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公开(公告)号：US4127649A
公开(公告)日：1978-11-28
申请号：US799791
申请日：1977-05-23
申请人： Frank R. Atherton , Michael J. Hall , Cedric H. Hassall , Peter S. Ringrose , Robert W. Lambert
发明人： Frank R. Atherton , Michael J. Hall , Cedric H. Hassall , Peter S. Ringrose , Robert W. Lambert
CPC分类号： C08G69/10 , A61K31/66 , C07F9/301 , C07F9/4006 , C07K5/06191 , A61K38/00
摘要： Compositions having antibiotic properties containing as antibiotic potentiators peptides of the formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl, lower cycloalkyl, (lower cycloalkyl)-(lower alkyl), aryl or aryl-(lower alkyl) group (said group being optionally substituted as the case may require by one or more amino, hydroxy, thio, methylthio, carboxy or guanidino groups so as to form the characterizing group of a naturally occurring L .alpha.-amino acid);R.sup.2 and R.sup.3 each represent the characterizing group of an .alpha.-amino acid of the type normally found in proteins with the proviso that R.sup.3 cannot represent a hydrogen atom when n is zero and R.sup.1 is a hydrogen atom or the phenyl group; R.sup.4 represents a hydroxy or methyl group; n stands for zero, 1, 2 or 3; and single asterisks denote that the configuration at the carbon atom so-marked is L when R.sup.2 or R.sup.3 as the case may be represents other than a hydrogen atom; and the double asterisk denotes that, when R.sup.1 represents other than a hydrogen atom, the configuration at the carbon atom so-marked is (R) (as hereinafter defined),And an antibiotic are disclosed.
摘要翻译： 具有抗生素特性的组合物，其含有下式的抗生素增效剂肽：其中R 1表示氢原子或低级烷基，低级环烷基，（低级环烷基） - （低级烷基），芳基或芳基 - （低级烷基） 基团可以被一个或多个氨基，羟基，硫代，甲硫基，羧基或胍基基团任选取代，以形成天然存在的Lα-氨基酸的表征基团）; R2和R3各自表示通常在蛋白质中发现的α-氨基酸的表征基团，条件是当n为0且R 1为氢原子或苯基时，R 3不能表示氢原子; R4表示羟基或甲基; n代表零，1,2或3; 并且单个星号表示当R2或R3表示除氢原子之外时，所标示的碳原子上的构型为L; 并且双星号表示当R1表示除氢原子以外的情况下，所示标记的碳原子上的构型为（R）（如下文定义），并且具有抗菌活性。
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公开(公告)号：US4808713A
公开(公告)日：1989-02-28
申请号：US205405
申请日：1988-06-10
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。
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13.发明授权Pyridazo[1,2]pyridazines and pyrazolo[1,2]pyridazines as antihypertensives 失效哒唑[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
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。
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公开(公告)号：US4134972A
公开(公告)日：1979-01-16
申请号：US850742
申请日：1977-11-11
申请人： Frank R. Atherton , Michael J. Hall , Cedric H. Hassall , Peter S. Ringrose , Robert W. Lambert
发明人： Frank R. Atherton , Michael J. Hall , Cedric H. Hassall , Peter S. Ringrose , Robert W. Lambert
CPC分类号： C08G69/10 , A61K31/66 , A61K38/04 , C07F9/301 , C07F9/4006 , Y10S930/19 , Y10S930/29
摘要： Compositions having antibiotic properties containing as antibiotic potentiators peptides of the formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl, lower cycloalkyl, (lower cycloalkyl)-(lower alkyl), aryl or aryl(lower alkyl) group (said group being optionally substituted as the case may require by one or more amino, hydroxy, thio, methylthio, carboxy or guanidino groups so as to form the characterizing group of a naturally occurring L .alpha.-amino acid);R.sup.2 and R.sup.3 each represent the characterizing group of an .alpha.-amino acid of the type normally found in proteins with the proviso that R.sup.3 cannot represent a hydrogen atom when n is zero and R.sup.1 is a hydrogen atom or the phenyl group; R.sup.4 represents a hydroxy or methyl group; n stands for zero, 1, 2 or 3; and single asterisks denote that the configuration at the carbon atom so-marked is L when R.sup.2 or R.sup.3 as the case may be represents other than a hydrogen atom; and the double asterisk denotes that, when R.sup.1 represents other than a hydrogen atom, the configuration at the carbon atom so-marked is (R) (as hereinafter defined), and an antibiotic are disclosed.
摘要翻译： 具有抗生素特性的组合物，其含有下式的抗生素增强剂肽：其中R 1表示氢原子或低级烷基，低级环烷基，（低级环烷基） - （低级烷基），芳基或芳基（低级烷基） 根据情况可以通过一个或多个氨基，羟基，硫代，甲硫基，羧基或胍基进行取代，以形成天然存在的Lα-氨基酸的表征基团）; R2和R3各自表示通常在蛋白质中发现的α-氨基酸的表征基团，条件是当n为0且R 1为氢原子或苯基时，R 3不能表示氢原子; R4表示羟基或甲基; n代表零，1,2或3; 并且单个星号表示当R2或R3表示除氢原子之外时，所标示的碳原子上的构型为L; 并且双星号表示当R 1表示除氢原子以外时，所示标记的碳原子上的构型为（R）（如下文定义），并且公开了抗生素。
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