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    2-BENZYL-POLYCYCLIC GUANINE DERIVATIVES AND PROCESS FOR PREPARING THEM
    1.
    发明公开
    2-BENZYL-POLYCYCLIC GUANINE DERIVATIVES AND PROCESS FOR PREPARING THEM 失效
    2 BENZYLPOLYCYCLISCH鸟嘌呤及其制备方法

    公开(公告)号：EP0686157A1

    公开(公告)日：1995-12-13

    申请号：EP94910124.0

    申请日：1994-02-24

    申请人： SCHERING CORPORATION

    发明人： TULSHIAN, Deen ,  McKITTRICK, Brian, A. ,  XIA, Yan ,  CHACKALAMANNIL, Samuel ,  GALA, Dinesh ,  DIBENEDETTO, Donald, J. ,  KUGELMAN, Max

    IPC分类号： C07D239 ,  C07D473 ,  C07D487

    CPC分类号： C07D487/14 ,  C07D239/54 ,  C07D473/40

    摘要： Antihypertensive and bronchodilating compounds of formula (I) or a pharmaceutically acceptable salt thereof, and a process for preparing them are disclosed, wherein: R1, R2 and R3 are hydrogen, lower alkyl, lower alkoxy, halogeno, hydroxy, (di-lower alkyl)amino, 4-morpholinyl, 1-pyrrolidinyl, 1-pyrrolyl, -CF3, -OCF3, phenyl or methoxyphenyl; or R1 and R2 together are methylenedioxy; or R1 and R2 together with the carbon atoms to which they are attached form a benzene ring; and Ra is hydrogen and R?b and Rc¿, together with the carbon atoms to which they are attached, form a saturated ring of 5 carbons; or Ra is lower alkyl, Rb is hydrogen or lower alkyl, and Rc is hydrogen; or Ra, Rb and the carbon atom to which they are attached form a saturated ring of 5-7 carbons, and Rc is hydrogen; or Ra is hydrogen, and Rb, Rc and the carbon atoms to which they are attached form a tetrahydrofuran ring; or R?a and Rb¿, together with the carbon atom to which they are attached, and R?b and Rc¿, together with the carbon atoms to which they are attached, each form a saturated ring of 5-7 carbons; pharmaceutical compositions containing said compounds: methods of treatment using said compounds; and a process for preparing polycyclic guanines comprising a) reducing a nitrosopyrimidine, and treating the reduced nitrosopyrimidine with an acylating reagent to give the amidopyrimidine; b) reacting the amidopyrimidine with a halogenating/cyclizing reagent to give a halopurine; c) reacting, in the presence of a base, the halopurine with an amine to give the substituted aminopurine; and d) closing the ring of the substituted aminopurine with a suitable dehydrating agent.

    SULFUR-SUBSTITUTED AZETIDINONE COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS
    3.
    发明授权
    SULFUR-SUBSTITUTED AZETIDINONE COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS 失效
    硫取代的AZETDINONE HYPOCHOLESTEROLMISCHMITTEL

    公开(公告)号：EP0792264B1

    公开(公告)日：2002-02-27

    申请号：EP95939677.1

    申请日：1995-11-15

    申请人： SCHERING CORPORATION

    发明人： McKITTRICK, Brian, A. ,  DUGAR, Sundeep ,  BURNETT, Duane, A.

    IPC分类号： C07D205/08 ,  C07D409/12 ,  C07D401/12 ,  A61K31/395 ,  A61K31/44

    CPC分类号： C07D401/12 ,  C07D205/08 ,  C07D409/12

    摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of formula (I), or a pharmaceutically acceptable salt thereof, wherein: Ar1 is aryl, R10-substituted aryl or heteroaryl; Ar2 is aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X and Y are -CH¿2?-, -CH(lower alkyl)- or -C(dilower alkyl)-; R is -OR?6¿, -O(CO)R6, -O(CO)OR9 or -O(CO)NR6R7; R1 is hydrogen, lower alkyl or aryl; or R and R1 together are =0; q is 0 or 1; r is 0, 1 or 2; m and n are 0-5; provided that the sum of m, n and q is 1-5; R4 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH¿2?)1-5OR?6¿, -O(CO)NR?6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO¿2R?9, -COOR6, -CONR6R7, -COR6, -SO¿2NR6R7, S(O)¿0-2R?9, -O(CH¿2?)1-10-COOR?6¿, -O(CH¿2?)1-10CONR?6R7¿, -(lower alkylene)-COOR6 and -CH=CH-COOR6; R5 is selected from -OR6, -O(CO)R6, -O(CO)OR9, -O(CH¿2?)1-5OR?6¿, -O(CO)NR?6R7, -NR6?R?7 -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO¿2R?9, -COOR6, -CONR6R7, -COR6, -SO¿2NR6R7, S(O)¿0-2R?9, -O(CH¿2?)1-10-COOR?6¿, -O(CH¿2?)1-10CONR?6R7, -CF¿3, -CN, -NO2, halogen, -(lower alkylene)COOR6 and -CH=CH-COOR?6; R6, R7 and R8¿ are H, lower alkyl, aryl or aryl-substitued lower alkyl; R9 is lower alkyl, aryl or aryl-sybstituted lower alkyl; and R10 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH¿2?)1-5OR?6¿, -O(CO)NR?6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO¿2R?9, -COOR6, -CONR6R7, COR6, -SO¿2NR6R7, -S(O)¿0-2R?9, -O(CH¿2?)1-10-COOR?6¿, -O(CH¿2?)1-10CONR?6R7, -CF¿3, -CN, -NO2 and halogen; are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

    SULFUR-SUBSTITUTED AZETIDINONE COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS
    4.
    发明公开
    SULFUR-SUBSTITUTED AZETIDINONE COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS 失效
    用于低分子量药物的硫取代的二氮杂萘酮化合物

    公开(公告)号：EP0792264A1

    公开(公告)日：1997-09-03

    申请号：EP95939677.0

    申请日：1995-11-15

    申请人： SCHERING CORPORATION

    发明人： McKITTRICK, Brian, A. ,  DUGAR, Sundeep ,  BURNETT, Duane, A.

    IPC分类号： A61K31 ,  A61P3 ,  A61P9 ,  C07D205 ,  C07D401 ,  C07D409

    CPC分类号： C07D401/12 ,  C07D205/08 ,  C07D409/12

    摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of formula (I), or a pharmaceutically acceptable salt thereof, wherein: Ar1 is aryl, R10-substituted aryl or heteroaryl; Ar2 is aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X and Y are -CH¿2?-, -CH(lower alkyl)- or -C(dilower alkyl)-; R is -OR?6¿, -O(CO)R6, -O(CO)OR9 or -O(CO)NR6R7; R1 is hydrogen, lower alkyl or aryl; or R and R1 together are =0; q is 0 or 1; r is 0, 1 or 2; m and n are 0-5; provided that the sum of m, n and q is 1-5; R4 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH¿2?)1-5OR?6¿, -O(CO)NR?6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO¿2R?9, -COOR6, -CONR6R7, -COR6, -SO¿2NR6R7, S(O)¿0-2R?9, -O(CH¿2?)1-10-COOR?6¿, -O(CH¿2?)1-10CONR?6R7¿, -(lower alkylene)-COOR6 and -CH=CH-COOR6; R5 is selected from -OR6, -O(CO)R6, -O(CO)OR9, -O(CH¿2?)1-5OR?6¿, -O(CO)NR?6R7, -NR6?R?7 -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO¿2R?9, -COOR6, -CONR6R7, -COR6, -SO¿2NR6R7, S(O)¿0-2R?9, -O(CH¿2?)1-10-COOR?6¿, -O(CH¿2?)1-10CONR?6R7, -CF¿3, -CN, -NO2, halogen, -(lower alkylene)COOR6 and -CH=CH-COOR?6; R6, R7 and R8¿ are H, lower alkyl, aryl or aryl-substitued lower alkyl; R9 is lower alkyl, aryl or aryl-sybstituted lower alkyl; and R10 is selected from lower alkyl, -OR6, -O(CO)R6, -O(CO)OR9, -O(CH¿2?)1-5OR?6¿, -O(CO)NR?6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO¿2R?9, -COOR6, -CONR6R7, COR6, -SO¿2NR6R7, -S(O)¿0-2R?9, -O(CH¿2?)1-10-COOR?6¿, -O(CH¿2?)1-10CONR?6R7, -CF¿3, -CN, -NO2 and halogen; are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

    摘要翻译： 式（I）的硫取代的氮杂环丁酮降血胆固醇剂或其药学上可接受的盐，其中：Ar 1是芳基，R 10取代的芳基或杂芳基; Ar 2是芳基或R 4取代的芳基; Ar3是芳基或R5-取代的芳基; X和Y是-CH 2 - ， - CH（低级烷基） - 或-C（低级烷基） - ; R是-OR 6，-O（CO）R 6，-O（CO）OR 9或-O（CO）NR 6 R 7; R1是氢，低级烷基或芳基; 或R和R1一起为= 0; q是0或1; r是0,1或2; m和n是0-5; 条件是m，n和q的和为1-5; R4选自低级烷基，-OR6，-O（CO）R6，-O（CO）OR9，-O（CH2-2）1-5OR6，-O（CO）NR6R7，-NR6R7 ，-NR6（CO）R7，-NR6（CO）OR9，-NR6（CO）NR7R8，-NR6SO2R9，-COOR6，-CONR6R7，-COR6，-SO2NR6R7，S（O） （低级亚烷基）-COOR 6和-CH = CH-COOR 6，-O（CH 2）2 -COOR 6，-O（CH 2 2）1-10 CONR 6 R 7， ; R5选自-OR6，-O（CO）R6，-O（CO）OR9，-O（CH2-2）1-5OR6，-O（CO）NR6R7，-NR6R5， （CO）R7，-NR6（CO）OR9，-NR6（CO）NR7R8，-NR6SO2R9，-COOR6，-CONR6R7，-COR6，-SO2NR6R7，S（O） 2（R 2）1-10 -COOR 6，-O（CH 2 2）1-10 CONR 6 R 7，-CF 3，-CN，-NO 2，卤素， - （ 低级亚烷基）COOR 6和-CH = CH-COOR 6; R6，R7和R8是H，低级烷基，芳基或芳基取代的低级烷基; R9是低级烷基，芳基或芳基 - 取代的低级烷基; （CO）R6，-O（CO）OR9，-O（CH2-2）1-5OR6，-O（CO）NR6R7， - NR6R7，-NR6（CO）R7，-NR6（CO）OR9，-NR6（CO）NR7R8，-NR6SO2R9，-COOR6，-CONR6R7，COR6，-SO2NR6R7，-S（O） -O（CH 2 2）1-10 -COOR 6，-O（CH 2 2）1-10 CONR 6 R 7，-CF 3，-CN，-NO 2和卤素; 以及含有它们的药物组合物以及通过单独或与胆固醇生物合成抑制剂组合给予所述化合物来降低血清胆固醇的方法。