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1. 发明授权

US4963662A Fluorinated nucleosides and method for treating retrovirus infections therewith 失效
标题翻译：氟化核苷和用于治疗逆转录病毒感染的方法
公开(公告)号：US4963662A
公开(公告)日：1990-10-16
申请号：US223677
申请日：1988-07-15
申请人： Eckart Matthes , Christine Lehmann , Dieter Scholz , Martin von Janta-Lipinski , Klaus Gaertner , Peter Langen , Hans-Alfred Rosenthal
发明人： Eckart Matthes , Christine Lehmann , Dieter Scholz , Martin von Janta-Lipinski , Klaus Gaertner , Peter Langen , Hans-Alfred Rosenthal
IPC分类号： C07H19/073 , A61K9/00 , A61K31/505 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61P31/12 , A61P31/18 , C07H17/00 , C07H19/06 , C07H19/09 , C07H19/14 , C07H19/16 , C07H19/173 , C07H19/19
CPC分类号： C07H19/06 , C07H19/16
摘要： A method for treating AIDS, which comprises administering to a patient in need therefor a pharmaceutical composition comprising a therapeutically effective amount of a compound having the formula ##STR1## wherein R.sub.1 is an adenine, cytosine, guanine, thymidine, uracil, 5-substituted uracil, 5-substituted cytosine derivative, 2-fluoroadenine, 2.6-diaminopurine, 2-aminopurine, 6-thioguanine, or 7-deazaadenine group;R.sub.2 is H, or a OH group;R.sub.3 is a OH, O-acyl, O-palmitoyl group, or phosphates (as free acid, or its alkali, ammonium or alkyl ammonium salts), or any other precursor group for the hydroxyl group;or a physiologically acceptable salt thereof. Furthermore, the present invention comprises the new compounds:2',3'-dideoxy-3'-fluoro-2-fluoroadenosine,2',3'-dideoxy-3'-fluoro-6-thioguanosine,2',3'-dideoxy-3'-fluoro-2,6-diaminopurineriboside,2',3'-dideoxy-3'-fluoro-2-aminopurineriboside,2',3'-dideoxy-3'-fluoro-5-aminomethyluridine,2',3'-dideoxy-3'-fluoro-5-azidomethyluridine, and2',3'-dideoxy-3'-fluoro-5-hydroxymethyluridine.
摘要翻译：一种治疗AIDS的方法，其包括向需要的患者施用包含治疗有效量的具有下式的化合物（I）的药物组合物，其中R1是腺嘌呤，胞嘧啶，鸟嘌呤，胸苷，尿嘧啶，5 取代尿嘧啶，5-取代胞嘧啶衍生物，2-氟腺嘌呤，2,6-二氨基嘌呤，2-氨基嘌呤，6-硫鸟嘌呤或7-脱氮腺嘌呤基团; R2是H或OH基; R3是OH，O-酰基，O-棕榈酰基或磷酸酯（作为游离酸，或其碱金属，铵或烷基铵盐）或羟基的任何其它前体基团; 或其生理上可接受的盐。此外，本发明包括新化合物：2'，3'-二脱氧-3'-氟-2-氟腺苷，2'，3'-二脱氧-3'-氟-6-硫代鸟苷，2'，3'- 二脱氧-3'-氟-2,6-二氨基嘌呤，2'，3'-二脱氧-3'-氟-2-氨基嘌呤，2'，3'-二脱氧-3'-氟-5-氨甲基尿苷，2' 3'-二脱氧-3'-氟-5-叠氮基甲基尿苷和2'，3'-二脱氧-3'-氟-5-羟甲基尿苷。

2. 发明授权

US5153180A Fluorinated nucleosides and process for treating retrovirus infections therewith 失效
标题翻译：氟化核苷和用于治疗逆转录病毒感染的方法
公开(公告)号：US5153180A
公开(公告)日：1992-10-06
申请号：US566486
申请日：1990-08-13
申请人： Eckart Matthes , Christine Lehmann , Dieter Scholz , Martin von Janta-Lipinski , Klaus Gaertner , Peter Langen , Hans-Alfred Rosenthal
发明人： Eckart Matthes , Christine Lehmann , Dieter Scholz , Martin von Janta-Lipinski , Klaus Gaertner , Peter Langen , Hans-Alfred Rosenthal
IPC分类号： C07H19/06 , C07H19/16
CPC分类号： C07H19/06 , C07H19/16
摘要： A process for treating AIDS, which comprises administering to a patient in need therefor a pharmaceutical composition comprising a therapeutically effective amount of a compound having the formula ##STR1## wherein: R.sub.1 is an adenine, cytosine, guanine, thymidine, uracil, 5-substituted uracil, 5-substituted cytosine derivative, 2-fluoroadenine, 2.6-diaminopurine, 2-aminopurine, 6-thioguanine, or 7-deazaadenine group;R.sub.2 is H, or a OH group;R.sub.3 is a OH, O-acyl, O-palmitoyl group or phosphates (as free acid, or its alkali, ammonium or alkyl ammonium salts), or any other precursor group for the hydroxyl group;or a physiologically acceptable salt thereof. Furthermore, the present invention comprises the new compounds:2',3'-dideoxy-3'-fluoro-2-fluoroadenosine,2',3'-dideoxy-3'-fluoro-6-thioguanosine,2',3'-dideoxy-3'-fluoro-2,6-diaminopurineriboside,2',3'-dideoxy-3'-fluoro-2-aminopurineriboside,2',3'-dideoxy-3'-fluoro-5-aminomethyluridine,2',3'-dideoxy-3'-fluoro-5-azidomethyluridine, and2',3'-dideoxy-3'-fluoro-5-hydroxymethyluridine.
摘要翻译：治疗AIDS的方法，其包括向需要的患者施用包含治疗有效量的具有下式的化合物（I）的药物组合物，其中：R1是腺嘌呤，胞嘧啶，鸟嘌呤，胸苷，尿嘧啶， 5-取代的尿嘧啶，5-取代的胞嘧啶衍生物，2-氟腺嘌呤，2,6-二氨基嘌呤，2-氨基嘌呤，6-硫鸟嘌呤或7-脱氮腺嘌呤基团; R2是H或OH基; R3是OH，O-酰基，O-棕榈酰基或磷酸酯（作为游离酸，或其碱金属，铵或烷基铵盐）或羟基的任何其它前体基团; 或其生理上可接受的盐。此外，本发明包括新化合物：2'，3'-二脱氧-3'-氟-2-氟腺苷，2'，3'-二脱氧-3'-氟-6-硫代鸟苷，2'，3'- 二脱氧-3'-氟-2,6-二氨基嘌呤，2'，3'-二脱氧-3'-氟-2-氨基嘌呤，2'，3'-二脱氧-3'-氟-5-氨甲基尿苷，2' 3'-二脱氧-3'-氟-5-叠氮基甲基尿苷和2'，3'-二脱氧-3'-氟-5-羟甲基尿苷。

3. 发明申请

US20090105186A1 Beta-L-N4-Hydroxycytosine Deoxynucleosides and their use as Pharmaceutical Agents in the Prophylaxis or Therapy of Viral Diseases 审中-公开
标题翻译： β-L-N4-羟基胞嘧啶脱氧核苷及其作为药物在预防或治疗病毒性疾病中的用途
公开(公告)号：US20090105186A1
公开(公告)日：2009-04-23
申请号：US11577677
申请日：2005-10-21
申请人： Eckart Matthes , Martin von Janta-Lipinski , Hans Will , Huseyin Sirma , Anneke Funk
发明人： Eckart Matthes , Martin von Janta-Lipinski , Hans Will , Huseyin Sirma , Anneke Funk
IPC分类号： A61K31/7068 , C07H19/067 , A61P35/00 , A61P31/18
CPC分类号： C07H19/06 , A61K31/706 , A61K31/7068 , A61K45/06 , C07H19/073 , C07H19/10
摘要： The invention relates to β-L-N4-hydroxycytosine nucleo-sides, pharmaceutical agents comprising same, and to the use of said β-L-N4-hydroxycytosine nucleosides and pharmaceutical agents in the prophylaxis or therapy of an infection caused by hepatitis B virus (HBV) or human immunodeficiency virus (HIV). The invention also relates to a method for the preparation of said β-L-nucleoside analogs.
摘要翻译：本发明涉及β-L-N4-羟基胞嘧啶核侧，包含其的药物，以及所述β-L-N4-羟基胞嘧啶核苷和药物在预防或治疗由乙型肝炎病毒引起的感染中的用途（HBV）或人类免疫缺陷病毒（HIV）。本发明还涉及制备所述β-L-核苷类似物的方法。

4. 发明授权

US5496935A 2',3'-dideoxynucleoside pyrimidine compounds and carbocyclic analogs 失效
标题翻译： 2'，3'-双脱氧核苷嘧啶化合物和碳环类似物
公开(公告)号：US5496935A
公开(公告)日：1996-03-05
申请号：US227587
申请日：1994-04-14
申请人： Eckart Matthes , Martin von Janta-Lipinski , Dieter Scholz , Klaus Gaertner , Juergen Schildt , Christine Lehmann , Peter Langen , Hans A. Rosenthal
发明人： Eckart Matthes , Martin von Janta-Lipinski , Dieter Scholz , Klaus Gaertner , Juergen Schildt , Christine Lehmann , Peter Langen , Hans A. Rosenthal
IPC分类号： C07D405/04 , C07H19/06 , C07H19/10 , C07H15/20
CPC分类号： C07D405/04 , C07H19/06 , C07H19/10
摘要： 2',3'-dideoxynucleoside pyrimidine compounds and 2-thiothymidine carbocyclic derivatives with antiviral activity are disclosed. These compounds are expected to exhibit antiviral activity recognized for 2',3'-dideoxynucleoside compounds and analogs thereof.
摘要翻译： 2'，3'-二脱氧核苷嘧啶化合物和具有抗病毒活性的2-硫代胸苷碳环衍生物。这些化合物预期表现出对2'，3'-二脱氧核苷化合物及其类似物所识别的抗病毒活性。

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