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31. 发明申请

WO1998022451A1 TAXOL DERIVATIVES 审中-公开
标题翻译： TAXOL衍生物
公开(公告)号：WO1998022451A1
公开(公告)日：1998-05-28
申请号：PCT/JP1997004175
申请日：1997-11-17
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , SOGA, Tsunehiko , UOTO, Kouichi , IIMURA, Shin
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： Substituted taxol derivatives of general formula (I) having an antitumor activity, wherein R is optionally substituted alkyl, alkenyl or alkynyl; and R is methyl, or together with R forms a three-membered ring, provided the cases wherein R is hydrogen, R is hydrogen or hydroxyl, and the linkage between the carbon atoms to which R and R are bonded respectively is a single bond are excepted.
摘要翻译：具有抗肿瘤活性的通式（I）的取代紫杉醇衍生物，其中R 6为任选取代的烷基，烯基或炔基; 并且R 5为甲基，或与R 4一起形成三元环，条件是其中R 3为氢，R 4为氢或羟基，并且碳原子与 R 3和R 4分别键合为单键。

32. 发明申请

WO1998018783A1 TRICYCLIC AMINE DERIVATIVES 审中-公开
标题翻译：三元胺衍生物
公开(公告)号：WO1998018783A1
公开(公告)日：1998-05-07
申请号：PCT/JP1997003842
申请日：1997-10-23
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , TAKAHASHI, Hisashi , KIMURA, Kenichi , MIYAUCHI, Rie , OHKI, Hitoshi , KAWAKAMI, Katsuhiro
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D455/02 , C07D471/04 , C07D513/04
摘要： Compounds represented by general formula (I) carrying a tricylic amine substituent optionally having various substituents, their salts, hydrates thereof or drugs containing these compounds as the active ingredient. Because of having favorable antibacterial activities on gram-negative and gram-positive bacteria and being excellent both in the dynamics in vivo and safety, these compounds are useful in treating infectious diseases. In said formula (I), Q represents a partial structure which is preferably represented by formula (a); or (b) and may have various substituents.
摘要翻译：由通式（I）表示的化合物，其携带任选具有各种取代基的三取代胺取代基，其盐，水合物或含有这些化合物作为活性成分的药物。由于对革兰氏阴性和革兰氏阳性细菌具有良好的抗菌活性，并且在体内和安全性方面都具有优异的作用，因此这些化合物可用于治疗感染性疾病。在所述式（I）中，Q表示优选由式（a）表示的部分结构。或（b），并且可以具有各种取代基。

33. 发明申请

WO1998002431A1 cis-SUBSTITUTED AMINOCYCLOPROPANE DERIVATIVES 审中-公开
标题翻译：顺式取代的氨基羰基衍生物
公开(公告)号：WO1998002431A1
公开(公告)日：1998-01-22
申请号：PCT/JP1997002411
申请日：1997-07-11
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , TAKAHASHI, Hisashi , ISHIDA, Yohhei
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D207/26 , A61K31/4375 , A61K31/4709 , C07D207/24 , C07D401/04 , Y02A50/475
摘要： Antibacterial drugs exhibiting potent antibacterial effects against various bacteria and high safety, which comprise compounds of general formula (1), or salts of the compounds or hydrates thereof: wherein R and R are each hydrogen or alkyl; n is an integer of 1 to 3; R is alkyl, alkenyl, halogenoalkyl, cyclic alkyl, aryl, heteroaryl, alkoxyl or alkylamino; R is hydrogen or alkylthio; R is hydrogen, amino, hydroxyl, mercapto, halogenomethyl, alkyl, alkenyl, alkynyl or alkoxyl; X is halogeno or hydrogen; A is nitrogen or (II); X is hydrogen, amino, halogeno, cyano, halogenomethyl, halogenomethoxyl, alkyl, alkenyl, alkynyl or alkoxyl; and Y is hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, ethoxycarbonyl, cholyl, dimethylaminoethyl, 5-indanyl, phthalidyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, alkyl, alkoxymethyl or phenylalkyl.
摘要翻译：对各种细菌和高度安全性具有强效抗菌作用的抗菌药物，其包含通式（1）的化合物或其化合物或其水合物的盐：其中R 1和R 2各自为氢或烷基; n为1〜3的整数， R 3是烷基，烯基，卤代烷基，环烷基，芳基，杂芳基，烷氧基或烷基氨基; R 4是氢或烷硫基; R 5是氢，氨基，羟基，巯基，卤代甲基，烷基，烯基，炔基或烷氧基; X 1是卤代或氢; A是氮或（II）; X 2是氢，氨基，卤代，氰基，卤代甲基，卤代甲氧基，烷基，烯基，炔基或烷氧基; 并且Y是氢，苯基，乙酰氧基甲基，新戊酰氧基甲基，乙氧基羰基，取代基，二甲基氨基乙基，5-二氢化茚基，邻苯二甲酰基，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，，烷氧基甲基或苯基烷基。

34. 发明申请

WO1997046261A1 PROCESS FOR PRODUCING DRUG COMPLEXES 审中-公开
标题翻译：生产药物复合物的方法
公开(公告)号：WO1997046261A1
公开(公告)日：1997-12-11
申请号：PCT/JP1997001915
申请日：1997-06-05
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , INOUE, Kazuhiro , SUSAKI, Hiroshi , IKEDA, Masahiro
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： A61K47/48
CPC分类号： A61K47/61
摘要： A process for producing drug complexes wherein a carboxylated polysaccharide derivative is bonded to a medicinal compound residue via a spacer consisting of an amino acid or a spacer consisting of two to eight amino acids bonded to each other via peptide bonds, or drug complexes wherein a carboxylated polysaccharide derivative is bonded to a medicinal compound residue via no spacer, which is characterized by reacting in a nonaqueous system an organic amine salt of the carboxylated polysaccharide derivative with the medicinal compound or the spacer bonded thereto. Thus, the reaction between the carboxylated polysaccharide derivative and the medicinal compound bonded to the spacer, etc., can be effected to achieve a high yield and side reactions can be inhibited in the case where, for example, the medicinal compound is one having a lactone ring.
摘要翻译：一种制备药物复合物的方法，其中羧化多糖衍生物通过由氨基酸组成的间隔物或由通过肽键彼此键合的2至8个氨基酸组成的间隔物结合到药用化合物残基，或其中羧化的多糖衍生物通过无间隔物与药物化合物残留物结合，其特征在于使非羧酸化多糖衍生物的有机胺盐与药物化合物或与其结合的间隔基反应。因此，可以实现羧化多糖衍生物与与间隔基等结合的药物化合物之间的反应，以达到高产率，并且可以抑制副反应，例如在药物化合物为内酯环。

35. 发明申请

WO1997019072A1 SUBSTITUTED AMINOCYCLOALKYLPYRROLIDINE DERIVATIVES 审中-公开
标题翻译：取代的氨基环丙基吡咯烷衍生物
公开(公告)号：WO1997019072A1
公开(公告)日：1997-05-29
申请号：PCT/JP1996003440
申请日：1996-11-22
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , TAKAHASHI, Hisashi , KIMURA, Kenichi , MIYAUCHI, Satoru , 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 aminocycloalkylpyrrolidine and represented by general formula (I), salts thereof, or hydrates of both, wherein Q is formula (II) or (IV).
摘要翻译：其具有抗菌活性和安全性优异的抗菌药物，其中Q为式（II）或（IV），其中喹诺酮衍生物具有各种取代基，包括取代的氨基环烷基吡咯烷并由通式（I）表示，其盐或两者的水合物。

36. 发明申请

WO1996037470A1 PROCESSES FOR PREPARING CYCLIC COMPOUNDS 审中-公开
标题翻译：制备循环化合物的方法
公开(公告)号：WO1996037470A1
公开(公告)日：1996-11-28
申请号：PCT/JP1996001373
申请日：1996-05-23
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , AKIBA, Toshifumi , EBATA, Tutomu , SAITO, Tatsuru , SHIMIZU, Sadahiro , HIRAI, Keiichi , OHTA, Naoki , TOJO, Toshiaki
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D209/54
CPC分类号： C07C271/22 , C07C255/31 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/54
摘要： Compounds of general formula (I), wherein n is an integer of 2 to 5; R is H or a substituent of general formula (R ) (wherein R , R and R are each phenyl, phenylmethyl or naphthyl optionally substituted with one or more substituents of at least one member selected from the group consisting of C1-C4 alkyl, C1-C4 alkoxy, halogeno and nitro, H or C1-C4 alkyl); and R is H or C1-C4 alkyl (with the proviso that the compound wherein n is 2, R is H and R is ethyl is excepted); other compounds of general formula (II) prepared from the compounds of general formula (I), being useful as an antimicrobial; and novel processes for preparing these compounds at a low cost and in less steps.
摘要翻译：通式（I）的化合物，其中n为2〜5的整数; R 1是H或通式（R 1）的取代基（其中R a，R b和R c各自为苯基，苯基甲基或萘基，其任选被一个或多个取代基取代在至少一个选自C 1 -C 4烷基，C 1 -C 4烷氧基，卤代和硝基，H或C 1 -C 4烷基）。 R 2为H或C 1 -C 4烷基（条件是其中n为2，R 1为H且R 2为乙基的化合物除外）; 由通式（I）的化合物制备的其它由通式（II）表示的化合物可用作抗微生物剂; 以及以低成本和较少步骤制备这些化合物的新方法。

37. 发明申请

WO1996033998A1 PENTACYCLIC COMPOUNDS 审中-公开
标题翻译： PENTACYCLIC化合物
公开(公告)号：WO1996033998A1
公开(公告)日：1996-10-31
申请号：PCT/JP1996001145
申请日：1996-04-25
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TERASAWA, Hirofumi , SOGA, Tsunehiko , ISHIYAMA, Takashi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D493/08
CPC分类号： C07D493/08 , C07D305/14
摘要： Compounds represented by general formula (I) and having an antitumor effect and salts thereof: wherein R represents phenyl; R represents alkyl, alkenyl, alkynyl, cycloalkyl or alkoxy; R represents hydrogen, hydroxy, halogeno, alkoxy, -O-R , acyloxy or -O-CO-R (wherein R represents alkylamino, alkenyl, alkynyl, cycloalkyl, aryl or a heterocycle); R and R represent each hydrogen, alkyl, alkenyl, alkynyl, aryl or a heterocycle; Z represents hydrogen, hydroxy, halogeno or alkyl; Z represents hydrogen, hydroxy, halogeno or alkyl; and Z represents alkyl, alkenyl, alkynyl, cycloalkyl, aryl or a heterocycle.
摘要翻译：由通式（I）表示并具有抗肿瘤作用的化合物及其盐：其中R 1表示苯基; R 2表示烷基，烯基，炔基，环烷基或烷氧基; R 3表示氢，羟基，卤代，烷氧基，-OR 31，酰氧基或-O-CO-R 31（其中R 31表示烷基氨基，烯基，炔基，环烷基，芳基或杂环） ; R 4和R 5各自代表氢，烷基，烯基，炔基，芳基或杂环; Z 1表示氢，羟基，卤代或烷基; Z 2表示氢，羟基，卤代或烷基; Z 3表示烷基，烯基，炔基，环烷基，芳基或杂环。

38. 发明申请

WO1996029308A1 ANHYDROUS CRYSTALS 审中-公开
标题翻译：无水晶体
公开(公告)号：WO1996029308A1
公开(公告)日：1996-09-26
申请号：PCT/JP1996000485
申请日：1996-03-01
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , SATO, Yukio , KITAOKA, Hiroaki , TERADA, Tatsuya , ONO, Makoto
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D207/27
CPC分类号： C07D207/27
摘要： Substantially nonhygroscopic anhydrous crystals of compounds represented by the general formula: R -CH2CONH-R (wherein R represents (un)substituted pyridyl or (un)substituted phenyl; and R represents (un)substituted 2-oxo-1-pyrrolidinyl). Drying the hydrous crystals of the above compounds at a temperature of 80 DEG C or above under reduced pressure yields the corresponding anhydrous crystals with a weight gain of at most 1 % caused by moisture absorption after storage at a relative humidity of 83 % and a temperature of 25 DEG C for 30 days. Medicines containing the above compounds in the form of anhydrous crystals are uniform in the active ingredient content.
摘要翻译：基本上不吸水的由以下通式表示的化合物的无水晶体：R 2 -CH 2 CONH-R 1（其中R 1表示（未）取代的吡啶基或（取代的）取代的苯基; R 2表示（un ）取代的2-氧代-1-吡咯烷基）。在80℃或更低的温度下减压干燥上述化合物的含水晶体，得到在相对湿度83％和温度下储存后由吸湿引起的重量增加至多为1％的相应无水晶体 25℃30天。含有无水晶体形式的上述化合物的药物的活性成分含量是均匀的。

39. 发明申请

WO1994012512A1 GLUCOSYLGLUCOSIDE DERIVATIVE 审中-公开
标题翻译：葡萄球菌衍生物
公开(公告)号：WO1994012512A1
公开(公告)日：1994-06-09
申请号：PCT/JP1993001710
申请日：1993-11-22
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , SOGA, Tsunehiko; , KUMAZAWA, Eiji;
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07H15/04
CPC分类号： C07H15/04
摘要： An antitumor compound represented by general formula (1), wherein Q represents carboxy or phosphono; Q represents carboxy, phosphono or hydrogen; m represents an integer of 0 to 10; n represents an integer of 0 to 10; R represents acyl or substituted acyl; R represents acyl or substituted acyl; and R represents acyl or substituted acyl.
摘要翻译：由通式（1）表示的抗肿瘤化合物，其中Q 1表示羧基或膦酰基; Q 2表示羧基，膦酰基或氢; m表示0〜10的整数。 n表示0〜10的整数， R 1表示酰基或取代的酰基; R 2表示酰基或取代的酰基; R 3表示酰基或取代的酰基。

40. 发明申请

WO1993012818A1 PHARMACEUTICAL PREPARATION FOR TOPICAL APPLICATION 审中-公开
标题翻译：用于局部应用的药物制剂
公开(公告)号：WO1993012818A1
公开(公告)日：1993-07-08
申请号：PCT/JP1992001684
申请日：1992-12-22
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , FUJI YAKUHIN KOGYO KABUSHIKI KAISHA , OSHIMA, Koichi , MORITA, Yasuo , SEKI, Sumie , MORIKAWA, Tadanori , MAFUNE, Eiichi
发明人： DAIICHI PHARMACEUTICAL CO., LTD. , FUJI YAKUHIN KOGYO KABUSHIKI KAISHA
IPC分类号： A61K47/32
CPC分类号： A61K47/32 , A61K9/0014
摘要： A pharmaceutical preparation for topical application comprising a drug held by a highly water-absorbent polymer. It can hold a drug stably, facilitates the regulation of a dose, and is capable of sustained release. Since it is nonsticky and does not exude, the affected part can be kept clean and the removal of excessive base is unnecessary, thus facilitating nursing and widening the application field of the preparation.
摘要翻译：用于局部应用的药物制剂，其包含由高吸水性聚合物保持的药物。它可以稳定地保持药物，有利于调节剂量，并且能够持续释放。由于不粘，不渗透，所以受影响的部位可以保持清洁，不需要除去过量的碱，从而有助于护理和扩大制剂的应用领域。

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