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111. 发明授权

US5646155A Drugs to prevent recurrent herpes virus infections 失效
标题翻译：药物可预防复发性疱疹病毒感染
公开(公告)号：US5646155A
公开(公告)日：1997-07-08
申请号：US365769
申请日：1994-12-29
申请人： George E. Wright
发明人： George E. Wright
IPC分类号： C07D473/16 , A61K31/52 , A61K31/522 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P31/12 , A61P31/22 , C07D473/00 , C07D473/18 , C07D473/32 , C07D473/40 , C07H19/16 , C07H19/173
CPC分类号： C07D473/00 , C07D473/18 , C07H19/16
摘要： N.sup.2 -substituted alkylguanine and N.sup.2 -substituted phenylguanine compounds which prevent recurrent herpes simplex infections are disclosed. By virtue of their ability to inhibit herpes virus thymidine kinase in vivo, such compounds will prevent, reduce the frequency of, or reduce the severity of recurring HSV infections in humans. The N.sup.2 -alkylguanine compounds are of the formula: ##STR1## where R.sub.1 is a normal or branched chain C.sub.n H.sub.2n+1 (where n is 1-12); R.sub.2 is H, 2-deoxyribofuranosyl, (CH.sub.2).sub.n OH (where n is 2-5), CH.sub.2 CH(OH)CH.sub.2 OH, (CH.sub.2).sub.n --COOH (where n is 1-4), CH.sub.2 CH(OH)CH.sub.2 --O--COR.sub.4, (CH.sub.2).sub.n --O--COR.sub.4 (where n is 2-5), or (CH.sub.2).sub.n CO--OR.sub.4 (where n is 1-4); R.sub.4 is CH.sub.3, CH.sub.2 CH.sub.3, CH.sub.2 CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 N(C.sub.2 H.sub.5).sub.2 or CH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.3 is OH, H, Cl or NH.sub.2, or a tautomer or a pharmaceutically acceptable salt thereof. The N.sup.2 -substituted phenylguanine compounds are of similar structure, where R.sub.1 is a phenyl or a phenyl substituted at the 3 and 4 positions with an H, a hydrophobic or electron extracting group, or a CH.sub.2 CH.sub.3.
摘要翻译：公开了N 2取代的烷基鸟嘌呤和N 2取代的苯基鸟嘌呤化合物，其预防复发性单纯疱疹感染。由于其在体内抑制疱疹病毒胸苷激酶的能力，这样的化合物将预防，降低人的复发性HSV感染的频率或降低其严重性。 N 2烷基鸟嘌呤化合物具有下式：其中R 1是正链或支链C n H 2n + 1（其中n是1-12）; R2是H，2-脱氧呋喃糖基，（CH2）nOH（其中n是2-5），CH2CH（OH）CH2OH，（CH2）n-COOH（其中n是1-4），CH2CH（OH）CH2-O- COR4，（CH2）nO-COR4（其中n为2-5）或（CH2）nCO-OR4（其中n为1-4）; R4是CH3，CH2CH3，CH2CH2NH2，CH2CH2N（C2H5）2或CH2CH2CO2H; 并且R 3是OH，H，Cl或NH 2，或互变异构体或其药学上可接受的盐。 N 2取代的苯基鸟嘌呤化合物具有相似的结构，其中R 1是苯基或在3和4位被H，疏水或电子提取基团或CH 2 CH 3取代的苯基。

112. 发明授权

US5616702A 2-'-ethenylidene cytidine, uridine and guanosine derivatives 失效
标题翻译： 2-乙烯基胞苷，尿苷和鸟苷衍生物
公开(公告)号：US5616702A
公开(公告)日：1997-04-01
申请号：US362366
申请日：1994-12-22
申请人： Michael L. Edwards , Donald P. Matthews , James R. McCarthy
发明人： Michael L. Edwards , Donald P. Matthews , James R. McCarthy
IPC分类号： C07H19/06 , C07H19/073 , C07H19/16 , C07H19/173 , C07H19/73
CPC分类号： C07H19/06 , C07H19/16
摘要： This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
摘要翻译：本发明涉及某些新的2'-卤代亚甲基，2'-亚乙基和2'-乙炔基胞苷，尿苷和鸟苷衍生物及其组合物，其可用于治疗患有肿瘤或病毒疾病状态的患者。

113. 发明授权

US5616566A Method of inhibiting HIV replication with 2',3'-dideoxyadenosine 失效
标题翻译：用2'，3'-二脱氧腺苷抑制HIV复制的方法
公开(公告)号：US5616566A
公开(公告)日：1997-04-01
申请号：US056043
申请日：1993-04-30
申请人： Hiroaki Mitsuya , Samuel Broder , Robert Yarchoan
发明人： Hiroaki Mitsuya , Samuel Broder , Robert Yarchoan
IPC分类号： A61K31/70 , C07D473/16 , C07H19/167 , C07H19/173 , C07H19/20
CPC分类号： A61K31/70
摘要： A method for inhibiting intracellular replication of HIV in an HIV-infected individual comprising contacting the HIV reverse transcriptase in the HIV-infected cells with 2',3'-dideoxyadenosine-5'-triphosphate whose source is 2',3'-dideoxyadenosine or a pharmaceutically acceptable salt or prodrug thereof.
摘要翻译：一种用于在HIV感染个体中抑制HIV的细胞内复制的方法，其包括将HIV感染细胞中的HIV逆转录酶与来源为2'，3'-双脱氧腺苷或其衍生物的2'，3'-二脱氧腺苷-5'-三磷酸其药学上可接受的盐或前药。

114. 发明授权

US5580860A Pharmaceutical composition containing 2-amino-6-chloropurine-9-.beta.-D-2',3'-dideoxyribofuranoxside 失效
标题翻译：含有2-氨基-6-氯嘌呤-9β-D-2'，3'-二脱氧呋喃核糖苷的药物组合物
公开(公告)号：US5580860A
公开(公告)日：1996-12-03
申请号：US446155
申请日：1989-12-05
申请人： Eiji Kojima , Hidetoshi Yoshioka , Kunichika Murakami , Hiroaki Mitsuya , Takuma Shirasaka , Samuel Broder
发明人： Eiji Kojima , Hidetoshi Yoshioka , Kunichika Murakami , Hiroaki Mitsuya , Takuma Shirasaka , Samuel Broder
IPC分类号： C07D473/40 , A61K31/52 , A61P31/12 , A61P31/18 , A61P37/04 , C07D473/00 , A61K31/70 , C07H19/173
CPC分类号： A61K31/70 , C07D473/00
摘要： An anti-AIDS virus agent is disclosed, which is characterized in that it contains the 2',3'-dideoxypurinenucleosides represented by the chemical formula (I): ##STR1## as an effective ingredient.
摘要翻译：公开了一种抗艾滋病病毒药物，其特征在于它含有以化学式（I）表示的2'，3'-二脱氧尿核苷：作为有效成分。

115. 发明授权

US5563049A 2',3'-dideoxy purine nucleosides and process for the preparation thereof 失效
标题翻译： 2'，3'-双脱氧嘌呤核苷及其制备方法
公开(公告)号：US5563049A
公开(公告)日：1996-10-08
申请号：US405395
申请日：1995-03-15
申请人： Eiji Kojima , Hidetoshi Yoshioka , Hidenori Fukinbara , Kunichika Murakami
发明人： Eiji Kojima , Hidetoshi Yoshioka , Hidenori Fukinbara , Kunichika Murakami
IPC分类号： C12P17/18 , A61K31/52 , A61P31/12 , C07D473/00 , C07D473/24 , C07D473/38 , C07D473/40 , C07D487/04 , C07H19/06 , C07H19/12 , C07H19/14 , C07H19/16 , C07H19/173 , C12N15/09 , C12R1/01 , C12R1/19 , C12R1/22 , C12P19/40
CPC分类号： C07H19/06 , C07H19/12 , C07H19/14 , C07H19/16 , Y10S435/847 , Y10S435/849 , Y10S435/852
摘要： 2',3'-Dideoxy purine nucleosides represented by following general formulae [I] and/or [II] ##STR1## (wherein X and Y indicate nitrogen atoms or carbon atoms and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 indicate each independently any of hydrogen atom, hydroxyl group, amino group, alkyl group, halogen atom, alkoxy group and mercapto group) are produced by bioconversion with strains of E. coli, K. pneumoniae and E. herbicola.
摘要翻译： 2'，3'-二脱氧嘌呤核苷由以下通式[I]和/或[II]表示：其中X和Y表示氮原子或碳原子，R1，R2 ，R3，R4和R5各自独立地表示氢原子，羟基，氨基，烷基，卤素原子，烷氧基和巯基中的任何一个），通过用大肠杆菌，肺炎克雷伯杆菌和大肠杆菌。

116. 发明授权

US4997924B1 5'-deoxy-4',-5'-unsaturated-5'-substituted adenosines 失效
标题翻译： 5'-脱氧-4'，-5'-不饱和-5'-取代腺苷
公开(公告)号：US4997924B1
公开(公告)日：1995-11-14
申请号：US44589289
申请日：1989-11-29
申请人： MERRELL PHARMA INC
发明人： JARVI ESA T , MCCARTHY JAMES R , PRAKASH NELL KUNJA J
IPC分类号： C07D249/18 , A61K31/41 , A61K31/435 , A61K31/495 , A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7076 , A61P31/12 , C07D471/04 , C07D473/00 , C07D473/16 , C07D473/32 , C07D473/34 , C07D473/40 , C07D487/04 , C07H19/052 , C07H19/056 , C07H19/12 , C07H19/16 , C07H19/23 , C07H19/167 , C07H19/173
CPC分类号： C07D473/00 , C07H19/052 , C07H19/056 , C07H19/16

117. 发明授权

US5459255A N-2 substituted purines 失效
标题翻译： N-2取代嘌呤
公开(公告)号：US5459255A
公开(公告)日：1995-10-17
申请号：US159088
申请日：1993-11-29
申请人： P. Dan Cook , Kanda S. Ramasamy , Muthiah Manoharan
发明人： P. Dan Cook , Kanda S. Ramasamy , Muthiah Manoharan
IPC分类号： C07D473/16 , A61K31/415 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61K31/7088 , A61K38/00 , A61K47/48 , A61K48/00 , A61P31/12 , C07D473/18 , C07D487/04 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/167 , C07H19/173 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04 , C07H23/00 , C07J43/00 , C12N9/02 , C12N15/113 , C12Q1/68 , C07H19/00
CPC分类号： C07H19/16 , A61K47/48007 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C07H23/00 , C07J43/003 , C12N15/113 , C12N15/1131 , C12N15/1132 , C12N15/1133 , C12N15/1135 , C12N15/1137 , C12N15/1138 , C12N9/0069 , C12Q1/68 , C12Y113/11012 , A61K38/00 , A61K48/00 , C12N2310/3125 , C12N2310/315 , C12N2310/318 , C12N2310/32 , C12N2310/321 , C12N2310/322 , C12N2310/33 , C12N2310/333 , C12N2310/336 , C12N2310/3521 , C12N2310/3523 , C12N2310/3527 , C12N2310/3531 , C12N2310/3533
摘要： This invention presents novel purine-based compounds for inclusion into oligonucleotides. The compounds of the invention, when incorporated into oligonucleotides are especially useful as agents that are capable of specific hybridization with a nucleotide sequence of an RNA. Oligonucleotides are used for a variety of purposes, such as regulating gene expression in experimental systems, assaying for RNA and for RNA products through the employment of interactions with such RNA, diagnosing diseases, modulating the production of proteins, and cleaving RNA in site specific fashions. The compounds of the invention include novel heterocyclic bases, nucleosides, and nucleotides. When incorporated into oligonucleotides, the compounds of the invention can be useful for modulating the activity of RNA.
摘要翻译：本发明提供了用于纳入寡核苷酸的新型基于嘌呤的化合物。当掺入寡核苷酸时，本发明的化合物特别可用作能够与RNA的核苷酸序列特异性杂交的试剂。寡核苷酸用于各种目的，例如在实验系统中调节基因表达，通过使用与这种RNA的相互作用，诊断疾病，调节蛋白质的产生和在现场特异性时尚中切割RNA来测定RNA和RNA产物。本发明的化合物包括新的杂环碱基，核苷和核苷酸。当掺入寡核苷酸时，本发明的化合物可用于调节RNA的活性。

118. 发明授权

US5378693A 2'-halomethylidene cytidine, uridine and guanosine compounds and their pharmaceutical compositions 失效
标题翻译： 2'-卤代亚甲基胞苷，尿苷和鸟苷化合物及其药物组合物
公开(公告)号：US5378693A
公开(公告)日：1995-01-03
申请号：US113505
申请日：1993-08-27
申请人： James R. McCarthy , Michael L. Edwards , Donald P. Matthews
发明人： James R. McCarthy , Michael L. Edwards , Donald P. Matthews
IPC分类号： A61K31/513 , A61K31/519 , A61K31/522 , A61K31/7072 , A61K31/7076 , C07D473/04 , C07D473/18 , C07D487/02 , C07H19/06 , C07H19/16 , C07H19/073 , C07H19/173
CPC分类号： C07H19/06 , C07H19/16
摘要： This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.
摘要翻译：本发明涉及某些新的2'-卤代亚甲基，2'-亚乙基和2'-乙炔基胞苷，尿苷和鸟苷衍生物及其组合物，其可用于治疗患有肿瘤或病毒疾病状态的患者。

119. 发明授权

US5376642A Treatment of retroviral induced dementia by administration of 2',3'-dideoxyinosine 失效
标题翻译：通过施用2'，3'-二脱氧肌苷治疗逆转录病毒诱导的痴呆
公开(公告)号：US5376642A
公开(公告)日：1994-12-27
申请号：US26188
申请日：1993-03-01
申请人： Robert Yarchoan , Hiroaki Mitsuya , Samuel Broder
发明人： Robert Yarchoan , Hiroaki Mitsuya , Samuel Broder
IPC分类号： A61K31/52 , A61K31/155 , A61K31/42 , A61K31/522 , A61K31/70 , A61P31/12 , C07D473/30 , C07H19/173
CPC分类号： A61K31/70
摘要： A preferred method and dosages for treatment of retrovirus-induced dementia by the administration of 2',3'-dideoxyinosine(ddI) is disclosed.
摘要翻译：公开了通过施用2'，3'-二脱氧肌苷（ddI）治疗逆转录病毒诱导的痴呆的优选方法和剂量。

120. 发明授权

US5290927A Process for preparing 2',3'-dideoxyadenosine 失效
标题翻译：制备2'，3'-二脱氧腺苷的方法
公开(公告)号：US5290927A
公开(公告)日：1994-03-01
申请号：US317567
申请日：1989-03-01
申请人： Yutaka Honda , Hiroshi Shiragami , Hisao Iwagami , Masayuki Arai
发明人： Yutaka Honda , Hiroshi Shiragami , Hisao Iwagami , Masayuki Arai
IPC分类号： C07H19/04 , C07H19/06 , C07H19/16 , C07H19/173 , C07H19/073
CPC分类号： C07H19/04 , C07H19/06 , C07H19/16
摘要： A process for preparing 2',3'-dideoxyadenosine of the formula ##STR1## wherein B is adenine, wherein R.sup.1 is hydrogen, C.sub.1-12 acyl, C.sub.1-12 alkyl, C.sub.7-8 aralkyl, or silyl, said process comprising:reducing a nucleoside of the formula IIIa or IIIb ##STR2## wherein R.sup.2 is hydrogen, C.sub.1-12 acyl, C.sub.1-12 alkyl, C.sub.7-8 aralkyl or silyl; X is Cl, Br or I; R.sup.5 is C.sub.1-12 acyl and B is adenine, with hydrogen in the presence of a palladium catalyst and aqueous solvent mixture of acetonitrile or ethyl acetate and water, said aqueous solvent containing a base selected from the group consisting of sodium hydroxide/sodium acetate and sodium carbonate/sodium acetate, wherein said solvent has a pH of 9-11.
摘要翻译：一种制备式“IMAGE”的2'，3'-二脱氧腺苷的方法，其中B是腺嘌呤，其中R 1是氢，C 1-12酰基，C 1-12烷基，C 7-8芳烷基或甲硅烷基，所述方法包括：（IIIa）（IIIb）其中R2是氢，C1-12酰基，C1-12烷基，C7-8芳烷基或甲硅烷基的式IIIa或IIIb的核苷。 X是Cl，Br或I; R5是C1-12酰基，B是腺嘌呤，在钯催化剂和乙腈或乙酸乙酯与水的水溶剂混合物的存在下，氢气，所述含水溶剂含有选自氢氧化钠/乙酸钠和碳酸钠/乙酸钠，其中所述溶剂的pH为9-11。

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