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    • 1. 发明申请
    • 2-AMINO-2-PHENYLALKANOL DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    • 2-氨基-2-苯基卡诺醇衍生物及其制备方法和含有该组合物的药物组合物
    • WO2009112703A1
    • 2009-09-17
    • PCT/FR2009000106
    • 2009-01-30
    • OROXCELLDENIS ALEXISPACHOT JEANDINI CHRISTOPHE
    • DENIS ALEXISPACHOT JEANDINI CHRISTOPHE
    • C07C217/48A61K31/135A61K31/24C07C219/22
    • C07C271/16A61K9/2054C07C219/22C07C271/22C07C271/48C07C333/04C07D213/80C07D213/82C07D317/40
    • Esters derived from 2-amino-2-phenylalkanol of general formula (I) in which: R1 is H, straight or branched C1 to C4 alkyl, straight or branched C2 to C4 alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a -CO-R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or else R2 is a -CO-Y-R4 radical for which Y is -O-, -S-, -NH-, or -Nalk- for which alk is straight or branched (C1 to C4) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, which may be substituted by one or more halogen atoms or OH radicals, straight or branched (C1 to C4) alkyl radicals, or straight or branched (C1 to C4) alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino radicals, or oxo radicals, or which may be substituted by R5COO- in which R5 is an alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by the residue of an amino acid, or represents a heterocycle, or else R2 is a (C2 to C4) alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino optionally forming, with the nitrogen atom to which they are attached, a 5-or 6-membered heterocycle optionally bearing another heteroatom (O or N), or substituted by alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, it being understood that said straight or branched substituted alkyl radical comprises at least C2 between >N-R2 and the substituent; and R3 is a straight or branched (C1 to C4) alkyl unless specifically mentioned, alkyl or acyl are straight or branched (C1 to C7), in their R or S forms or mixtures thereof, and also the pharmaceutically acceptable salts thereof when they exist.
    • 衍生自通式(I)的2-氨基-2-苯基烷醇的酯,其中:R 1是H,直链或支链C 1 -C 4烷基,被OH取代的直链或支链C 2 -C 4烷基,烷氧基,烷硫基,酰氧基,NH 2, 烷基氨基,二烷基氨基,烷基氨基甲酰氧基,烷氧基羰基氨基,脲基或烷基脲基,R 2为其中R为H,烷基,芳基,杂环基,苄基或杂环基甲基或其中R 2为-CO-Y- Y是-O - , - S - , - NH-或-Nalk-,其中alk是直链或支链(C1-C4)烷基,R4是烷基,芳基,芳烷基或杂环基烷基, (C 1 -C 4)烷基或直链或支链(C 1 -C 4)烷氧基,烷硫基,酰氨基烷硫基,烷氧羰基或酰氨基,或氧代基,或可被R 5 COO- 其中R5是任选被苄氧羰基氨基,酰氨基或氨基酸残基取代的烷基,或者代表a 杂环,或者R 2是被OH,烷氧基,烷硫基,酰氧基,NH 2,烷基氨基,二烷基氨基取代的(C 2 -C 4)烷基,其任选地与它们所连接的氮原子一起形成5-或6-元杂环 带有另一个杂原子(O或N),或被烷基氨基甲酰氧基,烷氧基羰基氨基,脲基或烷基脲基取代,应理解为所述直链或支链取代的烷基包含> N-R2与取代基之间的至少C2; 除非特别提及,R 3是直链或支链(C 1 -C 4)烷基,烷基或酰基是直链或支链(C 1 -C 7),它们的R或S形式或其混合物,以及它们存在时的药学上可接受的盐 。
    • 5. 发明专利
    • 2-AMINO-2-PHENYL-ALKANOL DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    • ZA201005316B
    • 2011-10-26
    • ZA201005316
    • 2010-07-26
    • OROXCELLDENIS ALEXIS
    • DENIS ALEXISPACHOT JEANDINI CHRISTOPHE
    • C07C20060101A61K20060101
    • 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino optionally forming, with the nitrogen atom to which they are attached, a 5- or 6-member heterocycle optionally having another heteroatom (O or N), or substituted by alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, it being understood that said straight or branched substituted alkyl radical comprises at least 2C between >N—R2 and the substituent; and R3 is alkyl (1 to 4C) straight or branched unless specifically mentioned, alkyl or acyl are straight or branched (1 to 7C), in their R or S forms or their mixtures, as well as their pharmaceutically acceptable salts when these exist.
    • 6. 发明专利
    • 2-amino-2-phenylalkanol derivatives, preparation thereof and pharmaceutical compositions containing same
    • AU2009224558A1
    • 2009-09-17
    • AU2009224558
    • 2009-01-30
    • OROXCELLDENIS ALEXIS
    • DINI CHRISTOPHEDENIS ALEXISPACHOT JEAN
    • C07C217/48A61K31/135A61K31/24C07C219/22
    • 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino optionally forming, with the nitrogen atom to which they are attached, a 5- or 6-member heterocycle optionally having another heteroatom (O or N), or substituted by alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, it being understood that said straight or branched substituted alkyl radical comprises at least 2C between >N—R2 and the substituent; and R3 is alkyl (1 to 4C) straight or branched unless specifically mentioned, alkyl or acyl are straight or branched (1 to 7C), in their R or S forms or their mixtures, as well as their pharmaceutically acceptable salts when these exist.
    • 7. 发明专利
    • DERIVES DE 2 AMINO -2- PHENYL-ALKANOL, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENENT
    • TN2010000328A1
    • 2011-12-29
    • TN2010000328
    • 2010-07-16
    • DENIS ALEXISOROXCELL
    • DENIS ALEXISPACHOT JEANDINI CHRISTOPHE
    • A61K31/135A61K31/24C07C217/48C07C219/22
    • Esters dérivés de 2-amino-2-phényl-alkanol de formule générale (I) dans laquelle : R1 est H, alkyle 1 à 4C droit ou ramifié, alkyle 2 à 4C droit ou ramifié substitué par OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, uréido ou alkyluréido, R2 est un radical -CO-R dans lequel R est H, alkyle, aryle, hétérocyclyle, benzyle ou hétérocyclylméthyle, ou bien R2 est un radical -CO- Y-R4 pour lequel Y est -O-, -S-, -NH-, -NaIk- pour lequel alk est alkyle droit ou ramifié (1 à 4C), et R4 est alkyle, aryle, aralkyle ou hétérocyclylalkyle, pouvant être substitués par un ou plusieurs atomes d'halogène ou radicaux OH, alkyle (1 à 4C) droit ou ramifié, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyle ou acylamino (1 à 4C) droits ou ramifiés, ou oxo, ou pouvant être substitués par R5COO- dans lequel R5 est alkyle éventuellement substitué par benzyloxycarbonylamino, acylamino ou par le reste d'un aminoacide, ou représente un hétérocycle, ou bien R2 est alkyle (2 à 4C) substitué par OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino formant éventuellement avec l'atome d'azote auquel elles sont attachées, un hétérocycle à 5 ou 6 chaînons portant éventuellement un autre hétéroatome (O ou N), ou substitué par alkylcarbamoyloxy, alkoxycarbonylamino, uréido ou alkyluréido, étant entendu que ledit radical alkyle substitué droit ou ramifié, comporte au moins 2C entre >N-R2 et le substituant; et R3 est alkyle (1 à 4C) droit ou ramifié sauf mention spéciale, alkyle ou acyle sont droits ou ramifiés (1 à 7C), sous leurs formes R ou S ou leurs mélanges, ainsi que leurs sels pharmaceutiquement acceptables lorsqu'ils existent.
    • 8. 发明专利
    • HK1147090A1
    • 2011-07-29
    • HK11101187
    • 2011-02-08
    • OROXCELLDENIS ALEXIS
    • DENIS ALEXISPACHOT JEANDINI CHRISTOPHE
    • A61K20060101C07C20060101
    • 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino optionally forming, with the nitrogen atom to which they are attached, a 5- or 6-member heterocycle optionally having another heteroatom (O or N), or substituted by alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, it being understood that said straight or branched substituted alkyl radical comprises at least 2C between >N—R2 and the substituent; and R3 is alkyl (1 to 4C) straight or branched unless specifically mentioned, alkyl or acyl are straight or branched (1 to 7C), in their R or S forms or their mixtures, as well as their pharmaceutically acceptable salts when these exist.
    • 9. 发明专利
    • Derivados de 2-amino-2-fenil-alcanol, su preparación y composiciones farmacéuticas que los contienen
    • ES2400080T3
    • 2013-04-05
    • ES09720924
    • 2009-01-30
    • OROXCELLDENIS ALEXIS
    • DENIS ALEXISPACHOT JEANDINI CHRISTOPHE
    • C07C217/48A61K31/135A61K31/24C07C219/22
    • Un éster derivado de 2-amino-2-fenil-alcanol de fórmula general: en la que: R1 es un átomo de hidrógeno, un radical alquilo que contiene de 1 a 4 átomos de carbono en cadena recta o ramificada, un radical alquilo que contiene de C2 a C4 en cadena recta o ramificada sustituido por hidroxi, alcoxi, alquiltio, aciloxi, amino, alquilamino, dialquilamino, alquil-carbamoyl-oxi, alcoxicarbonilamino, ureido o alquiureido, R2 es un radical -CO-R en el que R es un radical alquilo, un radical arilo, heterociclilo, bencilo o heterociclilmetilo,un radical -CO- Y-R4 para el que Y es un heteroátomo elegido entre -O-, -S-, -NH-, -Nalk- para el que alk es un radicalalquilo recto o ramificado que contiene de C1 a C4, y R4 se elige entre los radicales alquilo, arilo, aralquilo o heterociclilalquilo, que pueden sustituirse por uno o varios átomos de halógeno o radicales hidroxi, alquilo con C1 a C4en cadena recta o ramificada, alcoxi, alquiltio, acilamino alquiltio, alcoxicarbonilo o acilamino cuyos restos alquilocontienen de C1 a C4 en cadena recta o ramificada, u oxo, o que pueden sustituirse por un radical R5COO- en el que R5representa un radical alquilo, eventualmente sustituido por benciloxicarbonilamino, acilamino o por el resto de unaminoácido, o representa un heterociclo, o bien R2 es un radical alquilo que contiene de C2 a C4, sustituido por hidroxi, alcoxi, alquiltio, aciloxi, amino, alquilamino,dialquilamino cuyas partes alcohilo pueden formar con el átomo de nitrógeno al que están ligados, un heterociclo de 5 ó6 eslabones que contienen, eventualmente, otro heteroátomo elegido entre el oxígeno o el nitrógeno, o sustituido poralquil-carbamoyl-oxi, alcoxicarbonilamino, ureido o alquilureido, quedando entendido que dicho radical alquilo sustituidoestá en cadena recta o ramificada y contiene al menos 2 átomos de carbono entre el átomo de nitrógeno con R2 y el sustituyente; R3 es un radical alquilo que contiene de 1 a 4 átomos de carbono en cadena recta o ramificada,en sus formas R o S o sus mezclas, así como sus sales farmacéuticamente aceptables, cuando existen.
    • 10. 发明专利
    • Dérivés de 2-amino-2-phenyl-alkanol, leur preparation et les compositions pharmaceutiques qui les contiennent
    • MA32125B1
    • 2011-03-01
    • MA33019
    • 2010-07-15
    • OROXCELLDENIS ALEXIS
    • DENIS ALEXISPACHOT JEANDINI CHRISTOPHE
    • C07C217/48A61K31/135A61K31/24
    • Esters dérivés de 2-amino-2-phényl-alkanol de formule générale (i) dans laquelle : r1 est h, alkyle 1 à 4c droit ou ramifié, alkyle 2 à 4c droit ou ramifié substitué par oh, alkoxy, alkylthio, acyloxy, nh2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, uréido ou alkyluréido, r2 est un radical -co-r dans lequel r est h, alkyle, aryle, hétérocyclyle, benzyle ou hétérocyclylméthyle, ou bien r2 est un radical -co- y-r4 pour lequel y est -o-, -s-, -nh-, -naik- pour lequel alk est alkyle droit ou ramifié (1 à 4c), et r4 est alkyle, aryle, aralkyle ou hétérocyclylalkyle, pouvant être substitués par un ou plusieurs atomes d'halogène ou radicaux oh, alkyle (1 à 4c) droit ou ramifié, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyle ou acylamino (1 à 4c) droits ou ramifiés, ou oxo, ou pouvant être substitués par r5coo- dans lequel r5 est alkyle éventuellement substitué par benzyloxycarbonylamino, acylamino ou par le reste d'un aminoacide, ou représente un hétérocycle, ou bien r2 est alkyle (2 à 4c) substitué par oh, alkoxy, alkylthio, acyloxy, nh2, alkylamino, dialkylamino formant éventuellement avec l'atome d'azote auquel elles sont attachées, un hétérocycle à 5 ou 6 chaînons portant éventuellement un autre hétéroatome (o ou n), ou substitué par alkylcarbamoyloxy, alkoxycarbonylamino, uréido ou alkyluréido, étant entendu que ledit radical alkyle substitué droit ou ramifié, comporte au moins 2c entre >n-r2 et le substituant; et r3 est alkyle (1 à 4c) droit ou ramifié sauf mention spéciale, alkyle ou acyle sont droits ou ramifiés (1 à 7c), sous leurs formes r ou s ou leurs mélanges, ainsi que leurs sels pharmaceutiquement acceptables lorsqu'ils existent.