Abstract: The invention provides novel compounds useful as kinase inhibitors or as starting materials And/or intermediates in the synthesis of compounds useful as kinase inhibitors. The compounds have The general structure of formula (I) wherein A is a 3- to 8-membered ring, optionally substituted and/or heteroatom-containing, and R1, R2, R3, R4, R5, R6, X, Y, Z, p, and q are as defined herein. The compounds may also be in the form of a salt, ester, amide, or other analog. In preferred compounds, A is a 5- to 8-membered ring, R1 is hydrogen, q is a bond, X is N, Y is C?O, Z is N, R2 contains a terminal amino moiety, p is 1, and R3 and R4 are linked to form a pyrrole ring fused to a second cyclic group. Pharmaceutical compositions and methods for using the compounds are also provided.

Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: Disclosed are compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein the groups Ar1, Ar2, A, R1, R2, R3, E1, E2, X and n are as defined in the description and claims, which are effective modulators of chemokine activity.

Abstract: Compounds of formula (I): wherein: A is as defined in the description, Y represents a group selected from an oxygen atom and a methylene group, R2 represents a hydrogen atom and in that case: R3 represents a group selected from a hydrogen atom and the groups linear or branched (C1–C6)alkyl, aryl, aryl-(C1–C6)alkyl (in which the alkyl moiety is linear or branched) and SO2CF3, or R2 and R3 form a bond, R1 represents a group selected from a hydrogen atom and the groups linear or branched (C1–C6)alkyl, aryl and aryl-(C1–C6)alkyl (in which the alkyl moiety is linear or branched) or a linear or branched (C1–C6)alkylene chain, Z1 and Z2 each represent a hydrogen atom or Z1 and Z2, together with the carbon atoms carrying them, form a phenyl group. Medicaments.

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 compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.

Abstract: This patent discloses a substituted fullerenes, compositions comprising the same, and their use as antioxidants. The substituted fullerenes comprise a fullerene core (Cn) and at least one of: (i) from 1 to 6 (>CX1X2) groups bonded to the fullerene core; (ii) from 1 to 18 —X3 groups bonded to the fullerene core; (iii) from 1 to 6 —X4— groups bonded to the fullerene core; or (iv) from 1 to 6 dendrons bonded to the fullerene core.

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: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.

Abstract: A compound selected from those of formula (I): wherein: W1 represents, together with carbon to which it is bonded, phenyl, pyridyl, Z represents a group of formula U—V as defined in the description, Q1 represents oxygen, NR2 as defined in the description, Q2 represents oxygen, NR?2 as defined in the description, X1, X2, X?1 and X?2 each represents hydrogen, hydroxy, alkoxy, mercapto or alkylthio, Y1, Y2, Y?1 and Y?2 each represents hydrogen, or X1 and Y1, X2 and Y2, X?1 and Y?1, X?2 and Y?2 with carbon carrying them, together form carbonyl or thiocarbonyl, R1 is as defined in the description, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer.

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 relates to novel Pyrrole-Type compounds, compositions comprising Pyrrole-Type compounds, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Pyrrole-Type compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for treating or preventing a viral infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the replication and/or infectivity of a virus. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for causing immunosuppression. The present invention also relates to novel Pyrrole-Type compounds, compositions, and methods useful for treating or preventing an autoimmune disease.

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: 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: Liposomal pharmaceutical formulations incorporating porphyrin photosensitizers useful for photodynamic therapy or diagnosis of malignant cells. The liposomal formulations comprise a porphyrin photosensitizer, particularly the hydro-mono benzoporphyrins (BPD) having light absorption maxima in the range of 670–780 nanometers, a disaccharide or polysaccharide and one or more phospholipids.

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: Provided are methods and compositions for the photodynamic therapy (PDT) of ocular conditions characterized by the presence of unwanted choroidal neovasculature, for example, neovascular age-related macular degeneration. The selectivity and sensitivity of the PDT method can be enhanced by combining the PDT with an anti-angiogenesis factor, for example, angiostatin or endostatin, or with an apoptosis-modulating factor. Furthermore, the selectivity and sensitivity of the PDT may be further enhanced by coupling a targeting moiety to the photosensitizer so as to target the photosensitizer to choroidal neovasculature.

Abstract: The present invention relates to the use of low-dose photodynamic therapy (PDT) to prevent, treat, inhibit or reduce restenosis in blood vessels. The present invention may be used in combination with any angioplastic procedure to prevent restenosis or to decrease the intima thickness, and thus luminal narrowing.

Abstract: The present invention is directed to novel multicyclic molecules that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of PARP, VEGFR2, and MLK3 enzymes, including, for example, neurodegenerative diseases, inflammation, ischemia, and cancer.

Abstract: New compounds useful in photodynamic therapy are of the formula and their 1,4-diene isomers and the metallated and/or labeled and/or conjugated forms thereof wherein each R1 is independently alkyl (1–6C); each n is independently an integer of 0–6; and R2 is vinyl or a derivative form thereof.

Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.

Abstract: Development of colorectal neoplasia in a patient subject or predisposed to colorectal neoplasia is reduced by the steps of (a) determining a patient is subject or predisposed to colorectal neoplasia; and (b) enterically delivering into the gut of the person an effective amount of an aminoglycoside antibiotic having poor gut absorption, whereby the development of the colorectal neoplasia is reduced as compared with otherwise similar non-treated patients.

Abstract: Injectible formulations comprising motexafin gadolinium are described herein.

Abstract: The compounds disclosed herein are indolocarbazoles of Formula (I), which are potent CDK4 inhibitors, and are useful in the treatment of cell proliferative disorders, including cancer. Formula (I).

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: This invention relates to pyrrolocarbazole derivatives according formula I wherein R1, R2, R7, R8, R9, X and Y are as defined in the specification wherein said derivatives specifically inhibit one or both of the checkpoint kinases Wee1 and Chk1

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 is directed to cyclic substituted fused pyrrolocarbazoles and isoindolones. The invention also is directed to methods for making and using the cyclic substituted fused pyrrolocarbazoles and isoindolones.

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: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.

Abstract: The present invention is based on the discovery of a composition that provides radiosensitization effect. Specifically the composition contains an indolocarbazole derivative. The present invention provides methods for radiosensitizing neoplastic cells using indolocarbazole derivatives and methods for treating neoplastic cells using indolocarbazole derivatives in combination with radiation or radiation and chemotherapy.

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: The invention is directed to pharmaceutical compositions useful in the treatment of migraine. The compositions contain metoclopramide and one or more NSAIDs in unit dosage form. By selecting NSAIDs that are non-acidic or segregating the metoclopramide and NSAID, the storage life of the compositions has been increased. Also disclosed are coordinated dosage forms for the sequential release of drugs. The invention encompasses methods of treating migraine using any of these dosage forms.

Abstract: Pharmaceutical nitrone comprise condensates of an N-hydroxylamine and a physiological aldehyde, providing improved delivery and absorption, enhanced stability and reduced toxicity. Preferred physiological aldehydes are subject to endogenous cellular uptake transport, and include pyridoxal, pyridoxal phosphate, and heme-A. Essentially any physiologically compatible and pharmaceutically active hydroxylamine moiety may be incorporated, such as hydroxylamine moieties of prior pharmaceutical nitrones, and known pharmaceutically active hydroxylamines.

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: Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided: where R1 through R7 are defined herein. The compounds of formula (I) are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.

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: Conjugate are formed by covalently linking a target-specific compound to pyropheophorbide compound which conjugated are injected into a host and accumulate in tumor tissue to a higher degree than surrounding normal tissues. When the pyropheophorbide compound component of the conjugate is exposed to a particular wavelength of light the compound becomes cytotoxic destroying the tumor or diseased tissue without causing irreversible normal tissue damage. The pyropheophorbide compounds have been shown to have a variety of characteristics when used in photodynamic therapy. These characteristics are further improved when the compounds are bound to a target specific component such as a ligand capable of binding to a specific cellular receptor (e.g. growth hormones and growth factors) or an antibody capable of binding to a particular antigen.

Abstract: Pyropheophorbide compounds are injected into a host and accumulate in tumor tissue to a higher degree than surrounding normal tissues. When the pyropheophorbide compounds are exposed to a particular wavelength of light the compounds become cytotoxic and destroy the tumor or diseased tissue without causing irreversible normal tissue damage. The pyropheophorbide compounds have shown improved results as compared to drugs currently used in photodynamic therapy. Further, they absorb light further in the red, optimizing tissue penetration mad are retained in the skin for short time periods relative to other drugs used in photodynamic therapy.

Abstract: An apparatus for clogging blood vessels of an eye fundus includes an illuminating optical system (1) for illuminating an eye fundus of a subject, who has been given an injection of an infrared fluorescent agent, with infrared rays of light and exciting the infrared fluorescent agent so as to generate infrared fluorescence, a photographic optical system (2) for observing and photographing the eye fundus, and a projecting optical system (21) for projecting a laser beam of light having a specific wavelength onto the subject who has been also given an injection of a photosensitive substance which undergoes a photochemical change by the laser beam. In the apparatus, while a region which emits infrared fluorescence is being observed, the laser beam is projected onto the photosensitive substance so as to clog blood vessels of a diseased part in the depth of the eye fundus.