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    Derivatives of virginiamycin M1
    1.
    发明授权
    Derivatives of virginiamycin M1 失效
    维吉尼亚霉素M1的衍生物

    公开(公告)号：US5242938A

    公开(公告)日：1993-09-07

    申请号：US937075

    申请日：1992-08-27

    申请人： Yiu-Kuen T. Lam

    发明人： Yiu-Kuen T. Lam

    IPC分类号： C07D498/18

    CPC分类号： C07D498/18

    摘要： Dicarbonyloxy, carbonyloxy, carbanilate, and dihydroxy derivatives of Virginiamycin M.sub.1 are useful antibiotics and effectively bind gastrin and brain CCK receptors.

    摘要翻译： 弗吉尼亚霉素M1的二羰基氧基，羰基氧基，氨基苯甲酸酯和二羟基衍生物是有用的抗生素，并有效地结合胃泌素和脑CCK受体。

    Fermentation analogs of virginiamycin M.sub.1
    2.
    发明授权
    Fermentation analogs of virginiamycin M.sub.1 失效
    维吉尼亚霉素M1的发酵类似物

    公开(公告)号：US5006466A

    公开(公告)日：1991-04-09

    申请号：US426836

    申请日：1989-10-26

    申请人： Yiu-kuen T. Lam ,  Otto D. Hensens ,  Raymond S. Chang ,  Cheryl D. Schwartz ,  Deborah L. Zink

    发明人： Yiu-kuen T. Lam ,  Otto D. Hensens ,  Raymond S. Chang ,  Cheryl D. Schwartz ,  Deborah L. Zink

    IPC分类号： A61K38/00 ,  C07K5/078 ,  C12P17/18

    CPC分类号： C12R1/58 ,  C07K5/06139 ,  C12P17/188 ,  A61K38/00 ,  Y10S435/886 ,  Y10S435/902

    摘要： Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527, while the analog of Formula II is produced by chemical synthesis.

    摘要翻译： 维生素B1，具有下式的维他明霉素M1：具有式I-IV的维吉尼好霉素M1类似物：（I）图像（III） -IV是胆囊收缩素（CCK）和胃泌素的拮抗剂。 胆囊收缩素拮抗剂可用作止痛剂和用于治疗和预防动物，特别是人类的胃肠道，中枢神经和食欲调节系统的紊乱。 胃泌素拮抗剂可用于阻断人类胃泌素受体，并且可用作治疗溃疡，肿瘤或其它胃肠道疾病的药剂。 式I-IV的化合物是抗生素，并且可用作包括人在内的动物的抗微生物剂，并且可用作促进动物饲料利用的食品添加剂。 弗吉尼亚霉素M1和式I，III和IV的类似物是通过控制好氧发酵链霉菌链霉菌ATCC No.55327产生的，而式II的类似物是通过化学合成制备的。

    Process for preparing synthetic virginiamycin M.sub.1 analogs
    3.
    发明授权
    Process for preparing synthetic virginiamycin M.sub.1 analogs 失效
    合成维拉霉素M1类似物的制备方法

    公开(公告)号：US4942230A

    公开(公告)日：1990-07-17

    申请号：US365324

    申请日：1989-06-13

    申请人： Yiu-kuen T. Lam ,  Raymond S. Chang

    发明人： Yiu-kuen T. Lam ,  Raymond S. Chang

    IPC分类号： A61K38/00 ,  C07K5/078 ,  C12P17/18

    CPC分类号： C12R1/58 ,  C07K5/06139 ,  C12P17/188 ,  A61K38/00

    摘要： Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, II and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527, while the analog of Formula II is produced by chemical synthesis.

    摘要翻译： 维生素B1，具有下式的维他明霉素M1：具有式I-IV的维吉尼好霉素M1类似物：（I）图像（III） -IV是胆囊收缩素（CCK）和胃泌素的拮抗剂。 胆囊收缩素拮抗剂可用作止痛剂和用于治疗和预防动物，特别是人类的胃肠道，中枢神经和食欲调节系统的紊乱。 胃泌素拮抗剂可用于阻断人类胃泌素受体，并且可用作治疗溃疡，肿瘤或其它胃肠道疾病的药剂。 式I-IV的化合物也是抗生素，并且可用作包括人在内的动物的抗微生物剂，并且可用作促进动物饲料利用的食品添加剂。 弗吉尼亚霉素M1和式I，II和IV的类似物通过对链霉菌链霉菌ATCC No.55327的受控好氧发酵产生，而式II的类似物通过化学合成制备。

    Therapeutic virginiamycin M.sub.1 analogs
    4.
    发明授权
    Therapeutic virginiamycin M.sub.1 analogs 失效
    治疗维吉尼亚霉素M1类似物

    公开(公告)号：US4859690A

    公开(公告)日：1989-08-22

    申请号：US934212

    申请日：1986-11-21

    申请人： Yiu-kuen T. Lam ,  Raymond S. Chang ,  Otto D. Hensens ,  Cheryl D. Schwartz ,  Deborah L. Zink

    发明人： Yiu-kuen T. Lam ,  Raymond S. Chang ,  Otto D. Hensens ,  Cheryl D. Schwartz ,  Deborah L. Zink

    IPC分类号： A61K38/00 ,  C07K5/078 ,  C12P17/18

    CPC分类号： C12R1/58 ,  C07K5/06139 ,  C12P17/188 ,  A61K38/00

    摘要： Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527. The analog of Formula II is produced by chemical synthesis.

    摘要翻译： （I）图像（III）（IV）维他命霉素M1和类似物I -IV是胆囊收缩素（CCK）和胃泌素的拮抗剂。 胆囊收缩素拮抗剂可用作止痛剂和用于治疗和预防动物，特别是人类的胃肠道，中枢神经和食欲调节系统的紊乱。 胃泌素拮抗剂可用于阻断人类胃泌素受体，并且可用作治疗溃疡，肿瘤或其它胃肠道疾病的药剂。 式I-IV的化合物也是抗生素，并且可用作包括人在内的动物的抗微生物剂，并且可用作促进动物饲料利用的食品添加剂。 维生素霉素M1和式I，III和IV的类似物是通过控制好氧发酵的链霉菌链霉菌ATCC No.55327产生的。式II的类似物是通过化学合成制备的。

    Synthetic virginiamycin M1 analogs
    7.
    发明授权
    Synthetic virginiamycin M1 analogs 失效
    合成维吉尼亚霉素M1类似物

    公开(公告)号：US4772595A

    公开(公告)日：1988-09-20

    申请号：US934232

    申请日：1986-11-21

    申请人： Yiu-kuen T. Lam ,  Raymond S. Chang

    发明人： Yiu-kuen T. Lam ,  Raymond S. Chang

    IPC分类号： A61K38/00 ,  C07K5/078 ,  C12P17/18 ,  A61K31/33 ,  C07D498/12

    CPC分类号： C12R1/58 ,  C07K5/06139 ,  C12P17/188 ,  A61K38/00

    摘要： Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527, while the analog of Formula II is produced by chemical synthesis.

    摘要翻译： 维生素B1，具有下式的维他明霉素M1：具有式I-IV的维吉尼好霉素M1类似物：（I）图像（III） -IV是胆囊收缩素（CCK）和胃泌素的拮抗剂。 胆囊收缩素拮抗剂可用作止痛剂和用于治疗和预防动物，特别是人类的胃肠道，中枢神经和食欲调节系统的紊乱。 胃泌素拮抗剂可用于阻断人类胃泌素受体，并且可用作治疗溃疡，肿瘤或其它胃肠道疾病的药剂。 式I-IV的化合物也是抗生素，并且可用作包括人在内的动物的抗微生物剂，并且可用作促进动物饲料利用的食品添加剂。 弗吉尼亚霉素M1和式I，III和IV的类似物是通过控制好氧发酵链霉菌链霉菌ATCC No.55327产生的，而式II的类似物是通过化学合成制备的。

    Fermentation analogs of virginiamycin M1
    8.
    发明授权
    Fermentation analogs of virginiamycin M1 失效
    维吉尼亚霉素M1的发酵类似物

    公开(公告)号：US4762923A

    公开(公告)日：1988-08-09

    申请号：US934231

    申请日：1986-11-21

    申请人： Yiu-Kuen T. Lam ,  Raymond S. Chang ,  Otto D. Hensens ,  Cheryl D. Schwartz ,  Deborah L. Zink

    发明人： Yiu-Kuen T. Lam ,  Raymond S. Chang ,  Otto D. Hensens ,  Cheryl D. Schwartz ,  Deborah L. Zink

    IPC分类号： A61K31/41 ,  A61K38/00 ,  A61K38/55 ,  A61P1/00 ,  A61P25/00 ,  C07D498/04 ,  C07K5/078 ,  C12P17/18 ,  C12R1/58 ,  C07D498/16 ,  A61K31/42 ,  C12P17/14

    CPC分类号： C12R1/58 ,  C07K5/06139 ,  C12P17/188 ,  A61K38/00

    摘要： Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III, and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No. 53527, while the analog of Formula II is produced by chemical synthesis.

    摘要翻译： 维生素B1，具有下式的维他明霉素M1：具有式I-IV的维吉尼好霉素M1类似物：（I）图像（III） -IV是胆囊收缩素（CCK）和胃泌素的拮抗剂。 胆囊收缩素拮抗剂可用作止痛剂和用于治疗和预防动物，特别是人类的胃肠道，中枢神经和食欲调节系统的紊乱。 胃泌素拮抗剂可用于阻断人类胃泌素受体，并且可用作治疗溃疡，肿瘤或其它胃肠道疾病的药剂。 式I-IV的化合物也是抗生素，并且可用作包括人在内的动物的抗微生物剂，并且可用作促进动物饲料利用的食品添加剂。 维生素霉素M1和式I，III和IV的类似物通过对链霉菌链霉菌ATCC No.55327的受控好氧发酵产生，而式II的类似物通过化学合成产生。

    Antihypertensive compounds produced by fermentation
    9.
    发明授权
    Antihypertensive compounds produced by fermentation 失效
    通过发酵产生的抗高血压化合物

    公开(公告)号：US5240910A

    公开(公告)日：1993-08-31

    申请号：US870065

    申请日：1992-04-17

    申请人： Yiu-Kuen T. Lam ,  Deborah L. Zink ,  David L. Williams, Jr.

    发明人： Yiu-Kuen T. Lam ,  Deborah L. Zink ,  David L. Williams, Jr.

    IPC分类号： A61K38/00 ,  C07K7/06

    CPC分类号： C07K7/06 ,  A61K38/00

    摘要： Novel cyclic depsipeptides derived from a culture of Microbispora are antagonists of the receptor for endothelin, a potent vasoconstrictor, and are thus useful in treating cardiovascular disorders. Endothelin has other physiological effects, and the endothelin receptor antagonists of the present invention thus also have other therapeutic uses. The compounds are cyclical depsipeptides of N-(pyrrol-2-carboxy) - L-phe, D-allo-Thr, D-Phe, D-Ala, D- or L-dihydroxyphenyl-Gly, and D-dihydroxyphenyl-Gly.

    摘要翻译： 衍生自微生物双孢子培养物的新型环状缩酚酸肽是内皮素受体的拮抗剂，其是有效的血管收缩剂，因此可用于治疗心血管疾病。 内皮素具有其他生理作用，因此本发明的内皮素受体拮抗剂也具有其它治疗用途。 化合物是N-（吡咯-2-羧基）-L-phe，D-allo-Thr，D-Phe，D-Ala，D或L-二羟基苯基-Gly和D-二羟基苯基-Gly的循环衰减肽。