HUP0104588A2 - Szubsztituált heterociklusos acil-tripeptidek, mint trombin receptor modulátorok, azokat tartalmazó gyógyszerkészítmények, eljárás előállításukra és alkalmazásuk - Google Patents
Szubsztituált heterociklusos acil-tripeptidek, mint trombin receptor modulátorok, azokat tartalmazó gyógyszerkészítmények, eljárás előállításukra és alkalmazásukInfo
- Publication number
- HUP0104588A2 HUP0104588A2 HU0104588A HUP0104588A HUP0104588A2 HU P0104588 A2 HUP0104588 A2 HU P0104588A2 HU 0104588 A HU0104588 A HU 0104588A HU P0104588 A HUP0104588 A HU P0104588A HU P0104588 A2 HUP0104588 A2 HU P0104588A2
- Authority
- HU
- Hungary
- Prior art keywords
- substituted
- heteroaryl
- acid residue
- aryl
- arg
- Prior art date
Links
- 125000000623 heterocyclic group Chemical group 0.000 title abstract 3
- 102000003790 Thrombin receptors Human genes 0.000 title abstract 2
- 108090000166 Thrombin receptors Proteins 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000002253 acid Substances 0.000 abstract 4
- 125000005122 aminoalkylamino group Chemical group 0.000 abstract 4
- 125000003282 alkyl amino group Chemical group 0.000 abstract 2
- 125000001769 aryl amino group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- -1 pyrrolidinyl- Chemical group 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 2
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 229940075993 receptor modulator Drugs 0.000 abstract 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
- 230000029663 wound healing Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
- C07K5/10—Tetrapeptides
- C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
-
- 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)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Crystallography & Structural Chemistry (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
A tal lm ny t rgya (I) ltal nos képletű szubsztitu lt heterociklusosaciltripeptidek, amelyek hasznos trombin receptor modul torok.Alkalmaz suk lehetséges a sebgyógyít sban és a trombocita aggreg ciómegelőzésében. A tal lm ny szerinti szubsztitu lt heterociklusosaciltripeptideket tartalmazó gyógyszerkészítményekre is kiterjed a tallm ny. Az (I) ltal nos képletben a szubsztituensek jelentése ak"vetkező: A1 jelentése alkil-aminosav maradék, előny"sen Cha, Leuvagy Ile, amino-alkil-aminosav maradék, előny"sen Arg vagy Lys, aril-aminosav maradék, előny"sen Phe, szubsztitu lt Phe, Tyr vagy Trp; A2jelentése amino-alkil-aminosav maradék, előny"sen Lys, Orn, Arg vagyhomo Arg; A3 jelentése aril-aminosav maradék, előny"sen Phe,szubsztitu lt Phe, homo Phe, Tyr, Trp, phgly, 2-tala vagy 3-tala, vagyalkil-aminosav maradék, előny"sen Cha, Leu vagy Ile, amido-alkil-aminosav, előny"sen Asn vagy Gln, amino-alkil-aminosav maradék,előny"sen Arg, homo Arg, Orn vagy Lys; X jelentése CO, CS vagy SO2; Yjelentése aril-, szubsztitu lt aril-, heterocikloalkil-, szubsztitu ltheterocikloalkil-, heteroaril-, szubsztitu lt heteroaril-, heteroaril-etilenil-, szubsztitu lt heteroariletilenil-, aril-akril-amido-heteroaril-, szubsztitu lt aril-akrilamido-heteroaril-, heteroaril-akril-amido-heteroaril- vagy szubsztitu lt heteroaril-akril-amido-heteroarilcsoport, azzal a megk"téssel, hogy Y nem pirrolidinil-,fenil- vagy 2-amino-fenilcsoport; Z jelentése NH2, NH-alkil, NH-aralkil vagy amino-alkilaminosav, előny"sen Arg-NH2; és ahol az "sszesaminosav L-konfigur ciójú. Ó
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11231398P | 1998-12-14 | 1998-12-14 | |
| US44432799A | 1999-11-19 | 1999-11-19 | |
| PCT/US1999/027570 WO2000035942A1 (en) | 1998-12-14 | 1999-11-19 | Substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0104588A2 true HUP0104588A2 (hu) | 2002-04-29 |
| HUP0104588A3 HUP0104588A3 (en) | 2002-05-28 |
Family
ID=26809819
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0104588A HUP0104588A3 (en) | 1998-12-14 | 1999-11-19 | Substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators pharmaceutical compositions comprising thereof, method for their preparation and their use |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US6747127B1 (hu) |
| EP (1) | EP1140985A1 (hu) |
| CN (1) | CN1342164A (hu) |
| AU (1) | AU771844B2 (hu) |
| BR (1) | BR9916811A (hu) |
| CA (1) | CA2355818A1 (hu) |
| CZ (1) | CZ20012136A3 (hu) |
| HU (1) | HUP0104588A3 (hu) |
| NO (1) | NO20012939L (hu) |
| PL (1) | PL348504A1 (hu) |
| TR (1) | TR200102502T2 (hu) |
| WO (1) | WO2000035942A1 (hu) |
| YU (1) | YU42401A (hu) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6346510B1 (en) | 1995-10-23 | 2002-02-12 | The Children's Medical Center Corporation | Therapeutic antiangiogenic endostatin compositions |
| US20060159663A1 (en) * | 2004-07-30 | 2006-07-20 | Lu Helen H | Growth factor encapsulation system for enhancing bone formation |
| US20060293231A1 (en) * | 2004-07-30 | 2006-12-28 | Regina Landesberg | Method for enhancing bone formation |
| US8097582B2 (en) | 2006-05-09 | 2012-01-17 | Neobiotics Ab | Peptide derivatives useful as antimicrobial agents and for treating wounds |
| WO2008031534A1 (en) | 2006-09-11 | 2008-03-20 | Syngenta Participations Ag | Insecticidal compounds |
| CN101747410B (zh) * | 2008-11-28 | 2013-03-13 | 北京大学 | 具镇痛活性的氨基酰酪氨酰色氨酸三肽及制备方法和应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL60888A (en) | 1978-06-16 | 1984-07-31 | Yeda Res & Dev | Substrates and process for the quantitative assay of enzymes |
| GB9019558D0 (en) | 1990-09-07 | 1990-10-24 | Szelke Michael | Enzyme inhibitors |
| US5391705A (en) | 1991-03-15 | 1995-02-21 | Merrell Dow Pharmaceuticals Inc. | Polyfluorinated tripeptide thrombin inhibitors |
| EP0503203A1 (en) | 1991-03-15 | 1992-09-16 | Merrell Dow Pharmaceuticals Inc. | Novel thrombin inhibitors |
| HU221974B1 (hu) | 1992-06-04 | 2003-03-28 | Merrell Dow Pharmaceuticals Inc. | Eljárás trombingátló hatású fluortartalmú peptidszármazékok és ezeket tartalmazó gyógyszerkészítmények előállítására |
| US5696231A (en) | 1994-12-21 | 1997-12-09 | Corvas International, Inc. | N-substituted glycine derivatives as enzyme inhibitors |
| US6069232A (en) | 1995-10-02 | 2000-05-30 | Hoechst Marion Roussel, Inc. | Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors |
| US6017890A (en) | 1998-02-19 | 2000-01-25 | Ortho-Mcneil Pharmaceutical, Inc. | Azole peptidomimetics as thrombin receptor antagonists |
| CA2321104A1 (en) * | 1998-02-19 | 1999-08-26 | Ortho-Mcneil Pharmaceutical, Inc. | Azole peptidomimetics as thrombin receptor antagonists |
-
1998
- 1998-12-14 YU YU42401A patent/YU42401A/sh unknown
-
1999
- 1999-11-19 CA CA002355818A patent/CA2355818A1/en not_active Abandoned
- 1999-11-19 TR TR2001/02502T patent/TR200102502T2/xx unknown
- 1999-11-19 HU HU0104588A patent/HUP0104588A3/hu unknown
- 1999-11-19 EP EP99961738A patent/EP1140985A1/en not_active Withdrawn
- 1999-11-19 CZ CZ20012136A patent/CZ20012136A3/cs unknown
- 1999-11-19 CN CN99816184A patent/CN1342164A/zh active Pending
- 1999-11-19 BR BR9916811-1A patent/BR9916811A/pt not_active IP Right Cessation
- 1999-11-19 PL PL99348504A patent/PL348504A1/xx not_active Application Discontinuation
- 1999-11-19 WO PCT/US1999/027570 patent/WO2000035942A1/en not_active Application Discontinuation
- 1999-11-19 AU AU18256/00A patent/AU771844B2/en not_active Ceased
-
2000
- 2000-05-05 US US09/565,715 patent/US6747127B1/en not_active Expired - Lifetime
-
2001
- 2001-06-14 NO NO20012939A patent/NO20012939L/no unknown
-
2003
- 2003-06-26 US US10/606,422 patent/US7312306B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| NO20012939D0 (no) | 2001-06-14 |
| AU771844B2 (en) | 2004-04-01 |
| HUP0104588A3 (en) | 2002-05-28 |
| NO20012939L (no) | 2001-08-09 |
| WO2000035942A1 (en) | 2000-06-22 |
| CZ20012136A3 (cs) | 2002-02-13 |
| US6747127B1 (en) | 2004-06-08 |
| EP1140985A1 (en) | 2001-10-10 |
| BR9916811A (pt) | 2002-01-15 |
| PL348504A1 (en) | 2002-05-20 |
| CA2355818A1 (en) | 2000-06-22 |
| CN1342164A (zh) | 2002-03-27 |
| YU42401A (sh) | 2003-12-31 |
| AU1825600A (en) | 2000-07-03 |
| TR200102502T2 (tr) | 2002-05-21 |
| US20040063903A1 (en) | 2004-04-01 |
| US7312306B2 (en) | 2007-12-25 |
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