公开(公告)号：US20040214869A1

公开(公告)日：2004-10-28

申请号：US10843026

申请日：2004-05-11

申请人： Wyeth

发明人： John A. Butera ,  Craig E. Caufield ,  Russell F. Graceffa ,  Alexander Greenfield ,  Eric G. Gundersen ,  Lisa Marie Havran ,  Alan H. Katz ,  Joseph R. Lennox ,  Scott C. Mayer ,  Robert E. McDevitt

IPC分类号： A61K031/44 ,  A61K031/4035 ,  A61K031/404 ,  C07D209/46 ,  C07D209/04

CPC分类号： C07D213/40 ,  C07C17/16 ,  C07C45/68 ,  C07C45/71 ,  C07C47/575 ,  C07C205/35 ,  C07C205/37 ,  C07C309/77 ,  C07D209/08 ,  C07D233/54 ,  C07D263/58 ,  C07D307/58 ,  C07D307/80 ,  C07D307/81 ,  C07D317/54 ,  C07D333/74 ,  C07D413/12 ,  C07F9/4006 ,  C07C22/04

摘要： This invention provides compounds of Formula I having the structure 1 wherein: B and D are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, aryl, heteroaryl, aralkyl of 6-12 carbon atoms, or heteroaralkyl of 6-12 carbon atoms except where B and D both are hydrogen; R1 is hydrogen, alkyl of 1-6 carbon atoms, nullSO2Ph(OH)(CO2H), nullCH(R2)W, nullCH2CH2Y, or nullCH2CH2CH2Y; R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, nullCH2(1H-imidazol-4-yl), nullCH2(3-1H-indolyl), nullCH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), nullCH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or nullCH2(3-pyridyl); W is nullCO2R3, nullCONHOH, nullCN, nullCONHR3, aryl, heteroaryl, nullCHO, nullCHnullNOR3, or nullCHnullNHNHR3; Y is nullW, nullOCH2CO2R3, aryl, heteroaryl, nullC(nullNOH)NH2, nullOR3, nullO(CnullO)NR4R5, nullNR3(CnullO)OR3, nullNR3(CnullO)NR4R5, or nullNR4R5; R3 is hydrogen or alkyl of 1-6 carbon atoms; R4 and R5 are each, independently, hydrogen, or alkyl of 1-6 carbon atoms or R4 and R5 are, together, null(CH2)nnull, or nullCH2CH2XCH2CH2null; X is O, S, SO, SO2, NR3, or CH2; n is 2 to 5; C is alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, nullCONR6R7, nullNR3CONR6R7, nullNR3COR6, nullOR6, nullO2CNR6 R7, nullNR3CO2R6, nullO2CR6, nullCH2OR6, nullNR6R7, nullCR3nullCR3R8, nullCPh3, nullCH2NR5R6, or 2 R6 and R7 are each, independently, hydrogen, alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, cycloalkyl of 3-10 carbon atoms, null(CH2CH2O)nCH3, null(CH2)mA or R6 and R7 are, together, null(CH2)pnull, null(CH2)2N(CH3)(CH2)4null, null(CH2)2N(R8)(CH2)2null, or null(CH2)2CH(R8)null(CH2)2null; R8 is hydrogen, alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, cycloalkyl of 3-10 carbon atoms, null(CH2CH2O)nCH3, null(CH2CH2CH2O)nCH3, or null(CH2)mA; A is aryl, heteroaryl, aryloxy, heteroaryloxy, arylthio, heteroarylthio, arylsulfoxy, heteroarylsulfoxy, arylsulfonyl, heteroarylsulfonyl, nullCHF2, nullCH2F, nullCF3, null(CH2CH2O)nCH3, null(CH2CH2CH2O)nCH3, nullCO2R3, nullO(CnullO)NR6R7, aralkyloxy, or heteroaralkyloxy; m is 2 to 16 p is 2 to 12 or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

摘要翻译： 本发明提供具有以下结构的式I化合物：其中：B和D各自独立地为氢，卤素，1-6个碳原子的烷基，3-8个碳原子的环烷基，芳基，杂芳基，6-12个碳原子的芳烷基 原子或6-12个碳原子的杂芳烷基，除非B和D都是氢; R 1是氢，1-6个碳原子的烷基，-SO 2 Ph（OH）（CO 2 H），-CH（R 2）W，-CH 2 CH 2 Y或-CH 2 CH 2 CH 2 Y; R 2是氢，1-6个碳原子的烷基，6-12个碳原子的芳烷基，-CH 2（1H-咪唑-4-基），-CH 2（3-1H-吲哚基），-CH 2 CH 2（1， （2-氧代-1,3-二氢 - 异吲哚-2-基）或-CH 2（3-吡啶基）; W是-CO 2 R 3，-CONHOH，-CN，-CONHR 3，芳基，杂芳基，-CHO，-CH = NOR 3或-CH = NHNHR 3; Y是-W，-OCH 2 CO 2 R 3，芳基，杂芳基，-C（= NOH）NH 2，-OR 3，-O（C = O）NR 4 R 5，-NR 3 （C = O）OR 3，-NR 3（C = O）NR 4 R 5或-NR 4 R 5; R 3是氢或1-6个碳原子的烷基; R 4和R 5各自独立地为氢或1-6个碳原子的烷基或R 4和R 5一起为 - （CH 2）n - 或-CH 2 CH 2 XCH 2 CH 2 - ; X是O，S，SO，SO 2，NR 3或CH 2; n为2〜5; C是1-18个碳原子的烷基，芳基，杂芳基，6-20个碳原子的芳烷基，6-20个碳原子的杂芳烷基，-CONR 6 R 7，-NR 3 CONR 6 R <7>，-NR

公开(公告)号：US20030119890A1

公开(公告)日：2003-06-26

申请号：US10282540

申请日：2002-10-29

申请人： Wyeth

发明人： John A. Butera ,  Hassan M. Elokdah ,  Theodore S. Sulkowski ,  John L. Primeau ,  Joseph R. Lennox

IPC分类号： A61K031/4166 ,  C07D233/84

CPC分类号： C07D233/96

摘要： Compounds of Formula I are provided: 1 wherein: R is lower alkyl or branched lower alkyl; and Ar is phenyl, phenyl substituted with one or more of halogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylamino, cyano, or perfluoroalkoxy, or a heteroaromatic moiety; and pharmaceutically acceptable salts thereof.

摘要翻译： 提供式I化合物：其中：R是低级烷基或支链低级烷基; 和Ar是苯基，被一个或多个卤素，低级烷基，低级烷氧基，低级烷硫基，低级烷基氨基，氰基或全氟烷氧基取代的苯基或杂芳族部分; 及其药学上可接受的盐。

公开(公告)号：US20030083341A1

公开(公告)日：2003-05-01

申请号：US10215438

申请日：2002-08-09

申请人： Wyeth

发明人： John A. Butera ,  Craig E. Caufield ,  Russell F. Graceffa ,  Alexander Greenfield ,  Eric G. Gundersen ,  Lisa M. Havran ,  Alan H. Katz ,  Joseph R. Lennox ,  Scott C. Mayer ,  Robert E. McDevitt

IPC分类号： A61K031/435 ,  A61K031/445 ,  A61K031/4166 ,  A61K031/403 ,  A61K031/404 ,  A61K031/325 ,  A61K031/277 ,  A61K031/235

CPC分类号： C07F9/4006 ,  C07B2200/07 ,  C07C17/16 ,  C07C45/68 ,  C07C45/71 ,  C07C47/575 ,  C07C205/35 ,  C07C205/37 ,  C07C225/20 ,  C07C233/43 ,  C07C235/46 ,  C07C235/48 ,  C07C235/52 ,  C07C237/30 ,  C07C255/54 ,  C07C271/12 ,  C07C271/16 ,  C07C271/28 ,  C07C271/30 ,  C07C309/77 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/08 ,  C07D213/40 ,  C07D233/54 ,  C07D263/58 ,  C07D295/088 ,  C07D295/13 ,  C07D307/58 ,  C07D307/80 ,  C07D307/81 ,  C07D317/54 ,  C07D333/74 ,  C07D413/12 ,  C07C22/04

摘要： This invention provides compounds of Formula I having the structure 1 wherein: B and D are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, aryl, heteroaryl, aralkyl of 6-12 carbon atoms, or heteroaralkyl of 6-12 carbon atoms except where B and D both are hydrogen; R1 is hydrogen, alkyl of 1-6 carbon atoms, nullSO2Ph(OH)(CO2H), nullCH(R2)W, nullCH2CH2Y, or nullCH2CH2CH2Y; R2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, nullCH2(1H-imidazol-4-yl), nullCH2(3-1H-indolyl), nullCH2CH2(1,3-dioxo-1,3-dihydro-isoindol-2-yl), nullCH2CH2(1-oxo-1,3-dihydro-isoindol-2-yl), or nullCH2(3-pyridyl); W is nullCO2R3, nullCONHOH, nullCN, nullCONHR3, aryl, heteroaryl, nullCHO, nullCHnullNOR3, or nullCHnullNHNHR3; Y is nullW, nullOCH2CO2R3, aryl, heteroaryl, nullC(nullNOH)NH2, nullOR3, nullO(CnullO)NR4R5, nullNR3(CnullO)OR3, nullNR3(CnullO)NR4R5, or nullNR4R5; R3 is hydrogen or alkyl of 1-6 carbon atoms; R4 and R5 are each, independently, hydrogen, or alkyl of 1-6 carbon atoms or R4 and R5 are, together, null(CH2)nnull, or nullCH2CH2XCH2CH2null; X is O, S, SO, SO2, NR3, or CH2; n is 2 to 5; C is alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, nullCONR6R7, nullNR3CONR6R7, nullNR3COR6, nullOR6, nullO2CNR6R7, nullNR3CO2R6, nullO2CR6, nullCH2OR6, nullNR6R7, nullCR3nullCR3R8, nullCPh3, nullCH2NR6R7, or 2 R6 and R7 are each, independently, hydrogen, alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, cycloalkyl of 3-10 carbon atoms, null(CH2CH2O)nCH3, null(CH2)mA or R6 and R7 are, together, null(CH2)pnull, null(CH2)2N(CH3)(CH2)4null, null(CH2)2N(R8)(CH2)2null, or null(CH2)2CH(R8)null(CH2)2null; R8 is hydrogen, alkyl of 1-18 carbon atoms, aryl, heteroaryl, aralkyl of 6-20 carbon atoms, heteroaralkyl of 6-20 carbon atoms, cycloalkyl of 3-10 carbon atoms, null(CH2CH2O)nCH3, null(CH2CH2CH2O)nCH3, or null(CH2)mA; A is aryl, heteroaryl, aryloxy, heteroaryloxy, arylthio, heteroarylthio, arylsulfoxy, heteroarylsulfoxy, arylsulfonyl, heteroarylsulfonyl, nullCHF2, nullCH2F, nullCF3, null(CH2CH2O)nCH3, null(CH2CH2CH2O)nCH3, nullCO2R3, nullO(CnullO)NR6R7, aralkyloxy, or heteroaralkyloxy; m is 2 to 16 p is 2 to 12 or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

摘要翻译： 本发明提供具有以下结构的式I化合物：其中：B和D各自独立地为氢，卤素，1-6个碳原子的烷基，3-8个碳原子的环烷基，芳基，杂芳基，6-12个碳原子的芳烷基 原子或6-12个碳原子的杂芳烷基，除非B和D都是氢; R1是氢，1-6个碳原子的烷基，-SO2Ph（OH）（CO2H），-CH（R2）W，-CH2CH2Y或-CH2CH2CH2Y; R2是氢，1-6个碳原子的烷基，6-12个碳原子的芳烷基，-CH2（1H-咪唑-4-基），-CH2（3-1H-吲哚基），-CH2CH2（1,3-二氧代 -1,3-二氢 - 异吲哚-2-基），-CH 2 CH 2（1-氧代-1,3-二氢 - 异吲哚-2-基）或-CH2（3-吡啶基）; W是-CO 2 R 3，-CONHOH，-CN，-CONHR 3，芳基，杂芳基，-CHO，-CH = NOR 3或-CH = NHNHR 3; Y是-W，-OCH 2 CO 2 R 3，芳基，杂芳基，-C（= NOH）NH 2，-OR 3，-O（C = O）NR 4 R 5，-NR 3（C = O）OR 3，-NR 3（C = O）NR 4 R 5， 或-NR4R5; R3是氢或1-6个碳原子的烷基; R 4和R 5各自独立地为氢或1-6个碳原子的烷基，或者R 4和R 5一起为 - （CH 2）n - 或-CH 2 CH 2 XCH 2 CH 2 - ; X是O，S，SO，SO 2，NR 3或CH 2; n为2〜5; C为1-18个碳原子的烷基，芳基，杂芳基，6-20个碳原子的芳烷基，6-20个碳原子的杂芳烷基，-CONR6R7，-NR3CONR6R7，-NR3，