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PE20090548A1 - Compuestos aza-biciclohexano como inhibidores de trombina - Google Patents

Compuestos aza-biciclohexano como inhibidores de trombina

Info

Publication number
PE20090548A1
PE20090548A1 PE2008001125A PE2008001125A PE20090548A1 PE 20090548 A1 PE20090548 A1 PE 20090548A1 PE 2008001125 A PE2008001125 A PE 2008001125A PE 2008001125 A PE2008001125 A PE 2008001125A PE 20090548 A1 PE20090548 A1 PE 20090548A1
Authority
PE
Peru
Prior art keywords
aza
bicycle
hexane
halogen
alkyl
Prior art date
Application number
PE2008001125A
Other languages
English (en)
Inventor
Jonas Branalt
Ingemar Nilsson
Magnus Polla
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
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of PE20090548A1 publication Critical patent/PE20090548A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 three or more hetero rings
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

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

Abstract

REFERIDA A UN COMPUESTO DERIVADO DE AZA-BICICLOHEXANO DE FORMULA (I), DONDE EL GRUPO (X) ES UN AZA-BICICLO[3.1.0]HEXANO O AZA-BICICLO[2.1.1]HEXANO; R1 ES UN ANILLO HETEROARILO DE 5 MIEMBROS QUE CONTIENE 2, 3 O 4 HETEROATOMOS SELECCIONADOS ENTRE N, O Y S, DONDE DICHO HETEROARILO ESTA OPCIONALMENTE SUSTITUIDO POR ALQUILO C1-C6, ENTRE OTROS; R2 ES H, HALOGENO, CIANO, ALQUILO C1-C6, ENTRE OTROS; G ES (a), (b) O (c); R3 ES H, ALQUILO C1-C6, ALQUENILO C2-C6, CICLOALQUILO C3-C6, ENTRE OTROS; R4 ES OH O NHR8; R8 ES H O SO2R7; R7 ES ALQUILO C1-C6 OPCIONALMENTE SUSTITUIDO CON OH, HALOGENO, CIANO, ENTRE OTROS; R9 ES HALOGENO, OXO, NH2, ENTRE OTROS; R10 ES HALOGENO, OH, CIANO, ENTRE OTROS; Q ES O, CH2 O S(O)n; W ES C O N; n ES UN ENTERO DE 0 A 2; t ES UN ENTERO DE 0 A 2; u ES 0 O 1. SON COMPUESTOS PREFERIDOS: 5-CLORO-2-TETRAZOL-1-IL-BENCILAMIDA DEL ACIDO (1S,2S,5R)-3-((R)-2-HIDROXI-3,3-DIMETIL-BUTIRIL)-3-AZA-BICICLO[3.1.0]HEXANO-2-CARBOXILICO, 5-CLORO-2-TETRAZOL-1-IL-BENCILAMIDA DEL ACIDO (1S,2S,5R)-3-((R)-2-HIDROXI-2-FENIL-ACETIL)-3-AZA-BICICLO[3.1.0]HEXANO-2-CARBOXILICO, 5-CLORO-2-TETRAZOL-1-IL-BENCILAMIDA DEL ACIDO (1R,2S,5S)-3-((R)-2-HIDROXI-2-FENIL-ACETIL)-3-AZA-BICICLO[3.1.0]HEXANO-2-CARBOXILICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES COMPETITIVOS DE SERINA PROTEASAS DE TIPO TRIPSINA TAL COMO LA TROMBINA Y SON UTILES EN EL TRATAMIENTO DE TROMBOSIS Y TRANSTORNOS RELACIONADOS
PE2008001125A 2007-07-03 2008-07-03 Compuestos aza-biciclohexano como inhibidores de trombina PE20090548A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US94771207P 2007-07-03 2007-07-03

Publications (1)

Publication Number Publication Date
PE20090548A1 true PE20090548A1 (es) 2009-06-04

Family

ID=40002969

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001125A PE20090548A1 (es) 2007-07-03 2008-07-03 Compuestos aza-biciclohexano como inhibidores de trombina

Country Status (5)

Country Link
US (1) US20090012087A1 (es)
PE (1) PE20090548A1 (es)
TW (1) TW200911787A (es)
UY (1) UY31203A1 (es)
WO (1) WO2009004383A2 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110130432A1 (en) 2008-06-23 2011-06-02 Astrazeneca Ab Heterocyclic Carboxamides For Use As Thrombin Inhibitors
US8354444B2 (en) 2008-09-18 2013-01-15 Hoffmann-La Roche Inc. Substituted pyrrolidine-2-carboxamides
WO2010116328A2 (en) * 2009-04-08 2010-10-14 Actelion Pharmaceuticals Ltd 6-(3-aza-bicyclo[3.1.0]hex-3-yl)-2-phenyl-pyrimidines
DE102011078695A1 (de) 2011-07-05 2013-01-10 Charité - Universitätsmedizin Berlin Dialyseverfahren zur Entfernung proteingebundener Toxine aus dem Blut von Patienten unter Einsatz hochfrequenter elektromagnetischer Felder
WO2014025658A1 (en) * 2012-08-08 2014-02-13 Merck Sharp & Dohme Corp. Pyrrolidine thrombin inhibitors
WO2015047973A1 (en) * 2013-09-27 2015-04-02 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
ES2541870B1 (es) 2013-12-27 2016-05-12 Servicio Andaluz De Salud Uso de antagonistas no peptídicos de NK1 en una determinada dosis para el tratamiento del cáncer
WO2020185982A1 (en) * 2019-03-12 2020-09-17 Amgen Inc. Polymorphs and cocrystals of a cardiac troponin activator
US20220185791A1 (en) * 2019-03-12 2022-06-16 Amgen Inc. Polymorphs of a cardiac troponin activator
CN110256297B (zh) * 2019-07-05 2022-07-26 爱斯特（成都）生物制药股份有限公司 一种N-Boc-(R)-2-氨基-4,4-二甲基戊酸的制备方法
CN110343056B (zh) * 2019-07-19 2022-01-07 爱斯特（成都）生物制药股份有限公司 一种n-叔丁氧羰基-n-甲基-2-氨基-4,4-二甲基戊酸的制备方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2793248B1 (fr) * 1999-05-03 2001-06-29 Adir Nouveaux derives de 2,3-methano-aminoacides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6528503B2 (en) * 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
JP2004516286A (ja) * 2000-12-18 2004-06-03 メルク エンド カムパニー インコーポレーテッド ベンジルアミン誘導体およびそれのトロンビン阻害薬としての使用
WO2002064559A2 (en) * 2001-02-09 2002-08-22 Merck & Co., Inc. Thrombin inhibitors
US7030141B2 (en) * 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
DE502004009440D1 (de) * 2003-04-03 2009-06-10 Merck Patent Gmbh Pyrrolidin-1,2-dicarbonsäure-1-(phenylamid)-2-(4-(3-oxo-morpholin-4-yl)-phenylamid) derivate und verwandte verbindungen als inhibitoren des koagulationsfaktors xa zur behandlung von thromboembolischen erkrankungen
DE102004045796A1 (de) * 2004-09-22 2006-03-23 Merck Patent Gmbh Arzneimittel enthaltend Carbonylverbindungen sowie deren Verwendung
WO2006055951A2 (en) * 2004-11-19 2006-05-26 Portola Pharmaceuticals, Inc. Tetrahydroisoquinolines as factor xa inhibitors

Also Published As

Publication number Publication date
WO2009004383A2 (en) 2009-01-08
US20090012087A1 (en) 2009-01-08
WO2009004383A3 (en) 2009-04-23
UY31203A1 (es) 2009-01-30
TW200911787A (en) 2009-03-16

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