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1. 发明授权

US5830911A Pyranoindole and tetrahydrocarbazole inhibitors of COX-2 失效
标题翻译：吡咯并吲哚和COX-2的四氢咔唑抑制剂
公开(公告)号：US5830911A
公开(公告)日：1998-11-03
申请号：US906361
申请日：1997-08-05
申请人： Amedeo A. Failli , Robert J. Steffan , Anthony F. Kreft , Thomas J. Caggiano , Craig E. Caufield
发明人： Amedeo A. Failli , Robert J. Steffan , Anthony F. Kreft , Thomas J. Caggiano , Craig E. Caufield
IPC分类号： C07D209/88 , C07D491/04 , A61K31/40 , C07D209/86
CPC分类号： C07D491/04 , C07D209/88
摘要： This invention provides compounds of formula I having the structure ##STR1## wherein R is (CH.sub.2).sub.n COOR.sup.4 ; R.sup.1 is hydrogen, alkyl, alkenyl, alkynyl, alkylcycloalkyl, and alkoxyalkyl; R.sup.4 is hydrogen or alkyl; R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, arylalkoxy, fluoroalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, cyano, nitro, --SCF.sub.3, --COR.sup.3, alkanoyloxy, hydroxy, trifluoromethyl, amino, alkylamino, dialkylamino, alkylamido, or alkylsulfonamido; wherein at least one of R.sup.5, R.sup.6, R.sup.7, or R.sup.8 is cyano; R.sup.3 is alkyl, hydroxy, alkoxy, amino, alkylamino; X is --O-- or --C--; and n=1-4 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图1的式I化合物，其中R是（CH 2）n COOR 4; R1是氢，烷基，烯基，炔基，烷基环烷基和烷氧基烷基; R4是氢或烷基; R5，R6，R7和R8各自独立地为氢，卤素，烷基，烯基，炔基，烷氧基，芳基烷氧基，氟烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，氰基，硝基，-SCF3，-COR3，烷酰氧基，羟基，，氨基，烷基氨基，二烷基氨基，烷基酰氨基或烷基磺酰氨基; 其中R 5，R 6，R 7或R 8中的至少一个为氰基; R3是烷基，羟基，烷氧基，氨基，烷基氨基; X是-O-或-C-; 和n = 1-4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。

2. 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。

3. 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。

4. 发明授权

US5446048A Rapamycin oximes 失效
标题翻译：雷帕霉素肟
公开(公告)号：US5446048A
公开(公告)日：1995-08-29
申请号：US309816
申请日：1994-09-21
申请人： Amedeo A. Failli , Robert J. Steffan , Craig E. Caufield , David C. Hu , Alexander A. Grinfeld
发明人： Amedeo A. Failli , Robert J. Steffan , Craig E. Caufield , David C. Hu , Alexander A. Grinfeld
IPC分类号： C07D498/18 , A61K31/44
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.3 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or --CO.sub.2 R.sup.8 ;R.sup.4 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, aminoalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, or --CO.sub.2 R.sup.8 ;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, or --CO.sub.2 R.sup.8 ;R.sup.6 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.7 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, fluorenylmethyl, or Ar;Y is O or S;X is .dbd.N--O--(CH.sub.2).sub.f --Z or .dbd.N--O--Ar;Z is hydrogen, alkenyl, alkynyl, alkoxy, cyano, fluoro, trifluoromethyl, --NR.sup.5 R.sup.6, aryloxy, or Ar;Ar is aryl which may be optionally mono-, di-, or tri-substituted;a=0-4;b=0-1;c=0-4;d=0-6;e=0-6; andf=0-6;or a pharmaceutically acceptable salt thereof, with the proviso that when f is 0, Z is hydrogen and further provided that when R.sup.3 or R.sup.5 is --CO.sub.2 R.sup.8, R.sup.8 is not hydrogen which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：其中R1是氢，烷基，烯基，炔基，三氟甲基，芳基烷基或Ar的结构化合物 R3是氢，烷基，烯基，炔基，三氟甲基，芳烷基或-CO2R8; R4是烷基，烯基，炔基，三氟甲基，芳基烷基，Ar，氨基烷基，硫代烷基，烷硫基烷基，羟基烷基或-CO 2 R 8; R5是氢，烷基，烯基，炔基，三氟甲基，芳基烷基，Ar或-CO 2 R 8; R6是氢，烷基，烯基，炔基，三氟甲基，芳烷基或Ar; R7是烷基，烯基，炔基，三氟甲基，芳烷基或Ar; R8是氢，烷基，烯基，炔基，三氟甲基，芳基烷基，芴基甲基或Ar; Y为O或S; X = N-O-（CH 2）f-Z或= N-O-Ar; Z是氢，烯基，炔基，烷氧基，氰基，氟，三氟甲基，-NR5R6，芳氧基或Ar; Ar是可任选被单，二或三取代的芳基; a = 0-4; b = 0-1; c = 0-4; d = 0-6; e = 0-6; 和f = 0-6; 或其药学上可接受的盐，条件是当f为0时，Z为氢，并且还提供当R3或R5为-CO2R8时，R8不为氢，可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤代理商

5. 发明授权

US5130307A Aminoesters of rapamycin 失效
标题翻译：雷帕霉素的氨基酯
公开(公告)号：US5130307A
公开(公告)日：1992-07-14
申请号：US657294
申请日：1991-02-19
申请人： Amedeo A. Failli , Craig E. Caufield , Robert J. Steffan
发明人： Amedeo A. Failli , Craig E. Caufield , Robert J. Steffan
IPC分类号： A61K38/00 , C07D498/18 , C07H19/01 , C07K5/06
CPC分类号： C07D498/18 , C07H19/01 , C07K5/06026 , A61K38/00
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or ##STR2## with the proviso that R.sup.1 and R.sup.2 are not both hydrogen; R.sup.3 is hydrogen, alkyl, aralkyl, --(CH.sub.2).sub.q CO.sub.2 R.sup.6,--(CH.sub.2).sub.r NR.sup.7 CO.sub.2 R.sup.8, carbamylalkyl, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenyklmethyl, imidazoylmethyl or phenyl which is optionally mono-, di-, or tri-substituted with a sustituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid;R.sup.4 and R.sup.7 are each, independently, hydrogen, alkyl, or aralkyl;R.sup.5, R.sup.6, and R.sup.8 are each, indpendently, alkyl, aralkyl, fluorenylmethyl, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid;m is 0-4;n is 0-4;p is 1-2;q is 0-4;r is 0-4;wherein R.sup.3, R.sup.4, m, and n are independent in each of the ##STR3## subunits when p=2; or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, and by virtue of its antifungal activity is useful in treating fungal infections.
摘要翻译：结构的化合物，其中R1和R2各自独立地为氢或“IMAGE”，条件是R1和R2不同时为氢; R3是氢，烷基，芳烷基， - （CH2）rNR7CO2R8，氨基甲酰基烷基，氨基烷基，羟基烷基，脒基烷基，巯基烷基，烷基硫代烷基，吲哚甲基，羟基苯甲酮，咪唑基甲基或苯基，其任选是单 - ，二 - 或三被选自烷基，烷氧基，羟基，氰基，卤素，硝基，烷氧基，三氟甲基，氨基或羧酸的取代基取代; R 4和R 7各自独立地为氢，烷基或芳烷基; R5，R6和R8各自独立地是烷基，芳烷基，芴基甲基或苯基，其任选被选自烷基，烷氧基，羟基，氰基，卤素，硝基，烷氧基中的取代基单，二或三取代，三氟甲基，氨基或羧酸; m为0-4; n为0-4; p是1-2; q为0-4; r为0-4; 当p = 2时，R 3，R 4，m和n在每个亚基中是独立的; 或其药学上可接受的盐，其由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病，并且由于其抗真菌活性可用于治疗真菌感染。

6. 发明授权

US5373014A Rapamycin oximes 失效
标题翻译：雷帕霉素肟
公开(公告)号：US5373014A
公开(公告)日：1994-12-13
申请号：US134237
申请日：1993-10-08
申请人： Amedeo A. Failli , Robert J. Steffan , Craig E. Caufield , David C. Hu , Alexander A. Grinfeld
发明人： Amedeo A. Failli , Robert J. Steffan , Craig E. Caufield , David C. Hu , Alexander A. Grinfeld
IPC分类号： C07D498/18 , A61K31/395 , C07D491/16
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.3 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or --CO.sub.2 R.sup.8 ;R.sup.4 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, aminoalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, or --CO.sub.2 R.sup.8 ;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, At, or --CO.sub.2 R.sup.8 ;R.sup.6 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.7 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, fluorenylmethyl, orAr;Y is O or S;X is .dbd.N--O--(CH.sub.2).sub.f --Z or .dbd.N--O--Ar;Z is hydrogen, alkenyl, alkynyl, alkoxy, cyano, fluoro, trifluoromethyl, --NR.sup.5 R.sup.6, aryloxy, or Ar;Ar is aryl which may be optionally mono-, di-, or tri- substituted;a=0-4;b=0-1;c=0-4;d=0-6;e=0-6; andf=0-6;or a pharmaceutically acceptable salt thereof, with the proviso that when f is 0, Z is hydrogen and further provided that when R.sup.3 or R.sup.5 is --CO.sub.2 R.sup.8, R.sup.8 is not hydrogen which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：其中R1是氢，烷基，烯基，炔基，三氟甲基，芳烷基或Ar的结构化合物 R3是氢，烷基，烯基，炔基，三氟甲基，芳烷基或-CO2R8; R4是烷基，烯基，炔基，三氟甲基，芳基烷基，Ar，氨基烷基，硫代烷基，烷硫基烷基，羟基烷基或-CO 2 R 8; R5是氢，烷基，烯基，炔基，三氟甲基，芳烷基，At或-CO2R8; R6是氢，烷基，烯基，炔基，三氟甲基，芳烷基或Ar; R7是烷基，烯基，炔基，三氟甲基，芳烷基或Ar; R8是氢，烷基，烯基，炔基，三氟甲基，芳基烷基，芴基甲基或Ar; Y为O或S; X = N-O-（CH 2）f-Z或= N-O-Ar; Z是氢，烯基，炔基，烷氧基，氰基，氟，三氟甲基，-NR5R6，芳氧基或Ar; Ar是可任选被单，二或三取代的芳基; a = 0-4; b = 0-1; c = 0-4; d = 0-6; e = 0-6; 和f = 0-6; 或其药学上可接受的盐，条件是当f为0时，Z为氢，并且还提供当R3或R5为-CO2R8时，R8不为氢，可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤代理商

7. 发明授权

US5023264A Rapamycin oximes 失效
标题翻译：雷帕霉素肟
公开(公告)号：US5023264A
公开(公告)日：1991-06-11
申请号：US553720
申请日：1990-07-16
申请人： Craig E. Caufield , Amedeo A. Failli
发明人： Craig E. Caufield , Amedeo A. Failli
IPC分类号： C07D498/18 , C07H19/01
CPC分类号： C07D498/18 , C07H19/01
摘要： A derivative of rapamycin in which the 27-position has the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl, or --CH.sub.2 Ar;Ar is ##STR2## wherein R.sup.2, R.sup.3, and R.sup.4 are each, independently, hydrogen, alkyl, aralkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid;X is N, O, or S;or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppresive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：雷帕霉素的衍生物，其中27位具有结构，其中R 1是氢，烷基或-CH 2 Ar; Ar是其中R 2，R 3和R 4各自独立地是氢，烷基，芳烷基，烷氧基，羟基，氰基，卤素，硝基，烷氧基，三氟甲基，氨基或羧酸。 X是N，O或S; 或其药学上可接受的盐，其由于其免疫抑制活性可用于治疗移植排斥宿主与移植物疾病，自身免疫疾病和炎症疾病。

8. 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。

9. 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。

10. 发明授权

US5218124A Substituted benzoylbenzene-, biphenyl- and 2-oxazole-alkanoic acid derivatives as inhibitors of pla2 and lipoxygenase 失效
标题翻译：取代的苯甲酰基苯，联苯基和2-恶唑烷酸衍生物作为pla2和脂氧合酶的抑制剂
公开(公告)号：US5218124A
公开(公告)日：1993-06-08
申请号：US891537
申请日：1992-06-01
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
CPC分类号： C07D413/10 , C07C205/45 , C07C255/40 , C07C45/004 , C07C45/63 , C07C45/72 , C07C59/90 , C07C69/738 , C07D215/14 , C07D263/32
摘要： There are disclosed compounds of the formulaA(CH.sub.2).sub.n O--BwhereinA is a group having the formula ##STR1## wherein X is --N-- or ##STR2## Z is ##STR3## R.sup.1 is hydrogen, lower alkyl or phenyl; R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring, with the proviso that when X is --N--, Z is other than ##STR4## R.sup.3 is hydrogen or lower alkyl; n is 1-2;B is ##STR5## wherein Y is OR.sup.5 or N(OH)R.sup.8 ;R.sup.4 and R.sup.5 are each, independently, hydrogen or lower alkyl;R.sup.6 is hydrogen, halo or nitro;R.sup.7 is ##STR6## R.sup.8 is lower alkyl; m is 0-3;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是具有下式的基团：其中X是-N-或者Z是R 1是氢，低级烷基或苯基; R2是氢或低级烷基; 或者R 1和R 2一起形成苯环，条件是当X是-N-时，Z不是R 3是氢或低级烷基; n为1-2; B是其中Y是OR 5或N（OH）R 8; R 4和R 5各自独立地为氢或低级烷基; R6是氢，卤素或硝基; R7是 R8是低级烷基; m为0-3; 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。

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