Abstract: A melanin-concentrating hormone antagonist which comprises a compound of the formula: wherein Ar1 is a cyclic group which may have substituents; X is a spacer having a main chain of 1 to 6 atoms; Y is a bond or a spacer having a main chain of 1 to 6 atoms; Ar is a monocyclic aromatic ring which may be condensed with a 4 to 8 membered non-aromatic ring, and may have further substituents; R1 and R2 are independently hydrogen atom or a hydrocarbon group which may have substituents; R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing hetero ring which may have substituents; R2 may form a spiro ring together with Ar; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing hetero ring which may have substituents; or a salt thereof; which is useful as an agent for preventing or treating obesity, etc.

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: The present invention relates to a novel titanyl phthalocyanine crystal which can prepare a coating solution having excellent storage stability because it satisfies both of the following two characteristics (a) and (b), a method of producing the same, an electrophotosensitive material using the above crystal as an electric charge generating material. (a) The crystal has a maximum peak at a Bragg angle 2?±0.2°=27.2° and has no peak at 7.4° in a CuK? characteristic X-ray diffraction spectrum. (b) The crystal does not have a peak of a change in temperature within a range from 50 to 400° C. except for a peak associated with evaporation of adsorbed water in differential scanning calorimetry.

Abstract: The present invention is based on the unexpected discovery that CoQ-10 can be made commercially in a highly bioavailable form suitable for topical, sublingual formulations, or for oral ingestion. One such bioavailable form is a water dispersible freeze-dried CoQ-10/?-cyclodextrin complex. Complexation in general with ?- or ?-cyclodextrin improved the cellular uptake of CoQ-10 as compared to water dispersible liposomal or micellar forms of CoQ-10. Thus, the present invention includes a highly bioavailable CoQ-10/cyclodextrin complex for use in the nutritional supplement, oral care, and pharmaceutical industry.

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: 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: 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: 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 use of triaryl acid derivatives of formula (I) and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.

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: Methods of making high molecular weight hyaluronates are disclosed. The methods include contacting a hyaluronate-containing source with an acid to make an acidic hyaluronate suspension, contacting that suspension with an anionic ion exchange medium in the presence of an acidic buffer, and thereafter contacting the medium with an acidic buffer having a higher salt content to desorb the hyaluronate from the medium. The methods are amenable for isolating hyaluronate from such sources as avian (e.g., chicken, duck, turkey, or goose) eggshells and connective tissues of animals.

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: 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 present invention provides an oxidative coupling procedure that allows efficient synthesis of novel cyclo[n]pyrrole macrocycles. Therefore, the present invention provides cyclo[n]pyrroles where n is 6, 7, 8, 9, 10, 11, or 12, and derivatives, multimers, isomers, and ion and neutral molecule complexes thereof as new compositions of matter. A protonated form of cyclo[n]pyrrole displays a gap of up to 700 nm between strong Soret and Q-like absorption bands in the electronic spectrum, demonstrating no significant ground state absorption in the visible portion of the electronic spectrum. Uses of cyclo[n]pyrroles as separation media, nonlinear optical materials, information storage media and infrared filters are provided.

Abstract: This invention is concerned with novel polycyclic compounds of formula [I], wherein ring A, ring B, R1, R2, R3, R4, R5, R6, X, Y, R1?, R2?, R3?, R4?, R5?, R6?, ring A?, ring B? and X? are as defined hereinabove as well as pharmaceutically acceptable salts thereof. The compounds have anti-tumor activity and are useful for the treatment of cell proliferative disorders.

Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, R1, R2, R3a, R3b, R4, R5, R6, R7 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: Taxane antineoplastic agents which have heretofore exhibited poor or non-existent oral bioavailability are administered orally to human patients suffering from taxane-responsive disease conditions and made sufficiently bioavailable to achieve therapeutic blood levels. In a preferred embodiment, the taxane, preferably paclitaxel, is co-administered to the patient with an oral cyclosporin enhancing agent, preferably cyclosporin A. By one preferred method, a dose of oral enhancer is administered about 0.5-72 hours before the taxane and a second dose of the enhancer and administered immediately before, together with or immediately after the taxane. A method of treating human patients suffering from taxane-responsive disease conditions is also provided, as well as a method for providing such treatment while preventing or reducing hypersensitivity and allergic reactions without the need for pre-medication.