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公开(公告)号：US5486523A
公开(公告)日：1996-01-23
申请号：US449444
申请日：1995-05-24
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.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.6 R.sup.7).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, --OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12, and R.sup.13 are each, independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each, independently, hydrogen or alkyl;R.sup.17 is ##STR3## or --C.ident.C--R.sup.21 ; R.sup.18, R.sup.19, R.sup.20, and R.sup.21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, dio, or tri-substituted; ##STR4## is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ring may optionally contain NR.sup.22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyl, arylalkyl, halogen, --CF.sub.3, --OR.sup.14, or --CO.sub.2 R.sup.10 ;R.sup.22 is hydrogen, alkyl, or arylalkyl;m=0-6;n=1-6;p=0-6; andr=1-6with the proviso that R.sup.1 and R.sup.2 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 1和R 2各自独立地为氢，-CONR 3（CR 4 R 5）m（CR 6 R 7）n（CR 8 R 9）pNR 10 R 11或者或者-CONR 3 R 13; R3是氢，烷基或芳基烷基; R 4，R 5，R 8和R 9各自独立地为氢，烷基，-OH，-CF 3或-F; R6是氢或-OR13; R7是氢或烷基; R 10是氢，烷基或芳基烷基; R 11，R 12和R 13各自独立地为 - （CR 15 R 16）r R 17; R 14为氢，1-6个碳原子的烷基，三（烷基）甲硅烷基，三（烷基）甲硅烷基乙基，三苯基甲基，苄基，烷氧基甲基，三（烷基）甲基乙氧基甲基或四氢吡喃基; R 15和R 16各自独立地为氢或烷基; R17是
或-C = C-R21; R 18，R 19，R 20和R 21各自独立地为氢，烷基，卤素或苯基，其中苯基可以是任选的单，二取代或三取代的; 含有至少2个环氮的5-7元饱和或部分不饱和杂环基，其中该杂环可以在杂环中任意含有NR 22，并且环碳可任选地被烷基，芳基烷基，卤素， -CF 3，-OR 14或-CO 2 R 10; R 22是氢，烷基或芳基烷基; m = 0-6; n = 1-6; p = 0-6; 并且r = 1-6，条件是R 1和R 2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：US5486524A
公开(公告)日：1996-01-23
申请号：US449166
申请日：1995-05-24
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## where the substituents are defined in the specification.
摘要翻译： 其中取代基在说明书中定义的结构式II的化合物。
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公开(公告)号：US5484791A
公开(公告)日：1996-01-16
申请号：US449443
申请日：1995-05-24
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.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NR.sup.5 R.sup.6, --CN, --CF.sub.3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 is ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; andm=1-6;with the proviso that R.sup.1 and R.sup.2 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 1和R 2各自独立地为氢或-CONH-O-（CR 3 R 4）m Z; R 3和R 4各自独立地为氢，烷基，环烷基，-CF 3或F; Z是氢，烷基，-OR 5，-SR 5，-NR 5 R 6，-CN，-CF 3，-OAr，-Ar或R 7; R 5和R 6各自独立地为氢，烷基，芳基烷基，烯基，炔基，烷氧基烷基，烷基硫代烷基，烷基氨基烷基，二烷基氨基烷基，环烷基或Ar; R7是
或-C 3BOND C-R11; R 8，R 9，R 10和R 11各自独立地为氢，1-6个碳原子的烷基，卤素或苯基，其中苯基可以是任选的单，二或三取代; Ar是可以任选被单，二或三取代的芳基; m = 1-6; 条件是R1和R2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：US5559227A
公开(公告)日：1996-09-24
申请号：US449593
申请日：1995-05-24
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.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.6 R.sup.7).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, --OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12 and R.sup.13 are each, independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each, independently, hydrogen or alkyl;R.sup.17 is ##STR3## or --C.tbd.C--R.sup.21 ; R.sup.18, R.sup.19, R.sup.20, and R.sup.21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; ##STR4## is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ting may optionally contain NR.sup.22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyl, arylalkyl, halogen, --CF.sub.3, --OR.sup.14, or --CO.sub.2 R.sup.10 ;R.sup.22 is hydrogen, alkyl, or arylalkyl;m=0-6;n=1-6;p=0-6; andr=1-6with the proviso that R.sup.1 and R.sup.2 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 1和R 2各自独立地为氢，-CONR 3（CR 4 R 5）m（CR 6 R 7）n（CR 8 R 9）pNR 10 R 11或者或者-CONR 3 R 13; R3是氢，烷基或芳基烷基; R 4，R 5，R 8和R 9各自独立地为氢，烷基，-OH，-CF 3或-F; R6是氢或-OR13; R7是氢或烷基; R 10是氢，烷基或芳基烷基; R 11，R 12和R 13各自独立地为 - （CR 15 R 16）r R 17; R 14为氢，1-6个碳原子的烷基，三（烷基）甲硅烷基，三（烷基）甲硅烷基乙基，三苯基甲基，苄基，烷氧基甲基，三（烷基）甲基乙氧基甲基或四氢吡喃基; R 15和R 16各自独立地为氢或烷基; R17是
或-C 3BOND C-R21; R 18，R 19，R 20和R 21各自独立地为氢，烷基，卤素或苯基，其中苯基可以是任选的单，二或三取代; 含有至少2个环氮原子的5-7元饱和或部分不饱和杂环基，其中该杂环可以任意地含有杂环中的NR 22，并且该环碳可任选地被烷基，芳烷基，卤素， -CF 3，-OR 14或-CO 2 R 10; R 22是氢，烷基或芳基烷基; m = 0-6; n = 1-6; p = 0-6; 并且r = 1-6，条件是R 1和R 2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：US5550133A
公开(公告)日：1996-08-27
申请号：US448869
申请日：1995-05-24
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 the variables are defined in the specification, with the proviso that R.sup.1 and R.sup.2 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，其中变量在说明书中定义，条件是R 1和R 2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 抗肿瘤药。
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公开(公告)号：US5484790A
公开(公告)日：1996-01-16
申请号：US448812
申请日：1995-05-24
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.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NR.sup.5 R.sup.6, --CN, --CF.sub.3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 is ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; andm=1-6;with the proviso that R.sup.1 and R.sup.2 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：US5480988A
公开(公告)日：1996-01-02
申请号：US284764
申请日：1994-08-02
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.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.4 R.sup.5).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## --R.sup.12, or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, p--OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12, and R.sup.13 are each independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, Tri-(alkyl)silyethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each independently, hydrogen or alkyl; ##STR3## R.sup.18, R.sup.19, R.sup.20, and R.sup.21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; ##STR4## is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ring may optionally contain NR.sup.22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyll, arylalkyl, halogen, --CF.sub.3, ---OR.sup.14, or --CO.sub.2 R.sup.10 ;R.sup.22 is hydrogen, alkyl, or arylalkyl;m=0-6;n=1-6;p=0-6; andr=1-6with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, anti inflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译： 结构式II的化合物，其中R 1和R 2各自独立地为氢，-CONR 3（CR 4 R 5）m（CR 4 R 5）n（CR 8 R 9）pNR 10 R 11或CONR 3（CR 4 R 5）m（CR 6 R 7）n（CR 8 R 9）pNR 10 R 11， 或
-R12或-CONR3R13; R3是氢，烷基或芳基烷基; R 4，R 5，R 8和R 9各自独立地为氢，烷基，p-OH，-CF 3或-F; R6是氢或-OR13; R7是氢或烷基; R 10是氢，烷基或芳基烷基; R 11，R 12和R 13各自独立地为 - （CR 15 R 16）r R 17; R 14为氢，1-6个碳原子的烷基，三（烷基）甲硅烷基，三（烷基）甲硅烷基，三苯基甲基，苄基，烷氧基甲基，三（烷基）甲基乙氧基甲基或四氢吡喃基; R 15和R 16各自独立地为氢或烷基; R18，R19，R20和R21各自独立地为氢，烷基，卤素或苯基，其中苯基可以是任选的单，二或三取代; 含有至少2个环氮原子的5-7元饱和或部分不饱和杂环基，其中该杂环可以在杂环中任选地含有NR 22，并且该环碳可任选地被烷基，芳烷基，卤素， -CF 3，-OR 14或-CO 2 R 10; R 22是氢，烷基或芳基烷基; m = 0-6; n = 1-6; p = 0-6; 并且r = 1-6，条件是R 1和R 2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：US5504204A
公开(公告)日：1996-04-02
申请号：US449453
申请日：1995-05-24
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## or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent. The substituents are defined elsewhere in the specification.
摘要翻译： 可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂的结构式II的化合物或其药学上可接受的盐。 取代基在本说明书的其他地方定义。
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公开(公告)号：US5489680A
公开(公告)日：1996-02-06
申请号：US284765
申请日：1994-08-02
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.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NRSR.sup.6, --CN, --CF3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; and m=1-6;with the proviso that R.sup.1 and R.sup.2 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 1和R 2各自独立地为氢或-CONH-O-（CR 3 R 4）m Z; R 3和R 4各自独立地为氢，烷基，环烷基，-CF 3或F; Z是氢，烷基，-OR5，-SR5，-NRSR6，-CN，-CF3，-OAr，-Ar或R7; R 5和R 6各自独立地为氢，烷基，芳基烷基，烯基，炔基，烷氧基烷基，烷基硫代烷基，烷基氨基烷基，二烷基氨基烷基，环烷基或Ar; R7
或-C 3BOND C-R11; R 8，R 9，R 10和R 11各自独立地为氢，1-6个碳原子的烷基，卤素或苯基，其中苯基可以是任选的单，二或三取代; Ar是可以任选被单，二或三取代的芳基; m = 1-6; 条件是R1和R2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：US5489595A
公开(公告)日：1996-02-06
申请号：US449499
申请日：1995-05-24
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.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NR.sup.5 R.sup.6, --CN, --CF.sub.3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 is ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; andm=1-6;with the proviso that R.sup.1 and R.sup.2 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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