ES2260428T3 - Diamidas que inhiben la actividad de la triptasa y del factor xa. - Google Patents
Diamidas que inhiben la actividad de la triptasa y del factor xa.Info
- Publication number
- ES2260428T3 ES2260428T3 ES02724182T ES02724182T ES2260428T3 ES 2260428 T3 ES2260428 T3 ES 2260428T3 ES 02724182 T ES02724182 T ES 02724182T ES 02724182 T ES02724182 T ES 02724182T ES 2260428 T3 ES2260428 T3 ES 2260428T3
- Authority
- ES
- Spain
- Prior art keywords
- group
- aryl
- aralkyl
- heteroaryl
- heterocycloalkyl
- 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
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- 125000003118 aryl group Chemical group 0.000 claims abstract description 37
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- 125000000217 alkyl group Chemical group 0.000 claims abstract description 35
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract description 35
- 125000004404 heteroalkyl group Chemical group 0.000 claims abstract description 31
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 30
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims abstract description 29
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims abstract description 23
- 239000000203 mixture Substances 0.000 claims abstract description 23
- 150000003839 salts Chemical class 0.000 claims abstract description 18
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- 125000002102 aryl alkyloxo group Chemical group 0.000 claims abstract description 10
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- 238000009472 formulation Methods 0.000 claims abstract description 8
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- 239000012453 solvate Substances 0.000 claims abstract description 7
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- 125000001424 substituent group Chemical group 0.000 claims abstract description 4
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- 239000003054 catalyst Substances 0.000 description 4
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
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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
- 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
- 108010022999 Serine Proteases Proteins 0.000 description 3
- 102000012479 Serine Proteases Human genes 0.000 description 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 3
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- 102000001400 Tryptase Human genes 0.000 description 3
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- 239000002585 base Substances 0.000 description 3
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 description 3
- 125000004093 cyano group Chemical group *C#N 0.000 description 3
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- 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
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 description 3
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- 229910052698 phosphorus Inorganic materials 0.000 description 3
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Classifications
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- 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
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- 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 (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01103662 | 2001-02-23 | ||
| EP01103662 | 2001-02-23 | ||
| EP01116782 | 2001-07-20 | ||
| EP01116782 | 2001-07-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2260428T3 true ES2260428T3 (es) | 2006-11-01 |
Family
ID=26076479
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES02724182T Expired - Lifetime ES2260428T3 (es) | 2001-02-23 | 2002-02-22 | Diamidas que inhiben la actividad de la triptasa y del factor xa. |
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 |
| AU2002254907A1 (en) | 2002-09-12 |
| DE60211665T2 (de) | 2006-09-28 |
| 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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