公开(公告)号：US09856238B2

公开(公告)日：2018-01-02

申请号：US15041852

申请日：2016-02-11

Applicant: Sunovion Pharmaceuticals Inc. ,  PGI Drug Discovery LLC

Inventor： Linghong Xie ,  Philip Glyn Jones ,  Kerry L. Spear ,  Noel Aaron Powell ,  Taleen G. Hanania ,  Vadim Alexandrov

IPC: C07D405/04 ,  C07D413/14 ,  C07D405/14 ,  C07D493/04 ,  C07D413/04

CPC classification number: C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D493/04

Abstract: Disclosed are compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, Ra, R1, R2, R3, R4, R6, w and n1 are defined and described herein; compositions thereof; and methods of use thereof. These compounds are useful for treating a variety of neurological and psychiatric disorders, such as those described herein.

公开(公告)号：US09708331B2

公开(公告)日：2017-07-18

申请号：US15013741

申请日：2016-02-02

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Michele L. R. Heffernan ,  Larry Wendell Hardy ,  Frank Xinhe Wu ,  Lakshmi D. Saraswat ,  Kerry L. Spear

IPC: C07D487/14 ,  C07D487/04 ,  C07D471/04 ,  C07D471/14 ,  C07D471/20 ,  C07D487/18 ,  C07D491/147 ,  C07D491/20 ,  C07D491/22 ,  C07D498/04 ,  C07D487/10

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D471/14 ,  C07D471/20 ,  C07D487/10 ,  C07D487/14 ,  C07D487/18 ,  C07D491/147 ,  C07D491/20 ,  C07D491/22 ,  C07D498/04

Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.

公开(公告)号：US09669021B2

公开(公告)日：2017-06-06

申请号：US14971532

申请日：2015-12-16

Applicant: Sunovion Pharmaceuticals Inc.

Inventor： Anthony John Giovinazzo ,  David Bruce Hedden ,  Marc L. De Somer ,  Nathan John Bryson

IPC: A61F13/00 ,  A61K31/485 ,  A61K9/00 ,  A61K9/06 ,  A61K9/20 ,  A61K9/70 ,  A61K31/473 ,  A61K47/02 ,  A61K47/10 ,  A61K47/18

CPC classification number: A61K31/485 ,  A61K9/0056 ,  A61K9/006 ,  A61K9/06 ,  A61K9/2086 ,  A61K9/7007 ,  A61K31/473 ,  A61K47/02 ,  A61K47/10 ,  A61K47/183 ,  Y10T428/2982

Abstract: Disclosed are methods of treating Parkinson's disease by (i) providing a pharmaceutical composition in unit dosage form that is a film having a first portion including apomorphine particles containing an acid addition salt of apomorphine and a second portion containing a pH neutralizing agent, where the film contains the acid addition salt of apomorphine in an amount effective to treat Parkinson's disease, and (ii) administering the film by placing the film sublingually in the mouth of the subject and contacting sublingual mucosal tissue with the film.

公开(公告)号：US09669020B2

公开(公告)日：2017-06-06

申请号：US14963971

申请日：2015-12-09

Applicant: Sunovion Pharmaceuticals Inc.

Inventor： Anthony John Giovinazzo ,  David Bruce Hedden ,  Marc L. De Somer ,  Nathan John Bryson

IPC: A61F13/00 ,  A61K31/485 ,  A61K9/00 ,  A61K9/06 ,  A61K9/20 ,  A61K9/70 ,  A61K31/473 ,  A61K47/02 ,  A61K47/10 ,  A61K47/18

CPC classification number: A61K31/485 ,  A61K9/0056 ,  A61K9/006 ,  A61K9/06 ,  A61K9/2086 ,  A61K9/7007 ,  A61K31/473 ,  A61K47/02 ,  A61K47/10 ,  A61K47/183 ,  Y10T428/2982

Abstract: The invention features mucoadhesive sublingual films containing a pH neutralizing agent and apomorphine particles containing an acid addition salt of apomorphine. The pH neutralizing agent in these films can be sodium phosphate monobasic, sodium phosphate dibasic, sodium phosphate tribasic, potassium phosphate monobasic, potassium phosphate dibasic, potassium phosphate tribasic, or a mixture thereof.

公开(公告)号：US09056830B2

公开(公告)日：2015-06-16

申请号：US14078284

申请日：2013-11-12

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Liming Shao ,  Jianguo Ma

IPC: C07D207/06 ,  C07D207/08 ,  C07D405/04 ,  A61K31/4025 ,  A61K31/40 ,  C07D207/12

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.

Abstract translation: 在各种实施方案中，本发明提供环烷基吡咯烷化合物及其用于治疗和/或预防各种疾病，病症和综合征的方法，包括中枢神经系统（CNS）障碍，例如抑郁症，焦虑症，精神分裂症和睡眠障碍 以及它们的合成方法。 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。

公开(公告)号：US08877755B2

公开(公告)日：2014-11-04

申请号：US12541686

申请日：2009-08-14

Applicant: Timothy J. Barberich

Inventor： Timothy J. Barberich

IPC: A61K31/4985 ,  A61P25/14 ,  A61K31/137 ,  A61K45/06 ,  A61K31/425

CPC classification number: A61K45/06 ,  A61K31/137 ,  A61K31/425 ,  A61K31/4985 ,  A61K2300/00

Abstract: The present invention generally relates to pharmaceutical compositions comprising a dopamine agonist and sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine; and the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. The pharmaceutical compositions of the invention are useful in the treatment of restless-leg syndrome and periodic-limb-movement disorder, as well as various sleep disorders. In addition, the present invention relates to a method of treating a patient suffering from restless-leg syndrome, periodic-limb-movement disorder, a sleep abnormality, or insomnia, comprising coadministering a therapeutically effective amount of a dopamine agonist and a therapeutically effective amount of a sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine; and the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone.

Abstract translation: 本发明一般涉及包含多巴胺激动剂和镇静剂的药物组合物。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明。 在优选的实施方案中，镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基佐匹克隆。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明; 并且镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基佐匹克隆。 本发明的药物组合物可用于治疗不宁腿综合征和周期性肢体运动障碍以及各种睡眠障碍。 此外，本发明涉及治疗患有不宁腿综合征，周期性肢体运动障碍，睡眠异常或失眠的患者的方法，包括共同施用治疗有效量的多巴胺激动剂和治疗有效量 的镇静剂。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明。 在优选的实施方案中，镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基佐匹克隆。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明; 并且镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基佐匹克隆。

公开(公告)号：US20140135300A1

公开(公告)日：2014-05-15

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 ,  A61K31/4015 ,  A61K45/06 ,  A61K31/167

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：US20140121282A1

公开(公告)日：2014-05-01

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 ,  C07C217/76

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 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一元胺如多巴胺，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：US08592608B2

公开(公告)日：2013-11-26

申请号：US13139967

申请日：2009-12-15

Applicant: Liming Shao ,  Fengjiang Wang ,  Scott C. Malcolm ,  Michael C. Hewitt

Inventor： Liming Shao ,  Fengjiang Wang ,  Scott C. Malcolm ,  Michael C. Hewitt

IPC: C07D209/44 ,  C07D205/00 ,  C07D217/00 ,  C07D217/10 ,  A61K31/40 ,  A61K31/397 ,  A61K31/47

CPC classification number: C07D209/44 ,  A61K31/4035 ,  C07D209/08 ,  C07D209/52

Abstract: Provided herein are bicyclic compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders. Compounds provided herein inhibit uptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations containing the compounds are also provided.

Abstract translation: 本文提供的是双环化合物及其合成方法。 本文提供的化合物可用于治疗，预防和/或管理各种神经障碍。 本文提供的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吸收（例如，从突触裂缝）并调节一种或多种单胺转运蛋白。 还提供了含有这些化合物的药物制剂。

公开(公告)号：US20130244988A1

公开(公告)日：2013-09-19

申请号：US13867674

申请日：2013-04-22

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Mark G. CURRIE ,  Steve JONES ,  Paul GROVER ,  Chris H. SENANAYAKE ,  Q. Kevin FANG

IPC: A61K45/06 ,  A61K31/137 ,  A61K31/58

CPC classification number: A61K45/06 ,  A61K31/137 ,  A61K31/56 ,  A61K31/573 ,  A61K31/58 ,  Y10S514/87 ,  A61K2300/00

Abstract: Compositions containing β2 adrenergic agonists in combination with carbonates and carbamates of the formula. and in combination with related steroid carbonates and carbamates are disclosed. The compositions are useful for treating bronchospasm, for inducing bronchodilation and for treating rhinitis, asthma, and chronic obstructive pulmonary disease (COPD) and inflammatory diseases, particularly by inhalation.