公开(公告)号：US06171520B2

公开(公告)日：2001-01-09

申请号：US08945885

申请日：1997-11-14

申请人： Kazuhiro Imai ,  Hiromichi Eto ,  Takeshi Kotsugai ,  Tadashi Narita

发明人： Kazuhiro Imai ,  Hiromichi Eto ,  Takeshi Kotsugai ,  Tadashi Narita

IPC分类号： C09K1107

CPC分类号： C07D401/12 ,  G01N33/533

摘要： Disclosed are SH-labeling reagents containing acridine compounds represented by the following formula (I): wherein A represents the following group: —(CH2)m1— or —(CH2)m2—Q—(CH2)n— in which Q represents a group —S+RX−—, a group —N+RR1X−— wherein R1 represents an alkyl group having 1 to 6 carbon atoms or an aryl group, a group wherein R2 and R3 may be the same or different and are each independently a group —(CH2)k— (k: a number of 1 to 3) or —O(CH2CH2O)l— (l: a number of 1 to 3), m1 stands for a number of 1 to 6, m2 denotes a number of 0 to 2, n means a number of 1 to 2; R represents an alkyl group having 1 to 6 carbon atoms or an aryl group; and X− represents an anion, or intermediates thereof; preparation processes of the acridine compounds; and methods for labeling analytes by using the compounds.

摘要翻译： 公开了含有下式（I）表示的吖啶化合物的SH-标记试剂：其中A表示以下基团：Q表示-S + RX-的基团，-N + RR1X--基团，其中R1表示烷基 具有1至6个碳原子的基团或芳基，其中R2和R3中的基团可以相同或不同，并且各自独立地为基团 - （CH 2）k - （k：1至3的数）或-O（CH 2 CH 2 O ）1-（1：1〜3的数），m1表示1〜6的数，m2表示0〜2的数，n表示1〜2的数; R表示1〜 6个碳原子或芳基; 和X-表示阴离子或其中间体; 吖啶化合物的制备方法; 以及通过使用化合物标记分析物的方法。

公开(公告)号：US6008239A

公开(公告)日：1999-12-28

申请号：US135163

申请日：1998-08-17

申请人： Yasushi Kaneko ,  Sunao Takeda ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

发明人： Yasushi Kaneko ,  Sunao Takeda ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

IPC分类号： A01N43/653 ,  C07D249/08 ,  C07D521/00 ,  A61K31/505

CPC分类号： C07D231/12 ,  A01N43/653 ,  C07D233/56 ,  C07D249/08

摘要： Described is a triazole derivative represented by the formula (1): ##STR1## wherein R.sup.1 represents a lower alkyl group or an aralkyl group, R.sup.2 represents a hydrogen atom, a lower alkyl group, an aralkyl group or an acyl group, X.sup.1 and X.sup.2 are the same or different and each independently represents a hydrogen atom, a halogen atom or a trifluoromethyl group, n stands for an integer of 0 to 2 and m stands for an integer of 1 to 5, or salt thereof; and also a pharmaceutical comprising the derivative or salt thereof as an effective ingredient. The compound as described above has a high antimycotic activity and is useful for the prevention and treatment of mammalian mycotic infections.

摘要翻译： 描述了由式（1）表示的三唑衍生物：其中R1表示低级烷基或芳烷基，R2表示氢原子，低级烷基，芳烷基或酰基，X1和X2相同 或不同，各自独立地表示氢原子，卤素原子或三氟甲基，n表示0〜2的整数，m表示1〜5的整数，或其盐。 以及包含其衍生物或其盐作为有效成分的药物。 如上所述的化合物具有高的抗真菌活性，并且可用于预防和治疗哺乳动物真菌感染。

公开(公告)号：US06172266B2

公开(公告)日：2001-01-09

申请号：US09471286

申请日：1999-12-23

申请人： Sunao Takeda ,  Yasushi Kaneko ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

发明人： Sunao Takeda ,  Yasushi Kaneko ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

IPC分类号： C07C32307

CPC分类号： C07D231/12 ,  C07C323/22 ,  C07C2601/02 ,  C07D233/56 ,  C07D249/08 ,  C07D303/34

摘要： Described is a triazole derivative represented by the formula (1): wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group, X1 and X2 are the same or different and each independently represents a hydrogen atom, a halogen atom or a halogenoalkyl and n stands for an integer of 0 to 2, or salt thereof; a preparation process of said compound and a pharmaceutical comprising said compound as an effective ingredient. The compound as described above has high antimycotic activity and is useful for the prevention and treatment of mammalian mycotic infections.

摘要翻译： 描述了由式（1）表示的三唑衍生物：其中R1表示氢原子，低级烷基或芳烷基，X1和X2相同或不同，并且各自独立地表示氢原子，卤素原子或 卤代烷基，n表示0〜2的整数，或其盐; 所述化合物的制备方法和包含所述化合物作为有效成分的药物。如上所述的化合物具有高抗真菌活性，并且可用于预防和治疗哺乳动物真菌感染。

公开(公告)号：US5939448A

公开(公告)日：1999-08-17

申请号：US872159

申请日：1997-06-10

申请人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

发明人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： C07D249/08 ,  C07D303/34 ,  C07D521/00 ,  A61K31/41

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/34

摘要： Described is a triazole derivative represented by the formula (1): wherein R represents a hydrogen atom, an alkyl group, an aralkyl group or an acyl group, n stands for 0 to 2 and m stands for 1 to 5 or salt thereof, and a pharmaceutical containing the derivative or salt as an effective ingredient.

摘要翻译： 描述了由式（1）表示的三唑衍生物：其中R表示氢原子，烷基，芳烷基或酰基，n表示0至2，m表示1至5或其盐， 含有衍生物或盐作为有效成分的药物。

公开(公告)号：US06229049B1

公开(公告)日：2001-05-08

申请号：US09488746

申请日：2000-01-21

申请人： Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Susumu Sato

发明人： Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Susumu Sato

IPC分类号： C07C31914

CPC分类号： C07C319/20 ,  C07C323/22

摘要： The invention relates to a process for preparing a difluoroacetophenone derivative (4) by alkylthionating a compound (1) into a compound (2) and reacting this compound with a compound (3). wherein X1 is Cl, Br or I, X2 and X3 are independently a halogen atom, H or perfluoroalkyl group, X4 is a halogen atom, R1 is an alkyl, aryl or aralkyl group, and R2 is methyl, ethyl or cyclopropyl group.

摘要翻译： 本发明涉及通过将化合物（1）烷基化成化合物（2）并使该化合物与化合物（3）反应制备二氟苯乙酮衍生物（4）的方法，其中X1为Cl，Br或I，X2和X3 独立地为卤素原子，H或全氟烷基，X4为卤素原子，R1为烷基，芳基或芳烷基，R2为甲基，乙基或环丙基。

公开(公告)号：US06204415B1

公开(公告)日：2001-03-20

申请号：US09551567

申请日：2000-04-18

申请人： Sunao Takeda ,  Yasushi Kaneko ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

发明人： Sunao Takeda ,  Yasushi Kaneko ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

IPC分类号： C07C32307

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/48

摘要： Described is a triazole derivative represented by the formula (1): wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group, X1 and X2 are the same or different and each independently represents a hydrogen atom, a halogen atom or a halogenoalkyl and n stands for an integer of 0 to 2, or salt thereof; a preparation process of said compound and a pharmaceutical comprising said compound as an effective ingredient. The compound as described above has high antimycotic activity and is useful for the prevention and treatment of mammalian mycotic infections.

公开(公告)号：US6002028A

公开(公告)日：1999-12-14

申请号：US311058

申请日：1999-05-14

申请人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

发明人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato ,  Hideaki Matsuda

IPC分类号： C07D303/34 ,  C07D521/00

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/34

摘要： Described is a triazole derivative represented by the formula (1) or salt thereof, preparation process thereof, preparation intermediates represented by the formulas (2) and (3), and a pharmaceutical comprising the compound represented by the formula (1) or salt thereof. ##STR1## wherein n stands for 0, 1 or 2, X.sup.1 represents H or F and Y.sup.1 and Y.sup.2 each independently represents H, halogen or CF.sub.3.

公开(公告)号：US06737434B2

公开(公告)日：2004-05-18

申请号：US10380828

申请日：2003-03-19

申请人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Koji Kusano ,  Hiromichi Eto ,  Koichi Tachibana ,  Susumu Sato ,  Tadayoshi Taniyama

发明人： Minoru Tokizawa ,  Sunao Takeda ,  Yasushi Kaneko ,  Koji Kusano ,  Hiromichi Eto ,  Koichi Tachibana ,  Susumu Sato ,  Tadayoshi Taniyama

IPC分类号： C07D23360

CPC分类号： C07D233/64 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

摘要： Imidazole derivatives of the formula (1) or salts thereof, pharmaceuticals containing the derivatives or the salts, and intermediates for the synthesis of the derivatives or the salts (wherein R1 is lower alkyl; R2 is alkyl or aralkyl; and X1 is halogeno). These compounds exhibit G-CSF-like activities and can be substituted for G-CSF preparations.

摘要翻译： 式（1）的咪唑衍生物或其盐，含有衍生物或盐的药物，以及用于合成衍生物或盐的中间体（其中R 1为低级烷基; R 2为烷基或芳烷基; X 1为卤素）。 这些化合物表现出G-CSF样活性，可代替G-CSF制剂。

公开(公告)号：US06194592B1

公开(公告)日：2001-02-27

申请号：US09551569

申请日：2000-04-18

申请人： Sunao Takeda ,  Yasushi Kaneko ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

发明人： Sunao Takeda ,  Yasushi Kaneko ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

IPC分类号： C07D30334

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D303/48

摘要： Described is a triazole derivative represented by the formula (1): wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group, X1 and X2 are the same or different and each independently represents a hydrogen atom, a halogen atom or a halogenoalkyl and n stands for an integer of 0 to 2, or salt thereof; a preparation process of said compound and a pharmaceutical comprising said compound as an effective ingredient. The compound as described above has high antimycotic activity and is useful for the prevention and treatment of mammalian mycotic infections.

公开(公告)号：US06184396B2

公开(公告)日：2001-02-06

申请号：US09551854

申请日：2000-04-18

申请人： Sunao Takeda ,  Yasushi Kaneko ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

发明人： Sunao Takeda ,  Yasushi Kaneko ,  Minoru Tokizawa ,  Hiromichi Eto ,  Kazuya Ishida ,  Kazunori Maebashi ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Susumu Sato

IPC分类号： C07D30334

CPC分类号： C07D231/12 ,  C07C323/22 ,  C07C2601/02 ,  C07D233/56 ,  C07D249/08 ,  C07D303/34

摘要： Described is a triazole derivative represented by the formula (1): wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group, X1 and X2 are the same or different and each independently represents a hydrogen atom, a halogen atom or a halogenoalkyl and n stands for an integer of 0 to 2, or salt thereof; a preparation process of said compound and a pharmaceutical comprising said compound as an effective ingredient. The compound as described above has high antimycotic activity and is useful for the prevention and treatment of mammalian mycotic infections.