公开(公告)号：US09708334B2

公开(公告)日：2017-07-18

申请号：US15306064

申请日：2015-04-22

Applicant: DART NEUROSCIENCE (CAYMAN) LTD.

Inventor： Jillian Basinger ,  Brett Bookser ,  Mi Chen ,  DeMichael Chung ,  Varsha Gupta ,  Andrew Hudson ,  Alan Kaplan ,  James Na ,  Joel Renick ,  Vincent Santora

IPC: C07D471/04 ,  C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D519/00

Abstract: The invention provides a chemical entity of Formula (I), wherein R1, R2, R3, R4, R5 and X 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; radioactive treatments; modulating and treating disorders mediated by GlyT1 activity; treating neurological disorders, CNS disorders, dementia, neurodegenerative diseases, and trauma-dependent losses of function; treating stroke, including cognitive and motor deficits during stroke rehabilitation; facilitating neuroprotection and neurorecovery; enhancing the efficiency of cognitive and motor training, including animal skill training; and treating other disorders, including pain and alcohol-dependence.

公开(公告)号：US20160009691A1

公开(公告)日：2016-01-14

申请号：US14770759

申请日：2014-03-06

Applicant: DART NEUROSCIENCE (CAYMAN) LTD.

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

IPC: C07D403/06 ,  C07D401/06 ,  C07D239/34 ,  C07D213/64 ,  C07D405/12 ,  C07D417/06 ,  A61K51/04 ,  C07D401/14

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 peripheral disorders, including inflammatory and renal disorders.

Abstract translation: 本发明提供式（I）的化学实体和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：US09102674B2

公开(公告)日：2015-08-11

申请号：US14204738

申请日：2014-03-11

Applicant: DART NEUROSCIENCE (CAYMAN) LTD.

Inventor： Jillian Basinger ,  Graeme Freestone ,  Varsha Gupta ,  Alan Kaplan ,  Chi-Ching Mak ,  Benjamin Pratt ,  Vincent Santora ,  Dipanjan Sengupta ,  Lino Valdez

IPC: C07D215/54 ,  C07D471/04 ,  C07D215/60 ,  C07D401/12

CPC classification number: A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  C07D215/20 ,  C07D215/22 ,  C07D215/54 ,  C07D215/60 ,  C07D401/12 ,  C07D471/04

Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n 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 MAO, and MAO-B selectively, 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 obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.

Abstract translation: 本发明提供式（I）的化学实体，其中R 1，R 2，R 3，Y和n具有本文所述的任何值和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; 选择性地抑制MAO和MAO-B的治疗，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，增强 非人类动物训练方案的效率以及治疗周围疾病（包括肥胖，糖尿病和心脏代谢紊乱）及其相关并发症。

公开(公告)号：US20150329500A1

公开(公告)日：2015-11-19

申请号：US14720321

申请日：2015-05-22

Applicant: Dart Neuroscience (Cayman) Ltd.

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

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

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：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：US09675605B2

公开(公告)日：2017-06-13

申请号：US14862874

申请日：2015-09-23

Applicant: DART NEUROSCIENCE (CAYMAN) LTD.

Inventor： Jillian Basinger ,  Graeme Freestone ,  Varsha Gupta ,  Alan Kaplan ,  Chi Ching Mak ,  Benjamin Pratt ,  Vincent Santora ,  Dipanjan Sengupta ,  Lino Valdez

IPC: C07D471/04 ,  A61K31/4375 ,  A61K31/47 ,  C07D215/54 ,  C07D215/60 ,  C07D401/12 ,  A61K31/4709 ,  C07D215/20 ,  C07D215/22

CPC classification number: A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  C07D215/20 ,  C07D215/22 ,  C07D215/54 ,  C07D215/60 ,  C07D401/12 ,  C07D471/04

Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n 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 MAO, and MAO-B selectively, 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 obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.

公开(公告)号：US09650349B2

公开(公告)日：2017-05-16

申请号：US14709206

申请日：2015-05-11

Applicant: Dart Neuroscience (Cayman) Ltd.

Inventor： Alan Kaplan ,  Terence Keenan ,  Andrew McRiner

IPC: A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  C07D261/08 ,  C07D413/04 ,  C07D413/14 ,  C07D453/02 ,  C07D487/04 ,  C07D491/044

CPC classification number: C07D491/044 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/454 ,  A61P25/00 ,  C07D261/08 ,  C07D413/04 ,  C07D413/14 ,  C07D453/02 ,  C07D487/04

Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B 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 monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.

公开(公告)号：US09573937B2

公开(公告)日：2017-02-21

申请号：US14720321

申请日：2015-05-22

Applicant: Dart Neuroscience (Cayman) Ltd.

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

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

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：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。