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    • 5. 发明授权
    • Alpha-heterocyclc substituted tolunitriles
    • α-杂环取代的亚苄基
    • US4978672A
    • 1990-12-18
    • US240862
    • 1988-09-06
    • Robert M. BowmanRonald E. SteeleLeslie Browne
    • Robert M. BowmanRonald E. SteeleLeslie Browne
    • C07D213/57C07D233/61C07D249/02C07D249/08C07D521/00
    • C07D231/12C07D213/57C07D233/56C07D249/02C07D249/08
    • The invention is concerned with aromatase inhibiting compounds of formula I ##STR1## wherein R and Ro represent hydrogen or lower alkyl; or R and Ro located on adjacent carbon atoms and together when combined with the benzene ring to which they are attached form a naphthalene or tetrahydronaphthalene ring; R.sub.1 and R.sub.2 independently represent hydrogen, lower alkyl, (lower alkyl, aryl or aryl-lower alkyl)-thio, lower alkenyl, aryl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl, or C.sub.3 -C.sub.6 -cycloalkyl-lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylidene, mono- or di-aryl-lower alkylidene; R.sub.1 and R.sub.2 combined also represent C.sub.4 -C.sub.6 -straight chain alkylene, lower alkyl-substituted straight chain alkylene or ortho-phenylene bridged-C.sub.2 -C.sub.4 -straight chain alkylene, each forming with the carbon atom attached thereto a corresponding optionally substituted or benzo-fused 5, 6 or 7-membered ring; W represents 1-imidazolyl, 1-(1,2,4- or 1,3,4)-triazolyl or 3-pyridyl; or W represents 1-imidazolyl, 1-(1,2,4 or 1,3,4)-triazolyl or 3-pyridyl substituted by lower alkyl; and pharmaceutically acceptable salts thereof.
    • 本发明涉及芳香酶抑制化合物,其中R和R 4代表氢或低级烷基; 或R和Ro位于相邻的碳原子上并与它们所连接的苯环组合时形成萘或四氢萘环; R 1和R 2独立地表示氢,低级烷基,(低级烷基,芳基或芳基 - 低级烷基) - 硫代,低级链烯基,芳基,芳基 - 低级烷基,C 3 -C 6环烷基或C 3 -C 6环烷基 - 低级烷基。 或R 1和R 2组合​​表示低级亚烷基,单 - 或二 - 芳基 - 低级亚烷基; R1和R2组合也表示C4-C6-直链亚烷基,低级烷基取代的直链亚烷基或邻 - 亚苯基桥连的C 2 -C 4 - 直链亚烷基,每个亚甲基与连接有相应的任选取代的或苯并 - 稠合的5,6或7元环; W表示1-咪唑基,1-(1,2,4-或1,3,4) - 三唑基或3-吡啶基; 或W表示1-咪唑基,1-(1,2,4或1,3,4) - 三唑基或被低级烷基取代的3-吡啶基; 及其药学上可接受的盐。
    • 6. 发明授权
    • Alpha-heterocycle substituted tolunitriles
    • α-杂环取代的亚苄基
    • US5112845A
    • 1992-05-12
    • US628732
    • 1990-12-17
    • Robert M. BowmanRonald E. SteeleLeslie J. BrowneBruce H. EwaldRobert Diener
    • Robert M. BowmanRonald E. SteeleLeslie J. BrowneBruce H. EwaldRobert Diener
    • C07D213/57C07D521/00
    • C07D231/12C07D213/57C07D233/56C07D249/08
    • The invention is concerned with aromatase inhibiting compounds of formula I ##STR1## wherein R and Ro represent hydrogen or lower alkyl; or R and Ro located on adjacent carbon atoms and together when combined with the benzene ring to which they are attached form a naphthalene or tetrahydronaphthalene ring; R.sub.1 and R.sub.2 independently represent hydrogen, lower alkyl, (lower alkyl, aryl or aryl-lower alkyl)-thio, lower alkenyl, aryl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl, or C.sub.3 -C.sub.6 -cycloalkyl-lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylidene, mono- or di-aryl-lower alkylidene; R.sub.1 and R.sub.2 combined also represent C.sub.4 -C.sub.6 -straight chain alkylene, lower alkyl-substituted straight chain alkylene or ortho-phenylene bridged-C.sub.2 -C.sub.4 -straight chain alkylene, each forming with the carbon atom attached thereto a corresponding optionally substituted or benzo-fused 5, 6 or 7-membered ring; W represents 1-imidazolyl, 1-(1,2,4- or 1,3,4)-triazolyl or 3-pyridyl; or W represents 1-imidazolyl, 1-(1,2,4 or 1,3,4)-triazolyl or 3-pyridyl substituted by lower alkyl; and pharmaceutically acceptable salts thereof.
    • 本发明涉及芳香酶抑制化合物,其中R和R 4代表氢或低级烷基; 或R和Ro位于相邻的碳原子上并与它们所连接的苯环组合时形成萘或四氢萘环; R 1和R 2独立地表示氢,低级烷基,(低级烷基,芳基或芳基 - 低级烷基) - 硫代,低级链烯基,芳基,芳基 - 低级烷基,C 3 -C 6环烷基或C 3 -C 6环烷基 - 低级烷基。 或R 1和R 2组合​​表示低级亚烷基,单 - 或二 - 芳基 - 低级亚烷基; R1和R2组合也表示C4-C6-直链亚烷基,低级烷基取代的直链亚烷基或邻 - 亚苯基桥连的C 2 -C 4 - 直链亚烷基,每个亚甲基与连接有相应的任选取代的或苯并 - 稠合的5,6或7元环; W表示1-咪唑基,1-(1,2,4-或1,3,4) - 三唑基或3-吡啶基; 或W表示1-咪唑基,1-(1,2,4或1,3,4) - 三唑基或被低级烷基取代的3-吡啶基; 和其药学上可接受的盐。
    • 7. 发明授权
    • Alpha-heterocycle substituted tolunitriles
    • α-杂环取代的亚苄基
    • US5071861A
    • 1991-12-10
    • US510501
    • 1990-04-18
    • Robert M. BowmanRonald E. SteeleLeslie J. Browne
    • Robert M. BowmanRonald E. SteeleLeslie J. Browne
    • C07D213/57C07D249/08C07D521/00
    • C07D231/12C07D213/57C07D233/56C07D249/08
    • The invention is concerned with aromatase inhibiting compounds of formula I ##STR1## wherein R and Ro represent hydrogen or lower alkyl; or R and Ro located on adjacent carbon atoms and together when combined with the benzene ring to which they are attached form a naphthalene or tetrahydronaphthalene ring; R.sub.1 and R.sub.2 independently represent hydrogen, lower alkyl, (lower alkyl, aryl or aryl-lower alkyl)-thio, lower alkenyl, aryl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl, or C.sub.3 -C.sub.6 -cycloalkyl-lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylidene, mono- or di-aryl-lower alkylidene; R.sub.1 and R.sub.2 combined also represent C.sub.4 -C.sub.6 -straight chain alkylene, lower alkyl-substituted straight chain alkylene or ortho-phenylene bridged-C.sub.2 -C.sub.4 -straight chain alkylene, each forming with the carbon atom attached thereto a corresponding optionally substituted or benzo-fused 5, 6 or 7-membered ring; W represents 1-imidazolyl, 1-(1,2,4- or 1,3,4-triazolyl or 3-pyridyl; or W represents 1-imidazolyl, (1-1,2,4 or 1,3,4)-triazolyl or 3-pyridyl substituted by lower alkyl; and pharmaceutically acceptable salts thereof.
    • 本发明涉及芳香酶抑制化合物,其中R和R 4代表氢或低级烷基; 或R和Ro位于相邻的碳原子上并与它们所连接的苯环组合时形成萘或四氢萘环; R 1和R 2独立地表示氢,低级烷基,(低级烷基,芳基或芳基 - 低级烷基) - 硫代,低级链烯基,芳基,芳基 - 低级烷基,C 3 -C 6环烷基或C 3 -C 6环烷基 - 低级烷基。 或R 1和R 2组合​​表示低级亚烷基,单 - 或二 - 芳基 - 低级亚烷基; R1和R2组合也表示C4-C6-直链亚烷基,低级烷基取代的直链亚烷基或邻 - 亚苯基桥连的C 2 -C 4 - 直链亚烷基,每个亚甲基与连接有相应的任选取代的或苯并 - 稠合的5,6或7元环; W代表1-咪唑基,1-(1,2,4-或1,3,4-三唑多醇或3-吡啶基;或W代表1-咪唑基,(1-1,2,4或1,3,4) 三唑基或被低级烷基取代的3-吡啶基;及其药学上可接受的盐。