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1. 发明授权

US07572909B2 Method for the preparation of 2-halo-2′-deoxyadenosine compounds from 2′-deoxyguanosine 有权
标题翻译：从2'-脱氧鸟苷配制2-卤代-2'-脱氧腺苷化合物的方法
公开(公告)号：US07572909B2
公开(公告)日：2009-08-11
申请号：US10529106
申请日：2003-09-25
申请人： Morris J. Robins , Zlatko Janeba , Paula Francom
发明人： Morris J. Robins , Zlatko Janeba , Paula Francom
IPC分类号： C07H19/173
CPC分类号： C07H19/167 , C07H19/173 , Y02P20/55
摘要： The present invention is a method for preparing 2-halo-6-aminopurines, and more specifically for preparing the clinical agent cladribine (2-chloro-2′-deoxyadenosine, CldAdo, 4), a drug of choice against hairy-cell leukemia and other neoplasms, from 2-amino-6-oxopurines, which are readily obtained from the naturally occurring compound 2′-deoxyguanosine. According to the methods of the present invention, the 6-oxo group of a protected 2′-deoxyguanosine (1) is converted to a 6-(substituted oxy) leaving group, or alternatively to a 6-chloro leaving group, the 2-amino group is replaced with a 2-chloro group, the 6-(substituted oxy) leaving group, or alternatively the 6-chloro leaving group, is replaced with a 6-amino group or, alternatively, a 2,6-dichloro substituted compound is selectively replaced with a 6-amino group, and the protecting groups are removed.
摘要翻译：本发明是一种制备2-卤代-6-氨基嘌呤的方法，更具体地说是制备临床药物克拉屈滨（2-氯-2'-脱氧腺苷，CldAdo4），一种针对毛细胞白血病的药物，来自2-氨基-6-氧代嘌呤的其它肿瘤，它们容易从天然存在的化合物2'-脱氧鸟苷中获得。根据本发明的方法，将受保护的2'-脱氧鸟苷（1）的6-氧代基转化为6-（取代的氧基）离去基团，或者选择为6-氯离去基团，氨基被2-氯基取代，6-（取代的氧基）离去基团或另外的6-氯离去基团被6-氨基取代，或者可选地，2,6-二氯取代的化合物被选择性地被6-氨基取代，除去保护基。

2. 发明申请

US20090270604A1 METHOD FOR THE PREPARATION OF 2-HALO-2'-DEOXYADENOSINE COMPOUNDS FROM 2'-DEOXYGUANOSINE 有权
标题翻译：从2'-脱氧葡萄糖苷制备2-脱氧-2'-脱氧肾苷化合物的方法
公开(公告)号：US20090270604A1
公开(公告)日：2009-10-29
申请号：US12497287
申请日：2009-07-02
申请人： Morris J. Robins , Zlatko Janeba , Paula Francom
发明人： Morris J. Robins , Zlatko Janeba , Paula Francom
IPC分类号： C07H19/173
CPC分类号： C07H19/167 , C07H19/173 , Y02P20/55
摘要： The present invention is a method for preparing 2-halo-6-aminopurines, and more specifically for preparing the clinical agent cladribine (2-chloro-2′-deoxyadenosine, CldAdo, 4), a drug of choice against hairy-cell leukemia and other neoplasms, from 2-amino-6-oxopurines, which are readily obtained from the naturally occurring compound 2′-deoxyguanosine. According to the methods of the present invention, the 6-oxo group of a protected 2′-deoxyguanosine (1) is converted to a 6-(substituted oxy) leaving group, or alternatively to a 6-chloro leaving group, the 2-amino group is replaced with a 2-chloro group, the 6-(substituted oxy) leaving group, or alternatively the 6-chloro leaving group, is replaced with a 6-amino group or, alternatively, a 2,6-dichloro substituted compound is selectively replaced with a 6-amino group, and the protecting groups are removed.
摘要翻译：本发明是一种制备2-卤代-6-氨基嘌呤的方法，更具体地说是制备临床药物克拉屈滨（2-氯-2'-脱氧腺苷，CldAdo4），一种针对毛细胞白血病的药物，来自2-氨基-6-氧代嘌呤的其它肿瘤，它们容易从天然存在的化合物2'-脱氧鸟苷中获得。根据本发明的方法，将受保护的2'-脱氧鸟苷（1）的6-氧代基转化为6-（取代的氧基）离去基团，或者选择为6-氯离去基团，氨基被2-氯基取代，6-（取代的氧基）离去基团或另外的6-氯离去基团被6-氨基取代，或者可选地，2,6-二氯取代的化合物被选择性地被6-氨基取代，除去保护基。

3. 发明授权

US5039667A Antiviral therapy for hepatitis B with 2',3'-dideoxypurine nucleosides 失效
标题翻译：用2'，3'-脱氨基嘌呤核苷的乙型肝炎的抗病毒治疗
公开(公告)号：US5039667A
公开(公告)日：1991-08-13
申请号：US228745
申请日：1988-08-05
申请人： David L. J. Tyrrell , Morris J. Robins , Satoru Suzuki
发明人： David L. J. Tyrrell , Morris J. Robins , Satoru Suzuki
IPC分类号： A61K31/70 , C07H19/16 , C07H19/173
CPC分类号： A61K31/70
摘要： A method is disclosed for the treatment of hepadnavirus infection in animals. Animals infected with duck hepatitis B virus may be treated with the 2',3'-dideoxynucleoside of adenine, guanine, hypoxanthine, 2,6-diaminopurine or various analogs of substituted purines. Several purine 2',3'-dideoxynucleosides inhibit duck hepatitis B virus in hepatocyte culture >99% at 1 .mu.g/ml. Potent in vivo efficacy of the 2,6-diaminopurine 2',3'-dideoxynucleoside for clearance of duck hepatitis B virus from the sera of Pekin ducks is demonstrated. The selective effect on hepadnavirus replication by the purine 2',3'-dideoxynucleosides is based on the discovery of an unexpected sensitivity of hepadnavirus to purine 2',3'-dideoxynucleoside analogs. These compounds present a new antiviral therapy of acute or persistent hepadnavirus infections.
摘要翻译：公开了用于治疗动物中的肝炎病毒感染的方法。用乙型肝炎病毒感染的动物可以用腺嘌呤，鸟嘌呤，次黄嘌呤，2,6-二氨基嘌呤或取代嘌呤的各种类似物的2'，3'-二脱氧核苷进行处理。几种嘌呤2'，3'-双脱氧核苷在肝细胞培养中抑制鸭乙型肝炎病毒> 1 9 g / ml。证明了2,6-二氨基嘌呤2'，3'-二脱氧核苷对从北京鸭血清中清除鸭乙型肝炎病毒的有效体内功效。嘌呤2'，3'-双脱氧核苷的肝炎病毒复制的选择性作用是基于肝炎病毒对嘌呤2'，3'-二脱氧核苷类似物的意想不到的敏感性的发现。这些化合物提供了急性或持续性肝炎病毒感染的新抗病毒治疗。

4. 发明授权

US08466275B2 Method for the preparation of 2-halo-2′-deoxyadenosine compounds from 2′-deoxyguanosine 有权
公开(公告)号：US08466275B2
公开(公告)日：2013-06-18
申请号：US12497287
申请日：2009-07-02
申请人： Morris J. Robins , Zlatko Janeba , Paula Francom
发明人： Morris J. Robins , Zlatko Janeba , Paula Francom
IPC分类号： C07H19/173
CPC分类号： C07H19/167 , C07H19/173 , Y02P20/55
摘要： The present invention is a method for preparing 2-halo-6-aminopurines, and more specifically for preparing the clinical agent cladribine (2-chloro-2′-deoxyadenosine, CldAdo, 4), a drug of choice against hairy-cell leukemia and other neoplasms, from 2-amino-6-oxopurines, which are readily obtained from the naturally occurring compound 2′-deoxyguanosine. According to the methods of the present invention, the 6-oxo group of a protected 2′-deoxyguanosine (1) is converted to a 6-(substituted oxy) leaving group, or alternatively to a 6-chloro leaving group, the 2-amino group is replaced with a 2-chloro group, the 6-(substituted oxy) leaving group, or alternatively the 6-chloro leaving group, is replaced with a 6-amino group or, alternatively, a 2,6-dichloro substituted compound is selectively replaced with a 6-amino group, and the protecting groups are removed.

5. 发明授权

US07855285B2 Methods for selective N-9 glycosylation of purines 有权
标题翻译：嘌呤选择性N-9糖基化方法
公开(公告)号：US07855285B2
公开(公告)日：2010-12-21
申请号：US11917544
申请日：2006-06-14
申请人： Morris J. Robins , Minghong Zhong
发明人： Morris J. Robins , Minghong Zhong
IPC分类号： C07H21/00
CPC分类号： C07H19/16 , C07D473/40 , Y02P20/55
摘要： A process for providing regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs is described. The introduction of the sugar moiety on to 6-(azolyl)-substituted purine bases is performed so that highly stereoselective formation of the β anomers of only the 9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs, and in particular 2′-deoxy, 3′-deoxy, 2′-deoxy-2′-halo-arabino and 2′,3′-dideoxy-2′-halo-threo purine nucleoside analogs, in high yields without formation of the 7-positional regioisomers. Processes for providing novel 6-(azolyl)purines for the regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs are described. The compounds are drugs or intermediates to drugs.
摘要翻译：提供9-区域特异性和高度立体选择性合成的方法描述了异头体嘌呤核苷类似物。将糖部分引入到6-（唑基） - 取代的嘌呤碱基上进行，使得高度立体选择性地形成β- 仅获得嘌呤核苷类似物（D或L对映异构体）的9个位置区域异构体的端基异构体。糖部分的这种区域特异性和立体选择性引入允许合成核苷类似物，特别是2'-脱氧-3'-脱氧-2'-脱氧-2'-卤 - 阿拉伯糖和2'，3'-二脱氧-2 '-al-threo嘌呤核苷类似物，高产率而不形成7-位置区域异构体。提供用于区域特异性和高度立体选择性合成9- [bgr]的新型6-（唑基）嘌呤的方法。描述了异头体嘌呤核苷类似物。这些化合物是药物或药物的中间体。

6. 发明申请

US20080207891A1 Methods For Selective N-9 Glycosylation of Purines 有权
标题翻译：嘌呤选择性N-9糖基化方法
公开(公告)号：US20080207891A1
公开(公告)日：2008-08-28
申请号：US11917544
申请日：2006-06-14
申请人： Morris J. Robins , Minghong Zhong
发明人： Morris J. Robins , Minghong Zhong
IPC分类号： C07H19/16 , C07D473/34
CPC分类号： C07H19/16 , C07D473/40 , Y02P20/55
摘要： A process for providing regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs is described. The introduction of the sugar moiety on to 6-(azolyl)-substituted purine bases is performed so that highly stereoselective formation of the β anomers of only the 9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs, and in particular 2′-deoxy, 3′-deoxy, 2′-deoxy-2′-halo-arabino and 2′,3′-dideoxy-2′-halo-threo purine nucleoside analogs, in high yields without formation of the 7-positional regioisomers. Processes for providing novel 6-(azolyl)purines for the regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs are described. The compounds are drugs or intermediates to drugs.
摘要翻译：描述了提供9-β-端基异构嘌呤核苷类似物的区域特异性和高度立体选择性合成的方法。进行糖部分在6-（唑基） - 取代的嘌呤碱基上的进行，从而获得仅嘌呤核苷类似物（D或L对映异构体）的9个位置区域异构体的高度立体选择性形成。糖部分的这种区域特异性和立体选择性引入允许核苷类似物的合成，特别是2'-脱氧-3'-脱氧，2'-脱氧-2'-卤 - 阿拉伯糖和2'，3'-二脱氧-2 '-al-threo嘌呤核苷类似物，高产率而不形成7-位置区域异构体。描述了用于为9-β-端基异构嘌呤核苷类似物的区域特异性和高立体选择性合成提供新的6-（唑基）嘌呤的方法。这些化合物是药物或药物的中间体。

7. 再颁专利

USRE35904E Method and probes for detecting nucleoside transporter and method for producing the probes 失效
标题翻译：用于检测核苷转运蛋白的方法和探针及其制备方法
公开(公告)号：USRE35904E
公开(公告)日：1998-09-22
申请号：US516172
申请日：1995-08-17
申请人： Alan R. P. Paterson , Carol E. Cass , Wendy P. Gati , John K. Buolamwini , Gary P. Jamieson , David P. McAdam , William A. Sawyer , James S. Wiley , James D. Craik , Morris J. Robins
发明人： Alan R. P. Paterson , Carol E. Cass , Wendy P. Gati , John K. Buolamwini , Gary P. Jamieson , David P. McAdam , William A. Sawyer , James S. Wiley , James D. Craik , Morris J. Robins
IPC分类号： C07H19/04 , C07H19/16 , G01N33/50 , G01N33/68 , A61K31/70 , C07H19/167 , G01N33/566
CPC分类号： A61K31/70 , C07H19/04 , C07H19/16 , G01N33/5005 , G01N33/68
摘要： The present invention is directed to compounds capable of binding to the es nucleoside transporter of animal cells having the general formula: ##STR1## wherein n is 1-12; E is H, halogen, NH.sub.2, OH, OCH.sub.3, O(CH.sub.2).sub.n CH.sub.3 (where n is 1 to 12), SH, SR (where R is CH.sub.3 or (CH.sub.2).sub.n CH.sub.3 and n is 1 to 12); A is HN, S, O, Se; X is N or C; Y is N or C; Z is N or C; R.sub.1 is H or acyl; R.sub.2 is C1 to C20 substituted or unsubstituted alkyl or heteroalkyl; substituted or unsubstituted aliphatic carbocycle or heterocycle; substituted or unsubstituted arene or heteroarene, aryl or substituted aryl; heteroaryl or substituted heteroaryl; R.sub.3 is H, halogen, NO.sub.2, N.sub.3, SH, SR (where R is CH.sub.3 or (CH.sub.2).sub.n CH.sub.3 and n is 1 to 12) .Iadd.when Y is C and R.sub.3 is absent when Y is N.Iaddend.; R.sub.4 is H, OH .�.is.!. .Iadd.or .Iaddend.halogen; R.sub.5 is H, OH, halogen, N.sub.3, acetal, hemiacetal.Iadd.; .Iaddend.and R.sub.6 is H, .�.--C.dbd.O--HN.sub.2 .!. .Iadd.--CO--NH.sub.2 .Iaddend.or --C.tbd.N when X is C and R.sub.6 is .�.H.!. .Iadd.absent .Iaddend.when X is N.
摘要翻译：本发明涉及能够结合具有以下通式的动物细胞的核苷转运蛋白的化合物：其中n为1-12; E为H，卤素，NH 2，OH，OCH 3，O（CH 2）n CH 3（其中n为1至12），SH，SR（其中R为CH 3或（CH 2）n CH 3且n为1至12）; A是HN，S，O，Se; X为N或C; Y为N或C; Z是N或C; R1是H或酰基; R2是C1至C20取代或未取代的烷基或杂烷基; 取代或未取代的脂族碳环或杂环; 取代或未取代的芳烃或杂芳烃，芳基或取代的芳基; 杂芳基或取代的杂芳基; 当Y为C时，R 3为H，卤素，NO 2，N 3，SH，SR（其中R为CH 3或（CH 2）n CH 3且n为1至12） R4是H，OH [或]或卤素; R5是H，OH，卤素，N3，缩醛，半缩醛; 当X为C时，R6为H，[-C = O-HN2] -CO-NH2或-C3NN，当X为N时，R6为[H]

8. 发明授权

US5236902A Method and probes for detecting nucleoside transporter and method for producing the probes 失效
标题翻译：用于检测核苷转运蛋白的方法和探针及其制备方法
公开(公告)号：US5236902A
公开(公告)日：1993-08-17
申请号：US617714
申请日：1990-11-26
申请人： Alan R. P. Paterson , Carol E. Cass , Wendy P. Gati , John K. Buolamwini , Gary P. Jamieson , David P. McAdam , William A. Sawyer , James S. Wiley , James D. Craik , Morris J. Robins
发明人： Alan R. P. Paterson , Carol E. Cass , Wendy P. Gati , John K. Buolamwini , Gary P. Jamieson , David P. McAdam , William A. Sawyer , James S. Wiley , James D. Craik , Morris J. Robins
IPC分类号： C07H19/04 , C07H19/16 , G01N33/50 , G01N33/68
CPC分类号： A61K31/70 , C07H19/04 , C07H19/16 , G01N33/5005 , G01N33/68
摘要： The present invention is directed to compounds capable of binding to the es nucleoside transporter of animal cells having the general formula: ##STR1## wherein n is 1-12; E is H, halogen, NH.sub.2, OH, OCH.sub.3, O(CH.sub.2).sub.n CH.sub.3 (where n is 1 to 12), SH, SR (where R is CH.sub.3 or (CH.sub.2).sub.n CH.sub.3 and n is 1 to 12); A is HN, S, O, Se; X is N or C; Y is N or C; Z is N or C; R.sub.1 is H or acyl; R.sub.2 is C1 to C20 substituted or unsubstituted alkyl or heteroalkyl; substituted or unsubstituted aliphatic carbocycle or heterocycle; substituted or unsubstituted arene or heteroarene, aryl or substituted aryl; heteroaryl or substituted heteroaryl; R.sub.3 is H, halogen, NO.sub.2, N.sub.3, SH, SR (where R is CH.sub.3 or (CH.sub.2).sub.n CH.sub.3 and n is 1 to 12); R.sub.4 is H, OH is halogen; R.sub.5 is H, OH, halogen, N.sub.3, acetal, hemiacetal and R.sub.6 is H, --C.dbd.O--HN.sub.2 or --C.dbd.N when X is C and R.sub.6 is H when X is N.
摘要翻译：本发明涉及能够结合具有以下通式的动物细胞的核苷转运蛋白的化合物：其中n为1-12; E为H，卤素，NH 2，OH，OCH 3，O（CH 2）n CH 3（其中n为1至12），SH，SR（其中R为CH 3或（CH 2）n CH 3且n为1至12）; A是HN，S，O，Se; X为N或C; Y为N或C; Z是N或C; R1是H或酰基; R2是C1至C20取代或未取代的烷基或杂烷基; 取代或未取代的脂族碳环或杂环; 取代或未取代的芳烃或杂芳烃，芳基或取代的芳基; 杂芳基或取代的杂芳基; R3是H，卤素，NO2，N3，SH，SR（其中R是CH3或（CH2）nCH3，n是1至12）; R4是H，OH是卤素; 当X为C时，R5为H，OH，卤素，N3，缩醛，半缩醛，R6为H，-C = O-HN2或-C = N，当X为N时，R6为H

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