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31. 发明专利

JPS6256434A PRODUCTION OF CHINESE HERB EXTRACT 失效
公开(公告)号：JPS6256434A
公开(公告)日：1987-03-12
申请号：JP19385285
申请日：1985-09-04
申请人： TSUMURA JUNTENDO KK
发明人： UCHIDA HISAHIRO , KOMATA KAZUHIRO , KURITA KOJI , KIMURA TAKAYOSHI
IPC分类号： A61K36/00 , A61P3/00
摘要： PURPOSE:To obtain a Chinese herb extract having excellent disintegrability, by contacting an extracted liquid of Chinese herb drug or its concentrated liquid with an immobilized amylase, drying the reaction product and mixing the obtained powder optionally with an excipient. CONSTITUTION:A Chinese herb drug including crude drug is extracted preferably with water at 90-100 deg.C, concentrated at 30-50 deg.C under reduced pressure, and the obtained extract liquid or its concentrate is made to contact and react with an immobilized amylase. The immobilized amylase is alpha-amylase, beta-amylase, etc., and can be produced by the conventional enzyme-immibilization method, however, a commercially available immobilized alpha-amylase (e.g. A-5386, product of Sigma Corp.) can be used for the purpose. The contact reaction can be carried out by adding the immobilized amylase directly to the extracted liquid or concentrated liquid at 6-8pH and 30-40 deg.C. The reaction liquid is dried to obtain Chinese herb extract powder, which is optionally mixed with an excipient such as starch, sugar, etc., to form Chinese herb extract drugs having various forms.

32. 发明专利

JPS6236315A ANTIHYPERLIPEMIC AGENT 失效
公开(公告)号：JPS6236315A
公开(公告)日：1987-02-17
申请号：JP17400685
申请日：1985-08-09
申请人： TSUMURA JUNTENDO KK
发明人： YUDA MASAKI , OTSUKI SHINICHI , MAEMURA SHUNICHI
IPC分类号： C07D311/16 , A61K31/37 , A61P3/06
摘要： PURPOSE:To provide an antihyperlipemic agent containing hymecromone as an active component and having remarkably high pharmacological activity and safety. CONSTITUTION:Hymecromone (4-methylumbelliferone) of formula known as a cholagogue is used as an active component of an antihyperlipemic agent. The compound does not increase the body weight, exhibits antihyperlipemic action, and has extremely low toxicity and high safety. Accordingly, it can be administered to an animal or man singly or in combination with conventional drug carrier, e.g. in the form of an oral drug such as tablet, capsule, powder, etc. The dose of the compound to achieve the desired effect is usually 150-250mg of the compound daily for an adult by oral administration.

33. 发明专利

JPS61282319A PRODUCTION OF CHINESE HERB EXTRACT 失效
公开(公告)号：JPS61282319A
公开(公告)日：1986-12-12
申请号：JP12255285
申请日：1985-06-07
申请人： TSUMURA JUNTENDO KK
发明人： UCHIDA HISAHIRO , KOMATA KAZUHIRO , KURITA KOJI , KIMURA TAKAYOSHI
IPC分类号： A61K36/25 , A61K36/00
摘要： PURPOSE:To obtain a Chinese herb extract having excellent disintegrability, by adding and reacting amylase to the extracted or concentrated liquid of Chinese herb, drying and pulverizing the reaction product and optional mixing with an excipient such as sugar, cellulose, etc. CONSTITUTION:Chinese herb drug [e.g. KAKKON-TO (decocted root of Pueraria lobata), ANCHU-SAN (mixed powder of the root of Glycyrrhiza glaba, rhizome of Zingiber officinale, etc.), KOSAIKO-TO, etc.] is extracted with a solvent (e.g. water, aqueous solution of ethanol of

34. 发明专利

JPS61263924A NASAL DROP 失效
公开(公告)号：JPS61263924A
公开(公告)日：1986-11-21
申请号：JP10269685
申请日：1985-05-16
申请人： TSUMURA JUNTENDO KK
发明人： TAKEUCHI YOSHIO , SAIGA TOSHIKAZU
IPC分类号： A61K36/00 , A61K9/08 , A61K9/14 , A61P37/08
摘要： PURPOSE:A nasal drop, containing dried powder of an aqueous extract of crude drugs, e.g. ephedra root, poeny root, etc., as an active constituent and effective for treating allergic rhinitis with little irritancy. CONSTITUTION:A nansal drop obtained by extracting 8 kinds of crude drugs prepared by mixing 1pts.wt. each ephedra herb, poeny root, dried ginger, licorice, cinnamon bark, asiasarum root and schisandra fruit with 2pts.wt. pinellia tuber with water while hot at 50-100 deg.C drying the resultant extract by freeze-drying, spray drying, etc., to give dried powder of the aqueous extract of the 8 kinds of the crude drugs, dissolving the resultant dried extract powder in a buffer solution of 6.5-7.5pH, e.g. physiological saline solution buffered with phosphoric acid and, as necessary, filtering and sterilizing the resultant solution, e.g. filtration and sterilization with a millipore filter, etc. The resultant nasal drop is put into a sterilized container, etc., for preventing the contamination by bacteria, etc., and preferably preserved at a low temperature, e.g. about 4 deg.C, but the preservation at ordinary temperature can be carried out by adding a preservative thereto.

35. 发明专利

JPS61134338A Preparation of phenol ketone compound 失效
标题翻译：酚醛酮化合物的制备
公开(公告)号：JPS61134338A
公开(公告)日：1986-06-21
申请号：JP25616984
申请日：1984-12-03
申请人： Tsumura Juntendo Inc , Wako Pure Chem Ind Ltd
发明人： TANAKA MIKIAKI , URANO FUMIYOSHI , TANI TSUTOMU
IPC分类号： C07C49/255 , C07C45/00 , C07C45/45 , C07C45/61 , C07C45/64 , C07C45/72 , C07C67/00
CPC分类号： Y02P20/55
摘要： PURPOSE: To obtain the titled compound, by protecting phenolic hydroxyl group of zingerone with benzyl group, reacting the resultant compound with a strong base of a counter ion of an alkali metal first and then with n-hexanal to form the corresponding aldol, and eliminating the protecting group.
CONSTITUTION: Vanillin and acetone are subjected to aldol condensation reaction to obtain 4-hydroxy-3-methoxy-benzylineacetone, and phenolic hydroxyl group of a reduction product thereof, zingerone expressed by formula I, is protected with an optionally substituted benzyl group (example; benzyl, p-nitrobenzyl). Thus obtained product is then reacted with a strong base of a counter ion of an alkali metal to produce an enolate anion, further added with n-hexanal to form the corresponding aldol, and then the protecting group thereof is eliminated to obtain [6]-zingerol expressed by formula II or, by further being subjected to dehydration, [6]-shogaol expressed by formula III.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：为了获得标题化合物，通过用苄基保护姜酮的酚羟基，首先使所得化合物与碱金属的抗衡碱的强碱反应，然后与正己醛反应形成相应的醛醇，并除去保护组。构成：将香草醛和丙酮进行醛醇缩合反应，得到4-羟基-3-甲氧基 - 苄基丙酮，其还原产物的酚羟基，由式I表示的姜酮，用任选取代的苄基保护（例如; 苄基，对硝基苄基）。然后将所得产物与碱金属的抗衡离子的强碱反应以产生烯醇化物阴离子，进一步加入正己醛以形成相应的醛醇，然后除去其保护基，得到[6] - 由式II表示的姜黄素或通过进一步脱水，由式III表示的[6] - 高糖。

36. 发明专利

JPS6033086B2 失效
公开(公告)号：JPS6033086B2
公开(公告)日：1985-08-01
申请号：JP9779577
申请日：1977-08-17
申请人： TSUMURA JUNTENDO KK
发明人： MAEDA SHINYA , YUDA MASAKI , IKETANI YUKINOBU , TAGUCHI HEIHACHIRO , YOSHIOKA ICHIRO
IPC分类号： A61K31/09 , A61K31/357 , A61K31/36 , A61P25/04 , A61P29/00 , C07C41/00 , C07C43/23 , C07C67/00 , C07D317/70

37. 发明专利

JPS59227823A TONIC 失效
公开(公告)号：JPS59227823A
公开(公告)日：1984-12-21
申请号：JP10270083
申请日：1983-06-10
申请人： KOSUGE TAKUO , TSUMURA JUNTENDO KK
发明人： KOSUGE TAKUO , ISHIDA KINJI , NAGASAWA MICHIO
IPC分类号： C07J17/00 , A61K31/704 , A61K36/25 , A61P7/00
摘要： PURPOSE:To provide a tonic having blood activating action and useful as an agent to suppress the hemorrhage, a fatigue releaving agent, etc., by using a panaxadiol glycoside obtained from the rhizome of Panax ginseng C.A. Meyer belonging to Araliaceae family as a main component. CONSTITUTION:The objective tonic contains, as a main component, the panaxadiol glycoside of formula [R1 is beta-D-glucopyranosyl-(1 2)-beta-D-glucopyranosyl; R2 is beta-D-glucopyranosyl-(1 6)-beta-D-glucopyranosyl or alpha-L-arabinopyranosyl-(1 6)-beta- D-glucopyranosyl]. The glycoside of the formula can be prepared by extracting the rhizome of Panax ginseng C.A. Meyer with methanol, defatting the extract liquid with ether, partitioning with butanol-water, and purifying the butanol layer by silica gel column chromatography. The glycoside of formula has also the bleed suppressing activity, and is used as a bleed-suppressing agent or for the general health maintenance, relief from fatigue, etc.

38. 发明专利

JPS59164721A Respiratory complement 失效
标题翻译：呼吸补充
公开(公告)号：JPS59164721A
公开(公告)日：1984-09-17
申请号：JP3917483
申请日：1983-03-11
申请人： Takuo Kosuge , Tsumura Juntendo Inc
发明人： KOSUGE TAKUO , ISHIDA KINJI , NAGASAWA MICHIO
IPC分类号： A61K31/70 , A61K31/704 , A61P1/00 , A61P7/00 , A61P43/00 , C07H15/24 , C07J17/00
摘要： PURPOSE: To provide the titled agent containing a saponin derivative as a main component and having blood activation effect.
CONSTITUTION: A respiratory complement having blood activation effect is prepared by using the compound of formula as a main component. Preferable dose in an urgent blood activation in flooding is 15W25mg/dose for intravenous injection, 30W40mg/dose for peritoneal infusion and 50W100mg/dose for oral administration, and ≤3 doses a day. The agent is effective to improve the function of blood in the case of flooding in major operation, etc., and to recover the fatigue quickly. It is also useful for the improvement of intractable diseases such as rheumatism, neuralgia, etc. by continuous use for a long period, and for the maintenance of health. The main component can be prepared by crushing the rhizome of Panax japonicus, extracting with hot water containing 50% of methanol, concentrating the extract liquid, extracting the concentrated aqueous solution of the extract with n-butanol, and subjecting the resultant extract e.g. to counter-current partition, etc.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：提供含有皂苷衍生物作为主要成分并具有血液活化作用的标本。构成：通过使用式的化合物作为主要成分制备具有血液活化作用的呼吸补体。淹水紧急血液活化的优选剂量为静脉注射剂量为15-25mg /剂量，腹膜输注剂为30-40mg /剂量，口服给药量为50-100mg /剂量，每天剂量为3剂。在主要操作等情况下，代理人有效改善血液的功能，并迅速恢复疲劳。通过连续使用长时间改善顽固性疾病如风湿病，神经痛等，以及维持健康也是有用的。主要成分可以通过粉碎Pan the的根茎，用含有50％甲醇的热水提取，浓缩提取液，用正丁醇萃取提取物的浓缩水溶液，并将所得提取物例如逆流分区等

39. 发明专利

JPS59141574A Preparation of lignan 失效
标题翻译： LIGNAN的准备
公开(公告)号：JPS59141574A
公开(公告)日：1984-08-14
申请号：JP1458683
申请日：1983-02-02
申请人： Tsumura Juntendo Inc
发明人： TAKEYA TETSUYA , KOTANI EIICHI , TOBINAGA KIYOTERU
IPC分类号： C07D307/92 , C07D317/00 , C07D407/04 , C07D493/04
摘要： PURPOSE: To obtain a lignan useful as an antitumor agent or microtube polymerization inhibitor, etc. in high yield in one stage, by oxidizing a phenylpropene with an oxidizing composition prepared by dissolving chromic acid anhydride in a strong acid and an organic solvent in the above-mentioned organic solvent.
CONSTITUTION: A compound of formula I (R
1 WR
5 are H or electron donative group, such as halogen, lower alkoxyl, benzyloxy, NH
2 , etc.; two thereof together form methylenedioxy or ethylenedioxy group; at least one of the o-positions with respect to the side chain on the benzene ring is H) is oxidized with an oxidizing composition prepared by dissolving chromic acid anhydride in a strong acid and one or more organic solvents selected from acetonitrile, propionitrile, butyronitrile and nitromethane in the above-mentioned organic solvents to give the aimed compound of formula II (R
7 is H or OH) useful as the above-mentioned medicine, e.g. podophyllotoxin, etc. advantageously by easy operation.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：为了在一个阶段中以高产率获得用作抗肿瘤剂或微管阻聚剂等的木酚素，通过将上述的酸酐和有机溶剂中的铬酸酐溶解而成的氧化性组合物氧化苯丙酮所述有机溶剂。构成：式I化合物（R 1 -R 5为H或电子给予基团，例如卤素，低级烷氧基，苄氧基，NH 2等;其中两个一起形成亚甲二氧基或亚乙二氧基;至少一个与相对于苯环上的侧链是H）用通过将铬酸酐溶解在上述有机溶剂中的铬酸酐和选自乙腈，丙腈，丁腈和硝基甲烷中的一种或多种有机溶剂制备的氧化组合物来氧化得到目标化合物II（R7为H或OH），可用作上述药物，例如鬼臼毒素等，容易操作。

40. 发明专利

JPS59106416A Cholagogue 失效
标题翻译：利胆
公开(公告)号：JPS59106416A
公开(公告)日：1984-06-20
申请号：JP21552882
申请日：1982-12-10
申请人： Tsumura Juntendo Inc
发明人： FUJIMURA HAJIME , SAWADA TOKUNOSUKE , YAMAHARA JIYOUJI
IPC分类号： A61K31/11 , A61K36/18 , A61P1/00
摘要： PURPOSE: A cholagogue having high safety and durability of action, containing cinnamic aldehyde as an active ingredient.
CONSTITUTION: A cholagogue containing cinnamic aldehyde, a main component of cinnamon oil, as an active ingredient. After cinnamic aldehyde (A) is compared with sodium dehydrocholate (B) in terms of cholagogic action (by Wistar male rat) and acute toxicity (by -Y male mouse) and discussed, B has temporary effect in cholagogic action, and A has excellent cholagogic action and durability. A has ≥5,000mg/kg LD
50 value, B has 2,050mg/kg LD
50 value. A is observed to have high cholagogic action and high safety. An effective dose of cinnamic aldehyde is properly regarded to be 50W100mg per time adult and ≤3 times administration daily.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：具有高安全性和耐久性的胆碱，含有肉桂醛作为活性成分。构成：含有肉桂醛肉桂醛作为活性成分的主要成分的胆碱。肉桂醛（A）与胆酸作用（Wistar雄性大鼠）和急性毒性（通过-Y雄性小鼠）进行比较，并讨论了B，在胆碱作用中具有临时作用，A具有优异的作用胆汁酸作用和耐久性。 A具有> = 5,000mg / kg LD50值，B具有2050mg / kg LD 50值。观察到A具有高胆固醇作用和高安全性。肉桂醛的有效剂量适当地被认为是每次成年人50-100mg，每天施用<= 3次。

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