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    • 6. 发明授权
    • Cyclic tetrapeptide compound and use thereof
    • 环状四肽化合物及其用途
    • US06656905B1
    • 2003-12-02
    • US09806500
    • 2001-05-04
    • Hiroaki MoriKazutoshi SakamotoYasuhisa TsurumiShigehiro TakaseMotohiro Hino
    • Hiroaki MoriKazutoshi SakamotoYasuhisa TsurumiShigehiro TakaseMotohiro Hino
    • A61K3807
    • A61K38/12C07K5/126
    • A cyclic tetrapeptide compound and use thereof. Especially, a compound WF27082, a process for production of the compound by culturing, in a nutrient medium, a WF27082-producing strain belonging to Acremonium and recovering the compound from a culture broth, a pharmaceutical composition containing the compound as an active ingredient, in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient, the compound for use as a medicament, a use of the compound for manufacture of a medicament for inhibiting histone deacetylase, a use of the compound for manufacture of a medicament for treating or preventing inflammatory disorders, diabetes, diabetic complications, homozygous thalassemia, fibrosis, cirrhosis, acute promyelocytic leukaemia (APL), protozoal infections, organ transplant rejections, autoimmune diseases, or tumors, a use of histone deacetylase inhibitors as an immunosuppressant or an antitumor agent, and a use of histone deacetylase inhibitors for manufacture of a medicament for treating or preventing organ transplant rejections, autoimmune diseases or tumors are described.
    • 一种环状四肽化合物及其用途。 特别地,化合物WF27082是通过在营养培养基中培养属于顶孢菌属的WF27082产生菌株并从培养液中回收化合物,将含有该化合物作为活性成分的药物组合物生产化合物的方法, 与药学上可接受的,基本上无毒的载体或赋形剂的相关联,用作药物的化合物,该化合物用于制备用于抑制组蛋白脱乙酰酶的药物的用途,该化合物用于制备用于治疗或 预防炎性疾病,糖尿病,糖尿病并发症,纯合地中海贫血,纤维化,肝硬化,急性早幼粒细胞白血病(APL),原生动物感染,器官移植排斥,自身免疫疾病或肿瘤,组蛋白脱乙酰酶抑制剂作为免疫抑制剂或抗肿瘤剂的用途, 以及使用组蛋白脱乙酰酶抑制剂来制造用于治疗或预防的药物 描述器官移植排斥,自身免疫性疾病或肿瘤。
    • 10. 发明申请
    • Compound Ws727713
    • 化合物Ws727713
    • US20070254829A1
    • 2007-11-01
    • US11547729
    • 2005-03-22
    • Takanao OtsukaHirotsugu UedaKeiko FujieHideyuki MuramatsuMichizane HashimotoShigehiro Takase
    • Takanao OtsukaHirotsugu UedaKeiko FujieHideyuki MuramatsuMichizane HashimotoShigehiro Takase
    • A61K38/00C07K14/00C12N1/21C12P1/04
    • C12R1/01A61K8/99A61K35/74A61K2800/85A61Q5/065A61Q19/00C07G17/00C12P1/06
    • The present invention relates to a new compound useful as a modulator of melanxocortin receptors. In particular, the present invention relates to a compound WS727713, a process for production of the compound by culturing, in a culture medium, a WS727713-producing strain belonging to Pseudonocardia and recovering the compound from a culture broth, a pharmaceutical composition containing the compound, a use of the compound for manufacture of a medicament or a cosmetic for melanocortin receptor modulation, a use of the compound for manufacture of a medicament or a cosmetic for treating or preventing ishemia/reperfusion injury, brain and renal inflammatory diseases, hepatitis, sepsis/septic shock, hypoxic shock, acute respiratory distress syndrome (ARDS), rheumatic arthritis (RA), gouty arthritis, aortic regurgitation (AR), juvenile chronic arthritis, osteoarthritis, nephritis, induction of tolerance, contact hypersensitivity, inflammatory bowel disease (IBD), sexual dysfunction, transplantation, pain, disease progression of HIV, postinflammatory hypopigmentation, tinea versicolor, idiopathic guttate hypomelanosis, fever, functional bowel disease, obesity, satiety effect, diabetes mellitus, modulation of dermal exocrine function, canities (canities circumscripta), gray hair, pancreatitis, fibrotic disorders (hypertrophic scars, keloids, localized scleroderma, systematic sclerosis, sclerodermic graft versus host disease of the skin, cirrhosis of the liver, idiopathic and bleomycin induced lung fibrosis, cyclosporin induced nephropathy), uveitis (especially in Behçet's syndrome and sarcoidosis), vasculitis, microbial infections, celiac disease, vulvar vestibulitis syndrome, melonoma invasion, anorexia or the like.
    • 本发明涉及可用作黑皮皮素受体调节剂的新化合物。 特别地,本发明涉及化合物WS727713,该化合物的生产方法是在培养基中培养属于假诺卡氏菌属的WS727713生产菌株并从培养液中回收该化合物,含有该化合物的药物组合物 ,该化合物用于制造用于黑皮质素受体调节的药物或化妆品的用途,该化合物用于制备用于治疗或预防缺血/再灌注损伤,脑和肾炎性疾病,肝炎,败血症的药物或化妆品的用途 /脓毒性休克,缺氧休克,急性呼吸窘迫综合征(ARDS),风湿性关节炎(RA),痛风性关节炎,主动脉瓣反流(AR),青少年慢性关节炎,骨关节炎,肾炎,耐受诱导,接触性超敏反应,炎性肠病 ),性功能障碍,移植,疼痛,艾滋病病毒进展,炎性色素沉着,花斑斑, 乳糜泻黄斑病,发热,功能性肠病,肥胖症,饱腹感,糖尿病,皮肤外分泌功能的调节,阴毛(canence circumscripta),灰白色头发,胰腺炎,纤维化疾病(肥大性瘢痕,瘢痕疙瘩,局部硬皮病,系统性硬化症,硬皮病 皮肤移植物抗宿主病,肝硬化,特发性和博来霉素引起的肺纤维化,环孢菌素诱导的肾病),葡萄膜炎(尤其是Behçet综合征和结节病),血管炎,微生物感染,乳糜泻,外阴前庭炎综合征,美黄酮侵袭, 厌食症等。