P-cadherin ligands

Abstract

The present invention is related to a P-cadherin binding compound; a composition comprising the P-cadherin binding compound; the P-cadherin binding compound and the composition, respectively, for use in a method for the diagnosis of a disease; the P-cadherin binding compound and the composition, respectively, for use in a method for the treatment of a disease; the P-cadherin binding compound and the composition, respectively, for use in a method of diagnosis and treatment of a disease which is also referred to as "thera(g)nosis" or "thera(g)nostics"; the P-cadherin binding compound and the composition, respectively, for use in a method for delivering a radionuclide to a P-cadherin expressing tissue; a method for the diagnosis of a disease using the P-cadherin binding compound and the composition, respectively; a method for the treatment of a disease using the P-cadherin binding compound and the composition, respectively; a method for the diagnosis and treatment of a disease which is also referred to as "thera(g)nosis" or "thera(g)nostics, using the P-cadherin binding compound and the composition, respectively; a method for the delivery of a radionuclide to a P-cadherin expressing tissue using the P-cadherin binding compound and the composition, respectively.

Description

[0001] P-Cadherin Ligands

[0002] FIELD OF THE INVENTION

[0003] The present invention is related to a P-cadherin (P-cad) binding compound; a composition comprising the P-cadherin binding compound; the P-cad binding compound and the composition, respectively, for use in a method for the diagnosis of a disease; the P-cad binding compound and the composition, respectively, for use in a method for the treatment of a disease; the P-cad binding compound and the composition, respectively, for use in a method of diagnosis and treatment of a disease which is also referred to as “thera(g)nosis” or “thera(g)nostics”; the P-cad binding compound and the composition, respectively, for use in a method for delivering a radionuclide to a P-cad expressing tissue; a method for the diagnosis of a disease using the P- cad binding compound and the composition, respectively; a method for the treatment of a disease using the P-cad binding compound and the composition, respectively; a method for the diagnosis and treatment of a disease which is also referred to as “thera(g)nosis” or “thera(g)nostics, using the P-cad binding compound and the composition, respectively; a method for the delivery of a radionuclide to a P-cad expressing tissue using the P-cad binding compound and the composition, respectively.

[0004] BACKGROUND OF THE INVENTION

[0005] Despite the increasing availability of therapeutic options, cancer is still the second leading cause of death globally. The complexity and heterogeneity of cancerous tumors continue to pose severe obstacles. Thus, novel therapeutic approaches that target specific molecules critical to cancer development and progression are continually sought after. P-cadherin, a member of the cadherin superfamily, has garnered considerable attention as a potential therapeutic target due to its important role in cell adhesion, allowing cells to bind together and form tissues.

[0006] The Cadherin Superfamily and P-cadherin

[0007] The name Cadherin was derived from the superfamily's main function, namely the "calciumdependent adhesion". The superfamily comprises a group of transmembrane proteins involved in cell-cell adhesion and communication. They play a crucial role in various cellular processes, such as tissue morphogenesis, embryonic development, and maintenance of tissue integrity in adult organisms (van Roy, Nat Rev Cancer, 2014, 14, 121-134). Cadherins are characterized by the presence of extracellular cadherin domains responsible for homophilic calcium-dependent binding with cadherin molecules on adjacent cells (Niessen et al., Physiol Rev, 2011, 91, 691- 731).

[0008] P-cadherin was described for the first time in 1986, as part of “a novel class of cadherins that appeared in developing mouse embryos” and its name is derived from the site where this adhesion molecule was firstly characterized, the placenta (Nose et al., J Cell Biol, 1986, 103, 2649-2658). P-cadherin, which is also known as placental cadherin or cadherin-3, is a member of the classical type I cadherins family, whose members are known for mainly mediating cell adhesion by homophilic interactions. P-cadherin is widely expressed in various tissues during embryonic development and has a more restricted distribution in adult tissues (Hirai et al., Development, 1989, 105, 263-270). Notably, P-cadherin is particularly abundant in epithelial tissues and is significantly upregulated in numerous cancer types.

[0009] Additional members of the classical type I cadherin family are neural cadherin (N-cadherin), epithelial cadherin (E-cadherin), muscle cadherin (M-cadherin) and retinal cadherin (R- cadherin). While initially named after the tissues where they were initially discovered, it is important to note that the presence of cadherins extends beyond the confines of these specific tissues. Many subtypes have since been identified in other species and there are now more than 100 known members in this superfamily (Stemmier, MolBiosyst, 2008, 4, 835-850). E-cadherin shares the highest sequence homology with P-cadherin (around 66%) (Nollet et al., J Mol Biol, 2000, 299, 551-572). E-cadherin forms the key functional component of adherens junctions of epithelial cell and plays a vital role in the establishment and maintenance of intercellular adhesion, cell polarity, and tissue architecture.

[0010] P-cadherin and Cancer

[0011] In recent years, a growing body of evidence has linked P-cadherin to the onset and advancement of diverse cancers, encompassing breast, ovarian, lung, pancreatic, and gastric cancer, among others (see Table 1). Its overexpression has been associated with aggressive phenotypes, increased tumor invasiveness, and enhanced metastatic potential (Vieira et al., Mol Cancer, 2015, 14, 178). In tumor cells, P-cadherin promotes the loss of cell-cell adhesion, leading to enhanced cell motility and invasion, crucial steps in metastasis. Studies have also linked P-cadherin to cancer stem cell properties, conferring self-renewal and chemoresistance capabilities to the tumor cells (Ribeiro et al., Front Oncol, 2014, 4, 371). Additionally, P-cadherin has been shown to modulate various signaling pathways, including Wnt / p-catenin, PI3K / AKT, and MAPK, further contributing to tumor growth and survival (Vieira et al., Mol Cancer, 2015, 14, 178).

[0012] Table 1: P-cadherin expression in primary tumors and its relevance in malignancy. The tumor promoting or tumor suppressive effects associated with P-cadherin expression is dependent on the cellular and tissue context (Table modified from (Vieira et al., Mol Cancer, 2015, 14, 178))

[0013] Expression in neoplastic

[0014] Malignancy tissue / cells in comparison to Behavior normal tissue / cells

[0015] Breast cancer Up-regulation Tumor promoting

[0016] Gastric cancer Up-regulation Tumor promoting

[0017] Endometrial cancer Up-regulation Tumor promoting

[0018] Ovarian cancer Up-regulation Tumor promoting

[0019] Pancreatic cancer

[0020] Basocellular and squamous

[0021] Up-regulation Tumor promoting carcinoma of the skin

[0022] Cholangiocarcinoma Up-regulation Tumor promoting

[0023] Up-regulation Tumor promoting

[0024] Colorectal carcinoma

[0025] Down-regulation Tumor suppressive

[0026] Up-regulation Tumor promoting

[0027] Bladder cancer

[0028] Down-regulatio Tumor suppressive

[0029] Prostate cancer Up-regulation Tumor promoting

[0030] Down-regulation Tumor suppressive

[0031] Melanoma Down-regulation Tumor suppressive

[0032] Oral squamous cell carcinoma Down-regulation Tumor suppressive

[0033] Hepatocellular carcinoma Down-regulation Tumor suppressive Rationale for Targeting P-cadherin

[0034] Given the critical role of P-cadherin in promoting tumorigenesis and metastasis, its targeting presents a promising strategy for cancer therapy. Since P-cadherin is mainly expressed in the tumor cells rather than in surrounding stroma, it represents an attractive tumor-specific target, reducing potential off-target effects.

[0035] State of the Art

[0036] The main compound class so far for targeting P-cad are antibodies and their derivatives. They have been investigated for inhibiting expression or function of P-cad (e.g., W02006114704A2), stimulating immune response (e.g., W02016001810A1) or delivery of cytotoxic payloads (e.g., W02016075670A1, WO2011099524A1). Typically, these antibody-based compounds of the prior art targeting P-cad suffer from at least one of the following shortcomings rendering them unsuitable for use in the diagnosis and / or treatment, respectively, of a subject such as a human being: immunogenicity, unfavorable pharmacokinetic behavior, insufficient pharmacological activity, and limited preclinical and / or clinical data. However, P-cad-modulating small molecules and peptide-based approaches have been scarcely described.W02009025116Al discloses immunogenic peptides that can serve as vaccine for cancers highly expressing P-cad.

[0037] Recent studies also point to the potential use of the anti-cancer protein azurin in P-cadherin overexpressing breast cancer models (Bernardes et al, PLoS One, 2013, 8, e69023; Bernardes et al.. Ini J Biochem Cell Biol, 2014, 50, 1-9; Warso etal., Br J Cancer, 2013, 108, 1061-1070).

[0038] DETAILED DESCRIPTION OF THE INVENTION

[0039] The problem underlying the present invention is the provision of a compound (a peptide, e.g., having a molecular weight of less than 10000) which is suitable as a diagnostic agent and / or a therapeutic agent, particularly if it comprises an effector such as a cytotoxic drug or a chelator comprising a diagnostically and / or therapeutically active radionuclide.

[0040] A further problem underlying the present invention is the provision of a compound which is suitable as a diagnostic agent and / or a therapeutic agent, particularly if it comprises a diagnostically and / or therapeutically active radionuclide, said compound having a pICso of equal to or greater than 6.0 for P-cad, i.e., an IC50 equal or less than 1.0 pM for P-cad.

[0041] A further problem underlying the present invention is the provision of a compound which is suitable as a diagnostic agent and / or a therapeutic agent, particularly if it comprises a diagnostically and / or therapeutically active radionuclide, in the diagnosis and / or therapy of a disease where the diseased cells and / or diseased tissues express P-cad. A still further problem underlying the instant invention is the provision of a compound which is suitable for delivering a diagnostically and / or therapeutically effective radionuclide to a diseased cell and / or diseased tissue, respectively, and more particularly a P-cad-expressing diseased cell and / or diseased tissue, preferably the diseased tissue comprises cancer or tumor cells.

[0042] Also, a problem underlying the present invention is the provision of a method for the diagnosis of a disease, of a method for the treatment and / or prevention of a disease, and a method for the combined diagnosis and treatment of a disease; preferably such disease is a disease involving P-cad-expressing cells and / or tissues, more particularly a P-cad-expressing diseased cell and / or diseased tissue, preferably the diseased tissue comprises or contains cancer or tumor cells.

[0043] A still further problem underlying the present invention is the provision of a method for the identification of a subject, wherein the subject is likely to respond or likely not to respond to a treatment of a disease, a method for the selection of a subject from a group of subjects, wherein the subject is likely to respond or likely not to respond to a treatment of a disease; preferably, the disease is cancer, more preferably the disease is a solid tumor.

[0044] Also, a problem underlying the present invention is the provision of a pharmaceutical composition containing a compound having the characteristics as outlined above. Furthermore, a problem underlying the present invention is the provision of a kit which is suitable for use in any of the above methods.

[0045] The above problems are solved by the subject matter of the attached independent claims; preferred embodiments may be taken from the attached dependent claims. In particular, the present invenrtion provides a compound which is suitable as a diagnostic agent and / or a therapeutic agent, particularly if it comprises a diagnostically and / or therapeutically active radionuclide.

[0046] The compound of the present invention comprises a peptide, which is represented by the following formula (I):

[0047] H - Xaal - Xaa2 - Xaa3 - Xaa4 - Xaa5 - Xaa6 - Xaa7 - Cext (I) or a pharmaceutically acceptable salt thereof, wherein, Xaal is (a) a residue of an a-amino acid comprising a side chain and one N- terminal modification group Nmod covalently attached to the a-nitrogen atom of the amino acid, preferably a residue of an L-a-amino acid comprising a side chain and one N-terminal modification group Nmod covalently attached to the a-nitrogen atom of the amino acid, wherein Nmod is a group containing one or more selected from hydrogen, carbon, nitrogen oxygen and sulfur and optionally comprises a group Zla, wherein the side chain of Xaal optionally comprises a group Zlb, wherein the side chain of Xaal and the a-nitrogen atom of Xaal optionally form a heterocycle, with the proviso that if the side chain of Xaal and the a-nitrogen atom of Xaal form a heterocycle, the N-terminal modification group Nmod is absent, or

[0048] (b) a residue of an L-a-hydroxy acid comprising a side chain, wherein the side chain optionally comprises a group Zlb,

[0049] H is a hydrogen atom which is covalently attached to (a) the a-nitrogen atom of Xaal if Xaal is a residue of an a-amino acid comprising a side chain and one N-terminal modification group Nmod covalently attached to the a-nitrogen atom of the amino acid, or (b) the oxygen atom of the a-hydroxy group of Xaal if Xaal is a residue of an L-a-hydroxy acid comprising a side chain,

[0050] Xaa2 is a residue of an L-a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain comprises an optionally substituted indole or benzothiophene group,

[0051] Xaa3 is a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z2,

[0052] Xaa4 is a residue of an L-a-amino acid comprising a hydrophobic side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain of Xaa4 and the a-nitrogen atom of Xaa4 optionally form a heterocycle,

[0053] Xaa5 is a residue of an a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z3,

[0054] Xaa6 is a residue of an a-amino acid comprising a side chain, preferably a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z4, wherein the side chain of Xaa6 and the a-nitrogen atom of Xaa6 optionally form a heterocycle,

[0055] Xaa7 is a residue of an L-a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain comprises an aryl or heteroaryl group, preferably a bicyclic aryl or heteroaryl group,

[0056] Cext is a moiety covalently attached to the carbonyl group of Xaa7, which is represented by one of the formulae (la), (lb), (Ic), (Id), and (le):

[0057] Cterm (la)

[0058] Xaa8 - Cterm (lb)

[0059] Xaa8 - Xaa9 - Cterm (Ic)

[0060] Xaa8 - Xaa9 - XaalO - Cterm (Id)

[0061] Xaa8 - Xaa9 - XaalO - Xaal 1 (le) wherein,

[0062] Xaa8 is a residue of glycine or a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z5,

[0063] Xaa9 is a residue of an a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, preferably Xaa9 is a residue of an L-a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain optionally comprises a group Z6, wherein the side chain of Xaa9 and the a-nitrogen atom of Xaa9 optionally form a heterocycle,

[0064] XaalO is a residue of an a-amino acid comprising a side chain, preferably a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z7, wherein the side chain of XaalO and the a-nitrogen atom of XaalO optionally form a heterocycle,

[0065] Xaal l is a residue of a compound comprising an amino group and optionally comprising a carbonyl group, wherein the amino group is covalently attached to the carbonyl group of XaalO, wherein if the carbonyl group is present, said carbonyl group is covalently attached to a C-terminal modification group Cterm, preferably Xaal 1 is

[0066] (a) a residue of an a-amino acid comprising a side chain, a C-terminal modification group Cterm and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain optionally comprises a group Z8, wherein the side chain of Xaal l and the a-nitrogen atom of

[0067] Xaal 1 optionally form a heterocycle, or

[0068] (b) a residue of an optionally substituted P-amino alcohol, or

[0069] (c) a residue of a (C1-C6)alkylamine such as cyclohexylamine, or of a (C2- Ce)alkyldiamine such as ethylenediamine,

[0070] Cterm is a C-terminal modification group, which is selected from the group consisting of -NH2, -OH, a group Z9, and -NHRcterm, wherein Rctermis selected from group consisting of a (Ci-Ce)alkyl group, a benzyl group, a 2-phenylethyl group and a 3 -phenylpropyl group, each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently an effector E, such as a chelator, which may optionally comprise a linker moiety L that covalently links the effector E to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, the effector E being preferably selected from the group consisting of:

[0071] (a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and

[0072] (P) a chelator optionally comprising a radionuclide; and

[0073] (y) a drug, preferably a cytotoxic drug; and

[0074] (5) an immune cell engaging effector, preferably recruiting and stimulating T cells, natural killer cells (NK cells) and / or phagocytotic cells.

[0075] 1. DEFINITIONS

[0076] Unless stated otherwise, the following terms and phrases as used herein are intended to have the following meanings.

[0077] The term “linkage” as used herein refers an attachment of two atoms of two independent moieties. A preferred linkage is a chemical bond or a plurality of chemical bonds. More preferably, a chemical bond is a covalent bond or a plurality of chemical bonds. Most preferably, the linkage is a covalent bond or a coordinate bond. As preferably used herein, an embodiment of a coordinate bond is a bond or group of bonds as realized when a metal is bound (e.g., chelated) by a chelator. Depending on the type of atoms linked and their atomic environment different types of linkages are created. These types of linkage are defined by the type of atom arrangements created by the linkage.

[0078] For instance, the linking of a moiety comprising an amine with a moiety comprising a carboxylic acid leads to a linkage named “amide” (which may also be referred to as amide linkage, -CO-N-, -N-CO-). It will be acknowledged by a person skilled in the art that this and the following examples of creating linkages are only prototypical examples and are by no means limiting the scope of the present invention. It will be acknowledged by a person in the art that the linking of a moiety comprising an isothiocyanate with a moiety comprising an amine leads to a thiourea (which may also be referred to as a thiourea linkage, -N-C(=S)-N-), and linking of a moiety comprising a C atom with a moiety comprising a thiol-group (-C-SH) leads to a thioether (which may also be referred to as a thioether linkage, -C-S-C-). A non-limiting list of linkages as used, for example, in connection with the effector and linker of the invention and their characteristic type of atom arrangement is given Table 2. Table 2:

[0079] Examples of reactive groups which, in some embodiments of the invention, are used in the formation of linkages, for example between the effector and the linker or directly between the effector and the rest of the compound of the invention (peptide), are summarized in Table 3. It will, however, be understood by a person skilled in the art that neither the linkages which may be realized in embodiments of the present invention are limited to the ones of Table 3 nor the reactive groups forming such linkages.

[0080] Table 3:

[0081] The following are reactive groups and functionalities which are utilized or amenable of forming linkages between moieties or structures as used in embodiments of the present invention: Primary or secondary amino, carboxylic acid (carboxyl), activated carboxylic acid, chloro, bromo, iodo, sulfhydryl, hydroxyl, sulfonic acid, activated sulfonic acid, sulfonic acid esters like mesylate or tosylate, Michael acceptors, strained alkenes like trans cyclooctene, isocyanate, isothiocyanate, azide, alkyne and tetrazine.

[0082] The term “activated carboxylic acid” as used herein refers to a carboxylic acid group with the general formula -CO-X, wherein X is a leaving group. For example, activated forms of a carboxylic acid group may include, but are not limited to, acyl chlorides, symmetrical or unsymmetrical anhydrides, and esters. Preferably, the activated carboxylic acid group is an ester with pentafluorophenol, nitrophenol, benzotri azole, azabenzotri azole, thiophenol or N- hydroxysuccinimide (NHS) as leaving group.

[0083] The expression “mediating a linkage” as used herein means that a linkage or a type of linkage is established, preferably a linkage between two moieties. In a preferred embodiment, the linkage and the type of linkage is as defined herein.

[0084] Unless indicated otherwise, when it is referred in the present disclosure to a range indicated by a lower integer and a higher integer such as, for example, 1-4, such range is a representation of the lower integer, the higher integer and any integer between the lower integer and the higher integer. Insofar, the range is actually an individualized disclosure of said integer. In said example, the range of 1-4 thus means 1, 2, 3 and 4.

[0085] The term “alkyl” as used herein characterizes a saturated, straight-chain or branched hydrocarbon group and may be accompanied by a qualifier which specifies the number of carbon atoms it contains. For example, the expression (C1-C3)alkyl means each and individually any of methyl, ethyl, n-propyl and isopropyl. An alkyl group can be unsubstituted or substituted with one or more groups, including, but not limited to, -O-[(C1- C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO-NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -((C1-C8))alkyl and aryl. If the alkyl group comprises CH2 groups, a CH2group can optionally be replaced by an S or O atom.

[0086] The term “(C1-C2)alkyl” as used herein refers any of methyl and ethyl.

[0087] The term “(C1-C3)alkyl” as used herein refers to any of methyl, ethyl, n-propyl and isopropyl.

[0088] The term “(C1-C4)alkyl” as used herein refers to a saturated or unsaturated, straight-chain or branched hydrocarbon group having from 1 to 4 carbon atoms. Representative examples of (C1- C4)alkyl include, but are not limited to, any of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl and tert-butyl.

[0089] The term “(C1-C6)alkyl” as used herein refers to a saturated or unsaturated, straight-chain or branched hydrocarbon group having from 1 to 6 carbon atoms. Representative examples of (Ci- Ce)alkyl include, but are not limited to, any of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2-methyl-butyl, 3 -methyl -butyl, 3-pentyl, 3- methyl-but-2-yl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-hexyl, 2-methyl-pentyl, 3- methyl-pentyl, 4-methyl-pentyl, 3 -hexyl, 2-ethyl -butyl, 2-methyl-pent-2-yl, 2,2-dimethyl- butyl, 3,3-dimethyl-butyl, 3 -methyl-pent-2 -yl, 4-methyl-pent-2-yl, 2,3-dimethyl-butyl, 3- m ethyl-pent-3 -yl, 2-m ethyl-pent-3 -yl, 2,3-dimethyl-but-2-yl and 3,3-dimethyl-but-2-yl. A (C1- Ce)alkyl group can be unsubstituted or substituted with one or more groups, including, but not limited to, -O-[(C1-C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO- NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -(C1-C8)alkyl and aryl.

[0090] The term “(C1-C8)alkyl” as used herein refers to a saturated or unsaturated, straight-chain or branched hydrocarbon group having from 1 to 8 carbon atoms. Representative (C1-C8)alkyl groups include, but are not limited to, any of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2-methyl-butyl, 3 -methyl -butyl, 3-pentyl, 3- methyl-but-2-yl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-hexyl, 2-methyl-pentyl, 3- methyl-pentyl, 4-methyl-pentyl, 3 -hexyl, 2-ethyl -butyl, 2-methyl-pent-2-yl, 2,2-dimethyl- butyl, 3,3-dimethyl-butyl, 3 -methyl-pent-2 -yl, 4-methyl-pent-2-yl, 2,3-dimethyl-butyl, 3- m ethyl-pent-3 -yl, 2-methyl-pent-3-yl, 2,3-dimethyl-but-2-yl, 3,3-dimethyl-but-2-yl, n-heptyl,

[0091] 2-heptyl, 2-methyl-hexyl, 3-methyl-hexyl, 4-methyl-hexyl, 5-methyl-hexyl, 3-heptyl, 2-ethyl- pentyl, 3-ethyl-pentyl, 4-heptyl, 2-methyl-hex-2-yl, 2,2-dimetyhl-pentyl, 3,3-dimetyhl-pentyl,

[0092] 4.4-dimetyhl-pentyl, 3 -methyl-hex-2 -yl, 4-methyl-hex-2-yl, 5-methyl-hex-2-yl, 2,3-dimethyl- pentyl, 2,4-dimethyl-pentyl, 3,4-dimethyl-pentyl, 3-methyl-hex-3-yl, 2-ethyl-2-methyl-butyl, 4-methyl-hex-3-yl, 5-methyl-hex-3-yl, 2-ethyl-3-methyl-butyl, 2,3 -dimethyl-pent-2 -yl,

[0093] 2.4-dimethyl-pent-2-yl, 3, 3 -dimethyl-pent-2 -yl, 4,4-dimethyl-pent-2-yl, 2,2,3-trimethyl-butyl,

[0094] 2.3.3-trimethyl-butyl, 2,3,3-trimethyl-but-2-yl, n-octyl, 2-octyl, 2-methyl-heptyl,

[0095] 3-methyl-heptyl, 4-methyl-heptyl, 5 -methyl -heptyl, 6-methyl-heptyl, 3-octyl, 2-ethyl-hexyl,

[0096] 3-ethyl-hexyl, 4-ethyl-hexyl, 4-octyl, 2-propyl-pentyl, 2-methyl-hept-2-yl, 2,2-dimethyl-hexyl,

[0097] 3.3-dimethyl-hexyl, 4,4-dimethyl-hexyl, 5,5-dimethyl-hexyl, 3-methyl-hept-2-yl,

[0098] 4-methyl-hept-2-yl, 5-methyl-hept-2-yl, 6-methyl-hept-2-yl, 2,3 -dimethyl-hex- 1-yl,

[0099] 2.4-dimethyl-hex-l-yl, 2,5-dimethyl-hex-l-yl, 3,4-dimethyl-hex-l-yl, 3,5-dimethyl-hex-l-yl,

[0100] 3.5-dimethyl-hex-l-yl, 3-methyl-hept-3-yl, 2-ethyl-2-methyl-l-yl, 3 -ethyl-3 -methyl- 1-yl, 4-methyl-hept-3-yl, 5-methyl-hept-3-yl, 6-methyl-hept-3-yl, 2-ethyl-3-methyl-pentyl,

[0101] 2-ethyl-4-methyl-pentyl, 3-ethyl-4-methyl-pentyl, 2,3-dimethyl-hex-2-yl, 2,4-dimethyl-hex-2- yl, 2,5-dimethyl-hex-2-yl, 3,3-dimethyl-hex-2-yl, 3,4-dimethyl-hex-2-yl, 3,5-dimethyl-hex-2- yl, 4,4-dimethyl-hex-2-yl, 4,5-dimethyl-hex-2-yl, 5,5-dimethyl-hex-2-yl, 2,2,3-trimethyl- pentyl, 2,2,4-trimethyl-pentyl, 2,3,3-trimethyl-pentyl, 2,3,4-trimethyl-pentyl, 2,4,4-trimethyl- pentyl, 3,3,4-trimethyl-pentyl, 3,4,4-trimethyl-pentyl, 2,3,3-trimethyl-pent-2-yl, 2,3,4- trimethyl-pent-2-yl, 2,4,4-trimethyl-pent-2-yl, 3,4,4-trimethyl-pent-2-yl, 2, 2,3,3 -tetram ethylbutyl, 3,4-dimethyl-hex-3-yl, 3,5-dimethyl-hex-3-yl, 4,4-dimethyl-hex-3-yl, 4,5-dimethyl-hex-

[0102] 3-yl, 5,5-dimethyl-hex-3-yl, 3 -ethyl-3 -m ethyl-pent-2 -yl, 3-ethyl-4-methyl-pent-2-yl, 3-ethyl- hex-3-yl, 2,2-diethyl-butyl, 3 -ethyl-3 -methyl-pentyl, 4-ethyl-hex-3-yl, 5-methyl-hept-3-yl, 2- ethyl-3-methyl-pentyl, 4-methyl-hept-4-yl, 3-methyl-hept-4-yl, 2-methyl-hept-4-yl, 3-ethyl- hex-2-yl, 2-ethyl-2-methyl-pentyl, 2-isopropyl-pentyl, 2,2-dimethyl-hex-3-yl, 2,2,4-trimethyl- pent-3-yl and 2-ethyl-3 -methyl-pentyl. A ((C1-C)8)alkyl group can be unsubstituted or substituted with one or more groups, including, but not limited to, -O-[(C1-C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO-NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -((C1-C)8)alkyl and aryl. The term “(C2-C4)alkyl” as used herein refers to a saturated or unsaturated, straight-chain or branched hydrocarbon group having from 2 to 4 carbon atoms. Representative examples of (C2- C4)alkyl include, but are not limited to, any of ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec- butyl and tert-butyl.

[0103] The term “(C3-Cs)alkyl” as used herein refers to a saturated or unsaturated, straight-chain or branched hydrocarbon group having from 3 to 4 carbon atoms. Representative examples of (C3- C4)alkyl include, but are not limited to, any of n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2-methyl-butyl, 3 -methyl -butyl, 3 -pentyl, 3-methyl-but-2-yl, 2- methyl-but-2-yl and 2,2-dimethylpropyl. A (C3-Cs)alkyl group can be unsubstituted or substituted with one or more groups, including, but not limited to, -O-[(Ci- C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO-NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -((C1-C)8)alkyl and aryl.

[0104] The term “(C3-Cs)alkyl” as used herein refers to a saturated or unsaturated, straight-chain or branched hydrocarbon group having from 3 to 8 carbon atoms. Representative (C3-C8)alkyl groups include, but are not limited to, any of n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2-methyl-butyl, 3 -methyl -butyl, 3 -pentyl, 3-methyl-but-2-yl, 2- methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-hexyl, 2-methyl-pentyl, 3-methyl-pentyl, 4- methyl-pentyl, 3 -hexyl, 2-ethyl-butyl, 2-methyl-pent-2-yl, 2,2-dimethyl-butyl, 3, 3 -dimethylbutyl, 3 -methyl-pent-2 -yl, 4-methyl-pent-2-yl, 2,3-dimethyl-butyl, 3 -methyl-pent-3 -yl, 2- m ethyl-pent-3 -yl, 2,3-dimethyl-but-2-yl, 3,3-dimethyl-but-2-yl, n-heptyl, 2-heptyl, 2-m ethylhexyl, 3-methyl-hexyl, 4-methyl-hexyl, 5-methyl-hexyl, 3-heptyl, 2-ethyl-pentyl, 3-ethyl- pentyl, 4-heptyl, 2-methyl-hex-2-yl, 2, 2-dimetyhl -pentyl, 3,3-dimetyhl-pentyl, 4,4-dimetyhl- pentyl, 3 -methyl-hex-2 -yl, 4-methyl-hex-2-yl, 5-methyl-hex-2-yl, 2,3-dimethyl-pentyl,

[0105] 2.4-dimethyl-pentyl, 3,4-dimethyl-pentyl, 3 -methyl-hex-3 -yl, 2-ethyl-2-methyl-butyl, 4-methyl-hex-3-yl, 5-methyl-hex-3-yl, 2-ethyl-3-methyl-butyl, 2,3 -dimethyl-pent-2 -yl,

[0106] 2.4-dimethyl-pent-2-yl, 3, 3 -dimethyl-pent-2 -yl, 4,4-dimethyl-pent-2-yl, 2,2,3-trimethyl-butyl,

[0107] 2.3.3-trimethyl-butyl, 2,3,3-trimethyl-but-2-yl, n-octyl, 2-octyl, 2-methyl-heptyl, 3-methyl-heptyl, 4-methyl-heptyl, 5 -methyl -heptyl, 6-methyl-heptyl, 3-octyl, 2-ethyl-hexyl,

[0108] 3-ethyl-hexyl, 4-ethyl-hexyl, 4-octyl, 2-propyl-pentyl, 2-methyl-hept-2-yl, 2,2-dimethyl-hexyl,

[0109] 3.3-dimethyl-hexyl, 4,4-dimethyl-hexyl, 5,5-dimethyl-hexyl, 3-methyl-hept-2-yl,

[0110] 4-methyl-hept-2-yl, 5-methyl-hept-2-yl, 6-methyl-hept-2-yl, 2,3 -dimethyl-hex- 1-yl,

[0111] 2.4-dimethyl-hex-l-yl, 2,5-dimethyl-hex-l-yl, 3,4-dimethyl-hex-l-yl, 3,5-dimethyl-hex-l-yl,

[0112] 3.5-dimethyl-hex-l-yl, 3-methyl-hept-3-yl, 2-ethyl-2-methyl-l-yl, 3 -ethyl-3 -methyl- 1-yl, 4-methyl-hept-3-yl, 5-methyl-hept-3-yl, 6-methyl-hept-3-yl, 2-ethyl-3-methyl-pentyl,

[0113] 2-ethyl-4-methyl-pentyl, 3-ethyl-4-methyl-pentyl, 2,3-dimethyl-hex-2-yl, 2,4-dimethyl-hex-2- yl, 2,5-dimethyl-hex-2-yl, 3,3-dimethyl-hex-2-yl, 3,4-dimethyl-hex-2-yl, 3,5-dimethyl-hex-2- yl, 4,4-dimethyl-hex-2-yl, 4,5-dimethyl-hex-2-yl, 5,5-dimethyl-hex-2-yl, 2,2, 3 -trimethylpentyl, 2,2,4-trimethyl-pentyl, 2,3,3-trimethyl-pentyl, 2,3,4-trimethyl-pentyl, 2,4,4-trimethyl- pentyl, 3,3,4-trimethyl-pentyl, 3,4,4-trimethyl-pentyl, 2,3,3-trimethyl-pent-2-yl, 2,3,4- trimethyl-pent-2-yl, 2,4,4-trimethyl-pent-2-yl, 3,4,4-trimethyl-pent-2-yl, 2, 2,3,3 -tetram ethylbutyl, 3,4-dimethyl-hex-3-yl, 3,5-dimethyl-hex-3-yl, 4,4-dimethyl-hex-3-yl, 4,5-dimethyl-hex-

[0114] 3-yl, 5,5-dimethyl-hex-3-yl, 3 -ethyl-3-m ethyl-pent-2 -yl, 3-ethyl-4-methyl-pent-2-yl, 3-ethyl- hex-3-yl, 2,2-diethyl-butyl, 3-ethyl-3-methyl-pentyl, 4-ethyl-hex-3-yl, 5-methyl-hept-3-yl, 2- ethyl-3-methyl-pentyl, 4-methyl-hept-4-yl, 3-methyl-hept-4-yl, 2-methyl-hept-4-yl, 3-ethyl- hex-2-yl, 2-ethyl-2-methyl-pentyl, 2-isopropyl-pentyl, 2,2-dimethyl-hex-3-yl, 2,2,4-trimethyl- pent-3-yl and 2-ethyl-3-methyl-pentyl. A (Cri-Csjalkyl group can be unsubstituted or substituted with one or more groups, including, but not limited to, -O-[(C1-C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO-NR’2, - NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -(C1-C8)alkyl and aryl.

[0115] The term “carbocycle” as used herein refers to a saturated or unsaturated non-aromatic hydrocarbon ring and is usually accompanied by a qualifier which specifies the number of carbon atoms it may contain. For example, representative (C3-C4)carbocycles include but are not limited to any of a cyclopropyl and cyclobutyl group. A carbocycle may contain one ring or two or more rings that are fused together. A carbocycle can be unsubstituted or substituted with one or more groups, including, but not limited to, -((C1-C)8)alkyl, -O-[(Ci- C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO-NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -(C1-C8)alkyl and aryl. A ring CH2 group of the carbocycle can optionally be replaced by an S or O atom.

[0116] The term “heterocycle” as used herein refers to a saturated or unsaturated non-aromatic heterocyclic ring and is usually accompanied by a qualifier which specifies the number of carbon atoms it may contain. For example, representative (C5-C6)heterocycles include but are not limited to any of a tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, oxathiolanyl, sulfolanyl, thianyl, tetrahydropyranyl, piperidinyl, morpholinyl, thiomorpholinyl, dioxanyl, dithianyl and trithianyl group. A heterocycle may contain one ring or two or more rings that are fused together, preferably it contains one ring. The term “(C3-C4)carbocycle” as used herein refers to a 3- or 4-membered saturated or unsaturated non-aromatic carbocyclic ring. Representative (C3-C4)carbocycles include, but are not limited to, any of a cyclopropyl, cyclobutyl, and cyclobutenyl group. A (C3-C4)carbocycle group can be unsubstituted or substituted with one or more groups, including, but not limited to, (C1-C8)alkyl, -O-[(C1-C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO-NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -(C1-C8)alkyl and aryl. A CH2 group of the (C3- C4)carbocycle ring can optionally be replaced by an S or O atom.

[0117] The term “(C3-C7)carbocycle” as used herein refers to a 3-, 4-, 5-, 6- or 7-membered saturated or unsaturated non-aromatic carbocyclic ring. Representative (C3-C7)carbocycles include, but are not limited to, any of a cyclopropyl, cyclobutyl, cyclobutenyl, cyclopentyl, cyclopentadienyl, cyclohexyl, cyclohexenyl, 1,3 -cyclohexadienyl, 1,4-cyclohexadienyl, cycloheptyl, 1,3 -cycloheptadienyl and 1,3,5-cycloheptatrienyl group. A (C3-C7)carbocycle group can be unsubstituted or substituted with one or more groups, including, but not limited to, (C1-C8)alkyl, -O-[(C1-C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO-NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -(C1-C8)alkyl and aryl. A CH2 group of the (C3- C7)carbocycle ring can optionally be replaced by an S or O atom.

[0118] The term “(Cs-C6)carbocycle” as used herein refers to a 5- or 6-membered saturated or unsaturated non-aromatic carbocyclic ring. Representative (C5-Ce)carbocycles include, but are not limited to, any of a cyclopentyl, cyclopentenyl, cyclopentadienyl, cyclohexyl, cyclohexenyl, 1,3 -cyclohexadienyl and 1,4-cyclohexadienyl group. A (C5-Ce)carbocycle group can be unsubstituted or substituted with one or more groups, including, but not limited to, (Ci- C8)alkyl, -O-[(C1-C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO- NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -(C1-C8)alkyl and aryl. A CH2 group of the (C5- Ce)carbocycle ring can optionally be replaced by an S or O atom. The term “(Ci- C6)alkylamine” as used herein refers to a saturated or unsaturated, straight-chain, branched or cyclic hydrocarbon group having from 1 to 6 carbon atoms, which is substituted with one -NH2 group. Representative (C1-C6)alkylamines include, but are not limited to, any of cyclohexylamine, cyclopentylamine, cyclobutylamine, n-hexylamine, n-pentylamine, n- butylamine, n-propylamine, n-ethylamine, methylamine, isopropylamine, isobutylamine, isopentylamine, isohexylamine, tert-butylamine, neopentylamine and neohexylamine. The term “(C2-C6)alkyldiamine” as used herein refers to a saturated or unsaturated, straightchain, branched or cyclic hydrocarbon group having from 1 to 6 carbon atoms, which is substituted with two -NH2 groups, preferably in vicinal positions. Representative (C2- Ce)alkyldiamines include, but are not limited to, any of ethylendiamine, 1,2-diaminopropane, 1,2-diaminobutane, 1,2-diaminopentane, 1,2-diaminohexane, 2,3 -diaminobutane, 2,3- diaminopentane, 2,3 -diaminohexane, 3,4-diaminohexane, 1,2-diaminocyclohexane, 1,2- diaminocyclopentane and 1,2-diaminocyclobutane.

[0119] The term “aliphatic” as used herein refers to an alkyl or carbocycle group as defined herein.

[0120] The term “(C3-C7)heterocycle” as used herein refers to a 3-, 4-, 5-, 6- or 7-membered saturated or unsaturated non-aromatic heterocyclic ring. Representative (C3-C7)heterocycles include, but are not limited to, any of a aziridinyl, oxiranyl, thiiranyl, azetidinyl, oxetanyl, thietanyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, oxathiolanyl, sulfolanyl, thianyl, tetrahydropyranyl, piperidinyl, morpholinyl, thiomorpholinyl, dioxanyl, dithianyl, trithianyl, oxepanyl, thiepanyl and azepanyl, group. A (C3-C7)heterocycle group can be unsubstituted or substituted with one or more groups, including, but not limited to, (C1-C8)alkyl, -O-[(C1- C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO-NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -(C1-C8)alkyl and aryl.

[0121] The term “aryl” or “aryl ring” as used herein refers to a carbocyclic aromatic group, wherein the carbocyclic aromatic group is selected from the group consisting of aromatic groups with a single ring and aromatic groups with two or more fused rings, preferably two rings. Examples of carbocyclic aromatic groups with a single benzene ring include, but are not limited to, phenyl, and examples of carbocyclic aromatic groups with two or more fused benzene rings include, but are not limited to naphthyl and anthracenyl. For example, representative (Ce-Cio)aryl groups include but are not limited to any of a phenyl and naphthyl group. A carbocyclic aromatic group can be unsubstituted or substituted with one or more groups including, but not limited to, -(C1- C8)alkyl, -O-[(C1-C8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO- NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, -N3, -NH2, -NHR’, -NR’ 2 and -CN; where each R’ is independently selected from -(C1-C8)alkyl and aryl. In a more preferred embodiment the carbocyclic aromatic group comprises two of the aforementioned one or more substituent groups, wherein the first of said two groups is attached to a first ring atom of the carbocyclic aromatic group, and the second of said two groups is attached either to a second ring atom of the carbocyclic aromatic group directly adjacent to said first ring atom or to a second ring atom of the carbocyclic aromatic group, the second ring atom being separated from the first ring atom by a further ring atom.

[0122] The term “heteroaryl” or “heteroaryl ring” as used herein refers to a heterocyclic aromatic group, wherein the heterocyclic aromatic group is selected from the group consisting of heterocyclic aromatic groups with a single ring and heterocyclic aromatic group with two or more fused rings, preferably two rings. Examples of heterocyclic aromatic groups with a single ring include, but are not limited to, furanyl, thienyl, pyrrolyl, pyrazolyl, oxazolyl, thiazolyl, imidazolyl, pyridinyl pyrimidinyl and examples of heterocyclic aromatic groups with two or more fused rings include, but are not limited to benzothiophenyl, benzofuranyl, indolyl and quinolinyl. A heterocyclic aromatic group can be unsubstituted or substituted with one or more groups including, but not limited to, -((C1-C)8)alkyl, -O-[( (C1-C)8)alkyl], -aryl, -CO-R’, -O-CO-R’, -CO-OR’, -CO-NH2, -CO-NHR’, -CO-NR’2, -NH-CO-R’, -SO2-R’, -SO-R’, -OH, -halogen, - N3, -NH2, -NHR’, -NR’ 2 and -CN, wherein each R’ is independently selected from -(Ci- Qjalkyl and aryl. In a more preferred embodiment the heterocyclic aromatic group comprises two of the aforementioned one or more substituent groups, wherein the first of said two groups is attached to a first ring atom of the heterocyclic aromatic group, and the second of said two groups is attached either to a second ring atom of the heterocyclic aromatic group directly adjacent to said first ring atom or to a second ring atom of the heterocyclic aromatic group, the second ring atom being separated from the first ring atom by a further ring atom.

[0123] The expression “hydrophobic group” as used herein refers to a group that comprises an aliphatic, a heterocyclic, an aryl or a heteroaryl group as defined herein wherein the ratio of heteroatoms to carbon atoms is up to 1 :3 and wherein said aliphatic, heterocyclic, aryl or heteroaryl group each and individually can be substituted by no more than one polar or charged group, preferably no polar or charged group is present. Representative hydrophobic groups include, but are not limited to, any of an ethyl, n-propyl, iso-propyl, n-butyl, isobutyl, t-butyl, phenyl, naphthyl, thienyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, thietanyl, tetrahydrothiophenyl and thianyl.

[0124] The expression “hydrophobic side chain” as used herein refers to a side chain wherein the side chain comprises a “hydrophobic group” as defined herein.

[0125] The expressions “aromatic residue” or / and “aromatic ring” as used herein refer to an aryl as defined herein.

[0126] The expression “aromatic side chain” as used herein refers to a side chain wherein the side chain comprises an “aromatic ring” as defined herein. The expression “bicyclic aromatic ring” as used herein refers to an aryl as defined herein, wherein the carbocyclic aromatic group of the aryl is selected from the group of aromatic groups with two or more fused rings, preferably two rings.

[0127] The expression “bicyclic aromatic side chain” as used herein refers to a side chain wherein the side chain comprises a “bicyclic aromatic ring” as defined herein.

[0128] The term “polar group” as used herein refers to a group of atoms that feature an uneven distribution of electrons between them due to differences in the electronegativity between the elements of a bond. Elements with higher electronegativity can withdraw bonding electrons from their neighbour, resulting in that the former presents a partial negative charge and the latter a partial positive charge. Polar groups typically contain one or more atoms selected from the group consisting of O, N, S and P. Examples of polar groups include, but are not limited to, -OH, -OR’, -CONH2, -CO-NHR’, -CO-NR’R”, -NHC(O)NH2, -NHC(NH)NH2, -COOH, -O- CO-R’, -CO-OR’, -SO3H, SO3R’, -CN, -NH2, -NHR’, -NR’R”, -SO-, -SO2-, -SO2NH2, -NO2, -P(O)(OH)2, and tetrazole, wherein each R’ and R” independently represent a group comprising one or more atoms selected from C, N, O, and S, preferably a group selected from -((C1-C)8)alkyl and aryl. Preferred examples of polar groups as used herein include -OH, -OR’, -CONH2, -CO-NHR’, -CO-NR’R”, -NHC(O)NH2, -NHC(NH)NH2, -COOH, -O-CO-R’, -CO- OR’, -SO3H, -SO3R’, -CN, -NH2, -NHR’, -NR’R”, -SO-, -SO2-, -SO2NH2, -NO2, -P(O)(OH)2, and tetrazole, wherein each of R and R’ is independently selected from -((C1-C8))alkyl and aryl. More preferred examples of polar groups as used herein include -OH, -CONH2, -COOH, -SO3H, -CN, -NH2, -SO-, -SO2-, and NO2.

[0129] The expression “polar side chain” as used herein refers to a side chain wherein the side chain comprises an “polar group” as defined herein.

[0130] The expression “charged group” as used herein refers to a functional group which can be charged at a certain pH, esp. in the range of 4 to 8. Examples of groups that can be positively charged include, but are not limited to, guanidine, ammonium and amino nitrogen. Examples of groups that can be negatively charged include, but are not limited to, COOH, phosphate, phosphonate, sulfate and sulfonate.

[0131] The expression “positvely charged side chain” as used herein refers to a side chain wherein the side chain comprises an “positively charged group” as defined herein, and the expression “negatively charged side chain” refers to a side chain wherein the side chain comprises an “negatively charged group” as defined herein. Unless specified otherwise, atoms with unspecified atomic mass numbers in any structural formula or in any passage of the instant specification including the claims are either of unspecified isotopic composition, naturally occurring mixtures of isotopes or individual isotopes. This applies in particular to carbon, oxygen, nitrogen, sulfur, phosphorus, halogens and metal atoms, including but not limited to C, O, N, S, F, P, Cl, Br, At, Sc, Cr, Mn, Co, Fe, Cu, Ga, Sr, Zr, Y, Mo, Tc, Ru, Rh, Pd, Pt, Ag, In, Sb, Sn, Te, I, Pr, Pm, Dy, Sm, Gd, Tb, Ho, Dy, Er, Yb, Tm, Lu, Sn, Re, Rd, Os, Ir, Au, Pb, Bi, Po, Fr, Ra, Ac, Th and Fm.

[0132] The term “chelator” as used herein refers to a compound or a moiety which is capable of forming a chelate, whereby a chelate is a compound or a moiety, preferably a cyclic compound wherein a metal or a moiety having an electron gap or a lone pair of electrons participates in the formation of the ring. More preferably, a chelator is a kind of compound or moiety wherein a single ligand occupies more than one coordination site at a central atom or ion.

[0133] The expression “Z group” (or “group Z”, or “group Zn” with n=l to 9) as used herein refers to an effector, such as a chelator, which optionally comprises a linker that covalently links the effector to the rest of the compound (peptide). The group and position, respectively, of the compound of the invention where a Z group may be covalently attached, is also referred to herein as Z group attachment point.

[0134] In accordance with the present invention, Z group attachment points are in particular one or more of the following ones: the N-terminal modification group Nmod which comprises an attachment point for one Z group (Zla); the side chain of Xaal which comprises an attachment point for one Z group (Zlb); the side chain of Xaa3 comprising an attachment point for one Z group (Z2); the side chain of Xaa5 comprising an attachment point for one Z group (Z3); the side chain of Xaa6 comprising an attachment point for one Z group (Z4); the side chain of Xaa8 comprising an attachment point for one Z group (Z5); the side chain of Xaa9 comprising an attachment point for one Z group (Z6); the side chain of Xaal 0 comprising an attachment point for one Z group (Z7); the side chain of Xaal 1 comprising an attachment point for one Z group (Z8); and the carbonyl group of Xaa7, Xaa8, Xaa9, XaalO, Xaal 1 which provide an attachment point for the C-terminal modification group Cterm, which can comprise or consist of one Z- group (Z9).

[0135] More preferred Z group attachment points are one or more, i.e., one, two or three, of the following ones: the side chain of Xaa5 comprising one Z-group (Z3); the side chain of Xaa6 comprising one Z group (Z4), and the side chain of Xaa8 comprising one Z-group (Z5). An even more preferred Z group attachment point is the side chain of Xaa5 comprising one Z group (Z3). As will be appreciated by a person skilled in the art, the chemical nature of the effector and of the linker, if present, define the kind of amino acid residue to be used for attaching any one of them to the compound of the invention. Typically, the effector and the linker, if present, comprise a functional group suitable for reacting with another functional group in the amino acid residue, whereby such functional group is preferably selected from the group comprising a carboxylic acid group and an amino group.

[0136] The term “amino acid residue” as used herein refers to all atoms of an amino acid, which remain in a peptide chain after the combination of said amino acid with one or more other amino acids, an N-terminal end group, an N-terminal modification group Nmod, a C-terminal modification group C-term, a C-terminal end group and / or a Z group to the a-nitrogen atom and / or the carbonyl group of said amino acid.

[0137] The term “N-terminal end group” as used herein refers to an atom or moiety that is covalently attached to the N atom of the N-terminus of the peptide chain or to the N atom of the N-terminus of an amino acid residue and is usually an N-terminal blocking group or simply an H atom. N- terminal blocking groups when attached to the peptide N-terminus cap the peptide N-terminus and prevent elongation of the peptide chain in N-terminal direction during synthesis. Representative N-terminal blocking groups include, but are not limited to, any of an acetyl group, hexyl group, n-butyloxycarbonyl group (Boc), allyloxycarbonyl (Alloc), 9- fluorenylmethoxycarbonyl (Fmoc), n-butylcarbamoyl group and n-butyl sulfonyl group. If a peptide or an amino acid has a free N-terminus, the N-terminal end group is an H atom. In contrast, the term “N-terminal modification group” (also referred to as “Nmod”) as used herein refers specifically to a moiety that is covalently attached to the a-nitrogen atom of Xaal and is different from the N-terminal end group attached to Xaal which is an H atom in compounds of formula (I).

[0138] The term “C-terminal end group” as used herein refers to a moiety that is covalently attached to the C atom of the carbonyl group of the C-terminal (last) amino acid residue of the peptide chain and is usually NH2 or OH. In contrast, the term “C-terminal modification group” (also referred to as “Cterm”) as used herein refers to a moiety that can be covalently attached to the carboxy terminus of the peptide chain of formula (I), i.e., specifically to the C atom of the carbonyl group of Xaa7, Xaa8, Xaa9, XaalO, or Xaal 1. If Cterm is a Z group (i.e. a group Z9), Cterm can comprise a linker to which a chelator is covalently attached, e.g. Cterm can be the Z group -Ttds-Lys(DOTA)-NH2 attached to the carbonyl group of Xaal 1, wherein the C-terminal end group is -NH2 which is attached to the carbonyl group of the very C-terminal Lys(DOTA) residue.

[0139] The terms “L-configuration” and “D-configuration” as used herein refer to the stereo configuration of the a-carbon atom of an a-amino acid or a residue of an a-amino acid. The same nomenclature can be used accordingly for an a-hydroxy acid or a residue of an a-hydroxy acid.

[0140] The term “side chain” as used herein refers to all atoms of an amino acid residue that are not comprised in the “main chain” (or “backbone”) portion of said amino acid residue. The “main chain” refers to the structure that is formed by the consecutive connection of at least a first amino acid and a second amino acid, whereby the a-nitrogen atom of an a-amino acid being the second amino acid, the P-nitrogen atom of a P-amino acid being the second amino acid, the y-nitrogen of a y-amino acid being the second amino acid, the 5-nitrogen atom of a 5-amino acid being the second amino acid, the s-nitrogen of an s-amino acid being the second amino acid or the co-nitrogen of an co-amino acid being the second amino acid is connected or covalently linked to the C-l carbonyl group of a preceding amino acid being the first amino acid.

[0141] The term “linking”, “linked” or “link” as used herein refers to or describes a scenario, where two or more moieties are connected either directly or indirectly with an interspersed group. Typically, and as preferably used herein, such moieties are an effector, such as a chelator, and an amino acid residue. In a more preferred embodiment, such interspersed group is a linker.

[0142] The term “interspersed” as used herein refers to or describes a scenario in which a group, preferably a linker, is inserted between a first moiety and a second moiety. Such moieties, for example, can be an amino acid residue and an effector such as a chelator. The inserted group is covalently attached to both of the moieties.

[0143] Compounds of the invention typically contain amino acid sequences as provided herein. Conventional amino acids, also referred to as natural amino acids are identified according to their standard three-letter codes, as set forth in Table 4. Table 4: Conventional amino acids and their abbreviations

[0144] 3-letter Amino acid 3-letter Amino acid codes codes

[0145] Ala Alanine Met Methionine

[0146] Cys Cysteine Asn Asparagine

[0147] Asp Aspartic acid Pro Proline

[0148] Glu Glutamic acid Gin Glutamine

[0149] Phe Phenylalanine Arg Arginine

[0150] Gly Glycine Ser Serine

[0151] His Histidine Thr Threonine

[0152] He Isoleucine Vai Valine

[0153] Lys Lysine Trp Tryptophan

[0154] Leu Leucine Tyr Tyrosine

[0155] A “non-conventional amino acid”, also referred to as “non-natural amino acid”, is any kind of non-oligomeric compound, which comprises an amino group and a carboxylic group and is not a conventional amino acid.

[0156] Examples of conventional amino acids, non-conventional amino acids and other building blocks as used for the description of compounds of the invention are identified according to their abbreviation or name found in Table 5. The structures of some building blocks are depicted as resiudes of the corresponding amino acids (amino acid residues) or these building blocks are shown as residue, which is completely attached to another structure like a peptide or amino acid residue. Structures of amino acids are shown as building blocks and as residues of the corresponding amino acids how they are present after implementation in the peptide sequence. Some larger chemical moi eties consisting of more than one moiety are also shown for the reason of clarity (e.g. Apc(DOTA)). Table 5: Abbreviation, name and structure of non-natural amino-acid and other building blocks and chemical moieties

[0157]

[0158]

[0159] The amino acid sequences of the peptides disclosed herein are depicted in typical peptide sequence format, as will be understood by a person skilled in the art. For example, the three- letter code for a residue of a conventional amino acid, the code for a residue of a non- conventional amino acid or the abbreviation for a residue of a building block other than a conventional or non-conventional amino acid indicates the presence of the residue, of the amino acid residue or the presence of the residue of the building block at a specified position within the peptide sequence. The code for a residue of an amino acid and the abbreviation for a residue of a building block, respectively, is connected to the code for a subsequent residue of an amino acid and / or to the code for a preceding residue of an amino acid and, respectively, is connected to the abbreviation for a subsequent residue of a building block and / or to the abbreviation for a preceding residue of a building block, respectively, in the peptide sequence by a hyphen which typically represents an amide linkage. For example, if the hyphen is located before the code for a residue of an amino acid, this usually symbolizes that the amino group (as indicated in the corresponding entry in Table 5) of the residue of the amino acid is covalently attached to a carbonyl group of a preceding residue of an amino acid, and if the hyphen is located after the code for a residue of an amino acid, this usually symbolizes that the carbonyl group (as indicated in the corresponding entry in Table 5) of the residue of the amino acid is covalently attached to an amino group of a subsequent residue of an amino acid.

[0160] Depending on the spacing between the amino- and the carboxy group in amino acids they are classified into a-, P-, y-, 5-, a-, (and so forth) -amino acids, which means that these groups are typically are spaded apart by 1, 2, 3, 4, and 5 heavy-atoms (typically carbon), respectively.

[0161] For amino acids, in their abbreviations the first letter indicates the stereochemistry of the C-a-atom if applicable. For example, a capital first letter indicates that the L-form of the amino acid is present in the peptide sequence, while a lower case first letter indicating that the D-form of the correspondent amino acid is present in the peptide sequence. If the abbreviation starts with a number, the first letter in the abbreviation will be characteristic for the stereochemistry, if applicable. However, for enhanced clarity it is at any abbreviation an option to further clearly specify the stereochemistry of an amino acid abreviation by adding for instance the prefix “D-“. As example “lys”, “D-Lys” or “D-lys” describe all a D-configured Lys.

[0162] For someone skilled in the art it is evident that many amino acids can be N-methylated at their amino group. These N-methyl amino acid feature can occur in combination with some other attributes like L-a- or D-a-N-methyl amino acids which are N-methylated L-a- or D-a-amino acids.

[0163] The term “a,a-dialkylamino acid” as used herein refers to amino acid which comprise independently two alkyl groups at the a-carbon atom which maybe in some cases form a ringstructure with each other. Representative a,a-dialkylamino acids include, but are not limited to, any of Aib, Deg, Egz, Ape, and Thp.

[0164] The term “aromatic amino acid” as used herein refers to an amino acid, which comprises an aromatic structure and this includes a heteroaromatic structure whereas the term “non-aromatic amino acid” refers to an amino acid which is devoid of any aromatic structure. Examples of aromatic amino acids include, but are not limited to, phenylalanine, tyrosine, 2-chloro phenylalanine, 4-guanidino phenylalanine, 1 -naphthylalanine, 4-carboxymethyl phenylalanine, 3 -fluoro phenylalanine, phenyl glycine, homophenylalanine and Levodopa.

[0165] The term “heteroaromatic amino acid” as used herein refers to an amino acid, which comprises any kind of heteroaromatic structure. Examples of heteroaromatic amino acids include, but are not limited to, histidine, tryptophan, 2-thienyl alanine, thiazolyl alanine, 3- pyridyl alanine, 7-chloro tryptophan, benzothienyl alanine, furanyl alanine, 4-pyridyl alanine and 2-quinolyl alanine.

[0166] An “aliphatic amino acid” is a non-aromatic amino acid, which comprises an aliphatic group. Examples of aliphatic amino acids include, but are not limited to, noreleucine, leucine, isoleucine, valine, cyclohexyl alanine, a-aminobutyric acid, tert-leucine, neopentyl glycine and 2-cyclopropyl glycine.

[0167] A “polar amino acid” is any kind of amino acid, which comprises apart from the amino and carboxy group one or more polar groups as defined herein. Examples of polar amino acids include, but are not limited to, serine, threonine, asparagine, glutamine, citrulline, aspartic acid, glutamic acid, lysine, arginine and homoglutamine.

[0168] A “charged amino acid” is any kind of amino acid which comprises, apart from the amino and carboxy group, one or more charged groups as defined herein. Such charged groups can be positively or negatively charged and a charged amino acid can as well be zwitterionic, i.e. comprising both positively and negatively charged groups at the same time. Examples of positively charged amino acids include, but are not limited to, lysine, arginine, ornithine, homoarginine, KMe3, Lys(Me), Dab, Dap and KMe2. Examples of negatively charged amino acids include, but are not limited to, aspartic acid, glutamic acid, cysteic acid, Pcof, Fso and y- carb oxy glutamic acid. Examples of zwitterionic amino acids include, but are not limited to, Kzw and s-(y-glutamyl)-lysine.

[0169] If an amino acid contains more than one amino and / or carboxy group all orientations of this amino acid are in principle possible for formation of a covalent bond, but in a-amino acid the utilization of the a-amino and the a-carboxy group is preferred for the attachment to the neighbouring moieties and if other orientations are preferred they are explicitly specified.

[0170] Those skilled in the art will recognize if a stereocenter exists in the compounds disclosed herein irrespective thereof whether such stereocenter is part of an amino acid moiety or any other part or moiety of the compound of the invention. When a compound is desired as a single enantiomer or diastereomer, it may be obtained by stereospecific synthesis or by resolution of the final product or any convenient intermediate. Resolution of the final product, an intermediate, or a starting material may be affected by any suitable method known in the art. See, for example, "Stereochemistry of Organic Compounds" by E. L. Eliel, S. H. Wilen, and L. N. Mander (Wiley -Interscience, 1994).

[0171] The term “aromatic L-a-amino acid” as used herein refers any kind of L-a-amino acid, which comprises an aryl group. The term “heteroaromatic L-a-amino acid” as used herein any kind of L-a-amino acid which comprises a heteroaryl group.

[0172] The term “L-a-hydroxy acid” as used herein refers to any kind of non-oligomeric compound, which comprises a hydroxy group and a carboxylic group that are linked by one stereogenic (a) carbon atom in L-configuration. In some aspects, the L-a-hydroxy acid represents the derivative of an L-a-amino acid in which the a-amino group has been replaced by a hydroxy group. Examples of L-a-hydroxy acids include, but are not limited to, L-lactic acid, L-malic acid, and (5)-2 -hydroxyhexanoic acid.

[0173] The expression “residue of an L-a-hydroxy acid” as used herein characterizes a substance that remains when an L-a-hydroxy acid is combined with one or more amino acids to form an amino acid derivative or a peptide derivative or analog. For example, the C-atom of the carbonyl group of an L-a-hydroxy acid Xaal such as Lac can be covalently attached to the a-nitrogen of an amino acid Xaa2 to form an amino acid derivative Xaal-Xaa2. Similarly, the C-atom of the carbonyl group of an L-a-hydroxy acid Xaal can be covalently attached to the amino terminus of a peptide Xaa2-[...]-Xaa(n-l) (wherein n-1 represents the number of amino acids forming the peptide) to form a peptide Xaal-Xaa2-[...]-Xaa(n-l). Since the N-terminal end group (which usually is an H atom) is attached to the O atom of the L-a-hydroxy acid, the residue of an L-a-hydroxy acid only contains the O atom of the OH group.

[0174] The term “P-amino alcohol” as used herein refers to any kind of non-oligomeric compound, which comprises a hydroxy group and an amino group on adjacent carbon atoms. Examples of P-amino alcohols include, but are not limited to, ethanolamine, alaninol, phenylalaninol, tyrosinol, 2-thienylalaninol, leucinol, valinol, tert-leucinol and norleucinol. Furthermore, the expression “residue of a p-amino alcohol” as used herein characterizes a substance that remains when a P-amino alcohol is combined with, e.g., an amino acid to form a derivative. For example, the N-atom of the amino group of a P-amino alcohol can be covalently attached to the carboxyl group of an amino acid to form a derivative.

[0175] Unless indicated to the contrary, the amino acid sequences are presented herein in N- to C -terminus direction (from left to right).

[0176] Linear Peptides

[0177] A general linear peptide is typically written from N-to C-terminal direction (from left to right) as shown below:

[0178] H-Xaa 1 -Xaa2 -Xaa3 -Xaa4- > Xaan -Cterm ; Therein

[0179] A) “Xaax” is the abbreviation, descriptor or symbol for amino acids or building blocks at specific sequence position x as shown in Table 5,

[0180] B) “H” is the hydrogen atom that is covalently attached to the a-nitrogen of Xaal (when Xaal represents (a) a residue of an L-a-amino acid comprising a side chain) or to the oxygen atom comprised in the hydroxy group of Xaal (when Xaal represents (b) a residue of an L-a-hydroxy acid comprising a side chain), and

[0181] C) “Cterm” is the C-terminal group, which is typically -NH2, -OH, a group Z9or -NHRctermand linked to the C-terminal amino acid code (Xaan) via a hyphen.

[0182] In the context of the statement 2, it is understood that “H” is an atom that is naturally present in Xaal, i.e., “H” may be considered as forming part of the amino group (when Xaal represents (a) a residue of an L-a-amino acid comprising a side chain) or hydroxyl group (when Xaal represents (b) a residue of an L-a-hydroxy acid comprising a side chain) of Xaal.

[0183] Branched peptides with side chains modified by specific building blocks or peptides

[0184] Linear, branched peptides are written from the N-to C-terminal direction as shown below:

[0185] H-Xaal -Xaa2-Xaa3(A7-Xa / i / -Aa / i2- > Xabri)- > Xaan-Cterm

[0186] Therein, the statements 1. - 3. of the description of linear peptides for the specification of “Xaax”, “H” and “C-term” in the main chain of the branched peptide apply. An individual branch is specified by an expression in parentheses, wherein the positioning of the branch within the peptide sequence / structure is indicated by the positioning of the parenthesized expression right next to an ’’Xaax” abbreviation (e.g., “Xaa3”). Branches typically either occur at lysine (Lys) residues or 4-aminopiperidine-4-carboxylic acid (Ape) (or similar), which means that the branch is attached to side chain s-amino function of the lysine or to the nitrogen atom within the piperidine ring of 4-aminopiperidine-4-carboxylic acid via an amide bond.

[0187] The content of the parentheses describes the sequence / structure of the peptide branch “NT-Xab 1-Xab2- > Xabir . Herein

[0188] I. “Xabx” is the abbreviation, descriptor or symbol for amino acids or building blocks at specific sequence position x of the branch as shown in Table 5, whereby the linear connection of individual Xabx is indicated by a hyphen,

[0189] II. “NT” is an N-terminal group, e.g. an abbreviation for a specific terminating carboxylic acid like ’Ac’ for acetyl or other chemical group or structural formula of chemical groups, more specifically “NT” is a Z group, linked to the N-terminal amino acid code (Xabi) via a hyphen and the last building block of the branch “Xabri\ which connects the branch with the main chain by forming an amide bond with its own carboxyl function with the side chain amino function of this lysine or 4-aminopiperidine-4-carboxylic acid (or similar residue).

[0190] The term “effector” as used herein characterizes a chemical moiety and / or element (e.g., a naturally occurring or synthetic substance) attached to the compound for the purpose of diagnostic and / or therapeutic intervention with P-cadherin-related diseases and / or cancer cells. In some embodiments, the term “effector” is to be understood as a moiety (e.g., chromophore, fluorophore, radiolabeled moiety, chelator comprising a chelated diagnostically active nuclide) that enables and / or facilitates the detection and / or visualization of a complementary moiety to which it is attached. For instance, the moiety can be detected and / or visualized by molecular imaging techniques known in the art such as single photon emission computed tomography (SPECT), positron emission tomography (PET), etc. In some embodiments, the term “effector” is to be understood as a pharmacologically active substance (e.g., chelator comprising a chelated therapeutically active nuclide, cytotoxic drug, immune cell engaging effector) which can inhibit or prevent the function of cells and / or kill cells. In some embodiments, the term “effector” is to be understood as being synonymous with other terms commonly used in the art such as “cytotoxic agent”, “toxin” or “drug” used in the field of cancer therapy. In some embodiments, it is to be understood that the “effector” does not itself exert the therapeutically exploited cytotoxic effect, but that it rather attracts and stimulates effector cells of the immune system (e.g. T cells, NK cells, phagocytotic immune cells) that directly or indirectly trigger immune cell mediated killing of the cancer cells.

[0191] The term “chromophore” as used herein refers to an organic or metal-organic compound which is able to absorb electromagnetic radiation in the range of from 350 nm to 1100 nm, or a subrange thereof, e.g. 350-500 nm or 500-850 nm, or 350-850 nm.

[0192] The term “phosphorophore” as used herein refers to a compound which, when excited by exposure to a particular wavelength of light, emits light at a different wavelength and lower intensity over a prolonged period of time, e.g. up to several hours.

[0193] The term “fluorophore” as used herein refers to a compound which, when excited by exposure to a particular wavelength of light, emits light at a different (higher) wavelength. Fluorophores are usually described in terms of their emission profile or “color”. For example, green fluorophores such as Cy3 or FITC generally emit at wavelengths in the range of 515-540 nm, while red fluorophores such as Cy5 or tetramethylrhodamine generally emit at wavelengths in the range of 590-690 nm. The term “fluorophore” is to be understood as encompassing, in particular, organic fluorescent dyes such as fluorescein, rhodamine, AMCA, Alexa Fluor dyes (e.g., Alexa Fluor 647), and biological fluorophores.

[0194] The term “immune cell engaging effector” as used herein refers to a compound which is capable of binding one or more cell surface molecules of effector cells of the immune system. When covalently linked to a compound that binds to cell surface molecules of cancer cells, these compounds act as immune cell engagers, i.e. they activate the effector cells of the immune system and directly and / or indirectly trigger immune cell mediated killing of the cancer cells. In principle, all effector cells of the immune system can be exploited for this approach, including but not limited to T cells (both CD8 and CD4 cells), natural killer cells (NK cells), phagocytotic myeloid cells (monocytes, macrophages, dendritic cells and cytokine-activated neutrophils) and B cells. Preferably, immune effector cells regardless of their antigen specificity are targeted by immune cell engaging effectors, with T cells, NK cells, macrophages and monocytes being the preferably engaged effector cells. Typical cell surface molecules that are targeted by immune cell engaging effectors include, but are not limited to, CD3, CD27, CD28, CD40, CD134, CD137, CD278, CD16, NKG2D, NKp30, and CD64. Typical immune cell engaging effectors are antibodies and binding fragments thereof, such as Fab, Fv or single domain fragments that target e.g. CD3, CD28, CD137, CD16, NKG2D, and CD64 (Fuca et al. ESMO Open 2021, 6, 100046), but also scaffolds using designed ankyrin repeat proteins (= DARPins) and even small peptides have been employed for this purpose (e.g. targeting CD137, Claus et al. Mabs 2023, 15, 2167189).

[0195] The term “chelator” (or “chelating agent”) as used herein refers to a molecule containing two or more electron donor atoms that can form coordinate bonds to a single central metal ion, e.g. to a radionuclide. Typically, chelating agents coordinate metal ions through oxygen, nitrogen, or sulfur donor atoms, or combinations thereof. After the first coordinate bond is formed, each successive donor atom that binds creates a ring containing the metal ion. A chelating agent may be bidentate, tridentate, tetradentate, etc., depending on whether it contains 2, 3, 4, or more donor atoms capable of binding to the metal ion. However, the chelating mechanism is not fully understood and depends on the chelating agent and / or radionuclide. For example, it is believed that DOTA can coordinate a radionuclide via carboxylate and amino groups (donor groups) thus forming complexes having high stability (Dai et al. Nature Com. 2018, 9, 857). The term “chelating agent” is to be understood as including the chelating agent as well as salts thereof. Chelating agents having carboxylic acid groups, e.g., DOTA, TRITA, HET A, HEXA, EDTA, DTPA etc., may, for example, be derivatized to convert one or more carboxylic acid groups to amide groups for attachment to the compound, i.e. to the reactive moiety or the linker, alternatively, for example, said compounds may be derivatized to enable attachment to the compound via one of the CH2 groups in the chelate ring.

[0196] The term "radionuclide" as used herein refers to an atom with an unstable nucleus, which is a nucleus characterized by excess energy that is released by different types of radioactive decay. Radionuclides occur naturally or can be artificially produced. In one embodiment, references to “nuclide(s)” made in the present specification and claims are preferably to be understood as references to “radionuclide(s)”.

[0197] The expression “moiety derived from a drug” as used herein refers to a moiety corresponding to a native drug, which differs from the native drug only by the structural modification required for bonding to adjacent moi eties, e.g. for bonding to the reactive moiety, linker or branching group comprised in the compound of the present invention. This may include covalent bonds formed by existing functional groups (available in the native drug) or covalent bonds and adjacent functional groups newly introduced for this purpose. By consequence, the drug can be used in its non-modified form (except for the replacement of e.g. a hydrogen atom by a covalent bond), or it can be chemically modified in order to incorporate one functional group allowing covalent attachment to the reactive moiety, linker, or branching group comprised in the compound of the present invention. The expression or term “moiety derived from a drug” as used herein is meant to encompass both meanings.

[0198] In an analogous manner, the term “derivative” is used to characterize moieties bonded to adjacent moieties, which moieties differ from the molecules from which they are derived only by the structural elements responsible for bonding to adjacent moieties. This may include covalent bonds formed by existing functional groups or covalent bonds and adjacent functional groups newly introduced for this purpose.

[0199] The term “linker” as used herein refers to an element, moiety, or structure which connects two parts of a molecule.

[0200] A "pharmaceutically acceptable salt" of the compound of the present invention is preferably an acid salt or a base salt that is generally considered in the art to be suitable for use in contact with the tissues of human beings or animals without excessive toxicity or carcinogenicity, and preferably without irritation, allergic response, or other problem or complication. Such salts include mineral and organic acid salts of basic residues such as amines, as well as alkali or organic salts of acidic residues such as carboxylic acids. Compounds of the invention are capable of forming internal salts which are also pharmaceutically acceptable salts.

[0201] Suitable pharmaceutically acceptable salts include, but are not limited to, salts of acids such as hydrochloric, phosphoric, hydrobromic, malic, glycolic, fumaric, sulfuric, sulfamic, sulfanilic, formic, toluenesulfonic, methanesulfonic, benzene sulfonic, ethane disulfonic, 2- hydroxyethylsulfonic, nitric, benzoic, 2-acetoxybenzoic, citric, tartaric, lactic, stearic, salicylic, glutamic, ascorbic, pamoic, succinic, fumaric, maleic, propionic, hydroxymaleic, hydroiodic, phenylacetic, alkanoic such as acetic, H00C-(CH2)n-C00H where n is any integer from 0 to 4, z.e., 0, 1, 2, 3, or 4, and the like. Similarly, pharmaceutically acceptable cations include, but are not limited to sodium, potassium, calcium, aluminum, lithium and ammonium. Those of ordinary skill in the art will recognize further pharmaceutically acceptable salts for the compounds provided herein. In general, a pharmaceutically acceptable acid or base salt can be synthesized from a parent compound that contains a basic or acidic moiety by any conventional chemical method. Briefly, such salts can be prepared by reacting the free acid or base forms of these compounds with a stoichiometric amount of the appropriate base or acid in water or in an organic solvent, or in a mixture of the two. Generally, the use of non-aqueous media, such as ether, ethyl acetate, ethanol, isopropanol or acetonitrile, is preferred.

[0202] A "pharmaceutically acceptable solvate" of the compound of the invention is preferably a solvate of the compound of the invention formed by association of one or more solvent molecules to one or more molecules of a compound of the invention. Preferably, the solvent is one which is generally considered in the art to be suitable for use in contact with the tissues of human beings or animals without excessive toxicity or carcinogenicity, and preferably without irritation, allergic response, or other problem or complication. Such solvent includes an organic solvent such as alcohols, ethers, esters and amines.

[0203] A “hydrate” of the compound of the invention is formed by association of one or more water molecules to one or more molecules of a compound of the invention. Such hydrate includes but is not limited to a hemihydrate, monohydrate, dihydrate, trihydrate and tetrahydrate. Independent of the hydrate composition all hydrates are generally considered as pharmaceutically acceptable.

[0204] Hereinafter, in the present description of the invention and the claims, the use of the terms “containing” and “comprising” is to be understood such that additional unmentioned elements may be present in addition to the mentioned elements. However, these terms should also be understood as disclosing, as a more restricted embodiment, the term “consisting of’ as well, such that no additional unmentioned elements may be present, as long as this is technically meaningful.

[0205] Unless specified otherwise or the context dictates otherwise, references to groups being “substituted” or “optionally substituted” are to be understood as references to the presence (or optional presence, as the case may be) of at least one substituent selected from F, Cl, Br, I, CN, NO2, NH2, NH-(Ci-C6)alkyl, N[(Ci-C6)alkyl]2, -X-(Ci-C6)alkyl, -X-(C2-C6)alkenyl, -X-(C2- Ce)alkynyl, -X-(Ce-Ci4)aryl, -X-(5-14-membered heteroalkyl with 1-3 heteroatoms selected from N, O, S), wherein X represents a single bond, -(CH2)-, -O-, -S-, -S(O)-, -S(O)2-, -NH-, -CO-, or any combination thereof including, for instance, -C(O)-NH-, -NH-C(O)-. The number of substituents is not particularly limited and may range from 1 to the maximum number of valences that can be saturated with substituents. It is typically 1, 2 or 3 and usually 1 or 2, most typically 1.

[0206] Unless specified otherwise, all valencies of the individual atoms of the compounds or moieties described herein are saturated. In particular, they are saturated by the indicated binding partners. If no binding partner or a too small number of binding partners is indicated, the remaining valencies of the respective atom are saturated by a corresponding number of hydrogen atoms.

[0207] Unless specified otherwise, chiral compounds and moieties may be present in the form of a pure stereoisomer or in the form of a mixture of stereoisomers, including the 50:50 racemate. In the context of the present invention, references to specific stereoisomers are to be understood as references to compounds or moieties, wherein the designated stereoisomer is present in at least 90% enantiomeric excess (ee), more preferably at least 95 %ee and most preferably 100 %ee, wherein %ee is defined as (|R-S|) / (R+S)*100% with R and S representing the amount of moles of the respective enantiomers.

[0208] Molecules in which free rotation around one or more bonds is restricted may exist as distinct stable conformational isomers called rotamers. Rotamers often form around amide bonds due to the double bond character of the N-C bond. Unless specified otherwise, compounds that can form rotamers, may be present as individual (stable) rotamers or as a mixture of rotamers.

[0209] The term "specifically binds" as used herein refers to the ability of the compound of the invention to bind to its target (i.e., P-cadherin) with greater affinity than it binds to a non-target. In certain embodiments, specific binding refers to binding for P-cadherin with an affinity that is at least 10, 50, 100, 250, 500, or 1000 times greater than the affinity for a non-target. The term "binding affinity" refers to the strength of interaction between the compound of the invention and its target (i.e., P-cadherin) as a function of its association and dissociation constants. Higher affinities typically mean that the compound has a fast on rate (association) and a slow off rate (dissociation). Binding affinities can change under various physiological conditions due to changes that occur to the compound or target under those conditions. Binding affinities of the compound may also change when effectors and / or linkers are attached.

[0210] The term "inhibit" or "inhibition of" as used herein means to reduce by a measurable amount, or to prevent entirely.

[0211] The term "therapeutically effective amount" refers to an amount of compound effective to treat a disease or disorder in a mammal. In the case of cancer, the therapeutically effective amount of the compound may reduce the number of cancer cells; reduce the tumor size; inhibit (i.e., slow to some extent and preferably stop) cancer cell infiltration into peripheral organs; inhibit (i.e., slow to some extent and preferably stop) tumor metastasis; inhibit, to some extent, tumor growth; and / or relieve to some extent one or more of the symptoms associated with the cancer. When the compound comprises a drug, and to the extent the drug may inhibit growth and / or kill existing cancer cells, it may be cytostatic and / or cytotoxic. For cancer therapy, efficacy can, for example, be measured by assessing the time to disease progression (TTP) and / or determining the response rate (RR).

[0212] The term "cytotoxic drug" (or “cytotoxic agent”) as used herein refers to a substance that has cytotoxic activity and causes destruction of cells. The term is intended to include radioactive isotopes, chemotherapeutic agents, and toxins such as small molecule toxins or enzymatically active toxins of bacterial, fungal, plant or animal origin, including synthetic analogs and derivatives thereof.

[0213] The term “diagnostically active compound” as used herein refers to a compound which is suitable for or useful in the diagnosis of a disease.

[0214] The term “diagnostic agent” or “diagnostically active agent” as used herein efers to a compound which is suitable for or useful in the diagnosis of a disease.

[0215] The term “therapeutically active compound” as used herein refers to a compound which is suitable for or useful in the treatment of a disease.

[0216] The term “therapeutic agent” or “therapeutically active agent” refers to a compound which is suitable for or useful in the treatment of a disease. The term “theragnostically active compound” as used herein refers to a compound which is suitable for or useful in both the diagnosis and therapy of a disease.

[0217] The terms “theragnostic agent” or “theragnostically active agent” as used herein refers to a compound which is suitable for or useful in both the diagnosis and therapy of a disease.

[0218] The term “thera(g)nostics” as used herein refers to a method for the combined diagnosis and therapy of a disease; preferably, the combined diagnostically and therapeutically active compounds used in theragnostics are radiolabeled.

[0219] The expression “treatment of a disease” as used refers to treatment and / or prevention of a disease, e.g., cancer.

[0220] The expression “disease involving P-cad” as used herein refers to a disease where cells including, but not limited to, tumor cells expressing, preferably in an upregulated manner, P- cad and tissue either expressing P-cad, preferably in an upregulated manner respectively, are either a or the cause for the disease and / or the symptoms of the disease, or are part of the pathology underlying the disease. A preferred P-cad-expressing cell is a tumor cell. In an embodiment of the disease, preferably when used in connection with the treatment, treating and / or therapy of the disease, affecting the cells, the tissue and pathology, respectively, results in cure, treatment or amelioration of the disease and / or the symptoms of the disease. In an embodiment of the disease, preferably when used in connection with the diagnosis and / or diagnosing of the disease, labeling of the P-cad-expressing cells and / or of the P-cad-expressing tissue allows discriminating or distinguishing said cells and / or said tissue from healthy or P- cad-non-expressing cells and / or healthy or P-cad-non-expressing tissue. More preferably such discrimination or distinction forms the basis for said diagnosis and diagnosing, respectively. In an embodiment thereof, “labeling” means the interaction of a detectable label either directly or indirectly with the P-cad-expressing cells and / or with the P-cad-expressing tissue or tissue containing such P-cad-expressing cells; more preferably such interaction involves or is based on the interaction of the label or a compound bearing such label with P-cad.

[0221] The term “target cell” as used herein refers to a cell which is expressing P-cad and is a or the cause for a disease and / or the symptoms of a disease, or is part of the pathology underlying a disease. P-cad expression can be determined by methods known in the art such as Western blotting.

[0222] The term “non-target cell” as used herein refers to a cell which is either not expressing P-cad and / or is not a or the cause for a disease and / or the symptoms of a disease, or is part of the pathology underlying a disease. The term “neoplasm” as used herein refers an abnormal new growth of cells. Typically, the cells in a neoplasm grow more rapidly than normal cells and will continue to grow if not treated. A neoplasm may be benign or malignant.

[0223] The term “tumor” as used herein refers to a mass lesion that may be benign or malignant.

[0224] The terms "cancer" and "cancerous" as used herein refer to or describe the physiological condition or disorder in mammals that is typically characterized by unregulated cell growth. A "tumor" comprises one or more cancerous cells. A “cancer” may be a malignant neoplasm.

[0225] The term "patient" as used herein refers to a subject to which the compound of the invention is administered. Examples of a "patient" include, but are not limited to, a human, rat, mouse, guinea pig, non-human primate, pig, goat, cow, horse, dog, cat, bird and fowl. Typically, a patient is a rat, mouse, dog, non-human primate or human. In some aspects, the patient is a human in need of an effective amount of the compound.

[0226] The terms "treat" or "treatment" unless otherwise indicated by context, refer to therapeutic treatment and prophylactic measures to prevent relapse, wherein the object is to inhibit or slow down (lessen) an undesired physiological change or disorder, such as, for example, the development or spread of cancer. For purposes of this invention, beneficial or desired clinical results include, but are not limited to, alleviation of symptoms, diminishment of extent of disease, stabilized (i.e., not worsening) state of disease, delay or slowing of disease progression, amelioration or palliation of the disease state, and remission (whether partial or total), whether detectable or undetectable. "Treatment" can also mean prolonging survival as compared to expected survival if not receiving treatment. Those in need of treatment include those already with the condition or disorder as well as those prone to have the condition or disorder.

[0227] In the context of cancer, the term "treating" includes any or all of: inhibiting growth of tumor cells, cancer cells, or of a tumor; inhibiting replication of tumor cells or cancer cells, lessening of overall tumor burden or decreasing the number of cancerous cells, and ameliorating one or more symptoms associated with the disease.

[0228] Unless the context dictates otherwise, and / or alternative meanings are explicitly provided herein, all terms are intended to have meanings generally accepted in the art, as reflected by IUPAC Gold Book (status of 1st Nov. 2023), or the Dictionary of Chemistry, Oxford, 8th Ed. 2. COMPOUND OF THE INVENTION

[0229] The present invention relates to a chemical compound having a structure represented by the general formula (I). In particular, the present inventors have surprisingly found that the compound of the invention shows a high binding affinity for P-cadherin while not binding E- cadherin, the closest protein relative which is commonly expressed in adult epithelial tissues. That is, the compound of the invention contains a peptide motif (also referred to as “targeting unit”) that leads to strong interactions with the P-cadherin protein - i.e., polar, hydrophobic interactions - resulting in high binding affinity and selectivity for P-cadherin. In addition, the present inventors have surprisingly found that the compound of the invention shows other properties that makes it particularly suitable for use in the diagnosis and / or therapy of diseases in which P-cadherin is involved. Such other properties include a high stability in plasma deriving from high stability against both soluble plasma proteases and membrane-bound peptidases on the surface of blood cells such as neutral endopeptidase (NEP). Moreover, hydrophobic and hydrophilic moieties are well balanced, providing a favorable solubility profile. Having a low molecular weight, the compound of the invention - without being bound by any theory - is believed to have a short plasma half life and to efficiently penetrate into (tumor) tissues, thus, having a favorable pharmacokinetic profile for a diagnostic and therapeutic application: while being able to efficiently transport a radioactive or cytoxic payload into the tumor and to provide a long rentention in the tumor tissue, excessive compound will be quickly eliminated via the renal pathway and not remain in the circulation and / or expose healthy tissues to the toxic payload. Surprisingly, the inventors found that the compound of the invention, when equipped with a chelator and a radionuclide, shows little to no accumulation of radioactivity in any healthy tissues. This is even true for the kidneys that are involved in the excretion pathway and particularly prone to accumulate peptidic compounds. This limits, prevents and / or supresses renal toxicity and makes the compound of the invention particularly suitable for use in therapeutic applications.

[0230] Without being bound by any theory, it is considered that the peptide structure formed by the residues Xaal to Xaa7, as defined herein, results in a high affinity for P-cadherin. In particular, the present inventors consider that the following core structures or motifs lead to a compound having a high affinity for P-cadherin:

[0231] 1) the a-amino (= the peptide N-terminus) or the a-hydroxy group of Xaal (defined as (a) a residue of an L-a-amino acid comprising a side chain or (b) a residue of an L-a-hydroxy acid comprising a side chain) promotes an important polar interaction with the protein (without being bound by any theory, it is believed that this interaction mimics the salt bridge formed between the side chain of E89 (i.e. E196 in SEQ ID NO: 1) and the protein N-terminus as described by Vendome, et al., PNAS, 2014, 777: E4175 in the context of the self-dimerization mechanism), particularly when forming a salt bridge between the negatively charged side chain of E89 and the positively charged a-amino group of Xaal; and / or

[0232] 2) without being bound by any theory, the side chain of Xaa2 (defined as a residue of an L-a-amino acid comprising a side chain, which comprises an optionally substituted indole or benzothiophene group) is believed to occupy the Trp-binding pocket of P-cadherin (mimicking W2 in the natural sequence as described by Kudo, etaL, Structure, 2016, 24\ 1523 in the context of the self-dimerization mechanism); and / or

[0233] 3) the side chain of Xaa4 (defined as a residue of an L-a-amino acid comprising a hydrophobic side chain) is believed to promote a hydrophobic contact with the protein; and / or

[0234] 4) the side chain of Xaa7 (defined as a residue of an L-a-amino acid comprising a side chain, which comprises an aryl or heteroaryl group) is believed to promote another hydrophobic contact with the protein.

[0235] The present inventors have also found that preferred compounds of the invention comprise certain core structures or motifs as will be described further below. When the compounds comprise these core structure or motifs, the technical effects in terms of binding affinity for P- cadherin are even more pronounced.

[0236] The present invention relates to a compound comprising a peptide, or to a peptide represented by the following formula (I):

[0237] H - Xaal - Xaa2 - Xaa3 - Xaa4 - Xaa5 - Xaa6 - Xaa7 - Cext (I) or a pharmaceutically acceptable salt thereof, wherein,

[0238] Xaal is (a) a residue of an a-amino acid comprising a side chain and one N- terminal modification group Nmod covalently attached to the a-nitrogen atom of the amino acid, preferably a residue of an L-a-amino acid comprising a side chain and one N-terminal modification group Nmod covalently attached to the a-nitrogen atom of the amino acid, wherein Nmod is a group containing one or more selected from hydrogen, carbon, nitrogen oxygen and sulfur and optionally comprises a group Zla, preferably Nmod is selected from the group consisting of -H, -CH2COOH, -CH2CONH2, -CH2C(O)Zla, -(CH2)cNH(Zla), a (Ci-C6) alkyl group and a group of formula -(CH2)cRle, wherein Rleis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein Rleoptionally comprises a group Zla, preferably Rleis selected from the group consisting of -H, -NH(Zla), a polar and a charged group, more preferably Rleis selected from the group consisting of -H, -OH, -CONH2, -COOH, -NH-CONH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Zla) and -NH-C(NH)NH2, wherein c = 2, 3, 4 or 5, wherein optionally one or two hydrogens of said two, three, four or five -CH2- groups of the - (CH2)cRlegroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)cRlegroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably c = 2 or 3, more preferably Nmod is selected from the group consisting of -H, a (C1-C3)alkyl group and -CH2COOH, still more preferably Nmod is selected from the group consisting of a methyl group and -CH2COOH, and most preferably Nmod is a methyl group, wherein the side chain of Xaal optionally comprises a group Zlb, wherein the side chain of Xaal and the a-nitrogen atom of Xaal optionally form a heterocycle, with the proviso that if the side chain of Xaal and the a-nitrogen atom of Xaal form a heterocycle, the N-terminal modification group Nmod is absent, or

[0239] (b) a residue of an L-a-hydroxy acid comprising a side chain, wherein the side chain optionally comprises a group Zlb,

[0240] H is a hydrogen atom which is covalently linked to (a) the a-nitrogen atom of Xaal if Xaal is a residue of an a-amino acid comprising a side chain and one N-terminal modification group Nmod covalently attached to the a-nitrogen atom of the amino acid, or (b) the oxygen atom of the a-hydroxy group of Xaal if Xaal is a residue of an L-a-hydroxy acid comprising a side chain,

[0241] Xaa2 is a residue of an L-a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain comprises an optionally substituted indole or benzothiophene group,

[0242] Xaa3 is a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z2,

[0243] Xaa4 is a residue of an L-a-amino acid comprising a hydrophobic side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain of Xaa4 and the a-nitrogen atom of Xaa4 optionally form a heterocycle,

[0244] Xaa5 is a residue of an a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z3,

[0245] Xaa6 is a residue of an a-amino acid comprising a side chain, preferably a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z4, wherein the side chain of Xaa6 and the a-nitrogen atom of Xaa6 optionally form a heterocycle,

[0246] Xaa7 is a residue of an L-a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain comprises an aryl or heteroaryl group, preferably a bicyclic aryl or heteroaryl group,

[0247] Cext is a moiety covalently attached to the carbonyl group of Xaa7, which is represented by one of the formulae (la), (lb), (Ic), (Id), and (le): Cterm (la)

[0248] Xaa8 - Cterm (lb)

[0249] Xaa8 - Xaa9 - Cterm (Ic)

[0250] Xaa8 - Xaa9 - XaalO - Cterm (Id)

[0251] Xaa8 - Xaa9 - XaalO - Xaal 1 (le) wherein,

[0252] Xaa8 is a residue of glycine or a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z5,

[0253] Xaa9 is a residue of an a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, preferably Xaa9 is a residue of an L-a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain optionally comprises a group Z6, wherein the side chain of Xaa9 and the a-nitrogen atom of Xaa9 optionally form a heterocycle,

[0254] XaalO is a residue of an a-amino acid comprising a side chain, preferably a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z7, wherein the side chain of XaalO and the a-nitrogen atom of XaalO optionally form a heterocycle,

[0255] Xaal l is a residue of a compound comprising an amino group and optionally comprising a carbonyl group, wherein the amino group is covalently attached to the carbonyl group of XaalO, wherein if the carbonyl group is present, said carbonyl group is covalently attached to a C-terminal modification group Cterm, preferably Xaal 1 is

[0256] (a) a residue of an a-amino acid comprising a side chain, a C-terminal modification group Cterm and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain optionally comprises a group Z8, wherein the side chain of Xaal l and the a-nitrogen atom of Xaal 1 optionally form a heterocycle, or

[0257] (b) a residue of an optionally substituted P-amino alcohol, or

[0258] (c) a residue of a (C1-C6)alkylamine such as cyclohexylamine, or of a (C2- Ce)alkyldiamine such as ethylenediamine,

[0259] Cterm is a C-terminal modification group, which is selected from the group consisting of -NH2, -OH, a group Z9, and -NHRcterm, wherein Rctermis selected from group consisting of a (Ci-Ce)alkyl group, a benzyl group, a 2-phenylethyl group and a 3 -phenylpropyl group, each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently an effector E, such as a chelator, which may optionally comprise a linker moiety L that covalently links the effector E to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, the effector E being preferably selected from the group consisting of:

[0260] (a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and

[0261] (P) a chelator optionally comprising a radionuclide; and

[0262] (y) a drug, preferably a cytotoxic drug; and

[0263] (5) an immune cell engaging effector, preferably recruiting and stimulating T cells, natural killer cells (NK cells) and / or phagocytotic cells.

[0264] In a preferred embodiment, the compound of the invention comprises at least one group Z, i.e. at least one of Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and / or Z9, wherein each group Z independently comprise an optional linker moiety L.

[0265] In a more preferred embodiment, the compound of the invention comprises one or two groups Z, i.e. one or two selected from the group consisting of Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9which independently comprise an optional linker moiety L. In particular, the compound of the invention may comprise one or two groups Z selected from Z3, Z4and Z5, preferably from Z3and Z5. More preferably, the compound of the invention comprises one group Z selected from the group consisting of Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9, which optionally comprises a linker moiety L. In particular, the compound of the invention may comprise one group Z selected from Z3, Z4and Z5. Most preferably, the compound of the invention comprises a group Z3.

[0266] In a preferred embodiment, each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently a chelator which may optionally comprise a linker moiety L, wherein the chelator comprises a radionuclide (as described below), and wherein preferably the chelator is independently a residue of DOTA, DOTAGA, DOTAM, Crown, DOTP, NOTA, NOD AGA, NODA-MPAA, HBED, TETA, CB-TE2A, DTP A, CHX-A”-DTPA, DFO, Macropa, HOPO ligand platform, TRAP, THP, AAZTA, DATA, NOPO, PCTA, PSC, sarcophagine, FSC, DEPA, DE4TA, NETA, NE3TA, H4octapa, H4CHXoctapa, H4pypa, H4py4pa, HYNIC, NxS4-x (N4, N2S2, N3S),99mTc(CO)3-chelators.

[0267] More preferably, each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently a chelator which may optionally comprise a linker moiety L, wherein the chelator comprises a radionuclide (as described below), and wherein the chelator is independently a residue of is a residue of DOTA, DOTAGA, DOTAM, Crown, NOTA, NODAGA, NODA-MPAA, CB- TE2A, CHX-A”-DTPA, DFO, Macropa, THP, AAZTA, NOPO, PCTA, PSC, sarcophagine, NETA, H4CHXoctapa, H4pypa and N4, preferably of DOTA, DOTAGA, DOTAM, NOTA, NODAGA, Macropa, Crown, NOPO, PCTA, PSC and N4, more preferably of DOTA, DOTAM, Macropa, NOTA, PSC or NODAGA, and most preferably of DOTA.

[0268] In one embodiment, Cterm is attached to the carbonyl group of the residue Xaa7 in formula (la), Xaa8 in formula (lb), Xaa9 in formula (Ic), XaalO in formula (Id) and Xaal 1 in formula (le) via a linker L comprising one amino acid or a dipeptide, preferably the linker is absent or consists of one or two a-amino acids, most preferably the linker is absent or consists of one or two a-amino acids, wherein at least one of the amino acids comprises a polar or charged side chain.

[0269] In one embodiment, Cext is a moiety covalently attached to the carbonyl group of Xaa7, which is represented by any one of the formulae (la), (lb), (Ic), (Id), (le), (If) and (Ig):

[0270] Cterm (la)

[0271] Xaa8 - Cterm (lb)

[0272] Xaa8 - Xaa9 - Cterm (lc) Xaa8 - Xaa9 - XaalO - Cterm (Id)

[0273] Xaa8 - Xaa9 - XaalO - Xaal 1 (le)

[0274] Xaa8 - Xaa9 - XaalO - Xaal 1 - Xaal 2 - Cterm (If)

[0275] Xaa8 - Xaa9 - XaalO - Xaal 1 - Xaal2 - Xaal3 - Cterm (Ig) wherein,

[0276] Cterm, Xaa8, Xaa9 and XaalO are as defined above with respect to formulae (la) to (le), and

[0277] • if Cext is represented by the formula (le):

[0278] Xaal l is a residue of a compound comprising an amino group and optionally a carbonyl group, wherein the amino group is covalently attached to the carbonyl group of XaalO, wherein if the carbonyl group is present, said carbonyl group is covalently attached to a C-terminal modification group Cterm, preferably Xaal 1 is

[0279] (a) a residue of an a-amino acid comprising a side chain, a C-terminal modification group Cterm and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain optionally comprises a group Z8, wherein the side chain of Xaal l and the a-nitrogen atom of

[0280] Xaal 1 optionally form a heterocycle, or

[0281] (b) a residue of an optionally substituted P-amino alcohol, or

[0282] (c) a residue of a (C1-C6)alkylamine such as cyclohexylamine, or of a (C2- Ce)alkyldiamine such as ethylenediamine,

[0283] • if Cext is represented by the formula (If):

[0284] Xaal l is a residue of an a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain optionally comprises a group Z8, wherein the side chain of Xaal l and the a-nitrogen atom of

[0285] Xaal 1 optionally form a heterocycle, and

[0286] Xaal2 is a residue of an amino acid comprising a side chain, wherein the side chain optionally comprises a group Z10, wherein a C-terminal modification group Cterm is covalently attached to the carbonyl group of Xaal2, preferably Xaal2 is a residue of an a-amino acid comprising a polar or charged side chain, wherein the side chain optionally comprises a group Z10;

[0287] • if Cext is represented by the formula (Ig):

[0288] Xaal l is a residue of an a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain optionally comprises a group Z8, wherein the side chain of Xaal l and the a-nitrogen atom of Xaal 1 optionally form a heterocycle,

[0289] Xaal2 is a residue of an amino acid comprising a side chain, wherein the side chain optionally comprises a group Z10, preferably Xaal2 is a residue of an a-amino acid comprising a polar or charged side chain,

[0290] Xaal 3 is a residue of an amino acid comprising a side chain, wherein the side chain optionally comprises a group Z11, wherein a C-terminal modification group Cterm is covalently attached to the carbonyl group of Xaal3, preferably Xaal 3 is a residue of an a-amino acid comprising a polar or charged side chain, wherein the side chain optionally comprises a group Z11, more preferably at least one of Xaal2 and Xaal3 is a residue of an a-amino acid comprising a polar or charged side chain, each group Z8, Z10and Z11is independently an effector E, such as a chelator, which may optionally comprise a linker moiety L that covalently links the effector E to Xaal 1, Xaal2 or Xaal3, the effector E being preferably selected from the group consisting of

[0291] (a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and

[0292] (P) a chelator optionally comprising a chelated radionuclide; and

[0293] (y) a drug, preferably a cytotoxic drug; and (5) an immune cell engaging effector, preferably recruiting and stimulating T cells, natural killer cells (NK cells) and / or phagocytotic cells.

[0294] In a preferred embodiment, the compound is represented by the formula (I), wherein at least one, e.g., one, two, three, four, five, six, seven, eight, nine, ten, eleven, twelve or thirteen of Xaal, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO, Xaal l, Cext and Cterm is defined as follows:

[0295] (1) Xaal is a residue of formula (Ila) or formula (lib) : wherein, in formula (Ila):

[0296] Rlais selected from the group consisting of -H, a (Ci-Ce)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)bRld, preferably Rlais selected from the group consisting of -H and a group of formula -(CH2)bRld, wherein Rldis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein Rldoptionally comprises a group Zlb, preferably Rldis selected from the group consisting of -H, a polar and a charged group, more preferably Rldis selected from the group consisting of -H, -OH, -CONH2, -COOH, -C(O)Zlb, -NH2, -NH(Zlb), -NH(CH3), -N(CH3)2, -N(CH3)3+, -SO3H, -NH-CONH2, -NH-C(NH)NH2and -NH-C(NH)-NH(CH3), wherein b = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)bRldgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)bRldgroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably b = 1, 2 or 3,

[0297] Rlbis selected from the group consisting of -H and a methyl group, with the proviso that if Rlais -H, Rlbis -H, preferably Rlbis -H, Xlais selected from the group consisting of -O- and -N(Nmod)-, preferably Xlais -N(Nmod)-, wherein Nmod is selected from the group consisting of -H, -CH2COOH, -CH2CONH2, -CH2C(O)Zla, -(CH2)cNHZla, a (Ci-C6)alkyl group and a group of formula -(CH2)cRle, wherein Rleis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein Rleoptionally comprises a group Zla, preferably Rleis selected from the group consisting of -H, -NH(Zla), a polar and a charged group, more preferably Rleis selected from the group consisting of -H, -OH, -CONH2, -COOH, -NH-CONH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Zla) and -NH-C(NH)NH2, wherein c = 2, 3, 4 or 5, wherein optionally one or two hydrogens of said two, three, four or five -CH2- groups of the -(CH2)cRlegroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)cRlegroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably c = 2 or 3, preferably Nmod is selected from the group consisting of -H, a (C1-C3)alkyl group and -CH2COOH, more preferably Nmod is selected from the group consisting of a methyl group and -CH2COOH, most preferably Nmod is a methyl group, in formula (lib) : a = 1, 2 or 3, preferably a = 1 or 2, more preferably a = 2,

[0298] Rlcselected from the group consisting of -H, -OH, -F, -NH2 and a (C1-C3)alkyl group, preferably Rlcis -H,

[0299] Xlbis selected from the group consisting of -CH2-, -CH(OH)-, -CH(F)-, -CH(NH2)-, -CH(NHRlg)-, -NH-, -S-, -SO-, -SO2- and -O-, wherein Rlgis a methyl, an acetyl (Ac) or a group Zlb, preferably Xlbis -CH2-, preferably Xaal is a residue of an M-methyl-I.-a-amino acid, an Na-(carboxymethyl)- L-a-amino acid, iminodiacetic acid (Ida) or (5)-piperidine-2-carboxylic acid (Pip), more preferably Xaal is a residue of an amino acid selected from the group consisting of Pip, 7V-methyl-glycine (Nmg), A-methyl-I.-alanine (Nma), N-methyl-L-serine (Nms), N- methyl-L-aspartic acid (Nmd), A-methyl-L-glutamic acid (Nme), M-methyl-L-lysine (Nmk), Mz-methyl-M-methyl-I.-lysine (Nmk(Me)), M / -i'nethyl-M,M-dimethyl-I.-lysine (KMe3a), Na- methyl-M,M,M-trimethyl-I.-lysine (KMe4), M-methyl-I.-ornithine (Nmo), M-methyl-M- methyl-L-omithine (Nmo(Me)), M-(carboxymethyl)-I.-ornithine (Cmo), M-(carboxymethyl)- M-methyl-L-omithine (Cmo(Me)), (S)-4-amino-2-(methylamino)butanoic acid (Mdab), N- (carboxymethyl)-L-alanine (Mida), (5)-2,4-bis(methylamino)butanoic acid (Mdab(Me)), (5)-3- amino-2-(methylamino)propanoic acid (Mdap), (5)-2,3-bis(methylamino)propanoic acid (Mdap(Me)), (S)-azepane-2-carboxylic acid (Azp), (S)-morpholine-3 -carboxylic acid (Mor) and Ida, most preferably Xaal is a residue of an amino acid selected from the group consisting of Pip and Nma,

[0300] (2) Xaa2 is a residue of an amino acid of formula (III): wherein, in formula (III):

[0301] R2ais selected from the group consisting of H and a (C1-C2)alkyl group, preferably R2ais selected from the group consisting of -H and a methyl group, more preferably R2ais -H,

[0302] R2band R2care each independently selected from the group consisting of -H and a methyl group,

[0303] R2dand R2eare each independently selected from the group consisting of -H, -OH, -F, -Cl and a methyl group,

[0304] R2f, R2gand R2hare each independently selected from the group consisting of -H and -F, preferably each of R2b, R2c, R2d, R2e, R2f, R2gand R2his -H, preferably Xaa2 is a residue of an amino acid selected from the group consisting of Trp, 7-chloro-L -tryptophan (7Clw), 7-methyl-L -tryptophan (7Mw), 7-fluoro-L -tryptophan (7Fw), (2 S, 3 S)-P-methyl-L -tryptophan (Bmw) and N-methyl-L -tryptophan (Nmw), more preferably Xaa2 is a residue of Trp,

[0305] (3) Xaa3 is a residue of an amino acid of formula (IV): wherein, in formula (IV):

[0306] R3aand R3b(a) are each independently selected from the group consisting of -H, -F and a (C1-C2)alkyl group, or

[0307] (b) form together a 3-, 4-, 5- or 6-membered carbocycle or heterocycle, preferably a 3-, 4- or 5-membered carbocycle, preferably R3aand R3bare each independently selected from the group consisting of H and a methyl group,

[0308] R3cis selected from the group consisting of a halogen atom, a polar group, a negatively charged group and an aliphatic group, wherein R3coptionally comprises a group Z2, preferably R3cis selected from the group consisting of -OH, -COOH, -SO3H, -C0NH(R3d), -NH-C0NH(R3d), -SO2NH(R3d), -F, -Cl, a (Ci-C4)alkyl group, a (C3-C4)carbocycle group and -NH(Z2), wherein R3Cis optionally linked to the P-carbon atom of Xaa3 by a linker comprising one, two or three -CH2- groups and one hydrogen atom of said one, two, or three -CH2- groups that link R3cto the P-carbon atom of Xaa3 is optionally replaced by a substituent selected from the group consisting of -F, -OH, -COOH, a methyl group, and / or wherein one of the said -CH2- groups, which is different from the R3cadjacent -CH2- group, is optionally replaced by -O-, -S-, -SO- or -SO2-, wherein R3dis selected from the group consisting of -H, a methyl group and a (C2- C4)alkyl group, wherein said (C2-C4)alkyl group is optionally substituted by one or two substituents independently selected from the group consisting of -OH, -COOH, -SO3H and -CONH2, more preferably R3cis selected from the group consisting of a methyl group, -COOH, -CONH2 and -SO3H and R3cis optionally linked to the P-carbon atom of Xaa3 by one -CH2- group, most preferably R3cis selected from the group consisting of -COOH and -SO3H and the optional linker is absent, preferably Xaa3 is a residue of an amino acid selected from the group consisting of Asp, L-cysteic acid (Cya), P,P-dimethyl-L-aspartic acid (Dmd), P,P-dimethyl-L-cysteic acid (Penox), Glu, Vai and Asn, more preferably Xaa3 is a residue of an amino acid selected from the group consisting of Penox, Asp and Cya,

[0309] (4) Xaa4 is a residue of an amino acid of formula (V): wherein, in formula (V):

[0310] R4ais selected from the group consisting of -H and a (C1-C3)alkyl group, preferably R4ais selected from the group consisting of -H and a methyl group,

[0311] R4bis selected from the group consisting of a (C3-Cs)alkyl group, a (C3-C7)carbocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)dR4c, wherein one or two hydrogen atoms of R4bare optionally replaced by atoms or groups each and independently selected from the group consisting of -NH2, -OH, a halogen atom and a (Ci- C3)alkyl group, preferably -F, -Cl or a methyl group, preferably R4bis selected from the group consisting of a (C3-Cs)alkyl group, a (C5-Ce)carbocycle, a phenyl group, a 2-thienyl group and a group of formula -(CH2)dR4c, wherein d = 1, 2 or 3, preferably d = 1, wherein R4cis selected from the group consisting of a (C3-C7)carbocycle, an aryl group and a heteroaryl group, wherein one or two hydrogen atoms of R4Care optionally replaced by atoms or groups each and independently selected from the group consisting of -NH2, -OH, a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, preferably R4cis selected from the group consisting of a (C4-Ce)carbocycle, a phenyl group and a 2-thienyl group, and wherein one -CH2- group of R4bis optionally replaced by an atom selected from the group consisting of -O- and -S-, or alternatively, R4aand R4bform together an optionally up to two-fold substituted 5-, 6-, or 7-membered heterocycle, wherein each substituent is each and independently selected from the group consisting of a (Ci- Cs)alkyl group, a halogen atom, -NH2 and -OH, preferably R4aand R4bform together a 6-membered unsubstituted heterocycle, preferably Xaa4 is a residue of an amino acid selected from the group consisting of L-neopentyl-glycine (Npg), V-methyl-I.-neopentyl-glycine (Mnpg), Leu, A-m ethyl -L -leucine (Nml), L-homoleucine (Hie), Phe, L-y-ethyl-leucine (Gel), V-methyl-L-y-ethyl-leucine (Mgel), L-norleucine (Nle), V-methyl-L-norleucine (NMB), L-cyclobutyl-alanine (Cba), L-cyclopentyl- alanine (Cpa), L-cyclohexyl-alanine (Cha), L-cyclopentyl-glycine (Cpg) and L-cyclohexyl- glycine (Chg), more preferably Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Leu, Mnpg, Nml, and Chg, even more preferably Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, most preferably Xaa4 is a residue of Npg,

[0312] (5) Xaa5 is a residue of an amino acid of formula (Via) or of (VIb): wherein, in formula (Via): R5ais selected from the group consisting of -H, a (Ci-Ce)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)fR5c, preferably R5aselected from the group consisting of -H and a group of formula -(CH2)fR5c, wherein R5cis selected from the group consisting of -H, a polar, a charged and a hydrophobic group, wherein R5coptionally comprises a group Z3, preferably R5cis selected from the group consisting of -H, - NH(Z3), -C(O)Z3, a polar group and a charged group, more preferably R5cis selected from the group consisting of -H, -OH, -CONH2, -COOH, -C(O)Z3, -NH-CONH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Z3), -NH-C(NH)NH2and -NH-C(NH)-NH(CH3), wherein f = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)fR5cgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)fR5cgroup which is different from the terminal -CH2- groups of is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably f = 1, 2, 3 or 4,

[0313] R5bis selected from the group consisting of -Hand a group of formula - (CH2)gR5d, wherein R5dis selected from the group consisting of -H, a polar, a charged and a hydrophobic group, wherein R5doptionally comprises a Z3group, preferably R5dis selected from the group consisting of -H, a polar group and a charged group, more preferably R5dis selected from the group consisting of -H, -OH, -CONH2, -COOH, -SO3H, -NH2, -NH(CH3), -N(CH3)2 and -N(CH03+, most preferably R5dis selected from the group consisting of -H and -OH, wherein g = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)gR5dgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)gR5dgroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably R5bis selected from the group consisting of -H and a methyl group, preferably g = 1, 2, 3 or 4, more preferably g = 1 or 2, in formula (VIb): e = 0, 1, 2 or 3, preferably e = 2,

[0314] X5is absent or selected from the group consisting of -N(R5e)-, -O-, -S- , -SO-, -SO2- and -CH2-, wherein R5eis selected from the group consisting of -H, -Ac, (Ci- C3)alkyl group and a group Z3, preferably R5eis selected from the group consisting of -H, a methyl group and a group Z3, more preferably R5eis a group Z3, wherein optionally one or two hydrogen atoms of any -CH2- groups that form the side chain are each and individually replaced by -F or a methyl group, preferably X5is selected from the group consisting of -N(R5e)-, -O- and -CH2-, more preferably X5is -N(R5e)-, preferably Xaa5 is a residue of an a,a-dialkylamino acid of formula (Via), an L-a-amino acid of formula (Via) comprising a polar or charged side chain, or an amino acid of formula (VIb), more preferably Xaa5 is a residue of an amino acid selected from the group consisting of 2-aminoisobutyric acid (Aib), a-methyl-serine (Ams), a-methyl-lysine (Amk), (5)-2,3- diaminopropionic acid (Dap), (5)-2,4-diaminobutyric acid (Dab), L-omithine (Orn), Lys, Ns- methyl-L-omithine (Om(Me)), M>,M>-dimethyl-I.-ornithine (OMe2), M,M,V5-timethyl-L- ornithine (OMe3), M-methyl-I.-lysine (Lys(Me)), M,M-dimethyl-I.-lysine (KMe2), NE,NE,NE- trimethyl-L-lysine (KMe3), Gly, Ala, Ser, 4-amino-tetrahydropyran-4-carboxylic acid (Thp), 4- amino-piperidine-4-carboxylic acid (Ape), 1 -amino- 1 -cyclohexane carboxylic acid (Egz), Apc(Z3), Lys(Z3), Om(Z3), Dab(Z3) and Dap(Z3), most preferably Xaa5 is a residue of an amino acid selected from the group consisting of Aib, Ams, Thp, Ape, Lys(Z3), Om(Z3) and Apc(Z3),

[0315] (6) Xaa6 is a residue of an amino acid of formula (Vila), (Vllb) or (Vile): wherein, in formula (Vila):

[0316] R6ais selected from the group consisting of -Hand a group of formula -(CH2)kR6d, wherein R6dis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein R6doptionally comprises a group Z4, preferably R6dis selected from the group consisting of -H, a polar group and a charged group, more preferably R6dis selected from the group consisting of -H, -OH, -CONH2, -COOH, - SO3H, -NH2, -NH(CH3), -N(CH3)2and -N(CH3)3+, most preferably R6dis selected from the group consisting of -H, -OH, -CONH2 and -COOH, wherein k = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)kR6dgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)kR6dgroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably k = 1, 2 or 3, more preferably k = 1 or 2, preferably R6ais selected from the group consisting of -H and a methyl group, more preferably R6ais -H,

[0317] R6bis selected from the group consisting of -H, a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)mR6e, preferably R6bis selected from the group consisting of -H and a group of formula -(CH2)mR6e, wherein R6eis selected from the group consisting of -H, a polar, a charged and a hydrophobic group, wherein R6eoptionally comprises a group Z4, preferably R6eis selected from the group consisting of -H, -NH(Z4), -C(O)Z4, a polar group and a charged group, more preferably R6eis selected from the group consisting of -H, -OH, -CONH2, -COOH, -C(O)Z4, -NH-C0NH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Z4) and -NH-C(NH)NH2and -NH-C(NH)-NH(CH3), wherein m = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)mR6egroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)mR6egroup which is different from the terminal -CH2- groups of is optionally replaced by -O-, -S-, -SO- or -SO2- , preferably m = 1, 2, 3 or 4, in formula (Vllb): h = 0, 1, 2 or 3, preferably h = 2,

[0318] X6ais absent or selected from the group consisting of -NR6f-, -O-, -S- , -SO-, -SO2- and -CH2-, wherein R6fis selected from the group consisting of -H, -Ac, (Ci- C3)alkyl group and a group Z4, preferably R6fis selected from the group consisting of -H, a methyl group and a group Z4, more preferably R6fis a group Z4, wherein optionally one or two hydrogen atoms of any of the -CH2- groups that form the side chain are each and individually substituted by -F or a methyl group, preferably X6ais selected from the group consisting of -N(R6f)-, -O- and -CH2-, more preferably X6ais -N(R6f)-, in formula (Vile):

[0319] R6Cis selected from the group consisting of -H, -OH, -F, -NH2, a (Ci- C3)alkyl group, preferably R6cis -H,

[0320] X6bis selected from the group consisting of -CH(R6g)-, -S-, -O-, -NH-, preferably X6bis -CH(R6g)-, wherein R6gis selected from the group consisting of -H, -OH, -F, -NH2 and a (C1-C3)alkyl group, preferably R6gis -H, i = 1 or 2, preferably i = 1, preferably Xaa6 is a residue of an L-amino acid amino acid of formula (Vila), and more preferably Xaa6 is a residue of an L-amino acid of formula (Vlld): wherein, in formula (Vlld): R6bis selected from the group consisting of -Hand a group of formula - (CH2)mR6e, wherein R6eis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein R6eoptionally comprises a group Z4, preferably R6eis selected from the group consisting of -H, -NH(Z4), -C(O)Z4, a polar and a charged group, more preferably R6eis selected from the group consisting of -H, -OH, -CONH2, -COOH, -C(O)Z4, -NH-CONH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Z4) and -NH-C(NH)NH2and -NH-C(NH)-NH(CH3), wherein m = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)mR6egroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)mR6egroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably m = 1, 2, 3 or 4, more preferably m = 1 or 2, preferably Xaa6 is a residue of an amino acid selected from the group consisting of Asn, Asp, Glu, Gin, Cya, Lys, Lys(Me), Om, Orn(Me), Dab, Dab(Me), Gly, Ala, Thr, Ser, Leu, Tyr, Ape, Lys(Z4) and Apc(Z4), more preferably Xaa6 is a residue of an amino acid selected from the group consisting of Ala, Asn, Asp, Cya, Lys, Lys(Z4), Lys(Me), Thr and Ser, and most preferably a residue of Asn,

[0321] (7) Xaa7 is a residue of an amino acid of formula (Villa) or of formula (VIHb): (Vlllb) wherein, in formula (Villa):

[0322] R7ais selected from the group consisting of -H and a (C1-C2)alkyl group, preferably R7ais -H or a methyl group, more preferably R7ais -H, R7band R7care each independently selected from the group consisting of -H and a methyl group, preferably R7band R7care -H,

[0323] R7dpje j^7fancj j^7hare each independently selected from the group consisting of -H, -OH, a (C1-C2)alkyl group, -OCH3 and a halogen atom, preferably R7d, R7e, R7fand R7hare each independently selected from the group consisting of -H, -F, -Cl, -Br and a methyl group, more preferably R7d, R7eand R7hare each independently selected from the group consisting of -H, -F, -Cl and a methyl group, most preferably R7d, R7eand R7hare -H, and R7fis selected from the group consisting of -Br and -Cl, R7gis selected from the group consisting of -H, -F and -Cl, more preferably R7gis selected from the group consisting of -H and -F, most preferably R7gis -H,

[0324] X7aselected from the group consisting of -NH- and -S-, preferably X7ais -NH-, in formula (Vlllb):

[0325] R7ais selected from the group consisting of -H and a (C1-C2)alkyl group, preferably R7ais -H or a methyl group, more preferably R7ais -H,

[0326] R7band R7care each independently selected from the group consisting of -H and a methyl group, preferably R7band R7care -H,

[0327] R71and R7kare each independently selected from the group consisting of -H, -OH, a methyl group, -OCH3 and a halogen atom, preferably R71and R7kare each independently selected from the group consisting of -H, -F, -Cl and a methyl group, more preferably R71and R7kare -H,

[0328] X7bselected from the group consisting of -CH= and -N=, preferably X7bis -CH=, preferably Xaa7 is a residue of an amino acid selected from the group consisting of Trp, 6-chloro-L -tryptophan (6Clw), L-6-methyl-tryptophan (6Mw), 5-chloro-L -tryptophan (5Clw), 3-benzothienyl-L-alanine (Bta), 3-(l-naphthyl)-L-alanine (INi), 5 -fluoro-L -tryptophan (5Fw), 6-fluoro-L -tryptophan (6Fw), 7Fw and 6-bromo-L -tryptophan (Brw6), more preferably Xaa7 is a residue of an amino acid selected from the group consisting of 6Clw and Brw6, (8) Xaa8 is a residue of an amino acid of formula (IX): wherein, in formula (IX):

[0329] R8ais selected from the group consisting of -H and a group of formula - (CH2)nR8b, wherein R8bis selected from the group consisting of -H, a polar, a charged and a hydrophobic group, wherein R8boptionally comprises a group Z5, preferably R8bis selected from the group consisting of -H, -NH(Z5), -C(O)Z5, a polar group and a charged group, more preferably R8bcomprises a positively charged group, and even more preferably R8bis selected from the group consisting of -N(R8c)(R8d), -N(CH3)2(R8e)+, -NH(Z5), -N(R8f)-C(N(R8g))-N(R8h)(R81) and a piperidinyl group, wherein R8c, R8d, R8f, R8g, R8hand R8iare each independently selected from the group consisting of -H and a (C1-C3)alkyl group, preferably R8cand R8dare each independently selected from the group consisting of -H and a methyl group, wherein R8eis selected from the group consisting of a (C1-C3)alkyl group and -(CEh^SOs’, most preferably R8bis selected from the group consisting of -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH-C(NH)NH2, -NH-C(NH)-NH(CH3), -NH-C(NH)-N(CH3)2and -NH-C(N(CH3))-NH(CH3), wherein n = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of the -(CH2)nR8bgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)nR8bgroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably n = 1, 2, 3 or 4, more preferably n = 3 or 4, preferably Xaa8 is a residue of an amino acid selected from the group consisting of Lys, Lys(Me), KMe2, KMe3, (5)-3-((5-amino-5-carboxypentyl)dimethylammonio)propane-l- sulfonate (Kzw), Lys(Z5), 3-(4-piperidinyl)-L-alanine (Egg), Arg, A® -methyl -L-argi nine (Arg(Me)), A®,A®-dimethyl-L-arginine (RMe2), L-homoarginine (Har), Orn, Orn(Me), 0Me2, 0Me3, y-(2-pyridyl)-L-omithine (Opy), L-homolysine (Hly), L-citrulline (Cit), Gin, L -homocitrulline (Hci), M.,,M. / -dirnethyl-I,-arginine (Egd) and M-iso-propyl-I.-lysine (Kip), more preferably Xaa8 is a residue of an amino acid selected from the group consisting of Lys(Me), KMe2, KMe3, Kzw, Egg, Lys(Z5), Arg(Me) and RMe2, and most preferably a residue of KMe3,

[0330] (9) Xaa9 is a residue of an amino acid of formula (Xa) or (Xb): wherein, in formula (Xa):

[0331] R9ais selected from the group consisting of -H and (C1-C2)alkyl group, preferably R9ais -H,

[0332] R9bis selected from the group consisting of -H and a group of formula -(CH2)0R9e, wherein R9eis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein R9eoptionally comprises a group Z6, preferably R9eis selected from the group consisting of -H, an aryl group, a heteroaryl group, a polar group and a charged group, more preferably R9eis selected from the group consisting of -H, an aryl group, a heteroaryl group, -OH, -CONH2, -COOH, -NH-CONH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Z4) and -NH- C(NH)NH2, most preferably R9eis selected from the group consisting of -H, a methyl group, an aryl group and a heteroaryl group, wherein said aryl group or heteroaryl group is optionally substituted by 1 or 2 substituents, preferably 1 substituent, wherein, preferably, each substituent is independently selected from the group consisting of a halogen atom, a (C1-C3)alkyl group, -CN, -COOH, -CONH2, -NO2, - NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C3)alkyl group, wherein each substituent is optionally linked, preferably via a methylene group, to the aryl group or heteroaryl group, and wherein said aryl group or heteroaryl group preferably comprises one aromatic ring, wherein o = 1, 2, 3 or 4, wherein optionally one or two hydrogen atoms of said one, two, three or four -CH2- groups of the -(CH2)0R9egroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)0R9egroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably o = 1 or 2, more preferably o = 1,

[0333] R9Cis selected from the group consisting of -H and methyl group, with the proviso that if R9bis -H, R9cis -H, preferably R9cis -H, in formula (Xb):

[0334] R9dis selected from the group consisting of -H, -OH, -F, -NH2, a (Ci- C3)alkyl group, preferably R9dis -H,

[0335] X9is selected from the group consisting of -CH(R9f)-, -S-, -O-, -NH-, preferably X9is -CH(R9f)-, wherein R9fis selected from the group consisting of -H, -OH, -F, -NH2 and a methyl group, preferably R9fis -H, p = 1 or 2, preferably p = 1, preferably Xaa9 is a residue of an amino acid selected from the group consisting of Gly, Ala, Dab, Glu, Pro, 4-carbamoyl-L-phenylalanine (Pcnf), Lys(Z6) and Tyr, more preferably Xaa9 is a residue of an amino acid selected from the group consisting of Ala and Tyr,

[0336] (10) XaalO is a residue of formula (Xia) or (Xlb): wherein, in formula (Xia):

[0337] R10ais selected from the group consisting of -H and a group of formula -(CH2)rR10c, wherein R10cis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein R10coptionally comprises a group Z7, preferably R10cis selected from the group consisting of -NH(Z7), a polar group and a charged group, more preferably R10cis a negatively charged group, most preferably R10cis selected from the group consisting of -COOH and -SO3H, wherein r = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)rR10cgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)rR10cgroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably r = 1, 2, 3 or 4, more preferably r = 1 or 2, in formula (Xlb):

[0338] R10bis selected from the group consisting of -H, -OH, -F, -NH2, a (Ci- C3)alkyl group, preferably R10bis -H,

[0339] X10is selected from the group consisting of -CH(R10d)-, -S-, -O-, -NH-, preferably X9is -CH(R10d)-, wherein R10dis selected from the group consisting of -H, -OH, -F, -NH2 and a methyl group, preferably R10dis -H, q = 1 or 2, preferably q = 1, preferably XaalO is a residue of an amino acid selected from the group consisting of Asp, Cya, Glu, Ser, Lys and Thr, more preferably XaalO is a residue of an amino acid selected from the group consisting of Asp and Cya,

[0340] (11) Xaal 1 is a residue of formula (Xlla):

[0341] R11 a

[0342] ^N^R11 d

[0343] R11 bR11 c(Xlla) wherein, in formula (Xlla): Rl lais selected from the group consisting of -H and a (C1-C2)alkyl group, preferably Rllais -H,

[0344] Rl lbis selected from the group consisting of -H, a ((C1-C)8)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)sRl le, wherein Rl leis selected from the group consisting of a polar group, a charged group and a hydrophobic group, wherein Rl leoptionally comprises a group Z8, preferably Rl leis a hydrophobic group, more preferably Rlleis selected from the group consisting of an aryl group and a heteroaryl group, wherein s = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)sRl legroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)sRllegroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably s = 1, 2 or 3, more preferably s = 1, or alternatively, Rl laand Rllbform together an optionally up to two-fold substituted 5-, 6-, or 7-membered heterocycle, wherein each substituent is each and independently selected from the group consisting of a (Ci- C3)alkyl group, a halogen atom, -NH2 and -OH, preferably Rl laand Rllbform together a 5- or 6-membered heterocycle,

[0345] Rl lcis selected from the group consisting of -H and a (C1-C2)alkyl group, preferably Rllcis -H, or alternatively, Rllband Rl lcform together an optionally substituted 3-, 4-, 5-, 6- or 7-membered carbocycle or heterocycle, preferably a 6- membered carbocycle, wherein each substituent is independently selected from the group consisting of a (C1-C2)alkyl group, a halogen atom, -NH2 and -OH,

[0346] Rl ldis selected from the group consisting of -H, a (C1-C2)alkyl group, -CH2(0H) and -C(O)-Cterm, preferably Rlldis -C(O)-Cterm, preferably Xaal l is a residue of formula (Xllb) or (XIIc): R11ao i

[0347] N J ICI Cterm

[0348] ' Cterm

[0349] R11b'R11c (XIIb) wherein in formula (Xllb):

[0350] Rl lais selected from the group consisting of -H and a (C1-C2)alkyl group, preferably Rllais -H,

[0351] Rl lbis selected from the group consisting of -H, a ((C1-C)8)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)sRlle, wherein Rl leis selected from the group consisting of a polar group, a charged group and a hydrophobic group, wherein Rl leoptionally comprises a group Z8, preferably Rl leis a hydrophobic group, more preferably Rlleis selected from the group consisting of an aryl group and a heteroaryl group, wherein said aryl group or heteroaryl group is optionally substituted by atoms or groups each and independently selected from the group consisting of -NH2, -OH, -CN, -CONH2, -OCH3, a halogen atom and a (C1-C3)alkyl group, wherein s = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)sRl legroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)sRllegroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably s = 1, 2 or 3, more preferably s = 1,

[0352] Rl lcis selected from the group consisting of -H and a (C1-C2)alkyl group, with the proviso that if Rl lbis -H, Rl lcis -H, preferably Rllcis -H, or alternatively, Rllband Rl lcform together an optionally substituted 3-, 4-, 5-, 6- or 7-membered carbocycle or heterocycle, preferably a 6- membered carbocycle, wherein each substituent is independently selected from the group consisting of a (C1-C2)alkyl group, a halogen atom, -NH2 and -OH,

[0353] Cterm is selected from the group consisting of -NH2, -OH, -NHRctermand a group Z9, wherein Rctermis selected from group consisting of a (Ci- Ce)alkyl group, a benzyl group, a 2-phenylethyl group and a 3- phenylpropyl group, preferably Cterm is NH2, in formula (XIIc):

[0354] Rl lfis selected from the group consisting of -H, -OH, -F, -NH2, a (Ci- C3)alkyl group, preferably Rllfis -H,

[0355] X11is selected from the group consisting of -CH(Rllg)-, -S-, -O-, -NH-, preferably X10is -CH(Rllg)-, wherein Rllgis selected from the group consisting of -H, -OH, -F, -NH2 and a methyl group, preferably Rllgis -H, t = 1, 2 or 3, preferably t = 1 or 2,

[0356] Cterm is selected from the group consisting of -NH2, -OH, -NHRctermand a group Z9, wherein Rctermis selected from group consisting of a (Ci- Ce)alkyl group, a benzyl group, a 2-phenylethyl group and a 3- phenylpropyl group, preferably Cterm is NH2, more preferably Xaal l is a residue of an L-a-amino acid of formula (Xllb), wherein Rl lbis a group of formula -QHR116, wherein Rlleis selected from the group consisting of an aryl group and a heteroaryl group, preferably a phenyl group or 2-thienyl group, wherein said aryl group or heteroaryl group is optionally substituted by one or more, e.g., one, two or three, atoms or groups each and independently selected from the group consisting of -NH2, -OH, - CN, -CONH2, -OCH3, a halogen atom and a (C1-C3)alkyl group, preferably the aryl group or heteroaryl group is unsubstituted or has one substituent, and wherein preferably Cterm is NH2, even more preferably Xaal l is a residue of an amino acid selected from the group consisting of Thi, Phe, Egz, ortho-chloro-phenylalanine (Ocf), 3-(l-naphthyl)alanine (INi), 3- fluoro-phenylalanine (Mff), 2-cyano-L-phenylalanine (Onf), 2-fluoro-L-phenylalanine (Off), Ala and Vai, with Cterm being preferably -NH2, and even more preferably Xaal l is a residue of an amino acid selected from the group consisting of Thi, Phe and Ocf, with Cterm being preferably -NH2, most preferably Xaal 1 is Thi, with Cterm being preferably -NH2,

[0357] (12) Cext is a moiety of formula (le), and (13) Cterm is selected from the group consisting of -NH2, -OH, -NHRctermand a group Z9, wherein Rctermis selected from group consisting of a (Ci-Ce)alkyl group, a benzyl group, a 2-phenylethyl group and a 3 -phenylpropyl group, preferably Cterm is NH2, wherein, in the above formulae, each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently an effector E, such as a chelator, which may optionally comprise a linker moiety L that covalently links the effector E to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, the effector E being preferably selected from the group consisting of:

[0358] (a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and

[0359] (P) a chelator optionally comprising a radionuclide; and

[0360] (y) a drug, preferably a cytotoxic drug; and

[0361] (5) an immune cell engaging effector, preferably recruiting and stimulating T cells, NK cells and / or phagocytotic cells.

[0362] In a preferred embodiment, the compound is represented by the formula (I), wherein at least one, e.g., one, two, three or four, of Xaa2, Xaa4, Xaa7 and Cext is defined as follows:

[0363] (1) Xaa2 is a residue of an amino acid of formula (III) as described above, preferably a residue of an amino acid selected from the group consisting of Trp, 7Clw, 7Mw, 7Fw, Bmw and Nmw, more preferably a residue of Trp,

[0364] (2) Xaa4 is a residue of an amino acid of formula (V) as described above, preferably a residue of an amino acid selected from the group consisting of Npg, Mnpg, Leu, Nml, Hie, Phe, Gel, Mgel, Nle, NMB, Cba, Cpa, Cha, Cpg and Chg, more preferably a residue of an amino acid selected from the group consisting of Npg, Leu, Mnpg, Nml, and Chg, even more preferably a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, and most preferably a residue of Npg,

[0365] (3) Xaa7 is a residue of an amino acid of formula (Villa) or formula (Vlllb) as described above, preferably a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and 6-bromo-L -tryptophan Brw6, more preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6, and

[0366] (4) Cext is a moiety of formula (le) as described above.

[0367] In a more preferred embodiment, the compound is represented by the formula (I), wherein Xaa2, Xaa4, Xaa7 and Cext are defined as follows:

[0368] (1) Xaa2 is a residue of an amino acid of formula (III) as described above, preferably a residue of an amino acid selected from the group consisting of Trp, 7Clw, 7Mw, 7Fw, Bmw and Nmw, more preferably a residue of Trp,

[0369] (2) Xaa4 is a residue of an amino acid of formula (V) as described above, preferably a residue of an amino acid selected from the group consisting of Npg, Mnpg, Leu, Nml, Hie, Phe, Gel, Mgel, Nle, NMB, Cba, Cpa, Cha, Cpg and Chg, more preferably a residue of an amino acid selected from the group consisting of Npg, Leu, Mnpg, Nml, and Chg, even more preferably a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, and most preferably a residue of Npg,

[0370] (3) Xaa7 is a residue of an amino acid of formula (Villa) or formula (Vlllb) as described above, preferably a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, more preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6, and

[0371] (4) Cext is a moiety of formula (le) as described above.

[0372] In a more preferred embodiment, the compound is represented by the formula (I), wherein at least one, e.g., one, two, three, four, five, six, seven, eight, nine, ten, eleven, twelve or thirteen, of Xaal, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO, Xaal l, Cext and Cterm is / are defined as follows:

[0373] (a) Xaal is a residue of an Va-methyl-L-a-amino acid, an Va-(carboxymethyl)-L-a-amino acid,, Ida or Pip, preferably a residue of an amino acid selected from the group consisting of Pip, Nmg, Nma, Nms, Nmd, Nme, Nmk, Nmk(Me), KMe3a, KMe4, Nmo, Nmo(Me), Cmo, Cmo(Me), Mdab, Mdab(Me), Mida, Mdap, Mdap(Me), Azp, Mor and Ida, more preferably a residue of an amino acid selected from the group consisting of Pip and Nma, and still more preferably a residue of Pip,

[0374] (b) Xaa2 is a residue of an amino acid selected from the group consisting of Trp, 7Clw, 7Mw, 7Fw, Bmw and Nmw, and preferably Xaa2 is a residue of Trp,

[0375] (c) Xaa3 is a residue of an amino acid selected from the group consisting of Asp, Cya, Glu, Dmd, Penox, Vai and Asn, and preferably a residue of an amino acid selected from the group consisting of Penox, Asp and Cya,

[0376] (d) Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Mnpg, Leu, Nml, Hie, Phe, Gel, Mgel, Nle, NMB, Cba, Cpa, Cha, Cpg and Chg, preferably a residue of an amino acid selected from the group consisting of Npg, Leu, Mnpg, Nml and Chg, and more preferably a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, and most preferably Xaa4 is a residue of Npg,

[0377] (e) Xaa5 is a residue of an amino acid selected from the group consisting of Aib, Ams, Amk, Dap, Dab, Om, Orn(Me), 0Me2, 0Me3, Lys, Lys(Me), KMe2, KMe3, Gly, Ala, Ser, Thp, Ape, Egz, Apc(Z3), Lys(Z3), Orn(Z3), Dab(Z3) and Dap(Z3), and preferably a residue of an amino acid selected from the group consisting of Aib, Ams, Thp, Ape, Lys(Z3), Orn(Z3) and Apc(Z3), wherein Z3is preferably selected from the group consisting of DOTA, DOTAM, PSC, DOTAGA, NOPO, NODAGA, BnTCMC, DOTAMGAM, PSCGA and NOTA, more preferably Xaa5 is a residue of an amino acid selected from the group consisting of Apc(DOTA), Apc(DOTAM), Apc(PSC), Apc(DOTAGA), Apc(NOPO), Apc(NODAGA), Apc(PSCGA), Apc(BnTCMC), Apc(DOTAMGAM), Apc(PSCGA) and Apc(NOTA),

[0378] (f) Xaa6 is a residue of an amino acid selected from the group consisting of Asn, Asp, Glu, Gin, Cya, Lys(Me), Orn, Orn(Me), Dab, Dab(Me), Gly, Ala, Thr, Ser, Leu, Tyr, Ape, Lys(Z4) and Apc(Z4), wherein Z4is preferably selected from the group consisting of DOTA, DOTAM and PSC, and Xaa6 is preferably a residue of an amino acid selected from the group consisting of Ala, Asn, Asp, Cya, Lys, Lys(Z4), Lys(Me), Thr and Ser, and more preferably Xaa6 is a residue of Asn,

[0379] (g) Xaa7 is a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, and preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6, (h) Xaa8 is a residue of an amino acid selected from the group consisting of Lys, Lys(Me), KMe2, KMe3, Kzw, Egg, Arg, Arg(Me), Lys(Z5), RMe2, Har, Orn, Orn(Me), 0Me2, 0Me3, Opy, Hly, Cit, Gin, Hci, Egd and Kip, wherein Z5is preferably selected from the group consisting of DOTA, DOTAM and PSC, preferably Xaa8 is a residue of an amino acid selected from the group consisting of Lys(Me), KMe2, KMe3, Kzw, Egg, Arg(Me), Lys(Z5) and RMe2, and more preferably a residue of KMe3,

[0380] (i) Xaa9 is a residue of an amino acid selected from the group consisting of Gly, Ala, Dab, Glu, Pro, Pcnf, Lys(Z6) and Tyr, wherein Z6is preferably selected from the group consisting of DOTA, DOTAM and PSC, and preferably Xaa 9 is a residue of an amino acid selected from the group consisting of Ala and Tyr,

[0381] (j) XaalO is a residue of an amino acid selected from the group consisting of Asp, Cya, Glu, Thr, Lys and Ser, and preferably a residue of an amino acid selected from the group consisting of Asp and Cya,

[0382] (k) Xaal 1 is a residue of an amino acid selected from the group consisting of Thi, Phe, Ocf, INi, Mff, Onf, Off, Ala and Vai, preferably a residue of an amino acid selected from the group consisting of Thi, Phe and Ocf, and more preferably a residue of Thi,

[0383] (l) Cext is a moiety of formula (le), and

[0384] (m) Cterm is NH2.

[0385] In an even more preferred embodiment, the compound is represented by the formula (I), wherein at least one, e.g., one, two, three, four, five, six, seven, eight, nine, ten, eleven, twelve or thirteen, of Xaal, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO, Xaal l, Cext and Cterm is / are defined as follows:

[0386] (a) Xaal is a residue of an amino acid selected from the group consisting of Pip and Nma, and preferably a residue of Pip,

[0387] (b) Xaa2 is a residue of Trp,

[0388] (c) Xaa3 is a residue of an amino acid selected from the group consisting of Penox, Asp and Cya,

[0389] (d) Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Leu, Mnpg, Nml and Chg, and preferably a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, and more preferably Xaa4 is a residue of Npg, (e) Xaa5 is a residue of an amino acid selected from the group consisting of Aib, Ams, Thp, Ape, Lys(Z3), Orn(Z3) and Apc(Z3), wherein Z3is preferably selected from the group consisting of DOTA, DOTAM, PSC, DOTAGA, NOPO, NODAGA, BnTCMC, DOTAMGAM, PSCGA and NOTA, preferably Xaa5 is a residue of an amino acid selected from the group consisting of Apc(DOTA), Apc(DOTAM), Apc(PSC), Apc(DOTAGA), Apc(NOPO), Apc(NODAGA), Apc(PSCGA), Apc(BnTCMC), Apc(DOTAMGAM), Apc(PSCGA) and Apc(NOTA),

[0390] (f) Xaa6 is a residue of an amino acid selected from the group consisting of Ala, Asn, Asp, Cya, Lys, Lys(Z4), Lys(Me), Thr and Ser, wherein Z4is preferably selected from the group consisting of DOTA, DOTAM and PSC, and preferably Xaa6 is a residue of Asn,

[0391] (g) Xaa7 is a residue of an amino acid selected from the group consisting of 6Clw and Brw6,

[0392] (h) Xaa8 is a residue of an amino acid selected from the group consisting of Lys(Me), KMe2, KMe3, Kzw, Egg, Arg(Me), Lys(Z5) and RMe2, wherein Z5is preferably selected from the group consisting of DOTA, DOTAM and PSC, and preferably a residue of KMe3,

[0393] (i) Xaa9 is a residue of an amino acid selected from the group consisting of Ala and Tyr,

[0394] (j) XaalO is a residue of an amino acid selected from the group consisting of Asp and Cya,

[0395] (k) Xaal l is a residue of an amino acid selected from the group consisting of Thi, Phe and Ocf, and preferably a residue of Thi,

[0396] (l) Cext is a moiety of formula (le), and

[0397] (m) Cterm is NH2.

[0398] Still more preferably, the compound is represented by the formula (1), wherein at least one, e.g., one, two, three, four, five, six, seven, eight, nine, ten, eleven, twelve or thirteen, of Xaal, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO, Xaal l, Cext and Cterm is / are defined as follows:

[0399] (a) Xaal is a residue of Pip,

[0400] (b) Xaa2 is a residue of Trp,

[0401] (c) Xaa3 is a residue of an amino acid selected from the group consisting of Penox, Asp and Cya, (d) Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, and preferably Xaa4 is a residue of Npg,

[0402] (e) Xaa5 is a residue of an amino acid selected from the group consisting of Aib, Ams, Thp, Ape, Lys(Z3), Orn(Z3) and Apc(Z3), wherein Z3is preferably selected from the group consisting of DOTA, DOTAM, PSC, DOTAGA, NOPO, NODAGA, BnTCMC, DOTAMGAM, PSCGA and NOTA, preferably Xaa5 is a residue of an amino acid selected from the group consisting of Apc(DOTA), Apc(DOTAM), Apc(PSC), Apc(DOTAGA), Apc(NOPO), Apc(NODAGA), Apc(PSCGA), Apc(BnTCMC), Apc(DOTAMGAM), Apc(PSCGA) and Apc(NOTA),

[0403] (f) Xaa6 is a residue of Asn,

[0404] (g) Xaa7 is a residue of an amino acid selected from the group consisting of 6Clw and Brw6,

[0405] (h) Xaa8 is a residue of KMe3,

[0406] (i) Xaa9 is a residue of an amino acid selected from the group consisting of Ala and Tyr,

[0407] (j) XaalO is a residue of an amino acid selected from the group consisting of Asp and Cya,

[0408] (k) Xaal l is a residue of Thi,

[0409] (l) Cext is a moiety of formula (le), and

[0410] (m) Cterm is NH2.

[0411] In an even more preferred embodiment, the compound is represented by the formula (1), wherein Xaa2, Xaa4, Xaa7 and Cext are defined as follows:

[0412] (b) Xaa2 is a residue of an amino acid selected from the group consisting of Trp, 7Clw, 7Mw, 7Fw, Bmw and Nmw, and preferably Xaa2 is a residue of Trp, and

[0413] (d) Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Mnpg, Leu, Nml, Hie, Phe, Gel, Mgel, Nle, NMB, Cba, Cpa, Cha, Cpg and Chg, preferably a residue of an amino acid selected from the group consisting of Npg, Leu, Mnpg, Nml and Chg, more preferably a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, and most preferably a residue of Npg, and

[0414] (g) Xaa7 is a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, and preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6, and (1) Cext is a moiety of formula (le).

[0415] Still more preferably, the compound is represented by the formula (1), wherein Xaa2, Xaa4, Xaa7 and Cext are defined as follows:

[0416] (b) Xaa2 is a residue of Trp, and

[0417] (d) Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Leu, Mnpg, Nml and Chg, preferably a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, and most preferably a residue of Npg, and

[0418] (g) Xaa7 is a residue of an amino acid selected from the group consisting of 6Clw and Brw6, and

[0419] (1) Cext is a moiety of formula (le).

[0420] In a preferred embodiment, the compound is represented by the formula (I), wherein

[0421] (a) Xaal - Xaa2 - Xaa3 - Xaa4 is a moiety selected from the group consisting of Pip-Trp- Asp-Npg, Pip-Trp-Cya-Npg, Pip-Trp-Glu-Npg, Pip-Trp-Val-Npg, Pip-Trp-Asn-Npg, Pip-Trp-Dmd-Npg, Pip-Trp-Asp-Leu, Pip-Trp-Cya-Leu, Pip-Trp-Glu-Leu, Pip-Trp- Val-Leu, Pip-Trp-Asn-Leu, Pip-Trp-Dmd-Leu, Pip-Trp-Asp-Chg, Pip-Trp-Cya-Chg, Pip-Trp-Glu-Chg, Pip-Trp-Val-Chg, Pip-Trp-Asn-Chg, Pip-Trp-Dmd-Chg, Pip-Trp- Asp-Nml, Pip-Trp-Cya-Nml, Pip-Trp-Glu-Nml, Pip-Trp-Val-Nml, Pip-Trp-Asn-Nml, Pip-Trp-Dmd-Nml, Pip-Trp-Asp-Mnpg, Pip-Trp-Cya-Mnpg, Pip-Trp-Glu-Mnpg, Pip- Trp-Val-Mnpg, Pip-Trp-Asn-Mnpg, Pip-Trp-Dmd-Mnpg, Nma-Trp-Asp-Npg, Nma- Trp-Cya-Npg, Nma-Trp-Glu-Npg, Nma-Trp-Val-Npg, Nma-Trp-Asn-Npg, Nma-Trp- Dmd-Npg, Nma-Trp-Asp-Leu, Nma-Trp-Cya-Leu, Nma-Trp-Glu-Leu, Nma-Trp-Val- Leu, Nma-Trp-Asn-Leu, Nma-Trp-Dmd-Leu, Nma-Trp-Asp-Chg, Nma-Trp-Cya-Chg, Nma-Trp-Glu-Chg, Nma-Trp-Val-Chg, Nma-Trp-Asn-Chg, Nma-Trp-Dmd-Chg, Nma- Trp-Asp-Nml, Nma-Trp-Cya-Nml, Nma-Trp-Glu-Nml, Nma-Trp-Val-Nml, Nma-Trp- Asn-Nml, Nma-Trp-Dmd-Nml, Nma-Trp-Asp-Mnpg, Nma-Trp-Cya-Mnpg, Nma-Trp- Glu-Mnpg, Nma-Trp-Val-Mnpg, Nma-Trp-Asn-Mnpg, Pip-Trp-Penox-Npg, Pip-Trp- Penox-Nml, Pip-Trp-Penox-Mnpg, Nma-Trp-Penox-Npg, Nma-Trp-Penox-Nml, Nma- Trp-Penox-Mnpg, Nmo(Me)-Trp-Cya-Mnpg, Nmg-Trp-Cya-Mnpg, Nmo(Me)-Trp- Cya-Nml, Nmg-Trp-Cya-Nml, Nmo(Me)-Trp-Asp-Mnpg, Nmg-Trp-Asp-Mnpg, Nmo(Me)-Trp-Asp-Nml, Nmg-Trp-Asp-Nml, Nmo(Me)-Trp-Asp-Npg, Nmg-Trp-Asp- Npg, Nmo(Me)-Trp-Penox-Npg, Nmg-Trp-Penox-Npg, Nmo(Me)-Trp-Penox-Nml, Nmg-Trp-Penox-Nml, Nmo(Me)-Trp-Penox-Mnpg, Nmg-Trp-Penox-Mnpg, Nmo(Me)-Trp-Cya-Npg, Nmg-Trp-Cya-Npg, Azp-Trp-Cya-Mnpg, Mor-Trp-Cya- Mnpg, Azp-Trp-Cya-Nml, Mor-Trp-Cya-Nml, Azp-Trp-Asp-Mnpg, Mor-Trp-Asp- Mnpg, Azp-Trp-Asp-Nml, Mor-Trp-Asp-Nml, Azp-Trp-Asp-Npg, Mor-Trp-Asp-Npg, Azp-Trp-Penox-Npg, Mor-Trp-Penox-Npg, Azp-Trp-Penox-Nml, Mor-Trp-Penox- Nml, Azp-Trp-Penox-Mnpg, Mor-Trp-Penox-Mnpg, Nma-Trp-Dmd-Mnpg, Azp-Trp- Cya-Npg, and Mor-Trp-Cya-Npg, and

[0422] (b) Xaa7 is preferably a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, more preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6.

[0423] In a more preferred embodiment, the compound is represented by the formula (I), wherein

[0424] (a) Xaal - Xaa2 - Xaa3 - Xaa4 is a moiety selected from the group consisting of Pip-Trp- Asp-Npg, Pip-Trp-Cya-Npg, Pip-Trp-Dmd-Npg, Pip-Trp-Asp-Nml, Pip-Trp-Cya-Nml, Pip-Trp-Dmd-Nml, Pip-Trp-Asp-Mnpg, Pip-Trp-Cya-Mnpg, Pip-Trp-Dmd-Mnpg, Pip- Trp-Penox-Npg, Pip-Trp-Penox-Nml, Pip-Trp-Penox-Mnpg, Nma-Trp-Penox-Npg, Nma-Trp-Penox-Nml, Nma-Trp-Penox-Mnpg, Nma-Trp-Asp-Npg, Nma-Trp-Cya- Npg, Nma-Trp-Dmd-Npg, Nma-Trp-Asp-Nml, Nma-Trp-Cya-Nml, Nma-Trp-Dmd- Nml, Nma-Trp-Asp-Mnpg, Nma-Trp-Cya-Mnpg and Nma-Trp-Dmd-Mnpg, and

[0425] (b) Xaa7 is preferably a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, more preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6.

[0426] Still more preferably, the compound is represented by the formula (I), wherein

[0427] (a) Xaal - Xaa2 - Xaa3 - Xaa4 is a moiety selected from the group consisting of Pip-Trp- Asp-Npg, Pip-Trp-Cya-Npg, Pip-Trp-Glu-Npg, Pip-Trp-Val-Npg, Pip-Trp-Asn-Npg, Pip-Trp-Dmd-Npg, Pip-Trp-Asp-Leu, Pip-Trp-Cya-Leu, Pip-Trp-Glu-Leu, Pip-Trp- Val-Leu, Pip-Trp-Asn-Leu, Pip-Trp-Dmd-Leu, Pip-Trp-Asp-Chg, Pip-Trp-Cya-Chg, Pip-Trp-Glu-Chg, Pip-Trp-Val-Chg, Pip-Trp-Asn-Chg, Pip-Trp-Dmd-Chg, Pip-Trp- Asp-Nml, Pip-Trp-Cya-Nml, Pip-Trp-Glu-Nml, Pip-Trp-Val-Nml, Pip-Trp-Asn-Nml, Pip-Trp-Dmd-Nml, Pip-Trp-Asp-Mnpg, Pip-Trp-Cya-Mnpg, Pip-Trp-Glu-Mnpg, Pip- Trp-Val-Mnpg, Pip-Trp-Asn-Mnpg, Pip-Trp-Dmd-Mnpg, Nma-Trp-Asp-Npg, Nma- Trp-Cya-Npg, Nma-Trp-Glu-Npg, Nma-Trp-Val-Npg, Nma-Trp-Asn-Npg, Nma-Trp- Dmd-Npg, Nma-Trp-Asp-Leu, Nma-Trp-Cya-Leu, Nma-Trp-Glu-Leu, Nma-Trp-Val- Leu, Nma-Trp-Asn-Leu, Nma-Trp-Dmd-Leu, Nma-Trp-Asp-Chg, Nma-Trp-Cya-Chg, Nma-Trp-Glu-Chg, Nma-Trp-Val-Chg, Nma-Trp-Asn-Chg, Nma-Trp-Dmd-Chg, Nma- Trp-Asp-Nml, Nma-Trp-Cya-Nml, Nma-Trp-Glu-Nml, Nma-Trp-Val-Nml, Nma-Trp- Asn-Nml, Nma-Trp-Dmd-Nml, Nma-Trp-Asp-Mnpg, Nma-Trp-Cya-Mnpg, Nma-Trp- Glu-Mnpg, Nma-Trp-Val-Mnpg, Nma-Trp-Asn-Mnpg, Pip-Trp-Penox-Npg, Pip-Trp- Penox-Nml, Pip-Trp-Penox-Mnpg, Nma-Trp-Penox-Npg, Nma-Trp-Penox-Nml, Nma- Trp-Penox-Mnpg, Nmo(Me)-Trp-Cya-Mnpg, Nmg-Trp-Cya-Mnpg, Nmo(Me)-Trp- Cya-Nml, Nmg-Trp-Cya-Nml, Nmo(Me)-Trp-Asp-Mnpg, Nmg-Trp-Asp-Mnpg, Nmo(Me)-Trp-Asp-Nml, Nmg-Trp-Asp-Nml, Nmo(Me)-Trp-Asp-Npg, Nmg-Trp-Asp- Npg, Nmo(Me)-Trp-Penox-Npg, Nmg-Trp-Penox-Npg, Nmo(Me)-Trp-Penox-Nml, Nmg-Trp-Penox-Nml, Nmo(Me)-Trp-Penox-Mnpg, Nmg-Trp-Penox-Mnpg, Nmo(Me)-Trp-Cya-Npg, Nmg-Trp-Cya-Npg, Azp-Trp-Cya-Mnpg, Mor-Trp-Cya- Mnpg, Azp-Trp-Cya-Nml, Mor-Trp-Cya-Nml, Azp-Trp-Asp-Mnpg, Mor-Trp-Asp- Mnpg, Azp-Trp-Asp-Nml, Mor-Trp-Asp-Nml, Azp-Trp-Asp-Npg, Mor-Trp-Asp-Npg, Azp-Trp-Penox-Npg, Mor-Trp-Penox-Npg, Azp-Trp-Penox-Nml, Mor-Trp-Penox- Nml, Azp-Trp-Penox-Mnpg, Mor-Trp-Penox-Mnpg, Nma-Trp-Dmd-Mnpg, Azp-Trp- Cya-Npg, and Mor-Trp-Cya-Npg, and

[0428] (b) Xaa7 is preferably a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, more preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6, and at least one, e.g., one, two, three, four, five, six, seven or eight, of Xaa5, Xaa6, Xaa8, Xaa9, XaalO, Xaal 1, Cext and Cterm is / are defined as follows:

[0429] (e) Xaa5 is a residue of a residue of an amino acid of formula (Via) or (VIb) as described above, preferably an amino acid selected from the group consisting of Aib, Ams, Thp, Ape, Lys(Z3), Orn(Z3) and Apc(Z3), wherein Z3is preferably selected from the group consisting of DOTA, DOTAM, PSC, DOTAGA, NOPO, NODAGA, BnTCMC, DOTAMGAM, PSCGA and NOTA, more preferably Xaa5 is a residue of an amino acid selected from the group consisting of Apc(DOTA), Apc(DOTAM), Apc(PSC), Apc(DOTAGA), Apc(NOPO), Apc(NODAGA), Apc(PSCGA), Apc(BnTCMC), Apc(DOTAMGAM), Apc(PSCGA) and Apc(NOTA), (f) Xaa6 is a residue of an amino acid of formula (Vila), (Vllb) or (Vile) as described above, preferably a residue of an L-amino acid of formula (Vlld) as described above, more preferably a residue of an amino acid selected from the group consisting of Ala, Asn, Asp, Cya, Lys, Lys(Me), Lys(Z4), Thr and Ser, most preferably Xaa6 is a residue of Asn,

[0430] (h) Xaa8 is a residue of an amino acid of formula (IX) as described above, preferably a residue of an amino acid selected from the group consisting of Lys(Me), KMe2, KMe3, Kzw, Egg, Arg(Me), Lys(Z5) and RMe2, more preferably a residue of KMe3,

[0431] (i) Xaa9 is a residue of an amino acid of formula (Xa) or (Xb) as described above, preferably a residue of an amino acid selected from the group consisting of Gly, Ala, Dab, Glu, Pro, Pcnf, Lys(Z6) and Tyr, more preferably a residue of an amino acid selected from the group consisting of Ala and Tyr,

[0432] (j) XaalO is a residue of formula (Xia) or (Xlb) as described above, preferably a residue of an amino acid selected from the group consisting of Asp, Cya, Glu, Lys, Thr and Ser, more preferably a residue of an amino acid selected from the group consisting of Asp and Cya,

[0433] (k) Xaal l is a residue of formula (Xlla) as described above, preferably a residue of an amino acid selected from the group consisting of Thi, Phe and Ocf, more preferably a residue of Thi,

[0434] (l) Cext is a moiety of formula (le), and

[0435] (m) Cterm is NH2.

[0436] Most preferably, the compound is represented by the formula (I), wherein

[0437] (a) Xaal - Xaa2 - Xaa3 - Xaa4 is a moiety selected from the group consisting of Pip-Trp- Asp-Npg, Pip-Trp-Cya-Npg, Pip-Trp-Dmd-Npg, Pip-Trp-Asp-Nml, Pip-Trp-Cya-Nml, Pip-Trp-Dmd-Nml, Pip-Trp-Asp-Mnpg, Pip-Trp-Cya-Mnpg, Pip-Trp-Dmd-Mnpg, Pip- Trp-Penox-Npg, Pip-Trp-Penox-Nml, Pip-Trp-Penox-Mnpg, Nma-Trp-Penox-Npg, Nma-Trp-Penox-Nml, Nma-Trp-Penox-Mnpg, Nma-Trp-Asp-Npg, Nma-Trp-Cya- Npg, Nma-Trp-Dmd-Npg, Nma-Trp-Asp-Nml, Nma-Trp-Cya-Nml, Nma-Trp-Dmd- Nml, Nma-Trp-Asp-Mnpg, Nma-Trp-Cya-Mnpg and Nma-Trp-Dmd-Mnpg, and (b) Xaa7 is preferably a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, more preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6, and at least one, e.g., one, two, three, four, five, six, seven or eight, of Xaa5, Xaa6, Xaa8, Xaa9, XaalO, Xaal 1, Cext and Cterm is / are defined as follows:

[0438] (e) Xaa5 is a residue of an amino acid of formula (Via) or (VIb) as described above, preferably a residue of an amino acid selected from the group consisting of Aib, Ams, Thp, Ape, Lys(Z3), Orn(Z3) and Apc(Z3), wherein Z3is preferably selected from the group consisting of DOTA, DOTAM, PSC, DOTAGA, NOPO, NOD AGA, BnTCMC, DOTAMGAM, PSCGA and NOTA, more preferably Xaa5 is a residue of an amino acid selected from the group consisting of Apc(DOTA), Apc(DOTAM), Apc(PSC), Apc(DOTAGA), Apc(NOPO), Apc(NODAGA), Apc(PSCGA), Apc(BnTCMC), Apc(DOTAMGAM), Apc(PSCGA) and Apc(NOTA),

[0439] (f) Xaa6 is a residue of an amino acid of formula (Vila), (Vllb) or (Vile) as described above, preferably a residue of an L-amino acid of formula (Vlld) as described above, more preferably a residue of an amino acid selected from the group consisting of Ala, Asn, Asp, Cya, Lys, Lys(Me), Lys(Z4), Thr and Ser, most preferably Xaa6 is a residue of Asn,

[0440] (h) Xaa8 is a residue of an amino acid of formula (IX) as described above, preferably a residue of an amino acid selected from the group consisting of Lys(Me), KMe2, KMe3, Kzw, Egg, Arg(Me), Lys(Z5) and RMe2, more preferably a residue of KMe3,

[0441] (i) Xaa9 is a residue of an amino acid of formula (Xa) or (Xb) as described above, preferably a residue of an amino acid selected from the group consisting of Gly, Ala, Dab, Glu, Pro, Pcnf, Lys(Z6) and Tyr, more preferably a residue of an amino acid selected from the group consisting of Ala and Tyr,

[0442] (j) XaalO is a residue of formula (Xia) or (Xlb) as described above, preferably a residue of an amino acid selected from the group consisting of Asp, Cya, Glu, Lys, Thr and Ser, more preferably a residue of an amino acid selected from the group consisting of Asp and Cya,

[0443] (k) Xaal l is a residue of formula (Xlla) as described above, preferably a residue of an amino acid selected from the group consisting of Thi, Phe and Ocf, more preferably a residue of Thi, (l) Cext is a moiety of formula (le), and

[0444] (m) Cterm is NH2.

[0445] 2.1. Group Z comprising an effector E and an optional linker L

[0446] In accordance with the present invention, the compound may comprise one or more of groups Z, wherein each group Z comprises an effector E (such as a chelator) and an optional linker L, the effector E being preferably selected from the group consisting of:

[0447] (a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and

[0448] (P) a chelator optionally comprising a chelated radionuclide; and

[0449] (y) a drug, preferably a cytotoxic drug; and

[0450] (5) an immune cell engaging effector, preferably recruiting and stimulating T cells, natural killer cells (NK cells) and / or phagocytotic cells.

[0451] If the compound comprises more than one group Z, the groups Z may be identical or different, and each effector E may be independently selected from the group consisting of (a), (P), (y) and (5).

[0452] In one embodiment, the compound of the invention comprises one or more of groups Z, wherein each group Z comprises an effector E (such as a chelator) and an optional linker L, each effector E being selected from the group consisting of:

[0453] (a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and

[0454] (P) a chelator optionally comprising a chelated radionuclide; and

[0455] (y) a drug, preferably a cytotoxic drug; and

[0456] (5) an immune cell engaging effector, preferably recruiting and stimulating T cells, natural killer cells (NK cells) and / or phagocytotic cells.

[0457] If the compound comprises more than one group Z, the groups Z may be identical or different, and each effector E is independently selected from the group consisting of (a), (P), (y) and (5). In a preferred embodiment, the compound of the invention comprises one or more groups Z, wherein each group Z (i.e., Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8, Z9) is independently a moiety represented by the following formula (XVa):

[0458] E-L-* (XVa) wherein,

[0459] * indicates covalent attachment to an attachment point (i.e., to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1),

[0460] L is a linker, and

[0461] E is selected from the group consisting of:

[0462] (a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and

[0463] (P) a chelator optionally comprising a chelated radionuclide; and

[0464] (y) a drug, preferably a cytotoxic drug; and

[0465] (5) an immune cell engaging effector, preferably recruiting and stimulating T cells, natural killer cells (NK cells) and / or phagocytotic cells.

[0466] In a more preferred embodiment, each group Z (i.e., Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8, Z9) comprises an effector E and an optional linker L, and each effector E represents (P) a chelator optionally comprising a chelated radionuclide.

[0467] 2.1.1 Linker L

[0468] As used herein, a linker is an element, moiety, or structure, which connects two parts of a molecule. In the present invention, the linker forms a covalent bond with the effector and the respective part of the compounds of the invention where the Z group is attached. A first functional group of the linker forming the bond with the effector (e.g., chelator) may in principle, be any chemical group, which is capable of forming a bond, preferably a covalent bond with the effector. In addition, the linker comprises a second functional group forming the bond, preferably a covalent bond with the part of the compound of the invention at the specified positions, where the Z group is attached. Such second functional group may in principle, be any chemical group, which is capable of forming such bond with said part of the compound of the invention at the specific positions where the Z group is attached. An important property or feature of a linker is that it spaces apart the effector (e.g., effector) from the peptide part of the compound of the invention. This is especially important in cases where the target binding ability of the peptide is compromised by the close proximity of the chelator. However, the overall linker length in its most extended conformer should not exceed 200 A, preferably not more than 150 A and most preferably not more than 100 A.

[0469] A further important feature or property of a linker is that it enables the attachment of the effector (e.g., chelator) to suitable positions of the peptide part of the compound of the invention.

[0470] In an embodiment, a residue of a dicarboxylic acid may represent a building block for a linker. Dicarboxylic acid-based linkers are typically used to enable the attachment of an effector to an amino group comprised in the side chain of an amino acid residue of the compound of the invention. Such amino side chain provides an amino group as functional group to which one of the at least two carboxyl groups provided by the dicarboxylic acid building block is covalently attached forming an amide linkage. The effector provides an amino group as functional group to which another of the at least two carboxyl groups provided by the dicarboxylic acid building block is covalently attached forming an amide linkage, too. The very kind of dicarboxylic acid used as building block for a linker is dependent on the nature of the effector and the attachment site on the compound of the invention, and more specifically any functional group available at or provided by the effector, respectively, which is reacted with one of the at least two carboxyl groups of the dicarboxylic acid building block.

[0471] Preferred building blocks are dicarboxylic acids, which are selected from bluiding blocks of the following formulae (Linl), (Lin2) and (Lin3):

[0472] More preferred dicarboxylic acid building blocks of formula (Linl) are malonic acid, succinic acid, glutaric acid, adipic acid, wherein the two carboxylic acid groups are attached to ends of the aliphatic chain; of formula (Lin2) are phthalic acid, terephthalic acid, isophthalic acid, and of formula (Lin3) is 2-, 3- or 4-carboxy-phenyl acetic acid. A most preferred dicarboxylic acid building block is glutaric acid (Glutar).

[0473] In an embodiment, a residue of a diamine represents a building block for a linker. Diamine based linkers are used to enable the attachment of an effector (e.g., a chelator) to the C-terminal carboxyl group of the compound of the invention or to a carboxyl group comprised in the side chain of an amino acid residue of the compound of the invention. Such carboxyl-containing C -terminal group or carboxyl-containing side chain provides a carboxyl group as functional group to which one of the at least two amino groups provided by the diamine is covalently attached forming an amide linkage. The effector provides a carboxyl group as functional group to which another of the at least two amino groups provided by the diamine building block is covalently attached forming an amide linkage, too. The very kind of diamine used as building block for a linker is dependent on the nature of the effector (e.g., chelator) and the attachment site on the compound of the invention, and more specifically any functional group available at or provided by the effector, respectively, which is reacted with one of the at least two amino groups of the diamine building block.

[0474] Preferred building blocks are diamines, which are selected from building blocks of the following formulae (Lin4), (Lin5), (Lin6), (Lin7) and (Lin8):

[0475] More preferred diamine building blocks are ethylenediamine (en), 1,4-diaminobutane, 1,5-diaminopentane (Ape), 1,6-diaminohexane, 4, 7, 10-tri oxa- 1,13 -tridecanediamine, 1,3- dazetine, piperazine (PP), 1,3-diazinane, o-, m- and p-phenylenediamine, 4-aminobenzylamine, and l,4-bis(aminomethyl)benzene. Most preferred diamino building blocks are 1,5- diaminepentane (Ape), ethylenediamine (en), and piperazine (PP).

[0476] In an embodiment, a residue of an amino acid represents the building block for a linker. Amino acid-based linkers are used to enable the attachment of an effector (e.g., chelator) to an amino group comprised in the side chain of an amino acid residue or to the C-terminal carboxylic acid moiety of the compound of the invention. Such amino-containing side chain of the compound of the invention provides an amino group to which the carboxyl group of the amino acid linker is attached covalently by formation of an amide bond. The effector provides a carboxyl group as functional group, to which the amino group of the amino acid linker is attached covalently by formation of an amide bond. Furthermore, to the amino group of the linker, the carboxyl group of another linker can be attached covalently by formation of an amide bond, which preferably is an a-amino acid linker. As an alternative such C-terminal carboxyl group of the compound of the invention provides a carboxyl group to which the amino group of the amino acid linker is attached covalently by formation of an amide bond. In this case, the effector (e.g., chelator) provides an amino group as functional group to which the carboxyl group of the linker is attached covalently by formation of an amide bond. Furthermore, to the carboxyl group of the linker, the amino group of another linker can be attached covalently by formation of an amide bond, which preferably is an a-amino acid linker. It is within the present invention that two or more amino acid linkers can be covalently attached to each other, forming a peptidic linker with an amino group and a carboxyl group which equally well functions as an amino acid-based linker.

[0477] Preferred building blocks are amino acids, which are selected from amino acids of any of the following formulae (Lin9), (LinlO), (Linl l), (Linl2) and (Linl3):

[0478] It is within the present invention that such amino acid linker is not further substituted. It is, however, also within the present invention that such amino acid linker is further substituted; preferably such substitution is CO-NH2 and / or Ac-NH-.

[0479] Representative amino acids of the formula Lin8 inlcude glycine (Gly), P-alanine (Bal), y- aminobutyric acid (Gab), 5-amino-pentanoic acid, 6-amino-hexanoic acid and homologs thereof with up to 10 CH2 groups.

[0480] Representative amino acids of the formula Lin 10 include N-m ethylglycine (Nmg), N-methyl- P-alanine, A-methyl-gamma-aminobutyric acid, N-methyl-5-amino-pentanoic acid, N-methyl- 6-amino-hexanoic acid, and homologs thereof with up to 10 CH2 groups.

[0481] Representative amino acids of the formula Linl l inlcude 3 -aminomethyl-benzoic acid, 4-aminom ethyl-benzoic acid, anthranilic acid, 3 -amino-benzoic acid, and 4-amino-benzoic acid.

[0482] Representative amino acids of the formula Lin 12 include 4-carboxymethyl-piperidine (Cmp), 3 -piperidinecarboxylic acid (nipecotic acid, Rni), and 4-piperidinecarboxylic acid (isonipecotic acid, Inp). Representative amino acids of the formula Lin 13 include (4-aminopiperidin-l-yl)acetic acid (APAc), 2-(piperazin-l-yl)-acetic acid (PPAc), and 4-(aminomethyl)cyclohexanecarboxylic acid (tranexamic acid, 4Amc).

[0483] It will be appreciated by a person skilled in the art that in case of amino acids with stereogenic centers all stereoisomeric forms may be used as such a linker.

[0484] In a further embodiment, the amino acid is an amino acid which contains, preferably as a backbone, a polyether. Preferably such polyether is polyethylene glycol and consists of up to 30 monomer (ethylene oxide) units. Preferably, an amino acid comprising such polyether shows an increase in hydrophilicity compared to an amino acid not comprising such polyether. If incorporated as a linker the result is typically an increase in hydrophilicity which may, in turn, improve the solubility of the compound of the invention. A preferred embodiment of this kind of amino acid is depicted by the following formula Linl4, wherein it will be acknowledged that such amino acid may comprise 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 ethylene oxide units: 0-12 (Lin 14)

[0485] Preferred ethylene glycol containing amino acids are Ttds, O2Oc, PEG6, and PEG12.

[0486] In a further embodiment, a residue of an alpha amino acid represents a building block for a linker. Alpha amino acid-based linkers are used to enable the attachment of an effector to an amino group comprised in the side chain of an amino acid residue of the compound (peptide) of the invention and / or to the C-terminal carboxyl group of the compound (peptide) of the invention. Thereby, up to two effectors can be attached to one site of the compound of the invention. Such amino-containing side chain provides an amino group to which one of the one or more carboxyl groups provided by the alpha amino acid building block is covalently attached by formation of an amide linkage. Such C-terminal carboxyl group provides a carboxyl group as funtional group to which one of the one or more amino groups provided by the alpha amino acid covalently attached by formation of an amide linkage. In such cases, wherein the alpha amino acid has more than one amino group, the effector (e.g., chelator) provides a carboxylic group as functional group, which is attached covalently to said amino group of the alpha amino acid by an amide linkage, while the other one of the amino groups is used as a linkage to the compound of the invention. In such cases, wherein the alpha amino acid has more than one carboxyl groups, the effector (e.g., chelator) provides an amino group as functional group, which is attached covalently to said carboxyl group of the alpha amino acid by an amide linkage, while the other one of the carboxyl groups is used as a linkage to the compound of the invention. It is within the present invention that when an alpha amino acid building block contains multiple amino groups, that the carboxyl group and any of the amino groups can be used to mediate linkages to both the effector and the compound (peptide) of the invention while the other amino groups which are not engaged in amide linkages can fine-tune the physicochemical properties of the compound. In one embodiment, such amino groups (which are not engaged in amide linkages) can be modified by up to three methyl groups. It is also within the present invention that when an alpha amino acid building block contains multiple carboxyl groups, that the amino group and any of the carboxyl groups can be used to mediate linkages to both the effector and the compound (peptide) of the invention while the other carboxyl groups which are not engaged in amide linkages can fine tune the physicochemical properties of the compound. In one embodiment, such carboxyl groups (which are not engaged in amide linkages) can optionally be replaced by carboxamide groups or sulfonate groups.

[0487] Preferred building blocks are alpha amino acids, which are selected from building blocks of the following formula (Lin 15), (Lin 16), (Lin 17) or (Lin 18):

[0488] More preferred alpha amino acids building blocks are di-amino-propionic acid (Dap), di-amino- butyric acid (Dab), ornithine (Orn), lysine (Lys), aspartic acid, and glutamic acid. The most preferred alpha amino acid building blocks are lysine and glutamic acid. It will be appreciated by a person skilled in the art that, in case of alpha amino acids with stereogenic centers, all stereoisomeric forms may be used as such a linker. The use of a linker usually follows a purpose. In some circumstances, a linker can be used to space apart moieties in a compound, such as a larger moiety from a bioactive molecule, in order to retain high bioactivity. In other circumstances, the introduction of a linker allows for tuning physicochemical properties of the compound by introducting polarity and / or multiple charges. In certain circumstances, the site of attachment within the sequence of the compound of the invention and the chemical nature of the effector may necessitate the use of a linker. Further, in certain circumstances, it might be desirable to combine the effector and compound without the need of a linker. Compounds of the present invention where the effector is directly attached to the side chain of an amino acid residue by forming an amide bond typically perform excellently without the use of any dedicated linker.

[0489] In a preferred embodiment, the compound of the invention comprises one or more groups Z, wherein each group Z (i.e., Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8, Z9) is independently a moiety represented by the following formula (XVb):

[0490] E-L-* (XVb) wherein,

[0491] * indicates covalent attachment to an attachment point (i.e., to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1),

[0492] E is selected from the group consisting of:

[0493] (a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and

[0494] (P) a chelator optionally comprising a chelated radionuclide; and

[0495] (y) a drug, preferably a cytotoxic drug; and

[0496] (5) an immune cell engaging effector, preferably recruiting and stimulating T cells, natural killer cells (NK cells) and / or phagocytotic cells; and

[0497] L is a linker moiety represented by any one of the formulae (XVIIa) to (XVIIy): wherein, nl and n24 are each independently 1 to 5, n2, n3, n4 and nl2 are each independently 0 to 2, n5, n6 and n29 are each independently 1 to 10, n7 and n8 are each independently 0 to 4, n9, nl3, nl4, nl5, nl8 n20, n21, n25 and n26 are each independently 1 or 2, n 10 and ni l are each independently 0 or 1, nl6 is 0 to 12, nl7, nl9, n22, n27 and n28 are each independently 1 to 4, n23 is 2 to 4,

[0498] XL1, XL2, XL3, XL4, XL5, XL8and XL9are each independently =CH- or =N-, XL6, XL7, XL1° and XL11are each independently -OH or -NH2,

[0499] RL1, RL2, RL3, RL4, RL5, RL6, RL7, RL8, RL9, RL1°, RL12and RL12are each independently -H or a methyl group,

[0500] * indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and

[0501] **’ indicates covalent attachment to E.

[0502] 2.1.2 Radionuclide

[0503] It will be recognized by a person skilled in the art that when a radioactive nuclide is present in the compound of the invention, the radioactive nuclide is selected taking into consideration the disease to be treated and / or the disease to be diagnosed, respectively, and / or the particularities of the patient and / or patient group, respectively, to be treated and / or to be diagnosed, respectively.

[0504] In the present invention, the “radioactive nuclide” may also be referred to as “radionuclide” and vice versa. Radioactive decay is the process by which an atomic nucleus of an unstable atom loses energy by emitting ionizing particles (ionizing radiation). There are different types of radioactive decay. A decay, or loss of energy, results when an atom with one type of nucleus, called the parent radionuclide, transforms to an atom with a nucleus in a different state, or to a different nucleus containing different numbers of protons and neutrons. Either of these products is named the daughter nuclide. In some decays the parent and daughter are different chemical elements, and thus the decay process results in nuclear transmutation (creation of an atom of a new element). For example, the radioactive decay can be alpha decay, beta decay, and gamma decay. Alpha decay occurs when the nucleus ejects an alpha particle (helium nucleus). This is the most common process of emitting nucleons, but in rarer types of decays, nuclei can eject protons, or specific nuclei of other elements (in the process called cluster decay). Beta decay occurs when the nucleus emits an electron (P'-decay) or positron (P+-decay) and a type of neutrino, in a process that changes a proton to a neutron or the other way around. By contrast, there exist radioactive decay processes that do not result in transmutation. The energy of an excited nucleus may be emitted as a gamma ray in gamma decay, or used to eject an orbital electron by interaction with the excited nucleus in a process called internal conversion, or used to absorb an inner atomic electron from the electron shell whereby the change of a nuclear proton to neutron causes the emission of an electron neutrino in a process called electron capture (EC), or may be emitted without changing its number of proton and neutrons in a process called isomeric transition (IT). Another form of radioactive decay, the spontaneous fission (SF), is found only in very heavy chemical elements resulting in a spontaneous breakdown into smaller nuclei and a few isolated nuclear particles.

[0505] In a preferred embodiment of the present invention, the radionuclide can be used for labeling of the compound of the invention.

[0506] In an embodiment of the present invention, the radionuclide is suitable for complexing with a chelator, leading to a radionuclide chelate complex.

[0507] In a further embodiment, one or more atoms of the compound of the invention are of nonnatural isotopic composition, preferably these atoms are radionuclides; more preferably radionuclides of carbon, oxygen, nitrogen, sulfur, phosphorus and halogens: These radioactive atoms are typically part of amino acids, in some case halogen containing amino acids, and / or building blocks and in some cases halogenated building blocks each of the compound of the invention.

[0508] In a preferred embodiment of the present invention, the radionuclide has a half-life that allows for diagnostic and / or therapeutic medical use. Specifically, the half-life is between 1 min and 100 days.

[0509] In a preferred embodiment of the present invention, the radionuclide has a decay energy that allows for diagnostic and / or therapeutic medical use. Specifically, for y-emitting isotopes, the decay energy is between 0.004 and 10 MeV, preferably between 0.05 and 4 MeV, for diagnostic use. For positron-emitting isotopes, the mean decay energy is between 0.6 and 13 MeV, preferably between 1 and 6 MeV, for diagnostic use. For P'-emitting isotopes, the mean decay energy is between 0.02 and 3 MeV, preferably between 0.1 and 1 MeV, for therapeutic use. For a-emitting isotopes, the decay energy is between 3 and 10 MeV, preferably between 3.9 and 7 MeV, for therapeutic use. In a preferred embodiment of the present invention, the radionuclide is industrially produced for medical use. Specifically, the radionuclide is available in GMP quality.

[0510] In a preferred embodiment of the present invention, the daughter nuclide(s) after radioactive decay of the radionuclide are compatible with the diagnostic and / or therapeutic medical use. Furthermore, the daughter nuclides are either stable or further decay in a way that does not interfere with or even support the diagnostic and / or therapeutic medical use. Representative radionuclides which may be used in connection with the present invention are well known to the person skilled in the art and include, but are not limited, to the following ones:nC,13N,18F,24Na,28Mg,31Si,32P,33P,38S,34mCl,38C1,39C1,37Ar,41Ar,44Ar,42K,43K,44K,45K,47Ca,43Sc,44Sc,44mSc,47Sc,48Sc,49Sc,45Ti,47V,48V,48Cr,49Cr,51Cr,51Mn,52Mn,52mMn,56Mn,52Fe,59Fe,55Co,61Co,62mCo,56Ni,57Ni,65Ni,66Ni,60Cu,61Cu,64Cu,67Cu,62Zn,63Zn,69Zn,69mZn,71mZn,72Zn,65Ga,66Ga,67Ga,68Ga,70Ga,72Ga,73Ga,66Ge,67Ge,69Ge,71Ge,75Ge,77Ge,78Ge,69As,70As,71As,72As,74As,76As,77As,78As,70Se,72Se,73Se,73mSe,81Se,81mSe,83Se,74Br,74mBr,

[0511] 75Br,76Br,77Br,80Br,80mBr,82Br,83Br,84Br,74Kr,76Kr,77Kr,79Kr,85Kr,87Kr,88Kr,78Rb,79Rb,

[0512] 81Rb,82Rb,84Rb,84mRb,86Rb,88Rb,89Rb,80Sr,81Sr,82Sr,83Sr,85mSr,87Sr,91Sr,92Sr,84Y,85Y,

[0513] 89mNb, ^0Nb, 92Nb, 95Nb, 95mNb, 96^ 97^ 98mNb, 101Mo, 102Mo, 90^ 91MQ, 93,^^ 99^ i°iTc,104TC,93TC,93mTc,94TC,94mTc,95TC,96TC, "mTc,103Ru,105Ru,94Ru,95Ru,97Ru,100Rh,101mRh,105Rh,106mRh,107Rh,97Rh,97mRh, "Rh, "mRh,100Pd,101Pd,103Pd,109Pd,mPd,l l lmPd,112Pd,98Pd, "Pd,101Ag,103Ag,104Ag,104mAg,105Ag,106Ag,106mAg,1 HAg,112Ag,113Ag,115Ag,104Cd,105Cd,107Cd,mCd,115Cd,115mCd,117Cd,117mCd,118Cd,107In,108mIn,109In,110In,110mIn,mIn,112In,113In,114mIn,115mIn,116mIn,117In,117mIn,119mIn,108Sn,109Sn,110Sn,mSn,117Sn,

[0514] 121Sn,123mSn,125Sn,127Sn,128Sn,115Sb,116Sb,116mSb,117Sb,118mSb,119Sb,120Sb,120mSb,122Sb,126Sb,126mSb,127Sb,128Sb,128mSb,129Sb,129mSb,130Sb,131Sb,114Te,116Te,117Te,118Te,119Te.

[0515] 119mTe121T127T129^ 129mTe131T131mTe132?133?133mT134Te118j 119j 120j 120mj

[0516] 121j 123j 124j 125j 126j 128j 130j 131j 132j 132mj 133j 134j 135j ! 20ye121^122Xe123Xe125Xe127Xe,133Xe,133mXe,135Xe,135mXe,138Xe,125Cs,127Cs,129Cs,130Cs,131Cs,132Cs,134Cs,135Cs,136Cs,138Cs,124Ba,126Ba,127Ba,128Ba,129Ba,129mBa,131Ba,131mBa,133Ba,135Ba,139Ba,140Ba,141Ba,142Ba,129La,131La,132La,133La,135La,140La,141La,142La,143La,130Ce,132Ce,133Ce,133mCe,134Ce,135Ce,137Ce,137mCe,141Ce,143Ce,146Ce,134Pr,134mPr,136Pr,137Pr,138mPr,139Pr,

[0517] 142Pr,143Pr,144Pr,145Pr,146Pr,147Pr,135Nd,136Nd,137Nd,138Nd,139Nd,139mNd,140Nd,141Nd,147Nd,149Nd,151Nd,152Nd,141Pm,148Pm,148mPrn,149Pm,150Pm,151Pm,140Sm,141Sm,141mSrn,142Sm,153Sm,155Sm,156Sm,145Eu,146Eu,147Eu,150Eu,152mEu,154Eu,156Eu,157Eu,158Eu,159Eu,145Gd,146Gd,147Gd,149Gd,159Gd,147Tb,148Tb,149Tb,150Tb,151Tb,152Tb,153Tb,154Tb,154mTb,155Tb,156Tb,156mTb,161Tb,163Tb,151Dy,152Dy,153Dy,155Dy,157Dy,165Dy,166Dy,154Ho,155Ho,156HO,157HO,158mHo,159HO,161HO,162HO,162mHo,164Ho,164mHo,166Ho,167Ho,156Er,157Er,158Er,159Er,160Er,161Er,163Er,165Er,169Er,171Er,172Er,161Tm,162Tm,163Tm,165Tm,166Tm,167Tm,172Tm,173Tm,175Tm,162Yb,163Yb,164Yb,166Yb,167Yb,169Yb,175Yb,177Yb,178Yb,167Lu,169Lu,170LU,171LU,172LU,176mLu,177LU,178LU,178mLu,179Lu,168Hf,170Hf,173Hf,177mHf,179mHf,180mHf,181Hf,182mHf,183Hf,184Hf,172Ta,173Ta,174Ta,175Ta,176Ta,177Ta,178Ta,180Ta,182mTa,183Ta,184Ta,185Ta,186Ta,174W,175W,177W,178W,179W,187W,190W,177Re,178Re,179Re,181Re,182Re,182mRe,184Re,186Re,188Re,188mRe,189Re,190mRe,180Os,1810s,1820s,1830s,183mOs,1910s,1930s, 196QS 182jj. 183jj. 184jj. 185jj. 186jj. 186mjj. 187jj. 188jj. 189jj. 190jj. 194jj. 195jj. 195mjj. 196mjj. 184p^186Pt,187Pt,188Pt,189Pt,191Pt,195Pt,197Pt,197mPt,199Pt,200Pt,202Pt,186Au,190Au,191Au,192Au, 203pb 204pfo 209pfo 211pfo 212pfo 214pfo 200gj 200mgj 201gj 202gj 203gj 204gj 205gj 206gj 210gj 212Bi, 212mBi, 213Bi214^ 200pQ, 201pQ, 202pQ, 203pQ, 204pQ, 205pQ, 206pQ, 207pQ, 205^ 206^ 207^208At,209At,210At,211At,208Rn,209Rn,210Rn,211Rn,212Rn,221Rn,222Rn,223Rn,212Fr,222Fr,223Fr,223Ra,224Ra,225Ra,227Ra,230Ra,224Ac,225Ac,226Ac,228Ac,229Ac,226Th,227Th,231Th,233Th,234Th,236Th,227Pa,228Pa,229Pa,230Pa,232Pa,233Pa,234Pa,235Pa,229U,230U,231U,237U,239U,240U,242U,231Np,232Np,233Np,234Np,236mNp,238Np,239Np,240Np,241Np,232Pu,235Pu,237Pu,243Pu,245Pu,246Pu,235Am,237Am,238Am,239Am,240Am,242Am,244Am,244mArn,245Am,246Am,246mArn,247Am,239Cm,240Cm,241Cm,251Cm,245Bk,246Bk,248Bk,250Bk,251Bk,244Cf,245Cf,246Cf,247Cf,253Cf,255Cf,249ES,250ES,250mEs,251ES,253ES,254mEs,255Es,256mEs,250Fm,251Fm,252Fm,254Fm,255Fm,255Md,256Md,257Md,259No. Their properties are described in more detail, for instance, in Nuclear Data Sheets (Elsevier, Amsterdam, NL).

[0518] In an embodiment of the present invention, the radionuclide is used for diagnosis (in this context, the radionuclide may also be referred to as “diagnostically active radionuclide”). Preferably, the radionuclide is selected from the group comprising43Sc,44Sc,51Mn,52Mn,64Cu,67Ga,68Ga,86Y,89Zr,94mTc, "mTc,mIn,149Tb,152Tb,155Tb,161Tb,177Lu,2O1T1,203Pb,18F for example as A1-18F,76Br,77Br,123I,124I, and125I. More preferably, the radionuclide is selected from the group comprising A1-18F,44Sc,64Cu,67Ga,68Ga,86Y,89Zr, "mTc,U 1ln,203Pb. Even more preferably, the radionuclide is64Cu,68Ga,U 1ln and203Pb. It will, however, also be acknowledged by a person skilled in the art that the use of said radionuclide is not limited to diagnostic purposes, but also encompasses their use in therapy and theragnostics when conjugated to the compound of the invention. In an embodiment of the present invention, the radionuclide is used for therapy (in this context, the radionuclide may also be referred to as “therapeutically active radionuclide”). Preferably, the radionuclide is selected from the group comprising47Sc,67Cu,89Sr,90Y,i nIn,153Sm,149Tb,161Tb,177LU,186Re,188Re,212Pb,213Bi,223Ra,225Ac,226Th,227Th,125I131I, and211At. More preferably, the radioactive isotope is selected from the group comprising67Cu,90Y,149Tb,161Tb,177LU,212Pb,213Bi,225Ac,227Th. Even more preferably, the radionuclide is selected from the group comprising90Y,177Lu,212Pb and225Ac. It will, however, also be acknowledged by a person skilled in the art that the use of said radionuclide is not limited to therapeutic purposes, but also encompasses their use in diagnostic and theragnostics when conjugated to the compound of the invention.

[0519] In a preferred embodiment, the radionuclide is selected from:

[0520] (i) a diagnostically active radionuclide selected from the group consisting of A1-18F,43Sc, 44Sc,51Mn,52Mn,64Cu,67Ga,68Ga,86Y,89Zr,94mTc, "mTc,mIn,149Tb,152Tb,155Tb, 161Tb,177LU,2O1T1,203Pb,18F,76Br,77Br,123I,124I, and125I, preferably from the group consisting of A1-18F,44Sc,64Cu,67Ga,68Ga,86Y,89Zr, "mTc,i nIn,203Pb, and more preferably from the group consisting of64Cu,68Ga,i nIn and203Pb; and / or

[0521] (ii) a therapeutically active radionuclide selected from the group consisting of47Sc,67Cu, 89Sr,90Y,mIn,153Sm,149Tb,161Tb,177Lu,186Re,188Re,212Pb,213Bi,223Ra,225Ac,226Th, 227Th,1251,131I, and211At, preferably from the group consisting of67Cu,90Y,149Tb,161Tb, 177LU,212Pb,213Bi,225Ac,227Th, and more preferably from the group consisting of90Y, 177LU,212Pb and225Ac.

[0522] 2.1.3 Effector E

[0523] 2, 1 ,3, 1 Chelator

[0524] In an embodiment, the compound of the invention comprises, as the effector, a chelator. The chelator is part of the compound of the invention, whereby the chelator is either directly or indirectly, such as by a linker, attached to the rest of the compound of the invention. A preferred chelator is a chelator which forms metal chelates and preferably comprises at least one radionuclide. The at least one radionuclide is useful in or suitable for diagnostic and / or therapeutic and / or theranostic purposes, and is preferably useful in or suitable for imaging and / or radiotherapy. Chelators in principle useful in and / or suitable for the present invention including diagnosis and / or therapy of a disease are known to the person skilled in the art. A variety of respective chelators is available and has been reviewed, e.g., by Banerjee et al. (Banerjee, et al., Dalton Trans, 2005, 24: 3886), and references therein (Price, et al., Chem Soc Rev, 2014, 43: 260; Wadas, et al. , Chem Rev, 2010, 110: 2858). Such chelators include, but are not limited to linear, cyclic, macrocyclic, tetrapyridine, N3S, N2S2 and N4 chelators as disclosed in US 5,367,080 A, US 5,364,613 A, US, 5,021,556 A, US 5,075,099 A and US 5,886,142 A.

[0525] Representative chelators and their derivatives including any bifunctional versions that can be attached to the compound of the invention include, but are not limited to, the examples listed in Table 6.

[0526] Table 6: Examples of chelators with their corresponding chemical names and exemplary reference of their disclosure. s) Kostelnik et aL, Chem. Rev. 2019, 119(2), 902 t) Li et al., Pharmaceutics 2023, 75, 414 u) McAuley, et al., Can. J. Chem. 1989, 67, 1657 v) Maecke et al. in: PET Chemistry (Springer Berlin Heidelberg) 2007, 64, 215 w) Mazzi et al. in: Technetium-99m pharmaceuticals (Berlin: Springer) 2007, 7-58 x) McDonagh et al. , Inorg. Chem. 2021, 60, 10030 y) Poty et al, ChemMedChem 2015, 10(9), 1475 z) AlHokbany et al. , EJNMMI Radiopharm Chem. 2022, 7(19) aa) Urbanovsky et al., RSC Adv. 2020, 10, 21329 bb) Egorova et al. , Molecules 2022, 27, 3115 cc) Straathof et al. , Molecules 2021, 26, 4603 dd) Yu et al, J. Inorg. Biochem. 2016, 154, 89 ee) Lozza et al, Front. Oncol. 2013, 3, 247 ff) Heath et al., Nutrients 2013, 5(8), 2836 gg) Wadas et al, Chem. Rev. 2010, 110(5), 2858 hh) Stimmel et al, Bioconjugate Chem. 1995, 6(2), 219 ii) Yokel et al., J. Pharm. Sci. 2000, 89(4), 545 jj) Woodin et al., Eur. J. Inorg. Chem. 2005, 4829 kk) Lima et al., Inorg. Chem. 2014, 53(10), 5269

[0527] 11) Cai et al., J. Label Compd. Radiopharm 2014, 57, 224 mm) Guo et al., JHematol Oncol. 2016, 9, 98 nn) Kanchi et al., Arab. J. Chem. 2014, 7(1), 11 oo) Feiner et al, Cancers 2021, 13, 4466 pp) Lyczko et al. , Polyhedron 2020, 192, 114822 qq) Chang et al., Dalton Trans., 2013, 42, 6397 rr) Serda et al, PLOS ONE 2014, 9(10), el l0291 ss) Ingham et al., Inorg. Chem. 2022, 61(24), 9119 tt) McBride et al., EJNMMI Research 2013, 3(36)

[0528] The diagnostic and / or therapeutic use of some of the above chelators is described in the prior art. For example, 2-hydrazino nicotinamide (HYNIC) has been widely used in the presence of a coligand for incorporation of "mTc andl 86J 88Re (Schwartz, etal., Bioconjug Chem, 1991, 2: 333; Babich, et al., J Nucl Med, 1993, 34'. 1964; Babich, et al., Nucl Med Biol, 1995, 22: 25); DTPA is used in Octreoscan® for complexingn iIn and several modifications are described in the literature (Li, et aL, Nucl Med Biol, 2001, 28: 145; Brechbiel, et al. , Bioconjug Chem, 1991, 2: 187); DOTA-type chelators for radiotherapy applications are described by Tweedie et al. (US Pat 4,885,363); other polyaza macrocycles for chelating trivalent isotopes metals are described by Eisenwiener et al. (Eisenwiener, et al. , Bioconjug Chem, 2002, 13: 530); and N4- chelators such as a "mTc-N4-chelator have been used for peptide labeling in the case of minigastrin for targeting CCK-2 receptors (Nock, et al, J Nucl Med, 2005, 46: 1727).

[0529] In preferred embodiments, the chelator used in the compound of the invention is selected from the group, but not limited to, comprising DOTA, DOTAGA, DOTAM, Crown, DOTP, NOTA, NODAGA, NODA-MPAA, HBED, TETA, CB-TE2A, DTPA, CHX-A”-DTPA, DFO, Macropa, HOPO ligand platform, TRAP, THP, AAZTA, DATA, NOPO, PCTA, PSC, sarcophagine, FSC, DEPA, DE4TA, NETA, NE3TA, ELoctapa, ELCHXoctapa, ELpypa, H4py4pa, HYNIC, NxS4-x (N4, N2S2, N3S),99mTc(CO)3-chelators and their analogs. Preferably, the chelator additionally comprises one or more functional groups or functionalities allowing for attachment to the compound of the invention. The chemical structures of these chelators and the residues resulting from preferred functionalization and / or conjugation (exemplifying possible attachment points) are shown in Table 7 below.

[0530] Table 7: Chemical structures of chelators and preferred residues.

[0531]

[0532]

[0533] 'I' as disclosed in: Mazzi et al. in: Technetium-99m pharmaceuticals (Berlin: Springer) 2007, 7-58 as disclosed in: Santos et al., Molecules 2021, 26(22), 6997 wherein X* is selected from the group consisting of (a) -NH- and (b) -NH-C(S)-, wherein in (a) the N atom is the attachment point of both the chelator and the rest of the compound of the invention and in (b) the N atom is the attachment point of the chelator and the C atom of the thiocarbonyl group is the attachment point of the rest of the compound of the invention.

[0534] In a more preferred embodiment, the chelator is selected from the group consisting of DOTA, DOTAGA, DOTAM, Crown, NOTA, NODAGA, NODA-MPAA, CB-TE2A, CHX-A”- DTPA, DFO, Macropa, THP, AAZTA, NOPO, PCTA, PSC, sarcophagine, NETA, EUCHXoctapa, EUpypa and N4, preferably from the group consisting of DOTA, DOTAGA, DOTAM, NOTA, NODAGA, Macropa, Crown, NOPO, PCTA, PSC and N4, more preferably from the group consisting of DOTA, DOTAM, Macropa, NOTA, PSC and NODAGA.

[0535] Most preferably, the chelator is DOTA.

[0536] Preferably, the chelator additionally comprises one or more functional groups or functionalities allowing attachment to the compounds of the invention.

[0537] It will be acknowledged by the persons skilled in the art that the chelator, in principle, may be used regardless of whether the compound of the invention is used in or suitable for diagnosis or therapy (as described, for example, in international patent application WO 2009 / 109332 Al).

[0538] It will be further acknowledged by the persons skilled in the art that the presence of a chelator in the compound of the invention includes, if not stated otherwise, the possibility that the chelator is complexed to any metal complex partner, i.e., any metal which, in principle, can be complexed by the chelator. An explicitly mentioned chelator of a compound of the invention or the general term chelator in connection with the compound of the invention refers either to the uncomplexed chelator as such or to the chelator to which any metal complex partner is bound, wherein the metal complex partner is any radioactive or non-radioactive metal complex partner. Preferably the chelator-metal complex, i.e., the chelator to which the metal complex partner is bound, is a stable chelator-metal complex.

[0539] Non-radioactive chelator-metal complexes have several applications, e.g., for assessing properties like stability or activity, which are otherwise difficult to determine. One aspect is that cold variants of the radioactive versions of the metal complex partner (e.g., non-radioactive indium complexes as described in the examples) can act as surrogates of the radioactive compounds. Furthermore, they are valuable tools for identifying metabolites in vitro or in vivo, as well as for assessing toxicity properties of the compounds of the invention. Additionally, chelator-metal complexes can be used in binding assays utilizing the fluorescence properties of some metal complexes with distinct ligands (e.g., Europium salts).

[0540] Chelators can be synthesized or are commercially available with a wide variety of (possibly already activated) groups for the conjugation to peptides or amino acids.

[0541] Due to the ready availability of carboxyl groups, DTPA, DOTA, DOTAGA, NOTA, NODAGA, NODA-MPAA, HBED, TETA, CB-TE2A, DATA, AAZTA, NETA, DEP A, Crown, NOPO, TRAP, HYNIC, PCTA, PSC and N2S2- as well as N3S-based chelators are particularly suitable for direct attachment to an amino nitrogen of the compound or to an amino group of a linker attached to the compound. The resulting linkage in this respect is an amide linkage.

[0542] Isothiocynate-functionalized chelator derivatives of for example DOTA, NOTA, DOTAM, DTPA, CHX-A”-DTPA, H4octapa, PCTA, DOTP, DEP A, DE4TA, NETA, NE3TA and HOPO ligand platform chelators are particularly suitable for direct attachment to an amino nitrogen of the compound or to an amino group of a linker attached to the compound. The resulting linkage in this respect is a thiourea linkage.

[0543] Functional groups in a chelator which are preferred groups for the direct attachment of a chelator to an amino-nitrogen are known to the person skilled in the art and include, but are not limited to, carboxylic acid, activated carboxylic acid, e.g., active ester like for instance NHS-ester, pentafluorophenol-ester, HOBt-ester, HOAt-ester, and isothiocyanate. Functional groups in a chelator which are preferred reactive groups for the direct attachment of a chelator to a carboxyl group are known to the person skilled in the art and include, but are not limited to, alkylamino and arylamino groups. Respective chelator reagents are commercially available, e.g., alkylamino or arylamino-functionalized DOTA.

[0544] Functional groups in a chelator which are preferred groups for the direct attachment of a chelator to a thiol group are known to the person skilled in the art and include, but are not limited to maleimide nitrogens. Respective chelator reagents are commercially available, e.g., maleimide-functionalized DOTA.

[0545] Functional groups in a chelator which are preferred groups for the direct attachment of a chelator to an azido group are known to the person skilled in the art and include, but are not limited to, acyclic and cyclic alkynes. Respective chelator reagents are commercially available, e.g., propargyl or butynyl-functionalized DOTA.

[0546] Functional groups in a chelator which are preferred groups for the direct attachment of a chelator to an alkyne group are known to the person skilled in the art and include, but are not limited to, alkyl and aryl azines. Respective chelator reagents are commercially available, e.g., azidopropyl-functionalized DOTA.

[0547] In an embodiment, each Z group of the compound of the invention independently comprises a chelator and a linker. It will be acknowledged by the persons skilled in the art that, in principle, a chelator as defined herein can be combined with an appropriate linker as defined herein so as to form a linkage to both the chelator and to a functional group in the compound of the invention (i.e., a functional group that provides a suitable attachment point for the linker). A non-limiting list of preferred Z groups comprising a chelator and a linker (exemplified for DOTA as the chelator) is as follows:

[0548] DOTA-Ttds: DOTA-O2Oc: DOTA-OlPen:

[0549] DOTA-Cmp: DOTA-Nmg: DOTA-Gab: D0TA-4Amc:

[0550] DOTA-Pamb: DOTA-Mamb:

[0551] DOTA-Rni: DOTA-asp:

[0552] DOTA-glu: D0TA-KMe3:

[0553]

[0554] In preferred embodiments, the chelator (which may be comprised as an effector in each group Z) is a residue of DOTA, DOTAGA, DOTAM, Crown, DOTP, NOTA, NOD AGA, NODA- MPAA, HBED, TETA, CB-TE2A, DTP A, CHX-A”-DTPA, DFO, Macropa, HOPO ligand platform, TRAP, THP, AAZTA, DATA, NOPO, PCTA, PSC, sarcophagine, FSC, DEP A, DE4TA, NET A, NE3TA, H4octapa, H4CHXoctapa, H4pypa, H4py4pa, HYNIC, NxS4-x (N4, N2S2, N3S),99mTc(CO)3-chelators.

[0555] In more preferred embodiments, the chelator (which may be comprised as an effector in each group Z) is a residue of DOTA, DOTAGA, DOTAM, Crown, NOTA, NODAGA, NODAMP AA, CB-TE2A, CHX-A”-DTPA, DFO, Macropa, THP, AAZTA, NOPO, PCTA, PSC, sarcophagine, NET A, H4CHXoctapa, H4pypa and N4, preferably of DOTA, DOTAGA, DOTAM, NOTA, NOD AGA, Macropa, Crown, NOPO, PCTA, PSC and N4, more preferably of DOTA, DOTAM, Macropa, NOTA, PSC or NOD AGA, and most preferably of DOTA.

[0556] In a more preferred embodiment, in formula (I), each group Z (i.e., Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9) is independently a moiety represented by the following formula (XIII): E-* (XIII) wherein,

[0557] * indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, and

[0558] E is a residue represented by any one of the following formulae (XlVa) to (XlVn):

[0559] wherein,

[0560] Xci and XC2 are each independently selected from the group consisting of -OH and -NH2, and

[0561] XC3 is independently selected from the group consisting of -NH-* and -N-C(S)-*,

[0562] * indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, and the residue E optionally comprises a radionuclide. Preferably, if Z (or E) is covalently attached to an N atom of an amino group of (or comprised in) the side chain of any one of Xaal, Xaa3, Xaa5, Xaa6, Xaa8, Xaa9, XaalO and Xaal l, E is a residue represented by any one of the formulae (XlVa) to (XlVn), wherein XC3 is -N-C(S)-*; and if Z (or E) is covalently attached to a C atom of a carbonyl group of (or comprised in) the side chain of any of Xaal, Xaa3, Xaa5, Xaa6, Xaa8, Xaa9, XaalO and Xaal l or of (or comprised in) the main chain of any of Xaa7, Xaa8, Xaa9, XaalO and Xaal l, E is a residue represented by any one of the formulae (XIVc), (XlVf), (XlVj) and (XlVn), wherein XC3 is - NH*-. In a more preferred embodiment, in formula (I), each group Z (i.e., Zla, Zlb, Z2, Z3, Z4, Z5, Z6,

[0563] Z7, Z8and Z9) is independently a moiety represented by the following formula (XV):

[0564] E-L-* (XV) wherein,

[0565] * indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, and

[0566] (a) E is a residue represented by any one of the following formulae (XVIa) to (XVIn): wherein,

[0567] Xci and XC2 are each independently selected from the group consisting of -OH and -NH2, and

[0568] ** indicates covalent attachment to L, the residue E optionally comprises a chelated radionuclide, and

[0569] L is a linker moiety represented by any one of the formulae (XVIIa) to (XVIIt): wherein, nl is 1 to 5, n2, n3, n4 and nl2 are each independently 0 to 2, n5, n6 and n29 are each independently 1 to 10, n7 and n8 are each independently 0 to 4, n9, nl3, nl4, nl5, nl8, n20 and n21 are each independently 1 or 2, n 10 and ni l are each independently 0 or 1, nl6 is 0 to 12, nl7, nl9, n22, n27 and n28 are each independently 1 to 4, n23 is 2 to 4,

[0570] XL1, XL2, XL3, XL4and XL5are each independently =CH- or =N-,

[0571] XL6, XL7, XL1° and XL11are each independently -OH or -NH2,

[0572] RL1, RL2, RL3, RL4, RL5and RL6are each independently -H or a methyl group, * indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and

[0573] **’ indicates covalent attachment to E; or,

[0574] (b) E is a residue represented by the following formula (XVIo) or (XVIr): wherein,

[0575] Xci and XC2 are each independently selected from the group consisting of -OH and -NH2, and

[0576] ** indicates covalent attachment to L, and the residue E optionally comprises a radionuclide, L is a linker moiety represented by any one of the formulae (XVIIu) to (XVIIy): wherein, n24 is 1 to 5, n25 and n26 are each independently 1 or 2,

[0577] XL8and XL9are each independently =CH- or =N-,

[0578] RL7, RL8, RL9, RL1°, RL12and RL12are each independently -H or a methyl group, and

[0579] * indicates covalent attachment to an N atom of an amino group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and

[0580] **’ indicates covalent attachment to E.

[0581] Preferably, in the above formula (XV), if Z (or L) is covalently attached to a C atom of a carbonyl group of (or comprised in) the side chain of any of Xaal, Xaa3, Xaa5, Xaa6, Xaa8, Xaa9, XaalO and Xaal l or of (or comprised in) the main chain of any of Xaa7, Xaa8, Xaa9, XaalO and Xaal 1, L is selected from any one of the formulae (XVIIa) to (XVIIg); and if Z (or L) is covalently attached to an N atom of an amino group of (or comprised in) the main chain (backbone) of Xaal or the side chain of any one of Xaal, Xaa3, Xaa5, Xaa6, Xaa8, Xaa9, XaalO and Xaal 1, L is selected from any one of the formulae (XVIIh) to (XVIIy).

[0582] In a more preferred embodiment, in formula (I), each group Z (i.e., Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9) is independently a moiety represented by the following formula (XV’):

[0583] E-L1-L2-* (XV’) wherein,

[0584] * indicates covalent attachment to a carbonyl group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and E is a residue represented by any one of the following formulae (XVIa) to (XVIn): wherein,

[0585] Xci and XC2 are each independently selected from the group consisting of -OH and -NH2, and

[0586] ** indicates covalent attachment to Li, the residue E optionally comprises a radionuclide, and

[0587] Li is a linker moiety represented by any one of the formulae (XVII’a) to (XVII’g): wherein, nl is 1 to 5, n2, n3 and n4 are each independently 0 to 2, n29 is 1 to 10, n27 and n28 are each independently 1 to 4, n23 is 2 to 4,

[0588] XL1and XL2are each independently =CH- or =N-,

[0589] XL1° and XL11are each independently -OH or -NH2, *** indicates covalent attachment to L2, and

[0590] **’ indicates covalent attachment to E; and

[0591] L2 is a linker moiety represented by any one of the formulae (XVII’h) to (XVII’t): wherein, nl2 is 0 to 2, n5 and n6 are each independently 1 to 10, n7 and n8 are each independently 0 to 4, n9, nl3, nl4, nl5, nl8, n20 and n21 are each independently 1 or 2, n 10 and ni l are each independently 0 or 1, nl6 is 0 to 12, nl7, nl9 and n22 are each independently 1 to 4, n23 is 2 to 4,

[0592] XL3, XL4and XL5are each independently =CH- or =N-,

[0593] XL6and XL7are each independently -OH or -NH2,

[0594] RL1, RL2, RL3, RL4, RL5and RL6are each independently -H or a methyl group, * indicates covalent attachment to a carbonyl group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and ***’ indicates covalent attachment to Li.

[0595] Preferably, in the above formula (XV’), L2 is covalently attached to a C atom of a carbonyl group of (or comprised in) the side chain of any of Xaal, Xaa3, Xaa5, Xaa6, Xaa8, Xaa9, XaalO and Xaal l or of (or comprised in) the main chain of any of Xaa7, Xaa8, Xaa9, XaalO and Xaal l.

[0596] In a more preferred embodiment, in formula (I), each group Z (i.e., Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9) is independently a moiety represented by the following formula (XV”):

[0597] E-L-* (XV”) wherein,

[0598] * indicates covalent attachment to a carbonyl group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and

[0599] E is a residue represented by the following formula (XVIo) or (XVIr):

[0600] Xci and XC2 are each independently selected from the group consisting of -OH and -NH2, and

[0601] ** indicates covalent attachment to L, and the residue E optionally comprises a radionuclide,

[0602] L is a linker moiety represented by any one of the formulae (XVIP'h) to (XVII’ ’t): wherein, nl2 is 0 to 2, n5 and n6 are each independently 1 to 10, n7 and n8 are each independently 0 to 4, n9, nl3, nl4, nl5, nl8, n20 and n21 are each independently 1 or 2, n 10 and ni l are each independently 0 or 1, nl6 is 0 to 12, nl7, nl9 and n22 are each independently 1 to 4, n23 is 2 to 4, XL3, XL4and XL5are each independently =CH- or =N-, XL6and XL7are each independently -OH or -NH2, RL1, RL2, RL3, RL4, RL5and RL6are each independently -H or a methyl group, * indicates covalent attachment to a carbonyl group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and **’ indicates covalent attachment to L.

[0603] Preferably, in the above formula (XV”), L is covalently attached to a C atom of a carbonyl group of (or comprised in) the side chain of any of Xaal, Xaa3, Xaa5, Xaa6, Xaa8, Xaa9, XaalO and Xaal l or of (or comprised in) the main chain of any of Xaa7, Xaa8, Xaa9, XaalO and Xaal l.

[0604] Moreover, if the compound of formula (I) contains more than one group Z, each group Z (i.e., Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9) may be independently selected from the moi eties of formulae (XIII), (XV), (XV’) and (XV”) described above.

[0605] In the above formulae (XIII), (XV), (XV’) and (XV”), the radionuclide, if present, is preferably as described in above section 2.1.2, and more preferably a diagnostically active radionuclide or a therapeutically active radionuclide (as described above).

[0606] In an embodiment of the present invention, it is preferred that the chelator E and the radionuclide comprised therein are as defined in the table below. The left column indicates the chelator and the right columns indicate, for each chelator, the corresponding radionuclides by order of preference. Table 8: Overview of preferred chelator-nuclide combinations in the context of the present invention. t as disclosed in: Santos et al., Molecules 2021, 26(22), 6997

[0607] In an even more preferred embodiment, in formula (I), each group Z (i.e., Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9) is independently a moiety represented by any one of the following formulae (XVIIIa) to (XVIIIn):

[0608] wherein,

[0609] Xci, XC2, XL6and XL7are each independently selected from the group consisting of -OH and -NH2, and n6 is 1 to 10, and n7 and n8 are each independently 0 to 4, n9, nl3, nl4, nl5, nl8, n20 and n21 are each independently 1 or 2, and nlO and ni l are each independently 0 or 1, and nl2 is 0 to 2, nl6 and n27 are each independently 0 to 12, and nl7, nl9 and n22 are each independently 1 to 4, and n23 is 2 to 4, and

[0610] XL3, XL4and XL5are each independently =N- or =CH-, and

[0611] RL1, RL2, RL3, RL4, RL5, RL6and RL13are each independently -H or a methyl group, and * indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, and the moiety represented by any one of the above formulae (XVIIIa) to (XVIIIn) optionally comprises a radionuclide, the radionuclide being preferably selected from the group consisting of A118F,43Sc,44Sc,47Sc,51Mn,52Mn,64Cu,64Cu,67Cu,67Ga,68Ga, 86Y,89Zr,90Y,mIn,149Tb,152Tb,153Sm,155Tb,161Tb,177Lu,2O1T1,203Pb,212Pb,213Bi, 225Ac,226Th and227Th.

[0612] In a still more preferred embodiment, in formula (I), each group Z (i.e., Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9) is independently a moiety represented by any one of the following formulae (XVIIIa) to (XVIIIv): XVIIIk) (XVIII1) (XVIIIm) (XVIIIn) wherein,

[0613] * indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, and the moiety represented by any one of the above formulae (XVIIIa) to (XVIIIv) optionally comprises a radionuclide, the radionuclide being preferably selected from the group consisting of A118F,43Sc,44Sc,47Sc,51Mn,52Mn,64Cu,64Cu,67Cu,67Ga,68Ga, 86Y,89Zr,90Y,mIn,149Tb,152Tb,153Sm,155Tb,161Tb,177Lu,2O1T1,203Pb,212Pb,213Bi, 225Ac,226Th and227Th.

[0614] 2, 1.3.2 Drug

[0615] According to one embodiment, the effector is a drug, preferably a cytotoxic drug. The cytotoxic drug can be covalently bound to the peptide structure, optionally by means of a linker which may be cleavable or not. According to this embodiment, it is preferred that the compound of the present invention does not comprise a chelator. In these embodiments, the drug, preferably the cytotoxic drug, may be covalently bound to the peptide structure by means of linker moieties such as LI, L3, L4, or L6 (as described above).

[0616] Hereinafter are exemplary drugs that can be used as effector in the compound of the present invention:

[0617] (A) Antineoplastic agents such as

[0618] (Al) DNA-alkylating agents, e.g. duocarmycin (including synthetic analogues thereof: adozelesin, carzelesin, bizelesin, KW-2189 and CBI-TMI), nitrogen mustard analogues (e.g. cyclophosphamide chlorambucil, melphalan, chlormethine, ifosfamide, trofosfamide, prednimustine, bendamustine, chlornaphazine, estramustine, mechlorethamine, mechlorethamine oxide hydrochloride, mannomustine, mitolactol, novembichin, phenesterine, uracil mustard), alkyl sulphonates (e.g. busulfan, treosulfan, mannosulfan, improsulfan and piposulfan), ethylene imines (e.g. thiotepa, triaziquone, carboquone), nitrosoureas (e.g. carmustine, lomustine, semustine, streptozocin, chlorozotocin, fotemustine, nimustine, ranimustine), epoxides (e.g. etoglucid), other alkylating agents (e.g. mitobronitol, pipobroman, temozolomide, dacarbazine);

[0619] (A2) Topoisomerase inhibitors, e.g. doxorubicin, morpholino-doxorubicin, cyanomorpholino-doxorubicin, 2-pyrrolino- doxorubicin, deoxydoxorubicin, etoposide, etoposide phosphate, irinotecan and metabolites thereof such as SN- 38, teniposide, topotecan, resveratrol, epipodophyllins (e.g. 9- aminocamptothecin, camptothecin, crisnatol, daunomycin, mitoxantrone, novantrone, retinoic acids (retinols), 9-nitrocamptothecin (RFS 2000));

[0620] (A3) RNA-polymerase II inhibitors, e.g. alpha-amanitin, other amatoxins;

[0621] (A4) DNA-cleaving agents, e.g. calicheamicin;

[0622] (A5) Antimitotic agents or microtubule disruptors, e.g. vinca alkaloids (e.g. vincristine, vinblastine, vindesine, vinorelbine, navelbin, vinflunide, vintafolide), taxanes (e.g. paclitaxel, docetaxel, paclitaxel polyglumex, cabazitaxel) and their analogs, maytansinoids (e.g. DM1, DM2, DM3, DM4, maytansine and ansamitocins) and their analogs, cryptophycins (e.g. cryptophycin 1 and cryptophycin 8), epothilones, eleutherobin, discodermolide, bryostatins, dolostatins, auristatins (e.g. monomethyl auristatin E (MMAE), monomethyl auristatin F), tubulysins, cephalostatins; pancrati statin, sarcodictyin, spongistatin, demecolcine, mitomycins;

[0623] (A6) Anti-metabolites, e.g. DHFR inhibitors (e.g. methotrexate, trimetrexate, denopterin, pteropterin, aminopterin (4-aminopteroic acid) or other folic acid analogues such as raltitrexed, pemetrexed, pralatrexate), IMP dehydrogenase inhibitors (e.g. mycophenolic acid, tiazofurin, ribavirin, EICAR), ribonucleotide reductase inhibitors (e.g. hydroxyurea, deferoxamine), pyrimidine analogs (e.g. cytarabine, fluorouracil, 5-fluorouracil and metabolites thereof, tegafur, carmofur, gemcitabine, capecitabine, azacitidine, decitabine, fluorouracil combinations, tegafur combinations, trifluridine combinations, cytosine arabinoside, ancitabine, floxuridine, doxifluridine), uracil analogs (e.g. 6- azauridine, deoxyuridine), cytosine analogs (e.g. enocitabine), purine analogs (e.g. azathioprine, fludarabine, mercaptopurine, thiamiprine, thioguanine, cladribine, clofarabine, nelarabine), folic acid replenisher such as folinic acid;

[0624] (A7) Akinesin spindle protein inhibitor, e.g. filanesib;

[0625] (A8) Kinase inhibitors, e.g. ipatasertib, BIBW 2992 (anti-EGFR / Erb2), imatinib, gefitinib, pegaptanib, sorafenib, dasatinib, sunitinib, erlotinib, nilotinib, lapatinib, axitinib, pazopanib, vandetanib, afatinib, vemurafenib, crizotinib, regorafenib, masitinib, dabrafenib, trametinib, ibrutinib, ceritinib, lenvatinib, nintedanib, cediranib, palbocidib, osimertinib, alectinib, alectinib, rociletinib, cobimetinib, midostaurin, olmutinib, E7080 (anti-VEGFR2), mubritinib, ponatinib (AP24534), bafetinib (INNO-406), bosutinib (SKI-606), cabozantinib, vismodegib, iniparib, ruxolitinib, CYT387, tivozanib, ispinesib, temsirolimus, everolimus, ridaforolimus;

[0626] (A9) Anicotinamide phosphoribosyltransferase inhibitor e.g. CAS No.2241014-82-2;

[0627] (A10) A matrix metallopeptidase 9 inhibitor, e.g. derivatives of CGS27023A;

[0628] (All) A phosphatase inhibitor, e.g. mycrocystin-LR;

[0629] (B) Immunomodulatory agents including immunostimulants, immunosuppressants, cyclosporine, cyclosporine A, aminocaproic acid, azathioprine, bromocriptine, chlorambucil, chloroquine, cyclophosphamide, corticosteroids (e.g. amcinonide, betamethasone, budesonide, hydrocortisone, flunisolide, fluticasone propionate, fluocortolone danazol, dexamethasone, prednisone, triamcinolone acetonide, beclometasone dipropionate), DHEA, hydroxychloroquine, meloxicam, methotrexate, mofetil, mycophenylate, sirolimus, tacrolimus, everolimus, fmgolimod, ibrutinib, imiquimod, resiquimod, cytokines, peptidic immunomodulators such as TLR agonists (e.g. CpG oligonucleotides);

[0630] (C) Anti-infectious disease agents including antibacterial drugs, antimycobacterial drugs and antiviral drugs. A non-limiting example of antibiotic used in an antibiotic-antibody drug conjugate is rifalogue, i.e. a rafamycin derivative;

[0631] (D) Radionuclides, metabolites, pharmaceutically acceptable salts, and / or prodrugs of any of the aforementioned agents (A) to (C).

[0632] According to one embodiment, the effector is a moiety derived from exatecan, PNU- 159682, DM4, amanitin, duocarmycin, auristatin, maytansine, tubulysin, calicheamicin, SN-38, taxol, daunomycin, vinblastine, doxorubicine, methotrexate, pyrrolobenzodiazepine, pyrrole-based kinesin spindle protein (KSP) inhibitors, indolino-benzodiazepine dimers, or radioisotopes and / or pharmaceutically acceptable salts thereof.

[0633] In an embodiment, the compound of the invention is present as a pharmaceutically acceptable salt.

[0634] 2.2. Preferred compounds

[0635] In a preferred embodiment, the compound or salt of the present invention is represented by any one of the following formulae:

[0636] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys(Me)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe2-Tyr-Cya-Thi-NH2

[0637] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Har-Tyr-Cya-Thi-NH2

[0638] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Asp-Thi-NH2

[0639] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys(Me)-Tyr-Asp-Thi-NH2

[0640] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2

[0641] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Pcnf-Cya-Thi-NH2

[0642] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Guf-Cya-Thi-NH2

[0643] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-en

[0644] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Onf-NH2

[0645] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Off-NH2

[0646] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Ser-Thi-NH2

[0647] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Thr-Thi-NH2

[0648] H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys-6Clw-KMe3-Tyr-Ser-Thi-NH2

[0649] H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0650] H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys(Me)-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0651] H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-KMe3-Lys(Z6)-Cya-Thi-NH2

[0652] H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-Lys(Z5)-Tyr-Cya-Thi-NH2

[0653] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0654] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NHMe

[0655] H-Pip-Trp-Cya-Npg-Orn(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0656] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0657] H-Pip-Trp-Cya-Npg-Apc(Z3)-Cya-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0658] H-Nma-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0659] H-KMe4-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0660] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2

[0661] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2

[0662] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-RMe2-Tyr-Cya-Thi-NH2

[0663] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Kip-Tyr-Cya-Thi-NH2

[0664] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Egd-Tyr-Cya-Thi-NH2

[0665] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Om-Tyr-Cya-Thi-NH2

[0666] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2

[0667] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Opy-Tyr-Cya-Thi-NH2

[0668] H-Pip-Trp-Asn-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2

[0669] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Kzw-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Egg-Tyr-Cya-Thi-NH2

[0670] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Om-Tyr-Cya-Thi-NH2

[0671] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Ocf-NH2

[0672] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Mff-NH2

[0673] H-Pip-Trp-Cya-Npg-Lys-Apc(Z4)-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0674] H-Pip-Trp-Cya-Npg-Apc-Lys(Z4)-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0675] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2

[0676] H-Pip-Trp-Cya-Mnpg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0677] H-Pip-Trp-Dmd-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0678] H-Pip-Trp-Cya-Nml-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0679] H-Ida-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0680] H-Mida-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0681] H-Pip-Trp-Cya-Mnpg-Om(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0682] H-Nmg-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0683] H-Pip-Trp-Cya-Gel-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0684] H-Pip-Trp-Cya-Npg-Apc(Z3)-Thr-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0685] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Thr-Tyr-Cya-Thi-NH2

[0686] H-Pip-Trp-Cya-Mnpg-Apc(Z3)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2

[0687] H-Pip-Trp-Cya-Mgel-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0688] H-Pip-Trp-Penox-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0689] H-Nmo(Me)-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0690] H-Pip-Trp-Cya-Npg-Dab(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0691] H-Mor-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0692] H-Nmo-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0693] H-Pip-Trp-Cya-Npg-Apc(Z3)-Ser-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0694] H-Azp-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0695] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Phe-NH2

[0696] In a more preferred embodiment, the compound or salt of the present invention is represented by any one of the following formulae:

[0697] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2

[0698] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys(Me)-Tyr-Cya-Thi-NH2

[0699] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe2-Tyr-Cya-Thi-NH2

[0700] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Har-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Asp-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys(Me)-Tyr-Asp-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2 H-Pip-T rp- Asp-Npg- Apc(Z3)- Asn-6C1 w-RMe2-T yr-Cy a-Thi -NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Kip-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Egd-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Om-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Opy-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asn-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Pcnf-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Guf-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-en H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Kzw-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Ocf-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Mff-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Cya-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Nma-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Orn(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Off-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Ser-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Thr-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys(Me)-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-Lys(Z5)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Om(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Nmg-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Gel-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cy a-Thi -NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Thr-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mgel-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0701] H-Pip-Trp-Penox-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Nmo(Me)-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Dab(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Ser-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Phe-NH2

[0702] In an even more preferred embodiment, the compound or salt of the present invention is represented by any one of the following formulae:

[0703] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2

[0704] H-Pip-T rp- Asp-Npg- Apc(Z3)- Asn-6C1 w-RMe2-T yr-Cy a-Thi -NH2

[0705] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Kip-Tyr-Cya-Thi-NH2

[0706] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0707] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2

[0708] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0709] H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Pcnf-Cya-Thi-NH2

[0710] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Kzw-Tyr-Cya-Thi-NH2

[0711] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Ocf-NH2

[0712] H-Nma-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0713] H-Pip-Trp-Cya-Npg-Orn(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0714] H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys(Me)-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0715] H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2

[0716] H-Pip-Trp-Cya-Mnpg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0717] H-Pip-Trp-Cya-Mnpg-Om(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0718] H-Pip-Trp-Cya-Gel-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cy a-Thi -NH2

[0719] H-Pip-Trp-Cya-Npg-Apc(Z3)-Thr-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Dab(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Phe-NH2

[0720] In the above formulae, each group Z3, Z4, Z5and Z6is independently an effector E which may optionally comprise a linker moiety L, the effector E being preferably selected from the group consisting of: (a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and

[0721] (P) a chelator optionally comprising a radionuclide; and

[0722] (y) a drug, preferably a cytotoxic drug; and

[0723] (5) an immune cell engaging effector, preferably recruiting and stimulating T cells, NK cells and / or phagocytotic cells.

[0724] Still more preferably, each group Z3, Z4, Z5and Z6is independently a chelator which may optionally comprise a linker moiety L, wherein the chelator comprises a radionuclide, and wherein preferably the chelator is independently a residue of DOTA, DOTAGA, DOTAM, Crown, DOTP, NOTA, NODAGA, NODA-MPAA, HBED, TETA, CB-TE2A, DTP A, CHX- A”-DTPA, DFO, Macropa, HOPO ligand platform, TRAP, THP, AAZTA, DATA, NOPO, PCTA, PSC, sarcophagine, FSC, DEP A, DE4TA, NETA, NE3TA, H4octapa, H4CHXoctapa, H4pypa, H4py4pa, HYNIC, NxS4-x (N4, N2S2, N3S),99mTc(CO)3-chelators.

[0725] Most preferably, each group Z3, Z4, Z5and Z6is independently a chelator which may optionally comprise a linker moiety L, wherein the chelator comprises a radionuclide, and wherein the chelator is independently a residue of is a residue of DOTA, DOTAGA, DOTAM, Crown, NOTA, NODAGA, NODA-MPAA, CB-TE2A, CHX-A”-DTPA, DFO, Macropa, THP, AAZTA, NOPO, PCTA, PSC, sarcophagine, NETA, H4CHXoctapa, H4pypa and N4, preferably of DOTA, DOTAGA, DOTAM, NOTA, NODAGA, Macropa, Crown, NOPO, PCTA, PSC and N4, more preferably of DOTA, DOTAM, Macropa, NOTA, PSC or NODAGA, and most preferably of DOTA.

[0726] In a preferred embodiment, the compound or salt of the present invention is represented by any one of the following formulae:

[0727] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Lys(Me)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe2-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Har-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Lys-Tyr-Asp-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Lys(Me)-Tyr-Asp-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Pcnf-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Guf-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-en

[0728] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Onf-NH2

[0729] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Off-NH2

[0730] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Ser-Thi-NH2

[0731] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Thr-Thi-NH2

[0732] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Lys-6Clw-KMe3-Tyr-Ser-Thi-NH2

[0733] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Lys-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0734] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Lys(Me)-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0735] H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-KMe3-Lys(DOTA)-Cya-Thi-NH2

[0736] H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-Lys(DOTA)-Tyr-Cya-Thi-NH2

[0737] H-Ida-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0738] H-Pip-Trp-Cya-Nml-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0739] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0740] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NHMe

[0741] H-Pip-Trp-Cya-Npg-Orn(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0742] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0743] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Cya-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0744] H-Nma-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0745] H-KMe4-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2

[0746] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2

[0747] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2

[0748] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-RMe2-Tyr-Cya-Thi-NH2

[0749] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Kip-Tyr-Cya-Thi-NH2

[0750] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Egd-Tyr-Cya-Thi-NH2

[0751] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Orn-Tyr-Cya-Thi-NH2

[0752] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2

[0753] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Opy-Tyr-Cya-Thi-NH2

[0754] H-Pip-Trp-Asn-Npg-Apc(DOTA)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2

[0755] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Kzw-Tyr-Cya-Thi-NH2

[0756] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Egg-Tyr-Cya-Thi-NH2

[0757] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Orn-Tyr-Cya-Thi-NH2

[0758] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Ocf-NH2

[0759] H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Mff-NH2

[0760] H-Pip-Trp-Cya-Npg-Apc(NOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(NODAGA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTAGA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(NOPO)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(BnTCMC)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA-PPAc)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA-glu)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA-Kzw)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTAM)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(PSC)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Ala-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Om(PSC)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Om(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Nmg-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Gel-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Thr-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Thr-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Apc(DOTA)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mgel-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Penox-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Nmo(Me)-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Dab(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Mor-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Nmo-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Ser-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Azp-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Phe-NH2 wherein the DOTA, NOTA, PSC, DOTAGA, NOPO, BnTCMC or NOD AGA moiety optionally comprises a radionuclide, the radionuclide being preferably selected from the group consisting of A118F,43Sc,44Sc,47Sc,51Mn,52Mn,64Cu,64Cu,67Cu,67Ga,68Ga,86Y,89Zr,90Y,mIn,149Tb,152Tb,153Sm,155Tb,161Tb,177Lu,2O1T1,203Pb,212Pb,213Bi,225Ac,226Th and227Th. In a more preferred embodiment, the compound or salt of the present invention is represented by any one of the following formulae:

[0761] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2

[0762] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-RMe2-Tyr-Cya-Thi-NH2

[0763] H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Pcnf-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Kzw-Tyr-Cya-Thi-NH2 H-Nma-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Orn(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Lys(Me)-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(NOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(NODAGA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA-PPAc)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(PSC)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Om(PSC)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Om(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Gel-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Thr-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Dab(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Phe-NH2 wherein the DOTA, NOTA, PSC or NODAGA moiety optionally comprises a radionuclide, the radionuclide being preferably selected from the group consisting of A118F,43SC,44SC,47SC,51Mn,52Mn,64Cu,64Cu,67Cu,67Ga,68Ga,86Y,89Zr,90Y,mIn, 149Tb,152Tb,153Sm,155Tb,161Tb,177Lu,2O1T1,203Pb,212Pb,213Bi,225Ac,226Th and227Th.

[0764] In some embodiments, the compound or salt of the present invention is represented by any one of the following formulae: H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-KMe3-Tyr-Cya-Thi-Ttds-Lys(DOTA)-NH2 H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-KMe3-Tyr-Lys(DOTA)-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-KMe3-Lys(DOTA)-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-Lys(DOTA)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Lys-Apc(DOTA)-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Lys(DOTA)-Npg-Apc-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Ida(O3TdN2-DOTA)-Trp-Cya-Npg-Apc-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-KMe3-Tyr-Cya-Lys(DOTA)-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-NH2 H-Pip-Trp-Cya-Npg-Apc(AF488-Ttds)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Lys(DOTA)-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Lys(DOTA)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Tap(DOTA)-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Lys(DOTA)-6Clw-Lys(DOTA)-Tyr-Cya-Thi-NH2wherein AF488 refers to the fluorophore Alexa Fluor 488, and DOTA moiety optionally comprises a radionuclide, the radionuclide being preferably selected from the group consisting of A118F,43Sc,44Sc,47Sc,51Mn,52Mn,64Cu,64Cu,67Cu,67Ga,68Ga,86Y,89Zr, 90Y,mIn,149Tb,152Tb,153Sm,155Tb,161Tb,177Lu,2O1T1,203Pb,212Pb,213Bi,225Ac,226Th and227Th.

[0765] Most preferably, the compound or salt of the present invention is any one selected from the following compounds:

[0766] the depicted compounds are preferably in complex with a radionuclide, which is preferably selected from the group consisting of A118F,43Sc,44Sc,47Sc,51Mn,52Mn,64Cu,64Cu,67Cu,67Ga,68Ga,86Y,89Zr,90Y,mIn,149Tb,152Tb,153Sm,155Tb,161Tb,177Lu,2O1T1,203Pb,212Pb,213Bi,225Ac,226Th and227Th. In this context, the expression “in complex with a radionuclide” means that the DOTA, NOTA, PSC or NODAGA moiety in the above compounds comprises or chelates a radionuclide.

[0767] 3. USE OF COMPOUND OR COMPOSITION FOR DIAGNOSTIC AND / OR

[0768] THERAPEUTIC PURPOSES

[0769] In an embodiment, the compound or pharmaceutical composition of the present invention may be used in a method of diagnosing and / or treating a disease, preferably cancer, and more preferably a P-cadherin expressing cancer.

[0770] The P-cad expression pattern in solid tumors makes it a compelling therapeutic and diagnostic target. Severe overexpression can be observed in many solid tumors, dominantly across numerous cell layers. Head and neck tumors are particularly affected, as are tumors of the lung, breast, esophagus, cervix, thymus, uterus, mesothelium, pancreas, colon, rectum, bladder, and ovary (Subbiah, et aL, Clin Cancer Res, 2020, 26: 5830). In breast cancer, high P-cadherin expression serves as a marker for particularly aggressive tumors. Here, P-cadherin has been shown to mediate increased cell migration and invasion (quite analogous to its natural function in early embryonic development). The consequences are metastasis and poor prognosis (Paredes, et al, Breast Cancer Res, 2007, 9: 214).

[0771] The compounds of the invention have a high binding affinity to P-cad. Because of this high binding affinity, the compounds of the invention are effective as, useful as and / or suitable as a targeting agent and, if conjugated to another moiety, as a targeting moiety. As preferably used herein a targeting agent is an agent which interacts with the target molecule which is in the instant case said P-cad. In terms of cells and tissues thus targeted and targetable, respectively, by the compounds of the invention any cell and tissue, respectively, expressing said P-cad in particular is targeted and targetable, respectively.

[0772] As is known from the prior art, while the protein occupies the role of a developmental cadherin and is found in diverse fetal structures, its occurrence in adult tissues is extremely limited. In adult humans, expression is mostly limited to the basal (proliferative) layer of some epithelia such as in skin, ovary, uterus, thymus, lung, breast, and prostate (Imai, et al. , Clin Cancer Res, 2008, 14: 6487). In contrast, P-cad is highly expressed in a mammalian body and a human body in particular on several neoplastic cells in several tumor indications, whereas the expression of P-cad in other tissues of the mammalian and the human body is low. These P-cad-expressing tumor indications include but are not limited to breast (Albergaria, et al. , Int J Dev Biol, 2011, 55: 811, Margan, et al., Anticancer Res, 2020, 40: 5557), colorectal (Kumara, et al, Oncoscience, 2017, 4: 139), ovarian (Kayahashi, et al, BMC Cancer, 2021, 21: 32), endometrial (Lewczuk, et al., Oncol Lett, 2021, 21: 261), cervical (Li, et al., PLoS One, 2016, 11: e0155910), head-and-neck (Seppala, et al. , Apnris, 2021, 129: 717), pancreatic (Siret, et al, Br J Cancer, 2018, 118: 546), biliary (Kim, et al., Medicine (Baltimore), 2016, 95: e4132), bladder (Wang, et al, Eur J Surg Oncol, 2014, 40: 255), gastric and lung cancer (Imai, et al, Clin Cancer Res, 2008, 14: 6487) as well as glioblastioma (Martins, et al., Mol Oncol, 2022, 16: 2611), sarcoma (Thuault, et al., Oncogene, 2013, 32: 1876) and cholangiocarcinoma (Sakamoto, et al., Cancer Sci, 2015, 106: 1153). Most preferably, the disease is selected from the group comprising or consisting of ovarian cancer, colorectal cancer and breast cancer.

[0773] In a still further embodiment, the aforementioned indications may occur in organs and tissues selected from the group comprising external upper lip, external lower lip, external lip nos, upper lip mucosa, lower lip mucosa, mucosa lip nos, commissure lip, overlapping lesion of lip, base of tongue nos, dorsal surface tongue nos, border of tongue, ventral surface of tongue nos, anterior 2 / 3 of tongue nos, lingual tonsil, overlapping lesion of tongue, tongue nos, upper gum, lower gum, gum nos, anterior floor of mouth, lateral floor of mouth, overlapping lesion of floor of mouth, floor of mouth nos, hard palate, soft palate nos, uvula, overlapping lesion of palate, palate nos, cheek mucosa, vestibule of mouth, retromolar area, overlapping lesion of other and unspecified parts of mouth, mouth nos, parotid gland, submaxillary gland, sublingual gland, overlapping lesion of major salivary glands, major salivary gland nos, tonsillar fossa, tonsillar pillar, overlapping lesion of tonsil, tonsil nos, vallecula, anterior surface of epiglottis, lateral wall oropharynx, posterior wall oropharynx, branchial cleft, overlapping lesion of oropharynx, oropharynx nos, superior wall of nasopharynx, posterior wall nasopharynx, lateral wall nasopharynx, anterior wall nasopharynx, overlapping lesion of nasopharynx, nasopharynx nos, pyriform sinus, postcricoid region, hypopharyngeal aspect of aryepiglottic fold, posterior wall hypopharynx, overlapping lesion of hypopharynx, hypopharynx nos, pharynx nos, laryngopharynx, waldeyer's ring, overlapping lesion of lip oral cavity and pharynx, cervical esophagus, thoracic esophagus, abdominal esophagus, upper third of esophagus, middle third of esophagus, esophagus lower third, overlapping lesion of esophagus, esophagus nos, cardia nos, fundus stomach, body stomach, gastric antrum, pylorus, lesser curvature of stomach nos, greater curvature of stomach nos, overlapping lesion of stomach, stomach nos, duodenum, jejunum, ileum, meckel's diverticulum, overlapping lesion of small intestine, small intestine nos, cecum, appendix, ascending colon, hepatic flexure of colon, transverse colon, splenic flexure of colon, descending colon, sigmoid colon, overlapping lesion of colon, colon nos, rectosigmoid junction, rectum nos, anus nos, anal canal, cloacogenic zone, overlapping lesion of rectum anus and anal canal, liver, intrahepatic bile duct, gallbladder, extrahepatic bile duct, ampulla of vater, overlapping lesion of biliary tract, biliary tract nos, head of pancreas, body pancreas, tail pancreas, pancreatic duct, islets of langerhans, neck of pancreas, overlapping lesion of pancreas, pancreas nos, intestinal tract nos, overlapping lesion of digestive system, gastrointestinal tract nos, nasal cavity, middle ear, maxillary sinus, ethmoid sinus, frontal sinus, sphenoid sinus, overlapping lesion of accessory sinuses, accessory sinus nos, glottis, supraglottis, subglottis, laryngeal cartilage, overlapping lesion of larynx, larynx nos, trachea, main bronchus, upper lobe lung, middle lobe lung, lower lobe lung, overlapping lesion of lung, lung nos, thymus, heart, anterior mediastinum, posterior mediastinum, mediastinum nos, pleura nos, overlapping lesion of heart mediastinum and pleura, upper respiratory tract nos, overlapping lesion of respiratory system and intrathoracic organs, respiratory tract nos, upper limb long bones joints, upper limb short bones joints, lower limb long bones joints, lower limb short bones joints, overlapping lesion of bones joints and articular cartilage of limbs, bone limb nos, skull and facial bone, mandible, vertebral column, rib sternum clavicle, pelvic bone, overlapping lesion of bones joints and articular cartilage, bone nos, blood, bone marrow, spleen, reticuloendothelial system nos, hematopoietic system nos, skin lip nos, eyelid nos, external ear, skin face, skin scalp neck, skin trunk, skin limb upper, skin limb lower, peripheral nerve head neck, peripheral nerve shoulder arm, peripheral nerve leg, peripheral nerve thorax, peripheral nerve abdomen, peripheral nerve pelvis, peripheral nerve trunk, overlapping lesion of peripheral nerves and autonomic nervous system, autonomic nervous system nos, retroperitoneum, peritoneum, peritoneum nos, overlapping lesion of retroperitoneum and peritoneum, connective tissue head, connective tissue arm, connective tissue leg, connective tissue thorax, connective tissue abdomen, connective tissue pelvis, connective tissue trunk nos, overlapping lesion of connective subcutaneous and other soft tissues, connective tissue nos, nipple, central portion of breast, upper inner quadrant of breast, lower inner quadrant of breast, upper outer quadrant of breast, lower outer quadrant of breast, axillary tail of breast, overlapping lesion of breast, breast nos, labium majus, labium minus, clitoris, overlapping lesion of vulva, vulva nos, vagina nos, endocervix, exocervix, overlapping lesion of cervix uteri, cervix uteri, isthmus uteri, endometrium, myometrium, fundus uteri, overlapping lesion of corpus uteri, corpus uteri, uterus nos, ovary, fallopian tube, broad ligament, round ligament, parametrium, uterine adnexa, wolffian body, overlapping lesion of female genital organs, female genital tract nos, prepuce, glans penis, body penis, overlapping lesion of penis, penis nos, prostate gland, undescended testis, descended testis, testis nos, epididymis, spermatic cord, scrotum nos, tunica vaginalis, overlapping lesion of male genital organs, male genital organs nos, kidney nos, renal pelvis, ureter, trigone bladder, dome bladder, lateral wall bladder, posterior wall bladder, ureteric orifice, urachus, overlapping lesion of bladder, bladder nos, urethra, paraurethral gland, overlapping lesion of urinary organs, urinary system nos, conjunctiva, cornea nos, retina, choroid, ciliary body, lacrimal gland, orbit nos, overlapping lesion of eye and adnexa, eye nos, cerebral meninges, spinal meninges, meninges nos, cerebrum, frontal lobe, temporal lobe, parietal lobe, occipital lobe, ventricle nos, cerebellum nos, brain stem, overlapping lesion of brain, brain nos, spinal cord, cauda equina, olfactory nerve, optic nerve, acoustic nerve, cranial nerve nos, overlapping lesion of brain and central nervous system, nervous system nos, thyroid gland, adrenal gland cortex, adrenal gland medulla, adrenal gland nos, parathyroid gland, pituitary gland, craniopharyngeal duct, pineal gland, carotid body, aortic body, overlapping lesion of endocrine glands and related structures, endocrine gland nos, head face or neck nos, thorax nos, abdomen nos, pelvis nos, upper limb nos, lower limb nos, other illdefined sites, overlapping lesion of ill-defined sites, lymph node face head neck, intrathoracic lymph node, intra-abdominal lymph nodes, lymph node axilla arm, lymph node inguinal region leg, lymph node pelvic, lymph nodes of multiple regions, lymph node nos, unknown primary site.

[0774] In an embodiment of the present invention, the cancers listed herein are locally advanced, unresectable, metastatic, or any combination thereof.

[0775] In particular embodiments, the compound or composition of the present invention is for use in a method of diagnosing and / or treating cancer, preferably a P-cadherin expressing cancer, wherein the cancer is selected from the group consisting of ovarian cancer, colorectal cancer, cholangiocarcinoma, non-small cell lung cancer (NSCLC) including squamous NSCLC, esophageal cancer, head-and-neck cancer including squamous cell carcinoma of head and neck (SCCHN), and tumors of the breast including triple negative breast cancer (TNBC), pancreatic cancer including pancreatic ductal adenocarcinoma (PDAC), endometrial cancer, cervical cancer, gastric cancer and sarcoma, and preferably from the group consisting of ovarian cancer, colorectal cancer, esophageal cancer, head-and-neck cancer and breast cancer.

[0776] The subjects treated with the compounds of the invention may be treated in combination with other non-surgical anti-proliferative (e.g., anti-cancer) drug therapy. In one embodiment, the compounds may be administered in combination with an anti-cancer compound such as a cytostatic compound. A cytostatic compound is a compound (e.g., a small molecule, a nucleic acid, or a protein) that suppresses cell growth and / or proliferation. In some embodiments, the cytostatic compound is directed towards the malignant cells of a tumor.

[0777] Suitable anti-proliferative drugs or cytostatic compounds to be used in combination with the compounds of the invention include anti-cancer drugs. Numerous anti-cancer drugs which may be used are well known and include, but are not limited to: Acivicin; Aclarubicin; Acodazole Hydrochloride; Acronine; Adozelesin; Aldesleukin; Altretamine; Ambomycin; Ametantrone Acetate; Aminoglutethimide; Amsacrine; Anastrozole; Anthramycin; Asparaginase; Asperlin; Azacitidine; Azetepa; Azotomycin; Batimastat; Benzodepa; Bicalutamide; Bisantrene Hydrochloride; Bisnafide Dimesylate; Bizelesin; Bleomycin Sulfate; Brequinar Sodium; Bropirimine; Busulfan; Cactinomycin; Calusterone; Caracemide; Carbetimer; Carboplatin; Carmustine; Carubicin Hydrochloride; Carzelesin; Cedefingol; Chlorambucil; Cirolemycin; Cisplatin; Cladribine; Crisnatol Mesylate; Cyclophosphamide; Cytarabine; Dacarbazine; Dactinomycin; Daunorubicin Hydrochloride; Decitabine; Dexormaplatin; Dezaguanine; Dezaguanine Mesylate; Diaziquone; Docetaxel; Doxorubicin; Doxorubicin Hydrochloride; Droloxifene; Droloxifene Citrate; Dromostanolone Propionate; Duazomycin; Edatrexate; Eflornithine Hydrochloride; Elsamitrucin; Enloplatin; Enpromate; Epipropidine; Epirubicin Hydrochloride; Erbulozole; Esorubicin Hydrochloride; Estramustine; Estramustine Phosphate Sodium; Etanidazole; Etoposide; Etoposide Phosphate; Etoprine; Fadrozole Hydrochloride; Fazarabine; Fenretinide; Floxuridine; Fludarabine Phosphate; Fluorouracil; Fluorocitabine; Fosquidone; Fostriecin Sodium; Gemcitabine; Gemcitabine Hydrochloride; Hydroxyurea; Idarubicin Hydrochloride; Ifosfamide; Ilmofosine; Interferon Alfa-2a; Interferon Alfa-2b; Interferon Alfa-nl; Interferon Alfa-n3; Interferon Beta-I a; Interferon Gamma-I b; Iproplatin; Irinotecan Hydrochloride; Lanreotide Acetate; Letrozole; Leuprolide Acetate; Liarozole Hydrochloride; Lometrexol Sodium; Lomustine; Losoxantrone Hydrochloride; Masoprocol; Maytansine; Mechlorethamine Hydrochloride; Megestrol Acetate; Melengestrol Acetate; Melphalan; Menogaril; Mercaptopurine; Methotrexate; Methotrexate Sodium; Metoprine; Meturedepa; Mitindomide; Mitocarcin; Mitocromin; Mitogillin; Mitomalcin; Mitomycin; Mitosper; Mitotane; Mitoxantrone Hydrochloride; Mycophenolic Acid; Niraparib; Nocodazole; Nogalamycin; Olaparib; Ormaplatin; Oxisuran; Paclitaxel; Pegaspargase; Peliomycin; Pentamustine; Peplomycin Sulfate; Perfosfamide; Pipobroman; Piposulfan; Piroxantrone Hydrochloride; Plicamycin; Plomestane; Porfimer Sodium; Porfiromycin; Prednimustine; Procarbazine Hydrochloride; Puromycin; Puromycin Hydrochloride; Pyrazofurin; Riboprine; Rogletimide; Rucaparib; Safingol; Safingol Hydrochloride; Semustine; Simtrazene; Sparfosate Sodium; Sparsomycin; Spirogermanium Hydrochloride; Spiromustine; Spiroplatin; Streptonigrin; Streptozocin; Sulofenur; Talazoparib; Talisomycin; Taxol; Taxotere; Tecogalan Sodium; Tegafur; Teloxantrone Hydrochloride; Temoporfm; Teniposide; Teroxirone; Testolactone; Thiamiprine; Thioguanine; Thiotepa; Tiazofurin; Tirapazamine; Topotecan Hydrochloride; Toremifene Citrate; Trestolone Acetate; Triciribine Phosphate; Trimetrexate; Trimetrexate Glucuronate; Tubulozole Hydrochloride; Uracil Mustard; Uredepa; Vapreotide; Velaparib; Verteporfin; Vinblastine Sulfate; Vincristine Sulfate; Vindesine; Vindesine Sulfate; Vinepidine Sulfate; Vinglycinate Sulfate; Vinleurosine Sulfate; Vinorelbine Tartrate; Vinrosidine Sulfate; Vinzolidine Sulfate; Vorozole; Zeniplatin; Zinostatin; and Zorubicin Hydrochloride.

[0778] Other anti-cancer drugs include, but are not limited to: 20-epi-l,25 dihydroxyvitamin D3; 5- ethynyluracil; abiraterone; acylfulvene; adecypenol; adozelesin; ALL-TK antagonists; ambamustine; amidox; amifostine; aminolevulinic acid; amrubicin; anagrelide; andrographolide; angiogenesis inhibitors; antagonist D; antagonist G; antarelix; anti- dorsalizing morphogenetic protein-1; antiestrogen; antineoplaston; antisense oligonucleotides; aphidicolin glycinate; apoptosis gene modulators; apoptosis regulators; apurinic acid; ara-CDP- DL-PTBA; arginine deaminase; asulacrine; atamestane; atrimustine; axinastatin 1; axinastatin 2; axinastatin 3; azasetron; azatoxin; azatyrosine; baccatin III derivatives; balanol; batimastat; BCR / ABL antagonists; benzochlorins; benzoylstaurosporine; beta lactam derivatives; beta- alethine; betaclamycin B; betulinic acid; bFGF inhibitor; bisaziridinylspermine; bisnafide; bistratene A; breflate; budotitane; buthionine sulfoximine; calcipotriol; calphostin C; camptothecin derivatives; canarypox IL-2; capecitabine; carboxamide-amino-triazole; carboxyamidotriazole; CaRest M3; CARN 700; cartilage derived inhibitor; casein kinase inhibitors (ICOS); castanospermine; cecropin B; cetrorelix; chlorins; chloroquinoxaline sulfonamide; cicaprost; cis-porphyrin; clomifene analogues; clotrimazole; collismycin A; collismycin B; combretastatin A4; combretastatin analogue; conagenin; crambescidin 816; crisnatol; cryptophycin 8; cryptophycin A derivatives; curacin A; cyclopentanthraquinones; cycloplatam; cypemycin; cytarabine ocfosfate; cytolytic factor; cytostatin; dacliximab; dehydrodidemnin B; deslorelin; dexifosfamide; dexrazoxane; dexverapamil; didemnin B; didox; diethylnorspermine; dihydro-5-azacytidine; dihydrotaxol, 9-; dioxamycin; diphenyl spiromustine; docosanol; dolasetron; doxifluridine; dronabinol; duocarmycin SA; ebselen; ecomustine; edelfosine; edrecolomab; eflomithine; elemene; emitefur; epirubicin; epristeride; estramustine analogue; estrogen agonists; estrogen antagonists; etanidazole; etoposide phosphate; exemestane; filgrastim; finasteride; flavopiridol; flezelastine; fhiasterone; fludarabine; fhiorodaunorunicin hydrochloride; forfenimex; formestane; fotemustine; gadolinium texaphyrin; gallium nitrate; galocitabine; ganirelix; gelatinase inhibitors; glutathione inhibitors; hepsulfam; heregulin; hexamethylene bisacetamide; hypericin; ibandronic acid; idoxifene; idramantone; ilmofosine; ilomastat; imidazoacridones; imiquimod; immunostimulant peptides; insulin-like growth factor-I receptor inhibitor; interferon agonists; interferons; interleukins; iobenguane; iododoxorubicin; ipomeanol, 4-; irinotecan; iroplact; irsogladine; isobengazole; isohomohalicondrin B; itasetron; jasplakinolide; kahalalide F; lamellarin-N triacetate; lanreotide; leinamycin; lenograstim; lentinan sulfate; leptolstatin; leukemia inhibiting factor; leukocyte alpha interferon; leuprolide+estrogen+progesterone; leuprorelin; levamisole; liarozole; linear polyamine analogue; lipophilic disaccharide peptide; lipophilic platinum compounds; lissoclinamide 7; lobaplatin; lombricine; lometrexol; lonidamine; losoxantrone; lovastatin; loxoribine; lurtotecan; lutetium texaphyrin; lysofylline; lytic peptides; maitansine; mannostatin A; marimastat; masoprocol; maspin; matrilysin inhibitors; matrix metalloproteinase inhibitors; merbarone; meterelin; methioninase; metoclopramide; MIF inhibitor; mifepristone; miltefosine; mirimostim; mismatched double stranded RNA; mitoguazone; mitolactol; mitomycin analogues; mitonafide; mitotoxin fibroblast growth factor-saporin; mofarotene; molgramostim; monoclonal antibody, human chorionic gonadotrophin; monophosphoryl lipid A+myobacterium cell wall sk; mopidamol; multiple drug resistance gene inhibitor; multiple tumor suppressor 1 -based therapy; mustard anti cancer compound; mycaperoxide B; mycobacterial cell wall extract; myriaporone; N- acetyldinaline; N-substituted benzamides; nafarelin; nagrestip; naloxone+pentazocine; napavin; naphterpin; nartograstim; nedaplatin; nemorubicin; neridronic acid; neutral endopeptidase; nilutamide; nisamycin; nitric oxide modulators; nitroxide antioxidant; nitrullyn; O6-benzylguanine; octreotide; okicenone; oligonucleotides; onapristone; ondansetron; ondansetron; oracin; oral cytokine inducer; osaterone; oxaliplatin; oxaunomycin; paclitaxel analogues; paclitaxel derivatives; palauamine; palmitoylrhizoxin; pamidronic acid; panaxytriol; panomifene; parabactin; pazelliptine; pegaspargase; peldesine; pentosan polysulfate sodium; pentostatin; pentrozole; perflubron; perfosfamide; perillyl alcohol; phenazinomycin; phenylacetate; phosphatase inhibitors; picibanil; pilocarpine hydrochloride; pirarubicin; piritrexim; placetin A; placetin B; plasminogen activator inhibitor; platinum complex; platinum compounds; platinum-triamine complex; porfimer sodium; porfiromycin; propyl bis-acridone; prostaglandin J2; proteasome inhibitors; protein A-based immune modulator; protein kinase C inhibitor; protein kinase C inhibitors, microalgal; protein tyrosine phosphatase inhibitors; purine nucleoside phosphorylase inhibitors; purpurins; pyrazoloacridine; pyridoxylated hemoglobin polyoxyethylene conjugate; raf antagonists; raltitrexed; ramosetron; ras famesyl protein transferase inhibitors; ras inhibitors; ras-GAP inhibitor; retelliptine demethylated; rhenium Re 186 etidronate; rhizoxin; ribozymes; RII retinamide; rohitukine; romurtide; roquinimex; rubiginone Bl; ruboxyl; saintopin; SarCNU; sarcophytol A; sargramostim; Sdi 1 mimetics; senescence derived inhibitor 1; sense oligonucleotides; signal transduction inhibitors; signal transduction modulators; single chain antigen binding protein; sizofuran; sobuzoxane; sodium borocaptate; sodium phenylacetate; solverol; somatomedin binding protein; sonermin; sparfosic acid; spicamycin D; spiromustine; splenopentin; spongistatin 1; squalamine; stem cell inhibitor; stem-cell division inhibitors; stipiamide; stromelysin inhibitors; sulfinosine; superactive vasoactive intestinal peptide antagonist; suradista; suramin; swainsonine; synthetic glycosaminoglycans; tallimustine; tamoxifen methiodide; tauromustine; tazarotene; tecogalan sodium; tegafur; tellurapyrylium; telomerase inhibitors; temozolomide; tetrachlorodecaoxide; tetrazomine; thaliblastine; thalidomide; thiocoraline; thrombopoietin; thrombopoietin mimetic; thymalfasin; thymopoietin receptor agonist; thymotrinan; thyroid stimulating hormone; tin ethyl etiopurpurin; titanocene dichloride; topsentin; toremifene; totipotent stem cell factor; translation inhibitors; tretinoin; triacetyluridine; triciribine; tropisetron; turosteride; tyrosine kinase inhibitors; tyrphostins; UBC inhibitors; ubenimex; urogenital sinus-derived growth inhibitory factor; urokinase receptor antagonists; variolin B; vector system, erythrocyte gene therapy; velaresol; veramine; verdins; vinorelbine; vinxaltine; vitaxin; zanoterone; zilascorb; and zinostatin stimalamer.

[0779] The compounds of the present invention can also be used in combination with any of the following treatments:

[0780] Therapy in combination with inhibitors of Poly(ADP -ribose) polymerases (PARP), a class of chemotherapeutic agents directed at targeting cancers with defective DNA-damage repair (Yuan, et al., Expert Opin Ther Pat, 2017, 27: 363). Such PARP inhibitors include but are not limited to olaparib, rupacarib, velaparib, niraparib, talazoparib, pamiparib, iniparib, E7449, and A-966492.

[0781] Therapy in combination with inhibitors of signaling pathways and mechanisms leading to repair of DNA single and double strand breaks as e.g. nuclear factor-kappaB signaling (Pilie, et al., Nat Rev Clin Oncol, 2019, 16'. 81; Zhang, etal., Chin J Cancer, 2012, 31: 359). Such inhibitors include but are not limited to inhibitors of ATM and ATR kinases, checkpoint kinase 1 and 2, DNA-dependen protein kinase, and WEE1 kinase (Pilie, et al., Nat Rev Clin Oncol, 2019, 16: 81).

[0782] Therapy in combination with an immunomodulator (Khalil, et al., Nat Rev Clin Oncol, 2016, 13: 394), a cancer vaccine (Hollingsworth, et al., NPJ Vaccines, 2019, 4: 7), an immune checkpoint inhibitor (e.g. PD-1, PD-L1, CTLA-4-inhibitor) (Wei, et al., Cancer Di scov, 2018, 8: 1069), a Cyclin-D-Kinase 4 / 6 inhibitor (Goel, et al., Trends Cell Biol, 2018, 28: 911), an antibody being capable of binding to a tumor cell and / or metastases and being capable of inducing antibody-dependent cellular cytotoxicity (ADCC) (Kellner, et al., Transfus Med Hemother, 2017, 44: 327), a T cell- or NK cell engager (e.g. bispecific antibodies) (Yu, et al., J Cancer Res Clin Oncol, 2019, 145: 941), a cellular therapy using expanded autologous or allogeneic immune cells (e.g. chimeric antigen receptor T (CAR-T) cells) (Khalil, et al., Nat Rev Clin Oncol, 2016, 13: 394). Immune checkpoint inhibitors induce but are not limited to nivolumab, ipilimumab, pembrolizumab, atezolizumab, avelumab, durvalumab, and cemiplimab.

[0783] According to the present invention, the compounds may be administered prior to, concurrent with, or following other anti-cancer compounds. The administration schedule may involve administering the different agents in an alternating fashion. In other embodiments, the compounds may be delivered before and during, or during and after, or before and after treatment with other therapies. In some cases, the compound is administered more than 24 hours before the administration of the other anti-proliferative treatment. In other embodiments, more than one anti -proliferative therapy may be administered to a subject. For example, the subject may receive the present compounds, in combination with both surgery and at least one other anti-proliferative compound. Alternatively, the compound may be administered in combination with more than one anti-cancer drug.

[0784] In an embodiment, the compounds of the present invention are used to detect cells and tissues overexpressing P-cad, whereby such detection is achieved by conjugating a detectable label to the compounds of the invention, preferably a detectable radionuclide. In a preferred embodiment, the cells and tissues detected are diseased cells and tissues and / or are either a or the cause for the disease and / or the symptoms of the disease, or are part of the pathology underlying the disease. In a further preferred embodiment, the diseased cells and tissues are causing and / or are part of an oncology indication (e.g. neoplasms, tumors, and cancers).

[0785] In another embodiment, the compounds of the present invention are used to treat cells and tissues overexpressing P-cad. In a preferred embodiment, the cells and tissues treated are diseased cells and tissues and / or are either a or the cause for the disease and / or the symptoms of the disease, or are part of the pathology underlying the disease. In a further preferred embodiment, the diseased cells and tissues are causing and / or are part of an oncology indication (e.g. neoplasms, tumors, and cancers) and the therapeutic activity is achieved by conjugating therapeutically active effector to the compounds of the present invention, preferably a therapeutically active radionuclide.

[0786] An effective amount is a dosage of the compound sufficient to provide a therapeutically or medically desirable result or effect in the subject to which the compound is administered. The effective amount will vary with the particular condition being treated, the age and physical condition of the subject being treated, the severity of the condition, the duration of the treatment, the nature of the concurrent or combination therapy (if any), the specific route of administration and like factors within the knowledge and expertise of the health practitioner. For example, in connection with methods directed towards treating subjects having a condition characterized by abnormal cell proliferation, an effective amount to inhibit proliferation would be an amount sufficient to reduce or halt altogether the abnormal cell proliferation so as to slow or halt the development of or the progression of a cell mass such as, for example, a tumor. As used in the embodiments, “inhibit” embraces all of the foregoing.

[0787] In other embodiments, a therapeutically effective amount will be an amount necessary to extend the dormancy of micrometastases or to stabilize any residual primary tumor cells following surgical or drug therapy.

[0788] In a preferred embodiment, the compound of the present invention is for use in the treatment and / or prevention of a disease, whereby such treatment is targeted radionuclide therapy. Targeted radionuclide therapy is a form of radiation therapy (also called radiotherapy) using molecules labeled with a radionuclide to deliver a toxic level of radiation to sites of disease. Targeted radionuclide therapy may be applied systemically or locally. In contrast, in external beam radiation therapy a source outside of the body is producing a high-energy beam, which is then focused at sites of disease, passing through the skin into the body. It is as well distinguished from internal radiation therapy (brachytherapy), where a radioactive implant is placed at or near the site of disease.

[0789] Preferably, radionuclide therapy makes use of or is based on different forms of radiation emitted by a radionuclide. Such radiation can, for example, be any one of alpha (a), beta (P) or gamma (y) radiation caused by the emission of photons, emission of electrons including but not limited to P'-particles and Auger-electrons, emission of protons, emission of neutrons, emission of positrons or emission of a-particles. Depending on the kind of particle or radiation emitted by said radionuclide, radionuclide therapy can, for example, be distinguished as P-particle radionuclide therapy, a-particle radionuclide therapy or Auger electron radionuclide therapy. All of these forms of radionuclide therapy are encompassed by the present invention, and all of these forms of radionuclide therapy can be realized by the compound of the invention, preferably under the proviso that the radionuclide attached to the compound of the invention, more preferably as an effector, is providing for this kind of radiation.

[0790] Radionuclide therapy preferably works by damaging the DNA of cells. The damage is caused by a P-particle, a-particle, or Auger electron directly or indirectly ionizing the atoms which make up the DNA chain. Indirect ionization happens as a result of the ionization of water, forming free radicals, notably hydroxyl radicals, which then damage the DNA.

[0791] In the most common forms of radionuclide therapy, most of the radiation effect is through free radicals. Because cells have mechanisms for repairing DNA damage, breaking the DNA on both strands proves to be the most significant technique in modifying cell characteristics. Because cancer cells generally are undifferentiated and stem cell-like, they reproduce more, and have a diminished ability to repair sub-lethal damage compared to most healthy differentiated cells. The DNA damage is inherited through cell division, accumulating damage to the cancer cells, causing them to die or reproduce more slowly.

[0792] Oxygen is a potent radiosensitizer, increasing the effectiveness of a given dose of radiation by forming DNA-damaging free radicals. Therefore, use of high-pressure oxygen tanks, blood substitutes that carry increased oxygen, hypoxic cell radiosensitizers such as misonidazole and metronidazole, and hypoxic cytotoxins, such as tirapazamine may be applied.

[0793] The total radioactive dose may be fractionated, i.e. spread out over time in one or more treatments for several important reasons. Fractionation allows normal cells time to recover, while tumor cells are generally less efficient in repair between fractions. Fractionation also allows tumor cells that were in a relatively radio-resistant phase of the cell cycle during one treatment to cycle into a sensitive phase of the cycle before the next fraction is given.

[0794] It is generally known that different cancers respond differently to radiation therapy. The response of a cancer to radiation is described by its radiosensitivity. Highly radiosensitive cancer cells are rapidly killed by modest doses of radiation. These include leukemias, most lymphomas, and germ cell tumors.

[0795] Radionuclide therapy is in itself painless. Many low-dose palliative treatments cause minimal or no side effects. Treatment to higher doses may cause varying side effects during treatment (acute side effects), in the months or years following treatment (long-term side effects), or after re-treatment (cumulative side effects). The nature, severity, and longevity of side effects depends on the organs that receive the radiation, the treatment itself (type of radionuclide, dose, fractionation, concurrent chemotherapy), and the patient.

[0796] It is within the present inventions that the method for the treatment of a disease of the invention may realize each and any of the above strategies which are as such known in the art, and which insofar constitute further embodiments of the invention.

[0797] It is also within the present invention that the compound of the invention is used in a method for the diagnosis of a disease as disclosed herein. Such method, preferably, comprises the step of administering to a subject in need thereof a diagnostically effective amount of the compound of the invention.

[0798] In accordance with the present invention, an imaging method is selected from the group consisting of scintigraphy, Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET).

[0799] Scintigraphy is a form of diagnostic test or method used in nuclear medicine, wherein radiopharmaceuticals are internalized by cells, tissues and / or organs, preferably internalized in vivo, and radiation emitted by said internalized radiopharmaceuticals is captured by external detectors (gamma cameras) to form and display two-dimensional images. In contrast thereto, SPECT and PET forms and displays three-dimensional images. Because of this, SPECT and PET are classified as separate techniques to scintigraphy, although they also use gamma cameras to detect internal radiation. Scintigraphy is unlike a diagnostic X-ray where external radiation is passed through the body to form an image.

[0800] Single Photon Emission Tomography (SPECT) scans are a type of nuclear imaging technique using gamma rays. They are very similar to conventional nuclear medicine planar imaging using a gamma camera. Before the SPECT scan, the patient is injected with a radiolabeled compound emitting gamma rays that can be detected by the scanner. A computer collects the information from the gamma camera and translates this into two-dimensional cross-sections. These crosssections can be added back together to form a three-dimensional image of an organ or a tissue. SPECT involves detection of gamma rays emitted singly, and sequentially, by the radionuclide provided by the radiolabeled compound. To acquire SPECT images, the gamma camera is rotated around the patient. Projections are acquired at defined points during the rotation, typically every 3 - 6 degrees. In most cases, a full 360 degree rotation is used to obtain an optimal reconstruction. The time taken to obtain each projection is also variable, but 15 - 20 seconds is typical. This gives a total scan time of 15 - 20 minutes. Multi-headed gamma cameras are faster. In recent years, several SPECT systems have become available that are composed of stationary rather than rotating detectors. Since SPECT acquisition is very similar to planar gamma camera imaging, the same radiopharmaceuticals may be used.

[0801] Positron Emitting Tomography (PET) is a non-invasive, diagnostic imaging technique for measuring the biochemical, physiological and pathophysiological processes within the human body. PET is unique since it is able to produce images of the body's basic biochemistry or functions. Traditional diagnostic techniques, such as X-rays, CT scans, or MRI, produce images of the body's anatomy or structure. The premise with these techniques is that any changes in structure or anatomy associated with a disease can be seen. Biochemical and physiological processes are also altered by a disease, and may occur before any gross changes in anatomy. PET is an imaging technique that can visualize some of these early biochemical and physiological changes. PET scanners rely on radiation emitted from the patient to create the images. Each patient is given a minute amount of a radioactive compound that either closely resembles a natural substance used by the body or binds specifically to a receptor or molecular structure. As the radioisotope undergoes positron emission decay (also known as positive beta decay), it emits a positron, the antiparticle counterpart of an electron. After traveling up to a few millimeters, the positron encounters an electron and annihilates, producing a pair of annihilation (gamma) photons moving in opposite directions. These are detected when they reach a scintillation material in the scanning device, creating a burst of light, which is detected by photomultiplier tubes or silicon avalanche photodiodes. The technique depends on simultaneous or coincident detection of the pair of photons. Photons that do not arrive in pairs, i.e., within a few nanoseconds, are ignored. All coincidences are forwarded to the image processing unit where the final image data is produced using image reconstruction procedures. SPECT / CT and PET / CT is the combination of SPECT and PET with computed tomography (CT). The key benefits of combining these modalities are improving the reader’s confidence and accuracy. With traditional PET and SPECT, the limited number of photons emitted from the area of abnormality produces a very low-level background that makes it difficult to anatomically localize the area. Adding CT helps determine the location of the abnormal area from an anatomic perspective and categorize the likelihood that this represents a disease.

[0802] It is within the present inventions that the method for the diagnosis of a disease of the invention may realize each and any of the above strategies which are as such known in the art, and which insofar constitute further embodiments of the invention.

[0803] The compound of the invention has a high binding affinity to P-cad. Because of this high binding affinity, the compound of the invention is effective as, useful as and / or suitable as a targeting agent and, if conjugated to another moiety, as a targeting moiety. As preferably used herein a targeting agent is an agent which interacts with the target molecule which is in the instant case said P-cad. In terms of cells and tissues thus targeted by the compound of the invention any cell and tissue, respectively, expressing said P-cad is or may be targeted.

[0804] In an embodiment, the compound interacts with a P-cadherin (P-cad), preferably with human P-cad having an amino acid sequence of SEQ ID NO: 1 or a homolog thereof, wherein the amino acid sequence of the homolog has an identity of P-cad that is at least 85% to the amino acid sequence of SEQ ID NO: 1. In preferred embodiments, the identity is 90%, preferably 95 %, 96 %, 97 %, 98 % or 99%.

[0805] The identity between two nucleic acid molecules can be determined as known to the person skilled in the art. More specifically, a sequence comparison algorithm may be used for calculating the percent sequence homology for the test sequence(s) relative to the reference sequence, based on the designated program parameters. The test sequence is preferably the sequence or protein or polypeptide which is said to be identical or to be tested whether it is identical, and if so, to what extent, to a different protein or polypeptide, whereby such different protein or polypeptide is also referred to as the reference sequence and is preferably the protein or polypeptide of wild type, more preferably the human P-cad of SEQ ID NO: 1.

[0806] Optimal alignment of sequences for comparison can be conducted, e.g., by the local homology algorithm of Smith & Waterman (Smith, el al.. Advances in Applied Mathematics, 1981, 2: 482), by the homology alignment algorithm of Needleman & Wunsch (Needleman, et al, J Mol Biol, 1970, 48: 443), by the search for similarity method of Pearson & Lipman (Pearson, etal., Proc Natl Acad Sci U S A, 1988, 85: 2444), by computerized implementations of these algorithms (GAP, BESTFIT, FASTA, and TFASTA in the Wisconsin Genetics Software Package, Genetics Computer Group, 575 Science Dr., Madison, Wis.), or by visual inspection.

[0807] One example of an algorithm that is suitable for determining percent sequence identity is the algorithm used in the basic local alignment search tool (hereinafter "BLAST "), see, e.g. Altschul et al., 1990 (Altschul, et al., J Mol Biol, 1990, 215: 403) and Altschul et al., 1997 (Altschul, et al., Nucleic Acids Res, 1997, 25: 3389). Software for performing BLAST analyses is publicly available through the National Center for Biotechnology Information (hereinafter "NCBI"). The default parameters used in determining sequence identity using the software available from NCBI, e.g., BLASTN (for nucleotide sequences) and BLASTP (for amino acid sequences) are described in McGinnis et al. (McGinnis, et al., Nucleic Acids Res, 2004, 32: W20).

[0808] Compounds of the present invention are useful to stratify patients, i.e. to create subsets within a patient population that provide more detailed information about how the patient will respond to a given drug. Stratification can be a critical component to transforming a clinical trial from a negative or neutral outcome to one with a positive outcome by identifying the subset of the population most likely to respond to a novel therapy.

[0809] Stratification includes the identification of a group of patients with shared "biological" characteristics to select the optimal management for the patients and achieve the best possible outcome in terms of risk assessment, risk prevention and achievement of the optimal treatment outcome

[0810] A compound of the present invention may be used to assess or detect, a specific disease as early as possible (which is a diagnostic use), the risk of developing a disease (which is a susceptibility / risk use), the evolution of a disease including indolent vs. aggressive (which is a prognostic use) and it may be used to predict the response and the toxicity to a given treatment (which is a predictive use).

[0811] It is also within the present invention that the compound of the invention is used in a theragnostic method. The concept of theragnostics is to combine a therapeutic agent with a corresponding diagnostic test that can increase the clinical use of the therapeutic drug. The concept of theragnostics is becoming increasingly attractive and is widely considered the key to improving the efficiency of drug treatment by helping doctors identify patients who might profit from a given therapy and hence avoid unnecessary treatments.

[0812] The concept of theragnostics is to combine a therapeutic agent with a diagnostic test that allows doctors to identify those patients who will benefit most from a given therapy. In an embodiment and as preferably used herein, a compound of the present invention is used for the diagnosis of a patient, i.e. identification and localization of the primary tumor mass as well as potential local and distant metastases. Furthermore, the tumor volume can be determined, especially utilizing three-dimensional diagnostic modalities such as SPECT or PET. Only those patients having P- cad-positive tumor masses and who, therefore, might profit from a given therapy are selected for a particular therapy and hence unnecessary treatments are avoided. Preferably, such therapy is a P-cad-targeted therapy using a compound of the present invention. In one particular embodiment, chemically identical tumor-targeted diagnostics, preferably imaging diagnostics for scintigraphy, PET or SPECT and radiotherapeutics are applied. Such compounds only differ in the radionuclide and therefore usually have a very similar if not identical pharmacokinetic profile. This can be realized using a chelator and a diagnostic or therapeutic radiometal. Alternatively, this can be realized using a precursor for radiolabeling and radiolabeling with either a diagnostic or a therapeutic radionuclide. In one embodiment diagnostic imaging is used preferably by means of quantification of the radiation of the diagnostic radionuclide and subsequent dosimetry which is known to those skilled in the art and the prediction of drug concentrations in the tumor compared to vulnerable side effect organs. Thus, a truly individualized drug dosing therapy for the patient is achieved.

[0813] In an embodiment and as preferably used herein, the theragnostic method is realized with only one theragnostically active compound such as a compound of the present invention labeled with a radionuclide emitting diagnostically detectable radiation (e.g. positrons or gamma rays) as well as therapeutically effective radiation (e.g. electrons or alpha particles).

[0814] The invention also contemplates a method of intraoperatively identifying / disclosing diseased tissues expressing P-cad in a subject. Such method uses a compound of the invention, whereby such compound of the invention preferably comprises as effector a diagnostically active agent.

[0815] According to a further embodiment of the invention, the compound of the invention, particularly if complexed with a radionuclide, may be employed as adjunct or adjuvant to any other tumor treatment including, surgery as the primary method of treatment of most isolated solid cancers, radiation therapy involving the use of ionizing radiation in an attempt to either cure or improve the symptoms of cancer using either sealed internal sources in the form of brachytherapy or external sources, chemotherapy such as alkylating agents, antimetabolites, anthracyclines, plant alkaloids, topoisomerase inhibitors, and other antitumor agents, hormone treatments that modulate tumor cell behavior without directly attacking those cells, targeted agents which directly target a molecular abnormality in certain types of cancer including monoclonal antibodies and tyrosine kinase inhibitors, angiogenesis inhibitors, immunotherapy, cancer vaccination, palliative care including actions to reduce the physical, emotional, spiritual, and psycho-social distress to improve the patient's quality of life and alternative treatments including a diverse group of health care systems, practices, and products that are not part of conventional medicine.

[0816] In an embodiment of the methods of the invention, the subject is a patient. In an embodiment, a patient is a subject which has been diagnosed as suffering from or which is suspected of suffering from or which is at risk of suffering from or developing a disease, whereby the disease is a disease as described herein and preferably a disease involving P-cad.

[0817] Dosages employed in practicing the methods for treatment and diagnosis, respectively, where a radionuclide is used and more specifically attached to or part of the compound of the invention will vary depending, e.g., on the particular condition to be treated, for example the known radiosensitivity of the tumor type, the volume of the tumor and the therapy desired. In general, the dose is calculated on the basis of radioactivity distribution to each organ and on observed target uptake. A y-emitting complex may be administered once or at several times for diagnostic imaging. In animals, an indicated dose range may be from 0.1 ng / kg to 5 mg / kg of the compound of the invention complexed, e.g., with 1 kBq to 200 MBq of a y-emitting radionuclide, including, but not limited to,n iIn or89Zr. For instance, an indicated dose range of the compound of the invention when complexed with a y-emitting radionuclide may be from 0.2 mg / kg to 2 mg / kg, e.g., from 0.4 mg / kg to 1 mg / kg, such as about 0.6 mg / kg or 0.8 mg / kg. In an embodiment, an indicated dose range of the compound of the invention when complexed with a y-emitting radionuclide is from 0.1 pg / kg to 10.0 pg / kg, e.g., 0.1 pg / kg to 5.0 pg / kg, e.g., 0.1 pg / kg to 2.0 pg / kg such as about 0.5 pg / kg, or 0.8 pg / kg, or 1.0 pg / kg. An y- or P- emitting complex of the compound of the invention may be administered at several time points e.g., 1 dose about every 28 days, e.g., over a period of 1 to 3 weeks or longer e.g., over a period of 16 to 32 weeks. In animals, an indicated dosage range may be of from 0.1 ng / kg to 5 mg / kg of the compound of the invention complexed, e.g., with 1 kBq to 200 MBq of an y- or P-emitting radionuclide, including, but not limited to,225Ac or177Lu. For instance, an indicated dose range of the compound of the invention when complexed with an y- or P-emitting radionuclide may be from 0.2 mg / kg to 2 mg / kg, e.g., from 0.4 mg / kg to 1 mg / kg, such as about 0.6 mg / kg or 0.8 mg / kg. In larger mammals, for example humans, an indicated dosage range is from 0.1 to 100 pg / kg, e.g., 0.1 pg / kg to 10.0 pg / kg, e.g., 0.1 pg / kg to 5.0 pg / kg, e.g., such as about 1.0 pg / kg, or 2.0 pg / kg, or 4.0 pg / kg, of the compound of the invention complexed with, e.g., 10 to 400 MBqU 1ln or89Zr. In larger mammals, for example humans, an indicated dosage range is of from 0.1 ng / kg to 100 pg / kg of the compound of the invention complexed with, e.g., 1 to 100000 MBq of an a- or P-emitting radionuclide, including, but not limited to,225Ac or177Lu. Preferably, in larger mammals, for example humans, an indicated dosage range of the compound of the invention when complexed with a P-emitting radionuclide such as177Lu, e.g., with 200 to 50000 MBq, preferably 500 to 20000 MBq, more preferably 1000 to 15000 MBq, such as 1500 to 10000 MBq of P-emitting radionuclide, is from 0.01 pg / kg to 80 pg / kg, more preferably from 0.1 pg / kg to 50 pg / kg, such as about 1.0 pg / kg to 35 pg / kg, or 2.0 pg / kg to 20 pg / kg. In one aspect, in larger mammals, for example humans, the effective dose resulting from, e.g., the intravenous administration of the compound of the invention complexed with, e.g., 1 to 100000 MBq of an y- or P-emitting radionuclide, including, but not limited to,225Ac or177Lu, is from 0.01 mSv / MBq to 10.0 mSv / MBq, e.g., 0.1 mSv / MBq to 1 mSv / MBq, such as about 0.1 mSv / MBq to 0.5 mSv / MBq, or 0.2 mSv / MBq to 0.3 mSv / MBq. In one further aspect, in larger mammals, for example humans, the effective dose resulting from, e.g., the intravenous administration of the compound of the invention complexed with a P-emitting radionuclide such as177LU is typically less than 5.0 mSv / MBq, more typically less than 2.0 mSv / MBq, even more typically less than 1.0 mSv / MBq, and most typically less than 0.5 mSv / MBq. Furthermore, in this aspect, the effective dose may be 0.05 mSv / MBq or more, e.g., 0.08 mSv / MBq or more, e.g., 0.1 mSv / MBq or more. In an embodiment, the effective dose resulting from, e.g., the intravenous administration of the compound of the invention complexed with a P-emitting radionuclide such as177Lu is less than 1.0 mSv / MBq, e.g., less than 0.5 mSv / MBq, e.g., 0.35 mSv / MBq, such as about 0.25 mSv / MBq. Furthermore, in this embodiment, the effective dose may be 0.1 mSv / MBq or more, e.g., 0.1 mSv / MBq or more, e.g., 0.15 mSv / MBq or more. In another aspect, in larger mammals, for example humans, the radiation dose delivered to a tumor after, e.g., the intravenous administration of the compound of the invention complexed with a P-emitting radionuclide such as177Lu results ranges from about 4.4 to about 660 Gy.

[0818] 4. COMPOSITION, PHARMACEUTICAL COMPOSITION AND KIT

[0819] In a further aspect, the instant invention is related to a composition and a pharmaceutical composition in particular, comprising the compound of the invention.

[0820] The pharmaceutical composition of the present invention comprises at least one compound of the invention and, optionally, one or more carrier substances, excipients and / or adjuvants. The pharmaceutical composition may additionally comprise, for example, one or more of water, buffers such as, e.g., neutral buffered saline or phosphate buffered saline, ethanol, mineral oil, vegetable oil, dimethylsulfoxide, carbohydrates such as e.g., glucose, mannose, sucrose or dextrans, mannitol, proteins, adjuvants, polypeptides or amino acids such as glycine, antioxidants, chelating agents such as EDTA or glutathione and / or preservatives. Furthermore, one or more other active ingredients may, but need not, be included in the pharmaceutical composition of the invention.

[0821] The pharmaceutical composition of the invention may be formulated for any appropriate route of administration, including, for example, topical such as, e.g., transdermal or ocular, oral, buccal, nasal, vaginal, rectal or parenteral administration. The term parenteral as used herein includes subcutaneous, intradermal, intravascular such as, e.g., intravenous, intramuscular, intrathecal and intraperitoneal injection, as well as any similar injection or infusion technique. A preferred route of administration is intravenous administration.

[0822] In an embodiment of the invention the compound of the invention comprising a radionuclide is administered by any conventional route, in particular intravenously, e.g. in the form of injectable solutions or suspensions. The compound of the invention may also be administered advantageously by infusion, e.g., by an infusion of 30 to 60 min.

[0823] Depending on the site of the tumor, the compound of the invention may be administered as close as possible to the tumor site, e.g. by means of a catheter. Such administration may be carried out directly into the tumor tissue or into the surrounding tissue or into the afferent blood vessels. The compound of the invention may also be administered repeatedly in doses, preferably in divided doses.

[0824] According to a preferred embodiment of the invention, a pharmaceutical composition of the invention comprises a stabilizer, e.g., a free radical scavenger, which inhibits autoradiolysis of the compound of the invention. Suitable stabilizers include, e.g., ethanol, A -acetyl cysteine, methionine, ascorbic acid, gentisic acid or derivatives thereof. Ascorbic acid and gentisic acid are preferred.

[0825] A pharmaceutical composition of the invention may comprise further additives, e.g. an agent to adjust the pH between 7.2 and 7.4, e.g. sodium or ammonium acetate or ISfeHPCU. Preferably, the stabilizer is added to the non-radioactive compound of the invention and introduction of the radionuclide, for instance the complexation with the radionuclide, is performed in the presence of the stabilizer, either at room temperature or, preferably, at a temperature of from 40 to 120° C. The complexation may conveniently be performed under air free conditions, e.g., under N2 or Ar. Further stabilizer may be added to the composition after complexation. Excretion of the compound of the invention, particularly if the effector comprises a chelator, essentially takes place through the kidneys. Further protection of the kidneys from radioactivity accumulation may be achieved by administration of lysine or arginine or an amino acid solution having a high content of lysine and / or arginine, e.g., a commercially available amino acid solution such as Synthamin®-14 or -10, prior to the injection of or together with the compound of the invention, particularly if the effector is a radionuclide. Protection of the kidneys may also be achieved by administration of plasma expanders such as, e.g., gelofusine, either instead of or in addition to amino acid infusion. Protection of the kidneys may also be achieved by administration of diuretics providing a means of forced diuresis which elevates the rate of urination. Such diuretics include high ceiling loop diuretics, thiazides, carbonic anhydrase inhibitors, potassium-sparing diuretics, calcium-sparing diuretics, osmotic diuretics and low ceiling diuretics. A pharmaceutical composition of the invention may contain, apart from a compound of the invention, at least one of these further compounds intended for or suitable for kidney protection, preferably kidney protection of the subject to which the compound of the invention is administered.

[0826] It will be understood by a person skilled in the art that the compound of the invention is disclosed herein for use in various methods. It will be further understood by a person skilled in the art that the composition of the invention and the pharmaceutical composition of the invention can be equally used in said various methods. It will also be understood by a person skilled in the art that the composition of the invention and the pharmaceutical composition are disclosed herein for use in various methods. It will be equally understood by a person skilled in the art that the compound of the invention can be equally used in said various methods.

[0827] It will be acknowledged by a person skilled in the art that the composition of the invention and the pharmaceutical composition of the invention contain one or more further compounds in addition to the compound of the invention. To the extent that such one or more further compounds are disclosed herein as being part of the composition of the invention and / or of the pharmaceutical composition of the invention, it will be understood that such one or more further compounds can be administered separately from the compound of the invention to the subject which is exposed to or the subject of a method of the invention. Such administration of the one or more further compounds can be performed prior, concurrently with or after the administration of the compound of the invention. It will also be acknowledged by a person skilled in the art that in a method of the invention, apart from a compound of the invention, one or more further compound may be administered to a subject. Such administration of the one or more further compounds can be performed prior, concurrently with or after the administration of the compound of the invention. To the extent that such one or more further compounds are disclosed herein as being administered as part of a method of the invention, it will be understood that such one or more further compounds are part of a composition of the invention and / or of a pharmaceutical composition of the invention. It is within the present invention that the compound of the invention and the one or more further compounds may be contained in the same or a different formulation. It is also within the present invention that the compound of the invention and the one or more further compounds are not contained in the same formulation, but are contained in the same package containing a first formulation comprising a compound of the invention, and a second formulation comprising the one or more further compounds, whereby the type of formulation may be the same or may be different.

[0828] It is within the present invention that more than one type of a compound of the invention is contained in the composition of the invention and / or the pharmaceutical composition of the invention. It is also within the present invention that more than one type of a compound of the invention is used, preferably administered, in a method of the invention.

[0829] It will be acknowledged that a composition of the invention and a pharmaceutical composition of the invention may be manufactured in conventional manner.

[0830] Radiopharmaceuticals have decreasing content of radioactivity with time, as a consequence of the radioactive deca...

Claims

Claims1. A compound comprising a peptide of formula (I):H - Xaal - Xaa2 - Xaa3 - Xaa4 - Xaa5 - Xaa6 - Xaa7 - Cext (I) or a pharmaceutically acceptable salt thereof, wherein,Xaal is (a) a residue of an a-amino acid comprising a side chain and one N- terminal modification group Nmod covalently attached to the a-nitrogen atom of the amino acid, preferably a residue of an L-a-amino acid comprising a side chain and one N-terminal modification group Nmod covalently attached to the a-nitrogen atom of the amino acid, wherein Nmod is a group containing one or more selected from hydrogen, carbon, nitrogen oxygen and sulfur and optionally comprises a group Zla, wherein the side chain of Xaal optionally comprises a group Zlb, wherein the side chain of Xaal and the a-nitrogen atom of Xaal optionally form a heterocycle, with the proviso that if the side chain of Xaal and the a-nitrogen atom of Xaal form a heterocycle, the N-terminal modification group Nmod is absent, or(b) a residue of an L-a-hydroxy acid comprising a side chain, wherein the side chain optionally comprises a group Zlb,H is a hydrogen atom which is covalently linked to (a) the a-nitrogen atom of Xaal if Xaal is a residue of an a-amino acid comprising a side chain and one N-terminal modification group Nmod covalently attached to the a-nitrogen atom of the amino acid, or (b) the oxygen atom of the a-hydroxy group of Xaal if Xaal is a residue of an L-a-hydroxy acid comprising a side chain,Xaa2 is a residue of an L-a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain comprises an optionally substituted indole or benzothiophene group,Xaa3 is a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z2,Xaa4 is a residue of an L-a-amino acid comprising a hydrophobic side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain of Xaa4 and the a-nitrogen atom of Xaa4 optionally form a heterocycle,Xaa5 is a residue of an a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z3,Xaa6 is a residue of an a-amino acid comprising a side chain, preferably a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z4, wherein the side chain of Xaa6 and the a-nitrogen atom of Xaa6 optionally form a heterocycle,Xaa7 is a residue of an L-a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain comprises an aryl or heteroaryl group, preferably a bicyclic aryl or heteroaryl group,Cext is a moiety covalently attached to the carbonyl group of Xaa7, which is represented by one of the formulae (la), (lb), (Ic), (Id), and (le):Cterm (la)Xaa8 - Cterm (lb)Xaa8 - Xaa9 - Cterm (Ic)Xaa8 - Xaa9 - XaalO - Cterm (Id)Xaa8 - Xaa9 - XaalO - Xaal 1 (le) wherein,Xaa8 is a residue of glycine or a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z5,Xaa9 is a residue of an a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, preferably Xaa9 is a residue of an L-a-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain optionally comprises a group Z6, wherein the side chain of Xaa9 and the a-nitrogen atom of Xaa9 optionally form a heterocycle,XaalO is a residue of an a-amino acid comprising a side chain, preferably a residue of an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a group Z7, wherein the side chain of XaalO and the a-nitrogen atom of XaalO optionally form a heterocycle,Xaal l is a residue of a compound comprising an amino group and optionally comprising a carbonyl group, wherein the amino group is covalently attached to the carbonyl group of XaalO, wherein if the carbonyl group is present, said carbonyl group is covalently attached to a C-terminal modification group Cterm, preferably Xaal 1 is(a) a residue of an a-amino acid comprising a side chain, a C-terminal modification group Cterm and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the side chain optionally comprises a group Z8, wherein the side chain of Xaal l and the a-nitrogen atom ofXaal 1 optionally form a heterocycle, or(b) a residue of an optionally substituted P-amino alcohol, or(c) a residue of a (C1-C6)alkylamine such as cyclohexylamine, or of an (C2- Ce)alkyldiamine such as ethylenediamine,Cterm is a C-terminal modification group, which is selected from the group consisting of -NH2, -OH, a group Z9, and -NHRcterm, wherein Rctermis selected from group consisting of a (Ci-Ce)alkyl group, a benzyl group, a 2-phenylethyl group and a 3 -phenylpropyl group, each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently an effector E, such as a chelator, which may optionally comprise a linker moiety L that covalently links the effector E to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, the effector E being preferably selected from the group consisting of:(a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and(P) a chelator optionally comprising a radionuclide; and(y) a drug, preferably a cytotoxic drug; and(5) an immune cell engaging effector, preferably recruiting and stimulating T cells, natural killer cells (NK cells) and / or phagocytotic cells.

2. The compound or salt of claim 1, wherein at least one, e.g., one, two, three, four, five, six, seven, eight, nine, ten, eleven, twelve or thirteen of Xaal, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO, Xaal 1, Cext and Cterm is defined as follows:Xaal is a residue of formula (Ila) or formula (lib) :wherein, in formula (Ila):Rlais selected from the group consisting of -H, a (Ci-Ce)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl groupand a group of formula -(CH2)bRld, preferably Rlais selected from the group consisting of -H and a group of formula -(CH2)bRld, wherein Rldis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein Rldoptionally comprises a group Zlb, preferably Rldis selected from the group consisting of -H, a polar and a charged group, more preferably Rldis selected from the group consisting of -H, -OH, -CONH2, -COOH, -C(O)Zlb, -NH2, -NH(Zlb), -NH(CH3), -N(CH3)2, -N(CH3)3+, -SO3H, -NH-CONH2, -NH-C(NH)NH2and -NH-C(NH)-NH(CH3), wherein b = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)bRldgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)bRldgroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably b = 1, 2 or 3,Rlbis selected from the group consisting of -H and a methyl group, with the proviso that if Rlais -H, Rlbis -H, preferably Rlbis -H,Xlais selected from the group consisting of -O- and -N(Nmod)-, preferably Xlais -N(Nmod)-, wherein Nmod is selected from the group consisting of -H, -CH2COOH, -CH2CONH2, -CH2C(O)Zla, -(CH2)cNH(Zla), a (Ci- Ce)alkyl group and a group of formula -(CH2)cRle, wherein Rleis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein Rleoptionally comprises a group Zla, preferably Rleis selected from the group consisting of -H, -NH(Zla), a polar and a charged group, more preferably Rleis selected from the group consisting of -H, -OH, -CONH2, -COOH, -NH-CONH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Zla) and -NH-C(NH)NH2, wherein c = 2, 3, 4 or 5, wherein optionally one or two hydrogens of said two, three, four or five -CH2- groups of the -(CH2)cRlegroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)cRlegroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably c = 2 or 3,preferably Nmod is selected from the group consisting of -H, a (C1-C3)alkyl group and -CH2COOH, more preferably Nmod is selected from the group consisting of a methyl group and -CH2COOH, most preferably Nmod is a methyl group, in formula (lib) : a = 1, 2 or 3, preferably a = 1 or 2, more preferably a = 2,Rlcselected from the group consisting of -H, -OH, -F, -NH2 and a (C1-C3)alkyl group, preferably Rlcis -H,Xlbis selected from the group consisting of -CH2-, -CH(OH)-, -CH(F)-, -CH(NH2)-, -CH(NHRlg)-, -NH-, -S-, -SO-, -SO2- and -O-, wherein Rlgis a methyl, an acetyl (Ac) or a group Zlb, preferably Xlbis -CH2-, preferably Xaal is a residue of an M-methyl-I.-a-amino acid, an M-(carboxymethyl)- L-a-amino acid, iminodiacetic acid (Ida) or (5)-piperidine-2-carboxylic acid (Pip), more preferably Xaal is a residue of an amino acid selected from the group consisting of Pip, N-methyl-glycine (Nmg), N-methyl-I.-alanine (Nma), N-methyl-L-serine (Nms), N- methyl-L-aspartic acid (Nmd), N-methyl-I.-glutamic acid (Nme), M-methyl-I.-lysine (Nmk), M-methyl-M-methyl-I.-lysine (Nmk(Me)), M-methyl-M,M-dimethyl-I.-lysine (KMe3a), Na- methyl-M,M,M-trimethyl-I.-lysine (KMe4), M-methyl-I.-ornithine (Nmo), M-methyl-M- methyl-L-omithine (Nmo(Me)), M-(carboxymethyl)-I.-ornithine (Cmo), M-(carboxymethyl)- M-methyl-I.-ornithine (Cmo(Me)), (S)-4-amino-2-(methylamino)butanoic acid (Mdab), N- (carboxymethyl)-L-alanine (Mida), (S')-2,4-bis(methylamino)butanoic acid (Mdab(Me)), CS')-3- amino-2-(methylamino)propanoic acid (Mdap), (5)-2,3-bis(methylamino)propanoic acid (Mdap(Me)), (S)-azepane-2-carboxylic acid (Azp), (S)-morpholine-3 -carboxylic acid (Mor) and Ida, most preferably Xaal is a residue of an amino acid selected from the group consisting of Pip and Nma,Xaa2 is a residue of an amino acid of formula (III):wherein, in formula (III):R2ais selected from the group consisting of H and a (C1-C2)alkyl group, preferably R2ais selected from the group consisting of -H and a methyl group, more preferably R2ais -H,R2band R2care each independently selected from the group consisting of -H and a methyl group,R2dand R2eare each independently selected from the group consisting of -H, -OH, -F, -Cl and a methyl group,R2f, R2gand R2hare each independently selected from the group consisting of -H and -F, preferably each of R2b, R2c, R2d, R2e, R2f, R2gand R2his -H, preferably Xaa2 is a residue of an amino acid selected from the group consisting of Trp, 7-chloro-L -tryptophan (7Clw), 7-methyl-L -tryptophan (7Mw), 7-fluoro-L -tryptophan (7Fw), (2S, 35)-P-methyl-L -tryptophan (Bmw) and N-methyl-L -tryptophan (Nmw), more preferably Xaa2 is a residue of Trp,Xaa3 is a residue of an amino acid of formula (IV):wherein, in formula (IV):R3aand R3b(a) are each independently selected from the group consisting of -H, -F and a (C1-C2)alkyl group, or(b) form together a 3-, 4-, 5- or 6-membered carbocycle or heterocycle, preferably a 3-, 4- or 5-membered carbocycle, preferably R3aand R3bare each independently selected from the group consisting of H and a methyl group,R3cis selected from the group consisting of a halogen atom, a polar group, a negatively charged group and an aliphatic group, wherein R3coptionally comprises a group Z2, preferably R3cis selected from the group consisting of -OH, -COOH, -SO3H, -CONH(R3d), -NH-CONH(R3d), -SO2NH(R3d), -F, -Cl, a (Ci-C4)alkyl group, a (C3-C4)carbocycle group and -NH(Z2), wherein R3Cis optionally linked to the P-carbon atom of Xaa3 by a linker comprising one, two or three -CH2- groups and one hydrogen atom of said one, two, or three -CH2- groups that link R3cto the P-carbon atom of Xaa3 is optionally replaced by a substituent selected from the group consisting of -F, -OH, -COOH, a methyl group, and / or wherein one of the said -CH2- groups, which is different from the R3cadjacent -CH2- group, is optionally replaced by -O-, -S-, -SO- or -SO2-, wherein R3dis selected from the group consisting of -H, a methyl group and a (C2- C4)alkyl group, wherein said (C2-C4)alkyl group is optionally substituted by one or two substituents independently selected from the group consisting of -OH, -COOH, -SO3H and -CONH2, more preferably R3cis selected from the group consisting of a methyl group, -COOH, -CONH2and -SO3H and R3cis optionally linked to the P-carbon atom of Xaa3 by one -CH2- group, most preferably R3cis selected from the group consisting of -COOH and -SO3H and the optional linker is absent, preferably Xaa3 is a residue of an amino acid selected from the group consisting of Asp, L-cysteic acid (Cya), P,P-dimethyl-L-aspartic acid (Dmd), P,P-dimethyl-L-cysteic acid (Penox), Glu, Vai and Asn, more preferably Xaa3 is a residue of an amino acid selected from the group consisting of Penox, Asp and Cya,Xaa4 is a residue of an amino acid of formula (V):wherein, in formula (V):R4ais selected from the group consisting of -H and a (C1-C3)alkyl group, preferably R4ais selected from the group consisting of -H and a methyl group,R4bis selected from the group consisting of a (C3-Cs)alkyl group, a (C3-C7)carbocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)dR4c, wherein one or two hydrogen atoms of R4bare optionally replaced by atoms or groups each and independently selected from the group consisting of -NH2, -OH, a halogen atom and a (Ci- C3)alkyl group, preferably -F, -Cl or a methyl group, preferably R4bis selected from the group consisting of a (C3-Cs)alkyl group, a (C5-Ce)carbocycle, a phenyl group, a 2-thienyl group and a group of formula -(CH2)dR4c, wherein d = 1, 2 or 3, preferably d = 1, wherein R4cis selected from the group consisting of a (C3-C7)carbocycle, an aryl group and a heteroaryl group, wherein one or two hydrogen atoms of R4Care optionally replaced by atoms or groups each and independently selected from the group consisting of -NH2, -OH, a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, preferably R4cis selected from the group consisting of a (C4-Ce)carbocycle, a phenyl group and a 2-thienyl group, and wherein one -CH2- group of R4bis optionally replaced by an atom selected from the group consisting of -O- and -S-, or alternatively, R4aand R4bform together an optionally up to two-fold substituted 5-, 6-, or 7-membered heterocycle, wherein each substituent is each and independently selected from the group consisting of a (Ci- C3)alkyl group, a halogen atom, -NH2 and -OH, preferably R4aand R4bform together a 6-membered unsubstituted heterocycle,preferably Xaa4 is a residue of an amino acid selected from the group consisting of L-neopentyl-glycine (Npg), V-methyl-I.-neopentyl-glycine (Mnpg), Leu, A-m ethyl -L -leucine (Nml), L-homoleucine (Hie), Phe, L-y-ethyl-leucine (Gel), V-methyl-L-y-ethyl-leucine (Mgel), L-norleucine (Nle), V-methyl-L-norleucine (NMB), L-cyclobutyl-alanine (Cba), L-cyclopentyl- alanine (Cpa), L-cyclohexyl-alanine (Cha), L-cyclopentyl-glycine (Cpg) and L-cyclohexyl- glycine (Chg), more preferably Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Leu, Mnpg, Nml, and Chg, even more preferably Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, most preferably Xaa4 is a residue of Npg,Xaa5 is a residue of an amino acid of formula (Via) or (VIb):wherein, in formula (Via):R5ais selected from the group consisting of -H, a (Ci-Ce)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)fR5c, preferably R5aselected from the group consisting of -H and a group of formula -(CH2)fR5c, wherein R5cis selected from the group consisting of -H, a polar, a charged and a hydrophobic group, wherein R5coptionally comprises a group Z3, preferably R5cis selected from the group consisting of -H, -NH(Z3), -C(O)Z3, a polar group and a charged group, more preferably R5Cis selected from the group consisting of -H, -OH, -CONH2, -COOH, -C(O)Z3, -NH-CONH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Z3), -NH-C(NH)NH2and -NH-C(NH)-NH(CH3), wherein f = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)fR5cgroup are replaced by a methyl group, and / or wherein one -CH2- groupof the -(CH2)fR5cgroup which is different from the terminal -CH2- groups of is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably f = 1, 2, 3 or 4,R5bis selected from the group consisting of -H and a group of formula -(CH2)gR5d, wherein R5dis selected from the group consisting of -H, a polar, a charged and a hydrophobic group, wherein R5doptionally comprises a Z3group, preferably R5dis selected from the group consisting of -H, a polar group and a charged group, more preferably R5dis selected from the group consisting of -H, -OH, -CONH2, -COOH, -SO3H, -NH2, -NH(CH3), -N(CH3)2 and -N(CH3)3+, most preferably R5dis selected from the group consisting of -H and -OH, wherein g = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)gR5dgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)gR5dgroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably R5bis selected from the group consisting of -H and a methyl group, preferably g = 1, 2, 3 or 4, more preferably g = 1 or 2, in formula (VIb): e = 0, 1, 2 or 3, preferably e = 2,X5is absent or selected from the group consisting of -N(R5e)-, -O-, -S- , -SO-, -SO2- and -CH2-, wherein R5eis selected from the group consisting of -H, -Ac, (Ci- C3)alkyl group and a group Z3, preferably R5eis selected from the group consisting of -H, a methyl group and a group Z3, more preferably R5eis a group Z3, wherein optionally one or two hydrogen atoms of any -CH2- groups that form the side chain are each and individually replaced by -F or a methyl group, preferably X5is selected from the group consisting of -N(R5e)-, -O- and -CH2-, more preferably X5is -N(R5e)-,preferably Xaa5 is a residue of an a,a-dialkylamino acid of formula (Via), an L-a-amino acid of formula (Via) comprising a polar or charged side chain, or an amino acid of formula (VIb), more preferably Xaa5 is a residue of an amino acid selected from the group consisting of 2-aminoisobutyric acid (Aib), a-methyl-serine (Ams), a-methyl-lysine (Amk), (5)-2,3- diaminopropionic acid (Dap), (5)-2,4-diaminobutyric acid (Dab), L-omithine (Orn), Lys, Ns- methyl-L-omithine (Om(Me)), M>,M>-dimethyl-I.-ornithine (0Me2),A / s-timethyl-L- ornithine (0Me3), M-methyl-I.-lysine (Lys(Me)), M,M-dimethyl-I.-lysine (KMe2), NE,NE,NE- trimethyl-L-lysine (KMe3), Gly, Ala, Ser, 4-amino-tetrahydropyran-4-carboxylic acid (Thp), 4- amino-piperidine-4-carboxylic acid (Ape), 1 -amino- 1 -cyclohexane carboxylic acid (Egz), Apc(Z3), Lys(Z3), Om(Z3), Dab(Z3) and Dap(Z3), most preferably Xaa5 is a residue of an amino acid selected from the group consisting of Aib, Ams, Thp, Ape, Lys(Z3), Om(Z3) and Apc(Z3),Xaa6 is a residue of an amino acid of formula (Vila), (VHb) or (Vile):wherein, in formula (Vila):R6ais selected from the group consisting of -H and a group of formula - (CH2)kR6d, wherein R6dis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein R6doptionally comprises a group Z4, preferably R6dis selected from the group consisting of -H, a polar group and a charged group, more preferably R6dis selected from the group consisting of -H, -OH, -CONH2, -COOH, -SO3H, -NH2, -NH(CH3), -N(CH3)2and -N(CH3)3+, most preferably R6dis selected from the group consisting of -H, -OH, -CONH2and -COOH, wherein k = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)kR6dgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)kR6dgroup which is different from theterminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably k = 1, 2 or 3, more preferably k = 1 or 2, preferably R6ais selected from the group consisting of -H and a methyl group, more preferably R6ais -H,R6bis selected from the group consisting of -H, a (Ci-Ce)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)mR6e, preferably R6bis selected from the group consisting of -H and a group of formula -(CH2)mR6e, wherein R6eis selected from the group consisting of -H, a polar, a charged and a hydrophobic group, wherein R6eoptionally comprises a group Z4, preferably R6eis selected from the group consisting of -H, -NH(Z4), -C(O)Z4, a polar group and a charged group, more preferably R6eis selected from the group consisting of -H, -OH, -CONH2, -COOH, -C(O)Z4, -NH-CONH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Z4) and -NH-C(NH)NH2and -NH-C(NH)-NH(CH3), wherein m = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)mR6egroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)mR6egroup which is different from the terminal -CH2- groups of is optionally replaced by -O-, -S-, -SO- or -SO2- , preferably m = 1, 2, 3 or 4, in formula (VHb): h = 0, 1, 2 or 3, preferably h = 2,X6ais absent or selected from the group consisting of -NR6f-, -O-, -S- , -SO-, -SO2- and -CH2-, wherein R6fis selected from the group consisting of -H, -Ac, (Ci- C3)alkyl group and a group Z4, preferably R6fis selected from the group consisting of -H, a methyl group and a group Z4, more preferably R6fis a group Z4, wherein optionally one or two hydrogen atoms of any of the -CH2- groups that form the side chain are each and individually substituted by -F or a methyl group,preferably X6ais selected from the group consisting of -N(R6f)-, -O- and -CH2-, more preferably X6ais -N(R6f)-, in formula (Vile):R6Cis selected from the group consisting of -H, -OH, -F, -NH2, a (Ci- C3)alkyl group, preferably R6cis -H,X6bis selected from the group consisting of -CH(R6g)-, -S-, -O-, -NH-, preferably X6bis -CH(R6g)-, wherein R6gis selected from the group consisting of -H, -OH, -F, -NH2 and a (C1-C3)alkyl group, preferably R6gis -H, i = 1 or 2, preferably i = 1, preferably Xaa6 is a residue of an L-amino acid amino acid of formula (Vila), and more preferably Xaa6 is a residue of an L-amino acid of formula (Vlld):wherein, in formula (Vlld):R6bis selected from the group consisting of -Hand a group of formula - (CH2)mR6e, wherein R6eis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein R6eoptionally comprises a group Z4, preferably R6eis selected from the group consisting of -H, -NH(Z4), a polar and a charged group, more preferably R6eis selected from the group consisting of -H, -OH, -CONH2, -COOH, -C(O)Z4, -NH-CONH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Z4) and -NH-C(NH)NH2and -NH-C(NH)-NH(CH3), wherein m = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)mR6egroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)mR6egroup which is different from theterminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably m = 1, 2, 3 or 4, more preferably m = 1 or 2, preferably Xaa6 is a residue of an amino acid selected from the group consisting of Asn, Asp, Glu, Gin, Cya, Lys, Lys(Me), Om, Orn(Me), Dab, Dab(Me), Gly, Ala, Thr, Ser, Leu, Tyr, Ape, Lys(Z4) and Apc(Z4), more preferably Xaa6 is a residue of an amino acid selected from the group consisting of Ala, Asn, Asp, Cya, Lys, Lys(Z4), Lys(Me), Thr and Ser, and most preferably a residue of Asn,Xaa7 is a residue of an amino acid of formula (Villa) or of formula (Vlllb):(Vlllb) wherein, in formula (Villa):R7ais selected from the group consisting of -H and a (C1-C2)alkyl group, preferably R7ais -H or a methyl group, more preferably R7ais -H,R7band R7care each independently selected from the group consisting of -H and a methyl group, preferably R7band R7care -H,R7d, R7e, R7fand R7hare each independently selected from the group consisting of -H, -OH, a (C1-C2)alkyl group, -OCH3 and a halogen atom, preferably R7d, R7e, R7fand R7hare each independently selected from the group consisting of -H, -F, -Cl, -Br and a methyl group, more preferably R7d, R7eand R7hare each independently selected from the group consisting of -H, -F, -Cl and a methyl group, most preferably R7d, R7eand R7hare -H, and R7fis selected from the group consisting of -Br and -Cl, R7gis selected from the group consisting of -H, -F and -Cl, more preferably R7gis selected from the group consisting of -H and -F, most preferably R7gis -H,X7aselected from the group consisting of -NH- and -S-, preferably X7ais -NH-, in formula (Vlllb):R7ais selected from the group consisting of -H and a (C1-C2)alkyl group, preferably R7ais -H or a methyl group, more preferably R7ais -H,R7band R7care each independently selected from the group consisting of -H and a methyl group, preferably R7band R7care -H,R71and R7kare each independently selected from the group consisting of -H, -OH, a methyl group, -OCH3 and a halogen atom, preferably R71and R7kare each independently selected from the group consisting of -H, -F, -Cl and a methyl group, more preferably R71and R7kare -H,X7bselected from the group consisting of -CH= and -N=, preferably X7bis -CH=, preferably Xaa7 is a residue of an amino acid selected from the group consisting of Trp,-chloro-L -tryptophan (6Clw), L-6-methyl-tryptophan (6Mw), 5-chloro-L -tryptophan (5Clw),-benzothienyl-L-alanine (Bta), 3-(l-naphthyl)-L-alanine (INi), 5 -fluoro-L -tryptophan (5Fw),-fluoro-L -tryptophan (6Fw), 7Fw and 6-bromo-L -tryptophan (Brw6), more preferably Xaa7 is a residue of an amino acid selected from the group consisting of 6Clw and Brw6,Xaa8 is a residue of an amino acid of formula (IX):wherein, in formula (IX):R8ais selected from the group consisting of -H and a group of formula - (CH2)nR8b, wherein R8bis selected from the group consisting of -H, a polar, a charged and a hydrophobic group, wherein R8boptionally comprises a group Z5, preferably R8bis selected from the group consisting of -H,-NH(Z5), -C(O)Z5, a polar group and a charged group, more preferably R8bcomprises a positively charged group, and even more preferably R8bis selected from the group consisting of -N(R8c)(R8d), -N(CH3)2(R8e)+, -NH(Z5), -N(R8f)-C(N(R8g))-N(R8h)(R81) and a piperidinyl group, wherein R8c, R8d, R8f, R8g, R8hand R8iare each independently selected from the group consisting of -H and a (C1-C3)alkyl group, preferably R8cand R8dare each independently selected from the group consisting of -H and a methyl group, wherein R8eis selected from the group consisting of a (C1-C3)alkyl group and -(CEh^SOf, most preferably R8bis selected from the group consisting of -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH-C(NH)-NH2, -NH-C(NH)-NH(CH3), -NH-C(NH)-N(CH3)2and -NH-C(N(CH3))NH(CH3), wherein n = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of the -(CH2)nR8bgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)nR8bgroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably n = 1, 2, 3 or 4, more preferably n = 3 or 4, preferably Xaa8 is a residue of an amino acid selected from the group consisting of Lys, Lys(Me), KMe2, KMe3, (5)-3-((5-amino-5-carboxypentyl)dimethylammonio)propane-l- sulfonate (Kzw), Lys(Z5), 3-(4-piperidinyl)-L-alanine (Egg), Arg, A® -methyl -L-argi nine (Arg(Me)), A®,A®-dimethyl-L-arginine (RMe2), L-homoarginine (Har), Orn, Orn(Me), 0Me2, 0Me3, y-(2-pyridyl)-L-omithine (Opy), L-homolysine (Hly), L-citrulline (Cit), Gin, L -homocitrulline (Hci), A®,A® -dimethyl-L-arginine (Egd) and M-iso-propyl-I.-lysine (Kip), more preferably Xaa8 is a residue of an amino acid selected from the group consisting of Lys(Me), KMe2, KMe3, Kzw, Egg, Lys(Z5), Arg(Me) and RMe2, and most preferably a residue of KMe3,Xaa9 is a residue of an amino acid of formula (Xa) or (Xb):wherein, in formula (Xa):R9ais selected from the group consisting of -H and (C1-C2)alkyl group, preferably R9ais -H,R9bis selected from the group consisting of -H and a group of formula -(CH2)0R9e, wherein R9eis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein R9eoptionally comprises a group Z6, preferably R9eis selected from the group consisting of -H, an aryl group, a heteroaryl group, a polar group and a charged group, more preferably R9eis selected from the group consisting of -H, an aryl group, a heteroaryl group, -OH, -CONH2, -COOH, -NH-CONH2, -SO3H, -NH2, -NH(CH3), -N(CH3)2, -N(CH3)3+, -NH(Z4) and -NH- C(NH)NH2, most preferably R9eis selected from the group consisting of -H, a methyl group, an aryl group and a heteroaryl group, wherein said aryl group or heteroaryl group is optionally substituted by 1 or 2 substituents, preferably 1 substituent, wherein, preferably, each substituent is independently selected from the group consisting of a halogen atom, a (C1-C3)alkyl group, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C3)alkyl group, wherein each substituent is optionally linked, preferably via a methylene group, to the aryl group or heteroaryl group, and wherein said group aryl group or heteroaryl group preferably comprises one aromatic ring, wherein o = 1, 2, 3 or 4, wherein optionally one or two hydrogen atoms of said one, two, three or four -CH2- groups of the -(CH2)0R9egroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)0R9egroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably o = 1 or 2, more preferably o = 1,R9Cis selected from the group consisting of -H and methyl group, with the proviso that if R9bis -H, R9cis -H, preferably R9cis -H, in formula (Xb):R9dis selected from the group consisting of -H, -OH, -F, -NH2, a (Ci- C3)alkyl group, preferably R9dis -H,X9is selected from the group consisting of -CH(R9f)-, -S-, -O-, -NH-, preferably X9is -CH(R9f)-, wherein R9fis selected from the group consisting of -H, -OH, -F, -NH2 and a methyl group, preferably R9fis -H, p = 1 or 2, preferably p = 1, preferably Xaa9 is a residue of an amino acid selected from the group consisting of Gly, Ala, Dab, Glu, Pro, 4-carbamoyl-L-phenylalanine (Pcnf), Lys(Z6) and Tyr, more preferably Xaa9 is a residue of an amino acid selected from the group consisting of Ala and Tyr,XaalO is a residue of formula (Xia) or (Xlb):wherein, in formula (Xia):R10ais selected from the group consisting of -H and a group of formula -(CH2)rR10c, wherein R10cis selected from the group consisting of -H, a polar group, a charged group and a hydrophobic group, wherein R10coptionally comprises a group Z7, preferably R10cis selected from the group consisting of -NH(Z7), a polar group and a charged group, more preferably R10cis a negatively charged group, most preferably R10cis selected from the group consisting of -COOH and -SO3H, wherein r = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)rR10cgroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)rR10cgroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably r = 1, 2, 3 or 4, more preferably r = 1 or 2,in formula (Xlb):R10bis selected from the group consisting of -H, -OH, -F, -NH2, a (Ci- C3)alkyl group, preferably R10bis -H,X10is selected from the group consisting of -CH(R10d)-, -S-, -O-, -NH-, preferably X9is -CH(R10d)-, wherein R10dis selected from the group consisting of -H, -OH, -F, -NH2 and a methyl group, preferably R10dis -H, q = 1 or 2, preferably q = 1, preferably XaalO is a residue of an amino acid selected from the group consisting of Asp, Cya, Glu, Ser, Lys and Thr, more preferably XaalO is a residue of an amino acid selected from the group consisting of Asp and Cya,Xaal l is a residue of formula (Xlla):R11 a^N^,R11 dR11 bR11 c(Xlla) wherein, in formula (Xlla):Rl lais selected from the group consisting of -H and a (C1-C2)alkyl group, preferably Rllais -H,Rl lbis selected from the group consisting of -H, a ((C1-C)8)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)sRl le, wherein Rl leis selected from the group consisting of a polar group, a charged group and a hydrophobic group, wherein Rl leoptionally comprises a group Z8, preferably Rl leis a hydrophobic group, more preferably Rlleis selected from the group consisting of an aryl group and a heteroaryl group, wherein s = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)sRl legroup are replaced by a methyl group, and / or wherein one -CH2- groupof the -(CH2)sRllegroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably s = 1, 2 or 3, more preferably s = 1, or alternatively, Rl laand Rllbform together an optionally up to two-fold substituted 5-, 6-, or 7-membered heterocycle, wherein each substituent is each and independently selected from the group consisting of a (Ci- C3)alkyl group, a halogen atom, -NH2 and -OH, preferably Rl laand Rllbform together a 5- or 6-membered heterocycle,Rl lcis selected from the group consisting of -H and a (C1-C2)alkyl group, preferably Rllcis -H, or alternatively, Rllband Rl lcform together an optionally substituted 3-, 4-, 5-, 6- or 7-membered carbocycle or heterocycle, preferably a 6- membered carbocycle, wherein each substituent is independently selected from the group consisting of a (C1-C2)alkyl group, a halogen atom, -NH2 and -OH,Rl ldis selected from the group consisting of -H, a (C1-C2)alkyl group, -CH2(0H) and -C(O)-Cterm, preferably Rlldis -C(O)-Cterm, preferably Xaal l is a residue of formula (Xllb) or (XIIc):wherein in formula (XHb):Rl lais selected from the group consisting of -H and a (C1-C2)alkyl group, preferably Rllais -H,Rl lbis selected from the group consisting of -H, a ((C1-C)8)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, an aryl group, a heteroaryl group and a group of formula -(CH2)sRlle, wherein Rl leis selected from the group consisting of a polar group, a charged group and a hydrophobic group, wherein Rl leoptionally comprises a group Z8, preferably Rl leis a hydrophobic group, more preferably Rlleis selected from the group consisting of an aryl group anda heteroaryl group, wherein said aryl group or heteroaryl group is optionally substituted by atoms or groups each and independently selected from the group consisting of -NH2, -OH, -CN, -CONH2, -OCH3, a halogen atom and a (C1-C3)alkyl group, wherein s = 1, 2, 3, 4 or 5, wherein optionally one or two hydrogen atoms of said one, two, three, four or five -CH2- groups of the -(CH2)sRl legroup are replaced by a methyl group, and / or wherein one -CH2- group of the -(CH2)sRllegroup which is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-, preferably s = 1, 2 or 3, more preferably s = 1,Rl lcis selected from the group consisting of -H and a (C1-C2)alkyl group, with the proviso that if Rl lbis -H, Rl lcis -H, preferably Rllcis -H, or alternatively, Rllband Rl lcform together an optionally substituted 3-, 4- , 5-, 6- or 7-membered carbocycle or heterocycle, preferably a 6- membered carbocycle, wherein each substituent is independently selected from the group consisting of a (C1-C2)alkyl group, a halogen atom, -NH2 and -OH,Cterm is selected from the group consisting of -NH2, -OH, -NHRctermand a group Z9, wherein Rctermis selected from group consisting of a (Ci- Ce)alkyl group, a benzyl group, a 2-phenylethyl group and a 3- phenylpropyl group, preferably Cterm is NH2, in formula (XIIc):Rl lfis selected from the group consisting of -H, -OH, -F, -NH2, a (Ci- C3)alkyl group, preferably Rllfis -H,X11is selected from the group consisting of -CH(Rllg)-, -S-, -O-, -NH-, preferably X10is -CH(Rllg)-, wherein Rllgis selected from the group consisting of -H, -OH, -F, -NH2 and a methyl group, preferably Rllgis -H, t = 1, 2 or 3, preferably t = 1 or 2,Cterm is selected from the group consisting of -NH2, -OH, -NHRctermand a group Z9, wherein Rctermis selected from group consisting of a (Ci- Ce)alkyl group, a benzyl group, a 2-phenylethyl group and a 3- phenylpropyl group, preferably Cterm is NH2,more preferably Xaal l is a residue of an L-a-amino acid of formula (Xllb), wherein Rl lbis a group of formula -CH2Rl le, wherein Rlleis selected from the group consisting of an aryl group and a heteroaryl group, preferably a phenyl group or a 2-thienyl group, wherein said aryl group or heteroaryl group is optionally substituted by one or more, e.g., one, two or three, atoms or groups each and independently selected from the group consisting of -NH2, -OH, - CN, -CONH2, -OCH3, a halogen atom and a (C1-C3)alkyl group, preferably the aryl group or heteroaryl group is unsubstituted or has one substituent, and wherein preferably Cterm is NH2, even more preferably Xaal l is a residue of an amino acid selected from the group consisting of Thi, Phe, Egz, ortho-chloro-phenylalanine (Ocf), 3-(l-naphthyl)alanine (INi), 3- fluoro-phenylalanine (Mff), 2-cyano-L-phenylalanine (Onf), 2-fluoro-L-phenylalanine (Off), Ala and Vai, with Cterm being preferably -NH2, and even more preferably Xaal l is a residue of an amino acid selected from the group consisting of Thi, Phe and Ocf, with Cterm being preferably -NH2, most preferably Xaal 1 is Thi, with Cterm being preferably -NH2,Cext is a moiety of formula (le), andCterm is selected from the group consisting of -NH2, -OH, -NHRctermand a group Z9, wherein Rctermis selected from group consisting of a (Ci-Ce)alkyl group, a benzyl group, a 2- phenylethyl group and a 3 -phenylpropyl group, preferably Cterm is NH2, in the above formulae, each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently an effector E, such as a chelator, which may optionally comprise a linker moiety L that covalently links the effector E to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, the effector E being preferably selected from the group consisting of:(a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and(P) a chelator optionally comprising a radionuclide; and(y) a drug, preferably a cytotoxic drug; and(5) an immune cell engaging effector, preferably recruiting and stimulating T cells, NK cells and / or phagocytotic cells.

3. The compound or salt of claim 1 or 2, wherein at least one, e.g., one, two, three, four, five, six, seven, eight, nine, ten, eleven, twelve or thirteen, of Xaal, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO, Xaal 1, Cext and Cterm is / are defined as follows:(a) Xaal is a residue of an M-methyl-L-a-amino acid, an M-(carboxymethyl)-L-a-amino acid,, Ida or Pip, preferably a residue of an amino acid selected from the group consisting of Pip, Nmg, Nma, Nms, Nmd, Nme, Nmk, Nmk(Me), KMe3a, KMe4, Nmo, Nmo(Me), Cmo, Cmo(Me), Mdab, Mdab(Me), Mida, Mdap, Mdap(Me), Azp, Mor and Ida, more preferably a residue of an amino acid selected from the group consisting of Pip and Nma, and still more preferably a residue of Pip,(b) Xaa2 is a residue of an amino acid selected from the group consisting of Trp, 7Clw, 7Mw, 7Fw, Bmw and Nmw, and preferably Xaa2 is a residue of Trp,(c) Xaa3 is a residue of an amino acid selected from the group consisting of Asp, Cya, Glu, Dmd, Penox, Vai and Asn, and preferably a residue of an amino acid selected from the group consisting of Penox, Asp and Cya,(d) Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Mnpg, Leu, Nml, Hie, Phe, Gel, Mgel, Nle, NMB, Cba, Cpa, Cha, Cpg and Chg, preferably a residue of an amino acid selected from the group consisting of Npg, Leu, Mnpg, Nml and Chg, and more preferably a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, and most preferably Xaa4 is a residue of Npg,(e) Xaa5 is a residue of an amino acid selected from the group consisting of Aib, Ams, Amk, Dap, Dab, Om, Orn(Me), 0Me2, 0Me3, Lys, Lys(Me), KMe2, KMe3, Gly, Ala, Ser, Thp, Ape, Egz, Apc(Z3), Lys(Z3), Orn(Z3), Dab(Z3) and Dap(Z3), and preferably a residue of an amino acid selected from the group consisting of Aib, Ams, Thp, Ape, Lys(Z3), Orn(Z3) and Apc(Z3), wherein Z3is preferably selected from the group consisting of DOTA, DOTAM, PSC, DOTAGA, NOPO, NODAGA, BnTCMC, DOTAMGAM, PSCGA and NOTA, more preferably Xaa5 is a residue of an amino acid selected from the group consisting of Apc(DOTA), Apc(DOTAM), Apc(PSC), Apc(DOTAGA), Apc(NOPO), Apc(NODAGA), Apc(PSCGA), Apc(BnTCMC), Apc(DOTAMGAM), Apc(PSCGA) and Apc(NOTA),(f) Xaa6 is a residue of an amino acid selected from the group consisting of Asn, Asp, Glu, Gin, Cya, Lys(Me), Orn, Orn(Me), Dab, Dab(Me), Gly, Ala, Thr, Ser, Leu, Tyr, Ape,Lys(Z4) and Apc(Z4), wherein Z4is preferably selected from the group consisting of DOTA, DOTAM and PSC, and Xaa6 is preferably a residue of an amino acid selected from the group consisting of Ala, Asn, Asp, Cya, Lys, Lys(Z4), Lys(Me), Thr and Ser, and more preferably Xaa6 is a residue of Asn,(g) Xaa7 is a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, and preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6,(h) Xaa8 is a residue of an amino acid selected from the group consisting of Lys, Lys(Me), KMe2, KMe3, Kzw, Egg, Arg, Arg(Me), Lys(Z5), RMe2, Har, Orn, Orn(Me), 0Me2, 0Me3, Opy, Hly, Cit, Gin, Hci, Egd and Kip, wherein Z5is preferably selected from the group consisting of DOTA, DOTAM and PSC, preferably Xaa8 is a residue of an amino acid selected from the group consisting of Lys(Me), KMe2, KMe3, Kzw, Egg, Arg(Me), Lys(Z5) and RMe2, and more preferably a residue of KMe3,(i) Xaa9 is a residue of an amino acid selected from the group consisting of Gly, Ala, Dab, Glu, Pro, Pcnf, Lys(Z6) and Tyr, wherein Z6is preferably selected from the group consisting of DOTA, DOTAM and PSC, and preferably Xaa 9 is a residue of an amino acid selected from the group consisting of Ala and Tyr,(j) XaalO is a residue of an amino acid selected from the group consisting of Asp, Cya, Glu, Thr, Lys and Ser, and preferably a residue of an amino acid selected from the group consisting of Asp and Cya,(k) Xaal 1 is a residue of an amino acid selected from the group consisting of Thi, Phe, Ocf, INi, Mff, Onf, Off, Ala and Vai, preferably a residue of an amino acid selected from the group consisting of Thi, Phe and Ocf, and more preferably a residue of Thi,(l) Cext is a moiety of formula (le), and(m) Cterm is NH2.

4. The compound of any one of claims 1 to 3, wherein at least one, e.g., one, two, three or four, of Xaa2, Xaa4, Xaa7 and Cext is / are defined as follows:(b) Xaa2 is a residue of an amino acid selected from the group consisting of Trp, 7Clw, 7Mw, 7Fw, Bmw and Nmw, and preferably Xaa2 is a residue of Trp, and(d) Xaa4 is a residue of an amino acid selected from the group consisting of Npg, Mnpg, Leu, Nml, Hie, Phe, Gel, Mgel, Nle, NMB, Cba, Cpa, Cha, Cpg and Chg, preferably a residue of an amino acid selected from the group consisting of Npg, Leu, Mnpg, Nml and Chg, more preferably a residue of an amino acid selected from the group consisting of Npg, Mnpg and Nml, and most preferably a residue of Npg, and(g) Xaa7 is a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, and preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6, and(1) Cext is a moiety of formula (le), all Xaa2, Xaa4, Xaa7 and Cext preferably having the meanings defined in the above items (b), (d), (g) and (1).

5. The compound or salt of any one of claims 1 to 4, wherein in formula (I),Xaal - Xaa2 - Xaa3 - Xaa4 is a moiety selected from the group consisting of Pip-Trp- Asp-Npg, Pip-Trp-Cya-Npg, Pip-Trp-Glu-Npg, Pip-Trp-Val-Npg, Pip-Trp-Asn-Npg, Pip-Trp- Dmd-Npg, Pip-Trp-Asp-Leu, Pip-Trp-Cya-Leu, Pip-Trp-Glu-Leu, Pip-Trp-Val-Leu, Pip-Trp- Asn-Leu, Pip-Trp-Dmd-Leu, Pip-Trp-Asp-Chg, Pip-Trp-Cya-Chg, Pip-Trp-Glu-Chg, Pip-Trp- Val-Chg, Pip-Trp-Asn-Chg, Pip-Trp-Dmd-Chg, Pip-Trp-Asp-Nml, Pip-Trp-Cya-Nml, Pip- Trp-Glu-Nml, Pip-Trp-Val-Nml, Pip-Trp-Asn-Nml, Pip-Trp-Dmd-Nml, Pip-Trp-Asp-Mnpg, Pip-Trp-Cya-Mnpg, Pip-Trp-Glu-Mnpg, Pip-Trp-Val-Mnpg, Pip-Trp-Asn-Mnpg, Pip-Trp- Dmd-Mnpg, Nma-Trp-Asp-Npg, Nma-Trp-Cya-Npg, Nma-Trp-Glu-Npg, Nma-Trp-Val-Npg, Nma-Trp-Asn-Npg, Nma-Trp-Dmd-Npg, Nma-Trp-Asp-Leu, Nma-Trp-Cya-Leu, Nma-Trp- Glu-Leu, Nma-Trp-Val-Leu, Nma-Trp-Asn-Leu, Nma-Trp-Dmd-Leu, Nma-Trp-Asp-Chg, Nma-Trp-Cya-Chg, Nma-Trp-Glu-Chg, Nma-Trp-Val-Chg, Nma-Trp-Asn-Chg, Nma-Trp- Dmd-Chg, Nma-Trp-Asp-Nml, Nma-Trp-Cya-Nml, Nma-Trp-Glu-Nml, Nma-Trp-Val-Nml, Nma-Trp-Asn-Nml, Nma-Trp-Dmd-Nml, Nma-Trp-Asp-Mnpg, Nma-Trp-Cya-Mnpg, Nma- Trp-Glu-Mnpg, Nma-Trp-Val-Mnpg, Nma-Trp-Asn-Mnpg, Nma-Trp-Dmd-Mnpg, Pip-Trp- Penox-Npg, Pip-Trp-Penox-Nml, Pip-Trp-Penox-Mnpg, Nma-Trp-Penox-Npg, Nma-Trp- Penox-Nml, Nma-Trp-Penox-Mnpg, Nmo(Me)-Trp-Cya-Mnpg, Nmg-Trp-Cya-Mnpg, Nmo(Me)-Trp-Cya-Nml, Nmg-Trp-Cya-Nml, Nmo(Me)-Trp-Asp-Mnpg, Nmg-Trp-Asp- Mnpg, Nmo(Me)-Trp-Asp-Nml, Nmg-Trp-Asp-Nml, Nmo(Me)-Trp-Asp-Npg, Nmg-Trp-Asp- Npg, Nmo(Me)-Trp-Penox-Npg, Nmg-Trp-Penox-Npg, Nmo(Me)-Trp-Penox-Nml, Nmg-Trp-Penox-Nml, Nmo(Me)-Trp-Penox-Mnpg, Nmg-Trp-Penox-Mnpg, Nmo(Me)-Trp-Cya-Npg, Nmg-Trp-Cya-Npg, Azp-Trp-Cya-Mnpg, Mor-Trp-Cya-Mnpg, Azp-Trp-Cya-Nml, Mor-Trp- Cya-Nml, Azp-Trp-Asp-Mnpg, Mor-Trp-Asp-Mnpg, Azp-Trp-Asp-Nml, Mor-Trp-Asp-Nml, Azp-Trp-Asp-Npg, Mor-Trp-Asp-Npg, Azp-Trp-Penox-Npg, Mor-Trp-Penox-Npg, Azp-Trp- Penox-Nml, Mor-Trp-Penox-Nml, Azp-Trp-Penox-Mnpg, Mor-Trp-Penox-Mnpg, Azp-Trp- Cya-Npg and Mor-Trp-Cya-Npg, preferably Xaal - Xaa2 - Xaa3 - Xaa4 is a moiety selected from the group consisting of Pip- Trp-Asp-Npg, Pip-Trp-Cya-Npg, Pip-Trp-Dmd-Npg, Pip-Trp-Asp-Nml, Pip-Trp-Cya-Nml, Pip-Trp-Dmd-Nml, Pip-Trp-Asp-Mnpg, Pip-Trp-Cya-Mnpg, Pip-Trp-Dmd-Mnpg, Pip-Trp- Penox-Npg, Pip-Trp-Penox-Nml, Pip-Trp-Penox-Mnpg, Nma-Trp-Penox-Npg, Nma-Trp- Penox-Nml, Nma-Trp-Penox-Mnpg, Nma-Trp-Asp-Npg, Nma-Trp-Cya-Npg, Nma-Trp-Dmd- Npg, Nma-Trp-Asp-Nml, Nma-Trp-Cya-Nml, Nma-Trp-Dmd-Nml, Nma-Trp-Asp-Mnpg, Nma-Trp-Cya-Mnpg and Nma-Trp-Dmd-Mnpg, andXaa7 is preferably a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, more preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6.

6. The compound or salt of any one of claims 1 to 5, wherein in formula (I),Xaal - Xaa2 - Xaa3 - Xaa4 is a moiety selected from the group consisting of Pip-Trp- Asp-Npg, Pip-Trp-Cya-Npg, Pip-Trp-Dmd-Npg, Pip-Trp-Asp-Nml, Pip-Trp-Cya-Nml, Pip- Trp-Dmd-Nml, Pip-Trp-Asp-Mnpg, Pip-Trp-Cya-Mnpg, Pip-Trp-Dmd-Mnpg, Pip-Trp-Penox- Npg, Pip-Trp-Penox-Nml, Pip-Trp-Penox-Mnpg, Nma-Trp-Penox-Npg, Nma-Trp-Penox-Nml, Nma-Trp-Penox-Mnpg, Nma-Trp-Asp-Npg, Nma-Trp-Cya-Npg, Nma-Trp-Dmd-Npg, Nma- Trp-Asp-Nml, Nma-Trp-Cya-Nml, Nma-Trp-Dmd-Nml, Nma-Trp-Asp-Mnpg, Nma-Trp-Cya- Mnpg and Nma-Trp-Dmd-Mnpg, andXaa7 is preferably a residue of an amino acid selected from the group consisting of Trp, 6Clw, 6Mw, 5Clw, Bta, INi, 5Fw, 6Fw, 7Fw and Brw6, more preferably a residue of an amino acid selected from the group consisting of 6Clw and Brw6.

7. The compound or salt of claim 5 or 6, wherein at least one, e.g., one, two, three, four, five, six, seven or eight, of Xaa5, Xaa6, Xaa8, Xaa9, XaalO, Xaal l, Cext and Cterm is / are defined as follows:(e) Xaa5 is a residue of an amino acid selected from the group consisting of Aib, Ams, Thp, Ape, Lys(Z3), Orn(Z3) and Apc(Z3), wherein Z3is preferably selected from the group consisting of DOTA, DOTAM, PSC, DOTAGA, NOPO, NODAGA, BnTCMC, DOTAMGAM, PSCGA and NOTA, preferably Xaa5 is a residue of an amino acid selected from the group consisting of Apc(DOTA), Apc(DOTAM), Apc(PSC), Apc(DOTAGA), Apc(NOPO), Apc(NODAGA), Apc(PSCGA), Apc(BnTCMC), Apc(DOTAMGAM), Apc(PSCGA) and Apc(NOTA),(f) Xaa6 is a residue of an amino acid selected from the group consisting of Ala, Asn, Asp, Cya, Lys, Lys(Me), Lys(Z4), Thr and Ser, preferably Xaa6 is a residue of Asn,(h) Xaa8 is a residue of an amino acid selected from the group consisting of Lys(Me), KMe2, KMe3, Kzw, Egg, Arg(Me), Lys(Z5) and RMe2, preferably a residue of KMe3,(i) Xaa9 is a residue of an amino acid selected from the group consisting of Gly, Ala, Dab, Glu, Pro, Pcnf, Lys(Z6) and Tyr, preferably a residue of an amino acid selected from the group consisting of Ala and Tyr,(j) XaalO is a residue of an amino acid selected from the group consisting of Asp, Cya, Glu, Lys, Thr and Ser, preferably a residue of an amino acid selected from the group consisting of Asp and Cya,(k) Xaal l is a residue of an amino acid selected from the group consisting of Thi, Phe and Ocf, preferably a residue of Thi,(l) Cext is a moiety of formula (le), and(m) Cterm is NH2.

8. The compound or salt of any one of claims 1 to 7, which is represented by one of the following formulae:H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys(Me)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe2-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Har-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Asp-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys(Me)-Tyr-Asp-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Pcnf-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Guf-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-enH-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Onf-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Off-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Ser-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Thr-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys-6Clw-KMe3-Tyr-Ser-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys(Me)-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-KMe3-Lys(Z6)-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-Lys(Z5)-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NHMeH-Pip-Trp-Cya-Npg-Orn(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Cya-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Nma-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-KMe4-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-RMe2-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Kip-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Egd-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Om-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Opy-Tyr-Cya-Thi-NH2H-Pip-Trp-Asn-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Kzw-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Egg-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Om-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Ocf-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Mff-NH2H-Pip-Trp-Cya-Npg-Lys-Apc(Z4)-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc-Lys(Z4)-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Mnpg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Dmd-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Nml-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Ida-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Mida-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Mnpg-Om(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Nmg-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Gel-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Thr-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Thr-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Mnpg-Apc(Z3)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Mgel-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Penox-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Nmo(Me)-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Dab(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Mor-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Nmo-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Ser-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Azp-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Phe-NH2 wherein, in the above formulae, en is a residue of ethylenediamine, and each of Z3, Z4, Z5or Z6is independently an effector E which may optionally comprise a linker moiety L, the effector E being preferably selected from the group consisting of:(a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and(P) a chelator optionally comprising a radionuclide; and(y) a drug, preferably a cytotoxic drug; and(5) an immune cell engaging effector, preferably recruiting and stimulating T cells, NK cells and / or phagocytotic cells.

9. The compound or salt of any one of claims 1 to 8, which is represented by one of the following formulae:H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys(Me)-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe2-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Har-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Asp-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Lys(Me)-Tyr-Asp-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2H-Pip-T rp- Asp-Npg- Apc(Z3)- Asn-6C1 w-RMe2-T yr-Cy a-Thi -NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Kip-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Egd-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Om-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Opy-Tyr-Cya-Thi-NH2H-Pip-Trp-Asn-Npg-Apc(Z3)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Pcnf-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Guf-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-enH-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Kzw-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Ocf-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Mff-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Cya-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Nma-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Orn(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Off-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Ser-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Thr-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys(Me)-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-Lys(Z5)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Om(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Nmg-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Gel-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Thr-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mgel-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Penox-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Nmo(Me)-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Dab(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Ser-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Phe-NH2 and preferably by one of the following formulae:H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2 H-Pip-T rp- Asp-Npg- Apc(Z3)- Asn-6C1 w-RMe2-T yr-Cy a-Thi -NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-Kip-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(Z3)-Asn-6Clw-KMe3-Pcnf-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-Kzw-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Ocf-NH2 H-Nma-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Orn(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Lys(Me)-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Om(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Gel-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cy a-Thi -NH2H-Pip-Trp-Cya-Npg-Apc(Z3)-Thr-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Dab(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(Z3)-Asn-6Clw-KMe3-Tyr-Cya-Phe-NH2 wherein, in the above formulae, en is a residue of ethylenediamine, and each group Z3and Z5is independently an effector E which may optionally comprise a linker moiety L, the effector E being preferably selected from the group consisting of:(a) a chromophore, wherein the chromophore is preferably selected from (al) a phosphorophore and (a2) a fluorophore such as fluorescein or rhodamine; and(P) a chelator optionally comprising a radionuclide; and(y) a drug, preferably a cytotoxic drug; and(5) an immune cell engaging effector, preferably recruiting and stimulating T cells, NK cells and / or phagocytotic cells.

10. The compound or salt of any one of claims 1 to 9, wherein each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently a chelator which may optionally comprise a linker moiety L, wherein the chelator comprises a radionuclide, and wherein preferably the chelator is independently a residue of DOTA, DOTAGA, DOTAM, Crown, DOTP, NOTA, NODAGA, NODA-MPAA, HBED, TETA, CB-TE2A, DTP A, CHX-A”-DTPA, DFO, Macropa, HOPO ligand platform, TRAP, THP, AAZTA, DATA, NOPO, PCTA, PSC, sarcophagine, FSC, DEP A, DE4TA, NET A, NE3TA, H4octapa, H4CHXoctapa, H4pypa, H4py4pa, HYNIC, NxS4-x (N4, N2S2, N3S),99mTc(CO)3-chelators.

11. The compound or salt of claim 10, wherein the chelator is a residue of DOTA, DOTAGA, DOTAM, Crown, NOTA, NODAGA, NODA-MPAA, CB-TE2A, CHX-A”- DTPA, DFO, Macropa, THP, AAZTA, NOPO, PCTA, PSC, sarcophagine, NETA, H4CHXoctapa, H4pypa and N4, preferably of DOTA, DOTAGA, DOTAM, NOTA, NODAGA, Macropa, Crown, NOPO, PCTA, PSC and N4, more preferably of DOTA, DOTAM, Macropa, NOTA, PSC or NODAGA, and most preferably of DOTA.

12. The compound or salt of any one of claims 1 to 11, wherein each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently a moiety represented by the following formula (XIII):E-* (XIII) wherein,* indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, andE is a residue represented by any one of the following formulae (XlVa) to (XlVn):wherein,Xci and XC2 are each independently selected from the group consisting of -OH and -NH2, andXC3 is independently selected from the group consisting of -NH-* for attachment to a carbonyl group and -N-C(S)-* for attachment to an N atom of an amino group, and* indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, and the residue E optionally comprises a radionuclide.

13. The compound or salt of any one of claims 1 to 12, wherein each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently a moiety represented by the following formula (XV):E-L-* (XV) wherein,* indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal l, and(a) E is a residue represented by any one of the following formulae (XVIa) to (XVIn) :wherein,Xci and XC2 are each independently selected from the group consisting of -OH and -NH2, and** indicates covalent attachment to L, the residue E optionally comprises a radionuclide, andL is a linker moiety represented by any one of the formulae (XVIIa) to (XVIIt):wherein, nl is 1 to 5, n2, n3, n4 and nl2 are each independently 0 to 2, n5, n6 and n29 are each independently 1 to 10, n7 and n8 are each independently 0 to 4, n9, nl3, nl4, nl5, nl8, n20 and n21 are each independently 1 or 2, n 10 and ni l are each independently 0 or 1, nl6 is 0 to 12, nl7, nl9, n22, n27 and n28 are each independently 1 to 4, n23 is 2 to 4,XL1, XL2, XL3, XL4and XL5are each independently =CH- or =N-,XL6, XL7, XL1° and XL11are each independently -OH or -NH2,RL1, RL2, RL3, RL4, RL5and RL6are each independently -H or a methyl group, * indicates covalent attachment to Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and**’ indicates covalent attachment to E; or,(b) E is a residue represented by the following formula (XVIo) or (XVIr):wherein,Xci and XC2 are each independently selected from the group consisting of -OH and -NH2, and** indicates covalent attachment to L, and the residue E optionally comprises a radionuclide,L is a linker moiety represented by any one of the formulae (XVIIu) to (XVIIy):wherein,n24 is 1 to 5, n25 and n26 are each independently 1 or 2,XL8and XL9are each independently =CH- or =N-,RL7, RL8, RL9, RL1°, RL12and RL12are each independently -H or a methyl group, and* indicates covalent attachment to an N atom of an amino group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and**’ indicates covalent attachment to E.

14. The compound or salt of any one of claims 1 to 12, wherein each group Zla, Zlb, Z2, Z3,Z4, Z5, Z6, Z7, Z8and Z9is independently a moiety represented by the following formula (XV’):E-L1-L2-* (XV’) wherein,* indicates covalent attachment to a carbonyl group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, andE is a residue represented by any one of the following formulae (XVIa) to (XVIn):wherein,Xci and XC2 are each independently selected from the group consisting of -OH and -NH2, and** indicates covalent attachment to Li, the residue E optionally comprises a radionuclide, andLi is a linker moiety represented by any one of the formulae (XVII’a) to (XVIEg):wherein, nl is 1 to 5, n2, n3 and n4 are each independently 0 to 2, n29 is 1 to 10, n27 and n28 are each independently 1 to 4, n23 is 2 to 4,XL1and XL2are each independently =CH- or =N-, XL1° and XL11are each independently -OH or -NH2, *** indicates covalent attachment to L2, and **’ indicates covalent attachment to E; andL2 is a linker moiety represented by any one of the formulae (XVII’h) to (XVII’t):wherein, nl2 is 0 to 2, n5 and n6 are each independently 1 to 10, n7 and n8 are each independently 0 to 4, n9, nl3, nl4, nl5, nl8, n20 and n21 are each independently 1 or 2, n 10 and ni l are each independently 0 or 1, nl6 is 0 to 12, nl7, nl9 and n22 are each independently 1 to 4, n23 is 2 to 4,XL3, XL4and XL5are each independently =CH- or =N-,XL6and XL7are each independently -OH or -NH2,RL1, RL2, RL3, RL4, RL5and RL6are each independently -H or a methyl group, * indicates covalent attachment to a carbonyl group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and ***’ indicates covalent attachment to Li.

15. The compound or salt of any one of claims 1 to 12, wherein each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7, Z8and Z9is independently a moiety represented by the following formula (XV”):E-L-* (XV”)wherein,* indicates covalent attachment to a carbonyl group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7,Xaa8, Xaa9, XaalO or Xaal 1, andE is a residue represented by the following formula (XVIo) or (XVIr):wherein,Xci and XC2 are each independently selected from the group consisting of -OH and -NH2, and** indicates covalent attachment to L, and the residue E optionally comprises a radionuclide,L is a linker moiety represented by any one of the formulae (XVIP'h) to (XVII’ ’t):wherein, nl2 is 0 to 2, n5 and n6 are each independently 1 to 10, n7 and n8 are each independently 0 to 4, n9, nl3, nl4, nl5, nl8, n20 and n21 are each independently 1 or 2, n 10 and ni l are each independently 0 or 1, nl6 is 0 to 12, nl7, nl9 and n22 are each independently 1 to 4, n23 is 2 to 4,XL3, XL4and XL5are each independently =CH- or =N-,XL6and XL7are each independently -OH or -NH2,RL1, RL2, RL3, RL4, RL5and RL6are each independently -H or a methyl group, * indicates covalent attachment to a carbonyl group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and **’ indicates covalent attachment to L.

16. The compound or salt of any one of claims 1 to 15, wherein the radionuclide is selected from:(i) a diagnostically active radionuclide selected from the group consisting of A1-18F,43Sc, 44Sc,51Mn,52Mn,64Cu,67Ga,68Ga,86Y,89Zr,94mTc, "mTc,mIn,149Tb,152Tb,155Tb, 161Tb,177LU,2O1T1,203Pb,18F,76Br,77Br,123I,124I, and125I, preferably from the group consisting of A1-18F,44Sc,64Cu,67Ga,68Ga,86Y,89Zr, "mTc,i nIn,203Pb, and more preferably from the group consisting of64Cu,68Ga,i nIn and203Pb; and / or(ii) a therapeutically active radionuclide selected from the group consisting of47Sc,67Cu, 89Sr,90Y,mIn,153Sm,149Tb,161Tb,177Lu,186Re,188Re,212Pb,213Bi,223Ra,225Ac,226Th, 227Th,1251,131I, and211At, preferably from the group consisting of67Cu,90Y,149Tb,161Tb, 177LU,212Pb,213Bi,225Ac,227Th, and more preferably from the group consisting of90Y,177LU,212Pb and225Ac.

17. The compound or salt of any one of claims 1 to 16, wherein each group Zla, Zlb, Z2, Z3, Z4, Z5, Z6, Z7and Z8is independently a moiety represented by any one of the following formulae (XVIIIa) to (XVIIIo), and Z9is a moiety of formula (XVIIIo):5(XVIIIm)wherein,Xci, XC2, XL6, XL7and XL1° are each independently selected from the group consisting of -OH and -NH2, and n6 is 1 to 10, and n7 and n8 are each independently 0 to 4, n9, nl3, nl4, nl5, nl8, n20 and n21 are each independently 1 or 2, and nlO and ni l are each independently 0 or 1, and nl2 is 0 to 2, nl6 and n27 are each independently 0 to 12, and nl7, nl9, n22 and n27 are each independently 1 to 4, and n23 is 2 to 4, andXL3, XL4and XL5are each independently =N- or =CH-, andRL1, RL2, RL3, RL4, RL5, RL6and RL13are each independently -H or a methyl group, and* indicates covalent attachment of the structures in formulae (XVIIIa) to (XVIIIo) to an N atom of an amino group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1 or covalent attachment of the structure in formula (XVIIIo) to a carbonyl group of Xaal, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO or Xaal 1, and the moiety represented by any one of the above formulae (XVIIIa) to (XVIIIn) optionally comprises a radionuclide, the radionuclide being preferably selected from the group consisting of A118F,43Sc,44Sc,47Sc,51Mn,52Mn,64Cu,64Cu,67Cu,67Ga,68Ga, 86Y,89Zr,90Y,mIn,149Tb,152Tb,153Sm,155Tb,161Tb,177Lu,2O1T1,203Pb,212Pb,213Bi, 225Ac,226Th and227Th.

18. The compound or salt of any one of claims 1 to 16, which is represented by any one of the following formulae:H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Lys(Me)-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe2-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Har-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Lys-Tyr-Asp-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Lys(Me)-Tyr-Asp-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Pcnf-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Guf-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-enH-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Onf-NH2H-Pip-Trp-Cya-Npg-Apc(D0TA)-Asn-6Clw-KMe3-Tyr-Cya-0ff-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Ser-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Thr-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Lys-6Clw-KMe3-Tyr-Ser-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Lys-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Lys(Me)-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-KMe3-Lys(DOTA)-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc-Asn-6Clw-Lys(DOTA)-Tyr-Cya-Thi-NH2H-Ida-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Nml-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NHMeH-Pip-Trp-Cya-Npg-Orn(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Cya-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Nma-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-KMe4-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-RMe2-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Kip-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Egd-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Orn-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Opy-Tyr-Cya-Thi-NH2H-Pip-Trp-Asn-Npg-Apc(DOTA)-Asn-6Clw-Lys-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Kzw-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Egg-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Orn-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Ocf-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Mff-NH2H-Pip-Trp-Cya-Npg-Apc(NOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(NODAGA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTAGA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(NOPO)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(BnTCMC)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA-PPAc)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA-glu)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA-Kzw)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Mnpg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTAM)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(PSC)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Ala-Cya-Thi-NH2H-Pip-Trp-Cya-Mnpg-Om(PSC)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Mnpg-Om(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Nmg-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Gel-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Thr-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Thr-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Mnpg-Apc(DOTA)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Mgel-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Penox-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Nmo(Me)-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Dab(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Mor-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Nmo-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Ser-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Azp-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Phe-NH2 wherein the DOTA, NOTA, PSC, DOTAGA, NOPO, BnTCMC or NOD AGA moiety optionally comprises a radionuclide, the radionuclide being preferably selected from the group consisting of A118F,43Sc,44Sc,47Sc,51Mn,52Mn,64Cu,64Cu,67Cu,67Ga,68Ga, 86Y,89Zr,90Y,mIn,149Tb,152Tb,153Sm,155Tb,161Tb,177Lu,2O1T1,203Pb,212Pb,213Bi, 225Ac,226Th and227Th.

19. The compound or salt of any one of claims 1 to 18, which is represented by any one of the following formulae:H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-RMe2-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Arg(Me)-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Asp-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Pcnf-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-Kzw-Tyr-Cya-Thi-NH2 H-Nma-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Orn(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Lys(Me)-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(NOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(NODAGA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA-PPAc)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(PSC)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-Brw6-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Om(PSC)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2 H-Pip-Trp-Cya-Mnpg-Om(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Gel-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Thr-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Dab(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Thi-NH2H-Pip-Trp-Cya-Npg-Apc(DOTA)-Asn-6Clw-KMe3-Tyr-Cya-Phe-NH2wherein the DOTA, NOTA, PSC or NODAGA moiety optionally comprises a radionuclide, the radionuclide being preferably selected from the group consisting of A118F,43SC,44SC,47SC,51Mn,52Mn,64Cu,64Cu,67Cu,67Ga,68Ga,86Y,89Zr,90Y,mIn, 149Tb,152Tb,153Sm,155Tb,161Tb,177Lu,2O1T1,203Pb,212Pb,213Bi,225Ac,226Th and227Th.

20. The compound or salt of any one of claims 1 to 19, which is any one selected from the following compounds:wherein the depicted compounds are preferably in complex with a radionuclide, which is preferably selected from the group consisting of A118F,43Sc,44Sc,47Sc,51Mn,52Mn, 64Cu,64Cu,67Cu,67Ga,68Ga,86Y,89Zr,90Y,n iIn,149Tb,152Tb,153Sm,155Tb,161Tb,177Lu,2O1T1,203Pb,212Pb,213Bi,225Ac,226Th and227Th.

21. Pharmaceutical composition comprising the compound or salt of any one of claims 1 to 20 and a pharmaceutically acceptable excipient.

22. The compound, salt or pharmaceutical composition of any one of claims 1 to 20 for use in a method of diagnosing and / or treating a disease, preferably cancer, and more preferably a P-cadherin expressing cancer.

23. The compound, salt or composition for use of claim 22, wherein the disease is cancer and said cancer is selected from the group consisting of ovarian cancer, colorectal cancer, cholangiocarcinoma, non-small cell lung cancer (NSCLC) including squamous NSCLC,esophageal cancer, head-and-neck cancer including squamous cell carcinoma of head and neck (SCCHN), and tumors of the breast including triple negative breast cancer (TNBC), pancreatic cancer including pancreatic ductal adenocarcinoma (PDAC), endometrial cancer, cervical cancer, gastric cancer, and sarcoma, and preferably from the group consisting of ovarian cancer, colorectal cancer, esophageal cancer, head-and-neck cancer and breast cancer.