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1. WO2013106646 - COMPOUNDS AND METHODS FOR THE INHIBITION OF VCB E3 UBIQUITIN LIGASE

Publication Number WO/2013/106646
Publication Date 18.07.2013
International Application No. PCT/US2013/021141
International Filing Date 11.01.2013
IPC
C07D 413/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 417/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
A61K 31/42 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42Oxazoles
A61K 31/427 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425Thiazoles
427not condensed and containing further heterocyclic rings
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 413/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 417/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • YALE UNIVERSITY [US]/[US]
  • GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED [GB]/[GB]
  • CAMBRIDGE ENTERPRISE LIMITED UNIVERSITY OF CAMBRIDGE [GB]/[GB]
Inventors
  • CREWS, Craig, M.
  • BUCKLEY, Dennis
  • CIULLI, Alessio
  • JORGENSEN, William
  • GAREISS, Peter, C.
  • MOLLE, Inge, Van
  • GUSTAFSON, Jeffrey
  • TAE, Hyun-Seop
  • MICHEL, Julien
  • HOYER, Dentin, Wade
  • ROTH, Anke, G.
  • HARLING, John, David
  • SMITH, Ian Edward, David
  • MIAH, Afjal, Hussain
  • CAMPOS, Sebastian, Andre
  • LE, Joelle
Agents
  • COLEMAN, Henry, D.
Priority Data
61/585,73612.01.2012US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) COMPOUNDS AND METHODS FOR THE INHIBITION OF VCB E3 UBIQUITIN LIGASE
(FR) COMPOSÉS ET PROCÉDÉS POUR L'INHIBITION DE L'UBIQUITINE LIGASE VCB E3
Abstract
(EN) 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.
(FR) La présente invention concerne de nouveaux composés qui trouvent une utilité comme modulateurs, en particulier inhibiteurs de l'ubiquitine ligase VCB E3 et comme agents bioactifs en vue de l'utilisation comme produits thérapeutiques pour la stimulation de l'érythropoïèse chez un patient ou un sujet, comprenant l'induction de production d'EPO chez le patient ou le sujet, pour le traitement d'anémie et d'ischémie chroniques (limite une lésion cérébrale pendant des épisodes d'anémie, ischémie et/ou accident vasculaire cérébral localisés et un endommagement au tissu cardiovasculaire pendant une ischémie cardiovasculaire), ainsi que l'amélioration des processus de cicatrisation des plaies. L'invention concerne également des compositions pharmaceutiques comprenant des quantités efficaces de composés selon la présente invention individuellement ou en combinaison avec un agent supplémentaire stimulant l'érythropoïèse, tel que l'EPO, sous la marque Procrit ou Epogène, ou la darbapoïétine alpha sous la marque Aranesp. L'invention concerne aussi des procédés de stimulation de l'érythropoïèse chez un sujet ou patient, comprenant l'augmentation du nombre de globules rouges et/ou de l'hématocrite du patient, le traitement d'anémie, comprenant l'anémie chronique et l'anémie associée à une maladie rénale chronique, la dialyse et la chimiothérapie du cancer, l'ischémie, l'accident vasculaire cérébral et un endommagement au tissu cardiovasculaire pendant une ischémie cardiovasculaire ainsi que l'amélioration des processus de cicatrisation de plaies et la prévention/réduction de cicatrices consécutives à la cicatrisation. La présente invention concerne également l'amélioration locale de l'angiogenèse par l'induction de VEGF comprenant la cicatrisation des plaies et la réduction d'occlusion d'endoprothèse.
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