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    ESTERIFIED CELLULOSE ETHERS HAVING A SPECIFIC SUBSTITUENT DISTRIBUTION
    1.
    发明申请
    ESTERIFIED CELLULOSE ETHERS HAVING A SPECIFIC SUBSTITUENT DISTRIBUTION 有权
    具有特殊取代分布的蛋白质酯

    公开(公告)号：US20150065547A1

    公开(公告)日：2015-03-05

    申请号：US14390041

    申请日：2012-10-24

    申请人： Dow Global Technologies LLC

    发明人： Robert L. Schmitt ,  Robert L. Sammler ,  Meinolf Brackhagen ,  Oliver Petermann ,  Roland Adden ,  Nicholas S. Grasman ,  Steven J. Guillaudeu

    IPC分类号： A61K47/38 ,  A61K47/10 ,  A61K9/48 ,  A61K31/4166 ,  A61K9/14 ,  C08B13/00 ,  A61K31/343

    CPC分类号： A61K47/38 ,  A61K9/08 ,  A61K9/145 ,  A61K9/146 ,  A61K9/4816 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/343 ,  A61K31/4166 ,  A61K47/10 ,  C08B11/193 ,  C08B13/00

    摘要： An esterified cellulose ether comprises (i) aliphatic monovalent acyl groups or (ii) groups of the formula —C(O)—R—COOA wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation or (iii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein the cellulose ether has anhydroglucose units joined by 1-4 linkages and has methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl as substituents such that the esterified cellulose ether has an MS (hydroxyalkyl) of 0.05 to 1.00, and hydroxyl groups of anhydroglucose units are substituted with methyl groups such that [s23/s26−0.2*MS(hydroxyalkyl)] is 0.36 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 3-positions of the anhydroglucose unit are substituted with a methyl group and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 6-positions of the anhydroglucose unit are substituted with a methyl group. The esterified cellulose ether is useful as an excipient for poorly water-soluble drugs.

    摘要翻译： 酯化的纤维素醚包括（i）脂族一价酰基或（ii）式-C（O）-R-COOA的基团，其中R是二价脂族或芳族烃基，A是氢或阳离子或（iii） 脂族一价酰基和式-C（O）-R-COOA基团的组合，其中纤维素醚具有通过1-4键连接并具有甲基，羟基烷基和任选的烷基的脱水葡萄糖单元， 甲基作为取代基使得酯化纤维素醚具有0.05至1.00的MS（羟烷基），脱水葡萄糖单元的羟基被甲基取代，使得[s23 / s26-0.2 * MS（羟烷基）]为0.36以下， 其中s23是脱水葡萄糖单元的摩尔分数，其中只有脱水葡萄糖单元的2-和3-位上的两个羟基被甲基取代，其中s26是脱水葡萄糖单元的摩尔分数，其中仅th 脱水葡萄糖单元的2-和6-位上的两个羟基被甲基取代。 酯化纤维素醚可用作水溶性差的药物的赋形剂。

    COMPOSITION COMPRISING AN ORGANIC LIQUID DILUENT AND A SPECIFIC HYDROXYPROPYL METHYLCELLULOSE
    2.
    发明申请
    COMPOSITION COMPRISING AN ORGANIC LIQUID DILUENT AND A SPECIFIC HYDROXYPROPYL METHYLCELLULOSE 审中-公开
    包含有机液体稀释剂和特定的羟丙基甲基纤维素的组合物

    公开(公告)号：US20140024723A1

    公开(公告)日：2014-01-23

    申请号：US13942775

    申请日：2013-07-16

    申请人： Dow Global Technologies LLC

    发明人： Meinolf Brackhagen ,  Robert L. Schmitt ,  Matthias Knarr

    IPC分类号： A61K47/38

    CPC分类号： A61K47/38 ,  A61K9/146 ,  A61K9/2866 ,  A61K9/5047 ,  A61K9/5089

    摘要： A liquid composition which comprises an organic liquid diluent and at least one hydroxypropyl methylcellulose having 28 to 30 weight percent of methoxyl groups, 7 to 12 weight percent of hydroxypropoxyl groups and a sum of methoxyl groups and hydroxypropoxyl groups of from 38.5 to 42 weight percent is stable over an extended time period.The liquid composition is useful for preparing a solid dispersion comprising at least one active ingredient in at least one hydroxypropyl methylcellulose by spray-drying.Alternatively a solid dispersion can be produced by blending and extruding at least one active ingredient, at least one hydroxypropyl methylcellulose described above and optionally one or more adjuvants.

    摘要翻译： 一种液体组合物，其包含有机液体稀释剂和至少一种羟甲基纤维素，其具有甲氧基28-30重量％，羟丙氧基7-12重量％，甲氧基和羟丙氧基之和为38.5至42重量％ 在延长的时间内稳定。 液体组合物可用于通过喷雾干燥制备包含至少一种羟丙基甲基纤维素中的至少一种活性成分的固体分散体。 或者，可以通过共混和挤出至少一种活性成分，至少一种上述羟丙基甲基纤维素和任选的一种或多种佐剂来制备固体分散体。

    Esterified cellulose ethers having a specific substituent distribution
    3.
    发明授权
    Esterified cellulose ethers having a specific substituent distribution 有权
    具有特定取代基分布的酯化纤维素醚

    公开(公告)号：US09320799B2

    公开(公告)日：2016-04-26

    申请号：US14390041

    申请日：2012-10-24

    申请人： Dow Global Technologies LLC

    发明人： Robert L. Schmitt ,  Robert L. Sammler ,  Meinolf Brackhagen ,  Oliver Petermann ,  Roland Adden ,  Nicholas S. Grasman ,  Steven J. Guillaudeu

    IPC分类号： A61K31/343 ,  A61K31/4166 ,  A61K47/10 ,  A61K47/38 ,  A61K9/14 ,  A61K9/48 ,  C08B13/00 ,  C08B11/193 ,  A61K9/08

    CPC分类号： A61K47/38 ,  A61K9/08 ,  A61K9/145 ,  A61K9/146 ,  A61K9/4816 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/343 ,  A61K31/4166 ,  A61K47/10 ,  C08B11/193 ,  C08B13/00

    摘要： An esterified cellulose ether comprises (i) aliphatic monovalent acyl groups or (ii) groups of the formula —C(O)—R—COOA wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation or (iii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein the cellulose ether has anhydroglucose units joined by 1-4 linkages and has methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl as substituents such that the esterified cellulose ether has an MS (hydroxyalkyl) of 0.05 to 1.00, and hydroxyl groups of anhydroglucose units are substituted with methyl groups such that [s23/s26−0.2*MS(hydroxyalkyl)] is 0.36 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 3-positions of the anhydroglucose unit are substituted with a methyl group and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 6-positions of the anhydroglucose unit are substituted with a methyl group. The esterified cellulose ether is useful as an excipient for poorly water-soluble drugs.

    摘要翻译： 酯化的纤维素醚包括（i）脂族一价酰基或（ii）式-C（O）-R-COOA的基团，其中R是二价脂族或芳族烃基，A是氢或阳离子或（iii） 脂族一价酰基和式-C（O）-R-COOA基团的组合，其中纤维素醚具有通过1-4键连接并具有甲基，羟基烷基和任选的烷基的脱水葡萄糖单元， 甲基作为取代基使得酯化纤维素醚具有0.05至1.00的MS（羟烷基），脱水葡萄糖单元的羟基被甲基取代，使得[s23 / s26-0.2 * MS（羟烷基）]为0.36以下， 其中s23是脱水葡萄糖单元的摩尔分数，其中只有脱水葡萄糖单元的2-和3-位上的两个羟基被甲基取代，其中s26是脱水葡萄糖单元的摩尔分数，其中仅th 脱水葡萄糖单元的2-和6-位上的两个羟基被甲基取代。 酯化纤维素醚可用作水溶性差的药物的赋形剂。

    PROCESS FOR PREPARING AN ESTER OF A CELLULOSE ETHER IN THE PRESENCE OF AN ALIPHATIC CARBOXYLIC ACID
    4.
    发明申请
    PROCESS FOR PREPARING AN ESTER OF A CELLULOSE ETHER IN THE PRESENCE OF AN ALIPHATIC CARBOXYLIC ACID 审中-公开
    制备纤维素醚的方法在存在一种二羧酸的情况下

    公开(公告)号：US20150218197A1

    公开(公告)日：2015-08-06

    申请号：US14420921

    申请日：2013-08-15

    申请人： DOW GLOBAL TECHNOLOGIES LLC

    发明人： Oliver Petermann ,  Matthias Sprehe ,  Robert L. Schmitt ,  Andrew C. Arthur ,  Warren K. Miller ,  David K. Lyon

    IPC分类号： C07H3/06

    CPC分类号： C07H3/06 ,  C08B11/20 ,  C08B13/00

    摘要： Two or more esters of a cellulose ether, each having the same ether and ester substituents but different weight average molecular weights are prepared in a process which comprises the steps of esterifying a cellulose ether with (i) an aliphatic monocarboxylic acid anhydride or (ii) a dicarboxylic acid anhydride or (iii) a combination of an aliphatic monocarboxylic acid anhydride and a dicarboxylic acid anhydride in the presence of an aliphatic carboxylic acid as a reaction diluent in two or more separate reactions, wherein in each reaction a different molar ratio [aliphatic carboxylic acid/anhydroglucose units of cellulose ether] is used to produce esters of the cellulose ether of different weight average molecular weights.

    摘要翻译： 在包括以下步骤的方法中制备两种或更多种纤维素醚的酯，它们各自具有相同的醚和酯取代基但不同的重均分子量，该方法包括以下步骤：（i）脂肪族单羧酸酐或（ii） 二羧酸酐或（iii）脂肪族单羧酸酐和二羧酸酐在脂肪族羧酸作为反应稀释剂的存在下在两个或更多个分开的反应中的组合，其中在每个反应中不同的摩尔比[脂族 纤维素醚的羧酸/脱水葡萄糖单元]用于生产不同重均分子量的纤维素醚的酯。

    CELLULOSE ETHERS ESTERIFIED WITH DICARBOXYLIC ACID
    7.
    发明申请
    CELLULOSE ETHERS ESTERIFIED WITH DICARBOXYLIC ACID 有权
    用二羧酸测定的纤维素

    公开(公告)号：US20160289344A1

    公开(公告)日：2016-10-06

    申请号：US14777838

    申请日：2014-05-07

    申请人： DOW GLOBAL TECHNOLOGIES LLC ,  REGENTS OF THE UNIVERSITY OF MINNESOTA

    发明人： Ligeng Yin ,  Marc A. Hillmyer ,  Steven J. Guillaudeu ,  Robert L. Schmitt

    IPC分类号： C08B13/00 ,  A61K31/4166 ,  A61K31/095 ,  A61K47/38

    CPC分类号： C08B13/00 ,  A61K9/146 ,  A61K31/095 ,  A61K31/4166 ,  A61K47/38

    摘要： Esterified cellulose ethers comprising groups of formula —C(O)—CHR′—CHR″—COOA, wherein, R′ and R″ are hydrogen or (—S)m (—R1)n-R2, wherein R1 is a hydrocarbon group having 1 to 4 carbon atoms, R2 is an optionally substituted 5- or 6-membered cyclic group, m and n each independently are 0 or 1, and A is hydrogen or a cation, with the proviso that in each group CHR′—CHR″ one of R′ and R″ is hydrogen and the other one is (—S)m (—R1)n-R′, are useful as excipients for maintaining the concentration of poorly water-soluble drugs in aqueous liquids at supersaturation levels.

    摘要翻译： 包含式-C（O）-CHR'-CHR“-COOA基团的酯化纤维素醚，其中R'和R”是氢或（-S）m（-R1）n -R2，其中R1是烃基 具有1至4个碳原子，R 2是任选取代的5或6元环基，m和n各自独立地是0或1，A是氢或阳离子，条件是在CHR'-CHR “R”和R“之一是氢，另一个是（-S）m（-R1）nR'，可用作在过饱和水平下维持水溶液中难溶于水的药物浓度的赋形剂。