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1. 发明授权

US09120774B2 Novobiocin analogues having modified sugar moieties 有权
标题翻译：具有改性糖部分的新生霉素类似物
公开(公告)号：US09120774B2
公开(公告)日：2015-09-01
申请号：US13202382
申请日：2010-02-19
申请人： Brian S. J. Blagg , Huiping Zhao , Alison Catherine Donnelly
发明人： Brian S. J. Blagg , Huiping Zhao , Alison Catherine Donnelly
IPC分类号： C07H17/06 , C07D407/12 , C07D487/14 , C07H19/00
CPC分类号： C07D407/12 , C07D487/14 , C07H19/00
摘要： The disclosure provides novobiocin analogues with noviose replacements which are useful as Hsp90 inhibitors in the treatment of cancer.
摘要翻译：该公开内容提供具有noviose替代物的新生儿素类似物，其可用作治疗癌症中的Hsp90抑制剂。

2. 发明授权

US4894449A Diosmin octakis (hydrogen sulfate) aluminum complex 失效
标题翻译： Diosmin octakis（硫酸氢盐）铝络合物
公开(公告)号：US4894449A
公开(公告)日：1990-01-16
申请号：US225544
申请日：1988-07-28
申请人： Aurelio O. Venero , Ramon M. Pestana
发明人： Aurelio O. Venero , Ramon M. Pestana
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/04 , C07F20060101 , C07F5/06 , C07H20060101 , C07H17/07 , C07H23/00 , C07H11/00 , C07H15/00 , C07H15/24 , C07H17/06
CPC分类号： C07H17/07
摘要： The invention refers to the preparation of diosmin octakis (hydrogen sulfate) aluminum complex, a new derivative of diosmin, by reaction of diosmin with a sulfating agent, such as sulfur trioxide-pyridine complex, sulfur trioxide-trimethylamine complex and sulfur trioxide-triethylamine complex, at a temperature between 40.degree. and 110.degree. C., in an appropriate medium, with preference pyridine, dimethylformamide and dimethylacetamide, and final addition of aluminum hydroxychloride.

3. 发明授权

US4217445A 5-Oxy-substituted derivatives of Psoralene useful in dermatology 失效
标题翻译：补骨脂素的5-氧基取代衍生物可用于皮肤病学
公开(公告)号：US4217445A
公开(公告)日：1980-08-12
申请号：US800782
申请日：1977-05-26
申请人： Eckhard Nikolaiski
发明人： Eckhard Nikolaiski
IPC分类号： A61K31/37 , A61K36/75 , A61P17/00 , C07D493/04 , C07F9/6561 , C07H17/04 , C07H17/06
CPC分类号： C07D493/04 , C07F9/6561 , C07H17/04
摘要： An improved process for obtaining 5-methoxy-psoralene from bergamot oil, a method for preparing the compound 5-hydroxy-psoralene from 5-methoxy-psoralene and a method of making novel psoralene derivatives by replacing the hydrogen atom of the 5-hydroxy group with an R group are disclosed. These compounds are prepared by reacting the 5-hydroxy-psoralene with a halide RX in the presence of sodium hydride. Compounds of particular interest are those of which the radical R is: alkanoyl of not more than 10 carbon atoms; orthoacetoxy-benzoyl; .alpha.thenoyl; O,O diethyl-phosphono; diethylaminoethyl, and 2'3'4'6' tetra .alpha. acetyl D-gluco pyranosyl.
摘要翻译：从佛手柑油获得5-甲氧基 - 补骨脂素的改进方法，从5-甲氧基 - 补骨脂素制备化合物5-羟基 - 补骨脂素的方法和通过替换5-羟基的氢原子制备新的补骨脂素衍生物的方法与R组被披露。这些化合物通过在氢化钠存在下使5-羟基 - 补骨脂素与卤化物RX反应来制备。特别感兴趣的化合物是其自由基R为：不超过10个碳原子的烷酰基; 正乙酰氧基 - 苯甲酰基; α-甲酰基; O，O二乙基膦酰基; 二乙基氨基乙基和2'3'4'6'四α乙酰基D-葡萄糖吡喃糖基。

4. 发明授权

US4148992A Allylic methyl-hydroxylated novobiocins 失效
标题翻译：烯丙基甲基羟基化新生霉素
公开(公告)号：US4148992A
公开(公告)日：1979-04-10
申请号：US878115
申请日：1978-02-15
申请人： Oldrich K. Sebek , Lester A. Dolak
发明人： Oldrich K. Sebek , Lester A. Dolak
IPC分类号： C12P19/60 , C07D311/16 , C07D311/54 , C07H17/075 , A61K31/71 , C07H17/06
CPC分类号： C07D311/54 , C07H17/075 , Y10S435/822 , Y10S435/827
摘要： The present invention relates to a fermentation process for producing allylic methyl-hydroxylated novobiocin and derivatives thereof. These hydroxy novobiocins (II) are useful as antibiotics.
摘要翻译：本发明涉及产生烯丙基甲基羟基化的新生霉素及其衍生物的发酵方法。这些羟基新生霉素（II）可用作抗生素。

5. 发明申请

US20100197619A1 CYCLIN-DEPENDENT PROTEIN KINASES INHIBITORS OF SCUTELLARIA FLAVONOID ORGANIC AMINE DERIVATIVES, SYNTHESIS AND USE THEREOF 有权
标题翻译：环孢菌素依赖性蛋白激酶抑制剂佛兰西兰有机胺衍生物，合成及其用途
公开(公告)号：US20100197619A1
公开(公告)日：2010-08-05
申请号：US12676121
申请日：2009-07-07
申请人： Shixuan Zhang , Yongming Bao , Yuming Sun , Kangjian Li , Liang Zou , Jigang Ma , Xiaodan Sun , Haiyan Shang , Jing Li
发明人： Shixuan Zhang , Yongming Bao , Yuming Sun , Kangjian Li , Liang Zou , Jigang Ma , Xiaodan Sun , Haiyan Shang , Jing Li
IPC分类号： A61K31/7048 , C07H17/06 , A61P35/00 , A61P31/18
CPC分类号： A61K31/496 , A61K31/7048 , A61K36/539 , C07D311/30
摘要： The present invention provides a series of cyclin-dependent protein kinases (Cdks) inhibitors, Scutellaria flavonoid organic amine derivatives, synthesis and use thereof. The preparation method is as follows: taking Baicalein (or Wogonin) from Scutellaria baicalensis as lead compound, mixting it with formaldehyde solution and organic amine compounds based on the molar ratio of 1:1-1.2:1-1.2, adding methanol of duplicate weight than baicalein and reacting at 50-70° C., filtering the sediment and washing and then drying so as to get the product with a content of not less than 97% (weight). Similar to Flavopiridol and P276-00, the activity of baicalein organic amine derivatives inhibiting Cdks has an increase of 50 times compared with that of Baicalin. It can selectively induce apoptosis of the proliferative phase cancer cells, which has scarcely any influence to the normal structure, and it belongs to anticancer drugs of cell cycle inhibitor kind. The product has a rich source of raw materials and has simple process, high purity, low cost, clear metabolic mechanism, high efficiency and low toxicity, which can be made into oral preparations or injections together with acid salts and is expected to become high efficient and low toxicity anti-cancer and AIDS drugs.
摘要翻译：本发明提供了一系列细胞周期蛋白依赖性蛋白激酶（Cdks）抑制剂，黄芩类黄酮有机胺衍生物，其合成和用途。制备方法如下：以黄芩黄芩苷（或Wogonin）为铅化合物，以1：1-1.2：1-1.2的摩尔比与甲醛溶液和有机胺化合物混合，加入重量重量的甲醇比黄芩苷在50-70℃下反应，过滤沉淀物，然后洗涤，然后干燥，得到含量不小于97％（重量）的产品。与黄酮类药物和P276-00类似，抑制镉的黄芩素有机胺衍生物的活性与黄芩苷相比增加了50倍。可选择性诱导增殖期癌细胞凋亡，对正常结构几乎没有任何影响，属于细胞周期抑制剂类抗癌药物。该产品原料丰富，工艺简单，纯度高，成本低，代谢机理清晰，效率高，毒性低，可与酸性盐一起口服制剂或注射，预计效率高和低毒性抗癌和艾滋病药物。

6. 发明申请

US20090187014A1 Novobiocin Analogues 有权
标题翻译：新生霉素类似物
公开(公告)号：US20090187014A1
公开(公告)日：2009-07-23
申请号：US12390011
申请日：2009-02-20
申请人： Brian Blagg
发明人： Brian Blagg
IPC分类号： C07H17/06
CPC分类号： C07D487/14 , C07D405/12 , C07D491/04 , C07D491/14 , C07D493/04 , C07H19/00
摘要： Novobiocin analogues and pharmaceutical composition containing such compounds useful for the treatment and/or prevention of neurodegenerative disorders and autoimmune disorders, as well as cancer.
摘要翻译：含有可用于治疗和/或预防神经变性疾病和自身免疫性疾病以及癌症的化合物的新生霉素类似物和药物组合物。

7. 发明申请

US20050209171A1 Treatment of periodontal disease 有权
标题翻译：治疗牙周病
公开(公告)号：US20050209171A1
公开(公告)日：2005-09-22
申请号：US11004677
申请日：2004-12-03
申请人： Leo Romanczyk , Harold Schmitz
发明人： Leo Romanczyk , Harold Schmitz
IPC分类号： A23G1/32 , A23G3/36 , A23K1/16 , A23K1/18 , A61K9/20 , A61K9/48 , A61K31/353 , A61K31/7048 , A61K36/185 , A61K45/06 , C07D311/32 , C07D311/62 , C07D311/64 , C07H17/06 , C11B5/00
CPC分类号： C07H17/06 , A23G1/32 , A23G3/36 , A23K20/111 , A23K50/40 , A61K9/2018 , A61K9/2068 , A61K9/4858 , A61K31/353 , A61K31/7048 , A61K36/185 , A61K45/06 , C07D311/32 , C07D311/62 , C07D311/64 , C11B5/0035 , A61K2300/00
摘要： Disclosed and claimed are cocoa extracts, compounds, combinations thereof and compositions containing the same, such as polyphenols or procyanidins, methods for preparing such extracts, compounds and compositions, as well as uses for them, especially a polymeric compound of the formula An, wherein A is a monomer of the formula: wherein n is an integer from 2 to 18, such that there is at least one terminal monomeric unit A, and one or a plurality of additional monomeric units; R is 3-(α)-OH, 3-(β)-OH, 3-(α)-O-sugar, or 3-(β)-O-sugar; bonding between adjacent monomers takes place at positions 4, 6 or 8; a bond of an additional monomeric unit in position 4 has alpha or beta stereochemistry; X, Y and Z are selected from the group consisting of monomeric unit A, hydrogen, and a sugar, with the provisos that as to the at least one terminal monomeric unit, bonding of the additional monomeric unit thereto (the bonding of the additional monomeric unit adjacent to the terminal monomeric unit) is at position 4 and optionally Y=Z=hydrogen; the sugar is optionally substituted with a phenolic moiety, at any position on the sugar, for instance via an ester bond, and pharmaceutically acceptable salts or derivatives thereof (including oxidation products).
摘要翻译：公开并要求保护的是可可提取物，化合物，其组合和含有它们的组合物，例如多酚或原花青素，制备此类提取物的方法，化合物和组合物，以及它们的用途，特别是式A的< 其中A是下式的单体：其中n是2至18的整数，使得存在至少一个末端单体单元A和一个或多个另外的单体单元; R是3-（α）-OH，3-（β）-OH，3-（α）-O-糖或3-（β）-O-糖; 相邻单体之间的结合发生在位置4,6或8; 位置4的附加单体单元的键具有α或β立体化学; X，Y和Z选自单体单元A，氢和糖，条件是对于至少一个末端单体单元，附加单体单元与其结合（附加单体单元的键合邻近末端单体单元的单元）在位置4且任选地Y = Z =氢; 糖任选被酚部分取代，在糖上的任何位置，例如通过酯键，及其药学上可接受的盐或衍生物（包括氧化产物）。

8. 发明授权

US06900241B2 Compositions for, and methods of, treating atherosclerosis 有权
标题翻译：治疗动脉粥样硬化的组合物和方法
公开(公告)号：US06900241B2
公开(公告)日：2005-05-31
申请号：US10770969
申请日：2004-05-06
申请人： Leo J. Romanczyk, Jr. , Harold H. Schmitz
发明人： Leo J. Romanczyk, Jr. , Harold H. Schmitz
IPC分类号： A23G1/32 , A23G3/36 , A23K1/16 , A23K1/18 , A61K9/20 , A61K9/48 , A61K31/353 , A61K31/7048 , A61K36/185 , A61K45/06 , C07D311/32 , C07D311/62 , C07D311/64 , C07H17/06 , C11B5/00 , C07D311/78
CPC分类号： C07H17/06 , A23G1/32 , A23G3/36 , A23K20/111 , A23K50/40 , A61K9/2018 , A61K9/2068 , A61K9/4858 , A61K31/353 , A61K31/7048 , A61K36/185 , A61K45/06 , C07D311/32 , C07D311/62 , C07D311/64 , C11B5/0035 , A61K2300/00
摘要： Disclosed and claimed are cocoa extracts, compounds, combinations thereof and compositions containing the same, such as polyphenols or procyanidins, methods for preparing such extracts, compounds and compositions, as well as uses for them, especially a polymeric compound of the formula An, wherein A is a monomer of the formula: wherein n is an integer from 2 to 18, such that there is at least one terminal monomeric unit A, and one or a plurality of additional monomeric units; R, X, Y and Z are as defined in the specification.
摘要翻译：公开并要求保护的是可可提取物，化合物，其组合和含有它们的组合物，例如多酚或原花青素，制备此类提取物的方法，化合物和组合物，以及它们的用途，特别是式A的< 其中A是下式的单体：其中n是2至18的整数，使得存在至少一个末端单体单元A和一个或多个另外的单体单元; R，X，Y和Z如说明书中所定义。

9. 发明授权

US4373095A Macrolide antibacterial AR-5 components 失效
标题翻译：大环内酯抗菌AR-5成分
公开(公告)号：US4373095A
公开(公告)日：1983-02-08
申请号：US244541
申请日：1981-03-17
申请人： Ashit K. Ganguly , Olga Sarre , Yi-Tsung Liu
发明人： Ashit K. Ganguly , Olga Sarre , Yi-Tsung Liu
IPC分类号： C07H17/08 , C12P19/48 , C12P19/62 , C07H17/06
CPC分类号： C07H17/08 , C12P19/48 , C12P19/62 , C12R1/29
摘要： Desmycinosyl derivatives of 12,13-desepoxy-12,13-dehydro antibiotic AR-5 component 1 and 12,13-desepoxy-12,13-dehydro antibiotic AR-5 component 2 are useful antibacterial agents and may be converted to other such agents by processes analogous to those generally known in the art.
摘要翻译： 12,13-去环氧-12,13-脱氢抗菌素AR-5组分1和12,13-去环氧-12,13-脱氢抗生素AR-5组分2的去霉霉素衍生物是有用的抗菌剂，并且可以转化成其它这样的试剂通过与本领域中通常已知的方法类似的方法。

10. 发明授权

US08377895B2 Cyclin-dependent protein kinases inhibitors of Scutellaria flavonoid organic amine derivatives, synthesis and use thereof 有权
标题翻译：黄芩类黄酮有机胺衍生物的细胞周期蛋白依赖性蛋白激酶抑制剂的合成及其应用
公开(公告)号：US08377895B2
公开(公告)日：2013-02-19
申请号：US12676121
申请日：2009-07-07
申请人： Shixuan Zhang , Yongming Bao , Yuming Sun , Kangjian Li , Liang Zou , Jigang Ma , Xiaodan Sun , Haiyan Shang , Jing Li
发明人： Shixuan Zhang , Yongming Bao , Yuming Sun , Kangjian Li , Liang Zou , Jigang Ma , Xiaodan Sun , Haiyan Shang , Jing Li
IPC分类号： A61K31/7048 , C07H17/06 , A61P35/00 , A61P31/18
CPC分类号： A61K31/496 , A61K31/7048 , A61K36/539 , C07D311/30
摘要： The present invention provides a series of cyclin-dependent protein kinases (Cdks) inhibitors, Scutellaria flavonoid organic amine derivatives, synthesis and use thereof. The preparation method is as follows: taking Baicalein (or Wogonin) from Scutellaria baicalensis as lead compound, mixting it with formaldehyde solution and organic amine compounds based on the molar ratio of 1:1-1.2:1-1.2, adding methanol of duplicate weight than baicalein and reacting at 50-70° C., filtering the sediment and washing and then drying so as to get the product with a content of not less than 97% (weight). Similar to Flavopiridol and P276-00, the activity of baicalein organic amine derivatives inhibiting Cdks has an increase of 50 times compared with that of Baicalin. It can selectively induce apoptosis of the proliferative phase cancer cells, which has scarcely any influence to the normal structure, and it belongs to anticancer drugs of cell cycle inhibitor kind. The product has a rich source of raw materials and has simple process, high purity, low cost, clear metabolic mechanism, high efficiency and low toxicity, which can be made into oral preparations or injections together with acid salts and is expected to become high efficient and low toxicity anti-cancer and AIDS drugs.
摘要翻译：本发明提供了一系列细胞周期蛋白依赖性蛋白激酶（Cdks）抑制剂，黄芩类黄酮有机胺衍生物，其合成和用途。制备方法如下：以黄芩黄芩苷（或Wogonin）为铅化合物，以1：1-1.2：1-1.2的摩尔比与甲醛溶液和有机胺化合物混合，加入重量重量的甲醇比黄芩苷在50-70℃下反应，过滤沉淀物，然后洗涤，然后干燥，得到含量不小于97％（重量）的产品。与黄酮类药物和P276-00类似，抑制镉的黄芩素有机胺衍生物的活性与黄芩苷相比增加了50倍。可选择性诱导增殖期癌细胞凋亡，对正常结构几乎没有任何影响，属于细胞周期抑制剂类抗癌药物。该产品原料丰富，工艺简单，纯度高，成本低，代谢机理清晰，效率高，毒性低，可与酸性盐一起口服制剂或注射，预计效率高和低毒性抗癌和艾滋病药物。

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