公开(公告)号：US06245911B1

公开(公告)日：2001-06-12

申请号：US09555807

申请日：2000-06-05

申请人： Akio Imai ,  Toshiyuki Ichinohe ,  Takashi Endo ,  Tomio Tsurugi ,  Makoto Uemura

发明人： Akio Imai ,  Toshiyuki Ichinohe ,  Takashi Endo ,  Tomio Tsurugi ,  Makoto Uemura

IPC分类号： C07D21106

CPC分类号： C07D211/32

摘要： The present invention provides novel polymorphic crystals (A) to (C) having excellent handling properties and an extremely low content of residual solvent of donepezil used as a precursor for production of donepezil hydrochloride having an excellent action as a medicament, and an industrial process for producing the same. Further, the novel polymorphic crystals (A) to (C) according to the present invention are characterized by the powder X-ray diffraction pattern and/or IR absorption peaks of donepezil represented by the following formula:

摘要翻译： 本发明提供了具有优异的操作性和作为药物用作为优良作用的盐酸多奈哌齐的前体的多奈哌齐含量极低的新型多晶型（A）〜（C） 生产相同。 此外，根据本发明的新型多晶型晶体（A）至（C）的特征在于由下式表示的多奈哌齐的粉末X射线衍射图和/或IR吸收峰：

公开(公告)号：US20110105759A1

公开(公告)日：2011-05-05

申请号：US11996741

申请日：2006-07-24

申请人： Akio Imai ,  Akihiko Shimotani ,  Tomio Tsurugi ,  Yukio Narabu

发明人： Akio Imai ,  Akihiko Shimotani ,  Tomio Tsurugi ,  Yukio Narabu

IPC分类号： C07D211/08

CPC分类号： C07D211/32

摘要： It is intended to provide a process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methylpiperidine represented by the structural formula (I): (I) which is useful as an intermediate material for a pharmaceutical or a solvate thereof in which impurity content is further reduced and operation is simple and suitable for industrial production by reacting 5,6-dimethoxy-1-indanone with 1-benzyl-4-formylpiperidine in a reaction solvent in the presence of a base and then gradually crystallizing a target substance in a reaction mixture in a high temperature region.

摘要翻译： 本发明提供一种制备由结构式（I）表示的1-苄基-4 - [（5,6-二甲氧基-1-茚满酮）-2-亚基]甲基哌啶的方法：（I），其可用作 药物或溶剂化物的中间体材料，其中杂质含量进一步降低并且操作简单并且适合于通过使5,6-二甲氧基-1-二氢茚酮与1-苄基-4-甲酰基哌啶在反应溶剂中反应的工业生产 碱的存在，然后在高温区域的反应混合物中逐渐结晶目标物质。

公开(公告)号：US07795438B2

公开(公告)日：2010-09-14

申请号：US10580908

申请日：2005-04-27

申请人： Akio Imai ,  Hiroshi Nishimura

发明人： Akio Imai ,  Hiroshi Nishimura

IPC分类号： C07D211/32

CPC分类号： C07D211/32 ,  B01J25/02

摘要： Processes for preparing 1-benzyl-4-[(5,6-dimethoxy-lindanon)-2-yl]methylpiperidine (donepezil), which is useful as an intermediate for medicines, and for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride (donepezil hydrochloride), which is useful as a medicine. The process for donepezil hydrochloride production comprises catalytically hydrogenating the compound represented by the structural formula (III) [1-benzyl-4-[(5,6-dimethoxy-lindanon)-2-ylidene]methylpiperidine] with a Raney nickel catalyst under mild conditions and subsequently treating it with hydrochloric acid. Thus, impurities are further diminished. The operations are simple and the process is suitable for industrial production.

摘要翻译： 用于制备1-苄基-4 - [（5,6-二甲氧基 - 茚满酮）-2-基]甲基哌啶（多奈哌齐）的方法，其可用作药物的中间体，并用于制备1-苄基-4 - [（5 ，6-二甲氧基-1-茚满酮）-2-基]甲基哌啶盐酸盐（盐酸多奈哌齐），其可用作药物。 盐酸多奈哌齐的方法包括用温和的阮内镍催化剂催化氢化由结构式（III）[1-苄基-4 - [（5,6-二甲氧基 - 茚满酮）-2-亚基]甲基哌啶]代表的化合物 然后用盐酸处理。 因此，杂质进一步减少。 操作简单，适用于工业生产。

公开(公告)号：US20090171094A1

公开(公告)日：2009-07-02

申请号：US11994494

申请日：2006-07-12

申请人： Kazuhide Ashizawa ,  Akio Imai

发明人： Kazuhide Ashizawa ,  Akio Imai

IPC分类号： C07D211/32

CPC分类号： C07D211/32

摘要： 1-Benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine p-toluenesulfonate or a solvate thereof.

摘要翻译： 1-苄基-4 - [（5,6-二甲氧基-1-茚满酮）-2-基]甲基哌啶对甲苯磺酸盐或其溶剂合物。

公开(公告)号：US20080306272A1

公开(公告)日：2008-12-11

申请号：US12121454

申请日：2008-05-15

申请人： Naoyuki Shimomura ,  Seiji Yoshikawa ,  Yoshihiko Hisatake ,  Akio Imai

发明人： Naoyuki Shimomura ,  Seiji Yoshikawa ,  Yoshihiko Hisatake ,  Akio Imai

IPC分类号： C07D401/02

CPC分类号： C07D401/10 ,  Y02P20/55

摘要： A compound represented by the following formula (1): wherein R represents a 4-fluorophenyl group and the like; Q represents —CH(CH3)— and the like; and n represents 1 and the like and a pharmaceutically acceptable salt thereof can be prepared in one-pot by reacting a compound represented by the following formula (2): wherein R1 represents a 4-fluorophenyl group and the like; and Q and n have the same meaning as described above, with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base and, if necessary, removing a protecting group.

摘要翻译： 由下式（1）表示的化合物：其中R表示4-氟苯基等; Q表示-CH（CH 3） - 等; 和n表示1等的化合物及其药学上可接受的盐可以通过使由下式（2）表示的化合物反应而制备：其中R1表示4-氟苯基等; 和Q和n具有与上述相同的含义，与3-甲氧基-4-（4-甲基-1H-咪唑-1-基）苯甲醛在碱存在下反应，如果需要，除去保护基。

公开(公告)号：US20070088055A1

公开(公告)日：2007-04-19

申请号：US11546444

申请日：2006-10-12

申请人： Akio Imai

发明人： Akio Imai

IPC分类号： C07D211/06 ,  A61K31/445

CPC分类号： C07D211/32

摘要： 1-Benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine or hydrochloride thereof, which is useful as a drug, can be produced in high purity by safer and easier operations suitable for industrial production by subjecting 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methyl-piperidine or a solvate thereof to catalytic hydrogenation in the presence of a palladium-alumina catalyst and if necessary, converting the thus obtained compound to its hydrochloride.

摘要翻译： 可用作药物的1-苄基-4 - [（5,6-二甲氧基-1-茚满酮）-2-基]甲基哌啶或其盐酸盐可以通过适合于工业生产的更安全和更容易的操作而以高纯度制备 通过在钯 - 氧化铝催化剂的存在下使1-苄基-4 - [（5,6-二甲氧基-1-茚满酮）-2-亚基]甲基 - 哌啶或其溶剂合物进行催化氢化，如果需要， 从而得到化合物至其盐酸盐。

公开(公告)号：US06187883B1

公开(公告)日：2001-02-13

申请号：US08910830

申请日：1997-08-13

申请人： Makoto Satoh ,  Teruyoshi Kiyota ,  Akio Imai

发明人： Makoto Satoh ,  Teruyoshi Kiyota ,  Akio Imai

IPC分类号： C08F444

CPC分类号： C08F10/00 ,  C08F110/06 ,  Y10S526/908 ,  C08F4/6565 ,  C08F2500/17 ,  C08F2500/18

摘要： The present invention relates to a solid catalyst component for &agr;-olefin polymerization having a narrow particle size distribution of not less than 6.0 in terms of the value of N in a Rosin-Rammler function of particle size distribution and giving a catalytic activity of not less than 10,000 ((g-polymer produced/g-solid catalyst component)/hour) in polymerization. The catalyst component is obtained by a process which comprises reducing a titanium compound with an organomagnesium compound in the presence of an organosilicon compound and an ester to obtain a solid product, then treating the solid product with: (a) a mixture of titanium tetrachloride and an ether, (b) an organic acid halide, and (c) a mixture of titanium tetrachloride and an ether optionally containing an ester.

摘要翻译： 本发明涉及一种用于α-烯烃聚合的固体催化剂组分，其具有窄的粒度分布，在松散Rammler的粒度分布函数中的N值不小于6.0，并且给出的催化活性不低于 （（g-聚合物生产/ g-固体催化剂组分）/小时）。 催化剂组分通过包括在有机硅化合物和酯存在下还原钛化合物以获得固体产物的方法获得，然后用以下物质处理固体产物：（a）四氯化钛和 醚，（b）有机酰卤，和（c）任选含有酯的四氯化钛和醚的混合物。

公开(公告)号：US5854164A

公开(公告)日：1998-12-29

申请号：US731439

申请日：1996-10-15

申请人： Hiroyuki Shiraishi ,  Eiji Nakaishi ,  Takahiro Hino ,  Akio Imai

发明人： Hiroyuki Shiraishi ,  Eiji Nakaishi ,  Takahiro Hino ,  Akio Imai

IPC分类号： C08F4/651 ,  C08F4/653 ,  C08F4/654 ,  C08F10/00 ,  C08F210/16

CPC分类号： C08F10/00 ,  C08F210/16

摘要： A solid catalyst component (A) for olefin polymerization comprising Mg, Ti, a halogen and a cyclic organic nitrogen compound (C), a solid catalyst comprising the solid catalyst component and an organoaluminum compound, and a process for producing an olefin polymer with the catalyst. According to the present invention, there can be provided an olefin polymerization catalyst having a high catalyst activity per titanium enough to make the removal of catalyst residues unnecessary and a process for producing an olefin polymer having a low content of low molecular weight component with the catalyst.

摘要翻译： 包含Mg，Ti，卤素和环状有机氮化合物（C）的固体催化剂组分（A），包含固体催化剂组分和有机铝化合物的固体催化剂，以及烯烃聚合物的制备方法 催化剂。 根据本发明，可以提供一种对每个钛具有高催化活性的烯烃聚合催化剂，足以使催化剂残留物不必要地除去，以及用催化剂制备低含量低分子量组分的烯烃聚合物的方法 。

公开(公告)号：US5219938A

公开(公告)日：1993-06-15

申请号：US848095

申请日：1992-03-09

申请人： Akio Imai ,  Tomoaki Seki ,  Keisaku Yamamoto

发明人： Akio Imai ,  Tomoaki Seki ,  Keisaku Yamamoto

IPC分类号： B60C1/00 ,  C08C19/42

CPC分类号： B60C1/0016 ,  C08C19/42

摘要： A process for preparing modified diene polymer rubbers having an increased impact resilience, a reduced hardness at low temperatures and an improved processability, and useful as rubber materials for automobile tires and other industries which comprises producing a conjugated diene polymer having alkali metal end or ends, and reacting the alkali metal-containing polymer with (a) a silicon or tin compound of the formula: R.sub.a MX.sub.b wherein R is an alkyl group, an alkenyl group, a cycloalkenyl group or an aromatic hydrocarbon atom, a is 0, 1 or 2 and b is 2, 3 or 4, and (b) at least one member selected from the group consisting of a nitro compound; a phosphoryl chloride compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are an alkyl group; an aminosilane compound of the formula (2): ##STR2## wherein R.sup.5, R.sup.6 and R.sup.7 are an alkyl group or an alkoxyl group, R.sup.8 and R.sup.9 are an alkyl group, and n is an integer; an acrylamide compound of the formula (3): ##STR3## wherein R.sup.10 is hydrogen atom or methyl group, R.sup.11 and R.sup.12 are an alkyl group, and m is an integer; and an aminovinylsilane compound of the formula (4): ##STR4## wherein R.sup.13, R.sup.14, R.sup.15, R.sup.16 and R.sup.17 are an alkyl group.

摘要翻译： 一种制备具有增加的冲击弹性，在低温下降低的硬度和改善加工性能的改性二烯聚合物橡胶的方法，并且可用作汽车轮胎和其它工业的橡胶材料，其包括制备具有碱金属末端或末端的共轭二烯聚合物， 并使含碱金属的聚合物与（a）下式的硅或锡化合物：其中R是烷基，烯基，环烯基或芳族烃原子，其中R是一个或多个， b是2,3或4，和（b）至少一种选自硝基化合物; 式（1）的磷酰氯化合物：其中R1，R2，R3和R4是烷基; （2）的氨基硅烷化合物：其中R5，R6和R7是烷基或烷氧基，R8和R9是烷基，n是整数; 式（3）的丙烯酰胺化合物：其中R 10是氢原子或甲基，R 11和R 12是烷基，m是整数; 和式（4）的氨基乙烯基硅烷化合物：其中R 13，R 14，R 15，R 16和R 17是烷基。

公开(公告)号：US4981760A

公开(公告)日：1991-01-01

申请号：US378000

申请日：1989-07-11

申请人： Yukio Naito ,  Kohzoh Miyazaki ,  Yuji Gotoh ,  Masashi Hamba ,  Akio Imai ,  Kiyoyuki Sugimori

发明人： Yukio Naito ,  Kohzoh Miyazaki ,  Yuji Gotoh ,  Masashi Hamba ,  Akio Imai ,  Kiyoyuki Sugimori

IPC分类号： B32B27/32 ,  C08F10/00 ,  C08F110/02 ,  C08F210/02 ,  C08F210/16 ,  C08F297/08 ,  C08J5/18 ,  C08L23/00 ,  C08L23/06 ,  C08L23/08

CPC分类号： C08J5/18 ,  C08F210/02 ,  C08F210/16 ,  C08F297/08 ,  C08L23/0815 ,  C08F110/02 ,  C08J2323/08 ,  C08L23/06 ,  Y10T428/31855 ,  Y10T428/31938

摘要： An ethylene-.alpha.-olefin copolymer comprising ethylene and an .alpha.-olefin having from 3 to 10 carbon atoms, the copolymer having an .alpha.-olefin content of from 1.0 to 8.0 mol %, a density of from 0.900 to 0.930 g/cm.sup.3, and a melt flow rate of from 0.1 to 100 g/10 min., the programed-temperature thermogram of said copolymer as determined with a differential scanning calorimeter after being completely melted and then gradually cooled showing an endothermic peak (a) in a range of from 75.degree. to 100.degree. C. and an endothermic peak (b) in a range of from 120.degree. to 140.degree. C., with the ratio of an endotherm at the endothermic peak (b), .DELTA.Hb, to an endotherm at the endothermic peak (a), .DELTA.Ha, i.e., .DELTA.Hb/.DELTA.Ha, being from 0.03 to 2.0. The copolymer provides a film exhibiting excellent physical properties required for packaging film.