Publication number: 20080058377
Abstract: This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).
Type:
Application
Filed:
October 26, 2004
Publication date:
March 6, 2008
Applicant:
Bayer HealthCare AG
Inventors:
Muneto Mogi, Hiroshi Fujishima, Masaomi Tajimi, Noriyuki Yamamoto, Klaus Urbahns, Fumihiko Hayashi, Yasuhiro Tsukimi, Jang Gupta, Hiroaki Yuasa
Publication number: 20080058389
Abstract: The invention relates to novel carboxamides of formula (I), in which M represents a phenyl ring, pyridine ring or pyrimidine, pyridazine or pyrazine ring, respectively monosubstituted by R8, or represents a thiazole ring substituted by R8-A; R8 represents hydrogen, fluorine, chlorine, methyl, isopropyl, methylthio or trifluoromethyl; R8 can also represent methoxy; R8-A represents hydrogen, methyl, methylthio or trifluoromethyl; L1 represents C1-C10 alkene (alkanediyl); Q represents O, S, SO, SO2 or NR9; L2 represents a direct bond, SiR10R11 or CO; R represents hydrogen, C1-C8 alkyl, C1-C8 alkoxy, C1-C4 alkoxy-C1-C4-alkyl, C1-C4 alkylthio-C1-C4-alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C1-C6 haloalkyl, C2-C6-haloalkenyl, C2-C6 haloalkynyl or C3-C6 cycloalkyl; A represents the group of formula (AI); the remaining substituents are defined in claim 1.
Type:
Application
Filed:
January 22, 2005
Publication date:
March 6, 2008
Inventors:
Ralf Dunkel, Hans-Ludwig Elbe, Benoit Hartmann, Jorg Nico Greul, Stefan Herrmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck