公开(公告)号：US09133117B2

公开(公告)日：2015-09-15

申请号：US14062626

申请日：2013-10-24

Applicant: SUNOVION PHARMACEUTICALS INC.

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

IPC: C07D209/44 ,  C07D205/00 ,  C07D217/00 ,  C07D217/10 ,  C07D209/52 ,  C07D209/08

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 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 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。 还提供了含有这些化合物的药物制剂。

公开(公告)号：US09114086B2

公开(公告)日：2015-08-25

申请号：US14243146

申请日：2014-04-02

Applicant: Sunovion Pharmaceuticals Inc.

Inventor： Richard Hsia ,  Cai Gu Huang ,  Konstantinos E. Saranteas ,  Tushar K. Misra ,  Philip J. Bonasia, Jr.

IPC: A61K9/20 ,  A61K9/30 ,  A61K31/4985 ,  A61K9/28

CPC classification number: A61K9/2866 ,  A61K31/4985 ,  Y10T436/147777

Abstract: Coated tablets 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. The tablets minimize the perceived bitterness of the medicament. A method for analyzing instantaneous dissolution of sub-microgram quantities of core material is also disclosed.

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）。 片剂使药物的感觉到的苦味最小化。 还公开了一种用于分析亚微米数量的芯材料的瞬时溶解的方法。

公开(公告)号：US09072700B2

公开(公告)日：2015-07-07

申请号：US14139339

申请日：2013-12-23

Applicant: Sunovion Pharmaceuticals Inc.

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

IPC: A61K31/135 ,  A61K31/137 ,  A61K31/277 ,  C07C213/00 ,  C07C213/02 ,  C07C215/64 ,  C07C217/74

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：US20140271858A1

公开(公告)日：2014-09-18

申请号：US14243146

申请日：2014-04-02

Applicant: Sunovion Pharmaceuticals Inc.

Inventor： Richard HSIA ,  Cai Gu HUANG ,  Konstantinos E. SARANTEAS ,  Tushar K. MISRA ,  Philip J. BONASIA, JR.

IPC: A61K9/28 ,  A61K31/4985

CPC classification number: A61K9/2866 ,  A61K31/4985 ,  Y10T436/147777

Abstract: Coated tablets 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. The tablets minimize the perceived bitterness of the medicament. A method for analyzing instantaneous dissolution of sub-microgram quantities of core material is also disclosed.

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）。 片剂使药物的感觉到的苦味最小化。 还公开了一种用于分析亚微米数量的芯材料的瞬时溶解的方法。

公开(公告)号：US08772301B2

公开(公告)日：2014-07-08

申请号：US12972293

申请日：2010-12-17

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

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

IPC: A61K31/519 ,  A61K31/5365 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

CPC classification number: C07D239/88 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D413/04 ,  C07D417/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/20 ,  C07D487/04 ,  C07D487/08 ,  C07D487/20 ,  C07D491/20 ,  C07D498/04

Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

Abstract translation: 本文提供的化合物及其合成方法。 本文所述的化合物可用于治疗，预防和/或治疗各种疾病，例如神经障碍，神经变性疾病，神经精神障碍，认知障碍，学习或记忆障碍，胃肠道疾病，下尿路障碍和癌症 。 本文所述的化合物调节代谢型谷氨酸受体5（mGluR5）在中枢神经系统或周边的活性。 本文还提供了含有化合物及其使用方法的药物制剂。

公开(公告)号：US08710245B2

公开(公告)日：2014-04-29

申请号：US13513176

申请日：2010-12-03

Applicant: Liming Shao ,  John Emmerson Campbell ,  Michael Charles Hewitt ,  Una Campbell ,  Taleen G. Hanania

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

IPC: C07D495/02 ,  A61K31/38 ,  C07D495/04

CPC classification number: A61K31/381 ,  A61K31/435 ,  A61K31/55 ,  A61K45/06 ,  C07D277/60 ,  C07D333/54 ,  C07D333/76 ,  C07D333/78 ,  C07D495/04 ,  C07D495/20

Abstract: Provided herein are multicyclic 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: 本文提供多环化合物，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：US08658700B2

公开(公告)日：2014-02-25

申请号：US13693489

申请日：2012-12-04

Applicant: Sunovion Pharmaceuticals Inc.

Inventor： Thomas Jerussi ,  Qun Kevin Fang ,  Mark G. Currie

IPC: A61K31/135 ,  C07C211/42

CPC classification number: A61K31/135 ,  C07B2200/07 ,  C07C211/42 ,  C07C2602/10

Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

Abstract translation: 用（1R，4S） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺处理CNS病症; 和（1S，4R） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺。 还公开了制备4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺的方法。 该方法包括制备N- [4-（3,4-二氯苯基）-1,2,3,4-四氢萘-1-基]甲酰胺的全部四种异构体，它们也是有用的。

公开(公告)号：US20130065904A1

公开(公告)日：2013-03-14

申请号：US13673076

申请日：2012-11-09

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Judy CARON ,  Thomas WESSEL ,  Karim LALJI ,  Mark VARNEY ,  Roger P. BAKALE ,  Surendra P. SINGH ,  H. Scott WILKINSON ,  Xiping SU ,  Zhengxu HAN ,  Stefan G. KOENIG

IPC: A61K31/4985 ,  A61P25/00 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P15/12 ,  A61P25/22

CPC classification number: A61K31/4985 ,  A61K31/135 ,  C07C211/42 ,  C07C2602/10 ,  A61K2300/00

Abstract: One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine or trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.

Abstract translation: 本发明的一个方面涉及含有两种或更多种活性剂的药物组合物，所述活性剂当一起用于治疗例如更年期，情绪障碍，焦虑障碍或认知障碍时。 药物组合物的第一组分是镇静剂佐佐匹克。 药物组合物的第二组分是反式4-（3,4-二氯苯基）-1,2,3,4-四氢-N-甲基-1-萘胺或反式4-（3,4-二氯苯基） 2,3,4-四氢-1-萘胺。 本发明还涉及治疗绝经，围绝经期，情绪障碍，焦虑障碍和认知障碍的方法。

公开(公告)号：US08269005B2

公开(公告)日：2012-09-18

申请号：US12498756

申请日：2009-07-07

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

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

IPC: C07D495/00

CPC classification number: C07D487/04

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：US20120220597A1

公开(公告)日：2012-08-30

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: A61K31/4985 ,  A61P25/20

CPC classification number: C07D487/04 ,  C07C59/245

Abstract: A novel L-malate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is 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）。