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公开(公告)号：US11795187B2
公开(公告)日：2023-10-24
申请号：US17579886
申请日：2022-01-20
IPC分类号： C07F13/00 , C07C59/265 , A61K31/194 , C07F1/00 , C07F3/06 , C07F3/02 , C07F3/04 , A61P3/00 , A61P19/02 , A61P29/00 , A61P19/10
CPC分类号： C07F13/005 , A61K31/194 , C07C59/265 , C07F1/005 , C07F3/02 , C07F3/04 , C07F3/06 , A61P3/00 , A61P19/02 , A61P19/10 , A61P29/00
摘要： Hydroxycitric acid-metal heterocyclic compounds with covalent characteristics are provided. The subject hydroxycitric acid compounds include monomeric hydroxycitric acid (HCA) compounds having a divalent metal, lactone forms thereof, and dimeric compound forms thereof. The monomeric HCA compound includes a divalent metal (X) bonded via a 5-membered ring to both the carboxylic acid and the hydroxy group of the central C2 carbon of the HCA. In addition, a monovalent metal (Y) can also be bonded to the carboxylic acid of C3 or C1, or to both C1 and C3. The subject dimeric compounds include monomeric HCA compounds linked via a second divalent metal (X) to a carboxylic acid group of each HCA unit at C3 or C1. Also provided are compositions including a monomeric HCA compound and one or more other additional compounds. Methods of alleviating at least one symptom associated with a target disease or condition in a subject are provided.
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公开(公告)号：US20190153024A1
公开(公告)日：2019-05-23
申请号：US16203273
申请日：2018-11-28
申请人： SCYNEXIS, INC.
发明人： Yi ZHANG
IPC分类号： C07J71/00 , C07C59/265 , C07D405/14
CPC分类号： C07J71/0005 , C07C59/265 , C07D405/14
摘要： SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078.
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公开(公告)号：US10039761B2
公开(公告)日：2018-08-07
申请号：US15130266
申请日：2016-04-15
发明人： Kwame Wiredu Nti-Addae , Simon Adam O'Neil , Yuegang Zhang , Michael Waldo , Praveen Mudunuri , Bin Song , John Gregg Van Alsten , Mark Strohmeier , Kathy Stavropoulos , Irina Nikolaevna Kadiyala , Mettachit Navamal
IPC分类号： A61K31/33 , A61K31/506 , C07D401/14 , A61K31/337 , A61K31/5025 , A61K31/513 , A61K31/517 , A61K31/555 , A61K31/704 , A61K31/7048 , A61K33/24 , A61K38/14 , A61K39/395 , A61K45/06 , C07B59/00 , C07C55/10 , C07C55/14 , C07C57/145 , C07C57/15 , C07C59/265 , C07C63/08 , C07K16/28 , A61N5/10
CPC分类号： A61K31/506 , A61K31/337 , A61K31/5025 , A61K31/513 , A61K31/517 , A61K31/555 , A61K31/704 , A61K31/7048 , A61K33/24 , A61K38/14 , A61K39/39558 , A61K45/06 , A61N2005/1098 , A61P35/00 , C07B59/002 , C07B2200/05 , C07B2200/13 , C07C55/10 , C07C55/14 , C07C57/145 , C07C57/15 , C07C59/265 , C07C63/08 , C07D401/14 , C07K16/2863 , C07K2317/24
摘要： The present invention relates to compositions and co-crystals each comprising a compound of formula I having the structure: wherein each of R1 and R2 is H or 2H and a co-crystal former selected from adipic acid, citric acid, fumaric acid, maleic acid, succinic acid, or benzoic acid. Also within the scope of this invention are methods of making and using the same.
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公开(公告)号：US20170275264A1
公开(公告)日：2017-09-28
申请号：US15452430
申请日：2017-03-07
申请人： Yves AUBERSON , Mark Gary BOCK , Dario BRAGA , Marco CURZI , Stephanie Kay DODD , Stefano Luca GIAFFREDA , Haiyang JIANG , Piotr KARPINSKI , Thomas J. TROXLER , Tie-Lin WANG , Xiaoyang WANG , Xuechun ZHANG
发明人： Yves AUBERSON , Mark Gary BOCK , Dario BRAGA , Marco CURZI , Stephanie Kay DODD , Stefano Luca GIAFFREDA , Haiyang JIANG , Piotr KARPINSKI , Thomas J. TROXLER , Tie-Lin WANG , Xiaoyang WANG , Xuechun ZHANG
IPC分类号： C07D401/04 , C07D403/04 , C07C57/15 , C07C59/265 , A61K31/496 , A61K31/501
CPC分类号： C07D401/04 , A61K31/496 , A61K31/501 , C07B2200/13 , C07C57/15 , C07C59/265 , C07D403/04
摘要： The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
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公开(公告)号：US20170260167A1
公开(公告)日：2017-09-14
申请号：US15354832
申请日：2016-11-17
发明人： Srinivasa Rao Akireddy , Balwinder Singh Bhatti , Timothy J. Cuthbertson , Gary Maurice Dull , Craig Harrison Miller , Joseph Pike Mitchener, JR. , Julio A. Munoz , Pieter Albert Otten
IPC分类号： C07D403/06 , C07C59/255 , C07C59/265 , A61K31/4025
CPC分类号： C07D403/06 , A61K31/4025 , C07C59/255 , C07C59/265
摘要： The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
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公开(公告)号：US09757416B2
公开(公告)日：2017-09-12
申请号：US14701933
申请日：2015-05-01
IPC分类号： A61K33/26 , A61K31/295 , C07C51/41 , C07C59/265
CPC分类号： A61K33/26 , A61K31/295 , C07C51/412 , C07C51/418 , C07C59/265 , C07C55/10 , C07C59/255 , C07C53/08 , C07C59/245 , C07C57/15
摘要： The present invention discloses pharmaceutical-grade ferric organic compounds, including ferric citrate, which are soluble over a wider range of pH, and which have a large active surface area. A manufacturing and quality control process for making a pharmaceutical-grade ferric citrate that consistently complies with the established Manufacture Release Specification is also disclosed. The pharmaceutical-grade ferric organic compounds are suitable for treating disorders characterized by elevated serum phosphate levels.
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公开(公告)号：US20170114034A1
公开(公告)日：2017-04-27
申请号：US15115063
申请日：2015-01-30
发明人： Istvan LING , Gyorgy JEGES , Gyorgyi KOVANYINE LAX , Balazs VOLK , Peter GREGOR , Jeno Peter SERES , Andras DANCSO , Zoltan VARGA , Eva SZABO
IPC分类号： C07D295/096 , C07C59/265 , C07C55/10 , C07C55/08 , C07C309/29 , C07C53/10 , C07C55/07 , C07C65/10
CPC分类号： C07D295/096 , C07B2200/13 , C07C53/10 , C07C55/07 , C07C55/08 , C07C55/10 , C07C59/265 , C07C65/10 , C07C309/29 , C07D295/08
摘要： The invention relates to an improved process for the preparation of pharmaceutical active ingredients and also to high purity salts and pharmaceutical compositions prepared by said process. More particularly the invention relates to an economical process for the preparation of the compound having the international non-proprietary name (INN) vortioxetine and the chemical nomenclature 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]-piperazine. Vortioxetine corresponds to the following Formula Still more particularly the invention relates to the preparation of high purity vortioxetine L-(+)-mandelate salt of the Formula IX, the conversion of this salt into other highly pure salts and also to the formulation of said salts.
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公开(公告)号：US09624192B2
公开(公告)日：2017-04-18
申请号：US15049739
申请日：2016-02-22
申请人： Yves Auberson , Mark Gary Bock , Dario Braga , Marco Curzi , Stephanie Kay Dodd , Stefano Luca Giaffreda , Haiyang Jiang , Piotr Karpinski , Thomas J. Troxler , Tie-Lin Wang , Xiaoyang Wang , Xuechun Zhang
发明人： Yves Auberson , Mark Gary Bock , Dario Braga , Marco Curzi , Stephanie Kay Dodd , Stefano Luca Giaffreda , Haiyang Jiang , Piotr Karpinski , Thomas J. Troxler , Tie-Lin Wang , Xiaoyang Wang , Xuechun Zhang
IPC分类号： A61K31/501 , C07D401/04 , A61K31/496 , C07C57/15 , C07C59/265 , C07D403/04
CPC分类号： C07D401/04 , A61K31/496 , A61K31/501 , C07B2200/13 , C07C57/15 , C07C59/265 , C07D403/04
摘要： The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
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公开(公告)号：US20170101365A1
公开(公告)日：2017-04-13
申请号：US15314082
申请日：2015-05-26
IPC分类号： C07C247/04 , C07D498/04 , C07C59/265 , C07C209/82
CPC分类号： C07C247/04 , C07C59/265 , C07C209/82 , C07D498/04
摘要： The present invention relates to azidoalkylamine salts of formula (I) with organic acids, a process for their preparation, and their use as intermediates in the preparation of active pharmaceutical ingredients or polymers, or as spacers useful in organis synthesis. NH2—(CH2)n-N3 (I)
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公开(公告)号：US09573951B2
公开(公告)日：2017-02-21
申请号：US14524686
申请日：2014-10-27
申请人： Cyclacel Limited
发明人： Benjamin Mark Skead , Christopher Peter Worrall , Jonathan Charles Christian Atherton , Julian Scott Northen , Philippe Fernandes
IPC分类号： C07D473/00 , C07D473/16 , G01F1/115 , G01P3/48 , G01P5/07 , A61K31/52 , C07C51/41 , C07C57/145 , C07C57/15 , C07C59/245 , C07C59/255 , C07C59/265 , C07C65/05 , C07C303/32 , C07C309/04 , C07C309/29
CPC分类号： C07D473/16 , A61K31/52 , C07B2200/13 , C07C51/412 , C07C57/145 , C07C57/15 , C07C59/245 , C07C59/255 , C07C59/265 , C07C65/05 , C07C303/32 , C07C309/04 , C07C309/29 , G01F1/115 , G01P3/4802 , G01P5/07
摘要： The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumor activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.
摘要翻译： 本发明涉及嘌呤衍生物的新结晶形式，其具有优异的抗肿瘤活性。 本发明还涉及含有所述结晶形式作为活性成分的药物组合物及其在预防或治疗疾病中的用途。 本发明还涉及制备结晶形式的方法。
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