公开(公告)号：US11905232B2

公开(公告)日：2024-02-20

申请号：US17429183

申请日：2020-02-10

申请人： Nogra Pharma Limited

发明人： Salvatore Demartis ,  Francesca Viti ,  Marie McNulty

IPC分类号： C07C231/10 ,  C07C201/12 ,  C07C205/56 ,  C07C231/18 ,  C07C233/54 ,  C07C231/02 ,  C07C227/04 ,  C07C303/28

CPC分类号： C07C231/10 ,  C07C201/12 ,  C07C205/56 ,  C07C227/04 ,  C07C231/02 ,  C07C231/18 ,  C07C233/54 ,  C07C303/28 ,  C07C201/12 ,  C07C205/56 ,  C07C303/28 ,  C07C309/66 ,  C07C227/04 ,  C07C229/42 ,  C07C231/02 ,  C07C233/54

摘要： The disclosure provides a process for the preparation of 3-(4′-aminophenyl)-2-methoxypropionic acid, and analogs and intermediates thereof, contemplated to be capable of modulating the activity of receptors, e.g., PPARs receptors.

公开(公告)号：US20230113948A1

公开(公告)日：2023-04-13

申请号：US17787089

申请日：2020-12-17

申请人： ARBUTUS BIOPHARMA CORPORATION

发明人： Mahesh PALLERLA ,  Ganapati Reddy PAMULAPATI ,  Jan SPINK

IPC分类号： A61K47/54 ,  C07D491/048 ,  C07D207/08 ,  C07C213/08 ,  C07H1/00 ,  C07H15/08 ,  C07C231/12 ,  C07C231/02 ,  C07D207/46 ,  C07C201/12 ,  C07C227/04 ,  C07C231/10 ,  C07C237/06 ,  C07C237/16 ,  C12N15/113 ,  A61K45/06

摘要： The invention provides synthetic processes and synthetic intermediate compounds that can be used to prepare therapeutic conjugates. The invention also provides methods for treating HBV and/or HDV infection in a human by administering a therapeutic conjugate prepared by the synthetic methods of the invention.

公开(公告)号：US20220298116A1

公开(公告)日：2022-09-22

申请号：US17619383

申请日：2019-07-04

申请人： F.l.S. - FABBRICA ITALIANA SINTETICI S.P.A

发明人： Paolo STABILE ,  Floriana SEMERARO

IPC分类号： C07D231/46 ,  B01J23/44 ,  C07C65/105 ,  C07C201/08 ,  C07C227/04

摘要： Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of Eltrombopag, passing through/using intermediate 5′-Chloro-2′-hydroxy[1,1′-biphenyl]-3-carboxylic acid alkaline metal salt of formula: wherein A is an alkaline metal.

公开(公告)号：US20190276388A1

公开(公告)日：2019-09-12

申请号：US16335342

申请日：2017-09-06

申请人： Umicore AG & Co. KG

发明人： Adam M Johns ,  Jessica R. HERRON ,  Richard L. PEDERSON ,  Thay A. UNG ,  Ba L. TRAN ,  Daryl P. ALLEN

IPC分类号： C07C227/04 ,  C07C229/08 ,  B01J31/22

摘要： The invention relates to a method for synthesizing amino acids or amino acid derivatives involving cross metathesis of functionalized olefins and a tandem amination-reduction process. Amino acids and amino acid derivatives present many interesting physical and chemical properties finding many uses in the automotive, fuel, electronic, and textile industries.

公开(公告)号：US10399926B1

公开(公告)日：2019-09-03

申请号：US16150517

申请日：2018-10-03

申请人： Divi's Laboratories Ltd.

发明人： Satchandra Kiran Divi ,  Mysore AswathaNarayana Rao ,  Surendra Kalyan Nuthi

IPC分类号： C07C227/04 ,  C07C235/88 ,  C07C231/12

摘要： The present invention relates to an improved process for the preparation of Gabapentin. The process also relates to a new process for the preparation of 1, 1-cyclohexane diaceitic acid monoamide (CDMA), which is a key intermediate for the preparation of Gabapentin.

公开(公告)号：US10377700B2

公开(公告)日：2019-08-13

申请号：US15912772

申请日：2018-03-06

申请人： BRACCO IMAGING S.P.A.

发明人： Elisa Battistini ,  Federica Buonsanti ,  Daniela Imperio ,  Luciano Lattuada ,  Roberta Napolitano

IPC分类号： C07C231/14 ,  C07C231/02 ,  C07F5/04 ,  C07F5/05 ,  C07C201/12 ,  C07C227/04 ,  C07C231/12 ,  C07F5/02 ,  C07C237/46

摘要： The present invention discloses a process for recovery of a boronic acid of formula R3—B(OH)2, wherein R3 is selected from the group consisting of C1-C6 linear or branched alkyl, C3-C6 cycloalkyl, and C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl, and phenyl, comprising admixing the boronic acid with a water-immiscible organic solvent in a weight ratio between the boronic acid and the water-immiscible organic solvent from 1:10 to 1:20, adding an aqueous solution to a final pH of neutral, and partitioning the boronic acid into an organic water-immiscible phase and recovery of the organic water-immiscible phase.

公开(公告)号：US20190077745A1

公开(公告)日：2019-03-14

申请号：US16052695

申请日：2018-08-02

申请人： BRACCO IMAGING S.P.A.

发明人： Elisa BATTISTINI ,  Federica BUONSANTI ,  Daniela IMPERIO ,  Luciano LATTUADA ,  Roberta NAPOLITANO

IPC分类号： C07C231/14 ,  C07C231/02 ,  C07F5/04 ,  C07F5/05 ,  C07F5/02 ,  C07C201/12 ,  C07C227/04 ,  C07C231/12 ,  C07C237/46

摘要： The present invention discloses a process for the preparation of Iopamidol of formula (II) and comprising the following steps: a) reacting the Compound (I) wherein X is OR2 or R3, and wherein R2 and R3 are a C1-C6 linear or branched alkyl, C3-C6 cycloalkyl, C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl and phenyl, with the acylating agent (S)-2-(acetyloxy)propanoyl chloride in a reaction medium to provide the acetyloxy derivative of Compound (I); b) hydrolyzing the intermediate from step a) with an aqueous solution at a pH comprised from 0 to 7, by adding water or a diluted alkaline solution such as sodium hydroxide or potassium hydroxide, freeing the hydroxyls from the boron-containing protective groups, obtaining the N-(S)-2-(acetyloxy)propanoyl derivative of Compound (II); c) alkaline hydrolysis to restore the (S)-2-(hydroxy)propanoyl group and to obtain Iopamidol (II) and optional recovery of the boron derivative from the solution obtained in step b). The boron-containing protective group is versatile, efficient and recyclable. A one-pot synthesis, without intermediate isolation is provided, leading to a decreasing of recovered and recycled solvents and a significant increasing in the yield, representing a significant advantage in terms of cost-effectiveness of the entire process and environmental awareness.

公开(公告)号：US10207984B2

公开(公告)日：2019-02-19

申请号：US15145323

申请日：2016-05-03

申请人： Emory University ,  Wake Forest University Health Sciences

发明人： Huw M. L. Davies ,  Spandan Chennamadhavuni ,  Thomas J. Martin ,  Steven R. Childers

IPC分类号： C07C229/46 ,  A61K31/195 ,  A61K45/06 ,  C07C227/16 ,  C07C67/313 ,  C07C69/757 ,  C07C227/04 ,  A61K31/216

摘要： The disclosure relates to cyclopropyl derivatives and methods of use. In some embodiments, the disclosure relates to methods of managing medical disorders with pharmaceutical compositions disclosed herein administered to subject in need thereof. In certain embodiments, the disclosure relates to methods of managing mental disorders, mood disorders, pain, and fibromyalgia and related conditions with pharmaceutical compositions disclosed herein.

公开(公告)号：US10118169B2

公开(公告)日：2018-11-06

申请号：US15129851

申请日：2015-03-30

申请人： The University of Chicago ,  The University of North Carolina at Chapel Hill

发明人： Wenbin Lin ,  Joseph M. Falkowski ,  Takahiro Sawano

IPC分类号： B01J31/16 ,  C07C45/69 ,  C07C231/02 ,  B01J31/18 ,  B01J31/24 ,  C07C227/04 ,  C07C29/44 ,  C07C41/09 ,  C07C67/303 ,  C07D307/93

摘要： Metal-organic framework (MOFs) compositions based on chiral phosphine-, chiral oxazoline-, chiral pyridine-, and chiral diene-derived organic bridging ligands were synthesized and then post-synthetically metalated with metal precursors such as Ru and Rh complexes. The metal complexes could also be directly incorporated into the MOFs. The MOFs provide a versatile family of recyclable and reusable single-site solid catalysts for catalyzing a variety of asymmetric organic transformations, including the addition of arylboronic acids to α,β-unsaturated ketones and alkimines, the hydrogenation of substituted alkene and carbonyl compounds, and cyclization reactions. The solid catalysts can also be integrated into a flow reactor or a supercritical fluid reactor.

公开(公告)号：US20180282259A1

公开(公告)日：2018-10-04

申请号：US15764596

申请日：2016-09-28

申请人： ARKEMA FRANCE

发明人： Thierry BRIFFAUD ,  Jean-Luc COUTURIER ,  Jean-Luc DUBOIS ,  Jean-François DEVAUX

IPC分类号： C07C227/04 ,  C08G69/08 ,  C08G69/04 ,  C07C227/40

摘要： The present invention relates to a composition which comprises at least one α,ω-amino-alkanoic acid or ester and at least one alkanoic ester or acid, characterised in that: the α,ω-amino-alkanoic acid or ester has formula H2N-(CH2)n—COOR, wherein n=9 to 13 and R is an alkyl group or a hydrogen; the alkanoic ester or acid has formula R1-COOR2, wherein R1 is a straight or branched alkyl group with formula CmH2m+1 or CmH2m−3, wherein m=6 to 20 and R2 is an alkyl group or a hydrogen; the molar ratio between the alkanoic acid(s) or ester(s) and the α,ω-amino-alkanoic acid(s) or ester(s) is in the range from 0.001 to 0.4%. The present invention also relates to novel methods for obtaining such a composition.