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1. 发明申请

US20220306578A1 TETRACYCLIC COMPOUND 有权
公开(公告)号：US20220306578A1
公开(公告)日：2022-09-29
申请号：US16862125
申请日：2020-04-29
申请人： Chugai Seiyaku Kabushiki Kaisha
发明人： Kazutomo KINOSHITA , Kohsuke ASOH , Noriyuki FURUICHI , Toshiya ITO , Hatsuo KAWADA , Nobuya ISHII , Hiroshi SAKAMOTO , WooSang HONG , MinJeong PARK , Yoshiyuki ONO , Yasuharu KATO , Kenji MORIKAMI , Takashi EMURA , Nobuhiro OIKAWA
IPC分类号： C07D209/58 , C07D209/88 , C07D307/77 , C07D307/92 , C07D333/50 , C07D333/76 , C07D401/04 , C07D401/06 , C07D403/04 , C07D405/12 , C07D405/14 , C07D471/04 , C07D491/107 , C07D209/56 , A61K31/404 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/7056 , C07D307/78 , C07D333/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D413/14 , C07D471/10 , C07F7/08 , C07H15/26
摘要： A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).

2. 发明授权

US09537105B2 Materials for organic electroluminescent devices 有权
标题翻译：有机电致发光器件材料
公开(公告)号：US09537105B2
公开(公告)日：2017-01-03
申请号：US14800828
申请日：2015-07-16
申请人： Merck Patent GmbH
发明人： Christof Pflumm , Arne Buesing , Amir Hossain Parham , Teresa Mujica-Fernaud , Holger Heil , Philipp Stoessel
IPC分类号： H01L51/54 , C09K11/06 , H01L51/00 , C07D209/70 , C07D401/14 , C07D493/04 , C09K11/02 , H01L51/50 , C07D209/82 , C07D307/78 , C07D333/52 , C07D403/04 , C07D403/10 , C07D403/14 , C07D407/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/10 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07F9/6568 , C07F9/6584 , C07F15/00 , C09B15/00 , C09B17/00 , C09B19/00 , C09B57/00 , H05B33/10
CPC分类号： H01L51/006 , C07D209/70 , C07D209/82 , C07D307/78 , C07D333/52 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D407/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/10 , C07D471/04 , C07D487/04 , C07D493/04 , C07D498/04 , C07D513/04 , C07F9/65683 , C07F9/65685 , C07F9/65848 , C07F15/0033 , C07F15/0086 , C09B15/00 , C09B17/00 , C09B19/00 , C09B57/00 , C09K11/025 , C09K11/06 , C09K2211/1007 , C09K2211/1011 , C09K2211/1014 , C09K2211/1029 , C09K2211/1033 , C09K2211/1037 , C09K2211/1044 , C09K2211/1059 , C09K2211/1088 , C09K2211/1092 , H01L51/001 , H01L51/0061 , H01L51/0067 , H01L51/0071 , H01L51/0072 , H01L51/5012 , H01L51/5016 , H01L51/5048 , H01L51/5056 , H01L51/5072 , H01L51/5096 , H01L2251/308 , H01L2251/5384 , H05B33/10 , Y02E10/549
摘要： The present invention describes indenocarbazole derivatives having electron- and hole-transporting properties, in particular for use in the emission and/or charge-transport layer of electroluminescent devices or as matrix material. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising same.
摘要翻译：本发明描述了具有电子和空穴传输性质的茚基咔唑衍生物，特别是用于电致发光器件的发射和/或电荷传输层或作为基质材料。本发明还涉及制备根据本发明的化合物的方法和包含其的电子器件。

3. 发明授权

US09499507B2 Method for preparing 5-amino-benzoyl-benzofuran derivatives 有权
标题翻译：制备5-氨基苯甲酰基 - 苯并呋喃衍生物的方法
公开(公告)号：US09499507B2
公开(公告)日：2016-11-22
申请号：US14361562
申请日：2012-11-28
申请人： Sanofi
发明人： Xavier Bon , Jean-Louis Delepine , Laure Jourdin , Denis Largeau , Philippe Vayron
IPC分类号： C07D307/78 , C07D307/80 , C07D307/82
CPC分类号： C07D307/80 , C07D307/82
摘要： The invention relates to a method for preparing 5-amino-benzoyl-benzofuran derivatives having the general formula in which R1 is hydrogen or an alkyl or aryl group and R2 is hydrogen, an alkyl, alkoxy or dialkylaminoalkoxy group. According to the invention, the compounds having formula I are prepared by hydrogenating a 5-nitro-benzofuran derivative having the general formula in which R1 and R2 have the same meaning as above in the presence of palladized charcoal as a catalyst and in an ether or a mixture of ether as a solvent, thus forming the desired compounds.
摘要翻译：本发明涉及一种制备具有以下通式的5-氨基苯甲酰基 - 苯并呋喃衍生物的方法，其中R1是氢或烷基或芳基，R2是氢，烷基，烷氧基或二烷基氨基烷氧基。根据本发明，具有式I的化合物通过氢化具有以下通式的5-硝基 - 苯并呋喃衍生物来制备：其中R 1和R 2具有与上述相同的含义，在作为催化剂的钯化物存在下，在醚或乙醚作为溶剂的混合物，从而形成所需的化合物。

4. 发明授权

US09309267B2 Compounds suitable as precursors to compounds that are useful for imaging amyloid deposits 有权
标题翻译：适合用作成像淀粉样蛋白沉积物的化合物的前体的化合物
公开(公告)号：US09309267B2
公开(公告)日：2016-04-12
申请号：US14149563
申请日：2014-01-07
申请人： AstraZeneca AB
发明人： Seth Björk , Peter Johnström , Nils A. Nilsson , Katinka Ruda , Per M. Schou , Britt-Marie Swahn , Vern Delisser
IPC分类号： C07D407/04 , C07F5/02 , A61K51/04 , C07D307/78 , C07D405/04 , C07D213/76
CPC分类号： C07F5/025 , A61K51/0455 , C07D213/76 , C07D307/78 , C07D405/04
摘要： The present invention relates to novel derivatives that are suitable as precursors to compounds that are useful for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. The compounds deriving from these precursors are useful in methods of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease by positron emission tomography (PET) as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents. Furthermore, the present invention also discloses the precursor compounds in crystalline form.
摘要翻译：本发明涉及适用于化合物前体的新衍生物，其可用于成像活体患者的淀粉样蛋白沉积物，其组合物，使用方法和制备此类化合物的方法。衍生自这些前体的化合物可用于体内脑中淀粉样蛋白沉积物成像的方法，以通过正电子发射断层扫描（PET）进行阿尔茨海默氏病的止血诊断以及测量阿尔茨海默病治疗剂的临床疗效。此外，本发明还公开了晶体形式的前体化合物。

5. 发明授权

US09126970B2 Materials for organic electroluminescent devices 有权
标题翻译：有机电致发光器件材料
公开(公告)号：US09126970B2
公开(公告)日：2015-09-08
申请号：US13322614
申请日：2010-05-03
申请人： Christof Pflumm , Arne Buesing , Amir Hossain Parham , Teresa Mujica-Fernaud , Holger Heil , Philipp Stoessel
发明人： Christof Pflumm , Arne Buesing , Amir Hossain Parham , Teresa Mujica-Fernaud , Holger Heil , Philipp Stoessel
IPC分类号： H01L51/54 , C07D209/56 , C07D403/04 , C07D401/14 , C07D403/14 , C09K11/06 , C07D491/048 , C07D487/04 , C07D401/04 , C07D209/82 , C07D307/78 , C07D333/52 , C07D403/10 , C07D407/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/10 , C07D471/04 , C07D498/04 , C07D513/04 , C07F9/6568 , C07F9/6584 , C07F15/00 , C09B15/00 , C09B17/00 , C09B19/00 , C09B57/00 , H05B33/10 , H01L51/00 , H01L51/50
CPC分类号： H01L51/006 , C07D209/70 , C07D209/82 , C07D307/78 , C07D333/52 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D407/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/10 , C07D471/04 , C07D487/04 , C07D493/04 , C07D498/04 , C07D513/04 , C07F9/65683 , C07F9/65685 , C07F9/65848 , C07F15/0033 , C07F15/0086 , C09B15/00 , C09B17/00 , C09B19/00 , C09B57/00 , C09K11/025 , C09K11/06 , C09K2211/1007 , C09K2211/1011 , C09K2211/1014 , C09K2211/1029 , C09K2211/1033 , C09K2211/1037 , C09K2211/1044 , C09K2211/1059 , C09K2211/1088 , C09K2211/1092 , H01L51/001 , H01L51/0061 , H01L51/0067 , H01L51/0071 , H01L51/0072 , H01L51/5012 , H01L51/5016 , H01L51/5048 , H01L51/5056 , H01L51/5072 , H01L51/5096 , H01L2251/308 , H01L2251/5384 , H05B33/10 , Y02E10/549
摘要： The present invention describes indenocarbazole derivatives having electron- and hole-transporting properties, in particular for use in the emission and/or charge-transport layer of electroluminescent devices or as matrix material. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising same.
摘要翻译：本发明描述了具有电子和空穴传输性质的茚基咔唑衍生物，特别是用于电致发光器件的发射和/或电荷传输层或作为基质材料。本发明还涉及制备根据本发明的化合物的方法和包含其的电子器件。

6. 发明授权

US08481763B2 Preparation process of dronedarone and its salts 有权
标题翻译：决奈达隆及其盐的制备方法
公开(公告)号：US08481763B2
公开(公告)日：2013-07-09
申请号：US13701642
申请日：2011-06-03
申请人： Xianshan Hou , Yongjiang Chen
发明人： Xianshan Hou , Yongjiang Chen
IPC分类号： C07D307/78
CPC分类号： C07D307/80 , A61K31/343 , C07D307/82
摘要： A process is provided for preparing dronedarone or pharmaceutically acceptable salts thereof. The process comprises reacting 5-amino-2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)benzofuran (compound A) with methanesulfonyl chloride without any catalyst to provide crude dronedarone hydrochloride, which is purified to afford highly pure product. Then, the dronedarone hydrochloride can be converted to highly pure dronedarone through treatment with an alkaline solvent, the dronedarone can be further converted to other pharmaceutically acceptable salts of dronedarone. In this process, acylation between compound A and methanesulfonyl chloride is carried out successfully and the formation of the dimethylsulfonyl by-product is inhibited.
摘要翻译：提供了制备决奈达隆或其药学上可接受的盐的方法。该方法包括不用任何催化剂使5-氨基-2-丁基-3-（4- [3-（二丁基氨基）丙氧基]苯甲酰基）苯并呋喃（化合物A）与甲磺酰氯反应，得到粗制决奈罗酮盐酸盐，将其纯化得到高纯产品。然后，盐酸决奈达隆可以通过用碱性溶剂处理而转化为高纯度的决奈达隆，决奈达隆可以进一步转化成其他药学上可接受的决奈达隆盐。在该方法中，化合物A与甲磺酰氯之间的酰化成功进行，二甲基磺酰副产物的形成被抑制。

7. 发明授权

US08389571B2 Benzofuran derived HIV protease inhibitors 失效
标题翻译：苯并呋喃衍生的HIV蛋白酶抑制剂
公开(公告)号：US08389571B2
公开(公告)日：2013-03-05
申请号：US13186297
申请日：2011-07-19
申请人： Michael Eissenstat
发明人： Michael Eissenstat
IPC分类号： A61K31/343 , C07D307/78 , C07D407/12
CPC分类号： C07D493/04
摘要： Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.
摘要翻译：提供抗驱虫和多药耐药的逆转录病毒蛋白酶抑制剂。还提供了包含这些化合物的药物组合物，以及使用这些化合物治疗哺乳动物HIV感染的方法。

8. 发明授权

US08309545B2 Benzofuran potassium channel blockers and uses thereof 有权
标题翻译：苯并呋喃钾通道阻滞剂及其用途
公开(公告)号：US08309545B2
公开(公告)日：2012-11-13
申请号：US12444211
申请日：2007-10-04
申请人： Bernard Luke Flynn , Jonathan B. Baell , Andrew J. Harvey , Jason Hugh Chaplin , Dharam Paul , Jorgen Alvar Mould
发明人： Bernard Luke Flynn , Jonathan B. Baell , Andrew J. Harvey , Jason Hugh Chaplin , Dharam Paul , Jorgen Alvar Mould
IPC分类号： A61K31/5377 , A61K31/343 , C07D413/12 , C07D307/78
CPC分类号： C07D307/79 , C07D405/12 , C07D413/12
摘要： The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
摘要翻译：本发明涉及可用于调节细胞中钾通道活性的化合物，特别是在T细胞中发现的Kv1.3通道的活性。本发明还涉及这些化合物在治疗或预防自身免疫性和炎性疾病，包括多发性硬化症中的用途，含有这些化合物的药物组合物及其制备方法。

9. 发明申请

US20120148494A1 ISOTOPICALLY-LABELED BENZOFURAN COMPOUNDS AS IMAGING AGENTS FOR AMYLOIDOGENIC PROTEINS 审中-公开
标题翻译：同位素标记的苯甲醚化合物作为淀粉样蛋白成像剂
公开(公告)号：US20120148494A1
公开(公告)日：2012-06-14
申请号：US13359040
申请日：2012-01-26
申请人： William E. KLUNK , Chester A. MATHIS, JR.
发明人： William E. KLUNK , Chester A. MATHIS, JR.
IPC分类号： A61K49/00 , G01N33/53 , C07D307/78
CPC分类号： C07D307/79
摘要： Benzofuran compounds which contain at least one detectable label selected from the group consisting of 131I, 123I, 124I, 76Br, 75Br, 18F, 19F, 11C, 13C, 14C and 3H are provided as amyloid imaging agents for detecting brain amyloid deposits as well as other amyloidogenic peptides associated with systemic or localized amyloidosis. Additionally, the compounds are useful for determining if patients, presenting with clinically confusing cases of dementia or presenting with mild cognitive impairment, have Alzheimer's disease. The compounds are additionally useful as surrogate markers for monitoring the efficacy of anti-amyloidosis therapies.
摘要翻译：提供含有选自131I，123I，124I，76Br，75Br，18F，19F，11C，13C，14C和3H中的至少一种可检测标记的苯并呋喃化合物作为用于检测脑淀粉样沉积物的淀粉样成像剂与全身或局部淀粉样变性相关的其他淀粉样变性肽。此外，这些化合物可用于确定呈现临床上混淆的痴呆病例或呈现轻度认知障碍的患者是否患有阿尔茨海默氏病。该化合物另外可用作用于监测抗淀粉样变性治疗功效的替代标志物。

10. 发明授权

US08008511B2 Process for modifying drug crystal formation 有权
标题翻译：改变药物晶体形成的方法
公开(公告)号：US08008511B2
公开(公告)日：2011-08-30
申请号：US12337663
申请日：2008-12-18
申请人： Sabine Pfeffer , Dierk Wieckhusen
发明人： Sabine Pfeffer , Dierk Wieckhusen
IPC分类号： C07D307/78
CPC分类号： C07D307/88 , A61K9/14 , A61K9/2866
摘要： A process for modifying the crystal habit of acicular drug substances, crystals obtained by such a process, and particular crystal forms or modifications of mycophenolic acid or mycophenolate sodium are provided, as well as pharmaceutical compositions comprising the crystals, methods of treatment and uses thereof.
摘要翻译：提供了一种改变针状药物晶体习性的方法，通过这种方法获得的晶体，以及特定的霉酚酸或霉酚酸钠的晶型或改性物，以及包含晶体，治疗方法及其用途的药物组合物。

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