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公开(公告)号：US11053227B2
公开(公告)日：2021-07-06
申请号：US16954704
申请日：2018-12-19
申请人： OLON S.P.A.
发明人： Corrado Colli , Giorgio Bertolini , Mara Sada , Faris Garis , Filippo Nisic , Aldo Bianchi , Cinzia Biaggi , Romano Di Fabio , Silvano Ronzoni , Stefania Bertuolo , Adolfo Prandi , Stefano Maiorana
IPC分类号： C07D405/06 , C07D207/408 , C12P13/02
摘要： Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof.
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公开(公告)号：US10669496B2
公开(公告)日：2020-06-02
申请号：US16223485
申请日：2018-12-18
发明人： James H. Bush , Robert H. Barbour , David J. Moreton , Hannah Greenfield , Paul R. Stevenson , David C. Arters
IPC分类号： C10L10/04 , C10L10/06 , C08G63/91 , C10L1/22 , C07D207/408 , C10L1/08 , C07D303/04 , C10L10/18 , C07C235/10 , C10L1/2387 , C10L1/2383 , C10L1/238 , C10L1/224 , C10L1/222 , C10L10/02 , C10L1/232
摘要： The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors.
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公开(公告)号：US20190270712A1
公开(公告)日：2019-09-05
申请号：US16319957
申请日：2017-07-28
发明人： Karen Annette DUGGAN
IPC分类号： C07D239/26 , C07D237/08 , C07D213/56 , C07D277/30 , C07C233/11 , C07D263/44 , C07C215/54 , C07D207/408 , C07D261/14 , C07D401/10 , C07D403/10 , C07C39/15 , A61P11/00
摘要： The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.
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公开(公告)号：US10398679B2
公开(公告)日：2019-09-03
申请号：US15934246
申请日：2018-03-23
申请人： ITEOS THERAPEUTICS
IPC分类号： A61K31/404 , A61K31/4015 , C07D207/408 , C07D207/40 , C07D403/04 , C07D207/46
摘要： Uses of compound of Formula I: or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof are described. The compounds of Formula I are useful as IDO1 inhibitors. These are also useful for the treatment and/or prevention of cancer and endometriosis.
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25.发明授权公开(公告)号：US09949951B2
公开(公告)日：2018-04-24
申请号：US15331446
申请日：2016-10-21
申请人： ITEOS THERAPEUTICS
IPC分类号： A61K31/404 , A61K31/4015 , C07D207/408 , C07D207/40 , C07D403/04 , C07D207/46
CPC分类号： A61K31/404 , A61K31/4015 , C07D207/40 , C07D207/408 , C07D207/46 , C07D403/04
摘要： Uses of compound of Formula I: or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof are described. The compounds of Formula I are useful as IDO1 inhibitors. These are also useful for the treatment and/or prevention of cancer and endometriosis.
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公开(公告)号：US09630934B2
公开(公告)日：2017-04-25
申请号：US14616727
申请日：2015-02-08
申请人： Mark Quang Nguyen
发明人： Mark Quang Nguyen
IPC分类号： C07D207/408 , C07D263/24 , C07D233/78
CPC分类号： C07D263/24 , C07D207/16 , C07D207/408 , C07D207/416 , C07D233/78 , C07D241/08
摘要： Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.
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公开(公告)号：US20160318875A1
公开(公告)日：2016-11-03
申请号：US15105127
申请日：2014-12-09
IPC分类号： C07D233/86 , C07D207/408 , C07D249/18 , C07C333/08 , C07C231/12
CPC分类号： C07D233/86 , C07C231/12 , C07C333/08 , C07D207/408 , C07D249/18
摘要： The present invention provides processes for the preparation of enzalutamide.
摘要翻译： 本发明提供了制备恩扎拉平的方法。
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28.发明授权Aqueous coating compositions including the reaction product of maleic anhydride with an unsaturated compound and an amine 有权水性涂料组合物，包括马来酸酐与不饱和化合物和胺的反应产物公开(公告)号：US09469785B2
公开(公告)日：2016-10-18
申请号：US14428523
申请日：2013-09-19
IPC分类号： C09D191/00 , C09D5/00 , C09D7/00 , C09D7/02 , C09F7/00 , C07D207/40 , C07D207/408 , B65D23/02 , C23F11/00 , C09D125/08 , C09D133/00 , C09D163/00 , C09D173/02 , C09D175/04
CPC分类号： C09D191/005 , B65D23/02 , C07D207/40 , C07D207/408 , C09D5/00 , C09D7/00 , C09D7/45 , C09D125/08 , C09D133/00 , C09D163/00 , C09D173/02 , C09D175/04 , C09F7/00 , C23F11/00
摘要： The invention includes an aqueous coating composition having a substituted succinimide compound, wherein the substituted succinimide compound has an acid value of at least about 30 mg KOH/g of the substituted succinimide compound. The substituted succinimide compound may be the reaction product of an unsaturated oil comprising at least one non-aromatic unsaturated carbon-carbon bond, a polymer derived from the unsaturated oil, or a combination thereof with maleic anhydride and a primary amine.
摘要翻译： 本发明包括具有取代的琥珀酰亚胺化合物的水性涂料组合物，其中取代的琥珀酰亚胺化合物的酸值至少为约30mg KOH / g的取代的琥珀酰亚胺化合物。 取代的琥珀酰亚胺化合物可以是包含至少一种非芳族不饱和碳 - 碳键的不饱和油，源自不饱和油的聚合物或其与马来酸酐和伯胺的组合的反应产物。
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公开(公告)号：US09321726B2
公开(公告)日：2016-04-26
申请号：US14426881
申请日：2013-10-16
申请人： INTERQUIM, S.A.
IPC分类号： C07D213/75 , C07D233/60 , C07D249/08 , C07D207/408 , C07D209/48 , C07D295/104 , C07D233/90 , C07D249/10
CPC分类号： C07D213/75 , C07D207/408 , C07D209/48 , C07D233/60 , C07D233/90 , C07D249/08 , C07D249/10 , C07D295/104
摘要： The invention relates to a process for the preparation of Roflumilast by reaction of an activated form of 3-(cyclopropylmethoxy)-4-(difluoromethoxy)-benzoic acid with an activating agent selected from (a) carbonyldiimidazole (CDI), (b) 1,1′-carbonyl-di-(1,2,4-triazol) (CDT), (c) 1,1′-carbonyl-bis-(2-methylimidazol), (d), 1′-carbonyl-dipyperidin, (e) N,N′-dicyclohexylcarbodiimide (DCC), (f) N,N′-diisopropylcarbodiimide (DIC), (g) 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) and a combination of one of the previous (a)-(g) with (h) N-hydroxysuccinimide or (i) N-hydroxyphthalimide, and the subsequent reaction with 3,5-dichloropyridine-4-amine in the presence of an inorganic base. The invention also relates to the synthesis intermediates.
摘要翻译： 本发明涉及一种通过活化形式的3-（环丙基甲氧基）-4-（二氟甲氧基） - 苯甲酸与选自（a）羰基二咪唑（CDI），（b）1 ，1'-羰基 - 二 - （1,2,4-三唑）（CDT），（c）1,1'-羰基 - 双 - （2-甲基咪唑），（d），1'-羰基 - （e）N，N'-二环己基碳二亚胺（DCC），（f）N，N'-二异丙基碳二亚胺（DIC），（g）1-乙基-3-（3-二甲基氨基丙基）碳二亚胺（EDC） 前述（a） - （g）与（h）N-羟基琥珀酰亚胺或（i）N-羟基邻苯二甲酰亚胺，随后在无机碱存在下与3,5-二氯吡啶-4-胺反应。 本发明还涉及合成中间体。
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30.发明授权公开(公告)号：US09296690B2
公开(公告)日：2016-03-29
申请号：US14293879
申请日：2014-06-02
申请人： Metacine, Inc.
发明人： Bae Keun Park , Sung-Hwa Yoon , Ju-Young Park , Sung Hoon Park
IPC分类号： A61K31/4015 , C07D207/448 , C07D207/452 , C07D207/38 , C07D207/444 , C07D409/04 , C07D207/20 , C07D207/408 , C07D207/456
CPC分类号： C07D207/448 , A61K31/4015 , C07D207/20 , C07D207/38 , C07D207/408 , C07D207/444 , C07D207/452 , C07D207/456 , C07D409/04
摘要： The present invention is for method of treating metabolic bone disease, new compounds and pharmaceutical compositions comprising the active ingredients having inhibition effects on osteoclast differentiation. The pharmaceutical composition comprising new compounds according to the present invention can be used as medicines for treating metabolic bone diseases such as bone metastatic cancer, solid cancer bone metastasis, musculoskeletal complication by solid cancer bone metastasis, hypercalcemia by malignant tumor, multiple myeloma, primary bone tumor, osteoporosis, rheumatoid arthritis, osteoarthritis, periodontal disease, inflammatory resorption of alveolar bone, inflammatory resorption of bone, and Paget's disease.
摘要翻译： 本发明是治疗代谢性骨病的方法，新化合物和药物组合物，其含有对破骨细胞分化具有抑制作用的活性成分。 包含根据本发明的新化合物的药物组合物可用作治疗代谢性骨疾病如骨转移癌，固体癌骨转移，通过固体癌骨转移的肌肉骨骼并发症，恶性肿瘤的高钙血症，多发性骨髓瘤，原发骨 肿瘤，骨质疏松症，类风湿关节炎，骨关节炎，牙周病，牙槽骨炎症吸收，骨吸收性炎症和佩吉特氏病。
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