Patent number: 6911443
Abstract: A compound of the formula (I) in which R1 is —OR11, —SR11, —SOR11, —SO2R11, —NHR11, or —NR12R13 , and R11, R12, and R13 are as defined broadly in the text. R2 is H, C1-C6alkyl, carbamoyl, or an ester group. R3 is thienyl, pyridyl optionally substituted by halogen or C1-C6alkoxy; naphthyl optionally substituted by C1-C6alkoxy; dioxane fused phenyl; dioxacyclopentane fused phenyl; or optionally substituted phenyl. Y is CH or N. A process for preparing such compounds, pharmaceutical compositions containing such compounds, and a method of treating asthma using them are also disclosed and claimed.
Type:
Grant
Filed:
April 17, 2001
Date of Patent:
June 28, 2005
Assignee:
Bayer Aktiengesellschaft
Inventors:
Takeshi Yura, Arnel B. Concepcion, Gyoonhee Han, Makiko Marumo, Hiroko Yoshino, Norihiro Kawamura, Toshio Kokubo, Hiroshi Komura, Yingfu Li, Timothy B. Lowinger, Muneto Mogi, Noriyuki Yamamoto, Nagahiro Yoshida, Scott Miller, Margaret A. Popp, Aniko M. Redmann, Martha E. Rodriguez, William J. Scott, Ming Wang
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
Publication number: 20040054179
Abstract: A compound of the formula (I) wherein R1 is —X—R4, an optionally substituted heterocyclic residue, an optionally substituted carbocyclic residue or optionally substituted condensed ring moiety; X is CR5R6, O, S, SO, SO2 or NR7; Y is CH or N; R2 is H, an optionally substituted C1-C10 alkyl,etc.; R3 is an optionally substituted aryl, or an optionally substituted heteroaryl, etc.; R4 is an optionally substituted aryl, an optionally substituted heteroaryl, etc.; R5, R6, and R7 can be identical or different and represent H, an optionally substituted C1-C10 alkyl, etc. The compound has an excellent anti-allergic activity and the like.
Type:
Application
Filed:
February 14, 2003
Publication date:
March 18, 2004
Inventors:
Takeshi Yura, Arnel b Concepcion, Gyoonhee Han, Makiko Marumo, Hiroko Yoshino, Norihiro Kawamura, Toshio Kokubo, Hiroshi Komura, Yingfu Li, Timothy B LOwinger, Muneto Mogi, Noriyuki Yamamoto, Nagahiro Yoshida, Scott Miller, Margaret A Popp, Aniko M Redmann, Martha E Rodriguez, William J Scott, Ming Wang