Abstract: This invention discloses compositions and method for treating various types of skin disorders, based on topical cutaneous delivery of copper chemically bound with botanical pigments. Sodium-copper-chlorophyllin is used as an example, showing benefits in the treatment of rosacea, acne, oily skin, enlarged pores, and in relieving skin inflammation. Benefits are also disclosed in treatment of environmentally caused premature skin aging, via reductions in fine facial lines and wrinkles, increased tensile strength of the skin, and increased protection against sunlight via increased production of melanin. Therapeutic outcomes are improved when the copper-pigment complex is enclosed within submicron liposomes.

Abstract: The present invention relates to a method for the prevention and/or treatment of vascular disorders and/or secondary disorders associated therewith, such as depression. The method according to the invention comprises the oral administration of a preparation which contains at least the following fractions: a) long chain polyunsaturated fatty acids; b) at least two different phospholipids selected from the group consisting of phosphatidylserine, phosphatidylinositol, phosphatidylcholine and phosphatidylethanolamine and c) one or more compounds which are a factor in methionine metabolism, which compounds are selected from the group consisting of folate, vitamin B12, vitamin B6, magnesium and zinc or equivalents thereof. The invention also relates to a preparation for oral dosage comprising: at least 120 mg of long chain polyunsaturated fatty acids; at least 200 mg phospholipids; at least 200 ?g folate; and at least 0.1 mg hypericin and/or at least 100 mg extract of Withania somnifera.

Abstract: The invention relates to the use of arsenic compounds to treat a variety of neoplastic diseases. The present invention encompasses the administration to a mammal of arsenic in the form of a salt, complex, organic compound or ionic solution to treat tumors of epithelial tissue, connective tissue, central nervous system, lymphoid tissue, hematopoietic cells and tumors associated with oncogenic viruses. This invention also encompasses the treatment of hematopoietic disorders in mammals by the administration of one or more arsenic compounds to said mammal. Further, the arsenic compounds may be used to treat metastatic neoplastic diseases.

Abstract: A photo-functional molecule element having, on a substrate, a porphyrin polymer containing covalently-fixed porphyrin units, and the method of preparing the same. The photo-functional molecule element may be used as a photoelectric conversion element such as an organic solar cell or a three-dimensional, non-linear organic material.

Abstract: The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating cellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods.

Abstract: The invention relates to the use of arsenic compounds to treat a variety of neoplastic diseases. The present invention encompasses the administration to a mammal of arsenic in the form of a salt, complex, organic compound or ionic solution to treat tumors of epithelial tissue, connective tissue, central nervous system, lymphoid tissue, hematopoietic cells and tumors associated with oncogenic viruses. This invention also encompasses the treatment of hematopoietic disorders in mammals by the administration of one or more arsenic compounds to said mammal. Further, the arsenic compounds may be used to treat metastatic neoplastic diseases.

Abstract: Novel coordination polymers, their pharmaceutical formulations, useful for treating atheroma, tumors and other neoplastic tissue, as well as other conditions that are responsive to the induction of targeted oxidative stress, are disclosed.

Abstract: A compound of the formula where R1 is H, C1–C4 alkyl and OH; R2 in is H, C1–C4 alkyl and OH; R3 is H and C1–C4 alkyl; R4 is H and C1–C4 alkyl; n is an integer between 0 and 2 inclusive; R5 is a nullity, NHR7C(O)—, C6H4—, C6H4—O—; R7 is C2–C6 alkyl; and R6 is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine, blood brain barrier (BBB) peptide, membrane translocating peptide, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, transferrin, glucosylamine, amino saccharin, saccharin ester, lactylamine, leucine, tryptophan, amino glutamate and amino cholines.

Abstract: Phthalocyanine analogues having an active group able to link the phthalocyanine t carriers molecules and phthalocyanine to carriers molecules and phthalocyanine analogues as phthalocyanine-carrier conjugates showing enhanced photodynamic properties, red shifted absorption characteristic, all useful for photodynamic therapy, are described. Photosensitizers themselves or the photosensitizers-carriers conjugates are useful compounds either for treatment of various infectious diseases, the in vivo eradication of micro-organisms as well as diseases characterized by cellular hyperproliferation, in particular tumours psoriasis, actinic keratosis, atheromas, endoarterial hyperplasia and prostate hyperplasia. The above compounds can be also useful for blood and blood derivatives sterilization and in vivo/vitro diagnostics.

Abstract: A compound having the structural formula: where R is H or lower alkyl of 1 through 12 carbon atoms. In general, the compounds of the invention are 132-Oxo-bacteriopyropheophorbide—a carboxylic acid and C1–C12 alkyl esters thereof. A method for the preparation of the carboxylic acid compounds of the invention includes the step of reacting bacteriopyropheophorbide—a alkyl ester with lithium hydroxide tetrahydrofuran and water.

Abstract: The present invention is directed to metal-phthalocyanines of general formula (I) to the corresponding conjugates, the processes for their preparation and use in the photodynamic therapy of microbial infections (viral, bacterial and mycotic), tumor, pre-cancerous and proliferative pathologies and/or in the diagnosis, as well as for blood and blood derivatives sterilization

Abstract: Amphiphilic biocompatible cyclodextrin grafted polymers comprising a hydrophobically modified cyclodextrin moiety, a linear linker and a biocompatible hydrophilic polymer backbone, wherein said cyclodextrin moiety is grafted to said biocompatible hydrophilic polymer backbone by said linker are disclosed. The cyclodextrin-grafted biocompatible polymers of this invention may be used as bioactive agent carriers. Methods of making and using such cyclodextrin-grafted biocompatible polymers are disclosed.

Abstract: The present invention provides an IR-absorbing dye of formula (I) or (II): wherein Q1, Q2, Q3 and Q4 are the same or different and are independently selected from a C3-20 heteroarylene group comprising at least one N atom; M is selected from Si(A1)(A2), Ge(A1)(A2), Ga(A1), Mg, Al(A1), TiO, Ti(A1)(A2), ZrO, Zr(A1)(A2), VO, V(A1)(A2), Mn, Mn(A1), Fe, Fe(A1), Co, Ni, Cu, Zn, Sn, Sn(A1)(A2), Pb, Pb(A1)(A2), Pd and Pt; A1 and A2 are axial ligands, which may be the same or different, and are selected from —OH, halogen, —OR3, a hydrophilic ligand and/or a ligand suitable for reducing cofacial interactions; R3 is a selected from C1-12 alkyl, C5-12 aryl, C5-12 arylalkyl or Si(Rx)(Ry)(Rz); and Rx, Ry and Rz may be the same or different and are selected from C1-12 alkyl, C5-12 aryl, C5-12 arylalkyl, C1-12 alkoxy, C5-12 aryloxy or C5-12 arylalkoxy. Dyes of this type are especially suitable for use in netpage and Hyperlabel systems.

Abstract: The present invention provides a pharmaceutical composition comprising at least one pharmaceutically acceptable bismuth-containing compound, at least one pharmaceutically acceptable non-clay-derived suspending agent, and water. The suspension exhibits reduced upward pH drift by comparison with an otherwise similar suspension which comprises a clay-derived suspending agent. Such compositions are useful in the prevention and treatment of gastrointestinal diseases and/or disorders.

Abstract: A porphyrin metal complex that can form a stable oxygen complex and acts effectively as an oxygen infusion, which comprises: a transition metal ion M of period 4 or 5 coordinating to a porphyrin derivative represented by the following general wherein R1 is an alicyclic hydrocarbon group which may contain a substituent, R2 is an alkylene group and R3 is a group which does not hinder the coordination of an imidazolyl group to M.

Abstract: This invention provides antioxidant cyclic salen-metal compounds, compositions of such antioxidant cyclic salen-metal compounds having superoxide activity, catalase activity and/or peroxidase activity and methods of using such antioxidant cyclic salen-metal compositions to treat or prevent a disease associated with cell or tissue damage produced by free radicals, such as superoxide.

Abstract: The present invention relates to compounds of the Formula wherein R3, R5, R6, R7, and Z, and other variables enumerated under one or more of R3, R5, R6, R7, and Z, are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. This invention also relates to pharmaceutical compositions and methods of treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.

Abstract: The invention provides mitochondrially targeted antioxidant compounds comprising a lipophilic cation moiety covalently coupled to a glutathione peroxidase mimetic. These compounds can be used to treat patients who would benefit from the reduction of oxidative stress.

Abstract: Injectible formulations comprising motexafin gadolinium are described herein.

Abstract: The topical administration of statins for the treatment of bone disorders is disclosed.

Abstract: A covalently linked linear porphyrin polymer represented by formula (1): wherein R represents an alkyl group or ?(wherein a, b and d independently represent H, an alkyl group or aryl group); X represents —O—, —S—, >NR101 (wherein R101 represents H or an alkyl group), —CH2— or a single bond; Y represents ?O, ?S, or 2H; m represents an integer of 0 to 4; n represents an integer of 0 to 6; Z represents a five- or six-membered, nitrogen-containing, coordinating hetero aromatic ring group; M represents an ion of metal selected from typical metals and transition metals; Q1 represents a single bond or a linear, divalent linking group; and p1 represents an integer of 2 or more.

Abstract: The invention provides methods for treating cancer and compounds that are useful for the treatment of tumors, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates useful for preparing the compounds.

Abstract: The invention relates to novel, water-soluble porphyrin platinum compounds of the tetraarylporphyrin platinum derivatives type or of the hematoporphyrin platinum derivatives type with high tumor selectivity and their use for the treatment of benign and malignant tumor diseases. In particular, the compounds are suitable for photodynamic anti-tumor therapy.

Abstract: Metal-complexable substituted bis-indole derivatives comprising the structure shown in formula (I) hereunder: enantiomers and pharmaceutically acceptable salts thereof and metal complexes thereof, wherein L, R1, R2, R3, C1, C2, m, n, p, q and r are as defined in claim 1 for use as constrats agents.

Abstract: The invention provides a method for enhancing bone formation, inhibiting osteoclastic differentiation and/or activating osteoblastic differentiation whereby to manage, treat or achieve prophylaxis of bone disease which comprises administering to a human or animal subject suffering from, or susceptible to bone disease a therapeutically or prophylactically effective amount of a lanthanum compound.

Abstract: A method to enhance the cytotoxic activity of an antineoplastic drug comprising administering an effective amount of the antineoplastic drug to a host exhibiting abnormal cell proliferation in combination with an effective cytotoxicity-increasing amount of an antioxidant. The invention also includes a method to decrease the toxicity to an antineoplastic agent or increase the therapeutic index of an antineoplastic agent administered for the treatment of a solid growth of abnormally proliferating cells, comprising administering an antioxidant prior to, with, or following the antineoplastic treatment.

Abstract: This invention relates to a class of heterocycles and their metal complexes, and is particularly concerned with the use of these compounds in the preparation of prodrugs or as prodrugs that may be activated under hypoxic conditions by enzymes or by therapeutic ionising radiation, in the treatment of cancer. The invention also relates to the use of these heterocycles and the corresponding metal complexes in the preparation of medicaments and to compositions including the heterocycles or their metal complexes and to methods for preparing these compounds.

Abstract: An improved method to treat conditions of the eye characterized by ocular neovascularization is provided in which patients are given and initial photodynamic therapy (PDT) treatment to destroy the neovasculature, and then are re-evaluated at least twice during the following 6 months, and retreated as necessary. Preferably, three retreatments are provided.

Abstract: A process for the preparation of pyropheophorbide a and its derivatives, including 3-devinyl-3-(1?-hexyloxy)ethyl-pyropheophorbide-a, otherwise known as HPPH, is provided. The process involves treating chlorin e6, in the form of its trimethyl ester, with a base, followed by heating to give pyropheophorbide a, which is converted to HPPH by treatment with acid, followed by hexyl alcohol under basic conditions.

Abstract: An estrogen/antiestrogen-porphyrin conjugate, their composition and methods for their use are claimed. The active compounds of the invention are conjugates consisting of an estrogen or anti estrogen portion, tether or linker portion and a porphyrin portion. The method of invention exploits an active process that involves strong and specific interactions between nuclear receptor and its cognate ligand.

Abstract: Nitrosylation of proteins and amino acid groups enables selective regulation of protein function, and also endows the proteins and amino acids with additional smooth muscle relaxant and platelet inhibitory capabilities. Thus, the invention relates to novel compounds achieved by nitrosylation of protein thiols. Such compounds include: S-nitroso-heme proteins, S-nitroso-t-PA, S-nitroso-cathepsin; S-nitroso-lipoproteins; and S-nitroso-immunoglobulins. The invention also relates to therapeutic use if S-nitroso-protein compounds for regulating protein function, cellular metabolism and effecting vasodilation, platelet inhibition, relaxation of non-vascular smooth muscle, and increasing blood oxygen transport by hemoglobin and myoglobin. The compounds are also used to deliver nitric oxide in its most bioactive form in order to achieve the effects described above, or for in vitro nitrosylation of molecules present in the body.

Abstract: The invention provides a method for preparing glutathionylcobalamin (GluSCbl) which involves running the reaction in an aqueous solvent with a relatively small excess of glutathione, i.e. GluSH, specifically from one to less than four molar equivalents of GluSH. The formed GluSCbl is precipitated from the aqueous solvent, preferably by the addition of a precipitate inducing solvent. This provides GluSCbl in acceptable purity without the need for an additional chromatographic purification step. Additionally, it has been found that the reaction can be run to an acceptable level of purity by using very high concentrations of the reactants, i.e. around saturation concentrations for aquocobalamin. This has the advantage of eliminating the need for air-free conditions.

Abstract: Porphyrin-polyamine conjugate compounds are disclosed which have anticancer and antitumor effects. The porphyrin moiety selectively localizes in tumors, while the polyamine moiety serves as a cytotoxic agent. Methods of making and using the porphyrin-polyamine conjugate compounds are also disclosed.

Abstract: A porphyrin array exhibiting a large two-photon absorption property, and being linked with an acetylenic bond(s), represented by the following formulas: wherein R1 represents an alkyl or aryl group, M1 represents a metal ion capable of serving as a core metal and forming a coordinate bond with Im, M2 represents two protons or a metal ion incapable of forming a coordinate bond with Im, R2 and R3 represent a group selected from a porphyrin residue or porphyrin metal complex residue, a cyclic diimide residue, a dialkylviologen residue, a benzoquinone residue, an N-methylpyrrolidine-fullerene derivative residue and a ferrocene residue, Im is represented by Im1 or Im2: (R8 represents methyl or H), L1 represents —(—C?C—)m— (m=1 to 3); n represents an integer of 1 or more; R9 represents one of R1, R2, R3 and Im.

Abstract: The present invention is related to novel photopyrin compounds and the pharmaceutically acceptable salt thereof useful as an anticancer or photodynamic diagnostic agent by way of reproducing singlet state oxygen radical and the inventive compounds have superior advantages such as excellent photon yield to produce singlet oxygen, good physical stability and potent cell cytotoxicity to conventional photosensitizer. The present invention also provides a pharmaceutical composition comprising a novel photopyrin compound of formula (I) to (VII) or a pharmaceutically acceptable salt thereof as an active ingredient for preventing or treating various cancers such as stomach cancer, liver cancer, lung cancer, cervical cancer and breast cancer in human or mammal together with a pharmaceutically acceptable carrier.

Abstract: Several classes of in vivo carbon monoxide-releasing compounds are useful for the treatment and/or prevention of diseases, such as chronic inflammatory, e.g., rheumatoid arthritis, and of diseases with a strong inflammatory component, such as atherosclerosis, stroke, coronary disease, and Alzheimers disease. The in vivo carbon monoxide-releasing compounds can be attached to known drug vectors and/or known anti-inflammatory drugs, such as aspirin.

Abstract: A process for forming a cocrystalline mixture of titanyl phthalocyanine (TiOPc) and titanyl fluorophthalocyanine (TiOFPc) includes: dry milling a mixture of crude TiOPc and crude TiOFPc, thereby forming an amorphous pigment mixture of TiOPc and TiOFPc; and heating the amorphous pigment mixture at a temperature effective to form a cocrystalline composition comprising titanyl phthalocyanine (TiOPc) and titanyl fluorophthalocyanine (TiOFPc), the cocrystalline composition being characterized by an X-ray diffraction spectrum exhibiting intensity peaks at 7.2°, 12.9°, 16.3°, 22.3°, 24.6°, 26.2°, and 28.8° with respect to X-rays of Cu K?at a wavelength of 1.54 1 ? of the Bragg angle 2?.

Abstract: The present invention provides a class of porphyrins and metal chelated porphyrins for use as inhibitors of heme iron uptake. The porphyrin/metal chelated porphyrin molecules of the invention are tetra-positively charged porphyrins based on meso-tetra(4-pyridyl)porphines. Several such agents are shown herein to cause inhibition of iron uptake in vivo and in vitro. The invention further provides therapeutic compositions including the porphyrins and/or metalloporphyrins of the invention. In addition, methods of inhibition of heme iron uptake in vivo are taught, as well as methods of treatment of diseases characterized by iron-overload. These methods include the administration of a porphyrin or metalloporphyrin in a therapeutic composition of the invention to prevent uptake of heme iron, thus preventing replenishment of a patient's iron stores.

Abstract: This invention relates to a method of preparing a compound of formula (I): The method includes reacting one or more compounds of formula (II): in the presence of a base and a halogenating agent. In formulas (I) and (II) above, each A, independently, is aryl or heteroaryl; each n, independently, is 0–3; and each R1, independently, is C1–C10 alkyl, C3–C20 cycloalkyl, C3–C20 heterocycloalkyl, aryl, heteroaryl, halo, cyano, nitro, ORa, NRaRb, SiRaRbRc, COORa, OC(O)Ra, C(O)NRaRb, N(Ra)—C(O)Rb, or SO3Ra; wherein each of Ra, Rb, and Rc, independently, is H, C1–C10 alkyl, C3–C20 cycloalkyl, C3–C20 heterocycloalkyl, aryl, or heteroaryl; thereby producing the compound of formula (I) in a one-pot reaction. This invention also relates to the compounds prepared by the method described above.

Abstract: The present invention provides a novel paramagnetic metal-phthalocyanine complexes and pharmaceutically acceptable salts thereof, which are useful as contrast agents for MRI(Magnetic Resonance Imaging), diagnostic X-ray imaging and computed tomography(CT). The present invention also provides contrast agents for imaging, comprising the new paramagnetic metal-phthalocyanine complexes. The new contrast agents of the present invention show high imaging enhancement effects at lower concentration and are safer than the previously reported contrast agents.

Abstract: Expanded porphyrin comprising substitutions for at least two NH groups by S, Se or Te are non-photoactive and are selective for binding G-quadruplexes characteristic of the c-MYC control region. Accordingly, these expanded porphyrins are useful to modulate the expression of genes controlled by the formation of c-MYC type G-quadruplexes, such as c-MYC itself.

Abstract: The present invention is directed to low toxicity boronated compounds and methods for their use in the treatment, visualization, and diagnosis of tumors. More specifically, the present invention is directed to low toxicity carborane-containing 5, 10, 15, 20-tetraphenylporphyrin compounds and methods for their use particularly in boron neutron capture therapy (BNCT) and photodynamic therapy (PDT) for the treatment of tumors of the brain, head and neck, and surrounding tissue. The invention is also directed to using these carborane-containing tetraphenyl porphyrin compounds to methods of tumor imaging and/or diagnosis such as MRI, SPECT, or PET.

Abstract: A process of isolation of pure Acteoside of high hepatoprotection from plant Colerbrookea oppositifolia, said process comprising steps of drying aerial parts of the plant, grounding the dried parts into powder, percolating the powder with water or ethanol for 3-4 times to obtain an extract, filtering the extract for clearing of suspended particles to obtain supernatant, drying the supernatant at about 45 to 55° C.

Abstract: The present invention is directed to low toxicity boronated compounds and methods for their use in the treatment, visualization, and diagnosis of tumors. More specifically, the present invention is directed to low toxicity carborane-containing 5, 10, 15, 20-tetraphenylporphyrin compounds and methods for their use particularly in boron neutron capture therapy (BNCT) and photodynamic therapy (PDT) for the treatment of tumors of the brain, head, neck, and surrounding tissue. The invention is also directed to using these carborane-containing tetraphenyl porphyrin compounds to methods of tumor imaging and/or diagnosis such as MRI, SPECT, or PET.

Abstract: The invention provides mitochondrially targeted antioxidant compounds comprising a lipophilic cation moiety covalently coupled to an antioxidant moiety which is either a superoxide dismutase (SOD) mimetic or a glutathione peroxidase mimetic. These compounds can be used to treat patients who would benefit from the reduction of oxidative stress.

Abstract: The invention relates to medicine and concerns a photosensitizer for detecting and curing tumors. The inventive photosensitizer is embodied in the form of a composition containing chlorin in the form of salt and alkali metals. The chlorin is composed of 80-90% of chlorin e6, 5-20 of purpurin 5 and the rest being purpurin 18 -chlorin p6. Said photosensitizer is produced by extracting Spirulina biomass with the aid of acetone. Afterwards said biomass is exposed to acid treatment, neutralization, hydrolysis, extraction of pheophorbide a, dissolution in acetone, addition of a strong base, neutralization and reprecipitation of chlorin e6.

Abstract: This invention provides a novel class of substituted macrocyclic metallic complexes. The complexes are useful as peroxynitrite decomposition catalysts. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereof are also described.

Abstract: Vanadium compounds for inhibiting angiogenesis useful for treating or preventing diabetic retinopathy, hemangiomas, cancers with abnormal blood vessel supply, restenosis following vascular injury, and the like.

Abstract: The present invention covers halogenated derivatives of boronated phorphyrins containing multiple carborane cages having the formula which selectively accumulate in neoplastic tissue within the irradiation volume and thus can be used in cancer therapies including, but not limited to, boron neutron-capture therapy and photodynamic therapy. The present invention also covers methods for using these halogenated derivatives of boronated porphyrins in tumor imaging and cancer treatment.

Abstract: Dye-peptide conjugates useful for diagnostic imaging and therapy are disclosed. The dye-peptide conjugates include several cyanine dyes with a variety of bis- and tetrakis(carboxylic acid) homologues. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350-1300 nm, the exact range being dependent upon the particular dye. Use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The molecules of the invention are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities and for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.