公开(公告)号：US09062001B2

公开(公告)日：2015-06-23

申请号：US14266048

申请日：2014-04-30

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Sepehr Sarshar

IPC分类号： C07D211/72 ,  A61K31/44 ,  A61K38/36 ,  C07K14/75 ,  C07K14/475 ,  A61K38/39 ,  C07D213/64 ,  A61K31/4418 ,  A61K45/06 ,  C07B59/00

CPC分类号： A61K31/4418 ,  A61K45/06 ,  C07B59/002 ,  C07D213/64

摘要： Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

公开(公告)号：US20140107040A1

公开(公告)日：2014-04-17

申请号：US14132528

申请日：2013-12-18

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Sepehr Sarshar

IPC分类号： C07D213/64 ,  A61K45/06 ,  C07B59/00 ,  A61K31/4418

CPC分类号： A61K31/4418 ,  A61K45/06 ,  C07B59/002 ,  C07D213/64

摘要： Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

摘要翻译： 本文公开了取代的N-芳基吡啶酮纤维化抑制剂和/或式I的胶原浸润调节剂，其制备方法，其药物组合物及其使用方法。

公开(公告)号：US08680123B1

公开(公告)日：2014-03-25

申请号：US13663188

申请日：2012-10-29

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Sepehr Sarshar

IPC分类号： A61K31/44 ,  A61K38/36 ,  C07K14/75 ,  C07K14/475 ,  A61K38/39

CPC分类号： A61K31/4418 ,  A61K45/06 ,  C07B59/002 ,  C07D213/64

摘要： Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

摘要翻译： 本文公开了取代的N-芳基吡啶酮纤维化抑制剂和/或式I的胶原浸润调节剂，其制备方法，其药物组合物及其使用方法。

公开(公告)号：US20210101863A1

公开(公告)日：2021-04-08

申请号：US16999367

申请日：2020-08-21

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Sepehr Sarshar ,  Soon Hyung Woo

IPC分类号： C07C211/64 ,  C07B59/00 ,  C07C215/64 ,  C07C217/74 ,  C07D265/16

摘要： Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, attention deficit hyperactivity disorder, fibromyalgia, irritable bowel syndrome, and/or premature ejaculation are described.

公开(公告)号：US20200000794A1

公开(公告)日：2020-01-02

申请号：US16568666

申请日：2019-09-12

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Manouchehr Shahbaz ,  Chengzhi Zhang

IPC分类号： A61K31/473 ,  C07D471/04 ,  C07D455/06 ,  A61K45/06 ,  C07C217/60 ,  C07C233/18 ,  C07C291/04 ,  C07D217/02 ,  C07D221/06

摘要： The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.

公开(公告)号：US20180256517A1

公开(公告)日：2018-09-13

申请号：US15975570

申请日：2018-05-09

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Sepehr Sarshar

IPC分类号： A61K31/137 ,  A61K45/06 ,  C07B59/00 ,  C07C255/37 ,  C07C217/74 ,  C07C65/21 ,  C07C235/34

CPC分类号： A61K31/137 ,  A61K45/06 ,  C07B59/001 ,  C07B2200/05 ,  C07C65/21 ,  C07C217/74 ,  C07C235/34 ,  C07C255/37 ,  C07C2601/14

摘要： Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and/or premature ejaculation are described.

公开(公告)号：US20170246159A1

公开(公告)日：2017-08-31

申请号：US15597733

申请日：2017-05-17

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Manouchehr Shahbaz ,  Chengzhi Zhang

IPC分类号： A61K31/473 ,  C07D455/06 ,  A61K45/06 ,  C07C217/60 ,  C07C233/18 ,  C07C291/04 ,  C07D217/02 ,  C07D471/04 ,  C07D221/06

CPC分类号： A61K31/473 ,  A61K45/06 ,  C07C217/60 ,  C07C233/18 ,  C07C291/04 ,  C07D217/02 ,  C07D221/06 ,  C07D455/06 ,  C07D471/04

摘要： The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.

公开(公告)号：US20160361275A1

公开(公告)日：2016-12-15

申请号：US15244575

申请日：2016-08-23

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Sepehr Sarshar

IPC分类号： A61K31/137

CPC分类号： A61K31/137 ,  A61K45/06 ,  C07B59/001 ,  C07B2200/05 ,  C07C65/21 ,  C07C217/74 ,  C07C235/34 ,  C07C255/37 ,  C07C2601/14

摘要： Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and/or premature ejaculation are described.

公开(公告)号：US09504677B2

公开(公告)日：2016-11-29

申请号：US14718993

申请日：2015-05-21

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Sepehr Sarshar

IPC分类号： A01N43/40 ,  A61K31/44 ,  C07D211/72 ,  A61K31/4418 ,  C07D213/64 ,  A61K45/06 ,  C07B59/00

CPC分类号： A61K31/4418 ,  A61K45/06 ,  C07B59/002 ,  C07D213/64

摘要： Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

公开(公告)号：US20160318847A1

公开(公告)日：2016-11-03

申请号：US15205491

申请日：2016-07-08

申请人： Auspex Pharmaceuticals, Inc.

发明人： Thomas G. Gant ,  Sepehr Sarshar

IPC分类号： C07C217/74 ,  A61K45/06 ,  C07B59/00 ,  A61K31/137

CPC分类号： A61K31/137 ,  A61K45/06 ,  C07B59/001 ,  C07B2200/05 ,  C07C65/21 ,  C07C217/74 ,  C07C235/34 ,  C07C255/37 ,  C07C2601/14

摘要： Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and/or premature ejaculation are described.