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1. 发明授权

US07091206B2 Process for producing pyrimidine derivative and intermediate thereof 失效
标题翻译：制备嘧啶衍生物及其中间体的方法
公开(公告)号：US07091206B2
公开(公告)日：2006-08-15
申请号：US10363232
申请日：2001-09-07
申请人： Toshio Tomita
发明人： Toshio Tomita
IPC分类号： C07D239/42
CPC分类号： C07D239/34
摘要： The present invention relates to a method for producing a pyrimidine derivate useful as a neurocyte neurocyte necrosis inhibitor and an intermediate thereof. Disclosed is a method for producing an acid salt of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy) pyrimidine. The method comprises reacting 4-chloro-6-(4-fluorophenyl)-2-methylpyrimidine with 5-piperidino-1-pentanol, hydrating the thus obtained 4-(4-fluorophenyl)-2-mehtyl-6-(5-piperidinopentylox) pyrimidine and then converting the resultant the hydrate into an acid salt. The hydrate as a describe above; and a method for producing the hydrate is part of this invention. According to the present invention, a highly pure acid salt of 4-(4-fluorophenyl)-2-methyl-6-(5-piperidinopentyloxy) pyrimidine can be readily and efficiently produced without using a column chromatography. Thus, this method is suitable for the production thereof on a industrial scale.
摘要翻译：本发明涉及可用作神经细胞神经细胞坏死物抑制剂的嘧啶衍生物及其中间体的制备方法。公开了4-（4-氟苯基）-2-甲基-6-（5-哌啶基戊氧基）嘧啶酸盐的制备方法。该方法包括使4-氯-6-（4-氟苯基）-2-甲基嘧啶与5-哌啶子基-1-戊醇反应，将由此得到的4-（4-氟苯基）-2-甲基-6-（5-哌啶子戊酸）嘧啶，然后将所得水合物转化为酸盐。水合物如上所述; 水合物的制造方法是本发明的一部分。根据本发明，可以容易且高效地制备4-（4-氟苯基）-2-甲基-6-（5-哌啶基戊氧基）嘧啶的高纯度酸盐，而不使用柱色谱法。因此，该方法适合于以工业规模生产。

2. 发明授权

US4857515A Certain antihypertensive 1,4-dihydro-6-methyl-5-phosphonic acid-4-aryl-3-carboxylic acid-2-cyano diesters 失效
标题翻译：某些抗高血压的1,4-二氢-6-甲基-5-膦酸-4-芳基-3-羧酸-2-氰基二酯
公开(公告)号：US4857515A
公开(公告)日：1989-08-15
申请号：US115170
申请日：1987-10-30
申请人： Kiyoshi Kimura , Masahiro Kise , Iwao Morita , Toshio Tomita , Masami Tsuda
发明人： Kiyoshi Kimura , Masahiro Kise , Iwao Morita , Toshio Tomita , Masami Tsuda
IPC分类号： C07F9/58 , A61K31/675 , A61P9/08 , A61P9/12 , C07F9/59
CPC分类号： C07F9/597
摘要： A compound of formula (I): ##STR1## wherein R.sup.1 is alkenyl or alkyl or both of the depicted R.sup.1 groups together represent trimethylene and form a six-membered ring together with the depicted oxygen and phosphorus atoms, R.sup.2 is nitro, trifluoromethyl or halogen, R.sup.3 is alkyl, and R.sup.4 is dimethoxymethyl, formyl, hydroxymethyl or nitrile.
摘要翻译：式（I）的化合物：其中R 1是烯基或烷基或所描述的R 1基团两者一起表示三亚甲基，并与所描述的氧和磷原子一起形成六元环，R 2是硝基，三氟甲基或卤素，R 3是烷基，R 4是二甲氧基甲基，甲酰基，羟甲基或腈。

3. 发明授权

US3991186A Steryl-.beta.-D-glucoside ester pharmaceutical compositions and method of use 失效
标题翻译：（62-D-糖苷酯）药物组合物及其使用方法
公开(公告)号：US3991186A
公开(公告)日：1976-11-09
申请号：US603085
申请日：1975-08-08
申请人： Hiromu Murai , Koji Kitaguchi , Tatsuo Suminokura , Akira Sano , Massahiro Kise , Masahiko Kitano , Toshio Tomita
发明人： Hiromu Murai , Koji Kitaguchi , Tatsuo Suminokura , Akira Sano , Massahiro Kise , Masahiko Kitano , Toshio Tomita
IPC分类号： C07J17/00 , C07J19/00
CPC分类号： C07J17/005
摘要： Steryl-6-O-palnitoyl and -2,3,4,6-O-tetrapalmitoyl-.beta.-D-glucosides are anti-inflammatory agents. The compounds, of which .beta.-sitosteryl-2,3,4,6-O-tetrapalmitoyl-.beta.-D-glucoside is a representative embodiment, are prepared through the reaction of a steryl-.beta.-D-glucoside with a lower alkyl ester of palmitic acid in the presence of a basic catalyst.
摘要翻译： Steryl-6-O- palnitoyl和-2,3,4,6-O-四棕榈酰-β-D-糖苷是抗炎剂。 β-淀粉-2,3,4,6-O-四棕榈酰-β-D-葡萄糖苷是其代表性实施方案的化合物通过将甾体-β-D-葡萄糖苷与低级烷基酯的棕榈酸在碱性催化剂存在下进行。

4. 发明授权

US5102882A Pyroglutamide derivatives 失效
标题翻译：吡咯烷酮衍生物
公开(公告)号：US5102882A
公开(公告)日：1992-04-07
申请号：US661523
申请日：1991-02-26
申请人： Koyishi Kimura , Shoichi Chokai , Toshio Tomita , Masahiro Kise , Kenichi Nakamura
发明人： Koyishi Kimura , Shoichi Chokai , Toshio Tomita , Masahiro Kise , Kenichi Nakamura
IPC分类号： C07D207/28 , C07D401/06 , C07D401/12 , C07D403/06 , C07D407/12 , C07D409/12
CPC分类号： C07D401/06 , C07D207/28 , C07D401/12 , C07D403/06 , C07D407/12 , C07D409/12
摘要： Pyroglutamide derivatives have been found to be useful as nootropic agents for administration to humans and animals.
摘要翻译：已经发现焦呋喃酰胺衍生物可用作用于给予人和动物的诱导剂。

5. 发明授权

US4642307A 1-phenoxy-3-(4-phenylpiperidino)-2-propand having both alpha- and beta-adrenergic action 失效
标题翻译：具有α-和β-肾上腺素能作用的1-苯氧基-3-（4-苯基哌啶子基）-2-丙酸
公开(公告)号：US4642307A
公开(公告)日：1987-02-10
申请号：US476857
申请日：1983-03-18
申请人： Yoshiaki Aoyagi , Takashi Okubo , Toshio Tomita , Hiroshi Nishida , Hiroshi Enomoto
发明人： Yoshiaki Aoyagi , Takashi Okubo , Toshio Tomita , Hiroshi Nishida , Hiroshi Enomoto
IPC分类号： C07D295/08 , A61K31/495 , A61P9/12 , C07D295/092 , C07D295/155 , C07D303/22 , C07D401/00
CPC分类号： C07D295/088 , C07D295/155 , C07D303/22
摘要： 1-phenoxy-3-(4-phenylpiperazino)-2-propanol derivatives of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 is hydrogen, halo or lower alkyl; R.sup.2 is pyrrolidino, piperidino, morpholino or perhydroazepino unsubstituted or substituted by carbonyl at the alpha-position; R.sup.3 is hydrogen, lower alkyl or lower alkoxycarbonyl; and R.sup.4 is hydrogen, lower alkyl unsubstituted or alpha-substituted by lower alkoxy, lower alkoxy, halo or lower alkanoyl are useful for their alpha and beta-adrenergic blocking action and their hypotensive activity in humans and animals.
摘要翻译：式（I）的1-苯氧基-3-（4-苯基哌嗪基）-2-丙醇衍生物：其中R 1是氢，卤素或低级烷基; R2是吡咯烷子基，哌啶子基，吗啉代或全氢氮杂基，未被取代或被α-位上的羰基取代; R3是氢，低级烷基或低级烷氧基羰基; R4是氢，低级烷氧基，低级烷氧基，卤素或低级烷酰基被α-取代的低级烷基用于人和动物的α和β-肾上腺素能阻断作用及其降血压活性。

6. 发明授权

US4031303A Steryl-.beta.-D-glucoside esters and method of preparation 失效
标题翻译：甾体 - {62 -D-糖苷酯及其制备方法
公开(公告)号：US4031303A
公开(公告)日：1977-06-21
申请号：US603110
申请日：1975-08-08
申请人： Hiromu Murai , Koji Kitaguchi , Tatsuo Suminokura , Akira Sano , Masahiro Kise , Masahiko Kitano , Toshio Tomita
发明人： Hiromu Murai , Koji Kitaguchi , Tatsuo Suminokura , Akira Sano , Masahiro Kise , Masahiko Kitano , Toshio Tomita
IPC分类号： C07J17/00 , C07G17/00
CPC分类号： C07J17/005 , Y10S514/87
摘要： Steryl-6-0-palmitoyl-.beta.-D-glucosides are anti-inflammatory agents. The compounds, of which .beta.-sitosteryl-6-0-palmitoyl-.beta.-D-glucoside is a representative embodiment, are prepared through the reaction of a steryl-6-0-sulfonyl-.beta.-D-glucoside with an alkali metal salt of palmitic acid.
摘要翻译： Steryl-6-0-棕榈酰-β-D-糖苷是抗炎剂。其中β-谷甾基-6-0-棕榈酰-β-D-葡萄糖苷是代表性实施方案的化合物是通过将甾-6-基 - 磺酰基-β-D-葡萄糖苷与一种碱金属盐的棕榈酸。

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