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11. 发明授权

US5250565A Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds 失效
标题翻译：含吲哚，苯并呋喃和苯并噻吩的脂氧合酶抑制化合物
公开(公告)号：US5250565A
公开(公告)日：1993-10-05
申请号：US823411
申请日：1992-01-21
申请人： Dee W. Brooks , James B. Summers
发明人： Dee W. Brooks , James B. Summers
IPC分类号： C07D209/14 , C07D307/81 , C07D333/58 , A61K31/38 , A61K31/34 , C07D209/04 , C07D333/52
CPC分类号： C07D209/14 , C07D307/81 , C07D333/58
摘要： Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula ##STR1## in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted nitrogen, and Y is a group which includes substituted or unsubstituted carbocyclic or substituted or unsubstituted heterocyclic aryl. R.sup.1 is an alkyl, alkenyl, amino, alkylamino, dialkylamino, or hydroxyamino group or an amine group bearing a metabolically cleavable leaving group. M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable leaving group, with the proviso that either M or R.sup.1 must bear a metabolically cleavable leaving group.
摘要翻译：有效的5-脂氧合酶抑制化合物的前药包括其中A为亚烷基或亚烯基的式（IMAGE）化合物，X为氧，硫，亚砜基或取代的氮，Y为包括取代或未取代的基团碳环或取代或未取代的杂环芳基。 R 1是烷基，烯基，氨基，烷基氨基，二烷基氨基或羟基氨基或具有代谢可切割离去基团的胺基。 M是氢，药学上可接受的阳离子或代谢可切割的离去基团，条件是M或R 1必须承载代谢可切割的离去基团。

12. 发明授权

US5214204A Arylamidoalkyl-N-hydroxyurea compounds having lipoxygenase inhibitory activity 失效
标题翻译：具有LIPOXYGENASE抑制活性的ARYLAMIDOALKYL-N-HYDROXYUREA化合物
公开(公告)号：US5214204A
公开(公告)日：1993-05-25
申请号：US732520
申请日：1991-07-19
申请人： Joseph F. Dellaria , Dee W. Brooks , Jimmie L. Moore , Kevin J. Sallin
发明人： Joseph F. Dellaria , Dee W. Brooks , Jimmie L. Moore , Kevin J. Sallin
IPC分类号： A61K31/165 , A61K31/17 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P29/00 , A61P43/00 , C07C275/64 , C07C311/13 , C07C311/18 , C07C311/27 , C07C311/29 , C07C311/35 , C07C311/41 , C07C317/40 , C07C317/44 , C07C323/41 , C07C323/60 , C07D207/34 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/38 , C07D213/64 , C07D213/65 , C07D213/68 , C07D215/48 , C07D233/64 , C07D233/68 , C07D233/70 , C07D233/88 , C07D239/26 , C07D277/20 , C07D277/24 , C07D277/26 , C07D277/28 , C07D277/56 , C07D307/38 , C07D307/42 , C07D307/52 , C07D307/68 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/84 , C07D307/85 , C07D333/16 , C07D333/18 , C07D333/20 , C07D333/36 , C07D333/38 , C07D333/54 , C07D333/56 , C07D333/70 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D213/64 , C07C275/64 , C07C311/18 , C07C317/40 , C07C317/44 , C07C323/41 , C07C323/60 , C07D207/34 , C07D215/48 , C07D277/56 , C07D307/68 , C07D307/85 , C07D333/20 , C07D333/38 , C07D333/70 , C07D405/12
摘要： The present invention provides certain (substituted carbocyclic aryl)amidoalkyl-and (substituted heterocyclic aryl)amidoalkyl-N-Hydroxy urea compounds which inhibit lipoxygenase enzyme activity and are thus useful in the treatment of allergic and inflammatory disease states.
摘要翻译：本发明提供某些（取代的碳环芳基）酰氨基烷基 - 和（取代的杂环芳基）酰氨基烷基-N-羟基脲化合物，其抑制脂氧合酶活性并因此可用于治疗过敏性和炎性疾病状态。

13. 发明授权

US5124342A 4-hydroxythiazoles as 5-lipoxygenase inhibitors 失效
公开(公告)号：US5124342A
公开(公告)日：1992-06-23
申请号：US553836
申请日：1990-07-18
申请人： Francis A. J. Kerdesky , James H. Holms , Dee W. Brooks
发明人： Francis A. J. Kerdesky , James H. Holms , Dee W. Brooks
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61K31/44 , A61P1/00 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D277/34 , C07D277/54 , C07D277/64 , C07D417/04
CPC分类号： C07D417/04 , C07D277/34 , C07D277/54 , C07D277/64
摘要： A composition for the inhibition of lipoxygenase enzymes comprising a pharmaceutically acceptable carrier and a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, arylalkenyl, reduced heteroaryl, and reduced heteroarylalkyl and substituted derivatives thereof having one or more substituents independently selected from the group consisting of halogen, alkyl, halosubstituted alkyl, aryl, arylalkyl, reduced heteroaryl, arylalkoxy, cyano, nitro, COR.sub.4, SO.sub.2 R.sub.4, NR.sub.5 R.sub.6, OR.sub.6, COCX.sub.1 X.sub.2 NR.sub.6 R.sub.7, CON(OH)R.sub.6, NR.sub.6 COR.sub.4, CR.sub.5 (NH.sub.2)CO.sub.2 R.sub.5, NHCX.sub.1 X.sub.2 CO.sub.2 R.sub.5, N(OH)CONR.sub.5 R.sub.6, N(OH)COR.sub.4, NHCONR.sub.5 R.sub.6, C(NOH)NHOH and CONHNR.sub.5 R.sub.6 ;R.sub.3 is selected from the group consisting of hydrogen, a pharmaceutically acceptable salt, COR.sub.4, COCX.sub.1 X.sub.2 NR.sub.6 R.sub.7, CR.sub.8 R.sub.9 OR.sub.10, CH.sub.2 CR.sub.8 (OR.sub.10)CH.sub.2 OR.sub.11 and SiR.sub.12 R.sub.13 R.sub.14 ;R.sub.4 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced heteroaryl, reduced heteroarylalkyl, OR.sub.5, NHCX.sub.1 X.sub.2 CO.sub.2 R.sub.5 and NR.sub.6 R.sub.7 ;R.sub.5 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, reduced heteroaryl, and reduced heteroarylalkyl;R.sub.6 and R.sub.7 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, reduced heteroaryl, reduced heteroarylalkyl and (CH.sub.2).sub.n OR.sub.5 where n is 2-4 and R.sub.5 is as defined above;R.sub.8, R.sub.9, R.sub.10 and R.sub.11 are independently selected from the group consisting of hydrogen, alkyl, aryl, arylalkyl and (CH.sub.2).sub.n OR.sub.5 or at least two of R.sub.8, R.sub.9, R.sub.10 and R.sub.11 together form a ring system containing 5-10 atoms wherein said ring system is carbocyclic, heterocyclic or reduced heterocyclic and R.sub.5 and n are as defined above;R.sub.12, R.sub.13 and R.sub.14 are independently selected from the group consisting of alkyl and aryl; andX.sub.1 and X.sub.2 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, and arylalkyl; and the acid addition salts thereof.

14. 发明授权

US5068251A Lipoxygenase inhibiting compounds 失效
标题翻译： LIPOXYGENASE抑制化合物
公开(公告)号：US5068251A
公开(公告)日：1991-11-26
申请号：US285439
申请日：1988-12-16
申请人： Dee W. Brooks , Karen E. Rodriques
发明人： Dee W. Brooks , Karen E. Rodriques
IPC分类号： C12N9/99 , A61K31/19 , A61K31/195 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/405 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/54 , A61K31/5415 , A61P3/00 , A61P11/08 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C275/64 , C07D207/08 , C07D209/28 , C07D209/40 , C07D209/46 , C07D209/88 , C07D231/04 , C07D263/32 , C07D263/56 , C07D277/20 , C07D277/30 , C07D279/20 , C07D279/22 , C07D333/24 , C07D491/052
CPC分类号： C07C275/64 , C07D209/40
摘要： Compounds of the formula: ##STR1## wherein A is CH.sub.2 ; n is 0 or 1; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, aralkyl and cycloalkyl; Z is the residue from a non-steroidal anti-inflammatory carboxylic acid compound; and M is a pharmaceutically acceptable cation or a metabolically cleavable group; and the pharmaceutically acceptable salts thereof; and a non toxic pharmaceutically acceptable carrier.These compounds are useful as inhibitors of 5-lipoxygenase.

15. 发明授权

US5512581A Iminoxycarboxylates and derivatives as inhibitors of leukotriene biosynthesis 失效
标题翻译：亚氨基羧酸盐和衍生物作为白细胞三烯生物合成的抑制剂
公开(公告)号：US5512581A
公开(公告)日：1996-04-30
申请号：US432491
申请日：1995-05-01
申请人： Dee W. Brooks , Pramila Bhatia , Teodozyi Kolasa
发明人： Dee W. Brooks , Pramila Bhatia , Teodozyi Kolasa
IPC分类号： A61K31/426 , A61K31/428 , A61K31/437 , A61K31/4406 , A61K31/4409 , A61K31/4433 , A61K31/4439 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/498 , A61K31/505 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P19/06 , A61P27/14 , A61P43/00 , C07D213/30 , C07D215/14 , C07D215/22 , C07D215/227 , C07D215/36 , C07D235/12 , C07D239/26 , C07D241/42 , C07D263/56 , C07D277/24 , C07D277/64 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D513/04 , C07D215/12
CPC分类号： C07D213/30 , C07D215/14 , C07D215/227 , C07D215/36 , C07D235/12 , C07D239/26 , C07D241/42 , C07D263/56 , C07D277/24 , C07D277/64 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D513/04
摘要： The present invention relates to a compound of formulaW--X--Q--Y--CH(R.sup.1)--O--N.dbd.C(R.sup.2)--A--COMor a pharmaceutically acceptable salt thereof wherein W is optionally substituted aryl or heteroaryl; X is a valence bond, or methylene, divalent alkylene, alkenylene, alkynylene or alkyloxy; Q is a valence bond, or --O--, --S--, >NR.sup.4 or >NCOR.sup.5 ; Y is optionally substituted phenyl, biphenyl, naphthyl, tetrahydronaphthyl, indolyl, pyridyl, or benzo b!thienyl, thienyl, thiazolyl, or thiazolylphenyl; R.sup.1 is alkyl, cycloalkyl, alkoxyalkyl, aryl or arylalkyl, heteroaryl or heteroarylalkyl; R.sup.2 is hydrogen, alkyl or hydroxyalkyl; A is a valence bond or is selected from alkylene, alkenylene, alkynylene, cycloalkylene, phenylene, pyridylene, thienylene and furylene; and M is a pharmaceutically acceptable, metabolically cleavable group, --OR.sup.6, --NR.sup.6 R.sup.7, --NH-tetrazoyl, --NH-2-, 3-, or 4-pyridyl, and --NH-2-, 4-, or 5-thiazolyl which inhibit leukotriene biosynthesis and are useful in the treatment of inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method for inhibiting lipoxygenase activity and leukotriene biosynthesis.
摘要翻译：本发明涉及式W-X-Q-Y-CH（R 1）-O-N = C（R 2）-A-COM的化合物或其药学上可接受的盐，其中W为任选取代的芳基或杂芳基; X是价键，或亚甲基，二价亚烷基，亚烯基，亚炔基或烷氧基; Q是价键，或-O-，-S-，> NR4或> NCOR5; Y是任选取代的苯基，联苯基，萘基，四氢萘基，吲哚基，吡啶基或苯并[b]噻吩基，噻吩基，噻唑基或噻唑基苯基; R 1是烷基，环烷基，烷氧基烷基，芳基或芳基烷基，杂芳基或杂芳基烷基; R2是氢，烷基或羟烷基; A是价键或选自亚烷基，亚烯基，亚炔基，亚环烷基，亚苯基，亚吡啶基，亚噻吩基和亚芳基; 并且M是药学上可接受的代谢可裂解基团-OR 6，-NR 6 R 7，-NH-四唑基，-NH-2-，3-或4-吡啶基和-NH-2-，4-或5-噻唑基其抑制白细胞三烯生物合成并且可用于治疗炎性疾病状态。还公开了白三烯生物合成抑制组合物和抑制脂氧合酶活性和白三烯生物合成的方法。

16. 发明授权

US5459150A Indole derivatives which inhibit leukotriene biosynthesis 失效
标题翻译：抑制白细胞三烯生物合成的吲哚衍生物
公开(公告)号：US5459150A
公开(公告)日：1995-10-17
申请号：US969294
申请日：1993-02-16
申请人： Dee W. Brooks , George W. Carter , Joseph F. Dellaria , Robert G. Maki , Karen E. Rodriques
发明人： Dee W. Brooks , George W. Carter , Joseph F. Dellaria , Robert G. Maki , Karen E. Rodriques
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/505 , A61P29/00 , A61P37/08 , A61P43/00 , C07D209/22 , C07D209/30 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/12 , A61K31/475
CPC分类号： C07D401/12 , C07D209/30 , C07D409/06
摘要： Substituted indolyl compounds of the formula ##STR1## are potent inhibitors of the lipoxygenase enzymes and are useful as agents for the treatment of allergies and inflammatory disease states.
摘要翻译： PCT No.PCT / US91 / 05621 Sec。 371日期：1993年2月16日 102（e）日期1993年2月16日PCT 1991年8月7日PCT PCT。公开号WO92 / 03132 日期：1992年3月5日。异丙烯酰胺酶的取代吲哚基化合物，可用作治疗过敏和炎性疾病状态的药剂。

17. 发明授权

US5095031A Indole derivatives which inhibit leukotriene biosynthesis 失效
标题翻译：含有低分子量生物化学的衍生物
公开(公告)号：US5095031A
公开(公告)日：1992-03-10
申请号：US570248
申请日：1990-08-20
申请人： Dee W. Brooks , George W. Carter , Joseph F. Dellaria , Robert G. Maki , Karen E. Rodriques
发明人： Dee W. Brooks , George W. Carter , Joseph F. Dellaria , Robert G. Maki , Karen E. Rodriques
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/505 , A61P29/00 , A61P37/08 , A61P43/00 , C07D209/22 , C07D209/30 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/12
CPC分类号： C07D401/12 , C07D209/30 , C07D409/06
摘要： Substituted indolyl compounds of the formula ##STR1## are potent inhibitors of the lipoxygenase enzymes and are useful as agents for the treatment of allergies and inflammatory disease states.
摘要翻译：式“IMAGE”的取代吲哚基化合物是脂氧合酶的有效抑制剂，可用作治疗过敏和炎性疾病状态的药剂。

18. 发明授权

US5037853A Cyclopropyl derivative lipoxygenase inhibitors 失效
标题翻译：环丙基衍生物脂氧合酶抑制剂
公开(公告)号：US5037853A
公开(公告)日：1991-08-06
申请号：US458067
申请日：1989-12-28
申请人： Dee W. Brooks , Karen E. Rodriques
发明人： Dee W. Brooks , Karen E. Rodriques
IPC分类号： C07C259/06 , C07C259/08 , C07C275/64 , C07D207/32 , C07D207/335 , C07D209/14 , C07D213/30 , C07D213/40 , C07D213/61 , C07D213/64 , C07D213/643 , C07D213/65 , C07D213/68 , C07D277/28 , C07D277/34 , C07D277/64 , C07D307/52 , C07D307/56 , C07D307/81 , C07D317/58 , C07D319/18 , C07D333/16 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/56 , C07D333/58 , C07D405/04 , C07D409/04
CPC分类号： C07D207/335 , C07C259/06 , C07C259/08 , C07C275/64 , C07D209/14 , C07D213/30 , C07D213/40 , C07D213/61 , C07D213/643 , C07D213/65 , C07D213/68 , C07D277/28 , C07D277/34 , C07D277/64 , C07D307/52 , C07D307/56 , C07D307/81 , C07D317/58 , C07D319/18 , C07D333/16 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/56 , C07D333/58 , C07D405/04 , C07D409/04 , C07C2101/02
摘要： Certain carbocyclic aryl- and heterocyclic aryl-substituted cyclopropyl N-hydroxyureas, N-hydoroxycarboxamides, and N-acyl-N-hydroxyamides inhibit 5- and/or 12-lipoxygenase and are useful in the treatment of inflammatory disease states.
摘要翻译：某些碳环芳基和杂环芳基取代的环丙基N-羟基脲，N-羟基甲酰胺和N-酰基-N-羟基酰胺抑制5-和/或12-脂氧合酶，并且可用于治疗炎性疾病状态。

19. 发明授权

US5026729A Lipoxygenase inhibiting compounds 失效
标题翻译：脂氧合酶抑制化合物
公开(公告)号：US5026729A
公开(公告)日：1991-06-25
申请号：US430841
申请日：1989-11-02
申请人： Dee W. Brooks , James B. Summers , James H. Holms
发明人： Dee W. Brooks , James B. Summers , James H. Holms
IPC分类号： C07C275/64
CPC分类号： C07C275/64
摘要： Compounds having 5- and 12-lipoxygenase inhibitory activity have the structure ##STR1## where A is straight or branched divalent alkylene of from one to four carbon atoms, R.sub.1 is methyl, amino, or alkylamino of from one to six carbon atoms and the substituent group R.sub.2 is C.sub.1 -C.sub.2 alkyl.The group R.sub.3 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, halogen, cyano, and trihalomethyl, and R.sub.4 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, hydroxy, halogen, cyano, and trihalomethyl, with the proviso that when R.sub.1 is amino and A is >CHCH.sub.3, R.sub.3 and R.sub.4 may not both be hydrogen.The group designated M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group. Pharmaceutical compositions and a method of inhibiting 5- and 12-lipoxygenase activity are also disclosed.
摘要翻译：具有5-和12-脂氧合酶抑制活性的化合物具有结构，其中A是1-4个碳原子的直链或支链二价亚烷基，R1是甲基，氨基或1-6个碳原子的烷基氨基，基团R2是C1-C2烷基。基团R3是一个或多个选自氢，一至六个碳原子的烷基，一个至六个碳原子的烷氧基，一个至六个碳原子的硫代烷氧基，卤素，氰基和三卤甲基的取代基，R4是一个或更多取代基选自氢，一至六个碳原子的烷基，一至六个碳原子的烷氧基，一至六个碳原子的硫代烷氧基，羟基，卤素，氰基和三卤代甲基，条件是当R1为氨基和A是> CHCH 3，R 3和R 4可以不都是氢。指定为M的基团是氢，可药用阳离子或代谢可裂解基团。还公开了药物组合物和抑制5-和12-脂肪氧合酶活性的方法。

20. 发明授权

US4873259A Indole, benzofuran, benzothiophene containing lipoxygenase inhibiting compounds 失效
标题翻译：吲哚，苯并呋喃，苯并噻吩含脂氧合酶抑制化合物
公开(公告)号：US4873259A
公开(公告)日：1989-10-10
申请号：US138073
申请日：1988-01-11
申请人： James B. Summers, Jr. , Bruce P. Gunn , Dee W. Brooks
发明人： James B. Summers, Jr. , Bruce P. Gunn , Dee W. Brooks
IPC分类号： C07D209/14 , C07D307/81 , C07D333/58
CPC分类号： C07D333/58 , C07D209/14 , C07D307/81
摘要： Compounds of the formula: ##STR1## wherein R.sub.1 is (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl, (3) C.sub.2 to C.sub.4 alkenyl, or (4) NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 are independently selected from (1) hydrogen, (2) C.sub.1 to C.sub.4 alkyl and (3) hydroxyl, but R.sub.2 and R.sub.3 are not simultaneously hydroxyl;wherein X is oxygen, sulfur, SO.sub.2, or NR.sub.4, wherein R.sub.4 is (1) hydrogen, (2) C.sub.1 to C.sub.6 alkyl, (3) C.sub.1 to C.sub.6 alkoyl, (4) aroyl, or (5) alkylsulfonyl;A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene;n is 1-5;Y is selected independently at each occurrence from (1) hydrogen, (2) halogen, (3) hydroxy, (4) cyano, (5) halosubstituted alkyl, (6) C.sub.1 to C.sub.12 alkyl, (7) C.sub.2 to C.sub.12 alkenyl, (8) C.sub.1 to C.sub.12 alkoxy, (9) C.sub.3 to C.sub.8 cycloalkyl, (10) C.sub.1 -C.sub.8 thioalkyl, (11) aryl, (12) aryloxy, (13) aroyl, (14) C.sub.1 to C.sub.12 arylalkyl, (15) C.sub.2 to C.sub.12 arylalkenyl, (16) C.sub.1 to C.sub.12 arylalkoxy, (17) C.sub.1 to C.sub.12 arylthioalkoxy, and substituted derivatives of (18) aryl, (19) aryloxy, (20) aroyl, (21) C.sub.1 to C.sub.12 arylalkyl, (22) C.sub.2 to C.sub.12 arylalkenyl, (23) C.sub.1 to C.sub.12 arylalkoxy, or (24) C.sub.1 to C.sub.12 arylthioalkoxy, wherein substituents are selected from halo, nitro, cyano, C.sub.1 to C.sub.12 alkyl, alkoxy, and halosubstituted alkyl;Z is oxygen or sulfur;and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C.sub.1 to C.sub.12 alkoyl, are potent inhibitors of 5- and/or 12-lipoxygenase enzymes.Also disclosed are lipoxygenase inhibiting compositions and a method for inhibiting lipoxygenase activity.
摘要翻译：其中R 1是（1）氢，（2）C 1至C 4烷基，（3）C 2至C 4链烯基或（4）NR 2 R 3，其中R 2和R 3独立地选自（1）氢，（2）C1至C4烷基和（3）羟基，但R2和R3不同时为羟基; 其中X是氧，硫，SO 2或NR 4，其中R 4是（1）氢，（2）C 1至C 6烷基，（3）C 1至C 6烷酰基，（4）芳酰基或（5）烷基磺酰基; A选自C1至C6亚烷基和C2至C6亚烯基; n为1-5; 在（1）氢，（2）卤素，（3）羟基，（4）氰基，（5）卤代烷基，（6）C1至C12烷基，（7）C2至C12烯基，（8）C1至C12烷氧基，（9）C3至C8环烷基，（10）C1-C8硫代烷基，（11）芳基，（12）芳氧基，（13）芳酰基，（14）C1至C12芳烷基，（15）（18）芳基，（19）芳氧基，（20）芳酰基，（21）C1〜C12芳基烷基，（22）C1〜C12芳基烷氧基，（17）C1〜C12芳基烷氧基，（17））C 2至C 12芳基烯基，（23）C 1至C 12芳基烷氧基或（24）C 1至C 12芳硫基烷氧基，其中取代基选自卤素，硝基，氰基，C 1至C 12烷基，烷氧基和卤代烷基; Z是氧或硫; 和M是氢，可药用阳离子，芳酰基或C 1至C 12烷酰基，是5-和/或12-脂氧合酶的有效抑制剂。还公开了脂氧合酶抑制组合物和抑制脂氧合酶活性的方法。

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