Publication number: 20040259875
Abstract: An amine derivative, its tautomeric or stereoisomeric form, or a salt thereof which has vanilloid receptor 1 (VR1) antagonistic activity, is disclosed. The amine derivative has an excellent activity as VR1 antagonist and 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.
Type:
Application
Filed:
July 26, 2004
Publication date:
December 23, 2004
Inventors:
Takeshi Yura, Muneto Mogi, Yuka Ikegami, Tsutomu Masuda, Toshio Kokubo, Klaus Urbahns, Timothy B Lowinger, Nagahiro Yoshida, Joachim Freitag, Heinrich Meier, Reilinde Nopper, Makiko Marumo, Masahiro Shiroo, Masaomi Tajimi, Keisuke Takeshita, Toshiya Moriwaki, Yasuhiro Tsukimi
Patent number: 6589949
Abstract: The invention relates to novel 3-oxo-2,1-benzisomazol-1(3H)-carboxamides (I), where R1, R2 are the same or different and independently=H, halogen, C1 C6 alkyl C1 C6 alkoxy, C1 C3 perfluoroalkyl, or a group NR5R6; R3, R4 are the same or different and independently=C1 C8 alkyl, whose carbon chain is optionally interrupted by an O, S or NR7 and is optionally singly or severally substituted by C3 C6 cycloalkyl, C1 C4 alkoxy, OH, halogen or NR8R9; C3 C8 cycloalkyl whose carbon chain is optionally interrupted by an O, S or NR10 and is optionally singly or severally substituted by C1 C4 alkoxy, OH, halogen or NR11R12, or R3 and R4 together with a nitrogen atom form a saturated or partially unsaturated 3- to 10-membered mono- or bi-cyclic heteocycle, which, optionally, contains up to two further heteroatoms, from N, O or S and is, optionally, substituted by C1 C4 alkyl, C1 C4 alkoxy, OH, halogen, COOR13 or NR14R15 and X=O or S.
Type:
Grant
Filed:
October 22, 2002
Date of Patent:
July 8, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Toshiya Moriwaki, Chantal Fürstner, Bernd Riedl, Jens-Kerim Ergüden, Frank Böss, Bernard Schmidt, Franz-Josef van der Staay, Werner Schröder, Karl-Heinz Schlemmer, Nagahiro Yoshida