Process for the production of nuclear substituted cinnamoylanthranilic
acid derivatives
    2.
    发明授权
    Process for the production of nuclear substituted cinnamoylanthranilic acid derivatives 失效
    制备核取代肉桂酰邻氨基苯甲酸衍生物的方法

    公开(公告)号:US4587356A

    公开(公告)日:1986-05-06

    申请号:US654231

    申请日:1984-09-25

    CPC分类号: C07D295/027

    摘要: The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound.Illustrative of the process is the reaction of 3-hydroxy-4-methoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of a molar excess of piperidine to provide a high purity intermediate salt precipitate, and the salt is treated with an acidic reagent to yeild N-(3-hydroxy-4-methoxycinnamoyl)anthranilic acid product.

    摘要翻译: 本发明提供了制备核取代肉桂酰邻氨基苯甲酸化合物的改进方法。 该方法的实例是在惰性溶剂介质中,在摩尔过量的哌啶存在下,3-羟基-4-甲氧基苯甲醛与2-羧基丙二酸的反应,得到高纯度的中间盐沉淀物,盐用 酸性试剂洗脱N-(3-羟基-4-甲氧基肉桂酰)邻氨基苯甲酸产物。

    Imidazole derivatives
    3.
    发明授权
    Imidazole derivatives 失效
    咪唑衍生物

    公开(公告)号:US4461905A

    公开(公告)日:1984-07-24

    申请号:US413204

    申请日:1982-08-30

    摘要: The imidazole derivatives of the general formula: ##STR1## wherein A and B may be the same or different, and each is a straight- or branched-chain alkylene or alkenylene group having 1 to 8 carbon atoms, D is an acyl group having 2 to 10 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms or a dialkoxymethyl group having 3 to 13 carbon atoms, Q is a cyano group or an alkoxycarbonyl group having 2 to 7 carbon atoms, X is a halogen atom, Z is ##STR2## (wherein E is a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms, Y is an oxygen atom or a sulfur atom and may be connected with either A or B), n is zero or 1, with the proviso that n is 1 when Y connects with B.These compounds are novel compounds and are useful as intermediates in producing 1-substituted imidazole derivatives which possess strong and specific inhibitory effects on thromboxane synthetase and thus are useful as therapeutically active agents for treatment of diseases caused by thromboxane A.sub.2.

    摘要翻译: 具有以下通式的咪唑衍生物:其中A和B可以相同或不同,并且各自是具有1至8个碳原子的直链或支链亚烷基或亚烯基,D是具有2个 碳原子数为2〜7的烷氧基羰基或碳原子数3〜13的二烷氧基甲基,Q为氰基或碳原子数2〜7的烷氧基羰基,X为卤素原子,Z为< IMAGE>(其中E是氢原子,卤素原子,具有1至6个碳原子的烷基或具有1至6个碳原子的烷氧基,Y是氧原子或硫原子,并且可以与A 或B),n为0或1,条件是当Y与B连接时n为1。这些化合物是新化合物,可用作生产1-取代咪唑衍生物的中间体,其具有对凝血恶烷合成酶的强和特异性抑制作用 因此可用作治疗活性剂 治疗由血栓素A2引起的疾病。

    Piperidino-3,4-dihydrocarbostyril compounds
    5.
    发明授权
    Piperidino-3,4-dihydrocarbostyril compounds 失效
    哌啶子基-3,4-二氢喹诺酮类化合物

    公开(公告)号:US5294718A

    公开(公告)日:1994-03-15

    申请号:US101006

    申请日:1993-08-03

    CPC分类号: C07D401/04

    摘要: Piperidino-3,4-dihydrocarbostyril compounds represented by the formula: ##STR1## wherein R.sup.1 represents a hydroxy group or an acyloxy group having 2 to 11 carbon atoms; one of R.sup.2 and R.sup.3 represents a nitro group, a cyano group, an alkoxycarbonyl group having 2 to 7 carbon atoms, an alkyl group having 1 to 4 carbon atoms, a haloalkyl group having 1 to 3 carbons atoms, or a halogen atom, and the other represents a hydrogen atom; and pharmaceutically acceptable salts thereof, exhibit platelet aggregation inhibiting activity and thus being useful as therapeutic agents for the prevention or treatment of cerebral ischemic disorders and arterial ischemic disorders.

    摘要翻译: 由下式表示的哌啶子基-3,4-二氢喹诺酮化合物:其中R 1表示羟基或具有2至11个碳原子的酰氧基; R 2和R 3中的一个表示硝基,氰基,具有2至7个碳原子的烷氧基羰基,具有1至4个碳原子的烷基,具有1至3个碳原子的卤代烷基或卤素原子,以及 另一个表示氢原子; 其药学上可接受的盐具有血小板聚集抑制活性,因此可用作预防或治疗脑缺血障碍和动脉缺血障碍的治疗剂。

    1,3-Disubstituted imidazoles
    6.
    发明授权
    1,3-Disubstituted imidazoles 失效
    1,3-二取代的咪唑

    公开(公告)号:US4469865A

    公开(公告)日:1984-09-04

    申请号:US423332

    申请日:1982-09-24

    摘要: 1,3-Disubstituted imidazoles of the general formula (I): ##STR1## wherein A and B may be the same or different, and each is a straight- or branched-chain alkylene or alkenylene group having 1 to 8 carbon atoms, Y is an acyl group having 2 to 10 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms or an dialkoxymethyl group having 3 to 13 carbon atoms, Z is a cyano group or an alkoxycarbonyl group having 2 to 7 carbon atoms, X is a halogen atom, n is zero or 1. The said compounds are intermediates for producing the imidazole derivatives of the general formula (V) above which possess strong and specific inhibitory effects on thromboxane synthetase and thus are useful as therapeutical agents for treatment of diseases caused by thromboxane A.sub.2.

    摘要翻译: 通式(I)的1,3-二取代咪唑:其中A和B可以相同或不同,并且各自是具有1至8个碳的直链或支链亚烷基或亚烯基 原子,Y为碳原子数2〜10的酰基,碳原子数2〜7的烷氧基羰基或碳原子数3〜13的二烷氧基甲基,Z为氰基或碳原子数为2〜7的烷氧基羰基, X是卤素原子,n是0或1.所述化合物是用于生产上述通式(V)的咪唑衍生物的中间体,其具有对凝血恶烷合成酶的强和特异性抑制作用,因此可用作治疗药物 血栓素A2引起的疾病。

    Polyphenylene ether resin
    10.
    发明授权
    Polyphenylene ether resin 失效
    聚苯醚树脂

    公开(公告)号:US5861437A

    公开(公告)日:1999-01-19

    申请号:US930433

    申请日:1997-10-07

    CPC分类号: C08L71/126 C08G65/485

    摘要: A poly(phenylene ether) resin composed of structural units represented by the general formula: ##STR1## (wherein R.sup.1, R.sup.2 and R.sup.3 represent each alkyl, cycloalkyl, etc. or H (provided that two or more of R.sup.1, R.sup.2 and R.sup.3 do not represent H at the same time), or one of R.sup.1, R.sup.2 and R.sup.3 represents alkyl or H while the others together form a saturated ring, or R.sup.1, R.sup.2 and R.sup.3 together form an aromatic ring; A represents alkyl; p is an integer of from 3 to 5; and Y.sup.- represents a pharmaceutically acceptable acid residue) and/or structural units represented by the general formula: ##STR2## (wherein R.sup.4, R.sup.5 and R.sup.6 represents each alkyl, cycloalkyl, etc. or H (provided that two or more of R.sup.4, R.sup.5 and R.sup.6 do not represent H at the same time), or one of R.sup.4, R.sup.5 and R.sup.6 represents alkyl or H while the others together form a saturated ring, or R.sup.4, R.sup.5 and R.sup.6 together form an aromatic ring; and A, p and Y.sup.- have same meanings as defined above) and structural units represented by the general formula: ##STR3## (wherein R.sup.7 and R.sup.8 represents each alkyl, cycloalkyl, etc. or together form a saturated ring; q is an integer of from 3 to 20; and A, p, and Y.sup.- have same meanings as defined above) wherein the sum of the contents of the structural units represented by the general formula (I) and the structural units represented by the general formula (II) amounts to 40 to 96% by mole and the content of the structural units represented by the general formula (III) amounts to 4 to 60% by mole based upon the content of phenylene ether component and a process for producing the same. The poly(phenylene ether) resins have the effect of adsorbing bile acids and are useful as a cholesterol reducing agent.

    摘要翻译: PCT No.PCT / JP96 / 00931 Sec。 371日期1997年10月7日第 102(e)日期1997年10月7日PCT提交1996年4月5日PCT公布。 公开号WO96 / 32435 日期:1996年10月17日由以下通式表示的结构单元构成的聚苯醚树脂:烷基,环烷基等或H(前提是R1,R2和R3中的两个或更多个不表示相同的H 时间),或者R1,R2和R3中的一个表示烷基或H,而另一个一起形成饱和环,​​或者R1,R2和R3一起形成芳香环; A代表烷基; p是3至5的整数; 和/或由以下通式表示的结构单元:其中R 4,R 5和R 6表示各自的烷基,环烷基等或H(条件是两个或多个 R4,R5和R6不同时表示H),或者R4,R5和R6中的一个表示烷基或H,而另一个共同形成饱和环,​​或者R4,R5和R6一起形成芳香环; A,p和Y-具有与上述相同的含义)和由通式(III)表示的结构单元(其中R 7和R 8表示各个烷基,环烷基等或一起形成饱和环; q为 3〜20的整数,A,p,Y-具有与上述相同的含义),其中由通式(I)表示的结构单元的含量和由通式 (II)表示的结构单元的含量为40〜96摩尔%,通式(I)表示的结构单元的含量 II)相对于亚苯基醚成分的含量为4〜60摩尔%及其制造方法。 聚苯醚树脂具有吸附胆汁酸的作用,可用作胆固醇降低剂。