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  Metastin derivatives and use thereofUSPTO Application #: 20060241051Title: Metastin derivatives and use thereof Abstract: The present invention provides a metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivitives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action. (end of abstract) Agent: Edwards & Angell, LLP - Boston, MA, US Inventors: Chieko Kitada, Taiji Asami, Naoki Nishizawa, Tetsuya Ohtaki, Naoki Tarui, Hirokazu Matsumoto, Jiro Noguchi, Hisanori Matsui USPTO Applicaton #: 20060241051 - Class: 514015000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai, Cyclopeptides, 9 To 11 Peptide Repeating Units In Known Peptide Chain The Patent Description & Claims data below is from USPTO Patent Application 20060241051. Brief Patent Description - Full Patent Description - Patent Application Claims
TECHNICAL FIELD [0001] The present invention relates to metastin derivatives and use thereof. BACKGROUND ART [0002] Human-derived metastin (also termed KiSS-1 peptide) (WO 00/24890) and mouse or rat-derived metastin (WO 01/75104 2) are known. Also, sustained released preparations containing metastin are known ((WO 02/85399). [0003] Reportedly, metastin has an effect of suppressing cancer metastasis and is therefore effective for preventing/treating cancers (for example, lung cancer, gastric cancer, liver cancer, pancreatic cancer, colorectal cancer, rectal cancer, colonic cancer, prostate cancer, ovarian cancer, cervical cancer, breast cancer, renal cancer, bladder cancer, brain tumor, etc.); metastin also has an effect of regulating a function of the pancreas and is effective for preventing/treating pancreatic diseases (e.g., acute or chronic pancreatitis, pancreatic cancer, etc.); and metastin further has an effect of regulating a function of the placenta and is effective for preventing/treating choriocarcinoma, hydatid moles, invasive moles, miscarriage, fetal hypoplasia, sugar dysbolism, lipid dysbolism or abnormal delivery (WO00/24890; WO01/75104 2; WO 02/85399). DISCLOSURE OF THE INVENTION [0004] The present invention aims at providing stable metastin derivatives having excellent biological activities such as a cancer metastasis suppressing activity, and a cancer proliferation suppressing activity, etc. [0005] The present inventors have made extensive studies to solve the foregoing problems. As a result, the inventors have found that by modifying the metastin-constituting amino acids with a specific modifying group, metastin derivatives unexpectedly show improved blood stability, etc. as compared to native metastin and exhibit an excellent cancer metastasis suppressing activity or a cancer proliferation suppressing activity. In addition, the inventors have found that unexpectedly, these metastin derivatives have an effect of suppressing gonadotropic hormone secretion, an effect of suppressing sex hormone secretion, etc., which are totally different from the effects known so far. Based on these findings, the inventors have continued further investigations and come to accomplish the present invention. [0006] That is, the present invention provides the following features. [0007] [1] A metastin derivative represented by formula (I): [wherein, [0008] each of Z.sup.1, Z.sup.3, Z.sup.5 and Z.sup.7 represents hydrogen atom or a C.sub.1-3 alkyl group; each of Z.sup.2, Z.sup.4, Z.sup.6 and Z.sup.8 represents hydrogen atom, O or S; [0009] R.sup.1 represents (1) hydrogen atom, or (2) a C.sub.1-8 alkyl group optionally substituted with a substituent selected from the group consisting of an optionally substituted carbamoyl group, an optionally substituted hydroxyl group and an optionally substituted aromatic cyclic group; [0010] R.sup.2 represents (1) hydrogen atom or (2) a cyclic or linear C.sub.1-10 alkyl group, or (3) a C.sub.1-10 alkyl group consisting of a cyclic alkyl group and a linear alkyl group; [0011] R.sup.3 represents: [0012] (1) a C.sub.1-8 alkyl group having an optionally substituted basic group and optionally having an additional substituent, [0013] (2) an aralkyl group having an optionally substituted basic group and optionally having an additional substituent, [0014] (3) a C.sub.1-4 alkyl group having a non-aromatic cyclic hydrocarbon group of carbon atoms not greater than 7 having an optionally substituted basic group, and optionally having an additional substituent, or, [0015] (4) a C.sub.1-4 alkyl group having a non-aromatic heterocyclic group of carbon atoms not greater than 7 having an optionally substituted basic group, and optionally having an additional substituent; [0016] R.sup.4 represents a C.sub.1-4 alkyl group, which may optionally be substituted with a substituent selected from the group consisting of: [0017] (1) an optionally substituted C.sub.6-12 aromatic hydrocarbon group, [0018] (2) an optionally substituted 5- to 14-membered aromatic heterocyclic group consisting of 1 to 7 carbon atoms and hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atoms, [0019] (3) an optionally substituted C.sub.8-14 aromatic fused-ring group, [0020] (4) an optionally substituted 5- to 14-membered aromatic fused heterocyclic group consisting of 3 to 11 carbon atoms and hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atoms, [0021] (5) an optionally substituted non-aromatic cyclic hydrocarbon group having carbon atoms not greater than 7, and, Continue reading... 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