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1. 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。

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

US5185363A Urea based lipoxygenase inhibiting compounds 失效
标题翻译：基于尿素的脂氧合酶抑制化合物
公开(公告)号：US5185363A
公开(公告)日：1993-02-09
申请号：US768621
申请日：1991-09-30
申请人： Dee W. Brooks , Daniel J. Kerkman , Jonathan G. Martin , Andrew O. Stewart , James B. Summers
发明人： Dee W. Brooks , Daniel J. Kerkman , Jonathan G. Martin , Andrew O. Stewart , James B. Summers
IPC分类号： C07C275/64 , C07C323/47 , C07D333/36 , C07D335/08 , C07D409/04 , C07D409/06 , C07D409/12
CPC分类号： C07D409/04 , C07C275/64 , C07C323/47 , C07D333/36 , C07D335/08 , C07D409/06 , C07D409/12
摘要： Substituted phenyl, naphthyl, and thienyl N-hydroxy urea compounds form a class of potent inhibitors of 5- and 12-lipoxygenase and are thus useful compounds in the treatment of inflammatory disease states where leukotrienes and other products of lipoxygenase enzyme activity are implicated.
摘要翻译： PCT No.PCT / US90 / 01488 Sec。 371日期1991年9月30日 102（e）1991年9月30日PCT 1991年3月20日PCT公布。 WO90 / 12008 PCT出版物 1990年10月18日。取代的苯基，萘基和噻吩基N-羟基脲化合物形成一类5-和12-脂肪氧合酶的有效抑制剂，因此是治疗炎性疾病状态的有用化合物，其中白细胞三烯和其它产物涉及脂氧合酶活性。

4. 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。

5. 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。

6. 发明授权

US5112848A Furan and pyrrole containing lipoxygenase inhibiting compounds 失效
标题翻译：呋喃和吡咯含有脂氧合酶抑制化合物
公开(公告)号：US5112848A
公开(公告)日：1992-05-12
申请号：US487982
申请日：1990-04-19
申请人： Dee W. Brooks , Bruce P. Gunn , James H. Holms , James B. Summers
发明人： Dee W. Brooks , Bruce P. Gunn , James H. Holms , James B. Summers
IPC分类号： A61K31/34 , A61K31/341 , A61K31/38 , A61K31/40 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P29/00 , A61P43/00 , C07D207/32 , C07D207/335 , C07D207/34 , C07D307/52 , C07D307/58 , C07D307/68 , C07D401/04 , C07D401/06 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D417/04
CPC分类号： C07D207/335 , C07D307/52 , C07D405/04 , C07D409/04 , C07D417/04
摘要： Substituted furan and pyrrole compounds which are useful in inhibiting lipoxygenase enzymes, particularly 5-lipoxygenase.
摘要翻译： PCT No.PCT / US88 / 04048 Sec。 371日期1990年04月19日 102（e）1990年04月19日PCT PCT。11月14日提交。用于抑制脂氧合酶，特别是5-脂氧合酶的取代的呋喃和吡咯化合物。

7. 发明授权

US5120751A Benzoylphenyl pyridinylthiazolidine compounds as platelet activating antagonists 失效
标题翻译：苯甲酰基苯基吡啶基噻唑烷化合物作为血小板激活拮抗剂
公开(公告)号：US5120751A
公开(公告)日：1992-06-09
申请号：US677687
申请日：1991-03-29
申请人： James B. Summers , Douglas H. Steinman , Denise E. Guinn , Steven K. Davidsen , Paul D. May
发明人： James B. Summers , Douglas H. Steinman , Denise E. Guinn , Steven K. Davidsen , Paul D. May
IPC分类号： C07D401/04 , C07D409/04 , C07D417/04
CPC分类号： C07D401/04 , C07D409/04 , C07D417/04
摘要： Benzoylphenyl derivatives of 2-(3-pyridinyl)-3-alkyl-4-thiazolidinecarboxamide, 2-(3-pyridinyl)-thiazolid-4-ylacetamide, 2-(3-pyridinyl)-4-dithiolanecarboxamide or 2-(3-pyridinyl)dithiolan-4-yl] urea are potent inhibitors of PAF and are useful in the treatment of PAF-related disorders including anaphylactic shock, respiratory distress syndrome, acute inflammation, delayed cellular immunity, parturtition, fetal lung maturation, and cellular differentiation.
摘要翻译： 2-（3-吡啶基）-4-二硫代甲烷甲酰胺或2-（3-吡啶基）-4-二硫代甲烷甲酰胺或2-（3-吡啶基）-4-二硫代甲烷甲酰胺的2-（3-吡啶基）-3-烷基-4-噻唑烷羧酰胺，吡啶基）二硫戊环-4-基]脲是PAF的有效抑制剂，可用于治疗PAF相关疾病，包括过敏性休克，呼吸窘迫综合征，急性炎症，延迟的细胞免疫，分娩，胎儿肺成熟和细胞分化。

8. 发明授权

US5567711A Indole-3-carbonyl and indole-3-sulfonyl derivatives as platelet activating factor antagonists 失效
标题翻译：吲哚-3-羰基和吲哚-3-磺酰基衍生物作为血小板激活因子拮抗剂
公开(公告)号：US5567711A
公开(公告)日：1996-10-22
申请号：US424911
申请日：1995-04-19
申请人： George S. Sheppard , Steven K. Davidsen , James B. Summers , George M. Carrera, Jr.
发明人： George S. Sheppard , Steven K. Davidsen , James B. Summers , George M. Carrera, Jr.
IPC分类号： C07D403/12 , A61K31/435 , A61P7/02 , C07D471/04 , A61K31/445
CPC分类号： C07D471/04
摘要： The present invention provides compounds of formula ##STR1## and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.
摘要翻译：本发明提供了作为PAF的有效拮抗剂的式“IMAGE”+ TR“IMA”的化合物及其药学上可接受的盐，可用于治疗PAF相关疾病，包括哮喘，休克，呼吸窘迫综合征，急性炎症，移植器官排斥，胃肠溃疡，过敏性皮肤病，延迟的细胞免疫，分娩，胎儿肺成熟和细胞分化。

9. 发明授权

US4822809A Benzazole lipoxygenase inhibiting compounds 失效
标题翻译：苯唑脂氧合酶抑制化合物
公开(公告)号：US4822809A
公开(公告)日：1989-04-18
申请号：US120251
申请日：1987-11-13
申请人： James B. Summers , Andrew O. Stewart
发明人： James B. Summers , Andrew O. Stewart
IPC分类号： C07D235/14 , C07D263/56 , C07D277/64 , A61K31/425
CPC分类号： C07D263/56 , C07D235/14 , C07D277/64
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;X is (1) oxygen, (2) sulfur, (3) SO.sub.2, or (4) 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 alkyl or (4) aroyl;A is selected from C.sub.1 to C.sub.6 alkylene and C.sub.2 to C.sub.6 alkenylene; n is 0-4;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) aryl, (11) aryloxy, (12) aroyl, (13) C.sub.1 to C.sub.12 arylalkyl, (14) C.sub.2 to C.sub.12 arylalkenyl, (15) C.sub.1 to C.sub.12 arylalkoxy, (16) C.sub.1 to C.sub.12 arylthioalkoxy, and substituted derivatives of (17) aryl, (18) aryloxy, (19) aroyl, (20) C.sub.1 to C.sub.12 arylalkyl, (21) C.sub.2 to C.sub.12 arylalkenyl, (22) C.sub.1 to C.sub.12 arylalkoxy, or (23) 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;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.
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; X是（1）氧，（2）硫，（3）SO2或（4）NR4，其中R4是（1）氢，（2）C1至C6烷基，（3）C1至C6烷基或（4）芳酰基 A选自C1至C6亚烷基和C2至C6亚烯基; n为0-4; 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）芳基，（11）芳氧基，（12）芳酰基，（13）C1至C12芳烷基，（14）C2至C12芳基烯基，（15）（17）芳基，（18）芳氧基，（19）芳酰基，（20）C1〜C12芳基烷基，（21）C2〜C12芳基烯基，（22）中碳原子数1〜12的芳基烷氧基，（16））C 1 -C 12芳基烷氧基或（23）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; 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的方法。

10. 发明授权

US5952320A Macrocyclic inhibitors of matrix metalloproteinases and TNF.alpha. secretion 失效
标题翻译：基质金属蛋白酶和TNFα分泌的大环抑制剂
公开(公告)号：US5952320A
公开(公告)日：1999-09-14
申请号：US992668
申请日：1997-12-17
申请人： Steven K. Davidsen , Douglas H. Steinman , George S. Sheppard , Lianhong Xu , James H. Holms , Yan Guo , James B. Summers , Alan S. Florjancic , Michael R. Michaelides
发明人： Steven K. Davidsen , Douglas H. Steinman , George S. Sheppard , Lianhong Xu , James H. Holms , Yan Guo , James B. Summers , Alan S. Florjancic , Michael R. Michaelides
IPC分类号： C07D245/06 , C07D267/00 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/12 , C07D487/08 , A61K31/33 , C07D225/04 , C07D267/22 , C07D281/18
CPC分类号： C07D413/04 , C07D245/06 , C07D267/00 , C07D413/06 , C07D413/12 , C07D417/12 , C07D487/08
摘要： Macrocyclic compounds of formula ##STR1## are potent inhibitors of matrix metalloproteinase and are useful in the treatment of diseases in which matrix metalloproteinase play a role. Also disclosed are matrix metalloproteinase inhibiting compositions and a method of inhibiting matrix metalloproteinase in a mammal.
摘要翻译：大环化合物是基质金属蛋白酶的有效抑制剂，可用于治疗基质金属蛋白酶发挥作用的疾病。还公开了抑制哺乳动物的基质金属蛋白酶抑制组合物和抑制基质金属蛋白酶的方法。

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