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公开(公告)号:US08138177B2
公开(公告)日:2012-03-20
申请号:US11909763
申请日:2006-03-02
申请人: Kazuo Ando , Makoto Kawai , Tsutomu Masuda , Hirofumi Omura
发明人: Kazuo Ando , Makoto Kawai , Tsutomu Masuda , Hirofumi Omura
IPC分类号: A61K31/541 , A61K31/5377 , A61K31/454 , C07D413/02 , C07D211/32 , C07D471/02
CPC分类号: C07D471/04 , C07D235/26 , C07D401/06 , C07D403/12 , C07D405/06 , C07D413/12 , C07D417/12
摘要: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts 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 binding 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, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, 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, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis or 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各自如本文所述,含有这些化合物的组合物和这些化合物在治疗 由CB2受体结合活性介导的病症,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,肠易激惹 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,ul 结肠炎,哮喘,皮炎,季节性过敏性鼻炎,胃食管反流病(GERD),便秘,腹泻,功能性胃肠道疾病,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,慢性阻塞性肺病(COPD),隐源性纤维化肺泡炎或支气管炎。
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公开(公告)号:US20110230467A1
公开(公告)日:2011-09-22
申请号:US13130527
申请日:2009-11-20
申请人: Shohei Shirakami , Fumie Takahashi , Yutaka Nakajima , Hirofumi Omura , Naohiro Aoyama , Hiroshi Sasaki , Takeshi Hondo , Hiroaki Tominaga
发明人: Shohei Shirakami , Fumie Takahashi , Yutaka Nakajima , Hirofumi Omura , Naohiro Aoyama , Hiroshi Sasaki , Takeshi Hondo , Hiroaki Tominaga
IPC分类号: A61K31/55 , A61K31/5513 , A61K31/5377 , A61P43/00 , A61K31/497 , A61K31/506 , A61K31/444 , A61K31/4439 , C07D401/14 , C07D413/14 , C07D401/12 , C07D417/14 , C07D409/14 , C07D401/00
CPC分类号: C07D401/12 , C07D213/82 , C07D401/14 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/10
摘要: [Problem] The present invention provides a 4,6-diaminonicotinamide compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for treating diseases caused by undesirable and/or abnormal cytokine signal transduction.[Means for Solution] The present inventors have extensively studied compounds having a JAK3 inhibitory action, and as a result, they have found that a 4,6-diaminonicotinamide compound which is the compound of the present invention has an excellent JAK3 inhibitory action and is useful as an agent for preventing or treating diseases caused by undesirable and/or abnormal cytokine signal transduction, thereby completing the present invention.
摘要翻译: 本发明提供了可用作药物组合物的活性成分的特征的4,6-二氨基烟酰胺化合物,特别是用于治疗由不希望的和/或异常的细胞因子信号转导引起的疾病的药物组合物。 [解决方案]本发明人广泛研究了具有JAK3抑制作用的化合物,结果发现作为本发明化合物的4,6-二氨基烟酰胺化合物具有优异的JAK3抑制作用, 可用作预防或治疗由不良和/或异常细胞因子信号转导引起的疾病的药剂,从而完成本发明。
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公开(公告)号:US20090298811A1
公开(公告)日:2009-12-03
申请号:US12440646
申请日:2007-09-03
申请人: Kazuo Ando , Ingrid Price Buchler , Shridhar Gajanan Hedge , Makoto Kawai , Tsutomu Masuda , Hirofumi Omura
发明人: Kazuo Ando , Ingrid Price Buchler , Shridhar Gajanan Hedge , Makoto Kawai , Tsutomu Masuda , Hirofumi Omura
IPC分类号: A61K31/55 , A61K31/5377 , A61K31/4965 , A61K31/437 , A61K31/4245 , A61K31/4184 , C07D405/14 , C07D413/06 , C07D403/08 , C07D471/04 , C07D413/12 , C07D235/24
CPC分类号: C07D413/06 , A61K31/16 , C07D235/26 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/12 , C07D413/14 , C07D471/04
摘要: This invention relates to compounds and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein. These compounds are useful in the treatment of a condition mediated by CB2 receptor binding 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, spasticity, epilepsy, Tourette's syndrome, Parkinson's disease, neuroprotection, anxiety, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, cachexia, nausea, emesis, chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasodialation, hypertension, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis and bronchitis.
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公开(公告)号:US20090181957A1
公开(公告)日:2009-07-16
申请号:US11909763
申请日:2006-03-02
申请人: Kazuo Ando , Makoto Kawai , Tsutomu Masuda , Hirofumi Omura
发明人: Kazuo Ando , Makoto Kawai , Tsutomu Masuda , Hirofumi Omura
IPC分类号: A61K31/541 , C07D413/02 , A61K31/5377 , C07D211/32 , A61K31/454 , C07D235/04 , A61K31/4184 , C07D471/02 , A61K31/437 , C07D413/14 , C07D417/02 , A61P29/00 , A61P35/00
CPC分类号: C07D471/04 , C07D235/26 , C07D401/06 , C07D403/12 , C07D405/06 , C07D413/12 , C07D417/12
摘要: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts 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 binding 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, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, 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, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis or 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各自如本文所述,含有这些化合物的组合物和这些化合物在治疗 由CB2受体结合活性介导的病症,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,肠易激惹 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,ul 结肠炎,哮喘,皮炎,季节性过敏性鼻炎,胃食管反流病(GERD),便秘,腹泻,功能性胃肠道疾病,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,慢性阻塞性肺病(COPD),隐源性纤维化肺泡炎或支气管炎。
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公开(公告)号:US5190826A
公开(公告)日:1993-03-02
申请号:US699073
申请日:1991-05-13
申请人: Kenichi Asahina , Naoki Ueda , Hirofumi Omura
发明人: Kenichi Asahina , Naoki Ueda , Hirofumi Omura
CPC分类号: B32B17/10761 , B32B17/10009 , B32B17/10045 , B32B17/10064 , B32B27/30 , Y10T428/3163 , Y10T428/31909 , Y10T428/31942 , Y10T428/31946
摘要: An interlayer for use in sound-insulating laminated glasses which is in the form of a laminated film of two kinds of resin films (A) and (B), each comprising a polyvinyl acetal acetalized with an aldehyde having 6 to 10 carbon atoms for the film (A) or with an aldehyde having 1 to 4 carbon atoms for the film (B), or is in the form of a resin film (C) comprising a mixture of the two kinds of polyvinyl acetal resins. The interlayer mitigates the coincidence effect to prevent the reduction of TL value without impairing the basic characteristics required of laminated glasses thereby permitting the interlayer to exhibit outstanding sound-insulating properties over a wide temperature range for a prolonged period of time.
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公开(公告)号:US4925725A
公开(公告)日:1990-05-15
申请号:US293579
申请日:1989-01-04
CPC分类号: B32B17/10577 , B29C59/022 , B32B17/10981 , B29C59/04 , Y10T428/24479 , Y10T428/3163
摘要: An interlayer for a laminated glass, said interlayer being composed of a film or sheet of a thermoplastic resin, at least one surface of the film or sheet of a thermoplastic resin having numerous coarse raised and depressed portions and numerous fine raised and depressed portions existing on the surfaces of the coarse raised and depressed portions, the average distance between two adjacent coarse depressed or raised portions being about 2 to about 10 times the 10-point average roughness of the coarse raised and depressed portions measured in accordance with ISO-R468.
摘要翻译: 夹层玻璃的中间层,所述中间层由热塑性树脂的薄膜或薄片组成,热塑性树脂薄膜或薄片的至少一个表面具有许多粗的凸起和凹陷部分,以及许多细小的凸起和凹陷部分存在于 粗凸起和凹陷部分的表面,两个相邻的粗凹陷或凸起部分之间的平均距离是根据ISO-R468测量的粗提升和凹陷部分的10点平均粗糙度的约2至约10倍。
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