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1. 发明授权

US06949521B2 Therapeutic azide compounds 失效
标题翻译：治疗叠氮化合物
公开(公告)号：US06949521B2
公开(公告)日：2005-09-27
申请号：US09849870
申请日：2001-05-04
申请人： Chung K. Chu , Lakshmi P. Kotra , Konstantine Manouilov , Jinfa Du , Raymond Schinazi
发明人： Chung K. Chu , Lakshmi P. Kotra , Konstantine Manouilov , Jinfa Du , Raymond Schinazi
IPC分类号： C07D499/21 , A61K31/00 , A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7076 , A61K47/48 , A61P43/00 , C07D239/46 , C07D473/16 , C07D473/34 , C07D501/14 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/19 , C07H19/20 , A01N43/04
CPC分类号： A61K31/7076 , A61K47/52 , C07H19/04 , C07H19/10 , C07H19/16 , C07H19/20
摘要： Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.
摘要翻译：提供药物前药组合物，其包含能够在体内转化为药物的药物的叠氮衍生物。具有胺，酮和羟基取代基的药物的叠氮衍生物在体内转化为相应的药物，增加药物的半衰期。此外叠氮化物前药通常比相应的药物更好地穿透血脑屏障。特别有用的是虫草素，2'-F-ara-ddI，AraA，阿昔洛韦，喷昔洛韦和相关药物的叠氮衍生物。有用的叠氮化物前药是治疗脂环族胺，酮和羟基取代的化合物的叠氮化物衍生物，包括芳烷基，杂环芳烷基和环状脂族化合物，其中胺或氧部分在环上，或胺或氧部分在其上脂肪族侧链，以及治疗性嘌呤和嘧啶，核苷类似物和磷酸化核苷类似物。

2. 发明授权

US06271212B1 Prodrug azide compositions and compounds 失效
标题翻译：前药叠氮组合物和化合物
公开(公告)号：US06271212B1
公开(公告)日：2001-08-07
申请号：US09033996
申请日：1998-03-03
申请人： Chung K. Chu , Lakshimi Kotra , Kostantine K. Manouilov , Jinfa Du , Raymond Schinazi
发明人： Chung K. Chu , Lakshimi Kotra , Kostantine K. Manouilov , Jinfa Du , Raymond Schinazi
IPC分类号： A61K3170
CPC分类号： A61K31/7076 , A61K47/52 , C07H19/04 , C07H19/10 , C07H19/16 , C07H19/20
摘要： Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.
摘要翻译：提供药物前药组合物，其包含能够在体内转化为药物的药物的叠氮衍生物。具有胺，酮和羟基取代基的药物的叠氮衍生物在体内转化为相应的药物，增加药物的半衰期。此外叠氮化物前药通常比相应的药物更好地穿透血脑屏障。特别有用的是虫草素，2'-F-ara-ddI，AraA，阿昔洛韦，喷昔洛韦和相关药物的叠氮衍生物。有用的叠氮化物前药是治疗脂环族胺，酮和羟基取代的化合物的叠氮化物衍生物，包括芳烷基，杂环芳烷基和环状脂族化合物，其中胺或氧部分在环上，或胺或氧部分在其上脂肪族侧链，以及治疗性嘌呤和嘧啶，核苷类似物和磷酸化核苷类似物。

3. 发明授权

US06894159B2 Process for the preparation of 2′-fluoro-5-methyl-beta-L-arabino-furanosyluridine 有权
标题翻译：制备2'-氟-5-甲基-β-L-阿拉伯 - 呋喃糖基尿苷的方法
公开(公告)号：US06894159B2
公开(公告)日：2005-05-17
申请号：US10351222
申请日：2003-01-24
申请人： Chung K. Chu , Jinfa Du , Yongseok Choi
发明人： Chung K. Chu , Jinfa Du , Yongseok Choi
IPC分类号： C07H3/02 , C07H9/04 , C07H19/06 , C07H19/00 , C07H19/22
CPC分类号： C07H9/04 , C07H3/02 , C07H19/06
摘要： The present invention relates to a novel and improved process for preparing 2′-fluoro-5-methyl-β-L-arabinofuranosyluridine represented by formula (1) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus and Epstein-Barr virus:
摘要翻译：本发明涉及一种制备式（1）所示的2'-氟-5-甲基-β-L-阿拉伯呋喃糖基尿苷的新型改进方法，该方法显示出抗病毒活性，特别是抗乙型肝炎病毒的抗病毒活性和爱泼斯坦 - 巴尔病毒：

4. 发明授权

US5648489A Syntheses of acyclic guanine nucleosides 失效
标题翻译：无环鸟嘌呤核苷的合成
公开(公告)号：US5648489A
公开(公告)日：1997-07-15
申请号：US466802
申请日：1995-06-06
申请人： Chung K. Chu , Jinfa Du , Chunguang Wang
发明人： Chung K. Chu , Jinfa Du , Chunguang Wang
IPC分类号： C07D473/00 , C07D473/18 , E07B43/04
CPC分类号： C07D473/00
摘要： A method is provided for the synthesis of synthesis of acyclic purine nucleosides, particularly 9-(2-hydroxy-ethoxymethyl)-guanine (acyclovir) and 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine ("DHPG") where the N.sup.2,N.sup.9 -diprotected guanine is reacted with CH.sub.3 C(O)OCH.sub.2 O(CH.sub.2).sub.2)OC(O)CH.sub.3 or 2-acetoxymethoxy-1,3-diacetoxypropane, respectively, in the presence of a mixture of an acid and acetic anhydride, or in the presence of an acid, where the acid can be phosphoric acid or polyphosphoric acid.
摘要翻译：提供了合成无环嘌呤核苷，特别是9-（2-羟基 - 乙氧基甲基）鸟嘌呤（无环鸟苷）和9 - [（1,3-二羟基-2-丙氧基）甲基]鸟嘌呤（“DHPG” “）其中N 2，N 9 - 二保护的鸟嘌呤分别与CH 3 C（O）OCH 2 O（CH 2）2）OC（O）CH 3或2-乙酰氧基甲氧基-1,3-二乙酰氧基丙烷在酸的混合物存在下反应和乙酸酐，或在酸存在下，其中酸可以是磷酸或多磷酸。

5. 发明授权

US06197777B1 Synthesis, anti-human immunodeficiency virus, and anti-hepatitis B virus activities of 1,3-oxaselenolane nucleosides 失效
标题翻译：合成，抗人免疫缺陷病毒和1,3-乙氧基硫茚核苷的抗乙型肝炎病毒活性
公开(公告)号：US06197777B1
公开(公告)日：2001-03-06
申请号：US09517955
申请日：2000-03-03
申请人： Raymond F. Schinazi , Chung K. Chu , Jinfa Du
发明人： Raymond F. Schinazi , Chung K. Chu , Jinfa Du
IPC分类号： A01N4390
CPC分类号： C07D473/00 , C07D421/04 , C07D473/18 , C07F9/65586 , C07F9/65616
摘要： A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
摘要翻译：公开了用于治疗人类和其他宿主动物中的HIV感染，HBV感染或异常细胞增殖的方法和组合物，其包括施用有效量的1,3-氧硫杂环戊烷核苷或其药学上可接受的盐，任选地在药学上可接受的载体中。

6. 发明授权

US06590107B1 Synthesis, anti-human immunodeficiency virus, and anti-hepatitis B virus activities of 1,3-oxaselenolane nucleosides 失效
标题翻译：合成，抗人免疫缺陷病毒和1,3-乙氧基硫茚核苷的抗乙型肝炎病毒活性
公开(公告)号：US06590107B1
公开(公告)日：2003-07-08
申请号：US09799327
申请日：2001-03-05
申请人： Raymond F. Schinazi , Chung K. Chu , Jinfa Du
发明人： Raymond F. Schinazi , Chung K. Chu , Jinfa Du
IPC分类号： C07F928
CPC分类号： C07D473/00 , C07D421/04 , C07D473/18 , C07F9/65586 , C07F9/65616
摘要： A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
摘要翻译：公开了用于治疗人类和其他宿主动物中的HIV感染，HBV感染或异常细胞增殖的方法和组合物，其包括施用有效量的1,3-氧硫杂环戊烷核苷或其药学上可接受的盐，任选地在药学上可接受的载体中。

7. 发明授权

US06512107B2 Process for the preparation of 2′-fluoro-5-methyl-&bgr;-L-arabinofuranosyluridine 失效
标题翻译： 2'-氟-5-甲基-β-L-阿拉伯呋喃糖基尿苷的制备方法
公开(公告)号：US06512107B2
公开(公告)日：2003-01-28
申请号：US09121294
申请日：1998-07-23
申请人： Chung K. Chu , Jinfa Du , Yongseok Choi
发明人： Chung K. Chu , Jinfa Du , Yongseok Choi
IPC分类号： C07H1919
CPC分类号： C07H9/04 , C07H3/02 , C07H19/06
摘要： The present invention relates to a novel and improved process for preparing 2′-fluoro-5-methyl-&bgr;-L-arabinofuranosyluridine represented by formula (I) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus and Epstein-Barr virus:
摘要翻译：本发明涉及一种制备式（I）表示的2'-氟-5-甲基-β-L-阿拉伯呋喃糖基尿苷的新型改进方法，该方法显示出抗病毒活性，特别是抗乙型肝炎病毒的抗病毒活性和爱泼斯坦 - 巴尔病毒：

8. 发明授权

US6071922A Synthesis, anti-human immunodeficiency virus, and anti-hepatitis B virus activities of 1,3-oxaselenolane nucleosides 失效
公开(公告)号：US6071922A
公开(公告)日：2000-06-06
申请号：US44558
申请日：1998-03-19
申请人： Raymond F. Schinazi , Chung K. Chu , Jinfa Du
发明人： Raymond F. Schinazi , Chung K. Chu , Jinfa Du
IPC分类号： C07D421/04 , C07D473/00 , C07D473/18 , C07F9/6558 , C07F9/6561 , A61K31/505 , C07D239/02
CPC分类号： C07D473/00 , C07D421/04 , C07D473/18 , C07F9/65586 , C07F9/65616
摘要： A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

9. 发明授权

US5583225A Syntheses of acyclic guanine nucleosides 失效
标题翻译：无环鸟嘌呤核苷的合成
公开(公告)号：US5583225A
公开(公告)日：1996-12-10
申请号：US245024
申请日：1994-05-17
申请人： Chung K. Chu , Jinfa Du
发明人： Chung K. Chu , Jinfa Du
IPC分类号： C07D473/00 , C07D473/18
CPC分类号： C07D473/00
摘要： A method is provided for the synthesis of synthesis of acyclic purine nucleosides, particularly 9-(2-hydroxyethoxymethyl)-guanine (acyclovir) and 9-[(1,3-dihydroxy-2-propoxy)methyl]guanine ("DHPG") where the N.sup.2,N.sup.9 -diprotected guanine is reacted with CH.sub.3 C(O)OCH.sub.2 O(CH.sub.2).sub.2)OC(O)CH.sub.3 or diacetoxypropane, respectively, in the presence of a mixture of an acid and acetic anhydride, or in the presence of an acid, where the acid can be phosphoric acid or polyphosphoric acid.
摘要翻译：提供了合成无环嘌呤核苷，特别是9-（2-羟基乙氧基甲基）鸟嘌呤（无环鸟苷）和9 - [（1,3-二羟基-2-丙氧基）甲基]鸟嘌呤（“DHPG”）的合成方法。其中在酸和乙酸酐的混合物存在下，或者在存在下，将N 2，N 9 - 二保护的鸟嘌呤分别与CH 3 C（O）OCH 2 O（CH 2）2）OC（O）CH 3或二乙酰氧基丙烷反应酸，其中酸可以是磷酸或多磷酸。

10. 发明授权

US08716263B2 Synthesis of purine nucleosides 有权
标题翻译：嘌呤核苷的合成
公开(公告)号：US08716263B2
公开(公告)日：2014-05-06
申请号：US12645821
申请日：2009-12-23
申请人： Byoung-Kwon Chun , Jinfa Du , Suguna Rachakonda , Bruce Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Wonsuk Chang , Hai-Ren Zhang , Dhanapalan Nagarathnam
发明人： Byoung-Kwon Chun , Jinfa Du , Suguna Rachakonda , Bruce Ross , Michael Joseph Sofia , Ganapati Reddy Pamulapati , Wonsuk Chang , Hai-Ren Zhang , Dhanapalan Nagarathnam
IPC分类号： A01N43/04 , A61K31/70 , C07H19/00 , C07H19/04 , C07H19/20
CPC分类号： C07H19/20 , C07H1/00 , C07H5/02 , C07H15/04 , C07H19/167 , C07H19/213 , Y02P20/55
摘要： A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.
摘要翻译：制备核苷衍生物的氨基磷酸酯前药或环磷酸酯前药的方法，其为化合物，其立体异构体，盐（酸或碱加成盐），水合物，溶剂合物或其结晶形式。

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