Prostate-specific membrane antigen (PSMA) ligands and uses thereof

Abstract

The present disclosure provides a compound of formula (I) Regarding TIFF2025530229000542.tif78101.

Description

[Technical Field]

[0001] The present invention relates to chemical compounds; ligands for prostate-specific membrane antigen (PSMA); compositions comprising the compounds; compounds or compositions, respectively, for use in methods for the diagnosis of disease; compounds or compositions, respectively, for use in methods for the treatment of disease; compounds or compositions, respectively, for use in methods for the diagnosis and treatment of diseases also referred to as "thera(g)nosis" or "theragnostics"; compounds or compositions, respectively, for use in methods for the delivery of therapeutically or diagnostically active nuclides to PSMA-expressing tissue; methods for the diagnosis of disease using the compounds or compositions, respectively; methods for the treatment of disease using the compounds or compositions, respectively; methods for the diagnosis and treatment of diseases also referred to as "theragnosis" or "theragnostics" using the compounds or compositions, respectively; and methods for the delivery of therapeutically or diagnostically active nuclides to PSMA-expressing tissue using the compounds or compositions, respectively. [Background technology]

[0002] Prostate cancer (PCa) is one of the most frequently diagnosed cancers in men and is the second most common cause of cancer-related death in men, after lung cancer. The risk of developing prostate cancer increases dramatically with age, especially in men over the age of 50. With the aging population and increasing life expectancy that have characterized the last 30 years, the incidence of prostate cancer in the United States is approaching 1 in 6 men.

[0003] Early diagnosis and successful treatment of prostate cancer remain major clinical challenges. In addition to new techniques for accurately detecting prostate lesions, understanding the key molecular cascades during prostate carcinogenesis, metastasis, and drug resistance is crucial for the development of new therapeutics and interventions. A molecular hallmark of prostate cancer is the aberrant expression of the transmembrane glycoprotein prostate-specific membrane antigen (PSMA) in the cell membrane of almost all prostate neoplasms. The expression profile of PSMA in prostate cancer and its limited expression in normal organs suggests that it may play an important role in prostate cancer and is an attractive target for pharmacological intervention. The ability to target PSMA for specific delivery of anticancer compounds may be useful in the treatment of cancer as well as other diseases and conditions that express PSMA.

[0004] PSMA is a 750-amino acid transmembrane type II glycoprotein (SEQ ID NO: 1) with abundant and restricted expression on the surface of prostate cancer, particularly in androgen-independent advanced and metastatic disease. The latter is important because almost all prostate cancers become androgen-independent over time. PSMA meets the criteria for being a promising target for therapy: abundant and restricted (in the prostate) expression at all stages of disease, cell surface presentation but not shed into the circulation, and association with enzymatic or signaling activity. Metastatic spread and disease progression under androgen deprivation therapy signify the onset of metastatic castration-resistant prostate cancer (mCRPC), a fatal disease form that significantly worsens patients' quality of life. Although several treatments have been approved for mCRPC, their survival benefit is generally limited to less than six months.

[0005] PSMA is also present in the angiogenic endothelial cells of non-prostate tumors, including those of the kidney, lung, stomach, colon, and breast, where it may promote endothelial cell sprouting and invasion through modulation of lytic proteases capable of cleaving the extracellular matrix.

[0006] Selective targeting of cancer cells with radiopharmaceuticals for either imaging or therapeutic purposes is challenging. A variety of radionuclides are known to be useful for radioimaging or cancer radiotherapy. Summary of the Invention [Problem to be solved by the invention]

[0007] Despite significant advances in cancer diagnosis and treatment, improved therapies remain needed. There is a clinical need for improved therapies for the treatment of cancers such as prostate cancer, including therapies that may provide more effective and / or sustained responses. [Means for solving the problem]

[0008] One aspect of the present disclosure is a compound of formula (I)

[0009] [ka]

[0010] {In the formula, X is selected from the group consisting of a bond and -CH2-; Z 1 is selected from the group consisting of a chelator and NT; NT is selected from the group consisting of H, Ac, Hex, HPA, HO-succinyl, SaPr, Iva, HYDAc, Bio, nBuCAyl, AF488Ahx, and Hib; L 1 is the bond and -(Xaa1) k - selected from the group consisting of k is selected from the group consisting of 1, 2 and 3; Xaa1 is each and individually an amino acid residue, preferably an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI)

[0011] [ka]

[0012] is selected from the group consisting of g is an integer selected from the group consisting of 0 to 23; where: When k=1, Xaa1 is Z 1 is covalently bound to Xaa2, When k=2, the first of the two Xaa1 is Z 1 is covalently bound to the second of two Xaa1, the second of two Xaa1 is covalently bound to the first of two Xaa1, and is covalently bound to Xaa2, When k=3, the first of the three Xaa1 is Z 1 covalently bound to the second of three Xaa1, the second of three Xaa1 is covalently bound to the first of three Xaa1, covalently bound to the third of three Xaa1, the third of three Xaa1 is covalently bound to the second of three Xaa1, and covalently bound to Xaa2; where L 1 If is a bond, Z 1 is NT; Xaa2 is a group represented by formula (II) and formula (III):

[0013] [ka]

[0014] is selected from the group consisting of where R 2a is H, (C1-C6) alkyl and CH2R 2g selected from the group consisting of: R 2g is selected from the group consisting of OH and COH; R 2b is selected from the group consisting of H and (C1-C6) alkyl; Or alternatively, R2a and R 2b may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R 2c is selected from the group consisting of H and CH3; R 2d is selected from the group consisting of H, F and OH; R 2e is selected from the group consisting of H and F; R 2f is selected from the group consisting of H and CH3; However, L 1 is binding and NT is Hib, Xaa2 may be absent; Xaa3 is a group represented by formula (IV):

[0015] [ka]

[0016] is selected from where R 3a is selected from the group consisting of aryl, (C-C)heteroaryl, indol-3-yl, 6-chloro-1H-indol-3-yl, and -S-CH-phenyl; R 3a wherein said aryl or said heteroaryl ring is optionally substituted by 1, 2 or 3 substituents independently selected from the group consisting of halogen, (C1-C6)alkyl, CN, OH and —O(C1-C3)alkyl, wherein said (C1-C6)alkyl may be optionally substituted by one or more fluorines; R 3b is selected from the group consisting of H and CH3; h is selected from the group consisting of 1 and 2; Xaa5 is a group represented by the formula (Va) or (Vb):

[0017] [ka]

[0018] selected from the group consisting of Hgn, Lys, Nle, Tap, Aph and Gln; where R 5a is H, (C1-C6) alkyl, Ac, C(=NR 5d )NR 5e R 5f and Bio; R 5d is selected from the group consisting of H and CH3; R 5e and R 5f is independently selected from the group consisting of H and (C1-C6) alkyl; R 5b is selected from the group consisting of H and (C1-C6) alkyl; R 5c is selected from the group consisting of H and CH3; m is selected from the group consisting of 2, 3, 4 and 5; and R 5g , R 5h and R 5i is independently selected from the group consisting of (C1-C6) alkyl; Xaa6 is a group represented by formula (VI), formula (VII):

[0019] [ka]

[0020] selected from the group consisting of Nle and arg; where R 6a is H, C(=NR 6e )NR 6f R 6g , C(=O)R 6h and pyridyl; R 6e is selected from the group consisting of H and CH3; R 6f is H, (C1-C6) alkyl, Ac, NO2 and C(=O)NR 6i R 6j selected from the group consisting of: R 6i and R6j is independently selected from the group consisting of H and (C1-C2) alkyl; R 6g is selected from the group consisting of H and (C1-C6) alkyl; Or alternatively, R 6e and R 6f may together form a 5- or 6-membered heterocyclic ring; R 6h is (C1-C6) alkyl, NR 6k R 6m and N.R. 6n C(=NR 6p )NR 6q R 6r selected from the group consisting of: R 6k and R 6m is independently selected from the group consisting of H and (C1-C6) alkyl; R 6n and R 6p is independently selected from the group consisting of H and CH3; R 6q and R 6r is independently selected from the group consisting of H and (C1-C6) alkyl; R 6b is selected from the group consisting of H and (C1-C6) alkyl; R 6c is selected from the group consisting of H and CH3; n is selected from the group consisting of 1, 2, 3 and 4; R 6d is NR 6s C(=NR 6t )NR 6u R 6v , OH and NR 6w R 6x selected from the group consisting of: R 6s and R 6t is independently selected from the group consisting of H and CH3; R 6u , R 6v , R 6w and R 6xis independently selected from the group consisting of H and (C1-C6) alkyl; and q is selected from the group consisting of 2, 3 and 4; Xaa7 is an amino acid residue, and the amino acid residue is preferably a residue of formula (VIII), formula (IX), formula (X), formula (XI):

[0021] [ka]

[0022] selected from the group consisting of Dtc and Oic; where R 7a is H, (C1-C6) alkyl and (CH2) t R 7g selected from the group consisting of: R 7g are OH, COH and NR 7h R 7i selected from the group consisting of: R 7h and R 7i is independently selected from the group consisting of H and (C1-C6) alkyl; t is selected from the group consisting of 1, 2, 3 and 4; R 7b is selected from the group consisting of H and (C1-C6) alkyl; Or alternatively, R 7a and R 7b may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R 7c is selected from the group consisting of H and CH3; R 7d is selected from the group consisting of H, F and OH; R 7e is selected from the group consisting of H and F; R 7f is selected from the group consisting of H and CH3; u is selected from the group consisting of 2, 3 and 4; L 3 is bonded and -(Xab1) v- selected from the group consisting of v is selected from the group consisting of 1, 2 and 3; Xab1 are each and individually an amino acid residue, preferably an amino acid residue selected from the group consisting of an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI), When v=1, Xab1 is Z 3 and covalently bonded to a side chain amino functionality of formula (X) or of formula (XI), If v=2, the first of the two Xab1 is Z 3 is covalently bonded to the second of the two Xab1s, the second of the two Xab1s is covalently bonded to the first of the two Xab1s, and is covalently bonded to a side chain amino functional group of formula (X) or formula (XI), If v=3, the first of the three Xab1 is Z 3 covalently bonded to the second of three Xab1s, the second of three Xab1s covalently bonded to the first of three Xab1s, the third of three Xab1s covalently bonded to the second of three Xab1s, and the third of three Xab1s covalently bonded to the second of three Xab1s, covalently bonded to a side chain amino functional group of formula (X) or of formula (XI); Z 3 is selected from the group consisting of H and a chelator; Xaa8 is an α-amino acid residue, and the α-nitrogen atom of Xaa8 is unsubstituted or optionally substituted by CH3; Xaa10 is a group represented by formula (XII):

[0023] [ka]

[0024] and where: R 10a is selected from the group consisting of (C1-C6) alkyl; R10b is selected from the group consisting of H and (C1-C6) alkyl; Or alternatively, R 10a and R 10b may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R 10c is selected from the group consisting of H and CH3; L 2 teeth, bond and -Xaa11-(Xaa12) s - selected from the group consisting of: - whereby Xaa11 is covalently linked to Xaa10; Xaa11 is an amino acid residue, and the amino acid residue is preferably selected from the group consisting of an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI); s is selected from the group consisting of 0, 1, 2, 3, 4 and 5; and Xaa12 are each and individually an amino acid residue, which amino acid residue is preferably selected from the group comprising an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI), When s=0, Xaa11 is Z 2 is covalently bonded to When s=1, Xaa12 is covalently linked to Xaa11, and Z 2 is covalently bonded to When s=2, the first of the two Xaa12 is covalently bonded to Xaa11, the second of the two Xaa12 is covalently bonded to Xaa11, the second of the two Xaa12 is covalently bonded to the first of the two Xaa12, and Z 2 is covalently bonded to When s=3, the first of the three Xaa12 is covalently bonded to Xaa11 and the second of the three Xaa12 is covalently bonded to Xaa11, the second of the three Xaa12 is covalently bonded to the first of the three Xaa12 and the third of the three Xaa12, the third of the three Xaa12 is covalently bonded to the second of the three Xaa12, and Z 2 is covalently bonded to When s=4, the first of four Xaa12 is covalently bonded to Xaa11, the second of four Xaa12 is covalently bonded to Xaa11, the second of four Xaa12 is covalently bonded to the first of four Xaa12, the third of four Xaa12 is covalently bonded to the second of four Xaa12, the fourth of four Xaa12 is covalently bonded to the third of four Xaa12, and the fourth of four Xaa12 is covalently bonded to the third of four Xaa12; Z 2 is covalently bonded to When s=5, the first of the five Xaa12 is covalently bonded to Xaa11, the second of the five Xaa12 is covalently bonded to the first of the five Xaa12, the third of the five Xaa12 is covalently bonded to the second of the five Xaa12, the fourth of the five Xaa12 is covalently bonded to the third of the five Xaa12, the fourth of the five Xaa12 is covalently bonded to the third of the five Xaa12, the fifth of the five Xaa12 is covalently bonded to the fourth of the five Xaa12, and Z 2 is covalently bound to; Z 2 comprises CT, an XDa-chelator and an α-amino acid residue of formula (CT-I):

[0025] [ka]

[0026] is selected from the group consisting of CT is represented by the formula (CT-II) or (CT-III):

[0027] [ka]

[0028] AF488N3K-NH2, OH and Throl-OH; where: R CT1 is selected from the group consisting of H and CH3; R CT2 is selected from the group consisting of H and (C1-C6) alkyl; R CT3 and R CT4 are each and individually selected from the group consisting of H and CH3; R CT5 is selected from the group consisting of H and (C1-C6) alkyl; x is selected from the group consisting of 2 to 10; XDa is a diamine, said diamine preferably being selected from the group consisting of en and Ape; w is selected from the group consisting of 1, 2, 3, 4, 5 and 6; L 4 binds and -(Xac1) y - selected from the group consisting of where: y is selected from the group consisting of 0, 1, 2 and 3; Xac1 is each and individually an amino acid residue, preferably the amino acid residue is selected from the group comprising an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI), When y=0, the side chain amino functional group of the α-amino acid residue of formula (CT-I) is Z 4 is covalently bonded to When y=1, Xac1 is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), and Z 4 is covalently bonded to When y=2, the first of the two Xac1s is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), the second of the two Xac1s is covalently bonded to the first of the two Xac1s, and Z 4 is covalently bonded to When y=3, the first of the three Xac1s is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), the second of the three Xac1s is covalently bonded to the first of the three Xac1s, the third of the three Xac1s is covalently bonded to the third of the three Xac1s, the third of the three Xac1s is covalently bonded to the second of the three Xac1s, and Z 4 is covalently bonded to When y=4, the first of four Xac1s is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), the second of four Xac1s is covalently bonded to the second of four Xac1s, the second of four Xac1s is covalently bonded to the first of four Xac1s, the third of four Xac1s is covalently bonded to the second of four Xac1s, the fourth of four Xac1s is covalently bonded to the third of four Xac1s, and Z 4 is covalently bound to; Z 4 is selected from the group consisting of H and a chelator; However, L 2 is a bond, CT is a group represented by formula (CT-II), wherein R CT1 is selected from the group consisting of H and CH3, and R CT2 is (C4-C6) alkyl, Xaa10 may be absent. which may contain a therapeutically active nuclide or a diagnostically active nuclide.

[0029] The following detailed description, given by way of example and not intended to limit the invention, is further illustrated by reference to the following drawings from which additional features, embodiments and advantages can be seen. [Brief explanation of the drawings]

[0030] [Figure 1] Figure 1(a) is a schematic of the PSMA activity inhibition assay. Figure 1(b) shows the enzyme inhibition curves for PSM-0374, PSM-0516, PSM-0194, PSM-0416, PSM-0424, and 2-PMPA in the human PSMA activity inhibition assay. [Figure 2] FIG. 2 shows a representative radiochromatogram for PSM-0433 labeled with 111In. [Figure 3(a)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(a) shows the %ID / g uptake of In-PSM-0234 at 1, 4, and 24 hours post-injection. [Figure 3(b)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(b) shows the %ID / g uptake of In-PSM-0425 at 1, 4, and 24 hours post-injection. [Figure 3(c)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(c) shows the %ID / g uptake of In-PSM-0218 at 1, 4, and 24 hours post-injection. [Figure 3(d)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(d) shows the %ID / g uptake of In-PSM-0365 at 1, 4, and 24 hours post-injection. [Figure 3(e)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(e) shows the %ID / g uptake of In-PSM-0580 at 1, 4, and 24 hours post-injection. [Figure 3(f)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(f) shows the %ID / g uptake of In-PSM-0492 at 1, 4, and 24 hours post-injection. [Figure 3(g)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(g) shows the %ID / g uptake of In-PSM-0285 at 1, 4, and 24 hours post-injection. [Figure 3(h)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(h) shows the %ID / g uptake of In-PSM-0237 at 1, 4, and 24 hours post-injection. [Figure 3(i)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(i) shows the %ID / g uptake of In-PSM-0428 at 1, 4, and 24 hours post-injection. [Figure 3(j)]Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(j) shows the %ID / g uptake of In-PSM-0283 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(k)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(k) shows the %ID / g uptake of In-PSM-0573 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(l)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(l) shows the %ID / g uptake of In-PSM-0190 at 4 and 24 hours post-injection. [Figure 3(m)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(m) shows the %ID / g uptake of In-PSM-0239 at 1, 4, and 24 hours post-injection. [Figure 3(n)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(n) shows the %ID / g uptake of In-PSM-0371 at 1, 4, and 24 hours post-injection. [Figure 3(o)]Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(o) shows the %ID / g uptake of In-PSM-0339 at 1, 4, and 24 hours post-injection. [Figure 3(p)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(p) shows the %ID / g uptake of In-PSM-0301 at 1, 4, and 24 hours post-injection. [Figure 3(q)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(q) shows the %ID / g uptake of In-PSM-0243 at 1, 4, and 24 hours post-injection. [Figure 3(r)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(r) shows the %ID / g uptake of In-PSM-0199 at 1, 4, 24, and 48 hours post-injection. [Figure 3(s)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(s) shows the %ID / g uptake of In-PSM-0361 at 1, 4, 24, and 48 hours post-injection. [Figure 3(t)]Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(t) shows the %ID / g uptake of In-PSM-0273 at 1, 4, 24, and 48 hours post-injection. [Figure 3(u)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(u) shows the %ID / g uptake of In-PSM-0433 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(v)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(v) shows the %ID / g uptake of In-PSM-0534 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(w)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(w) shows the %ID / g uptake of In-PSM-0269 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(x)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(x) shows the %ID / g uptake of In-PSM-0267 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(y)]Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(y) shows the %ID / g uptake of In-PSM-0481 at 1, 4, 24, and 48 hours post-injection. [Figure 3(z)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(z) shows the %ID / g uptake of In-PSM-0416 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(aa)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(aa) shows the %ID / g uptake of In-PSM-0194 at 1, 4, 24, and 48 hours post-injection. [Figure 3(bb)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(bb) shows the %ID / g uptake of In-PSM-0377 at 1, 4, 24, and 48 hours post-injection. [Figure 3(cc)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(cc) shows the %ID / g uptake of In-PSM-0516 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(dd)]Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(dd) shows the %ID / g uptake of In-PSM-0467 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(ee)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(ee) shows the %ID / g uptake of In-PSM-0384 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(ff)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(ff) shows the %ID / g uptake of In-PSM-0449 at 1, 4, 24, and 48 hours post-injection. [Figure 3(gg)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(gg) shows the %ID / g uptake of In-PSM-0241 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 3(hh)] Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(hh) shows the %ID / g uptake of In-PSM-0579 at 1, 4, 24, and 48 hours post-injection. [Figure 3(ii)]Figures 3(a)-3(ii) show the %ID / g uptake (biodistribution) of In-labeled compounds in the PC3-PIP tumor model in mice (see Example 35). Figure 3(ii) shows the %ID / g uptake of In-PSM-0531 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 4(a)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(a) shows the %ID / g uptake of In-PSM-0285 at 1, 4, and 24 hours post-injection. [Figure 4(b)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(b) shows the %ID / g uptake of In-PSM-0428 at 1, 4, and 24 hours post-injection. [Figure 4(c)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(c) shows the %ID / g uptake of In-PSM-0492 at 1, 4, 24, and 72 hours post-injection. [Figure 4(d)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(d) shows the %ID / g uptake of In-PSM-0365 at 1, 4, and 24 hours post-injection. [Figure 4(e)]Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(e) shows the %ID / g uptake of In-PSM-0218 at 1, 4, and 24 hours post-injection. [Figure 4(f)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(f) shows the %ID / g uptake of In-PSM-0243 at 1, 4, and 24 hours post-injection. [Figure 4(g)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(g) shows the %ID / g uptake of In-PSM-0339 at 1, 4, and 24 hours post-injection. [Figure 4(h)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(h) shows the %ID / g uptake of In-PSM-0301 at 1, 4, and 24 hours post-injection. [Figure 4(i)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(i) shows the %ID / g uptake of In-PSM-0283 at 1, 4, 24, and 72 hours post-injection. [Figure 4(j)]Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(j) shows the %ID / g uptake of In-PSM-0433 at 1, 4, 24, and 72 hours post-injection. [Figure 4(k)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(k) shows the %ID / g uptake of In-PSM-0194 at 1, 4, 24, and 72 hours post-injection. [Figure 4(l)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(l) shows the %ID / g uptake of In-PSM-0345 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 4(m)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(m) shows the %ID / g uptake of In-PSM-0380 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 4(n)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(n) shows the %ID / g uptake of In-PSM-0483 at 1, 4, 24, and 48 hours post-injection. [Figure 4(o)]Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(o) shows the %ID / g uptake of In-PSM-0420 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 4(p)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(p) shows the %ID / g uptake of In-PSM-0246 at 1, 4, 24, and 48 hours post-injection. [Figure 4(q)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(q) shows the %ID / g uptake of In-PSM-0244 at 1, 4, 24, 48, and 72 hours post-injection. [Figure 4(r)] Figures 4(a)-4(r) show the %ID / g uptake (biodistribution) of In-labeled compounds in the C4-2 tumor model in mice (see Example 35). Figure 4(r) shows the %ID / g uptake of In-PSM-0203 at 1, 4, 24, and 48 hours post-injection. [Figure 5] FIG. 5 shows the observed in vivo biodistribution of 177Lu-PSM-0194 over time (at 4, 24, and 76 hours pi) in the ST1273 model (%ID / g, decay-corrected mean values ​​are shown for each organ (blood, kidney (left), kidney (right), liver, tail, and tumor) ROI). [Figure 6] FIG. 6 shows individual ST1273 tumor volumes over time following treatment with 177Lu-PSM-0194 (dotted line on study day 0 indicates the day of treatment). [Figure 7-1] FIG. 7 shows the amino acid sequence of PSMA (SEQ ID NO: 1). [Figure 7-2] FIG. 7 shows the amino acid sequence of PSMA (SEQ ID NO: 1). [Figure 7-3] FIG. 7 shows the amino acid sequence of PSMA (SEQ ID NO: 1). [Figure 7-4] FIG. 7 shows the amino acid sequence of PSMA (SEQ ID NO: 1). DETAILED DESCRIPTION OF THE INVENTION

[0031] The present disclosure relates to novel compounds suitable for use as diagnostic and / or pharmaceutical agents for the diagnosis and / or treatment of prostate cancer and other diseases and conditions mediated by PSMA. The present disclosure provides novel compounds capable of interacting with PSMA that can deliver therapeutically or diagnostically active nuclides that can provide for the detection, treatment, and / or management of various diseases associated with one or more PSMA-expressing tumors or cells, including prostate cancer.

[0032] The present disclosure is based on the surprising discovery that the compounds of the present disclosure provide highly specific and potent binding to PSMA. These compounds are capable of interacting with PSMA to achieve improved binding affinity and other properties described herein. The compounds of the present invention are surprisingly useful as imaging agents and in delivering radionuclides to tumors.

[0033] The compounds of the present disclosure have one or more advantageous properties, including but not limited to, rapid tumor uptake, prolonged tumor retention, rapid compound clearance from non-tumor tissues, improved efficacy, and / or favorable biodistribution properties, and are accompanied by improved toxicity and side effect profiles.In one embodiment, and as preferably used herein, a compound exhibits rapid tumor uptake if, within 1 hour after administration of the compound to a tumor-bearing subject, at least 0.1% of the amount of compound administered to the subject is taken up by the tumor; such tumor uptake is preferably determined by nuclear imaging.

[0034] For effective clinical use, PSMA ligand selection should be based on, for example, rapid uptake and sustained localization at the target site, as well as negligible retention in non-target tissues. Low levels of endogenous PSMA expression have been found in non-target tissues, including normal prostate, proximal tubules of the kidney, lacrimal and salivary glands, spleen, liver, mesentery, testes, ovaries, and brain (Chakravarty et al. 2018 Am J Nucl Med Mol Imaging 8(4):247-267).

[0035] For diagnosis and / or treatment, the compounds of the present disclosure can be complexed with radionuclides that are α-emitters, β-emitters, γ-emitters, or Auger-emitters. α-emitter radionuclides have the ability to destroy tumors while causing very limited damage to surrounding healthy tissue due to the short penetration depth of α particles. Due to their high linear energy transfer (LET), they have increased relative biological effectiveness (RBE) compared to other radionuclide therapies. Furthermore, when α-emitting radionuclides are targeted to specific tumor cells in the body, they can be highly effective in destroying metastases that are difficult to treat with currently used techniques (de Kruijff et al., 2015 Pharmaceuticals, 8, 321-336). However, toxicity is a major limitation of the use of α-emitters.

[0036] Actinium-225( 225 For small molecule PSMA-targeting agents used for the delivery of α-emitting radionuclides such as Ac), irradiation of the salivary glands has been reported to be a major dose-limiting side effect, particularly due to the irreversible nature of xerostomia.

[0037] The compounds of the present invention surprisingly exhibit reduced binding to human salivary glands compared to known PSMA inhibitors. In the clinic, it was conjugated with a PSMA inhibitor 225 Treatment with α-emitting radionuclides, such as Ac, has been shown to result in irreversible grade 3 / 4 xerostomia, causing significant impairment of patient quality of life and thus representing a dose-limiting side effect for the therapeutic use of α-emitting small-molecule PSMA inhibitors (Tonnesmann et al., 2019, Pharmaceuticals 12, 18). However, PSMA-targeting antibodies have not shown significant uptake in salivary glands. While salivary glands are known to have low levels of PSMA, the uptake of PSMA inhibitors detected in clinical studies by salivary glands did not correlate with the relatively low physiological PSMA expression in that tissue, implying that binding to salivary glands is largely nonspecific (Tonnesmann et al., 2019).

[0038] Because the PSMA ligands disclosed herein can provide effective treatment for diseases associated with one or more PSMA-expressing tumors or cells, including prostate cancer, with reduced uptake by the salivary glands, they are surprisingly suitable as carriers for therapeutic α-emitters, allowing such compounds to be administered at higher doses, potentially resulting in improved response rates and better tumor control.

[0039] Compounds of the present disclosure have favorable uptake ratios of tumor to non-tumor tissue (eg, salivary gland, kidney, or other non-tumor tissue). In certain embodiments, the compound's preferred uptake in non-tumor tissues over tumor tissues allows for the delivery of radionuclides at doses that can reduce tumor growth or partially or completely destroy tumors while minimizing side effects.In certain embodiments, due to the favorable uptake ratio of the compound of the present disclosure in tumor targets relative to non-tumor targets, the compound of the present disclosure can surprisingly overcome the unnecessary side effect of severe xerostomia associated with known PSMA inhibitors.In certain embodiments, the compound of the present disclosure can advantageously provide effective treatment for diseases associated with one or more PSMA-expressing tumors or cells, including prostate cancer, and can allow for the administration of higher doses, potentially resulting in improved response rates and better tumor management.In certain embodiments, the compound of the present disclosure can advantageously maximize therapeutic efficacy while minimizing negative side effects.

[0040] In some embodiments, compounds of the present disclosure can be advantageously used in methods for identifying subjects, or for selecting subjects from a group of subjects, or for stratifying a group of subjects, where the subjects are likely or unlikely to respond to disease treatment, the method comprising performing a diagnostic method using a compound according to the present disclosure. In certain embodiments, such methods can advantageously optimize drug treatments, including minimizing risks and maximizing effectiveness, for example, by helping medical professionals identify subjects who would most benefit from a given treatment and avoid unnecessary treatment.

[0041] The present disclosure is further described herein, including in the following embodiments. Embodiment 1. A compound of formula (I)

[0042] [ka]

[0043] {In the formula, X is selected from the group consisting of a bond and -CH2-; Z 1 is selected from the group consisting of a chelator and NT; NT is selected from the group consisting of H, Ac, Hex, HPA, HO-succinyl, SaPr, Iva, HYDAc, Bio, nBuCAyl, AF488Ahx, and Hib; L 1 is the bond and -(Xaa1) k - selected from the group consisting of k is selected from the group consisting of 1, 2 and 3; Xaa1 is each and individually an amino acid residue, preferably an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI)

[0044] [ka]

[0045] is selected from the group consisting of g is an integer selected from the group consisting of 0 to 23; where: When k=1, Xaa1 is Z 1 is covalently bound to Xaa2, When k=2, the first of the two Xaa1 is Z 1 is covalently bound to the second of two Xaa1, the second of two Xaa1 is covalently bound to the first of two Xaa1, and is covalently bound to Xaa2, When k=3, the first of the three Xaa1 is Z 1 covalently bound to the second of three Xaa1, the second of three Xaa1 is covalently bound to the first of three Xaa1, covalently bound to the third of three Xaa1, the third of three Xaa1 is covalently bound to the second of three Xaa1, and covalently bound to Xaa2; where L1 If is a bond, Z 1 is NT; Xaa2 is a group represented by formula (II) and formula (III):

[0046] [ka]

[0047] is selected from the group consisting of where R 2a is H, (C1-C6) alkyl and CH2R 2g selected from the group consisting of: R 2g is selected from the group consisting of OH and COH; R 2b is selected from the group consisting of H and (C1-C6) alkyl; Or alternatively, R 2a and R 2b may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R 2c is selected from the group consisting of H and CH3; R 2d is selected from the group consisting of H, F and OH; R 2e is selected from the group consisting of H and F; R 2f is selected from the group consisting of H and CH3; However, L 1 is binding and NT is Hib, Xaa2 may be absent; Xaa3 is a group represented by formula (IV):

[0048] [ka]

[0049] is selected from where R 3ais selected from the group consisting of aryl, (C-C)heteroaryl, indol-3-yl, 6-chloro-1H-indol-3-yl, and -S-CH-phenyl; R 3a wherein the aryl or heteroaryl ring is optionally substituted by 1, 2 or 3 substituents independently selected from the group consisting of halogen, (C1-C6)alkyl, CN, OH and —O(C1-C3)alkyl, wherein the (C1-C6)alkyl is optionally substituted by one or more fluorines; R 3b is selected from the group consisting of H and CH3; h is selected from the group consisting of 1 and 2; Xaa5 is a group represented by the formula (Va) or (Vb):

[0050] [ka]

[0051] selected from the group consisting of Hgn, Lys, Nle, Tap, Aph and Gln; where R 5a is H, (C1-C6) alkyl, Ac, C(=NR 5d )NR 5e R 5f and Bio; R 5d is selected from the group consisting of H and CH3; R 5e and R 5f is independently selected from the group consisting of H and (C1-C6) alkyl; R 5b is selected from the group consisting of H and (C1-C6) alkyl; R 5c is selected from the group consisting of H and CH3; m is selected from the group consisting of 2, 3, 4 and 5; and R 5g , R 5h and R 5i is independently selected from the group consisting of (C1-C6) alkyl; Xaa6 is a group represented by formula (VI), formula (VII):

[0052] [ka]

[0053] selected from the group consisting of Nle and arg; where R 6a is H, C(=NR 6e )NR 6f R 6g , C(=O)R 6h and pyridyl; R 6e is selected from the group consisting of H and CH3; R 6f is H, (C1-C6) alkyl, Ac, NO2 and C(=O)NR 6i R 6j selected from the group consisting of: R 6i and R 6j is independently selected from the group consisting of H and (C1-C2) alkyl; R 6g is selected from the group consisting of H and (C1-C6) alkyl; Or alternatively, R 6e and R 6f may together form a 5- or 6-membered heterocyclic ring; R 6h is (C1-C6) alkyl, NR 6k R 6m and N.R. 6n C(=NR 6p )NR 6q R 6r selected from the group consisting of: R 6k and R 6m is independently selected from the group consisting of H and (C1-C6) alkyl; R 6n and R 6p is independently selected from the group consisting of H and CH3; R 6q and R 6ris independently selected from the group consisting of H and (C1-C6) alkyl; R 6b is selected from the group consisting of H and (C1-C6) alkyl; R 6c is selected from the group consisting of H and CH3; n is selected from the group consisting of 1, 2, 3 and 4; R 6d is NR 6s C(=NR 6t )NR 6u R 6v , OH and NR 6w R 6x selected from the group consisting of: R 6s and R 6t is independently selected from the group consisting of H and CH3; R 6u , R 6v , R 6w and R 6x is independently selected from the group consisting of H and (C1-C6) alkyl; q is selected from the group consisting of 2, 3 and 4; Xaa7 is an amino acid residue, and the amino acid residue is preferably a residue of formula (VIII), formula (IX), formula (X), formula (XI):

[0054] [ka]

[0055] selected from the group consisting of Dtc and Oic; where R 7a is H, (C1-C6) alkyl and (CH2) t R 7g selected from the group consisting of: R 7g are OH, COH and NR 7h R 7i selected from the group consisting of: R 7h and R 7i is independently selected from the group consisting of H and (C1-C6) alkyl; t is selected from the group consisting of 1, 2, 3 and 4; R 7b is selected from the group consisting of H and (C1-C6) alkyl; Or alternatively, R 7a and R 7b may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R 7c is selected from the group consisting of H and CH3; R 7d is selected from the group consisting of H, F and OH; R 7e is selected from the group consisting of H and F; R 7f is selected from the group consisting of H and CH3; u is selected from the group consisting of 2, 3 and 4; L 3 is bonded and -(Xab1) v - selected from the group consisting of v is selected from the group consisting of 1, 2 and 3; Xab1 are each and individually an amino acid residue, preferably an amino acid residue selected from the group consisting of an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI), When v=1, Xab1 is Z 3 and covalently bonded to a side chain amino functionality of formula (X) or of formula (XI), If v=2, the first of the two Xab1 is Z 3 is covalently bonded to the second of the two Xab1s, the second of the two Xab1s is covalently bonded to the first of the two Xab1s, and is covalently bonded to a side chain amino functional group of formula (X) or formula (XI), If v=3, the first of the three Xab1 is Z 3covalently bonded to the second of three Xab1s, the second of three Xab1s covalently bonded to the first of three Xab1s, the third of three Xab1s covalently bonded to the second of three Xab1s, and the third of three Xab1s covalently bonded to the second of three Xab1s, covalently bonded to a side chain amino functional group of formula (X) or of formula (XI); Z 3 is selected from the group consisting of H and a chelator; Xaa8 is an α-amino acid residue, and the α-nitrogen atom of Xaa8 is unsubstituted or may be substituted by CH3; Xaa10 is a group represented by formula (XII):

[0056] [ka]

[0057] and where: R 10a is selected from the group consisting of (C1-C6) alkyl; R 10b is selected from the group consisting of H and (C1-C6) alkyl; Or alternatively, R 10a and R 10b may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R 10c is selected from the group consisting of H and CH3; L 2 teeth, bond and -Xaa11-(Xaa12) s - selected from the group consisting of: - whereby Xaa11 is covalently linked to Xaa10; Xaa11 is an amino acid residue, and the amino acid residue is preferably selected from the group consisting of an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI); s is selected from the group consisting of 0, 1, 2, 3, 4 and 5; Xaa12 are each and individually an amino acid residue, which amino acid residue is preferably selected from the group comprising an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI), When s=0, Xaa11 is Z 2 is covalently bonded to When s=1, Xaa12 is covalently linked to Xaa11, and Z 2 is covalently bonded to When s=2, the first of the two Xaa12 is covalently bonded to Xaa11, the second of the two Xaa12 is covalently bonded to Xaa11, the second of the two Xaa12 is covalently bonded to the first of the two Xaa12, and Z 2 is covalently bonded to When s=3, the first of the three Xaa12 is covalently bonded to Xaa11 and the second of the three Xaa12 is covalently bonded to Xaa11, the second of the three Xaa12 is covalently bonded to the first of the three Xaa12 and the third of the three Xaa12, the third of the three Xaa12 is covalently bonded to the second of the three Xaa12, and Z 2 is covalently bonded to When s=4, the first of four Xaa12 is covalently bonded to Xaa11, the second of four Xaa12 is covalently bonded to Xaa11, the second of four Xaa12 is covalently bonded to the first of four Xaa12, the third of four Xaa12 is covalently bonded to the second of four Xaa12, the fourth of four Xaa12 is covalently bonded to the third of four Xaa12, and the fourth of four Xaa12 is covalently bonded to the third of four Xaa12; Z 2 is covalently bonded to When s=5, the first of the five Xaa12 is covalently bonded to Xaa11, the second of the five Xaa12 is covalently bonded to the first of the five Xaa12, the third of the five Xaa12 is covalently bonded to the second of the five Xaa12, the fourth of the five Xaa12 is covalently bonded to the third of the five Xaa12, the fourth of the five Xaa12 is covalently bonded to the third of the five Xaa12, the fifth of the five Xaa12 is covalently bonded to the fourth of the five Xaa12, and Z 2 is covalently bound to; Z 2 comprises CT, an XDa-chelator and an α-amino acid residue of formula (CT-I):

[0058] [ka]

[0059] is selected from the group consisting of CT is represented by the formula (CT-II) or (CT-III):

[0060] [ka]

[0061] AF488N3K-NH2, OH and Throl-OH; where: R CT1 is selected from the group consisting of H and CH3; R CT2 is selected from the group consisting of H and (C1-C6) alkyl; R CT3 and R CT4 are each and individually selected from the group consisting of H and CH3; R CT5 is selected from the group consisting of H and (C1-C6) alkyl; x is selected from the group consisting of 2 to 10; XDa is a diamine, said diamine preferably being selected from the group consisting of en and Ape; w is selected from the group consisting of 1, 2, 3, 4, 5 and 6; L 4 binds and -(Xac1) y - selected from the group consisting of where: y is selected from the group consisting of 0, 1, 2 and 3; Xac1 is each and individually an amino acid residue, preferably the amino acid residue is selected from the group comprising an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI), When y=0, the side chain amino functional group of the α-amino acid residue of formula (CT-I) is Z 4 is covalently bonded to When y=1, Xac1 is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), and Z 4 is covalently bonded to When y=2, the first of the two Xac1s is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), the second of the two Xac1s is covalently bonded to the first of the two Xac1s, and Z 4 is covalently bonded to When y=3, the first of the three Xac1s is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), the second of the three Xac1s is covalently bonded to the first of the three Xac1s, the third of the three Xac1s is covalently bonded to the third of the three Xac1s, the third of the three Xac1s is covalently bonded to the second of the three Xac1s, and Z 4 is covalently bonded to When y=4, the first of four Xac1s is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), the second of four Xac1s is covalently bonded to the second of four Xac1s, the second of four Xac1s is covalently bonded to the first of four Xac1s, the third of four Xac1s is covalently bonded to the second of four Xac1s, the fourth of four Xac1s is covalently bonded to the third of four Xac1s, and Z 4 is covalently bound to; Z 4 is selected from the group consisting of H and a chelator; However, L 2 is a bond, CT is a group represented by formula (CT-II), wherein R CT1 is selected from the group consisting of H and CH3, and R CT2 is (C4-C6) alkyl, Xaa10 may be absent. or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, which may contain a therapeutically active nuclide or a diagnostically active nuclide. Embodiment 2. A compound of formula (I)

[0062] [ka]

[0063] {In the formula, X is selected from the group consisting of a bond and -CH2-; Z 1 is selected from the group consisting of a chelator and NT; NT is selected from the group consisting of H, Ac, Hex, HPA, HO-succinyl, SaPr, Iva, HYDAc, Bio, nBuCAyl, AF488Ahx, and Hib; L 1 is the bond and -(Xaa1) k - selected from the group consisting of; k is selected from the group consisting of 1, 2 and 3; where: When k=1, Xaa1 is Z 1 is covalently bound to Xaa2, When k=2, the first of the two Xaa1 is Z 1 is covalently bound to the second of two Xaa1, the second of two Xaa1 is covalently bound to the first of two Xaa1, and is covalently bound to Xaa2, when k=3, the first of three Xaa1 is covalently bonded to Z1 and covalently bonded to the second of three Xaa1, the second of three Xaa1 is covalently bonded to the first of three Xaa1 and covalently bonded to the third of three Xaa1, and the third of three Xaa1 is covalently bonded to the second of three Xaa1 and covalently bonded to Xaa2; where L 1 If is a bond, Z 1 is NT; Xaa1 is each and individually selected from the group consisting of Thr, Ala, Ser, Pamp, Leu, Ile, Nmt, Pamb, Ahx, APAc, PPAc, Bal, Cmp, Pab, O2Oc, Met, and Ttds; Xaa2 is selected from the group consisting of Aib, Ala, Amd, Ams, amd, ams, Deg, Nmg, Pam, and Pro; 1 is binding and NT is Hib, Xaa2 may be absent; Xaa3 is selected from the group consisting of Phe, Nmf, 1Ni, 2Ni, 6Clw, Cys(Bzl), Hfe, Trp, Mpa, Opa, and Ppa; Phe, Nmf, and Hfe may be independently substituted by one or two substituents selected from the group consisting of halogen, CH3, CN, CF3, and OH; Xaa5 is a group represented by the formula (Va) or (Vb):

[0064] [ka]

[0065] selected from the group consisting of Hgn, Lys, Nle, Tap, Aph and Gln; where R 5a is H, (C1-C6) alkyl, Ac, C(=NR 5d )NR 5e R 5f and Bio; R 5d is selected from the group consisting of H and CH3; R 5e and R 5f is independently selected from the group consisting of H and (C1-C6) alkyl; R 5b is selected from the group consisting of H and (C1-C6) alkyl; R 5c is selected from the group consisting of H and CH3; m is selected from the group consisting of 2, 3, 4 and 5; R 5g , R 5h and R 5i is independently selected from the group consisting of (C1-C6) alkyl; Xaa6 is a group represented by formula (VI), formula (VII):

[0066] [ka]

[0067] selected from the group consisting of Nle and arg; where R 6a is H, C(=NR 6e )NR 6f R 6g , C(=O)R 6h and pyridyl; R 6e is selected from the group consisting of H and CH3; R 6f is H, (C1-C6) alkyl, Ac, NO2 and C(=O)NR 6i R 6j selected from the group consisting of: R 6i and R6j is independently selected from the group consisting of H and (C1-C2) alkyl; R 6g is selected from the group consisting of H and (C1-C6) alkyl; Or alternatively, R 6e and R 6f may together form a 5- or 6-membered heterocyclic ring; R 6h is (C1-C6) alkyl, NR 6k R 6m and N.R. 6n C(=NR 6p )NR 6q R 6r selected from the group consisting of: R 6k and R 6m is independently selected from the group consisting of H and (C1-C6) alkyl; R 6n and R 6p is independently selected from the group consisting of H and CH3; R 6q and R 6r is independently selected from the group consisting of H and (C1-C6) alkyl; R 6b is selected from the group consisting of H and (C1-C6) alkyl; R 6c is selected from the group consisting of H and CH3; n is selected from the group consisting of 1, 2, 3 and 4; R 6d is NR 6s C(=NR 6t )NR 6u R 6v , OH and NR 6w R 6x selected from the group consisting of: R 6s and R 6t is independently selected from the group consisting of H and CH3; R 6u , R 6v , R 6w and R 6xis independently selected from the group consisting of H and (C1-C6) alkyl; q is selected from the group consisting of 2, 3 and 4; Xaa7 is a group represented by formula (VIII), formula (IX), formula (X), or formula (XI):

[0068] [ka]

[0069] selected from the group consisting of Dtc and Oic; where R 7a is H, (C1-C6) alkyl and (CH2) t R 7g selected from the group consisting of: R 7g are OH, COH and NR 7h R 7i selected from the group consisting of: R 7h and R 7i is independently selected from the group consisting of H and (C1-C6) alkyl; t is selected from the group consisting of 1, 2, 3 and 4; R 7b is selected from the group consisting of H and (C1-C6) alkyl; Or alternatively, R 7a and R 7b may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R 7c is selected from the group consisting of H and CH3; R 7d is selected from the group consisting of H, F and OH; R 7e is selected from the group consisting of H and F; R 7f is selected from the group consisting of H and CH3; u is selected from the group consisting of 2, 3 and 4; L 3 is bonded and -(Xab1) v - selected from the group consisting of; v is selected from the group consisting of 1, 2 and 3; Xab1 is each and individually selected from the group consisting of Ttds, Pamb, APAc, O2Oc, Ahx, Pab, and Cmp; Here, when v=1, Xab1 is Z 3 and covalently bonded to a side chain amino functionality of formula (X) or of formula (XI), If v=2, the first of the two Xab1 is Z 3 is covalently bonded to the second of the two Xab1s, the second of the two Xab1s is covalently bonded to the first of the two Xab1s, and is covalently bonded to a side chain amino functional group of formula (X) or formula (XI), If v=3, the first of the three Xab1 is Z 3 covalently bonded to the second of three Xab1s, the second of three Xab1s covalently bonded to the first of three Xab1s, the third of three Xab1s covalently bonded to the second of three Xab1s, and the third of three Xab1s covalently bonded to the second of three Xab1s, covalently bonded to a side chain amino functional group of formula (X) or of formula (XI); Z 3 is selected from the group consisting of H and a chelator; Xaa8 is an α-amino acid residue, and the α-nitrogen atom of Xaa8 is unsubstituted or may be substituted by CH3; Xaa10 is a group represented by the formula (XII)

[0070] [ka]

[0071] and where: R 10a is selected from the group consisting of (C1-C6) alkyl; R 10b is selected from the group consisting of H and CH3; R 10c is selected from the group consisting of H and CH3; L 2 teeth, bond and -Xaa11-(Xaa12) s - selected from the group consisting of: - whereby Xaa11 is covalently linked to Xaa10; Xaa11 is selected from the group consisting of Thr, Ala, Bal, Gab, Gln, Glu, Gly, Leu, Nmt, Phe, Pro, and Trp; s is selected from the group consisting of 0, 1, 2, 3, 4 and 5; Xaa12 is each and individually selected from the group consisting of Asp, asp, Ala, Gab, Ttds, Pamb, Cmp, O2Oc, APAc, Gly, Ser, Lys(Bio), and Pab; Here, when s=0, Xaa11 is Z 2 is covalently bonded to When s=1, Xaa12 is covalently linked to Xaa11, and Z 2 is covalently bonded to When s=2, the first of the two Xaa12 is covalently bonded to Xaa11, the second of the two Xaa12 is covalently bonded to Xaa11, the second of the two Xaa12 is covalently bonded to the first of the two Xaa12, and Z 2 is covalently bonded to When s=3, the first of the three Xaa12 is covalently bonded to Xaa11 and the second of the three Xaa12 is covalently bonded to Xaa11, the second of the three Xaa12 is covalently bonded to the first of the three Xaa12 and the third of the three Xaa12, the third of the three Xaa12 is covalently bonded to the second of the three Xaa12, and Z 2 is covalently bonded to When s=4, the first of four Xaa12 is covalently bonded to Xaa11, the second of four Xaa12 is covalently bonded to Xaa11, the second of four Xaa12 is covalently bonded to the first of four Xaa12, the third of four Xaa12 is covalently bonded to the second of four Xaa12, the fourth of four Xaa12 is covalently bonded to the third of four Xaa12, and the fourth of four Xaa12 is covalently bonded to the third of four Xaa12; Z 2 is covalently bonded to When s=5, the first of the five Xaa12 is covalently bonded to Xaa11, the second of the five Xaa12 is covalently bonded to the first of the five Xaa12, the third of the five Xaa12 is covalently bonded to the second of the five Xaa12, the fourth of the five Xaa12 is covalently bonded to the third of the five Xaa12, the fourth of the five Xaa12 is covalently bonded to the third of the five Xaa12, the fifth of the five Xaa12 is covalently bonded to the fourth of the five Xaa12, and Z 2 is covalently bound to; Z 2 is a compound of CT, an -en-chelator, an -Ape-chelator and formula (CT-I)

[0072] [ka]

[0073] is selected from the group consisting of CT is selected from the group consisting of NH2, en, en(Me)2, en(Me), NHBu, NHnPen, AF488N3K-NH2, OH and Throl-OH; w is selected from the group consisting of 2, 3 and 4; L 4 is selected from the group consisting of Bond, Ttds, Pamb, APAc, O2Oc, Ahx, Pab and Cmp; Z 4is a chelator; However, L 2 is a bond and CT is NHnPen, then Xaa10 may be absent. or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, which may contain a therapeutically active nuclide or a diagnostically active nuclide. Embodiment 3. Z 1 , Z 2 , Z 3 and Z 4 or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein only one of Embodiment 4. A compound according to any one of embodiments 1, 2 and 3, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein X is a bond. Embodiment 5. A compound of any one of embodiments 1, 2, and 3, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein X is CH2. Embodiment 6.

[0074] Z 2 But CT; Xaa7 is selected from the group consisting of formula (VIII), formula (IX), Dtc and Oic; A compound according to any one of embodiments 1, 2, 3, 4 and 5, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 7. Z 1 The compound of embodiment 6, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Embodiment 8.

[0075] L 1 But -(Xaa1) k wherein k is selected from the group consisting of 1 and 2. A compound according to any one of embodiments 6 and 7, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 9. k is 2 and L 1 is represented by formula (XIII): -Xaa1 b -Xaa1 a - (XIII) and In the formula, Xaa1 a is covalently linked to Xaa2; Xaa1 a is selected from the group consisting of Thr, Ile, and Leu; Xaa1 b is selected from the group consisting of Cmp, Ttds, Pamb, Ahx, APAc, Bal, O2Oc and Pab; A compound according to any one of embodiments 6, 7 and 8, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 10. Xaa1 a is Thr, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 11. Xaa1 b The compound of any one of embodiments 9 and 10, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein Embodiment 12. The compound of any one of embodiments 6, 7, and 8, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein k is 1 and Xaa1 is selected from the group consisting of Cmp, Pamb, Bal, Pab, Ahx, APAc, Thr, Pamp, and PPAc. Embodiment 13. The compound of embodiment 12, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa1 is Pamb. Embodiment 14. L 2 bond and -Xaa11-(Xaa12) s-, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 15. L 2 But -Xaa11-(Xaa12) s - and; s is selected from the group consisting of 0 and 1; Xaa11 is selected from the group consisting of Thr, Bal, Gln, Phe, Gab, Nmt, Gly, Leu, Trp, Glu and Pro; A compound according to embodiment 14, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 16. A compound according to any one of embodiments 14 and 15, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa11 is selected from the group consisting of Thr and Bal. Embodiment 17. The compound of embodiment 16, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa11 is Thr. Embodiment 18. The compound of embodiment 16, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa11 is Bal. Embodiment 19. A compound according to any one of embodiments 15, 16, 17, and 18, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein s is 0. Embodiment 20. A compound according to any one of embodiments 14, 15, 16, 17, and 18, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein s is 1; and Xaa12 is Asp. Embodiment 21. L 2 The compound of embodiment 14, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein is a bond. Embodiment 22. The compound of any one of embodiments 14, 15, 16, 17, 18, 19, 20, and 21, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein CT is selected from the group consisting of NH2, en, en(Me), en(Me)2, NHBu, Throl-OH, and OH. Embodiment 23. A compound of embodiment 22, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein CT is NH2. Embodiment 24. L 2 -Z 2 A compound according to any one of embodiments 6, 7, 8, 9, 10, 11, 12, 13 and 14, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein is selected from the group consisting of Thr-NH2, Bal-NH2, Glu-NH2, Pro-NH2, Gln-NH2, Trp-NH2, Leu-NH2, Gly-NH2, Nmt-NH2, Gab-NH2, Phe-NH2, Throl-OH and Thr-OH. Embodiment 25. L 2 -Z 2 is selected from the group consisting of Thr-NH2 and Bal-NH2, or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, or a hydrate thereof. Embodiment 26. L 2 -Z 2 is Thr-NH2, or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, or a hydrate thereof. Embodiment 27. L 2 -Z 2 is Bal-NH2, or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, or a hydrate thereof. Embodiment 28. Xaa7 is selected from the group consisting of formula (VIII), formula (IX), Dtc and Oic, wherein: R 7a is H, (C1-C6) alkyl and (CH2) t R 7g selected from the group consisting of: t is selected from the group consisting of 1 and 2; R 7g is selected from the group consisting of OH, CO2H and NH2; 28. A compound according to any one of embodiments 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26 and 27, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 29. The compound of embodiment 28, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa7 is selected from the group consisting of Aib, Ala, Glu, Pro, Dfp, glu, Amd, 4Tfp, Pam, Deg, Nmg, Ams, ams, amd, Dtc, and Oic. Embodiment 30. Xaa7 is selected from formula (VIII), wherein: R 7a is selected from the group consisting of H, (C1-C2) alkyl, CH2OH, CH2CO2H and CH2CH2CO2H; R 7b is selected from the group consisting of H and (C1-C2) alkyl; R 7c But H, 29. A compound according to embodiment 28, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 31. The compound of any one of embodiments 28, 29, and 30, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa7 is selected from the group consisting of Aib and Ala. Embodiment 32. A compound according to any one of embodiments 28, 29, 30, and 31, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa7 is Aib. Embodiment 33. A compound according to any one of embodiments 28, 29, 30, and 31, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa7 is Ala. Embodiment 34.

[0076] Z 1 is NT, and Xaa7 is selected from the group consisting of formula (VIII), formula (IX), Dtc and Oic; A compound according to any one of embodiments 1, 2, 3, 4 and 5, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 35. Z 2 is selected from the group consisting of en-chelators, -Ape-chelators and formula (CT-I), and Z 2 is formula (CT-I), Z 4 The compound of embodiment 34, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Embodiment 36.

[0077] L 1 , bond and (Xaa1) k selected from the group consisting of: k is selected from the group consisting of 1 and 2; A compound according to any one of embodiments 34 and 35, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 37. k is 2 and L 1 Formula (XIII) -Xaa1 b -Xaa1 a - (XIII) and In the formula, Xaa1 a is covalently attached to Xaa2 of formula (I); Xaa1 a But Thr; Xaa1 b is Met or Cmp, A compound according to embodiment 36, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 38. Xaa1 bis Met, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 39. A compound according to any one of embodiments 37 and 38, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein NT is selected from the group consisting of H, Ac, and nBuCAyl. Embodiment 40. The compound of embodiment 39, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein NT is Ac. Embodiment 41. The compound of embodiment 36, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein k is 1 and Xaa1 is selected from the group consisting of Thr, Ala, Pamp, and Ser. Embodiment 42. The compound of any one of embodiments 37 and 38, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa1 is Thr. Embodiment 43. The compound of any one of embodiments 41 and 42, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein Xaa1 is selected from the group consisting of Thr and Pamp; and NT is selected from the group consisting of Ac, nBuCAyl and Hex. Embodiment 44. A compound according to embodiment 43, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa1 is Thr and NT is Ac. Embodiment 45. L 1 The compound of embodiment 36, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein is a bond. Embodiment 46. The compound of embodiment 45, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein NT is selected from the group consisting of Ac, HPA, HYDAc, Iva, SaPr, and HO-succinyl. Embodiment 47. The compound of embodiment 46, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein NT is Ac. Embodiment 48.

[0078] L 2 But -Xaa11-(Xaa12) s - and; and s is selected from the group consisting of 0, 1 and 2; A compound according to any one of embodiments 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46 and 47, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 49. Z 2 is Formula (CT-I), or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, or a hydrate thereof. Embodiment 50. The compound of any one of embodiments 48 and 49, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa11 is Thr. Embodiment 51. L 2 but, -Xaa11-(Xaa12) s and s is 1; and Xaa12 is selected from the group consisting of Asp, Cmp, Ttds, Pamb, O2Oc, APAc and Pab; A compound according to any one of embodiments 48, 49 and 50, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 52. A compound according to embodiment 51, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa11 is Thr and Xaa12 is Cmp. Embodiment 53. L 2 But -Xaa11-(Xaa12) s and s is 2 and L 2 But the structure -Xaa11-Xaa12 a -Xaa12 b -having the formula Xaa12 ais selected from the group consisting of Asp, Cmp, Ttds, Pamb, O2Oc, APAc, and Pab; and Xaa12 b But Ttds, A compound according to any one of embodiments 48, 49 and 50, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 54. Xaa11 is Thr and Xaa12 a is Asp, and Xaa12 b is Ttds, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 55. Z 2 49. The compound of any one of embodiments 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, and 48, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Embodiment 56. Z 2 The compound of embodiment 55, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Embodiment 57. L 2 57. The compound of any one of embodiments 55 and 56, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa11 is a bond or Xaa11. Embodiment 58. L 2 The compound of embodiment 57, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein is a bond. Embodiment 59. L 2 is Xaa11 and Xaa11 is Thr, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 60. Z 2 is an -Ape- chelator, and L 256. The compound of embodiment 55, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein: is -Xaa11-; and Xaa11 is Thr. Embodiment 61. Xaa7 is selected from formula (VIII), formula (IX), Dtc and Oic, wherein: R 7a is H, (C1-C6) alkyl and (CH2) t R 7g selected from the group consisting of: R 7g is selected from the group consisting of OH and COH; t is selected from the group consisting of 1 and 2; R 7b is selected from the group consisting of H and (C1-C6) alkyl; 61. A compound according to any one of embodiments 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59 and 60, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 62. The compound of embodiment 61, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa7 is selected from the group consisting of Aib, Ala, Glu, Pro, Dfp, glu, Amd, 4Tfp, Pam, Deg, Nmg, Ams, ams, amd, Dtc, and Oic. Embodiment 63. Xaa7 is of formula (VIII), wherein: R 7a is selected from the group consisting of H, (C1-C2) alkyl, CH2OH, CH2CO2H and CH2CH2CO2H; R 7b is selected from the group consisting of H and (C1-C2) alkyl; R 7c But H, A compound according to embodiment 61, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 64. A compound according to any one of embodiments 61, 62, and 63, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa7 is selected from the group consisting of Ala and Aib. Embodiment 65. A compound according to any one of embodiments 61, 62, 63, and 64, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa7 is Aib. Embodiment 66. A compound according to any one of embodiments 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, and 65, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa7 is Ala. Embodiment 67. Xaa7 is selected from the group consisting of formula (X) and formula (XI); Z 3 is a chelator; Z 1 But in the NT; Z 2 However, CT is A compound according to any one of embodiments 1, 2, 3, 4 and 5, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 68.

[0079] L 1 bond and -(Xaa1) k - is selected from the group consisting of: k is 1; A compound according to embodiment 67, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 69. A compound according to embodiment 68, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa1 is Thr. Embodiment 70. L 1 The compound of embodiment 68, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein is a bond. Embodiment 71. The compound of any one of embodiments 67, 68, 69, and 70, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein NT is selected from the group consisting of Ac, SaPr, Iva, and HPA. Embodiment 72. A compound of embodiment 71, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein NT is Ac. Embodiment 73. L 2 bond and -Xaa11-(Xaa12) s -, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 74. The compound of embodiment 73, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa11 is selected from the group consisting of Thr, Gln, Phe, Gab, Nmt, Bal, Gly, Leu, Trp, Glu, and Pro. Embodiment 75. A compound according to any one of embodiments 73 and 74, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa11 is Thr. Embodiment 76. A compound according to any one of embodiments 73, 74, and 75, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein s is 1; and Xaa12 is Asp. Embodiment 77. A compound according to any one of embodiments 73, 74, 75, and 76, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein CT is NH2. Embodiment 78. The compound of any one of embodiments 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, and 77, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa7 is selected from the group consisting of Lys and Apc, and the chelator is attached to the ε-nitrogen atom of Lys or the γ-nitrogen atom of Apc, and an optional linker is interspersed between Apc or Lys and the chelator. Embodiment 79. The compound of embodiment 78, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein the chelator is selected from the group consisting of DOTA, DOTAGA, LSC, NOPO, PCTA, DOTAM, Macropa, Crown, NOTA, and NODAGA. Embodiment 80. The compound of any one of embodiments 78 and 79, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein, when the linker is interspersed, the linker is selected from the group consisting of O2Oc, Pab, Ahx, APAc, Pamb, Cmp and Ttds. Embodiment 81. The compound of any one of embodiments 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, and 80, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa7 is selected from the group consisting of Apc(DOTA), Lys(DOTAGA-O2Oc), Lys(DOTA-O2Oc), Lys(DOTA-Pab), Lys(DOTA-Ahx), Lys(DOTA-APAc), Lys(DOTA-Pamb), Lys(DOTA-Cmp), Lys(DOTA-Ttds), Lys(DOTA). Embodiment 82. Xaa7 is selected from formula (X), wherein: u is 4; L 3 However, -(Xab1) v - and; v is 1; and Xab1 is selected from the group consisting of Ttds, Pamb, APAc, O2Oc, Ahx and Pab; A compound according to any one of embodiments 67, 68, 69, 70, 71, 72, 73, 74, 75, 76 and 77, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 83. Any 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 8, 39, 40, 41, 42, 43, 44, 45, 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, 73, 74, 75, 76, 77, 78, 79, 80, 81 and 82, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 84. The compound of embodiment 83, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein the chelator is selected from the group consisting of DOTA and DOTAGA. Embodiment 85. The compound of embodiment 84, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein the chelator is DOTA. Embodiment 86. 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, wherein Xaa2 is selected from the group consisting of Aib, Ala, Ams, ams, Deg, Pam and Pro. 45, 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, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84 and 85, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 87. The compound of embodiment 86, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa2 is selected from the group consisting of Aib, Ala, Pam, Deg, Ams, and ams. Embodiment 88. A compound according to embodiment 87, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa2 is Aib. Embodiment 89. The compound of embodiment 87, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa2 is Ala. Embodiment 90. 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, wherein Xaa3 is selected from the group consisting of Phe, 1Ni, 2Ni, 6Clw, Cys(Bzl), Hfe, and Trp, and Phe, Nmf, and Hfe are optionally substituted by one or two substituents independently selected from the group consisting of Cl, CH3, F, CN, CF3, and OH. 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 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, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, and 89, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 91. The compound of embodiment 90, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is selected from the group consisting of Phe, Nmf, and Hfe, and Phe, Nmf, and Hfe are optionally substituted by one substituent selected from the group consisting of Cl, CH3, F, CN, CF3, and OH. Embodiment 92. The compound of embodiment 91, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is Phe optionally substituted with one substituent selected from the group consisting of Cl, CH3, F, CN, CF3, and OH. Embodiment 93. The compound of embodiment 92, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is Phe optionally substituted with 1 substituent selected from the group consisting of Cl, CH3, F, CN, CF3. Embodiment 94. The compound of embodiment 93, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is selected from the group consisting of Phe, Pcf, Mcf, Mff, Mnf, Mmf, Pmf, Pnf, Pff, Mtf, and Ptf. Embodiment 95. A compound according to embodiment 94, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is selected from the group consisting of Phe and Pcf. Embodiment 96. A compound according to embodiment 94, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is Phe. Embodiment 97. A compound of embodiment 94, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is Pcf. Embodiment 98. Xaa5 is selected from the group consisting of Formula (Va), Formula (Vb), Hgn and Nle; R 5g , R 5h and R 5i But CH3, 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96 and 97, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 99. Xaa5 is selected from formula (Va): R 5a H, CH3, Ac and C(=NR 5d )NR 5e R 5fselected from the group consisting of: R 5e and R 5f is independently selected from the group consisting of H and CH3; R 5b But H; R 5c But H; m is selected from the group consisting of 3 and 4; A compound according to embodiment 98, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 100. R 5a is selected from the group consisting of H and CH3; and m is 4, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 101. A compound according to any one of embodiments 98, 99, and 100, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa5 is Lys. Embodiment 102. The compound of any one of embodiments 98, 99, and 100, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa5 is Lys(Me). Embodiment 103. The compound of any one of embodiments 98, 99, and 100, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa5 is Kip. Embodiment 104. The compound of any one of embodiments 98, 99, and 100, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa5 is KMe3. Embodiment 105. Xaa6 is selected from the group consisting of formula (VI), formula (VII) and Nle; In the formula, R 6a However, H, C(=NR 6e )NR 6f R 6g and C(=O)R 6h selected from the group consisting of: R 6e But H; R6f H, CH3, Ac, NO2 and C(=O)NR 6i R 6j selected from the group consisting of: R 6g is selected from the group consisting of H and CH3; R 6h is selected from the group consisting of CH3, NH2 and NHC(=NH)NH2; R 6b But H; R 6c But H; R 6d is selected from the group consisting of NHC(=NH)NH2 and NH2; 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 105, 106, 107, 108, 109, 110, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 1 104, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 106. The compound of embodiment 105, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa6 is selected from the group consisting of Arg, Arg(Me), Cit, Egd, RMe2a, RMe3, Nle, Gln, Lys(Ac), Hgn, Arg(EtCAyl), Urr, Arg(Ac), Gln(Gu), Orn, Har, RMe2, and Eew. Embodiment 107. Xaa6 is selected from formula (VI), wherein: n is 3; R 6a But C(=NH)NHR 6f and; R 6f is selected from the group consisting of H, Ac, NO2 and CH3; A compound according to embodiment 105, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 108. The compound of any one of embodiments 105, 106, and 107, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa6 is Arg. Embodiment 109. A compound according to any one of embodiments 105, 106, and 107, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa6 is Arg(Me). Embodiment 110. A compound according to any one of embodiments 105 and 106, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa6 is Cit. Embodiment 111. The compound of any one of embodiments 105 and 106, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa6 is Egd. Embodiment 112. The compound of any one of embodiments 105 and 106, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa6 is RMe2a. Embodiment 113. A compound according to any one of embodiments 105 and 106, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa6 is RMe3. Embodiment 114. Xaa8 is a group of formula (XIV):

[0080] [ka]

[0081] , Gly, Val, Met, Ile, and Thr; In the formula, R 8ais selected from the group consisting of H, OH, NH2, COOH, C(=O)NH2, NHC(=NH)NH2, (C1-C8) alkyl, aryl, and heteroaryl; w is selected from the group consisting of 1, 2 and 3; R 8b is selected from the group consisting of H and CH3; 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69 9, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112 and 113, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 115.

[0082] R 8a is selected from the group consisting of OH, COOH, C(=O)NH2, phenyl, NHC(=NH)NH2, indole, and CH(CH3)2; w is selected from the group consisting of 1 and 2; A compound according to embodiment 114, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 116. The compound of any one of embodiments 114 and 115, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa8 is selected from the group consisting of Asn, Trp, Phe, Arg, Ser, Gly, Leu, Asp, Nmn, Glu, and asn. Embodiment 117. A compound according to embodiment 116, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa8 is Asn. Embodiment 118. Xaa10 is a compound of formula (XII):

[0083] [ka]

[0084] wherein: R 10b is selected from the group consisting of H and CH3; R 10c But H, 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116 and 117, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 119. The compound of embodiment 118, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa10 is selected from the group consisting of Tle, Leu, Val, Npg, and Ile. Embodiment 120. The compound of embodiment 119, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa10 is selected from the group consisting of Tle, Leu, Val, and Npg. Embodiment 121. A compound according to embodiment 120, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein XaalO is Tle. Embodiment 122. The compound of embodiment 120, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein XaalO is Leu. Embodiment 123. A compound of Formula (Ia)

[0085] [ka]

[0086] 34. The compound 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, and 33, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Embodiment 124. The compound of embodiment 123, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is selected from the group consisting of Phe, 1Ni, 2Ni, 6Clw, Cys(Bzl), Hfe, and Trp, and Phe, Nmf, and Hfe are optionally substituted by one or two substituents independently selected from the group consisting of Cl, CH3, F, CN, CF3, and OH. Embodiment 125. The compound of embodiment 124, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is selected from the group consisting of Phe, Nmf, and Hfe, and Phe, Nmf, and Hfe are optionally substituted by one substituent selected from the group consisting of Cl, CH3, F, CN, CF3, and OH. Embodiment 126. The compound of embodiment 125, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is Phe optionally substituted with one substituent selected from the group consisting of Cl, CH3, F, CN, CF3, and OH. Embodiment 127. The compound of embodiment 125, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is Phe. Embodiment 128. A compound of embodiment 125, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa3 is Pcf. Embodiment 129. Xaa10 is a group of formula (XII)

[0087] [ka]

[0088] wherein: R 10b is selected from the group consisting of H and CH3; R 10c But H, 129. A compound according to any one of embodiments 123, 124, 125, 126, 127 and 128, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 130. Xaa10 is a compound of Formula (XIV)

[0089] [ka]

[0090] or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 131. R 10a is selected from the group consisting of C(CH3)3, CH2CH(CH3)2, CH(CH3)2, CH(CH3)C2H5 and CH2C(CH3)3, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 132. R 10ais C(CH3)3, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 133. R 10a is CH2CH(CH3)2, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 134. A compound of Formula (Ib)

[0091] [ka]

[0092] and In the formula, R 3c is selected from the group consisting of H, Cl, CH3, F, CN, CF3 and OH; R 3c is in the meta or para position of the phenyl ring of formula (Ib), 134. A compound according to any one of embodiments 123, 124, 125, 126, 127, 128, 129, 130, 131, 132 and 133, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 135. R 3c is H, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 136. R 3c is Cl and R 3c is in the para position of the phenyl ring of Formula (Ib), or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 137.

[0093] R 5a H, CH3, C(CH3)2, Ac and C(=NR 5d )NR 5e R 5f selected from the group consisting of: R 5d , R 5e and R5f is independently selected from the group consisting of H and CH3; and R 5b is selected from the group consisting of H and CH3; m is selected from the group consisting of 3 and 4; 135. A compound according to any one of embodiments 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, and 134, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 138. R 5a is selected from the group consisting of H and CH3, and R 5b The compound of embodiment 137, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein is H and m is 4. Embodiment 139. R 5a is CH3 and R 5b The compound of embodiment 137, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein is H and m is 4. Embodiment 140. R 5a is C(CH3)2 and R 5b The compound of embodiment 137, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein is H and m is 4. Embodiment 141.

[0094] R 6a However, H, C(=NR 6e )NR 6f R 6g and C(=O)R 6h selected from the group consisting of: R 6e is selected from the group consisting of H and CH3; R 6f H, CH3, Ac, NO2 and C(=O)NR 6i R 6j selected from the group consisting of: R 6i is selected from the group consisting of H and (C1-C2) alkyl; R6j But H; R 6g is selected from the group consisting of H and CH3; R 6h is selected from the group consisting of CH3, NH2 and NHC(=NH)NH2; R 6b and R 6c are each and individually selected from the group consisting of H and CH3; n is selected from the group consisting of 3 and 4; 140. A compound according to any one of embodiments 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139 and 140, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 142. n is selected from the group consisting of 3 and 4, and R 6c is H, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 143.

[0095] n is 3; R 6a However, C(=NR 6e )NR 6f R 6g and; R 6e But H; R 6f H, CH3, Ac, NO2 and C(=O)NHR 6i selected from the group consisting of: R 6g is H; and R 6b But H, 141 and 142. A compound according to any one of embodiments 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141 and 142, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 144. R6f is selected from the group consisting of H, Ac, NO2 and CH3, or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate or hydrate thereof. Embodiment 145. R 6f A compound according to any one of embodiments 141, 142, 143, and 144, preferably embodiment 143, wherein is H, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 146. R 6f A compound according to any one of embodiments 141, 142, 143, and 144, preferably embodiment 143, wherein is CH3, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 147.

[0096] n is 3 and R 6e , R 6f and R 6g are each and independently selected from the group consisting of CH3; A compound according to embodiment 143, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 148.

[0097] n is 3; R 6a But C(=O)R 6h and R 6h is NH2, 143. A compound according to any one of embodiments 141 and 142, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 149.

[0098] R 7a is selected from the group consisting of H, (C1-C2) alkyl, CH2OH and CH2CO2H and CH2CH2CO2H; R 7b is selected from the group consisting of H and (C1-C2) alkyl; The compound of any one of embodiments 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, and 148. Embodiment 150. R 7c is H, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 151.

[0099] R 7a is selected from the group consisting of (C1-C2) alkyl, CH2OH, CH2CO2H, and CH2CH2CO2H; R 7b is selected from the group consisting of (C1-C2) alkyl; 151. A compound according to any one of embodiments 149 and 150, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 152. R 7a is CH3;R 7b The compound of embodiment 151, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein is CH3. Embodiment 153. R 7a is H;R 7b The compound of embodiment 151, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein is CH3. Embodiment 154.

[0100] R 8a is selected from the group consisting of H, OH, COOH, C(=O)NH2, CH2CH2NHC(=NH)NH2, (C1-C8)alkyl, aryl, and heteroaryl; R 8b is selected from the group consisting of H and CH3; 152, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 155.

[0101] R 8a is selected from the group consisting of OH, COOH, C(=O)NH2, CH(CH3)2, CH2CH2NHC(=NH)NH2, phenyl and indole; 152, 153, and 154, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 156. R 8b is H. Embodiment 157. R 8a The compound according to any one of embodiments 154, 155, and 156, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein is C(=O)NH2. Embodiment 158. R 3c is selected from the group consisting of H, Cl, CH3, F, CN and CF3, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 159. R 3cis H, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 160. R 3c is Cl and is in the para position, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof. Embodiment 161.

[0102] Xaa2 is Aib or Ala; Xaa3 is Phe or Pcf; Xaa5 is Lys(Me), Lys, Kip, or KMe3; Xaa6 is Arg(Me), Arg, Egd, Cit, RMe2a, or RMe3; Xaa7 is Aib or Ala; Xaa8 is Asn; and Xaa10 is Tle or Leu, 34. A compound according to 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 and 33, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 162.

[0103] Xaa2 is Aib or Ala; Xaa3 is Phe or Pcf; Xaa5 is Lys(Me), Lys, or Kip; Xaa6 is Arg(Me), Arg, Egd, Cit, or RMe2a; Xaa7 is Aib or Ala; Xaa8 is Asn; and Xaa10 is Tle or Leu, A compound according to embodiment 161, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 163.

[0104] Xaa2 is Aib or Ala; Xaa3 is Phe or Pcf; Xaa5 is Lys(Me) or Lys; Xaa6 is Arg(Me) or Arg; Xaa7 is Aib or Ala; Xaa8 is Asn; and Xaa10 is Tle or Leu, A compound according to embodiment 161, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 164.

[0105] Xaa2 is Aib or Ala; Xaa3 is Phe or Pcf; Xaa5 is Lys(Me) or Lys; Xaa6 is Arg(Me) or Arg; Xaa7 is Aib or Ala; Xaa8 is Asn; and Xaa10 is Tle, A compound according to embodiment 161, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 165.

[0106] Z 1 is a chelator; L 1 Formula (XIII) -Xaa1 b -Xaa1 a - (XIII) and In the formula, Xaa1 a is covalently linked to Xaa2; Xaa1 a is Thr; and Xaa1 b But Cmp, A compound according to any one of embodiments 161, 162, 163, 164 and 165, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof. Embodiment 1669.

[0107] Z 1 is a chelator; L 1 But, Pamb, A compound according to any one of embodiments 161, 162, 163 and 164, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 167.

[0108] Z 2 is NH2; and L 2 But Thr is 167. A compound according to any one of embodiments 161, 162, 163, 164, 165 and 166, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 168.

[0109] Z 2 is NH2; and L 2 But Bal, 167. A compound according to any one of embodiments 161, 162, 163, 164, 165 and 166, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 169.

[0110] Z 2 is NH2; and L 2 is Thr-Asp, 167. A compound according to any one of embodiments 161, 162, 163, 164, 165 and 166, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 170.

[0111] Z 2 is NH2; and L2 is a bond, 167. A compound according to any one of embodiments 161, 162, 163, 164, 165 and 166, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 171.

[0112] Xaa2 is Aib or Ala; Xaa3 is Phe or Pcf; Xaa5 is Lys or Lys(Me); Xaa6 is Arg or Arg(Me); Xaa7 is Aib or Ala; Xaa8 is Ans; and Xaa10 is Tle or Leu, 67. A compound according to any one of embodiments 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65 and 66, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 172.

[0113] Z 1 is Ac; and L 1 But Thr is A compound according to embodiment 171, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 173.

[0114] Z 1 is Ac; and L 1 is a bond, A compound according to embodiment 171, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 174.

[0115] Z 1 But, Ac; L 1Formula (XIII) -Xaa1 b -Xaa1 a - (XIII) and In the formula, Xaa1 a is covalently attached to Xaa2 of formula (I); Xaa1 a is Thr; and Xaa1 b is Met or Cmp, A compound according to embodiment 171, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 175.

[0116] Z 2 is a chelator; and L 2 But, en, A compound according to any one of embodiments 171, 172, 173 and 174, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 176.

[0117] Z 2 is a chelator; L 2 But -Xaa11-Xaa12 a -Xaa12 b - in which Xaa11 is Thr; Xaa12 a is Asp; and Xaa12 b But Ttds, A compound according to any one of embodiments 171, 172, 173 and 174, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 177.

[0118] Z 2 is a chelator; and L 2 is -Xaa11-Xaa12; Xaa11 is Thr; Xaa12 a is Cmp; and Xaa12 b But Ttds, A compound according to any one of embodiments 171, 172, 173 and 174, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 178. Embodiments 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 300, 309, 309, 309, 400, 410, 411, 412, 413, 414, 415, 420, 421, 42 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 200, 204, 205, 206, 207, 208, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176 and 177, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 179. The compound of embodiment 178, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, wherein the chelator is selected from the group consisting of DOTA and DOTAGA. Embodiment 180. The compound of embodiment 179, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, wherein the chelator is DOTA. Embodiment 181. The following: DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0194); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH2(PSM-0433); DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0492); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0178); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0179); Ac-Thr-Aib-Phe-[Cys-Lys-Gln-Ala-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0180); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Hyp-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0181); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-Ttds-Ttds-AF488N3K-NH2(PSM-0183); DOTA-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH2(PSM-0184); Ac-Pamp-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en-DOTA(PSM-0186); Ac-Thr-Deg-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0187); SaPr-Aib-Pcf-[Cys-Lys-Arg-Lys(DOTA-APAc)-Asn-Cys]-Tle-Thr-NH2(PSM-0188); Ac-Thr-Aib-Pcf-[Cys-Lys-Gln(Gu)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0189); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH2(PSM-0190); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-APAc-lys(DOTA)-NH2(PSM-0191); DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0193); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Glu-Asn-Cys]-Nle-Thr-Asp-NH2(PSM-0197); DOTA-Cmp-Tle-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0198); DOTA-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(PSM-0199); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg-Aib-Asn-Cys]-Tle-NH2(PSM-0200); DOTA-Pamb-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0202); DOTA-Cmp-Thr-Aib-Pcf-[Cys-KMe2-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0203); nBuCAyl-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0204); Ac-Thr-Aib-Pcf-[Cys-Nle-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0205); nBuCAyl-Thr-Aib-Mcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0207); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-NHnPen(PSM-0208); DOTA-Bal-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0209); Ac-Thr-Aib-Phe-[Cys-Gln-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0210); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Pab)-Asn-Cys]-Tle-Thr-NH2(PSM-0211); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH2(PSM-0212); SaPr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0215); DOTA-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH2(PSM-0216); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Dfp-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0217); DOTAGA-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0218); DOTA-Cmp-Leu-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0220); DOTA-Pamb-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(PSM-0221); DOTA-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(PSM-0222); DOTA-Cmp-Aib-Pcf-[Cys-Lys-Arg(Ac)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0223); SaPr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0224); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Har-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0225); H-Met-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Leu-Thr-Asp-Gly-Ser-Ttds-Ttds-Ttds-Lys(Bio)-NH2(PSM-0226); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-amd-Asn-Cys]-Tle-Thr-NH2(PSM-0227); Ac-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0228); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Met-Cys]-Tle-Thr-NH2(PSM-0229); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH2(PSM-0230); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH2(PSM-0231); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Nmg-Asn-Cys]-Tle-Thr-NH2(PSM-0232); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Pam-Asn-Cys]-Tle-Thr-NH2(PSM-0233); DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0234); Ac-Thr-Aib-Phe-[Cys-Lys-Nmr-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0235); Ac-Thr-Aib-Pcf-[Cys-Nle-Gln(Gu)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0236); DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-NH2(PSM-0237); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Trp-Cys]-Tle-Thr-NH2(PSM-0238); Hex-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH2(PSM-0239); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Arg-Cys]-Tle-Thr-NH2(PSM-0240); DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(PSM-0241); Ac-Thr-Aib-Mcf-[Cys-Lys-Arg-Lys(DOTA-O2Oc)-Asn-Cys]-Tle-Thr-NH2(PSM-0243); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Kip-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0244); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Orn-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0245); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-ala-Asn-Cys]-Tle-Thr-NH2(PSM-0246); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-RMe2-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0247); DOTA-Cmp-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0248); Ac-Thr-Aib-1Ni-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0249); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Ttds-Ttds-Lys(Bio)-NH2(PSM-0250); DOTA-Ttds-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Leu-Thr-Asp-NH2(PSM-0251); Ac-Thr-Aib-Phe-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0252); Ac-Thr-Aib-Phe-[Cys-Lys-Glu-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0253); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Eew-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0254); DOTA-Cmp-Thr-Aib-Mpa-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0255); DOTA-Cmp-Thr-ams-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0256); DOTA-Cmp-Thr-Aib-Opa-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0257); nBuCAyl-Thr-Aib-Phe-[Cys-Lys-Opy-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0258); DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0259); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-glu-Asn-Cys]-Tle-Thr-NH2(PSM-0260); DOTA-APAc-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0261); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Glu-NH2(PSM-0262); DOTA-APAc-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0263); Ac-Thr-Aib-Mtf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0264); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH2(PSM-0266); HPA-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH2(PSM-0267); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en-DOTA(PSM-0269); DOTA-Pamb-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0270); AF488Ahx-Ttds-Ttds-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0272); DOTA-Pamb-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(PSM-0273); DOTA-Cmp-Thr-Aib-Eaa-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0274); Ac-Thr-Aib-Mcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0275); Ac-Thr-Aib-Pnf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0278); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Ser-Cys]-Tle-Thr-NH2(PSM-0279); Ac-Thr-Aib-Phe-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0280); Ac-Aib-Pcf-[Cys-Lys-Arg-Lys(DOTA-APAc)-Asn-Cys]-Tle-Thr-NH2(PSM-0282); DOTA-Pamb-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0283); Ac-Thr-Aib-Mcf-[Cys-Lys-Cit-Lys(DOTA-O2Oc)-Asn-Cys]-Tle-Thr-NH2(PSM-0284); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH2(PSM-0285); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH2(PSM-0287); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH2(PSM-0288); Hex-Thr-Aib-Phe-[Cys-Lys-Gln-Aib-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH2(PSM-0289); Iva-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH2(PSM-0292); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Ser-Cys]-Tle-Thr-NH2(PSM-0293); Ac-Thr-Aib-Pff-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0294); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH2(PSM-0295); DOTA-Cmp-Thr-Aib-Mpa-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0296); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Gab-NH2(PSM-0297); Ac-Aib-Pcf-[Cys-Lys-Arg(Ac)-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0298); Ac-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Leu-Thr-Asp-Ttds-lys(DOTA)-NH2(PSM-0299); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-OH(PSM-0300); Ac-Thr-Aib-Mcf-[Cys-Lys-Arg-Lys(DOTAGA-O2Oc)-Asn-Cys]-Tle-Thr-NH2(PSM-0301); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Amd-Asn-Cys]-Tle-Thr-NH2(PSM-0302); Ac-Thr-Aib-Phe-[Cys-Lys-Gln-Aib-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH2(PSM-0303); DOTA-Cmp-Thr-Aib-6Clw-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0304); DOTA-Ttds-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Leu-Thr-NH2(PSM-0305); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(Me)2(PSM-0306); Ac-Thr-Aib-Phe-[Cys-Lys-Cit-Ala-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0307); DOTA-Cmp-Thr-Aib-5Clw-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0308); DOTA-Ahx-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0310); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Gab-OH(PSM-0313); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-ams-Asn-Cys]-Tle-Thr-NH2(PSM-0314); Ac-Thr-Aib-Phe-[Cys-Lys-arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0315); DOTA-Pab-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0316); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Har-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0317); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0318); Ac-Thr-Ala-Nmf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0319); Ac-Aib-Pcf-[Cys-Lys-Arg(Me)-Aib-Asn-Cys]-Tle-en-DOTA(PSM-0320); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Apc(DOTA)-Asn-Cys]-Tle-Thr-NH2(PSM-0321); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH2(PSM-0322); HPA-Aib-Pcf-[Cys-Lys-Arg-Lys(DOTA-APAc)-Asn-Cys]-Tle-Thr-NH2(PSM-0324); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA)-Asn-Cys]-Tle-Thr-NH2(PSM-0326); SaPr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH2(PSM-0328); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0329); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Leu-Thr-Asp-Ttds-lys(DOTA)-NH2(PSM-0330); DOTA-Cmp-Thr-Aib-Pcf-[Smc-Lys-Arg-Aib-Asn-Cys]-Tle-NH2(Alternative: DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Smc]-Tle-NH2)(PSM-0332); Ac-Thr-Aib-Phe-[Cys-Lys-Gln-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0334); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Ala-Cys]-Nle-Thr-Asp-NH2(PSM-0335); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0336); Ac-Thr-Aib-Pcf-[Cys-Lys-Nle-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0338); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTAGA)-NH2(PSM-0339); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Nmr-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0340); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Lys(Ac)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0341); DOTA-Ttds-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0342); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0345); DOTA-Cmp-Thr-Amd-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0346); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0349); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-leu-Thr-NH2(PSM-0350); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0351); DOTA-Bal-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0352); Iva-Aib-Pcf-[Cys-Lys-Arg-Lys(DOTA-APAc)-Asn-Cys]-Tle-Thr-NH2(PSM-0353); DOTA-Cmp-Thr-Aib-Mcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0354); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-RMe3-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0355); DOTA-Cmp-Ile-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0357); DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH2(PSM-0361); Ac-Thr-Aib-Phe-[Cys-Lys-Glu-Ala-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0363); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0365); DOTA-Cmp-Thr-amd-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0366); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH2(PSM-0367); DOTA-Ahx-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0368); DOTA-Cmp-Thr-Ams-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0369); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Lys(DOTA-O2Oc)-Asn-Cys]-Tle-Thr-NH2(PSM-0370); nBuCAyl-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0371); Ac-Thr-Aib-Pmf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0372); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0374); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Deg-Asn-Cys]-Tle-Thr-NH2(PSM-0375); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Trp-NH2(PSM-0376); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Val-Nmt-NH2(PSM-0377); H-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0378); Ac-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en-DOTA(PSM-0379); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0380); DOTA-Pamb-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH2(PSM-0381); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Ams-Asn-Cys]-Tle-Thr-NH2(PSM-0382); Ac-Thr-Aib-Mcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0383); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(PSM-0384); Ac-Thr-Aib-Phe-[Cys-Lys-Gln-Lys(DOTA)-Asn-Cys]-Tle-Thr-NH2(PSM-0385); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Pro-NH2(PSM-0388); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-asp-NH2(PSM-0389); DOTA-Cmp-Thr-Aib-6Clw-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0390); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Ape-DOTA(PSM-0391); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-4Tfp-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0392); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(PSM-0393); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Aib-Thr-NH2(PSM-0394); DOTA-Cmp-Thr-Aib-Pff-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0395); DOTA-Cmp-Thr-Aib-Mtf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0396); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA)-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0397); DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0398); Hex-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH2(PSM-0400); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-O2Oc)-Asn-Cys]-Tle-Thr-NH2(PSM-0401); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-asn-Cys]-Tle-Thr-NH2(PSM-0402); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Oic-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0403); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH2(PSM-0404); Hex-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Leu-Thr-Asp-Ttds-lys(DOTA)-NH2(PSM-0405); DOTA-Cmp-Thr-Ams-Pcf-[Cys-Lys-Arg-Ams-Asn-Cys]-Tle-Thr-NH2(PSM-0407); Ac-Thr-Nmg-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0408); DOTA-Cmp-Thr-Aib-Opa-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0409); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0410); Ac-Thr-Aib-Hfe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0411); Ac-Thr-Aib-Mmf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2 (PSM-0412); DOTA-PPAc-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2 (PSM-0413); Ac-Thr-Ala-Amf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2 (PSM-0414); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Cmp)-Asn-Cys]-Tle-Thr-NH2 (PSM-0415); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Glu-Asn-Cys]-Tle-Thr-NH2 (PSM-0416); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Pamb)-Asn-Cys]-Tle-Thr-NH2 (PSM-0419); DOTA-Cmp-Thr-Aib-Pcf-[Smc-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2 (Substitute: DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Smc]-Tle-NH2) (PSM-0420); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-leu-Thr-NH2 (PSM-0421); Ac-Thr-Aib-Phe-[Cys-Tap-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH2 (PSM-0422); Ac-Thr-Aib-Phe-[Cys-Lys-Gln-Lys(DOTA-Ttds)-Asn-Cys]-Tle-Thr-NH2 (PSM-0423); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH2 (PSM-0424); Hex-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH2(PSM-0425); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH2(PSM-0426); nBuCAyl-Thr-Aib-Pcf-[Cys-Lys-Opy-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0427); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0428); DOTA-Cmp-Thr-Aib-Mcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0431); DOTA-Pamb-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH2(PSM-0432); nBuCAyl-Thr-Aib-Phe-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0434); Ac-Thr-Aib-Phe-[Cys-Gln-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0435); DOTA-Bal-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0437); Ac-Thr-Aib-Phe-[Cys-Aph-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0439); Ac-Thr-Aib-Cys(Bzl)-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0441); Ac-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0442); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-NH2(PSM-0443); Iva-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH2(PSM-0444); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0445); DOTA-Pab-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0448); DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH2(PSM-0449); Iva-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0450); Ac-Thr-Aib-Phe-[Cys-Nmk-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0451); nBuCAyl-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH2(PSM-0452); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Leu-NH2(PSM-0453); DOTA-Cmp-Thr-Aib-Ppa-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0454); DOTA-Cmp-Nmt-Ala-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0455); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(Me)(PSM-0456); DOTA-Pamb-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH2(PSM-0458); DOTA-Cmp-Thr-Aib-Mnf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0459); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Pro-Asn-Cys]-Nle-Thr-Asp-NH2(PSM-0460); Hib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0461); Hex-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH2(PSM-0462); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-APAc)-Asn-Cys]-Tle-Thr-NH2(PSM-0464); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Ttds)-Asn-Cys]-Tle-Thr-NH2(PSM-0465); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Ac)-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0466); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH2(PSM-0467); Ac-Ser-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH2(PSM-0469); nBuCAyl-Thr-Aib-Mcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0470); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Pab-lys(DOTA)-NH2(PSM-0471); Ac-Aib-Pcf-[Cys-Lys(Me)-Arg-Aib-Asn-Cys]-Tle-en-DOTA(PSM-0472); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Ala-Asp-NH2(PSM-0476); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Gly-NH2(PSM-0477); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asp-Cys]-Tle-Thr-NH2(PSM-0478); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Gly-Cys]-Tle-Thr-NH2(PSM-0479); DOTA-Ttds-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Leu-NH2(PSM-0480); Ac-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-en-DOTA(PSM-0481); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0482); DOTA-Cmp-Thr-Aib-Pcf-[Cys-KMe3-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0483); nBuCAyl-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0484); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Hgn-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0485); Ac-Thr-Aib-Mcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0486); Ac-Thr-Aib-Tyr-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0488); DOTA-Cmp-Aib-Pcf-[Cys-Lys-Gln(Gu)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0489); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Bio)-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0490); Ac-Ala-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH2(PSM-0491); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-OH(PSM-0493); Ac-Aib-Pcf-[Cys-Lys-Gln(Gu)-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0494); Crown-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0495); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Glu-Cys]-Tle-Thr-NH2(PSM-0496); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Nml-Thr-NH2(PSM-0497); H-Met-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Leu-Thr-Asp-Gly-Ser-NH2(PSM-0498); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Egd-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0499); nBuCAyl-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH2(PSM-0500); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH2(PSM-0501); Hex-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH2(PSM-0502); DOTA-Cmp-Thr-Aib-Mmf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0503); DOTA-Ttds-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH2(PSM-0504); DOTA-O2Oc-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0505); Ac-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0506); DOTA-Cmp-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0507); Ac-Thr-Pam-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0508); HPA-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH2(PSM-0509); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NHBu(PSM-0510); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Orn-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0511); DOTA-Cmp-Thr-Aib-Opa-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0512); DOTA-Ahx-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0513); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH2(PSM-0514); Macropa-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0515); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en-DOTA(PSM-0516); Ac-Thr-Aib-2Ni-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0517); HYDAc-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0518); DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys-Gln-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0521); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Pamb-lys(DOTA)-NH2(PSM-0522); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-O2Oc-lys(DOTA)-NH2(PSM-0529); HPA-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0530); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Hgn-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0531); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Dtc-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0532); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-Ttds-lys(DOTA)-NH2(PSM-0533); DOTA-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH2(PSM-0534); Ac-Thr-Aib-Phe-[Cys-lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0535); DOTA-Cmp-Tle-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0538); DOTA-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH2(PSM-0539); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Gln-NH2(PSM-0540); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Phe-Cys]-Tle-Thr-NH2(PSM-0541); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Ttds)-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0542); DOTA-APAc-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0543); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Leu-Cys]-Tle-Thr-NH2(PSM-0545); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Urr-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0546); Ac-Thr-Pro-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH2(PSM-0547); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Nmk-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0548); DOTA-Cmp-Thr-Aib-Ptf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0549); Ac-Thr-Aib-Ptf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0550); Ac-Thr-Aib-Mff-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0551); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-NH2(PSM-0552); DOTA-Cmp-Thr-Aib-Mff-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH2(PSM-0553); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Throl-OH(PSM-0554); Ac-Thr-Aib-Mnf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0555); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Phe-NH2(PSM-0556); Ac-Thr-Aib-Ocf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0558); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0559); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Npg-NH2 (PSM-0560); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Ala-NH2 (PSM-0562); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Glu-Cys]-Tle-Thr-NH2 (PSM-0563); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH2 (PSM-0565); Ac-Thr-Aib-Phe-[Smc-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH2 (Substitute: Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Smc]-Tle-Thr-Asp-NH2) (PSM-0567); Hex-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-Ttds-lys (DOTA)-NH2 (PSM-0568); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg(Ac)-Aib-Asn-Cys]-Tle-Thr-NH2 (PSM-0569); Ac-Thr-Aib-Pcf-[Cys-Nle-Arg(Ac)-Aib-Asn-Cys]-Tle-Thr-NH2 (PSM-0570); nBuCAyl-Thr-Aib-Mcf-[Cys-Lys-Opy-Aib-Asn-Cys]-Tle-Thr-Cmp-lys (DOTA)-NH2 (PSM-0571); DOTA-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2 (PSM-0573); DOTA-Pamb-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH2 (PSM-0574); Bio-Ttds-Ttds-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0575); Hex-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH2(PSM-0576); HO-スクシニル-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0577); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Nle-Thr-Asp-NH2(PSM-0578); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg(EtCAyl)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0579); DOTA-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0580); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Ahx)-Asn-Cys]-Tle-Thr-NH2(PSM-0582); DOTA-Cmp-Thr-Aib-Mcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0583); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Leu-Cys]-Tle-Thr-NH2(PSM-0584); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Ala-Nmn-Cys]-Tle-Thr-NH2(PSM-0585); Ac-Thr-Aib-Trp-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH2(PSM-0587); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Trp-Cys]-Tle-Thr-NH2(PSM-0589); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-RMe2a-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0590): Macropa-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0591); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-RMe1-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0592); DOTAM-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0593); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-OH(PSM-0594); LSC-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0601); DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-en-H (PSM-0605) and DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Bal-NH2(PSM-0606) or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 182. The antibody 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, 47, 48, 49, 50, 51, 52, 53, or any combination thereof, which is capable of binding to PSMA. 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180 and 181, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 183. The method of any 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, 47, 48, 49, 50, 51, comprising a diagnostically active nuclide or a therapeutically active nuclide. 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163 07, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181 and 182, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 184. A compound of embodiment 183, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, comprising a diagnostically active nuclide. Embodiment 185. The compound of embodiment 184, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, wherein the diagnostically active nuclide is a diagnostically active radionuclide. Embodiment 186. The diagnostically active radionuclide is 43 Sc, 44 Sc, 51 Mn, 52 Mn, 64 Cu, 67 Ga,68 Ga, 86 Y, 89 Zr, 94m Tc, 99m Tc, 111 In, 152 Tb, 155 Tb, 177 Lu, 201 Tl, 203 Pb, 18 F, 76 Br, 77 Br, 123 I, 124 I and 125 I, or a pharmaceutically acceptable salt, solvate, or hydrate thereof. Embodiment 187. The diagnostically active radionuclide is 18 F, 43 Sc, 44 Sc, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 99m Tc, 111 In, 152 Tb, 155 Tb and 203 Pb, or a pharmaceutically acceptable salt, solvate, or hydrate thereof. Embodiment 188. The diagnostically active radionuclide is 18 F, 64 Cu, 68 Ga and 111 In, or a pharmaceutically acceptable salt, solvate, or hydrate thereof. Embodiment 189. The composition of any 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 200, 210, 2 5, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 1 09, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182 and 183, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 190. The compound of embodiment 189, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, wherein the therapeutically active nuclide is a therapeutically active radionuclide. Embodiment 191. The therapeutically active radionuclide is 47 Sc, 67 Cu, 89 Sr, 90 Y, 111 In, 153 Sm, 149 Tb, 161 Tb, 177 Lu, 186 Re, 188 Re,212 Pb, 212 Bi, 213 Bi, 223 Ra, 224 Ra, 225 Ac, 226 Th, 227 Th, 131 I and 211 191. The compound according to embodiment 190, or a pharmaceutically acceptable salt, solvate or hydrate thereof, selected from the group consisting of At. Embodiment 192. The therapeutically active radionuclide is 47 Sc, 67 Cu, 90 Y, 161 Tb, 177 Lu, 188 Re, 212 Pb, 212 Bi, 213 Bi, 225 Ac and 227 192. The compound of embodiment 191, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, selected from the group consisting of: Th. Embodiment 193. The therapeutically active radionuclide is 90 Y, 161 Tb, 177 Lu, 212 Pb, 225 Ac and 227 193. The compound of embodiment 192, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, selected from the group consisting of: Th. Embodiment 194. The method of any 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, 47, 48, 49, 50, 51, 52, 53, 54, for use in a method for the diagnosis of a disease. 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110 , 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 1 55, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187 and 188, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 195. The compound of any 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110 , 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 1 55, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 189, 190, 191, 192 and 193, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 196. The compound for use according to any one of embodiments 194 and 195, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the disease is a disease involving the prostate-specific membrane antigen (PSMA) protein. Embodiment 197. The compound for use according to any one of embodiments 194, 195 and 196, or its pharmaceutically acceptable salt, solvate or hydrate, wherein the disease involves diseased tissues containing cells that show upregulated expression of prostate-specific membrane antigen (PSMA), preferably cells that show upregulated expression of PSMA. Embodiment 198. The compound for use according to any one of embodiments 194, 195, 196 and 197, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the disease is a neoplasm, preferably a cancer or tumor. Embodiment 199. The compound for use according to embodiment 198, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the tumor is selected from the group comprising advanced tumors, metastatic tumors and primary tumors. Embodiment 200. The compound for use according to any one of embodiments 198 and 199, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the tumor is selected from the group comprising prostate tumor, metastatic prostate tumor, lung tumor, kidney tumor, glioblastoma, pancreatic tumor, bladder tumor, sarcoma, melanoma, breast tumor, colon tumor, pheochromocytoma, esophageal tumor, gastric tumor, carcinoma, squamous cell carcinoma (e.g., cervix, eyelid, conjunctiva, vagina, lung, oral cavity, skin, bladder, tongue, larynx and esophagus), and adenocarcinoma (e.g., prostate, small intestine, endometrium, cervix, large intestine, lung, pancreas, esophagus, rectum, uterus, stomach, breast and ovary), and combinations thereof. Embodiment 201. The compound for use according to embodiment 200, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the tumor is a prostate tumor or a metastatic prostate tumor. Embodiment 202. The cancer is prostate cancer (e.g., metastatic castration-resistant prostate cancer), kidney cancer (e.g., clear cell carcinoma), head cancer, neck cancer, head and neck cancer, lung cancer (e.g., non-small cell lung cancer), salivary gland cancer, breast cancer, colorectal cancer, esophageal cancer, gastric cancer, liver cancer (e.g., hepatocellular carcinoma), thyroid cancer, glioblastoma, glioma, gallbladder cancer, laryngeal cancer, leukemia / lymphoma, uterine cancer, skin cancer (e.g., melanoma), endocrine cancer, sarcoma, urinary cancer, pancreatic cancer. 199. The compound for use according to embodiment 198, or a pharmaceutically acceptable salt, solvate or hydrate thereof, selected from the group comprising cancer, gastrointestinal cancer, ovarian cancer, cervical cancer, endometrial cancer, fallopian tube cancer, primary peritoneal cancer, blood cancer (e.g., diffuse large B-cell lymphoma, Hodgkin's lymphoma, non-Hodgkin's lymphoma, follicular lymphoma, acute myeloid leukemia or multiple myeloma), cancer of unknown primary, adenoma and tumor angiogenesis. Embodiment 203. The compound for use according to embodiment 202, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the cancer is prostate cancer. Embodiment 204. The compound for use according to any one of embodiments 194, 196, 197, 198, 199, 200, 201, 202, and 203, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, comprising a diagnostically active nuclide, preferably a diagnostically active radionuclide. Embodiment 205. The diagnostically active nuclide is 43 Sc, 44 Sc, 51 Mn, 52 Mn, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 94m Tc, 99m Tc, 111 In, 152 Tb, 155 Tb, 177 Lu, 201 Tl, 203 Pb, 18 F, 76 Br, 77 Br, 123 I, 124 I, 125I, preferably 18 F, 43 Sc, 44 Sc, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 99m Tc, 111 In, 152 Tb, 155 Tb, 203 Pb, more preferably 18 F, 64 Cu, 68 Ga and 111 The compound for use according to embodiment 204, or a pharmaceutically acceptable salt, solvate or hydrate thereof, selected from the group comprising In. Embodiment 206. The compound for use according to any one of embodiments 194 and 196, 197, 198, 199, 200, 201, 202, 203, 204 and 205, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the method for diagnosis is an imaging method. Embodiment 207. The compound for use according to embodiment 206, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the imaging method is selected from the group consisting of scintigraphy, single photon emission computed tomography (SPECT), positron emission tomography (PET), SPECT / computed tomography, PET / computed tomography, and combinations thereof. Embodiment 208. The compound for use according to any one of embodiments 194, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, and 207, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, wherein the method comprises administering a diagnostically effective amount of the compound to a subject, preferably a mammal, wherein the mammal is selected from the group comprising mankind, companion animals, pets, and livestock, more preferably the subject is selected from the group comprising mankind, dogs, cats, horses, and cattle, and most preferably the subject is a human. Embodiment 209. The compound for use according to any one of embodiments 195, 196, 197, 198, 199, 200, 201, 202 and 203, or a pharmaceutically acceptable salt, solvate or hydrate thereof, comprising a therapeutically active nuclide, preferably a therapeutically active radionuclide. Embodiment 210. The therapeutically active radionuclide is 47 Sc, 67 Cu, 89 Sr, 90 Y, 111 In, 153 Sm, 149 Tb, 161 Tb, 177 Lu, 186 Re, 188 Re, 212 Pb, 212 Bi, 213 Bi, 223 Ra, 224 Ra, 225 Ac, 226 Th, 227 Th, 131 I, 211 At, preferably 47 Sc, 67 Cu, 90 Y, 161 Tb, 177 Lu, 188 Re, 212 Pb, 212 Bi, 213 Bi, 225 Ac, 227 Th, more preferably 90 Y, 161 Tb, 177 Lu, 212 Pb, 225 Ac and 227 The compound for use according to embodiment 209, or a pharmaceutically acceptable salt, solvate or hydrate thereof, selected from the group comprising Th. Embodiment 211. The compound for use according to any one of embodiments 195, 196, 197, 198, 199, 200, 201, 202, 203, 209 and 210, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the method comprises administering a therapeutically effective amount of the compound to a subject, preferably a mammal, wherein the mammal is selected from the group comprising mankind, companion animals, pets and livestock, more preferably the subject is selected from the group comprising mankind, dogs, cats, horses and cattle, and most preferably the subject is a human. Embodiment 212. The compound, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, is for use in a method for identifying a subject, wherein the subject is likely to respond or not likely to respond to treatment of a disease, and the method for identifying a subject is any 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111 9, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90 , 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 204 and 205, or a pharmaceutically acceptable salt, solvate or hydrate thereof, preferably comprising performing a method for the diagnosis of a disease described in any one of embodiments 194, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207 and 208.26, 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, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 8, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184 23, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162 2, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 204 and 205, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 213. The compound, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, is for use in a method for selecting a subject from a group of subjects, wherein the subject is likely to respond or is unlikely to respond to treatment of a disease, and the method for selecting a subject from a group of subjects is any 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109 5, 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, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86 , 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 204 and 205, or a pharmaceutically acceptable salt, solvate or hydrate thereof, preferably comprising performing a method for the diagnosis of a disease described in any one of embodiments 194, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207 and 208.22, 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, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139 5, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121 , 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161 , 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 204 and 205, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 214. The compound, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, is for use in a method for stratifying a group of subjects into those likely to respond to treatment of a disease and into those unlikely to respond to treatment of a disease, wherein the method for stratifying a group of subjects is any 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107 7, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121 1, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 1 2, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 2 201, 202, 203, 204, 205, 206, 207, and 208, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, preferably comprising performing a method for the diagnosis of a disease described in 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 204, and 205, or a pharmaceutically acceptable salt, solvate, or hydrate thereof. Embodiment 215. The compound for use according to any one of embodiments 212, 213 and 214, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the disease is a disease involving the prostate-specific membrane antigen (PSMA) protein. Embodiment 216. The compound for use according to any one of embodiments 212, 213, 214 and 215, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the disease involves cells that exhibit upregulated expression of prostate-specific membrane antigen (PSMA). Embodiment 217. The compound for use according to any one of embodiments 212, 213, 214, 215 and 216, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the disease is a neoplasm, preferably a cancer or tumor. Embodiment 218. The compound for use according to embodiment 217, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the tumor is selected from the group comprising prostate tumor, metastatic prostate tumor, lung tumor, kidney tumor, glioblastoma, pancreatic tumor, bladder tumor, sarcoma, melanoma, breast tumor, colon tumor, pheochromocytoma, esophageal tumor, gastric tumor, carcinoma, squamous cell carcinoma (e.g., cervix, eyelid, conjunctiva, vagina, lung, oral cavity, skin, bladder, tongue, larynx and esophagus), and adenocarcinoma (e.g., prostate, small intestine, endometrium, cervix, large intestine, lung, pancreas, esophagus, rectum, uterus, stomach, breast and ovary), and combinations thereof. Embodiment 219. The compound for use according to embodiment 218, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the tumor is a prostate tumor or a metastatic prostate tumor. Embodiment 220. The neoplasms, cancers and tumors are each and individually prostate cancer (e.g., metastatic castration-resistant prostate cancer), renal cancer (e.g., clear cell carcinoma), head cancer, neck cancer, head and neck cancer, lung cancer (e.g., non-small cell lung cancer), salivary gland cancer, breast cancer, colorectal cancer, esophageal cancer, gastric cancer, liver cancer (e.g., hepatocellular carcinoma), thyroid cancer, glioblastoma, glioma, gallbladder cancer, laryngeal cancer, leukemia / lymphoma, uterine cancer, skin cancer (e.g., melanoma), endocrine cancer, sarcoma. , urinary cancer, pancreatic cancer, gastrointestinal cancer, ovarian cancer, cervical cancer, endometrial cancer, fallopian tube cancer, primary peritoneal cancer, blood cancer (e.g., diffuse large B-cell lymphoma, Hodgkin's lymphoma, non-Hodgkin's lymphoma, follicular lymphoma, acute myeloid leukemia or multiple myeloma), cancer of unknown primary, adenoma and tumor angiogenesis, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 221. The compound for use according to embodiment 220, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the cancer is prostate cancer. Embodiment 222. The compound for use according to any one of embodiments 212, 213, 214, 215, 216, 217, 218, 219, 220, and 221, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, wherein the method of diagnosis is an imaging method. Embodiment 223. The compound for use according to embodiment 222, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the imaging method is selected from the group comprising scintigraphy, single photon emission computed tomography (SPECT), positron emission tomography (PET), SPECT / computed tomography, PET / computed tomography, and combinations thereof, and combinations thereof. Embodiment 224. The compound for use according to any one of embodiments 212, 213, 214, 215, 216, 217, 218, 219, 220, and 221, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, comprising a diagnostically active nuclide, preferably a diagnostically active radionuclide. Embodiment 225. The diagnostically active nuclide is 43 Sc, 44 Sc, 51 Mn, 52 Mn, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 94m Tc, 99m Tc, 111 In, 152 Tb, 155 Tb, 177 Lu, 201 Tl, 203 Pb, 18 F, 76 Br, 77 Br, 123 I, 124 I and 125 I, preferably 18 F, 43 Sc, 44 Sc, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 99m Tc,111 In, 152 Tb, 155 Tb and 203 Pb, more preferably 18 F, 64 Cu, 68 Ga and 111 The compound for use according to embodiment 224, selected from the group comprising In, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 226. The compound of any 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 1 45, 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, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110 7, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 1 56, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192 and 193, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 227. The diagnostically active radionuclide is 43 Sc, 44 Sc, 51 Mn, 52 Mn, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 94m Tc, 99m Tc, 111 In, 152 Tb, 155 Tb, 177 Lu, 201 Tl, 203 Pb, 18 F, 76 Br, 77 Br, 123 I, 124 I and 125 I, preferably 18 F, 43 Sc, 44 Sc, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 99m Tc, 111 In, 152 Tb, 155 Tb and 203 Pb, more preferably 18 F, 64 Cu, 68 Ga and 111 In, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 228. The therapeutically active radionuclide is 47 Sc, 67 Cu, 89 Sr, 90 Y, 111 In, 153 Sm, 149 Tb, 161 Tb, 177 Lu, 186 Re, 188 Re, 212 Pb, 212 Bi, 213Bi, 223 Ra, 224 Ra, 225 Ac, 226 Th, 227 Th, 131 I, 211 At, preferably 47 Sc, 67 Cu, 90 Y, 161 Tb, 177 Lu, 188 Re, 212 Pb, 212 Bi, 213 Bi, 225 Ac, 227 Th, more preferably 90 Y, 161 Tb, 177 Lu, 212 Pb, 225 Ac and 227 227. The compound for use according to embodiment 226, selected from the group consisting of Th, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 229. The compound for use according to any one of embodiments 226 to 228, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein prostate-specific membrane antigen (PSMA) is expressed by cells, preferably prostate cells, metastatic prostate cells, lung cells, kidney cells, pancreatic cells, bladder cells, breast cells, colon cells, germ cells, esophageal cells, stomach cells, endothelial cells, and combinations thereof, each of which exhibits upregulated expression of PSMA. Embodiment 230. The compound or a pharmaceutically acceptable salt, solvate or hydrate thereof for use according to embodiment 229, wherein the cell is contained in or is part of a tissue, preferably a diseased tissue of a subject suffering from a disease. Embodiment 231. The compound or a pharmaceutically acceptable salt, solvate or hydrate thereof for use according to embodiment 230, wherein the disease involves cells that exhibit upregulated expression of PSMA, preferably diseased tissue containing cells that exhibit upregulated expression of PSMA. Embodiment 232. The compound for use according to any one of embodiments 230 and 231, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the disease is a neoplasm, preferably a cancer or tumor. Embodiment 233. The compound for use according to embodiment 232, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the tumor is selected from the group comprising prostate tumor, metastatic prostate tumor, lung tumor, kidney tumor, glioblastoma, pancreatic tumor, bladder tumor, sarcoma, melanoma, breast tumor, colon tumor, pheochromocytoma, esophageal tumor, gastric tumor, carcinoma, squamous cell carcinoma (e.g., cervix, eyelid, conjunctiva, vagina, lung, oral cavity, skin, bladder, tongue, larynx and esophagus), and adenocarcinoma (e.g., prostate, small intestine, endometrium, cervix, large intestine, lung, pancreas, esophagus, rectum, uterus, stomach, breast and ovary), and combinations thereof. Embodiment 234. The cancer is prostate cancer (e.g., metastatic castration-resistant prostate cancer), kidney cancer (e.g., clear cell carcinoma), head cancer, neck cancer, head and neck cancer, lung cancer (e.g., non-small cell lung cancer), salivary gland cancer, breast cancer, colorectal cancer, esophageal cancer, gastric cancer, liver cancer (e.g., hepatocellular carcinoma), thyroid cancer, glioblastoma, glioma, gallbladder cancer, laryngeal cancer, leukemia / lymphoma, uterine cancer, skin cancer (e.g., melanoma), endocrine cancer, sarcoma, urinary cancer, pancreatic cancer. 233. The compound for use according to embodiment 232, or a pharmaceutically acceptable salt, solvate or hydrate thereof, selected from the group comprising cancer, gastrointestinal cancer, ovarian cancer, cervical cancer, endometrial cancer, fallopian tube cancer, primary peritoneal cancer, blood cancer (e.g., diffuse large B-cell lymphoma, Hodgkin's lymphoma, non-Hodgkin's lymphoma, follicular lymphoma, acute myeloid leukemia or multiple myeloma), cancer of unknown primary, adenoma and tumor angiogenesis. Embodiment 235. The diagnostically active nuclide is 18 F, wherein the diagnostically active nuclide is bound to aluminum, the aluminum is bound to a chelator, and 18 The compound of any one of embodiments 186-188, 205, 225, and 227, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, which is attached to F. Embodiment 236. 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 205, 210, 224, 225, 227 and 228, or a pharmaceutically acceptable salt, solvate or hydrate thereof, and a pharmaceutically acceptable excipient, preferably a pharmaceutical composition. Embodiment 237. The composition of embodiment 236 for use in any method defined in any of the preceding embodiments. Embodiment 238. A method for diagnosis of a disease in a subject, comprising administering to the subject a diagnostically effective amount of any 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 1 2, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110 , 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187 and 188, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 239. The method of embodiment 238, wherein the compound, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, comprises a diagnostically active nuclide, wherein the nuclide is preferably a diagnostically active radionuclide. Embodiment 240. A method for treating a disease in a subject, comprising administering to the subject a therapeutically effective amount of any 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 11 2, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155 , 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 189, 190, 191, 192 and 193, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 241. The method of embodiment 240, wherein the compound, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, comprises a therapeutically active nuclide, wherein the nuclide is preferably a therapeutically active radionuclide. Embodiment 242. The method of any one of embodiments 238, 239, 240, and 241, wherein the disease is a disease involving the prostate-specific membrane antigen (PSMA) protein. Embodiment 243. The method of any one of embodiments 238, 239, 240, 241 and 242, wherein the disease involves diseased tissue containing cells that exhibit upregulated expression of prostate-specific membrane antigen (PSMA), preferably cells that exhibit upregulated expression of PSMA. Embodiment 244. 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, 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 , 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 3, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186 , 187, 188, 189, 190, 191, 192, 193, 205, 210, 224, 225, 227 and 228, or a pharmaceutically acceptable salt, solvate or hydrate thereof, and optionally one or more excipients, and optionally one or more devices, wherein the device is selected from the group consisting of a labeling device, a purification device, a manipulation device, a radiation protection device, an analytical device or an administration device. Embodiment 245. The kit of embodiment 244 for use in any method defined in any of the preceding embodiments. Embodiment 246. Any 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, 47, 48, 49, 50 in the manufacture of or for the manufacture of a medicament, preferably a medicament for the treatment of a disease disclosed herein. , 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 1 11, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 209, 2010, 2011, 2012, 2013, 2014, 2015, 2016, 2017, 2018, 20 9, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194 and 195, or a pharmaceutically acceptable salt, solvate or hydrate thereof. Embodiment 247. Any 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, 47, 48, 49 in the manufacture of or for the manufacture of a diagnostic means, preferably a diagnostic means for the diagnosis of a disease disclosed herein. , 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110 , 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 1 192, 193, 194 and 195, or a pharmaceutically acceptable salt, solvate or hydrate thereof.

[0119] It will be recognized by one of ordinary skill in the art that a compound of the present disclosure is any compound disclosed herein, including, but not limited to, any compound described in any of the above embodiments and any of the following embodiments.

[0120] It will be recognized by one of ordinary skill in the art that a method of the present disclosure is any method disclosed herein, including, but not limited to, any method described in any of the above embodiments and any of the following embodiments.

[0121] It will be recognized by one of ordinary skill in the art that a composition of the present disclosure is any composition disclosed herein, including, but not limited to, any composition described in any of the above embodiments and any of the following embodiments.

[0122] It will be recognized by one of skill in the art that a kit of the present disclosure is any kit disclosed herein, including, but not limited to, any kit described in any of the above embodiments and any of the following embodiments.

[0123] It will be appreciated by those skilled in the art that the phrase "aspects of the disclosure" is used synonymously with the terms "aspects of the invention" and, respectively, "aspects of the present invention," and that the phrase "embodiments of the disclosure" is used synonymously with the terms "embodiments of the invention" and, respectively, "embodiments of the present invention."

[0124] Unless otherwise indicated, all numerical values ​​expressing quantities, states, or other amounts used in this disclosure should be understood to be modified in all instances by the term "about." Accordingly, unless indicated to the contrary, the numerical parameters set forth in this disclosure are approximations that may vary depending upon the desired properties sought to be obtained by the present disclosure. At the very least, and not as an attempt to limit the application of the doctrine of equivalents, each numerical parameter should be construed in light of the number of significant digits and ordinary rounding practices.

[0125] Additionally, disclosure of numerical ranges within this disclosure is considered to be a disclosure of all numerical values ​​and ranges within that range. For example, if a range is 1 to 10, it is considered to include, for example, 1, 2, 2.2, 3, 4, 5, 6, 7, 7.4, 7.6, 8, 8.7, 9, 9.5, 10, or any other value or range (integer or non-integer) within the range. Furthermore, as used herein, the term "at least" includes the indicated numerical value, for example, "at least 50" includes 50.

[0126] The term alkyl, as preferably used herein, refers, each and individually, to a saturated straight-chain or branched-chain hydrocarbon group, usually accompanied by a modifier specifying the number of carbon atoms it may contain. For example, the term (C1-C6) alkyl, each and individually, refers to any of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 1-methylbutyl, 1-ethylpropyl, 3-methylbutyl, 1,2-dimethylpropyl, 2-methylbutyl, 1,1-dimethylpropyl, 2,2-dimethylpropyl, n-hexyl, 1,1-dimethylbutyl, and any other isoform of an alkyl group containing 6 saturated carbon atoms.

[0127] In one embodiment, and as preferably used herein, "(C1-C2) alkyl" each and individually refers to either methyl or ethyl. In one embodiment, and as preferably used herein, "(C1-C3) alkyl" each and individually means any of methyl, ethyl, n-propyl, and isopropyl.

[0128] In one embodiment, and as preferably used herein, "(C1-C4) alkyl" each and individually means any of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, and tert-butyl.

[0129] In one embodiment, and as preferably used herein, "(C1-C6) alkyl" each and individually includes methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2-methyl-butyl, 3-methyl-butyl, 3-pentyl, 3-methyl-but-2-yl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-hexyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2,2-dimethylpropyl, n-methyl-but-2- ...

[0033] In the present invention, the aryl group represents any of the following: ethyl-pentyl, 3-methyl-pentyl, 4-methyl-pentyl, 3-hexyl, 2-ethyl-butyl, 2-methyl-pent-2-yl, 2,2-dimethyl-butyl, 3,3-dimethyl-butyl, 3-methyl-pent-2-yl, 4-methyl-pent-2-yl, 2,3-dimethyl-butyl, 3-methyl-pent-3-yl, 2-methyl-pent-3-yl, 2,3-dimethyl-but-2-yl and 3,3-dimethyl-but-2-yl.

[0130] In one embodiment, and as preferably used herein, "(C1-C8) alkyl" refers to a saturated or unsaturated, straight-chain or branched-chain hydrocarbon group having 1 to 8 carbon atoms. Representative (C1-C8) alkyl groups include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2-methylbutyl, 3-methylbutyl, 3-pentyl, 3-methylbut-2-yl, 2-methylbut-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-hexyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, and the like. yl, 3-hexyl, 2-ethyl-butyl, 2-methyl-pent-2-yl, 2,2-dimethyl-butyl, 3,3-dimethyl-butyl, 3-methyl-pent-2-yl, 4-methyl-pent-2-yl, 2,3-dimethyl-butyl, 3-methyl-pent-3-yl, 2-methyl-pent-3-yl, 2,3-dimethyl-but-2-yl, 3,3-dimethyl-but-2-yl, n-heptyl, 2-heptyl, 2-methyl-hexyl, 3-methyl -hexyl, 4-methyl-hexyl, 5-methyl-hexyl, 3-heptyl, 2-ethyl-pentyl, 3-ethyl-pentyl, 4-heptyl, 2-methyl-hex-2-yl, 2,2-dimethyl-pentyl, 3,3-dimethyl-pentyl, 4,4-dimethyl-pentyl, 3-methyl-hex-2-yl, 4-methyl-hex-2-yl, 5-methyl-hex-2-yl, 2,3-dimethyl-pentyl, 2,4-dimethyl-pentyl, 3, 4-Dimethyl-pentyl, 3-methyl-hex-3-yl, 2-ethyl-2-methyl-butyl, 4-methyl-hex-3-yl, 5-methyl-hex-3-yl, 2-ethyl-3-methyl-butyl, 2,3-dimethyl-pent-2-yl, 2,4-dimethyl-pent-2-yl, 3,3-dimethyl-pent-2-yl, 4,4-dimethyl-pent-2-yl, 2,2,3-trimethyl-butyl, 2,3,3-trimethyl-butyl, 2,3,3-trimethyl-but-2-yl, n-octyl, 2-octyl, 2-methyl-heptyl, 3-methyl-heptyl, 4-methyl-heptyl, 5-methyl-heptyl, 6-methyl-heptyl, 3-octyl, 2-ethyl-hexyl, 3-ethyl-hexyl, 4-ethyl-hexyl, 4-octyl, 2-propyl-pentyl, 2-methyl-hept-2-yl, 2,2-dimethyl-hexyl, 3,3-dimethyl-hexyl, 4,4-dimethyl-hexyl, 5,5-dimethyl-hexyl, 3-methyl-hept-2-yl, 4-methyl-hept-2-yl, 5 -Methyl-hept-2-yl, 6-methyl-hept-2-yl, 2,3-dimethyl-hex-1-yl, 2,4-dimethyl-hex-1-yl, 2,5-dimethyl-hex-1-yl, 3,4-dimethyl-hex-1-yl, 3,5-dimethyl-hex-1-yl, 3,5-dimethyl-hex-1-yl, 3-methyl-hept-3-yl, 2-ethyl-2-methyl-1-yl, 3-ethyl-3-methyl-1-yl, 4-methyl-hept-3-yl, 5-methyl-hept-3-yl, 6-methyl-hept-3-yl, 2-ethyl-3-methyl-pentyl , 2-ethyl-4-methyl-pentyl, 3-ethyl-4-methyl-pentyl, 2,3-dimethyl-hex-2-yl, 2,4-dimethyl-hex-2-yl, 2,5-dimethyl-hex-2-yl, 3,3-dimethyl-hex-2-yl, 3,4-dimethyl-hex-2-yl, 3,5-dimethyl-hex-2-yl, 4,4-dimethyl-hex-2-yl, 4,5-dimethyl-hex-2-yl, 5,5-dimethyl-hex-2-yl, 2,2,3-trimethyl-pentyl, 2,2,4-trimethyl-pentyl, 2,3,3-trimethyl-pentyl butyl, 2,3,4-trimethylpentyl, 2,4,4-trimethylpentyl, 3,3,4-trimethylpentyl, 3,4,4-trimethylpentyl, 2,3,3-trimethylpent-2-yl, 2,3,4-trimethylpent-2-yl, 2,4,4-trimethylpent-2-yl, 3,4,4-trimethylpent-2-yl, 2,2,3,3-tetramethylbutyl, 3,4-dimethylhex-3-yl, 3,5-dimethylhex-3-yl, 4,4-dimethylhex-3-yl, 4,5-dimethylhex-3-yl, 5,Examples of aryl esters include, but are not limited to, 5-dimethyl-hex-3-yl, 3-ethyl-3-methyl-pent-2-yl, 3-ethyl-4-methyl-pent-2-yl, 3-ethyl-hex-3-yl, 2,2-diethyl-butyl, 3-ethyl-3-methyl-pentyl, 4-ethyl-hex-3-yl, 5-methyl-hept-3-yl, 2-ethyl-3-methyl-pentyl, 4-methyl-hept-4-yl, 3-methyl-hept-4-yl, 2-methyl-hept-4-yl, 3-ethyl-hex-2-yl, 2-ethyl-2-methyl-pentyl, 2-isopropyl-pentyl, 2,2-dimethyl-hex-3-yl, 2,2,4-trimethyl-pent-3-yl and 2-ethyl-3-methyl-pentyl. The (C1-C8) alkyl group may be unsubstituted or substituted with one or more groups including, but not limited to, (C1-C8) alkyl, -O-[(C1-C8) alkyl], -aryl, -CO-R', -O-CO-R', -CO-OR', -CO-NH, -CO-NHR', -CO-NR', -NH-CO-R', -SO2-R', -SO-R', -OH, -halogen, -N3, -NH, -NHR', -NR'2, and -CN; where each R' is independently selected from -(C1-C8) alkyl and aryl.

[0131] In one embodiment, and as preferably used herein, "(2C2-C6) alkyl" refers to, each and individually, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2-methyl-butyl, 3-methyl-butyl, 3-pentyl, 3-methyl-but-2-yl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-hexyl, 2-methyl -pentyl, 3-methyl-pentyl, 4-methyl-pentyl, 3-hexyl, 2-ethyl-butyl, 2-methyl-pent-2-yl, 2,2-dimethyl-butyl, 3,3-dimethyl-butyl, 3-methyl-pent-2-yl, 4-methyl-pent-2-yl, 2,3-dimethyl-butyl, 3-methyl-pent-3-yl, 2-methyl-pent-3-yl, 2,3-dimethyl-but-2-yl and 3,3-dimethyl-but-2-yl.

[0132] In one embodiment, and as preferably used herein, "(C4-C6) alkyl" refers to any of the following alkyl groups: n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2-methyl-butyl, 3-methyl-butyl, 3-pentyl, 3-methyl-but-2-yl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-hexyl, 2-methyl-pentyl, 3-methyl-but-2-yl, 2,2-dimethylpropyl, n-hexyl, 2-hexyl, 2-methyl-pentyl, 3-methyl-but-2-yl, 2,2-dimethylpropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2 ...butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-methyl-but-2-yl, 2,2-dimethylpropyl, n-butyl, iso

[0033] In the present invention, the aryl group represents any of the following: ethyl-pentyl, 4-methyl-pentyl, 3-hexyl, 2-ethyl-butyl, 2-methyl-pent-2-yl, 2,2-dimethyl-butyl, 3,3-dimethyl-butyl, 3-methyl-pent-2-yl, 4-methyl-pent-2-yl, 2,3-dimethyl-butyl, 3-methyl-pent-3-yl, 2-methyl-pent-3-yl, 2,3-dimethyl-but-2-yl and 3,3-dimethyl-but-2-yl.

[0133] In one embodiment, and as preferably used herein, "carbocycle" refers to a saturated, unsaturated, or aromatic monocyclic or bicyclic carbocyclic ring. The carbocycle may be unsubstituted or substituted with one or more groups including, but not limited to, (C1-C8) alkyl, -O-[(C1-C8) alkyl], -aryl, -CO-R', -O-CO-R', -CO-OR', -CO-NH, -CO-NHR', -CO-NR'2, -NH-CO-R', -SO2-R', -SO-R', -OH, -halogen, -N3, -NH2, -NHR', -NR'2, and -CN; where each R' is independently selected from -(C1-C8) alkyl and aryl.

[0134] In one embodiment, and as preferably used herein, "heterocycle" refers to a saturated, unsaturated, or aromatic monocyclic or bicyclic heterocyclic ring. The heterocyclic group may be unsubstituted or substituted with one or more groups, including but not limited to, (C1-C8) alkyl, -O-[(C1-C8) alkyl], -aryl, -CO-R', -O-CO-R', -CO-OR', -CO-NH, -CO-NHR', -CO-NR'2, -NH-CO-R', -SO2-R', -SO-R', -OH, -halogen, -N3, -NH2, -NHR', -NR'2, and -CN; where each R' is independently selected from -(C1-C8) alkyl and aryl.

[0135] In one embodiment, and as preferably used herein, "aryl" refers to a carbocyclic aromatic group. Examples of aryl groups include, but are not limited to, phenyl, naphthyl, and anthracenyl.

[0136] In one embodiment, and as preferably used herein, "heteroaryl" refers to a heterocyclic aromatic group. Examples of heteroaryl groups include, but are not limited to, furan, thiophene, pyridine, pyrimidine, benzothiophene, benzofuran, and quinoline.

[0137] In one embodiment, and as preferably used herein, "(C5-C6)heteroaryl" refers to a heteroaromatic group consisting of 5 or 6 ring atoms, where at least one atom is different from carbon and includes, for example, nitrogen, sulfur, or oxygen. The heteroaromatic group can be unsubstituted or substituted with one or more groups, including, but not limited to, -(C1-C8)alkyl, -O-[(C1-C8)alkyl], -aryl, -CO-R', -O-CO-R', -CO-OR', -CO-NH2, -CO-NHR', -CO-NR'2, -NH-CO-R', -SO2-R', -SO-R', -OH, -halogen, -N3, -NH2, -NHR', -NR'2, and -CN; where each R' is independently selected from -(C1-C8)alkyl and aryl.

[0138] In one embodiment, and as preferably used herein, "amino acid residue" refers to all atoms of an amino acid that remain after combination of said amino acid with other amino acids in a peptide chain.

[0139] In one embodiment, and as preferably used herein, a "side chain" refers to all atoms of an amino acid residue that are not included in the "main chain" portion of the amino acid residue. A "main chain" refers to the structure formed by the consecutive connection of amino acids, whereby the α-nitrogen atom of an α-amino acid, the β-nitrogen atom of a β-amino acid, the γ-nitrogen of a γ-amino acid residue, the δ-nitrogen atom of a δ-amino acid, the ε-nitrogen of an ε-amino acid, or the ω-nitrogen of an ω-amino acid is connected to the C-1 carbonyl atom of the amino acid.

[0140] In one embodiment, and as preferably used herein, the atom with unspecified atomic mass number in any structural formula or in any part of this specification is either unspecified isotopic composition, mixture of naturally occurring isotopes, or individual isotopes.This applies particularly to carbon, oxygen, nitrogen, sulfur, phosphorus, halogen and metal atoms, including but not limited to C, O, N, S, F, P, Cl, Br, At, Sc, Cr, Mn, Co, Fe, Cu, Ga, Sr, Zr, Y, Mo, Tc, Ru, Rh, Pd, Pt, Ag, In, Sb, Sn, Te, I, Pr, Pm, Dy, Sm, Gd, Tb, Ho, Dy, Er, Yb, Tm, Lu, Sn, Re, Rd, Os, Ir, Au, Pb, Bi, Po, Fr, Ra, Ac, Th and Fm.

[0141] In one embodiment, and as preferably used herein, a "chelator" is a compound capable of forming a chelate, where the chelate is, for example, a compound including a cyclic compound in which a metal or moiety having an electron gap or an unshared electron pair participates in forming a ring. In certain embodiments, the chelator is a class of compounds in which a single ligand occupies two or more coordination sites at a central atom.

[0142] In one embodiment, and as preferably used herein, a "diagnostically active compound" is a compound that is at least suitable for or useful in diagnosing a disease.

[0143] In one embodiment, and as preferably used herein, a "diagnostic agent" or "diagnostically active agent" is a compound that is at least suitable for or useful in diagnosing a disease.

[0144] In one embodiment, and as preferably used herein, a "diagnostically active radionuclide" is a radionuclide that is suitable or useful in at least diagnosing disease. However, it will also be recognized by those skilled in the art that the use of said diagnostically active radionuclide may not be limited to diagnostic purposes, but may include their use in therapy and theragnostics.

[0145] In one embodiment, and as preferably used herein, a "therapeutically active compound" is a compound that is at least suitable for or useful in the treatment of a disease.

[0146] In one embodiment, and as preferably used herein, a "therapeutic agent" or "therapeutically active agent" is at least a compound suitable for or useful in the treatment of a disease.

[0147] In one embodiment, and as preferably used herein, a "therapeutically active radionuclide" is a radionuclide that is suitable for or useful in treating at least a disease. However, it will also be recognized by those skilled in the art that the use of said therapeutically active radionuclide may not be limited to therapeutic purposes, but may include their use in diagnosis and theragnostics.

[0148] In one embodiment, and as preferably used herein, a "theragnostically active compound" is a compound suitable for or useful in both the diagnosis and treatment of disease.

[0149] In one embodiment, and as preferably used herein, a "theragnostic agent" or "theragnostically active agent" is a compound suitable for or useful in both the diagnosis and treatment of disease.

[0150] In one embodiment, and as preferably used herein, a "theragnostically active radionuclide" is a radionuclide that is suitable for or useful in both the diagnosis and treatment of disease.

[0151] In one embodiment, and as preferably used herein, "theragnostics" refers to a method for the combined diagnosis and treatment of disease. In certain embodiments, the combined diagnostically and therapeutically active compounds used in theragnostics are radiolabeled.

[0152] In one embodiment, and as preferably used herein, "treatment of a disease" refers to the treatment and / or prevention of a disease. In one embodiment, and as preferably used herein, the terms "treat," "treating," and "treatment" are meant to include alleviating or arresting a disorder, disease, or condition; or one or more symptoms associated with a disorder, disease, or condition; or alleviating or eradicating the cause of the disorder, disease, or condition itself.

[0153] In one embodiment, and as preferably used herein, "preventing" or "prevent" describes reducing or eliminating the onset of symptoms or complications of a disease, condition, or disorder.

[0154] In one embodiment, and as preferably used herein, the term "subject" or "patient" includes a mammal. The mammal can be, for example, any mammal, such as a human, companion animal, pet, livestock, dog, cat, horse, and cow.

[0155] In one embodiment, and as preferably used herein, a "disease involving prostate-specific membrane antigen (PSMA) protein" is a disease involving cells that exhibit upregulated expression of PSMA, which is one of or the cause of the disease and / or symptoms of the disease, or is part of the underlying pathology of the disease.

[0156] In one embodiment, and as preferably used herein, a "target cell" or "target tissue" is a cell or tissue that expresses prostate-specific membrane antigen (PSMA) and is one of or responsible for a disease and / or symptoms of a disease, or is part of the underlying pathology of a disease.

[0157] In one embodiment, and as preferably used herein, a "non-target cell" or "non-target tissue" is a cell or tissue that does not express prostate-specific membrane antigen (PSMA) and / or is not one of or responsible for the disease and / or symptoms of the disease, or is part of the underlying pathology of the disease.

[0158] In one embodiment, and as preferably used herein, a "neoplasm" is an abnormal new growth of cells. Cells in a neoplasm grow more rapidly than normal cells and continue to grow unless treated. Neoplasms can be benign or malignant.

[0159] In one embodiment, and as preferably used herein, a "tumor" is a large lesion that can be benign or malignant. In one embodiment, and as preferably used herein, "cancer" refers to a malignant neoplasm.

[0160] In one embodiment, and as preferably used herein, "pharmaceutically acceptable excipient" refers to an ingredient other than an active agent and / or compound that is suitable for use in a pharmaceutical composition, including, but not limited to, pharmaceutically acceptable adjuvants, diluents, carriers, buffers, binders, colorants, lubricants, fillers, disintegrants, preservatives, surfactants, and stabilizers.

[0161] In one embodiment, the disclosed compounds, and compounds that are the subject of the embodiments disclosed herein, include pharmaceutically acceptable salts of such compounds, solvates of such compounds, or hydrates of such compounds.

[0162] In one embodiment, and as preferably used herein, a "linkage" refers to the bonding of two atoms of two independent moieties. A preferred linkage is a chemical bond or multiple chemical bonds. Preferably, the chemical bond is a covalent bond or multiple chemical bonds. Preferably, the linkage is a covalent bond or a coordinate bond. As preferably used herein, a coordinate bond embodiment refers to a bond or group of bonds, such as those realized when a metal is bound by a chelator. Depending on the type of atoms being linked and their atomic environment, various types of linkages are created. These types of linkages are defined by the type of atomic arrangement created by the linkage. For example, the linkage of an amine-containing moiety to a carboxylic acid-containing moiety results in a linkage designated as an amide (also referred to as an amide linkage, -CO-N-, -N-CO-). It will be recognized by those skilled in the art that this and the following examples of creating linkages are merely prototypical examples and in no way limit the scope of this application. Those skilled in the art will recognize that linking an isothiocyanate-containing moiety to an amine-containing moiety results in a thiourea (also referred to as a thiourea linkage, -N-CS-N-), and linking a C-atom-containing moiety to a thiol group (-C-SH) results in a thioether (also referred to as a thioether linkage, -CSC). A non-limiting list of exemplary linkages used in connecting chelators to the remainder of the compounds of the present disclosure, and their characteristic types of atomic arrangements, is shown in Table 1.

[0163] [Table 1]

[0164] In some embodiments of the present disclosure, examples of reactive groups used in forming a linkage between a chelator and the remainder of a compound of the present disclosure are summarized in Table 2. However, it will be understood by one of skill in the art that neither the linkage for forming a compound of the present disclosure nor the reactive group forming such a linkage is limited to one in Table 2.

[0165] [Table 2]

[0166] In one embodiment, and as preferably used herein, the term "activated carboxylic acid" refers to a carboxylic acid group having the general formula -CO-X, where X is a leaving group. For example, activated forms of carboxylic acid groups can include, but are not limited to, acyl chlorides, symmetrical or asymmetrical anhydrides, and esters. In some embodiments, the activated carboxylic acid group is an ester with pentafluorophenol, nitrophenol, benzotriazole, azabenzotriazole, thiophenol, ethyl 2-cyano-2-(hydroxyimino)acetate, or N-hydroxysuccinimide (NHS) as the leaving group.

[0167] In one embodiment, and as preferably used herein, the term "mediate a linkage" means that a link or type of linkage, preferably a linkage between two moieties, is established.

[0168] The compounds of the present disclosure can contain the amino acid sequences provided herein. Conventional amino acids, also referred to as natural amino acids, are identified according to their standard three-letter and one-letter abbreviations, as shown in Table 3.

[0169] [Table 3]

[0170] Non-conventional amino acids, also called unnatural amino acids, are any type of non-oligomeric compound that contains an amino group and a carboxylic acid group and is not a conventional amino acid. Examples of unconventional amino acids and other building blocks used in the building compounds of the present invention are identified according to their abbreviations or names found in Table 4. The structures of some building blocks are shown along with an exemplary reagent for introducing the building block into a peptide (e.g., as a carboxylic acid), or these building blocks are shown as residues fully attached to another structure, such as a peptide or amino acid. Amino acid structures are shown as explicit amino acids, not as residues of amino acids, but how they appear after implementation in a peptide sequence. Some larger chemical moieties consisting of two or more parts are also shown for clarity.

[0171] [Table 4-1]

[0172] [Table 4-2]

[0173] [Table 4-3]

[0174] [Table 4-4]

[0175] [Table 4-5]

[0176] [Table 4-6]

[0177] [Table 4-7]

[0178] [Table 4-8]

[0179] [Table 4-9]

[0180] [Table 4-10]

[0181] [Table 4-11]

[0182] [Table 4-12]

[0183] The amino acid sequence of peptide provided herein is depicted in typical peptide sequence format, as can be understood by those skilled in the art.For example, the three-letter code of conventional amino acid, or the code of non-conventional amino acid, or the abbreviation of additional building blocks indicate the presence of amino acid or building block at the specified position in peptide sequence.The code of each amino acid or building block is connected to the code of the next and / or previous amino acid or building block in sequence by a hyphen (typically representing amide linkage).

[0184] When an amino acid contains two or more amino and / or carboxy groups, all orientations of the amino acid are in principle possible, but in α-amino acids, utilization of the α-amino and α-carboxy groups is preferred; otherwise, the preferred orientation is expressly specified.

[0185] For amino acids, the first letter in their abbreviations indicates the stereochemistry of the C-α-atom, if applicable, e.g., a capitalized first letter indicates that the L-form of the amino acid is present in the peptide sequence, while a lowercase first letter indicates that the D-form of the corresponding amino acid is present in the peptide sequence.

[0186] In one embodiment, and as preferably used herein, an aromatic amino acid is any type of amino acid that contains an aryl or heteroaryl group. In one embodiment, and as preferably used herein, an aromatic α-amino acid is any kind of α-amino acid that contains an aryl or heteroaryl group.

[0187] In one embodiment, and as preferably used herein, an α-amino acid is an amino acid in which the amino group and the carboxyl group are substituents of the same carbon atom. Those skilled in the art will recognize that if a stereocenter exists in the compounds disclosed herein, regardless of whether such stereocenter is part of the amino acid moiety or any other part or moiety of the compounds of the present disclosure. Therefore, the present disclosure includes possible stereoisomers, including not only racemates but also individual enantiomers and / or diastereomers. If a compound is desired as a single enantiomer or diastereomer, it can be obtained by stereospecific synthesis or by resolution of the final product or any convenient intermediate. Resolution of the final product, intermediate, or starting material can be carried out by any suitable method known in the art. For example, see "Stereochemistry of Organic Compounds" by EL Eliel, SH Wilen, and LN Mander (Wiley-Interscience, 1994).

[0188] In this disclosure, the structural formulas of compounds may in some cases conveniently represent certain isomers, but the present disclosure includes all isomers, such as geometric isomers, optical isomers based on asymmetric carbons, stereoisomers, tautomers, and the like.

[0189] Unless indicated to the contrary, amino acid sequences are presented herein in the N- to C-terminal direction. Linear peptides A typical linear peptide is typically written N to C terminally as shown below: Z 1 -Xaa1-Xaa2-Xaa3-Xaa4-....Xaan-Z 2 During the ceremony, 1. Xaax is an abbreviation, descriptor, or symbol for the amino acid or building block at a particular sequence position x as shown in Table 4, where the linear connection of individual Xaax is indicated by a hyphen; 2. Z 1is the N-terminal group, which may be a chelator or an abbreviation for the N-terminal group NT, e.g., "H" (hydrogen for the free N-terminal amino group), or a specific terminal carboxylic acid such as "Ac" for acetic acid, or other chemical group or structural formula of a chemical group linked via a hyphen to the N-terminal amino acid code (Xaa1), and 3. Z 2 is the C-terminal group CT, e.g., "OH" or "NH2" (as a terminal carboxylic acid or amide), but may also be an amino acid, to which the chelator is attached via an optional linker.

[0190] Branched peptides with side chains modified by specific building blocks or peptides Typical linear and branched peptides are written N-to-C-terminally as shown below: Z 1 -Xaa1-Xaa2-Xaa3(Z 3 -Xab1-Xab2-.......Xabn)-........Xaan-Z 2 In the formula, Xaax, Z in the main chain of the branched peptide 1 and Z 2 For the detailed explanation of linear peptides, the descriptions 1. to 3. apply.

[0191] The location of the branching is identified by parentheses immediately adjacent to the Xaax abbreviation. Branching typically occurs at a lysine (Lys) residue (or analog), meaning that the branching is attached to the lysine side chain ε-amino functionality via an amide bond.

[0192] The contents of the brackets are the peptide branch "Z 3 -Xab1-Xab2-.......Xabn" sequence / structure. 1. Xabx is an abbreviation, descriptor or symbol for the amino acid or building block at a particular sequence position x of the branch as shown in Table 4, the linear connection of the individual Xabx's being indicated by a hyphen; 2. Z 3is the N-terminal group of said branch, which is typically a chelator linked to the N-terminal amino acid Xabl or "H" representing the free amino group of said Xabl, 3. The last building block of the branched Xabn connects the branch to the backbone by forming an amide bond with its own carboxylic acid function via the side chain amino function of this lysine (or similar residue).

[0193] Additionally, the contents of the brackets may be a chemical group attached to a particular heteroatom in the side chain of said building block / amino acid Xaax (e.g., Me for a methyl group). For clarity, such residues (e.g., Arg(Me) or Gln(Gu)) are included in Table 4.

[0194] Cyclic peptides An exemplary generic cyclic peptide written N-to-C-terminally is shown below: Z 1 -Xaa1-[Xaa2-Xaa3-Xaa4-.......Xaan]-Z 2 In the formula, Xaax and Z in the main chain of the cyclic peptide 1 and Z 2 For the detailed description of the formula, statements 1. to 3. in the description of linear peptides apply. The characteristics of the peptide ring are specified by square brackets. 1. The left bracket indicates the unit where the ring begins in the side chain, 2. A right bracket indicates a building block in which the ring is terminated in a side chain.

[0195] The chemical nature of the connection between these two residues is 1. A disulfide bond, typically when both residues / amino acids are cysteines and therefore contain sulfhydryl moieties, or 2. If one of the residues is S-methylcysteine ​​and the other is cysteine, a thio-acetal bond is.

[0196] Furthermore, a cyclic peptide may contain branches at certain positions within its linear sequence, in which case the description "branched peptides with side chains modified by specific building blocks or peptides" applies.

[0197] As a non-limiting example, the structure of DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH2 (PSM-0492) is depicted below:

[0198] [ka]

[0199] During the ceremony, 1. The DOTA chelator is represented by the general formula (I) at Z 1 Corresponds to. 2. Cmp and Thr are both L in general formula (I). 1 Form.

[0200] 3. Aib and Phe correspond to Xaa2 and Xaa3, respectively, in general formula (I). 4. Lys, Arg, Aib and Asn correspond to Xaa5, Xaa6, Xaa7 and Xaa8, respectively, in general formula (I).

[0201] 5. Tle corresponds to Xaa10 in general formula (I). 6. Thr is L in general formula (I). 2 Corresponds to. 7. NH2 is Z in general formula (I). 2 Corresponds to.

[0202] 8. A left square bracket ("[") immediately to the left of the N-terminal cysteine ​​in the sequence indicates that the cycle begins at this residue. 9. The right square bracket ("]") adjacent to the N-terminal cysteine ​​in the sequence indicates that the cycle terminates at this residue.

[0203] In one embodiment, the compound of the present invention comprises a chelator. Preferably, the chelator is a part of the compound of the present invention, wherein the chelator is attached to the compound of the present invention directly or indirectly, such as by a linker. Preferred chelators are those that form metal chelates, preferably containing at least one radiometal. The at least one radiometal is preferably useful or suitable for diagnostic and / or therapeutic and / or theranostic uses, more preferably useful or suitable for imaging and / or radiotherapy.

[0204] The chelators useful and / or suitable for carrying out the present invention, including the diagnosis and / or treatment of disease, are known to those skilled in the art.A wide variety of chelators can be used, as reviewed by, for example, Banerjee et al. (Banerjee et al., Dalton Trans, 2005, 24:3886) and references therein (Price et al., Chem Soc Rev, 2014, 43:260; Wadas et al., Chem Rev, 2010, 110:2858).Such chelators include, but are not limited to, linear, cyclic, macrocyclic, tetrapyridine, N3S, N2S2 and N4 chelators disclosed in US5,367,080A, US5,364,613A, US5,021,556A, US5,075,099A and US5,886,142A.

[0205] Representative chelators and their derivatives, including any bifunctional versions, that can be conjugated to targeting vectors include, but are not limited to, the examples listed in Table 7.

[0206] [Table 5-1]

[0207] [Table 5-2]

[0208]

Table 5-3

[0209]

Table 5-4

[0210]

Table 5-5

[0211]

Table 5-6

[0212]

Table 5-7

[0213]

Table 5-8

[0214]

Table 5-9

[0215]

Table 5-10

[0216] HYNIC, DTPA, EDTA, DOTA, TETA and bisaminobisthiol (BAT) based chelators are disclosed in US 5,720,934; desferrioxamine (DFO) is disclosed in Doulias et al. (Doulias et al., Free Radic Biol Med, 2003, 35:719); tetrapyridine and N3S, N2S2 and N4 chelators are disclosed in US 5,367,080A, US 5,364,613A, US 5,021,556A, US 5,075,099A, US 5,886,142A, all references hereby incorporated by reference in their entirety. 6-Amino-6-methylperhydro-1,4-diazepine-N,N',N'',N''-tetraacetic acid (AAZTA) is disclosed in Pfister et al. (Pfister et al., EJNMMI Res, 2015, 5:74); deferiprone, 1,2-dimethyl-3,4-hydroxypyridinone, and hexadentate tris(3,4-hydroxypyridinone) (THP) are disclosed in Cusnir et al. (Cusnir et al., Int J Mol Sci, 2017, 18); monoamine-monoamide dithiol (MAMA)-based chelators are disclosed in Demoin et al. (Demoin et al., Nucl Med Biol, 2016, 43:802); Macropa and analogs are disclosed in Thiele et al. (Thiele et al., Angew Chem Int Ed Engl, 2017, 56:14712); 1,4,7,10,13,16-hexaazacyclohexadecane-N,N',N'',N''',N'''',N'''''-hexaacetic acid (HEHA) and PEPA analogs are disclosed in Price and Orvig (Price et al., Chem Soc Rev, 2014, 43:260);Pycup and analogs are disclosed in Boros et al. (Boros et al., Mol Pharm, 2014, 11:617) and contain N,N-bis(2-hydroxybenzyl)ethylenediamine-N,N-diacetic acid (HBED), 1,4,7,10-tetrakis(carbamoylmethyl)-1,4,7,10-tetraazacyclododecane (TCM), 2-[(carboxymethyl)]-[5-(4-nitrophenyl)-1-[4,7,10-tris-(carboxymethyl)-1,4,7, 10-Tetraazacyclododecan-1-yl]pentan-2-yl)-amino]acetic acid (3p-C-DEPA), CB-TE2A, TE2A, TE1A1P, DiAmSar, 1-N-(4-aminobenzyl)-3,6,10,13,16,19-hexaazabicyclo[6.6.6]-eicosane-1,8-diamine (SarAr), NETA, tris(2-mercaptoethyl)-1,4,7-triazacyclonona TACN-TM), {4-[2-(bis-carboxymethyl-amino)-ethyl]-7-carboxymethyl-[1,4,7]triazonan-1-yl}-acetic acid (NETA), diethylenetriaminepentaacetic acid (DTP), 3-({4,7-bis-[(2-carboxy-ethyl)-hydroxy-phosphinoylmethyl]-[1,4,7]triazonan-1-ylmethyl}-hydroxy-phosphinoyl)-propionyl carboxylic acid (TRAP), NOPO, H4octapa, SHBED, BPCA, 3,6,9,15-tetraazabicyclo[9.3.1]-pentadeca-1(15),11,13-triene-3,6,9-triacetic acid (PCTA) and 1,4,7,10,13-pentaazacyclopentadecane-N,N',N'',N''',N''''-pentaacetic acid (PEPA) are disclosed by Price and Orvig (Price et al., Chem Soc Rev, 2014, 43:260); 1-hydroxy-2-pyridone ligand (HOPO) is disclosed by Allott et al. (Allott et al., Chem Commun (Camb), 2017, 53:8529);[4-carboxymethyl-6-(carboxymethyl-methyl-amino)-6-methyl-[1,4]diazepan-1-yl]-acetic acid (DATA) is disclosed in Tornesello et al. (Tornesello et al., Molecules, 2017, 22:1282); tetrakis(aminomethyl)methane (TAM) and analogs are disclosed in McAuley 1988 (McAuley et al., Canadian Journal of Chemistry, 1989, 67:1657); hexadentate tris(3,4-hydroxypyridinone) (THP) and analogs are disclosed in Ma et al. (Ma et al., Dalton Trans, 2015, 44:4884);

[0217] The diagnostic and / or therapeutic uses of some of the above chelators are described in the prior art. For example, 2-hydrazinonicotinamide (HYNIC) 99m Tc and 186,188 It has been widely used in the presence of co-ligands for the incorporation of Re (Schwartz et al., Bioconjug Chem, 1991, 2:333; Babich et al., J Nucl Med, 1993, 34:1964; Babich et al., Nucl Med Biol, 1995, 22:25); DTPA 111 In complexation with Octreoscan®, some modifications have been described in the literature (Li et al., Nucl Med Biol, 2001, 28:145; Brechbiel et al., Bioconjug Chem, 1991, 2:187); DOTA-type chelators for radiotherapy applications have been described by Tweedle et al. (U.S. Pat. No. 4,885,363); other polyazamacrocycles for chelating trivalent isotope metals have been described by Eisenwiener et al. (Eisenwiener et al., Bioconjug Chem, 2002, 13:530); N4-chelators, e.g. 99m Tc-N4-chelators have been used for peptide labeling in the case of minigastrins to target the CCK-2 receptor (Nock et al., J Nucl Med, 2005, 46:1727).

[0218] In one embodiment, the chelator is DOTA, DOTAGA, DOTAM, Crown, DOTP, NOTA, NODAGA, NODA-MPAA, HBED, TETA, CB-TE2A, DTPA, CHX-A''-DTPA, DFO, Macro pa, HOPO, TRAP, THP, DATA, NOPO, NOTP, PCTA, LSC (substitute: PSC), sarcophagin, FSC, NETA, NE3TA, H4octapa, pycup, HYNIC, NxS4-x (N4, N2S2, N3S), 99m The chelator is selected from the group including, but not limited to, Tc(CO)3-chelators and their analogs. Preferably, the chelator further comprises one or more functional groups or functionality that allow for binding to the compounds of the present invention.

[0219] Their chemical structures are as follows:

[0220] [ka]

[0221] In one embodiment, the chelator is DOTA, DOTAGA, NOPO, PCTA, NOTA, NODAGA, NODA-MPAA, HBED, TETA, CB-TE2A, DTPA, DFO, Macropa, Crown, DOTAM, HOPO, TRAP, THP, DATA, NOTP, LSC (alternative to PSC), sarcofadin, FSC, NETA, H4octapa, Pycup, N x S 4-x (N4, N2S2, N3S), Hynic, 99m Tc(CO)3-chelators.

[0222] In another embodiment, the chelator is selected from the group consisting of DOTA, DOTAGA, NOPO, PCTA, DOTAM, Macropa, Crown, NOTA, NODAGA, NODA-MPAA, HBED, CB-TE2A, DFO, THP, LSC (a substitute for PSC), and N4.

[0223] In another embodiment, the chelator is selected from the group consisting of DOTA, DOTAGA, NOPO, PCTA, DOTAM, Macropa, Crown, NOTA, LSC (a substitute for PSC), and NODAGA.

[0224] In another embodiment, the chelator is selected from the group consisting of DOTA, DOTAM, Macropa, Crown, NOTA, LSC (a substitute for PSC), and NODAGA.

[0225] In another embodiment, the chelator is DOTA. Preferably, the chelator further comprises one or more functional groups or functionality that allow for attachment to a compound of the invention.

[0226] It will be recognized by those skilled in the art that, in principle, chelators can be used regardless of whether the compounds of the invention are used in or suitable for diagnosis or therapy. Such principles are outlined, inter alia, in WO2009 / 109332 A1.

[0227] It will be further recognized by those skilled in the art that the presence of a chelator in a compound of the present invention, unless otherwise stated, includes the possibility that the chelator may be complexed with any metal complex partner, i.e., any metal that can, in principle, be complexed by a chelator. Explicitly mentioned chelators in the compounds of the present invention, or the general term chelator in relation to the compounds of the present invention, refer to either the intact, uncomplexed chelator, or a chelator to which any metal complex partner is bound, where the metal complex partner is any radioactive or non-radioactive metal complex partner. Preferably, the chelator-metal complex, i.e., the chelator to which the metal complex partner is bound, is a suitable chelator-metal complex.

[0228] Non-radioactive chelator-metal complexes have several applications, for example, for assessing properties such as stability or activity that are otherwise difficult to determine. One aspect is that cold variants of radioactive versions of metal complex partners (e.g., the non-radioactive indium complexes described in the Examples) can act as surrogates for radioactive compounds. Furthermore, they are valuable tools for identifying metabolites in vitro or in vivo and for assessing the toxicity properties of compounds of the invention. In addition, chelator-metal complexes can be used in binding assays that take advantage of the fluorescein properties of some metal complexes with distinct ligands (e.g., europium salts).

[0229] Chelators may be synthesized or are commercially available with a wide variety of groups (possibly already activated) for conjugation to peptides or amino acids.

[0230] Direct conjugation of a chelator to the amino nitrogen of each of the compounds of the invention is fully possible for chelators selected from the group consisting of DTPA, DOTA, DOTAGA, NOTA, NODAGA, NODA-MPAA, HBED, TETA, CB-TE2A, DFO, DATA, sarcofazine, and N4, preferably DTPA, DOTA, DOTAGA, NOTA, NODAGA, NODA-MPAA, CB-TE2A, and N4. A preferred linkage in this regard is an amide linkage.

[0231] Direct conjugation of an isothiocyanate-functionalized chelator to the amino nitrogen of each of the compounds of the invention is fully possible for chelators selected from the group consisting of DOTA, DOTAGA, NOTA, NODAGA, DTPA, CHX-A″-DTPA, DFO and THP, preferably DOTA, DOTAGA, NOTA, NODAGA, DTPA and CHX-A″-DTPA. A preferred linkage in this regard is the thiourea linkage.

[0232] Functional groups on chelators that are preferred precursors for direct conjugation to the amino nitrogen of a chelator are known to those skilled in the art and include, but are not limited to, carboxylic acids, activated carboxylic acids, e.g., active esters such as NHS-esters, pentafluorophenol-esters, HOBt-esters, HOAt-esters, and isothiocyanates.

[0233] Functional groups on chelators that are preferred precursors for direct conjugation of the chelator to a carboxylic acid group are known to those skilled in the art and include, but are not limited to, alkylamino and arylamino nitrogens. Respective chelator reagents are commercially available for some chelators, such as DOTA with either alkylamino or arylamino nitrogens.

[0234] Functional groups on chelators that are preferred precursors for direct conjugation of the chelator to a thiol group are known to those skilled in the art and include, but are not limited to, maleimide nitrogen. Respective chelator reagents are commercially available for some chelators, such as DOTA with a maleimide nitrogen.

[0235] Functional groups on chelators that are preferred precursors for direct conjugation of the chelator to the azide group are known to those skilled in the art and include, but are not limited to, acyclic and cyclic alkynes. Respective chelator reagents are commercially available for some chelators, for example, DOTA with propargyl or butynyl.

[0236] Functional groups on chelators that are preferred precursors for direct conjugation of the chelator to an alkyne group are known to those skilled in the art and include, but are not limited to, alkyl and aryl azines. The respective chelator reagents are commercially available for some chelators, for example, DOTA with azidopropyl.

[0237] It will be appreciated by those skilled in the art that the radioactive nuclide attached or to be attached to the compounds of the present disclosure will be selected taking into account the particularities of the disease to be treated and / or the disease to be diagnosed, respectively, and / or the patient and patient group to be treated and diagnosed, respectively.

[0238] In this disclosure, radioactive nuclei are also referred to as radionuclides. Radioactive decay is the process by which the nuclei of unstable atoms lose energy by emitting ionizing particles (ionizing radiation). There are various types of radioactive decay. Decay, i.e., energy loss, occurs when an atom with one type of nucleus, called a parent radionuclide, transforms into an atom with a nucleus in a different state or into a different nucleus containing a different number of protons and neutrons. Any of these products is named a daughter nuclide. In some decays, the parent and daughter are different chemical elements; therefore, the decay results in nuclear transmutation (the creation of atoms of a new element). For example, radioactive decay can be alpha decay, beta decay, or gamma decay. Alpha decay occurs when a nucleus emits an alpha particle (helium nucleus). This is the most common process of emitting nucleons, but in rarer types of decay, the nucleus can emit protons or specific nuclei of other elements (in a process called cluster decay). Beta decay occurs when a nucleus loses electrons (β - -decay) or positron (β + -decay) and releases a type of neutrino. In contrast, there are radioactive decay processes that do not result in transmutation. The energy of an excited nucleus may be released as gamma rays in gamma decay; used to eject an orbital electron by interaction with the excited nucleus in a process called internal conversion; used to absorb an inner atomic electron from an electron shell in a process called electron capture (EC), which changes a nuclear proton to a neutron and causes the emission of an electron neutrino; or may be emitted without changing the number of protons and neutrons in a process called isomerization (IT). Another form of radioactive decay, spontaneous fission (SF), is only seen in very heavy chemical elements and results in the spontaneous breakdown into smaller nuclei and a few isolated nuclear particles.

[0239] In one embodiment, compounds containing radionuclides are described herein.Generally, the type of radionuclides used in therapeutic radiopharmaceuticals can be individually tailored for specific types of cancer and types of targeting moieties.Radionuclides that undergo α-decay produce particles consisting of two neutrons and two protons, while radionuclides that undergo β-decay emit energetic electrons from their nuclei.In addition, some radionuclides can emit Auger electrons.In some embodiments, conjugates comprise alpha particle-emitting radionuclides.Alpha radiation can cause direct and irreparable double-stranded DNA breaks, compared to gamma and beta radiation, which can cause single-strand breaks through indirect DNA damage.In addition, the range of these particles in tissue and the half-life of radionuclides can be taken into consideration when designing radiopharmaceutical conjugates.

[0240] Alpha-emitter radionuclides have the ability to destroy tumors while causing very limited damage to surrounding healthy tissue due to the short penetration depth of alpha particles. Because of their high linear energy transfer (LET), they have a high relative biological effectiveness (RBE) compared to other radionuclide therapies. Furthermore, when alpha-emitting radionuclides are targeted to specific tumor cells in the body, they can be highly effective in destroying metastases, which are difficult to treat with currently used techniques (de Kruijff et al., Pharmaceuticals, 2015, 8:321-336).

[0241] In one embodiment of the present disclosure, radionuclides may be used for labeling of the compounds of the present disclosure. In one embodiment of the present disclosure, the radionuclide is suitable for complexation with a chelator, resulting in a radionuclide chelate complex.

[0242] In further embodiments, one or more atoms of the compounds of the present disclosure are of non-natural isotopic composition, e.g., the atoms are radionuclides, e.g., radionuclides of carbon, oxygen, nitrogen, sulfur, phosphorus, and halogens. These radioactive atoms are typically part of amino acids, in some cases halogen-containing amino acids, and / or building blocks, in some cases halogenated building blocks, of each of the compounds of the present disclosure.

[0243] In one embodiment of the present disclosure, the radionuclide has a half-life that allows for diagnostic and / or therapeutic medical use, particularly a half-life of between 1 minute and 100 days. In one embodiment of the present disclosure, the radionuclide has a decay energy that allows for diagnostic and / or therapeutic medical use. In particular, for γ-emitting isotopes, the decay energy is 0.004 to 10 MeV, e.g., 0.05 to 4 MeV, for diagnostic use. For positron-emitting isotopes, the decay energy is 0.6 to 13.2 MeV, e.g., 1 to 6 MeV, for diagnostic use. For particle-emitting isotopes, the decay energy is 0.039 to 10 MeV, e.g., 0.4 to 6.5 MeV, for therapeutic use.

[0244] In one embodiment of the present invention, the radionuclide is produced industrially for medical use, in particular the radionuclide is available in GMP quality. In one embodiment of the present disclosure, the daughter nuclide after radioactive decay of the radionuclide is suitable for diagnostic and / or therapeutic medical use. Furthermore, the daughter nuclide is stable or decays further so as not to interfere with or even support diagnostic and / or therapeutic medical use. Representative radionuclides that can be used in connection with the present disclosure are well known to those skilled in the art and include the following: 11 C. 13 N, 18 F, 24 Na, 28 Mg, 31 Si, 32 P, 33 P, 38 S, 34m Cl, 38 Cl,39 Cl 37 Ar 41 Ar 44 Ar 42 K、 43 K、 44 K、 45 K、 47 Ca、 43 sc、 44 sc、 44m sc、 47 sc、 48 sc、 49 sc、 45 tea 47 V、 48 V、 48 Cr、 49 Cr、 51 Cr、 51 Mn 52 Mn 52m Mn 56 Mn 52 Fe 59 Fe 55 Co. 61 Co. 62m Co. 56 Ni 57 Ni 65 Ni 66 Ni 60 Cu、 61 Cu、 64 Cu、 67 Cu、 62 Zn、 63 Zn、 69 Zn、 69m Zn、 71m Zn、 72 Zn、 65 Ga 66 Ga 67 Ga 68 Ga 70 Ga 72 Ga 73 Ga 66 Ge 67 Ge 69 Ge 71 Ge 75 Ge 77 Ge 78 Ge 69 As 70 As 71 As 72 As 74 As76 I, 77 I, 78 I, 70 Yes, 72 Yes, 73 Yes, 73m Yes, 81 Yes, 81m Yes, 83 Yes, 74 Br、 74m Br、 75 Br、 76 Br、 77 Br、 80 Br、 80m Br、 82 Br、 83 Br、 84 Br、 74 Cr、 76 Cr、 77 Cr、 79 Cr、 85 Cr、 87 Cr、 88 Cr、 78 Rb, 79 Rb, 81 Rb, 82 Rb, 84 Rb, 84m Rb, 86 Rb, 88 Rb, 89 Rb, 80 Mr. 81 Mr. 82 Mr. 83 Mr. 85m Mr. 87 Mr. 91 Mr. 92 Mr. 84 Y、 85 Y、 85m Y、 86 Y、 86m Y、 87 Y、 87m Y、 90 Y、 90m Y、 91m Y、 92 Y、 93 Y、 94 Y、 95 Y、 86 Zr、 87 Zr、 89 Zr、 97 Zr、 88 Nb,89 Nb, 89m Nb, 90 Nb, 92 Nb, 95 Nb, 95m Nb, 96 Nb, 97 Nb, 98m Nb, 101 Monday, 102 Monday, 90 Monday, 91M oh, 93m Monday, 99 Monday, 101 Tc, 104 Tc, 93 Tc, 93m Tc, 94 Tc, 94m Tc, 95 Tc, 96 Tc, 99m Tc, 103 Ru, 105 Ru, 94 Ru, 95 Ru, 97 Ru, 100 Rh, 101m Rh, 105 Rh, 106m Rh, 107 Rh, 97 Rh, 97m Rh, 99 Rh, 99m Rh, 100 Pd, 101 Pd, 103 Pd, 109 Pd, 111 Pd, 111m Pd, 112 Pd, 98 Pd, 99 Pd, 101 Ah, 103 Ah, 104 Ah, 104m Ah, 105 Ah, 106 Ah, 106m Ah, 111 Ah, 112 Ah, 113 Ah, 115 Ah, 104 CD, 105 CD, 107 CD, 111 CD, 115Cd、 115m Cd、 117 Cd、 117m Cd、 118 Cd、 107 In、 108m In、 109 In、 110 In、 110m In、 111 In、 112 In、 113 In、 114m In、 115m In、 116m In、 117 In、 117m In、 119m In、 108 Sn、 109 Sn、 110 Sn、 111 Sn、 117 Sn、 121 Sn、 123m Sn、 125 Sn、 127 Sn、 128 Sn、 115 Sb、 116 Sb、 116m Sb、 117 Sb、 118m Sb、 119 Sb、 120 Sb、 120m Sb、 122 Sb、 126 Sb、 126m Sb、 127 Sb、 128 Sb、 128m Sb、 129 Sb、 129m Sb、 130 Sb、 131 Sb、 114 Te、 116 Te、 117 Te、 118 Te、 119 Te、 119m Te、 121 Te、 127 Te、 129 Te、 129m Te、 131 Te、 131m Te、 132 Te、 133 Te、 133m Te、 134 Te、118 I、 119 I、 120 I、 120m I、 121 I、 123 I、 124 I、 126 I、 128 I、 130 I、 131 I、 132 I、 132m I、 133 I、 134 I、 135 I、 120 Car, 121 Car, 122 Car, 123 Car, 125 Car, 127 Car, 133 Car, 133m Car, 135 Car, 135m Car, 138 Car, 125 Cs、 127 Cs、 129 Cs、 130 Cs、 131 Cs、 132 Cs、 134 Cs、 135 Cs、 136 Cs、 138 Cs、 124 Three, 126 Three, 127 Three, 128 Three, 129 Three, 129m Three, 131 Three, 131m Three, 133 Three, 135 Three, 139 Three, 140 Three, 141 Three, 142 Three, 129 Yes 131 Yes 132 Yes 133 Yes 135 Yes 140 Yes 141 Yes 142 Yes 143 Yes 130 Ce 132 Ce 133 Ce 133mWhat, 134 What, 135 What, 137 What, 137m What, 141 What, 143 What, 146 What, 134 Mr. 134m Mr. 136 Mr. 137 Mr. 138m Mr. 139 Mr. 142 Mr. 143 Mr. 144 Mr. 145 Mr. 146 Mr. 147 Mr. 135 Yes, 136 Yes, 137 Yes, 138 Yes, 139 Yes, 139m Yes, 140 Yes, 141 Yes, 147 Yes, 149 Yes, 151 Yes, 152 Yes, 141 P.m, 148 P.m, 148m P.m, 149 P.m, 150 P.m, 151 P.m, 140 Sm、 141 Sm、 141m Sm、 142 Sm、 153 Sm、 155 Sm、 156 Sm、 145 I, 146 I, 147 I, 150 I, 152m I, 154 I, 156 I, 157 I, 158 I, 159 I, 145 Gd、 146 Gd、 147 Gd、 149 Gd、 159 Gd、 147 Tb、 148 Tb、 149 Tb、150 Tb、 151 Tb、 152 Tb、 153 Tb、 154 Tb、 154m Tb、 155 Tb、 156 Tb、 156m Tb、 161 Tb、 163 Tb、 151 Live, 152 Live, 153 Live, 155 Live, 157 Live, 165 Live, 166 Live, 154 Hey, 155 Hey, 156 Hey, 157 Hey, 158m Hey, 159 Hey, 161 Hey, 162 Hey, 162m Hey, 164 Hey, 164m Hey, 166 Hey, 167 Hey, 156 Is, 157 Is, 158 Is, 159 Is, 160 Is, 161 Is, 163 Is, 165 Is, 169 Is, 171 Is, 172 Is, 161 Tm, 162 Tm, 163 Tm, 165 Tm, 166 Tm, 167 Tm, 172 Tm, 173 Tm, 175 Tm, 162 Yb、 163 Yb、 164 Yb、 166 Y b、 167 Yb、 169 Yb、 175 Yb、 177 Yb、178 Yb、 167 sun 169 sun 170 sun 171 sun 172 sun 176m sun 177 sun 178 sun 178m sun 179 sun 168 Hf 170 Hf 173 Hf 177m Hf 179m Hf 180m Hf 181 Hf 182m Hf 183 Hf 184 Hf 172 Ta 173 Ta 174 Ta 175 Ta 176 Ta 177 Ta 178 Ta 180 Ta 182m Ta 183 Ta 184 Ta 185 Ta 186 Ta 174 W、 175 W、 177 W、 178 W、 179 W、 187 W、 190 W、 177 Re 178 Re 179 Re 181 Re 182 Re 182m Re 184 Re 186 Re 188 Re 188m Re 189 Re 190m Re 180 Or 181 Or 182 Or 183 Or 183m Or 191 Or 193 Or 196 Or 182 Ir 183 Ir184 Ir, 185 Ir, 186 Ir, 186m Ir, 187 Ir, 188 Ir, 189 Ir, 190 Ir, 194 Ir, 195 Ir, 195m Ir, 196m Ir, 184 Pt. 186 Pt. 187 Pt. 188 Pt. 189 Pt. 191 Pt. 195 Pt. 197 Pt. 197m Pt. 199 Pt. 200 Pt. 202 Pt. 186 I, 190 I, 191 I, 192 I, 193 I, 194 I, 196 I, 196m I, 198 I, 198m I, 199 I, 200 I, 200m I, 190 Hg, 191 Hg, 192 Hg, 193 Hg, 195 Hg, 195m Hg, 197 Hg, 197m Hg, 199 Hg, 203 Hg, 194 Hello, 194m Hello, 195 Hello, 196 Hello, 196m Hello, 197 Hello, 198 Hello, 198m Hello, 199 Hello, 200 Hello, 201 Hello, 202 Hello, 194 Pb, 195 Pb, 196 Pb, 197mPb、 198 Pb、 199 Pb、 199m Pb、 200 Pb、 201 Pb、 202m Pb、 203 Pb、 204 Pb、 209 Pb、 211 Pb、 212 Pb、 214 Pb、 200 Hello 200m Hello 201 Hello 202 Hello 203 Hello 204 Hello 205 Hello 206 Hello 210 Hello 212 Hello 212m Hello 213 Hello 214 Hello 200 Night, 201 Night, 202 Night, 203 Night, 204 Night, 205 Night, 206 Night, 207 Night, 205 And 206 And 207 And 208 And 209 And 210 And 211 And 208 Rn 209 Rn 210 Rn 211 Rn 212 Rn 221 Rn 222 Rn 223 Rn 212 Fr. 222 Fr. 223 Fr. 223 Ra 224 Ra 225 Ra 227 Ra 230 Ra 224 And 225 And 226 And 228 And 229 And 226 Th227 Th、 231 Th、 233 Th、 234 Th、 236 Th、 227 Pa、 228 Pa、 229 Pa、 230 Pa、 232 Pa、 233 Pa、 234 Pa、 235 Pa、 229 U、 230 U、 231 U、 237 U、 239 U、 240 U、 242 U、 231 Np、 232 Np、 233 Np、 234 Np、 236m Np、 238 Np、 239 Np、 240 Np、 241 Np、 232 Pu、 235 Pu、 237 Pu、 243 Pu、 245 Pu、 246 Pu、 235 Am、 237 Am、 238 Am、 239 Am、 240 Am、 242 Am、 244 Am、 244m Am、 245 Am、 246 Am、 246m Am、 247 Am、 239 Cm、 240 Cm、 241 Cm、 251 Cm、 245 Bk、 246 Bk、 248 Bk、 250 Bk、 251 Bk、 244 Cf、 245 Cf、 246 Cf、 247 Cf、 253 Cf、 255 Cf、 249 Es、250 Es, 250m Es, 251 Es, 253 Es, 254m Es, 255 Es, 256m Es, 250 Fm, 251 Fm, 252 Fm, 254 Fm, 255 Fm, 255 Md, 256 Md, 257 Md, 259 These include, but are not limited to, No. Their properties are described in more detail, for example, in Nuclear Data Sheets (Elsevier, Amsterdam, NL).

[0245] In one embodiment of the present disclosure, the radionuclide is used in diagnosis. In some embodiments, the radioisotope is 43 Sc, 44 Sc, 51 Mn, 52 Mn, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 94m Tc, 99m Tc, 111 In, 152 Tb, 155 Tb, 177 Lu, 201 Tl, 203 Pb, 18 F, 76 Br, 77 Br, 123 I, 124 I and 125 In some embodiments, the radionuclide is selected from the group including, but not limited to, I. 18 F, 43 Sc, 44 Sc, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 99m Tc, 111 In,152 Tb, 155 Tb and 203 Pb. In some embodiments, the radionuclide is selected from 18 F, 64 Cu, 68 Ga and 111 In one embodiment of the present disclosure, the radionuclide is selected from: 18 F, where 18 F forms a covalent bond to aluminum, which then forms a metal complex with the chelator. 18 Methods and compositions for F labeling are disclosed, for example, in WO2012 / 082618. However, it will also be recognized by those skilled in the art that the use of such radionuclides is not limited to diagnostic purposes, but also encompasses their use in therapy and theragnostics when conjugated to compounds of the present disclosure.

[0246] In one embodiment of the present disclosure, a radionuclide is used in therapy. In some embodiments, the radioisotope is 47 Sc, 67 Cu, 89 Sr, 90 Y, 111 In, 153 Sm, 149 Tb, 161 Tb, 177 Lu, 186 Re, 188 Re, 212 Pb, 212 Bi, 213 Bi, 223 Ra, 224 Ra, 225 Ac, 226 Th, 227 Th, 131 I and 211 In some embodiments, the radioisotope is selected from: 47 Sc, 67 Cu, 90 Y, 161 Tb, 177 Lu, 188 Re, 212 Pb, 212 Bi,213 Bi, 225 Ac and 227 In some embodiments, the radionuclide is selected from: 90 Y, 161 Tb, 177 Lu, 212 Pb, 225 Ac and 227 However, it will also be recognized by those skilled in the art that the use of said radionuclides is not limited to therapeutic purposes, but also encompasses their use in diagnostics and theragnostics when conjugated to compounds of the present disclosure.

[0247] In one embodiment, the compounds of the present invention and disclosure each comprise a nuclide that is bound, preferably coordinated, by a chelator that forms part of the compound. It will be recognized and understood by those skilled in the art that the coordination geometry of such complexes between a nuclide and a chelator can vary. Examples of structures, coordination geometries, and overall complex charges for various chelate complexes are shown in Table 8.

[0248] [Table 6-1]

[0249] [Table 6-2]

[0250] [Table 6-3]

[0251] In one embodiment, the compounds of the present disclosure are present as pharmaceutically acceptable salts. In certain embodiments, a "pharmaceutically acceptable salt" of a compound of the present disclosure is an acid or base salt generally considered in the art to be suitable for use in contact with human or animal tissues without excessive toxicity or carcinogenicity, and without, for example, irritation, allergic reaction, or other problems or complications. Such salts include mineral and organic acid salts of basic residues, such as amines, and alkali or organic salts of acidic residues, such as carboxylic acids. The compounds of the present disclosure are capable of forming internal salts, which are also pharmaceutically acceptable salts.

[0252] Suitable pharmaceutically acceptable salts include those derived from acids such as hydrochloric acid, phosphoric acid, hydrobromic acid, malic acid, glycolic acid, fumaric acid, sulfuric acid, sulfamic acid, sulfanilic acid, formic acid, toluenesulfonic acid, methanesulfonic acid, benzenesulfonic acid, ethanedisulfonic acid, 2-hydroxyethylsulfonic acid, nitric acid, benzoic acid, 2-acetoxybenzoic acid, citric acid, tartaric acid, lactic acid, stearic acid, salicylic acid, glutamic acid, ascorbic acid, pamoic acid, succinic acid, fumaric acid, maleic acid, propionic acid, hydroxymaleic acid, hydroiodic acid, phenylacetic acid, alkanoic acids such as acetic acid, HOOC-(CH2) n The salts include, but are not limited to, salts of -COOH, etc. Similarly, pharmaceutically acceptable cations include, but are not limited to, sodium, potassium, calcium, aluminum, lithium and ammonium. Those skilled in the art will recognize additional pharmaceutically acceptable salts for the compounds provided herein. Generally, pharmaceutically acceptable acid or base salts can be synthesized from parent compounds containing a basic or acidic moiety by any conventional chemical method. Briefly, such salts can be prepared by reacting the free acid or free base form of these compounds with a stoichiometric amount of an appropriate base or acid in water or an organic solvent, or a mixture of both. Generally, the use of non-aqueous media, such as ether, ethyl acetate, ethanol, isopropanol or acetonitrile, is preferred.

[0253] In one embodiment, the compounds of the present disclosure exist as pharmaceutically acceptable solvates. In certain embodiments, the " pharmaceutically acceptable solvate " of a compound of the present disclosure is a solvate of a compound of the present disclosure formed by the association of one or more solvent molecules with one or more molecules of the compound of the present disclosure. In some embodiments, the solvent is a solvent generally considered in the art to be suitable for use in contact with human or animal tissues without excessive toxicity or carcinogenicity, and without, for example, irritation, allergic reaction, or other problems or complications. Such solvents include organic solvents, such as alcohols, ethers, esters, and amines.

[0254] In one embodiment, the compounds of the present disclosure are present as hydrates, preferably pharmaceutically acceptable hydrates. In certain embodiments, the "hydrate" of the compound of the present disclosure is formed by associating one or more water molecules with one or more molecules of the compound of the present disclosure. Such hydrates include, but are not limited to, hemihydrate, monohydrate, dihydrate, trihydrate and tetrahydrate. Regardless of the hydrate composition, all hydrates are generally considered to be pharmaceutically acceptable.

[0255] The compound of the present disclosure has high binding affinity to PSMA.Because of this high binding affinity, the compound of the present disclosure is effective, useful and / or suitable as targeting agent, and wherein target is PSMA and / or the cell and / or tissue that expresses PSMA.Regarding the cell and tissue that is targeted by the compound of the present disclosure, any cell and tissue that expresses PSMA can be targeted or can be targeted, respectively.

[0256] It is within the scope of the present disclosure that the compounds of the present disclosure are used in or for use in methods for treating the diseases disclosed herein.In certain embodiments, such methods for treating the diseases disclosed herein comprise administering a therapeutically effective amount of a compound of the present disclosure to a subject in need of disease treatment.Such methods include, but are not limited to, curative or adjuvant cancer treatment.When cure is not possible and the purpose is local disease management or symptom relief, it is used as a symptomatic treatment, or when the treatment has a survival benefit and can be curative, it is used as a therapeutic treatment.

[0257] The methods for treating diseases disclosed herein include the treatment of diseases disclosed herein, including tumors and cancers, and can be used as first-line treatment, or as second, third, fourth or final treatment.It is also within the scope of this disclosure to combine the compounds of the present disclosure with additional therapeutic approaches.It is well known to those skilled in the art that the precise treatment intent, including curative, adjuvant, neoadjuvant, therapeutic or symptomatic treatment intent, depends on the type, location and stage of tumor and the overall health of the patient.

[0258] In one embodiment of the present disclosure, the disease is a prostate tumor, metastatic prostate tumor, lung tumor, kidney tumor, glioblastoma, pancreatic tumor, bladder tumor, sarcoma, melanoma, breast tumor, colon tumor, pheochromocytoma, esophageal tumor, gastric tumor, carcinoma, squamous cell carcinoma (e.g., of the cervix, eyelid, conjunctiva, vagina, lung, oral cavity, skin, bladder, tongue, larynx, and esophagus), and adenocarcinoma (e.g., of the prostate, small intestine, endometrium, cervix, large intestine, lung, pancreas, esophagus, rectum, uterus, stomach, breast, and ovary), prostate cancer (e.g., metastatic castration-resistant prostate cancer), kidney cancer (e.g., clear cell carcinoma), head cancer, neck cancer, head and neck cancer, lung cancer (e.g., non-small cell lung cancer, lung cancer), salivary gland cancer, breast cancer, colorectal cancer, esophageal cancer, gastric cancer, liver cancer (e.g., hepatocellular carcinoma), thyroid cancer, glioblastoma, glioma, gallbladder cancer, laryngeal cancer, leukemia / lymphoma, uterine cancer, skin cancer (e.g., melanoma), endocrine cancer, sarcoma, urinary tract cancer, pancreatic cancer, gastrointestinal cancer, ovarian cancer, cervical cancer, endometrial cancer, fallopian tube cancer, primary peritoneal cancer, blood cancer (e.g., diffuse large B-cell lymphoma, Hodgkin's lymphoma, non-Hodgkin's lymphoma, follicular lymphoma, acute myeloid leukemia or multiple myeloma), cancer of unknown primary, adenoma and tumor angiogenesis.

[0259] In some embodiments, subjects treated with the compounds of the present disclosure may be treated in combination with other non-surgical antiproliferative (e.g., anti-cancer) drug therapies. In some embodiments, the compounds may be administered in combination with anti-cancer compounds, such as cytostatic compounds. Cytostatic compounds are compounds (e.g., small molecules, nucleic acids, or proteins) that inhibit cell growth and / or proliferation. In some embodiments, the cytostatic compounds are directed against malignant cells of tumors. In some embodiments, the cytostatic compounds are cytostatic compounds that inhibit the growth and / or proliferation of vascular smooth muscle cells or fibroblasts.

[0260] In some embodiments, the compound described herein is used in combination with or is intended for use in combination with chemotherapy, for example, chemotherapy that damages DNA.Non-limiting examples of chemotherapy that damages DNA include topoisomerase I inhibitor, topoisomerase II inhibitor; alkylating agent; DNA intercalator; DNA intercalator and free radical generator, such as bleomycin; and nucleoside mimetics.

[0261] In some embodiments, the compounds described herein can be administered alone or in combination with one or more additional therapeutic agents. For example, combination therapy can include a composition comprising the conjugate described herein formulated and / or co-administered with one or more additional therapeutic agents, such as one or more anticancer agents, such as cytotoxic or cytostatic agents, immune checkpoint inhibitors, hormone therapy, vaccines, and / or immunotherapy. In some embodiments, the additional therapeutic agent can be selected from cell cycle inhibitors, CDK inhibitors, radiosensitizers, agents that upregulate PSMA expression, angiogenesis inhibitors, other drugs that reduce hypoxia and increase radiosensitivity, and / or renal protective agents. In some embodiments, the conjugate is administered in combination with other therapeutic treatment modalities, including surgery, cryosurgery, and / or chemotherapy. Such combination therapy can advantageously utilize lower dosages of the administered therapeutic agent, thus avoiding the potential toxicity or complications associated with various monotherapies.

[0262] Suitable antiproliferative or cytostatic compounds to be used in combination with the compounds of the present disclosure include anticancer drugs. Many anticancer drugs that can be used are well known and include acivicin, aclarubicin, acodazole hydrochloride, acronine, adozelesin, aldesleukin, altretamine, ambomycin, amethanthrone acetate, aminoglutethimide, amsacrine, anastrozole, anthramycin, asparaginase, asperlin, azacitidine, azaribine, azetepa, azotomycin, batimastat, benzodepa, bicalutamide, bisantrene hydrochloride, bisnafide mesylate, bizelesin, bleomycin, bleomycin sulfate, etc. Benzene;Brequinar sodium;Bropirimine;Bryostatin 1;Busulfan;Cactinomycin;Calsterone;Caracemide;Carbetimer;Carboplatin;Carmustine;Carubicin hydrochloride;Carzelcin;Cedefingol;Celebrex;Chlorambucil;Ciloremycin;Cisplatin;Cladribine;Crisnatol mesylate;Cyclophosphamide;Cytarabine;Dacarbazine;Dactinomycin;Daunorubicin;Daunorubicin hydrochloride;Decitabine;Dexormaplatin;Desaguanine;Desaguanine mesylate Guanine; Diaziquone; Docetaxel; Doxorubicin; Doxorubicin hydrochloride; Doxorubicin glucuronide; Cyano-morpholinodoxorubicin; 2-pyrrolinodoxorubicin (2P-DOX), droloxifene; droloxifene citrate; Dromostanolone propionate; Duazomycin; Edatrexate; Eflornithine hydrochloride; Elsamitrucin; Enloplatin; Enpromate; Epipropizin; Epirubicin hydrochloride; Epirubicin glucuronide; Elbrozole; Esorubicin hydrochloride; Estrella Mustine;Estramustine phosphate sodium;Etanidazole;Etoposide;Etoposide phosphate;Etoposide glucuronide;Etoprine;Fadrozole hydrochloride;Fazarabine;Fenretinide;Floxuridine (FUdR);3',5'-O-dioleoyl-FudR (FUdR-dO);Fludarabine;Fludarabine phosphate;Fluorouracil;Fluorocitabine;Flutamide;Fluoxymesterone;Fosquidone;Fostriecin sodium;Gemcitabine;Gemcitabine hydrochloride;Hydroxyurea;Hydroxyprogesterone caproate; Idarubicin; Idarubicin hydrochloride; Ifosfamide; Ilmofosine; Interferon alfa-2a; Interferon alfa-2b; Interferon alfa-n1; Interferon alfa-n3; Interferon beta-Ia; Interferon gamma-Ib; Iproplatin; Irinotecan hydrochloride; L-asparaginase; Lanreotide acetate; Letrozole; Leucovorin; Leuprorelin acetate; Liarozole hydrochloride; Lometrexol sodium; Lomustine; Losoxantrone hydrochloride; Masoprocol; Maytansine; Mechlorethamine; Mechlorethamine hydrochloride; Medroxyprogesterone acetate acetate); Megestrol acetate; Melengestrol acetate; Melphalan; Menogaril; Mercaptopurine; 6-mercaptopurine; Methotrexate; Methotrexate sodium; Metoprine; Meturedepa; Mithramycin; Mitindomide; Mitocalcin; Mitochromin; Mitodiline; Mitomarcin; Mitomycin; Mitosper; Mitotane; Mitoxantrone; Mitoxantrone hydrochloride; Mycophenolic acid; Niraparib; Nocodazole; Nogalamycin; Olaparib; Ormaplatin; Oxisuran; Paclitaxel; Pegaspargase; Periomycin; Pentamustine; Peplomycin sulfate; Perfosfamide; Sodium phenylbutyrate, Pipobroman; Piposulfan; Piroxantrone hydrochloride; Plicamycin; Promethazine Stan; Porfimer sodium; Porfiromycin; Prednimustine; Prednisone; Procarbazine; Procarbazine hydrochloride; PSI-341, Puromycin; Puromycin hydrochloride; Pyrazofurin; Ribopurin; Rogletimide; Rucaparib; Safingol; Safingol hydrochloride; Semustine; Semustine streptozocin; Simtrazene; Sparphosate sodium; Sparsomycin; Spirogermanium hydrochloride; Spiromustine; Spiroplatin; Streptonigrin; Streptozocin; Surofenur; Talazoparib; Tallysomycin; Taxol; Taxotere; Tecogalan sodium; Tegafur; Teloxantrone hydrochloride; Temoporfin; Teniposide; Teloxylon; Testolactone; Thiamiprine; Thioguanine;These include, but are not limited to, thiotepa, tiazofurin, tirapazamine, topotecan, topotecan hydrochloride, toremifene citrate, trestron acetate, triciribine phosphate, trimetrexate, trimetrexate glucuronate, tuburozole hydrochloride, uracil mustard, uredepa, vapreotide, veliparib, velcade, verteporfin, vinblastine, vinblastine sulfate, vincristine, vincristine sulfate, vindesine, vindesine sulfate, vinepidine sulfate, vinglicinate sulfate, vinleurosine sulfate, vinorelbine, vinorelbine tartrate, vinrocidine sulfate, vinzolidine sulfate, vorozole, zeniplatin, zinostatin, and zorubicin hydrochloride.

[0263] Other anticancer drugs include 20-epi-1,25-dihydroxyvitamin D3; 5-ethynyluracil; abiraterone; acylfulvene; adecipenol; adzelesin; ALL-TK antagonists; ambamustine; amidox; amifostine; aminolevulinic acid; amrubicin; anagrelide; andrographolide; angiogenesis inhibitors; antagonist D; antagonist G; antarelix; ADMP (anti-dorsalizing morphogenetic protein)-1;Antiestrogens;Antineoplastons;Antisense oligonucleotides;Aphidicolin glycinate;Apoptosis gene modulators;Apoptosis regulators;Apurinic acid;Ara-CDP-DL-PTBA;Arginine deaminase;Asulaculin;Atamestane;Atrimustine;Axinastatin 1;Axinastatin 2;Axinastatin 3;Azasetron;Azatoxin;Azatyrosine;Baccatin III derivatives;Balanol;Batimastat;BCR / ABL antagonists Benzochlorins;Benzoylstaurosporine;Beta-lactam derivatives;Beta-arretin;Betaclamycin B;Betulinic acid;bFGF inhibitors;Bisaziridinylspermine;Bisnafide;Bistraten A;Bortezomib;Brephlate;Budotitane;Buthionine sulfoximine;Calicheamicin;Calcipotriol;Calphostin C;Camptothecin derivatives;Canarypox IL-2;Capecitabine;Carboxamido-amino-triazole;Carboxamidotriazole;CaRest M3; CARN 700; cartilage-derived inhibitors; casein kinase inhibitors (ICOS); castanospermine; cecropin B; cetrorelix; chlorins; chloroquinoxaline sulfonamides; cicaprost; cis-porphyrins; clomiphene analogs; clotrimazole; colismycin A; colismycin B; combretastatin A4; combretastatin analogs; conagenin; clambecidin 816; crisnatol; cryptophycin 8; cryptophycin A derivatives; curacin A; cyclopentaanthraquinones; cycloplatam; cypemycin; cytarabine ocfosfate; cytolytic factors; cytostatin;Dacliximab; Daunomycin; Daunorubicin; Dehydrodidemnin B; Diethylstilbestrol; Deslorelin; Dexamethasone; Dexifosfamide; Dexrazoxane; Dexverapamil; Didemnin B; Didox; Diethylnorspermine; Azacitidine; Dihydro-5-azacytidine; Dihydrotaxol, 9-; Dioxamycin; Diphenylspiromustine; Docosanol; Dracena Tron; Doxifluridine; Dronabinol; Duocarmycin SA; Ebselen; Ecomustine; Edelfosine; Edrecolomab; Eflomitine; Elemene; Emiteflu; Epirubicin; Epristeride; Estramustine analogs; Estrogen agonists; Estrogen antagonists; Etanidazole; Ethinyl estradiol; Etoposide phosphate; Exemestane; Filgrastim; Finasteride; Flavopiridol; Flezelastine; Fluasterone; Fludarabine; Fluorodaunorubicin hydrochloride hydrochloride; forfenimex; formestane; fotemustine; gadolinium texaphyrin; gallium nitrate; galocitabine; ganirelix; gelatinase inhibitors; glutathione inhibitors; hepsulfam; heregulin; hexamethylene bisacetamide; hypericin; ibandronic acid; idoxifene; idramantone; ilmofosine; ilomastat; imidazoacridone azoacridones; imiquimod; immunostimulatory peptides; insulin-like growth factor-I receptor inhibitors; interferon agonists; interferons; interleukins; iobenguane; iododoxorubicin; 4-iomeanol; irinotecan; iroplact; irsogladine; isobengazole; isohomohalichondrin B; itasetron; jasplakinolide; kahalalide F;Lamellarin-N triacetate; lanreotide; leinamycin; lenograstim; lentinan sulfate; leptolstatin; leukemia inhibitory factor; leukocyte alpha interferon; leuprolide + estrogen + progesterone; leuprorelin; levamisole; liarozole; linear polyamine analogs; lipophilic disaccharide peptides; lipophilic platinum compounds; rissoclinamide 7; lobaplatin; lombricin; lometrexol; lonidamine; losoxantrone; lovastatin; loxoribine; lurtotecan; lutetium texaphyrin; lysofylline; lytic peptides; maytansine; mannostatin A; marimastat ;Masoprocol;Maspin;Matrilysin inhibitors;Matrix metalloproteinase inhibitors;Melbarone;Meterelin;Methioninase;Metoclopramide;MIF inhibitors;Mifepristone;Miltefosine;Mirimostim;Incompatible double-stranded RNA;Mitoguazone;Mitolactol;Mitomycin analogs;Mitonafide;Mitotoxin fibroblast growth factor-saporin;Mofalotene;Molgramostim;Monoclonal antibodies, human chorionic gonadotropin;Monophosphoryl lipid A + Mycobacterium cell wall sk;Mopidamol;Multidrug resistance gene inhibitors;MTS1 (multiple Tumor suppressor 1)-based therapy; mustard anticancer compounds; mycaperoxide B; mycobacterial cell wall extract; myriaporone; N-acetyldinaline; N-substituted benzamides; nafarelin; nagrestip; naloxone + pentazocine; napavin; naphterpin; nartograstim; nedaplatin; nemorubicin; neridronic acid; neutral endopeptidase; nilutamide; nisamycin; nitric oxide modulators; nitroxide antioxidants; nitrulline; O6-benzylguanine; octreotide; oxenone; oligonucleotides; onapristone; ondansetron; oracin; oral cytokine inducers; osaterone; oxaliplatin;Oxaunomycin; Paclitaxel analogs; Paclitaxel derivatives; Palauamine; Palmitoylrhizoxin; Pamidronic acid; Panaxytriol; Panomyphen; Parabactin; Pazeliptin; Pegaspargase; Perdecin; Pentosan polysulfate sodium; Pentostatin; Pentrozole; Perflubron; Perfosfamide; Perillyl alcohol; Phenazinomycin; Phenyl acetate; Phosphatase inhibitors; Picibanil; Pilocarpine hydrochloride; Pirarubicin; Piritrexim; Placetin A; Placetin B; Plasminogen activator inhibitors; Platinum complexes; Platinum compounds; Platinum- Triamine conjugates; Porfimer sodium; Porfiromycin; Propyl bis-acridone; Prostaglandin J2; Proteasome inhibitors; Protein A-based immunomodulators; Protein kinase C inhibitors; Microalgae protein kinase C inhibitors; Protein tyrosine phosphatase inhibitors; Purine nucleoside phosphorylase inhibitors; Purpurins; Pyrazoloacridines; Pyridoxylated hemoglobin polyoxyethylene conjugates; RAF antagonists; Raltitrexed; Ramosetron; Ras farnesyl protein transferase inhibitors; Ras inhibitors; Ras-GAP inhibitors; Demethylated retelliptine; Rhenium Re 186 etidronate; rhizoxin; ribozyme; RII retinamide; rohitukine; romurtide; roquinimex; rubiginone B1; ruboxil; saintpine; SarCNU; sarcophytol A; sargramostim; Sdi 1 mimetics; senescence derived inhibitor 1; sense oligonucleotides; signal transduction inhibitors; signal transduction modulators; single-chain antigen binding proteins; sizofuran; SN-38; sobuzoxane; borocaptate sodium; sodium phenylacetate; sorberol; somatomedin binding proteins; sonermin; sparfosic acid; spicamycin D; spiromustine; splenopentin;Spongistatin 1; Squalamine; Stem cell inhibitors; Stem cell division inhibitors; Stipiamide; Stromelysin inhibitors; Sulfinosine; Superactive vasoactive intestinal peptide antagonists; Suradista; Suramin; Swainsonine; Synthetic glycosaminoglycans; Tallimustine; Tamoxifen; Tamoxifen methiodide; Tauromustine; Taxanes; Tazarotene; Tecogalan sodium; Tegafur; Telluropyrylium; Telomerase inhibitors; Temozolomide; Testosterone propionate proprionate, tetrachlorodecaoxide; tetrazomine; thaliblastine; thalidomide; thiocoraline; thrombopoietin; thrombopoietin mimetics; thymalfasin; thymopoietin receptor agonists; thymotrin; thyroid-stimulating hormone; ethyl etiopurpurin tin; titanocene dichloride; topsentin; toremifene; totipotent stem cell factor; translation inhibitors; tretinoin; triacetyluridine; triciribine; tropisetron; turosteride; tyrosine kinase inhibitors; tyrphostins; UBC inhibitors; ubenimex; urogenital sinus The present invention includes, but is not limited to, derived growth inhibitory factors; urokinase receptor antagonists; variolin B; vector systems, erythrocyte gene therapy; velaresol; veramine; verdins; vinorelbine; vinxaltine; vitaxin; zanoterone; zilascorb; zinostatin stimalamer; abrin; ricin; ribonuclease; onconase; rapLR1; DNase I; Staphylococcal enterotoxin-A; pokeweed antiviral protein; gelonin; diphtheria toxin; Pseudomonas aeruginosa exotoxin; and Pseudomonas aeruginosa endotoxin; or combinations thereof.

[0264] In some embodiments, the drugs to be used in combination with the disclosed compounds are duocarmycin and its analogs, dolastatins, combretastatin, calicheamicin, N-acetyl-γ-calicheamycin (CMC), calicheamycin derivatives, maytansine and its analogs, DM-I, auristatin E, auristatin EB (AEB), auristatin EFP (AEFP), monomethylauristatin E (MMAE), monomethylauristatin F (MMAF), tubulysin, disorazole (dis orazole), epothilones, paclitaxel, docetaxel, topotecan, echinomycin, estramustine, cemadotin, eluterobin, methopterin, actinomycin, daunorubicin, daunorubicin conjugates, mitomycin C, mitomycin A, vincristine, retinoic acid, camptothecin, camptothecin derivatives, SN38, maytansine, maytansinoid-type derivatives, DM1, DM4, TK1, amanitin, pyrrolobenzodiazepine, pyrrolobenzodiazepine dimer, methotrexate, ilomedine, aspirin, IMID, lenalidomide, and pomalidomide.

[0265] The compounds of the present disclosure may also be used in combination with any of the following treatments: androgen deprivation techniques and treatment in combination with compounds that target the androgen receptor, including antiandrogens, such as, but not limited to, enzalutamide, apalutamide, darolutamide, and the like.

[0266] Treatment in combination with inhibitors of poly(ADP-ribose) polymerase (PARP), a class of chemotherapy drugs that targets cancers with defective DNA damage repair (Yuan et al., Expert Opin Ther Pat, 2017, 27:363). Such PARP inhibitors include but are not limited to olaparib, rucaparib, velaparib, niraparib, talazoparib, pamiparib, iniparib, E7449 and A-966492.

[0267] For example, treatment in combination with inhibitors of signal transduction pathways and mechanisms that cause DNA single-strand and double-strand break repair, such as nuclear factor-kappa B signal transduction (Pilie et al., Nat Rev Clin Oncol, 2019, 16:81; Zhang et al., Chin J Cancer, 2012, 31:359). Such inhibitors include, but are not limited to, inhibitors of ATM and ATR kinase, checkpoint kinase 1 and 2, DNA-dependent protein kinase and WEE1 kinase (Pilie et al., Nat Rev Clin Oncol, 2019, 16:81).

[0268] These include immune modulators (Khalil et al., Nat Rev Clin Oncol, 2016, 13:394), cancer vaccines (Hollingsworth et al., NPJ Vaccines, 2019, 4:7), immune checkpoint inhibitors (e.g., PD-1, PD-L1, CTLA-4 inhibitors) (Wei et al., Cancer Discov, 2018, 8:1069), cyclin-D kinase 4 / 6 inhibitors (Goel et al., Trends Cell Biol, 2018, 28:911), antibodies capable of binding to tumor cells and / or metastases and inducing antibody-dependent cellular cytotoxicity (ADCC) (Kellner et al., Transfus Med Hemother, 2017, 44:327), T cell or NK cell engagers (e.g., bispecific antibodies) (Yu et al., J Cancer Res Clin Oncol, 2019, 145:941), in combination with cell therapy using expanded autologous or allogeneic immune cells (e.g., chimeric antigen receptor T (CAR-T) cells) (Khalil et al., Nat Rev Clin Oncol, 2016, 13:394). Immune checkpoint inhibitors include, but are not limited to, nivolumab, ipilimumab, pembrolizumab, atezolizumab, avelumab, durvalumab, and cemiplimab.

[0269] According to the present disclosure, the compound can be administered before, simultaneously with, or after other anti-cancer compounds. The administration schedule can include administering different agents in an alternating manner. In other embodiments, the compound can be delivered before and during, or during and after, or before and after, or before and after, and after treatment with other therapies. In some embodiments, the compound is administered more than 24 hours before the administration of other anti-proliferative treatments. In some embodiments, two or more anti-proliferative therapies can be administered to a subject. For example, a subject may receive the compound in combination with both surgery and at least one other anti-proliferative compound. In some embodiments, the compound can be administered in combination with two or more anti-cancer drugs.

[0270] In some embodiments, the compounds of the present disclosure are used to detect PSMA-overexpressing cells and tissues, and such detection is achieved by conjugating detectable labels, such as detectable radionuclides, to the compounds of the present disclosure, or by binding dyes to peptides.In some embodiments, the cells and tissues to be detected are diseased cells and tissues, and / or are one of or the cause of disease and / or disease symptoms, or are part of the underlying pathology of disease.In some embodiments, the diseased cells and tissues cause and / or are part of oncological symptoms (for example, neoplasms, tumors and cancers).

[0271] In some embodiments, the compounds of the present disclosure are used to treat the cells and tissues that overexpress prostate-specific membrane antigen (PSMA).In some embodiments, the cells and tissues that are treated are diseased cells and tissues, and / or are one of or the cause of disease and / or disease symptoms, or are part of the underlying pathology of disease.In some embodiments, the diseased cells and tissues cause and / or are part of oncological symptoms (for example, neoplasm, tumor and cancer), and therapeutic activity is achieved by conjugating therapeutically active nuclides, for example therapeutically active radionuclides, to the compounds of the present disclosure.

[0272] In further embodiments, the compound of the present disclosure is administered in a therapeutically effective amount. In some embodiments, a therapeutically effective amount is a dosage of a compound sufficient to provide a therapeutically or medically desired result or effect in the subject to which the compound is administered. A therapeutically effective amount will vary depending on the specific condition being treated, the age and health of the subject being treated, the severity of the condition, the duration of treatment, the nature of concurrent or combined treatment (if any), the specific route of administration, and other factors within the knowledge and expertise of a medical professional. For example, in the context of a method intended to treat a subject with a condition characterized by abnormal cell proliferation, an effective amount that inhibits proliferation may be an amount sufficient to reduce or completely stop abnormal cell proliferation, for example, to slow down or stop the development or progression of a cell mass such as a tumor. In one embodiment, and as preferably used herein, the term "inhibit" encompasses all of the above.

[0273] In some embodiments, a therapeutically effective amount is the amount necessary to prolong the quiescence of micrometastases or stabilize any residual primary tumor cells following surgery or drug therapy.

[0274] Generally, a therapeutically effective amount may vary based on factors such as the subject's age, condition, and sex, as well as the nature and extent of the disease in the subject, all of which can be determined by one skilled in the art. Dosages can be adjusted by the individual physician or veterinarian, particularly in the event of any complications. In some embodiments, a therapeutically effective amount includes, but is not limited to, an amount within the range of 0.1 μg / kg to about 2000 mg / kg, or 1.0 μg / kg to about 1000 mg / kg, or about 0.1 mg / kg to about 500 mg / kg, or about 1.0 mg / kg to about 100 mg / kg, administered daily in one or more doses for one or several days. If desired, the effective daily dose of the active compound may be administered as two, three, four, five, six, or more subdoses, e.g., administered separately at appropriate intervals throughout the day, optionally in unit dosage form. In some embodiments, the compound is administered for more than 7 days, more than 10 days, more than 14 days, or more than 20 days. In some embodiments, the compound is administered for a period of weeks, months, or years. In some embodiments, the compound is delivered every other day, for example, the agent is delivered every 2 days, or every 3 days, or every 4 days, or every 5 days, or every 6 days, or every week, or every month.

[0275] In some embodiments, the compounds of the present disclosure are for use in the treatment and / or prevention of disease, where such treatment is radionuclide therapy. For example, radionuclide therapy utilizes or is based on various forms of radiation emitted by radionuclides. Such radiation includes, for example, photon radiation, including but not limited to, β -The radiation can be any one of particle and electron radiation including Auger electron radiation, proton radiation, neutron radiation, positron radiation, alpha particle or ion beam radiation.Depending on the type of particle or radiation emitted by the radionuclide, radionuclide therapy can be classified as, for example, photon radionuclide therapy, electron radionuclide therapy, proton radionuclide therapy, neutron radionuclide therapy, positron radionuclide therapy, alpha particle radionuclide therapy or ion beam radionuclide therapy.All these types of radionuclide therapy are encompassed by the present disclosure, and all these types of radionuclide therapy can be realized by the compound of the present disclosure, and the radionuclide bound to the compound of the present disclosure provides this type of radiation.

[0276] Radionuclide therapy preferably works by damaging the DNA of cells.Damage is caused by photons, electrons, protons, neutrons, positrons, alpha particles or ion beams, which directly or indirectly ionize the atoms that make up DNA chains.Indirect ionization occurs as a result of the ionization of water, forming free radicals, especially hydroxyl radicals, which then damage DNA.

[0277] In the most common forms of radionuclide therapy, most of the radiation effects are due to free radicals. Because cells have mechanisms for repairing DNA damage, breaking DNA on both strands proves to be the most important technique in altering cellular characteristics. Because cancer cells are generally undifferentiated and stem cell-like, they are more likely to reproduce and have a reduced ability to repair non-lethal damage compared to most healthy, differentiated cells. DNA damage is inherited through cell division, and damage accumulates in cancer cells, causing them to die or reproduce more slowly.

[0278] Oxygen is a potent radiosensitizer, increasing the effectiveness of a given dose of radiation by forming DNA-damaging free radicals. Therefore, the use of hyperbaric oxygen tanks, hyperoxic blood substitutes, hypoxic cell radiosensitizers such as misonidazole and metronidazole, and hypoxic cytotoxins such as tirapazamine may be applied.

[0279] Other factors considered when selecting the radiation dose include whether the patient is receiving chemotherapy, whether radiation therapy is being administered before or after surgery, and the degree of success of the surgery.

[0280] The total radiation dose may be fractionated, i.e., spread over time across one or more treatments, for one or more of several important reasons. For example, fractionation allows normal cells time to recover, whereas tumor cells generally repair less efficiently between treatments. Also, for example, fractionation allows tumor cells that were in a relatively radioresistant phase of the cell cycle during one treatment to enter a sensitive phase of the cycle before the next treatment is administered. Similarly, tumor cells that were chronically or acutely hypoxic and therefore more radioresistant may be reoxygenated between treatments, improving tumor cell killing.

[0281] It is generally known that various cancers respond differently to radiation therapy. A cancer's response to radiation is described by its radiosensitivity. Highly radiosensitive cancer cells are rapidly killed by moderate doses of radiation. These include leukemias, most lymphomas, and germ cell tumors.

[0282] To some extent, it is important to distinguish the radiosensitivity of a particular tumor, a laboratory measurement, from the "cure potential" of the cancer with an internally delivered dose of radiation in actual clinical practice. For example, because leukemias are dispersed throughout the body, they are generally not curable with radiation therapy. Lymphomas, when localized to one area of ​​the body, may be completely curable. Similarly, many common moderately radiation-responsive tumors can be treated with curative doses of radiation when they are in their early stages. This applies, for example, to non-melanoma skin cancer, head and neck cancer, non-small cell lung cancer, cervical cancer, anal cancer, and prostate cancer.

[0283] Additionally, tumor response to radiation therapy is related to its size. For complex reasons, very large tumors do not respond to radiation as well as smaller tumors or microscopic disease. Various strategies are used to overcome this effect. The most common technique is surgical resection before radiation therapy. This is most commonly seen in the treatment of breast cancer and involves wide local excision or mastectomy followed by adjuvant radiation therapy. Another method is to shrink the tumor with neoadjuvant chemotherapy before radical radionuclide therapy. A third technique is to increase the cancer's radiosensitivity by administering certain drugs during the radiation therapy course. Examples of radiosensitizing drugs include, but are not limited to, cisplatin, nimorazole, and cetuximab.

[0284] Intraoperative radiation therapy is a special type of radiation therapy that is delivered immediately after the surgical removal of the cancer. This method has been used in breast cancer (targeted intraoperative radiotherapy), brain tumors, and rectal cancer.

[0285] Radionuclide therapy itself is painless. Many low-dose palliative treatments cause minimal or no side effects. Treatment with higher doses can cause a variety of side effects during treatment (acute side effects), months or years after treatment (long-term side effects), or after retreatment (cumulative side effects). The nature, severity, and duration of side effects depend on the organ receiving the radiation, the treatment itself (type of radionuclide, dose, fractionation, concurrent chemotherapy), and the patient.

[0286] It is within the scope of this disclosure that the methods for the treatment of diseases of the present invention may implement each and any of the above measures which are known per se in the art and which, to the extent possible, constitute further embodiments of the present disclosure.

[0287] It is also within the scope of the present disclosure that the compounds of the present disclosure are used in methods for diagnosing the diseases disclosed herein, hi some embodiments, such methods comprise administering to a subject in need thereof a diagnostically effective amount of a compound of the present disclosure.

[0288] In accordance with the present disclosure, the imaging method is selected from the group consisting of scintigraphy, single photon emission computed tomography (SPECT), positron emission tomography (PET), computed tomography, and combinations thereof.

[0289] Scintigraphy is a type of diagnostic test or method used in nuclear medicine, in which a radiopharmaceutical is internalized by cells, tissues, and / or organs, for example, in vivo, and the radiation emitted by the internalized radiopharmaceutical is captured by an external detector (gamma camera) to form and display a two-dimensional image.In contrast, SPECT and PET form and display a three-dimensional image.For this reason, SPECT and PET are classified as techniques separate from scintigraphy, but they also use a gamma camera to detect internal radiation.Scintigraphy is different from diagnostic X-ray, in which external radiation passes through the body to form an image.

[0290] Single-photon emission computed tomography (SPECT) scans are a type of nuclear imaging technique that uses gamma rays. They are very similar to conventional nuclear medicine planar imaging, which uses a gamma camera. Before a SPECT scan, the patient is injected with a radiolabeled chemical that emits gamma rays that can be detected by the scanner. A computer collects information from the gamma camera and converts it into two-dimensional slices. These slices can be realigned to form a three-dimensional image of the organ or tissue. SPECT involves the detection of gamma rays emitted singly and sequentially by radionuclides provided by the radiolabeled chemical. To acquire a SPECT image, the gamma camera rotates around the patient. Projections are acquired at specified points during the rotation, typically every 3–6 degrees. In most cases, a full 360-degree rotation is used to obtain an optimal reconstruction. The time it takes to acquire each projection is variable, but 15–20 seconds is typical. This results in a total scan time of 15–20 minutes. Multihead gamma cameras are faster. SPECT acquisition is very similar to planar gamma camera imaging, so the same radiopharmaceuticals can be used.

[0291] Positron emission tomography (PET) is a noninvasive diagnostic imaging technique for measuring the biochemical state or metabolic activity of cells in the human body. PET is unique because it produces images of the body's basic biochemistry or function. Traditional diagnostic techniques, such as X-rays, computed tomography scans, or MRI, produce images of the body's anatomical structures or structures. The premise of these techniques is that any changes in the structure or anatomy associated with disease can be seen. Also, biochemical processes, altered by disease, may occur before any visible changes in the anatomy. PET is an imaging technique that can visualize some of these early biochemical changes. PET scanners create images by relying on radiation emitted by the patient. Each patient is given a minute amount of a radiopharmaceutical that mimics a natural substance used by the body or that specifically binds to a receptor or molecular structure. As the radioisotope undergoes positron-emitting decay (also known as positive beta decay), it emits a positron, the antiparticle of the electron. After traveling up to several millimeters, the positron encounters and annihilates an electron, generating a pair of counter-traveling (gamma) photons. These are detected when they reach the scintillation material in the examination device and create a burst of light, which is detected by a photomultiplier tube or silicon avalanche photodiode. The technique relies on coincidence or coincidence detection of photon pairs. Unpaired photons, i.e., photons that do not pair within a few nanoseconds, are ignored. All coincidences are forwarded to an image processing unit, where the final image data is generated using image reconstruction techniques.

[0292] SPECT / computed tomography and PET / computed tomography are combinations of SPECT and PET with computed tomography. A significant advantage of combining these modalities is improved reader confidence and accuracy. In traditional PET and SPECT, the limited number of photons emitted from abnormal regions creates a very low level of background that makes it difficult to localize the region anatomically. The addition of computed tomography helps determine the location of the abnormal region from an anatomical perspective and categorize the likelihood that this represents disease.

[0293] It is within the scope of the present disclosure that the methods for diagnosing diseases of the present disclosure may implement each and any of the above measures which are known per se in the art and which to the extent constitute further embodiments of the present disclosure.

[0294] In some embodiments, the compounds of the present disclosure may be useful for stratifying patients, i.e., creating subsets within a patient population that provide more detailed information about how patients will respond to a given drug. Stratification may be a crucial component for converting a clinical trial from one with a negative or neutral outcome to one with a positive outcome by identifying the subset of the population most likely to respond to a new treatment.

[0295] Stratification involves identifying groups of patients with shared "biological" characteristics in order to select optimal management for the patient and achieve the best possible outcome in terms of risk assessment, risk prevention, and achieving optimal treatment outcomes.

[0296] In some embodiments, the compounds of the present disclosure may be used to assess or detect a particular disease as early as possible (which are diagnostic uses), the risk of developing the disease (which are susceptibility / risk uses), the progression of the disease, including whether it will be low-grade or high-grade (which are prognostic uses), or it may be used to predict the response and toxicity to a given treatment (which are predictive uses).

[0297] In addition, the compounds of the present disclosure can be used in theragnostics method.The concept of theragnostics is to combine a therapeutic agent with a corresponding diagnostic test, which can increase the clinical use of the therapeutic agent.The concept of theragnostics is becoming increasingly attractive and is widely considered to be important for improving the efficiency of drug treatment by helping doctors identify patients who may benefit from a given treatment, and therefore avoid unnecessary treatment.

[0298] The concept of theragnostics is to combine therapeutic agents with diagnostic tests that allow physicians to identify patients who will benefit most from a given treatment. In one embodiment, the compounds of the present disclosure are used to diagnose patients, i.e., to identify and localize the primary tumor mass and potential local and distant metastases. Furthermore, tumor volume can be determined, particularly using three-dimensional diagnostic modalities such as SPECT or PET. Only patients with PSMA-positive tumor masses and therefore likely to benefit from a given treatment are selected for a specific treatment, thus avoiding unnecessary procedures. For example, such treatment is PSMA-targeted therapy using the compounds of the present disclosure. In some embodiments, chemically identical tumor-targeted diagnostics are applied, including imaging diagnostics such as scintigraphy, PET, or SPECT and radiotherapy. Such compounds differ only in the radionuclide and therefore usually have very similar or otherwise identical pharmacokinetic profiles. This can be achieved using a chelator and a diagnostic or therapeutic radiometal. Alternatively, this can be achieved by using a precursor for radiolabeling and radiolabeling with either a diagnostic or therapeutic radionuclide. In one embodiment, diagnostic imaging is used by means of quantification of diagnostic radionuclide radiation and subsequent dosimetry as known to those skilled in the art, and prediction of drug concentrations in tumors relative to organs susceptible to side effects, thus achieving truly personalized drug therapy for patients.

[0299] In some embodiments, the theragnostic method is achieved with a single theragnostically active compound, such as a compound of the present disclosure labeled with a radionuclide that emits diagnostically detectable radiation (e.g., positrons or gamma rays) and therapeutically effective radiation (e.g., electrons or alpha particles).

[0300] The present disclosure also contemplates methods for intraoperatively identifying / disclosing diseased tissues expressing PSMA in a subject, using compounds of the present disclosure, wherein in some embodiments, such compounds of the present disclosure comprise a diagnostically active agent, e.g., a diagnostically active radionuclide.

[0301] In accordance with further embodiments of the present disclosure, the compounds of the present disclosure, particularly when complexed with a radionuclide, may be used as an adjunct or adjuvant to any other tumor treatment, including surgery as the primary method of treatment for most isolated solid cancers; radiation therapy, which includes the use of ionizing radiation in an attempt to cure or ameliorate cancer symptoms, using either a sealed internal radiation source in the form of brachytherapy, or external radiation; chemotherapy, such as alkylating agents, antimetabolites, anthracyclines, plant alkaloids, topoisomerase inhibitors and other antitumor agents; hormonal treatments, which modulate the behavior of tumor cells without directly attacking them; targeted agents, which directly target molecular abnormalities in certain types of cancer, including monoclonal antibodies and tyrosine kinase inhibitors; angiogenesis inhibitors; immunotherapy; cancer vaccination; palliative care, which includes actions that reduce physical, emotional, spiritual and psychosocial distress to improve a patient's quality of life; and alternative treatments, which include a diverse group of health care systems, practices and products that are not part of conventional medicine.

[0302] In one embodiment of the method of the present disclosure, object is patient.In one embodiment, patient is diagnosed with disease, or suspected with disease, or has the object of disease or risk of developing disease, wherein disease is the disease described herein, and disease is involved in prostate specific membrane antigen (PSMA).

[0303] When a radionuclide is used, and more specifically, when it is bound to or part of the compound of the present disclosure, the dosage used in carrying out the method for treatment and diagnosis will vary depending on, for example, the specific condition to be treated, such as the known radiosensitivity of the tumor type, the tumor volume, and the desired treatment. Generally, the dose is calculated based on the radioactive distribution to each organ and the observed target uptake. The γ-emitting complex can be administered once or several times for diagnostic imaging. In animals, the dose ranges shown include, for example, but are not limited to, 111 In or 89 For example, 0.1 ng / kg to 5 mg / kg of a compound of the present disclosure complexed with 1 kBq to 200 MBq of a gamma-emitting radionuclide, including Zr. Alpha- or beta-emitting complexes of compounds of the present disclosure can be administered at several time points, for example, over a period of 1 to 3 weeks or longer. In animals, the indicated dosage ranges include, but are not limited to, 225 Ac or 177 For example, 0.1 ng / kg to 5 mg / kg of a compound of the present disclosure complexed with 1 kBq to 200 MBq of an α- or β-emitting radionuclide, including Lu. In larger mammals, including humans, indicated dosage ranges include, but are not limited to, 111 In or 89 For example, 0.1 ng / kg to 5 mg / kg, or for example, 0.1 ng / kg to 100 μg / kg of a compound of the present disclosure complexed with 10 to 1000 MBq of a γ-emitting radionuclide, including Zr. In larger mammals, including humans, indicated dosage ranges include, but are not limited to, 225 Ac or177 The compound of the present disclosure may be, for example, 0.1 ng / kg to 5 mg / kg, or for example, 0.1 ng / kg to 100 μg / kg, complexed with 1 to 100,000 MBq of an α- or β-emitting radionuclide, including Lu.

[0304] In certain embodiments, uptake can be measured in terms of absorbed dose (mGy / MBq), SUVmax, and / or SUVmean. In animals, uptake across tissues is reported as a percentage of the injected dose / gram (%ID / g). Sensitivity to radiation is tumor and non-tumor tissue dependent. The favorable tumor versus non-tumor tissue uptake of the present compounds allows for the delivery of radioactive nuclides at doses that can reduce tumor growth or partially or completely destroy tumors. At such doses, permanent or definitive damage to non-tumor tissues is not expected.

[0305] In a further aspect, the present disclosure relates to compositions and pharmaceutical compositions, particularly comprising the compounds of the present disclosure. The pharmaceutical compositions of the present disclosure comprise at least one compound of the present disclosure and, optionally, one or more carrier substances, excipients, and / or adjuvants. The pharmaceutical compositions may further comprise, for example, one or more of water, a buffer solution such as neutral buffered saline or phosphate buffered saline, ethanol, mineral oil, vegetable oil, dimethyl sulfoxide, a carbohydrate such as glucose, mannose, sucrose, or dextran, mannitol, a protein, an adjuvant, a polypeptide, or an amino acid such as glycine, an antioxidant, a chelating agent such as EDTA, or glutathione, and / or a preservative. In addition, one or more other active ingredients may, but need not, be included in the pharmaceutical compositions of the present disclosure.

[0306] The pharmaceutical composition of the present disclosure can be formulated for any suitable administration route, including, for example, topical, oral, sublingual, nasal, vaginal, rectal or parenteral administration, for example, transdermal or ocular administration.In one embodiment, and as preferably used herein, the term parenteral includes subcutaneous, intradermal, intravascular, for example, intravenous, intramuscular, intrathecal and intraperitoneal injection, and any similar injection or infusion technique.In some embodiments, the administration route is intravenous administration.

[0307] In one embodiment of the present disclosure, the compounds of the present disclosure containing radionuclides are administered by any conventional route, particularly intravenously, for example, in the form of an injectable solution or suspension. The compounds of the present disclosure may also be advantageously administered by infusion, for example, by infusion over a period of 30 to 60 minutes.

[0308] In some embodiments, depending on the location of the tumor, the compounds of the present disclosure may be administered as close to the tumor site as possible, for example, by means of a catheter. Such administration may be directly into the tumor tissue, into surrounding tissue, or into afferent blood vessels. The compounds of the present disclosure may also be administered repeatedly, in doses that, in some embodiments, include administration in fractionated doses.

[0309] According to one embodiment of the present disclosure, the pharmaceutical composition of the present disclosure comprises a stabilizer, such as a free radical scavenger, that inhibits the self-radiolysis of the compound of the present disclosure.Suitable stabilizers include, for example, serum albumin, ascorbic acid, retinol, gentisic acid or their derivatives, or commercially available amino acid infusions that do not contain electrolytes and glucose, for example, amino acid infusions used for parenteral protein supplementation, such as Proteinsteril® KE Nephro.In some embodiments, ascorbic acid and gentisic acid are used.

[0310] The pharmaceutical compositions of the present disclosure may contain additional additives, such as agents for adjusting the pH to 7.2-7.4, such as sodium or ammonium acetate or Na2HP04. In some embodiments, a stabilizer is added to the non-radioactive compound of the present disclosure, and the introduction of the radionuclide, e.g., complexation with the radionuclide, is carried out in the presence of the stabilizer at room temperature or at a temperature of, e.g., 40-120°C. Complexation can be conveniently carried out under air-free conditions, e.g., under N2 or Ar. In some embodiments, an additional stabilizer can be added to the composition after complexation.

[0311] Elimination of the compounds of the present disclosure occurs primarily through the kidneys, especially when the compounds contain radionuclides. In some embodiments, further protection of the kidney from radioactive accumulation can be achieved by administering lysine or arginine, or an amino acid solution containing a high content of lysine and / or arginine, such as commercially available amino acid solutions such as Synthamin®-14 or -10, before or together with the injection of the compounds of the present disclosure, especially when the compounds contain radionuclides. In some embodiments, kidney protection can also be achieved by administering a plasma expander, such as gelofuscin, instead of or in addition to an amino acid infusion. In some embodiments, kidney protection can also be achieved by administering a diuretic, which provides a means of forced diuresis by increasing the rate of urination. Such diuretics include high-ceiling loop diuretics, thiazides, carbonic anhydrase inhibitors, potassium-sparing diuretics, calcium-sparing diuretics, osmotic diuretics, and low-ceiling diuretics. In some embodiments, the pharmaceutical compositions of the present disclosure may contain, in addition to a compound of the present disclosure, at least one of these additional compounds intended for or suitable for renal protection, including, for example, renal protection of a subject to whom a compound of the present disclosure is administered.

[0312] It is understood by those skilled in the art that the compounds of the present disclosure are disclosed herein for use in various methods.It is further understood by those skilled in the art that the compositions of the present disclosure and the pharmaceutical compositions of the present disclosure can be equally used in the various methods.It is also understood by those skilled in the art that the compositions of the present disclosure and the pharmaceutical compositions can be equally used in the various methods.It is also understood by those skilled in the art that the compounds of the present disclosure can be equally used in the various methods.

[0313] Those skilled in the art will recognize that the compositions and / or pharmaceutical compositions disclosed herein may contain one or more additional compounds in addition to the compounds of the present disclosure. As long as such one or more additional compounds are disclosed herein as being part of the compositions and / or pharmaceutical compositions of the present disclosure, it is understood that such one or more additional compounds may be administered to a subject exposed to or subjected to the methods of the present disclosure separately from the compounds of the present disclosure. Such administration of one or more additional compounds may occur before, simultaneously with, or after administration of the compounds of the present disclosure. It will also be recognized by those skilled in the art that, in addition to the compounds of the present disclosure, one or more additional compounds may be administered to a subject in the methods of the present disclosure. Such administration of one or more additional compounds may occur before, simultaneously with, or after administration of the compounds of the present disclosure. As long as such one or more additional compounds are disclosed herein as being administered as part of the methods of the present disclosure, it is understood that such one or more additional compounds are part of the compositions and / or pharmaceutical compositions of the present disclosure. It is within the scope of the present disclosure that the compounds of the present disclosure and one or more additional compounds may be contained in the same or different formulations. It is also within the scope of the present disclosure that the compound of the present disclosure and the one or more additional compounds are not contained in the same formulation, but are contained in the same package that contains a first formulation comprising the compound of the present disclosure and a second formulation comprising the one or more additional compounds, and the types of formulations may be the same or different.

[0314] It is within the scope of the present disclosure that more than one compound of the present disclosure may be included in a composition of the present disclosure and / or a pharmaceutical composition of the present disclosure, and that more than one compound of the present disclosure may be used, and preferably administered, in a method of the present disclosure.

[0315] It will be appreciated that the compositions of the present disclosure and pharmaceutical compositions of the present disclosure may be prepared in conventional manner. Radiopharmaceuticals have a radioactive content that decreases over time as a result of radioactive decay. The physical half-life of the radionuclide is often short for radiopharmaceutical diagnostic agents. In these cases, final preparation must be carried out shortly before administration to the patient. This is particularly the case for positron-emitting radiopharmaceuticals for tomography (PET radiopharmaceuticals). This often leads to the use of semi-finished products, such as radionuclide generators, radioactive precursors, and kits.

[0316] In some embodiments, kits of the present disclosure, in addition to one or more compounds of the present disclosure, typically include at least one of the following: instructions for use, final preparation and / or quality control controls, one or more optional excipients, one or more optional reagents for a labeling procedure, optionally one or more radionuclides with or without a sealed container, and optionally one or more devices, wherein the device is selected from the group including a labeling device, a purification device, an analytical device, a manipulation device, a radiation protection device, or an administration device.

[0317] Sealed containers known as "pigs" for general handling and transport of radiopharmaceutical containers come in a variety of configurations for holding radiopharmaceutical containers such as bottles, vials, syringes, etc. One type includes a removable cover that allows access to the held radiopharmaceutical container. When the pig cover is in situ, radiation exposure is acceptable.

[0318] In some embodiments, the labeling device is selected from the group of an open reactor, a closed reactor, a microfluidic system, a nanoreactor, a cartridge, a pressure vessel, a vial, a temperature-controllable reactor, a mixing or shaking reactor, and combinations thereof.

[0319] In some embodiments, the purification device is selected from the group of an ion exchange chromatography column or device, a size exclusion chromatography column or device, an affinity chromatography column or device, a gas or liquid chromatography column or device, a solid phase extraction column or device, a filtration device, a centrifuge vial column or device, and combinations thereof.

[0320] In some embodiments, the analytical device is selected from the group of tests or test devices for determining the identity, radiochemical purity, radionuclide purity, radioactive content, and specific radioactivity of a radiolabeled compound, and combinations thereof.

[0321] In some embodiments, the manipulation device is selected from the group consisting of devices for mixing, diluting, dispensing, labeling, injecting and administering radiopharmaceuticals to a subject, and combinations thereof.

[0322] In some embodiments, radiation protection devices are used to protect physicians and other personnel from radiation when using therapeutic or diagnostic radionuclides. In some embodiments, the radiation protection device is selected from the group consisting of devices having a protective wall of radiation absorbing material selected from the group consisting of aluminum, plastics, wood, lead, iron, leaded glass, water, rubber, plastic, and cloth, devices that ensure sufficient distance from the radiation source, devices that reduce exposure time to the radionuclide, devices that limit inhalation, ingestion, or other modes of entry of radioactive material into the body, and devices that provide a combination of these measures.

[0323] In some embodiments, the administration device is selected from the group of syringes, shielded syringes, needles, pumps, and infusion devices, and combinations thereof. Syringe shields are typically hollow cylindrical structures that house a cylindrical syringe and are constructed from lead or tungsten with a lead-glass window that allows the operator to view the syringe plunger and the liquid volume within the syringe. [Example]

[0324] The following examples are included to provide guidance to those skilled in the art for carrying out representative embodiments of the presently disclosed subject matter. In light of this disclosure and the general level of skill in the art, those skilled in the art will understand that the following examples are intended to be merely illustrative, and that many changes, modifications, and variations can be used without departing from the scope of the presently disclosed subject matter. The following general description and specific examples are intended for illustrative purposes only and should not be construed as limiting in any way to prepare compounds of the present disclosure by other methods.

[0325] Abbreviations used in this application and particularly in the examples below are as follows:

[0326] [Table 7-1]

[0327] [Table 7-2]

[0328] [Table 7-3]

[0329] [Table 7-4]

[0330] Example 1 Materials, equipment and methods The materials and methods and general procedures are further illustrat...

Claims

1. Compounds of formula (I) 【Chemical 1】 {During the ceremony, X is a bond and —CH ２ - selected from the group consisting of; Z １ is selected from the group consisting of a chelator and NT; NT is selected from the group consisting of H, Ac, Hex, HPA, HO-succinyl, SaPr, Iva, HYDAc, Bio, nBuCAyl, AF488Ahx, and Hib; L １ is a bond and -(Xaa1) ｋ - selected from the group consisting of k is selected from the group consisting of 1, 2 and 3; Xaa1 is each and individually an amino acid residue, preferably said amino acid residue is an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI) 【Chemistry 2】 is selected from the group consisting of g is an integer selected from the group consisting of 0 to 23; where: When k=1, Xaa1 is Z １ is covalently linked to Xaa2, When k=2, the first of the two Xaa1 is Z １ is covalently bound to the second of the two Xaa1's, the second of the two Xaa1's is covalently bound to the first of the two Xaa1's and is covalently bound to Xaa2; When k=3, the first of the three Xaa1 is Z １ covalently bound to the second of said three Xaa1, said second of said three Xaa1 being covalently bound to said first of said three Xaa1 and covalently bound to the third of said three Xaa1, said third of said three Xaa1 being covalently bound to said second of said three Xaa1 and covalently bound to Xaa2; Here, L １ is a bond, Z １ is NT; Xaa2 is a group represented by formula (II) and formula (III): 【Chemistry 3】 is selected from the group consisting of Here, R ２ａ is H, (C １ ~C ６ ) alkyl and CH ２ R ２ｇ selected from the group consisting of: R ２ｇ is OH and CO ２ H; R ２ｂ is H and (C １ ~C ６ ) alkyl; Or alternatively, R ２ａ and R ２ｂ may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R ２ｃ is H and CH ３ selected from the group consisting of: R ２ｄ is selected from the group consisting of H, F and OH; R ２ｅ is selected from the group consisting of H and F; R ２ｆ is H and CH ３ selected from the group consisting of: However, L １ is the binding and NT is Hib, then Xaa2 may be absent; Xaa3 is a group represented by formula (IV): 【Chemistry 4】 is selected from Here, R ３ａ is aryl, (C ５ ~C ６ ) heteroaryl, indol-3-yl, 6-chloro-1H-indol-3-yl and —S—CH ２ -phenyl; R ３ａ The aryl or heteroaryl rings are independently selected from halogen, (C １ ~C ６ ) alkyl, CN, OH and —O(C １ ~C ３ ) alkyl, wherein the (C １ ~C ６ ) alkyl may be substituted with one or more fluorines; R ３ｂ is H and CH ３ selected from the group consisting of: h is selected from the group consisting of 1 and 2; Xaa5 is a group represented by formula (Va) or (Vb): 【Chemistry 5】 selected from the group consisting of Hgn, lys, Nle, Tap, Aph and Gln; Here, R ５ａ is H, (C １ ~C ６ ) alkyl, Ac, C(=NR ５ｄ ) NR ５ｅ R ５ｆ and Bio; R ５ｄ is H and CH ３ selected from the group consisting of: R ５ｅ and R ５ｆ are independently H and (C １ ~C ６ ) alkyl; R ５ｂ is H and (C １ ~C ６ ) alkyl; R ５ｃ is H and CH ３ selected from the group consisting of: m is selected from the group consisting of 2, 3, 4 and 5; and R ５ｇ , R ５ｈ and R ５ｉ are independently １ ~C ６ ) alkyl; Xaa6 is represented by formula (VI), formula (VII): 【Chemistry 6】 selected from the group consisting of Nle and arg; Here, R ６ａ is H, C (=NR ６ｅ ) NR ６ｆ R ６ｇ , C(=O)R ６ｈ and pyridyl; R ６ｅ is H and CH ３ selected from the group consisting of: R ６ｆ is H, (C １ ~C ６ ) Alkyl, Ac, NO ２ and C(═O)NR ６ｉ R ６ｊ selected from the group consisting of: R ６ｉ and R ６ｊ are independently H and (C １ ~C ２ ) alkyl; R ６ｇ is H and (C １ ~C ６ ) alkyl; Or alternatively, R ６ｅ and R ６ｆ may together form a 5- or 6-membered heterocycle; R ６ｈ is (C １ ~C ６ ) alkyl, NR ６ｋ R ６ｍ and N.R. ６ｎ C (=NR ６ｐ ) NR ６ｑ R ６ｒ selected from the group consisting of: R ６ｋ and R ６ｍ are independently H and (C １ ~C ６ ) alkyl; R ６ｎ and R ６ｐ are independently H and CH ３ selected from the group consisting of: R ６ｑ and R ６ｒ are independently H and (C １ ~C ６ ) alkyl; R ６ｂ is H and (C １ ~C ６ ) alkyl; R ６ｃ is H and CH ３ selected from the group consisting of: n is selected from the group consisting of 1, 2, 3 and 4; R ６ｄ is NR ６ｓ C (=NR ６ｔ ) NR ６ｕ R ６ｖ , OH and NR ６ｗ R ６ｘ selected from the group consisting of: R ６ｓ and R ６ｔ are independently H and CH ３ selected from the group consisting of: R ６ｕ , R ６ｖ , R ６ｗ and R ６ｘ are independently H and (C １ ~C ６ ) alkyl; q is selected from the group consisting of 2, 3, and 4; Xaa7 is an amino acid residue, and the amino acid residue is preferably a residue represented by formula (VIII), formula (IX), formula (X), or formula (XI): 【Chemistry 7】 Dtc and Oic; Here, R ７ａ is H, (C １ ~C ６ ) alkyl and (CH ２ ) ｔ R ７ｇ selected from the group consisting of: R ７ｇ OH, CO ２ H and NR ７ｈ R ７ｉ selected from the group consisting of: R ７ｈ and R ７ｉ are independently H and (C １ ~C ６ ) alkyl; t is selected from the group consisting of 1, 2, 3 and 4; R ７ｂ is H and (C １ ~C ６ ) alkyl; Or alternatively, R ７ａ and R ７ｂ may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R ７ｃ is H and CH ３ selected from the group consisting of: R ７ｄ is selected from the group consisting of H, F and OH; R ７ｅ is selected from the group consisting of H and F; R ７ｆ is H and CH ３ selected from the group consisting of: u is selected from the group consisting of 2, 3 and 4; L ３ is a bond and -(Xab1) ｖ - selected from the group consisting of v is selected from the group consisting of 1, 2 and 3; Xabl is each and individually an amino acid residue, preferably said amino acid residue is selected from the group consisting of an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI); When v=1, Xab1 is Z ３ and covalently bonded to a side chain amino functionality of formula (X) or of formula (XI), When v=2, the first of the two Xab1 is Z ３ covalently bonded to the second of the two Xab1s, the second of the two Xab1s being covalently bonded to the first of the two Xab1s, and covalently bonded to a side chain amino functional group of formula (X) or formula (XI), When v=3, the first of the three Xab1 is Z ３ covalently bonded to the second of the three Xab1s, the second of the three Xab1s is covalently bonded to the first of the three Xab1s, the third of the three Xab1s is covalently bonded to the second of the three Xab1s, and the third of the three Xab1s is covalently bonded to the second of the three Xab1s, and is covalently bonded to a side chain amino functional group of formula (X) or formula (XI); Z ３ is selected from the group consisting of H and a chelator; Xaa8 is an α-amino acid residue, and the α-nitrogen atom of Xaa8 is unsubstituted or is CH ３ may be substituted by Xaa10 is a group represented by formula (XII): 【Chemistry 8】 and where: R １０ａ is (C １ ~C ６ ) alkyl; R １０ｂ is H and (C １ ~C ６ ) alkyl; Or alternatively, R １０ａ and R １０ｂ may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R １０ｃ is H and CH ３ selected from the group consisting of: L ２ teeth, bond and -Xaa11-(Xaa12) ｓ -wherein Xaa11 is covalently linked to Xaa10; Xaa11 is an amino acid residue, said amino acid residue is preferably selected from the group consisting of an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI); s is selected from the group consisting of 0, 1, 2, 3, 4 and 5; Xaa12 are each and individually an amino acid residue, said amino acid residue being preferably selected from the group comprising an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI), When s=0, Xaa11 is Z ２ is covalently bonded to When s=1, Xaa12 is covalently linked to Xaa11, and Z ２ is covalently bonded to When s=2, the first of the two Xaa12 is covalently bound to Xaa11, the second of the two Xaa12 is covalently bound to Xaa11, the second of the two Xaa12 is covalently bound to the first of the two Xaa12, and Z ２ is covalently bonded to When s=3, the first of the three Xaa12 is covalently bound to Xaa11 and is covalently bound to the second of the three Xaa12, the second of the three Xaa12 is covalently bound to the first of the three Xaa12 and is covalently bound to the third of the three Xaa12, and the third of the three Xaa12 is covalently bound to the second of the three Xaa12; Z ２ is covalently bonded to When s=4, the first of the four Xaa is covalently bonded to Xaa and is covalently bonded to the second of the four Xaa, the second of the four Xaa is covalently bonded to the first of the four Xaa and is covalently bonded to the third of the four Xaa, the third of the four Xaa is covalently bonded to the second of the four Xaa and is covalently bonded to the fourth of the four Xaa, and the fourth of the four Xaa is covalently bonded to the third of the four Xaa; ２ is covalently bonded to When s=5, the first of the five Xaa is covalently bonded to Xaa, the second of the five Xaa is covalently bonded to the first of the five Xaa, the third of the five Xaa, the third of the five Xaa is covalently bonded to the second of the five Xaa, the fourth of the five Xaa, the fourth of the five Xaa is covalently bonded to the third of the five Xaa, the fifth of the five Xaa, the fifth of the five Xaa is covalently bonded to the fourth of the five Xaa; ２ is covalently bonded to; Z ２ comprises a CT, an XDa-chelator and an α-amino acid residue of formula (CT-I): 【Chemistry 9】 is selected from the group consisting of CT is represented by formula (CT-II) or (CT-III): 【Chemistry 10】 AF488N3K-NH ２ , OH and Throl-OH; where: R ＣＴ１ is H and CH ３ selected from the group consisting of: R ＣＴ２ is H and (C １ ~C ６ ) alkyl; R ＣＴ３ and R ＣＴ４ are each and individually H and CH ３ selected from the group consisting of: R ＣＴ５ is H and (C １ ~C ６ ) alkyl; x is selected from the group consisting of 2 to 10; XDa is a diamine, said diamine preferably being selected from the group consisting of en and Ape; w is selected from the group consisting of 1, 2, 3, 4, 5 and 6; L ４ is a bond and -(Xac1) ｙ - selected from the group consisting of where: y is selected from the group consisting of 0, 1, 2 and 3; Xac1 is each and individually an amino acid residue, preferably said amino acid residue is selected from the group comprising an α-amino acid residue, a β-amino acid residue, a γ-amino acid residue, a δ-amino acid residue, an ε-amino acid residue, an ω-amino acid residue and an amino acid residue of formula (YI), When y=0, the side chain amino functional group of the α-amino acid residue of formula (CT-I) is Z ４ is covalently bonded to When y=1, Xac1 is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), and Z ４ is covalently bonded to When y=2, the first of the two Xac1s is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), the second of the two Xac1s is covalently bonded to the first of the two Xac1s, and Z ４ is covalently bonded to When y=3, the first of the three Xac1s is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), the second of the three Xac1s is covalently bonded to the first of the three Xac1s, the third of the three Xac1s is covalently bonded to the second of the three Xac1s, and the third of the three Xac1s is covalently bonded to the second of the three Xac1s; Z ４ is covalently bonded to When y=4, the first of the four Xac1's is covalently bonded to the side chain amino functional group of the α-amino acid residue of formula (CT-I), the second of the four Xac1's is covalently bonded to the first of the four Xac1's, the third of the four Xac1's is covalently bonded to the second of the four Xac1's, the fourth of the four Xac1's is covalently bonded to the third of the four Xac1's, and the fourth of the four Xac1's is covalently bonded to the third of the four Xac1's; and Z ４ is covalently bonded to; Z ４ is selected from the group consisting of H and a chelator; However, L ２ is a bond, CT is represented by formula (CT-II), wherein R ＣＴ１ is H and CH ３ and R ＣＴ２ But (C ４ ~C ６ ) When Xaa10 is alkyl, Xaa10 may be absent. or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, which may contain a therapeutically active nuclide or a diagnostically active nuclide.

2. Compounds of formula (I) 【Chemistry 11】 {During the ceremony, X is a bond and —CH ２ - selected from the group consisting of; Z １ is selected from the group consisting of a chelator and NT; NT is selected from the group consisting of H, Ac, Hex, HPA, HO-succinyl, SaPr, Iva, HYDAc, Bio, nBuCAyl, AF488Ahx, and Hib; L １ is a bond and -(Xaa1) ｋ - selected from the group consisting of; k is selected from the group consisting of 1, 2 and 3; where: When k=1, Xaa1 is Z １ is covalently linked to Xaa2, when k=2, one of the two Xaa1's is covalently bonded to Z1 and covalently bonded to the second of the two Xaa1's, and the second of the two Xaa1's is covalently bonded to the first of the two Xaa1's and covalently bonded to Xaa2; when k=3, the first of the three Xaa1 is covalently bonded to Z1 and is covalently bonded to the second of the three Xaa1, the second of the three Xaa1 is covalently bonded to the first of the three Xaa1 and is covalently bonded to the third of the three Xaa1, and the third of the three Xaa1 is covalently bonded to the second of the three Xaa1 and is covalently bonded to Xaa2; Here, L １ is a bond, Z １ is NT; Xaa1 is each and individually selected from the group consisting of Thr, Ala, Ser, Pamp, Leu, He, Nmt, Pamb, Ahx, APAc, PPAc, Bal, Cmp, Pab, O2Oc, Met, and Ttds; Xaa2 is selected from the group consisting of Aib, Ala, Amd, Ams, amd, ams, Deg, Nmg, Pam, and Pro; １ is the binding and NT is Hib, then Xaa2 may be absent; Xaa3 is selected from the group consisting of Phe, Nmf, 1Ni, 2Ni, 6Clw, Cys(Bzl), Hfe, Trp, Mpa, Opa, and Ppa; Phe, Nmf, and Hfe are independently selected from halogen, CH ３ , C.N., C.F. ３ and OH; Xaa5 is a group represented by formula (Va) or (Vb): 【Chemistry 12】 selected from the group consisting of Hgn, lys, Nle, Tap, Aph and Gln; Here, R ５ａ is H, (C １ ~C ６ ) alkyl, Ac, C(=NR ５ｄ ) NR ５ｅ R ５ｆ and Bio; R ５ｄ is H and CH ３ selected from the group consisting of: R ５ｅ and R ５ｆ are independently H and (C １ ~C ６ ) alkyl; R ５ｂ is H and (C １ ~C ６ ) alkyl; R ５ｃ is H and CH ３ selected from the group consisting of: m is selected from the group consisting of 2, 3, 4 and 5; R ５ｇ , R ５ｈ and R ５ｉ are independently １ ~C ６ ) alkyl; Xaa6 is represented by formula (VI), formula (VII): 【Chemistry 13】 selected from the group consisting of Nle and arg; Here, R ６ａ is H, C (=NR ６ｅ ) NR ６ｆ R ６ｇ , C(=O)R ６ｈ and pyridyl; R ６ｅ is H and CH ３ selected from the group consisting of: R ６ｆ is H, (C １ ~C ６ ) Alkyl, Ac, NO ２ and C(=O)NR ６ｉ R ６ｊ selected from the group consisting of: R ６ｉ and R ６ｊ are independently H and (C １ ~C ２ ) alkyl; R ６ｇ is H and (C １ ~C ６ ) alkyl; Or alternatively, R ６ｅ and R ６ｆ may together form a 5- or 6-membered heterocycle; R ６ｈ is (C １ ~C ６ ) alkyl, NR ６ｋ R ６ｍ and N.R. ６ｎ C (=NR ６ｐ ) NR ６ｑ R ６ｒ selected from the group consisting of: R ６ｋ and R ６ｍ are independently H and (C １ ~C ６ ) alkyl; R ６ｎ and R ６ｐ are independently H and CH ３ selected from the group consisting of: R ６ｑ and R ６ｒ are independently H and (C １ ~C ６ ) alkyl; R ６ｂ is H and (C １ ~C ６ ) alkyl; R ６ｃ is H and CH ３ selected from the group consisting of: n is selected from the group consisting of 1, 2, 3 and 4; R ６ｄ is NR ６ｓ C (=NR ６ｔ ) NR ６ｕ R ６ｖ , OH and NR ６ｗ R ６ｘ selected from the group consisting of: R ６ｓ and R ６ｔ are independently H and CH ３ selected from the group consisting of: R ６ｕ , R ６ｖ , R ６ｗ and R ６ｘ are independently H and (C １ ~C ６ ) alkyl; q is selected from the group consisting of 2, 3, and 4; Xaa7 is a group represented by formula (VIII), formula (IX), formula (X), or formula (XI): 【Chemistry 14】 Dtc and Oic; Here, R ７ａ is H, (C １ ~C ６ ) alkyl and (CH ２ ) ｔ R ７ｇ selected from the group consisting of: R ７ｇ OH, CO ２ H and NR ７ｈ R ７ｉ selected from the group consisting of: R ７ｈ and R ７ｉ are independently H and (C １ ~C ６ ) alkyl; t is selected from the group consisting of 1, 2, 3 and 4; R ７ｂ is H and (C １ ~C ６ ) alkyl; Or alternatively, R ７ａ and R ７ｂ may together form a 5- or 6-membered carbocyclic or heterocyclic ring; R ７ｃ is H and CH ３ selected from the group consisting of: R ７ｄ is selected from the group consisting of H, F and OH; R ７ｅ is selected from the group consisting of H and F; R ７ｆ is H and CH ３ selected from the group consisting of: u is selected from the group consisting of 2, 3 and 4; L ３ is a bond and -(Xab1) ｖ - selected from the group consisting of; v is selected from the group consisting of 1, 2 and 3; Xab1 is each and individually selected from the group consisting of Ttds, Pamb, APAc, O2Oc, Ahx, Pab, and Cmp; where, when v=1, Xab1 is Z ３ and covalently bonded to a side chain amino functionality of formula (X) or of formula (XI), When v=2, the first of the two Xab1 is Z ３ covalently bonded to the second of the two Xab1s, the second of the two Xab1s being covalently bonded to the first of the two Xab1s, and covalently bonded to a side chain amino functional group of formula (X) or formula (XI), When v=3, the first of the three Xab1s is covalently bonded to Z3, is covalently bonded to the second of the three Xab1s, the second of the three Xab1s is covalently bonded to the first of the three Xab1s, is covalently bonded to the third of the three Xab1s, and the third of the three Xab1s is covalently bonded to the second of the three Xab1s, and is covalently bonded to a side chain amino functional group of formula (X) or formula (XI); Z ３ is selected from the group consisting of H and a chelator; Xaa8 is an α-amino acid residue, and the α-nitrogen atom of Xaa8 is unsubstituted or is CH ３ may be substituted by Xaa10 is a group represented by formula (XII) 【Chemistry 15】 and where: R １０ａ is (C １ ~C ６ ) alkyl; R １０ｂ is H and CH ３ selected from the group consisting of: R １０ｃ is H and CH ３ selected from the group consisting of: L ２ teeth, bond and -Xaa11-(Xaa12) ｓ -wherein Xaa11 is covalently linked to Xaa10; Xa11 is selected from the group consisting of Thr, Ala, Bal, Gab, Gln, Glu, Gly, Leu, Nmt, Phe, Pro, and Trp; s is selected from the group consisting of 0, 1, 2, 3, 4 and 5; Xaa12 is each and individually selected from the group consisting of Asp, asp, Ala, Gab, Ttds, Pamb, Cmp, O2Oc, APAc, Gly, Ser, Lys(Bio), and Pab; Here, when s=0, Xaa11 is Z ２ is covalently bonded to When s=1, Xaa12 is covalently linked to Xaa11, and Z ２ is covalently bonded to When s=2, the first of the two Xaa12 is covalently bound to Xaa11, the second of the two Xaa12 is covalently bound to Xaa11, the second of the two Xaa12 is covalently bound to the first of the two Xaa12, and Z ２ is covalently bonded to When s=3, the first of the three Xaa12 is covalently bound to Xaa11 and is covalently bound to the second of the three Xaa12, the second of the three Xaa12 is covalently bound to the first of the three Xaa12 and is covalently bound to the third of the three Xaa12, and the third of the three Xaa12 is covalently bound to the second of the three Xaa12; Z ２ is covalently bonded to When s=4, the first of the four Xaa is covalently bonded to Xaa and is covalently bonded to the second of the four Xaa, the second of the four Xaa is covalently bonded to the first of the four Xaa and is covalently bonded to the third of the four Xaa, the third of the four Xaa is covalently bonded to the second of the four Xaa and is covalently bonded to the fourth of the four Xaa, and the fourth of the four Xaa is covalently bonded to the third of the four Xaa; ２ is covalently bonded to When s=5, the first of the five Xaa is covalently bonded to Xaa, the second of the five Xaa is covalently bonded to the first of the five Xaa, the third of the five Xaa, the third of the five Xaa is covalently bonded to the second of the five Xaa, the fourth of the five Xaa, the fourth of the five Xaa is covalently bonded to the third of the five Xaa, the fifth of the five Xaa, the fifth of the five Xaa is covalently bonded to the fourth of the five Xaa; ２ is covalently bonded to; Z ２ is a compound of CT, an -en-chelator, an -Ape-chelator and formula (CT-I) 【Chemistry 16】 is selected from the group consisting of CT is NH ２ , en, en (Me) ２ , en(Me), NHBu, NHnPen, AF488N3K-NH ２ , OH and Throl-OH; w is selected from the group consisting of 2, 3 and 4; L ４ is selected from the group consisting of Bond, Ttds, Pamb, APAc, O2Oc, Ahx, Pab, and Cmp; Z ４ is a chelator; However, L ２ is a bond and CT is NHnPen, then Xaa10 may be absent. or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, which may contain a therapeutically active nuclide or a diagnostically active nuclide.

3. Z １ , Z ２ , Z ３ and Z ４ 3. The compound of claim 1, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein only one of:

4. Z ２ is CT; and Xaa7 is selected from the group consisting of formula (VIII), formula (IX), Dtc and Oic; 4. A compound according to any one of claims 1, 2 and 3, or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate or hydrate thereof.

5. Z １ 5. The compound of claim 4, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein: is a chelator.

6. L １ But -(Xaa1) ｋ -; wherein k is selected from the group consisting of 1 and 2, or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate or hydrate thereof.

7. k is 2 and L １ is of formula (XIII): ︁︁] ｂ ︁︁] ａ ︍(︩). and wherein Xaa1 ａ is covalently linked to Xaa2; Xaa1 ａ is selected from the group consisting of Thr, He, and Leu; and Xaa1 ｂ is selected from the group consisting of Cmp, Ttds, Pamb, Ahx, APAc, Bal, O2Oc and Pab; 7. A compound according to any one of claims 4, 5 and 6, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

8. 8. A compound according to any one of claims 4, 5, 6 and 7, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein k is 1 and Xaa1 is selected from the group consisting of Pamb, Bal, Cmp, Pab, Ahx, APAc, Thr, Pamp and PPAc.

9. L ２ is bond and -Xaa11-(Xaa12) ｓ - s is selected from the group consisting of 0 and 1, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

10. L ２ is -Xaa11-(Xaa12) ｓ - and; s is selected from the group consisting of 0 and 1; and Xa11 is selected from the group consisting of Thr, Bal, Gln, Phe, Gab, Nmt, Gly, Leu, Trp, Glu and Pro; 10. The compound of claim 9, or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate or hydrate thereof.

11. 11. The compound of claim 10, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein s is 0.

12. 11. The compound of any one of claims 9 and 10, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein s is 1; and Xaa12 is Asp.

13. L ２ 10. The compound of claim 9, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein: is a bond.

14. CT scan shows NH ２ , en, en(Me), en(Me) ２ 14. The compound according to any one of claims 9, 10, 11, 12 and 13, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein the compound is selected from the group consisting of NHBu, Throl-OH and OH.

15. L ２ -Z ２ But Thr-NH ２ , Bal-NH ２ , Glu-NH ２ , Pro-NH ２ , Gln-NH ２ , Trp-NH ２ , Leu-NH ２ , Gly-NH ２ and Nmt-NH ２ 10. The compound of any one of claims 4, 5, 6, 7, 8 and 9, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, selected from the group consisting of:

16. Xaa7 is selected from the group consisting of formula (VIII), formula (IX), Dtc and Oic, R ７ａ But, H, (C １ ~C ６ ) alkyl and (CH ２ ) ｔ R ７ｇ selected from the group consisting of: t is selected from the group consisting of 1 and 2; and R ７ｇ But OH, CO ２ H and NH ２ is selected from the group consisting of Preferably, Xaa7 is selected from the group consisting of Aib, Ala, Glu, Pro, Dfp, glu, Amd, 4Tfp, Pam, Deg, Nmg, Ams, ams, amd, Dtc and Oic, or Preferably, Xaa7 is selected from formula (VIII), wherein: R ７ａ But, H, (C １ ~C ２ ) alkyl, CH ２ OH, CH ２ CO ２ H and CH ２ CH ２ CO ２ H; R ７ｂ is H and (C １ ~C ２ ) alkyl; R ７ｃ is H; more preferably, Xaa7 is selected from the group consisting of Aib and Ala.

16. A compound according to any one of claims 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 and 15, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

17. Z １ is NT, and Xaa7 is selected from the group consisting of formula (VIII), formula (IX), Dtc and Oic; 4. A compound according to any one of claims 1, 2 and 3, or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate or hydrate thereof.

18. Z ２ is selected from the group consisting of en-chelators, -Ape-chelators and formula (CT-I), and Z ２ is formula (CT-I), Z ４ 18. The compound of claim 17, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein: is a chelator.

19. L １ is the bond and (Xaa1) ｋ and k is selected from the group consisting of 1 and 2; 19. A compound according to any one of claims 17 and 18, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

20. k is 2 and L １ is represented by formula (XIII) ︁︁] ｂ ︁︁] ａ ︍(︩). and wherein Xaa1 ａ is covalently linked to Xaa2 of formula (I); Xaa1 ａ is Thr; Xaa1 ｂ is Met or Cmp; 20. The compound of claim 19, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof.

21. Xaa1 ｂ 21. The compound of claim 20, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein is Met.

22. 22. The compound of any one of claims 20 and 21, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein NT is selected from the group consisting of H, Ac and nBuCAyl.

23. 20. The compound of claim 19, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein k is 1 and Xaa1 is selected from the group consisting of Thr, Ala, Pamp and Ser.

24. 24. The compound of claim 23, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein Xaa1 is selected from the group consisting of Thr and Pamp; and NT is selected from the group consisting of Ac, nBuCAyl and Hex.

25. L １ is a bond, and preferably NT is selected from the group consisting of Ac, HPA, HYDAc, Iva, SaPr and HO-succinyl, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

26. L ２ is -Xaa11-(Xaa12) ｓ - and; s is selected from the group consisting of 0, 1 and 2; 26. A compound according to any one of claims 17, 18, 19, 20, 21, 22, 23, 24 and 25, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

27. Z ２ 27. The compound of claim 26, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein: is formula (CT-I):

28. 28. The compound of any one of claims 26 and 27, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein Xaa11 is Thr.

29. L ２ but, a) -Xaa11- (Xaa12) ｓ s is 1; and Xaa12 is selected from the group consisting of Asp, Cmp, Ttds, Pamb, O2Oc, APAc and Pab; or b) -Xaa11- (Xaa12) ｓ s is 2; L ２ But the structure -Xaa11-Xaa12 ａ -Xaa12 ｂ -having; During the ceremony, Xaa12 ａ is selected from the group consisting of Asp, Cmp, Ttds, Pamb, O2Oc, APAc, and Pab; and Xaa12 ｂ But, Ttds, 29. A compound according to any one of claims 26, 27 and 28, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

30. Z ２ 27. The compound of any one of claims 17, 18, 19, 20, 21, 22, 23, 24, 25 and 26, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein:

31. L ２ is a bond or Xaa11, where L ２ 31. The compound of claim 30, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein when is Xaa11, Xaa11 is preferably Thr.

32. Xaa7 is selected from formula (VIII), formula (IX), Dtc and Oic, R ７ａ But, H, (C １ ~C ６ ) alkyl and (CH ２ ) ｔ R ７ｇ selected from the group consisting of: R ７ｇ OH and CO ２ H; t is selected from the group consisting of 1 and 2; R ７ｂ is H and (C １ ~C ６ ) alkyl; preferably, Xaa7 is a) selected from the group consisting of Aib, Ala, Glu, Pro, Dfp, glu, Amd, 4Tfp, Pam, Deg, Nmg, Ams, ams, amd, Dtc and Oic; or b) of formula (VIII), wherein R ７ａ But, H, (C １ ~C ２ ) alkyl, CH ２ OH, CH ２ CO ２ H and CH ２ CH ２ CO ２ H; R ７ｂ is H and (C １ ~C ２ ) alkyl; R ７ｃ is H, 32. A compound according to any one of claims 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30 and 31, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

33. 33. The compound of claim 32, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein Xaa7 is selected from the group consisting of Ala and Aib.

34. Xaa7 is selected from the group consisting of formula (X) and formula (XI); Z ３ is a chelator; Z １ is NT; and Z ２ But it is CT.

4. A compound according to any one of claims 1, 2 and 3, or a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate or hydrate thereof.

35. L １ is a bond and -(Xaa1) ｋ -; k is 1, where L １ is Xaa1, Xaa1 is preferably Thr; 35. The compound of claim 34, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

36. 36. The compound of any one of claims 34 and 35, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein NT is selected from the group consisting of Ac, SaPr, Iva and HPA.

37. L ２ is bond and -Xaa11-(Xaa12) ｓ -, and s is selected from the group consisting of 0 and 1; preferably, Xaa11 is selected from the group consisting of Thr, Gln, Phe, Gab, Nmt, Bal, Gly, Leu, Trp, Glu and Pro, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

38. CT scan shows NH ２ 38. The compound of claim 37, wherein:

39. 39. The compound of any one of claims 34, 35, 36, 37 and 38, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein Xaa7 is selected from the group consisting of Lys and Apc, and a chelator is attached to the ε-nitrogen atom of Lys or the γ-nitrogen atom of Apc, and a linker is optionally interspersed between Apc or Lys and the chelator.

40. 40. The compound of any one of claims 34, 35, 36, 37, 38 and 39, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein Xaa7 is selected from the group consisting of Apc(DOTA), Lys(DOTAGA-O2Oc), Lys(DOTA-O2Oc), Lys(DOTA-Pab), Lys(DOTA-Ahx), Lys(DOTA-APAc), Lys(DOTA-Pamb), Lys(DOTA-Cmp), Lys(DOTA-Ttds), Lys(DOTA).

41. Xaa7 is selected from formula (X): u is 4; L ３ But -(Xab1) ｖ - and; v is 1; and Xab1 is selected from the group consisting of Ttds, Pamb, APAc, O2Oc, Ahx and Pab; 39. A compound according to any one of claims 34, 35, 36, 37 and 38, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

42. 42. The compound of any one of claims 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, and 41, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein the chelator is selected from the group consisting of DOTA, DOTAGA, LSC, NOPO, PCTA, DOTAM, Macropa, Crown, NOTA, and NODAGA.

43. 43. The compound of any one of claims 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, and 42, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof, wherein Xaa2 is selected from the group consisting of Aib, Ala, Ams, ams, Deg, Pam, and Pro.

44. Xaa3 is selected from the group consisting of Phe, 1Ni, 2Ni, 6Clw, Cys(Bzl), Hfe, and Trp, and Phe, Nmf, and Hfe are independently selected from Cl, CH ３ , F., C.N., C.F. ３ and OH; preferably, Xaa3 is selected from the group consisting of Phe and Pcf, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

45. Xaa5 is selected from the group consisting of Formula (Va), Formula (Vb), Hgn and Nle; R ５ｇ , R ５ｈ and R ５ｉ But CH ３ and Preferably, Xaa5 is selected from formula (Va): R ５ａ But H, CH ３ , Ac and C(=NR ５ｄ ) NR ５ｅ R ５ｆ selected from the group consisting of: R ５ｅ and R ５ｆ are independently H and CH ３ selected from the group consisting of: R ５ｂ is H; R ５ｃ is H; m is selected from the group consisting of 3 and 4; More preferably, Xaa5 is selected from the group consisting of Lys, Lys(Me), Kip and KMe3.

45. A compound according to any one of claims 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 and 44, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

46. Xaa6 is selected from the group consisting of formula (VI), formula (VII) and Nle; In the formula, R ６ａ However, H, C (= NR ６ｅ ) NR ６ｆ R ６ｇ and C(=O)R ６ｈ selected from the group consisting of: R ６ｅ is H; R ６ｆ But H, CH ３ , Ac, NO ２ and C(=O)NR ６ｉ R ６ｊ selected from the group consisting of: R ６ｇ H and CH ３ selected from the group consisting of: R ６ｈ But CH ３ , N.H. ２ and NHC(=NH)NH ２ selected from the group consisting of: R ６ｂ is H; R ６ｃ is H; and R ６ｄ is NHC(=NH)NH ２ and N.H. ２ selected from the group consisting of: Preferably, Xaa6 is a) selected from the group consisting of Arg, Arg(Me), Cit, Egd, RMe2a, RMe3, Nle, Gln, Lys(Ac), Hgn, Arg(EtCAyl), Urr, Arg(Ac), Gln(Gu), Orn, Har, RMe2 and Eew; or b) of formula (VI), wherein n is 3; R ６ａ C(=NH)NHR ６ｆ and R ６ｆ However, H, Ac, NO ２ and C.H. ３ selected from the group consisting of 46. ​​A compound according to any one of claims 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, and 45, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof.

47. 47. The compound of claim 46, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein Xaa6 is selected from the group consisting of Arg, Arg(Me), Cit, Egd, RMe2a and RMe3.

48. Xaa8 is a group represented by formula (XIV): 【Chemistry 17】 , Gly, Val, Met, Ile, and Thr; In the formula, R ８ａ But H, OH, NH ２ , COOH, C(=O)NH ２ ,NHC(=NH)NH ２ , (C １ ~C ８ ) selected from the group consisting of alkyl, aryl, and heteroaryl; w is selected from the group consisting of 1, 2 and 3; R ８ｂ H and CH ３ selected from the group consisting of: Preferably, R ８ａ is OH, COOH, C(=O)NH ２ , phenyl, CH ２ NHC (=NH)NH ２ , indole and CH(CH ３ ) ２ selected from the group consisting of: w is selected from the group consisting of 1 and 2; 48. A compound according to any one of claims 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 and 47, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

49. 49. The compound of claim 48, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof, wherein Xaa8 is selected from the group consisting of Asn, Trp, Phe, Arg, Ser, Gly, Leu, Asp, Nmn, Glu and asn.

50. Xaa10 is a group represented by formula (XII): 【Chemistry 18】 wherein R １０ｂ H and CH ３ selected from the group consisting of: R １０ｃ is H; Preferably, Xaa10 is selected from the group consisting of Tle, Leu, Val, Npg and Ile.

49. A compound according to any one of claims 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, 47, 48, and 49, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or hydrate thereof.

51. Compounds of formula (Ia) 【Chemistry 19】 17. The compound of any one of claims 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 and 16, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

52. Xaa3 is selected from the group consisting of Phe, 1Ni, 2Ni, 6Clw, Cys(Bzl), Hfe, and Trp, and Phe, Nmf, and Hfe are independently selected from Cl, CH ３ , F., C.N., C.F. ３ and OH; preferably, Xaa3 is selected from the group consisting of Phe and Pcf, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

53. Xaa10 is a group represented by formula (XII) 【Chemistry 20】 wherein: R １０ｂ H and CH ３ selected from the group consisting of: R １０ｃ is H; Preferably, Xaa10 is a compound of formula (XIV) 【Chemical 21】 selected from the group consisting of: More preferably, R １０ａ But C(CH ３ ) ３ , C.H. ２ CH (CH ３ ) ２ , CH(CH ３ ) ２ , CH(CH ３ ) C ２ H ５ and C.H. ２ C(CH ３ ) ３ selected from the group consisting of 53. A compound according to any one of claims 51 and 52, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

54. Compound of formula (Ib) 【Chemical 22】 and In the formula, R ３ｃ H, Cl, CH ３ , F., C.N., C.F. ３ and OH; and R ３ｃ is in the meta or para position of the phenyl ring of formula (Ib), 54. A compound according to any one of claims 51, 52 and 53, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

55. Xaa2 is Aib or Ala; Xaa3 is Phe or Pcf; Xaa5 is Lys(Me), Lys, Kip, or KMe3; Xaa6 is Arg(Me), Arg, Egd, Cit, RMe2a, or RMe3; Xaa7 is AiB or Ala; Xaa8 is Asn; and Xaa10 is Tle or Leu; 17. A compound according to any one of claims 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 and 16, or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate or hydrate thereof.

56. Xaa2 is Aib or Ala; Xaa3 is Phe or Pcf; Xaa5 is Lys or Lys(Me); Xaa6 is Arg or Arg(Me); Xaa7 is AiB or Ala; Xaa8 is Ans; and Xaa10 is Tle or Leu; 34. A compound according to any one of claims 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32 and 33, or a pharmaceutically acceptable salt, solvate or hydrate thereof.

57. The following DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0194); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH ２ (PSM-0433); DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0492); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0178); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0179); Ac-Thr-Aib-Phe-[Cys-Lys-Gln-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0180); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Hyp-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0181); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-Ttds-Ttds-AF488N3K-NH ２ (PSM-0183); DOTA-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH ２ (PSM-0184); Ac-Pamp-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en-DOTA (PSM-0186); Ac-Thr-Deg-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0187); SaPr-Aib-Pcf-[Cys-Lys-Arg-Lys(DOTA-APAc)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0188); Ac-Thr-Aib-Pcf-[Cys-Lys-Gln(Gu)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0189); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH ２ (PSM-0190); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-APAc-lys(DOTA)-NH ２ (PSM-0191); DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys- Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0193); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Glu-Asn-Cys]-Nle-Thr-Asp-NH ２ (PSM-0197); DOTA-Cmp-Tle-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0198); DOTA-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en (PSM-0199); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg-Aib-Asn-Cys]-Tle-NH ２ (PSM-0200); DOTA-Pamb-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0202); DOTA-Cmp-Thr-Aib-Pcf-[Cys-KMe2-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0203); nBuCAyl-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0204); Ac-Thr-Aib-Pcf-[Cys-Nle-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0205); nBuCAyl-Thr-Aib-Mcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0207); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-NHnPen (PSM-0208); DOTA-Bal-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0209); Ac-Thr-Aib-Phe-[Cys-Gln-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0210); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Pab)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0211); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH ２ (PSM-0212); SaPr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0215); DOTA-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH ２ (PSM-0216); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Dfp-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0217); DOTAGA-R-R-R-[R- ２ (PSM-0218); DOTA-Cmp-Leu-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0220); DOTA-Pamb-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en (PSM-0221); DOTA-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en (PSM-0222); DOTA-Cmp-Aib-Pcf-[Cys-Lys-Arg(Ac)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0223); SaPr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0224); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Har-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0225); H-Met-Thr-Ala-Phe-[Cys -Lys-Arg-Ala-Asn-Cys]-L Hiyori Komatsu ２ (PSM-0226); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-amd-Asn-Cys]-Tle-Thr-NH ２ (PSM-0227); Ac-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0228); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Met-Cys]-Tle-Thr-NH ２ (PSM-0229); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH ２ (PSM-0230); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH ２ (PSM-0231); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Nmg-Asn-Cys]-Tle-Thr-NH ２ (PSM-0232); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Pam-Asn-Cys]-Tle-Thr-NH ２ (PSM-0233); DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0234); Ac-Thr-Aib-Phe-[Cys-Lys-Nmr-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0235); Ac-Thr-Aib-Pcf-[Cys-Nle-Gln(Gu)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0236); DOTA-Ttds-Thr-Aib-Phe-[Cys-Ly s-Arg-Ala-Asn-Cys]-Tle-Thr-NH ２ (PSM-0237); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Trp-Cys]-Tle-Thr-NH ２ (PSM-0238); Hex-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH ２ (PSM-0239); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Arg-Cys]-Tle-Thr-NH ２ (PSM-0240); DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en (PSM-0241); Ac-Thr-Aib-Mcf-[Cys-Lys-Arg-Lys(DOTA-O2Oc)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0243); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Kip-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0244); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Orn-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0245); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-ala-Asn-Cys]-Tle-Thr-NH ２ (PSM-0246); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-RMe2-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0247); DOTA-Cmp-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0248); Ac-Thr-Aib-1Ni-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0249); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Ttds-Ttds-Lys(Bio)-NH ２ (PSM-0250); Xingtai Mountain ２ (PSM-0251); Ac-Thr-Aib-Phe-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0252); Ac-Thr-Aib-Phe-[Cys-Lys-Glu-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0253); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Eew-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0254); DOTA-Cmp-Thr-Aib-Mpa-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0255); DOTA-Cmp-Thr-ams-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0256); DOTA-Cmp-Thr-Aib-Opa-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0257); THIS IS YOUR LIFE THIS IS YOUR LIFE(SYS69). ２ (SPIRITUAL 2558) DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0259); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-glu-Asn-Cys]-Tle-Thr-NH ２ (PSM-0260); DOTA-APAc-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0261); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Glu-NH ２ (PSM-0262); DOTA-APAc-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0263); Ac-Thr-Aib-Mtf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0264); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH ２ (PSM-0266); HPA-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH ２ (PSM-0267); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en-DOTA (PSM-0269); DOTA-Pamb-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0270); AF488Ahx-Ttds-Ttds-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0272); DOTA-Pamb-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en (PSM-0273); DOTA-Cmp-Thr-Aib-Eaa-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0274); Ac-Thr-Aib-Mcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0275); Ac-Thr-Aib-Pnf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0278); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Ser-Cys]-Tle-Thr-NH ２ (PSM-0279); Ac-Thr-Aib-Phe-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0280); Ac-Aib-Pcf-[Cys-Lys-Arg-Lys(DOTA-APAc)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0282); DOTA-Pamb-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0283); Ac-Thr-Aib-Mcf-[Cys-Lys-Cit-Lys(DOTA-O2Oc)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0284); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH ２ (PSM-0285); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH ２ (PSM-0287); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH ２ (PSM-0288); Hex-Thr-Aib-Phe-[Cys-Lys-Gln-Aib-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH ２ (PSM-0289); Iva-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH ２ (PSM-0292); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Ser-Cys]-Tle-Thr-NH ２ (PSM-0293); Ac-Thr-Aib-Pff-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0294); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH ２ (PSM-0295); DOTA-Cmp-Thr-Aib-Mpa-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0296); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Gab-NH ２ (PSM-0297); Ac-Aib-Pcf-[Cys-Lys-Arg(Ac)-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0298); __________________________________________ ________________________________________________(________) ２ ? Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-OH (PSM-0300); Ac-Th+ ２ (PSM-0301); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Amd-Asn-Cys]-Tle-Thr-NH ２ (PSM-0302); Ac-Thr-Aib-Phe-[Cys-Lys-Gln-Aib-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH ２ (PSM-0303); DOTA-Cmp-Thr-Aib-6Clw-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0304); T-shirt ２ (PSM-0305); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(Me) ２ (PSM-0306); Ac-Thr-Aib-Phe-[Cys-Lys-Cit-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0307); DOTA-Cmp-Thr-Aib-5Clw-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0308); DOTA-Ahx-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0310); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Gab-OH (PSM-0313); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-ams-Asn-Cys]-Tle-Thr-NH ２ (PSM-0314); Ac-Thr-Aib-Phe-[Cys-Lys-arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0315); DOTA-Pab-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0316); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Har-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0317); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0318); Ac-Thr-Ala-Nmf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0319); Ac-Aib-Pcf-[Cys-Lys-Arg(Me)-Aib-Asn-Cys]-Tle-en-DOTA (PSM-0320); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Apc(DOTA)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0321); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH ２ (PSM-0322); HPA-Aib-Pcf-[Cys-Lys-Arg-Lys(DOTA-APAc)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0324); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0326); SaPr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH ２ (PSM-0328); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0329); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn -Cys]-Leu-Thr-Asp-Ttds-lys(DOTA)-NH ２ (PSM-0330); DOSTA-Cmp-Thr-Aib-Pcf-[Smc-Lys-Arg-Aib-Asn-Cys]-Tle-NH ２ (Substitute: DOSTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Smc]-Tle-NH ２ ) (PSM-0332); Ac-Thr-Aib-Phe-[Cys-Lys-Gln-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0334); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Ala-Cys]-Nle-Thr-Asp-NH ２ (PSM-0335); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0336); Ac-Thr-Aib-Pcf-[Cys-Lys-Nle-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0338); Ac-Th-A-Ph-[Cy-Ly-Arg-A-Asn-Cy-]-T-Th-Cmp-ly-(DOT-AG-)-NH ２ (PSM-0339); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Nmr-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0340); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Lys(Ac)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0341); HONG KONG ２ (PSM-0342); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0345); DOTA-Cmp-Thr-Amd-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0346); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0349); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-leu-Thr-NH ２ (PSM-0350); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0351); DOTA-Bal-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0352); Iva-Aib-Pcf-[Cys-Lys-Arg-Lys(DOTA-APAc)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0353); DOTA-Cmp-Thr-Aib-Mcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0354); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-RMe3-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0355); DOTA-Cmp-Ile-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0357); DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH ２ (PSM-0361); Ac-Thr-Aib-Phe-[Cys-Lys-Glu-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0363); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0365); DOTA-Cmp-Thr-amd-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0366); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH ２ (PSM-0367); DOTA-Ahx-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0368); DOTA-Cmp-Thr-Ams-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0369); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Lys(DOTA-O2Oc)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0370); nBuCAyl-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0371); Ac-Thr-Aib-Pmf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0372); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0374); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Deg-Asn-Cys]-Tle-Thr-NH ２ (PSM-0375); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Trp-NH ２ (PSM-0376); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Val-Nmt-NH ２ (PSM-0377); H-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0378); Ac-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en-DOTA (PSM-0379); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0380); DOTA-Pamb-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH ２ (PSM-0381); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Ams-Asn-Cys]-Tle-Thr-NH ２ (PSM-0382); Ac-Thr-Aib-Mcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0383); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en (PSM-0384); Ac-Thr-Aib-Phe-[Cys-Lys-Gln-Lys(DOTA)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0385); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Pro-NH ２ (PSM-0388); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-asp-NH ２ (PSM-0389); DOTA-Cmp-Thr-Aib-6Clw-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0390); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Ape-DOTA (PSM-0391); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-4Tfp-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0392); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(PSM-0393); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Aib-Thr-NH ２ (PSM-0394); DOTA-Cmp-Thr-Aib-Pff-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0395); DOTA-Cmp-Thr-Aib-Mtf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0396); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA)-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0397); DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0398); Hex-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH ２ (PSM-0400); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-O2Oc)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0401); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-asn-Cys]-Tle-Thr-NH ２ (PSM-0402); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Oic-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0403); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH ２ (PSM-0404); Hex-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Leu-Thr-Asp-Ttds-lys(DOTA)-NH ２ (PSM-0405); DOTA-Cmp-Thr-Ams-Pcf-[Cys-Lys-Arg-Ams-Asn-Cys]-Tle-Thr-NH ２ (PSM-0407); Ac-Thr-Nmg-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0408); DOTA-Cmp-Thr-Aib-Opa-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0409); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0410); Ac-Thr-Aib-Hfe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0411); Ac-Thr-Aib-Mmf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0412); DOTA-PPAc-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0413); Ac-Thr-Ala-Amf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0414); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Cmp)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0415); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Glu-Asn-Cys]-Tle-Thr-NH ２ (PSM-0416); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Pamb)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0419); DOSTA-Cmp-Thr-Aib-Pcf-[Smc-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (Substitute: DOSTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Smc]-Tle-NH ２ ) (PSM-0420); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-leu-Thr-NH ２ (PSM-0421); Ac-Thr-Aib-Phe-[Cys-Tap-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0422); Ac-Thr-Aib-Phe-[Cys-Lys-Gln-Lys(DOTA-Ttds)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0423); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH ２ (PSM-0424); Hex-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH ２ (PSM-0425); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH ２ (PSM-0426); THIS IS YOUR LIFE THIS IS YOUR LIFE(SYS69). ２ (S0000427) Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0428); DOTA-Cmp-Thr-Aib-Mcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0431); DOTA-Pamb-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH ２ (PSM-0432); nBuCAyl-Thr-Aib-Phe-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0434); Ac-Thr-Aib-Phe-[Cys-Gln-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0435); DOTA-Bal-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0437); Ac-Thr-Aib-Phe-[Cys-Aph-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0439); Ac-Thr-Aib-Cys(Bzl)-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0441); Ac-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0442); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-NH ２ (PSM-0443); Iva-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA)-NH ２ (PSM-0444); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0445); DOTA-Pab-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0448); DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH ２ (PSM-0449); Iva-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0450); Ac-Thr-Aib-Phe-[Cys-Nmk-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0451); nBuCAyl-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH ２ (PSM-0452); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Leu-NH ２ (PSM-0453); DOTA-Cmp-Thr-Aib-Ppa-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0454); DOTA-Cmp-Nmt-Ala-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0455); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en(Me)(PSM-0456); DOTA-Pamb-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH ２ (PSM-0458); DOTA-Cmp-Thr-Aib-Mnf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0459); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Pro-Asn-Cys]-Nle-Thr-Asp-NH ２ (PSM-0460); Hib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0461); Hex-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH ２ (PSM-0462); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-APAc)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0464); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Ttds)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0465); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Ac)-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0466); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH ２ (PSM-0467); Ac-Ser-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH ２ (PSM-0469); nBuCAyl-Thr-Aib-Mcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0470); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Pab-lys(DOTA)-NH ２ (PSM-0471); Ac-Aib-Pcf-[Cys-Lys(Me)-Arg-Aib-Asn-Cys]-Tle-en-DOTA(PSM-0472); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Ala-Asp-NH ２ (PSM-0476); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Gly-NH ２ (PSM-0477); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asp-Cys]-Tle-Thr-NH ２ (PSM-0478); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Gly-Cys]-Tle-Thr-NH ２ (PSM-0479); DOTA-Ttds-Thr-Ala-Phe-[Cys- Lys-Arg-Ala-Asn-Cys]-Leu-NH ２ (PSM-0480); Ac-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-en-DOTA(PSM-0481); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0482); DOTA-Cmp-Thr-Aib-Pcf-[Cys-KMe3-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0483); nBuCAyl-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0484); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Hgn-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0485); Ac-Thr-Aib-Mcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0486); Ac-Thr-Aib-Tyr-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0488); DOTA-Cmp-Aib-Pcf-[Cys-Lys-Gln(Gu)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0489); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Bio)-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0490); Ac-Ala-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH ２ (PSM-0491); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-OH(PSM-0493); Ac-Aib-Pcf-[Cys-Lys-Gln(Gu)-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0494); Crown-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0495); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Glu-Cys]-Tle-Thr-NH ２ (PSM-0496); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Nml-Thr-NH ２ (PSM-0497); H-Met-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Leu-Thr-Asp-Gly-Ser-NH ２ (PSM-0498); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Egd-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0499); nBuCAyl-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-lys(DOTA-Cmp)-NH ２ (PSM-0500); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH ２ (PSM-0501); Hex-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH ２ (PSM-0502); DOTA-Cmp-Thr-Aib-Mmf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0503); HONG KONG ２ (PSM-0504); DOTA-O2Oc-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0505); Ac-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0506); DOTA-Cmp-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0507); Ac-Thr-Pam-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0508); HPA-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0509); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NHBu(PSM-0510); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Orn-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0511); DOTA-Cmp-Thr-Aib-Opa-[Cys-Lys-Cit-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0512); DOTA-Ahx-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0513); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH ２ (PSM-0514); Macropa-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0515); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-en-DOTA(PSM-0516); Ac-Thr-Aib-2Ni-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0517); HYDAc-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0518); DOTA-Ttds-Thr-Aib-Phe-[Cys-Lys-Gln-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0521); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Pamb-lys(DOTA)-NH ２ (PSM-0522); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-O2Oc-lys(DOTA)-NH ２ (PSM-0529); HPA-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0530); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Hgn-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0531); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Dtc-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0532); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn -Cys]-Nle-Thr-Asp-Ttds-lys(DOTA)-NH ２ (PSM-0533); DOTA-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-NH ２ (PSM-0534); Ac-Thr-Aib-Phe-[Cys-lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0535); DOTA-Cmp-Tle-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0538); DOTA-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH ２ (PSM-0539); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Gln-NH ２ (PSM-0540); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Phe-Cys]-Tle-Thr-NH ２ (PSM-0541); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Ttds)-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0542); DOTA-APAc-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0543); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Leu-Cys]-Tle-Thr-NH ２ (PSM-0545); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Urr-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0546); Ac-Thr-Pro-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Asp-NH ２ (PSM-0547); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Nmk-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0548); DOTA-Cmp-Thr-Aib-Ptf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0549); Ac-Thr-Aib-Ptf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0550); Ac-Thr-Aib-Mff-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0551); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-NH ２ (PSM-0552); DOTA-Cmp-Thr-Aib-Mff-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-NH ２ (PSM-0553); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Throl-OH(PSM-0554); Ac-Thr-Aib-Mnf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0555); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Phe-NH ２ (PSM-0556); Ac-Thr-Aib-Ocf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0558); Ac-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0559); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Npg-NH ２ (PSM-0560); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Nle-Thr-Ala-NH ２ (PSM-0562); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Glu-Cys]-Tle-Thr-NH ２ (PSM-0563); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0565); Ac-Thr-Aib-Phe-[Smc-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-NH ２ (Substitute: Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Ala-Asn-Smc]-Tle-Thr-Asp-NH ２ )(PSM-0567); Hex-Thr-Ala-Phe-[Cys-Lys-Arg-Ala-Asn-Cys]-Tle-Thr-Asp-Ttds-lys(DOTA)-NH ２ (PSM-0568); Ac-Thr-Aib-Pcf-[Cys-Lys-Arg(Ac)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0569); Ac-Thr-Aib-Pcf-[Cys-Nle-Arg(Ac)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0570); nBuCAyl-Thr-Aib-Mcf-[Cys-Lys-Opy-Aib-Asn-Cys]-Tle-Thr-Cmp-lys(DOTA)-NH ２ (PSM-0571); DOTA-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0573); DOTA-Pamb-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Bal-NH ２ (PSM-0574); Bio-Ttds-Ttds-Thr-Aib-Pcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0575); Hex-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Ttds-lys(DOTA)-NH ２ (PSM-0576); HO-Succinyl-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0577); Ac-Thr-Ala-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Nle-Thr-Asp-NH ２ (PSM-0578); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg(EtCAyl)-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0579); DOTA-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0580); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Lys(DOTA-Ahx)-Asn-Cys]-Tle-Thr-NH ２ (PSM-0582); DOTA-Cmp-Thr-Aib-Mcf-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0583); Ac-Thr-Aib-Pcf-[Cys-Lys-Cit-Aib-Leu-Cys]-Tle-Thr-NH ２ (PSM-0584); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys-Arg-Ala-Nmn-Cys]-Tle-Thr-NH ２ (PSM-0585); Ac-Thr-Aib-Trp-[Cys-Lys-Arg-Aib-Asn-Cys]-Tle-Thr-Asp-NH ２ (PSM-0587); Ac-Thr-Aib-Phe-[Cys-Lys-Arg-Aib-Trp-Cys]-Tle-Thr-NH ２ (PSM-0589); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-RMe2a-Aib-Asn-Cys]-Tle-Thr-NH ２ (PSM-0590): Macropa-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0591); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-RMe1-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0592); DOTAM-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0593); DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-OH(PSM-0594); LSC-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Thr-NH2(PSM-0601); DOTA-Cmp-Thr-Aib-Phe-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-en-H(PSM-0605)および DOTA-Cmp-Thr-Aib-Pcf-[Cys-Lys(Me)-Arg(Me)-Aib-Asn-Cys]-Tle-Bal-NH2 (PSM-0606) 2. The compound of claim 1 selected from: or a pharmaceutically acceptable salt, solvate or hydrate thereof.

58. 58. A compound according to any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56 and 57, or a pharmaceutically acceptable salt, solvate or hydrate thereof, comprising a diagnostically active nuclide or a therapeutically active nuclide.

59. a diagnostically active nuclide; preferably, the diagnostically active nuclide is a diagnostically active radionuclide, more preferably, said diagnostically active radionuclide is ４３ Sc, ４４ Sc, ５１ Mn, ５２ Mn, ６４ Cu, ６７ Ga, ６８ Ga, ８６ Y. ８９ Zr, ９４ｍ Tc, ９９ｍ Tc, １１１ In, １５２ Tb, １５５ Tb, １７７ Lu, ２０１ Tl, ２０３ Pb, １８ F. ７６ Br, ７７ Br, １２３ I, １２４ I and １２５ 59. The compound of claim 58, selected from the group consisting of: I, or a pharmaceutically acceptable salt, solvate or hydrate thereof.

60. a therapeutically active nuclide; preferably, said therapeutically active nuclide is a therapeutically active radionuclide; more preferably, said therapeutically active radionuclide is ４７ Sc, ６７ Cu, ８９ Sr, ９０ Y. １１１ In, １５３ Sm, １４９ Tb, １６１ Tb, １７７ Lu, １８６ Re, １８８ Re, ２１２ Pb, ２１２ Bi, ２１３ Bi, ２２３ Ra, ２２４ Ra, ２２５ Ac, ２２６ Th, ２２７ Th, １３１ I and ２１１ 58. The compound of any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56 and 57, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the compound is selected from the group consisting of:

61. 60. A compound according to any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58 and 59, or a pharmaceutically acceptable salt, solvate or hydrate thereof, for use in a method for the diagnosis of a disease.

62. 60, or a pharmaceutically acceptable salt, solvate or hydrate thereof, for use in a method for the treatment of a disease.

63. A compound for use according to any one of claims 61 and 62, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the disease involves affected tissue containing cells that exhibit upregulated expression of prostate-specific membrane antigen (PSMA), preferably cells that exhibit upregulated expression of PSMA.

64. The disease is a neoplasm, preferably a cancer or a tumor; more preferably, the tumor is selected from the group comprising advanced tumors, metastatic tumors and primary tumors; most preferably, the tumor is a) from the group comprising prostate tumors, metastatic prostate tumors, lung tumors, kidney tumors, glioblastoma, pancreatic tumors, bladder tumors, sarcomas, melanomas, breast tumors, colon tumors, pheochromocytoma, esophageal tumors, gastric tumors, carcinomas, squamous cell carcinomas (e.g., of the cervix, eyelid, conjunctiva, vagina, lung, oral cavity, skin, bladder, tongue, larynx and esophagus), and adenocarcinomas (e.g., of the prostate, small intestine, endometrium, cervix, large intestine, lung, pancreas, esophagus, rectum, uterus, stomach, breast and ovary) and combinations thereof; or b) from the group comprising prostate cancer (e.g., metastatic castration-resistant prostate cancer), renal cancer (e.g., clear cell carcinoma), head cancer, neck cancer, head and neck cancer, lung cancer (e.g., non-small cell lung cancer), salivary gland cancer, breast cancer, colorectal cancer, esophageal cancer, gastric cancer, liver cancer (e.g., hepatocellular carcinoma), thyroid cancer, glioblastoma, glioma, gallbladder cancer, laryngeal cancer, leukemia / lymphoma, uterine cancer, skin cancer (e.g., melanoma), endocrine cancer, sarcoma, urinary tract cancer, pancreatic cancer, gastrointestinal cancer, ovarian cancer, cervical cancer, endometrial cancer, fallopian tube cancer, primary peritoneal cancer, blood cancer (e.g., diffuse large B-cell lymphoma, Hodgkin's lymphoma, non-Hodgkin's lymphoma, follicular lymphoma, acute myeloid leukemia or multiple myeloma), cancer of unknown primary, adenoma and tumor angiogenesis 64. A selected compound for use according to any one of claims 61, 62 and 63, or a pharmaceutically acceptable salt, solvate or hydrate thereof.

65. 65. The compound for use according to any one of claims 61, 63 and 64, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein said method for diagnosis is an imaging method.

66. 56, 57, 58, and 59, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, for use in a method for identifying a subject, wherein the subject is likely or unlikely to respond to treatment of a disease, and wherein the method for identifying a subject comprises using a compound of any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, and 59, or a pharmaceutically acceptable salt, solvate, or hydrate thereof. 61, 63, 64 and 65. A compound according to any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58 and 59, or a pharmaceutically acceptable salt, solvate or hydrate thereof, comprising the step of performing a method for diagnosis using a pharmaceutically acceptable salt, solvate or hydrate thereof, preferably a method for diagnosis of a disease as described in any one of claims 61, 63, 64 and 65.

67. 60. The compound, or a pharmaceutically acceptable salt, solvate or hydrate thereof, for use in a method for selecting a subject from a group of subjects, wherein the subject is likely to respond or is unlikely to respond to treatment of a disease, said method for selecting a subject from a group of subjects comprising the step of:

64. A compound according to any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58 and 59, or a pharmaceutically acceptable salt, solvate or hydrate thereof, comprising the step of performing a method for diagnosis using said compound, or a pharmaceutically acceptable salt, solvate or hydrate thereof, preferably a method for diagnosis of a disease as described in any one of claims 61, 63, 64 and 65.

68. 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 16 64. A compound according to any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58 and 59, or a pharmaceutically acceptable salt, solvate or hydrate thereof, comprising the step of performing a method for diagnosis using the compound, or a pharmaceutically acceptable salt, solvate or hydrate thereof, preferably a method for diagnosis of a disease as described in any one of claims 61, 63, 64 and 65.

69. 69. The compound for use according to any one of claims 66, 67 and 68, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the disease is a disease involving prostate-specific membrane antigen (PSMA) protein or the disease involves cells that show upregulated expression of prostate-specific membrane antigen (PSMA); preferably, the tumor is selected from the group consisting of prostate tumor, metastatic prostate tumor, lung tumor, kidney tumor, glioblastoma, pancreatic tumor, bladder tumor, sarcoma, melanoma, breast tumor, colon tumor, pheochromocytoma, esophageal tumor, gastric tumor, carcinoma, squamous cell carcinoma (e.g., cervix, eyelid, conjunctiva, vagina, lung, oral cavity, skin, bladder, tongue, larynx and esophagus), and adenocarcinoma (e.g., prostate, small intestine, endometrium, cervix, large intestine, lung, pancreas, esophagus, rectum, uterus, stomach, breast and ovary), and combinations thereof.

70. The compound, or a pharmaceutically acceptable salt, solvate or hydrate thereof, is for use in a method for delivering a diagnostically active radionuclide or a therapeutically active radionuclide to prostate-specific membrane antigen (PSMA), preferably wherein the diagnostically active radionuclide is ４３ Sc, ４４ Sc, ５１ Mn, ５２ Mn, ６４ Cu, ６７ Ga, ６８ Ga, ８６ Y. ８９ Zr, ９４ｍ Tc, ９９ｍ Tc, １１１ In, １５２ Tb, １５５ Tb, １７７ Lu, ２０１ Tl, ２０３ Pb, １８ F. ７６ Br, ７７ Br, １２３ I, １２４ I and １２５ I, preferably １８ F. ４３ Sc, ４４ Sc, ６４ Cu, ６７ Ga, ６８ Ga, ８６ Y. ８９ Zr, ９９ｍ Tc, １１１ In, １５２ Tb, １５５ Tb and ２０３ Pb, more preferably １８ F. ６４ Cu, ６８ Ga and １１１ In, wherein the therapeutically active radionuclide is selected from the group consisting of: ４７ Sc, ６７ Cu, ８９ Sr, ９０ Y. １１１ In, １５３ Sm, １４９ Tb, １６１ Tb, １７７ Lu, １８６ Re, １８８ Re, ２１２ Pb, ２１２ Bi, ２１３ Bi, ２２３ Ra, ２２４ Ra, ２２５ Ac, ２２６ Th, ２２７ Th, １３１ I, ２１１ At, preferably ４７ Sc, ６７ Cu, ９０ Y. １６１ Tb, １７７ Lu, １８８ Re, ２１２ Pb, ２１２ Bi, ２１３ Bi, ２２５ Ac, ２２７ Th, more preferably ９０ Y. １６１ Tb, １７７ Lu, ２１２ Pb, ２２５ Ac and ２２７ 60. The compound of any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, and 59, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, wherein the compound is selected from the group consisting of:

71. The compound for use of claim 70, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein the prostate-specific membrane antigen (PSMA) is expressed by cells, preferably prostate cells, metastatic prostate cells, lung cells, kidney cells, pancreatic cells, bladder cells, breast cells, colon cells, germ cells, esophageal cells, gastric cells, endothelial cells and combinations thereof, each of which exhibits upregulated expression of PSMA.

72. 61. A composition, preferably a pharmaceutical composition, comprising a compound according to any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58 and 60, or a pharmaceutically acceptable salt, solvate or hydrate thereof, and a pharmaceutically acceptable excipient.

73. 30. A method for diagnosing a disease in a subject, comprising administering to the subject a diagnostically effective amount of a compound of claim 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, 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, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 8, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58 and 59, or a pharmaceutically acceptable salt, solvate or hydrate thereof; preferably, said compound, or a pharmaceutically acceptable salt, solvate or hydrate thereof, comprises a diagnostically active nuclide, said nuclide preferably being a diagnostically active radionuclide.

74. 30. A method for treating a disease in a subject, comprising administering to the subject a therapeutically effective amount of any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58 and 60, or a pharmaceutically acceptable salt, solvate or hydrate thereof; preferably, said compound, or a pharmaceutically acceptable salt, solvate or hydrate thereof, comprises a therapeutically active nuclide, said nuclide preferably being a therapeutically active radionuclide.

75. The method of any one of claims 73 and 74, wherein the disease is a disease in which the prostate-specific membrane antigen (PSMA) protein is involved; or the disease involves affected tissue containing cells that exhibit upregulated expression of prostate-specific membrane antigen (PSMA), preferably cells that exhibit upregulated expression of PSMA.

76. 50. A kit comprising a compound of any one of claims 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, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, and 60, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, and optionally including one or more excipients, and optionally including one or more devices, wherein the device is selected from the group comprising a labeling device, a purification device, a manipulation device, a radiation protection device, an analytical device, or an administration device.

77. 77. A kit according to claim 76 for use in any method as defined in any of the preceding claims.

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