ES2188280T3 - Acetales heteroaril-ciclicos. - Google Patents

Acetales heteroaril-ciclicos.

Info

Publication number
ES2188280T3
ES2188280T3 ES99962334T ES99962334T ES2188280T3 ES 2188280 T3 ES2188280 T3 ES 2188280T3 ES 99962334 T ES99962334 T ES 99962334T ES 99962334 T ES99962334 T ES 99962334T ES 2188280 T3 ES2188280 T3 ES 2188280T3
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ES
Spain
Prior art keywords
compounds
formula
optionally substituted
prodrugs
oxides
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES99962334T
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English (en)
Inventor
Alan John Collis
Frank Rhene-Poulenc Ror Halley
Iain Mcfarlane Rhene-Pou Mclay
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sanofi Aventis UK Holdings Ltd
Original Assignee
Aventis Pharma 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
Priority claimed from GBGB9827721.3A external-priority patent/GB9827721D0/en
Application filed by Aventis Pharma Ltd filed Critical Aventis Pharma Ltd
Application granted granted Critical
Publication of ES2188280T3 publication Critical patent/ES2188280T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic 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
    • A61P3/04—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
    • A61P3/08—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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07D413/14—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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto de fórmula (I):**(Fórmula)** en la que Het es un anillo heteroaromático de cinco o seis miembros de fórmula **(Fórmula)** en la que uno de R1 y R2 es heteroarilo opcionalmente sustituido y el otro es heteroarilo opcionalmente sustituido o arilo opcionalmente sustituido; X1 es un enlace, X3 y X4 son cada uno independientemente N o C, y X2 y X5 son independientemente CH, N, NH, O o S; o X3 y X4 son C, uno de X1, X2 y X5 es N y los otros son N o CH; pero excluyendo compuestos en los que X1 es un enlace, uno de X2 y X5 es N y el otro es NH y X3 y X4 son ambos C; R3 representa un grupo -L1-R6; R4 representa hidrógeno, alquilo o hidroxialquilo; o R3 y R4, cuando están unidos al mismo átomo de carbono, pueden formar con dicho átomo de carbono un anillo de cicloalquilo, cicloalquenilo o heterocicloalquilo o un grupo C=CH2; R5 representa hidrógeno o alquilo; R6 es hidrógeno, alquilo, azido, hidroxi, alcoxi, arilo, arilalquiloxi, ariloxi, carboxi (o -C(=O)-NHOH, -C(=O)-CH2OH, -C(=O)-CH2SH, -C(=O)-NH-CN, sulfo, fosfono, alquilsulfonilcarbamoilo, tetrazolilo, arilsulfonil-carbamoilo, heteroarilsulfonilcarbamoilo, N-metoxi-carbamoilo, 3-hidroxi-3-ciclobuten1, 2-diona, 3, 5-dioxo-1, 2, 4-oxadiazolidinilo, 3-hidroxiisoxazolilo, o 3-hidroxi-1-metilpirazolilo), cicloalquilo, cicloalquiloxi, heteroarilo, heteroarilalquiloxi, heteroariloxi, hetero-cicloalquilo, heterocicloalquiloxi, nitro, -NY1Y2, -N(R7)-C(=Z~-R8, -N(R7)-C%=Z)-L2-R9, -NH-C(=Z)-NH-R8, -NH-C(=Z)-NH-L2-R9, -N(R7)SO2-R8, -N(R7)-SO2-L-R9, -S(O)nR1, -C(=Z)-NY1Y2 o -C(=Z)-OR10; R7 es hidrógeno, alquilo, arilo, arilalquilo, cicloalquilo, heteroarilo, heteroarilalquilo o heterocicloalquilo; R8 es alquilo, alcoxi, arilo, arilalquiloxi, cicloalquilo, heteroarilo, heteroarilalquiloxi o heterocicloalquilo; R9 es alcoxi, arilo, arilalquiloxi, arilalquiloxicarbonilamino, carboxi (o un -C(=O)-NHOH, (C=O)-CH2OH, -C(=O)-CH2SH, -C(=)-NH-CN, sulfo, fosfono, alquilsulfonilcarbamoilo, tetrazolilo, arilsulfonil-carbamoilo, heteroarilsulfonilcarbamoilo, N-metoxi-carbamoilo, 3-hidroxi-3-ciclobuten-1, 2diona, 3, 5-dioxo-1, 2, 4-oxadiazolidinilo, 3-hidroxiisoxazolilo o 3-hidroxi-1-metilpirazolilo), cicloalquilo, ciano, halógeno, heteroarilo, heteroarilalcoxi, heterocicloalquilo, hidroxi, o -NY3Y4; R10 es alquilo, arilo, arilalquilo, cicloalquilo, heteroarilo, heteroarilalquilo o heterocicloalquilo; L1 representa un enlace directo o una unión alquileno de cadena lineal o ramificada que contiene de 1 a 6 átomos de carbono, y opcionalmente sustituido con halógeno, hidroxi, alcoxi u oxo; L2 es una unión alquileno de cadena lineal o ramificada que contiene de 1 a 6 átomos de carbono; Y1 e Y2 son independientemente hidrógeno, alquenilo, alquinilo, arilo, cicloalquilo, heterocicloalquilo, heteroarilo o alquilo opcionalmente sustituido con alcoxi, arilo, ciano, cicloalquilo, heteroarilo, heterocicloalquilo, hidroxi, oxo, -CO2R7, -CONY3Y4 o -NY3Y4, o el grupo -NY1Y2 puede formar una amina cíclica de 5-7 miembros, la cual (i) puede estar opcionalmente sustituida con uno o más sustituyentes seleccionados de alcoxi, carboxamido, carboxi, hidroxi, oxo (o uno de sus derivados acetal cíclico de 5, 6, ó 7 miembros), alquilo, arilo, arilalquilo, cicloalquilo, heteroarilo, heteroarilalquilo o heterocicloalquilo o alquilo sustituido con carboxi, carboxamido, o hidroxi, (ii) también puede contener un heteroátomo adicional seleccionado de O, S, SO2 o NY5 y (iii) también puede estar condensada a anillos de arilo, heteroarilo, heterocicloalquilo o cicloalquilo adicionales para formar un sistema de anillo bicíclico o tricíclico: Y3 e Y4 son independientemente hidrógeno, alquenilo, alquilo, alquinilo, arilo, arilalquilo, cicloalquilo, heteroarilo o heteroarilalquilo, o el grupo -NY3Y4 puede formar una amina cíclica de 5-7 miembros como se ha definido para -NY1Y2 antes; Y5 es hidrógeno, alquilo, arilo, arilalquilo, -C(=Z)R10, -C(=Z)OR10 o -SO2R10; Z es un átomo de oxígeno o azufre; m es cero o un número entero 1 ó 2; y n es cero o un número entero 1 ó 2; y sus N-óxidos, y sus profármacos; y sales y solvatos farmacéuticamente aceptables de compuestos de fórmula (I), y sus N-óxidos, y sus profármacos.
ES99962334T 1998-12-16 1999-12-16 Acetales heteroaril-ciclicos. Expired - Lifetime ES2188280T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9827721.3A GB9827721D0 (en) 1998-12-16 1998-12-16 Chemical compounds
US12242599P 1999-03-02 1999-03-02

Publications (1)

Publication Number Publication Date
ES2188280T3 true ES2188280T3 (es) 2003-06-16

Family

ID=26314848

Family Applications (1)

Application Number Title Priority Date Filing Date
ES99962334T Expired - Lifetime ES2188280T3 (es) 1998-12-16 1999-12-16 Acetales heteroaril-ciclicos.

Country Status (11)

Country Link
US (1) US7479501B2 (es)
EP (1) EP1140916B1 (es)
JP (1) JP4634613B2 (es)
AT (1) ATE227719T1 (es)
AU (1) AU768259B2 (es)
CA (1) CA2355075C (es)
DE (1) DE69903976T2 (es)
DK (1) DK1140916T3 (es)
ES (1) ES2188280T3 (es)
PT (1) PT1140916E (es)
WO (1) WO2000035911A1 (es)

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DE69914357T2 (de) 1998-11-04 2004-11-11 Smithkline Beecham Corp. Pyridin-4-yl oder pyrimidin-4-yl substituierte pyrazine
GB9923078D0 (en) * 1999-09-29 1999-12-01 Phytopharm Plc Sapogenin derivatives and their use
EP1233950B1 (en) 1999-11-23 2005-10-05 Smithkline Beecham Corporation 3,4-DIHYDRO-(1H)QUINAZOLIN-2-ONE COMPOUNDS AS CSBP/P39 kINASE INHIBITORS
ATE281439T1 (de) 1999-11-23 2004-11-15 Smithkline Beecham Corp 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren
JP2003514900A (ja) 1999-11-23 2003-04-22 スミスクライン・ビーチャム・コーポレイション ＣＳＢＰ／ｐ３８キナーゼ阻害剤としての３，４−ジヒドロ−（１Ｈ）−キナゾリン−２−オン化合物
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
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Also Published As

Publication number Publication date
JP4634613B2 (ja) 2011-02-16
ATE227719T1 (de) 2002-11-15
DE69903976T2 (de) 2003-07-24
AU1871100A (en) 2000-07-03
US20050090501A1 (en) 2005-04-28
DE69903976D1 (de) 2002-12-19
PT1140916E (pt) 2003-03-31
JP2002532495A (ja) 2002-10-02
EP1140916B1 (en) 2002-11-13
WO2000035911A1 (en) 2000-06-22
CA2355075A1 (en) 2000-06-22
DK1140916T3 (da) 2003-03-10
EP1140916A1 (en) 2001-10-10
US7479501B2 (en) 2009-01-20
AU768259B2 (en) 2003-12-04
CA2355075C (en) 2009-12-08

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