公开(公告)号：US5795900A

公开(公告)日：1998-08-18

申请号：US703441

申请日：1996-09-17

申请人： Clint D. Brooks ,  Pramila Bhatia ,  Teodozyj Kolasa ,  Andrew O. Stewart ,  David E. Gunn ,  Richard A. Craig

发明人： Clint D. Brooks ,  Pramila Bhatia ,  Teodozyj Kolasa ,  Andrew O. Stewart ,  David E. Gunn ,  Richard A. Craig

IPC分类号： C07D239/26 ,  A61K31/4184 ,  A61K31/421 ,  A61K31/4402 ,  A61K31/454 ,  A61K31/47 ,  A61K31/498 ,  A61K31/506 ,  A61P37/08 ,  A61P43/00 ,  C07D213/30 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D241/42 ,  C07D263/56 ,  C07D277/24 ,  C07D277/64 ,  C07D417/14 ,  C07D401/10

CPC分类号： C07D213/30 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D241/42 ,  C07D277/64

摘要： Compounds having the formula: ##STR1## wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH.dbd.N--O--A--COM, (c) CH.sub.2 --O--N.dbd.A--COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.6, (c) --NR.sup.7 R.sup.8, (d)--NR.sup.6 SO.sub.2 R.sup.9, (e)-NH-Tetrazolyl, and (f) glycinyl inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.

摘要翻译： 具有下式的化合物：其中W在每次出现时相同，并且选自任选取代的喹啉基，任选取代的苯并噻唑基，任选取代的苯并恶唑基，任选取代的苯并咪唑基，任选取代的喹喔啉基，任选取代的吡啶基，任选取代的嘧啶基， 取代的噻唑基; R 1和R 2独立地选自氢，烷基，卤代烷基，烷氧基，卤素; R3是价键或选自氢和烷基; X是价键或选自亚烷基，烯基和亚炔基; 并且Z选自（a）COM，（b）CH = NOA-COM，（c）CH2-ON = A-COM其中A选自亚烷基和亚环烷基，M选自（a）药学上可接受的代谢 可裂解基团，（b）-OR6，（c）-NR7R8，（d）-NR6SO2R9，（e）-NH-四唑基，（f）甘氨酰抑制白三烯生物合成，可用于治疗过敏性和炎性疾病状态。 还公开了白三烯生物合成抑制组合物和抑制白三烯生物合成的方法。