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    • 2. 发明申请
    • NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
    • 新型半合成糖苷作为抗菌剂
    • US20110015119A1
    • 2011-01-20
    • US12552221
    • 2009-09-01
    • Daniel ChuTao YeBing Wang
    • Daniel ChuTao YeBing Wang
    • A61K38/12C07K7/50A61P31/04
    • C07K9/008A61K38/00A61K45/06
    • Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
    • 具体描述了具有抗菌活性的半合成糖肽,特别是本文所述的半合成糖肽通过化学修饰糖肽(化合物A,化合物B,化合物H或化合物C)或通过水解二糖部分 在酸性介质中母体糖肽的氨基酸-4得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 在这些支架上的氨基酸4氨基取代的糖部分上的氨基取代基被某些酰基酰化; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。 关键反应是用异氰酸酯处理适当保护的中间体化合物。 还提供了合成化合物的方法,含有该化合物的药物组合物,以及该化合物用于治疗和/或预防疾病,特别是细菌感染的方法。
    • 3. 发明申请
    • NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
    • 新型半合成糖苷作为抗菌剂
    • US20100105607A1
    • 2010-04-29
    • US12603435
    • 2009-10-21
    • Daniel ChuTao YeBing Wang
    • Daniel ChuTao YeBing Wang
    • A61K38/08C07K9/00A61P31/04
    • C07K9/006
    • Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of the a glycopeptide (Compound A, Compound B, Compound H or Compound C) or the monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; conversion of the amide group in amino acid-3 on these scaffolds to various acylamide, acylsulfonamide, acylsulfonylurea derivatives; aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid-7 through Mannich reaction; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
    • 具体描述了具有抗菌活性的半合成糖肽,特别是本文所述的半合成糖肽通过化学修饰糖肽(化合物A,化合物B,化合物H或化合物C)或通过水解二糖而制备的单糖 在酸性介质中母体糖肽的氨基酸-4部分得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 在这些支架上的氨基酸4氨基取代的糖部分上的氨基取代基被某些酰基酰化; 这些支架上氨基酸-3中的酰胺基转化为各种酰基酰胺,酰基磺酰胺,酰基磺酰脲衍生物; 通过曼尼希反应在氨基酸-7上氨基甲基化与含有磺酰胺或酰基磺酰胺基团的取代基; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。 还提供了合成化合物的方法,含有该化合物的药物组合物,以及该化合物用于治疗和/或预防疾病,特别是细菌感染的方法。
    • 4. 发明申请
    • NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
    • 新型半合成糖苷作为抗菌剂
    • US20120252741A1
    • 2012-10-04
    • US13440692
    • 2012-04-05
    • Daniel ChuTao YeBing Wang
    • Daniel ChuTao YeBing Wang
    • A61K38/14A61P31/04C07K1/06C07K9/00
    • C07K9/006
    • Provided herein are semi-synthetic glycopeptides having antibacterial activity. The semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety with certain acyl groups; conversion of the amide group in amino acid-3 to various acylamide, acylsulfonamide, acylsulfonylurea derivatives; aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid-7 through Mannich reaction; and conversion of the acid moiety on the macrocyclic ring to certain substituted amides. Also provided herein are pharmaceutical compositions comprising the semi-synthetic glycopeptides, and methods of use of the semi-synthetic glycopeptides for the treatment and/or prophylaxis of diseases, especially bacterial infections.
    • 本文提供具有抗菌活性的半合成糖肽。 本文所述的半合成糖肽通过在酸性介质中水解母体糖肽的氨基酸-4的二糖部分而使糖肽进行化学修饰来制备,得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 用某些酰基酰化氨基酸4氨基取代的糖部分上的氨基取代基; 氨基酸-3中的酰胺基转化为各种酰基酰胺,酰基磺酰胺,酰基磺酰脲衍生物; 通过曼尼希反应在氨基酸-7上氨基甲基化与含有磺酰胺或酰基磺酰胺基团的取代基; 并将大环上的酸部分转化为某些取代的酰胺。 本文还提供了包含半合成糖肽的药物组合物,以及使用半合成糖肽来治疗和/或预防疾病,特别是细菌感染的方法。
    • 6. 发明申请
    • NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
    • 新型半合成糖苷作为抗菌剂
    • US20120129763A1
    • 2012-05-24
    • US13358374
    • 2012-01-25
    • Daniel ChuTao Ye
    • Daniel ChuTao Ye
    • A61K38/14A61P31/04C07K9/00
    • C07K9/008
    • Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate or carrying a Hofmann degradation of the primary amide of the 3rd amino acid asparagines with phenyl-bis-trifluoroacetate to give the primary amine. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
    • 具体描述了具有抗菌活性的半合成糖肽,特别是本文所述的半合成糖肽通过化学修饰糖肽(化合物A,化合物B,化合物H或化合物C)或通过水解二糖部分 在酸性介质中母体糖肽的氨基酸-4得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 在这些支架上的氨基酸4氨基取代的糖部分上的氨基取代基被某些酰基酰化; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。 关键反应是用异氰酸酯处理适当保护的中间体化合物或者用苯基二 - 三氟乙酸盐对第三氨基酸天门冬酰胺的伯酰胺进行霍夫曼降解,得到伯胺。 还提供了合成化合物的方法,含有该化合物的药物组合物,以及该化合物用于治疗和/或预防疾病,特别是细菌感染的方法。
    • 7. 发明申请
    • SEMI-SYNTHETIC GLYCOPEPTIDES HAVING ANTIBACTERIAL ACTIVITY
    • 具有抗菌活性的半合成糖蛋白
    • US20100216699A1
    • 2010-08-26
    • US12697967
    • 2010-02-01
    • Daniel ChuTao Ye
    • Daniel ChuTao Ye
    • A61K38/14C07K9/00C07K7/64A61K38/12A61P31/04
    • C07K9/008A61K38/00C07K7/06
    • Semi-synthetic glycopeptides having antibacterial activity are described. Also described are processes of preparing such semi-synthetic glycopeptides by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or the monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in mild acidic medium to give the amino acid-4 monosaccharide; protection of the amino groups in the molecule; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Also included are the process of conversion of the amide group in amino acid-3 on these scaffolds to various acylureas, acylamide, acylsulfonamide, acylsulfonylurea derivatives and aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid-7 through Mannich reaction procedures. Further provided herein are pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, including bacterial infections.
    • 描述了具有抗菌活性的半合成糖肽。 还描述了通过糖肽(化合物A,化合物B,化合物H或化合物C)的化学修饰或通过水解母体糖肽的氨基酸-4的二糖部分制备的单糖制备这种半合成糖肽的方法 温和酸性培养基,得到氨基酸-4单糖; 保护分子中的氨基; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。 还包括在氨基酸-7上通过曼尼希反应方法将这些支架上的氨基酸3中的酰胺基团转化为各种酰基脲,酰基酰胺,酰基磺酰胺,酰基磺酰脲衍生物和氨基甲基化,其中氨基酸-7的取代基含有磺酰胺或酰基磺酰胺基团。 本文进一步提供含有该化合物的药物组合物,以及该化合物用于治疗和/或预防疾病包括细菌感染的方法。
    • 8. 发明授权
    • Tunable impedance matching networks and tunable diplexer matching systems
    • 可调谐阻抗匹配网络和可调谐双工器匹配系统
    • US07907033B2
    • 2011-03-15
    • US11715835
    • 2007-03-08
    • Arthur S. Morris, IIITao YeScott Griffith
    • Arthur S. Morris, IIITao YeScott Griffith
    • H03H7/38
    • H03H7/38H01G4/38H01G5/18H03H7/463
    • Tunable impedance matching networks and tunable diplexer matching systems are provided. A tunable impedance matching network can include an impedance element connected between first and second nodes for communicating signals between the first and second nodes. For example, the impedance element can be a transmission line or an inductor. Further, the matching network can include a first capacitor connected in parallel with the impedance element, wherein the first capacitor is tunable. The matching network can also include a second capacitor comprising first and second terminals. The first terminal of the second capacitor can be connected to the first node. The second terminal of the second capacitor can be connected to a local voltage reference for the first node. A third capacitor comprises first and second terminals. The first terminal of the second capacitor can be connected to the second node. The second and third capacitors can also be tunable.
    • 提供可调阻抗匹配网络和可调谐双工器匹配系统。 可调阻抗匹配网络可以包括连接在第一和第二节点之间的用于在第一和第二节点之间传送信号的阻抗元件。 例如,阻抗元件可以是传输线或电感器。 此外,匹配网络可以包括与阻抗元件并联连接的第一电容器,其中第一电容器是可调谐的。 匹配网络还可以包括包括第一和第二终端的第二电容器。 第二电容器的第一端可以连接到第一节点。 第二电容器的第二端子可以连接到第一节点的本地电压基准。 第三电容器包括第一和第二端子。 第二电容器的第一端子可以连接到第二节点。 第二和第三电容器也可以是可调谐的。