Ingenol-3-acylates iii and ingenol-3-carbamates

The disclosure relates to ingenol-3-acylate and ingenol-3-carbamate compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is -NR11R12; and pharmaceutically acceptable salt...

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Main Authors LIANG XIFU, MÅNSSON KRISTOFFER, GRUE-SØRENSEN GUNNAR, VIFIAN THOMAS, HÖGBERG THOMAS, VEDSØ PER
Format Patent
LanguageEnglish
Published 26.08.2016
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The disclosure relates to ingenol-3-acylate and ingenol-3-carbamate compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is -NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in combination with one or more other pharmaceutically active compounds- in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis. Conditions treated include those associated with hyperplasia or neoplasia, cutaneous warts, genitial warts, actinic keratosis, squamous cell carcinoma (SCC), basal cell carcinoma (BCC), lentigo maligna, cervical intraepithelial neoplasia, anal intraepithelial neoplasia or vulva intraepithelial neoplasia. Compounds of the disclosure include: 3-(N-methyl-N-phenyl-carbamate); and 3-(N-(3-fluoro-phenyl)-N-methyl-carbamate)
Bibliography:Application Number: NZ20110710133