公开(公告)号：US20170204050A1

公开(公告)日：2017-07-20

申请号：US15418986

申请日：2017-01-30

Applicant: Sunovion Pharmaceuticals Inc.

Inventor： Liming SHAO ,  Fengjiang WANG ,  Scott Christopher MALCOLM ,  Michael Charles HEWITT ,  Jianguo MA ,  Seth RIBE ,  Mark A. VARNEY ,  Una CAMPBELL ,  Sharon Rae ENGEL ,  Larry Wendell HARDY ,  Patrick KOCH ,  Rudy SCHREIBER ,  Kerry L. Spear

IPC: C07C215/42 ,  C07C217/76

CPC classification number: C07C215/42 ,  A61K31/135 ,  A61P25/24 ,  A61P25/28 ,  C07B2200/07 ,  C07C217/52 ,  C07C217/76 ,  C07C2601/14

Abstract: Phenyl-substituted cyclohexylamine derivatives and methods for their synthesis and characterization are disclosed. Use of these compounds to treat/prevent neurological disorders as well as methods for their synthesis are set forth herein. Exemplary compounds of the invention inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations incorporating compounds of the invention are also provided.

公开(公告)号：US09670230B2

公开(公告)日：2017-06-06

申请号：US14646888

申请日：2013-11-25

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： John Emmerson Campbell ,  Philip Jones

IPC: C07D519/00 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/553

CPC classification number: C07D519/00 ,  A61K31/4985 ,  A61K31/5383 ,  A61K31/553 ,  C07D487/04

Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.

公开(公告)号：US09586888B2

公开(公告)日：2017-03-07

申请号：US14149492

申请日：2014-01-07

Applicant: Sunovion Pharmaceuticals Inc.

Inventor： Liming Shao ,  Fengjiang Wang ,  Scott Christopher Malcolm ,  Michael Charles Hewitt ,  Jianguo Ma ,  Seth Ribe ,  Mark A. Varney ,  Una Campbell ,  Sharon Rae Engel ,  Larry Wendell Hardy ,  Patrick Koch ,  Rudy Schreiber ,  Kerry L. Spear

IPC: C07C215/42 ,  C07C217/52 ,  C07C217/76 ,  A61K31/135

CPC classification number: C07C215/42 ,  A61K31/135 ,  A61P25/24 ,  A61P25/28 ,  C07B2200/07 ,  C07C217/52 ,  C07C217/76 ,  C07C2601/14

Abstract: Phenyl-substituted cyclohexylamine derivatives and method for their synthesis and characterization are disclosed. Use of these compounds to treat/prevent neurological disorders as well as methods for their synthesis are set forth herein. Exemplary compounds of the invention inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations incorporating compounds of the invention are also provided.

Abstract translation: 公开了苯基取代的环己胺衍生物及其合成和表征的方法。 本文阐述了这些化合物治疗/预防神经系统疾病及其合成方法的用途。 本发明的示例性化合物抑制内源性单胺如多巴胺，5-羟色胺和去甲肾上腺素的再摄取（例如，从突触腭裂）并调节一种或多种单胺转运蛋白。 还提供了掺入本发明化合物的药物制剂。

公开(公告)号：US09505716B2

公开(公告)日：2016-11-29

申请号：US14726797

申请日：2015-06-01

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Liming Shao ,  Jianguo Ma

IPC: C07D207/08 ,  C07D207/06 ,  A61K31/40 ,  C07D207/12 ,  C07D405/04

CPC classification number: C07D207/06 ,  A61K31/40 ,  C07D207/08 ,  C07D207/12 ,  C07D405/04

Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

公开(公告)号：US09040588B2

公开(公告)日：2015-05-26

申请号：US14157793

申请日：2014-01-17

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Craig R. Abolin ,  H. Scott Wilkinson ,  Paul McGlynn ,  William K. McVicar

IPC: C07C233/43 ,  A61K31/167 ,  A61K31/4015 ,  A61K45/06 ,  C07C231/18

CPC classification number: C07C233/43 ,  A61K9/0075 ,  A61K9/008 ,  A61K31/167 ,  A61K31/4015 ,  A61K45/06 ,  C07B2200/13 ,  C07C231/18

Abstract: The compound of formula (I) is a water-stable, long acting β2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.

Abstract translation: 式（I）化合物是用作治疗与可逆性阻塞性气道疾病等相关的支气管收缩剂的支气管扩张剂的水稳定性长效β2-选择性肾上腺素受体激动剂。 公开了制备式（I）化合物以及相关中间体的方法。

公开(公告)号：US20150071969A1

公开(公告)日：2015-03-12

申请号：US14283754

申请日：2014-05-21

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Paul MCGLYNN ,  Roger Bakale ,  Craig Sturge

IPC: C07C215/60 ,  A61K9/00 ,  A61M15/00 ,  C07C59/255

CPC classification number: C07C215/60 ,  A61K9/008 ,  A61K9/14 ,  A61K31/205 ,  A61M15/002 ,  A61M15/009 ,  A61M2202/0484 ,  A61M2202/0488 ,  A61M2202/064 ,  C07B2200/07 ,  C07B2200/13 ,  C07C59/255 ,  C09K3/30

Abstract: Levalbuterol L-tartrate affords crystals possessing properties desirable for use in a metered dose inhaler.

Abstract translation: 莱伐珠特醇L-酒石酸盐提供具有期望用于计量剂量吸入器的性质的晶体。

公开(公告)号：US08969349B2

公开(公告)日：2015-03-03

申请号：US13700051

申请日：2011-05-26

Applicant: John Emmerson Campbell ,  Michael Charles Hewitt ,  Philip Jones ,  Linghong Xie

Inventor： John Emmerson Campbell ,  Michael Charles Hewitt ,  Philip Jones ,  Linghong Xie

IPC: A61K31/498 ,  C07D241/40 ,  C07D403/06 ,  C07D401/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/056 ,  C07D498/14 ,  C07D519/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06 ,  C07D498/04

CPC classification number: C07D498/06 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5383 ,  C07D233/58 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04 ,  C07D471/06 ,  C07D471/14 ,  C07D487/04 ,  C07D491/056 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00

Abstract: Provided herein are compounds of formula A-L-B, and pharmaceutically acceptable salts and stereoisomers thereof, wherein A is R1 and R2 together with the carbon atoms to which they are attached form a 1,2-phenylene ring optionally substituted with one or more R11; L is —C(R6)2—C(R6)2—; B is a heteroaromatic group defined herein; and -A1-A2- , A3, R11 and R6 are defined herein. Also disclosed are methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.

Abstract translation: 本文提供了式A-L-B的化合物及其药学上可接受的盐和立体异构体，其中A是R 1和R 2与它们所连接的碳原子一起形成任选被一个或多个R 11取代的1,2-亚苯基环; L是-C（R6）2 -C（R6）2-; B是本文定义的杂芳族基团; 并且-A1-A2-，A3，R11和R6在本文中定义。 还公开了它们的合成方法，包含该化合物的药物组合物及其使用方法。 在一个实施方案中，本文提供的化合物可用于治疗，预防和/或治疗各种疾病，例如CNS障碍和代谢紊乱，包括但不限于例如神经障碍，精神病，精神分裂症，肥胖症， 和糖尿病。

公开(公告)号：US08957114B2

公开(公告)日：2015-02-17

申请号：US13513170

申请日：2010-12-03

Applicant: Sharon M. Laughlin ,  Michael J. Sizensky ,  Surendra P. Singh ,  Harold Scott Wilkinson ,  Cai Gu Huang ,  Philip James Bonasia ,  Susan S. D'Souza

Inventor： Sharon M. Laughlin ,  Michael J. Sizensky ,  Surendra P. Singh ,  Harold Scott Wilkinson ,  Cai Gu Huang ,  Philip James Bonasia ,  Susan S. D'Souza

IPC: A01N33/02 ,  A61K31/135 ,  C07C211/00 ,  A61K9/20 ,  A61K9/48 ,  C07C211/42

CPC classification number: A61K31/135 ,  A61K9/2018 ,  A61K9/4858 ,  C07C211/42

Abstract: Provided herein are pharmaceutical compositions comprising transnorsertraline, salts and polymorphic forms of transnorsertraline, methods of making the compositions, and methods for their use for the treatment of CNS diseases, including depression.

Abstract translation: 本文提供的药物组合物包含过度心律，盐和多形态的跨屈曲胆碱，制备组合物的方法，及其用于治疗包括抑郁症在内的CNS疾病的方法。

公开(公告)号：US20150031709A1

公开(公告)日：2015-01-29

申请号：US14377673

申请日：2013-02-08

Applicant: Sunovion Pharmaceuticals, Inc.

Inventor： John Emmerson Campbell ,  Una Campbell ,  Taleen G. Hanania ,  Liming Shao

IPC: C07D409/04 ,  C07D409/14 ,  C07D491/048 ,  C07D405/04 ,  C07D495/04

CPC classification number: C07D409/04 ,  C07D405/04 ,  C07D409/14 ,  C07D491/048 ,  C07D495/04

Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

Abstract translation: 本文提供噻吩化合物，其合成方法，包含该化合物的药物组合物及其使用方法。 本文提供的化合物可用于治疗，预防和/或治疗各种神经障碍，包括但不限于精神病和精神分裂症。

公开(公告)号：US08877975B2

公开(公告)日：2014-11-04

申请号：US12688474

申请日：2010-01-15

Applicant: Liming Shao ,  Fengjiang Wang ,  Scott Christopher Malcolm ,  Michael Charles Hewitt ,  Larry R. Bush ,  Jianguo Ma ,  Mark A. Varney ,  Una Campbell ,  Sharon Rae Engel ,  Larry Wendell Hardy ,  Patrick Koch ,  John E. Campbell

Inventor： Liming Shao ,  Fengjiang Wang ,  Scott Christopher Malcolm ,  Michael Charles Hewitt ,  Larry R. Bush ,  Jianguo Ma ,  Mark A. Varney ,  Una Campbell ,  Sharon Rae Engel ,  Larry Wendell Hardy ,  Patrick Koch ,  John E. Campbell

IPC: C07C211/17 ,  A61K31/137 ,  C07C211/29 ,  C07C211/40 ,  C07C215/42 ,  C07C215/44 ,  C07C217/52 ,  C07C217/74 ,  C07C323/32 ,  C07D207/06 ,  C07D207/08 ,  C07D211/14 ,  C07D265/14 ,  C07D277/28 ,  C07D295/06 ,  C07D307/52 ,  C07D317/58 ,  C07D317/72 ,  C07D319/06 ,  C07D333/20 ,  C07D491/056

CPC classification number: C07D333/20 ,  C07C211/17 ,  C07C211/29 ,  C07C211/40 ,  C07C215/42 ,  C07C215/44 ,  C07C217/52 ,  C07C217/74 ,  C07C323/32 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/08 ,  C07D207/06 ,  C07D207/08 ,  C07D211/14 ,  C07D211/16 ,  C07D265/14 ,  C07D277/28 ,  C07D295/06 ,  C07D307/52 ,  C07D317/58 ,  C07D317/72 ,  C07D319/06 ,  C07D491/056

Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

Abstract translation: 本发明涉及新的环己胺衍生物及其在治疗和/或预防中枢神经系统（CNS）障碍如抑郁，焦虑，精神分裂症和睡眠障碍中的用途及其合成方法。 本发明还涉及含有本发明化合物的药物组合物，以及抑制内源性单胺如从突触间隙中再摄取多巴胺，5-羟色胺和去甲肾上腺素以及调节一种或多种单胺转运蛋白的方法。