Indolocarbazole derivatives, processes for their preparation and their use

Synthesis and elucidation of azamitosene and iminoazamitosene

Condensed diazepinones, process for their preparation, and medicaments containing these compounds

Novel inhibitors of retroviral reverse transcriptace

Disclosed are nucleic acid molecules, and methods of their use, which have a specific structure including a double helical domain and a G-quadruplex domain physically connected by a linker domain which may be nucleosidic or non-nucleosidic. These aptamers demonstrate potent inhibition of phylogenetically diverse primate lentiviral reverse transcriptases, which effect is largely independent of aptamer sequence provided that the aptamer has the specified structure.

Organic electronic device, compounds for same, and terminal

Disclosed are an organic electronic device and a compound thereof, and a terminal.

Bridged compounds as hiv integrase inhibitors

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, χ3, Y, Z, R1, R2 and R3 are defined herein. The N compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Extracellular matrix compositions for tissue regeneration

The invention is compositions of extracellular matrix that comprise mammalian extracellular matrix from two or more tissue sources in a mammal. The invention also includes methods of using these compositions to regenerate tissue or generate new tissue at sites of defects or wounds in mammals.

Novel Indicator Platform

A novel indicator platform comprises a plurality of 1H-lndol-3-yl indicator compounds that are capable of converting to a signalophore compound in response to an external stimulus. In one class of indicator compounds, the resulting signalophores are 2-benzylideneindoline compounds that are formed by an intermolecular Aldol-type process; in a further class of indicator compounds, the resulting signalophores are 10H-indolo[1,2-a]indole compounds that are formed by an intramolecular Aldol-type process. The indicators can be used in a wide array of applications relating, for example, to biological systems or optical data storage.

Materials for organic electroluminescent devices

The present invention relates to 4,4′-substituted spirobifluorenes which are suitable, owing to excellent properties, as functional materials in organic electroluminescent devices. In addition, the present invention relates to a process for the preparation of 4,4′-substituted spirobifluorenes and to the use of these compounds in organic electroluminescent devices.

Light-emitting device material and light-emitting device

Embodiments provide a light emitting device material characterized by containing an anthracene compound represented by the following general formula. where R 19 to R 37 are a hydrogen atom, alkyl group, cycloalkyl group, heterocyclic group or the like; n is 1 or 2; and A is a heteroarylene group or arylene group. Any one of the R 19 to R 27 and any one of the R 28 to R 37 are used for linking with A. The present teachings allow a light emitting device having high luminous efficiency and excellent durability.

Multi-layered gradient vaginal ring

Multi-layered vaginal rings 2 comprising silicone elastomers and pharmaceutically active ingredients are disclosed. The rings comprise a number of layers, at least one of which contains a pharmaceutically active ingredient, and each of which is a silicone elastomer. The multiple layers preferably are produced from these layers of different compositions, including an inner layer 4, a middle layer 5, and an outer layer 6. After extrusion and simultaneous curing, however, the ring 2 includes a contiguous body which comprises a continuous silicone body providing unimpeded diffusion of the pharmaceutically active ingredient from the inner layer (s) 4 to the outer layer (s) 6. Methods of producing these vaginal rings and of using them are also disclosed.

Polymerizable composition, color filter, and method of producing the same, solid-state imaging device, and planographic printing plate precursor, and novel compound

Disclosed is a photopolymerizable composition which contains a photopolymerization initiator (A) that has a partial structure represented by the following Formula (1) and a polymerizable compound (B). In General formula (1), R 3 and R 4 each independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group or an alkoxy group; R 3 and R 4 may form a ring with each other; and X represents OR 5 , SR 6 , or NR 17 R 18 . The photopolymerizable composition is capable of forming a cured film that has high sensitivity, excellent intra-membrane curability and excellent adhesion to a support. The cured film is able to maintain a patterned shape even during post-heating after development and has good pattern formability, while coloring due to heating with passage of time being suppressed.

Inhibition of nfk-b mediated virus replication with specific oligosaccharides

The inventors surprisingly found that specific oligosaccharides are capable of inhibiting viral replication through inhibiting NF-κB activation. The invention thus pertains to a composition comprising pectin (in the form of digalacturonic acid, trigalacturonic acid, polygalacturonic acid), Arabinoxylan from rice bran, β-glucan from bakers yeast, D-Ribose or mixtures there-of for inhibiting viral replication in a mammal with a viral disease.

Treatment and prevention of hiv infection

This invention relates to the long term treatment of HIV infection by intermittently administering a parenteral formulation comprising brecanavir at relatively long time intervals. This invention further concerns pharmaceutical compositions for parenteral administration, comprising micro- or nanoparticles of brecanavir, suspended in an aqueous pharmaceutically acceptable carrier, for the treatment and prophylaxis of HIV infection.

Modified agrin-fragment capable of restoring muscle strength for use as a medicament

Modified agrin fragment having in vivo activity, comprising at least the domains LG2 and LG3 of human agrin in covalently interlinked form and modified in such a way that the fragment cannot be cleaved by neurotrypsin for use as medicament.

Organic light emitting device and flat panel display device comprising the same

Provided are an organic light emitting device including: a substrate; a first electrode; a second electrode; and an organic layer interposed between the first electrode and the second electrode and including an emission layer, wherein one of the first electrode and the second electrode is a reflective electrode and the other is a semitransparent or transparent electrode, and wherein the organic layer includes a layer having at least one of the compounds having at least one carbazole group, and a flat panel display device including the organic light emitting device. The organic light emitting device has low driving voltage, excellent current density, high brightness, excellent color purity, high efficiency, and long lifetime.

HUMAN LYMPHOID TISSUE INDUCER (LTi) CELL COMPOSITIONS AND METHODS OF USE

The invention provides human lymphoid tissue inducer (LTi) cells, methods of producing human lymphoid tissue inducer (LTi) cells, and methods of using human lymphoid tissue inducer (LTi) cells. Such methods include treatment of a subject that would benefit from human lymphoid tissue inducer (LTi) cells, for example, an immunocompromised or immunosuppressed subject.

Processes for the synthesis of bazedoxifene acetate and intermediates thereof

Efficient processes for the synthesis of pharmaceutically useful compounds such as (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate (Formula IX) using cyanomethoxybenzyl halides of Formula III, where X=Halogens e.g., Cl, F, Br, I; G=Any electron donating or electron withdrawing substituent.

Novel Polymorphs of Efavirenz

The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz.

HIV Integrase Inhibitors

The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

Organic compound, anthracene derivative, and light-emitting element, light-emitting device, and electronic device using anthracene derivative

Objects of the present invention are to provide novel anthracene derivatives and novel organic compounds; a light-emitting element that has high emission efficiency; a light-emitting element that is capable of emitting blue light with high luminous efficiency; a light-emitting element that is capable of operation for a long time; and a light-emitting device and an electronic device that have lower power consumption. An anthracene derivative represented by a general formula (1) and an organic compound represented by a general formula (17) are provided. A light-emitting element that has high emission efficiency can be obtained by use of the anthracene derivative represented by the general formula (1). Further, a light-emitting element that has a long life can be obtained by use of the anthracene derivative represented by the general formula (1).

Novel organic compound and organic light-emitting device

A novel organic compound suitable for blue light emission and an organic light-emitting device containing the novel organic compound are provided. An organic compound represented by the following general formula (1) wherein R 1 to R 18 independently denote a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group.

Novel methods for the preparation of p2x7r antagonists

Disclosed are novel methods for the synthesis of N-substituted indol-3-yl-alkylamide compounds which act as P2X7R antagonists, said methods involving the rearrangement of an oxime intermediate.

Methods and Compositions for Treatment of Human Immunodeficiency Virus Infection with Conjugated Antibodies or Antibody Fragments

The present invention concerns methods and compositions for treatment of HIV infection in a subject. The compositions may comprise a targeting molecule against an HIV antigen, such as an anti-HIV antibody or antibody fragment. The anti-HIV antibody or fragment may be conjugated to a variety of cytotoxic agents, such as doxorubicin. In a preferred embodiment, the antibody or fragment is P4/D10. Other embodiments may concern methods of imaging, detection or diagnosis of HIV infection in a subject using an anti-HIV antibody or fragment conjugated to a diagnostic agent. In alternative embodiments, a bispecific antibody with at least one binding site for an HIV antigen and at least one binding site for a carrier molecule may be administered, optionally followed by a clearing agent, followed by administration of a carrier molecule conjugated to a therapeutic agent.

PESTICIDAL COMPOSITIONS

This document discloses molecules having the following formula (“Formula I”): 3. A molecule according to wherein(a) X is CR8;(b) R1 is H;(c) R2 is H;(d) R3 is H;{'sub': 1', '3, '(e) R4 is Cor CH;'}{'sub': 1', '6, '(f) R5 is H or unsubstituted C-Calkyl;'}(g) R6 is O;{'sub': 1', '6', 'n', '1', '6', '1', '6', 'n', '1', '6', '1', '6', '1', '6, '(h) R7 is (unsubstituted C-Calkyl)S(O)(unsubstituted C-Calkyl), (unsubstituted C-Calkyl)S(O)(unsubstituted C-Calkenyl), O(unsubstituted C-Calkyl), (C-Calkyl);'}(i) R8 is H or F; and(k) n is 0, 1, or 2.4. A molecule according to or in the form of a pesticidally acceptable acid addition salt claim 2 , salt derivative claim 2 , or solvate.5. A molecule according to or having at least one H.6. A molecule according to or having at least one C.7. A molecule according to or that is a resolved stereoisomer.8. A composition comprising a molecule according to or and at least one member of the Insecticide Group claim 2 , Acaricide Group claim 2 , Nematicide Group claim 2 , Fungicide Group claim 2 , or Herbicide Group.9. A composition comprising a molecule according to or and at least one biopesticide.10. A composition comprising a molecule according to or and at least one of the following compounds:(a) 3-(4-chloro-2,6-dimethylphenyl)-4-hydroxy-8-oxa-1-azaspiro[4,5]dec-3-en-2-one;(b) 3-(4′-chloro-2,4-dimethyl[1,1′-biphenyl]-3-yl)-4-hydroxy-8-oxa-1-azaspiro[4,5]dec-3-en-2-one;(c) 4-[[(6-chloro-3-pyridinyl)methyl]methylamino]-2(5H)-furanone;(d) 4-[[(6-chloro-3-pyridinyl)methyl]cyclopropylamino]-2(5H)-furanone;(e) 3-chloro-N2-[(1S)-1-methyl-2-(methylsulfonyl)ethyl]-N1-[2-methyl-4-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]-1,2-benzenedicarboxamide;(f) 2-cyano-N-ethyl-4-fluoro-3-methoxy-benenesulfonamide;(g) 2-cyano-N-ethyl-3-methoxy-benzene sulfonamide;(h) 2-cyano-3-difluoromethoxy-N-ethyl-4-fluoro-benzene sulfonamide;(i) 2-cyano-3-fluoromethoxy-N-ethyl-benzenesulfonamide;(j) 2-cyano-6-fluoro-3-methoxy-N,N-dimethyl-benzenesulfonamide ...

BICYCLIC TETRAHYDROPYRROLE COMPOUNDS

The present invention relates to substituted bicyclic tetrahydropyrrole compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals. 2. The method according to claim 1 , characterized in that Rrepresents a hydrogen atom; an unbranched or branched claim 1 , saturated or unsaturated claim 1 , optionally at least mono-substituted aliphatic radical; a saturated or unsaturated claim 1 , optionally at least mono-substituted claim 1 , optionally at least one heteroatom as ring member containing cyclyl group claim 1 , which may be condensed with an optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched alkyl-cycloalkyl group in which either the alkyl group and/or the cycloalkyl group is optionally at least mono-substituted; a branched or unbranched claim 1 , saturated or unsaturated claim 1 , optionally at least mono-substituted alkyl-aryl group in which the aryl group may be condensed with another claim 1 , optionally at least mono-substituted mono- or polycyclic ring system; a branched or unbranched claim 1 , saturated or unsaturated claim 1 , optionally at least mono-substituted alkyl-heterocyclyl group in which the heterocyclyl group is optionally condensed with another claim 1 , at least mono-substituted mono- or polycyclic ring system; an optionally claim 1 , at least mono-substituted benzhydryl group; a (C═O)—Rgroup; a (C═O)—ORgroup; a (SO)—Rgroup; a (C═O)—NRRgroup;wherein the bond between Y and Z is unsaturated (Y═Z),{'sup': 6', '7', '7a', '8', '9', '10', '10a', '10', '10a, 'sub': 2', '2', '2', '2, 'with Y representing CH and Z representing C—R; C—CHRR; a C—(C═O)—Rgroup; a C—CH(SO)—Rgroup; a C—CH(SO)—NRRgroup; or a C—(C═O)—NRRgroup;'}{'sup': 2', '3', '4', '5', '5a', '6', '7', '7a', '8', '9', '10', '10a, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'R, R, R, R, R, R, R, R, R, R, Rand R, ...

2-PHENYL BENZOYLAMIDES

Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein. 2. A compound according to wherein Ris —C(O)—N—RRand q is 0.5. A compound according to wherein p is 0 and Ris hydrogen or (C-C)alkyl.6. A compound according to wherein Ris —C(O)—O—(C-C)alkyl.7. A compound according to wherein m and n are each independently 0 or 1 and Rand Rare each independently (C-C)alkyl claim 6 , (C-C)alkoxy or trifluoromethyl.8. The compound:Ethyl (1R)-1-({2-[3-(Dimethylcarbamoyl)-4-({[6-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-{[(4′-isopropoxybiphenyl-2-yl)carbonyl]amino}phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl 1-({2-[3-(dimethylcarbamoyl)-4-({[5-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl 7-({2-[3-(dimethylcarbamoyl)-4-({[5-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-7-carboxylate;Ethyl 7-({2-[3-(dimethylcarbamoyl)-4-({[6-methyl-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-6,7-dihydro-5H-cyclopenta[b]pyridine-7-carboxylate:Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-({[5-methoxy-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-({[6-methoxy-4′-(trifluoromethyl)biphenyl-2-yl]carbonyl}amino)phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl (1R)-1-({2-[3-(dimethylcarbamoyl)-4-{[(4′-isopropoxy-5-methylbiphenyl-2-yl)carbonyl]amino}phenyl]acetoxy}methyl)-2-methyl-3-oxoisoindoline-1-carboxylate;Ethyl 7-({2-[3-(dimethylcarbamoyl)-4-{[(4′-isopropoxybiphenyl-2-yl)carbonyl]amino}phenyl]acetoxy}methyl ...

Solid dispersion comprising an anti-hiv agent

The present invention relates to solid dispersions comprising a compound of formula or a salt, a solvate or a solvate of a salt thereof, dispersed in a polymeric, inert, non-toxic, pharmaceutically acceptable excipient.

PHARMACEUTICALLY ACCEPTABLE SALTS OF THYMODEPRESSIN AND PREOCESSES FOR THEIR MANUFACTURE.

The present invention relates to pharmaceutically acceptable crystalline and amorphous salts of D-isoglutamyl-D-tryptophan as well as processes for their manufacture, pharmaceutical compositions comprising them, and their uses in the preparation of pharmaceutical compositions for the treatment of various conditions and/or diseases. In particular, the present invention relates to D-isoglutamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1). 120.-. (canceled)3235.-. (canceled) The present invention relates to novel crystalline and amorphous pharmaceutically acceptable salts of D-isoglutamyl-D-tryptophan. In particular, the present invention relates to D-isog!utamyl-D-tryptophan potassium salt (1:1), D-isoglutamyl-D-tryptophan lithium salt (1:1), D-isoglutamyl-D-tryptophan calcium salt (2:1), D-isoglutamyl-D-tryptophan magnesium salt (2:1), and D-isoglutamyl-D-tryptophan organic ammonium salts (1:1) which have improved properties over amorphous D-isoglutamyl-D-tryptophan, crystalline D-isoglutamyl-D-tryptophan and D-isoglutamyl-D-tryptophan disodium salt. The present invention also relates to processes for the manufacture of these novel salts of D-isoglutamyl-D-tryptophan.The compound D-isoglutamyl-D-tryptophan (also known as H-D-iGlu-D-Trp-OH or Thymodepressin) is a synthetic hemoregulatory dipeptide having the following formula:Thymodepressin is the free diacid having Chemical Abstracts Service (CAS) Registry Number® of 186087-26-3. U.S. Pat. No. 5,736,519 discloses H-D-iGlu-D-Trp-OH and a process for its preparation wherein it is purified by ion exchange chromatography. It is an immunosuppressant and selectively inhibits proliferation of hemopoietic precursor cells and stimulates granulocyte and lymphocyte apoptosis (Sapuntsova, S. G., et al. (May 2002), Bulletin of Experimental ...

AMINOBENZENE COMPOSITIONS AND RELATED DEVICES AND METHODS

Oligomers and/or polymers comprising a backbone comprising arylamine and fluorinated alkyleneoxy moieties which may be crosslinked. Ink formulations and devices can be formed from the oligomers or polymers, or corresponding monomers. Doped compositions can be formed. Charge injection and transport layers can be formed. Improved stability can be achieved in organic electronic devices such as OLEDs and OPVs. 1. A composition comprising a polymeric or oligomeric backbone comprising at least one repeat moiety comprising at least one O-arylamine , and at least one repeat moiety comprising at least one fluorinated alkyleneoxy.2. The composition of claim 1 , wherein the repeat moiety comprising O-arylamine and the repeat moiety comprising fluorinated alkyleneoxy are alternating moieties.3. The composition of claim 1 , wherein the O-arylamine comprises triarylamine.4. The composition of claim 1 , wherein the O-arylamine moiety comprises at least two nitrogen atoms.5. The composition of claim 1 , wherein the fluorinated alkyleneoxy comprises a C-Calkylene ether.6. The composition of claim 1 , wherein the fluorinated alkyleneoxy comprises a fluorinated C-Cvinyl ether.7. The composition of claim 1 , wherein the fluorinated alkyleneoxy comprises a trifluoroalkyleneoxy moiety.8. The composition of claim 1 , wherein the composition comprises a soluble claim 1 , linear polymer comprising the O-arylamine and the fluorinated alkyleneoxy.9. The composition of claim 1 , wherein the composition is crosslinked.10. An oligomer or polymer comprising repeat units represented by{'br': None, 'sup': '1', '\ue8a0O—Ar\ue8a0 and\u2003\u2003(I)'}{'br': None, 'sup': 1', '2', '2, '\ue8a0O—R—O—Ar—O—R\ue8a0\u2003\u2003(II)'}wherein,{'sup': '1', 'Arcomprises arylamine,'}{'sup': '2', 'Arcomprises an aryl, and'}{'sup': 1', '2, 'sub': 1', '10, 'Rand Rare independently selected from C-Cfluorinated alkylenes.'}11. The oligomer or polymer of claim 10 , wherein the repeat units (I) and (II) are alternating. ...

Aromatic Amine Compound, and Light-Emitting Element, Light-Emitting Device, and Electronic Device Using the Aromatic Amine Compound

Novel aromatic amine compounds are provided. Light-emitting elements having high emission efficiency and high reliability are provided. Further, light-emitting devices and electronic devices using the light-emitting devices are provided. Specifically, an aromatic amine compound represented by the general formula (1), and light-emitting elements, light-emitting devices and electronic devices that are formed using the aromatic amine compound represented by the general formula (1) are provided. By using the aromatic amine compound represented by the general formula (1) for light-emitting elements, light-emitting devices and electronic devices, the light-emitting elements, light-emitting devices and electronic devices can have high emission efficiency. 125-. (canceled)28. The aromatic amine compound according to claim 27 ,{'sup': 1', '1, 'wherein Arand Arfurther comprise independently a substituent comprising an aryl group comprising 6 to 13 carbon atoms or a substitute comprising an alkyl group comprising 1 to 4 carbon.'}30. The aromatic amine compound according to claim 29 ,{'sup': 1', '2, 'wherein Arand Arfurther comprise independently a substituent comprising an aryl group comprising 6 to 13 carbon atoms or a substitute comprising an alkyl group comprising 1 to 4 carbon.'}32. The aromatic amine compound according to claim 31 ,{'sup': 1', '2, 'wherein Arand Arfurther comprise independently a substituent comprising an aryl group comprising 6 to 13 carbon atoms or a substitute comprising an alkyl group comprising 1 to 4 carbon.'}34. The aromatic amine compound according to claim 33 ,{'sup': 1', '2, 'wherein Arand Arfurther comprise independently a substituent comprising an aryl group comprising 6 to 13 carbon atoms or a substitute comprising an alkyl group comprising 1 to 4 carbon.'}37. The light-emitting element according to claim 36 ,{'sup': 1', '2, 'wherein Arand Arfurther comprise independently a substituent comprising an aryl group comprising 6 to 13 carbon atoms ...

NOVEL ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

Provided are a novel organic compound appropriate for emission of green light and an organic light-emitting device including the organic compound. Provided is a substituted or unsubstituted indeno[1,2,3-cd]naphtho[2,3-k]fluoranthene appropriate for emission of green light. The substituents of the indeno[1,2,3-cd]naphtho[2,3-k]fluoranthene are each independently selected from a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted amino group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocyclic group. 2. The organic compound according to claim 1 , wherein Rto Rare each independently selected from a hydrogen atom and a substituted or unsubstituted aryl group.4. An organic light-emitting device comprising:an anode;a cathode; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an organic compound layer disposed between the anode and the cathode, the organic compound layer containing the organic compound according to .'}5. An organic light-emitting device comprising:an anode;a cathode; and{'claim-ref': {'@idref': 'CLM-00003', 'claim 3'}, 'an organic compound layer disposed between the anode and the cathode, the organic compound layer containing the organic compound according to .'}6. The organic light-emitting device according to claim 4 , wherein the organic compound layer is a light-emitting layer.7. The organic light-emitting device according to claim 6 , wherein the organic light-emitting device emits green light.8. A display apparatus having a plurality of pixels claim 4 , each including the organic light-emitting device according to and a switching device connected to the organic light-emitting device.9. An image input apparatus comprising:an image input unit configured to input an image; and{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'a display unit configured to display the image, the display unit having a plurality of pixels, each ...

Method for Separating off Tryptophan

The invention relates to a method for separating off tryptophan from aqueous mixtures of matter, in particular fermentation broths that are already partially processed, using simulated countercurrent chromatography or simulated moving bed (SMB) chromatography, and a device for carrying out the method. 117.-. (canceled)18. A method for separating off tryptophan from an aqueous mixture of matter using simulated countercurrent chromatography or SMB chromatography in which , in a separation section having a column arrangement consisting of more than one series-connected columns packed with an organic polymer suitable as adsorbent , which column arrangement is subdivided into a plurality of functional zones ,a) the tryptophan-containing mixture of matter and water as desorbent are continuously fed to the column arrangement at separate points andb) at a point situated between these feeds, the tryptophan-enriched extract stream, and at a further point situated upstream of the feed of tryptophan-containing mixture of matter, a raffinate stream containing further compounds from the mixture of matter used, are taken off separately, the extract stream optionally processed further and optionallyc) the columns that are loaded with non-desorbed compounds from the mixture of matter are cleaned by extraction of said compounds.19. The method as claimed in claim 18 , in which the water is optionally desalted and is fed at a temperature of from 20 to 98° C.20. The method as claimed in claim 18 , in which a mixture of matter is used that contains tryptophan at a concentration from 0.1 to 39 g/l.21. The method as claimed in claim 18 , in which a mixture of matter is used that has a pH from 2.5 to 9.22. The method as claimed in claim 18 , in which a mixture of matter obtained by fermentation is used that claim 18 , in addition to tryptophan claim 18 , also contains phenylalanine and/or tyrosine.23. The method as claimed in claim 22 , in which the mixture of matter used is the mother ...

Method for treating varicocele or male infertility using anthocyanin extracted from black soybean

The present invention relates to the therapeutic or ameliorating effects of anthocyanin extracted from black soybean on varicocele or male infertility. In particular, the present invention relates to a method for treating or ameliorating varicocele or male infertility using anthocyanin extracted from black soybean.

CRYSTALLINE FORMS OF 4, 4'- [4-FLUORO-7-( ETHYNYL)-2-METHYL-1H-INDOLE-1,3-DIYL] DIBUTANOIC ACID, 4,4'-[2-METHYL-7-( ETHYNYL)-1H-INDOLE-1, 3-DIYL] DIBUTANOIC ACID, AND 4,4'-[4-FLUORO-2-METHYL-7- ( ETHYNYL)-1H-INDOLE-1, 3-DIYL] DIBUTANOIC ACID

The present invention provides type C crystal of compound I, type B crystal of compound II, or type C crystal of compound III set forth in this specification. 1. A crystal of 4 ,4′-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1 ,3-diyl]dibutanoic acid having at least peaks of about 7.29 , 10.24 , 12.15 , 17.95 , and 18.44 at 2θ degree in powdered X-ray diffraction spectrum.2. The crystal of 4 claim 1 ,4′-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1 claim 1 ,3-diyl]dibutanoic acid according to claim 1 , having peaks of about 6.41 claim 1 , 7.29 claim 1 , 9.22 claim 1 , 10.03 claim 1 , 10.24 claim 1 , 12.15 claim 1 , 12.59 claim 1 , 13.36 claim 1 , 13.88 claim 1 , 14.15 claim 1 , 14.44 claim 1 , 16.60 claim 1 , 17.33 claim 1 , 17.95 claim 1 , 18.44 claim 1 , 18.86 claim 1 , 19.27 claim 1 , 20.23 claim 1 , 21.10 claim 1 , 21.85 claim 1 , 22.26 claim 1 , 23.11 claim 1 , 23.63 claim 1 , and 24.38 at 2θ degree in powdered X-ray diffraction spectrum.3. The crystal of 4 claim 2 ,4′-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1 claim 2 ,3-diyl]dibutanoic acid according to claim 2 , characterized by the chart of powdered X-ray diffraction spectrum shown in .4. A crystal of 4 claim 2 ,4′-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1 claim 2 ,3-diyl]dibutanoic acid having an endothermic peak of about 157° C. in differential scanning calorimetry.5. The crystal of 4 claim 4 ,4′-[4-fluoro-7-({4-[4-(3-fluoro-2-methylphenyl)butoxy]phenyl}ethynyl)-2-methyl-1H-indole-1 claim 4 ,3-diyl]dibutanoic acid according to claim 4 , characterized by the chart of differential scanning calorimetry shown in .6. A crystal of 4 claim 4 ,4′-[2-methyl-7-({4-[4-(pentafluorophenyl)butoxy]phenyl}ethynyl)-1H-indole-1 claim 4 ,3-diyl]dibutanoic acid having at least peaks of about 5.12 claim 4 , 10.16 claim 4 , 10.51 claim 4 , 14.90 claim 4 , ...

ARYLTHIAZOLYL PIPERIDINES AND RELATED COMPOUNDS AS MODULATORS OF SURVIVAL MOTOR NEURON (SMN) PROTEIN PRODUCTION

Aryl substituted thiazol-2-yl-piperidines and related compounds useful as modulators of survival motor neuron (SMN) protein production are provided herein. Without being bound to any particular theory it is believed the aryl substituted thiazol-2-yl-piperidines and related compounds provided herein act to increase production of the SMN2 form of survival motor neuron protein. These compounds are useful for treating spinal muscular atrophy. Pharmaceutical compositions containing a carrier and one or more of the aryl substituted thiazol-2-yl-piperidine or related compounds described herein are also provided. Methods of treating spinal muscular atrophy are also provided by this disclosure. 3. A compound or salt of claim 1 , wherein Ris(i) a 5-membered heteroaryl group containing 1, 2 or 3 heteroatoms chosen from N, O, and S and not more than one O or S heteroatoms:(ii) phenyl, naphthyl, or a 6-membered heteroaryl group containing one or two nitrogen atoms;(iii) a phenyl group fused to a 5, 6, or 7-membered heterocycloalkyl group containing one or two heteroatoms independently chosen from N, O, and S;(iv) a benzofuranyl, indolyl, 9H-fluorenyl, or dibenzo[b,d]thiophenyl group;each of which (i) and (ii) is substituted with 0 to 3 substituents independently chosen from:{'sub': 2', '1', '6', '1', '6', '2', '4', '1', '4', '1', '4', '1', '4', '0', '2', '1', '4', '1', '4', '1', '2', '1', '2, '(a) halogen, hydroxy, amino, cyano, nitro, oxo, —(C═O)NH, C-Calkyl, C-Calkoxy, C-Calkanoyl, C-Calkylthio, C-Calkylsulfonyl, mono- and di-(C-Calkylamino)C-Calkyl, mono- and di-(C-Calkyl)carboxamide, mono- and di-(C-Calkyl)sulfonamide, C-Chaloalkyl, and C-Chaloalkoxy, and'}{'sub': 3', '6', '0', '2', '0', '2', '0', '2', '0', '2', '1', '2', '1', '2, '(b) (C-Ccycloalkyl)C-Calkyl, (heterocycloalkyl)C-Calkyl; (phenyl)C-Calkyl, (phenyl)C-Calkoxy, and thienyl, each of which (b) is substituted with 0 to 2 substituents independently chosen from halogen, C-Calkyl, and C-Calkoxy; and'}{'sub': 1', '2', ...

PROCESSES AND INTERMEDIATES

A process for preparing enantioselectively a compound of formula I-1a or I-1b: 2. The process of claim 1 , wherein ring A is Ccycloaliphatic.32. The process of - claims 1 , wherein ring A is cyclopropyl.42. The process of - claims 1 , wherein ring A is cyclopentyl.52. The process of - claims 1 , wherein ring A is 1 claims 1 ,1-dimethylcyclopropyl.9. The process of claim 1 , wherein ring B is a 5-membered heterocyclic ring.11. The process of claim 1 , wherein ring B is substituted with an aryl ring optionally substituted with 0 to 4 groups claim 1 , each independently selected from alkyl claim 1 , halo claim 1 , alkoxy claim 1 , and hydroxyl.12. The process of claim 11 , wherein the aryl ring is phenyl.1514. The process of - claims 1 , wherein Ris H.1614. The process of - claims 1 , wherein Ris Caliphatic.1714. The process of - claims 1 , wherein Ris tert-butyl.2120. The process of - claims 18 , wherein Ris Caliphatic.2220. The process of - claims 18 , wherein Ris a cycloaliphatic.2320. The process of - claims 18 , wherein Ris Caliphatic.2420. The process of - claims 18 , wherein Ris Calkyl.2520. The process of - claims 18 , wherein Ris selected from methyl claims 18 , ethyl claims 18 , n-propyl claims 18 , iso-propyl claims 18 , iso-butyl claims 18 , n-butyl claims 18 , n-pentyl claims 18 , and iso-pentyl.2620. The process of - claims 1 , wherein Ris iso-butyl.2726. The process of - claims 1 , wherein Ris tert-butyl carbamate (Boc).2827. The process of - claims 1 , wherein the carboxylation step includes treating a compound of formula II with carbon dioxide and a lithium base in the presence of an aprotic solvent.29. The process of claim 28 , wherein the aprotic solvent is toluene claim 28 , ethyl acetate claim 28 , benzene claim 28 , and methyl tert-butyl ether.30. The process of claim 28 , wherein the aprotic solvent is methyl tert-butyl ether.31. The process of claim 28 , wherein the lithium base is sec-butyl lithium.3231. The process of - claims 1 , wherein the ...

REDUCTION OF ALDEHYDES AND KETONES TO ALCOHOLS

The embodiments described herein provide a reduction of an aldehyde or a ketone, such as a Meerwein-Ponnorf-Verley (MPV) reaction of an aldehyde or ketone. In some embodiments, the reaction occurs in the presence of Al[OC(CH)]. In some embodiments, the reaction occurs in the presence of an aprotic solvent. In some embodiments, the aldehyde or ketone is an amino aldehyde or an amino ketone wherein the amine is group is protected such that the nitrogen of the amine has no proton. Other embodiments related to compositions and compounds related to the reduction reaction, or to the preparation or use of the aldehyde, the ketone, or the resulting alcohol. 1. A method of reducing a C═O of an aldehyde or a ketone to a CH—OH of a product alcohol comprising reacting the aldehyde or ketone in the presence of Al[OC(CH)] and a reactant alcohol which comprises a carbon atom directly bonded to both a hydroxyl group and a hydrogen atom2. A method of reducing a C═O of an aldehyde or a ketone to a CH—OH of a product alcohol comprising reacting the aldehyde or ketone in the presence of: Al(OR) , a reactant alcohol comprising a carbon atom directly bonded to both a hydroxyl group and a hydrogen atom , and an aprotic solvent , wherein each Ris independently Calkyl or optionally substituted aryl.3. The method of claim 2 , wherein the aprotic solvent comprises ethyl acetate claim 2 , tetrahydrofuran claim 2 , toluene claim 2 , dichloromethane claim 2 , or an ether.4. The method of claim 2 , wherein the volume ratio of the aprotic solvent to the reactant alcohol is at least about 1:1.7. The method of claim 5 , wherein Ris COR.12. The method of claim 11 , wherein the ratio of diastereomer 1 to diastereomer 2 is at least about 0.5.13. The method of claim 11 , wherein the ratio of diastereomer 1 to diastereomer 2 has a value in the range of about 1 to about 10 claim 11 ,000. 1. Field of the InventionThe embodiments disclosed herein relate to reduction of an aldehyde or ketone, such as by ...

ORGANIC PHOTOELECTRIC CONVERSION ELEMENT AND SOLAR CELL USING SAME

Disclosed is an organic photoelectric conversion element which has a reverse layer structure wherein at least a first electrode, a photoelectric conversion layer and a second electrode are arranged on a substrate in this order. The organic photoelectric conversion element is characterized in that: the photoelectric conversion layer is a bulk heterojunction layer that is composed of a p-type organic semiconductor material and an n-type organic semiconductor material; and a compound that has a linear or branched fluorinated alkyl group having 6-20 carbon atoms is contained as the p-type organic semiconductor material. 1. An organic photoelectric conversion element having a reverse layer structure comprising a substrate having thereon at least a first electrode , a photoelectric conversion layer and a second electrode in this order , whereinthe photoelectric conversion layer is a bulk heterojunction layer comprising a p-type organic semiconductor material and an n-type organic semiconductor material, andthe p-type organic semiconductor material comprises a compound that has a linear or branched fluorinated alkyl group having 6 to 20 carbon atoms.2. The organic photoelectric conversion element of claim 1 , wherein the fluorinated alkyl group has 8 to 20 carbon atoms.4. The organic photoelectric conversion element of claim 3 , wherein Formula (1) meets 3≧m+n≧2.5. The organic photoelectric conversion element of claim 3 , wherein Formula (1) meets m≧1 and n≧1.7. The organic photoelectric conversion element of claim 6 , wherein claim 6 , in Formula (2) claim 6 , L represents a carbonyl group claim 6 , an ester group or an amide group.8. The organic photoelectric conversion element of wherein claim 6 , in Formula (2) claim 6 , L represents an ester group.9. The organic photoelectric conversion element of claim 1 , wherein at least one fluorinated alkyl group has 7 to 17 fluorine atoms.10. The organic photoelectric conversion element of claim 1 , wherein the compound having ...

BIPOLAR COMPOUND AS A HOST MATERIAL FOR ORGANIC LIGHT EMITTING DIODES

The present invention provides a bipolar compound represented by formula (I) and the derivatives thereof as a host material having excellent bipolar transporting properties for organic light-emitting diodes (OLEDs). The present invention also relates to a device including at least a layer of the bipolar compound and/or the derivatives thereof as a host material and a method of making the same. 2. The bipolar compound of claim 1 , wherein said substituted or unsubstituted alkyl group is Calkyl selected from one or more of a methyl group claim 1 , an ethyl group claim 1 , an n-propyl group claim 1 , an n-butyl group claim 1 , an n-pentyl group claim 1 , an n-hexyl group claim 1 , an n-heptyl group claim 1 , an n-octyl group claim 1 , an n-decyl group claim 1 , an iso-propyl group claim 1 , an iso-butyl group claim 1 , a sec-butyl group claim 1 , a tert-butyl group claim 1 , an iso-pentyl group claim 1 , a neopentyl group claim 1 , a tert-octyl group claim 1 , a fluoromethyl group claim 1 , a difluoromethyl group claim 1 , a trifluoromethyl group claim 1 , a 2-fluoroethyl group claim 1 , a 2 claim 1 ,2 claim 1 ,2-trifluoroethyl group claim 1 , a perfluoroethyl group claim 1 , a 3-fluoropropyl group claim 1 , a perfluoropropyl group claim 1 , a 4-fluorobutyl group claim 1 , a perfluorobutyl group claim 1 , a 5-fluoropentyl group claim 1 , a 6-fluorohexyl group claim 1 , a chloromethyl group claim 1 , a trichloromethyl group claim 1 , a 2-chloroethyl group claim 1 , a 2 claim 1 ,2 claim 1 ,2-trichloroethyl group claim 1 , a 4-chlorobutyl group claim 1 , a 5-chloropentyl group claim 1 , a 6-chlorohexyl group claim 1 , a bromomethyl group claim 1 , a 2-bromoethyl group claim 1 , an iodomethyl group claim 1 , a 2-iodoethyl group claim 1 , a hydroxymethyl group claim 1 , a hydroxyethyl group claim 1 , a cyclopropyl group claim 1 , a cyclobutyl group claim 1 , a cyclopentyl group claim 1 , a cyclohexyl group claim 1 , a cyclopentylmethyl group claim 1 , a cyclohexylmethyl ...

TARGETED NITROXIDE AGENTS

Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation. 45-. (canceled)6. The compound of claim 1 , in which R is Ac claim 1 , Boc claim 1 , Cbz claim 1 , or —P(O)-Ph.7. The compound of claim 1 , in which R claim 1 , R claim 1 , Rand Rare independently chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , 2-propyl claim 1 , butyl claim 1 , t-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , benzyl claim 1 , hydroxybenzyl claim 1 , phenyl and hydroxyphenyl.8. The compound of claim 1 , wherein when X is —CH═CR— claim 1 , Ris hydrogen claim 1 , methyl or ethyl.912-. (canceled)13. The compound of in which R1 claim 1 , R2 and R3 independently are methyl claim 1 , ethyl claim 1 , propyl claim 1 , 2-propyl claim 1 , butyl claim 1 , t-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , benzyl claim 1 , hydroxybenzyl claim 1 , phenyl and hydroxyphenyl.1421-. (canceled)27. A method of making a targeted antioxidant compound claim 1 , comprising:{'sub': 1', '1', '1', '6', '6', '5, 'a. reacting an aldehyde of structure R—C(O)— with (R)-2-methylpropane-2-sulfinamide to form an imine, in which Ris C-Cstraight or branched-chain alkyl, optionally including a phenyl (CH) group, that optionally is methyl-, hydroxyl- or fluoro-substituted;'}{'sub': 2', '2', '2, 'b. reacting a terminal alkyne-1-ol (HCC—R—CH—OH), in which Ris not present or is branched or straight-chained alkylene, with a tert-butyl)diphenylsilane salt to produce an alkyne;'}c. ...

NOVEL CURING AGENTS

A curable resin comprising a compound having the structure (I): wherein each carbon 2, together with either its carbon 1 or carbon 3, arc members of a fused cycloaliphatic ring, and when carbon 1 is a member of the ring so is N, and wherein each of the aliphatic or aromatic ring-member carbons may either be members of further fused cycloaliphatic rings or be bonded to a group selected from H or linear or branched Cto Calkyl. 2. A curable resin according to claim 1 , wherein any carbons forming part of any further fused cycloaliphatic rings are also bonded to either an H or linear or branched Cto Calkyl.3. A curable resin according to claim 1 , wherein each of the aliphatic or aromatic ring-member carbons claim 1 , which are not members of a fused cycloaliphatic ring claim 1 , are bonded to an H or linear or branched Cto Calkyl.4. A curable resin according to claim 1 , wherein the compound has a molecular weight of no greater than 600.5. A curable resin according to claim 1 , wherein the fused cycloaliphatic rings comprise five or six carbons.8. A curable resin according to claim 1 , wherein carbon 2 is a member of two fused cycloaliphatic rings claim 1 , one with carbon 1 and the other with carbon 3.9. A curable resin according to claim 1 , having a melting point of from 80° C. to 200° C.10. A curable resin according to claim 1 , wherein the resin is an epoxy or urethane.11. A curable resin according to claim 1 , comprising a fibre reinforcement.12. A curable resin according to claim 11 , which is a prepreg claim 11 ,13. A cured resin made by exposing a curable resin according to to elevated temperature.14. A cured resin according to claim 13 , which has a glass transition temperature of greater than 100° C.15. A cured resin according to which forms part of a structural member of an aerospace structure. The present invention relates to novel resin curing agents, particularly for epoxy and urethane resins.Curable resin systems are widely known and have a wide range ...

LIGHT EMITTING ELEMENT

Provided is an organic thin film light emitting element which has achieved all of improved luminous efficiency, improved driving voltage and improved durability life. Specifically provided is a light emitting element which comprises a hole transport layer and an electron transport layer between a positive electrode and a negative electrode and emits light by means of electrical energy. The light emitting element is characterized in that: the hole transport layer of the light emitting element contains a compound represented by general formula (1); the electron transport layer contains a donor compound; and the donor compound is an alkali metal, an inorganic salt containing an alkali metal, a complex of an alkali metal and an organic substance, an alkaline earth metal, an inorganic salt containing an alkaline earth metal, or a complex of an alkaline earth metal and an organic substance. (In the formula, R-Reach represents one group selected from the group consisting of hydrogen, deuterium, an alkyl group, a cycloalkyl group, an amino group, an aryl group, a heterocyclic group, a heteroaryl group, an alkenyl group, a cycloalkenyl group, an alkynyl group, analkoxy group, an alkylthio group, an arylether group, an arylthioether group, a halogen, a cyano group, a —P(═O)RRgroup and a silyl group; Rand Reach represents an aryl group or a heteroaryl group; and these substituents may be further substituted, or adjacent two substituents may combine together to form a ring. Meanwhile, R-Rmay be the same or different and each represents one group selected from the group consisting of an alkyl group, a cycloalkyl group, an aryl group and a heteroaryl group; and these substituents maybe further substituted.) 2. A light-emitting element claim 1 , according to claim 1 , wherein a hole injection layer exists between the hole transport layer and the anode and consists of an acceptor compound alone or contains an acceptor compound3. A light-emitting element claim 2 , according to claim ...

FAAH Inhibitors

The present disclosure relates to N-benzyl pyrrole compounds of formula (I) useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders. 2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring B is an optionally substituted ring selected from the group consisting of phenyl claim 1 , pyridine claim 1 , pyrimidine claim 1 , pyrazine claim 1 , pyridazine claim 1 , pyrrole claim 1 , imidazole claim 1 , pyrazole claim 1 , furan claim 1 , thiophene claim 1 , triazole claim 1 , tetrazole claim 1 , thiazole claim 1 , oxathiazole and oxazole.3. The compound according to claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein ring B is an optionally substituted pyridine or an optionally substituted phenyl.45.-. (canceled)6. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is selected from the group consisting of 0 and 1.7. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Jis independently selected from the group consisting of halogen claim 1 , Calkyl claim 1 , cyclopropyl claim 1 , cyclopropyloxy claim 1 , Chaloalkyl claim 1 , Calkoxy and Chaloalkoxy.8. The compound according to claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein each Jis independently selected from the group consisting of halogen claim 7 , methyl claim 7 , ethyl claim 7 , propyl claim 7 , isopropyl claim 7 , trifluoromethyl claim 7 , methoxy claim 7 , trifluoromethoxy claim 7 , ethoxy claim 7 , propyloxy and isopropyloxy.10. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein p is selected from the group consisting of 0 claim 1 , 1 and 2.11. The compound ...

GPR120 RECEPTOR AGONISTS AND USES THEREOF

GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control. 125.-. (canceled)26. A compound selected from the group consisting of:3-(4-((5-fluoro-1-(methoxycarbonyl)-2,2-dimethylindolin-7-yl)methoxy)-2,3-dimethylphenyl)propanoic acid;3-(4-((5-fluoro-2,2-dimethylindolin-7-yl)methoxy)-2,3-dimethylphenyl)propanoic acid; and3-(4-((5-fluoro-1,2,2-trimethylindolin-7-yl)methoxy)-2,3-dimethylphenyl)propanoic acid,or a pharmaceutically acceptable salt thereof.27. A composition comprising a compound of and a pharmaceutically acceptable carrier.28. A method of treating a disease or condition selected from the group consisting of Type I diabetes claim 26 , Type II diabetes and metabolic syndrome claim 26 , said method comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of .29. The method of claim 28 , wherein said disease is Type II diabetes.30. A method of lowering blood glucose in a mammal claim 26 , said method comprising administering a therapeutically effective amount of a compound of to a mammal in need of such treatment.31. The method of claim 30 , wherein said mammal is a human. Diabetes mellitus can be divided into two clinical syndromes, Type I and Type II diabetes mellitus. Type I diabetes, or insulin-dependent diabetes mellitus, is a chronic autoimmune disease characterized by the extensive loss of beta cells in the pancreatic islets of Langerhans (hereinafter referred to as “pancreatic islet cells” or “islet cells”), which produce insulin. As these cells are progressively destroyed, the amount of secreted insulin decreases, eventually leading to hyperglycemia (abnormally high level of glucose in the blood) when the amount secreted drops below the level required for euglycemia (normal blood glucose level). Although the exact trigger for this immune response is not known, patients with Type I ...

AMIDE DERIVATIVES OF N-UREA SUBSTITUTED AMINO ACIDS AS FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS

The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor. 2. A compound according to claim 1 , wherein:a is 1 and b is 0.3. A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': 5', '14, 'sub': 'n', 'Ris —S(O)R.'}4. A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': '5', 'sub': '3', 'Ris —CF.'}5) A compound according to claim 1 , wherein:a is 1 and b is 0; and{'sup': '5', 'Ris halogen.'}6. A compound according to claim 1 , wherein:a is 1 and b is 0;{'sup': 1', '11', '12', '13, 'sub': '1-8', 'Ris optionally substituted Calkyl, —NRRor —OR;'}{'sup': '2', 'sub': '1-8', 'Ris optionally substituted Calkyl;'}{'sup': 3', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 4', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 5', '14, 'sub': 3', 'n, 'Ris halogen, —CFor —S(O)R;'}n is 0, 1 or 2;{'sup': 6', '15', '13', '11', '−12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': 7', '15', '13', '11', '12, 'sub': '1-8', 'Ris hydrogen, optionally substituted Calkyl, halogen, —COOR, —OR, —NRR;'}{'sup': '8', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '9', 'sub': 1-8', '6-10, 'Ris hydrogen, optionally substituted Calkyl or optionally substituted Caryl;'}{'sup': '10', 'sub': '1-8', 'Ris hydrogen or optionally substituted C;'}{'sup': '11', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '12', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '13', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl;'}{'sup': '14', 'sub': '1-8', 'Ris hydrogen or optionally substituted Calkyl; ...

COMPOUND HAVING CARBAZOLE RING STRUCTURE, AND ORGANIC ELECTROLUMINESCENT DEVICE

There is provided an organic compound of excellent characteristics that exhibits excellent hole-injecting/transporting performance and has high triplet exciton confining capability with an electron blocking ability, and that has high stability in the thin-film state and high luminous efficiency. The compound is used to provide a high-efficiency, high-durability organic electroluminescent device, particularly a phosphorescent organic electroluminescent device. The present invention is a compound of the following general formula having a carbazole ring structure. The compound is used as a constituent material of at least one organic layer in an organic electroluminescent device that includes a pair of electrodes, and one or more organic layers sandwiched between the pair of electrodes. 3. (canceled)4. (canceled)6. An organic electroluminescent device that comprises a pair of electrodes , and one or more organic layers sandwiched between the pair of electrodes ,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the compound having a carbazole ring structure of is used as a constituent material of at least one organic layer.'}7. The organic electroluminescent device according to claim 6 , wherein the organic layer is a hole transport layer.8. The organic electroluminescent device according to claim 6 , wherein the organic layer is a hole injection layer.9. The organic electroluminescent device according to claim 6 , wherein the organic layer is an electron blocking layer.10. The organic electroluminescent device according to claim 6 , further comprising a light emitting layer that contains a phosphorescent light-emitting material.11. The organic electroluminescent device according to claim 10 , wherein the phosphorescent light-emitting material is a metal complex that contains iridium or platinum.12. An organic electroluminescent device that comprises a pair of electrodes claim 10 , and one or more organic layers sandwiched between the pair of electrodes claim ...

(METHYLSULFONYL) ETHYL BENZENE ISOINDOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USES

Provided are (methylsulfonyl)ethyl benzene isoindoline compounds, and pharmaceutically acceptable salts, solvates, or stereoisomers thereof. Methods of use and pharmaceutical compositions of these compounds are also disclosed. 2. The compound of claim 1 , wherein Ris hydrogen.3. The compound of claim 1 , wherein Ris (cyclopropyl)-C(O)—.4. The compound of claim 1 , wherein Ris hydrogen.5. The compound of claim 1 , wherein Ris methyl.6. The compound of claim 1 , wherein Ris gluc.7. The compound of claim 1 , wherein Ris hydrogen.8. The compound of claim 1 , wherein Ris ethyl.9. The compound of claim 1 , wherein Ris hydroxyl.10. The compound of claim 1 , wherein Ris —O-gluc.13. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or stereoisomer thereof.14. A method of treating claim 1 , managing or preventing a disease or disorder comprising administering to a patient a compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or stereoisomer thereof claim 1 , wherein the disease or disorder is cancer claim 1 , a disorder associated with angiogenesis claim 1 , pain claim 1 , macular degeneration or a related syndrome claim 1 , a skin disease claim 1 , a pulmonary disorder claim 1 , an asbestos-related disorder claim 1 , a parasitic disease claim 1 , an immunodeficiency disorder claim 1 , a CNS disorder claim 1 , CNS injury claim 1 , atherosclerosis or a related disorder claim 1 , dysfunctional sleep or a related disorder claim 1 , hemoglobinopathy or a related disorder claim 1 , or a TNFα related disorder. Provided herein are (methylsulfonyl)ethyl benzene isoindoline derivatives. Pharmaceutical compositions comprising the compounds and methods for treating, preventing and managing various disorders are also provided.Many cellular functions are mediated by levels of adenosine 3′,5′-cyclic monophosphate (cAMP). Such cellular functions can contribute to inflammatory ...

METAL COMPLEXES WITH ORGANIC LIGANDS AND USE THEREOF IN OLEDS

The present invention relates, inter alia, to metal complexes having improved solubility, to processes for the preparation of the metal complexes, to devices comprising these metal complexes and to the use of the metal complexes. M(L)n(L′)m formula 1 where the compound contains a moiety M(L)n of the formula (2) W is equal to the formula (3). 117-. (canceled)23. The compound according to claim 18 , wherein m is 1 claim 18 , 2 claim 18 , 3 claim 18 , or 4.28. The compound according to claim 18 , wherein M is equal to iridium.30. A formulation comprising at least one compound according to and at least one solvent.31. An electronic device which comprises the compound according to .32. The electronic device as claimed in claim 31 , wherein in the device is an organic electroluminescent device claim 31 , an organic integrated circuit claim 31 , an organic field-effect transistor claim 31 , an organic thin-film transistor claim 31 , an organic light-emitting transistor claim 31 , an organic solar cell claim 31 , an organic optical detector claim 31 , an organic photoreceptor claim 31 , an organic field-quench device claim 31 , a light-emitting electrochemical cell or an organic laser diode.33. An organic electroluminescent device which comprises the compound according to is employed as emitting compound in one or more emitting layers.34. An organic electroluminescent device which comprises the compound according to is employed as emitting compound in one or more emitting layers claim 18 , in combination with a matrix material.35. The organic electroluminescent device according to claim 34 , wherein the matrix material is a ketone claim 34 , phosphine oxide claim 34 , sulfoxide claim 34 , sulfone claim 34 , triarylamine claim 34 , carbazole derivative claim 34 , indolocarbazole derivative claim 34 , indenocarbazole derivativs claim 34 , azacarbazole derivative claim 34 , bipolar matrix material claim 34 , silane claim 34 , azaborole claim 34 , boronic ester claim 34 , ...

PHOTOELECTRIC CONVERSION DEVICE, PRODUCTION METHOD THEREOF, PHOTOSENSOR, IMAGING DEVICE AND THEIR DRIVE METHODS

A photoelectric conversion device comprising a transparent electrically conductive film, a photoelectric conversion film and an electrically conductive film in this order, wherein the photoelectric conversion film comprises a photoelectric conversion layer, and an electron blocking layer, wherein the electron blocking layer contains a compound represented by the specific formula. 2. An electron blocking material comprising the compound according to .3. A film comprising the compound according to claim 1 , wherein the film has a thickness of 1 to 1 claim 1 ,000 nm.4. The compound according to claim 1 , wherein Rand R′in formula (F-10) are the same.5. The compound according to claim 1 , wherein Aand Ain formula (F-10) are the same.6. The compound according to claim 1 , wherein Xa in formula (A-1) represents a single bond.7. The compound according to claim 1 , wherein the compound represented by formula (F-10) has a molecular weight of 500 to 2000.8. The compound according to claim 1 , wherein the compound represented by formula (F-10) has an ionization potential of 5.8 eV or less. 1. Field of the InventionThe present invention relates to a photoelectric conversion device, a production method thereof, a photosensor, an imaging device and their driving methods.2. Description of the Related ArtAs for the solid-state imaging device, there is widely used a flat light-receiving device where photoelectric conversion sites are two-dimensionally arrayed in a semiconductor to form pixels and a signal generated by photoelectric conversion in each pixel is charge-transferred and read out through a CCD or CMOS circuit. The conventional photoelectric conversion site generally used is a photodiode part formed using PN junction in a semiconductor such as Si.In recent years, fabrication of a multipixel device is proceeding, and the pixel size and in turn, the area of a photodiode part become small, which brings about problems of reduction in the aperture ratio, reduction in the light ...

ALLOSTERIC BINDING COMPOUNDS

The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds. 2. The method according to claim 1 , comprising administering the compound of formula (I) wherein A is an aryl ring.35.-. (canceled)6. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein B is a 6-membered cycloalkyl claim 1 , aryl claim 1 , or heteroaryl ring claim 1 , which ring together with A forms an annulated ring system.78.-. (canceled)9. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein B is a 5-membered heteroaryl ring claim 1 , which ring together with A forms an annulated ring system.1011.-. (canceled)14. (canceled)15. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein Lis selected from the group consisting of —O— claim 1 , —NH— claim 1 , and —NR—.16. The method according to claim 15 , wherein Ris Calkyl.17. The method according to claim 16 , wherein Ris selected from the group consisting of methyl claim 16 , ethyl claim 16 , propyl claim 16 , isopropyl claim 16 , butyl claim 16 , iso-butyl claim 16 , sec-butyl claim 16 , and tert-butyl.1821.-. (canceled)22. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein Ris selected from the group consisting of Calkyl claim 1 , Calkoxy claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , and —NH—Calkyl claim 1 , where any of these optionally is substituted with one or more substituents.23. (canceled)24. The method according to claim 22 , wherein Ris Calkyl claim 22 , wherein the alkyl optionally is substituted with one or more substituents.2527.-. (canceled)29. The method according to claim 28 , wherein Lis selected from the group consisting of —O— and —S—.3038.-. (canceled)39. The method ...

ACENAPHTHO HETEROCYCLIC COMPOUND AND APPLICATION THEREOF

The present invention relates to acenaphtho heterocyclic compounds and their uses in manufacturing the BH3 mimetics as Bcl-2-like protein inhibitors. Structures are shown in the following: 2. The compound according to claim 1 , wherein the said Z is a straight or branched Calkyl which is unsubstituted or substituted.3. The compound according to claim 2 , wherein Ris (CH)Ph-(o claim 2 ,m claim 2 ,p)Z claim 2 , the said Z is a straight or branched Calkyl which is unsubstituted or substituted.4. The compound according to claim 2 , or claim 2 , wherein the said W is H claim 2 , NHor OH.5. The compound according to claim 4 , wherein the said X is O or S.6. The compound according to claim 5 , wherein Ris (CH)Y claim 5 , the said Y is selected from the group consisting of Ph claim 5 , CF claim 5 , OCH claim 5 , SCH claim 5 , NH claim 5 , Br claim 5 , isopropyl claim 5 , isobutyl and secbutyl.7. The compound according to claim 1 , selected from the group consisting of:9-(butylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(hexylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(3-phenylpropylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;3-ethoxy-9-(3-phenylpropylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;3-benzoyl-9-(butylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(butyl(methyl)amino)-8H-acenaphtho[1,2-b]pyrrol-8-one;3-(4-bromophenylthio)-9-(butylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;3-(4-bromophenylthio)-9-(3-phenylpropylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(butylamino)-3-thiomorpholino-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(3-phenylpropylamino)-3-thiomorpholino-8H-acenaphtho[1,2-b]pyrrol-8-one;9-(butylamino)-3-(4-isopropylphenoxy)-8H-acenaphtho[1,2-b]pyrrol-8-one; and3-(4-isopropylphenoxy)-9-(3-phenylpropylamino)-8H-acenaphtho[1,2-b]pyrrol-8-one.10. The compound according to claim 9 , wherein Ris XRand Ris H.11. The compound according to or claim 9 , wherein It is CN.12. The compound according to claim 11 , wherein Ris (CH)Ph-(0 claim 11 , m claim 11 , p)Y.13. The compound according to ...

MATERIALS FOR ELECTRONIC DEVICES

The present invention relates to compounds of the formula (I), to the use of compounds of the formula (I) in electronic devices and electronic devices comprising one or more compounds of the formula (I). The invention furthermore relates to the preparation of the compounds of the formula (I) and to formulations comprising one or more compounds of the formula (I). 114-. (canceled)16. The compound according to claim 15 , wherein n is equal to 0 or 1.17. The compound according to claim 15 , wherein at least one of the groups X′ claim 15 , Xand Xrepresents a group NR.18. The compound according to claim 15 , wherein 0 claim 15 , 1 or 2 groups Z per aromatic or heteroaromatic six-membered ring are equal to N.19. The compound according to claim 15 , wherein the groups X claim 15 , Xand Xare selected claim 15 , identically or differently claim 15 , from C(R) claim 15 , C═O claim 15 , Si(R) claim 15 , NR claim 15 , PR claim 15 , P(═O)R claim 15 , O and S.20. The compound according to claim 15 , wherein Rrepresents on each occurrence claim 15 , identically or differently claim 15 , an aromatic or heteroaromatic ring system having 5 to 30 aromatic ring atoms claim 15 , which optionally in each case be substituted by one or more radicals R.21. The compound according to claim 15 , wherein at least one group is present as substituent Ror Rwhich is selected from electron-deficient heteroaryl groups claim 15 , aromatic or heteroaromatic ring systems having 10 to 30 aromatic ring atoms and from arylamine groups claim 15 , each of which is optionally substituted by one or more radicals as defined in .23. A process for the preparation of the compound of the formula (I) according to claim 15 , which comprises ring-closure reacting one or more condensed heteroaromatic five-membered rings.24. An oligomer claim 15 , polymer or dendrimer comprising one or more compounds of the formula (I) according to claim 15 , where the bond(s) to the polymer claim 15 , oligomer or dendrimer is ...

Organic luminescent material and organic electroluminescent apparatus

An organic luminescent material includes a host luminescent material and a guest luminescent material. The host luminescent material includes a compound represented by formula (1), where n is 0˜8; R 2 and R 3 respectively represent H, CF 3 , CN, CH 3 or C 5 H 11 ; R 1 is CH 3 or one of substituents shown as follows:

ORGANIC ELECTROLUMINESCENT DEVICE

An organic electroluminescence device comprising a cathode, an anode and at least one layer comprising a phosphorescent light emitting material and a host material which is sandwiched between the cathode and the anode and further comprising an electron injecting layer which is adhered to the light emitting layer and is capable of transporting electrons, wherein an ionization potential of the host material is 5.9 eV or smaller, and wherein an energy gap of the electron transporting material in the electron injecting layer is smaller than that of the host material in the light emitting layer or wherein a triplet energy of the electron transporting material in the electron injecting layer is smaller than that of the host material in the light emitting layer. It emits phosphorescent light with enhanced efficiency because it comprises a light emitting layer and an electron injecting layer both satisfying specified condition and employs a light emitting layer capable of electron transporting. 115.-. (canceled)18. An organic electroluminescence device according to claim 16 , wherein the host material is an electron transporting material having an electron mobility of 10cm/V.s or greater.19. An organic electroluminescence device according to claim 17 , wherein the host material is an electron transporting material having an electron mobility of 10cm/V.s or greater.20. An organic electroluminescence device according to claim 16 , wherein the host material is represented by formula (1) or (2):{'br': None, 'sub': 'm', '(Cz-)A\u2003\u2003(1),'}{'br': None, 'sub': 'n', 'Cz-A\u2003\u2003(2),'}wherein Cz represents a substituted or unsubstituted carbazolyl group or a substituted or unsubstituted azacarbazolyl group; A represents an aryl-substituted ring group having nitrogen atom, a diaryl-substituted ring group having nitrogen atom, or a triaryl-substituted ring group having nitrogen atom; and m or n is an integer of 1 to 3; andthe ring group having nitrogen atom in A is selected ...

PHOTOACTIVE COMPOSITION AND ELECTRONIC DEVICE MADE WITH THE COMPOSITION

There is provided a photoactive composition including: (a) 50-99 wt % based on the total weight of the photoactive composition, of at least one host material having a HOMO energy level; (b) 1-10 wt % based on the total weight of the photoactive composition, of an emissive dopant; and (c) 0.1 to 10 wt % based on the total weight of the photoactive composition, of a non-emissive dopant. The non-emissive dopant is an organometallic iridium complex that has a HOMO energy level shallower than the HOMO energy level of the host. 1. A photoactive composition comprising:(a) 50-99 wt % based on the total weight of the photoactive composition, of at least one first host material having a HOMO energy level;(b) 1-10 wt % based on the total weight of the photoactive composition, of an emissive dopant; and(c) 0.1 to 10 wt % based on the total weight of the photoactive composition, of a non-emissive dopant, wherein the non-emissive dopant is an organometallic iridium complex having a HOMO energy level shallower than the HOMO energy level of the host.2. The composition of claim 1 , further comprising:(d) 1-49 wt % based on the total weight of the photoactive composition, of a second host material having a HOMO energy level that is deeper than the HOMO energy level of the non-emissive dopant.3. The composition of claim 2 , wherein the weight ratio of the first host material to the second host material is in the range of 19:1 to 2:1.4. The composition of claim 1 , wherein at least one material is deuterated.5. The composition of claim 1 , wherein the first host material has a HOMO energy level deeper than −5.0 eV.6. The composition of claim 1 , wherein the first host material has a Tg greater than 95° C.7. The composition of claim 1 , wherein the first host material is selected from the group consisting of phenanthrolines claim 1 , quinoxalines claim 1 , phenylpyridines claim 1 , benzodifurans claim 1 , and metal quinolinate complexes.9. The composition of claim 2 , wherein the second ...

NOVEL COMPOSITIONS AND METHODS FOR TREATING CANCER

Provided herein are methods and compositions inter alia for treating diseases, including hyperproliferative diseases, migraine headaches, and depression. 7. The compound of claim 1 , wherein{'sup': 1A', '7A', '7A, 'Ris independently —C(O)Ror —C(O)—OR;'}{'sup': 1B', '7B', '7B, 'Ris independently —C(O)Ror —C(O)—OR;'}{'sup': '7A', 'sub': 1', '20', '3', '8', '6', '10, 'Ris independently hydrogen, substituted or unsubstituted C-Calkyl, substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C-Ccycloalkyl, substituted or unsubstituted 3 to 8 membered heterocycloalkyl, substituted or unsubstituted C-Caryl, or substituted or unsubstituted 5 to 10 membered heteroaryl; and'}{'sup': '7B', 'sub': 1', '20', '3', '8', '6', '10, 'Ris independently hydrogen, substituted or unsubstituted C-Calkyl, substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C-Ccycloalkyl, substituted or unsubstituted 3 to 8 membered heterocycloalkyl, substituted or unsubstituted C-Caryl, or substituted or unsubstituted 5 to 10 membered heteroaryl.'}8. The compound of claim 1 , wherein{'sup': 2A', '9A', '9A, 'Ris independently —C(O)Ror —C(O)—OR;'}{'sup': 2B', '9B', '9B, 'Ris independently —C(O)Ror —C(O)—OR;'}{'sup': '9A', 'sub': 1', '20', '3', '8', '6', '10, 'Ris independently hydrogen, substituted or unsubstituted C-Calkyl, substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C-Ccycloalkyl, substituted or unsubstituted 3 to 8 membered heterocycloalkyl, substituted or unsubstituted C-Caryl, or substituted or unsubstituted 5 to 10 membered heteroaryl; and'}{'sup': '9B', 'sub': 1', '20', '3', '8', '6', '10, 'Ris independently hydrogen, substituted or unsubstituted C-Calkyl, substituted or unsubstituted 2 to 20 membered heteroalkyl, substituted or unsubstituted C-Ccycloalkyl, substituted or unsubstituted 3 to 8 membered heterocycloalkyl, substituted or unsubstituted C-Caryl, or substituted or unsubstituted 5 to ...

NOVEL ALKENE OXINDOLE DERIVATIVES

The present invention provides compounds of formula (I), 2. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , halogen and alkoxy.3. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , fluoro and chloro.4. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , halogen and alkoxy.5. The method according to claim 1 , wherein Ris hydrogen or fluoro.6. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , halogen and alkoxy.7. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , fluoro claim 1 , chloro and methoxy.8. The method according to claim 1 , wherein Ris selected from the group consisting of: hydrogen claim 1 , halogen and alkoxy.9. The method according to claim 1 , wherein Ris hydrogen or fluoro.10. The method according to claim 1 , wherein Ris selected from the group consisting of: alkyl claim 1 , halophenylalkyl claim 1 , phenyl claim 1 , substituted phenyl claim 1 , thiophenyl and pyridinyl claim 1 , wherein said substituted phenyl is phenyl substituted with one to three substituents independently selected from the group consisting of alkyl claim 1 , alkoxy claim 1 , halogen claim 1 , cyano claim 1 , haloalkyl claim 1 , alkylsulfanyl claim 1 , aminosulfonyl claim 1 , alkylsulfonyl claim 1 , haloalkoxy and alkylcarbonyl.11. The method according to claim 1 , wherein Ris halophenyl or cyanophenyl.12. The method according to claim 1 , wherein Ris chlorophenyl or cyanophenyl.13. The method according to claim 1 , wherein Ris selected from the group consisting of: alkyl claim 1 , hydroxyalkyl claim 1 , cycloalkyl claim 1 , phenyl and halophenyl.14. The method according to claim 1 , wherein Ris alkyl or phenyl.15. The method according to claim 1 , wherein Ris isopropyl or phenyl.16. The method according to claim 1 , ...

Novel Fluorescent Dyes and Uses Thereof

The present invention provides fluorescent dyes that are based on firefly luciferin structure. These dyes are optimally excited at shorter wavelengths and have Stokes shift of at least 50 nm. The fluorescent dyes of the invention are useful for preparation of dye-conjugates, which can be used in detection of an analyte in a sample. 2. The dye-conjugate of wherein the conjugated molecule is a peptide or a protein.3. The dye-conjugate of wherein the protein is an antibody claim 1 , or a fragment of an antibody.4. The dye-conjugate of wherein the antibody is selected from the group consisting of an anti CD3 antibody claim 3 , an anti CD4 antibody claim 3 , and an anti CD45 antibody.5. The dye-conjugate of wherein Yand Yare each a halogen.6. The dye-conjugate of wherein Yand Yare each chlorine.7. The dye-conjugate of wherein Yand Yare each fluorine.8. The dye-conjugate of wherein Yis CFand Yis H.9. The dye-conjugate of wherein each W is alkyl.10. The dye-conjugate of wherein each W is methyl.11. The dye-conjugate of wherein L is selected from the group consisting of a carbonyl group (C═O) claim 1 , —C(═O)NH(CH)C(═O)— wherein n is an integer from 1-5 claim 1 , and —(CH)C(═O)— wherein n is an integer from 1-5. This application is a divisional application of U.S. Non-Provisional application Ser. No. 12/836,747, filed on Jul. 15, 2010 which claims priority to U.S. Provisional Application Ser. No. 61/225,985, filed Jul. 16, 2009, the contents of which are hereby incorporated by reference in their entirety into this application.The present invention relates to fluorescent dyes, more specifically, ultraviolet excitable fluorescent dye compositions, compounds and conjugates, as well as method of using and making the same.Fluorescent dyes are widely used for labeling, detecting, and/or quantifying components in a sample. The various approaches used for such detection and/or quantification include fluorescence microscopy, fluorescence immunoassay, flow cytometric analysis of ...

Light-Emitting Element, Light Emitting Device, and Electronic Device

A light-emitting element includes a light-emitting layer having a two-layer structure in which a first light-emitting layer containing a first light-emitting substance and a second light-emitting layer containing a second light-emitting substance, which is in contact with the first light-emitting layer, are provided between an anode and a cathode. The first light-emitting layer is separated into two layers of a layer provided on the anode side and a layer provided on the cathode side. The layer provided on the anode side contains only a first light-emitting substance, or a first organic compound of less than 50 wt % and the first light-emitting substance of 50 wt % to 100 wt %. The layer provided on the cathode side contains a second organic compound and the first light-emitting substance. The second light-emitting layer, which is provided in contact with the first light-emitting layer, contains the second light-emitting substance and a third organic compound. 12-. (canceled)3. A light-emitting element comprising:a first light-emitting layer between an anode and a cathode; anda second light-emitting layer between the anode and the cathode, the second light-emitting layer being in contact with a cathode side of the first light-emitting layer,wherein the first light-emitting layer includes a first layer provided on an anode side and a second layer provided on a cathode side,wherein the first layer provided on the anode side contains a first light-emitting substance,wherein the second layer provided on the cathode side contains a second organic compound and the first light-emitting substance,wherein an amount of the second organic compound in the second layer provided on the cathode side is greater than or equal to 50 wt % and less than or equal to 99.9 wt %,wherein the second light-emitting layer contains a third organic compound and a second light-emitting substance, andwherein an amount of the third organic compound in the second light-emitting layer is greater than ...

Plant-derived formulations for treatment of hiv

Disclosed herein are methods for treating mammals with HIV/AIDS comprising administering a therapeutically effective amount of a composition comprising an extract of Rubia cordifolia . The extract is preferably an alcohol extract, an aqueous extract, or mixtures thereof. The alcohol preferably comprises ethanol, isopropyl alcohol, or mixtures thereof.

NOVEL COMPOUNDS AS DPP-IV INHIBITORS AND PROCESS FOR PREPARATION THEREOF

The present invention relates to process for preparation of novel compounds which are acting as inhibitors of dipeptidyl peptidase-IV enzyme and is depicted by the structural formula as given below: Formula VI. Which are useful in the treatment or prevention of diseases in which the dipeptidylpeptidase-IV enzyme is involved, such as diabetes and particularly type-2 diabetes. 5. The process as claimed in claim 3 , wherein Peptide bond is formed by coupling between a carboxyl group and an amino group in presence of coupling agents.6. The coupling agents as claimed in are selected from DCC claim 5 , EDC claim 5 , DIC and like.7. The process as claimed in claim 3 , the saponification reaction is carried out by using Inorganic base.8. The process as claimed in claim 7 , wherein the inorganic base is selected from NaOH claim 7 , KOH claim 7 , LiOH and like claim 7 , preferably NaOH and LiOH.1519-. (canceled)21. The process as claimed in claim 4 , wherein Peptide bond is formed by coupling between a carboxyl group and an amino group in presence of coupling agents.22. The coupling agents as claimed in are selected from DCC claim 21 , EDC claim 21 , DIC and like.23. The process as claimed in claim 4 , the saponification reaction is carried out by using Inorganic base.24. The process as claimed in claim 23 , wherein the inorganic base is selected from NaOH claim 23 , KOH claim 23 , LiOH and like claim 23 , preferably NaOH and LiOH. The present invention relates to process for preparation of novel compounds which are acting as inhibitors of dipeptidyl peptidase-IV enzyme and are useful in the treatment or prevention of diseases in which the dipeptidylpeptidase-IV enzyme is involved, such as diabetes, particularly type-2 diabetes.Various amino peptidases are present in the mammals and catalyze the sequential release of peptides from polypeptides such as pyroglutamyl aminopeptidase and prolyaminpeptidase in addition to dipeptidyl peptidase. Dipeptidyl peptidase family includes ...

PROCESS FOR PRODUCING OPTICALLY ACTIVE 3-SUBSTITUTED-3-FORMYL-2-HYDROXYPROPANOIC ACID COMPOUND

The present invention provides a production method of optically active 3-substituted-3-formyl-2-hydroxypropanoic acid compound (4), which includes a step of reacting glyoxylic acid compound (1-1) or (1-2) with aldehyde (2) in the presence of optically active pyrrolidine compound (3); 2. The method of claim 1 , wherein the reaction is carried out in the presence of a solvent.3. The method of claim 2 , wherein the solvent is at least one selected from the group consisting of an aromatic hydrocarbon solvent claim 2 , an alcohol solvent claim 2 , a halogenated hydrocarbon solvent claim 2 , an ether solvent claim 2 , a nitrile solvent and water.4. The method of claim 1 , wherein the reaction is carried out within the range of 0-50° C.5. The method of claim 1 , wherein Ris a hydrogen atom.6. The method of claim 1 , wherein Ris a hydroxyl group claim 1 , and Arand Arare each independently a phenyl group optionally having C-Cfluorinated alkyl group(s).7. The method of claim 1 , wherein Ris a hydroxyl group claim 1 , and Arand Arare both 3 claim 1 ,5-bis(trifluoromethyl)phenyl groups.8. The method of claim 6 , wherein the absolute configuration of C** is S-configuration claim 6 , and the absolute configuration of C* is R-configuration.11. The method of claim 7 , wherein the absolute configuration of C** is S-configuration claim 7 , and the absolute configuration of C* is R-configuration. The present invention relates to a production method of an optically active 3-substituted-3-formyl-2-hydroxypropanoic acid compound.An optically active 3-substituted-3-formyl-2-hydroxypropanoic acid compound is known to be useful for, for example, as a drug substance or synthetic intermediate for a medicament, a pesticide and the like, or as a synthetic intermediate for vitamins such as pantothenic acid and the like.Concerning production method of an optically active 3-substituted-3-formyl-2-hydroxypropanoic acid compound, non-patent document 1 discloses a method of reacting ethyl glyoxylate ...

HOST MATERIAL AND ORGANIC LIGHT EMITTING DISPLAY DEVICE USING THE SAME

A host material is disclosed. The host material, as a compound which is represented by the following formula 1, has a chemical structure in which nitrogen and silicon atoms are chemically and directly bonded to each other. 3. The host material of claim 1 , wherein the substitute capable of being substituted into the aromatic or heterocyclic groups includes at least one among an alkyl group claim 1 , an alkoxy group claim 1 , a halogen group claim 1 , a silyl group claim 1 , a cyano group claim 1 , deuterium claim 1 , tritium and hydrogen.4. The host material of claim 1 , wherein the heterocyclic group includes 4 through 16 carbon atoms and at least one of one through three nitrogen atoms claim 1 , one or two oxygen atoms and one or two sulfide atoms.8. The organic light emitting display device of claim 6 , wherein the substitute capable of being substituted into the aromatic or heterocyclic groups includes at least one among an alkyl group claim 6 , an alkoxy group claim 6 , a halogen group claim 6 , a silyl group claim 6 , a cyano group claim 6 , deuterium claim 6 , tritium and hydrogen.9. The organic light emitting display device of claim 6 , wherein the heterocyclic group includes 4 through 16 carbon atoms and at least one of one through three nitrogen atoms claim 6 , one or two oxygen atoms and one or two sulfide atoms.11. The organic light emitting display device of claim 6 , wherein the dopant material is one of green and blue phosphorescent dopants.12. The organic light emitting display device of claim 6 , further comprising:at least one of a hole injection layer and a hole transport layer which are interposed between the anode and the light emission layer; andat least one of an electron injection layer and an electron transport layer which are interposed between the light emission layer and the cathode. The present application claims priority under 35 U.S.C. §119(a) of Korean Patent Application No. 10-2011-0129902 filed on Dec. 6, 2011, which is hereby ...

DEUTERATED COMPOUNDS FOR ELECTRONIC APPLICATIONS

This invention relates to deuterated indolocarbazole compounds that are useful in electronic applications. It also relates to electronic devices in which the active layer includes such a deuterated compound. 2. The compound of claim 1 , which is at least 10% deuterated.3. The compound of claim 1 , which is at least 50% deuterated.4. The compound of claim 1 , which is 100% deuterated.5. The compound of claim 1 , wherein Aris a nitrogen-containing heteroaromatic group.7. The compound of claim 6 , wherein Ris selected from D and aryl.9. The compound of claim 1 , wherein Rand Rare aryl.10. The compound of claim 1 , wherein Rand Rare H or D.11. The compound of claim 1 , selected from Compounds H1 through H14.12. An organic thin-film transistor comprising:a substratean insulating layer;a gate electrode;a source electrode;a drain electrode; andan organic semiconductor layer comprising an indolocarbazole compound having at least one deuterium substituent;wherein the insulating layer, the gate electrode, the semiconductor layer, the source electrode and the drain electrode can be arranged in any sequence provided that the gate electrode and the semiconductor layer both contact the insulating layer, the source electrode and the drain electrode both contact the semiconductor layer and the electrodes are not is in contact with each other.14. An organic electronic device comprising a first electrical contact layer claim 1 , a second electrical contact layer claim 1 , and at least one active is layer therebetween claim 1 , wherein the active layer comprises an indolocarbazole compound having at least one deuterium substituent.16. The device of claim 14 , wherein the active layer is an electroactive layer which further comprises an electroactive dopant capable of electroluminescence having an emission maximum between 380 and 750 nm.17. The device of claim 15 , wherein the active layer is an electroactive layer and consists essentially of a compound having Formula I or Formula II ...

Compounds Having Semiconducting Properties and Related Compositions and Devices

Disclosed are new compounds having semiconducting properties. Such compounds can be processed into thin film semiconductors that exhibit high carrier mobility and/or good current modulation characteristics. 4. The compound of claim 1 , wherein M comprises a thieno[3 claim 1 ,2-b]thiophene moiety.7. The compound of claim 1 , wherein Rand Rindependently are selected from the group consisting of a branched Calkyl and haloalkyl group.8. The compound of claim 1 , wherein Rand Rindependently are a branched Calkyl group.9. The compound of claim 1 , wherein each of Rand Ris CHR′R″ claim 1 , wherein R′ is selected from a linear Calkyl group and a linear Chaloalkyl group; and R″ is selected from CH claim 1 , CF claim 1 , CH claim 1 , CHCF claim 1 , CFCH claim 1 , and CF.10. A thin film semiconductor comprising a compound of .11. A composite comprising a substrate and the thin film semiconductor of deposited on the substrate.12. An electronic device claim 10 , an optical device claim 10 , or an optoelectronic device comprising the thin film semiconductor of .13. A field effect transistor comprising a source electrode claim 10 , a drain electrode claim 10 , a gate electrode claim 10 , and the thin film semiconductor of in contact with a dielectric material.14. The field effect transistor of claim 13 , wherein the field effect transistor has a structure selected from top-gate bottom-contact structure claim 13 , bottom-gate top-contact structure claim 13 , top-gate top-contact structure claim 13 , and bottom-gate bottom-contact structure.15. The field effect transistor of claim 13 , wherein the dielectric material comprises an organic dielectric material.16. The field effect transistor of claim 13 , wherein the dielectric material comprises an inorganic dielectric material or a hybrid organic/inorganic dielectric material.17. An electroluminescent display device comprising a plurality of field effect transistors according to .18. An organic light-emitting transistor comprising a ...

COMPOUNDS FOR USE IN LIGHT-EMITTING DEVICES

Compounds including optionally substituted Ring Systems 1-4 may be used as host in light-emitting devices. 2. A light-emitting layer comprising a compound of .3. The light-emitting layer of claim 2 , wherein the compound is a host.5. A light-emitting device comprising the compound of .6. The light-emitting device of claim 5 , further comprising a light-emitting layer that contains the compound.7. The light emitting device of claim 6 , wherein the compound is a host in the light-emitting layer.9.10. The light-emitting device of claim 5 , further comprising a hole-transport layer disposed between the light-emitting layer and an anode.11. The light-emitting device of claim 7 , further comprising a hole-transport layer disposed between the light-emitting layer and an anode.12. The light-emitting device of claim 5 , further comprising an electron-transport layer disposed between the light-emitting layer and a cathode.13. The light-emitting device of claim 7 , further comprising an electron-transport layer-disposed between the light-emitting layer and a cathode.14. The light-emitting device of claim 10 , further comprising an electron-transport layer disposed between the light-emitting layer and a cathode.15. The light-emitting device of claim 10 , further comprising an electron-transport layer disposed between the light-emitting layer and a cathode.16. The light-emitting device of claim 5 , wherein the light-emitting device emits white light. This application is a continuation of U.S. patent application Ser. No. 13/033,473, filed Feb. 23, 2011, which claims the benefit of U.S. Provisional Patent Application No. 61/426,259, filed Dec. 22, 2010, both of which are incorporated by reference herein in their entirety.1. FieldThe embodiments include compounds for use in light-emitting devices.2. Description of the Related ArtOrganic light-emitting devices have been widely developed for flat panel displays, and are moving fast toward solid state lighting (SSL) applications. ...

Use of FAAH Inhibitors for Treating Parkinson's Disease and Restless Legs Syndrome

The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD. 182-. (canceled)83. A method of treating or preventing an impulse control disorder (ICD) , dopamine dysregulation syndrome (DDS) or sleep disorder arising from the treatment of a patient suffering from Parkinson's disease (PD) , restless legs syndrome (RLS) or periodic limb movement disorder (PLMD) or combination thereof with a dopaminergic agent , comprising administering a therapeutically effective amount of a FAAH inhibitor , or a therapeutically effective amount of a dopaminergic agent and a therapeutically effective amount of a FAAH inhibitor to said patient.84. The method according to claim 83 , wherein the dopaminergic agent is a dopamine replacement agent claim 83 , a dopamine agonist claim 83 , a dopamine uptake inhibitor or a monoamine oxidase inhibitor.85. The method according to claim 84 , wherein the dopamine replacement agent comprises melevodopa or L-3 claim 84 ,4-dihydroxyphenylalanine (levodopa claim 84 , L-DOPA) claim 84 , or an AADC enzyme inhibitor or both an AADC enzyme inhibitor and a COMT inhibitor.86. The method according to claim 85 , wherein the AADC enzyme inhibitor is carbidopa or benserazide and the COMT inhibitor claim 85 , if present claim 85 , is entacapone or tolcapone.87. The method according to claim 84 , wherein the dopamine agonist is bromocriptine (Parlodel®) claim 84 , pergolide (Permax®) claim 84 , pramipexole (Mirapex®) claim 84 , ropinirole (Requip®) claim 84 , rotigotine (Neupro®) claim 84 , cabergoline (Dostinex®) claim 84 , apomorphine (Apokyn®) claim 84 , lisuride (Dopergine®) or ...

Etravirine Formulations and Uses Thereof

Provided herein is a pharmaceutical formulation of etravirine, said formulation comprising: etravirine; a dipolar aprotic solvent; a non-ionic water dispersible surfactant; and water. Further provided is a pharmaceutical formulation of etravirine, said formulation comprising: etravirine; a non-ionic water dispersible surfactant; and water.

NITROGEN-CONTAINING AROMATIC COMPOUND, ORGANIC SEMICONDUCTOR MATERIAL, AND ORGANIC ELECTRONIC DEVICE

Provided are a nitrogen-containing aromatic heterocyclic compound useful as an organic semiconductor material and an organic electronic device using this compound. The nitrogen-containing aromatic heterocyclic compound has a fused indole skeleton represented by the following formula (1), the organic semiconductor material contains the said compound, and the organic electronic device uses the said organic semiconductor material. In general formula (1), X is N-A′, O, S, or Se; A is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more; and R is a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group exclusive of a fused heterocycle consisting of 4 rings or more. 2. An organic electronic dcvice as described in wherein claim 1 , in general formula (1) claim 1 , Xis N—A′.3. (canceled)4. (canceled)5. (canceled)6. An organic electronic device as described in wherein the organic electronic device is a light-emitting device claim 1 , a thin film transistor claim 1 , or a photovoltaic device.7. An organic electronic device as described in wherein the light-emitting device is an organic electroluminescent device. This invention relates to a novel nitrogen-containing aromatic compound and an organic electronic device using the said compound and, further, to a light-emitting device, a thin film transistor, and a photovoltaic device utilizing the said compound as an organic semiconductor material.In recent years, organic electronic devices in which organic compounds are used as semiconductor materials have enjoyed remarkable prosperity. Typical examples of their applications include organic electroluminescent devices (hereinafter referred to as organic EL device) that are expected to become next generation flat panel displays, organic thin ...

INDOLE DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE

Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity. 2. The method of claim 1 , further comprising administering to the subject a second therapeutic agent claim 1 , selected from among abarelix (Plenaxis®); aldesleukin (Prokine®); Aldesleukin (Proleukin®); Alemtuzumab (Campath®); alitretinoin (Panretin®); allopurinol (Zyloprim®); altretamine (Hexalen®); amifostine (Ethyol®); anastrozole (Arimidex™); arsenic trioxide (Trisenox®); asparaginase (Elspar®); azacitidine (Vidaza®); bevacizumab (Avastin®); bexarotene (Targretin®); bleomycin (Blenoxane®); bortezomib (Velcade®); busulfan (Busulfex®); busulfan (Myleran®); calusterone (Methosarb®); capecitabine (Xeloda®); carboplatin Paraplatin®); carmustine (BCNU claim 1 , BiCNU); carmustine (Gliadel®); celecoxib (Celebrex®); cetuximab (Erbitux®); chlorambucil (Leukeran®); cisplatin (Platinol®); cladribine (Leustatin®); clofarabine (Clolar®); cyclophosphamide (Cytoxan®); cytarabine (Cytosar-U®); cytarabine liposomal (DepoCyt); dacarbazine (DTIC-Dome); dactinomycin (actinomycin D claim 1 , Cosmegen®); Darbepoetin alfa (Aranesp®); dasatinib (Sprycel®); daunorubicin liposomal (DanuoXome); daunorubicin (daunomycin claim 1 , Daunorubicin®); daunorubicin (daunomycin claim 1 , Cerubidine®); decitabine (Dacogen®); denileukin (Ontak®); dexrazoxane (Zinecard®); docetaxel (Taxotere®); doxorubicin (Adriamycin®); doxorubicin liposomnal (Doxil®); dromostanolone propionate; epirubicin (Ellence®); Epirubicin; Epoetin alfa (EPOGEN®); erlotinib (Tarceva®); estramustine (Emcyt®); etoposide phosphate (Etopophos®); etoposide (VP-16; Vepesid®); exemestane (AROMASIN®); Filgrastim (Neupogen®); floxuridine (FUDR); fludarabine (Fludara®); fluorouracil (5-FU ...

Fatty Acid Conjugates of Quetiapine, Process for Making and Using the Same

The presently described technology provides a novel class of prodrugs of quetiapine that can be synthesized by chemically conjugating fatty acids to quetiapine. Pharmaceutical compositions and methods of synthesizing conjugates of the present technology are also provided. Methods of treating patients with the compositions of the present technology are also provided. 1. A composition for treating a psychiatric disorder in a subject , comprising a prodrug conjugate of 2-(2-(4-(dibenzo[b ,f][1 ,4]thiazepin-11-yl)piperazin-1-yl)ethoxy)ethanol (quetiapine) and a straight chain , saturated fatty acid having the general formula of CH—COH , wherein n is 1-7.3. The composition of claim 1 , wherein n is 1.4. The composition of claim 1 , wherein n is 4.5. The composition of claim 1 , wherein n is 7.6. The composition of claim 1 , wherein the straight chain claim 1 , saturated fatty acid is acetate or ethanoate.8. The composition of claim 1 , wherein the straight chain claim 1 , saturated fatty acid is valerate or pentanoate.10. The composition of claim 1 , wherein the straight chain claim 1 , saturated fatty acid is caprylate or octanoate.12. The composition of claim 1 , wherein the composition has a higher relative bioavailability than non-conjugated quetiapine when administered orally.13. The composition of claim 1 , wherein the prodrug conjugate is in a salt form selected from the group consisting of acetate claim 1 , L-aspartate claim 1 , besylate claim 1 , bicarbonate claim 1 , carbonate claim 1 , D-camsylate claim 1 , L-camsylate claim 1 , citrate claim 1 , edisylate claim 1 , formate claim 1 , fumarate claim 1 , gluconate claim 1 , hydrobromide/bromide claim 1 , hydrochloride/chloride claim 1 , D-lactate claim 1 , L-lactate claim 1 , D claim 1 ,L-lactate claim 1 , D claim 1 ,L-malate claim 1 , L-malate claim 1 , mesylate claim 1 , pamoate claim 1 , phosphate claim 1 , succinate claim 1 , sulfate claim 1 , bisulfate claim 1 , D-tartrate claim 1 , L-tartrate claim 1 , D ...

POLYMORPHS OF SAXAGLIPTIN HYDROCHLORIDE AND PROCESSES FOR PREPARING THEM

The invention provides polymorphs of Saxagliptin hydrochloride, processes for preparing polymorphs of Saxagliptin hydrochloride, and pharmaceutical compositions of polymorphs of Saxagliptin hydrochloride. 118-. (canceled)19. Amorphous Saxagliptin hydrochloride.20. The amorphous Saxagliptin hydrochloride of claim 19 , characterized by an X-ray powder diffraction pattern substantially as depicted in .21. A pharmaceutical composition comprising the amorphous Saxagliptin hydrochloride according to any one of and claim 19 , and at least one pharmaceutically acceptable excipient.22. A method of treating a patient suffering from type 2 diabetes claim 21 , comprising administering a pharmaceutical composition according to . This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application Nos. 61/389,399, filed on Oct. 4, 2010; 61/415,017, filed on Nov. 18, 2010; 61/418,951, filed on Dec. 2, 2010; 61/424,889, filed on Dec. 20, 2010; 61/436,747, filed on Jan. 27, 2011; 61/448,316, filed on Mar. 2, 2011; 61/467,125, filed on Mar. 24, 2011; 61/482,362, filed on May 4, 2011; and 61/484,761, filed on May 11, 2011.The invention relates to polymorphs of Saxagliptin hydrochloride, processes for preparing them, and pharmaceutical compositions thereof.Saxagliptin, (1S,3S,5S)-2-((2S)-2-Amino-2-(3-hydroxyadamantan-1-yl)-acetyl)-2-azabicyclo[3.1.0]hexane-3-carbonitrile of the following chemical structure:is a dipeptidyl peptidase IV (DPP4) inhibitor. Saxagliptin is marketed under the trade name ONGLYZA® by Bristol-Myers Squibb for the treatment of type 2 diabetes.Saxagliptin and its hydrochloride and trifluoroacetic acid salts are disclosed in U.S. Pat. No. 6,395,767. In addition, U.S. Pat. No. 7,420,079 discloses Saxagliptin and its hydrochloride, trifluoroacetic acid and benzoate salts, as well as Saxagliptin monohydrate.U.S. 2009/054303 and the corresponding WO 2008/131149 application disclose several crystalline forms of Saxagliptin and of Saxagliptin salts ...

GPR 17 Agonists and Screening Assay

The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I. 17.-. (canceled)9. The method according to claim 8 , wherein the GPR17 mediated disease is multiple sclerosis.11. The screening assay according to further comprising means for determining the GPR17 activity claim 10 ,wherein, optionally, said means for determining the GPR17 activity is selected from one or more of the group consisting of:a. means for determining the release of calcium from intracellular calcium stores associated with GPR17 activation, said means optionally comprising a cell membrane permeable indicator which binds to calcium released within the cell thereby providing a measurable signal, preferably fluorescence or luminescence;{'sub': Y', 'Y, 'sup': '35', 'b. means for determining GTPS binding to heterotrimeric G proteins, wherein said heterotrimeric G protein is optionally SGTPS;'}c. means for determining the inhibition of cAMP formation or its increase associated with GPR17 activation, said means optionally comprising a stimulator of the adenylyl cyclase and a suitable cAMP indicator system;d. means for determining the increase in inositolphosphates (IP), quantified as IP1, said means optionally comprising a suitable IP 1 detector system; ande. means for determining the recruitment of cytoplasmic β-arrestin proteins, optionally by detection of the B-arrestin translocation to the receptor using fluorescence or bioluminescence resonance energy transfer.12. The screening assay according to (c) wherein said stimulator of the adenylyl cyclase is forskolin claim 11 , and wherein said cAMP indicator system is a competitive immunoassay claim 11 , optionally providing a fluorescence signal.13. (canceled)14. A compound selected from3-(2- ...

(AZA)INDOLE DERIVATIVE SUBSTITUTED IN POSITION 5, PHARMACEUTICAL COMPOSITION COMPRISING IT, INTERMEDIATE COMPOUNDS AND PREPARATION PROCESS THEREFOR

An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor. 125-. (canceled)27. An intermediate compound according to claim 26 , wherein R1 is:{'sub': 1', '3', '1', '3', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', '2', 'n', '2', '2', 'n', '2', '1', '3', '1', '3', '1', '3, 'sup': I', 'II', 'III', 'II', 'III', 'I', 'II', 'I', 'I', 'II', 'I', 'I', 'I', 'II', 'III, 'a (C-C)alkyl, (C-C)alkylOR, (CH)NRR, (CH)CONRR, (CH)COR, (CH)COOR, (CH)OCOR, SOR, (CH)NRSOR, or (CH)SORgroup, optionally substituted with 1 to 3 hydroxy groups, wherein n is an integer from 1 to 4, Ris a (C-C)alkyl or (C-C)alkylOH group, and Rand R, which may be identical or different, are a hydrogen atom or a (C-C)alkyl group; or'}{'sub': 1', '3', '1', '3', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', '2', 'n', '2', '2', 'n', '2', '3', '2', '5', '2', '2', '4', '3', '2', '5, 'sup': I', 'II', 'III', 'I', 'II', 'I', 'I', 'II', 'I', 'I', 'I', 'II', 'III, 'a (C-C)alkyl, (C-CalkylOR, (CH)CONRR, (CH)COR, (CH)COOR, (CH)OCOR, SOR, (CH)NRSOR, or (CH)SORgroup, optionally substituted with 1 to 3 hydroxy groups, wherein n is an integer from 1 to 3, Ris a CH, CH, CHOH, a CHOH group, and Rand R, which may be identical or different, are a hydrogen atom or a CH, CHgroup.'}28. An intermediate compound according to claim 26 , wherein W is:{'sub': 1', '3', '1', '4', '1', '3', '2', '3', '2', 'p', '2', 'q', '2', 'p', '2', 'q, 'a σ bond, a (C-C)alkyl, (C-C)alkenyl, O(C-C)alkyl, O(C-C)alkenyl, C(O)NH, (CH)CO(CH), or (CH)C(OH)(CH)group, wherein p and q, which may be identical or different, are an integer from 1 to 3; or'}{'sub': 2', '2', '4', '2', '2', '4', '2', 'p', '2', 'q', '2', 'p', '2', 'q, 'a σ bond, a CH, CH, CH═CH, OCH, OCH, OCH═CH, C(O)NH, (CH)CO(CH), or (CH)C(OH)(CH)group, wherein p and q, which may be ...

METHOD FOR PRODUCING PHENYL-SUBSTITUTED HETEROCYCLIC DERIVATIVE BY MEANS OF COUPLING METHOD USING PALLADIUM COMPOUND

The present invention provides a method for producing a xanthine oxidase inhibitor, which is a therapeutic agent for hyperuricemia, or intermediates of the same, said method being efficient and using a short process. The present invention is a novel coupling method for obtaining a compound represented by formula (3) by bringing about a coupling reaction between a compound represented by formula (1) and a compound represented by formula (2), in the presence of a palladium compound, a ligand capable of coordinating to the palladium compound, a base, a C-Ccarboxylic acid, and at least one kind of additive. 2. The method of production according to claim 1 , wherein A is a Cto Calkyl group.3. The method of production according to claim 1 , wherein A is an isobutyl group.4. The method of production according to claim 1 , wherein X is an oxygen atom.5. The method of production according to claim 1 , wherein Ris a hydrogen atom.6. The method of production according to claim 1 , wherein Ris a cyano group.7. The method of production according to claim 1 , wherein Y represents a halogen atom claim 1 , —OCO—(Cto Calkyl group) claim 1 , —OCO— (phenyl group) claim 1 , —OSO—(Cto Calkyl group) claim 1 , —OSO-(phenyl group) claim 1 , or a diazonium group claim 1 , and claim 1 , in Y claim 1 , the Cto Calkyl group can be substituted with 1 to 3 halogen atoms claim 1 , and the phenyl group can be substituted with 1 to 5 optional substituents selected from halogen atoms and Cto Calkyl groups.9. The method of production according to claim 1 , wherein Ris COORand Ris a Cto Calkyl group.10. The method of production according to claim 1 , wherein Ris a methyl group.11. The method of production according to claim 1 , wherein the palladium compound is zerovalent palladium claim 1 , or a salt of monovalent or divalent palladium.12. The method of production according to claim 1 , wherein the palladium compound is palladium(II) acetate (Pd(OAc)) claim 1 , palladium(II) propionate (Pd(O(C═O)CHCH ...

PHOSPHAPHENANTHRENE-CARBAZOLE-BASED ORGANIC LIGHT-EMITTING COMPOUND, AND ORGANIC LIGHT-EMITTING DEVICE COMPRISING SAME

Provided are a phosphaphenanthrene-carbazole-based organic light-emitting compound having superior light emitting properties, and an organic light-emitting device including the same. 3. A light-emitting device comprising the phosphaphenanthrene-carbazole-based organic light-emitting compound of .4. The light-emitting device of claim 3 , wherein the phosphaphenanthrene-carbazole-based organic light-emitting compound is included in at least one layer selected from a group consisting of a hole injection layer claim 3 , a hole transfer layer claim 3 , an electron injection layer claim 3 , an electron transfer layer claim 3 , a light emitting layer claim 3 , and a mixed function layer thereof.5. A light-emitting device comprising a first electrode claim 1 , a second electrode claim 1 , and at least one organic layer disposed between the first and second electrodes claim 1 , wherein at least one of the organic layers includes the phosphaphenanthrene-carbazole-based organic light-emitting compound of .6. The light-emitting device of claim 5 , wherein the organic layer includes at least one layer selected from a group consisting of a hole injection layer claim 5 , a hole transfer layer claim 5 , an electron injection layer claim 5 , an electron transfer layer claim 5 , and a mixed function layer thereof and a light emitting layer.7. The light-emitting device of claim 6 , wherein the phosphaphenanthrene-carbazole-based organic light-emitting compound is included in at least one of the electron transport layer and the light emitting layer. The present invention relates to a phosphaphenanthrene-carbazole-based organic light-emitting compound having superior light-emitting properties, and an organic light-emitting device including the same.A organic light-emitting device, which is a self light-emitting device, has various advantages such as a wide viewing angle, a rapid response speed, a low driving voltage, or the like, and is currently applied as a next generation flat panel ...

Method for producing crystals of mutivalent metal salt of (2r, 4r) monatin

The present invention provides a method of efficiently producing a crystal of a (2R,4R)Monatin multivalent metal salt that has a good sweetness property and is excellent in storage stability. Specifically, the present invention provides the method of producing the crystal of the (2R,4R)Monatin multivalent metal salt comprising allowing an aldehyde or one or two or more enzymes capable of forming (2R,4R)Monatin from (2S,4R)Monatin to be acted on an aqueous solution containing the (2S,4R)Monatin in the presence of a multivalent metal ion to obtain the crystal of the (2R,4R)Monatin multivalent metal salt. The aldehyde may preferably be an aromatic aldehyde. The one or two or more enzyme may preferably be a racemase or one or more aminotransferases. The multivalent metal may preferably be a bivalent alkaline earth metal.

Continuous process for the alkylation of cyclic tertiary amines

A continuous process for the alkylation of tertiary amines and, in particular, to a continuous process for the quaternization of cyclic tertiary amines useful for the preparation of cyclic quaternary ammonium salts with high purity is described.

METHOD FOR THE SYNTHESIS OF AN AMINO ACETAL

The present invention relates to a method for the synthesis of an α amino acetal, comprising (i) oxidizing a tertiary amine in the presence of a copper catalyst, at least one oxidant and a solvent, or (ii) reacting a secondary amine and an aliphatic aldehyde in the presence of a copper catalyst, at least one oxidant and a solvent. 1. A method for the synthesis of an α-amino acetal , comprising(i) oxidizing a tertiary amine in the presence of a copper catalyst, at least one oxidant and a solvent, or(ii) reacting a secondary amine and an aliphatic aldehyde in the presence of a copper catalyst, at least one oxidant and a solvent.5. The method of claim 1 , wherein the reaction is carried out in the presence of a nitrogen donor ligand.6. The method of claim 5 , wherein the nitrogen donor ligand is N claim 5 ,N claim 5 ,N′ claim 5 ,N′-tetramethylethylenediamine (TMEDA).7. The method of claim 6 , wherein the molar ratio of copper catalyst:TMEDA is between about 1:1 and about 1:5.8. The method of claim 7 , wherein the molar ratio of copper catalyst:TMEDA is about 1:2.9. The method of claim 1 , wherein the copper catalyst is copper (II) halide or copper (I) halide.10. The method of claim 9 , wherein the halide is iodide claim 9 , bromide or chloride.11. The method of claim 10 , wherein the copper catalyst is selected from the group consisting of CuBr claim 10 , CuI claim 10 , CuI claim 10 , and CuBr.12. The method of claim 2 , wherein the copper catalyst is CuBror CuI.13. The method of claim 3 , wherein the copper catalyst is CuI claim 3 , CuBr or CuBr.14. The method of claim 1 , wherein the one or more alcohols are methanol or ethanol.1516.-. (canceled)17. The method of claim 1 , wherein the solvent is an organic solvent selected from the group consisting of acetonitrile (MeCN) claim 1 , methanol (MeOH) claim 1 , 1 claim 1 ,2-dichloroethane (DCE) claim 1 , tetrahydrofuran (THF) claim 1 , dimethyl sulfoxide (DMSO) claim 1 , and mixtures thereof.18. The method of claim 17 , ...

ORGANOSELENIUM MATERIALS AND THEIR USES IN ORGANIC LIGHT EMITTING DEVICES

The present invention provides organoselenium compounds comprising dibenzoselenophene, benzo[b]selenophene or benzo[c]selenophene and their uses in organic light emitting devices. 1. An organic light emitting device , comprising an organic layer positioned between an anode layer and a cathode layer , said organic layer comprising an organoselenium material selected from the group consisting of a compound comprising a dibenzoselenophene , a compound comprising a benzo[b]selenophene , and a compound comprising benzo[c]selenophene.46-. (canceled)73. The organic light emitting device of any of to claims 1 , wherein said organoselenium material is a host material claims 1 , and wherein said organic layer further comprises a dopant material.8. The organic light emitting device of claim 7 , wherein said organic layer is an emissive layer claim 7 , and wherein said dopant material is a phosphorescent or fluorescent dopant material.9. The organic light emitting device of claim 8 , wherein said dopant material is a phosphorescent dopant material.13. The organic light emitting device of claim 9 , further comprising one or more organic layers selected from the group consisting of a hole injecting layer claim 9 , an electron injecting layer claim 9 , a hole transporting layer claim 9 , an electron transporting layer claim 9 , a hole blocking layer claim 9 , an exciton blocking layer claim 9 , and an electron blocking layer.14. The organic light emitting device of claim 13 , wherein said hole transporting layer comprises an organoselenium material.15. The organic light emitting device of claim 13 , wherein said electron transporting layer comprises an organoselenium material.163. The organic light emitting device of any of to claims 1 , wherein said organic layer is a hole transporting layer or an electron transporting layer.17. (canceled)2022-. (canceled) This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application No. 61/100,229, filed Sep. 25, ...

PROCESSES AND INTERMEDIATES

The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections. 3. The process of claim 2 , wherein the 2-anion is prepared by treating the compound of Formula 6 with a strong lithium base in the presence of a complexing agent and an aprotic solvent.4. The process of claim 3 , wherein the base is sec-butyl lithium.5. The process of claim 4 , wherein the complexing agent is tetramethylethylenediamine claim 4 , tetraethylethylenediamine claim 4 , tetramethyl-1 claim 4 ,2-cyclohexyldiamine claim 4 , sparteine claim 4 , or 3 claim 4 ,7-dipropyl-3 claim 4 ,7-diazabicyclo[3.3.1]nonane.6. The process of claim 2 , wherein the complexing agent is tetramethylethylenediamine claim 2 , tetraethylethylenediamine claim 2 , tetramethyl-1 claim 2 ,2-cyclohexyldiamine claim 2 , or 3 claim 2 ,7-dipropyl-3 claim 2 ,7-diazabicyclo[3.3.1]nonane.7. The process of claim 2 , wherein the trans-/cis- ratio is 1 to 1.8. The process of claim 2 , wherein the trans-/cis- ratio is 60 to 40.9. The process of claim 2 , wherein the trans-/cis- ratio is 80 to 20.10. The process of claim 2 , wherein the trans/cis- ratio is 90 to 10.11. The process of claim 2 , wherein the trans-/cis- ratio is greater than 98 to 2.12. The process of claim 2 , wherein the complexing agent is D-sparteine.13. The process of claim 3 , wherein the lithium base is sec-butyl lithium and the complexing agent is 3 claim 3 ,7-dipropyl-3 claim 3 ,7-diazabicyclo[3.3.1]nonane to give a mixture of racemic trans-/cis-N-alkoxycarbonyl-octahydrocyclopenta[c]pyrrole-1-carboxylic acids of Formula 7 claim 3 , in which the trans/cis- ratio is greater than 90 to 10.14. The process of claim 13 , wherein the trans-N-alkoxycarbonyl-octahydrocyclopenta[c]pyrrole-1-carboxylic acid is trans-N-t-butoxycarbonyl-octahydrocyclopenta[c]pyrrole-1-carboxylic acid.16. The process of claim 15 , wherein the ...

CONDENSED-CYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DIODE INCLUDING THE SAME

Embodiments of the present invention are directed to a condensed-cyclic compound and an OLED including the same. 5. The condensed-cyclic compound of claim 1 , wherein Xin Formula 2 is N(R) claim 1 , B(R) claim 1 , or Si(R)(R) claim 1 , wherein Rand Rare each independently hydrogen claim 1 , deuterium claim 1 , a halogen atom claim 1 , a hydroxyl group claim 1 , a cyano group claim 1 , a nitro group claim 1 , an amino group claim 1 , an amidino group claim 1 , hydrazine claim 1 , hydrazone claim 1 , a carboxylic acid group or a salt thereof claim 1 , a sulfonic acid group or a salt thereof claim 1 , a phosphoric acid group or a salt thereof claim 1 , a substituted or unsubstituted C-Calkyl group claim 1 , a substituted or unsubstituted C-Calkenyl group claim 1 , a substituted or unsubstituted C-Calkynyl group claim 1 , a substituted or unsubstituted phenyl group claim 1 , a substituted or unsubstituted pentalenyl claim 1 , a substituted or unsubstituted indenyl claim 1 , a substituted or unsubstituted naphthyl group claim 1 , a substituted or unsubstituted azulenyl claim 1 , a substituted or unsubstituted heptalenyl claim 1 , a substituted or unsubstituted indacenyl claim 1 , a substituted or unsubstituted acenaphthyl group claim 1 , a substituted or unsubstituted fluorenyl group claim 1 , a substituted or unsubstituted phenalenyl group claim 1 , a substituted or unsubstituted phenanthrenyl group claim 1 , a substituted or unsubstituted anthryl group claim 1 , a substituted or unsubstituted fluoranthenyl group claim 1 , a substituted or unsubstituted triphenylenyl group claim 1 , a substituted or unsubstituted pyrenyl group claim 1 , a substituted or unsubstituted chrysenyl group claim 1 , a substituted or unsubstituted naphthacenyl group claim 1 , a substituted or unsubstituted picenyl group claim 1 , a substituted or unsubstituted perylenyl group claim 1 , a substituted or unsubstituted pentaphenyl group claim 1 , a substituted or unsubstituted hexacenyl group ...

Wnt inhibitors for human stem cell differentiation

Methods and small molecule compounds for stem cell differentiation and treatment of animals with diseases are provided. One example of a class of compounds that may be used is represented by the compound of Formula I and II: or a pharmaceutically acceptable salt or solvate thereof, wherein A, X, Q, R 1 , R 2 , R 3 , R 4 are as described herein.

DELTA CRYSTALLINE FORM OF THE ARGININE SALT OF PERINDOPRIL, A PROCESS FOR ITS PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT

Delta crystalline form of the compound of formula (I): 2. The delta crystalline form according to claim 1 , having the following X-ray powder diffraction peaks measured using a diffractometer with a copper anticathode and expressed in terms of Bragg's angle 2 theta: 4.3 claim 1 , 11.0 claim 1 , 11.1 claim 1 , 11.9 claim 1 , 12.5 claim 1 , 13.2 claim 1 , 14.6 claim 1 , 16.0 claim 1 , 19.2 claim 1 , 19.4 claim 1 , 20.0 claim 1 , 21.9 claim 1 , 22.2 and 22.6.5. A process for the preparation of the delta crystalline form according to claim 1 , comprising crystallisation or recrystallisation from a binary mixture of acetonitrile claim 1 , ethyl acetate or methyl tert-butyl ether and dimethyl sulphoxide or a ternary mixture of acetonitrile claim 1 , dimethyl sulphoxide and toluene claim 1 , at a temperature higher than 20° C.6. The process according to claim 5 , wherein the binary mixture of acetonitrile claim 5 , ethyl acetate or methyl tert-butyl ether and dimethyl sulphoxide has a ratio of acetonitrile/dimethyl sulphoxide claim 5 , ethyl acetate/dimethyl sulphoxide or methyl tert-butyl ether/dimethyl sulphoxide ranging from 90/10 w/w to 10/90 w/w.7. The process according to claim 5 , wherein the temperature of the medium is between 25 and 80° C. claim 5 , inclusive.8. The process according to claim 7 , wherein the mixture is heated to a temperature of from 60 to 80° C.9. The process according to claim 5 , wherein the mixture is seeded with the delta crystalline form.10. A pharmaceutical composition comprising claim 1 , as active ingredient claim 1 , the delta crystalline form according to claim 1 , in combination with one or more inert claim 1 , non-toxic claim 1 , pharmaceutically acceptable carriers.11. The pharmaceutical composition according to claim 10 , further comprising a diuretic claim 10 , a calcium antagonist or an If current inhibitor.12. The pharmaceutical composition according to claim 11 , wherein the diuretic is indapamide.13. The pharmaceutical ...

COMPOUNDS AND ORGANIC ELECTRONIC DEVICE USING THE SAME

The present invention provides a new compound and an organic electronic device using the same. The organic electronic device according to the present invention exhibits excellent properties in views of efficiency, driving voltage and a life span. 5. The compound of claim 4 , wherein the arylene group is a phenylene group or a naphthalene group claim 4 , and the aryl group is a phenyl group claim 4 , a naphthyl group claim 4 , a phenanthrenyl group claim 4 , a fluorene group claim 4 , a dimethylfluorene group claim 4 , a triphenylene group claim 4 , a benzocrycene group or a fluoranthrene group.9. The compound of claim 1 , wherein p is 0 claim 1 , and Yis heavy hydrogen claim 1 , a nitrile group claim 1 , a halogen group claim 1 , a substituted or unsubstituted boron group claim 1 , a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group.10. The compound of claim 1 , wherein Lis a substituted or unsubstituted arylene group or a substituted or unsubstituted heteroarylene group claim 1 , and{'sub': '1', 'Yis a substituted or unsubstituted boron group; a substituted or unsubstituted alkylamine group; a substituted or unsubstituted aralkylamine group; a substituted or unsubstituted arylamine group; a substituted or unsubstituted heteroarylamine group; a substituted or unsubstituted aryl group; a substituted or unsubstituted fluorenyl group; a substituted or unsubstituted carbazole group; or a substituted or unsubstituted heterocyclic group comprising one or more of N, O and S atoms.'}18. An organic electronic device comprising:a first electrode;a second electrode; andone or more organic material layers interposed between the first electrode and the second electrode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein one or more layers of the organic material layers comprise the compound of .'}19. The organic electronic device of claim 18 , wherein the organic material layer comprises one or more layers of a hole injection ...

Methods for Treating Parkinson's Disease Using Pro-Neurogenic Compounds

This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. 2. The method of claim 1 , wherein when A is CRR claim 1 , the carbon attached to Rand Ris substituted with four different substituents claim 1 , and is (R) or (S) configured.3. The method of claim 2 , wherein the compound or salt is (+) (dextrorotatory) or (−) (levororotatory).4. The method of claim 1 , wherein the effective amount of the compound or salt stimulates neurogenesis.5. The method of claim 1 , wherein the effective amount of the compound or salt reduces neuron cell death.6. The method of claim 1 , wherein the compound is selected from:R-1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;S-1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(2-iminopyridin-[(2H)-yl)propan-2-ol;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(phenylthio)propan-2-ol;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-hydroxypropyl)-N-(3-methoxyphenyl)acetamide;5-((3,6-dibromo-9H-carbazol-9-yl)methyl)-3-(3-methoxyphenyl)-oxazolidin-2-one;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2- ...

Methods of Treating Traumatic Brain Injury Using Pro-Neurogenic Compounds

This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death. 2. The method of claim 1 , wherein when A is CRR claim 1 , the carbon attached to Rand Ris substituted with four different substituents claim 1 , and is (R) or (S) configured.3. The method of claim 2 , wherein the compound or salt is (+) (dextrorotatory) or (−) (levororotatory).4. The method of claim 1 , wherein the effective amount of the compound or salt stimulates neurogenesis.5. The method of claim 1 , wherein the effective amount of the compound or salt reduces neuron cell death.6. The method of claim 1 , wherein the compound is selected from:R-1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;S-1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(2-iminopyridin-1(2H)-yl)propan-2-ol;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(phenylthio)propan-2-ol;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-hydroxypropyl)-N-(3-methoxyphenyl)acetamide;5-((3,6-dibromo-9H-carbazol-9-yl)methyl)-3-(3-methoxyphenyl)-oxazolidin-2-one;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-3-methoxyaniline;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-one;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-methoxypropyl)-3-methoxyaniline;1-(3,6-Dimethyl-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)propan-2-ol;1-(3-Bromo-6-methyl-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;1-(3,6-Dichloro-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)propan-2-ol;1-(5-bromo-2,3-dimethyl-1H-indol-1-yl)-3-(phenylamino)propan-2-ol;1-(3,6-Dibromo-9H-pyrido[3,4-b]indol-9-yl)-3-(phenylamino)propan-2-ol;1-(3-Azidophenylamino)-3-(3,6-dibromo-9H-carbazol-9-yl)propan-2-ol;1,3-Bis(3,6-dibromo-9H-carbazol-9-yl)propan-2-ol;1-(9H-Carbazol-9-yl)-3-(3,6-dibromo-9H-carbazol-9-yl)propan-2-ol;3-(3,6-Dibromo-9H-carbazol-9-yl)-2-hydroxy-N-(3-methoxyphenyl)-propanamide;Ethyl 5-(2-Hydroxy- ...

Methods of Treating Post-Traumatic Stress Disorder Using Pro-Neurogenic Compounds

This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death. 2. The method of claim 1 , wherein when A is CRR claim 1 , the carbon attached to Rand Ris substituted with four different substituents claim 1 , and is (R) or (S) configured.3. The method of claim 2 , wherein the compound or salt is (+) (dextrorotatory) or (−) (levororotatory).4. The method of claim 1 , wherein the effective amount of the compound or salt stimulates neurogenesis.5. The method of claim 1 , wherein the effective amount of the compound or salt reduces neuron cell death.6. The method of claim 1 , wherein the compound is selected from:R-1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;S-1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(2-iminopyridin-1(2H)-yl)propan-2-ol;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(phenylthio)propan-2-ol;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-hydroxypropyl)-N-(3-methoxyphenyl)acetamide;5-((3,6-dibromo-9H-carbazol-9-yl)methyl)-3-(3-methoxyphenyl)-oxazolidin-2-one;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-3-methoxyaniline;1-(3,6-dibromo-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-one;N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-methoxypropyl)-3-methoxyaniline;1-(3,6-Dimethyl-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)propan-2-ol;1-(3-Bromo-6-methyl-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)-propan-2-ol;1-(3,6-Dichloro-9H-carbazol-9-yl)-3-(3-methoxyphenylamino)propan-2-ol;1-(5-bromo-2,3-dimethyl-1H-indol-1-yl)-3-(phenylamino)propan-2-ol;1-(3,6-Dibromo-9H-pyrido[3,4-b]indol-9-yl)-3-(phenylamino)propan-2-ol;1-(3-Azidophenylamino)-3-(3,6-dibromo-9H-carbazol-9-yl)propan-2-ol;1,3-Bis(3,6-dibromo-9H-carbazol-9-yl)propan-2-ol;1-(9H-Carbazol-9-yl)-3-(3,6-dibromo-9H-carbazol-9-yl)propan-2-ol;3-(3,6-Dibromo-9H-carbazol-9-yl)-2-hydroxy-N-(3-methoxyphenyl)-propanamide;Ethyl 5-(2-Hydroxy- ...

Tetomilast Polymorphs

The present invention provides a tetomilast crystal that is industrially easily produced in a large volume. (1) a tetomilast hydrate crystal having a power X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. ; (2) an anhydrous tetomilast type A crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. ; (3) an anhydrous tetomilast type C crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. ; (4) a tetomilast acetonitrile solvate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in FIG. ; and (5) a mixture consisting of the above anhydrous tetomilast type A crystal and an anhydrous tetomilast type B crystal. These crystals are stable towards heat and moisture, and are also excellent in terms of the disintegration property and dissolution property of tablets. Accordingly, these crystals are preferably used as pharmaceutical compositions. 1. A tetomilast hydrate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in .2. A pharmaceutical composition comprising at least one type of tetomilast crystal selected from the group consisting of a tetomilast hydrate crystal , an anhydrous tetomilast type A crystal , an anhydrous tetomilast type C crystal , and a tetomilast acetonitrile solvate crystal with one or more pharmaceutically acceptable carriers , wherein the composition is in the form of a tablet , pill , powder , granule , capsule or suppository.3. A method of treating gastrointestinal ulcer claim 2 , cardiacischemic disease claim 2 , cerebrovascular disease claim 2 , a liver and kidney function improver used for disorders caused by transplantation claim 2 , microcirculation failure claim 2 , ...

NITROGENATED AROMATIC COMPOUND, ORGANIC SEMICONDUCTOR MATERIAL, AND ORGANIC ELECTRONIC DEVICE

Provided are a novel nitrogen-containing aromatic heterocyclic compound and an organic electronic device using the compound. This nitrogen-containing aromatic compound is represented by the general formula (1). Further, the present invention relates to organic electronic devices such as a light-emitting device, a thin-film transistor, and a photovoltaic device each using the nitrogen-containing aromatic compound. 2. A nitrogen-containing aromatic compound according to . claim 1 , wherein the n in the general formula (1) represents 0.3. A nitrogen-containing aromatic compound according to claim 1 , wherein the X's in the general formula (1) each represent N-A.4. A compound according to claim 1 , wherein the m in the general formula (1) represents 2 or 3.5. An organic semiconductor material claim 1 , comprising the nitrogen-containing aromatic compound according to .6. An organic semiconductor thin film claim 5 , which is formed of the organic semiconductor material according to .7. An organic electronic device claim 5 , which is obtained by using the organic semiconductor material according to .8. An organic electronic device according to claim 7 , wherein the organic electronic device is selected from a light-emitting device claim 7 , a thin-film transistor claim 7 , and a photovoltaic device.9. An organic electronic device according to claim 8 , wherein the light-emitting device comprises an organic electroluminescence device.10. An organic semiconductor material claim 2 , comprising the nitrogen-containing aromatic compound according to .11. An organic semiconductor material claim 3 , comprising the nitrogen-containing aromatic compound according to .12. An organic semiconductor material claim 4 , comprising the nitrogen-containing aromatic compound according to .13. An organic semiconductor thin film claim 10 , which is formed of the organic semiconductor material according to .14. An organic semiconductor thin film claim 11 , which is formed of the organic ...

AROMATIC AMINE DERIVATIVE AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME

An aromatic amine derivative with a specific structure having a carbazole skeleton to which a diarylamino group bonds via a bonding group. An organic electroluminescence device which is composed of one or more organic thin film layers including at least one light emitting layer sandwiched between a cathode and an anode, wherein at least one of the organic thin film layers contains the aromatic amine derivative singly or as its mixture component. Organic electroluminescence devices with enhanced efficiency of light emission and a compound realizing the devices are provided. 121-. (canceled)23. The organic electroluminescence device according to claim 22 , wherein Lin the general formulae (1-a) claim 22 , (1-b) claim 22 , (1-c) claim 22 , (1-d) claim 22 , (1-e) and (1-f) represents an unsubstituted arylene group having 6 to 60 carbon atoms forming the aromatic ring claim 22 , an unsubstituted fluorenylene group or an unsubstituted heteroarylene group having 5 to 60 atoms forming a ring; Arand Areach independently represents an unsubstituted aryl group having 6 to 60 carbon atoms forming the aromatic ring or an unsubstituted heteroaryl group having 5 to 60 atoms forming a ring; Rrepresents an unsubstituted aryl group having 6 to 60 carbon atoms forming the aromatic ring; Rrepresents a hydrogen atom claim 22 , an unsubstituted aryl group having 6 to 60 carbon atoms forming the aromatic ring or an unsubstituted alkyl group having 1 to 50 carbon atoms; and the aromatic amine derivative represented by general formula (1-a) claim 22 , (1-b) claim 22 , (1-c) claim 22 , (1-d) claim 22 , (1-e) or (1-f) has 1 or 2 carbazole structures.24. The organic electroluminescence device according to claim 22 , comprising at least one organic amine derivative of formula (1-b) claim 22 , (1-c) claim 22 , (1-d) claim 22 , (1-e) and (1-f) wherein Ar′ claim 22 , Arto Ar claim 22 , Ar claim 22 , Ar claim 22 , Arand Areach independently represents a substituted or unsubstituted phenyl group ...

OXIME ESTER

Compounds of the formula (I), wherein R, R, R, R, R, R, Rand Rfor example independently of each other are hydro-gen, C-Calkyl, (II), CORor NO, provided that at least one pair of Rand R, Rand R, Rand R, Rand R, Rand R, or Rand Ris (III); R, R, Rand Rfor example independently of each other are hydrogen, C-Calkyl which optionally substituted; or R, R, R, and Rindependently of each other are unsubstituted or substituted phenyl; X is CO or a direct bond; Ris for example C-Calkyl which optionally is substituted, C-Calkenyl, C-Ccycloalkenyl, C-Calkinyl, C-C-cycloalkyl, phenyl or naphthyl both of which are optionally substituted; Ris for example hydrogen, C-Ccycloalkyl, C-Calkenyl, C-Calkoxy, C-Calkyl, phenyl or naphthyl; Ris for example C-Caryl or C-Cheteroaryl; Ris for example C-Caryl which is unsubstituted or substituted by one or more C-Calkoxy or C-Calkyl; are in particular suitable as photoinitiators for color filter applications. 4. A photopolymerizable composition , comprising:an ethylenically unsaturated photopolymerizable compound; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'as a photoinitiator, the compound of .'}5. The photopolymerizable composition according to claim 4 ,wherein an ethylenically unsaturated photopolymerizable compound is a resin obtained by a process comprising reacting a saturated or unsaturated polybasic acid anhydride with a product obtained by a process comprising reacting an epoxy resin and an unsaturated monocarboxylic acid.6. The photopolymerizable composition according to claim 4 , further comprising:an additional photoinitiator;an additional additive; orany combination thereof.7. The photopolymerizable composition according to claim 6 , as the additional additive claim 6 , the photopolymerizable composition comprises a pigment or a mixture of pigments.8. The photopolymerizable composition according to claim 6 , as the additional additive claim 6 , the photopolymerizable composition comprises a dispersant or a mixture of ...

COMPOSITIONS AND METHODS FOR INHIBITING THE PROLIFERATION OF CELLS

The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like. 2. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier. This application is a continuation of pending U.S. patent application Ser. No. 11/643,614, filed Dec. 21, 2006, which is a Divisional of allowed U.S. patent application Ser. No. 10/427,211, filed May 1, 2003 (now U.S. Pat. No. 7,572,788), which is a Continuation-in-Part of abandoned U.S. patent application Ser. No. 10/217,878, filed Aug. 13, 2002, which is a Continuation of allowed U.S. patent application Ser. No. 09/767,283, filed Jan. 22, 2001 (now U.S. Pat. No. 7,220,739), which is a Continuation of allowed U.S. patent application Ser. No. 09/700,101, filed Nov. 8, 2000 (now U.S. Pat. No. 7,125,866), which is the National entry of expired International Patent Application No. PCT/US00/11599 filed Apr. 27, 2000, which claims priority to expired U.S. Provisional Application No. 60/131,761, filed Apr. 30, 1999, to expired U.S. Provisional Application No. 60/165,511, filed Nov. 15, 1999, and to expired U.S. Provisional Application No. 60/191,855, filed Mar. 24, 2000. Abandoned U.S. application Ser. No. 10/217,878 also claims priority to expired U.S. Provisional Application No. 60/312,560, filed Aug. 15, 2001, to expired U.S. Provisional Application No. 60/313,689, filed Aug. 20, 2001, and to expired U.S. Provisional Application No. 60/396,670, filed Jul. 18, 2002. Each aforementioned application is specifically incorporated herein by reference in its entirety.This invention was made in part with government support under Grant Nos. GM46831 and ...

PHOTOACID COMPOSITIONS HAVING EXTENDED LIFETIME OF PROTON DISSOCIATION STATE

A photoacid includes a nucleophilic (NuH) moiety having a photodissociable proton, an electron accepting (EA) moiety, and a bridge structure (X) bonded to both the NuH moiety and EA moiety positioned between the NuH and EA moieties. The NuH and EA moieties each include respective structure so that the EA moiety bonds to a proton photodissociated form of the NuH moiety during a reversible photoinduced intramolecular reaction to form a ring, which has been found to significantly increase the lifetime of the proton dissociation state. 1. A photoacid composition , comprising:a nucleophilic (NuH) moiety having a photodissociable proton;an electron accepting (EA) moiety, anda bridge structure (X) bonded to both said NuH moiety and said EA moiety positioned between said NuH moiety and said EA moiety,wherein said NuH moiety and said EA moiety include respective structure so that said EA moiety bonds to a proton photodissociated form of said NuH moiety during a reversible photoinduced intramolecular reaction to form a ring.2. The photoacid composition of claim 1 , wherein said NuH moiety and said EA moiety each include at least one ring.3. The photoacid composition of claim 1 , wherein said NuH moiety comprises a heteroaromatic structure with more than one nitrogen atom.4. The photoacid composition of claim 1 , wherein said bridge structure comprises N which provides a C═N bond with a C of said EA moiety.5. The photoacid composition of claim 1 , wherein said bridge structure comprises CH which provides a C═C bond with a C of said EA moiety.6. The photoacid composition of claim 3 , wherein said heteroaromatic structure comprises indazole claim 3 , pyrazole claim 3 , benzotriazole claim 3 , or triazole.7. The photoacid composition of claim 1 , wherein said NuH moiety comprises a protonated merocyanine and said EA moiety comprises a sulfonate group.8. A method of controlling a process involving protons claim 1 , comprising: a nucleophilic (NuH) moiety having a photodissociable ...

ORGANIC ELECTROLUMINESCENT ELEMENT

Provided are a novel nitrogen-containing aromatic heterocyclic compound and an organic electronic device using the compound. Specifically provided is an organic electroluminescent device, including a plurality of organic layers between an anode and a cathode laminated on a substrate, in which at least one of the organic layers contains a nitrogen-containing aromatic compound represented by the following formula (1). In the formula, L represents an n+m-valent group arising from an alkane, a cycloalkane, an aromatic hydrocarbon, an aromatic heterocyclic compound, a triarylamine, or a diarylsulfone, A represents an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a silyl group, an acyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group, X represents C(R), oxygen, S, or Se, R represents H, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group, m represents an integer of 1 to 4, and n represents an integer of 0 to 3. The total number of m and n is 2 to 4. 3. An organic electroluminescent device according to claim 2 , wherein p in the general formula (2) represents 2 or 3.4. An organic electroluminescent device according to claim 1 , wherein the layer which contains the compound represented by the general formula (1) comprises at least one layer selected from the group consisting of a light-emitting layer claim 1 , a hole-transporting layer claim 1 , and an electron-blocking layer.5. An organic electroluminescent device according to claim 4 , wherein the layer which contains the compound represented by the general formula (1) comprises a light-emitting layer containing a phosphorescent light-emitting dopant.6. An organic electroluminescent device according to claim 2 , wherein the layer which contains the compound represented by the general formula (1) comprises at least one layer selected from the group consisting of a light-emitting layer claim 2 , ...

Potent, stable and non-immunosuppressive anti-cd4 antibodies

Novel antibodies and their fragments are disclosed that specifically bind to CD4. Anti-CD4 antibodies are disclosed having amino acid substitutions in the hinge region that prevent intrachain disulfide bond formation resulting in antibody molecules with surprisingly improved bivalent stability. Increased stability facilitates manufacturing and provides increased in vivo stability. Antibodies are also disclosed that have amino acid substitutions that reduce binding to Fc receptor and ADCC activity that also result in a surprising effect on CD4 internalization. In addition, genes for such antibodies are disclosed that have been modified such that they have increased expression over their unmodified counterparts.

Detection of Synthetic Cannabinoids

The invention describes methods and kits for detecting and determining current and future synthetic cannabinoids from the JWH and RCS families. Unique antibodies derived from novel immunogens enable said methods and kits.

COMPOSITION AND METHODS FOR TREATING GLIOBLASTOMA

The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful the treatment of glioblastoma. 2. The compound according to claim 1 , wherein X is CH.3. The compound according to claim 1 , wherein Ris C-Calkyl or C-Calkoxy.4. The compound according to claim 3 , wherein Ris methyl or methoxy.5. The compound according to claim 1 , wherein Ris H.6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. The compound according to claim 1 , wherein Rand Rtaken together with the atoms to which they are attached form a 6-membered heterocyclyl optionally substituted with one to four R.12. The compound according to claim 1 , wherein Rand Rare each independently H claim 1 , C-Calkoxy claim 1 , C-Chaloalkoxy claim 1 , halogen claim 1 , or —OH.13. (canceled)15. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to and one or more pharmaceutically acceptable diluents claim 1 , preservatives claim 1 , solubilizers claim 1 , emulsifiers claim 1 , adjuvants claim 1 , excipients claim 1 , or carriers.16. A method of treating or inhibiting glioblastoma claim 1 , acognition disorder claim 1 , schizophrenia claim 1 , Alzheimer's disease and dementia claim 1 , Parkinson's disease claim 1 , depression claim 1 , multiple sclerosis claim 1 , amyotrophic lateral sclerosis (ALS) claim 1 , Huntington's disease claim 1 , Fronto temporal dementia claim 1 , parkinsonism linked to chromosome 17 claim 1 , and prion diseases claim 1 , comprising administering to the subject an effective amount of a compound according to .17. The method according to claim 16 , wherein the method is for treating or inhibiting glioblastoma.1832-. (canceled)34. A method of screening for therapeutic agents useful in the treatment of glioblastomas in a subject comprising the steps of:contacting a test compound with a GPR124 polypeptide or a fragment thereof;measuring a ...

TRYPTAMINE DERIVATIVES, THEIR PREPARATION AND THEIR USE IN GASTROPATHY

The synthesis and evaluation of gastroprotective effect of different tryptamine derivatives. Tryptamine derivatives have been synthesized by formation of amide or ester with some known anti oxidant molecules. These derivatives show excellent antioxidant property in vitro. Among all the derivatives the compound SEGA (3a), that was prepared by the combination of serotonin with gallic acid shows the greater antioxidant property than the other synthesized compounds both in vivo and in vitro. SEGA(3a) shows the gastroprotective effect against NSAIDs (indomethacin or diclofenac)-induced gastropathy in dose dependent manner and also accelerates the healing from injury. It prevents the NSAIDs-induced mitochondrial oxidative stress in vivo. This derivative prevents NSAID-induced mitochondrial oxidative stress-mediated apoptosis in vivo by preventing the activation of caspase 9 and caspase-3 and restores NSAIDs-mediated collapse of mitochondroial transmembrane potential and dehydrogenase activity. SEGA (3a) plays an important role as an iron chelator as well as intra mitochondrial ROS scavenger. Thus, SEGA (3a) is a potent antioxidant antiapototic molecule, which efficiently prevents NSAID-induced gastropathy and stress or alcohol-mediated gastric damage. 2. The compounds of general formula 1 as claimed in claim 1 , wherein represented compounds comprising:3,4,5-trihydroxy-N-(2-(5-hydroxy-1H-indol-3-yl)ethyl)benzamide; SE GA (3a);N-(2-(1H-indol-3-yl) ethyl)-3,4,5-trihydroxybenzamide TRGA (3b);3,4,5-trihydroxy-N-(2-(5-methoxy-1H-indol-3-yl)ethyl)benzamide MEGA (3c);3-(2-aminoethyl)-1H-indol-5-yl 3,4,5-trihydroxybenzoate GASA (4d).4. The compounds as claimed in claim 1 , wherein said compounds are useful for the treatment of gastropathy.5. The compounds as claimed in claim 1 , wherein said compounds exhibiting antioxidant property in vitro.6. The compounds as claimed in claim 1 , wherein ferric reducing antioxidant power (FRAP) value at 6 min claim 1 , 65 min and absorbance ...

PHARMACEUTICAL COMPOSITION CONTAINING A TRYPTOPHAN DERIVATIVE

Pharmaceutical compositions containing a compound of formula (I) wherein the radicals denote e.g.: Ris hydrogen or C-C-alkyl; Ris hydrogen or C-C-alkyl; R3 is hydrogen or C-C-alkyl; Ris OH; Ris hydrogen, and a pharmaceutically acceptable cyclodextrin derivative can be used for the preparation of ophthalmic formulations. 2. A pharmaceutical composition according to claim 1 , wherein the composition contains at least one compound of formula (I) in which:{'sup': '1', 'sub': 1', '8', '3', '8', '6', '14, 'Ris hydrogen, C-C-alkyl, C-C-cycloalkyl or C-C-aryl,'}{'sup': '2', 'sub': 1', '8', '3', '8', '6', '14, 'Ris hydrogen, C-C-alkyl, C-C-cycloalkyl or C-C-aryl,'}{'sup': '3', 'sub': 1', '8, 'Ris hydrogen or C-C-alkyl,'}{'sup': '4', 'sub': 1', '8, 'Ris OH or O—C-C-alkyl,'}{'sup': '5', 'sub': 1', '8, 'Ris hydrogen or C-C-alkyl,'}or a pharmaceutically acceptable salt thereof,and comprises at least one further component (F).3. A pharmaceutical composition according to claim 2 , wherein the composition contains a compound of formula (I) wherein{'sup': '1', 'sub': 1', '3, 'Ris hydrogen or C-C-alkyl,'}{'sup': '2', 'sub': 1', '3, 'Ris hydrogen or C-C-alkyl,'}{'sup': '3', 'Ris hydrogen or methyl,'}{'sup': '4', 'Ris OH,'}{'sup': '5', 'sub': 1', '8, 'Ris hydrogen or C-C-alkyl,'}or a pharmaceutically acceptable salt thereof,and comprises the solvent water and optionally further components (F).4. A pharmaceutical composition according to claim 3 , wherein the composition contains a compound of formula (I) wherein Rand Rare hydrogen claim 3 , Ris methyl claim 3 , Ris OH and Ris hydrogen claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , and comprises the solvent water and optionally further components (F).6. A pharmaceutical composition according to claim 1 , wherein the cyclodextrin compound (C) is selected from the group consisting of:alpha-cyclodextrin, beta-cyclodextrin, randomly alkylated beta-cyclodextrin, 2-O-methyl-beta-cyclodextrin, heptakis-(2,6-di-0-methyl)-beta ...

Novel Heterocyclic Alkanol Derivatives

The present invention relates to novel heterocyclic alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. 110.-. (canceled) The present invention relates to novel heterocyclic alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.It is already known that particular heterocyclic alkanol derivatives can be used in crop protection as fungicides and/or growth regulators (cf. EP-A 0 395 175, EP-A 0 409 418).Since the ecological and economic demands made on modern active ingredients, for example fungicides, are increasing constantly, for example with respect to activity spectrum, toxicity, selectivity, application rate, formation of residues and favourable manufacture, and there can also be problems, for example, with resistances, there is a constant need to develop novel fungicidal compositions which have advantages over the known compositions at least in some areas.Novel heterocyclic alkanol derivatives of the formula (I)have now been found, in whichThe salts obtainable in this way likewise have fungicidal and/or plant growth-regulating properties.The heterocyclic alkanol derivatives usable in accordance with the invention are defined in general terms by the formula (I). Preferred radical definitions for the formulae specified above and below are given below. These definitions apply equally to the end products of the formula (I) and to all intermediates (see also below under “Illustrations of the processes and intermediates”).The radical definitions and explanations given above in general ...

Electronic Device Comprising an Organic Semiconducting Material

The present invention relates to an electronic device comprising at least one organic semiconducting material according to the following formula (I): wherein Rare independently selected from H, halogen, CN, substituted or unsubstituted C-C-alkyl or heteroalkyl, C-C-aryl or C-C-heteroaryl, C-C-alkoxy or C-C-aryloxy, Ar is selected from substituted or unsubstituted C-C-aryl or C-C-heteroaryl, and R5 is selected from substituted or unsubstituted C-C-aryl or C-C-heteroaryl, H, F or formula (II). 2. The electronic device according to claim 1 , wherein Ar and Rare independently selected from C-Caryl or C-C-heteroaryl.5. The electronic device according to claim 1 , wherein the device has a layered structure and at least one layer comprises at least one compound according to formula (I).6. The electronic device according to claim 1 , wherein the organic semiconducting material is doped by an n-dopant.7. The electronic device according to claim 6 , wherein the organic semiconducting material is doped by an organic n-dopant having a HOMO energy level which is more positive than −3.3 eV.8. The electronic device according to claim 1 , wherein the device is an electronic claim 1 , optoelectronic or electroluminescent device having an electronically functionally effect region claim 1 , wherein the electronically effective region comprises at least one compound according to formula (I).9. The electronic device according to claim 1 , wherein the device is an organic light-emitting diode claim 1 , a field-effect transistor claim 1 , a sensor claim 1 , a photodetector claim 1 , an organic thin-film transistor claim 1 , an organic integrated circuit claim 1 , an organic light-emitting transistor claim 1 , a light-emitting electrochemical cell claim 1 , or an organic laser diode. The present invention relates to an organic semiconducting layer, preferably an electronic device, comprising at least one organic semiconducting material.Conjugated organic compounds have different ...