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1. 发明授权

US6048975A Process for the chemical synthesis of oligonucleotides 失效
标题翻译：寡核苷酸化学合成的方法
公开(公告)号：US6048975A
公开(公告)日：2000-04-11
申请号：US800123
申请日：1997-02-13
申请人： Wolfgang Pfleiderer , Frank Bergmann
发明人： Wolfgang Pfleiderer , Frank Bergmann
IPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H1/00 , C07H19/00 , C07H21/00
CPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , Y02P20/55
摘要： A process for the chemical synthesis of oligonucleotidesUse of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable synthetic processes.The ease of detection of the dansyl protective group and the ease of elimination from the sugar residue of the nucleotide without side reactions make oligonucleotide synthesis possible with high yields in very small quantities.
摘要翻译：寡核苷酸的化学合成方法在DNA和RNA的化学合成中使用丹参乙氧基羰基作为碱不稳定的5'-羟基保护基团和合适的合成方法。丹磺酰基保护基的易于检测和不含副反应的核苷酸的糖残基的易于消除使寡核苷酸合成成为非常少的高产率。

2. 发明授权

US5945524A Process for the chemical synthesis of oligonucleotides 失效
标题翻译：寡核苷酸化学合成的方法
公开(公告)号：US5945524A
公开(公告)日：1999-08-31
申请号：US487229
申请日：1995-06-07
申请人： Wolfgang Pfleiderer , Frank Bergmann
发明人： Wolfgang Pfleiderer , Frank Bergmann
IPC分类号： C12N15/09 , C07B51/00 , C07C315/04 , C07C317/36 , C07H19/04 , C07H19/06 , C07H19/067 , C07H19/073 , C07H19/10 , C07H19/14 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/20 , C07H19/207 , C07H19/23 , C07H21/00 , C07H21/02 , C07H21/04 , C07H1/00
CPC分类号： C07H21/00 , C07C315/04 , C07C317/36 , C07H19/10 , C07H19/16 , C07H19/20 , Y02P20/55
摘要： Use of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable synthetic processes.The ease of detection of the dansyl protective group and the ease of elimination from the sugar residue of the nucleotide without side reactions make oligonucleotide synthesis possible with high yields in very small quantities.
摘要翻译：在DNA和RNA的化学合成中使用丹酰乙氧基羰基作为碱不稳定的5'-羟基保护基团和合适的合成方法。丹磺酰基保护基的易于检测和不含副反应的核苷酸的糖残基的易于消除使寡核苷酸合成成为非常少的高产率。

3. 发明授权

US5631362A 5'-O-Dans EOC modified nucleosides and methods for preparing same 失效
标题翻译： 5'-O-Dans EOC修饰核苷及其制备方法
公开(公告)号：US5631362A
公开(公告)日：1997-05-20
申请号：US437566
申请日：1995-05-09
申请人： Wolfgang Pfleiderer , Frank Bergmann
发明人： Wolfgang Pfleiderer , Frank Bergmann
IPC分类号： C12N15/09 , C07B51/00 , C07C315/04 , C07C317/36 , C07H19/04 , C07H19/06 , C07H19/067 , C07H19/073 , C07H19/10 , C07H19/14 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/20 , C07H19/207 , C07H19/23 , C07H21/00 , C07H21/02 , C07H21/04 , C07H1/00
CPC分类号： C07H21/00 , C07C315/04 , C07C317/36 , C07H19/10 , C07H19/16 , C07H19/20 , Y02P20/55
摘要： Dansylethoxycarbonyl (Dans-EOC) groups which can be employed as base-labile 5'hydroxyl protective groups in chemical oligonucleotide synthesis are disclosed. These groups allow the preparation of a compound of the formula (I) ##STR1## which comprises reacting the compound of the formula (II) ##STR2## with a chlorocarbonyl donor.
摘要翻译：公开了可用作化学寡核苷酸合成中的碱不稳定的5'-羟基保护基的Dansylethoxycarbonyl（Dans-EOC）基团。这些基团允许制备式（I）化合物（I），其包括使式（II）化合物与式

4. 发明申请

US20080004285A1 PYRIDO(3,2-D)PYRIMIDINES AND PHARMACEUTICAL COMPOSITIONS USEFUL FOR MEDICAL TREATMENT 审中-公开
标题翻译：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。

5. 发明申请

US20060189620A1 Immunosuppressive effects of pteridine derivatives 审中-公开
标题翻译：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。

6. 发明授权

US06716971B1 Pteridine nucleotide analogs 失效
标题翻译：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。

7. 发明授权

US06281201B1 Base-modified derivatives of 2′,5′-oligoadenylate and antiviral uses thereof 有权
标题翻译： 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。

8. 发明授权

US5902810A Pteridine derivatives as no synthase inhibitors 失效
标题翻译：蝶啶衍生物不含合酶抑制剂
公开(公告)号：US5902810A
公开(公告)日：1999-05-11
申请号：US737657
申请日：1997-02-18
申请人： Wolfgang Pfleiderer , Harald Schmidt , Rainer Henning
发明人： Wolfgang Pfleiderer , Harald Schmidt , Rainer Henning
IPC分类号： A61K31/505 , A61K31/519 , A61P1/04 , A61P3/08 , A61P9/02 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P25/04 , A61P25/08 , A61P25/28 , A61P29/00 , A61P31/12 , C07D475/04 , C07D475/08 , C12N9/99 , A61K31/495
CPC分类号： C12N9/99 , A61K31/519 , C07D475/04 , C07D475/08
摘要： The present invention relates to the use of pteridine derivatives of the formula I ##STR1## in which X is O, NH or N--(C.sub.1-C.sub.5)-alkanoyl, R.sup.3 is the radical --OR.sup.4, --NR.sup.5 R.sup.6 or --S(O).sub.m R.sup.7, and R, R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and m have the meanings given in claim 1, which are nitric oxide synthase inhibitors, for the treatment of diseases which are caused by an increased nitric oxide level.
摘要翻译： PCT No.PCT / EP95 / 01731 Sec。 371日期1997年2月18日 102（e）日期1997年2月18日PCT提交1995年5月6日PCT公布。 WO95 / 31987 PCT公开号 1995年11月30日的日本本发明涉及式I的蝶啶衍生物的用途，其中X为O，NH或N-（C 1 -C 5） - 烷酰基，R 3为基团-OR 4，-NR 5 R 6或-S（ O）mR7，并且R，R1，R2，R4，R5，R6，R7和m具有权利要求1中给出的含义，其是一氧化氮合酶抑制剂，用于治疗由一氧化氮水平升高引起的疾病。

9. 发明授权

US5863905A 2',5'-phosphorothioate/phosphodiester oligoadenylates and anti-viral uses thereof 失效
标题翻译： 2'，5'-硫代磷酸酯/磷酸二酯寡聚腺苷酸及其抗病毒用途
公开(公告)号：US5863905A
公开(公告)日：1999-01-26
申请号：US780244
申请日：1997-01-08
申请人： Robert J. Suhadolnik , Wolfgang Pfleiderer
发明人： Robert J. Suhadolnik , Wolfgang Pfleiderer
IPC分类号： C07H21/02 , A01N57/16 , A61K9/127 , A61K31/70 , A61K31/7125 , A61K38/00 , A61K47/48 , A61P17/00 , A61P31/12 , A61P31/18 , A61P31/22 , A61P35/00 , C07F9/6561 , C07H21/00 , C07K14/47
CPC分类号： C07H21/00 , A61K47/48192 , A61K47/48223 , Y10S514/885 , Y10S514/889 , Y10S514/934
摘要： Optically active antiviral compounds having the formula ##STR1## wherein m is 0, 1, 2, or 3; n and q are selected from the group of 0 and 1, provided that n and q may not both be zero; and R, R.sub.1, and R.sub.2 are independently of each other selected from the group consisting of oxygen and sulfur, provided that all R, R.sub.1 and R.sub.2, may not be oxygen, and further provided that all R, R.sub.1, and R.sub.2 may not be sulfur. The compounds possess increased antiviral activity and/or metabolic stability.
摘要翻译：具有下式的光学活性抗病毒化合物：其中m为0,1,2或3; n和q选自0和1组，条件是n和q不能都为零; 并且R，R 1和R 2彼此独立地选自氧和硫，条件是所有R 1，R 2和R 2可以不是氧，并且进一步规定，所有R，R 1和R 2可以不是硫。该化合物具有增加的抗病毒活性和/或代谢稳定性。

10. 发明授权

US3971792A Process for the manufacture of 4-amino-3-aminomethylpiperidine 失效
标题翻译：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。

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