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    Mycophenolic acid derivatives in the treatment of rheumatoid arthritis
    3.
    发明授权
    Mycophenolic acid derivatives in the treatment of rheumatoid arthritis 失效
    霉酚酸衍生物治疗类风湿关节炎

    公开(公告)号：US4959387A

    公开(公告)日：1990-09-25

    申请号：US125027

    申请日：1987-11-24

    申请人： Peter H. Nelson ,  Anthony C. Allison ,  Elsie M. Eugui ,  Joseph M. Muchowski

    发明人： Peter H. Nelson ,  Anthony C. Allison ,  Elsie M. Eugui ,  Joseph M. Muchowski

    IPC分类号： C07D307/88

    CPC分类号： C07D307/88

    摘要： A method of treating rheumatoid arthritis which method comprises administering to a mammal in need of such treatment a therapeutically effective amount of a compound of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein: A is oxygen or sulfur;R.sup.1 is selected from the group consisting of H, ##STR2## in which Y is oxygen or sulfur:R.sup.2 is alkyl, haloalkyl or --NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are independently H, alkyl, haloalkyl, cycloalkyl, phenyl optionally monosubstituted with halogen, hydroxy, carboxy, chlorocarbonyl, nitro, cyano, phenyl, alkyl, acyl, alkoxycarbonyl, acylamino, dialkylamino or dialkylaminoethoxycarbonyl, phenyl optionally disubstituted with hydroxy, carboxy, nitro or alkyl, or benzyl optionally substituted with dialkylamino;n is an integer from 0-6;R.sup.3 is H alkyl or a pharmaceutically acceptable cation;Q and R are independently H or --CO.sub.2 R.sup.3 ; andZ is selected from the group consisting of ##STR3## in which X is oxygen or sulfur,R.sup.7 is H, alkyl, alkenyl, cycloalkyl, optionally substituted phenyl, optionally substituted benzyl or a pharmaceutically acceptable cation; andR.sup.8 and R.sup.9 are independently H, alkyl or cycloalkyl, or R.sup.8 and R.sup.9 taken together are --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --(CH.sub.2).sub.2 O(CH.sub.2).sub.2 --;with the proviso that R.sup.1 and R.sup.7 cannot both be H if X and A are oxygen.

    摘要翻译： 治疗类风湿性关节炎的方法，该方法包括向需要这种治疗的哺乳动物施用治疗有效量的下式化合物及其药学上可接受的盐，其中：A为氧或硫; R1选自H，其中Y是氧或硫的R 2是烷基，卤代烷基或-NR 4 R 5，其中R 4和R 5独立地是H，烷基，卤代烷基，环烷基，任选被卤素单取代的苯基， 羟基，羧基，氯代羰基，硝基，氰基，苯基，烷基，酰基，烷氧基羰基，酰基氨基，二烷基氨基或二烷基氨基乙氧基羰基，任选被羟基，羧基，硝基或烷基二取代的苯基或任选被二烷基氨基取代的苄基; n是0-6的整数; R3是H烷基或药学上可接受的阳离子; Q和R独立地是H或-CO 2 R 3; Z选自CH 2 OH，CHO，CN，1H-四唑基，其中X是氧或硫，R7是H，烷基，烯基，环烷基，任选取代的苯基，任选取代的苄基或药学上 可接受的阳离子 并且R 8和R 9独立地为H，烷基或环烷基，或者R 8和R 9一起为 - （CH 2）4 - ， - （CH 2）5 - 或 - （CH 2）2 O（CH 2）2 - 条件是如果X和A是氧，则R1和R7不能都是H。

    Hypotensive benzoxathiole pyrrolidines
    7.
    发明授权
    Hypotensive benzoxathiole pyrrolidines 失效
    低血压苯并硫代吡咯烷

    公开(公告)号：US4548951A

    公开(公告)日：1985-10-22

    申请号：US487335

    申请日：1983-04-21

    申请人： Joseph M. Muchowski ,  Jack Ackrell

    发明人： Joseph M. Muchowski ,  Jack Ackrell

    IPC分类号： C07D295/108 ,  C07D317/54 ,  C07D317/58 ,  C07D327/04 ,  C07D411/06 ,  A61K31/39

    CPC分类号： C07D295/108 ,  C07C309/00 ,  C07C323/00 ,  C07D317/54 ,  C07D317/58 ,  C07D327/04 ,  C07D411/06

    摘要： Compounds of the formula ##STR1## and the pharmaceutically acceptable, nontoxic, acid addition salts thereof, whereinR.sub.1 and R.sub.2 are each independently --H, lower alkyl, or cycloalkyl, with the proviso that R.sub.1 and R.sub.2 cannot both be --H or cycloalkyl at the same time;R.sub.1 and R.sub.2 taken together are cycloalkyl of 4-7 carbons;n is 0 or 1;X is (CH.sub.2).sub.2, CH.dbd.CH, or C.tbd.C;Y is independently selected from the group of --H, --Fl, --Br, --Cl, lower alkyl, and --OR.sub.3 ; wherein R.sub.3 is --H or lower alkyl; anda is 1 or 2, ortwo Y's taken together are --OCH.sub.2 O--;are useful as regulators of the cardiovascular system, particularly as hypotensive agents.

    摘要翻译： 式IMA的化合物及其药学上可接受的无毒的酸加成盐，其中R 1和R 2各自独立地为-H，低级烷基或环烷基，条件是R 1和R 2不能均为-H或环烷基 同一时间; R 1和R 2一起是4-7个碳的环烷基; n为0或1; X是（CH 2）2，CH = CH或C 3 F 3; Y独立地选自-H，-F 1，Br，-Cl，低级烷基和-OR 3; 其中R3是-H或低级烷基; 和a为1或2，或两个Y一起为-OCH 2 O-; 作为心血管系统的调节剂是有用的，特别是作为降血压剂。

    11.alpha.-Hydroxymethyl prostaglandins
    8.
    发明授权
    11.alpha.-Hydroxymethyl prostaglandins 失效
    11 {60-羟丙基前列腺素

    公开(公告)号：US3931282A

    公开(公告)日：1976-01-06

    申请号：US444689

    申请日：1974-02-21

    申请人： Joseph M. Muchowski ,  Angel Guzman

    发明人： Joseph M. Muchowski ,  Angel Guzman

    IPC分类号： C07C405/00 ,  C07D309/08 ,  C12P31/00 ,  C07C61/38 ,  C07C69/74

    CPC分类号： C07C405/00 ,  C07C405/0041 ,  C07D309/08 ,  C12P31/00

    摘要： Novel process for the preparation of 11.alpha.-hydroxymethyl derivatives of natural (8R-) and racemic 9-keto-15.alpha.-hydroxy- and 9,15.alpha.-dihydroxy-prosta-5-cis,13-trans-dienoic and prost-13-transenoic acids, and the novel 15-methyl and ethyl substituted derivatives thereof, as well as the esters of the primary and secondary hydroxy groups and the non-toxic, pharmaceutically acceptable salts of the novel compounds.

    摘要翻译： 用于制备天然（8R-）和外消旋9-酮-15α-羟基和9,15α-二羟基 - 前列腺-5-顺式，13-反式二烯酸和前列腺素的11α-羟甲基衍生物的新方法， 13-变态酸及其新型的15-甲基和乙基取代的衍生物，以及该新化合物的一级和二级羟基酯和无毒的药学上可接受的盐的酯。