公开(公告)号：US20130059855A1

公开(公告)日：2013-03-07

申请号：US13698183

申请日：2011-05-16

申请人： Itsuro Shimada ,  Yutaka Hirakura ,  Kouji Yamazaki ,  Kazuhiro Takeguchi ,  Norihiro Ueda

发明人： Itsuro Shimada ,  Yutaka Hirakura ,  Kouji Yamazaki ,  Kazuhiro Takeguchi ,  Norihiro Ueda

IPC分类号： A61K31/53 ,  A61P35/00 ,  C07D401/14

CPC分类号： C07D401/12 ,  A61K31/53

摘要： Provided are crystals of compound A which have properties suitable for industrial production.MEANS FOR SOLVINGAs the results of intensive studies to provide crystals of compound A having an inhibitory activity on the kinase activity of an EML4-ALK fusion protein and a mutant EGFR protein, crystals of compound A were found. Moreover, it was found that A04-type crystal of compound A, from among the aforesaid crystals of compound A, unexpectedly have preferred properties as a drug substance.

摘要翻译： 提供具有适于工业生产的性质的化合物A的晶体。 解决方法作为提供对EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有抑制活性的化合物A的晶体的深入研究的结果，发现了化合物A的晶体。 此外，发现化合物A的上述晶体中的化合物A的A04型晶体意外地具有作为药物的优选性质。

公开(公告)号：US07034047B2

公开(公告)日：2006-04-25

申请号：US10848386

申请日：2004-05-19

申请人： Takahiko Tobe ,  Takashi Sugane ,  Wataru Hamaguchi ,  Itsuro Shimada ,  Kyoichi Maeno ,  Junji Miyata ,  Tetsuya Kimizuka ,  Takeshi Suzuki ,  Atsuyuki Kohara ,  Takuma Morita ,  Michael Arlt ,  Hartmut Greiner

发明人： Takahiko Tobe ,  Takashi Sugane ,  Wataru Hamaguchi ,  Itsuro Shimada ,  Kyoichi Maeno ,  Junji Miyata ,  Tetsuya Kimizuka ,  Takeshi Suzuki ,  Atsuyuki Kohara ,  Takuma Morita ,  Michael Arlt ,  Hartmut Greiner

IPC分类号： C07D239/08 ,  A61K31/4196

CPC分类号： C07D249/08 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D495/04

摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

摘要翻译： 本发明涉及具有活性抑制甘氨酸转运体并用作药物的三唑衍生物和新的三唑衍生物。 本发明的三唑衍生物具有优异的抑制甘氨酸转运蛋白的活性，可用作痴呆，精神分裂症，认知障碍或参与各种疾病如阿尔茨海默病，帕金森病或亨廷顿病等的认知障碍或痉挛的治疗剂 涉及诸如神经退行性疾病和脑血管障碍等疾病。 特别地，药物对于改善痴呆等的学习障碍是有用的。

公开(公告)号：US20060025461A1

公开(公告)日：2006-02-02

申请号：US11232011

申请日：2005-09-22

申请人： Takahiko Tobe ,  Takashi Sugane ,  Wataru Hamaguchi ,  Itsuro Shimada ,  Kyoichi Maeno ,  Junji Miyata ,  Tetsuya Kimizuka ,  Takeshi Suzuki ,  Atsuyuki Kohara ,  Takuma Morita ,  Michael Arlt ,  Hartmut Greiner

发明人： Takahiko Tobe ,  Takashi Sugane ,  Wataru Hamaguchi ,  Itsuro Shimada ,  Kyoichi Maeno ,  Junji Miyata ,  Tetsuya Kimizuka ,  Takeshi Suzuki ,  Atsuyuki Kohara ,  Takuma Morita ,  Michael Arlt ,  Hartmut Greiner

IPC分类号： A61K31/4196 ,  C07D403/02

CPC分类号： C07D249/08 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  C07D249/10 ,  C07D249/12 ,  C07D249/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/10 ,  C07D495/04

摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

公开(公告)号：US20090181964A1

公开(公告)日：2009-07-16

申请号：US11887384

申请日：2006-03-30

申请人： Masaaki Hirano ,  Isao Kinoyama ,  Shunichiro Matsumoto ,  Eiji Kawaminami ,  Kei Ohnuki ,  Hirofumi Yamamoto ,  Kazuhiko Osoda ,  Tatsuhisa Takahisa ,  Takashi Shin ,  Takanori Koike ,  Itsuro Shimada ,  Hiroyuki Hisamichi ,  Toshiyuki Kusayama

发明人： Masaaki Hirano ,  Isao Kinoyama ,  Shunichiro Matsumoto ,  Eiji Kawaminami ,  Kei Ohnuki ,  Hirofumi Yamamoto ,  Kazuhiko Osoda ,  Tatsuhisa Takahisa ,  Takashi Shin ,  Takanori Koike ,  Itsuro Shimada ,  Hiroyuki Hisamichi ,  Toshiyuki Kusayama

IPC分类号： A61K31/5377 ,  C07D235/04 ,  A61K31/4184 ,  C07D401/02 ,  A61K31/4439 ,  C07D403/02 ,  A61K31/496 ,  C07D413/14 ,  A61K31/506 ,  A61K31/501 ,  A61P35/00

CPC分类号： C07D235/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.

摘要翻译： 旨在提供可用作GnRH受体拮抗剂的化合物。 本发明人进一步研究了丙烷-1,3-二酮衍生物。 结果证实，在具有2-（1,3-二氢-2H-苯并咪唑）的丙烷-1,3-二酮衍生物中具有被-SO 2 -R 3表示的基团取代的苯环或噻吩环的化合物 -2-亚基）具有优异的GnRH受体拮抗作用，完成了本发明。 因为本发明的化合物具有强的GnRH受体拮抗作用，因此可用于治疗性激素依赖性疾病，特别是GnRH相关疾病。 此外，由于本发明的化合物在人体中具有优异的代谢稳定性，药物相互作用少，因此作为上述疾病的药物具有优选的特性。

公开(公告)号：US06642264B1

公开(公告)日：2003-11-04

申请号：US09958174

申请日：2001-10-05

申请人： Satoshi Hayashibe ,  Hirotsune Itahana ,  Masamichi Okada ,  Atsuyuki Kohara ,  Kyoichi Maeno ,  Kiyoshi Yahiro ,  Itsuro Shimada ,  Kazuhito Tanabe ,  Kenji Negoro ,  Takashi Kamikubo ,  Shuichi Sakamoto

发明人： Satoshi Hayashibe ,  Hirotsune Itahana ,  Masamichi Okada ,  Atsuyuki Kohara ,  Kyoichi Maeno ,  Kiyoshi Yahiro ,  Itsuro Shimada ,  Kazuhito Tanabe ,  Kenji Negoro ,  Takashi Kamikubo ,  Shuichi Sakamoto

IPC分类号： A61K31425

CPC分类号： C07D513/04 ,  A61K31/429

摘要： This invention relates to novel thiazolo[3,2-a]benzoimidazole derivatives represented by the following general formula (I). The compounds provided by the invention act specifically on metabotropic glutamate receptors and are used as medicaments. The invention also provides novel compounds useful as intermediates for the synthesis of the compounds of the invention. (Symbols in the formula represent the following meanings. R1: carbamoyl, carbonyl, oxy, amino, carbonylamino or the like which may be substituted; R2: hydrogen, lower alkyl or the like; and R3, R4 and R5: hydrogen, lower alkyl and the like which may be the same or different from one another.)

摘要翻译： 本发明涉及由以下通式（I）表示的新型噻唑并[3,2-a]苯并咪唑衍生物。 本发明提供的化合物特异性地代表代谢型谷氨酸受体并用作药物。 本发明还提供了可用作合成本发明化合物的中间体的新化合物（式中的符号表示以下含义：R 1：可以被取代的氨基甲酰基，羰基，氧基，氨基，羰基氨基等 R 2：氢，低级烷基等; R 3，R 4和R 5：氢，低级烷基等可以彼此相同或不同。）