公开(公告)号：US20030138847A1

公开(公告)日：2003-07-24

申请号：US10245839

申请日：2002-09-16

Applicant: H. Lundbeck A/S

Inventor： Thomas Ruhland ,  Per Holm ,  Kirsten Schultz ,  Jannie Egeskov Holm ,  Kim Andersen

IPC: G01N033/53 ,  C08G063/91 ,  G01N033/543 ,  C08G063/48

CPC classification number: C07K1/042 ,  B01J19/0046 ,  B01J2219/00351 ,  B01J2219/00459 ,  B01J2219/00497 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00592 ,  B01J2219/0072 ,  C07B2200/11 ,  C40B60/14

Abstract: A dosing form for a polymer support for organic chemical synthesis in a solvent medium comprising a fixed weight amount of beads of a polymer containing functional groups, which polymer is insoluble in the solvent for the intended synthesis, is provided as compressed tablets of essentially equal weight and composition wherein the polymer beads are essentially intact and are released as such when the tablets are disintegrated in said solvent. Use of the dosing form is made in conventional synthesis, in parallel synthesis, in split and mix synthesis and/or combinatorial chemistry. In a method for producing the dosing form, beads of a polymer having functional gropusgroups is compressed into tablets after pre-treatment with an aprotic organic solvent groups are compressed into tablets after pre-treatment with an aprotic organic solvent.

Abstract translation: 提供用于溶剂介质中有机化学合成的聚合物载体的剂型，其包含固定重量的含有官能团的聚合物珠，该聚合物不溶于用于预期合成的溶剂中，作为基本相等重量的压片 和组合物，其中当片剂在所述溶剂中崩解时，聚合物珠基本上是完整的并且如此释放。 在分批和混合合成和/或组合化学中，在常规合成，并行合成中使用配料形式。 在制备给药形式的方法中，具有功能性组蛋白的聚合物的珠粒在用非质子有机溶剂基团预处理后被压缩成片剂，在用非质子有机溶剂预处理后被压缩成片剂。

公开(公告)号：US20030138376A1

公开(公告)日：2003-07-24

申请号：US10245836

申请日：2002-09-16

Applicant: H. Lundbeck A/S

Inventor： Thomas Ruhland ,  Per Holm ,  Kirsten Schultz ,  Jannie Egeskov Holm ,  Kim Andersen

IPC: A61K049/00 ,  G01N033/543

CPC classification number: C07K1/023 ,  B01J4/02 ,  B01J19/0046 ,  B01J2219/00351 ,  B01J2219/00459 ,  B01J2219/00497 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00592 ,  C07K1/04 ,  C07K1/1077 ,  C40B60/14

Abstract: A dosing form for at least one solid reagent for use in conventional organic and inorganic synthesis, in parallel synthesis, and in split and mix synthesis in combinatorial chemistry is provided as compressed tablets each containing the same predetermined amount of said at least one reagent embedded in a polymer matrix comprising beads of a polymer insoluble in the solvents for the intended synthesis, which tablets are capable of disintegrating in said solvent for release of the at least one reagent and disperse the matrix as polymer beads into the solvent. The polymer beads forming the matrix and the reagents of the dosing form can easily be removed by filtration in order to separate these from a formed soluble product. In a method for producing the dosing form, beads of one or more polymers are mixed with the reagents and compressed into tablets after pre-treatment with an aprotic organic solvent.

Abstract translation: 提供用于常规有机和无机合成，并行合成和组合化学中的分离和混合合成中的至少一种固体试剂的给药形式，其为包含相同预定量的所述至少一种试剂 聚合物基质，其包含不溶于用于预期合成的溶剂中的聚合物的珠粒，该片剂能够在所述溶剂中分解以释放至少一种试剂并将基质作为聚合物珠分散到溶剂中。 形成基质的聚合物珠粒和剂型的试剂可以通过过滤容易地除去，以将它们与形成的可溶性产物分离。 在制备给药形式的方法中，将一种或多种聚合物的珠粒与试剂混合，并用非质子有机溶剂预处理后压制成片剂。