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1. 发明授权

US5516789A Lipoxygenase and cyclooxygenase inhibiting compounds 失效
标题翻译：脂氧合酶和环加氧酶抑制化合物
公开(公告)号：US5516789A
公开(公告)日：1996-05-14
申请号：US421125
申请日：1995-04-12
申请人： Clint D. W. Brooks , Andrew O. Stewart , Anwer Basha , Randy L. Bell
发明人： Clint D. W. Brooks , Andrew O. Stewart , Anwer Basha , Randy L. Bell
IPC分类号： C07C275/64 , C07D307/52 , C07D333/20 , C07D333/58 , C07D409/12 , A61K31/405 , C07D209/14
CPC分类号： C07D409/12 , C07C275/64 , C07D307/52 , C07D333/20 , C07D333/58
摘要： Compounds having the structure ##STR1## or a pharmaceutically acceptable salt thereof have activity as inhibitors of cylooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4 and cylooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optinally substituted carbocyclic aryl, (b) optinally substituted furyl, (c) optinally substituted benzo[b]furyl, (d) optinally substituted thienyl, (e) optinally substituted pyridyloxy, (f) optinally substituted pyridylalkyl, (g) optinally substituted benzo[b]thienyl, (h) optinally substituted pyridyl, (i) optinally substituted quinolyl, and (j) optinally substituted indolyl; X is selected from (a) optionally substituted alkyl, (b) optinally substituted alkenyl, and (c) optinally substituted alkynyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, hydroxy, and alkyl; and Z is a residue of a non-steroidal anti-inflammatory drug of the general formula Z--COOH.
摘要翻译：具有结构或其药学上可接受的盐的化合物具有作为环氧合酶和5-脂氧合酶抑制剂的活性，降低白细胞三烯B4，C4，D4和E4以及环加氧酶产物如前列腺素和血栓烷的生物合成，并且可用于治疗炎症和过敏性疾病状态。化合物具有上述结构，其中A选自（a）光学取代的碳环芳基，（b）光取代的呋喃基，（c）光取代的苯并[b]呋喃基，（d）最佳取代的噻吩基，（e）吡啶基氧基，（f）选择性取代的吡啶基烷基，（g）最佳取代的苯并[b]噻吩基，（h）最佳取代的吡啶基，（i）最佳取代的喹啉基和（j） X选自（a）任选取代的烷基，（b）光学取代的烯基和（c）最佳取代的炔基; R 1和R 2独立地选自氢，羟基和烷基; Z为通式Z-COOH的非甾体抗炎药物的残基。

2. 发明授权

US5616596A Substituted arylalkynyl-and heteroarylalkynl-N-hydroxyurea inhibitors of leukotriene biosynthesis 失效
标题翻译：白三烯生物合成的取代的芳基炔基和杂芳基炔基-N-羟基脲抑制剂
公开(公告)号：US5616596A
公开(公告)日：1997-04-01
申请号：US416807
申请日：1995-04-13
申请人： Anwer Basha , Clint D. W. Brooks , Pramila Bhatia , Richard A. Craig , James D. Ratajczyk , Andrew O. Stewart
发明人： Anwer Basha , Clint D. W. Brooks , Pramila Bhatia , Richard A. Craig , James D. Ratajczyk , Andrew O. Stewart
IPC分类号： A61K31/17 , A61K31/38 , A61K31/381 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4433 , A61P9/00 , A61P9/10 , A61P11/00 , A61P17/00 , A61P25/00 , A61P27/16 , A61P29/00 , A61P37/08 , A61P43/00 , C07C273/18 , C07C275/24 , C07C275/64 , C07D213/61 , C07D277/28 , C07D307/52 , C07D333/20 , C07D333/22 , C07D405/06 , C07D409/04 , C07D409/06 , C07D417/04 , A61K31/42 , C07D263/30 , C07D277/20
CPC分类号： C07D405/06 , C07C275/64 , C07D213/61 , C07D277/28 , C07D307/52 , C07D333/20 , C07D409/06
摘要： The invention relates to compounds having activity to inhibit lipoxygenase enzyme activity, to pharmaceutical compositions comprising these compounds, and to a medical method of treating. More particularly, this invention concerns certain substituted arylalkynyl- and ((heteroaryl)alkynyl)-N-hydroxy-ureas which inhibit leukotriene biosynthesis, to pharmaceutical compositions of these compounds and to a method of inhibiting leukotriene biosynthesis.
摘要翻译： PCT No.PCT / US93 / 10675 Sec。 371日期1995年04月13日 102（e）日期1995年4月13日PCT 1993年11月5日PCT公布。公开号WO94 / 11342 日期：1994年5月26日本发明涉及具有抑制脂氧合酶活性的活性的化合物，涉及包含这些化合物的药物组合物以及治疗方法。更具体地，本发明涉及抑制白细胞三烯生物合成的某些取代的芳基炔基 - 和（（杂芳基）炔基）-N-羟基脲，这些化合物的药物组合物和抑制白三烯生物合成的方法。

3. 发明授权

US5446055A Polyether naphthalenic lignan lactones as inhibitors of 5-lipoxygenase 失效
标题翻译：聚醚萘木酚素内酯作为5-脂氧合酶的抑制剂
公开(公告)号：US5446055A
公开(公告)日：1995-08-29
申请号：US344443
申请日：1994-11-23
申请人： Joseph F. Dellaria , James D. Ratajczyk , Clint D. W. Brooks , Anwer Basha
发明人： Joseph F. Dellaria , James D. Ratajczyk , Clint D. W. Brooks , Anwer Basha
IPC分类号： C07D307/92 , C07D405/04 , C07D405/14 , C07D407/12 , C07D409/04 , C07D409/14 , A61K31/44
CPC分类号： C07D307/92 , C07D405/04 , C07D405/14 , C07D407/12 , C07D409/04 , C07D409/14
摘要： Compounds of formula ##STR1## Ar is optionally substituted phenyl, furyl, pyridyl, or thienyl; Y is selected from hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, and alkoxycarbonyl; L is selected from ##STR2## and R.sup.1 and R.sup.2 are alkyl or together define a group of formula ##STR3## are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
摘要翻译：式的化合物Ar是任选取代的苯基，呋喃基，吡啶基或噻吩基; Y选自氢，卤素，氰基，烷基，卤代烷基，烷氧基和烷氧基羰基; L选自，R 1和R 2是烷基或一起界定一组式（IMAGE）是脂氧合酶的有效抑制剂，从而抑制白细胞三烯的生物合成。这些化合物可用于治疗或改善过敏性和炎性疾病状态。

4. 发明授权

US5426111A [Alkoxy-, alkenyloxy-, alkynyloxy-, and phenylmethyloxyalkoxycycloalkyl or alkoxycycloheteroalkyl]naphtho[2,3-c]furan-1(3H)-one inhibitors of 5-lipoxygenase 失效
标题翻译：烷氧基 - ，烯氧基 - ，炔氧基 - 和苯基甲氧基烷氧基环烷基或烷氧基环杂烷基]萘并[2,3-c]呋喃-1（3H） - 酮抑制剂5-脂氧合酶
公开(公告)号：US5426111A
公开(公告)日：1995-06-20
申请号：US344774
申请日：1994-11-23
申请人： Joseph F. Dellaria , James D. Ratajczyk , Clint D. W. Brooks , Anwer Basha
发明人： Joseph F. Dellaria , James D. Ratajczyk , Clint D. W. Brooks , Anwer Basha
IPC分类号： C07C65/26 , C07D307/92 , C07D405/04 , C07D405/14 , C07D407/12 , C07D407/14 , C07D409/04 , C07D409/14 , A61K31/435 , C07C63/64 , C07D315/00 , C07D409/00
CPC分类号： C07D307/92 , C07C65/26 , C07D405/04 , C07D405/14 , C07D407/12 , C07D407/14 , C07D409/04 , C07D409/14
摘要： Compounds of formula ##STR1## Ar is selected from (a) phenyl, (b) phenyl substituted with one or more groups selected from halogen, cyano, alkyl, haloalkyl, alkoxy, and alkoxycarbonyl, (c) furyl, (d) furyl substituted with one or more groups selected from halogen, alkyl, and alkoxy, (e) pyridyl, (f) pyridyl substituted with one or more groups selected from halogen, alkyl, and alkoxy, (g) thienyl, and (h) thienyl substituted with one or more groups selected from halogen, alkyl, and alkoxy; L is selected from alkylene of one to three carbon atoms, alkenylene of two to three carbon atoms, and alkynylene of two to three carbon atoms, and ##STR2## wherein p is an integer of 1 to 4, inclusive, and R.sup.4 is selected from the group consisting of hydrogen, alkyl of one to four carbon atoms, halogen, haloalkyl of one to four carbon atoms, and alkoxy of one to six carbon atoms;R.sup.1 is alkyl; R.sup.2 is hydrogen or alkyl; m is 1 or 2; Z is oxygen or CHOR.sup.3, and n is 0 or 1 are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
摘要翻译：式（Ia）化合物选自（a）苯基，（b）被一个或多个选自卤素，氰基，烷基，卤代烷基，烷氧基和烷氧基羰基的基团取代的苯基，（c）呋喃基，（d （f）吡啶基，（f）被一个或多个选自卤素，烷基和烷氧基的基团取代的吡啶基，（g）噻吩基，和（h）被卤素，烷基和烷氧基取代的吡啶基，被一个或多个选自卤素，烷基和烷氧基的基团取代的噻吩基; L选自1至3个碳原子的亚烷基，2至3个碳原子的亚烯基和2至3个碳原子的亚炔基，和其中p是1至4的整数，并且R 4选自由氢，1-4个碳原子的烷基，卤素，1-4个碳原子的卤代烷基和1至6个碳原子的烷氧基组成的组; R1是烷基; R2是氢或烷基; m为1或2; Z是氧或CHOR3，n是0或1是脂氧合酶的有效抑制剂，从而抑制白细胞三烯的生物合成。这些化合物可用于治疗或改善过敏性和炎性疾病状态。

5. 发明授权

US5750558A Oxime derivatives of indole and indene compounds as inhibitors of prostaglandin biosynthesis 失效
标题翻译：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。

6. 发明授权

US5756531A Iminoxy derivatives of indole and indene compounds as inhibitors of prostaglandin biosynthesis 失效
标题翻译：吲哚和茚化合物的亚氨基衍生物作为前列腺素生物合成的抑制剂
公开(公告)号：US5756531A
公开(公告)日：1998-05-26
申请号：US640271
申请日：1996-04-30
申请人： Clint D. W. Brooks , Richard A. Craig , David E. Gunn , Teodozyji Kolasa , Jimmie L. Moore , Andrew O. Stewart
发明人： Clint D. W. Brooks , Richard A. Craig , David E. Gunn , Teodozyji Kolasa , Jimmie L. Moore , Andrew O. Stewart
IPC分类号： C07C317/22 , C07C323/19 , C07D209/12 , C07D213/30 , C07D257/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/40 , A61K31/405 , C07D209/14
CPC分类号： C07D213/30 , C07C317/22 , C07C323/19 , C07D209/12 , C07D257/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07C2102/08
摘要： The present invention provides a class of substituted indole and indene iminoxy derivatives of the formula ##STR1## which inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states.
摘要翻译：本发明提供了一类抑制白细胞三烯生物合成的式“IMAGE”，“IMAGE”和“IMAGE”的吲哚和茚亚氨基衍生物，可用于治疗过敏性和炎症性疾病。

7. 发明授权

US5863946A Iminoxyderivatives of fenamates as inhibitors of prostaglandin biosynthesis 失效
标题翻译：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

8. 发明授权

US5843968A Symmetrical bis-heteroarylmethoxy-phenylalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
标题翻译：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：US5843968A
公开(公告)日：1998-12-01
申请号：US958301
申请日：1997-10-27
申请人： Clint D. W. Brooks , Pramila Bhatia , Teodozyj Kolasa , Andrew O. Stewart , David E. Gunn , Richard A. Craig
发明人： Clint D. W. 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 , A61K31/38 , A61K31/405 , A61K31/42 , A61K31/425
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; R1和R2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。

9. 发明授权

US5840758A Oxime derivatives of fenamates as inhibitors of prostaglandin biosynthesis 失效
标题翻译：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。

10. 发明授权

US5691351A Bis-(Heteroarylmethoxyphenyl)cycloalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
标题翻译：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。

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