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公开(公告)号：US20040223915A1
公开(公告)日：2004-11-11
申请号：US10773928
申请日：2004-02-06
发明人： Bernhard Keppler
IPC分类号： C07F005/00 , A61K031/555
CPC分类号： C07F5/003
摘要： The invention relates to cerium compounds having general formulas (I) RninullYinnull and (II) RbnullYbnull and their application as medicaments in the prophylaxis and/or treatment of cancer diseases. In formula (I), R is a group of general formula (A): 1 and in formula (II), Rb is a group of general formula (B) 2
摘要翻译： 本发明涉及具有通式（I）RnⅪn和（Ⅱ）Rb + Yb +）的铈化合物及其在预防和/或治疗癌症疾病中的用途。 式（I）中，R为通式（A）的基团：式（II）中，R b为通式（B）的基团，
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公开(公告)号：US20040176346A1
公开(公告)日：2004-09-09
申请号：US10773823
申请日：2004-02-06
发明人： Bernhard Keppler
IPC分类号： C07F005/00 , A61K031/555
CPC分类号： C07F5/069
摘要： Lanthanum compounds are provided having general formulas (I) RninullYinnull and (II) RbnullYbnull which may be used as medicaments in the prophylaxis and/or treatment of cancer diseases. In formula (I), R is a group of general formula (A): 1 and in general formula (II) Rb is a group of general formula (B): 2
摘要翻译： 提供了可用作预防和/或治疗癌症疾病的药物的具有通式（I）RnⅪi和（Ⅱ）Rb + Yb - 的镧化合物。 式（I）中，R为通式（A）的基团：通式（II）中Rb为通式（B）的基团：
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公开(公告)号：US20030118600A1
公开(公告)日：2003-06-26
申请号：US10152212
申请日：2002-05-20
IPC分类号： A61K048/00 , C12P021/02 , C12N005/06 , C07H021/04 , A61K039/00 , C07K014/47
CPC分类号： C12N15/87 , A61K38/00 , C07K14/4738 , C07K2319/00
摘要： The invention relates to the use of a carboxy-terminal fragment of the Ki-67 protein or of an active part, fragment or homologue thereof as a compound that can be used for intracellular transfer and for the introduction in and the release by the cells. The invention further relates to transfer compounds that contain the above-mentioned Ki-67 protein and to the vectors encoding the same. The invention also relates to corresponding pharmaceutical compositions and to the use of the transfer protein as an excipient or active agent in the treatment of diseases.
摘要翻译： 本发明涉及Ki-67蛋白或其活性部分，其片段或同源物的羧基末端片段作为可用于细胞内转移和引入细胞释放的化合物的用途。 本发明还涉及含有上述Ki-67蛋白质的转移化合物及其编码载体。 本发明还涉及相应的药物组合物以及转运蛋白作为赋形剂或活性剂在治疗疾病中的用途。
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公开(公告)号：US20070293468A1
公开(公告)日：2007-12-20
申请号：US11696114
申请日：2007-04-03
申请人： Bernhard Keppler
发明人： Bernhard Keppler
IPC分类号： A61K31/555 , A61P35/00 , C07F15/00
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”→> np-2pr [RuX 6-npq-2r] B n（H 2 O）p（n） （OH）q（O）R 2] 2r + 1（I）<？在线公式描述=“在线公式 “end =”tail“？>与通式（II）的化合物<？in-line-formula description =”In-line Formulas“end =”lead“？> B'（HX'） （II）。 另外，本发明涉及通过将通式（III）的化合物＆lt;＆lt;＆lt;＆lt; line-formula description =“In-line Formulas”end =“lead”？>（B'H）3-np-2pr
（III）<β在线式描述=“In-line formula”end =“tail” line-formula description =“In-line Formulas”end =“lead”？> MX'（IV）。<？in-line-formula description =“In-line Formulas”end =“tail”？> -
公开(公告)号：US07057059B2
公开(公告)日：2006-06-06
申请号：US11011433
申请日：2004-12-14
申请人： Bernhard Keppler
发明人： Bernhard Keppler
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.
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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。
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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.
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公开(公告)号：US20050032801A1
公开(公告)日：2005-02-10
申请号：US10627519
申请日：2003-07-25
申请人： Bernhard Keppler
发明人： Bernhard Keppler
IPC分类号： C07D231/56 , A61K9/08 , A61K31/416 , A61K33/24 , A61K45/06 , A61K47/02 , A61P35/00 , A61P35/04 , C07F15/00 , A61K31/50 , A61K31/4965 , A61K31/505
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M3-np-2pr [RuX6-npq-2rBn（H2O）p（OH）q（O）r] 2r + 1（ I）与通式（II）B'（HX'）S（II）的化合物反应。 此外，本发明涉及通过将通式（III）的化合物（B'H）3-np-2pr [RuX6-npq-2rBn（H2O）p（OH）q（O） ）r] 2r + 1（III）与通式（IV）的化合物MX'（IV）反应。
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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。
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