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    Controlled functional density polyamines and method for preparation thereof
    21.
    发明授权
    Controlled functional density polyamines and method for preparation thereof 失效
    受控功能密度多胺及其制备方法

    公开(公告)号：US5559193A

    公开(公告)日：1996-09-24

    申请号：US169236

    申请日：1993-12-20

    申请人： Martin P. McGrath ,  Samuel J. Tremont

    发明人： Martin P. McGrath ,  Samuel J. Tremont

    IPC分类号： C08F8/04 ,  C08F8/32 ,  C08F26/00 ,  C08F290/00 ,  C08F299/00 ,  C08F2/00 ,  C08F8/00

    CPC分类号： C08F8/32 ,  C08F8/04

    摘要： A process for preparing a polyamine containing a controlled amount of pendant tertiary amine groups and a controlled amount of pendant secondary amine or different tertiary amine groups and reactive carbon-carbon double bonds comprising reductively animating essentially all aldehyde groups in a polyaldehyde containing a controlled amount of pendant aldehyde groups and reactive carbon-carbon double bonds with a first secondary amine to produce a poly(tertiary amine), hydroformylating the poly(tertiary amine) having a controlled amount of pendant aldehyde groups, and reductively aminating the poly(tertiary amine) with pendant aldehyde groups with a primary amine or a second secondary amine. In another embodiment for preparing the polyamines of the invention, the polyaldehyde is reductively aminated with an amount of a first secondary amine to reductively aminate a controlled amount of the aldehyde groups and further reductively aminated with a primary amine or a second secondary amine to reductively aminate essentially all the remaining aldehyde groups.

    摘要翻译： 一种制备含有受控量的叔胺胺基的多胺和受控量的仲胺或不同叔胺基团和反应性碳 - 碳双键的多胺的方法，其包括在含有受控量的 侧链醛基和反应性碳 - 碳双键与第一仲胺反应以产生聚（叔胺），加氢甲酰化具有受控量的侧基醛基团的聚（叔胺），并还原胺化聚（叔胺）与 侧链醛基与伯胺或第二仲胺。 在制备本发明的多胺的另一个实施方案中，多醛用一定量的第一仲胺还原胺化以还原胺化受控量的醛基并进一步用伯胺或第二仲胺进行还原胺化以还原性胺化 基本上所有剩余的醛基。

    Dehydrocoupling of toluene
    24.
    发明授权
    Dehydrocoupling of toluene 失效
    甲苯脱氢耦合

    公开(公告)号：US4278826A

    公开(公告)日：1981-07-14

    申请号：US101944

    申请日：1979-12-10

    申请人： Samuel J. Tremont ,  Alex N. Williamson ,  Arthur J. Solodar

    发明人： Samuel J. Tremont ,  Alex N. Williamson ,  Arthur J. Solodar

    IPC分类号： C07C2/84 ,  C07C2/72

    CPC分类号： C07C2/84 ,  C07C2523/14 ,  C07C2523/18

    摘要： Toluene dehydrocoupled products are produced by heating toluene in the vapor phase with an inorganic metal/oxygen composition which functions as an oxygen carrier and has the empirical formula:M.sub.a.sup.1 M.sub.b.sup.2 M.sub.c.sup.3 O.sub.xwhere M.sup.1 is lead, M.sup.2 is antimony, and M.sup.3 is at least one element selected from silver, zinc, gallium, arsenic, the lanthanides or rare earths, Groups 1a, 2a, 3b, 4b, and 8 of the Periodic Table of the Elements, and mixtures thereof, and wherein a is 1, b is 0.01 to 10, c is 0.01 to 10, and x is a number taken to satisfy the average valences of M.sup.1, M.sup.2, and M.sup.3 in the oxidation states in which they exist in the composition. Alternatively, the same inorganic metal/oxygen composition can be employed as a catalyst or as a combination catalyst/oxygen carrier for the dehydrocoupling reaction when oxygen or an oxygen-containing gas is heated with the toluene.

    摘要翻译： 甲苯脱氢耦合产物是通过用作为氧载体的无机金属/氧组合物在气相中加热甲苯来制备的，具有以下经验式：其中M1为铅，M2为锑的Ma1Mb2Mc3Ox，M3为选自以下的至少一种元素： 银，锌，镓，砷，镧系元素或稀土元素周期表第1a，2a，3b，4b和8族及其混合物，其中a为1，b为0.01至10，c 为0.01〜10，x为满足组成中存在的氧化态的M1，M2，M3的平均化合价的数。 或者，当氧气或含氧气体与甲苯一起加热时，可以使用相同的无机金属/氧组合物作为催化剂或用作脱氢耦合反应的组合催化剂/氧载体。

    Ph-selective delivery system using crosslinked polymeric resins as vehicles
    26.
    发明授权
    Ph-selective delivery system using crosslinked polymeric resins as vehicles 失效
    使用交联聚合物树脂作为载体的选择性递送系统

    公开(公告)号：US06471955B1

    公开(公告)日：2002-10-29

    申请号：US09050042

    申请日：1998-03-30

    申请人： Samuel J. Tremont ,  Denis Forster ,  Ricky L. Fenton ,  Yinong Ma

    发明人： Samuel J. Tremont ,  Denis Forster ,  Ricky L. Fenton ,  Yinong Ma

    IPC分类号： A61K3175

    CPC分类号： A61K31/5575 ,  A61K47/58 ,  A61K47/6927 ,  Y10S514/926 ,  Y10S514/927

    摘要： This invention provides a method of preparing a polymeric delivery system for active ingredients having enhanced site specific release performance characteristics. The delivery system is formed either by attaching the active ingredient to a linker through an acid-sensitive covalent bond, then forming a covalent bond between the linker and a portion of the subunits of a crosslinked polystyrene polymer, or by attaching a linker to a portion of the subunits of a crosslinked polystyrene polymer, then attaching the active ingredient to the polymer-linker combination through an acid-sensitive covalent bond. The invention also provides a delivery system comprising an active ingredient covalently bonded through an acid-sensitive covalent bond to a linker, which is in turn covalently bonded to a portion of subunits of a crosslinked polystyrene polymer. The invention further provides a method for treatment or prevention of gastric ulcers using a delivery system capable of delivering prostaglandin or prostacyclin drugs, especially misoprostol.

    摘要翻译： 本发明提供了制备具有增强的位点特异性释放性能特征的活性成分的聚合物递送系统的方法。 递送系统通过将活性成分通过酸敏感共价键连接到接头上，然后在接头与交联聚苯乙烯聚合物的一部分亚单位之间形成共价键，或通过将接头连接到部分 的交联聚苯乙烯聚合物的亚基，然后通过酸敏感共价键将活性成分连接到聚合物 - 连接体组合。 本发明还提供了一种递送系统，其包含通过酸敏感共价键共价结合至接头的活性成分，其接触共价键合到交联聚苯乙烯聚合物的一部分亚单位。 本发明还提供了使用能够递送前列腺素或前列环素药物，特别是米索前列醇的递送系统来治疗或预防胃溃疡的方法。

    Gastro-specific prodrugs
    27.
    发明授权
    Gastro-specific prodrugs 失效
    胃特异性前药

    公开(公告)号：US06413945B1

    公开(公告)日：2002-07-02

    申请号：US09514819

    申请日：2000-02-28

    申请人： Samuel J. Tremont ,  Paul W. Collins ,  Ricky L. Fenton

    发明人： Samuel J. Tremont ,  Paul W. Collins ,  Ricky L. Fenton

    IPC分类号： C07F710

    CPC分类号： A61K47/60 ,  C07F7/1804

    摘要： A compound is disclosed havin the formula AW—SiR1R2R3 wherein R1 and R2 are independently alkyl, cycloalkyl, alkenyl, alkynyl, aryl, aralkyl, alkaryl, or a hydrophilic group; R3 is a hydrophilic group; and AW is the covalently bonded form of a drug AWH, wherein W is O, NH, S, or an enolate group. The hydrophilic group may be either non-neutral, or may be a polyol. This compound serves as a prodrug for the drug AWH. A method for preparing these compounds is also disclosed. Also disclosed is a method of treatment or prevention of gastric ulcers by administering the prodrug compounds.

    摘要翻译： 公开了化合物，其中R 1和R 2独立地为烷基，环烷基，烯基，炔基，芳基，芳烷基，烷芳基或亲水基团; R3是亲水基团; AW是药物AWH的共价键合形式，其中W是O，NH，S或烯醇化物基团。 亲水基团可以是非中性的，也可以是多元醇。 该化合物用作药物AWH的前药。 还公开了制备这些化合物的方法。 还公开了通过施用前药化合物治疗或预防胃溃疡的方法。

    Controlled functional density poly (secondary amines)
    29.
    发明授权
    Controlled functional density poly (secondary amines) 失效
    受控功能密度聚（仲胺）

    公开(公告)号：US5457155A

    公开(公告)日：1995-10-10

    申请号：US383045

    申请日：1995-02-03

    申请人： Martin P. McGrath ,  Samuel J. Tremont

    发明人： Martin P. McGrath ,  Samuel J. Tremont

    IPC分类号： C08C19/34 ,  C08F8/04 ,  C08F8/32 ,  C08K3/38

    CPC分类号： C08F8/04 ,  C08C19/34 ,  C08F8/32

    摘要： A process for preparing a controlled functional density poly(secondary amine) comprising: (a) contacting a polymer containing olefinic unsaturation with carbon monoxide in hydrogen under hydroformylation conditions in the presence of a hydroformylation catalyst to produce a controlled functional density polyaldehyde containing reactive carbon-carbon double bonds, and (b) contacting the polyaldehyde with hydrogen and a primary amine under reductive amination conditions in the presence of a ruthenium-containing imine hydrogenation catalyst or (b.sup.1) contacting the polyaldehyde with a sterically hindered aliphatic or cycloaliphatic primary amine or an aromatic primary amine under reductive amination conditions in the presence of an alkali metal borohydride to produce poly(secondary amine) having a substantially equivalent ratio of secondary amine groups to reactive carbon-carbon double bonds as the ratio of aldehyde groups to reactive carbon-carbon double bonds in the polyaldehyde.

    摘要翻译： 一种制备受控功能密度聚（仲胺）的方法，包括：（a）在加氢甲酰化条件下，在加氢甲酰化催化剂存在下，使含有烯属不饱和的聚合物与一氧化碳在氢气中接触，以产生受控的功能密度聚醛， 碳双键，和（b）在还原胺化条件下，在含钌亚胺氢化催化剂存在下使聚醛与伯胺接触，或（b1）使多醛与空间位阻的脂族或脂环族伯胺或 芳族伯胺在还原胺化条件下在碱金属硼氢化物存在下反应生成具有基本上当量的仲胺基与反应性碳 - 碳双键的比例的聚（仲胺）作为醛基与反应性碳 - 碳双重比例 多醛中的键。

    Controlled functional density poly(secondary amines)
    30.
    发明授权
    Controlled functional density poly(secondary amines) 失效
    受控功能密度聚（仲胺）

    公开(公告)号：US5434309A

    公开(公告)日：1995-07-18

    申请号：US234500

    申请日：1994-04-28

    申请人： Martin P. McGrath ,  Samuel J. Tremont

    发明人： Martin P. McGrath ,  Samuel J. Tremont

    IPC分类号： C08C19/34 ,  C08F8/04 ,  C08F8/32 ,  C07C209/26

    CPC分类号： C08F8/04 ,  C08C19/34 ,  C08F8/32

    摘要： A process for preparing a controlled functional density poly(secondary amine) comprising:(a) contacting a polymer containing olefinic unsaturation with carbon monoxide in hydrogen under hydroformylation conditions in the presence of a hydroformylation catalyst to produce a controlled functional density polyaldehyde containing reactive carbon-carbon double bonds, and (b) contacting the polyaldehyde with hydrogen and a primary amine under reductive amination conditions in the presence of a ruthenium-containing imine hydrogenation catalyst or (b.sup.1) contacting the polyaldehyde with a sterically hindered aliphatic or cycloaliphatic primary amine or an aromatic primary amine under reductive amination conditions in the presence of an alkali metal borohydride to produce poly(secondary amine) having a substantially equivalent ratio of secondary amine groups to reactive carbon-carbon double bonds as the ratio of aldehyde groups to reactive carbon-carbon double bonds in the polyaldehyde.

    摘要翻译： 一种制备受控功能密度聚（仲胺）的方法，包括：（a）在加氢甲酰化条件下，在加氢甲酰化催化剂存在下，使含有烯属不饱和的聚合物与一氧化碳在氢气中接触，以产生受控的功能密度聚醛， 碳双键，和（b）在还原胺化条件下，在含钌亚胺氢化催化剂存在下使聚醛与伯胺接触，或（b1）使多醛与空间位阻的脂族或脂环族伯胺或 芳族伯胺在还原胺化条件下在碱金属硼氢化物存在下反应生成具有基本上当量的仲胺基与反应性碳 - 碳双键的比例的聚（仲胺）作为醛基与反应性碳 - 碳双重比例 多醛中的键。