CO5640134A2 - Derivados de pirrol-2,5-ditiona como moduladores de receptor hepatico x - Google Patents

Derivados de pirrol-2,5-ditiona como moduladores de receptor hepatico x

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Publication number
CO5640134A2
CO5640134A2 CO06005238A CO06005238A CO5640134A2 CO 5640134 A2 CO5640134 A2 CO 5640134A2 CO 06005238 A CO06005238 A CO 06005238A CO 06005238 A CO06005238 A CO 06005238A CO 5640134 A2 CO5640134 A2 CO 5640134A2
Authority
CO
Colombia
Prior art keywords
alkyl
phenyl
optionally substituted
group
pyridylmethyl
Prior art date
Application number
CO06005238A
Other languages
English (en)
Inventor
Patrick Holm
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 CO5640134A2 publication Critical patent/CO5640134A2/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/44Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

1.- Un compuesto de fórmula I en donde:R1 se selecciona de fenil(1-4C)alquilo en donde el fenilo se sustituye en forma opcional por (1-4C)alcoxicarbonilo o un grupo de fórmula NRaRb en la cual Ra y Rb representan independientemente H ó (1-4C)alquilo;heteroaril(1-4C)alquilo en donde el heteroarilo se sustituye en forma opcional por (1-4C)alquilo o un grupo de fórmula NRaRb en la cual Ra y Rb representan independientemente H ó (1-4C)alquilo; o un grupo (1-6C)alquilo, el cual se sustituye en forma opcional por uno o más de los siguientes: fluoro, (1-4C)alcoxicarbonilo, (1-3C)alquiltio ó (1-3C)alcoxi sustituido en forma opcional por uno o más fluoro;R2 es fenilo;R3 se selecciona de fenilo, indol ilo o benzofuranilo cada uno sustituido en forma opcional por uno o más de los siguientes: (1-3C)alcanoilo, (1-4C)alcoxi sustituido en forma opcional por uno o más fluoro; (1-3C)alquiltio; o un grupo de fórmula NRaRb, en la cual Ra y Rb representan independientemente H, (1-3C)alquilo o (1-3C)alcanoilo o Ra y Rb junto con el átomo de nitrógeno al cual se unen, representan morfolino;X es O ó S, o su sal farmacéuticamente aceptable, o su solvato, o un solvato de tal sal.2.- Un compuesto de acuerdo con la reivindicación 1 en donde X es O.3.- Un compuesto de acuerdo con la reivindicación 1 en donde X es S.4.- Un compuesto de acuerdo con cualquier reivindicación precedente en la cual R1 se selecciona de metilo, etilo, propilo, butilo, 2-metoxietilo, 2,2,2-trifluoroetilo, bencilo, 4-piridilmetilo, 3-piridilmetilo ó 6-amino-3-piridilmetilo.
CO06005238A 2003-07-11 2006-01-20 Derivados de pirrol-2,5-ditiona como moduladores de receptor hepatico x CO5640134A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0316237.7A GB0316237D0 (en) 2003-07-11 2003-07-11 Therapeutic agents

Publications (1)

Publication Number Publication Date
CO5640134A2 true CO5640134A2 (es) 2006-05-31

Family

ID=27741986

Family Applications (1)

Application Number Title Priority Date Filing Date
CO06005238A CO5640134A2 (es) 2003-07-11 2006-01-20 Derivados de pirrol-2,5-ditiona como moduladores de receptor hepatico x

Country Status (26)

Country Link
US (1) US20060189663A1 (es)
EP (1) EP1646625B1 (es)
JP (1) JP2007521313A (es)
KR (1) KR20060034284A (es)
CN (1) CN100478340C (es)
AR (1) AR045720A1 (es)
AT (1) ATE399776T1 (es)
AU (1) AU2004256000B2 (es)
BR (1) BRPI0412479A (es)
CA (1) CA2532068A1 (es)
CO (1) CO5640134A2 (es)
DE (1) DE602004014772D1 (es)
ES (1) ES2308205T3 (es)
GB (1) GB0316237D0 (es)
HK (1) HK1088318A1 (es)
IL (1) IL172759A0 (es)
IS (1) IS8291A (es)
MX (1) MXPA06000447A (es)
NO (1) NO20060080L (es)
RU (1) RU2006102129A (es)
SA (1) SA04250203B1 (es)
TW (1) TW200507836A (es)
UA (1) UA82108C2 (es)
UY (1) UY28407A1 (es)
WO (1) WO2005005416A1 (es)
ZA (1) ZA200600229B (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2592771A1 (en) 2005-01-10 2006-07-13 Astrazeneca Ab Derivatives of isothiazol-3(2h)-one 1,1-dioxides as liver x receptor modulators
SE0500055D0 (sv) 2005-01-10 2005-01-10 Astrazeneca Ab Therapeutic agents 3
SE0500058D0 (sv) * 2005-01-10 2005-01-10 Astrazeneca Ab Therapeutic agents 5
WO2007002654A2 (en) * 2005-06-28 2007-01-04 Daiichi Sankyo Company, Limited. Lxr ligand testing method
ES2528797T3 (es) 2006-08-21 2015-02-12 Genentech, Inc. Compuestos de aza-benzotiofenilo y métodos de uso
US10004703B2 (en) 2006-10-12 2018-06-26 Biogen Chesapeake Llc Treatment of alzheimer's disease using compounds that reduce the activity of non-selective CA++ activated ATP-sensitive cation channels regulated by SUR1 channels
US20100056444A1 (en) 2006-10-12 2010-03-04 Sven Martin Jacobson Treatment of Alzheimer's Disease Using Compounds that Reduce the Activity of Non Selective Ca Activated ATP- Sensitive Cation Channels Regulated by SUR1 Receptors
WO2008103818A1 (en) * 2007-02-21 2008-08-28 University Of Louisville Research Foundation Therapeutic cotinine compositions
PT2868315T (pt) 2007-12-04 2017-09-04 Remedy Pharmaceuticals Inc Formulações melhoradas e métodos para liofilização e liofilizados assim produzidos
WO2009097443A2 (en) * 2008-01-29 2009-08-06 Remedy Pharmaceuticals, Inc. Liquid formulations of compounds active at sulfonylurea receptors
PE20110570A1 (es) 2008-07-01 2011-08-26 Genentech Inc Heterociclos biciclicos sustituidos
US8492427B2 (en) 2008-07-01 2013-07-23 Genentech, Inc. Isoindolones derivatives as MEK kinase inhibitors and methods of use
US20130274212A1 (en) 2010-09-07 2013-10-17 Snu R&Db Foundation Sesterterpene Compounds and Use Thereof
EP3091970B1 (en) 2014-01-10 2020-10-28 Rgenix, Inc. Lxr agonists and uses thereof
JP7025022B2 (ja) 2016-01-11 2022-02-24 ザ ロックフェラー ユニバーシティー 骨髄系由来抑制細胞関連障害の治療のための方法
WO2019104062A1 (en) 2017-11-21 2019-05-31 Rgenix, Inc. Polymorphs and uses thereof
KR200492570Y1 (ko) 2018-12-04 2020-11-05 박규환 조립식 계단장치를 위한 발판
JP2023509845A (ja) 2019-12-13 2023-03-10 インスピルナ,インコーポレーテッド 金属塩及びその使用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2234300T3 (es) * 1998-10-08 2005-06-16 Smithkline Beecham Plc 3-(3-cloro-4-hidroxifenilamino)-4-(2-nitrofenil)-1h-pirrol-2,5-diona como inhibidor de glucogeno cinasa-3 (gsk-3)sintetasa.
CA2377999A1 (en) * 1999-07-08 2001-01-18 Tularik Inc Compositions and methods for raising hdl cholesterol levels

Also Published As

Publication number Publication date
TW200507836A (en) 2005-03-01
ZA200600229B (en) 2007-04-25
UY28407A1 (es) 2005-02-28
NO20060080L (no) 2006-02-08
SA04250203B1 (ar) 2008-02-25
MXPA06000447A (es) 2006-04-07
GB0316237D0 (en) 2003-08-13
BRPI0412479A (pt) 2006-09-19
ES2308205T3 (es) 2008-12-01
EP1646625A1 (en) 2006-04-19
IL172759A0 (en) 2006-04-10
CN1820003A (zh) 2006-08-16
EP1646625B1 (en) 2008-07-02
ATE399776T1 (de) 2008-07-15
RU2006102129A (ru) 2006-08-27
AR045720A1 (es) 2005-11-09
CN100478340C (zh) 2009-04-15
UA82108C2 (uk) 2008-03-11
CA2532068A1 (en) 2005-01-20
DE602004014772D1 (de) 2008-08-14
WO2005005416A1 (en) 2005-01-20
JP2007521313A (ja) 2007-08-02
HK1088318A1 (en) 2006-11-03
US20060189663A1 (en) 2006-08-24
AU2004256000A1 (en) 2005-01-20
KR20060034284A (ko) 2006-04-21
AU2004256000B2 (en) 2007-07-26
IS8291A (is) 2006-02-09

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