JPWO2021018923A5 - - Google Patents

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Publication number
JPWO2021018923A5
JPWO2021018923A5 JP2022506524A JP2022506524A JPWO2021018923A5 JP WO2021018923 A5 JPWO2021018923 A5 JP WO2021018923A5 JP 2022506524 A JP2022506524 A JP 2022506524A JP 2022506524 A JP2022506524 A JP 2022506524A JP WO2021018923 A5 JPWO2021018923 A5 JP WO2021018923A5
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JP
Japan
Prior art keywords
gly
peptide
glu
seq
cancer
Prior art date
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Pending
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JP2022506524A
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Japanese (ja)
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JP2022543227A (en
Publication date
Priority claimed from EP19189468.2A external-priority patent/EP3771464A1/en
Application filed filed Critical
Priority claimed from PCT/EP2020/071319 external-priority patent/WO2021018923A1/en
Publication of JP2022543227A publication Critical patent/JP2022543227A/en
Publication of JPWO2021018923A5 publication Critical patent/JPWO2021018923A5/ja
Pending legal-status Critical Current

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Claims (15)

一般配列Ｘａ－Ｌｅｕ－Ｇｌｎ－Ｇｌｙ－Ｘｂ（配列番号１）からなり、ＸａがＰｒｏ－Ｇｌｙ、ＧｌｙおよびＡｃ－Ｇｌｙから選択され、ＸｂがＧｌｕおよびＧｌｕ－ＮＨ２から選択されるペプチド、またはその薬学的に許容される塩。 A peptide consisting of the general sequence Xa-Leu-Gln-Gly-Xb (SEQ ID NO: 1), wherein Xa is selected from Pro-Gly, Gly and Ac-Gly, and Xb is selected from Glu and Glu- NH2 , or pharmaceutically acceptable salts. ＸａがＧｌｙおよびＡｃ－Ｇｌｙから選択され、ＸｂがＧｌｕおよびＧｌｕ－ＮＨ２から選択される請求項１に記載のペプチド、またはその薬学的に許容される塩。 2. The peptide of claim 1, or a pharmaceutically acceptable salt thereof, wherein Xa is selected from Gly and Ac-Gly and Xb is selected from Glu and Glu- NH2 . ＸａがＡｃ－ＧｌｙでＸｂがＧｌｕである（配列番号３）か、またはＸａがＧｌｙでＸｂがＧｌｕ－ＮＨ２である（配列番号４）、請求項１または２に記載のペプチド。 3. The peptide of claim 1 or 2, wherein Xa is Ac-Gly and Xb is Glu (SEQ ID NO: 3 ) or Xa is Gly and Xb is Glu-NH2 (SEQ ID NO:4). ＸａがＧｌｙであり、ＸｂがＧｌｕであり、ＧｌｕがＧｌｙに結合して環状ペプチド（配列番号５）：
を形成する、請求項１または２に記載のペプチド。 Xa is Gly, Xb is Glu, and Glu is attached to Gly to form a cyclic peptide (SEQ ID NO:5):
3. The peptide of claim 1 or 2, which forms ＸａがＰｒｏ－Ｇｌｙであり、ＸｂがＧｌｕであり、ＰｒｏがＧｌｕに結合して環状ペプチド（配列番号６）：
を形成する、請求項１に記載に記載のペプチド。 Xa is Pro-Gly, Xb is Glu, and Pro is bound to Glu to form a cyclic peptide (SEQ ID NO: 6):
2. The peptide of claim 1, which forms a. 請求項１に記載のペプチドＸａ－Ｌｅｕ－Ｇｌｎ－Ｇｌｙ－Ｘｂ（配列番号１）、またはその薬学的に許容される塩を、薬学的に許容される媒体、賦形剤および希釈剤からなる群から選択される少なくとも１つと共に含む医薬組成物。 The peptide Xa-Leu-Gln-Gly-Xb (SEQ ID NO: 1) of claim 1 , or a pharmaceutically acceptable salt thereof , in a pharmaceutically acceptable vehicle, excipient and dilution . A pharmaceutical composition comprising together with at least one selected from the group consisting of agents. ＸａがＧｌｙおよびＡｃ－Ｇｌｙから選択され、ＸｂがＧｌｕおよびＧｌｕ－ＮＨ２から選択される請求項６に記載の医薬組成物。 7. The pharmaceutical composition according to claim 6, wherein Xa is selected from Gly and Ac-Gly and Xb is selected from Glu and Glu- NH2 . ＸａがＡｃ－Ｇｌｙで、ＸｂがＧｌｕである（配列番号３）か、またはＸａがＧｌｙでＸｂがＧｌｕ－ＮＨ２である（配列番号４）、請求項６または７に記載の医薬組成物。 8. The pharmaceutical composition according to claim 6 or 7, wherein Xa is Ac-Gly and Xb is Glu (SEQ ID NO:3) or Xa is Gly and Xb is Glu- NH2 (SEQ ID NO:4). 前記ペプチドが
である、請求項６または７に記載の医薬組成物。 the peptide is
The pharmaceutical composition according to claim 6 or 7, which is 前記ペプチドが
である、請求項６に記載の医薬組成物。 the peptide is
The pharmaceutical composition according to claim 6, which is 組織および／または器官における細胞外マトリックスの過剰な蓄積を特徴とする線維性状態の治療における使用のための、請求項１～５のいずれか一項に記載のペプチド。 A peptide according to any one of claims 1 to 5 for use in treating fibrotic conditions characterized by excessive accumulation of extracellular matrix in tissues and/or organs. 前記線維性状態が、肝線維症、肝硬変、肺線維症、慢性呼吸不全、心筋線維症、虚血性心疾患、心不全、糖尿病性腎症、糸球体腎炎、骨髄線維症、乳癌、子宮癌、前立腺癌、膵臓癌、結腸癌、皮膚癌、血液細胞癌、中枢神経系の癌、子宮筋腫、線維腫、線維腺腫および線維肉腫からなる群から選択される、請求項１１に記載の使用のためのペプチド。 The fibrotic condition is liver fibrosis, liver cirrhosis, pulmonary fibrosis, chronic respiratory failure, myocardial fibrosis, ischemic heart disease, heart failure, diabetic nephropathy, glomerulonephritis, myelofibrosis, breast cancer, uterine cancer, prostate 12. For use according to claim 11, selected from the group consisting of cancer, pancreatic cancer, colon cancer, skin cancer, blood cell cancer, cancer of the central nervous system, uterine fibroids, fibroids, fibroadenomas and fibrosarcomas. peptide. 前記ペプチドがＸａ－Ｌｅｕ－Ｇｌｎ－Ｇｌｙ－Ｘｂ（配列番号１）であり、ＸａがＡｃ－Ｇｌｙであり、ＸｂがＧｌｕである（配列番号３）か、またはＸａがＧｌｙであり、ＸｂがＧｌｕ－ＮＨ２である（配列番号４）、請求項１１または１２に記載の使用のためのペプチド。 said peptide is Xa-Leu-Gln-Gly-Xb (SEQ ID NO: 1) and Xa is Ac-Gly and Xb is Glu (SEQ ID NO: 3) or Xa is Gly and Xb is Glu -NH2 (SEQ ID NO: 4), a peptide for use according to claim 11 or 12. 前記ペプチドが、
である、請求項１１または１２に記載の使用のためのペプチド。 the peptide is
13. A peptide for use according to claim 11 or 12, which is 前記ペプチドが
である、請求項１１または１２に記載の使用のためのペプチド。 the peptide is
13. A peptide for use according to claim 11 or 12, which is
JP2022506524A 2019-07-31 2020-07-28 Peptides as inhibitors of fibrous matrix accumulation Pending JP2022543227A (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP19189468.2 2019-07-31
EP19189468.2A EP3771464A1 (en) 2019-07-31 2019-07-31 Peptides as inhibitor of fibrotic matrix accumulation
EP19194798 2019-08-30
EP19194798.5 2019-08-30
PCT/EP2020/071319 WO2021018923A1 (en) 2019-07-31 2020-07-28 Peptides as inhibitors of fibrotic matrix accumulation

Publications (2)

Publication Number Publication Date
JP2022543227A JP2022543227A (en) 2022-10-11
JPWO2021018923A5 true JPWO2021018923A5 (en) 2023-07-19

Family

ID=71738168

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2022506524A Pending JP2022543227A (en) 2019-07-31 2020-07-28 Peptides as inhibitors of fibrous matrix accumulation

Country Status (5)

Country Link
US (1) US20220267378A1 (en)
EP (1) EP3996694A1 (en)
JP (1) JP2022543227A (en)
CN (1) CN114364691B (en)
WO (1) WO2021018923A1 (en)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0494264B1 (en) 1989-09-29 1997-06-18 La Jolla Cancer Research Foundation Inhibiting transforming growth factor to prevent accumulation of extracellular matrix
AU771635B2 (en) 1999-01-05 2004-04-01 American National Red Cross, The Methods for treating conditions associated with the accumulation of excess extracellular matrix
WO2011097401A1 (en) * 2010-02-03 2011-08-11 University Of Rochester Treatment of fibrosis-related disorders using fibronectin binding proteins and polypeptides

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