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    • 3. 发明授权
    • Carboxamide compounds and their use as calpain inhibitors V
    • 羧酰胺化合物及其作为钙蛋白酶抑制剂的用途
    • US09062027B2
    • 2015-06-23
    • US13992582
    • 2011-12-08
    • Andreas KlingKatja JantosHelmut MackAchim MollerWilfried HornbergerYanbin LaoGisela BackfischMarjoleen Nijsen
    • Andreas KlingKatja JantosHelmut MackAchim MollerWilfried HornbergerYanbin LaoGisela BackfischMarjoleen Nijsen
    • C07D401/14C07D401/04A61K31/4439A61P25/28
    • 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 R1, R2, R3, R4, 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 R1 is optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2—C(O)OCH3, R3 and R4 independently of one another are halogen, CN, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-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,其水合物和药学上合适的盐 其中。 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。
    • 4. 发明授权
    • Recycled wood product with platelets
    • 回收木制品与血小板
    • US5686175A
    • 1997-11-11
    • US416759
    • 1995-07-25
    • Achim Moller
    • Achim Moller
    • B27L11/02B27N1/00B32B5/16B32C17/00
    • B27L11/02B27N1/00Y10S241/38Y10T428/253
    • A recycled wood product is formed from wood products originally made from first cut wood. The recycled wood product is formed by removing external fittings, if any, projecting from the original, wood product and thereafter chipping the original wood product into platelets which are thereafter assembled in layers, glued together and then pressed together. Any excess formaldehyde in the original wood product is removed by the addition of urea. Machinery to practice the process includes a chipping tool which chips the original product into platelets as the original wood product is advanced against the chipping tool on a movable support structure.
    • 回收木材产品由原始由第一切割木材制成的木制品形成。 回收的木制品通过从原始木制品中除去外部配件(如果有的话)而形成,然后将原始木制品切碎成小片,然后将其组装成层,粘合在一起然后压在一起。 通过添加尿素来除去原始木制品中的任何多余的甲醛。 实施该过程的机器包括一种切屑工具,当原始木制品在可移动支撑结构上抵靠切屑工具前进时,将原始产品切割成血小板。
    • 5. 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
    • US20140005227A1
    • 2014-01-02
    • US13992582
    • 2011-12-08
    • Andreas KlingKatja JantosHelmut MackAchim MollerWilfried HornbergerYanbin LaoGisela BackfischMarjoleen Nijsen
    • Andreas KlingKatja JantosHelmut MackAchim MollerWilfried HornbergerYanbin LaoGisela BackfischMarjoleen Nijsen
    • C07D401/04
    • 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 R1, R2, R3, R4, 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 R1 is optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, R2 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or CH2—C(O)OCH3, R3 and R4 independently of one another are halogen, CN, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-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,其水合物和药学上合适的盐 其中。 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。