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28 条记录 (耗时 0.035 秒)

    4-substituted beta-carbolines and analogs thereof
    1.
    发明授权
    4-substituted beta-carbolines and analogs thereof 失效
    4-取代的β-咔啉及其类似物

    公开(公告)号：US6093723A

    公开(公告)日：2000-07-25

    申请号：US908211

    申请日：1997-08-08

    申请人： Clara K Miao ,  Ian F. Potocki ,  Roger J. Snow ,  Karl D. Hargrave ,  Thomas P. Parks

    发明人： Clara K Miao ,  Ian F. Potocki ,  Roger J. Snow ,  Karl D. Hargrave ,  Thomas P. Parks

    IPC分类号： C07D491/048 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/444 ,  A61P37/02 ,  C07D471/04 ,  C07D495/04 ,  A61K31/44 ,  A61K31/535

    CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444

    摘要： This invention relates to 4-substituted .beta.-carbolines and .beta.-carboline analogs that inhibit Ca.sup.+2 influx and interleukin-2 (IL-2) production. The 4-substituted .beta.-carbolines and .beta.-carboline analogs of this invention are represented by formula (I): ##STR1## wherein Q, n, R, R', R" and R.sub.1 -R.sub.4 are as defined herein. This invention also relates to methods for producing .beta.-carbolines. Because of their selective immunomodulating properties, the compounds and pharmaceutical compositions of this invention are particularly well suited for preventing and treating immune disorders, including autoimmune disease, inflammatory disease, organ transplant rejection and other disorders associated with IL-2 mediated immune response.

    摘要翻译： 本发明涉及抑制Ca + 2流入和白细胞介素-2（IL-2）产生的4-取代的β-咔啉和β-咔啉类似物。 本发明的4-取代的β-咔啉和β-咔啉类似物由式（I）表示：其中Q，n，R，R'，R“和R 1 -R 4如本文所定义。 本发明还涉及生产β-咔啉的方法。 由于其选择性免疫调节特性，本发明的化合物和药物组合物特别适用于预防和治疗包括自身免疫性疾病，炎性疾病，器官移植排斥和与IL-2介导的免疫应答相关的其它病症的免疫疾病。

    Alkylarylketo acids
    3.
    发明授权
    Alkylarylketo acids 失效
    烷基芳基酮酸

    公开(公告)号：US5504244A

    公开(公告)日：1996-04-02

    申请号：US166401

    申请日：1993-12-14

    申请人： Karl D. Hargrave ,  John P. Devlin

    发明人： Karl D. Hargrave ,  John P. Devlin

    IPC分类号： C07C59/76 ,  C07C59/90 ,  C07C205/56 ,  C07C229/42 ,  C07D257/04 ,  C07C69/76

    CPC分类号： C07D257/04 ,  C07C205/56 ,  C07C229/42 ,  C07C59/76 ,  C07C59/90

    摘要： Disclosed are novel alkylarylketocarboxylic acids and 5-substituted tetrazoles represented by the formula ##STR1## wherein Z is aryl or an alkyl of the structure ##STR2## W is a carboxyl moiety or a tetrazole moiety bound to Z at the 5-position of the tetrazole;R.sub.1 is C.sub.4 -C.sub.12 alkyl where Z is aryl and X is oxygen or is C.sub.5 -C.sub.12 alkyl where Z is alkyl and where Z is aryl and X is a bond;R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy, C.sub.1 -C.sub.4 alkoxy, halogen, trihalomethyl, nitro, cyano or C.sub.1 -C.sub.4 acyl;R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl or R.sub.4 and R.sub.6 or R.sub.5 and R.sub.7 can combine to form a carbocyclic ring;X is oxygen, or a bond at the ortho or para position;m is 0, 1 or 2; andn is 0 or 1, and nontoxic, pharmaceutically acceptable addition salts and carboxylic acid esters thereof.

    摘要翻译： 公开了新的烷基芳基酮羧酸和由下式表示的5-取代的四唑：其中Z是芳基或结构的烷基W是羧基部分或在四唑的5位与Z结合的四唑部分 ; R1是C4-C12烷基，其中Z是芳基，X是氧，或者是C5-C12烷基，其中Z是烷基，Z是芳基，X是一个键; R2和R3各自独立地为氢，C1-C4烷基，羟基，C1-C4烷氧基，卤素，三卤甲基，硝基，氰基或C1-C4酰基; R4，R5，R6和R7各自独立地为氢或C1-C4烷基或R4，R6或R5和R7可以结合形成碳环; X是氧，或邻位或对位的键; m为0,1或2; 和n为0或1，以及无毒的药学上可接受的加成盐和羧酸酯。

    Substituted phenylalkyl-(piperazinyl or homopiperazinyl)alkyl thiols and thiocarbamates useful for the treatment of immunological, inflammatory, and allergic disorders
    6.
    发明授权
    Substituted phenylalkyl-(piperazinyl or homopiperazinyl)alkyl thiols and thiocarbamates useful for the treatment of immunological, inflammatory, and allergic disorders 失效
    可用于治疗免疫学，炎症和过敏性疾病的取代的苯基烷基 - （哌嗪基或高哌嗪基）烷基硫醇和硫代氨基甲酸酯

    公开(公告)号：US4722926A

    公开(公告)日：1988-02-02

    申请号：US889106

    申请日：1986-07-23

    申请人： Karl D. Hargrave ,  John P. Devlin ,  Edward A. Barsumian

    发明人： Karl D. Hargrave ,  John P. Devlin ,  Edward A. Barsumian

    IPC分类号： C07D241/04 ,  C07D243/08 ,  C07D295/088 ,  A61K31/33

    CPC分类号： C07D295/088 ,  C07D241/04 ,  C07D243/08

    摘要： Compounds of the formula ##STR1## wherein R is hydrogen or ##STR2## A is alkyl of 1 to 8 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; phenyl; or phenyl mono-, di- or tri-substituted independently with alkyl of 1 to 4 carbon atoms, halogen, trihalomethyl, alkoxy of 1 to 3 carbon atoms, carboxylic acyl of 1 to 3 carbon atoms, carboxyl, (alkoxy of 1 to 3 carbon atoms)carbonyl, nitro, cyano or di(alkyl of 1 to 3 carbon atoms)amino;R.sub.1, R.sub.2 and R.sub.3, are independently hydrogen, halogen, alkyl of 1 to 4 carbon atoms, trihalomethyl, nitro, cyano, di(alkyl of 1 to 4 carbon atoms)amino, (alkoxy of 1 to 4 carbon atoms)carbonyl, alkoxy of 1 to 4 carbon atoms or hydroxyl;R.sub.4 and R.sub.5 are independently hydrogen, alkyl of 1 to 4 carbon atoms, or phenyl;R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are independently hydrogen or methyl;Y is --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --;j is 0 to 1;k and m are independently 0, 1, 2, or 3, their sum being no more than 6 and must be 0 when j is 1;n is 2, 3, or 4, with the proviso that n must be 3 or 4 when R.sub.1 is hydrogen or 2-methyl, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R are each and j, k, and m are each 0, and Y is --CH.sub.2 --;and non-toxic, pharmaceutically acceptable acid addition salts thereof are useful for the treatment of immunological, inflammatory and allergic disorders.

    摘要翻译： 其中R是氢或者A是具有1至8个碳原子的烷基; 3至7个碳原子的环烷基; 苯基; 或独立地具有1至4个碳原子的烷基，卤素，三卤代甲基，1至3个碳原子的烷氧基，1至3个碳原子的羧基酰基，羧基（1至3个的烷氧基） 碳原子）羰基，硝基，氰基或二（1至3个碳原子的烷基）氨基; R1，R2和R3独立地是氢，卤素，1-4个碳原子的烷基，三卤甲基，硝基，氰基，二（1-4个碳原子的烷基）氨基，（1-4个碳原子的烷氧基）羰基，烷氧基 1至4个碳原子或羟基; R4和R5独立地是氢，1-4个碳原子的烷基或苯基; R6，R7，R8和R9独立地是氢或甲基; Y是-CH 2 - 或-CH 2 -CH 2 - ; j为0〜1; k和m独立为0,1,2或3，它们的和不大于6，当j为1时必须为0; n为2,3或4，条件是当R1为氢或2-甲基时，n必须为3或4，R2，R3，R4，R5，R6，R7，R8，R9和R分别为和j， k和m各自为0，Y为-CH 2 - ; 其无毒的药学上可接受的酸加成盐可用于治疗免疫学，炎性和过敏性疾病。