Inhibitors of mammalian collagenase

C - Chemistry – Metallurgy – 07 – K

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C07K 5/04 (2006.01) C07C 55/02 (2006.01) C07C 323/52 (2006.01) C07C 323/56 (2006.01) C07K 5/06 (2006.01) C07K 5/083 (2006.01) C07K 5/103 (2006.01)

Patent

CA 1248296

Abstract INHIBITORS OF MAMMALIAN COLLAGENASE Mammalian collagenase is inhibited by compounds of the formula Image or salts thereof, wherein R is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl; R1 is of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; R2 is hydrogen, -(lower alkyl)- Image or -(lower alkyl)- Image ; R3 is Image , Image , Image , Image , Image , Image , -ORg, -Cl, -Br or Image ; R4 is hydrogen, methyl, ethyl, or Image ; R5 and R6 are each independently selected as -OCH3 or -OCH2CH3 or are combined as -OCH2 CH2O- or -O-(CH2)3-O-; R7 and R8 are each independently selected as hydrogen, methyl or ethyl or are combined as -(CH2)4-, -(CH2)5- or -CH2CH2-O-CH2CH2-; R9 is hydrogen, methyl, ethyl Image or Image ; m is an integer from 0 to 7; p is an integer from 1 to 3; AAn is an amino acid chain of from one to three amino acids; n is 1 or 1, 2 or 1, 2, 3; when p is 1, AAn is AAl; when p is 2, AAn is AAl - AA2; when p is 3, AAn is AAl - AA2 - AA3; AA1 is glycine or alanine; AA2 is glycine or alanine; AA3 is leucine, glutamine or isoleucine.

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