公开(公告)号：US5045549A

公开(公告)日：1991-09-03

申请号：US70351

申请日：1987-07-06

申请人： Fritz Sauter ,  Ulrich Jordis ,  Manfred Rudolf ,  Josef Wieser ,  Karl Baumann

发明人： Fritz Sauter ,  Ulrich Jordis ,  Manfred Rudolf ,  Josef Wieser ,  Karl Baumann

IPC分类号： C07D487/18 ,  A61K31/40 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/55 ,  A61P31/04 ,  C07D487/08 ,  C07D519/00

CPC分类号： C07D487/08

摘要： New 4-Pyridone derivatives of General Formula are claimed ##STR1## in which R.sub.1 is methylamino,4-fluorophenyl, 2,4-difluorophenyl, R.sub.2 is hydrogen or a sulfur atom that is joined to the ring nitrogen by an ethylene bride, X is a hydrogen or a physiologically removable ester group and Y is a base of the general formula ##STR2## In formula IIa and IIb, R.sub.3 is hydrogen, lower alkyl, benzyl, formyl, acetonyl or a moiety of the formula ##STR3## Also claimed are the addition salts of compounds of formula I with pharmaceutically acceptable inorganic or organic acids or base and/or their hydrates. Also claimed are the methods of manufacture of compounds of formula I and their use as antibacterial agents.

摘要翻译： 新的通式的4-吡啶酮衍生物要求保护其中R1是甲基氨基，4-氟苯基，2,4-二氟苯基，R2是氢或通过乙烯新娘连接到环氮的硫原子的（I） ，X是氢或生理上可除去的酯基，Y是通式为（IIa）或（IIb）或IIb的碱在式IIa和IIb中，R 3是氢，低级烷基，苄基，甲酰基， 丙酮基或下式的部分还要求保护的是式I化合物与药学上可接受的无机酸或有机酸或碱和/或其水合物的加成盐。 还要求的是制备式I化合物及其作为抗菌剂的用途的方法。

公开(公告)号：US4532136A

公开(公告)日：1985-07-30

申请号：US570225

申请日：1984-01-12

申请人： Wilhelm Sittenthaler ,  Fritz Sauter ,  Peter Stanetty

发明人： Wilhelm Sittenthaler ,  Fritz Sauter ,  Peter Stanetty

IPC分类号： A01N43/40 ,  C07D213/30 ,  C07D213/50

CPC分类号： C07D213/30 ,  A01N43/40 ,  C07D213/50

摘要： 4,4,4-trichloro-(x-pyridyl)-but-2-ene-1-one, wherein x is 2, 3 and 4, and a process for making the same. The compounds are effective fungicides used singly or in combination.

摘要翻译： 4,4,4-三氯 - （x-吡啶基）丁-2-烯-1-酮，其中x为2,3和4，以及其制备方法。 这些化合物是单独使用或组合使用的有效杀真菌剂。

公开(公告)号：US4157399A

公开(公告)日：1979-06-05

申请号：US857134

申请日：1977-12-05

申请人： Fritz Sauter

发明人： Fritz Sauter

IPC分类号： A61K31/38 ,  C07D295/084 ,  C07D295/185 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04

CPC分类号： C07D295/185 ,  C07C323/00 ,  C07D295/092 ,  C07D333/64 ,  C07D333/66

摘要： The present invention relates to new derivatives of 2-phenyl -benzo(b)thiophene mono- or disubstituted on the nitrogen atom of formula ##STR1## in which X.sup.1 to X.sup.9 which are identical or different are hydrogen, alkyl having up to 3 carbon atoms, chlorine, bromine, methoxy or methylthio, R.sup.1 is hydrogen, alkyl having up to 8 carbon atoms, optionally chlorinated or methoxylated, phenyl optionally chlorinated or methoxylated, aralkyl having in all up to 9 carbon atoms, optionally chlorinated or methoxylated on the phenyl nucleus, R.sup.2 is hydrogen, phenyl,Or a radical of the formula ##STR2## in which A is two hydrogen atoms or one oxygen atom andR.sup.3 can assume the same meanings as given for R.sup.1, the meanings assumed by R.sup.1 and R.sup.3 being independent from one another, or R.sup.1 and R.sup.2 together form the radical of a Schiff base of formula.dbd.CH--R.sup.4 (III)in which R.sup.4 is not hydrogen, but can otherwise assume the same meanings as R.sup.3, or the group ##STR3## forms the radical of a heterocyclic secondary amine. The invention also relates to the acid addition salts of the above compounds, notably those which are pharmaceutically compatible. The compounds of formula I are useful in normalizing the blood lipid value.

摘要翻译： 本发明涉及在式（I）的氮原子上单取代或二取代的2-苯基 - 苯并（b）噻吩的新衍生物，其中相同或不同的X 1至X 9为氢，烷基具有至多 3个碳原子，氯，溴，甲氧基或甲硫基，R1是氢，具有至多8个碳原子的烷基，任选被氯化或甲氧基化，任选被氯化或甲氧基化的苯基，具有全部高达9个碳原子的芳烷基，任选氯化或甲氧基化 苯基核，R2是氢，苯基，其中A是两个氢原子或一个氧原子，R3可以表示与R1相同的含义，R1和R3假定为 或者R 1和R 2一起形成其中R 4不是氢的式= CH-R 4（III）的席夫碱的基团，或者可以表示与R 3相同的含义，或者“IMAGE”形式 杂环仲胺的基团。 本发明还涉及上述化合物的酸加成盐，特别是与药学上相容的那些。 式I的化合物可用于标准化血脂值。

公开(公告)号：US4189486A

公开(公告)日：1980-02-19

申请号：US863980

申请日：1977-12-23

申请人： Fritz Sauter ,  Otto Eberle ,  Beate Suss ,  Rudolf Weissgerber

发明人： Fritz Sauter ,  Otto Eberle ,  Beate Suss ,  Rudolf Weissgerber

IPC分类号： A01N43/40 ,  A01N47/12 ,  A01N47/20 ,  C07D213/30 ,  C07D213/89 ,  A01N9/22

CPC分类号： C07D213/89 ,  A01N43/40 ,  A01N47/12 ,  A01N47/20 ,  C07D213/30

摘要： 1-(3-Pyridyl)-2,2,2-trihaloethyl compounds of the general formula I ##STR1## in which n is 0 or 1, R represents oxygen, hydrogen or an organic radical having at the most 12 C-atoms, m is 0 when R is oxygen, m is 1/2 or 1 when R is hydrogen or an aliphatic or aralkyl radical, and X represents a negative ion, R' represents a radical of the general formula II ##STR2## wherein V, Y, Z represent chlorine or bromine and may be identical or different, but are preferably identical; A represents hydrogen or a radical of the general formula III ##STR3## wherein B' is oxygen or sulphur, and B stands for an organic radical having up to 12 C atoms, or for an amino group of the general formula IV ##STR4## wherein F and D are identical or different, and represent hydrogen or organic radicals having at most 12 C-atoms; A may further be a sulphonyl group of the general formula --SO.sub.2 --B, in which B has the same meaning as in formula III. The invention also relates to a process of making the compounds, which are effective ingredients of fungicides and seed-dressing agents.

摘要翻译： 1-（3-吡啶基）-2,2,2-三卤代乙基化合物，其中n为0或1，R代表氧，氢或至多12个C原子的有机基团 当R为氧时，m为0，当R为氢或脂族或芳烷基时，m为1/2或1，X为负离子，R'为通式II的基团，其中V ，Y，Z表示氯或溴，可以相同或不同，但优选相同; A表示氢或通式III的基团III，其中B'是氧或硫，B代表具有至多12个C原子的有机基团，或者表示通式IV的氨基。 IV其中F和D相同或不同，并且表示氢或具有至多12个C原子的有机基团; A还可以是通式-SO 2 -B的磺酰基，其中B具有与式III相同的含义。 本发明还涉及制备化合物的方法，它们是杀真菌剂和拌种剂的有效成分。

公开(公告)号：US4339455A

公开(公告)日：1982-07-13

申请号：US58350

申请日：1979-07-17

申请人： Fritz Sauter ,  Otto Eberle ,  Beate Suss ,  Rudolf Weissgerber

发明人： Fritz Sauter ,  Otto Eberle ,  Beate Suss ,  Rudolf Weissgerber

IPC分类号： A01N43/40 ,  A01N47/12 ,  A01N47/20 ,  C07D213/30 ,  C07D213/89 ,  C07D211/84

CPC分类号： C07D213/89 ,  A01N43/40 ,  A01N47/12 ,  A01N47/20 ,  C07D213/30

摘要： A 1-(3-pyridyl)-2,2,2-trihaloethyl compound of the formula I ##STR1## in which n is 0 or 1, R represents methyl and X is iodide, R' represents a radical of the formula II ##STR2## wherein V, Y and Z each represent a chlorine or bromine atom, A represents a radical of the general formula III ##STR3## in which B' is oxygen or sulphur and B stands for a member of the group consisting of an aliphatic radical having from 1-10 C-atoms of the group consisting of alkenyl radicals and alkyl radicals of the branched and straight chain type, the phenyl radical, an aralkyl radical having from 7-12 C-atoms and an amino group of the general formula IV ##STR4## in which F and D are identical or different, and represent a member of the group consisting of hydrogen, aliphatic radicals of the branched or straight chain type and having from 1-10 C-atoms, the phenyl radical, a substituted phenyl radical containing at least one substituent selected from the group consisting of lower alkoxy, lower alkanoyl, lower alkyl ester, COOH, halogen, lower alkyl, halo lower alkyl, nitro, and hydroxyl, and aralkyl radicals having from 7-12 C-atoms. A also representing a sulphonyl group of the general formula-SO.sub.2 -B, in which B has the same meaning as in formula III. The invention also relates to fungicidal compositions containing the compound according to the invention as active ingredients.

摘要翻译： 式I的1-（3-吡啶基）-2,2,2-三卤代乙基化合物其中n为0或1，R为甲基且X为碘，R'为式II的基团 其中V，Y和Z各自表示氯或溴原子，A表示通式III的基团，其中B'是氧或硫，B代表由以下组成的组的成员： 由具有支链和直链型烯基和烷基的1-10个碳原子的脂族基团，苯基，具有7-12个碳原子的芳烷基和 通式IV其中F和D相同或不同，并且表示由氢，支链或直链型脂肪族基团和具有1-10个C原子的基团的成员，苯基 ，含有至少一个选自以下的取代基的取代苯基：低级烷氧基，低级a 烷酰基，低级烷基酯，COOH，卤素，低级烷基，卤代低级烷基，硝基和羟基，以及具有7-12个C原子的芳烷基。 A也表示通式-SO 2 -B的磺酰基，其中B具有与式III相同的含义。 本发明还涉及含有根据本发明的化合物作为活性成分的杀真菌组合物。