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    2-AMINO-2-PHENYL-ALKANOL DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    31.
    发明申请
    2-AMINO-2-PHENYL-ALKANOL DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权
    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

    公开(公告)号：US20090197924A1

    公开(公告)日：2009-08-06

    申请号：US12360306

    申请日：2009-01-27

    申请人： Jean Pachot ,  Christophe Dini ,  Alexis Denis

    发明人： Jean Pachot ,  Christophe Dini ,  Alexis Denis

    IPC分类号： A61K31/24 ,  C07D213/56 ,  C07C271/22 ,  C07D317/34 ,  C07C333/04 ,  C07D213/80 ,  A61K31/4406 ,  A61K31/27 ,  A61K31/357 ,  A61P25/04

    CPC分类号： C07C271/16 ,  A61K9/2054 ,  C07C219/22 ,  C07C271/22 ,  C07C271/48 ,  C07C333/04 ,  C07D213/80 ,  C07D213/82 ,  C07D317/40

    摘要： 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.

    摘要翻译： 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。

    6-deoxy erythromycin derivatives, method for preparing same and use as medicines
    34.
    发明授权
    6-deoxy erythromycin derivatives, method for preparing same and use as medicines 有权
    6-脱氧红霉素衍生物，其制备方法，用作药物

    公开(公告)号：US06706692B1

    公开(公告)日：2004-03-16

    申请号：US09744320

    申请日：2001-04-10

    申请人： Jean-Michel Auger ,  Alexis Denis

    发明人： Jean-Michel Auger ,  Alexis Denis

    IPC分类号： A61K3170

    CPC分类号： C07H17/08

    摘要： The invention concerns compounds of formula (I) wherein: X represents a (NH)a, CH2 or SO2 radical or an oxygen atom; a represents 0 or 1; Y represents a (CH2)m-(CH═CH)n-(CH2)o radical with m+n+o≦8, n=0 or 1; Ar represents an aryl or heteroaryl radical, optionally substituted; W represents a hydrogen atom or a halogen atom; Z represents a hydrogen atom or an acid residue, and their addition salts with acids. The compounds of formula (I) have antibiotic properties

    摘要翻译： 本发明涉及式（I）的化合物，其中：X表示（NH）a，CH 2或SO 2基团或氧原子; a表示0或1; Y表示具有m + n + o = 8，n = 0或1的（CH = CH）n - （CH 2） Ar表示任选取代的芳基或杂芳基; W表示氢原子或卤素原子; Z表示氢原子或酸残基，它们与酸的加成盐。 式（I）化合物具有抗生素特性

    Derivatives of erythromycin, their preparation process and their use as medicaments
    36.
    发明授权
    Derivatives of erythromycin, their preparation process and their use as medicaments 有权
    红霉素的衍生物，其制备方法及其作为药物的用途

    公开(公告)号：US06440941B1

    公开(公告)日：2002-08-27

    申请号：US09442681

    申请日：1999-11-18

    申请人： Alexis Denis

    发明人： Alexis Denis

    IPC分类号： A61K3170

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07H17/08

    摘要： A subject of the invention is the compounds of formula (I) in which Y represents a hydrogen atom or a fluorine atom, n represents an integer comprised between 1 and 8, Z represents a hydrogen atom or the remainder of a carboxylic acid, optionally substituted on the heterocycle by one or more alkyl, alkenyl, alkynyl, O-alkyl, O-alkenyl, O-alkynyl, S-alkyl, S-alkenyl, S-alkynyl radicals containing up to 8 carbon atoms, one or more OH, NH2, C═N, NO2, CF3 radicals or one or more aryl radicals containing up to 14 carbon atoms or heteroaryl radicals containing one or more nitrogen oxygen or sulphur atoms, the aryl or heteroaryl radicals themselves being able to be substituted as well as their addition salts with acids, The products of formula (I) have antibiotic properties.

    摘要翻译： 本发明的主题是式（I）的化合物，其中Y代表氢原子或氟原子，n表示1至8之间的整数，Z表示氢原子或羧酸的其余部分，任选在 通过一个或多个烷基，烯基，炔基，O-烷基，O-链烯基，O-炔基，S-烷基，S-烯基，含有至多8个碳原子的S-炔基，一个或多个OH，NH 2， C = N，NO 2，CF 3基团或含有至多14个碳原子的一个或多个芳基或含有一个或多个氮氧原子或硫原子的杂芳基，芳基或杂芳基自身能够被取代，以及它们的加成盐 与酸，式（I）的产物具有抗生素特性。

    Erythromycin derivatives, a process for their preparation and their use as medicaments
    37.
    发明授权
    Erythromycin derivatives, a process for their preparation and their use as medicaments 有权
    红霉素衍生物，其制备方法及其用作药物

    公开(公告)号：US06433151B1

    公开(公告)日：2002-08-13

    申请号：US09350224

    申请日：1999-07-08

    申请人： Alexis Denis ,  Giuseppe Gigliotti

    发明人： Alexis Denis ,  Giuseppe Gigliotti

    IPC分类号： C07H1708

    CPC分类号： C07H17/08

    摘要： The invention relates to compounds of the formula (I) in which R represents a radical (CH2)mOn(X)YAr  in which m represents the number 0 or 1, n represents the number 0 or 1, X represents a radical (NH)a, CH2 or SO2, where a represents the number 0 or 1, Y represents a radical (CH2)b—(CH═CH)c—(CH2)d, where c=0 or 1 and b+c+d ≦8, Z represents a hydrogen or halogen atom, Ar represents an optionally substituted aryl or heteroaryl radical and W represents a hydrogen atom or an acyl radical, and their acid addition salts. The compounds of the formula (1) have antibiotic properties.

    摘要翻译： 本发明涉及式（I）化合物，其中R表示基团，其中m表示数字0或1，n表示数字0或1，X表示基团（NH）a，CH 2或SO 2，其中a表示 数字0或1，Y表示基团（CH 2）b - （CH = CH）c - （CH 2）d，其中c = 0或1，b + c + d <= 8，Z表示氢或卤素原子 ，Ar表示任选取代的芳基或杂芳基，W表示氢原子或酰基，以及它们的酸加成盐。式（1）化合物具有抗生素特性。