DE60211665T2 - Diamide, die tryptase und faktor-xa-aktivität hemmen - Google Patents
Diamide, die tryptase und faktor-xa-aktivität hemmen Download PDFInfo
- Publication number
- DE60211665T2 DE60211665T2 DE60211665T DE60211665T DE60211665T2 DE 60211665 T2 DE60211665 T2 DE 60211665T2 DE 60211665 T DE60211665 T DE 60211665T DE 60211665 T DE60211665 T DE 60211665T DE 60211665 T2 DE60211665 T2 DE 60211665T2
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- Germany
- Prior art keywords
- group
- aryl
- alkyl
- aralkyl
- heterocycloalkyl
- Prior art date
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- Expired - Lifetime
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- 125000004432 carbon atom Chemical group C* 0.000 claims description 40
- 125000003118 aryl group Chemical group 0.000 claims description 27
- 125000000217 alkyl group Chemical group 0.000 claims description 26
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 24
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 21
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- 125000002102 aryl alkyloxo group Chemical group 0.000 claims description 8
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- QKNYBSVHEMOAJP-UHFFFAOYSA-N 2-amino-2-(hydroxymethyl)propane-1,3-diol;hydron;chloride Chemical compound Cl.OCC(N)(CO)CO QKNYBSVHEMOAJP-UHFFFAOYSA-N 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical compound ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 3
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 3
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- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 239000008103 glucose Substances 0.000 description 3
- 150000004677 hydrates Chemical class 0.000 description 3
- NPZTUJOABDZTLV-UHFFFAOYSA-N hydroxybenzotriazole Substances O=C1C=CC=C2NNN=C12 NPZTUJOABDZTLV-UHFFFAOYSA-N 0.000 description 3
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- 239000003765 sweetening agent Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 230000002537 thrombolytic effect Effects 0.000 description 1
- 125000003944 tolyl group Chemical group 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 108010036927 trypsin-like serine protease Proteins 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 125000005023 xylyl group Chemical group 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- 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
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
- C07D209/16—Tryptamines
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Compounds Of Unknown Constitution (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01103662 | 2001-02-23 | ||
| EP01103662 | 2001-02-23 | ||
| EP01116782 | 2001-07-20 | ||
| EP01116782 | 2001-07-20 | ||
| PCT/EP2002/001934 WO2002068390A1 (en) | 2001-02-23 | 2002-02-22 | Diamides which inhibit tryptase and factor xa activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60211665D1 DE60211665D1 (de) | 2006-06-29 |
| DE60211665T2 true DE60211665T2 (de) | 2006-09-28 |
Family
ID=26076479
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60211665T Expired - Lifetime DE60211665T2 (de) | 2001-02-23 | 2002-02-22 | Diamide, die tryptase und faktor-xa-aktivität hemmen |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US7256194B2 (enExample) |
| EP (1) | EP1370526B1 (enExample) |
| JP (1) | JP2004523560A (enExample) |
| AT (1) | ATE327221T1 (enExample) |
| AU (1) | AU2002254907A1 (enExample) |
| CA (1) | CA2437114A1 (enExample) |
| CY (1) | CY1105506T1 (enExample) |
| DE (1) | DE60211665T2 (enExample) |
| DK (1) | DK1370526T3 (enExample) |
| ES (1) | ES2260428T3 (enExample) |
| PT (1) | PT1370526E (enExample) |
| WO (1) | WO2002068390A1 (enExample) |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0893437A4 (en) * | 1996-04-10 | 2000-12-27 | Ono Pharmaceutical Co | GUANIDINO TRYPTASE INHIBITOR |
| DK0921116T3 (da) * | 1997-12-04 | 2003-10-06 | Hoffmann La Roche | N-(4-carbamimido-phenyl)-glycinamidderivater |
| DE19939910A1 (de) * | 1999-08-23 | 2001-03-01 | Morphochem Ag | Neue Verbindungen, die Tryptase-Aktivität hemmen |
| DE10041402A1 (de) * | 2000-08-23 | 2002-03-14 | Morphochem Ag | Neue Verbindungen, die Faktor Xa-Aktivität inhibieren |
-
2002
- 2002-02-22 AT AT02724182T patent/ATE327221T1/de not_active IP Right Cessation
- 2002-02-22 ES ES02724182T patent/ES2260428T3/es not_active Expired - Lifetime
- 2002-02-22 US US10/468,975 patent/US7256194B2/en not_active Expired - Fee Related
- 2002-02-22 DE DE60211665T patent/DE60211665T2/de not_active Expired - Lifetime
- 2002-02-22 WO PCT/EP2002/001934 patent/WO2002068390A1/en not_active Ceased
- 2002-02-22 CA CA002437114A patent/CA2437114A1/en not_active Abandoned
- 2002-02-22 EP EP02724182A patent/EP1370526B1/en not_active Expired - Lifetime
- 2002-02-22 PT PT02724182T patent/PT1370526E/pt unknown
- 2002-02-22 AU AU2002254907A patent/AU2002254907A1/en not_active Abandoned
- 2002-02-22 DK DK02724182T patent/DK1370526T3/da active
- 2002-02-22 JP JP2002567904A patent/JP2004523560A/ja active Pending
-
2006
- 2006-07-03 CY CY20061100900T patent/CY1105506T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ATE327221T1 (de) | 2006-06-15 |
| EP1370526A1 (en) | 2003-12-17 |
| US7256194B2 (en) | 2007-08-14 |
| EP1370526B1 (en) | 2006-05-24 |
| US20040082547A1 (en) | 2004-04-29 |
| CY1105506T1 (el) | 2010-04-28 |
| ES2260428T3 (es) | 2006-11-01 |
| AU2002254907A1 (en) | 2002-09-12 |
| JP2004523560A (ja) | 2004-08-05 |
| DK1370526T3 (da) | 2006-07-31 |
| DE60211665D1 (de) | 2006-06-29 |
| WO2002068390A1 (en) | 2002-09-06 |
| CA2437114A1 (en) | 2002-09-06 |
| WO2002068390A8 (en) | 2002-10-31 |
| PT1370526E (pt) | 2006-08-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition | ||
| 8330 | Complete renunciation |