AR045720A1 - Derivados de pirrol 2,5 tio y oxo sustituidos como moduladores de receptores hormonales de higado - Google Patents

Derivados de pirrol 2,5 tio y oxo sustituidos como moduladores de receptores hormonales de higado

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Publication number
AR045720A1
AR045720A1 ARP040102418A ARP040102418A AR045720A1 AR 045720 A1 AR045720 A1 AR 045720A1 AR P040102418 A ARP040102418 A AR P040102418A AR P040102418 A ARP040102418 A AR P040102418A AR 045720 A1 AR045720 A1 AR 045720A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
phenyl
group
formula
Prior art date
Application number
ARP040102418A
Other languages
English (en)
Inventor
Patrik Holm
Original Assignee
Astrazeneca Uk 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 Astrazeneca Uk Ltd filed Critical Astrazeneca Uk Ltd
Publication of AR045720A1 publication Critical patent/AR045720A1/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

Landscapes

  • 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

Derivados de Pirrol 2,5 tio y oxo sustituidos como moduladores de receptores hormonales de higado. Tratamiento de estados clínicos que incluyen enfermedades cardiovasculares tales omo aterosclerosis; enfermedades inflamatorias, enfermedad de alzheimer, trastornos lipídicos (dislipidemias) asociados o no con la resistencia a la insulina, diabetes de tipo 2 y otra manifestaciones del síndrome metabólico, métodos para su utilización terapéutica y composiciones farmacéuticas que los contienen. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula 1 donde R1 se selecciona entre fenil (C1-4) alquilo donde el fenilo se sustituye opcionalmente por (C1-4)alcoxicarbonilo o un grupo de fórmula NRaRb donde Ra y Rb independientemente representan H o (C1-4) alquilo o un grupo de fórmulka NRaRb donde Ra y Rb independientemente representa H o (C1-4) alquilo; o un grupo (C1-6) alquilo el cual se sustituye opcionalmente por uno o más de los siguientes : fluoro, (C1-4)alcoxicarbonilo , (C1-3) alquiltio o (C1-3) alcoxi opcionalmente sustituido por uno o más fluoro; R2 es fenilo; R3 se selecciona entre fenilo, indolilo o benzofuranilo cada uno opcionalmente sustituiddo por uno o más de los siguientes: (C1- 3)alcanoilo, (C1-4) alcoxi opcionalmente sustituido por uno o más fluoreo; ( C1-3) alquiltio; o un grupo de fórmula NRaRb donde Ra Rb independientemente representan H, (C1-3)alquilo o (C1-3) alcanoilo o Ra y Rb junto con el átomo de nitrógeno al cual se encuentran unidos representan morfolino; X es O o S; o una sal o solvarto aceptable para uso farmacéutico de los mismos, o un solvato de dicha sal.
ARP040102418A 2003-07-11 2004-07-08 Derivados de pirrol 2,5 tio y oxo sustituidos como moduladores de receptores hormonales de higado AR045720A1 (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
AR045720A1 true AR045720A1 (es) 2005-11-09

Family

ID=27741986

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040102418A AR045720A1 (es) 2003-07-11 2004-07-08 Derivados de pirrol 2,5 tio y oxo sustituidos como moduladores de receptores hormonales de higado

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
CO5640134A2 (es) 2006-05-31
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
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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