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Cyclic peptide compound or pharmacologically acceptable salt thereof and method for producing same コモンズ

外国特許コード F140007866
整理番号 KG0093-US01
掲載日 2014年5月7日
出願国 アメリカ合衆国
出願番号 201113808772
公報番号 20130109833
公報番号 8653235
出願日 平成23年7月6日(2011.7.6)
公報発行日 平成25年5月2日(2013.5.2)
公報発行日 平成26年2月18日(2014.2.18)
国際出願番号 JP2011065521
国際公開番号 WO2012005313
国際出願日 平成23年7月6日(2011.7.6)
国際公開日 平成24年1月12日(2012.1.12)
優先権データ
  • 特願2010-155576 (2010.7.8) JP
  • 2011JP065521 (2011.7.6) WO
発明の名称 (英語) Cyclic peptide compound or pharmacologically acceptable salt thereof and method for producing same コモンズ
発明の概要(英語) Provided are a cyclic peptide compound or a pharmacologically acceptable salt thereof capable of inhibiting parakeratosis of skin, and a method for producing the same.
This method comprises subjecting a cyclic peptide compound of Formula (I): or a pharmacologically acceptable salt thereof, wherein Xaa1 and Xaa5 are each optionally substituted Ser, optionally substituted Thr, or optionally substituted Tyr; Xaa2 is optionally substituted Ile, optionally substituted Val, or optionally substituted Leu; Xaa3 and Xaa4 are each optionally substituted Asn, optionally substituted Gln, optionally substituted Asp, or optionally substituted Glu; and R1 is a group of Formula (II): -CO-(CH2)n-NH-(II), or Formula (III): -NH-(CH2)n-CO-(III), wherein n is the same as defined above, and in Formula (I), the linkage between Cys and Cys is a peptide bond or a disulfide bond, and the other linkages are peptide bonds, to cyclization with a compound of Formula (IV): Cys-R1-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Cys(IV), wherein, Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, and R1 are the same as defined above.
特許請求の範囲(英語) [claim1]
1. A cyclic peptide compound represented by Formula (I):

or a pharmacologically acceptable salt thereof, wherein Xaa1 and Xaa5 are each independently optionally substituted seryl, optionally substituted threonyl, or optionally substituted tyrosinyl;
Xaa2 is optionally substituted isoleucyl, optionally substituted valyl, or optionally substituted leucyl;
Xaa3 and Xaa4 are each independently optionally substituted asparaginyl, optionally substituted glutaminyl, optionally substituted aspartyl, or optionally substituted glutamyl;
Cys is cysteinyl; and
R1is a group represented by either Formula (II):
-- CO -- (CH2)n -- NH -- (II)
wherein n is an integer of 1 to 10, or Formula (III):
-- NH -- (CH2)n -- CO -- (III)
wherein n is an integer of 1 to 10; and in Formula (I), the linkage between Cys and Cys is a peptide bond or a disulfide bond, and the other linkages are peptide bonds.
[claim2]
2. The cyclic peptide compound or a pharmacologically acceptable salt thereof according to claim 1, wherein in Formula (I), Xaa1 is seryl, Xaa2 is isoleucyl, Xaa3 is glutamyl, Xaa4 is glutaminyl, Xaa5 is seryl, and R1 is a group represented by Formula (III) wherein n is 1.
[claim3]
3. The cyclic peptide compound or a pharmacologically acceptable salt thereof according to claim 1 or 2, wherein in Formula (I), Cys and Cys are linked through a disulfide bond.
[claim4]
4. A method for producing a cyclic peptide compound represented by Formula (I):

or a pharmacologically acceptable salt thereof, wherein Xaa1 and Xaa5 are each independently optionally substituted seryl, optionally substituted threonyl, or optionally substituted tyrosinyl;
Xaa2 is optionally substituted isoleucyl, optionally substituted valyl, or optionally substituted leucyl;
Xaa3 and Xaa4 are each independently optionally substituted asparaginyl, optionally substituted glutaminyl, optionally substituted aspartyl, or optionally substituted glutamyl;
Cys is cysteinyl; and
R1 is a group represented by either Formula (II):
-- CO -- (CH2)n -- NH -- (II),
wherein n is an integer of 1 to 10, or Formula (III):
-- NH -- (CH2)n -- CO -- (III)
wherein n is an integer of 1 to 10; and in Formula (I), the linkage between Cys and Cys is a peptide bond or a disulfide bond, and the other linkages are peptide bonds, the method comprising cyclizing a compound represented by Formula (IV):
Cys-R1-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Cys (IV),
wherein Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, Cys, and R1 are the same as Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, Cys, and R1 of Formula (I).
[claim5]
5. The production method according to claim 4, wherein the cyclic peptide compound is a compound represented by Formula (I) wherein Xaa1 is seryl, Xaa2 is isoleucyl, Xaa3 is glutamyl, Xaa4 is glutaminyl, Xaa5 is seryl, and R1 is a group represented by Formula (III) wherein n is 1, and wherein a compound used as a starting material is a compound represented by Formula (IV) wherein Xaa1 is seryl, Xaa2 is isoleucyl, Xaa3 is glutamyl, Xaa4 is glutaminyl, Xaa5 is seryl, and R1 is a group represented by Formula (III).
[claim6]
6. The production method according to claim 4 or 5, wherein the cyclic peptide compound is a compound in which Cys and Cys of Formula (I) are linked through a disulfide bond, and wherein the cyclization is performed by oxidative crosslinking of the thiol groups of the cysteines at both ends of the compound represented by Formula (IV).
[claim7]
7. The cyclic peptide compound or a pharmacologically acceptable salt thereof according to claim 1, wherein in Formula (I), Xaa1 is seryl, Xaa2 is isoleucyl, Xaa3 is glutamyl, Xaa4 is glutaminyl, Xaa5 is seryl, and R1 is a group represented by Formula (III) wherein n is 5 or 8.
[claim8]
8. A pharmaceutical composition comprising the cyclic peptide compound or a pharmacologically acceptable salt thereof of claim 1 as an active ingredient, the pharmaceutical composition being in an oral dosage form.
[claim9]
9. A method for treating diseases or disorders induced by epimorphin or resulting from overexpression of epimorphin, comprising a step of administering orally the cyclic peptide compound or a pharmacologically acceptable salt thereof of claim 1 to a patient with disease or disorders induced by epimorphin or resulting from overexpression of epimorphin, wherein the disease or disorders induced by epimorphin or resulting from overexpression of epimorphin are chronic arteriosclerosis obliterans, Buerger's disease, or damaged organs.
[claim10]
10. The production method according to claim 4,
wherein the cyclic peptide compound is a compound represented by Formula (I) wherein Xaa1 is seryl, Xaa2 is isoleucyl, Xaa3 is glutamyl, Xaa4 is glutaminyl, Xaa5 is seryl, and R1 is a group represented by Formula (III) wherein n is 5 or 8, and
wherein a compound used as a starting material is a compound represented by Formula (IV) wherein Xaa1 is seryl, Xaa2 is isoleucyl, Xaa3 is glutamyl, Xaa4 is glutaminyl, Xaa5 is seryl, and R1 is a group represented by Formula (III).
  • 発明者/出願人(英語)
  • HIRAI YOHEI
  • OKUGAWA YOJI
  • KWANSEI GAKUIN
国際特許分類(IPC)
米国特許分類/主・副
  • 530/300
  • 530/317
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