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1. 发明授权

US06518279B2 Cyclopentanone dihydropyridine compounds useful as potassium channel openers 失效
标题翻译：可用作钾通道开放剂的环戊酮二氢吡啶化合物
公开(公告)号：US06518279B2
公开(公告)日：2003-02-11
申请号：US09262441
申请日：1999-03-04
申请人： William A. Carroll , Yiyuan Chen , Irene Drizin , James F. Kerwin , Jimmie L. Moore
发明人： William A. Carroll , Yiyuan Chen , Irene Drizin , James F. Kerwin , Jimmie L. Moore
IPC分类号： A61K314353
CPC分类号： C07D221/04 , C07C45/298 , C07D221/06 , C07C47/55
摘要： Compounds of formula I are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.
摘要翻译：式I化合物可用于治疗用钾通道开放剂预防或改善的疾病。还公开了钾通道开放组合物和在哺乳动物中开放钾通道的方法。

2. 发明授权

US5350765A Ether-containing inhibitors of 5-lipoxygenase 失效
标题翻译：含醚的5-脂氧合酶抑制剂
公开(公告)号：US5350765A
公开(公告)日：1994-09-27
申请号：US113942
申请日：1993-08-30
申请人： Joseph F. Dellaria , Jimmie L. Moore , Dee W. Brooks
发明人： Joseph F. Dellaria , Jimmie L. Moore , Dee W. Brooks
IPC分类号： C07D309/10 , C07D405/12 , A61K31/35 , C07D309/02
CPC分类号： C07D405/12 , C07D309/10
摘要： Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, or benzo[b]thienyl, A.sub.1 is propynyl, methylene, or a direct link to X, X is oxy, thio, sulfonyl, or NR.sub.4, A.sub.2 is selected from ##STR2## where Y is hydrogen, halogen, or nitrile; Z is hydrogen, R.sub.1 is alkyl, and R.sub.2 is hydrogen or alkyl 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Ar是任选取代的碳环芳基，5-或6-元杂环芳基，含有一个或两个氮原子的10元双环杂环芳基，含有一个或两个氮原子的9元或10元杂环的结构化合物并且任选地含有另外的氮或氧原子和一个氧代或硫代取代基，苯并[b]呋喃基或苯并[b]噻吩基，A1是丙炔基，亚甲基或与X的直接连接，X是氧基，硫代，磺酰基，或NR4，A2选自，其中Y是氢，卤素或腈; Z是氢，R1是烷基，R2是氢或烷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。

3. 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.

4. 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。

5. 发明授权

US5268379A Ether-containing inhibitors of 5-lipoxygenase 失效
标题翻译：含醚的5-脂氧合酶抑制剂
公开(公告)号：US5268379A
公开(公告)日：1993-12-07
申请号：US935079
申请日：1992-08-24
申请人： Joseph F. Dellaria , Jimmie L. Moore , Dee W. Brooks
发明人： Joseph F. Dellaria , Jimmie L. Moore , Dee W. Brooks
IPC分类号： C07D309/10 , C07D405/12 , A61K31/47
CPC分类号： C07D405/12 , C07D309/10
摘要： Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, or benzo[b]thienyl, A.sub.1 is propynyl, methylene, or a direct link to X, X is oxy, thio, sulfonyl, or NR.sub.4, A.sub.2 is selected from ##STR2## where Y is hydrogen, halogen, or nitrile; Z is hydrogen, R.sub.1 is alkyl, and R.sub.2 is hydrogen or alkyl 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Ar是任选取代的碳环芳基，5-或6-元杂环芳基，含有一个或两个氮原子的10元双环杂环芳基，含有一个或两个氮原子的9元或10元杂环的结构化合物并且任选地含有另外的氮或氧原子和一个氧代或硫代取代基，苯并[b]呋喃基或苯并[b]噻吩基，A1是丙炔基，亚甲基或与X的直接连接，X是氧基，硫代，磺酰基，或NR4，A2选自，其中Y是氢，卤素或腈; Z是氢，R1是烷基，R2是氢或烷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。

6. 发明授权

US06506766B1 Glucocortiocoid-selective antinflammatory agents 失效
标题翻译：糖皮质激素选择性抗炎药
公开(公告)号：US06506766B1
公开(公告)日：2003-01-14
申请号：US09610638
申请日：2000-07-05
申请人： Michael J. Coghlan , James P. Edwards , Steven W. Elmore , Todd K. Jones , Michael E. Kort , Philip R. Kym , Jimmie L. Moore , John K. Pratt , Alan X. Wang
发明人： Michael J. Coghlan , James P. Edwards , Steven W. Elmore , Todd K. Jones , Michael E. Kort , Philip R. Kym , Jimmie L. Moore , John K. Pratt , Alan X. Wang
IPC分类号： A61K314741
CPC分类号： C07D491/04
摘要： Compounds having Formula I are useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor and treating immune, autoimmune and inflammatory diseases in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of inhibiting immune or autoimmune diseases in a mammal.
摘要翻译：具有式I的化合物可用于部分或完全拮抗，抑制，激动或调节糖皮质激素受体并在哺乳动物中治疗免疫，自身免疫和炎性疾病。还公开了包含式I化合物的药物组合物和在哺乳动物中抑制免疫或自身免疫性疾病的方法。

7. 发明授权

US4336260A Method and compositions using 1-aryl-1,2,3,4-tetrahydro-.beta.-carboline-3-carboxylic acid for treating depression 失效
标题翻译：使用1-芳基-1,2,3,4-四氢-β-咔啉-3-羧酸治疗抑郁症的方法和组合物
公开(公告)号：US4336260A
公开(公告)日：1982-06-22
申请号：US16757
申请日：1979-03-02
申请人： Alan J. Payne , Michael V. Aylott , Jimmie L. Moore , Edward M. Yokley
发明人： Alan J. Payne , Michael V. Aylott , Jimmie L. Moore , Edward M. Yokley
IPC分类号： C07D471/04 , A61K31/44 , A61K31/435 , A61K31/455
CPC分类号： C07D471/04
摘要： Treatment of central nervous system depression in a mammal using method and compositions employing 1-aryl-1,2,3,4-tetrahydro-.beta.-carboline-3-carboxylic acids, esters and pharmaceutically-acceptable salts.
摘要翻译：使用1-芳基-1,2,3,4-四氢-β-咔啉-3-羧酸，酯和药学上可接受的盐的方法和组合物治疗哺乳动物的中枢神经系统抑制。

8. 发明授权

US06951942B2 Glucocorticoid-selective anti-inflammatory agents 有权
标题翻译：糖皮质激素选择性抗炎药
公开(公告)号：US06951942B2
公开(公告)日：2005-10-04
申请号：US10201524
申请日：2002-07-23
申请人： Michael J. Coghlan , James P. Edwards , Steven W. Elmore , Todd K. Jones , Michael E. Kort , Philip R. Kym , Jimmie L. Moore , John K. Pratt , Alan X. Wang
发明人： Michael J. Coghlan , James P. Edwards , Steven W. Elmore , Todd K. Jones , Michael E. Kort , Philip R. Kym , Jimmie L. Moore , John K. Pratt , Alan X. Wang
IPC分类号： C07D491/052 , A61K31/4741 , A61K31/519 , A61K31/5377 , A61P29/00 , A61P37/00 , A61P43/00 , C07D491/04 , C07D491/02 , C07D491/06
CPC分类号： C07D491/04
摘要： Compounds having Formula I are useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor and treating immune, autoimmune and inflammatory diseases in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula I and methods of inhibiting immune or autoimmune diseases in a mammal.
摘要翻译：具有式I的化合物可用于部分或完全拮抗，镇压，激动或调节糖皮质激素受体并治疗哺乳动物的免疫，自身免疫和炎性疾病。还公开了包含式I化合物的药物组合物和在哺乳动物中抑制免疫或自身免疫性疾病的方法。

9. 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。

10. 发明授权

US4108853A N,15-Didehydro-15-deoxo-pyrimidino-(4,5-b)rifamycin S 失效
标题翻译： N，15-二氢-15-脱氧嘧啶并（4,5-b）利福霉素S
公开(公告)号：US4108853A
公开(公告)日：1978-08-22
申请号：US802214
申请日：1977-05-31
申请人： James R. McCarthy , Jimmie L. Moore
发明人： James R. McCarthy , Jimmie L. Moore
IPC分类号： C07D498/18 , C07D241/36 , A61K31/505
CPC分类号： C07D498/18
摘要： The subject compound is prepared by an activated manganese dioxide oxidation of N,15-didehydro-15-deoxo-3,15-epi(methano(imino)rifamycin SV. The new compound has antimicrobial utility.
摘要翻译：本发明化合物通过活化二氧化锰氧化N，15-二脱氢-15-脱氧-3,15-表（亚硝基）利福霉素SV制备。新化合物具有抗菌效用。

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