• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    The hitherto unknown phenylpropargylamine derivative 1-(3,5-bistrifluoromethylphenyl)-3-(4-tert-butyl- piperidino)prop-I-yne, and acid addition salts thereof, have been found to be useful as rodenticides. Processes for the preparation of the new phenylpropargylamine derivative by the application of known methods are described and so are suitable rodenticidal compositions.
    公开号:SU1344228A3
    申请号:SU813287651
    申请日:1981-05-11
    公开日:1987-10-07
    发明作者:Питер Лэфтвис Аллэн；Вильям Парнэлл Эдгар
    申请人:Мей Энд Бейкер Лимитед (Фирма)；
    IPC主号:
    专利说明:

    The invention relates to agriculture, in particular to the control of rodents.
    The purpose of the invention is the higher efficacy of the oral compositions.
    The active ingredient has the general formula
    О-С2ссн - О-с () з
    GZS
    Example 1. Warfarin-resistant rats (Rattus norvesicus) and mice (mus musciilus) taken from
    EXAMPLE 2 Field tests were carried out on warfarin-resistant rats on three forms. Baits were prepared using either medium-ground oatmeal or soaked wheat, into which 0.1% by weight of 1- (3,5-bis-trifluorome-tIlphenyl) -3- (4-tert-butylpiperidin) - -prop -1-ina In those places where running animals were observed, 100-gram portions of food were placed. The amount of food that was eaten by animals every day was determined by weighing, and the presence or absence of rats was judged by the amount of food eaten and by counting the traces of the presence of rats in areas that were peppered with powder for this purpose. The results are summarized in table. 2
    wild populations were kept under laboratory conditions, where they were fed food containing 90% whole-grain oat flour, 5% whole grain flour, and 5% corn oil. After being kept for 4 days on this feed, fro was replaced with a treated feed of the same composition, in which 0.1% by weight of the test compound was introduced, 1- (3,5-bis-trifluoromethyl-phenyl) -3- (4-tert-butylpiperidine) - -prop-1-in hydr ohlor ida.
    In tab. Table 1 shows the results of the determination of the lethal dose of the preparation, which were obtained by observations during a specified period of time from the beginning of feeding with the treated food.
    Table
    one
    40
    table 2
    Continued table. 2
    The total number of dead animals found during the test
    PRI mme
    and e. - - the amount consumed but not fixed.
    From tab. 2 it follows that the amount of feed that is eaten daily is reduced on the quarter of the day of testing by 85 - 97% compared to
    912
    368
    897
    441
    1880
    929
    Note. - - - the number is not defined.
    the amount that was eaten on the first day of testing. Thus, it was found that approximately 80% of the rats that originally lived on the farms died on the fourth test day, as a result of which the number of dead pests in this case significantly exceeded the percentage of dead pests during the same period of time when using anti- coagulant rodenticides.
    15
    about
    Example 3. Field tests were carried out on mice (Mus musculos).
    The pickled bait was placed at three sites infected with mice, and the amount of feed eaten was determined by weighing. Then the non-poisoned bait was removed and replaced with a similar bait, into which 0.1% by weight of the compound was introduced, according to Example 25 (poisoned feed). The amount of poison bait eaten was determined in a similar way, i.e. weighing in over a three week period of time.
    The poison bait was removed and replaced with a non-poison bait, and the amount of eaten non-poison bait was also determined by similar weighing. The results are summarized in table. 3, the degree of pest control effectiveness was calculated by comparing the amounts of non-poisoned bait that were eaten over periods of time before and after using the poison bait.
    Table 3
    thirty
    35
    40
    eleven
    ten
    98.8 98.9
    115
    eleven
    ABOUT
    100
    5134422
    In the examples, preparations of rodenticidal compositions comprising an active substance are given.
    PRI me R 4. The concentrate is prepared by dissolving 2 g of 1- (3,5-bis-trif-ormethylphenyl) -3- (4-tert-butylpiperine) -prop-1-yna in 100 ml of peanut oils. This concentrate can be led into an edible bait in quantities that ensure the concentration of the indicated compound is in the range of 0.001 to 10 wt.%, More preferably 0.05 to 0.2 wt.%, Of the total mass of the bait by mixing ig with grain, cereals, flour, bran, fruit, vegetables, or mom. Such digestible compositions are suitable for use in combating unwanted gnawing by us.
    Example 5. The rodenticide composition is prepared by dissolving 1.0 g of 1- (3,5-bis-trifluoromethylphenyl) -3 - (- 4-tert-butylpiperidine) -prop-1-yna in 25 to 20 ml of acetone with followed by a uniform impregnation with the composition of laboratory rat crumbs (1 kg), which makes it possible to prepare poison bait suitable for use in the fight against unwanted rodents.
    Example 5 g of 1- (355-bis-trifluoromethylphenyl) -3- (4-tert-butyl-piperidine) -prop 1-in hydrochloride is evenly mixed with a mixture of 100 g of sucrose, 30 g of wheat flour and 70 g of corn starch. This powdered concentrate is used to coat pieces of scrap.
    40
    meat, in particular beef and pork, with bait, which is designed to combat unwanted rodents.
    Example 7. A rodenticidal composition is prepared by uniformly mixing 1.0 g of 1- (3,5-bis-trifluoromethyl-phenyl) -3- (4-tert-butylpiperidine) - -prop-1-in hydrochloride, 899 g oat flour, 50 g whole grain flour and 50 g corn oil, these components being thoroughly mixed in a mixer to achieve a uniform distribution of the active and other components throughout the whole mixture, resulting in a bait that is suitable for use in with unwanted rodents. If desired, the composition of this
    g
    5 Q

    0
    5 0 gg
    eight
    compositions can be added with 0.05% by weight of a suitable coloring substance for the purpose of prevention, for example, sky-blue chlorazole.
    Example 1.0 g of 1- (3,5-bis-β-trifluoromethyl-phenyl) -3- (4-tert-butylpiperidine) -prop-1-hydrochloride, 949 g of moistened wholemeal oatmeal and 50 g of sugar are thoroughly mixed in the mixer in order to ensure a uniform distribution of the components throughout the entire mass of the mixture, as a result of which a rodenticide composition is obtained in the form of a bait, which can be used in the fight against undesirable rodents. If desired, a suitable colourant of the cautionary purpose can be added to the composition of the composition, for example, 0.05% by weight of sky-blue chlorazole.
    PRI me R 9. A concentrate is prepared by thoroughly mixing 1- (3,5-bis-trifluoromethylphenyl) -3- (4-tert-butylpiperidine) -prop-1-in hydrochloride (90 g) and flour from whole grains (10 g) in the mixer, so that a uniform distribution of the components in the mixture is achieved.
    The concentrate prepared in this way (100 g) is thoroughly mixed with oat flour (8900 g), whole grain flour (500 g) and corn oil (500 g), mixing is carried out in a mixer to obtain bait, suitable for the destruction of harmful rodents, moreover, the components of the composition are evenly distributed in the bait.
    权利要求:
    Claims (1)
    [1]
    Invention Formula
    A rodenticidal composition comprising an active substance and a carrier, characterized in that 1- (3,5-bis-trifluoromethylphenyl) -3- (4-tert-butsh1-piperidine) -prop-1- is used as an active substance in formulas
     k
    PbC CCH-NQhC (CH3) j
    jC
    and its hydrochloride in the following ratio, wt.%: The active substance is 0.001-90.0
    Carrier10.0-99.999
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    同族专利:
    公开号 | 公开日
    KR830006209A|1983-09-20|
    PT73018B|1982-07-15|
    JPS577467A|1982-01-14|
    CU21474A|1982-08-24|
    PT73018A|1981-06-01|
    EP0041324B1|1983-06-08|
    RO82949B|1984-01-30|
    PH17070A|1984-05-24|
    GB2075978A|1981-11-25|
    CS221830B2|1983-04-29|
    PL231109A1|1982-04-13|
    RO86734A|1985-04-17|
    ZA813127B|1982-05-26|
    DK155320C|1989-09-18|
    DK210081A|1981-11-14|
    AU542214B2|1985-02-14|
    HU190365B|1986-08-28|
    TR21388A|1984-05-10|
    PL128653B1|1984-02-29|
    YU119381A|1983-12-31|
    MA19145A1|1981-12-31|
    MY8500402A|1985-12-31|
    NZ197056A|1983-12-16|
    EP0041324A1|1981-12-09|
    AU7041981A|1981-11-19|
    GR75260B|1984-07-13|
    IE51445B1|1986-12-24|
    US4347252A|1982-08-31|
    DK155320B|1989-03-28|
    ES8203839A1|1982-04-01|
    AR226595A1|1982-07-30|
    OA06808A|1982-12-31|
    IL62838A|1984-06-29|
    CA1158245A|1983-12-06|
    DD160270A5|1983-05-25|
    DE3160415D1|1983-07-14|
    JPH0243739B2|1990-10-01|
    AT3714T|1983-06-15|
    BR8102924A|1982-02-02|
    KR840002065B1|1984-11-09|
    ES502101A0|1982-04-01|
    RO82949A|1984-01-14|
    IL62838D0|1981-07-31|
    IE811032L|1981-11-13|
    RO86734B|1985-05-01|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    WO2012173701A1|2011-06-16|2012-12-20|President And Fellows Of Harvard College|Novel rodent control agents and uses thereof|US3156726A|1961-09-19|1964-11-10|Eastman Kodak Co|Acetylenic amines|
    GB1055548A|1965-08-23|1967-01-18|Acraf|New substituted 1-aryl-3-aminopropynes and process for their preparation|
    US4104383A|1973-11-02|1978-08-01|C M Industries|Derivatives of phenylpropenylamine|
    AR206937A1|1974-09-06|1976-08-31|Lilly Co Eli|PROCEDURE FOR PREPARING 1-SUBSTITUTE-4-ALKYL-4-PHENYL-PIPERIDINE COMPOUNDS|US4871748A|1984-02-08|1989-10-03|May & Baker Limited|Phenylpropargylamine derivatives|
    EP0208919B1|1985-06-14|1994-08-17|Dai Nippon Insatsu Kabushiki Kaisha|Multicolor sublimation type thermal recording method and device therefor|
    JPH01114487A|1987-10-28|1989-05-08|Toppan Printing Co Ltd|Thermal transfer recording medium|
    GB8824050D0|1988-10-13|1988-11-23|Wellcome Found|Antidotes|
    EP1420644B1|2001-08-23|2006-05-31|Bayer CropScience S.A.|Substituted propargylamines|
    GB2410436A|2004-01-30|2005-08-03|Reckitt Benckiser|Rodenticidal bait composition|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    GB8015740|1980-05-13|
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