IPC분류정보
| 국가/구분 |
United States(US) Patent
등록
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| 국제특허분류(IPC7판) |
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| 출원번호 |
US-0449681
(1995-05-24)
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발명자
/ 주소 |
- Sessler Jonathan L. (Austin TX) Harriman Anthony M. (Bischheim FRX) Miller Richard A. (Portola Valley CA) Mody Tarak D. (Sunnyvale CA) Hemmi Gregory W. (Sunnyvale CA) Kral Vladimir A. (Austin TX) Mag
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| 출원인 / 주소 |
- Pharmacyclics, Inc. (Sunnyvale CA 02) Board of Trustees, Univ. of TX Sys. (Austin TX 02)
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| 인용정보 |
피인용 횟수 :
13 인용 특허 :
0 |
초록
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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
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.
대표청구항
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A texaphyrin having the structure: [Figure] wherein R1-R4 and R6-R9 are independently hydrogen, halide other than iodide, hydroxyl, alkyl, aryl, haloalkyl other than iodoalkyl, nitro, formyl, acyl, hydroxyalkyl, oxyalkyl, oxyhydroxyalkyl, saccharide, carboxy, carboxyalkyl, carboxyamidealkyl, a site-
A texaphyrin having the structure: [Figure] wherein R1-R4 and R6-R9 are independently hydrogen, halide other than iodide, hydroxyl, alkyl, aryl, haloalkyl other than iodoalkyl, nitro, formyl, acyl, hydroxyalkyl, oxyalkyl, oxyhydroxyalkyl, saccharide, carboxy, carboxyalkyl, carboxyamidealkyl, a site-directing molecule or a couple to a site-directing molecule; R5 and R10 are independently hydrogen, alkyl, aryl, hydroxyalkyl, oxyalkyl, oxyhydroxyalkyl, carboxyalkyl, carboxyamidealkyl or a couple to a site-directing molecule; R11 is alkyl, alkenyl, oxyalkyl or hydroxyalkyl having up to about 3 carbon atoms and having rotational flexibility around a first-bound carbon atom; where R6 and R9 are other than hydrogen, then R5 and R10 are hydrogen or methyl; and where R5 and R10 are other than hydrogen, then R6 and R9 are hydrogen, hydroxyl, or halide other than iodide.
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