专利号:US-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
专利号:US-8828984-B2 优先权日:2012-11-19 标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection 发明人:CHE CHI MING; ZOU TAOTAO 权利人:UNIV HONG KONG; UNIV HONG KONG 摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.
专利号:US-10577387-B1 优先权日:2018-08-09 标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment 发明人:CHE CHI MING; Fung Sin Ki; Chen tian feng 权利人:UNIV HONG KONG 摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.
专利号:US-8877171-B2 优先权日:2010-02-03 标 题 :Polyanionic multivalent macromolecules for intracellular targeting of proliferation and protein synthesis 发明人:LICHA KAI; SCHIRNER MICHAEL; WELKER PIA; HAAG RAINER; WEINHART MARIE; PAULUS FLORIAN 权利人:LICHA KAI; SCHIRNER MICHAEL; WELKER PIA; HAAG RAINER; WEINHART MARIE; PAULUS FLORIAN; MIVENION GMBH 摘要:The present invention relates generally to methods and compositions for targeting of intracellular molecules involved in proliferation and protein synthesis of activated cells using polyanionic multivalent macromolecules. In particular aspect, multiple sulfate groups linked to polyol are specifically targeted to the cytoplasm and nucleus of proliferating and activated cells. The invention further comprises novel polyanionic macromolecular compounds and formulations.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
1: Choudhary D, Sharma SK, Gupta N, Kharya G, Pavecha P, Handoo A, Setia R, Katewa S. Treosulfan-Thiotepa-Fludarabine-Based Conditioning Regimen for Allogeneic Transplantation in Patients with Thalassemia Major: A Single-Center Experience from North India. Biol Blood Marrow Transplant. 2012 Nov 15. doi:pii: S1083-8791(12)00480-6. 10.1016/j.bbmt.2012.11.007. [Epub ahead of print] doi: 10.1016/j.jpba.2012.10.005. Epub 2012 Oct 16. doi: 10.1016/j.clim.2012.10.003. Epub 2012 Oct 14. Review. doi: 10.1182/blood-2012-04-423822. Epub 2012 May 29. doi: 10.1007/s00432-012-1221-3. Epub 2012 Apr 15. 8: Michallet M, Sobh M, Milpied N, Bay JO, Fürst S, Harousseau JL, Mohty M, Nicolini FE, Labussière H, Tedone N, Morisset S, Vigouroux S, Baumgart J, Tabrizi R, Blaise D. Phase II prospective study of treosulfan-based reduced-intensity conditioning in allogeneic HSCT for hematological malignancies from 10/10 HLA-identical unrelated donor. Ann Hematol. 2012 Aug;91(8):1289-97. doi: 10.1007/s00277-012-1429-y. Epub 2012 Feb 25. doi: 10.1038/bmt.2012.4. Epub 2012 Feb 13. doi: 10.1016/j.jpba.2011.12.021. Epub 2011 Dec 24. doi: 10.1038/bmt.2011.242. Epub 2011 Dec 12. doi: 10.1111/j.1600-0609.2011.01732.x. Epub 2011 Nov 22. doi: 10.3324/haematol.2011.043810. Epub 2011 Jun 9. 14: Chemnitz JM, von Lilienfeld-Toal M, Holtick U, Theurich S, Shimabukuro-Vornhagen A, Krause A, Brossart P, Hallek M, Scheid C. Intermediate intensity conditioning regimen containing FLAMSA, treosulfan, cyclophosphamide, and ATG for allogeneic stem cell transplantation in elderly patients with relapsed or high-risk acute myeloid leukemia. Ann Hematol. 2012 Jan;91(1):47-55. doi: 10.1007/s00277-011-1253-9. Epub 2011 May 17. doi: 10.1038/bmt.2011.88. Epub 2011 Apr 11. Review. doi: 10.1182/blood-2010-10-312082. Epub 2011 Feb 16. Treosulfan-based preparative regimens for allo-HSCT in childhood hematological malignancies: a retrospective study on behalf of the EBMT pediatric diseases working party. Bone Marrow Transplant. 2011 Dec;46(12):1510-8. doi: 10.1038/bmt.2010.343. Epub 2011 Feb 7. doi: 10.1517/13543784.2010.517744. Review. doi: 10.1016/j.bbmt.2010.05.007. Epub 2010 May 26.