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1. 发明授权

US06465476B1 Immuno-modulator exhibiting antimicrobial and anti-mycrobacterial activities, method for producing the same and pharmaceutical preparation 失效
标题翻译：表现出抗菌和抗菌活性的免疫调节剂，其制备方法和药物制剂
公开(公告)号：US06465476B1
公开(公告)日：2002-10-15
申请号：US09485779
申请日：2000-02-14
申请人： Nikolai Mikhailovich Goloschapov , Elena Nikolaevna Goloschapova , Tamara Petrovna Filipskikh , Elena Andreevna Michurina , Ljubov Elizarovna Kostjuk , Rakhim Musaevich Khaitov , Galina Ivanovna Tsyvkina , Vladimir Kuzmich Grishin , Nikolai Alexandrovich Stukalov
发明人： Nikolai Mikhailovich Goloschapov , Elena Nikolaevna Goloschapova , Tamara Petrovna Filipskikh , Elena Andreevna Michurina , Ljubov Elizarovna Kostjuk , Rakhim Musaevich Khaitov , Galina Ivanovna Tsyvkina , Vladimir Kuzmich Grishin , Nikolai Alexandrovich Stukalov
IPC分类号： C07D23960
CPC分类号： C07D401/12
摘要： The present invention pertains to the field of medicine and more precisely relates to a novel immuno-modulator of the following formula which exhibits anti-microbial and anti-mycobacterial activities. This modulator is produced by reacting equimolecular amount of 6-methyluracyl-5-sulphochloride and isoniazide in acetonitrile at a high temperature. The preparation is practically not toxic (LD50 in severe conditions exceeding 7000 mg/kg) and can be used according to a given clinical tests for expressing the immuno-modulating and anti-mycobacterial activity. This preparation can be used for correcting various immuno-deficiencies including in HIV-infected patients as well as for treating mycobacterioses such as leprosy, tuberculosis, etc. This preparation can be administrated internally or parenterally. The compound described in the present invention represents the active substance of this pharmaceutical preparation, wherein said preparation can be used against secondary various immuno-deficiencies or mycobacterioses.
摘要翻译：本发明涉及医学领域，更准确地说涉及以下具有抗微生物和抗分枝杆菌活性的新型免疫调节剂。该调节剂是通过使等分子量的6-甲基尿酰基-5-亚磺酰氯和异烟肼在乙腈中在高温下反应制备的。该制剂实际上没有毒性（LD50在严重条件下超过7000mg / kg），并且可以根据用于表达免疫调节和抗分枝杆菌活性的给定临床试验使用。该制剂可用于校正各种免疫缺陷，包括HIV感染患者以及治疗分枝杆菌，如麻风病，结核病等。该制剂可在内部或肠胃外给药。本发明中描述的化合物代表该药物制剂的活性物质，其中所述制剂可用于次级各种免疫缺陷或分枝杆菌。

2. 发明授权

US06686369B1 &agr;-hydrdroxylic acid derivatives, their production and use 失效
标题翻译： α-羟基甲酸衍生物，其生产和使用
公开(公告)号：US06686369B1
公开(公告)日：2004-02-03
申请号：US09155944
申请日：1998-10-08
申请人： Dagmar Klinge , Wilhelm Amberg , Ernst Baumann , Andreas Kling , Hartmut Riechers , Liliane Unger , Manfred Raschack , Stefan Hergenröder , Sabine Schult
发明人： Dagmar Klinge , Wilhelm Amberg , Ernst Baumann , Andreas Kling , Hartmut Riechers , Liliane Unger , Manfred Raschack , Stefan Hergenröder , Sabine Schult
IPC分类号： C07D23960
CPC分类号： C07D217/22 , C07D239/34 , C07D239/48 , C07D239/52 , C07D239/56 , C07D239/60 , C07D239/80 , C07D239/96 , C07D251/20 , C07D251/22 , C07D251/30 , C07D251/38 , C07D251/52 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The present invention relates to carboxylic acid derivatives of the formula where the radicals have the meanings stated in the description, to the preparation of these compounds and to their use as drugs.
摘要翻译：本发明涉及式的羧酸衍生物，其中自由基具有说明书中所述的含义，这些化合物的制备及其作为药物的用途。

3. 发明授权

US06693194B2 Process for the preparation of 4,6-dimethoxy-2-(methylsulfonyl)-1,3-pyrimidine 有权
标题翻译：制备4,6-二甲氧基-2-（甲基磺酰基）-1,3-嘧啶的方法
公开(公告)号：US06693194B2
公开(公告)日：2004-02-17
申请号：US10332248
申请日：2003-01-06
申请人： Beat Jau , Bernhard Urwyler
发明人： Beat Jau , Bernhard Urwyler
IPC分类号： C07D23960
CPC分类号： C07D405/12 , C07D239/60
摘要： Process for preparing 4,6-dimethoxy-2-(methylsulfonyl)-1,3-pyrimidine by reacting 4,6dichloro-2-(methyltio)-1,3-pyrimidine in an inert organic solvent with an alkali metal methoxide, transfer of the resulting 4,6-dimethoxy-2-(methylthio)-1,3-pyrimidine into an aqueous-acidic medium and subsequent oxidation of this compound, of appropriate in the presence of a catalyst, wherein the oxidation is followed by a purification step in which the aqueous-acidic reaction mixture is adjusted with aqueous base to a pH in the range of 5-8 and stirred either in the presence or in the absence of an organic solvent, and the use of this compound for preparing herbicides, for example 7-[(4,6-dimethoxy-pyrimidin-2-yl)thio]-3-methylphthalide.
摘要翻译：通过使四氯-2-（甲基氧基）-1,3-嘧啶在惰性有机溶剂中与碱金属甲醇盐反应制备4,6-二甲氧基-2-（甲基磺酰基）-1,3-嘧啶的方法，将将所得的4,6-二甲氧基-2-（甲硫基）-1,3-嘧啶转化为酸性介质，随后在催化剂存在下氧化该化合物，其中氧化后进行纯化步骤其中将水性 - 酸性反应混合物用碱水溶液调节至pH为5-8，并在有机溶剂存在或不存在下搅拌，并使用该化合物制备除草剂，例如 7 - [（4,6-二甲氧基 - 嘧啶-2-基）硫基] -3-甲基苯酞。

4. 发明授权

US06579982B1 Pyrimidine-2,4,6-trione metalloproteinase inhibitors 失效
标题翻译：嘧啶-2,4,6-三酮金属蛋白酶抑制剂
公开(公告)号：US06579982B1
公开(公告)日：2003-06-17
申请号：US09635156
申请日：2000-08-09
申请人： Julian Blagg
发明人： Julian Blagg
IPC分类号： C07D23960
CPC分类号： C07D239/60
摘要： The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
摘要翻译：本发明涉及X，Y，Ar1，Z，R1，R2和R3的嘧啶-2,4,6-三酮金属蛋白酶抑制剂，如本说明书中所定义，以及治疗炎症，癌症的药物组合物和方法和其他疾病。

5. 发明授权

US06177437B1 Inhibitors of Herpes Simplex virus uracil-DNA glycosylase 失效
标题翻译：单纯疱疹病毒尿嘧啶-DNA糖基化酶抑制剂
公开(公告)号：US06177437B1
公开(公告)日：2001-01-23
申请号：US09388006
申请日：1999-09-01
申请人： George E. Wright
发明人： George E. Wright
IPC分类号： C07D23960
CPC分类号： C07D239/545 , A61K31/513 , A61K31/515 , C07D239/60
摘要： The invention is directed to novel 6-aromatic substituted uracil compounds of formula I therapeutic compositions comprising the compounds, and methods of treating Herpes simplex virus Type I and Type II recurrent infections and Herpes simplex virus Type I and Type II encephalitis in humans using the compounds and/or therapeutic compositions.
摘要翻译：本发明涉及式I化合物的新型6-芳族取代尿嘧啶化合物，其包含该化合物，以及使用该化合物治疗人类单纯疱疹病毒I型和II型复发感染和单纯疱疹病毒I型和II型脑炎的方法，以及 /或治疗组合物。

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