Triazole derivatives
    21.
    发明申请
    Triazole derivatives 失效
    三唑衍生物

    公开(公告)号:US20060211750A1

    公开(公告)日:2006-09-21

    申请号:US11226677

    申请日:2005-09-14

    IPC分类号: A61K31/422 C07D413/02

    CPC分类号: C07D413/12

    摘要: The present invention relates to the compounds of formula I their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, compositions containing such compounds and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.

    摘要翻译: 本发明涉及式I化合物的药学上可接受的盐或酯,对映体形式,非对映异构体和外消旋物,上述化合物的制备,含有这些化合物的组合物及其制备方法以及这些化合物在 控制或预防癌症等疾病。

    Pyrazolo(3,4-d)pyrimidine compounds, compositions and method of use
    23.
    发明授权
    Pyrazolo(3,4-d)pyrimidine compounds, compositions and method of use 失效
    吡唑并(3,4-d)嘧啶化合物,组合物和使用方法

    公开(公告)号:US4904666A

    公开(公告)日:1990-02-27

    申请号:US181729

    申请日:1988-04-14

    CPC分类号: C07D487/04

    摘要: The present invention provides pyrazolo[3,4-d]-pyrimidines of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 to C.sub.6 -alkyl radical, a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aryl radical, R.sub.2 is a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aralkyl or hetaralkyl radical with 1 to 6 carbon atoms in the alkyl moiety and substituted, if desired, one or more times by halogen, C.sub.1 to C.sub.6 -alkyl, hydroxyl, C.sub.1 to C.sub.6 -alkoxy, C.sub.1 to C.sub.3 -haloalkyl, C.sub.3 to C.sub.7 -alkoxy carbonyl, aminocarbonyl, C.sub.2 to C.sub.7 -alkylaminocarbonyl, C.sub.3 to C.sub.13 -dialkylaminocarbonyl, cyano or C.sub.1 to C.sub.6 -alkylthio and R.sub.3 is a hydrogen atom or a C.sub.2 to C.sub.6 -alkyl radical substituted, if desired, one or more times by hydroxyl or is a tetrahydrofuranyl or tetrahydropyranyl radical, with the proviso that R.sub.2 cannot be an unsubstituted benzyl radical when R.sub.1 is a methyl radical, and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

    摘要翻译: 本发明提供通式如下的吡唑并[3,4-d] - 嘧啶:其中R 1为C 1至C 6 - 烷基,C 2至C 6链烯基,C 3至C 7环烷基 基团或芳基,R 2是C 2至C 6 - 烯基,C 3至C 7 - 环烷基或在烷基部分具有1至6个碳原子的芳烷基或杂烷基,如果需要, 卤素,C1至C6烷基,羟基,C1至C6烷氧基,C1至C3-卤代烷基,C3至C7-烷氧基羰基,氨基羰基,C2至C7-烷基氨基羰基,C3至C13-二烷基氨基羰基,氰基或C1至C6-烷硫基 并且R 3是氢原子或C 2至C 6烷基如果需要,被羟基取代一次或多次,或者是四氢呋喃基或四氢吡喃基,条件是当R 1是甲基时,R 2不能是未被取代的苄基 ,以及其与无机和有机酸的生理上可接受的盐。 本发明还提供了制备这些化合物的方法和含有它们的药物组合物。

    N.sup.6 -disubstituted purine derivatives, and pharmaceutical
compositions containing them, useful for treating allergic diseases,
bronchospastic and bronchoconstrictory conditions
    24.
    发明授权
    N.sup.6 -disubstituted purine derivatives, and pharmaceutical compositions containing them, useful for treating allergic diseases, bronchospastic and bronchoconstrictory conditions 失效
    N6-二取代嘌呤衍生物和含有它们的药物组合物,其可用于治疗过敏性疾病,支气管痉挛和支气管收缩条件

    公开(公告)号:US4853386A

    公开(公告)日:1989-08-01

    申请号:US897109

    申请日:1986-08-15

    摘要: The present invention provides N.sup.6 -disubstituted purine derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.4 are the same or different and each represents a hydrogen or halogen atom or an --NR.sub.6 R.sub.7 group, R.sub.2 and R.sub.3 are the same or different and each represents a C.sub.1 -C.sub.6 alkyl radical, a C.sub.2 -C.sub.6 alkenyl radical, a C.sub.3 -C.sub.7 cycloalkyl radical, a phenalkyl radical containing up to 4 carbon atoms in the alkyl moiety, which can be straight-chained or branched, the phenyl moiety of which can be substituted one or more times by halogen, hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio or trifluoromethyl; a furylmethyl or furylethyl radical, a thiophenemethyl or thiopheneethyl radical, a pyridylmethyl or pyridylethyl radical optionally substituted by a C.sub.1 -C.sub.4 alkyl radical, an indanyl radical or a tetrahydronaphthyl radical, R.sub.5 is a hydrogen atom, a tetrahydrofuranyl or tetrahydropyranyl radical or a C.sub.1 -C.sub.10 radical which is optionally substituted one or more times by hydroxyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.2 -C.sub.6 carboxyalkanoyloxy, C.sub.2 -C.sub.6 hydroxyalkoxy, C.sub.3 -c.sub.6 dihydroxyalkoxy, carboxyl, cyano or 1H-tetrazol-5-yl radical, R.sub.6 and R.sub.7 are the same or different and each represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical or together represent a C.sub.2 -C.sub.5 alkylene radical optionally interrupted by oxygen, sulphur or an NR.sub.8 group and R.sub.8 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical; as well as the pharmacologically acceptable salts thereof.

    摘要翻译: 本发明提供以下通式的N6-二取代的嘌呤衍生物:其中R 1和R 4相同或不同,并且各自表示氢或卤素原子或-NR 6 R 7基团,R 2和R 3相同或不同, 各自表示C1-C6烷基,C2-C6链烯基,C3-C7环烷基,在烷基部分含有至多4个碳原子的苯烷基,其可以是直链或支链的,苯基 其部分可以被卤素,羟基,C 1 -C 6烷基,C 1 -C 6烷氧基,C 1 -C 6烷硫基或三氟甲基取代一次或多次; 呋喃基甲基或呋喃乙基,噻吩甲基或噻吩乙基,任选被C 1 -C 4烷基,茚满基或四氢萘基取代的吡啶基甲基或吡啶基,R5是氢原子,四氢呋喃基或四氢吡喃基或C1- C 1 -C 6烷氧基,C 1 -C 6烷氧基羰基,C 2 -C 6羧基烷酰氧基,C 2 -C 6羟基烷氧基,C 3 -C 6二羟基烷氧基,羧基,氰基或1H-四唑-5-基 ,R6和R7相同或不同,各自表示氢原子或C1-C6烷基,或一起代表任选被氧,硫或NR8基中断的C2-C5亚烷基,R8是氢原子或C1 -C6烷基; 以及其药理学上可接受的盐。

    Dibenz�b,e!oxepin derivatives and pharmaceutical agents which contain
them
    27.
    发明授权
    Dibenz�b,e!oxepin derivatives and pharmaceutical agents which contain them 失效
    二苯并[b,e] oxepin衍生物和含有它们的药剂

    公开(公告)号:US5696155A

    公开(公告)日:1997-12-09

    申请号:US632473

    申请日:1996-09-10

    CPC分类号: C07D493/04 C07D313/12

    摘要: Compounds of formula I ##STR1## in which Q denotes hydrogen, a hydroxy group or a C.sub.1 to C.sub.8 alkoxy group which can be substituted if desired, by carboxyl or C.sub.1 to C.sub.6 alkoxycarbonyl and either Y and Z together form a group ##STR2## and X represents hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.2 to C.sub.6 alkenyl or Y and X together form a group ##STR3## or an alkylene residue of 2-4 carbon atoms and Z represents hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.1 to C.sub.6 alkanoyl, where R denotes hydrogen or a C.sub.1 to C.sub.6 alkyl residue as well as physiologically tolerated salts thereof, processes for their production and pharmaceutical agents containing these compounds for the treatment of inflammatory diseases and allergic diseases.

    摘要翻译: PCT No.PCT / EP94 / 03479 371日期:1996年9月10日 102(e)1996年9月10日PCT PCT日期:1994年10月22日PCT公布。 公开号WO95 / 11906 日期:1995年5月4日,式I的化合物(I)其中Q表示氢,羟基或可根据需要被取代的C 1至C 8烷氧基,由羧基或C 1至C 6烷氧基羰基以及Y和Z一起 形成基团,X表示氢,C 1至C 6烷基或C 2至C 6烯基或Y和X一起形成基团Z表示氢,C 1至C 6烷基或C 1至C 6烷酰基,其中R表示氢或 C1至C6烷基残基以及其生理上耐受的盐,其制备方法和含有这些化合物用于治疗炎症性疾病和过敏性疾病的药剂。

    Pyrrolobenzimidazoles and pharmaceutical compositions containing them
    28.
    发明授权
    Pyrrolobenzimidazoles and pharmaceutical compositions containing them 失效
    吡咯并苯并咪唑和含有它们的药物组合物

    公开(公告)号:US4863945A

    公开(公告)日:1989-09-05

    申请号:US131367

    申请日:1987-12-10

    CPC分类号: C07D487/04

    摘要: Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.

    摘要翻译: 下式的吡咯并苯并咪唑:可用于治疗心脏和循环系统疾病。 R1是取代的苯基; 或任选取代的萘基或可与苯环缩合形成双环基团的五元或六元杂环基。 R2是氢,烷基,烯基或环烯基; R3是烷基,烯基或羟基烷基或与R2一起形成亚环烷基; 或者R 2和R 3一起形成亚烷基或亚环烷基。 R4是氢或低级烷酰基。 X是价键,亚烷基,亚乙烯基,亚氨基或羰基氨基。 T代表两个氢原子。 当X是价键时,R 1也可以是氢,也可以含有氧,氨基,硫,羰基和磺酰基的烃基。 当X是亚氨基或羰基氨基时,或当R1是双环基时,T也可以是氧。 化合物还包括与无机和有机酸形成的互变异构体和生理上可接受的盐。

    Nitroxy amino propanols for treating heart and circulatory diseases
    29.
    发明授权
    Nitroxy amino propanols for treating heart and circulatory diseases 失效
    用于治疗心脏和循环系统疾病的硝基氨基丙醇

    公开(公告)号:US4801596A

    公开(公告)日:1989-01-31

    申请号:US803497

    申请日:1985-12-02

    摘要: The present invention provides new aminopropanol derivatives of the general formula: ##STR1## wherein A is a direct bond, a straight-chained or branched alkylene chain containing up to 3 carbon atoms or a --CO--CH.sub.2 -- group; X is a direct bond or a carbonyl group; B is a straight-chained or branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, in which one or two --CH.sub.2 -- groups can also be replaced by a saturated or unsaturated alkylene ring containing 3 to 7 carbon atoms and/or by an oxygen or sulphur atom or an --S(.dbd.O)-- or --S(.dbd.O).sub.2 -- group, n is 1, 2 or 3; R.sub.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl radical containing up to 6 carbon atoms or a --B--(ONO.sub.2).sub.n group, in which B and n have the same meanings as above, or when A is a --CO--CH.sub.2 -- group and X is a direct bond, R.sub.1 together with the nitrogen atom and a carbon atom of chain B can represent a heteroaliphatic ring containing 2 to 7 carbon atoms; R.sub.2 is a hydrogen or halogen atom or a cyano, hydroxyl, amino, nitro, carboxyl, carbamoyl, ureido or sulphamoyl group or an alkyl, alkoxy, alkylamino, alkylthio, hydroxyalkyl, aminoalkyl, alkoxycarbonyl, alkylcarbonyl, alkylaminocarbonyl, alkylcarbonylamino, alkoxycarbonylamino or alkylaminocarbonylamino radical; and R.sub.3 is an alkyl or nitroxyalkyl radical containing 3 to 8 carbon atoms; and the physiologically acceptable salts thereof.The present invention also provides processes for the preparation of these aminopropanol derivatives and pharmaceutical compositions containing them, as well as intermediates for the preparation of the new aminopropanol derivatives.

    摘要翻译: 本发明提供了以下通式的新的氨基丙醇衍生物:其中A是直接键,含有至多3个碳原子的直链或支链亚烷基链或-CO-CH 2 - 基团; X是直接键或羰基; B是含有至多12个碳原子的直链或支链,饱和或不饱和的亚烷基链,其中一个或两个-CH 2 - 基团也可以被含有3至7个碳原子的饱和或不饱和亚烷基环和/或 通过氧或硫原子或-S(= O) - 或-S(= O)2 - 基团,n是1,2或3; R1是氢原子或含有至多6个碳原子的直链或支链,饱和或不饱和的烷基或-B-(ONO 2)n基团,其中B和n具有与上述相同的含义,或当A 是-CO-CH 2 - 基团,X是直接键,R 1与氮原子一起形成,链B的碳原子可以表示含有2至7个碳原子的杂脂肪族环; R2是氢或卤原子或氰基,羟基,氨基,硝基,羧基,氨基甲酰基,脲基或氨磺酰基或烷基,烷氧基,烷基氨基,烷硫基,羟基烷基,氨基烷基,烷氧基羰基,烷基羰基,烷基氨基羰基,烷基羰基氨基,烷氧基羰基氨基或烷基氨基羰基氨基 激进; R3为含有3-8个碳原子的烷基或硝基烷基; 及其生理上可接受的盐。 本发明还提供制备这些氨基丙醇衍生物和含有它们的药物组合物的方法,以及制备新的氨基丙醇衍生物的中间体。

    Anti-allergy bicyclic phenol ethers
    30.
    发明授权
    Anti-allergy bicyclic phenol ethers 失效
    抗过敏双酚酚醚

    公开(公告)号:US4486442A

    公开(公告)日:1984-12-04

    申请号:US469856

    申请日:1983-02-25

    摘要: The present invention provides bicyclic phenol ethers of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom or an acyl radical,X is an oxygen or sulphur atom or an --NH-- group;Y is a --CO--CHR.sub.3 -- group or a ##STR2## group; R.sub.3 is a hydrogen atom, a lower alkyl radical which can be optionally substituted by an aryl radical, or a cycloalkyl radical containing 3 to 7 carbon atoms; andR.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms, lower alkyl radicals, lower alkyl radicals, alkenyl radicals containing 2 to 16 carbon atoms, which can be optionally substituted by an aryl radical, or an aryl radical; orR.sub.4 and R.sub.5, together with the carbon atom to which they are attached, form a cycloalkyl ring containing 3 to 7 carbon atoms; and thesalts thereof with pharmacologically acceptable acids.The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them.

    摘要翻译: 本发明提供以下通式的双环酚醚:其中R 1为氢原子或低级烷基,R 2为氢原子或酰基,X为氧或硫原子或 - NH-基团; Y是-CO-CHR3-基团或基团; R3是氢原子,可任意被芳基取代的低级烷基或含有3至7个碳原子的环烷基; 和可以相同或不同的R 4和R 5是氢原子,低级烷基,低级烷基,含有2至16个碳原子的烯基,其可任选被芳基或芳基取代; 或R 4和R 5与它们所连接的碳原子一起形成含有3至7个碳原子的环烷基环; 其盐与药理学上可接受的酸。 本发明还提供了制备这些化合物的方法,以及含有它们的药物组合物。