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    Extract of bacterial macromolecules, a process for its preparation and a pharmaceutical composition containing the same
    2.
    发明授权
    Extract of bacterial macromolecules, a process for its preparation and a pharmaceutical composition containing the same 失效
    细菌大分子的提取物，其制备方法和含有该大分子的药物组合物

    公开(公告)号：US5424287A

    公开(公告)日：1995-06-13

    申请号：US119124

    申请日：1993-09-20

    申请人： Jacques Bauer ,  Pierre Hirt ,  Adrian Schulthess

    发明人： Jacques Bauer ,  Pierre Hirt ,  Adrian Schulthess

    IPC分类号： A61K35/74 ,  A61K38/00 ,  A61P35/00 ,  A61P37/00 ,  C07K1/16 ,  C07K1/34 ,  C07K14/00 ,  C07K14/005 ,  C07K14/195 ,  C07K14/245 ,  C07K14/41 ,  C12P1/00 ,  C12P21/00 ,  C12R1/19

    CPC分类号： C07K14/245 ,  C12P1/00 ,  A61K38/00 ,  Y10S435/822 ,  Y10S435/849 ,  Y10S435/851 ,  Y10S435/852 ,  Y10S435/871 ,  Y10S435/885 ,  Y10S435/886

    摘要： An extract based on modified bacterial proteins includes a mixture of acid bacterial polyanions having a molecular weight in the range from 10,000 to 1,000,000 and an isoelectric point in the range from 2.5 to 5.5, and in which the added weights of the constituent amino acids amount to at least 50% of the extract. The preparation or this protein extract includes a cultivation of bacteria in an aqueous medium and then the alkaline extraction of this bacterial suspension and the purification of the protein extract. The alkaline extraction is carried out in the presence of a dilute aqueous source of OH.sup.- ions and at a stable pH in the range from 11 to 13, the decrease of this pH during the acid extraction not exceeding 0.4. The protein extract thus obtained can be used as an active ingredient in a pharmaceutical composition.

    摘要翻译： PCT No.PCT / CH93 / 00029 Sec。 371日期：1993年9月20日 102（e）1993年9月20日PCT 1993年2月3日提交PCT公布。 出版物WO93 / 16190 日期为1993年8月19日。基于修饰的细菌蛋白质的提取物包括分子量在10,000至1,000,000范围内且等电点在2.5至5.5范围内的酸性细菌聚阴离子的混合物，其中添加重量 的组成氨基酸达到提取物的至少50％。 制备物或该蛋白质提取物包括在水性培养基中培养细菌，然后碱性提取该细菌悬浮液并纯化蛋白质提取物。 碱性萃取在OH-离子水溶液的存在下进行，在11-13的稳定pH范围内，酸萃取时pH值的降低不超过0.4。 由此获得的蛋白质提取物可以用作药物组合物中的活性成分。

    Immunomodulatory compounds and treatment of diseases related to an overproduction of inflammatory cytokines
    5.
    发明授权
    Immunomodulatory compounds and treatment of diseases related to an overproduction of inflammatory cytokines 失效
    免疫调节化合物和与炎症细胞因子过度生成有关的疾病的治疗

    公开(公告)号：US07915240B2

    公开(公告)日：2011-03-29

    申请号：US12279845

    申请日：2007-03-09

    申请人： Jacques Bauer ,  Carlo Chiavaroli ,  Stéphane Moutel

    发明人： Jacques Bauer ,  Carlo Chiavaroli ,  Stéphane Moutel

    IPC分类号： A01N57/00 ,  A61K31/66

    CPC分类号： A61K31/661 ,  A61K31/16 ,  A61K31/221 ,  A61K31/6615 ,  C07F9/091

    摘要： Method of using immunomodulatory compounds for treating diseases related to an overproduction of inflammatory cytokines, including diseases selected from asthma, atopic dermatitis, allergic rhinitis, prostatitis, inflammatory bowel disease, diabetes, and rhumatoid arthritis, the compounds being of general formula (I): wherein: m and n, independently from each other, are an integer ranging from 1 to 4, X and Y represent —COOH, —O—P(O)(OH)2, —O—SO2(OH), —NH2, —OH, —CONH(CH2)n1—NH2, —CO—NH—CH(COOH)—(CH2)n1—COOH, —CO—NH—CH(COOH)—(CH2)n1—NH2, —O—CO—(CH2)n1—NH2, —O—CO—(CH2)n1—CHOH—CH2OH, —O—CO—(CH2)n1—OH, —O—CO—(CH2)n1—COOH, —O—CO—(CH2)n1—CHO, —O—CO—(CH2)n1—NH—CO—(CH2)n2—COOH, R1 and R2 each designate an acyl group derived from a saturated or unsaturated, straight- or branched-chain carboxylic acid having from 2 to 18 carbon atoms, which is unsubstituted or bears one to three substituents selected among hydroxyl, dihydroxyphosphoryloxy, alkyl of 2 to 18 carbon atoms, alkoxy of 2 to 18 carbon atoms, acyloxy of 2 to 18 carbon atoms in the acyl moiety, amino, acylamino.

    摘要翻译： 使用免疫调节化合物治疗与炎性细胞因子过度生成有关的疾病的方法，所述疾病包括选自哮喘，特应性皮炎，过敏性鼻炎，前列腺炎，炎性肠病，糖尿病和类风湿性关节炎的疾病，所述通式（I）的化合物： 其中：m和n彼此独立地为1至4的整数，X和Y表示-COOH，-O-P（O）（OH）2，-O-SO 2（OH），-NH 2， -OH，-CONH（CH2）n1-NH2，-CO-NH-CH（COOH） - （CH2）n1-COOH，-CO-NH-CH（COOH） - （CH2）n1-NH2，-O-CO - （CH2）n1-NH2，-O-CO-（CH2）n1-CHOH-CH2OH，-O-CO-（CH2）n1-OH，-O-CO-（CH2）n1-COOH，-O-CO - （CH2）n1-CHO，-O-CO-（CH2）n1-NH-CO-（CH2）n2-COOH，R1和R2各自表示衍生自饱和或不饱和的直链或支链的酰基 具有2至18个碳原子的羧酸，其是未取代的或带有1-3个选自a的取代基 芳基羟基，二羟基磷酰氧基，碳原子数2〜18的烷基，碳原子数为2〜18的烷氧基，酰基部分为2〜18个碳原子的酰氧基，氨基，酰氨基。

    Immunomodulatory compounds and treatment of diseases related to an overproduction of inflammatory cytokines
    8.
    发明授权
    Immunomodulatory compounds and treatment of diseases related to an overproduction of inflammatory cytokines 失效
    免疫调节化合物和与炎症细胞因子过度生成有关的疾病的治疗

    公开(公告)号：US08618080B2

    公开(公告)日：2013-12-31

    申请号：US13073737

    申请日：2011-03-28

    申请人： Jacques Bauer ,  Carlo Chiavaroli ,  Stephane Moutel

    发明人： Jacques Bauer ,  Carlo Chiavaroli ,  Stephane Moutel

    IPC分类号： A01N57/00 ,  A61K31/66

    CPC分类号： A61K31/661 ,  A61K31/16 ,  A61K31/221 ,  A61K31/6615 ,  C07F9/091

    摘要： Method of using immunomodulatory compounds for treating diseases related to an overproduction of inflammatory cytokines, including diseases selected from asthma, atopic dermatitis, allergic rhinitis, prostatitis, inflammatory bowel disease, diabetes, and rheumatoid arthritis, the compounds being of general formula (I): wherein: m and n, independently from each other, are an integer ranging from 1 to 4, X and Y represent —COON, —O—P(O)(OH)2, —O—S02(OH), —NH2, —OH, —CONH(CH2)n1—NH2, —CO—NH—CH(COOH)—(CH2)n1—COOH, —CO—NH—CH(COOH)—(CH2)n1—NH2, —O—CO—(CH2)n1—NH2, —O—CO—(CH2)n1—CHOH—CH2OH, —O—CO—(CH2)n1—OH, —O—CO—(CH2)n1—COOH, —O—CO—(CH2)n1—CHO, —O—CO—(CH2)n1—NH—CO—(CH2)n2—COOH, R1 and R2 each designate an acyl group derived from a saturated or unsaturated, straight-or branched-chain carboxylic acid having from 2 to 18 carbon atoms, which is unsubstituted or bears one to three substituents selected among hydroxyl, dihydroxyphosphoryloxy, alkyl of 2 to 18 carbon atoms, alkoxy of 2 to 18 carbon atoms, acyloxy of 2 to 18 carbon atoms in the acyl moiety, amino, acylamino.

    摘要翻译： 使用免疫调节化合物治疗与炎性细胞因子过度生成有关的疾病的方法，所述疾病包括选自哮喘，特应性皮炎，过敏性鼻炎，前列腺炎，炎性肠病，糖尿病和类风湿性关节炎的疾病，所述通式（I）的化合物： 其中：m和n彼此独立地为1至4的整数，X和Y表示-COON，-OP（O）（OH）2，-O-SO 2（OH），-NH 2，-OH ，-CONH（CH2）n1-NH2，-CO-NH-CH（COOH） - （CH2）n1-COOH，-CO-NH-CH（COOH） - （CH2）n1-NH2，-O-CO- （CH2）n1-NH2，-O-CO-（CH2）n1-CHOH-CH2OH，-O-CO-（CH2）n1-OH，-O-CO-（CH2）n1-COOH，-O-CO- CH2）n1-CHO，-O-CO-（CH2）n1-NH-CO-（CH2）n2-COOH，R1和R2各自表示衍生自饱和或不饱和的直链或支链羧酸的酰基 具有2至18个碳原子，其是未取代的或带有1-3个选自羟基，二羟基磷酰氧基，2至18个碳原子的烷基，2至18个碳原子的烷氧基 原子，酰基部分中2至18个碳原子的酰氧基，氨基，酰氨基。

    Acyl pseudodipeptides which carry a functionalised auxialiary arm
    9.
    发明授权
    Acyl pseudodipeptides which carry a functionalised auxialiary arm 失效
    载有官能化辅助臂的酰基假二肽

    公开(公告)号：US07799762B2

    公开(公告)日：2010-09-21

    申请号：US10169053

    申请日：2000-12-21

    申请人： Jacques Bauer ,  Olivier Richard Martin ,  Sylvain Rodriguez

    发明人： Jacques Bauer ,  Olivier Richard Martin ,  Sylvain Rodriguez

    IPC分类号： A61K38/00

    CPC分类号： A61K38/04 ,  A61K39/385 ,  A61K47/6811 ,  A61K2039/6018 ,  A61K2039/6037 ,  C07C237/22 ,  C07C323/60 ,  C07F9/091 ,  C07K5/04 ,  Y02A50/412

    摘要： The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state.Compounds of the present invention have immunomodulating properties like adjuvants, In addition, compounds of the invention can be grafted on a given antigen in order to modulate or tune the immune response or can be equally grafted on a pharmaceutical carrier to enhance the therapeutic effect or targeting thereof. Accordingly, compounds of the invention find use in human and veterinary medicine both as immunogens and diagnostic tools.

    摘要翻译： 本发明特别涉及衍生自功能取代的氨基酸的二肽样化合物，其具有通过所述二肽类化合物的胺官能团的酰胺化而结合的脂肪酸链，其一个末端部分具有辅助功能侧链 间隔物，另一端部分为中性或带电状态的酸基。 本发明的化合物具有如佐剂的免疫调节特性。此外，本发明的化合物可以接枝在给定抗原上以调节或调节免疫应答，或者可以同样地接枝在药物载体上以增强治疗效果或靶向 其中。 因此，本发明的化合物可用作人和兽医学作为免疫原和诊断工具。

    Acyl pseudodipeptides which carry a functionalized auxiliary arm
    10.
    发明授权
    Acyl pseudodipeptides which carry a functionalized auxiliary arm 失效
    载有官能化辅助臂的酰基假二肽

    公开(公告)号：US08173133B2

    公开(公告)日：2012-05-08

    申请号：US12640527

    申请日：2009-12-17

    申请人： Jacques Bauer ,  Olivier Martin ,  Sylvain Rodriguez

    发明人： Jacques Bauer ,  Olivier Martin ,  Sylvain Rodriguez

    IPC分类号： A61K39/00

    CPC分类号： A61K38/04 ,  A61K39/385 ,  A61K47/6811 ,  A61K2039/6018 ,  A61K2039/6037 ,  C07C237/22 ,  C07C323/60 ,  C07F9/091 ,  C07K5/04 ,  Y02A50/412

    摘要： The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state.Compounds of the present invention have immunomodulating properties like adjuvants, In addition, compounds of the invention can be grafted on a given antigen in order to modulate or tune the immune response or can be equally grafted on a pharmaceutical carrier to enhance the therapeutic effect or targeting thereof. Accordingly, compounds of the invention find use in human and veterinary medicine both as immunogens and diagnostic tools.

    摘要翻译： 本发明特别涉及衍生自功能取代的氨基酸的二肽样化合物，其具有通过所述二肽类化合物的胺官能团的酰胺化而结合的脂肪酸链，其一个末端部分具有辅助功能性侧链 间隔物，另一端部分为中性或带电状态的酸基。 本发明的化合物具有如佐剂的免疫调节特性。此外，本发明的化合物可以接枝在给定抗原上以调节或调节免疫应答，或者可以同样地接枝在药物载体上以增强治疗效果或靶向 其中。 因此，本发明的化合物可用作人和兽医学作为免疫原和诊断工具。