Pyranobenzoxadiazole derivatives
    3.
    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

    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。

    T-TYPE CALCIUM CHANNEL BLOCKER
    5.
    发明申请
    T-TYPE CALCIUM CHANNEL BLOCKER 审中-公开
    T型钙通道阻塞器

    公开(公告)号:US20100105636A1

    公开(公告)日:2010-04-29

    申请号:US12651849

    申请日:2010-01-04

    CPC分类号: A61K31/675

    摘要: There is provided a T-type calcium channel blocker that is a compound of formula (1), a pharmaceutically acceptable salt thereof or a solvate thereof: wherein Ar1 is phenyl group, pyridyl group, furyl group or 2,1,3-benzoxadiazol-4-yl group; nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring or pyridine ring; Z is a group of formula (2) or CO2R2; Ra and Rb are independently of each other C1-6alkyl group, ANR8R9, CH2OANR8R9, or the like; in case where the nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring, R1 is C1-6alkyl group, ANR8R9, AN(CH2CH2)2NR8, AN(CH2CH2)2O, AOR8 or benzyl group; R3 is hydrogen atom, C1-20alkyl group, ANR8R9, a group of formula or the like.

    摘要翻译: 提供了式(1)化合物,其药学上可接受的盐或其溶剂化物的T型钙通道阻断剂:其中Ar1是苯基,吡啶基,呋喃基或2,1,3-苯并恶二唑-2-基, 4-基; 含氮杂环部分为1,4-二氢吡啶环或吡啶环; Z是式(2)或CO 2 R 2的基团; R a和R b彼此独立地为C 1-6烷基,ANR 8 R 9,CH 2 OANR 8 R 9等; 在含氮杂环部分为1,4-二氢吡啶环的情况下,R 1为C 1-6烷基,ANR 8 R 9,AN(CH 2 CH 2)2 NR 8,AN(CH 2 CH 2)2 O,AOR 8或苄基; R3是氢原子,C1-20烷基,ANR8R9,式等基团。

    T-type calcium channel blocker
    6.
    发明申请
    T-type calcium channel blocker 审中-公开
    T型钙通道阻滞剂

    公开(公告)号:US20070129335A1

    公开(公告)日:2007-06-07

    申请号:US10580532

    申请日:2004-11-25

    CPC分类号: A61K31/675

    摘要: There is provided a T-type calcium channel blocker that is a compound of formula (1), a pharmaceutically acceptable salt thereof or a solvate thereof. wherein Ar1 is phenyl group, pyridyl group, furyl group or 2,1,3-benzoxadiazol-4-yl group; nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring or pyridine ring; Z is a group of formula (2) or CO2R2; Ra and Rb are independently of each other C1-6alkyl group, ANR8R9, CH2OANR8R9, or the like; in case where the nitrogen-containing hetero ring moiety is 1,4-dihydropyridine ring, R1 is C1-6alkyl group, ANR8R9, AN(CH2CH2)2NR8, AN(CH2CH2)2O, AOR8 or benzyl group; R3 is hydrogen atom, C1-20alkyl group, ANR8R9, a group of formula or the like.

    摘要翻译: 提供了一种T型钙通道阻断剂,其是式(1)的化合物,其药学上可接受的盐或其溶剂化物。 其中Ar 1是苯基,吡啶基,呋喃基或2,1,3-苯并二唑-4-基; 含氮杂环部分为1,4-二氢吡啶环或吡啶环; Z是式(2)或CO 2 R 2的基团; R a a和R b彼此独立地是C 1-6烷基,ANR 8 R 12 > 9 ,CH 2,OANR 8,9,9等等; 在含氮杂环部分为1,4-二氢吡啶环的情况下,R 1为C 1-6烷基,ANR 8 O AN(CH 2 CH 2 CH 2)2 NR 8,其中R 1,R 2, AN(CH 2 CH 2)2 O,AOR 8或苄基; R 3是氢原子,C 1-20烷基,ANR 8 R 9,式 或类似物。

    Process for producing alpha-(benzylidene)acetonylphosphonates
    8.
    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

    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.

    Process for the optical resolution of pyranobenzoxadiazole compounds
    9.
    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

    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:< IMAGE>并分离如此形成的非对映体盐。