CREWS, Craig, M.,HOYER, Dentin, Wade,ROTH, Anke, G.,HARLING, John, David,SMITH, Ian Edward, David,MIAH, Afjal, Hussain,CAMPOS, Sebastian, Andre,LE, Joelle,BUCKLEY, Dennis,CIULLI, Alessio,JORGENSEN, Wi
申请号:
USUS2013/021141
公开号:
WO2013/106646A2
申请日:
2013.01.11
申请国别(地区):
WO
年份:
2013
代理人:
摘要:
The present invention relates to novel compounds which find utility as modulators, especially inhibitors of VCB E3 Ubiquitin Ligase and as bioactive agents for use as therapeutics for the stimulation of erythropoiesis in a patient or subject including inducement of EPO production in the patient or subject, for the treatment of chronic anemia and ischemia (limits brain injury during episodes of localized anemia, ischemia and/or stroke and damage to cardiovascular tissue during cardiovascular ischemia), as well as enhancing wound healing processes. Pharmaceutical compositions comprising effective amounts of compounds according to the present invention alone or in combination with an additional erythropoieses stimulating agent such as EPO under the tradename procrit or epogen or darbapoietin alfa under the tradename aranesp. Methods of stimulating erythropoiesis in a subject or patient, including increasing the number of red blood cells and/or hematocrit of the patient, treating anemia, including chronic anemia and anemia associated with chronic kidney disease, dialysis, and cancer chemotherapy, ischemia, stroke and damage to cardiovascular tissue during cardiovascular ischemia as well as enhancing wound healing processes and preventing/reducing scarring secondary to healing represent additional aspects of the present invention. Local enhancement of angiogenesis through induction of VEGF including wound healing and reduction of stent occlusion remain additional aspects of the present invention.La présente invention concerne de nouveaux composés qui trouvent une utilité comme modulateurs, en particulier inhibiteurs de lubiquitine ligase VCB E3 et comme agents bioactifs en vue de lutilisation comme produits thérapeutiques pour la stimulation de lérythropoïèse chez un patient ou un sujet, comprenant linduction de production dEPO chez le patient ou le sujet, pour le traitement danémie et dischémie chroniques (limite une lésion cérébrale pendant des épisodes danémie, ischém