Abstract: The present invention is directed to a somatostatin antagonist according to formula (I): A1-cyclo {D-Cys-A2-D-Trp-A3-A4-Cys}-A5Y1, wherein A1 is an optionally substituted aromatic a-amino acid; A2 is an optionally substituted aromatic ?-amino acid; A3 is Dab, Dap, Lys or Om; A4 is ?-Hydroxyvaline, Ser, Hser, or Thr; A5 is an optionally substituted D- or L-aromatic amino acid; and Y1 is OH, NH2 or NHR1? where RI is (C1-6)alkyl; wherein each said optionally substituted aromatic amino acid is optionally substituted with one or more substituents each independently selected from the group consisting of halogen, NO2, OH, CN, (C1-6) alkyl, (C2-6) alkenyl, (C2-6) alkynyl, (C1-6)alkoxy, Bzl, O-Bzl, and NR9R10? wherein R9 ad R10 each is independently H, O, or (C1-6) alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of A1 of formula (I) is optionally substituted with a methyl group, provided that there is at least one said methyl group; or a pharmaceutically acceptable salt thereof,

Abstract: The present invention is directed to a method for synthesizing a peptide using solid-state chemistry in which at least one amide bond is N-methylated, wherein said method of synthesis utilizes N-Boc protected amino acids. For example, the a peptide is first synthesized using N-BOC protected amino acids and 4-methylbenzylhydrylamine functionalized 1% cross linked polystyrene resin until reaching the amide bond to be N-methylated. Then, the amino group at the desired methylation site is methylated. If desired, the synthesis of additional peptide using N-BOC protected amino acids may continued until the desired peptide is complete.

Abstract: The present invention is directed to a somatostatin antagonist according to formula (I), wherein A1 is an optionally substituted aromatic ?-amino acid; A2 is an optionally substituted aromatic ?-amino acid; A3 is Dab, Dap, Lys or Orn; A4 is ?-Hydroxyvaline, Ser, Hser, or Thr; A5 is an optionally substituted D- or L-aromatic -amino acid; and Y1 is OH, NH2 or NHR1, or NHR1, where R1 is (C1-6)alkyl; wherein each said optionally substituted aromatic -amino acid is optionally substituted with one or more substituents substituents each independently selected from the group consisting of halogen, NO2, OH, CN, (C1-6)alkyl, (c2-6)alkenyl, (c2-6)alkynyl, (C1-6)alkoxy, Bzl, O-Bzl, and NR9R10, where R9 ad R10 each is independently H, O, or (C1-6)alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of A1 of formula (I) is optionally substituted with a methyl group, provided that there is at least one said methyl group; or a pharmaceutically acceptable salt thereof, and to uses thereof.

Abstract: Claimed are a series of somatostatin agonists and uses thereof, according to formula (I), A1-cyclo[Cys-A2-D-Trp-A3-A4-Cys]-A5-Y1, ??(I) wherein A1, A2, A3, A4, A5 and Y1 are as defined in specification provided that the amine nitrogen of at least one peptide bond is substituted with a methyl group or pharmaceutically acceptable salts thereof.

Abstract: The present invention is directed to a somatostatin antagonist according to formula (I), wherein A1 is an optionally substituted aromatic ∝-amino acid; A2 is an optionally substituted aromatic ∝-amino acid; A3 is Dab, Dap, Lys or Orn; A4 is &bgr;-Hydroxyvaline, Ser, Hser, or Thr; A5 is an optionally substituted D- or L-aromatic -amino acid; and Y1 is OH, NH2 or NHR1, where R1 is (C1-6)alkyl; wherein each said optionally substituted aromatic -amino acid is optionally substituted with one or more substituents each independently selected from the group consisting of halogen, NO2, OH, CN, (C1-6)alkyl, (c2-6)alkenyl, (c2-6)alkynyl, (C1-6)alkoxy, Bzl, O-Bzl, and NR9R10, where R9 ad R10 each is independently H, O, or (C1-6)alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of A1 of formula (I) is optionally substituted with a methyl group, provided that there is at least one said methyl group; or a pharmaceutically acceptable salt thereof, and to uses thereof.

Abstract: Claimed are a series of somatostatin agonists typically characterized by alkylation of the amide nitrogen, and uses thereof.

Abstract: A compound of Formula (I): wherein R is a linkage independently selected from (CH2)12 or (CH2)4O3; and acid addition salts, solvates and hydrates thereof. The compounds have unusually high affinity for muscarinic receptors, and exhibit agonist activity useful in the treatment of neurological and other disorders, in which stimulating cholinergic activity is desirable.

Abstract: A compound of Formula (I): wherein R is independently selected from (CH2)9−12, (CH2CH2)2O, (CH2CH2)3O2, (CH2CH2)4O3, (CH2CH2)5O4, (CH2CH2)6O5 or (CH2CH2CH2)3O2; or an acid addition salt or hydrate thereof. The compounds, with improved water solubility, have unusually high affinity for muscarinic receptors, and exhibit agonist activity useful in the treatment of neurological and other disorders, in which stimulating cholinergic activity is desirable.

Abstract: A compound of Formula (I): ##STR1## wherein R is a linkage independently selected from (CH.sub.2).sub.12 or (CH.sub.2).sub.4 O.sub.3 ; and acid addition salts, solvates and hydrates thereof. The compounds have unusually high affinity for muscarinic receptors, and exhibit agonist activity useful in the treatment of neurological and other disorders, in which stimulating cholinergic activity is desirable.