Patents Assigned to Dainippon Pharmaceutical Co., Ltd.
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Patent number: 6458824Abstract: The present invention provides a solid preparation comprising a crystal of [3-[(2R)-[[(2R)-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1H-indol-7-yloxy]acetic acid (Compound A), especially a crystal of Compound A having a particle size of not larger than 100 &mgr;m at the cumulative weight distribution value of 50%, and not larger than 200 &mgr;m at the cumulative weight distribution value of 95%, preferably a solid preparation having the excellent stability and the content uniformity of Compound A, which is prepared by preparing granules of the crystal of Compound A with fillers, disintegrants and binders, and then followed by mixing said granules with external excipients.Type: GrantFiled: September 14, 2000Date of Patent: October 1, 2002Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Motokazu Iwata, Teruaki Kuriyama, Megumi Fujita, Keiichi Fujiwara, Shiro Kato, Hiroshi Harada, Akihito Fujii, Osamu Odai, Hitoshi Kawashima
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Patent number: 6413541Abstract: Method for producing intrabuccally disintegrating tablets, which comprises the following Steps (a), (b) and (c), wherein a medicament is mixed before granulation or tabletting: (a) a step of dissolving at least one saccharide having a high solubility in water and at least one water-soluble binder in water alone or in water and an alcohol; (b) a step of mixing the solution obtained in above Step (a) with at least one excipient, granulating, drying, and tabletting the mixture under a low compression pressure; (c) a step of aging the tablets obtained in Step (b), and intrabuccally disintegrating tablets produced by the above method are provided. The method of the present invention is a simple method for producing intrabuccally disintegrating tablets in large scale without using specific facility, and by which intrabuccally disintegrating tablets showing good disintegrating property in oral cavity as well as having sufficient strength can be obtained.Type: GrantFiled: July 11, 2000Date of Patent: July 2, 2002Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Yoshimi Shirai, Kiyomi Sogo, Kazuyoshi Ogasawara, Yutaka Higashi, Yasuhiko Nakamura
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Patent number: 6372740Abstract: 2-Aryl-8-oxodihydropurine derivative of the following formula (I): wherein W is H, lower alkyl, halogen, lower alkoxy, amino, mono- or di-lower alkylamino, or substituted or unsubstituted phenyl; X is H, lower alkyl, cycloalkyl-lower alkyl, substituted or unsubstituted phenyl-lower alkyl, lower alkenyl, carbamoyl, di-lower alkylcarbamoyl, or a group of the formula (Q): —CH(R3)CON(R1)(R2); Y is H, lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, lower alkenyl, substituted or unsubstituted phenyl-lower alkyl, or a group of the formula (Q): —CH(R3)CON(R1)(R2); A is substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; provided that when one of X and Y of the above formula (I) is the group of the formula (Q), then the other is the same groups for X or Y as described above except for the group of the formula (Q), or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: June 1, 2000Date of Patent: April 16, 2002Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Teruya Murata, Kaoru Masumoto, Katsunori Kondo, Kiyoshi Furukawa, Makoto Oka
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Patent number: 6342515Abstract: The present invention provides a medicament for neurodegenerative diseases comprising zonisamide or an alkali metal salt thereof as an active ingredient. The present medicament can be used in the prevention and treatment of neurodegenerative diseases such as Parkinson's disease, Huntington's disease, choreic syndrome and dystonic syndrome in mammals (including human).Type: GrantFiled: June 26, 2000Date of Patent: January 29, 2002Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Yoshinobu Masuda, Yoshiaki Ochi
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Patent number: 6297244Abstract: A stabilized pharmaceutical composition comprising (R)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3′-pyrrolidine-1,2′,3,5′-tetrone (hereinafter, referred to as “AS-3201”) and as a stabilizer at least one acidic substance having an acidity more potent than that of AS-3201, such as ascorbic acid, citric acid, tartaric acid, lactic acid, maleic acid, malic acid or phosphoric acid.Type: GrantFiled: April 19, 2000Date of Patent: October 2, 2001Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Mamoru Ohashi, Kazuyoshi Ogasawara, Yoshimi Shirai, Hiroshi Fujioka
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Patent number: 6294555Abstract: Compound of the formula (I): wherein Ar is a group of the following formula (Ar-1) or (Ar-2): A is a group of the formula: —Z—N(Q1)(Q2), —CO—R7 or —(CH2)p—CH(R8)—COR9, or a pharmaceutically acceptable acid addition salt thereof, a process for preparing the same, a pharmaceutical composition containing the same, and intermediates therefor. The compounds of the present invention show a potent affinity for 5-HT4 receptors, and they are useful as a gastrointestinal motility enhancer or a gastrointestinal prokinetic agent.Type: GrantFiled: October 27, 2000Date of Patent: September 25, 2001Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Shiro Kato, Yoshihito Toyotomi, Hirotake Tateishi, Hiroshi Harada, Naoyuki Yoshida, Kazuo Morikage, Yukiko Morikage
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Patent number: 6277993Abstract: A 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivative of the formula (I): wherein Het is oxadiazolyl, R1 is H, lower alkyl, cyclo-lower alkyl, trifluoromethyl, lower alkenyl, lower alkynyl, lower alkoxy, lower alkoxy-lower alkyl, hydroxy-lower alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaromatic group, and R2 is H, lower alkyl, cyclo-lower alkyl, cyclo-lower alkylmethyl, lower alkenyl, cyclo-lower alkenyl, lower alkynyl, substituted or unsubstituted aryl, or substituted or unsubstituted hetero-aromatic group, or a pharmaceutically acceptable acid addition salt thereof, which has high selective affinity to benzodiazepine receptor and is useful particularly as a benzodiazepine inverse agonist, for example, as psychoanaleptic drug or a drug for the treatment of dysmnesia in senile dementia or Alzheimer's disease.Type: GrantFiled: September 1, 2000Date of Patent: August 21, 2001Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Kazunori Ohno, Osamu Odai, Kaoru Masumoto, Kiyoshi Furukawa, Makoto Oka
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Patent number: 6245354Abstract: The present invention relates to a pharmaceutical sustained release preparation prepared by using as a sustained release ingredient a partial degradation product of the galactose of a galactoxyloglucan and a method for sustained releasing of a drug thereby. In more detail, it relates to a pharmaceutical sustained release preparation, wherein the sustained release of a drug is effected by utilizing the thermally reversible gel characteristics of the galactose-partial degradation product, which is produced by partial removal of the galactose on the side-chain of a galactoxyloglucan with an enzyme.Type: GrantFiled: August 12, 1998Date of Patent: June 12, 2001Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Shozo Miyazaki, Mayumi Shirakawa, Kazuhiko Yamatoya
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Patent number: 6172079Abstract: A 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivative of the formula (I): wherein Het is oxadiazolyl, R1 is H, lower alkyl, cyclo-lower alkyl, trifluoromethyl, lower alkenyl, lower alkynyl, lower alkoxy, lower alkoxy-lower alkyl, hydroxy-lower alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaromatic group, and R2 is H, lower alkyl, cyclo-lower alkyl, cyclo-lower alkylmethyl, lower alkenyl, cyclo-lower alkenyl, lower alkynyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaromatic group, or a pharmaceutically acceptable acid addition salt thereof, which has high selective affinity to benzodiazepine receptor and is useful particularly as a benzodiazepine inverse agonist, for example, as psychoanaleptic drug or a drug for the treatment of dysmnesia in senile dementia or Alzheimer's disease.Type: GrantFiled: January 10, 2000Date of Patent: January 9, 2001Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Kazunori Ohno, Osamu Odai, Kaoru Masumoto, Kiyoshi Furukawa, Makoto Oka
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Patent number: 6017911Abstract: This invention relates to pyridonecarboxylic acid derivatives of the following general formula, esters thereof and salts thereof, as well as pharmaceutical preparations containing them. ##STR1## wherein: R is cycloalkyl which may be substituted by halogen, or the like;X is hydrogen, lower alkyl, amino or the like;Y is hydrogen or halogen;A is nitrogen or a group of the formula C--Z in which Z is lower alkoxy that may be substituted by halogen, or the like;R.sub.1 and R.sub.2 may be the same or different and are each hydrogen or the like;R.sub.3 is hydrogen or lower alkyl;R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 may be the same or different and are each hydrogen, halogen or lower alkyl;m is 0 or 1; andn and p may be the same or different and are each 0 or 1.This invention also relates to bicyclic amine compounds useful as direct intermediates for the synthesis of the above-described pyridonecarboxylic acid derivatives.Type: GrantFiled: August 25, 1998Date of Patent: January 25, 2000Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Nobuhiko Horiuchi, Takenori Yonezawa, Katsumi Chiba, Hiroaki Yoshida
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Patent number: 5990106Abstract: This invention relates to bicyclic amino group-substituted pyridonecarboxylic acid derivatives of the general formulaA--Priesters thereof and salts thereof, wherein: Pri is a pyridonecarboxylic acid residue, and A is a bicyclic amino group represented by the following formula and joined to the 7-position of the pyridonecarboxylic acid or a position equivalent to the 7-position thereof. ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represents a hydrogen atom, a lower alkyl group or an amino-protecting group; R.sub.3 and R.sub.4 may be the same or different and each represents a hydrogen atom, a halogen atom, a cyano group, a hydroxyl group, an oxo group, a lower alkoxy group or a lower alkyl group; and n is an integer of 0 or 1.The above-described pyridonecarboxylic acid derivatives, esters thereof and salts thereof are useful as antibacterial agents.Type: GrantFiled: August 4, 1997Date of Patent: November 23, 1999Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Masato Sakamoto, Katsumi Chiba, Yukio Tominaga, Akira Minami
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Patent number: 5972946Abstract: An acetamide derivative of the formula (I): ##STR1## wherein X is --0-- or --NR.sub.4 --, R.sub.1 is H, lower alkyl, lower alkenyl or cyclolalkyl-lower-alkyl, R.sub.2 is lower alkyl, cycloalkyl, substituted or unsubstituted phenyl, etc., R.sub.3 is H, lower alkyl or hydroxy-lower alkyl, R.sub.4 is H, lower alkyl, etc., R.sub.5 is H, lower alkyl, lower alkenyl, hydroxy-lower alkyl, etc., R.sub.6 is H, lower alkyl, CF.sub.3, substituted or unsubstituted phenyl, or R.sub.5 and R.sub.6 may optionally combine to form --(CH.sub.2)n--, R.sub.7 is H, halogen, lower alkyl, lower alkoxy, CF.sub.3, OH, NH.sub.2, etc., R.sub.8 is H, halogen, lower alkyl or lower alkoxy, or a pharmaceutically acceptable acid addition salt thereof. The compounds of the present invention selectively act on the peripheral-type BZ.omega..sub.Type: GrantFiled: October 14, 1997Date of Patent: October 26, 1999Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Teruya Murata, Katsuhiko Hino, Kiyoshi Furukawa, Makoto Oka, Mari Itoh
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Patent number: 5945415Abstract: This invention discloses a compound which is expressed by formula (I) below: ##STR1## or physiologically acceptable acid addition salts thereof. The claimed compound exhibits excellent antiemetic effect based on its potent serotonin S.sub.3 and dopamine D.sub.2 receptor antagonistic activities, and is useful for treatment or prophylaxis of various gastrointestinal symptoms which are associated with various diseases and drug administration.Type: GrantFiled: January 23, 1998Date of Patent: August 31, 1999Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Shiro Kato, Yoshimi Hirokawa, Toshiya Morie, Hiroshi Harada, Naoyuki Yoshida
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Patent number: 5932781Abstract: The nucleotide sequence of a DNA coding for ectoine synthase has been determined by isolating a gene coding for an enzyme involved in the biosynthesis of ectoine in the form of a DNA comprising about 4.2 kilobase pairs which is obtained from Halomonas sp. KS-3 by cleaving with restriction endonucleases EcoRI and SalI. By introducing the obtained gene DNA into E. coli, it is possible to provide the capability of biosynthetizing ectoine and the characteristic of high osmotic tolerance, thus permitting the development of an efficient fermentation technique utilizing the resultant transformant and the creation of plants having high resistance to drought.Type: GrantFiled: May 9, 1996Date of Patent: August 3, 1999Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Mitsuo Takano, Hisayo Ono, Hiroyuki Yamada, Kazuhiko Yamatoya
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6-methoxy-1H-benzotriazole-5-carboxamide derivatives and pharmaceutical compositions containing them
Patent number: 5932568Abstract: 6-Methoxy-1H-benzotriazole-5-carboxamide derivatives which are represented by the formula (I) below: ##STR1## ?in which R.sup.1 stands for ethyl or cyclopropylmethyl group, R.sup.2 stands for hydrogen atom, methyl or ethyl group,n is 1, 2 or 3, andthe wavy line () signifies that configuration of the substituents on the carbon atom bound to the N-atom in the amide moiety is racemic (RS) or optically active (R or S)!or their pharmaceutically acceptable acid addition salts; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or its pharmaceutically acceptable acid addition salt; and novel intermediates. The compounds of the present invention possess concurrently excellent antiemetic activity and gastrointestinal motility enhancing activity.Type: GrantFiled: May 21, 1997Date of Patent: August 3, 1999Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Shiro Kato, Yoshimi Hirokawa, Hiroshi Yamazaki, Toshiya Morie, Naoyuki Yoshida -
Patent number: 5847159Abstract: 1-?.omega.-(3,4-Dihydro-2-naphthalenyl)alkyl!cyclic amine derivative of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are H, halogen, OH, alkyl, alkoxy, hydroxymethyl, etc., or R.sup.1 and R.sup.2 combine to form methylenedioxy, trimethylene, etc., R.sup.3 is H, etc., R.sup.4 is H, OH, alkyl, etc., R.sup.5 is H, alkyl, etc., p is integer of from 2 to 6, and q is integer of from 3 to 7, provided that when p is 2, and q is 5, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are not simultaneously H, or salts thereof, or N-oxide derivatives thereof, or a process for preparing the same, or pharmaceutical composition containing the same. The compounds of the present invention show potent inhibitory effect on the micturition reflex, and are useful as agents for treatment of frequent urination and urinary incontinence.Type: GrantFiled: October 14, 1997Date of Patent: December 8, 1998Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Naoki Kai, Aki Kanehira, Toshiya Morie, Katsuhiko Hino, Katsuyoshi Kawashima, Isao Shimizu, Kazuhisa Akiyama
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Patent number: 5817669Abstract: This invention relates to pyridone-carboxylic acid derivatives of the following formula or salts thereof: ##STR1## wherein R.sub.1 is a hydrogen atom, a halogen atom, etc.,R.sub.2 is a carboxyl group etc.,R.sub.3 is a hydrogen atom etc.,A is a nitrogen atom or CH,m is 1 or 2, andY is an eliminable group or a group having the following formula: ##STR2## wherein R.sub.4 is a hydrogen atom or a lower alkyl group,Z is a hydrogen atom, a lower alkyl group, etc.,R.sub.5 is a hydrogen atom, a lower alkyl group, etc.,n is 0 or 1, andp is 1, 2, 3 or 4and to processes for the preparation of these compounds, and further to anti-tumor agents which contain the above compounds as effective ingredients.Type: GrantFiled: December 13, 1996Date of Patent: October 6, 1998Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Kyoji Tomita, Katsumi Chiba, Shigeki Kashimoto, Koh-ichiro Shibamori, Yasunori Tsuzuki
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Patent number: 5817689Abstract: An indole derivative of the formula: ##STR1## wherein R.sub.1 is lower alkoxy, lower alkoxycarbonyl-lower alkoxy, carboxy-lower alkoxy, lower alkoxycarbonyl, phenyl-lower alkoxy, lower alkyl being optionally substituted by hydroxy, di-lower alkylaminosulfonyl, etc., R.sub.2 is hydrogen, halogen, lower alkoxy, lower alkoxycarbonyl-lower alkoxy, carboxy-lower alkoxy, etc., R.sub.3 is hydrogen or lower alkyl, R.sub.4 is halogen or trifluoromethyl, R.sub.5 is lower alkyl, or a salt thereof, these compounds being potent .beta..sub.3 -adrenergic receptor-stimulating agent with excellent adrenoceptor selectivity, and being useful in the prophylaxis or treatment of obesity or diabetes mellitus.Type: GrantFiled: May 29, 1997Date of Patent: October 6, 1998Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Shiro Kato, Hiroshi Harada, Yoshimi Hirokawa, Naoyuki Yoshida, Hitoshi Kawashima
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Patent number: 5602111Abstract: An agent for inducing a phytoalexin comprising a xyloglucan-oligosaccharide as an active ingredient thereof and a method for inducing a phytoalexin in a plant body comprising an application of a xyloglucan-oligosaccharide to the plant. The present invention is useful for promoting growth of a plant and maintaining freshness of a plant while a crop has been grown, or a vegetable or a fruit has been transported and/or stored.Type: GrantFiled: November 28, 1994Date of Patent: February 11, 1997Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Akira Misaki, Keiji Sekiya, Kazuhiko Yamatoya
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Patent number: 5527801Abstract: The present invention is to provide an ameliorant for blood lipid metabolism which comprises as an active ingredient N-(6,11-dihydrodibenzo[b,e]thiepin-11-yl)-4-(4-fluorophenyl)-1-piperazineb utanamide or a pharmaceutically acceptable salt thereof, more particularly, to provide a hyperlipidemia inhibitor and an atherosclerosis inhibitor.Type: GrantFiled: March 14, 1994Date of Patent: June 18, 1996Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Yoshinobu Masuda, Hisao Minato, Akihisa Ikeno, Kunihiko Takeyama, Kanoo Hosoki