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1. 发明申请

WO2005000307A1 OPHTHALMIC COMPOSITION CONTAINING QUINOLONES AND METHOD OF USE 审中-公开
标题翻译：含有喹啉酮的眼用组合物及其使用方法
公开(公告)号：WO2005000307A1
公开(公告)日：2005-01-06
申请号：PCT/US2004/020448
申请日：2004-06-25
申请人： SANTEN PHARMACEUTICAL CO., LTD. , DAIICHI PHARMACEUTICAL CO., LTD. , LASKAR, Paul, A. , HICKOK, Shawn, D.
发明人： LASKAR, Paul, A. , HICKOK, Shawn, D.
IPC分类号： A61K31/44
CPC分类号： A61K31/44
摘要： A preservative-free opthalmic composition for treating eye infections is disclosed. The composition contains a quinolone compound in an amount effective as an antibiotic when the composition is placed in the eye. The composition is rendered isoosmotic with polyhydric alcohol. The composition may be utilized to treat ophthalmic conditions by topically applying the composition to the affected tissues.
摘要翻译：公开了一种用于治疗眼部感染的无防腐剂的眼用组合物。当组合物放置在眼睛中时，组合物含有有效量的喹诺酮化合物作为抗生素。将该组合物与多元醇等渗。该组合物可用于通过将组合物局部施用于受影响的组织来治疗眼科病症。

2. 发明申请

WO1998026803A1 PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION 审中-公开
标题翻译：用于口服管理的药物组合物
公开(公告)号：WO1998026803A1
公开(公告)日：1998-06-25
申请号：PCT/JP1997004650
申请日：1997-12-17
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKAHASHI, Masayuki , MORITA, Hiromi , KIKUCHI, Hiroshi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： A61K47/40
CPC分类号： A61K9/4858 , A61K47/14 , A61K47/40
摘要： A pharmaceutical composition for oral administration, comprising a basic medicine and a lipophilic material and/or a cyclodextrin compound. This composition can improve peroral absorption of a basic medicine which is less likely to be absorbed by oral administration.
摘要翻译：一种用于口服给药的药物组合物，其包含碱性药物和亲脂性物质和/或环糊精化合物。该组合物可以改善不太可能被口服给药的基础药物的口服吸收。

3. 发明申请

WO1998024781A1 SUBSTITUTED AMINOMETHYLPYRROLIDINE DERIVATIVES 审中-公开
标题翻译：取代的氨基甲基吡咯烷衍生物
公开(公告)号：WO1998024781A1
公开(公告)日：1998-06-11
申请号：PCT/JP1996003552
申请日：1996-12-04
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , KAWAKAMI, Katsuhiro , SUGITA, Kazuyuki , OHKI, Hitoshi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： Antibacterial drugs excellent in antibacterial activity and safety, comprising quinolone derivatives having various substituents including a substituted aminomethylpyrrolidine and represented by general formula (I) or salts thereof, or hydrates of both. In said formula, Q is (II) or (IV).
摘要翻译：包含抗菌活性和安全性优异的抗菌药物，包括具有各种取代基的喹诺酮衍生物，包括取代的氨基甲基吡咯烷，并且由通式（I）表示的盐或其盐，或两者的水合物。在所述式中，Q为（II）或（IV）。

4. 发明申请

WO1998013370A1 PYRIDOBENZOXAZINE DERIVATIVES 审中-公开
标题翻译：吡咯烷酮衍生物
公开(公告)号：WO1998013370A1
公开(公告)日：1998-04-02
申请号：PCT/JP1997003440
申请日：1997-09-26
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , TAKAHASHI, Hisashi , KAWAKAMI, Katsuhiro
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D498/06
CPC分类号： C07D498/06
摘要： Derivatives having potent antibacterial activities on gram-negative and gram-positive bacteria and, at the same time, favorable dynamics in vivo and a high safety; and excellent drugs. Compounds represented by general formula (I) and salts thereof, hydrates thereof, and antibacterial agents containing the same as the active ingredient. In said formula, R represents hydrogen or C1-6 alkyl optionally having substituent(s) selected from the group consisting of hydroxy, halogeno, C1-6 alkylthio and C1-6 alkoxy; R represents hydrogen or amino optionally having one or two substituents selected from the group consisting of formyl, C1-6 alkyl and C2-6 acyl; and R represents hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, etoxycarbonyl, cholin, dimethylaminoethyl, 5-indanyl, phthalidinyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, C1-6 alkyl, C2-7 alkoxymethyl, or phenylalkyl composed of C1-6 alkylene and phenyl.
摘要翻译：衍生物对革兰阴性和革兰氏阳性细菌具有强力的抗菌活性，同时体内有利的动力学和高安全性; 和优良的药物。由通式（I）表示的化合物及其盐，其水合物和含有该活性成分的抗菌剂。在所述式中，R 1表示氢或任选具有选自羟基，卤代C 1-6烷硫基和C 1-6烷氧基的取代基的C 1-6烷基; R 2表示氢或任选具有一个或两个选自甲酰基，C 1-6烷基和C 2-6酰基的取代基的氨基; 并且R 3表示氢，苯基，乙酰氧基甲基，新戊酰氧基甲基，丁氧基羰基，胆碱，二甲基氨基乙基，5-二氢化茚基，邻苯二基苯基，5-烷基-2-氧代-1,3-二氧杂环戊烯-4-基甲基，3-乙酰氧基-2- 氧代丁基，C 1-6烷基，C 2-7烷氧基甲基或由C 1-6亚烷基和苯基组成的苯基烷基。

5. 发明申请

WO1998003202A1 SORBEFACIENTS 审中-公开
公开(公告)号：WO1998003202A1
公开(公告)日：1998-01-29
申请号：PCT/JP1997002500
申请日：1997-07-18
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , NAKAGAMI, Hiroaki , YAMAO, Tadanao , FUJII, Yoshimine
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： A61K47/30
CPC分类号： A61K47/32 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/405 , A61K31/445 , A61K31/4535 , A61K31/454
摘要： Medicinal compositions for improving the absorbability in the digestive tract of drugs poor in the absorbability therein. The compositions contain drugs and anion exchange resins and show excellent absorbability in the digestive tract.
摘要翻译：用于提高消化道吸收能力差的药物吸收性的药用组合物。组合物含有药物和阴离子交换树脂，并且在消化道中显示出优异的吸收性。

6. 发明申请

WO1996028416A1 AMINOPHENOL DERIVATIVES 审中-公开
标题翻译：氨基酚衍生物
公开(公告)号：WO1996028416A1
公开(公告)日：1996-09-19
申请号：PCT/JP1996000611
申请日：1996-03-12
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , YOKOHAMA, Shuichi , KAWAGOE, Keiichi , TAKEDA, Yasuyuki , YOKOMIZO, Yoshihiro , YOKOMIZO, Aki
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07C275/28
CPC分类号： C07C275/28 , C07C275/16 , Y10S514/925 , Y10S514/927
摘要： Aminophenol derivatives represented by general formula (1), salts thereof or optical isomers thereof, and a gastrin receptor antagonist, a cholecystokinin receptor antagonist and a remedy for digestive tract diseases containing the same, wherein X represents O or S; A represents alkylene; R represents phenyl, etc.; R and R represent each H or alkyl; R represents substituted carbamoylalkyl, etc.; and R represents substituted amino, etc. The compounds have a potent gastrin or CCK-A receptor antagonism and a high selectivity for one of the CCK-A and gastrin receptor and are useful as a preventive or remedy particularly for digestive tract diseases such as peptic ulcer or a remedy for central nervous diseases.
摘要翻译：由通式（1）表示的氨基苯酚衍生物，其盐或其光学异构体，胃泌素受体拮抗剂，缩胆囊素受体拮抗剂和含有它们的消化道疾病的治疗剂，其中X表示O或S; A表示亚烷基; R 1表示苯基等; R 2和R 3各自表示H或烷基; R 4表示取代的氨基甲酰基烷基等。并且R 5代表取代的氨基等。该化合物对CCK-A和胃泌素受体之一具有有效的胃泌素或CCK-A受体拮抗作用和高选择性，并且可用作特别用于消化道疾病的预防或治疗如消化性溃疡或中枢神经疾病的补救措施。

7. 发明申请

WO1996024593A1 HETEROCYCLIC SPIRO DERIVATIVES 审中-公开
标题翻译：杂环螺旋衍生物
公开(公告)号：WO1996024593A1
公开(公告)日：1996-08-15
申请号：PCT/JP1996000248
申请日：1996-02-06
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , OHKI, Hitoshi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： Antibacterial compounds useful as medicines, animal drugs, aquacultural drugs or antibacterial preservatives; and antibacterial drugs or preparations containing the same, having an excellent activity against a wide variety of bacteria including particularly quinolone-resistant bacteria and being highly safe, more specifically quinolone derivatives that are represented by general formula (I) wherein R at the 7-position represents a group derived from a heterocyclic spiro compound and N at the 1-position bears a halogenocyclopropyl group and that comprise each preferably a single isomer.
摘要翻译：用作药物，动物药物，水产养殖药物或抗菌防腐剂的抗菌化合物; 和含有该抗菌药物或其制剂的抗菌药物或制剂，具有优异的抗多种细菌，特别是喹诺酮抗性细菌的活性，并且是高度安全的，更具体地，通式（I）表示的喹诺酮衍生物，其中R 2在 7-位表示衍生自杂环螺环化合物的基团，1-位上的N具有卤代环丙基，并且每个优选包含单个异构体。

8. 发明申请

WO1996000570A1 ANTIBACTERIAL AGENT 审中-公开
标题翻译：抗菌剂
公开(公告)号：WO1996000570A1
公开(公告)日：1996-01-11
申请号：PCT/JP1995001289
申请日：1995-06-28
申请人： DAIICHI PHARMACEUTICAL CO., LTD.
发明人： DAIICHI PHARMACEUTICAL CO., LTD. , KATO, Shozo , ITAHANA, Hidenobu , ISHIZAKI, Masahiko +di , FURUKI, Makiko , YAMAGUCHI, Masao , OHMURO, Fumio , NAGATA, Seiji , OHARA, Eiji , KITAJIMA, Toshio
IPC分类号： A61K31/275
CPC分类号： C07D213/64 , A61K31/275 , A61K31/277 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/423 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4412 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4453 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/495 , A61K31/498 , A61K31/505 , A61K31/506 , A61K31/5375 , A61K31/55 , C07C255/21 , C07D213/57 , C07D239/30 , C07D241/44 , C07D263/58 , C07D277/68 , C07D295/15 , C07D295/185 , C07D307/54 , C07D333/24
摘要： An antibacterial containing a ketonitrile derivative represented by general formula (1) or a salt thereof as the active ingredient and having an excellent antibacterial activity against Gram-positive and Gram-negative bacteria, wherein R represents hydrogen or lower alkyl; R , R , R and R represent each independently hydrogen, halogen, nitro, lower alkyl, lower alkoxy or (un)substituted phenoxy; X represents (un)substituted aromatic hydrocarbyl or (un)substituted heterocycle; Y represents (un)substituted aromatic hydrocarbyl, (un)substituted heterocycle, carbonyl substituted by (un)substituted aromatic hydrocarbyl, carbonyl substituted by (un)substituted heterocycle, or N,N-disubstituted carbamoyl.
摘要翻译：一种抗菌剂，其含有通式（1）表示的酮腈衍生物或其盐作为活性成分，对革兰氏阳性菌和革兰氏阴性菌具有优异的抗菌活性，其中R 1表示氢或低级烷基; R 2，R 3，R 4和R 5各自独立地表示氢，卤素，硝基，低级烷基，低级烷氧基或（取代的）取代的苯氧基; X表示（un）取代的芳族烃基或（un）取代的杂环; Y代表（取代的）取代的芳族烃基，（取代的）取代的杂环，由（未）取代的芳族烃基取代的羰基，被（未）取代的杂环取代的羰基或N，N-二取代的氨基甲酰基。

9. 发明申请

WO1995033740A1 DEACETOXYTAXOL DERIVATIVE 审中-公开
标题翻译：脱乙酰氧基衍生物
公开(公告)号：WO1995033740A1
公开(公告)日：1995-12-14
申请号：PCT/JP1995001163
申请日：1995-06-09
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TERASAWA, Hirofumi , SOGA, Tsunehiko , NAKAYAMA, Kiyoshi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D305/14
CPC分类号： C07D407/12 , C07D305/14
摘要： A novel antitumor taxol derivative that is represented by general formula (I) has various substituents, and is modified with a carbon-carbon bond at the 10-position.
摘要翻译：由通式（I）表示的新型抗肿瘤紫杉醇衍生物具有各种取代基，并且在10位被碳 - 碳键修饰。

10. 发明申请

WO1995011674A1 GRANULAR PREPARATION 审中-公开
标题翻译：颗粒制备
公开(公告)号：WO1995011674A1
公开(公告)日：1995-05-04
申请号：PCT/JP1993001553
申请日：1993-10-27
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , NAKAGAMI, Hiroaki , KESHIKAWA, Taketoshi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/41
CPC分类号： A61K9/1652 , A61K9/1623 , A61K9/1635 , A61K31/41
摘要： A granular preparation produced by granulating finely powdered ebselen (2-phenyl-1,2-benzisoselenazol-3(2H)-one) with a hydrophilic polymer, and an aqueous suspension of the preparation. The preparation is excellent as a preparation for administration through a stomach tube, because it can readily and homogeneously be dispersed in water or an aqueous solution when suspended therein prior to use and keeps a good suspension state, thus facilitating the production of a drug solution containing the same and the administration thereof through the tube. Also, the granular preparation and the drug solution containing the same can be administered without remaining in the tube and hence the dose can be kept accurate. In addition, this preparation can be produced without ressort to any special apparatus and process, thus being adaptable to mass production.
摘要翻译：通过用亲水性聚合物将细粉末依依硒硒（2-苯基-1,2-苯并异恶唑-3（2H） - 酮）制粒而制备的颗粒状制剂和该制剂的水性悬浮液。该制剂作为用于通过胃管施用的制剂是优异的，因为在使用之前悬浮在水中或水溶液中可容易且均匀地分散在其中并保持良好的悬浮状态，从而有助于制备含有相同并通过管的管理。此外，粒状制剂和含有它们的药物溶液可以不留在管中而被施用，因此剂量可以保持准确。另外，这种制备方法可以在不退出任何特殊装置和方法的情况下生产，从而适应于批量生产。

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