公开(公告)号：US08673920B2

公开(公告)日：2014-03-18

申请号：US12768209

申请日：2010-04-27

Applicant: Alexander Pasternak ,  Aurash Shahripour ,  Haifeng Tang ,  Nardos H. Teumelsan ,  Lihu Yang ,  Yuping Zhu ,  Shawn P. Walsh

Inventor： Alexander Pasternak ,  Aurash Shahripour ,  Haifeng Tang ,  Nardos H. Teumelsan ,  Lihu Yang ,  Yuping Zhu ,  Shawn P. Walsh

IPC: A61K31/496 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  A61K31/407 ,  A61K31/495 ,  A61K31/551 ,  C07D295/092 ,  C07D487/08

CPC classification number: C07D307/88 ,  C07D295/135 ,  C07D295/155 ,  C07D405/08 ,  C07D407/08 ,  C07D413/08 ,  C07D487/08 ,  C07D493/04

Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.

Abstract translation: 本发明涉及具有结构式I的化合物及其药学上可接受的盐，它们是肾外
膜（ROMK）通道（Kir1.1）的抑制剂。 式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水保持引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。

公开(公告)号：US06730690B2

公开(公告)日：2004-05-04

申请号：US10457682

申请日：2003-06-09

Applicant: Steven H. Olson ,  James M. Balkovec ,  Yuping Zhu

Inventor： Steven H. Olson ,  James M. Balkovec ,  Yuping Zhu

IPC: A61K314196

CPC classification number: C07D249/08

Abstract: Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11&bgr;-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.

Abstract translation: 具有式I的化合物，包括其药学上可接受的盐，水合物和溶剂化物：是11beta-HSD1酶的选择性抑制剂。 这些化合物可用于治疗糖尿病，例如非胰岛素依赖性糖尿病（NIDDM），高血糖症，肥胖症，胰岛素抵抗，甲状腺脂肪血症，高脂血症，高血压，X综合征和与NIDDM相关的其他症状。