JP2008540565A5 - - Google Patents
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- JP2008540565A5 JP2008540565A5 JP2008511371A JP2008511371A JP2008540565A5 JP 2008540565 A5 JP2008540565 A5 JP 2008540565A5 JP 2008511371 A JP2008511371 A JP 2008511371A JP 2008511371 A JP2008511371 A JP 2008511371A JP 2008540565 A5 JP2008540565 A5 JP 2008540565A5
- Authority
- JP
- Japan
- Prior art keywords
- xaa
- compound according
- glu
- pegylated glp
- cys
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 102100003818 GCG Human genes 0.000 claims 12
- 101710042131 GCG Proteins 0.000 claims 12
- -1 GLP-1 compound Chemical class 0.000 claims 12
- 101700071595 GRZ1 Proteins 0.000 claims 12
- 101700078733 ZGLP1 Proteins 0.000 claims 12
- 229920001223 polyethylene glycol Polymers 0.000 claims 8
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 5
- XUJNEKJLAYXESH-REOHCLBHSA-N L-cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 4
- 125000000267 glycino group Chemical group [H]N([*])C([H])([H])C(=O)O[H] 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 claims 1
- 206010012601 Diabetes mellitus Diseases 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 1
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- MTCFGRXMJLQNBG-REOHCLBHSA-N L-serine Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 1
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 150000001413 amino acids Chemical group 0.000 claims 1
- 230000001419 dependent Effects 0.000 claims 1
- 229920001427 mPEG Polymers 0.000 claims 1
- PEEHTFAAVSWFBL-UHFFFAOYSA-N maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
Claims (12)
- 式：Ｈｉｓ−Ｘａａ８−Ｇｌｕ−Ｇｌｙ−Ｔｈｒ−Ｐｈｅ−Ｔｈｒ−Ｓｅｒ−Ａｓｐ−Ｖａｌ−Ｓｅｒ−Ｓｅｒ−Ｔｙｒ−Ｌｅｕ−Ｇｌｕ−Ｘａａ２２−Ｇｌｎ−Ａｌａ−Ａｌａ−Ｌｙｓ−Ｇｌｕ−Ｐｈｅ−Ｉｌｅ−Ａｌａ−Ｔｒｐ−Ｌｅｕ−Ｘａａ３３−Ｌｙｓ−Ｇｌｙ−Ｇｌｙ−Ｐｒｏ−Ｓｅｒ−Ｓｅｒ−Ｇｌｙ−Ａｌａ−Ｐｒｏ−Ｐｒｏ−Ｐｒｏ−Ｃｙｓ４５−Ｘａａ４６式Ｉ（配列番号：１）のアミノ酸配列を含むＰＥＧ化ＧＬＰ−１化合物。
［式中、Ｘａａ８は、Ｄ−Ａｌａ、Ｇｌｙ、Ｖａｌ、Ｌｅｕ、Ｉｌｅ、Ｓｅｒ又はＴｈｒであり、Ｘａａ２２は、Ｇｌｙ、Ｇｌｕ、Ａｓｐ又はＬｙｓであり、Ｘａａ３３は、Ｖａｌ又はＩｌｅであり、Ｘａａ４６は、Ｃｙｓ又はＣｙｓ−ＮＨ２であり、１つのＰＥＧ分子は、Ｃｙｓ４５に共有結合され、１つのＰＥＧ分子は、Ｃｙｓ４６又はＣｙｓ４６−ＮＨ２に共有結合される。] - Ｘａａ８がＧｌｙ又はＶａｌであり、Ｘａａ２２がＧｌｕである、請求項１に記載のＰＥＧ化ＧＬＰ−１化合物。
- Ｘａａ８がＶａｌであり、Ｘａａ２２がＧｌｕである、請求項２に記載のＰＥＧ化ＧＬＰ−１化合物。
- Ｘａａ８がＶａｌであり、Ｘａａ２２がＧｌｕであり、Ｘａａ３３がＩｌｅである、請求項３に記載のＰＥＧ化ＧＬＰ−１化合物。
- Ｘａａ８がＶａｌであり、Ｘａａ２２がＧｌｕであり、Ｘａａ３３がＩｌｅであり、Ｘａａ４６がＣｙｓ−ＮＨ２である、請求項４に記載のＰＥＧ化ＧＬＰ−１化合物。
- ＰＥＧ分子の分子量が５０００〜４００００ダルトンである、請求項１〜５のいずれかに記載のＰＥＧ化ＧＬＰ−１化合物。
- ＰＥＧ分子の分子量が２００００〜６００００ダルトンである、請求項１〜５のいずれかに記載のＰＥＧ化ＧＬＰ−１化合物。
- ＰＥＧ分子の分子量が２００００〜４００００ダルトンである、請求項１〜５のいずれかに記載のＰＥＧ化ＧＬＰ−１化合物。
- ＰＥＧ分子の分子量が約２００００ダルトンである、請求項１〜５のいずれかに記載のＰＥＧ化ＧＬＰ−１化合物。
- ＰＥＧ分子が直鎖状メトキシＰＥＧマレイミドである、請求項９に記載のＰＥＧ化ＧＬＰ−１化合物。
- 医薬として使用するための請求項１〜１０のいずれかに記載のＰＥＧ化ＧＬＰ−１化合物。
- インスリン非依存性糖尿病又は肥満の治療のための医薬の製造における請求項１〜１０のいずれかに記載のＰＥＧ化ＧＬＰ−１化合物の使用。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68068805P | 2005-05-13 | 2005-05-13 | |
| US60/680,688 | 2005-05-13 | ||
| PCT/US2006/018284 WO2006124529A1 (en) | 2005-05-13 | 2006-05-11 | Glp-1 pegylated compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012266820A Division JP2013079256A (ja) | 2005-05-13 | 2012-12-06 | Ｇｌｐ−１ｐｅｇ化化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008540565A JP2008540565A (ja) | 2008-11-20 |
| JP2008540565A5 true JP2008540565A5 (ja) | 2009-06-25 |
| JP5225074B2 JP5225074B2 (ja) | 2013-07-03 |
Family
ID=36926842
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008511371A Expired - Fee Related JP5225074B2 (ja) | 2005-05-13 | 2006-05-11 | Ｇｌｐ−１ｐｅｇ化化合物 |
| JP2012266820A Withdrawn JP2013079256A (ja) | 2005-05-13 | 2012-12-06 | Ｇｌｐ−１ｐｅｇ化化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012266820A Withdrawn JP2013079256A (ja) | 2005-05-13 | 2012-12-06 | Ｇｌｐ−１ｐｅｇ化化合物 |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US8183340B2 (ja) |
| EP (1) | EP1881850B1 (ja) |
| JP (2) | JP5225074B2 (ja) |
| KR (1) | KR101011081B1 (ja) |
| CN (1) | CN101166545B (ja) |
| AT (1) | ATE482724T1 (ja) |
| AU (1) | AU2006247734B2 (ja) |
| BR (1) | BRPI0609676A2 (ja) |
| CA (1) | CA2608311C (ja) |
| CY (1) | CY1110853T1 (ja) |
| DE (1) | DE602006017202D1 (ja) |
| DK (1) | DK1881850T3 (ja) |
| EA (1) | EA012442B1 (ja) |
| ES (1) | ES2350852T3 (ja) |
| HR (1) | HRP20100543T1 (ja) |
| IL (1) | IL186772A0 (ja) |
| ME (1) | ME02786B (ja) |
| MX (1) | MX2007014052A (ja) |
| NO (1) | NO20076415L (ja) |
| PL (1) | PL1881850T3 (ja) |
| PT (1) | PT1881850E (ja) |
| RS (1) | RS51637B (ja) |
| SI (1) | SI1881850T1 (ja) |
| UA (1) | UA90896C2 (ja) |
| WO (1) | WO2006124529A1 (ja) |
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| WO2008019147A2 (en) | 2006-08-04 | 2008-02-14 | Amylin Pharmaceuticals, Inc. | Use of exendins, exendin agonists and glp-1 receptor agonists for altering the concentration of fibrinogen |
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| CN101578102B (zh) | 2007-01-05 | 2013-07-17 | 印第安纳大学研究及科技有限公司 | 在生理性pH缓冲液中显示增强的溶解性的胰高血糖素类似物 |
| EP2111414B1 (en) | 2007-02-15 | 2014-07-02 | Indiana University Research and Technology Corporation | Glucagon/glp-1 receptor co-agonists |
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- 2006-05-11 DK DK06759598.3T patent/DK1881850T3/da active
- 2006-05-11 RS RS20100486A patent/RS51637B/en unknown
- 2006-05-11 WO PCT/US2006/018284 patent/WO2006124529A1/en active Application Filing
- 2006-05-11 AT AT06759598T patent/ATE482724T1/de active
- 2006-05-11 JP JP2008511371A patent/JP5225074B2/ja not_active Expired - Fee Related
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- 2006-05-11 ES ES06759598T patent/ES2350852T3/es active Active
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