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    Heteroarylmethoxyphenylthioalkyl carboxylates as inhibitors of leukotriene biosynthesis
    2.
    发明授权
    Heteroarylmethoxyphenylthioalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
    作为白三烯生物合成抑制剂的杂芳基甲氧基苯硫基烷基羧酸盐

    公开(公告)号：US5783586A

    公开(公告)日：1998-07-21

    申请号：US724200

    申请日：1996-10-01

    申请人： Teodozyj Kolasa ,  Clint D. W. Brooks ,  David E. Gunn

    发明人： Teodozyj Kolasa ,  Clint D. W. Brooks ,  David E. Gunn

    IPC分类号： C07D215/14 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  A61K31/47

    CPC分类号： C07D405/14 ,  C07D215/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14

    摘要： Compounds having the formula: ##STR1## wherein W.sup.1 and W.sup.2 are independently selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted naphthyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is selected from thienyl, furyl, phenyl, naphthyl, benzo�b!thienyl, alkyl, hydroxyl, and hydrogen; Y an alkylene of one to six carbon atoms; and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.4, (c) --NR.sup.5 R.sup.6, (d)--NR.sup.4 SO.sub.2 R.sup.7 (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W1和W2独立地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，任选取代的萘基; R 1和R 2独立地选自氢，烷基，卤代烷基，烷氧基，卤素; R 3选自噻吩基，呋喃基，苯基，萘基，苯并[b]噻吩基，烷基，羟基和氢; Y为1至6个碳原子的亚烷基; 并且M选自（a）药学上可接受的代谢可裂解基团，（b）-OR4，（c）-NR5R6，（d）-NR4SO2R7（e）-NH-四唑基和（f）甘氨酰基; 抑制白细胞三烯生物合成，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。

    Bis-(Heteroarylmethoxyphenyl)cycloalkyl carboxylates as inhibitors of leukotriene biosynthesis
    3.
    发明授权
    Bis-(Heteroarylmethoxyphenyl)cycloalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
    双（（杂芳基甲氧基苯基）环烷基羧酸盐作为白三烯生物合成的抑制剂

    公开(公告)号：US5691351A

    公开(公告)日：1997-11-25

    申请号：US596058

    申请日：1996-02-06

    申请人： Teodozyj Kolasa ,  David E. Gunn ,  Clint D. W. Brooks

    发明人： Teodozyj Kolasa ,  David E. Gunn ,  Clint D. W. Brooks

    IPC分类号： C07D215/14 ,  C07D215/18 ,  C07D241/42 ,  C07D277/64 ,  A61K31/47 ,  C07D401/12

    CPC分类号： C07D215/18 ,  C07D215/14 ,  C07D241/42 ,  C07D277/64

    摘要： Compounds having the structure ##STR1## where m is an integer of from one to nine; n is an integer of from one to four; W is selected from substituted or unsubstituted quinolyl, benzothiazolyl, or quinoxalyl, X is selected from C.sub.1-6 alkylene, C.sub.2-6 alkenylene and C.sub.2-6 alkynylene; Y is selected from halogen, C.sub.1-6 alkyl and C.sub.1-6, alkoxy; and Z is selected from --C(O)B; --C(R.sub.2).sup.2 --O--N.dbd.A--C(O)B; and --C(R.sup.2).dbd.N--O--A--C(O)B where A is C.sub.1-6 alkylene and B is --OH, --O--M.sup.+, --OD where D is a metabolically cleavable group, --OR.sup.6 where R.sup.6 is hydrogen or C.sub.1-6 alkyl, --NR.sup.6 R.sup.7 where R.sup.7 is hydrogen, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkoxy, or where R.sup.6 and R.sup.7 taken together form a five to eight membered ring optionally containing one heteroatom selected from nitrogen, oxygen or sulfur, are inhibitors of leukotriene biosynthesis.

    摘要翻译： 具有结构的化合物，其中m是1至9的整数; n是1到4的整数; W选自取代或未取代的喹啉基，苯并噻唑基或喹喔啉基，X选自C 1-6亚烷基，C 2-6亚烯基和C 2-6亚炔基; Y选自卤素，C 1-6烷基和C 1-6烷氧基; 并且Z选自-C（O）B; -C（R 2）2 -O-N = A-C（O）B; 和-C（R 2）= NOAC（O）B，其中A是C 1-6亚烷基，B是-OH，-O-M +，-OD，其中D是代谢可裂解基团，-OR 6，其中R 6是氢或C 1-6 烷基，-NR 6 R 7，其中R 7是氢，C 1-6烷基，羟基或C 1-6烷氧基，或者其中R 6和R 7一起形成任选地含有一个选自氮，氧或硫的杂原子的五至八元环， 白三烯生物合成。

    Non-symmetrical bis-heteroarylmethoxyphenylalkyl carboxylates as inhibitors of leukotriene biosynthesis
    5.
    发明授权
    Non-symmetrical bis-heteroarylmethoxyphenylalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
    非对称双杂芳基甲氧基苯基烷基羧酸盐作为白三烯生物合成的抑制剂

    公开(公告)号：US5668150A

    公开(公告)日：1997-09-16

    申请号：US686841

    申请日：1996-07-26

    申请人： Clint D.W. Brooks ,  Teodozyj Kolasa ,  David E. Gunn

    发明人： Clint D.W. Brooks ,  Teodozyj Kolasa ,  David E. Gunn

    IPC分类号： A61K31/47 ,  A61K31/4709 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D215/14 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/475 ,  C07D215/18

    CPC分类号： C07D401/12 ,  C07D215/14 ,  C07D413/12 ,  C07D417/12

    摘要： Compounds having the formula ##STR1## wherein W and Y are independently selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, and optionally substituted naphthyl with the proviso that W and Y are not simultaneously the same substituent; R.sup.1 and R.sup.2 are independently hydrogen, alkyl, haloalkyl, alkoxy, or halogen; R.sup.3 is hydrogen or alkyl; X is absent or is alkylene, alkenylene, or alkynylene; and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.4 wherein R.sup.4 is hydrogen or alkyl; and (c) --NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from hydrogen, alkyl, hydroxy and alkoxy are disclosed. These compounds inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states.

    摘要翻译： 具有式的化合物，其中W和Y独立地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和任选取代的萘基，条件是W和Y不同时为 相同的取代基; R1和R2独立地是氢，烷基，卤代烷基，烷氧基或卤素; R3是氢或烷基; X不存在或是亚烷基，亚烯基或亚炔基; 并且M选自（a）药学上可接受的代谢可切割基团，（b）-OR 4，其中R 4是氢或烷基; 和（c）-NR 5 R 6，其中R 5和R 6独立地选自氢，烷基，羟基和烷氧基。 这些化合物抑制白细胞三烯生物合成，并且可用于治疗过敏性和炎性疾病状态。

    Symmetrical bis-heteroaryl-methoxy-phenylalkyl carboxylates as inhibitors of leukotriene biosynthesis
    6.
    发明授权
    Symmetrical bis-heteroaryl-methoxy-phenylalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
    对称双杂芳基 - 甲氧基 - 苯基烷基羧酸盐作为白三烯生物合成的抑制剂

    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。