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Title:
DERIVATIVES OF N-(1H-INDAZOLYL)- AND N-(1H-INDOLYL)-UREA AS WELL AS RELATED COMPOUNDS AS MODULATORS OF THE VANILLOID-1 RECEPTOR (VR1) FOR THE TREATMENT OF PAIN
Document Type and Number:
WIPO Patent Application WO2005028445
Kind Code:
A3
Abstract:
Compounds of formula (I): wherein A, B and D are each C, N, O or S; E is C or N; the dotted circle within the five-membered ring indicates that the ring may be unsaturated or partially saturated;. R <1> is halogen, hydroxy, C 1-6 álkyl, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, C 1-6 alkoxy, halo C 1-6 alkoxy, hydroxyC 1-6 alkoxy, C 3-7 cycloalkyl, C 3-5 cycloalkylC 1-4 alkyl, NR<7>R<8>, C 1-6 alkyl substituted with NR<7>R<8>, C, 1-6 alkoxy substituted with NR<7>R<8>, oxo, cyano, SO2NR<7>R<8>, CONR<7>R<8>, NHCOR<9> or NHSO2R <9> ; R<2 >is halogen, hydroxy, C 1-6 alkyl, halo C 1-6 alkyl, hydroxyC 1-6 alkyl, C 1-6 alkoxy, halo C 1-6 alkoxy, hydroxyC 1-6 alkoxy, C 3-7 cycloalkyl, C 3-5 cycloalkylC 1-4 alkyl, NR<7>R<8>, C 1-6 alkyl substituted with NR<7>R<8>, C 1-6 , alkoxy substituted with NR<7>R<8>, cyano, SON2R<7>R<8>, CONR<7>R<8>, NHCOR<9> , or NHSO2R<9>; R<3 >and R <4> are each independently hydrogen, C 1-6 ,alkyl, phenyl or halophenyl; R<5 >and R <6> are, at each occurrence, independently hydrogen, C 1-6 alkyl, phenyl, halophenyl or carboxy; X is an oxygen or sulfur atom; Y is an aryl, heteroaryl, carbocyclyl or fused-carbocyclyl group; n is either zero or an integer from 1 to 3; p is either zero or an integer from, 1 to 4; and q is either zero or an integer from 1 to 3; the other substituents are defined in claim 1; are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).

Inventors:
FLETCHER STEPHEN ROBERT (GB)
HOLLINGWORTH GREGORY JOHN (GB)
JONES A BRIAN (GB)
MOYES CHRISTOPHER RICHARD (GB)
ROGERS LAUREN (GB)
Application Number:
GB2004003968W
Publication Date:
June 02, 2005
Filing Date:
September 16, 2004
Export Citation:
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Assignee:
MERCK SHARP & DOHME (GB)
FLETCHER STEPHEN ROBERT (GB)
HOLLINGWORTH GREGORY JOHN (GB)
JONES A BRIAN (GB)
MOYES CHRISTOPHER RICHARD (GB)
ROGERS LAUREN (GB)
International Classes:
C07C275/28; C07D209/34; C07D231/56; C07D235/06; C07D263/56; C07D275/04; C07D307/79; C07D471/04; (IPC1-7): A61K31/416; A61K31/428; A61K31/404; A61K31/437; A61K31/4245; A61K31/343; C07D231/56; C07D277/62; C07D209/08; C07D471/04; C07D275/04; C07D263/56; C07D209/34; C07D307/79; C07C275/28
Domestic Patent References:
WO2003055484A12003-07-10
WO2003070247A12003-08-28
WO2002016318A12002-02-28
WO1999000357A11999-01-07
WO1997028143A11997-08-07
WO2003087046A12003-10-23
Foreign References:
EP1256574A12002-11-13
US3711610A1973-01-16
US3486894A1969-12-30
US20040157849A12004-08-12
Other References:
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 14 August 2003 (2003-08-14), MENON, SANJAY ET AL: "A parallel synthesis demonstration library of tri-substituted indazoles containing new antimutagenic/antioxidant hits related to benzydamine", XP002309640, retrieved from STN Database accession no. 2003:625432
HONMA ET AL.: "Structure-based generation of Cdk4 Inhibitors", JOURNAL OF MEDICINAL CHEMISTRY, vol. 44, no. 26, 2001, pages 4615 - 1627, XP002309787
NAKAO ET AL.: "Qualitative Structure-Activity Analysies of Novel Hydroxyphenylurea Cerivatives as Antioxidants", BIOORGANIC AND MEDICINAL CHEMISTRY, vol. 6, no. 6, 1998, pages 849 - 868, XP002309788
TAKAMI ET AL.: "Design and synthesis of Rho kinase inhibitors (I)", BIOORGANIC AND MEDICINAL CHEMISTRY, vol. 12, no. 9, 1 May 2004 (2004-05-01), pages 2115 - 2137, XP002309639
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