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25 条记录 (耗时 0.02 秒)

    Imidazole ethyl oxyalkoxy derivatives and thio analogues thereof
    11.
    发明授权
    Imidazole ethyl oxyalkoxy derivatives and thio analogues thereof 失效
    咪唑乙氧基烷氧基衍生物及其硫代类似物

    公开(公告)号：US4177350A

    公开(公告)日：1979-12-04

    申请号：US950825

    申请日：1978-10-12

    申请人： Ludwig Zirngibl ,  Kurt Thiele

    发明人： Ludwig Zirngibl ,  Kurt Thiele

    IPC分类号： A61K31/415 ,  A61P31/04 ,  C07D233/60 ,  C07D233/64 ,  C07D233/94 ,  C07D401/12 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07C323/00 ,  C07D233/56 ,  C07D233/94 ,  C07D249/08 ,  Y10S514/962 ,  Y10S514/967 ,  Y10S514/969

    摘要： Antimycotically and antibacterially effective imidazole derivatives of the formula (1) ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen and lower alkyl; R.sup.4 is hydrogen, lower alkyl or selected from unsubstituted or substituted cycloalkyl, benzyl and phenyl groups wherein the substituents are selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, phenyl, cyano, nitro and amino, or wherein R.sup.4 is an unsubstituted or halosubstituted pyridyl, R.sup.5 is nitro or lower alkyl in any unsubstituted position of the imidazole ring, Ar is a phenyl group optionally substituted with at least one substituent which is halogen, lower alkyl, lower alkoxy or a C.sub.4 -C.sub.8 cycloalkyl, or wherein Ar is a benzyl group optionally substituted with a substituent of the type set forth for R.sup.4, X and Y are independently selected from oxygen (--O--) or sulfur (--S), n is an integer of from 1 to 5 inclusive and p is Zero or an integer of from 1 to 3 inclusive, and the addition salts of formula (1) compounds with pharmaceutically acceptable organic or inorganic acids; the formula (1) compounds and their addition salts as specified have a relatively low oral toxicity or/and an improved solubility and are suitable for use in human and veterinary medicine and for chemo-agricultural fungus control purposes. Suitable pharmaceutical compositions including the novel derivatives or/and their addition salts with acceptable acids as well as methods for producing such novel derivatives are disclosed.

    摘要翻译： 式（1）的抗真菌和抗菌有效的咪唑衍生物其中R 1，R 2和R 3相同或不同，为氢和低级烷基; R4是氢，低级烷基或选自未取代或取代的环烷基，苄基和苯基，其中取代基选自卤素，低级烷基，低级烷氧基，低级烷硫基，苯基，氰基，硝基和氨基，或其中R4是未取代或未取代的 卤素取代的吡啶基，R5是咪唑环的任何未取代的位置的硝基或低级烷基，Ar是任选被至少一个取代基取代的苯基，该取代基是卤素，低级烷基，低级烷氧基或C 4 -C 8环烷基，或其中Ar是 任选被R4，X和Y所示类型的取代基取代的苄基独立地选自氧（-O-）或硫（-S），n为1至5的整数，p为零 或1〜3的整数，式（1）化合物与药学上可接受的有机酸或无机酸的加成盐; 式（1）化合物及其加成盐具有相对较低的口服毒性或/和改善的溶解性，适用于人兽药和化学农药真菌控制目的。 公开了包括新型衍生物和/或其与可接受的酸的加成盐的合适的药物组合物以及用于制备这些新型衍生物的方法。

    Phenoxy alkanoic acid derivatives having the ability to lower the level of fatty substances in the blood
    14.
    发明授权
    Phenoxy alkanoic acid derivatives having the ability to lower the level of fatty substances in the blood 失效
    具有降低血液中脂肪物质水平的能力的苯氧基链烷酸衍生物

    公开(公告)号：US4483999A

    公开(公告)日：1984-11-20

    申请号：US773148

    申请日：1977-03-01

    申请人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    发明人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    IPC分类号： C07C59/68 ,  C07C59/70 ,  C07C69/712 ,  C07D211/46 ,  C07D473/08 ,  C07C69/76

    CPC分类号： C07C321/00 ,  C07C59/68 ,  C07C59/70 ,  C07D211/46 ,  C07D473/08

    摘要： Novel compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, or alkyl or alkoxy containing from 1 to 4 carbon atoms,R.sup.2 is hydrogen, halogen, hydroxy or alkyl of alkoxy containing from 1 to 4 carbon atoms,n and m are integers such that the sum (n+m) lies in the range from 3 to 10 inclusive and n differs from m, andx is alkyl containing from 1 to 4 carbon atoms, hydrogen or a cation which is a metal cation of main Groups 1, 2 and 3 of the Periodic System of the Elements, an organic base cation or an ammonium ion. These compounds have pharmaceutical utility by virtue of their considerable ability to reduce the level of fatty substances in the blood.

    摘要翻译： 式中，R 1为氢，卤素，含有1至4个碳原子的烷基或烷氧基，R2为氢，卤素，羟基或含有1至4个碳原子的烷氧基烷基，n和m的新型化合物 整数，使得和（n + m）在3〜10的范围内，n与m不同，x是含有1〜4个碳原子的烷基，氢或作为主体1的金属阳离子的阳离子 ，元素周期系统的2和3，有机碱性离子或铵离子。 这些化合物由于其相当的降低血液中脂肪物质含量的能力而具有药用效用。

    Cholesterol-lowering phenoxyalkanoic acid esters
    15.
    发明授权
    Cholesterol-lowering phenoxyalkanoic acid esters 失效

    公开(公告)号：US4153803A

    公开(公告)日：1979-05-08

    申请号：US773144

    申请日：1977-03-01

    申请人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    发明人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    IPC分类号： A61K31/22 ,  C07C59/68 ,  C07C59/70 ,  C07C69/712 ,  C07C69/736 ,  C07D211/46 ,  C07D213/30 ,  C07D473/08 ,  C07C69/76

    CPC分类号： C07C321/00 ,  C07C59/68 ,  C07C59/70 ,  C07D211/46 ,  C07D473/08

    摘要： Compounds possessing pharmaceutical activity as substances able to lower the level of fatty substances in the blood possess the following general formula: ##STR1## wherein R represents hydrogen, halogen, hydroxy or alkyl or alkoxy containing from 1 to 4 carbon atoms;A.sup.1 and A.sup.2 which can be the same or different are hydrogen or alkyl containing from 1 to 9 carbon atoms such that A.sup.1 and A.sup.2 contain together not more than 10 carbon atoms,Y is oxygen, in which case X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiary aminoalkoxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, or X is hydrogen and Z is pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, orY is oxygen, X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is alkoxy containing from 1 to 4 carbon atoms, hydroxy or O.sup.- M.sup.+, M being a metal cation of Main Groups I, II or III of the Periodic System of the Elements or an organic base cation or ammonium ion, A.sup.1 and A.sup.2 being the same and being as aforesaid or being different with one of A.sup.1 and A.sup.2 being hydrogen or both being hydrogen and X being a para substituent with respect to Y in the benzene ring in the same general formula,Y is oxygen, X is hydrogen and Z is amine, azacyclohydrocarbyloxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms,Or Y is sulphur, in which case X is hydrogen, benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy, alkoxy containing from 1 to 4 carbon atoms, hydroxy, O.sup.- M.sup.+ wherein M is a metal cation of Main Groups I, II or III of the Periodic System of The Elements or an organic base cation or ammonium ion, cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiaryaminoalkoxy, pivaloyloxyalkoxy or pyridyl-C-alkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, and pharmacologically acceptable acid addition and quaternary ammonium salts of compounds containing basic groups, and optical isomers of said compounds when A.sup.1 and A.sup.2 are different.

    Xanthine oxidase inhibitor and therapeutic treatment using same
    16.
    发明授权
    Xanthine oxidase inhibitor and therapeutic treatment using same 失效
    黄嘌呤氧化酶抑制剂及其治疗方法

    公开(公告)号：US4305942A

    公开(公告)日：1981-12-15

    申请号：US201500

    申请日：1980-10-28

    申请人： Kurt Thiele ,  James S. G. Cox ,  Johanna Fischer ,  Ulrich Jahn

    发明人： Kurt Thiele ,  James S. G. Cox ,  Johanna Fischer ,  Ulrich Jahn

    IPC分类号： A61K31/53 ,  A61K31/535 ,  A61P19/06 ,  A61P43/00 ,  C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/00

    摘要： Therapeutic xanthine oxidase inhibitor composition containing as an active ingredient 3-dimethylamino-7-methyl-1,2-(n-propylmalonyl)-1,2-dihydro-1,2,4-benzotriazine dihydrate of the formula ##STR1## Uratic diathesis in warm-blooded animals is therapeutically treated by administering the aforementioned xanthine oxidase inhibitor to such animals, e.g., human, either orally or by means of an injection, thereby inhibiting their xanthine oxidase activity.

    摘要翻译： 含有下式的作为活性成分的3-二甲基氨基-7-甲基-1,2-（正丙基丙二酰基）-1,2-二氢-1,2,4-苯并三嗪二水合物的治疗性黄嘌呤氧化酶抑制剂组合物 通过以口服或注射方式向这些动物例如人类施用上述黄嘌呤氧化酶抑制剂来治疗温血动物的素质，由此抑制其黄嘌呤氧化酶活性。

    Lipid lowering alkylene glycols and ester derivatives thereof
    17.
    发明授权
    Lipid lowering alkylene glycols and ester derivatives thereof 失效
    脂质降解亚烷基二醇及其酯衍生物

    公开(公告)号：US4275068A

    公开(公告)日：1981-06-23

    申请号：US48536

    申请日：1979-04-23

    申请人： Kurt Thiele ,  Quazi Ahmed ,  Ulrich Jahn ,  Rudolf Adrian

    发明人： Kurt Thiele ,  Quazi Ahmed ,  Ulrich Jahn ,  Rudolf Adrian

    IPC分类号： C07D213/80 ,  A61K31/455 ,  A61K31/60 ,  C07C69/90

    CPC分类号： C07D213/80

    摘要： Novel alkylene glycol derivatives of the formula (1) ##STR1## in which R.sup.1 is the hydrogen atom, an alkyl group having 1-4 C-atoms or an aryl group, R.sup.2 is the hydrogen atom or an alkyl group having 1-4 C-atoms, R.sup.3 is the hydrogen atom or a group of the formula ##STR2## in which Z is an alkyl residue, an optionally substituted aryl residue or a heterocyclic residue and R.sup.4 is a residue of the formula ##STR3## in which R.sup.5 is the hydrogen atom or chlorine atom, or the methyl group, exhibit an advantageous activity in regard of lowering the cholesterol and triglyceride level in the blood. Production of the novel derivatives by reduction of the corresponding acids, or by reacting a phenol of the formula ##STR4## and an alcohol of the formula ##STR5## optionally with subsequent esterification, is described.

    摘要翻译： 式（1）的新型亚烷基二醇衍生物其中R1是氢原子，具有1-4个碳原子的烷基或芳基，R2是氢原子或具有1个碳原子的烷基 -4个C原子，R3是氢原子或其中Z是烷基残基，任选取代的芳基残基或杂环残基的式“IMAGE”的基团，R4是式“IMAGE”的残基，其中 R5是氢原子或氯原子或甲基，在降低血液中的胆固醇和甘油三酯水平方面表现出有利的活性。 描述了通过还原相应的酸或通过使式（IMAGE）的酚与式（IMAGE）的醇任选地随后的酯化反应制备新衍生物。

    2-Amino-3-acylamino-6-benzylamino-pyridine-derivative having antiepileptic action
    19.
    发明授权
    2-Amino-3-acylamino-6-benzylamino-pyridine-derivative having antiepileptic action 失效
    具有抗癫痫作用的2-氨基-3-酰基氨基-6-苄基氨基 - 吡啶衍生物

    公开(公告)号：US4554281A

    公开(公告)日：1985-11-19

    申请号：US545930

    申请日：1983-10-27

    申请人： Walter vonBebenburg, deceased ,  Joachim Heese ,  Jurgen Engel ,  Kurt Thiele

    发明人： Walter vonBebenburg, deceased ,  Joachim Heese ,  Jurgen Engel ,  Kurt Thiele

    IPC分类号： C07D213/74 ,  A61K31/44 ,  A61P25/08 ,  C07D213/75

    CPC分类号： C07D213/75

    摘要： Compounds of the formula ##STR1## where R is a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a phenoxy group or a phenyl-C.sub.1 -C.sub.2 -alkoxy group, R.sub.1 is hydrogen or a C.sub.1 -C.sub.4 -alkyl group and R.sub.5 is hydrogen or a C.sub.1 -C.sub.4 -alkyl group and the groups R.sub.2, R.sub.3, and R.sub.4 are the same or different and are hydrogen, halogen atoms, C.sub.1 -C.sub.4 alkyl groups, C.sub.1 -C.sub.4 -alkylcarbonyl group, the aminosulfonyl group, the trifluoromethyl group and their acid addition salts are effective as antiepileptics.

    摘要翻译： 其中R是C 1 -C 4烷基，C 1 -C 4烷氧基，苯氧基或苯基-C 1 -C 2 - 烷氧基的式Ⅺ化合物，R 1是氢或C 1 -C 4 - 烷基 并且R 5为氢或C 1 -C 4烷基，基团R 2，R 3和R 4相同或不同，为氢，卤素原子，C 1 -C 4烷基，C 1 -C 4烷基羰基，氨基磺酰基， 三氟甲基及其酸加成盐作为抗癫痫药有效。