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11. 发明申请

US20160222040A1 PROCESS FOR STABILIZING HYDROCYANATION CATALYST 审中-公开
标题翻译：稳定化学催化剂的方法
公开(公告)号：US20160222040A1
公开(公告)日：2016-08-04
申请号：US15015252
申请日：2016-02-04
申请人： INVISTA NORTH AMERICA S.A R.L.
发明人： William J. TENN, III
IPC分类号： C07F9/06 , C07C253/30 , B01J31/18
CPC分类号： C07F9/06 , B01J31/185 , B01J31/2221 , B01J2231/322 , B01J2231/70 , B01J2531/847 , C07C253/10 , C07C253/30 , C07F9/145 , C07F9/4006 , C07F9/65744 , C07F15/04
摘要： The invention provides a method of forming a phosphonate diester compound from a ligand hydrolysis product (LHP) of a phosphite ligand used in a nickel-phosphite hydrocyanation catalyst, such as for conversion of 3-pentenenitrile to adiponitrile, which serves to eliminate acidic LHP compound for a hydrocyanation reaction milieu where the acidic LHP can catalyze further catalyst ligand destruction. The invention further provides phosphonate disester compounds prepared by alkylation of diarylphosphite LHP in the presence of a nickel-phosphite catalyst comprising a bidentate ligand, and a continuous hydrocyanation process for production of adiponitrile wherein catalyst ligand breakdown is inhibited through inactivation of ligand hydrolysis products towards further breakdown. A method of stabilizing a hydrocyanation catalyst is provided.
摘要翻译：本发明提供了一种由亚磷酸氢氰化催化剂中使用的亚磷酸酯配位体的配体水解产物（LHP）形成膦酸二酯化合物的方法，例如用于将3-戊烯腈转化成己二腈，其用于消除酸性LHP化合物对于氢化反应环境，其中酸性LHP可以催化另外的催化剂配体破坏。本发明还提供了在含有二齿配位体的亚磷酸二氢镍催化剂的存在下烷基化亚磷酸二氢钠LHP制备的膦酸酯二酯化合物，以及用于生产己二腈的连续氢氰化方法，其中通过使配体水解产物失活而进一步抑制催化剂配体分解分解。提供了一种稳定氢氰化催化剂的方法。

12. 发明申请

US20160200748A1 FLUORINATED COMPOUNDS USABLE AS AN ORGANIC SOLVENT FOR LITHIUM SALTS 审中-公开
标题翻译：氟化合物可用作锂盐的有机溶剂
公开(公告)号：US20160200748A1
公开(公告)日：2016-07-14
申请号：US14912741
申请日：2014-08-22
申请人： COMMISSARIAT À L'ÉNERGIE ATOMIQUE ET AUX ÉNERGIES ALTERNATIVES , ECOLE NATIONALE SUPÉRIEURE DE CHIMIE DE MONTPELLIER , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
发明人： Hervé Galiano , Stéphane Cadra , Nathalie Pierre , Bruno Ameduri , Ali Alaaeddine
IPC分类号： C07F9/40 , H01M10/052 , H01M10/0569
CPC分类号： C07F9/4006 , H01M10/052 , H01M10/0569 , H01M2300/0034
摘要： The disclosure relates to compounds of following formula (I): where: X corresponds to a repeat unit of following formula (II): or to a sequence of said repeat units of formula (II), and R1 and R2 are each independently an alkyl group. The disclosure further relates to the use of these compounds as organic solvents of at least one lithium salt.
摘要翻译：本公开涉及下式（I）的化合物：其中：X对应于下式（II）的重复单元：或式（II）的所述重复单元的序列，并且R 1和R 2各自独立地为烷基组。本公开还涉及这些化合物作为至少一种锂盐的有机溶剂的用途。

13. 发明申请

US20160200664A1 Process for Preparing Cinacalcet and Pharmaceutically Acceptable Salts Thereof 审中-公开
标题翻译：制备西那卡塞和药学上可接受的盐的方法
公开(公告)号：US20160200664A1
公开(公告)日：2016-07-14
申请号：US15075268
申请日：2016-03-21
申请人： Produits Chimiques Auxiliaires et de Synthese
发明人： Jean-Marie Schneider , Jonathan Madec , Sergio Kreimerman , Gerard Guillamot
IPC分类号： C07C209/68 , C07C211/30 , C07C209/84
CPC分类号： C07C209/68 , C07B2200/13 , C07C209/52 , C07C209/84 , C07C211/30 , C07C249/02 , C07F9/40 , C07F9/4006 , C07F9/4015 , C07C251/16
摘要： The present patent application relates to a process for preparing cinacalcet or a pharmaceutically acceptable salt thereof, which comprises reacting 3-trifluoromethylbenzaldehyde having the following formula (II) with the phosphorus-comprising derivative having the following formula (III) in which R1 and R2, which may be identical or different, are each a (C1-C6)alkyl group. The present invention also relates to the phosphorus-comprising derivative having the formula (III), to the use thereof and to the process for preparing same. The present invention also relates to the phosphate salt of cinacalcet and to uses thereof.
摘要翻译：本发明涉及一种制备西那卡塞或其药学上可接受的盐的方法，其包括使具有下式（II）的3-三氟甲基苯甲醛与下式（III）的含磷衍生物反应，其中R 1和R 2，其可以相同或不同，各自为（C 1 -C 6）烷基。本发明还涉及具有式（III）的含磷衍生物，其用途及其制备方法。本发明还涉及西那卡塞的磷酸盐及其用途。

14. 发明授权

US09328131B2 Benzimidazolium compounds 有权
标题翻译：苯并咪唑化合物
公开(公告)号：US09328131B2
公开(公告)日：2016-05-03
申请号：US14330020
申请日：2014-07-14
申请人： Boehringer Ingelheim International GmbH
发明人： Joerg Kley , Sara Frattini , Dieter Hamprecht
IPC分类号： C07D403/02 , C07F9/6558 , A61K45/06 , C07D401/14 , A61K31/497 , C07D403/12 , C07D405/14 , C07F9/572 , C07F9/40
CPC分类号： C07F9/65583 , A61K31/497 , A61K45/06 , C07D401/14 , C07D403/12 , C07D405/14 , C07F9/4006 , C07F9/4021 , C07F9/5728
摘要： The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
摘要翻译：本发明涉及通式（I）的化合物及其互变异构体及其盐，特别是其与无机或有机酸和碱的药学上可接受的盐，其具有有价值的药理学性质，特别是对上皮钠通道的抑制作用，其用于治疗疾病，特别是肺和气道疾病。

15. 发明授权

US09303051B2 Phosphonate ester derivatives and methods of synthesis thereof 有权
公开(公告)号：US09303051B2
公开(公告)日：2016-04-05
申请号：US14808388
申请日：2015-07-24
申请人： Chimerix, Inc.
发明人： Roy W. Ware , Merrick R. Almond , Bernhard M. Lampert
IPC分类号： A61K31/675 , C07F9/40 , C07F9/38 , C07F9/6512 , C07F9/6571
CPC分类号： C07F9/4021 , A61K31/675 , C07F9/3808 , C07F9/4006 , C07F9/6512 , C07F9/657181 , Y02A50/467 , Y02P20/55
摘要： The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives.

16. 发明申请

US20150274915A1 ORGANOPHOSPHORUS COMPOUNDS FOR FLAME RETARDANT POLYURETHANE FOAMS 有权
标题翻译：用于阻燃聚氨酯泡沫塑料的有机磷化合物
公开(公告)号：US20150274915A1
公开(公告)日：2015-10-01
申请号：US14433728
申请日：2012-10-08
申请人： Ravi B. Shankar , Matthew Martin Yonkey , YuDong Qi , Nahrain E. Kamber
发明人： Ravi B. Shankar , Matthew Martin Yonkey , YuDong Qi , Nahrain E. Kamber
IPC分类号： C08J9/00 , C07F9/6574 , C09K21/12 , C08G18/76 , C08G18/48 , C07F9/40 , C08G18/08
CPC分类号： C08J9/0038 , C07F9/4006 , C07F9/4075 , C07F9/657181 , C07F9/65742 , C08G18/14 , C08G18/165 , C08G18/2063 , C08G18/244 , C08G18/288 , C08G18/3275 , C08G18/4816 , C08G18/4833 , C08G18/4841 , C08G18/485 , C08G18/6688 , C08G18/7621 , C08G2101/0083 , C08J2375/08 , C08K5/5333 , C08K5/5353 , C08K5/5357 , C09K21/12
摘要： An organophosphorus compound useful in a phosphorus containing flame retardant and a flame retardant polyurethane foam, where the organophosphorus compound is shown in Formula (I) where Y is selected from the group consisting of an —OH group, an —NH2 group, an —NHR3 group, and an —SH group, where R3 is a monovalent hydrocarbyl group having 1 to 10 carbon atoms; R is a divalent hydrocarbyl group; X is a heteroatom group; and R1 and R2 are each independently a substituted or unsubstituted hydrocarbyl group, wherein R1 and R2 can be optionally joined to form a ring.
摘要翻译：可用于含磷阻燃剂和阻燃聚氨酯泡沫的有机磷化合物，其中有机磷化合物显示在式（I）中，其中Y选自-OH基团，-NH 2基团，-NHR 3 基团和-SH基，其中R3是具有1-10个碳原子的一价烃基; R是二价烃基; X是杂原子基团; 并且R 1和R 2各自独立地为取代或未取代的烃基，其中R 1和R 2可以任选地连接形成环。

17. 发明申请

US20150246869A1 Process for Preparing Cinacalcet and Pharmaceutically Acceptable Salts Thereof 有权
标题翻译：制备西那卡塞和药学上可接受的盐的方法
公开(公告)号：US20150246869A1
公开(公告)日：2015-09-03
申请号：US14425905
申请日：2013-09-09
申请人： Produits Chimiques Auxiliaires et de Synthese
发明人： Jean-Marie Schneider , Jonathan Madec , Sergio Kreimerman , Gerard Guillamot
IPC分类号： C07C209/68 , C07F9/40
CPC分类号： C07C209/68 , C07B2200/13 , C07C209/52 , C07C209/84 , C07C211/30 , C07C249/02 , C07F9/40 , C07F9/4006 , C07F9/4015 , C07C251/16
摘要： The present patent application relates to a process for preparing, cinacalcet or a pharmaceutically acceptable salt thereof, which comprises reacting 3-trifluoromethylbenzaldehyde having the following formula (II) with the phosphorus-comprising derivative having the following formula all) in which R1 and R2, which may he identical or different, are each a (C1-C6)alkyl group. The present invention also relates to the phosphorus-comprising derivative having the formula (III), to the use thereof and to the process for preparing same. The present invention also relates to the phosphate salt of cinacalcet and to uses thereof.
摘要翻译：本专利申请涉及一种制备西他西酮或其药学上可接受的盐的方法，其包括使具有下式（II）的3-三氟甲基苯甲醛与所有具有下式的含磷衍生物反应：其中R1和R2，其可以相同或不同，各自为（C 1 -C 6）烷基。本发明还涉及具有式（III）的含磷衍生物，其用途及其制备方法。本发明还涉及西那卡塞的磷酸盐及其用途。

18. 发明授权

US09018413B2 Method for the production of alkylphosphonic acids, esters, and salts by oxidizing alkylphosphonous acids, and use thereof 有权
标题翻译：通过氧化烷基亚磷酸生产烷基膦酸，酯和盐的方法及其用途
公开(公告)号：US09018413B2
公开(公告)日：2015-04-28
申请号：US13140225
申请日：2009-10-06
申请人： Michael Hill , Werner Krause , Martin Sicken
发明人： Michael Hill , Werner Krause , Martin Sicken
IPC分类号： C07F9/22 , C09K21/12 , C07F9/38 , C07F9/40 , C07F9/48 , C08K5/5317
CPC分类号： C09K21/12 , C07F9/3808 , C07F9/4006 , C07F9/4816 , C07F9/4866 , C08K5/5317
摘要： The invention relates to a method for producing monocarboxy-functionalized dialkylphosphinic acids, esters, and salts, characterized in that a) a phosphinic acid source (I) is reacted with olefins (IV) in the presence of a catalyst A to obtain an alkylphosphonous acid, the salt or ester (II) thereof, and b) the obtained alkylphosphonous acid, the salt or ester (II) thereof is reacted with an oxidizing agent or with an oxidizing agent and water or with oxygen and water in the presence of a catalyst B to obtain the alkylphosphonic acid derivative (III), wherein R1, R2, R3, R4 are identical or different from each other and independently represent, inter alia, H, C1-C18-alkyl, C6-C18-aryl, C6-C18-aralkyl, C6-C18-alkylaryl, X and Y are identical or different from each other and independently represent H, C1-C18-alkyl, C6-C18-aryl, C6-C18-aralkyl, C6-C18-alkylaryl, Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Cu, Ni, Li, Na, K and/or a protonated nitrogenous base, and catalysts A and B are transition metals and/or transition metal compounds and/or catalyst systems composed of a transition metal and/or a transition metal compound and at least one ligand.
摘要翻译：本发明涉及一种用于制备单羧基官能化二烷基次膦酸，酯和盐的方法，其特征在于a）在催化剂A存在下，使次膦酸源（I）与烯烃（Ⅳ）反应得到烷基亚磷酸，其盐或酯（II），和b）得到的烷基亚磷酸，其盐或酯（II）与氧化剂或氧化剂和水或者在氧化和水中在催化剂存在下反应 B获得烷基膦酸衍生物（III），其中R 1，R 2，R 3，R 4彼此相同或不同，并且独立地表示H，C 1 -C 18 - 烷基，C 6 -C 18 - 芳基，C 6 -C 18 芳烷基，C 6 -C 18烷基芳基，X和Y彼此相同或不同，独立地表示H，C 1 -C 18烷基，C 6 -C 18芳基，C 6 -C 18芳烷基，C 6 -C 18烷基芳基， Ca，Al，Sb，Sn，Ge，Ti，Fe，Zr，Zn，Ce，Bi，Sr，Mn，Cu，Ni，Li，Na，K和/或质子化的含氮碱，催化剂A 和B是由过渡金属和/或过渡金属化合物和至少一种配体组成的过渡金属和/或过渡金属化合物和/或催化剂体系。

19. 发明申请

US20150105355A1 4-DEDIMETHYLAMINO TETRACYCLINE COMPOUNDS 有权
标题翻译： 4-DEDIMETHYLAMINO TETRACYCLINE化合物
公开(公告)号：US20150105355A1
公开(公告)日：2015-04-16
申请号：US14176923
申请日：2014-02-10
申请人： Paratek Pharmaceuticals, Inc.
发明人： Mark L. Nelson , Kwasi Ohemeng
IPC分类号： C07C237/26
CPC分类号： A61K31/65 , C07C235/70 , C07C237/26 , C07C251/48 , C07C255/41 , C07C271/22 , C07C271/54 , C07C271/58 , C07C275/42 , C07C275/54 , C07C279/18 , C07C311/06 , C07C311/08 , C07C333/08 , C07C335/22 , C07C381/10 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2603/46 , C07D295/155 , C07D295/185 , C07D317/60 , C07F9/2475 , C07F9/4006
摘要： The present invention pertains, at least in part, to novel substituted 4-dedimethylamino tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
摘要翻译：本发明至少部分地涉及新的取代的4-脱二甲基氨基四环素化合物。这些四环素化合物可用于治疗多种四环素化合物反应状态，例如细菌感染和肿瘤，以及其他已知的米诺环素和四环素化合物的一般应用，例如阻断四环素外排和调节基因表达。

20. 发明申请

US20150080487A1 METHOD OF MAKING HYDROXYMETHYLPHOSPHONATE, POLYURETHANE FOAM-FORMING COMPOSITIONS, POLYURETHANE FOAM AND ARTICLES MADE THEREFROM 审中-公开
标题翻译：制备羟基甲基磷酸酯的方法，聚氨酯泡沫成分组合物，聚氨酯泡沫及其制品
公开(公告)号：US20150080487A1
公开(公告)日：2015-03-19
申请号：US14314795
申请日：2014-06-25
申请人： ICL-IP America Inc
发明人： Jeffrey K. Stowell , Ronald L. Pirrelli , Ryan Yanosy
IPC分类号： C07F9/40 , C08J9/00
CPC分类号： C07F9/4006 , C08J9/0038 , C08J2375/04 , C08K5/5333 , C08L75/04
摘要： A method of making hydroxymethylphosphonate comprising heating paraformaldehyde in a solvent to a desired reaction temperature, wherein the solvent is present in at least an amount necessary to solvate or suspend the paraformaldehyde; adding at least one alkyl phosphite to the heated paraformaldehyde, to provide hydroxymethylphosphonate, the alkyl phosphite being added to the heated paraformaldehyde at a rate which will avoid or inhibit the production of a significant exotherm and resulting high/significant level of acid by-product(s), there being present in the reaction medium at least one hindered amine catalyst in which the nitrogen in the amine is directly bound to a secondary and/or tertiary carbon of an organic group; and, optionally, following the completion of the addition, heating the reaction mixture to an elevated temperature.
摘要翻译：一种制备羟甲基膦酸酯的方法，其包括在溶剂中加热多聚甲醛至所需的反应温度，其中所述溶剂以至少一定的量存在以溶解或悬浮多聚甲醛; 向加热的多聚甲醛中加入至少一种亚磷酸烷基酯以提供羟甲基膦酸酯，亚磷酸烷基酯以可避免或抑制显着放热产生和产生高/显着水平的副产物的速率加入到加热的多聚甲醛中在反应介质中存在至少一种受阻胺催化剂，其中胺中的氮直接与有机基团的仲碳和/或叔碳键合; 并且任选地，在完成添加之后，将反应混合物加热到升高的温度。

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