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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。
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公开(公告)号：US20050261177A1
公开(公告)日：2005-11-24
申请号：US10469233
申请日：2002-03-07
申请人： Ayako Toda , Hiroaki Mizuno , Takahiro Matsuya , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Hitomi Ogino , Keiji Matsuda
发明人： Ayako Toda , Hiroaki Mizuno , Takahiro Matsuya , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Hitomi Ogino , Keiji Matsuda
摘要： This invention relates to new polypeptide compound represented by the following general formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译： 本发明涉及由以下通式（I）表示的新的多肽化合物：其中R 1，R 2，R 3，R 3， SUP> 4，R 5和R 6如说明书中所定义或其具有抗微生物活性（特别是抗真菌活性）的抑制活性 β-1,3-葡聚糖合酶，其制备方法，涉及含有该组合物的药物组合物，以及用于预防和/或治疗感染性疾病的方法，包括卡氏肺囊虫感染（例如肺孢子虫卡氏肺炎） 人类或动物。
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公开(公告)号：US06884868B1
公开(公告)日：2005-04-26
申请号：US09926385
申请日：2000-04-25
申请人： Takashi Tojo , Hidenori Ohki , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Keiji Matsuda , Masaharu Ichihara , Norio Hashimoto , Atsushi Kanda , Atsushi Ohigashi
发明人： Takashi Tojo , Hidenori Ohki , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Keiji Matsuda , Masaharu Ichihara , Norio Hashimoto , Atsushi Kanda , Atsushi Ohigashi
摘要： This invention relates to new polypeptide compound represented by general formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译： 本发明涉及由通式（I）表示的新的多肽化合物，其中R 1，R 2，R 3，R 3， 4，R 5和R 6如描述中所定义，或其盐具有抗微生物活性（特别是抗真菌活性），对β的抑制活性 -1,3-葡聚糖合酶，其制备方法，涉及包含其的药物组合物，以及用于预防和/或治疗感染性疾病的方法，所述传染病包括人类卡氏肺囊虫感染（例如肺孢子虫卡氏肺炎） 或动物。
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公开(公告)号：US20050014685A1
公开(公告)日：2005-01-20
申请号：US10873305
申请日：2004-06-23
摘要： This invention relates to new lipopeptide compound represented by the following general formula (I): Wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译： 本发明涉及由以下通式（I）表示的新的脂肽化合物：其中R 1，R 2，R 3，R 4，R 5和R 6如上所定义 在具有抗微生物活性（特别是抗真菌活性）的描述中，其对β-1,3-葡聚糖合酶的抑制活性，其制备方法，含有该活性的药物组合物，以及预防性方法 和/或治疗性处理感染性疾病，包括人或动物的卡氏肺囊虫感染（例如肺孢子虫肺炎）。
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公开(公告)号：US06232290B1
公开(公告)日：2001-05-15
申请号：US09446101
申请日：1999-12-22
申请人： Hidenori Ohki , Kenji Murano , Takashi Tojo , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Hiroaki Mizuno , David Barrett , Keiji Matsuda , Kohji Kawabata
发明人： Hidenori Ohki , Kenji Murano , Takashi Tojo , Nobuyuki Shiraishi , Takahiro Matsuya , Hiroshi Matsuda , Hiroaki Mizuno , David Barrett , Keiji Matsuda , Kohji Kawabata
IPC分类号： A61K3812
摘要： This invention relates to new polypeptide compounds represented by general formula (I), wherein R1, R2, R3 and R4 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on &bgr;-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译： 本发明涉及由通式（I）表示的新的多肽化合物，其中R1，R2，R3和R4如说明书中所定义或其具有抗微生物活性（特别是抗真菌活性）的盐，对β-1的抑制活性 3-葡聚糖合酶，其制备方法，涉及含有该组合物的药物组合物，以及用于预防和/或治疗感染性疾病的方法，包括卡介菌肺炎卡介菌感染（例如肺孢子虫卡氏肺炎）在人或 动物。
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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。
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公开(公告)号：US06884774B2
公开(公告)日：2005-04-26
申请号：US10030161
申请日：2001-02-20
申请人： Ayako Toda , Takahiro Matsuya , Hiroaki Mizuno , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Keiji Matsuda
发明人： Ayako Toda , Takahiro Matsuya , Hiroaki Mizuno , Hiroshi Matsuda , Kenji Murano , David Barrett , Takashi Ogino , Keiji Matsuda
IPC分类号： A61K38/00 , A01N43/90 , A61J1/03 , A61K38/12 , A61P31/00 , A61P31/10 , C07K1/113 , C07K7/54 , C07K7/56 , C07K5/00
摘要： This invention relates to new polypeptide compound represented by the general formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystic carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译： 本发明涉及由通式（I）表示的新的多肽化合物，其中R 1，R 2，R 3，R 3， 4，R 5和R 6如描述中所定义，或其盐具有抗微生物活性（特别是抗真菌活性），对β的抑制活性 -1,3-葡聚糖合酶，其制备方法，涉及含有该组合物的药物组合物，以及用于预防和/或治疗感染性疾病的方法，包括人类卡氏肺囊虫感染（例如肺孢子虫卡氏肺炎） 或动物。
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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。
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公开(公告)号：US20050004014A1
公开(公告)日：2005-01-06
申请号：US10860508
申请日：2004-06-04
摘要： This invention relates to new lipopeptide compound represented by the following general formula (I): wherein R1, R2, R3, R4 and R5 are as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on β-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g. Pneumocystis carinii pneumonia) in a human being or an animal.
摘要翻译： 本发明涉及由以下通式（I）表示的新的脂肽化合物：其中R 1，R 2，R 3，R 4和R 5如说明书中所定义或 其具有抗微生物活性（特别是抗真菌活性），对β-1,3-葡聚糖合酶的抑制活性，其制备方法，包含其的药物组合物，以及预防和/或治疗方法 的感染性疾病，包括人或动物中的卡氏肺囊虫感染（例如肺孢子虫肺炎）。
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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。
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