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    • 1. 发明授权
    • Bicyclic compounds
    • 双环化合物
    • US4762924A
    • 1988-08-09
    • US62033
    • 1987-06-15
    • Cedric H. HassallGeoffrey LawtonSally Redshaw
    • Cedric H. HassallGeoffrey LawtonSally Redshaw
    • C07D237/04C07D487/04C07D245/00A61K31/50C07D487/06
    • C07D487/04C07D237/04
    • Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl,as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.
    • 式Ⅰ的化合物,其中R1是氢,烷酰基或芳酰基; R2是氢或烷基; R3是氢或芳基; R4和R5各自为氢或R4和R5一起为氧代; 其中当R 2为氢时,其中R 6为氢,烷基或芳烷基,以及其与碱的药学上可接受的盐及其与Y的药学上可接受的盐,Y为-CH 2 - , - CH 2 CH 2 - 或-N(R 6) 描述了具有抗高血压活性并且可以用作药物制剂形式的药物的-N(R 6) - 。 式I化合物含有至少一个不对称碳原子。 因此,本发明不仅包括这些化合物的光学均匀形式,还包括各种非对映异构体外消旋体和不同非对映异构体外消旋体的混合物。
    • 3. 发明授权
    • Pyridazine intermediates
    • 哒嗪中间体
    • US4826980A
    • 1989-05-02
    • US217805
    • 1988-07-12
    • Cedric H. HassallGeoffrey LawtonSally Redshaw
    • Cedric H. HassallGeoffrey LawtonSally Redshaw
    • C07D237/04C07D487/04C07D237/24C07D237/18
    • C07D487/04C07D237/04
    • Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl, as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.
    • 式Ⅰ的化合物,其中R1是氢,烷酰基或芳酰基; R2是氢或烷基; R3是氢或芳基; R4和R5各自为氢或R4和R5一起为氧代; 其中当R 2为氢时,其中R 6为氢,烷基或芳烷基,以及其与碱的药学上可接受的盐及其与Y的药学上可接受的盐,Y为-CH 2 - , - CH 2 CH 2 - 或-N(R 6) 描述了具有抗高血压活性并且可以用作药物制剂形式的药物的-N(R 6) - 。 式I化合物含有至少一个不对称碳原子。 因此,本发明不仅包括这些化合物的光学均匀形式,还包括各种非对映异构体外消旋体和不同非对映异构体外消旋体的混合物。
    • 4. 发明授权
    • Pyridazo (1,2-a) (1,2) diazepine derivatives
    • 哒唑(1,2-a)(1,2)二氮杂衍生物
    • US4743687A
    • 1988-05-10
    • US877085
    • 1986-06-23
    • Geoffrey LawtonSally Redshaw
    • Geoffrey LawtonSally Redshaw
    • C07D487/04C07F20060101C07F9/645C07F9/6561A61K31/50A61K31/55C07D237/04
    • C07D487/04C07F9/645C07F9/6561
    • Compounds of the formula ##STR1## wherein R.sup.1 represents hydroxy, alkyl, aralkyl, aralkoxy-alkyl, hydroxy-alkyl, amino-alkyl, acylamino-alkyl, monoalkylamino-alkyl, dialkylamino-alkyl, alkoxycarbonylamino-alkyl, halo-alkyl, carboxy-alkyl, alkoxycarbonyl-alkyl, alkoxy or aralkoxy; R.sup.2 and R.sup.3 each represent hydrogen, alkyl or aralkyl; R.sup.4 and R.sup.5 each represent hydrogen or R.sup.4 and R.sup.5 together represent oxo; and X represents an oxygen atom or the group --NR.sup.6 -- in which R.sup.6 represents hydrogen, alkyl or aralkyl or --(CH.sub.2).sub.n -- in which n stands for zero, 1 or 2,and racemates, enantiomers, diastereoisomers or pharmaceutically acceptable salts thereof have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations. They can be prepared according to known methods.Compounds useful as starting materials for producing the compounds of formula I are also provided.
    • 式I的化合物,其中R 1表示羟基,烷基,芳烷基,芳烷氧基 - 烷基,羟基 - 烷基,氨基 - 烷基,酰氨基 - 烷基,单烷基氨基 - 烷基,二烷基氨基 - 烷基,烷氧基羰基氨基 - 烷基,卤代烷基,羧基 烷基,烷氧基羰基 - 烷基,烷氧基或芳烷氧基; R2和R3各自表示氢,烷基或芳烷基; R4和R5各自表示氢或R4和R5一起代表氧代; 并且X表示氧原子或基团-NR 6 - ,其中R 6表示氢,烷基或芳烷基或 - (CH 2)n - ,其中n代表0,1或2,以及外消旋物,对映异构体,非对映异构体或其药学上可接受的盐 具有抗高血压活性,可用作药物制剂形式的药物。 它们可以根据已知方法制备。 还提供了可用作制备式I化合物的起始原料的化合物。
    • 5. 发明授权
    • Bicyclic compounds
    • 双环化合物
    • US4785093A
    • 1988-11-15
    • US48172
    • 1987-05-11
    • Cedric H. HassallGeoffrey LawtonSally Redshaw
    • Cedric H. HassallGeoffrey LawtonSally Redshaw
    • C07D237/04C07D487/04C07D245/00A61K31/50C07D487/06
    • C07D487/04C07D237/04
    • Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --or--N(R.sup.6)--in which R.sup.6 is hydrogen, alkyl or aralkyl, as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.
    • 式Ⅰ的化合物,其中R1是氢,烷酰基或芳酰基; R2是氢或烷基; R3是氢或芳基; R4和R5各自为氢或R4和R5一起为氧代; 并且Y是-CH 2 - , - CH 2 CH 2 - 或-N(R 6) - 当R 2是氢时,R 6是氢,烷基或芳烷基,以及其与碱的药学上可接受的盐,当Y是 描述了具有抗高血压活性并且可以用作药物制剂形式的药物的-N(R 6) - 。 式I化合物含有至少一个不对称碳原子。 因此,本发明不仅包括这些化合物的光学均匀形式,还包括各种非对映异构体外消旋体和不同非对映异构体外消旋体的混合物。
    • 8. 发明授权
    • Pyridazo-diazepines, diazocines, and -triazepines having
anti-hypertensive activity
    • 具有抗高血压活性的哒唑二氮杂,二氮嗪类和三氮类
    • US4692438A
    • 1987-09-08
    • US764372
    • 1985-08-12
    • Cedric H. HassallGeoffrey LawtonSally Redshaw
    • Cedric H. HassallGeoffrey LawtonSally Redshaw
    • C07D237/04C07D487/04A61K31/50C07D237/02C07D245/00C07D487/06
    • C07D487/04C07D237/04
    • Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl,as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.
    • 式Ⅰ的化合物,其中R1是氢,烷酰基或芳酰基; R2是氢或烷基; R3是氢或芳基; R4和R5各自为氢或R4和R5一起为氧代; 其中当R 2为氢时,其中R 6为氢,烷基或芳烷基,以及其与碱的药学上可接受的盐及其与Y的药学上可接受的盐,Y为-CH 2 - , - CH 2 CH 2 - 或-N(R 6) 描述了具有抗高血压活性并且可以用作药物制剂形式的药物的-N(R 6) - 。 式I化合物含有至少一个不对称碳原子。 因此,本发明不仅包括这些化合物的光学均匀形式,还包括各种非对映异构体外消旋体和不同非对映异构体外消旋体的混合物。
    • 9. 发明授权
    • Pyridazo[1,2-a][1,2]diazepines
    • 哒唑[1,2-a] [1,2]二氮杂
    • US4512924A
    • 1985-04-23
    • US493876
    • 1983-05-12
    • Michael R. AttwoodCedric H. HassallRobert W. LambertGeoffrey LawtonSally Redshaw
    • Michael R. AttwoodCedric H. HassallRobert W. LambertGeoffrey LawtonSally Redshaw
    • C07D209/48C07D231/04C07D237/04C07D403/06C07D487/04C07F9/38C07F9/40C07F9/6509C07F9/6561C07K5/078
    • C07D209/48C07D231/04C07D237/04C07D403/06C07D487/04C07F9/3886C07F9/409C07F9/650947C07F9/6561C07K5/06139
    • Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylaminoalkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.7 together with the nitrogen atom to which they are attached represent a 5-membered or 6-membered heteromonocyclic ring which may contain a further nitrogen atom or an oxygen or sulphur atom, and n stands for zero, 1 or 2,and pharmaceutically acceptable salts thereof have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations.
    • 新颖的式Ⅰ化合物,其中B代表亚甲基,亚乙基或亚乙烯基,R1代表氢原子或烷基,芳烷基,氨基 - 烷基,单烷基氨基 - 烷基,二烷基氨基烷基,酰氨基 - 烷基,邻苯二甲酰亚氨基 - 烷基 烷氧基羰基氨基 - 烷基,芳氧基羰基氨基 - 烷基,烷基氨基羰基氨基 - 烷基,芳基氨基羰基氨基 - 烷基,芳烷基氨基羰基氨基 - 烷基,烷基磺酰基氨基 - 烷基或芳基磺酰基氨基 - 烷基,R2表示羧基, 图示> R3表示羧基,烷氧基羰基或芳烷氧基羰基,R4和R5各自表示氢原子或R4和R5一起表示氧代基,R6和R7各自表示氢原子或烷基或芳烷基或R6和R7连同 它们所连接的氮原子表示可以含有另外的氮原子或氧的5元或6元杂环, 硫原子,n表示0,1或2,其药学上可接受的盐具有抗高血压活性,可用作药物制剂形式的药物。