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    THE PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS
    1.
    发明申请
    THE PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS 审中-公开
    化合物作为蛋白酶抑制剂的制备和使用

    公开(公告)号：WO2006138230A2

    公开(公告)日：2006-12-28

    申请号：PCT/US2006022849

    申请日：2006-06-12

    Applicant: SCHERING CORP ,  MCKITTRICK BRIAN ,  ZHU ZHAONING ,  STAMFORD ANDREW

    Inventor： MCKITTRICK BRIAN ,  ZHU ZHAONING ,  STAMFORD ANDREW

    IPC: C07D205/06

    CPC classification number: C07D487/04 ,  C07D205/06

    Abstract: ABSTRACT Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein, X is -C(R 3 R 4 )-; Y is -N(R 5 )-; Z is -C(=N-R 5 ')-; and R 1 , R 2 , R 3 , and R 4 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

    Abstract translation: 摘要公开了式（I）化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂化物，其中X是-C（R 3）4， - ; Y是-N（R 5） - ; Z是-C（= N-R 5） - ; 和R 1，R 2，R 3和R 4如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶D 和原生动物酶。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱拮抗剂组合来治疗认知或神经变性疾病的方法。

    NEUROPEPTIDE RECEPTOR MODULATORS
    4.
    发明申请
    NEUROPEPTIDE RECEPTOR MODULATORS 审中-公开
    神经肽受体调节剂

    公开(公告)号：WO2005111031A3

    公开(公告)日：2005-12-22

    申请号：PCT/US2005014518

    申请日：2005-04-28

    Applicant: SCHERING CORP ,  ZHU ZHAONING ,  SUN ZHONG-YUE ,  YE YUANZAN ,  MULLINS DEBORRA E ,  MCKITTRICK BRIAN ,  STAMFORD ANDREW ,  GREENLEE WILLIAM J

    Inventor： ZHU ZHAONING ,  SUN ZHONG-YUE ,  YE YUANZAN ,  MULLINS DEBORRA E ,  MCKITTRICK BRIAN ,  STAMFORD ANDREW ,  GREENLEE WILLIAM J

    IPC: A61K31/428 ,  A61K31/541 ,  C07D417/00 ,  C07D417/12 ,  C07D487/04 ,  C07D513/04

    CPC classification number: C07D487/04 ,  C07D417/12 ,  C07D513/04

    Abstract: The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. The compounds are represented by the structural Formula 1, Chemical formula should be inderted here as it appears on the abstract in paper form. a prodrug thereof, or any pharmaceutically acceptable salt, solvate, isomer or racemic mixture of the compound or said prodrug wherein R1 is heteroaryl, N-arylaminocarbonyl, N-heteroarylaminocarbonyl, benzimidazolyl or benzothiazolyl; R15 is present or not and if present is H, aryl, alkyl, arylalky or heteroarylalkyl; A is aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene or heterocycloalkyl wherein said aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene and heterocycloalkyl moieties may be substituted or unsubstituted; and B, L, X and R18 are defined herein.

    Abstract translation: 本发明公开了作为NPY Y1的新受体拮抗剂的化合物以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含这种NPY Y1受体拮抗剂的药物组合物以及使用它们治疗肥胖症，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。 这些化合物由结构式1表示，化学式在此以摘要形式出现在本文中应该没有改变。 其中R 1为杂芳基，N-芳基氨基羰基，N-杂芳基氨基羰基，苯并咪唑基或苯并噻唑基的化合物或所述前药的任何药学上可接受的盐，溶剂化物，异构体或外消旋混合物; R15存在或不存在并且如果存在则为H，芳基，烷基，芳基烷基或杂芳基烷基; A是芳基，杂芳基，环烷基，环亚烷基，亚杂环烷基或杂环烷基，其中所述芳基，杂芳基，环烷基，亚环烷基，亚杂环烷基和杂环烷基部分可以被取代或未被取代; 并且B，L，X和R 18如本文所定义。

    HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS
    6.
    发明申请
    HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 审中-公开
    杂环ASPARTYL蛋白酶抑制剂

    公开(公告)号：WO2007050721A3

    公开(公告)日：2007-06-14

    申请号：PCT/US2006041716

    申请日：2006-10-25

    Applicant: SCHERING CORP ,  ZHU ZHAONING ,  STAMFORD ANDREW W ,  MCKITTRICK BRIAN

    Inventor： ZHU ZHAONING ,  STAMFORD ANDREW W ,  MCKITTRICK BRIAN

    IPC: C07D409/04 ,  A61K31/395 ,  A61P9/00 ,  A61P25/28 ,  A61P31/18 ,  A61P33/02 ,  C07D487/04 ,  C07D498/04

    CPC classification number: C07D409/04 ,  C07D487/04

    Abstract: Disclosed are compounds of the formula I Chemical formula should be inserted here as it appears on the abstract in paper form. or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

    Abstract translation: 所公开的是式I化合物，化学式应插入此处，因为它以摘要形式出现在纸上。 或其立体异构体，互变异构体或药学上可接受的盐或溶剂化物，其中Ar，R1，R2，R3，R4和R5如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经退行性疾病的方法。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经退行性疾病的方法。

    THE PREPARATION AND USE OF COMPOUNDS AS ASPARTYL PROTEASE INHIBITORS
    7.
    发明申请
    THE PREPARATION AND USE OF COMPOUNDS AS ASPARTYL PROTEASE INHIBITORS 审中-公开
    化合物作为ASPARTYL蛋白酶抑制剂的制备和使用

    公开(公告)号：WO2006138266A3

    公开(公告)日：2007-03-08

    申请号：PCT/US2006022920

    申请日：2006-06-12

    Applicant: SCHERING CORP ,  MCKITTRICK BRIAN ,  ZHU ZHAONING ,  STAMFORD ANDREW ,  SMITH ELIZABETH M

    Inventor： MCKITTRICK BRIAN ,  ZHU ZHAONING ,  STAMFORD ANDREW ,  SMITH ELIZABETH M

    IPC: C07D251/10 ,  A61K31/53 ,  A61P9/00

    CPC classification number: C07D251/72 ,  C07D239/70 ,  C07F9/6584

    Abstract: Disclosed are compounds of the formula I (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein A is a bond, -C(O)-, or -C(R 3' )(R 4' )-; X is -N(R 1 )- or -C(R 6 )(R 7 )-; Y is -S(O) 2 -, -C(=O)-, -PO(OR 9 ) or -C(R 6' R 7' )-; is a single or double bond and R, R 1 , R 2 , R 3 , R 4 , R 3' , R 4' , R 5 , R 6 , R 6' , R 7 and R 7' are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

    Abstract translation: 公开了式I的化合物（化学式应该在此插入，如其以纸的形式出现）（I）或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物，其中A为键，-C（O ） - 或-C（R 3'）（R 4'） - ; X是-N（R 1） - 或-C（R 6）（R 7） - ; Y是-S（O）2 - ， - C（= O） - ， - PO（OR 9）或-C（R 6' SUP> - [R 7' ） - ; 是单键或双键，R 1，R 2，R 2，R 3，R 4，R 4， R 4，R 4，R 5，R 6，R 6，S 6， >，R 7和R 7'如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶D 和原生动物酶。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱拮抗剂组合来治疗认知或神经变性疾病的方法。

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