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118 条记录 (耗时 0.077 秒)

    4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS
    101.
    发明申请
    4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS 有权
    4-（4-吡啶基） - 苯甲酸酯及其作为岩石活性调节剂的用途

    公开(公告)号：US20100273828A1

    公开(公告)日：2010-10-28

    申请号：US12675430

    申请日：2008-08-26

    申请人： Helmut Mack ,  Nicole Teusch ,  Bernhard K. Müller ,  Wilfried Hornberger ,  Michael F. Jarvis ,  Daryl Sauer ,  Steve Swann, JR. ,  Anil Vasudevan

    发明人： Helmut Mack ,  Nicole Teusch ,  Bernhard K. Müller ,  Wilfried Hornberger ,  Michael F. Jarvis ,  Daryl Sauer ,  Steve Swann, JR. ,  Anil Vasudevan

    IPC分类号： A61K31/4545 ,  A61K31/444 ,  A61K31/4439 ,  A61K31/44 ,  C07D401/02 ,  C07D213/56 ,  A61P25/16 ,  A61K9/00 ,  A61P35/00 ,  A61P11/06 ,  A61P25/00 ,  A61P25/28

    CPC分类号： C07D401/12 ,  C07D213/56 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

    摘要： The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R1 and R2 are, independently of each other, hydrogen, hydroxy, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-haloalkoxy; R3, R4, R5 and R6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, amino, C1-C8-alkylamino or di-(C1-C8-alkyl)-amino; R7 is hydrogen, C1-C8-alkyl, C1-C8-haloalkyl, aryl or aryl-C1-C8-alkyl; R8 is a group of the formula —X—W, where X is a single bond, C1-C4-alkylene or C1-C4-alkylene-O—, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected from O, S and N and optionally 1 or 2 carbonyl groups; R9 is a group of the formula —Y—Z, where Z is hydrogen, halogen, OR11, NR12R13, S(O)m—R14, phenyl which may carry 1, 2, 3 or 4 substituents R15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C1C4-alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.

    摘要翻译： 本发明涉及式（I）的新型4-（4-吡啶基） - 苯甲酰胺。 化合物I具有有价值的治疗特性，特别适用于治疗对Rho激酶（ROCK）的调节作用的疾病。 R 1和R 2彼此独立地为氢，羟基，氰基，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，C 1 -C 8 - 烷氧基或C 1 -C 8 - 卤代烷氧基; R3，R4，R5和R6彼此独立地为氢，羟基，卤素，氰基，C1-C8-烷基，C1-C8-卤代烷基，C1-C8-烷氧基，C1-C8-卤代烷氧基，氨基，C1- C 8 - 烷基氨基或二 - （C 1 -C 8 - 烷基） - 氨基; R 7是氢，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，芳基或芳基-C 1 -C 8 - 烷基; R8是式-X-W的基团，其中X是单键，C1-C4-亚烷基或C1-C4-亚烷基-O-，其中三个最后提到的基团中的亚烷基可以是直链或支链 并且可以部分或完全卤化和/或可以被羟基取代和/或可以被氧原子中断; 并且W是选自苯基和5-或6-元饱和，部分不饱和或芳族杂环的环状基团，其含有作为环成员1,2或3的选自O，S和N的杂原子以及任选的1或2个羰基 ; R 9是式-Y-Z的基团，其中Z是氢，卤素，OR 11，NR 12 R 13，S（O）m -R 14，可带有1,2,3或4个取代基R 15或5-或6的苯基 饱和的，部分不饱和的或芳族的杂环; Y是可部分或完全卤化和/或可被羟基和/或苯环取代的直链或支链C 1 -C 4亚烷基; 或者Z为苯基或上述5-或6-元杂环的情况下，Y也可以是单键。

    Composition acting as coupling agent for filled and peroxidically crosslinking rubber compounds
    103.
    发明授权
    Composition acting as coupling agent for filled and peroxidically crosslinking rubber compounds 失效
    用作填充和过氧化交联橡胶化合物的偶联剂的组合物

    公开(公告)号：US07625975B2

    公开(公告)日：2009-12-01

    申请号：US10524689

    申请日：2003-06-20

    申请人： Dieter Barfurth ,  Helmut Mack ,  Burkhard Standke

    发明人： Dieter Barfurth ,  Helmut Mack ,  Burkhard Standke

    IPC分类号： C08L9/00

    CPC分类号： C08K5/5425 ,  C08L21/00 ,  Y10T428/2991 ,  Y10T428/2995 ,  Y10T428/31663

    摘要： The present invention relates to a composition acting as coupling agent between fillers and peroxidically crosslinking elastomers in rubber compounds, which comprises, as component comprising silicon compounds, a mixture a) of vinylalkoxysiloxanes with alkylalkoxy-siloxanes, or b) of vinylalkoxysiloxanes with phenylalkoxy-siloxanes, or c) of vinylalkoxysiloxanes with phenyl/alkyl-alkoxysiloxanes or d) of acrylic or methacrylic alkoxysiloxanes with alkylalkoxysiloxanes, or e) of acrylic or methacrylic alkoxysiloxanes with phenylalkoxysiloxanes, or f) of acrylic or methacrylic alkoxysiloxanes with phenyl/alkylalkoxysiloxanes, or g) of at least one co-oligomeric organosiloxane which, as organofunctional groups, bears at least one group from the series vinyl, acrylic and methacrylic, and at least one group from the series alkyl and phenyl, and at least one alkoxy or hydroxy group. The present invention further relates to the use of a composition of the invention as a coupling agent in filled and peroxidically crosslinking rubber compounds, to rubber compounds obtained in this way, and to items made therefrom.

    摘要翻译： 本发明涉及在橡胶化合物中作为填料和过氧化交联弹性体之间的偶联剂的组合物，其包含作为包含硅化合物的组分的乙烯基烷氧基硅氧烷与烷基烷氧基硅氧烷的混合物，或b）乙烯基烷氧基硅氧烷与苯基烷氧基硅氧烷 或c）具有苯基/烷基 - 烷氧基硅氧烷的乙烯基烷氧基硅氧烷或d）丙烯酸或甲基丙烯酸烷氧基硅氧烷与烷基烷氧基硅氧烷，或e）丙烯酸或甲基丙烯酸烷氧基硅氧烷与苯基烷氧基硅氧烷，或f）丙烯酸或甲基丙烯酸烷氧基硅氧烷与苯基/烷基烷氧基硅氧烷，或g） 的至少一种共低聚有机硅氧烷，其作为有机官能团，从乙烯基，丙烯酸和甲基丙烯酸系列中至少包含一个基团，以及至少一个来自烷基和苯基的基团，以及至少一个烷氧基或羟基。 本发明还涉及本发明的组合物作为填充和过氧化交联的橡胶化合物中的偶联剂，以这种方式获得的橡胶化合物以及由其制备的物质的用途。

    Organofunctional siloxane mixtures
    106.
    发明申请
    Organofunctional siloxane mixtures 有权
    有机官能硅氧烷混合物

    公开(公告)号：US20070032622A1

    公开(公告)日：2007-02-08

    申请号：US10555984

    申请日：2004-03-18

    申请人： Dieter Barfurth ,  Helmut Mack

    发明人： Dieter Barfurth ,  Helmut Mack

    IPC分类号： C08G77/04

    CPC分类号： C08G77/26 ,  C07F7/21 ,  C08G77/04

    摘要： The present Invention relates to a mixture comprising catenary, branched andfor cyclic siloxanes of the general formula (I) where x is 1, 2 or 3, the substituents R are (i) organofunctional groups selected from —CH2—SH, —CH2—S—(CO)—R′, —CH2(O—C2H4)a—OH with a =1 to 10, —CH2(O—C2H4)b—OR′ with b =1 to 40, —(CH2)—NH2, —(CH2)—NHR′, —(CH2)—NR′2, —(CH2)—NH(CH2)2—NH2, —(CH2)—N[(CH2)2—NH2]2 and —(CH2) —NH(CH2)2—NH(CH2)2—NH2, In which R′ is a linear, branched or cyclic alkyl group having 1 to 18 carbon atoms or an aryl group having 6 to 12 carbon atoms, (ii) hydroxyl, methoxy, ethoxy, 2-methoxyethoxy, isopropoxy, n-propoxy, isobutoxy andfor n-butoxy groupe, and (iii) where appropriate, alkyl, alkenyl, isoalkyl, cycloalkyl or fluorcalkyl groups having 1 to 18 carbon atoms or aryl groups having 6 to 12 carbon atoms, whit the proviso that not more than one organofunctional group (i) is attached per silicon atom, the quotient of the molar ratio of the moiety (ii) to silicon le from I to 2, and the degree of oligornerization for compounds of the general formula I is in the range from 2 to 50. The present invention also relates to a specific process for preparing said siloxane mixtures and also to their use.

    摘要翻译： 本发明涉及包含通式（I）的链状，支链和环状硅氧烷的混合物，其中x为1,2或3，取代基R为（i）选自-CH 2的有机官能团 > -SH，-CH 2 -S-（CO）-R'，-CH 2（OC 2 H 4） 其中a = 1至10，-CH 2（OC 2 H 4） ）b = 1至40， - （CH 2）2 NH 2 - ， - （CH 2） ） - NHR'， - （CH 2） - NR'2， - （CH 2） - NH（CH

    Composition acting as coupling agent for filled and peroxidically crosslinking rubber compounds
    107.
    发明申请
    Composition acting as coupling agent for filled and peroxidically crosslinking rubber compounds 失效
    用作填充和过氧化交联橡胶化合物的偶联剂的组合物

    公开(公告)号：US20070032609A1

    公开(公告)日：2007-02-08

    申请号：US10524689

    申请日：2003-06-20

    申请人： Dieter Barfurth ,  Helmut Mack ,  Burkhard Standke

    发明人： Dieter Barfurth ,  Helmut Mack ,  Burkhard Standke

    IPC分类号： C08L83/04 ,  B32B27/00 ,  B32B27/18 ,  B32B9/04

    CPC分类号： C08K5/5425 ,  C08L21/00 ,  Y10T428/2991 ,  Y10T428/2995 ,  Y10T428/31663

    摘要： The present invention relates to a composition acting as coupling agent between fillers and peroxidically crosslinking elastomers in rubber compounds, which comprises, as component comprising silicon compounds, a mixture a) of vinylalkoxysiloxanes with alkylalkoxy-siloxanes, or b) of vinylalkoxysiloxanes with phenylalkoxy-siloxanes, or c) of vinylalkoxysiloxanes with phenyl/alkyl-alkoxysiloxanes or d) of acrylic or methacrylic alkoxysiloxanes with alkylalkoxysiloxanes, or e) of acrylic or methacrylic alkoxysiloxanes with phenylalkoxysiloxanes, or f) of acrylic or methacrylic alkoxysiloxanes with phenyl/alkylalkoxysiloxanes, or g) of at least one co-oligomeric organosiloxane which, as organofunctional groups, bears at least one group from the series vinyl, acrylic and methacrylic, and at least one group from the series alkyl and phenyl, and at least one alkoxy or hydroxy group. The present invention further relates to the use of a composition of the invention as a coupling agent in filled and peroxidically crosslinking rubber compounds, to rubber compounds obtained in this way, and to items made therefrom.

    摘要翻译： 本发明涉及在橡胶化合物中作为填料和过氧化交联弹性体之间的偶联剂的组合物，其包含作为包含硅化合物的组分的乙烯基烷氧基硅氧烷与烷基烷氧基硅氧烷的混合物，或b）乙烯基烷氧基硅氧烷与苯基烷氧基硅氧烷 或c）具有苯基/烷基 - 烷氧基硅氧烷的乙烯基烷氧基硅氧烷或d）丙烯酸或甲基丙烯酸烷氧基硅氧烷与烷基烷氧基硅氧烷，或e）丙烯酸或甲基丙烯酸烷氧基硅氧烷与苯基烷氧基硅氧烷，或f）丙烯酸或甲基丙烯酸烷氧基硅氧烷与苯基/烷基烷氧基硅氧烷，或g） 的至少一种共低聚有机硅氧烷，其作为有机官能团，从乙烯基，丙烯酸和甲基丙烯酸系列中至少包含一个基团，以及至少一个来自烷基和苯基的基团，以及至少一个烷氧基或羟基。 本发明还涉及本发明的组合物作为填充和过氧化交联的橡胶化合物中的偶联剂，以这种方式获得的橡胶化合物以及由其制备的物质的用途。

    Prodrugs of thrombin inhibitors
    108.
    发明授权
    Prodrugs of thrombin inhibitors 有权
    凝血酶抑制剂的前药

    公开(公告)号：US07144902B1

    公开(公告)日：2006-12-05

    申请号：US09958349

    申请日：2000-04-05

    申请人： Dorit Baucke ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger ,  Gisela Backfisch ,  Juergen Delzer

    发明人： Dorit Baucke ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger ,  Gisela Backfisch ,  Juergen Delzer

    IPC分类号： A61K31/425 ,  C07D277/20

    CPC分类号： C07K5/06078 ,  A61K38/00 ,  C07B43/00 ,  C07K5/0222

    摘要： The present invention relates to prodrugs of pharmacologically active five-membered heterocyclic amidines from which are produced in vivo compounds which are competitive inhibitors of trypsin-like serine proteases, in particular thrombin and kininogenases such as kallikrein, to the preparation thereof and to the use thereof as medicines. The invention also relates to pharmaceutical compositions which comprise the prodrugs of the active compounds as ingredients, and to the use of the compounds as thrombin inhibitors, anticoagulants and as antiinflammatory agents.

    摘要翻译： 本发明涉及药理活性五元杂环脒的前体药物，它们是体内化合物，其是胰蛋白酶样丝氨酸蛋白酶的竞争性抑制剂，特别是凝血酶和激肽释放酶如激肽释放酶对其制备及其用途 作为药物 本发明还涉及包含活性化合物作为成分的前药以及该化合物作为凝血酶抑制剂，抗凝剂和抗炎剂的用途的药物组合物。

    3-Substituted 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof
    110.
    发明申请
    3-Substituted 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives, production and use thereof 有权
    3-取代的3,4-二氢 - 噻吩并[2,3-d]嘧啶-4-酮衍生物，的制备和用途

    公开(公告)号：US20060142317A1

    公开(公告)日：2006-06-29

    申请号：US10539708

    申请日：2003-12-17

    申请人： Margaretha Bakker ,  Wilfried Hornberger ,  Andreas Kling ,  Udo Lange ,  Helmut Mack ,  Achim Moeller ,  Reinhold Mueller ,  Kurt Schelhaas ,  Martin Schmidt ,  Gerd Steiner ,  Karsten Wicke

    发明人： Margaretha Bakker ,  Wilfried Hornberger ,  Andreas Kling ,  Udo Lange ,  Helmut Mack ,  Achim Moeller ,  Reinhold Mueller ,  Kurt Schelhaas ,  Martin Schmidt ,  Gerd Steiner ,  Karsten Wicke

    IPC分类号： A61K31/519 ,  C07D498/14

    CPC分类号： C07D495/14

    摘要： The invention relates to 3,4-dihydro-thieno[2,3-d]pyrimidin-4-one derivatives which are substituted in position 3 by 5-membered heteroaryl which may be fused to an aryl or heteroaryl radical, where the heteroaryl and, if appropriate, the fused aryl or heteroaryl radical may have 1, 2 or 3 substituents selected independently of one another from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halo-C1-5-alkyl, halo-C1-5-alkoxy, hydroxy, —NH2, —N(R6)2, —NH(R6), aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl, where the substituents aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl may have 1, 2 or 3 substituents selected independently of one another from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halo-C1-5-alkyl, halo-C1-5-alkoxy, hydroxy, —NH2, —N(R6)2 and —NH(R6). The preparation and use of these derivatives, especially for therapeutic purposes, e.g. for the treatment of depressions, are likewise described.

    摘要翻译： 本发明涉及在3位被5元杂芳基取代的3,4-二氢 - 噻吩并[2,3-d]嘧啶-4-酮衍生物，其可以与芳基或杂芳基稠合，其中杂芳基和 如果合适，稠合的芳基或杂芳基可以具有1,2或3个彼此独立地选自C 1-5 - 烷基，C 1-5 - 烷氧基，C 1-5 - 烷硫基，卤素，CN，卤代-C 1-5 - 烷基，卤代C 1-5 - 烷氧基，羟基，-NH 2，-N（R 6）2，-NH（R 6），芳基，芳氧基，芳烷基，芳烷氧基和杂芳基，其中取代基芳基， 芳氧基，芳烷基，芳烷氧基和杂芳基可以具有1,2或3个选自C 1-5 - 烷基，C 1-5 - 烷氧基，C 卤代C 1 -C 5烷基，卤素，CN，卤代-C 1-5烷基，卤代-C 1-5烷氧基，羟基 ，-NH 2，-N（R 6）2和-NH（R 6）。 这些衍生物的制备和使用，特别是用于治疗目的，例如 为了处理凹陷，同样地描述。