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22 条记录 (耗时 0.025 秒)

    2-Pyridyl-2-thiazoline-4-carboxylic acid derivatives
    1.
    发明授权
    2-Pyridyl-2-thiazoline-4-carboxylic acid derivatives 失效
    2-吡啶基-2-噻唑啉-4-羧酸衍生物

    公开(公告)号：US4406905A

    公开(公告)日：1983-09-27

    申请号：US285909

    申请日：1981-07-23

    申请人： Hans Zahner ,  Hans-Ulrich Naegeli ,  Heinrich Peter

    发明人： Hans Zahner ,  Hans-Ulrich Naegeli ,  Heinrich Peter

    IPC分类号： C07D213/79 ,  C07D417/04 ,  C07F7/08 ,  C12P17/16 ,  A61K31/44 ,  C07D409/04

    CPC分类号： C07D213/79 ,  C07D417/04 ,  C07F7/0812 ,  C12P17/167 ,  C12R1/48

    摘要： The invention relates especially to 2-(3'-hydroxypyrid-2'-yl)-2-thiazoline-4-carboxylic acid derivatives of the formula (I) and salts and also certain metal complexes of these compounds, processes for their manufacture, pharmaceutical agents containing such compounds and the use of these compounds. ##STR1## In the formula, R.sup.1 represents free, etherified or esterified hydroxy, R.sup.2 represents hydrogen or an aliphatic, carbocyclic or carbocyclic-aliphatic radical having 1-12 carbon atoms, and R.sup.3 represents hydrogen or an unsubstituted aliphatic radical having 1-7 carbon atoms.The compounds of the formula (I) can be used, for example, for the abstraction of heavy metals from the organism of warm-blooded animals and/or they have an antibiotic action.

    摘要翻译： 本发明特别涉及式（I）的2-（3'-羟基吡啶-2'-基）-2-噻唑啉-4-羧酸衍生物及其盐以及这些化合物的某些金属配合物，其制备方法， 含有这些化合物的药剂和这些化合物的用途。 （I）式中，R1表示游离的醚化或酯化的羟基，R 2表示氢或具有1-12个碳原子的脂族，碳环或碳环脂族基，R3表示氢或未取代的具有1个 -7个碳原子。 式（I）的化合物可用于例如从温血动物的生物体中提取重金属和/或具有抗生素作用。

    Esterified hydroxy dihydropyridinones for treating diseases associated with trivalent metal ion overload
    3.
    发明授权
    Esterified hydroxy dihydropyridinones for treating diseases associated with trivalent metal ion overload 失效
    用于治疗与三价金属离子超载相关的疾病的酯化羟基二氢吡啶酮

    公开(公告)号：US4908371A

    公开(公告)日：1990-03-13

    申请号：US265646

    申请日：1988-11-01

    申请人： Theophile Moerker ,  Heinrich Peter

    发明人： Theophile Moerker ,  Heinrich Peter

    IPC分类号： A61K31/435 ,  A61P7/00 ,  A61P31/00 ,  A61P33/02 ,  A61P43/00 ,  C07D213/69

    CPC分类号： C07D213/69

    摘要： 3-Substituted 4(1H)-pyridone compounds of formula ##STR1## wherein R.sub.1 is an unsubstituted or substituted hydrocarbon radical, X is a bond or a group of formula --O-- or --N(R.sub.3)--, wherein R.sub.3 is hydrogen or an unsubstituted or substituted hydrocarbon radical, and R.sub.2 is an unsubstituted or substituted hydrocarbon radical, or wherein R.sub.2 and R.sub.3, when taken together, are an unsubstituted or substituted divalent hydrocarbon radical, and wherein the other ring carbon atoms of the 4(1H)-pyridinone ring, independently of one another, are unsubstituted or substituted by an unsubstituted or substituted hydrocarbon radical or by etherified or esterified hydroxy, and salts of compounds of formula I with salt-forming properties, form chelate-type metal complexes, especially with trivalent metal ions, and can be used, for example, as pharmacologically active compounds.

    摘要翻译： 3-取代的式（I）的4（1H） - 吡啶酮化合物，其中R 1是未取代或取代的烃基，X是式-O-或-N（R 3） - 的键或基团，其中R 3 是氢或未取代或取代的烃基，R 2是未取代或取代的烃基，或其中当R 2和R 3一起为未取代或取代的二价烃基时，其中R 4和R 4的其它环碳原子 1H） - 吡啶酮环，彼此独立地是未取代的或被未取代或取代的烃基或醚化或酯化的羟基取代或具有成盐性的式I化合物的盐形成螯合型金属络合物，特别是 具有三价金属离子，并且可以用作例如药理活性化合物。

    Heteroarylacetamido cephalosporin
    4.
    发明授权
    Heteroarylacetamido cephalosporin 失效
    杂芳基乙酰氨基头孢菌素

    公开(公告)号：US4024249A

    公开(公告)日：1977-05-17

    申请号：US561444

    申请日：1975-03-24

    申请人： Beat Muller ,  Heinrich Peter ,  Peter Schneider ,  Hans Bickel

    发明人： Beat Muller ,  Heinrich Peter ,  Peter Schneider ,  Hans Bickel

    IPC分类号： C07D307/52 ,  C07D307/54 ,  C07D333/22 ,  C07D333/24 ,  C07D501/20

    CPC分类号： C07D307/54 ,  C07D307/52 ,  C07D333/22 ,  C07D333/24 ,  Y02P20/55

    摘要： Novel aminomethyl compounds of the formula ##STR1## wherein X denotes sulphur or oxygen, R denotes hydrogen or an amino protective group, R.sub.1 denotes hydrogen, a free, etherified or esterified hydroxyl group or mercapto group or a substituted ammonium group, R.sub.2 denotes hydroxyl or a carboxyl protective radical which together with the carbonyl grouping of the formula -C(=0)- forms a protected carboxyl group, and their salts, are antibacterial antibiotics or intermediates for the preparation thereof; pharmaceutical preparations containing such active compounds, are useful for combating micro-organisms such as gram-positive or gram-negative bacteria; An illustrative example is 3-acetoxymethyl-7.beta.-[2-(5-aminomethyl-2-thienyl)-acetylamino]-ceph-3-em-4-carboxylic acid.

    摘要翻译： 式（I）的新型氨基甲基化合物其中X表示硫或氧，R表示氢或氨基保护基，R 1表示氢，游离的醚化或酯化的羟基或巯基或 取代的铵基，R2表示羟基或羧基保护基，其与式-C（= O） - 的羰基一起形成被保护的羧基，其盐为抗菌抗生素或其制备的中间体; 含有这种活性化合物的药物制剂可用于对抗微生物如革兰氏阳性或革兰氏阴性细菌; 示例性实例是3-乙酰氧基甲基-7β-[2-（5-氨基甲基-2-噻吩基） - 乙酰氨基] - 头孢-3-烯-4-羧酸。

    N,N-disubstituted ureas and processes for their manufacture
    6.
    发明授权
    N,N-disubstituted ureas and processes for their manufacture 失效
    N，N-二取代脲及其制备方法

    公开(公告)号：US4940811A

    公开(公告)日：1990-07-10

    申请号：US126981

    申请日：1987-11-30

    申请人： Heinrich Peter

    发明人： Heinrich Peter

    IPC分类号： C07C275/16

    CPC分类号： C07C275/16 ,  Y02P20/55

    摘要： N,O-acylates, derived from N-acylated carbamic acids, of desferrioxamine B of the formula ##STR1## in which B represents a carbamoyl radical of the partial formula --CO--NH--Alk--CO--O--R.sub.a.sup.1 (II) in which R.sub.a.sup.1 represents C.sub.1 -C.sub.4 -alkyl or C.sub.2 -C.sub.4 -alkyenyl and Alk represents C.sub.1 -C.sub.7 -alkylene that is optionally substituted by hydroxy, C.sub.1 -C.sub.4 -alkanoyloxy, amino, C.sub.1 -C.sub.4 -alkoxycarbonyl, carbamoyl, phenyl, hydroxyphenyl, methoxyphenyl or by indolyl, and each of the symbols A.sup.1, A.sup.2 and A.sup.3, independently of the others, represents hydrogen, an acyl radical Ac derived from a carboxylic acid, or an above-defined carbamoyl radical of the partial formula II, form strong iron(III) and aluminium complexes in living cells. They can therefore be used therapeutically for the treatment of pathological conditions in warm-blooded animals, including humans, that are associated with an excess of iron(III) or aluminium in the body or are caused by iron(III)-dependent pathogenic organisms. The compounds according to the invention can be obtained, for example, by conventional reaction of desferrioxamine B, or a suitable N- and O-silylated derivative thereof, with an isocyanatoalkanoic acid ester.

    摘要翻译： 衍生自N-酰化的氨基甲酸的N，O-酰化物，其中B表示部分式-CO-NH-Alk-CO-O的氨基甲酰基的式（I）的去铁草胺B -Ra1（II）其中Ra1表示C1-C4-烷基或C2-C4-烷基，Alk表示任选被羟基，C 1 -C 4 - 烷酰氧基，氨基，C 1 -C 4 - 烷氧基羰基，氨基甲酰基 ，苯基，羟基苯基，甲氧基苯基或吲哚基，符号A1，A2和A3各自独立地代表氢，衍生自羧酸的酰基酰基或上述定义的部分式 II，在活细胞中形成强铁（III）和铝络合物。 因此，它们可用于治疗温血动物（包括人）中与过量的铁（III）或铝在体内或由铁（III）依赖的致病生物体引起的病理状况的治疗。 根据本发明的化合物可以例如通过脱铁三胺B或其合适的N-和O-甲硅烷基化衍生物与异氰酸根合链烷酸酯的常规反应获得。

    3-R-methyl-7-amino-ceph-em-4-carboxylic acid compounds
    7.
    发明授权
    3-R-methyl-7-amino-ceph-em-4-carboxylic acid compounds 失效
    3-R-甲基-7-氨基 - 头孢烯-4-羧酸化合物

    公开(公告)号：US3932465A

    公开(公告)日：1976-01-13

    申请号：US159527

    申请日：1971-07-02

    申请人： Heinrich Peter ,  Herman Robert Rodriguez ,  Hans Bickel

    发明人： Heinrich Peter ,  Herman Robert Rodriguez ,  Hans Bickel

    IPC分类号： C07D501/20

    CPC分类号： C07D501/04

    摘要： 3-R-Methyl-7-amino-ceph-2-em-4.xi.-carboxylic acid compounds, in which R is the C-residue of a C-nucleophilic compound are valuable intermediates, for example, in the manufacture of the corresponding 3-R-methyl-7-amino-ceph-3-em-4-carboxylic acid compounds with antibiotic properties.

    摘要翻译： 其中R为C-亲核化合物的C-残基的3-R-甲基-7-氨基 - 头孢烯-2-em-4 xi-羧酸化合物是有价值的中间体，例如制备相应的 具有抗生素性质的3-R-甲基-7-氨基 - 头孢-3-烯-4-羧酸化合物。

    8-Oxo-5-thia-1-azabicyclo(4,2,0)oct-2-ene compounds
    9.
    发明授权
    8-Oxo-5-thia-1-azabicyclo(4,2,0)oct-2-ene compounds 失效
    8-氧代-5-硫杂-1-氮杂双环（4,0,0）辛-2-烯化合物

    公开(公告)号：US4430498A

    公开(公告)日：1984-02-07

    申请号：US227832

    申请日：1981-01-23

    申请人： Karl Heusler ,  Hans Bickel ,  Bruno Fechtig ,  Heinrich Peter ,  Riccardo Scartazzini

    发明人： Karl Heusler ,  Hans Bickel ,  Bruno Fechtig ,  Heinrich Peter ,  Riccardo Scartazzini

    IPC分类号： A61K31/545 ,  C07D501/18 ,  C07D501/20

    CPC分类号： C07D501/20 ,  C07D501/18 ,  Y02P20/55

    摘要： The invention concerns 7-amino-ceph-3-em-4-carboxylic acid compounds of the formula ##STR1## wherein R.sub.1.sup.a represents hydrogen or an amino protective group R.sub.1.sup.A and R.sub.1.sup.b represent hydrogen or an acyl group Ac, or R.sub.1.sup.A and R.sub.1.sup.b together denote a bivalent amino protective group, and R.sub.2 represents hydrogen or an organic radical R.sub.2.sup.A which together with the --C(.dbd.O)--O-- grouping forms a protected carboxyl group, or salts such compounds which possess salt-forming groups; these compounds have antibiotic properties.

    摘要翻译： 本发明涉及下式的7-氨基 - 头孢-3-烯-4-羧酸化合物，其中R 1a表示氢或氨基保护基R1A和R 1b表示氢或酰基Ac或R 1A和 R1b一起表示二价氨基保护基，R2表示氢或与-C（= O）-O-基团一起形成保护的羧基的有机基团R2A，或具有成盐基团的盐的盐; 这些化合物具有抗生素特性。