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88 条记录 (耗时 0.045 秒)

    Gastrin releasing peptide-like peptides
    2.
    发明授权
    Gastrin releasing peptide-like peptides 失效
    胃泌素释放肽样肽

    公开(公告)号：US4613586A

    公开(公告)日：1986-09-23

    申请号：US602116

    申请日：1984-04-19

    申请人： Jack D. Barchas ,  Eckard Weber ,  Christopher J. Evans ,  Jaw-Kang Chang ,  Robin G. Lorenz ,  Kevin A. Roth

    发明人： Jack D. Barchas ,  Eckard Weber ,  Christopher J. Evans ,  Jaw-Kang Chang ,  Robin G. Lorenz ,  Kevin A. Roth

    IPC分类号： A61K38/00 ,  C07K14/575 ,  C07K7/06 ,  C07K7/08

    CPC分类号： C07K14/57572 ,  A61K38/00

    摘要： Novel peptides having gastrin releasing peptide-like activity having the structures Ala-Pro-Val-Ser-Val-Gly-Gly-Gly-Thr-Val-Leu-Ala-Lys-Met-Tyr-Pro-NH.sub.2 and Gly-Asn-His-Trp-Ala-Val-Gly-His-Leu-Met-NH.sub.2, have been isolated from rat and guinea pig brain extracts and synthesized by a solid phase peptide synthesis methods. The GRP-like peptides are useful as pharmaceuticals to lower body temperature, increase respiratory activity, reduce food intake, stimulate pancreatic hormone release, stimulate pituitary hormone release and suppress thyroid hormone release in mammals.

    摘要翻译： 具有胃泌素释放肽样活性的具有Ala-Pro-Val-Ser-Val-Gly-Gly-Gly-Thr-Val-Leu-Ala-Lys-Met-Tyr-Pro-NH2和Gly-Asn- His-Trp-Ala-Val-Gly-His-Leu-Met-NH2已经从大鼠和豚鼠脑提取物中分离并通过固相肽合成方法合成。 GRP样肽可用作降低体温，增加呼吸活动，减少食物摄取，刺激胰腺激素释放，刺激垂体激素释放和抑制哺乳动物中甲状腺激素释放的药物。

    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
    8.
    发明授权
    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 有权
    碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途

    公开(公告)号：US06458843B1

    公开(公告)日：2002-10-01

    申请号：US09421403

    申请日：1999-10-21

    申请人： Yan Wang ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F. W. Keana ,  Victor I. Ilyin ,  Eckard Weber

    发明人： Yan Wang ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F. W. Keana ,  Victor I. Ilyin ,  Eckard Weber

    IPC分类号： A61K3117

    CPC分类号： C07D213/643 ,  A61K31/17 ,  A61K31/175 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K31/505 ,  C07C281/12 ,  C07C281/14 ,  C07C2601/14 ,  C07D209/14 ,  C07D211/46 ,  C07D213/68 ,  C07D215/12 ,  C07D307/91 ,  C07D309/12 ,  C07D317/50 ,  C07D317/58 ,  C07D317/62 ,  C07D317/64 ,  C07D319/18

    摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones 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), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.

    摘要翻译： 本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基; 或R 22和R 23与N一起形成杂环; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。 本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来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），用于治疗和预防 涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。

    Tri-and tetra-substituted guanidines and their use as excitatory amino acid antagonists
    10.
    发明授权
    Tri-and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
    三取代和四取代的胍和它们作为兴奋性氨基酸拮抗剂的用途

    公开(公告)号：US5767162A

    公开(公告)日：1998-06-16

    申请号：US470345

    申请日：1995-06-06

    申请人： Eckard Weber ,  John F. W. Keana

    发明人： Eckard Weber ,  John F. W. Keana

    IPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18 ,  A61K31/37 ,  A61K31/655

    CPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18

    摘要： Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

    摘要翻译： 表现出对苯环利定（PCP）受体的高结合亲和力，更优选对大脑σ受体的低亲和力的三取代和四取代胍基。 这些胍衍生物通过作为NMDA受体 - 离子通道复合物的离子通道的阻断剂，作为NMDA受体的谷氨酸诱导反应的非竞争性抑制剂。 因此，这些化合物发挥神经保护活性，并且可用于治疗缺氧，低血糖，脑或脊髓缺血以及脑或脊髓创伤中的神经元损失，以及用于治疗癫痫，阿尔茨海默病，肌萎缩性侧索硬化症 ，帕金森病，亨廷顿舞蹈病，唐氏综合征，柯萨科夫病和其他神经退行性疾病。