WO2006064530A3 - Analogues de la dermorphine a activite analgesique - Google Patents
Analogues de la dermorphine a activite analgesique Download PDFInfo
- Publication number
- WO2006064530A3 WO2006064530A3 PCT/IT2005/000733 IT2005000733W WO2006064530A3 WO 2006064530 A3 WO2006064530 A3 WO 2006064530A3 IT 2005000733 W IT2005000733 W IT 2005000733W WO 2006064530 A3 WO2006064530 A3 WO 2006064530A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- dermorphin
- analgesic activity
- aminoacid
- fact
- analogs
- Prior art date
Links
- FHZPGIUBXYVUOY-VWGYHWLBSA-N Dermorphin Chemical class C([C@H](N)C(=O)N[C@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)NCC(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)C1=CC=C(O)C=C1 FHZPGIUBXYVUOY-VWGYHWLBSA-N 0.000 title abstract 3
- 230000000202 analgesic effect Effects 0.000 title abstract 2
- 101800002242 Dermorphin Proteins 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 2
- 239000004475 Arginine Substances 0.000 abstract 1
- 150000007650 D alpha amino acids Chemical class 0.000 abstract 1
- QNAYBMKLOCPYGJ-UWTATZPHSA-N D-alanine Chemical compound C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 abstract 1
- 235000001014 amino acid Nutrition 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 abstract 1
- 210000000929 nociceptor Anatomy 0.000 abstract 1
- 108091008700 nociceptors Proteins 0.000 abstract 1
- 229940127240 opiate Drugs 0.000 abstract 1
- 230000002093 peripheral effect Effects 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
L'invention concerne des nouveaux analogues heptapeptides opioïdes de la dermorphine, qui se caractérisent en ce que, comme la dermorphine, ils conservent un reste de tyrosine en position 1 et un Dα-aminoacide, de préférence D-Ala, en position 2, et en ce qu'en position 7, ils possèdent l'aminoacide de basicité maximum, à savoir l'arginine. Le peptide préféré de l'invention, l'Arg7-dermorphine, appelé arginorphine, possède une activité analgésique puissante. Cette activité se produit largement au niveau du nocicepteur à opioïde périphérique, sans les effets secondaires centraux graves typiques des opiacés.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05823581A EP1831244A2 (fr) | 2004-12-15 | 2005-12-14 | Analogues de la dermorphine a activite analgesique |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ITRM2004A000607 | 2004-12-15 | ||
| ITRM20040607 ITRM20040607A1 (it) | 2004-12-15 | 2004-12-15 | Analoghi della dermorfina ad attivita' analgesica. |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2006064530A2 WO2006064530A2 (fr) | 2006-06-22 |
| WO2006064530A3 true WO2006064530A3 (fr) | 2007-02-08 |
Family
ID=36358951
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/IT2005/000733 WO2006064530A2 (fr) | 2004-12-15 | 2005-12-14 | Analogues de la dermorphine a activite analgesique |
Country Status (3)
| Country | Link |
|---|---|
| EP (1) | EP1831244A2 (fr) |
| IT (1) | ITRM20040607A1 (fr) |
| WO (1) | WO2006064530A2 (fr) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2012255119B2 (en) | 2011-05-18 | 2017-04-20 | Mederis Diabetes, Llc | Improved peptide pharmaceuticals for insulin resistance |
| KR102126484B1 (ko) | 2011-05-18 | 2020-06-25 | 메더리스 다이어비티즈, 엘엘씨 | 개선된 펩티드 제약 |
| WO2014081864A1 (fr) | 2012-11-20 | 2014-05-30 | Eumederis Pharmaceuticals, Inc. | Agents pharmaceutiques peptidiques améliorés |
| JP6525456B2 (ja) | 2012-11-20 | 2019-06-05 | メデリス ダイアビーティーズ，エルエルシー | インスリン抵抗性のための改善されたペプチド製剤 |
| AU2015266854B2 (en) | 2014-05-28 | 2020-03-26 | Mederis Diabetes, Llc | Improved peptide pharmaceuticals for insulin resistance |
| PT3735295T (pt) | 2018-01-03 | 2024-12-11 | Mederis Diabetes Llc | Farmacêuticos peptídicos melhorados para tratamento de nash e outras disfunções |
| US12171806B2 (en) | 2021-09-28 | 2024-12-24 | Spitfire Pharma Llc | Therapeutic regimens and methods for lowering blood glucose and/or body weight using GLP-1R and GCGR balanced agonists |
| PL439243A1 (pl) * | 2021-10-18 | 2023-04-24 | Instytut Medycyny Doświadczalnej I Klinicznej Im. Mirosława Mossakowskiego Polskiej Akademii Nauk | Nowy analog dermorfiny jako lek przeciwbólowy do stosowania w leczeniu bólu przewlekłego |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5602100A (en) * | 1988-06-30 | 1997-02-11 | Astra Ab | Dermorphin analogs having pharmacological activity |
-
2004
- 2004-12-15 IT ITRM20040607 patent/ITRM20040607A1/it unknown
-
2005
- 2005-12-14 EP EP05823581A patent/EP1831244A2/fr not_active Withdrawn
- 2005-12-14 WO PCT/IT2005/000733 patent/WO2006064530A2/fr active Application Filing
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5602100A (en) * | 1988-06-30 | 1997-02-11 | Astra Ab | Dermorphin analogs having pharmacological activity |
Non-Patent Citations (1)
| Title |
|---|
| NEGRI, LUCIA ET AL: "Dermorphin-related peptides from the skin of Phyllomedusa bicolor and their amidated analogs activate two .mu. opioid receptor subtypes that modulate antinociception and catalepsy in the rat", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA , 89(15), 7203-7 CODEN: PNASA6; ISSN: 0027-8424, 1992, XP002382460 * |
Also Published As
| Publication number | Publication date |
|---|---|
| ITRM20040607A1 (it) | 2005-03-15 |
| WO2006064530A2 (fr) | 2006-06-22 |
| EP1831244A2 (fr) | 2007-09-12 |
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