公开(公告)号：US20140073682A1

公开(公告)日：2014-03-13

申请号：US14078284

申请日：2013-11-12

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Liming SHAO ,  Jianguo MA

IPC: C07D207/08 ,  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.

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：US08669291B2

公开(公告)日：2014-03-11

申请号：US12131845

申请日：2008-06-02

Applicant: 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

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: A61K31/133 ,  A61K31/135 ,  C07C211/17

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：US08664441B2

公开(公告)日：2014-03-04

申请号：US13934996

申请日：2013-07-03

Applicant: Sunovion Pharmaceuticals Inc.

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

IPC: C07C233/05

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的长效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：US20140057990A1

公开(公告)日：2014-02-27

申请号：US13956765

申请日：2013-08-01

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Hang Zhao ,  Stefan G. Koenig ,  Charles P. Vandenbossche ,  Surendra Singh ,  Harold Scott Wilkinson ,  Roger P. Bakale

IPC: C07C231/14 ,  C07C209/50 ,  C07C211/42 ,  C07C231/12

CPC classification number: C07C231/14 ,  C07B43/06 ,  C07C209/50 ,  C07C209/62 ,  C07C211/42 ,  C07C231/12 ,  C07C249/08 ,  C07C2602/10

Abstract: This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.

Abstract translation: 本发明提供了将肟转化成烯酰胺的方便方法。 该方法不需要使用金属试剂。 因此，它产生所需化合物，而不伴随产生大量的金属废物。 酰胺是酰胺和胺的有用前体。 本发明提供了将前手性烯酰胺转化成相应的手性酰胺的方法。 在示例性方法中，通过使用手性氢化催化剂在氢化期间引入手性氨基中心。 在选择的实施方案中，本发明提供了制备包括1,2,3,4-四氢-N-烷基-1-萘胺或1,2,3,4-四氢-1-萘胺亚结构的酰胺和胺的方法。

公开(公告)号：US08642662B2

公开(公告)日：2014-02-04

申请号：US13481584

申请日：2012-05-25

Applicant: Thomas P. Jerussi ,  Chrisantha H. Senanayake ,  Nandkumar N. Bhongle

Inventor： Thomas P. Jerussi ,  Chrisantha H. Senanayake ,  Nandkumar N. Bhongle

IPC: A61K31/135

CPC classification number: C07C217/74 ,  A61K31/137 ,  A61K31/277 ,  C07B2200/07 ,  C07C213/00 ,  C07C213/02 ,  C07C215/64 ,  C07C2601/14

Abstract: Methods of preparing, and compositions comprising, derivatives of (−)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.

Abstract translation: 公开了制备方法和包含（ - ） - 文拉法辛的衍生物的组合物。 还公开了治疗和预防疾病和病症的方法，包括但不限于情感障碍如抑郁，双相和躁狂症，注意力缺陷障碍，具有多动症的注意缺陷障碍，帕金森病，癫痫，脑功能障碍，肥胖症和 体重增加，失禁，痴呆和相关疾病。

公开(公告)号：US08541416B2

公开(公告)日：2013-09-24

申请号：US13470003

申请日：2012-05-11

Applicant: H. Scott Wilkinson ,  Richard Hsia ,  Tushar Misra ,  Kostas Saranteas ,  Patrick Mousaw

Inventor： H. Scott Wilkinson ,  Richard Hsia ,  Tushar Misra ,  Kostas Saranteas ,  Patrick Mousaw

IPC: A61K31/495

CPC classification number: C07D487/04 ,  C07C59/245

Abstract: L-malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl) carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.

Abstract translation: （6-（5-氯-2-吡啶基）-5 - [（4-甲基-1-哌嗪基）羰氧基] -7-氧代-6,7-二氢-5H-吡咯并[3,4 -b]吡嗪）。

公开(公告)号：US08497278B2

公开(公告)日：2013-07-30

申请号：US12993679

申请日：2009-05-19

Applicant: Qun Kevin Fang ,  Frank Xinhe Wu ,  Paul T. Grover ,  Seth C. Hopkins ,  Una Campbell ,  Milan Chytil ,  Kerry L. Spear

Inventor： Qun Kevin Fang ,  Frank Xinhe Wu ,  Paul T. Grover ,  Seth C. Hopkins ,  Una Campbell ,  Milan Chytil ,  Kerry L. Spear

IPC: C07D249/08 ,  C07D271/06 ,  C07D403/12 ,  A61K31/506 ,  A61K31/4245

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed. Many of the compounds disclosed herein may be represented by the following generic formula: in which Y is a direct bond or heteroatom and A3 is usually a nitrogenous heterocycle.

Abstract translation: 公开了咪唑并[1,2-a]吡啶。 本发明的化合物是有用的治疗剂，并且它们包括在药物制剂中并用于治疗方法。 本文公开的许多化合物可以由以下通式表示：其中Y是直接键或杂原子，并且A3通常是含氮杂环。

公开(公告)号：US20130158003A1

公开(公告)日：2013-06-20

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: C07D403/06 ,  C07D409/06 ,  C07D405/14 ,  C07D409/14 ,  C07D498/04 ,  C07D417/06 ,  C07D413/06 ,  C07D487/04 ,  C07D471/14 ,  C07D471/04 ,  C07D401/14

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 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：US08445470B2

公开(公告)日：2013-05-21

申请号：US12277004

申请日：2008-11-24

Applicant: Mark G. Currie ,  Steve Jones ,  Paul Grover ,  Chris H. Senanayake ,  Q. Kevin Fang

Inventor： Mark G. Currie ,  Steve Jones ,  Paul Grover ,  Chris H. Senanayake ,  Q. Kevin Fang

IPC: A61K31/58 ,  A61K31/573

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.

Abstract translation: 含有β2肾上腺素能激动剂与下式的碳酸酯和氨基甲酸酯组合的组合物。 并结合相关类固醇碳酸酯和氨基甲酸酯。 该组合物可用于治疗支气管痉挛，用于诱发支气管扩张和治疗鼻炎，哮喘和慢性阻塞性肺疾病（COPD）和炎性疾病，特别是通过吸入治疗。

公开(公告)号：US20130028845A1

公开(公告)日：2013-01-31

申请号：US13633801

申请日：2012-10-02

Applicant: Paul McGlynn ,  Roger Bakale ,  Craig Sturge

Inventor： Paul McGlynn ,  Roger Bakale ,  Craig Sturge

IPC: A61K31/137 ,  A61P11/06 ,  A61P11/00 ,  A61K9/12

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.