Eisai R&D Management Co., Ltd. Patent applications |
Patent application number | Title | Published |
20160130237 | PYRIMIDINE FGFR4 INHIBITORS - Provided herein are compounds of Formula I useful as FGFR4 inhibitors, as well as methods of use of the same. | 05-12-2016 |
20140371319 | NOVEL INDANESULFAMlDE DERIVATIVES - Novel indansulfamide derivatives or a pharmaceutically acceptable salt thereof such as N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, N-[(1S)-2,2,4,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, (+)-N-(2,2,4,6,7-pentafluoro-2,3-dihydro-1H-inden-1-yl)sulfamide, have an action of improving Seizure Severity Index (Score) in mice kindling model. Thus the compounds or the salt thereof are expected as a drug for treating epilepsy. | 12-18-2014 |
20140323739 | COMPOUNDS FOR PREPARING IMMUNOLOGICAL ADJUVANT - The present invention provides methods for preparing TLR-4 receptor agonist E6020: | 10-30-2014 |
20140243316 | Tetrahydroimidazo(1,5-D)[1,4]Oxazepine Derivative - A compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof works as an mGluR2 antagonist, and is applicable as a therapeutic agent for neurological disorders related to glutamate dysfunction and diseases involving the mGluR2, such as Alzheimer's disease: | 08-28-2014 |
20140235707 | METHODS AND COMPOSITIONS FOR PREDICTING RESPONSE TO ERIBULIN - The invention provides methods for predicting the efficacy of eribulin, an analog thereof, or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate), in the treatment of a subject suffering from breast cancer by determining the level of particular biomarkers in a sample derived from the subject. | 08-21-2014 |
20140235614 | MONOCYCLIC PYRIDINE DERIVATIVE - The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: | 08-21-2014 |
20140221635 | INTERMEDIATES FOR THE PREPARATION OF ANALOGS OF HALICHONDRIN B - Intermediates and methods of their use in the synthesis of anslogs of halichondrin B are provided. | 08-07-2014 |
20140193836 | NOVEL MARKERS FOR DOPAMINERGIC NEURON PROGENITOR CELLS - The present invention provides a method for selecting dopaminergic neuron progenitor cells, which comprises detecting any one or more of markers selected from the group consisting of CD15 (SSEA-1), CD24, CD46, CD47, CD49b, CD57, CD58, CD59, CD81, CD90, CD98, CD147, CD184, Disalogangliosid GD2, SSEA-4, CD49f, SERINC4, CCR9, PHEX, TMPRSS11E, HTR1E, SLC25A2, Ctxn3, Cc17, Chrnb4, Chrna3, Kcnv2, Grm2, Syt2, Lim2, Mboat1, St3ga16, Slc39a12, Tacr1, Lrtm1, Dscam and CD201. | 07-10-2014 |
20140193421 | Anti-Human XCR1 Antibodies - An object of the present invention is to provide a monoclonal antibody binding to human XCR1, wherein the antibody binds to linear or discontinuous epitopes which comprise at least three amino acids selected from the group consisting of the 8th, 11th, 12th, 13th, 14th, 16th, 17th, 22nd, 23rd, 176th, and 177th amino acids in the amino acid sequence of SEQ ID NO: 91. | 07-10-2014 |
20140187577 | BIOMARKERS FOR PREDICTING AND ASSESSING RESPONSIVENESS OF THYROID AND KIDNEY CANCER SUBJECTS TO LENVATINIB COMPOUNDS - Biomarkers are provided that are predictive of a subject's responsiveness to a therapy comprising lenvatinib or a pharmaceutically acceptable salt thereof (e.g., lenvatinib mesylate). The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for a subject having cancer (e.g., thyroid cancer, kidney cancer), suspected of having cancer, or at risk of developing cancer. | 07-03-2014 |
20140179690 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; R is monofluoromethyl or difluoromethyl; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia. | 06-26-2014 |
20140163244 | HALICHONDRIN B ANALOGS - The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediate. | 06-12-2014 |
20140163242 | INTERMEDIATES FOR THE PREPARATION OF ANALOGS OF HALICHONDRIN B - Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided. | 06-12-2014 |
20140163095 | USE OF ERIBULIN IN THE TREATMENT OF BREAST CANCER - The invention provides methods of treating breast cancer in subjects having locally advanced or metastatic breast cancer. | 06-12-2014 |
20140155452 | PHARMACEUTICAL COMPOSITION - The present invention provides compounds of Formula I: | 06-05-2014 |
20140148483 | Method For Predicting Effectiveness Of Angiogenesis Inhibitor - The purpose of the present invention is to provide a method for predicting the effectiveness of an angiogenesis inhibitor in a subject suffering from a tumor. Provided is a method comprising a step of testing for the presence or absence of an a mutation or loss of expression of B-Raf and PTEN in a sample of tumor tissue from the subject. By using the presence or absence of or a mutation or loss of expression of B-Raf and PTEN as an indicator, this method enables the antitumor effectiveness of the angiogenesis inhibitor to be predicted without administering the angiogenesis inhibitor to the subject. | 05-29-2014 |
20140142315 | METHOD FOR PRODUCING 1,2-DIHYDROPYRIDINE-2-ONE COMPOUND - The present inventions provide a method for commercially producing a 1,2-dihydropyridine-2-one compound represented by the following formula (III-a) | 05-22-2014 |
20140142091 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - The present invention relates to a fused aminodihydrothiazine derivative of formula (I): | 05-22-2014 |
20140099366 | Composition Containing Two Anti-Dementia Drugs - An object of the present invention is to provide, for the case of implementing a therapeutic method in which at least two kinds of anti-dementia drugs are used together, a composition that has a good therapeutic effect on dementia, and also gives excellent compliance. Another object of the present invention is to provide a composition containing at least two kinds of anti-dementia drugs, in which release of the anti-dementia drugs from the composition is controlled, whereby a combined effect of the anti-dementia drugs can be achieved well. Still another object of the present invention is to provide a composition for which the frequency of administration and the amount taken are reduced and hence compliance can be improved, and a method of manufacturing such a composition. According to the present invention, there is provided a composition containing at least two kinds of anti-dementia drugs; such a composition containing at least one sustained-release portion containing an anti-dementia drug; and such a composition containing at least one cholinesterase inhibitor, and at least one N-methyl-D-aspartate receptor antagonist. | 04-10-2014 |
20140080146 | METHOD FOR DETECTING NEUROLOGICAL DISEASE ASSOCIATED WITH COGNITIVE IMPAIRMENT BY MEASURING EPHA4 EXTRACELLULAR DOMAIN - A method for detecting a neurological disease associated with cognitive impairment, wherein the extracellular domain of EphA4 is measured from a biological sample taken from a subject. | 03-20-2014 |
20140065100 | Compositions and Methods for Cancer Immunotherapy - The invention relates to immunotherapeutic compounds and to methods for stimulating an immune response in a subject individual at risk for developing cancer, diagnosed with a cancer, in treatment for cancer, or in post-therapy recovery from cancer or the compounds of the invention can be administered as a prophylactic to a subject individual to prevent or delay the development of cancer. | 03-06-2014 |
20140044777 | Liposome Composition - The present invention provides a novel liposome composition containing eribulin or its pharmacologically permissible salt, and its method of manufacture. | 02-13-2014 |
20140031384 | THERAPEUTIC AGENT FOR TUMOR - A therapeutic agent for tumor for combined use of a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and a compound represented by Formula (II): | 01-30-2014 |
20140024070 | METHOD FOR SCREENING FOR COMPOUND CAPABLE OF ENHANCING OR INHIBITING OATP1B1 TRANSPORT ACTIVITY, AND METHOD FOR DETERMINING EXPRESSION LEVEL OF OATP1B1 - The present invention provides a method of screening for a compound that enhances or inhibits the transport activity of OATP1B1, using dichlorofluorescein. The present invention also provides a use of dichlorofluorescein in measurement of the expression level of OATP1B1. The present invention further provides a method for measuring the expression level of OATP1B1 in test cells, using dichlorofluorescein. The present invention further provides a use of a kit including dichlorofluorescein and positive cells expressing OATP1B1 in measurement of the expression level of OATP1B1 in test cells. | 01-23-2014 |
20140012011 | COMPOUNDS FOR PREPARING IMMUNOLOGICAL ADJUVANT - The present invention provides methods for preparing TLR-4 receptor agonist E6020: | 01-09-2014 |
20140011999 | Method for Producing Phenoxypyridine Derivative - A method for producing a compound or a salt thereof represented by a formula (I), comprising reacting a compound or a salt thereof represented by a formula (II) and an aniline derivative represented by a formula (III) in water or a mixed solvent of water and an organic solvent in the presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide and substantially in the absence of a base is disclosed, | 01-09-2014 |
20130303489 | MULTIKINASE INHIBITORS FOR USE IN THE TREATMENT OF CANCER - The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): | 11-14-2013 |
20130288956 | COMBINED PHARMACEUTICAL COMPOSITION AS ANTIFUNGAL AGENT - An object of the present invention is to provide a pharmaceutical composition having superior antifungal activity. The present invention provides a pharmaceutical composition comprising 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-ylamine or 2-amino-1-((phosphonooxy)methyl)-3-(3-((4-((2-pyridinyloxy)methyl)phenyl)methyl)-5-isoxazolyl)-pyridinium or a salt thereof in combination with an antifungal agent. | 10-31-2013 |
20130288278 | SCREENING METHOD USING GELATINASE-MEDIATED EphA4 CLEAVAGE REACTION AS AN INDICATOR - The object of the present invention is to provide a method for screening a substance that affects gelatinase-mediated EphA4 processing. The present invention provides a method for screening a substance that affects gelatinase-mediated EphA4 processing, which comprises the steps of: (a) allowing a first biological composition containing gelatinase or a biologically active fragment thereof to be contacted with a second biological composition containing EphA4 in the presence and absence of a candidate substance; (b) measuring the presence or amount of the EphA4 ectodomain and/or endodomain fragment; and (c) selecting the candidate substance as a substance that affects gelatinase-mediated EphA4 processing if the results of the step (b) measured in the presence of the candidate substance are changed in comparison with the results of the step (b) measured in the absence of the candidate substance. | 10-31-2013 |
20130266589 | Biomarker for Alzheimer`s Disease or Mild Cognitive Impairment - Desmosterol alone, the combination of desmosterol and amyloid beta, the combination of desmosterol and gelsolin and the combination of desmosterol, amyloid beta and gelsolin can be used as in-blood biomarkers for Alzheimer's disease or mild cognitive impairment. A method for evaluating the effect of a candidate for a therapeutic agent to treat Alzheimer's disease or mild cognitive impairment, a method for aiding the diagnosis of Alzheimer's disease or mild cognitive impairment, and a method for diagnosing Alzheimer's disease or mild cognitive impairment are provided in which the biomarkers are used. | 10-10-2013 |
20130237711 | INTERMEDIATES FOR THE PREPARATION OF ANALOGS OF HALICHONDRIN B - Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided. | 09-12-2013 |
20130237578 | PHARMACEUTICAL COMPOSITION - The present invention provides compounds of Formula I: | 09-12-2013 |
20130237565 | Pharmaceutical compositions of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinoli- necarboxamide - A pharmaceutical composition comprising: an active ingredient consisting of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, salt thereof, or solvate of the foregoing; and (i) a compound, a 5% (w/w) aqueous solution or suspension of which has a pH of 8 or more, and/or (ii) silicic acid, salt thereof, or solvate of the foregoing is a highly stable pharmaceutical composition, wherein under humidified and heated storage conditions, the decomposition of said compound is sufficiently reduced, or the gelation on the surface of the pharmaceutical composition is sufficiently inhibited. | 09-12-2013 |
20130231466 | METHODS FOR DETECTING TH1 CELLS - The inventors discovered that the adhesion molecule CAR, known to be localized in intracellular adhesion sites, functioned as an adhesion molecule for activated lymphocytes. Further, the inventors identified CARL, a novel CAR ligand expressed in lymphocytes, and clarified that the ligand was expressed selectively in Th1 cells. In addition, they found that anti-CAR antibodies could inhibit the adhesion of activated lymphocytes to CAR molecules. Thus, the present invention provides methods for detecting Th1 cells using CAR or anti-CARL antibodies, and methods of screening for inhibitors suppressing the adhesion of Th1 cells using the binding between CAR and CARL as an index. Furthermore, the present invention relates to methods of screening for inhibitors of the binding between CAR and CARL, antibodies that inhibit the binding between CAR and CARL, and therapeutic compositions comprising these antibodies. These are expected to be useful in diagnosing diseases, such as inflammation, in which infiltration of Th1 cells is involved, and in providing pharmaceutical agents for alleviating such diseases. | 09-05-2013 |
20130230523 | METHODS FOR DETECTING TH1 CELLS - The inventors discovered that the adhesion molecule CAR, known to be localized in intracellular adhesion sites, functioned as an adhesion molecule for activated lymphocytes. Further, the inventors identified CARL, a novel CAR ligand expressed in lymphocytes, and clarified that the ligand was expressed selectively in Th1 cells. In addition, they found that anti-CAR antibodies could inhibit the adhesion of activated lymphocytes to CAR molecules. Thus, the present invention provides methods for detecting Th1 cells using CAR or anti-CARL antibodies, and methods of screening for inhibitors suppressing the adhesion of Th1 cells using the binding between CAR and CARL as an index. Furthermore, the present invention relates to methods of screening for inhibitors of the binding between CAR and CARL, antibodies that inhibit the binding between CAR and CARL, and therapeutic compositions comprising these antibodies. These are expected to be useful in diagnosing diseases, such as inflammation, in which infiltration of Th1 cells is involved, and in providing pharmaceutical agents for alleviating such diseases. | 09-05-2013 |
20130211103 | INTERMEDIATES AND METHODS FOR MAKING ZEARALENONE MACROLIDE ANALOGS - Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) | 08-15-2013 |
20130203741 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - A compound represented by the general formula: | 08-08-2013 |
20130203740 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - The present invention relates to a fused aminodihydrothiazine derivative of formula (I): | 08-08-2013 |
20130197244 | METHODS AND COMPOUNDS USEFUL IN THE SYNTHESIS OF FUSED AMINODIHYDROTHIAZINE DERIVATIVES - Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme. | 08-01-2013 |
20130197045 | SITAXENTAN DERIVATIVE - A compound represented by formula (1-1) or (1-2), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of sitaxentan and has an improved CYP inhibitory effect: | 08-01-2013 |
20130197033 | PAROXETINE DERIVATIVE - A compound represented by Formula (1), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of paroxetine and has an improved CYP inhibitory effect: | 08-01-2013 |
20130189360 | COMPRESSED COMPOSITION - An object of the present invention is to provide a compressed composition that is superior in terms of maintaining the function of a film or in terms of content uniformity even during tableting process. | 07-25-2013 |
20130183299 | ANTI-FOLATE RECEPTOR ALPHA ANTIBODIES AND USES THEREOF - Described herein are antibodies, and antigen-binding fragments thereof, that are specific for folate receptor alpha, related polynucleotides, expression vectors, and cells that express the described antibodies. Also provided are methods of using the described antibodies, and antigen-binding fragments thereof, and related kits. Provided herein are also methods for diagnosing cancers, such as breast cancer, thyroid cancer, colorectal cancer, endometrial cancer, fallopian tube cancer, ovarian cancer, or lung cancer, using the described antibodies, and antigen-binding fragments thereof. The methods involve determining the amount of folate receptor alpha in a sample derived from a subject and comparing this level with the level of folate receptor alpha in a control sample or reference sample. | 07-18-2013 |
20130143907 | PYRAZOLOQUINOLINE DERIVATIVES - A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. | 06-06-2013 |
20130123274 | Antitumor Agent Using Compounds Having Kinase Inhibitory Effect in Combination - An antitumor agent for combined use of a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and a compound or pharmaceutically acceptable salt thereof represented by Formula (II) exhibits an excellent antitumor effect compared to cases where these are individually used, and exhibits antitumor effects against various cancer types: | 05-16-2013 |
20130123234 | Aryl- or Heteroaryl-Substituted Benzene Compounds - The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 05-16-2013 |
20130095518 | METHOD FOR PRODUCING TUMOR CELLS FROM NORMAL MAMMARY EPITHELIAL CELLS - An object of the present invention is to provide a method for producing tumor cells from cells derived from normal cells without using hTERT.
| 04-18-2013 |
20130095068 | AGENT FOR TREATING HCV INFECTION - Provided is an imidazolylbenzene compound or salt thereof that controls HCV replication and in addition is particularly capable of strongly controlling HCV replication, and is very effective in the prevention and treatment of HCV infection when used in combination with another agent for treating HCV infection such as Interferon. | 04-18-2013 |
20130085152 | Method For Assay On The Effect Of Vascularization Inhibitor - The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EOF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity. | 04-04-2013 |
20130065925 | PYRROLIDIN-3-YLACETIC ACID DERIVATIVE - A compound represented by formula (1) or a pharmaceutically acceptable salt thereof has an inhibitory effect in the fractalkine-CX3CR1 pathway: | 03-14-2013 |
20130053563 | PRODRUG OF TRIAZOLONE COMPOUND - By oral administration of a compound represented by the following Formula (I): the blood level of Compound (IV): which has an excellent inhibitory action against blood coagulation factor VIIa and the anticoagulant action, reaches a level sufficient for expression of its pharmacological actions. Therefore, the compound of the present invention is useful as a therapeutic and/or prophylactic agent for diseases caused by thrombus formation. | 02-28-2013 |
20120309988 | INTERMEDIATES FOR THE PREPARATION OF ANALOGS OF HALICHONDRIN B - Intermediates and methods of their use in the synthesis of anslogs of halichondrin B are provided. | 12-06-2012 |
20120232049 | PYRIDINE OR PYRIMIDINE DERIVATIVE HAVING EXCELLENT CELL GROWTH INHIBITION EFFECT AND EXCELLENT ANTI-TUMOR EFFECT ON CELL STRAIN HAVING AMPLIFICATION OF HGFR GENE - A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. | 09-13-2012 |
20120213799 | COMPOSITIONS AND METHODS FOR TREATING INFLAMMATORY DISORDERS - The present invention features compositions and methods related to humanized antibodies and FKN-binding fragments thereof that bind fractalkine. | 08-23-2012 |
20120202828 | FUSED AMINODIHYDROPYRIMIDONE DERIVATIVES - A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C | 08-09-2012 |
20120202804 | FUSED AMINODIHYDRO-OXAZINE DERIVATIVES - A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C | 08-09-2012 |
20120190672 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - The present invention relates to a fused aminodihydrothiazine derivative of formula (I): | 07-26-2012 |
20120178083 | SPECIFIC MARKER Lmx1a ON DOPAMINERGIC NEURONS - The present invention identified Lmx1a genes, which are expressed in dopaminergic neurons at all differentiation stages, from proliferating dopaminergic neuron progenitor cells before cell cycle exit to cells after cell cycle exit. Lmx1a expression in cells can be used as an indicator when selecting cells suitable for transplantation therapy for neurodegenerative diseases such as Parkinson's disease, and is useful as a marker for screening agents involved in the induction of dopaminergic neuron differentiation. | 07-12-2012 |
20120165339 | CYCLOPROPANE DERIVATIVES - A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: | 06-28-2012 |
20120128757 | Method of Manufacture of Liposome Composition - The present invention provides a method of manufacture of a liposome composition including a step in which: a liposome dispersion liquid containing a liposome, and further containing cyclodextrin in the liposome internal phase is provided and a step in which an active compound is introduced into said liposome internal phase, and the liposome composition. | 05-24-2012 |
20120095242 | INTERMEDIATES AND METHODS FOR THE SYNTHESIS OF HALICHONDRIN B ANALOGS - Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described. | 04-19-2012 |
20120095031 | CYCLOPROPANE COMPOUND - A cyclopropane compound represented by the following formula (A) or a pharmaceutically acceptable salt thereof has orexin receptor antagonism, and therefore has a potencial of usefulness for the treatment of sleep disorder for which orexin receptor antagonism is effective, for example, insomnia: | 04-19-2012 |
20120094984 | FUSED AMINODIHYDROTHIAZINE DERIVATIVES - A compound represented by the general formula: | 04-19-2012 |
20120077842 | QUINOLINE DERIVATIVE-CONTAINING PHARMACEUTICAL COMPOSITION - A pharmaceutical composition comprising a compound represented by the formula (I) or pharmaceutically acceptable salt thereof or solvate thereof; and a basic substance is excellent in dissolution, is stable even after a long term storage, and is useful as a preventive or therapeutic agent against a tumor: | 03-29-2012 |
20120077837 | ANTI-TUMOR AGENT - A combination therapy for tumor is provided. Disclosed is a method of treating tumor, the method comprises administering to a patient, a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and everolimus represented by Formula (II): | 03-29-2012 |
20120058178 | Liposome Composition - The present invention provides a novel liposome composition containing eribulin or its pharmacologically permissible salt, and its method of manufacture. | 03-08-2012 |
20120029213 | INTERMEDIATES FOR THE PREPARATION OF ANALOGS OF HALICHONDRIN B - Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided. | 02-02-2012 |
20120028284 | TRAPPING COMPOUNDS AND METHOD FOR IDENTIFYING REACTIVE METABOLITES - A compound of formula (I) is useful to identify reactive metabolites. | 02-02-2012 |
20120021417 | DOPAMINERGIC NEURON PROLIFERATIVE PROGENITOR CELL MARKER Nato3 - The present invention is a probe, a primer, and an antibody, for detecting a dopaminergic neuron proliferative progenitor cell. According to the present invention, there is provided a polynucleotide probe and a polynucleotide primer for use in the detection or selection of a dopaminergic neuron proliferative progenitor cell, which can hybridize with a polynucleotide consisting of a nucleotide sequence of a Nato3 gene, or a complementary sequence thereto, and an antibody against a Nato3 protein, or a part thereof for use in the detection or selection of a dopaminergic neuron proliferative progenitor cell. | 01-26-2012 |
20120003311 | METHOD FOR CONTROLLED RELEASE OF AN ACID-UNSTABLE PHYSIOLOGICALLY ACTIVE SUBSTANCE - It is an object of the present invention, in the case of a controlled-release pharmaceutical composition, particularly a pulsed-release pharmaceutical composition, containing an acid-unstable physiologically active substance, to provide a pharmaceutical composition having little variation in dissolution lag time and high reliability of dissolution characteristics. The present invention discloses a controlled-release pharmaceutical composition comprising: 1) a core containing an acid-unstable physiologically active substance and a disintegrant; and 2) a release-controlling coating which covers the core, and which contains a water-insoluble polymer, an enteric polymer and a hydrophobic wax. | 01-05-2012 |
20110294986 | Methods For Detecting Th1 Cells - The inventors discovered that the adhesion molecule CAR, known to be localized in intracellular adhesion sites, functioned as an adhesion molecule for activated lymphocytes. Further, the inventors identified CARL, a novel CAR ligand expressed in lymphocytes, and clarified that the ligand was expressed selectively in Th1 cells. In addition, they found that anti-CAR antibodies could inhibit the adhesion of activated lymphocytes to CAR molecules. Thus, the present invention provides methods for detecting Th1 cells using CAR or anti-CARL antibodies, and methods of screening for inhibitors suppressing the adhesion of Th1 cells using the binding between CAR and CARL as an index. Furthermore, the present invention relates to methods of screening for inhibitors of the binding between CAR and CARL, antibodies that inhibit the binding between CAR and CARL, and therapeutic compositions comprising these antibodies. These are expected to be useful in diagnosing diseases, such as inflammation, in which infiltration of Th1 cells is involved, and in providing pharmaceutical agents for alleviating such diseases. | 12-01-2011 |
20110293615 | Use of Combination of Anti-Angiogenic Substance and c-kit Kinase Inhibitor - The object of the present invention is to find a pharmaceutical composition and a method for treating cancer that show an excellent antitumor effect. Combinational use of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide and analogues thereof can result in an excellent antitumor effect when combined with a substance having a c-kit kinase-inhibiting activity. | 12-01-2011 |
20110263845 | METHOD FOR MANUFACTURING HETEROCYCLE SUBSTITUTED PYRIDINE DERIVATIVES - It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I): | 10-27-2011 |
20110256548 | METHOD FOR OBTAINING PANCREATIC PROGENITOR CELL USING NEPH3 - The present invention provides markers that can selectively distinguish pancreatic progenitor cells. The present invention also provides methods for distinguishing pancreatic progenitor cells by using the markers as an indicator, and reagents to be used in the methods. | 10-20-2011 |
20110250171 | Compositions and Methods for Cancer Immunotherapy - The invention relates to immunotherapeutic compounds and to methods for stimulating an immune response in a subject individual at risk for developing cancer, diagnosed with a cancer, in treatment for cancer, or in post-therapy recovery from cancer or the compounds of the invention can be administered as a prophylactic to a subject individual to prevent or delay the development of cancer. | 10-13-2011 |
20110243935 | Compositions and Methods for Immunotherapy - The invention relates to immunotherapeutic compounds, compositions that include such compounds, and methods of using the compounds, for example, to treat an individual having, at risk for, or previously treated for a cancer. | 10-06-2011 |
20110237805 | INTERMEDIATES AND METHODS FOR MAKING ZEARALENONE MACROLIDE ANALOGS - Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) wherein R | 09-29-2011 |
20110229889 | DOPAMINERGIC NEURON PROLIFERATIVE PROGENITOR CELL MARKER Msx1/2 - The present invention is a probe, a primer, and an antibody, for detecting a dopaminergic neuron proliferative progenitor cell. According to the present invention, there is provided a polynucleotide probe and a polynucleotide primer for use in the detection or selection of a dopaminergic neuron proliferative progenitor cell, which can hybridize with a polynucleotide consisting of a nucleotide sequence of an Msx1 gene or an Msx2 gene, or a complementary sequence thereto, and an antibody against an Msx1 protein or an Msx2 protein, or a part thereof for use in the detection or selection of a dopaminergic neuron proliferative progenitor cell. | 09-22-2011 |
20110207756 | ANTITUMOR AGENT FOR THYROID CANCER - The objective of the present invention is to provide a pharmaceutical composition and a therapeutic method that are specifically effective against at least one disease selected from multiple endocrine neoplasia, type IIA, multiple endocrine neoplasia, type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract. | 08-25-2011 |
20110207723 | NOVEL FUSED AMINODIHYDROTHIAZINE DERIVATIVE - A compound represented by the general formula (I): | 08-25-2011 |
20110201816 | METHODS OF SCREENING FOR COMPOUNDS THAT INHIBIT THE BIOSYNTHESIS OF GPI IN MALARIA PARASITES - The present inventors succeeded in isolating GWT1 (PfGWT1), which is one of the enzymes involved in GPI biosynthesis in the malaria parasite | 08-18-2011 |
20110201003 | METHOD FOR OBTAINING PURKINJE PROGENITOR CELL BY USING NEPH3(65B13) AND E-CADHERIN - 65B13 was discovered to be a useful marker for isolating GABA neuron progenitor cells including Purkinje cells. Furthermore, E-cadherin was revealed to be a useful marker for isolating Purkinje progenitor cells from a 65B13-positive cell population. Specifically, when used in combination with 65B13, E-cadherin was found to be a useful marker for isolating Purkinje progenitor cells. | 08-18-2011 |
20110195951 | DIAZAINDOLE DERIVATIVES AND THEIR USE IN THE INHIBITION OF C-JUN N-TERMINAL KINASE - The invention relates to diazaindole derivatives represented by the general formula (I): where A, E, G, R | 08-11-2011 |
20110184190 | COMPOUNDS USEFUL IN THE SYNTHESIS OF HALICHONDRIN B ANALOGS - In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III): | 07-28-2011 |
20110183967 | BENZOXAZOLE COMPOUNDS AND METHODS OF USE - The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides methods of use as described herein. | 07-28-2011 |
20110183318 | METHOD FOR SCREENING OF SUBSTANCE EFFECTIVE ON DISEASE USING GPR120 AND PHOSPHOLIPASE - The present invention provides a screening method for determining whether a substance of interest is a substance which alters GPR120 mediated cell stimulating activities, comprising using a substance of interest, a biomembrane containing GPR120, or cells containing said biomembrane, and phospholipase or salts thereof. According to a screening method of the present invention, the method can screen substances such as CCK and GLP-1 which are involved in the secretion of hormones in gastrointestinal tracts. | 07-28-2011 |
20110172427 | PROCESS FOR PREPARING CERTAIN CINNAMIDE COMPOUNDS - This invention relates to a new synthesis, intermediates and precursors leading to a mixture of the compounds 11 and 12 as shown below. It also relates to the resolution of the stereoisomeric mixture to provide in substantial stereochemical purity compound 12. The synthesis of the invention involves preparation of compound 7 and compound 10 as shown below and their reaction to prepare a mixture of compound 11 and compound 12. | 07-14-2011 |
20110152521 | Method for Producing Quinazoline Derivative - [4-(3-aminophenyl)-6,7-dimethoxyquinazolin-2-yl]methylamine with a favorable yield and high purity can be produced by subjecting a compound represented by the following formula (I) to a step of reacting with methylamine and a step of deprotection if desired: | 06-23-2011 |
20110152508 | REAGENTS AND METHODS FOR PREPARING LPS ANTAGONIST B1287 AND STEREOISOMERS THEREOF - The present invention provides methods for preparing LPS antagonist lipodisaccharide B1287 and stereoisomers thereof, which compounds are useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock. Also provided are synthetic intermediates useful for implementing the inventive methods. | 06-23-2011 |
20110152253 | SPIROAMINODIHYDROTHIAZINE DERIVATIVES - A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia. | 06-23-2011 |
20110137013 | NOVEL COLLAGEN-LIKE PROTEIN CLAC, PRECURSOR THEREOF AND GENES ENCODING THE SAME - A novel human collagen-like protein CLAC occurring in brain amyloid and its precursor CLAC-P; genes encoding the same; cDNA of mouse CLAC-P and its deduced amino acid sequence; antibodies specific to these proteins; and methods of diagnosing treating and preventing Alzheimer's disease by using the same. | 06-09-2011 |
20110130353 | HIGHLY PURIFIED ANTIENDOTOXIN COMPOUND - The invention provides compositions containing a highly purified antiendotoxin compound and methods of preparing and using such compositions. | 06-02-2011 |
20110111444 | Method of Screening for Compounds which Affect the Processing of EphA4 by Gamma-Secretase - The present invention provides a method of screening for compounds which affect the processing of EphA4 by γ-secretase, comprising the following steps: (i) contacting a first biological composition containing γ-secretase or a biologically active fragment thereof with a second biological composition containing EphA4 in the presence and absence of a candidate compound; (ii) measuring the cleavage of the EphA4 in the presence and absence of the candidate compound; (iii) selecting those candidate compounds which affect the cleavage of the EphA4 by γ-secretase; and (iv) identifying the candidate compounds selected in step (iii) as compounds which affect the processing of EphA4 by γ-secretase. | 05-12-2011 |
20110104171 | EphA4 Polypeptide Having a Novel Activity and Use Thereof - The present invention provides a polynucleotide which consists of a partial sequence of a polynucleotide encoding the amino acid sequence as shown in SEQ ID NO:2, wherein the former polynucleotide encodes a polypeptide consisting of a partial amino acid sequence of SEQ ID NO:2 whose N-terminus starts between positions 564 and 621 of SEQ ID NO:2. | 05-05-2011 |
20110086898 | PYRAZOLOOXAZOLE COMPOUND - A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism. | 04-14-2011 |
20110086882 | PYRAZOLOTHIAZOLE COMPOUND - A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism | 04-14-2011 |
20110054194 | Halichondrin B Analogs - The invention includes halichondrin B analogs having pharmaceutical activity; in some cases, crystalline forms thereof, and in some cases, halichondrin B analogs having a further utility as synthetic intermediates. | 03-03-2011 |
20110053981 | Methods and Compositions Using Cholinesterase Inhibitors - The invention provides methods for treating and/or preventing Alzheimer's disease, psychiatric illnesses, encephalitis, meningitis, fetal alcohol syndrome, Karsakoff's syndrome, anoxic brain injury, cardiopulmonary resuscitation injuries, diabetes, Sjogren's syndrome, mental retardation, developmental delay, menopause, strokes, macular degeneration, neuronal loss associated with macular degeneration, sleep disorders, severe Alzheimer's disease, jet lag, post-traumatic stress disorder, anxiety disorders, panic attacks, obsessive-compulsive disorder, amnesia, and other disorders by administering to a patient in need thereof at least one cholinesterase inhibitor. The invention also provides novel pharmaceutical compositions that can be administered to the eyes or to the nose of patients. In one embodiment, the cholinesterase inhibitor is donepezil, a stereoisomer thereof and/or a pharmaceutically acceptable salt thereof. In other embodiments, the cholinesterase inhibitor can be one or more of phenserine, tolserine, phenethylnorcymserine, ganstigmine, epastigmine, tacrine, physostigmine, pyridostigmine, neostigmine, rivastigmine, galantamine, citicoline, velnacrine, huperzine, metrifonate, heptastigmine, edrophonium, TAK-147, T-82, and upreazine. | 03-03-2011 |
20110046398 | INTERMEDIATES IN THE SYNTHESIS ZEARALENONE MACROLIDE ANALOGS - Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV), wherein R | 02-24-2011 |
20110045074 | MATRIX TYPE SUSTAINED-RELEASE PREPARATION CONTAINING BASIC DRUG OR SALT THEREOF AND, METHOD FOR MANUFACTURING THE SAME - A matrix type sustained-release preparation and a manufacturing method therefor are provided wherein dissolution with low pH dependence of a basic drug or a salt thereof at the early stage of dissolution can be ensured in a dissolution test, and wherein as the dissolution test proceeds, a ratio of a dissolution rate of the basic drug or the salt thereof in an acidic test solution to a dissolution rate of the basic drug or the salt thereof in a neutral test solution (dissolution rate in the acidic test solution/dissolution rate in the neutral test solution) decreases with dissolution time at the late stage of dissolution, as compared to the early stage of dissolution. According to the present invention, the matrix type sustained-release preparation contains a basic drug or a salt thereof and at least one enteric polymer, in which solubility of the basic drug or the salt thereof in a 0.1 N hydrochloric acid solution and a neutral aqueous solution, pH 6.0 is higher than in a basic aqueous solution, pH 8.0. | 02-24-2011 |
20110021545 | NOVEL PREPARATION FOR EXTERNAL USE - A compound represented by the formula (I), salt thereof, or hydrate thereof has an excellent anti-pruritic effect and an excellent effect in terms of metabolism. The topical formulation of the present invention has excellent skin absorption properties of the compound represented by the formula (I), salt thereof, or hydrate thereof. Furthermore, the topical formulation of the present invention is excellent in stability because ingredients are hardly bled after long-term storage. | 01-27-2011 |
20110009619 | POLYCYCLIC COMPOUND - Disclosed is a compound represented by the formula (I): | 01-13-2011 |
20110008769 | DOPAMINERGIC NEURON PROGENITOR CELL MARKER 187A5 - An object of the present invention is to provide a probe, a primer, a primer set and an antibody for use in the detection or selection of a dopaminergic neuron progenitor cell. The present invention provides a probe, a primer and a primer set for use in the detection or selection of a mesencephalon dopaminergic neuron progenitor cell, and preferably a dopaminergic neuron proliferative progenitor cell, which can hybridize with a nucleotide sequence of a 187A5 gene, or a complementary sequence thereto, and an antibody for use in the detection or selection of a mesencephalon dopaminergic neuron progenitor cell, and preferably a dopaminergic neuron progenitor cell, which is capable of binding to a 187A5 protein. | 01-13-2011 |
20100333216 | Non-human gene-disrupted animal with disrupted Adam11 gene - It is an object of the present invention to provide a non-human gene-disrupted animal with a disrupted ADAM11 gene. According to the present invention, a non-human gene-disrupted animal, wherein either one of or both alleles of an ADAM11 gene are disrupted, is provided. | 12-30-2010 |
20100324087 | COMBINED USE OF ANGIOGENESIS INHIBITOR AND TAXANE - The problems of the present invention are to find a pharmaceutical composition and a method for treating cancer that exhibit excellent anti-tumor effect. Excellent anti-tumor effect is achieved when 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, an analogous compound thereof, a pharmacologically acceptable salt thereof or a solvate thereof is used in combination with taxane. | 12-23-2010 |
20100323366 | Methods of Selecting a Dopaminergic Neuron Proliferative Progenitor Cells Using LRP4/CORIN Markers - In neuron transplantation therapy, in terms of safety, it is preferable to use a cell population consisting only of a desired type of cells, and to use postmitotic neurons in consideration to avoid the risk of tumorigenesis. Moreover, greater therapeutic effects would be expected through the use of earlier progenitor cells in consideration of post-transplantation viability, proper network formation ability, and such. | 12-23-2010 |
20100297181 | AMPA Receptor Antagonists for Epilepsy, Mental Disorders or Deficits in Sensory Organ - The invention provides methods for treating epilepsy, mental disorders and/or deficits in sensory organ by administering to patients therapeutically effective amounts of AMPA receptor antagonists in combination with one or more other active ingredients useful for treating epilepsy, mental disorders and/or deficits in sensory organ. The invention also provides pharmaceutical combinations, kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists, and optionally, one or more other active ingredients that are useful for treating epilepsy, mental disorders and/or deficits in sensory organ. | 11-25-2010 |
20100286087 | PHARMACEUTICAL COMPOSITION, USE OF 2-IMINOPYRROLIDINE DERIVATIVE FOR PRODUCTION OF PHARMACEUTICAL COMPOSITION, AND KIT FOR TREATMENT OR AMELIORATION OF HEART DISEASES - One embodiment of the present invention is a pharmaceutical composition comprising at least one specific 2-iminopyrrolidine derivative and at least one other compound (B). Another embodiment of the present invention is a pharmaceutical composition comprising at least one specific 2-iminopyrrolidine derivative, which is to be used in combination with at least one other compound (B). According to the present invention, there are provided pharmaceutical compositions capable of treating or ameliorating diseases, such as heart diseases, effectively. | 11-11-2010 |
20100279978 | METHODS OF REDUCING THE SEVERITY OF MUCOSITIS - The invention provides methods of reducing the severity of mucositis, involving administration of a toll-like receptor 4 antagonist. | 11-04-2010 |
20100255522 | Screening Method Utilizing Novel Substrate EphA7 for Gamma-Secretase - The present invention provides a method of screening for compounds which affect the processing of EphA7 by γ-secretase, comprising the following steps:
| 10-07-2010 |
20100240074 | Set of Yeast Cells, Method of Identifying Target Candidate Molecule, Method of Analyzing Action Mechanism and Screening Method - Provided is a set of yeast gene knockout strains whose drug sensitivity is significantly improved. A set of yeast cells of the invention is a set of yeast cells comprising two or more types of yeast cells, wherein at least one mutually different gene has been deleted or mutated in each of the two or more types of yeast cells, and all of the two or more types of yeast cells are drug hypersensitive yeast cells in which the expression of at least one drug sensitivity-related gene is regulated. | 09-23-2010 |
20100227835 | SUBSTITUTED LIPOSACCHARIDES USEFUL IN THE TREATMENT AND PREVENTION OF ENDOTOXEMIA - Novel substituted liposaccharides useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock and methods of using these agents are provided. Also provided are methods of preparing these agents and intermediates useful therein. | 09-09-2010 |
20100227350 | Method of Screening Substance Useful in Treating Disease With the Use of GPR40 and Phospholipase - The present invention relates to a screening method for determining whether a substance of interest is a substance which alters GPR40-mediated cell stimulating activities, comprising using a substance of interest, a biomembrane containing GPR40, or cells containing said biomembrane, and phospholipase or salts thereof. According to the present invention, substances involved in insulin secretion can be screened. In addition, according to the present invention, substance useful for the prevention or treatment of diabetes, diabetic complications and degenerative diseases, hyperglycemia, polyuria, ketonemia, acidosis, insulin resistance, impaired glucose tolerance, neurodegenerative diseases, insulinoma, cancers, hyperinsulinemia, hyperglyceridemia, fatty liver, hypoglycemia due to insulin hypersecretion, arteriosclerosis, hyperlipidemia, cerebral stroke, obesity, various diseases induced by diabetes or obesity, and the like. | 09-09-2010 |
20100216164 | MAMMALIAN PRICKLE GENE - The present invention provides the mPrickle gene which encodes a protein present in mammalian PSD fractions. The mPrickle protein is localized in synapses, and binds to the scaffold protein PSD-95. Precipitation of endogenous mPrickle using an anti-mPrickle antibody results in the coprecipitation of NMDA receptors, and thus, mPrickle can be used in drug delivery systems that target NMDA receptors. NMDA receptors are closely related to learning and memory, and are also suggested to be involved in mental disorders. Thus, in the future, mPrickle is expected to be applicable to the diagnosis and/or treatment of neurodegenerative diseases associated with learning/memory, such as mental deterioration and dementia. | 08-26-2010 |
20100203570 | GENE SPECIFICALLY EXPRESSED IN POSTMITOTIC DOPAMINERGIC NEURON PRECURSOR CELLS - A novel gene 65B13 expressed specifically and transiently in dopaminergic neuron precursor cells immediately after cell cycle exit was obtained by the present invention. The cellular expression of 65B13 can be used as an index to select cells that are suitable in terms of their safety, survival rate, and network formation ability, for transplant therapy of neurodegenerative diseases such as Parkinson's disease. | 08-12-2010 |
20100203505 | DOPAMINERGIC NEURON PROLIFERATIVE PROGENITOR CELL MARKER Msx1/2 - The present invention is a probe, a primer, and an antibody, for detecting a dopaminergic neuron proliferative progenitor cell. According to the present invention, there is provided a polynucleotide probe and a polynucleotide primer for use in the detection or selection of a dopaminergic neuron proliferative progenitor cell, which can hybridize with a polynucleotide consisting of a nucleotide sequence of an Msx1 gene or an Msx2 gene, or a complementary sequence thereto, and an antibody against an Msx1 protein or an Msx2 protein, or a part thereof for use in the detection or selection of a dopaminergic neuron proliferative progenitor cell. | 08-12-2010 |
20100197911 | Nitrogen-Containing Aromatic Derivatives - Compounds represented by the following general formula: | 08-05-2010 |
20100190843 | Tubulin Isotype Screening in Cancer Therapy Using Halichondrin B Analogs - Chemotherapeutic agents that interfere with microtubule assembly or disassembly in the cell are potent inhibitors of cell replication. Examples of such agents include halichondrin B analogs. It has been shown that the susceptibility of certain cancers to analogs of halichondrin B correlates with the expression of particular tubulin isotypes or other microtubule-associated proteins such as MAP-4 and stathmin. Correlations such as these may be used in identifying patients suitable for treatment using a particular chemotherapeutic agent. Such a system avoids treating patients with cytotoxic compounds where there is a minimal or no effect on the cancer. The invention also provides a system of establishing these correlations for different compounds and cancer types. The system will be particularly useful in establishing correlations between anti-microtubule agents and cancers such as lung, breast, and ovarian cancer. Kits and reagents useful in practicing the invention are also provided. | 07-29-2010 |
20100179193 | AMPA Receptor Antagonists and Zonisamide for Neuropathic Pain - The invention provides methods for treating and/or preventing neuropathic pain by administering to patients therapeutically effective amounts of AMPA receptor antagonists and zonisamide. The neuropathic pain may be diabetic neuropathy. The invention also provides kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists and zonisamide. The AMPA receptor antagonist may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-di-hydropyridin-2-one. | 07-15-2010 |
20100168174 | Combination of AMPA Receptor Antagonists and Acetylcholinesterase Inhibitors for the Treatment of Neuropathic Pain - The invention provides methods for treating and/or preventing neuropathic pain by administering to patients in need thereof therapeutically effective amounts of AMPA receptor antagonists; and cholinesterase inhibitors and/or anti-neuropathic pain agents. The neuropathic pain may be painful diabetic neuropathy. The invention also provides kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists; and cholinesterase inhibitors and/or anti-neuropathic pain agents. The AMPA receptor antagonists may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. The cholinesterase inhibitor may be, for example, 1-benzyl-4-((5,6-dimethoxy-1-indanon)-2-yl)methylpiperidine (donepezil). | 07-01-2010 |
20100152429 | SODIUM SALT OF DISACCHARIDE COMPOUND, METHOD FOR PRODUCING THE SAME, AND USE OF THE SAME - Disclosed are a sodium salt represented by the average formula (I) below, and a method for producing such a sodium salt. (In the formula, m | 06-17-2010 |
20100152164 | Method For Stabilizing Anti-Dementia Drug - The present invention provides a method for stabilizing an anti-dementia drug in a pharmaceutical composition containing the anti-dementia drug and a high molecular weight basic substance by adding a high molecular weight acidic substance to said pharmaceutical composition. Further, the present invention provides a pharmaceutical composition containing an anti-dementia drug and a high molecular basic substance in which a high molecular weight acidic substance is contained for stabilizing the anti-dementia drug. Furthermore, the present invention provides a method for manufacturing a pharmaceutical composition which comprises steps wherein a solution or suspension containing a high molecular weight acidic substance is added to a mixture of an anti-dementia drug and a high molecular weight basic substance for the sake of stabilizing the anti-dementia drug. | 06-17-2010 |
20100130537 | CINNAMIDE COMPOUNDS FOR DEMENTIA - The invention provides methods for treating, preventing, and delaying the onset of dementia and mild cognitive impairments by administering to a patient in need thereof at least one cinnamide compound and one or more second-line active ingredients, such as cholinesterase inhibitors; AMPA receptor antagonists; NMDA receptor antagonists; and the like. The invention also provides pharmaceutical compositions, combinations, and kits. | 05-27-2010 |
20100099714 | AMPA and NMDA Receptor Antagonists for Neurodegenerative Diseases - The invention provides methods for treating, preventing, and delaying the onset of neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, Pick's disease, and the like), dementia, mild cognitive impairments, glaucoma, ocular hypertension, and pain (e.g., neuropathic pain, headaches, and the like) by administering therapeutically effective amounts of AMPA receptor antagonists and NMDA receptor antagonists to patents in need thereof. The invention also provides combinations, kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists and NMDA receptor antagonists. Exemplary AMPA receptor antagonists include 1,2-dihydropyridine compounds, such as 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. Exemplary NMDA receptor antagonists include adamantane compounds, such as memantine. | 04-22-2010 |
20100094020 | POLYCATIONIZED PHOSPHOLIPID DERIVATIVES - The present invention provides novel phospholipid derivatives. Furthermore, the present invention provides lipid membrane structures excellent in gene/nucleic acid introduction efficiency into a cell. | 04-15-2010 |
20100094001 | COMPOSITION CONTAINING STABILITY-IMPROVED CHLOROMETHYL PHOSPHATE DERIVATIVE AND PROCESS FOR PRODUCING SAME - The present invention provides a process or the like which is employed for producing chloromethyl phosphate derivatives that are useful for producing water-soluble prodrugs, and which are excellent from the points of view of workability, operativity and energy saving. According to the present invention, there is provided a process for producing a composition containing a compound represented by the following formula (I) and a tertiary amine, | 04-15-2010 |
20100093999 | NOVEL FUSED AMINODIHYDROTHIAZINE DERIVATIVE - A compound represented by the general formula: | 04-15-2010 |
20100092490 | METHOD FOR ASSAY ON THE EFFECT OF VASCULARIZATION INHIBITOR - The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity. | 04-15-2010 |
20100086931 | METHOD FOR ASSAYING ACTION OF ANTITUMOR AGENT USING DECREASE IN GENE EXPRESSION LEVEL AS INDEX - An object of the present invention is to provide a method, a probe, a primer, an antibody, a reagent, and a kit for assaying an action of a pladienolide derivative to a living subject. According to the present invention, there is provided a method for assaying an action of the pladienolide derivative using a decrease in gene expression level as an index. | 04-08-2010 |
20100069358 | USE OF 7-AZAINDOLES IN THE INHIBITION OF C-JUN N-TERMINAL KINASE - The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them. | 03-18-2010 |
20100069354 | 7-AZAINDOLE DERIVATIVES AND THEIR USE IN THE INHIBITION OF C-JUN N-TERMINAL KINASE - The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and the use in medicine and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them. | 03-18-2010 |
20100028866 | DOPAMINERGIC NEURON PROLIFERATIVE PROGENITOR CELL MARKER Nato3 - The present invention is a probe, a primer, and an antibody, for detecting a dopaminergic neuron proliferative progenitor cell. According to the present invention, there is provided a polynucleotide probe and a polynucleotide primer for use in the detection or selection of a dopaminergic neuron proliferative progenitor cell, which can hybridize with a polynucleotide consisting of a nucleotide sequence of a Nato3 gene, or a complementary sequence thereto, and an antibody against a Nato3 protein, or a part thereof for use in the detection or selection of a dopaminergic neuron proliferative progenitor cell. | 02-04-2010 |
20100021918 | METHOD FOR ASSAYING ACTION OF ANTITUMOR AGENT USING SPLICING DEFECTS AS INDEX - An object of the present invention is to provide a method, a probe, a primer, an antibody, a reagent, and a kit for assaying an action of a pladienolide derivative to a living subject. According to the present invention, there is provided a method for assaying an action of the pladienolide derivative using splicing defect as an index. | 01-28-2010 |
20100016603 | PRODUCTION PROCESS OF 2,3'-BIPYRIDYL-6'-ONE - A production process where 2,3′-bipyridyl-6′-one can be produced in high purity at low cost on an industrial scale without using an expensive catalyst or special equipment is provided. A process for producing 2,3′-bipyridyl-6′-one comprises reacting an acetylpyridine derivative with at least one of compounds represented by formulae (II) to (V) to synthesize a bipyridine derivative and hydrolyzing the bipyridine derivative by one-pot preparation. In formulae (II) to (V), each of R2 to R8, X and Y represents a given group. | 01-21-2010 |
20100010043 | PERCUTANEOUSLY ABSORBABLE PREPARATION - The present invention provides a percutaneously absorbable preparation comprising 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one and/or a hydrochloride thereof wherein the percuneously absorbable preoaration is able to administer to a patient such that Cmax per unit surface area of the percutaneously absorbable preparation is 0.025 to 0.5 ng/ml·cm | 01-14-2010 |
20100005534 | SASPASE KNOCKOUT ANIMAL - Knockout animals in which a gene encoding a SASPase has been deleted (hereinafter, referred to as SASPase KO animals) are provided. The SASPase KO animals deficient in expression of functional SASPase were produced by deleting a gene encoding a stratified epithelium-specific protease, SASPase, through targeted disruption. The SASPase KO animals showed a significant increase in wrinkles on the sides of the body and so on. The SASPase KO animals find utility as animal models of wrinkles. | 01-07-2010 |
20100000111 | METHOD OF MEASURING MOISTURE CONTENT OF AN OBJECT FOR DRYING - The present invention provides a method of measuring moisture content of an object for drying during drying in a drying chamber by, for example, freeze-drying, fluidized bed drying or shelf drying, in real-time and in a non-destructive manner. According to the present invention, when measuring moisture content of an object for drying, a near infrared absorption spectrum of moisture present around the object for drying is measured, and the moisture content of the object for drying is calculated from a predetermined relationship based on a measured amount obtained from the measured near infrared absorption spectrum. | 01-07-2010 |
20090325228 | FUNGAL CELL WALL SYNTHESIS GENE - A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved. | 12-31-2009 |
20090318690 | Benzisoxazole Compound - Disclosed is a compound represented by the general formula (I) or a salt thereof: | 12-24-2009 |
20090317800 | REPORTER VECTOR FOR USE IN EVALUATION OF CYP1A2 INDUCTION - A reporter vector which can evaluate the ability of a drug to induce CYP1A2 or both of CYP1A1 and CYP1A2 and a method for evaluation of the ability of a drug to induce CYP1A2 or both of CYP1A1 and CYP1A2 by using the reporter vector. A reporter system which can evaluate the ability of a drug capable of inducing CYP1A2 or both of CYP1A1 and CYP1A2 is completed by constructing a reporter vector having a reporter gene linked to the 3′ end of a region between CYP1A1 and CYP1A2 or a reporter vector having different reporter genes linked to the both ends of the region, respectively, so as to sandwich the region, and a reporter vector having a deletion mutation in the region, and confirming that the expression of a reporter molecule is increased by the drug capable of inducing CYP1A2 or both of CYP1A1 and CYP1A2 in the reporter system using the reporter vector. | 12-24-2009 |
20090270433 | 2,3-DIHYDRO-IMINOISOINDOLE DERIVATIVES - A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. | 10-29-2009 |
20090270369 | BICYCLOAMINE DERIVATIVES - Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. | 10-29-2009 |
20090215795 | CYCLIC AMIDINE DERIVATIVES - A cyclic amidine derivative represented by the formula: | 08-27-2009 |
20090203771 | NOVEL INTERMEDIATE FOR HALICHONDRIN B ANALOG SYNTHESIS AND NOVEL DESULFONYLATION REACTION USED FOR THE INTERMEDIATE - The present invention provides a novel method for producing a compound represented by formula (III) shown below, which comprises treating a compound represented by formula (I) shown below with a trivalent chromium compound and at least one kind of metal selected from the group consisting of manganese and zinc in a solvent in the presence of a ligand represented by formula (II) shown below, and the present invention further provides the novel compound represented by formula (I). | 08-13-2009 |
20090203738 | Pharmaceutical Composition for Treating Bulimia and Depression Arising from Bulimia - Provided is a pharmaceutical composition for the treatment of bulimia in which a cholinesterase inhibitor is combined with at least one member selected from the group consisting of sibutramine, a pharmacologically acceptable salt thereof, an active metabolite thereof, a prodrug thereof and a solvate thereof. The pharmaceutical composition is useful in treating bulimia and depression arising from bulimia. | 08-13-2009 |
20090186855 | COMPOUNDS AND METHODS FOR TREATING TOLL-LIKE RECEPTOR 2-RELATED DISEASES AND CONDITIONS - The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation. | 07-23-2009 |
20090176797 | PHARMACEUTICAL COMPOSITION FOR TREATING ESOPHAGEAL CANCER - A compound represented by the following formula, a salt thereof or a hydrate of the foregoing is useful as a pharmaceutical composition for treating esophageal cancer treating esophageal cancer. | 07-09-2009 |
20090170925 | Methods for prognosing the ability of a zearalenone analog compound to treat cancer - The instant invention provides methods of prognosing the ability of a zearalenone analog compound to treat a cancer in a subject, methods of prognosing the ability of a zearalenone analog compound to inhibit the growth of a cancer in a subject, and methods of prognosing the ability of a zearalenone analog compound to promote the activation of apoptosis of a cancer in a subject. Methods of treating a cancer in a subject are also provided. The invention also pertains to methods of determining whether a cancer in a subject is sensitive to treatment with a zearalenone analog compound. | 07-02-2009 |
20090156686 | Composition containing higher fatty acid derivative and foods and drinks - An object of the invention is to provide a composition containing a higher fatty acid derivative, which can be easily produced at low cost, is effective as an agent for prevention and treatment of osteoporosis induced by various factors such as diet, dietary restriction, etc., is highly safe, and can be used regularly; and foods and drinks comprising the composition, which is effective as an agent for prevention and treatment of osteoporosis induced by various factors such as diet, dietary restriction, etc., and suitable as foods and drinks for hospitals, healthy drinks or foods, feeds, etc. | 06-18-2009 |
20090156589 | 1,2-DI(CYCLIC GROUP)SUBSTITUTED BENZENE DERIVATIVE - A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action and cell infiltration inhibitory action. | 06-18-2009 |
20090149647 | PROCESS FOR PRODUCTION OF LIPID A ANALOGUE - Discloses is a process for producing α-D-glucopyranose, 3-O-decyl-2-deoxy-6-O-[2-deoxy-3-O-[(3R)-3-methoxydecyl]-6-O-methyl-2-[(11Z)-1-oxo-11-octadecenyl]amino]-4-O-phosphono-β-D-glucopyranosyl]-2-[(1,3-dioxotetradecyl)amino]- or 1-(dihydrogen phosphate) tetrasodium salt which is useful as an active ingredient of a pharmaceutical or an intermediate for the synthesis thereof, which is environment-friendly and excellent in safety, operationality and reproducibility. A process for producing a compound represented by the formula (I) comprising the steps of reacting a compound represented by the formula (VIII) with a palladium catalyst in the presence of a nucleopholic agent and treating the product with a sodium source. | 06-11-2009 |
20090136564 | MICELLES - The present invention provides micelles, solutions comprising micelles, methods for preparing micelles, and methods for delivering micelles to patients. The micelles have fixed, preselected hydrodynamic diameters and are formed from basic or acidic amphiphilic compounds. | 05-28-2009 |
20090117586 | FUNGAL CELL WALL SYNTHESIS GENE - A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved. | 05-07-2009 |
20090114877 | Composition Containing Stability-Improved Chloromethyl Phosphate Derivatve and Process for Producing Same - The present invention provides a production process or the like, which is a process for producing a chloromethyl phosphate derivative useful for producing a water-soluble prodrug, and which is excellent from the points of view of workability, operativity and energy saving. According to the present invention, there is provided a process for producing a composition containing a compound represented by the following Formula (I) and a tertiary amine, | 05-07-2009 |
20090111122 | METHOD FOR NON-INVASIVE EXAMINATION OF NON-ALCOHOLIC STEATOHEPATITIS BY QUANTIFICATION OF CYTOCHROME-c, AND TEST KIT - It is found that blood cytochrome c levels quantified for non-alcoholic steatohepatitis patients are higher than those for healthy persons, and that the quantified blood cytochrome c values correlated with fat deposition rates in hepatocytes. It is possible to test non-alcoholic steatohepatitis by quantifying cytochrome c in serum. A test method and a test kit for the test are provided. | 04-30-2009 |
20090098636 | FUNGAL CELL WALL SYNTHESIS GENE - A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved. | 04-16-2009 |
20090087842 | Presynaptic protein cast - The present invention enabled the detection and quantification of CAST, which is localized to synapses and tightly bound to the cytomatrix, and of the mRNA encoding the CAST. Furthermore, it was revealed that CAST functions as a protein scaffold for localizing RIM1 to synapses, contributing as a molecular basis for active zone formation. | 04-02-2009 |
20090082313 | Multikinase Inhibitors for Use in the Treatment of Cancer - The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): | 03-26-2009 |
20090075290 | IMMUNOCHEMICAL DETERMINATION METHOD AND DETERMINATION REAGENT FOR CYTOCHROME - An immunochemical method for the accurate measurement of the quantity of cytochrome c in a body fluid, in particular, blood, and a kit for the measurement. The quantity of cytochrome c can be measured accurately without being affected by any interfering substrate by reacting an antibody with cytochrome c in a buffer solution in an acidic range. | 03-19-2009 |
20090062539 | CRYSTALS, AMORPHOUS SUBSTANCES OR SALTS OF METHYL N-[3-(6,7-DIMETHOXY-2-METHYLAMINOQUINAZOLIN-4-YL) PHENYL] TEREPHTHALAMIC ACID - Crystals, amorphous substances, salts, and hydrates of salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid have PDE4 inhibitory action and are useful for treating allergic diseases such as atopic dermatitis. | 03-05-2009 |
20090023778 | Composition Containing Anti-Dementia Drug - An object of the present invention is to provide, for the case of implementing a therapeutic method in which at least two kinds of anti-dementia drugs are used together, a composition that has a good therapeutic effect on dementia, and also gives excellent compliance. Another object of the present invention is to provide a composition containing at least two kinds of anti-dementia drugs, in which release of the anti-dementia drugs from the composition is controlled, whereby a combined effect of the anti-dementia drugs can be achieved well. Still another object of the present invention is to provide a composition for which the frequency of administration and the amount taken are reduced and hence compliance can be improved, and a method of manufacturing such a composition. According to the present invention, there is provided a composition containing at least two kinds of anti-dementia drugs; such a composition containing at least one sustained-release portion containing an anti-dementia drug; and such a composition containing at least one cholinesterase inhibitor, and at least one N-methyl-D-aspartate receptor antagonist. | 01-22-2009 |
20090018331 | CONDENSED IMIDAZOLE DERIVATIVES - The present invention is related to compounds represented by the following formula, or salts or hydrates thereof | 01-15-2009 |
20090011951 | Method of Gene Screening With Yeast Having Ergosterol Synthase Undergoing Inducible Expression - An expression of an ergosterol biosynthetic enzyme such as ERG6 and ERG3 is regulated with an inducible promoter, and transformation is performed in a state where the enzyme is expressed, and then screening or assay of drug-resistant colonies is performed in a state where the expression of the enzyme is repressed. | 01-08-2009 |
20080319188 | Novel pyridine derivatives and pyrimidine derivatives (3) - A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. | 12-25-2008 |
20080318924 | PHENOXYPYRIDINE DERIVATIVE SALTS AND CRYSTALS THEREOF, AND PROCESS FOR PREPARING THE SAME - The invention provides acid addition salts of the compounds represented by formula (1) or (2), or crystals thereof, and processes for preparing the same. The salts or crystals have HGFR inhibitory activity and excellent physical properties (solubility, safety, etc.) and are therefore useful as anti-tumor agents, angiogenesis inhibitors and inhibitors for metastasis for a various types of tumor. | 12-25-2008 |
20080312317 | 12 MEMBERED-RING MACROLACTAM DERIVATIVES - There provided a 12-membered-ring macrolactam derivative having antitumor activity: A compound represented by Formula (1) or a salt thereof. In this Formula, R | 12-18-2008 |
20080312284 | Amorphous Form of 1,2-Dihydropyridine Compound - An amorphous form of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridine-2-one. | 12-18-2008 |
20080306272 | ONE-POT METHODS FOR PREPARING CINNAMIDE DERIVATIVES - A compound represented by the following formula ( | 12-11-2008 |
20080280301 | Lrp4/Corin DOPAMINERGIC NEURON PROLIFERATIVE PROGENITOR CELL MARKERS - In neuron transplantation therapy, in terms of safety, it is preferable to use a cell population consisting only of a desired type of cells, and to use postmitotic neurons in consideration to avoid the risk of tumorigenesis. Moreover, greater therapeutic effects would be expected through the use of earlier progenitor cells in consideration of post-transplantation viability, proper network formation ability, and such. | 11-13-2008 |
20080261272 | FUNGAL CELL WALL SYNTHESIS GENE - A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved. | 10-23-2008 |
20080248963 | Hybridization Method - A hybridization method is provided in which an efficient hybridization reaction can be carried out. Further, there are provided, using this hybridization method, a method for detecting a target gene with high sensitivity and a signal amplifying method for markedly improving the detection sensitivity of the target gene. There is provided a hybridization method comprising the use of oligonucleotides in a reaction solution, the method comprising forming partially a reaction temperature region in the reaction solution and performing a hybridization reaction in the reaction temperature region. | 10-09-2008 |
20080248502 | Methods For Detecting Th1 Cells - The inventors discovered that the adhesion molecule CAR, known to be localized in intracellular adhesion sites, functioned as an adhesion molecule for activated lymphocytes. Further, the inventors identified CARL, a novel CAR ligand expressed in lymphocytes, and clarified that the ligand was expressed selectively in Th1 cells. In addition, they found that anti-CAR antibodies could inhibit the adhesion of activated lymphocytes to CAR molecules. Thus, the present invention provides methods for detecting Th1 cells using CAR or anti-CARL antibodies, and methods of screening for inhibitors suppressing the adhesion of Th1 cells using the binding between CAR and CARL as an index. Furthermore, the present invention relates to methods of screening for inhibitors of the binding between CAR and CARL, antibodies that inhibit the binding between CAR and CARL, and therapeutic compositions comprising these antibodies. These are expected to be useful in diagnosing diseases, such as inflammation, in which infiltration of Th1 cells is involved, and in providing pharmaceutical agents for alleviating such diseases. | 10-09-2008 |
20080242859 | Oxymethyl Boron Compounds - The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity. | 10-02-2008 |
20080214834 | Methods For Producing Isoindole Derivatives - The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II): | 09-04-2008 |
20080214815 | Process for preparing phenoxypyridine derivatives - A process for preparing a compound represented by the formula (I): | 09-04-2008 |
20080214564 | MACROLIDE COMPOUND IN SOLID FORM, PROCESS FOR PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed. | 09-04-2008 |
20080214557 | METHOD FOR PREPARATION OF PHARMACEUTICAL COMPOSITION HAVING IMPROVED DISINTEGRATABILITY AND PHARMACEUTICAL COMPOSITION MANUFACTURED BY SAME METHOD - There exists a strong desire both for pharmaceutical compositions which rapidly exhibit pharmacological effects without an increase in the size of the dosage form or a decline in quality due to interactions between a pharmaceutically active ingredient and the disintegrant, and also for a method of preparing such pharmaceutical compositions. Such a desire is especially acute with regard to, for example, preparations which contain a drug such as an analgesic or a quick-acting hypoglycemic drug that requires the rapid appearance of pharmacological effects following administration, preparations which have a high content of the pharmaceutically active ingredient, and preparations which contain two or more different pharmaceutically active ingredients. Thus, the object of the present invention is to improve the disintegratability of the pharmaceutical compositions without increasing the size of the dosage form and without a decline in quality due to interactions between the pharmaceutically active ingredient and the disintegrant. The present invention provides a method for preparing a pharmaceutical composition having a rapid disintegration time, comprising: blending, in the pharmaceutical composition containing a pharmaceutically active ingredient, at least one disintegrant and at least one water-soluble salt having a pH being from 3 to 9 in an aqueous solution of 2.5% concentration. The invention also provides a premix composition obtained by the preliminary mixture of a disintegrant with a water-soluble inorganic salt having a pH of from 3 to 9 in an aqueous solution of 2.5% concentration. | 09-04-2008 |
20080213757 | Methods of Distinguishing Types of Spinal Neurons Using Corl1 Gene as an Indicator - As a result of screening for genes that are selectively expressed in fetal mouse brain region by subtraction method, the present inventors obtained a cDNA fragment encoding Corl1. The expression of Corl1 was examined by RT-PCR, in situ hybridization, and immunostaining using polyclonal antibodies. The results demonstrated that Corl1 was especially expressed at a high level of selectively in the central nervous system during embryonic stages. The expression patterns of Corl1 determined using various markers in embryonic spinal cord were compared to identify types of neurons expressing Corl1. The results revealed that Corl1 was specifically expressed in spinal cord interneurons dI4, dI5, dILA, and dILB. Accordingly, the present invention provides for discrimination between dI4 and dI6, neurons which previously could only be discriminated based on developmental location, using the expression of Corl1 as an indicator. | 09-04-2008 |