HUP0303272A2 - Metabolikus modulátorként alkalmazható melonil-CoA dekarboxiláz inhibitor azol-származékok és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Metabolikus modulátorként alkalmazható melonil-CoA dekarboxiláz inhibitor azol-származékok és ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

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HUP0303272A2
HUP0303272A2 HU0303272A HUP0303272A HUP0303272A2 HU P0303272 A2 HUP0303272 A2 HU P0303272A2 HU 0303272 A HU0303272 A HU 0303272A HU P0303272 A HUP0303272 A HU P0303272A HU P0303272 A2 HUP0303272 A2 HU P0303272A2
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group
heteroatoms
substituted
substituent
membered ring
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HU0303272A
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Thomas Arrhenius
Jie Fei Cheng
Rossy Serafimov
Mark Wilson
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Chugai Seiyaku Kabushiki Kaisha
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Publication of HUP0303272A3 publication Critical patent/HUP0303272A3/hu
Publication of HU229431B1 publication Critical patent/HU229431B1/hu

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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Abstract

A találmány szerinti vegyületek (I) vagy (II) általános képletében Yjelentése S, O, C jelentése szubsztituált monociklusos 5-7 tagú gyűrű,amely 1-3 heteroatomként O, N és/vagy S atomot tartalmaz, ahol aszubsztituens egymástól függetlenül R1 vagy R2, R1 és R2 jelentéseegymástól eltérő és egymástól függetlenül hidrogénatom; halogénatom,hidroxilcsoport, nitrocsoport, cianocsoport, 1-12 szénatomosalkilcsoport, 1-12 szénatomos szubsztituált alkilcsoport,alkilaminocsoport, alkilszulfanilcsoport, arilcsoport, 1-12 szénatomosalkoxicsoport, 1-12 szénatomos szubsztituált alkoxicsoport, C(X)R3, -CR11(V)R12; -CH2CR11(V)R12, -S(O)nR3, -NR4P(O)(R5)2, vagy -P(O)(R5)2,képletű csoport vagy adott esetben szubsztituált monociklusos 3-7 tagúgyűrű, amely 0-3 heteroatomként O, N és/vagy S atomot tartalmaz, ésahol a szubsztituens R9 csoport, vagy R1 vagy R2 jelentése (a), (b),(c) vagy (d) általános képletű csoport, vagy R1 és R2 jelentése együttadott esetben szubsztituált 5-7 tagú gyűrű, amely 0-3 heteroatomkéntN, O és/vagy S atomot tartalmaz, és ahol a szubsztituens R9 csoport,R6 jelentése a (II) általános képletben 5 vagy 6 helyzetben előfordulócsoport, amely NR8P(O)(R5)2 képletű csoport (a), (b'), (c') vagy (d')általános képletű csoport, R7 jelentése hidrogénatom, 1-12 szénatomosalkilcsoport, 1-12 szénatomos alkoxicsoport, halogénatom,cianocsoport, SO2R4 vagy SO2NR4R4 képletű csoport, vagy R7 és R6jelentése együtt fuzionált szubsztituált 5-7 tagú gyűrű, amely 1-3heteroatomként N, O és/vagy S atomot tartalmaz, ahol a szubsztituensR9 csoport, és ezek enantiomer, diasztereoizomer vagy tautomer formáiés ezek farmakológiailag alkalmazható sói vagy prodrug formáifarmakológiailag alkalmazható hordozóanyagban. A találmány kiterjed afenti vegyületek gyógyszerként történő alkalmazására, és avegyületeket tartalmazó gyógyszerkészítményekre is. Ó
HU0303272A 2001-02-20 2002-02-19 Azoles as malonyl-coa decarboxylase inhibitors useful as metabolic modulators HU229431B1 (en)

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US27003401P 2001-02-20 2001-02-20
PCT/US2002/004777 WO2002066035A2 (en) 2001-02-20 2002-02-19 Azoles as malonyl-coa decarboxylase inhibitors useful as metabolic modulators

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HUP0303272A2 true HUP0303272A2 (hu) 2004-01-28
HUP0303272A3 HUP0303272A3 (en) 2007-03-28
HU229431B1 HU229431B1 (en) 2013-12-30

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EP (2) EP1379243B1 (hu)
JP (4) JP4155351B2 (hu)
KR (1) KR100659427B1 (hu)
CN (1) CN100383132C (hu)
AT (2) ATE442141T1 (hu)
AU (1) AU2002251987B2 (hu)
BR (1) BR0207408A (hu)
CA (1) CA2437409C (hu)
CY (1) CY1110986T1 (hu)
DE (2) DE60233650D1 (hu)
DK (1) DK1370260T3 (hu)
ES (2) ES2353686T3 (hu)
HK (1) HK1062633A1 (hu)
HU (1) HU229431B1 (hu)
IL (2) IL156827A0 (hu)
MX (1) MXPA03007441A (hu)
NO (1) NO20033665L (hu)
NZ (1) NZ526883A (hu)
PL (1) PL204456B1 (hu)
PT (1) PT1370260E (hu)
RU (1) RU2258706C2 (hu)
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US7709510B2 (en) * 2001-02-20 2010-05-04 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
WO2003090746A1 (en) * 2002-04-23 2003-11-06 Chugai Seiyaku Kabushiki Kaisha 1,3-thiazoles as lxr modulators in the treatment of cardiovascular diseases
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