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86 条记录 (耗时 0.071 秒)

    Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them
    1.
    发明授权
    Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them 有权
    取代的噻吩并[3,2-d]嘧啶酮作为MCHR1拮抗剂及其使用方法

    公开(公告)号：US08618115B2

    公开(公告)日：2013-12-31

    申请号：US11586255

    申请日：2006-10-25

    申请人： William N. Washburn ,  Mark C. Manfredi ,  Jeffrey A. Robl ,  Andres S. Hernandez

    发明人： William N. Washburn ,  Mark C. Manfredi ,  Jeffrey A. Robl ,  Andres S. Hernandez

    IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P3/04 ,  A61P3/10 ,  A61P25/22 ,  A61P25/24

    CPC分类号： C07D495/04

    摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.

    摘要翻译： 本申请提供化合物，包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式。另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。 最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有MCHR-1调节的疾病或病症例如肥胖，糖尿病，抑郁或焦虑的患者的方法。

    N-formyl hydroxylamine containing compounds useful as ACE inhibitors and/or NEP inhibitors
    6.
    发明授权
    N-formyl hydroxylamine containing compounds useful as ACE inhibitors and/or NEP inhibitors 失效
    可用作ACE抑制剂的N-甲酰基羟胺化合物和/或NEP抑制剂

    公开(公告)号：US06777550B1

    公开(公告)日：2004-08-17

    申请号：US08833172

    申请日：1997-04-04

    申请人： Jeffrey A. Robl

    发明人： Jeffrey A. Robl

    IPC分类号： C07D22312

    CPC分类号： C07K5/0202

    摘要： N-formyl hydroxylamines are provided which have the structure wherein R is H, alkyl, alkenyl, aryl-(CH2)p—, heteroaryl-(CH2)p— or cycloheteroalkyl-(CH2)p— R1 is H or COR2 where R2 is alkyl, aryl-(CH2)p—, cycloheteroalkyl-(CH2)p—, heteroaryl-(CH2)p—, alkoxy or cycloalkyl-(CH2)p—, p is 0 to 8, and A is a dipeptide derived from an amino acid or is a conformationally restricted dipeptide mimic. The above compounds are useful in treating hypertension congestive heart failure, renal failure, and hepatic cirrhosis.

    摘要翻译： 提供了N-甲酰基羟胺，其具有其中R为H，烷基，烯基，芳基 - （CH 2）p - ，杂芳基 - （CH 2）p - 或环杂烷基 - （CH 2）p R 1的结构为H或COR 2 其中R 2是烷基，芳基 - （CH 2）p - ，环杂烷基 - （CH 2）p - ，杂芳基 - （CH 2）p - ，烷氧基或环烷基 - （CH 2）p - ，p是0至8，并且A 是衍生自氨基酸的二肽或是构象限制性二肽模拟物。上述化合物可用于治疗高血压充血性心力衰竭，肾衰竭和肝硬化。

    Tetrahydropyrimidone inhibitors of fatty acid binding protein and method
    8.
    发明授权
    Tetrahydropyrimidone inhibitors of fatty acid binding protein and method 有权
    脂肪酸结合蛋白的四氢嘧啶酮抑制剂及方法

    公开(公告)号：US06649622B2

    公开(公告)日：2003-11-18

    申请号：US09771310

    申请日：2001-01-26

    申请人： Richard Sulsky ,  Jeffrey A. Robl

    发明人： Richard Sulsky ,  Jeffrey A. Robl

    IPC分类号： C07D23922

    CPC分类号： C07D239/10 ,  C07D401/12 ,  C07D403/12 ,  C07D491/10 ,  C07F9/6506

    摘要： aP2 inhibiting compounds are provided having the formula wherein A, B, X, and Y are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.

    摘要翻译： 本发明提供了一种具有脯氨酸A，B，X和Y的aP2抑制化合物，如本文所述。还提供了一种治疗糖尿病和相关疾病，特别是II型糖尿病的方法，使用这种P 2抑制剂或这种pP抑制剂和 另一种抗糖尿病药如二甲双胍，格列本脲，曲格列酮和/或胰岛素。

    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。

    Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
    10.
    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。