专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US4880820A Guanine derivatives 失效
标题翻译：鸟嘌呤衍生物
公开(公告)号：US4880820A
公开(公告)日：1989-11-14
申请号：US150478
申请日：1988-02-08
申请人： Wallace T. Ashton , Laura F. Canning , Arthur K. Field , Richard L. Tolman
发明人： Wallace T. Ashton , Laura F. Canning , Arthur K. Field , Richard L. Tolman
IPC分类号： C07D473/00 , C07F9/6561
CPC分类号： C07D473/00 , C07F9/65616
摘要： (S)-9-(2,3-dihydroxy-1-propoxymethyl)guanine has potent antiherpetic activity which is superior to the corresponding racemic mixture or the (R)-enantiomer and also is much more potent than 9-(2-hydroxyethoxymethyl)guanine. Acyl derivatives (prodrugs) of the (S)-enantiomer, which are more effective than the corresponding (R)-enantiomer analogs or related racemic mixtures provide formulation advantages and even higher plasma half lives in animals or man than the (S)-isomer.
摘要翻译：（S）-9-（2,3-二羟基-1-丙氧基甲基）鸟嘌呤具有有效的抗皮肤活性，其优于相应的外消旋混合物或（R） - 对映体，并且还比9-（2-羟基乙氧基甲基）鸟嘌呤。（S） - 对映体的酰基衍生物（前药）比相应的（R） - 对映异构体类似物或相关的外消旋混合物更有效，提供了比（S） - 异构体在动物或人中更好的血浆半衰期。

2. 发明授权

US4816447A Anti-viral guanine compounds 失效
标题翻译：抗病毒鸟嘌呤化合物
公开(公告)号：US4816447A
公开(公告)日：1989-03-28
申请号：US617868
申请日：1984-06-06
申请人： Wallace T. Ashton , Arthur K. Field , John D. Karkas , Richard L. Tolman
发明人： Wallace T. Ashton , Arthur K. Field , John D. Karkas , Richard L. Tolman
IPC分类号： C07D473/18 , A61K31/52 , A61K31/522 , A61P31/12 , C07D473/00 , C07F9/6561
CPC分类号： C07D473/00 , C07F9/65616
摘要： 9-(1,3-Dihydroxy-2-propoxymethyl)guanine and 9-(2,3-dihydroxy-1-propoxymethyl)guanine have been found to have potent anti-viral activity against herpes viruses. These compounds, their acyl derivatives, their phosphate derivatives and their pharmaceutically acceptable salts, pharmaceutical formulations containing these compounds, the treatment of DNA viral or herpes viral infections with these compounds, method of preparing these compounds, and novel intermediates useful in their preparation are all disclosed.The compounds may be prepared by reaction of the appropriate acetoxymethyl ether with diacetylguanine, followed by deprotection. The acetoxymethyl ethers may be obtained by reaction of glycerol formal with acetic anhydride in the presence of a catalyst.
摘要翻译：已经发现9-（1,3-二羟基-2-丙氧基甲基）鸟嘌呤和9-（2,3-二羟基-1-丙氧基甲基）鸟嘌呤对疱疹病毒具有有效的抗病毒活性。这些化合物，其酰基衍生物，其磷酸酯衍生物及其药学上可接受的盐，含有这些化合物的药物制剂，用这些化合物治疗DNA病毒或疱疹病毒感染，制备这些化合物的方法和用于制备这些化合物的新型中间体都是披露化合物可以通过合适的乙酰氧基甲基醚与二乙酰基鸟嘌呤的反应制备，然后脱保护。乙酰氧基甲基醚可以通过甘油缩甲醛与乙酸酐在催化剂存在下反应获得。

3. 发明授权

US4863927A 1-(2-hydroxymethyl)cycloalkylmethyl)-5-substituted uracils 失效
标题翻译： 1-（2-羟甲基）环烷基甲基）-5-取代的尿嘧啶
公开(公告)号：US4863927A
公开(公告)日：1989-09-05
申请号：US48290
申请日：1987-05-11
申请人： Richard L. Tolman , Wallace T. Ashton
发明人： Richard L. Tolman , Wallace T. Ashton
IPC分类号： A61K31/505 , A61P31/12 , A61P31/22 , C07D239/54 , C07D239/553
CPC分类号： C07D239/54 , C07D239/553
摘要： 1-[2-(Hydroxymethyl)cycloalkylmethyl]-5-substituted uracils which are herpes simplex viral thymidine kinase inhibitors, their acyl derivatives, and their pharmaceutically-acceptable salts; pharmaceutical formulations containing these compounds; the treatment of DNA viral, particularly herpes viral, infections with these compounds; methods of preparing these compounds; and novel intermediates useful in their preparation.

4. 发明授权

US4782062A 9-(2-hydroxymethyl)cycloalkylmethyl) guanines 失效
标题翻译： 9-（2-羟甲基）环烷基甲基）鸟嘌呤
公开(公告)号：US4782062A
公开(公告)日：1988-11-01
申请号：US48289
申请日：1987-05-11
申请人： Richard L. Tolman , John D. Karkas , Wallace T. Ashton
发明人： Richard L. Tolman , John D. Karkas , Wallace T. Ashton
IPC分类号： C07D473/18 , A61K31/52 , A61K31/522 , A61P31/12 , C07D473/00
CPC分类号： C07D473/00
摘要： 9-[2-(Hydroxymethyl)cycloalkylmethyl]guanines which are herpes simplex viral thymidine kinase inhibitors, their acyl derivatives, their phosphate derivatives and their pharmaceutically-acceptable salts; pharmaceutical formulations containing these compounds; the treatment of DNA viral, particularly herpes viral, infections with these compounds; methods of preparing these compounds; and novel intermediates useful in their preparation.

5. 发明授权

US4277603A Preparation of 5-deazariboflavins 失效
标题翻译： 5-deazariboflavins的制备
公开(公告)号：US4277603A
公开(公告)日：1981-07-07
申请号：US19986
申请日：1979-03-12
申请人： Richard L. Tolman , Wallace T. Ashton , Ronald D. Brown
发明人： Richard L. Tolman , Wallace T. Ashton , Ronald D. Brown
IPC分类号： C07D239/54 , C07D239/545 , C07D471/04 , C07H15/18
CPC分类号： C07D239/545 , C07D471/04 , C07H15/18
摘要： This invention relates generally to a novel process for preparing 5-deazariboflavins by the cyclization of the corresponding 6-(N-substituted arylamino)uracils with trialkylorthoformate in the presence of a strong acid catalyst. An improved process for preparing the uracil intermediate is also disclosed. More particularly, it is concerned with the process for preparing 5-deazariboflavin by cyclizing 6-[3,4-dimethyl-N-(D-ribityl)anilino[uracil with trialkylorthoformate in the presence of a strong acid catalyst and hydrolyzing the resulting alkoxymethylene derivative. The corresponding uracil intermediate is prepared by reacting 6-chlorouracil with N-D-ribityl-3,4-xylidine.5-Deazariboflavins having the general Formula (I) herein below: ##STR1## wherein R.sub.7 is hydrogen or methyl, R.sub.8 is methyl, hydroxy or acyloxy and R.sub.10 is a ribityl group and the corresponding acyl and alkoxymethylene derivatives are useful as riboflavin antagonists with particular utility for the chemotherapy of coccidiosis in chickens or as intermediates for the preparation of said antagonists. The bis(alkoxymethylene) derivatives described herein are useful as prodrug forms of 5-deazariboflavins.When used for the treatment of coccidiosis, such compounds are administered to the animals by way of the feed and are effective in preventing coccidiosis when administered at levels of from about 0.0005% to about 0.05% by weight of the total feed consumed, the amount required for optimum prevention or control of the disease varying with the particular compound employed.
摘要翻译：本发明一般涉及在强酸催化剂存在下，通过使相应的6-（N-取代的芳基氨基）尿嘧啶与三烷基原甲酸酯环化制备5-脱氮黄素的新方法。还公开了一种制备尿嘧啶中间体的改进方法。更具体地说，它涉及通过在强酸催化剂存在下使6- [3,4-二甲基-N-（D-核糖基）苯胺基[尿嘧啶与三烷基原甲酸酯]环化来制备5-脱氮黄素的方法，并水解得到的烷氧基亚甲基衍生物。通过6-氯尿嘧啶与N-D-核糖基-3,4-二甲苯胺反应制备相应的尿嘧啶中间体。具有下述通式（I）的5-脱氮维生素：其中R 7是氢或甲基，R 8是甲基，羟基或酰氧基，R 10是ribityl基团，并且相应的酰基和烷氧基亚甲基衍生物可用作特定的核黄素拮抗剂用于鸡的球虫病化疗或用作制备所述拮抗剂的中间体的效用。本文所述的双（烷氧基亚甲基）衍生物可用作5-脱氮白蛋白的前药形式。当用于治疗球虫病时，通过饲料将这些化合物施用于动物，并且当以所消耗的总饲料的约0.0005重量％至约0.05重量％的水平施用量时，有效地预防球虫病，所需量用于最佳预防或控制随所用特定化合物变化的疾病。

6. 发明授权

US5114925A Renin inhibitors containing the 2-[[(2R,3S)-3-amino-4-cyclohexyl-2-hydroxy-1-butyl]thio)alkanoyl moiety and the corresponding sulfoxide and sulfone derivatives 失效
标题翻译：含有2 - [[（2R，3S）-3-氨基-4-环己基-2-羟基-1-丁基]硫基）烷酰基部分和相应的亚砜和砜衍生物的肾素抑制剂
公开(公告)号：US5114925A
公开(公告)日：1992-05-19
申请号：US756632
申请日：1991-09-09
申请人： Wallace T. Ashton , Christine L. Cantone , Richard L. Tolman
发明人： Wallace T. Ashton , Christine L. Cantone , Richard L. Tolman
IPC分类号： A61K38/00 , C07C317/44 , C07C323/52 , C07D207/46 , C07D233/54 , C07D295/108 , C07D295/13 , C07D303/36 , C07K5/02
CPC分类号： C07D233/64 , C07C317/44 , C07C323/52 , C07D207/46 , C07D295/108 , C07D295/13 , C07D303/36 , C07K5/0227 , A61K38/00
摘要： Compounds of the formula: ##STR1## which are potent inhibitors of human renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory compounds, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these conditions which employ these novel compounds.
摘要翻译：下式的化合物：其是人肾素的有效抑制剂，可用于治疗各种形式的肾素相关性高血压，醛固酮增多症和充血性心力衰竭; 含有这些肾素抑制性化合物的组合物，任选与其它抗高血压药物组合; 以及治疗高血压，醛固酮增多症或充血性心力衰竭的方法，或在使用这些新化合物的这些病症中建立肾素作为致病因子。

7. 发明授权

US5110799A Antiherpetic agents 失效
标题翻译：抗菌剂
公开(公告)号：US5110799A
公开(公告)日：1992-05-05
申请号：US386071
申请日：1989-07-28
申请人： Richard L. Tolman , Wallace T. Ashton , Mu T. Wu
发明人： Richard L. Tolman , Wallace T. Ashton , Mu T. Wu
IPC分类号： A61K38/00 , A61P31/12 , A61P31/22 , C07D233/54 , C07K5/06 , C07K5/072 , C07K5/078 , C07K5/08 , C07K5/097
CPC分类号： C07D233/64 , C07K5/06113 , C07K5/06139 , C07K5/06147 , A61K38/00
摘要： A series of carboxyl-containing N-alkyldipeptides have been found to posess antiviral potency--specifically against herpes simplex virus--by selectively inhibiting the viral ribonucleotide reductase enzyme.

8. 发明授权

US4859680A Pyrimidine derivatives as antiviral compounds 失效
标题翻译：嘧啶衍生物作为抗病毒化合物
公开(公告)号：US4859680A
公开(公告)日：1989-08-22
申请号：US157076
申请日：1988-02-04
申请人： Wallace T. Ashton , Edward Walton , Richard L. Tolman
发明人： Wallace T. Ashton , Edward Walton , Richard L. Tolman
IPC分类号： A61K31/505 , C07D233/90 , C07D239/46 , C07D239/48 , C07D239/50 , C07D239/54 , C07D303/16 , C07D471/04 , C07D473/00 , C07D487/04
CPC分类号： C07D239/47 , C07C255/00 , C07D233/90 , C07D239/48 , C07D239/50 , C07D239/54 , C07D303/16 , C07D471/04 , C07D473/00 , C07D487/04
摘要： Pyrimidines having a fused cyclopropane ring in the side chain and the heterocyclic isosteres of said pyrimidines, which have antiviral activity, especially against viruses of the herpes class.
摘要翻译：具有侧链中稠合环丙烷环的嘧啶和所述嘧啶的杂环等位基团，其具有抗病毒活性，特别是抗疱疹病毒的抗病毒活性。

9. 发明授权

US4755516A Antiviral compounds 失效
标题翻译：抗病毒化合物
公开(公告)号：US4755516A
公开(公告)日：1988-07-05
申请号：US035127
申请日：1987-04-06
申请人： Richard L. Tolman , Wallace T. Ashton
发明人： Richard L. Tolman , Wallace T. Ashton
IPC分类号： C07D317/24 , C07D473/00 , C07F9/6561 , C07D473/02 , A61K31/52
CPC分类号： C07D473/00 , C07D317/24 , C07F9/65616
摘要： 4-(Guanin-9-yl)butanals and their 3-oxa, 3-thia, and 2-ene counterparts and derivatives thereof, wherein the aldehyde is protected, which have antiviral activity, and are useful in treating viral infections, particularly herpes viral infections, such as herpes simplex viral infections, in mammals (especially humans), birds or fish.
摘要翻译： 4-（胍基-9-基）丁醛及其3-氧杂，3-硫杂和2-烯对应物及其衍生物，其中所述醛被保护，其具有抗病毒活性，并且可用于治疗病毒感染，特别是疱疹病毒感染，如单纯疱疹病毒感染，哺乳动物（尤其是人类），鸟类或鱼类。

10. 再颁专利

USRE39056E1 4-Azasteroids for treatment of hyperandrogenic conditions 失效
标题翻译： 4-Azasteroids用于治疗雄激素过多的病症
公开(公告)号：USRE39056E1
公开(公告)日：2006-04-04
申请号：US10020740
申请日：1996-09-11
申请人： Raman K. Bakshi , Soumya P. Sahoo , Richard L. Tolman
发明人： Raman K. Bakshi , Soumya P. Sahoo , Richard L. Tolman
IPC分类号： A61K31/435 , A61K31/44 , A61P5/28 , C07D221/02 , C07D221/18
CPC分类号： C07J73/005 , A61K31/435
摘要： Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.
摘要翻译：结构式（I）的化合物及其药理学上可接受的盐和酯具有5α-还原酶抑制活性。这些化合物抑制1型和2型5α-还原酶。结构式I的化合物可用于全身，包括口服和肠胃外，包括局部治疗和预防高雄激素症状，包括前列腺癌，良性前列腺增生症，寻常痤疮，皮脂溢，雄激素性脱发（也称雄激素性脱发），包括男性和女性型秃发，女性多毛症和前列腺炎。一类本发明的化合物也是有效的抗雄激素。本发明还涉及含有这些化合物的新型组合物，其用途及其制备方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式