WO2003014064A8 - Naphthylurea and naphthylacetamide derivatives as vanilloid receptor 1 (vr1) antagonists - Google Patents

Naphthylurea and naphthylacetamide derivatives as vanilloid receptor 1 (vr1) antagonists

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Publication number
WO2003014064A8
WO2003014064A8 PCT/EP2002/008493 EP0208493W WO03014064A8 WO 2003014064 A8 WO2003014064 A8 WO 2003014064A8 EP 0208493 W EP0208493 W EP 0208493W WO 03014064 A8 WO03014064 A8 WO 03014064A8
Authority
WO
WIPO (PCT)
Prior art keywords
formula
naphthylurea
naphthylacetamide
derivatives
vanilloid receptor
Prior art date
Application number
PCT/EP2002/008493
Other languages
French (fr)
Other versions
WO2003014064A1 (en
Inventor
Takeshi Yura
Muneto Mogi
Yuka Ikegami
Tsutoma Masuda
Toshio Kokubo
Klaus Urbahns
Timothy B Lowinger
Nagahiro Yoshida
Joachim Freitag
Heinrich Meier
Reilinde Wittka-Nopper
Makiko Marumo
Masahiro Shiroo
Masaomi Tajimi
Keisuke Takeshita
Toshiya Moriwaki
Yasuhiro Tsukimi
Original Assignee
Bayer Ag
Takeshi Yura
Muneto Mogi
Yuka Ikegami
Tsutoma Masuda
Toshio Kokubo
Klaus Urbahns
Timothy B Lowinger
Nagahiro Yoshida
Joachim Freitag
Heinrich Meier
Reilinde Wittka-Nopper
Makiko Marumo
Masahiro Shiroo
Masaomi Tajimi
Keisuke Takeshita
Toshiya Moriwaki
Yasuhiro Tsukimi
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 JP2001232503A external-priority patent/JP2003055209A/en
Application filed by Bayer Ag, Takeshi Yura, Muneto Mogi, Yuka Ikegami, Tsutoma Masuda, Toshio Kokubo, Klaus Urbahns, Timothy B Lowinger, Nagahiro Yoshida, Joachim Freitag, Heinrich Meier, Reilinde Wittka-Nopper, Makiko Marumo, Masahiro Shiroo, Masaomi Tajimi, Keisuke Takeshita, Toshiya Moriwaki, Yasuhiro Tsukimi filed Critical Bayer Ag
Priority to AU2002325381A priority Critical patent/AU2002325381A1/en
Priority to JP2003524319A priority patent/JP2005501873A/en
Priority to EP02758413A priority patent/EP1414788A1/en
Priority to US10/485,481 priority patent/US20040259875A1/en
Priority to CA002455754A priority patent/CA2455754A1/en
Publication of WO2003014064A1 publication Critical patent/WO2003014064A1/en
Publication of WO2003014064A8 publication Critical patent/WO2003014064A8/en

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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/38—Nitrogen atoms
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    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes

Abstract

Naphthylurea and naphthylacetamide derivatives of formula (I) which have vanilloid receptor 1 (VR1) antagonistic activity are disclosed, formula (I) wherein Y represents formula (II) and formula (III) and the variables Q, X, R6, R7, R8, R8a, R9, R10 and R11 are as defined in the claims. The compounds are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.
PCT/EP2002/008493 2001-07-31 2002-07-31 Naphthylurea and naphthylacetamide derivatives as vanilloid receptor 1 (vr1) antagonists WO2003014064A1 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
AU2002325381A AU2002325381A1 (en) 2001-07-31 2002-07-31 Naphthylurea and naphthylacetamide derivatives as vanilloid receptor 1 (vr1) antagonists
JP2003524319A JP2005501873A (en) 2001-07-31 2002-07-31 Amine derivatives
EP02758413A EP1414788A1 (en) 2001-07-31 2002-07-31 Naphthylurea and naphthylacetamide derivatives as vanilloid receptor 1 (vr1) antagonists
US10/485,481 US20040259875A1 (en) 2001-07-31 2002-07-31 Amine derivatives
CA002455754A CA2455754A1 (en) 2001-07-31 2002-07-31 Amine derivatives

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2001232503A JP2003055209A (en) 2001-07-31 2001-07-31 Phenylnaphthylurea derivative
JP232503-2001 2001-07-31
JP2001392310 2001-12-25
JP392310-2001 2001-12-25

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WO2003014064A8 true WO2003014064A8 (en) 2003-11-27

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