AR030224A1 - BOMBESINE ANALOGS, FOR THE TREATMENT OF CANCER, A SOLID PHASE SYNTHESIS PROCEDURE, A PHARMACEUTICAL COMPOSITION AND THE USE OF SUCH PEPTIDES FOR THE MANUFACTURE OF A MEDICINAL PRODUCT. - Google Patents
BOMBESINE ANALOGS, FOR THE TREATMENT OF CANCER, A SOLID PHASE SYNTHESIS PROCEDURE, A PHARMACEUTICAL COMPOSITION AND THE USE OF SUCH PEPTIDES FOR THE MANUFACTURE OF A MEDICINAL PRODUCT.Info
- Publication number
- AR030224A1 AR030224A1 ARP010102428A ARP010102428A AR030224A1 AR 030224 A1 AR030224 A1 AR 030224A1 AR P010102428 A ARP010102428 A AR P010102428A AR P010102428 A ARP010102428 A AR P010102428A AR 030224 A1 AR030224 A1 AR 030224A1
- Authority
- AR
- Argentina
- Prior art keywords
- peptides
- alpha
- cancer
- treatment
- manufacture
- Prior art date
Links
- 108090000765 processed proteins & peptides Proteins 0.000 title abstract 8
- 102000004196 processed proteins & peptides Human genes 0.000 title abstract 6
- 206010028980 Neoplasm Diseases 0.000 title abstract 3
- 201000011510 cancer Diseases 0.000 title abstract 3
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 229940126601 medicinal product Drugs 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 238000010532 solid phase synthesis reaction Methods 0.000 title 1
- 102000013585 Bombesin Human genes 0.000 abstract 2
- 108010051479 Bombesin Proteins 0.000 abstract 2
- DNDCVAGJPBKION-DOPDSADYSA-N bombesin Chemical class C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC=1NC2=CC=CC=C2C=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1NC(=O)CC1)C(C)C)C1=CN=CN1 DNDCVAGJPBKION-DOPDSADYSA-N 0.000 abstract 2
- NILQLFBWTXNUOE-UHFFFAOYSA-N 1-aminocyclopentanecarboxylic acid Chemical compound OC(=O)C1(N)CCCC1 NILQLFBWTXNUOE-UHFFFAOYSA-N 0.000 abstract 1
- 125000001431 2-aminoisobutyric acid group Chemical group [#6]C([#6])(N*)C(*)=O 0.000 abstract 1
- QIVBCDIJIAJPQS-SECBINFHSA-N D-tryptophane Chemical group C1=CC=C2C(C[C@@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-SECBINFHSA-N 0.000 abstract 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 150000001371 alpha-amino acids Chemical class 0.000 abstract 1
- 235000008206 alpha-amino acids Nutrition 0.000 abstract 1
- FUOOLUPWFVMBKG-UHFFFAOYSA-N alpha-amino-isobutyric acid Natural products CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 abstract 1
- 235000001014 amino acid Nutrition 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Landscapes
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Análogo de bombesina, que comprenden un péptido que tiene la formula X-D-Phe-Gln-R1-R2-Val-R3-His-R4-NH2 donde X es acetilo o un grupo alcanoilo recto ramificado o cíclico de C3-16, o X está seleccionado R1 es Trp o D-Trp, R2 es Ala, Aib oDeg, R3 es Gly, Aib, Deg, Dpg o Ac5c, R4 es Leu o Ile o un grupo protector carboxi hidrolizable; donde por lo menos uno de R2 o R3 es un amino ácido alfa, alfa-dialquilado; o una sal farmacéuticamente aceptable del mismo péptido; en donde Aib es el ácido alfa-aminoisobutírico, Dpg es alfa-alfa-di-n-propilglicina y Ac5c es el ácido 1-aminociclopentano carboxílico; que son antagonistas de péptidos de bombesina y del tipo de bombesina y que son utiles en el tratamiento de cáncer. Se refiere en particular al diseno y síntesis de los nuevos péptidos que incorporan alfa, alfa-amino ácidos de manera específica de un sitio. También describe métodos para la generacion de estos péptidos, composiciones que contienen los péptidos y el uso de dichos péptidos para la manufactura de un medicamento para aplicaciones farmacologicas de estos péptidos especialmente para el tratamiento y prevencion del cáncer.Bombesin analog, comprising a peptide having the formula XD-Phe-Gln-R1-R2-Val-R3-His-R4-NH2 where X is acetyl or a straight or branched C3-16 cyclic alkanoyl group, or X R1 is Trp or D-Trp, R2 is Ala, Aib oDeg, R3 is Gly, Aib, Deg, Dpg or Ac5c, R4 is Leu or Ile or a hydrolysable carboxy protecting group; where at least one of R2 or R3 is an alpha, alpha-dialkylated amino acid; or a pharmaceutically acceptable salt of the same peptide; wherein Aib is alpha-aminoisobutyric acid, Dpg is alpha-alpha-di-n-propylglycine and Ac5c is 1-aminocyclopentane carboxylic acid; that they are antagonists of bombesin peptides and the type of bombesin and that they are useful in the treatment of cancer. It refers in particular to the design and synthesis of new peptides that incorporate alpha, alpha-amino acids specifically from a site. It also describes methods for the generation of these peptides, compositions containing the peptides and the use of said peptides for the manufacture of a medicament for pharmacological applications of these peptides especially for the treatment and prevention of cancer.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/630,333 US6989371B1 (en) | 1996-08-16 | 2000-07-31 | Bombesin analogs for treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR030224A1 true AR030224A1 (en) | 2003-08-13 |
Family
ID=37515843
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010102428A AR030224A1 (en) | 2000-07-31 | 2001-05-22 | BOMBESINE ANALOGS, FOR THE TREATMENT OF CANCER, A SOLID PHASE SYNTHESIS PROCEDURE, A PHARMACEUTICAL COMPOSITION AND THE USE OF SUCH PEPTIDES FOR THE MANUFACTURE OF A MEDICINAL PRODUCT. |
Country Status (2)
| Country | Link |
|---|---|
| AR (1) | AR030224A1 (en) |
| MY (1) | MY136393A (en) |
-
2001
- 2001-05-22 AR ARP010102428A patent/AR030224A1/en active IP Right Grant
- 2001-05-24 MY MYPI20012469 patent/MY136393A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MY136393A (en) | 2008-09-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |