公开(公告)号：US09150581B2

公开(公告)日：2015-10-06

申请号：US14368111

申请日：2012-12-26

Applicant: RESEARCH TRIANGLE INSTITUTE ,  THE REGENTS OF THE UNIVERSITY OF MICHIGAN ,  VIRGINIA COMMONWEALTH UNIVERSITY

Inventor： Frank Ivy Carroll ,  Pauline Wanjiku Ondachi ,  Hernan A. Navarro ,  M. Imad Damaj ,  James H. Woods ,  Emily M. Jutkiewicz

IPC: C07D487/08

CPC classification number: C07D487/08

Abstract: Compounds and compositions for promoting smoking cessation or decreasing tobacco use or nicotine addiction are provided. The compounds are 2′-fluoro-3′-(substituted phenyl) deschloroepibatidine analogs. The compounds have been found to modulate neuronal nicotine acetylcholine receptors and are useful in methods for the treatment of conditions or disorders influenced by the modulation of neuronal nicotinic acetylcholine receptors.

Abstract translation: 提供了用于促进戒烟或减少烟草使用或尼古丁成瘾的化合物和组合物。 这些化合物是2'-氟-3' - （取代苯基）脱氯替巴替坦类似物。 已经发现这些化合物调节神经元尼古丁乙酰胆碱受体，并且可用于治疗受神经元烟碱乙酰胆碱受体调节影响的病症或障碍的方法。

公开(公告)号：US09750738B2

公开(公告)日：2017-09-05

申请号：US14968258

申请日：2015-12-14

Applicant: RESEARCH TRIANGLE INSTITUTE

Inventor： Frank Ivy Carroll ,  Juan P. Cueva ,  James B. Thomas ,  S. Wayne Mascarella ,  Scott P. Runyon

IPC: A61K31/495 ,  A61K31/496 ,  C07D241/04 ,  C07D401/12 ,  C07D295/096

CPC classification number: A61K31/495 ,  A61K31/496 ,  C07D241/04 ,  C07D295/096 ,  C07D401/12

Abstract: Provided are opioid receptor antagonists represented by the formula (I): where R, Y3, R1, R2, R3, R4 and R5 are as defined herein.

公开(公告)号：US20150307502A9

公开(公告)日：2015-10-29

申请号：US14368111

申请日：2012-12-26

Applicant: RESEARCH TRIANGLE INSTITUTE ,  THE REGENTS OF THE UNIVERSITY OF MICHIGAN ,  VIRGINIA COMMONWEALTH UNIVERSITY

Inventor： Frank Ivy Carroll ,  Pauline Wanjiku Ondachi ,  Hernan A. Navarro ,  M. Imad Damaj ,  James H. Woods ,  Emily M. Jutkiewicz

IPC: C07D487/08

CPC classification number: C07D487/08

Abstract: Compounds and compositions for promoting smoking cessation or decreasing tobacco use or nicotine addiction are provided. The compounds are 2′-fluoro-3′-(substituted phenyl) deschloroepibatidine analogs. The compounds have been found to modulate neuronal nicotine acetylcholine receptors and are useful in methods for the treatment of conditions or disorders influenced by the modulation of neuronal nicotinic acetylcholine receptors.

Abstract translation: 提供了用于促进戒烟或减少烟草使用或尼古丁成瘾的化合物和组合物。 这些化合物是2'-氟-3' - （取代苯基）脱氯替巴替坦类似物。 已经发现这些化合物调节神经元尼古丁乙酰胆碱受体，并且可用于治疗受神经元烟碱乙酰胆碱受体调节影响的病症或障碍的方法。

公开(公告)号：US20150152119A1

公开(公告)日：2015-06-04

申请号：US14616313

申请日：2015-02-06

Applicant: Research Triangle Institute

Inventor： Frank Ivy Carroll ,  Pauline Wanjiku Ondachi

IPC: C07D487/08

CPC classification number: C07D487/08 ,  A61K31/407 ,  C07D401/14 ,  C07D409/14

Abstract: Provided herein are compounds and methods of preparation of compounds that are capable of functioning as agonists or antagonists of a nicotinic receptor. Also provided are pharmaceutical compositions comprising one or more of these compounds, which may further comprise one or more additional therapeutic agents. Further provided are methods of treatment of various conditions that may be responsive to such activity at the nicotinic receptors, such as nicotine dependence.

Abstract translation: 本文提供了能够作为烟碱受体的激动剂或拮抗剂起作用的化合物的化合物和方法。 还提供了包含一种或多种这些化合物的药物组合物，其可进一步包含一种或多种另外的治疗剂。 还提供了治疗可能对烟碱受体上的这种活性有反应的各种病症的方法，例如尼古丁依赖性。

公开(公告)号：US11292783B2

公开(公告)日：2022-04-05

申请号：US16333849

申请日：2017-09-15

Applicant: Research Triangle Institute

Inventor： Frank Ivy Carroll ,  Chad M. Kormos ,  Pauline W. Ondachi ,  Scott P. Runyon ,  Hernan A. Navarro ,  James B. Thomas ,  S. Wayne Mascarella

IPC: A61K31/472 ,  C07D217/26 ,  C07D401/12 ,  A61P25/34 ,  A61P25/36 ,  A61P25/32 ,  A61P25/18 ,  A61P25/24 ,  C07D211/18 ,  C07D413/12 ,  C07D487/08 ,  A61P25/00

Abstract: Potent opioid receptor antagonists of formula (I) and their use as pharmacotherapies for treating depression, anxiety, schizophrenia, eating disorders, and addiction to cocaine, methamphetamine, nicotine, alcohol, and opiates are disclosed. More specifically, the disclosure provides potent and selective kappa opioid receptor antagonist compounds, pharmaceutical compositions of those compounds and uses of those compounds to ameliorate or treat addictions, eating disorders, etc.

公开(公告)号：US20140357674A1

公开(公告)日：2014-12-04

申请号：US14368111

申请日：2012-12-26

Applicant: RESEARCH TRIANGLE INSTITUTE ,  THE REGENTS OF THE UNIVERSITY OF MICHIGAN ,  VIRGINIA COMMONWEALTH UNIVERSITY

Inventor： Frank Ivy Carroll ,  Pauline Wanjiku Ondachi ,  Hernan A. Navarro ,  M. Imad Damaj ,  James H. Woods ,  Emily M. Jutkiewicz

IPC: C07D487/08

CPC classification number: C07D487/08

Abstract: Compounds and compositions for promoting smoking cessation or decreasing tobacco use or nicotine addiction are provided. The compounds are 2′-fluoro-3′-(substituted phenyl) deschloroepibatidine analogs. The compounds have been found to modulate neuronal nicotine acetylcholine receptors and are useful in methods for the treatment of conditions or disorders influenced by the modulation of neuronal nicotinic acetylcholine receptors.

Abstract translation: 提供了用于促进戒烟或减少烟草使用或尼古丁成瘾的化合物和组合物。 这些化合物是2'-氟-3' - （取代苯基）脱氯替巴替坦类似物。 已经发现这些化合物调节神经元尼古丁乙酰胆碱受体，并且可用于治疗受神经元烟碱乙酰胆碱受体调节影响的病症或障碍的方法。

公开(公告)号：US20190263781A1

公开(公告)日：2019-08-29

申请号：US16333849

申请日：2017-09-15

Applicant: Research Triangle Institute

Inventor： Frank Ivy Carroll ,  Chad M. Kormos ,  Pauline W. Ondachi ,  Scott P. Runyon ,  Hernan A. Navarro ,  James B. Thomas ,  S. Wayne Mascarella

IPC: C07D401/12 ,  C07D413/12 ,  A61P25/18 ,  A61P25/24 ,  A61P25/32 ,  A61P25/34 ,  A61P25/36 ,  C07D217/26 ,  C07D211/18

Abstract: Potent opioid receptor antagonists of formula (I) and their use as pharmacotherapies for treating depression, anxiety, schizophrenia, eating disorders, and addiction to cocaine, methamphetamine, nicotine, alcohol, and opiates are disclosed. More specifically, the disclosure provides potent and selective kappa opioid receptor antagonist compounds, pharmaceutical compositions of those compounds and uses of those compounds to ameliorate or treat addictions, eating disorders, etc.

公开(公告)号：US20180215701A1

公开(公告)日：2018-08-02

申请号：US15388770

申请日：2016-12-22

Applicant: Research Triangle Institute

Inventor： Frank Ivy Carroll ,  Bruce Edward Blough ,  Philip Abraham

IPC: C07C225/16 ,  C07C211/27 ,  C07C225/18 ,  C07C211/35 ,  C07C211/29

CPC classification number: C07C225/16 ,  C07C211/27 ,  C07C211/29 ,  C07C211/35 ,  C07C225/18 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14

Abstract: The invention provides bupropion analogue compounds capable of inhibiting the reuptake of one or more monoamines. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin. Such compounds may be used to treat conditions that are responsive to inhibition of the reuptake of monoamines, including addiction, depression, and obesity.

公开(公告)号：US09527823B2

公开(公告)日：2016-12-27

申请号：US14537124

申请日：2014-11-10

Applicant: Research Triangle Institute ,  Dignity Health ,  Virginia Commonwealth University

Inventor： Frank Ivy Carroll ,  Bruce E. Blough ,  Hernan A. Navarro ,  S. Wayne Mascarella ,  Ana Zamfira Muresan ,  M. Imad Damaj ,  Ronald J. Lukas

IPC: C07D265/32 ,  A61K31/5375

CPC classification number: C07D265/32 ,  A61K31/5375

Abstract: The invention provides hydroxybupropion analogs capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.

Abstract translation: 本发明提供了能够抑制一种或多种单胺再摄取和/或在烟碱乙酰胆碱受体上作为拮抗剂的羟基安非他丁类似物。 所述化合物可以选择性地结合一种或多种单胺转运蛋白，包括用于多巴胺，去甲肾上腺素和5-羟色胺的单胺转运蛋白和/或可以选择性地结合一种或多种烟碱型乙酰胆碱受体亚型。 这些化合物可用于治疗对单胺水平的修饰和/或烟碱乙酰胆碱受体的拮抗作用有反应的病症，包括药物依赖性，抑郁症和肥胖症。

公开(公告)号：US10919841B2

公开(公告)日：2021-02-16

申请号：US15388770

申请日：2016-12-22

Applicant: Research Triangle Institute

Inventor： Frank Ivy Carroll ,  Bruce Edward Blough ,  Philip Abraham

IPC: C07C225/16 ,  C07C211/27 ,  C07C211/29 ,  C07C211/35 ,  C07C225/18

Abstract: The invention provides bupropion analogue compounds capable of inhibiting the reuptake of one or more monoamines. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin. Such compounds may be used to treat conditions that are responsive to inhibition of the reuptake of monoamines, including addiction, depression, and obesity.