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1. 发明授权

US07358266B2 Cyclopropyl and cyclobutyl epothilone analogs 失效
标题翻译：环丙基和环丁基埃博霉素类似物
公开(公告)号：US07358266B2
公开(公告)日：2008-04-15
申请号：US10227073
申请日：2002-08-23
申请人： Kyriacos C. Nicolaou , Kenji Namoto , Andreas Ritzen , Mitsuru Shoji , Trond Ulven , Karl-Heinz Altmann
发明人： Kyriacos C. Nicolaou , Kenji Namoto , Andreas Ritzen , Mitsuru Shoji , Trond Ulven , Karl-Heinz Altmann
IPC分类号： A61K31/425 , C07D277/30 , D27
CPC分类号： C07D495/08 , C07D313/00 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12
摘要： The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IV wherein Ar is a radical represented by the following structure: and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.
摘要翻译：本发明涉及式I至IV的顺式 - 和反式12,13-环丙基和12,13-环丁基埃坡霉素，其中Ar是由以下结构表示的基团：其它基团和符号具有如本文所定义的含义; 对其化学合成和生物学评价; 它们在治疗肿瘤疾病中的用途以及含有这些化合物的药物制剂。本文所述的化合物是有效的微管蛋白聚合启动子和细胞毒性剂。

2. 发明授权

US07825141B2 Epothilone derivatives 失效
标题翻译：埃博霉素衍生物
公开(公告)号：US07825141B2
公开(公告)日：2010-11-02
申请号：US10591921
申请日：2005-03-15
申请人： Karl-Heinz Altmann
发明人： Karl-Heinz Altmann
IPC分类号： A61K31/426 , C07D277/20
CPC分类号： C07D493/04
摘要： Epothilone derivatives of Formula (I) and their use as a pharmaceutical.
摘要翻译：式（I）的埃坡霉素衍生物及其作为药物的用途。

3. 发明申请

US20090191264A1 EPOTHILONE COMPOSITIONS 审中-公开
标题翻译： EPOTHILONE组合物
公开(公告)号：US20090191264A1
公开(公告)日：2009-07-30
申请号：US12417717
申请日：2009-04-03
申请人： Jean-Claude Sonntag , Markus Wartmann , Karl-Heinz Altmann
发明人： Jean-Claude Sonntag , Markus Wartmann , Karl-Heinz Altmann
IPC分类号： A61K9/127 , A61K31/425
CPC分类号： A61K9/127 , A61K9/1271 , A61K31/427
摘要： This invention provides liposomal compositions comprising an epothilone.
摘要翻译：本发明提供包含埃坡霉素的脂质体组合物。

4. 发明申请

US20050159374A1 2'-Substituted nucleosides and oligonucleotide derivatives 审中-公开
标题翻译： 2'-取代的核苷和寡核苷酸衍生物
公开(公告)号：US20050159374A1
公开(公告)日：2005-07-21
申请号：US10696488
申请日：2003-10-29
申请人： Bernard Cuenoud , Karl-Heinz Altmann , Pierre Martin , Heinz Moser
发明人： Bernard Cuenoud , Karl-Heinz Altmann , Pierre Martin , Heinz Moser
IPC分类号： C12N15/09 , C07H21/00 , A61K48/00 , C07H21/02 , C12Q1/68
CPC分类号： C07H21/00
摘要： The invention relates to an oligonucleotide derivative which comprises at least one nucleoside building block of the formula (I) The invention furthermore relates to nucleoside building blocks, intermediates and processes for preparing the oligonucleotide derivatives and the nucleoside building blocks. The invention also relates to pharmaceutical compositions and to uses of the oligonucleotide derivatives and the nucleoside building blocks.
摘要翻译：本发明涉及包含至少一种式（I）核苷结构单元的寡核苷酸衍生物。本发明还涉及核苷结构单元，中间体和制备寡核苷酸衍生物和核苷结构单元的方法。本发明还涉及药物组合物以及寡核苷酸衍生物和核苷结构单元的用途。

5. 发明授权

US06329519B1 Intermediates for oligonucleotide synthesis 有权
标题翻译：寡核苷酸合成中间体
公开(公告)号：US06329519B1
公开(公告)日：2001-12-11
申请号：US09202294
申请日：1999-03-15
申请人： Stephen Paul Collingwood , Heinz Ernst Moser , Karl-Heinz Altmann , Mark Edward Douglas
发明人： Stephen Paul Collingwood , Heinz Ernst Moser , Karl-Heinz Altmann , Mark Edward Douglas
IPC分类号： C07H1920
CPC分类号： C07H19/04 , Y02P20/55
摘要： A compound of formula (I) wherein B1 is a radical of a nucleoside base, R1 is hydrogen or a hydroxy-protecting group, R2 is hydrogen, hydroxy or a 2′-nucleoside-modifying atom or group, R3 is an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, and Z is halogen or a group of formula (II) where R4 and R5 are each independently an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, or R4 is said group and R5 is hydrogen or R4 and R5 together with the nitrogen atom to which they are attached denote a five- to thirteen-membered heterocyclic ring, or Z is a group of formula (III): Nuc-O—, where Nuc is the residue of a natural or synthetic nucleoside or oligonucleotide after removal of a 5′-hydroxyl group therefrom attached through a 5′-methylene thereof to the indicated oxygen atom.
摘要翻译：式（I）的化合物，其中B1是核苷碱基的基团，R1是氢或羟基保护基，R2是氢，羟基或2'-核苷修饰的原子或基团，R3是未取代或取代的 C1至C10烷基，C2至C10烯基，C4至C10环烷基烷基，C6至C10芳基或C7至C13芳烷基，Z为卤素或式（Ⅱ）基团，其中R4和R5各自独立地为未取代或取代的C1 C 10至C 10链烯基，C 4至C 10环烷基烷基，C 6至C 10芳基或C 7至C 13芳烷基，或R 4为所述基团，R 5为氢或R 4和R 5与它们所连接的氮原子一起表示 5至13元杂环，或Z为式（III）的基团：Nuc-O-，其中Nuc是除去其中的5'-羟基之后天然或合成的核苷或寡核苷酸的残基，其通过其指示氧原子的5'-亚甲基。

6. 发明授权

US07002022B2 N-Aryl (thio) anthranilic acid amide derivatives, their preparation and their use as VEGF 失效
标题翻译： N-芳基（硫代）邻氨基苯甲酸酰胺衍生物，其制备及其作为VEGF的用途
公开(公告)号：US07002022B2
公开(公告)日：2006-02-21
申请号：US10828951
申请日：2004-04-21
申请人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
发明人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
IPC分类号： C07C49/76 , C07C49/786 , C07C49/82 , C07C49/825 , C07C49/884
CPC分类号： A61K31/415 , A61K31/44 , A61K31/47 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/89 , C07D215/12 , C07D233/54 , C07D405/12
摘要： Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R2 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y=SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.
摘要翻译：描述的是式（I）的化合物，其中W是O或S; X是NR 8; Y为CR 9 R 10 - （CH 2）n其中R 9和R 10为氢， / SUB>彼此独立地为氢或低级烷基，n为0〜3的整数。或Y为SO 2; R 2是芳基; R 2是包含一个或多个环氮原子的单环或双环杂芳基，除了R 2不能表示2-邻苯二甲酰亚氨基，并且在Y = SO的情况下 2不能表示2,1,3-苯并噻二唑-4-基; R 3，R 4，R 5和R 6中的任何一个独立地是H或除氢以外的取代基; 和R 7和R 8彼此独立地为H或低级烷基; 或N-氧化物或其药学上可接受的盐在制备用于治疗对VEGF受体酪氨酸激酶活性的抑制作出反应的肿瘤疾病的药物产品中的用途。式（I）化合物可用于治疗，例如，的肿瘤疾病，如肿瘤疾病，视网膜病变和年龄相关性黄斑变性。

7. 发明申请

US20050042275A1 Epothilone compositions 审中-公开
标题翻译：埃坡霉素组合物
公开(公告)号：US20050042275A1
公开(公告)日：2005-02-24
申请号：US10937056
申请日：2004-09-09
申请人： Jean-Claude Sonntag , Markus Wartmann , Karl-Heinz Altmann
发明人： Jean-Claude Sonntag , Markus Wartmann , Karl-Heinz Altmann
IPC分类号： A61K9/127 , A61K31/427
CPC分类号： A61K9/127 , A61K9/1271 , A61K31/427
摘要： The present invention provides pharmaceutical liposomal compositions comprising epothilones.
摘要翻译：本发明提供包含埃坡霉素的药物脂质体组合物。

8. 发明授权

US5948898A Methoxyethoxy oligonucleotides for modulation of protein kinase C expression 失效
标题翻译：用于调节蛋白激酶C表达的甲氧基乙氧基寡核苷酸
公开(公告)号：US5948898A
公开(公告)日：1999-09-07
申请号：US601269
申请日：1996-02-14
申请人： Nicholas M. Dean , Pierre Martin , Karl-Heinz Altmann
发明人： Nicholas M. Dean , Pierre Martin , Karl-Heinz Altmann
IPC分类号： C12N15/09 , A61K31/00 , A61K31/70 , A61K31/7088 , A61K31/712 , A61K38/00 , A61K48/00 , A61P17/00 , A61P17/06 , A61P29/00 , A61P35/00 , C07H21/00 , C12N9/12 , C12N15/113 , C12Q1/68 , C07H21/04
CPC分类号： C12N15/1137 , C07H21/00 , C12N9/12 , C12Q1/6876 , C12Q1/6883 , C12Y207/11013 , A61K38/00 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/341 , C12N2310/346 , C12N2310/3521 , C12N2310/3527 , C12N2310/3533
摘要： Compositions and methods are provided for modulating the expression of protein kinase C. Oligonucleotides are provided which are targeted to nucleic acids encoding PKC. The oligonucleotides contain a methoxyethoxy (--O--CH.sub.2 CH.sub.2 OCH.sub.3) modification at the 2' position of at least one nucleotide. Methods of inhibiting PKC expression and methods of treating conditions associated with expression of PKC using oligonucleotides of the invention are disclosed.
摘要翻译：提供组合物和方法用于调节蛋白激酶C的表达。提供靶向编码PKC的核酸的寡核苷酸。寡核苷酸在至少一个核苷酸的2'位置含有甲氧基乙氧基（-O-CH 2 CH 2 OCH 3）修饰。公开了使用本发明的寡核苷酸抑制PKC表达的方法和治疗与PKC表达相关的病症的方法。

9. 发明授权

US5744362A Antisense oligonucleotide modulation of raf gene expression 失效
公开(公告)号：US5744362A
公开(公告)日：1998-04-28
申请号：US463912
申请日：1995-06-05
申请人： Brett P. Monia , Pierre Martin , Karl-Heinz Altmann
发明人： Brett P. Monia , Pierre Martin , Karl-Heinz Altmann
IPC分类号： C07H21/04 , A61K31/70 , A61K31/7088 , A61K38/00 , A61K48/00 , A61P9/00 , A61P9/10 , A61P17/00 , A61P17/06 , A61P35/00 , A61P35/02 , A61P43/00 , C07H21/00 , C12N15/09 , C12N15/113 , C07H21/02 , C12N5/08
CPC分类号： C12N15/1135 , C07H21/00 , A61K38/00 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/3341 , C12N2310/341 , C12N2310/346 , C12N2310/3517
摘要： Oligonucleotides are provided which are targeted to nucleic acids encoding human c-raf and capable of inhibiting raf expression. The oligonucleotides contain a methoxyethoxy (2'-O--CH.sub.2 CH.sub.2 OCH.sub.3) modification at the 2' position of at least one nucleotide. Methods of inhibiting the expression of human raf using oligonucleotides of the invention are also provided. The present invention further comprises methods of inhibiting hyperproliferation of cells and methods of treating abnormal proliferative conditions which employ oligonucleotides of the invention.

10. 发明授权

US06710047B2 Phthalazines with angiogenesis inhibiting activity 失效
标题翻译：具有血管生成抑制活性的酞嗪类
公开(公告)号：US06710047B2
公开(公告)日：2004-03-23
申请号：US10338062
申请日：2003-01-07
申请人： Guido Bold , Jörg Frei , Peter Traxler , Karl-Heinz Altmann , Helmut Mett , David Raymond Stover , Jeanette Marjorie Wood
发明人： Guido Bold , Jörg Frei , Peter Traxler , Karl-Heinz Altmann , Helmut Mett , David Raymond Stover , Jeanette Marjorie Wood
IPC分类号： A61K31495
CPC分类号： C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D471/04
摘要： The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etheritied or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, or alkylphenylsulfony; and wherein the bonds characterized by a wavy line are either single or double bonds; or an N-oxide of said compound with the stipulation that, if Y is pyridyl or unsubstituted cycloalkyl, X is imino, and the remaining radicals are as defined, then G is selected from the group comprising lower alkylene, —CH2—O—, —CH2—S—, oxa and thia; or a salt thereof. The compounds inhibit angiogenesis.
摘要翻译：本发明涉及式I化合物，其中r为0至2，n为0至2; m为0〜4; R1和R2（i）在每种情况下都是低级烷基，或（ii）一起在子式I *中形成桥，或（iii）一起形成子式I **中的桥，其中一个或两个环成员T1，T2 ，T3和T4是氮，余数分别为CH; A，B，D和E是N或CH，其中不多于2个这些基团是N; G是低级亚烷基，酰氧基或羟基 - 低级亚烷基，-CH 2 -O-，-CH 2 -S-，-CH 2 -NH-，氧杂，硫杂或亚氨基; Q是甲基; R是H或低级烷基; X是亚氨基，氧杂或硫杂; Y是芳基，吡啶基或（未）取代的环烷基; 羟基，醚基或酯化的羟基，硝基，氰基，羧基，酯化的羧基，烷酰基，氨基甲酰基，N-单或N，N-二取代的氨基甲酰基，脒基，胍基，巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯硫基，苯基亚磺酰基，苯基 - 低级烷基亚磺酰基，烷基苯基亚磺酰基，苯基磺酰基，苯基 - 低级烷基磺酰基或烷基苯基磺酰基。并且其中以波浪线表征的键是单键或双键; 或所述化合物的N-氧化物，其规定如果Y是吡啶基或未取代的环烷基，则X是亚氨基，剩余的基团如所定义，则G选自低级亚烷基，-CH 2 -O-， -CH 2 -S-，氧杂和硫杂; 或其盐。该化合物抑制血管发生。

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