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公开(公告)号：US11337971B2
公开(公告)日：2022-05-24
申请号：US17265150
申请日：2019-09-09
发明人： Amy Hauck Newman , Vivek Kumar , Anver Basha Shaik
IPC分类号： A61K31/496 , A61P25/36 , A61K31/485
摘要： Disclosed herein are novel methods of treating pain in a patient in need thereof by providing to the patient a selective dopamine D3 receptor antagonist/partial agonist which when used with an opioid analgesic, can mitigate the development of opioid dependence, by preventing the need for dose escalation while either maintaining the opioid analgesic effect or providing analgesia with a lower dose of the opioid. In addition, the D3 antagonists/partial agonists described herein may be used to augment the effectiveness of current Medication Assisted Treatment regimens (e.g. methadone or buprenorphine) for the treatment of opioid use disorders.
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2.发明授权公开(公告)号：US11299476B2
公开(公告)日：2022-04-12
申请号：US16084093
申请日：2017-03-08
发明人： Amy Hauck Newman , Vivek Kumar , Anver Basha Shaik
IPC分类号： C07D403/12 , A61P25/36 , C07D405/12
摘要： Disclosed herein novel dopamine D3 receptor selective antagonists/partial agonists compounds with high affinity and metabolic stability useful for the treatment of psychiatric and neurological disorders and as research and diagnostic tools. Also disclosed are methods of making the compounds.
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3.发明授权公开(公告)号：US11555013B2
公开(公告)日：2023-01-17
申请号：US17139583
申请日：2020-12-31
IPC分类号： A61K45/06 , C07C323/60 , A61K31/135 , C07C317/44 , C07C317/28 , C07C323/25 , C07D295/08 , C07D295/088 , C07D295/108 , C07D295/185
摘要： Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds.
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公开(公告)号：US20130202529A1
公开(公告)日：2013-08-08
申请号：US13739724
申请日：2013-01-11
发明人： Amy Hauck Newman , Mu-Fa Zou , Jonathan L. Katz
CPC分类号： A61K31/46 , A61K51/0455 , C07D451/08
摘要： Disclosed are benztropine analogs having the formula (I) in which Ar is a C6-C20 monocyclic aryl group or a C10-C20 bicyclic aryl group or a heteroaryl, heterocyclic, or arylheterocyclic group having 2 to 12 carbon atoms and one or more heteroatoms selected from the group consisting of N, O, S, P, and any combination thereof; m=1 to 5; n=1 to 3; and R1 to R4 are as described in the specification; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions and use thereof, e.g., in treating mental disorders.
摘要翻译： 公开了具有式（I）的苯并三嗪类似物，其中Ar是C6-C20单环芳基或C10-C20双环芳基或具有2至12个碳原子和一个或多个杂原子的杂芳基，杂环或芳基杂环基团 由N，O，S，P及其任何组合组成的组; m = 1〜5; n = 1〜3; R1至R4如说明书所述; 或其药学上可接受的盐或溶剂化物; 药物组合物及其用途，例如治疗精神障碍。
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公开(公告)号：US11365195B2
公开(公告)日：2022-06-21
申请号：US16762998
申请日：2018-11-12
IPC分类号： C07D471/10 , C07D211/58 , C07D241/04
摘要： Disclosed herein are a series of modafinil analogue compounds that bind with moderate to high affinity to the dopamine (DA) transporter (DAT) and several analogues also having affinity for the serotonin (5-HT) transporter (SERT) and/or sigma-1 receptor. Employing aminopiperidine, piperidineamino, spirobicyclodiaza, or substituted piperazine functional groups, desired dopamine transporter affinity has been retained along with improved metabolic stability over unsubstituted piperazine ring analogues. Importantly, these compounds have no predicted addictive liability. Also disclosed are methods for treating substance use disorders as well as other neuropsychiatric disorders such as ADHD, depression, narcolepsy, and cognitive impairment.
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6.发明授权公开(公告)号：US10590074B2
公开(公告)日：2020-03-17
申请号：US15830244
申请日：2017-12-04
IPC分类号： C07C323/60 , A61K45/06 , A61K31/135 , C07C317/44 , C07C317/28 , C07C323/25 , C07D295/08 , C07D295/088 , C07D295/108 , C07D295/185
摘要： Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds.
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7.发明授权公开(公告)号：US09862679B2
公开(公告)日：2018-01-09
申请号：US14772486
申请日：2014-03-07
IPC分类号： A61K31/495 , C07C323/60 , A61K45/06 , A61K31/135 , C07C317/44 , C07C317/28 , C07C323/25 , C07D295/08 , C07D295/088 , C07D295/108 , C07D295/185
CPC分类号： C07C323/60 , A61K31/135 , A61K45/06 , C07C317/28 , C07C317/44 , C07C323/25 , C07C2601/02 , C07D295/08 , C07D295/088 , C07D295/108 , C07D295/185 , A61K2300/00
摘要： Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds.
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