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    Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
    4.
    发明授权
    Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method 有权
    二丙基稠合吡咯烷基二肽基肽酶IV抑制剂及方法

    公开(公告)号：US06395767B2

    公开(公告)日：2002-05-28

    申请号：US09788173

    申请日：2001-02-16

    申请人： Jeffrey A. Robl ,  Richard B. Sulsky ,  David J. Augeri ,  David R. Magnin ,  Lawrence G. Hamann ,  David A. Betebenner

    发明人： Jeffrey A. Robl ,  Richard B. Sulsky ,  David J. Augeri ,  David R. Magnin ,  Lawrence G. Hamann ,  David A. Betebenner

    IPC分类号： C07D20907

    CPC分类号： C07C271/22 ,  C07C2603/74 ,  C07D209/52 ,  C07D401/06 ,  C07D403/06

    摘要： Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where x is 0 or 1 and y is 0 or 1 (provided that x=1 when y=0 and x=0 when y=1); n is 0 or 1; X is H or CN; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor *or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.

    摘要翻译： 提供二肽基肽酶IV（DP 4）抑制化合物，其具有0或1并且y为0或1（当y = 0时X = 1，当y = 1时x = 0）; n为0或1; X是H或CN;并且其中R 1，R 2，R 3和R 4如本文所述。还提供了用于治疗糖尿病和相关疾病，特别是II型糖尿病和本文所列的其它疾病的方法，使用这种DP 4抑制剂 *或这种DP 4抑制剂与一种或多种其它抗糖尿病药如二甲双胍，格列本脲，曲格列酮，吡格列酮，罗格列酮和/或胰岛素和/或降血脂药和/或抗肥胖剂中的一种或多种的组合，以及 /或其他治疗剂。

    Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
    5.
    再颁专利
    Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method 有权
    二丙基稠合吡咯烷基二肽基肽酶IV抑制剂及方法

    公开(公告)号：USRE44186E1

    公开(公告)日：2013-04-30

    申请号：US13308658

    申请日：2011-12-01

    申请人： Jeffrey A. Robl ,  Richard B. Sulsky ,  David J. Augeri ,  David R. Magnin ,  Lawrence G. Hamann ,  David A. Betebenner

    发明人： Jeffrey A. Robl ,  Richard B. Sulsky ,  David J. Augeri ,  David R. Magnin ,  Lawrence G. Hamann ,  David A. Betebenner

    IPC分类号： C07D209/02 ,  A61K31/403

    CPC分类号： C07C271/22 ,  C07C2603/74 ,  C07D209/52 ,  C07D401/06 ,  C07D403/06

    摘要： Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where x is 0 or 1 and y is 0 or 1 (provided that x=1 when y=0 and x=0 when y=1); n is 0 or 1; X is H or CN; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor *or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.

    摘要翻译： 提供二肽基肽酶IV（DP 4）抑制化合物，其具有下式，其中x为0或1，y为0或1（当y = 0时x = 1，y = 1时x = 0）; n为0或1; X是H或CN; 并且其中R 1，R 2，R 3和R 4如本文所述。 还提供了一种用于治疗糖尿病和相关疾病，特别是II型糖尿病和本文所列的其它疾病的方法，其使用这种DP 4抑制剂*或这种DP 4抑制剂与一种或多种其它抗糖尿病药如二甲双胍的组合 ，格列本脲，曲格列酮，吡格列酮，罗格列酮和/或胰岛素和/或降血脂药和/或抗肥胖剂和/或其它治疗剂中的一种或多种。

    2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
    9.
    发明授权
    2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method 有权
    2,1-恶唑啉和1,2-吡唑啉类抑制剂二肽基肽酶IV及方法

    公开(公告)号：US06573287B2

    公开(公告)日：2003-06-03

    申请号：US10107279

    申请日：2002-03-26

    申请人： Richard B. Sulsky ,  Jeffrey A. Robl

    发明人： Richard B. Sulsky ,  Jeffrey A. Robl

    IPC分类号： A61K31415

    CPC分类号： C07D231/06 ,  A61K31/415 ,  A61K31/42 ,  C07D231/04 ,  C07D261/02 ,  A61K2300/00

    摘要： Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where n is 0 or 1; X is H or CN; Y is N, NH or O; Z is CH2 when Y is O or N—H, with Y—Z forming a single bond, and Z is CH when Y is N, with Y—Z forming a double bond; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.

    摘要翻译： 提供二肽基肽酶IV（DP 4）抑制化合物，其中n为0或1; X为H或CN; Y为N，NH或O;当Y为O或NH时，Z为CH2，YZ为单键，Y为N时Z为CH，YZ为双键，其中R1 R2，R3和R4如本文所述。还提供了一种用于治疗糖尿病和相关疾病，特别是II型糖尿病和本文所列的其它疾病的方法，使用这种DP 4抑制剂或这种DP 4抑制剂和 一种或多种另一种抗糖尿病药如二甲双胍，格列本脲，曲格列酮，吡格列酮，罗格列酮和/或胰岛素和/或降血脂药和/或抗肥胖剂和/或其它治疗剂中的一种或多种。