COMPUESTOS CARBOXAMIDA Y SU USO COMO INHIBIDORES DE CALPAINA

    公开(公告)号:CO6470862A2

    公开(公告)日:2012-06-29

    申请号:CO11167060

    申请日:2011-12-05

    Abstract: Compuesto carboxamida novedosos y su uso para la fabricación de 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 dichos compuestos carboxamida para tratar un trastorno asociado con una alta actividad de calpaína. Los compuestos carboxamida son compuestos de la fórmula general IDonde R1, R2, R3a, R3b, R4, Q, Y, A y X tienen los significados que se mencionan en las reivindicaciones y la descripción, los tautómeros de los mismos y las sales de los mismos apropiados para uso farmacéutico. En particular, los compuestos tienen la fórmula general la e lbDonde R1, r, R2b, R3a, R3b, R4 Y y X tienen los significados que se mencionan en las reivindicadores, incluyendo a los tautómeros de los mismos y a las sales farmacéuticamente: apropiadas de los mismo. De dichos compuestos, se prefieren aquellos donde Y es una unidad CHr2-CH2, CH2-CH2-CH2, N(RY'')-CH2, N(RY'')-CH2-CH2 O CH=CH-CH=, en cada uno de los cuales opcionalmente se han reemplazada 1 ó 2 átomos de H por radicales RY idénticos o diferentes, donde RY y RY'' tienen los significados que se mencionan en las reivindicaciones.

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS

    公开(公告)号:CA2760464A1

    公开(公告)日:2010-11-11

    申请号:CA2760464

    申请日:2010-05-06

    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

    公开(公告)号:NZ706401A

    公开(公告)日:2015-08-28

    申请号:NZ70640110

    申请日:2010-05-06

    Abstract: 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). Additionally disclosed is the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity, interleukin-I, TNF or A&bgr; level, such as malaria, HIV or disorders associated with the kidneys. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3a, R3b, 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

    公开(公告)号:PH12013502359A1

    公开(公告)日:2014-11-10

    申请号:PH12013502359

    申请日:2013-11-15

    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.

    TNF-alpha binding proteins
    8.
    发明专利

    公开(公告)号:AU2011338313A1

    公开(公告)日:2013-05-02

    申请号:AU2011338313

    申请日:2011-12-08

    Abstract: TNF-α binding proteins, including chimeric, CDR-grafted, and humanized antibodies that bind TNF-α are provided. Binding proteins have high affinity for TNF-α and neutralize TNF-α activity. A binding protein can be a full-length antibody or a TNF-α-binding portion thereof. Methods of making and methods of using the binding proteins are also described. The TNF-α binding proteins are useful for detecting TNF-α and for inhibiting TNF-α activity, including in a human subject suffering from a disease or disorder in which TNF-α activity is detrimental.

    COMPUESTOS CARBOXAMIDA Y SU USO COMO INHIBIDORES DE CALPAINA IV.

    公开(公告)号:MX2012007322A

    公开(公告)日:2012-11-06

    申请号:MX2012007322

    申请日:2010-12-21

    Applicant: ABBOTT LAB

    Abstract: La presente invención se relaciona con compuestos carboxamida novedosos y su uso para la elaboración de 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 dichos compuestos carboxamida para tratar un trastorno asociado con una actividad elevada de calpaína. Los compuestos carboxamida son compuestos de la fórmula general I, donde R1, R2, R3, R4, R5, m y n tienen los significados mencionados en las reivindicaciones y la descripción, los tautómeros, los hidratos y las sales de los mismos farmacéuticamente apropiados. Entre estos compuestos, se prefieren aquellos en donde R1 es fenil-C1-C2-alquilo o hetaril-C1-C2-alquilo opcionalmente sustituido, R2 es arilo, hetarilo, aril-C1-C6-alquilo, aril-C2-C6-alquenilo o hetaril-C1-C4-alquilo opcionalmente sustituido, R3 es C3-C4-alquilo, C1-C4-haloalquilo, C2-C4-alquenilo, C3-C6-cicloalquilo, C3-C6-cicloalquil-C1-C2-alquilo, C3-C6-heterocicloalquil-C1-C2-alquilo, fenil-C1-C3-alquilo, piridin-2-il-C1-C3-alquilo o 1 ,3-benzoxazol-2-il-metilo, R4 y R5 son, de manera independiente entre sí, halógeno, CF3, CHF2, CH2F, C1-C2-alquilo o C1-C2-alcoxi, y m y n son, de manera independiente entre sí, O ó 1(Ver Formula).

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