公开(公告)号：US5187074A

公开(公告)日：1993-02-16

申请号：US840601

申请日：1992-02-20

申请人： Laszlo R. Treiber ,  Russell B. Lingham ,  Byron H. Arison ,  Lawrence F. Colwell, Jr. ,  Georgette Dezeny ,  Nancy E. Kohl

发明人： Laszlo R. Treiber ,  Russell B. Lingham ,  Byron H. Arison ,  Lawrence F. Colwell, Jr. ,  Georgette Dezeny ,  Nancy E. Kohl

IPC分类号： C07D295/092 ,  C12P17/14

CPC分类号： C07D295/088 ,  C12P17/14

摘要： A novel dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

摘要翻译： 新型二肽等排物是与Streptomyces培养物孵育后的生物转化产物。 它可以抑制HIV蛋白酶，并且可用作预防或治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是作为前药还是作为与其它抗病毒药物的组合， 抗感染药，免疫调节剂，抗生素或疫苗。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

公开(公告)号：US5192668A

公开(公告)日：1993-03-09

申请号：US842814

申请日：1992-02-27

申请人： Laszlo R. Treiber ,  Lawrence F. Colwell, Jr. ,  Byron H. Arison ,  Georgette Dezeny ,  Russell B. Lingham ,  Wayne J. Thompson ,  Suresh K. Balani

发明人： Laszlo R. Treiber ,  Lawrence F. Colwell, Jr. ,  Byron H. Arison ,  Georgette Dezeny ,  Russell B. Lingham ,  Wayne J. Thompson ,  Suresh K. Balani

IPC分类号： C07C271/22 ,  C12P13/02 ,  C12P21/04

CPC分类号： C07C271/22 ,  C12P13/02

摘要： A dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

摘要翻译： 二肽等体积是与Streptomyces培养物孵育后的生物转化产物。 它可以抑制HIV蛋白酶，并且可用作预防或治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是作为前药还是作为与其它抗病毒药物的组合， 抗感染药，免疫调节剂，抗生素或疫苗。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

公开(公告)号：US5225403A

公开(公告)日：1993-07-06

申请号：US720550

申请日：1991-06-25

申请人： Laszlo R. Treiber ,  Georgette Dezeny ,  Lawrence F. Colwell, Jr. ,  Byron H. Arison ,  Francis Dumont

发明人： Laszlo R. Treiber ,  Georgette Dezeny ,  Lawrence F. Colwell, Jr. ,  Byron H. Arison ,  Francis Dumont

IPC分类号： A61K31/435 ,  C07D498/18 ,  C12P17/18

CPC分类号： C07D498/18 ,  A61K31/435 ,  C12P17/188 ,  C12R1/55 ,  Y10S435/886 ,  Y10S435/898

摘要： Described is a process for producing a new FK-506 antagonist agent, a C-21 hydroxylated analog of FR-900520 under novel fermentation conditions utilizing the novel microorganism, Streptomyces hygroscopicus (Merck Culture Collection MA 6832) ATCC No. 55166. The macrolide antagonist is useful in preventing and/or counteracting accidental or inadvertent FK-506 overdosage in an FK-506 therapeutic program designed to prevent autoimmune diseases or human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

摘要翻译： 描述了在新型发酵条件下利用新型微生物吸水链霉菌（Streptomyces hygroscopicus）（Merck Culture Collection MA 6832）ATCC No.555166生产新的FK-506拮抗剂，FR-900520的C-21羟基化类似物的方法。大环内酯拮抗剂 可用于预防和/或抵制在FK-506治疗计划中意外或无意的FK-506过量剂量，其旨在防止自身免疫性疾病或人类宿主排斥外来器官移植，例如 骨髓，肝，肺，肾和心脏移植。

公开(公告)号：US5273979A

公开(公告)日：1993-12-28

申请号：US738997

申请日：1991-08-01

申请人： Shieh-Shung T. Chen ,  Raymond F. White ,  Georgette Dezeny ,  Byron H. Arison ,  Thomas R. Beattie ,  Amy M. Hale ,  Francis Dumont

发明人： Shieh-Shung T. Chen ,  Raymond F. White ,  Georgette Dezeny ,  Byron H. Arison ,  Thomas R. Beattie ,  Amy M. Hale ,  Francis Dumont

IPC分类号： A61K31/445 ,  A61P37/06 ,  C07D498/22 ,  C07H19/01 ,  C12N1/20 ,  C12P17/18 ,  C12P19/44 ,  C12R1/56 ,  A61K31/395 ,  C07D491/16

CPC分类号： C12P19/445 ,  C07H19/01

摘要： Described is a process for producing a new immunosuppressant, a C-31 desmethyl, C-19/C-22 cyclic hemiketal biotransformation analog (Compound I) of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces, lavendulae ATCC No. 55209. Also disclosed is the C-31 methylated derivative (Compound II) of Compound I produced by enzymatic methylation using 31-O-desmethylimmunomycin O-methyl transferase, (DIMT), a methyl transferase enzyme. The macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

公开(公告)号：US5221625A

公开(公告)日：1993-06-22

申请号：US818936

申请日：1992-01-10

申请人： Shieh-Shung T. Chen ,  Raymond F. White ,  Georgette Dezeny ,  Brian R. Petuch ,  George M. Garrity ,  Byron H. Arison ,  Amy M. Bernick

发明人： Shieh-Shung T. Chen ,  Raymond F. White ,  Georgette Dezeny ,  Brian R. Petuch ,  George M. Garrity ,  Byron H. Arison ,  Amy M. Bernick

IPC分类号： C12P17/16

CPC分类号： C12P17/16 ,  Y10S435/899

摘要： Described is a process for producing a new immunosuppressant, a C-19/C-22 cyclic hemiketal (Compound I) biotransformation analog of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces sp. (Merck Culture Collection MA6963) ATCC No. 55230. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.

摘要翻译： 描述了在新型发酵条件下利用新型微生物Streptomyces sp。生产新的免疫抑制剂，FR-900520的C-19 / C-22环状半缩酮（化合物I）生物转化类似物的方法。 （Merck Culture Collection MA6963）ATCC No.55530。大环内酯类免疫抑制剂可用于预防异种器官移植的人宿主排斥反应。 骨髓，肝，肺，肾和心脏移植。