WO2007016979A3 - NOVEL HETEROCYCLIC NF-κB INHIBITORS - Google Patents

NOVEL HETEROCYCLIC NF-κB INHIBITORS Download PDF

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Publication number
WO2007016979A3
WO2007016979A3 PCT/EP2006/002396 EP2006002396W WO2007016979A3 WO 2007016979 A3 WO2007016979 A3 WO 2007016979A3 EP 2006002396 W EP2006002396 W EP 2006002396W WO 2007016979 A3 WO2007016979 A3 WO 2007016979A3
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WO
WIPO (PCT)
Prior art keywords
alkyl
haloalkyl
hydroxyalkyl
heteroaryl
cycloalkyl
Prior art date
Application number
PCT/EP2006/002396
Other languages
French (fr)
Other versions
WO2007016979A2 (en
Inventor
Johann Leban
Harald Schmitt
Kristina Wolf
Stefano Pegoraro
Andreas Wuzik
Original Assignee
4Sc Ag
Johann Leban
Harald Schmitt
Kristina Wolf
Stefano Pegoraro
Andreas Wuzik
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
Priority claimed from PCT/EP2005/008261 external-priority patent/WO2006032322A1/en
Application filed by 4Sc Ag, Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik filed Critical 4Sc Ag
Priority to AU2006278998A priority Critical patent/AU2006278998A1/en
Priority to UAA200802635A priority patent/UA97348C2/en
Priority to EP06707574A priority patent/EP1912982A2/en
Priority to CA002617225A priority patent/CA2617225A1/en
Priority to JP2008523136A priority patent/JP2009502816A/en
Priority to NZ565470A priority patent/NZ565470A/en
Priority to BRPI0614188-9A priority patent/BRPI0614188A2/en
Priority to EA200800175A priority patent/EA016300B1/en
Publication of WO2007016979A2 publication Critical patent/WO2007016979A2/en
Priority to BRPI0709595-3A priority patent/BRPI0709595A2/en
Priority to MX2008011696A priority patent/MX2008011696A/en
Priority to PCT/EP2007/002265 priority patent/WO2007104557A2/en
Priority to CNA2007800092336A priority patent/CN101405278A/en
Priority to CA002646223A priority patent/CA2646223A1/en
Priority to AU2007224659A priority patent/AU2007224659A1/en
Priority to EA200801838A priority patent/EA200801838A1/en
Priority to JP2008558718A priority patent/JP2009529555A/en
Priority to KR1020087022353A priority patent/KR20080104147A/en
Priority to EP07711946A priority patent/EP1994017A2/en
Publication of WO2007016979A3 publication Critical patent/WO2007016979A3/en
Priority to IL189112A priority patent/IL189112A0/en
Priority to NO20081056A priority patent/NO20081056L/en
Priority to IL193981A priority patent/IL193981A0/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61P37/02—Immunomodulators
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three 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
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    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07D417/02—Heterocyclic 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 containing two hetero rings
    • C07D417/06—Heterocyclic 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 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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 containing two hetero rings
    • C07D417/12—Heterocyclic 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 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/14—Heterocyclic 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 containing three or more hetero rings
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Toxicology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The present invention relates to compounds of the general formula (III) or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof, Formula (III) wherein R3 is H, -C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4’ OR5’ , NH2, amine, alkylamine, alkoxy, cycloalkyl, heterocyclo-alkyl,hydroxyalkyl, or haloalkyloxy; R4 is H, halogen, alkyl, -C(NR7)NR7’R8, -(CH2)paryl, -(CH2)PNR7R8, -C(O)NR7R8, -N=CR7R8, -NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hydroxyalkylamino, alkylamino, heteroaryl, or aryl; R5 is halogen, alkyl, -C(NR7)NR7’R8, -(CH2)paryl, -(CH2)PNR7R8, -C(O)NR7R8, -N=CR7R8, -NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hydroxyalkylamino, alkylamino, heteroaryl, or aryl.
PCT/EP2006/002396 2005-07-29 2006-03-15 NOVEL HETEROCYCLIC NF-κB INHIBITORS WO2007016979A2 (en)

Priority Applications (21)

Application Number Priority Date Filing Date Title
AU2006278998A AU2006278998A1 (en) 2005-07-29 2006-03-15 Novel heterocyclic NF-kB inhibitors
UAA200802635A UA97348C2 (en) 2005-07-29 2006-03-15 HETEROCYCLIC NF-kB INHIBITORS
EP06707574A EP1912982A2 (en) 2005-07-29 2006-03-15 Novel heterocyclic nf- b inhibitors
CA002617225A CA2617225A1 (en) 2005-07-29 2006-03-15 Novel heterocyclic nf-kb inhibitors
JP2008523136A JP2009502816A (en) 2005-07-29 2006-03-15 Novel heterocyclic NF-κB inhibitor
NZ565470A NZ565470A (en) 2005-07-29 2006-03-15 Novel heterocyclic NF-kB inhibitors
BRPI0614188-9A BRPI0614188A2 (en) 2005-07-29 2006-03-15 heterocyclic nf-kappab inhibitor compounds, their use and pharmaceutical composition
EA200800175A EA016300B1 (en) 2005-07-29 2006-03-15 NOVEL HETEROCYCLIC NF-κB INHIBITORS
KR1020087022353A KR20080104147A (en) 2006-03-15 2007-03-14 Novel heterocyclic nf-kappa;b inhibitors
EP07711946A EP1994017A2 (en) 2006-03-15 2007-03-14 Novel heterocyclic nf-kb inhibitors
JP2008558718A JP2009529555A (en) 2006-03-15 2007-03-14 Novel heterocyclic NF-κB inhibitor
BRPI0709595-3A BRPI0709595A2 (en) 2006-03-15 2007-03-14 heterocyclic nf-kapab inhibitors
PCT/EP2007/002265 WO2007104557A2 (en) 2006-03-15 2007-03-14 Novel heterocyclic nf-kb inhibitors
CNA2007800092336A CN101405278A (en) 2006-03-15 2007-03-14 Novel heterocyclic NF-kB inhibitors
CA002646223A CA2646223A1 (en) 2006-03-15 2007-03-14 Novel heterocyclic nf-kb inhibitors
AU2007224659A AU2007224659A1 (en) 2006-03-15 2007-03-14 Novel heterocyclic NF-KB inhibitors
EA200801838A EA200801838A1 (en) 2006-03-15 2007-03-14 NEW HETEROCYCLIC INHIBITORS NF-kB
MX2008011696A MX2008011696A (en) 2006-03-15 2007-03-14 Novel heterocyclic nf-kb inhibitors.
IL189112A IL189112A0 (en) 2005-07-29 2008-01-29 NOVEL HETEROCYCLIC NF-kB INHIBITORS
NO20081056A NO20081056L (en) 2005-07-29 2008-02-28 Novel, heterocyclic NF-kB inhibitors
IL193981A IL193981A0 (en) 2006-03-15 2008-09-09 Novel heterocyclic nf-kb inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EPPCT/EP2005/008261 2005-07-29
PCT/EP2005/008261 WO2006032322A1 (en) 2004-09-20 2005-07-29 NOVEL HETEROCYCLIC NF-κB INHIBITORS

Publications (2)

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WO2007016979A2 WO2007016979A2 (en) 2007-02-15
WO2007016979A3 true WO2007016979A3 (en) 2007-08-02

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Application Number Title Priority Date Filing Date
PCT/EP2006/002396 WO2007016979A2 (en) 2005-07-29 2006-03-15 NOVEL HETEROCYCLIC NF-κB INHIBITORS

Country Status (13)

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JP (1) JP2009502816A (en)
KR (1) KR20080031038A (en)
CN (1) CN101233119A (en)
AU (1) AU2006278998A1 (en)
BR (1) BRPI0614188A2 (en)
CA (1) CA2617225A1 (en)
EA (1) EA016300B1 (en)
IL (1) IL189112A0 (en)
NO (1) NO20081056L (en)
NZ (2) NZ588971A (en)
SG (1) SG172738A1 (en)
UA (1) UA97348C2 (en)
WO (1) WO2007016979A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11690853B2 (en) 2015-06-29 2023-07-04 Reveragen Biopharma, Inc. Non-hormonal steroid modulators of NF-κβ for treatment of disease

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA012607B1 (en) * 2004-09-20 2009-10-30 4Сц Аг NOVEL HETEROCYCLIC NF-kB INHIBITORS
EA200801838A1 (en) * 2006-03-15 2009-02-27 4ЭсЦэ АГ NEW HETEROCYCLIC INHIBITORS NF-kB
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