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1. 发明授权

US06362329B1 Process to prepare pyrimidine nucleosides 失效
标题翻译：制备嘧啶核苷的方法
公开(公告)号：US06362329B1
公开(公告)日：2002-03-26
申请号：US09618783
申请日：2000-07-18
申请人： Elie Abushanab , Palle V. P. Pragnacharyulu
发明人： Elie Abushanab , Palle V. P. Pragnacharyulu
IPC分类号： C07H19073
CPC分类号： C07H19/06
摘要： A process for the production of a compound of the formula: wherein R1 is hydrogen, alkyl, C1-C16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cyano, carboxy, carboxy esters, carboxamido, N-mono substituted and N,N-disubstituted carboxamido with alkyl, aralkyl and aryl groups; R2 is hydrogen, alkyl C1-C16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl; R3 is alkyl C2-C6, branched alkyl, aryl C2-C6, substituted aryl and R4 is halogen or H. A condensation reaction is effected between compounds of the formulae: to form a novel compound of the formula: Compound (2) is acylated with a compound of the formula: R3COCl to form a novel compound of the formula: Compound (3) is mixed with pyridine and is reacted with thionyl chloride to form compound (4) and compound (4) is dehalogenated to form compound (5).
摘要翻译：制备下式化合物的方法：其中R 1是氢，烷基，C 1 -C 16取代的烷基，芳基，取代的芳基，芳烷基，取代的芳烷基，烯基，取代的烯基，炔基，取代的炔基，氰基，羧基，羧基酯，甲酰氨基，N-单取代和N，N-二取代的甲酰氨基与烷基，芳烷基和芳基; R2是氢，烷基C1-C16取代的烷基，芳基，取代的芳基，芳烷基，取代的芳烷基，烯基，取代的烯基，炔基，取代的炔基; R3是烷基C2-C6，支链烷基，芳基C2-C6，取代的芳基，R4是卤素或在下式化合物之间进行HA缩合反应：形成下式的新化合物：化合物（2）用形成下式的新化合物：将化合物（3）与吡啶混合并与亚硫酰氯反应形成化合物（4），化合物（4）脱卤以形成化合物（5）。

2. 发明授权

US06596859B1 Process to prepare pyrimidine nucleosides 失效
标题翻译：制备嘧啶核苷的方法
公开(公告)号：US06596859B1
公开(公告)日：2003-07-22
申请号：US09618780
申请日：2000-07-18
申请人： Elie Abushanab , Palle V. P. Pragnacharyulu
发明人： Elie Abushanab , Palle V. P. Pragnacharyulu
IPC分类号： C07H100
CPC分类号： C07H19/06
摘要： A process for the production of a compound of the formula: wherein R1 is hydrogen, alkyl, C1-C16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cyano, carboxy, carboxy esters, carboxamido, N-mono substituted and N,N-disubstituted carboxamido with alkyl, aralkyl and aryl groups; R2 is hydrogen, alkyl C1-C16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl; R3 is alkyl C2-C6, branched alkyl, aryl C2-C, substituted aryl and R4 is halogen or H. A condensation reaction is effected between compounds of the formulae: to form a novel compound of the formula: Compound (2) is acylated with a compound of the formula: R3COCl to form a novel compound of the formula: Compound (3) is mixed with pyridine and is reacted with thionyl chloride to form compound (4) and compound (4) is dehalogenated to form compound (5).
摘要翻译：制备下式化合物的方法：其中R1是氢，烷基，C1-C16取代的烷基，芳基，取代的芳基，芳烷基，取代的芳烷基，烯基，取代的烯基，炔基，取代的炔基，氰基，羧基，羧基酯，甲酰氨基，N-单取代和N，N-二取代的甲酰氨基与烷基，芳烷基和芳基; R2是氢，烷基C1-C16取代的烷基，芳基，取代的芳基，芳烷基，取代的芳烷基，烯基，取代的烯基，炔基，取代的炔基; R3是烷基C2-C6，支链烷基，芳基C2-C，取代的芳基，R4是卤素或在下式化合物之间进行HA缩合反应：形成下式的新化合物：化合物（2）用化合物R3COCl形成下式新化合物：将化合物（3）与吡啶混合，并与亚硫酰氯反应形成化合物（4），化合物（4）脱卤以形成化合物（5）。

3. 发明授权

US5703084A Adenosine deaminase inhibitors 失效
标题翻译：腺苷脱氨酶抑制剂
公开(公告)号：US5703084A
公开(公告)日：1997-12-30
申请号：US680413
申请日：1996-07-15
申请人： Elie Abushanab , Palle V. P. Pragnacharyulu
发明人： Elie Abushanab , Palle V. P. Pragnacharyulu
IPC分类号： C07D473/34 , A61K31/52 , A61P43/00 , C07D473/00 , C07D473/18
CPC分类号： C07D473/00
摘要： This invention disclosed (2S,3R)-3(6-aminopurin-9-yl) aralkan-2-ols, a novel class of adenine derivatives (also called 9-aralkyladenines, ARADS), which have been shown to inhibit the enzyme adenosine deaminase at therapeutically useful levels. The relevant inhibitory constant (K.sub.i) values are in the range of 10.sup.-7 -10.sup.-10 M. These compounds with potencies in this range can reversibly inhibit ADA in an effective manner, without permanently deactivating the enzyme. ADA inhibitors that have similar biological profiles have been shown to be of therapeutic value when used to protect heart muscle against ischemic damage.
摘要翻译：本发明公开了已显示抑制酶腺苷的新一类腺嘌呤衍生物（也称为9-芳烷基腺嘌呤，ARADS）的（2S，3R）-3（6-氨基嘌呤-9-基）芳烷基-2- 脱氨酶在治疗有用的水平。相关抑制常数（Ki）值在10-7-10-10M的范围内。这些具有该范围内效力的化合物可以以有效的方式可逆地抑制ADA，而不会使酶永久失活。具有相似生物学特征的ADA抑制剂已被证明在用于保护心肌免受缺血性损伤时具有治疗价值。

4. 发明授权

US06326491B1 Process to prepare pyrimidine nucleosides 失效
标题翻译：制备嘧啶核苷的方法
公开(公告)号：US06326491B1
公开(公告)日：2001-12-04
申请号：US09618247
申请日：2000-07-18
申请人： Elie Abushanab , Palle V. P. Pragnacharyulu
发明人： Elie Abushanab , Palle V. P. Pragnacharyulu
IPC分类号： C07H100
CPC分类号： C07H19/06
摘要： A process for the production of a compound of the formula: wherein R1 is hydrogen, alkyl, C1-C16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cyano, carboxy, carboxy esters, carboxamido, N-mono substituted and N,N-disubstituted carboxamido with alkyl, aralkyl and aryl groups; R2 is hydrogen, alkyl C1-C16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl; R3 is alkyl C2-C6, branched alkyl, aryl C2-C6, substituted aryl and R4 is halogen or H. A condensation reaction is effected between compounds of the formulae: to form a novel compound of the formula: Compound (2) is acylated with a compound of the formula: R3COCl to form a novel compound of the formula: Compound (3) is mixed with pyridine and is reacted with thionyl chloride to form compound (4) and compound (4) is dehalogenated to form compound (5).
摘要翻译：制备下式化合物的方法：其中R1是氢，烷基，C1-C16取代的烷基，芳基，取代的芳基，芳烷基，取代的芳烷基，烯基，取代的烯基，炔基，取代的炔基，氰基，羧基，羧基酯，甲酰氨基，N-单取代和N，N-二取代的甲酰氨基与烷基，芳烷基和芳基; R2是氢，烷基C1-C16取代的烷基，芳基，取代的芳基，芳烷基，取代的芳烷基，烯基，取代的烯基，炔基，取代的炔基; R3是烷基C2-C6，支链烷基，芳基C2-C6，取代的芳基，R4是卤素或在下式化合物之间进行HA缩合反应：形成下式的新化合物：化合物（2）用形成下式的新化合物：将化合物（3）与吡啶混合并与亚硫酰氯反应形成化合物（4），化合物（4）脱卤以形成化合物（5）。

5. 发明授权

US6121438A Process to prepare pyrimidine nucleosides 失效
标题翻译：制备嘧啶核苷的方法
公开(公告)号：US6121438A
公开(公告)日：2000-09-19
申请号：US327739
申请日：1999-06-08
申请人： Elie Abushanab , Palle V. P. Pragnacharyulu
发明人： Elie Abushanab , Palle V. P. Pragnacharyulu
IPC分类号： C07H19/06 , C07H19/073
CPC分类号： C07H19/06
摘要： A process for the production of a compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl C.sub.1 -C.sub.16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cyano, carboxy, carboxy esters, carboxamido, N-mono substituted and N,N-disubstituted carboxamido with alkyl, aralkyl and aryl groups; R.sub.2 is hydrogen, alkyl C.sub.1 -C.sub.16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl; R.sub.3 is alkyl C.sub.2 -C.sub.6, branched alkyl, aryl C.sub.2 -C.sub.6, substituted aryl and R.sub.4 is halogen or H. A condensation reaction is effected between compounds of the formulae: ##STR2## to form a novel compound of the formula: ##STR3## Compound (2) is acylated with a compound of the formula:R.sub.3 COClto form a novel compound of the formula: ##STR4## Compound (3) is mixed with pyridine and is reacted with thionyl chloride to form compound (4) and compound (4) is dehalogenated to form compound (5).
摘要翻译：制备下式化合物的方法：其中R 1是氢，烷基C 1 -C 16取代的烷基，芳基，取代的芳基，芳烷基，取代的芳烷基，烯基，取代的烯基，炔基，取代的炔基，氰基，羧基，羧基酯芳基，芳烷基和芳基; N，N-二取代的甲酰氨基; R2是氢，烷基C1-C16取代的烷基，芳基，取代的芳基，芳烷基，取代的芳烷基，烯基，取代的烯基，炔基，取代的炔基; R3是烷基C2-C6，支链烷基，芳基C2-C6，取代的芳基，R4是卤素或H.在下式化合物之间进行缩合反应：形成下式的新型化合物：化合物（2）被酰化与下式的化合物反应形成下式化合物：化合物（3）与吡啶混合并与亚硫酰氯反应形成化合物（4），化合物（4）脱卤以形成化合物（5）。

6. 发明授权

US5932719A Process to prepare pyrimidine nucleosides 失效
公开(公告)号：US5932719A
公开(公告)日：1999-08-03
申请号：US956336
申请日：1997-10-23
申请人： Elie Abushanab , Palle V. P. Pragnacharyulu
发明人： Elie Abushanab , Palle V. P. Pragnacharyulu
IPC分类号： C07H19/06 , C07H1/00 , C07H19/073
CPC分类号： C07H19/06
摘要： A process for the production of a compound of the formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl C.sub.1 -C.sub.16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cyano, carboxy, carboxy esters, carboxamido, N-mono substituted and N,N-disubstituted carboxamido with alkyl, aralkyl and aryl groups; R.sub.2 is hydrogen, alkyl C.sub.1 -C.sub.16 substituted alkyl, aryl, substituted aryl, aralkyl, substituted aralkyls, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl; R.sub.3 is alkyl C.sub.2 -C.sub.6, branched alkyl, aryl C.sub.2 -C.sub.6, substituted aryl and R.sub.4 is halogen or H.A condensation reaction is effected between compounds of the formulae: ##STR2## to form a novel compound of the formula: ##STR3## Compound (2) is acylated with a compound of the formula:R.sub.3 COCl to form a novel compound of the formula: ##STR4## Compound (3) is mixed with pyridine and is reacted with thionyl chloride to form compound (4) and compound (4) is dehalogenated to form compound (5).

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