| Takeda Pharmaceutical Company Limited Patent applications |
| Patent application number | Title | Published |
|---|
| 20120129868 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Compounds of the following formula are provided for use with PARP: | 05-24-2012 |
| 20120122835 | Poly (ADP-Ribose) Polymerase (PARP) Inhibitors - Disclosed are compounds of the following formula: | 05-17-2012 |
| 20120095057 | PYRAZOLE COMPOUND - Provided is a compound having a superior acid secretion suppressive action, antiulcer activity and the like. | 04-19-2012 |
| 20120094992 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): | 04-19-2012 |
| 20120094899 | NEUROMEDIN U DERIVATIVE - An object of the present invention is to provide a novel anorectic agent. Another object of the invention is to provide an NMU derivative which exhibits a high anorectic effect even when administered in a usual manner, for example, peripherally. These objects can be achieved by the compound represented by formula (I) | 04-19-2012 |
| 20120094898 | PEPTIDE DERIVATIVE - The present invention relates to a peptide derivative selected from the group consisting of
| 04-19-2012 |
| 20120088826 | PROCESS FOR PRODUCTION OF OPTICALLY ACTIVE AMINE DERIVATIVES - An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)ethylamine to asymmetric reduction, catalytically reducing the obtained product at a reaction temperature of 40 to 100° C. and a pH of 3 to 9, subjecting the obtained (S)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethylamine to propionylation, and then crystallizing the reaction mixture. | 04-12-2012 |
| 20120088797 | 1-HETEROCYCLYLSULFONYL, 3-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 04-12-2012 |
| 20120077985 | PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME - The present invention provides an industrially advantageous process for producing a steroid C | 03-29-2012 |
| 20120077799 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a compound represented by the formula (I): | 03-29-2012 |
| 20120071486 | THIENOPYRIMIDINE COMPOUNDS AND USE THEREOF - The present invention provides a compound represented by the formula: | 03-22-2012 |
| 20120040981 | THIENOPYRIMIDINE AS CDC7 KINASE INHIBITORS - The present invention relates to a compound represented by the formula (I): | 02-16-2012 |
| 20120028951 | PYRIDAZINONE COMPOUNDS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I | 02-02-2012 |
| 20120015868 | Metastin derivatives and use thereof - The present invention provides a metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivitives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action. | 01-19-2012 |
| 20110319450 | BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent. | 12-29-2011 |
| 20110312898 | PROPHYLACTIC / THERAPEUTIC AGENT FOR CANCER - A prophylactic/therapeutic agent for androgen-independent cancer is provided. A prophylactic/therapeutic agent for androgen-independent cancer includes a metastin derivative, and is particularly useful as a prophylactic/therapeutic agent for androgen-independent cancer, in particular, androgen-independent prostate cancer. | 12-22-2011 |
| 20110306769 | PROCESS FOR PRODUCING PYRROLE COMPOUND - The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction. | 12-15-2011 |
| 20110301174 | 1-HETEROCYCLYLSULFONYL, 3-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 12-08-2011 |
| 20110301173 | 1-HETEROCYCLYLSULFONYL, 3-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 12-08-2011 |
| 20110300068 | AGENT FOR PROPHYLAXIS OR TREATMENT OF CANCER - The present invention provides an agent for the prophylaxis or treatment of kidney cancer or urinary bladder cancer, and a diagnostic reagent for these cancers which comprise an antibody against nerve growth factor 2/neurotrophin-3 or a partial peptide thereof or a salt thereof, which antibody neutralizes nerve growth factor 2/neurotrophin-3 and does not cross-react with the Nerve Growth Factor. | 12-08-2011 |
| 20110288040 | ARYL- OR HETEROARYL-SULFONYL COMPOUNDS AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like. | 11-24-2011 |
| 20110257405 | PROCESS FOR PRODUCING CRYSTAL - The present invention relates to a production method of a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.n′H | 10-20-2011 |
| 20110237620 | HETEROCYCLIC COMPOUND AND USE THEREOF - A compound represented by formula (I) or a salt thereof, which has a potent Raf inhibitory activity. | 09-29-2011 |
| 20110212982 | Administration of Dipeptidyl Peptidase Inhibitors - Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions. | 09-01-2011 |
| 20110212890 | METASTIN DERIVATIVE AND USE THEREOF - Disclosed is a stable metastin derivative having excellent biological activities (e.g., a cancer metastasis inhibiting activity, a cancer proliferation inhibiting activity, a gonadotropin secretion promoting activity, a sex hormone secretion promoting activity). A metastin derivative produced by substituting a constituent amino acid in metastin can be improved in stability in the blood and can have an excellent cancer metastasis inhibiting activity, an excellent cancer proliferation inhibiting activity, an excellent gonadotropin secretion inhibiting activity, an excellent sex hormone secretion inhibiting activity and the like by binding the metastin derivative to polyethylene glycol. | 09-01-2011 |
| 20110201818 | POLO-LIKE KINASE INHIBITORS - Compounds of the following formula are provided for use with kinases: | 08-18-2011 |
| 20110196003 | TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula | 08-11-2011 |
| 20110192748 | Administration of Dipeptidyl Peptidase Inhibitors - Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions. | 08-11-2011 |
| 20110190361 | TRICYCLIC COMPOUND AND PHARMACEUTICAL USE THEREOF - The present invention provides a compound represented by the formula | 08-04-2011 |
| 20110190261 | MAPK/ERK Kinase Inhibitors - Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(pyrimidinylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: | 08-04-2011 |
| 20110189282 | TABLET - The present invention can retain the volume of a tablet large without increasing the thickness of the tablet or the like dimension and prevents a plurality of tablets from sticking to each other even if they are subjected to a film-coating or the like treatment, so as to improve the yield. The tablet is a tablet ( | 08-04-2011 |
| 20110184178 | POLYMORPHS OF 5-(3-(ETHYLSULFONYL)PHENYL)-3,8-DIMETHYL-N-(1-METHYLPIPERIDIN-4-YL)-9H-PY- RIDO[2,3-B]INDOLE-7-CARBOXAMIDE AND METHODS OF USE THEREFOR - The invention relates to polymorphic forms of 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide (referred to herein as Compound I), which has the formula: | 07-28-2011 |
| 20110178070 | PI3K/mTOR INHIBITORS - The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula: | 07-21-2011 |
| 20110172275 | PYRROLE COMPOUNDS - The present invention relates to a compound represented by the formula: | 07-14-2011 |
| 20110172245 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a heterocyclic compound showing strong Raf inhibitory activity. A compound represented by the formula | 07-14-2011 |
| 20110172204 | COMPOUNDS AND THEIR USE - A compound of the formula: | 07-14-2011 |
| 20110158989 | Poly (ADP-Ribose) Polymerase (PARP) INHIBITORS - Disclosed are compounds of the following formula: | 06-30-2011 |
| 20110152273 | FUSED HETEROAROMATIC PYRROLIDINONES - Disclosed are compounds of Formula 1, | 06-23-2011 |
| 20110144161 | 1-HETEROCYCLYLSULFONYL, 2-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 06-16-2011 |
| 20110136780 | DIHYDROPYRROLONAPHTYRIDINONE COMPOUNDS AS INHIBITORS OF JAK - Disclosed are JAK inhibitors of formula I | 06-09-2011 |
| 20110130384 | AMIDE COMPOUND - The present invention aims to provide a prophylactic or therapeutic agent for schizophrenia and the like, containing the compound of the present invention having a GPR52 agonist activity. A compound represented by the following formula (I) or a salt thereof: | 06-02-2011 |
| 20110124876 | IMINOPYRIDINE DERIVATIVES AND USE THEREOF - The present invention aims to provide an iminopyridine derivative compound having an α | 05-26-2011 |
| 20110124875 | IMINOPYRIDINE DERIVATIVES AND USES THEREOF - The present invention aims to provide an iminopyridine derivative compound having an α | 05-26-2011 |
| 20110124874 | IMINOPYRIDINE DERIVATIVES AND USE THEREOF - The present invention aims to provide an iminopyridine derivative compound having an α | 05-26-2011 |
| 20110124687 | PHARMACEUTICAL COMPOSITION - The present invention provides a pharmaceutical composition or a solid preparation containing a stabilized pharmaceutically active ingredient and a stabilizing method thereof. | 05-26-2011 |
| 20110124626 | BENZAZEPINE DERIVATIVES AND THEIR USE AS HISTAMINE H3 ANTAGONISTS - A compound having the formula (1) wherein: R1 is a group selected from C | 05-26-2011 |
| 20110118172 | METASTIN DERIVATIVE AND USE THEREOF - The invention provides a stable metastin derivative having excellent biological activities (a cancer metastasis-inhibiting activity, a cancer proliferation-inhibiting activity, a gonadotropin secretion-promoting activity, a sex hormone secretion-promoting activity, etc.). By replacing the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, the blood stability and solubility of the metastin derivative can be more improved, the gel tendency of the metastin derivative can be reduced, the pharmacokinetics of the metastin derivative can be improved, and the metastin derivative can exhibit an excellent cancer metastasis-inhibiting activity and cancer proliferation-inhibiting activity. The metastin derivative can also exhibit a gonadotropin secretion-inhibiting activity, a sex hormone secretion-inhibiting activity, etc. | 05-19-2011 |
| 20110112133 | DIHYDRO PYRROLOQUINOLINE DERIVATIVES - A compound represented by the formula (I) | 05-12-2011 |
| 20110104705 | Musclin receptor and use thereof - The present invention provides a receptor of musclin and a screening system for an agonist and/or antagonist of the receptor by means of the interaction of musclin and the receptor. Hence, provided is a screening method for a substance that alters the bindability (i) a protein containing the same or substantially the same amino acid sequence as the amino acid sequence shown by SEQ ID NO:2 or a partial peptide thereof or a salt thereof and (ii) musclin or a partial peptide thereof or a salt thereof, containing using both. | 05-05-2011 |
| 20110098336 | PYRROLIDIN-2-ONE DERIVATIVES AS ANDROGEN RECEPTOR MODULATOR - A compound represented by the formula (I) according to claim | 04-28-2011 |
| 20110098297 | FUSED RING COMPOUNDS AND USE THEREOF - The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof. | 04-28-2011 |
| 20110091563 | ORALLY-DISINTERGRATING SOLID PREPARATION - The present invention provides an orally-disintegrating solid preparation such as a tablet produced by tabletting fine granules showing controlled release of a pharmaceutically active ingredient and an additive, and the like, and the orally-disintegrating solid preparation containing fine granules coated with a coating layer containing a polymer affording a casting film having an elongation at break of about 100-about 700%. With the preparation, breakage of fine granules during tabletting can be suppressed in the production of an orally-disintegrating solid preparation containing fine granules showing controlled release of a pharmaceutically active ingredient. | 04-21-2011 |
| 20110082111 | POLO-LIKE KINASE INHIBITORS - Compounds of the following formula are provided for use with kinases: | 04-07-2011 |
| 20110081412 | ORALLY DISINTEGRABLE TABLETS - An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 μm or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration. | 04-07-2011 |
| 20110077402 | ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions. | 03-31-2011 |
| 20110070297 | GLUCOKINASE ACTIVATORS - Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: | 03-24-2011 |
| 20110065733 | MAPK/ERK KINASE INHIBITORS - Compounds of the following formula are provided for use with MEK: | 03-17-2011 |
| 20110059888 | METASTIN DERIVATIVES AND USE THEREOF - The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotropic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids, the metastin derivatives of the present invention achieve more improved blood stability, solubility, etc., reduced gelation tendency, improved pharmacokinetics, as well as exhibit an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity. The metastin derivatives of the present invention also have a gonadotropic hormone secretion suppressing activity, sex hormone secretion suppressing activity, etc. | 03-10-2011 |
| 20110053921 | HEXAHYDROOXAZINOPTERINE COMPOUNDS - The present invention provides mTOR inhibitors of the formula | 03-03-2011 |
| 20110053873 | HSP90 INHIBITORS - The invention relates to HSP90 inhibiting compounds consisting of the formula: (I) wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds. | 03-03-2011 |
| 20110052563 | GONADAL FUNCTION IMPROVING AGENTS - Metastin, compounds that promote the activity of metastin or its receptors and the like are excellent gonadal function improving agents, ovulation inducers or promoters, gonadotropic hormone secretion promoters, gonadotropic hormone secretion inhibitors, sex hormone secretion promoters, sex hormone secretion inhibitors, etc., and can be used as agents for preventing/treating sterility, hormone-sensitive cancers, endometriosis, etc. Metastin and its receptors are useful for screening for these pharmaceuticals. | 03-03-2011 |
| 20110046183 | CRYSTAL OF BENZIMIDAZOLE COMPOUND - Provided is a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole showing an X-ray powder diffraction pattern having characteristic peaks at interplanar spacings (d) of 10.06±0.2, 8.70±0.2, 6.57±0.2, 5.59±0.2 and 4.00±0.2 Angstroms. The present invention provides a stable antiulcer drug superior in the absorbability. | 02-24-2011 |
| 20110046169 | FUSED HETEROCYCLIC DERIVATIVES AND USE THEREOF - The present invention provides a fused heterocyclic derivative having a strong kinase inhibitory activity and use thereof. | 02-24-2011 |
| 20110045028 | SUSTAINED RELEASE PREPARATION - Disclosed is a sustained-release preparation which is prepared by shaping a granule comprising a blood coagulation factor Xa inhibitor and a mixture of at least two hydrophilic polymers. Also disclosed is a pharmaceutical composition comprising a combination of the sustained-release preparation and an immediate release preparation comprising a blood coagulation factor Xa inhibitor. It becomes possible to provide a controlled release preparation comprising a blood coagulation factor Xa inhibitor for the prevention or treatment of thrombosis, which can control the activity of blood coagulation factor Xa for a long term and is excellent in convenience and compliance. It is also becomes possible to provide a method for producing the controlled release preparation. | 02-24-2011 |
| 20110039892 | IMINOPYRIDINE DERIVATIVE AND USE THEREOF - The present invention aims to provide a compound having a superior selective α | 02-17-2011 |
| 20110039846 | IMINOPYRIDINE DERIVATIVES AND USE THEREOF - The present invention aims to provide an iminopyridine derivative compound having an α1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof. | 02-17-2011 |
| 20110039786 | METASTIN DERIVATIVE AND USE THEREOF - The present invention provides a metastin derivative represented by the formula (I): | 02-17-2011 |
| 20110034469 | Heterocyclic Compound - The present invention provides a compound represented by the formula | 02-10-2011 |
| 20110034464 | IMINOPYRIDINE DERIVATIVES AND USE THEREOF - The present invention aims to provide an iminopyridine derivative compound having an α | 02-10-2011 |
| 20110021515 | DIHYROFUROPYRMINDINE COMPOUNDS - The present invention provides mTOR inhibitors of the formula | 01-27-2011 |
| 20110020410 | STABLE SOLID PREPARATIONS - It is intended to provide a process for producing unstable amorphous benzimidazole compounds having a proton pump inhibitor function, and stable solid preparations for medicinal use containing these compounds which are produced by blending such an amorphous benzimidazole compound with a nontoxic base such as a basic inorganic salt, forming an intermediate coating layer on the layer containing the active ingredient and further forming an enteric coating layer or a release-controlling coating layer. | 01-27-2011 |
| 20110014299 | SOLID PREPARATION COMPRISING ALOGLIPTIN AND METFORMIN HYDROCHLORIDE - The present invention provides a solid preparation containing compound (I) [compound (I) is as defined in the specification] or a salt thereof, and metformin hydrochloride, which is useful as a therapeutic drug for diabetes and the like, and superior in the preservation stability. A solid preparation having a first part and a second part: a first part: a part containing compound (I) or a salt thereof and substantially free of metformin hydrochloride a second part: a part containing metformin hydrochloride and substantially free of compound (I) and a salt thereof. | 01-20-2011 |
| 20110009421 | COMPOUND HAVING 6-MEMBERED AROMATIC RING - An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPRS2 agonist activity. | 01-13-2011 |
| 20110009389 | IMIDAZOLE DERIVATIVE, THEIR PRODUCTION AND USE - There is provided an imidazole derivative useful as a thrombosis treating agent, which is represented by the formula (I): | 01-13-2011 |
| 20110003807 | Thiazole derivatives - The present invention relates to a compound represented by the formula (I) or (I′): | 01-06-2011 |
| 20110003806 | Heteroaryls and uses thereof - This invention provides compounds of formula IA or IB: | 01-06-2011 |
| 20110003805 | CONCOMITANT DRUG - Provided is a combination drug. The present invention provides a pharmaceutical agent comprising (1) a HER2 inhibitor having a pyrrolopyrimidine skeleton or pyrazolopyrimidine skeleton, and (2) not less than one pharmaceutical agent selected from an mTOR inhibitor, a PI3 kinase inhibitor and a cMet inhibitor in combination. | 01-06-2011 |
| 20110003788 | FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR | 01-06-2011 |
| 20100331520 | METASTIN DERIVATIVES AND USE THEREOF - The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotrophic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, blood stability, solubility, etc. are more improved, gelation tendency is reduced, pharmacokinetics are also improved, and an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity is exhibited. Furthermore, the metastin derivative of the present invention has the effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc. | 12-30-2010 |
| 20100331402 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR ATTENTION DEFICIT/HYPERACTIVITY DISORDER - The present invention provides a novel prophylactic or therapeutic agent for attention deficit/hyperactivity disorder. | 12-30-2010 |
| 20100331373 | DRUG-CONTAINING NANOPARTICLES - The present invention relates to nanoparticles containing pioglitazone or a salt thereof and a biocompatible polymer, a pharmaceutical preparation containing the nanoparticles for the prophylaxis or treatment of arteriosclerotic diseases, and a stent carrying the nanoparticles. Using the nanoparticles of the present invention, rupture of arteriosclerotic plaque can be suppressed, and they are useful for the prophylaxis or treatment of arteriosclerotic diseases. | 12-30-2010 |
| 20100331357 | PHARMACEUTICAL COMPOSITION - The present invention provides a pharmaceutical composition, wherein solubility and stability of a water-insoluble or slightly water-soluble compound represented by formula (I): wherein each symbol is as defined in the specification, are improved, by combination of the above-mentioned compound and a cyclodextrin derivative and a method for improving solubility, stability and the like of the above-mentioned compound. | 12-30-2010 |
| 20100324010 | AMIDE COMPOUNDS AND USE OF THE SAME - A renin inhibitor comprising a compound represented by the formula: | 12-23-2010 |
| 20100316709 | ORALLY DISINTEGRATING SOLID PREPARATION - The present invention provides an orally-disintegrating solid preparation comprising fine granules showing controlled release of a pharmaceutically active ingredient, wherein the outermost layer of the fine granules is coated with a coating layer comprising hydroxypropylmethylcellulose and low-substituted hydroxypropylcellulose and breakage of the fine granules during tableting is suppressed. | 12-16-2010 |
| 20100311077 | Use of GPR100 Receptor in Diabetes and Obesity Regulation - We describe a method of identifying a molecule suitable for the treatment, prophylaxis or alleviation of a Gpr100 associated disease, in particular diabetes and obesity, the method comprising determining whether a candidate molecule is an agonist or antagonist of Gpr100 polypeptide, in which the Gpr100 polypeptide comprises the amino acid sequence shown in SEQ ID NO: 3 or SEQ ID NO: 5, or a sequence which is at least 90% identical thereto. | 12-09-2010 |
| 20100311075 | HUMAN SODIUM-DEPENDENT BILE ACID TRANSPORTER PROTEINS - A novel sodium-dependent bile acid transporter protein, an Na | 12-09-2010 |
| 20100310670 | SUSTAINED-RELEASE MICROSPHERE CONTAINING SHORT CHAIN DEOXYRIBONUCLEIC ACID OR SHORT CHAIN RIBONUCLEIC ACID AND METHOD OF PRODUCING THE SAME - A sustained-release microsphere formulation containing a short chain deoxyribonucleic acid or a short chain ribonucleic acid as an active ingredient, which has improved sustained-release properties and long-lasting efficacy, is provided. A fine particle formulation, encapsulating stably a short chain deoxyribonucleic acid or a short chain ribonucleic acid, being capable of inhibiting, for a long period, expression of a specific protein related to a disease, and which can be administered by injection or transmucosally, and a production method of the same are provided. A sustained-release microsphere formulation containing a short chain deoxyribonucleic acid or a short chain ribonucleic acid, particularly siRNA, as an active ingredient, especially a sustained-release microsphere prepared through a w | 12-09-2010 |
| 20100286400 | CRYSTALLINE SOLVATED FORMS OF (R)-2-[[[3-METHYL-4-(2,2,2-TRIFLUOROETHOXY)-2-PYRIDINYL]METHYL]SULFINYL]-- 1H-BENZIMIDAZOLE - The novel hydrate, methanol solvate, ethanol solvate, ethanol•hydrate and isopropanol•hydrate crystals of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole of the present invention are useful as excellent antiulcer agents. | 11-11-2010 |
| 20100286120 | PYRIDOOXAZEPINE DERIVATIVE AND USE THEREOF - The present invention provides a compound having a superior serotonin 5-HT | 11-11-2010 |
| 20100286035 | NEUROMEDIN U DERIVATIVE - The objective of the present invention is to provide a new antifeedant. The other objective of the present invention is to provide a NMU derivative showing a high antifeedant activity even in common administration forms such as peripheral administration. A neuromedin U derivative wherein a methoxypolyethylene glycol is bound via a linker having a specific structure to a polypeptide which contains at least 8 amino acids of the C-terminus of an amino acid sequence of neuromedin U and which consists of the same or substantially the same amino acid sequence as the amino acid sequence of neuromedin U. | 11-11-2010 |
| 20100285120 | CONTROLLED RELEASE PREPARATION - A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient. | 11-11-2010 |
| 20100278911 | CONTROLLED RELEASE PREPARATION - A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient. | 11-04-2010 |
| 20100273852 | PHARMACEUTICAL COMPOSITION - There is provided a pharmaceutical composition comprising (1) (R)-5,6-dimethoxy-2-[2,2,4,6,7-pentamethyl-3-(4-methylphenyl)-2,3-dihydro-1-benzofuran-5-yl]isoindoline, (2) a lipophilic component, and (3) a surfactant, which can stably and sufficiently provide improvement in the absorbability of the drug without being affected by the amount and quality of a meal. | 10-28-2010 |
| 20100273788 | FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. | 10-28-2010 |
| 20100272798 | CONTROLLED RELEASE PREPARATION - A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient. | 10-28-2010 |
| 20100272727 | COMPOUND FOR CONTROLLING APPETITE - Insl5 has been found to be orexigenic, i.e. it increases appetite. Insl5, or a derivative or fragment thereof that retains the ability to bind to the GPR100 receptor, or an Insl5 antibody, are useful in therapy, in particular to treat anorexia nervosa, bulimia, cachexia or wasting disease. | 10-28-2010 |
| 20100267821 | PROPHYLACTIC OR THERAPEUTIC AGENT FOR IRRITABLE BOWEL SYNDROME - The present invention provides a prophylactic or therapeutic agent for irritable bowel syndrome, which comprises a compound represented by formula (I): | 10-21-2010 |
| 20100249119 | HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention provides a heterocyclic compound having a strong Raf inhibitory activity, which is represented by the following formula | 09-30-2010 |
| 20100240743 | CANNABINOID RECEPTOR MODULATOR - A cannabinoid receptor modulator containing a compound represented by Formula (I | 09-23-2010 |
| 20100239501 | GENE SENSITIVE TO BONE/JOINT DISEASE AND USE THEREOF - The present invention provides a suppressing agent for inflammatory cytokine expression in joints and/or joint destruction (e.g., articular cartilage destruction) and/or pain in a bone/joint disease, comprising a substance that suppresses the expression or activity of a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence shown by SEQ ID NO:2, a screening method for a substance that regulates inflammatory cytokine expression in joints and/or joint destruction (e.g., articular cartilage destruction) and/or pain in a bone/joint disease, comprising using the protein or a partial peptide thereof, and a diagnostic method for genetic susceptibility to a bone/joint disease, comprising detecting a polymorph in the base shown by base number 24007 in the partial base sequence of the human EDG2 gene shown by SEQ ID NO:3. | 09-23-2010 |
| 20100234389 | AMIDE COMPOUND - An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. | 09-16-2010 |
| 20100234351 | FUSED NITROGEN-COMPRISING HETEROCYCLIC COMPOUND - A compound of the formula: | 09-16-2010 |
| 20100227846 | SUBSTITUTED PYRAZOLE DERIVATIVE - The present invention provides a novel pyrazole derivative and an androgen receptor antagonist containing the derivative. The present invention provides a compound represented by the formula (I′) | 09-09-2010 |
| 20100222575 | POLO-LIKE KINASE INHIBITORS - The present invention relates generally to processes of making 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide and Form A of 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide. | 09-02-2010 |
| 20100222391 | BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent. | 09-02-2010 |
| 20100216810 | HETEROCYCLIC COMPOUND AND USE THEREOF - Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. | 08-26-2010 |
| 20100216788 | FUSED HETEROCYCLIC COMPOUND - The present invention provides a compound represented by the formula: | 08-26-2010 |
| 20100216765 | KINASE INHIBITORS - Compounds, pharmaceutical compositions and kits are provided for use with kinases that comprise a compound selected from the group consisting of: | 08-26-2010 |
| 20100210696 | 5-MEMBERED HETEROCYCLIC COMPOUND - Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like. | 08-19-2010 |
| 20100210635 | RENIN INHIBITORS - Compounds, pharmaceutical compositions, kits and methods are provided for use with Renin that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. | 08-19-2010 |
| 20100204471 | MAPK/ERK KINASE INHIBITORS - Compounds, pharmaceutical compositions, kits and methods are provided for use with MEK that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. | 08-12-2010 |
| 20100190816 | KINASE INHIBITORS - Compounds, pharmaceutical compositions, kits and methods are provided for use with kinases that comprise a compound selected from the group consisting of: | 07-29-2010 |
| 20100190763 | Poly (ADP-Ribose) Polymerase (PARP) Inhibitors - Disclosed are compounds of the following formula: | 07-29-2010 |
| 20100183604 | PREVENTIVE/REMEDY FOR CANCER - The present invention provides an agent for preventing or treating a trastuzumab-resistant cancer, which contains one or more medicaments selected from a cofilin inhibitor, a PAK1 inhibitor, a LIMK inhibitor, a RHO inhibitor, a ROCK1 inhibitor and a ROCK2 inhibitor. | 07-22-2010 |
| 20100168424 | FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof | 07-01-2010 |
| 20100160633 | KINASE INHIBITORS - Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: | 06-24-2010 |
| 20100160629 | CYCLIC AMIDE DERIVATIVE, AND ITS PRODUCTION AND USE - The present invention provides a cyclic amide derivative useful as a drug for treating thrombosis, which is represented by the formula (I): | 06-24-2010 |
| 20100160255 | SPIRO-CYCLIC COMPOUND - The present invention provides a compound represented by the formula (I): | 06-24-2010 |
| 20100158894 | PREVENTIVE OR REMEDY FOR ER-NEGATIVE AND HER2-NEGATIVE BREAST CANCER AND METHOD OF SCREENING THE SAME - The present invention provides (1) an agent for the prevention or treatment of an estrogen receptor-negative and HER2-negative breast cancer comprising an Akt inhibitor, (2) an agent for the prevention or treatment of an estrogen receptor-negative, progesterone receptor-negative and HER2-negative breast cancer comprising an Akt inhibitor, (3) a method of screening an agent for the prevention or treatment of a breast cancer which is negative for hormone receptors such as an estrogen receptor, a progesterone receptor, etc. and is negative for HER2, which comprises using an Akt inhibitory activity as an indicator; and so on. | 06-24-2010 |
| 20100152236 | Cyclic amine compound - A compound represented by the formula (I) | 06-17-2010 |
| 20100144806 | Cyclopropanecarboxylic Acid Compound - A compound of the formula (I): | 06-10-2010 |
| 20100137310 | RENIN INHIBITORS - The invention provides compounds, pharmaceutical compositions, kits, method of preparing, and method of using the compounds which exhibit renin and other S9 proteases activities and consist of the formula:—wherein the variables are as defined herein. | 06-03-2010 |
| 20100137281 | HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like, which is useful for the prophylaxis or treatment s of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases, cerebral apoplexy and the like and/or metabolic diseases such as hyperlipidemia, obesity, diabetes and the like, central nervous disorders such as cerebral infarction and the like, mental diseases such as dementia, depression and the like, and the like. | 06-03-2010 |
| 20100130737 | Regulating Agent of GPR34 Receptor Function - The present invention provides a GPR receptor function regulator comprising the compound represented by the formula: | 05-27-2010 |
| 20100130518 | MAPK/ERK KINASE INHIBITORS - Compounds of the following formula are provided for use with MEK (I): wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds. | 05-27-2010 |
| 20100125138 | PROCESS FOR MAKING (R)-3-(2,3-DIHYDROXYPROPYL)-6-FLUORO-5-(2-FLOURO-4-IODOPHENYLAMINO)-8-MET- HYLPYRIDO[2,3-d]PYRIMIDINE-4,7(3H,8H)-DIONE AND INTERMEDIATES THEREOF - The present invention relates generally to processes of making (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione, intermediates thereof, and a process for making a particular polymorph of (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione. | 05-20-2010 |
| 20100119598 | SEAMLESS CAPSULE - The present invention aims to provide a seamless capsule free of an interfacial tension modifier and a gelling agent. The present invention provides a shell formed by a shell composition containing gelatin and a plasticizer, but free of an interfacial tension modifier and a gelling agent, and a seamless capsule comprising a capsule content free of an interfacial tension modifier and a gelling agent. | 05-13-2010 |
| 20100113418 | HETEROCYCLIC COMPOUND - The present invention provides a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention provides a compound represented by the formula (I): | 05-06-2010 |
| 20100113413 | MAPK/ERK Kinase Inhibitors - Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(arylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: | 05-06-2010 |
| 20100105922 | PROCESS FOR PRODUCING FUSED IMIDAZOLE COMPOUND, REFORMATSKY REAGENT IN STABLE FORM, AND PROCESS FOR PRODUCING THE SAME - The present invention provides an industrially advantageous process for producing a steroid C | 04-29-2010 |
| 20100105665 | RENIN INHIBITORS - Compounds, pharmaceutical compositions, kits, article of manufacture, methods of using, and method of preparing of compounds having the formula of: | 04-29-2010 |
| 20100099106 | CELL DEATH INHIBITOR - The cell death inhibitor comprising a substance capable of binding to macrophage migration inhibitory factor is useful as a preventive/therapeutic agent for, e.g., heart diseases, neurodegenerative diseases, cerebrovascular diseases, central nervous infections, traumatic diseases, demyelinating diseases, bone/joint diseases, kidney diseases, liver diseases, myelodysplastic diseases, arteriosclerosis, diabetes, pulmonary hypertension, sepsis, inflammatory bowel diseases, autoimmune diseases, failure accompanying rejection in organ transplantation, AIDS, cancer, etc. | 04-22-2010 |
| 20100094000 | PYRAZOLE COMPOUNDS - The present invention relates to | 04-15-2010 |
| 20100093777 | SPIRO-RING COMPOUND - The present invention aims to provide a compound having an acetyl-CoA carboxylase (ACC) inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. | 04-15-2010 |
| 20100087506 | CYCLIC AMINE COMPOUND - Provision of a compound having a superior androgen receptor regulating action. | 04-08-2010 |
| 20100075973 | POLO-LIKE KINASE INHIBITORS - The present invention provides PLK inhibitors of the formula | 03-25-2010 |
| 20100069362 | Thienopyrimidone compound - The present invention relates to a compound represented by the formula: | 03-18-2010 |
| 20100063745 | METHOD OF ESTIMATING SECONDARY STRUCTURE IN RNA AND PROGRAM AND APPARATUS THEREFOR - Assuming frame F having specific short length L | 03-11-2010 |
| 20100063054 | cMET INHIBITORS - Compounds of the following formula are provided for use with cMET: | 03-11-2010 |
| 20100056577 | PYRROLE COMPOUNDS - The present invention relates to a compound represented by the formula: | 03-04-2010 |
| 20100047349 | Stabilized solid preparation - A stabilized solid preparation having stabilized drug content and stabilized appearance, comprising a main ingredient layer and a coating layer formed on the main ingredient layer, wherein the main ingredient layer comprises a granule or a fine particle comprising a substance capable of being unstabilized when losing water of crystallization and a water-soluble polymer and the coating layer comprises a water-soluble polymer and a sugar. | 02-25-2010 |
| 20100041891 | AMIDE COMPOUND - A compound having GPR52 agonist activity or a salt thereof is provided. | 02-18-2010 |
| 20100040621 | Novel polpeptide and use thereof - The present invention provides various useful polypeptides and so on. In particular, a polypeptide comprising the amino acid sequence represented by SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 7, SEQ ID NO: 8 or SEQ ID NO: 9, a compound or its salt that promotes the activity of said polypeptide, etc. can be utilized as a preventive/therapeutic agent for, e.g., renal edema, dysuria, hyponatremia, syndrome of inappropriate secretion of antidiuretic hormone, hypertension or the like. Furthermore, a compound or its salt that inhibits the activity of the polypeptide is useful as a preventive/therapeutic agent for, e.g., urine storage disorders, polyuria, diabetes insipidus, hypernatremia, metabolic alkalosis, hypokalemia, Cushing syndrome or the like. Moreover, the polypeptide comprising the amino acid sequence represented by SEQ ID NO: 7, SEQ ID NO: 8 or SEQ ID NO: 9 can be utilized as a preventive/therapeutic agent for anorexia, etc., an eating (appetite) stimulant, or the like. | 02-18-2010 |
| 20100034891 | TASTE-MASKING SOLID PREPARATION OF PIOGLITAZONE - A solid preparation sufficiently masking the unpleasant taste of pioglitazone or a salt thereof; a solid preparation sufficiently masking the unpleasant taste of pioglitazone or a salt thereof and having superior properties of superior disintegration property in the oral cavity, appropriate preparation strength, long-term preservation stability and the like is provided. The present invention provides a solid preparation comprising particles comprising (i) core particles comprising an excipient, and (ii) pioglitazone or a salt thereof and an acid-soluble polymer both coating the core particles. | 02-11-2010 |
| 20100029941 | PREPARATION OF (R)-3-AMINOPIPERIDINE DIHYDROCHLORIDE - Described herein are methods for making chiral derivatives of 3-aminopiperidine, including the production of such derivatives in quantities exceeding 1 kilogram. The chiral 3-aminopiperidine derivatives include (R)-3-aminopiperidine derivatives which may be used to synthesize inhibitors of Dipeptidyl Peptidase IV. (R)-3-Aminopiperidine dihydrochloride is prepared by reducing (R)-3-aminopiperidin-2-one hydrochloride with lithium aluminum hydride. The preparation of (R)-3-aminopiperidin-2-one hydrochloride starting from (R)-methyl-2,5-diaminopentanoate dihydrochloride or (R)-2,5-diaminopentanoic acid hydrochloride is also described. | 02-04-2010 |
| 20100016381 | STABLE EMULSION COMPOSITION - The present invention provides an emulsion composition comprising (A) a compound stable in an acidic range, and (B) a buffer, wherein the pH is adjusted from about 3.7 to about 5.5. | 01-21-2010 |
| 20100008926 | NOVEL PROTEINS AND USE THEREOF - Compounds that inhibit the expression of a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, SEQ ID NO: 4, SEQ ID NO: 7 or SEQ ID NO: 10 or the expression of a gene for the protein, the antisense polynucleotide comprising the entire or part of a base sequence complementary or substantially complementary to DNA encoding the protein or its partial peptide, the antibody to the protein or its partial peptide, etc. are useful as prophylactic/therapeutic agents for cancer, etc., apoptosis promoters, etc. | 01-14-2010 |
| 20100008912 | COMBINATION DRUG - The present invention provides a pharmaceutical agent containing an HER2 inhibitor and a hormonal therapeutic agent or anti-cancer agent in combination. The present invention provides a pharmaceutical agent containing (1) an HER2 inhibitor having a pyrrolopyrimidine skeleton or pyrazolopyrimidine skeleton, and (2) a hormonal therapeutic agent or an anti-cancer agent in combination. | 01-14-2010 |
| 20100004458 | PROCESS FOR PRODUCING CRYSTAL - The present invention relates to a production method of a crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]sulfinyl]benzimidazole.n′H | 01-07-2010 |
| 20100004238 | FUSED HETEROCYCLIC COMPOUND - The present invention provides a fused heterocyclic compound having a tyrosine kinase inhibitory action, which is represented by the formula: | 01-07-2010 |
| 20090318425 | APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS - The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula | 12-24-2009 |
| 20090318365 | METASTIN DERIVATIVES AND USE THEREOF - The present invention provides a metastin derivative in which the amino acids comprising metastin were modified by alternative chemical substituents resulting in metastin derivatives, having excellent blood stability and exhibiting cancer metastasis inhibiting action or cancer growth inhibiting action. | 12-24-2009 |
| 20090312383 | Fused Heterocyclic Compounds - There is provided a CRF receptor antagonist comprising a compound of the formula (I): | 12-17-2009 |
| 20090312288 | KINASE INHIBITORS - Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: | 12-17-2009 |
| 20090311701 | Organ-specific gene, method for identifying the same and use thereof - The present invention provides a method of extracting an organ- or tissue-specific highly expressed gene, including: | 12-17-2009 |
| 20090306379 | POLYMORPHS OF BENZOATE SALT OF 2-[[6-[(3r)-3-AMINO-1- PIPERIDINYL]-3,4-DIHYDRO-3- METHYL-2,4-DIOXO-1(2H)-PYRIMIDINYL]METHYL]-BENZONITRILE AND METHODS OF USE THEREFORE - Compositions comprising Compound I, wherein the Compound I is present in one or more polymorphic forms. Also provided are kits and articles of manufacture with compositions comprising one or more polymorphs of Compound I, and methods of using the compositions to treat various diseases. | 12-10-2009 |
| 20090306374 | FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. | 12-10-2009 |
| 20090306200 | Prophylactic or Therapeutic Agent for Nocturnal Conduct Disorder Associated With Dementia - The present invention provides a prophylactic or therapeutic agent for nocturnal conduct disorders associated with dementia, comprising (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide. | 12-10-2009 |
| 20090305998 | HSP90 INHIBITORS - The invention relates to HSP90 inhibiting compounds consisting of the formula: | 12-10-2009 |
| 20090304821 | Pharmaceutical Combination - Disclosed is a pharmaceutical combination comprising a calcium receptor modulator and a bone resorption inhibitor, wherein the calcium receptor modulator comprises a compound represented by the formula (I): | 12-10-2009 |
| 20090298765 | Metastin derivatives and use thereof - The invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, etc.). By modifying the constituent amino acids of metastin with specific modifying groups, metastin derivatives having more improved blood stability, etc. than native metastin and showing excellent cancer metastasis suppressing activity or cancer growth suppressing activity have been found. Furthermore, it has been found that these metastin derivatives exhibit effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc., which are wholly different from the effects heretofore known. | 12-03-2009 |
| 20090291938 | POLO-LIKE KINASE INHIBITORS - Compounds of the following formula are provided for use with kinases: | 11-26-2009 |
| 20090286791 | Amide Compounds - The present invention provides compounds represented by the formula (Ia): | 11-19-2009 |
| 20090281097 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND - The object of the present invention is to provide a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and has superior properties such as efficacy, duration of activity, specificity, low toxicity and the like. | 11-12-2009 |
| 20090281092 | POLO-LIKE KINASE INHIBITORS - Compounds of the following formula are provided for use with kinases: | 11-12-2009 |
| 20090275568 | FUSED QUINOLINE DERIVATIVE AND USE THEREOF - The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) | 11-05-2009 |
| 20090270442 | POLYMORPHS OF HYDROCHLORIDE SALT OF 5-(3-(ETHYLSULFONYL)PHENYL)-3,8-DIMETHYL-N-(1-METHYLPIPERIDIN-4-YL)-9H-PY- RIDO[2,3-B]INDOLE-7-CARBOXAMIDE AND METHODS OF USE THEREFOR - Polymorphic forms of the hydrochloride salt of 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide (referred to herein as Compound 1) which has the formula: | 10-29-2009 |
| 20090270393 | Iminopyridine Derivatives and Use Thereof - The present invention aims to provide an iminopyridine derivative compound having an α | 10-29-2009 |
| 20090270361 | Substituted pyrazole derivatives and use thereof - The present invention aims to provide a novel pyrazole derivative and a pharmaceutical agent containing the same. The present invention provides a compound represented by the formula (I′) | 10-29-2009 |
| 20090270359 | SUBSTITUTED PYRAZOLE DERIVATIVES - The present invention provides a novel pyrazole derivative and an androgen receptor antagonist containing the derivative. The present invention provides a compound represented by the formula (I′) | 10-29-2009 |
| 20090270326 | Cell Death Inhibitor - The present invention relates to an antioxidant response element (ARE) activator comprising a macrophage migration inhibitory factor (MIF) or a modified form thereof, an ARE activator comprising a combination of MIF or a modified form thereof and a substance capable of binding to MIF, and so on. These ARE activators are useful as safe and excellent cell death inhibitors, such as agents for the prevention/treatment of cardiovascular diseases, bone/joint diseases, infectious diseases, inflammatory diseases, renal diseases, central nervous system diseases, cancer or diabetes. | 10-29-2009 |
| 20090258893 | FUSED QUINOLINE DERIVATIVE AND USE THEREOF - The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) | 10-15-2009 |
| 20090253789 | Preventive/Remedy for Arteriosclerotic Disease and Method of Evaluating Therapeutic Procedure - There is provided an evaluation method of effect of a remedy or a therapeutic procedure for atherosclerosis directly or indirectly acting on a substance having a nature of exacerbating atherosclerosis (particularly, a protein) and being present in an atherosclerotic lesion to improve the atherosclerotic lesion, which comprises performing an evaluation by, regarding respective atherosclerotic lesion samples of a mammal origin collected from an administration- or application-group of the remedy or therapeutic procedure, and from a non-administration- or non-application-group, comparing a value of one group corresponding to strength of an atherosclerosis-exacerbating activity of the substance (for example, a pharmacological activity such as an enzyme activity) present in the sample and corrected by an amount of a correction marker in the atherosclerotic lesion, with that of the other group, said amount of the correction maker varying correlating with an amount of the substance in the atherosclerotic lesion and being not influenced by the remedy or therapeutic procedure to be evaluated. | 10-08-2009 |
| 20090253725 | ACETYL CoA CARBOXYLASE INHIBITORS - The present invention relates to acetyl coenzyme-A carboxylase (“ACC”) inhibiting compounds of the formula | 10-08-2009 |
| 20090253635 | PEPTIDES AND PEPTIDOMIMETICS HAVING ANTI-PROLIFERATIVE ACTIVITY AND/OR THAT AUGMENT NUCLEIC ACID DAMAGING AGENTS OR TREATMENTS - This invention provides compounds including peptides and peptidomimetics that can be used to treat cell proliferative disorders, such as those associated with benign and malignant tumor cells. While the invention is not limited to any particular mechanism, the compounds of the invention appear to function at least in part by inhibiting G2 cell cycle checkpoint. Thus, invention compounds can be used to inhibit cell growth alone or be used in combination with a nucleic acid damaging treatment to inhibit cell growth. | 10-08-2009 |
| 20090246198 | MAPK/ERK KINASE INHIBITORS AND METHODS OF USE THEREOF - Compounds of the following formula are provided: | 10-01-2009 |
| 20090239839 | RECEPTOR ANTAGONIST - An agent for modulating the function of an RFRP receptor, characterized by containing either a compound represented by the formula (I) | 09-24-2009 |
| 20090232771 | Method of controlling cell functions - The present invention provides methods of screening genes associated with cell regeneration, growth and differentiation and regulators for cell regeneration, growth or differentiation; regulators for cell regeneration, growth or differentiation; and so on. More specifically, the present invention provides methods of screening genes associated with cell regeneration, growth and differentiation, which comprises the step of quantitatively analyzing expression levels of multiple genes collectively in a cell having a regeneration, differentiation or growth capability to thereby identify the genes associated with the regeneration, growth or differentiation of the cell; methods of screening genes associated with cell regeneration, growth and differentiation, which comprises the step of quantitatively analyzing expression levels of multiple genes collectively in a cell having a regeneration, differentiation or growth capability to thereby identify one or more genes that show higher expression levels in the cell or are specific in expression as compared to the other cells; and, the step of contacting at least one candidate substance capable of regulating the functions of the identified genes or their gene products with the cell and comparing changes before and after the contact; and so on. | 09-17-2009 |
| 20090215700 | Metastin derivatives and use thereof - The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotropic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). | 08-27-2009 |
| 20090209510 | Novel Method of Treating Hyperlipidemia - A pharmaceutical composition useful for a prevention and/or treatment of hyperlipidemia, which comprises combining an effective amount of squalene synthase inhibitor and HMG-CoA reductase inhibitor is provided. | 08-20-2009 |
| 20090203717 | FUSED HETEROCYCLIC COMPOUND - The present invention relates to a compound represented by the formula: | 08-13-2009 |
| 20090192090 | PEPTIDES AND PEPTIDOMIMETICS HAVING IMMUNE-MODULATING, ANTI-INFLAMMATORY, AND ANTI-VIRAL ACTIVITY - The invention provides compounds having immune-modulating and/or anti-inflammatory and/or anti-viral activity, wherein compounds of the invention include peptides and peptidomimetics. The invention further provides methods of using immune-modulating and/or anti-inflammatory and/or anti-viral compounds of the invention. In particular, the invention provides methods for treating a disease related to an immune disorder or inflammation or viral infection by administering an amount of a G2-checkpoint-abrogating peptide or peptidomimetic sufficient to inhibit the disease. | 07-30-2009 |
| 20090186946 | Genetically Modified Animal and Use Thereof - The present invention provides a non-human mammal deficient in the expression of the SLC-1 gene, having the characteristics of (1) a lower blood insulin level in glucose tolerance test, (2) increased insulin sensitivity, (3) higher resistance to obesity even on high fat diet, (4) a smaller white fat cell size, and (5) accentuated lipolysis, compared with the corresponding wild-type animal, or a portion of the body thereof. Also provided is an obesity and/or type II diabetes model non-human mammal that is deficient in the expression of the SLC-1 gene, having the characteristics of (1) elevated expression of adiponectin, (2) delayed onset of hyperglycemia, (3) a lower blood glycohemoglobin level, and (4) accentuated energy consumption, compared with the corresponding obesity and/or type II diabetes model non-human mammal wherein the expression of the gene is normal, or a portion of the body thereof. | 07-23-2009 |
| 20090186879 | TRICYCLIC COMPOUNDS AND USE THEREOF - There is provided a compound of the formula (I′): | 07-23-2009 |
| 20090175959 | Controlled Release Solid Preparation - The present invention provides a controlled release solid preparation superior in the stability of an active ingredient, which can exhibit pharmacological effects steadily and rapidly after administration, and shows a sustained pharmacological effect for a prolonged period of time: a controlled release solid preparation containing (1) an antacid, (2) an immediate-release part containing a compound unstable to acid and a basic substance, and (3) a sustained-release part containing a compound unstable to acid and a pH-independent material in combination. | 07-09-2009 |
| 20090170116 | IL-13 Production Inhibitor - The present invention provides a screening method/screening kit for an IL-13 production inhibitor, which comprises using (a) a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1, or its partial peptide, or a salt thereof; and (b) a ligand capable of specifically binding to the protein; an IL-13 production inhibitor which is obtainable by said screening, and the like. The IL-13 production inhibitor which can be obtained by the screening of the present invention is useful as a prophylactic/therapeutic agent for, e.g., respiratory disease, etc. | 07-02-2009 |
| 20090163553 | BENZIMIDAZOLE COMPOUND CRYSTAL - A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent. | 06-25-2009 |
| 20090163508 | AMIDE COMPOUND - An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. | 06-25-2009 |
| 20090163488 | FUSED HETEROCYCLE DERIVATIVES AND USE THEREOF - A compound represented by the formula (I): | 06-25-2009 |
| 20090156646 | PYRIDYLPHENOL COMPOUND AND USE THEREOF - The present invention provides a compound which has metastin receptor antagonist activity and is useful for preventing and treating hormone-dependent cancer, benign prostatomegaly, endometriosis, precocious puberty, uterine myoma or the like. More specifically, the present invention provides a compound, represented by the formula: | 06-18-2009 |
| 20090156642 | 5-Membered heterocyclic compound - The present invention provides 5-membered heterocycle compounds represented by the following general formula (I): | 06-18-2009 |
| 20090155241 | Prophylactic/therapeutic agent for cancer - A compound or its salt that inhibits the activity of a protein having the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1; a compound or its salt that inhibits the expression of a gene for the protein; an antisense polynucleotide comprising a nucleotide sequence complementary or substantially complementary to the nucleotide sequence of a polynucleotide encoding the protein or a partial peptide thereof or a part of the nucleotide sequence; an antibody against the protein; etc. are useful as preventive/therapeutic agents for cancer, apoptosis promoters for cancer cells, or the like. | 06-18-2009 |
| 20090143444 | ACID SECRETION INHIBITOR - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) | 06-04-2009 |
| 20090142399 | DISPERSANT AGENT FOR SUSTAINED-RELEASE PREPARATIONS - The present invention provides a bilayer dispersing agent for a sustained-release preparation, which contains a non water-soluble solvent and an aqueous solvent, and a sustained-release preparation wherein a microcapsule containing a physiologically active substance is dispersed in the aforementioned dispersing agent. When this preparation is subcutaneously administered, the initial release of a physiologically active substance immediately after administration is strikingly suppressed, a constant amount of a physiologically active substance is released for a long period of time from immediately after administration, superior dispersibility is afforded, and the preparation can readily pass through a needle as an injection. | 06-04-2009 |
| 20090142346 | Preventive/Remedy for Cancer - A human monoclonal antibody against a protein comprising the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1 or SEQ ID NO: 3, its partial peptide, or a salt thereof, is useful as an agent for preventing/treating cancer, etc., an apoptosis inducer of cancer cells, a growth inhibitor of cancer cells, a cytotoxic agent against cancer cells through a host defense mechanism mediated by the Fc region of an antibody, and so on. | 06-04-2009 |
| 20090142345 | PROPHYLACTIC/THERAPEUTIC AGENT FOR CANCER - The present invention provides a safe drug that targets a molecule specifically expressed in cancer cells, and that induces cancer cell growth inhibition. More specifically, the present invention provides a neutralizing antibody against a protein comprising the same or substantially the same amino acid sequence as that shown by SEQ ID NO:1, SEQ ID NO:3, SEQ ID NO:5, SEQ ID NO:7 or SEQ ID NO:9, or a partial peptide thereof or a salt thereof, and a prophylactic/therapeutic agent for cancers (for example, breast cancer, ovarian cancer, colorectal cancer, lung cancer, pancreatic cancer) and the like, apoptosis promoter, cancer cell growth suppressant, DDR1 antagonist and the like, comprising the neutralizing antibody. | 06-04-2009 |
| 20090137603 | HETEROCYCLIC AMIDE COMPOUND AND USE THEREOF - The present invention provides a novel amide compound represented by the following formula, which has a matrix metalloproteinase inhibitory activity and is useful as a pharmaceutical agent. | 05-28-2009 |
| 20090137595 | FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF - The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. | 05-28-2009 |
| 20090137580 | Fused Heterocyclic Derivatives and Use Thereof - The present invention provides a fused heterocyclic derivative showing a potent kinase inhibitory activity and use thereof. A compound represented by the formula: | 05-28-2009 |
| 20090124595 | MAPK/ERK KINASE INHIBITORS - Compounds of the following formula are provided for use with MEK: | 05-14-2009 |
