AR013084A1 - Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados - Google Patents

Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados

Info

Publication number
AR013084A1
AR013084A1 ARP980102696A ARP980102696A AR013084A1 AR 013084 A1 AR013084 A1 AR 013084A1 AR P980102696 A ARP980102696 A AR P980102696A AR P980102696 A ARP980102696 A AR P980102696A AR 013084 A1 AR013084 A1 AR 013084A1
Authority
AR
Argentina
Prior art keywords
alkyl
preparation
compounds
independently
alkylene
Prior art date
Application number
ARP980102696A
Other languages
English (en)
Original Assignee
Astrazeneca Ab
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
Priority claimed from SE9702378A external-priority patent/SE9702378D0/xx
Priority claimed from SE9801099A external-priority patent/SE9801099D0/xx
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR013084A1 publication Critical patent/AR013084A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyrrole Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Un compuesto caracterizado porque comprende la formula (I), en la cual: R1 representa H, C1-4 alquilo (opcionalmente sustituido por uno o mássustituyentes seleccionados entre los siguientes: ciano, halo, OH, C(O)OR1a o C(O)N(R1b)(R1c) u OR1d; R1d representa H, C(O)R11, SiR12R13R14 o C1-6 alquilo,el ultimo grupo es opcionalmente sustituido por uno o más sustituyentes seleccionados entre los siguientes: OR15 o (CH2)qR16; R12, R13 y R14,independientemente el uno del otro, representa H, fenilo o C1-6 alquilo, R16 representa C1-4 alquilo, fenilo, OH, C(O)R17 o C(O)N(H)R18; R18 representaH, C1-4 alquilo o CH2C(O)OR19; R15 y R16, independientemente el uno del otro, representan H, C1-6 alquilo o C1-3 alquilfenilo; R1a, R1b, R1c, R11 y R19,independientemente el uno del otro, representan H o C1-4 alquilo; y q es un numero entero que vale, 0, 1 o 2; Rx representa un fragmento estructural de laformula IIa, IIb o IIc; en la cuales: las líneas de puntos, independientemente el uno del otro, representan dobles enlaces opcionales; A y B,independientemente el uno del otro, representan O o S, CH o CH2 (de acuerdo con necesidad), o N o N(R21) (de acuerdo con necesidad); D representa -CH2-,O, S, N(R22), -(CH2)2-, -CH=CH-, -CH2N(R22)-, -N(R22)CH2-, -CH=N-, -N=CH-, -CH2O-, -OCH2-, -CH2S- o -SCH2; X1 representa C2-4 alquileno, C2-3 alquilenointerrumpido por Z, -C(O)-Z-A1, -Z-C(O)-A1, -CH2-C(O)-A1, -Z-C(O)-Z-A2, -CH2-Z-C(O)-A2, -Z-CH2-C(O)-A2-, -Z-CH2-S(O)m-A2-, -CH2-Z-S(O)m-A2-, -C(O)-A3-,-Z-A3- o -A3-Z-; X2 representa C2-3 alquileno, -C(O)-A4- o A4-C(O)-; X3 representa CH o N; X4 representa un unico enlace, O, S, C(O), N(R23), -CH(R23)-, -CH(R23)-CH(R24)- o -C(R23)=C(R24)-; A representa un enlace simple o C1-2 alquileno; A2 representa un enlace simple o -CH2-; A3 representa C1-3
ARP980102696A 1997-06-19 1998-06-05 Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados AR013084A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE9702378A SE9702378D0 (sv) 1997-06-19 1997-06-19 New compounds
SE9801099A SE9801099D0 (sv) 1998-03-30 1998-03-30 New compounds

Publications (1)

Publication Number Publication Date
AR013084A1 true AR013084A1 (es) 2000-12-13

Family

ID=26663014

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980102696A AR013084A1 (es) 1997-06-19 1998-06-05 Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados

Country Status (20)

Country Link
US (2) US6265397B1 (es)
EP (1) EP1012140B1 (es)
JP (2) JP3919236B2 (es)
KR (1) KR100540413B1 (es)
CN (1) CN1205187C (es)
AR (1) AR013084A1 (es)
AT (1) ATE277902T1 (es)
AU (1) AU737645C (es)
BR (1) BR9810177A (es)
CA (1) CA2294059C (es)
DE (1) DE69826693T2 (es)
EE (1) EE9900600A (es)
IL (1) IL133490A0 (es)
IS (1) IS5302A (es)
NO (1) NO315156B1 (es)
NZ (1) NZ501635A (es)
PL (1) PL337645A1 (es)
SK (1) SK167099A3 (es)
TR (1) TR199903134T2 (es)
WO (1) WO1998057932A1 (es)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR013084A1 (es) * 1997-06-19 2000-12-13 Astrazeneca Ab Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados
SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
SE9804313D0 (sv) * 1998-12-14 1998-12-14 Astra Ab New compounds
CN1170842C (zh) 1999-01-13 2004-10-13 阿斯特拉曾尼卡有限公司 新的脒基苄基胺衍生物及其作为凝血酶抑制剂的用途
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
EP1059302A1 (en) * 1999-06-08 2000-12-13 Aventis Pharma Deutschland GmbH Factor VIIa inhibitors
SE0000382D0 (sv) 2000-02-07 2000-02-07 Astrazeneca Ab New process
US6403818B1 (en) 2000-02-28 2002-06-11 Eisai Co., Ltd. Process for producing α-hydroxy-carbonyl compound
SE0001803D0 (sv) * 2000-05-16 2000-05-16 Astrazeneca Ab New compounds i
US6433186B1 (en) 2000-08-16 2002-08-13 Astrazeneca Ab Amidino derivatives and their use as thormbin inhibitors
US7129233B2 (en) * 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
AR035216A1 (es) * 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
CN100350036C (zh) 2001-04-27 2007-11-21 宝洁公司 用于控制生物膜的装置和方法
AR034517A1 (es) * 2001-06-21 2004-02-25 Astrazeneca Ab Formulacion farmaceutica
SE0201659D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab Modified release pharmaceutical formulation
SE0201661D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab New salts
CN101880277A (zh) 2003-04-24 2010-11-10 因塞特公司 作为金属蛋白酶抑制剂的氮杂螺烷衍生物
US7781424B2 (en) * 2003-05-27 2010-08-24 Astrazeneca Ab Modified release pharmaceutical formulation
ES2291951T3 (es) * 2003-11-07 2008-03-01 F. Hoffmann-La Roche Ag Derivados de benzo (b) (1,4) dioxepina.
US7524354B2 (en) * 2005-07-07 2009-04-28 Research Foundation Of State University Of New York Controlled synthesis of highly monodispersed gold nanoparticles
UA95788C2 (en) 2005-12-15 2011-09-12 Ф. Хоффманн-Ля Рош Аг Fused pyrrole derivatives
TW200827336A (en) * 2006-12-06 2008-07-01 Astrazeneca Ab New crystalline forms
US20090061000A1 (en) * 2007-08-31 2009-03-05 Astrazeneca Ab Pharmaceutical formulation use 030
DE102008007440A1 (de) * 2008-02-01 2009-08-13 Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg Aminosäurederivate als Arzneistoffe
KR20110025970A (ko) * 2008-06-23 2011-03-14 아스트라제네카 아베 트롬빈 억제제로서 사용하기 위한 신규 복소환 카복스아미드
CN104327029A (zh) * 2014-09-21 2015-02-04 湖南华腾制药有限公司 一种含氧杂环化合物的制备方法

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU178398B (en) 1979-06-12 1982-04-28 Gyogyszerkutato Intezet Process for producing new agmatine derivatives of activity against haemagglutination
HU192646B (en) 1984-12-21 1987-06-29 Gyogyszerkutato Intezet Process for preparing new n-alkyl-peptide aldehydes
CA1341029C (en) 1985-02-04 2000-06-20 Michael Kolb Peptidase inhibitors
US5187157A (en) 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
EP0362002B1 (en) 1988-09-01 1995-07-26 Merrell Dow Pharmaceuticals Inc. HIV protease inhibitors
ZA897515B (en) 1988-10-07 1990-06-27 Merrell Dow Pharma Novel peptidase inhibitors
TW201303B (es) 1990-07-05 1993-03-01 Hoffmann La Roche
CA2075154A1 (en) 1991-08-06 1993-02-07 Neelakantan Balasubramanian Peptide aldehydes as antithrombotic agents
SE9102462D0 (sv) 1991-08-28 1991-08-28 Astra Ab New isosteric peptides
CZ333492A3 (en) 1991-11-12 1993-09-15 Lilly Co Eli Dipeptide of l-azetidine-2-carboxylic acids and l-argininaldehyde, process of its preparation and pharmaceutical preparation in which said dipeptide is comprised
SE9103612D0 (sv) 1991-12-04 1991-12-04 Astra Ab New peptide derivatives
JPH08501057A (ja) * 1992-03-04 1996-02-06 ヂョヂセルクタトー インテーゼット カーエフテー 新規な抗凝結因子ペプチド誘導体及びそれを含有する製薬学的組成物及びその製造方法
TW223629B (es) 1992-03-06 1994-05-11 Hoffmann La Roche
US5583146A (en) 1992-12-02 1996-12-10 Bristol-Myers Squibb Company Heterocyclic thrombin inhibitors
AU675981B2 (en) 1992-12-02 1997-02-27 Bristol-Myers Squibb Company Guanidinyl-substituted heterocyclic thrombin inhibitors
JPH06340619A (ja) 1993-05-03 1994-12-13 Bristol Myers Squibb Co グアニジニルまたはアミジニル置換メチルアミノ複素環トロンビン抑制剤
SE9301916D0 (sv) 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
US5783563A (en) 1993-06-03 1998-07-21 Astra Aktiebolag Method for treatment or prophylaxis of venous thrombosis
EP0648780A1 (en) 1993-08-26 1995-04-19 Bristol-Myers Squibb Company Heterocyclic thrombin inhibitors
TW394760B (en) 1993-09-07 2000-06-21 Hoffmann La Roche Novel Carboxamides, process for their preparation and pharmaceutical composition containing the same
AU1025795A (en) 1994-01-27 1995-08-03 Mitsubishi Chemical Corporation Prolineamide derivatives
ZA951617B (en) 1994-03-04 1997-02-27 Lilly Co Eli Antithrombotic agents.
US5707966A (en) 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5705487A (en) 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
US5726159A (en) 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
US5561146A (en) 1994-06-10 1996-10-01 Bristol-Myers Squibb Company Modified guanidino and amidino thrombin inhibitors
DE4421052A1 (de) 1994-06-17 1995-12-21 Basf Ag Neue Thrombininhibitoren, ihre Herstellung und Verwendung
US5510369A (en) 1994-07-22 1996-04-23 Merck & Co., Inc. Pyrrolidine thrombin inhibitors
DE4443390A1 (de) 1994-12-06 1996-06-13 Basf Ag Neue dipeptidische p-Amidinobenzylamide mit N-terminalen Sulfonyl- bzw. Aminosulfonylresten
EA002767B1 (ru) 1995-02-10 2002-08-29 Басф Акциенгезельшафт Ингибиторы тромбина
CZ245797A3 (cs) 1995-02-17 1998-06-17 Basf Aktiengesellschaft Derivát amidinu dipeptidu jako inhibitor thrombinu
US5914319A (en) 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
US5710130A (en) 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
AU698911B2 (en) 1995-04-04 1998-11-12 Merck & Co., Inc. Thrombin inhibitors
US5629324A (en) 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
SA96170106A (ar) 1995-07-06 2005-12-03 أسترا أكتيبولاج مشتقات حامض أميني جديدة
TWI238827B (en) 1995-12-21 2005-09-01 Astrazeneca Ab Prodrugs of thrombin inhibitors
AU1990197A (en) 1996-03-12 1997-10-01 Bristol-Myers Squibb Company Carbamyl guanidine and amidine prodrugs
SE9602263D0 (sv) 1996-06-07 1996-06-07 Astra Ab New amino acid derivatives
JPH1095898A (ja) 1996-09-25 1998-04-14 Sumitomo Bakelite Co Ltd 難燃性樹脂組成物およびこれを用いた積層板
SE9602646D0 (sv) 1996-07-04 1996-07-04 Astra Ab Pharmaceutically-useful compounds
DE19632773A1 (de) 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren
DE19632772A1 (de) 1996-08-14 1998-02-19 Basf Ag Neue Benzamidine
AR013084A1 (es) * 1997-06-19 2000-12-13 Astrazeneca Ab Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados

Also Published As

Publication number Publication date
US20020022612A1 (en) 2002-02-21
IL133490A0 (en) 2001-04-30
CA2294059A1 (en) 1998-12-23
AU737645C (en) 2002-03-21
SK167099A3 (en) 2000-06-12
AU7946198A (en) 1999-01-04
JP3919236B2 (ja) 2007-05-23
PL337645A1 (en) 2000-08-28
KR100540413B1 (ko) 2006-01-12
NO996313D0 (no) 1999-12-17
IS5302A (is) 1999-12-15
DE69826693T2 (de) 2006-02-16
TR199903134T2 (xx) 2000-07-21
BR9810177A (pt) 2000-08-08
CA2294059C (en) 2008-12-09
NO315156B1 (no) 2003-07-21
KR20010013982A (ko) 2001-02-26
JP2002503256A (ja) 2002-01-29
CN1205187C (zh) 2005-06-08
NO996313L (no) 2000-02-21
CN1266427A (zh) 2000-09-13
AU737645B2 (en) 2001-08-23
JP2006321807A (ja) 2006-11-30
ATE277902T1 (de) 2004-10-15
EE9900600A (et) 2000-08-15
DE69826693D1 (de) 2004-11-04
US6576657B2 (en) 2003-06-10
WO1998057932A1 (en) 1998-12-23
US6265397B1 (en) 2001-07-24
EP1012140B1 (en) 2004-09-29
EP1012140A1 (en) 2000-06-28
NZ501635A (en) 2001-09-28

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