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    TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF
    52.
    发明申请
    TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF 有权
    TRPV1拮抗剂包括二氢替代物及其用途

    公开(公告)号：US20140329829A1

    公开(公告)日：2014-11-06

    申请号：US14127903

    申请日：2012-06-21

    Applicant: Shigeru Ando ,  Noriyuki Kurose ,  Laykea Tafesse

    Inventor： Shigeru Ando ,  Noriyuki Kurose ,  Laykea Tafesse

    IPC: C07D417/14

    CPC classification number: C07D417/14 ,  A61K31/428 ,  A61K31/496 ,  C07C57/15 ,  C07C59/255 ,  C07C309/29 ,  C07C309/30 ,  C07D417/12

    Abstract: The disclosure relates to Compounds of Formula (I) and pharmaceutically acceptable derivatives thereof, where R1, R4, R8, R9, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, UI, an ulcer, IBD, and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof.

    Abstract translation: 本公开涉及式（I）化合物及其药学上可接受的衍生物，其中R 1，R 4，R 8，R 9和m如本文所定义，包含有效量的式（I）化合物或其药学上可接受的衍生物 以及用于治疗或预防与骨关节炎，骨关节炎，UI，溃疡，IBD和IBS相关的疼痛，疼痛，溃疡，IBD和IBS等症状的治疗或预防方法，其包括向有需要的动物施用有效量的式（I）化合物， 或其药学上可接受的衍生物。

    Bicycloheteroaryl compounds and their use as TRPV1 ligands
    53.
    发明授权
    Bicycloheteroaryl compounds and their use as TRPV1 ligands 有权
    双环杂芳基化合物及其作为TRPV1配体的用途

    公开(公告)号：US08759362B2

    公开(公告)日：2014-06-24

    申请号：US12603719

    申请日：2009-10-22

    Applicant: Laykea Tafesse

    Inventor： Laykea Tafesse

    IPC: C07D471/04 ,  A61K31/519 ,  A61P23/00 ,  A61P1/00 ,  A61P1/04

    CPC classification number: A61K31/502 ,  C07D401/04 ,  C07D401/14 ,  C07D417/14 ,  C07D471/04

    Abstract: The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.

    Abstract translation: 本发明涉及式I化合物及其药学上可接受的衍生物，包含有效量的式I化合物或其药学上可接受的衍生物的组合物，以及用于治疗或预防诸如疼痛，UI，溃疡，IBD的病症的方法 和IBS，包括向有需要的动物施用有效量的式I化合物或其药学上可接受的衍生物。

    Therapeutic agents useful for treating pain
    54.
    发明授权
    Therapeutic agents useful for treating pain 有权

    公开(公告)号：US08604037B2

    公开(公告)日：2013-12-10

    申请号：US13212941

    申请日：2011-08-18

    Applicant: Qun Sun ,  Laykea Tafesse ,  Sam Victory

    Inventor： Qun Sun ,  Laykea Tafesse ,  Sam Victory

    IPC: A61K31/501 ,  A61K31/497 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D417/12

    CPC classification number: C07D417/12 ,  A61K31/495 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

    Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.

    Substituted pyridines useful for treating pain
    56.
    发明授权
    Substituted pyridines useful for treating pain 有权
    用于治疗疼痛的替代吡啶

    公开(公告)号：US08389549B2

    公开(公告)日：2013-03-05

    申请号：US12596997

    申请日：2008-04-25

    Applicant: Laykea Tafesse

    Inventor： Laykea Tafesse

    IPC: A61K31/44

    CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D417/14

    Abstract: A compound of Formula: (I) or a pharmaceutically acceptable derivative thereof, where Ar1, Ar2, X, R3, and m are as disclosed herein. Compounds of Formulae (I)-(V) and pharmaceutically acceptable derivatives thereof; compositions comprising an effective amount of a compound of Formulae (I)-(V) or a pharmaceutically acceptable derivative thereof; and methods for treating or preventing pain, UI, an ulcer, IBD, or IBS in an animal comprising administering to an animal in need thereof an effective amount of a compound of Formulae (I)-(V) or a pharmaceutically acceptable derivative thereof are disclosed herein.

    Abstract translation: 式（I）化合物或其药学上可接受的衍生物，其中Ar1，Ar2，X，R3和m如本文所公开。 式（I） - （V）化合物及其药学上可接受的衍生物; 包含有效量的式（I） - （V）化合物或其药学上可接受的衍生物的组合物; 以及用于治疗或预防动物中的疼痛，UI，溃疡，IBD或IBS的方法，包括向有需要的动物施用有效量的式（I） - （V）化合物或其药学上可接受的衍生物 这里公开。

    Therapeutic agents useful for treating pain
    58.
    发明授权
    Therapeutic agents useful for treating pain 有权
    用于治疗疼痛的治疗剂

    公开(公告)号：US07582635B2

    公开(公告)日：2009-09-01

    申请号：US10739190

    申请日：2003-12-19

    Applicant: Qun Sun ,  Laykea Tafesse ,  Sam Victory

    Inventor： Qun Sun ,  Laykea Tafesse ,  Sam Victory

    IPC: A61K31/497

    CPC classification number: C07D417/12 ,  A61K31/495 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

    Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.

    Abstract translation: 下式的化合物：其中Ar1，A，R3，x和m如本文所公开，Ar 2是苯并噻唑基，苯并恶唑基或苯并咪唑基或其药学上可接受的盐（“苯并恶唑基哌嗪化合物”），包含苯并恶唑基哌嗪化合物 以及用于治疗或预防疼痛，UI，溃疡，IBD，IBS，成瘾性障碍，帕金森病，帕金森综合征，焦虑，癫痫，中风，癫痫发作，瘙痒症状，精神病，认知障碍，记忆缺陷， 限制性脑功能，亨廷顿氏舞蹈病，肌萎缩性侧索硬化，痴呆，视网膜病变，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症，其中包括向有需要的动物施用有效量的苯并恶唑基哌嗪化合物。

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