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1. 发明公开

EP1669357A1 SUBSTANCE WHICH EXHIBITS ANTIVIRAL AND ANTIBACTERIAL ACTIVITY AND IS BASED ON DERIVATIVES OF 2,8-DITHIOXO-1H-PYRANO 2,3D&cedi l;6,5-D DIPYRIMIDYNE AND 10-AZA-ANALOGUE THEREOF 审中-公开
标题翻译： SUBSTANZ MIT ANTIVIRALER UND ANTIBAKTERIELLER WIRKUNG AUF DER B
公开(公告)号：EP1669357A1
公开(公告)日：2006-06-14
申请号：EP03810030.1
申请日：2003-11-05
申请人： Tets, Viktor Veniaminovich , Krasnov, Konstantin Andreevich , Ashkinazi, Rimma Iliinichna
发明人： TETS, Viktor Veniaminovich , KRASNOV, Konstantin Andreevich , ASHKINAZI, Rimma Iliinichna
IPC分类号： C07D491/147 , C07D471/14 , A61K31/519 , A61P31/00
CPC分类号： C07D471/14 , C07D491/14
摘要： The inventive substance which exibits antiviral and antibacterial activity is based on derivatives of 2,8-dithioxo-1H-pyrano[2,3-d; 6,5-d']dipyrimidine and 10-aza-analogue, differs in that comprises the derivative of said group of general formula A1 * M:

where: X is selected from a group of O, NH, N-Alkyl;
R1 is selected from the group of H, OH, Cl, O-Alkyl, NH 2 , NH-Alkyl, NH-Ar, N(Alkyl) 2 , SH, S-Alkyl, S-Ar, S-Hetaryl;
R2 is selected from the group of C6H5, Aryl;
R3 is selected from the group of H, Cl, O-Alkyl, NH2, NH-Alkyl, NH-Ar, S-Hetaryl;
M-is absent or is selected from a group: cation Na, K, Li, ammonium or any other pharmacologically acceptable cation or complex of pharmacologically acceptable cation (see above) with anion of one of derivatives of A1 (variants R1-R3 are given above).
摘要翻译：发挥抗病毒和抗菌活性的本发明物质是基于2,8-二硫代-1H-吡喃并[2,3-d 6,5-d']二嘧啶和10-氮杂 - 类似物的不同之处在于包含通式A1 * M的所述基团的衍生物：其中：X选自O，NH，N-烷基; R 1选自H，OH，Cl，O-烷基，NH 2，NH-烷基，NH-Ar，N（烷基）2，SH，S-烷基，S-Ar，S-杂芳基; R2选自C6H5，Aryl; R 3选自H，Cl，O-烷基，NH 2，NH-烷基，NH-Ar，S-杂芳基; M不存在或选自阳离子Na，K，Li，铵或药理学上可接受的阳离子（见上文）与A1衍生物之一的阴离子的任何其他药学上可接受的阳离子或络合物（变体R1-R3）以上）。

2. 发明公开

EP1083172A4 N-SUBSTITUTED DERIVATIVES OF 5-OXYIMINOBARBITURIC ACID 失效
标题翻译： N-SUBSTITUIERTE DERIVATE VON 5-OXYAMINOBARBITURSAÜRE
公开(公告)号：EP1083172A4
公开(公告)日：2001-10-10
申请号：EP98940701
申请日：1998-05-26
申请人： ASHKINAZI RIMMA ILIINICHNA
发明人： ASHKINAZI RIMMA ILIINICHNA
IPC分类号： C07D239/62 , A61K31/515 , A61P1/04 , A61P1/16 , A61P3/08 , A61P7/02 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/18 , A61P31/04 , A61P31/12 , A61P33/00 , A61P37/04 , A61P39/06 , C07D239/60 , C07D239/66 , A61K31/505
CPC分类号： C07D239/66 , C07D239/60
摘要： The present invention pertains to the field of medicine and essentially relates to synthetic biologically active compounds of the heterocyclic series having a wide range of biological activities. This invention more precisely relates to compounds of N-substituted derivatives of 5-oxyiminobarbituric acid of general formula (I) where [X] is an oxygen or sulphur atom, R1 is selected from the group comprising saturated or unsaturated alkanes, cycloalkanes, arylalkanes and aromatic compounds, and (R2) is a hydrogen atom or is selected from the group comprising saturated or unsaturated alkanes, cycloalkanes, arylalkanes and aromatic compounds having a biological activity. The compounds of general formula (I) exhibit an anti-viral activity (concerning the herpes simplex viruses), an immuno-stimulating activity, an anti-chlamydial and anti-tuberculosis activity as well as anti-microbial, anti-aggregating, psycho-stimulating, psycho-depressive, anti-oxidant, analgesic, hypoglycemic, anti-arteriosclerosis, anti-ulcer and hepatic-protection activities.
摘要翻译：本发明涉及医学领域，并且本质上涉及具有广泛生物活性的杂环系列的合成生物活性化合物。本发明更精确地涉及通式（I）的5-氧亚氨基巴比妥酸的N-取代衍生物的化合物，其中[X]为氧或硫原子，R 1选自饱和或不饱和烷烃，环烷烃，芳基烷烃和芳香族化合物，并且（R2）为氢原子或选自饱和或不饱和烷烃，环烷烃，芳基烷烃和具有生物活性的芳族化合物。通式（I）的化合物表现出抗病毒活性（涉及单纯疱疹病毒），免疫刺激活性，抗衣原体和抗结核活性以及抗微生物，抗聚集，心理 - 刺激，心理抑郁，抗氧化，镇痛，降血糖，抗动脉硬化，抗溃疡和肝脏保护活动。

3. 发明公开

EP1136472A1 ARYL- AND HETEROARYLAMIDES OF CARBOALKOXYSULFANILIC ACIDS 审中-公开
标题翻译：芳香族 - 芳香族酰胺类的芳香族 - 和芳香族酰胺类
公开(公告)号：EP1136472A1
公开(公告)日：2001-09-26
申请号：EP98966999.9
申请日：1998-12-04
申请人： Ashkinazi, Rimma Iliinichna , Krutikov, Viktor Iosifovich
发明人： Ashkinazi, Rimma Iliinichna , Krutikov, Viktor Iosifovich
IPC分类号： C07C311/44 , C07D249/08 , C07D251/04 , C07D285/08
CPC分类号： C07D285/08 , C07C311/47 , C07D239/69 , C07D251/52
摘要： The invention relates to medicine, and more specifically to pharmacology, and in particular to synthetic biologically active compounds of heterocyclic series, and it is designated mainly for use in medicine practice.
The objective of the invention is obtaining new chemical substances possessing wide range of biological activities, including antiviral activity (regarding Herpes Simplex virus ), immune stimulating activity (for the expense of inducing production of endogenic interferons in a body), and antichlamydial, hepatoprotective, antiaggregational, and antimicrobial activities. In other words, the objective of the invention is to synthesize new biologically active compounds that outperform known analogs in some characteristics and range of action. The proposed objective is achieved by synthesis of aryl- and heterylamides of carboalkoxysulfanilic acids of the general formula (1)
where: R 1 is taken from the group of aryls or heteryls; R 2 is taken from the group of alkyls.
General method of producing the claimed compounds and results of identification, a list of 42 compounds synthesized and tested, and experimental data on comparative testing their biological properties and toxicity are presented.
1 independ. and 42 depend. items of the formula, 9 tables, 10 ref.
摘要翻译：本发明涉及药物，更具体地涉及药理学，并且尤其涉及杂环系列的合成生物活性化合物，并且其主要指定用于医学实践。本发明的目的是获得具有广泛生物活性的新化学物质，包括抗病毒活性（关于单纯疱疹病毒），免疫刺激活性（以诱导体内内源性干扰素的产生为代价），以及抗发炎，保肝，抗聚集性和抗微生物活性。换句话说，本发明的目的是合成新的生物活性化合物，其在某些特征和作用范围上优于已知的类似物。所提出的目的是通过合成通式（1）的烷氧羰基氨基磺酸的芳基 - 和杂芳酰胺来实现的，其中：R1取自芳基或杂环基; R2取自烷基组。生产要求保护的化合物的一般方法和鉴定结果，合成和测试的42种化合物的列表以及关于比较测试它们的生物学性质和毒性的实验数据。 1个独立。和42取决于。公式的项目，9表，10参考。

4. 发明公开

EP1669357A8 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： WITH抗菌和抗病毒有效物质对2,8-二硫代-1H-吡喃并[2,3-D 6,5-D“] dipyrimidine及其-10-氮杂类似物衍生物的基础
公开(公告)号：EP1669357A8
公开(公告)日：2006-08-23
申请号：EP03810030.1
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 , C07D471/14 , A61K31/519 , A61P31/00
CPC分类号： C07D471/14 , C07D491/14
摘要： The inventive substance which exibits antiviral and antibacterial activity is based on derivatives of 2,8-dithioxo-1H-pyrano[2,3-d; 6,5-d']dipyrimidine and 10-aza-analogue, differs in that comprises the derivative of said group of general formula A1 * M:

where: X is selected from a group of O, NH, N-Alkyl;
R1 is selected from the group of H, OH, Cl, O-Alkyl, NH 2 , NH-Alkyl, NH-Ar, N(Alkyl) 2 , SH, S-Alkyl, S-Ar, S-Hetaryl;
R2 is selected from the group of C6H5, Aryl;
R3 is selected from the group of H, Cl, O-Alkyl, NH2, NH-Alkyl, NH-Ar, S-Hetaryl;
M-is absent or is selected from a group: cation Na, K, Li, ammonium or any other pharmacologically acceptable cation or complex of pharmacologically acceptable cation (see above) with anion of one of derivatives of A1 (variants R1-R3 are given above).

5. 发明公开

EP1083172A1 N-SUBSTITUTED DERIVATIVES OF 5-OXYIMINOBARBITURIC ACID 失效
标题翻译： 5-氧代亚氨基二硫代乙酸的N-取代衍生物
公开(公告)号：EP1083172A1
公开(公告)日：2001-03-14
申请号：EP98940701.0
申请日：1998-05-26
申请人： Ashkinazi, Rimma Iliinichna
发明人： Ashkinazi, Rimma Iliinichna
IPC分类号： C07D239/62 , C07D239/66
CPC分类号： C07D239/66 , C07D239/60
摘要： The invention relates to medicine, and more specifically to pharmacology, and in particular to synthetic biologically active compounds of heterocyclic series, possessing wide spectrum of biological activities.
Objective of the invention is obtaining new chemical substances possessing antiviral activity (respecting to Herpes Simplex virus ), immune-stimulating activity (at the expense of induction of producing endogenic interferons in organism), antichlamydial and antituberculous activities, and also antimicrobial, antiaggregational, psychostimulative, psychodepressive, antioxidant, analgesic, hypoglycemic, antiatherosclerotic, antiulcerous, and hepatoprotective activities.
The proposed objective is achieved by synthesis of the group of new chemical compounds - N-substituted derivatives of 5-oximinobarbituric acid of the general formula
where

X is the atom of oxygen or sulfur;
R1 is taken from the group of saturated or unsaturated alkanes, cycloalkanes, arylalkanes, aromatic compounds;
R2 is the hydrogen atom or taken from the group of saturated or unsaturated alkanes, cycloalkanes, arylalkanes, aromatic compounds.

Examples of synthesis of the intermediate and the claimed substances, data on outputs of the intermediate and target products, data on element analysis of the target products, and results of experiments for determination of their biological properties (antimicrobial effect, maximal tolerance dose, effect of the claimed substances on Herpes virus, immune-stimulating activity, effect of the claimed substances on Chlamydia trachomatis, antiaggregational, antiatherosclerotic, psychostimulative, psychodepressive, analgesic, hypoglycemic, antiulcerous, hepatoprotective, and antioxidant effects) are presented. Biological activities of other types were also discovered.
摘要翻译：本发明涉及药物，更具体地涉及药理学，并且尤其涉及具有广谱生物活性的杂环系列的合成生物活性化合物。本发明的目的是获得具有抗病毒活性（关于单纯疱疹病毒），免疫刺激活性（以诱导在生物体中产生内源干扰素为代价），抗发炎和抗结核活性以及抗微生物，抗聚集性，心理刺激性，精神抑制，抗氧化，镇痛，降血糖，抗动脉粥样硬化，抗溃疡和保肝活性。所提出的目的是通过合成一组新的化合物 - 通式为5-氧亚氨基巴比妥酸的N-取代衍生物，其中X是氧或硫的原子; R1取自饱和或不饱和烷烃，环烷烃，芳基烷烃，芳族化合物的组; R2是氢原子或取自饱和或不饱和烷烃，环烷烃，芳基烷烃，芳族化合物的组。中间体和要求保护的物质的合成实例，中间产物和目标产物的输出数据，目标产物的元素分析数据，以及测定其生物学性质的实验结果（抗微生物作用，最大耐受剂量，所要求的物质对疱疹病毒，免疫刺激活性，要求保护的物质对沙眼衣原体的影响，抗聚集性，抗动脉粥样硬化，心理刺激，精神抑制，镇痛，降血糖，抗溃疡，保肝和抗氧化作用）。其他类型的生物活动也被发现。

6. 发明公开

EP1022278A4 TETRACYCLICAL DERIVATIVES FROM PYRIMIDINE 失效
标题翻译：嘧啶的TETRA环状衍生物
公开(公告)号：EP1022278A4
公开(公告)日：2000-12-27
申请号：EP97930907
申请日：1997-04-02
申请人： ASHKINAZI RIMMA ILIINICHNA
发明人： ASHKINAZI RIMMA ILIINICHNA , KRASNOV KONSTANTIN ANDREEVICH
IPC分类号： A61K31/542 , A61P31/00 , A61P31/12 , A61P33/00 , A61P37/04 , C07D513/14 , A61K31/54
CPC分类号： C07D513/14
摘要： The present invention relates to medicine, and especially to pharmacology, veterinary medicine, cosmetology and, more concretely, to synthetical biologically active compounds of a heterocyclical series having antimicrobial, antiviral, antichlamydia and immunostimulating effects: derivatives from 5-oxy-5H-(1)benzopyrano-(5,6-b)-4-oxy-4H-(1,2)-pyrimido-1,4,5,6-tetrahydro-1,3-thiazine. It is characterized by the synthesis of the new class of heterocyclical compounds, i.e. derivatives from 5-oxy-5H-(1)benzopyrano-(5,6-b)-4-oxy-4H-(1,2)-pyrimido-1,4,5,6-tetrahydro-1,3-thiazine (1) of general formula (1); (1-X) where R1 is H or halogen; R2 is H or halogen or a nitro group or a hydroxy group or a metoxy group. The above-mentioned objective can be reached with R1=R2=H (I); R1=C1 (II); R1=R2=C2 (III); R1=H and R2=Br (IV); R1=R2=Br (V); R1=H and R2=NO2 (VII); R1=Br and R2=NO2 (VIII); R1=H and R2=OCN3 (IX); R1=H and R2=OH (X). The inventive synthesis of the substances concerned is a two-step processus: 1) synthesis of 5-oxy-5H-(1)benzopyrano-(5,6-b)-4-oxy-4H-(1,2)-pyrimido-1,4,5,6-tetrahydro-1,3-thiazine (XI) from 2-thiobarbituric acid (XII) and 1,3-dihalogenpropane (XIII); 2) the compound concerned (1-X) is obtained from the intermediate substance produced during the first step and the derivative corresponding to salicylaldehyde (XIV).

7. 发明公开

EP1022278A1 TETRACYCLICAL DERIVATIVES FROM PYRIMIDINE 失效
标题翻译：来自嘧啶的四环衍生物
公开(公告)号：EP1022278A1
公开(公告)日：2000-07-26
申请号：EP97930907.7
申请日：1997-04-02
申请人： Ashkinazi, Rimma Iliinichna
发明人： ASHKINAZI, Rimma Iliinichna , KRASNOV, Konstantin Andreevich
IPC分类号： C07D513/14 , A61K31/54
CPC分类号： C07D513/14
摘要： Biologically active substance on the basis of tetracyclic nitrogen heterocycles of pyrimidine series (applicant - inventors R.I. Ashkinazi and K.A. Krasnov). The present invention relates to medicine, and more specifically to pharmacology, veterinary cosmetology, and in particular to synthetic biologically active compounds of a heterocycle series, which possess antimicrobial, antiviral, antichlamydia and immune stimulating activities: derivatives of 5-oxo-5H-[1]-benzopyrano-[5,6-b]-4-oxo-4H-[1,2]-pyrimido-1,4,5,64-tetrahydro-1,3-thiazine. The compounds are provided mainly for treating tuberculosis, mycobacteriosis, viral diseases, infections caused by chlamydias, and diseases which are accompanied by immunodeficiency, particularly malignant neoplasm. In addition, the above mentioned compounds can be used for the same purposes in veterinary medicine and cosmetology.
An objective of the invention is to obtain new chemical compounds which have high antimicrobial activity, particularly with respect to strains of mycobacteria that are resistant to isoniazid, which is standardly used to treat mycobacteria. Compounds of the invention simultaneously possess antiviral activity (relative to herpes simplex viruses), antichlamydial activity, and also stimulate production of endogenic interferons in organisms. In other words, the objective of the invention is a chemical synthesis of biologically active substances which are superior to the prototype not only in a range of action on strains of tuberculosis and other mycobacteria, but also possess antiviral, antichylamidial and immuno stimulating action.
The objective is solved by synthesis of new class of heterocyclic compounds-derivatives of 5-oxo-5H-[1]-benzopyrano[5,6-b]-4-oxo-4H-[1,2]-pyrimido-1,4,5,6-tetrahydro-1,3-thiazine (1) of general formula (1).
(I-X),where: R 1 = H or a halogen; R 2 = H, halogen, nitro, hydroxy, or methoxy.
The objective can be solved with R 1 = R 2 = H (I); R 1 = H and R 2 = Cl (II); R 1 = R 2 = Cl (III); R 1 = H and R 2 = Br (IV); R 1 = R 2 = Br (V); R 1 = H and R 2 = NO 2 (VI); R 1 = Cl and R 2 = NO 2 (VIIl); R 1 = Cl and R 2 = NO 2 (VII); R 1 = Br and R 2 = NO 2 (VIII); R 1 = H and R 2 = OCH 3 (IX); R 1 = H and R 2 = OH (X).
The proposed synthesis of the claimed compounds includes two main stages:

1. 4-oxo-4H-6-oxy-[1,2-d]-pyrimido-1, 4, 5, 6-tetrahydro-1,3-thiazine(XI) is synthesized from 2-thiobarbituric acid (XII) and 1,3-dihalogenopropane(XIII); and
2. A target compound (I-X) is produced from the intermediate substance (XI) obtained in the first stage and corresponding derivative of salicylaldehyde (XIV). The method is common for all members of the group.

The subject matter of the present invention it explained by two examples of synthesis of the intermediate substance and three examples of synthesis of claimed substances, two tables of yield of intermediate and target products, two tables of characteristics of target products, and data of seven experiments for determination of their biological properties.
摘要翻译：基于嘧啶系列的四环氮杂环的生物活性物质（申请人 - 发明人R.I.Ashkinazi和K.A.Krasnov）。本发明涉及药物，并且更具体地涉及药理学，兽医美容学，并且具体地涉及具有抗微生物，抗病毒，抗虫和免疫刺激活性的杂环系列的合成生物活性化合物：5-氧代-5H- [ 1] -benzopyrano- [5,6-b] -4-氧代-4H- [1,2]嘧啶并-1,4,5,64四氢-1,3-噻嗪。该化合物主要用于治疗肺结核，分枝杆菌病，病毒性疾病，由衣原体引起的感染和伴有免疫缺陷的疾病，特别是恶性肿瘤。另外，上述化合物可用于兽医学和美容学中的相同目的。本发明的一个目的是获得具有高抗微生物活性的新型化合物，特别是对于抗异烟肼的分支杆菌菌株，其通常用于治疗分枝杆菌。本发明的化合物同时具有抗病毒活性（相对于单纯疱疹病毒），抗黑色素活性，并且还刺激生物体中内源性干扰素的产生。换句话说，本发明的目的是生物活性物质的化学合成，不仅在对结核菌和其他分枝杆菌菌株有作用的范围内，而且还具有抗病毒，抗蚁酰胺和免疫刺激作用，其优于原型。通过合成新的一类5-氧代-5H- [1] - 苯并吡喃并[5，6-b] -4-氧代-4H- [1,2] - 嘧啶-1,3,5-三嗪的杂环化合物衍生物，（1）的4,5,6-四氢-1,3-噻嗪（1）。（I-X），其中：R1 = H或卤素; R2 = H，卤素，硝基，羟基或甲氧基。目标可以通过R1 = R2 = H（I）来解决; R1 = H且R2 = Cl（II）; R1 = R2 = Cl（III）; R1 = H且R2 = Br（IV）; R1 = R2 = Br（V）; R1 = H和R2 = NO2（VI）; R1 = Cl和R2 = NO2（VIIl）; R1 = Cl和R2 = NO2（VII）; R1 = Br和R2 = NO2（VIII）; R1 = H和R2 = OCH3（IX）; R1 = H和R2 = OH（X）。所提出的要求保护的化合物的合成包括两个主要阶段：1,4-氧代-4H-6-氧 - [1,2-d] - 嘧啶-1,4,5,6-四氢-1,3-噻嗪（ XI）由2-硫代巴比妥酸（XII）和1,3-二卤代丙烷（XIII）合成; 和2.由第一阶段获得的中间体（XI）和水杨醛（XIV）的相应衍生物制备目标化合物（I-X）。该方法对于该组的所有成员都是常见的。本发明的主题通过合成中间物质的两个例子和合成所要求物质的三个例子，中间产物和目标产物的两个产量表，目标产物的两个特征表以及七个实验的数据来解释用于确定其生物学特性。

8. 发明公开

EP3115394A1 ANTIVIRAL AGENT 有权转让
标题翻译： VIRUZID
公开(公告)号：EP3115394A1
公开(公告)日：2017-01-11
申请号：EP14884461.6
申请日：2014-12-10
申请人： Ashkinazi, Rimma Iliinichna
发明人： Ashkinazi, Rimma Iliinichna
IPC分类号： C08G73/02 , C07C279/02 , A61K31/155 , A61P31/12
CPC分类号： A01N47/44 , A61K31/785 , C07C281/16 , C08G73/02 , C08G2310/00
摘要： The invention relates to antiviral agents and specifically to synthetic biologically-active derivatives, and can be used in the pharmaceutical industry, in medicine, in plant husbandry and in biotechnology. The antiviral agent is based on poly-N1-hydrazino(imino)methyl-1,6-hexanediamine-poly-N1-amino(imino)methyl-1,6-hexane diamine of general formula (1),

where: HX is an acid, n=3-20, and m=4-20, and which is active against viruses of humans, animals, plants, bacteria and fungi, said viruses being non-enveloped and envelopedand containing RNA or DNA. The antiviral agent exhibits a broad range of effectiveness, and is active against viruses both in intracellular and extracellular locations.
摘要翻译：本发明涉及抗病毒剂，特别涉及合成的生物活性衍生物，可用于制药工业，医药，植物饲料和生物技术领域。抗病毒剂是基于通式（1）的聚-N 1 - 肼基（亚氨基）甲基-1,6-己二胺 - 多 - N1-氨基（亚氨基）甲基-1,6-己二胺，其中：HX是酸，n = 3-20，m = 4-20，并且其对人，动物，植物，细菌和真菌的病毒具有活性，所述病毒是非包膜的并且包含并含有RNA或DNA。抗病毒剂具有广泛的有效性，并且在细胞内和细胞外位置对病毒具有活性。

9. 发明公开

EP1156040A1 2,4-DIOXO-5-ARYLIDENIMINO-1,3-PYRIMIDINES 审中-公开
标题翻译： 2,4-二氧代-5- ARYLIDENIMINO -1,3-嘧啶类
公开(公告)号：EP1156040A1
公开(公告)日：2001-11-21
申请号：EP98966989.0
申请日：1998-12-04
申请人： Ashkinazi, Rimma Iliinichna
发明人： ASHKINAZI, Rimma Illiinichna , KRUTIKOV, Viktor Iosifovich
IPC分类号： C07D239/545 , A61K31/505 , A61P25/24 , A61P29/00 , A61P31/00 , A61P31/12 , A61P37/00
CPC分类号： C07D239/545 , C07D405/12
摘要： The invention relates to medicine, and more specifically to pharmacology, and in particular to synthetic biologically active derivatives of pyrimidine, and it is designated mainly for use as antiviral, immune-stimulating, antichlamydial, antituberculous, psychodepressant, analgesic, and hepatoprotective remedies. Besides that, these compounds may be used for treating malignant neoplasms, and also in veterinary.
The objective of the invention is obtaining new chemical substances possessing pronounced biological activity of wide range.
The proposed objective is achieved by synthesis of 2,4-dioxo-5-arylidenimino-1,3-pyrimidines of the general formula
where R is chosen out of group H, OH, alkoxyl, dialkylamino, benzo, dibenzo, or 3,4-dioxolano
General method of producing the claimed compounds and example of synthesis, a list of 25 compounds synthesized and tested, results of identification, and data on wide comparative testing their biological properties and toxicity are presented.
1 independ. and 25 depend. items of the formula, 10 tables, 10 ref.
摘要翻译：本发明涉及药物，并且更具体地涉及药理学，并且更具体地涉及嘧啶的合成生物活性衍生物，并且它主要被指定用作抗病毒，免疫刺激，抗发炎，抗结核，精神抑制，镇痛和保肝治疗。除此之外，这些化合物可用于治疗恶性肿瘤，也可用于兽医。本发明的目的是获得具有广泛范围的显着生物活性的新化学物质。所提出的目的是通过合成具有以下通式的2,4-二氧代-5-芳基亚氨基-1,3-嘧啶来实现的：其中R选自H，OH，烷氧基，二烷基氨基，苯并，二苯并或3,4 - 二氧杂环戊烷制备要求保护的化合物和合成实施例的一般方法，合成并测试的25种化合物的列表，鉴定结果和广泛对比测试的数据，其生物学性质和毒性。 1个独立。和25取决于。公式的项目，10表，10参考。

10. 发明公开

EP3115394A4 ANTIVIRAL AGENT 有权转让
标题翻译： VIRUZID
公开(公告)号：EP3115394A4
公开(公告)日：2017-08-30
申请号：EP14884461
申请日：2014-12-10
申请人： ASHKINAZI RIMMA ILIINICHNA
发明人： ASHKINAZI RIMMA ILIINICHNA
IPC分类号： C08G73/02 , A61K31/155 , A61P31/12 , C07C279/02
CPC分类号： A01N47/44 , A61K31/785 , C07C281/16 , C08G73/02 , C08G2310/00
摘要： The invention relates to antiviral agents and specifically to synthetic biologically-active derivatives, and can be used in the pharmaceutical industry, in medicine, in plant husbandry and in biotechnology. The antiviral agent is based on poly-N1-hydrazino(imino)methyl-1,6-hexanediamine-poly-N1-amino(imino)methyl-1,6-hexane diamine of general formula (1), where: HX is an acid, n=3-20, and m=4-20, and which is active against viruses of humans, animals, plants, bacteria and fungi, said viruses being non-enveloped and envelopedand containing RNA or DNA. The antiviral agent exhibits a broad range of effectiveness, and is active against viruses both in intracellular and extracellular locations.
摘要翻译：本发明涉及抗病毒剂，特别涉及合成的生物活性衍生物，并且可用于制药工业，医药，植物生产和生物技术。抗病毒剂基于通式（1）的聚-N 1 - 肼基（亚氨基）甲基-1,6-己二胺 - 聚-N 1 - 氨基（亚氨基）甲基-1,6-己二胺，其中：HX是酸，n = 3-20，和m = 4-20，并且对人，动物，植物，细菌和真菌的病毒具有活性，所述病毒是无包膜的并且包封并含有RNA或DNA。抗病毒剂具有广泛的有效性，并且对细胞内和细胞外位置的病毒均有活性。

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