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1. 发明公开

EP1033369A4 5H-PYRANO [2,3-d:6,5-d']DIPYRIMIDINE DERIVATIVES HAVING AN ANTIBACTERIAL, ANTIVIRAL AND IMMUNO-MODULATING ACTIVITY 失效
标题翻译： -5H-吡喃并[2,3-D：6,5-D“] dipyrimidine衍生物具有抗菌，抗病毒和免疫调节效应
公开(公告)号：EP1033369A4
公开(公告)日：2001-07-18
申请号：EP97954962
申请日：1997-11-19
申请人： TETS VIKTOR VENIAMINOVICH
发明人： ASHKINAZI RIMMA ILIINICHNA
IPC分类号： A61K31/519 , A61P31/04 , A61P31/12 , A61P31/22 , A61P35/00 , A61P37/02 , C07D491/14 , C07D491/147 , A61K31/505
CPC分类号： C07D491/14
摘要： The present invention relates to the production of new substances having an antibacterial, antiviral, immuno-modulating and anti-tumoral activity. This invention more precisely relates to the synthesis of 5H-pyrano[2,3-d:6,5-d']dipyrimidine derivatives of general formula (I) where R1 represents a hydroxy group, a mercapto group or halogen, R2 represents a hydroxy group, an alkoxy group or halogen and R3 is hydrogen or aryl. In the preferred embodiments of the above-mentioned substances, the following conditions are observed: when R?1=R2=OH, R3=4-O¿2NC6H4 (I); when R?1=R2=Cl, R3=C¿6H5 (II); when R?1=R2=OH, R3=4-IC¿6H4 (III); when R?1=R2=OH, R3¿=H (IV); when R?1=OH, R2=OCH¿3 and R3=4-O2NC6H4 (V); when R?1=R2=OH, R3¿=4-ClC¿6?H4 (VI); when R?1=R2=OH, R3¿=4-BrC¿6?H4 (VII); when R?1=SH, R2¿=OH and R3=4-ClC¿6?H4 (VIII); and when R?1=SH, R2¿=OH and R3=4-O2NC6H4 (IX).

2. 发明公开

EP1043318A4 SALTS OF 5,5'-ARYLIDENEBISBARBITURIC AND 5,5'-ARYLIDENEBIS(2-THIOBARBITURIC) ACIDS AND 5,5'-ARYLIDENEBIS(2-THIOBARBITURIC) ACIDS HAVING AN ANTIBACTERIAL, ANTI-CHLAMYDIAL, ANTIVIRAL AND IMMUNO-MODULATING ACTIVITY 失效
标题翻译： SALZE DER 5,5'-芳基二硫代巴比妥 - 5,5'-亚氨基二苯胺（2-硫代巴比妥）苏氨酸5,5'-亚氨基二苯基（2-硫代巴比土酸）麻省理工学院抗胆碱，抗胆碱，抗病毒和免疫调节剂丹麦EIGENSCHAFTEN
公开(公告)号：EP1043318A4
公开(公告)日：2001-02-07
申请号：EP97954963
申请日：1997-11-19
申请人： TETS VIKTOR VENIAMINOVICH
发明人： ASHKINAZI RIMMA ILIINICHNA
IPC分类号： C07D239/62 , A61K31/515 , A61P31/12 , A61P31/22 , A61P35/00 , C07D239/60 , C07D239/64 , C07D239/66 , C07D239/68
CPC分类号： C07D239/60 , C07D239/64 , C07D239/68
摘要： The present invention relates to the production of new chemical substances having an anti-microbial, antiviral, immuno-modulating and anti-tumoral activity. This invention more precisely relates to the synthesis of new substances consisting of 5,5'-arylidenebis(2-thiobarbituric) acids and in salts of 5,5'-arylidenebisbarbituric and 5,5'-arylidenebis(2-thiobarbituric) acids of general formula (I) where X is oxygen or sulphur. R1 is hydrogen, a nitro group or an alkoxy group, R2 is hydrogen, a nitro group, an alkoxy group or halogen and Cat+ is a proton or a pyridin- or 2-hydroxyethylammonium-cation. In the preferred embodiments of these substances, the following conditions are observed: X=O, Cat+ is pyridine, R1=H and R2=Cl (I); X=O, Cat+ is pyridine, R1=H and R2=NO2 (II); X=O, Cat+ is H3N+CH2CH2OH, R1=H and R2=NO2 (III); X=S, Cat+ is pyridine, R1=H and R2=Cl (IV); X=S, Cat+ is pyridine, R1=H and R2=OH (V); X=S, Cat+ is pyridine, R1=NO2 and R2=H (VI); X=S, Cat+ is pyridine and R1=R2=MeO (VII); X=O, Cat+ is pyridine, R1=H and R2=Br (VIII); X=O, Cat?+ is H+, R1¿=H and R2=Cl (IX); X=O, Cat?+ is H+, R1¿=H and R2=NO2 (X). This invention also relates to eight synthesis instances of these substances, to three tables representing the chemical and physical characteristics of the substances thus obtained and to the results of five series of experiments. These synthesis instances, tables and results demonstrate the biological properties of these substances on myco-bacteria, on herpes viruses and on Chlamydia trachomatis as well as their interferon-inducing activity and the absence of acute toxicity.
摘要翻译：本发明涉及具有抗微生物，抗病毒，免疫调节和抗肿瘤活性的新化学物质的生产。本发明更精确地涉及由5,5'-亚芳基双（2-硫代巴比妥酸）和5,5'-亚芳基双巴比妥酸和5,5'-亚芳基双（2-硫代巴比妥酸）盐组成的新物质的合成式（I）其中X是氧或硫。 R1是氢，硝基或烷氧基，R2是氢，硝基，烷氧基或卤素，并且Cat +是质子或吡啶或2-羟乙基铵阳离子。在这些物质的优选实施方案中，观察到以下条件：X = O，Cat +为吡啶，R 1 = H且R 2 = Cl（I）; X = O，Cat +为吡啶，R 1 = H和R 2 = NO 2（II）; X = O，Cat +为H3N + CH2CH2OH，R1 = H和R2 = NO2（III）; X = S，Cat +为吡啶，R 1 = H且R 2 = Cl（IV）; X = S，Cat +为吡啶，R 1 = H且R 2 = OH（V）; X = S，Cat +是吡啶，R 1 = NO 2和R 2 = H（VI）; X = S，Cat +是吡啶并且R 1 = R 2 = MeO（VII）; X = O，Cat +为吡啶，R 1 = H且R 2 = Br（VIII）; X = O，Cat 5+为H +，R 1 = H和R 2 = Cl（IX）; X = O，Cat？+是H +，R1？= H，R2 = NO2（X）。本发明还涉及这些物质的八个合成实例，代表由此获得的物质的化学和物理特性的三个表格以及五个系列实验的结果。这些合成实例，表格和结果证明了这些物质在myco-细菌，疱疹病毒和沙眼衣原体上的生物学性质以及它们的干扰素诱导活性和无急性毒性。

3. 发明公开

EP1669357A4 SUBSTANCE WHICH EXHIBITS ANTIVIRAL AND ANTIBACTERIAL ACTIVITY AND IS BASED ON DERIVATIVES OF 2,8-DITHIOXO-1H-PYRANO[ 2,3-D,6,5-D'] DIPYRIMIDINE AND 10-AZA-ANALOGUE THEREOF 审中-公开
标题翻译： SUBSTANZ MIT ANTIVIRALER UND ANTIBKTERIELLER WIRKUNG AUF DER BASIC VON DERIVATEN VON 2,8-DITHIOXO-1H-PYRANO [2,3-D 6,5-D'] DIPYRIMIDIN UND DENEN 10-AZA-ANALOGA
公开(公告)号：EP1669357A4
公开(公告)日：2006-10-25
申请号：EP03810030
申请日：2003-11-05
申请人： TETS VIKTOR VENIAMINOVICH , ASHKINAZI RIMMA ILIINICHNA
发明人： TETS VIKTOR VENIAMINOVICH , KRASNOV KONSTANTIN ANDREEVICH , ASHKINAZI RIMMA ILIINICHNA
IPC分类号： C07D491/147 , A61K31/519 , A61P31/00 , C07D211/00 , C07D239/00 , C07D309/00 , C07D471/14 , C07D491/14
CPC分类号： C07D471/14 , C07D491/14
摘要： The invention relates to organic chemistry and medicine, more specifically to synthetic pyrimidine derivatives, i.e. 2,8-dithioxo-1H-pyrano[2,3d¸6,5-d']dipyrimidyne and 10-aza-analogue thereof and to the complexes and salts thereof which exhibit antiviral and antimicrobial activity. Said invention can be used for medicine and veterinary science for treating viral diseases, bacteria-induced diseases and for cosmetology in the form of an additive for preventing and treating infections. The aim of said invention is to develop a novel more efficient substance exhibiting antiviral and antimicrobial activity. The inventive substance which exhibits antiviral and antimicrobial activity is based on derivatives of 2,8-dithioxo-1H-pyrano[2,3d¸6,5-d']dipyrimidyne and 10-aza-analogue thereof and characterised in that it comprises the derivative of said group of general formula A1 ∗ M: wherein X is selected from a group O, NH, N-Alkyl; R1 is selected from a group H, Oh, Cl, O-Alkyl, NH2, NH-Alkyl; NH-Ar, N(Alkyl)2, SH, S-Alkyl, S-Ar, S-Hetaryl; R2 is selected from a group C6H5, Aryl; R3 is selected from a group H, Cl, O-Alkyl; NH2, NH-Alkyl, NH-Ar, S-Heratyl; M is absent or selected from a group of Na, K, Li, ammonium cation or another pharmacologically acceptable cation; or said complex of pharmacologically acceptable cation with the anion of one of derivatives A1 (above-mentioned variants R1-R3).
摘要翻译：本发明涉及有机化学和医学，更具体地涉及合成的嘧啶衍生物，即2,8-二硫代-1H-吡喃并[2,3-d，6,5-d']二嘧啶及其10-氮杂 - 类似物和该络合物及其显示抗病毒和抗微生物活性的盐。本发明可用于医学和兽医科学，用于治疗病毒性疾病，细菌引起的疾病和用于预防和治疗感染的添加剂形式的美容。所述发明的目的是开发一种新的更有效的显示抗病毒和抗微生物活性的物质。显示抗病毒和抗微生物活性的本发明物质基于2,8-二硫代-1H-吡喃并[2,3-d，6,5-d']二嘧啶及其10-氮杂 - 类似物的衍生物，其特征在于它包含所述通式A1 * M的基团的衍生物：其中X选自O，NH，N-烷基; R1选自H，O，Cl，O-烷基，NH2，NH-烷基; NH-Ar，N（烷基）2，SH，S-烷基，S-Ar，S-Hetary1; R2选自C6H5，芳基; R3选自H，Cl，O-烷基; NH2，NH-烷基，NH-Ar，S-乙酰基; M不存在或选自Na，K，Li，铵阳离子或另一药理学上可接受的阳离子; 或所述药理学上可接受的阳离子与衍生物A1之一的阴离子的复合物（上述变体R1-R3）。

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