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    PYRIDO(3,2-D)PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS USEFUL FOR MEDICAL TREATMENT
    1.
    发明申请
    PYRIDO(3,2-D)PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS USEFUL FOR MEDICAL TREATMENT 审中-公开
    吡哆醛（3,2-D）嘧啶和药物治疗有用的药物组合物

    公开(公告)号：US20080004285A1

    公开(公告)日：2008-01-03

    申请号：US11771924

    申请日：2007-06-29

    申请人： Steven De Jonghe ,  Eduard Dolusic ,  Ling-Jie Gao ,  Piet Andre Herdewijn ,  Wolfgang Pfleiderer

    发明人： Steven De Jonghe ,  Eduard Dolusic ,  Ling-Jie Gao ,  Piet Andre Herdewijn ,  Wolfgang Pfleiderer

    IPC分类号： A61K31/519 ,  C07D487/02

    CPC分类号： C07D471/04

    摘要： This invention relates to substituted pyrido(3,2-d)pyrimidine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These derivatives are also useful in preventing or treating cardiovascular disorders, disorders of the central nervous system, TNF-α related disorders, viral diseases (including hepatitis C), erectile dysfunction and cell proliferative disorders.

    摘要翻译： 本发明涉及取代吡啶并（3,2-d）嘧啶衍生物，它们的药学上可接受的盐，N-氧化物，溶剂合物，前药和对映异构体，其特别是具有高度活性的免疫抑制剂，以及作为 这在治疗移植排斥和/或某些炎性疾病的治疗中是有用的。 这些衍生物也可用于预防或治疗心血管疾病，中枢神经系统疾病，TNF-α相关病症，病毒性疾病（包括丙型肝炎），勃起功能障碍和细胞增殖性疾病。

    Immunosuppressive effects of pteridine derivatives
    2.
    发明申请
    Immunosuppressive effects of pteridine derivatives 审中-公开
    蝶啶衍生物的免疫抑制作用

    公开(公告)号：US20060189620A1

    公开(公告)日：2006-08-24

    申请号：US11275601

    申请日：2006-01-18

    申请人： Mark Jozef Waer ,  Piet Andre Herdewijn ,  Wolfgang Pfleiderer

    发明人： Mark Jozef Waer ,  Piet Andre Herdewijn ,  Wolfgang Pfleiderer

    IPC分类号： A61K31/525 ,  C07D475/12

    CPC分类号： C07D475/10 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K38/13 ,  C07D471/04 ,  C07D475/04 ,  C07D475/08 ,  A61K2300/00

    摘要： This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydroderivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.

    摘要翻译： 本发明涉及一组三取代和四取代的蝶啶衍生物，其药学上可接受的盐，N-氧化物，溶剂化物，二氢和四氢衍生物和对映异构体，具有特别期望的药物性质，特别是高活性免疫抑制剂，因此是 可用于移植排斥和/或治疗某些炎性疾病的治疗。 这些化合物也可用于预防或治疗心血管疾病，过敏性疾病，中枢神经系统疾病和细胞增殖性疾病。

    Pteridine nucleotide analogs
    3.
    发明授权
    Pteridine nucleotide analogs 失效
    蝶啶核苷酸类似物

    公开(公告)号：US06716971B1

    公开(公告)日：2004-04-06

    申请号：US09786666

    申请日：2001-06-15

    申请人： Mary E. Hawkins ,  Wolfgang Pfleiderer ,  Frank Balis

    发明人： Mary E. Hawkins ,  Wolfgang Pfleiderer ,  Frank Balis

    IPC分类号： C07H2100

    CPC分类号： C07H21/00 ,  C12Q1/6816 ,  C12Q2565/107 ,  C12Q2563/107 ,  C12Q2525/301 ,  C12Q2531/113 ,  C12Q2561/119

    摘要： The invention provides pteridine nucleotides of formula (I) which are highly fluorescent and which can be used in the chemical synthesis of fluorescent oligonucleotide. The invention further provides for fluorescent oligonucleotide comprising one or more pteridine nucleotides. In addition the invention provides for pteridine nucleotide triphosphates which may be used as the constituent monomers in DNA amplification procedures. The pteridine nucleotides are more stable and possess higher quantum yields than structurally similar pteridine nucleotides.

    摘要翻译： 本发明提供了高度荧光的式（I）的蝶啶核苷酸，可用于荧光寡核苷酸的化学合成。 本发明还提供了包含一个或多个蝶啶核苷酸的荧光寡核苷酸。 此外，本发明提供了可用作DNA扩增方法中构成单体的蝶啶核苷三磷酸。 蝶啶核苷酸比结构上类似的蝶啶核苷酸更稳定，具有更高的量子产率。

    Base-modified derivatives of 2′,5′-oligoadenylate and antiviral uses thereof
    4.
    发明授权
    Base-modified derivatives of 2′,5′-oligoadenylate and antiviral uses thereof 有权
    2'，5'-寡聚腺苷酸的碱基修饰的衍生物及其抗病毒用途

    公开(公告)号：US06281201B1

    公开(公告)日：2001-08-28

    申请号：US09445552

    申请日：1999-12-08

    申请人： Robert J. Suhadolnik ,  Wolfgang Pfleiderer

    发明人： Robert J. Suhadolnik ,  Wolfgang Pfleiderer

    IPC分类号： A61K3170

    CPC分类号： C07H21/00 ,  C07H21/02 ,  C07H21/04

    摘要： Antiviral compounds have the formula wherein m is zero, 1, 2 or 3; n is from 1 to 8, preferably 1, 2 or 3; most preferably 1 or 2; R is independently selected from the group consisting of  provided that all R may not be R1 is independently selected from the group consisting of hydroxyl and hydrogen; R2 is independently selected from the group consisting of oxygen and sulfur; or water soluble salts thereof.

    摘要翻译： 抗病毒化合物的制备方法为零，1,2或3; n为1至8，优选1,2或3; 最优选1或2; R独立地选自由以下组成的组：所有R不为R 1独立地选自羟基和氢; R 2独立地选自氧和硫;或水溶性 的盐。

    Process for the manufacture of 4-amino-3-aminomethylpiperidine
    7.
    发明授权
    Process for the manufacture of 4-amino-3-aminomethylpiperidine 失效
    制备4-氨基-3-氨基甲基哌啶的方法

    公开(公告)号：US3971792A

    公开(公告)日：1976-07-27

    申请号：US477890

    申请日：1974-06-10

    申请人： Helmut Zondler ,  Wolfgang Pfleiderer

    发明人： Helmut Zondler ,  Wolfgang Pfleiderer

    IPC分类号： C07D211/98

    摘要： The new compound 4-amino-3-aminomethylpiperidine is manufactured by hydrogenating 4-amino-3-cyano-1,2,5,6-tetrahydropyridine under pressure and in the presence of ammonia and a hydrogenation catalyst. The 4-amino-3-cyano-1,2,5,6-tetrahydropyridine used as the starting substance can be obtained by cyclization of bis-cyanoethylenated ammonia. The new compound 4-amino-3-aminomethylpiperidine represents a valuable curing agent for epoxide resins, and advantageously 0.5 to 1.3 equivalents of nitrogen-bonded active hydrogen atoms of the 4-amino-3-aminomethylpiperidine are used per 1 equivalent of epoxide groups of the polyepoxide compound.

    摘要翻译： 通过在压力和氨和氢化催化剂的存在下氢化4-氨基-3-氰基-1,2,5,6-四氢吡啶来制备新的化合物4-氨基-3-氨基甲基哌啶。 用作起始物质的4-氨基-3-氰基-1,2,5,6-四氢吡啶可以通过双氰基乙烯化氨的环化获得。 新化合物4-氨基-3-氨基甲基哌啶代表环氧树脂的有价值的固化剂，并且每1当量的环氧化物基团使用4-氨基-3-氨基甲基哌啶的0.5至1.3当量的氮键合的活性氢原子。 聚环氧化合物。

    NOVEL PHOTOLABILE PROTECTIVE GROUPS FOR IMPROVED PROCESSES TO PREPARE OLIGONUCLEOTIDE ARRAYS
    9.
    发明申请
    NOVEL PHOTOLABILE PROTECTIVE GROUPS FOR IMPROVED PROCESSES TO PREPARE OLIGONUCLEOTIDE ARRAYS 有权
    改进方法制备寡核苷酸阵列的新型可溶性保护基

    公开(公告)号：US20100292458A1

    公开(公告)日：2010-11-18

    申请号：US12792122

    申请日：2010-06-02

    申请人： Sigrid BÜHLER ,  Markus Ott ,  Wolfgang Pfleiderer

    发明人： Sigrid BÜHLER ,  Markus Ott ,  Wolfgang Pfleiderer

    IPC分类号： C07H19/173 ,  C07H19/073 ,  C07C205/06 ,  C07C69/76 ,  C07C63/04

    CPC分类号： C07H13/12 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  Y02P20/55

    摘要： The present invention discloses novel and improved nucleosidic and nucleotidic compounds that are useful in the light-directed synthesis of oligonucleotides, as well as, methods and reagents for their preparation. These compounds are characterized by novel photolabile protective groups that are attached to either the 5′- or the 3′-hydroxyl group of a nucleoside moiety. The photolabile protective group is comprised of a 2-(2-nitrophenyl)-ethyoxycarbonyl skeleton with at least one substituent on the aromatic ring that is either an aryl, an aroyl, a heteroaryl or an alkoxycarbonyl group. The present invention includes the use of the aforementioned compounds in light-directed oligonucleotide synthesis, the respective assembly of nucleic acid microarrays and their application.

    摘要翻译： 本发明公开了可用于寡核苷酸的光定向合成的新型和改进的核苷和核苷酸化合物，以及其制备方法和试剂。 这些化合物的特征在于与核苷部分的5'-或3'-羟基连接的新的光不稳定保护基。 光不稳定保护基由在芳环上具有芳基，芳酰基，杂芳基或烷氧基羰基的至少一个取代基的2-（2-硝基苯基） - 乙氧基羰基骨架组成。 本发明包括上述化合物在光导寡核苷酸合成中的用途，核酸微阵列的各自组装及其应用。

    Nucleoside derivatives with photolabile protective groups
    10.
    发明授权
    Nucleoside derivatives with photolabile protective groups 失效
    具有光不稳定保护基团的核苷衍生物

    公开(公告)号：US5763599A

    公开(公告)日：1998-06-09

    申请号：US693217

    申请日：1996-08-09

    申请人： Wolfgang Pfleiderer ,  Heiner Giegrich

    发明人： Wolfgang Pfleiderer ,  Heiner Giegrich

    IPC分类号： C07H19/02 ,  C07H19/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C07H1/02

    CPC分类号： C07H19/06 ,  C07H19/04 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  Y02P20/55

    摘要： The invention relates to nucleoside derivatives having photolabile protective groups of the general formula (I) ##STR1## in which R.sup.1 .dbd.H, NO.sub.2, CN, OCH.sub.3, halogen or alkyl or alkoxyalkyl having 1 to 4 C atoms R.sup.2 .dbd.H, OCH.sub.3 R.sup.3 .dbd.H, F, Cl, Br, NO.sub.2 R.sup.4 .dbd.H, halogen, OCH.sub.3, or an alkyl radical having 1 to 4 C atoms R.sup.5 .dbd.H or a usual functional group for preparing oligonucleotides R.sup.6 .dbd.H, OH, halogen or XR.sup.8, where X.dbd.O or S and R.sup.8 represents a protective group usual in nucleotide chemistry, B=adenine, cytosine, guanine, thymine, uracil, 2,6-diaminopurin-9-yl, hypoxanthin-9-yl, 5-methylcytosin-1-yl, 5-amino-4-imidazolcarboxamid-1-yl, or 5-amino-4-imidazolcarboxamid-3-yl, where in the case of B=adenine, cytosine or guanine, the primary amino function optionally exhibits a permanent protective group. These derivatives may be used for the light-controlled synthesis of oligonucleotides on a DNA chip.

    摘要翻译： PCT No.PCT / EP95 / 04976 Sec。 371日期：1996年8月9日 102（e）日期1996年8月9日PCT提交1995年12月15日PCT公布。 出版物WO96 / 日本1996年6月20日本发明涉及具有通式（I）的光不稳定保护基的核苷衍生物，其中R1 = H，NO2，CN，OCH3，卤素或具有1-4个碳原子的烷基或烷氧基烷基R2 = H，OCH 3 R 3 = H，F，Cl，Br，NO 2 R 4 = H，卤素，OCH 3或具有1至4个C原子的烷基R 5 = H或用于制备寡核苷酸的通常官能团R6 = H，OH， 或XR8，其中X = O或S，R8表示核苷酸化学中通常的保护基，B =腺嘌呤，胞嘧啶，鸟嘌呤，胸腺嘧啶，尿嘧啶，2,6-二氨基嘌呤-9-基，次黄嘌呤-9-基， 甲基胞嘧啶-1-基，5-氨基-4-咪唑甲酰胺-1-基或5-氨基-4-咪唑甲酰胺-3-基，其中在B =腺嘌呤，胞嘧啶或鸟嘌呤的情况下，伯氨基官能团任选地显示 永久保护组。 这些衍生物可用于DNA芯片上寡核苷酸的轻度控制合成。