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    THIENOTRIAZOLODIAZEPINE DERIVATIVES ACTIVE ON APO A
    1.
    发明申请
    THIENOTRIAZOLODIAZEPINE DERIVATIVES ACTIVE ON APO A 有权
    在APO A上活性的三硝基脲衍生物

    公开(公告)号：US20110230460A1

    公开(公告)日：2011-09-22

    申请号：US13126600

    申请日：2009-10-29

    申请人： Herman Kempen ,  Daniel Bellus ,  Barbara Staehelin

    发明人： Herman Kempen ,  Daniel Bellus ,  Barbara Staehelin

    IPC分类号： A61K31/397 ,  C07D495/14 ,  A61K31/551 ,  A61P25/28 ,  A61P9/10

    CPC分类号： C07D495/14

    摘要： The invention relates to new thienotriazolodiazepine derivatives of the formula (1) wherein R1 is CH3, R2 is CH3 or —(CH2)n—R4 or —(CH2)n—O—R4 or —(CH2)n—S—R4 wherein n is 1, 2, 3 or 4 and R4 is CH3, CH2CH3 or CH2CH2OCH3, and R3 is hydrogen or —OCH2O— or —OCH2CH2O— connected to the ortho/meta position or meta/para position of the phenyl ring; or wherein R1 and R2 are hydrogen and R3 is —OCH2O— Or —OCH2CH2O— connected to the ortho/meta position or meta/para position of the phenyl ring; and pharmaceutically acceptable acid addition salts thereof. These compounds and pharmaceutical compositions containing them are useful in the treatment and prevention of atherosclerotic artery diseases, such as myocardial infarction and stroke, and of Alzheimer's disease.

    摘要翻译： 本发明涉及式（1）的新型噻吩并三氮杂环恶类衍生物，其中R 1为CH 3，R 2为CH 3或 - （CH 2）n -R 4或 - （CH 2）n -O-R 4或 - （CH 2）n -S- n为1,2,3或4，R4为CH3，CH2CH3或CH2CH2OCH3，R3为氢或-OCH2O-或-OCH2CH2O-连接至苯环的邻位/间位或间位/对位; 或其中R 1和R 2是氢并且R 3是-OCH 2 O-或-OCH 2 CH 2 O-连接到苯环的邻位/间位或间位/对位; 及其药学上可接受的酸加成盐。 这些化合物和含有它们的药物组合物可用于治疗和预防动脉粥样硬化性动脉疾病如心肌梗死和中风，以及阿尔茨海默氏病。

    Certain 1-phenyl-cyclobutane-1,3-dicarboxylic acid type compounds
    2.
    发明授权
    Certain 1-phenyl-cyclobutane-1,3-dicarboxylic acid type compounds 失效
    某些1-苯基 - 环丁烷-1,3-二羧酸类化合物

    公开(公告)号：US4857660A

    公开(公告)日：1989-08-15

    申请号：US185205

    申请日：1988-04-22

    申请人： Alex Alder ,  Jaroslav Stanek ,  Daniel Bellus

    发明人： Alex Alder ,  Jaroslav Stanek ,  Daniel Bellus

    IPC分类号： A61K31/435 ,  A61P35/00 ,  A61P43/00 ,  C07D211/88 ,  C07D221/22 ,  C07D311/00 ,  C12N9/99

    CPC分类号： C07D221/22 ,  C07D311/00

    摘要： 1-Phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.

    摘要翻译： 式（I）的1-苯基-3-氮杂双环[3.1.1] - 庚烷-2,4-二酮其中R 1表示氢或饱和或不饱和的脂族，脂环族，脂环族 - 脂族，芳族或芳族 具有至多并包括18个，优选至多且包含12个碳原子的芳族 - 脂族烃基，R 2表示氢，低级烷基，磺基或酰基，R 3表示氢或低级烷基，R 4表示氢，低级烷基，苯基或苯基 被-N（R2）（R3）取代，并且这些化合物的盐具有有价值的药理学性质，作为芳香酶抑制剂是有效的，因此可用于治疗激素依赖性疾病，特别是乳腺癌。

    Substituted-3-azabicyclo[3.1.1]heptane-2,4-diones useful for treating hormone-dependent diseases
    3.
    发明授权
    Substituted-3-azabicyclo[3.1.1]heptane-2,4-diones useful for treating hormone-dependent diseases 失效
    可用于治疗激素依赖性疾病的取代的3-氮杂双环[3.1.1]庚烷-2,4-二硫杂

    公开(公告)号：US4677129A

    公开(公告)日：1987-06-30

    申请号：US746814

    申请日：1985-06-20

    申请人： Alex Alder ,  Jaroslav Stanek ,  Daniel Bellus

    发明人： Alex Alder ,  Jaroslav Stanek ,  Daniel Bellus

    IPC分类号： A61K31/435 ,  A61P35/00 ,  A61P43/00 ,  C07D211/88 ,  C07D221/22 ,  C07D311/00 ,  C12N9/99

    CPC分类号： C07D221/22 ,  C07D311/00

    摘要： 1-phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.

    摘要翻译： 式（Ⅰ）的1-苯基-3-氮杂双环[3.1.1] - 庚烷-2,4-二酮其中R 1表示氢或饱和或不饱和的脂族，脂环族，脂环族 - 脂族，脂族，芳族或 具有至多并包括18个，优选至多且包含12个碳原子的芳族 - 脂族烃基，R 2表示氢，低级烷基，磺基或酰基，R 3表示氢或低级烷基，R 4表示氢，低级烷基，苯基或苯基 被-N（R2）（R3）取代，并且这些化合物的盐具有有价值的药理学性质，作为芳香酶抑制剂是有效的，因此可用于治疗激素依赖性疾病，特别是乳腺癌。

    Cyclobutanedicarboxylic acid imides, and compositions for their use as phytopathogenic fungicides
    4.
    发明授权
    Cyclobutanedicarboxylic acid imides, and compositions for their use as phytopathogenic fungicides 失效
    环丁烷二羧酸酰亚胺及其用作植物病原性杀真菌剂的组合物

    公开(公告)号：US4361576A

    公开(公告)日：1982-11-30

    申请号：US201950

    申请日：1980-10-29

    申请人： Niklaus Buhler ,  Marcus Baumann ,  Daniel Bellus ,  Elmar Sturm

    发明人： Niklaus Buhler ,  Marcus Baumann ,  Daniel Bellus ,  Elmar Sturm

    IPC分类号： A01N37/32 ,  C07C51/353 ,  C07D209/52 ,  C07D209/02

    CPC分类号： C07D209/52 ,  A01N37/32 ,  C07C51/353

    摘要： Cyclobutanecarboxylic acid imides of the formula I ##STR1## wherein one of R.sub.1 and R.sub.6 is hydrogen, methyl or ethyl, and the other is methyl or ethyl, R.sub.2 and R.sub.3 independently of one another are each hydrogen, fluorine or methyl, or R.sub.2 is acetoxy or chlorine while R.sub.3 is hydrogen, and wherein R.sub.4 is hydrogen, methyl or chlorine, and R.sub.5 is hydrogen or methyl, whereby R.sub.3 and R.sub.4 together can also form an additional bond in the four-membered ring, are suitable for combating various fungi and have a particularly excellent action against Botrytis. They can be produced in an especially advantageous manner by photochemical [2+2] cycloaddition of alkenes or alkines with for example appropriately substituted maleic acid-(3,5-dichlorophenyl)-imides.

    摘要翻译： 式I（I）的环丁烷羧酸酰亚胺其中R 1和R 6中的一个为氢，甲基或乙基，另一个为甲基或乙基，R 2和R 3彼此独立地为氢，氟或甲基，或 R2是乙酰氧基或氯，而R3是氢，R4是氢，甲基或氯，R5是氢或甲基，其中R3和R4一起也可以在四元环中形成另外的键，适于对抗各种 真菌，对Botrytis有特别出色的作用。 它们可以通过烯烃或烯烃与例如适当取代的马来酸 - （3,5-二氯苯基） - 酰亚胺的光化学[2 + 2]环加成以特别有利的方式制备。

    Cyclobutanedicarboxisoimides and use thereof as fungicides
    5.
    发明授权
    Cyclobutanedicarboxisoimides and use thereof as fungicides 失效
    环丁烷二异氰脲酰胺及其作为杀真菌剂的用途

    公开(公告)号：US4349565A

    公开(公告)日：1982-09-14

    申请号：US251835

    申请日：1981-04-08

    申请人： Marcus Baumann ,  Niklaus Buhler ,  Daniel Bellus

    发明人： Marcus Baumann ,  Niklaus Buhler ,  Daniel Bellus

    IPC分类号： A01N43/12 ,  C07C61/04 ,  C07D307/93 ,  A61K31/365

    CPC分类号： A01N43/12 ,  C07C61/04 ,  C07D307/93

    摘要： The invention relates to cyclobutanedicarboxisoimides of the formula I ##STR1## wherein one of X and Y is oxygen and the other is ##STR2## each of R.sub.1 and R.sub.6 independently is methyl or ethyl, each of R.sub.2 and R.sub.3 independently is hydrogen, fluorine or methyl, or R.sub.2 is aceto hydrogen or methyl, while R.sub.3 and R.sub.4 together can also form an additional valency in the 4-membered cycloaliphatic ring. These compounds are suitable for controlling a variety of phytopathogenic fungi. They can be obtained by cyclizing the corresponding cyclobutanedicarboxylic acid monoamides in the temperature range from about -20.degree. to +100.degree. C., in the presence of dehydrating agents such as acetic anhydride or N,N'-dicyclohexylcarbodiimide.

    摘要翻译： 本发明涉及式I（I）的环丁烷二羧酸二酰亚胺，其中X和Y之一是氧而另一个是R 1和R 6各自独立地是甲基或乙基，R 2和R 3各自独立地是氢， 氟或甲基，或R 2是乙酰基氢或甲基，而R 3和R 4一起也可以在4元环脂族环中形成额外的化合价。 这些化合物适用于控制各种植物病原真菌。 它们可以在脱水剂如乙酸酐或N，N'-二环己基碳二亚胺存在下，在约-20℃至+ 100℃的温度范围内使相应的环丁烷二羧酸单酰胺环化来获得。

    Use of 1,2-dimethyl-3-fluoro-, 1-methyl-3,3-difluoro-, and 1,2-dimethyl-3,3-difluoro-cyclobutane-1,2-dicarbonic acid 3,5-dichlorophenyl imides as plant fungicides
    6.
    发明授权
    Use of 1,2-dimethyl-3-fluoro-, 1-methyl-3,3-difluoro-, and 1,2-dimethyl-3,3-difluoro-cyclobutane-1,2-dicarbonic acid 3,5-dichlorophenyl imides as plant fungicides 失效
    使用1,2-二甲基-3-氟-1-甲基-3,3-二氟 - 和1,2-二甲基-3,3-二氟 - 环丁烷-1,2-二羧酸3,5-二氯苯基 作为植物杀真菌剂

    公开(公告)号：US4349564A

    公开(公告)日：1982-09-14

    申请号：US141746

    申请日：1980-04-18

    申请人： Niklaus Buhler ,  Marcus Baumann ,  Daniel Bellus ,  Elmar Sturm

    发明人： Niklaus Buhler ,  Marcus Baumann ,  Daniel Bellus ,  Elmar Sturm

    IPC分类号： A01N37/32 ,  C07C51/353 ,  C07D209/52 ,  A01N43/38

    CPC分类号： C07D209/52 ,  A01N37/32 ,  C07C51/353

    摘要： Cyclobutanecarboxylic acid imides of the formula I ##STR1## wherein one of R.sub.1 and R.sub.6 is hydrogen, methyl or ethyl, and the other is methyl or ethyl, R.sub.2 and R.sub.3 independently of one another are each hydrogen, fluorine or methyl, or R.sub.2 is acetoxy or chlorine while R.sub.3 is hydrogen, and wherein R.sub.4 is hydrogen, methyl or chlorine, and R.sub.5 is hydrogen or methyl, whereby R.sub.3 and R.sub.4 together can also form an additional bond in the four-membered ring, are suitable for combating various fungi and have a particularly excellent action against Botrytis. They can be produced in an especially advantageous manner by photochemical [2+2] cycloaddition of alkenes or alkynes with for example appropriately substituted maleic acid-(3,5-dichlorophenyl)imides.

    摘要翻译： 式I（I）的环丁烷羧酸酰亚胺其中R 1和R 6中的一个为氢，甲基或乙基，另一个为甲基或乙基，R 2和R 3彼此独立地为氢，氟或甲基，或 R2是乙酰氧基或氯，而R3是氢，R4是氢，甲基或氯，R5是氢或甲基，其中R3和R4一起也可以在四元环中形成另外的键，适于对抗各种 真菌，对Botrytis有特别出色的作用。 它们可以通过烯烃或炔烃与例如适当取代的马来酸 - （3,5-二氯苯基）酰亚胺的光化学[2 + 2]环加成以特别有利的方式制备。