公开(公告)号：DE69902821D1

公开(公告)日：2002-10-10

申请号：DE69902821

申请日：1999-11-30

Applicant: BUCKMAN LABOR INC

Inventor： HEINDEL D ,  WHITTEMORE S ,  GUILLON CHRISTOPHE ,  RAPP D ,  LASKIN D ,  MCNEEL E ,  HECK E

IPC: C07D493/04 ,  A61K31/35

Abstract: The invention relates to 4'-substituted-4',5'-dihydropsoralen compounds of formula(V):In the formula R is hydrogen, a halogen, CN or an acyl group; T is a halogen, CN, a carboalkoxy group NR1R2, or (N+R1R2R3)X-, R1 and R2 are independently a C1-C6 alkyl, or R1 and R2 together with the nitrogen form a 5-8 member heterocyclic ring, or when T is (N+R1R2R3)X-, R1 and R2 together with the nitrogen form a 5-8 member heterocyclic ring or heterocyclic aromatic ring; R3 is hydrogen, a C1-C12 alkyl, or, when R1 and R2 together with the nitrogen form a heterocyclic aromatic ring, R3 is a double bond within the heterocyclic aromatic ring; X- is a halide. In another embodiment, the invention relates to processes for preparing 4'-substituted-4',5'-dihydropsoralen compounds described above. The compounds of the invention have beneficial pharmaceutical properties and can be used alone or in pharmaceutical compositions used to treat a proliferative skin disorder and to treat microbial infections in a mammal by administering to the mammal an effective amount of a compound of the invention and then irradiating the mammal with ultraviolet light.

公开(公告)号：DE69902821T2

公开(公告)日：2003-01-09

申请号：DE69902821

申请日：1999-11-30

Applicant: BUCKMAN LABOR INC

Inventor： HEINDEL D ,  WHITTEMORE S ,  GUILLON CHRISTOPHE ,  RAPP D ,  LASKIN D ,  MCNEEL E ,  HECK E

IPC: C07D493/04 ,  A61K31/35

Abstract: The invention relates to 4'-substituted-4',5'-dihydropsoralen compounds of formula(V):In the formula R is hydrogen, a halogen, CN or an acyl group; T is a halogen, CN, a carboalkoxy group NR1R2, or (N+R1R2R3)X-, R1 and R2 are independently a C1-C6 alkyl, or R1 and R2 together with the nitrogen form a 5-8 member heterocyclic ring, or when T is (N+R1R2R3)X-, R1 and R2 together with the nitrogen form a 5-8 member heterocyclic ring or heterocyclic aromatic ring; R3 is hydrogen, a C1-C12 alkyl, or, when R1 and R2 together with the nitrogen form a heterocyclic aromatic ring, R3 is a double bond within the heterocyclic aromatic ring; X- is a halide. In another embodiment, the invention relates to processes for preparing 4'-substituted-4',5'-dihydropsoralen compounds described above. The compounds of the invention have beneficial pharmaceutical properties and can be used alone or in pharmaceutical compositions used to treat a proliferative skin disorder and to treat microbial infections in a mammal by administering to the mammal an effective amount of a compound of the invention and then irradiating the mammal with ultraviolet light.