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US5369101A Expired / Lapsed US ⏱️ 0.0 years remaining

Expanded porphyrins: large porphyrin-like tripyrroledimethine-derived macrocycles

Assignee: The University of Texas System
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Filing: 1993-12-16
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Granted: 1994-11-29
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Expires: 2013-12-16
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Abstract

Abstract The present invention involves a novel tripyrrole dimethine-derived "expanded porphyrin" (texaphyrin), the synthesis of such compounds, their analogs or derivatives and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Metal complexes of these compounds are active as photosensitizers for the generation of singlet oxygen and thus potentially for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus and tumor cells as well. A variety of texaphyrin derivatives have been produced and many more are readily obtainable. Various metal (e.g., transition, main group, and lanthanide) complexes with the texaphyrin and texaphyrin derivatives of the present invention have unusual water solubility and stability which render them particularly useful. These metallotexaphyrin complexes have optical properties making them unique as compared to existing porphyrin-like or other macrocycles. For example, they absorb light strongly in a physiologically important region (i.e. 690-880 nm). These complexes also form long-lived triplet states in high yield and act as efficient photosensitizers for the formation of singlet oxygen. These properties, coupled with their high chemical stability and appreciable solubility in polar media such as water, add to their usefulness.

Inventors

  • 👤 Jonathan L. Sessler
  • 👤 Gregory W. Hemmi
  • 👤 Toshiaki Murai

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 09:40
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/22; A; A61; A61K; A61K41/00; A61K41/0038; A61K41/0057; A61K41/0076; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/545; A61K47/546; A61P; A61P31/00; A61P31/12; A61P31/14; A61P31/18; A61P35/00

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 194 words
A compound having the structure: ##STR17## wherein: M is H; a trivalent metal cation selected from the group consisting of Mn +3 , Co +3 , Ni +3 , Fe +3 , Ho +3 , Ce +3 , Y +3 , In +3 , Pr +3 , Nd +3 , Sm +3 , Eu +3 , Gd +3 , Tb +3 , Dy +3 , Er +3 , Tm +3 , Yb +3 , Lu +3 , La +3 , and U +3 ; or a divalent metal cation selected from the group consisting of Ca +2 , Mn +2 , Co +2 , Ni +2 , Zn +2 , Cd +2 , Hg +2 , Sm +2 , and UO 2 +2 ; R 1 , R 2 , and R 3 are independently hydrogen, alkyl, carboxy or carboxyalkyl where at least one of R 1 , R 2 , and R 3 is carboxy or carboxyalkyl; the molecular weight of any one of R 1 , R 2 , or R 3 is less than or equal to about 1000 daltons; and n is an integer less than or equal to 2.
Claim 2
Dependent Claim 194 words
A compound having the structure: ##STR17## wherein: M is H; a trivalent metal cation selected from the group consisting of Mn +3 , Co +3 , Ni +3 , Fe +3 , Ho +3 , Ce +3 , Y +3 , In +3 , Pr +3 , Nd +3 , Sm +3 , Eu +3 , Gd +3 , Tb +3 , Dy +3 , Er +3 , Tm +3 , Yb +3 , Lu +3 , La +3 , and U +3 ; or a divalent metal cation selected from the group consisting of Ca +2 , Mn +2 , Co +2 , Ni +2 , Zn +2 , Cd +2 , Hg +2 , Sm +2 , and UO 2 +2 ; R 1 , R 2 , and R 3 are independently hydrogen, alkyl, carboxy or carboxyalkyl where at least one of R 1 , R 2 , and R 3 is carboxy or carboxyalkyl; the molecular weight of any one of R 1 , R 2 , or R 3 is less than or equal to about 1000 daltons; and n is an integer less than or equal to 2.
Claim 3
Dependent Claim 12 words
The compound of claim 1 wherein R 1 is CH 2 COOH.
Claim 4
Dependent Claim 13 words
The compound of claim 1 wherein R 2 or R 3 is COOH.
Claim 5
Dependent Claim 23 words
The compound of claim 1 wherein R 1 is CH 2 CH 3 , R 2 is H and R 3 is COOH.
Claim 6
Dependent Claim 20 words
The compound of claim 1 wherein R 1 is CH 2 COOH, and R 2 and R 3 are H.
Claim 7
Dependent Claim 20 words
The compound of claim 1 wherein R 1 is CH 2 COOH, and R 2 and R 3 are alkyl.
Claim 8
Dependent Claim 28 words
A compound having the structure: ##STR18## wherein M is a divalent metal ion and n is 1 or M is a traivalent metal ion and n is 2.
Claim 9
Dependent Claim 28 words
A compound having the structure: ##STR18## wherein M is a divalent metal ion and n is 1 or M is a traivalent metal ion and n is 2.
Claim 10
Dependent Claim 134 words
A compound having the structure: ##STR19## wherein M is H, a divalent metal cation selected from the group consisting of Ca +2 , Mn +2 , Co +2 , Ni +2 , Zn +2 , Cd +2 , Hg +2 , Sm +2 and UO 2 +2 ; or a trivalent metal cation selected from the group consisting of Mn +3 , Co +3 , Ni +3 , Fe +3 , Ho +3 . Ce +3 , Y +3 . In +3 , Pr +3 , Nd +3 , Sm +3 , Eu +3 , Gd +3 , Tb +3 , Dy +3 , Er +3 , Tm +3 , Yb +3 , Lu +3 , La +3 , and U +3 ; and n is an integer less than or equal to 2.
Claim 11
Dependent Claim 134 words
A compound having the structure: ##STR19## wherein M is H, a divalent metal cation selected from the group consisting of Ca +2 , Mn +2 , Co +2 , Ni +2 , Zn +2 , Cd +2 , Hg +2 , Sm +2 and UO 2 +2 ; or a trivalent metal cation selected from the group consisting of Mn +3 , Co +3 , Ni +3 , Fe +3 , Ho +3 . Ce +3 , Y +3 . In +3 , Pr +3 , Nd +3 , Sm +3 , Eu +3 , Gd +3 , Tb +3 , Dy +3 , Er +3 , Tm +3 , Yb +3 , Lu +3 , La +3 , and U +3 ; and n is an integer less than or equal to 2.

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