3b Pharmaceuticals Gmbh

Jan Ungewiß

Ulrich Reineke

Frank Osterkamp

Christian Haase

Christiane Smerling

Matthias Paschke

The present invention is related to a compound of formula (I) wherein Ris selected from the group consisting of hydrogen, methyl and cyclopropylmethyl; AA-COOH is an amino acid selected from the group consisting of 2-amino-2-adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3.3.1]nonane-9-carboxylic acid; Ris selected from the group consisting of (C-C)alkyl, (C-C)cycloalkyl, (C-C)cycloalkylmethyl, halogen, nitro and trifluoromethyl; ALK is (C-C)alkylidene; R, Rand Rare each and independently selected from the group consisting of hydrogen and (C-C)alkyl under the proviso that one of R, Rand Ris of the formula (II) wherein ALK' is (C-C)alkylidene; Ris selected from the group consisting of hydrogen and (C-C)alkyl; and Ris selected from the group consisting of H and an Effector moiety; or a pharmacologically acceptable salt, solvate or hydrate thereof. 

Neurotensin receptor ligands

The present invention is related to a conjugate comprising a structure of general formula (1) [TM1]-[AD1]-[LM]-[AD2]-[TM2] (1), wherein TM1 is a first targeting moiety, wherein the first targeting moiety is capable of binding to a first target, AD1 is a first adapter moiety or is absent, LM is a linker moiety or is absent, AD2 is a second adapter moiety or is absent, and TM2 is a second targeting moiety, wherein the second targeting moiety is capable of binding to a second target; wherein the first targeting moiety and/or the second targeting moiety is a compound of formula (2): wherein Ris selected from the group consisting of hydrogen, methyl and cyclopropylmethyl; AA-COOH is an amino acid selected from the group consisting of 2-amino-2 adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3.3.1]nonane-9 carboxylic acid; Ris selected from the group consisting of (C-C)alkyl, (C-C)cycloalkyl, (CC)cycloalkylmethyl, halogen, nitro and trifluoromethyl; ALK' is (C-C)alkylidene; R, Rand Rare each and independently selected from the group consisting of hydrogen and (C-C)alkyl under the proviso that one of R, Rand Ris of the following formula (3) wherein ALK&#x2032; is (C-C)alkylidene; Ris selected from the group consisting of hydrogen and (C-C)alkyl; and Ris a bond; or a pharmacologically acceptable salt, solvate or hydrate thereof. 

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Berlin, Germany

Jan Ungewiß