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    • 7. 发明申请
    • COMPOSITION ACTING AS COUPLING AGENT FOR FILLED AND PEROXIDICALLY CROSSLINKING RUBBER COMPOUNDS
    • 作为填充剂和过氧化物交联橡胶化合物的联合剂的组合物
    • WO2004018546A1
    • 2004-03-04
    • PCT/EP2003/006543
    • 2003-06-20
    • DEGUSSA AGBARFURTH, DieterMACK, HelmutSTANDKE, Burkhard
    • BARFURTH, DieterMACK, HelmutSTANDKE, Burkhard
    • C08G77/18
    • C08K5/5425C08L21/00Y10T428/2991Y10T428/2995Y10T428/31663
    • 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.
    • 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至少一个基团,和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圆片中的偶联剂的用途 d和过氧化交联橡胶化合物,以这种方式获得的橡胶化合物,以及由其制备的物品。
    • 9. 发明申请
    • CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V
    • 羧酰胺化合物及其作为钙抑制剂V
    • WO2012076639A1
    • 2012-06-14
    • PCT/EP2011/072164
    • 2011-12-08
    • ABBOTT GMBH & CO. KGABBOTT LABORATORIESKLING, AndreasJANTOS, KatjaMACK, HelmutMÖLLER, AchimHORNBERGER, WilfriedLAO, YanbinBACKFISCH, GiselaNIJSEN, Marjoleen
    • KLING, AndreasJANTOS, KatjaMACK, HelmutMÖLLER, AchimHORNBERGER, WilfriedLAO, YanbinBACKFISCH, GiselaNIJSEN, Marjoleen
    • A61K31/4439C07D401/04A61P25/28
    • C07D401/04A61K31/4439C07D401/14Y02A50/411
    • The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R 1 , R 2 , R 3 R 4 , X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R 1 is optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R 2 is C 1 -C 4 - alkyl, C 1 -C 4 -haloalkyl, C 2 -C 4 -alkenyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, C 3 -C 6 -heterocycloalkyl-C 1 -C 2 -alkyl, phenyl, phenyl-C 1 -C 3 -alkyl, pyridin-2-yl-C 1 -C 3 -alkyl or CH 2 -C(O)OCH 3 ,R 3 and R 4 independently of one another are halogen, CN, CF 3 , CHF 2 , CH 2 F, C 1 -C 2 -alkyl or C 1 -C 2 -alkoxy, and m and n independently of one another are 0 or 1.
    • 本发明涉及新的羧酰胺化合物及其用于制备药物的用途。 羧酰胺化合物是钙蛋白酶(钙依赖性半胱氨酸蛋白酶)的抑制剂。 因此,本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。 羧酰胺化合物是通式(I)的化合物,其中R 1,R 2,R 3,R 4,X,m和n具有权利要求书和描述中所述的含义,其互变异构体,其水合物及其药学上合适的盐 。 在这些化合物中,优选其中R 1为任选取代的苄基或杂芳基 - 甲基,X为单键或氧原子,R 2为C 1 -C 4烷基,C 1 -C 4卤代烷基,C 2 -C 4 - 烯基,C 3 -C 6 环烷基,C 3 -C 6 - 环烷基-C 1 -C 2 - 烷基,C 3 -C 6 - 杂环烷基-C 1 -C 2烷基,苯基,苯基-C 1 -C 3 - 烷基,吡啶-2-基-C 1 -C 3 - 烷基或CH 2 -C(O)OCH 3,R 3和R 4彼此独立地是卤素,CN,CF 3,CHF 2,CH 2 F,C 1 -C 2 - 烷基或C 1 -C 2 - 烷氧基,m和n彼此独立地为0或1。
    • 10. 发明申请
    • CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV
    • 羧酰胺化合物及其作为抑制剂的用途IV
    • WO2011076812A1
    • 2011-06-30
    • PCT/EP2010/070420
    • 2010-12-21
    • ABBOTT GMBH & CO. KGABBOTT LABORATORIESKLING, AndreasJANTOS, KatjaMACK, HelmutMÖLLER, AchimHORNBERGER, WilfriedBACKFISCH, GiselaLAO, YanbinNIJSEN, Marjoleen
    • KLING, AndreasJANTOS, KatjaMACK, HelmutMÖLLER, AchimHORNBERGER, WilfriedBACKFISCH, GiselaLAO, YanbinNIJSEN, Marjoleen
    • C07D401/04A61K31/4439A61P25/00
    • C07D401/04C07D401/14C07D413/14
    • The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R 1 , R 2 , R 3 R 4 , R 5 ,, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R 1 is optionally substituted phenyl-C 1 -C 2 -alkyl or hetaryl-C 1 -C 2 -alkyl, R 2 is optionally substituted aryl, hetaryl, aryl-C 1 -C 6 -alkyl, aryl-C 2 -C 6 -alkenyl or hetaryl-C 1 -C 4 -alkyl, R 3 is C 3 -C 4 -alkyl, C 1 -C 4 -haloalkyl, C 2 -C 4 -alkenyl, C 3 -C 6 -cycloalkyl, C 3 -C 6 -cycloalkyl-C 1 -C 2 -alkyl, C 3 -C 6 - heterocycloalkyl-C 1 -C 2 -alkyl, phenyl-C 1 -C 3 -alkyl, pyridin-2-yl-C 1 -C 3 -alkyl or 1,3- benzoxazol-2-yl-methyl, R 4 and R 5 independently of one another are halogen, CF 3 , CHF 2 , CH 2 F, C 1 -C 2 -alkyl or C 1 -C 2 -alkoxy, and m and n independently of one another are 0 or 1.
    • 本发明涉及新的羧酰胺化合物及其用于制备药物的用途。 羧酰胺化合物是钙蛋白酶(钙依赖性半胱氨酸蛋白酶)的抑制剂。 因此,本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。 羧酰胺化合物是通式I的化合物,其中R 1,R 2,R 3,R 4,R 5,m和n具有权利要求书和说明书中所述的含义,其互变异构体,其水合物及其药学上合适的盐。 在这些化合物中,优选其中R 1为任选取代的苯基-C 1 -C 2 - 烷基或杂芳基-C 1 -C 2烷基,R 2为任选取代的芳基,杂芳基,芳基-C 1 -C 6 - 烷基,芳基-C 2 -C 6 - 烯基 或杂芳基-C 1 -C 4 - 烷基,R 3是C 3 -C 4 - 烷基,C 1 -C 4 - 卤代烷基,C 2 -C 4 - 烯基,C 3 -C 6 - 环烷基,C 3 -C 6 - 环烷基-C 1 -C 2烷基,C 3 -C 6 - 杂环烷基-C 1 -C 2 - 烷基,苯基-C 1 -C 3 - 烷基,吡啶-2-基-C1-C3-烷基或1,3-苯并恶唑-2-基 - 甲基,R4和R5彼此独立地是卤素 ,CF 3,CHF 2,CH 2 F,C 1 -C 2烷基或C 1 -C 2烷氧基,m和n彼此独立地为0或1。