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1. 发明授权

US5948914A Piperidine derivative and process for preparing the same 失效
标题翻译：哌啶衍生物及其制备方法
公开(公告)号：US5948914A
公开(公告)日：1999-09-07
申请号：US53653
申请日：1998-04-02
申请人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
发明人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
IPC分类号： C07D211/22 , C07D211/60 , C07D211/76 , C07D405/12
CPC分类号： C07D405/12 , C07D211/22 , C07D211/60 , C07D211/76
摘要： A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R.sup.2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or --CO.sub.2 R.sup.7 group in which R.sup.7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group.
摘要翻译：哌啶衍生物，其可以用作药物的中间体，例如用作抗抑郁药的帕罗西汀，由通式（I）表示：其中R1是氢原子，苄氧基羰基或叔丁氧基羰基; R2是羟甲基，具有1〜2个碳原子的烷基部分的烷基磺酰氧基甲基，4-位可具有甲基的苯基磺酰氧基甲基，（3,4-亚甲二氧基苯基）氧甲基，羧基或-CO 2 R 7基，其中 R 7为碳原子数为1〜5的烷基，Z为亚甲基或羰基。

2. 发明授权

US06815548B2 Process for preparing a piperidine derivative 失效
标题翻译：哌啶衍生物的制备方法
公开(公告)号：US06815548B2
公开(公告)日：2004-11-09
申请号：US10336678
申请日：2003-01-06
申请人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
发明人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
IPC分类号： C07D40512
CPC分类号： C07D405/12 , C07D211/22 , C07D211/60 , C07D211/76
摘要： A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is carbonyl group, then R2 is carboxyl group or —CO2R7 group (R7 is as defined above); or (C) when R1 is hydrogen atom and Z is methylene group, then R2 is hydroxymethyl group.

3. 发明授权

US06610851B1 Process for preparing a piperidine derivative 失效
标题翻译：哌啶衍生物的制备方法
公开(公告)号：US06610851B1
公开(公告)日：2003-08-26
申请号：US09695383
申请日：2000-10-25
申请人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
发明人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
IPC分类号： C07D40512
CPC分类号： C07D405/12 , C07D211/22 , C07D211/60 , C07D211/76
摘要： A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is carbonyl group, then R2 is carboxyl group or —CO2R7 group (R7 is as defined above); or (C) when R1 is hydrogen atom and Z is methylene group, then R2 is hydroxymethyl group.
摘要翻译：哌啶衍生物，其可以用作药物的中间体，例如用作抗抑郁药的帕罗西汀，由通式（I）表示：其中R1是氢原子，苄氧基羰基或叔丁氧基羰基; R2是羟甲基，具有1〜2个碳原子的烷基部分的烷基磺酰氧基甲基，4-位可具有甲基的苯基磺酰氧基甲基，（3,4-亚甲二氧基苯基）氧甲基，羧基或-CO 2 R 7基，其中 R7为碳原子数为1〜5的烷基，Z为亚甲基或羰基，条件是（A）当R1为苄氧羰基或叔丁氧基羰基时，则R2为羟甲基，烷基磺酰氧基甲基为具有1至2个碳原子的烷基部分，可以在4-位具有甲基的苯基磺酰氧基甲基或（3,4-亚甲二氧基苯基）氧基甲基，Z是亚甲基; 或（B）当R 1为氢原子且Z为羰基时，则R 2为羧基或-CO 2 R 7基（R 7如上所定义）; 或（C）当R 1为氢原子且Z为亚甲基时，则R 2为羟甲基。

4. 发明授权

US06476227B1 Piperidine derivative and process for preparing the same 失效
标题翻译：哌啶衍生物及其制备方法
公开(公告)号：US06476227B1
公开(公告)日：2002-11-05
申请号：US09550175
申请日：2000-04-14
申请人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
发明人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
IPC分类号： C07D21140
CPC分类号： C07D405/12 , C07D211/22 , C07D211/60 , C07D211/76
摘要： A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is carbonyl group, then R2 is carboxyl group or —CO2R7 group (R7 is as defined above); or (C) when R1 is hydrogen atom and Z is methylene group, then R2 is hydroxymethyl group.
摘要翻译：哌啶衍生物，其可以用作药物的中间体，例如用作抗抑郁药的帕罗西汀，由通式（I）表示：其中R1是氢原子，苄氧基羰基或叔丁氧基羰基; R2是羟甲基，具有1〜2个碳原子的烷基部分的烷基磺酰氧基甲基，4-位可具有甲基的苯基磺酰氧基甲基，（3,4-亚甲二氧基苯基）氧甲基，羧基或-CO 2 R 7基，其中 R7为碳原子数为1〜5的烷基，Z为亚甲基或羰基，条件是（A）当R1为苄氧羰基或叔丁氧基羰基时，则R2为羟甲基，烷基磺酰氧基甲基为具有1至2个碳原子的烷基部分，可以在4-位具有甲基的苯基磺酰氧基甲基或（3,4-亚甲二氧基苯基）氧基甲基，Z是亚甲基; 或（B）当R 1为氢原子且Z为羰基时，则R 2为羧基或-CO 2 R 7基（R 7如上所定义）; 或（C）当R 1为氢原子且Z为亚甲基时，则R 2为羟甲基。

5. 发明授权

US06316628B1 L-tartrate of trans-(-)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound and process for preparing the same 失效
标题翻译：反式 - （ - ） - 4-（4-氟苯基）-3-羟甲基哌啶化合物的L-酒石酸盐及其制备方法
公开(公告)号：US06316628B1
公开(公告)日：2001-11-13
申请号：US09342149
申请日：1999-06-29
申请人： Shigeya Yamazaki , Taro Ishibashi , Yoshihiro Kawada , Hiroyuki Yumoto , Taichi Yoshikawa , Masami Igi
发明人： Shigeya Yamazaki , Taro Ishibashi , Yoshihiro Kawada , Hiroyuki Yumoto , Taichi Yoshikawa , Masami Igi
IPC分类号： C07D21122
CPC分类号： C07D211/22
摘要： An L-tartrate of a trans-(−)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound, represented by the formula (I): wherein R1 is hydrogen atom, a substituted or unsubstituted, linear or branched alkyl group having 1 to 6 carbon atoms, or an aralkyl group having 7 to 12 carbon atoms. The L-tartrate of trans-(−)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound can be suitably used as an intermediate for pharmaceuticals such as paroxetine which is useful, for example, as an antidepressant.
摘要翻译：由式（I）表示的反 - （ - ） - 4-（4-氟苯基）-3-羟甲基哌啶化合物的L-酒石酸盐：其中R1是氢原子，取代或未取代的直链或支链烷基，其具有 1至6个碳原子，或具有7至12个碳原子的芳烷基。反式 - （ - ） - 4-（4-氟苯基）-3-羟甲基哌啶化合物的L-酒石酸盐可以适当地用作药物例如帕罗西汀的中间体，其可用作例如抗抑郁药。

6. 发明授权

US06433168B1 Highly pure phenothiazine compound, production method thereof, production method of intermediate therefor, and hydrate and novel crystal as starting materials for the intermediate 失效
标题翻译：高纯吩噻嗪化合物，其制备方法，其中间体的制备方法，水合物和新型晶体为中间体的起始原料
公开(公告)号：US06433168B1
公开(公告)日：2002-08-13
申请号：US09621782
申请日：2000-07-21
申请人： Shigeya Yamazaki , Hiroyuki Yumoto , Masami Igi
发明人： Shigeya Yamazaki , Hiroyuki Yumoto , Masami Igi
IPC分类号： C07D41700
CPC分类号： C07D453/02
摘要： According to the method of the present invention, an alkali metal compound, dimethyl sulfoxide, trimethyloxosulfonium halide and 3-quinuclidinone are added in a specific order to give the following compound [II]. This compound is, without treatment or isolation, directly reacted with an alkali metal salt of phenothiazine to give the following compound [III], from which the following compound [I] is obtained. During the production of compound [I], a by-produced acidic gas is removed and water is added to ensure industrial, safe and efficient production of compound [I] at a constantly high yield. Inasmuch as the present invention enables production of the following highly pure compound [A] by eliminating hydrogen halide of compound [I] in glyme in the presence of at least one kind of a base selected from potassium hydroxide and potassium alkoxide, compound [A] having a high purity of not less than 85 mol % can be provided.
摘要翻译：根据本发明的方法，以特定的顺序加入碱金属化合物，二甲基亚砜，三甲基锍卤化物和3-奎宁环酮，得到下列化合物[II]。该化合物在不经处理或分离的情况下与吩噻嗪的碱金属盐直接反应，得到以下化合物[III]，由此得到下列化合物[I]。在化合物[I]的生产过程中，除去副产的酸性气体，加入水以确保化合物[I]的工业，安全和有效的生产以不断的高产率。由于本发明能够通过在至少一种选自氢氧化钾和醇钾的碱的存在下，通过除去甘醇二甲醚中的化合物[I]的卤化氢来制备下列高纯度化合物[A]，化合物[A] 可以提供不小于85mol％的高纯度。

7. 发明申请

US20090118542A1 Process for Production of Optically Active Carboxlic Acid Compound 审中-公开
标题翻译：光活性羧酸化合物的制备方法
公开(公告)号：US20090118542A1
公开(公告)日：2009-05-07
申请号：US12224043
申请日：2007-02-15
申请人： Shigeya Yamazaki , Takeshi Hosoya
发明人： Shigeya Yamazaki , Takeshi Hosoya
IPC分类号： C07C51/00
CPC分类号： C07D275/06 , C07B53/00 , C07B2200/07 , C07C51/06 , C07C57/03
摘要： An optically active acylated camphorsultam can be hydrolyzed with an aqueous solution of an alkaline earth metal hydroxide in the presence of a branched alkanol, to give a corresponding optically active carboxylic acid compound in safely and inexpensively.
摘要翻译：光学活性的酰化樟脑磺酸钠可以在碱性金属氢氧化物的水溶液中在支链烷醇的存在下水解，得到相应的光学活性羧酸化合物，其安全且廉价。

8. 发明申请

US20060048696A1 Methods of crystal precipitation 失效
标题翻译：晶体析出方法
公开(公告)号：US20060048696A1
公开(公告)日：2006-03-09
申请号：US10527317
申请日：2003-09-17
申请人： Shigeya Yamazaki , Taichi Yoshikawa
发明人： Shigeya Yamazaki , Taichi Yoshikawa
IPC分类号： H01L21/322 , C30B15/14
CPC分类号： C07D263/58 , C07D405/12
摘要： Crystals of paroxetine hydrochloride ½-hydrate are allowed to separate out by adding water to a solution or suspension comprising paroxetine hydrochloride and a polar organic solvent which contains no water or at most 60% by weight of water to adjust the water content to at least 70% by weight when crystals of paroxetine hydrochloride ½-hydrate are allowed to separate out in a water-containing polar organic solvent. Crystals of paroxetine hydrochloride ½-hydrate being not colored in pink can be allowed to separate out in the presence of hydrogen chloride when crystals of paroxetine hydrochloride ½-hydrate are allowed to separate out in water or a water-containing polar organic solvent.
摘要翻译：通过向包含盐酸帕罗西汀和不含水或至多60重量％水的极性有机溶剂的溶液或悬浮液中加入水分离使水分含量达到至少70，允许盐酸帕罗西汀水合物晶体分离出来使盐酸帕罗西汀1/2水合物的晶体在含水极性有机溶剂中分离出来时的重量％。当盐酸帕罗西汀1/2水合物的结晶在水或含水极性有机溶剂中分离出来时，盐酸帕罗西汀晶体可以在氯化氢存在下将不着色的粉红色半水合物分离出来。

9. 发明授权

US07329318B2 Methods of crystal precipitation 失效
标题翻译：晶体析出方法
公开(公告)号：US07329318B2
公开(公告)日：2008-02-12
申请号：US10527317
申请日：2003-09-17
申请人： Shigeya Yamazaki , Taichi Yoshikawa
发明人： Shigeya Yamazaki , Taichi Yoshikawa
IPC分类号： C30B7/04
CPC分类号： C07D263/58 , C07D405/12
摘要： Crystals of paroxetine hydrochloride ½-hydrate are allowed to separate out by adding water to a solution or suspension comprising paroxetine hydrochloride and a polar organic solvent which contains no water or at most 60% by weight of water to adjust the water content to at least 70% by weight when crystals of paroxetine hydrochloride ½-hydrate are allowed to separate out in a water-containing polar organic solvent. Crystals of paroxetine hydrochloride ½-hydrate being not colored in pink can be allowed to separate out in the presence of hydrogen chloride when crystals of paroxetine hydrochloride ½-hydrate are allowed to separate out in water or a water-containing polar organic solvent.
摘要翻译：通过向包含盐酸帕罗西汀和不含水或至多60重量％水的极性有机溶剂的溶液或悬浮液中加入水分离使水分含量达到至少70，允许盐酸帕罗西汀水合物晶体分离出来使盐酸帕罗西汀1/2水合物的晶体在含水极性有机溶剂中分离出来时的重量％。当盐酸帕罗西汀1/2水合物的结晶在水或含水极性有机溶剂中分离出来时，盐酸帕罗西汀晶体可以在氯化氢存在下将不着色的粉红色半水合物分离出来。

10. 发明申请

US20060041138A1 Process for producing paroxetine hydrochloride hydrate 审中-公开
标题翻译：盐酸帕罗西汀水合物的制备方法
公开(公告)号：US20060041138A1
公开(公告)日：2006-02-23
申请号：US10527337
申请日：2003-09-17
申请人： Shigeya Yamazaki , Taichi Yoshikawa
发明人： Shigeya Yamazaki , Taichi Yoshikawa
IPC分类号： C07D407/02
CPC分类号： C07D405/12
摘要： A process for preparing a paroxetine hydrochloride hydrate, comprising reacting (3S, 4R)-1-tert-butoxycarbonyl-4-(4-fluorophenyl)-3-[(3,4-methylene-dioxy)phenoxymethyl]piperidine with hydrogen chloride in the presence of water, and allowing crystals to separate out from the resulting reaction mixture in the presence of water.
摘要翻译：一种制备盐酸帕罗西汀水合物的方法，包括使（3S，4R）-1-叔丁氧基羰基-4-（4-氟苯基）-3 - [（3,4-亚甲基 - 二氧基）苯氧基甲基]哌啶与氯化氢反应水的存在，并允许晶体在水存在下从所得反应混合物中分离出来。

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