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    Process for the optical resolution of pyranobenzoxadiazole compounds
    2.
    发明授权
    Process for the optical resolution of pyranobenzoxadiazole compounds 失效
    吡喃并苯并恶二唑化合物的光学拆分方法

    公开(公告)号：US5319089A

    公开(公告)日：1994-06-07

    申请号：US780357

    申请日：1991-10-22

    申请人： Hiroo Matsumoto ,  Kiyotomo Seto ,  Ryozo Sakoda

    发明人： Hiroo Matsumoto ,  Kiyotomo Seto ,  Ryozo Sakoda

    IPC分类号： C07D498/04

    CPC分类号： C07D498/04

    摘要： A process for the optical resolution of a pyranobenzoxadiazole compound represented by the formula [(.+-.)I]: ##STR1## which comprises reacting the compound [(.+-.)I] with an optically active carboxylic acid represented by the formula [II]: ##STR2## and separating the diastereomeric salt thus formed is disclosed.

    摘要翻译： 用于光学拆分由式[（+/-）I]表示的吡喃并苯并恶二唑化合物的方法：包括使化合物[（+/-）I]与光学 公开了由式[II]表示的活性羧酸：＆lt; IMAGE＆gt;并分离如此形成的非对映体盐。

    Process for producing alpha-(benzylidene)acetonylphosphonates
    4.
    发明授权
    Process for producing alpha-(benzylidene)acetonylphosphonates 失效
    制备α-（亚苄基）丙酰基膦酸酯的方法

    公开(公告)号：US4879400A

    公开(公告)日：1989-11-07

    申请号：US145042

    申请日：1988-01-19

    申请人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Ryozo Sakoda

    发明人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Ryozo Sakoda

    IPC分类号： C07F9/40 ,  C07F9/6571

    CPC分类号： C07F9/657181 ,  C07F9/4015

    摘要： A process for producing an .alpha.-(benzylidene)acetonylphosphonate of the formula: ##STR1## wherein Ar is phenyl substituted by at least one substituent selected from the group consisting of fluorine, chlorine, bromine, nitro, chloromethyl, dichloromethyl, trichloromethyl, trifluoromethyl, --CO.sub.2 R.sup.7 wherein R.sup.7 is C.sub.1 -C.sub.5 alkyl, --CONR.sup.7 R.sup.8 wherein R.sup.7 is as defined above and R.sup.8 is C.sub.1 -C.sub.5 alkyl, --C(O)R.sup.7 wherein R.sup.7 is as defined above, --OC(O)R.sup.7 wherein R.sup.7 is as defined above, --OSO.sub.3 R.sup.7 wherein R.sup.7 is as defined above, --OCF.sub.3, --S(.dbd.O).sub.2 R.sup.7 wherein R.sup.7 is as defined above, --CN and --SO.sub.3 R.sup.7 wherein R.sup.7 is as defined above, and each of R.sup.1 and R.sup.2 which may be the same or different is a saturated or unsaturated C.sub.1 -C.sub.12 aliphatic group, or R.sup.1 and R.sup.2 together form 1,2-ethylene, 1,3-propylene or 1,4-butylene, which is unsubstituted or substituted by from one to four C.sub.1 -C.sub.3 alkyl groups, which comprises:(a) reacting an aldehyde of the formula:ArCHO (I)wherein Ar is as defined above, with an acetonylphosphonate of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, in the presence of a secondary amine of the formula: ##STR3## wherein each of R.sup.3 and R.sup.4 which may be the same or different is C.sub.1 -C.sub.4 alkyl, or R.sub.3 and R.sub.4 together form 1,4-butylene or 1,5-pentylene, which is unsubstituted or substituted by from one to four C.sub.1 -C.sub.2 alkyl groups, --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 NHCH.sub.2 CH.sub.2 --, and an .alpha.-halogeno fatty acid of the formula: ##STR4## wherein X is fluorine, chlorine, bromine or iodine, and each of R.sup.5 and R.sup.6 which may be the same or different is hydrogen, fluorine, chlorine, bromine, iodine or C.sub.1 -C.sub.4 alkyl; or(b) reacting a compound of the formula ##STR5## wherein Ar, R.sup.1 and R.sup.2 are as defined above, with an acetonylphosphonate of the formula II as defined above, in the presence of an .alpha.-halogeno fatty acid of the formula V as defined above.

    Pyranobenzoxadiazole derivatives
    7.
    发明授权
    Pyranobenzoxadiazole derivatives 失效
    苯并恶唑衍生物

    公开(公告)号：US4900752A

    公开(公告)日：1990-02-13

    申请号：US304641

    申请日：1989-02-01

    申请人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Kazuhiko Ohrai ,  Kyoko Nakayama ,  Ryozo Sakoda ,  Yukinori Masuda

    发明人： Kiyotomo Seto ,  Hiroo Matsumoto ,  Yoshimasa Kamikawaji ,  Kazuhiko Ohrai ,  Kyoko Nakayama ,  Ryozo Sakoda ,  Yukinori Masuda

    IPC分类号： C07D491/052 ,  A61K31/352 ,  A61K31/41 ,  A61K31/4245 ,  A61P9/02 ,  A61P9/12 ,  A61P11/06 ,  C07D20060101 ,  C07D498/04

    CPC分类号： C07D498/04

    摘要： A compounds of the formula (I): ##STR1## wherein A represents OH or OC(O)CH.sub.3-n X.sub.n, B represents hydrogen atom, or A and B together represent a bond; R.sup.1 represents hydrogen atom, R.sup.2 represents hydrogen atom, C(Z)CH.sub.3-n X.sub.n or C(Z)NHCH.sub.3-n X.sub.n or R.sup.1 and R.sup.2 together represents (CH.sub.2).sub.m, (CH.sub.2).sub.m-1 C(Z), N(R.sup.3)(CH.sub.2).sub.2 C(Z), (CH.sub.2).sub.m-2 NHC(Z) or (CH.sub.2).sub.m-2 OC(Z) in which X represents fluorine atom, chlorine atom, bromine atom, a methyl group or a methoxy group and n represents 0 or an integer of 1 to 3, Z represents oxygem atom or sulfur atom, m represents an integer of 4 or 5 and R.sup.3 represents hydrogen atom or a methyl group, and pharmacological acceptable salts of the compounds which can form salts, processes therefor and pharmaceutical use of the compounds.

    摘要翻译： 本发明包括式（I）的化合物：其中A表示OH或OC（O）CH 3 -n Xn，B表示氢原子，或A和B一起表示键; R 1表示氢原子，R 2表示氢原子，C（Z）CH 3 -n Xn或C（Z）NHCH 3 -n X n或R 1和R 2一起表示（CH 2）m， ）m-1C（Z），N（R 3）（CH 2）2 C（Z），（CH 2）m -NHHC（Z）或（CH 2）m -OOC（Z） 原子，溴原子，甲基或甲氧基，n表示0或1〜3的整数，Z表示氧原子或硫原子，m表示4或5的整数，R 3表示氢原子或 甲基和可以形成盐的化合物的药理学可接受的盐，其制备方法，化合物的药物用途和包含该化合物的组合物。

    Dihydropyridine-5-phosphonic acid cyclic propylene ester
    8.
    发明授权
    Dihydropyridine-5-phosphonic acid cyclic propylene ester 失效
    二氢吡啶-5-膦酸环丙烯酯

    公开(公告)号：US4885284A

    公开(公告)日：1989-12-05

    申请号：US851158

    申请日：1986-04-14

    申请人： Kiyotomo Seto ,  Sakuya Tanaka ,  Ryozo Sakoda

    发明人： Kiyotomo Seto ,  Sakuya Tanaka ,  Ryozo Sakoda

    IPC分类号： C07F9/6571

    CPC分类号： C07F9/657181

    摘要： A compound of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 which may be the same or different, is hydrogen or C.sub.1 -C.sub.4 alkyl; one of X.sup.1 and X.sup.2 is nitro, fluroine, chlorine, difluoromethyoxy or trifluoromethyl and the other is hydrogen, or both of X.sup.1 and X.sup.2 are chlorine; and Y is ##STR2## wherein A is C.sub. -C.sub.6 alkylene, each of Ar.sup.1 and Ar.sup.2 which may be the same or different, is phenyl which may be substituted by chlorine, fluorine or C.sub.1 -C.sub.3 alkoxy, and m is an integer of from 0 to 4, or Y is ##STR3## wherein A, Ar.sup.1 and Ar.sup.2 are as defined above when that both X.sup.1 and X.sup.2 are chlorine; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 下式的化合物：其中R 1，R 2，R 3，R 4，R 5和R 6可以相同或不同的是氢或C 1 -C 4烷基; X1和X2之一是硝基，氟，氯，二氟甲氧基或三氟甲基，另一个是氢，或者X1和X2都是氯; 并且Y为其中A为C-C6亚烷基，Ar1和Ar2可以相同或不同，为可被氯，氟或C1-C3烷氧基取代的苯基，m为 0〜4，或Y为，其中当X1和X2都为氯时，A，Ar1和Ar2如上定义; 或其药学上可接受的盐。