摘要:
Methods of treating an inflammatory disorder include administering an effective amount of a compound represented by Structural Formula (I): Ring A is optionally substituted, contains zero, one, two, or three double bonds, and is optionally fused to an aliphatic, aryl or heteroaryl ring; X is an optionally substituted 1 to 3 carbon aliphatic chain that is optionally fused to a monocyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring, wherein one or two carbons in X are optionally replaced with —O—, —S—, or —NRe—; Y is carbon or nitrogen; R1 and R2 are independently —H, —OH, —CN, —NO2, —NRfRg, halogen, optionally substituted alkyl, or optionally substituted alkoxy; or R1 and R2 together link the carbons to which they are bonded with a bond, —O—, —S—, or —NRh—; R3 and R4 are independently —H, —OH, —CN, —NO2, —NRiRj, halogen, optionally substituted alkyl, or optionally substituted alkoxy, or R4 is ═O; or R3 and R4, taken together with the atoms to which they are bonded, form a monocyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring that is optionally fused to a monocyclic or bicyclic, optionally substituted, aliphatic, heterocyclic, aryl, or heteroaryl ring; Re-Rj are independently —H or optionally substituted alkyl; and each of the OSM signaling inhibitor compounds has at least one hydrogen atom bonded to an oxygen, nitrogen, or sulfur atom. The OSM signaling inhibitor compounds also include pharmaceutically acceptable salt or solvates of the compounds represented by Structural Formula (I).
摘要:
The invention features compounds of formulas I or II: and pharmaceutically acceptable salts and prodrugs thereof, as well methods for modulating the effects of local and systemic hypoxic events using the compounds.
摘要:
Methods for treatment of ocular disorders using steroids modulate the effects of local and systemic hypoxic events mediated by hypoxia inducible factor-1 (HIF-1). Steroids that are useful as HIF-1 modulators include bufalin, digitoxigenin, digoxin, lanatoside C, strophantin K, uzarigenin, ouabain and proscillaridin. In some embodiments the ocular disorder is characterized by ischmia.
摘要:
The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach to treat refractory cancers using Na+/K+-ATPase inhibitors, such as cardiac glycosides (e.g. ouabain or proscillaridin, etc.).
摘要翻译:本发明的试剂,药物制剂,试剂盒和方法提供了一种使用Na + / K + + ATPase抑制剂治疗难治性癌症的新方法,例如强心苷( 例如哇巴因或前列腺素等)。
摘要:
The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach for treating pancreatic cancers. The invention provides the use of Na+/K+-ATPase inhibitors, such as cardiac glycosides (e.g. ouabain and proscillaridin, etc.), either alone or in combination with other standard therapeutic agents (chemo- or radio-therapies, etc.) for treating pancreatic cancers.
摘要:
The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach to treat refractory cancers using Na+/K+-ATPase inhibitors, such as cardiac glycosides, including bufadienolides or their corresponding aglycones (e.g., proscillaridin, scillaren, and scillarenin, etc.), especially in oral formulations and/or solid dosage forms containing more than 1 mg of active ingredients.
摘要翻译:本发明的试剂,药物制剂,试剂盒和方法提供了使用Na + / K + + ATPase抑制剂如强心苷治疗难治性癌症的新方法, 包括bufadienolides或其相应的糖苷配基(例如proscillaridin,scillaren和scillarenin等),特别是含有超过1mg活性成分的口服制剂和/或固体剂型。
摘要:
The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach to alleviate or eliminate certain negative effects associated with the use of certain cancer treatment agents (e.g. chemotherapy therapeutics, etc.) or regimens (e.g. radio therapies, etc.), including stimulation of the hypoxic stress response in tumor cells. The reagent and pharmaceutical formulation of the invention relates to Na+/K+-ATPase inhibitors, such as cardiac glycosides, including bufadieneolides or their corresponding aglycones (e.g., proscillaridin, scillaren, and scillarenin, etc.), especially in oral formulations and/or solid dosage forms containing more than 1 mg of active ingredients.
摘要:
The invention provides isolated nucleic acids encoding human lipase proteins and fragments, derivatives, and variants thereof. These nucleic acids and proteins are useful for diagnosis, prevention, and therapy of a number of human and other animal disorders associated, for example, with aberrant lipid metabolism or aberrant pancreatic activity. The invention also provides antisense nucleic acid molecules, expression vectors containing the nucleic acid molecules of the invention, host cells into which the expression vectors have been introduced, and non-human transgenic animals in which a nucleic acid molecule of the invention has been introduced or disrupted. The invention still further provides isolated polypeptides, fusion polypeptides, antigenic peptides, and antibodies. Diagnostic, prognostic, screening, and therapeutic methods involving use of compositions of the invention are also provided. The nucleic acids and polypeptides of the present invention are useful as modulating agents in regulating a variety of cellular processes relating to mono-, di-, and triglyceride metabolism and pancreatic function.
摘要:
The present invention provides methods for identifying compounds that bind to MTBX, a novel cardiovascular system associated transcription factor regulatory polpeptide.
摘要:
The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach to alleviate or eliminate certain negative effects associated with the use of certain cancer treatment agents (e.g. chemotherapy therapeutics, etc.) or regimens (e.g. radio therapies, etc.), including stimulation of the hypoxic stress response in tumor cells.