公开(公告)号：US20060040916A1

公开(公告)日：2006-02-23

申请号：US11259509

申请日：2005-10-26

Applicant: Hiroyuki Chiba ,  Masahiko Tsujii ,  Astsushi Koiwa ,  Shin Sakurai ,  Akio Kayano ,  Hiroyuki Ishizuka ,  Hiroyuki Saito ,  Taiju Nakamura ,  Ikuo Kushida ,  Yasuyuki Suzuki ,  Takako Yoshiba ,  Kazuhide Ashizawa ,  Masahiro Sakurai ,  Eiichi Yamamoto

Inventor： Hiroyuki Chiba ,  Masahiko Tsujii ,  Astsushi Koiwa ,  Shin Sakurai ,  Akio Kayano ,  Hiroyuki Ishizuka ,  Hiroyuki Saito ,  Taiju Nakamura ,  Ikuo Kushida ,  Yasuyuki Suzuki ,  Takako Yoshiba ,  Kazuhide Ashizawa ,  Masahiro Sakurai ,  Eiichi Yamamoto

IPC: C07D487/04 ,  A61K31/407

CPC classification number: C07D477/20 ,  A61K31/407

Abstract: The present invention provides carbapenem hydrochloride trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection containing them. That is, it provides carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 Å, a process for producing them, and a powdery charged preparation for injection containing them.

Abstract translation: 本发明提供化学稳定，易于纯化和用作抗微生物剂的盐酸碳青霉烯盐酸盐三水合物晶体，其制备方法和含有它们的注射用粉末状药物制剂。 也就是说，它提供了具有包含晶格距离（d）为9.0,4.1和2.8的粉末X射线衍射图的碳青霉烯盐酸盐三水合物晶体，其制备方法和含有它们的注射用粉末状药物制剂。

公开(公告)号：US07612208B2

公开(公告)日：2009-11-03

申请号：US10577531

申请日：2004-12-22

Applicant: Tomohiro Matsushima ,  Taiju Nakamura ,  Kazuhiro Yoshizawa ,  Atsushi Kamada ,  Yusuke Ayata ,  Naoko Suzuki ,  Itaru Arimoto ,  Takahisa Sakaguchi ,  Masaharu Gotoda

Inventor： Tomohiro Matsushima ,  Taiju Nakamura ,  Kazuhiro Yoshizawa ,  Atsushi Kamada ,  Yusuke Ayata ,  Naoko Suzuki ,  Itaru Arimoto ,  Takahisa Sakaguchi ,  Masaharu Gotoda

IPC: C07D215/38

CPC classification number: C07D215/48

Abstract: A crystal of a 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide hydrochloride, hydrobromide, p-toluenesulfonate, sulfate, methanesulfonate or ethanesulfonate, or a solvate thereof.

Abstract translation: 4-（3-氯-4-（环丙基氨基羰基）氨基苯氧基）-7-甲氧基-6-喹啉甲酰胺盐酸盐，氢溴酸盐，对甲苯磺酸盐，硫酸盐，甲磺酸盐或乙磺酸盐或其溶剂化物的晶体。

公开(公告)号：US07585982B2

公开(公告)日：2009-09-08

申请号：US11573814

申请日：2005-07-27

Applicant: Kazuhiro Yoshizawa ,  Taiju Nakamura ,  Shigeto Negi

Inventor： Kazuhiro Yoshizawa ,  Taiju Nakamura ,  Shigeto Negi

IPC: C07D209/44

CPC classification number: C07C255/59 ,  C07D209/44

Abstract: The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II): (wherein R1 and R2 each independently represents a C1-6 alkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I): (wherein R1 and R2 have the same meanings as R1 and R2 in formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).

Abstract translation: 本发明涉及具有下列通式（II）的异吲哚衍生物（化合物（II））的制备方法：（其中R1和R2各自独立地表示C1-6烷基）或其盐，其包含步骤 在溶剂中使具有以下通式（I）的化合物（I）：其中R 1和R 2具有与上述式（II）中的R 1和R 2相同的含义）或其盐或其水合物或溶剂合物 在碱的存在下（步骤1）。

公开(公告)号：US20110172427A1

公开(公告)日：2011-07-14

申请号：US13060979

申请日：2009-08-26

Applicant: Taiju Nakamura ,  Masaaki Matsuda ,  Yongbo Hu ,  Daiju Hasegawa ,  Yorihisa Hoshino ,  Kazato Inanaga ,  Minetaka Isomura ,  Nobuaki Sato ,  Kazuhiro Yoshizawa ,  George A. Moniz ,  Gordon D. Wilkie ,  Francis G. Fang ,  Yoshihiro Nishikawa

Inventor： Taiju Nakamura ,  Masaaki Matsuda ,  Yongbo Hu ,  Daiju Hasegawa ,  Yorihisa Hoshino ,  Kazato Inanaga ,  Minetaka Isomura ,  Nobuaki Sato ,  Kazuhiro Yoshizawa ,  George A. Moniz ,  Gordon D. Wilkie ,  Francis G. Fang ,  Yoshihiro Nishikawa

IPC: C07D471/04 ,  C07C257/06 ,  C07D401/14 ,  C07D401/04

CPC classification number: C07D471/04 ,  C07C257/06 ,  C07D401/04

Abstract: This invention relates to a new synthesis, intermediates and precursors leading to a mixture of the compounds 11 and 12 as shown below. It also relates to the resolution of the stereoisomeric mixture to provide in substantial stereochemical purity compound 12. The synthesis of the invention involves preparation of compound 7 and compound 10 as shown below and their reaction to prepare a mixture of compound 11 and compound 12.

Abstract translation: 本发明涉及如下所示的通过化合物11和12的混合物的新合成，中间体和前体。 它还涉及立体异构体混合物的拆分以提供基本的立体化学纯度化合物12.本发明的合成包括如下所示的化合物7和化合物10的制备及其制备化合物11和化合物12的混合物的反应。

公开(公告)号：US20090270623A1

公开(公告)日：2009-10-29

申请号：US12093287

申请日：2006-11-17

Applicant: Naoyuki Shimomura ,  Nobuaki Sato ,  Toshihiko Kaneko ,  Mamoru Takaishi ,  Kazunori Wakasugi ,  Seiji Yoshikawa ,  Yoshihiro Nishikawa ,  Taiju Nakamura ,  Tohru Fukuyama

Inventor： Naoyuki Shimomura ,  Nobuaki Sato ,  Toshihiko Kaneko ,  Mamoru Takaishi ,  Kazunori Wakasugi ,  Seiji Yoshikawa ,  Yoshihiro Nishikawa ,  Taiju Nakamura ,  Tohru Fukuyama

IPC: C07F9/59 ,  C07D401/10 ,  C07D211/76

CPC classification number: C07D401/10

Abstract: A compound (8) represented by the formula: (8) wherein R1 represents a 6- to 14-membered aromatic hydrocarbon ring group which may have a substituent; and n represents 0 to 2, can be produced with good efficiency by reacting a compound (3) represented by the formula: (3) wherein R1 and n are as defined above; and Q represents a single bond or —CH(Y)— where Y represents a hydrogen atom or a C1-6 alkyl group] with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base.

Abstract translation: 由式（8）表示的化合物（8）：其中R1表示可具有取代基的6至14元芳族烃环基团; n表示0〜2，可以通过使式（3）表示的化合物（3）（其中R 1和n如上所定义）反应而得到良好的效率。 和Q表示单键或-CH（Y） - ，其中Y表示氢原子或C 1-6烷基]与3-甲氧基-4-（4-甲基-1H-咪唑-1-基）苯甲醛在 存在基地

公开(公告)号：US07084268B1

公开(公告)日：2006-08-01

申请号：US09979679

申请日：2000-06-05

Applicant: Hiroyuki Chiba ,  Masahiko Tsujii ,  Astsushi Koiwa ,  Shin Sakurai ,  Akio Kayano ,  Hiroyuki Ishizuka ,  Hiroyuki Saito ,  Taiju Nakamura ,  Ikuo Kushida ,  Yasuyuki Suzuki ,  Takako Yoshiba ,  Kazuhide Ashizawa ,  Masahiro Sakurai ,  Eiichi Yamamoto

Inventor： Hiroyuki Chiba ,  Masahiko Tsujii ,  Astsushi Koiwa ,  Shin Sakurai ,  Akio Kayano ,  Hiroyuki Ishizuka ,  Hiroyuki Saito ,  Taiju Nakamura ,  Ikuo Kushida ,  Yasuyuki Suzuki ,  Takako Yoshiba ,  Kazuhide Ashizawa ,  Masahiro Sakurai ,  Eiichi Yamamoto

IPC: C07D477/20 ,  A61K31/407 ,  A61P31/04

CPC classification number: C07D477/20 ,  A61K31/407

Abstract: The present invention provides carbapenem hydrochloride trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection containing them. That is, it provides carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 Å, a process for producing them, and a powdery charged preparation for injection containing them.

Abstract translation: 本发明提供化学稳定，易于纯化和用作抗微生物剂的盐酸碳青霉烯盐酸盐三水合物晶体，其制备方法和含有它们的注射用粉末状药物制剂。 也就是说，它提供了具有包含晶格距离（d）为9.0,4.1和2.8的粉末X射线衍射图的碳青霉烯盐酸盐三水合物晶体，其制备方法和含有它们的注射用粉末状药物制剂。

公开(公告)号：US20090048448A1

公开(公告)日：2009-02-19

申请号：US12093929

申请日：2006-11-17

Applicant: Ikuo Kushida ,  Eriko Doi ,  Koichi Ito ,  Taiju Nakamura

Inventor： Ikuo Kushida ,  Eriko Doi ,  Koichi Ito ,  Taiju Nakamura

IPC: C07D401/10

CPC classification number: C07D401/10

Abstract: The invention provides crystals of dihydrochloride monohydrate of the compound of the following formula having an Aβ production inhibiting effect which crystals are characterized by exhibiting a diffraction peak at an angle of diffraction (2θ±0.2°) of 10.9° in powder X-ray diffractometry. Further, the invention also provides the compound in the form of various salts, crystal forms and amorphous forms which are suitable for the development of drugs.

Abstract translation: 本发明提供下式化合物的二盐酸盐一水合物晶体，其具有抑制Aβ生成的作用，其结晶的特征在​​于在粉末X射线衍射中以衍射角（2θ±0.2°）为10.9°的衍射峰。 此外，本发明还提供了适合于开发药物的各种盐，晶型和无定形形式的化合物。

公开(公告)号：US20080214834A1

公开(公告)日：2008-09-04

申请号：US11573814

申请日：2005-07-27

Applicant: Kazuhiro Yoshizawa ,  Taiju Nakamura ,  Shigeto Negi

Inventor： Kazuhiro Yoshizawa ,  Taiju Nakamura ,  Shigeto Negi

IPC: C07D209/44 ,  C07C255/59

CPC classification number: C07C255/59 ,  C07D209/44

Abstract: The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II): (wherein R1 and R2 each independently represents a C1-6 alkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I): (wherein R1 and R2 have the same meanings as R1 and R2 in formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).

Abstract translation: 本发明涉及以下通式（II）制备异吲哚衍生物（化合物（II））的方法：其中R 1和R 2各自独立地 代表C 1-6烷基）或其盐，包括在溶剂中使具有以下通式（I）的化合物（I）环化的步骤：（其中R“ 1和R 2具有与上述式（II）中的R 1和R 2相同的含义）或其盐 ，或其水合物或溶剂化物在碱的存在下（步骤1）。

公开(公告)号：US06642377B1

公开(公告)日：2003-11-04

申请号：US10030909

申请日：2002-01-14

Applicant: Akio Kayano ,  Hiroyuki Chiba ,  Taiju Nakamura ,  Shin Sakurai ,  Hiroyuki Ishizuka ,  Hiroyuki Saito ,  Yuuki Komatsu ,  Manabu Sasho ,  Nobuaki Sato ,  Shigeto Negi

Inventor： Akio Kayano ,  Hiroyuki Chiba ,  Taiju Nakamura ,  Shin Sakurai ,  Hiroyuki Ishizuka ,  Hiroyuki Saito ,  Yuuki Komatsu ,  Manabu Sasho ,  Nobuaki Sato ,  Shigeto Negi

IPC: C07D47720

CPC classification number: C07D477/20 ,  C07D477/02 ,  C07D477/08 ,  Y02P20/55

Abstract: A production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: wherein the ring A means the basic antibiotic; R10 means a protected functional group used in organic synthesis; Ak—E means the alkali earth metal; and B means the inorganic acid, respectively.

Abstract translation: 一种制备方法，其包括使碱性抗生素 - 草酸盐（II）与无机酸的碱土金属盐（III）进行盐交换：其中环A表示碱性抗生素; R 10表示有机合成中使用的被保护的官能团; Ak-E表示碱土金属; B分别表示无机酸。