公开(公告)号：NZ282185A

公开(公告)日：1998-03-25

申请号：NZ28218595

申请日：1995-02-15

Applicant: UNIV TEXAS ,  PHARMACYCLICS INC

Inventor： SESSLER JONATHAN L ,  MODY TARAK D ,  HEMMI GREGORY W

IPC: A61K31/40 ,  A61K41/00 ,  A61K47/48 ,  A61K49/00 ,  A61K49/06 ,  A61K49/08 ,  A61K51/00 ,  A61K51/04 ,  A61L2/00 ,  A61P35/00 ,  C07D487/22 ,  C07H21/00 ,  A61K49/04 ,  A61K31/555 ,  A61K31/395 ,  A61K51/06

Abstract: Texaphyrin metal complexes having improved functionalization include the addition of electron-donating groups to positions 2, 7, 12, 15, 18 and/or 21 and/or the addition of electron-withdrawing groups to positions 15 and/or 18 of the macrocycle. Electron-donating groups at positions 2, 7, 12, 15, 18 and/or 21 contribute electrons to the aromatic pi system of the macrocycle which stabilizes the metal complex to demetallation and the imine bonds to hydrolysis. The addition of substituents to the 12 and 21 positions of the macrocycle offer steric protection for the imine bonds against possible in vivo enzyme hydrolysis. Electron-withdrawing groups at positions 15 and/or 18 render the macrocycle more readily reduced, i.e. the redox potential is lower and the macrocycle more readily gains an electron to form a radical. Such texaphyrins having a low redox potential and imine bond stabilization are useful in a variety of applications.

公开(公告)号：NO971317L

公开(公告)日：1997-05-16

申请号：NO971317

申请日：1997-03-20

Applicant: UNIV TEXAS ,  PHARMACYCLICS INC

Inventor： MAGDA DARREN ,  SESSLER JONATHAN L ,  IVERSON BRENT L ,  SANSOM PETRA I ,  WRIGHT MEREDITH ,  MODY TARAK D ,  HEMMI GREGORY W

IPC: A61K31/70 ,  A61K38/00 ,  C12N15/09 ,  A61K38/22 ,  A61K39/395 ,  A61K41/00 ,  A61K47/48 ,  A61K49/00 ,  A61K49/06 ,  A61K49/08 ,  A61K51/04 ,  A61L2/00 ,  B01J31/06 ,  B01J31/16 ,  B01J31/18 ,  C07D487/22 ,  C07H21/00 ,  C07H21/04 ,  C12N15/113 ,  A61K48/00

Abstract: Methods of cleavage of a polymer of deoxyribonucleic acid using photosensitive texaphyrins are disclosed. A preferred method of use is the site-specific cleavage of a polymer of deoxyribonucleic acid and a preferred texaphyrin is a derivatized texaphyrin having binding specificity, in particular, a texaphyrin covalently coupled to a site-directing molecule, preferably an oligonucleotide.

公开(公告)号：NO961436D0

公开(公告)日：1996-04-11

申请号：NO961436

申请日：1996-04-11

Applicant: UNIV TEXAS ,  PHARMACYCLICS INC

Inventor： SESSLER JONATHAN L ,  HARRIMAN ANTHONY M ,  MILLER RICHARD A ,  MODY TARAK D ,  HEMMI GREGORY W ,  KRAL VLADIMIR A ,  MAGDA DARREN

IPC: A61K31/40 ,  A61K31/407 ,  A61K41/00 ,  A61K47/48 ,  A61K49/00 ,  A61K49/06 ,  A61K49/08 ,  A61K51/00 ,  A61K51/04 ,  A61L2/00 ,  A61P35/02 ,  A61P43/00 ,  B01J31/06 ,  B01J31/16 ,  B01J31/18 ,  C07D487/22 ,  C07H21/00 ,  A61K

Abstract: Texaphyrins are provided for use as radiation sensitizers. Advantageous properties of texaphyrins for use as a radiation sensitizer include: i) a low redox potential which allows radiation-induced hydrated electrons to flow to texaphyrin rather than neutralizing hydroxyl radicals, allowing hydroxyl radicals to cause cellular damage, ii) a relatively stable texaphyrin radical that reacts readily to covalently modify neighboring molecules causing further cellular damage, iii) intrinsic biolocalization, and iv) indifference to the presence or absence of O2. These properties allow texaphyrins to be particularly effective for treating the hypoxic areas of solid neoplasms. Methods of treatment for an individual having a neoplasm or atheroma include the use of a texaphyrin as a radiation sensitizer and as an agent for photodynamic tumor therapy, or the use of a texaphyrin for internal and for external ionizing radiation. Novel texaphyrins are provided.

公开(公告)号：AU3727095A

公开(公告)日：1996-04-09

申请号：AU3727095

申请日：1995-09-21

Applicant: UNIV TEXAS ,  PHARMACYCLICS INC

Inventor： MAGDA DARREN ,  SESSLER JONATHAN L ,  IVERSON BRENT L ,  SANSOM PETRA I ,  WRIGHT MEREDITH ,  MODY TARAK D ,  HEMMI GREGORY W

IPC: C12N15/09 ,  A61K31/70 ,  A61K38/00 ,  A61K38/22 ,  A61K39/395 ,  A61K41/00 ,  A61K47/48 ,  A61K49/00 ,  A61K49/06 ,  A61K49/08 ,  A61K51/04 ,  A61L2/00 ,  B01J31/06 ,  B01J31/16 ,  B01J31/18 ,  C07D487/22 ,  C07H21/00 ,  C07H21/04 ,  C12N15/113 ,  C12N15/11

Abstract: Methods of cleavage of a polymer of deoxyribonucleic acid using photosensitive texaphyrins are disclosed. A preferred method of use is the site-specific cleavage of a polymer of deoxyribonucleic acid and a preferred texaphyrin is a derivatized texaphyrin having binding specificity, in particular, a texaphyrin covalently coupled to a site-directing molecule, preferably an oligonucleotide.