Nippon Shinyaku Co., LTD Patent applications |
Patent application number | Title | Published |
20160046612 | Heterocyclic Derivative and Pharmaceutical Drug - The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: | 02-18-2016 |
20150266830 | FORM-III CRYSTAL OF 2--N-(METHYLSULFONYL)ACETAMIDE, METHOD FOR PRODUCING THE SAME, AND USE THEREOF - Form-III crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide and a method of producing the crystal are provided. The Form-III crystal exhibits diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2θ when the spectrum is obtained by using Cu Kα radiation: 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees, and 23.5 degrees. The Form-III crystal can be produced by crystallizing the subject compound from an ester solvent or an aromatic hydrocarbon solvent. The crystal may be administered as an active ingredient to a subject for the purpose of treating or preventing certain diseases, disorders, and symptoms, or for promoting angiogenesis or gene therapy. The targeted diseases and disorders include transient ischemic attack, diabetic neuropathy, diabetic gangrene, peripheral circulatory disturbance, connective tissue disease, reocclusion/restenosis after percutaneous transluminal coronary angioplasty, arteriosclerosis, thrombosis, hypertension, pulmonary hypertension, and diabetic nephropathy. | 09-24-2015 |
20150225404 | PYRIDINE DERIVATIVE AND MEDICINE - The main purpose of the invention is to provide a novel pyridine derivative or a pharmaceutically acceptable salt thereof. Examples of the invention include a pyridine derivative represented by general formula [1], and a pharmaceutically acceptable salt thereof. This compound or a pharmaceutically acceptable salt thereof exhibits mGluR5 inhibitory activity, and can therefore be used as an agent for the prevention or treatment of, e.g., pain (for example, acute pain, chronic pain, inflammatory pain, neuropathic pain, hyperalgesia, thermal hyperalgesia, allodynia, pain due to noxious thermal stimulation, pain due to noxious mechanical stimulation, pain in the lower urinary tract or reproductive organs, or migraine), pruritus, lower urinary tract symptoms or lower urinary tract dysfunctions, gastroesophageal reflux disease (GERD), gastroesophageal reflux associated with transient lower esophageal sphincter relaxation (TLESR), and diseases of the central nervous system. | 08-13-2015 |
20150152095 | AROMATIC HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL - The main purpose of the invention is to provide a novel aromatic heterocyclic derivative or a pharmaceutically acceptable salt thereof. Examples of the invention include aromatic heterocyclic derivatives represented by general formula [1] and pharmaceutically acceptable salts thereof. | 06-04-2015 |
20140343266 | ANTISENSE NUCLEIC ACIDS - The present invention provides a pharmaceutical agent which causes skipping of the 55th, 45th, 50th or 44th exon in the human dystrophin gene with a high efficiency. | 11-20-2014 |
20140221397 | FIBROSIS INHIBITOR - [Object] The main object of the present invention is to provide a fibrosis inhibitor. | 08-07-2014 |
20140221339 | Heterocyclic Derivative and Pharmaceutical Drug - The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: | 08-07-2014 |
20140155414 | CRYSTALS OF 2- {4- [N- (5,6-DIPHENYLPYRAZIN-2-YL) -N-ISOPROPYLAMINO]BUTYLOXY}-N- (METHYLSULFONYL) ACETAMIDE - A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (hereinafter referred to as “compound A”). A Form-I crystal of compound A shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder X-ray diffraction spectrum thereof. A Form-II crystal of compound A shows diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the powder X-ray diffraction spectrum thereof. A Form-III crystal of compound A shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the powder X-ray diffraction spectrum thereof. | 06-05-2014 |
20140148469 | USE OF FORM-I CRYSTAL OF 2--N-(METHYLSULFONYL)ACETAMIDE - A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (hereinafter referred to as “compound A”). A Form-I crystal of compound A shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder X-ray diffraction spectrum thereof. A Form-II crystal of compound A shows diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the powder X-ray diffraction spectrum thereof. A Form-III crystal of compound A shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the powder X-ray diffraction spectrum thereof. | 05-29-2014 |
20130225613 | QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R | 08-29-2013 |
20130225548 | Pyridine Derivative and Medicinal Agent - A main object of the present invention is to provide a novel pyridine derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof. | 08-29-2013 |
20130211062 | ANTISENSE NUCLEIC ACIDS - The present invention provides a pharmaceutical composition which causes skipping of the 53rd exon in the human dystrophin gene with a high efficiency. | 08-15-2013 |
20130197220 | Morpholino Nucleic Acid Derivatives - The present invention provides a useful morpholino nucleic acid derivative for synthesizing a morpholino nucleic acid oligomer. The present invention provides a compound represented by the following general formula (1) or a salt thereof. | 08-01-2013 |
20130131082 | Aminopyrazine Derivative and Medicine - The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutically acceptable salt of the compound. | 05-23-2013 |
20120322993 | Phosphorylation Reagent - Disclosed are a novel phosphorylating reagent and related methods. Specifically disclosed is a compound represented by general formula (A). | 12-20-2012 |
20120101276 | CRYSTALS - A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (hereinafter referred to as “compound A”). A Form-I crystal of compound A shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder X-ray diffraction spectrum thereof. A Form-II crystal of compound A shows diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the powder X-ray diffraction spectrum thereof. A Form-III crystal of compound A shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the powder X-ray diffraction spectrum thereof. | 04-26-2012 |
20110288065 | AMINOPYRAZINE DERIVATIVE AND MEDICINE - The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. | 11-24-2011 |
20110105518 | THERAPEUTIC AGENT FOR SPINAL CANAL STENOSIS - The main object of the present invention is to provide a novel agent for the treatment of spinal canal stenosis. | 05-05-2011 |
20110098344 | DRUG CARRIER - A drug carrier characterized by mainly containing a polyethylene-glycol-modified phospholipid and a cationic lipid and containing the polyethylene-glycol-modified phospholipid in a concentration within a specific range. The drug carrier, which is of the in-blood residence type, is characterized by comprising a polyethylene-glycol-modified phospholipid represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: | 04-28-2011 |
20110015211 | FIBROSIS INHIBITOR - [Object] The main object of the present invention is to provide a fibrosis inhibitor. | 01-20-2011 |
20100233262 | COATED TABLET - A main object of the present invention is to provide a novel coated tablet which contains a drug having a guanidino group and does not suffer an obvious color change even when packed in a one-dose pack together with a drug having a (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (DMDO) group. The present invention provides a coated tablet characterized in that an uncoated tablet containing a drug having a guanidino group has been coated with a polyvinyl alcohol for film coating which comprises polyvinyl alcohol, acrylic acid, and methyl methacrylate. | 09-16-2010 |
20100130454 | 9,10-SECOPREGNANE DERIVATIVES AND MEDICINE - A novel useful vitamin D3 derivative which is reduced in influence on systemic calcium metabolism while retaining excellent vitamin D3 activity. The derivative is a 9,10-secopregnane derivative represented by the following general formula [1]. Also provided is a medicinal composition containing the derivative as an active ingredient. In the general formula [1], Y represents (1) a single bond, (2) alkylene (3) alkenylene, or (4) phenylene; R | 05-27-2010 |
20100074880 | POLYETHYLENE GLYCOL DERIVATIVE - The present invention includes a novel polyethylene glycol derivative; a drug carrier comprising the derivative; and a pharmaceutical composition comprising the drug carrier having a pharmacologically active substance included therein. Specifically disclosed are: a polyethylene glycol derivative represented by the general formula (I); a drug carrier comprising the derivative and 2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoyl-glycerol; and a pharmaceutical composition comprising the drug carrier and a pharmacologically active substance (preferably double-stranded RNA, double-stranded DNA or an oligonucleic acid), wherein R represents a saturated or unsaturated aliphatic hydrocarbon group having 10 to 30 carbon atoms or a saturated or unsaturated fatty acid residue having 10 to 30 carbon atoms; and n represents an integer of 30 to 150. | 03-25-2010 |
20100048537 | HETEROARYL DERIVATIVES - The present invention relates to a compound represented by formula [1] or a pharmaceutically acceptable salt thereof: | 02-25-2010 |
20100022566 | QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R | 01-28-2010 |
20100016263 | 9, 10-SECOPREGNANE DERIVATIVE AND PHARMACEUTICAL - A main object of the invention is to provide a novel useful vitamin D | 01-21-2010 |
20090312534 | METHOD FOR REMOVAL OF NUCLEIC ACID-PROTECTING GROUP - A method is provided for efficiently removing the silicon substituent which protects the 3′-hydroxyl group and the 5′-hydroxyl group of a ribose of a ribonucleic acid derivative in which the 2′-hydroxyl group of the ribose is protected with the following substituent (I) | 12-17-2009 |
20090292005 | GALACTOSE DERIVATIVE, DRUG CARRIER AND MEDICINAL COMPOSITION - The object of the present invention is to provide a novel and useful galactose derivative, which is a component of a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the drug carrier and a medicine. | 11-26-2009 |
20090286970 | METHOD FOR INTRODUCING A NUCLEIC-ACID PROTECTING GROUP - The present invention relates to a simple, economical method for introducing substituent (I) at the 2′-hydroxyl group of the ribose of a ribonucleic acid derivative whose 3′-hydroxyl group and 5′-hydroxyl group are protected with a silicon protecting group, wherein WG | 11-19-2009 |
20090149645 | METHOD FOR DETACHING PROTECTING GROUP ON NUCLEIC ACID - A method is provided for removing a 2-cyanoethoxymethyl (CEM) group and substituting the 2′-hydroxyl group of each ribose of an oligonucleic acid derivative with good reproducibility and high efficiency. | 06-11-2009 |
20090137790 | METHOD OF CAPPING OLIGONUCLEIC ACID - The present invention relates to a method for producing an oligonucleic acid derivative characterized by using a phenoxyacetic acid derivative anhydride as an acylating agent and a pyridine derivative as the acylation reaction activator, in a capping step for protecting the 5′-hydroxyl group of a ribose of an oligonucleic acid derivative. | 05-28-2009 |
20090123532 | OLIGONUCLEIC ACID-BEARING COMPOSITE AND PHARMACEUTICAL COMPOSITION CONTAINING THE COMPOSITE - The present invention provides a complex, which comprises a cationic liposome comprising 2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoylglycerol and a phospholipid as main ingredients, and an oligo nucleic acid which is carried on the liposome. Also, the present invention provides a pharmaceutical composition containing the complex to be used for treating or preventing diseases caused by a target molecule of the oligo nucleic acid (target DNA, target RNA, target protein) since it is possible to administer the complex in vivo and to put the complex into practical use as a medicament because the complex can exhibit pharmacological efficacy in vivo. | 05-14-2009 |
20090069260 | METHOD FOR PRODUCING A NUCLEIC-ACID-CONTAINING COMPLEX PREPARATION - The present invention relates to a method of preparing a nucleic-acid-containing complex formulation which can be sterilized by filtration and administered intravenously to a human, and can retain stability of polynucleotides included in the nucleic-acid-containing complex formulation. The invention also relates to a method of preparing a nucleic-acid-containing complex formulation, comprising the following steps: mixing a solution comprising two separate single-stranded polynucleotides (for example, poly I and poly C) capable of forming a double strand and a solution comprising a cationic carrier or the ingredients thereof to form the cationic carrier, and performing a dispersion treatment on the mixture. | 03-12-2009 |
20090042879 | PHTHALAZINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME - The present invention provides a novel compound having an excellent PDE4 inhibitory activity and TNF-α production-suppressing activity, and also provides a preventive and therapeutic agent for atopic dermatitis or the like. The present invention includes a novel phthalazinone derivative of the following general structural formula [1] or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising it as an active ingredient. | 02-12-2009 |
20080299192 | Intraorally Rapidly Disintergrating Tablets and Their Production - The object of the present invention is to provide, as a solid preparation for making it easy to take, thus improving patient's compliance etc., an intraorally rapidly disintegrating tablet which can be produced easily without any particular problem by a usual method of producing tablets with a usual tabletting machine, has practically unproblematic hardness, and disintegrate rapidly in the oral cavity. This tablet is produced by tabletting cores coated with a pharmaceutical disintegrating agent, wherein the core is a granule containing a water-soluble medicament or containing a medicament and a sugar. | 12-04-2008 |