C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 263/56 (2006.01) A61K 31/423 (2006.01) A61P 3/04 (2006.01) A61P 3/10 (2006.01) A61P 25/28 (2006.01) C07D 413/04 (2006.01)
Patent
CA 2566923
Compounds, compositions and methods are provided for stabilizing transthyretin and for treating, preventing, or ameliorating one or more symptoms of transthyretin mediated diseases. In one embodiment, the compounds are benzoxazoles and related compounds, where Y is COOH, COOR5, CONR7R8, tetrazolyl, CONHOH, B(OH)2, CONHSO2Ar, CONHCH(R6)COOH, OH, CH2OH or -(CH2)n- C(R6)(NH2)-COOH; X is O, S or NR11; Het is heteroaryl, optionally substituted with halo, OR, alkyl or haloalkyl; and where R, R1-R3, R5-R8 and R11 are as described in the application.
Il est fourni des composés, des compositions et des procédés servant à stabiliser la transthyrétine et à traiter, prévenir ou améliorer un ou plusieurs symptômes de maladies médiées par la transthyrétine. Dans un mode de réalisation, les composés sont des benzoxazoles et des composés apparentés, où Y est COOH, COOR?5¿, CONR?7¿R?8¿, un tétrazolyle, CONHOH, B(OH)¿2?, CONHSO¿2?Ar, CONHCH(R?6¿)COOH, OH, CH¿2?OH ou -(CH¿2?)¿n?-C(R?6¿)(NH¿2?)-COOH ; X est O, S ou NR?11¿ ; Het est un hétéroaryle, facultativement substitué par un halo, OR, un alkyle ou un haloalkyle ; et où R, R?1¿-R?3¿, R?5¿-R?8¿ et R?11¿ sont tels que décrits dans la demande.
Foldrx Pharmaceuticals Inc.
Gowling Lafleur Henderson Llp
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