Abstract: The present invention provides for synthetic processes for the making of substituted 3-((pyrrol-2-yl)methylene)-2-pyrrolones, including sunitinib. The present invention also provides for a process of crystallizing substantially pure sunitinib L-malate.
Abstract: Provided are systems, apparatus, materials and methods for directly monitoring products and intermediates of solid phase chemical synthesis such as solid phase peptide synthesis.
Type:
Grant
Filed:
October 28, 2011
Date of Patent:
September 16, 2014
Assignees:
ScinoPharm Taiwan, Ltd., National Sun Yat-Sen University
Inventors:
Li-Chiao Chang, Jentaie Shiea, Yi-Tzu Cho
Abstract: A method for screening cells with high level expression of a target protein is disclosed. The method includes introducing into a plurality of host cells a DNA construct that encodes both a target protein and an inhibitor to an endogenous selectable marker in the host cells, screening host cells harboring the DNA construct for the expression of the endogenous selectable marker, and isolating cells with reduced expression of the selectable marker. Also disclosed is a DNA construct configured to express both the target protein and the inhibitor inside the host cell.
Abstract: A process for the preparation of topiramate in an one pot reaction comprises the following steps: A) reacting 2,3:4,5-bis-O-{1-methylethylidene)-?-D-fructopyranose with sulfurylchloride in xylene in the presence of an organic or inorganic base to form 2,3:4,5-bis-O-(1-methylethylidene)-?-D-fructopyranose sulfuryl chloride, B) adding a second organic solvent to the mixture obtained in step A) C) reacting the mixture obtained in step B) with ammonia to form topiramate.
Abstract: A process for preparing a prostaglandin analogue comprising a step of converting a compound of formula (8?): to the prostaglandin analogue, wherein R3 represents hydrogen or a hydroxyl protecting group.
Type:
Grant
Filed:
March 27, 2013
Date of Patent:
June 3, 2014
Assignee:
Scinopharm Taiwan, Ltd.
Inventors:
Julian P. Henschke, Yuanlian Liu, Yung-Fa Chen, Dechao Meng, Ting Sun
Abstract: The present invention provides crystalline forms, including an anhydrate form, of cabazitaxel and processes for the preparation of these forms, designated as Forms C1, C2, C3, C4, C5, C6, C7, C8, C8b, C9 and C9p.
Type:
Grant
Filed:
August 12, 2013
Date of Patent:
May 27, 2014
Assignee:
ScinoPharm Taiwan, Ltd.
Inventors:
Julian Paul Henschke, TsungYu Hsiao, MengFen Ho, YuanChang Huang
Abstract: The present invention relates to processes for making cabazitaxel, cabazitaxel analogues and intermediates thereof. The invention provides novel compounds useful in the synthesis of cabazitaxel.
Type:
Grant
Filed:
October 30, 2012
Date of Patent:
May 13, 2014
Assignee:
ScinoPharm Taiwan, Ltd.
Inventors:
TsungYu Hsiao, Julian Paul Henschke, HsinChang Tseng
Abstract: The present invention provides processes for stereoselectively preparing C-arylglucosides that can be useful as synthetic building block or drugs, including SGLT2 inhibitors.
Abstract: The present invention provides crystalline forms, including an anhydrate form, of cabazitaxel and processes for the preparation of these forms, designated as Forms C1, C2, C3, C4, C5, C6, C7, C8, C8b, C9 and C9p.
Type:
Application
Filed:
August 12, 2013
Publication date:
February 13, 2014
Applicant:
ScinoPharm Taiwan, Ltd.
Inventors:
Julian Paul Henschke, TsungYu Hsiao, MengFen Ho, YuanChang Huang
Abstract: A process for making clofarabine comprising: fluorinating a compound of formula VII wherein each R4 is independently a hydroxy protecting group, OR6 is a leaving group, with a fluorinating agent in the presence of guanidine carbonate to give a compound of formula VIII: wherein R4 is as defined above; and deprotecting the compound of formula VIII to give the clofarabine.
Type:
Grant
Filed:
July 8, 2011
Date of Patent:
February 11, 2014
Assignee:
Scinopharm Taiwan, Ltd.
Inventors:
Julian Paul Henschke, Xiaoheng Zhang, Lijun Mei, Yung-Fa Chen
Abstract: The present invention provides for a method of characterizing and classifying a sample containing a complex molecule, such as a peptide or polypeptide mixture, protein, protein mixture, biologic and biosimilar by using physical analysis, such as mass spectrometry, and statistic methods.
Abstract: A method for screening cells with high level expression of a target protein is disclosed. The method includes introducing into a plurality of host cells a DNA construct that encodes both a target protein and an inhibitor to an endogenous selectable marker in the host cells, screening host cells harboring the DNA construct for the expression of the endogenous selectable marker, and isolating cells with reduced expression of the selectable marker. Also disclosed is a DNA construct configured to express both the target protein and the inhibitor inside the host cell.
Abstract: A method for producing a ?-enriched protected decitabine comprising: a) coupling a protected 2-deoxy-ribofuranose with a protected 5-azacytosine in the presence of a catalyst to form a reaction mixture comprising the protected decitabine of formula I; and b) quenching the reaction mixture of step a) with a base. The ?-enriched protected decitabine so made may be deprotected to produce a decitabine product in a high yield and purity.
Type:
Grant
Filed:
October 2, 2009
Date of Patent:
November 19, 2013
Assignee:
Scinopharm Taiwan Ltd.
Inventors:
Julian Paul Henschke, Xiaoheng Zhang, Jianbo Yu, Kun Hu, Lijun Mei
Abstract: The present invention provides crystalline forms, including an anhydrate form, of cabazitaxel and processes for the preparation of these forms, designated as Forms C1, C2, C3, C4, C5, C6, C7, C8, C8b, C9 and C9p.
Type:
Grant
Filed:
September 6, 2012
Date of Patent:
November 5, 2013
Assignee:
Scinopharm Taiwan, Ltd.
Inventors:
Julian Paul Henschke, TsungYu Hsiao, MengFen Ho, YuanChang Huang
Abstract: The present invention provides a process for making lapatinib and its pharmaceutically acceptable salt by use of new intermediates. A new process for obtaining a pharmaceutical form of lapatinib ditosylate monohydrate is also provided.
Abstract: The present invention provides amorphous forms and the crystalline complexes of SGLT2 inhibitors as a novel material, in particular in pharmaceutically acceptable form. The crystalline forms of SGLT2 inhibitor canagliflozin are designated as Forms CS1, CS2, CS3, CS4 and CS5.
Type:
Application
Filed:
October 30, 2012
Publication date:
September 12, 2013
Applicant:
Scinopharm Taiwan, LTD.
Inventors:
Julian Paul Henschke, Meng-Fen Ho, Shu-Ping Chen, Yung-Fa Chen
Abstract: A process for preparing a prostaglandin analogue comprising a step of converting a compound of formula (8?): to the prostaglandin analogue, wherein R3 represents hydrogen or a hydroxyl protecting group.
Type:
Application
Filed:
March 27, 2013
Publication date:
August 15, 2013
Applicant:
SCINOPHARM TAIWAN LTD.
Inventors:
Julian P. HENSCHKE, Yuanlian LIU, Yung-Fa CHEN, Dechao MENG, Ting SUN