http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-049938-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_28e3113097dd6d28720572e47f2f2407 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K14-4703 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 |
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-47 |
| filingDate | 2005-06-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e661434bc21b28d703462cc19a4a08e0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f9e0f670ae3e1ce4eab489a822112aaa http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_80177a68ece32dc6c371df95e9af6f30 |
| publicationDate | 2006-09-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-049938-A1 |
| titleOfInvention | METASTININE DERIVATIVES AND USE OF THE SAME |
| abstract | This provides stable metastin derivatives that have biological activities, such as: Cancer metastasis suppressing activity, a cancer growth suppressing activity. By modifying the constituent amino acids of metastin with specific modifying groups, it has been found that metastin derivatives have improved blood stability, etc. with respect to natural metastin and demonstrate suppression activity of cancer metastasis or cancer growth. In addition, it has been found that these metastin derivatives exhibit suppression effects of gonadotropic hormone secretion, while suppressing the secretion of sex hormone, etc., which is totally different from the effects known so far. Claim 1: A metastin II derivative characterized in that it is represented by the formula (1), [wherein: V represents a group represented by the formula (2), or a group represented by the formula (3), n represents 0 or one; W1 represents N, CH or O (with the condition that when W1 is N or CH, n represents 1 and when W1 is O, n represents 0); W2 represents N or CH; Z1, Z3, Z5 and Z7 each represents a hydrogen atom or a C1-3 alkyl group; Z4, Z6 and Z8 each represents hydrogen atom, O or S; R2 represents: a) hydrogen atom or b) a C1-10, cyclic or linear alkyl group, or c) a C1-10 alkyl group consisting of a cyclic alkyl group and a linear alkyl group, or d) a C1- alkyl group 8 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; R3 represents: a) a C1-8 alkyl group possessing an optionally substituted basic group and optionally possessing an additional substituent, b) an aralkyl group possessing an optionally substituted basic group and optionally possessing an additional substituent, c) a C1 alkyl group -4 having a non-aromatic cyclic hydrocarbon group of a quantity of carbon atoms not greater than 7 which has an optionally substituted basic group, and optionally possessing an additional substituent, od) a C1-4 alkyl group having a non-heterocyclic group aromatic of amount of carbon atoms not greater than 7 which has an optionally substituted basic group, and optionally possesses an additional substituent; R4 represents a C1-4 alkyl group, which may be optionally substituted with a substituent selected from the group consisting of: a) an optionally substituted C6-12 aromatic hydrocarbon group, b) an optionally substituted 5 to 14 membered aromatic heterocyclic group consisting of C1-7 and heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur atoms, c) an optionally substituted C8-14 aromatic fused cyclic group, d) an optionally substituted 5 to 14 membered aromatic fused heterocyclic group that consists of C3-11 and heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur atoms, e) an optionally substituted non-aromatic cyclic hydrocarbon group having a quantity of carbon atoms not greater than 7, and f) a non-heterocyclic group optionally substituted aromatic having a quantity of carbon atoms not greater than 7; Q1 represents a C1-4 alkyl group which may be optionally substituted with a substituent selected from the group consisting of: a) an optionally substituted C6-12 aromatic hydrocarbon group, b) an optionally substituted 5-14 membered aromatic heterocyclic group consisting of C1-7 and heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur atoms, c) an optionally substituted C8-14 aromatic fused cyclic group, d) an optionally substituted 5 to 14 membered aromatic fused heterocyclic group consisting of C3-11 and heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur atoms, e) an optionally substituted non-aromatic cyclic hydrocarbon group having a quantity of carbon atoms not greater than 7, and f) an optionally non-aromatic heterocyclic group substituted which has a quantity of carbon atoms not greater than 7; Q2 represents: a) CH2 which may be optionally substituted with a C1-4 alkyl group optionally substituted with a substituent selected from the group consisting of carbamoyl group and hydroxyl group, b) NH, which may be optionally substituted with a C1 alkyl group -4 optionally substituted with a substituent selected from the group consisting of carbamoyl group and hydroxyl group, oc) O; Y represents a group represented by the formula: -CONH-, -CSNH-, -CH2NH-, -NHCO-, -CH2O-, -CH2S-, -COO-, -CSO- or -CH2CH2- that can be optionally substituted with a C1-6 alkyl group; and Z9 represents hydrogen atom, O or S; and, P and P ', which can be the same or different, each can form a combined ring P and P' or P and Q1 together represent: a) hydrogen atom; b) an optional amino acid residue continuously or discontinuously limited from the C terminal of amino acid sequence 1-48 in the amino acid sequence represented by SEQ ID NO: 1; c) a group represented by the formula: J1-J2-C (J3) (Q3) Y1C (J4) (Q4) Y2C (J5) (Q5) Y3C (J6) (Q6) C (= Z10) - (where : J1 represents a) hydrogen atom or b) i) a C1-15 acyl group, ii) a C1-15 alkyl group, iii) a C6-14 aryl group, iv) carbamoyl group, v) carboxyl group, vi) group sulfino, vii) amidino group, viii) glyoxyloyl group or ix) amino group, whose groups may be optionally substituted with a substituent containing an optionally substituted cyclic group; J2 represents a) NH optionally substituted with a C1-6 alkyl group, b) CH2 optionally substituted with a C1-6 alkyl group, c) O or d) S; J3 to J6 represents hydrogen atom or a C1-3 alkyl group; Q3 to Q6 represents a C1-4 alkyl group which may have a substituent optionally selected from the group consisting of: a) an optionally substituted C6-12 aromatic hydrocarbon group; b) an optionally substituted 5-14 membered heterocyclic aromatic group consisting of C1-7 and heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur atom; c) an optionally substituted C8-14 aromatic fused cyclic group; d) an optionally substituted 5 to 14 membered aromatic fused heterocyclic group consisting of C3-11 and heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur atoms; e) an optionally substituted non-aromatic cyclic hydrocarbon group having a quantity of carbon atoms not greater than 7; f) an optionally substituted non-aromatic heterocyclic group having a quantity of carbon atoms not greater than 7; g) an optionally substituted amino group; h) an optionally substituted guanidino group; i) an optionally substituted hydroxyl group; j) an optionally substituted carboxyl group; k) an optionally substituted carbamoyl group; and l) an optionally substituted sulfhydryl group, or hydrogen atom; They can be combined together J3 and Q3, J4 and Q4, J5 and Q5 or J6 and Q6 together, or, they can be combined together J2 and Q3, Y1 and Q4, Y2 and Q5, or Y3 and Q6, to form a ring; Y1 to Y3 represents a group represented by the formula: -CON (J13) -, -CSN (J13) -, -C (J14) N (J13) - or -N (J13) CO-, (where J13 and J14 each represents hydrogen atom or a C1-3 alkyl group; and, Z10 represents hydrogen atom, O or S); d) a group represented by the formula: J1-J2-C (J7) (Q7) Y2C (J8) (Q8) Y3C (J9) (Q9) C (= Z10) - (where: J1 and J2, each it has the same meaning as described above; J7 to J9 have the same meaning as for J3; Q7 to Q9 has the same meaning as for Q3; Y2 and Y3 each has the same meaning as described above; Z10 has the same meaning as described above; J7 and Q7, J8 and Q8 or J9 and Q9 can be combined with each other, or J2 and Q7, Y2 and Q8 or Y3 and Q9 can be combined together to form a ring); e) a group represented by the formula: J1-J2-C (J10) (Q10) Y3C (J11) (Q11) C (= Z10) - (where: J1 and J2 have the same meaning as described above represents; J10 and J11 have the same meaning as for J3; Q10 and Q11 have the same meaning as for Q3; Y3 has the same meaning as described above; Z10 has the same meaning as described above; and can be combined with each other J10 and Q10 or J11 and Q11, or, J2 and Q10 or Y3 and Q11 can be combined together to form a ring); f) a group represented by the formula: J1-J2-C (J12) (Q12) C (= Z10) - (where: J1 and J2 have the same meaning as described above; J12 has the same meaning of J3; Q12 has the same meaning of Q3; Z10 has the same meaning as described above; J12 and Q12 can be combined with each other, or J2 and Q12 can be combined together to form a ring); or, g) a group represented by the formula: J1- (where: J1 has the same meaning as described above)] (with the condition that a peptide consisting of the amino acid sequence of 1-54, 2-54 , 3-54, 4-54, 5-54, 6-54, 7-54, 8-54, 9-54, 10-54, 11-54, 12-54, 13-54, 14-54, 15 -54, 15-54, 16-54, 17-54, 18-54, 19-54, 20-54, 21-54, 22-54, 23-54, 24-54, 25-54, 26-54 , 27-54, 28-54, 29-54, 30-54, 31-54, 32-54, 33-54, 34-54, 35-54, 36-54, 37-54, 38-54, 39 -54, 40-54, 41-54, 42-54, 43-54, 44-54, 45-54, 46-54, 47-54, 48-54 or 49-54 in the amino acid sequence represented by SEQ ID NO .: 1 is excluded), or a salt thereof. |
| priorityDate | 2004-06-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 57.