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1. 发明申请

WO2005040151A1 PYRAZINE DERIVATIVES AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：吡嗪衍生物及其药物用途
公开(公告)号：WO2005040151A1
公开(公告)日：2005-05-06
申请号：PCT/JP2004/016193
申请日：2004-10-25
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , YONISHI, Satoshi , AOKI, Satoshi , MATSUSHIMA, Yuji , AKAHANE, Atsushi
发明人： YONISHI, Satoshi , AOKI, Satoshi , MATSUSHIMA, Yuji , AKAHANE, Atsushi
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14
摘要： A pyrazine derivative of the following formula (I): or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer’s disease, cerebrovascular dementia, dementia accompanying Parkinson’s, disease, etc.), Parkinson’s disease, anxiety, pain, cerebrovascular disease (e.g. stroke), etc.), heart failure and the like.
摘要翻译：下式（I）的吡嗪衍生物或其盐。本发明的吡嗪化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁，痴呆（例如阿尔茨海默病，脑血管性痴呆，伴随帕金森病，疾病等的痴呆），帕金森病疾病，焦虑，疼痛，脑血管疾病（例如中风）等），心力衰竭等。

2. 发明申请

WO2003040110A1 TRIAZOLE DERIVATIVES AS CYCLOOXYGENASE (COX) INHIBITORS 审中-公开
标题翻译：三唑衍生物作为CYCLOOXYGENASE（COX）抑制剂
公开(公告)号：WO2003040110A1
公开(公告)日：2003-05-15
申请号：PCT/JP2002/011314
申请日：2002-10-30
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , AOKI, Satoshi , NAKAGAWA, Toshiya , KONISHI, Nobukiyo , NAKAMURA, Katsuya , OMORI, Hiroki , KUBOTA, Ariyoshi , HASHIMOTO, Norio
发明人： AOKI, Satoshi , NAKAGAWA, Toshiya , KONISHI, Nobukiyo , NAKAMURA, Katsuya , OMORI, Hiroki , KUBOTA, Ariyoshi , HASHIMOTO, Norio
IPC分类号： C07D249/08
CPC分类号： C07D249/08 , C07D401/04 , C07D401/14 , C07D403/10 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12
摘要： Compound of formula (I) wherein R 1 is lower alkyl which is optionally substituted with halogen, cyano, N,N-di(lower)alkylcarbamoyl, phenyl optionally substituted with halogen, or heterocyclic group, cyclo(lower)alkyl, lower alkynyl, or N,N-di(lower) alkylcarbamoyl; R 2 is lower alkyl, lower alkoxy amino, cyano, or 1H-pyrrol-1-yl; R 3 is lower alkyl, lower alkoxy, or cyano; X is O, S, SO or SO 2 ; Y and Z are each CH or N; and m is 0 or 1; or salts thereof, which are useful as a medicament.
摘要翻译：氰基，N，N-二（低级）烷基氨基甲酰基，任选被卤素取代的苯基或杂环基，低级（低级）烷基，低级炔基或N，N-二（低级）烷基氨基甲酰基; R 2是低级烷基，低级烷氧基氨基，氰基或1H-吡咯-1-基; R 3是低级烷基，低级烷氧基或氰基; X是O，S，SO或SO 2; Y和Z各自为CH或N; m为0或1; 或其盐，其可用作药物。

3. 发明申请

WO2003026659A1 LOW HYGROSCOPIC ARIPIPRAZOLE DRUG SUBSTANCE AND PROCESSES FOR THE PREPARATION THEREOF 审中-公开
标题翻译：低剂量阿维替唑药物及其制备方法
公开(公告)号：WO2003026659A1
公开(公告)日：2003-04-03
申请号：PCT/JP2002/009858
申请日：2002-09-25
申请人： OTSUKA PHARMACEUTICAL CO., LTD. , BANDO, Takuji , AOKI, Satoshi , KAWASAKI, Junichi , ISHIGAMI, Makoto , TANIGUCHI, Youichi , YABUUCHI, Tsuyoshi , FUJIMOTO, Kiyoshi , NISHIOKA, Yoshihiro , KOBAYASHI, Noriyuki , FUJIMURA, Tsutomu , TAKAHASHI, Masanori , ABE, Kaoru , NAKAGAWA, Tomonori , SHINHAMA, Koichi , UTSUMI, Naoto , TOMINAGA, Michiaki , OI, Yoshihiro , YAMADA, Shohei , TOMIKAWA, Kenji
发明人： BANDO, Takuji , AOKI, Satoshi , KAWASAKI, Junichi , ISHIGAMI, Makoto , TANIGUCHI, Youichi , YABUUCHI, Tsuyoshi , FUJIMOTO, Kiyoshi , NISHIOKA, Yoshihiro , KOBAYASHI, Noriyuki , FUJIMURA, Tsutomu , TAKAHASHI, Masanori , ABE, Kaoru , NAKAGAWA, Tomonori , SHINHAMA, Koichi , UTSUMI, Naoto , TOMINAGA, Michiaki , OI, Yoshihiro , YAMADA, Shohei , TOMIKAWA, Kenji
IPC分类号： A61K31/496
CPC分类号： C07D215/227 , C07B2200/13 , C07D215/22 , Y10T428/2982
摘要： The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the aripiprazole anhydride crystals is stored for an extended period.
摘要翻译：本发明提供低吸湿形式的阿立哌唑及其制备方法，即使当含有阿立哌唑酐晶体的药物制剂长时间储存时，其也不会转化为水合物或丧失其原始溶解度。

4. 发明申请

WO2013002420A1 METHOD FOR PRODUCING FINE PARTICLES OF ARIPIPRAZOLE ANHYDRIDE CRYSTALS B 审中-公开
标题翻译：生产阿维拉唑无定形晶体细颗粒的方法B
公开(公告)号：WO2013002420A1
公开(公告)日：2013-01-03
申请号：PCT/JP2012/067258
申请日：2012-06-29
申请人： OTSUKA PHARMACEUTICAL CO., LTD. , BANDO, Takuji , YANO, Katsuhiko , FUKANA, Makoto , AOKI, Satoshi
发明人： BANDO, Takuji , YANO, Katsuhiko , FUKANA, Makoto , AOKI, Satoshi
IPC分类号： C07D215/22 , A61K31/4704 , A61P25/18
CPC分类号： C07D215/22
摘要： The present invention provides a novel method for producing fine particles of aripiprazole anhydride crystals B. The method for producing fine particles of aripiprazole anhydride crystals B comprises the steps of: (1) heating and dissolving crude aripiprazole in a lower alcohol, and subsequently cooling the resulting mixture to precipitate crystals to obtain crystals of aripiprazole lower alcohol solvate; (2) subjecting the crystals of aripiprazole lower alcohol solvate to wet-milling in the form of a slurry containing the lower alcohol; and (3) subjecting the dispersion of the wet-milled crystals to solid-liquid separation to obtain the crystals, and heating the crystals.
摘要翻译：本发明提供一种制备阿立哌唑酐晶体B的微粒的新方法。阿立哌唑无定形晶体B的微粒的制造方法包括以下步骤：（1）将阿立哌唑粗制物加热溶解在低级醇中，得到的混合物沉淀出晶体，得到阿立哌唑低级醇溶剂化物晶体; （2）使阿立哌唑低级醇溶剂化物的晶体以含有低级醇的浆液的形式进行湿磨; 和（3）将经湿磨的晶体的分散液进行固液分离，得到晶体，并加热晶体。

5. 发明申请

WO2009095963A1 MAGNETIC POLE POSITION ESTIMATION METHOD FOR AC SYNCHRONOUS MOTOR 审中-公开
标题翻译：交流同步电机的磁极位置估计方法
公开(公告)号：WO2009095963A1
公开(公告)日：2009-08-06
申请号：PCT/JP2008/003318
申请日：2008-11-14
申请人： MITSUBISHI ELECTRIC CORPORATION , TERADA, Kei , AOKI, Satoshi
发明人： TERADA, Kei , AOKI, Satoshi
IPC分类号： G05B13/02
CPC分类号： H02P21/0035 , H02P21/18 , H02P21/22 , H02P21/24
摘要： If there is static friction, the magnetic pole position estimation is completed at the time when error torque used for magnetic pole position estimation becomes less than the friction, so that there remains magnetic pole error. A problem has been that when the error torque becomes less than a forward static friction, there remains a positive magnetic pole deviation and when the error torque becomes less than a backward static friction, there remains a negative magnetic pole deviation. By shifting in the negative direction and the positive direction initial values for estimating a magnetic pole error in operation sets, a true pole-error estimation value is estimated in the use of a pole-error estimation value having a positive magnetic pole error obtained by the positive shift operation and a negative one obtained by the negative shift operation, which can reduce estimation error due to the static friction.
摘要翻译：如果存在静摩擦，磁极位置估计在用于磁极位置估计的误差转矩小于摩擦时完成磁极位置估计，从而保持磁极误差。一个问题是，当误差转矩小于正向静摩擦时，仍然存在正磁极偏移，当误差转矩小于反向静摩擦时，仍然存在负磁极偏差。通过在负方向和正方向上移动用于估计操作组中的磁极误差的初始值，在使用由具有正磁极误差的极性误差估计值得到的极性误差估计值时，估计真正的极点误差估计值正移位操作和通过负移位操作获得的负移动操作，这可以减少由于静摩擦引起的估计误差。

6. 发明申请

WO2007119496A1 TETOMILAST POLYMORPHS 审中-公开
公开(公告)号：WO2007119496A1
公开(公告)日：2007-10-25
申请号：PCT/JP2007/055931
申请日：2007-03-15
申请人： OTSUKA PHARMACEUTICAL CO., LTD. , AOKI, Satoshi , NAKAYA, Kenji , SOTA, Masahiro , ISHIGAMI, Masashi
发明人： AOKI, Satoshi , NAKAYA, Kenji , SOTA, Masahiro , ISHIGAMI, Masashi
IPC分类号： C07D417/04 , A61K31/4439 , A61P11/00
CPC分类号： A61K31/4436 , C07D417/04
摘要： The present invention provides a tetomilast crystal that is industrially easily produced in a large volume. (1) a tetomilast hydrate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 2; (2) an anhydrous tetomilast type A crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 4; (3) an anhydrous tetomilast type C crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 8; (4) a tetomilast acetonitrile solvate crystal having a powder X-ray diffraction spectrum that is substantially the same as the powder X-ray diffraction spectrum shown in Fig. 10; and (5) a mixture consisting of the above anhydrous tetomilast type A crystal and an anhydrous tetomilast type B crystal. These crystals are stable towards heat and moisture, and are also excellent in terms of the disintegration property and dissolution property of tablets. Accordingly, these crystals are preferably used as pharmaceutical compositions.
摘要翻译：本发明提供了一种工业上易于大量生产的替托司特晶体。（1）具有与图1所示的粉末X射线衍射光谱基本相同的粉末X射线衍射光谱的替托司特水合物晶体。 2; （2）具有粉末X射线衍射光谱的无水替托司特A型晶体，其与图1所示的粉末X射线衍射光谱基本相同。 4; （3）具有粉末X射线衍射光谱的无水替托司特C型晶体，其与图1所示的粉末X射线衍射光谱基本相同。 8; （4）具有与图1所示的粉末X射线衍射光谱基本相同的粉末X射线衍射光谱的替托司特乙腈溶剂合物晶体。 10; 和（5）由上述无水替托司特A型晶体和无水替托司特B型晶体组成的混合物。这些晶体对于热和水分是稳定的，并且在片剂的崩解性和溶解性方面也是优异的。因此，这些晶体优选用作药物组合物。

7. 发明公开

EP1140836A1 AMIDE COMPOUNDS 有权
标题翻译：酰胺化合物
公开(公告)号：EP1140836A1
公开(公告)日：2001-10-10
申请号：EP00900121.5
申请日：2000-01-06
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： YAMADA, Akira , AOKI, Satoshi
IPC分类号： C07D211/58 , C07D213/75 , C07D211/96 , C07D295/20 , C07D295/18 , C07D295/22 , A61K31/445 , A61K31/496 , A61P25/28
CPC分类号： C07D213/75 , C07D211/58 , C07D295/26 , C07D401/12
摘要： This invention relates to new amide compounds having the potentiation of the cholinergic activity, etc., and represented by general formula (I), wherein R1 is acyl, R2 is lower alkyl, etc., A is a single bond, (1) or -SO¿2?-, E is lower alkylene, etc., X is CH or N, Y is a single bond, etc., Q is -CH2-, etc., and R?3 and R4¿ are taken together to form lower alkylene, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and a pharmaceutical composition comprising the same.
摘要翻译：本发明涉及具有胆碱能活性增强等的新型酰胺化合物，并且由通式（I）表示，其中R1为酰基，R2为低级烷基等，A为单键，（1）或 -SO 2 - ， - E为低级亚烷基等，X为CH或N，Y为单键等，Q为-CH 2 - 等，R 3和R 4一起为形成低级亚烷基等及其药学上可接受的盐，其制备方法和包含其的药物组合物。

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