IPC분류정보
국가/구분 |
United States(US) Patent
등록
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국제특허분류(IPC7판) |
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출원번호 |
US-0112872
(1993-08-25)
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발명자
/ 주소 |
- Sessler Jonathan L. (Austin TX) Hemmi Gregory W. (Austin TX) Mody Tarak D. (Austin TX)
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출원인 / 주소 |
- Board of Regents, The University of Texas System (Austin TX 02)
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인용정보 |
피인용 횟수 :
28 인용 특허 :
0 |
초록
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The present invention involves water soluble hydroxy-substituted texaphyrins retaining lipophilicity, the synthesis of such compounds and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Various metal (e.g., transition, main group, a
The present invention involves water soluble hydroxy-substituted texaphyrins retaining lipophilicity, the synthesis of such compounds and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Various metal (e.g., transition, main group, and lanthanide) complexes of the hydroxy-substituted texaphyrin derivatives of the present invention have unusual water solubility and stability. They absorb light strongly in a physiologically important region (i.e. 690-880 nm). They have enhanced relaxivity and therefore are useful in magnetic resonance imaging. They form long-lived triplet states in high yield and act as photosensitizers for the generation of singlet oxygen. Thus, they are useful for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus as well as tumor cells. They are water soluble, yet they retain sufficient lipophilicity so as to have greater affinity for lipid rich areas such as atheroma and tumors. They may be used for magnetic resonance imaging followed by photodynamic tumor therapy in the treatment of atheroma and tumors. These properties, coupled with their high chemical stability and appreciable solubility in water, add to their usefulness.
대표청구항
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A method of treating a host harboring atheroma, leukemia., lymphoma, sarcoma, or carcinoma comprising: administering to the host as a first agent a water soluble hydroxy-substituted texaphyrin having structure (A); [Figure] (A) wherein M is a detectable metal; R1, R2, R3, R4, and R5 are independentl
A method of treating a host harboring atheroma, leukemia., lymphoma, sarcoma, or carcinoma comprising: administering to the host as a first agent a water soluble hydroxy-substituted texaphyrin having structure (A); [Figure] (A) wherein M is a detectable metal; R1, R2, R3, R4, and R5 are independently hydrogen, hydroxyl, alkyl, hydroxyalkyl, oxyalkyl, oxyhydroxyalkyl, saccharide, carboxyalkyl or carboxyamidealkyl where at least one of R1, R2, R3, R4, and R5 is hydroxyl, oxyhydroxyalkyl, saccharide, oxyalkyl, carboxyalkyl, carboxyamidealkyl or hydroxyalkyl; the molecular weight of any one of R1, R2, R3, R4, or R5 is less than or equal to about 1000 daltons; N is an integer less than or equal to 2; determining localization sites in the host by reference to the detectable metal; administering to the host as a second agent a water soluble hydroxy-substituted texaphyrin having structure (A) wherein M is a diamagnetic metal, and R1, R2, R3, R4, R5, the molecular weight and N are as described above; and photoirradiating the second agent in proximity to said atheroma, leukemia, lymphoma, sarcoma, or carcinoma.
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