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1. 发明授权

US5446062A ((4-alkoxypyran-4-yl) substituted) ether, arylalkyl-, arylalkenyl-, and arylalkynyl)urea inhibitors of 5-lipoxygenase 失效
标题翻译：（（4-烷氧基吡喃-4-基）取代的）醚，芳基烷基 - ，芳基烯基 - 和芳基炔基）尿素抑制剂5-脂氧合酶
公开(公告)号：US5446062A
公开(公告)日：1995-08-29
申请号：US152569
申请日：1993-11-12
申请人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Chernesky , Wendy Lee
发明人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Chernesky , Wendy Lee
IPC分类号： C07D309/10 , C07D405/12 , A61K31/35 , C07D405/10
CPC分类号： C07D405/12 , C07D309/10
摘要： Compounds of the structure ##STR1## where W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.6 and R.sup.7 are hydrogen or alkyl, or R.sup.6 and R.sup.7, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## Z is --CH.sub.2 --, oxygen, sulfur, or --NR.sup.9, L.sup.1 and L.sup.2 are selected from a valence bond, alkylene, propenylene, and propynylene; R.sup.1 and R.sup.2 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl; Y is selected from oxygen, >NR.sup.10, and ##STR4## L.sup.3 is selected from alkylene of one to three carbon atoms, propenylene, propynylene, ##STR5## and R.sup.3, R.sup.4, and R.sup.5 are hydrogen or alkyl of one to four carbon atoms inhibit the synthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
摘要翻译：其中W选自的结构的化合物，其中Q是氧或硫，R6和R7是氢或烷基，或R6和R7与它们所连接的氮原子一起定义为式Z是-CH 2 - ，氧，硫或-NR 9，L 1和L 2选自价键，亚烷基，亚丙烯基和亚丙炔基; R 1和R 2独立地选自烷基，烷氧基，卤代烷基，卤素，氰基，氨基，烷氧基羰基和二烷基氨基羰基; Y选自氧，> NR10，并且 L3选自1至3个碳原子的亚烷基，亚丙烯基，亚丙炔基，R 3，R 4和R 5是氢或1-4个碳原子的烷基抑制白三烯的合成。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

US5432194A (4-alkoxypyran-4-yl) substituted arylalkylaryl-, aryalkenylaryl-, and aryalkynylarylurea inhibitors of 5-lipoxygenase 失效
标题翻译：（4-烷氧基吡喃-4-基）取代的芳基烷基芳基 - 芳烯基芳基和芳氧基炔基芳基脲抑制剂5-脂氧合酶
公开(公告)号：US5432194A
公开(公告)日：1995-07-11
申请号：US236001
申请日：1994-05-09
申请人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Chernesky , Wendy Lee
发明人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Chernesky , Wendy Lee
IPC分类号： C07D309/12 , C07D405/12 , A61K31/35 , C07D309/10
CPC分类号： C07D405/12 , C07D309/12
摘要： Compounds of the structure ##STR1## wherein W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.6 and R.sup.7 are hydrogen or alkyl, or R.sup.6 and R.sup.7, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## R.sup.8 is selected from hydrogen, alkyl, haloalkyl, optionally substituted phenyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, (alkoxycarbonyl)alkyl, and (alkylaminocarbonyl)alkyl; Z is --CH.sub.2 --, oxygen, sulfur, or --NR.sup.9 where R.sup.9 is hydrogen or alkyl, L.sup.1 and L.sup.2 are selected from a valence bond, alkylene, propenylene, and propynylene, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is selected from oxygen, --NR.sup.10, where R.sup.10 is hydrogen or alkyl, and ##STR4## where n=0, 1, or 2, and R.sup.5 is alkyl, 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W选自其中Q是氧或硫的结构的化合物，R6和R7是氢或烷基，或R6和R7与它们所连接的氮原子一起定义为烷基，卤代烷基，任选取代的苯基，羟基烷基，氨基烷基，羧基烷基，（烷氧基羰基）烷基和（烷基氨基羰基）烷基; Z是-CH 2 - ，氧，硫或-NR 9，其中R 9是氢或烷基，L 1和L 2选自价键，亚烷基，亚丙烯基和亚丙炔基，R 1，R 2，R 3和R 4独立地选自烷基卤素，卤素，氰基，氨基，烷氧基羰基和二烷基氨基羰基，Y选自氧，-NR10，其中R10是氢或烷基，和其中n = 0,1或2，R5是烷基，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。

3. 发明授权

US5516795A Heteroatom substituted propanyl derivatives having 5-lipoxygenase inhibitory activity 失效
标题翻译：具有5-脂氧合酶抑制活性的杂原子取代的丙烷基衍生物
公开(公告)号：US5516795A
公开(公告)日：1996-05-14
申请号：US304745
申请日：1994-09-12
申请人： Joseph F. Dellaria , Linda J. Chernesky
发明人： Joseph F. Dellaria , Linda J. Chernesky
IPC分类号： C07C323/44 , C07D317/28 , A61K31/335 , C07D317/26
CPC分类号： C07D317/28 , C07C323/44
摘要： Compounds of the structure ##STR1## where R.sup.1 is alkyl of one to four carbon atoms and R.sup.2 is selected from(a) alkenyl of one to four carbon atoms,(b) ##STR2## (c) ##STR3## and (d) ##STR4## 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R1是1-4个碳原子的烷基，R2选自（a）1-4个碳原子的链烯基，（b）（c）（c）和（d） 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

US5484786A Pyran-4-ylmethyl substituted arylalkylaryl-, arylalkenylylaryl-, and arylalkynylarylurea inhibitors of 5-lipoxygenase 失效
标题翻译：吡喃-4-基甲基取代的芳烷基芳基 - ，芳基烯基芳基 - 和芳基炔基芳基脲抑制剂5-脂氧合酶
公开(公告)号：US5484786A
公开(公告)日：1996-01-16
申请号：US111090
申请日：1993-08-24
申请人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Chernesky , Wendy Lee
发明人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Chernesky , Wendy Lee
IPC分类号： C07D309/04 , C07D309/06 , C07D405/12 , A61K31/35 , A61K31/495 , C07D239/04 , C07D315/00
CPC分类号： C07D405/12 , C07D309/04 , C07D309/06
摘要： Compounds of structure ##STR1## where W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.5 and R.sup.6 are independently selected from hydrogen and alkyl, or R.sup.5 and R.sup.6, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## L.sup.1 and L.sup.2 are independently selected from a valence bond, alkylene, propenylene, and propynylene, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is oxygen, >NR.sup.9 where R.sup.9 is hydrogen or alkyl, or ##STR4## where n=0, 1, or 2, and A is selected from ##STR5## 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W选自的结构的化合物，其中Q是氧或硫，R5和R6独立地选自氢和烷基，或R5和R6连同它们所连接的氮原子定义式为基团的基团，L1和L2独立地选自价键，亚烷基，亚丙烯基和亚丙炔基，R 1，R 2，R 3和R 4独立地选自烷基，烷氧基，卤代烷基，卤素，氰基，氨基，烷氧基羰基和二烷基氨基羰基，Y是氧，NR9，其中R9是氢或烷基，或者其中n = 0,1或2的A，并且A选自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

US5475009A 1, 2-dialkoxyethanes as 5-lipoxygenase inhibitors 失效
标题翻译： 1,2-二烷氧基乙烷作为5-脂氧合酶抑制剂
公开(公告)号：US5475009A
公开(公告)日：1995-12-12
申请号：US304066
申请日：1994-09-12
申请人： Linda J. Chernesky , Joseph F. Dellaria
发明人： Linda J. Chernesky , Joseph F. Dellaria
IPC分类号： C07C323/19 , C07C323/45 , C07D215/22 , C07D215/227 , C07D317/22 , C07D317/28 , C07D405/06 , A61K31/47 , C07D215/14
CPC分类号： C07D215/227 , C07C323/19 , C07C323/45 , C07D317/22 , C07D317/28 , C07D405/06
摘要： Compounds of the structure ##STR1## where Ar.sup.1 is selected from optionally substituted carbocyclic aryl; optionally substituted 5- or 6-membered heterocyclic aryl; optionally substituted 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms; optionally substituted benzo[b]furyl; optionally substituted benzo[b]thienyl; ##STR2## L.sup.1 is a valence bond, alkylene, propenylene, or propynylene; Y is oxygen, >NR.sup.5, or >S(O)n; Ar.sup.2 is optionally substituted phenyl; L.sup.2 is ##STR3## and R.sup.1 and R.sup.2 are alkyl, or taken together define a group of formula ##STR4## 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Ar1选自任选取代的碳环芳基的结构的化合物; 任选取代的5-或6-元杂环芳基; 任选取代的含有一个或两个氮原子的10元双环杂环芳基; 任选取代的苯并[b]呋喃基; 任选取代的苯并[b]噻吩基; L1是价键，亚烷基，亚丙烯基或亚丙炔基; Y是氧，> NR5或> S（O）n; Ar 2是任选取代的苯基; L2是，R 1和R 2是烷基，或者一起限定式为“IMAGE”的组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

US5407959A (Trans-1,4-dialkoxycyclohexyl) substituted arylalkylaryl-arylalkenylaryl-, and arylalkynylarylurea inhibitors of 5-lipoxygenase 失效
标题翻译：（反-1,4-二烷氧基环己基）取代芳基烷基芳基 - 芳基烯基芳基 - 和芳基炔基芳基脲抑制剂5-脂氧合酶
公开(公告)号：US5407959A
公开(公告)日：1995-04-18
申请号：US152115
申请日：1993-11-12
申请人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Chernesky , Wendy Lee
发明人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Chernesky , Wendy Lee
IPC分类号： C07C275/32 , C07C317/42 , C07C323/41 , C07C323/44 , C07C335/20 , C07D295/215 , A61K31/17 , C07C275/06 , C07C275/30
CPC分类号： C07D295/215 , C07C275/32 , C07C317/42 , C07C323/41 , C07C323/44 , C07C335/20 , C07C2101/14
摘要： Compounds of structure ##STR1## where W is selected from the group consisting of ##STR2## where Q is oxygen or sulfur, R.sup.7 and R.sup.8 are independently selected from hydrogen and alkyl, or R.sup.7 and R.sup.8, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## L.sup.1 and L.sup.2 are independently selected from a valence bond, alkylene, propenylene, and propynylene; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl; Y is oxygen, >NR.sup.11, where R.sup.11 is hydrogen or alkyl, or ##STR4## where n=0, 1, or 2; and R.sup.5 and R.sup.6 are alkyl, 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W选自其中Q是氧或硫，R7和R8独立地选自氢和烷基，或R7和R8与它们所在的氮原子一起 L1和L2独立地选自价键，亚烷基，亚丙烯基和亚丙炔基; R 1，R 2，R 3和R 4独立地选自烷基，烷氧基，卤代烷基，卤素，氰基，氨基，烷氧基羰基和二烷基氨基羰基。 Y是氧，NR 11，其中R 11是氢或烷基，或者其中n = 0,1或2; R5和R6是烷基，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。

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