C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/04 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) A61K 31/435 (2006.01) A61K 31/50 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 38/00 (2006.01) A61K 38/02 (2006.01) A61K 38/05 (2006.01) C07D 487/04 (2006.01) C07D 498/04 (2006.01) C07D 513/04 (2006.01) C07K 2/00 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01)
Patent
CA 2215695
There are disclosed .beta.-sheet mimetics and methods relating to the same for imparting or stabilizing the .beta.-sheet structure of a peptide, protein or molecule. In one aspect, the .beta.-sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The .beta.-sheet mimetics have utility as protease inhibitors generally, including activity as serine protease inhibitors such as thrombin, elastase and Factor X. The .beta.-sheet mimetic has the structure: (see formula I) wherein R1, R2 and R3 are independently selected from amino acid side chain moieties and derivatives thereof; A is selected from -C(=O)-, -(CH2)1-4-, -C(=O)(CH2)1-3-, -(CH2)1-2O- and -(CH2)1-2S-; B is selected from N and CH; C is selected from -C(=O)-, -(CH2)1-3-, -O-, -S-, -O-(CH2)1-2- and -S(CH2)1-2-; Y and Z represent the remainder of the molecule; and any two adjacent CH groups of the bicyclic ring may form a double bond; with the provisos that (i) R1 is an amino acid side chain moiety or derivative thereof other than hydrogen, (ii) when R1 is benzyl, R2 and R3 are both hydrogen, A is -CH2CH2- and B is CH, then C is not -CH2-, (iii) when R1 is methyl, R2 and R3 are both hydrogen, A is -CH2O- and B is CH, then C is not -CH2-, and (iv) when R1 is benzyl, R2 and R3 are both hydrogen, A is - CH2- and B is CH, then C is not -S-.
L'invention concerne des imitateurs de feuillets beta et des procédés afférents destinés à conférer ou à stabiliser la structure de feuillets beta d'un peptide, d'une protéine ou d'une molécule. Dans un aspect, les imitateurs de feuillets beta sont fixés de manière covalente à l'extrémité ou dans la longueur du peptide ou de la protéine. Les imitateurs de feuillets beta présentent une utilité, d'une manière générale, en tant qu'inhibiteurs de protéase, y compris une activité d'inhibiteurs de sérine protéase telle que la thrombine, l'élastase et le facteur X.
Gowling Lafleur Henderson Llp
Molecumetics Ltd.
Myriad Genetics Inc.
LandOfFree
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