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公开(公告)号：US5362718A
公开(公告)日：1994-11-08
申请号：US229261
申请日：1994-04-18
IPC分类号： C07D487/18 , A61K31/00 , A61K31/435 , A61K31/436 , A61P9/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/10 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/695 , A61K31/395 , C07D498/16 , C07D7/04
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CO(CR.sup.3 R.sup.4).sub.b (CR.sup.5 R.sup.6).sub.d CR.sup.7 R.sup.8 R.sup.9 ;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or --F;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11, or R.sup.5 and R.sup.6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with --(CR.sup.3 R.sup.4).sub.f 0R.sup.10 ;R.sup.7 is hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11 ;R.sup.8 and R.sup.9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11, or R.sup.8 and R.sup.9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with --(CR.sup.3 R.sup.4).sub.f OR.sup.10 ;R.sup.10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl;R.sup.11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl;X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxanyl, 4-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2dialkyl)[1,3]dioxalanyl, or 4-(2,2-dicycloalkyl)[1,3]dioxalanyl;b=0-6;d=0-6; andf=0-6with the proviso that R.sup.1 and R.sup.2 are both not hydrogen and further provided that either R.sup.1 or R.sup.2 contains at least one --(CR.sup.3 R.sup.4).sub.f OR.sup.10, X, or --(CR.sup.3 R.sup.4).sub.f OR.sup.10 substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 其中R 1和R 2各自独立地是氢或-CO（CR 3 R 4）b（CR 5 R 6）d CR 7 R 8 R 9的结构化合物
R 3和R 4各自独立地为氢，烷基，烯基，炔基，三氟甲基或-F; R 5和R 6各自独立地为氢，烷基，烯基，炔基， - （CR 3 R 4）fOR 10，-CF 3，-F或-CO 2 R 11，或者R 5和R 6可以一起形成X或环烷基环， 用 - （CR 3 R 4）f O R 10单取代，二取代或三取代; R 7是氢，烷基，烯基，炔基， - （CR 3 R 4）fOR 10，-CF 3，-F或-CO 2 R 11; R 8和R 9各自独立地为氢，烷基，烯基，炔基， - （CR 3 R 4）fOR 10，-CF 3，-F或-CO 2 R 11，或者R 8和R 9可以一起形成X或环烷基环， 用 - （CR 3 R 4）fOR 10单取代，二取代或三取代; R 10是氢，烷基，烯基，炔基，三（烷基）甲硅烷基，三（烷基）甲硅烷基乙基，三苯甲基，苄基，烷氧基甲基，三（烷基）甲基乙氧基甲基，氯乙基或四氢吡喃基; R11是氢，烷基，烯基，炔基或苯基烷基; X是5-（2,2-二烷基）[1,3]二烷基，5-（2,2-二环烷基）[1,3]二氧杂环己基，4-（2,2-二烷基）[1,3] 4-（2,2-二环烷基）[1,3]二烷基，4-（2,2-二烷基）[1,3]二氧戊环基或4-（2,2-二环烷基）[1,3]二氧戊环基; b = 0-6; d = 0-6; 并且f = 0-6，条件是R 1和R 2都不是氢，并且进一步规定R1或R2含有至少一个 - （CR 3 R 4）fOR 10，X或 - （CR 3 R 4）fOR 10取代的环烷基，或药学上 其可接受的盐可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。 -
公开(公告)号：US5637590A
公开(公告)日：1997-06-10
申请号：US450772
申请日：1995-05-24
IPC分类号： A61K31/435 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/395 , C07D498/16
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted;with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 结构
的化合物，其中R和R 1各自独立地为氢，或者R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5，-COR 5，-CN，-NO 2 ，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R4是氢，烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。 -
公开(公告)号：US5559119A
公开(公告)日：1996-09-24
申请号：US391399
申请日：1995-02-27
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; ##STR3## are each, independently, a 5-7 membered saturated, unsaturated, or partially unsaturated heterocyclic radical, that is optionally fused to a phenyl ring or a cycloalkane or cycloalkene ring, wherein the heterocyclic ring may optionally contain O, S, or NR.sup.8 in the heterocyclic ring, and may be optionally substituted by R.sup.7 ;R.sup.7 is alkyl of 1-6 carbon atoms, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 结构式II的化合物，其中R和R 1各自独立地为氢，R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5，-COR 5，-CN ，-NO 2，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R4是氢，烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; 每个独立地是5-7元饱和的，不饱和的或部分不饱和的杂环基团，其任选地与苯环或环烷烃或环烯烃稠合，其中杂环可以任选地含有O， S或NR8，并且可以任选被R 7取代; R7是1-6个碳原子的烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6 ，或Ar; R 8是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。
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公开(公告)号：US5541192A
公开(公告)日：1996-07-30
申请号：US448902
申请日：1995-05-24
IPC分类号： A61K31/435 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/44 , A61K31/505 , A61K31/53
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5,--COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3R.sup.5, --OR.sup.5, --SR.sup.5, or Ar; R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6,--NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
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公开(公告)号：US5532355A
公开(公告)日：1996-07-02
申请号：US395012
申请日：1995-02-27
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6 or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; ##STR3## are each, independently, a 5-7 membered saturated, unsaturated, or partially unsaturated heterocyclic radical, that is optionally fused to a phenyl ring or a cycloalkane or cycloalkene ring, wherein the heterocyclic ring may optionally contain O, S, or NR.sup.8 in the heterocyclic ring, and may be optionally substituted by R.sup.7 ;R.sup.7 is alkyl of 1-6 carbon atoms, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 结构式II的化合物，其中R和R 1各自独立地为氢，R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5，-COR 5，-CN ，-NO 2，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R4是氢，烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; 各自独立地是5-7元饱和的，不饱和的或部分不饱和的杂环基，其任选地与苯环或环烷烃或环烯烃稠合，其中杂环可以任选地含有O，S或 NR8在杂环中，并且可以任选地被R 7取代; R7是1-6个碳原子的烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6 ，或Ar; R 8是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。
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6.发明授权
公开(公告)号：US4808612A
公开(公告)日：1989-02-28
申请号：US47970
申请日：1987-05-07
IPC分类号： A61K31/445 , A61K31/495 , A61K31/535 , A61K31/44
CPC分类号： A61K31/445 , A61K31/495 , A61K31/535
摘要： There is disclosed a method for the treatment of inflammatory conditions and of collegenase-induced tissue destruction which comprises the administration of a therapeutically effective amount of a compound of the formula ##STR1## wherein R.sup.1 is phenyl or naphthyl, or phenyl or naphthyl substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.2, N(R.sup.2).sub.2, CON(R.sup.2).sub.2, SO.sub.3 R.sup.2, SO.sub.2 N(R.sup.2).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano nitro or trifluoromethyl;R.sup.2 is hydrogen, lower alkyl or phenyl;R.sup.3 is halo, morpholino, 4-methylpiperazino R.sup.4 NNHR.sup.5, NR.sup.4 R.sup.5, OR.sup.5, SR.sup.5, ##STR2## R.sup.4 is hydrogen or lower alkyl; R.sup.5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; andR.sup.6 and R.sup.7 are each independently, hydrogen, halo, nitro, lower alkoxy, lower alkyl, cyano, trifluoromethyl, phenyl, carboxy or lower alkoxycarbonyl;which compounds, by virtue of their ability to inhibit interleukin 1, are useful as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction, and are also intermediates in the preparation of other compounds which possess identical activities.
摘要翻译： 公开了一种治疗炎性病症和共促酶组织破坏的方法，其包括施用治疗有效量的下式化合物，其中R 1是苯基或萘基，或被卤素取代的苯基或萘基 ，低级烷基羰基，苯甲酰基，羧基，低级烷氧基羰基，OR2，N（R2）2，CON（R2）2，SO3R2，SO2N（R2）2，苯基磺酰基，低级烷基磺酰基，氰基硝基或三氟甲基; R2是氢，低级烷基或苯基; R3为卤素，吗啉代，4-甲基哌嗪基，R4NNHR5，NR4R5，OR5，SR5，R4NCH2CH2OCH3，SCH2CH2CH2NH2或+ TR4为氢或低级烷基; R5是氢，低级烷基，低级烷酰基，低级环烷基或苯基; 氰基，三氟甲基，苯基，羧基或低级烷氧基羰基; R 6和R 7各自独立地为氢，卤素，硝基，低级烷氧基，低级烷基，氰基， 这些化合物由于其抑制白细胞介素1的能力，可用作抗炎剂和治疗涉及酶组织破坏的疾病状态，并且也是制备具有相同活性的其它化合物的中间体。
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公开(公告)号：US4719302A
公开(公告)日：1988-01-12
申请号：US25316
申请日：1987-03-13
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： There are disclosed compounds having the formula ##STR1## wherein R is hydrogen or lower alkyl;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, phenyl or any of the foregoing substituted with halo;R.sup.2 is hydrogen, carboxy or lower alkoxy carbonyl; andR.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or any of the foregoing substituted with carboxy, methoxycarbonyl, hydroxy, amino, dilower alkyl amino, cyano, nitro or lower alkoxy;and their use as antifungal agents.
摘要翻译： 公开了具有式“IMAGE”的化合物，其中R是氢或低级烷基; R 1是氢，低级烷基，低级烯基，低级炔基，苯基或被卤素取代的任何一个; R2是氢，羧基或低级烷氧基羰基; 低级烷基，低级烯基，低级炔基或被羧基，甲氧基羰基，羟基，氨基，二元烷基氨基，氰基，硝基或低级烷氧基取代的任何前述基团。 并将其用作抗真菌剂。
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8.发明授权C-3' acylaminooxy-7-[(2-aminothiazol-4-yl)-.alpha.-(substituted-oximino)acety l]cephalosporin derivatives 失效C-3'酰氨基氧基-7 - [（2-氨基噻唑-4-基）-α-（取代肟基）乙酰基]头孢菌素衍生物
公开(公告)号：US4692517A
公开(公告)日：1987-09-08
申请号：US842123
申请日：1986-03-20
IPC分类号： C07D501/34
CPC分类号： C07D501/34
摘要： There are disclosed novel antibacterial compounds having the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo lower alkyl, aryl of 6-12 carbon atoms, all the said foregoing groups being optionally substituted with carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hydroxy, lower alkoxy, phenoxy, carbamoyl, lower alkyl carbonyl, benzoyl, cyano, nitro, formamido, lower alkanoylamino or benzamido;R.sup.1 is hydrogen, lower alkyl or an alkali metal cation;A is lower alkoxy, lower alkenoxy, lower alkynoxy, aryloxy of 6-12 carbon atoms, di-lower alkyl substituted amino, di-lower alkenyl substituted amino, di-lower alkynyl substituted amino, di-aryl of 6-12 carbon atoms substituted amino, lower alkyl, lower alkenyl, lower alkynyl, aryl of 6-12 carbon atoms.
摘要翻译： 公开了具有式“IMAGE”的新型抗菌化合物，其中R是氢，低级烷基，低级烯基，低级炔基，环低级烷基，6-12个碳原子的芳基，所有上述基团任选被羧基取代，低级 烷氧基羰基，苯氧基羰基，氨基，一或二低级烷基取代的氨基，羟基，低级烷氧基，苯氧基，氨基甲酰基，低级烷基羰基，苯甲酰基，氰基，硝基，甲酰氨基，低级烷酰氨基或苯甲酰氨基。 R1是氢，低级烷基或碱金属阳离子; A为6-12个碳原子的低级烷氧基，低级链烯氧基，低级炔氧基，芳氧基，二低级烷基取代氨基，二低级烯基取代氨基，二低级炔基取代氨基，取代6-12个碳原子的二芳基 氨基，低级烷基，低级烯基，低级炔基，6-12个碳原子的芳基。
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9.发明授权Beta-sulfonamide hydroxamic acid inhibitors of tace/matrix metalloproteinase 失效锥形/基质金属蛋白酶的β-磺酰胺异羟肟酸抑制剂公开(公告)号：US07595327B2
公开(公告)日：2009-09-29
申请号：US11377886
申请日：2006-03-16
申请人： Jeremy I. Levin , Zhong Li , George Diamantidis , Frank E. Lovering , Weiheng Wang , Jeffrey S. Condon , Yang-I Lin , Jerauld S. Skotnicki , Kaapjoo Park
发明人： Jeremy I. Levin , Zhong Li , George Diamantidis , Frank E. Lovering , Weiheng Wang , Jeffrey S. Condon , Yang-I Lin , Jerauld S. Skotnicki , Kaapjoo Park
IPC分类号： A61K31/44 , C07D453/02
CPC分类号： C07D215/04 , C07D235/12 , C07D249/18 , C07D271/12 , C07D401/12 , C07D405/12
摘要： This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-α, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, osteoarthritis etc), tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection, ankylosing spondylitis, psoriasis, sepsis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, asthma, idiopathic pulmonary fibrosis, vasculitis, systemic lupus erythematosus, irritable bowel syndrome, acute coronary syndrome, hepatitis C, cachexia, COPD, stroke or type 2 diabetes, and for alleviation of symptoms thereof. The invention further provides methods for use of the compounds.
摘要翻译： 本发明提供具有以下结构的式I化合物：其可用于治疗由TNF-α介导的疾病或病症，例如关节炎（类风湿性关节炎（RA），幼年型RA，牛皮癣关节炎，骨关节炎等），肿瘤转移，组织 溃疡，异常伤口愈合，牙周病，骨病，糖尿病（胰岛素抵抗）和HIV感染，强直性脊柱炎，牛皮癣，败血症，多发性硬化，克罗恩病，退行性软骨损失，哮喘，特发性肺纤维化，血管炎，系统性红斑狼疮， 肠易激综合征，急性冠状动脉综合征，丙型肝炎，恶病质，COPD，中风或2型糖尿病，以及缓解其症状。 本发明还提供了使用该化合物的方法。
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公开(公告)号：US5463048A
公开(公告)日：1995-10-31
申请号：US259763
申请日：1994-06-14
IPC分类号： A61K31/435 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/395 , C07D498/16
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 结构
的化合物，其中R和R 1各自独立地为氢，或者R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5，-COR 5，-CN，-NO 2 ，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R 4是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-NO 2，卤素，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。
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