Iodinated somatostatins

Details Iodinated somatostatins Iodinated somatostatins

C - Chemistry, Metallurgy

07

K

530/7.26, 167/10

C07K 14/655 (2006.01) A61K 38/08 (2006.01) A61K 38/31 (2006.01) C07K 7/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2012115

An octapeptide of the formula: Image wherein each A1 and A2, independently, is H, C1-12 alkyl, C7-10 phenylalkyl, R1CO (where R1 is C1-20 alkyl, C3-20 alkenyl, C3-20 alkynyl, phenyl, naphthyl, or C7-10 phenylalkyl), or R2OCO (where R2 is C1-10 alkyl or C7-10 phenylalkyl), provided that when one of A1 or A2 is R1CO or R2OCO, the other must be H; A3 is CH2-A6 (where A6 is pentafluorophenyl, naphthyl, pyridyl, phenyl, or o-, m-, or, more preferably, p-substituted phenyl, where the substituent is a halogen, NH2, NO2, OH, or C1-3 alkyl); (I) indicates that tyrosine is iodinated on the phenyl ring at its 3 or 5 carbon positions; A5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile, provided that when A3 is phenyl, A1 is H, and A2 is H, A5 cannot be Val; and A7 is Thr, Trp, or .beta.-Nal; or a pharmaceutically acceptable salt thereof.

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