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31. 发明授权

US06911424B2 2′-fluoronucleosides 有权
标题翻译： 2'-核糖核苷
公开(公告)号：US06911424B2
公开(公告)日：2005-06-28
申请号：US10061128
申请日：2002-01-30
申请人： Raymond F. Schinazi , Dennis C. Liotta , Chung K. Chu , J. Jeffrey McAtee , Junxing Shi , Yongseok Choi , Kyeong Lee , Joon H. Hong
发明人： Raymond F. Schinazi , Dennis C. Liotta , Chung K. Chu , J. Jeffrey McAtee , Junxing Shi , Yongseok Choi , Kyeong Lee , Joon H. Hong
IPC分类号： C07D239/47 , A61K31/505 , A61K31/506 , A61K31/52 , A61K31/522 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/20 , A61P35/00 , C07D405/04 , C07D473/00 , C07D473/18 , C07D473/34 , C07F7/18 , C07F9/547 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H19/207 , A01N61/00 , A01N43/04 , C07H1/00 , C07H11/00 , C07H19/00
CPC分类号： A61K31/7076 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/708 , C07D405/04 , C07D473/00 , C07H19/06 , C07H19/10 , C07H19/16
摘要： A class of 2′-fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein Base is a purine or pyrimidine base; R1 is OH, H, OR3, N3, CN, halogen, including F, or CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy, and base refers to a purine or pyrimidine base; R2 is H, phosphate, including monophosphate, diphosphate, triphosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of providing a compound wherein R2 is H or phosphate; sulfonate ester including alkyl or arylalkyl sulfonyl including methanesulfonyl, benzyl, wherein the phenyl group is optionally substituted with one or more substituents as described in the definition of aryl given above, a lipid, an amino acid, peptide, or cholesterol; and R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of being cleaved to the parent compound, or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了一类可用于治疗乙型肝炎感染，丙型肝炎感染，HIV和异常细胞增殖（包括肿瘤和癌症）的2'-氟 - 核苷化合物。所述化合物具有以下通式：其中碱是嘌呤或嘧啶碱; R 1是OH，H，OR 3，N 3，CN，卤素，包括F或CF 3 N ，低级烷基，氨基，低级烷基氨基，二（低级）烷基氨基或烷氧基，碱是指嘌呤或嘧啶碱基; R 2是H，磷酸盐，包括单磷酸盐，二磷酸盐，三磷酸盐或稳定化的磷酸盐前药; 酰基或其它药学上可接受的离去基团，其当在体内施用时能够提供其中R 2是H或磷酸酯的化合物; 磺酸酯，包括烷基或芳基烷基磺酰基，包括甲磺酰基，苄基，其中苯基任选被一个或多个取代基取代，如上述芳基定义中所述，脂质，氨基酸，肽或胆固醇; 并且R 3是酰基，烷基，磷酸酯或其它药学上可接受的离去基团，当其在体内施用时，其能够被切割成母体化合物或其药学上可接受的盐。

32. 发明授权

US06602664B2 3′-azido-2′,3′-dideoxyuridine in an anti-HIV effectiveness test protocol 有权
标题翻译： 3'-叠氮基-2'，3'-二脱氧尿苷在抗HIV有效性测试方案中
公开(公告)号：US06602664B2
公开(公告)日：2003-08-05
申请号：US09793346
申请日：2001-02-26
申请人： Raymond F. Schinazi , Martin L. Bryant , Maureen W. Myers
发明人： Raymond F. Schinazi , Martin L. Bryant , Maureen W. Myers
IPC分类号： C12Q168
CPC分类号： A61K45/06 , A61K31/70 , A61K31/7072 , A61K2300/00
摘要： It has been discovered that 3′-azido-2′,3′-dideoxyuridine (CS-87) induces a transient mutation in HIV-1 at the 70th codon (K to R, i.e., lysine to arginine) of the reverse transcriptase region of the virus. Based on this discovery, a method and composition for treating HIV is provided that includes administering CS-87 or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70th codon of the reverse transcriptase region. This invention can be practiced by referring to the published mutation patterns for known anti-HIV drugs, or by determining the mutation pattern for a new drug.
摘要翻译：已经发现3'-叠氮基-2'，3'-二脱氧尿苷（CS-87）在逆转录酶区域的第70个密码子（K至R，即赖氨酸至精氨酸）中诱导HIV-1中的瞬时突变的病毒。基于这一发现，提供了一种用于治疗HIV的方法和组合物，其包括将CS-87或其药学上可接受的盐或前药给予需要治疗的人与与HIV-1中突变的药物组合或交替除了逆转录酶区域的第70个密码子之外的位置。本发明可以通过参考公知的抗HIV药物的突变模式，或通过确定新药的突变模式来实施。

33. 发明授权

US06204391B1 Water soluble fullerenes with antiviral activity 失效
公开(公告)号：US06204391B1
公开(公告)日：2001-03-20
申请号：US09246011
申请日：1998-09-21
申请人： Simon H. Friedman , Raymond F. Schinazi , Fred Wudl , Craig L. Hill , Diane L. DeCamp , Rintje P. Sijbesma , George L. Kenyon
发明人： Simon H. Friedman , Raymond F. Schinazi , Fred Wudl , Craig L. Hill , Diane L. DeCamp , Rintje P. Sijbesma , George L. Kenyon
IPC分类号： C07C22932
CPC分类号： C07C57/50 , C07C13/64 , C07C49/255 , C07C55/00 , C07C211/27 , C07C211/42 , C07C211/50 , C07C233/36 , C07C2601/00 , C07C2601/14 , C07C2603/18 , C07C2603/94 , C07D231/56 , C07D233/64 , C07D239/26 , C07D261/08 , C07D471/10 , C07D487/10 , Y10S977/904
摘要： A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.

34. 发明授权

US5872107A Treatment of urogenital cancer with boron neutron capture therapy 失效
标题翻译：用硼中子捕获治疗泌尿生殖系癌
公开(公告)号：US5872107A
公开(公告)日：1999-02-16
申请号：US792370
申请日：1997-02-03
申请人： Raymond F. Schinazi , Thomas E. Keane , Dennis C. Liotta
发明人： Raymond F. Schinazi , Thomas E. Keane , Dennis C. Liotta
IPC分类号： C12N15/09 , A61K31/69 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7076 , A61K31/7088 , A61K41/00 , A61K48/00 , A61K49/00 , A61K49/08 , A61N5/00 , A61P13/02 , A61P15/00 , A61P31/12 , A61P35/00 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/04 , C07H23/00 , C12N9/12 , C12N15/10 , C12N15/113 , C12Q1/68
CPC分类号： C07H21/00 , A61K41/0095 , A61K49/085 , A61K49/10 , C07H19/06 , C07H19/10 , C07H19/20 , C07H23/00 , C12N15/10 , C12N15/113 , C12N9/1276 , C12Q1/6816 , C12Q1/6827 , C12Q1/6886 , C12N2310/318 , C12N2310/33 , C12N2310/3527
摘要： Methods and compositions for treating urogenital tumors, and in particular, cancer of the prostate, bladder, and kidney, with BCNT, are disclosed. Any boron-containing compound that is sufficiently lipophilic to pass through the appropriate urogenital membranes in a quantity high enough to achieve therapy on irradiation with low-energy neutrons can be used. Carboranyl-containing nucleosides and oligonucleotides are particularly suited for use in BNCT of urogenital tumors. Preferred compounds include 5-carboranyl-2'-deoxyuridine (CDU) and 5-o-carboranyl-1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)uracil (CFAU). Nucleosides and oligonucleotides bearing an -O-�(carboran-1-yl)alkyl!phosphate, S-�(carboran-1-yl)alkyl!phosphorothioate, or Se-�(carboran-1-yl)alkyl!phosphoroselenoate in place of the (carboran-1-yl)phosphonate moiety can be used. Oligonucleotides of specific gene sequences that include one or more 3',5'-linking-(carboran-1-yl)phosphonate moieties can also be used in antisense therapy in the selective modification of gene expression. Compounds can be used in urogenital BNCT therapy that contain boron clusters as a means to enhance lipophilicity wherein the boron is not enriched in .sup.10 B, but instead, in the .sup.11 B isotope. The therapy is accomplished by administering the boron-containing compound by any appropriate route, including by intravenous injection, oral delivery or by catheter or other direct means, in such a manner that the compound accumulates in the target tumor. After desired accumulation of the compound in the tumor, the site is irradiated with an effective amount of low energy neutrons.
摘要翻译：公开了用BCNT治疗泌尿生殖肿瘤，特别是前列腺癌，膀胱癌和肾癌的方法和组合物。可以使用任何足够亲油的通过合适的泌尿生殖膜的含硼化合物，其量足够高以实现对低能中子的照射治疗。含有硼烷基的核苷和寡核苷酸特别适用于泌尿生殖器肿瘤的BNCT。优选的化合物包括5-碳硼烷基-2'-脱氧尿苷（CDU）和5-邻硼烷基-1-（2-脱氧-2-氟-β-阿拉伯呋喃糖基）尿嘧啶（CFAU）。具有-O - [（碳硼烷-1-基）烷基]磷酸酯，S - [（碳硼烷-1-基）烷基]硫代磷酸酯或Se - [（碳硼烷-1-基）烷基]亚硒酸酯的核苷和寡核苷酸就位的（碳硼烷-1-基）膦酸酯部分。包括一个或多个3'，5'-连接 - （碳硼烷-1-基）膦酸酯部分的特定基因序列的寡核苷酸也可用于基因表达的选择性修饰中的反义治疗。化合物可用于含有硼簇的泌尿生殖系BNCT治疗，作为增强亲脂性的手段，其中硼不富含10B，而是在11B同位素中。通过任何合适的途径施用含硼化合物，包括通过静脉内注射，口服递送或通过导管或其它直接方式，以化合物累积在靶肿瘤中的方式来实现治疗。在化合物在肿瘤中期望的积聚之后，用有效量的低能中子照射该部位。

35. 发明授权

US5827727A Method of resolution of 1,3-oxathiolane nucleoside enantiomers 失效
标题翻译： 1,3-氧硫杂环戊烷核苷对映体的拆分方法
公开(公告)号：US5827727A
公开(公告)日：1998-10-27
申请号：US483653
申请日：1995-06-07
申请人： Dennis C. Liotta , Raymond F. Schinazi , Woo-Baeg Choi , Yung-Chi Cheng
发明人： Dennis C. Liotta , Raymond F. Schinazi , Woo-Baeg Choi , Yung-Chi Cheng
IPC分类号： C07D327/04 , C07D405/04 , C07D411/04 , C07H19/00 , C07H19/06 , C07H19/10 , C12P17/16 , C12P41/00
CPC分类号： C07D327/04 , C07D405/04 , C07D411/04 , C07H19/00 , C07H19/06 , C07H19/10
摘要： A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (-)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner. In particular, deaminase, PPL, PLE and subtilisn are used to resolve 1,3-oxathiolane nucleoside enantiomers.
摘要翻译：一种用于拆分核苷对映异构体外消旋混合物的方法，其包括将外消旋混合物暴露于优先催化其中一种对映异构体中的反应的酶的步骤。核苷对映异构体（ - ） - 2-羟甲基-5-（5-氟胞嘧啶-1-基）-1,3-氧硫杂环戊烷是以类似方式复制的有效的抗HIV，HBV和其他病毒的抗病毒剂。特别地，使用脱氨酶，PPL，PLE和枯草芽孢杆菌来分解1,3-氧硫杂环戊烷核苷对映异构体。

36. 发明授权

US5767122A Enantiomerically pure .beta.-d-dioxolane nucleosides 失效
标题翻译：对映异构体纯的β-二氧戊环核苷
公开(公告)号：US5767122A
公开(公告)日：1998-06-16
申请号：US469465
申请日：1995-06-06
申请人： Chung K. Chu , Raymond F. Schinazi
发明人： Chung K. Chu , Raymond F. Schinazi
IPC分类号： C07D473/18 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/52 , A61K31/522 , A61K31/53 , A61K31/675 , A61K31/7076 , A61K38/21 , A61P31/12 , A61P31/18 , A61P37/04 , C07D327/04 , C07D405/04 , C07D411/04 , C07D473/00 , C07D473/16 , C07D473/30 , C07D473/34 , C07D473/40 , C07D497/08 , C07F9/6561
CPC分类号： C07D473/00 , A61K31/675 , A61K31/70 , A61K31/704 , A61K31/7076 , A61K38/21 , C07D327/04 , C07D411/04 , C07D497/08 , C07B2200/07
摘要： A method and composition for the treatment of humans infected with HIV that includes the administration of an HIV treatment amount of an enantiomerically pure .beta.-D-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.
摘要翻译：用于治疗感染HIV的人的方法和组合物，其包括施用HIV治疗量的下式的对映体纯的β-D-二氧戊环嘌呤核苷：其中R是OH，Cl，NH 2或H ，或化合物的药学上可接受的盐或衍生物，任选地在药学上可接受的载体或稀释剂中。

37. 发明授权

US5512305A Invitroinhibition of the HIV virus with ionic tungstoniobate compounds 失效
标题翻译：用离子桐酯化合物体外抑制HIV病毒
公开(公告)号：US5512305A
公开(公告)日：1996-04-30
申请号：US66007
申请日：1993-08-26
申请人： Michael J. Abrams , Gerald E. Bossard , Craig L. Hill , Raymond F. Schinazi , Brian R. C. Theobald
发明人： Michael J. Abrams , Gerald E. Bossard , Craig L. Hill , Raymond F. Schinazi , Brian R. C. Theobald
IPC分类号： A61K33/24 , A61K33/42 , C01G39/00
CPC分类号： A61K33/24 , A61K33/42
摘要： Tungstoniobate compounds containing an ion of general formula A.sub.x W.sub.y Nb.sub.a O.sub.b !.sup.p- Iwhere A=P, Si, Ge, x=0 or an integer from 1 to 10, y is an integer from 1 to 10, y is an integer from 1 to 40, a is an integer from 1 to 8, b is an integer from 15 to 150, and p is an integer dependent upon the nature and oxidation state of element A, have been found to be active against viruses including especially HIV and Herpes Simplex. Pharmaceutical compositions and methods of treatment are disclosed.
摘要翻译： PCT No.PCT / GB91 / 02101 Sec。 371日期：1993年8月26日 102（e）日期1993年8月26日PCT 1991年11月27日PCT公布。出版物WO92 / 09292 日期：1992年6月11日，含有通式[Ax Wy Nba Ob] pI的离子的噻吩类化合物，其中A = P，Si，Ge，x = 0或1至10的整数，y为1至10的整数 y为1至40的整数，a为1至8的整数，b为15至150的整数，p为取决于元素A的性质和氧化态的整数，已被发现是有活性的针对特别是HIV和单纯疱疹的病毒。公开了药物组合物和治疗方法。

38. 发明授权

US5444063A Enantiomerically pure .beta.-D-dioxolane nucleosides with selective anti-Hepatitis B virus activity 失效
标题翻译：具有选择性抗乙型肝炎病毒活性的对映异构体纯的β-二氧戊环核苷
公开(公告)号：US5444063A
公开(公告)日：1995-08-22
申请号：US967460
申请日：1992-10-28
申请人： Raymond F. Schinazi
发明人： Raymond F. Schinazi
IPC分类号： C07D473/18 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/52 , A61K31/522 , A61K31/53 , A61K31/675 , A61K31/70 , A61K31/7076 , A61K31/708 , A61K38/21 , A61P31/12 , A61P31/18 , A61P31/20 , A61P37/04 , C07D327/04 , C07D405/04 , C07D411/04 , C07D473/00 , C07D473/02 , C07D473/16 , C07D473/30 , C07D473/32 , C07D473/34 , C07D473/40 , C07D497/08
CPC分类号： A61K31/70 , A61K31/52 , A61K31/675 , A61K31/704 , A61K31/7076 , A61K31/708 , A61K38/21 , C07D327/04 , C07D411/04 , C07D473/00 , C07D497/08
摘要： A method and composition for the treatment of humans infected with HBV that includes the administration of an HBV treatment amount of a .beta.-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.
摘要翻译：用于治疗感染HBV的人的方法和组合物，其包括给予HBV治疗量的下式的β-二氧杂环戊基嘌呤核苷：其中R是OH，Cl，NH 2或H，或药学上化合物的可接受的盐或衍生物，任选地在药学上可接受的载体或稀释剂中。

39. 发明授权

US5304554A 4-[(alkyl or dialkyl)amino]quinolines and their method of preparation 失效
标题翻译： 4 - [（烷基或二烷基）氨基]喹啉及其制备方法
公开(公告)号：US5304554A
公开(公告)日：1994-04-19
申请号：US849790
申请日：1992-03-11
申请人： Lucjan Strekowski , Roman L. Wydra , Steven E. Patterson , Raymond F. Schinazi
发明人： Lucjan Strekowski , Roman L. Wydra , Steven E. Patterson , Raymond F. Schinazi
IPC分类号： C07D215/46 , C07D221/18 , C07D401/04 , C07D401/14 , C07D405/04 , C07D409/04 , C07D471/04 , C07D491/04 , C07D495/04 , A61K31/54 , A61K31/495 , A61K31/50 , A61K31/535
CPC分类号： C07D401/04 , C07D215/46 , C07D221/18 , C07D401/14 , C07D405/04 , C07D409/04 , C07D471/04 , C07D491/04 , C07D495/04
摘要： Novel 4-[(alkyl or dialkyl)amino]quinolines are disclosed that are prepared by condensinBACKGROUND OF THE INVENTIONThe United States government has rights in this invention as a result of a grant from the NIAID of the National Institute of Health, Bethesda, Md.
摘要翻译：公开了通过2-（三氟甲基）苯胺或其衍生物与烷基乙烯基酮和烷基酮，烷基杂芳基酮或环酮酮缩合制备的新的4 - [（烷基或二烷基）氨基]喹啉，相应的酮亚胺，其被阴离子环化成喹啉。喹啉可用作DNA的嵌入剂，并且还抑制包括HIV在内的逆转录病毒的复制。

40. 发明授权

US5281616A Porphyrin and phthalocyanine antiviral compositions 失效
标题翻译：卟啉和酞菁抗病毒组合物
公开(公告)号：US5281616A
公开(公告)日：1994-01-25
申请号：US873415
申请日：1992-04-24
申请人： Dabney W. Dixon , Raymond F. Schinazi , Luigi G. Marzilli
发明人： Dabney W. Dixon , Raymond F. Schinazi , Luigi G. Marzilli
IPC分类号： A61K31/40 , A61K31/44 , A61K31/66 , A61K33/24 , A61K38/21
CPC分类号： A61K31/44 , A61K31/40 , A61K31/66 , A61K31/70 , A61K33/24 , A61K38/21 , Y10S530/826
摘要： Compositions for the inhibition of replication of human immunodeficiency virus containing one or more "porphyrins" possessing antiviral activity. As used herein "porphyrins" includes porphyrins, phthalocyanines, chlorins, metallo derivatives thereof, and other porphyrin-like compounds. Examples of natural and synthetic, positively, negatively, and neutrally charged porphyrins, phthalocyanines, and derivatives thereof have been found to exhibit selective anti-HIV activity which is not dependent on the presence of light.
摘要翻译：用于抑制含有一种或多种具有抗病毒活性的“卟啉”的人类免疫缺陷病毒复制的组合物。如本文所用，“卟啉”包括卟啉，酞菁，二氢卟酚，其金属衍生物和其它卟啉样化合物。已经发现天然和合成，正，负和中性带电的卟啉，酞菁及其衍生物的实例表现出不依赖于光的选择性抗HIV活性。

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