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1. 发明专利

JP2005320267A Small-sized clarithromycin high content tablet and method for producing the same 审中-公开
标题翻译：小尺寸CLARITHROMYCIN高内容片及其制造方法
公开(公告)号：JP2005320267A
公开(公告)日：2005-11-17
申请号：JP2004138020
申请日：2004-05-07
申请人： Maruko Seiyaku Kk , マルコ製薬株式会社
发明人： BAN TOSHIHIRO , OTANI KAZUFUMI
IPC分类号： A61K9/20 , A61K9/28 , A61K31/7048 , A61K47/08 , A61K47/12 , A61K47/32
摘要： PROBLEM TO BE SOLVED: To prepare a clarithromycin high content tablet that is improved in medication properties and high preparation stability by miniaturizing the tablet size.
SOLUTION: This clarithromycin high content tablet is prepared by adding crospovidone as an excpient that has strong disintegration action and an organic acid or its pharmaceutically acceptable inorganic salt having strong sliding properties to clarithromycin that is hardly soluble in water and strongly sticks to metals, or the like, wherein the content of clarithromycin in the tablet is increased more than 75 mass%.
COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：要解决的问题：制备通过使片剂尺寸小型化而改善药物性质和高制备稳定性的克拉霉素高含量片剂。解决方案：这种克拉霉素高含量片剂是通过加入交联聚维酮作为具有强烈崩解作用的螯合剂制备的，并且对克拉霉素具有很强的滑动性能的有机酸或其药学上可接受的无机盐难溶于水并强烈粘附于金属，其中片剂中克拉霉素的含量增加超过75质量％。版权所有（C）2006，JPO＆NCIPI

2. 发明专利

JPH0524893B2 失效
公开(公告)号：JPH0524893B2
公开(公告)日：1993-04-09
申请号：JP7924285
申请日：1985-04-16
申请人： MITSUI NORIN KK , MARUKO SEIYAKU KK
发明人： HARA MASAHIKO , ASAI HAJIME , KITAMIKADO TADASHI , YAMAMOTO HAJIME , OKISHIO KAZUO , NAKAMURA KOZO
IPC分类号： A23F3/16 , A61K31/35 , A61K33/08 , A61K36/00 , A61K36/18 , A61K36/82 , A61P1/00 , A61P1/04 , C07D311/62

3. 发明专利

JPS6193160A Dihydropyridine derivative and its production 失效
标题翻译：二氢吡啶衍生物及其生产
公开(公告)号：JPS6193160A
公开(公告)日：1986-05-12
申请号：JP21553284
申请日：1984-10-15
申请人： Maruko Seiyaku Kk
发明人： ONO SACHIO , EBIHARA YUUKO , MIZUKOSHI SEISHI , KOMATSU OSAMU
IPC分类号： C07D211/90
摘要： NEW MATERIAL:A 1,4-dihydropyridine derivative shown by the formula I (R is lower alkyl; X is H, halogen, lower alkyl, lower alkoxy, etc.).
EXAMPLE: 2-(p-Toluenesulfonyloxy)ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(3-nitro phenyl)pyridine-3,5--dica-rboxyl ate.
USE: An intermediate capable of producing easily nicardipine hydrochloride useful as a vasodilator, an antihypertensive, etc. in high yield.
PREPARATION: A compound shown by the formula II producible easily in high yield is reacted with a compound shown by the formula III under a basic condi tion to give a compound shown by the formula I in high yield easily. SInce the compound is extremely reactive, it is easily reacted with N-methylbenzy lamine to give nicardipine hydrochloride in high yield.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：新材料：式I所示的1,4-二氢吡啶衍生物（R为低级烷基; X为H，卤素，低级烷基，低级烷氧基等）。实施例：2-（对甲苯磺酰氧基）乙基甲基1,4-二氢-2,6-二甲基-4-（3-硝基苯基）吡啶-3,5-二甲基 - 用途：能够容易地生产盐酸尼卡地平作为血管舒张剂，抗高血压药等产生高产率的中间体。制备：在碱性条件下，可以容易地以高产率生产的式II化合物与式III所示的化合物反应，以高产率容易地得到式I化合物。该化合物极易反应，容易与N-甲基苄胺反应，以高产率得到盐酸尼卡地平。

4. 发明专利

JPS59141583A Thiopyranopyrimidine derivative and its acid addition salt 失效
标题翻译：三硝基吡啶衍生物及其酸添加盐
公开(公告)号：JPS59141583A
公开(公告)日：1984-08-14
申请号：JP1509783
申请日：1983-02-01
申请人： Maruko Seiyaku Kk
发明人： OONO SACHIO , MIZUKOSHI SEISHI , KOMATSU OSAMU , YAMAMOTO HAJIME , KUNOU YASUO
IPC分类号： C07D495/04 , A61K31/505 , A61P3/08 , A61P3/10
摘要： NEW MATERIAL:The thiopyranopyrimidine derivative of formula I (R
1 is amino, hydroxyethylamino, piperazino, etc.; R
2 is amino, dimethylamino, morpholino, etc.).
EXAMPLE: 2-Amino-4-piperazino-7,8-dihydro-6H-thiopyrano[ 3,2-d ]-pyrimidine dimaleate.
USE: Remedy for diabetes.
PREPARATION: The compound of formula I wherein R
2 is NH
2 can be prepared by reacting 2-amino-4-chloro-7,8-dihydro-6H-thiopyrano[3,2-d]-pyrimidine of formula II (novel substance) with excessive amount of corresponding amine (e.g. ammonia, methylamine, etc.) in the absence or presence of a solvent such as dichloromethane at 0W100°C for 0.5W10hr. The starting compound of formula IIcan be obtained by reacting the compound of formula III with guanidine carbonate in the presence of a base, and reacting the resultant novel compound of formula IV with phosphorus oxychloride in the presence of N,N-dimethylaniline, etc.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I的噻喃并嘧啶衍生物（R 1是氨基，羟乙基氨基，哌嗪基等; R 2是氨基，二甲基氨基，吗啉代等）。实施例：2-氨基-4-哌嗪基-7,8-二氢-6H-噻喃并[3,2-d] - 嘧啶二马来酸盐。用途：糖尿病补救。制备：其中R 2是NH 2的式I化合物可以通过使式II的2-氨基-4-氯-7,8-二氢-6H-噻喃并[3,2-d] - 嘧啶（新颖的物质）与过量的相应的胺（如氨，甲胺等）在0-100℃的溶剂（如二氯甲烷）存在或不存在下反应0.5-10小时。式II的起始化合物可以通过在碱的存在下使式III化合物与碳酸胍反应而得到，并在N，N-二甲基苯胺等的存在下，使得到的式Ⅳ的新化合物与磷酰氯反应。

5. 发明专利

JPS6197264A Production of dihydropyridine derivative 失效
标题翻译：二氢吡啶衍生物的生产
公开(公告)号：JPS6197264A
公开(公告)日：1986-05-15
申请号：JP21799384
申请日：1984-10-17
申请人： Maruko Seiyaku Kk
发明人： ONO SACHIO , EBIHARA YUUKO , MIZUKOSHI SEISHI , KOMATSU OSAMU
IPC分类号： C07D211/90
摘要： PURPOSE: To obtain nicardipine hydrochloride in high yield easily, by replacing phenylsulfonyloxy group of 1,4-dihydropyridine derivative corresponding to the aimed compound with N-methylbenzylamine, wherein the phenylsulfonyloxy group may contain a substituent group such as halogen, etc.
CONSTITUTION: A compound shown by the formula I (X is H, halogen, lower alkyl, lower alkoxy, etc.) is reacted with N-methylbenzylamine in a solvent such as toluene, xylene, etc., or in the absence of a solvent, to give the aimed compound shown by the formula II having improved pharmaceutical action such as vasodilating action, antihypertensive action, etc., industrially advantageously. The compound shown by the formula I is obtained in high yield by reacting a compound shown by the formula III (R' is Me) with a compound shown by the formula IV, it has extremely high reactivity and its easily reacted with N-methylbenzylamine.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：通过用N-甲基苄胺代替对应于目标化合物的1,4-二氢吡啶衍生物的苯基磺酰氧基，其中苯基磺酰氧基可以含有卤素等取代基，可以容易地获得高产率的盐酸尼卡地平。构成：A 在溶剂如甲苯，二甲苯等中或在不存在溶剂的情况下，将式I化合物（X为H，卤素，低级烷基，低级烷氧基等）的化合物与N-甲基苄胺反应，得到具有改善的药物作用的式II化合物所示的目标化合物，例如血管舒张作用，抗高血压作用等，在工业上有利。通过使式III（R'为Me）表示的化合物与式IV所示的化合物反应，通过使式I所示的化合物以高收率得到，具有非常高的反应性并且易与N-甲基苄基胺反应。

6. 发明专利

JPS6193161A Production of dihydropyridine derivative 失效
标题翻译：二氢吡啶衍生物的生产
公开(公告)号：JPS6193161A
公开(公告)日：1986-05-12
申请号：JP21553384
申请日：1984-10-15
申请人： Maruko Seiyaku Kk
发明人： ONO SACHIO , EBIHARA YUUKO , MIZUKOSHI SEISHI , KOMATSU OSAMU
IPC分类号： C07D211/90
摘要： PURPOSE: To obtain nicardipine hydrochloride useful as a vasodilator, etc. in high yield, by reacting a 2-alkylsulfonyloxyethyl methyl 3,5-dicarboxylate corresponding to the aimed compound with N-methylbenzylamine.
CONSTITUTION: A compound shown by the formula I (R is lower alkyl) is reacted with N-methylbenzylamine in a solvent such as toluene, xylene, etc. inert to the reaction or in the absence of a solvent under heating to the aimed compound shown by the formula II having improved action such as vasodilating action, antihypertensive action, etc., in high yield industrially advantageously. The compound shown by the formula I has improved reactivity, and is easily reacted with N-methylbenzylamine. The compound shown by the formula I can be produced in high yield by reacting a compound shown by the formula III (R' is lower alkyl) with a compound shown by the formula RSO
2 Cl or (RSO
2 )
2 O.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：通过使相应于目标化合物的2-烷基磺酰氧基乙基甲基3,5-二羧酸酯与N-甲基苄基胺反应，以高产率获得用作血管扩张剂等的盐酸尼卡地平。构成：将式I化合物（R为低级烷基）与N-甲基苄胺在反应惰性的溶剂如甲苯，二甲苯等中反应，或在不加溶剂的情况下与所示目标化合物反应通过具有改善作用的式II，如血管扩张作用，抗高血压作用等，在工业上有利地以高产率。式I所示的化合物具有改善的反应性，并且容易与N-甲基苄胺反应。通式I所示的化合物（R'是低级烷基）与式RSO 2 Cl或（RSO 2）2 O所示的化合物反应，可以高产率制备式I化合物。

7. 发明专利

JPS6191169A Dihydropyridine derivative and its preparation 失效
标题翻译：二氢吡啶衍生物及其制备
公开(公告)号：JPS6191169A
公开(公告)日：1986-05-09
申请号：JP21163384
申请日：1984-10-09
申请人： Maruko Seiyaku Kk
发明人： ONO SACHIO , EBIHARA YUUKO , MIZUKOSHI SEISHI , KOMATSU OSAMU
IPC分类号： C07D211/90
摘要： NEW MATERIAL:The 1,4-dihydropyridine derivative of formula I (R
1 and R
2 are lower alkyl).
EXAMPLE: 2-Methanesulfonyloxyethyl methyl 1,4-dihydro-2,6-dimethyl-4-(3- nitrophenyl)pyridine-3,5-dicarboxylate.
USE: It has high reactivity and is used as a preparation intermediate of nicardipine hydrochloride known as a drug having vasodilating and antihypertensive activities, etc.
PREPARATION: The compound of formula I can be prepared easily in thigh yield, by reacting the compound of formula II with the sulfonic acid derivative of formula R
2 SO
2 Cl or (R
2 SO
2 )O in a solvent inert to the reaction such as tetrahydrofuran or in the absence of solvent, in the presence of a base such as triethylamine.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：新材料：式I的1,4-二氢吡啶衍生物（R 1和R 2是低级烷基）。实施例：2-甲磺酰氧基乙基1,4-二氢-2,6-二甲基-4-（3-硝基苯基）吡啶-3,5-二羧酸甲酯。用途：具有高反应性，用作盐酸尼卡地平，称为具有血管扩张和抗高血压活性的药物的制剂中间体。制备：式Ⅰ化合物可以通过使式II化合物与式R 2 SO 2 Cl或（R 2 SO 2）O的磺酸衍生物在反应惰性的溶剂如四氢呋喃中或在不存在溶剂的条件下，在碱如三乙胺存在下反应。

8. 发明专利

JPS592280B2 JPS592280B2 - 失效
公开(公告)号：JPS592280B2
公开(公告)日：1984-01-18
申请号：JP241980
申请日：1980-01-11
申请人： Maruko Seiyaku Kk , Mamoru Sugiura
发明人： SUGIURA MAMORU , SAWAKI SHUNJI , KATO KENJI , HIRANO KAZUYUKI , ITO YOSHIMASA , ADACHI TETSUO
IPC分类号： G01N33/50 , C12Q1/26 , C12Q1/34 , C12Q1/37 , C12Q1/48 , C12Q1/68 , G01N31/22

9. 发明专利

JPS58201764A Dihydropyridine derivative 失效
标题翻译：二氢吡啶衍生物
公开(公告)号：JPS58201764A
公开(公告)日：1983-11-24
申请号：JP8284782
申请日：1982-05-17
申请人： Maruko Seiyaku Kk
发明人： OONO SACHIO , MIZUKOSHI SEISHI , KOMATSU OSAMU , ICHIHARA KENJI , MORISHIMA TAKASHI
IPC分类号： C07D211/90 , A61K31/455 , A61P9/08 , A61P9/12
摘要： NEW MATERIAL:The 1,4-dihydropyridine derivative of formula I (R is lower alkyl such as methyl, ethyl, propyl, etc.).
EXAMPLE: 2-Hydroxyethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.
USE: Vasodilator. It has hypotensive activity and useful as a drug. Useful also as a synthetic intermediate of other pharmacologically active substance. If has low toxicity.
PROCESS: The compound of formula I can be prepared by reacting ethylene glycol with diketene in the presence of a base, and without separating the reaction product, further reacting with 3-nitrobenzaldehyde and a β-aminocrotonate of formula II.
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：式I的1,4-二氢吡啶衍生物（R是低级烷基，例如甲基，乙基，丙基等）。实施例：2,6-二甲基-4-（3-硝基苯基）-1,4-二氢吡啶-3,5-二甲酸二羟乙酯。用途：血管扩张剂它具有低血压活性，作为药物有用。也可用作其他药理活性物质的合成中间体。毒性低。方法：式I化合物可以通过使乙二醇与双烯酮在碱的存在下反应而制备，并且不分离反应产物，进一步与式II的3-硝基苯甲醛和β-氨基巴豆酸酯反应。

10. 发明专利

JPS5767544A Improved preparation of 1-2(allylphenyxy)-3-isopropylaminopropan-2-ol 失效
标题翻译：改进制备1-2（全甲基）-3-异丙基氨基酚-2-OL
公开(公告)号：JPS5767544A
公开(公告)日：1982-04-24
申请号：JP14265480
申请日：1980-10-13
申请人： Maruko Seiyaku Kk
发明人： OONO SACHIO , MIZUKOSHI SEISHI , KOMATSU OSAMU
IPC分类号： C07D263/24 , C07C67/00 , C07C213/00 , C07C217/32
摘要： PURPOSE: To obtain the titled compound useful as an antiarrhythmic agent easily in high yield at a low cost, by reacting 3-isopropylamino-1,2-propanediol as a starting material with ethyl carbonate, and converting the resultant novel intermediate oxazolidinone derivative into the titled compound.
CONSTITUTION: 3-Isopropylamino-1,2-propanediol of formulaIis reacted with ethyl carbonate to give a 5-hydroxymethyl-3-isopropyl-2-oxazolidinone of formula II, which is then reacted with p-toluenesulfonyl chloride in pyridine at room temperature to afford a compound of formula III. The resultant compound of formula III is reacted with an alkaline metallic salt of 2-allylphenol in DMF at 60W100°C to give a compound of formula IV, which is then refluxed in a mixed solution of 4N- NaOH-ethanol (1:3) to afford the aimed compound of formula V. The optimal concentration of the alkali is such that the final concentration of 1N is reached. The concentration higher than the valve or a temperature of 100°C or above causes the isomerization of the alkyl group.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：目的：以3-异丙基氨基-1,2-丙二醇为起始原料与碳酸乙酯反应，以低成本容易地获得用作抗心律失常药物的标题化合物，将所得新型中间体恶唑烷酮衍生物转化为标题化合物。构型：式I的3-异丙基氨基-1,2-丙二醇与碳酸乙酯反应得到式II的5-羟甲基-3-异丙基-2-恶唑烷酮，然后与对甲苯磺酰氯在吡啶中在室温下反应至得到式III化合物。所得到的式III化合物与2-烯丙基苯酚的碱金属盐在DMF中在60-100℃反应，得到式Ⅳ化合物，然后将其在4N-NaOH-乙醇（1 ：3）得到目标化合物V。碱的最佳浓度使得达到最终浓度为1N。浓度高于阀门或温度为100℃以上时，会导致烷基异构化。

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