摘要:
A class of 2′-fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein Base is a purine or pyrimidine base; R1 is OH, H, OR3, N3, CN, halogen, including F, or CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy, and base refers to a purine or pyrimidine base; R2 is H, phosphate, including monophosphate, diphosphate, triphosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of providing a compound wherein R2 is H or phosphate; sulfonate ester including alkyl or arylalkyl sulfonyl including methanesulfonyl, benzyl, wherein the phenyl group is optionally substituted with one or more substituents as described in the definition of aryl given above, a lipid, an amino acid, peptide, or cholesterol; and R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of being cleaved to the parent compound, or a pharmaceutically acceptable salt thereof.
摘要翻译:公开了一类可用于治疗乙型肝炎感染,丙型肝炎感染,HIV和异常细胞增殖(包括肿瘤和癌症)的2'-氟 - 核苷化合物。 所述化合物具有以下通式:其中碱是嘌呤或嘧啶碱; R 1是OH,H,OR 3,N 3,CN,卤素,包括F或CF 3 N ,低级烷基,氨基,低级烷基氨基,二(低级)烷基氨基或烷氧基,碱是指嘌呤或嘧啶碱基; R 2是H,磷酸盐,包括单磷酸盐,二磷酸盐,三磷酸盐或稳定化的磷酸盐前药; 酰基或其它药学上可接受的离去基团,其当在体内施用时能够提供其中R 2是H或磷酸酯的化合物; 磺酸酯,包括烷基或芳基烷基磺酰基,包括甲磺酰基,苄基,其中苯基任选被一个或多个取代基取代,如上述芳基定义中所述,脂质,氨基酸,肽或胆固醇; 并且R 3是酰基,烷基,磷酸酯或其它药学上可接受的离去基团,当其在体内施用时,其能够被切割成母体化合物或其药学上可接受的盐。
摘要:
A class of 2′-fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein Base is a purine or pyrimidine base; R1 is OH, H, OR3, N3, CN, halogen, including F, or CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy, and base refers to a purine or pyrimidine base; R2 is H, phosphate, including monophosphate, diphosphate, triphosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of providing a compound wherein R2 is H or phosphate; sulfonate ester including alkyl or arylalkyl sulfonyl including methanesulfonyl, benzyl, wherein the phenyl group is optionally substituted with one or more substituents as described in the definition of aryl given above, a lipid, an amino acid, peptide, or cholesterol; and R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of being cleaved to the parent compound, or a pharmaceutically acceptable salt thereof.
摘要翻译:公开了一类可用于治疗乙型肝炎感染,丙型肝炎感染,HIV和异常细胞增殖(包括肿瘤和癌症)的2'-氟 - 核苷化合物。 所述化合物具有以下通式:其中碱是嘌呤或嘧啶碱; R 1是OH,H,OR 3,N 3,CN,卤素,包括F或CF 3 N ,低级烷基,氨基,低级烷基氨基,二(低级)烷基氨基或烷氧基,碱是指嘌呤或嘧啶碱基; R 2是H,磷酸盐,包括单磷酸盐,二磷酸盐,三磷酸盐或稳定化的磷酸盐前药; 酰基或其它药学上可接受的离去基团,其当在体内施用时能够提供其中R 2是H或磷酸酯的化合物; 磺酸酯,包括烷基或芳基烷基磺酰基,包括甲磺酰基,苄基,其中苯基任选被一个或多个取代基取代,如上述芳基定义中所述,脂质,氨基酸,肽或胆固醇; 并且R 3是酰基,烷基,磷酸酯或其它药学上可接受的离去基团,当其在体内施用时,其能够被切割成母体化合物或其药学上可接受的盐。
摘要:
The present invention includes compounds and compositions of β-halonucleosides, as well as methods to treat HIV, HBV or abnormal cellular proliferation comprising administering said compounds or compositions.
摘要:
Disclosed herein is a battery pack having a plurality of battery cells or unit modules (‘unit cells’) electrically connected to each other, wherein the unit cells are arranged in a width direction (traverse direction) of the battery pack in an upright fashion in a state in which the unit cells are spaced apart from each other to form coolant flow channels, thereby constituting a battery module layer, and two or more battery module layers are mounted in a pack case such that the battery module layers are stacked in a height direction (vertical direction) of the battery pack, and wherein the battery pack includes a coolant introduction part, through which a coolant is introduced into the two or more battery module layers to simultaneously cool some or all of the unit cells in the two or more battery module layers, and a coolant discharge part, through which the coolant, having passed the unit cells, is discharged.
摘要:
Disclosed are indole derivatives, a preparation method thereof, and a composition for the prevention and treatment of metabolic diseases, containing the same as an active ingredient. The indole derivatives have inhibitory activity against DGAT (diacylglycerol acyltransferase), which causes metabolic diseases such as obesity and diabetes in the process of lipid metabolism. With the ability to effectively control lipid metabolism and energy metabolism, the composition is thus useful in the prevention and treatment of metabolic diseases, such as obesity and diabetes.
摘要:
Disclosed are indole derivatives a preparation method thereof, and a composition for the prevention and treatment of metabolic diseases, containing the same as an active ingredient. The indole derivatives have inhibitory activity against DGAT (diacylglycerol acyltransferase), which causes metabolic diseases such as obesity and diabetes in the process of lipid metabolism. With the ability to effectively control lipid metabolism and energy metabolism, the composition is thus useful in the prevention and treatment of metabolic diseases, such as obesity and diabetes.
摘要:
A communication system comprising one or more ubiquitous sensor(s) for generating awareness data relating to a user, a context engine for receiving and processing the awareness data to determine the user's current context for the purpose of event handling, a policy engine for receiving and relating at least one pertinent evidential indicator of an incoming event from a caller to the user's current context and in response selecting a preferred event handling feature, and a delivery agent for executing the preferred event handling feature.
摘要:
A method to reduce consumption of static and dynamic energy in a memory system. The method efficiently reduces dynamic and static energy consumed by the memory system by analyzing factors including characteristics of application programs, hardware performance, and the state of memory address buses, which may affect energy consumption, and by controlling a memory device based on the analysis.
摘要:
Disclosed herein is a battery pack having a plurality of battery cells or unit modules (‘unit cells’) electrically connected to each other, wherein the unit cells are arranged in a width direction (traverse direction) of the battery pack in an upright fashion in a state in which the unit cells are spaced apart from each other to form coolant flow channels, thereby constituting a battery module layer, and two or more battery module layers are mounted in a pack case such that the battery module layers are stacked in a height direction (vertical direction) of the battery pack, and wherein the battery pack includes a coolant introduction part, through which a coolant is introduced into the two or more battery module layers to simultaneously cool some or all of the unit cells in the two or more battery module layers, and a coolant discharge part, through which the coolant, having passed the unit cells, is discharged.
摘要:
2′-Fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein Base is a purine or pyrimidine base; R1 is OH, H, OR3, N3, CN, halogen, CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy; R2 is H, phosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving benzyl, a lipid, an amino acid, peptide, or cholesterol; and R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group; or a pharmaceutically acceptable salt thereof.