OCTAPEPTIDE ANALOGS OF SOMATOSTATIN HAVING THREONINE AT THE SIXTH POSITION
    103.
    发明授权
    OCTAPEPTIDE ANALOGS OF SOMATOSTATIN HAVING THREONINE AT THE SIXTH POSITION 失效
    生长抑素OKTAPEPTIDANALOGE在位置6苏氨酸

    公开(公告)号:EP0457888B1

    公开(公告)日:1996-07-10

    申请号:EP91901181.7

    申请日:1990-12-04

    IPC分类号: C07K14/655 A61K38/16

    摘要: A compound of the formula: wherein each A1 and A2, independently, is H, C1-12 alkyl, C7-10 phenylalkyl, R1CO (where R1 is C1-20 alkyl, C3-20 alkenyl, C3-20 alkinyl, phenyl, naphthyl, or C7-10 phenylalkyl), or R2OCO (where R2 is C1-10 alkyl or C7-10 phenylalkyl), provided that when one of A1 or A2 is R1CO or R2OCO, the other must be H; each X1 and X2, independently, is H, F, Cl, Br, OH, CH3, or CF3, provided that at least one of X1 and X2 must be H; A3 is Phe or Tyr; and A4 is OH, NH2, or NH-R3 (wherein R3 is a saturated aliphatic C1-8 alkyl); or a pharmaceutically acceptable salt thereof. A therapeutic composition containing the compound of the present invention and a method of using the same are also described.

    Antisense oligonucleotides complementary to the macromolecular synthesis operon of bacteria, and their uses in diagnosis and therapy
    106.
    发明公开
    Antisense oligonucleotides complementary to the macromolecular synthesis operon of bacteria, and their uses in diagnosis and therapy 失效
    细菌的大分子合成操作的反义寡核苷酸及其在诊断和治疗中的用途

    公开(公告)号:EP0472434A3

    公开(公告)日:1993-06-09

    申请号:EP91307750.9

    申请日:1991-08-22

    摘要: A method of treating bacterial infections comprising the step of interrupting the expression of a macromolecular synthesis operon in bacteria by hybridizing an antisense oligonucleotide to a single stranded DNA or to a mRNA transcribed from the macromolecular synthesis operon. The antisense oligonucleotide can be either sequence specific to a unique intergenic sequence or a sequence specific to a bacterial homologous sequence. By interrupting the expression of the macromolecular synthesis operon bacterial infections can be treated. Specific antisense oligonucleotides and macromolecular synthesis operon sequences are disclosed. The ability of the antisense oligonucleotide to bind the mRNA or single stranded DNA also allows the identification of the bacteria by using a unique intergenic antisense oligonucleotide to bind to the single stranded DNA or to the mRNA transcribed from the macromolecular synthesis operon. A method for competitively inhibiting the protein products of the MMS operon with oligonucleotides is also disclosed. Methods of identifying unique intergenic sequence is also disclosed.