Patents by Inventor Tsung-Yu Hsiao

Tsung-Yu Hsiao has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20210078956
    Abstract: The present invention provides improved processes for the preparation of elagolix and intermediates thereof. The intermediate of formula VII is achieved by a coupling reaction of a compound of formula V and a N-benzylidene protected compound of formula IV: The present invention is suitable for a large-scale production, avoiding the use of potential genotoxic substances and can be performed under mild conditions.
    Type: Application
    Filed: September 17, 2020
    Publication date: March 18, 2021
    Inventors: Yung-Hung Chang, Tsung-Yu Hsiao, Yuan-Xiu Liao, Hsin-Chang Tseng
  • Publication number: 20200308218
    Abstract: The present invention provides improved processes for purifying liraglutide. Liraglutide is purified via two sequential RP-HPLC purifications followed by a salt-exchange step, where a pH is kept constant in the first and second purification steps. In particular, the processes utilize a halogenated solvent in a sample preparation step, which provides better solubility and an environment suitable for decarboxylation for crude liraglutide prior to a RP-HPLC purification.
    Type: Application
    Filed: March 25, 2020
    Publication date: October 1, 2020
    Inventors: Ming-Chih WU, Hsin-Che HUANG, Tsung-Yu HSIAO
  • Patent number: 10428052
    Abstract: The present disclosure provides efficient, economical, and improved processes for synthesizing lifitegrast and intermediates thereof. The currently discloses processes provide a direct synthetic route, avoiding protection or deprotection steps. The currently disclosed process also provides processes for synthesizing lifitegrast using a reduced number of synthetic steps.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: October 1, 2019
    Assignee: ScinoPharm Taiwan, Ltd.
    Inventors: Ming-Chih Wu, Tsung-Yu Hsiao
  • Publication number: 20190241606
    Abstract: A process for preparing cangrelor tetrasodium comprising: a) reacting a compound of formula M1 with morpholine to form a compound of formula M2; and b) reacting the compound of formula M2 with clodronic acid to provide cangrelor tetrasodium
    Type: Application
    Filed: February 5, 2018
    Publication date: August 8, 2019
    Inventors: Tsung-Yu Hsiao, Chen-Wei Lin, Yu-Hui Huang, Meng-Fen Ho, Kuan-Hsun Wang
  • Publication number: 20190002445
    Abstract: The present disclosure provides efficient, economical, and improved processes for synthesizing lifitegrast and intermediates thereof. The currently discloses processes provide a direct synthetic route, avoiding protection or deprotection steps. The currently disclosed process also provides processes for synthesizing lifitegrast using a reduced number of synthetic steps.
    Type: Application
    Filed: June 29, 2018
    Publication date: January 3, 2019
    Inventors: Ming-Chih WU, Tsung-Yu HSIAO
  • Patent number: 10138215
    Abstract: The present invention provides processes for the preparation of ataluren. Intermediates for preparing ataluren are also provided.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: November 27, 2018
    Assignee: SCINOPHARM TAIWAN, LTD.
    Inventors: Tsung-Yu Hsiao, Yu-Hui Huang, Wei-Yu Chen
  • Patent number: 10118937
    Abstract: A process for making ixazomib citrate of formula VI comprising reacting a compound of formula V with citric acid to form ixazomib citrate of formula VI: wherein R is hydrogen or an amide protecting group.
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: November 6, 2018
    Assignee: SCINOPHARM TAIWAN, LTD.
    Inventors: Tsung-Yu Hsiao, Jyh-Hsiung Liao
  • Patent number: 10100017
    Abstract: Provided herein are novel processes and methods for making 4-[(3-[(4-cyclopropylcarbonyl)piperazin-1-yl]carbonyl)-4-fluorophenyl]methyl(2H)phthalazin-1-one (Olaparib) and intermediates thereof. Olaparib is a poly ADP ribose polymerase (PARP) inhibitor useful in the treatment of cancers. Benefits of the present disclosure include the use of less toxic compounds and improved yields.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: October 16, 2018
    Assignee: SCINOPHARM TAIWAN, LTD.
    Inventors: Tsung-Yu Hsiao, Yung-Hung Chang
  • Publication number: 20180265472
    Abstract: A process for preparing a compound of formula I?: or a pharmaceutically acceptable salt thereof, in which R represents optionally substituted or unsubstituted alkyl group, comprising reacting a compound of formula III: with a carboxylic acid in the presence of a coupling reagent and an organic solvent to obtain the compound of formula I?.
    Type: Application
    Filed: March 8, 2018
    Publication date: September 20, 2018
    Inventors: Tsung-Yu Hsiao, Yu-Hui Huang
  • Publication number: 20180057464
    Abstract: Provided herein are novel processes and methods for making 4-[(3-[(4-cyclopropylcarbonyl)piperazin-1-yl]carbonyl)-4-fluorophenyl]methyl(2H)phthalazin-1-one (Olaparib) and intermediates thereof. Olaparib is a poly ADP ribose polymerase (PARP) inhibitor useful in the treatment of cancers. Benefits of the present disclosure include the use of less toxic compounds and improved yields.
    Type: Application
    Filed: August 23, 2017
    Publication date: March 1, 2018
    Inventors: Tsung-Yu HSIAO, Yung-Hung CHANG
  • Publication number: 20170362192
    Abstract: The present invention provides processes for the preparation of ataluren. Intermediates for preparing ataluren are also provided.
    Type: Application
    Filed: June 19, 2017
    Publication date: December 21, 2017
    Inventors: Tsung-Yu HSIAO, Yu-Hui HUANG, Wei-Yu CHEN
  • Patent number: 9834561
    Abstract: The present invention provides efficient, economical, and improved methods for synthesizing ibrutinib and intermediates thereof. The invention involves a unique biphasic acylation reaction system which advantageously allows for easy separation of ibrutinib from the reaction mixture without additional extraction and wash steps. The isolated ibrutinib formed using the methods described herein can be useful in the preparation of an amorphous form of ibrutinib. In some embodiments, the isolated ibrutinib produced by the processes described herein is a homogenous solution of ibrutinib and DMSO which may be directly used in the formation of the amorphous polymorph. In some embodiments, the isolated ibrutinib is solid ibrutinib. The solid ibrutinib may also be used in the formation of amorphous ibrutinib.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: December 5, 2017
    Assignee: SCINOPHARM TAIWAN, LTD.
    Inventors: Tsung-Yu Hsiao, MengFen Ho, HsinChang Tseng, WenShing Tsao, YuanChang Huang, Wei-Shuo Lo
  • Patent number: 9834533
    Abstract: The present invention provides processes for preparing SGLT2 inhibitors, such as dapagliflozin and empagliflozin.
    Type: Grant
    Filed: February 10, 2017
    Date of Patent: December 5, 2017
    Assignee: ScinoPharm Taiwan, Ltd.
    Inventors: Tsung-Yu Hsiao, Jyh-Hsiung Liao
  • Publication number: 20170240520
    Abstract: The present invention provides processes for preparing SGLT2 inhibitors, such as dapagliflozin and empagliflozin.
    Type: Application
    Filed: February 10, 2017
    Publication date: August 24, 2017
    Applicant: ScinoPharm Taiwan, Ltd.
    Inventors: Tsung-Yu Hsiao, Jyh-Hsiung Liao
  • Publication number: 20170145017
    Abstract: The present invention provides efficient, economical, and improved methods for synthesizing ibrutinib and intermediates thereof. The invention involves a unique biphasic acylation reaction system which advantageously allows for easy separation of ibrutinib from the reaction mixture without additional extraction and wash steps. The isolated ibrutinib formed using the methods described herein can be useful in the preparation of an amorphous form of ibrutinib. In some embodiments, the isolated ibrutinib produced by the processes described herein is a homogenous solution of ibrutinib and DMSO which may be directly used in the formation of the amorphous polymorph. In some embodiments, the isolated ibrutinib is solid ibrutinib. The solid ibrutinib may also be used in the formation of amorphous ibrutinib.
    Type: Application
    Filed: October 27, 2016
    Publication date: May 25, 2017
    Inventors: Tsung-Yu HSIAO, MengFen HO, HsinChang TSENG, WenShing TSAO, YuanChang HUANG, Wei-Shuo LO
  • Patent number: 9309259
    Abstract: The present invention relates to a novel process of making ixabepilone, ixabepilone derivatives and analogues, and intermediates thereof.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: April 12, 2016
    Assignee: SCINOPHARM TAIWAN, LTD.
    Inventors: Yue Chen, Tsung Yu Hsiao, Julian P. Henschke
  • Patent number: 9150615
    Abstract: The invention provides a process for the preparation of leuprolide or its pharmaceutical acceptable salts by a combination of solid phase synthesis and post assembly solution phase amidation. The invention also relates to applying a non-protected leuprolide precursor to prepare leuprolide or its pharmaceutically acceptable salts.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: October 6, 2015
    Assignee: ScinoPharm Taiwan, Ltd.
    Inventors: Tsung Yu Hsiao, Shih Wei Lee
  • Publication number: 20150166602
    Abstract: The invention provides a process for the preparation of leuprolide or its pharmaceutical acceptable salts by a combination of solid phase synthesis and post assembly solution phase amidation. The invention also relates to applying a non-protected leuprolide precursor to prepare leuprolide or its pharmaceutically acceptable salts.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 18, 2015
    Applicant: ScinoPharm Taiwan, Ltd.
    Inventors: Tsung Yu Hsiao, Shih Wei Lee
  • Patent number: 8952139
    Abstract: The present invention provides processes (e.g., arylation reaction) for stereoselectively preparing C-arylglucosides that can be useful as synthetic building block or drugs, including SGLT2 inhibitors.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: February 10, 2015
    Assignee: ScinoPharm Taiwan, Ltd
    Inventors: Julian Paul Henschke, Chen-Wei Lin, Ping-Yu Wu, Chi-Nung Hsiao, Jyh-Hsiung Liao, Tsung-Yu Hsiao
  • Patent number: 8889853
    Abstract: The invention provides an intermediate and the process for making the same. This intermediate is useful in the process for making polysaccharides, and more particularly fondaparinux.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: November 18, 2014
    Assignee: Scinopharm Singapore Pte Ltd.
    Inventors: Tsung Yu Hsiao, Chen Wei Lin