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    • 13. 发明授权
    • Chiral synthesis of alpha-aminophosponic acids
    • α-氨基磷酸的手性合成
    • US5362899A
    • 1994-11-08
    • US120007
    • 1993-09-09
    • David A. Campbell
    • David A. Campbell
    • C07F9/40
    • C07F9/4006
    • A stereospecific method of preparing alpha-aminophosphonic acids and derivatives thereof is provided. A protected amino acid is converted to a acyl aroyl or diacyl peroxide which spontaneously rearranges to form an alpha-amino ester. This rearrangement occurs stereospecifically with retention of configuration. The ester is subsequently converted to an appropriate leaving group and displaced with a phosphite yielding a chiral alpha-aminophosphonic acid or derivative.Alpha-aminophosphonic acids are useful for the synthesis of peptide analogs that possess a phosphonate linkage in the place of an amide linkage. This substitution can impart protease resistance in therapeutic peptides thereby increasing the serum half-life.
    • 提供了制备α-氨基膦酸及其衍生物的立体特异性方法。 被保护的氨基酸被转化为酰基芳酰基或二酰基过氧化物,其自发重排以形成α-氨基酯。 这种重排立体特异性地保留配置。 随后将酯转化为合适的离去基团,并用亚磷酸酯置换,得到手性α-氨基膦酸或衍生物。 α-氨基膦酸可用于合成具有代替酰胺键的膦酸酯键的肽类似物。 该取代可以在治疗性肽中赋予蛋白酶抗性,从而增加血清半衰期。
    • 15. 发明授权
    • Vaccines for equine influenza
    • 马流感疫苗
    • US4693893A
    • 1987-09-15
    • US596447
    • 1984-04-03
    • David A. Campbell
    • David A. Campbell
    • A01N63/00A61K39/145C12N7/00C12N7/02C12N7/04A61K39/155A61K39/295
    • C12N7/00A61K39/12A61K39/145A61K2039/5252A61K2039/5256A61K2039/552A61K2039/55505A61K2039/55544C12N2760/16134C12N2760/16151
    • It is known that the human influenza virus strain A/Puerto Rico/8/34 grows particularly well in eggs and that reassorted viruses having it as a parent may also grow well in eggs. It has now been found that certain reassortants of A/PR/8/34 and equine influenza viruses, namely those which comprise the RNA7 segment from A/PR/8/34, will grow in cell culture, even though the parent equine influenza vius will not.Thus the specification describes and claims: reassorted viruses comprising genes for surface antigens of equine influenza viruses and the RNA7 segment from A/PR/8/34; methods of obtaining such viruses by reassortment; methods of propagating such reassorted viruses in cell culture, especially Vero cells; vaccines against equine influenza comprising such reassorted viruses; and methods of vaccinating equines against influenza.
    • 已知人类流感病毒株A /波多黎各/ 8/34在卵中生长特别好,并且将其作为亲本的病毒重新配制也可以在鸡蛋中生长良好。 现在已经发现,A / PR / 8/34和马流感病毒的某些重配体,即包含A / PR / 8/34的RNA7片段的重组将在细胞培养物中生长,即使母体马流感病毒 将不会。 因此,本说明书描述和权利要求:重新组合的病毒,其包含马流感病毒表面抗原的基因和来自A / PR / 8/34的RNA7区段; 通过重配获得此类病毒的方法; 在细胞培养物中繁殖这种重配病毒的方法,特别是Vero细胞; 针对马流感疫苗的疫苗,包括重新接种的病毒; 和针对流感的马接种疫苗的方法。