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1. WO2013059245 - INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER

Publication Number WO/2013/059245
Publication Date 25.04.2013
International Application No. PCT/US2012/060508
International Filing Date 17.10.2012
IPC
A61K 31/405 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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
C07D 209/26 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
26with an acyl radical attached to the ring nitrogen atom
CPC
A61K 31/404
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
A61K 31/405
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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
C07D 209/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
08with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 209/26
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
26with an acyl radical attached to the ring nitrogen atom
C07D 209/70
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56Ring systems containing three or more rings
58[b]- or [c]-condensed
70containing carbocyclic rings other than six-membered
C07D 231/56
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
54condensed with carbocyclic rings or ring-systems
56Benzopyrazoles; Hydrogenated benzopyrazoles
Applicants
  • VANDERBILT UNIVERSITY [US]/[US]
  • THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA [US]/[US]
Inventors
  • MARNETT, Lawrence, J.
  • LIEDTKE, Andy, J.
  • PENNING, Trevor, M.
  • ADENIJI, Adegoke, O.
  • BYRNS, Michael, C.
Agents
  • PERKINS, Christopher, P.
Priority Data
61/548,00417.10.2011US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER
(FR) ANALOGUES DE L'INDOMÉTACINE DESTINÉS AU TRAITEMENT DU CANCER DE LA PROSTATE RÉSISTANT À LA CASTRATION
Abstract
(EN) Provided are compositions for inhibiting a biological activity of an aldoketo reductase family 1, member C3 (AKR1 C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1 C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.
(FR) L'invention concerne des compositions destinées à inhiber l'activité biologique d'un polypeptide du membre C3 (AKR1 C3) de la famille 1 des aldocéto-réductases. Dans certaines formes de réalisation, les compositions sont des dérivés de l'indométacine constituant des inhibiteurs spécifiques d'AKR1 C3. L'invention concerne aussi des procédés de production des dérivés décrits de l'indométacine qui sont sensiblement dépourvus d'activité d'inhibition de la cyclooxygénase, mais possèdent une activité d'inhibition d'AKR1C3, des procédés visant à inhiber les activités biologiques du polypeptide AKR1C3 et des méthodes de traitement de tumeurs de la prostate chez des sujets.
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