05-07-2012 дата публикации
Номер: US20120172393A1
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds that, inter alia, inhibit 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc. 1124-. (canceled)126. A compound according to claim 125 , wherein:{'sup': '1', '—Yis —OH;'}{'sup': 2', '2A, '—Yis —Y;'}{'sup': 3', '3A', '3C, '—Yis —Yor —Y;'}{'sup': '4', '—Yis —F; and'}{'sup': '5', '—Yis —CN;'}{'sup': 2A', 'YA, '—Yis —OR;'}{'sup': 3A', 'YA, '—Yis —R;'}{'sup': 3C', 'YC, '—Yis —R;'}{'sup': 'YA', 'each —Ris -Me; and'}{'sup': 'YC', 'sub': '2', '—Ris —CHOH.'}127. A compound according to claim 126 , wherein —Y is —Yor —Y.128. A compound according to claim 126 , wherein:{'sup': 1', '2', '3', '4, 'each of -J, -J, -J, and -Jis —H; or'}{'sup': 2', '4', '1', '3, 'sub': 2', '2, 'each of -Jand -Jis —H, and -Jand -Jtaken together form —CHCH—; or'}{'sup': 1', '3', '2', '4, 'sub': 2', '2, 'each of -Jand -Jis —H; and -Jand -Jtaken together form —CHCH—.'}129. A compound according to claim 127 , wherein:{'sup': 1', '2', '3', '4, 'each of -J, -J, -J, and -Jis —H; or'}{'sup': 2', '4', '1', '3, 'sub': 2', '2, 'each of -Jand -Jis —H, and -Jand -Jtaken together form —CHCH—; or'}{'sup': 1', '3', '2', '4 ...
Подробнее