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1. 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。

2. 发明申请

US20060217345A1 Beta-L-nucleosides and use thereof as pharmaceutical agents for the treatment of viral diseases 审中-公开
标题翻译： β-L-核苷及其用作治疗病毒性疾病的药剂
公开(公告)号：US20060217345A1
公开(公告)日：2006-09-28
申请号：US11373062
申请日：2006-03-10
申请人： Eckart Matthes , Martin Janta-Lipinski , Hans Will , Huseyin Sirma , Lin Li
发明人： Eckart Matthes , Martin Janta-Lipinski , Hans Will , Huseyin Sirma , Lin Li
IPC分类号： A61K31/7072 , A61K31/675 , A61K31/513 , C07H19/04 , C07H19/12 , C07F9/6512
CPC分类号： C07H19/06 , C07H19/09
摘要： Nucleoside analogs, nucleic acids and pharmaceutical agents comprising same, and to the use of said nucleoside analogs, nucleic acids and pharmaceutical agents in the diagnosis, prophylaxis or therapy of a viral, bacterial, fungicidal and/or parasitic infection, or of cancer, particularly of hepatitis infections. The invention also relates to a method for the preparation of said nucleoside analogs and to a kit and the use thereof in the prophylaxis and therapy of viral diseases, particularly of hepatitis infections. As stated in 37 C.F.R. §1.72(b): A brief abstract of the technical disclosure in the specification must commence on a separate sheet, preferably following the claims, under the heading “Abstract of the Disclosure.” The purpose of the abstract is to enable the Patent and Trademark Office and the public generally to determine quickly from a cursory inspection the nature and gist of the technical disclosure. The abstract shall not be used for interpreting the scope of the claims. Therefore, any statements made relating to the abstract are not intended to limit the claims in any manner and should not be interpreted as limiting the claims in any manner.
摘要翻译：核苷类似物，核酸和包含其的药物，以及所述核苷类似物，核酸和药物在诊断，预防或治疗病毒，细菌，杀真菌和/或寄生虫感染或癌症中的用途，特别是的肝炎感染。本发明还涉及制备所述核苷类似物和试剂盒的方法及其用于预防和治疗病毒性疾病，特别是肝炎感染的用途。如37 C.F.R. §1.72（b）：说明书中技术性披露的简要摘要必须在单独的表格上开始，优选按照权利要求，在“披露摘要”标题下。摘要的目的是使专利商标局和公众一般能够从粗略检查中快速确定技术披露的性质和要点。摘要不得用于解释权利要求的范围。因此，与摘要有关的任何陈述不旨在以任何方式限制权利要求，也不应被解释为以任何方式限制权利要求。

3. 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。

4. 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。

5. 发明授权

US4916249A Glycero-3(2)-phospho-L-serine derivatives and salts thereof 失效
标题翻译：甘油-3（2） - 磷酸-L-丝氨酸衍生物及其盐
公开(公告)号：US4916249A
公开(公告)日：1990-04-10
申请号：US376161
申请日：1989-07-07
申请人： Hans Brachwitz , Peter Langen , Christine Lehmann , Eckart Matthes , Jurgen Schildt , Iduna Fichtner , Albin Hermetter , Friedrich Paltauf
发明人： Hans Brachwitz , Peter Langen , Christine Lehmann , Eckart Matthes , Jurgen Schildt , Iduna Fichtner , Albin Hermetter , Friedrich Paltauf
IPC分类号： C07F9/10
CPC分类号： C07F9/10
摘要： The invention relates to novel glycero-3(2)phospho-L-serine derivatives of the general formula ##STR1## in which A represents unsubstituted or substituted (C5-C30) alkoxy, or unsubstituted or substituted (C5-C30) alkenoxy, whereby a double bond of the alkenoxy residue does not originate at the C atom bound to oxygen, or halogen, or a group of the general formula--O--(CH.sub.2).sub.n --CF.sub.3 II,wherein n is 0 or an integer 1, 2 or 3, one of the two residues B and C, which is identical to or different from A, has one of the definitions given for A or represents hydrogen, and the respective other residue represents the phosphatidyl-Lserine group of the formula ##STR2## with the proviso that at least one residue A, B or C represents (C5-C30) alkoxy or (C5-C30) alkenoxy; and the pharmaceutically acceptable salts of compounds of general formula I with bases, a process for the preparation thereof, pharmaceutical preparations containing the said compounds, and their use in drugs with cytostatic activity.
摘要翻译：本发明涉及通式“IMAGE”I的新的甘油基-3（2）磷酸-L-丝氨酸衍生物，其中A代表未取代或取代的（C 5 -C 30）烷氧基或未取代或取代的（C 5 -C 30）烯氧基，其中链烯氧基残基的双键不是起源于与氧或卤素键合的C原子或通式-O-（CH 2）n -CF 3 II的基团，其中n为0或整数1,2或 3中，与A相同或不同的两个残基B和C之一之一具有对A给出的定义之一或代表氢，并且各自的其它残基表示式III的磷脂酰-L-丝氨酸基条件是至少一个残基A，B或C表示（C 5 -C 30）烷氧基或（C 5 -C 30）链烯氧基; 和通式I的化合物的药学上可接受的盐与碱，其制备方法，含有所述化合物的药物制剂，以及它们在具有细胞抑制活性的药物中的用途。

6. 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。

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