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1. 发明授权

US06951867B2 N-substituted piperidinyl-imidazopyridine compounds as 5-HT4 receptor modulators 失效
标题翻译： N-取代的哌啶基 - 咪唑并吡啶化合物作为5-HT 4受体调节剂
公开(公告)号：US06951867B2
公开(公告)日：2005-10-04
申请号：US10667182
申请日：2003-09-17
申请人： Yasuhiro Katsu , Kana Kon-I , Mikio Morita , Hirohide Noguchi , Chikara Uchida
发明人： Yasuhiro Katsu , Kana Kon-I , Mikio Morita , Hirohide Noguchi , Chikara Uchida
IPC分类号： C07D471/04 , A61K31/437 , A61P1/04
CPC分类号： C07D471/04
摘要： This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt, amide or ester thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom, etc.; R3 represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of R3 is substituted by at least one substituent selected from the group consisting of substituents α; said substituents α is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents α, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，酰胺或酯，其中R 1表示氢原子或卤素原子; R 2表示氢原子等; R 3表示具有1至10个碳原子的烷基; 所述R 3的烷基被至少一个选自取代基α的取代基取代; 所述取代基α是芳基，羟基，氧代等; 所述芳基具有6至10个碳原子; 所述芳基是未取代的或被至少一个具有1至6个碳原子的烷基取代; 所述杂环基和所述杂环羰基的杂环部分，两个取代基α为含有1至4个选自氮原子，氧原子和硫原子的杂原子的5至10元环基这些化合物具有5-HT 受体结合活性，因此可用于治疗哺乳动物，特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。本发明还提供了包含上述化合物的药物组合物。

2. 发明授权

US07012080B2 Imidazopyridine compounds as 5-HT4 receptor agonists 失效
标题翻译：咪唑并吡啶化合物作为5-HT4受体激动剂
公开(公告)号：US07012080B2
公开(公告)日：2006-03-14
申请号：US10667188
申请日：2003-09-17
申请人： Satoru Iguchi , Yasuhiro Katsu , Kana Kon-I , Hirohide Noguchi , Chikara Uchida
发明人： Satoru Iguchi , Yasuhiro Katsu , Kana Kon-I , Hirohide Noguchi , Chikara Uchida
IPC分类号： A61K31/437 , C07D471/04 , A61P1/04
CPC分类号： C07D471/04
摘要： This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a methyl group or an ethyl group; R3 represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms; with the proviso that when the terminal carbon atom of said alkyl group of R3 is substituted by said alkoxy group, said alkyl group is a branched alkyl group. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中R 1表示氢原子或卤素原子; R 2表示甲基或乙基; R 3表示具有3至6个碳原子的支链烷基或具有3至6个碳原子的烷基，被具有1至6个碳原子的烷氧基取代; 条件是当所述R 3烷基的末端碳原子被所述烷氧基取代时，所述烷基是支链烷基。这些化合物具有5-HT 4受体结合活性，因此可用于治疗哺乳动物，特别是人类中的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。本发明还提供了包含上述化合物的药物组合物。

3. 发明授权

US07598393B2 Sulfonyl benzimidazole derivatives 失效
标题翻译：磺酰基苯并咪唑衍生物
公开(公告)号：US07598393B2
公开(公告)日：2009-10-06
申请号：US11266107
申请日：2005-11-02
申请人： Kana Kon-I , Miyako Matsumizu , Akiko Shima
发明人： Kana Kon-I , Miyako Matsumizu , Akiko Shima
IPC分类号： C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D235/16 , A61K31/33
CPC分类号： C07D471/04 , C07D235/08 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/06
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中A，B，R 1，R 2和R 3各自如本文所述，含有这些化合物的组合物以及这些化合物在治疗中的用途由CB2受体活性介导的病症。

4. 发明申请

US20060094750A1 Sulfonyl benzimidazole derivatives 失效
标题翻译：磺酰基苯并咪唑衍生物
公开(公告)号：US20060094750A1
公开(公告)日：2006-05-04
申请号：US11266107
申请日：2005-11-02
申请人： Kana Kon-I , Miyako Matsumizu , Akiko Shima
发明人： Kana Kon-I , Miyako Matsumizu , Akiko Shima
IPC分类号： A61K31/4745 , A61K31/4184 , C07D471/02
CPC分类号： C07D471/04 , C07D235/08 , C07D401/06 , C07D403/06 , C07D405/06 , C07D413/06
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, GERD, constipation, diarrhea, functional gastrointestinal disorders, irritable bowel syndrome, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, COPD, cryptogenic fibrosing alveolitis and bronchitis.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中A，B，R 1，R 2和R 3， / SUP>各自如本文所述，含有这些化合物的组合物以及这些化合物在治疗由CB2受体活性介导的病症（例如但不限于炎性疼痛，伤害性疼痛，神经性疼痛，纤维肌痛）慢性腰痛，内脏痛，急性脑缺血，疼痛，慢性疼痛，急性疼痛，疱疹后神经痛，神经病，神经痛，糖尿病性神经病，HIV相关神经病，神经损伤，类风湿性关节炎疼痛，骨关节炎疼痛，背痛，癌症疼痛，牙痛，纤维肌痛，神经炎，坐骨神经痛，炎症，神经变性疾病，咳嗽，支气管收缩，肠易激综合征（IBS），炎性肠病（IBD），结肠炎，脑血管缺血，呕吐如癌症化疗诱发呕吐，类风湿关节炎，a 哮喘，克罗恩病，溃疡性结肠炎，哮喘，皮炎，季节性过敏性鼻炎，GERD，便秘，腹泻，功能性胃肠道疾病，肠易激综合征，皮肤T细胞淋巴瘤，多发性硬化症，骨关节炎，牛皮癣，系统性红斑狼疮，糖尿病，青光眼，骨质疏松症，肾小球肾炎，肾缺血，肾炎，肝炎，脑中风，血管炎，心肌梗死，脑缺血，可逆气道阻塞，成人呼吸道疾病综合征，COPD，隐源性纤维化肺泡炎和支气管炎。

5. 发明授权

US07700618B2 Sulfonyl benzimidazole derivatives 失效
标题翻译：磺酰基苯并咪唑衍生物
公开(公告)号：US07700618B2
公开(公告)日：2010-04-20
申请号：US12280586
申请日：2007-02-23
申请人： Tomoki Kato , Kana Kon-I , Yohei Yuki , Kazuo Ando
发明人： Tomoki Kato , Kana Kon-I , Yohei Yuki , Kazuo Ando
IPC分类号： A61K31/437 , A61K31/4184 , C07D471/04 , C07D235/08
CPC分类号： C07D235/08 , C07D235/12 , C07D405/12 , C07D471/04
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R1, R2, R3, R4, R5, m and n are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, GERD, constipation, diarrhea, functional gastrointestinal disorders, irritable bowel syndrome, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, COPD, cryptogenic fibrosing alveolitis and bronchitis.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3，R 4，R 5，m和n各自如本文所述，和含有这些化合物的组合物，治疗由CB2受体活性介导的病症，例如但不限于炎症性疼痛，伤害性疼痛，神经性疼痛，纤维肌痛，慢性腰痛，内脏痛，急性脑缺血，疼痛，慢性疼痛，急性疼痛，疱疹后神经痛，神经病，神经痛，糖尿病性神经病，HIV相关神经病，神经损伤，类风湿关节炎疼痛，骨关节炎疼痛，背痛，癌症疼痛，牙痛，纤维肌痛，神经炎，坐骨神经痛，炎症，神经变性疾病，咳嗽，支气管收缩，肠易激综合征（IBS），炎性肠病（IBD），结肠炎，脑血管缺血，呕吐如癌症化疗诱发的呕吐，类风湿性关节炎，哮喘，克罗恩病溃疡性结肠炎，哮喘，皮炎，季节性过敏性鼻炎，GERD，便秘，腹泻，功能性胃肠道疾病，肠易激综合征，皮肤T细胞淋巴瘤，多发性硬化症，骨关节炎，牛皮癣，系统性红斑狼疮，糖尿病，青光眼，骨质疏松症，肾小球性肾炎，肾缺血，肾炎，肝炎，脑中风，血管炎，心肌梗死，脑缺血，可逆性气道阻塞，成人呼吸道疾病综合征，COPD，隐源性纤维化肺泡炎和支气管炎。

6. 发明申请

US20090137584A1 SULFONYL BENZIMIDAZOLE DERIVATIVES 失效
标题翻译：磺酰苯并咪唑衍生物
公开(公告)号：US20090137584A1
公开(公告)日：2009-05-28
申请号：US12280586
申请日：2007-02-23
申请人： Tomoki Kato , Kana Kon-I , Yohei Yuki , Kazuo Ando
发明人： Tomoki Kato , Kana Kon-I , Yohei Yuki , Kazuo Ando
IPC分类号： A61K31/5377 , C07D235/08 , C07D413/12 , A61P25/00 , A61K31/4184
CPC分类号： C07D235/08 , C07D235/12 , C07D405/12 , C07D471/04
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R1, R2, R3, R4, R5, m and n are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, GERD, constipation, diarrhea, functional gastrointestinal disorders, irritable bowel syndrome, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, COPD, cryptogenic fibrosing alveolitis and bronchitis.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3，R 4，R 5，m和n各自如本文所述，和含有这些化合物的组合物，治疗由CB2受体活性介导的病症，例如但不限于炎症性疼痛，伤害性疼痛，神经性疼痛，纤维肌痛，慢性腰痛，内脏痛，急性脑缺血，疼痛，慢性疼痛，急性疼痛，疱疹后神经痛，神经病，神经痛，糖尿病性神经病，HIV相关神经病，神经损伤，类风湿关节炎疼痛，骨关节炎疼痛，背痛，癌症疼痛，牙痛，纤维肌痛，神经炎，坐骨神经痛，炎症，神经变性疾病，咳嗽，支气管收缩，肠易激综合征（IBS），炎性肠病（IBD），结肠炎，脑血管缺血，呕吐如癌症化疗诱发的呕吐，类风湿性关节炎，哮喘，克罗恩病溃疡性结肠炎，哮喘，皮炎，季节性过敏性鼻炎，GERD，便秘，腹泻，功能性胃肠道疾病，肠易激综合征，皮肤T细胞淋巴瘤，多发性硬化症，骨关节炎，牛皮癣，系统性红斑狼疮，糖尿病，青光眼，骨质疏松症，肾小球性肾炎，肾缺血，肾炎，肝炎，脑中风，血管炎，心肌梗死，脑缺血，可逆性气道阻塞，成人呼吸道疾病综合征，COPD，隐源性纤维化肺泡炎和支气管炎。

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