Substituted 1-(4-piperidyl)-3-(aryl) isothioureas their preparation and their therapeutic application
    1.
    发明授权
    Substituted 1-(4-piperidyl)-3-(aryl) isothioureas their preparation and their therapeutic application 失效
    取代的1-(4-哌啶基)-3-(芳基)异硫脲的制备及其治疗应用

    公开(公告)号:US06531469B1

    公开(公告)日:2003-03-11

    申请号:US09889805

    申请日:2001-07-20

    IPC分类号: C07D41712

    CPC分类号: C07D413/12 C07D417/12

    摘要: The invention concerns novel substituted N-benzo(thia/oxa)zines-2-yl-1-arylalkyloxyalkyl-4-piperidinamine, their preparation and their therapeutic use. The invention concerns compounds of formula (1) wherein: X represents an oxygen or sulphur atom; Y represents either an alkylene radical, branched or not and containing 2 to 6 carbon atoms or a CH2—CH(OH)—CH2— radical. R represents a hydrogen, an alkyl radical, branched or not and containing 1 to 7 carbon atoms; R1 to R6, identical or different, represent a hydrogen, a saturated or unsaturated alkyl, branched or not and containing 1 to 5 carbon atoms, a saturated or unsaturated alkyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or acyloxy group comprising 2 to 3 carbon atoms, an alkylamino group containing 1 to 5 carbon atoms, a trifluoro methyl or trifluoro methoxyl group; n is an integer ranging from 1 to 6 inclusively, and their pure, enantiomers or their mixtures, the therapeutically acceptable mineral and organic salts of the compounds of formula (1) and their possible hydrates.

    摘要翻译: 本发明涉及新型取代的N-苯并(噻唑/氧杂)嗪-2-基-1-芳基烷氧基烷基-4-哌啶胺及其制备及其治疗用途。 本发明涉及式(1)的化合物,其中:X表示氧或硫原子; Y表示亚烷基,支链或不支链,含有2-6个碳原子或CH2-CH(OH)-CH2-基。 R表示氢,烷基,支链或不支链,含有1至7个碳原子; R 1至R 6相同或不同,表示氢,饱和或不饱和的烷基,支链或不含并且含有1至5个碳原子,饱和或不饱和烷氧基,支链或不具有1至5个碳原子,卤代,硝基 ,含有2〜3个碳原子的羟基,酰基或酰氧基,含1至5个碳原子的烷基氨基,三氟甲基或三氟甲氧基; n是1至6的整数,以及它们的纯的对映体或它们的混合物,式(1)化合物的治疗上可接受的矿物和有机盐及其可能的水合物。

    Benzoxathiepine derivatives and their use as medicines
    2.
    发明授权
    Benzoxathiepine derivatives and their use as medicines 有权
    苯并噻肟衍生物及其作为药物的用途

    公开(公告)号:US07109234B2

    公开(公告)日:2006-09-19

    申请号:US10472728

    申请日:2002-03-20

    IPC分类号: A61K31/38 C07D327/00

    CPC分类号: C07C323/22 C07D327/02

    摘要: The invention concerns 3-arylthio-propyl-amino-3,4-dihydro-2H-1,5-aryloxathiepin derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a hydrogen atom, a fluorine atom or a chlorine atom, a hydroxy group, an alkyl, cyclopropyl, alkoxy, cyclopropoxy radical or when they occupy adjacent positions, form with the carbon atoms bearing them a carbon-containing cycle or an oxygen-containing heterocycle with five non-aromatic rings; R3 represents an alkyl radical, a hydroxy group or a methoxy radical; R4 represents a hydrogen atom or a methyl radical; and R5 and R6, identical or different represent a hydrogen atom, an alkyl, alkoxy, alkylthio, alkylamino radical, or the groups OR4 and R5 form with the carbons which bear them a non-aromatic heterocycle with five or six rings containing at least an oxygen atom; and their pharmaceutically acceptable additions salts

    摘要翻译: 本发明涉及通式(I)的3-芳硫基 - 丙基 - 氨基-3,4-二氢-2H-1,5-芳基硫代吗啉衍生物,其中:R 1和R 2相同或不同,表示氢原子,氟原子 或者当氯原子,羟基,烷基,环丙基,烷氧基,环丙氧基或当它们占据相邻位置时,与带有碳环的碳原子一起形成含有五个非芳香环的含氧杂环; R3表示烷基,羟基或甲氧基; R4表示氢原子或甲基; 并且R 5和R 6相同或不同地表示氢原子,烷基,烷氧基,烷硫基,烷基氨基或OR 4和R 5基团与与其形成非芳族杂环的碳一起形成,所述非芳族杂环具有至少包含至少一个 氧原子 及其药学上可接受的添加盐

    Substitute 1-(piperidin-4-yl)-3-(aryl)-isothioureas, their preparation and therapeutic use
    3.
    发明授权
    Substitute 1-(piperidin-4-yl)-3-(aryl)-isothioureas, their preparation and therapeutic use 失效
    替代1-(哌啶-4-基)-3-(芳基) - 异硫脲,其制备和治疗用途

    公开(公告)号:US06583159B1

    公开(公告)日:2003-06-24

    申请号:US09889811

    申请日:2001-07-20

    IPC分类号: A61K31445

    CPC分类号: C07D211/58

    摘要: The invention concerns compounds of formula (I) wherein: R1 and R2, identical or different, represent a saturated or unsaturated alkyl radical, branched or not and containing 1 to 7 carbon atoms; R3 to R8, identical or different, represent a hydrogen, an alkyl branched or not and containing 1 to 5 carbon atoms, an acyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or alkoxy group containing 1 to 5 carbon atoms, a dialkylamino group containing 1 to 5 carbon atoms, a trifluoromethyl or trifluoro methoxyl group; Z represents an oxygen or sulphur atom or methylene; m represents an integer between 0 and 4 inclusively; n represents an integer between 2 and 7 inclusively; and their pure enantiomers and mixtures, the therapeutically acceptable mineral or organic salts of the compounds of formula (I) and their possible hydrates.

    摘要翻译: 本发明涉及式(I)的化合物,其中:R 1和R 2相同或不同,表示饱和或不饱和的烷基,分支或不具有1至7个碳原子; R3至R8相同或不同,表示氢,支链或不支链,含有1至5个碳原子的烷基,酰氧基,支链或不支化,含有1至5个碳原子,卤代,硝基,羟基,酰基或烷氧基 含有1至5个碳原子的二烷基氨基,含有1至5个碳原子的二烷基氨基,三氟甲基或三氟甲氧基; Z表示氧或硫原子或亚甲基; m表示0和4之间的整数; n表示2〜7的整数, 和它们的纯对映异构体和混合物,式(I)化合物的治疗上可接受的矿物或有机盐及其可能的水合物。

    Fuel composition producing a colored flame
    4.
    发明授权
    Fuel composition producing a colored flame 失效
    燃料组成产生着色的火焰

    公开(公告)号:US06419713B1

    公开(公告)日:2002-07-16

    申请号:US09600741

    申请日:2001-01-05

    IPC分类号: C10L700

    CPC分类号: C11C5/004

    摘要: The invention concerns a solid or liquid fuel composition capable while burning of producing a selected and varied colored flame other than the color of a standard flame. The composition comprises triethanolamine and a color-forming agent. The invention also concerns a candle or lighting device with a colored flame prepared from the composition. The invention further concerns a method for making a candle with a colored flame comprising the steps of casting the composition into a mold wherein a wick has previously been fixed, cooling the cast composition, and removing the cooled composition from the mold.

    摘要翻译: 本发明涉及一种固体或液体燃料组合物,其能够在燃烧时产生除了标准火焰的颜色之外的选定和变化的着色火焰。 组合物包含三乙醇胺和成色剂。 本发明还涉及一种具有由组合物制备的着色火焰的蜡烛或照明装置。 本发明还涉及一种制造具有着色火焰的蜡烛的方法,其包括以下步骤:将组合物浇铸到模具中,其中预先将灯芯固定,冷却铸造组合物,并从模具中除去冷却的组合物。

    Heterocyclic compounds for treating myocardial ischemia
    5.
    发明授权
    Heterocyclic compounds for treating myocardial ischemia 失效
    用于治疗心肌缺血的杂环化合物

    公开(公告)号:US6011032A

    公开(公告)日:2000-01-04

    申请号:US11207

    申请日:1998-01-26

    CPC分类号: C07D413/12 C07D417/12

    摘要: Substituted N-heterocyclyl-1-aryloxyalkyl-4-piperldineamines of formula (I) ##STR1## wherein each of R.sub.1 to R.sub.4, which are the same or different, is hydrogen, optionally branched C.sub.1-4 alkyl, optionally branched C.sub.1-4 alkyloxy, halo, nitro, hydroxy, or trifluoromethyl or trifluoromethoxyl; R.sub.5 is hydrogen, optionally branched C.sub.1-6 alkyl, optionally branched C.sub.7-12 phenylalkyl optionally substituted on the phenyl by one or more radicals having the same definition as R.sub.1 ; W and X are oxygen or sulphur; Y is C.sub.2-6 polymethylene or --CH.sub.2 --CH(OH)--CH.sub.2 --; and n is 0 or 1; and pure R or S isomers of said compounds, where applicable, as well as mixtures thereof, as well as therapeutically-acceptable organic or inorganic salts and hydrates of the compounds and a method for preparing the compounds and their use as drugs are all disclosed.

    摘要翻译: PCT No.PCT / FR96 / 01176 Sec。 371日期1998年1月26日 102(e)1998年1月26日PCT PCT 1996年7月25日PCT公布。 出版物WO97 / 05134 日期1997年2月13日,式(I)的取代的N-杂环基-1-芳氧基烷基-4-哌嗪胺其中R 1至R 4各自相同或不同,为氢,任选支链C 1-4烷基,任选支链C1- 4-烷氧基,卤素,硝基,羟基或三氟甲基或三氟甲氧基; R 5是氢,任选支链的C 1-6烷基,任意支化的C 7-12苯基烷基,其在苯基上被一个或多个与R 1相同定义的基团取代; W和X是氧或硫; Y为C2-6多亚甲基或-CH2-CH(OH)-CH2-; 并且n为0或1; 并且所有化合物的纯R或S异构体,如适用,以及其混合物,以及化合物的治疗上可接受的有机或无机盐和水合物,以及制备化合物的方法及其作为药物的用途。