公开(公告)号：US20100099658A1

公开(公告)日：2010-04-22

申请号：US12448759

申请日：2008-07-04

申请人： Yutaka Kondoh ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

发明人： Yutaka Kondoh ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

IPC分类号： A61K31/397 ,  C07D239/72 ,  A61K31/497 ,  A61K31/517 ,  C07D413/02 ,  A61K31/5377 ,  C07D403/02 ,  A61K31/53 ,  C07D279/12 ,  A61K31/541 ,  A61P35/00

CPC分类号： A61K31/551 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  C07D239/95 ,  C07D251/18 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/08 ,  C07D491/113 ,  C07D498/10

摘要： The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins.As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.

摘要翻译： 本发明提供了可用作抑制EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性的化合物。 作为对具有对EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有抑制作用的化合物的广泛和深入研究的结果，本发明的发明人已经发现本发明的二（芳基氨基）芳基化合物具有 对EML4-ALK融合蛋白和突变型EGFR蛋白激酶活性的抑制活性。 这一发现导致了本发明的完成。 本发明的化合物可以用作预防和/或治疗癌症，肺癌，非小细胞肺癌，小细胞肺癌，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸的药物组合物， 阳性癌症，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性肺癌或EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性非小细胞肺癌等。

公开(公告)号：US20130096100A1

公开(公告)日：2013-04-18

申请号：US13618732

申请日：2012-09-14

申请人： Yutaka KONDOH ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

发明人： Yutaka KONDOH ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

IPC分类号： A61K31/551 ,  A61K31/541 ,  A61K31/53 ,  A61K31/517 ,  A61K31/5377

CPC分类号： A61K31/551 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  C07D239/95 ,  C07D251/18 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/08 ,  C07D491/113 ,  C07D498/10

摘要： The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins.As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.

摘要翻译： 本发明提供了可用作抑制EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性的化合物。 作为对具有对EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有抑制作用的化合物的广泛和深入研究的结果，本发明的发明人已经发现本发明的二（芳基氨基）芳基化合物具有 对EML4-ALK融合蛋白和突变型EGFR蛋白激酶活性的抑制活性。 这一发现导致了本发明的完成。 本发明的化合物可以用作预防和/或治疗癌症，肺癌，非小细胞肺癌，小细胞肺癌，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸的药物组合物， 阳性癌症，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性肺癌或EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性非小细胞肺癌等。

公开(公告)号：US08318702B2

公开(公告)日：2012-11-27

申请号：US12448759

申请日：2008-07-04

申请人： Yutaka Kondoh ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

发明人： Yutaka Kondoh ,  Kazuhiko Iikubo ,  Sadao Kuromitsu ,  Nobuaki Shindo ,  Takatoshi Soga ,  Takashi Furutani ,  Itsuro Shimada ,  Takahiro Matsuya ,  Kazuo Kurosawa ,  Akio Kamikawa ,  Hiroyuki Mano

IPC分类号： A01N57/00 ,  A01N43/00 ,  A01N43/66 ,  A61K31/675 ,  A61K31/00 ,  A61K31/53 ,  C07D251/00 ,  C07D253/00 ,  C07D251/40 ,  C07D251/18 ,  C07D251/48

CPC分类号： A61K31/551 ,  A61K31/517 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  C07D239/95 ,  C07D251/18 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/08 ,  C07D491/113 ,  C07D498/10

摘要： The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins.As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.

摘要翻译： 本发明提供了可用作抑制EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性的化合物。 作为对具有对EML4-ALK融合蛋白和突变型EGFR蛋白的激酶活性具有抑制作用的化合物的广泛和深入研究的结果，本发明的发明人已经发现本发明的二（芳基氨基）芳基化合物具有 对EML4-ALK融合蛋白和突变型EGFR蛋白激酶活性的抑制活性。 这一发现导致了本发明的完成。 本发明的化合物可以用作预防和/或治疗癌症，肺癌，非小细胞肺癌，小细胞肺癌，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸的药物组合物， 阳性癌症，EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性肺癌或EML4-ALK融合多核苷酸阳性和/或突变型EGFR多核苷酸阳性非小细胞肺癌等。

公开(公告)号：US20120040968A1

公开(公告)日：2012-02-16

申请号：US13266164

申请日：2010-05-06

申请人： Itsuro Shimada ,  Kazuo Kurosawa ,  Takahiro Matsuya ,  Kazuhiko Iikubo ,  Yutaka Kondoh ,  Akio Kamikawa ,  Hiroshi Tomiyama ,  Yoshinori Iwai

发明人： Itsuro Shimada ,  Kazuo Kurosawa ,  Takahiro Matsuya ,  Kazuhiko Iikubo ,  Yutaka Kondoh ,  Akio Kamikawa ,  Hiroshi Tomiyama ,  Yoshinori Iwai

IPC分类号： A61K31/497 ,  C07D405/14 ,  C07D401/14 ,  C07D491/113 ,  C07D403/12 ,  A61K31/551 ,  A61K31/538 ,  C07D409/14 ,  C07D417/12 ,  A61K31/55 ,  A61K31/541 ,  C07D471/08 ,  C07D241/28 ,  C07D401/12 ,  A61K31/513 ,  C07D239/48 ,  A61P35/00 ,  A61K31/5377

CPC分类号： C07D239/48 ,  C07D241/26 ,  C07D241/28 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/08 ,  C07D491/113

摘要： Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein.As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.

摘要翻译： 提供了可用作抑制EML4-ALK融合蛋白的激酶活性的化合物。 作为对具有针对EML4-ALK融合蛋白的激酶活性的抑制活性的化合物进行了深入和广泛的研究的结果，本发明人发现本发明的二氨基杂环羧酰胺化合物对EML4-ALK融合体的激酶活性具有抑制活性 蛋白。 通过这一发现，完成了本发明。 本发明的化合物可以用作预防和/或治疗癌症的药物组合物，例如肺癌，非小细胞肺癌和小细胞肺癌。

公开(公告)号：US08969336B2

公开(公告)日：2015-03-03

申请号：US13266164

申请日：2010-05-06

申请人： Itsuro Shimada ,  Kazuo Kurosawa ,  Takahiro Matsuya ,  Kazuhiko Iikubo ,  Yutaka Kondoh ,  Akio Kamikawa ,  Hiroshi Tomiyama ,  Yoshinori Iwai

发明人： Itsuro Shimada ,  Kazuo Kurosawa ,  Takahiro Matsuya ,  Kazuhiko Iikubo ,  Yutaka Kondoh ,  Akio Kamikawa ,  Hiroshi Tomiyama ,  Yoshinori Iwai

IPC分类号： A61K31/55 ,  A61K31/497 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/54 ,  C07D243/08 ,  C07D413/14 ,  C07D241/02 ,  C07D237/02 ,  C07D401/12 ,  C07D239/48 ,  C07D241/26 ,  C07D241/28 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/08 ,  C07D491/113

CPC分类号： C07D239/48 ,  C07D241/26 ,  C07D241/28 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/08 ,  C07D491/113

摘要： Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein.As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.

摘要翻译： 提供了可用作抑制EML4-ALK融合蛋白的激酶活性的化合物。 作为对具有针对EML4-ALK融合蛋白的激酶活性的抑制活性的化合物进行了深入和广泛的研究的结果，本发明人发现本发明的二氨基杂环羧酰胺化合物对EML4-ALK融合体的激酶活性具有抑制活性 蛋白。 通过这一发现，完成了本发明。 本发明的化合物可以用作预防和/或治疗癌症的药物组合物，例如肺癌，非小细胞肺癌和小细胞肺癌。

公开(公告)号：US20100227866A1

公开(公告)日：2010-09-09

申请号：US12600894

申请日：2008-05-26

申请人： Hiroyuki Hisamichi ,  Itsuro Shimada ,  Tsukasa Ishihara ,  Tomofumi Takuwa ,  Takafumi Shimizu ,  Noriko Ishikawa ,  Kyoichi Maeno ,  Norio Seki

发明人： Hiroyuki Hisamichi ,  Itsuro Shimada ,  Tsukasa Ishihara ,  Tomofumi Takuwa ,  Takafumi Shimizu ,  Noriko Ishikawa ,  Kyoichi Maeno ,  Norio Seki

IPC分类号： A61K31/4725 ,  C07D401/12 ,  C07D401/14 ,  A61K31/53 ,  A61K31/506 ,  A61P1/00 ,  A61P35/00

CPC分类号： A61K31/4725 ,  A61K31/435 ,  A61K31/439 ,  A61K31/445 ,  A61K31/472 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/695 ,  C07D217/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D471/04

摘要： [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS).[Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.

摘要翻译： [问题]提供药物，特别是可用作肠易激综合征（IBS）治疗剂的化合物。 [解决问题的手段]发现在4-位具有酰胺基的四氢异喹啉-1-酮衍生物或其药学上可接受的盐具有优异的铃蟾肽2（BB2）受体拮抗作用。 还发现四氢异喹啉-1-酮衍生物对肠运动障碍是高度有效的。 从上述可以看出，本发明的四氢异喹啉-1-酮衍生物可用作与BB2受体，特别是IBS相关疾病的治疗剂。

公开(公告)号：US08486970B2

公开(公告)日：2013-07-16

申请号：US12600894

申请日：2008-05-26

申请人： Hiroyuki Hisamichi ,  Itsuro Shimada ,  Tsukasa Ishihara ,  Tomofumi Takuwa ,  Takafumi Shimizu ,  Noriko Ishikawa ,  Kyoichi Maeno ,  Norio Seki

发明人： Hiroyuki Hisamichi ,  Itsuro Shimada ,  Tsukasa Ishihara ,  Tomofumi Takuwa ,  Takafumi Shimizu ,  Noriko Ishikawa ,  Kyoichi Maeno ,  Norio Seki

IPC分类号： A01N43/40 ,  A61K31/445

CPC分类号： A61K31/4725 ,  A61K31/435 ,  A61K31/439 ,  A61K31/445 ,  A61K31/472 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/695 ,  C07D217/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D471/04

摘要： [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS).[Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.

摘要翻译： [问题]提供药物，特别是可用作肠易激综合征（IBS）治疗剂的化合物。 [解决问题的手段]发现在4-位具有酰胺基的四氢异喹啉-1-酮衍生物或其药学上可接受的盐具有优异的铃蟾肽2（BB2）受体拮抗作用。 还发现四氢异喹啉-1-酮衍生物对肠运动障碍是高度有效的。 从上述可以看出，本发明的四氢异喹啉-1-酮衍生物可用作与BB2受体，特别是IBS相关疾病的治疗剂。

公开(公告)号：US07960562B2

公开(公告)日：2011-06-14

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 Takahashi ,  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 Takahashi ,  Takashi Shin ,  Takanori Koike ,  Itsuro Shimada ,  Hiroyuki Hisamichi ,  Toshiyuki Kusayama

IPC分类号： A61K31/4184 ,  C07D235/12

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：US07084164B2

公开(公告)日：2006-08-01

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： A61K31/41 ,  C07D249/08

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：US06245796B1

公开(公告)日：2001-06-12

申请号：US09445104

申请日：1999-12-02

申请人： Kyoichi Maeno ,  Ken-ichi Kazuta ,  Hideki Kubota ,  Itsuro Shimada ,  Tetsuya Kimizuka ,  Shuichi Sakamoto ,  Fumikazu Wanibuchi

发明人： Kyoichi Maeno ,  Ken-ichi Kazuta ,  Hideki Kubota ,  Itsuro Shimada ,  Tetsuya Kimizuka ,  Shuichi Sakamoto ,  Fumikazu Wanibuchi

IPC分类号： A01N4356

CPC分类号： C07D231/54 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

摘要： A tricyclic pyrrole or pyrazole derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof, which shows strong affinity and selectivity for the 5-HT2C receptor and is useful for the treatment of central nervous system diseases such as sexual disorders, eating disorders, anxiety, depression and sleeping disorders. (In the above formula, each symbol means as follows; Y ring: an unsaturated five-membered ring which may have 1 to 3 of one or more types of hetero atom(s) each selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom or an unsaturated six-membered ring having 1 or 2 nitrogen atom(s), X: a bond or a carbon atom, a double bond or a single bond, V: a nitrogen atom or a group represented by a formula CH, and A: a straight or branched lower alkylene group which may be substituted with a halogen atom or a cycloalkyl group).

摘要翻译： 由以下通式（I）表示的三环吡咯或吡唑衍生物或其药学上可接受的盐对5-HT 2C受体表现出强亲和力和选择性，可用于治疗中枢神经系统疾病如性功能障碍 （进食障碍，焦虑症，抑郁症和睡眠障碍）（上式中，每个符号表示如下：Y环：每个可以具有1至3个一个或多个杂原子的不饱和五元环 选自氮原子，氧原子和硫原子或具有1或2个氮原子的不饱和六元环，X：键或碳原子，双键或单键，V为氮原子或式CH所示基团，A为直链或支链低级亚烷基， 可以被卤素原子或环烷基取代）。