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公开(公告)号:US08168827B2
公开(公告)日:2012-05-01
申请号:US12487813
申请日:2009-06-19
申请人: Tadakiyo Nakagawa , Tamotsu Suzuki , Kaoru Takenaka , Shinichi Fujita , Youji Yamada , Yoichiro Shima , Tatsuya Okuzumi , Toshihiko Yoshimura , Masanao Yoshida , Masahiro Murata
发明人: Tadakiyo Nakagawa , Tamotsu Suzuki , Kaoru Takenaka , Shinichi Fujita , Youji Yamada , Yoichiro Shima , Tatsuya Okuzumi , Toshihiko Yoshimura , Masanao Yoshida , Masahiro Murata
IPC分类号: C07C233/05 , A61K31/65
CPC分类号: C07D401/04 , C07C237/04 , C07D401/14
摘要: Amide derivatives represented by the formula (I): wherein: A is a cycloalkyl group, an aryl group or a heteroaryl group; X is a nitrogen atom or CR17; Y is —NRa-, —(CRbRb′)m-, and the like; m is 0 to 4; and R1 to R17 may be the same or different and each is a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxyl group, a formyl group, a hydroxyl group, an ammonium group, an alkyl group optionally having one or more substituents, -ZR18 and the like, Z is —O—, —S(O)p-, —S(O)pO—, —NH—, —NR19-, and the like; or a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof may be applied to pharmaceutical use such as anti-inflammatory and analgesic action and the like.
摘要翻译: 由式(I)表示的酰胺衍生物:其中:A为环烷基,芳基或杂芳基; X是氮原子或CR 17; Y是-NR a - , - (CR b R b')m - 等; m为0〜4; R 1〜R 17可以相同或不同,各自为氢原子,卤素原子,氰基,硝基,羧基,甲酰基,羟基,铵基,任选具有 一个或多个取代基,-ZR 18等,Z是-O - , - S(O)p - , - S(O)p O - , - NH - , - NR 19 - 等; 或其药学上可接受的盐,其水合物或其溶剂合物可以用于药物用途,例如抗炎和镇痛作用等。
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公开(公告)号:US20090258900A1
公开(公告)日:2009-10-15
申请号:US12487813
申请日:2009-06-19
申请人: Tadakiyo Nakagawa , Tamotsu Suzuki , Kaoru Takenaka , Shinichi Fujita , Youji Yamada , Yoichiro Shima , Tatsuya Okuzumi , Toshihiko Yoshimura , Masanao Yoshida , Masahiro Murata
发明人: Tadakiyo Nakagawa , Tamotsu Suzuki , Kaoru Takenaka , Shinichi Fujita , Youji Yamada , Yoichiro Shima , Tatsuya Okuzumi , Toshihiko Yoshimura , Masanao Yoshida , Masahiro Murata
IPC分类号: A61K31/4545 , A61K31/444 , A61P29/00 , A61P1/00 , A61P13/00 , A61P11/06 , C07D401/14 , C07D401/04
CPC分类号: C07D401/04 , C07C237/04 , C07D401/14
摘要: Amide derivatives represented by the formula (I): wherein: A is a cycloalkyl group, an aryl group or a heteroaryl group; X is a nitrogen atom or CR17; Y is —NRa—, —(CRbRb′)m-, and the like; m is 0 to 4; and R1 to R17 may be the same or different and each is a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxyl group, a formyl group, a hydroxyl group, an ammonium group, an alkyl group optionally having one or more substituents, -ZR18 and the like, Z is —O—, —S(O)p-, —S(O)pO—, —NH—, —NR19-, and the like; or a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof may be applied to pharmaceutical use such as anti-inflammatory and analgesic action and the like.
摘要翻译: 由式(I)表示的酰胺衍生物:其中:A为环烷基,芳基或杂芳基; X是氮原子或CR 17; Y是-NR a - , - (CR b R b')m - 等; m为0〜4; R 1〜R 17可以相同或不同,各自为氢原子,卤素原子,氰基,硝基,羧基,甲酰基,羟基,铵基,任选具有 一个或多个取代基,-ZR 18等,Z是-O - , - S(O)p - , - S(O)p O - , - NH - , - NR 19 - 等; 或其药学上可接受的盐,其水合物或其溶剂合物可以用于药物用途,例如抗炎和镇痛作用等。
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公开(公告)号:US20060128755A1
公开(公告)日:2006-06-15
申请号:US11281627
申请日:2005-11-18
申请人: Tadakiyo Nakagawa , Tamotsu Suzuki , Kaoru Takenaka , Shinichi Fujita , Youji Yamada , Yoichiro Shima , Tatsuya Okuzumi , Toshihiko Yoshimura , Masanao Yoshida , Masahiro Murata
发明人: Tadakiyo Nakagawa , Tamotsu Suzuki , Kaoru Takenaka , Shinichi Fujita , Youji Yamada , Yoichiro Shima , Tatsuya Okuzumi , Toshihiko Yoshimura , Masanao Yoshida , Masahiro Murata
IPC分类号: A61K31/444 , C07D401/14
CPC分类号: C07D401/04 , C07C237/04 , C07D401/14
摘要: Amide derivatives represented by the formula (I): wherein: A is a cycloalkyl group, an aryl group or a heteroaryl group; X is a nitrogen atom or CR17; Y is —NRa—, —(CRbRb′)m—, and the like; m is 0 to 4; and R1 to R17 may be the same or different and each is a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxyl group, a formyl group, a hydroxyl group, an ammonium group, an alkyl group optionally having one or more substituents, ZR18 and the like, Z is —O—, —S(O)p—, —S(O)pO—, —NH—, —NR19—, and the like; or R1 and R2 may in combination form a ring, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof may be applied to pharmaceutical use such as anti-inflammatory and analgesic action and the like.
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公开(公告)号:US07572815B2
公开(公告)日:2009-08-11
申请号:US11281627
申请日:2005-11-18
申请人: Tadakiyo Nakagawa , Tamotsu Suzuki , Kaoru Takenaka , Shinichi Fujita , Youji Yamada , Yoichiro Shima , Tatsuya Okuzumi , Toshihiko Yoshimura , Masanao Yoshida , Masahiro Murata
发明人: Tadakiyo Nakagawa , Tamotsu Suzuki , Kaoru Takenaka , Shinichi Fujita , Youji Yamada , Yoichiro Shima , Tatsuya Okuzumi , Toshihiko Yoshimura , Masanao Yoshida , Masahiro Murata
IPC分类号: C07D401/04 , A61K31/444
CPC分类号: C07D401/04 , C07C237/04 , C07D401/14
摘要: Amide derivatives represented by the formula (I): wherein: A is a cycloalkyl group, an aryl group or a heteroaryl group; X is a nitrogen atom or CR17; Y is —NRa—, —(CRbRb′)m-, and the like; m is 0 to 4; and R1 to R17 may be the same or different and each is a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxyl group, a formyl group, a hydroxyl group, an ammonium group, an alkyl group optionally having one or more substituents, ZR18 and the like, Z is —O—, —S(O)p-, —S(O)pO—, —NH—, —NR19-, and the like; or R1 and R2 may in combination form a ring, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof may be applied to pharmaceutical use such as anti-inflammatory and analgesic action and the like.
摘要翻译: 由式(I)表示的酰胺衍生物:其中:A为环烷基,芳基或杂芳基; X是氮原子或CR 17; Y是-NR a - , - (CR b R b')m - 等; m为0〜4; R 1〜R 17可以相同或不同,各自为氢原子,卤素原子,氰基,硝基,羧基,甲酰基,羟基,铵基,任选具有 一个或多个取代基,ZR 18等,Z是-O - , - S(O)p - , - S(O)p O - , - NH - , - NR 19 - 等; 或者R1和R2可以组合形成环,其药学上可接受的盐,其水合物或其溶剂合物可以用于药物用途,例如抗炎和止痛作用等。
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公开(公告)号:US20080280909A1
公开(公告)日:2008-11-13
申请号:US11767969
申请日:2007-06-25
申请人: Tatsuya Okuzumi , Kazuyuki Sagi , Toshihiko Yoshimura , Yuji Tanaka , Eiji Nakanishi , Miho Ono , Masahiro Murata
发明人: Tatsuya Okuzumi , Kazuyuki Sagi , Toshihiko Yoshimura , Yuji Tanaka , Eiji Nakanishi , Miho Ono , Masahiro Murata
IPC分类号: A61K31/47 , C07D215/227 , A61K31/502 , A61P29/00 , C07D237/32
CPC分类号: C07D209/48 , A61K31/403 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/502 , A61K31/517 , C07D215/22 , C07D215/227 , C07D215/36 , C07D215/38 , C07D237/32 , C07D239/96 , C07D401/12 , C07D403/12 , C07D471/04
摘要: Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α4 integrin in which α4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection. wherein R1 is a methyl group and R2 is a methoxy group.
摘要翻译: 下式的苯丙氨酸衍生物,其类似物和其药学上可接受的盐对α4整联蛋白具有拮抗活性。 它们用作涉及α4整联蛋白的各种疾病的治疗剂或预防剂,其中α4整联蛋白依赖性粘附过程参与病理学,例如炎性疾病,类风湿性关节炎,炎性肠病,系统性红斑狼疮,多发性硬化症,Siegren综合征, 哮喘,牛皮癣,过敏,糖尿病,心血管疾病,动脉硬化,再狭窄,肿瘤增生,肿瘤转移和移植排斥。 其中R1是甲基,R2是甲氧基。
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公开(公告)号:US07605165B2
公开(公告)日:2009-10-20
申请号:US10921929
申请日:2004-08-20
申请人: Kazuyuki Sagi , Hiroyuki Izawa , Akira Chiba , Tatsuya Okuzumi , Toshihiko Yoshimura , Yuji Tanaka , Miho Ono , Masahiro Murata
发明人: Kazuyuki Sagi , Hiroyuki Izawa , Akira Chiba , Tatsuya Okuzumi , Toshihiko Yoshimura , Yuji Tanaka , Miho Ono , Masahiro Murata
IPC分类号: A61K31/517 , C07D239/88 , C07D239/96
CPC分类号: C07D265/26 , C07D239/54 , C07D239/80 , C07D239/96 , C07D253/04 , C07D285/16 , C07D285/24 , C07D403/12 , C07D405/12 , C07D471/04 , C07D487/04
摘要: The present invention relates to the following phenylalanine derivatives or analogues thereof having an antagonistic activity to α4 integrin and therapeutic agents for various diseases concerning α4 integrin.
摘要翻译: 本发明涉及对α4整联蛋白具有拮抗作用的以下苯丙氨酸衍生物或其类似物,以及涉及α4整联蛋白的各种疾病的治疗剂。
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公开(公告)号:US07193108B2
公开(公告)日:2007-03-20
申请号:US10763237
申请日:2004-01-26
申请人: Akira Chiba , Kazuyuki Sagi , Toshihiko Yoshimura , Tatsuya Okuzumi , Hiroyuki Izawa , Masahiro Murata
发明人: Akira Chiba , Kazuyuki Sagi , Toshihiko Yoshimura , Tatsuya Okuzumi , Hiroyuki Izawa , Masahiro Murata
IPC分类号: C07C315/00 , C07C317/00 , C07C229/00 , A61K31/00
CPC分类号: A61K31/517 , A61K31/235 , C07C275/42 , C07D239/96
摘要: Specified phenylpropionic acid derivatives and analogues thereof have an antagonistic activity to α 4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α 4 integrin, such as inflammatory diseases in which α 4 integrin-depending adhesion process participates in the pathology, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.
摘要翻译: 指定的苯丙酸衍生物及其类似物对α4整联蛋白具有拮抗作用。 它们被用作关于α4整联蛋白的各种疾病的治疗剂或预防剂,例如其中α4整联蛋白依赖性粘附过程参与病理学,类风湿性关节炎,炎性肠病,系统性红斑狼疮,多发性硬化症,Sjögren's 综合征,哮喘,牛皮癣,过敏,糖尿病,心血管疾病,动脉硬化,再狭窄,肿瘤增殖,肿瘤转移和移植排斥。
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公开(公告)号:US08222405B2
公开(公告)日:2012-07-17
申请号:US12951180
申请日:2010-11-22
申请人: Shingo Makino , Tatsuya Okuzumi , Toshihiko Yoshimura , Yuko Satake , Nobuyasu Suzuki , Hiroyuki Izawa , Kazuyuki Sagi , Akira Chiba , Eiji Nakanishi , Masahiro Murata , Takashi Tsuji
发明人: Shingo Makino , Tatsuya Okuzumi , Toshihiko Yoshimura , Yuko Satake , Nobuyasu Suzuki , Hiroyuki Izawa , Kazuyuki Sagi , Akira Chiba , Eiji Nakanishi , Masahiro Murata , Takashi Tsuji
IPC分类号: C07D285/24 , C07D239/72 , C07D403/04 , C07D253/08 , C07D265/26 , C07D487/04
CPC分类号: C07D239/22 , C07D239/54 , C07D239/78 , C07D239/80 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D265/26 , C07D285/16 , C07D285/24 , C07D401/12 , C07D471/04 , C07D475/02 , C07D487/04 , Y02P20/582
摘要: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
摘要翻译: 指定的苯丙氨酸衍生物及其类似物对α4整联蛋白具有拮抗作用。 它们被用作关于α4整联蛋白的各种疾病的治疗剂。
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公开(公告)号:US20110065918A1
公开(公告)日:2011-03-17
申请号:US12951180
申请日:2010-11-22
申请人: Shingo MAKINO , Tatsuya Okuzumi , Toshihiko Yoshimura , Yuko Satake , Nobuyasu Suzuki , Hiroyuki Izawa , Kazuyuki Sagi , Akira Chiba , Eiji Nakanishi , Masahiro Murata , Takashi Tsuji
发明人: Shingo MAKINO , Tatsuya Okuzumi , Toshihiko Yoshimura , Yuko Satake , Nobuyasu Suzuki , Hiroyuki Izawa , Kazuyuki Sagi , Akira Chiba , Eiji Nakanishi , Masahiro Murata , Takashi Tsuji
IPC分类号: C07D285/24 , C07D239/72 , C07D403/04 , C07D253/08 , C07D265/26 , C07D487/04 , C07D239/54
CPC分类号: C07D239/22 , C07D239/54 , C07D239/78 , C07D239/80 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D265/26 , C07D285/16 , C07D285/24 , C07D401/12 , C07D471/04 , C07D475/02 , C07D487/04 , Y02P20/582
摘要: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
摘要翻译: 指定的苯丙氨酸衍生物及其类似物对α4整联蛋白具有拮抗作用。 它们被用作关于α4整联蛋白的各种疾病的治疗剂。
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公开(公告)号:US07872125B2
公开(公告)日:2011-01-18
申请号:US11442141
申请日:2006-05-30
申请人: Shingo Makino , Tatsuya Okuzumi , Toshihiko Yoshimura , Yuko Satake , Nobuyasu Suzuki , Hiroyuki Izawa , Kazuyuki Sagi , Akira Chiba , Eiji Nakanishi , Masahiro Murata , Takashi Tsuji
发明人: Shingo Makino , Tatsuya Okuzumi , Toshihiko Yoshimura , Yuko Satake , Nobuyasu Suzuki , Hiroyuki Izawa , Kazuyuki Sagi , Akira Chiba , Eiji Nakanishi , Masahiro Murata , Takashi Tsuji
IPC分类号: A61K31/517 , C07D239/96
CPC分类号: C07D239/22 , C07D239/54 , C07D239/78 , C07D239/80 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D265/26 , C07D285/16 , C07D285/24 , C07D401/12 , C07D471/04 , C07D475/02 , C07D487/04 , Y02P20/582
摘要: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
摘要翻译: 指定的苯丙氨酸衍生物及其类似物对α4整联蛋白具有拮抗作用。 它们被用作关于α4整联蛋白的各种疾病的治疗剂。
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