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1. 发明申请

US20180325897A1 CO-CRYSTALS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME 审中-公开
公开(公告)号：US20180325897A1
公开(公告)日：2018-11-15
申请号：US16038696
申请日：2018-07-18
申请人： Vertex Pharmaceuticals Incorporated
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： A61K31/506 , C07K16/28 , A61K31/5025 , A61K31/513 , A61K31/517 , A61K31/337 , C07D401/14 , C07C63/08 , C07C59/265 , C07C57/15 , C07C57/145 , C07C55/14 , C07C55/10 , C07B59/00 , A61K45/06 , A61K39/395 , A61K38/14 , A61K33/24 , A61K31/7048 , A61K31/704 , A61K31/555 , A61N5/10
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.

2. 发明申请

US20180319766A1 CO-CRYSTALS OF BENZIMIDAZOLE COMPOUNDS 审中-公开
公开(公告)号：US20180319766A1
公开(公告)日：2018-11-08
申请号：US15775831
申请日：2016-11-18
申请人： FAES FARMA, S.A.
发明人： Gonzalo Hernandez Herrero , Victor Rubio Royo , Neftali Garcia Dominguez , Gonzalo Canal Mori , Carme Jimenez Gonzalez , Jordi De Mier Vinue , Nicolas Tesson
IPC分类号： C07D401/04 , C07C55/12 , C07C55/14 , C07C57/10 , C07C55/10 , C07C63/06 , C07C229/60 , C07C59/245 , C07C39/10 , C07C69/88 , C07C235/34
CPC分类号： C07D401/04 , C07B2200/13 , C07C39/10 , C07C55/10 , C07C55/12 , C07C55/14 , C07C57/10 , C07C59/245 , C07C63/06 , C07C69/88 , C07C229/60 , C07C235/34
摘要： The invention relates to a cocrystal comprising a) at least bilastine and, b) at least a cocrystal forming compound selected from the group consisting of glutaric acid, adipic acid, sorbic acid, succinic acid, benzoic acid, 4-aminobenzoic acid, L-malic acid, resorcinol, methyl 4-hydroxy benzoate and N-(4-hydroxyphenyl)acetamide and mixtures thereof, or a solvate thereof. The invention further relates to methods for obtaining said cocrystals and to their use in the treatment and/or prevention of conditions mediated by H1 histamine receptor, such as allergic disorders or diseases. The invention also relates to a method for increase the aqueous solubility of the above compounds of formula (I).

3. 发明授权

US10029977B2 Process for preparing a diamine/dicarboxylic acid salt 有权
公开(公告)号：US10029977B2
公开(公告)日：2018-07-24
申请号：US15258835
申请日：2016-09-07
申请人： DSM IP ASSETS B.V.
发明人： Eric Grolman , Rudy Rulkens
IPC分类号： C07C209/68 , C07C211/09 , C07C211/12 , C07C51/41 , C07C55/14 , C07C55/20 , C07C63/28 , C08G69/04 , C08G69/26
摘要： The present invention also relates to a process for preparing a diamine/dicarboxylic acid salt wherein the dicarboxylic acid comprises an aromatic dicarboxylic acid and is provided in a powder form; the diamine is provided in a liquid form gradually dosed to the dicarboxylic acid powder, while keeping the dicarboxylic acid powder in constant movement; the processing temperature is above 0° C. and below the boiling temperature of the diamine and the melting temperature of the acid and the salt, and the reaction mixture comprises at most 5 wt. % of water. The present invention also relates to an anhydrous diamine/dicarboxylic acid salt obtainable by the process according to invention, or any embodiment thereof as described above.

4. 发明授权

US09676793B2 Co-crystals of 5-amino-2-oxothiazolo[4,5-d]pyrimidin-3(2H)-yl-5-hydroxymethyl tetrahydrofuran-3-yl acetate and methods for preparing and using the same 有权
公开(公告)号：US09676793B2
公开(公告)日：2017-06-13
申请号：US14976713
申请日：2015-12-21
申请人： Hoffmann-La Roche Inc.
发明人： Urs Schwitter , Fritz Bliss , Michael Kammerer , Florence Tixeront
IPC分类号： C07D513/04 , C07C55/12 , C07C55/08 , C07C57/15 , C07C55/14 , C07C59/06 , C07C59/185
CPC分类号： C07D513/04 , C07C55/08 , C07C55/12 , C07C55/14 , C07C57/15 , C07C59/06 , C07C59/185
摘要： Co-crystals of Formula I compounds and their pharmaceutical compositions are novel therapeutics for the treatment of diseases, such as human immunodeficiency virus (HIV) infection, hepatitis B virus (HBV) infection, hepatitis C virus (HCV) infection and cancer. The co-crystal are more stable to oxidation and aqueous degradation, have a better pharmacokinetic profile and superior biological activity than the corresponding tosylate salt form of Formula I compound.

5. 发明授权

US09388103B2 Process for producing phenol 有权
标题翻译：苯酚生产工艺
公开(公告)号：US09388103B2
公开(公告)日：2016-07-12
申请号：US14343199
申请日：2012-08-09
申请人： Kun Wang , Roberto Garcia , Francisco M. Benitez
发明人： Kun Wang , Roberto Garcia , Francisco M. Benitez
IPC分类号： C08G61/02 , C07C37/08 , C07C45/53 , C07C407/00 , C07C2/74 , C07C39/21 , C07C55/14 , C07C251/44 , C07D223/10 , C08G6/00 , C08G65/38 , C08G69/00
CPC分类号： C07C37/08 , C07C2/74 , C07C39/21 , C07C45/53 , C07C55/14 , C07C251/44 , C07C407/00 , C07C2529/70 , C07C2601/14 , C07D223/10 , C08G6/00 , C08G65/38 , C08G69/00 , C07C39/04 , C07C49/403 , C07C409/14 , C07C13/28
摘要： In a process for producing phenol, a feed comprising cyclohexylbenzene hydroperoxide is contacted with a cleavage catalyst comprising an acidic ionic liquid under cleavage conditions effective to cleave at least a portion of said cyclohexylbenzene hydroperoxide and produce a cleavage product stream comprising phenol and cyclohexanone.
摘要翻译：在生产苯酚的方法中，将包含环己基苯氢过氧化物的进料与包含酸性离子液体的裂解催化剂在有效切割至少一部分所述环己基苯氢过氧化物的裂解条件下接触并产生包含苯酚和环己酮的裂解产物流。

6. 发明申请

US20150329460A1 PROCESS FOR THE PREPARATION OF ADIPIC ACID 审中-公开
标题翻译：制备丙二酸的方法
公开(公告)号：US20150329460A1
公开(公告)日：2015-11-19
申请号：US14653010
申请日：2013-12-19
申请人： DSM IP ASSETS B.V.
发明人： Michele Catherine Christianne JANSSEN , Jacob VAN SOOLINGEN , Henricus Wilhelmus Leonardus Marie VAESSEN
IPC分类号： C07C51/09 , C07C55/14
CPC分类号： C07C51/09 , C07C55/14
摘要： The invention relates to a process for the preparation of adipic acid from adipic acid alkyl ester comprising: subjecting an adipic acid alkyl ester to a hydrolysis reaction in the presence of water, at conditions of temperature and time suitable to form a hydrolysate comprising adipic acid; and optionally recovering adipic acid from said hydrolysate, characterized in that the hydrolysis reaction is carried out in the initial presence of adipic acid, and further to adipic acid obtained by the process. The invention also relates to the use of adipic acid as an acid catalyst in the hydrolysis of adipic acid alkyl ester. The process may advantageously be carried out in the absence of a mineral acid or a heterogeneous catalyst. The adipic acid produces with the process may be low in metals and/or sulphates.
摘要翻译：本发明涉及一种从己二酸烷基酯制备己二酸的方法，包括：在适宜形成包含己二酸的水解产物的温度和时间的条件下，使己二酸烷基酯在水存在下进行水解反应; 并且任选地从所述水解产物中回收己二酸，其特征在于水解反应在己二酸的初始存在下进一步进行，并进一步通过该方法获得的己二酸进行。本发明还涉及在己二酸烷基酯的水解中使用己二酸作为酸催化剂。该方法可有利地在不存在无机酸或多相催化剂的情况下进行。己二酸产生的方法可能是低的金属和/或硫酸盐。

7. 发明申请

US20150051213A1 NOVEL SALTS OF SITAGLIPTIN 审中-公开
标题翻译： SITAGLIPTIN的新口号
公开(公告)号：US20150051213A1
公开(公告)日：2015-02-19
申请号：US14129893
申请日：2012-06-26
申请人： Suresh Babu Jayachandra , Jigar Bhaskarbhai Shah , Sailu Chiguru
发明人： Suresh Babu Jayachandra , Jigar Bhaskarbhai Shah , Sailu Chiguru
IPC分类号： C07D487/04 , C07C55/14 , C07C63/24 , C07D213/79 , C07C65/10 , C07C53/126
CPC分类号： C07D487/04 , C07C53/126 , C07C55/14 , C07C63/24 , C07C65/10 , C07D213/79
摘要： The present invention provides sitagliptin 4-methylsalicylate, sitagliptin myristate, sitagliptin isophthalate, sitagliptin isonicotinide, sitagliptin adipate, their polymorphic form, processes for their preparation and pharmaceutical compositions thereof.
摘要翻译：本发明提供西他列汀4-甲基水杨酸酯，肉豆蔻酸西他列霉素，间苯二甲酸西他列霉素，西他列汀异烟肼，西他列汀己二酸酯，其多晶型物，其制备方法及其药物组合物。

8. 发明申请

US20130115654A1 METHOD FOR PRODUCING BIOBASED CHEMICALS FROM AGRICULTURAL BIOMASS 审中-公开
标题翻译：从农业生物质生产生物化学品的方法
公开(公告)号：US20130115654A1
公开(公告)日：2013-05-09
申请号：US13292531
申请日：2011-11-09
申请人： John R. Peterson , Christopher M. Yost , Jian Wu
发明人： John R. Peterson , Christopher M. Yost , Jian Wu
IPC分类号： C12P1/00 , C07C43/23 , C07C43/205 , C07C1/00 , C07C31/08 , C08B3/06 , C08B3/00 , C07C55/14 , C07C69/52 , C07C63/04 , C07C69/66 , C07D307/02 , C07C31/20 , C07D307/33 , C07C31/22 , C07D307/06 , C07C31/26 , C07D307/50 , C07C39/20 , C07C63/06 , C07C65/03 , C07C45/00 , C07C39/10 , C07C39/04 , C07C41/01
CPC分类号： C07D307/42 , C07C27/00 , C07D307/06 , C07D307/33 , C07D307/50 , C07D307/54 , C08B37/0057 , C08H8/00
摘要： A method for utilizing agricultural biomass components, namely cellulose, hemicellose, and lignin, and converting them to value-added biobased chemical products is described herein. The present method provides treatments to obtain a plurality of component streams from agricultural biomass for producing derivative products while minimizing waste products.
摘要翻译：本文描述了利用农业生物质成分（即纤维素，半纤维素和木质素）并将其转化为增值生物基化学产品的方法。本方法提供了从农业生物质获得多个组分流的方法，用于生产衍生产物，同时使废物最小化。

9. 发明申请

US20080039653A1 Process for Producing Adipic Acid 失效
标题翻译：生产己二酸的方法
公开(公告)号：US20080039653A1
公开(公告)日：2008-02-14
申请号：US11596455
申请日：2004-05-18
申请人： Masaji Hirota , Koji Hagiya
发明人： Masaji Hirota , Koji Hagiya
IPC分类号： C07C55/14
CPC分类号： C07C51/313 , B01J23/30 , C07C51/487 , C07C55/14
摘要： It is provided to a process for producing adipic acid which comprises making a wastewater containing hydroxycaproic acid and discharged from the step of oxidizing cyclohexane with molecular oxygen in a liquid phase react with hydrogen peroxide in the presence of a tungsten catalyst in the pH range of 0 to 6.
摘要翻译：提供了一种生产己二酸的方法，其包括制备含有羟基己酸的废水，并且在氧化环己烷的步骤中与分子氧在液相中与在过氧化氢中反应的步骤在钨催化剂存在下在pH范围为0的条件下与过氧化氢反应到6。

10. 发明申请

US20050004381A1 Amino acid derived prodrugs of propofol, compositions and uses thereof 有权
标题翻译：丙泊酚的氨基酸衍生前药，其组合物和用途
公开(公告)号：US20050004381A1
公开(公告)日：2005-01-06
申请号：US10766990
申请日：2004-01-28
申请人： Mark Gallop , Feng Xu , Kenneth Cundy , Vivek Sasikumar , Thomas Woiwode
发明人： Mark Gallop , Feng Xu , Kenneth Cundy , Vivek Sasikumar , Thomas Woiwode
IPC分类号： A61K31/05 , A61K38/00 , A61K38/04 , A61P25/00 , C07C39/07 , C07C55/12 , C07C55/14 , C07C237/12 , C07C329/06
CPC分类号： C07C229/24 , A61K47/64 , C07C229/08 , C07C237/12 , C07C329/06
摘要： The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting.
摘要翻译：本发明提供丙泊酚前药，制备异丙酚前药的方法，异丙酚前药的药物组合物和使用异丙酚前药的方法及其药物组合物，用于治疗或预防疾病或病症如偏头痛头痛和化疗后或术后手术恶心和呕吐。

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