PE45295A1 - PROTEASE INHIBITING PEPTIDES - Google Patents
PROTEASE INHIBITING PEPTIDESInfo
- Publication number
- PE45295A1 PE45295A1 PE1995260194A PE26019495A PE45295A1 PE 45295 A1 PE45295 A1 PE 45295A1 PE 1995260194 A PE1995260194 A PE 1995260194A PE 26019495 A PE26019495 A PE 26019495A PE 45295 A1 PE45295 A1 PE 45295A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- compounds
- formula
- aralkyl
- aryl
- Prior art date
Links
- 108091005804 Peptidases Proteins 0.000 title 1
- 239000004365 Protease Substances 0.000 title 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- 102000004196 processed proteins & peptides Human genes 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000013522 chelant Substances 0.000 abstract 3
- 150000001413 amino acids Chemical class 0.000 abstract 2
- -1 AMINO GROUP Chemical group 0.000 abstract 1
- 101150047265 COR2 gene Proteins 0.000 abstract 1
- 101100467189 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) QCR2 gene Proteins 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 229940039227 diagnostic agent Drugs 0.000 abstract 1
- 239000000032 diagnostic agent Substances 0.000 abstract 1
- 150000002009 diols Chemical class 0.000 abstract 1
- 239000002184 metal Substances 0.000 abstract 1
- SONNWYBIRXJNDC-VIFPVBQESA-N phenylephrine Chemical class CNC[C@H](O)C1=CC=CC(O)=C1 SONNWYBIRXJNDC-VIFPVBQESA-N 0.000 abstract 1
- 239000003001 serine protease inhibitor Substances 0.000 abstract 1
- 239000002699 waste material Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
- A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
- A61K51/04—Organic compounds
- A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
- A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
-
- 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)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Optics & Photonics (AREA)
- Pharmacology & Pharmacy (AREA)
- Physics & Mathematics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
SE REFIERE A COMPUESTOS DE FORMULA I DONDE: 1) Y1, Y2 SON OH, F, o FORMAN UNA PORCION DERIVADA DE UN COMPUESTO DIHIDROXI; 2) R1 ES -(CH2)2-X, -CH(CH3)-(CH2)2-X, -CH2-CH(CH3)-(CH2)2-X, Y OTROS, DONDE X ES NH2, -NH-C(NH)-NH2, -S-C(NH)-NH2; 3) r, o, p, q SON 0 o 1; m ES 1 o 2; 4) A, A2, A3 SON AMINOACIDOS; 5) W ES UN GRUPO QUELANTE UNIDO AL GRUPO AMINO TERMINAL, QUE PUEDE SER DE FORMULA W`-CH2-Xa-NH, SIENDO W' UN QUELANTE DERIVADO DE ACIDO o ANHIDRIDO POLIAMINO-POLIACETICO NO CICLICO o CICLICO Y Xa ES FENILENO o ALQUILENO C1-C3; 6) Z ES UN ENLACE DIRECTO O UN SEPARADOR; Y A COMPUESTOS DE FORMULA II, DONDE: 1) Y ES UNA SECUENCIA DE AMINOACIDOS; 2) Q1 Y Q2 SE SELECCIONAN DE OH, COR2, -CONR2R3, -NR2R3, -OR6; DONDE R2, R3, R6 SON ALQUILO C1-C10, ARILO C6-C10, ARALQUILO C6-C10, FENILO SUSTITUIDO o Q1 Y Q2 TOMADOS JUNTOS FORMAN UN RESIDUO DIOL; 3) R4 ES H, ALQUILO C1-C10; 4) R5 ES -Z1-X1, DONDE Z1 ES UN ALQUILO QUE PUEDE ESTAR RAMIFICADO, ARILO o ARALQUILO Y X1 ES NH2, -NH-C(NH)-NH2, -S-C-(NH)-NH2, -N3, ALCOXI Y OTROS; ESTOS COMPUESTOS PUEDEN SER UTILES COMO INHIBIDORES DE PROTEASAS DE SERINA, TAL COMO TROMBINA, O COMO AGENTES DE DIAGNOSTICO, AL PODER UNIRSE EL QUELATO A UN METAL POSIBLE DE DETECTAR, PERMITIENDO LA VISUALIZACION DE TROMBOSIT REFERS TO COMPOUNDS OF FORMULA I WHERE: 1) Y1, Y2 ARE OH, F, or FORM A PORTION DERIVED FROM A DIHYDROXY COMPOUND; 2) R1 IS - (CH2) 2-X, -CH (CH3) - (CH2) 2-X, -CH2-CH (CH3) - (CH2) 2-X, AND OTHERS, WHERE X IS NH2, -NH -C (NH) -NH2, -SC (NH) -NH2; 3) r, o, p, q ARE 0 or 1; m IS 1 or 2; 4) A, A2, A3 ARE AMINO ACIDS; 5) W IS A CHELANT GROUP JOINED TO THE TERMINAL AMINO GROUP, WHICH MAY BE OF THE FORMULA W`-CH2-Xa-NH, W IS A CHELANT DERIVED FROM A POLYAMINE-POLYACETIC ACID OR NON-CYCLICAL OR ANKYLENE AND Xa IS PHENYLENE OR ALKYLENE C1-C3; 6) Z IS A DIRECT LINK OR A SPACER; AND TO COMPOUNDS OF FORMULA II, WHERE: 1) AND IT IS A SEQUENCE OF AMINO ACIDS; 2) Q1 AND Q2 ARE SELECTED FROM OH, COR2, -CONR2R3, -NR2R3, -OR6; WHERE R2, R3, R6 ARE ALKYL C1-C10, ARYL C6-C10, ARALKYL C6-C10, SUBSTITUTED PHENYL or Q1 AND Q2 TAKEN TOGETHER FORM A DIOL WASTE; 3) R4 IS H, C1-C10 ALKYL; 4) R5 IS -Z1-X1, WHERE Z1 IS AN ALKYL THAT MAY BE BRANCHED, ARYL or ARALKYL AND X1 IS NH2, -NH-C (NH) -NH2, -SC- (NH) -NH2, -N3, ALCOXI AND OTHERS; THESE COMPOUNDS MAY BE USEFUL AS SERINE PROTEASE INHIBITORS, SUCH AS THROMBINE, OR AS DIAGNOSTIC AGENTS, BY BEING ABLE TO JOIN THE CHELATE TO A METAL POSSIBLE TO DETECT, ALLOWING THE DISPLAY OF THROMBS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9401483A GB9401483D0 (en) | 1994-01-26 | 1994-01-26 | Organic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE45295A1 true PE45295A1 (en) | 1995-12-29 |
Family
ID=10749357
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1995260194A PE45295A1 (en) | 1994-01-26 | 1995-01-24 | PROTEASE INHIBITING PEPTIDES |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP0741747A1 (en) |
| JP (1) | JPH09509653A (en) |
| AU (1) | AU1576495A (en) |
| CA (1) | CA2179889A1 (en) |
| GB (1) | GB9401483D0 (en) |
| IL (1) | IL112423A0 (en) |
| PE (1) | PE45295A1 (en) |
| SG (1) | SG47079A1 (en) |
| WO (1) | WO1995020603A1 (en) |
| ZA (1) | ZA95636B (en) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9515489D0 (en) * | 1995-07-28 | 1995-09-27 | Sandoz Ltd | Organic compounds |
| DE10046514A1 (en) | 2000-09-15 | 2002-04-25 | Diagnostikforschung Inst | Process for imaging and diagnosis of thrombi using magnetic resonance imaging using particulate contrast media |
| AU2003263343A1 (en) | 2002-09-09 | 2004-03-29 | Trigen Limited | Boronic acid salts ant their use in the treatment of thromobis |
| US7576206B2 (en) | 2003-08-14 | 2009-08-18 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| US7223745B2 (en) | 2003-08-14 | 2007-05-29 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| US7468383B2 (en) | 2005-02-11 | 2008-12-23 | Cephalon, Inc. | Proteasome inhibitors and methods of using the same |
| WO2011087822A1 (en) | 2009-12-22 | 2011-07-21 | Cephalon, Inc. | Proteasome inhibitors and processes for their preparation, purification and use |
| WO2017222914A1 (en) | 2016-06-21 | 2017-12-28 | Inception 4, Inc. | Carbocyclic prolinamide derivatives |
| EP4257191A3 (en) | 2016-06-21 | 2023-11-22 | Orion Ophthalmology LLC | Heterocyclic prolinamide derivatives |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4668503A (en) * | 1982-07-26 | 1987-05-26 | Trustees Of University Of Massachusetts | Process for labeling amines with 99m Tc |
| US5187157A (en) * | 1987-06-05 | 1993-02-16 | Du Pont Merck Pharmaceutical Company | Peptide boronic acid inhibitors of trypsin-like proteases |
| EP0403243B1 (en) * | 1989-06-16 | 1995-11-08 | Merck Frosst Canada Inc. | Chelate derivatives of atrial natriuretic factor (ANF) |
| GB9017694D0 (en) * | 1990-08-13 | 1990-09-26 | Sandoz Ltd | Improvements in or relating to organic chemistry |
| US5252721A (en) * | 1990-09-28 | 1993-10-12 | Neorx Corporation | S3 N chelating compounds |
| ATE186550T1 (en) * | 1991-04-22 | 1999-11-15 | Mallinckrodt Medical Inc | COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR DETECTING AND LOCALIZING TISSUES HAVING NEUROKININ-1 RECEPTORS |
-
1994
- 1994-01-26 GB GB9401483A patent/GB9401483D0/en active Pending
-
1995
- 1995-01-24 PE PE1995260194A patent/PE45295A1/en not_active Application Discontinuation
- 1995-01-24 IL IL11242395A patent/IL112423A0/en unknown
- 1995-01-25 AU AU15764/95A patent/AU1576495A/en not_active Abandoned
- 1995-01-25 JP JP7519884A patent/JPH09509653A/en active Pending
- 1995-01-25 EP EP95907611A patent/EP0741747A1/en not_active Ceased
- 1995-01-25 SG SG1996005775A patent/SG47079A1/en unknown
- 1995-01-25 CA CA002179889A patent/CA2179889A1/en not_active Abandoned
- 1995-01-25 WO PCT/EP1995/000269 patent/WO1995020603A1/en not_active Ceased
- 1995-01-26 ZA ZA95636A patent/ZA95636B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ZA95636B (en) | 1996-07-26 |
| SG47079A1 (en) | 1998-03-20 |
| JPH09509653A (en) | 1997-09-30 |
| GB9401483D0 (en) | 1994-03-23 |
| WO1995020603A1 (en) | 1995-08-03 |
| AU1576495A (en) | 1995-08-15 |
| CA2179889A1 (en) | 1995-08-03 |
| IL112423A0 (en) | 1995-03-30 |
| EP0741747A1 (en) | 1996-11-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |