摘要:
Methods of modifying polypyrrolic macrocycles by use of a 1,3-dipolar cycloaddition are described. The methods may be used to produce compounds for further derivatization to produce photosensitizing agents of interest.
摘要:
The invention provides for tripyrrane compounds of the formula ##STR1## wherein: each Q represents, typically, an alkyl group, cycloalkyl group, aryl group, or a heteroaryl group; and each R represents hydrogen, an alkyl group, alcohol group, or a carbonyl-containing group. Additionally, there are described methods to prepare such compounds, for example, comprising the steps of:(a) reacting a compound of the formula:Q--CHO or Q--CH(OS)(OS')wherein S and S' are independently lower alkyl, an aryl group containing from 5 to 14 ring atoms, and --(CH.sub.2).sub.n -- where n=2-4;with a stoichiometric excess of a pyrrole having the formula: ##STR2## in the presence of a catalytic amount of an acid; (b) removing the unreacted pyrrole or any other solvents used in (a) by evaporation to form a residue; and(c) treating the residue to remove high molecular weight polymeric materials and the corresponding dipyrromethane by-product, leaving the desired compound.
摘要:
Compounds of the formula ##STR1## and the metalated forms and salts thereof; wherein n is an integer of 1-4; and wherein each P.sub.i is independently a pyrrole residue of the formula ##STR2## wherein each R.sub.ia and R.sub.ib is independently a noninterfering substituent, and wherein each Z.sub.i is independently a covalent bond; or is a meso bridging group of the formula ##STR3## or is an N-meso bridging group of the formula .dbd.N--.revreaction.--N.dbd.; or is a CC linkage of the formula ##STR4## or is a CNCCNC linkage of the formula ##STR5## wherein each R.sub.ic, R.sub.id, R.sub.ie, R.sub.if and R.sub.ig is independently a noninterfering substituent; or is a CNC linkage of the formula --CH.dbd.N--CH.dbd..revreaction..dbd.CH--N.dbd.CH-- wherein at least one Z.sub.i is said CNC linkage, are disclosed. These compounds are useful in photodynamic therapy and diagnosis. The metalated forms when the metal is paramagnetic are useful as MRI contrast agents.
摘要:
The invention is generally related to the field of photodynamic therapy by use of photosensitizers and stabilized formulations of the photosensitizers. These formulations may be used to deliver a photosensitizer as a pharmaceutical, agricultural, or industrial agent. The photosensitizer containing formulations and compositions of the invention comprise one or more block copolymers. Furthermore, the invention relates to processes for the production of, and application of, said formulations and compositions as photosensitizer drug delivery systems.
摘要:
A method for the separation of benzoporphyrin derivative mono and diacid (BPD-MA, BPD-DA) enantiomers by Laser-Induced Fluorescence Capillary Electrophoresis has been developed. The limits of detection are 2.06×10−6 M, and the relative standard deviation for the separation was 2.90% to 4.64%. The BPD enantiomers can be quantitatively determined in the range of 10−2 to 10−5 mg mL−1. In comparison with HPLC, CE has better resolution and efficiency. This separation method was successfully applied to the BPD enantiomers obtained from a matrix of bovine serum and from liposomally formulated material as well as from studies with rat, dog and human microsomes.
摘要:
A group of novel expanded porphyrin-like compounds, porphacyanine (Pc) and porphacyanine-like compounds, having absorption maxima in the range of 400-850 nanometers is useful in detecting and treating targeted tissues, cells and viruses. The use of the Pc of the invention permits the irradiation to comprise wavelengths other than those absorbed by blood. The Pc of the invention may also be conjugated to target-specific moieties such as immunoglobulins or fragments thereof to target specific tissues or cells for the radiation treatment. Use of these materials permits greater depth of treatment penetration and greater specificity in targeting tissues or cells. Coupled with an appropriate paramagnetic ion or radioisotope, the Pc of the invention is suitable for use in nuclear magnetic resonance imaging and radioimaging.
摘要:
A group of hydro-dibenzoporphyrins prepared by di-Diels-Alder additions at the A and C rings of the appropriate divinyl porphyrins have absorption maxima in the range of 700-820 nanometers and are photosensitizing agents. These compounds are useful in treating disorders or conditions which are subject to hematoporphyrin derivative (HPD) treatment in the presence of light, or in treating biological materials generally to destroy unwanted targets such as viruses, cells and tissues. The use of the compounds of the invention permits irradiation with wavelengths other than those absorbed by blood. The compounds of the invention may also be conjugated to ligands specific for receptors or to specific immunoglobulins or fragments thereof to home to target tissues or cells for the radiation treatment. Use of these materials permits lower levels of photosensitizer to be used, thus preventing side reactions which might destroy normal tissues.