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1. 发明专利

JP2002371042A Dimamine compound, method for producing the same and use thereof 审中-公开
标题翻译：二甲胺化合物，其生产方法及其用途
公开(公告)号：JP2002371042A
公开(公告)日：2002-12-26
申请号：JP2001177827
申请日：2001-06-12
申请人： Takeda Chem Ind Ltd , 武田薬品工業株式会社
发明人： KAMIYAMA KEIJI , KANZAKI NAOYUKI , HASUOKA ATSUSHI , MOCHIZUKI MANABU , KAWAMOTO TETSUJI
IPC分类号： C07D249/10 , A61K31/135 , A61K31/138 , A61K31/166 , A61K31/18 , A61K31/215 , A61K31/24 , A61K31/34 , A61K31/381 , A61K31/40 , A61K31/404 , A61K31/415 , A61K31/4155 , A61K31/4184 , A61K31/4192 , A61K31/42 , A61K31/422 , A61K31/425 , A61K31/427 , A61K31/429 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4439 , A61K31/455 , A61K31/47 , A61K31/498 , A61K31/542 , A61K31/55 , A61K31/7068 , A61K45/00 , A61P31/18 , A61P43/00 , C07C217/08 , C07C217/14 , C07C229/12 , C07C233/62 , C07C233/78 , C07C235/50 , C07C235/70 , C07C311/13 , C07C311/16 , C07C311/18 , C07C311/29 , C07C311/46 , C07C317/28 , C07C323/25 , C07D209/08 , C07D209/42 , C07D213/70 , C07D213/78 , C07D213/81 , C07D213/82 , C07D215/48 , C07D223/16 , C07D231/14 , C07D233/64 , C07D235/08 , C07D235/28 , C07D237/28 , C07D241/44 , C07D249/18 , C07D261/18 , C07D277/20 , C07D277/56 , C07D285/06 , C07D307/68 , C07D307/79 , C07D333/34 , C07D333/40 , C07D333/70 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D471/16 , C07D487/16 , C07D513/04 , C07D513/16
摘要： PROBLEM TO BE SOLVED: To obtain a diamine compound useful for the treatment of acquired immune deficiency, cancer, or the like, based on CXCR4 antagonistic action.
SOLUTION: The diamine compound is a compound expressed by formula (I) (R
1 and R
2 are each H or an alkyl; A is a (substituted) cyclic group; X is a bond or an alkylene or an alkenylene group bonded to A optionally through a heteroatom; Y is S, O, C(=O)-N(R
15 ) (R
15 is H or a (substituted) alkyl), SO
2 -N(R
16 ) (R
16 is H or a (substxtuted) alkyl), C(=O)-O, SO, SO
2 , or N(R
17 ) (R
17 is H or a (substituted) alkyl); A-X-Y may form a (substituted) heterocyclic group; (1) is 2-6; (m) is 2-4; and (n) is O-8) (when Y is -N(R
17 ), A is a (substituted) aromatic heterocyclic group) or its salt.
COPYRIGHT: (C)2003,JPO
摘要翻译：要解决的问题：基于CXCR4拮抗作用获得可用于治疗获得性免疫缺陷，癌症等的二胺化合物。解决方案：二胺化合物是由式（I）表示的化合物（R 1和R 2各自为H或烷基; A为（取代的）环基; X为亚烷基或亚烯基基团任选地通过杂原子键合; Y是S，O，C（= O）-N（R 15）（R 15是H或（取代的）烷基），SO 2 -N（R 16）（R 16）是H或（取代的）烷基），C（= O）-O，SO，SO 2或N（R 17）（R 17）是H或）; AXY可以形成（取代的）杂环基;（1）为2-6;（m）为2-4;和（n）为O-8）（当Y为-N（R 17） A是（取代的）芳族杂环基）或其盐。

2. 发明专利

JP2003313186A Benzimidazole compound, method for producing the same, and application of the same 审中-公开
标题翻译：苯并咪唑化合物，其制备方法及其应用
公开(公告)号：JP2003313186A
公开(公告)日：2003-11-06
申请号：JP2002277780
申请日：2002-09-24
申请人： Takeda Chem Ind Ltd , 武田薬品工業株式会社
发明人： KAMIYAMA KEIJI , SATO FUMIHIKO , SAKANO HIROSHI , HASUOKA ATSUSHI
IPC分类号： C07D401/12 , A61K31/4439 , A61P1/04 , A61P31/04 , A61P35/00 , C07D405/14
摘要： PROBLEM TO BE SOLVED: To obtain a prodrug of 2-[[[3-methy1-4-(2,2,2-trifluoroethoxy)-2- pyridyl]methyl]sulfinyl]-1H-benzimidazole, having excellent acid stability. SOLUTION: The prodrug comprises a benzimidazole compound of formula (I) (A and R are each defined in the specification) or its salt. The prodrug has the following effects (1) to (5): (1) antiulcer action, gastic acid secretion- suppressing action, mucosa-preventing action, Helicobacter pylori-resisting action, or the like, which are excellent in an organism; (2) low toxicity; (3) the excellent acid stability (so that the prodrug is administered at a reduced cost because it is needless to be used as an enteric preparation, and further the prodrug is easily administered due to reduction of a size of a preparation); (4) rapid absorption when compared with the enteric preparation (so that the gastic acid secretion-suppressing action is rapidly developed); and (5) persistence. COPYRIGHT: (C)2004,JPO
摘要翻译：待解决的问题：获得具有优异酸性的2 - [[[3-甲基-4-（2,2,2-三氟乙氧基）-2-吡啶基]甲基]亚磺酰基] -1H-苯并咪唑的前药稳定性。解决方案：前药包括式（I）的苯并咪唑化合物（A和R各自在说明书中定义）或其盐。前药具有以下效果（1）〜（5）：（1）生物体优异的抗溃疡作用，胃酸分泌抑制作用，粘膜预防作用，幽门螺杆菌抗性作用等，（2）毒性低; （3）优异的酸稳定性（因为不需要用作肠溶制剂，所以前药以降低的成本进行给药，而且由于制剂的尺寸减小，前药容易施用）; （4）与肠溶制剂相比，快速吸收（使得胃酸分泌抑制作用迅速发展）; 和（5）坚持。版权所有（C）2004，JPO

3. 发明专利

JP2013100316A Acid secretion inhibitor 有权
标题翻译：酸分泌抑制剂
公开(公告)号：JP2013100316A
公开(公告)日：2013-05-23
申请号：JP2013001273
申请日：2013-01-08
申请人： Takeda Chem Ind Ltd , 武田薬品工業株式会社
发明人： KAJINO MASAHIRO , HASUOKA ATSUSHI , NISHIDA HARUYUKI
IPC分类号： A61K31/4155 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/444 , A61K31/501 , A61K31/506 , A61K31/519 , A61K45/00 , A61P31/04 , A61P43/00
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical agent which has a superior acid secretion inhibitory effect and is used for Helicobacter pylori sterilizing.SOLUTION: The pharmaceutical agent used for Helicobacter pylori sterilizing includes a compound represented by formula (I) wherein Ris a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), Ris an optionally substituted Caryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, Rand Rare each a hydrogen atom, or one of Rand Ris a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and Ris an alkyl group.
摘要翻译：待解决的问题：提供具有优异的酸分泌抑制作用并用于幽门螺杆菌灭菌的药剂。解决方案：用于幽门螺杆菌灭菌的药剂包括由式（I）表示的化合物，其中R 1 是任选与苯稠合的含氮单环杂环基环或杂环，任选地与苯环或杂环稠合的含氮单环杂环基任选具有取代基，R 2是任选取代的C 6-4 芳基，任选取代的噻吩基或任选取代的吡啶基，R 4 各自为氢原子，或者R 3 中的一个为氢原子，并且R 4 为氢原子，另一个是任选取代的低级烷基，酰基，卤素原子，氰基或硝基，并且R 5是烷基。版权所有（C）2013，JPO＆INPIT

4. 发明专利

JP2008056659A Acid secretion inhibitor 有权
标题翻译：酸分泌抑制剂
公开(公告)号：JP2008056659A
公开(公告)日：2008-03-13
申请号：JP2007155692
申请日：2007-06-12
申请人： Takeda Chem Ind Ltd , 武田薬品工業株式会社
发明人： KAJINO MASAHIRO , HASUOKA ATSUSHI , NISHIDA HARUYUKI
IPC分类号： C07D401/12 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/506 , A61K31/519 , A61P1/04 , A61P11/06 , A61P11/08 , A61P31/04 , A61P35/00 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D487/04
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D417/12 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To obtain a compound having excellent inhibitory action on acid secretion and antiulcer action. SOLUTION: The medicine comprises a compound represented by formula (I), its salt or its prodrug (R 1 is a monocyclic nitrogen-containing heterocyclic group which may be condensed with a benzene ring or a heterocyclic ring; the monocyclic nitrogen-containing heterocyclic group which may be condensed with the benzene ring or the heterocyclic ring may arbitrarily contain a substituent group; R 2 is a 6-14C aryl group which may be substituted, a thienyl group which may be substituted or a pyridyl group which may be substituted; R 3 and R 4 are each a hydrogen atom or one of R 3 and R 4 is a hydrogen atom and the other is a lower alkyl group which may be substituted, an acyl group, a halogen atom, a cyano group or a nitro group; R 5 is an alkyl group). COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：获得对酸分泌和抗溃疡作用具有优异抑制作用的化合物。解决方案：药物包含由式（I）表示的化合物，其盐或其前药（R 1 SP 1是可以与苯环或苯环稠合的单环含氮杂环基团）可以与苯环或杂环稠合的单环含氮杂环基可以任意含有取代基; R 2是可以被取代的6-14C芳基，可被取代的噻吩基或可被取代的吡啶基; R 3和R 4都是氢原子或R 3中的一个， SP>和R 4 是氢原子，另一个是可以被取代的低级烷基，酰基，卤素原子，氰基或硝基; R 5 是烷基）。版权所有（C）2008，JPO＆INPIT

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