公开(公告)号：WO1992015551A1

公开(公告)日：1992-09-17

申请号：PCT/CA1992000090

申请日：1992-02-28

Applicant: UNIVERSITY OF SASKATCHEWAN ,  YU, Peter, H. ,  DAVIS, Bruce, A. ,  BOULTON, Alan, A.

Inventor： UNIVERSITY OF SASKATCHEWAN

IPC: C07C211/23

CPC classification number: C07C211/23 ,  C07C215/08 ,  C07C229/12

Abstract: The invention relates to a series of propargylamines, their salts and pharmaceutical compositions containing a compound of formula (III) wherein R1, R3 and R4 are the same or different and represent hydrogen or a straight chain or branched lower alkyl; y is an integer ranging from 0 to 5; z is an integer ranging from 0 to 5; and R2 is a straight chain or branched alkyl, alkenyl, alkynyl, alkoxy, alkylthio or alkyl sulphinyl group having from 3 to 11 carbon atoms, said group being unsubstituted or substituted with at least one of the substituents selected from hydroxy, aldehyde, oxo, loweracyloxy, halogen, thio, sulfoxide, sulfone, phenyl, halogen-substituted phenyl, hydroxy-substituted phenyl, cycloalkyl having from 3 to 6 carbon atoms and heterocyclic substituents having between 3 and 6 atoms, of which form 1 to 3 are heteroatoms selected from O, S and/or N, and pharmaceutically acceptable salts thereof, in admixture with a pharmaceutically acceptable carrier, excipient or adjuvant. The compounds are useful as selective monoamine oxidase B inhibitors and have demonstrated neuroprotective properties in human and veterinary medicine.

Abstract translation: 本发明涉及一系列含有式（III）化合物的炔丙胺，其盐和药物组合物，其中R 1，R 3和R 4相同或不同，表示氢或直链或支链的低级烷基; y为0〜5的整数; z为0〜5的整数; 并且R 2是具有3至11个碳原子的直链或支链烷基，烯基，炔基，烷氧基，烷硫基或烷基亚磺酰基，所述基团是未取代的或被至少一个选自羟基，醛，氧代， 低级酰氧基，卤素，硫代，亚砜，砜，苯基，卤素取代的苯基，羟基取代的苯基，具有3至6个碳原子的环烷基和3至6个原子的杂环取代基，其形成1至3个是选自 O，S和/或N及其药学上可接受的盐与药学上可接受的载体，赋形剂或佐剂混合。 该化合物可用作选择性单胺氧化酶B抑制剂，并且已经在人和兽医学中证明了神经保护性质。

公开(公告)号：WO1992013568A1

公开(公告)日：1992-08-20

申请号：PCT/CA1992000029

申请日：1992-01-29

Applicant: UNIVERSITY OF SASKATCHEWAN

Inventor： UNIVERSITY OF SASKATCHEWAN ,  REDMOND, Mark, J. ,  CAMPOS, Manuel

IPC: A61K47/42

CPC classification number: A61K9/5184 ,  A61K38/2013 ,  A61K38/217 ,  A61K47/6901 ,  C07K14/005 ,  C12N2710/14143 ,  C12N2720/12322

Abstract: Compositions and methods for preparing and delivering encapsulated biologically active agents to specific cell types are disclosed. Substances can be encapsulated in the VP6 inner capsid protein of rotavirus and delivered to selected cells, tissues and organs. Targeting agents can be linked to the surface of the VP6 sphere so that appropriate agents can be delivered to preselected cells and tissue types.

Abstract translation: 公开了用于制备和递送包封的生物活性剂到特定细胞类型的组合物和方法。 物质可以封装在轮状病毒的VP6内衣壳蛋白中，并被递送到选定的细胞，组织和器官。 靶向剂可以连接到VP6球体的表面，使得适当的药剂可以递送到预选的细胞和组织类型。