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1. 发明授权

US06245910B1 Process for producing purine derivatives 失效
标题翻译：嘌呤衍生物的制备方法
公开(公告)号：US06245910B1
公开(公告)日：2001-06-12
申请号：US09427989
申请日：1999-10-27
申请人： Kunisuke Izawa , Hiroshi Shiragami , Keizo Yamashita
发明人： Kunisuke Izawa , Hiroshi Shiragami , Keizo Yamashita
IPC分类号： C07D47330
CPC分类号： C07D473/00
摘要： Purine derivatives in which a desired substituent is introduced into the 9-position only are synthesized by first introducing an easily-removable substituent in the 7-position of a purine base of natural purine nucleosides obtained through fermentation or derivatives thereof, then hydrolyzing the ribose moiety to form purine derivatives having the substituent in the 7-position, subsequently introducing the desired substituent in the 9-position, and then removing the substituent in the 7-position.
摘要翻译：其中将所需的取代基引入9-位的嘌呤衍生物仅通过首先在通过发酵或其衍生物获得的天然嘌呤核苷的嘌呤碱基的7-位上引入容易移除的取代基来合成，然后水解核糖部分以形成在7-位具有取代基的嘌呤衍生物，随后将所需取代基引入9-位，然后除去7-位上的取代基。

2. 发明授权

US06407237B1 Crystal forms of 9-substituted hypoxanthine derivatives 失效
标题翻译： 9-取代的次黄嘌呤衍生物的晶体形式
公开(公告)号：US06407237B1
公开(公告)日：2002-06-18
申请号：US09505984
申请日：2000-02-16
申请人： Alvin J. Glasky , Heinrich Bollinger , Hans Rudolf Müller
发明人： Alvin J. Glasky , Heinrich Bollinger , Hans Rudolf Müller
IPC分类号： C07D47330
CPC分类号： C07D473/30
摘要： The bifunctional compound N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide monopotassium salt occurs in a number of crystal forms which differ in their stability. Of these forms, the most stable is designated Type I, which is a monopotassium salt monohydrate in which the water is held as water of crystallization. Other crystalline forms, designated Type II and Type III, convert to Type I. Methods are disclosed for the synthesis of Type I and for the conversion of Type II or Type III to Type I.
摘要翻译：双官能化合物N-4-羧基苯基-3-（6-氧代氢嘌呤-9-基）丙酰胺单钾盐以稳定性不同的多种晶体形式存在。在这些形式中，最稳定的是指定为I型的单钾盐一水合物，其中水被保持为结晶水。其他指定为II型和III型的结晶形式转化为I型。公开了合成I型和II型或III型转化为I型的方法。

3. 发明授权

US06310070B1 Purine derivatives and medicinal use thereof 失效
标题翻译：嘌呤衍生物及其药用
公开(公告)号：US06310070B1
公开(公告)日：2001-10-30
申请号：US09462861
申请日：2000-04-28
申请人： Akihisa Yokoyama , Sumitsugu Kisanuki , Yoshikazu Matsuda , Junko Matsui , Yoshiaki Isobe
发明人： Akihisa Yokoyama , Sumitsugu Kisanuki , Yoshikazu Matsuda , Junko Matsui , Yoshiaki Isobe
IPC分类号： C07D47330
CPC分类号： C07D473/30
摘要： A novel purine derivative exhibiting an effect to control inflammatory symptoms characteristic to nephritis and a medicine comprising this compound as an effective ingredient are provided. The compound is represented by the following general formula (I), wherein R1 is a hydrocarbon group having 17 or less carbon atoms and R2 is a hydrocarbon group having 16 or less carbon atoms, wherein one or more CH2 g roups in the hydrocarbon group which 7013 do not directly bind with the carbon atom at 2 or 7 position of the purine ring replaced are by carbonyl groups, sulfonyl groups, O, or S and/or one or more CH groups in the hydrocarbon group which do not directly bind with the carbon atom at 2 or 7 position of the purine ring are replaced by N, C-halogen, or C—C≡N, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了具有控制肾炎特征性炎症症状的效果的新型嘌呤衍生物和含有该化合物作为有效成分的药物。该化合物由以下通式（I）表示，其中R 1是具有17个或更少碳原子的烃基，R 2是具有16个或更少碳原子的烃基，其中一个或多个在烃基中的CH 2 7013不与嘌呤环的2或7位的碳原子直接结合，所取代的碳原子是羰基，磺酰基，O或S和/或烃基中一个或多个不与直接键合的CH基团嘌呤环2或7位的碳原子被N，C-卤素或CC = N取代，或其药学上可接受的盐。

4. 发明授权

US06303617B1 Serotonin-like 9-substituted hypoxanthine and methods of use 有权
标题翻译： 5-羟色胺样9-取代次黄嘌呤及其使用方法
公开(公告)号：US06303617B1
公开(公告)日：2001-10-16
申请号：US09304728
申请日：1999-05-04
申请人： Alvin J. Glasky
发明人： Alvin J. Glasky
IPC分类号： C07D47330
CPC分类号： C07D473/00
摘要： Novel 9-substituted hypoxanthine derivatives with unexpected physiological effects are disclosed. These compounds are of formula (I) where n is an integer from 1 to 6, R1 is selected from the group consisting of H, COOH, and COOW1, where W1 is selected from the group consisting of lower alkyl, amino, and lower alkylamino, and R2 is selected from the group consisting of H and OH. Among these compounds are N-(2-(5-hydroxyindol-3-yl)ethyl-3-6-oxyhydropurin-9-yl)propanamide, N-2-(indol-3-yl)ethyl)-3-(6-oxyhydropurin-9-yl)propanamide and N-(1-carboxyl)-(2-(5-hydroxyindol-3-yl)ethyl-3-(6-oxyhydropurin-9-yl)propanamide. These compounds have a number of utilities, including inhibition of the activity of monoamine oxidases, treating obesity, lowering serum cholesterol, and increasing the level of HDL cholesterol. Also disclosed are pharmaceutical compositions and methods of use of the derivatives to treat a number of disorders or conditions.
摘要翻译：公开了具有意想不到的生理效应的新型9-取代的次黄嘌呤衍生物。这些化合物具有式（I），其中n是1至6的整数，R1选自H，COOH和COOW1，其中W1选自低级烷基，氨基和低级烷基氨基并且R 2选自H和OH。在这些化合物中，N-（2-（5-羟基吲哚-3-基）乙基-3,6-壬基嘌呤-9-基）丙酰胺，N-2-（吲哚-3-基）乙基）-3-（6 - 氧基嘌呤-9-基）丙酰胺和N-（1-羧基） - （2-（5-羟基吲哚-3-基）乙基-3-（6-羟基嘌呤-9-基）丙酰胺，这些化合物具有包括抑制单胺氧化酶的活性，治疗肥胖症，降低血清胆固醇，以及提高HDL胆固醇的水平。还公开了使用衍生物治疗多种疾病或病症的药物组合物和方法。

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