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    Pyrrolobenzimidazoles, pharmaceutical compositions containing them and method of using them to treat certain heart and circulatory diseases
    4.
    发明授权
    Pyrrolobenzimidazoles, pharmaceutical compositions containing them and method of using them to treat certain heart and circulatory diseases 失效
    吡咯并苯并咪唑，含有它们的药物组合物和使用它们治疗某些心脏和循环系统疾病的方法

    公开(公告)号：US4695567A

    公开(公告)日：1987-09-22

    申请号：US820259

    申请日：1986-01-17

    申请人： Alfred Mertens ,  Jens-Peter Holck ,  Herbert Berger ,  Bernd Muller-Beckmann ,  Klaus Strein ,  Egon Roesch

    发明人： Alfred Mertens ,  Jens-Peter Holck ,  Herbert Berger ,  Bernd Muller-Beckmann ,  Klaus Strein ,  Egon Roesch

    IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/50 ,  A61K31/505 ,  A61P9/00 ,  A61P9/04 ,  C07D403/12 ,  C07D405/12 ,  C07D487/04 ,  C07D403/06

    CPC分类号： C07D403/12 ,  C07D405/12 ,  C07D487/04

    摘要： The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.sub.4 alkylene or vinylene andT is oxygen or sulphur;and Het is furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, pyrazinyl, pyrimidinyl or pyridazinyl wherein the heterocyclic five- and six-membered rings are unsubstituted or substituted by one or more C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, hydroxyl, oxo, nitro, amino, halo, carboxyl, C.sub.2 -C.sub.7 alkoxycarbonyl, aminocarbonyl or cyano groups; or a physiologically acceptable salt thereof with an inorganic or organic acid. These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.

    摘要翻译： 本发明提供了以下通式的吡咯并苯并咪唑或其互变异构体：其中R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 7环烷基; R2是氢，氰基，C1-C6烷基，C2-C6烯基或被羟基，C1-C6烷基，C1-C6烷氧基，氨基，C1-C6烷基氨基，C2-C12二烷基氨基或肼基取代的羰基或R2 并且R 1与它们所连接的碳一起形成C 3 -C 8螺环烷基环，或者R 1和R 2一起形成C 3 -C 7亚烷基或C 3 -C 7环烷基，X是价键，C 1 -C 4亚烷基或亚乙烯基，T是 氧或硫; 并且Het是呋喃基，噻吩基，吡咯基，吡唑基，咪唑基，恶唑基，噻唑基，三唑基，恶二唑基，噻二唑基，吡嗪基，嘧啶基或哒嗪基，其中杂环五元和六元环是未取代的或被一个或多个C 1 -C 6烷基 C 1 -C 6烷氧基，C 1 -C 6烷硫基，羟基，氧代，硝基，氨基，卤素，羧基，C 2 -C 7烷氧基羰基，氨基羰基或氰基; 或其生理上可接受的盐与无机或有机酸反应。 这些化合物可用于治疗心脏或循环系统疾病，特别是那些响应血压变化，心输出量增加和/或微循环变化的化合物。

    N-Substituted aziridine-2-carboxylic acid derivatives for immuno stimulation
    6.
    发明授权
    N-Substituted aziridine-2-carboxylic acid derivatives for immuno stimulation 失效
    N-取代的氮丙啶-2-羧酸衍生物用于免疫刺激

    公开(公告)号：US4321194A

    公开(公告)日：1982-03-23

    申请号：US59863

    申请日：1979-07-23

    申请人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    发明人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    IPC分类号： C07D203/08 ,  A61K31/395 ,  A61K31/396 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P37/04 ,  C07D203/06 ,  C07D401/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D203/10 ,  C07D203/12 ,  C07D203/14

    CPC分类号： C07D203/06 ,  Y10S514/885

    摘要： Aziridine-2-carboxylic acid derivatives of the formula ##STR1## wherein X is a carboxyl, nitrile, alkoxycarbonyl or carbamoyl group, andR and R.sup.1 are various organic radicals, or pharmacologically acceptable salts thereof, exhibit marked immunostimulant activity, especially in conjunction with added chemotherapeutic agents such as a penicillin, a cephalosporin, a nitrofuran or chloramphenicol. Those compounds are new where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, but R' is not an unsubstituted alkyl radical or an alkyl radical substituted by hydroxyl, alkoxy, dialkylamino, phenyl, 4-chlorophenyl or 4-methoxyphenyl or a vinyl radical substituted by a phenyl or methyl radical, or a cycloalkyl radical, a phenyl a 4-chlorophenyl, a 4-methoxyphenyl, an s-triazinyl or a pyridinyl radical; or where X is a carbamoyl group and R.sub.1 is a hydrogen atom, R' is not an unsubstituted cyclohexyl, alkyl or benzyl radical; or where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a phenyl radical, R' is not an isopropyl, cyclohexyl, phenyl, benzyl or p-chlorobenzyl radical; or where R.sub.1 is a methyl radical, R.sup.1 is not a benzyl, p-chloro- or p- methoxybenzyl radical.

    摘要翻译： 其中X是羧基，腈，烷氧基羰基或氨基甲酰基的氮杂环丁烷-2-羧酸衍生物，R和R 1是各种有机基团或其药理学上可接受的盐，具有显着的免疫刺激活性，特别是与 添加化学治疗剂如青霉素，头孢菌素，硝基呋喃或氯霉素。 那些化合物是新的，其中X是氰基或烷氧基羰基，R 1是氢原子，但R'不是未取代的烷基或被羟基，烷氧基，二烷基氨基，苯基，4-氯苯基或4- 甲氧基苯基或被苯基或甲基取代的乙烯基，或环烷基，苯基，4-氯苯基，4-甲氧基苯基，s-三嗪基或吡啶基; 或其中X为氨基甲酰基，R 1为氢原子，R'为未取代的环己基，烷基或苄基; 或其中X为氰基或烷氧基羰基，R 1为苯基，R'不为异丙基，环己基，苯基，苄基或对氯苄基; 或其中R 1是甲基，R 1不是苄基，对氯或对甲氧基苄基。

    N-Substituted aziridine-2-carboxylic acid derivatives and their immuno-stimulation compositions and methods
    7.
    发明授权
    N-Substituted aziridine-2-carboxylic acid derivatives and their immuno-stimulation compositions and methods 失效
    N-取代的氮丙啶-2-羧酸衍生物及其免疫刺激组合物和方法

    公开(公告)号：US4410532A

    公开(公告)日：1983-10-18

    申请号：US334614

    申请日：1981-12-28

    申请人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    发明人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    IPC分类号： C07D203/08 ,  A61K31/395 ,  A61K31/396 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P37/04 ,  C07D203/06 ,  C07D401/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D213/36

    CPC分类号： C07D203/06 ,  Y10S514/885

    摘要： A 2-cyanaziridine derivative of the formula ##STR1## wherein R' is a straight-chained or branched, saturated or mono- or polyunsaturated aliphatic hydrocarbon radical with up to 8 carbon atoms, which is substituted by an aromatic nitrogen-containing heterocyclic radical with 5 or 6 ring-members and 1, 2 or 3 nitrogen atoms optionally substituted by halogen, alkoxy with up to 8 carbon atoms, alkyl with up to 8 carbon atoms, hydroxyl, carbalkoxy with up to 9 carbon atoms, carbamoyl, dialkylamino the alkyl moieties of which having up to 8 carbon atoms, cycloalkylamino, the cycloalkyl moiety having 3-10 carbon atoms, acetylamino, nitro, cyano, acetyl, alkylthio with up to 8 carbon atoms, alkylsulphinyl with up to 8 carbon atoms, alkylsulphonyl with up to 8 carbon atoms, sulphamoyl, phenyl, trifluoromethyl, phenoxy, acetoxy or methylenedioxy;or a pharmacologically acceptable salt thereof, exhibits immune stimulating activity.

    摘要翻译： 具有式“IMAGE”的2-氰基氮丙啶衍生物，其中R'是具有至多8个碳原子的直链或支链，饱和或单或多不饱和脂族烃基，其被含芳族含氮杂环基团取代， 5或6个环成员和1,2或3个任选被卤素取代的氮原子，具有至多8个碳原子的烷氧基，至多8个碳原子的烷基，羟基，至多9个碳原子的烷氧基，氨基甲酰基，二烷基氨基烷基 其具有至多8个碳原子的部分，环烷基氨基，具有3-10个碳原子的环烷基部分，乙酰氨基，硝基，氰基，乙酰基，具有至多8个碳原子的烷硫基，具有至多8个碳原子的烷基亚磺酰基，烷基磺酰基， 8个碳原子，氨磺酰基，苯基，三氟甲基，苯氧基，乙酰氧基或亚甲二氧基; 或其药理学上可接受的盐显示免疫刺激活性。

    Dispensing adapter
    9.
    发明申请
    Dispensing adapter 审中-公开
    分配适配器

    公开(公告)号：US20070158474A1

    公开(公告)日：2007-07-12

    申请号：US11563370

    申请日：2006-11-27

    申请人： Herbert Berger

    发明人： Herbert Berger

    IPC分类号： B05B1/18 ,  B05B1/26

    CPC分类号： B05C17/00516 ,  B05B15/652

    摘要： In a dispensing adapter (1) for cartridges, cans or tubes adapted for storing and metered dispensing of highly viscous materials, in particular liquids such as adhesives, sealants, foamed-in plastics or the like, through a nozzle head, the nozzle head of the metering nozzle (6, 17) has several spaced-apart openings (7, 25) for discharge of the material.

    摘要翻译： 在用于盒，罐或管的分配适配器（1）中，适用于通过喷嘴头存储和计量分配高粘度材料，特别是液体，例如粘合剂，密封剂，泡沫塑料等，喷嘴头 计量喷嘴（6,17）具有用于排出材料的几个间隔开的开口（7,25）。

    N-Substituted aziridine-2-carboxylic acid derivatives and immuno-stimulation composition and method
    10.
    发明授权
    N-Substituted aziridine-2-carboxylic acid derivatives and immuno-stimulation composition and method 失效
    N-取代的氮丙啶-2-羧酸衍生物和免疫刺激组合物和方法

    公开(公告)号：US4409236A

    公开(公告)日：1983-10-11

    申请号：US268964

    申请日：1981-06-01

    申请人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    发明人： Elmar Bosies ,  Herbert Berger ,  Wolfgang Kampe ,  Uwe Bicker ,  Alfred Grafe

    IPC分类号： C07D203/08 ,  A61K31/395 ,  A61K31/396 ,  A61K31/40 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P37/04 ,  C07D203/06 ,  C07D401/04 ,  C07D403/06 ,  C07D405/04 ,  C07D409/04 ,  C07D333/30

    CPC分类号： C07D203/06 ,  Y10S514/885

    摘要： Aziridine-2-carboxylic acid derivatives of the formula ##STR1## wherein X is a carboxyl, nitrile, alkoxycarbonyl or carbamoyl group, andR and R.sup.1 are various organic radicals; or pharmacologically acceptable salts thereof, exhibit marked immunostimulant activity, especially in conjunction with added chemotherapeutic agents such as a penicillin, a cephalosporin, a nitrofuran or chloramphenicol. Those compounds are new where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, but R' is not an unsubstituted alkyl radical or an alkyl radical substituted by hydroxyl, alkoxy, dialkylamino, phenyl, 4-chlorophenyl or 4-methoxyphenyl or a vinyl radical substituted by a phenyl or methyl radical, or a cycloalkyl radical, a phenyl, a 4-chlorophenyl, a 4-methoxyphenyl, an s-triazinyl or a pyridinyl radical; or where X is a carbamoyl group and R.sub.1 is a hydrogen atom, R' is not an unsubstituted cyclohexyl, alkyl or benzyl radical; or where X is a cyano group or an alkoxycarbonyl radical and R.sub.1 is a phenyl radical, R' is not an isopropyl, cyclohexyl, phenyl, benzyl or p-chlorobenzyl radical; or where R.sub.1 is a methyl radical, R.sup.1 is not a benzyl, p-chloro- or p- methoxybenzyl radical.

    摘要翻译： 其中X是羧基，腈，烷氧基羰基或氨基甲酰基，R和R 1是各种有机基团; 或其药理学上可接受的盐具有显着的免疫刺激活性，特别是与添加的化学治疗剂如青霉素，头孢菌素，硝基呋喃或氯霉素结合使用。 那些化合物是新的，其中X是氰基或烷氧基羰基，R 1是氢原子，但R'不是未取代的烷基或被羟基，烷氧基，二烷基氨基，苯基，4-氯苯基或4- 甲氧基苯基或被苯基或甲基取代的乙烯基，或环烷基，苯基，4-氯苯基，4-甲氧基苯基，s-三嗪基或吡啶基; 或其中X为氨基甲酰基，R 1为氢原子，R'为未取代的环己基，烷基或苄基; 或其中X为氰基或烷氧基羰基，R 1为苯基，R'不为异丙基，环己基，苯基，苄基或对氯苄基; 或其中R 1是甲基，R 1不是苄基，对氯或对甲氧基苄基。