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1. 发明申请

WO1994017058A1 IMIDAZOLE COMPOUND 审中-公开
标题翻译：咪唑化合物
公开(公告)号：WO1994017058A1
公开(公告)日：1994-08-04
申请号：PCT/JP1993001822
申请日：1993-12-15
申请人： THE GREEN CROSS CORPORATION , YANAI, Kzuhiko , WATANABE, Takehiko , GOTOH, Tomokazu , SAKASHITA, Hiroshi , MURAKAMI, Kazuki , SUGIURA, Masanori , FUKAYA, Chikara
发明人： THE GREEN CROSS CORPORATION
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The invention aims at providing a novel compound having vitamin H3 receptor antagonism and relates to a compound represented by general formula (O) or pharmaceutically acceptable salts thereof, wherein m represents an integer of 4 to 6; R1 represents hydrogen, lower alkyl or aralkyl; R2 and R3 may be the same or different from each other and each represents hydrogen or lower alkyl; R4 represents hydrogen, linear or branched alkyl, cycloalkyl, cycloalkylalkyl, optionally substituted aryl, or optionally substituted aralkyl; Z represents R5 or A-R6; A represents S or O; R5 represents hydrogen, lower alkyl, optionally substituted aryl, or optionally substituted aralkyl; and R6 represents lower alkyl, lower alkenyl, lower alkynyl, or optionally substituted aralkyl.
摘要翻译：本发明旨在提供一种具有维生素H3受体拮抗作用的新化合物，涉及由通式（O）表示的化合物或其药学上可接受的盐，其中m表示4至6的整数; R1代表氢，低级烷基或芳烷基; R2和R3可以相同或不同，各自代表氢或低级烷基; R 4表示氢，直链或支链烷基，环烷基，环烷基烷基，任选取代的芳基或任选取代的芳烷基; Z表示R5或A-R6; A表示S或O; R5表示氢，低级烷基，任选取代的芳基或任选取代的芳烷基; 并且R 6表示低级烷基，低级烯基，低级炔基或任选取代的芳烷基。

2. 发明申请

WO1990011278A1 THIAZOLE COMPOUNDS AND APPLICATIONS THEREOF 审中-公开
标题翻译：噻唑化合物及其应用
公开(公告)号：WO1990011278A1
公开(公告)日：1990-10-04
申请号：PCT/JP1990000385
申请日：1990-03-22
申请人： THE GREEN CROSS CORPORATION , GOTO, Tomokazu; , OKANO, Tadashi; , SUGIYAMA, Naoki; , AKABOSHI, Fumihiko; , ONO, Shinichiro; , NAITO, Yoichiro; , YAMAURA, Yasunari; , FUKAYA, Chikara; , YOKOYAMA, Kazumasa;
发明人： THE GREEN CROSS CORPORATION
IPC分类号： C07D277/20
CPC分类号： C07D277/22 , C07D277/24 , C07D277/34 , C07D277/56 , C07D277/60
摘要： The invention provides thiazole compounds and pharmacologically acceptable salts thereof excellent in analgesic, antiinflammatory and antipyretic activities, represented by general formula (I), wherein R and R represent each independently hydrogen, halogen, alkyl, alkenyl, nitro, CF3, phenyl, substituted phenyl, pyridyl, substituted pyridyl, carboxyl, alkoxycarbonyl, -CONR R (wherein R and R represent each hydrogen or alkyl), acyl, hydroxy, alkoxy or thioalkyl, or alternatively R and R are combined together to form -(CH2)m- (wherein m is 3 to 5); R represents hydrogen or alkyl; R represents hydroxy, alkoxy or -NR R (wherein R and R represent each hydrogen or alkyl); X represents carbonyl or -(CH2)n- (wherein n is 0 or 1); and Y represents hydrogen, halogen, alkyl, nitro, CF3, -NR R (wherein R and R represent each hydrogen or alkyl), hydroxy (only when the position of X is para to the CHR COR group), alkoxy (only when the position of X is para to the CHR COR group), or alkylthio.
摘要翻译：本发明提供了由通式（I）表示的止痛，抗炎和解热活性优异的噻唑化合物及其药理学上可接受的盐，其中R 1和R 2各自独立地表示氢，卤素，烷基，链烯基，硝基， CF 3，苯基，取代的苯基，吡啶基，取代的吡啶基，羧基，烷氧基羰基，-CONR 5 R 6（其中R 5和R 6各自代表氢或烷基），酰基，羟基，烷氧基或硫代烷基或者R 1和R 2组合在一起形成 - （CH 2）m - （其中m为3至5）; R 3表示氢或烷基; R 4表示羟基，烷氧基或-NR 7 R 8（其中R 7和R 8表示各自的氢或烷基）。 X表示羰基或 - （CH 2）n - （其中n为0或1）; 和Y表示氢，卤素，烷基，硝基，CF 3，-NR 9 R 10（其中R 9和R 10表示各自的氢或烷基），羟基（仅当X的位置为对至CHR 3 COR 4基团），烷氧基（仅当X的位置对于CHR 3 COR 4基团时）或烷硫基。

3. 发明申请

WO1995003286A1 TRIAZOLE DERIVATIVE AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：三唑衍生物和药物用途
公开(公告)号：WO1995003286A1
公开(公告)日：1995-02-02
申请号：PCT/JP1994001215
申请日：1994-07-22
申请人： THE GREEN CROSS CORPORATION , AKAHOSHI, Fumihiko , OKADA, Takehiro , TAKEDA, Shinji , NAITO, Youichiro , FUKAYA, Chikara , KUWAHARA, Shigeki , KAJII, Masahiko , NISHIMURA, Hiroko , SUGIURA, Masanori
发明人： THE GREEN CROSS CORPORATION
IPC分类号： C07D249/14
CPC分类号： C07D487/04 , C07D249/14
摘要： Prophylactic or therapeutic agents for immune-related diseases, in particular, immunosuppressant, prophylactic or therapeutic agent for allergic diseases, prophylactic or therapeutic agent for eosinocyte-related diseases and eosinophilia inhibitor, said agents containing a novel mono- or bicyclic triazole derivative represented by general formula (I) or (III) or a pharmaceutically acceptable salt thereof as the active ingredient, wherein X represents O or S; and W represents -NR R or -SR . The derivatives have excellent activities of inhibiting eosinophilia and lymphocyte activation, low toxicity and persistent effect, and are particularly efficacious in treating accumulation and activation of eosinocytes and lymphocytes, inflammatory respiratory tract diseases, eosinocyte-related diseases such as eosinophilia, and immune-related diseases.
摘要翻译：用于免疫相关疾病的预防或治疗剂，特别是用于过敏性疾病的免疫抑制剂，预防或治疗剂，用于与嗜酸细胞有关的疾病和嗜酸性粒细胞减少症抑制剂的预防或治疗剂，所述药物含有一般性的一价或双环三唑衍生物式（I）或（III）或其药学上可接受的盐作为活性成分，其中X表示O或S; W表示-NR 4 R 5或-SR 6。该衍生物具有抑制嗜酸性粒细胞增多和淋巴细胞活化，低毒性和持续作用的优异活性，并且对于治疗嗜酸性细胞和淋巴细胞的积累和活化，炎症性呼吸道疾病，与嗜酸性粒细胞增多症有关的嗜酸粒细胞相关疾病和免疫相关疾病特别有效。

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