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    INDOLE AND INDOLINE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF
    21.
    发明申请
    INDOLE AND INDOLINE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF 有权
    吲哚和吲哚型哌啶化合物及其用途

    公开(公告)号：US20150315201A1

    公开(公告)日：2015-11-05

    申请号：US14654727

    申请日：2013-12-23

    Applicant: Laykea TAFESSE

    Inventor： Laykea Tafesse

    IPC: C07D487/08

    CPC classification number: C07D487/08 ,  C07D471/08

    Abstract: The disclosure relates to indole-type piperidine compounds, indoline-type piperidine compounds and related piperidine-type bicyclic compounds containing a five-membered nitrogen-containing ring (e.g., pyrrole or dihydropyrrole) fused to a heteroaryl ring, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an indole-type piperidine compound, indoline-type piperidine compound or related piperidine-type bicyclic compound containing a five-membered nitrogen-containing ring (e.g., pyrrole or dihydropyrrole) fused to a heteroaryl ring.

    Abstract translation: 本公开内容涉及吲哚型哌啶化合物，二氢吲哚型哌啶化合物和含有与杂芳基环稠合的五元含氮环（例如吡咯或二氢吡咯）的相关哌啶型双环化合物，其包含有效量的 这些化合物以及治疗或预防诸如疼痛的病症的方法，包括向有需要的动物施用有效量的吲哚型哌啶化合物，二氢吲哚型哌啶化合物或相关的哌啶型双环化合物，其含有五 （例如，吡咯或二氢吡咯）与杂芳基环稠合。

    Fused and spirocycle compounds and the use thereof
    23.
    发明授权
    Fused and spirocycle compounds and the use thereof 有权
    熔融和螺环化合物及其用途

    公开(公告)号：US08546417B2

    公开(公告)日：2013-10-01

    申请号：US13486267

    申请日：2012-06-01

    Applicant: Zhengming Chen ,  Laykea Tafesse

    Inventor： Zhengming Chen ,  Laykea Tafesse

    IPC: A61K31/438 ,  A61K51/04 ,  C07D471/10

    CPC classification number: C07D491/107 ,  C07D221/20 ,  C07D471/10 ,  G01N33/566

    Abstract: The invention relates to fused and spirocycle compounds of Formula I: or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1, R2, Q1-Q3, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

    Abstract translation: 本发明涉及式I的稠合和螺环化合物：或其药学上可接受的盐，前药或溶剂化物，其中R1，R2，Q1-Q3和Z如本说明书所述定义。 本发明还涉及式I化合物用于治疗，预防或改善对阻塞钙通道，特别是N型钙通道有响应的病症的用途。 本发明的化合物特别适用于治疗疼痛。

    PHOSPHORUS-SUBSTITUTED QUINOXALINE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF
    27.
    发明申请
    PHOSPHORUS-SUBSTITUTED QUINOXALINE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF 有权
    磷酸替代的喹啉类型哌啶化合物及其用途

    公开(公告)号：US20140128346A1

    公开(公告)日：2014-05-08

    申请号：US13996440

    申请日：2011-12-21

    Applicant: Dawit Tadesse ,  Laykea Tafesse ,  Zhou Xiaoming

    Inventor： Dawit Tadesse ,  Laykea Tafesse ,  Zhou Xiaoming

    IPC: C07F9/6561

    CPC classification number: C07F9/6561 ,  C07F9/65583

    Abstract: The disclosure relates to Phosphorus-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein the dashed line, A, B, Q, R1, R2, R3, R4, Y1, Z, and a are as defined herein, compositions comprising an effective amount of a Phosphorus-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Phosphorus-Substituted Quinoxaline-Type Piperidine Compound.

    Abstract translation: 本公开涉及式（I）的磷取代的喹喔啉型哌啶化合物及其药学上可接受的衍生物，其中虚线A，B，Q，R 1，R 2，R 3，R 4，Y 1，Z和a分别为 包含有效量的磷取代的喹喔啉型哌啶化合物的组合物，以及治疗或预防诸如疼痛的病症的方法，包括向有需要的动物施用有效量的磷取代的喹喔啉 - 类哌啶化合物。

    Therapeutic agents useful for treating pain
    29.
    发明授权
    Therapeutic agents useful for treating pain 有权

    公开(公告)号：US08536177B2

    公开(公告)日：2013-09-17

    申请号：US13205323

    申请日：2011-08-08

    Applicant: Qun Sun ,  Laykea Tafesse ,  Sam Victory

    Inventor： Qun Sun ,  Laykea Tafesse ,  Sam Victory

    IPC: A61K31/497 ,  A61K31/435 ,  C07D279/10 ,  C07D401/14

    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.

    Therapeutic agents useful for treating pain
    30.
    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：US08008300B2

    公开(公告)日：2011-08-30

    申请号：US12499480

    申请日：2009-07-08

    Applicant: Qun Sun ,  Laykea Tafesse ,  Sam Victory

    Inventor： Qun Sun ,  Laykea Tafesse ,  Sam Victory

    IPC: A61K31/50 ,  A61K31/497 ,  C07D403/04 ,  C07D241/02

    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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