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1.发明公开SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS 审中-公开取代的咪唑并[1,2-B]哒嗪衍生物，药物组合物和用作β-分泌酶抑制剂的方法
公开(公告)号：EP2549874A1
公开(公告)日：2013-01-30
申请号：EP11759968.8
申请日：2011-03-21
发明人： MJALLI, Adnan, M.M. , HARI, Anitha , GADDAM, Bapu , GOHIMUKKULA, Devi, Reddy , POLISETTI, Dharma, Rao , RAO, Mohan , GOWDA, Raju, Bore , ANDREWS, Robert, Carl , XIE, Rongyuan , SAHOO, Soumya, P. , REN, Tan , BANNER, William, Kenneth
IPC分类号： A01N43/52 , A61K31/415
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutically acceptable salts thereof, and tautomers of any of the foregoing, where such compounds inhibit β-site amyloid precursor protein-cleaving enzyme (BACE), which may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention also provides pharmaceutical compositions comprising any of these compounds and the use of any of these compounds and compositions in the treatment of diseases, disorders, or conditons in which BACE is involved.
摘要翻译： 本发明提供了取代的咪唑并[1,2-b]哒嗪衍生物，其药学上可接受的盐和任何前述的互变异构体，其中这些化合物抑制可能有用的β-位点淀粉样前体蛋白切割酶（BACE） 用于治疗BACE所涉及的疾病，如阿尔茨海默氏病。 本发明还提供了包含任何这些化合物的药物组合物以及这些化合物和组合物中的任何一种在治疗涉及BACE的疾病，病症或病症中的用途。
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公开(公告)号：EP2150109B1
公开(公告)日：2012-09-19
申请号：EP08745501.0
申请日：2008-04-10
IPC分类号： A01N37/12 , A01N37/44 , A61K31/195
CPC分类号： C07C235/40 , C07C235/20 , C07C235/22 , C07C311/46 , C07C317/22 , C07C317/30 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07C2602/44 , C07C2603/74 , C07D207/09 , C07D209/52 , C07D211/34 , C07D295/104 , C07D471/04 , C07D487/04
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公开(公告)号：EP2362730A4
公开(公告)日：2012-08-29
申请号：EP09828106
申请日：2009-11-17
IPC分类号： A01N43/42 , A61K31/44 , A61K31/50 , A61P27/06 , C07D213/64 , C07D213/70 , C07D213/71 , C07D213/72 , C07D237/14
CPC分类号： A61K31/44 , C07D213/643 , C07D213/70 , C07D213/71 , C07D213/74 , C07D237/14 , C07D239/42
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4.发明授权
公开(公告)号：EP1979311B1
公开(公告)日：2012-06-13
申请号：EP06830789.1
申请日：2006-12-21
发明人： SAUERBERG, Per , PIHERA, Pavel , POLIVKA,Zdenék , HAVRANEK, Miroslav , PETTERSSON, Ingrid , MOGENSEN, John, Patrick
IPC分类号： C07C323/16 , A61K31/44 , A61P3/10 , C07D213/30 , C07D211/46 , C07D333/54 , C07D333/16 , C07D231/12 , C07D307/79 , C07C59/68 , C07D295/08
CPC分类号： A61K31/5377 , A61K31/192 , A61K31/195 , A61K31/343 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4402 , A61K31/445 , A61K31/495 , A61K31/5375 , C07C59/70 , C07C217/48 , C07C323/16 , C07C323/32 , C07C2601/02 , C07D211/46 , C07D213/30 , C07D213/36 , C07D231/12 , C07D265/30 , C07D295/096 , C07D295/112 , C07D307/79 , C07D307/81 , C07D333/16 , C07D333/20 , C07D333/54
摘要： Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR´ and should be useful for treating conditions mediated by the same.
摘要翻译： 新的通式（I）化合物，这些化合物作为药物组合物的用途，包含该化合物的药物组合物和使用这些化合物和组合物的治疗方法。 本发明化合物是PPAR'的活化剂，应用于治疗由其介导的病症。
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公开(公告)号：EP2402324A1
公开(公告)日：2012-01-04
申请号：EP11182795.2
申请日：2007-05-22
发明人： Hohlweg, Rolf
IPC分类号： C07D237/20 , C07D405/04
CPC分类号： C07D405/04
摘要： A process for synthesizing 3-(1,3-benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine, where the process comprises reacting 3-chloro-6-(4-cyclopropyl-piperazin-1-yl)pyridazine with 3,4-methylene-dioxybenzene boronic acid.
摘要翻译： 合成3-（1,3-苯并间二氧杂环戊烯-5-基）-6-（4-环丙基哌嗪-1-基）哒嗪的方法，其中该方法包括使3-氯-6-（4-环丙基 - 哌嗪-1 - 基）哒嗪与3,4-亚甲基 - 二氧苯硼酸反应。
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公开(公告)号：EP2362730A1
公开(公告)日：2011-09-07
申请号：EP09828106.6
申请日：2009-11-17
CPC分类号： A61K31/44 , C07D213/643 , C07D213/70 , C07D213/71 , C07D213/74 , C07D237/14 , C07D239/42
摘要： Embodiments of the present invention provide adamantyl benzamide derivtives and pharmaceutical compositions comprising adamantyl benzamide derivatives. Methods of use of such compounds and compositions to modulate the activity of 11&bgr;-hydroxysteroid dehydrogenase type 1 (11&bgr;HSD1) in a subject are also provided.
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公开(公告)号：EP2239012A3
公开(公告)日：2011-06-15
申请号：EP10164336.9
申请日：2004-04-06
发明人： Andersen, Henrik Sune , Kampen, Gita Camilla Tejlgaard , Christensen, Inge Thoger , Mogensen, John Patrick , Larsen, Annette Rosendal , Kilburn, John Paul
IPC分类号： A61P3/04 , A61K31/16 , A61K31/415
CPC分类号： C07D209/02 , A61K31/16 , A61K31/415 , A61K45/06 , C07D401/06 , C07D401/12 , C07D403/12 , C07D487/08
摘要： The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
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公开(公告)号：EP1745002B1
公开(公告)日：2010-11-03
申请号：EP05747382.9
申请日：2005-05-03
IPC分类号： C07C59/70 , C07C323/20 , C07D213/30 , C07D295/08 , C07D333/16 , C07D409/06 , A61K31/192 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/50
CPC分类号： C07C323/20 , C07D213/30 , C07D295/092 , C07D333/16
摘要： Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPARδ subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hypertriglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.
摘要翻译： 其中变量如权利要求1中所定义的通式（I）的新化合物，这些化合物作为药物组合物的用途，包含所述化合物的药物组合物和使用这些化合物和组合物的治疗方法。 本发明化合物可用于治疗和/或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，特别是PPARδ亚型，即1型糖尿病，2型糖尿病，血脂障碍，X综合征（包括代谢综合征 即葡萄糖耐量降低，胰岛素抵抗，高甘油三酯血症和/或肥胖），心血管疾病（包括动脉粥样硬化）和高胆固醇血症。
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公开(公告)号：EP2152081A4
公开(公告)日：2010-10-06
申请号：EP08745333
申请日：2008-04-09
CPC分类号： A01N43/40 , A01N37/40 , C07C235/54 , C07C2603/74 , C07D213/643
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公开(公告)号：EP2233470A1
公开(公告)日：2010-09-29
申请号：EP10166493.6
申请日：2006-06-30
IPC分类号： C07D213/74 , C07D401/04 , C07D401/08 , C07D403/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D413/10 , C07D213/84 , C07D213/87 , C07D413/04 , C07D413/14 , C07D241/20 , A61P3/00 , A61K31/444
CPC分类号： C07D213/74 , C07D213/84 , C07D213/87 , C07D237/20 , C07D403/04 , C07D403/12 , C07D417/10
摘要： Novel compounds of formula I-9:
which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.摘要翻译： 定义了与组胺H3受体相互作用的式I-9的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在环的其余位置上有碳原子或氮原子。
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