公开(公告)号：US06294580B1

公开(公告)日：2001-09-25

申请号：US09125750

申请日：1998-08-25

申请人： Timothy Mark Willson ,  Robert Anthony Mook ,  Istvan Kaldor ,  Brad Richard Henke ,  David Norman Deaton ,  Jon Loren Collins ,  Jeffrey Edmond Cobb ,  Marcus Brackeen ,  Matthew Jude Sharp ,  John Mark O'Callaghan ,  Greg Alan Erickson ,  Grady Evan Boswell

发明人： Timothy Mark Willson ,  Robert Anthony Mook ,  Istvan Kaldor ,  Brad Richard Henke ,  David Norman Deaton ,  Jon Loren Collins ,  Jeffrey Edmond Cobb ,  Marcus Brackeen ,  Matthew Jude Sharp ,  John Mark O'Callaghan ,  Greg Alan Erickson ,  Grady Evan Boswell

IPC分类号： A61K3119

CPC分类号： C07D213/64 ,  A61K31/192 ,  A61K31/216 ,  A61K31/353 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/422 ,  A61K31/423 ,  A61K31/425 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4439 ,  A61K31/4453 ,  A61K31/454 ,  A61K31/495 ,  C07C229/36 ,  C07C229/56 ,  C07C237/40 ,  C07C255/54 ,  C07C323/12 ,  C07C2601/14 ,  C07C2601/16 ,  C07D207/08 ,  C07D213/65 ,  C07D213/70 ,  C07D213/74 ,  C07D231/12 ,  C07D233/64 ,  C07D235/12 ,  C07D237/14 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D263/56 ,  C07D277/24 ,  C07D277/42 ,  C07D311/22 ,  C07D333/36 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04

摘要： A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C1-6alkyl, C1-3alkoxy, C1-3fluoroalkoxy, nitrile, or —NR7R8 where R7 and R8 are independently hydrogen or C1-3alkyl; (ii) a 5- or 6-membered hetrocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C1-6alkylene; (v) —MC1-6alkylene or C1-6alkyleneMC1-6alkylene, wherein M is O, S, or —NR2 wherein R2 represents hydrogen or C1-3alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C1-3alkyl; and (vii) Het-C1-6alkylene, wherein Het represents a heterocyclic group as defined in point (vi) above; Alk represents C1-3alkylene; R1 represents hydrogen or C1-3alkyl; Z is selected from the group consisting of: (viii) —(C1-3alkylene) phenyl, which phenyl is optionally substituted by one or more halogen atoms; and (ix) —NR3R4, wherein R3 represents hydrogen or C1-3alkyl, and R4 represents —Y—(C═O)—T—R5, or —Y—(CH(OH))—T—R5.

摘要翻译： 具有式（I）的化合物，其中A选自：（i）苯基，其中所述苯基任选被一个或多个卤素原子取代，C 1-6烷基，C 1-3烷氧基，C 1-3氟烷氧基，腈， 或-NR 7 R 8，其中R 7和R 8独立地是氢或C 1-3烷基; （ii）含有至少一个选自氧，氮和硫的杂原子的5-或6-元环庚基; 和（iii）稠合双环（a），其中环C表示如上述点（ii）中所定义的杂环基，该双环通过环C的环原子连接至基团B; B选自：（iv）C 1-6亚烷基; （v）-MC1-6亚烷基或C 1-6亚烷基基团，C 1-6亚烷基，其中M为O，S或-NR 2，其中R 2表示氢或C 1-3烷基; （vi）含有至少一个氮杂原子和任选至少一个选自氧，氮和硫的另外的杂原子并任选被C 1-3烷基取代的5-或6-元杂环基; 和（vii）Het-C 1-6亚烷基，其中Het表示如上述（vi）中所定义的杂环基; Alk表示C1-3亚烷基; R1代表氢或C1-3烷基; Z选自：（ii） - （C 1-3亚烷基）苯基，该苯基任选被一个或多个卤素原子取代; 和（ix）-NR3R4，其中R3表示氢或C1-3烷基，R4表示-Y-（C = O）-T-R5或-Y-（CH（OH））-T-R5。