AR039757A1 - THROMBIN INHIBITING THIOPHEN DERIVATIVES - Google Patents

THROMBIN INHIBITING THIOPHEN DERIVATIVES

Info

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
Application number
ARP030102305A
Other languages
Spanish (es)
Inventor
Suk Kyoon Yoon
Bong-Chan Kim
Sung-Ji Kim
Sangyeul Hwang
Hee Dong Park
Sun Hwa Lee
Ae Ri Kim
Ho Jun Kim
Su-Kyung Park
Koo Lee
Kunhye Nam
Original Assignee
Lg Life Sciences Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Lg Life Sciences Ltd filed Critical Lg Life Sciences Ltd
Publication of AR039757A1 publication Critical patent/AR039757A1/en

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
    • 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
    • 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.

ARP030102305A 2002-06-27 2003-06-26 THROMBIN INHIBITING THIOPHEN DERIVATIVES AR039757A1 (en)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

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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