专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

51. 发明授权

US5446055A Polyether naphthalenic lignan lactones as inhibitors of 5-lipoxygenase 失效
标题翻译：聚醚萘木酚素内酯作为5-脂氧合酶的抑制剂
公开(公告)号：US5446055A
公开(公告)日：1995-08-29
申请号：US344443
申请日：1994-11-23
申请人： Joseph F. Dellaria , James D. Ratajczyk , Clint D. W. Brooks , Anwer Basha
发明人： Joseph F. Dellaria , James D. Ratajczyk , Clint D. W. Brooks , Anwer Basha
IPC分类号： C07D307/92 , C07D405/04 , C07D405/14 , C07D407/12 , C07D409/04 , C07D409/14 , A61K31/44
CPC分类号： C07D307/92 , C07D405/04 , C07D405/14 , C07D407/12 , C07D409/04 , C07D409/14
摘要： Compounds of formula ##STR1## Ar is optionally substituted phenyl, furyl, pyridyl, or thienyl; Y is selected from hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, and alkoxycarbonyl; L is selected from ##STR2## and R.sup.1 and R.sup.2 are alkyl or together define a group of formula ##STR3## 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：式的化合物Ar是任选取代的苯基，呋喃基，吡啶基或噻吩基; Y选自氢，卤素，氰基，烷基，卤代烷基，烷氧基和烷氧基羰基; L选自，R 1和R 2是烷基或一起界定一组式（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。

52. 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。

53. 发明授权

US5346914A (4-alkoxypyran-4-yl) substituted arylalkylaryl-, arylalkenylaryl-, and arylalkynylarylurea inhibitors of 5-lipoxygenase 失效
标题翻译：（4-烷氧基吡喃-4-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：US5346914A
公开(公告)日：1994-09-13
申请号：US61988
申请日：1993-05-14
申请人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Dorn , Wendy Lee
发明人： Joseph F. Dellaria , Anwer Basha , Lawrence A. Black , Linda J. Dorn , Wendy Lee
IPC分类号： C07D309/12 , C07D405/12 , A61K31/35 , A61K31/415 , A61K31/495 , C07D309/10 , C07D405/10
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。

54. 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.

55. 发明授权

US4645759A Renin inhibiting compounds 失效
标题翻译：肾素抑制化合物
公开(公告)号：US4645759A
公开(公告)日：1987-02-24
申请号：US735491
申请日：1985-05-17
申请人： Jay R. Luly , John J. Plattner , Joseph F. Dellaria
发明人： Jay R. Luly , John J. Plattner , Joseph F. Dellaria
IPC分类号： A61K38/00 , C07K5/02 , C07K5/065 , A61K37/43 , C07K5/08
CPC分类号： C07K5/06078 , C07K5/0227 , A61K38/00 , Y02P20/55 , Y10S530/86
摘要： The invention relates to renin inhibiting compounds of the formula ##STR1## wherein A is an N-protecting group; n is 0 or 1; B is hydrogen, hydroxy, NH, loweralkyl or arylalkyl; with the proviso that when A is an N-protecting group, B is NH and when n is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R.sub.1, R.sub.3 and R.sub.5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R.sub.2, R.sub.4, R.sub.7, R.sub.8 and R.sub.9 are hydrogen or loweralkyl and may be the same or different; X is NH, O, S, SO or SO.sub.2 ; and R.sub.6 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group, with the proviso that R.sub.6 may be an N-protecting group when X is NH.
摘要翻译：本发明涉及下式的肾素抑制化合物，其中A是N-保护基; n为0或1; B是氢，羟基，NH，低级烷基或芳基烷基; 条件是当A是N-保护基时，B是NH，当n是0时，B是氢，羟基，低级烷基或芳基烷基; R 1，R 3和R 5是低级烷基或亲水性，亲油性或芳族氨基酸侧链，可以相同或不同; R2，R4，R7，R8和R9是氢或低级烷基，可以相同或不同; X是NH，O，S，SO或SO 2; 并且R 6为低级烷基，环烷基，环烷基烷基，芳基，芳烷基或N-保护基，条件是当X为NH时，R 6可为N-保护基。

56. 发明授权

US08802853B2 Arylalkenyl and arylalkynyl substituted imidazoquinolines 有权
标题翻译：芳基烯基和芳基炔基取代的咪唑并喹啉
公开(公告)号：US08802853B2
公开(公告)日：2014-08-12
申请号：US10596890
申请日：2004-12-17
申请人： Jason D. Bonk , Joseph F. Dellaria, Jr.
发明人： Jason D. Bonk , Joseph F. Dellaria, Jr.
IPC分类号： C07D487/04 , C07D487/06 , A61K31/4375
CPC分类号： C07D471/04
摘要： Arylalkenyl and aryalkynyl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
摘要翻译：公开了芳基烯基和芳炔基取代的咪唑并喹啉化合物，含有化合物的化合物的药物组合物，中间体和这些化合物作为免疫调节剂的用途，用于诱导动物中的细胞因子生物合成和治疗包括病毒和肿瘤的疾病。

57. 发明授权

US08778963B2 Hydroxylamine and oxime substituted imidazoquinolines, imidazopyridines, and imidazonaphthyridines 有权
标题翻译：羟胺和肟取代的咪唑并喹啉，咪唑并吡啶和咪唑并吡啶类
公开(公告)号：US08778963B2
公开(公告)日：2014-07-15
申请号：US10595895
申请日：2004-11-24
申请人： Larry R. Krepski , Joseph F. Dellaria, Jr. , Gregory J. Marszalek
发明人： Larry R. Krepski , Joseph F. Dellaria, Jr. , Gregory J. Marszalek
IPC分类号： C07D487/06 , C07D471/06 , A61K31/437
CPC分类号： C07D471/04 , C07D471/14
摘要： Imidazo-quinoline, -pyridine, and -naphthyridine ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
摘要翻译：在1-位取代的咪唑并喹啉，吡啶和萘啶环体系，含有这些化合物的化合物，中间体和使用方法作为免疫调节剂的药物组合物，用于在动物中诱导细胞因子生物合成和治疗疾病，包括公开了病毒和肿瘤疾病。

58. 发明授权

US08697873B2 Amide substituted imidazopyridines, imidazoquinolines, and imidazonaphthyridines 有权
标题翻译：酰胺取代的咪唑并吡啶，咪唑并喹啉和咪唑并吡啶
公开(公告)号：US08697873B2
公开(公告)日：2014-04-15
申请号：US10599159
申请日：2005-03-24
申请人： Larry R. Krepski , Joseph F. Dellaria, Jr. , Daniel E. Duffy , David T. Amos , Bernhard M. Zimmermann , William H. Moser
发明人： Larry R. Krepski , Joseph F. Dellaria, Jr. , Daniel E. Duffy , David T. Amos , Bernhard M. Zimmermann , William H. Moser
IPC分类号： C07D401/02 , A61K31/437
CPC分类号： C07D471/04 , C07D413/14 , C07D471/02 , C07D471/12 , C07D471/14
摘要： Imidazopyridine, imidazoquinoline, and imidazonaphthyridine compounds having an amide substituent at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
摘要翻译：咪唑并吡啶，咪唑并喹啉和咪唑并吡啶化合物，其在1-位具有酰胺基取代基，含有化合物的药物组合物，中间体及其制备方法以及这些化合物作为免疫调节剂的用途，用于调节动物中的细胞因子生物合成和治疗公开了包括病毒和肿瘤疾病在内的疾病。

59. 发明授权

US08541438B2 Substituted imidazoquinolines, imidazopyridines, and imidazonaphthyridines 有权
公开(公告)号：US08541438B2
公开(公告)日：2013-09-24
申请号：US12974459
申请日：2010-12-21
申请人： Doris Stoermer , Joseph F. Dellaria, Jr. , David T. Amos , Bernhard M. Zimmermann , Luke T. Dressel , Jason D. Bonk , Matthew R. Radmer
发明人： Doris Stoermer , Joseph F. Dellaria, Jr. , David T. Amos , Bernhard M. Zimmermann , Luke T. Dressel , Jason D. Bonk , Matthew R. Radmer
IPC分类号： C07D487/16 , C07D487/14 , A61K31/437
CPC分类号： C07D471/04 , A61K31/341 , A61K31/351 , A61K31/435 , A61K31/437 , A61K31/445 , C07D471/14
摘要： Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

60. 发明申请

US20120035209A1 Hydroxy Substituted 1H-Imidazopyridines and Methods 审中-公开
标题翻译：羟基取代的1H-咪唑并吡啶及其方法
公开(公告)号：US20120035209A1
公开(公告)日：2012-02-09
申请号：US13277619
申请日：2011-10-20
申请人： Joseph F. Dellaria, JR. , William H. Moser , Matthew R. Radmer , George W. Griesgraber
发明人： Joseph F. Dellaria, JR. , William H. Moser , Matthew R. Radmer , George W. Griesgraber
IPC分类号： A61K31/437 , A61P35/00 , A61P31/12 , C07D471/04
CPC分类号： C07D471/04
摘要： Hydroxy substituted 1H-imidazo[4,5-c]pyridin-4-amines, with a hydroxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
摘要翻译：在2-位羟基取代的1H-咪唑并[4,5-c]吡啶-4-胺，含有这些化合物的药物组合物，制备化合物的方法，中间体和这些化合物的使用方法如公开了用于在动物中诱导细胞因子生物合成和用于治疗包括病毒和肿瘤疾病的疾病的免疫调节剂。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式