IN2014DN11023A - - Google Patents

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Publication number
IN2014DN11023A
IN2014DN11023A IN11023DEN2014A IN2014DN11023A IN 2014DN11023 A IN2014DN11023 A IN 2014DN11023A IN 11023DEN2014 A IN11023DEN2014 A IN 11023DEN2014A IN 2014DN11023 A IN2014DN11023 A IN 2014DN11023A
Authority
IN
India
Prior art keywords
compounds
pharmaceutically acceptable
methods
relates
dysplasia
Prior art date
Application number
Inventor
Xifu Liang
Thomas Högberg
Bjarne Nørremark
Kristoffer Månsson
Carsten Ryttersgaard
SØRENSEN Gunnar GRUE
Original Assignee
Leo Lab Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Leo Lab Ltd filed Critical Leo Lab Ltd
Publication of IN2014DN11023A publication Critical patent/IN2014DN11023A/en

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/70—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/20—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C07D271/07—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Gerontology & Geriatric Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Cosmetics (AREA)

Abstract

The present invention relates to a compound according to formula (I) wherein R1 represents optionally substituted heteroaryl and pharmaceutically acceptable salts hydrates solvates or pharmaceutically acceptable and physiologically cleavable esters thereof. The invention relates further to intermediates for the preparation of said compounds to said compounds for use in therapy to pharmaceutical compositions comprising said compounds to methods of treating diseases e.g. diseases associated with hyperplasia neoplasia or dysplasia with said compounds to methods of treatment of cosmetic indications with said compounds and to the use of said compounds in the manufacture of medicaments.
IN11023DEN2014 2012-06-26 2013-06-21 IN2014DN11023A (en)

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US201261664398P 2012-06-26 2012-06-26
US201361763206P 2013-02-11 2013-02-11
PCT/EP2013/062995 WO2014001215A2 (en) 2012-06-26 2013-06-21 3-o-heteroaryl-ingenol

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EP3060209A1 (en) 2013-10-25 2016-08-31 Leo Laboratories Limited A method for topically treating actinic keratosis on the full balding scalp with ingenol 3-(3,5-diethylisoxazole-4-carboxylate)
WO2016191835A1 (en) * 2015-06-03 2016-12-08 Amazônia Fitomedicamentos Ltda. Method for preparing ingenol-5,20-acetonide, method for preparing 3-ethynyl-3-hydroxy-4,7,7-trimethylbicyclo[4.1.0]heptane-2-carbaldehyde, method for preparing the compound 2,2-dimethyl-4-ethynyl-5-triphenylphosphorus anylidene-1,3-dioxane and intermediate compound
WO2017089300A1 (en) * 2015-11-27 2017-06-01 Leo Laboratories Limited 3-alkylamido-3-deoxy-ingenols
US10583140B2 (en) 2016-01-27 2020-03-10 Glaxosmithkline Intellectual Property Development Limited Ingenol analogs, pharmaceutical compositions and methods of use thereof
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment

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DE2902506A1 (en) * 1979-01-23 1980-07-24 Deutsches Krebsforsch USE OF DITERPENAL ALCOHOLS AND DERIVATIVES THEREOF AS AN ANTINEOPLASTIC AGENT, OR ONLY LITTLE IRRITATING AND / OR PROMOVING
AUPO864097A0 (en) 1997-08-19 1997-09-11 Peplin Pty Ltd Anti-cancer compounds
NZ583157A (en) * 2004-12-13 2011-12-22 Leo Lab Ltd Treatment of solid cancers with angeloyl substituted ingenanes
BRPI0618926A2 (en) * 2005-11-25 2011-09-13 Peplin Research Pty Ltd use of an ingenol compound or a pharmaceutically acceptable salt thereof
GB0525680D0 (en) 2005-12-16 2006-01-25 Peplin Ltd Therapeutic compositions
PL2152261T3 (en) * 2007-04-30 2016-06-30 Leo Laboratories Ltd Treatment of virally induced lesions
US20100189674A1 (en) 2007-05-11 2010-07-29 Sonneborn Inc. Petrolatum Having Silicone-Like Properties
JP5845283B2 (en) 2010-12-22 2016-01-20 レオ・ラボラトリーズ・リミテッドＬｅｏ Ｌａｂｏｒａｔｏｒｉｅｓ Ｌｉｍｉｔｅｄ Ingenol-3-acylate III and ingenol-3-carbamate
US9388124B2 (en) 2010-12-22 2016-07-12 Leo Laboratories Limited Ingenol-3-acylates I
EP2655312A1 (en) 2010-12-22 2013-10-30 Leo Laboratories Limited 3-acyl-ingenols ii

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ES2640612T3 (en) 2017-11-03
WO2014001215A3 (en) 2014-02-27
IL235925A0 (en) 2015-02-01
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US9422309B2 (en) 2016-08-23
MX2014015497A (en) 2015-03-06
AU2013283511B2 (en) 2017-10-26
WO2014001215A2 (en) 2014-01-03
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CN104411685A (en) 2015-03-11
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PT2864290T (en) 2017-09-19
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CN104411685B (en) 2017-03-29
DK2864290T3 (en) 2017-10-02
AU2013283511A1 (en) 2014-12-18
SG11201408016XA (en) 2015-03-30
EP2864290A2 (en) 2015-04-29
CA2875461A1 (en) 2014-01-03
PL2864290T3 (en) 2017-11-30

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