Diaryl purine derivatives with improved bioavailability

    公开(公告)号:US10696677B2

    公开(公告)日:2020-06-30

    申请号:US16472155

    申请日:2017-12-20

    Abstract: This disclosure is directed to various compounds and methods of preparation of improved compounds that are capable of functioning as cannabinoid receptor 1 (CB1) antagonists with reduced central nervous system (CNS) side effects. The application is also directed to pharmaceutical compositions containing one or more of these compounds, which may also contain one or more additional therapeutic agents. It is also directed to methods of treatment of various conditions that may be responsive to antagonism of the CB1 receptors, including, but not limited to, metabolic syndromes (including liver disease, obesity, and diabetes).

    PROLINE-BASED NEUROPEPTIDE FF RECEPTOR MODULATORS

    公开(公告)号:US20240058303A1

    公开(公告)日:2024-02-22

    申请号:US18484116

    申请日:2023-10-10

    CPC classification number: A61K31/40 A61P25/00

    Abstract: Neuropeptide FF receptor modulators based on a proline scaffold are provided which offer NPFF receptor potencies in the nanomolar range and antagonistic selectivity for the NPFF1 receptor. Methods, compounds and compositions for modulating the function of neuropeptide FF receptors are provided for pharmacotherapies capable of influencing conditions or disorders affected by the neuropeptide FF receptors.

    COMPOSITION AND METHOD FOR NEUROPEPTIDE S RECEPTOR (NPSR) ANTAGONISTS
    6.
    发明申请
    COMPOSITION AND METHOD FOR NEUROPEPTIDE S RECEPTOR (NPSR) ANTAGONISTS 有权
    神经元受体(NPSR)拮抗剂的组合物和方法

    公开(公告)号:US20150057268A1

    公开(公告)日:2015-02-26

    申请号:US14363079

    申请日:2012-12-06

    CPC classification number: C07D491/048 C07D491/04 C07D491/10 C07D491/107

    Abstract: Neuropeptide S receptor antagonists are provided that bind in functional assays to neuropeptide S receptors; methods are provided for use of these antagonists in treatment of conditions or disease states that are ameliorated by blocking of the neuropeptide S receptor, including substance abuse and substance abuse relapse; and for use of neuropeptide S receptor antagonists in the manufacture of therapeutics and pro-drugs for therapeutics useful in disease states and conditions sensitive to binding of the neuropeptide S receptor.

    Abstract translation: 提供神经肽S受体拮抗剂,其在功能测定中与神经肽S受体结合; 提供了这些拮抗剂用于治疗通过阻断神经肽S受体而改善的病症或疾病状态的方法,包括药物滥用和药物滥用复发; 并且用于神经肽S受体拮抗剂在制备用于治疗疾病状态和治疗神经肽S受体结合敏感的疾病状态的治疗剂的前药中的用途。

    DIARYL PURINE DERIVATIVES WITH IMPROVED BIOAVAILABILITY

    公开(公告)号:US20190352305A1

    公开(公告)日:2019-11-21

    申请号:US16472155

    申请日:2017-12-20

    Abstract: This disclosure is directed to various compounds and methods of preparation of improved compounds that are capable of functioning as cannabinoid receptor 1 (CB1) antagonists with reduced central nervous system (CNS) side effects. The application is also directed to pharmaceutical compositions containing one or more of these compounds, which may also contain one or more additional therapeutic agents. It is also directed to methods of treatment of various conditions that may be responsive to antagonism of the CB1 receptors, including, but not limited to, metabolic syndromes (including liver disease, obesity, and diabetes).

    PERIPHERALLY RESTRICTED DIPHENYL PURINE DERIVATIVES
    8.
    发明申请
    PERIPHERALLY RESTRICTED DIPHENYL PURINE DERIVATIVES 有权
    外用限制性二苯醚衍生物

    公开(公告)号:US20150031689A1

    公开(公告)日:2015-01-29

    申请号:US14378479

    申请日:2013-02-15

    CPC classification number: C07D473/34

    Abstract: The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.

    Abstract translation: 本发明提供了能够根据下式用作大麻素受体拮抗剂的化合物:这些化合物可用于治疗涉及大麻素受体系统的病症,例如肥胖症,肝病,糖尿病,疼痛和炎症。

    PROLINE-BASED NEUROPEPTIDE FF RECEPTOR MODULATORS

    公开(公告)号:US20230091922A1

    公开(公告)日:2023-03-23

    申请号:US17937450

    申请日:2022-10-02

    Abstract: Neuropeptide FF receptor modulators based on a proline scaffold are provided which offer NPFF receptor potencies in the nanomolar range and antagonistic selectivity for the NPFF1 receptor. Methods, compounds and compositions for modulating the function of neuropeptide FF receptors are provided for pharmacotherapies capable of influencing conditions or disorders affected by the neuropeptide FF receptors.

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