Abstract: Preparations for transferring efficiently oligonucleotides necessary in antisense therapy or the like into animal cells so as to be useful in treatment for various diseases, which comprises a collagen as an essential component are provided.
Abstract: The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula (I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof: wherein A is a group represented by Formula (a) or the like: (wherein either R4 or R5 represents cyano, nitro or the like, and the other represents a hydrogen atom or the like); either R1 or R2 represents a group: -D-(X)m-R6 or the like, and the other represents a group: -E-(Y)n-R7, hydrogen atom, aryl or the like; R3 is a hydrogen atom or the like; D and E independently represent aryl; X and Y independently represent O or the like; R6 and R7 independently represent alkyl, aryl, arylalkyl or the like; and m and n are independently 0 or 1, provided that the aryl is optionally substituted.
Abstract: An aryl-substituted alicyclic compound of the formula (I): wherein U is 1,4,5,6-tetrahydropyrimidin-2-yl, etc., A is phenylene, etc., B is piperidine-1,4-diyl, etc., Z is —CONH—, etc., R3 is hydrogen, etc., R5 is hydrogen, aryl, etc., R6 is a mono-substituted amino (e,g., benzyloxycarbonylamino), R7 is hydrogen, etc., and a process for preparation thereof, and a pharmaceutical composition containing the same. The compound of the present invention has a high selectivity for ?v?3 integrin, and exhibits a potent inhibitory activity thereto, and hence, it is useful as a preventive or/and a therapeutic agent for a disease in which ?v?3 integrin is involved.
Abstract: Disclosed are a process for preparation of an optically active 7-substituted 3-(2-aminopropyl)indole compound and an intermediate therefor. In the above preparation process, 7-substituted indole is reacted with L- or DL-serine in the presence of a tryptophan-synthesizing enzyme originating in microorganisms to form corresponding 7-substituted L-tryptophan, and it is subjected, if necessary, to reduction, protection, exchange and elimination.
Abstract: The present invention provides a novel protein that regulates degranulation of mast cells (degranulation regulator), a gene encoding it, a protein (conjugate factor) that interacts with the regulator, a gene encoding it, a screening method of an inhibitor of the degranulation, which uses this degranulation regulator and the conjugate factor, an inhibitor obtained by the screening method and the like.
Abstract: N-Arylphenylacetamide derivatives represented by the following formula [I]: (wherein R1 is C1-6 alkoxy, etc.; R2 is hydrogen, —(CH2)m—N(R6)(R7) (m is an integer of from 1 to 4; R6 is hydrogen, C1-4 alkyl, etc., R7 is hydrogen, etc.), etc.; R3 is hydrogen, halogen, etc.; R4 is C6-10 alkyl, —Y—R8 (Y is a single bond, C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, etc., R8 is aryl, C3-8 cycloalkyl, C6-15 polycycloalkyl, etc.), etc.; R5 is hydrogen, etc.; and X1 is hydrogen), or pharmaceutically acceptable salts thereof or hydrates or solvates of the same, and a pharmaceutical composition containing the same. These compounds are useful as preventives and/or remedies giving no pain at the early stage of administration, which are efficacious in oral administration and have potent analgesic and antiinflammatory effects.
Abstract: Heterocyclic compounds represented by the general formula (I) and having elastase inhibiting activity; and intermediates for the synthesis thereof: (I) wherein R1 is a heterocyclic group represented by the general formula (II): (II) [wherein A represents the presence or absence of a benzene ring; X is oxygen, sulfur or NH; and Y is nitrogen or CH], and the heterocyclic group may be substituted with one to three substituents which may be the same or different and are selected from the group consisting of lower alkyl, lower alkoxy, and phenyl which may be substituted with optionally halogenated lower alkyl, lower alkoxy or halogeno; and R2 and R3 are each hydrogen or hydroxyl, or R2 and R3 may be united to form an oxo group, with the proviso that both are not hydrogen.
Abstract: An object of the present invention is to provide a graph display processing device and method that facilitates easy viewing of data with periodicity. With each recognition of a cardiac cycle, a CPU of an electrocardiogram display device (100) finds a point between an R-wave and an S-wave in the cardiac cycle and at two-thirds from the lowest point, as a central point of the cardiocyclic waveform. The CPU determines whether or not the central point is displayed in a central region defined as one-third of the center of a display. When the central point is not in the central region, the CPU performs a scroll process on the electrocardiogram.
Abstract: The present invention provides a composition containing a substance being capable of supplying aldehyde-like substances to be used in the field of medicaments, cosmetics, hair care products, etc., that contains a low-molecular weight active substance the stability of which is impaired by the effects of aldehydes and a stabilizer having an amine structure and being capable of absorbing aldehydes, and has an improved stability to aldehyde of said low-molecular weight active the stability of which is impaired by the effects of aldehydes substance; and a method for stabilizing such a low-molecular weight active substance. An example of said stabilizer is an aminosugar or a polymer thereof, an aminosugar alcohol or a polymer thereof, an amino acid or a polymer thereof, a protein or a hydrolysate thereof, an alkylamine, a hydroxyalkylamine, or a salt thereof.
October 21, 2003
December 1, 2005
DAINIPPON PHARMACEUTICAL CO. LTD., TAKEDA PHARMACEUTICAL COMPANY LIMITED
Abstract: A spiro compound represented by the following formula (I) wherein R1 and R2 are the same or different and each is a hydrogen atom, a chlorine atom and the like, n is 1, 2 or 3, a bond containing a broken line is a single bond or a double bond, A is —X—(CH2)q—N(R3)(R4); a group represented by the following formula (a) and the like, wherein X is an oxygen atom or a sulfur atom, q is 2 or 3, R3 and R4 are the same or different and each is a C1-6 alkyl group and the like, or R3 and R4 optionally form, together with the adjacent nitrogen atom, a piperidine ring and the like optionally substituted by one or two C1-6 alkyl and the like, R5 is a C1-6 alkyl group and the like, R6 is a hydrogen atom and the like, and r and t are each independently one or two, or a pharmaceutically acceptable acid addition salt thereof.
Abstract: Medicines for treatment or prevention of dementia comprising 2-aryl-8-oxodihydropurine derivatives of the formula (I): wherein W is H, C1-6 alkyl, halogen, C1-6 alkoxy, or the like; X is H, C1-6 alkyl, a group of the formula (Q): —CH(R3)CON(R1) (R2) (wherein R1 is a C1-6 alkyl or the like; R2 is phenyl-substituted C1-4 alkyl or the like; and R3 is H or the like); Y is H, C1-6 alkyl, a group of the above formula (Q), or the like; and A is substituted phenyl or the like, with the proviso that one of X and Y is a group of the formula (Q) and the other is a group selected from those defined for X or Y except the groups (Q), or pharmaceutically acceptable acid addition salts thereof. The above compounds exhibit an extremely potent ameliorating effect on learning disorder and/or dymnesia and thus are useful in the treatment or prevention of Alzheimer-type dementia, cerebrovascular dementia, senile dementia, etc.
Abstract: The present invention provides a method of determining toxicity to the heart of an anthracycline-type anticancer chemotherapeutic agent such as adriamycin etc., which comprises detecting human H-FABP (Human Heart-type Fatty Acid-Binding Protein) in the blood separated from human, a reagent therefor, a kit therefor and the like.
Abstract: Plant fiber powder is mixed with plant binder powder, which is a mixture of starch powder and gummy matter powder. The mixture of the plant fiber powder and the plant binder powder is mixed with water to produce plant fiber molding material. The plant fiber molding material is molded.
Abstract: A process for the preparation of crystals of zonisamide containing residual 1,2-dichloroethane of not more than 5 ppm, by adding an aqueous C2-4 alcohol to crystals of zonisamide containing residual 1,2-dichloroethane of more than 5 ppm, removing the 1,2-dichloroethane by azeotropic distillation, followed by collecting the precipitated crystals from the residual mixture.
Abstract: Novel pyrrolidine derivatives, being useful as chymase inhibitor or intermediate for synthesis of the active compounds, which has the formula (I): wherein R1 is cycloalkyl, substituted or unsubstituted phenyl or naphthyl, indanyl, thienyl, furyl, substituted or unsubstituted indolyl, benzofuryl, substituted or unsubstituted benzothienyl, etc.; R2 is H, alkyl, phenyl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; R3 is (i) substituted or unsubstituted monocyclic heterocyclic group, (ii) substituted or unsubstituted benzene- or pyridine-fused heterocyclic group, or (iii) a group (a): R4 and R5 are independently H or OH, but R4 and R5 are not simultaneously H, or both form oxo; n is 0, 1, 2 or 3; or a salt thereof.
August 21, 2001
Date of Patent:
February 8, 2005
Dainippon Pharmaceutical Co., Ltd.
Takashi Deguchi, Ryotaro Shiratake, Fuminori Sato, Buichi Fujitani, Yayoi Honda, Akihiko Kiyoshi, Mitsue Notake, Graham Andrew Showell, Robert George Boyle, Sukhbinder Singh Klair
Abstract: The present invention relates to a heterocyclic compound of the following formula (I-a), its ester, or a salt thereof, and a human neutrophilic elastase inhibitor containing the same as the active ingredient, etc.
wherein A and B are the same or different and each is a lower alkylene group being optionally substituted by an oxo group, D is a heteromonocyclic or heterobicyclic group being optionally substituted by an oxo group, R1 and R2 are the same or different and each is a lower alkyl group, R3 and R4 are different from each other, and each is a hydrogen atom or a hydroxy group, or both combine together to form an oxo group, and R5 is 2-benzoxazolyl, trifluoromethyl, benzylamino-carbonyl, etc.
Abstract: Medicines for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease and schizophrenia of mammals (including human beings) through the retardation or inhibition of neurodegeneration due to hypofunction of glutamic acid receptor and which contain as an active ingredient 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivatives of the formula (I):
wherein Het is oxadiazolyl; R1 is hydrogen, lower alkyl, cyclo-lower alkyl, lower alkenyl, lower alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, etc.; and R2 is hydrogen, lower alkyl, cyclo-lower alkyl, substituted or unsubstituted aryl, etc., or physiologically acceptable acid addition salts thereof.
Abstract: (S)-4-Amino-5-chloro-2-methoxy-N-[1-[1-(2-tetrahydrofuryl-carbonyl) -4-piperidinylmethyl]-4-piperidinyl]benzamide of the following formula (I):
or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, and a process for preparing the same, a pharmaceutical composition containing the same, and intermediate therefor.
The compound of the present invention is useful as a gastrointestinal motility enhancer or a gastrointestinal prokinetic agent, which shows a potent affinity for 5-HT4 receptor, and shows few effects on the heart, and further shows few side effects on the central nervous system based on the dopamine D2 receptor.
Abstract: The present invention provides a process for industrially producing (aminomethyl)trifluoromethylcarbinol derivatives, in particularly, optically active compounds thereof, which are useful as starting compounds for drugs such as protease inhibitors, etc.
Abstract: A [5-chloro-6-phenyl-2-(4-trifluoromethylphenyl)-4-pyrimidinyl-amino]acetamide derivative of the formula (I):
wherein R1 is a methyl group or a cyclopropyl group, and a pharmaceutical composition containing the same. Said compounds exhibit a potent anti-rheumatoid activity and show low toxicity, and hence, they are useful as an agent for prophylaxis or treatment of immuno inflammatory diseases such as rheumatoid diseases (e.g., rheumatoid arthritis, Behcet disease, ankylosing spondylitis, etc.) and autoimmune diseases (e.g., multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, etc.).
May 13, 2002
Date of Patent:
September 16, 2003
Dainippon Pharmaceutical Co., Ltd.
Teruya Murata, Kazunori Ohno, Masayasu Tanaka, Mari Itoh