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    Benzenesulfonamide compounds and their use
    12.
    发明授权
    Benzenesulfonamide compounds and their use 有权
    苯磺酰胺化合物及其用途

    公开(公告)号：US08247442B2

    公开(公告)日：2012-08-21

    申请号：US12225743

    申请日：2007-03-29

    Applicant: Zhengming Chen ,  Khondaker Islam ,  Bin Shao ,  Jiangchao Yao ,  Donald J. Kyle

    Inventor： Zhengming Chen ,  Khondaker Islam ,  Bin Shao ,  Jiangchao Yao ,  Donald J. Kyle

    IPC: A61K31/40 ,  C07D207/14

    CPC classification number: C07D211/42 ,  C07D207/14 ,  C07D401/12

    Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use 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的氮杂环丁烷基，吡咯烷基，哌啶基和六氢氮杂卟啉化合物及其药学上可接受的盐，前药或溶剂合物，其中R1-R3和Z如说明书所述定义。 本发明还涉及使用式I的化合物来治疗，预防或改善对阻断钙通道，特别是N型钙通道有响应的病症。 本发明的化合物特别适用于治疗疼痛。

    Therapeutic agents useful for treating pain
    14.
    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：US07262194B2

    公开(公告)日：2007-08-28

    申请号：US10625708

    申请日：2003-07-24

    Applicant: Donald J. Kyle ,  Qun Sun

    Inventor： Donald J. Kyle ,  Qun Sun

    IPC: C07D403/04 ,  C07D403/14 ,  A61K31/501

    CPC classification number: C07D237/24

    Abstract: A compound of formula: wherein X is S or O and A, R1-R4, n, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Pyridazinylpiperazine Compound”), compositions comprising a Pyridazinylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD and IBS in an animal comprising administering to an animal in need thereof an effective amount of a Pyridazinylpiperazine Compound are disclosed herein.

    Abstract translation: 式（I）化合物或其药学上可接受的盐（其中X为S或O且A，R 1 -R 4， “哒嗪基哌嗪化合物”），包含哒嗪基哌嗪化合物的组合物，以及在动物中治疗或预防疼痛，UI，溃疡，IBD和IBS的方法，其包括向有需要的动物施用有效量的哒嗪基哌嗪化合物。

    Aryl substituted thiazolidinones and the use thereof
    15.
    发明授权
    Aryl substituted thiazolidinones and the use thereof 有权
    芳基取代的噻唑烷酮及其用途

    公开(公告)号：US07169782B2

    公开(公告)日：2007-01-30

    申请号：US10195530

    申请日：2002-07-16

    Applicant: Qun Sun ,  Donald J. Kyle ,  Parviz Gharagozloo ,  Ji Yang

    Inventor： Qun Sun ,  Donald J. Kyle ,  Parviz Gharagozloo ,  Ji Yang

    IPC: C07D277/14 ,  C07D417/06 ,  A61K31/426 ,  A61K31/4439

    CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/14 ,  C07D279/06 ,  C07D417/04 ,  C07D417/06

    Abstract: This invention relates aryl substituted thiazolidinones of Formula I: or a pharmaceutically acceptable salt, or solvate thereof, wherein R1 and R2, are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

    Abstract translation: 本发明涉及式I的芳基取代的噻唑烷酮：或其药学上可接受的盐或溶剂合物，其中R 1和R 2 2在本说明书中定义。 本发明还涉及式I化合物用于治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS）以及治疗，预防或改善的用途 作为抗惊厥剂，作为抗惊厥剂，作为抗躁狂抑制剂，作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病变。

    Bradykinin antagonist pseudopeptide derivatives of aminoalkanoic acids and related olefins
    16.
    发明授权
    Bradykinin antagonist pseudopeptide derivatives of aminoalkanoic acids and related olefins 失效
    氨基链烷酸和相关烯烃的缓激肽拮抗剂假肽衍生物

    公开(公告)号：US5552383A

    公开(公告)日：1996-09-03

    申请号：US118550

    申请日：1993-09-09

    Applicant: Donald J. Kyle ,  Babu J. Mavunkel

    Inventor： Donald J. Kyle ,  Babu J. Mavunkel

    IPC: A61K38/00 ,  C07K7/18 ,  A61K38/08

    CPC classification number: C07K7/18 ,  A61K38/00

    Abstract: Pseudopeptide compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. All or a portion of the amino acids at postions 2 through 5 of the bradykinin sequence are replaced by 2-pyrrolidinyl and/or amino-alkanoic acid or related olefinic derivatives to reduce the peptidic nature of the compounds.The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.

    Abstract translation: 基于修饰的缓激肽序列的假肽化合物是有效的缓激肽受体拮抗剂。 缓激肽序列的位置2至5处的氨基酸的全部或部分被2-吡咯烷基和/或氨基 - 链烷酸或相关的烯属衍生物代替，以降低化合物的肽性质。 所产生的类似物可用于治疗其中产生或注射过量的缓激肽或相关激肽的哺乳动物和人的病症和疾病，例如通过昆虫叮咬。

    Bradykinin antagonist peptides
    17.
    发明授权
    Bradykinin antagonist peptides 失效
    缓激肽拮抗肽

    公开(公告)号：US5385889A

    公开(公告)日：1995-01-31

    申请号：US167052

    申请日：1993-12-16

    Applicant: Donald J. Kyle ,  Roger N. Hiner

    Inventor： Donald J. Kyle ,  Roger N. Hiner

    IPC: A61K38/00 ,  A61K38/17 ,  A61P25/04 ,  A61P29/00 ,  C07D207/12 ,  C07K7/18 ,  A61K37/42

    CPC classification number: C07K7/18 ,  C07D207/12 ,  A61K38/00 ,  Y10S514/803

    Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with a D-configuration hydroxyproline ether or thioether converts bradykinin agonists into bradykinin antagonists. The invention further includes the intermediate compounds and additional modifications at other positions within the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency, and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.

    Abstract translation: 肽类激素缓激肽或缓激肽的其他取代类似物的L-位置被D-构型羟脯氨酸醚或硫醚取代，将缓激肽激动剂转化为缓激肽拮抗剂。 本发明还包括中间体化合物和在新的7-位修饰的缓激肽拮抗剂中的其它位置的其他改变，其增加新的缓激肽拮抗剂的抗酶性，拮抗剂效力和/或特异性。 所产生的类似物可用于治疗其中产生或注射过量的缓激肽或相关激肽的哺乳动物和人的病症和疾病，例如通过昆虫叮咬。

    Monocyclic compounds and their use as TRPV1 ligands
    20.
    发明授权
    Monocyclic compounds and their use as TRPV1 ligands 有权
    单环化合物及其作为TRPV1配体的用途

    公开(公告)号：US08703962B2

    公开(公告)日：2014-04-22

    申请号：US12603684

    申请日：2009-10-22

    Applicant: Donald J. Kyle ,  Laykea Tafesse

    Inventor： Donald J. Kyle ,  Laykea Tafesse

    IPC: C07D277/62 ,  C07D277/64 ,  C07D277/82 ,  A61K31/425

    CPC classification number: C07D213/61 ,  C07D213/82

    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。

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