C(O)R.sup.2 ].sub.2 M(OR.sup.4).sub.2-n X.sub.n (I)wherein M denotes titanium, zirconium or hafnium, R.sup.1 denotes hydrogen, C.sub.1 -C.sub.8 -alkyl or phenyl, which can be monosubstituted or polysubstituted by fluorine, chlorine, bromine, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or trifluoromethyl, R.sup.2 denotes C.sub.1 -C.sub.8 -alkyl, or phenyl, which can be monosubstituted or polysubstituted by fluorine, chlorine, bromine, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or trifluoromethyl, R.sup.3 denotes hydrogen or phenyl, R.sup.4 denotes C.sub.1 -C.sub.18 -alkyl, which can be substituted by hydroxyl, C.sub.1 -C.sub.3 -alkylamino or alkali metal sulfonato groups, or denotes C.sub.5 -C.sub.8 -cycloalkyl, which can be substituted by C.sub.1 -C.sub.5 -alkyl groups, hydroxyl or alkali metal sulfonato groups, X denotes fluorine, chlorine or bromine, m denotes the number 0 or 1, but does not denote 0 if R.sup.1 denotes hydrogen, and n denotes the number 0 or 1, and, if a radical R.sup.4 contains an amino group, hydrohalides thereof, exhibit a very good cytostatic activity, coupled with low toxicity. They are suitable for the production of medicaments having an antineoplastic action.

    摘要翻译： PCT No.PCT / EP82 / 00184 Sec。 371日期：1983年4月29日 102（e）日期1983年4月29日PCT申请日1982年8月28日PCT公布。 出版物WO83 / 00868 日期：1983年3月17日。通式I [R1（CH2）mC（O）CR3C（O）R2] 2M（OR4）2-nXn（I）的金属配合物，其中M表示钛，锆或铪，R1表示 氢，C 1 -C 8 - 烷基或苯基，其可以被氟，氯，溴，硝基，C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基或三氟甲基单取代或多取代，R 2表示C 1 -C 8烷基或苯基， 其可以被氟，氯，溴，硝基，C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基或三氟甲基单取代或多取代，R 3表示氢或苯基，R 4表示可以被羟基取代的C 1 -C 18烷基， C 1 -C 3 - 烷基氨基或碱金属磺酸基，或表示可被C 1 -C 5 - 烷基，羟基或碱金属磺酸基取代的C 5 -C 8 - 环烷基，X表示氟，氯或溴，m表示数 0或1，但如果R 1表示氢，并且n表示数字0或1，则不表示0，如果基团R 4含有氨基，则其氢卤化物表现出非常好的氰化物 静止活动，加上低毒性。 它们适用于生产具有抗肿瘤作用的药物。

    Anticancer compositions, and methods of making and using the same
    20.
    发明授权
    Anticancer compositions, and methods of making and using the same 有权
    抗癌组合物及其制备和使用方法

    公开(公告)号：US07485659B2

    公开(公告)日：2009-02-03

    申请号：US11696116

    申请日：2007-04-03

    申请人： Bernhard Keppler

    发明人： Bernhard Keppler

    IPC分类号： A61K31/415 ,  C07D231/56

    CPC分类号： C07F15/0053 ,  A61K31/28 ,  A61K31/415 ,  A61K31/416 ,  A61K33/00 ,  A61K33/02 ,  A61K33/14 ,  A61K33/24 ,  A61K45/06 ,  C07D231/56 ,  A61K2300/00

    摘要： Compositions, containing a ruthenium(III) complex and a heterocycle, methods for their manufacture, medicament containing these compositions and a kit.The invention relates to a composition (A), obtained by reacting a compound of the general formula (I) M3−n−p−2pr[RUX6−n−p−q−2rBn(H2O)p(OH)q(O)r]2r+1  (I) with a compound of the general formula (II) B′(HX′)s  (II). Furthermore, the invention relates to a composition (B), obtained by mixing a compound of the general formula (III) (B′H)3−n−p−2pr[RUX6−n−p−q−2rBn(H2O)p(OH)q(O)r]2r+1  (III) with a compound of the general formula (IV) MX′  (IV).

    摘要翻译： 包含钌（III）络合物和杂环的组合物，其制备方法，含有这些组合物的药物和试剂盒。 本发明涉及通过使通式（I）的化合物<？in-line-formula description =“In-Line Formulas”end =“lead”→> M3-np-2pr [ RUX6-npq-2rBn（H2O）p（OH）q（O）r] 2r + 1（I）<？在线公式描述=“在线公式”end =“tail” 通式（II）<？in-line-formula description =“In-line Formulas”end =“lead”？> B'（HX'）s（II）<？in-line-formula description =“In 另外，本发明涉及通过将通式（III）的化合物<？in-line-formula description =“In-Line Formulas”（混合）得到的组合物（B） （B'H）3-np-2pr [RUX6-npq-2rBn（H2O）p（OH）q（O）r] 2r + 1（III）<β在线公式描述 =“在线公式”end =“tail”？>与通式（IV）的化合物<？in-line-formula description =“In-line Formulas”end =“lead”？> MX'（IV ）。<？in-line-formula description =“In-line Formulas”end =“tail”？>