BR112014031845A2 - 2,3-diidro-1h-imidazo{1,2-a}pirimidin-5-ona e estes derivados de 1,2,3,4-tetraidropirimido{1,2-a}pirimidin-6-ona compreendendo uma morfolina substituída, preparação da mesma e uso farmacêutico da mesma - Google Patents

2,3-diidro-1h-imidazo{1,2-a}pirimidin-5-ona e estes derivados de 1,2,3,4-tetraidropirimido{1,2-a}pirimidin-6-ona compreendendo uma morfolina substituída, preparação da mesma e uso farmacêutico da mesma

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Publication number
BR112014031845A2
BR112014031845A2 BR112014031845A BR112014031845A BR112014031845A2 BR 112014031845 A2 BR112014031845 A2 BR 112014031845A2 BR 112014031845 A BR112014031845 A BR 112014031845A BR 112014031845 A BR112014031845 A BR 112014031845A BR 112014031845 A2 BR112014031845 A2 BR 112014031845A2
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Prior art keywords
alkyl
cycloalkyl
formula
pyrimidin
heteroaryl
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BR112014031845A
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English (en)
Inventor
Ronan Baptiste
Vivet Bertrand
Filoche-Romme Bruno
Marciniak Gilbert
Letallec Jean-Philippe
Brollo Maurice
El-Ahmad Youssef
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Sanofi Sa
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Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of BR112014031845A2 publication Critical patent/BR112014031845A2/pt

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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
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    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
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    • C07D487/04—Ortho-condensed systems

Abstract

abstract: (en)the invention relates to the novel products of formula (i) with p, q = 0, 1 or 2; r1 = phenyl, pyridyl; -(ch2) m -ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; -so2 -rb; -co-re; m = 1 or 2; ra = aryl, heteroaryl, -co-cycloalkyl, -co-heterocycloalkyl, -co-rb, -c(rb)=n-orc, -co 2 rd, -conrxry; rb = alkyl, aryl, heteroaryl; rc = h, alkyl; rd = alkyl, cycloalkyl; re = alkyl, cycloalkyl, aryl, heteroaryl; nrxry with rx,ry = h, alkyl, cycloalkyl, alkoxy, phenyl, or form with n a ring with optionally o, n; r2, r3 = h, alkyl, cf 3, or form with c a ring with optionally o, s and n; r4 = h, f, cl, ch3 or cn; the morpholine is substituted with me, and optionally substituted with f, oh; or is (formula 1a) and the isomer of configuration r,r (formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments. tradução do resumo resumo patente de invenção: "2,3-diidro-1h-imidazo{1,2-a}pirimidin-5-ona e estes derivados de 1,2,3,4-tetraidropirimido{1,2-a}pirimidin-6-ona compreendendo uma morfolina substituída, preparação da mesma e uso farmacêutico da mesma". a presente invenção refere-se a novos produtos de fórmula (i) com p, q = 0, 1 ou 2; r1 = fenila, piridila; -(ch2)m-ra; alquileno; cicloalquila; heterocicloalquila; alquila; -so2-rb; -co-re; m = 1 ou 2; ra = arila, heteroarila, -co-cicloalquila, -co-heterocicloalquila, -co-rb, -c(rb)=n-orc, -co2rd, -conrxry; rb = alquila, arila, heteroarila; rc = h, alquila; rd = alquila, cicloalquila; re = alquila, cicloalquila, arila, heteroarila; nrxry com rx,ry = h, alquila, cicloalquila, alcóxi, fenila, ou formam-se com n, um anel com opcionalmente o, n; r2, r3 = h, alquila, cf 3, ou formam-se com c, um anel com opcionalmente o, s e n; r4 = h, f, cl, ch3 ou cn; a morfolina é substituída com me, e opcionalmente substituída com f, oh; ou é (fórmula la) e o isômero da configuração r,r (fórmula lb) fórmula 1a fórmula 1b estes produtos sendo em todas as formas de isômero e os sais, como medicamentos, em particular como medicamentos anticâncer.
BR112014031845A 2012-06-22 2013-06-21 2,3-diidro-1h-imidazo{1,2-a}pirimidin-5-ona e estes derivados de 1,2,3,4-tetraidropirimido{1,2-a}pirimidin-6-ona compreendendo uma morfolina substituída, preparação da mesma e uso farmacêutico da mesma BR112014031845A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR1255917A FR2992314B1 (fr) 2012-06-22 2012-06-22 Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one et 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one comportant une morpholine substituee, leur preparation et leur utilisation pharmaceutique
PCT/IB2013/055099 WO2013190510A2 (en) 2012-06-22 2013-06-21 NOVEL 2,3-DIHYDRO-1H-IMIDAZO{1,2-a}PYRIMIDIN-5-ONE and this1,2,3,4-TETRAHYDROPYRIMIDO{1,2-a}PYRIMIDIN-6-ONE DERIVATIVES COMPRISING A SUBSTITUTED MORPHOLINE, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF

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BR112014031845A2 true BR112014031845A2 (pt) 2017-06-27

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BR112014031845A BR112014031845A2 (pt) 2012-06-22 2013-06-21 2,3-diidro-1h-imidazo{1,2-a}pirimidin-5-ona e estes derivados de 1,2,3,4-tetraidropirimido{1,2-a}pirimidin-6-ona compreendendo uma morfolina substituída, preparação da mesma e uso farmacêutico da mesma

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US (2) US10253043B2 (pt)
EP (1) EP2864295B1 (pt)
JP (1) JP2015525236A (pt)
KR (1) KR20150023799A (pt)
CN (1) CN104603113B (pt)
AR (1) AR091498A1 (pt)
AU (1) AU2013278875B2 (pt)
BR (1) BR112014031845A2 (pt)
CA (1) CA2877089A1 (pt)
DK (1) DK2864295T3 (pt)
ES (1) ES2662803T3 (pt)
FR (1) FR2992314B1 (pt)
IL (1) IL236170A (pt)
IN (1) IN2014KN02940A (pt)
MX (1) MX350682B (pt)
PL (1) PL2864295T3 (pt)
PT (1) PT2864295T (pt)
RU (1) RU2015101798A (pt)
SG (1) SG11201408207TA (pt)
TW (1) TW201402577A (pt)
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RU2561130C2 (ru) * 2009-07-02 2015-08-20 Санофи НОВЫЕ ПРОИЗВОДНЫЕ 1,2,3,4-ТЕТРАГИДРОПИРИМИДО{1,2-a}ПИРИМИДИН-6-ОНА, ИХ ПОЛУЧЕНИЕ И ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ
RU2554868C2 (ru) 2009-07-02 2015-06-27 Санофи НОВЫЕ ПРОИЗВОДНЫЕ 2,3-ДИГИДРО-1Н-ИМИДАЗО[1,2-а]ПИРИМИДИН-5-ОНА, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ В ФАРМАЦИИ
EP2655375B1 (fr) 2010-12-23 2014-12-03 Sanofi Derives de pyrimidinone, leur preparation et leur utilisation pharmaceutique
FR2992316A1 (fr) * 2012-06-22 2013-12-27 Sanofi Sa Derives de pyrimidinones, leur preparation et leur application en therapeutique

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US20150148328A1 (en) 2015-05-28
US20190292205A1 (en) 2019-09-26
FR2992314B1 (fr) 2015-10-16
JP2015525236A (ja) 2015-09-03
EP2864295A2 (en) 2015-04-29
IL236170A0 (en) 2015-02-01
WO2013190510A2 (en) 2013-12-27
AU2013278875B2 (en) 2017-06-15
CN104603113A (zh) 2015-05-06
PT2864295T (pt) 2018-03-15
RU2015101798A (ru) 2016-08-10
KR20150023799A (ko) 2015-03-05
CA2877089A1 (en) 2013-12-27
WO2013190510A3 (en) 2014-03-06
IN2014KN02940A (pt) 2015-05-08
MX350682B (es) 2017-09-13
AU2013278875A1 (en) 2015-01-22
US11739100B2 (en) 2023-08-29
PL2864295T3 (pl) 2018-06-29
TW201402577A (zh) 2014-01-16
EP2864295B1 (en) 2017-12-13
SG11201408207TA (en) 2015-01-29
CN104603113B (zh) 2020-01-21
US10253043B2 (en) 2019-04-09
IL236170A (en) 2017-03-30
AR091498A1 (es) 2015-02-11

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