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21. 发明授权

US5489680A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5489680A
公开(公告)日：1996-02-06
申请号：US284765
申请日：1994-08-02
申请人： Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
发明人： Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
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。

22. 发明授权

US5489595A Carbamates of rapamycin 失效
公开(公告)号：US5489595A
公开(公告)日：1996-02-06
申请号：US449499
申请日：1995-05-24
申请人： Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
发明人： Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
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.

23. 发明授权

US5486522A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5486522A
公开(公告)日：1996-01-23
申请号：US448709
申请日：1995-05-24
申请人： Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
发明人： Amedeo A. Failli , Oleg I. Bleyman , Wenling Kao , Magid A. Abou-Gharbia
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。

24. 发明授权

US5480989A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5480989A
公开(公告)日：1996-01-02
申请号：US297663
申请日：1994-09-01
申请人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
发明人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
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,R.sup.3, R.sup.4, R.sup.5, R.sup.6, B,R.sup.7 and R.sup.8,R.sup.9 and R.sup.10,are each defined in the specification or a pharmaceutically acceptable salt their, of which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：结构的化合物，其中R1和R2，R3，R4，R5，R6，B，R7和R8，R9和R10各自在说明书中定义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。

25. 发明授权

US5378836A Rapamycin oximes and hydrazones 失效
标题翻译：雷帕霉素肟和腙
公开(公告)号：US5378836A
公开(公告)日：1995-01-03
申请号：US134224
申请日：1993-10-08
申请人： Wenling Kao , Robert L. Vogel , Magid A. Abou-Gharbia , Craig E. Caufield
发明人： Wenling Kao , Robert L. Vogel , Magid A. Abou-Gharbia , Craig E. Caufield
IPC分类号： C07D498/22 , A61K31/395 , C07D491/06
CPC分类号： C07D498/22
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH.sub.a --{{(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p }.sub.q --B}.sub.r ; --SO.sub.2 R.sup.7 ; --SO.sub.3 H; --CHR.sup.8 O(CH.sub.2).sub.t R.sup.9 ; or ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.10, --SR.sup.10, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.10, --CO.sub.2 R.sup.10, --CONHR.sup.10, --SO.sub.2 R.sup.10, --OSO.sub.3 R.sup.10, --NR.sup.10 R.sup.11, --NHCOR.sup.10, --NHSO.sub.2 R.sup.10, or Ar;X is .dbd.NOR.sup.12 or .dbd.NNR.sup.12 R.sup.13 ;Y is O, .dbd.NOR.sup.12, or .dbd.NNR.sup.12 R.sup.13 ;R.sup.7, R.sup.12, and R.sup.13 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, arylalkyl;R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;A is --CH.sub.2 --, --NR.sup.8 --, --O--, --S--, --SO--, --SO.sub.2 --, --PR.sup.8 --, --CO--, --NHCO--, --NHSO--, or --P(O)(R.sup.8)--;Ar is aryl which may be optionally mono-, di-, or tri- substituted; ##STR3## is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted;a=0-1;m=0-6;n=0-6;p=0-1;q=0-1;r=1-2; andt=1-4;wherein R.sup.3, R.sup.4, R.sup.5, R.sup.6, A, B, m, n, p, and q are independent in each of the --CON--{{(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p }.sub.q --B}.sub.r subunits when r=2;with the proviso that R.sup.1 and R.sup.2 are not both hydrogen, and further provided that if r=2, then a=0, and if r=1, then a=1;or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：其中R1和R2各自独立地为氢，-CONHa - {{（CR3R4）m（-A-（CR5R6）n）p} q-B} r的结构化合物。 -SO2R7; -SO 3 H; -CHR 8 O（CH 2）t R 9; 或R 3，R 4，R 5，R 6和B各自独立地为氢，烷基，烯基，炔基，羟烷基，烷氧基烷基，烷硫基烷基，烷基氨基烷基，二烷基氨基烷基，芳烷基，环烷基，-OR 10，-SR 10，卤素， CN，-NO 2，-CF 3，-COR 10，-CO 2 R 10，-CONHR 10，-SO 2 R 10，-OSO 3 R 10，-NR 10 R 11，-NHCOR 10，-NHSO 2 R 10或Ar; X = NOR12或= NNR12R13; Y为O，= NOR12或= NNR12R13; R 7，R 12和R 13各自独立地为氢，烷基，烯基，炔基，芳基烷基; R 8，R 9，R 10和R 11各自独立地为氢，烷基，芳基烷基，烯基，炔基，羟烷基，烷氧基烷基，烷硫基烷基，烷基氨基烷基，二烷基氨基烷基，环烷基或Ar; A是-CH 2 - ， - NR 8 - ， - O - ， - S - ， - SO - ， - SO 2 - ， - PR 8 - ， - CO-，-NHCO-，-NHSO-或-P ） - ; Ar是可任选被单，二或三取代的芳基; 可以是饱和的，不饱和的或部分不饱和的，可以是任选的单，二或三取代的含氮杂环; a = 0-1; m = 0-6; n = 0-6; p = 0-1; q = 0-1; r = 1-2; 和t = 1-4; 其中R3，R4，R5，R6，A，B，m，n，p和q在-CON - {{（CR3R4）m（-A-（CR5R6）n）p} qB} 当r = 2时，条件是R1和R2不是氢，并且进一步规定如果r = 2，则a = 0，并且如果r = 1，那么a = 1; 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。

26. 发明授权

US06200963B1 Aryl sulfonic acids as FSH antagonists 失效
标题翻译：芳基磺酸作为FSH拮抗剂
公开(公告)号：US06200963B1
公开(公告)日：2001-03-13
申请号：US09537472
申请日：2000-03-24
申请人： Jay E. Wrobel , John F. Rogers , Wenling Kao
发明人： Jay E. Wrobel , John F. Rogers , Wenling Kao
IPC分类号： A61K31655
CPC分类号： C07D251/50 , A61K31/655 , C07C309/51
摘要： wherein: R1 is a moiety selected from: R2 is CH2CH2CONH2 or CH2CH2OH; R3 and R4 are independent substituents selected from the group including H, —N(CH3)2, or —OCH3; or pharmaceutically acceptable salts thereof.
摘要翻译：其中：R 1是选自：R 2是CH 2 CH 2 CONH 2或CH 2 CH 2 OH的部分; R 3和R 4是选自包括H，-N（CH 3）2或-OCH 3的独立取代基;或其药学上可接受的盐。

27. 发明授权

US5349060A Rapamycin 31-ester with N,N-dimethylglycine derivatives useful as immunosuppressive agents 失效
标题翻译：雷帕霉素31-酯与可用作免疫抑制剂的N，N-二甲基甘氨酸衍生物
公开(公告)号：US5349060A
公开(公告)日：1994-09-20
申请号：US58918
申请日：1993-05-06
申请人： Wenling Kao , Robert L. Vogel
发明人： Wenling Kao , Robert L. Vogel
IPC分类号： C07D498/18 , C07D491/16 , A61K31/395
CPC分类号： C07D498/18
摘要： A derivative of rapamycin of general formula (1) and (2) ##STR1## wherein ##STR2## or hydrogen; R.sup.2 =hydrogen, or lower alkyl having 1 to 6 carbon atoms; ##STR3## wherein X=hydrogen, lower alkyl having 1 to 6 carbon atoms, --CF.sub.3, --NO.sub.2, --OR.sup.2, NR.sup.2, SR.sup.2, or halogen; R.sup.4 =lower alkyl, alkenyl or alkynyl having 1 to 6 carbon atoms or an aromatic or heterocyclic moiety selected from the group consisting of phenyl, naphthyl, thiophenyl and quinolinyl;Y-=halide, methanesulfonate, toluene sulfonate or maleate; andZ=oxygen or OH and H.which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：（1）和（2）的雷帕霉素的衍生物其中图像或氢; R2 =氢或具有1至6个碳原子的低级烷基; 其中X =氢，具有1至6个碳原子的低级烷基，-CF 3，-NO 2，-OR 2，NR 2，SR 2或卤素; R4 =具有1至6个碳原子的低级烷基，烯基或炔基或选自苯基，萘基，噻吩基和喹啉基的芳族或杂环部分; Y- =卤化物，甲磺酸盐，甲苯磺酸盐或马来酸盐; Z =氧或OH和H.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，自身免疫性疾病和炎症疾病。

28. 发明授权

US5262423A Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosuppressive and antifungal agents 失效
标题翻译：雷帕霉素芳基羰基和烷氧基羰基氨基甲酸酯作为免疫抑制和抗真菌剂
公开(公告)号：US5262423A
公开(公告)日：1993-11-16
申请号：US968115
申请日：1992-10-29
申请人： Wenling Kao
发明人： Wenling Kao
IPC分类号： A61K31/435 , A61K31/436 , A61P29/00 , A61P31/10 , A61P37/06 , C07D498/18 , C07D498/16 , A61K31/395
CPC分类号： C07D498/18
摘要： N-arylcarbonyl and N-alkylcarbonyl carbamates of rapamycin of the formula shown below wherein ##STR1## R.sup.1 and R.sup.2 are both ##STR2## and where A is lower alkoxy or aryl or heteroaryl, R.sup.3 is H or methyl and R.sup.4 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl possess immunosuppressive and/or antifungal and/or antitumor and/or antiinflammatory activity in vitro and/or inhibit thymocyte proliferation in vivo. These compounds are thus expected to be useful in the treatment of transplantation rejection, autoimmune diseases, fungal infections, cancer, and diseases of inflammation.
摘要翻译：下式表示的雷帕霉素的N-芳基羰基和N-烷基羰基氨基甲酸酯，其中R 1和R 2均为“IMAGE”，其中A为低级烷氧基或芳基或杂芳基，R 3为H或甲基且R 4为C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基在体内具有免疫抑制和/或抗真菌和/或抗肿瘤和/或抗炎活性和/或抑制体内胸腺细胞增殖。因此预期这些化合物可用于治疗移植排斥反应，自身免疫性疾病，真菌感染，癌症和炎症疾病。

29. 发明授权

US4170709A 16-Keto PGE.sub.2 methyl esters 失效
标题翻译： 16-Keto PGE {HD 2 {B methyl esters
公开(公告)号：US4170709A
公开(公告)日：1979-10-09
申请号：US838614
申请日：1977-10-03
申请人： Wenling Kao , Richard W. Rees
发明人： Wenling Kao , Richard W. Rees
IPC分类号： C07C405/00 , C07D339/08 , C07C177/00
CPC分类号： C07D339/08 , C07C405/00
摘要： The preparation of the methyl esters of 16-keto prostaglandin E.sub.2 and 15-epi-16-keto prostaglandin E.sub.2 is described. The compounds have hypotensive activity.
摘要翻译：描述了16-酮前列腺素E2和15-epi-16-酮前列腺素E2的甲基酯的制备。这些化合物具有降血压活性。

30. 发明授权

US4086269A 11-Deoxy-15-substituted prostaglandins 失效
标题翻译： 11-脱氧-15-取代的前列腺素
公开(公告)号：US4086269A
公开(公告)日：1978-04-25
申请号：US714734
申请日：1976-08-16
申请人： Donald P. Strike , Wenling Kao
发明人： Donald P. Strike , Wenling Kao
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Processes for the total synthesis of dl-11-deoxy-15-substituted prostaglandins, novel intermediates therefore, certain novel final products, as well as optical resolutions of the final products are disclosed.The final products are bronchodilators.
摘要翻译：公开了dl-11-脱氧-15-取代的前列腺素的全合成方法，因此新颖的中间体，某些新的最终产物以及最终产品的光学分辨率。

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