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    • 1. 发明申请
      US20120129909A1 2-AMINO-2-PHENYL-ALKANOL DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 有权
    • 2-AMINO-2-PHENYL-ALKANOL DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    • 2-氨基-2-苯基 - 烷基醇衍生物，其制备方法和含有其的药物组合物
    • US20120129909A1
    • 2012-05-24
    • US13387462
    • 2010-07-28
    • Jean Pachot , Christophe Dini
    • Jean Pachot , Christophe Dini
    • A61K31/40 , A61P25/04 , C07D207/08
    • C07D207/08 , C07D205/04 , C07D211/22 , C07D223/04
    • Ester derivatives of 2-amino-2-phenyl-alkanol of general formula (I) in which: R1 forms with R3 and the nitrogen and carbon atoms to which they are respectively attached, a heterocycle with 4 to 7 members, optionally substituted in the α position of the nitrogen atom by one or two Ra and Rb radicals being able to be independently of one another hydrogen or linear or branched alkyl (1 to 4C), and R2 is H or a —CO—O—CHR4—OCOR5 radical for which R4 is H or linear or branched alkyl (1 to 4C), and R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by the remainder of an amino acid, or represents a heterocycle, or R2 is linear or branched alkyl (1 to 4C), alkyl (2 to 4C) substituted by OH, alkoxy, alkylthio, NH2, alkylamino, dialkylamino optionally forming with the nitrogen atom to which they are attached, a heterocycle with 5 or 6 members, it being understood that the substituted alkyl radical is linear or branched and comprises at least 2C between >N—R2 and the substituent, unless specified otherwise, alkyl or acyl are linear or branched (1 to 7C), in their R or S forms or their mixtures, as well as its pharmaceutically acceptable salts, if any.
    • 通式（I）的2-氨基-2-苯基 - 链烷醇的酯衍生物，其中：R 1与R 3及其分别连接的氮和碳原子一起形成具有4至7个成员的杂环，任选在 一个或两个R a和R b基团的氮原子的α位置能够彼此独立地为氢或直链或支链烷基（1-4C），R2为H或-CO-O-CHR4-OCOR5基团，用于 其中R 4为H或直链或支链烷基（1至4C），R 5为任选被苄氧基羰基氨基，酰氨基或氨基酸残基取代的烷基，或表示杂环，或R 2为直链或支链烷基 ），被OH，烷氧基，烷硫基，NH 2，烷基氨基，任选与其连接的氮原子形成的二烷基氨基，具有5或6个成员的杂环取代的（2至4C）烷基，应理解的是取代的烷基是 线性或分支，并且在> N-R2 a之间包含至少2C 除非另有说明，否则烷基或酰基以其R或S形式或其混合物以及其药学上可接受的盐（如果有的话）是直链或支链的（1至7C）。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 2. 发明授权
      US08217075B2 2-amino-2-phenyl-alkanol derivatives, their preparation and pharmaceutical compositions containing them 有权
    • 2-amino-2-phenyl-alkanol derivatives, their preparation and pharmaceutical compositions containing them
    • 2-氨基-2-苯基 - 链烷醇衍生物，其制备方法和含有它们的药物组合物
    • US08217075B2
    • 2012-07-10
    • US12360306
    • 2009-01-27
    • Jean Pachot , Christophe Dini , Alexis Denis
    • Jean Pachot , Christophe Dini , Alexis Denis
    • A61K31/27 , A61K31/235 , A61K31/24 , C07C261/00 , C07C69/00
    • C07C271/16 , A61K9/2054 , C07C219/22 , C07C271/22 , C07C271/48 , C07C333/04 , C07D213/80 , C07D213/82 , C07D317/40
    • 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.
    • 通式（I）的2-氨基-2-苯基 - 链烷醇酯衍生物，其中：R 1为H，直链或支链1至4C烷基，被OH，烷氧基，烷硫基，酰氧基，NH 2取代的直链或支链2至4C烷基 ，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，R2是-CO-R基团，其中R是H，烷基，芳基，杂环基，苄基或杂环基甲基，或R2是-CO-Y-R4基团， Y是-O - ， - S - ， - NH - ， - 烷基，其中alk是直链或支链（1-4C）烷基，R4是烷基，芳基，芳烷基或杂环基烷基，能够被一个或多个 卤原子或OH基团，直链或支链（1-4C）烷基，烷氧基，烷硫基，酰氨基烷硫基，烷氧基羰基或酰基氨基（1至4C）直链或支链或氧代，或能够被R5COO-取代，其中R5是烷基 任选地被苄氧羰基氨基，酰氨基或氨基酸残基取代，或表示杂环基， 或R 2是被OH，烷氧基，烷硫基，酰氧基，NH 2，烷基氨基，任选地与它们所连接的氮原子形成的二烷基氨基取代的任选具有另一个杂原子的5或6元杂环的（2至4C） 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，应理解所述直链或支链取代的烷基在> N-R2和取代基之间至少包含2C; 并且R 3是直链或支链烷基（1-4C），除非特别提及，烷基或酰基以R或S形式或其混合物为直链或支链（1至7C），以及它们的药学上可接受的盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 4. 发明申请
      US20090197924A1 2-AMINO-2-PHENYL-ALKANOL DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权
    • 2-AMINO-2-PHENYL-ALKANOL DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    • 2-氨基-2-苯基 - 烷基醇衍生物，其制备和含有它们的药物组合物
    • US20090197924A1
    • 2009-08-06
    • US12360306
    • 2009-01-27
    • Jean Pachot , Christophe Dini , Alexis Denis
    • Jean Pachot , Christophe Dini , Alexis Denis
    • A61K31/24 , C07D213/56 , C07C271/22 , C07D317/34 , C07C333/04 , C07D213/80 , A61K31/4406 , A61K31/27 , A61K31/357 , A61P25/04
    • C07C271/16 , A61K9/2054 , C07C219/22 , C07C271/22 , C07C271/48 , C07C333/04 , C07D213/80 , C07D213/82 , C07D317/40
    • 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.
    • 通式（I）的2-氨基-2-苯基 - 链烷醇酯衍生物，其中：R 1为H，直链或支链1至4C烷基，被OH，烷氧基，烷硫基，酰氧基，NH 2取代的直链或支链2至4C烷基 ，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，R2是-CO-R基团，其中R是H，烷基，芳基，杂环基，苄基或杂环基甲基，或R2是-CO-Y-R4基团， Y是-O - ， - S - ， - NH - ， - 烷基，其中alk是直链或支链（1-4C）烷基，R4是烷基，芳基，芳烷基或杂环基烷基，能够被一个或多个 卤原子或OH基团，直链或支链（1-4C）烷基，烷氧基，烷硫基，酰氨基烷硫基，烷氧基羰基或酰基氨基（1至4C）直链或支链或氧代，或能够被R5COO-取代，其中R5是烷基 任选地被苄氧羰基氨基，酰氨基或氨基酸残基取代，或表示杂环基，或R 2是烷基（2至4 ）被OH，烷氧基，烷硫基，酰氧基，NH 2，烷基氨基，任选地与它们所连接的氮原子形成的二烷基氨基取代，任选地具有另一个杂原子（O或N）的5或6元杂环，或被 烷基氨基甲酰氧基，烷氧基羰基氨基，脲基或烷基脲基，应理解所述直链或支链取代的烷基在> N-R2和取代基之间至少包含2C; 并且R 3是直链或支链烷基（1-4C），除非特别提及，烷基或酰基以R或S形式或其混合物为直链或支链（1至7C），以及它们的药学上可接受的盐。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 5. 发明授权
      US08436192B2 2-amino-2-phenyl-alkanol derivatives, preparation thereof, and pharmaceutical compositions containing same 有权
    • 2-amino-2-phenyl-alkanol derivatives, preparation thereof, and pharmaceutical compositions containing same
    • 2-氨基-2-苯基 - 链烷醇衍生物，其制备方法和含有它们的药物组合物
    • US08436192B2
    • 2013-05-07
    • US13387462
    • 2010-07-28
    • Jean Pachot , Christophe Dini
    • Jean Pachot , Christophe Dini
    • C07D207/02 , A61K31/40
    • C07D207/08 , C07D205/04 , C07D211/22 , C07D223/04
    • Ester derivatives of 2-amino-2-phenyl-alkanol of general formula (I) in which: R1 forms with R3 and the nitrogen and carbon atoms to which they are respectively attached, a heterocycle with 4 to 7 members, optionally substituted in the α position of the nitrogen atom by one or two Ra and Rb radicals being able to be independently of one another hydrogen or linear or branched alkyl (1 to 4C), and R2 is H or a —CO—O—CHR4—OCOR5 radical for which R4 is H or linear or branched alkyl (1 to 4C), and R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by the remainder of an amino acid, or represents a heterocycle, or R2 is linear or branched alkyl (1 to 4C), alkyl (2 to 4C) substituted by OH, alkoxy, alkylthio, NH2, alkylamino, dialkylamino optionally forming with the nitrogen atom to which they are attached, a heterocycle with 5 or 6 members, it being understood that the substituted alkyl radical is linear or branched and comprises at least 2C between >N—R2 and the substituent, unless specified otherwise, alkyl or acyl are linear or branched (1 to 7C), in their R or S forms or their mixtures, as well as its pharmaceutically acceptable salts, if any.
    • 通式（I）的2-氨基-2-苯基 - 链烷醇的酯衍生物，其中：R 1与R 3及其分别连接的氮和碳原子一起形成具有4至7个成员的杂环，任选在 一个或两个Ra和Rb基团的氮原子的α位置能够彼此独立地为氢或直链或支链烷基（1-4C），R2为H或-CO-O-CHR4-OCOR5基团，用于 其中R 4为H或直链或支链烷基（1至4C），R 5为任选被苄氧基羰基氨基，酰氨基或氨基酸残基取代的烷基，或表示杂环，或R 2为直链或支链烷基 ），被OH，烷氧基，烷硫基，NH 2，烷基氨基，任选与其连接的氮原子形成的二烷基氨基，具有5或6个成员的杂环取代的（2至4C）烷基，应理解的是取代的烷基是 线性或分支的，并且在> N-R2和...之间包含至少2C 取代基，除非另有说明，烷基或酰基以其R或S形式或其混合物以及其药学上可接受的盐（如果有的话）是直链或支链的（1至7C）。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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