公开(公告)号：US10328036B2

公开(公告)日：2019-06-25

申请号：US15873540

申请日：2018-01-17

Applicant: SUNOVION PHARMACEUTICALS INC.

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

IPC: A61K31/135 ,  C07C211/42

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.

公开(公告)号：US20190055204A1

公开(公告)日：2019-02-21

申请号：US16107385

申请日：2018-08-21

Applicant: SUNOVION PHARMACEUTICALS INC.

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

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

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.

公开(公告)号：US10189825B2

公开(公告)日：2019-01-29

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

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.

公开(公告)号：US10011559B2

公开(公告)日：2018-07-03

申请号：US15498726

申请日：2017-04-27

Applicant: SUNOVION PHARMACEUTICALS INC.

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

IPC: C07C231/14 ,  C07C249/08 ,  C07C209/62 ,  C07C231/12 ,  C07C209/50 ,  C07C211/42 ,  C07B43/06

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.

公开(公告)号：US09907764B2

公开(公告)日：2018-03-06

申请号：US15299186

申请日：2016-10-20

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.

公开(公告)号：US20180057506A1

公开(公告)日：2018-03-01

申请号：US15666719

申请日：2017-08-02

Applicant: Sunovion Pharmaceuticals Inc. ,  PGI Drug Discovery LLC

Inventor： Milan CHYTIL ,  Sharon Engel ,  Taleen G. HANANIA ,  Vadim ALEXANDROV ,  Emer LEAHY

IPC: C07D498/04 ,  C07D498/22 ,  C07D498/14 ,  C07D498/20

CPC classification number: C07D498/04 ,  C07D231/56 ,  C07D498/14 ,  C07D498/20 ,  C07D498/22

Abstract: Disclosed are compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein Ring B, A1, A2, 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：US20170157067A1

公开(公告)日：2017-06-08

申请号：US15299186

申请日：2016-10-20

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Thomas JERUSSI ,  Qun Kevin FANG ,  Mark G. CURRIE

IPC: A61K31/135

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.

公开(公告)号：US09669019B2

公开(公告)日：2017-06-06

申请号：US14963910

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: Disclosed are sublingual formulations of apomorphine in unit dosage form formulated for sublingual administration, where the unit dosage form is a mucoadhesive film containing a pH neutralizing agent and apomorphine particles containing an acid addition salt of apomorphine, and where the mucoadhesive film is formed by the steps of: (i) combining a film-forming mucoadhesive polymer, apomorphine particles comprising an acid addition salt of apomorphine, and a solvent to form a mixture; and (ii) pouring the mixture onto a surface and evaporating some of the solvent to form a first film comprising the apomorphine particles, where the steps further include contacting or impregnating the first film or mixture with a pH neutralizing agent to produce the mucoadhesive film containing the apomorphine particles and the pH neutralizing agent.

公开(公告)号：US09669018B2

公开(公告)日：2017-06-06

申请号：US14963835

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: Disclosed are methods of preparing a pharmaceutical composition that is a mucoadhesive film by: (i) combining a film-forming mucoadhesive polymer, apomorphine particles containing an acid addition salt of apomorphine, and a solvent to form a mixture; and (ii) pouring the mixture onto a surface and evaporating some of the solvent to form an intermediate film including the apomorphine particles; where the method further includes contacting or impregnating the intermediate film or mixture with a pH neutralizing agent to produce the mucoadhesive film containing the apomorphine particles and the pH neutralizing agent.

公开(公告)号：US09580409B2

公开(公告)日：2017-02-28

申请号：US14352294

申请日：2012-11-07

Applicant: Sunovion Pharmaceuticals Inc.

Inventor： Scott Malcolm ,  Carrie Bowen ,  Laurence Melnick ,  Linghong Xie

IPC: C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D487/04 ,  C07D487/14 ,  C07D498/04 ,  C07D471/04 ,  C07D405/14 ,  C07D487/10 ,  C07D491/10 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/501 ,  A61K31/551 ,  A61K31/553

CPC classification number: C07D403/04 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/501 ,  A61K31/551 ,  A61K31/553 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D487/14 ,  C07D491/10 ,  C07D498/04

Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., μ-opioid receptor) 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。 本文提供的化合物可用于治疗，预防和/或治疗各种疾病，例如疼痛，神经障碍，精神疾病和神经肌肉疾病。 本文提供的化合物调节中枢神经系统或周围的阿片受体（例如，μ-阿片受体）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。