- Discovery of a Slow Tight Binding LPA1 Antagonist (ONO-0300302) for the Treatment of Benign Prostatic Hyperplasia
-
Scaffold hopping from the amide group of lead compound ONO-7300243 (1) to a secondary alcohol successfully gave a novel chemotype lysophosphatidic acid receptor 1 (LPA1) antagonist 4. Wash-out experiments using rat isolated urethra showed that
- Terakado, Masahiko,Suzuki, Hidehiro,Hashimura, Kazuya,Tanaka, Motoyuki,Ueda, Hideyuki,Hirai, Keisuke,Asada, Masaki,Ikura, Masahiro,Matsunaga, Naoki,Saga, Hiroshi,Shinozaki, Koji,Karakawa, Naoko,Takada, Yuka,Minami, Masashi,Egashira, Hiromu,Sugiura, Yoshihiro,Yamada, Masanori,Nakade, Shinji,Takaoka, Yoshikazu
-
p. 1281 - 1286
(2017/12/26)
-
- COMPOUNDS HAVING LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISM AND USES THEREOF
-
The present invention relates to a compound represented by formula (I): (wherein the symbols in formula were described in the description), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention binds to and is antagonistic to an LPA receptor (particularly, EDG-2), it is useful for prevention and/or treatment of urinary system disease (prostatic hypertrophy or neurogenic bladder dysfunction disease, spinal cord neoplasm, nucleous hernia, spinal canal stenosis, diseases caused by diabetes, occlusion disease of lower urinary tract, inflammatory disease of lower urinary tract, and polyuria), carcinoma-associated disease, proliferative disease, inflammation system disease, immune system disease, disease by secretory dysfunction, brain-related disease and/or chronic disease.
- -
-
Page/Page column 56
(2010/11/23)
-