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公开(公告)号：US5880250A
公开(公告)日：1999-03-09
申请号：US689939
申请日：1996-08-16
申请人： Tyler Housel , Ira S. Katuran , Rocco Burgo , Oleg I. Bleyman
发明人： Tyler Housel , Ira S. Katuran , Rocco Burgo , Oleg I. Bleyman
CPC分类号： C08G63/02 , C08G18/0823 , C08G18/12 , C08G18/4263 , C08G2101/00 , C08G2101/0008
摘要： Polymeric acid functional polyols are provided which are the reaction product of at least one hydroxyl-terminated polymer and a nonaromatic polyanhydride. Polymeric acid functional polyols are also provided which are the esterification reaction product of a first component which is at least one of an aliphatic dicarboxylic acid, a polyol and mixtures thereof and a second component which has at least two unhindered functional groups and at least one hindered carboxylic acid functional group. Methods of making such polymeric acid functional polyols by reacting a hydroxyl-terminated polymer and a nonaromatic dianhydride or by the esterification reaction of the first and second component described herein are also included in the invention. Further, hydrophilic polyurethane foams and water borne polyurethanes formed from the reaction of these polymeric acid functional polyols with polyisocyanates are also provided.
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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：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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公开(公告)号：US5486522A
公开(公告)日：1996-01-23
申请号：US448709
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 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 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：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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