公开(公告)号：US20200024259A1

公开(公告)日：2020-01-23

申请号：US16424366

申请日：2019-05-28

Applicant: DART NEUROSCIENCE (CAYMAN) LTD.

Inventor： Venkataiah Bollu ,  James Breitenbucher ,  Alan Kaplan ,  Robert Lemus ,  Andrew Lindstrom ,  Troy Vickers ,  Michael Weinhouse ,  Mark E. Wilson ,  James Zapf

IPC: C07D403/06 ,  C07D401/06 ,  C07D405/14 ,  C07D413/06 ,  C07D417/06 ,  C07D409/14 ,  C07D213/73 ,  C07D213/74 ,  C07D213/81 ,  C07D213/64 ,  C07D241/18 ,  C07D401/14 ,  C07D405/12 ,  C07D409/06 ,  A61K51/04 ,  C07D239/34

Abstract: The invention provides a chemical entity of Formula (I), and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.

公开(公告)号：US09120770B2

公开(公告)日：2015-09-01

申请号：US14204934

申请日：2014-03-11

Applicant: DART NEUROSCIENCE (CAYMAN) LTD.

Inventor： Venkataiah Bollu ,  James Breitenbucher ,  Alan Kaplan ,  Robert Lemus ,  Andrew Lindstrom ,  Troy Vickers ,  Mark E. Wilson ,  James Zapf

IPC: C07D409/06 ,  C07D401/06 ,  C07D405/14 ,  C07D413/06 ,  C07D417/06 ,  C07D213/64 ,  C07D241/18 ,  C07D401/14 ,  C07D403/06 ,  C07D405/12

CPC classification number: C07D403/06 ,  A61K51/0459 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D213/81 ,  C07D239/34 ,  C07D241/18 ,  C07D401/06 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06

Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.

公开(公告)号：US09040692B2

公开(公告)日：2015-05-26

申请号：US14205033

申请日：2014-03-11

Applicant: DART NEUROSCIENCE (Cayman), LTD.

Inventor： Venkataiah Bollu ,  James Breitenbucher ,  Alan Kaplan ,  Robert Lemus ,  Andrew Lindstrom ,  Troy Vickers ,  Mark E. Wilson ,  James Zapf

IPC: C07D401/06 ,  C07D405/14 ,  C07D413/06 ,  C07D417/06 ,  C07D409/06 ,  C07D213/64 ,  C07D241/18 ,  C07D401/14 ,  C07D403/06 ,  C07D405/12

CPC classification number: C07D403/06 ,  A61K51/0459 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D213/81 ,  C07D239/34 ,  C07D241/18 ,  C07D401/06 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06

Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.

Abstract translation: 本发明提供式（I）的化学实体，其中R 1，R 2，R 3，R 4，Y和Z具有本文所述的任何值，以及包含这些化学实体的组合物; 制作方法; 并在广泛的方法中使用，包括代谢和反应动力学研究，检测和成像技术以及放射性治疗; 和治疗方法，包括抑制PDE4，增强神经元可塑性，治疗神经障碍，提供神经保护，治疗与CNS病症相关的认知障碍，提高认知和运动训练的效率，提供神经复发和神经康复，提高非人类动物的效率 训练方案和治疗外周疾病，包括炎症和肾脏疾病。

公开(公告)号：US20150087645A1

公开(公告)日：2015-03-26

申请号：US14508970

申请日：2014-10-07

Applicant: DART NEUROSCIENCE (CAYMAN) LTD.

Inventor： Alan P. Kaplan ,  Terence P. Keenan ,  Michael I. Weinhouse ,  Mark E. Wilson ,  Andrew K. Lindstrom ,  William C. Ripka ,  Mi Chen

IPC: C07D403/06 ,  C07D401/14 ,  C07D417/14 ,  C07D409/06 ,  C07D403/04 ,  C07D401/04 ,  C07D413/06 ,  C07D241/04 ,  C07D403/14

CPC classification number: C07D403/06 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D241/04 ,  C07D243/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  A61K2300/00

Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.

Abstract translation: 本发明包括式I化合物：其中R 1，Y，A，n，R 4和Z具有本文所述的任何值，以及这些化合物的盐，包含这些化合物的组合物，以及治疗方法， 这样的化合物。 这些化合物是PDE4功能的抑制剂，可用于改善认知功能和/或治疗动物，特别是人类的中枢和周围神经系统和/或精神疾病的认知障碍或损伤，创伤性和/或缺血性损伤。

公开(公告)号：US20180346448A1

公开(公告)日：2018-12-06

申请号：US16001883

申请日：2018-06-06

Applicant: DART NEUROSCIENCE (CAYMAN) LTD.

Inventor： Venkataiah Bollu ,  James Breitenbucher ,  Alan Kaplan ,  Robert Lemus ,  Andrew Lindstrom ,  Troy Vickers ,  Michael Weinhouse ,  Mark E. Wilson ,  James Zapf

IPC: C07D403/06 ,  C07D409/14 ,  C07D409/06 ,  C07D413/06 ,  C07D405/14 ,  C07D401/06 ,  C07D405/12 ,  C07D401/14 ,  C07D241/18 ,  A61K51/04 ,  C07D213/81 ,  C07D213/74 ,  C07D213/73 ,  C07D213/64 ,  C07D239/34 ,  C07D417/06

CPC classification number: C07D403/06 ,  A61K51/0459 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D213/81 ,  C07D239/34 ,  C07D241/18 ,  C07D401/06 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06

Abstract: The invention provides a chemical entity of Formula (I), and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating treating peripheral disorders, including inflammatory and renal disorders.

公开(公告)号：US09624200B2

公开(公告)日：2017-04-18

申请号：US14508970

申请日：2014-10-07

Applicant: DART NEUROSCIENCE (CAYMAN) LTD.

Inventor： Alan P. Kaplan ,  Terence P. Keenan ,  Michael I. Weinhouse ,  Mark E. Wilson ,  Andrew K. Lindstrom ,  William C. Ripka ,  Mi Chen

IPC: A61K31/551 ,  A61K31/495 ,  A61K31/496 ,  C07D403/04 ,  C07D401/04 ,  C07D417/14 ,  C07D409/06 ,  C07D243/08 ,  C07D241/04 ,  C07D413/14 ,  C07D417/06 ,  C07D403/06 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/06 ,  C07D413/06 ,  C07D401/14 ,  C07D403/14

CPC classification number: C07D403/06 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D241/04 ,  C07D243/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D409/06 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  A61K2300/00

Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.