An industrial microbicide and a method for killing microbes for industrial use
    82.
    发明公开
    An industrial microbicide and a method for killing microbes for industrial use 失效
    Industrielle Mikrobizide und Verfahren zur Vernichtung von Mikroben in der Wirtschaft。

    公开(公告)号:EP0571313A2

    公开(公告)日:1993-11-24

    申请号:EP93610031.2

    申请日:1993-05-18

    IPC分类号: A01N37/52

    摘要: An industrial microbicide which comprises at least one haloglyoxime derivative of the formula (I):

    wherein X is a halogen atom; Y is a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; and
    Z is a hydrogen atom or an optionally halogenated lower alkanoyl group having 1 to 5 carbon atoms; and
    a known industrial microbicidal ingredient selected from the group consisting of an organonitrogen-sulfur compound, an organohalogen compound, an organonitrogen compound and an organosulfur compound;
    and optionally a carrier or diluent.
    Also claimed is:
    An industrial microbicide which comprises as an effective ingredient at least one haloglyoxime derivative of the formula (I'):

    wherein X is a halogen atom; Y is a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; and Z' is a hydrogen atom or an optionally halogenated lower alkanoyl group having 1 to 5 carbon atoms; provided that Z' is an optionally halogenated lower alkanoyl group having 1 to 5 carbon atoms when Y is a halogen atom, and optionally a carrier or diluent.

    摘要翻译: 一种工业杀微生物剂,其包含至少一种式(I)的卤代肟衍生物:其中X为卤素原子; Y是氢原子,卤素原子或碳原子数1〜4的低级烷基; Z为氢原子或具有1〜5个碳原子的任选卤化的低级烷酰基; 以及选自有机硫 - 硫化合物,有机卤化合物,有机氮化合物和有机硫化合物的已知的工业杀微生物成分; 和任选的载体或稀释剂。

    Pyridine compounds for treating amnesia
    83.
    发明公开
    Pyridine compounds for treating amnesia 失效
    吡啶化合物用于遗忘症的治疗。

    公开(公告)号:EP0558094A1

    公开(公告)日:1993-09-01

    申请号:EP93103799.8

    申请日:1989-09-13

    摘要: A novel compound of the formula

    wherein R¹ means hydrogen and R² means hydrogen or a straight-chain or branched chain alkyl having 1 to 8 carbon atoms; Ar means phenyl, a phenyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, amino, nitro and cyano, furyl, a furyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano, thienyl, a thienyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano, pyrrolyl, a pyrrolyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano, pyridyl, or a pyridyl substituted by 1 to 3 substituent(s) selected from among halogens, straight-chain or branched chain alkyls having 1 to 8 carbon atoms, straight-chain or branched chain alkoxys having 1 to 8 carbon atoms, trifluoromethyl, straight-chain or branched chain alkylthiols having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfinyls having 1 to 8 carbon atoms, straight-chain or branched chain alkylsulfonyls having 1 to 8 carbon atoms, amino, nitro and cyano: Y means a single bond or a straight-chain or branched chain alkylene having 1 to 8 carbon atoms which may have double bond(s) in the chain; W means a group of the formula (i)

    (wherein R³ and R⁴ are the same or different and respectively mean hydrogen or a halogen, X means -O- or -S-, Z means a single bond or -O-, A is a straight-chain or branched chain alkylene having 1 to 8 carbon atoms, B means -N(R⁸)(R⁹) (wherein R⁸ and R⁹ are the same or different and respectively mean hydrogen or a straight-chain or branched chain alkyl having 1 to 8 carbon atoms, or combinedly means a group forming, taken together with the adjacent nitrogen, 1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, piperidino, 1-piperazinyl, a 1-piperazinyl substituted by a straight-chain or branched chain alkyl having 1 to 8 carbon atoms at the 4-position, 1-homopiperazinyl, morpholino and thiomorpholino) or a group of the formula (ii)

    (wherein R¹² and R¹³ are the same or different and respectively mean hydrogen or a straight-chain or branched chain alkyl having 1 to 8 carbon atoms, P is -S- and Q is hexamethylene, heptamethylene, octamethylene, 1-methylpentamethylene, 1-methylhexamethylene, 1-methylheptamethylene, -(CH₂)₂S(CH₂)₃-, -(CH₂)₂S(CH₂)₆-.

    or

    a pharmaceutically acceptable salt thereof or a hydrate thereof.
    The compounds exhibit inhibitory activity on prolylendopeptidase. Also disclosed are pharmaceutical compositions containing the novel pyridine compounds.

    Optically active thienotriazolodiazepine compounds
    86.
    发明公开
    Optically active thienotriazolodiazepine compounds 失效
    光学活性thienotriazolodiazepine化合物

    公开(公告)号:EP0480455A1

    公开(公告)日:1992-04-15

    申请号:EP91117375.5

    申请日:1991-10-11

    IPC分类号: C07D495/04 A61K31/55

    CPC分类号: C07D495/14

    摘要: Stable crystals of an acid addition salt of an optically active thienotriazolodiazepine compound or its hydrate of the formula

    wherein R 1 is hydrogen, R 2 is 2-phenylethyl substituted by alkyl having 1 to 5 carbon atoms, 2-morpholinocar- bonylethyl or alkyl having 6 to 12 carbon atoms, or R 1 and R 2 may combinedly form a saturated 5-membered ring having one substituent selected from the group consisting of morpholinomethyl, morpholinocarbonyl and N,N-dipropylcarbamoyl, R 3 is halogen, alkyl having 1 to 5 carbon atoms or alkoxy having 1 to 5 carbon atoms, R 4 is trifluoromethyl or alkyl having 1 to 5 carbon atoms, R 5 is hydrogen or methyl, m is 1-2, and n is 0-2. The present invention provides optically active thienotriazolodiazepine compounds having strong PAF-antagonistic activity as markedly stable crystals which are excellent in crystalline property, permit purification by recrystallization, and have high chemical purity and optical purity, thereby rendering industrial large-scale synthesis attainable. In addition, crystallization thereof facilitates medicinal standardization and pharmaceutical formulation.

    摘要翻译: 光学活性噻吩并三唑并二氮杂化合物或其水合物的酸加成盐的稳定晶体,其中R1是氢,R2是被具有1-5个碳原子的烷基取代的2-苯基乙基,2-吗啉代乙基乙基或具有6-12个碳原子的烷基 碳原子,或者R1和R2可以结合形成具有一个选自吗啉代甲基,吗啉代羰基和N,N-二丙基氨基甲酰基的取代基的饱和五元环,R3是卤素,具有1至5个碳原子的烷基或具有1个 至5个碳原子,R4是三氟甲基或具有1至5个碳原子的烷基,R5是氢或甲基,m是1-2,并且n是0-2。 本发明提供具有强PAF-拮抗活性的光学活性噻吩并三唑并二氮杂化合物作为结晶性优异,允许通过重结晶纯化,并具有高化学纯度和光学纯度的显着稳定的晶体,从而可实现工业大规模合成。 此外,其结晶促进了药物标准化和药物制剂。