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1. 发明授权

US4512924A Pyridazo[1,2-a][1,2]diazepines 失效
标题翻译：哒唑[1,2-a] [1,2]二氮杂
公开(公告)号：US4512924A
公开(公告)日：1985-04-23
申请号：US493876
申请日：1983-05-12
申请人： Michael R. Attwood , Cedric H. Hassall , Robert W. Lambert , Geoffrey Lawton , Sally Redshaw
发明人： Michael R. Attwood , Cedric H. Hassall , Robert W. Lambert , Geoffrey Lawton , Sally Redshaw
IPC分类号： C07D209/48 , C07D231/04 , C07D237/04 , C07D403/06 , C07D487/04 , C07F9/38 , C07F9/40 , C07F9/6509 , C07F9/6561 , C07K5/078
CPC分类号： C07D209/48 , C07D231/04 , C07D237/04 , C07D403/06 , C07D487/04 , C07F9/3886 , C07F9/409 , C07F9/650947 , C07F9/6561 , C07K5/06139
摘要： 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.
摘要翻译：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。

2. 发明授权

US4971982A Benzopyran derivatives 失效
公开(公告)号：US4971982A
公开(公告)日：1990-11-20
申请号：US210692
申请日：1988-06-23
申请人： Michael R. Attwood , Philip S. Jones , Sally Redshaw
发明人： Michael R. Attwood , Philip S. Jones , Sally Redshaw
IPC分类号： A61K31/35 , A61K20060101 , A61K31/352 , A61K31/353 , A61K31/44 , A61K31/443 , A61K31/47 , A61K31/495 , A61K31/505 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07C20060101 , C07D213/89 , C07D239/26 , C07D241/12 , C07D311/04 , C07D311/58 , C07D311/62 , C07D405/04
CPC分类号： C07D239/26 , C07D213/89 , C07D241/12 , C07D311/58 , C07D405/04
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, trifluoromethyl, nitro, cyano, lower alkyl, lower alkoxycarbonyl, lower alkylthio, lower alkylsulphonyl, lower alkanoyl, aroyl, carbamoyl, mono(lower alkyl)carbamoyl or di(lower alkyl)carbamoyl, R.sup.2 is hydrogen, lower alkyl or phenyl, R.sup.3 is hydrogen or lower alkyl, R.sup.4 and R.sup.5 each is hydrogen or R.sup.4 is hydroxy and R.sup.5 is hydrogen or R.sup.4 and R.sup.5 together are a carbon-carbon bond and R.sup.6 is an aryl or N-heteroaryl group carrying a hydroxy group in the 2-position or, in the case of a N-heteroaryl group, also a N-oxide group in the 2-position, and pharmaceutically acceptable acid addition salts of these compounds of formula I which are basic, possess pronounced potassium channel activating activity and can be used as medicaments, particularly in the control or prevention of hypertension, congestive heart failure, angina pectoris, peripheral and cerebral vascular disease and smooth muscle disorders.

3. 发明授权

US4920119A Triazine derivatives 失效
标题翻译：三嗪衍生物
公开(公告)号：US4920119A
公开(公告)日：1990-04-24
申请号：US124750
申请日：1987-11-24
申请人： Michael R. Attwood , Peter H. Crackett , Geoffrey Lawton
发明人： Michael R. Attwood , Peter H. Crackett , Geoffrey Lawton
IPC分类号： C07D471/04 , C07D487/04 , C07D513/04
CPC分类号： C07D471/04 , C07D487/04 , C07D513/04
摘要： Compounds of the formula ##STR1## wherein A represents a grouping of the formula ##STR2## in which R.sup.1 and R.sup.2 each individually represent hydrogen, halogen, trifluoromethyl, nitro, amino, cyano, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 14 C.sub.6 -alkanoylamino, aryloxy, aryl-(C.sub.1 -C.sub.6 -alkyl), aryl-(C.sub.1 -C.sub.6 -alkoxy), aryl-(C.sub.1 -C.sub.6 -alkoxy)carbonylamino or a group of the formula --O--CH.sub.2 --R.sup.3 or R.sup.1 and R.sup.2 on adjacent carbon atoms together represent a group of the formula --CH.dbd.CH--CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --O-- and R.sup.3 represents hydroxy-(C.sub.1 -C.sub.4 -alkyl) or vicinal dihydroxy-(C.sub.2 -C.sub.5 -alkyl), and pharmaceutically acceptable acid addition salts of those compounds of formula I in which R.sup.1 and/or R.sup.2 represents amino, possess xanthine oxidase inhibiting activity and can be used as medicaments, particularly for the control or prevention of ischemia or gout. These compounds can be manufactured according to known methods.
摘要翻译：（a）其中A表示下式的组：（a）其中R 1和R 2各自独立地表示氢，卤素，三氟甲基，硝基，（C 1 -C 6）氨基，氰基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 3 -C 6 - 烯氧基，C 1 -C 6 - 烷硫基，C 11 4 C 6 - 烷酰基氨基，芳氧基，芳基 - （C 1 -C 6 - 烷基） C 1 -C 6烷氧基），芳基 - （C 1 -C 6 - 烷氧基）羰基氨基或式-O-CH 2 -R 3基团或相邻碳原子上的R 1和R 2一起表示式-CH = CH-CH = CH - 或-CH 2 -CH 2 -O-和R 3表示羟基 - （C 1 -C 4 - 烷基）或邻位二羟基 - （C 2 -C 5 - 烷基）和其中R 1和/ 或R2表示氨基，具有黄嘌呤氧化酶抑制活性，可用作药物，特别是用于控制或预防缺血或痛风。这些化合物可以根据已知方法制造。

4. 发明授权

US4808713A Anthypertensive pyridazo [1,2-a][1,2]diazepines 失效
标题翻译：高血压哒唑[1,2-a] [1,2]二氮杂
公开(公告)号：US4808713A
公开(公告)日：1989-02-28
申请号：US205405
申请日：1988-06-10
申请人： Michael R. Attwood , Cedric H. Hassall , Robert W. Lambert , Geoffrey Lawton , Sally Redshaw
发明人： Michael R. Attwood , Cedric H. Hassall , Robert W. Lambert , Geoffrey Lawton , Sally Redshaw
IPC分类号： A61K31/50 , A61K31/55 , A61P9/12 , C07D209/48 , C07D231/04 , C07D237/04 , C07D403/06 , C07D487/04 , C07F9/38 , C07F9/40 , C07F9/547 , C07F9/6509 , C07F9/6561 , C07K5/078 , C07D471/06
CPC分类号： C07D209/48 , C07D231/04 , C07D237/04 , C07D403/06 , C07D487/04 , C07F9/3886 , C07F9/409 , C07F9/650947 , C07F9/6561 , C07K5/06139
摘要： 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, dialkylamino-alkyl, 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.
摘要翻译：新颖的式Ⅰ化合物，其中B代表亚甲基，亚乙基或亚乙烯基，R 1表示氢原子或烷基，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，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，式（Ⅰ）或（Ia）中，R 3表示羧基，烷氧基羰基或芳烷氧基羰基，R 4和R 5各自表示氢原子，R 4和R 5一起表示氧基，R 6和R 7各自表示氢原子或烷基或芳烷基或R6和R7与它们所连接的氮原子一起表示可以含有另外的硝基的5元或6元杂单环 n原子或氧或硫原子，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。

5. 发明授权

US4772701A Pyridazo[1,2]pyridazines and pyrazolo[1,2]pyridazines as antihypertensives 失效
标题翻译：哒唑[1,2]哒嗪和吡唑并[1,2]哒嗪作为抗高血压药
公开(公告)号：US4772701A
公开(公告)日：1988-09-20
申请号：US936003
申请日：1986-11-28
申请人： Michael R. Attwood , Cedric H. Hassall , Robert W. Lambert , Geoffrey Lawton , Sally Redshaw
发明人： Michael R. Attwood , Cedric H. Hassall , Robert W. Lambert , Geoffrey Lawton , Sally Redshaw
IPC分类号： C07D209/48 , C07D231/04 , C07D237/04 , C07D403/06 , C07D487/04 , C07F9/38 , C07F9/40 , C07F9/6509 , C07F9/6561 , C07K5/078 , C07D487/06
CPC分类号： C07D209/48 , C07D231/04 , C07D237/04 , C07D403/06 , C07D487/04 , C07F9/3886 , C07F9/409 , C07F9/650947 , C07F9/6561 , C07K5/06139
摘要： 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, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonyl-amino-alkly or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl carbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralykoxycarbonyl 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.
摘要翻译：新颖的式Ⅰ化合物，其中B代表亚甲基，亚乙基或亚乙烯基，R 1表示氢原子或烷基，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，芳烷氧基羰基氨基 - 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，烷氧基羰基或芳烷氧羰基羰基或（ⅰ）<））））））））））;;;;;;;;;;;;;;;;;;;;;;;;;;;;;;;;;;; R6和R7各自表示氢原子或烷基或芳烷基或R6和R7与它们所连接的氮原子一起表示可含有另外的氮原子或氧的5元或6元杂单环，或硫原子，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。

6. 发明授权

US5118694A Benzopyran derivatives 失效
标题翻译：苯并吡喃衍生物
公开(公告)号：US5118694A
公开(公告)日：1992-06-02
申请号：US580881
申请日：1990-09-11
申请人： Michael R. Attwood , Philip S. Jones , Sally Redshaw
发明人： Michael R. Attwood , Philip S. Jones , Sally Redshaw
IPC分类号： A61K31/35 , A61K20060101 , A61K31/352 , A61K31/353 , A61K31/44 , A61K31/443 , A61K31/47 , A61K31/495 , A61K31/505 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07C20060101 , C07D213/89 , C07D239/26 , C07D241/12 , C07D311/04 , C07D311/58 , C07D311/62 , C07D405/04
CPC分类号： C07D239/26 , C07D213/89 , C07D241/12 , C07D311/58 , C07D405/04
摘要： Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, trifluoromethyl, nitro, cyano, lower alkyl, lower alkoxycarbonyl, lower alkylthio, lower alkylsulphonyl, lower alkanoyl, aroyl, carbamoyl, mono(lower alkyl)carbamoyl or di(lower alkyl)carbamoyl, R.sup.2 is hydrogen, lower alkyl or phenyl, R.sup.3 is hydrogen or lower alkyl, R.sup.4 and R.sup.5 each is hydrogen or R.sup.4 is hydroxy and R.sup.5 is hydrogen or R.sup.4 and R.sup.5 together are a carbon-carbon bond and R.sup.6 is an aryl or N-heteroaryl group carrying a hydroxy group in the 2-position or, in the case of a N-heteroaryl group, also a N-oxide group in the 2-position,and pharmaceutically acceptable acid addition salts of these compounds of formula I which are basic, possess pronounced potassium channel activating activity and can be used as medicaments, particularly in the control or prevention of hypertension, congestive heart failure, angina pectoris, peripheral and cerebral vascular disease and smooth muscle disorders.
摘要翻译：下式的化合物其中R 1是氢，卤素，三氟甲基，硝基，氰基，低级烷基，低级烷氧基羰基，低级烷硫基，低级烷基磺酰基，低级烷酰基，芳酰基，氨基甲酰基，单（低级烷基）氨基甲酰基或二（低级烷基）氨基甲酰基，R2是氢，低级烷基或苯基，R3是氢或低级烷基，R4和R5各自是氢或R4是羟基，R5是氢或R4和R5一起是碳 - 碳键，R6是芳基或在2-位上带有羟基的N-杂芳基或2-杂芳基的情况下也是2-位上的N-氧化物基，以及这些式I化合物的药学上可接受的酸加成盐它们是基本的，具有明显的钾通道活化活性，可用作药物，特别是用于控制或预防高血压，充血性心力衰竭，心绞痛，外周和脑血管疾病和平滑肌疾病。

7. 发明授权

US4658024A Pyrazolo [1,2-a][1,2]-diazepines useful as antihypertensives 失效
标题翻译：吡唑并[1,2-a] [1,2] - 二氮杂作为抗高血压药物
公开(公告)号：US4658024A
公开(公告)日：1987-04-14
申请号：US697559
申请日：1985-02-01
申请人： Michael R. Attwood , Cedric H. Hassall , Robert W. Lambert , Geoffrey Lawton , Sally Redshaw
发明人： Michael R. Attwood , Cedric H. Hassall , Robert W. Lambert , Geoffrey Lawton , Sally Redshaw
IPC分类号： C07D209/48 , C07D231/04 , C07D237/04 , C07D403/06 , C07D487/04 , C07F9/38 , C07F9/40 , C07F9/6509 , C07F9/6561 , C07K5/078 , C07D403/04 , A61K31/33 , C07D401/04
CPC分类号： C07D209/48 , C07D231/04 , C07D237/04 , C07D403/06 , C07D487/04 , C07F9/3886 , C07F9/409 , C07F9/650947 , C07F9/6561 , C07K5/06139
摘要： 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, dialkylamino-alkyl, 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.
摘要翻译：新颖的式Ⅰ化合物，其中B代表亚甲基，亚乙基或亚乙烯基，R 1表示氢原子或烷基，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，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，式中，R 3表示羧基，烷氧基羰基或芳烷氧基羰基，R 4和R 5各自表示氢原子或R 4，R 5一起表示氧代基，R 6和R 7各自表示氢原子或烷基或芳烷基，或者R 6和R 7 与它们所连接的氮原子一起表示可以含有另外的氮原子或氧的5元或6元杂单环，或硫原子，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。

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