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1. 发明授权

US5326787A Cycloalkyl N-hydroxy derivatives having lipoxygenase inhibitory activity 失效
标题翻译：具有脂氧合酶抑制活性的环烷基N-羟基衍生物
公开(公告)号：US5326787A
公开(公告)日：1994-07-05
申请号：US111764
申请日：1993-08-25
申请人： Dee W. Brooks , Jimmie L. Moore , Karen E. Rodriques
发明人： Dee W. Brooks , Jimmie L. Moore , Karen E. Rodriques
IPC分类号： C07C275/64 , A01N55/02
CPC分类号： C07C275/64
摘要： Compounds of the structure ##STR1## where M is hydrogen, a pharmaceutically acceptable cation or metabolically cleavable group, R is alkyl, cycloalkyl, or NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl alkonyl, or carbocyclic aryl, Y is alkylene, alkenylene, or cyclopropyl, and A is optionally substituted cycloalkyl or cycloalkylene 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：结构的化合物，其中M是氢，药学上可接受的阳离子或代谢可裂解基团，R是烷基，环烷基或NR 1 R 2，其中R 1和R 2是氢，烷基，环烷基烷基或碳环芳基，Y是亚烷基，亚烯基或环丙基，A是任选取代的环烷基或环亚烷基是脂氧合酶的有效抑制剂，因此抑制白三烯的生物合成。这些化合物可用于治疗或改善过敏性和炎性疾病状态。

2. 发明授权

US4992464A Heteroaryl N-hydroxy amides and ureas with polar substituents as 5-lipoxygenase inhibitors 失效
公开(公告)号：US4992464A
公开(公告)日：1991-02-12
申请号：US430710
申请日：1989-11-01
申请人： Dee W. Brooks , James B. Summers , Karen E. Rodriques , Robert G. Maki , Joseph F. Dellaria , James H. Holms , Jimmie L. Moore
发明人： Dee W. Brooks , James B. Summers , Karen E. Rodriques , Robert G. Maki , Joseph F. Dellaria , James H. Holms , Jimmie L. Moore
IPC分类号： C07D209/14 , C07D307/81 , C07D333/58 , A61K31/38 , C07D333/56
CPC分类号： C07D333/58 , C07D209/14 , C07D307/81
摘要： Compounds, compositions a method of inhibiting lipoxygenase and treating related disorders are disclosed. The compounds are of the formula:Ar-A(R.sub.2).sub.n -N(OM)-CZ-R.sub.1whereinAr is ##STR1## where X is O, S, SO.sub.2 or NR.sub.3 ;R.sub.3 is hydrogen, alkyl, alkylaryl, alkoyl, alkylakoyl, aroyl or alkylaroyl;Y is hydrogen, halogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, arylalkenyl, --OR, --SR, --COOR, --COR, --CON(R).sub.2, --OCOR, --N(R).sub.2, --O(CH).sub.2, --SO.sub.2 R, --SO.sub.2 N(R).sub.2, --O(CH.sub.2).sub.p OR, --CN, --NO.sub.2, --O(CH).sub.p O(CH.sub.2).sub.p OR or --CF.sub.3 ;R is hydrogen, hydroxyl, alkyl, alkylaryl or aryl;m is 0 to 5;p is 1 to 4;A is C.sub.1 -C.sub.12 alkylene or C.sub.2 -C.sub.14 alkenylene;R.sub.2 is --OR, --SR, --COOR, --COR, --CON(R).sub.2, --OCOR, --N(R).sub.2, --O(CH.sub.2).sub.y CON(R).sub.2, --O(CH.sub.2).sup.y OR, --CN, --NO.sub.2, 1-tetrazolo, C.sub.4 -C.sub.8 cyclic amido, imidazolo, --O(CH.sub.2).sub.y O(CH.sub.2).sub.y OR, --CF.sub.3, --N(R) COCHR--NH(R), CONHCH(R)CO.sub.2 R, --OCOCHR-NH(R), --CR(NHR)CONR, --CR(NHR)COR, morpholino, --NH(CH.sub.2).sub.y OH, --N[(CH.sub.2).sub.y OH].sub.2, --N.sub.3, --SO.sub.2 N(R).sub.2, --N(R)COR, --N(R)COOR, --N(R)CON(R).sub.2, --C(.dbd.NOH)NHOH or --C(.dbd.NOH)NH.sub.2 where R is as defined above, y is 1 to 4 and --N(R).sub.2 can form a heterocyclic ring of 5-8 atoms;M is hydrogen, a pharmaceutically acceptable cation or a metabolically cleavable group;Z is oxygen or sulfur; andR.sub.1 us hydrogen, alkyl, alkenyl, --NR.sub.4 R.sub.5, --NCOR.sub.6 or --Q--(R.sub.2).sub.2 where R.sub.4 and R.sub.5 independently selected from the group consisting of hydrogen, hydroxyl, alkyl, substituted alkyl with 1-3 substituents selected from the group consisting of R.sub.2 as defined above, acyl, aryl and CON(R).sub.2 is as defined above, R.sub.6 is hydrogen alkyl, alkylaryl, aryl or NR.sub.4 R.sub.5 where R.sub.4 and R.sub.5 are as defined above and where NR.sub.4 R.sub.5 can form a heterocyclic ring of a 5-8 atoms, Q is alkyl, alkenyl or aryl and z is 0 to 3; provided when n is O, R.sub.1 is not hydrogen, alkyl, alkenyl, or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are as defined above; and the pharmaceutically acceptable salts thereof.

3. 发明授权

US5288743A Indole carboxylate 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羧酸衍生物
公开(公告)号：US5288743A
公开(公告)日：1994-02-22
申请号：US979138
申请日：1992-11-20
申请人： Dee W. Brooks , Keith W. Woods , Karen E. Rodriques
发明人： Dee W. Brooks , Keith W. Woods , Karen E. Rodriques
IPC分类号： C07D209/30 , C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12 , A61K31/405 , C07D277/04
CPC分类号： C07D401/12 , C07D209/30 , C07D403/12 , C07D409/12 , C07D417/12
摘要： Compounds of the structure ##STR1## where A is straight or branched divalent alkylene or divalent cycloalkylene, R.sub.1 is selected from hydrogen; alkylthio; optionally substituted phenylthio; optionally substituted phenylalkylthio; optionally substituted 2-, 3-, and 4-pyridyl; optionally substituted 2-, and 3-thienylthio; and optionally substituted 2-thiazolythio, R.sub.2 is selected from --COOB; --COOalkyl; --COOalkyl(carbocyclic aryl); --CONR.sub.5 R.sub.6 ; --COR.sub.6 ; and --OH, R.sub.3 is selected from phenylalkyl and heteroarylalkyl, and R.sub.4 is selected from optionally substituted alkoxy(carbocyclic aryl); optionally substituted carbocyclic aryloxy; optionally substituted heteroarylalkoxy; and optionally substituted heteroaryloxy are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
摘要翻译：其中A是直链或支链二价亚烷基或二价亚环烷基的结构化合物，其中A选自氢; 烷硫基任选取代的苯硫基; 任选取代的苯基烷硫基; 任选取代的2-，3-和4-吡啶基; 任选取代的2-和3-噻吩基硫基; 和任选取代的2-噻唑硫基，R2选自-COOB; -COO烷基; -COO烷基（碳环芳基）; -CONR5R6; -COR6; 和-OH，R 3选自苯基烷基和杂芳基烷基，并且R 4选自任选取代的烷氧基（碳环芳基）; 任选取代的碳环芳氧基; 任选取代的杂芳基烷氧基; 和任选取代的杂芳氧基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

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.

5. 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。

6. 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。

7. 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。

8. 发明授权

US5187192A Cyclobutyl derivatives having lipoxygenase inhibitory activity 失效
标题翻译：具有脂氧合酶抑制活性的环丁基衍生物
公开(公告)号：US5187192A
公开(公告)日：1993-02-16
申请号：US850719
申请日：1992-03-13
申请人： Dee W. Brooks , Karen E. Rodriques
发明人： Dee W. Brooks , Karen E. Rodriques
IPC分类号： C07C259/06 , C07C259/10 , C07C275/64 , C07D213/42 , C07D213/64 , C07D213/643 , C07D213/68 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/58
CPC分类号： C07D213/42 , C07C259/06 , C07C259/10 , C07C275/64 , C07D213/643 , C07D213/68 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/58 , C07C2101/14
摘要： Compounds of the structure ##STR1## where M is a pharmaceutically acceptable cation or a metabolically cleavable group, R is alkyl, cycloalkyl or --NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted alkyl, cycloalkyl, carbocyclic aryl, benzo[b]furyl, thienyl, or benzo[b]thienyl 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：其中M是药学上可接受的阳离子或代谢可裂解基团的结构的化合物，R是烷基，环烷基或-NR 1 R 2，其中R 1和R 2是氢，烷基，环烷基或烷酰基，A是任选取代的烷基，环烷基，碳环芳基，苯并[b]呋喃基，噻吩基或苯并[b]噻吩基是脂氧合酶的有效抑制剂，从而抑制白三烯的生物合成。这些化合物可用于治疗或改善过敏性和炎性疾病状态。

9. 发明授权

US5175183A Lipoxygenase inhibiting compounds 失效
标题翻译：脂氧合酶抑制化合物
公开(公告)号：US5175183A
公开(公告)日：1992-12-29
申请号：US721530
申请日：1991-07-10
申请人： Dee W. Brooks , James B. Summers , Karen E. Rodriques
发明人： Dee W. Brooks , James B. Summers , Karen E. Rodriques
IPC分类号： C07C275/64 , C07D209/14 , C07D213/30 , C07D213/68 , C07D307/42 , C07D307/52 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/32 , C07D333/56 , C07D333/58 , C07D333/64 , C07D405/06 , C07D409/04 , C07D409/06
CPC分类号： C07D213/30 , C07C275/64 , C07D209/14 , C07D213/68 , C07D307/42 , C07D307/52 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/32 , C07D333/56 , C07D333/58 , C07D333/64 , C07D405/06 , C07D409/04 , C07D409/06 , C07C2101/02
摘要： Certain N-aryl, N-heteroaryl-, N-arylalkyl-, N-heteroarylalkyl-, N-arylcyclopropyl- and N-heteroaryl-cyclopropyl-N'-hydroxyurea compounds are inhibitors of lipoxygenase enzyme activity and are thus useful agents in treating disease states such as asthma, arthritis, allergy, psoriasis, inflammatory bowel disease, gout, adult respiratory distress syndrome, endotoxin shock, and other inflammatory conditions in which the products of the arachidonic acid cascade are implicated.
摘要翻译： PCT No.PCT / US90 / 00376 Sec。 371日期：1991年7月10日 102（e）日期1991年7月10日PCT 1990年1月25日PCT申请。N-芳基，N-杂芳基 - ，N-芳烷基 - ，N-杂芳基烷基 - ，N-芳基环丙基 - 和N-杂芳基 - 环丙基-N ' - 羟基脲化合物是脂氧合酶活性的抑制剂，因此是治疗疾病状态如哮喘，关节炎，过敏，牛皮癣，炎性肠病，痛风，成人呼吸窘迫综合征，内毒素休克和其它炎性病症的有用药物，其中涉及花生四烯酸级联的产物。

10. 发明授权

US5120752A Cyclopropyl derivative lipoxygenase inhibitors 失效
标题翻译：环丙基衍生物LIPOXYGENASE抑制剂
公开(公告)号：US5120752A
公开(公告)日：1992-06-09
申请号：US621104
申请日：1990-12-06
申请人： Dee W. Brooks , Karen E. Rodriques , Bruce W. Horrom , Hormoz Mazdiyasni
发明人： Dee W. Brooks , Karen E. Rodriques , Bruce W. Horrom , Hormoz Mazdiyasni
IPC分类号： A61K31/16 , A61K31/17 , A61K31/335 , A61K31/357 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4412 , A61K31/4418 , A61K31/443 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P29/00 , A61P43/00 , C07C239/08 , C07C259/06 , C07C259/08 , C07C275/64 , C07D207/32 , C07D207/335 , C07D209/14 , C07D213/30 , C07D213/40 , C07D213/42 , C07D213/61 , C07D213/64 , C07D213/643 , C07D213/65 , C07D213/68 , C07D215/12 , C07D239/26 , C07D277/28 , C07D277/34 , C07D277/64 , C07D295/20 , C07D307/52 , C07D307/56 , C07D307/58 , C07D307/81 , C07D307/83 , C07D317/58 , C07D319/18 , C07D333/16 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/56 , C07D333/58 , C07D333/64 , 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-hydroxy-carboxamides, and N-acyl-N-hydroxyamines inhibit 5- and/or 12-lipoxygenase and are useful in the treatment of inflammatory disease states.

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