Abstract: Small molecule agonists, partial agonists, and antagonists for the TrkA receptor are described. The compounds are gambogic amines, where the carboxylic acid group of gambogic acid (CO2H) has been replaced by an amine group (CH2NR1R2). In some embodiments, the compounds selectively bind to TrkA but not TrkB or C, robustly induce its tyrosine phosphorylation and downstream signaling activation including Akt and MAP kinases. Further, they can strongly prevent glutamate-induced neuronal cell death and provoke prominent neurite outgrowth in PC12 cells. Gambogic amines specifically interact with the cytoplasmic juxtamembrane domain of TrkA receptor and trigger its dimerization. Administration of these compounds in can substantially diminishes Kainic acid-triggered neuronal cell death and decrease infarct volume in transient middle cerebral artery occlusion (MCAO) model of stroke.

Abstract: It is an object of the present invention to provide an on-off type fluorescent compound (a fluorescence-producing molecule system) used in gene analyses, which is highly stable (namely, being active for a long period of time) and highly sensitive, and which enables amplification of a trace amount of gene signal and observation thereof. The present invention provides a nonfluorescent molecule having a fluorescent substance skeleton such as fluorescein skeleton and having a group represented by —O—C(Y1)(Y2)-N3 wherein each of Y1 and Y2 represents a hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, an alkoxy group containing 1 to 6 carbon atoms, an aryl group containing 6 to 10 carbon atoms, or a cyano group, in the molecule.

Abstract: A chromene compound represented by the following formula (1): wherein R1 and R2 are each independently an alkyl group having 1 to 9 carbon atoms, cycloalkyl group having 3 to 12 carbon atoms, perfluoroalkoxy group having 1 to 6 carbon atoms, aralkyl group having 7 to 11 carbon atoms, aralkoxy group having 7 to 11 carbon atoms, aryl group having 6 to 10 carbon atoms, aryloxy group having 6 to 10 carbon atoms or alkoxy group having 1 to 6 carbon atoms, with the proviso that R1 and R2 cannot be alkoxy groups having 1 to 6 carbon atoms at the same time; R3 and R4 are each independently a hydrogen atom, hydroxyl group, alkyl group having 1 to 9 carbon atoms, cycloalkyl group having 3 to 12 carbon atoms, alkoxy group having 1 to 6 carbon atoms, aralkyl group having 7 to 11 carbon atoms, aralkoxy group having 7 to 11 carbon atoms, aryl group having 6 to 10 carbon atoms or aryloxy group having 6 to 10 carbon atoms; R1 and R3 or R2 and R4 may be bonded together to form an alkylene group or alkylenedioxy group; R5

Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.

Abstract: The present invention relates to photochromic benzopyrans and to the use thereof in plastics of all kinds, especially for ophthalmic purposes. The inventive compounds are photochromic benzopyran compounds in which a polycyclic aromatic is joined to the 5 and 6 positions of a benzopyran, where the bond in the 6 position is direct and the bond in the 5 position is via a mono- or diatomic bridge.

Abstract: The present invention relates to photochromic benzopyrans and to the use thereof in plastics of all kinds, especially for ophthalmic purposes. The inventive compounds are photochromic benzopyran compounds in which a polycyclic aromatic is joined to the 5 and 6 positions of a benzopyran, where the bond in the 6 position is direct and the bond in the 5 position is via a mono- or diatomic bridge.

Abstract: A chromene compound represented by the following formula (1), wherein, “A” is an annulated ring, R1 and R2 are hydrogen atoms, hydroxyl groups or the like groups, R3, R4, R5 and R6 are substituents such as hydroxyl groups or the like groups, “a” and “b” are, respectively, integers of 0 to 4, and “c” and “d” are, respectively, integers of 0 to 5. The chromene compound is a photochromic compound developing a color of a neutral tint, and has a high color density per a unit amount.

Abstract: A chromene compound represented by the following formula (1), wherein R1, R2, R3 and R4 are, respectively, hydrogen atoms, alkyl groups, aryl groups, or the like groups under a condition that at least two of R1 to R4 are not hydrogen atoms, R5, R6, R7 and R8 are, respectively, alkyl groups, aryl groups or the like groups, m and n are, respectively, integers of 0 to 4, and x and y are, respectively, integers of 0 to 5. The compound has a basic structure in which a 6-membered ring is condensed in a form of shearing a carbon atom at the fifth position and a carbon atom at the sixth position of a 2H-benzo[h]chromene skeleton. Owing to this molecular structure, the chromene compound of the invention develops a yellow color or a neutral tint by itself, exhibits favorable photochromic properties, and does not exhibit deteriorated photochromic properties even when it is used in combination with a photopolymerization initiator.

Abstract: Novel ent-kaurene diterpene compound and its derivatives, their preparation methods and their use. ent-Kaurene diterpene in the present invention could be used as desired intermediates for preparing asymmetric organic compounds and medicaments, and could be used as antitumor agent, anti-inflammatory agent and immune agent etc. The said ent-kaurene diterpene compound could be condensed with hydroxyl compounds to obtain various acetal derivatives, could be reacted with amine compounds to obtain various amino derivatives, and could be reacted with acyl halide or acid anhydride to obtain various acyl derivatives.

Abstract: Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure In addition, methods of making and using the dyes as fluorescent labels are disclosed.

Abstract: It is an object of the present invention to provide an on-off type fluorescent compound used in gene analyses, which is highly stable and highly sensitive, and which enables amplification of a trace amount of gene signal and observation thereof. The present invention provides a compound represented by the following formula (1) or (2): wherein R1 represents an alkyl group containing 1 to 6 carbon atoms, an amino group, an amide group optionally having a protecting group or a substituent, a halogen atom, or a hydrogen atom; R2 independently represents an alkyl group containing 1 to 6 carbon atoms, a halogen atom, or a hydrogen atom; R3 represents an alkyl group containing 1 to 6 carbon atoms, an aryl group, or a hydrogen atom; R4 represents a group containing an oxygen atom, or a hydrogen atom, wherein R3 may bind to R4 to form a ring.

Abstract: Provided herein are inhibitors of CYP17 enzyme. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.

Abstract: Novel compounds based on phenyl-substituted naphtho[1,2-g]chrysene compounds (A) are described. The compounds are obtainable by dimerisation of 3-phenylchroman (isoflavonoid) ring systems (B). Methods of synthesis of the novel dimeric compounds, compositions containing same and use of the dimers as therapeutic agents are also described.

Abstract: Described herein are C5-C6 annelated naphthopyrans that possess at least one electron-withdrawing group. The compounds possess desirable properties such as increased fading kinetics. Also described herein are new methods for synthesizing 2H-chromenes annelated at C5-C6. The methods involve less stringent reaction conditions as well as provide increased reaction yields. The methods permit the synthesis of a wide variety of substituted naphthopyrans that can be temperature sensitive, which was not possible with previous synthetic routes.

Abstract: The invention provides compounds that are A-type procyanidins. The compounds can be prepared by reacting flavylium salts with catechins or analogs thereof, for example, under anhydrous conditions in alcohol.

Abstract: Compounds represented by the general formula (1) wherein R1 and R3 are each independently hydrogen or a carboxyl group and R2 and R4 are each independently hydrogen or a hydroxyl group, or pharmaceutically acceptable salts thereof, which exhibit semaphorin-inhibitory activity and are useful as preventives or remedies for neuropathic and neurodegenerative diseases are provided.

Abstract: A method for preparing A-type procyanidins is provided by reacting flavylium salts with catechins and analogs thereof, under anhydrous conditions in alcohol.

Abstract: A semiconducting layer comprising a non-polymeric quinoid heteroacene compound of the formula (I) wherein X stands for O, S or NR, each of R, R1, R2, R3, R4, R5, R6, R7, R8 being independently selected from hydrogen and an organic residue, or 2 or more thereof together forming one or more annealed rings, which may be substituted or unsubstituted, carbocyclic or helerocyclic, aromatic, quinoid or aliphatic, may be used e.g. for the manufacture of a diode, an organic field effect transistor, an organic thin film transistor, or a device containing a diode and/or an organic field effect transistor and/or organic thin film transistor.

Abstract: Photochromic materials comprising indeno-fused naphthopyrans having a first electron-withdrawing substituent and, in certain non-limiting embodiments, a second electron-withdrawing substituent are disclosed. The photochromic materials according to the various embodiments may display faster fade rates, bathochromic shift, and higher performance ratings compared to comparable indeno-fused naphthopyrans without the electron-withdrawing substituents. Photochromic compositions and articles, such as optical elements, incorporating the photochromic materials are also disclosed.

Abstract: The cytotoxic natural product gambogic acid (GA) competes for BH3 peptide binding sites on several anti-apoptotic members of the Bcl-2 family of proteins and neutralizes the ability of these proteins to suppress release of apoptogenic proteins from isolated mitochondria. Structure-function analysis of GA using analogs suggested a general correlation between BH3 competition and cytoxicity activity. Compositions and methods are provided for using GA and its derivatives for treating cancer and for discovering other compounds that are useful for treating cancer through their interaction with Bcl-2-family proteins.

Abstract: The present invention provides rotenone analogs and methods of making and using them. Labeled with single photon and positron emitting isotopes, the rotenone analogs of the present invention are useful in, for example, clinical imaging applications as tracers to measure cardiac blood flow and detect regions of ischemia.

Abstract: One aspect of the invention relates to novel proanthocyandin compounds that are useful as antiinfective agents. In one embodiment, the invention relates to a pure and isolated compound of formula I or II: For example, compounds of the invention are useful antiviral agents against.

Abstract: Photochromic materials comprising indeno-fused naphthopyrans having substituents comprising a 4-fluorophenyl group and a 4-aminophenyl group bonded to the 3-position of the indeno-fused naphthopyran are disclosed. The photochromic materials may exhibit faster fade rates as compared to similar indeno-fused naphthopyrans without a 4-fluorophenyl group and a 4-aminophenyl group bonded to the 3-position of the indeno-fused naphthopyran. Substituted 2-propyn-1-ols utilized for the synthesis of the indeno-fused naphthopyrans disclosed herein are disclosed. Photochromic compositions and articles, such as optical elements, incorporating the photochromic materials disclosed herein are also disclosed.

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: Fluorescent phenyl xanthene dyes are described that comprise any fluorescein, rhodamine or rhodol comprising a particular C9 phenyl ring. One or both of the ortho groups on the lower C9 phenyl ring is ortho substituted with a group selected from alkyl, heteroalkyl, alkoxy, halo, haloalkyl, amino, mercapto, alkylthio, cyano, isocyano, cyanato, mercaptocyanato, nitroso, nitro, azido, sulfeno, sulfinyl, and sulfino. In one embodiment, halo and/or hydroxy groups are used. Optimal dyes contain a lower C9 phenyl ring in which both ortho groups are the same and the lower ring exhibits some form a symmetry relative to an imaginary axis running from the phenyl rings point of attachment to the remainder of the xanthene dye through a point para to the point of attachment. The phenyl xanthene dyes may be activated. Furthermore, the phenyl xanthene dyes may be conjugated to one or more substances including other dyes.

Abstract: Various non-limiting embodiments disclosed herein relate to photochromic materials having extended pi-conjugated systems, such as an indeno-fused naphthopyran, which comprises a group that extends the pi-conjugated system of the indeno-fused naphthopyran bonded at the 11-position thereof. Further, the photochromic materials according to certain non-limiting embodiments disclosed herein may display hyperchromic absorption of electromagnetic radiation as compared to conventional photochromic materials and/or may have a closed-form absorption spectrum that is bathochromically shifted as compared to conventional photochromic materials. Other non-limiting embodiments relate to photochromic compositions and photochromic articles, such as optical elements, made using the disclosed photochromic materials, and methods of making the same.

Abstract: The present invention provides lipase inhibitors containing dimers having an epigallocatechin gallate (EGCG) unit derived from teas as well as foods and beverages and medicines containing said inhibitors. More specifically, the present invention provides lipase inhibitors containing at least one of proanthocyanidins represented by the formula: wherein R1 and R2 independently represent H or OH, and R3 and R4 independently represent H or a galloyl group; as well as foods and beverages and pharmaceutical compositions containing said lipase inhibitors.

Abstract: The present invention discloses Mulberrofuran G, a method of extracting Mulberrofuran G, as well as various uses of Mulberrofuran G in manufacturing antibacterial medicaments or oral care products or for other antibacterial uses.

Abstract: The present invention discloses a new compound of formula (I), a method of extracting the new compound, as well as various uses of the new compound in manufacturing antibacterial medicaments or oral care products or for other antibacterial uses.

Abstract: Three new acylphloroglucinols, myrtucommulone-D (Compound 1), myrtucommulone-E (Compound 2), myrtucommulone-C (Compound 3), and a known acyphloroglucinol myrtucommulone B (Compound 4) were isolated from a methanolic extract of Myrtus communis L. The structures of compounds 1, 2 and 4 were also unambiguously determined by single X-ray diffraction analysis. The compounds 1-4 were found to be more potent ?-glucosidase inhibitors than the clinically used standards, acarbose and deoxynojirimycin. The compound 3 exhibited the highest activity among all the acylphloroglucinols, with an IC50=35.4±1.15 ?M. The compounds 1 and 2 also exhibited strong antibacterial activities.

Abstract: Certain bis-(coumarin) compounds as well as the products of their intramolecular cyclization including pharmaceutically acceptable salts, hydrates, solvates, clathrates, prodrugs, tautomers and stereoisomers thereof are disclosed. Certain processes and intermediates for the preparation of certain bis-(coumarin) compounds, as well as for the use of these compounds as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diseases and conditions in mammals, especially humans are also disclosed.

Abstract: The present invention relates to novel compounds of the naphthopyran type which have an annelated carbocycle in position 5,6. These compounds are of formula (I) given below: in which A is an alicyclic ring which is optionally annelated with an aromatic ring and in which two adjacent R3 can together form at least one ring, for example a benzo group. These compounds (I) possess interesting photochromic properties. The invention also relates to the method of preparing these compounds (I), as well as their applications as photochromes and compositions and (co)polymer matrices comprising them.

Abstract: Disclosed are novel benzo-, naphtho- and phenanthrochromenes substituted by carbamated or ureated phenyls having the following general formula (I): wherein R1 represents a group their preparation, photochromic compositions and articles containing them. This family of compounds have interesting and useful photochromic properties, especially in terms of absorption band and discoloration speed.

Abstract: The invention relates to chiral compounds of formula I wherein X1,X2,X1,X2,x1,x2,y1,y2,B,C,U1,U2,V1,V2,W1 and W2 have the meaning given in claim 1, to liquid crystal mixtures comprising at least one chiral compound of formula I, to chiral linear or crosslinked liquid crystal polymers obtainable by polymerizing a polymerizade mixture comprising at least one chiral compound of formula I, to the use of chiral compound of formula I and mixtures and polymers obtained thereof in liquid crystal display, active and passive optical elements, adhesives, synthetic resins with anisotropic mechanical properties, cosmetic and pharmaceutical compositions, diagnostics, liquid crystal pigments, for decorative and security applications, nonlinear optics, optical information storage or as chiral dopants, and to a liquid crystal display comprising a mixture comprising at least one chiral compound of formula I.

Abstract: An infrared dye, characterized in that the dye comprises a compound that can be described by molecule 1.

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 specific photochromic heterocyclically annellated indenochromene derivatives and the use thereof in plastics of all types, particularly for ophthalmic applications.

Abstract: Extended rhodamine compounds exhibiting favorable fluorescence characteristics having the structure are disclosed. In addition, novel intermediates for synthesis of these dyes are disclosed, such intermediates having the structure In addition, methods of making and using the dyes as fluorescent labels are disclosed.

Abstract: Sulfonated diarylrhodamine compounds are useful as fluorescent labels of nucleosides, nucleotides, polynucleotides, and polypeptides. The compounds find particular application in the area of fluorescent nucleic acid analysis, e.g., automated DNA sequencing and fragment analysis, detection of probe hybridization in hybridization arrays, detection of nucleic acid amplification products, and the like.

Abstract: Described are novel reversible photochromic indenonaphthopyran compounds, examples of which are 2H-naphtho[1,2-b]pyrans characterized by having a substituted or unsubstituted indeno group fused at the 2,3 positions of the group to the 1 side of the 2H-naphthopyran. The compounds also have substituents at the 3 position of the pyran ring. Substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12, or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formulae: Also described are various substrates, e.g., paper, glass, organic polymeric materials, etc., that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel indenonaphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., indenonaphthopyrans, naphthopyrans, benzopyrans, oxazine-type compounds, etc., are also described.

Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

Abstract: Dibenzorhodamine compounds having the structure 1

Abstract: The present invention relates to specific photochromic heterocyclically annellated indenochromene derivatives and the use thereof in plastics of all types, particularly for ophthalmic applications.

Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined in the specification.

Abstract: Sulfonated diarylrhodamine compounds are useful as fluorescent labels of nucleosides, nucleotides, polynucleotides, and polypeptides. The compounds find particular application in the area of fluorescent nucleic acid analysis, e.g., automated DNA sequencing and fragment analysis, detection of probe hybridization in hybridization arrays, detection of nucleic acid amplification products, and the like.

Abstract: The present invention relates to a process for the synthesis of oxandrolone from mestanolone. The process comprises the steps of: (a) oxidizing mestanolone to form 17&bgr;-hydroxy-17&agr;-methyl-5&agr;-androst-1-en-3-one; (b) hydroxylating the 17&bgr;-hydroxy-17&agr;-methyl-5&agr;-androst-1-en-3-one to form 1&agr;,2&agr;,17&bgr;-trihydroxy-17&agr;-methylandrostan-3-one; (c) cleaving the 1&agr;,2&agr;,17&bgr;-trihydroxy-17&agr;-methylandrostan-3-one to form 17&bgr;-hydroxy-17&agr;-methyl-1-oxo-1,2,-seco-A-nor-5&agr;-androstan-2-oic acid; and (d) reducing the 17&bgr;-hydroxy-17&agr;-methyl-1-oxo-1,2,-seco-A-nor-5&agr;-androstan-2-oic acid to form oxandrolone.

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 C14 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 invention relates to novel naphthopyran-type compounds, which are annelated in position C5-C6 with a seven-membered carbocycle, and which are of formula (I) given below: These compounds (I) possess interesting photochromic properties. The invention also relates to their preparation, their applications as photochromes as well as the compositions and (co)polymer matrices containing them.

Abstract: Described are polymeric matrix compatibilized naphthopyran compounds, examples of which are certain 2H-naphtho[1,2-b]pyrans, 3H-naphtho[2,1-b]pyrans and indeno[2,1-f]naphtho[1,2-b]pyrans each having at least one substituent containing terminal and/or pendant groups selected from hydroxyl, carboxyl, sulfo, sulfono, (meth)acryloxy, 2-(methacryloxy)ethylcarbamyl, epoxy or a mixture thereof. Specific substituents are also present on the naphtho, indeno and/or pyrano portions of the compounds. These compounds may be represented by the following graphic formulae: Also described are various substrates that contain or that are coated with such compounds. Optically clear articles such as contact lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, are also described.

Abstract: The subject invention provides substrates useful for analyzing the metabolic activity in cells by improving the retention of a detectable reporter molecule only in intact cells where a particular enzyme is present. In particular, improved retention results from a two part process involving conjugation of haloalkyl-substituted derivatives of a reporter molecule with intracellular cysteine-containing peptides while unblocking the reporter molecule. The substrates have the form XR-SPACER-REPORTER-BLOCK wherein -BLOCK is a group selected to be removable by action of a specific analyte, to give REPORTER spectral properties different from those of the substrate, -REPORTER- is a molecule that, when no longer bound to BLOCK by a BLOCK-REPORTER bond, has spectral properties different from those of the substrate, -SPACER- is a covalent linkage, and XR- is a haloalkyl moiety that can covalently react with an intracellular thiol (Z-S-H) to form a thioether conjugate (Z-S-R).