ES2072137T3 - Antagonistas nonapeptidos de la bombesina. - Google Patents
Antagonistas nonapeptidos de la bombesina.Info
- Publication number
- ES2072137T3 ES2072137T3 ES92900740T ES92900740T ES2072137T3 ES 2072137 T3 ES2072137 T3 ES 2072137T3 ES 92900740 T ES92900740 T ES 92900740T ES 92900740 T ES92900740 T ES 92900740T ES 2072137 T3 ES2072137 T3 ES 2072137T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- trp
- halogen
- group
- phe
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- QXZBMSIDSOZZHK-DOPDSADYSA-N 31362-50-2 Chemical compound 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=1C2=CC=CC=C2NC=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=CNC=N1 QXZBMSIDSOZZHK-DOPDSADYSA-N 0.000 title 1
- 102000013585 Bombesin Human genes 0.000 title 1
- 108010051479 Bombesin Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 abstract 9
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical compound BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 4
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical compound ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 abstract 3
- 229910052801 chlorine Inorganic materials 0.000 abstract 3
- 239000000460 chlorine Substances 0.000 abstract 3
- -1 CARBOXYL GROUP Chemical group 0.000 abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- 229910052794 bromium Inorganic materials 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 239000011737 fluorine Substances 0.000 abstract 2
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000007513 acids Chemical class 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 239000002790 bombesin antagonist Substances 0.000 abstract 1
- 150000007524 organic acids Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229920001184 polypeptide Polymers 0.000 abstract 1
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 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
- C07K7/02—Linear peptides containing at least one abnormal peptide link
-
- 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
- C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
- C07K7/086—Bombesin; Related peptides
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
LOS NUEVOS PSEUDOPOLIPEPTIDOS DE ESTA INVENCION SON POTENTES ANTAGONISTAS DE LA BOMBESINA. SE PRESENTAN LOS PROCESOS PARA SU PRODUCCION, LAS COMPOSICIONES FARMACEUTICAS QUE CONTIENEN DICHOS POLIPEPTIDOS Y SU UTILIZACION COMO AGENTES FARMACEUTICAMENTE ACTIVOS. EN PARTICULAR, LA PRESENTE INVENCION SE REFIERE A PSEUDOPEPTIDOS QUE CONTIENEN UNA UNIDAD NONAPEPTIDA DE LA FORMULA (I): X A9 C1-10, FENILO O FENILALQUILO C7-10; X ES HIDROGENO O UN ENLACE SENCILLO QUE SE UNE A A2, EL RESIDUO ACILO DE UN ACIDO ORGANICO O UN GRUPO DE LA FORMULA R1COLQUILO C1-10, FENILO O FENILALQUILO C7-10; 2) R1CO (R3)-COIL-C7-10-ALQUILO C710, R3 ES HIDROGENO O ALQUILO C1-10; B) R4-O-CO EN DONDE R4 ES ALQUILO C1-10, FENILO O FENILALQUILO C7-10. A1 ES D -, L MPP, TRP O TRP SUSTITUIDO EN EL ANILLO DE BENCENO POR UNO O MAS MIEMBROS SELECCIONADOS DEL GRUPO QUE CONSISTE EN HALOGENO, NO2, NH2, OH, ALQUILO C1-3 Y ALCOXI C1-3 EN DONDE EL HALOGENO ES FLUOR, CLORO Y BROMO, A2 ES ASN, DPA, GLN, HIS, MEHIS, HIS(BZ), HIS(Z) O UN GRUPO DE LA FORMULA DPA (X), ASP (Y), GLU [-] Y GLU (Y); EN DONDE X ES COMO SE HA DESCRITO ARRIBA, Y ES -OR5 O R6-NR7 EN DONDE R5 ES HIDROGENO, ALQUILO C1-3 O FENILO; R6 ES HIDROGENO O ALQUILO C1-3; R7 ES HIDROGENO, ALQUILO C1-3 O -NHCONH2 Y [-] ES UN ENLACE SENCILLO QUE UNE EL GRUPO CARBOXILO LATERAL CON EL GRUPO ALFA AMINO DE A1 DONDE X ES UN ENLACE SENCILLO, A3 ES NAL, PAL, TPI, TRP, METRP, TRP(FOR) O TRP SUSTITUIDO EN EL ANILLO DE BENCENO POR UNO O MAS MIEMBROS SELECCIONADOS DEL GRUPO QUE CONSISTE EN HALOGENO, NO2, NH2, OH, ALQUILO C1-3 Y ALCOXI C1-3 EN DONDE EL HALOGENO ES FLUOR, CLORO Y BROMO; A4 ES ALA, MEALA O GLN; A5 ES VAL O MEVAL; A6 ES GLY, PHE O D LA; A7 ES HIS, MEHIS, HIS(BZ), HIS(Z), LYS(Z) O PAL; A8 ES UN ISOSTERO REDUCIDO DE LEU O PHE; A9 ES LEU, PHE, TPI, TRP O TRP SUSTITUIDO EN EL ANILLO DE BENCENO POR UNO O MAS MIEMBROS SELECCIONADOS DEL GRUPO QUE CONSISTE EN HALOGENO, NO2, NH2, OH, ALQUILO C1-3 Y ALCOXI C1-3 EN DONDE EL HALOGENO ES FLUOR, CLORO Y BROMO; SIEMPRE QUE SI A9ES LEU O PHE, A1 SEA DISTINTO DE D DE LEU O PHE Y LAS SALES DE LOS MISMOS CON ACIDOS FARMACEUTICAMENTE ACEPTABLES.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US07/619,747 US5244883A (en) | 1990-11-29 | 1990-11-29 | Nonapeptide bombesin antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2072137T3 true ES2072137T3 (es) | 1995-07-01 |
Family
ID=24483142
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES92900740T Expired - Lifetime ES2072137T3 (es) | 1990-11-29 | 1991-11-15 | Antagonistas nonapeptidos de la bombesina. |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US5244883A (es) |
| EP (1) | EP0559756B1 (es) |
| JP (1) | JPH06503090A (es) |
| KR (1) | KR100225679B1 (es) |
| AT (1) | ATE120760T1 (es) |
| AU (1) | AU657723B2 (es) |
| CA (1) | CA2097192C (es) |
| CZ (1) | CZ281533B6 (es) |
| DE (1) | DE69108738T2 (es) |
| DK (1) | DK0559756T3 (es) |
| ES (1) | ES2072137T3 (es) |
| FI (1) | FI104253B (es) |
| GR (1) | GR3015866T3 (es) |
| HU (2) | HU213114B (es) |
| IE (1) | IE62722B1 (es) |
| LV (1) | LV5794B4 (es) |
| MC (1) | MC2326A1 (es) |
| NO (1) | NO311362B1 (es) |
| NZ (1) | NZ240628A (es) |
| PL (1) | PL169498B1 (es) |
| PT (1) | PT99667B (es) |
| RU (1) | RU2115659C1 (es) |
| SK (1) | SK283541B6 (es) |
| WO (1) | WO1992009626A1 (es) |
| YU (1) | YU48751B (es) |
| ZA (1) | ZA919387B (es) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5877277A (en) * | 1987-09-24 | 1999-03-02 | Biomeasure, Inc. | Octapeptide bombesin analogs |
| US5723578A (en) * | 1987-09-24 | 1998-03-03 | The Administrators Of Tulane Educational Fund | Peptide analogs of bombesin |
| CA2042027A1 (en) * | 1989-09-15 | 1991-03-16 | Arthur E. Bogden | Treatment of colon cancer |
| US5162336A (en) * | 1990-06-21 | 1992-11-10 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Tetrahydro-pyrido-indoles as cholecystokinin and gastrin antagonists |
| US5834433A (en) * | 1990-07-26 | 1998-11-10 | Merrell Pharmaceuticals Inc. | Compounds and pharmaceutical uses of peptides of bombesin and GRP |
| US5369094A (en) * | 1990-11-29 | 1994-11-29 | The Administrators Of The Tulane Educational Fund | Polypeptide bombesin antagonists |
| AU668909B2 (en) * | 1992-02-07 | 1996-05-23 | Merrell Dow Pharmaceuticals Inc. | Phenylalanine analogs of bombesin |
| US5620955A (en) * | 1993-06-18 | 1997-04-15 | Peptide Technologies Corporation | Bombesin receptor antagonists and uses thereof |
| DE4320201A1 (de) * | 1993-06-18 | 1995-01-12 | Asta Medica Ag | Verwendung von Cetrorelix und weiteren Nona- und Dekapeptiden zur Herstellung eines Arzneimittels zur Bekämpfung von Aids und zur Wachstumsstimulation |
| US5997870A (en) * | 1994-06-03 | 1999-12-07 | Ludwig Institute For Cancer Research | Isolated peptides which bind to HLA-B44 Molecules |
| US5650395A (en) * | 1995-03-13 | 1997-07-22 | Hurel; Steven | Treatment of pulmonary hypertension |
| US5972895A (en) * | 1996-12-11 | 1999-10-26 | A. Glenn Braswell | Composition and method for increasing growth hormone levels |
| JP2002506424A (ja) | 1997-04-22 | 2002-02-26 | キュレイター オブ ザ ユニバーシィティ オブ ミズーリ | ガストリン受容体−親和性ペプチド結合体 |
| RU2153623C1 (ru) * | 1999-04-20 | 2000-07-27 | Сысун Виктор Викторович | Светосигнальный огонь кругового обзора |
| EP1813625B1 (en) * | 2001-03-06 | 2009-04-29 | Il Consorzio Ferrara Richerche | Method of modulating the profileration of medullary thyroid carcinoma cells |
| US7922998B2 (en) * | 2003-01-13 | 2011-04-12 | Bracco Imaging S.P.A. | Gastrin releasing peptide compounds |
| US7226577B2 (en) | 2003-01-13 | 2007-06-05 | Bracco Imaging, S. P. A. | Gastrin releasing peptide compounds |
| US7611692B2 (en) * | 2003-01-13 | 2009-11-03 | Bracco Imaging S.P.A. | Gastrin releasing peptide compounds |
| US7850947B2 (en) * | 2003-01-13 | 2010-12-14 | Bracco Imaging S.P.A. | Gastrin releasing peptide compounds |
| AU2003303714B2 (en) * | 2003-01-13 | 2009-02-19 | Bracco Imaging S.P.A. | Improved linkers for radiopharmaceutical compounds |
| US20060239923A1 (en) * | 2003-01-13 | 2006-10-26 | Bracco Imaging S.P.A. | Gastrin releasing peptide compounds |
| US8420050B2 (en) * | 2003-01-13 | 2013-04-16 | Bracco Imaging S.P.A. | Gastrin releasing peptide compounds |
| US7795385B2 (en) * | 2004-12-17 | 2010-09-14 | Bexar Global, Inc. | Use of bombesin/gastrin-releasing peptide antagonists for the treatment of inflammatory conditions, acute lung injury and bipolar disorder |
| US8101580B2 (en) | 2005-04-21 | 2012-01-24 | Astellas Pharma Inc. | Therapeutic agent for irritable bowel syndrome |
| MX2009002492A (es) | 2006-09-08 | 2009-08-28 | Bayer Schering Pharma Ag | Agentes que comprenden compuestos marcados con 18f y metodos relacionados. |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4839465A (en) * | 1987-01-20 | 1989-06-13 | Sterling Drug Inc. | Di-(D-tryptophyl and/or tetrahydropyridoindolylcarbonyl)-containing peptide amides and process for preparation thereof |
| JP2795449B2 (ja) * | 1987-09-24 | 1998-09-10 | ジ・アドミニストレーターズ・オブ・ザ・ツーレイン・エデュケイショナル・ファンド | 治療用ペプチド |
| GB8808768D0 (en) * | 1988-04-14 | 1988-05-18 | Erba Carlo Spa | Peptide ligands for bombesin receptors |
| GR1000608B (el) * | 1988-07-21 | 1992-08-31 | Erba Carlo Spa | Μεθοδος για την παρασκευη ανταγωνιστων bombesin. |
| WO1990003980A1 (en) * | 1988-10-14 | 1990-04-19 | Administrators Of The Tulane Educational Fund | Therapeutic peptides |
-
1990
- 1990-11-29 US US07/619,747 patent/US5244883A/en not_active Expired - Lifetime
-
1991
- 1991-11-15 DK DK92900740.9T patent/DK0559756T3/da active
- 1991-11-15 SK SK551-93A patent/SK283541B6/sk unknown
- 1991-11-15 JP JP4501946A patent/JPH06503090A/ja active Granted
- 1991-11-15 AU AU90645/91A patent/AU657723B2/en not_active Ceased
- 1991-11-15 DE DE69108738T patent/DE69108738T2/de not_active Expired - Fee Related
- 1991-11-15 AT AT92900740T patent/ATE120760T1/de not_active IP Right Cessation
- 1991-11-15 CA CA002097192A patent/CA2097192C/en not_active Expired - Fee Related
- 1991-11-15 MC MC912326D patent/MC2326A1/xx unknown
- 1991-11-15 WO PCT/US1991/008534 patent/WO1992009626A1/en not_active Ceased
- 1991-11-15 HU HU9301567A patent/HU213114B/hu unknown
- 1991-11-15 EP EP92900740A patent/EP0559756B1/en not_active Expired - Lifetime
- 1991-11-15 ES ES92900740T patent/ES2072137T3/es not_active Expired - Lifetime
- 1991-11-15 RU RU93041053A patent/RU2115659C1/ru not_active IP Right Cessation
- 1991-11-15 CZ CS931006A patent/CZ281533B6/cs not_active IP Right Cessation
- 1991-11-15 PL PL91300477A patent/PL169498B1/pl not_active IP Right Cessation
- 1991-11-15 KR KR1019930701620A patent/KR100225679B1/ko not_active Expired - Fee Related
- 1991-11-18 NZ NZ24062891A patent/NZ240628A/en not_active IP Right Cessation
- 1991-11-22 YU YU183491A patent/YU48751B/sh unknown
- 1991-11-28 ZA ZA919387A patent/ZA919387B/xx unknown
- 1991-11-28 IE IE414091A patent/IE62722B1/en not_active IP Right Cessation
- 1991-11-29 PT PT99667A patent/PT99667B/pt not_active IP Right Cessation
-
1993
- 1993-05-28 FI FI932457A patent/FI104253B/fi not_active IP Right Cessation
- 1993-05-28 NO NO19931977A patent/NO311362B1/no unknown
-
1995
- 1995-04-19 GR GR950400995T patent/GR3015866T3/el unknown
- 1995-06-27 HU HU95P/P00466P patent/HU211603A9/hu unknown
-
1996
- 1996-07-22 LV LV960305A patent/LV5794B4/xx unknown
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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