TWI289566B - Antithrombotic compound - Google Patents
Antithrombotic compound Download PDFInfo
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- TWI289566B TWI289566B TW089124693A TW89124693A TWI289566B TW I289566 B TWI289566 B TW I289566B TW 089124693 A TW089124693 A TW 089124693A TW 89124693 A TW89124693 A TW 89124693A TW I289566 B TWI289566 B TW I289566B
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 78
- 230000002785 anti-thrombosis Effects 0.000 title abstract description 5
- 239000003146 anticoagulant agent Substances 0.000 title description 8
- 125000006850 spacer group Chemical group 0.000 claims abstract description 14
- 108090000190 Thrombin Proteins 0.000 claims abstract description 11
- 229960004072 thrombin Drugs 0.000 claims abstract description 11
- 150000003839 salts Chemical class 0.000 claims abstract description 8
- QAOWNCQODCNURD-UHFFFAOYSA-L sulfate group Chemical group S(=O)(=O)([O-])[O-] QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims abstract description 4
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- 238000000034 method Methods 0.000 claims description 16
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- 238000007639 printing Methods 0.000 claims description 9
- 230000002079 cooperative effect Effects 0.000 claims description 6
- 208000007536 Thrombosis Diseases 0.000 claims description 3
- 239000002671 adjuvant Substances 0.000 claims description 3
- 150000003573 thiols Chemical group 0.000 claims description 3
- 150000008065 acid anhydrides Chemical class 0.000 claims description 2
- 230000003213 activating effect Effects 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- PCTMTFRHKVHKIS-BMFZQQSSSA-N (1s,3r,4e,6e,8e,10e,12e,14e,16e,18s,19r,20r,21s,25r,27r,30r,31r,33s,35r,37s,38r)-3-[(2r,3s,4s,5s,6r)-4-amino-3,5-dihydroxy-6-methyloxan-2-yl]oxy-19,25,27,30,31,33,35,37-octahydroxy-18,20,21-trimethyl-23-oxo-22,39-dioxabicyclo[33.3.1]nonatriaconta-4,6,8,10 Chemical compound C1C=C2C[C@@H](OS(O)(=O)=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2.O[C@H]1[C@@H](N)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1/C=C/C=C/C=C/C=C/C=C/C=C/C=C/[C@H](C)[C@@H](O)[C@@H](C)[C@H](C)OC(=O)C[C@H](O)C[C@H](O)CC[C@@H](O)[C@H](O)C[C@H](O)C[C@](O)(C[C@H](O)[C@H]2C(O)=O)O[C@H]2C1 PCTMTFRHKVHKIS-BMFZQQSSSA-N 0.000 claims 1
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- 239000012622 synthetic inhibitor Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 125000003396 thiol group Chemical group [H]S* 0.000 description 1
- 229960003766 thrombin (human) Drugs 0.000 description 1
- 230000002537 thrombolytic effect Effects 0.000 description 1
- 201000005060 thrombophlebitis Diseases 0.000 description 1
- 230000001732 thrombotic effect Effects 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 229910021642 ultra pure water Inorganic materials 0.000 description 1
- 239000012498 ultrapure water Substances 0.000 description 1
- JOYRKODLDBILNP-UHFFFAOYSA-N urethane group Chemical group NC(=O)OCC JOYRKODLDBILNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H3/00—Compounds containing only hydrogen atoms and saccharide radicals having only carbon, hydrogen, and oxygen atoms
- C07H3/06—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K9/00—Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof
- C07K9/001—Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof the peptide sequence having less than 12 amino acids and not being part of a ring structure
-
- 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)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP99204172 | 1999-12-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TWI289566B true TWI289566B (en) | 2007-11-11 |
Family
ID=8240976
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW089124693A TWI289566B (en) | 1999-12-07 | 2000-11-21 | Antithrombotic compound |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US6875755B2 (enExample) |
| EP (1) | EP1237897B1 (enExample) |
| JP (1) | JP4820517B2 (enExample) |
| KR (1) | KR100776607B1 (enExample) |
| CN (1) | CN1195767C (enExample) |
| AR (1) | AR026726A1 (enExample) |
| AU (1) | AU781846B2 (enExample) |
| BR (1) | BR0016217A (enExample) |
| CA (1) | CA2393042C (enExample) |
| CO (1) | CO5251449A1 (enExample) |
| CZ (1) | CZ303385B6 (enExample) |
| HK (1) | HK1047593A1 (enExample) |
| HU (1) | HUP0203471A3 (enExample) |
| IL (2) | IL149628A0 (enExample) |
| NO (1) | NO323059B1 (enExample) |
| NZ (1) | NZ519100A (enExample) |
| PE (1) | PE20010935A1 (enExample) |
| PL (1) | PL202840B1 (enExample) |
| RU (1) | RU2266913C2 (enExample) |
| SK (1) | SK287682B6 (enExample) |
| TW (1) | TWI289566B (enExample) |
| WO (1) | WO2001042262A2 (enExample) |
| ZA (1) | ZA200203799B (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2557086A3 (en) * | 2001-09-07 | 2014-11-05 | Alchemia Limited | Synthetic heparin pentasaccharides |
| WO2004007468A1 (en) | 2002-07-15 | 2004-01-22 | Merck & Co., Inc. | Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes |
| WO2004032836A2 (en) | 2002-10-07 | 2004-04-22 | Merck & Co., Inc. | Antidiabetic beta-amino heterocylcic dipeptidyl peptidase inhibitors |
| JP4413863B2 (ja) | 2002-11-07 | 2010-02-10 | メルク エンド カムパニー インコーポレーテッド | 糖尿病の治療又は予防のためのジペチジルペプチダーゼ阻害剤としてのフェニルアラニン誘導体 |
| CA2512546A1 (en) | 2003-01-17 | 2004-08-05 | Merck & Co., Inc. | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| JP2006516573A (ja) | 2003-01-31 | 2006-07-06 | メルク エンド カムパニー インコーポレーテッド | 糖尿病の治療および予防のためのジペプチジルペプチダーゼ阻害薬としての３−アミノ−４−フェニルブタン酸誘導体 |
| WO2004103276A2 (en) | 2003-05-14 | 2004-12-02 | Merck & Co., Inc. | 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| WO2004110436A1 (en) | 2003-06-06 | 2004-12-23 | Merck & Co., Inc. | Fused indoles as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| US7456204B2 (en) | 2003-06-17 | 2008-11-25 | Merck & Co., Inc. | Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| CN1882551A (zh) | 2003-07-31 | 2006-12-20 | 麦克公司 | 用作用于治疗或预防糖尿病的二肽基肽酶－iv酶抑制剂的六氢二氮杂吖庚因酮 |
| EP1574516A1 (en) | 2004-03-05 | 2005-09-14 | Sanofi-Aventis | Antithrombotic compound |
| TW200621794A (en) * | 2004-10-06 | 2006-07-01 | Akzo Nobel Nv | Pulmonary administration of an antithrombotic compound |
| TWI403334B (zh) * | 2004-12-23 | 2013-08-01 | Merck Sharp & Dohme | 包含生物素殘基之抗血栓雙重抑制劑 |
| TWI376234B (en) | 2005-02-01 | 2012-11-11 | Msd Oss Bv | Conjugates of a polypeptide and an oligosaccharide |
| HRP20110331T1 (hr) * | 2005-10-10 | 2011-06-30 | N.V. Organon | Antikoagulantno-antitrombotski dvojni inhibitori, koji sadrže biotinski biljeg |
| CN102892411B (zh) | 2009-12-18 | 2015-01-21 | 恩多提斯药业公司 | 含有合成的低聚糖的药物口服剂型 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4115468A1 (de) * | 1991-05-11 | 1992-11-12 | Behringwerke Ag | Amidinophenylalaninderivate, verfahren zu deren herstellung, deren verwendung und diese enthaltende mittel als antikoagulantien |
| DE4206858A1 (de) * | 1992-03-05 | 1993-09-09 | Behringwerke Ag | Glycopeptid-derivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende pharmazeutische mittel |
| FR2704226B1 (fr) * | 1993-04-22 | 1995-07-21 | Sanofi Elf | 3-desoxy oligosaccharides, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent. |
| ES2147216T3 (es) * | 1993-09-01 | 2000-09-01 | Akzo Nobel Nv | Bisconjugados que comprenden dos sacaridos y un grupo de union. |
| IL126893A (en) * | 1997-11-19 | 2003-05-29 | Akzo Nobel Nv | Sulfated pentasaccharide derivatives and pharmaceutical compositions containing them |
| NZ508623A (en) * | 1998-06-17 | 2002-11-26 | Akzo Nobel Nv | Antithrombotic peptide compounds with saccharide radicals |
-
2000
- 2000-11-21 TW TW089124693A patent/TWI289566B/zh not_active IP Right Cessation
- 2000-12-01 NZ NZ519100A patent/NZ519100A/en not_active IP Right Cessation
- 2000-12-01 HU HU0203471A patent/HUP0203471A3/hu unknown
- 2000-12-01 US US10/148,868 patent/US6875755B2/en not_active Expired - Lifetime
- 2000-12-01 PL PL355484A patent/PL202840B1/pl not_active IP Right Cessation
- 2000-12-01 AU AU20038/01A patent/AU781846B2/en not_active Expired
- 2000-12-01 CA CA2393042A patent/CA2393042C/en not_active Expired - Lifetime
- 2000-12-01 JP JP2001543559A patent/JP4820517B2/ja not_active Expired - Lifetime
- 2000-12-01 KR KR1020027007186A patent/KR100776607B1/ko not_active Expired - Fee Related
- 2000-12-01 WO PCT/EP2000/012155 patent/WO2001042262A2/en not_active Ceased
- 2000-12-01 RU RU2002118117/04A patent/RU2266913C2/ru not_active IP Right Cessation
- 2000-12-01 BR BR0016217-5A patent/BR0016217A/pt active Search and Examination
- 2000-12-01 CN CNB008167753A patent/CN1195767C/zh not_active Expired - Fee Related
- 2000-12-01 EP EP00983209.8A patent/EP1237897B1/en not_active Expired - Lifetime
- 2000-12-01 HK HK02109170.1A patent/HK1047593A1/zh unknown
- 2000-12-01 IL IL14962800A patent/IL149628A0/xx unknown
- 2000-12-01 CZ CZ20021958A patent/CZ303385B6/cs not_active IP Right Cessation
- 2000-12-01 SK SK794-2002A patent/SK287682B6/sk not_active IP Right Cessation
- 2000-12-06 AR ARP000106443A patent/AR026726A1/es active IP Right Grant
- 2000-12-06 CO CO00093231A patent/CO5251449A1/es not_active Application Discontinuation
- 2000-12-06 PE PE2000001308A patent/PE20010935A1/es not_active Application Discontinuation
-
2002
- 2002-05-13 ZA ZA200203799A patent/ZA200203799B/xx unknown
- 2002-05-14 IL IL149628A patent/IL149628A/en not_active IP Right Cessation
- 2002-06-06 NO NO20022689A patent/NO323059B1/no not_active IP Right Cessation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Annulment or lapse of patent due to non-payment of fees |