CA2906694A1 - Peptide compositions - Google Patents
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- CA2906694A1 CA2906694A1 CA2906694A CA2906694A CA2906694A1 CA 2906694 A1 CA2906694 A1 CA 2906694A1 CA 2906694 A CA2906694 A CA 2906694A CA 2906694 A CA2906694 A CA 2906694A CA 2906694 A1 CA2906694 A1 CA 2906694A1
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- Prior art keywords
- arg
- phe
- cys
- trp
- seq
- Prior art date
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Classifications
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- C07K—PEPTIDES
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- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
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- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P3/06—Antihyperlipidemics
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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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
- C07K14/665—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
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Landscapes
- Health & Medical Sciences (AREA)
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- Endocrinology (AREA)
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- Gynecology & Obstetrics (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361790469P | 2013-03-15 | 2013-03-15 | |
| US61/790,469 | 2013-03-15 | ||
| PCT/US2014/028590 WO2014144260A1 (en) | 2013-03-15 | 2014-03-14 | Peptide compositions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2906694A1 true CA2906694A1 (en) | 2014-09-18 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2906694A Pending CA2906694A1 (en) | 2013-03-15 | 2014-03-14 | Peptide compositions |
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| EP (2) | EP2970388B1 (cg-RX-API-DMAC7.html) |
| JP (4) | JP6622690B2 (cg-RX-API-DMAC7.html) |
| CN (3) | CN105492456B (cg-RX-API-DMAC7.html) |
| AU (5) | AU2014227712B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2906694A1 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2693761T3 (cg-RX-API-DMAC7.html) |
| RU (2) | RU2020120797A (cg-RX-API-DMAC7.html) |
| TR (1) | TR201815173T4 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2014144260A1 (cg-RX-API-DMAC7.html) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2785889C1 (ru) * | 2015-09-30 | 2022-12-14 | Ритм Фармасьютикалз, Инк. | Способ лечения нарушений, ассоциированных с путем рецептора меланокортина 4 |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3539551T (pt) | 2011-12-29 | 2021-11-04 | Rhythm Pharmaceuticals Inc | Método de tratamento de distúrbios associados ao recetor de melanocortina-4 em portadores heterozigóticos |
| CA3209602A1 (en) | 2013-03-15 | 2014-09-18 | Rhythm Pharmaceuticals, Inc. | Pharmaceutical compositions |
| RU2020120797A (ru) * | 2013-03-15 | 2020-07-02 | Ритм Фармасьютикалз, Инк. | Пептидные композиции |
| WO2016168388A2 (en) | 2015-04-14 | 2016-10-20 | Palatin Technologies, Inc. | Therapies for obesity, diabetes and related indications |
| AU2016330773A1 (en) * | 2015-09-30 | 2018-04-19 | Charité-Universitätsmedizin Berlin | Method of treating melanocortin-4 receptor pathway-associated disorders |
| CN109803979B (zh) * | 2016-10-04 | 2023-01-31 | 帝斯曼知识产权资产管理有限公司 | 黑皮质素-1-受体激动剂 |
| CN111032680A (zh) * | 2017-03-15 | 2020-04-17 | 诺和诺德股份有限公司 | 能够与黑皮质素4受体结合的双环化合物 |
| WO2019195756A1 (en) | 2018-04-06 | 2019-10-10 | Rhythm Pharmaceuticals, Inc. | Compositions for treating kidney disease |
| WO2020053414A1 (en) * | 2018-09-14 | 2020-03-19 | Novo Nordisk A/S | Bicyclic compounds capable of acting as melanocortin 4 receptor agonists |
| CA3192873A1 (en) * | 2020-09-24 | 2022-03-31 | Leonardus H.T. Van Der Ploeg | Methods of treating melanocortin-4 receptor pathway-associated disorders |
| CN113332416B (zh) * | 2021-05-17 | 2022-02-22 | 宁波大学 | 丙谷二肽在制备治疗非酒精性脂肪肝药物中的应用 |
| CN113209270B (zh) * | 2021-05-17 | 2022-02-22 | 宁波大学 | 丙谷二肽在制备防治急性肝衰竭药物中的应用 |
| CN116789802A (zh) * | 2023-06-25 | 2023-09-22 | 湖北省农业科学院畜牧兽医研究所 | 一种山羊mc4r增强型突变体及其应用 |
| WO2025131101A1 (zh) * | 2023-12-22 | 2025-06-26 | 上海多米瑞生物技术有限公司 | 多肽化合物、其药物组合物及其用途 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0292291B1 (en) * | 1987-05-22 | 1994-08-10 | University Patents, Inc. | Linear and cyclic analogs of alpha-msh fragments with extraordinary potency |
| US5731408A (en) * | 1995-04-10 | 1998-03-24 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Peptides having potent antagonist and agonist bioactivities at melanocortin receptors |
| GB9827500D0 (en) * | 1998-12-14 | 1999-02-10 | Wapharm Ab | Compounds for control of eating, growth and body weight |
| US7176279B2 (en) * | 2000-06-28 | 2007-02-13 | Palatin Technologies, Inc. | Cyclic peptide compositions and methods for treatment of sexual dysfunction |
| WO2003006620A2 (en) * | 2001-07-11 | 2003-01-23 | Palatin Technologies, Inc. | Linear and cyclic melanocortin receptor-specific peptides |
| MXPA03001721A (es) * | 2000-08-30 | 2003-05-27 | Hoffmann La Roche | Peptidos ciclicos selectivos. |
| US7342089B2 (en) * | 2001-07-11 | 2008-03-11 | Palatin Technologies, Inc. | Cyclic peptides for treatment for cachexia |
| US7345144B2 (en) * | 2001-07-11 | 2008-03-18 | Palatin Technologies, Inc. | Cyclic peptides for treatment of cachexia |
| US7034004B2 (en) * | 2002-05-07 | 2006-04-25 | University Of Florida | Peptides and methods for the control of obesity |
| FR2851563B1 (fr) | 2003-02-26 | 2005-04-22 | Sod Conseils Rech Applic | Nouveaux derives de benzimidazole et d'imidazo-pyridine et leur utilisation en tant que medicament |
| FR2852957B1 (fr) | 2003-03-31 | 2005-06-10 | Sod Conseils Rech Applic | Nouveaux derives d'imidazo-pyridine et leur utilisation en tant que medicament |
| US20060293223A1 (en) * | 2003-06-19 | 2006-12-28 | Eli Lilly And Company Patent Division | Uses of melanocortin-3 receptor (mc3r) agonist peptides |
| EP1644023A2 (en) * | 2003-06-19 | 2006-04-12 | Eli Lilly And Company | Melanocortin recptor 4(mc4) agonists and their uses |
| FR2862971B1 (fr) | 2003-11-28 | 2006-03-24 | Sod Conseils Rech Applic | Nouveaux derives de benzimidazole et d'imidazo-pyridine et leur utilisation en tant que medicament |
| US8343031B2 (en) * | 2004-03-23 | 2013-01-01 | Michael Gertner | Obesity treatment systems |
| FR2872165B1 (fr) | 2004-06-24 | 2006-09-22 | Sod Conseils Rech Applic | Nouveaux derives de pyrimido-benzimidazole |
| CN101528250A (zh) | 2005-07-08 | 2009-09-09 | 研究及应用科学协会股份有限公司 | 黑皮质素受体的配体 |
| CN105837661B (zh) * | 2005-07-08 | 2024-10-15 | 益普生制药股份有限公司 | 黑皮质素受体配体 |
| EP2148692B1 (en) * | 2007-05-25 | 2017-01-25 | Ipsen Pharma S.A.S. | Melanocortin receptor ligands modified with hydantoin |
| US20100173834A1 (en) | 2007-06-15 | 2010-07-08 | Zheng Xin Dong | Cyclic peptide melanocortin receptor ligands |
| RU2453328C2 (ru) | 2007-11-05 | 2012-06-20 | Ипсен Фарма С.А.С. | Применение меланокортинов для лечения чувствительности к инсулину |
| WO2009151383A1 (en) * | 2008-06-09 | 2009-12-17 | Palatin Technologies, Inc. | Melanocortin receptor-specific peptides for the treatment of obesity and other diseases associated with melanocortin receptor function |
| NZ596617A (en) * | 2009-06-08 | 2014-04-30 | Palatin Technologies Inc | Melanocortin receptor-specific peptides |
| UY32690A (es) * | 2009-06-08 | 2011-01-31 | Astrazeneca Ab | Péptidos específicos para receptores de melanocortina |
| EP2461681A4 (en) * | 2009-08-05 | 2013-04-24 | Ipsen Pharma Sas | USE OF MELANOCORTINS FOR TREATING DYSLIPIDEMIA |
| US20120226018A1 (en) | 2009-11-16 | 2012-09-06 | Ipsen Pharma, S.A.S. | Process for the Synthesis of Ac-Arg-Cyclo(Cys-D-Ala-His-D-Phe-Arg-Trp-Cys)-NH2 |
| ES2654147T3 (es) | 2009-11-16 | 2018-02-12 | Ipsen Pharma S.A.S. | Composiciones farmacéuticas de ligandos del receptor de melanocortina |
| EP2720684B1 (en) | 2011-06-14 | 2019-01-16 | Ipsen Pharma S.A.S. | A sustained-release composition containing peptides as the active ingredient |
| EP2705835A1 (en) | 2012-06-08 | 2014-03-12 | Ipsen Pharma S.A.S. | Aqueous gelling compositions of soluble active pharmaceutical peptides providing modified release |
| RU2020120797A (ru) * | 2013-03-15 | 2020-07-02 | Ритм Фармасьютикалз, Инк. | Пептидные композиции |
| CA3209602A1 (en) * | 2013-03-15 | 2014-09-18 | Rhythm Pharmaceuticals, Inc. | Pharmaceutical compositions |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2785889C1 (ru) * | 2015-09-30 | 2022-12-14 | Ритм Фармасьютикалз, Инк. | Способ лечения нарушений, ассоциированных с путем рецептора меланокортина 4 |
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