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公开(公告)号:US5776948A
公开(公告)日:1998-07-07
申请号:US728431
申请日:1996-10-09
IPC分类号: C07D215/56 , C07D401/04 , C07D405/04 , A61K31/47 , C07D215/18 , C07D215/233
CPC分类号: C07D215/56 , C07D401/04 , C07D405/04
摘要: Antibacterial fluoroquinoline derivatives and salts thereof of the following formula are stable and have low toxicity and high photostability and low cytotoxicity under light irradiation: ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 is hydrogen, optionally protected amino, optionally protected aminocarbonyl or optionally protected carboxyl; R.sub.5 is halogen, lower alkyl or optionally protected hydroxyl or is the same as R.sub.2 ; R.sub.6 is lower alkyl; A is CH.sub.2, optionally protected nitrogen or oxygen; and n and m are each an integer of from 0 to 4, provided that n +m is an integer of from 1 to 4.
摘要翻译: 下式的抗菌氟喹啉衍生物及其盐是稳定的,并且在光照射下具有低毒性和高光稳定性和低细胞毒性:其中R1是氢或低级烷基; R2是氢,任选保护的氨基,任选保护的氨基羰基或任选被保护的羧基; R5是卤素,低级烷基或任意保护的羟基或与R2相同; R6是低级烷基; A是CH 2,任选地保护的氮或氧; n和m各自为0〜4的整数,条件是n + m为1〜4的整数。
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公开(公告)号:US20090093414A1
公开(公告)日:2009-04-09
申请号:US11547158
申请日:2005-04-01
申请人: Hitoshi Ikeya , Tadashi Morikawa , Koichi Takahashi , Noriyuki Izutani , Tatsuya Tamura , Akira Okamachi , Takenori Ishizawa , Haruhiko Sato , Yoshinobu Higuchi , Tatsuya Kato , Akie Honma
发明人: Hitoshi Ikeya , Tadashi Morikawa , Koichi Takahashi , Noriyuki Izutani , Tatsuya Tamura , Akira Okamachi , Takenori Ishizawa , Haruhiko Sato , Yoshinobu Higuchi , Tatsuya Kato , Akie Honma
IPC分类号: A61K31/728 , A61K38/03 , C07K2/00 , C07H3/00 , C07D475/00
CPC分类号: C08L5/08 , A61K31/519 , A61K47/61 , A61K47/65 , C07D475/08 , C08B37/0072
摘要: An object of the present invention is to provide a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint disorders. There is provided a hyaluronic acid-methotrexate conjugate useful for the treatment of joint disorders, wherein methotrexate is conjugated with a hydroxy group of hyaluronic acid through a linker containing a peptide chain consisting of 1 to 8 amino acids, and the linker is conjugated with the hyaluronic acid through a carbamate group.
摘要翻译: 本发明的目的是提供可用作关节病的治疗药物的透明质酸 - 甲氨蝶呤缀合物。 提供了可用于治疗关节疾病的透明质酸 - 甲氨蝶呤缀合物,其中甲氨蝶呤通过含有1至8个氨基酸的肽链的接头与透明质酸的羟基缀合,并且接头与 透明质酸通过氨基甲酸酯基团。
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公开(公告)号:US08088916B2
公开(公告)日:2012-01-03
申请号:US10591653
申请日:2005-03-04
申请人: Hitoshi Ikeya , Tadashi Morikawa , Koichi Takahashi , Tatsuya Tamura , Akira Okamachi , Takenori Ishizawa , Haruhiko Sato , Yoshinobu Higuchi
发明人: Hitoshi Ikeya , Tadashi Morikawa , Koichi Takahashi , Tatsuya Tamura , Akira Okamachi , Takenori Ishizawa , Haruhiko Sato , Yoshinobu Higuchi
CPC分类号: C08B37/0072 , A61K47/61 , A61K47/65 , C07D475/08 , C07K9/003
摘要: An object of the present invention is to provide a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint diseases.There is provided a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint diseases, wherein methotrexate is conjugated with a carboxyl group of hyaluronic acid through a linker containing a peptide chain consisting of 1 to 8 amino acids.
摘要翻译: 本发明的目的是提供可用作关节疾病的治疗药物的透明质酸 - 甲氨蝶呤缀合物。 提供了可用作关节疾病的治疗药物的透明质酸 - 甲氨蝶呤缀合物,其中甲氨蝶呤通过含有1至8个氨基酸的肽链的接头与透明质酸的羧基缀合。
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公开(公告)号:US07807675B2
公开(公告)日:2010-10-05
申请号:US11547158
申请日:2005-04-01
申请人: Hitoshi Ikeya , Tadashi Morikawa , Koichi Takahashi , Noriyuki Izutani , Tatsuya Tamura , Akira Okamachi , Takenori Ishizawa , Haruhiko Sato , Yoshinobu Higuchi , Tatsuya Kato , Akie Honma
发明人: Hitoshi Ikeya , Tadashi Morikawa , Koichi Takahashi , Noriyuki Izutani , Tatsuya Tamura , Akira Okamachi , Takenori Ishizawa , Haruhiko Sato , Yoshinobu Higuchi , Tatsuya Kato , Akie Honma
IPC分类号: C07D475/00 , A61K31/715
CPC分类号: C08L5/08 , A61K31/519 , A61K47/61 , A61K47/65 , C07D475/08 , C08B37/0072
摘要: An object of the present invention is to provide a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint disorders. There is provided a hyaluronic acid-methotrexate conjugate useful for the treatment of joint disorders, wherein methotrexate is conjugated with a hydroxy group of hyaluronic acid through a linker containing a peptide chain consisting of 1 to 8 amino acids, and the linker is conjugated with the hyaluronic acid through a carbamate group.
摘要翻译: 本发明的目的是提供一种可用作关节病的治疗药物的透明质酸 - 甲氨蝶呤缀合物。 提供了可用于治疗关节疾病的透明质酸 - 甲氨蝶呤缀合物,其中甲氨蝶呤通过含有1至8个氨基酸的肽链的接头与透明质酸的羟基缀合,并且接头与 透明质酸通过氨基甲酸酯基团。
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公开(公告)号:US20070197465A1
公开(公告)日:2007-08-23
申请号:US10591653
申请日:2005-03-04
申请人: Hitoshi Ikeya , Tadashi Morikawa , Koichi Takahashi , Tatsuya Tamura , Akira Okamachi , Takenori Ishizawa , Haruhiko Sato , Yoshinobu Higuchi
发明人: Hitoshi Ikeya , Tadashi Morikawa , Koichi Takahashi , Tatsuya Tamura , Akira Okamachi , Takenori Ishizawa , Haruhiko Sato , Yoshinobu Higuchi
IPC分类号: A61K31/728 , C08B37/00 , A61K31/525
CPC分类号: C08B37/0072 , A61K47/61 , A61K47/65 , C07D475/08 , C07K9/003
摘要: An object of the present invention is to provide a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint diseases. There is provided a hyaluronic acid-methotrexate conjugate useful as a therapeutic drug for joint diseases, wherein methotrexate is conjugated with a carboxyl group of hyaluronic acid through a linker containing a peptide chain consisting of 1 to 8 amino acids.
摘要翻译: 本发明的目的是提供可用作关节疾病的治疗药物的透明质酸 - 甲氨蝶呤缀合物。 提供了可用作关节疾病的治疗药物的透明质酸 - 甲氨蝶呤缀合物,其中甲氨蝶呤通过含有1至8个氨基酸的肽链的接头与透明质酸的羧基缀合。
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