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    HMG-CoA reductase inhibitors and method
    2.
    发明授权
    HMG-CoA reductase inhibitors and method 有权
    HMG-CoA还原酶抑制剂及方法

    公开(公告)号：US06812345B2

    公开(公告)日：2004-11-02

    申请号：US10602752

    申请日：2003-06-24

    Applicant: Jeffrey A. Robl ,  Bang-Chi Chen ,  Chong-Qing Sun

    Inventor： Jeffrey A. Robl ,  Bang-Chi Chen ,  Chong-Qing Sun

    IPC: C07D491044

    CPC classification number: C07D471/04 ,  C07D491/04 ,  C07D491/10 ,  C07D495/04

    Abstract: Compounds of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids such as lowering LDL cholesterol and/or increasing HDl cholesterol, and treating hyperlipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis and pharmaceutically acceptable salts thereof, wherein X is O, S, SO, SO2 or NR7; Z is n is 0 or 1; R1 and R2 are the same or different and are independently selected from alkyl, arylalkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, heteroaryl or cycloheteroalkyl; and R3 to R10 are as defined herein.

    Abstract translation: 以下结构的化合物是HMG CoA还原酶抑制剂，因此具有抑制胆固醇生物合成，调节血清脂质如降低LDL胆固醇和/或增加HDL胆固醇和治疗高脂血症，高胆固醇血症，高甘油三酯血症和动脉粥样硬化及其药学上可接受的盐的活性，其中 X是O，S，SO，SO 2或NR 7; Z isn是0或1; R 1和R 2相同或不同，并且独立地选自烷基，芳基烷基，环烷基，烯基，环烯基，芳基，杂芳基或环杂烷基; 和R 3至R 10如本文所定义。

    Processes and intermediates for preparing benzo-fused azepinone and piperidinone compounds useful in the inhibition of ACE and NEP
    3.
    发明授权
    Processes and intermediates for preparing benzo-fused azepinone and piperidinone compounds useful in the inhibition of ACE and NEP 失效
    制备用于抑制ACE和NEP的苯并稠合氮杂酮和哌啶酮化合物的方法和中间体

    公开(公告)号：US06235922B1

    公开(公告)日：2001-05-22

    申请号：US09205316

    申请日：1998-12-04

    Applicant: Jeffrey A. Robl ,  Chong-Qing Sun

    Inventor： Jeffrey A. Robl ,  Chong-Qing Sun

    IPC: C07C32734

    CPC classification number: C07K5/06139 ,  A61K38/00 ,  C07K5/0606 ,  C07K5/06191

    Abstract: Compounds having the following formula I, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: wherein: Y1 and Y2 are each independently hydrogen, alkyl, aryl, halogen, or alkoxy; X is O or S(O)t; A is t is zero, one or two; m and n are independently zero or one; and wherein R, R5, R5a, R5b, R6, R7, R11, q and r are defined herein.

    Abstract translation: 具有下式I的化合物及其药学上可接受的盐，包括ACE和NEP的双重抑制剂和选择性ACE抑制剂：其中：Y1和Y2各自独立地为氢，烷基，芳基，卤素或烷氧基; X为O或S（ O）t; A ist为零，一个或两个; m和n独立地为0或1;并且其中R，R 5，R 5a，R 5b，R 6，R 7，R 11，q和r在本文中定义。

    Substituted thieno[3,2-d]pyrimidinones as MCHR1 antagonists and methods for using them
    4.
    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

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

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

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

    CPC classification number: C07D495/04

    Abstract: 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.

    Abstract translation: 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
    9.
    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

    Applicant: Jeffrey A. Robl

    Inventor： Jeffrey A. Robl

    IPC: C07D22312

    CPC classification number: C07K5/0202

    Abstract: 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.

    Abstract translation: 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。

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