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    Bis-(Heteroarylmethoxyphenyl)cycloalkyl carboxylates as inhibitors of leukotriene biosynthesis
    1.
    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。

    Heteroarylmethoxyphenylthioalkyl carboxylates as inhibitors of leukotriene biosynthesis
    3.
    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。

    Oxime derivatives of indole and indene compounds as inhibitors of prostaglandin biosynthesis
    4.
    发明授权
    Oxime derivatives of indole and indene compounds as inhibitors of prostaglandin biosynthesis 失效
    吲哚和茚化合物的肟衍生物作为前列腺素生物合成的抑制剂

    公开(公告)号：US5750558A

    公开(公告)日：1998-05-12

    申请号：US660048

    申请日：1996-06-06

    申请人： Clint D. W. Brooks ,  Teodozyj Kolasa ,  Wendy Lee ,  Andrew O. Stewart

    发明人： Clint D. W. Brooks ,  Teodozyj Kolasa ,  Wendy Lee ,  Andrew O. Stewart

    IPC分类号： C07C317/32 ,  C07D209/14 ,  C07D257/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  A61K31/40

    CPC分类号： C07D257/04 ,  C07C317/32 ,  C07D209/14 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D417/14 ,  C07C2102/08

    摘要： Described herein are compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein L is selected from the group consisting of ##STR2## R.sup.2 is selected from (a) ##STR3## R.sup.3 is selected from optionally substituted phenyl, and optionally substituted pyridyl; Y is selected from halogen, alkyl, haloalkyl, alkoxy, pyridylmethoxy, thiazolylmethoxy, benzothiazolylmethoxy, quinolylmethoxy, and optionally substituted quinolylmethoxy; W is selected from hydrogen, alkyl, hydroxyalkyl, and hydroxy; A is absent or is selected from optionally substituted alkylene optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, and ##STR4## and X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from (b-1) a pharmaceutically acceptable metabolically cleavable group, (b-2)--OR.sup.10,(b-3)--O(CH.sub.2).sub.w --CH(OR.sup.12)--CH.sub.2 OR.sup.13, and (b-4)--NR.sup.15 R.sup.16 (c)--OR.sup.17, (d) tetrazolyl, (e)--CH(OR.sup.17)--CH.sub.2 OR.sup.18,(f)--CH(OR.sup.17)--CH.sub.2 --CH.sub.2 OR.sup.18, (g)--CH(OR.sup.17)--CH(OR.sup.18)--CH.sub.2 OR.sup.19, and (h).dbd.N--OR.sup.17 ; and R.sup.1 and R.sup.4 selected from (a) hydrogen, (b) alkyl, and (c) optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, and a method of inhibiting prostaglandin biosynthesis in a mammal.

    摘要翻译： 本文描述的是具有式“IMAGE”的化合物或其药学上可接受的盐，其中L选自由下列组成的组：R 2选自（a）图像（b）图像（c） （d）R 3选自任选取代的苯基和任选取代的吡啶基; Y选自卤素，烷基，卤代烷基，烷氧基，吡啶基甲氧基，噻唑基甲氧基，苯并噻唑基甲氧基，喹啉基甲氧基和任选取代的喹啉基甲氧基; W选自氢，烷基，羟基烷基和羟基; A不存在或选自任选取代的亚烷基任选取代的亚环烷基，任选取代的亚环烷基，其中一个或两个碳原子被一个或两个独立地选自O，S和N的杂原子替代，并且X不存在 或者是亚烷基; Z选自（a）氢，（b）COM，其中M选自（b-1）可药用代谢裂解基团，（b-2）-OR10，（b-3）-O（CH2）w- CH（OR 12）-CH 2 OR 13和（b-4）-NR 15 R 16（c）-OR 17，（d）四唑基，（e）-CH（OR 17）-CH 2 OR 18，（f）-CH（OR 17） （g）-CH（OR 17）-CH（OR 18）-CH 2 OR 19，和（h）= N-OR 17; 并且选自（a）氢，（b）烷基和（c）任选取代的苯基的R 1和R 4是前列腺素生物合成抑制剂，并且可用于治疗炎性疾病状态。 还公开了前列腺素抑制组合物和抑制哺乳动物中前列腺素生物合成的方法。

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

    公开(公告)号：US5668146A

    公开(公告)日：1997-09-16

    申请号：US703442

    申请日：1996-09-17

    申请人： Clint D. W. Brooks ,  Pramila Bhatia ,  Teodozyj Kolasa

    发明人： Clint D. W. Brooks ,  Pramila Bhatia ,  Teodozyj Kolasa

    IPC分类号： C07D213/30 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D239/26 ,  C07D241/42 ,  C07D263/56 ,  C07D277/24 ,  C07D277/64 ,  C07D417/14 ,  A61K31/47 ,  A61K31/44

    CPC分类号： C07D213/30 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D239/26 ,  C07D241/42 ,  C07D263/56 ,  C07D277/24 ,  C07D277/64 ,  C07D417/14

    摘要： Compounds having the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein W and Y at each occurrence are the same and W is selected from the group consisting of 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; Y is selected from optionally substituted phenylene and optionally substituted ##STR2## wherein the alkylene portion is of one to six carbon atoms; A is selected from alkylene, alkenylene, cycloalkylene, and optionally substituted ##STR3## wherein the alkylene portion is of one to six carbon atoms; and M is selected from hydrogen, a pharmaceutically acceptable cation, a pharmaceutically acceptable, metabolically cleavable group, --OR.sup.3, and --NR.sup.4 R.sup.5, 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 in a mammal.

    摘要翻译： 具有下式的化合物或其药学上可接受的盐，其中W和Y在每次出现时相同，W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，任选地 取代的喹喔啉基，任选取代的吡啶基，任选取代的嘧啶基和任选取代的噻唑基; Y选自任选取代的亚苯基和任选取代的，其中亚烷基部分具有1至6个碳原子; A选自亚烷基，亚烯基，亚环烷基和任选取代的，其中亚烷基部分为1至6个碳原子; 并且M选自氢，药学上可接受的阳离子，药学上可接受的，代谢可切割的基团-OR3和-NR4R5，抑制白三烯生物合成，并且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哺乳动物中白细胞三烯生物合成的方法。

    Oxime derivatives of fenamates as inhibitors of prostaglandin biosynthesis
    6.
    发明授权
    Oxime derivatives of fenamates as inhibitors of prostaglandin biosynthesis 失效
    芥酸肟衍生物作为前列腺素生物合成的抑制剂

    公开(公告)号：US5840758A

    公开(公告)日：1998-11-24

    申请号：US659474

    申请日：1996-06-06

    申请人： Clint D. W. Brooks ,  Teodozyj Kolasa ,  Wendy Lee ,  Andrew O. Stewart

    发明人： Clint D. W. Brooks ,  Teodozyj Kolasa ,  Wendy Lee ,  Andrew O. Stewart

    IPC分类号： C07C251/16 ,  C07C251/60 ,  C07C259/06 ,  C07D257/04 ,  A61K31/41 ,  A61K31/165 ,  A61K31/19 ,  A61K31/275

    CPC分类号： C07D257/04 ,  C07C251/16 ,  C07C251/60 ,  C07C259/06 ,  Y10S514/824 ,  Y10S514/825 ,  Y10S514/863 ,  Y10S514/886 ,  Y10S514/887 ,  Y10S514/916

    摘要： Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein Y is selected from halogen, alkyl, and haloalkyl; n is 0, 1, 2, or 3; A is selected from (a) optionally substituted alkylene, (b) optionally substituted cycloalkylene, (c) optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, (d) optionally substituted alkenylene and (e) ##STR2## X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from --OR.sup.4, --NR.sup.6 R.sup.7, and a pharmaceutically acceptable metabolically cleavable group, (c) --OR.sup.2, (d) tetrazolyl, (e) --CH(OR.sup.2)--CH.sub.2 OR.sup.8, (f) --CH(OR.sup.2)--CH.sub.2 --CH.sub.2 OR.sup.8, (g) --CH(OR.sup.2)--CH(OR.sup.8)--CH.sub.2 OR.sup.9, and (h).dbd.N--OR.sup.2 ; and R.sup.1 is selected from hydrogen, alkyl, and optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, a method of inhibiting prostaglandin biosynthesis in a mammal.

    摘要翻译： 具有式“IMAGE”的化合物或其药学上可接受的盐，其中Y选自卤素，烷基和卤代烷基; n为0,1,2或3; A选自（a）任选取代的亚烷基，（b）任选取代的亚环烷基，（c）任选取代的亚环烷基，其中一个或两个碳原子被一个或两个独立地选自O，S和N的杂原子置换，（ d）任选取代的亚烯基和（e）X不存在或是亚烷基; Z选自（a）氢，（b）COM，其中M选自-OR4，-NR6R7和药学上可接受的代谢可裂解基团，（c）-OR2，（d）四唑基，（e）-CH（OR2） ）-CH 2 OR 8，（f）-CH（OR 2）-CH 2 -CH 2 OR 8，（g）-CH（OR 2）-CH（OR 8）-CH 2 OR 9和（h）= N-OR 2; 并且R 1选自氢，烷基和任选取代的苯基，是前列腺素生物合成抑制剂，并且可用于治疗炎性疾病状态。 还公开了前列腺素抑制组合物，在哺乳动物中抑制前列腺素生物合成的方法。

    Iminoxyderivatives of fenamates as inhibitors of prostaglandin biosynthesis
    7.
    发明授权
    Iminoxyderivatives of fenamates as inhibitors of prostaglandin biosynthesis 失效
    作为前列腺素生物合成抑制剂的灭火剂的亚硝基衍生物

    公开(公告)号：US5863946A

    公开(公告)日：1999-01-26

    申请号：US660046

    申请日：1996-06-06

    申请人： Clint D. W. Brooks ,  Richard A. Craig ,  Teodozyj Kolasa ,  Andrew O. Stewart

    发明人： Clint D. W. Brooks ,  Richard A. Craig ,  Teodozyj Kolasa ,  Andrew O. Stewart

    IPC分类号： C07C251/58 ,  C07D257/04 ,  A61K31/195

    CPC分类号： C07D257/04 ,  C07C251/58

    摘要： Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein Y is selected from halogen, alkyl, and haloalkyl; n is 0, 1, 2, or 3; X is absent or is alkylene; A is absent or is selected from optionally substituted alkylene, optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, optionally substituted alkenylene, and ##STR2## or R.sup.2 and A together define a saturated 5- to 8-membered optionally substituted carbocyclic or heterocyclic ring to which the group Z is attached; Z is selected from (a) hydrogen, (b) COM wherein M is selected from the group consisting of --OR.sup.5, a pharmaceutically acceptable cation, --NR.sup.7 R.sup.8, and a pharmaceutically acceptable, metabolically cleavable group, (c) --OR.sup.3, (d) tetrazolyl, (e) --CH(OR.sup.3)--CH.sub.2 OR.sup.9, (f) --CH(OR.sup.3)--CH.sub.2 --CH.sub.2 OR.sup.9, (g) --CH(OR.sup.3)--CH(OR.sup.9)--CH.sub.2 OR.sup.10, and (h) .dbd.N--OR.sup.3 ; and R.sup.1, R.sup.2, R.sup.3, R.sup.9, and R.sup.10 are independently selected from (a) hydrogen, (b) alkyl, and (c) optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, a method of inhibiting prostaglandin biosynthesis in a mammal.

    摘要翻译： 具有式“IMAGE”的化合物或其药学上可接受的盐，其中Y选自卤素，烷基和卤代烷基; n为0,1,2或3; X不存在或是亚烷基; A不存在或选自任选取代的亚烷基，任选取代的亚环烷基，任选取代的亚环烷基，其中一个或两个碳原子被一个或两个独立地选自O，S和N的杂原子，任选取代的亚烯基取代，以及

    Bis-heteroarylylmethoxyphenyl ketone derivatives as inhibitors of leukotriene biosynthesis
    8.
    发明授权
    Bis-heteroarylylmethoxyphenyl ketone derivatives as inhibitors of leukotriene biosynthesis 失效
    双杂芳基甲氧基苯基酮衍生物作为白三烯生物合成的抑制剂

    公开(公告)号：US5714488A

    公开(公告)日：1998-02-03

    申请号：US703440

    申请日：1996-09-17

    申请人： Clint D. W. Brooks ,  Pramila Bhatia ,  Teodozyj Kolasa

    发明人： Clint D. W. Brooks ,  Pramila Bhatia ,  Teodozyj Kolasa

    IPC分类号： C07D213/30 ,  C07D213/36 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D239/26 ,  C07D241/42 ,  C07D263/56 ,  C07D277/24 ,  C07D277/64 ,  C07D417/14 ,  A61K31/47

    CPC分类号： C07D213/30 ,  C07D213/36 ,  C07D215/14 ,  C07D215/18 ,  C07D235/12 ,  C07D239/26 ,  C07D241/42 ,  C07D263/56 ,  C07D277/24 ,  C07D277/64 ,  C07D417/14

    摘要： Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein W is selected from the group consisting of 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 one or more groups independently selected from hydrogen, alkyl, halolalkyl, alkoxy, and halogen; Z is selected from the group consisting of N--OH, N--O--A--COM, CH--COM, and CH--CH.dbd.N--0--A--COM wherein A is selected from the group consisting of alkylene, alkenylene, cycloalkylene, and optionally substituted alkylphenyl wherein the alkyl portion is of one to six carbon atoms, and M is selected from the group consisting of a pharmaceutically acceptable, metabolically clearable group, --OR.sup.3, and --NR.sup.4 R.sup.5, 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： 具有式“IMAGE”的化合物或其药学上可接受的盐，其中W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， 和任选取代的噻唑基; R1和R2是独立地选自氢，烷基，卤代烷基，烷氧基和卤素的一个或多个基团; Z选自N-OH，NOA-COM，CH-COM和CH-CH = N-O-A-COM，其中A选自亚烷基，亚烯基，亚环烷基和任选取代的 烷基苯基，其中烷基部分为1至6个碳原子，M选自药学上可接受的，可代谢的基团-OR3和-NR4R5，抑制白三烯生物合成，并且可用于治疗过敏和炎症 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。