AR021173A1 - CYCLE PEPTIDES WITH BRADIQUININE ANTAGONIST ACTIVITY, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM AND USE OF SUCH PEPTIDES IN THE PREPARATION OF MEDICINES. - Google Patents
CYCLE PEPTIDES WITH BRADIQUININE ANTAGONIST ACTIVITY, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM AND USE OF SUCH PEPTIDES IN THE PREPARATION OF MEDICINES.Info
- Publication number
- AR021173A1 AR021173A1 ARP990103864A ARP990103864A AR021173A1 AR 021173 A1 AR021173 A1 AR 021173A1 AR P990103864 A ARP990103864 A AR P990103864A AR P990103864 A ARP990103864 A AR P990103864A AR 021173 A1 AR021173 A1 AR 021173A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- amino
- groups
- arg
- alkyl
- Prior art date
Links
- 239000005557 antagonist Substances 0.000 title abstract 2
- 102000004196 processed proteins & peptides Human genes 0.000 title 2
- 108090000765 processed proteins & peptides Proteins 0.000 title 2
- 239000003814 drug Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 abstract 9
- -1 amino, aminomethyl Chemical group 0.000 abstract 6
- 125000003277 amino group Chemical group 0.000 abstract 5
- 125000003837 (C1-C20) alkyl group Chemical group 0.000 abstract 4
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical compound NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 abstract 4
- 235000001014 amino acid Nutrition 0.000 abstract 4
- 150000001413 amino acids Chemical class 0.000 abstract 4
- 125000002252 acyl group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 101710085045 B2 bradykinin receptor Proteins 0.000 abstract 2
- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline Chemical compound NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 abstract 2
- RHGKLRLOHDJJDR-UHFFFAOYSA-N Ndelta-carbamoyl-DL-ornithine Natural products OC(=O)C(N)CCCNC(N)=O RHGKLRLOHDJJDR-UHFFFAOYSA-N 0.000 abstract 2
- 235000013477 citrulline Nutrition 0.000 abstract 2
- 229960002173 citrulline Drugs 0.000 abstract 2
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 abstract 2
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 102000001189 Cyclic Peptides Human genes 0.000 abstract 1
- 108010069514 Cyclic Peptides Proteins 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
- C07K7/50—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
- C07K7/60—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation occurring through the 4-amino group of 2,4-diamino-butanoic acid
-
- 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
- C07K7/18—Kallidins; Bradykinins; Related peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- General Health & Medical Sciences (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Péptidos cíclicos con actividad como antagonista específicos del receptor B2 de bradiquinina (BK) que tienen la formula general (1), donde: A1 es: H,un aminoácido básico, opcionalmente acilado en el grupo amino de cadena alfa o lateral con un grupo R14-CO donde R14 es un grupo alquilo C1-20, seleccionadodel grupo formado por: Arg, Omo-Arg, NMA, NIO, Lys, Orn, Dab, Dpr, His, citrulina, 3,4-dehidro-Arg, 3,4-dehidro-Orn, Pro 3-, 4-, o 5-sustituido(cis o trans) con grupos amino o guanidino y, opcionalmente sustituido con grupos alquilo C1-6 o con grupos acilo C1-6 en el grupo amino de cadena alfa olateral, Phe o-m-p sustituido con un grupo seleccionado de grupos amino, aminometilo, guanidina, metilguanidina, imidina, imidinometilo, N-metilguanidina;donde los grupos amino, guanidino, imidino pueden estar opcionalmente alquilados con uno o más grupos alquilo C1-3; un aminoácido, opcionalmente aciladoen el grupo alfa amino con un grupo R14-CO donde R14 es un grupo alquilo C1-20 de la formula(2), donde h=1-4, R14 es un grupo alquilo C1-20, un aminoácido,opcionalmente acilado en el grupo alfa amino con un grupo R14-CO donde R14 es un grupo alquilo C1-20, de la formula (3), donde k= 1-5, y R16, R17 y R18donde son iguales o diferentes, sonun grupo alquilo C1-4; un grupo acilo que tiene una cadena lateral básica, seleccionado del grupo: o-, m-, p-amino-benzoilo, o-, m-, p-acetil-guanidino-benzoilo, o-, m-, p-acetil-amidono-benzoilo, CO-(CH2) f-NH-U donde f = 1-6 y U = H o un grupo seleccionado imidina,imidinometilo, N-metilimidino; A2 es: un aminoácido básico seleccionado del grupo: Arg, Omo-Arg, NMA, NIO, Lys, Orn, Dab, Dpr, His, citrulina, 3,4-dehidro-Arg, 3,4-dehidro-Orn, Pro 3-, 4-, o 5-sustituido (cis o trans) con grupos amino o guanidino y opcionalmente sustituidos con grupos alquilo C1-6o con grupos acilo C1-6 en el grupo amino de cadena alfa o lateral, Phe o-m-p sustituido con un grupo seleccionado de amino, aminometilo, guanidina,metilguanidina, imidina, imidinometilo, N-metilguanidina; donde los grupos amino, guanidino, imidino pueden estar opcionalmente alquilados con uno o másCyclic peptides with activity as a specific antagonist of the Bradykinin B2 receptor (BK) having the general formula (1), where: A1 is: H, a basic amino acid, optionally acylated in the alpha or side chain amino group with an R14 group -CO where R14 is a C1-20 alkyl group, selected from the group consisting of: Arg, Omo-Arg, NMA, NIO, Lys, Orn, Dab, Dpr, His, citrulline, 3,4-dehydro-Arg, 3,4 -dehydro-Orn, Pro 3-, 4-, or 5-substituted (cis or trans) with amino or guanidino groups and, optionally substituted with C1-6 alkyl groups or with C1-6 acyl groups in the alpha chain amino group Olateral, Phe omp substituted with a group selected from amino, aminomethyl, guanidine, methylguanidine, imidine, imidinomethyl, N-methylguanidine groups, where the amino, guanidino, imidino groups may optionally be alkylated with one or more C1-3 alkyl groups; an amino acid, optionally acylated in the alpha amino group with an R14-CO group where R14 is a C1-20 alkyl group of the formula (2), where h = 1-4, R14 is a C1-20 alkyl group, an amino acid, optionally acylated in the alpha amino group with an R14-CO group where R14 is a C1-20 alkyl group, of the formula (3), where k = 1-5, and R16, R17 and R18 where they are the same or different, are a group C1-4 alkyl; an acyl group having a basic side chain, selected from the group: o-, m-, p-amino-benzoyl, o-, m-, p-acetyl-guanidino-benzoyl, o-, m-, p-acetyl- amidono-benzoyl, CO- (CH2) f-NH-U where f = 1-6 and U = H or a selected group imidine, imidinomethyl, N-methylimidino; A2 is: a basic amino acid selected from the group: Arg, Omo-Arg, NMA, NIO, Lys, Orn, Dab, Dpr, His, citrulline, 3,4-dehydro-Arg, 3,4-dehydro-Orn, Pro 3 -, 4-, or 5-substituted (cis or trans) with amino or guanidino groups and optionally substituted with C1-6 alkyl groups with C1-6 acyl groups in the alpha or side chain amino group, Phe omp substituted with a group selected from amino, aminomethyl, guanidine, methylguanidine, imidine, imidinomethyl, N-methylguanidine; where the amino, guanidino, imidino groups may be optionally alkylated with one or more
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT1998MI001832A IT1301992B1 (en) | 1998-08-04 | 1998-08-04 | CYCLIC PEPTIDES WITH SPECIFIC ANTAGONIST ACTIVITY FOR THE BRADYCHININ RECEPTOR B2 AND FORMULATIONS THAT CONTAIN THEM. |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR021173A1 true AR021173A1 (en) | 2002-07-03 |
Family
ID=11380610
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990103864A AR021173A1 (en) | 1998-08-04 | 1999-08-03 | CYCLE PEPTIDES WITH BRADIQUININE ANTAGONIST ACTIVITY, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM AND USE OF SUCH PEPTIDES IN THE PREPARATION OF MEDICINES. |
Country Status (4)
| Country | Link |
|---|---|
| AR (1) | AR021173A1 (en) |
| AU (1) | AU5289799A (en) |
| IT (1) | IT1301992B1 (en) |
| WO (1) | WO2000008049A1 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10745492B1 (en) * | 2019-04-03 | 2020-08-18 | Ark Diagnostics, Inc. | Antibodies to symmetrically dimethylated arginine analytes and use thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5648333A (en) * | 1988-11-24 | 1997-07-15 | Hoechst Aktiengesellschaft | Peptides having bradykinin antagonist action |
-
1998
- 1998-08-04 IT IT1998MI001832A patent/IT1301992B1/en active IP Right Grant
-
1999
- 1999-07-30 AU AU52897/99A patent/AU5289799A/en not_active Abandoned
- 1999-07-30 WO PCT/EP1999/005458 patent/WO2000008049A1/en active Application Filing
- 1999-08-03 AR ARP990103864A patent/AR021173A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IT1301992B1 (en) | 2000-07-20 |
| AU5289799A (en) | 2000-02-28 |
| WO2000008049A1 (en) | 2000-02-17 |
| ITMI981832A0 (en) | 1998-08-04 |
| ITMI981832A1 (en) | 2000-02-04 |
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