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    POLYETHYLENE GLYCOL CONJUGATES OF HETEROCYCLOALKYL CARBOXAMIDO PROPANOIC ACIDS
    4.
    发明公开
    POLYETHYLENE GLYCOL CONJUGATES OF HETEROCYCLOALKYL CARBOXAMIDO PROPANOIC ACIDS 审中-公开
    杂环羧酰胺酰胺丙酸的聚乙二醇共轭物

    公开(公告)号：EP1706399A1

    公开(公告)日：2006-10-04

    申请号：EP05712086.7

    申请日：2005-01-24

    申请人： ELAN PHARMACEUTICALS, INC.

    发明人： KONRADI, Andrei ,  PLEISS, Michael, A. ,  SEMKO, Chris, M. ,  SMITH, Jenifer, L. ,  VANDERVERT, Chris

    IPC分类号： C07D401/12 ,  C07D277/06 ,  A61K31/426 ,  A61P29/00

    CPC分类号： C08G63/91 ,  A61K47/60 ,  C07D295/205 ,  C07D417/12 ,  C07D417/14

    摘要： Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer’s disease, atherosclerosis, AIDS, dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

    摘要翻译： 公开了结合VLA-4的缀合物。 这些缀合物中的某些还抑制白细胞粘附，特别是抑制由VLA-4介导的白细胞粘附。 这样的缀合物可用于治疗哺乳动物患者例如人的炎性疾病，例如哮喘，阿尔茨海默氏病，动脉粥样硬化，AIDS，痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血。 该缀合物也可以用于治疗炎性脑疾如多发性硬化症。

    NOVEL DIPEPTIDYL PEPTIDASE IV (DP-IV) INHIBITORS AS ANTI-DIABETIC AGENTS
    8.
    发明公开
    NOVEL DIPEPTIDYL PEPTIDASE IV (DP-IV) INHIBITORS AS ANTI-DIABETIC AGENTS 审中-公开
    NEW二肽基肽IV（DP-IV）抑制剂作为抗糖尿病

    公开(公告)号：EP1450794A1

    公开(公告)日：2004-09-01

    申请号：EP02801961.0

    申请日：2002-10-23

    申请人： Ferring B.V.

    发明人： EVANS, David Michael ,  TARTAR, Andre

    IPC分类号： A61K31/426 ,  C07D207/16 ,  C07D277/06 ,  C07D277/04 ,  C07D403/12 ,  C07D417/12 ,  C07D401/12 ,  C07D401/06 ,  A61K31/427 ,  A61K31/4025 ,  A61P3/10

    CPC分类号： C07D213/82 ,  C07D277/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

    摘要： The present invention relates to a series of prodrugs of inhibitors of DP-IV with improved properties. The compounds can be used for the treatment of a number of human diseases, including impaired glucose tolerance and type II diabetes. The compounds of the invention are described by general formula (1); wherein R1 is H or CN; R2 is selected from CH¿2R?5, CH2CH2R5 and C(R?3)(R4)-X2-(CH¿2)aR?5; R3 and R4¿ are each independently selected from H and Me; R5 is selected from CON(R?6)(R7), N(R8)C(=0)R9, N(R8)C(=S)R9, N(R8)SO¿2R1O and N(R?8)R1O; R6 and R7¿ are each independently R11(CH2)b or together they are -(CH2)2-Z-(CH2)2- or CH2-o- C6H4-Z-CH2-; R8 is H or Me; R9 is selected from R11(CH2)b, R11(CH2)bO and N(R?6)(R7); R10 is R11(CH¿2)b; R11 is selected from H, alkyl, optionally substituted aryl, optionally substituted aroyl, optionally substituted arylsulphonyl and optionally substituted heteroaryl; R12 is selected from H¿2?NCH(R?13¿)CO, H¿2?NCH(R?14¿)CONHCH(R15)CO, C(R?16)=C(R17)COR18 and R19OCO; R13, R14 and R15¿ are selected from the side chains of the proteinaceous amino acids; R16 is selected from H, lower alkyl (C¿1?-C6) and phenyl; R?17¿ is selected from H and lower alkyl (C¿1?-C6); R?18¿ is selected from H, lower alkyl (C¿1?-C6), OH, O-(lower alkyl (C1-C6)) and phenyl; R?19¿ is selected from lower alkyl (C¿1?-C6), optionally substituted phenyl and R?20¿C(=0)OC(R?21)(R22); R20, R21 and R22¿ are each independently selected from H and lower alkyl (C¿1?-C6); Z is selected from a covalent bond, -(CH2)c-, -O-, -SOd- and -N(R?1O)-; X1¿ is S or CH¿2; X?2 is O, S or CH¿2?; a is 1, 2 or 3; b is 0-3; c is 1 or 2; and d is 0, 1 or 2.