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1. 发明授权

US4223143A Quinazoline derivatives 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US4223143A
公开(公告)日：1980-09-16
申请号：US968577
申请日：1978-12-11
申请人： Eckehard K. T. Cuny , Frieder W. Lichtenthaler
发明人： Eckehard K. T. Cuny , Frieder W. Lichtenthaler
IPC分类号： C07D231/56 , C07D239/88 , C07D487/04
CPC分类号： C07D487/04 , C07D231/56 , C07D239/88
摘要： Novel quinazoline derivatives of the formula (1) ##STR1## wherein ring C is a pyrazole ring fused to ring B in two vicinal positions thereof that are not fused with ring A. The novel formula (1) compounds or pyrazolo-quinazoline-ones are structurally related to allopurinol, a well known drug useful in the treatment of gout and are expected to replace or complement allopurinol in the therapeutic use thereof. The generic name Benzoallopurinol is suggested for the novel formula (1) compounds; formula (1) includes angular and linear structures of the interfused rings A, B and C.Two methods for producing the novel formula (1) compounds are disclosed. The first method starts from the indazole structure that includes the interfused rings B and C, and ring A is formed on the indazole moiety. The second method starts from the quinazoline structure that includes interfused rings A and B, and the pyrazole ring C is formed on the benzo moiety (ring B) of the quinazoline structure. Either method may lead to angular or linear benzoallopurinols depending upon the substituents introduced into the starting structure for forming the complemental ring thereon.
摘要翻译：新的式（1）化合物或吡唑并喹唑啉衍生物（1）其中环C是与环B的两个相邻位置稠合的环B的吡唑环。 - 酮在结构上与别嘌呤醇有关，别嘌呤醇是用于治疗痛风的众所周知的药物，并且预期在其治疗用途中替代或补充别嘌呤醇。对于新型配方（1）化合物，建议通用名称苯并嘌呤; 公式（1）包括界面环A，B和C的角度和线性结构。公开了制备新式（1）化合物的两种方法。第一种方法是从包含界面环B和C的吲唑结构开始，在吲唑部分上形成环A。第二种方法从包括嵌段环A和B的喹唑啉结构开始，吡唑环C形成在喹唑啉结构的苯并部分（环B）上。根据引入到起始结构中的取代基来形成其上的互补环，任一方法都可能导致角或线性的苯并嘌呤醇。

2. 发明授权

US4352931A Lin-benzoaminopurinols 失效
标题翻译：林 - 苯胺氨基嘌呤
公开(公告)号：US4352931A
公开(公告)日：1982-10-05
申请号：US152527
申请日：1980-05-22
申请人： Eckehard K. T. Cuny , Frieder W. Lichtenthaler , Alfred R. Moser
发明人： Eckehard K. T. Cuny , Frieder W. Lichtenthaler , Alfred R. Moser
IPC分类号： A61K31/505 , A61P19/06 , C07D231/56 , C07D487/04
CPC分类号： C07D487/04 , C07D231/56
摘要： Novel benzologs or pyrazolo-quinazoline derivatives of the formula (I) ##STR1## wherein X and Y are independently selected from oxygen, sulphur and imino and wherein ring (C) is a pyrazole ring fused to ring (B) via one of the three ortho positions or sides of ring (B); the fused pyrazole ring (C) is either in the 4,3- or the 3,4-arrangement; and tautomers of formula (I) compounds; when X is not oxygen, i.e. stands for sulphur or imino, Y may stand for a covalent bond that links the hydrogen directly to the carbon atom in position 2.Two methods for producing the novel formula (I) compounds are disclosed. The first or indazole method starts from a precursor having a benzene moiety (ring B) and a pyrazolo moiety (ring C) fused therewith, i.e. the indazole structure; ring (B) carries two vicinal substituents for forming the pyrimidine moiety or ring (A) by cyclization. The second or quinazoline method starts from a precursor having the pyrimidine moiety (A) and the benzene moiety (B) fused therewith, i.e. the quinazoline structure, and carrying two vicinal substituents for forming the pyrazole moiety (C) by cyclization.The first method, in addition to yielding the novel benzologs, provides for improved synthesis of previously disclosed benzo-allopurinols.Novel compounds of formula (I) are benzologs of such well known and biologically active compounds as oxipurinol, aminopurinol and thiopurinol and are expected to be applicable for comparable pharmaceutical purposes.
摘要翻译：式（I）的新型苯并或吡唑并喹唑啉衍生物其中X和Y独立地选自氧，硫和亚氨基，其中环（C）是通过一个与环（B）稠合的吡唑环的环（B）的三个邻位或侧面; 稠合吡唑环（C）为4,3-或3,4配位; 和式（I）化合物的互变异构体; 当X不是氧时，即代表硫或亚氨基，Y可以表示将氢直接连接到位置2的碳原子的共价键。公开了制备新式（I）化合物的两种方法。第一或吲唑方法从具有苯部分（环B）和与其稠合的吡唑基部分（环C）的前体即吲唑结构开始; 环（B）携带两个邻位取代基，用于通过环化形成嘧啶部分或环（A）。第二种或喹唑啉方法从具有嘧啶部分（A）和与其结合的苯部分（B）的前体即喹唑啉结构开始，并通过环化携带用于形成吡唑部分（C）的两个连位取代基。第一种方法除了产生新颖的苯甲酸之外，还提供了先前公开的苯并 - 别嘌呤醇的改进的合成。式（I）的新型化合物是诸如葫芦脲，氨基嘌呤醇和硫嘌呤醇的众所周知和生物活性化合物的苯并are，并且预期适用于可比较的药物目的。

3. 发明授权

US5218098A 5-(.alpha.-D-glucopyranosyloxymethyl)-furan-2-carboxaldehyde 失效
标题翻译： 5 - （（ALPHA）-D-GLUCOPYRANOSYLOXYMETHYL） - FURAN-2-CARBOXALDEHYDE
公开(公告)号：US5218098A
公开(公告)日：1993-06-08
申请号：US606278
申请日：1990-10-31
申请人： Frieder W. Lichtenthaler , Dierk Martin , Thomas Weber , Hubert Schiweck
发明人： Frieder W. Lichtenthaler , Dierk Martin , Thomas Weber , Hubert Schiweck
IPC分类号： C07H1/06 , B01F17/56 , C07H15/26
CPC分类号： C07H15/26
摘要： 5-(.alpha.-D-glucopyranosyloxymethyl)-furan-2-carboxaldehyde (GMF) is produced from isomaltulose by heating a solution of isomaltulose in a strongly polar aprotic solvent in the presence of an acidic ion-exchanger, either batchwise or by percolation of the solution through a column filled with the ion-exchanger. Novel derivatives of GMF of the formula (I) ##STR1## wherein R' is a hydrogen atom, an acyl group or an alkyl group and X represents --CH.sub.2 OH, --COOH, --C(H).dbd.NOH, --CN, --CH.sub.2 NHR" or --CH.dbd.CR"R'", where R" is a hydrogen atom, an acyl or aryl group or an alkyl group with up to 20 C atoms and R'" is a hydrogen atom, --NO.sub.2, --CN, --COOalkyl or acyl are described, and also their preparation and use for the preparation of surface-active compounds.
摘要翻译： 5-（α-D-吡喃葡萄糖氧基甲基） - 呋喃-2-甲醛（GMF）由异麦芽酮糖通过在酸性离子交换剂存在下加热异麦芽酮糖溶液在强极性非质子溶剂中分批或渗滤溶液通过填充有离子交换剂的柱。式（I）的GMF的新型衍生物其中R'为氢原子，酰基或烷基，X为-CH 2 OH，-COOH，-C（H）= NOH，-CN ，-CH 2 NHR“或-CH = CR''R”'，其中R“是氢原子，酰基或芳基或具有至多20个C原子的烷基，R”'是氢原子，-NO 2，-CN，-COO烷基或酰基，以及它们用于制备表面活性化合物的制备和用途。

4. 发明授权

US4618675A Derivatives and reduction products of D-glucopyranosyl-alpha(1.fwdarw.5)-d-arabinonic acid; and production of same 失效
标题翻译： D-吡喃葡萄糖基-α（1-> 5）-d-阿拉伯糖酸的衍生物和还原产物; 并生产相同
公开(公告)号：US4618675A
公开(公告)日：1986-10-21
申请号：US562135
申请日：1983-12-16
申请人： Frieder W. Lichtenthaler , Roger G. Klimesch
发明人： Frieder W. Lichtenthaler , Roger G. Klimesch
IPC分类号： A23L27/30 , C07H15/04 , C07H15/26
CPC分类号： C07H15/04 , A23L27/33 , C07H15/26
摘要： The invention relates to derivatives and reduction products of D-glucopyranosyl-alpha(1.fwdarw.5)-d-arabinonic acid, having the general formula: ##STR1## wherein X is one of the following groups: --COOM, --COOR', CONH.sub.2 or --CH.sub.2 OH, where M is an alkali metal and R' is an alkyl group; and where R is a hydrogen atom or an acyl group. The compounds of formula (I) include compounds in which the arabinonic acid chain is closed in a lactone ring.A method for producing the derivatives and reaction products is described, and uses therefor are also provided.
摘要翻译：本发明涉及D-吡喃葡萄糖基-α（1-> 5）-d-阿拉伯糖酸的衍生物和还原产物，具有以下通式：其中X是以下基团之一：-COOM， - COOR'，CONH 2或-CH 2 OH，其中M为碱金属，R'为烷基; 并且其中R是氢原子或酰基。式（I）化合物包括在内酯环中封闭阿拉伯糖酸链的化合物。对衍生物和反应产物的制造方法进行说明，并提供其用途。

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