JP6584953B2 - 長時間作用型単鎖インスリン類似体 - Google Patents
長時間作用型単鎖インスリン類似体 Download PDFInfo
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- JP6584953B2 JP6584953B2 JP2015541857A JP2015541857A JP6584953B2 JP 6584953 B2 JP6584953 B2 JP 6584953B2 JP 2015541857 A JP2015541857 A JP 2015541857A JP 2015541857 A JP2015541857 A JP 2015541857A JP 6584953 B2 JP6584953 B2 JP 6584953B2
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/62—Insulins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/28—Insulins
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- Diabetes (AREA)
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- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Description
本出願は、2012年11月5日付で出願した係属中の米国仮出願第61/722,350号の利益を主張する。
本発明は、助成金番号DK040949およびDK074176で国立衛生研究所により授与された協力協定の下で政府の支援により行われた。米国政府は、本発明に対して特定の権利を有する。
この出願の発明に関連する先行技術文献情報としては、以下のものがある(国際出願日以降国際段階で引用された文献及び他国に国内移行した際に引用された文献を含む)。
(先行技術文献)
(特許文献)
(特許文献1) 米国特許第8,192,957号明細書
(特許文献2) 米国特許出願公開第2012/0252724号明細書
Phe−Val−Asn−Gln−His−Leu−Cys−Gly−Ser−His−Leu−Val−Glu−Ala−Leu−Tyr−Leu−Val−Cys−Gly−Glu−Arg−Gly−Phe−Phe−Tyr−Thr−Pro−Lys−Thr−Arg−Arg−Glu−Ala−Glu−Asp−Leu−Gln−Val−Gly−Gln−Val−Glu−Leu−Gly−Gly−Gly−Pro−Gly−Ala−Gly−Ser−Leu−Gln−Pro−Leu−Ala−Leu−Glu−Gly−Ser−Leu−Gln−Lys−Arg−Gly−Ile−Val−Glu−Gln−Cys−Cys−Thr−Ser−Ile−Cys−Ser−Leu−Tyr−Gln−Leu−Glu−Asn−Tyr−Cys−Asn
Gly−Ile−Val−Glu−Gln−Cys−Cys−Thr−Ser−Ile−Cys−Ser−Leu−Tyr−Gln−Leu−Glu−Asn−Tyr−Cys−Asn
Phe−Val−Asn−Gln−His−Leu−Cys−Gly−Ser−His−Leu−Val−Glu−Ala−Leu−Tyr−Leu−Val−Cys−Gly−Glu−Arg−Gly−Phe−Phe−Tyr−Thr−Pro−Lys−Thr
Phe−Val−Asn−Gln−His−Leu−Cys−Gly−Ser−His−Leu−Val−Glu−Ala−Leu−Tyr−Leu−Val−Cys−Gly−Glu−Arg−Gly−Phe−Phe−Tyr−Thr−Pro−Xaa2−Thr−Xaa3−Glu−Gly−Arg−Ser−Arg−Gly−Ile−Val−Glu−Gln−Cys−Cys−Xaa1−Ser−Ile−Cys−Ser−Leu−Tyr−Gln−Leu−Glu−Asn−Tyr−Cys−Xaa4
Xaa1は、His、Arg、Lys、またはOrnを示し、Xaa2は、Lys、Arg、またはOrnであり、Xaa3は、Ala、Gly、またはSerであり、Xaa4は、Gly、Ala、またはSerである。
Phe−Val−Asn−Gln−His−Leu−Cys−Gly−Ser−His−Leu−Val−Glu−Ala−Leu−Tyr−Leu−Val−Cys−Gly−Glu−Arg−Gly−Phe−Phe−Tyr−Thr−Pro−Xaa2−Thr−Glu−Xaa3−Gly−Arg−Ser−Arg−Gly−Ile−Val−Glu−Gln−Cys−Cys−Xaa1−Ser−Ile−Cys−Ser−Leu−Tyr−Gln−Leu−Glu−Asn−Tyr−Cys−Xaa4
Xaa1は、His、Arg、Lys、またはOrnを示し、Xaa2は、Lys、Arg、またはOrnであり、Xaa3は、Ala、Gly、またはSerであり、Xaa4は、Gly、Ala、またはSerである。
Phe−Val−Asn−Gln−His−Leu−Cys−Gly−Ser−His−Leu−Val−Glu−Ala−Leu−Tyr−Leu−Val−Cys−Gly−Glu−Arg−Gly−Phe−Phe−Tyr−Thr−Pro−Xaa2−Thr−Glu−Glu−Gly−Arg−Arg−Ser−Arg−Gly−Ile−Val−Glu−Gln−Cys−Cys−Xaa1−Ser−Ile−Cys−Ser−Leu−Tyr−Gln−Leu−Glu−Asn−Tyr−Cys−Xaa3
Xaa1は、His、Arg、Lys、またはOrnを示し、Xaa2は、Lys、Arg、またはOrnであり、Xaa3は、Gly、Ala、またはSerである。
Phe−Val−Asn−Gln−His−Leu−Cys−Gly−Ser−His−Leu−Val−Glu−Ala−Leu−Tyr−Leu−Val−Cys−Gly−Glu−Arg−Gly−Phe−Phe−Tyr−Thr−Pro−Xaa2−Thr−Glu−Glu−Gly−Ser−Arg−Arg−Ser−Arg−Gly−Ile−Val−Glu−Gln−Cys−Cys−Xaa1−Ser−Ile−Cys−Ser−Leu−Tyr−Gln−Leu−Glu−Asn−Tyr−Cys−Xaa3
Xaa1は、His、Arg、Lys、またはOrnを示し、Xaa2は、Lys、Arg、またはOrnであり、Xaa3は、Gly、Ala、またはSerである。
Phe−Val−Asn−Gln−His−Leu−Cys−Gly−Ser−His−Leu−Val−Glu−Ala−Leu−Tyr−Leu−Val−Cys−Gly−Glu−Arg−Gly−Phe−Phe−Tyr−Thr−Pro−Xaa2−Thr−Glu−Glu−Gly−Val−Ser−Arg−Arg−Ser−Arg−Gly−Ile−Val−Glu−Gln−Cys−Cys−Xaa1−Ser−Ile−Cys−Ser−Leu−Tyr−Gln−Leu−Glu−Asn−Tyr−Cys−Xaa3
Xaa1は、His、Arg、Lys、またはOrnを示し、Xaa2は、Lys、Arg、またはOrnであり、Xaa3は、Gly、Ala、またはSerである。
Phe−Val−Asn−Gln−His−Leu−Cys−Gly−Ser−His−Leu−Val−Glu−Ala−Leu−Tyr−Leu−Val−Cys−Gly−Glu−Arg−Gly−Phe−Phe−Tyr−Thr−Pro−Xaa2−Thr−Glu−Glu−Gly−Arg−Val−Ser−Arg−Arg−Ser−Arg−Gly−Ile−Val−Glu−Gln−Cys−Cys−Xaa1−Ser−Ile−Cys−Ser−Leu−Tyr−Gln−Leu−Glu−Asn−Tyr−Cys−Xaa3
Xaa1は、His、Arg、Lys、またはOrnを示し、Xaa2は、Lys、Arg、またはOrnであり、Xaa3は、Gly、Ala、またはSerである。
Phe−Val−Asn−Gln−His−Leu−Cys−Gly−Ser−His−Leu−Val−Glu−Ala−Leu−Tyr−Leu−Val−Cys−Gly−Glu−Arg−Gly−Phe−Phe−Tyr−Thr−Pro−Xaa2−Thr−Glu−Glu−Gly−Ser−Arg−Val−Ser−Arg−Arg−Ser−Arg−Gly−Ile−Val−Glu−Gln−Cys−Cys−Xaa1−Ser−Ile−Cys−Ser−Leu−Tyr−Gln−Leu−Glu−Asn−Tyr−Cys−Xaa3
Xaa1は、His、Arg、Lys、またはOrnを示し、Xaa2は、Lys、Arg、またはOrnであり、Xaa3は、Gly、Ala、またはSerである。
TTCGTCAATCAACACTTGTGTGGTTCCCACTTGGTTGAGGCATTGTACTTGGTCTGTGGTG
AGAGAGGATTCTTCTACACCCCTAGAACTGAGGAGGGTTCTAGAAGATCTAGAGGAATCG
TCGAGCAATGTTGTAGATCCATTTGTTCCTTGTACCAATTGGAGAACTACTGCGGATAA
Hohsaka,T.,& Sisido,M.2012.Incorporation of non−natural amino acids into proteins.Curr.Opin.Chem.Biol.6,809−15.
Hua,Q.X.,Nakagawa,S.H.,Jia,W.,Huang,K.,Phillips,N.B.,Hu,S.& Weiss,M.A.(2008)Design of an active ultrastable single−chain insulin analog:synthesis,structure,and therapeutic implications.J.Biol.Chem.283,14703−14716.
Kristensen,C.,Andersen,A.S.,Hach,M.,Wiberg,F.C.,Schaffer,L.,& Kjeldsen,T.1995.A single−chain insulin−like growth factor I/insulin hybrid binds with high affinity to the insulin receptor.Biochem.J.305,981−6.
Lee,H.C.,Kim,S.J.,Kim,K.S.,Shin,H.C.,& Yoon,J.W. 2000.Remission in models of type 1 diabetes by gene therapy using a single−chain insulin analogue.Nature 408,483−8.Retraction in:Lee HC,Kim KS,Shin HC.2009.Nature 458,600.
Phillips,N.B.,Whittaker,J.,Ismail−Beigi,F.,& Weiss,M.A.(2012)Insulin fibrillation and protein design:topological resistance of single−chain analogues to thermal degradation with application to a pump reservoir.J.Diabetes Sci.Technol.6,277−288.
Sciacca,L.,Cassarino,M.F.,Genua,M.,Pandini,G.,Le Moli,R.,Squatrito,S.,& Vigneri,R.2010.Insulin analogues differently activate insulin receptor isoforms and post−receptor signalling.Diabetologia 53,1743−53.
Wang,Z.X.1995.An exact mathematical expression for describing competitive biding of two different ligands to a protein molecule FEBS Lett.360:111−114.
Whittaker,J.,and Whittaker,L.2005.Characterization of the functional insulin binding epitopes of the full−length insulin receptor.J.Biol.Chem.280:20932−20936.
Claims (8)
- 配列ID番号7の配列を含む単鎖インスリン類似体であって、29位のXaaはArgであり、59位のXaaはGlyであり、46位のXaaはArgまたはHisである、単鎖インスリン類似体。
- 46位のXaaはArgである、請求項1記載の単鎖インスリン類似体。
- 46位のXaaはHisである、請求項1記載の単鎖インスリン類似体。
- 配列ID番号7の単鎖インスリン類似体をコードする核酸であって、29位のXaaはArgであり、59位のXaaはGlyであり、46位のXaaはArgまたはHisである、核酸。
- 前記核酸は配列ID番号11を含む、請求項4記載の核酸。
- 患者の血糖値を低下させる薬剤を製造するための、配列ID番号7の配列を含む単鎖インスリン類似体の使用であって、29位のXaaはArgであり、59位のXaaはGlyであり、46位のXaaはArgまたはHisである、使用。
- 配列ID番号7の46位のXaaはArgである、請求項6記載の使用。
- 配列ID番号7の46位のXaaはHisである、請求項6記載の使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261722350P | 2012-11-05 | 2012-11-05 | |
US61/722,350 | 2012-11-05 | ||
PCT/US2013/068585 WO2014071405A2 (en) | 2012-11-05 | 2013-11-05 | Long-acting single-chain insulin analogues |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2016506366A JP2016506366A (ja) | 2016-03-03 |
JP2016506366A5 JP2016506366A5 (ja) | 2016-12-15 |
JP6584953B2 true JP6584953B2 (ja) | 2019-10-02 |
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JP2015541857A Active JP6584953B2 (ja) | 2012-11-05 | 2013-11-05 | 長時間作用型単鎖インスリン類似体 |
Country Status (15)
Country | Link |
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US (2) | US9499600B2 (ja) |
EP (1) | EP2914620B1 (ja) |
JP (1) | JP6584953B2 (ja) |
KR (1) | KR102163936B1 (ja) |
CN (2) | CN105008395B (ja) |
AU (1) | AU2013337250B2 (ja) |
BR (1) | BR112015010194B1 (ja) |
CA (1) | CA2890719C (ja) |
EA (1) | EA201590882A1 (ja) |
ES (1) | ES2694418T3 (ja) |
IL (1) | IL238651B (ja) |
MX (1) | MX2015005662A (ja) |
PH (1) | PH12015500989A1 (ja) |
SG (1) | SG11201503522RA (ja) |
WO (1) | WO2014071405A2 (ja) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2014015078A1 (en) * | 2012-07-17 | 2014-01-23 | Michael Weiss | O-linked carbohydrate-modified insulin analogues |
US9624287B2 (en) | 2012-07-17 | 2017-04-18 | Case Western Reserve University | O-linked carbohydrate-modified insulin analogues |
WO2015106269A2 (en) | 2014-01-13 | 2015-07-16 | Thermalin Diabetes, Llc | Rapid action insulin formulations and pharmaceutical delivery systems |
CZ308383B6 (cs) * | 2014-06-30 | 2020-07-15 | Ústav Organické Chemie A Biochemie Akademie Věd Čr, V.V.I. | Derivát inzulinu s cyklickou strukturou v C-konci B-řetězce |
CN107108716A (zh) * | 2014-10-06 | 2017-08-29 | 卡斯西部储备大学 | 双相性单链胰岛素类似物 |
AR105616A1 (es) | 2015-05-07 | 2017-10-25 | Lilly Co Eli | Proteínas de fusión |
SG11201803911PA (en) | 2015-12-23 | 2018-07-30 | Univ Case Western Reserve | Encapsulation of ultra-stable insulin analogues with polymer melts |
JP2022507627A (ja) * | 2018-11-19 | 2022-01-18 | ケース ウェスタン リザーブ ユニバーシティ | ポリ-アラニンc-ドメインのサブセグメントを有する単鎖インスリンアナログ |
CA3122637A1 (en) | 2018-12-11 | 2020-06-18 | Sanofi | Peptide binder |
TWI844709B (zh) | 2019-07-31 | 2024-06-11 | 美商美國禮來大藥廠 | 鬆弛素(relaxin)類似物及其使用方法 |
MX2022007034A (es) * | 2019-12-10 | 2022-06-23 | Sanofi Sa | Un metodo para formar un conjugado de una sulfonamida y un polipeptido. |
WO2023041758A1 (en) | 2021-09-20 | 2023-03-23 | Kyon Biotech Ag | Arginase-insulin fusion protein |
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DE60104069T2 (de) * | 2000-10-02 | 2005-08-25 | Yonsei University | Einkettige Insulinanaloge |
KR100449454B1 (ko) | 2000-10-02 | 2004-09-21 | 이현철 | 단일사슬 인슐린 유도체의 유전자를 포함하는 당뇨병치료용 벡터 |
WO2004096854A2 (en) * | 2003-04-29 | 2004-11-11 | Eli Lilly And Company | Insulin analogs having protracted time action |
KR100508616B1 (ko) * | 2003-06-20 | 2005-08-17 | 신항철 | 염기성 아미노산 첨가를 통한 활성이 증가된 단일사슬 인슐린 아날로그 |
ATE517119T1 (de) * | 2003-12-03 | 2011-08-15 | Novo Nordisk As | Einzelketteninsulin |
EP2074140B8 (en) * | 2006-10-04 | 2015-10-28 | Case Western Reserve University | Fibrillation-resistant insulin and insulin analogues |
WO2009132129A2 (en) * | 2008-04-22 | 2009-10-29 | Case Western Reserve University | Isoform-specific insulin analogues |
SG177567A1 (en) * | 2009-07-06 | 2012-02-28 | Sanofi Aventis Deutschland | Aqueous insulin preparations containing methionine |
US20120241356A1 (en) | 2009-07-06 | 2012-09-27 | Sanofi-Aventis Deutschland Gmbh | Heat- and vibration-stable insulin preparations |
US8399407B2 (en) | 2009-09-17 | 2013-03-19 | Case Western Reserve University | Non-standard insulin analogues |
KR20150021011A (ko) * | 2011-10-27 | 2015-02-27 | 케이스 웨스턴 리저브 유니버시티 | 초고도 농축된, 속효성 인슐린 유사체 제형 |
CA2898730A1 (en) * | 2012-01-20 | 2013-07-25 | Case Western Reserve University | Glutamic acid-stabilized insulin analogues |
JP6387008B2 (ja) * | 2012-09-26 | 2018-09-05 | インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションIndiana University Research And Technology Corporation | インスリンアナローグダイマー |
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- 2013-11-05 CN CN201380069346.0A patent/CN105008395B/zh not_active Expired - Fee Related
- 2013-11-05 KR KR1020157014591A patent/KR102163936B1/ko active IP Right Grant
- 2013-11-05 EP EP13850542.5A patent/EP2914620B1/en active Active
- 2013-11-05 JP JP2015541857A patent/JP6584953B2/ja active Active
- 2013-11-05 WO PCT/US2013/068585 patent/WO2014071405A2/en active Application Filing
- 2013-11-05 US US14/440,540 patent/US9499600B2/en active Active
- 2013-11-05 BR BR112015010194-1A patent/BR112015010194B1/pt not_active IP Right Cessation
- 2013-11-05 CN CN202010947063.3A patent/CN112266414A/zh active Pending
- 2013-11-05 AU AU2013337250A patent/AU2013337250B2/en active Active
- 2013-11-05 ES ES13850542.5T patent/ES2694418T3/es active Active
- 2013-11-05 SG SG11201503522RA patent/SG11201503522RA/en unknown
- 2013-11-05 CA CA2890719A patent/CA2890719C/en active Active
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Also Published As
Publication number | Publication date |
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PH12015500989A1 (en) | 2015-07-13 |
CA2890719A1 (en) | 2014-05-08 |
KR102163936B1 (ko) | 2020-10-13 |
KR20150096387A (ko) | 2015-08-24 |
AU2013337250B2 (en) | 2017-06-22 |
WO2014071405A2 (en) | 2014-05-08 |
EP2914620A4 (en) | 2016-05-25 |
US9499600B2 (en) | 2016-11-22 |
MX2015005662A (es) | 2015-08-20 |
BR112015010194A2 (pt) | 2017-12-12 |
WO2014071405A3 (en) | 2014-08-21 |
ES2694418T3 (es) | 2018-12-20 |
US9975940B2 (en) | 2018-05-22 |
IL238651A0 (en) | 2015-06-30 |
US20150274803A1 (en) | 2015-10-01 |
EA201590882A1 (ru) | 2015-09-30 |
CN112266414A (zh) | 2021-01-26 |
CN105008395A (zh) | 2015-10-28 |
EP2914620B1 (en) | 2018-08-08 |
EP2914620A2 (en) | 2015-09-09 |
BR112015010194B1 (pt) | 2022-03-22 |
CA2890719C (en) | 2023-02-14 |
JP2016506366A (ja) | 2016-03-03 |
CN105008395B (zh) | 2020-12-29 |
IL238651B (en) | 2020-03-31 |
SG11201503522RA (en) | 2015-06-29 |
US20170137488A1 (en) | 2017-05-18 |
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