Urokinase plasminogen activator surface receptor (UPAR) ligands for diagnostic or therapeutic use

Abstract

The present invention is related to a compound comprising a cyclic peptide of formula (I)

Description

[0001] UROKINASE PLASMINOGEN ACTIVATOR SURFACE RECEPTOR (UPAR) LIGANDS FOR DIAGNOSTIC OR THERAPEUTIC USE

[0002] FIELD OF THE INVENTION

[0003] The present invention is related to a chemical compound; a peptide; an Urokinase plasminogen activator surface receptor (uPAR) binding compound; an Urokinase plasminogen activator surface receptor (uPAR) binding peptide; a composition comprising the compound; a composition comprising the Urokinase plasminogen activator surface receptor (uPAR) binding compound; a composition comprising the peptide; a composition comprising the Urokinase plasminogen activator surface receptor (uPAR) peptide; the compound, the Urokinase plasminogen activator surface receptor (uPAR) binding compound, the peptide, the Urokinase plasminogen activator surface receptor (uPAR) peptide and the compositions, respectively, for use in a method for the diagnosis of a disease; the compound, the Urokinase plasminogen activator surface receptor (uPAR) binding compound, the peptide, the Urokinase plasminogen activator surface receptor (uPAR) peptide and the compositions, respectively, for use in a method for the treatment of a disease; the compound, the Urokinase plasminogen activator surface receptor (uPAR) binding compound, the peptide, the Urokinase plasminogen activator surface receptor (uPAR) peptide and the compositions, 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 compound, the Urokinase plasminogen activator surface receptor (uPAR) binding compound, the peptide, the Urokinase plasminogen activator surface receptor (uPAR) binding peptide, and the compositions, respectively, for use in a method for delivering a radionuclide to an Urokinase plasminogen activator surface receptor (uPAR) to a cell, preferably a uPAR overexpressing tumor cell; a method for the diagnosis of a disease using the compound, the Urokinase plasminogen activator surface receptor (uPAR) binding compound, the peptide, the Urokinase plasminogen activator surface receptor (uPAR) binding peptide and the compositions, respectively; a method for the treatment of a disease using the compound, the Urokinase plasminogen activator surface receptor (uPAR) binding compound, the peptide, the Urokinase plasminogen activator surface receptor (uPAR) binding peptide and the compositions, 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 compound, the Urokinase plasminogen activator surface receptor (uPAR) binding compound, the peptide, the Urokinase plasminogen activator surface receptor (uPAR) binding peptide and the compositions, respectively; a method for the delivery of a radionuclide to an Urokinase plasminogen activator surface receptor (uPAR) expressing tissue using the compound, the Urokinase plasminogen activator surface receptor (uPAR) binding compound, the peptide, the Urokinase plasminogen activator surface receptor (uPAR) binding peptide and the compositions, respectively.

[0004] BACKGROUND OF THE INVENTION

[0005] Metastasis is a hallmark of cancer which is in many cases responsible for the fatal outcome of the disease. The majority of cancer deaths is caused by metastasis (Dillekas, Rogers et al. 2019). Even though new therapeutic options that support the patient’s immune system to fight own cancer cells have been immensely successful for a number of cancer entities, the fraction of patients who benefit from this treatment is estimated to be below 15% (Haslam and Prasad 2019) with many solid tumors showing low susceptibility to this immune therapy. These two aspects highlight the need for new therapeutic options in cancer which specifically target invasive tumor cells which can lead to the formation and expansion of metastasis into other tissues. Since uPAR plays an important role in the remodelling of tissue and epithelial-mesenchymal transition (EMT), it is a promising target for diagnosis and treatment of aggressive tumors. uPAR as part of the plasminogen activation system

[0006] Urokinase plasminogen activator surface receptor (uPAR) was identified as the cell surface receptor for the Urokinase-type plasminogen activator (uPA) (Bajpai and Baker 1985, Stoppelli, Corti et al. 1985, Vassalli, Baccino et al. 1985) and isolated from a human cell line (Roldan, Cubellis et al. 1990). uPAR is also known as Monocyte activation antigen Mo3, Urokinase receptor, or CD87 (Cluster of Differentiation 87). It is a glycosylphosphotidylinositol-membrane-anchored multidomain protein and part of the plasminogen activation system and facilitates the focalization of the conversion of plasmin from the inactive precursor plasminogen (Stephens, Pollanen et al. 1989). This is achieved by the high affinity-binding of uPA.

[0007] Plasminogen is a central serine protease for the cleavage and thus activation or deactivation of enzymatic activities as collagenases, fibrin, fibronectin, thrombospondin, laminin, and von Willebrand factor. One of the factors activating Plasminogen to Plasmin is the Urokinase Plasminogen activator (uPA), another protease. The activity of uPA is focalized by its membrane bound receptor, uPAR. uPAR binds the progenitor form of uPA as well as the mature, active form of uPA which is generated by the proteolytic cleavage by Plasmin, the product of cleavage of plasminogen by uPA in a positive feedback loop (Nielsen, Hansen et al. 1982). uPAR plays a role in tissue degradation and remodelling as well as in extravascular fibrinolysis and embryogenesis, angiogenesis, cell migration, wound healing, inflammatory response, and apoptotic cell death (McMahon and Kwaan 2015). Even though uPAR has no own connection between extracellular and intracellular space it is involved in the control of cell morphology, migratory behaviour, angiogenesis and cell proliferation by interaction with vitronectin and transmembrane receptors as Integrins or Formyl Peptide Receptors (Metrangolo, Ploug et al. 2021).

[0008] Human uPAR is a 36978 Da protein of 335 amino acids coded on chromosome 19. It consists of an N- terminal signal peptide of 22 amino acids, the Urokinase plasminogen activator surface receptor of 283 amino acids and a C-terminal peptide of 30 amino acids which is cleaved off in the mature form. The structure is characterised by 14 disulfide bonds, at least 5 glycosylation sites and a lipidation in form of a GPI-membrane anchor at amino acid 305 (www.uniprot.org / uniprotkb / Q03405; 08-NOV-2023, entry version 221, SwissProt release 2023_05 / 2023_05). The receptor consists of three consecutive domains of the snake toxin like family which collects short proteins with a disulphide-rich structure. uPAR is the namesake for a family of proteins which contain such domains: Ly6 / PLAUR domain containing proteins. However, the sequence similarity between proteins with such domains is low and they possess different functions. There are at least 8 different Ly6 / PLAUR domain containing proteins known to date. The closest relative for uPAR is Ly6 / PLAUR domain-containing protein 3 with only 25% sequence identity.

[0009] Three Ly6 / PLAUR domains form the binding site for uPA, while on the outside of Ly6 / PLAUR domains 1 and 2 a Vitronectin binding site is formed.

[0010] Table 1 below indicates sequence identity for uPAR and uPA between species. More specifically, % identity between the human sequence and the indicated species are shown. The columns of Table 1 indicate the comparison between full length Proteins (PLAUR / uPAR; PLAU / uPA) and residues which are in the vicinity (<5A) of a binding ligand in a Complex structure for uPAR and a peptide (Contact Peptide; pdblywh) or uPA (Contact uPA, pdb4k24) and uPA with uPAR (Contact uPAR, pdb4k24).

[0011] Table 1 : Sequence identity for uPAR and uPA between species

[0012] Sequence similarity between species is moderate and even the binding pocket for uPA is not totally conserved. This is also the case for the natural ligand uPA (Table 1). This leads to species specificity for the interaction with e.g. a ~80-fold lower affinity for the human-uPAR - mouse-uPA interaction (Lin, Gardsvoll et al. 2010). uPAR is internalized as a complex with its ligands uPA and PAI-1 mediated by LRP1 (Conese, Nykjaer et al. 1995, Nykjaer, Conese et al. 1997). However, a second ligand independent constitutive way of internalization and recycling has been observed (Cortese, Sahores et al. 2008).

[0013] Two mechanisms lead to 5 different uPAR forms in organisms: the proteolytic cleavage of the full- length form behind an Arginine in position 105 or 111 in the linker region between domains 1 and 2 by its ligand uPA and the cleavage of the GPI anchor to a soluble form of uPAR (suPAR). Aditional to the membrane bound full-length uPAR the cleavage products are (1) soluble full length uPAR (suPAR), (2) membrane bound domains 1 and 2, (3) soluble domains 1 and 2 and (4) soluble domain 1 .

[0014] Upon proteolytic cleavage of domain 1 both products lose the ability to bind to ligands as uPA or Vitronectin (Hoyer-Hansen, Ronne et al. 1992). Soluble uPAR (suPAR) can also be a result of alternative splicing (Stewart and Sayers 2009). suPAR has been established as a prognostic marker for acute medical patients, kidney disease, infections and more (Thuno, Macho et al. 2009, Rasmussen, Ladelund et al. 2018). Also in cancer patients, suPAR levels are frequently elevated (Paraskevas, Mulita et al. 2022).

[0015] Apart from its physiological role, uPAR is involved in pathological processes. Elevated uPAR levels are observed in cardiac fibrosis (Saxena, Izmirly et al. 2015), chronic liver disease and Hepatidis B (Zimmermann, Koch et al. 2012, Akdogan, Atak Yucel et al. 2019), Cystic fibrosis, COPD (Xiao, Hsu et al. 2005), idiopathic pulmonary fibrosis (Desai, Mattson et al. 2011), glomerulosclerosis (Trimarchi, Canzonieri et al. 2017, Chebotareva, Vinogradov et al. 2022), systemic sclerosis (suPAR; (Legany, Toldi et al. 2015)), rheumatoid arthritis (Fibbi, Pucci et al. 1998), neurologic disorders as autism spectrum disorder or epileptogenic tissue remodelling (Campbell, D'Oronzio et al. 2007, Campbell, Li et al. 2008, Lahtinen, Huusko et al. 2009). uPAR expression in different cancers is extensively studied and it has a role in tumor growth, angiogenesis, tumor cell invasion, migration, epithelial-mesenchymal transition (EMT), and has been associated with the development of metastatic phenotypes (Andreasen, Egelund et al. 2000, Lund, Illemann et al. 2011, Madunic 2018, Mahmood, Mihalcioiu et al. 2018, Paraskevas, Mulita et al. 2022). In most cancers uPAR-expression is at higher levels as in the comparable healthy tissue (see, Figure 1).

[0016] Elevated uPAR expression is indicative for increased aggressiveness, postoperative progression, metastasis, poor response to therapy and poor prognosis in multiple cancer types as breast, prostate, ovarian, colorectal or lung cancer (Mahmood, Mihalcioiu et al. 2018). Rationale for Targeting uPAR

[0017] Given the expression pattern of uPAR in healthy and tumor tissues and the role of uPAR for tissue reorganization and promotion of invasive tumor growth and metastasis, its targeting presents a promising strategy for cancer diagnosis, stratification and therapy. Since uPAR is mainly expressed in tumor or tumor-related cells as tumour-associated macrophages, neutrophils, fibroblasts, endothelial and disseminated tumour cells (Smith and Marshall 2010), it represents an attractive tumor-specific target, reducing potential off-target effects.

[0018] State of the Art

[0019] Multiple approaches are used for targeting uPAR. Different Antibodies have been developed. The monoclonal antibody ATN-658 (huATN-658; MNPR-101) is developed for diagnosis and treatment of cancer and infectious disease (Van Buren, Gray et al. 2009, Mahmood, Arakelian et al. 2020) (W0002005116077, W0002007134274, W0002021257552) including as targeting moiety to carry alpha particle-emitting radionuclides.

[0020] Other uPAR-directed antibodies for the diagnosis and / or treatment of cancer, autoimmune disease are described in the literature (Elvin, Foltz et al. 2009) (W0002007120693; Amgen / AstraZeneca), (Duriseti, Goetz et al. 2010 W000201 1100620, LeBeau, Duriseti et al. 2013, Lu, Cong et al. 2021, W0002023125842), targeting deletion variants of uPAR (W0002002082077, Luther, Kotzsch et al. 2003) and for targeting uPAR-expressing cells for Immunotherapy of senescence related diseases (Amor, Feucht et al. 2020, W0002022261405).

[0021] Also proteins have been used as targeting moieties or for the inhibition of the uPA / uPAR interaction. These were mostly based on the sequence of the uPAR-binding fraction in the amino-terminal fragment (ATF) of uPA and focus on diagnosis or treatment of cancer or infectious disease (W0002001025410, Guo, Higazi et al. 2000, W0002002058714, Alfano, Sidenius et al. 2002). Different combinations of proteins which bind and block the uPA-binding site of uPAR and comprise a second functionality as binding of the Vitronectin binding site of uPAR (W0002012085076) or Cytokines (W0002022204267) or comprising an additional transmembrane domain, and an intracellular signaling domain for targeting immunotherapy (W0002022261398). The second functionality can also be a contrast agent for imaging of tumors (Yang, Mao et al. 2009, Yang, Sajja et al. 2013) or toxins for the targeted destruction of tumor cells (Rustamzadeh, Li et al. 2003, Hall 2006).

[0022] Also small molecules for the disruption of the uPA / uPAR (Mani, Wang et al. 2013, Liu, Xu et al. 2017, Zhou, Bum-Erdene et al. 2018, Bum-Erdene, Liu et al. 2021) and the Vitronectin / uPAR interaction (Rea, Lavecchia et al. 2013, W0002021198844) have been developed.

[0023] The uPAR binding region of uPA was identified (Appella, Robinson et al. 1987) and respective peptides were optimized (Magdolen, Burgle et al. 2001). Bacteriophage phage display was used for the identification of alternative peptide sequences for binding in the uPA site of uPAR which were optimized and resulted in a peptide AE105 with a Kj of 0.36 nM (Goodson, Doyle et al. 1994, Ploug, Ostergaard et al. 2001 ). AE105 was extensively investigated as targeting moiety for magnetic resonance- and near infrared-guided photothermal therapy and surgery for tumors (Li, Wang et al. 2021, W0002021130237), and for radioligand therapy (W0002014086364) in animals (Li, Niu et al. 2008, Persson, Madsen et al. 2012, Persson, Madsen et al. 2012, Persson, Rasmussen et al. 2012, Persson, Liu et al. 2013, Persson, Juhl et al. 2014) as well as in humans (Persson, El Ali et al. 2014, Persson, Skovgaard et al. 2015, Skovgaard, Persson et al. 2017, Skovgaard, Persson et al. 2017, Skovgaard, Persson et al. 2017, Fosbol, Kurbegovic et al. 2020, Fosbol, Kurbegovic et al. 2021, Carlsen, Loft et al. 2022, Riser, Clausen et al. 2022).

[0024] AE105 was also used in modified forms as dimers (Knor, Sato et al. 2008) and cyclized (Leth, Newcombe et al. 2023).

[0025] The problem underlying the present invention is the provision of a compound which is suitable as a diagnostic agent and / or a pharmaceutical agent, particularly if conjugated to a diagnostically and / or therapeutically active effector. A further problem underlying the present invention is the provision of a compound which is suitable as a diagnostic agent and / or a pharmaceutical agent, particularly if conjugated to a diagnostically and / or therapeutically active effector, whereby the compound is a potent binder of urokinase plasminogen activator surface receptor (uPAR); preferably the pIC50 of the compound is equal to or greater than 6.0, preferably equal or greater than 7.0. A further problem underlying the present invention is the provision of a compound which is suitable as a diagnostic agent and / or a pharmaceutical agent, particularly if conjugated to a diagnostically and / or therapeutically active effector, in the diagnosis and / or therapy of a disease where the diseased cells and / or diseased tissues express urokinase plasminogen activator surface receptor (uPAR). 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 agent to a diseased cell and / or diseased tissue, respectively, and more particularly a urokinase plasminogen activator surface receptor (uPAR)-expressing diseased cell and / or diseased tissue, preferably the diseased tissue comprises or contains cancer associated fibroblasts. 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 urokinase plasminogen activator surface receptor (uPAR)-expressing cells and / or tissues, more particularly a urokinase plasminogen activator surface receptor (uPAR)-expressing diseased cell and / or diseased tissue, preferably the diseased tissue comprises or contains cancer associated fibroblasts. 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. 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.

[0026] There is a need for compounds that are suitable as a diagnostic agent and / or pharmaceutical agent, particularly if conjugated to a diagnostically and / or therapeutically active effector. Furthermore, there is a need for compounds that are suitable as a diagnostic agent and / or a pharmaceutical agent, particularly if conjugated to a diagnostically and / or therapeutically active effector, whereby the compound is a potent binder of urokinase plasminogen activator surface receptor (uPAR) activity; preferably the pIC50 of the compound is equal to or greater than 6.0, preferably equal to or greater than 7.0. Further, there is a need for compounds suitable as diagnostic agents and / or pharmaceutical agents, particularly if conjugated to a diagnostically and / or therapeutically active effector, in the diagnosis and / or therapy of a disease where the diseased cells and / or diseased tissues express urokinase plasminogen activator surface receptor (uPAR). Furthermore, there is a need for a compound which is suitable for delivering a diagnostically and / or therapeutically effective agent to a diseased cell and / or diseased tissue, respectively, and more particularly a urokinase plasminogen activator surface receptor (uPAR)-expressing diseased cell and / or diseased tissue, preferably the diseased tissue comprises or contains cancer associated fibroblasts. Also, there is a need for 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 urokinase plasminogen activator surface receptor (uPAR)-expressing cells and / or tissues, more particularly a urokinase plasminogen activator surface receptor (uPAR)-expressing diseased cell and / or diseased tissue, preferably the diseased tissue comprises or contains cancer associated fibroblasts. Furthermore, there is a need for 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. Further, there is a need for a pharmaceutical composition containing a compound having the characteristics as outlined above. Furthermore, there is a need for a kit which is suitable for use in any of the above methods. The present invention satisfies these needs.

[0027] These and other problems are solved by the subject matter of the attached claims.

[0028] These and other problems underlying the present invention are also solved by the following is also referred to as list of embodiments herein, embodiments, which Embodiment 1. A compound comprising a cyclic peptide of formula (I) and optionally comprising a C-terminal modification group Cterm covalently attached to XaalO, wherein the C-terminal modification group Cterm comprises a Z group, wherein the peptide sequence is drawn from left to right in N to C-terminal direction,

[0029] Xaal is a residue of an L-α-amino acid comprising a side chain, wherein the side chain comprises a sulfur atom which is covalently attached to the sulfur atom of the thiol group of XaalO, wherein the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of Xaa2,

[0030] Xaa2 is a residue of an α-amino acid comprising a side chain, preferably an L-α-amino acid comprising a side chain, wherein the side chain optionally comprises a Z group, wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3,

[0031] Xaa3 is a residue of an α-amino acid comprising a side chain, preferably an L-α-amino acid comprising a side chain, wherein the side chain optionally comprises a Z group, wherein the carbonyl group of Xaa3 is covalently attached to the a-nitrogen atom of Xaa4,

[0032] Xaa4 is a residue of an L-α-amino acid comprising a side chain, wherein the side chain comprises a group selected from the group comprising an aryl group, a heteroaryl group, a carbocycle group and a heterocycle group, preferably an aryl or heteroaryl group, wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0033] Xaa5 is a residue of an L-α-amino acid comprising a side chain, wherein the side chain comprises an aryl group or a heteroaryl group, wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6, Xaa6 is a residue of an L-α-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of Xaa6, wherein the side chain comprises a hydrophobic group, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7, preferably the side chain of Xaa6 and the a-nitrogen atom form a heterocycle,

[0034] Xaa7 is a residue of an α-amino acid comprising a side chain and optionally comprising a substituent covalently attached to the a-nitrogen atom of Xaa7, wherein the side chain optionally comprising a Z group, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8, preferably Xaa7 is a residue of an L-α-amino acid comprising a side chain, wherein the side chain of Xaa7 and the a-nitrogen atom optionally form a heterocycle,

[0035] Xaa8 is a residue of an α-amino acid comprising a side chain, preferably a residue of an L-a- amino acid comprising a side chain, wherein the side chain comprises a hydrophobic group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0036] Xaa9 is a residue of an α-amino acid comprising a side chain, preferably a residue of an L-a- amino acid comprising a side chain, wherein the side chain comprises an aliphatic group, wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO,

[0037] XaalO is a residue of an amino thiol comprising an amine group, a thiol group and optionally a carbonyl group, wherein if the carbonyl group is present, the C atom of the carbonyl group is covalently attached to the amine group bearing C atom of XaalO, wherein the sulfur atom of the thiol group is covalently attached to the sulfur atom of the thiol group of Xaal, preferably XaalO is a residue of an L-α-amino acid comprising a side chain, wherein the side chain comprises a sulfur atom which is covalently attached to the sulfur atom of the thiol group of Xaal, wherein, if the carbonyl group is present, the C atom of the carbonyl group of XaalO is optionally covalently attached to the C-terminal modification group Cterm, an N-terminal modification group A, wherein the N-terminal modification group A is either a hydrophobic group Abl or XaaO, wherein A is covalently attached to the a-nitrogen atom of Xaal , wherein XaaO is a residue of an α-amino acid comprising a side chain and optionally comprising up to three substituents covalently attached to the a- nitrogen atom of XaaO, wherein the side chain comprises a hydrophobic group, and wherein, if present, one substituent covalently attached to the a- nitrogen atom of XaaO is an N-terminal extension group Nterm, and wherein the N-terminal extension group Nterm optionally comprises a Z group; or a pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate thereof.

[0038] Embodiment 2. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 1, wherein the N-terminal modification group A is either a blocking group Abl, preferably a hydrophobic blocking group Abl, or XaaO, the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein if the N-terminal modification group A is the blocking group Abl, the blocking group Abl is preferably of formula (Ila), of formula (lib) or of formula (lie) wherein XOais selected from the group consisting of -O-, -NH- and -S- preferably XOais selected from the group consisting of -O- and -NH-, wherein ROais selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROais unsubstituted or substituted, preferably ROais unsubsituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROais substituted, ROais substituted by one or two substituents, each and any substituent is independently different from a polar group or a charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, and wherein ROais optionally linked to XOaby a linker comprising one or two -CH2- groups, preferably the linker is absent or consists of one -CH2- group, more preferably ROais selected from the group consisting of a (C3-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, most preferably each and any of said (C3-C6)alkyl group, phenyl group and (C5-C6)carbocycle is unsubstituted, wherein RObis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein RObis unsubtituted or substituted, preferably RObis unsubstituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if Robis substituted, Robis substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, and wherein RObis optionally linked to the -SO2- moiety in formula (lib) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two -CH2- groups, preferably Robis selected from the group consisting of a (C4-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C4- C6))lkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted, wherein ROcis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis unsubstituted or substituted, preferably ROcis unsubstituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROcis substituted, ROcis substituted by one or two substituents, preferably each and any substituent is individually and independently different from a polar or charged group, preferably each and any subsitutent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, and wherein ROcis optionally linked to the carbonyl moiety in formula (lie) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two -CH2- groups, wherein one -CH2- group of ROcis optionally replaced by -O- or -S-, preferably ROcis selected from the group consisting of a (C4-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C4- C6)alkyl group, a phenyl group and a (C5-C6)carbocycle is unsubstituted, more preferably Abl is of formula (Ila) or (lie), most preferably Abl is of formula (Ila), wherein if the N-terminal modification group A is XaaO,

[0039] XaaO is a residue of an α-amino acid comprising a side chain and optionally comprising up to three substituents covalently attached to the a-nitrogen atom of XaaO, wherein the side chain comprises a hydrophobic group, and wherein, if present, one substituent covalently attached to the a-nitrogen atom of XaaO is an N-terminal extension group Nterm, and wherein the N-terminal extension group Nterm optionally comprises a Z group, and

[0040] XaaO is a residue of formula (lid) or of formula (lie) wherein ROdis selected from the group consisting of a (C2-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROdis unsubstituted or substituted, preferably Rodis unsubstituted, wherein any of said (C2-C8)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROdis substituted, ROdis substituted by one or two substitutes, wherein each and any of the substituent is individually and independently different from a polar or charged group, preferably each and any the substitutes ROdis individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- Cg)carbocycle group, an aryl group, a heteroaryl group, and a (C3- Cg)heterocycle and wherein ROdis optionally linked to the a-carbon atom of XaaO by a linker comprising one or two -CH2- groups, preferably the linker is absent or comprises one -CH2- group, preferably ROdis selected from the group consisting of a (C2-C5)alkyl group, a (C5-C6)carbocycle, and a phenyl group, more preferably each and any of the (C2-C5 alkyl group, the (C5-C6)carbocycle, and the phenyl group are unsubstituted, wherein ROeis selected from the group consisting of -H, an aryl group, a (C1-C6)alkyl group, and a (C3-C7) carbocycle, preferably ROeis selected from the group consisting of -H and a methyl group, or wherein ROdand ROetogether form a 4-, 5-, 6-, 7- or 8- membered carbocycle or heterocycle, wherein the carbocycle and the heterocycle are optionally substituted by one or two substituents, wherein, preferably, each substituent is independently selected from the group consisting of a methyl group, -F, -C1, and -OH, preferably ROdand ROetogether form a (C5-C6) carbocycle, more preferably an unsubstituted (C5-C6) carbocycle, wherein Rofis selected from the group consisting of -H and a (C1-C4)alkyl group, preferably ROfis selected from the group consisting of -H and a methyl group, more preferably Rofis -H, wherein Nterm is selected from the group consisting of -H, -ROg, R0g-CO-, R°8-NH-CO-, R°8-O-CO-, R°8-SO2-, R0g-S-CO-, ROg-NH-CNH-, and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, and wherein Nterm is optionally linked to the a-nitrogen atom of XaaO by a linker comprising one amino acid or a dipeptide, preferably the linker is absent or comprises one α-amino acid or a dipeptide composed of two α-amino acids, most preferably the linker is absent or comprises one amino acid or a dipeptide wherein at least one amino acid comprises a polar or charged side chain, wherein R°8is selected from the group consisting of a (C1-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3- Cs)heterocycle, wherein if ROgis a (C1-C8)alkyl group one of the -CH2- groups in R°8is optionally replaced by -S-, -SO-, -SO2-, -O-, or -NH-, and wherein ROgis optionally substituted by one, two or three substituents, wherein, preferably, each substituent is independently selected from the group consisting of -OH, - NH2, a halogen atom, -COOH, -CONH2, -SO3H, -NH-CNH-NH2, a (C1-C6)alkyl group, a (C3-C7)carbocycle, an aryl group, a heteroaryl group, and a (C3-C7)heterocycle, preferably R°8is a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -NH2, -COOH, -CONH2, -SO3H, -NH-CNH-NH2 and a (C1-C4)alkyl group, more preferably ROgis a (C1-C4alky 1 group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, - COOH and -CONH2, preferably Nterm is selected from the group consisting of -H, -R°8,

[0041] R0g-CO-, R°8-NH-CO- and a Z group, more preferably Nterm is selected from the group consisting of -H, -Ac, a succinyl group, a methyl group and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, wherein ROh, R0' and Rokare each and independently selected from the group consisting of a (C1-C4)alkyl group, preferably ROh, R0,and ROkeach are methyl groups,

[0042] Xaal is a residue of an L-α-amino acid comprising a side chain, wherein the side chain comprises a sulfur atom which is covalently attached to the sulfur atom of the thiol group of Xaal 0, wherein the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of Xaa2, preferably Xaal is a residue of an amino acid of formula (III) wherein

[0043] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0044] Xaa2 is a residue of an α-amino acid comprising a side chain and optionally comprising a Z group, wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an amino acid of formula (IVa), (IVb), or (IVc) wherein in formul

[0045] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e)-CN(R2f)-N(R2k)(R21), -

[0046] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2'1, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R21is selected from the group consisting of a methyl group and a -(C^hSChH group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R20is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal -CH2- groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0047] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is each and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and - OH, preferably said cycle is of formula (IVc) in formula (IVb)

[0048] X2ais selected from the group consisting of -CH2-, -CH(OH)-, -CH(F)-, - CH(NHR2p)-, -NH-, -S- and -O-, wherein R2pis selected from the group consisting of -H, -Ac, a (C1-C4)alkyl and a Z group, preferably R2pis selected from the group consisting of -H, a methyl group and a Z group, preferably X2ais -CH2-,

[0049] R2Cis selected from the group consisting of -H, -OH, -F, -NH2 and a (C1-C3)alkyl group, preferably R2cis -H, a = 1 or 2, preferably a = 1 , in formula (IVc) b = 1, 2 or 3,

[0050] X2bis selected from the group consisting of -N(R2p)-, -O-, -S-, -SO-, -SO2-, - NH-, and -CH2-, wherein R2pis selected from the group consisting of -Ac, a (C1-C3)alkyl group and a Z group, the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa) or Xaa2 is a residue of an amino acid of formula (IVc), and more preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0051] Xaa3 is a residue of an α-amino acid comprising a side chain and optionally comprising a Z group, wherein the carbonyl group of Xaa3 is covalently attached to the a-nitrogen atom of Xaa4, preferably Xaa3 is a residue of an amino acid of formula (Va), or (Vb), wherein in formula

[0052] R3ais 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 - (CH2)eR3c, wherein R3cis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R3Coptionally comprises a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR3care each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)eR3cwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-, R3bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R3ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C?)heterocycle, an aryl group, a heteroaryl group and -(CH2)eR3c, wherein said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH, and -F, preferably an -OH group, or R3bis -H under the proviso that R3ais -H, orR3aand R3bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is independently selected from the group consisting of a methyl group, a halogen, -COOH, -CONH2, -NHz and -OH, preferably said cycle is of formula (Vb) in formula (Vb) d = 1, 2 or 3,

[0053] X3ais selected from the group consisting of -N(R30)-, -O-, -S-, -SO-, SO2-, -NH-, and -CH-, wherein R3° is selected from the group consisting of - Ac, a (C1-C3)alkyl group and a Z group, the carbonyl group of Xaa3 is covalently attached to the a-nitrogen atom of Xaa4, preferably Xaa3 is a residue of an amino acid of formula (Va), more preferably Xaa3 is a residue of an L-a amino acid of formula (Vc) wherein in formula (Vc)

[0054] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R3g)(R3h)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R3i)(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3", and -NH-CO-R3m, wherein R3d, R31and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (Ci-Cj)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(Cft^SOsH group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R31is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R3mis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0055] Xaa4 is a residue of an L-α-amino acid comprising a side chain, wherein the side chain comprises an aryl, heteroaryl, carbocycle or heterocycle group, wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5, preferably Xaa4 is a residue of an amino acid of formula (VI), wherein

[0056] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl group, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0057] R4band R4care each and independently selected from the group consisting of - H and a methyl group, the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0058] Xaa5 is a residue of an L-α-amino acid comprising a side chain, wherein the side chain comprises an aryl or heteroaryl group, wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6, preferably Xaa5 is a residue of an amino acid of formula (VII), wherein

[0059] R5ais selected from the group consisting of a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -NHz, an -O(C1-C3)alkyl group, wherein the (Ci-Ca)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0060] Xaa6 is a residue of an L-α-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 a hydrophobic group, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7, preferably the side chain of Xaa6 and the a-nitrogen atom form a heterocycle, and preferably Xaa6 is a residue of an amino acid of formula (Villa), (VUIb) or (VIIIc) wherein in formula (Villa) f = 1 or 2, preferably f = 1,

[0061] R6ais selected from the group consisting of -H, -OH, -F, and a (C1-C4)alkyl group,

[0062] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, in formula (Vlllb) g = 0, 1 or 2, preferably g = 1 , h = 1, 2 or 3, preferably h = 1 or 2, in formula (VIIIc) i = 1 or 2, preferably i= 1 ,

[0063] R6bis selected from the group consisting of a (C2-C6)alkyl group, an aryl group, an aryl group substituted with 1 or 2 substituents, a (C5-C6)heteroaryl group, a (C5-C6)heteroaryl group substituted with 1 or 2 substituents, a (C5-C6)carbocycle, and a (C5-C6)carbocycle substituted with 1 or 2 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1-C6)alkyl group, -CN, -OH, and an -O(C1-C6)alkyl group,

[0064] R6Cis selected from the group consisting of -H and a (C1-C3)alkyl group, the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7, more preferably Xaa6 is a residue of an amino acid of formula (Villa),

[0065] Xaa7 is a residue of an α-amino acid comprising a side chain, optionally comprising a Z group, and optionally comprising a substituent covalently attached to the a-nitrogen atom of the amino acid, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8, preferably Xaa7 is a residue of an amino acid of formula (IXa), (IXb), (IXc), (IXd), and (IXe) wherein in formula (IXa)

[0066] R7ais selected from the group consisting of -H, -OH, -F, -NH2, and a(C1- C3)alkyl group, X7ais absent or selected from the group consisting of -CH(R7f)-, -S-, -O-, and - NH-, wherein R7fis selected from the group consisting of -H, -OH, -F, -NH(R7g) and a (C1-C6)alkyl group, and wherein R7gis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, in formula (IXb) k = 1 or 2, in formula (IXc) m = 1, 2 or 3,

[0067] R7bis selected from the group consisting of -H, and a (C1-C2)alkyl group,

[0068] X7bis absent or selected from the group consisting of -N(R7g)-, -O-, -S-, -SO- , -SO2- and -CH2-, wherein R7gis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, in formula (IXd)

[0069] R7bis selected from the group consisting of -H, and a (C1-C2)alkyl group,

[0070] R7Cis selected from the group consisting of -H, and -(CH2)nR7h, wherein n = 1, 2, or 3, preferably n = 1, and wherein one of the one, two, or three -CH2- groups of -(CH2)nR7hwhich is different from the terminal groups in formula (IXd) is optionally replaced by -O-, -S-, -SO-, or -SO-2, wherein R7his selected from the group consisting of -H, -OH,

[0071] NR7iR7k, -N(CH3)3+, -NH-CNH-NH2, -CONH2, -NH-CO-NH2 and a (C1- C3)alkyl group, an aryl group, a substituted aryl group substituted by one substituent, a heteroaryl group, a heteroaryl group substituted by one substituent, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -NH2 and -OH, wherein R71and R7kare each and independently selected from the group consisting of -H and a methyl group, in formula (IXe) R7dis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and - (CH2)OR71, preferably R7dis selected from the group consisting of -(CH2)OR71, R71is selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R71optionally comprises a Z group, o = 1, 2, 3, 4 or 5, and wherein one of the one, two, three, four or five -CH2- groups linking R71to the a-C atom of Xaa7 in formula (IXe) are optionally substituted by a methyl group, and / or wherein one of said -CH2- groups which is different from the terminal groups is optionally replaced by -O-, -S-, - SO-, or -SO2-, preferably R71is selected from the group consisting of -H, -OH,

[0072] N(R7m)(R7n), -N(R7o)(R7p)(R7q)+, -COOH, a halogen atom, -CN, -N3, -NO2,

[0073] -N(R7m)-CN(R7n)-N(R7r)(R7s), -SO2N(R7,n)(R7u),

[0074] CON(R7m)(R7u), -NH-CO-N(R7m)(R7u), -SO3H, -R71, -NH-SO2-R7', and -NH- CO-R7t, wherein R7m, R7rand R7sare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R70and R7pare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R7nis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R7qis selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R7qis selected from the group consisting of a methyl group and a -(CH2)SO3H group, wherein R7tis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a phenyl group and a (C5-C6)heteroaryl group, and R7* is optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R7tis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R71is a (C1-C3)alkyl group, wherein R7uis selected from the group consisting of -H and R7t, preferably R7uis selected from the group consisting of -H and a methyl group, most preferably R7Uis -H,

[0075] R7eis selected from the group consisting of -H, and a (C1-C3)alkyl group, wherein said (C1-C3)alkyl group is optionally substituted by a substituent preferably selected from the group consisting of -F, -Cl and -OH, the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8, preferably Xaa7 is a residue of an amino acid of formula (IXa), (IXd), and (IXe), more preferably Xaa7 is a residue of an amino acid of formula (IXa),

[0076] Xaa8 is a residue of an α-amino acid comprising a side chain, preferably a residue of an L-a- amino acid comprising a side chain, wherein in the side chain comprises a hydrophobic group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9, preferably Xaa8 is a residue of an amino acid of formula (Xa) or (Xb) wherein in formula (Xa)

[0077] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the P-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the p-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, in formula (Xb) p = 1, 2, or 3, a -CH2- group in the ring of formula (Xb) is optionally replaced by one atom selected from the group consisting of -O- and -S-, and one or more H atoms of the ring -CH2- groups are optionally substituted by a -F or -Cl atom, the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0078] Xaa9 is a residue of an α-amino acid comprising a side chain, wherein the side chain is an aliphatic side chain, wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO, preferably Xaa9 is a residue of an amino acid of formula (XI) wherein

[0079] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4 alky 1 group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO,

[0080] XaalO is a residue of an amino thiol comprising an amine group, a thiol group and optionally a carbonyl group, wherein if the carbonyl group is present, the C atom of the carbonyl group is covalently attached to the amine group bearing C atom of XaalO, wherein the sulfur atom of the thiol group is covalently attached to the sulfur atom of Xaal, preferably as disulfide, and wherein under the proviso that the amino thiol comprises a carbonyl group, a C-terminal modification group Cterm is optionally covalently attached to the C-atom of the carbonyl group, wherein the C-terminal modification group Cterm comprises a Z group, wherein the Z group is covalently attached to the C atom of the carbonyl group, preferably XaalO comprises a substituent preferably selected from the group consisting of - CONH2, -CO-Cterm, -CH2(OH) and -CON(R10d)(R10e), wherein said substituent is covalently attached to the amine group bearing C atom of XaalO, and wherein R10dand R10eare each and independently selected from the group consisting of -H and a methyl group, more preferably XaalO is a residue of formula (XII), wherein

[0081] R10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0082] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), and -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein R10dand R10eare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal, preferably as disulfide. Embodiment s. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1 and 2, wherein the N-terminal modification group A is either a blocking group Abl, preferably a hydrophobic blocking group Abl, or XaaO, the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein if the N-terminal modification group A is the blocking group Abl, the blocking group Abl is of formula (Ila), of formula (lib) or of formula (lie)

[0083] 9 O O 9

[0084] Rx Jk , ?szJkj xOa(Ila) Rotr(lib)rOc(lie) wherein XOais selected from the group consisting of -NH-, -S- and -O-, preferably XOais selected from the group consisting of -NH- and -O-, wherein ROais selected from the group consisting of a (C3-C9)alkyl group, a (C3-C9)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROais unsubstituted or substituted, preferably ROais unsubstituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROais substituted, ROais substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, and wherein ROais optionally linked to XOaby a linker comprising one or two -CH2- groups, preferably the linker is absent or consists of one -CH2- group, preferably ROais selected from the group consisting of a (C3-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C3-C6)alkyl group, the phenyl group and the (C5-C6Xarbocycle is unsubstituted, wherein Robis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein Robis unsubstituted or substituted, preferably RObis unsubstituted, wherein each and any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if RObis substituted, RObis substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably wherein each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- Cg)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8 heterocycle, and wherein RObis optionally linked to the -SO2- moiety in formula (lib) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two -CH2- groups, preferably Robis selected from the group consisting of a (C4-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C4- C6)alkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted, wherein ROcis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis unsubstituted or substituted, preferably ROcis unsubstituted, wherein any of said (Cs-C^alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROcis substituted, ROcis substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, and wherein ROcis optionally linked to the carbonyl moiety in formula (lie) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two -CH2- groups, wherein one -CH2- group of ROcis optionally replaced by -O- or -S-, preferably ROcis selected from the group consisting of a (C4-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C4- C6)alkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted, more preferably Abl is of formula (Ila) or (lie), most preferably Abl is of formula (Ila), wherein if the N-terminal modification group A is XaaO,

[0085] XaaO is a residue of an α-amino acid comprising a side chain and optionally comprising up to three substituents covalently attached to the a-nitrogen atom of XaaO, wherein the side chain comprises a hydrophobic group, and wherein, if present, one substituent covalently attached to the a-nitrogen atom of XaaO is an N-terminal extension group Nterm, and wherein the N-terminal extension group Nterm optionally comprises a Z group, and

[0086] XaaO is a residue of formula (lid) or of formula (He) wherein ROdis selected from the group consisting of a (C2-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROdis unsubstituted or substituted, preferably Rodis unsubstituted, wherein any of said (C2-C8)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROdis substituted, ROdis substituted by one or two substitutents, wherein each and any substituent is individually and independently different from a polar group or charged group, preferably each and any substiuent is individually and independently selected from the group consisting of a (Cj-C6)alkyl group, a (C3-C8)carbocycle group, an aryl group, a heteroaryl group, and a (C3- C8)heterocycle, and wherein ROdis optionally linked to the a-carbon atom of XaaO by a linker comprising one or two -CH2- groups, preferably the linker is absent or comprises one -CH2- group, preferably Rodis selected from the group consisting of a (C2-C5 alkyl group, a (C5-C6)carbocycle, and a phenyl group, more preferably each and any of the (C2-C5 alkyl group, a (C5-C6)carbocycle, and a phenyl group is unsubstituted, wherein ROeis selected from the group consisting of -H, an aryl group, a (C1-C6)alkyl group, and a (C3-C7) carbocycle, preferably ROeis selected from the group consisting of -H and a methyl group, or wherein ROdand ROetogether form a 4-, 5-, 6-, 7- or 8- membered carbocycle or heterocycle, wherein the carbocycle and the heterocycle are optionally substituted by one or two substituents, wherein preferably each substituent is independently selected from the group consisting of a methyl group, -F, -Cl, and -OH, preferably ROdand ROetogether form a (C5-C6) carbocycle, more preferably an unsubstituted (C5-C6) carbocycle, wherein ROfis selected from the group consisting of -H and a (C1-C4)alkyl group, preferably ROfis selected from the group consisting of -H and a methyl group, more preferably ROfis -H, wherein Nterm is selected from the group consisting of -H, -ROg, R0g-CO-, R0g-NH-CO-, R°8-O-CO-, R0g-SO2-, R0g-S-CO-, ROg-NH-CNH-, and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, and wherein Nterm is optionally linked to the a-nitrogen atom of XaaO by a linker comprising one amino acid or a dipeptide, preferably the linker is absent or comprises one α-amino acid or a dipeptide composed of two α-amino acids, most preferably the linker is absent or comprises one amino acid or a dipeptide wherein at least one amino acid comprises a polar or charged side chain, wherein ROgis selected from the group consisting of a (C1-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3- Cs)heterocycle, wherein if ROgis a (Ci-Cs)alkyl group one of the -CH2- groups in ROgis optionally replaced by -S-, -SO-, -SO2-, -O-, or -NH-, and wherein ROgis optionally substituted by one, two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of -OH, -NH2, a halogen atom, -COOH, -CONH2, -SO3H, -NH- CNH-NH2, a (C1-C6)alkyl group, a (C3-C7)carbocycle, an aryl group, a heteroaryl group, and a (C3-C7)heterocycle, preferably ROgis a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -NH2, -COOH, -CONH2, -SO3H, -NH-CNH-NH2and a (C1-C4)alkyl group, more preferably ROgis a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -COOH and -CONH2, preferably Nterm is selected from the group consisting of -H, -ROg, ROg- CO-, R0g-NH-CO- and a Z group, more preferably Nterm is selected from the group consisting of -H, -Ac, a succinyl group, a methyl group and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, wherein ROh, R01and ROkare each and independently selected from the group consisting of a (C1-C4)alkyl group, preferably ROh, R0,and Rokeach are methyl groups,

[0087] Xaal is a residue of an amino acid of formula (III) wherein

[0088] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0089] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0090] Xaa2 is a residue of an α-amino acid of formula (IVa), (IVb), or (IVc) wherein in formula (IVa)

[0091] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2s)(R2h)(R2,)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2c)-CN(R2f)-N(R2k)(R21), -

[0092] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2", wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2g and R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R2' is selected from the group consisting of a methyl group and a -(CH2)SO3H group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R2" is a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R2° is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0093] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (IVc), in formula (IVb)

[0094] X2ais selected from the group consisting of -CH2-, -CH(OH)-, -CH(F)-, CH(NHR2p)-, -NH-, -S- and -O-, wherein R2pis selected from the group consisting of -H, -Ac, a (C1-C4)alkyl and a Z group, preferably R2pis selected from the group consisting of -H, a methyl group and a Z group, preferably X2ais -CH2-,

[0095] R2Cis selected from the group consisting of -H, -OH, -F, -NH2 and a (C1-C3)alkyl group, preferably R2cis -H, a = 1 or 2, preferably a = 1, in formula (IVc) b = 1, 2 or 3,

[0096] X2bis selected from the group consisting of -N(R2p)-, -O-, -S-, -SO-, -SO2-, - NH-, and -CH2-, wherein R2pis selected from the group consisting of -Ac, a (C1-C3)alkyl group and a Z group, wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa) or Xaa2 is a residue of an amino acid of formula (IVc), and more preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0097] Xaa3 is a residue of an α-amino acid formula (Va), or (Vb) optionally comprising a Z group, wherein in formula R3ais 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 - (CH2)eR3c, wherein R3cis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R3Coptionally comprises a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)eR3cwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0098] R3bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R3ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)eR3c, wherein said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH, and -F, preferably an -OH group, or R3bis -H under the proviso that R3ais -H, orR3aand R3bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2and -OH, preferably said cycle is of formula (Vb) in formula (Vb) d = 1, 2 or 3,

[0099] X3ais selected from the group consisting of -N(R30)-, -O-, -S-, -SO-, -SO2, -NH- , and -CH2-, wherein R3° is selected from the group consisting of -Ac, a (C1-C3)alkyl group and a Z group, wherein the carbonyl group of Xaa3 is covalently attached to the a-nitrogen atom of Xaa4, preferably Xaa3 is a residue of an amino acid of formula (Va), more preferably Xaa3 is a residue of an L-a amino acid of formula (Vc) wherein in formula

[0100] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R3g)(R3h)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R31)(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3n, and -NH-CO-R3m, wherein R3d, R3' and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R31is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R3mis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0101] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0102] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl group, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked via a linker, preferably a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0103] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0104] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein R5ais selected from the group consisting of a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0105] Xaa6 is a residue of an L-α-amino acid of formula (Villa), ( VUIb) or (VIIIc) wherein in formula (Villa) f = 1 or 2, preferably f = 1,

[0106] R6ais selected from the group consisting of -H, -OH, -F, and a (C1-C4)alkyl group,

[0107] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C, -Chalky I group, -OH and -F, in formula (VUIb) g = 0, 1 or 2, preferably g = 1, h = 1, 2 or 3, preferably h = 1 or 2, in formula (VIIIc) i = 1 or 2, preferably i= 1 ,

[0108] R6bis selected from the group consisting of a (C2-C6)alkyl group, an aryl group, an aryl group substituted with 1 or 2 substituents, a (C5-C6)heteroaryl group, a (C5-C6)heteroaryl group substituted with 1 or 2 substituents, a (C5-C6)carbocycle, and a (C5-C6)carbocycle substituted with 1 or 2 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1-C6)alkyl group, -CN, -OH, and an -O(C1-C6)alkyl group,

[0109] R6Cis selected from the group consisting of -H and a (C1-C3)alkyl group, and wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7, more preferably Xaa6 is a residue of an amino acid of formula (Villa),

[0110] Xaa7 is a residue of an α-amino acid of formula (IXa), (IXb), (IXc), (IXd), or (IXe), each optionally comprising a Z group, wherein in formula (IXa)

[0111] R7ais selected from the group consisting of -H, -OH, -F, -NH2, and a (C1- C3)alkyl group,

[0112] X7ais absent or selected from the group consisting of -CH(R7f)-, -S-, -O-, and - NH-, wherein R7fis selected from the group consisting of -H, -OH, -F, -NH(R7g) and a (C1-C6)alkyl group, and wherein R7gis selected from the group consisting of -H, -Ac, a (Ci-Cj)alkyl group and a Z group, in formula (IXb) k = 1 or 2, in formula (IXc) m = 1, 2 or 3,

[0113] R7bis selected from the group consisting of -H, and a (C1-C2)alkyl group,

[0114] X7bis absent or selected from the group consisting of -N(R7g)-, -O-, -S-, -SO-, - SO2- and -CH2-, wherein R7gis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, in formula (IXd)

[0115] R7bis selected from the group consisting of -H, and a (C1-C2)alkyl group,

[0116] R7Cis selected from the group consisting of -H, and -(CH2)nR7h, wherein n = 1, 2, or 3, preferably n = 1, and wherein one of the one, two, or three -CH2- groups of -(CH2)nR7hwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO-, or -SO2-, wherein R7his selected from the group consisting of -H, -OH,

[0117] NR7iR7k, -N(CH3)3+, -NH-CNH-NH2, -CONH2, -NH-CO-NH2 and a (C1- C3)alkyl group, an aryl group, a substituted aryl group substituted by one substituent, a heteroaryl group, a heteroaryl group substituted by one substituent, wherein each substituent is preferably selected from the group consisting of a methyl group, a halogen atom, -NH2 and -OH, wherein R71and R7kare each and independently selected from the group consisting of -H and a methyl group, in formula (IXe) R7dis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and - (CH2)OR71, preferably R7dis selected from the group consisting of -(CH2)OR71, R71is selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R71optionally comprises a Z group, o = 1, 2, 3, 4 or 5, and wherein one of the one, two, three, four or five -CH2- groups linking R71to the a-C atom of Xaa7 in formula (IXe) are optionally substituted by a methyl group, and / or wherein one of said -CH2- groups which is different from the terminal groups is optionally replaced by -O-, -S-, - SO-, or -SO2-, preferably R71is selected from the group consisting of -H, -OH,

[0118] N(R7m)(R7n), -N(R7o)(R7p)(R7q)+, -COOH, a halogen atom, -CN, -N3, -NO2,

[0119] -N(R7m)-CN(R7n)-N(R7r)(R7s), -SO2N(R7m)(R7u),

[0120] CON(R7m)(R7u), -NH-CO-N(R7m)(R7u), -SO3H, -R7*, -NH-SO2-R7', and -NH- CO-R7t, wherein R7m, R7rand R7sare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R70and R7pare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R7nis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R7qis selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of -OH, -COOH, and -SO3H, preferably R7qis selected from the group consisting of a methyl group and a -(C^^SOjH group, wherein R7tis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a phenyl group and a (C5-C6)heteroaryl group, and R7tis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R7' is a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R7tis a (C1-C3)alkyl group, wherein R7uis selected from the group consisting of -H and R7t, preferably R7uis selected from the group consisting of -H and a methyl group, most preferably R7Uis -H,

[0121] R7eis selected from the group consisting of -H, and a (C1-C3)alkyl group, wherein said (C1-C3)alkyl group is optionally substituted by a substituent preferably selected from the group consisting of -F, -Cl and -OH, and wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8, preferably Xaa7 is a residue of an amino acid of formula (IXa), (IXd), and (IXe), more preferably Xaa7 is a residue of an amino acid of formula (IXa),

[0122] Xaa8 is a residue of an α-amino acid of formula (Xa) or (Xb) wherein in formula (Xa)

[0123] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the 0-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the 0-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, in formula (Xb) p = 1, 2, or 3, a -CH2- group in the ring of formula (Xb) is optionally replaced by one atom selected from the group consisting of -O- and -S-, and one or more H atoms of the ring -CH2- groups are optionally substituted by -F or -Cl, the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9, and wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0124] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0125] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO, XaalO is a residue of formula (XII), wherein

[0126] RIOaand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0127] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), and -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein R10dand R10eare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal, preferably as disulfide.

[0128] Embodiment 4. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is the blocking group Abl of formula (Ila) wherein XOais selected from the group consisting of -NH-, -S- and -O-, preferably XOais selected from the group consisting of -NH- and -O-, wherein ROais selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROais unsubstituted or substituted, preferably ROais unsubstituted, whrein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROais substituted, ROais substituted by one or two substituents, wherein each and any substitutent is individually and independently different from a polar group or a charged group, preferably each and any subsitutent is individually and independently selected from the group consisting of a(C1-C6)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, and wherein ROais optionally linked to XOaby a linker comprising one or two -CH2- groups, preferably the linker is absent or consists of one -CH2- group, preferably R°ais selected from the group consisting of a (C3-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C3- C6)alkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted,

[0129] Xaal is a residue of an amino acid of formula (III) wherein

[0130] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0131] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of XaalO, preferably as disulfide,

[0132] Xaa2 is a residue of an α-amino acid of formula (IVa) wherein

[0133] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2>CN(R2f)-N(R2k)(R21), -

[0134] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2n, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2sand R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R2' is selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R20is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-, R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -NH2and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0135] Xaa3 is a residue of an α-amino acid formula (Va), or (Vb) optionally comprising a Z group, wherein in formula

[0136] R3ais 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 - (CH2)eR3c, wherein R3cis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R3Coptionally comprises a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)eR3cwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0137] R3bis selected from the group consisting of H and a (C1-C3)alkyl group under the proviso that R3ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)eR3c, wherein said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent preferably is selected from the group consisting of -OH, -COOH, and -F, preferably an -OH group, or R3bis -H under the proviso that R3ais -H, orR3aand R3bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (Vb) in formula (Vb) d = 1, 2 or 3,

[0138] X3ais selected from the group consisting of -N(R30)-, -O-, -S-, -SO-, -SO2-, - NH-, and -CH2-, wherein R3° is selected from the group consisting of -Ac, a (C1-C3)alkyl group and a Z group, wherein the carbonyl group of Xaa3 is covalently attached to the a-nitrogen atom of Xaa4, preferably Xaa3 is a residue of an amino acid of formula (Va), more preferably Xaa3 is a residue of an L-a amino acid of formula (Vc) wherein in formula (Vc)

[0139] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R3g)(R3b)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R3')(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3", and -NH-CO-R31”, wherein R3d, R3' and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CFh^SChH group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R31is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R3mis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0140] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0141] R4ais selected from the group consisting of a (C5-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-Cio)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a(C1- C6)alkyl group, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked via a linker, preferably a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0142] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0143] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein

[0144] R5ais selected from the group consisting of a (C5-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0145] Xaa6 is a residue of an L-α-amino acid of formula (Villa) wherein f = 1 or 2, preferably f = 1,

[0146] R6ais selected from the group consisting of -H, -OH, -F, and a (C1-C4)alkyl group,

[0147] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7,

[0148] Xaa7 is a residue of an α-amino acid of formula (IXa) wherein

[0149] R7ais selected from the group consisting of -H, -OH, -F, -NH2, and a (C1- C3)alkyl group,

[0150] X7ais absent or selected from the group consisting of -CH(R7i)-, -S-, -O-, and - NH-, wherein R7fis selected from the group consisting of -H, -OH, -F, -NH(R7g) and a (C1-C6)alkyl group, and wherein R7gis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0151] Xaa8 is a residue of an α-amino acid of formula (Xa) wherein

[0152] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably RSais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the 0-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the 0-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, and wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9, Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0153] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO,

[0154] XaalO is a residue of formula (XII), wherein

[0155] R10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0156] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), -CON(Rl0d)(R10e), wherein Cterm comprises a Z group, wherein R10dand R10eare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal, preferably as disulfide. Embodiment 5. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1 to 4, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is the blocking group Abl of formula (Ila)

[0157] O

[0158] R°aJLJx (Ila) wherein XOais selected from the group consisting of -NH-, -S- and -O-, preferably XOais selected from the group consisting of -NH- and -O-, wherein ROais selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROais unsubstituted or substituted, preferably ROais unsubstituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROais substituted, ROais substituted by one or two substituents, wherein each and any substituent is different from a polar group or a charged group, preferably each and any substituent is each and individually selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle„ and wherein ROais optionally linked to XOaby a linker comprising one or two -CHj- groups, preferably the linker is absent or consists of one -CH2- group, preferably ROais selected from the group consisting of a (C3-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C3- C6)alkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted,

[0159] Xaal is a residue of an amino acid of formula (III) wherein

[0160] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0161] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0162] Xaa2 is a residue of an α-amino acid of formula (IVa) wherein

[0163] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e)-CN(R2f)-N(R2k)(R21), -

[0164] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2", wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R2' is selected from the group consisting of a methyl group and a -(CH2)SO3H group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2" is selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R2° is a Z group, wherein c = 1 , 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0165] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or, R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0166] Xaa3 is a residue of an α-amino acid formula (Va) optionally comprising a Z group, wherein

[0167] R3ais 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 - (CH2)eR3c, wherein R3cis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R3Coptionally comprises a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)eR3cwhich is different from the terminal groups of Xaa3 is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0168] R3bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R3ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)eR3c, wherein said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH, and -F, preferably an -OH group, or R3bis -H under the proviso that R3ais -H, or R3aand R3bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2and -OH, preferably said cycle is of formula (Vb), wherein the carbonyl group of Xaa3 is covalently attached to the a-nitrogen atom of Xaa4,

[0169] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0170] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl group, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0171] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0172] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein

[0173] R5ais selected from the group consisting of a (C6-C10)aryl and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0174] Xaa6 is a residue of an L-α-amino acid of formula (Villa) (Villa) wherein f = 1 or 2, preferably f = 1,

[0175] R6ais selected from the group consisting of -H, -OH, -F, and a (C1-C4)alkyl group,

[0176] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and -

[0177] NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7,

[0178] Xaa7 is a residue of an α-amino acid of formula (IXa) wherein

[0179] R7ais selected from the group consisting of -H, -OH, -F, -NH2, and a (C1- Cs)alkyl group, X7ais absent or selected from the group consisting of -CH(R7f)-, -S-, -O-, and - NH-, wherein R7fis selected from the group consisting of -H, -OH, -F, -NH(R7g) and a (C1-C6)alkyl group, and wherein R7gis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0180] Xaa8 is a residue of an L-α-amino acid of formula (Xa) wherein

[0181] R8ais selected from the group consisting of a (C4-Cg)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably RSais selected from the group consisting of of a (C4-Cfi)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the 0-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the p-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, and wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0182] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0183] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CHiR9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO,

[0184] XaalO is a residue of formula (XII), wherein

[0185] RIOaand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0186] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein R10dand RIOeare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal, preferably as disulfide. Embodiment 6. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2, 3 and 4, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is the blocking group Abl of formula (Ila)

[0187] O

[0188] R°ayOa JI x (Ila) wherein XOais selected from the group consisting of -NH-, -S- and -O-, preferably XOais selected from the group consisting of -NH- and -O-, wherein ROais selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROais unsubsituted of substituted, preferably ROais unsubstitited, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROais substituted, ROais substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any subustituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, and wherein ROais optionally linked to X°aby a linker comprising one or two -CH2- groups, preferably the linker is absent or consists of one -CH2- group, preferably ROais selected from the group consisting of a (C3-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C3- C6))lkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted,

[0189] Xaal is a residue of an amino acid of formula (III) wherein Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0190] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0191] Xaa2 is a residue of an α-amino acid of formula (IVa) wherein

[0192] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e)-CN(R2f)-N(R2k)(R21), -

[0193] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2”, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2® and R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R21is selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C5-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R2° is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0194] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent preferably is selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0195] Xaa3 is a residue of an α-amino acid of formula (Vc) wherein in formula (Vc)

[0196] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R3g)(R3h)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R3i)(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3n, and -NH-CO-R3m, wherein R3d, R31and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CH^sSOsH group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R31is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R3mis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0197] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0198] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0199] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0200] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein R5ais selected from the group consisting of a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0201] Xaa6 is a residue of an L-α-amino acid of formula (Villa) (Villa) wherein f = 1 or 2, preferably f = 1,

[0202] R6ais selected from the group consisting of -H, -OH, -F, and a (C1-C4)alkyl group,

[0203] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7,

[0204] Xaa7 is a residue of an α-amino acid of formula (IXa) wherein

[0205] R7ais selected from the group consisting of -H, -OH, -F, -NH2, and a (C1- C3)alkyl group,

[0206] X7ais absent or selected from the group consisting of -CH(R7f)-, -S-, -O-, and - NH-, wherein R7fis selected from the group consisting of -H, -OH, -F, -NH(R7g) and a (C1-C6)alkyl group, and wherein R7gis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0207] Xaa8 is a residue of an L-α-amino acid of formula (Xa) wherein

[0208] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the p-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the 0-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0209] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0210] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (Ci-Chalky 1 group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of Xaal 0,

[0211] Xaal 0 is a residue of formula (XII), wherein

[0212] R10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2, R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(0H), -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein R10dand R10eare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal .

[0213] Embodiment ?. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is the blocking group Abl of formula (Ila)

[0214] O

[0215] R°aArx (Ila) wherein XOais selected from the group consisting of -NH-, -S- and -O-, preferably XOais selected from the group consisting of -NH- and -O-, wherein ROais selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROais unsubsituted or substituted, preferably unsubsituted, wherein any of said (C3-Cs)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROais substituted, ROais substituted by one or two substituents, wherein each and any substitutent is different from a polar group or a charged group, preferably each and any substituent is individually and independenetly selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (Cj-Cgjheterocycle, and wherein ROais optionally linked to XOaby a linker comprising one or two -CH2- groups, preferably the linker is absent or consists of one -CH2- group, preferably ROais selected from the group consisting of a (C3-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C3- C6)alkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted,

[0216] Xaal is a residue of an amino acid of formula (III) wherein

[0217] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0218] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0219] Xaa2 is a residue of an α-amino acid of formula (IVa) wherein

[0220] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e>CN(R2f)-N(R2li)(R21), -

[0221] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2n, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R21is selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2inis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R20is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0222] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent preferably is selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of

[0223] Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0224] Xaa3 is a residue of an α-amino acid of formula (Vc) wherein in formula (Vc)

[0225] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R3g)(R3h)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R3i)(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3n, and -NH-CO-R3m, wherein R3d, R3' and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R31is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R3mis a

[0226] (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0227] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0228] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (C5-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0229] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5, Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein

[0230] R5ais selected from the group consisting of a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -Nth, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0231] Xaa6 is a residue of an L-α-amino acid of formula (Villa) (Villa) wherein f = 1 or 2, preferably f = 1,

[0232] R6ais selected from the group consisting of -H, -OH, -F, and a (Ci -C4)alky 1 group,

[0233] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7, Xaa7 is a residue of an α-amino acid of formula (IXd) wherein

[0234] R7bis selected from the group consisting of -H, and a (C1-C2)alkyl group,

[0235] R7Cis selected from the group consisting of -H, and -(CH2)„R7h, wherein n = 1, 2, or 3, preferably n = 1, and wherein one of the one, two, or three -CH2- groups of -(CH2)nR7hwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO-, or -SO2-, wherein R7his selected from the group consisting of -H, -OH,

[0236] NR71R7k, -N(CH3)3+, -NH-CNH-NH2, -CONH2, -NH-CO-NH2 and a (C1- C3)alkyl group, an aryl group, a substituted aryl group substituted by one substituent, a heteroaryl group, a heteroaryl group substituted by one substituent, wherein each substituent is preferably selected from the group consisting of a methyl group, a halogen atom, -NH2 and -OH, wherein R71and R7kare each and independently selected from the group consisting of -H and a methyl group, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0237] Xaa8 is a residue of an L-α-amino acid of formula (Xa) wherein

[0238] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the 0-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the 0-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0239] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0240] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO, XaalO is a residue of formula (XII), wherein

[0241] R10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0242] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), -CON(Rl0d)(R10e), wherein Cterm comprises a Z group, wherein R10dand RIOeare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal .

[0243] Embodiment 8. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is the blocking group Abl of formula (Ila)

[0244] O

[0245] R°avOa JLfx (Ila) wherein XOais selected from the group consisting of -NH-, -S- and -O-, preferably XOais selected from the group consisting of -NH- and -O-, wherein ROais selected from the group consisting of a (C3-C9alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROais unsubstituted or substituted, preferably ROais unsubstituted, whrein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROais substituted, ROais substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any subsituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, and wherein ROais optionally linked to XOaby a linker comprising one or two -CH2- groups, preferably the linker is absent or consists of one -CH2- group, preferably ROais selected from the group consisting of a (Cs-C6)alkyl group, a phenyl group and a (C5-C6)arbocycle, more preferably each and any of the (C3- Cs)alkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted,

[0246] Xaal is a residue of an amino acid of formula (III) wherein

[0247] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0248] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0249] Xaa2 is a residue of an α-amino acid of formula (IVa) wherein

[0250] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2i), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e)-CN(R2f)-N(R2k)(R21), -

[0251] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2", wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R2' is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R2' is selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R2° is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0252] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent preferably is selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0253] Xaa3 is a residue of an α-amino acid of formula (Vc) wherein in formula (Vc)

[0254] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R3g)(R3h)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R31)(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3", and -NH-CO-R3m, wherein R3d, R31and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R31is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R3rais a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0255] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0256] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (Cs-Cio)aryl group, the (C5-C10)heteroaryl group, the (Cs-Cio)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0257] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0258] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein

[0259] RSais selected from the group consisting of a (C6-C10)aryl group and a (Cs-Cio)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0260] Xaa6 is a residue of an L-α-amino acid of formula (Villa) (Villa) wherein f = 1 or 2, preferably f = 1, R6ais selected from the group consisting of -H, -OH, -F, and a (Ci-C^alkyl group,

[0261] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7,

[0262] Xaa7 is a residue of an α-amino acid of formula (IXe) wherein

[0263] R7dis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and - (CH2)OR71, preferably R7dis selected from the group consisting of -(CH2)OR71, R71is selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R71optionally comprises a Z group, o = 1, 2, 3, 4 or 5, and wherein one of the one, two, three, four or five -CH2- groups linking R71to the a-C atom of Xaa7 in formula (IXe) are optionally substituted by a methyl group, and / or wherein one of said -CH2- groups which is different from the terminal groups is optionally replaced by -O-, -S-, - SO-, or -SO2-, preferably R71is selected from the group consisting of -H, -OH,

[0264] N(R7m)(R7n), -N(R7o)(R7p)(R7q)+, -COOH, a halogen atom, -CN, -N3, -NO2,

[0265] -N(R7m)-CN(R7n)-N(R7r)(R7s), -SO2N(R7m)(R7u),

[0266] CON(R7m)(R7u), -NH-CO-N(R7ra)(R7u), -SO3H, -R7', -NH-SO2-R7t, and -NH- CO-R7*, wherein R7m, R7rand R7sare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R7° and R7pare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R7nis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R7qis selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of -OH, -COOH, and -SO3H, preferably R7qis selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R7tis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a phenyl group and a (C5-C6)heteroaryl group, and R7tis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R7' is a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R7tis a (C1-C3)alkyl group, wherein R7uis selected from the group consisting of -H and R7t, preferably R7uis selected from the group consisting of -H and a methyl group, most preferably R7Uis -H,

[0267] R7eis selected from the group consisting of -H, and a (C1-C3)alkyl group, wherein said (C1-C3)alkyl group is optionally substituted by a substituent preferably selected from the group consisting of -F, -Cl and -OH, and wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0268] Xaa8 is a residue of an L-α-amino acid of formula (Xa) wherein

[0269] RSais selected from the group consisting of a (C4-C8)c)rbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (Ci-Cg)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the p-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the p-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (Ci-Cj)alkyl group, preferably -F, -Cl or a methyl group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0270] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0271] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of Xaal 0,

[0272] XaalO is a residue of formula (XII), wherein

[0273] R10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0274] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CHXOH), -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein R10dand R10eare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal .

[0275] Embodiment 9. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is the blocking group Abl of formula (lie) wherein ROcis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis unsubstituted or substituted, preferably ROcis unsubstituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROcis substituted, ROcis substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis optionally linked to the carbonyl moiety in formula (lie) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two -CH2- groups, and wherein one -CH2- group of ROcis optionally replaced by -O- or -S-, preferably ROcis selected from the group consisting of a (C4-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C4- C6)alkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted,

[0276] Xaal is a residue of an amino acid of formula (III) wherein

[0277] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0278] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of XaalO, preferably as disulfide,

[0279] Xaa2 is a residue of an α-amino acid of formula (IVa), wherein

[0280] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e}-CN(R2f)-N(R2k)(R21), -

[0281] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2n, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R2' is selected from the group consisting of a (Ci-Cj)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R21is selected from the group consisting of a methyl group and a grou-p(,CH2)SO3H wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R2° is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0282] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent preferably is selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0283] Xaa3 is a residue of an α-amino acid of formula (Vc), wherein in formula (Vc)

[0284] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R3g)(R3b)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R3')(R3k), -SO2N(R3d)(R3'), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3n, and -NH-CO-R3m, wherein R3d, R3' and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R3' is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R3mis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CHz- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0285] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0286] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0287] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0288] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein

[0289] R5ais selected from the group consisting of a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0290] Xaa6 is a residue of an L-α-amino acid of formula (Villa) (Villa) wherein f = 1 or 2, preferably f = 1,

[0291] R6ais selected from the group consisting of -H, -OH, -F, and a (Ci-C^alkyl group,

[0292] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7,

[0293] Xaa7 is a residue of an α-amino acid of formula (IXa) wherein

[0294] R7ais selected from the group consisting of -H, -OH, -F, -NH2, and a (C1- C3)alkyl group,

[0295] X7ais absent or selected from the group consisting of -CH(R7f)-, -S-, -O-, and - NH-, wherein R7fis selected from the group consisting of -H, -OH, -F, -NH(R7g) and a (C1-C6)alkyl group, and wherein R7gis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0296] Xaa8 is a residue of an L-α-amino acid of formula (Xa) wherein

[0297] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the P-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the p-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0298] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0299] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -C1, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO,

[0300] XaalO is a residue of formula (XII), wherein

[0301] R10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0302] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein R10dand R10eare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal.

[0303] Embodiment 10. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is the blocking group Abl of formula (lIc) wherein ROcis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis unsubstituted or substituted, preferably ROcis unsubstituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROcis substituted, ROcis substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substitutent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis optionally linked to the carbonyl moiety in formula (He) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two -CH2- groups, and wherein one -CH2- group of ROcis optionally replaced by -O- or -S-, preferably ROcis selected from the group consisting of a (C4-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C4- C6)alkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted,

[0304] Xaal is a residue of an amino acid of formula (III) wherein

[0305] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0306] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0307] Xaa2 is a residue of an α-amino acid of formula (IVa) wherein

[0308] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e)-CN(R2f)-N(R2k)(R21), -

[0309] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2n, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R21is selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R20is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0310] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent preferably is selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0311] Xaa3 is a residue of an α-amino acid of formula (Vc) wherein in formula (Vc) R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R38)(R3h)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R3')(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3n, and -NH-CO-R3m, wherein R3d, R31and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3® are each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R31is selected from the group consisting of -H and R3"1, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R31is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R3mis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0312] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0313] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aiyl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0314] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0315] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein

[0316] R5ais selected from the group consisting of a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0317] Xaa6 is a residue of an L-α-amino acid of formula (Villa) (Villa) wherein f = 1 or 2, preferably f = 1,

[0318] R6ais selected from the group consisting of -H, -OH, -F, and a (C1-C4)alkyl group,

[0319] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7,

[0320] Xaa7 is a residue of an α-amino acid of formula (IXd) wherein

[0321] R7bis selected from the group consisting of -H, and a (C1-C2)alkyl group,

[0322] R7Cis selected from the group consisting of -H, and -(CH2)nR7h, wherein n = 1, 2, or 3, preferably n = 1, and wherein one of the one, two, or three -CH2- groups of -(CH2)nR7hwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO-, or -SO2-, wherein R7his selected from the group consisting of -H, -OH,

[0323] NR7iR7k, -N(CH3)3+, -NH-CNH-NH2, -CONH2, -NH-CO-NH2 and a (C1- C3)alkyl group, an aryl group, a substituted aryl group substituted by one substituent, a heteroaryl group, a heteroaryl group substituted by one substituent, wherein each substituent is preferably selected from the group consisting of a methyl group, a halogen atom, -NH2 and -OH, wherein R71and R7kare each and independently selected from the group consisting of -H and a methyl group, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0324] Xaa8 is a residue of an L-α-amino acid of formula (Xa) wherein

[0325] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the p-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the p-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0326] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0327] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO,

[0328] XaalO is a residue of formula (XII), wherein

[0329] R10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0330] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein RIOdand R10eare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of Xaal 0 is covalently attached to the sulfur atom of Xaal .

[0331] Embodiment 11 . The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is the blocking group Abl of formula (lie) wherein ROcis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis unsubstituted or substituted, preferably ROcis unsubstituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROcis substituted, ROcis substituted by one or two substituents, whrein each and any substituted is individually and independent different from a polar group or charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis optionally linked to the carbonyl moiety in formula (lie) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two -CH2- groups, and wherein one -CH2- group of ROcis optionally replaced by -O- or -S-, preferably ROcis selected from the group consisting of a (C4-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C4- C6)alkyl group, a phenyl group and a (C5-C6)carbocycle is unsubstituted,

[0332] Xaal is a residue of an amino acid of formula (III) wherein

[0333] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0334] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0335] Xaa2 is a residue of an α-amino acid of formula (IVa) wherein

[0336] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e)-CN(R2f)-N(R2k)(R21), -

[0337] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2”, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R21is selected from the group consisting of a methyl group and a -(Cffc^SOsH group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R2° is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0338] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent preferably is selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa), Xaa3 is a residue of an α-amino acid of formula (Vc) wherein in formula (Vc)

[0339] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R3g)(R3h)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R3i)(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3", and -NH-CO-R3m, wherein R3d, R31and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R31is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R3mis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1 , 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0340] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0341] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0342] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0343] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein

[0344] R5ais selected from the group consisting of a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- Cj)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0345] Xaa6 is a residue of an L-α-amino acid of formula (Villa) (Villa) wherein f = 1 or 2, preferably f = 1 ,

[0346] R6ais selected from the group consisting of -H, -OH, -F, and a (C1-C4)alkyl group,

[0347] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7,

[0348] Xaa7 is a residue of an α-amino acid of formula (IXe) wherein

[0349] R7dis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and - (CH2)OR71, preferably R7dis selected from the group consisting of -(CH2)OR71, R71is selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R71optionally comprises a Z group, o = 1, 2, 3, 4 or 5, and wherein one of the one, two, three, four or five -CH2- groups linking R71to the a-C atom of Xaa7 in formula (IXe) are optionally substituted by a methyl group, and / or wherein one of said -CH2- groups which is different from the terminal groups is optionally replaced by -O-, -S-, - SO-, or -SO2-, preferably R71is selected from the group consisting of -H, -OH,

[0350] N(R7m)(R7n), -N(R7o)(R7p)(R7q)+, -COOH, a halogen atom, -CN, -N3, -NO2,

[0351] -N(R7m)-CN(R7n)-N(R7r)(R7s), -SO2N(R7m)(R7u),

[0352] CON(R7m)(R7u), -NH-CO-N(R7m)(R7“), -SO3H, -R7t, -NH-SO2-R7t, and -NH- CO-R7t, wherein R7m, R7rand R7sare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R70and R7pare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R7nis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R7qis selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of -OH, -COOH, and -SO3H, preferably R7qis selected from the group consisting of a methyl group and a grou-p(,CH2)SO3H wherein R7tis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a phenyl group and a (C5-C6)heteroaryl group, and R7' is optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R7* is a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R71is a (C1-C3)alkyl group, wherein R7uis selected from the group consisting of -H and R7t, preferably R7uis selected from the group consisting of -H and a methyl group, most preferably R7Uis -H,

[0353] R7eis selected from the group consisting of -H, and a (C1-C3)alkyl group, wherein said (C1-C3)alkyl group is optionally substituted by a substituent preferably selected from the group consisting of -F, -Cl and -OH, and wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0354] Xaa8 is a residue of an L-α-amino acid of formula (Xa) wherein

[0355] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the 0-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the 0-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (Ci-Ca)alkyl group, preferably -F, -Cl or a methyl group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0356] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0357] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of Xaal 0,

[0358] XaalO is a residue of formula (XII), wherein

[0359] R10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0360] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), -CON(Rl0d)(Rl0e), wherein Cterm comprises a Z group, wherein R10dand RIOeare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal.

[0361] Embodiment 12. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1 , 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is XaaO, wherein XaaO is a residue of formula (lid),

[0362] RwO i ll

[0363] Nterrri „ / \ „ /

[0364] ROdROe(iid) wherein

[0365] Rodis selected from the group consisting of a (C2-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROdis unsubstituted or substituted, preferably ROdis unsubstituted, wherein any of said (C2-C8)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if Rodis substituted, Rodis substituted by one or two substituents, whrein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substituted is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- Cs)carbocycle group, an aryl group, a heteroaryl group and a (C3- Cg)heterocycle, wherein ROdis optionally linked to the a-carbon atom of XaaO by a linker comprising one or two -CH2- groups, preferably the linker is absent or comprises one -CH2- group, preferably ROdis selected from the group consisting of a (C2-C5 alkyl group, a (C5-C6)carbocycle, and a phenyl group, more preferably each and any of the (C2-C5 alkyl group, the (C5-C6)carbocycle, and the phenyl group is unsubstituted, wherein ROeis selected from the group consisting of -H, an aryl group, a (C1-C6)alkyl group, and a (C3-C7) carbocycle, preferably ROeis selected from the group consisting of -H and a methyl group, or wherein ROdand ROetogether form a 4-, 5-, 6-, 7- or 8- membered carbocycle or heterocycle, wherein the carbocycle and the heterocycle are optionally substituted by one or two substituents, wherein each substituent is independently selected from the group consisting of a methyl group, -F, -Cl, and -OH, preferably ROdand ROetogether form a (C5-C6) carbocycle, more preferably an unsubstituted (C5-C6) carbocycle, wherein Rofis selected from the group consisting of -H and a (C1-C4)alkyl group, preferably ROfis selected from the group consisting of -H and a methyl group, more preferably Rofis -H, wherein Nterm is selected from the group consisting of -H, -ROg, R°8-CO-, R°8-NH-CO-, R0g-O-CO-, R0g-SO2-, R°8-S-CO-, ROg-NH-CNH-, and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, and wherein Nterm is optionally linked to the a-nitrogen atom of XaaO by a linker comprising one amino acid or a dipeptide, preferably the linker is absent or comprises one α-amino acid or a dipeptide composed of two α-amino acids, most preferably the linker is absent or comprises one amino acid or a dipeptide wherein at least one amino acid comprises a polar or charged side chain, wherein ROgis selected from the group consisting of a (C1-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3- Cs)heterocycle, wherein if R°8is a (C1-C8)alkyl group one of the -CH2- groups in ROgis optionally replaced by -S-, -SO-, -SO2-, -O-, or -NH-, and wherein ROgis optionally substituted by one, two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of -OH, -NHz, a halogen atom, -COOH, -CONHz, -SO3H, -NH- CNH-NH2, a (C1-C6)alkyl group, a (C3-C7)carbocycle, an aryl group, a heteroaryl group, and a (C3-C7)heterocycle, preferably ROgis a (Ci -Chalky 1 group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -NH2, -COOH, -CONH2, -SO3H, -NH-CNH-NH2 and a (C1-C4)alkyl group, more preferably R°8is a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -COOH and -CONH2, preferably Nterm is selected from the group consisting of -H, -ROg, ROg- CO-, R°8-NH-CO- and a Z group, more preferably Nterm is selected from the group consisting of -H, -Ac, a succinyl group, a methyl group and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, Xaal is a residue of an amino acid of formula (III) wherein

[0366] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0367] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0368] Xaa2 is a residue of an α-amino acid of formula (IVa), wherein

[0369] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e>CN(R2f)-N(R2k)(R21), -

[0370] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2n, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2bare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R2' is selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2” is optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R20is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0371] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent preferably is selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of

[0372] Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0373] Xaa3 is a residue of an α-amino acid of formula (Vc), wherein in formula (Vc)

[0374] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R3g)(R3h)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R3i)(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3n, and -NH-CO-R3m, wherein R3d, R31and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R3' is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R3mis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0375] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0376] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0377] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0378] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein

[0379] R5ais selected from the group consisting of a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- Ca)alkyl group, -CN, -NHz, an -O(C1-C3)alkyl group, wherein the (Ci-Cj)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0380] Xaa6 is a residue of an L-α-amino acid of formula (Villa) (Villa) wherein f = 1 or 2, preferably f = 1,

[0381] R6ais selected from the group consisting of -H, -OH, -F, and a (C1-C4)alkyl group,

[0382] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7,

[0383] Xaa7 is a residue of an α-amino acid of formula (IXa) wherein

[0384] R7ais selected from the group consisting of -H, -OH, -F, -NH2, and a (C1- C3)alkyl group,

[0385] X7ais absent or selected from the group consisting of -CH(R7f)-, -S-, -O-, and - NH-, wherein R7fis selected from the group consisting of -H, -OH, -F, -NH(R7g) and a (C1-C6)alkyl group, and wherein R7gis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0386] Xaa8 is a residue of an L-α-amino acid of formula (Xa) wherein

[0387] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the 0-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the 0-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0388] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0389] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO, XaalO is a residue of formula (XII), wherein

[0390] R10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0391] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein R10dand RIOeare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal .

[0392] Embodiment 13. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is XaaO, wherein XaaO is a residue of formula (lid), wherein

[0393] ROdis selected from the group consisting of a (C2-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROdis unsubstituted or substituted, preferably ROdis unsubstituted, wherein any of said (C2-C8)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROdis substituted, Rodis substituted by one or two substituents, wherein each and any substituent is indiviudually and independently different from a polar group or a charged group, preferably each and any substituent is individually and independently selected from the group consisting of a(C1-C6)alkyl group, a (C3- C8)carbocycle group, an aryl group, a heteroaryl group and a (C3- C8)heterocycle, wherein ROdis optionally linked to the a-carbon atom of XaaO by a linker comprising one or two -CH2- groups, preferably the linker is absent or comprises one -CH2- group, preferably ROdis selected from the group consisting of a (C2-C5 alkyl group, a (C5-C6)carbocycle, and a phenyl group, more preferably each and any of the (C2-C5 alkyl group, the (C5-C6)carbocycle and the phenyl group is unsubstituted, wherein ROeis selected from the group consisting of -H, an aryl group, a (C1-C6)alkyl group, and a (C3-C7) carbocycle, preferably ROeis selected from the group consisting of -H and a methyl group, or wherein Rodand ROetogether form a 4-, 5-, 6-, 7- or 8- membered carbocycle or heterocycle, wherein the carbocycle and the heterocycle are optionally substituted by one or two substituents, wherein each substituent is independently selected from the group consisting of a methyl group, -F, -Cl, and -OH, preferably ROdand ROetogether form a (C5-C6) carbocycle, more preferably an unsubstituted (C5-C6) carbocycle, wherein Rofis selected from the group consisting of -H and a (C1-C4)alkyl group, preferably ROfis selected from the group consisting of -H and a methyl group, more preferably Rofis -H, wherein Nterm is selected from the group consisting of -H, -R°8, R°8-CO-, R°8-NH-CO-, R0g-O-CO-, R°8-SO2-, R°8-S-CO-, R°8-NH-CNH-, and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, and wherein Nterm is optionally linked to the a-nitrogen atom of XaaO by a linker comprising one amino acid or a dipeptide, preferably the linker is absent or comprises one α-amino acid or a dipeptide composed of two α-amino acids, most preferably the linker is absent or comprises one amino acid or a dipeptide wherein at least one amino acid comprises a polar or charged side chain, wherein ROgis selected from the group consisting of a (C1-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3- C8)heterocycle, wherein if R°8is a (Ci-Cg)alkyl group one of the -CH2- groups in ROgis optionally replaced by -S-, -SO-, -SO2-, -O-, or -NH-, and wherein ROgis optionally substituted by one, two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of -OH, -NH2, a halogen atom, -COOH, -CONH2, -SO3H, -NH- CNH-NH2, a (C1-C6)alkyl group, a (C3-C7)carbocycle, an aryl group, a heteroaryl group, and a (C3-C7)heterocycle, preferably ROgis a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -NH2, -COOH, -CONH2, -SO3H, -NH-CNH-NH2 and a (C1-C4)alkyl group, more preferably R°8is a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -COOH and -CONH2, preferably Nterm is selected from the group consisting of -H, -R°s, R°8- CO-, R°8-NH-CO- and a Z group, more preferably Nterm is selected from the group consisting of -H, -Ac, a succinyl group, a methyl group and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker,

[0394] Xaal is a residue of an amino acid of formula (III) wherein

[0395] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0396] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0397] Xaa2 is a residue of an α-amino acid of formula (IVa) wherein R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e>CN(R2f)-N(R2k)(R21), -

[0398] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2n, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R21is selected from the group consisting of a methyl group and a grou-p(,CH2)SO3H wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R2° is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0399] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent preferably is selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa),

[0400] Xaa3 is a residue of an α-amino acid of formula (Vc) wherein in formula (Vc)

[0401] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3f)(R3«)(R3b)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R3,)(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3n, and -NH-CO-R3m, wherein R3d, R3' and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CFh^SCbH group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R31is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R3mis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0402] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0403] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aiyl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0404] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0405] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein

[0406] R5ais selected from the group consisting of a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0407] Xaa6 is a residue of an L-α-amino acid of formula (Villa) (Villa) wherein f = 1 or 2, preferably f = 1,

[0408] R6ais selected from the group consisting of -H, -OH, -F, and a (C1-C4)alkyl group,

[0409] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4 alky 1 group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7,

[0410] Xaa7 is a residue of an α-amino acid of formula (IXd) wherein

[0411] R7bis selected from the group consisting of -H, and a (C1-C2)alkyl group,

[0412] R7Cis selected from the group consisting of -H, and -(CH2)nR7h, wherein n = 1, 2, or 3, preferably n = 1, and wherein one of the one, two, or three -CH2- groups of -(CH2)nR7hwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO-, or -SO2-, wherein R7his selected from the group consisting of -H, -OH,

[0413] NR7iR7k, -N(CH3)3+, -NH-CNH-NH2, -CONH2, -NH-CO-NH2 and a (C1- C3)alkyl group, an aryl group, a substituted aryl group substituted by one substituent, a heteroaryl group, a heteroaryl group substituted by one substituent, wherein each substituent is preferably selected from the group consisting of a methyl group, a halogen atom, -NH2 and -OH, wherein R71and R7kare each and independently selected from the group consisting of -H and a methyl group, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0414] Xaa8 is a residue of an L-α-amino acid of formula (Xa) wherein

[0415] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the 0-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups, of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the 0-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0416] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0417] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO,

[0418] XaalO is a residue of formula (XII), wherein

[0419] R10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0420] R10cis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein R10dand RIOeare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal.

[0421] Embodiment 14. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein the N-terminal modification group A is XaaO, wherein XaaO is a residue of formula (lid),

[0422] RwO

[0423] NteriTi _ AoRodR06(lid) wherein

[0424] Rodis selected from the group consisting of a (C2-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein Rodis unsubstituted or substituted, preferably unsubstituted, whrein any of said (C2-C8)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if Rodis substituted, Rodis substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substituent is individually and independent selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle group, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, wherein Rodis optionally linked to the a-carbon atom of XaaO by a linker comprising one or two -CH2- groups, preferably the linker is absent or comprises one -CH2- group, preferably Rodis selected from the group consisting of a (C2-C5 alkyl group, a (C5-C6)carbocycle, and a phenyl group, more preferably each and any of the (C2-C5 alkyl group, the (C5-C6)carbocycle and the phenyl group is unsubstituted, wherein ROeis selected from the group consisting of -H, an aryl group, a (C1-C6)alkyl group, and a (C3-C7) carbocycle, preferably ROeis selected from the group consisting of -H and a methyl group, or wherein ROdand ROetogether form a 4-, 5-, 6-, 7- or 8- membered carbocycle or heterocycle, wherein the carbocycle and the heterocycle are optionally substituted by one or two substituents, wherein each substituent is independently selected from the group consisting of a methyl group, -F, -Cl, and -OH, preferably ROdand ROetogether form a (C5-C6) carbocycle, more preferably an unsubstituted (C5-C6) carbocycle, wherein ROfis selected from the group consisting of -H and a (C1-C4)alkyl group, preferably Rofis selected from the group consisting of -H and a methyl group, more preferably ROfis -H, wherein Nterm is selected from the group consisting of -H, -ROg, R0g-CO-, R0g-NH-CO-, R0g-O-CO-, R0g-SO2-, R0g-S-CO-, ROg-NH-CNH-, and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, and wherein Nterm is optionally linked to the a-nitrogen atom of XaaO by a linker comprising one amino acid or a dipeptide, preferably the linker is absent or comprises one α-amino acid or a dipeptide composed of two α-amino acids, most preferably the linker is absent or comprises one amino acid or a dipeptide wherein at least one amino acid comprises a polar or charged side chain, wherein ROgis selected from the group consisting of a (C1-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3- Cs)heterocycle, wherein if ROgis a (C1-C8)alkyl group one of the -CH2- groups in ROgis optionally replaced by -S-, -SO-, -SO2-, -O-, or -NH-, and wherein ROgis optionally substituted by one, two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of -OH, -NH2, a halogen atom, -COOH, -CONH2, -SO3H, -NH- CNH-NH2, a (C1-C6)alkyl group, a (C3-C7)carbocycle, an aryl group, a heteroaryl group, and a (C3-C7)heterocycle, preferably ROgis a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -NH2, -COOH, -CONH2, -SO3H, -NH-CNH-NH2 and a (C1-C4)alkyl group, more preferably ROgis a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -COOH and -CONH2, preferably Nterm is selected from the group consisting of -H, -ROg, ROg- CO-, R0g-NH-CO- and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, more preferably Nterm is selected from the group consisting of -H, -Ac, a succinyl group, a methyl group and a Z group,

[0425] Xaal is a residue of an amino acid of formula (III) wherein

[0426] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of

[0427] Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of Xaal 0, preferably as disulfide,

[0428] Xaa2 is a residue of an α-amino acid of formula (IVa) wherein

[0429] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2i)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e>CN(R2f)-N(R2k)(R21), -

[0430] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2n, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2® and R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R2' is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R2' is selected from the group consisting of a methyl group and a -(CJ-ysSChH group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2"1is selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R2° is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0431] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent preferably is selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (IVc) wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom of Xaa3, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa), Xaa3 is a residue of an α-amino acid of formula (Vc) wherein in formula (Vc)

[0432] R3Cis selected from the group consisting of -H, -OH, -N(R3d)(R3e), N(R3*)(R3g)(R3h)+, -COOH, a halogen atom, -CN, -N3, -NO2, N(R3d)-CN(R3e)-N(R3')(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH-CO- N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3'”, -CO-R3”, and -NH-CO-R3"1, wherein R3d, R3' and R3kare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R3fand R3® are each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R3his selected from the group consisting of a methyl group and a -(CH2)3SO3H group, wherein R31is selected from the group consisting of -H and R3m, preferably R31is selected from the group consisting of -H and a methyl group, most preferably R31is -H, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R3mis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2and -OH, more preferably R3mis a (C1-C3)alkyl group, wherein R3nis a Z group, wherein e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0433] Xaa4 is a residue of an L-α-amino acid of formula (VI), wherein

[0434] R4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1 , 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C6)alkyl, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked, preferably via a methylene bridge, to the ring system of the (C6-C10)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,

[0435] R4band R4care each and independently selected from the group consisting of - H and a methyl group, and wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom of Xaa5,

[0436] Xaa5 is a residue of an L-α-amino acid of formula (VII), wherein

[0437] R5ais selected from the group consisting of a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1- C3)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group, and wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom of Xaa6,

[0438] Xaa6 is a residue of an L-α-amino acid of formula (Villa) (Villa) wherein f = 1 or 2, preferably f = 1,

[0439] R6ais selected from the group consisting of -H, -OH, -F, and a (C1-C4)alkyl group,

[0440] X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and - NH-, preferably X6is -CH(R6d)- or -S-, wherein R6dis selected from the group consisting of -H, a (C1-C4)alkyl group, -OH and -F, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom of Xaa7,

[0441] Xaa7 is a residue of an α-amino acid of formula (IXe) wherein

[0442] R7dis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and - (CH2)OR71, preferably R7dis selected from the group consisting of -(CH2)OR71, R71is selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R71optionally comprises a Z group, o = 1, 2, 3, 4 or 5, and wherein one of the one, two, three, four or five -CH2- groups linking R71to the a-C atom of Xaa7 in formula (IXe) are optionally substituted by a methyl group, and / or wherein one of said -CH2- groups which is different from the terminal groups is optionally replaced by -O-, -S-, - SO-, or -SO2-, preferably R71is selected from the group consisting of -H, -OH,

[0443] N(R7m)(R7n), -N(R7o)(R7p)(R7q)+, -COOH, a halogen atom, -CN, -N3, -NO2,

[0444] -N(R7m)-CN(R7n)-N(R7r)(R7s), -SO2N(R7m)(R7u),

[0445] CON(R7m)(R7u), -NH-CO-N(R7m)(R7u), -SO3H, -R7*, -NH-SO2-R7t, and -NH- CO-R7', wherein R7m, R7rand R7sare each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R70and R7pare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R7nis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R7qis selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of -OH, -COOH, and -SO3H, preferably R7qis selected from the group consisting of a methyl group and a -(CH^SOaH group, wherein R7tis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a phenyl group and a (C5-C6)heteroaryl group, and R7* is optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, preferably R7tis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R7tis a (C1-C3)alkyl group, wherein R7uis selected from the group consisting of -H and R7t, preferably R7uis selected from the group consisting of -H and a methyl group, most preferably R7Uis -H,

[0446] R7eis selected from the group consisting of -H, and a (C1-C3)alkyl group, wherein said (C1-C3)alkyl group is optionally substituted by a substituent preferably selected from the group consisting of -F, -Cl and -OH, and wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8,

[0447] Xaa8 is a residue of an L-α-amino acid of formula (Xa) wherein

[0448] R8ais selected from the group consisting of a (C4-C8)carbocycle, an aryl group, a heteroaryl group and a -CH(R8b)(R8c) group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, wherein said heteroaryl group comprises only one heteroatom in the ring, preferably R8cis selected from the group consisting of a (C1-C5)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and wherein R8cis optionally linked to the 0-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of RSaor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the 0-carbon atom of Xaa8 in the -CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom of Xaa9,

[0449] Xaa9 is a residue of an α-amino acid of formula (XI) wherein

[0450] R9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl, and wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO,

[0451] XaalO is a residue of formula (XII), wherein

[0452] R10aand RIObare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,

[0453] RIOcis selected from the group consisting of -H, -CO-Cterm, -CONH2, CH2(OH), -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein R10dand R10eare each and independently selected from the group consisting of -H and a methyl group, and the sulfur atom of XaalO is covalently attached to the sulfur atom of Xaal.

[0454] Embodiment 15. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, and the N-terminal modification group A is of formula (Ila), of formula (lib) or of formula (lie) wherein XOais selected from the group consisting of -NH-, -S- and -O-, preferably XOais selected from the group consisting of -NH- and -O-, wherein ROais selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROais unsubstituted or substituted, preferably unsubstituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROais substituted. ROais substituted by one or two substituents, whrein each and any substituent is individually and independently different from a polar or charged group, preferably each and any substitutent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, wherein ROais optionally linked to XOaby a linker comprising one or two -CH2- groups, preferably the linker is absent or consists of one -CH2- group, preferably ROais selected from the group consisting of a (C3-Cs)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C3- C6)alkyl group, a phenyl group and a (C5-C6)carbocycle unsubstituted, wherein RObis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein Robis unsubstituted or substituted, preferably unsubsituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if Robis substituted, Robis substituted by one or two substituent, whrein each and any substituent is individually and independently different from a polar or charged group, preferably each and any substituet is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, wherein RObis optionally linked to the -SO2- moiety in formula (lib) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two - CH2- group, preferably Robis selected from the group consisting of a (C4-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C4- C6)alkyl group, a phenyl group and a (C5-C6)carbocycle is unsubstituted, wherein ROcis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis unsubstitited or substituted, preferably unsubstituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group, and (C3-C8)heterocycle is unsubstituted, and wherein if ROcis substituted, ROcis substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis optionally linked to the carbonyl moiety in formula (He) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two - CH2- group, and wherein one -CH2- group of ROcis optionally replaced by -O- or -S-, preferably ROcis selected from the group consisting of a (C4-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, more preferably each and any of the (C4- Cg)alkyl group, the phenyl group and the (C5-C6)carbocycle is unsubstituted.

[0455] Embodiment 16. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2, 3 and 15, wherein the N-terminal modification group A is of formula (Ila) wherein XOais selected from the group consisting of -NH-, -S- and -O-, wherein ROais selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROais unsubstituted or substituted, preferably ROais unsubstituted, wherein any of said (C3-C9Oalkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROais substituted, ROais substituted by one or two substitutents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substituent is individually and independenetly selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, wherein ROais optionally linked to XOaby a linker comprising one or two -CH2- groups, preferably the linker is absent or consists of one -CH2- group,

[0456] Embodiment 17. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 15 and 16, wherein XOais selected from the group consisting of -NH- and -O-.

[0457] Embodiment 18. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 17, wherein XOais -O-.

[0458] Embodiment 19. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 15, 16, 17 and 18, preferably of Embodiment 18, wherein ROais selected from the group consisting of a (C3-C6)alkyl group, a phenyl group and a (C5- C6)carbocycle, wherein any of said (C3-C6)alkyl group, phenyl group and (C5-C6)carbocycle is optionally substituted by a substituent, wherein the substituent is different from a polar or charged group, preferably any of said (C3-C6)alkyl group, phenyl group and (C5-C6)carbocycle is unsubstituted.

[0459] Embodiment 20. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 19, wherein ROais selected from the group consisting of a (C3- C6)alky I group, wherein said (C3-C6)alkyl group is optionally substituted by a substituent, wherein the substituent is different from a polar group or a charged group, preferably said (C3-C6)alkyl group is unsubstituted, more preferably an n-butyl group.

[0460] Embodiment 21. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2, 3 and 15, wherein the N-terminal modification group A is of formula (lie) wherein ROcis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis unsubstituted or substituted, preferably unsubstituted, wherein any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROcis substituted, ROcis substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substitutent is individually and independent selected from the group consisting of a (C1-C6)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROcis optionally linked to the carbonyl moiety in formula (lie) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two -CH2- group, and wherein one -CH2- group of ROcis optionally replaced by -O- or -S-.

[0461] Embodiment 22. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 15 and 21, wherein ROcis selected from the group consisting of a (C4-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, wherein any of said (C4- C6)alkyl group, phenyl group and (C5-C6)carbocycle is optionally substituted by a substituent and wherein the substituent is different from a polar group or a charged group, preferably any of said (C4- C6)alkyl group, phenyl group and (C5-C6)carbocycle is unsubstituted.

[0462] Embodiment 23. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 22, wherein ROcis selected from the group consisting of a (C4-C6)alkyl group, wherein said (C4-Cfi)alkyl group is optionally substituted by a substituent, and wherein the substituent is different from a polar or charged group, preferably said (C4-C6)alkyl group is unsubstituted.

[0463] Embodiment 24. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2, 3 and 15, wherein the N-terminal modification group A is of formula (lib) (lib), wherein RObis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein RObis unsubstituted or substituted, preferably unsubstituted, wherein any of said (C3-C9alky! group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if RObis substituted, RObis substituted by one or two substituents wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- Cg)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, wherein RObis optionally linked to the -SO2- moiety in formula (lib) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two -CH2- groups, .

[0464] Embodiment 25. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 15 and 24, wherein RObis selected from the group consisting of a (C4-Cfi)alkyl group, a phenyl group and a (C5-C6)carbocycle, wherein any of said (C4- C6)alkyl group, phenyl group and (C5-C6)carbocycle is optionally substituted by a substituent, wherein the substituent is different from a polar or charged group, preferably any of said (C4-Ce)alkyl group, phenyl group and (C5-C6)carbocycle is unsubstituted.

[0465] Embodiment 26. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 25, wherein RObis selected from the group consisting of a (C4- C6)alkyl group, wherein said (C4-C6)alkyl group is optionally substituted by a substituent, wherein the substituent is different from a polar or charged group, preferably said (C4-C6)alkyl group is unsubstituted.

[0466] Embodiment 27. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2 and 3, wherein the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal , and wherein the N-terminal modification group A is XaaO, wherein

[0467] XaaO is a residue of an α-amino acid comprising a side chain and optionally comprising up to three substituents covalently attached to the a-nitrogen atom of XaaO, wherein the side chain comprises a hydrophobic group, and wherein, if present, one substituent covalently attached to the a-nitrogen atom of XaaO is an N-terminal extension group Nterm, and wherein the N-terminal extension group Nterm optionally comprises a Z group, and

[0468] XaaO is a residue of formula (lid) or of formula (lie) Nterrn

[0469] ROdR°® (lid) wherein ROdis selected from the group consisting of a (C2-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROdis unsubstituted or substituted, preferably any of said (C2-C8)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group, and (C3- C8)heterocycle is unsubstituted, and wherein if Rodis substituted, ROdis substituted by one or two substituents, wherein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle group, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein Rodis optionally linked to the a-carbon atom of XaaO by a linker comprising one or two -CH2- groups, preferably the linker is absent or comprises one -CH2- group, preferably ROdis selected from the group consisting of a (C2-C5 alkyl group, a (C5-C6)carbocycle, and a phenyl group, more preferably any of the (C2-C5 alkyl group, the (C5-C6)carbocycle and the phenyl group is unsubstituted, wherein ROeis selected from the group consisting of -H, an aryl group, a (C1-C6)alkyl group, and a (C3- C7) carbocycle, preferably ROeis selected from the group consisting of -H and a methyl group, or wherein ROdand ROetogether form a 4-, 5-, 6-, 7- or 8- membered carbocycle or heterocycle, wherein the carbocycle and the heterocycle are optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -F, -Cl, and -OH, preferably ROdand ROetogether form a (C5-C6) carbocycle, more preferably an unsubstituted (C5-C6) carbocycle, wherein ROfis selected from the group consisting of -H and a (C1-C4)alkyl group, preferably Rofis selected from the group consisting of -H and a methyl group, more preferably ROfis -H, wherein Nterm is selected from the group consisting of -H, -R°8, R°8-CO-, R0g-NH-CO-, R0g-O-CO-, R°8-SO2-, R°8-S-CO-, R°8-NH-CNH-, and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, and wherein Nterm is optionally linked to the a-nitrogen atom of XaaO by a linker comprising one amino acid or a dipeptide, preferably the linker is absent or comprises one α-amino acid or a dipeptide composed of two α-amino acids, most preferably the linker is absent or comprises one amino acid or a dipeptide wherein at least one amino acid comprises a polar or charged side chain, wherein ROgis selected from the group consisting of a (C1-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, wherein if ROgis a (Ci-Cg)alkyl group one of the -CH2- groups in ROgis optionally replaced by -S-, -SO-, -SO2-, -O-, or -NH-, and wherein ROgis optionally substituted by one, two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of -OH, -NH2, a halogen atom, - COOH, -CONH2, -SO3H, -NH-CNH-NH2, a (C1-C6)alkyl group, a (C3-C7)carbocycle, an aryl group, a heteroaryl group, and a (C3-C7)heterocycle, preferably ROgis a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -NH2, -COOH, - CONH2, -SO3H, -NH-CNH-NH2 and a (C1-C4)alkyl group, more preferably ROgis a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of - OH, -COOH and -CONH2, preferably Nterm is selected from the group consisting of -H, ROg, R0g-CO-, R0g-NH-CO- and a Z group, more preferably Nterm is selected from the group consisting of -H, -Ac, a succinyl group, a methyl group and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, wherein ROh, R0' and ROkare each and independently selected from the group consisting of a (C1-C4)alkyl group, preferably Roh, R01and Rokeach are methyl groups.

[0470] Embodiment 28. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiment 1, 2, 3 and 27, wherein

[0471] XaaO is a residue of formula (lid)

[0472] Nterni wherein

[0473] ROdis selected from the group consisting of a (C2-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROdis unsubstituted or substituted, preferably unsubstituted, wherein any of said (C2-C8)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if Rodis substituted, ROdis substituted by one or two substituents, wherein each and any a substituent is individually and independent different from a polar group or a charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3- C8)carbocycle group, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein ROdis optionally linked to the a-carbon atom of XaaO by a linker comprising one or two -CH2- groups, preferably the linker is absent or comprises one -CH2- group, and wherein Rodis optionally substituted by one or two substituents, wherein ROeis selected from the group consisting of -H, an aryl group, a (C1-C6)alkyl group, and a (C3- C7) carbocycle, or wherein ROdand ROetogether form a 4-, 5-, 6-, 7- or 8- membered carbocycle or heterocycle, wherein the carbocycle and the heterocycle are optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -F, -Cl, and -OH, wherein ROfis selected from the group consisting of -H and a (C1-C4 alky 1 group, wherein Nterm is selected from the group consisting of -H, -R°8, R°8-CO-, R°8-NH-CO-, R°8-O-CO-, R°8-SO2-, R0g-S-CO-, R°S-NH-CNH-, and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, and wherein Nterm is optionally linked to the a-nitrogen atom of XaaO by a linker comprising one amino acid or a dipeptide, wherein R°8is selected from the group consisting of a (C1-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, wherein if ROgis a (C1-C8)alkyl group one of the -CH2- groups in ROgis optionally replaced by -S-, -SO-, -SO2-, -O-, or -NH-, and wherein R°8is optionally substituted by one, two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of -OH, -NH2, a halogen atom, - COOH, -CONH2, -SO3H, -NH-CNH-NH2, a (C1-C6)alkyl group, a (C3-C7)carbocycle, an aryl group, a heteroaryl group, and a (C3-C7)heterocycle,

[0474] Embodiment 29. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27 and 28, wherein ROdis selected from the group consisting of a (C2-C5 alkyl group, a (C5-C6)carbocycle, and a phenyl group, wherein any of said (C2-C5 alkyl group, (C5-C6)carbocycle and phenyl group is optionally substituted by a substituent and wherein the substituent is different from a polar or charged group, preferably any of said (C2-C5)alkyl group, (C5-C6iicarbocycle and phenyl group is unsubstituted.

[0475] Embodiment 30. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 28 and 29, preferably Embodiment 29, wherein ROeis selected from the group consisting of -H and a methyl group. Embodiment 31. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 30, wherein ROeis -H.

[0476] Embodiment 32. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 28, 29, 30 and 31 , preferably any one of Embodiments 29, 30 and 31, wherein Rofis selected from the group consisting of -H and a methyl group.

[0477] Embodiment 33. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 32, wherein Rofis -H.

[0478] Embodiment 34. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 28, 29, 30, 31, 32 and 33, preferably any one of Embodiments 29, 30, 31, 32 and 33, wherein Nterm is selected from the group consisting of -H, -ROg, R0g-CO-, R0g-NH-CO- and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker.

[0479] Embodiment 35. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 34, wherein Nterm is selected from the group consisting of -H, -Ac, a succinyl group, a methyl group and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker.

[0480] Embodiment 36. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 28, 29, 30, 31, 32, 33, 34 and 35, preferably any one of Embodiments 29, 30, 31, 32, 33, 34 and 35, wherein ROgis a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -NH2, -COOH, - CONH2, -SO3H, -NH-CNH-NH2 and a (C1-C4)alkyl group.

[0481] Embodiment 37. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 36, wherein ROgis a (C1-C4)alkyl group and is optionally substituted by one substituent preferably selected from the group consisting of -OH, -COOH and -CONH2.

[0482] Embodiment 38. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 28, 29, 30, 31, 32, 33, 34, 35, 36 and 37, wherein Nterm is linked to the a-nitrogen atom of XaaO, preferably without a linker. Embodiment 39. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37 and 38, wherein Nterm is linked to the a-nitrogen atom of XaaO by a linker comprising one amino acid or a dipeptide.

[0483] Embodiment 40. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 39, wherein the linker is a linker comprising one amino acid and the one amino acid is an α-amino acid.

[0484] Embodiment 41. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 39, wherein the linker is a linker comprising a dipeptide, wherein the dipeptide consists of two α-amino acids, wherein at least one of the two α-amino acids comprises a polar or charged side chain.

[0485] Embodiment 42. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40 and 41, wherein XaaO is an L-α-amino acid of formula (lid).

[0486] Embodiment 43. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41 and 42, wherein ROdand ROetogether form a (C5-C6) carbocycle.

[0487] Embodiment 44. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 43, wherein Rodand ROetogether form an unsubstituted (C5-C6) carbocycle.

[0488] Embodiment 45. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1 , 2, 3 and 27, wherein XaaO is a residue of formula (lie) wherein ROdis selected from the group consisting of a (C2-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein Rodis unsubstituted or substituted, preferably unsubsituted, whrerein any of said (C2-C8)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, and wherein if ROdis substituted, Rodis substituted by one or two substituents, whrein each and any substituent is individually and independently different from a polar group or a charged group, preferably each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle group, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein Rodis optionally linked to the a- carbon atom of XaaO by a linker comprising one or two -CH2- groups, preferably the linker is absent or comprises one -CH2- group, wherein ROeis selected from the group consisting of -H, an aryl group, a (C1-C6)alkyl group, and a (C3- C7) carbocycle, or wherein ROdand ROetogether form a 4-, 5-, 6-, 7- or 8- membered carbocycle or heterocycle, wherein the carbocycle and the heterocycle are optionally substituted by one or two substituents, wherein, preferably each substituent is individually and independently selected from the group consisting of a methyl group, -F, -Cl, and -OH, wherein Roh, R°' and ROkare each and independently selected from the group consisting of a (C1-C4)alkyl group.

[0489] Embodiment 46. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27 and 45, wherein ROh, R01and ROkeach are methyl groups.

[0490] Embodiment 47. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 45 and 46, wherein ROdis selected from the group consisting of a (C2-C5 alkyl group, a (C5-C6)carbocycle, and a phenyl group, wherein any of said (C2-C5)alkyl group, (C5-C6)carbocycle and phenyl group is optionally substituted by a substituent, wherein the substituent is different from a polar group or a charged group, preferably any of said (C2-C5)alkyl group, (C5-C6)carbocycle and phenyl group is unsubstitued.

[0491] Embodiment 48. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 45, 46 and 47, preferably any of Embodiments 46 and 47, wherein ROeis selected from the group consisting of -H and a methyl group.

[0492] Embodiment 49. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 48, wherein ROeis -H.

[0493] Embodiment 50. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 45, 46, 47, 48 and 49, wherein XaaO is an L-α-amino acid of formula (He). Embodiment 51. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 27, 45 and 46, wherein Rodand ROetogether form a (C5- C6)carbocycle.

[0494] Embodiment 52. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 51, wherein Rodand ROetogether form an unsubstituted (C5-C6) carbocycle.

[0495] Embodiment 53. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30,31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46,

[0496] 47, 48, 49, 50, 51 and 52, preferably any one of Embodiments 1, 2, 3, 15, 16, 17, 18, 19, 20, 21, 22, 23,

[0497] 24, 25, 26, 27, 28, 29, 30,31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51 and 52, wherein Xaal is a residue of an amino acid of formula (III) wherein

[0498] Rlaand Rlbare each and independently selected from a group consisting of -H and a methyl group, the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of Xaa2, and the sulfur atom of Xaal is covalently attached to the sulfur atom of the thiol group of XaalO.

[0499] Embodiment 54. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 53, wherein the sulfur atom of Xaal is covalently attached as disulfide to the sulfur atom of the thiol group of XaalO.

[0500] Embodiment 55. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18,

[0501] 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30,31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46,

[0502] 47, 48, 49, 50, 51, 52, 53 and 54, preferably any one of Embodiments 1, 2, 3, 15, 16, 17, 18, 19, 20, 21,

[0503] 22, 23, 24, 25, 26, 27, 28, 29, 30,31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49,

[0504] 50, 51, 52, 53 and 54, wherein Xaa2 is a residue of an amino acid of formula (IVa), (IVb), or (IVc) wherein in formul

[0505] R2ais 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 - (CH2)cR2d, preferably R2ais selected from the group consisting of -H and - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, preferably R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2')+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R2e>CN(R2f)-N(R2k)(R21), -

[0506] SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, -R2n, -NH- SO2-R2n, -CO-R20, and -NH-CO-R2", wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2hare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R21is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, preferably R21is selected from the group consisting of a methyl group and a -(CH^SOaH group, wherein R2mis selected from the group consisting of -H and R2n, preferably R2mis selected from the group consisting of -H and a methyl group, most preferably R2mis -H, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aiyl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, preferably R2nis a (Ci -Chalky 1 group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, - NH-CNH-NH2, -NH2 and -OH, more preferably R2nis a (C1-C3)alkyl group, wherein R20is a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0507] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH, preferably said cycle is of formula (IVc) in formula (IVb)

[0508] X2ais selected from the group consisting of -CH2-, -CH(OH), -CH(F)-, CH(NHR2p)-, -NH-, -S- and -O-, wherein R2pis selected from the group consisting of -H, -Ac, a (C1-C4)alkyl and a Z group, preferably R2pis selected from the group consisting of -H, a methyl groupand a Z group, preferably X2ais -CH2-,

[0509] R2Cis selected from the group consisting of -H, -OH, -F, -NH2 and a (C1-C3)alkyl group, preferably R2cis -H, a = 1 or 2, preferably a = 1 , in formula (IVc) b = 1, 2 or 3,

[0510] X2bis selected from the group consisting of -N(R2p)-, -O-, -S-, -SO-, SO2-, -NH-, and -CH2-, wherein R2pis selected from the group consisting of -

[0511] Ac, a (C1-C3)alkyl group and a Z group, preferably Xaa2 is a residue of an L-a amino acid of formula (IVa) or Xaa2 is a residue of an amino acid of formula (IVc), and more preferably Xaa2 is a residue of an L-a amino acid of formula (IVa).

[0512] Embodiment 56. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18,

[0513] 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30,31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46,

[0514] 47, 48, 49, 50, 51, 52, 53, 54 and 55, preferably any one of Embodiments 1, 2, 3, 15, 16, 17, 18, 19, 20,

[0515] 21, 22, 23, 24, 25, 26, 27, 28, 29, 30,31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48,

[0516] 49, 50, 51, 52, 53, 54 and 55, wherein Xaa2 is a residue of an amino acid of formula (IVa) wherein

[0517] R2ais 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 - (CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,

[0518] R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH and -F, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2 and -OH.

[0519] Embodiment 57. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 55 and 56, wherein R2ais selected from the group consisting of -H and -(CH2)cR2d.

[0520] Embodiment 58. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 56 and 57, wherein R2dis selected from the group consisting of -H, -OH, -N(R2e)(R2f), -N(R2g)(R2h)(R2,)+, -COOH, a halogen atom, -CN, -N3, -NO2,

[0521] -N(R2e)-CN(R2f)-N(R2k)(R21), -SO2N(R2e)(R2m), -CON(R2e)(R2m), -NH-CO-N(R2e)(R2m), -SO3H, - R2n, -NH-SO2-R2n, -CO-R20, and -NH-CO-R2n, wherein R2e, R2kand R21are each and independently selected from the group consisting of -H and a (C1-C2)alkyl group, wherein R2gand R2bare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R2fis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, wherein R2' is selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2- C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, wherein R2mis selected from the group consisting of -H and R2n, wherein R2nis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-C10)aryl group and a (C5-C10)heteroaryl group, and R2nis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2 and -OH, wherein R20is a Z group. Embodiment 59. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 58, wherein R2e, R2kand R21are each -H.

[0522] Embodiment 60. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 58, wherein R2gand R2hare each a methyl group.

[0523] Embodiment 61. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any of Embodiments 58 and 59, wherein R2fis selected from the group consisting of -H, a methyl group and a Z group.

[0524] Embodiment 62. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any of Embodiments 58 and 60, wherein R21is selected from the group consisting of a methyl group and a -(CH2)3SO3H group.

[0525] Embodiment 63. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 58, wherein R2nis a (C1-C4)alkyl group which is optionally substituted by a substituent preferably selected from the group consisting of -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH.

[0526] Embodiment 64. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiment 58 and 63, wherein R2nis a (C1-C3)alkyl group.

[0527] Embodiment 65. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any of Embodiments 58 and 59, wherein R2mis selected from the group consisting of -H and a methyl group.

[0528] Embodiment 66. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 65, wherein R2mis H.

[0529] Embodiment 67. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 56 and 57, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged and a zwitterionic group, wherein R2doptionally comprises a Z group.

[0530] Embodiment 68. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 56, 57, 58, 63, 64 and 67, wherein R2dis selected from the group consisting of -H, -OH, -NH2, -NH(R2*), -N(CH3)2, -N(CHs)3+, -COOH, NH-CNH-NH2, -CONH2, -NH-CO-NH2, -SO3H, -CO-R20and -R2n, wherein R2fis selected from the group consisting of -H, a methyl group and a Z group, wherein R20is a Z group, and wherein R2nis selected from the group consisting of a (C1-C3)alkyl group.

[0531] Embodiment 69. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 68, wherein R2dis selected from the group consisting of -H, -OH, - NH2, -NH(R2f), -N(CH3)2, -N(CH3)3+, -NH-CNH-NH2, -CONH2, -NH-CO-NH2and -CO-R20, wherein R2fis selected from the group consisting of -H, a methyl group and a Z group and wherein R2° is a Z group.

[0532] Embodiment 70. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiment 1, 2, 3 and 56, wherein R2bis -H or a (C1-C3)alkyl group which is optionally substituted by -OH under the proviso that R2ais -(CH2)cR2d, or wherein R2bis -H under the proviso that R2ais -H.

[0533] Embodiment 71. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 70, wherein R2bis H.

[0534] Embodiment 72. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70 and 71 , preferably Embodiment 71 , wherein c = 1, 2, or 3, and wherein optionally one hydrogen atom of said one, two or three -CH2- groups of -(CH2)cR2dis substituted by a methyl group, preferably c = 1 , one hydrogen atom is substituted by a methyl group and R2dis OH.

[0535] Embodiment 73. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71 and 72, wherein Xaa2 is a residue of an L-a amino acid of formula (IVa).

[0536] Embodiment 74. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18,

[0537] 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45,

[0538] 46, 47, 48, 49, 50, 51, 52, 53, 54, 55 and 56, preferably any one of Embodiments 1, 2, 3, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45,

[0539] 46, 47, 48, 49, 50, 51, 52, 53, 54, 55 and 56, wherein Xaa2 is a residue of an amino acid of formula

[0540] (IVc) wherein b = 1, 2 or 3,

[0541] X2bis selected from the group consisting of -N(R2p)-, -O-, -S-, -SO-, -SO2-, -NH-, and -CH2-, wherein R2pis selected from the group consisting of -Ac, a (Ci-Cj)alkyl group and a Z group.

[0542] Embodiment 75. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of Embodiment 74, wherein b = 2.

[0543] Embodiment 76. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 74 and 75, wherein X2bis selected from the group consisting of -N(R2p)-, -O-, -NH-, and -CH2-, wherein R2pis selected from the group consisting of a methyl group and a Z group.

[0544] Embodiment 77. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18,

[0545] 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45,

[0546] 46, 47, 48, 49, 50, 51, 52, 53, 54 and 55, preferably any one of Embodiments 1, 2, 3, 15, 16, 17, 18, 19,

[0547] 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46,

[0548] 47, 48, 49, 50, 51, 52, 53, 54 and 55, wherein Xaa2 is a residue of an amino acid of formula (IVb) wherein

[0549] X2ais selected from the group consisting of -CH2-, -CH(OH)-, -CH(F)-, -CH(NHR2p)-, -NH-, - S- and -O-, wherein R2pis selected from the group consisting of -H, -Ac, a (C1-C4alky 1 and a Z group, R2Cis selected from the group consisting of -H, -OH, -F, -NH2and a (C1-C3)alkyl group, a = 1 or 2. Embodiment 78. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 55 and 77, wherein R2pis selected from the group consisting of -H, a methyl group and a Z group.

[0550] Embodiment 79. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 77 and 78, wherein R2cis -H.

[0551] Embodiment 80. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 77and 79, wherein X2ais -CH2-.

[0552] Embodiment 81. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 77, 78, 79 and 80, wherein a = 1.

[0553] Embodiment 82. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of Embodiments 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18,

[0554] 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31 , 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45,

[0555] 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72,

[0556] 73, 74, 75, 76, 77, 78, 79, 80 and, 81, preferably any one of Embodiments 1, 2, 3, 15, 16, 17, 18, 19,

[0557] 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46,

[0558] 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73,

[0559] 74, 75, 76, 77, 78, 79, 80 and 81, wherein Xaa3 is a residue of an amino acid of formula (Va), or (Vb), wherein in formula (Va)

[0560] R3ais selected from the group consisting of -...

Claims

1. Claims1. A compound comprising a cyclic peptide of formula (I)and optionally comprising a C-terminal modification group Cterm covalently attached to XaalO, wherein the C-terminal modification group Cterm comprises a Z group, wherein the peptide sequence is drawn from left to right in N to C-terminal direction,Xaal is a residue of an L-a-amino acid comprising a side chain, wherein the side chain comprises a sulfur atom which is covalently attached to the sulfur atom of the thiol group of XaalO, wherein the carbonyl group of Xaal is covalently attached to the a-nitrogen atom of Xaa2, and whereinXaal is a residue of an amino acid of formula (III)whereinRlaand Rlbare each and independently selected from a group consisting of -H and a methyl group,Xaa2 is a residue of an a-amino acid comprising a side chain, preferably an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a Z group, wherein the carbonyl group of Xaa2 is covalently attached to the a-nitrogen atom ofXaa3 and whereinXaa2 is a residue of an amino acid of formula (IVa), (IVb), or (IVc)wherein in formula (IVa)R2ais 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 -(CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, and wherein R2doptionally comprises a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal -CH2- groups is optionally replaced by -O- , -S-, -SO- or -SO2-,R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (Ci- Ce)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionallysubstituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH and -F, preferably an -OH group, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, in formula (IVb)X2ais selected from the group consisting of -CH2-, -CH(OH)-, -CH(F)-, -CH(NHR2p)-, -NH-, -S- and -O-, wherein R2pis selected from the group consisting of -H, -Ac, a (Ci-C4)alkyl and a Z group,R2Cis selected from the group consisting of -H, -OH, -F, -NH2 and a (C1-C3)alkyl group, a = 1 or 2, in formula (IVc) b = 1, 2 or 3,X2bis selected from the group consisting of -N(R2p)-, -O-, -S-, -SO-, -SO2-, -NH-, and -CH2-, wherein R2pis selected from the group consisting of -Ac, a (C1-C3)alkyl group and a Z group,Xaa3 is a residue of an a-amino acid comprising a side chain, preferably an L-a-amino acid comprising a side chain, wherein the side chain optionally comprises a Z group, wherein the carbonyl group of Xaa3 is covalently attached to the a-nitrogen atom of Xaa4, and whereinXaa3 is a residue of an amino acid of formula (Va), or (Vb),wherein in formula (Va)R3ais 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 -(CH2)eR3c, wherein R3cis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R3coptionally comprises a Z group, wherein e = 1 , 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)eR3cwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,R3bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R3ais selected from the group consisting of a (Ci- C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)eR3c, wherein said (C1-C3)alkyl group is optionally substituted by a substituent, or R3bis -H under the proviso that R3ais -H, or R3aand R3bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, in formula (Vb) d = 1, 2 or 3,X3ais selected from the group consisting of -N(R30)-, -O-, -S-, -SO-, SO2-, -NH-, and -CH2-, wherein R30is selected from the group consisting of -Ac, a (C1-C3)alkyl group and a Z group,Xaa4 is a residue of an L-a-amino acid comprising a side chain, wherein the carbonyl group of Xaa4 is covalently attached to the a-nitrogen atom ofXaa5, and whereinXaa4 is a residue of an amino acid of formula (VI),whereinR4ais selected from the group consisting of a (C6-C10)aryl group, a (C5-C10)heteroaryl group, a (C5-C10)carbocycle and a (C5-C10)heterocycle, and wherein each and any of the (C6-Cio)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle is optionally substituted by 1, 2, or 3 substituents wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1-C6)alkyl group, -CN, -COOH, -CONH2, -NO2, -NH2, -NH-CNH-NH2, -SO3H, -OH, an -O(C1-C6)alkyl group, wherein each substituent is optionally linked to the ring system of the (C6-Cio)aryl group, the (C5-C10)heteroaryl group, the (C5-C10)carbocycle and the (C5-C10)heterocycle, and wherein said (C1-C6)alkyl group is optionally substituted by one or more fluorine atoms,R4band R4care each and independently selected from the group consisting of -H and a methyl group,Xaa5 is a residue of an L-a-amino acid comprising a side chain, wherein the carbonyl group of Xaa5 is covalently attached to the a-nitrogen atom ofXaa6, and whereinXaa5 is a residue of an amino acid of formula (VII),whereinR5ais selected from the group consisting of a (C6-Cio)aryl group and a (C5-C10)heteroaryl group, and wherein each and any one of the (C6-C10)aryl group and the (C5-C10)heteroaryl group is optionally substituted by 1, 2, or 3 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a (C1-C3)alkyl group, -CN, -NH2, an -O(C1-C3)alkyl group, wherein the (C1-C3)alkyl group is optionally substituted by one or more fluorine atoms, wherein R5band R5care each and independently selected from the group consisting of -H and a methyl group,Xaa6 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 Xaa6, wherein the carbonyl group of Xaa6 is covalently attached to the a-nitrogen atom ofXaa7, and whereinXaa6 is a residue of an amino acid of formula (Villa), (Vlllb) or (VIIIc)wherein in formula (Villa) f = 1 or 2,R6ais selected from the group consisting of -F, -H, -OH, and a (Ci-C4)alkyl group,X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and -NH-, wherein R6dis selected from the group consisting of -H, a (Ci-C4)alkyl group, -OH and -F, in formula (Vlllb) g = 0, 1 or 2, h = 1, 2 or 3, in formula (VIIIc)1 = 1 or 2,R6bis selected from the group consisting of a (C2-C6)alkyl group, an aryl group, an aryl group substituted with 1 or 2 substituents, a (C5-C6)heteroaryl group, a (C5-C6)heteroaryl group substituted with 1 or2 substituents, a (C5-C6)carbocycle, and a (C5-C6)carbocycle substituted with 1 or 2 substituents,R6Cis selected from the group consisting of -H and a (C1-C3)alkyl group,Xaa7 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 Xaa7, wherein the side chain optionally comprising a Z group, wherein the carbonyl group of Xaa7 is covalently attached to the a-nitrogen atom of Xaa8, and whereinaal is a residue of an amino acid of formula (IXa), (IXb), (IXc), (IXd), and (IXe)(IXd)wherein in formula (IXa)R7ais selected from the group consisting of -H, -OH, -F, -NH2, and a (Ci- C3)alkyl group,X7ais absent or selected from the group consisting of -CH(R7f)-, -S-, -O- , and -NH-, or is absent, wherein R7fis selected from the group consisting of -OH, -H, -F, - NH(R7g) and a (C1-C6)alkyl group, and wherein R7gis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group, in formula (IXb) k = 1 or 2, in formula (IXc) m = 1, 2 or 3,R7 bis selected from the group consisting of -H, and a (C1-C2)alkyl group, X7bis absent or selected from the group consisting of -N(R7g)-, -O-, -S-, -SO-, -SO2- and -CH2-, wherein R7gis selected from the group consisting of -H, -Ac, a (Ci- C3)alkyl group and a Z group,in formula (IXd)R7bis selected from the group consisting of -H, and a (C1-C2)alkyl group, R7Cis selected from the group consisting of -H, and -(CH2)nR7h, wherein n = 1, 2, or 3, preferably n = 1, and wherein one of the one, two, or three -CH2- groups of -(CH2)nR7hwhich is different from the terminal groups in formula (IXd) is optionally replaced by -O-, -S-, - SO-, or -SO-2, wherein R7his selected from the group consisting of -H, -OH, NR7iR7k, -N(CH3)3+, -NH-CNH-NH2, -CONH2, -NH-CO-NH2 and a (C1- C3)alkyl group, an aryl group, a substituted aryl group substituted by one substituent, a heteroaryl group, a heteroaryl group substituted by one substituent, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -NH2 and -OH, wherein R71and R7kare each and independently selected from the group consisting of -H and a methyl group, in formula (IXe)R7dis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)OR71,R71is selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R71optionally comprises a Z group, o = 1, 2, 3, 4 or 5, and wherein one of the one, two, three, four or five -CH2- groups linking R71to the a-C atom of Xaa7 in formula (IXe) are optionally substituted by a methyl group, and / or wherein one of said -CH2- groups which is different from the terminal groups is optionally replaced by -O-, -S-, -SO-, or -SO2-,R7eis selected from the group consisting of -H, and a (C1-C3)alkyl group, wherein said (C1-C3)alkyl group is optionally substituted by a substituent preferably selected from the group consisting of -F, -Cl and -OH,Xaa8 is a residue of an a-amino acid comprising a side chain, wherein the carbonyl group of Xaa8 is covalently attached to the a-nitrogen atom ofXaa9, and whereinXaa8 is a residue of an amino acid of formula (Xa) or (Xb)wherein in formula (Xa)R8ais selected from the group consisting of a -CH(R8b)(R8c) group, (C4-Cs)carbocycle, an aryl group, and a heteroaryl group, preferably R8ais selected from the group consisting of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, and, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, and wherein R8cis optionally linked to the 0-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, preferably R8cis selected from the group consisting of a (Ci-Cs)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (Ci-Ce)alkyl group of R8care optionally replaced by one atom selected from the group consisting of - O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the 0-carbon atom of Xaa8 in the - CH(R8b)(R8c) group, are optionally replaced by atoms or groups each andindependently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group, in formula (Xb) p = 1, 2, or 3, a -CH2- group in the ring of formula (Xb) is optionally replaced by one atom selected from the group consisting of -O- and -S-, and one or more H atoms of the ring -CH2- groups are optionally substituted by a -F or -Cl atom,Xaa9 is a residue of an a-amino acid comprising a side chain, wherein the carbonyl group of Xaa9 is covalently attached to the nitrogen atom of the amine group of XaalO, and whereinXaa9 is a residue of an amino acid of formula (XI)whereinR9ais selected from the group consisting of a (C1-C3)alkyl group, a (C3-C5)carbocycle and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C4)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, and wherein one or two H atoms in R9aare optionally replaced by -F or -Cl,XaalO is a residue of an amino thiol comprising an amine group, a thiol group and optionally a carbonyl group,wherein the sulfur atom of the thiol group is covalently attached to the sulfur atom of the thiol group of Xaal, and whereinXaalO is a residue of formula (XII),whereinR10aand R10bare each and independently selected from the group consisting of -H and a methyl group, r = 1 or 2,R10cis selected from the group consisting of -CONH2, -H, -CO-Cterm, -CH2(OH), and -CON(R10d)(R10e), wherein Cterm comprises a Z group, wherein R10dand R10eare each and independently selected from the group consisting of -H and a methyl group, an N-terminal modification group A, the N-terminal modification group A is either a hydrophobic blocking group Abl, or XaaO, the N-terminal modification group A is covalently attached to the a-nitrogen atom of Xaal, wherein if the N-terminal modification group A is the blocking group Abl, the blocking group Abl is of formula (Ila), of formula (lib) or of formula (lie)wherein XOais selected from the group consisting of -O-, -NH- and -S- wherein ROais selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3- C8)heterocycle, wherein ROais unsubstituted or substituted, preferablyROais unsubstituted, wherein any of the (C3-C9)alkyl group, the (C3-C8)carbocycle, the aryl group, the heteroaryl group and the (C3- C8)heterocycle is unsubstitued, wherein if ROais substituted, ROais substituted by one or two substituents, wherein, preferably, each and any substituent is individually and independently selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, and wherein ROais optionally linked to XOaby a linker comprising one or two -CH2- groups, wherein RObis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3- Cs)heterocycle, preferably any of said (C3-C9)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstitued, and wherein RObis optionally linked to the -SO2- moiety in formula (lib) by a linker comprising one, two or three -CH2- groups, wherein ROcis selected from the group consisting of a (C3-C9)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3- C8)heterocycle, wherein ROcis unsubstituted or substituted, preferably ROcis unsubstituted, wherein any of the (C3-C9)alkyl group, the (C3-C8)carbocycle, the aryl group, the heteroaryl group and the (C3- C8)heterocycle is unsubstitued, and wherein if ROcis substituted, ROcis substituted by one or two substituents, wherein ROcis optionally linked to the carbonyl moiety in formula (lie) by a linker comprising one, two or three -CH2- groups, preferably the linker is absent or consists of one or two -CH2- groups, wherein one -CH2- group of ROcis optionally replaced by -O- or -S-, - wherein if the N-terminal modification group A is XaaO,XaaO is a residue of an a-amino acid comprising a side chain and optionally comprising up to three substituents covalently attached to the a-nitrogen atom of XaaO, wherein the side chain comprises a hydrophobic group, and wherein, if present, one substituent covalentlyatached to the a-nitrogen atom of XaaO is an N-terminal extension group Nterm, and wherein the N-terminal extension group Nterm optionally comprises a Z group, andXaaO is a residue of formula (lid) or of formula (lie)wherein Rodis selected from the group consisting of a (C2-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group and a (C3- C8)heterocycle, wherein ROdis unsubstituted or substituted, preferably ROdis unsubstituted, wherein any of said (C2-Cs)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, wherein if ROdis substituted, Rodis substituted by one or two substituents, wherein, preferably, each and any substituent is individually independently selected from the group consisting of -OH, - F, -C1, a (C1-C6)alkyl group, a (C3-C8)carbocycle group, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, and wherein ROdis optionally linked to the a-carbon atom of XaaO by a linker comprising one or two - CH2- groups, wherein ROeis selected from the group consisting of -H, an aryl group, a (C1-C6)alkyl group, and a (C3-C7) carbocycle, preferably ROeis selected from the group consisting of -H and a methyl group, or wherein ROdand ROetogether form a 4-, 5-, 6-, 7- or 8- membered carbocycle or heterocycle, wherein the carbocycle and the heterocycle are optionally substituted by one or two substituents, wherein, preferably, each substituent is independently selected from the group consisting of a methyl group, -F, -Cl, and -OH, wherein ROfis selected from the group consisting of -H and a (Ci-C4)alkyl group, wherein Nterm is selected from the group consisting of -H, -ROg, R0g-CO-, R0g-NH-CO-, R0g-O-CO-, R°8-SO2-, R0g-S-CO-, ROg-NH-CNH-, and a Zgroup, wherein if Nterm is a Z group, the Z group preferably comprises a linker, and wherein Nterm is optionally linked to the a-nitrogen atom of XaaO by a linker comprising one amino acid or a dipeptide, wherein ROgis selected from the group consisting of a (C1-C8)alkyl group, a (C3-C8)carbocycle, an aryl group, a heteroaryl group, and a (C3- C8)heterocycle, wherein if ROgis a (C1-C8)alkyl group one of the -CH2- groups in ROgis optionally replaced by -S-, -SO-, -SO2-, -O-, or -NH-, and wherein ROgis optionally substituted by one, two or three substituents, or a pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate thereof.

2. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of claim 1 , wherein the N-terminal modification group A is a blocking group Abl, the blocking group Abl is of formula (Ila)OR°aAtx°a(Ila) wherein XOais selected from the group consisting of -O-, -CH2-, -NH-, and -S-, wherein ROais selected from the group consisting of a (C3-C6)alkyl group, a phenyl group and a (C5-C6)carbocycle, preferably any of said (C3- C6)alkyl group, phenyl group and (C5-C6)carbocycle is unsubstituted.

3. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of claim 1, wherein the N-terminal modification group A is XaaO, whereinXaaO is a residue of formula (lid)wherein ROdis selected from the group consisting of a (C2-C8)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, wherein Rodis substituted or unsubstituted, preferably ROdis unsubstituted, wherein any of the (C2-C8)alkyl group, (C3-C8)carbocycle, aryl group, heteroaryl group and (C3-C8)heterocycle is unsubstituted, wherein if ROdis substituted, Rodis substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of -OH, - F, -Cl, a (C1-C6)alkyl group, a (C3-C8)carbocycle group, an aryl group, a heteroaryl group and a (C3-C8)heterocycle, and wherein ROdis optionally linked to the a-carbon atom of XaaO by a linker comprising one or two -CH2- groups, wherein ROeis selected from the group consisting of -H, an aryl group, a (C1-C6)alkyl group, and a (C3-C7) carbocycle, preferably ROeis selected from the group consisting of -H and a methyl group, or wherein ROdand ROetogether form a 4-, 5-, 6-, 7- or 8- membered carbocycle or heterocycle, wherein the carbocycle and the heterocycle are optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -F, -Cl, and -OH, wherein ROfis selected from the group consisting of -H and a (C1-C4)alkyl group, wherein Nterm is selected from the group consisting of -H, -ROg, R0g-CO-, R0g-NH-CO-, ROg- O-CO-, R0g-SO2-, R0g-S-CO-, ROg-NH-CNH-, and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker, and wherein Nterm is optionally linked to the a-nitrogen atom of XaaO by a linker comprising one amino acid or a dipeptide, wherein ROgis selected from the group consisting of a (C1-C8)alkyl group, a (C3- C8)carbocycle, an aryl group, a heteroaryl group, and a (C3-C8)heterocycle, wherein if ROgis a (C1-C8)alkyl group one of the -CH2- groups in ROgis optionally replaced by -S-, -SO-, -SO2-, -O-, or -NH-, and wherein ROgis optionally substituted by one, two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of -OH, -NH2, a halogen atom, -COOH, -CONH2, -SO3H, -NH-CNH-NH2, a (Ci- C6)alkyl group, a (C3-C7)carbocycle, an aryl group, a heteroaryl group, and a (C3- C7))eterocycle.

4. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of claim 3, whereinROdis selected from the group consisting of a (C2-Cs)alkyl group, a (C5-C6)carbocycle, and a phenyl group, preferably any of said (C2-C5)alkyl group, (C5-C6)carbocycle and phenyl group is unsubstituted,ROeis selected from the group consisting of -H and a methyl group;ROfis selected from the group consisting of -H and a methyl group andNterm is selected from the group consisting of -H, -ROg, R0g-CO-, R0g-NH-CO- and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker.

5. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 4, wherein Xaa2 is a residue of an a- amino acid of formula (IVa)whereinR2ais 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 -(CH2)cR2d, wherein R2dis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R2doptionally comprises a Z group, wherein c = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)cR2dare each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)cR2dwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,R2bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R2ais selected from the group consisting of a (Ci- C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)cR2d, said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH and -F, or R2bis -H under the proviso that R2ais -H, or R2aand R2bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, -COOH, -CONH2, -NH2and -OH, preferably R2bis H and R2ais selected from the group consisting of -H and -(CH2)cR2d.

6. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of claims 5, wherein c = 1, 2, or 3, and wherein optionally one hydrogen atom of said one, two or three -CH2- groups of -(CH2)cR2dis substituted by a methyl group, preferably c = 1 and one hydrogen atom is substituted by a methyl group and R2dis OH.

7. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 6, wherein Xaa3 is a residue of an amino acid of formula (Va),whereinR3ais 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 -(CH2)eR3c,wherein R3cis selected from the group consisting of a polar, a positively charged, a negatively charged, a zwitterionic and a hydrophobic group, wherein R3coptionally comprises a Z group, wherein e = 1 , 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and / or wherein one -CH2- group of -(CH2)eR3cwhich is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-,R3bis selected from the group consisting of -H and a (C1-C3)alkyl group under the proviso that R3ais selected from the group consisting of a (Ci- C6)alkyl group, a (C3-C7)carbocycle, (C3-C7)heterocycle, an aryl group, a heteroaryl group and -(CH2)eR3c, wherein said (C1-C3)alkyl group is optionally substituted by a substituent, wherein the substituent is preferably selected from the group consisting of -OH, -COOH, and -F, or R3bis -H under the proviso that R3ais -H, orR3aand R3bform together a 3-, 4-, 5-, 6-, or 7- membered carbocycle or heterocycle that is optionally substituted by one or two substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, a halogen atom, - NH2and -OH.

8. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 7, wherein Xaa3 is a residue of an L-a amino acid of formula (Vc)whereinR3Cis selected from the group consisting of -N(R3d)(R3e), -H, -OH, - N(R3f)(R3g)(R3h)+, -COOH, a halogen atom, -CN, -N3, -NO2, -N(R3d)-CN(R3e)-N(R3i)(R3k), -SO2N(R3d)(R31), -CON(R3d)(R31), -NH- CO-N(R3d)(R31), -SO3H, -R3m, -NH-SO2-R3m, -CO-R3", and -NH-CO- R3m, wherein R3d, R3' and R3kare each and independently selected from the group consisting of -H and a (Ci-C2)alkyl group, wherein R3fand R3gare each and independently selected from the group consisting of a (C1-C3)alkyl group, wherein R3eis selected from the group consisting of a Z group, -H, -Ac, and a (C1-C3)alkyl group , wherein R3his selected from the group consisting of a (C1-C3)alkyl group and a substituted (C2-C4)alkyl group, wherein the substituted (C2-C4)alkyl group is substituted by at least one substituent preferably selected from the group consisting of OH-, -COOH, and -SO3H, wherein R31is selected from the group consisting of -H and R3m, wherein R3mis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C7)carbocycle, a (C3-C7)heterocycle, a (C6-Cio)aryl group and a (C5-C10)heteroaryl group, and R3mis optionally substituted by one or two or three substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a methyl group, -CONH2, -COOH, a halogen atom, -NH-CNH-NH2, -NH2and -OH, wherein R3nis a Z group, e = 1, 2, 3, 4, or 5, wherein optionally one or two hydrogens of said one, two, three, four or five -CH2- groups of -(CH2)eR3care each and individually substituted by a methyl group, and wherein one -CH2- group which is different from the terminal groups is optionally replaced by -O-, -S-, -SO- or -SO2-.

9. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of claim 8, wherein wherein R3cof formula (Vc) is selected from the group consisting of -NH(R3e) and -CO-R3n, wherein R3eand R3nare each a Z group, preferably R3cis -NH(R3e) and e is 3 or 4.

10. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 9, wherein R4aof formula (VI) is selected from the group consisting of a phenyl group, wherein the phenyl group, is optionally substituted by 1 or 2 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of -F, -Cl, a methyl group, -CN, -CONH2, -NH2, -OH and an -OCH3 group, wherein each substituent is optionally linked via a linker, preferably a methylene bridge, to the ring system of the phenyl group, more preferably R4ais either a 4-carbamoylphenyl or a 3,4-dihydroxyphenyl group.

11. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 10, wherein R5aof formula (VII) is selected from the group consisting of a phenyl group, a 2-thienyl group, a 3 -pyridyl group, an 1 -naphthyl group and a 3 -benzo thienyl group, wherein each and any of these aryl and heteroaryl groups, is optionally substituted by 1 or 2 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of a halogen atom, a methyl group, -CN, -NH2 and an -OCH3 group, wherein the methyl group is optionally substituted by one or more fluorine atoms; more preferably R5ais selected from the group consisting of a phenyl group and a 2-thienyl group, wherein each and any of the phenyl group and a 2-thienyl group, is optionally substituted by 1 or 2 substituents, wherein, preferably, each substituent is individually and independently selected from the group consisting of -F, -Cl and a methyl group, most preferably R5ais a phenyl group.

12. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 11 , wherein Xaa6 is a residue of an L-a-amino acid of formula (Villa)(Villa) wherein f = 1 or 2,R6ais selected from the group consisting of -H, -OH, -F and a (Ci-C4)alkyl group,X6is absent or selected from the group consisting of -CH(R6d)-, -S-, -O- and -NH-, wherein R6dis selected from the group consisting of -H, a (Ci-C4)alkyl group, -OH and -F.

13. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of claim 12, wherein X6is -CH(R6d)- or -S-, and wherein R6dis selected from the group consisting of -F, -H, a (C1-C4)alkyl group and -OH, preferably f = 1, X6is -CH(R6d)-, wherein R6dis selected from the group consisting of -H, a methyl group, -OH and -F, more preferably R6dis -F.

14. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 13, wherein Xaa7 is a residue of an L-a-amino acid of formula (IXa) optionally comprising a Z groupwhereinR7ais selected from the group consisting of -H, -OH, -F, -NH2 and a (C1-C3)alkyl group,X7ais absent or selected from the group consisting of -CH(R7f)-, -S-, -O-, -NH-, wherein R7fis selected from the group consisting of -OH, -H, -F, -NH(R7g) and a (C1-C6)alkyl group, and wherein R7gis selected from the group consisting of -H, -Ac, a (C1-C3)alkyl group and a Z group.

15. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of claim 14, wherein X7ais -CH(R7f)-, and wherein R7fis selected from thegroup consisting of -OH, -H, , -F, -NH(R7g) and a methyl group, and wherein R7gis selected from the group consisting of -H, a methyl group and a Z group, preferably R7fis -OH.

16. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 15, wherein Xaa8 is a residue of an L-a-amino acid of formula (Xa)whereinR8ais selected from the group consisting of a -CH(R8b)(R8c) group, a (C4-C8)carbocycle, an aryl group, and a heteroaryl group, preferably R8ais selected from the group consisting of of a (C4-C6)carbocycle, a phenyl group, a 2-thienyl group and a -CH(R8b)(R8c) group, and, wherein R8bis selected from the group consisting of -H and a (C1-C3)alkyl group, wherein R8cis selected from the group consisting of a (C1-C6)alkyl group, a (C3-C8)carbocycle, an aryl group and a heteroaryl group, and wherein R8cis optionally linked to the 0-carbon atom of Xaa8 by a linker comprising one or or two -CH2- groups, preferably R8cis selected from the group consisting of a (Ci-Cs)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, and, wherein the -CH2- groups of the optional linker or any -CH2- groups of the carbocycle groups of R8aor of the (C1-C6)alkyl group of R8care optionally replaced by one atom selected from the group consisting of - O- and -S-, and wherein one, two or three hydrogen atoms of R8awhich are different from the hydrogen atom bound to the 0-carbon atom of Xaa8 in the - CH(R8b)(R8c) group, are optionally replaced by atoms or groups each and independently selected from the group consisting of a halogen atom and a (C1-C3)alkyl group, preferably -F, -Cl or a methyl group.

17. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of claim 16, wherein R8bis selected from the group consisting of -H and a methyl group, preferably R8bis a methyl group and wherein R8cis selected from the group consisting of a (C2-C4)alkyl group, a (C3-C6)carbocycle, a phenyl group and a 2-thienyl group, preferably R8cis an ethyl group.

18. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 17, wherein Xaa9 is a residue of an L-a-amino acid of formula (XI)whereinR9ais selected from the group consisting of a (C2-C3)alkyl group, a cyclobutyl group and -CH2R9b, wherein R9bis selected from the group consisting of a (C3-C4)carbocycle and a (C1-C3)alkyl group, wherein the -CH2- group linking R9bto the a-C atom of Xaa9 in formula (XI) is optionally substituted by a methyl group, wherein a -CH2- group of R9ais optionally replaced by one atom selected from the group consisting of -O- and -S-, preferably R9ais a n-propyl group.

19. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 18, wherein R10aand R10bare each -H, and wherein R10cis selected from the group consisting of, -CONH2, -CO-Cterm and -CH2(OH), and wherein Cterm is a Z group.

20. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 19,wherein the blocking group Abl is selected from the group consisting of Butoc, Hex, Pen, But, iHex, nBuCAyl, PrCAyl, Oct, EtOPr, Bz, Pha, Chex, Cp and PentylSOi, preferably the blocking group Abl is selected from the group consisting of Butoc, Hex, Pen, iHex, and nBuCAyl, more preferably the blocking group Abl is Butoc; wherein Xaal is a residue of an amino acid selected from the group consisting of Cys and Pen, preferably Xaal is a residue of Cys; wherein Xaa2 is a residue of an amino acid selected from the group consisting of Thr, Arg, Arg(Me), Asp, Glu, Gin, Lys, Lys(Me), Lys(Z), Cit, Ala, Aib, Har, Asn, Glu(Z), 0m(mPEG12), KMe3, Om, Om(Me), Om(Z), Ser, Thp, Ape, Apc(Z), Gly, Pro, Tyr and Leu, wherein Z is a Z group; preferably Xaa2 is a residue of an amino acid selected from the group consisting of Thr, Arg, Arg(Me), Asp, Glu, Gin, Om(DOTA), Lys, Lys(Me), Lys(DOTA), Cit, Ala, Aib, Har, Asn, Glu(AGLU), Om(mPEG12), KMe3, Om, Om(Me), Om(Tris-Nta(Tris)), Ser, Thp, Ape, Apc(DOTA), Gly, Pro, Tyr and Leu; more preefably Xaa2 is a residue of an amino acid selected from the group consisting of Thr and Cit, most preferably Xaa2 is a residue of Thr;Xaa3 is a residue of an amino acid selected from the group consisting of Om(Z), Lys(Z), Met, Arg, Arg(Me), Dap, Dab, Leu, Tyr, Gin, Glu, Glu(Z), Lys(Ac), Cit, Ala, Nle, Asp, Har, Asn, Thr, Apc(Z), Dab(Z), Dap(Z), Lys(AF488-Ttds), Lys, Lys(Me), KMe3, Om, Om(Me), Ser and Gly, wherein Z is a Z group; preferably Xaa3 is a residue of an amino acid selected from the group consisting of Om(DOTA), Lys(DOTA), Met, Arg, Arg(Me), Dap, Dab, Leu, Tyr, Gin, Glu, Lys(Ac), Cit, Ala, Nle, Asp, Har, Asn, Thr, Apc(DOTA), Dab(DOTA), Dap(DOTA), Lys(DOTA-PPAc), Lys(DOTA-asp), Lys(DOTA-PEG12), Lys(DOTA-Kzw), Lys(AF488- Ttds), Lys(NOTA), Lys(NODAGA), Lys, Lys(Me), KMe3, Om, Om(Me), Ser and Gly; more preferably Xaa3 is a residue of an amino acid selected from the group consisting of Om(DOTA), Lys(DOTA), Gin, Dab(DOTA), Dap(DOTA), Lys(NOTA), Lys(NODAGA), Lys(DOTA-PPAc), Lys(DOTA-asp), Lys(DOTA-PEG12) and Lys(DOTA-Kzw),most preferably Xaa3 is a residue of an amino acid selected from the group consisting of Om(DOTA) and Lys(DOTA); wherein Xaa4 is a residue of an amino acid selected from the group consisting of Pcnf, Dopa, Tyr, Phe, Aph, His, Mpa, My, Mcy, Guf, Ppa, Nif, Cha, Trp, Ay3, 2Ni and Ocf, preferablyXaa4 is a residue of an amino acid selected from the group consisting of Pcnf, Dopa, Tyr, Aph, Mpa, Nif, Ocf and My , more preferably Xaa4 is a residue of an amino acid selected from the group consisting of Pcnf and Dopa; wherein Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf, Egm, Mcf, INi, Pnf, Mpa, Bta and Trp, preferably Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf, Egm, Mcf, INi, Pnf and Mpa; more preferably Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf and Egm, most preferably Xaa5 is a residue of Phe; wherein Xaa6 is a residue of an amino acid selected from the group consisting of 4Cfp, Pro, Hyp, Eaz, Oic, Nmb, Leu, Cha, Chy, 4Tfp, Pip, Oxa, Aze and Phe; preferably Xaa6 is a residue of an amino acid selected from the group consisting of 4Cip, Pro and Hyp ,more preferably Xaa6 is a residue of 4Cfp; wherein Xaa7 is a residue of an amino acid selected from the group consisting of Hyp, Pro, 4Cfp, Tap, Ala, Aib, Asp, Ser, Tyr, ser, dap, tyr, Leu, 4Tfp, Chy, 4Ap, ala, Arg, Apc(Z), Tap(Z), Gly, nma, Aze, Oic, Oxa, Lys(Z) and Nmg, wherein Z is a Z group, preferably Z is a Z group comprising a chelator and optionally a linker, wherein the chelator is DOT A; preferably Xaa7 is a residue of an amino acid selected from the group consisting of Hyp, Pro, 4Cfp, Tap, Ala, Aib, 4Tfp, Chy, 4Ap, ala, Arg, Tap(Z), Lys(Z), Ser, ser, Leu, tyr and nma, wherein Z is a Z group comprising a chelator and optionally a linker, preferably the Z group comprises a chelator and no linker, more preferably the chelator is DOTA; even more preferably Xaa7 is a residue of an amino acid selected from the group consisting of Hyp, Pro, Aib, ala, nma, 4Tfp, Lys(DOTA) and Tap, most preferably Xaa7 is a residue of Hyp; wherein Xaa8 is a residue of an amino acid selected from the group consisting of IIe, Chg, Cha, Cpg, Cbg, Npg, Phe, Pcf, Egz, Hfe, Phg, Leu, Nle and Nva; preferably Xaa8 is a residue of an amino acid selected from the group consisting of He, Chg, Cha, Cpg, Phg, Pcf, Cbg and Npg; more preferably Xaa8 is a residue of an amino acid selected from the group consisting of He, Chg, Phg and Cha, most preferably Xaa8 is a residue of He; wherein Xaa9 is a residue of an amino acid selected from the group consisting of Nva, Leu, Cpra, Abu, Ser(Me), Cbg, Npg, Ala, Nle, He and Vai; preferably Xaa9 is a residue of an aminoacid selected from the group consisting of Nva, Leu, Cpra, Abu, Ser(Me) and Cbg; more preferably Xaa9 is a residue of an amino acid selected from the group consisting of Nva, Leu and Cpra, most preferably Xaa9 is a residue of Nva; and / orXaalO is a residue of an amino acid selected from the group consisting of Cys-NFb, Cysol-OH, AET, Hcy-NH2, Pen-NH2 and Cys-O2Oc-Lys(Z)-NH2, wherein Z is a Z group, preferably Z is a Z group comprising a chelator and optionally a linker, wherein the chelator is DOTA; more preferably XaalO is a residue of an amino acid selected from the group consisting of Cys-NFL and Cysol-OH; most preferably XaalO is a residue of Cys-NH2; or any combination of any one of Xaal, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO and blocking group Abl.

21. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 20, wherein a) the blocking group Abl is selected from the group consisting of Butoc, Hex, Pen, But, iHex, nBuCAyl, PrCAyl, Oct, EtOPr, Bz, Pha, Chex, Cp and PentylSO2,Xaal is a residue of an amino acid selected from the group consisting of Cys and Pen,Xaa2 is a residue of an amino acid selected from the group consisting of is a residue of an amino acid selected from the group consisting of Thr, Arg, Arg(Me), Asp, Glu, Gin, Lys, Lys(Me), Lys(Z), Cit, Ala, Aib, Har, Asn, Glu(Z), Om(mPEG12), KMe3, Om, Om(Me), Om(Z), Ser, Thp, Ape, Apc(Z), Gly, Pro, Tyr and Leu,Xaa3 is a residue of an amino acid selected from the group consisting of Om(Z), Lys(Z), Met, Arg, Arg(Me), Dap, Dab, Leu, Tyr, Gin, Glu, Glu(Z), Lys(Ac), Cit, Ala, Nle, Asp, Har, Asn, Thr, Apc(Z), Dab(Z), Dap(Z), Lys(AF488-Ttds), Lys, Lys(Me), KMe3, Om, Om(Me), Ser and Gly,Xaa4 is a residue of an amino acid selected from the group consisting of Pcnf, Dopa, Tyr, Phe, Aph, His, Mpa, My, Mcy, Guf, Ppa, Nif, Cha, Trp, Ay3, 2Ni and Ocf,Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf, Egm, Mcf, INi, Pnf, Mpa, Bta and Trp,Xaa6 is a residue of an amino acid selected from the group consisting of 4Cfp, Pro, Hyp, Eaz, Nmb, Oic, Leu, Cha, Chy, 4Tfp, Pip, Oxa, Aze and Phe,Xaa7 is a residue of an amino acid selected from the group consisting of Hyp, Pro, 4Cfp, Tap, Ala, Aib, Asp, Ser, Tyr, ser, dap, tyr, Leu, 4Tfp, Chy, 4Ap, ala, Arg, Apc(Z), Tap(Z), Gly, nma, Aze, Oic, Oxa, Lys(Z) and Nmg,Xaa8 is a residue of an amino acid selected from the group consisting of lie, Chg, Cha, Cpg, Cbg, Npg, Phe, Pcf, Egz, Hfe, Phg, Leu, Nle and Nva,Xaa9 is a residue of an amino acid selected from the group consisting of Nva, Leu, Cpra, Abu, Ser(Me), Cbg, Npg, Ala, Nle, He and Vai, andXaalO is a residue of an amino acid selected from the group consisting of Cys-NH2, Cysol-OH, AET, Hcy-NH2, Pen-NH2and Cys-O2Oc-Lys(Z)-NH2, wherein Z is a Z group or b) the blocking group Abl is selected from the group consisting of Butoc, Hex, Pen, iHex, and nBuCAyl,Xaal is a residue of Cys,Xaa2 is a residue of an amino acid selected from the group consisting of Thr, Arg, Arg(Me), Asp, Glu, Gin, Om(DOTA), Lys, Lys(Me), Lys(DOTA), Cit, Ala, Aib, Har, Asn,Glu(AGLU), Om(mPEG12), KMe3, Om, Om(Me), Om(Tris-Nta(Tris)), Ser, Thp, Ape, Apc(DOTA), Gly, Pro, Tyr and Leu,Xaa3 is a residue of an amino acid selected from the group consisting of Om(DOTA), Lys(DOTA), Met, Arg, Arg(Me), Dap, Dab, Leu, Tyr, Gin, Glu, Lys(Ac), Cit, Ala, Nle, Asp, Har, Asn, Thr, Apc(DOTA), Dab(DOTA), Dap(DOTA), Lys(DOTA-PPAc), Lys(DOTA-asp), Lys(DOTA-PEG12), Lys(DOTA-Kzw), Lys(AF488-Ttds), Lys(NOTA), Lys(NODAGA), Lys, Lys(Me), KMe3, Om, Om(Me), Ser and Gly,Xaa4 is a residue of an amino acid selected from the group consisting of Pcnf, Dopa, Tyr, Aph, Mpa, Nif, Ocf and My andXaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf, Egm, Mcf, INi, Pnf and Mpa,Xaa6 is a residue of an amino acid selected from the group consisting of 4Cfp, Pro and Hyp,Xaa7 is a residue of an amino acid selected from the group consisting of of Hyp, Pro, 4Cfp, Tap, Ala, Aib, 4Tfp, Chy, 4Ap, ala, Arg, Tap(DOTA), Lys(DOTA), Ser, ser, Leu, tyr and nma,Xaa8 is a residue of an amino acid selected from the group consisting of He, Chg, Cha, Cpg, Phg, Pcf, Cbg and Npg,Xaa9 is a residue of an amino acid selected from the group consisting of Nva, Leu, Cpra, Abu, Ser(Me) and Cbg, andXaalO is a residue of an amino acid selected from the group consisting of Cys-NH2 and Cysol-OH; or c)the blocking group Abl is selected from the group consisting of Butoc, Hex, Pen, iHex and nBuCAyl,Xaal is a residue of Cys,Xaa2 is a residue of an amino acid selected from the group consisting of Thr and Cit,Xaa3 is a residue of an amino acid selected from the group consisting of Om(DOTA), Lys(DOTA), Gin, Dab(DOTA), Dap(DOTA), Lys(NOTA), Lys(NODAGA), Lys(DOTA- PPAc), Lys(DOTA-asp), Lys(DOTA-PEG12) and Lys(DOTA-Kzw),Xaa4 is a residue of an amino acid selected from the group consisting of Pcnf, Dopa, Tyr, Aph, Mpa, Nif, Ocf and My,Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf and Egm,Xaa6 is a residue of an amino acid selected from the group consisting of 4Cfp, Pro and Hyp.Xaa7 is a residue of an amino acid selected from the group consisting of Hyp, Pro, Aib, ala, nma, 4Tfp, Lys(DOTA) and Tap,Xaa8 is a residue of an amino acid selected from the group consisting of He, Phg, Chg and Cha,Xaa9 is a residue of an amino acid selected from the group consisting of Nva, Leu and Cpra, andXaalO is a residue of Cys-NH?.

22. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 19,wherein XaaO is a residue of an amino acid selected from the group consisting of Met, Leu, leu, Ami, Egz, Nva, nva, Nle, nle, Nmb, Phg and Cha, preferably XaaO is selected from the group consisting of Phg, Leu, Nva, Ami, Egz, Nle and Cha, wherein Xaal is a residue of an amino acid selected from the group consisting of Cys and Pen, preferably Xaal is a residue of Cys; wherein Xaa2 is a residue of an amino acid selected from the group consisting of Thr, Arg, Arg(Me), Asp, Glu, Gin, Lys, Lys(Me), Lys(Z), Cit, Ala, Aib, Har, Asn, Glu(Z), 0m(mPEG12), KMe3, Om, Om(Me), Om(Z), Ser, Thp, Ape, Apc(Z), Gly, Pro, Tyr and Leu, wherein Z is a Z group; preferably Xaa2 is a residue of an amino acid selected from the group consisting of Thr, Arg, Arg(Me), Asp, Glu, Gin, Om(DOTA), Lys, Lys(Me), Lys(DOTA), Cit, Ala, Aib, Har, Asn, Glu(AGLU), Om(mPEG12), KMe3, Om, Om(Me), Om(Tris-Nta(Tris)), Ser, Thp, Ape, Apc(DOTA), Gly, Pro, Tyr and Leu; more preefably Xaa2 is a residue of an amino acid selected from the group consisting of Thr and Cit, most preferably Xaa2 is a residue of Thr;Xaa3 is a residue of an amino acid selected from the group consisting of Om(Z), Lys(Z), Met, Arg, Arg(Me), Dap, Dab, Leu, Tyr, Gin, Glu, Glu(Z), Lys(Ac), Cit, Ala, Nle, Asp, Har, Asn, Thr, Apc(Z), Dab(Z), Dap(Z), Lys(AF488-Ttds), Lys, Lys(Me), KMe3, Om, Om(Me), Ser and Gly, wherein Z is a Z group; preferably Xaa3 is a residue of an amino acid selected from the group consisting of Om(DOTA), Lys(DOTA), Met, Arg, Arg(Me), Dap, Dab, Leu, Tyr, Gin, Glu, Lys(Ac), Cit, Ala, Nle, Asp, Har, Asn, Thr, Apc(DOTA), Dab(DOTA), Dap(DOTA), Lys(DOTA-PPAc), Lys(DOTA-asp), Lys(DOTA-PEG12), Lys(DOTA-Kzw), Lys(AF488- Ttds), Lys(NOTA), Lys(NODAGA), Lys, Lys(Me), KMe3, Om, Om(Me), Ser and Gly; more preferably Xaa3 is a residue of an amino acid selected from the group consisting of Om(DOTA), Lys(DOTA), Gin, Dab(DOTA), Dap(DOTA), Lys(NOTA), Lys(NODAGA), Lys(DOTA-PPAc), Lys(DOTA-asp), Lys(DOTA-PEG12) and Lys(DOTA-Kzw),most preferably Xaa3 is a residue of an amino acid selected from the group consisting of Om(DOTA) and Lys(DOTA); wherein Xaa4 is a residue of an amino acid selected from the group consisting of Pcnf, Dopa, Tyr, Phe, Aph, His, Mpa, My, Mcy, Guf, Ppa, Nif, Cha, Trp, Ay3, 2Ni and Ocf, preferably Xaa4 is a residue of an amino acid selected from the group consisting of Pcnf, Dopa, Tyr, Aph,Mpa, Nif, Ocf and My , more preferably Xaa4 is a residue of an amino acid selected from the group consisting of Pcnf and Dopa; wherein Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf, Egm, Mcf, INi, Pnf, Mpa, Bta and Trp, preferably Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf, Egm, Mcf, INi, Pnf and Mpa; more preferably Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf and Egm, most preferably Xaa5 is a residue of Phe; wherein Xaa6 is a residue of an amino acid selected from the group consisting of 4Cfp, Pro, Hyp, Eaz, Oic, Nmb, Leu, Cha, Chy, 4Tfp, Pip, Oxa, Aze and Phe; preferably Xaa6 is a residue of an amino acid selected from the group consisting of 4Cfp, Pro and Hyp, more preferably Xaa6 is a residue of 4Cfp; wherein Xaa7 is a residue of an amino acid selected from the group consisting of Hyp, Pro, 4Cfp, Tap, Ala, Aib, Asp, Ser, Tyr, ser, dap, tyr, Leu, 4Tfp, Chy, 4Ap, ala, Arg, Apc(Z), Tap(Z), Gly, nma, Aze, Oic, Oxa, Lys(Z) and Nmg, wherein Z is a Z group comprising a chelator and optionally a linker, preferably the Z group comprises a chelator and no linker, more preferably the chelator is DOTA; more preferably Xaa7 is a residue of an amino acid selected from the group consisting of Hyp, Pro, 4Cfp, Tap, Ala, Aib, 4Tfp, Chy, 4Ap, ala, Arg, Tap(Z), Lys(Z), Ser, ser, Leu, tyr and nma, wherein Z is a Z group comprising a chelator and optionally a linker, preferably the Z group comprises a chelator and no linker, more preferably the chelator is DOTA; even more preferably Xaa7 is a residue of an amino acid selected from the group consisting of Hyp, Pro, Aib, ala, nma, 4Tfp, Lys(DOTA) and Tap, most preferably Xaa7 is a residue of Hyp; wherein Xaa8 is a residue of an amino acid selected from the group consisting of He, Chg, Cha, Cpg, Cbg, Npg, Phe, Pcf, Egz, Hfe, Phg, Leu, Nle and Nva; preferably Xaa8 is a residue of an amino acid selected from the group consisting of He, Chg, Cha, Cpg, Phg, Pcf, Cbg and Npg; more preferably Xaa8 is a residue of an amino acid selected from the group consisting of He, Chg, Phg and Cha, most preferably Xaa8 is a residue of He; wherein Xaa9 is a residue of an amino acid selected from the group consisting of Nva, Leu, Cpra, Abu, Ser(Me), Cbg, Npg, Ala, Nle, He and Vai; preferably Xaa9 is a residue of an aminoacid selected from the group consisting of Nva, Leu, Cpra, Abu, Ser(Me) and Cbg; more preferably Xaa9 is a residue of an amino acid selected from the group consisting of Nva, Leu and Cpra, most preferably Xaa9 is a residue of Nva; and / orXaalO is a residue of an amino acid selected from the group consisting of Cys-NH?, Cysol-OH, AET, Hcy-NH?, Pen-NFL and Cys-O2Oc-Lys(Z)-NH2, wherein Z is a Z group, preferably Z is a Z group comprising a chelator and optionally a linker, wherein the chelator is DOTA; more preferably XaalO is a residue of an amino acid selected from the group consisting of Cys-NH? and Cysol-OH; most preferably XaalO is a residue of Cys-NHz; or any combination of any one of Xaal, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6, Xaa7, Xaa8, Xaa9, XaalO and XaaO.

23. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 19 and 22, wherein a)XaaO is a residue of an amino acid selected from the group consisting of Met, Leu, leu, Ami, Egz, Nva, nva, Nle, nle, Nmb, Phg and Cha,Xaal is a residue of an amino acid selected from the group consisting of Cys and Pen,Xaa2 is a residue of an amino acid selected from the group consisting of is a residue of an amino acid selected from the group consisting of Arg, Arg(Me), Asp, Glu, Gin, Lys, Lys(Me), Lys(Z), Cit, Ala, Aib, Har, Asn, Thr, Glu(Z), Om(mPEG12), KMe3, Om, Om(Me), Om(Z), Ser, Ape, Apc(Z), Gly, Pro, Tyr and Leu,Xaa3 is a residue of an amino acid selected from the group consisting of Met, Arg, Arg(Me), Dap, Dab, Leu, Tyr, Gin, Glu, Glu(Z), Lys(Ac), Lys(Z), Cit, Ala, Nle, Asp, Har, Asn, Thr, Apc(Z), Om(Z), Dab(Z), Dap(Z), Lys(AF488-Ttds), Lys, Lys(Me), KMe3, Om, Om(Me), Ser and Gly,Xaa4 is a residue of an amino acid selected from the group consisting of Tyr, Dopa, Phe, Aph, His, Mpa, My, Mcy, Guf, Ppa, Nif, Pcnf, Cha, Trp, Ay3, 2Ni and Ocf,Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf, Egm, Mcf, INi, Pnf, Mpa, Bta and Trp,Xaa6 is a residue of an amino acid selected from the group consisting of Pro, 4Cfp, Hyp, Eaz, Oic, Leu, Cha, Chy, 4Tfp, Pip, Oxa, Aze and Phe,Xaa7 is a residue of an amino acid selected from the group consisting of Pro, 4Cfp, Hyp, Tap, Ala, Aib, Asp, Ser, Tyr, ser, dap, tyr, Leu, 4Tfp, Chy, 4Ap, ala, Arg, arg, Apc(Z), Tap(Z), Gly, nma, Aze, Oic, Oxa, Nmr, Lys(Z) and Nmg,Xaa8 is a residue of an amino acid selected from the group consisting of He, Chg, Cha, Cpg, Cbg, Npg, Phe, Pcf, Egz, Hfe, Phg, Leu, Nle and Nva,Xaa9 is a residue of an amino acid selected from the group consisting of Leu, Nva, Cpra, Abu, Ser(Me), Cbg, Npg, Ala, Nle, He and Vai, andXaalO is a residue of an amino acid selected from the group consisting of Cys-NH?, Cysol-OH, AET, Hcy-NH2, Pen-NH2and Cys-O2Oc-Lys(Z)-NH2, wherein Z is a Z group, and wherein an N-terminal modification group Nterm is covalently attached to the a- nitrogen atom of XaaO, wherein Nterm is preferably selected from the group consisting of a - Ac, a methyl group and a Z group wherein if Nterm is a Z group, the Z group preferably comprises a linker; or b)XaaO is a residue of an amino acid selected from the group consisting of Phg, Leu, Nva, Ami, Egz, Nle and Cha,Xaal is a residue of Cys,Xaa2 is a residue of an amino acid selected from the group consisting of Arg, Arg(Me), Asp, Glu, Gin, Om(DOTA), Lys, Lys(Me), Lys(DOTA), Cit, Ala, Aib, Har, Asn, Thr, Glu(AGLU), Om(mPEG12), KMe3, Om, Om(Me), Om(Tris-Nta(Tris)), Ser, Ape, Apc(DOTA), Gly, Pro, Tyr and Leu,Xaa3 is a residue of an amino acid selected from the group consisting of Met, Arg, Arg(Me), Dap, Dab, Leu, Tyr, Gin, Glu, Lys(Ac), Lys(DOTA), Cit, Ala, Nle, Asp, Har, Asn, Thr, Apc(DOTA), Om(DOTA), Dab(DOTA), Dap(DOTA), Lys(DOTA-PPAc), Lys(DOTA- asp), Lys(DOTA-PEG12), Lys(DOTA-Kzw), Lys(AF488-Ttds), Lys(NOTA), Lys(NODAGA), Lys, Lys(Me), KMe3, Om, Om(Me), Ser and Gly,Xaa4 is a residue of an amino acid selected from the group consisting of Tyr, Dopa, Aph, Mpa, Nif, Ocf, My and Pcnf,Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf, Egm, Mcf, INi, Pnf and Mpa,Xaa6 is a residue of an amino acid selected from the group consisting of Pro, 4Cfp and Hyp,Xaa7 is a residue of an amino acid selected from the group consisting of of Pro, 4Cfp, Hyp, Tap, Ala, Aib, 4Tfp, Chy, 4Ap, ala, Arg, Tap(DOTA), Lys(DOTA), Ser, ser, Leu, tyr and nma,Xaa8 is a residue of an amino acid selected from the group consisting of He, Chg, Cha, Cpg, Phg, Pcf, Cbg and Npg,Xaa9 is a residue of an amino acid selected from the group consisting of Leu, Nva, Cpra, Abu, Ser(Me) and Cbg, andXaalO is a residue of an amino acid selected from the group consisting of Cys-NH2 and Cysol-OH, and wherein an N-terminal modification group Nterm is covalently attached to the a- nitrogen atom of XaaO, wherein Nterm is preferably selected from the group consisting of a -Ac, a methyl group and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker; or c)XaaO is a residue of an amino acid selected from the group consisting of Phg, Leu, Nva, Ami, Egz, Nle and Cha,Xaal is a residue of Cys,Xaa2 is a residue of an amino acid selected from the group consisting of Thr and Cit,Xaa3 is a residue of an amino acid selected from the group consisting of Gin, Lys(DOTA), Om(DOTA), Dab(DOTA), Dap(DOTA), Lys(NOTA), Lys(NODAGA), Lys(DOTA-PPAc), Lys(DOTA-asp), Lys(DOTA-PEG12) and Lys(DOTA-Kzw),Xaa4 is a residue of an amino acid selected from the group consisting of Tyr, Dopa, Aph, Mpa, Nif, Ocf, My and Pcnf,Xaa5 is a residue of an amino acid selected from the group consisting of Phe, Thi, Pcf, Ocf and Egm,Xaa6 is a residue of an amino acid selected from the group consisting of Pro, 4Cfp and Hyp.Xaa7 is a residue of an amino acid selected from the group consisting of Pro, Aib, Hyp, ala, nma, 4Tfp, Lys(DOTA) and Tap,Xaa8 is a residue of an amino acid selected from the group consisting of He, Phg, Chg and Cha,Xaa9 is a residue of an amino acid selected from the group consisting of Leu, Nva and Cpra, andXaalO is a residue of Cys-NHi, and wherein an N-terminal modification group Nterm is covalently attached to the a- nitrogen atom of XaaO, wherein Nterm is preferably selected from the group consisting of a -Ac, a methyl group and a Z group, wherein if Nterm is a Z group, the Z group preferably comprises a linker.

24. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 23, wherein each Z group is each and independently selected from the group consisting of a chelator optionally comprising a linker moiety L and a bio-distribution modifier optionally comprising a linker.

25. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 24, wherein each Z group is each and independently a chelator optionally comprising a linker moiety L; preferably the chelator is selected from the group consisting of DOTA, DOTAGA, Crown, DOTP, NOTA, NODAGA, NODA-MPAA, HBED, TETA, CB-TE2A, DTP A, DOT AM, 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) and99mTc(CO)3-chelators; preferably the chelator is selected from the group consisting of DOTA, DOTAGA, Crown, NOTA, NODAGA, NODA-MPAA, CB-TE2A, CHX-A”-DTPA, DFO, Macropa, THP, AAZTA, NOPO, PCTA, sarcophagine, NETA, H4CHXoctapa, H4pypa and N4, more preferably the chelator is selected from the group consisting of DOTA, Macropa, NOTA and NODAGA, and most preferably the chelator is DOTA.

26. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 25, wherein the compound is selected from the group consisting ofcompound Butoc-[Cys-Thr-Om(DOTA)-Pcnf-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-276)compound Butoc-[Cys-Thr-Lys(DOTA)-Dopa-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-249) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA)-Tyr-Phe-Hyp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-128) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA)-Tyr-Thi-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-134) of the following formulacompound Pent-[Cys-Thr-Lys(DOTA)-Tyr-Phe-Hyp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-135) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Mpa-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-138) of the following formulacompound Hex-Lys(DOTA)-Leu-[Cys-Arg-Met-Tyr-Phe-Pro-Ala-Ile-Leu-Cys]-NH2 (UPAR-compound iHex-[Cys-Cit-Gln-Tyr-Phe-Pro-Lys(DOTA)-Ile-Leu-Cys]-NH2 (UPAR-145) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Guf-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-149) of the following formulacompound Pent-[Cys-KMe3-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-153) of the following formulacompound iHex-[Cys-Lys(DOTA)-Gln-Tyr-Phe-Pro-ala-Ile-Leu-Cys]-NH2 (UPAR-157) of the following formula, compound Ac-Leu-[Cys-Arg-Lys(DOTA)-Tyr-Phe-Pro-ala-Ile-Leu-Cys]-NH2 (UPAR-162) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA)-Mpa-Phe-4Cip-Hyp-Ile-Nva-Cys]-NH2 (UPAR-165) of the following formulacompound iHex-[Cys-Arg-Lys(DOTA)-Tyr-Phe-Pro-ala-Ile-Leu-Cys]-NH2 (UPAR-176) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA-PPAc)-Tyr-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2(UPAR-181) of the following formulacompound Ac-Asp-Leu-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-ala-Ile-Leu-Cys]-NH2 (UPAR- 189) of the following formulacompound Butoc-[Cys-Thr-Om(DOTA)-Tyr-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-192) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA-Kzw)-Dopa-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2(UPAR-194) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA-PPAc)-Dopa-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2compound Pent-[Cys-Cit-Lys(DOTA-PEG12)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR- 200) of the following formulacompound PrCAyl-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2(UPAR-210) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Chy-Ile-Nva-Cys]-NH2(UPAR-214) of the following formulacompound Pent-[Cys-Om(Tris-Nta(Tris))-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2(UPAR-224) of the following formulacompound Butoc-[Cys-Thr-Dab(DOTA)-Tyr-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2(UPAR-228) of the following formulacompound DOTA-O2Oc-Leu-[Cys-Cit-Gln-Tyr-Phe-Pro-Pro-Ile-Leu-Cys]-NH2 (UPAR-229) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Pcf-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-233) of the following formulacompound Butoc-[Cys-Thr-Om(DOTA)-Ay3-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-234) of the following formulacompound Hex-Asp-Leu-[Cys-Lys(DOTA)-Met-Tyr-Phe-Pro-Ala-Ile-Leu-Cys]-NH2 (UPAR-235) Of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA)-Tyr-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-237) of the following formulacompound iHex-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Leu-Cys]-NH2 (UPAR-240) of the following formulacompound nBuCAyl-[Cys-Thr-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UP AR- 242) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-4Tfp-Ile-Nva-Cys]-NH2 (UPAR-246) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-248) of the following formulacompound Butoc-[Cys-Thr-Lys(NOTA)-Dopa-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UP AR-250) of the following formulacompound iHex-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-ala-Ile-Leu-Cys]-NH2 (UPAR-256) of thecompound Pent-[Cys-Cit-Lys(DOTA)-Nif-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-257) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-261) of the following formulacompound Butoc-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-275) of the following formulacompound Pent-[Cys-Har-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-278) of the following formulacompound Butoc-[Cys-Thr-Oni(DOTA)-Dopa-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-compound Pent-[Cys-Asn-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-283) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA)-Dopa-Phe-Hyp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-284)compound Butoc-[Cys-Thr-Lys(DOTA)-Tyr-Phe-Pro-4Tfp-Ile-Nva-Cys]-NH2 (UPAR-289) ofcompound DOTA-Ahx-Leu-[Cys-Arg-Gln-Tyr-Phe-Pro-ala-Ile-Leu-Cys]-NH2 (UPAR-291) of the following formulacompound Succinyl-Nva-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR- 293) of the following formulacompound Succinyl-Nva-[Cys-Thr-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2(UPAR-compound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Aib-Ile-Nva-Cys]-NH2 (UPAR-299) ofcompound Pent-[Cys-Thr-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-301) of the following formulacompound Butoc-[Cys-Cit-Lys(DOTA)-Tyr-Pcf-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-304) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Egm-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-315) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Aph-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-320) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-4Ap-Ile-Nva-Cys]-NH2 (UPAR-325) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Ppa-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-336) of the following formulacompound Pent-[Cys-Ser-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2(UPAR-342) of the following formulacompound nBuCAyl-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-346) of the following formulacompound DOTA-Ttds-Nle-Asp-Leu-[Cys-Arg-Met-Tyr-Phe-Pro-Ala-Ile-Leu-Cys]-NH2 (UPAR-347) of the following formulacompound Hex-Asp-Leu-[Cys-Arg-Met-Tyr-Phe-Pro-Lys(DOTA)-Ile-Leu-Cys]-NH2 (UPAR- 351) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Thi-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-360) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Tap-Ile-Nva-Cys]-NH2 (UPAR-377) ofcompound Butoc-[Cys-Thr-Lys(DOTA)-Tyr-Pnf-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-378) of the following formulacompound iHex-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Pro-Ile-Leu-Cys]-NH2 (UPAR-382) of the following formulacompound Pent-[Cys-Om(mPEG12)-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2(UPAR-383) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-nma-Ile-Nva-Cys]-NH2 (UPAR-384) of the following formulacompound iHex-[Cys-Cit-Gln-Tyr-Phe-Pro-Tap(DOTA)-Ile-Leu-Cys]-NH2 (UPAR-389) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Pro-Ile-Leu-Cys]-NH2 (UPAR-396) of thecompound Pent-[Cys-Cit-Lys(DOTA)-Dopa-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-399) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Hyp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-403) of the following formulacompound Butoc-[Cys-Thr-Om(DOTA)-My-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-415) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA-Kzw)-Tyr-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR- 422) of the following formulacompound Ac-Asp-Leu-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Arg-Ile-Leu-Cys]-NH2 (UPAR- 423) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA-asp)-Tyr-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UP AR-compound Hex-Asp-Leu-[Cys-Arg-Lys(DOTA)-Tyr-Phe-Pro-Ala-Ile-Leu-Cys]-NH2 (UPAR- 427) of the following formulacompound Butoc-[Cys-Thr-Lys(NODAGA)-Dopa-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UP AR-444) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Ocf-Pro-Hyp-Ile-Nva-Cys]-NH2 (UPAR-450) ofcompound iHex-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Aib-Ile-Leu-Cys]-NH2 (UPAR-452) of the following formulacompound Butoc-[Cys-Thr-Dap(DOTA)-Tyr-Phe-4CQ)-Hyp-Ile-Nva-Cys]-NH2 (UPAR-455) of the following formulacompound Butoc-[Cys-Thr-Dab(DOTA)-Dopa-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR- 456) of the following formulacompound Butoc-[Cys-Thr-Lys(DOTA-asp)-Dopa-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR- 459) of the following formulacompound iHex-[Cys-Lys(DOTA)-Gln-Tyr-Phe-Pro-Pro-Ile-Leu-Cys]-NH2 (UPAR-466) of the following formulacompound Pent-[Cys-Glu-Lys(DOTA)-Tyr-Phe-Pro-Hyp-Ile-Nva-Cys]-NH2(UPAR-471) of the following formulacompound Pent-[Cys-Cit-Lys(DOTA)-Tyr-Phe-Pro-Pro-Ile-Nva-Cys]-NH2(UPAR-473) of the following formulacompound Butoc-[Cys-Cit-Lys(DOTA)-Tyr-Pcf-4Cfp-Hyp-Chg-Nva-Cys]-NH2(UPAR-476) of the following formulacompound Butoc- [Cy s-Thr-Om(DOT A)-Pcnf-Phe-4Cfp-Hyp-Ile-Cpra-Cy s] -NH2 (UP AR-498) of the following formulacompound Succinyl-Aml-[Cys-Thr-Om(DOTA)-Pcnf-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2 (UPAR-499) of the following formulaand compound Succinyl-Egz-[Cys-Thr-Om(DOTA)-Pcnf-Phe-4Cfp-Hyp-Ile-Nva-Cys]-NH2(UPAR-500) of the following formulaor pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of each and any thereof.

27. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 26, wherein the compound comprises a diagnostically active nuclide or a therapeutically active nuclide, wherein if the compound comprises a diagnostically active nuclidepreferably the diagnostically active nuclide is a diagnostically active radionuclide, and more preferably the diagnostically active radionuclide is selected from the group consisting of A1-18F,43Sc,44Sc,51Mn,52Mn,64Cu,67Ga,68Ga,86Y,89Zr,94mTc, "mTc,11’in,149Tb,152Tb,155Tb,161Tb,177Lu,2O1T1,203Pb,18F,76Br,77Br,1231,124I, and125I, preferably selected from the group consisting of A1-18F,44Sc,MCu,67Ga,68Ga,86Y,89Zr, "mTc and1"in, and more preferably selected from the group consisting of ^Cu,68Ga and11’in; and wherein if the compound comprises a therapeutically active nuclide, preferably therapeutically active nuclide is a therapeutically active radionuclide, more preferably the therapeutically active radionuclide is selected from the group consisting of47Sc,67Cu,89Sr,90Y, ”’ln,153Sm,149Tb,I6’Tb,177LU, ’86Re,188Re,212Pb,213Bi,223Ra,225Ac,226Th,227Th,125I,131I, and2’’At, preferably selected from the group consisting of67Cu,90Y,149Tb,161Tb,177Lu,213Bi,225Ac,227Th, and more preferably selected from the group consisting of90Y,177Lu and225Ac.

28. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 27, wherein the compound interacts with a urokinase plasminogen activator surface receptor (uPAR), preferably with human uPAR 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 at least 85% to the amino acid sequence of SEQ ID NO: 1 ; preferably the compound binds or is capable of binding to urokinase plasminogen activator surface receptor (uPAR)29. The compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 28, for use in a method for the diagnosis of a disease or for use in a method for the treatment of a disease, preferably the disease is a disease targetable with a urokinase plasminogen activator surface receptor binding compound or a disease involving or being associated with urokinase plasminogen activator surface receptor (uPAR), preferably upregulated expression of urokinase plasminogen activator surface receptor (uPAR).

30. A composition, preferably a pharmaceutical composition, wherein the composition comprises a compound or pharmaceutically acceptable salt or hydrate or pharmaceutically acceptable solvate of any one of claims 1 to 28 and a pharmaceutically acceptable excipient.

31. A kit comprising a compound according to any one of claims 1 to 28, one or more optional excipient(s) and optionally one or more device(s), whereby the device(s) is / are selected from the group comprising a labeling device, a purification device, a handling device, a radioprotection device, an analytical device or an administration device.

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