RU2550696C2 - Основанные на амидах пролекарства пептидов глюкагонового надсемейства - Google Patents
Основанные на амидах пролекарства пептидов глюкагонового надсемейства Download PDFInfo
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- RU2550696C2 RU2550696C2 RU2011129784/04A RU2011129784A RU2550696C2 RU 2550696 C2 RU2550696 C2 RU 2550696C2 RU 2011129784/04 A RU2011129784/04 A RU 2011129784/04A RU 2011129784 A RU2011129784 A RU 2011129784A RU 2550696 C2 RU2550696 C2 RU 2550696C2
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- Prior art keywords
- alkyl
- amino acid
- glucagon
- group
- peptide
- Prior art date
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- 108090000765 processed proteins & peptides Proteins 0.000 title claims abstract description 445
- 108060003199 Glucagon Proteins 0.000 title claims abstract description 409
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 title claims abstract description 393
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- 125000004429 atom Chemical group 0.000 claims description 125
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- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 35
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- CBQJSKKFNMDLON-JTQLQIEISA-N N-acetyl-L-phenylalanine Chemical compound CC(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 CBQJSKKFNMDLON-JTQLQIEISA-N 0.000 claims description 14
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- XVOYSCVBGLVSOL-UHFFFAOYSA-N cysteic acid Chemical compound OC(=O)C(N)CS(O)(=O)=O XVOYSCVBGLVSOL-UHFFFAOYSA-N 0.000 claims description 14
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 13
- 125000003295 alanine group Chemical group N[C@@H](C)C(=O)* 0.000 claims description 12
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- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims description 10
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- 125000001360 methionine group Chemical group N[C@@H](CCSC)C(=O)* 0.000 claims description 10
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- OYIFNHCXNCRBQI-BYPYZUCNSA-N L-2-aminoadipic acid Chemical compound OC(=O)[C@@H](N)CCCC(O)=O OYIFNHCXNCRBQI-BYPYZUCNSA-N 0.000 claims description 9
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- 125000001429 N-terminal alpha-amino-acid group Chemical group 0.000 claims description 7
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- A61P3/06—Antihyperlipidemics
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07K14/605—Glucagons
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- General Chemical & Material Sciences (AREA)
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Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13921008P | 2008-12-19 | 2008-12-19 | |
| US61/139,210 | 2008-12-19 | ||
| US14427109P | 2009-01-13 | 2009-01-13 | |
| US61/144,271 | 2009-01-13 | ||
| US18755609P | 2009-06-16 | 2009-06-16 | |
| US61/187,556 | 2009-06-16 | ||
| PCT/US2009/068745 WO2010071807A1 (en) | 2008-12-19 | 2009-12-18 | Amide based glucagon superfamily peptide prodrugs |
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| Publication Number | Publication Date |
|---|---|
| RU2011129784A RU2011129784A (ru) | 2013-01-27 |
| RU2550696C2 true RU2550696C2 (ru) | 2015-05-10 |
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| RU2011129784/04A RU2550696C2 (ru) | 2008-12-19 | 2009-12-18 | Основанные на амидах пролекарства пептидов глюкагонового надсемейства |
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| Country | Link |
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| US (1) | US8969288B2 (https=) |
| EP (2) | EP3075385A1 (https=) |
| JP (2) | JP2012512903A (https=) |
| KR (1) | KR20110110174A (https=) |
| CN (1) | CN102325539A (https=) |
| AR (1) | AR074811A1 (https=) |
| AU (1) | AU2009327418A1 (https=) |
| BR (1) | BRPI0922969A2 (https=) |
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| IL (1) | IL213113A (https=) |
| MX (1) | MX2011006524A (https=) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| RU2721282C2 (ru) * | 2017-11-21 | 2020-05-18 | Илья Владимирович Духовлинов | Способ лечения рассеянного склероза (варианты) |
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- 2009-12-18 US US13/130,962 patent/US8969288B2/en active Active
- 2009-12-18 JP JP2011542487A patent/JP2012512903A/ja active Pending
- 2009-12-18 TW TW098143717A patent/TWI489992B/zh not_active IP Right Cessation
- 2009-12-18 SG SG2011045283A patent/SG172291A1/en unknown
- 2009-12-18 EP EP09833836A patent/EP2376097A4/en not_active Ceased
- 2009-12-18 CA CA2747499A patent/CA2747499A1/en not_active Abandoned
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2011
- 2011-05-24 IL IL213113A patent/IL213113A/en not_active IP Right Cessation
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- 2015-05-07 JP JP2015095017A patent/JP2015180649A/ja active Pending
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| WO1998011126A1 (en) * | 1996-09-09 | 1998-03-19 | Zealand Pharmaceuticals A/S | Peptide prodrugs containing an alpha-hydroxyacid linker |
| WO2008021560A2 (en) * | 2006-08-17 | 2008-02-21 | Amylin Pharmaceuticals, Inc. | Dpp-iv resistant gip hybrid polypeptides with selectable properties |
| WO2009099763A1 (en) * | 2008-01-30 | 2009-08-13 | Indiana University Research And Technology Corporation | Ester-based peptide prodrugs |
| RU2010148308A (ru) * | 2008-04-29 | 2012-06-10 | Асцендис Фарма Ас (Dk) | Пэгилированные соединения рекомбинантного гормона роста человека |
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| DE, AMAB.: 'DESIGN OF PEPTIDE-BASED PRODRUG CHEMISTRY AND ITS APPLICATION TO GLUCAGON-LIKE PEPTIDE I.' SUBMITTED TO THE FACULTY OF THE UNIVERSITY GRADUATE SCHOOL IN PARTIAL FULFILLMENT OF THE REQUIREMENTS FOR THE DEGREE MASTER OF SCIENCES IN THE DEPARTMENT OF CHEMISTRY, [Online] August 2007, INDIANA UNIVERSITY, pages I-XIII, 1-123 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2721282C2 (ru) * | 2017-11-21 | 2020-05-18 | Илья Владимирович Духовлинов | Способ лечения рассеянного склероза (варианты) |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20110110174A (ko) | 2011-10-06 |
| RU2011129784A (ru) | 2013-01-27 |
| JP2015180649A (ja) | 2015-10-15 |
| US8969288B2 (en) | 2015-03-03 |
| CA2747499A1 (en) | 2010-06-24 |
| EP2376097A1 (en) | 2011-10-19 |
| MX2011006524A (es) | 2011-08-17 |
| US20110288003A1 (en) | 2011-11-24 |
| IL213113A (en) | 2017-09-28 |
| EP3075385A1 (en) | 2016-10-05 |
| PE20120332A1 (es) | 2012-04-14 |
| IL213113A0 (en) | 2011-07-31 |
| AU2009327418A1 (en) | 2010-06-24 |
| CL2011001498A1 (es) | 2012-03-09 |
| CN102325539A (zh) | 2012-01-18 |
| TWI489992B (zh) | 2015-07-01 |
| SG172291A1 (en) | 2011-07-28 |
| WO2010071807A1 (en) | 2010-06-24 |
| AR074811A1 (es) | 2011-02-16 |
| BRPI0922969A2 (pt) | 2019-09-24 |
| EP2376097A4 (en) | 2012-10-03 |
| JP2012512903A (ja) | 2012-06-07 |
| TW201028162A (en) | 2010-08-01 |
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| Date | Code | Title | Description |
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| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20171219 |