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    2-hydroxypropylamine aryl ester derivatives and pharmaceutical use
    61.
    发明授权
    2-hydroxypropylamine aryl ester derivatives and pharmaceutical use 失效
    2-羟基丙基胺芳酯衍生物和药物用途

    公开(公告)号：US4935421A

    公开(公告)日：1990-06-19

    申请号：US318147

    申请日：1989-03-01

    Applicant: Sheung T. Kam ,  William L. Matier

    Inventor： Sheung T. Kam ,  William L. Matier

    IPC: C07C275/14 ,  C07C275/28 ,  C07D295/215

    CPC classification number: C07D295/215 ,  C07C275/14 ,  C07C275/28

    Abstract: Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.

    Abstract translation: 新颖的通式的化合物，其中Ar表示取代或未取代的芳族或杂环基团; W表示1至约10个碳原子的亚烷基; 并且B代表-NR2COR1，-NR2CONR1R3，-NR2SO2R1，-NR2SO2NR1R3或-NR2COOR1，其中R1，R2和R3可以相同或不同，可以是氢，烷基，烷氧基烷基，环烷基，烯基，炔基，芳基，杂芳基或 除了当B是-NR 2 SO 2 R 1或-NR 2 COOR 1时，R 1不是氢，或者R 1和R 3可以与N一起形成5至7元杂环基; 及其药学上可接受的盐。 这些化合物表现出β-肾上腺素能阻断活性，并且也可用于治疗青光眼。

    N-(substituted aryl)-N'-(substituted alkoxy)-ureas and thioureas as antihypercholesterolemic and antiatherosclerotic agents
    62.
    发明授权
    N-(substituted aryl)-N'-(substituted alkoxy)-ureas and thioureas as antihypercholesterolemic and antiatherosclerotic agents 失效
    N-（取代的芳基）-N' - （取代的烷氧基） - 脲和硫脲作为抗高胆固醇血症和抗动脉粥样硬化剂

    公开(公告)号：US4923896A

    公开(公告)日：1990-05-08

    申请号：US308911

    申请日：1989-02-09

    Applicant: Bharat K. Trivedi

    Inventor： Bharat K. Trivedi

    IPC: C07C275/28 ,  C07C275/64

    CPC classification number: C07C275/28 ,  C07C275/64

    Abstract: Novel N-[substituted aryl]-N'-(substituted alkoxy)-urea and thiourea derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.

    Abstract translation: 描述了新的N- [取代的芳基] -N' - （取代的烷氧基） - 脲和硫脲衍生物，以及其制备方法和药物组合物，其可用于预防胆固醇的肠道吸收，因此是有用的 在治疗高胆固醇血症和动脉粥样硬化。

    Esters of aryloxypropanolamine derivatives
    63.
    发明授权
    Esters of aryloxypropanolamine derivatives 失效
    芳氧丙醇胺衍生物的酯

    公开(公告)号：US4906661A

    公开(公告)日：1990-03-06

    申请号：US308575

    申请日：1989-02-10

    Applicant: Paul W. Erhardt ,  William L. Matier

    Inventor： Paul W. Erhardt ,  William L. Matier

    IPC: C07C275/14 ,  C07C275/28 ,  C07D285/10 ,  C07D295/215 ,  C07D303/22 ,  C07D333/34 ,  C07D333/38

    CPC classification number: C07D285/10 ,  C07C275/14 ,  C07C275/28 ,  C07D295/215 ,  C07D303/22 ,  C07D333/34 ,  C07D333/38

    Abstract: Novel compounds of the general formula ##STR1## wherein R.sub.1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the ##STR2## group may be the same or different; Ar is heterocyclic, unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.sub.5 are not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.3 or --NR.sub.2 COOR.sub.5, or R.sub.3 and R.sub.4 may together with N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof.

    Abstract translation: 其中R1是低级烷基，低级环烷基，低级烯基，低级炔基，低级烷基羧甲基，芳基羧甲基，芳基或芳烷基的新型化合物。 A是直接键，低级亚烷基或低级亚烯基; x为1或2，条件是当x大于1时，组的不同出现可能相同或不同; Ar是杂环的，未取代的芳族或被低级烷基，低级烯基，低级炔基，低级烷氧基，卤素，乙酰氨基，氨基，硝基，低级烷基氨基，羟基，低级羟烷基或氰基取代的芳基; W是含有1至约10个碳原子的亚烷基; 并且B为-NR2COR3，-NR2CONR3R4，-NR2SO2R3，-NR2SO2NR3R4或-NR2COOR5，其中R2，R3，R4和R5可以相同或不同，可以是氢，烷基，烷氧基烷基，烷氧基芳基，环烷基，烯基，炔基， 芳基，杂芳基或芳烷基，但当B是-NR 2 SO 2 R 3或-NR 2 COOR 5时，R 3和R 5不是氢，或者R 3和R 4可以与N一起形成5至7元杂环基; 及其药学上可接受的盐。

    Esters of aryloxypropanolamine derivatives
    64.
    发明授权
    Esters of aryloxypropanolamine derivatives 失效
    芳氧丙醇胺衍生物的酯

    公开(公告)号：US4804677A

    公开(公告)日：1989-02-14

    申请号：US93669

    申请日：1987-09-08

    Applicant: Paul W. Erhardt ,  William L. Matier

    Inventor： Paul W. Erhardt ,  William L. Matier

    IPC: C07C275/14 ,  C07C275/28 ,  C07D285/10 ,  C07D295/215 ,  C07D303/22 ,  C07D333/34 ,  C07D333/38 ,  C07C103/22 ,  A61K31/165 ,  C07C103/78

    CPC classification number: C07D285/10 ,  C07C275/14 ,  C07C275/28 ,  C07D295/215 ,  C07D303/22 ,  C07D333/34 ,  C07D333/38

    Abstract: Novel compounds of the general formula ##STR1## wherein R.sub.1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the ##STR2## group may be the same or different; Ar is heterocyclic unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.sub.5 are not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.3 or --NR.sub.2 COOR.sub.5, or R.sub.3 and R.sub.4 may together with N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof.

    Abstract translation: 其中R1是低级烷基，低级环烷基，低级烯基，低级炔基，低级烷基羧甲基，芳基羧甲基，芳基或芳烷基的新型化合物。 A是直接键，低级亚烷基或低级亚烯基; x为1或2，条件是当x大于1时，组的不同出现可能相同或不同; Ar是被低级烷基，低级烯基，低级炔基，低级烷氧基，卤素，乙酰氨基，氨基，硝基，低级烷基氨基，羟基，低级羟基烷基或氰基取代的杂芳基， W是含有1至约10个碳原子的亚烷基; 并且B为-NR2COR3，-NR2CONR3R4，-NR2SO2R3，-NR2SO2NR3R4或-NR2COOR5，其中R2，R3，R4和R5可以相同或不同，可以是氢，烷基，烷氧基烷基，烷氧基芳基，环烷基，烯基，炔基， 芳基，杂芳基或芳烷基，但当B是-NR 2 SO 2 R 3或-NR 2 COOR 5时，R 3和R 5不是氢，或者R 3和R 4可以与N一起形成5至7元杂环基; 及其药学上可接受的盐。

    Method for inhibiting the growth of fungi with phenyl glycine compounds
    68.
    发明授权
    Method for inhibiting the growth of fungi with phenyl glycine compounds 失效
    用苯基甘氨酸化合物抑制真菌生长的方法

    公开(公告)号：US4492683A

    公开(公告)日：1985-01-08

    申请号：US406007

    申请日：1982-08-06

    Applicant: Krishen L. Nagpal

    Inventor： Krishen L. Nagpal

    IPC: A01N37/44 ,  A01N37/46 ,  A01N41/06 ,  A01N47/30 ,  C07C273/18 ,  C07C275/28 ,  C07C275/30 ,  C07C335/16 ,  A01N37/10 ,  A01N37/12

    CPC classification number: C07C273/1827 ,  A01N37/44 ,  A01N37/46 ,  A01N41/06 ,  A01N47/30 ,  C07C335/16

    Abstract: New compounds and a method for inhibiting the growth of fungus is disclosed which comprises contacting said fungus with a fungicidal amount of a phenyl glycine compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, alkenyl, phenyl, substituted phenyl, halogen, amino or hydroxy groups; R.sub.3 is a hydrogen, lower alkyl, substituted lower alkyl, cycloalkyl, benzoyl, halo or nitro substituted benzoyl, substituted cycloalkyl, methylcarbamoyl, cyclohexylcarbamoyl, phenylcarbamoyl, halophenylcarbamoyl, methylphenylcarbamoyl, methylthiocarbamoyl, phenyl, substituted phenyl, napthyl group or --SO.sub.2 R.sub.7 where R.sub.7 is a hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl or amino group; R.sub.4 and R.sub.5 are independently hydrogen, lower alkyl or substituted lower alkyl groups and R.sub.6 is a hydrogen, lower alkyl or substituted lower alkyl, alkenyl or substituted alkenyl group.

    Abstract translation: 公开了新的化合物和抑制真菌生长的方法，其包括使所述真菌与杀真菌剂量的下式的苯基甘氨酸化合物接触：其中R 1和R 2独立地是氢，低级烷基，取代的低级烷基，环烷基 取代的环烷基，烯基，苯基，取代的苯基，卤素，氨基或羟基; R3是氢，低级烷基，取代的低级烷基，环烷基，苯甲酰基，卤素或硝基取代的苯甲酰基，取代的环烷基，甲基氨基甲酰基，环己基氨基甲酰基，苯基氨基甲酰基，卤代苯基氨基甲酰基，甲基苯基氨基甲酰基，甲硫基氨基甲酰基，苯基，取代的苯基，萘基或-SO2R7，其中R7是 氢，烷基，取代的烷基，苯基，取代的苯基或氨基; R4和R5独立地是氢，低级烷基或取代的低级烷基，R6是氢，低级烷基或取代的低级烷基，烯基或取代的烯基。

    Process for preparing substituted urea derivatives
    70.
    发明授权
    Process for preparing substituted urea derivatives 失效
    制备取代脲衍生物的方法

    公开(公告)号：US4435567A

    公开(公告)日：1984-03-06

    申请号：US334470

    申请日：1981-12-28

    Applicant: Gyorgy Lugosi ,  Antal Simay ,  Janos Bodnar ,  Laszlo Simandi ,  Eva Somfai

    Inventor： Gyorgy Lugosi ,  Antal Simay ,  Janos Bodnar ,  Laszlo Simandi ,  Eva Somfai

    IPC: C07D295/20 ,  C07C67/00 ,  C07C239/00 ,  C07C273/18 ,  C07C275/02 ,  C07C275/06 ,  C07C275/26 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07D213/75 ,  C07D217/06 ,  C07D235/32 ,  C07D275/06 ,  C07D277/82 ,  C07D285/12 ,  C07D285/135 ,  C07D295/215 ,  C07C127/00 ,  C07C127/15 ,  C07C127/17 ,  C07C127/19

    CPC classification number: C07D213/75 ,  C07C273/1809 ,  C07D217/06 ,  C07D235/32 ,  C07D277/82 ,  C07D285/135 ,  C07D295/215

    Abstract: A process for the preparation of substituted urea derivatives, and compositions and concentrates for the same purpose are disclosed. According to the process the substituted urea derivatives of formula (I) ##STR1## wherein R is hydrogen, alkyl, aryl, cycloalkyl or aralkyl, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkinyl, alkoxy, oxyalkyl, cycloalkyl, aralkyl, alkoxycarbonylalkyl, aryl or heteroaryl, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom may form a saturated or unsaturated heterocycle, or a condensed and/or substituted ring system, and said heterocycle or said condensed and/or substituted ring system may contain also a sulfo group,can be manufactured by reacting an amine of formula (II) ##STR2## with an N-carbamoyl-benzoic acid sulfimide derivative of formula (III) ##STR3## The disclosed N-acylating composition comprises of from 3 to 60% by weight, preferably of from 5 to 50% by weight sulfimide derivative of formula (III), of from 97 to 40% by weight, preferably of from 95 to 50% by weight solvent, and if desired, an organic or inorganic base.The disclosed N-acylating concentrate comprises of from 60 to 95.5% by weight N-acylating agent of formula (III) and of from 4.5 to 40% by weight additives.

    Abstract translation: 公开了用于制备取代的脲衍生物的方法，以及用于相同目的的组合物和浓缩物。 根据该方法，式（I）的取代脲衍生物其中R是氢，烷基，芳基，环烷基或芳烷基，R1和R2是氢，烷基，烯基，炔基，烷氧基，烷氧基，环烷基，芳烷基，烷氧基羰基 ，芳基或杂芳基，或R 1和R 2与相邻的氮原子一起可以形成饱和或不饱和的杂环或稠合和/或取代的环系，并且所述杂环或所述缩合和/或取代的环系可以含有磺基 可以通过使式（II）的胺与式（III）的N-氨基甲酰基 - 苯甲酸硫酰亚胺衍生物反应来制备。所公开的N-酰化组合物包含3至60重量％ ，优选为5至50重量％的式（III）的亚磺酰亚胺衍生物，为97至40重量％，优选为95至50重量％的溶剂，如果需要，为有机或无机碱。 所公开的N-酰化浓缩物包含60至95.5重量％的式（III）的N-酰化剂和4.5至40重量％的添加剂。

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