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    COMPUESTOS CARBOXAMIDA Y SU USO COMO INHIBIDORES DE CALPAINA.
    21.
    发明专利
    COMPUESTOS CARBOXAMIDA Y SU USO COMO INHIBIDORES DE CALPAINA. 未知

    公开(公告)号：MX2011008798A

    公开(公告)日：2012-01-20

    申请号：MX2011008798

    申请日：2010-02-19

    Applicant: ABBOTT LAB

    Inventor： HORNBERGER WILFRIED ,  HUTCHINS CHARLES W ,  KLING ANDREAS ,  MOELLER ACHIM ,  MACK HELMUT ,  JANTOS KATJA

    IPC: C07D277/22 ,  A61K31/4439 ,  A61P25/00 ,  A61P31/18 ,  A61P35/00 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

    Abstract: La presente invención se refiere a compuestos carboxamída novedosos y su uso como un medicamento. Los compuestos carboxamida son inhibidores de calpaína (cisteína proteasas dependientes del calcio). Por lo tanto, la invención también se refiere al uso de tales compuestos carboxamida para tratar un trastorno asociado con una elevada actividad de la calpaína y a un método para el tratamiento terapéutico y/o profiláctico por administración de una cantidad eficaz de por lo menos uno de tales compuestos carboxamida. Los compuestos carboxamida son compuestos de fórmula general I en donde W-R2 se selecciona entre las fórmulas (1), (2) y (3) y R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw y RW* que tienen los valores que se mencionan en las reivindicaciones, los tautómeros de los mismos y las sales aceptables farmacéuticamente de los mismos. De tales compuestos, se prefieren aquellos en donde Y1, Y2, Y3 y Y4 son CRy, o una o dos de las variables Y1 a Y4 son un átomo de nitrógeno y las variables restantes son CRy, en donde los radicales Ry pueden ser idénticos o diferentes y tienen los valores que se mencionan en las reivindicaciones.

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    22.
    发明专利
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 未知

    公开(公告)号：SG175320A1

    公开(公告)日：2011-11-28

    申请号：SG2011077559

    申请日：2010-05-06

    Applicant: ABBOTT GMBH & CO KG ,  ABBOTT LAB

    Inventor： MACK HELMUT ,  KLING ANDREAS ,  JANTOS KATJA ,  MOELLER ACHIM ,  HORNBERGER WILFRIED ,  HUTCHINS CHARLES W

    Abstract: 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, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula (Ia) and (Ib) in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2-CH2, CH2-CH2-CH2, N(Ry#)-CH2, N(Ry#)-CH2-CH2 or CH=CH-CH=, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    23.
    发明专利
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 未知

    公开(公告)号：PH12013502359B1

    公开(公告)日：2014-11-10

    申请号：PH12013502359

    申请日：2013-11-15

    Applicant: ABBOTT GMBH & CO KG ,  ABBOTT LAB

    Inventor： MACK HELMUT ,  KLING ANDREAS ,  JANTOS KATJA ,  MOELLER ACHIM ,  HORNBERGER WILFRIED ,  HUTCHINS CHARLES W

    IPC: A61K31/4412 ,  C07D207/26 ,  C07D211/76 ,  C07D233/34 ,  C07D239/10

    Abstract: 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, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula (Ia) and (Ib) in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2-CH2, CH2-CH2-CH2, N(Ry#)-CH2, N(Ry#)-CH2-CH2 or CH=CH-CH=, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    25.
    发明专利
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 未知

    公开(公告)号：NZ596000A

    公开(公告)日：2013-10-25

    申请号：NZ59600010

    申请日：2010-05-06

    Applicant: ABBOTT GMBH & CO KG ,  ABBOTT LAB

    Inventor： MACK HELMUT ,  KLING ANDREAS ,  JANTOS KATJA ,  MOELLER ACHIM ,  HORNBERGER WILFRIED ,  HUTCHINS CHARLES W

    IPC: C07D207/26 ,  A61K31/4412 ,  C07D211/76 ,  C07D233/34 ,  C07D239/10

    Abstract: 596000 Disclosed herein are 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, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula (Ia) and (Ib) in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV
    27.
    发明专利
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV 未知

    公开(公告)号：CA2783714A1

    公开(公告)日：2011-06-30

    申请号：CA2783714

    申请日：2010-12-21

    Applicant: ABBOTT GMBH & CO KG ,  ABBOTT LAB

    Inventor： KLING ANDREAS ,  JANTOS KATJA ,  MACK HELMUT ,  MOELLER ACHIM ,  HORNBERGER WILFRIED ,  BACKFISCH GISELA ,  LAO YANBIN ,  NIJSEN MARJOLEEN

    IPC: C07D401/04 ,  A61K31/4439 ,  A61P25/00

    Abstract: 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, R5,, 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 phenyl-C1-C2-alkyl or hetaryl-C1-C2-alkyl, R2 is optionally substituted aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl or hetaryl-C1-C4-alkyl, R3 is C3-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6- heterocycloalkyl-C1-C2-alkyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or 1,3- benzoxazol-2-yl-methyl, R4 and R5 independently of one another are halogen, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    29.
    发明专利
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS 未知

    公开(公告)号：CA2750993A1

    公开(公告)日：2010-08-26

    申请号：CA2750993

    申请日：2010-02-19

    Applicant: ABBOTT GMBH & CO KG ,  ABBOTT LAB

    Inventor： KLING ANDREAS ,  MACK HELMUT ,  JANTOS KATJA ,  MOELLER ACHIM ,  HORNBERGER WILFRIED ,  HUTCHINS CHARLES W

    IPC: C07D277/22 ,  A61K31/4439 ,  A61P25/00 ,  A61P31/18 ,  A61P35/00 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

    Abstract: The present invention relates to novel carboxamide compounds and their use as 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 and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula (I) in which W-R2 is selected from formulae (1), (2) and (3) and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y1, Y2, Y3 and Y4 are CRy, or one or two of the variables Y1 to Y4 are a nitrogen atom and the remaining variables are CRy, wherein the radicals Ry may be identical or different and have the meanings mentionend in the claims.

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