Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.

Abstract: The invention relates to a family of dyes which fluoresce in the UV-VIS, far red and near infrared wavelengths of the spectrum and possess asymmetric lipophilic alkyl chains. The dyes of the invention are soluble in commercially available membrane staining dyes, are useful as probes for rapidly staining lipophilic structures such as membranes in cells or isolated from cells, and are well-retained therein. Methods of utilizing the dyes to detect stained cells both in vivo and in vitro are also disclosed.

Abstract: The invention provides compositions and methods for the detection of biological targets, (e.g. nucleic acids and proteins) by nucleic acid-templated chemistry, for example, by generating fluorescent polymethine dyes.

Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.

Abstract: A bis(indolestyryl) compound. The bis(indolestyryl) compound has formula (I): wherein A and B comprise benzene, naphthalene, or heterocyclic ring containing O, S, or N, R1 and R1? are H, halogen, C1-5 alkyl, nitro, ester, carboxyl, sulfo, sulfonamide, amide, sulfo ester, C1-3 alkoxy, amino, alkylamino, cyano, C1-6 alkylsulfonyl, or C2-7 alkoxy carbonyl, R2, R2?, R3, and R3? comprise H, C1-6 alkyl, C6-18 aryl, C2-6 alkenyl, C3-6 cycloalkenyl, or C3-6 cycloalkyl, R4 is H, C1-5 alkyl, hydroxyl, halogen, or alkoxy, R5 and R5? comprise H, halogen, C1-5 alkyl, nitro, C1-3 alkoxy, amino, cyano, C1-6 alkylsulfonyl, or C2-7 alkoxy carbonyl, W comprises oxygen, sulfur, selenium, —NR, or —C(CH3)2, n is 1˜18 and Z1 and Z2 are different and comprise an anion or an anionic organometallic complex with +1 or +2 valence, wherein R bonded to nitrogen is C1-4 alkyl.

Abstract: The present invention relates to novel isatin derivatives, pharmaceutical compositions comprising the isatin derivatives of the invention, methods of preparing the isatin derivatives of the invention, their use in the treatment of neurodegenerative diseases and for the regeneration or prevention of degeneration of lesioned and damaged neurons, and methods of treatment of neurodegenerative diseases and for the regeneration or prevention of degeneration of lesioned and damaged neurons.

Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).

Abstract: The present invention provides dichromic fluorescent compounds, as well as processes for making and methods for using the dichromic fluorescent compounds.

Abstract: The present invention relates to a endothelin receptor antagonist conjugate of the formula (I) wherein R2 is an alkoxy group and one of R1 and R3 represents an alkoxy group and the other represents a group of the formula: (OCH2CH2)n—NH—X, wherein n is an integer of 1 to 100 and X represents a fluorescent dye and tautomers thereof. Furthermore, the present invention relates to a diagnostic composition comprising the compounds of the invention. The present invention also relates to the use of the compounds of the invention for the preparation of a diagnostic composition for the diagnosis of cancer, the evaluation of cancer biology and/or monitoring of anticancer therapy. In a further aspect, the present invention relates to kits comprising the compounds of the invention.

Abstract: The present application describes modulators of CCR3 of formula (I): A—E—NR1—G??(I) or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.

Abstract: An optical recording medium provided with a recording layer that comprises a cation represented by the following general formula (1) and a chelate compound of an azo compound represented by the following general formula (2) and a metal. In the formulas, R1-R4 each independently represent a monovalent group represented by Chemical Formula (10) below or other groups, R5 and R6 each independently represent an optionally substituted alkyl group or other groups, R7 represents a hydrogen atom or other groups, Q1 and Q2 each independently represent a group that forms an optionally substituted benzene ring or other groups, at least one from among R1-R4 is a monovalent group represented by Chemical Formula (10) below, [Chemical Formula 2] [CH2?CH—CH2???(10) and at least one of Ar1 and Ar2 is an aryl or other group having a substituent capable of coordinating with a metal atom.

Abstract: This invention relates to new fluorescent chemical entities, especially fluorescent molecules that comprise biocompatible N,N-disubstituted sulfonamide fluorochromes. This invention also relates to the corresponding reactive versions of such molecules. This invention also relates to the corresponding conjugates with moieties such as peptides, proteins, various biomolecules, carbocyclic and heterocyclic compounds, sugars, and their uses thereof.

Abstract: An optical recording material comprising at least one kind of a cyanine compound represented by the following general formula (I): wherein ring A and ring B each independently represent a benzene ring or a naphthalene ring which may have a substituent; R1 represents a group represented by the general formula (II), (II?) or (II?); R2, R3 and R4 each independently represent a hydrogen atom, an organic group having 1 to 30 carbon atoms, or a group represented by the general formula (II), (II?) or (II?); R3 and R4 may be linked together to form a ring structure; Y1 and Y2 each independently represent an organic group having 1 to 30 carbon atoms or a group represented by the general formula (III); X represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, a phenyl group which may have a substituent, a benzyl group which may have a substituent, or a cyano group; Anm- represents an m-valent anion; m is 1 or 2; and p represents a coefficient keeping the charge neutral.

Abstract: The present invention relates to novel catecholamine derivatives of Formula I, to processes for their preparation, pharmaceutical compositions containing them and to their use in therapy.

Abstract: The invention encompasses fluorescent cyanine dyes and methods of using such dyes. In particular, the invention encompasses near infrared polymethine cyanine dyes.

Abstract: The present invention relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.

Abstract: Disclosed is a trimethine dimer compound represented by the following general formula (I) and optical recording medium containing such a compound in a recording layer. (I)(In the formula, symbols are as in the description. When both Xa2 and Xb2 are imino groups, one of Xa1, Xb1, Xa3 and Xb3 is necessarily a 1-alkyl-1-benzylmethylene group which may have a substituent, a 1,1-dibenzylmethylene group which may have a substituent or a cycloalkane-1,1-diyl group having 3 to 6 carbon atoms which may have a substituent.

Abstract: The present disclosure provides drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-cleavable substrate conjugates, and to methods of treatment using them.

Abstract: A matched set of fluorescent dyes is provided, wherein each dye of the set is capable of covalent attachment to a protein and wherein each of the dyes has a molecular structure and a charge that is matched one with the other, such that relative electrophoretic mobility of a protein labeled with one dye of the set is the same as the electrophoretic mobility of the protein labeled with a different dye of the set. The matched set comprises at least two different fluorescent dyes of formula: wherein n is 1, 2, or 3; Z1 and Z2 independently represent the carbon atoms necessary to complete a phenyl or naphthyl ring system; one of groups R1 and R2 is a target bonding group; remaining group R1 or R2 is selected from —(CH2)4—W or —(CH2)r—H; group R3 is hydrogen, except when either R1 or R2 is —(CH2)r—H, in which case R3 is W; and W is selected from sulphonic acid and sulphonate.

Abstract: The present invention provides novel organic compounds, which absorb the light in the ultra violet and the infrared regions, have improved light tolerance and solubility in solvents, and have thermal tolerance suitable for uses to which the organic compounds are applied, and provides uses of the same. The above objects are solved by providing indolenine compounds and methine dyes, which have a bis-indolenine skeleton composed of two indolenine rings linked together at their respective C-3 positions via a divalent linking group, and by providing optical recording media containing the methine dyes.

Abstract: A compound of the formula (I) wherein the variables are defined herein. Methods of dye-labeling biomolecules with the compound of formula (I) and dye-labeled biomolecules are also provided.

Abstract: The invention relates to a method for purification of synthetically-produced compounds, comprising a betaine structure in the molecule, for example, indocyan green, characterized in that reaction by-products, starting materials and/or other impurities such as NaI used during production are separated by extraction.

Abstract: Dibenzorhodamine compounds having the structure are disclosed, including nitrogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, —CH2OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.

Abstract: The present invention relates to novel catecholamine derivatives of Formula I, to processes for their preparation, pharmaceutical compositions containing them and to their use in therapy.

Abstract: A cyanine compound is represented by formula (I): A1: benzene or naphthalene ring. A3: 5- or 6-membered ring. R1, R2: hydrogen atom and the like. R7: an alkyl group and the like. R12: a substituent by formula (II) or (II?). R20: a hydrogen atom and the like. Anq-: a q-valent anion. q: 1 or 2; p: a coefficient for neutral charge. In formula (II): bond between L and T is a double, conjugated double, or triple bond. L: carbon atom. T: carbon, oxygen, sulfur, or nitrogen atom. x, y, z: 0 or 1. s: 0-4. R13: hydrogen atom and the like. R14, R15, and R16: hydrogen atom and the like. In formula (II?), the bond between L? and T? is a double or conjugated double bond. L?: carbon atom. T?: carbon, oxygen, nitrogen atom. s?: 0-4. Ring containing L? and T?: 5-membered ring, may contain a heteroatom.

Abstract: 3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Such compounds are useful for modulating activity of a 5-HT1A receptor (agonizing or antagonizing) in a patient. These compounds are further useful for inhibiting binding to a serotonin receptor. Methods of using the 3-amino chroman and 2-amino tetralin compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety, are also disclosed.

Abstract: The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.

Abstract: A method of preparing a sultine of formula (V) from a dihalogeno compound of formula (IV) is provided. The method comprises reacting the dihalogeno compound (IV) with a hydroxymethanesulfinate salt in a DMSO solvent, wherein: R1, R2, R3 and R4 are each independently selected from hydrogen, hydroxyl, C1-20alkyl, C1-20alkoxy, amino, C1-20alkylamino, di(C1-20alkyl)amino, halogen, cyano, thiol, C1-20alkylthio, nitro, C1-20alkylcarboxy, C1-20alkylcarbonyl, C1-20alkoxycarbonyl, C1-20alkylcarbonyloxy, C1-20alkylcarbonylamino, C5-20aryl, C5-20arylalkyl, C5-20arylalkoxy, C5-20heteroaryl, C5-20heteroaryloxy, C5-20heteroarylalkoxy or C5-20heteroarylalkyl; and X is Cl, Br or I.

Abstract: A method of effecting a one-pot conversion of a tetrahydronaphthalic anhydride to a benzisoindolenine salt is provided. The method comprises heating the tetrahydronaphthalic anhydride with a reagent mixture comprising ammonium nitrate.

Abstract: 3H-Benzo[e]indol-4,5-dione derivatives with antitumor activity, the processes for the preparation thereof and pharmaceutical compositions containing them.

Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: The present invention provides prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group containing a sulfonic acid containing phenyl carbamate, in which the protecting group confers enhanced water solubility upon the prodrug, and in which the prodrug also has a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody, and for the therapeutic use of such prodrug and conjugates, and for processes for preparing such prodrugs and conjugates.

Abstract: The present invention provides a process for preparation of 1-[9H-carbazol-4-yloxy]-3-[{2-(2-(methoxy)phenoxy)-ethyl}-amino]-propan-2-ol,a compound of formula 1 in racemic form or in the form of optically active R or S enantiomer or its pharmaceutically acceptable salt, comprising, reacting 4-(oxiranylmethoxy)-9H-carbazole, a compound of formula (2) or the R or S enantiomer thereof with a compound of formula (5), wherein R1 is benzyl or substituted benzyl group, in an aprotic organic solvent in presence of a catalyst to obtain a compound of formula (6), or the R or S enantiomer thereof, wherein R1 is as defined above. The resultant compound of formula (6) is subjected to debenzylation reaction by catalytic hydrogenation to obtain the compound of formula (1), if desired converting the resultant compound of formula (1) to a pharmaceutically acceptable salt thereof.

Abstract: The invention provides novel compounds useful as intermediates for the production of polymethine compounds containing a desired counter ion with high purity and in high yields. Thus provided are polymethine ether compounds of the general formula (I) given below and a method of producing polymethine compounds which comprises bringing those compounds into contact with an acid. In the above formula, R represents an alkyl group, an alkoxyalkyl group or an aryl group which may optionally be substituted, R1 and R2 each independently represents a hydrogen atom, halogen atom, nitro group, alkyl group, alkoxyalkyl group, alkoxy group or alkoxyalkoxy group and R1 and R2 may be bound to each other to form a ring; R3 represents an alkyl group, which may optionally be substituted; L is an alkylene group required for the formation of a ring structure; and X represents a hydrogen atom, halogen atom, alkoxy group, aryloxy group, alkylthio group, arylthio group or substituted amino group.

Abstract: A medicament having inhibitory activity against NF-?B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.

Abstract: The present invention provides a cost-effective, industrially feasible process for the manufacture of crystalline Carvedilol Form-II using novel Carvedilol salts comprising a step of reacting 4-(2,3-epoxy propoxy)carbazole (II) with 2-(2-methoxy phenoxy)ethyl amine (III) followed by acidification with mineral acid in presence of an organic solvent to yield acid addition salts, treatment of the said salts with base(s) in presence of organic solvent(s), water and isolation from the organic solvent(s) followed by crystallization from ethyl acetate.

Abstract: A squarylium dye represented by formula (1): wherein A1 and B1 each independently represents a ring structure, and R1 and R2 each independently represents a substituent having a carbon number of 1 to 12.

Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.

Abstract: The present disclosure provides cytoxic compounds useful as drugs or prodrugs and to drug-cleavable substrate conjugates where the drug and cleavable substrate are optionally linked through a self-immolative linker.

Abstract: A method of forming a CBI CC-1065 analog utilizes NH2 as a starting material, where R3 is H or alkyl and R6 is H, substituted or unsubstituted lower alkyl, cyano, or alkoxy. Intermediates (I) are used and are claimed.

Abstract: Methods for treating a neoplastic disease with an antibody-cytotoxin conjugate molecule, methods of synthesizing an antibody-cytotoxin conjugate molecule are provided. Compounds that are useful as antibody-cytotoxin conjugate molecule or useful in the synthesis of these molecules are also provided.

Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytotoxic drugs in a targeted fashion.

Abstract: A photosensitive composition includes a cyanine dye that has, on a methine chain thereof, a substituent which is a cation moiety of an onium salt structure.

Abstract: The present invention relates to a recording medium consisting of transparent substrate, recording layer, reflective layer, and protective layer, wherein the recording layer comprising at least one organic optical dye of structural formula (1): wherein each of R1, R2, R3, R4, R5, R6, X, and Y is defined as herein. The recording medium of present invention is useful as a write once recording medium, particularly is using as a recording medium for laser wavelength of 630 to 660 nm.

Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).

Abstract: An object of the present invention is to provide a composite material formed of an organic compound and an inorganic compound, and has an excellent carrier transporting property, an excellent carrier injecting property to the organic compound, as well as excellent transparency. A composite material of the present invention for achieving the above object is a composite material of an organic compound represented in the general formula below, and an inorganic compound. For the inorganic compound, an oxide of a transition metal, preferably an oxide of a metal belonging to groups 4 to 8 of the periodic table, in particular vanadium oxide, tantalum oxide, molybdenum oxide, tungsten oxide, rhenium oxide, and ruthenium oxide, can be used.

Abstract: A TBET cassette including at least one xanthine- or pyronin-based compound as a donor or acceptor is disclosed. Also, a method of TBET cassette design in which four criteria may be used is provided. TBET cassettes may be used to label biological molecules, in clothing dyes, and in cosmetics.

Abstract: According to the present invention, there is provided a near infrared ray absorbing material comprising at least a first compound having a spectral absorption maximum wavelength of 470 nm or less in a range of 270 to 1600 nm in solution, and a second compound represented by the following formula (II-1) or (II-2). where in the formulas, R201, R202, R211, R212, R221, and R222 each represent, independently, a hydrogen atom, an aliphatic group, an aromatic group, or a heterocyclic group linked via a carbon atom; Z201 and Z202 represent a nonmetal atomic group necessary for forming a nitrogen-containing heterocycle; R213 to R216 and R223 to R226 represent a hydrogen atom or a substituent.

Abstract: Compounds of formula (I): [in which: X is a group of formula >CR1R2 or >SO2; Y is a group of formula >NH or >CR1R2; Z is a group of formula >C?O or >CH2 or a direct bond; R1 is hydrogen and R2 is hydrogen, carboxy or hydroxy; or R1 and R2 together represent an oxo group, a methylenedioxy group or a hydroxyimino group; R3 is hydrogen or lower alkyl; R4 represents two hydrogen atoms, or an oxo or hydroxyimino group; R5 is hydrogen, lower alkyl or halogen; R6 is hydrogen, lower alkoxy or carboxy; R7 and R8 are each hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts and esters thereof can be used for the treatment or prophylaxis of acute or chronic neurodegenerative diseases or conditions such as Alzheimer's Disease, Parkinson's Disease, Huntington's Chorea, Multiple Sclerosis or the sequelae to acute ischaemic events such as heart attack, stroke or head injury and for protection against ischaemic damage to tissues of peripheral organs.