AR039757A1 - THROMBIN INHIBITING THIOPHEN DERIVATIVES - Google Patents
THROMBIN INHIBITING THIOPHEN DERIVATIVESInfo
- Publication number
- AR039757A1 AR039757A1 ARP030102305A ARP030102305A AR039757A1 AR 039757 A1 AR039757 A1 AR 039757A1 AR P030102305 A ARP030102305 A AR P030102305A AR P030102305 A ARP030102305 A AR P030102305A AR 039757 A1 AR039757 A1 AR 039757A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- hydrogen
- nhr2
- heteroaryl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07K5/022—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
- C07K5/0222—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2 with the first amino acid being heterocyclic, e.g. Pro, Trp
-
- 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
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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- 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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Compuesto inhibidor de trombina que tiene un buen efecto inhibidor contra la trombosis y puede ser administrado oralmente, un procedimiento para preparar el mismo, y una composición para el tratamiento terapéutico y/o profiláctico de varias enfermedades asociadas con el mecanismo de inhibición de trombina, que comprende el mismo como un ingrediente activo. Reivindicación 1: Un compuesto representado por la fórmula (1), un isómero, un solvato, un hidrato o una sal farmacéuticamente aceptable del mismo, caracterizado porque: A representa -CH2CO2R1, en donde R1 representa hidrógeno, alquilo C1-6, cicloalquilo C3-7, alquilo C5-10-ar-C1-6, o arilo C5-10; B representa H, OH, R2, OR2, OC(O)R2, OC(O)NHR2, OC(O)OR2, C(O)OR2, C(O)R2, C(O)NHR2, C(O)NR22, OP(O)(OR3)2 o C(O)O(CHR4)mOC(O)R5; en donde: R1 y B no son hidrógeno al mismo tiempo; R2 y R5 independientemente uno de otro representan nitro, o representan alquilo C1-6 no sustituido o mono- a poli-sustituido por sustituyentes seleccionados entre un grupo que consiste en halógeno, hidroxi y alcoxi C1-6, o representa (CH2)n-cicloalquilo C3-7, (CH2)n-heteroarilo, (CH2)n-heterociclo (n = 0, 1, 2, 3) (en donde heteroarilo o heterociclo significa un anillo de 5 ó 6 miembros que tiene uno o dos heteroátomos seleccionados entre un grupo que consiste en nitrógeno, oxígeno y azufre) o representa fenilo no sustituido o mono- a poli-sustituido por sustituyentes seleccionados entre un grupo que consiste en halógeno, hidroxi y alcoxi C1-6, o representa alquilo C5-10-ar-C1-6, arilo C5-10 o alquilo C1-6-N(R4)2; m denota un número entero de 1, 2, 3 ó 4; R3 representa hidrógeno o alquilo C1-6; y R4 representa hidrógeno o alquilo C1-3.Thrombin inhibitor compound that has a good inhibitory effect against thrombosis and can be administered orally, a procedure for preparing it, and a composition for the therapeutic and / or prophylactic treatment of various diseases associated with the thrombin inhibition mechanism, which It comprises the same as an active ingredient. Claim 1: A compound represented by the formula (1), an isomer, a solvate, a hydrate or a pharmaceutically acceptable salt thereof, characterized in that: A represents -CH2CO2R1, wherein R1 represents hydrogen, C1-6 alkyl, C3 cycloalkyl -7, C5-10-ar-C1-6 alkyl, or C5-10 aryl; B represents H, OH, R2, OR2, OC (O) R2, OC (O) NHR2, OC (O) OR2, C (O) OR2, C (O) R2, C (O) NHR2, C (O) NR22, OP (O) (OR3) 2 or C (O) O (CHR4) mOC (O) R5; where: R1 and B are not hydrogen at the same time; R2 and R5 independently of each other represent nitro, or represent unsubstituted C1-6 alkyl or mono- to poly-substituted by substituents selected from a group consisting of halogen, hydroxy and C1-6 alkoxy, or represents (CH2) n- C3-7 cycloalkyl, (CH2) n-heteroaryl, (CH2) n-heterocycle (n = 0, 1, 2, 3) (where heteroaryl or heterocycle means a 5 or 6 membered ring having one or two heteroatoms selected between a group consisting of nitrogen, oxygen and sulfur) or represents unsubstituted phenyl or mono- to poly-substituted by substituents selected from a group consisting of halogen, hydroxy and C1-6 alkoxy, or represents C5-10-ar alkyl -C1-6, C5-10 aryl or C1-6-N (R4) 2 alkyl; m denotes an integer of 1, 2, 3 or 4; R3 represents hydrogen or C1-6 alkyl; and R4 represents hydrogen or C1-3 alkyl.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR20020036219 | 2002-06-27 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR039757A1 true AR039757A1 (en) | 2005-03-09 |
Family
ID=29997390
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030102305A AR039757A1 (en) | 2002-06-27 | 2003-06-26 | THROMBIN INHIBITING THIOPHEN DERIVATIVES |
Country Status (5)
Country | Link |
---|---|
KR (1) | KR20040002699A (en) |
AR (1) | AR039757A1 (en) |
AU (1) | AU2003245060A1 (en) |
TW (1) | TW200400187A (en) |
WO (1) | WO2004002985A1 (en) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10294189B2 (en) * | 2016-09-20 | 2019-05-21 | Uchicago Argonne, Llc | Process for producing fluorinated electrolyte solvent |
EP3532057B1 (en) | 2016-10-31 | 2022-12-21 | Biocryst Pharmaceuticals, Inc. | Prodrugs of kallikrein inhibitors |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1999037611A1 (en) * | 1998-01-26 | 1999-07-29 | Basf Aktiengesellschaft | Heterocyclic amidines as callicrein protease inhibitors |
KR20000047461A (en) * | 1998-12-29 | 2000-07-25 | 성재갑 | Thrombin inhibitors |
AU765244B2 (en) * | 1999-04-09 | 2003-09-11 | Abbott Gmbh & Co. Kg | Prodrugs of thrombin inhibitors |
DE10064797A1 (en) * | 2000-12-22 | 2002-06-27 | Knoll Ag | Combination pack useful for the treatment of e.g. deep vein thrombosis and post-operative thrombosis, containing oral and parenteral formulations of thrombin inhibitor prodrugs |
-
2003
- 2003-06-13 WO PCT/KR2003/001166 patent/WO2004002985A1/en not_active Application Discontinuation
- 2003-06-13 AU AU2003245060A patent/AU2003245060A1/en not_active Abandoned
- 2003-06-25 TW TW092117213A patent/TW200400187A/en unknown
- 2003-06-25 KR KR1020030041527A patent/KR20040002699A/en not_active Application Discontinuation
- 2003-06-26 AR ARP030102305A patent/AR039757A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
AU2003245060A1 (en) | 2004-01-19 |
TW200400187A (en) | 2004-01-01 |
WO2004002985A1 (en) | 2004-01-08 |
KR20040002699A (en) | 2004-01-07 |
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