Patents by Inventor Koc-Kan Ho
Koc-Kan Ho 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).
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Patent number: 10030034Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.Type: GrantFiled: January 26, 2016Date of Patent: July 24, 2018Assignee: Ligand Pharmaceuticals IncorporatedInventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
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Publication number: 20170334885Abstract: This invention relates to pyrazole compounds or pharmaceutically acceptable salts thereof. Compounds of this invention are inhibitors of methionine aminopeptidase 2 (MetAP2) and dipeptidyl peptidase-4 (DPP-4). MetAP2 is a metalloproteinase that cleaves initiator methionine from nascent peptide emerging from the ribosomes. WO 2010/065879 reports small molecule MetAP2 inhibitors for obesity treatment. DPP-4 inhibitors are an established drug class to improve glycemic control in patients with type 2 diabetes mellitus. Compounds with dual inhibitory activity in both MetAP2 and DPP-4 are desired. The present invention provides novel compounds with dual MetAP2 and DPP-4 inhibitition. These dual inhibitor compounds can be useful in the treatment of a MetAP2 and DPP-4 mediated condition. The present invention provides a compound of the following Formula (I); or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 11, 2016Publication date: November 23, 2017Inventors: Koc Kan Ho, Weiqiang Zhan, Jingye Zhou
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Patent number: 9822101Abstract: This invention relates to pyrazole compounds or pharmaceutically acceptable salts thereof. Compounds of this invention are inhibitors of methionine aminopeptidase 2 (MetAP2) and dipeptidyl peptidase-4 (DPP-4). MetAP2 is a metalloproteinase that cleaves initiator methionine from nascent peptide emerging from the ribosomes. WO 2010/065879 reports small molecule MetAP2 inhibitors for obesity treatment. DPP-4 inhibitors are an established drug class to improve glycemic control in patients with type 2 diabetes mellitus. Compounds with dual inhibitory activity in both MetAP2 and DPP-4 are desired. The present invention provides novel compounds with dual MetAP2 and DPP-4 inhibitition. These dual inhibitor compounds can be useful in the treatment of a MetAP2 and DPP-4 mediated condition. The present invention provides a compound of the following Formula (I); or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 11, 2016Date of Patent: November 21, 2017Assignee: Eli Lilly and CompanyInventors: Koc Kan Ho, Weiqiang Zhan, Jingye Zhou
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Publication number: 20170015631Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: June 15, 2016Publication date: January 19, 2017Inventors: Koc-Kan Ho, Yong Xu, Michael David Saunders, Xiaohui Liu, Scott Albert Pearce, Kevin Bret Wright, Jason Marc Foulks, Kenneth Mark Parnell, Steven Brian Kanner, David Lee Vollmer, Jihua Liu
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Publication number: 20170002014Abstract: The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.Type: ApplicationFiled: July 11, 2016Publication date: January 5, 2017Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael David Saunders, Koc-Kan Ho
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Publication number: 20160347767Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.Type: ApplicationFiled: January 26, 2016Publication date: December 1, 2016Inventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
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Patent number: 9416132Abstract: The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.Type: GrantFiled: July 20, 2012Date of Patent: August 16, 2016Assignee: Tolero Pharmaceuticals, Inc.Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael Saunders, Koc-Kan Ho
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Patent number: 9394257Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: GrantFiled: October 16, 2013Date of Patent: July 19, 2016Assignee: Tolero Pharmaceuticals, Inc.Inventors: Koc-Kan Ho, Yong Xu, Michael David Saunders, Xiaohui Liu, Scott Albert Pearce, Kevin Bret Wright, Jason Marc Foulks, Kenneth Mark Parnell, Steven Brian Kanner, David Lee Vollmer, Jihua Liu
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Patent number: 9266874Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.Type: GrantFiled: December 20, 2013Date of Patent: February 23, 2016Assignee: LIGAND PHARMACEUTICALS INCORPORATEDInventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
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Publication number: 20150344436Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: October 16, 2013Publication date: December 3, 2015Inventors: Koc-Kan Ho, Yong Xu, Michael David Saunders, Xiaohui Liu, Scott Albert Pearce, Kevin Bret Wright, Jason Marc Foulks, Kenneth Mark Parnell, Steven Brian Kanner, David Lee Vollmer, Jihua Liu
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Patent number: 9174984Abstract: The invention is directed to substituted heteroaryl derivatives. Specifically, the invention is directed to compounds according to Formula Q: wherein D, L, M, W, X, Y, and Z are defined herein. The compounds of the invention are inhibitors of DNA methyltransferase (DNMT) activity—including DNMT1, DNMT3a, or DNMT3b—and are useful in the treatment of cancer and hyperproliferative diseases. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: October 23, 2012Date of Patent: November 3, 2015Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITEDInventors: Thomas Francis Hendrickson, Koc-Kan Ho, Michael David Saunders, Brian John Stevens, Krzysztof Swierczek, Kevin Bret Wright
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Publication number: 20140357594Abstract: This invention relates to heteroaryl compounds, containing a purinyl moiety, that inhibit DNA methyltransferase (DNMT) activity—including DNMT1, DNMT3a, or DNMT3b—useful in the treatment of cancer and hyperproliferative diseases.Type: ApplicationFiled: October 23, 2012Publication date: December 4, 2014Applicant: GlaxoSmithkline Intellectual Property (No.2) LimitedInventors: Thomas Francis Hendrickson, Koc-Kan Ho, Michael David Saunders, Brian John Stevens, Krzysztof Swierczek, Kevin Bret Wright
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Publication number: 20140329807Abstract: The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.Type: ApplicationFiled: July 20, 2012Publication date: November 6, 2014Applicant: TOLERO PHARMACEUTICALS, INC.Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael Saunders, Koc-Kan Ho
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Publication number: 20140296204Abstract: The invention is directed to substituted heteroaryl derivatives. Specifically, the invention is directed to compounds according to Formula Q: wherein D, L, M, W, X, Y, and Z are defined herein. The compounds of the invention are inhibitors of DNA methyltransferase (DNMT) activity—including DNMT1, DNMT3a, or DNMT3b—and are useful in the treatment of cancer and hyperproliferative diseases. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 23, 2012Publication date: October 2, 2014Inventors: Thomas Francis Hendrickson, Koc-Kan Ho, Michael David Saunders, Brian John Stevens, Krzysztof Swierczek, Kevin Bret Wright
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Patent number: 8822467Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.Type: GrantFiled: December 14, 2012Date of Patent: September 2, 2014Assignee: Ligand Pharmaceuticals IncorporatedInventors: Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
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Patent number: 8759352Abstract: The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterType: GrantFiled: August 26, 2009Date of Patent: June 24, 2014Assignees: Merck Sharp & Dohme B.V., Pharmacopeia LLC.Inventors: Andrew John Cooke, David Jonathan Bennett, Andrew Stanley Edwards, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Koc-Kan Ho, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer
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Publication number: 20140155379Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.Type: ApplicationFiled: December 20, 2013Publication date: June 5, 2014Applicant: Ligand Pharmaceuticals IncorporatedInventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
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Patent number: 8350043Abstract: Substituted pyridines, pyrimidines, pyrazines, pyridinones, pyrimidinones, pyrazinones and phenylacetamides useful in treating depression, stress and other disorders are disclosed. The compounds are of the formualae: Other embodiments are also disclosed.Type: GrantFiled: June 7, 2006Date of Patent: January 8, 2013Assignee: Pharmacopeia, Inc.Inventors: Jeffrey John Letourneau, Koc-Kan Ho, Michael J. Ohlmeyer, Patrick Jokiel, Christopher Mark Riviello
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Patent number: 8314091Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.Type: GrantFiled: August 19, 2008Date of Patent: November 20, 2012Assignees: MSD OSS B.V., Pharmacopeia, Inc.Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett
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Patent number: 8211927Abstract: The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.Type: GrantFiled: July 31, 2008Date of Patent: July 3, 2012Assignee: MSD, Oss B.V.Inventors: Andrew Laird Roughton, Koc-Kan Ho, Michael Ohlmeyer, Irina Neagu, Steven G. Kultgen, Nasrin Ansari, Yajing Rong, Paul David Ratcliffe, Ronald Palin