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    WF14573 or its salt, production thereof and use thereof
    1.
    发明授权
    WF14573 or its salt, production thereof and use thereof 失效
    WF14573或其盐，其制备及其用途

    公开(公告)号：US06730776B1

    公开(公告)日：2004-05-04

    申请号：US09646342

    申请日：2000-09-18

    申请人： Yasuhiro Hori ,  Shigehiro Takase ,  Yasuhisa Tsurumi ,  Michizane Hashimoto ,  Motohiro Hino

    发明人： Yasuhiro Hori ,  Shigehiro Takase ,  Yasuhisa Tsurumi ,  Michizane Hashimoto ,  Motohiro Hino

    IPC分类号： C07K750

    CPC分类号： C07K7/56 ,  A61K38/00

    摘要： The present invention provides a new antimicrobial compound WF14573, and a process for producing WF14573 by (a) culturing a WF14573A and/or B-producing microorganism in a nutrient medium and recovering WF14573A and/or B from the resultant cultured broth or (b) deacylating WF14573A and/or B in the presence of a microbial substance which is capable of deacylating WF14573A and/or B. Also provided are an antimicrobial agent comprising WF14573 and carrier(s), a pharmaceutical composition comprising an effective amount of WF14573 and pharmaceutically acceptable carrier(s), a method for killing microorganisms by applying WF14573 to the microorganisms, and use of WF14573 for the treatment of infectious diseases caused by pathogenic microorganisms.

    摘要翻译： 本发明提供了一种新的抗微生物化合物WF14573，以及（a）在营养培养基中培养WF14573A和/或产生B生物的微生物并从所得培养液中回收WF14573A和/或B或（b）生产WF14573的方法， 在能够脱酰基WF14573A和/或B的微生物物质存在下脱酰基WF14573A和/或B。还提供了包含WF14573和载体的抗微生物剂，包含有效量的WF14573和药学上可接受的药物组合物 载体，通过向微生物施用WF14573杀死微生物的方法，以及使用WF14573来治疗由病原微生物引起的感染性疾病。

    Compound Ws727713
    3.
    发明申请
    Compound Ws727713 失效
    化合物Ws727713

    公开(公告)号：US20070254829A1

    公开(公告)日：2007-11-01

    申请号：US11547729

    申请日：2005-03-22

    申请人： Takanao Otsuka ,  Hirotsugu Ueda ,  Keiko Fujie ,  Hideyuki Muramatsu ,  Michizane Hashimoto ,  Shigehiro Takase

    发明人： Takanao Otsuka ,  Hirotsugu Ueda ,  Keiko Fujie ,  Hideyuki Muramatsu ,  Michizane Hashimoto ,  Shigehiro Takase

    IPC分类号： A61K38/00 ,  C07K14/00 ,  C12N1/21 ,  C12P1/04

    CPC分类号： C12R1/01 ,  A61K8/99 ,  A61K35/74 ,  A61K2800/85 ,  A61Q5/065 ,  A61Q19/00 ,  C07G17/00 ,  C12P1/06

    摘要： 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.

    摘要翻译： 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。

    Compound WS 727713
    4.
    发明授权
    Compound WS 727713 有权
    化合物WS 727713

    公开(公告)号：US08133713B2

    公开(公告)日：2012-03-13

    申请号：US12757684

    申请日：2010-04-09

    申请人： Takanao Otsuka ,  Hirotsugu Ueda ,  Keiko Fujie ,  Hideyuki Muramatsu ,  Michizane Hashimoto ,  Shigehiro Takase

    发明人： Takanao Otsuka ,  Hirotsugu Ueda ,  Keiko Fujie ,  Hideyuki Muramatsu ,  Michizane Hashimoto ,  Shigehiro Takase

    IPC分类号： C12N1/12 ,  C12N1/00

    CPC分类号： C12R1/01 ,  A61K8/99 ,  A61K35/74 ,  A61K2800/85 ,  A61Q5/065 ,  A61Q19/00 ,  C07G17/00 ,  C12P1/06

    摘要： The present invention relates to a new compound useful as a modulator of melanocortin 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 dysfuntion, 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, melonozna invasion, anorexia or the like.

    摘要翻译： 本发明涉及可用作黑皮质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，艾滋病病毒发展，炎症色素沉着过度，花斑癣， 慢性淋巴细胞性黄斑病，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，canities（canence circumscripta），灰发，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（特别是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，疟原虫入侵， 厌食症等。

    COMPOUND WS 727713
    5.
    发明申请
    COMPOUND WS 727713 有权
    化合物WS 727713

    公开(公告)号：US20100297735A1

    公开(公告)日：2010-11-25

    申请号：US12757684

    申请日：2010-04-09

    申请人： Takanao Otsuka ,  Hirotsugu Ueda ,  Keiko Fujie ,  Hideyuki Muramatsu ,  Michizane Hashimoto ,  Shigehiro Takase

    发明人： Takanao Otsuka ,  Hirotsugu Ueda ,  Keiko Fujie ,  Hideyuki Muramatsu ,  Michizane Hashimoto ,  Shigehiro Takase

    IPC分类号： C12N1/20

    CPC分类号： C12R1/01 ,  A61K8/99 ,  A61K35/74 ,  A61K2800/85 ,  A61Q5/065 ,  A61Q19/00 ,  C07G17/00 ,  C12P1/06

    摘要： The present invention relates to a new compound useful as a modulator of melanocortin 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 infammatory 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 dysfuntion, 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, melonozna invasion, anorexia or the like.

    摘要翻译： 本发明涉及可用作黑皮质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，脑和肾脏炎症性疾病，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，炎性色素沉着减轻，花斑癣，特发性 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，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（特别是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，疟原虫入侵， 厌食症等。

    Cyclic peptide nuclei and derivatives thereof
    9.
    发明授权
    Cyclic peptide nuclei and derivatives thereof 失效
    环状肽核及其衍生物

    公开(公告)号：US5952299A

    公开(公告)日：1999-09-14

    申请号：US913365

    申请日：1997-09-29

    申请人： Michizane Hashimoto ,  Nobuharu Shigematsu ,  Seiji Hashimoto

    发明人： Michizane Hashimoto ,  Nobuharu Shigematsu ,  Seiji Hashimoto

    IPC分类号： A61K38/00 ,  A61P31/00 ,  C07K1/02 ,  C07K1/06 ,  C07K1/12 ,  C07K7/06 ,  C07K7/08 ,  C07K7/56 ,  C07K11/02 ,  A61K38/12 ,  C07K5/00 ,  C07K7/00

    CPC分类号： C07K7/08 ,  C07K7/56 ,  A61K38/00 ,  Y02P20/55

    摘要： New peptide compounds of the formula: ##STR1## wherein R.sup.1 is alkyl or aralkyl,R.sup.2 is amino(lower)alkyl or protected amino(lower)alkyl,R.sup.3 is hydroxy, protected hydroxy, amino or protected amino,R.sup.4 is hydroxy, orR.sup.3 and R.sup.4 are linked together to form --Z-- (in which --Z-- is --O-- or --NH--), andR.sup.5 is hydrogen or an amino protective group,R.sup.6 is hydroxy, orR.sup.5 and R.sup.6 are linked together to form bond,with proviso thatwhenR.sup.3 is hydroxy, protected hydroxy, amino or protected amino andR.sup.4 is hydroxy,then R.sup.5 and R.sup.6 are linked together to form bond,and a pharmaceutically acceptable salt thereof, which is useful as a medicament.

    摘要翻译： PCT No.PCT / JP96 / 00774 Sec。 371日期：1997年9月29日 102（e）1997年9月29日PCT PCT 1996年3月26日PCT公布。 WO96 / 30399 PCT出版物 日期1996年10月3日新的下式化合物：其中R1是烷基或芳烷基，R2是氨基（低级）烷基或被保护的氨基（低级）烷基，R3是羟基，被保护的羟基，氨基或被保护的氨基，R4是羟基， 或R 3和R 4连接在一起形成-Z-（其中-Z-为-O-或-NH-），并且R5为氢或氨基保护基，R6为羟基，或R5和R6连接在一起至 形成键，条件是当R3为羟基时，被保护的羟基，氨基或被保护的氨基，R4为羟基，则R5和R6连接在一起形成键，并且其药学上可接受的盐可用作药物。