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1. 发明授权

US11439612B2 Formulations for administration of eflornithine 有权
公开(公告)号：US11439612B2
公开(公告)日：2022-09-13
申请号：US17002117
申请日：2020-08-25
申请人： Orbus Therapeutics, Inc.
发明人： Victor A. Levin , Noymi Yam , Alexander Vakoula
IPC分类号： A61K31/197 , A61K47/26 , A61P43/00 , A61P35/00 , C07C229/00 , A61K9/00 , A61P25/00
摘要： Eflornithine is an agent that can be used to treat glioma, especially glioma of WHO Grade II or Grade III such as anaplastic glioma. Eflornithine can suppress or prevent mutations in glioma which can cause the glioma to progress to a higher grade. The present invention describes pharmaceutical compositions that contain eflornithine or a derivative, analog, or prodrug thereof. The pharmaceutical compositions can be prepared in a number of dosage forms and may contain another therapeutically active agent or an agent that enhances the therapeutic activity of the elformithine or the derivative, analog, or prodrug thereof. The present invention also describes a kit that includes dosage forms of pharmaceutical compositions according to the present invention.

2. 发明申请

US20220273606A1 Polyoxometalate Complexes and Pharmaceutical Compositions 有权
公开(公告)号：US20220273606A1
公开(公告)日：2022-09-01
申请号：US17744369
申请日：2022-05-13
申请人： Emory University
发明人： Jie Song , Shuming Nie , Craig Hill
IPC分类号： A61K31/28 , A61P35/00 , A61K33/243 , A61K31/282 , C07C229/00 , B32B21/02 , C09D7/65 , C09D5/08 , C09D5/02
摘要： The disclosure relates polyoxometalate complexes and uses in the management, treatment, or prevention of cancer. In certain embodiments, the polyoxometalate complexes comprise polydentate oxygen bridging ligands such as those of the following formula: [POM{(OCH2)3CX}2], [M6O13{(OCH2)3CX}2], [V6O13{(OCH2)3CX}2], salts, or derivatives thereof wherein POM is a polyoxometalate, M is a metal, and X is defined herein. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising polyoxometalate complexes disclosed herein.

3. 发明授权

US10189760B2 Method for preparing sitagliptin intermediate via asymmetrical reduction method 有权
公开(公告)号：US10189760B2
公开(公告)日：2019-01-29
申请号：US15319370
申请日：2015-10-09
申请人： ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD. , SHANGHAI SYNCORES TECHNOLOGIES INC. LTD.
发明人： Jian Hong , Yusheng Wang , Boyu Wang , Luning Huang , Eric Gu
IPC分类号： C07C229/00 , C07C29/153 , B01J27/18 , C07C25/13 , C07D487/04 , C07C29/151
CPC分类号： C07C29/153 , B01J27/18 , B01J2231/44 , B01J2531/004 , C07C25/13 , C07C29/1514 , C07C227/32 , C07C229/34 , C07C269/04 , C07C271/22 , C07D487/04
摘要： Disclosed is a method for synthesizing a sitagliptin intermediate, the method comprising: in the presence of hydrogen and a transition metal catalyst having a chiral phosphine ligand, subjecting a compound of formula II to an asymmetric reductive amination with ammonia or ammonium salt in a proper organic solvent under the condition of adding an acidic additive to produce a compound of formula I, wherein, an R- or S-configuration of a stereocenter is represented by *; the compound of formula I of R configuration can be used to prepare sitagliptin, and a reaction formula is as follows: R1 and R2 are each independently selected from hydrogen, C1-C12 linear or branched alkyl, C3-C12 cycloalkyl, C2-C12 alkenyl, C2-C12 alkynyl and C7-C12 arylalkyl. The method has a high yield and a high ee % value, a mild reaction condition and a low production cost, and is simple to operate, convenient to purify, environmental friendly and suitable for industrial production.

4. 发明授权

US09828334B2 Process for preparing levomilnacipran 有权
公开(公告)号：US09828334B2
公开(公告)日：2017-11-28
申请号：US15106024
申请日：2014-11-27
申请人： LABORATORIO CHIMICO INTERNAZIONALE S.p.A.
发明人： Paolo Maria Farina , René Ignacio Rodriguez Curiel , Stefano Maiorana , Aldo Bianchi , Federica Colombo , Gabriele Timpano
IPC分类号： C07C229/00 , C07C237/24 , C07C271/22 , C07C231/20 , C07C229/36
CPC分类号： C07C237/24 , C07B2200/07 , C07C229/36 , C07C231/20 , C07C271/22 , C07C2601/02
摘要： The present invention refers to a new process for preparing levomilnacipran, in particular to a process for the resolution of racemic tw-milnacipran with a derivative of optically active phenylglycine.

5. 发明授权

US09737503B2 Short acting phenylalkylamine calcium channel blockers and uses thereof 有权
公开(公告)号：US09737503B2
公开(公告)日：2017-08-22
申请号：US15262567
申请日：2016-09-12
申请人： Milestone Pharmaceuticals Inc.
发明人： Martin P. Maguire , Elise Rioux , Harry J. Leighton
IPC分类号： A61K31/275 , C07C229/00 , C07C255/43 , A61K31/277 , C07C229/34 , C07C255/42 , C07C229/38 , A61K31/216 , A61K31/26
CPC分类号： A61K31/277 , A61K31/216 , A61K31/26 , A61K31/275 , C07C229/34 , C07C229/38 , C07C255/42 , C07C255/43
摘要： The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.

6. 再颁专利

USRE46496E1 Metformin glycinate for blood glucose control 有权
公开(公告)号：USRE46496E1
公开(公告)日：2017-08-01
申请号：US15135018
申请日：2016-04-21
申请人： Laboratorios Silanes S.A. de C.V.
发明人： Jose Manuel Francisco Ochoa Lara
IPC分类号： A61K9/20 , A61K31/27 , C07C61/08 , C07C229/00 , C07C251/00 , A61K31/15 , A61K31/131 , A61K31/198 , C07C279/26 , C07C229/08
CPC分类号： C07C279/26 , C07C229/08
摘要： The present invention relates to metformin glycinate salt and pharmaceutical compositions thereof for the treatment of diabetes mellitus. The method includes administration of the metformin glycinate salt by various routes selected from oral, intravenous injectable, intramuscular injectable, nasal, intraperitoneal, or sublingual, in order to achieve a reduction in blood glucose levels. The invention further relates to the synthesis of a new 1,1-dimethylbiguanide glycinate salt, called Metformin Glycinate. The resulting salt exhibits advantages over other metformin salts. These advantages are due, in the first place, to the fact that the glycine counterion exhibits hypoglycemic effects by itself. Moreover, the salt exhibits more rapid absorption, reaching higher plasma concentrations than those produced with metformin hydrochloride.

7. 发明授权

US09714215B2 Method for producing isocyanate 有权
公开(公告)号：US09714215B2
公开(公告)日：2017-07-25
申请号：US14781192
申请日：2014-03-28
申请人： Asahi Kasei Chemicals Corporation
发明人： Masaaki Shinohata , Kouji Takeuchi , Naoki Fujimoto , Nobuhisa Miyake
IPC分类号： C07C229/00 , C07C263/04 , C07C269/04
CPC分类号： C07C263/04 , C07C269/04 , Y02P20/51 , C07C265/14 , C07C271/06
摘要： A method for producing an isocyanate, comprising: a carbamation step of generating an N-substituted carbamate from an organic primary amine, urea and an organic hydroxy compound according to a carbamation reaction, and then recovering a first gaseous phase component containing the urea and/or a compound having a carbonyl group derived from the urea, the organic hydroxy compound, and ammonia; a condensation step of condensing the first gaseous phase component with a condenser; an isocyanate production step of producing an isocyanate by subjecting the N-substituted carbamate to pyrolysis; an ammonia absorption step of allowing a second gaseous phase component containing ammonia recovered as a gaseous phase component from the condenser as a main component, to be absorbed by absorption water, and generating gas-absorbed water; and an ammonia stripping step of heating the gas-absorbed water to separate ammonia from the gas-absorbed water.

8. 发明授权

US09701619B2 Process for producing amino acids from precursors obtained by anaerobic fermentation from fermentable biomass 有权
公开(公告)号：US09701619B2
公开(公告)日：2017-07-11
申请号：US15053854
申请日：2016-02-25
申请人： AFYREN
发明人： Régis Nouaille , Jérémy Pessiot , Marie Thieulin
IPC分类号： C07C205/00 , C07C207/00 , C07C229/00 , C07C227/06 , C07C227/08 , C07C51/363 , C12P7/52 , C12P7/54
CPC分类号： C07C227/06 , C07C51/363 , C07C227/08 , C12P7/52 , C12P7/54 , C07C53/16 , C07C53/19 , C07C229/08
摘要： The process for producing amino acids from volatile fatty acid (VFA) molecules, referred to as precursors, produced by anaerobic fermentation from fermentable biomass, comprises at least the following steps: a) extracting the volatile fatty acid (VFA) molecules, without stopping the fermentation, via an extraction means chosen from means that are, at least, insoluble in the fermentation medium, b) collecting, outside the fermentation reactor, the volatile fatty acid (VFA) molecules once they have been extracted, c) synthesizing, by halogenation, using a type of volatile fatty acid (VFA) chosen from the volatile fatty acids collected in step b) and defined according to the desired type of amino acid, a given α-halo acid, d) synthesizing from this α-halo acid a defined amino acid.

9. 发明授权

US09572785B2 DP2 antagonist and uses thereof 有权
标题翻译： DP2拮抗剂及其用途
公开(公告)号：US09572785B2
公开(公告)日：2017-02-21
申请号：US14468183
申请日：2014-08-25
申请人： Brickell Biotech, Inc.
发明人： Jason Edward Brittain , Brian Andrew Stearns , Christopher David King , Kevin Ross Holme
IPC分类号： A61K31/4418 , A61K31/195 , C07D213/64 , C07C229/00
CPC分类号： A61K31/195
摘要： Described herein is the DP2 antagonist [2′-(3-benzyl-1-ethyl-ureidomethyl)-6-methoxy-4′-trifluoromethyl-biphenyl-3-yl]-acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.
摘要翻译：本文描述的是DP2拮抗剂[2' - （3-苄基-1-乙基 - 脲基甲基）-6-甲氧基-4'-三氟甲基 - 联苯-3-基] - 乙酸或其药学上可接受的盐。还描述了制备DP2拮抗剂或其药学上可接受的盐的方法。本文还描述了适用于给予哺乳动物包括DP2拮抗剂或其药学上可接受的盐的药物组合物，以及使用这些药物组合物治疗呼吸系统疾病或病症，过敏性疾病或病症，炎性疾病或病症的方法，如以及其他前列腺素D2依赖性或前列腺素D2介导的疾病或病症。

10. 发明授权

US09527806B2 Structure, synthesis, and applications for poly (phenylene) ethynylenes (PPEs) 有权
标题翻译：聚（亚苯基）乙炔（PPEs）的结构，合成和应用
公开(公告)号：US09527806B2
公开(公告)日：2016-12-27
申请号：US13809572
申请日：2011-07-13
申请人： David G. Whitten , Kirk S. Schanze , Anand Parthasarathy , Eunkyung Ji , Motokatsu Ogawa , Thomas S. Corbitt , Dimitri Dascier , Ying Wang , Linnea K. Ista , Eric H. Hill
发明人： David G. Whitten , Kirk S. Schanze , Anand Parthasarathy , Eunkyung Ji , Motokatsu Ogawa , Thomas S. Corbitt , Dimitri Dascier , Ying Wang , Linnea K. Ista , Eric H. Hill
IPC分类号： C07C229/00 , C07C309/24 , C07C217/14 , C07C309/11 , C07C217/20 , C07D333/16 , C07D487/08 , C08G61/02 , C08G75/00
CPC分类号： C07D487/08 , C07C217/14 , C07C217/20 , C07C309/11 , C07C309/24 , C07D333/16 , C08G61/02 , C08G61/126 , C08G75/00 , C08G2261/312 , C08G2261/3223 , C08G2261/3328 , C08G2261/3422 , C08G2261/93
摘要： The present disclosure provides novel poly(phenylene ethynylene) (PPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various PPEs show antibacterial, antiviral and antifungal activity.
摘要翻译：本公开提供了新的聚（亚苯基亚乙炔基）（PPE）化合物，合成这些化合物的方法，以及掺入这些化合物的材料和物质。各种PPE显示抗菌，抗病毒和抗真菌活性。

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