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    Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
    1.
    发明申请
    Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes 有权
    稠合苯丙氨酸衍生物作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病

    公开(公告)号：US20060281727A1

    公开(公告)日：2006-12-14

    申请号：US10573108

    申请日：2004-10-29

    申请人： Wallace Ashton ,  Hong Dong ,  Jinyou Xu

    发明人： Wallace Ashton ,  Hong Dong ,  Jinyou Xu

    IPC分类号： A61K31/513 ,  A61K31/498 ,  A61K31/4745 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/397 ,  C07D487/02 ,  C07D403/02

    CPC分类号： C07D207/10 ,  A61K38/00 ,  C07D205/04

    摘要： The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

    摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-RV抑制剂”）的抑制剂的稠合苯丙氨酸衍生物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如 作为糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

    Arylsulfonyloxy purine intermediates
    3.
    发明授权
    Arylsulfonyloxy purine intermediates 失效
    芳基磺酰氧基嘌呤中间体

    公开(公告)号：US4897479A

    公开(公告)日：1990-01-30

    申请号：US165360

    申请日：1988-02-29

    申请人： Richard L. Tolman ,  Wallace Ashton ,  Malcolm Maccoss

    发明人： Richard L. Tolman ,  Wallace Ashton ,  Malcolm Maccoss

    IPC分类号： C07D473/00 ,  C07F9/6561

    CPC分类号： C07D473/00 ,  C07F9/65616

    摘要： Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof are disclosed. In these compounds, R.sup.1 is halogen, --SR.sup.4 wherein R.sup.4 is H or alkyl of 1 to 4 carbon atoms, --OCH.sub.3, --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms, --NR.sup.4 R.sup.5 wherein R.sup.4 is as defined above and R.sup.5 is H, alkyl of 1 to 4 carbon atoms, amino, alkanoyl of 1 to 8 carbon atoms, benzoyl, methoxy or hydroxy or R.sup.1 is --N(CH.sub.3).sub.3.sup.+ X.sup.-whereinX is halogen or --OSO.sub.2 Ar wherein Ar is phenyl or alkyl substituted phenyl wherein the alkyl group has 1 to 6 carbon atoms;R.sup.2 is H, alkanoyl of 1 to 8 carbon atoms or benzoyl;R.sup.3 is A or B whereinA is ##STR2## and B is ##STR3## wherein R.sup.6 and R.sup.7 are independently selected from H and ##STR4## wherein R.sup.8 and R.sup.9 are independently selected from pharmaceutically acceptable cations and H, or R.sup.6 and R.sup.7 taken together are ##STR5## wherein R.sup.10 is selected from pharmaceutically acceptable cations and H; with the proviso that R.sup.4 is not H when: R.sup.5 is H, R.sup.3 is A, and R.sup.6 and R.sup.7 are H. The compounds have anti-viral activity.

    摘要翻译： 公开了式“IMAGE”的化合物及其药学上可接受的盐。 在这些化合物中，R 1是卤素，-SR 4，其中R 4是H或1-4个碳原子的烷基，-OCH 3，-OSO 2 Ar，其中Ar是苯基或烷基取代的苯基，其中烷基具有1-6个碳原子，-NR4R5其中 R 4如上所定义，R 5为H，具有1至4个碳原子的烷基，氨基，1至8个碳原子的烷酰基，苯甲酰基，甲氧基或羟基或R 1为-N（CH 3）3 + X-，其中X为卤素或 -OSO 2 Ar，其中Ar是苯基或烷基取代的苯基，其中烷基具有1至6个碳原子; R2是H，1-8个碳原子的烷酰基或苯甲酰基; R3是A或B，其中A是，B是，其中R6和R7独立地选自H和IMA，其中R8和R9独立地选自药学上可接受的阳离子，H或R6和R7一起 其中R 10选自药学上可接受的阳离子和H; 条件是当R 5为H，R 3为A且R 6和R 7为H时，R 4不为H。化合物具有抗病毒活性。

    Fused Triazole Derivatives as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes
    4.
    发明申请
    Fused Triazole Derivatives as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes 失效
    稠合三唑衍生物作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病

    公开(公告)号：US20070208010A1

    公开(公告)日：2007-09-06

    申请号：US11660130

    申请日：2005-08-19

    申请人： Ann Weber ,  Wallace Ashton

    发明人： Ann Weber ,  Wallace Ashton

    IPC分类号： A61K31/551 ,  A61K31/519 ,  A61K31/498 ,  C07D487/14

    CPC分类号： C07D471/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14 ,  C07D498/04 ,  C07D513/04

    摘要： The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

    摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DPP-IV抑制剂”）的抑制剂的新的稠合三唑衍生物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病， 如糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。