AR045721A1 - Derivados de pirrol 2,5 diona como moduladores de receptores hormonales de higado - Google Patents

Derivados de pirrol 2,5 diona como moduladores de receptores hormonales de higado

Info

Publication number
AR045721A1
AR045721A1 ARP040102419A ARP040102419A AR045721A1 AR 045721 A1 AR045721 A1 AR 045721A1 AR P040102419 A ARP040102419 A AR P040102419A AR P040102419 A ARP040102419 A AR P040102419A AR 045721 A1 AR045721 A1 AR 045721A1
Authority
AR
Argentina
Prior art keywords
alkyl
phenyl
optionally substituted
group
fluoro
Prior art date
Application number
ARP040102419A
Other languages
English (en)
Inventor
Jonas Broston
Kay Brickmann
Patrik Holm
Pernilla Marie Sandberg
Marianne Swanson
Christer Westerlund
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 AR045721A1 publication Critical patent/AR045721A1/es

Links

Classifications

    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/44—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/44—Heterocyclic 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
    • C07D207/444—Heterocyclic 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 having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/456—Heterocyclic 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 having two doubly-bound oxygen atoms directly attached in positions 2 and 5 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 other ring carbon atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

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 por (C1-4)alcoxicarbonilo o un grupo de fórmula NRaRb donde Ra y Rb independientemente representan H o ( C1-4)alquilo; hereoaril (C1-4) alquilo donde el heteroarilom opcionalmente se sustituye por (C1-4alquilo o un grupo de fórmula NRaRb donde Ra y Rb independientemente representan H o (C1-4)alquilo; o un grupo (C1-4)alquilo el cual se sustituye por uno o más de los siguientes: Fluoro, (C1-4) alcoxicarbonilo, (C1-3)alquiltio o (C1-3)alcoxi opcionalmetne sustituido por uno o más fluoro; R2 es fenilo, R3 se selecciona entre fenilo, indolilo o benzofuranilo, cada uno opcionalmente sustituido por uno o más de los siguientes: (C1-3) alcanoilo, (C1-3)alcoxi opcionalmente sustituido por uno o más fluoro; (C1-3)alquiltio; o un grupo de fórmula NRaRb donde Ra y Rb independientemente representan H, (C1-3) alquilo o (C1-3)alcanoilo o Ra y Rb junto con el átomo de nitrógneo al cual se encuentran unidos representan morfolino, o una sal o solvato aceptable para uso farmacéutico de los mismos, o un solvato de dicha sal. Procesos para preparar tales compuestos, su utilidad en la modulación de receptores de hormonas nucleares de hígado (LXR) (NR1H3) y/o (NR1H2) y para el tratamiento o prevención de estados clínicos que incluyen enfermedades cardiovasculares tales como aterosclerosis, enfermedades inflamatorias, enfermedad de alzheimer, trastornos lipídicos ( dislipidemias) asociados o no con la resistencia a la insulina. diabetes de tipo 2 y otras manifestaciones del síndrome metabólico, métodos para su utilización terapéutica y composiciones farmacéuticas que los contienen.
ARP040102419A 2003-07-11 2004-07-08 Derivados de pirrol 2,5 diona como moduladores de receptores hormonales de higado AR045721A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0316232.8A GB0316232D0 (en) 2003-07-11 2003-07-11 Therapeutic agents

Publications (1)

Publication Number Publication Date
AR045721A1 true AR045721A1 (es) 2005-11-09

Family

ID=27741983

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040102419A AR045721A1 (es) 2003-07-11 2004-07-08 Derivados de pirrol 2,5 diona como moduladores de receptores hormonales de higado

Country Status (26)

Country Link
US (1) US7432288B2 (es)
EP (1) EP1646626B1 (es)
JP (1) JP2007521312A (es)
KR (1) KR20060035748A (es)
CN (1) CN1823061A (es)
AR (1) AR045721A1 (es)
AT (1) ATE399777T1 (es)
AU (1) AU2004255999B2 (es)
BR (1) BRPI0412472A (es)
CA (1) CA2532056A1 (es)
DE (1) DE602004014773D1 (es)
ES (1) ES2308204T3 (es)
GB (1) GB0316232D0 (es)
HK (1) HK1088320A1 (es)
IL (1) IL172760A0 (es)
IS (1) IS8293A (es)
MX (1) MXPA06000414A (es)
MY (1) MY135821A (es)
NO (1) NO20060081L (es)
RU (1) RU2006102130A (es)
SA (1) SA04250204B1 (es)
TW (1) TW200503691A (es)
UA (1) UA82109C2 (es)
UY (1) UY28408A1 (es)
WO (1) WO2005005417A1 (es)
ZA (1) ZA200600222B (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE513823T1 (de) * 2004-08-17 2011-07-15 Simpson Biotech Co Ltd Mischung und verbindungen von mycelien von antrodia camphorata und deren verwendung
US7505238B2 (en) * 2005-01-07 2009-03-17 Agnes Neves Woo ESD configuration for low parasitic capacitance I/O
SE0500055D0 (sv) 2005-01-10 2005-01-10 Astrazeneca Ab Therapeutic agents 3
WO2006073363A1 (en) 2005-01-10 2006-07-13 Astrazeneca Ab Derivatives of isothiazol-3(2h)-one 1,1-dioxides as liver x receptor modulators
CA2640806A1 (en) * 2006-04-28 2007-11-15 Laboratorios Del Dr. Esteve, S.A. Bicyclic tetrahydropyrrole compounds
KR101475088B1 (ko) 2006-08-21 2014-12-23 제넨테크, 인크. 아자-벤조티오페닐 화합물 및 사용 방법
CN101456863B (zh) * 2007-12-14 2012-04-25 华北制药集团新药研究开发有限责任公司 Lxr激动剂及其制备方法和用途
WO2010003022A1 (en) 2008-07-01 2010-01-07 Genentech, Inc. Isoindolone derivatives as mek kinase inhibitors and methods of use
JP5544358B2 (ja) 2008-07-01 2014-07-09 ジェネンテック， インコーポレイテッド 置換二環式ヘテロ環化合物と使用方法
CN103517908A (zh) 2010-09-07 2014-01-15 Seoul大学校产学协力财团 二倍半萜化合物及其用途
WO2012074780A1 (en) 2010-12-03 2012-06-07 Allergan, Inc. Novel oxime azetidine derivatives as sphingosine 1-phosphate (s1p) receptor modulators
CA2819603A1 (en) 2010-12-03 2012-06-07 Allergan, Inc. Novel oxime derivatives as sphingosine 1-phosphate (s1p) receptor modulators
WO2015106164A1 (en) 2014-01-10 2015-07-16 Rgenix, Inc. Lxr agonists and uses thereof
EP3402477A4 (en) 2016-01-11 2019-08-21 The Rockefeller University METHODS FOR THE TREATMENT OF DISORDERS ASSOCIATED WITH SUPPRESSIVE CELLS DERIVED FROM MYELOID CELLS
WO2019104062A1 (en) 2017-11-21 2019-05-31 Rgenix, Inc. Polymorphs and uses thereof
ES2982346T3 (es) 2019-12-13 2024-10-15 Inspirna Inc Sales metálicas y usos de las mismas
US11753374B2 (en) * 2020-11-18 2023-09-12 Southern Reserach Institute Compounds for the treatment of acute and chronic kidney disease

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL141080A0 (en) 1998-07-30 2002-02-10 Japan Tobacco Inc Disubstituted maleimide derivatives and pharmaceutical compositions containing the same
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.
AU6074700A (en) * 1999-07-08 2001-01-30 Tularik Inc. Compositions and methods for raising hdl cholesterol levels
AU6593600A (en) 1999-08-20 2001-03-19 Rei Asakai Drugs inhibiting cell death
GB0008264D0 (en) 2000-04-04 2000-05-24 Smithkline Beecham Plc Novel method and compounds

Also Published As

Publication number Publication date
EP1646626B1 (en) 2008-07-02
JP2007521312A (ja) 2007-08-02
HK1088320A1 (en) 2006-11-03
IS8293A (is) 2006-02-09
US7432288B2 (en) 2008-10-07
NO20060081L (no) 2006-02-08
WO2005005417A1 (en) 2005-01-20
UY28408A1 (es) 2005-02-28
MY135821A (en) 2008-07-31
CA2532056A1 (en) 2005-01-20
DE602004014773D1 (de) 2008-08-14
US20060235015A1 (en) 2006-10-19
GB0316232D0 (en) 2003-08-13
AU2004255999A1 (en) 2005-01-20
EP1646626A1 (en) 2006-04-19
TW200503691A (en) 2005-02-01
ATE399777T1 (de) 2008-07-15
SA04250204B1 (ar) 2008-03-23
AU2004255999B2 (en) 2007-08-02
IL172760A0 (en) 2006-04-10
RU2006102130A (ru) 2007-08-20
UA82109C2 (uk) 2008-03-11
KR20060035748A (ko) 2006-04-26
ES2308204T3 (es) 2008-12-01
ZA200600222B (en) 2007-04-25
MXPA06000414A (es) 2006-03-17
BRPI0412472A (pt) 2006-09-19
CN1823061A (zh) 2006-08-23

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