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1. 发明申请

US20100022594A1 HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION 失效
标题翻译： β-淀粉酶生产的杂环磺酰胺抑制剂
公开(公告)号：US20100022594A1
公开(公告)日：2010-01-28
申请号：US12576513
申请日：2009-10-09
申请人： Anthony F. Kreft , Derek Cecil Cole , Kevin R. Woller , Joseph R. Stock , George Diamantidis , Dennis M. Kubrak , Kristina M. Kutterer , William J. Moore , David S. Casebier
发明人： Anthony F. Kreft , Derek Cecil Cole , Kevin R. Woller , Joseph R. Stock , George Diamantidis , Dennis M. Kubrak , Kristina M. Kutterer , William J. Moore , David S. Casebier
IPC分类号： A61K31/381 , A61K31/4535 , A61K31/382 , A61K31/34 , C07D409/12 , C07D333/34 , C07D307/64 , A61P25/00
CPC分类号： C07D409/12 , C07D307/64 , C07D333/34
摘要： Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.
摘要翻译：提供其中R1，R2，R3，R4，R5，R6，T，W，X，Y和Z如本文所定义的式（I）化合物及其药学上可接受的盐，水合物和/或前药。描述了使用这些化合物抑制β淀粉样蛋白生成和治疗阿尔茨海默病和唐氏综合征的方法。

2. 发明申请

US20090181932A1 COMPOSITIONS CONTAINING O-SULFATE AND O-PHOSPHATE CONTAINING ARYL SULFONAMIDE DERIVATIVES USEFUL AS beta-AMYLOID INHIBITORS 审中-公开
标题翻译：含有硫酸钠和含有磺酰亚胺衍生物的O-磷酸酯的组合物作为β-AMYLOID抑制剂有用
公开(公告)号：US20090181932A1
公开(公告)日：2009-07-16
申请号：US12349850
申请日：2009-01-07
申请人： David Zenan LI , Dane Springer , Sayed Elmarakby , Appavu Chandrasekaran , Anthony F. Kreft, III
发明人： David Zenan LI , Dane Springer , Sayed Elmarakby , Appavu Chandrasekaran , Anthony F. Kreft, III
IPC分类号： A61K31/18 , C07D333/34 , C07C305/02 , A61K31/66 , A61P35/00 , A61P25/28 , C07F9/09 , A61K31/381
CPC分类号： C07C305/04 , A61K31/18 , A61K31/381 , A61K31/661 , C07D333/34
摘要： A synthetic compound characterized by having the structure of formula I or II or a pharmaceutically acceptable salt and/or hydrate thereof is provided. Formula I and formula II are defined as follows. wherein R1 is substituted aryl or substituted heteroaryl; R2 and R3 are independently selected from the group consisting of CF3, substituted phenyl, C1-C4 alkyl, substituted C1-C4 alkyl, (CF3)nC1-C4alkyl, (CF3)n(substituted C1-C4 alkyl), provided that when R2 or R3 is CF3, the other is not an unsubstituted alkyl; R4 and R4′ are independently selected from the group consisting of M, C1-C4 alkyl, phenyl, and benzyl, wherein M is a metal ion is selected from the group consisting of sodium, lithium, calcium, magnesium and potassium, or R4 and R4′ are taken together to form a cyclic structure. Methods of making such compounds and uses thereof are also provided.
摘要翻译：提供了具有式I或II结构或其药学上可接受的盐和/或水合物的合成化合物。式I和式II定义如下。其中R1是取代的芳基或取代的杂芳基; R 2和R 3独立地选自CF 3，取代的苯基，C 1 -C 4烷基，取代的C 1 -C 4烷基，（CF 3）n C 1 -C 4烷基，（CF 3）n（取代的C 1 -C 4烷基），条件是当R 2 或R3是CF3，另一个不是未取代的烷基; R4和R4'独立地选自M，C1-C4烷基，苯基和苄基，其中M是金属离子选自钠，锂，钙，镁和钾，或R4和 R4'一起形成环状结构。还提供了制备这些化合物的方法及其用途。

3. 发明授权

US5824699A Carbazole inhibitors of Cox-2 失效
标题翻译： Cox-2的咔唑抑制剂
公开(公告)号：US5824699A
公开(公告)日：1998-10-20
申请号：US39871
申请日：1998-03-16
申请人： Anthony F. Kreft , Craig E. Caufield , Amedeo A. Failli , Thomas J. Caggiano , Alexander A. Greenfield , Dennis M. Kubrak
发明人： Anthony F. Kreft , Craig E. Caufield , Amedeo A. Failli , Thomas J. Caggiano , Alexander A. Greenfield , Dennis M. Kubrak
IPC分类号： C07D209/86 , C07D491/04 , C07D491/052 , A61K31/40 , C07D209/82
CPC分类号： C07D491/04 , C07D209/86
摘要： This invention provides compounds of formula I having the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are, each, independently, hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aralkoxy, trifluroalkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, cyano, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido; R.sub.5 is hydrogen, alkyl, alkenyl, alkoxyalkyl or alkylcycloalkyl; R.sub.6 is hydrogen, alkyl or alkenyl; X is oxygen or carbon; A is oxygen or NZ; Z is hydroxyl, alkoxy, aryloxy, carboxyalkyloxy of 2-7 carbon atoms, arylamino, or alkylsulfonyamino of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.
摘要翻译：本发明提供具有结构式I的式I化合物，其中R 1，R 2，R 3和R 4各自独立地为氢，烷基，烯基，炔基，烷氧基，芳烷氧基，三氟烷氧基，烷酰氧基，羟基，卤素，三氟甲基，氰基，氨基，单 - 或二 - 烷基氨基，烷酰氨基或烷磺酰氨基; R5是氢，烷基，烯基，烷氧基烷基或烷基环烷基; R6是氢，烷基或烯基; X是氧或碳; A是氧气或NZ; Z为2-7个碳原子的羟基，烷氧基，芳氧基，羧基烷氧基，芳基氨基或1-6个碳原子的烷基磺酰氨基; 或其药学上可接受的盐，其可用于治疗关节炎疾病，结肠直肠癌和阿尔茨海默氏病。

4. 发明授权

US5364944A Substituted benzoylbenzene-, biphenyl- and 2-oxazole- alkanoic acid compounds 失效
标题翻译：取代苯甲酰基苯，联苯基和2-恶唑烷酸化合物
公开(公告)号：US5364944A
公开(公告)日：1994-11-15
申请号：US001141
申请日：1993-01-06
申请人： Amedeo A. Failli , Anthony F. Kreft, III , John H. Musser , Annette L. Banker , James A. Nelson , Uresh S. Shah , Dennis M. Kubrak
发明人： Amedeo A. Failli , Anthony F. Kreft, III , John H. Musser , Annette L. Banker , James A. Nelson , Uresh S. Shah , Dennis M. Kubrak
IPC分类号： C07C45/00 , C07C45/63 , C07C45/72 , C07C59/90 , C07C69/738 , C07C205/45 , C07C255/40 , C07D215/14 , C07D263/32 , C07D277/24 , C07D413/12 , C07D233/54
CPC分类号： C07C45/004 , C07C205/45 , C07C255/40 , C07C45/63 , C07C45/72 , C07C59/90 , C07C69/738 , C07D215/14 , C07D263/32 , C07D413/10
摘要： There are disclosed substituted benzoylbenzene-, biphenyl- and 2-oxazole- alkanoic acid derivatives and the pharmacologically acceptable salts thereof as inhibitors of PLA.sub.2 and lipoxygenase, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated naso-bronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastric cytoprotective agents.
摘要翻译：公开了取代的苯甲酰基苯，联苯基和2-恶唑烷酸衍生物及其药理学上可接受的盐作为PLA2和脂氧合酶的抑制剂，以及它们在治疗炎性病症如类风湿性关节炎，溃疡性结肠炎，牛皮癣和其他立即超敏反应; 治疗白三烯介导的鼻支气管阻塞性通气条件，如过敏性鼻炎，过敏性支气管哮喘等; 和作为胃细胞保护剂。

5. 发明授权

US5229516A Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase 失效
标题翻译：取代的吲哚，茚，吡喃吲哚和四氢咔唑 - 链烷酸衍生物作为PLA2和脂氧合酶的抑制剂
公开(公告)号：US5229516A
公开(公告)日：1993-07-20
申请号：US911434
申请日：1992-07-10
申请人： John H. Musser , Anthony F. Kreft, III , Amedeo A. Failli , Christopher A. Demerson , Uresh S. Shah , James A. Nelson
发明人： John H. Musser , Anthony F. Kreft, III , Amedeo A. Failli , Christopher A. Demerson , Uresh S. Shah , James A. Nelson
IPC分类号： C07C323/62 , C07D209/22 , C07D215/14 , C07D401/12 , C07D401/14 , C07D417/12 , C07D491/04
CPC分类号： C07D401/12 , C07C323/62 , C07D209/22 , C07D215/14 , C07D401/14 , C07D417/12 , C07D491/04
摘要： There are disclosed compounds of the formulaA(CH.sub.2).sub.n O-BwhereinA is C.sub.4 -C.sub.8 alkyl, phenoxyethyl, phenoxyphenyl or a group having the formula ##STR1## wherein ##STR2## R.sup.1 is hydrogen, lower alkyl, phenyl or phenyl substituted with trifluoromethyl;R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring;R.sup.3 is hydrogen or lower alkyl;n is 1-2;B is ##STR3## wherein ##STR4## m is 0-3; R.sup.5 is ##STR5## or phenyl or phenyl substituted by halo, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl;R.sup.6 is A(CH.sub.2).sub.n O-- or halo; with the proviso that when R.sup.6 is halo, R.sup.5 is ##STR6## R.sup.7 is lower alkyl; Y is --CH.sub.2 -- or --O--;R.sup.8 is lower alkyl or --(CH.sub.2).sub.m CO.sub.2 R.sup.3 ;R.sup.9 is ##STR7## or --CH.sub.2 R.sup.10 ; R.sup.10 is lower alkyl, phenyl, phenyl substituted with carboxy, halo, loweralkylthio or loweralkylsulfinyl, pyridyl, furanyl or quinolinyl;R.sup.11 is lower alkyl or phenyl;Z is hydrogen, lower alkyl or --N(CH.sub.3)OH;and the pharmacologically acceptable salts thereof, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated naso-bronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastric cytoprotective agents.
摘要翻译：公开了式A（CH 2）n O-B的化合物，其中A是C 4 -C 8烷基，苯氧基乙基，苯氧基苯基或具有下式的基团：其中R 1是氢，低级烷基，苯基或被三氟甲基取代的苯基; R2是氢或低级烷基; 或R 1和R 2一起形成苯环; R3是氢或低级烷基; n为1-2; B是其中 m是0-3; R 5为苯基或被卤素，低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基取代的苯基; R6是A（CH2）nO-或卤素; 条件是当R 6为卤素时，R 5为低级烷基; Y是-CH 2 - 或-O-; R8是低级烷基或 - （CH2）mCO2R3; R9是或-CH2R10; R 10为低级烷基，苯基，被羧基，卤素，低级烷硫基或低级烷基亚磺酰基取代的苯基，吡啶基，呋喃基或喹啉基; R11为低级烷基或苯基; Z是氢，低级烷基或-N（CH 3）OH; 及其药理学上可接受的盐及其在治疗炎性病症如类风湿性关节炎，溃疡性结肠炎，牛皮癣和其他立即超敏反应中的用途; 治疗白三烯介导的鼻支气管阻塞性通气条件，如过敏性鼻炎，过敏性支气管哮喘等; 和作为胃细胞保护剂。

6. 发明授权

US4754043A Oxazole and thiazole naphthalenes as antiallergic agents 失效
标题翻译：恶唑和噻唑萘作为抗过敏剂
公开(公告)号：US4754043A
公开(公告)日：1988-06-28
申请号：US915444
申请日：1986-10-06
申请人： Anthony F. Kreft, III , John H. Musser , Thomas W. Pattison , John P. Yardley
发明人： Anthony F. Kreft, III , John H. Musser , Thomas W. Pattison , John P. Yardley
IPC分类号： C07D213/30 , C07D215/14 , C07D277/24 , C07D277/64 , C07D277/62 , C07D263/30 , C07D263/54 , C07D277/20
CPC分类号： C07D213/30 , C07D215/14 , C07D277/64
摘要： There are disclosed compounds of the formula ##STR1## wherein X is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## Z is CR or N, where n=1; or Z is O,S, or NR, when n=0; R is hydrogen or loweralkyl;n is 0 or 1;R.sup.1 is hydroxy, amino, loweralkyl sulfonamido, perfluoro loweralkyl sulfonamido or OR;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is hydrogen or loweralkyl; orR.sup.2 and R.sup.3 taken together form a benzene ring; andthe dotted line represents an optional double bond;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.
摘要翻译：公开了下式的化合物，其中X是-CH 2 CH 2 - ， - CH = CH-，Z是CR或N，其中n = 1; 或当N = 0时，Z为O，S或NR; R是氢或低级烷基; n为0或1; R1是羟基，氨基，低级烷基亚磺酰氨基，全氟低级烷基亚磺酰氨基或OR; R2是氢或低级烷基; R3是氢或低级烷基; 或R 2和R 3一起形成苯环; 虚线表示任选的双键; 及其药学上可接受的盐，以及它们在治疗白三烯介导的鼻支气管阻塞性空气通道病症如过敏性鼻炎，过敏性支气管哮喘等中的用途。

7. 发明授权

US4719308A Imidazolylmethoxy naphthalene compounds as antiallergic agents 失效
标题翻译：咪唑甲氧基萘化合物作为抗过敏剂
公开(公告)号：US4719308A
公开(公告)日：1988-01-12
申请号：US915443
申请日：1986-10-06
申请人： Anthony F. Kreft, III , John H. Musser , Thomas W. Pattison , John P. Yardley
发明人： Anthony F. Kreft, III , John H. Musser , Thomas W. Pattison , John P. Yardley
IPC分类号： C07D213/30 , C07D215/14 , C07D233/64 , C07D277/64
CPC分类号： C07D213/30 , C07D215/14 , C07D277/64
摘要： There are disclosed compounds of the formula ##STR1## wherein X is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## Z is CR or N, when n=1; or Z is O, S, or NR, when n=0, R is hydrogen or loweralkyl;n is 0 or 1;R.sup.1 is hydroxy, amino, loweralkyl sulfonamido, perfluoro loweralkyl sulfonamido or OR;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is hydrogen or loweralkyl; orR.sup.2 and R.sup.3 taken together form a benzene ring; andthe dotted line represents an optional double bond;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.
摘要翻译：公开了下式的化合物，其中当n = 1时，X是-CH 2 CH 2 - ， - CH = CH-，Z是CR或N; 或Z为O，S或NR，当n = 0时，R为氢或低级烷基; n为0或1; R1是羟基，氨基，低级烷基亚磺酰氨基，全氟低级烷基亚磺酰氨基或OR; R2是氢或低级烷基; R3是氢或低级烷基; 或R 2和R 3一起形成苯环; 虚线表示任选的双键; 及其药学上可接受的盐，以及它们在治疗白三烯介导的鼻支气管阻塞性空气通道病症如过敏性鼻炎，过敏性支气管哮喘等中的用途。

8. 发明授权

US4448729A Leucotriene antagonists 失效
标题翻译：白三烯拮抗剂
公开(公告)号：US4448729A
公开(公告)日：1984-05-15
申请号：US411200
申请日：1982-08-25
申请人： Dieter H. Klaubert , Anthony F. Kreft, III , Stanley C. Bell
发明人： Dieter H. Klaubert , Anthony F. Kreft, III , Stanley C. Bell
IPC分类号： C07C205/37 , C07C233/00 , C07C255/59 , C07C121/80 , C07C69/612 , C07C103/29
CPC分类号： C07C255/00 , C07C205/37
摘要： The compounds ##STR1## wherein each X is, independently, --O-- or --NR.sub.5, in which R.sub.5 is hydrogen or alkyl; R is alkyl, R.sub.1 is hydrogen or alkyl, R.sub.2 is hydrogen, hydroxy, amino, alkylamino, dialkylamino or alkanoylamino and when m or n is O, R.sub.2 is hydroxymethyl, aminomethyl, alkylaminomethyl, dialkylaminomethyl or alkanoylaminomethyl; R.sub.3 is hydrogen, --CN, --CONH.sub.2 or --CO.sub.2 M in which M is hydrogen, alkyl or ##STR2## in which p is an integer from 2 to 6 and R.sub.6 and R.sub.7 are, independently, hydrogen or alkyl; R.sub.4 is --NH.sub.2, --NHCOR.sub.8 in which R.sub.8 is alkyl, --NHCOCO.sub.2 Z or --NHCOCH.sub.2 CH.sub.2 CO.sub.2 Z in which Z is hydrogen or alkyl; m and n are 0, 1, 2, 3 or 4 such that when n is from 1 to 4, m is 0 or 1 and when m is from 1 to 4, n is 0 or 1; or pharmaceutically acceptable salts thereof are leucotriene antagonists useful as antiallergy agents.
摘要翻译：化合物＆lt; IMAGE＆gt;其中每个X独立地是-O-或-NR 5，其中R 5是氢或烷基; R是烷基，R 1是氢或烷基，R 2是氢，羟基，氨基，烷基氨基，二烷基氨基或烷酰基氨基，当m或n是O时，R 2是羟甲基，氨基甲基，烷基氨基甲基，二烷基氨基甲基或烷酰基氨基甲基。 R 3是氢，-CN，-CONH 2或-CO 2 M，其中M是氢，烷基或者其中p是2至6的整数，R 6和R 7独立地是氢或烷基; R4是-NH2，-NHCOR8，其中R8是烷基，-NHCOCO2Z或-NHCOCH2CH2CO2Z，其中Z是氢或烷基; m和n分别为0,1,2,3或4，使得当n为1至4时，m为0或1，当m为1至4时，n为0或1; 或其药学上可接受的盐是可用作抗过敏剂的白三烯拮抗剂。

9. 发明申请

US20110034513A1 Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production 审中-公开
标题翻译： β淀粉样蛋白生产的杂环磺酰胺抑制剂
公开(公告)号：US20110034513A1
公开(公告)日：2011-02-10
申请号：US12907123
申请日：2010-10-19
申请人： Anthony F. Kreft , Derek C. Cole , Kevin R. Woller , Joseph R. Stock , George Diamantidis , Dennis M. Kubrak , Kristina M. Kutterer , William J. Moore , David S. Casebier
发明人： Anthony F. Kreft , Derek C. Cole , Kevin R. Woller , Joseph R. Stock , George Diamantidis , Dennis M. Kubrak , Kristina M. Kutterer , William J. Moore , David S. Casebier
IPC分类号： A61K31/4535 , A61P25/28 , A61K31/381 , A61K31/341 , A61K31/382
CPC分类号： C07D409/12 , C07D307/64 , C07D333/34
摘要： Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.
摘要翻译：提供其中R1，R2，R3，R4，R5，R6，T，W，X，Y和Z如本文所定义的式（I）化合物及其药学上可接受的盐，水合物和/或前药。描述了使用这些化合物抑制β淀粉样蛋白生成和治疗阿尔茨海默病和唐氏综合征的方法。

10. 发明授权

US5776967A Pyranoindole inhibitors of COX--2 失效
标题翻译： COX-2的吡喃吲哚抑制剂
公开(公告)号：US5776967A
公开(公告)日：1998-07-07
申请号：US888983
申请日：1997-07-07
申请人： Anthony F. Kreft , Craig E. Caufield , Amedeo A. Failli , Thomas J. Caggiano , Alexander A. Greenfield , Dennis M. Kubrak
发明人： Anthony F. Kreft , Craig E. Caufield , Amedeo A. Failli , Thomas J. Caggiano , Alexander A. Greenfield , Dennis M. Kubrak
IPC分类号： C07D209/86 , C07D491/04 , C07D491/052 , A61K31/40 , A61K31/35 , C07D209/80 , C07D311/78
CPC分类号： C07D491/04 , C07D209/86
摘要： This invention provides compounds of formula I having the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are, each, independently, hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aralkoxy, trifluroalkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, cyano, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido; R.sub.5 is hydrogen, alkyl, alkenyl, alkoxyalkyl or alkylcycloalkyl; R.sub.6 is hydrogen, alkyl or alkenyl; X is oxygen or carbon; A is oxygen or NZ; Z is hydroxyl, alkoxy, aryloxy, carboxyalkyloxy of 2-7 carbon atoms, arylamino, or alkylsulfonyamino of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.
摘要翻译：本发明提供具有结构式I的式I化合物，其中R 1，R 2，R 3和R 4各自独立地为氢，烷基，烯基，炔基，烷氧基，芳烷氧基，三氟烷氧基，烷酰氧基，羟基，卤素，三氟甲基，氰基，氨基，单 - 或二 - 烷基氨基，烷酰氨基或烷磺酰氨基; R5是氢，烷基，烯基，烷氧基烷基或烷基环烷基; R6是氢，烷基或烯基; X是氧或碳; A是氧气或NZ; Z为2-7个碳原子的羟基，烷氧基，芳氧基，羧基烷氧基，芳基氨基或1-6个碳原子的烷基磺酰氨基; 或其药学上可接受的盐，其可用于治疗关节炎疾病，结肠直肠癌和阿尔茨海默氏病。

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