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1. 发明申请

WO2013050929A1 MANUFACTURING PROCESS FOR TIOTROPIUM BROMIDE 审中-公开
标题翻译：生物反应器的制造工艺
公开(公告)号：WO2013050929A1
公开(公告)日：2013-04-11
申请号：PCT/IB2012/055275
申请日：2012-10-02
申请人： DRUG PROCESS LICENSING ASS., LLC , SOUKUP, Milan
发明人： SOUKUP, Milan
IPC分类号： C07D451/12 , C07D409/14
CPC分类号： C07D409/14 , C07D491/08
摘要： The present invention relates to a novel manufacturing process of pharmaceutically active compound of Formula (I) used as a long-acting anticholinergic bronchodilator. Starting from oxalic acid derivative of Formula (III) the invention describes preparation of a novel cyclic anhydride of Formula (II) which is very efficient precursor in the synthesis of Tiotropium bromide (compound of Formula (I)).
摘要翻译：本发明涉及用作长效抗胆碱能支气管扩张剂的式（I）药物活性化合物的新型制造方法。从式（III）的草酸衍生物开始，本发明描述了在合成噻托溴铵（式（I）的化合物）中非常有效的前体的式（II）的新型环状酸酐的制备。

2. 发明申请

WO2011138916A1 多環式化合物审中-公开
标题翻译：多环化合物
公开(公告)号：WO2011138916A1
公开(公告)日：2011-11-10
申请号：PCT/JP2011/060242
申请日：2011-04-27
申请人：第一三共株式会社 , 池田拓也 , 山崎高典 , 城島孝明 , 高木奈々
发明人：池田　拓也 , 山崎　高典 , 城島　孝明 , 高木　奈々
IPC分类号： C07D401/12 , A61K31/435 , A61K31/4439 , A61K31/4545 , A61K31/46 , A61K31/496 , A61P1/02 , A61P1/04 , A61P1/08 , A61P7/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/08 , A61P11/10 , A61P11/14 , A61P13/08 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/16 , A61P25/22 , A61P25/24 , A61P27/02 , A61P29/00 , A61P37/08 , A61P43/00 , C07D409/14 , C07D413/14 , C07D451/12
CPC分类号： C07D401/12 , C07D213/75 , C07D409/14 , C07D413/14 , C07D451/12
摘要：　本発明は、優れたニューロキニンＮＫ１、ニューロキニンＮＫ２及びムスカリンＭ３受容体拮抗作用、又は、優れたニューロキニンＮＫ１及びムスカリンＭ３受容体拮抗作用を有し、気管支喘息、慢性閉塞性肺疾患等の治療薬として有用な化合物又はその薬理上許容される塩に関する。　一般式（Ｉ）［式中、　Ｙは、ニューロキニンＮＫ１及びニューロキニンＮＫ２受容体拮抗作用を有する部分構造、又は、ニューロキニンＮＫ１受容体拮抗作用を有する部分構造；Ａは、単結合、三重結合、酸素原子、カルボニル基等；Ｅは、ムスカリンＭ３受容体拮抗作用を有する部分構造；ｍは、０乃至４の整数；ｎは、１乃至８の整数］を有する化合物又はその薬理上許容される塩。
摘要翻译：公开了具有优异的神经激肽NK1，神经激肽NK2和毒蕈碱M3受体拮抗作用或优良的神经激肽NK1和毒蕈碱M3受体拮抗作用的化合物，也可用作支气管哮喘，慢性阻塞性肺病等的治疗剂，或其药学上可接受的盐。具体公开的是具有通式（I）的化合物或其盐。 [式中Y是具有神经激肽NK1和神经激肽NK2受体拮抗作用的部分结构或具有神经激肽NK1受体拮抗作用的部分结构。 A是单键，三键，氧原子，羰基等; E是具有毒蕈碱M3受体拮抗作用的部分结构; m是0-4的整数; n为1-8的整数。]

3. 发明申请

WO9109593A3 5-HT3 ANTAGONISTS FOR TREATMENT OF NAUSEA, BRADYCARDIA OF HYPOTENSION ASSOCIATED WITH MYOCARDIAL INSTABILITY 审中-公开
标题翻译： 5-HT3拮抗剂治疗NAUSEA，BRADYCARDIA与低密度脂蛋白胆固醇不稳定相关的HYPTECA
公开(公告)号：WO9109593A3
公开(公告)日：1991-09-05
申请号：PCT/GB9001996
申请日：1990-12-20
申请人： BEECHAM GROUP PLC
发明人： JOHNSON EDWARD STEWART , HAMILTON THOMAS CONWAY
IPC分类号： A61K31/40 , A61K31/00 , A61K31/403 , A61K31/415 , A61K31/4184 , A61K31/435 , A61P1/08 , A61P9/02 , A61P9/04 , A61P43/00 , C07D209/52 , C07D231/14 , C07D231/38 , C07D235/26 , C07D451/04 , C07D451/12 , C07D451/14 , C07D453/02 , C07D453/06 , C07D471/04
CPC分类号： A61K31/00
摘要： A method for the treatment and/or prophylaxis of nausea and bradycardia and/or hypotension associated with myocardial instability in mammals, such as humans, which method comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of a 5-HT3 receptor antagonist, such as a compound of formula (I): X-A-R, or a pharmaceutically acceptable salt thereof, wherein X is a phenyl group or a monocyclic 5 or 6 membered heteroaryl group, either of which group is optionally fused to a saturated or unsaturated 5-7 membered carbocyclic or heterocyclic ring; A is a linking moiety; and R is a saturated azabicyclic moiety or an imidazolyl moiety.

4. 发明申请

WO2013079040A1 MIXED SOLVATE OF TIOTROPIUM BROMIDE AND A METHOD OF ITS PREPARATION 审中-公开
标题翻译：溴化钍的混合溶剂及其制备方法
公开(公告)号：WO2013079040A1
公开(公告)日：2013-06-06
申请号：PCT/CZ2012/000121
申请日：2012-11-28
申请人： ZENTIVA K.S.
发明人： CERNA, Igor , RIDVAN, Ludek , KRAL, Vladimir , HAJICEK, Josef , DAMMER, Ondrej
IPC分类号： C07D451/12 , A61K31/46 , A61P11/00
CPC分类号： C07D451/12
摘要： Mixed solvate of propyleneglycol/ethanol solvate of tiotropium bromide of formula V contains ethanol in the range of 3,000 to 40,000 ppm and propyleneglycol in the range of 3,000 to 40,000 ppm. An additional solution provides a method of preparing the solvate of tiotropium bromide, wherein a form of tiotropium bromide, selected from an anhydrous form, hydrate, solvate, or mixed solvate, is dissolved in a mixture of propyleneglycol and ethanol at a temperature in the range of from 40°C to the boiling point of the solvent, the formed solution is cooled down and the precipitated solvate is isolated. The solvate of tiotropium bromide is used in preparing an inhalation therapeutic formulation.
摘要翻译：式V的噻托溴铵的丙二醇/乙醇溶剂合物的混合溶剂化物含有3,000至40,000ppm范围内的乙醇和3,000至40,000ppm范围内的丙二醇。另外的溶液提供了制备噻托溴铵的溶剂合物的方法，其中将选自无水形式，水合物，溶剂合物或混合溶剂化物的噻托溴铵的形式溶解在丙二醇和乙醇的混合物中，温度范围从40℃到溶剂的沸点，将形成的溶液冷却并分离沉淀的溶剂合物。噻托溴铵的溶剂合物用于制备吸入治疗剂型。

5. 发明申请

WO2012071509A3 BENZOXAZEPINES AS INHIBITORS OF P13K/MTOR AND METHODS OF THEIR USE AND MANUFACTURE 审中-公开
公开(公告)号：WO2012071509A3
公开(公告)日：2012-05-31
申请号：PCT/US2011/062040
申请日：2011-11-23
申请人： EXELIXIS, INC. , RICE, Kenneth
发明人： RICE, Kenneth
IPC分类号： C07D413/04 , C07D413/06 , C07D413/14 , C07D417/14 , C07D451/02 , C07D451/06 , C07D451/12 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D519/00 , A61K31/553 , A61P35/00
摘要： The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. 9936396.1

6. 发明申请

WO2009037111A2 METHOD FOR THE PRODUCTION OF 1,3-DIOXOLANE-2-ONES AND CARBOXYLIC ACID ESTERS BY MEANS OF TRANSACYLATION IN BASIC REACTION CONDITIONS 审中-公开
标题翻译：用于生产1,3-二氧杂环戊-2-酮和羧酸酯中在碱性条件下transacylation
公开(公告)号：WO2009037111A2
公开(公告)日：2009-03-26
申请号：PCT/EP2008061618
申请日：2008-09-03
申请人： BOEHRINGER INGELHEIM PHARMA , BRANDENBURG JOERG , BALTES HANFRIED , DACH ROLF
发明人： BRANDENBURG JOERG , BALTES HANFRIED , DACH ROLF
IPC分类号： C07D317/34 , A61K31/38 , A61K31/438 , A61P11/00 , C07D317/72 , C07D409/14 , C07D451/10 , C07D451/12 , C07D491/10
CPC分类号： C07D491/10 , C07D317/34 , C07D317/72 , C07D409/14 , C07D451/10 , C07D451/12
摘要： The invention relates to a method for producing 1,3-dioxolane-2-ones of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1 to R5 have the meanings indicated in the claims and the description. The invention further relates to a method for producing 2-hydroxy carboxylic acid esters of general formula (5) with or without isolation of the intermediate in the form of a derivative of the 1,3-dioxolane-2-one of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1, R2, and R6 have the meanings indicated in the claims and the description. The method according to the invention allows the reaction to take place in very gentle basic conditions, causing fewer secondary reactions and providing a greater yield than reactions in highly polar aprotic solvents. Acid-sensitive and/or temperature-sensitive compounds can be synthesized.
摘要翻译：本发明涉及一种方法，用于由通式的相应的酯的酯交换产生碱性反应条件下将通式（3）的1,3-二氧戊环-2-酮（1），其特征在于在权利要求中所列出的和R1至R5的描述有含义。本发明还涉及一种用于具有或不具有中间的隔离中的衍生物的形式的通式的1,3-二氧戊环-2-酮制备通式（5）的2-羟基羧酸酯（3）的酯交换碱性反应条件下通式的相应的酯（1），其中R1，R2和R6具有权利要求书和说明书中给出的含义。本发明的方法允许非常温和的碱性条件下的反应，提供了更少的副反应，并与在高极性的非质子溶剂中的反应更高的产量。酸，和/或温度敏感的化合物的合成是可能的。

7. 发明申请

WO02096855A3 ANTICHOLINERGIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：抗生素化合物及其使用方法
公开(公告)号：WO02096855A3
公开(公告)日：2003-02-13
申请号：PCT/US0210614
申请日：2002-04-03
申请人： ARYX THERAPEUTICS , DRUSGALA PASCAL
发明人： DRUSGALA PASCAL
IPC分类号： C07D295/14 , A61K31/137 , A61K31/195 , A61K31/197 , A61K31/205 , A61K31/216 , A61K31/222 , A61K31/225 , A61K31/24 , A61K31/265 , A61K31/40 , A61K31/439 , A61K31/46 , A61P1/00 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/00 , A61P25/02 , A61P27/08 , A61P43/00 , C07C219/20 , C07C229/30 , C07C229/34 , C07C229/38 , C07D451/06 , C07D451/10 , C07D451/12 , C07D453/02 , A61K31/235
CPC分类号： C07D451/06 , A61K31/225 , C07C219/20 , C07C229/34 , C07C229/38 , C07D453/02
摘要： In a preferred embodiment, the subject invention concerns novel analogs of oxybutynin. The present invention also concerns methods for synthesizing the oxybutynin analogs of the present invention. The invention also pertains to methods for treating patients suffering from incontinence and other conditions.
摘要翻译：在优选的实施方案中，本发明涉及奥昔布宁的新型类似物。本发明还涉及用于合成本发明的奥昔布宁类似物的方法。本发明还涉及治疗患有失禁和其他病症的患者的方法。

8. 发明申请

WO1994015935A1 DERIVATIVES OF BENZOYLECGONINE, ECGONINE AND ECGONIDINE AS MEDICINES 审中-公开
标题翻译：苯并恶嗪，心磷酯和心磷脂作为药物的衍生物
公开(公告)号：WO1994015935A1
公开(公告)日：1994-07-21
申请号：PCT/US1993012625
申请日：1993-12-23
申请人： ENTROPIN, INC. , SOMERS, Lowell, M. , WYNN, James, E.
发明人： ENTROPIN, INC.
IPC分类号： C07D451/12
CPC分类号： C07D451/02 , C07D451/12
摘要： A compound of formula (I), formula (II) or formula (III), wherein R1 is selected from the group consisting of H; branched or unbranched alkyl, alkenyl and alkynyl, said alkyl, alkenyl and alkynyl being optionally substituted with OH, SH, NH2 or halogen; COCH3; COPh; and COBn; R2 is selected from the group consisting of branched or unbranched alkyl, alkenyl and alkynyl, said alkyl, alkenyl and alkynyl being optionally substituted with OH, SH, NH2 or halogen; aryl; Het; and benzyl; R3 is selected from the group consisting of branched or unbranched alkyl, alkenyl and alkynyl, said alkyl, alkenyl and alkynyl being optionally substituted with OH, SH, NH2 or halogen; R4 is selected from the group consisting of H; and branched or unbranched alkyl, alkenyl and alkynyl, said alkyl, alkenyl and alkynyl being optionally substituted with OH, SH, NH2 or halogen; and X is selected from the group consisting of OH; SH; NH2; and halogen: which are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain.
摘要翻译：式（I），式（II）或式（III）的化合物，其中R 1选自H; 支链或非支链烷基，烯基和炔基，所述烷基，烯基和炔基任选被OH，SH，NH 2或卤素取代; COCH3; COPH; 和COBn; R 2选自支链或非支链烷基，烯基和炔基，所述烷基，烯基和炔基任选被OH，SH，NH 2或卤素取代; 芳基; HET; 和苄基; R 3选自支链或非支链烷基，烯基和炔基，所述烷基，烯基和炔基任选被OH，SH，NH 2或卤素取代; R4选自H; 所述烷基，链烯基和炔基任选被OH，SH，NH 2或卤素取代; X选自OH; SH; NH2; 和卤素：其可用于减轻免疫调节障碍，神经肌肉疾病，关节疾病，结缔组织疾病，循环障碍和疼痛的症状。

9. 发明申请

WO2019143508A1 PREPARATION OF (-)-COCAINE HYDROCHLORIDE 审中-公开
公开(公告)号：WO2019143508A1
公开(公告)日：2019-07-25
申请号：PCT/US2019/012897
申请日：2019-01-09
申请人： CODY LABORATORIES, INC.
发明人： YAO, Qingwei , KIM, Se-Ho
IPC分类号： C07D451/12 , C07D451/06 , A61K31/46 , A61P23/02
摘要： Efficient methods are provided for large scale production of ethyl cocaine-free cocaine hydrochloride. Compositions and methods comprising administration of cocaine hydrochloride are provided.

10. 发明申请

WO2017179976A1 MEANS AND METHODS FOR THE N-DEALKYLATION OF AMINES 审中-公开
标题翻译：胺的N-烷基化方法和方法
公开(公告)号：WO2017179976A1
公开(公告)日：2017-10-19
申请号：PCT/NL2017/050226
申请日：2017-04-13
申请人： RIJKSUNIVERSITEIT GRONINGEN , STICHTING VOOR DE TECHNISCHE WETENSCHAPPEN
发明人： YUAN, Tao , BISCHOFF, Rainer Paul Hermann , PERMENTIER, Hjalmar Petrus
IPC分类号： C07C213/08 , C07D451/12 , C07C231/12 , B01J23/52
CPC分类号： C07C231/12 , B01J23/52 , B01J25/00 , B01J35/0033 , B01J35/1061 , B01J37/06 , C07C213/08 , C07D451/10 , C07C237/04 , C07C217/34
摘要： The invention relates to improved means and methods for N- dealkylation of alkylated amines. Provided is a method for the catalytic N- dealkylation of an N-alkylated amine substrate, comprising incubating said amine substrate in a suitable solvent in the presence of a nanoporous gold (NPG) surface and allowing for the formation of an N-dealkylation product. Also provided is a reaction mixture comprising an N-alkylated amine substrate in a suitable solvent and a NPG surface.
摘要翻译：本发明涉及用于烷基化胺的N-脱烷基化的改进方法和方法。提供了用于N-烷基化胺底物的催化N-去烷基化的方法，包括在纳米多孔金（NPG）表面存在下将所述胺底物在合适的溶剂中温育并且允许形成N-脱烷基化产物。还提供了一种反应混合物，其包含在合适溶剂和NPG表面中的N-烷基化胺底物。

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