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    • 75. 发明申请
    • Parenteral Combination Therapy For Infective Conditions With Drug Resistant Bacterium
    • 肠胃外联合治疗用于耐药细菌的感染条件
    • US20080188403A1
    • 2008-08-07
    • US11816179
    • 2006-02-08
    • Manu Chaudhary
    • Manu Chaudhary
    • A61K38/14
    • A61K45/06A61K31/546Y02A50/401Y02A50/402Y02A50/406Y02A50/471Y02A50/473Y02A50/475Y02A50/478Y02A50/479Y02A50/481Y02A50/483A61K2300/00
    • The invention describes a pharmaceutical composition to combat multiple-drug-resistant bacteria in non-ocular infective conditions. Compositions comprising glycopeptides, in particular vancomycin, and cephalosporins, in particular ceftriaxone, are disclosed. Such compositions are found to be useful for parenteral administration for hospitalized patients with serious infections. Specifically, this invention also discloses a pharmaceutical composition further including an excipient such as CVMC agent and is available in dry powder form for reconstitution before injection with a suitable solvent. The pharmaceutical compositions of this invention have been found normally to enhance resistance to precipitation in solutions to be administered parenterally. The invention also gives details of the dosage forms stored in sealed containers to be reconstituted before use. The invention further provides a process to manufacture these compositions and also a method of treating a subject having non-ocular infective conditions due to multi drug resistant bacterium.
    • 本发明描述了用于在非眼部感染性病症中对抗多重耐药细菌的药物组合物。 公开了包含糖肽,特别是万古霉素和头孢菌素,特别是头孢曲松的组合物。 发现这种组合物对于严重感染的住院患者的肠胃外给药是有用的。 具体地说,本发明还公开了一种药物组合物,其进一步包括赋形剂如CVMC剂,并且可以以干粉形式获得,以在注射之前用合适的溶剂进行重新配制。 已经发现本发明的药物组合物通常用于增强肠胃外给药的溶液中的沉淀抗性。 本发明还提供储存在使用前重新配制的密封容器中的剂型的细节。 本发明还提供了制造这些组合物的方法,还提供了一种治疗由于多药耐药细菌引起的非眼部感染病症的受试者的方法。
    • 77. 发明申请
    • Polymyxin B analogs for LPS detoxification
    • 多粘菌素B类似物用于LPS解毒
    • US20060281684A1
    • 2006-12-14
    • US11398915
    • 2006-04-06
    • Massimo PorroMassimo VelucchiAlessandro RusticiMonique MoreauNoelle MistrettaTino Krell
    • Massimo PorroMassimo VelucchiAlessandro RusticiMonique MoreauNoelle MistrettaTino Krell
    • A61K38/10A61K38/08C07K7/08C07K7/06
    • C07K7/08A61K38/00C07K7/06C07K7/54Y02A50/471Y02A50/473Y02A50/475Y02A50/478Y02A50/481Y02A50/483
    • The invention relates to SAEP II peptide dimers that mimic polymyxin B i.a. in its ability to bind non-covalently the lipopolysaccharide (LPS) of Gram-negative bacteria with high affinity, and therefore to detoxify LPS as polymyxin B does. The dimeric structure is maintained by a pair of disulphide bonds involving the two cystein residues present in the peptide sequence, which does not exceed 17 amino acids and essentially comprises cationic and hydrophobic amino acid residues. In the dimers of the invention, peptides may have a parallel or anti-parallel orientation. As a matter of example, a dimer of the invention is constituted by a peptide of formula NH2-Lys-Thr-Lys-Cysl-Lys-Phe-Leu-Leu-Leu-Cys2-COOH, either in a parallel or antiparallel dimeric form. SAEP II dimers are useful for treating or preventing septic shock and related disorders generated by Gram-negative bacteria infection. The invention also relates to LPS-peptide complexes in which LPS and SAEP II diners are non-covalently bound together. These complexes are useful as vaccinal agents against Gram-negative bacteria infection.
    • 本发明涉及模拟多粘菌素B i.a.的SAEP II肽二聚体。 在其以高亲和力非共价结合革兰氏阴性细菌的脂多糖(LPS)的能力,因此使LPS作为多粘菌素B解毒。 二聚体结构通过涉及肽序列中存在的两个半胱氨酸残基的一对二硫键来维持,其不超过17个氨基酸并且基本上包含阳离子和疏水氨基酸残基。 在本发明的二聚体中,肽可以具有平行或反平行取向。 作为实例,本发明的二聚体由式NH2-Lys-Thr-Lys-Cys1-Lys-Phe-Leu-Leu-Leu-Leu-Cys2-COOH的肽构成,以平行或反向平行的二聚体形式 。 SAEP II二聚体可用于治疗或预防由革兰氏阴性菌感染引起的败血性休克和相关疾病。 本发明还涉及其中LPS和SAEP II食用者非共价结合在一起的LPS-肽复合物。 这些复合物可用作抗革兰氏阴性菌感染的疫苗。