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：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.

公开(公告)号：US5986144A

公开(公告)日：1999-11-16

申请号：US311057

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： C07D249/08 ,  C07D303/34 ,  C07D521/00 ,  C07C323/07

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. 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.

摘要翻译： 描述由式（1）表示的三唑衍生物或其盐，其制备方法，由式（2）和（3）表示的制备中间体，以及包含式（1）表示的化合物或其盐的药物 。 其中n表示0,1或2，X 1表示H或F，Y 1和Y 2各自独立地表示H，卤素或CF 3。

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：US5164513A

公开(公告)日：1992-11-17

申请号：US747632

申请日：1991-08-20

申请人： Minoru Tokizawa ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tatsuhiko Kateri

发明人： Minoru Tokizawa ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tatsuhiko Kateri

IPC分类号： C07D521/00

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

摘要： Novel imidazole derivatives and their acid adducts are disclosed. The imidazole derivatives are represented by formula: ##STR1## wherein R.sub.1 represents an alkyl group, R.sub.2 represents a hydrogen atom, an alkyl group which may have a substituent, or an aralkyl group which may have a substituent, provided that R.sub.1 and R.sub.2 are not both methyl groups at the same time. They have strong antimicrobial activity, especially against those fungi belonging to the genera Candida, Trichophyton, Microsporum, and Epidermorphyton, as well as against Gram-positive bacteria, and thus is useful as a antimicrobial agent.

摘要翻译： 公开了新的咪唑衍生物及其酸加成物。 咪唑衍生物由下式表示：其中R1表示烷基，R2表示氢原子，可以具有取代基的烷基或可具有取代基的芳烷基，条件是R1和 R2不同时同时为甲基。 它们具有很强的抗微生物活性，特别是针对属于假丝酵母属，毛癣菌属，微孢子虫属和表皮假单胞菌属的真菌，以及抗革兰氏阳性菌，因此可用作抗微生物剂。

公开(公告)号：US5147886A

公开(公告)日：1992-09-15

申请号：US626545

申请日：1990-12-12

申请人： Minoru Tokizawa ,  Yoshihiko Kanamaru ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi ,  Kazunori Maebashi ,  Naokata Taido ,  Ryuichi Kawahara

发明人： Minoru Tokizawa ,  Yoshihiko Kanamaru ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi ,  Kazunori Maebashi ,  Naokata Taido ,  Ryuichi Kawahara

IPC分类号： C07D249/08 ,  C07D521/00

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

摘要： A triazole derivative is disclosed. The compound have a general formula, ##STR1## wherein R.sup.1 and R.sup.2 represent a hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 together form a lower alkylene group, R.sup.3 represents a lower alkyl group, and n denotes an integer of 0 to 2, provided that not both R.sup.1 and R.sup.2 are a hydrogen atom at the same time. The triazole derivatives and their salts are effective for curing or preventing deep-seated mycoses, e.g. mycotic meningitis, mycotic infectious diseases of respiratory organs, fungemia, and urinary tract mycosis.

公开(公告)号：US4987144A

公开(公告)日：1991-01-22

申请号：US412152

申请日：1989-09-25

申请人： Yoshihiko Kanamaru ,  Minoru Tokizawa ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi

发明人： Yoshihiko Kanamaru ,  Minoru Tokizawa ,  Masaru Matsumoto ,  Takemitsu Asaoka ,  Hideaki Matsuda ,  Tadayuki Kuraishi

IPC分类号： A61K31/41 ,  A61P31/04 ,  A61P31/10 ,  C07D249/08 ,  C07D521/00

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

摘要： Disclosed herein is 1,3-bis(1,2,4-triazol-1-yl)-2-(4-trifluoromethylphenyl)propan-2-ol represented by the following formula (I): ##STR1## An antimycotic preparation containing the triazole compound (I) is also disclosed. Also disclosed is a method for the prevention and/treatment of a deep-seated mycosis of a human or mammal, which comprises administering an effective dose of the triazole compound (I) to the human or mammal.