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1. 发明申请

US20230121306A1 SYNTHETIC ROUTE TO SCOPOLAMINE AND/OR ATROPINE 有权
公开(公告)号：US20230121306A1
公开(公告)日：2023-04-20
申请号：US17450254
申请日：2021-10-07
申请人： Southwest Research Institute
发明人： Shawn T. BLUMBERG , Paul W. MIGUEL , Daniel A. HINOJOSA
IPC分类号： C07D451/10
摘要： A synthetic route to scopolamine and/or atropine. In such context, the present invention identifies a method for preparing 6,7-dehydro atropine, which can be converted into either scopolamine and/or atropine, along with a method for converting a protected pyrrole into a tetrachlorobicylic compound, such as benzyl 3-oxo-8-azabicyclo[3.2.1]oct-6-ene-8-carboxylate.

2. 发明授权

US11266623B2 Use of cannabinoids and terpenes for treatment of organophosphate and carbamate toxicity 有权
公开(公告)号：US11266623B2
公开(公告)日：2022-03-08
申请号：US16004004
申请日：2018-06-08
申请人： KOTZKER CONSULTING LLC
发明人： Joseph Morgan
IPC分类号： A61K31/352 , A61K31/045 , A61K31/015 , A61K31/05 , A61K31/5517 , A61K31/5513 , C07D451/10 , A61K45/06 , A61K31/01 , A61K31/4425 , A61K31/46 , C07D471/08
摘要： Pharmaceutical compositions in which isolated cannabinoid receptor modulators are optionally combined with terpene blends in a pharmaceutically acceptable carrier. Methods for treating or preventing a disease, disorder, dysfunction or condition caused by exposure to an organophosphate or carbamate acetylcholinesterase inhibitor with the inventive compositions are also disclosed.

3. 发明申请

US20200375940A1 USE OF CANNABINOIDS AND TERPENES FOR TREATMENT OF ORGANOPHOSPHATE AND CARBAMATE TOXICITY 审中-公开
公开(公告)号：US20200375940A1
公开(公告)日：2020-12-03
申请号：US16945839
申请日：2020-08-01
申请人： KOTZKER CONSULTING LLC
发明人： Joseph Morgan
IPC分类号： A61K31/352 , C07D451/10 , A61K31/045 , A61K45/06 , A61K31/01 , A61K31/015 , A61K31/05 , A61K31/4425 , A61K31/46 , C07D471/08
摘要： Pharmaceutical compositions in which isolated cannabinoid receptor modulators are optionally combined with terpene blends in a pharmaceutically acceptable carrier. Methods for treating or preventing a disease disorder dysfunction or condition caused by exposure to an organophosphate or carbamate acetylcholinesterase inhibitor with the inventive compositions are also disclosed.

4. 发明授权

US10351565B2 Therapeutic compounds for pain and synthesis thereof 有权
公开(公告)号：US10351565B2
公开(公告)日：2019-07-16
申请号：US16005366
申请日：2018-06-11
申请人： JANSSEN PHARMACEUTICA NV
发明人： Bart DeCorte , Jacob Cornelis Russcher , Menno Cornelis Franciscus Monnee
IPC分类号： C07D471/18 , C07D451/04 , C07D451/12 , C07D451/00 , C07D451/06 , C07D451/10
摘要： The invention provides compounds of Formula 1: and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

5. 发明授权

US09108962B2 Forms of tiotropium bromide and processes for preparation thereof 有权
标题翻译：噻托溴铵的形式及其制备方法
公开(公告)号：US09108962B2
公开(公告)日：2015-08-18
申请号：US14305177
申请日：2014-06-16
申请人： Sicor, Inc.
发明人： Nicola Diulgheroff , Francesca Scarpitta , Alessandro Pontiroli , Adrienne Kovacsne-Mezei , Judith Aronhime , Alexandr Jegorov
IPC分类号： C07D451/12 , C07D451/10
CPC分类号： C07D451/12 , C07D451/10
摘要： This invention relates to novel crystalline forms of tiotropium bromide, processes for preparing them, and their use in pharmaceutical formulations.
摘要翻译：本发明涉及噻托溴铵的新型结晶形式，其制备方法及其在药物制剂中的应用。

6. 发明授权

US09090607B2 Process for preparing tiotropium bromide 有权
标题翻译：制备噻托溴铵的方法
公开(公告)号：US09090607B2
公开(公告)日：2015-07-28
申请号：US14377271
申请日：2013-02-08
申请人： Hovione International Limited
发明人： Luis Sobral , Marcio Temtem , Rafael Antunes , Bruna Nunes
IPC分类号： C07D491/08 , C07D451/14 , C07D451/10
CPC分类号： C07D451/14 , C07D451/10
摘要： The present invention relates to a novel process for the preparation of tiotropium bromide there is provided a process for preparing tiotropium bromide comprising (i) reacting scopine oxalate with diethylamine in an inert solvent to form scopine; (ii) reacting scopine and methyl di-(2-dithienyl)glycolate (MDTG) in the presence of an inorganic base, and in an inert solvent to form N-demethyltiotropium; (iii) reacting N-demethyltiotropium with bromomethane in an inert solvent to form tiotropium bromide; (iv) crystallizing tiotropium bromide in a mixture of methanol and acetone, and optionally thereafter, (v) micronizing the tiotropium bromide so formed.
摘要翻译：本发明涉及一种制备噻托溴铵的新方法，其提供了一种制备噻托溴铵的方法，其包括（i）在惰性溶剂中使草酸草丁酯与二乙胺反应以形成胡萝卜素; （ii）在无机碱的存在下和在惰性溶剂中反应西酞菁和二（2-二噻吩基）乙醇酸甲酯（MDTG）以形成N-脱甲基噻托铵; （iii）使N-去甲基二氢卟酚与溴甲烷在惰性溶剂中反应形成噻托溴铵; （iv）在甲醇和丙酮的混合物中结晶噻托溴铵，随后任选地（v）使如此形成的噻托溴铵微粉化。

7. 发明授权

US09079983B2 Chemoselective enrichment for compound isolation 有权
标题翻译：用于化合物分离的化学选择性富集
公开(公告)号：US09079983B2
公开(公告)日：2015-07-14
申请号：US13571591
申请日：2012-08-10
申请人： Erin E. Carlson , Darci Trader , Antoinette Odendaal
发明人： Erin E. Carlson , Darci Trader , Antoinette Odendaal
IPC分类号： C08F8/00 , C08F8/10 , C08F12/14 , C07C269/08 , C07C303/44 , C07C213/10 , C07C319/28 , C07D451/10 , C07C231/24 , C07D207/12 , C07C249/14 , C07D207/34 , C07D209/18 , C07C253/34 , C07D211/40 , C07D211/62 , B01D15/08 , B01J20/32 , C07J1/00 , C07J5/00 , C07J9/00 , C07J51/00
CPC分类号： C08F8/10 , B01D15/08 , B01J20/321 , B01J20/3261 , C07C213/10 , C07C231/24 , C07C249/14 , C07C253/34 , C07C269/08 , C07C303/44 , C07C319/28 , C07C2601/14 , C07C2602/08 , C07C2602/30 , C07C2603/26 , C07D207/12 , C07D207/34 , C07D209/18 , C07D211/40 , C07D211/62 , C07D451/10 , C07J1/0011 , C07J5/0053 , C07J9/005 , C07J51/00 , C08F8/00 , C08F12/14 , C08F12/18 , C08F8/12 , C08F8/42 , C07C271/16 , C07C271/24 , C07C215/12 , C07C215/16 , C07C215/76 , C07C233/25 , C07C271/22 , C07C323/59 , C07C251/60 , C07C255/57 , C07C233/51 , C07C311/16
摘要： Chemoselective isolation of hydroxyl group-containing and carboxyl group-containing compounds is accomplished via formation of polymeric silyl ethers and polymeric siloxyl esters, respectively. Preparation of chemoselective polymeric reagents for capture of hydroxyl group containing compounds and carboxyl group containing compounds is described.
摘要翻译：含羟基和含羧基化合物的化学选择性分离通过分别形成聚合物甲硅烷基醚和聚合物硅氧烷酯来实现。描述了用于捕获含羟基化合物和含羧基化合物的化学选择性聚合物试剂的制备。

8. 发明申请

US20140336137A1 NOVEL NITROSO COMPOUNDS AS NITROXYL DONORS AND METHODS OF USE THEREOF 有权
标题翻译：新型硝基化合物作为硝基衍生物及其使用方法
公开(公告)号：US20140336137A1
公开(公告)日：2014-11-13
申请号：US14444750
申请日：2014-07-28
申请人： Cardioxyl Pharmaceuticals, Inc.
发明人： Lisa Marie Frost , Stephen Martin Courtney , Frederick Arthur Brookfield , Vincent Jacob Kalish
IPC分类号： C07F9/58 , C07D211/58 , C07C207/04 , C07D405/14 , C07D451/10 , C07F9/117 , C07D405/12 , C07D309/14 , C07D333/42
CPC分类号： C07C207/00 , C07C207/04 , C07C255/19 , C07D211/44 , C07D211/58 , C07D309/10 , C07D309/14 , C07D333/42 , C07D405/12 , C07D405/14 , C07D407/12 , C07D451/10 , C07F9/117 , C07F9/58 , C07F9/59
摘要： The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
摘要翻译：本发明涉及在生理条件下给予硝酰基（HNO）的羟基亚硝基化合物的羧酸和磷酸酯的亚硝基衍生物。本发明的化合物和组合物可用于治疗和/或预防对硝酰病毒治疗（包括心力衰竭，局部缺血/再灌注损伤和癌症）有反应的疾病或病症的发作和/或发展。

9. 发明授权

US08568699B2 Soft anticholinergic zwitterions 有权
公开(公告)号：US08568699B2
公开(公告)日：2013-10-29
申请号：US13286020
申请日：2011-10-31
申请人： Nicholas S. Bodor
发明人： Nicholas S. Bodor
IPC分类号： C07D207/10 , C07D451/10 , A61K31/4015 , A61K31/56 , A61K31/58 , A61K8/49 , A61P11/00 , A61P11/06 , A61P37/08 , A61P13/10 , A61P29/00 , A61Q15/00
CPC分类号： C07D207/10 , A61K9/0019 , A61K9/0048 , A61K9/0075 , A61K9/008 , A61K9/2059 , A61K31/167 , A61K31/40 , A61K31/439 , A61K31/56 , A61K31/58 , A61K45/06 , C07D451/10 , A61K2300/00
摘要： Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.

10. 发明授权

US08101763B2 Method for producing scopine esters 有权
标题翻译：西酞菁酯的制备方法
公开(公告)号：US08101763B2
公开(公告)日：2012-01-24
申请号：US12601571
申请日：2008-05-09
申请人： Waldemar Pfrengle , Werner Rall , Joerg Brandenburg , Rolf Herter
发明人： Waldemar Pfrengle , Werner Rall , Joerg Brandenburg , Rolf Herter
IPC分类号： C07D451/10 , C07D265/36
CPC分类号： C07D451/10
摘要： The invention relates to a novel method for producing scopine esters of the general formula (1), wherein X—, R, R1, R2, R3, R4, R3′, R4′, R6 and R6′ can have the meanings indicated in the claims and in the description.
摘要翻译：本发明涉及一种制备通式（1）的扇叶酯的新方法，其中X，R，R 1，R 2，R 3，R 4，R 3'，R 4'，R 6和R 6'可以具有声明和说明书。

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