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    Cyclic bradykinin antagonist peptides
    1.
    发明授权
    Cyclic bradykinin antagonist peptides 失效
    循环缓激肽拮抗剂肽

    公开(公告)号：US5543496A

    公开(公告)日：1996-08-06

    申请号：US279763

    申请日：1994-07-25

    Applicant: Donald J. Kyle ,  Sarvajit Chakravarty

    Inventor： Donald J. Kyle ,  Sarvajit Chakravarty

    IPC: A61K38/00 ,  C07K7/18 ,  A61K38/12 ,  C07K7/52

    CPC classification number: C07K7/18 ,  A61K38/00 ,  Y10S930/27

    Abstract: Cyclic compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acid substitutions are made at postions 2 and 5 or 6 to facilitate the cyclization of the peptide through covalent bonding of the amino acid side chains.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环化合物是有效的缓激肽受体拮抗剂。 在位置2和5或6处进行氨基酸取代，以通过氨基酸侧链的共价键来促进肽的环化。 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。

    Benzomorphan compounds
    3.
    发明授权
    Benzomorphan compounds 有权
    苯并吡喃化合物

    公开(公告)号：US08426594B2

    公开(公告)日：2013-04-23

    申请号：US12745472

    申请日：2008-11-28

    Applicant: Donald J. Kyle

    Inventor： Donald J. Kyle

    IPC: C07D221/26

    CPC classification number: C07D221/26

    Abstract: The invention relates to Benzomorphan Compounds of Formula (I): wherein X, R1, R2, R3, R4, and R5 are as defined herein. These compounds are useful for treating constipation preferably constipation caused by mu-opioid agonist therapy.

    Abstract translation: 本发明涉及式（I）的苯并恶嗪化合物：其中X，R 1，R 2，R 3，R 4和R 5如本文所定义。 这些化合物可用于治疗便秘，优选由μ-阿片样物质激动剂治疗引起的便秘。

    THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN
    4.
    发明申请
    THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN 审中-公开
    治疗药物有用的治疗药物

    公开(公告)号：US20110281885A1

    公开(公告)日：2011-11-17

    申请号：US12879885

    申请日：2010-09-10

    Applicant: Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse ,  Chongwu Zhang ,  Xiaoming Zhou

    Inventor： Donald J. Kyle ,  Qun Sun ,  Laykea Tafesse ,  Chongwu Zhang ,  Xiaoming Zhou

    IPC: A61K31/496 ,  A61K31/497 ,  C12N5/07 ,  C07D417/04 ,  C07D401/04 ,  A61P25/00

    CPC classification number: C07D213/74 ,  C07D213/85 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D285/06 ,  C07D333/16

    Abstract: A compound of formula: wherein A, Ar, R3, R6, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Cyanoiminopiperazine Compound”), compositions comprising an effective amount of a Cyanoiminopiperazine Compound, and methods for treating or preventing pain, urinary incontinence, an ulcer, inflammatory-bowel disease, irritable-bowel syndrome, 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 Cyanoiminopiperazine Compound are disclosed.

    Abstract translation: 本文公开的其中A，Ar，R 3，R 6和m的化合物或其药学上可接受的盐（“氰基亚氨基哌嗪化合物”），包含有效量的氰基亚氨基哌嗪化合物的组合物，以及治疗或预防的方法 疼痛，尿失禁，溃疡，炎性肠病，肠易激综合征，成瘾性疾病，帕金森病，帕金森综合征，焦虑症，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，包括向有需要的动物施用有效量的氰基亚氨基哌嗪化合物。

    1,2,5-Thiadiazol-3-yl-piperazine therapeutic agents useful for treating pain, depression and anxiety
    6.
    发明授权
    1,2,5-Thiadiazol-3-yl-piperazine therapeutic agents useful for treating pain, depression and anxiety 有权
    可用于治疗疼痛，抑郁和焦虑的1,2,5-噻二唑-3-基 - 哌嗪治疗剂

    公开(公告)号：US07342017B2

    公开(公告)日：2008-03-11

    申请号：US11246498

    申请日：2005-10-07

    Applicant: Donald J. Kyle ,  Qun Sun

    Inventor： Donald J. Kyle ,  Qun Sun

    IPC: A61K31/497 ,  C07D417/04

    CPC classification number: C07D285/10

    Abstract: A compound of formula: (wherein X, R1, R3, R4, and R5 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Thiadiazolylpiperazine Compound”), pharmaceutical compositions comprising a Thiadiazolylpiperazine Compound, and methods for treating or preventing, e.g., pain, depression and anxiety, in a patient comprising administering to a patient in need thereof an effective amount of a Thiadiazolylpiperazine Compound are disclosed.

    Abstract translation: 下式化合物：其中X，R 1，R 3，R 4和R 5均为 本文公开的）或其药学上可接受的盐（“噻二唑基哌嗪化合物”），包含噻二唑基哌嗪化合物的药物组合物，以及用于治疗或预防例如疼痛，抑郁和焦虑的方法，包括向有需要的患者施用 公开了有效量的噻二唑基哌嗪化合物。

    Therapeutic agents useful for treating pain
    7.
    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：US07256193B2

    公开(公告)日：2007-08-14

    申请号：US11368133

    申请日：2006-03-02

    Applicant: Donald J. Kyle ,  Sun Qun

    Inventor： Donald J. Kyle ,  Sun Qun

    IPC: A61K31/496

    CPC classification number: C07D405/12 ,  C07D213/74 ,  C07D417/12

    Abstract: A Compound of formula (wherein X is O or S and R1-R5 are disclosed herein) or a pharmaceutically acceptable salt thereof (each being a “Piperazine Compound”), pharmaceutical compositions comprising a Piperazine 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 Piperazine Compound are disclosed.

    Abstract translation: 式（其中X是O或S和R 1 -R 5）的化合物在此公开）或其药学上可接受的盐（各自为“哌嗪化合物”） ，包含哌嗪化合物的药物组合物和治疗或预防疼痛，UI，溃疡，IBD，IBS，成瘾性障碍，帕金森病，帕金森综合征，焦虑症，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，肌肉痉挛，偏头痛，呕吐，运动障碍或抑郁症，包括向有需要的动物施用有效量的 哌嗪化合物被公开。

    Bradykinin antagonist pseudopeptide derivatives of olefinic aminoalkanoic acids
    8.
    发明授权
    Bradykinin antagonist pseudopeptide derivatives of olefinic aminoalkanoic acids 失效
    烯酰氨基链烷酸的缓激肽拮抗剂假肽衍生物

    公开(公告)号：US5444048A

    公开(公告)日：1995-08-22

    申请号：US118981

    申请日：1993-09-09

    Applicant: Donald J. Kyle

    Inventor： Donald J. Kyle

    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. Amino acids at postions 2 through 5 are replaced by olefinic aminoalkenoyl groups 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。 位置2至5处的氨基酸被烯属的氨基烯酰基代替，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。

    Corticotropin-releasing factor antagonism compounds
    9.
    发明授权
    Corticotropin-releasing factor antagonism compounds 失效
    促肾上腺皮质激素释放因子拮抗剂

    公开(公告)号：US5063245A

    公开(公告)日：1991-11-05

    申请号：US500478

    申请日：1990-03-28

    Applicant: Mary E. Abreu ,  Waclaw Rzeszotarski ,  Donald J. Kyle ,  Roger N. Hiner ,  Richard L. Elliott

    Inventor： Mary E. Abreu ,  Waclaw Rzeszotarski ,  Donald J. Kyle ,  Roger N. Hiner ,  Richard L. Elliott

    IPC: C07D231/28

    CPC classification number: C07D231/28

    Abstract: The present invention relates to a method of producing corticotropin-releasing factor (CRF) antagonist activity and thus provides a method of treating a wide range of stress-related disorders, including affective illnesses, such as depression and anxiety, as well as irritable bowel syndrome, anorexia nervosa, cardiovascular abnormalities and stress-induced immune suppression. The invention also relates to compounds (4-substituted thio-5-oxo-3-pyrazolines) and to pharmaceutical compositions suitable for use in such a method.

    Abstract translation: 本发明涉及一种产生促肾上腺皮质激素释放因子（CRF）拮抗剂活性的方法，因此提供了治疗各种应激相关疾病（包括抑郁和焦虑等情感疾病）以及肠易激综合征 ，神经性厌食症，心血管异常和应激诱导的免疫抑制。 本发明还涉及化合物（4-取代的硫代-5-氧代-3-吡唑啉）和适用于这种方法的药物组合物。

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