公开(公告)号：US20150258128A1

公开(公告)日：2015-09-17

申请号：US14637334

申请日：2015-03-03

Applicant: UWM Research Foundation, Inc.

Inventor： James M. Cook ,  Terry S. Clayton ,  Hiteshkumar D. Jain ,  Yun Teng Johnson ,  Jie Yang ,  Sundari K. Rallipalli ,  Zhi-jian Wang ,  Ojas A. Namjoshi ,  Michael Ming-Jin Poe

IPC: A61K31/695 ,  A61K31/551

CPC classification number: A61K31/695 ,  A61K31/551 ,  C07D487/04 ,  C07D487/14 ,  C07D519/00

Abstract: Described herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.

Abstract translation: 本文描述的是α3或α2或α2/α3GABA能受体亚型选择性配体，药物组合物，以及这些配体和组合物在治疗焦虑症，癫痫和精神分裂症以及降低镇静和共济失调副作用中的应用的方法。 在实施方案中，诸如α3或α2或α2/α3GABA能受体亚型选择性配体缺少酯键，因此可能因酯酶水解而相对不敏感。

公开(公告)号：US09597342B2

公开(公告)日：2017-03-21

申请号：US14637334

申请日：2015-03-03

Applicant: UWM Research Foundation, Inc.

Inventor： James M. Cook ,  Terry S. Clayton ,  Hiteshkumar D. Jain ,  Yun Teng Johnson ,  Jie Yang ,  Sundari K. Rallipalli ,  Zhi-jian Wang ,  Ojas A. Namjoshi ,  Michael Ming-Jin Poe

IPC: A61K31/551 ,  C07D487/04 ,  A61K31/695 ,  C07D487/14 ,  C07D519/00

CPC classification number: A61K31/695 ,  A61K31/551 ,  C07D487/04 ,  C07D487/14 ,  C07D519/00

Abstract: Described herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.