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33 条记录 (耗时 0.246 秒)

    Carbostyril derivatives as combined thromboxane synthetase and cyclic-AMP phosphodiesterase inhibitors
    2.
    发明授权
    Carbostyril derivatives as combined thromboxane synthetase and cyclic-AMP phosphodiesterase inhibitors 失效
    卡波他汀衍生物作为联合血栓素合成酶和环AMP磷酸二酯酶抑制剂

    公开(公告)号：US4792561A

    公开(公告)日：1988-12-20

    申请号：US868845

    申请日：1986-05-29

    申请人： Keith A. M. Walker ,  John J. Bruno ,  Gregory R. Martinez

    发明人： Keith A. M. Walker ,  John J. Bruno ,  Gregory R. Martinez

    IPC分类号： C07D401/04 ,  C07D401/06 ,  C07D521/00 ,  A61K31/47 ,  C07D401/10 ,  C07D401/12

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06

    摘要： The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein:X is chosen from the group consisting of: ##STR2## and a covalent bond in which R.sup.1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R.sup.2 is H or OH, or R.sup.1 and R.sup.2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene;R.sup.3 is H or alkyl having 1-6 carbon atoms, R.sup.4 is H and R.sup.3 and R.sup.4 are either cis or trans to each other, or R.sup.3 and R.sup.4 taken together represent a covalent bond;n is an integer from 0-3;Het is 1-imidazolyl or 3-pyridyl; and the dotted line represents an optional covalent bond.

    摘要翻译： 本发明涉及一种抑制具有特征在于血栓素水平升高或前列环素/血栓素水平不平衡的疾病的哺乳动物中的血栓素合成酶和环-AMP磷酸二酯酶的方法，其用下式化合物或其药学上可接受的盐 其中：X选自：其中R 1为H，具有1-6个碳原子的烷基，任选取代的苯基或任选取代的苯基低级烷基的共价键， 当R 2为H或OH时，或R 1和R 2一起代表氧代，具有1-6个碳原子的亚烷基或任选取代的亚苄基; R3是H或具有1-6个碳原子的烷基，R4是H，R3和R4彼此是顺式或反式，或者R3和R4一起代表共价键; n是0-3的整数; Het是1-咪唑基或3-吡啶基; 而虚线表示任选的共价键。

    Carbostyril derivatives as combined thromboxane synthetase and cyclic-amp phosphodiesterase inhibitors
    3.
    发明授权
    Carbostyril derivatives as combined thromboxane synthetase and cyclic-amp phosphodiesterase inhibitors 失效
    卡波他特尔衍生物作为联合血栓素合成酶和环磷酸二酯酶抑制剂

    公开(公告)号：US4921862A

    公开(公告)日：1990-05-01

    申请号：US247134

    申请日：1988-09-21

    申请人： Keith A. M. Walker ,  John J. Bruno ,  Gregory R. Martinez

    发明人： Keith A. M. Walker ,  John J. Bruno ,  Gregory R. Martinez

    IPC分类号： C07D401/04 ,  C07D401/06 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06

    摘要： The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein:X is chosen from the group consisting of: ##STR2## and a covalent bond in which R.sup.1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R.sup.2 is H or OH, or R.sup.1 and R.sup.2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene;R.sup.3 is H or alkyl having 1-6 carbon atoms, R.sup.4 is H and R.sup.3 and R.sup.4 are either cis or trans to each other, or R.sup.3 and R.sup.4 taken together represent a covalent bond;n is an integer from 0-3;Het is 1-imidazolyl or 3-pyridyl; and the dotted line represents an optional covalent bond.

    摘要翻译： 本发明涉及一种抑制具有特征在于血栓素水平升高或前列环素/血栓素水平不平衡的疾病的哺乳动物中的血栓素合成酶和环-AMP磷酸二酯酶的方法，其用下式化合物或其药学上可接受的盐 其中：X选自：其中R 1为H，具有1-6个碳原子的烷基，任选取代的苯基或任选取代的苯基低级烷基的共价键， 当R 2为H或OH时，或R 1和R 2一起代表氧代，具有1-6个碳原子的亚烷基或任选取代的亚苄基; R3是H或具有1-6个碳原子的烷基，R4是H，R3和R4彼此是顺式或反式，或者R3和R4一起代表共价键; n是0-3的整数; Het是1-咪唑基或3-吡啶基; 而虚线表示任选的共价键。

    Derivatives of substituted N-alkylimidazoles
    4.
    发明授权
    Derivatives of substituted N-alkylimidazoles 失效
    取代的N-烷基咪唑衍生物

    公开(公告)号：US4321272A

    公开(公告)日：1982-03-23

    申请号：US180783

    申请日：1980-08-25

    申请人： Keith A. M. Walker

    发明人： Keith A. M. Walker

    IPC分类号： C07D405/06 ,  A61K31/415 ,  C07D233/60 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： Compounds useful as anticonvulsant agents, antifungals and antibacterials are represented by the formula ##STR1## wherein R.sup.1 is phenyl optionally substituted by one or more substituents selected from the group consisting of halo, lower alkyl of one to four carbon atoms, lower alkoxy of one to four carbon atoms and trifluoromethyl; Z is ethylene or propylene optionally substituted by one or more lower alkyl groups of one to four carbon atoms; m is 1, 2, 3 or 4 and n is 0, 1, 2 or 3 with the proviso that the sum of m and n is 2, 3 or 4; and the pharmaceutically acceptable acid addition salts thereof.The ketone intermediates useful in preparing compounds of formula (I) also have anticonvulsant activity.

    摘要翻译： 可用作抗惊厥剂，抗真菌剂和抗菌剂的化合物由式（I）表示，其中R 1是任选被一个或多个选自卤素，一至四个碳原子的低级烷基，低级烷氧基 一至四个碳原子和三氟甲基; Z是任选被一个或多个1-4个碳原子的低级烷基取代的乙烯或丙烯; m为1,2,3或4，n为0,1,2或3，条件是m和n之和为2,3或4; 及其药学上可接受的酸加成盐。 用于制备式（I）化合物的酮中间体也具有抗惊厥活性。

    1-[(Substituted-naphthyl)ethyl]-imidazole derivatives
    5.
    发明授权
    1-[(Substituted-naphthyl)ethyl]-imidazole derivatives 失效
    1 - [（取代的 - 萘基）乙基] - 咪唑衍生物

    公开(公告)号：US4277486A

    公开(公告)日：1981-07-07

    申请号：US19202

    申请日：1979-03-09

    申请人： Keith A. M. Walker

    发明人： Keith A. M. Walker

    IPC分类号： A61K31/415 ,  A61P25/00 ,  C07C45/46 ,  C07C45/63 ,  C07D233/60 ,  C07D521/00 ,  C07D405/06

    CPC分类号： C07D231/12 ,  C07C45/46 ,  C07C45/63 ,  C07D233/56 ,  C07D249/08

    摘要： Compounds of the formula ##STR1## wherein m is the integer 1, 2 or 3; R is independently selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, halo, trifluoromethyl and hydroxy when m is the integer 1, 2 or 3 and methylenedioxy when m is the integer 2; Z is hydroxymethylene, esterified hydroxymethylene, alkoxymethylene, alkylthiomethylene, carbonyl, or ketal-, thioketal- or hemithioketal- protected carbonyl, and the pharmaceutically acceptable acid addition salts thereof, are useful as anticonvulsants, anti-secretory agents and spermatocides.

    摘要翻译： 式（I）的化合物，其中m是整数1,2或3; 当m为整数2时，当m为整数1,2或3时，R独立地选自C 1至C 6烷基，C 1至C 6烷氧基，卤素，三氟甲基和羟基; Z是羟基亚甲基，酯化的羟基亚甲基，烷氧基亚甲基，烷基亚甲基，羰基或缩酮，硫代缩酮或半硫酮缩酮保护的羰基及其药学上可接受的酸加成盐，可用作抗惊厥药，抗分泌剂和精子霉素。

    1-[2-(1-Adamantyl)-2-(R-thio)ethyl]imidazoles and 1-[2-(1-adamantyl)-2-(R-oxy)ethyl]imidazoles
    6.
    发明授权
    1-[2-(1-Adamantyl)-2-(R-thio)ethyl]imidazoles and 1-[2-(1-adamantyl)-2-(R-oxy)ethyl]imidazoles 失效
    1- {8 2-（1-金刚烷基）-2-（R-硫代）乙基{9咪唑和1- {8 2-（1-金刚烷基）-2-（R-氧）乙基{9咪唑

    公开(公告)号：US4036975A

    公开(公告)日：1977-07-19

    申请号：US665012

    申请日：1976-03-08

    申请人： Keith A. M. Walker ,  Stefan Howard Unger

    发明人： Keith A. M. Walker ,  Stefan Howard Unger

    IPC分类号： C07D521/00 ,  A61K31/415 ,  C07D233/60

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： Compounds of the formula ##STR1## wherein R is alkyl, cycloalkyl, cycloalkyl lower alkyl, phenyl or phenyl lower alkyl, said phenyl and phenyl lower alkyl optionally substituted on the phenyl ring with one or more substituents independently selected from the group consisting of halo, lower alkyl and trifluoromethyl; and X is oxygen or sulfur with the proviso that X is not oxygen when R is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal, antibacterial and antiprotozoal agents.

    摘要翻译： 式（I）的化合物其中R是烷基，环烷基，环烷基低级烷基，苯基或苯基低级烷基，所述苯基和苯基低级烷基在苯环上任选被一个或多个取代基取代，所述取代基独立地选自 的卤素，低级烷基和三氟甲基; 并且X是氧或硫，条件是当R是苯基或取代的苯基时X不是氧; 其抗菌酸加成盐可用作抗真菌剂，抗菌剂和抗原虫剂。