公开(公告)号：US09499476B2

公开(公告)日：2016-11-22

申请号：US14692843

申请日：2015-04-22

Applicant: SUNOVION PHARMACEUTICALS INC.

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

IPC: C07C233/43 ,  A61K9/00 ,  A61K45/06 ,  A61K31/167 ,  C07C231/18 ,  A61K31/4015

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.

公开(公告)号：US09498452B2

公开(公告)日：2016-11-22

申请号：US14727260

申请日：2015-06-01

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-naphthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine 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：US09351954B2

公开(公告)日：2016-05-31

申请号：US14205859

申请日：2014-03-12

Applicant: Sunovion Pharmaceuticals Inc. ,  PGI Drug Discovery LLC.

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

IPC: C07D495/02 ,  C07D233/00 ,  C07D403/02 ,  C07D403/14 ,  C07D231/00 ,  C07D487/00 ,  C07D487/02 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  A61K31/415 ,  A61K31/40 ,  A61K31/48 ,  A61K31/381 ,  C07D277/60 ,  C07D333/54 ,  C07D333/76 ,  C07D333/78 ,  C07D495/04 ,  C07D495/20 ,  A61K31/435 ,  A61K31/55 ,  A61K45/06

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. For example, disclosed herein are compounds having formula (IIa) shown below, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein the variables are defined herein. 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。 例如，本文公开的是具有下面所示的式（IIa）的化合物或其药学上可接受的盐或立体异构体，其中变量在本文中定义。 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：US20150225334A1

公开(公告)日：2015-08-13

申请号：US14692843

申请日：2015-04-22

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Craig R. ABOLIN ,  H. Scott WILKINSON ,  Paul MCGLYNN ,  William K. MCVICAR

IPC: C07C233/43 ,  A61K9/00 ,  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：US20150209311A1

公开(公告)日：2015-07-30

申请号：US14502197

申请日：2014-09-30

Applicant: Sunovion Pharmaceuticals Inc.

Inventor： Timothy J. Barberich

IPC: A61K31/167 ,  A61K31/47 ,  A61K45/06 ,  A61K31/404

CPC classification number: A61K31/167 ,  A61K31/404 ,  A61K31/47 ,  A61K45/06 ,  C07C2601/16 ,  A61K2300/00

Abstract: This invention related to methods of treating, preventing and managing various pulmonary diseases or disorders using stereomerically pure (R,R)-formoterol in combination with other pharmacological agents such as leukotriene inhibitors and neurokinin receptor antagonists. Pharmaceutical compositions comprising (R,R)-formoterol and other pharmacological agents are also disclosed.

Abstract translation: 本发明涉及使用立体纯的（R，R） - 福莫特罗与其他药理学试剂如白三烯抑制剂和神经激肽受体拮抗剂组合治疗，预防和治疗各种肺部疾病或病症的方法。 还公开了包含（R，R） - 福莫特罗和其他药理学试剂的药物组合物。

公开(公告)号：US20140349992A1

公开(公告)日：2014-11-27

申请号：US14299364

申请日：2014-06-09

Applicant: Sunovion Pharmaceuticals Inc.

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

IPC: C07D239/88 ,  C07D405/06 ,  C07D413/04 ,  C07D401/14 ,  C07D471/14 ,  C07D471/20 ,  C07D487/08 ,  C07D498/04 ,  C07D491/20 ,  C07D417/06 ,  C07D487/04

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：US08889685B2

公开(公告)日：2014-11-18

申请号：US13928571

申请日：2013-06-27

Applicant: Sunovion Pharmaceuticals Inc.

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

IPC: A61K31/444 ,  A61K31/495 ,  A61K31/4985 ,  C07D213/61 ,  C07D295/182 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D487/04 ,  C07C57/145

Abstract: Maleate 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. The salts are useful for treating sleep disorders.

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）。 这些盐可用于治疗睡眠障碍。

公开(公告)号：US20140336218A1

公开(公告)日：2014-11-13

申请号：US14340736

申请日：2014-07-25

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Holly HUANG ,  Elizabeth B. GOODWIN ,  Kendyl M. SCHAEFER ,  John P. HANRAHAN ,  William T. ANDREWS ,  Paul MCGLYNN

IPC: A61K31/46 ,  A61K9/00 ,  A61K31/137

CPC classification number: A61K31/46 ,  A61K9/0078 ,  A61K9/008 ,  A61K31/137 ,  A61K31/16 ,  A61K31/439 ,  A61K2300/00

Abstract: Compositions and methods for the prevention and/or treatment of airway and/or respiratory disorders are provided. The compositions comprise arformoterol (the (R,R)-formoterol isomer) and tiotropium.

Abstract translation: 提供了预防和/或治疗气道和/或呼吸障碍的组合物和方法。 组合物包含阿霉素（（R，R） - 福莫特罗异构体）和噻托溴铵。

公开(公告)号：US20140256712A1

公开(公告)日：2014-09-11

申请号：US14205859

申请日：2014-03-12

Applicant: Psychogenics Inc. ,  Sunovion Pharmaceuticals Inc.

Inventor： Liming SHAO ,  John Emmerson CAMPBELL ,  Michael Charles HEWITT ,  Una CAMPBELL ,  Taleen G. HANANIA

IPC: C07D495/20 ,  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：US08765760B2

公开(公告)日：2014-07-01

申请号：US13347541

申请日：2012-01-10

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

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

IPC: A61K31/495 ,  C07D457/00 ,  C07D471/00 ,  C07D495/00 ,  C07D497/00

CPC classification number: C07D519/00 ,  A61K31/4375 ,  A61K31/4745 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04

Abstract: Provided herein are compounds of formula (I): A-L-B  (I) and pharmaceutically acceptable salts and stereoisomers thereof, wherein A is wherein X is (i) CR1 or N, or (ii) O or NR2, each Y is independently N or CR3, and each Z is independently N or C, wherein R1, R2 and R3 are defined in the specification; L is a linker, and B is a multicyclic ring; methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are inhibitors of phosphodiesterases and useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, e.g., neurological disorders, psychosis, schizophrenia, obesity and diabetes.

Abstract translation: 本文提供式（I）的化合物：其中A是其中X是（i）CR 1或N，或（ii）O或NR 2，其中每个Y独立地是N或CR 3 并且每个Z独立地为N或C，其中R1，R2和R3在说明书中定义; L为连接体，B为多环; 其合成方法，包含该化合物的药物组合物及其使用方法。 本文提供的化合物是磷酸二酯酶的抑制剂，并且可用于治疗，预防和/或治疗各种疾病，例如CNS障碍和代谢性疾病，例如神经障碍，精神病，精神分裂症，肥胖症和糖尿病。