公开(公告)号：US20040209919A1

公开(公告)日：2004-10-21

申请号：US10835442

申请日：2004-04-28

Applicant: TAKEDA CHEMICAL INDUSTRIES, LTD.

Inventor： Tadashi Makino ,  Tetsuro Tabata ,  Shin-Ichiro Hirai

IPC: A61K031/4439 ,  A61K033/00

CPC classification number: C07D401/12 ,  A61K9/1611 ,  A61K9/2009 ,  A61K9/5026 ,  A61K9/5078 ,  A61K31/44 ,  A61K31/4439 ,  A61K47/02 ,  Y10S514/951

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula 1 wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

Abstract translation: 本发明的药物组合物，其包含下式的苯并咪唑化合物其中R 1是氢，烷基，卤素，氰基，羧基，烷酰氧基，烷氧羰基烷基，氨基甲酰基，氨基甲酰基烷基，羟基，烷氧基，羟基烷基，三氟甲基，酰基，氨基甲酰氧基 ，硝基，酰氧基，芳基，芳氧基，烷硫基或烷基亚磺酰基，R 2是氢，烷基，酰基，烷氧羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，烷基羰基甲基，烷氧基羰基甲基或烷基磺酰基，R 3和R 5相同 或不同的，各自为氢，烷基，烷氧基或烷氧基烷氧基，R 4为氢，烷基，可任选氟化的烷氧基或烷氧基烷氧基，m为0至4的整数，以及碱性无机盐稳定剂， 身体稳定 镁和钙碱性无机盐稳定剂是特别有用的。

公开(公告)号：US20030211155A1

公开(公告)日：2003-11-13

申请号：US10335421

申请日：2003-01-03

Applicant: TAKEDA CHEMICAL INDUSTRIES, LTD.

Inventor： Tadashi Makino ,  Tetsuro Tabata ,  Shin-Ichiro Hirai

IPC: A61K031/4439 ,  B05D003/00 ,  A61K009/28

CPC classification number: C07D401/12 ,  A61K9/1611 ,  A61K9/2009 ,  A61K9/5026 ,  A61K9/5078 ,  A61K31/44 ,  A61K31/4439 ,  A61K47/02 ,  Y10S514/925 ,  Y10S514/927 ,  Y10S514/951

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula 1 wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonyl-methyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

Abstract translation: 本发明的药物组合物，其包含下式的苯并咪唑化合物其中R 1是氢，烷基，卤素，氰基，羧基，烷酰氧基，烷氧羰基烷基，氨基甲酰基，氨基甲酰基烷基，羟基，烷氧基，羟基烷基，三氟甲基，酰基，氨基甲酰氧基 ，硝基，酰氧基，芳基，芳氧基，烷硫基或烷基亚磺酰基，R 2是氢，烷基，酰基，烷氧羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，烷基羰基 - 甲基，烷氧基羰基甲基或烷基磺酰基，R 3和R 5是 相同或不同，各自为氢，烷基，烷氧基或烷氧基烷氧基，R 4为氢，烷基，可任选氟化的烷氧基或烷氧基烷氧基，m为0至4的整数，碱性无机盐稳定 代理，身体稳定。 镁和钙碱性无机盐稳定剂是特别有用的。

公开(公告)号：US20020137771A1

公开(公告)日：2002-09-26

申请号：US10079958

申请日：2002-02-19

Applicant: TAKEDA CHEMICAL INDUSTRIES, LTD.

Inventor： Tadashi Makino ,  Tetsuro Tabata ,  Shin-Ichiro Hirai

IPC: A61K031/4439 ,  B01J013/00

CPC classification number: C07D401/12 ,  A61K9/1611 ,  A61K9/2009 ,  A61K9/5026 ,  A61K9/5078 ,  A61K31/44 ,  A61K31/4439 ,  A61K47/02 ,  Y10S514/925 ,  Y10S514/927 ,  Y10S514/951

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula 1 wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

Abstract translation: 本发明的药物组合物包含下式的苯并咪唑化合物其中R 1是氢，烷基，卤素，氰基，羧基，烷氧羰基，烷氧基烷基，氨基甲酰基，氨基甲酰基烷基，羟基，烷氧基，羟基烷基，三氟甲基，酰基，氨基甲酰氧基，硝基， 酰氧基，芳基，芳氧基，烷硫基或烷基亚磺酰基，R2是氢，烷基，酰基，烷酰氧基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，烷基羰基甲基，烷氧基羰基甲基或烷基磺酰基，R3和R5相同或不同，各自为氢，烷基，烷氧基或烷氧基烷氧基 ，R4为氢，烷基，可任选氟化的烷氧基或烷氧基烷氧基，m为0〜4的整数，碱性无机盐稳定剂为物理上稳定的。 镁和钙碱性无机盐稳定剂是特别有用的。

公开(公告)号：US20020039598A1

公开(公告)日：2002-04-04

申请号：US09924234

申请日：2001-08-08

Applicant: Takeda Chemical Industries, Ltd.

Inventor： Tadashi Makino ,  Tetsuro Tabata ,  Shin-Ichiro Hirai

IPC: A61K009/30 ,  A61K009/16 ,  A61K009/50 ,  A61K031/4439

CPC classification number: C07D401/12 ,  A61K9/1611 ,  A61K9/2009 ,  A61K9/5026 ,  A61K9/5078 ,  A61K31/44 ,  A61K31/4439 ,  A61K47/02 ,  Y10S514/925 ,  Y10S514/927 ,  Y10S514/951

Abstract: The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula 1 wherein R1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful.

Abstract translation: 本发明的药物组合物包含下式的苯并咪唑化合物其中R 1是氢，烷基，卤素，氰基，羧基，烷氧羰基，烷氧基烷基，氨基甲酰基，氨基甲酰基烷基，羟基，烷氧基，羟基烷基，三氟甲基，酰基，氨基甲酰氧基，硝基， 酰氧基，芳基，芳氧基，烷硫基或烷基亚磺酰基，R2是氢，烷基，酰基，烷酰氧基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，烷基羰基甲基，烷氧基羰基甲基或烷基磺酰基，R3和R5相同或不同，各自为氢，烷基，烷氧基或烷氧基烷氧基 ，R4为氢，烷基，可任选氟化的烷氧基或烷氧基烷氧基，m为0〜4的整数，碱性无机盐稳定剂为物理上稳定的。 镁和钙碱性无机盐稳定剂是特别有用的。